DE102004038285A1 - Use of ethereal oils containing a polymer matrix for the production of drug delivery systems for the transdermal and/or by inhalation application of ethereal oils in aroma therapy - Google Patents

Abstract

Use of ethereal oils for the production of drug delivery systems for the transdermal and/or inhalation application of ethereal oils in aroma therapy, where the system is developed from a polymer matrix comprising e.g. polyisobutylene, containing Cetiol V or castor oil, polyacrylic acid, containing polyvinylpyrrolidone and silicon-, rubber- or styrene block copolymer hot melt matrices. Use of ethereal oils containing a polymer matrix for the production of drug delivery systems for the transdermal and/or per inhalation application of ethereal oils in aroma therapy, where the system is developed from a polymer matrix comprising polyisobutylene, containing Cetiol V or castor oil, polyurethane, polyacrylic acid, containing polyvinylpyrrolidone, silicon-, rubber- or styrene block copolymer hot melt matrices, moisturizing adhesive polymer foil based on polyvinyl alcohol (PVA)/polyacrylic acid (PAS) or gel matrix based on agar agar/PAS, where one or more ethereal oils or their components present are homogeneously distributed in the matrix, and a carrier layer, optionally an impermeable blockade layer for essential oils, optionally one or more permeation-controlling membrane, optionally a detention adhesive layer and a removable protective layer. An independent claim is also included for the use of the drug delivery system as a deodorant or perfume spreader for the improvement of the room air.

Description

The Invention relates to drug delivery systems based on polymer matrices, in particular polyurethane or Polyisobutylenpolymermatrices containing essential oils and their Use in aromatherapy.

Under The term aromatherapy refers to the treatment of different Disorders with essential oils wild or cultivated plants. The beginning of aromatherapy is set to 6000 years before our time and it is considered sure that already Egyptians, Chinese and Indians of North and South America essential oils to cure diseases inserting.

Robert Tisserand published the book "The Art of Aromatherapy" in 1977, which greatly aroused the interest of the public and the industry in aromatherapy, leading to the formation of the Olfactory Research Fund in 1982, which introduced the notion of aroma-chology In contrast to aromatherapy, the aroma-chology is based on scientific data obtained under controlled conditions, with the help of which data are verifiable statements about the effects of the essential oils possible.For more information on aromatherapy can also be found in US 6280751 ,

The Education and the occurrence of essential oils, the used in the context of aromatherapy, takes place in the Scroll, the flowers, the fruits, the roots, the rhizomes, the woods and the bark of various plants. They can be used in all tissues Plant occurrences (e.g., conifers) or are strict on particular plant parts limited (e.g., cinnamon tree: leaves and bark, peppermint: stems and leaves, citrus plants: flowers and Pericarp). Most and most important essential oils come in higher plants Pinaceae family, Lauraceae, Myrtaceae, Rutaceae, Lamiaceae, Apiaceae, Zingiberaceae, Piperaceae and Brassicaceae.

Under essential oils understands Plant-derived essences that are mainly used as natural raw materials the drug, perfume and food industry. Often the term essential oils is still used for that contained in the plants, volatile Ingredients used. In the true sense, however, essential oils are understood a mixture of volatile Components made from vegetable raw materials. In Typically, essential oils make mixtures several chemical compounds (e.g., menthol, anisaldehyde, geraniol, Citral, camphene, pinene, borneol, eugenol and bergapten), where represent the major components of these compounds with 90% terpenes. As other chemical structures found in the essential oils, are phenylpropane derivatives, simple phenols and their ethers, phenolcarboxylic acids, straight chain Hydrocarbons and their derivatives, short-chain acids, sulfur-containing Compounds (mustard oils) and nitrogen-containing substances.

at dominated by some essential oils an ingredient (for example, 85% eugenol in clove oil) while other essential oils are complex compound mixtures of a large number of individual components represent. Many of the commercially important essential oils work the number of identified components in the hundreds. Many many Ingredients of the essential oils are chiral, very often one enantiomer predominates or exclusively present is. As an example (-)-Menthol in peppermint oil or (-) - linalyl acetate in lavender oil to be named. The boiling point of the volatile constituents of the essential oils lies usually between 150 and 300 ° C. Go on the other side the essential oils due to their high vapor pressure even at significantly lower temperatures, below body temperature, from the liquid in the gaseous Condition over. This is used in aromatherapy with drug delivery systems, during the application of the essential oils through the breathing air takes place.

A list of other essential oils will be available in US 6280751 and US 5716928 disclosed.

The application of aromatherapy is usually carried out by a massage with essential oils, an addition of the essential oils to a bath, a distribution of essential oils in a room (evaporation of oils, room spray) or by inhalation. Since essential oils contain their active ingredients in a high concentration, there is the danger of overdosing in the described applications of the essential oils, which leads to more or less serious side effects, as disclosed in WO 98/17262. The use of inhalation should be considered as particularly critical as there is a risk that higher concentrations of the essential oils may come in contact with the mucous membranes of the face, especially the eyes, which may result in damage requiring medical treatment. Therapy must therefore be performed with diluted essential oils. The dilution is carried out either by the addition of the essential oils in an aqueous medium or the preparation of a mixture of essential oils and carrier oils. Carrier oils are therapeutically neutral, vegetarian oils, which include almond oil, peanut oil, grapeseed oil, evening primrose oil, avocado oil, castor oil, diest oil, wheat germ oil and sesame oil DE 4125562 and WO 98/17262. Some side effects and poisoning associated with the use of essential oils during aromatherapy are listed in the following table. These are to be observed in particular in case of abuse, improper use (overdose or too long use) or the use of oils which do not meet the purity requirements.

at the implementation Aromatherapy should be avoided due to the use of essential oils too pronounced Adverse effect on injury lead the patient could.

task Therefore, it is a possibility of aromatherapy in the present invention ready with essential oils to provide, which helps to avoid the listed disadvantages.

• – der Body Treatment Apparatus, der zur Massage des Körpers mit ätherischen Ölen eingesetzt wird, wie er in WO 01/03637 beschrieben ist,
• – rotierende Behälter, in denen durch die Rotation ein Flüssigkeitsfilm entsteht, der eine starke Verdunstung der ätherischen Öle zur Folge hat ( DE 19925273 ),
• – ätherisches Öl haltige Aroma Delivery Devices, die als hufeisenförmiger Nasenclip im Bereich der Nasenschleimhaut appliziert werden (WO 01/23024) und
• – der Aromatherapy Scent Dispenser ( US 6102300 ).

For the application of aromatherapy, a number of devices for the application of essential oils have been developed. examples are

• The body treatment apparatus which is used to massage the body with essential oils, as described in WO 01/03637,
• - Rotating containers in which the rotation creates a liquid film which results in a strong evaporation of the essential oils ( DE 19925273 )
• - Aroma Delivery Devices containing essential oil, which are applied as a horseshoe-shaped nose clip in the nasal mucosa (WO 01/23024) and
• - the Aromatherapy Scent Dispenser ( US 6102300 ).

Drug delivery systems are plaster-like dosage forms that contain the active ingredient in a reservoir called a matrix, which is usually made up of polymeric substances. The application of the drug delivery system takes place on the surface of the skin, where the active ingredient is released over a longer period by diffusion in the area of the matrix in order subsequently to reach the site of action by transdermal diffusion or by inhalation. Because of these properties, the drug delivery systems are able to provide the organism with a constant amount of active ingredient per unit of time over a long period, regardless of the drug concentration in the reservoir, and are therefore assigned to the group of sustained-release medicines. WO 01/39752 and WO 98/17262 describe such drug delivery systems. Due to the properties of the drug or the drug delivery system, the active ingredient can reach different locations of the organism. For this reason, the drug delivery systems in the two Divided into groups of topical and transdermal delivery. The topical formulations contain agents whose release and action is limited to the area directly below and the site of application. The transdermal formulations, on the other hand, contain active ingredients which diffuse through the skin in order subsequently to produce an effective active ingredient level through the penetration into the vascular system in the entire organism.

• • Die Drug Delivery Systeme, die eine diffusionskontrollierte Freisetzung des Wirkstoffs aufweisen, wie beispielsweise in 1a dargestellt, bestehen aus einer Matrix, in welcher der Wirkstoff enthalten ist. Die Wirkstofffreigabe erfolgt bei diesem System aufgrund der Diffusionseigenschaften des Wirkstoffs im Bereich der Matrix.
• • Bei einer membranpermeationskontrollierten Freisetzung wird die Freisetzung des Wirkstoffes über die Eigenschaften einer Membran gesteuert, wodurch eine konstante Freigabe des Wirkstoffs pro Zeiteinheit und eine hohe Dosiergenauigkeit gewährleistet werden, wie es beispielsweise 1b zeigt. Die Membran hat nichtporöse, mikroporöse oder semipermeable Eigenschaften, durch die die Freisetzung des Wirkstoffes reguliert wird. Als Membranen werden zum Beispiel Polypropylen, Polyvinylchlorid, Celluloseacetat oder Ethylen/Vinylactat-Copolymer eingesetzt. Als Nachteil dieses Systems ist das Dose dumping, eine schlagartige Freisetzung des Wirkstoffs, bei einer mechanischen Beschädigung der Membran zu nennen. Die Folge wäre eine Wirkstoffüberflutung des Organismus und unter Umständen eine deutliche Überschreitung der toxischen Konzentration mit entsprechenden Folgen.

In the course of the development of the drug delivery systems, different models were developed, with which a controlled release of the drugs over a long time interval and thus a sustained release effect was made possible. As examples may be mentioned the drug delivery systems with a matrix diffusion controlled release or drug delivery systems with a membrane permeation controlled release.

• • The drug delivery systems, which have a diffusion-controlled release of the drug, such as in 1a shown, consist of a matrix in which the active ingredient is contained. The drug release occurs in this system due to the diffusion properties of the drug in the region of the matrix.
• • In a membrane permeation-controlled release, the release of the active ingredient is controlled by the properties of a membrane, whereby a constant release of the active ingredient per unit time and a high dosing accuracy can be ensured, as for example 1b shows. The membrane has nonporous, microporous or semipermeable properties that regulate the release of the drug. The membranes used are, for example, polypropylene, polyvinyl chloride, cellulose acetate or ethylene / vinyl acetate copolymer. A disadvantage of this system is the can dumping, a sudden release of the drug, to call mechanical damage to the membrane. The consequence would be a drug over-saturation of the organism and under certain circumstances a clear exceeding of the toxic concentration with corresponding consequences.

The Application of essential oils in the course Aromatherapy can be transdermally and / or as previously described done with the breath. The controlled, over a long time interval sustained release of the essential oils from the Drug delivery systems is controlled by the use of systems with matrix diffusion or membrane permeation-controlled release of the active ingredients achieved as described in WO 98/17262.

WO 01/39752, whose aim is a controlled, sustained release of volatile substances from drug delivery systems, can be given as an example for drug delivery systems in whose active ingredient reservoir essential oils have been integrated. The active ingredients described in WO 01/39752 are the essential oils eucalyptus oil, pine oil, mountain pine oil, turpentine oil, nutmeg oil, pine needle oil, cedarwood oil and their ingredients menthol, thymol, camphor, limonene, borneol, camphene, α-pinene, β- Pinene, bornyl acetate, α-phellandrene, β-phellandrene, cardinen and 1,8-cineol. Further documents describing drug delivery systems are WO 01/78691, which describes the release of eucalyptus oil, turpentine oil, menthol and thymol from a matrix for the treatment of colds, and DE 19712359 which reproduces the release of volatile active substances such as aniseed oil, fennel oil, eucalyptus oil, turpentine oil, pine needle oil, peppermint oil, menthol, camphor or a mixture of these substances for application by inhalation with the elimination of transdermal uptake. WO 00/16752 deals with the invention of drug delivery systems whose matrices are composed of natural (inter alia chitosan, chitin, shellac, cyclodextrins) and synthetic (inter alia acrylates, silicones) polymers for use in aromatherapy. The use of essential oils of plant anise, bergamot, black pepper, chamomile, peppermint, lavender, coriander, cinnamon, ginger, lemon, jasmine, camphor, eucalyptus, lemon balm, thyme, marjoram, oregano, hazelnut, orange, angelica, cypress, According to WO 00/16752, Roman chamomile and many others make it possible to produce drug delivery systems which are used for the treatment of inflammations, insect bites, allergic reactions, burns, eczema, acne, dry or fat skin, abrasions, incisions, hematomas, fatigue, Headache and muscle tension are suitable. Another patch that releases the active ingredients Oleum Menthae pip., Oleum Eucalyptus and Oleum Pini, is after DE 3540515 by an application below the nose and the inhalation of the oils able to prevent the snoring. GB 2369055 however, it describes a Essential Oil Energy Patch that allows diffusion of the essential oil into the skin.

• • Die Zahl der Wirkstoffe, die mit dieser Darreichungsform ausreichend hohe Blutspiegel oder Konzentrationen im Bereich der Derma erzeugen, um im Organismus einen pharmakologischen Effekt zu erzielen, ist sehr gering.
• • Die Wirkung tritt, bedingt durch die zunächst notwendige Hautsättigung mit dem Wirkstoff, erst mit einer gewissen Verzögerung ein.
• • Im Bereich der Haut können aufgrund von Bestandteilen der Drug Delivery Systeme allergische Reaktionen ausgelöst werden.
• • Drug Delivery Systeme können insbesondere bei längerer Anwendung am gleichen Applikationsort Schäden im Bereich der Haut auslösen. Aus diesem Grund sollten die Drug Delivery Systeme lediglich im Bereich von Hautarealen appliziert werden, die gesund und intakt sind.

On the other hand, the known drug delivery systems have some disadvantages:

• • The number of active substances that generate sufficiently high blood levels or concentrations in the area of the derma in order to achieve a pharmacological effect in the organism with this dosage form is very low.
• • The effect occurs, due to the initially necessary skin saturation with the active ingredient, only with a certain delay.
• • In the area of the skin, allergic reactions may be triggered due to components of the drug delivery systems.
• • Drug delivery systems can cause damage to the skin, especially after prolonged use at the same application site. For this reason, the drug delivery systems should only be applied in areas of skin that are healthy and intact.

A Another object of the present invention is therefore a drug Delivery system to provide that a controlled and timed variably adjustable release of essential oils via the ambient air and / or allows transdermal, without causing irritation of the mucous membranes or the skin.

at the active ingredient-containing plaster systems that are on the skin for an extended period of time remain, of course, a main focus also on the skin compatibility the adhesive matrices. It is expected to be skin-friendly, good Adhesiveness especially about a longer one Application period, and a painless, residue-free removal of the Pavement guaranteed. Of many known adhesives, such as rubber, acrylates, silicones, Resins or styrene hydrocarbons, in particular to a Improvement of the adhesive properties will be used, this Expectation not fulfilled. These known adhesive substances lead often to the appearance of skin irritations, allergies, macerations and / or a painful detachment of the plaster from the skin.

Further Object of the present invention is therefore an active ingredient Paving systems ready to provide that the required properties of the adhesive matrices, i. a skin-friendly, long-lasting Bonding guaranteed and painless and residue-free removable is.

Active substance Plaster for The transdermal application is widely used in the literature and described in patents. The use of polyurethanes for controlled However, drug delivery is only known in a few cases (Lamba, Woodhouse, Cooper, "Polyurethanes in Biomedical Applications ", CRC Press, 1998, p. 240).

In EP 0 057 839 A1 Polyurethane gels, in which various active ingredients are incorporated, are described. These medicines are carriers of active substances with which a depot effect and thus the long-term supply of the active substance to the patient is achieved. Furthermore, WO 91/02763 A1 and WO 94/22934 A1 are concerned with the compositions of polyurethane-urea-based hydrogels which serve for the controlled release of active substances from the hydrogels.

In GB 2283750 Polyurethane foams containing aromatic substances are described. In the course of the work, aliphatic, cycloaliphatic and aromatic polyisocyanates were used. As compounds used for the preparation of the polyisocyanates are 2,4- and 2,6-methylcyclohexylene diisocyanate, tetramethylene diisocyanate, cyclohexane diisocyanate, naphthalene-1,5-diisocyanate, 1-methoxyphenyl-2,4-diisocyanate, 4,4 'Diphenylmethane diisocyanate, combination of the 4,4'- and 2,4-diphenylmethane diisocyanate and polymeric polyisocyanates such as polymethylene polyphenylene polisocyanate called. The aim of this work was the development of a method to determine the hardness of the polyurethane foam as a function of the integration of various flavoring agents into the polymer. Among the flavors are eugenol, geraniol, limonene and eucalyptol, which are essential oils.

The Delivery of active ingredients from polyurethane-based systems to the ambient air is not described in the patents. The known active ingredient-containing polyurethanes, in the cited Publications are described, are also products that no have self-adhesive properties.

The development of drug delivery systems with polyisobutylene was already in 1983 in DE 3347278 and DE 3347277 described. However, for these drugs, a combination of the polyisobutylene with olefinic diene rubbers or tackifier resins had to be performed to obtain sufficient adhesive properties. The two substances have a high allergic potential, so that the application of the appropriate drug delivery systems in many patients would lead to side effects. The representation of a drug delivery system made of polyisobutylene, with which the patient nicotine is administered, takes place in WO 96/22083. In order to enable a long-term use of this drug delivery system, the use of adhesive resins had to take place, which in turn would cause allergic reactions. US 4559222 On the other hand, it reflects the description of drug delivery systems whose adhesive properties are achieved without the addition of adhesive resins. On the other hand, the corresponding formulations contain a large proportion of mineral oils, the ratio of polyisobutylene to mineral oil min at least 1. The disadvantage of the high mineral oil content is that only those active ingredients can be incorporated into the drug delivery system, which have sufficient solubility in mineral oil. EP 1120115 provides information on a skin-friendly drug delivery system for the transdermal application of nonsteroidal anti-inflammatory drugs. According to this patent, it is possible to produce drug delivery systems with a polyisobutylene matrix without the need for addition of tackifier resins or mineral oils in order to obtain sufficient adhesive properties and solubility of the active ingredients. It describes a formulation for the production of drug-containing drug delivery systems, which are composed of a flexible cover layer and a drug-containing, pressure sensitive matrix. In addition to the polyisobutylenes, amorphous poly-α-olefins are another constituent of the formulations. On the properties of poly-α-olefins is in US 4186258 . US 5262216 and WO 98/54268, which specifically reflects the use of poly-α-olefins in the field of human skin. Furthermore, the addition of insoluble, hydrophilic fillers takes place after EP 1120115 responsible for increased skin friendliness of the drug delivery systems.

The The aim of the present invention is also drug delivery Systems with an adhesive resin and mineral oil-free polyisobutylene matrix to be able to develop a sustained release to allow of essential oils.

One Problem in the production of transdermal therapeutic systems is the introduction of polar active substances in the mostly non-polar polymer matrices. Thereby can preferred agents sometimes poor or limited Concentration to be incorporated into the polymer matrix. Furthermore There is a risk that due to the different polarity and insolubility the active ingredients in the polymer matrix the active ingredients over time crystallize out of the polymer system. A long-term stability is not always guaranteed.

Be solved the diverse ones Tasks through the use of a drug delivery system, i. with a plaster-like dosage form, according to the main claim. object the dependent claims are advantageous embodiments of the system according to the invention.

It was surprising and for the expert does not foresee that the use of an essential oil containing Polymer matrix for the production of drug delivery systems for transdermal and / or by inhalation application of essential oils in aromatherapy the Solves tasks.

The use according to the invention includes an essential oil-containing Polymer matrix for the production of drug delivery systems for transdermal and / or by inhalation application of essential oils in aromatherapy.

• – Polymermatrix umfassend • Polyisobutylen, enthaltend Cetiol V oder Rizinusöl, • Polyurethan, • Polyacrylsäure, enthaltend PVP, • Silikon-, Kautschuck- oder SBC-hotmelts-Matrices, • feuchtklebende Polymerfolie auf PVA/PAS-Basis oder • Gelmatrix auf Agar Agar/PAS-Basis, wobei in der Matrix ein oder mehrere ätherische Öle oder deren Bestandteile homogen verteilt vorliegen, und
• – einer Trägerschicht,
• – gegebenenfalls einer für ätherische Öle undurchlässige Blockadeschicht,
• – gegebenenfalls einer oder mehrerer permeationskontrollierenden Membranen,
• – gegebenenfalls einer Haftklebeschicht und
• – einer abziehbaren Schutzschicht.

The system is composed of a

• Polymer matrix comprising polyisobutylene containing Cetiol V or castor oil, polyurethane, polyacrylic acid containing PVP, silicone, rubber or SBC hotmelts matrices, wet-adhesive PVA / PAS-based polymer film or gel matrix on agar agar / PAS-based, wherein in the matrix one or more essential oils or their components are homogeneously distributed, and
• A carrier layer,
• - optionally a blockade layer impermeable to essential oils,
• Optionally one or more permeation controlling membranes,
• Optionally a pressure-sensitive adhesive layer and
• - a peelable protective layer.

Of the Advantage of the drug delivery system consists in a controlled Release of the essential oils over one longer Period without the risk of overdosing with essential oils.

In aromatherapy to use essential oils in the system of the invention can diverse chosen as described below.

terpenes are hydrocarbons, alcohols, esters, oxides, aldehydes, Ketones and ethers in front. Structurally, they can be subdivided into the following basic types:

• Monoterpenes:

2. Monocyclische Monoterpene: a) Kohlenwasserstoffe:

b) Alkohole und Phenole:

c) Ketone:

d) Aldehyde und Oxide

3. Bicyclische Monoterpene:

They are derived from 2,6-dimethyloctane or geraniol and are assigned to the acyclic, mono- or bicyclic series. 1. Acyclic monoterpenes:

2. Monocyclic monoterpenes: a) Hydrocarbons:

b) Alcohols and phenols:

c) ketones:

d) aldehydes and oxides

3. Bicyclic monoterpenes:

Sesquiterpenes:

she are derived from 2,6,10-trimethyl-n-dodecane or farnesol. you distinguishes between acyclic, monocyclic, bicyclic and tricyclic Sesquiterpenes.

• phenylpropane derivatives:

To include the phenylpropane derivatives Aldehydes, phenols and phenolic ethers, directly from the cinnamic acid derived. They are e.g. in some Apiaceen oils, in Peru balsam as well as in Cinnamon and clove oil contained in high concentrations.

Another way to classify the essential oils is their assignment to groups with certain therapeutic effects. Thus, for example, the essential oils for the treatment of pain, rheumatism, bronchitis, sleep disorders, headaches and migraines, skin problems, fears, depression, infections, back pain, stress, indigestion can be divided into individual groups. The following table gives some examples of the classification of plants according to the pharmacological action of their essential oils:

Around a connection between the essential oils and aromatherapy, the following are the composition and the pharmacological effects of essential oils are shown:

• Oleum Lavandulae:

The Effectiveness of lavender oil based on the ingredients linalyl acetate 20 - 55% (a), linalool 20 - 35% (b), Cineole (small amounts), camphor (small amounts), ocimen (small Amounts) and caryophyllene epoxide (small amounts), which are from the parent plant Lavendula angustifolia are obtained. (Pharmaceutical biology drugs and their ingredients, Gustav Fischer Verlag, Stuttgart).

The oil is used as a mild-acting antidepressant and sedative in restlessness, nervous exhaustion and sleep disorders. Its effect is due to a calming of the central nervous system attributed the release of the neurotransmitter serotonin. The active ingredients for this effect are the main ingredients linalyl acetate and linalool.

lavender belongs Furthermore to the group of medicines used to cure burns, Insect bites, minor cuts, bruises and abrasions be used.

• Oleum rosemary:

The essential oil of rosemary, which is made from the parent plant Rosmarinus officinalis contains as main components 1,8-cineol 15-30 % (a), camphor 15 - 25 % (b), α-pinene up to 25% (c) and as further constituents u. a. Camphen, Borneol and limes.

The Rosmarienöl is suitable for the treatment of muscle pain and muscle cramps.

While the oil at nervous tension balancing already in low dosage is to compensate of exhaustion and increase self-confidence to apply a high dosage (new Aromatherapy - Health and well-being through essential oils, vgs Publishing company, Cologne).

• Oleum Menthae:

to Preparation of the essential oil of peppermint the parent plants Mentha piperita and Mentha arvensis are used. The ingredients of peppermint oil are (-) - menthol 50 - 78% (a), Ester of menthol 5 - 20 %, (-) - menthone 10 - 20 % (b), menthofuran 2,5 - 5 % (c) and Jasmon 0.1%.

Peppermint oil has gone through its refreshing effect has a positive effect on fatigue and Difficulty concentrating. Further therapeutic effects of the oil are used to treat the Hypotension and travel sickness used.

The by far the most important indication, however, is the use of the oil in tension headaches and migraine. Recently, systematic investigations of the neurology of university Kiel on the use of peppermint oil in tension headaches in front. In the course of these studies were placebo-controlled studies with 105 patients over episodic tension headaches complained. The Results provided evidence that the peppermint oil release of painkillers (e.g., serotonin) in the brain, has a relaxing effect on the muscles, an increase in the Circulation of the aching muscle causes and the pain reflexes and reduces sensitivity to pain. The application of the oil takes place by large-scale application in the area of the forehead and temples. If the treatment instructions There are between the effectiveness of a painkiller like 1 g paracetamol or 1 g acetylsalicylic acid and the peppermint oil none Difference. A combination of peppermint oil and paracetamol has after 60 minutes of application the best headache relieving Effect (doctors Newspaper - online, 06.03.2002).

• Oleum Pini Pumilionis:

The essential oil of pine, which is obtained from the parent plant Pinus pumilio contains as main components α-phellandrene (a) and β-phellandrene (b) 60%, α-pinene (c) and β-pinene (d) 10-20 % and bornyl acetate 10% (e).

Pine needle oil is added Diseases are used in the respiratory tract, whose Cause infections, asthma, sinusitis and bronchitis are. Pharmacological effect of oil based here on an ejection of the mucus (mucus) from the area the trachea and the paranasal sinus, which allows free breathing becomes.

Next These indications may be pine oil for the treatment of muscle and joint pain with sore muscles, arthritis, and rheumatism following muscle spasms be used. Furthermore is the pine needle oil like the peppermint oil able to stimulate circulation and blood pressure during hypotension to increase.

• Oleum Caryophylli:

The clove oil is from the parent plant Syzygium aromaticum (or Caryophyllus aromaticum) and contains mainly Eugenol 85 - 95 % (a) and a few eugenol acetate (b), α-caryophyllene (c) and β-caryophyllene (d) (Tea Drugs and Phytopharmaceuticals, Scientific Publishing Company mbH, Stuttgart).

Because of its local anesthetic and disinfectant action, oil and eugenol are used in dentistry to kill the tooth nerve, disinfect the root canal, and as a local pain-reducing agent in inflamed or hypersensitive pulp. To treat the pain in the In the area of the muscles and joints, the clove oil is used because of its anti-inflammatory effect. The antiphlogistic effect of eugenol and aceteugenol is due to an inhibition of prostaglandin synthase, which is critically involved in the course of inflammation.

• Oleum Aurantii:

The orange oil contains the ingredients linalyl acetate 8 - 25% (a), limonene (b) and Terpene alcohols obtained from the parent plant Citrus aurantium become.

oleum Aurantii becomes a release of physical Tension and promotion used in the circulation and is therefore suitable for treatment of pain in the area of the musculature. On the psyche, the oil has one relaxing and at the same time mood-enhancing effect, that too an optimistic mood and helps to calm nervousness, so that the oil the fruit peel frequently is used as a calming component in therapy. Another treatment option arises from the appetizing and digestive Effect of the orange oil, those with nutritional problems can be applied.

in the The field of cosmetics Oleum Aurantii finds to care for dry, Cracked and irritated skin, to support the regenerative ability the skin, to protect the skin from dehydration, to soften the brittle and keratinized skin and in the treatment of orange peel Application.

• Oleum Citri:

The essential oil of lemon, which is made from the parent plant Citrus limonum contains limonene 90% (a), citral 3 - 5 % (b), citronellal (c), α-terpineol (d), linalyl acetate (e) and geranyl acetate (f).

The lemon oil is awarded an increase in the body's defenses. For this reason, the oil is used for the prevention and treatment of colds. Furthermore, Oleum Citri has a disinfecting and anti-inflammatory effect, which can also be used therapeutically. In the form of compresses, the oil quenches the itching in eczema or rashes. On the psyche the lemon oil has a psycho-stimulating effect, which leads to an increase in efficiency and concentration triensvermögens leads.

In In cosmetics, Oleum Citri is used to care for fat, blemished skin and used for the treatment of acne.

• Oleum Bergamottae:

The bergamot is derived from the parent plant Citrus bergamia and contains the active ingredients Limonene 50% (a), linalyl acetate 35-45% (b), linalool (c) 20-30%, Geraniol (d) and nerol (e). Characteristic of the oil of Citrus bergamia is the 5% relatively high bergapten content (5-methoxy-furanocoumarin).

oleum Bergamottae is used in diseases of the skin, to the appearance of acne and impure, oily skin too improve. Furthermore, the oil has a balancing effect on the mental state, which a reduction of stress and a mood-enhancing effect achieved become. In many cases the use of bergamot oil is due to a soothing and compensatory effect as a sleep aid.

For the perfumery is Bergamot among the oils the citrus family the most significant. It has been one for centuries concisely Part of the "cologne water". With a share from 20 - 30 % provides the bergamot oil in addition to citron, orange blossom, Lavender and rosemary oil the main ingredient the classical "cologne water" composition dar. In addition to its importance in the perfumery industry plays the oleum Bergamottae a role in the liqueur and sugar confectionery. Famous has become the tea variety "Earl Gray "by the Addition of this essential oil, the the "cooling" and encouraging Effectiveness of the tea causes.

• Oleum Thymi:

The Effectiveness of thyme oil is based on the ingredients thymol 25 - 50% (a), carvacrol 3 - 10% (b) and other monoterpenes such as p-cymene, γ-terpinene, linalool, camphor and limonene. The oil is going out the parent plant Thymus vulgaris won.

The thyme oil acts due to its thymol / carvacrol content still in a concentration from 1: 3000 inhibiting most bacteria. This results in an extremely broad spectrum of action in infectious diseases. As another Indications are diseases of the bronchial area such as bronchitis, To name asthma, catarrh of the upper respiratory tract and whooping cough, there thyme oil internally a secretomotor, secretolytic, antiseptic, shows antibacterial and spasmolytic activity. The application as an expectorant and bronchospasmolytic is by the direct Influence of the oil caused to the bronchial muscles. The antiseptic and antibacterial effect is due to the thymol.

Further it is possible Oleum Thymi for the treatment of headaches and muscle aches use.

Based These descriptions will clearly show how many indications go through the essential oils covered be and how versatile the oils can be used in the therapy of patients, without that when used after determination with strong side effects expected must become. It can be an increase in the effect of the simultaneous administration of different essential oils, which is an identical indication have to be achieved. In addition to the oils described in detail in the aromatherapy with the aid of the drug delivery system according to the invention u.a. following essential oils and Ingredients of essential oils used Oleum Abietis albae, Oleum Angelicae, Oleum Anisi, Oleum Artemisiae, Oleum Aurantii Floris, Oleum Basilici, Oleum Betulae, Oleum boswelliae, oleum Calendulae infusum, Oleum camphoratum, oleum Canarii, Oleum Capsici, Oleum cardamomi, Oleum Carvi, Oleum Chamomillae, Oleum Cinnamomi ceylanici, Oleum Citronellae, Oleum Coriandri, Oleum Cupressi, Oleum Cymbopogonis, Oleum Eucalypti, Oleum Foeniculi, Oleum Jecoris, Oleum Juniperi, Oleum Lauri, Oleum Limonis, Oleum Macidis, Oleum Majoranae, Oleum Melaleucae viridiflorae, Oleum Melissae, Oleum Millefolium, Oleum myristicae, Oleum myrrhae, Oleum myrtle, Oleum Orthosiphonis, Oleum Pelargonii, Oleum Petroselini, Oleum Piceae, Oleum Salviae, Oleum Pini Pumilionis, Oleum Pini sibricum, Oleum Pini silvestris, Oleum Piperi nigri, Oleum Rosae, Oleum Salviae, Oleum Santali, Oleum Terebinthinae rectificat, Oleum Valerianae, Oleum Zingiberis, Myrrha and Camphora, Borneol, Cineol, Citronellal, Citronellol, eugenol, camphor, limonene and / or menthol.

The essential oils and their Active ingredients have physicochemical properties that are good transdermal Diffusion of the oils cause it to be very good for the production of systems that have transdermal delivery, are suitable. On a use of enhancers, a term below the substances that are able to pass through different interactions with the active substance, the adhesive layer, the membrane that controls the release of the drug, the Matrix polymer and / or the skin improved and accelerated Penetrating the drug into the epidermis may be due to to dispense with this property.

The essential oils or their components are in the drug delivery system in a concentration range from 0.1 to 20.0 % By weight, preferably from 5 to 10% by weight, based on the polymer matrix, used.

Since most of the essential oils already have a high vapor pressure in the area of body temperature, in addition to the transdermal application, application of the essential oils to the respiratory air can be carried out by the drug delivery systems in the area of the breast, as in 2 is shown, or applied below the nose to ensure sufficient proximity to the respiratory system. Due to the polymer matrix according to the invention described below and the structure of the system, damage to the skin and above all to the mucous membranes is excluded.

Furthermore, it is possible to produce drug delivery systems in which the application of the essential oil is carried out simultaneously transdermally and by inhalation. The application of these drug delivery systems causes a combined absorption of the active substance into the organism, which leads to an accelerated dripping of the drug in the body ( 3 ). For indications of the lung such as Bronchitis or asthma also has the advantage that two different therapeutic effects occur at the same time, since the active ingredients of the essential oils in the area of the stomach and the lungs contribute to an improvement of the symptoms through different mechanisms of action. Another possibility for the application of aromatherapy is the release of the essential oils from the drug delivery system into a closed room in which the patient absorbs the essential oils with the respiratory air and thereby achieves a therapeutic effect.

Is possible also that the Drug Delivery systems not only used for therapeutic purposes but also improve the indoor air or deodorization be placed in the room or on the clothes.

The application of the essential oils in the course of an aromatherapy can be carried out as already described transdermally and / or with the respiratory air. The controlled sustained release of the essential oils from the drug delivery systems over a long time interval is achieved through the use of systems with matrix-diffusion-controlled or membrane-permeation-controlled release of the active ingredients. The 1 depicts the two systems based on the release of the essential oils into the respiratory air and the transdermal area. When the essential oils are taken in with the respiratory air, the application of the drug delivery systems takes place, for example, in the chest area of the patient ( 2 ) or around the nose to ensure sufficient proximity to the respiratory system. In the course of treatments where the release of the essential oils is transdermal only, the drug delivery systems should be used at the site of the complaint to give the patient the feeling that he is actively engaged in a cure.

The essential oils or their constituents are released from drug delivery systems transdermally and / or by inhalation, wherein a combination of diffusion-controlled, membrane permeation-controlled or blocked release can take place, as described in US Pat 6 is shown. The following possibilities arise:

• • Der Patient wird im Gegensatz zu den bereits beschriebenen Anwendungsarten, bei denen die freigesetzte Menge des Wirkstoffs in Abhängigkeit von der Applikationszeit deutlich abnimmt, über einen langen Zeitraum mit einer kontrollierten Menge der ätherischen Ölen pro Zeiteinheit versorgt. Das bedeutet, dass mit Hilfe dieser Applikationsform der therapeutische Effekt der ätherischen Ölen über einen langen Zeitraum konstant gehalten wird, ohne dass eine Unterbrechung der Behandlung auftritt. Die Behandlung einer Indikation kann so über den Verlauf des gesamten Tages und/oder der gesamten Nacht durchgeführt werden. Aufgrund dieser Eigenschaften des Drug Delivery Systems ergibt sich bei den Patienten eine deutlich höhere Compliance.
• • Ein Problem der Salbenapplikation besteht in der Kontamination der Hände mit schleimhautreizenden ätherischen Ölen. Um einen Augenkontakt zu vermeiden, ist es unerlässlich, dass der Patient sich nach der Anwendung die Hände wäscht. Dieses Problem wird durch die Anwendung des erfindungsgemäßen Drug Delivery Systems ausgeschaltet.
• • Die Gefahr von Nebenwirkungen oder Überdosierungen, die bei der Anwendung der flüssigen Öle besteht, wird deutlich reduziert, da die ätherischen Öle mit Hilfe des Drug Delivery Systems in vorgegebenen Menge appliziert werden und die Freisetzung der Bestandteile der ätherischen Öle durch deren Diffusion im Bereich der Matrix, die nachfolgend eingehender beschrieben wird, kontrolliert wird.
• • Beim Auftreten von Nebenwirkungen kann die Applikation des Wirkstoffs durch die Entfernung des Drug Delivery Systems schlagartig gestoppt werden.
• • Durch die konstante Freisetzung des Wirkstoffs werden die Schwankungen der Wirkstoffkonzentration, die bei einer wiederholten Applikation am Tag auftreten, im Bereich der Haut und des Organismus verhindert.

The properties of the drug delivery systems according to the invention in relation to the performance of an aromatherapy result in the following advantages for the patient:

• • The patient is supplied with a controlled amount of the essential oils per unit of time for a long period of time in contrast to the types of application described above, in which the amount of active substance released significantly decreases as a function of the application time. This means that with the help of this application form, the therapeutic effect of the essential oils is kept constant over a long period of time, without an interruption of treatment occurs. The treatment of an indication can thus be carried out over the course of the entire day and / or the entire night. Due to these characteristics of the drug delivery system, the patients are significantly more compliant.
• • One problem with ointment application is the contamination of hands with mucous membrane-irritating essential oils. To avoid eye contact, it is essential for the patient to wash their hands after use. This problem is eliminated by the use of the drug delivery system according to the invention.
• • The risk of side effects or overdoses associated with the use of liquid oils is significantly reduced as the essential oils are applied by the drug delivery system in a predetermined amount and the release of essential oil constituents by their diffusion in the area of the Matrix, which is described in more detail below, is controlled.
• • If side effects occur, the drug can be stopped abruptly by removing the drug delivery system.
• • The constant release of the active substance prevents fluctuations in the concentration of active substance in the skin and the organism during repeated daily use.

The In addition, dosage can be very easily across the area of drug delivery systems be defined because the applied amount of the essential oil with the surface of the Systems grow.

Next Aromatherapy also has the option of containing the essential oils Delivery systems as body or room perfumes. In the development and production of the body perfume The perfume patch must be constructed to be a transdermal Application of the essential oils prevented the wearer becomes.

This is achieved by the incorporation of a layer into the delivery system which must be impermeable to the essential oils used, as in US Pat 1a the layer (3) represents. The patch is adhered to the body by an adhesive layer and guarantees release of the perfume over a period of 12 to 24 hours so that repeated application of the perfume throughout the day can be dispensed with. The adhesive layer has a skin friendliness, good adhesion over a long period of use and a painless removal of the delivery system.

There many essential oils one Furthermore, the use of the Delivery systems as room perfumes. Due to the delayed release the essential oils will an improvement in the room air over a long time guaranteed.

In the course of the work carried out for this invention, polyurethane or polyisobutylene was preferably used for the matrix of the drug delivery systems. During the preparation of the matrices, the essential oils were incorporated into the drug delivery systems as individual active ingredients or combinations of several oils or their constituents in a concentration range of 0.1-20.0%, with a concentration range of 5 to 10%. was preferably used. Due to the different design of the drug delivery systems, a duration of action of 30 minutes to 2 days was reached. As an improved variant, a duration of 2 to 24 hours and preferably a duration of 4 to 12 hours was considered. The shape of the drug. Delivery systems can be customized to the location of the application, as in 5 shown so that optimum comfort for the patient is achieved. The 5a and b show drug delivery systems suitable for larger areas such as the chest, back and neck. For body parts that are more rounded, such as the arm, leg, or shoulder, the drug delivery system used in the 5c is shown. For the application of deodorant in the area of the armpit, the deodorant delivery system of the 5d be used. For indications in the area of the joints, the application of the drug delivery system in the 5e and for the application of essential oils in the area of the nose, the shape in the 5f suitable. As already described, it is possible to produce drug delivery systems in which the essential oils are applied transdermally and / or by inhalation. In the 6a -h drug delivery systems are described which represent the diffusion-controlled and membrane permeation-controlled release of the essential oils. Membranes of polyethylene terephthalate, polypropylene, ethylene vinyl acetate, polyethylene, polyurethane and ethylene-vinyl copolymers are used to carry out a membrane-permeation-controlled release of the essential oils. Through this control mechanism, in addition to the control over the polymer matrix, the release of the essential oils can be adjusted variably and purposefully.

To perform a transdermal or per inhalation application, a blocking layer is used on the corresponding side of the drug delivery system, which may consist of polycarbonate, polyamide, polyethylene, polyester or aluminum-coated films. The blockade layer is impermeable to the correspondingly used essential oils. Through this variety of Vari For the production of drug delivery systems, an optimal adaptation to different indications is possible.

When base for The polymer matrix has become polyurethane for the solution of upcoming tasks as extremely useful proved. The polyurethane can advantageously self-adhesive be prepared so that an additional pressure-sensitive adhesive layer does not is mandatory.

The polyurethanes can be prepared from the known starting compounds of polyurethane chemistry by known processes, which are described in the patents DE-OS 3103499, DE-OS 3103500, US Pat. EP 0 147 588 A1 . EP 0 665 856 B1 or DE 196 18 825 A1 being represented.

polyurethane is used as a basis for the self-adhesive drug-containing matrix used. The production of the polyurethane (c) is carried out by the polymerization of an alcohol (a) with an isocyanate (b).

One crucial advantage of polyurethane polymer or gel matrices are their self-adhesive properties that an additional Applying an adhesion layer make superfluous to the matrix for fixation in the area of the skin. In the simplest case is the active ingredient-containing polyurethane matrix between a firmly anchored with her cover layer, as well backing named, and a peelable release layer. The carrier layer is advantageously a non-woven polymer.

The peelable release layer serves to secure the adhesive layer, to Improvement of the transport and storage stability and before application removed to the skin.

The Polyurethane matrix can be applied to a carrier layer or film be, as it is known from the prior art. The carrier foil consists of an air and water vapor permeable but water-impermeable polymer layer with a thickness of about 10 to 100 microns. The u.U. flexible carrier foil preferably consists of polymers of polyurethane, PE, PP, polyamide, Polyester or polyetherester.

• a) 2 bis 6 Hydroxylgruppen aufweisenden Polyetherpolyolen mit OH-Zahlen von 20 bis 112 und einem Ethylenoxid (EO)-Gehalt von ≥ 10 Gew.-%,
• b) Antioxidantien,
• c) in den Polyolen a) löslichen Wismut-(III)-Carboxylaten auf Basis von Carbonsäuren mit 2 bis 18 C-Atomen als Katalysatoren sowie
• d) Hexamethylendiisocyanat,

mit einem Produkt der Funktionalitäten der Polyurethan bildenden Komponenten a) und d) von mindestens 5,2, wobei die Katalysatormenge c) 0,005 bis 0,25 Gew.-%, bezogen auf das Polyol a) beträgt, die Menge an Antioxidantien b) im Bereich von 0,1 bis 1,0 Gew.-%, bezogen auf Polyol a) liegt und ein Verhältnis von freien NCO-Gruppen der Komponente d) zu den freien OH-Gruppen der Komponente a) (Isocyanatkennzahl) im Bereich von 0,30 bis 0,70 gewählt wird.Suitable polyurethanes as a matrix are the subject of DE 196 18 825 in which hydrophilic, self-adhesive polyurethane gels are disclosed which consist of

• a) 2 to 6 hydroxyl-containing polyether polyols having OH numbers of 20 to 112 and an ethylene oxide (EO) content of ≥ 10% by weight,
• b) antioxidants,
• c) in the polyols a) soluble bismuth (III) carboxylates based on carboxylic acids having 2 to 18 carbon atoms as catalysts and
• d) hexamethylene diisocyanate,

with a product of the functionalities of the polyurethane-forming components a) and d) of at least 5.2, wherein the amount of catalyst c) 0.005 to 0.25 wt .-%, based on the polyol a), the amount of antioxidants b) in Range from 0.1 to 1.0 wt .-%, based on polyol a) and a ratio of free NCO groups of component d) to the free OH groups of component a) (isocyanate index) in the range of 0, 30 to 0.70 is selected.

It are preferably 3 to 4, most preferably 4-hydroxyl groups having polyether polyols used with an OH number in the range from 20 to 112, preferably from 30 to 56. The ethylene oxide content is in the inventively used Polyether polyols at preferably ≥ 20 wt .-%.

The polyether polyols are known per se and are, for example, by polymerization of epoxides such as ethylene oxide, propylene oxide, butylene oxide or tetrahydrofuran, with itself or by addition of these epoxides, preferably of ethylene oxide and propylene oxide - optionally in admixture with each other or separately Starter components having at least two reactive hydrogen atoms, such as water, ethylene glycol, propylene glycol, diethylene glycol, dipropylene glycol, glycerol, trime methylolpropane, pentaerythritol, sorbitol or sucrose. Representatives of the above-mentioned higher molecular weight polyhydroxyl compounds are listed, for example, in High Polymers, Vol. XVI, "Polyurethanes, Chemistry and Technology" (Saunders-Frisch, Interscience Publishers, New York, Vol. 1, 1962, pp. 32-42).

When Isocyanate component becomes monomeric or trimerized hexamethylene diisocyanate or by biuret, uretdione, allophanate groups or by prepolymerization with polyether polyols or mixtures of polyether polyols Basis of the known starter components with 2 or> 2 reactive H atoms and Epoxides, such as ethylene oxide or propylene oxide having an OH number of ≤ 850, are preferred 100 to 600, modified hexamethylene diisocyanate used. Prefers is the use of modified hexamethylene diisocyanate, in particular by prepolymerization with polyether diols of OH number 200 to 600 modified hexamethylene diisocyanate. Very particularly preferred are modifications of hexamethylene diisocyanate with polyether diols the OH number 200 - 600, their residual content of monomeric hexamethylene diisocyanate below 0.5% by weight lies.

When Catalysts are coming for the polyurethane gels of the invention in the anhydrous polyether polyols a) soluble bismuth (III) carboxylates based on linear, branched, saturated or unsaturated carboxylic acids with 2 to 18, preferably 6 to 18 carbon atoms in question. Preferred are Bi (III) salts branched saturated carboxylic acids with tertiary Carboxyl groups, such as 2,2-dimethyl-octanoic acid (for example Versatic acids, Shell). Well suited are preparations of these Bi (III) salts in excess proportions of these carboxylic acids. Excellent proven has a solution of 1 mol of the Bi (III) salt of Versatic 10-acid (2,2-dimethyloctanoic acid) in a surplus of 3 mol of this acid. with a bi-content of about 17%.

It the catalysts are preferably used in amounts of from 0.03 to 0.3% by weight, based on the polyol a) used.

When Antioxidants come for the polyurethane gels of the invention in particular sterically hindered phenolic stabilizers, such as BHT (2,6-di-tert-butyl-4-methylphenol), Vulkanox BKF (2,2-methyl-bis (6-tert-butyl-4-methyl phenol) (Bayer AG), Irganox 1010 (pentaerythrityl tetrakis [3- (3,5-di-tert-butyl-4-hydroxyphenyl) propionate]), Irganox 1076 (octadecyl-3- (3,5-di-tert-butyl-4-hydroxyphenyl) -propionate) (Ciba-Geigy) or tocopherol (vitamin E) into consideration. Prefers are those of the type of α-tocopherol used. The antioxidants are preferred in amounts of 0.15 to 0.5 wt .-%, based on the polyol a) used.

f:

Funktionalität der Isocyanat- oder Polyolkomponente

The isocyanate index (ratio of the free NCO groups used in the reaction to the free OH groups) of the polyurethane graft compositions according to the invention is in the range from 0.30 to 0.70, preferably in the range from 0, depending on the functionality of the isocyanate and polyol components used , 45 to 0.60. The isocyanate index required for gel formation can be estimated very simply by the following formula: f (Polyol) · (F (Isocyannt) - 1) · Code ≈ 2

f:

Functionality of the isocyanate or polyol component

ever after desired stickiness or elasticity of the gel can actually to using isocyanate index up to ± 20% of the calculated Value deviate.

The polyurethane gel masses according to the invention are made according to usual Processes as described, for example, in Becker / Braun, Kunststoff-Handbuch, Vol. 7, Polyurethane, p. 121 ff, Carl-Hauser, 1,983th

• 1. einem Polyurethangel, welches (A) 25 – 62 Gew.-%, vorzugsweise 30 – 60 Gew.-%, besonders bevorzugt 40 – 57 Gew.-%, bezogen auf die Summe aus (A) und (B), eines kovalent vernetzten Polyurethans als hochmolekulare Matrix und (B) 75 – 38 Gew.-%, vorzugsweise 70 – 40 Gew.-%, besonders bevorzugt 60 – 43 Gew.-%, bezogen auf die Summe aus (A) und (B) einer oder mehrerer in der Matrix durch Nebenvalenzkräfte fest gebundenen Polyhydroxylverbindungen mit einem mittleren Molekulargewicht zwischen 1000 und 12000, vorzugsweise zwischen 1500 und 8000, besonders bevorzugt zwischen 2000 und 6000, und einer mittleren OH-Zahl zwischen 20 und 112, vorzugsweise zwischen 25 und 84, besonders bevorzugt zwischen 28 und 56, als flüssigem Dispersionsmittel, wobei das Dispersionsmittel im wesentlichen frei ist an Hydroxylverbindungen mit einem Molekulargewicht unter 800, vorzugsweise unter 1000, besonders bevorzugt unter 1500, sowie gegebenenfalls (C) 0 bis 100 Gew.-%, bezogen auf die Summe aus (A) und (B), an Füll- und/oder Zusatzstoffen enthält, und welches erhältlich ist durch Umsetzung einer Mischung von a) einem oder mehreren Polyisocyanaten, b) einer oder mehreren Polyhydroxylverbindungen mit einem mittleren Molekulargewicht zwischen 1000 und 12000, und einer mittleren OH-Zahl zwischen 20 und 112, c) gegebenenfalls Katalysatoren oder Beschleunigern für die Reaktion zwischen Isocyanat- und Hydroxylgruppen sowie gegebenenfalls d) aus der Polyurethanchemie an sich bekannten Füll- und Zusatzstoffen, wobei diese Mischung im wesentlichen frei ist von Hydroxylverbindungen mit einem Molekulargewicht unter 800, die mittlere Funktionalität der Polyisocyanate (F_l) zwischen 2 und 4 liegt, die mittlere Funktionalität der Polyhydroxylverbindung (F_p) zwischen 3 und 6 beträgt und die Isocyanatkennzahl (K) der Formel
  
  gehorcht, in welcher X ≤ 120, vorzugsweise X ≤ 100, besonders bevorzugt X ≤ 90 ist und die Kennzahl K bei Werten zwischen 15 und 70 liegt, wobei die angegebenen Mittelwerte von Molekulargewicht und OH-Zahl als Zahlenmittel zu verstehen sind,
• 2. einem Wasser absorbierenden Material und/oder
• 3. einem nichtwässrigen Schäumungsmittel.

Further preferably polyurethane gels are used, as described in the EP 0 665 856 B1 are disclosed. The hydrophilic polyurethanes are therefore available from

• 1. a polyurethane gel which comprises (A) 25-62% by weight, preferably 30-60% by weight, particularly preferably 40-57% by weight, based on the sum of (A) and (B), of a Covalently crosslinked polyurethane as a high molecular weight matrix and (B) 75-38 wt .-%, preferably 70- 40 wt .-%, particularly preferably 60-43 wt .-%, based on the sum of (A) and (B) a or more poly bound in the matrix by secondary valence forces hydroxyl compounds having an average molecular weight between 1000 and 12000, preferably between 1500 and 8000, more preferably between 2000 and 6000, and an average OH number between 20 and 112, preferably between 25 and 84, particularly preferably between 28 and 56, as a liquid dispersant wherein the dispersing agent is substantially free of hydroxyl compounds having a molecular weight below 800, preferably below 1000, more preferably below 1500, and optionally (C) 0 to 100 wt .-%, based on the sum of (A) and (B) , containing fillers and / or additives, and which is obtainable by reacting a mixture of a) one or more polyisocyanates, b) one or more polyhydroxyl compounds having an average molecular weight between 1000 and 12000, and an average OH number between 20 and 112, c) optionally catalysts or accelerators for the reaction between isocyanate and hydroxyl groups and gegeb if appropriate d) from polyurethane chemistry known fillers and additives, said mixture is substantially free of hydroxyl compounds having a molecular weight below 800, the average functionality of the polyisocyanates (F _l ) is between 2 and 4, the average functionality of the polyhydroxy compound ( F _p ) is between 3 and 6 and the isocyanate index (K) of the formula
  
  in which X ≦ 120, preferably X ≦ 100, more preferably X ≦ 90, and the characteristic K is between 15 and 70, the mean values of molecular weight and OH number given being the number average,
• 2. a water-absorbing material and / or
• 3. a non-aqueous foaming agent.

Essential in the production of polyurethanes is that in the selection the yellow-forming components complied with the conditions defined above become. With that you can advantageously self-adhesive gels are produced, otherwise Tack-free, elastic gels are obtained.

preferred Polyhydroxyl compounds are polyether polyols as described in the above mentioned disclosure documents are mentioned in detail.

When Polyisocyanate components are both (cyclo) aliphatic and aromatic isocyanates suitable. Preferred (cyclo) aliphatic Polyisocyanates are 1,6-hexamethylene diisocyanate and its biurets and trimers or hydrogenated diphenylmethane diisocyanate ("MDI") types. preferred Aromatic polyisocyanates are those obtained by distillation like MDI blends of 4,4'- and 2,4'-isomers or 4,4'-MDI, as well Toluylene diisocyanate ("TDI") types.

The Diisocyanates can especially for example from the group of unmodified aromatic or aliphatic diisocyanates or else by prepolymerization modified with amines, polyols or polyether polyols formed Products selected become.

The Polyurethane matrix may be partially or fully foamed and / or unfoamed, unfilled or with additional fillers, such as superabsorbents, titanium dioxide, zinc oxide, plasticizers, dyes etc. are used.

About one Foam the matrix can have a better cushioning effect and associated with it an improved feel for the user can be reached.

The Polyurethane gels can optionally known from polyurethane chemistry per se additives included, such as fillers and short fibers of inorganic or organic origin, metal pigments, surfactants Substances or liquid Extenders such as substances with a boiling point above 150 ° C.

When inorganic fillers be, for example, barite, chalk, gypsum, kieserite, soda, titanium dioxide, Ceria, quartz sand, kaolin, soot and hollow microspheres.

On organic fillers, for example, powders based on polystyrene, polyvinyl chloride, urea-formaldehyde and polyhydrazodicarbonamide can be used. As short fibers come to Bei play glass fibers of 0.1 - 1 mm in length or fibers of organic origin, such as polyester or polyamide fibers in question. Metal powders, such as iron, aluminum, or copper powders may also be included in gel formation. In order to impart the desired color to the gels, the dyes or color pigments known per se in the dyeing of polyurethanes may be used on an organic or inorganic basis, for example iron oxide or chromium oxide pigments, phthalocyanine- or monoazo-based pigments. As surface-active substances, for example, cellulose powder, activated carbon and silicic acid preparations may be mentioned.

to Modification of the adhesive properties of the gels may optionally be added by polymeric vinyl compounds, polyacrylates and other in the Adhesive technique usual Copolymers or natural-based adhesives up to one Content of 10 wt .-%, based on the weight of the gel mass added without the advantageous properties of the polyurethanes change.

The Polyurethane matrix advantageously can also be adjusted transparently become. As transparent, permeable to water vapor and adhesive, the Polyurethane matrix with it aesthetic and application-friendly aspects. This represents a significant advantageous difference to the polyacrylate and silicone gel based The transparency also increases the acceptance of the Users, as the patch usually has a longer Period is worn on the skin.

Furthermore, it is possible to influence the properties of the drug delivery systems by the addition of further substances in the course of the production of the polyurethane:
The use of foaming agents causes a reduction in the density of the polymer and foaming of the matrix. The foaming agents used are gases which do not form any compounds with the starting compounds of the polyurethane, it being possible for the degree of foaming to be varied within wide limits by the incorporated amounts of foaming agent. As a rule, nitrogen is used to foam the matrix. It is also possible to vary the properties of the polyurethane composition by the addition of fillers, such as superabsorbents, titanium dioxide, zinc oxide, plasticizers, dyes, etc.

The use of polyurethane drug delivery systems may release a large amount of fluid that needs to be bound in the course of treatment. The fluid may form, for example, by sweating, in particular during prolonged wear of the system on the skin, which according to the invention is possible without disadvantages. Preferred liquid-absorbing materials are the salts of the polyacrylates and their copolymers, referred to as superabsorbents, in particular the sodium or potassium salts. These superabsorbents are produced uncrosslinked or crosslinked and are available as commercial products. Favorable properties are exhibited by those superabsorbents which are used in the DE 37 13 601 A1 and superabsorbers of the new generation, which have only a small proportion of evaporable water and a high swelling capacity under pressure. Preferred products are weakly crosslinked polymers based on acrylic acid / sodium acrylate. These sodium polyacrylates are commercially available as Favor T (Chemische Fabrik Stockhausen GmbH, Germany). Other absorbers, for example carboxymethylcellulose and karaya, are also suitable.

It is therefore an advantage in the drug delivery system superabsorbent or superabsorbent polymer in an amount of 0.01 to 30% by weight, in particular from 0.5 to 25% by weight, in particular 10% by weight, based on the total mass of the polymer matrix, incorporate.

polyurethane polymer or gel matrices have u.U. self-adhesive properties that usually have sufficient adhesive power to the drug Delivery systems to give a sufficient grip on the skin. Nevertheless, under certain circumstances an additional adhesion necessary, wherein the modification of the adhesive properties by the Addition of natural-based adhesives, polymeric vinyl compounds, Polyacrylates and other common in the adhesive art Copolymers up to a content of 10 wt .-% by weight the gel mass takes place. The adhesive matrices are expected to be Skin friendliness, good adhesion over a long period of use and ensure a painless removal of the drug delivery system.

Around the polyurethane in a desired Can produce color for coloring used dyes or color pigments on organic or inorganic Base be used. As an example, iron oxide, chromium oxide pigments or phthalocyanine or monoazo-based pigments.

• • Die Sauerstoffdurchlässigkeit des Polyurethans sorgt für eine gute Versorgung der abdeckten Hautstellen mit Sauerstoff, wodurch einer Schädigung des Gewebes entgegengewirkt wird.
• • Polyurethan ist allergieneutral, so dass nach der Applikation des Drug Delivery Systems mit keiner allergischen Reaktionen des Organismus zu rechnen ist.
• • Polyurethan stellt ein u.U. selbstklebendes System dar, wodurch auf einen Zusatz weiterer Klebstoffe, die unter Umständen Nebenwirkungen wie Mazeration, Entzündungen der dermalen Bereiche, Allergien, Reduktion der Hautatmung u.a. hervorrufen, verzichtet werden kann.
• • Polyurethan weist eine hohe Flexibilität auf, so dass keine Probleme bei der Anwendung der Drug Delivery Systeme im Bereich von Gelenken entstehen.
• • Durch die Schäumung des Polyurethan wird eine Matrix gebildet, die den schmerzverursachenden Einfluss von mechanischen Einwirkungen bei der Behandlung von Wunden, Insektenstichen und Verbrennungen reduziert.
• • Polyurethan weist eine sehr gute Wasseraufnahmefähigkeit und Wasserdampfdurchlässigkeit auf. Hierdurch ist gewährleistet, dass bei einem Applikation über einen längeren Zeitraum keine Mazeration der Haut erfolgen wird.

As advantages of the polyurethanes according to the invention in comparison to other polymers which are suitable for Her When using drug delivery systems, the following points can be

• • The oxygen permeability of the polyurethane provides a good supply of oxygen to the covered skin areas, which counteracts damage to the tissue.
• • Polyurethane is allergen-neutral, so that after the application of the drug delivery system with no allergic reactions of the organism is to be expected.
• • Polyurethane may be a self-adhesive system, which may require the addition of other adhesives, which may cause side effects such as maceration, inflammation of the dermal areas, allergies, reduction of skin respiration, among others.
• • Polyurethane has a high level of flexibility, so there are no problems with the use of the drug delivery systems in the area of joints.
• Foaming of the polyurethane forms a matrix that reduces the pain-causing influence of mechanical effects in the treatment of wounds, insect bites and burns.
• • Polyurethane has a very good water absorption and water vapor permeability. This ensures that in the case of an application over an extended period of time no maceration of the skin will take place.

at the essential oils that are incorporated into the polyurethane matrix is just on it to pay attention to such oils be used over Ingredients with functional groups have no reaction enter with the isocyanate. Otherwise it would lead to the formation of by-products, their toxic Effects no statement can be made. The use of appropriate Drug delivery systems in aromatherapy would be questionable in this case and could not done become. Another problem in the production of the doped with essential oils Polyurethane matrices is the odor nuisance in the area of manufacture. These annoyances leads to one to damage the employee, on the other hand, there is a risk that products, which are manufactured after the drug delivery system, with contaminated with the essential oils become. For this reason, a manufacturing process has been developed, which the possibility offers that endowed with essential oils Matrix on a carrier material apply without an unreasonable odor nuisance or contamination of the manufacturing plant and thus other products The result is.

simplified the polyurethane matrix is composed of components A, B and C. together, wherein A is the alcohol component and B is the isocyanate component represent. Since components A and B have a very low reaction rate is for the implementation the polymerization, the addition of the catalyst in the form of a bismuth compound necessary, which is referred to as component C. Table 1 shows a exemplary composition.

Tab. 1: Composition of components A, B and C

In the preparation of the polyurethane ( 4 ) a mixture of the components base, reactor and activator takes place in a mixing cell. Since the essential oil is already contained in the components A, no further dosage of the active ingredient must take place. As a result of the reaction between the components A, B and C, the ethereal oil-containing polyurethane matrix is formed, the ethereal oils being homogeneously distributed in the polymer matrix by this method of preparation, as is advantageous according to the invention. The matrix initially has a low viscosity and is therefore deformable over a limited period of time, so that the height of the drug delivery systems can be adjusted. The polyurethane composition is sandwiched between a polypropylene layer and a siliconized polyester film following the mixing of the components to be processed by means of a hot press into a polyurethane layer in a height range of 50 to 500 μm. The polyurethane laminate is then passed over a treadmill to ensure a sufficient time for curing the matrix material. The drug delivery system is finally obtained by replacing the top film with a carrier layer, which advantageously consists of a non-woven polymer. In drug delivery systems, where a membrane permeation controlled release of the drug is to take place, in addition, the lower film is replaced by a layer that is able to control drug release, and a new protective film. Immediately in the on After production, the plaster is packaged to prevent the loss of essential oils or their constituents.

Next Polyurethanes also have polyisobutylenes as a suitable base for the Polymer matrix shown.

As a template for the development of the polyisobutylene matrix served the patent EP 1120115 in which similar raw materials were used.

Prefers be used:

High molecular weight polyisobutylene:

polyisobutylene with an average molecular weight of 300,000 to 1,100,000, preferably polyisobutylene having a molecular weight of 650,000 until 850,000 is used. The product is under the trade names Oppanol B100 (BASF) and Vistanex MM-L80 (Exxon).

Low molecular weight polyisobutylene:

polyisobutylene having an average molecular weight of 40,000 to 120,000, wherein preferably polyisobutylene having a molecular weight of 60,000 to 100,000 is used. The product is under the trade name Oppanol B15 (BASF) and Vistanex LMMH (Exxon).

Amorphous poly-α-olefin:

amorphous Copolymers based on ethylene and propylene, butylene or 1-hexene. Average molecular weight of 5,000 to 100,000, wherein preferably amorphous poly-α-olefin with a molecular weight of 10,000 to 30,000 is used. The product is under the trade name Elastoflex (Eastman) and Vestoplast (Hüls) available.

Hydrophilic filler:

insoluble, hydrophilic particles based on cellulose, which has a medium Particle size of less than or equal 100 microns have and a uniform surface have. The product is under the trade name Avicel (FMC) and Elcema (Degussa-Huls) available.

Castor oil:

clear, Pale yellow and viscous oil that passes through cold squeezing of the seeds is gained to the passage of toxic ricin in the oil to prevent.

• Cetiol V:

Cetiol is a viscous Resin consisting of oleyl oleate. The addition of Cetiol V takes place instead of solubility of the essential oils in the Increase matrix.

An inventively advantageous matrix of the drug delivery system is composed of the following proportions of the raw materials:

The Production of the polyisobutylene matrix is carried out without the use of solvents by kneading the raw materials in the course of a temperature increase 75 to 90 ° C. The process of kneading becomes laboratory kneaders equipped with duplex blades carried out. By the expenditure of the mechanical force and the temperature increase becomes a homogeneous matrix material made, in which the essential oils in combination be incorporated with the Cetiol V or castor oil. The resulting drug delivery systems show very good adhesive properties, so that can be dispensed with an addition of adhesive resins. Because the adhesion force the matrix has a strong dependence of the molecular weight of the polyisobutylene and the amorphous poly-α-olefins shows, there is the possibility adapt the bond strength of the matrix to the respective requirements.

Around a homogeneous distribution of individual or combined essential oils or to achieve their constituents in the polyisobutylene matrix the essential oils in combination with the cetiol V or castor oil in the homogeneous mixture of the polyisobutylene, the amorphous poly-α-olefin and the hydrophilic filler by mechanical forces incorporated.

To the production of the matrix material with a homogeneous distribution The essential oils became the Mass between siliconized papers using a hot press at a temperature of 90 ° C over a Period of 30 seconds and a force of 150 kN to a matrix layer with a thickness of 150 to 500 microns processed.

by virtue of of the described process for the preparation of essential oil-containing drug delivery systems, is a further development of production with extruder technology possible.

The Peelable protective film of the drug delivery system is advantageous coated with silicone, polyethylene or polytetrafluoroethylene Paper, polypropylene, polyester or aluminum coated films.

When become the described blocking layer of the drug delivery system Polycarbonate, polyamide, polyethylene, polyester or aluminum coated Sheets used.

When the described permeation-controlling membranes of the drug Delivery Systems are polyethylene terephthalate, polypropylene, ethylene vinyl acetate, Polyethylene, polyurethane and ethylene-vinyl copolymers membranes used. The membranes have a fixed layer thickness as well a defined size of the pores and the pore density, whereby the release of the essential oils and their Ingredients is controlled.

When the additional described Pressure-sensitive adhesive layer of the drug delivery system will be layers of polyurethane, Polyisobutylene or acrylate-based polymers used.

Further possible Matrices as carrier masses for essential oils in the Aromatherapy are silicone, rubber or SBC hotmelts matrices, Moisture-adhesive polymer film based on PVA / PAS, commercially available acrylate matrices or gel matrices on agar agar / PAS basis.

Also that, of course occurring citronella oil can be preferred. Main ingredients are geraniol and citronellal, in particular for a repelling effect are responsible.

The maximum mixing ratio of citronella oil in the adhesive matrix was surprisingly up to 65 wt.%, Based on the total mass determined. Clear, homogeneous solutions could up to a ratio of up to 65% by weight citronella oil in 35% by weight of solvent-containing Acrylate matrix are obtained. In particular, have advantageous conditions from 50:50 Repellent made out to adhesive matrix.

The thereby obtained maximum release rates were up to 4 mg / h in the required range of a longer period of use than the application forms known from the prior art enable.

According to the invention preferred Patches show a release rate depending on the active ingredient used, Adhesive matrix and additives of at least 2 mg / h after 1 hour and at least 0.3 mg / h after 8 hours in the ambient air.

The Release rates are determined by the samples to be tested at 32 ° C be stored in a drying oven. The sample is taken with the support membrane fixed up on a release liner and at defined times removed from the oven, weighed and returned. From the weight difference between two withdrawals, the release rate be determined (in mg / h).

The Content determinations of citronella oil are made in the adhesive matrix Gas chromatographic according to the method of Ph.Eur. monograph for citronella oil.

The cohesion and adhesion the adhesive matrix is assessed qualitatively.

to further increase the release rate were experiments with various additives carried out, which at the same time also the cohesiveness of the matrix increase and thus the technical processability as well as the applicability improve by the consumer. It turned out that by the additive according to the invention on additives no delamination of the active ingredient-containing layer of the skin-sticking layer during the use occurred. Various concentrations were used of polyoxyethylene sorbitan monooleate, polyvinylpyrrolidone, silica and aluminum acetylacetonate as an additive.

The Release rates could be clearly demonstrated by the addition of additives be increased.

Around at the same time the cohesiveness of the adhesive matrix to optimize and to make the production of the plaster problem-free, were further investigations to the optimal concentration the additives, also as their mixture, in terms of physico-chemical Matrix properties with consistently high drug release carried out.

Surprisingly Mixtures of 0.5-1.5% aluminum acetylacetonate were found with 2 - 8 % Polyvinylpyrrolidone in the drug-containing adhesive matrix all other additives and their mixtures both in terms of cohesiveness and Adhesiveness of the matrix clearly superior. Particular preference is therefore given to mixtures having a ratio of 1.2% aluminum acetyl-acetonate to 4% PVP in the preferred active ingredient-containing Adhesive matrix consisting of citronella oil / acrylate matrix. By such Mixtures can Matrix systems with a high content of oily natural substances such. Citronella oil, produced with long-lasting sufficient drug release which, at the same time, have excellent adhesion as well as consistency to ensure processing as Insektenrepellent pavement.

at the production of matrices according to the invention come commercially Kneader or mixer for use. Will the basic adhesive matrix, here e.g. Acrylate matrix, containing solvents processed, the solvent must after laminating the matrix to a support in a drying channel become. This is on as possible careful drying. When using a solvent-free Matrix, the production can also be done in an extruder. at In this method, the matrix without drying channel is directly on the Carrier extruded.

at containing an inventive essential oils Polyacrylsäurematrix the crosslinking of the polyacrylic acid is advantageous with the aid of Polyvinylpyrrolidone (PVP) performed.

Crosslinking occurs via the formation of a quaternary ammonium salt of the PVP. This type of crosslinking leads to organic salts which, in contrast to the known metal salts, are bound as crosslinking agents via the hydroxyl functions of the polyacrylic acid molecules. As with the metal salts, the reaction is reversible and can be reversed by the addition of water or acids. The viscosity The resulting gel can be controlled not only by the amount of crosslinker, but also by the molecular weight of the PVP. High molecular weights lead to low viscosity gels and low molecular weights to high viscosity gels and tack. The advantage of this type of cross-linking is the targeted production of gel matrices via the parameters proportion PVP and molecular weight PVP, whose tackiness, cohesiveness and viscosity can be individually adjusted to the respective field of application.

This Effect of the influence of the molecular weight of the PVP on the viscosity and adhesion The gel matrix is due to the following finding: For long-chain PVP the number of pyrrolidone subunits per macromolecule is significant higher than with short-chain PVP. As a result, there are more reactions to the same Reaction partners with each other, since the macromolecules themselves easy to bundle can orient. These Reactions lead not for the formation of nodes with several polyacrylic acid molecules. It Therefore, only a few cross-links to other Polyacrylsäuremolekülen and so few, big ones Knotted. This circumstance leads to a loosely linked Low viscosity gel. In contrast, short-chain PVPs are due to the higher mobility and the lower tendency to orient the molecules into strands more connections formed into various polyacrylic acid molecules, which lead to a narrower mesh size and a lower flexibility and viscosity of the gel.

The viscosity the gels leaves about it beyond yet control other factors. For example, the amount of PVP plays a decisive role for the structure of the gel. If a saturation point is exceeded, Thus, there are competing reactions of the free PVP molecules with the already networked. These competing reactions lead to cross-linking points in favor of unlinked aggregates made of polyacrylic acid and the excess PVP molecules be broken up. The consequence of this supersaturation is a decrease in Total number of nodes and thus a decrease in the gel viscosity. As another option for controlling the gel viscosity may be the addition of protic solvents (e.g., water, alcohols, amines, thiols) or organic proton donors (Carboxylic acids e.g. salicylic acid) or inorganic agents (e.g., Lewis acids). Here In particular, compounds from the substance classes of tertiary polyamines are available and the polyamides. In each of these cases contributes the addition of the agents to reduce the coordination sites on either the polyacrylic acid or at the PVP. This will set the number of potential join points reduced to the formation of gel mesh, which has a direct impact on the viscosity of the gel.

Of Furthermore, the resulting gel properties of the matrices on the Molecular weight, degree of substitution and degree of crosslinking of the used polyacrylic acid influence.

to Preparation of special application properties the gel matrices with the appropriate plasticizers, solubilizers, Penetration enhancers, fillers and / or other known additives added.

As a gel base advantageous polyacrylates are acrylate-alkyl acrylate copolymers, in particular those from the group of so-called carbomers or carbopols (Carbopol ^® is actually a registered trademark of the BF Goodrich Company). In particular, the advantageous acrylate-alkyl acrylate copolymers or copolymers are characterized by the following structure:

In this put R 'one long-chain alkyl radical and x and y are numbers which the respective stoichiometric Symbolize the proportion of the respective comonomers.

According to the invention particularly preferably acrylate copolymers and / or acrylate-alkyl acrylate copolymers, which are available from the BFGoodrich Company under the trade names Carbopol ^® 1382, Carbopol ^® 981 and Carbopol ^® 5984, preferably polyacrylates from the group of Carbopol grades 980, 981 , 1382, 2984, 5984 and more preferably Carbomer 2001.

Also advantageous are copolymers of C _10-30 -alkyl acrylates and one or more monomers of acrylic acid, methacrylic acid or their esters, which are cross-linked with an allyl ether of sucrose or an allyl ether of pentaerythritol.

Polyacrylic acid and / or their copolymers are preferably used in an amount of 5 to 55% by weight, more preferably between 5 - 30 % By weight used. All percentages are by weight Gel matrix unless otherwise stated.

When Crosslinker will polyvinylpyrrolidone (PVP), e.g. Luviskol the company BASF, preferably in an amount of 0.25-60 wt.%, more preferably between 1 and 30 Wt.%. Equally can also PVP copolymers such as vinylpyrrolidone-vinyl acetate (Povidone acetate, Kollidon VA 64), terpolymers based on vinylpyrrolidone and acrylic acid or methacrylic acid or their esters (Luviflex VBM 35), copolymers of vinylpyrrolidone and vinylimidazolium methochloride (Luviquat brands) as so-called PVP crosslinking agent be used.

When other gel components can Polyalcohol or alcohols, e.g. 1,2-propanediol, glycerol, and / or Water are used, preferably in an amount of 5 to 90 wt.%, more preferably between 5-45 Wt.%.

Further Components of the gel matrix can Solubilizers, e.g. Polyethylene glycols (Lutrol E400, E600 BASF) in one Quantity from 0 - 50 % By weight, preferably 0-30 % By weight, neutralizing agents, e.g. Tromethamol, triethanolamine and / or Dexpanthenol, in an amount 0 - 30 % By weight, preferably 0-15 % By weight, filler (s), e.g. silica, micronised cellulose and / or gelatin, in an amount of 0-30% by weight, preferably 3 - 15 % By weight, and of course Active ingredient (s), e.g. jojoba oil, in an amount of 0 - 35 % By weight, preferably 0-15 % By weight.

Further possible Matrices as carrier masses for essential oils in the Aromatherapy are silicone, rubber or SBC hotmelts matrices, wet-adhesive polymer film based on PVA / PAS or gel matrix on agar Agar / PAS basis, which are explained in more detail below.

• a) Silikon
• b) Gelbildner
• c) gegebenenfalls einem Silikonharz.

A moisture-absorbing silicone-based matrix containing essential oils for delivery to the respiratory air, wherein the pressure-sensitive adhesive matrix consists of

• a) silicone
• b) gelling agent
• c) optionally a silicone resin.

• a) Silikon: 55 bis 80 Gew.-%, insbesondere 60 bis 75 Gew.-%
• b) Gelbildner: 20 bis 40 Gew.-%, insbesondere 25 bis 40 Gew.-%
• c) ätherische Öle 0,1 bis 15 Gew.-%, insbesondere 0,5 – 5 Gew. %

In a first advantageous embodiment of the invention, the matrix has the following composition:

• a) Silicone: 55 to 80% by weight, in particular 60 to 75% by weight
• b) gel formers: 20 to 40% by weight, in particular 25 to 40% by weight
• c) essential oils 0.1 to 15% by weight, in particular 0.5 to 5% by weight

silicones are processed as one- or two-component systems. The networking takes place as a rule as polycondensation with elimination of acetic acid, or as a polyaddition using a platinum catalyst.

verwendet.For the preparation of the described matrices, a commercially available two-component system of polydimethylsiloxane (see Figure), Q7-9600 A + B; Dow Corning Co.,

used.

to Adjustment of bond strength was optionally crosslinked with silicone resin Polydimethylsiloxane (PSA MD74602, Dow Corning).

Water absorbency of the matrix was achieved by using high relative gelling agents Surface incorporated in amounts such that the gelling agent may have intermolecular cross-links from the surface to the interior of the matrix. Such gelling agents are, for example, polyacrylic acid, polyacrylonitrile or microcrystalline cellulose. Mainly polyacrylic acid types of the Carbopol series, Goodrich Corp., were used.

to Variation of water absorbency were added strong gelling agent with low relative surface incorporated, such as Example sodium polyacrylate (Favorsorb, Stockhausen).

The Production takes place at room temperature in commercial Mixers. First become in 2-component systems, the two silicone components together mixed. Thereafter, if necessary, the silicone resin component is stirred, then the or the gel formers incorporated and finally ethereal oils are stirred.

The Matrix is on a support streaked and covered with a release liner. The duration of the crosslinking reaction The silicone matrix can be controlled depending on the temperature.

optional can the incorporated essential oil also after the crosslinking reaction as a solution or introduced in a cosmetic emulsion through the channels of the gelling agent become.

• a) Kautschuk
• b) Klebharzen
• c) hydrophiler, wasseraufnehmender dispers verteilter Feststoff.
• d) Alterungsschutzsystem

Moisture-absorbent essential oils containing rubber-based matrix for release to the atmosphere, wherein the pressure-sensitive adhesive matrix consists of

• a) rubber
• b) Adhesive resins
• c) hydrophilic, water-absorbing dispersed dispersed solid.
• d) aging protection system

In a first advantageous embodiment of the invention, the matrix has the following composition:

Rubber adhesives in the specified form are processed in solution. The rubber used is either more natural or synthetic origin. The mechanical properties of the different types result in the mixture of a recipe the desired scaffold properties a rubber adhesive.

The used adhesive resins impart the necessary pressure tack or tack. Plasticizers, e.g. Mineral oils are used for fine tuning the mechanical properties of the recipe.

A Water absorption capacity The matrix was achieved by adding a hydrophilic water-absorbent Solid finely dispersed distributed in the recipe.

When Substance group preferably come from plant root and cornstarch for use, possible are also celluloses and their derivatives as well as other water-absorbing Solids. The water absorption capacity can over the Type and amount of the hydrophilic solid can be influenced.

Rubber adhesives are sensitive to oxidation due to their chemistry. You must therefore be equipped with a suitable aging protection system. This has in addition to the function as an antioxidant additionally physiological to be safe.

The Production takes place at room temperature in commercial Mixers. The rubber ingredients are in a suitable solvent solved and subsequently the remaining components including the active ingredient are added.

The Crowd is on a support spread and leave the solvent evaporate from the mass. The duration of the evaporation process can be temperature dependent to be controlled. The adhesive side of the compound is covered with a release liner.

at This method of production should be noted that the necessary evaporation energy of the respective essential oil far above the evaporation energy of the solvent.

optional can Rubber matrices according to the invention containing essential oils also solvent-free per Extruders are produced.

tacky Matrix for the controlled release of essential oils to the respiratory air, wherein the scaffolding-forming Adhesive matrix substance by styrene block copolymers (SBC) is formed.

In an advantageous embodiment, the latex-free PSA has the following composition: 5% by weight to 90% by weight block copolymers, 5% by weight to 80% by weight Tackifiers such as oils, waxes, resins and / or mixtures thereof, preferably mixtures of resins and oils, less than 60% by weight plasticizers, less than 15% by weight additives less than 5% by weight stabilizers less than 20% by weight essential oils.

The tackifier aliphatic or aromatic oils, waxes and resins are preferably hydrocarbon oils, waxes and resins, wherein the oils (like paraffin hydrocarbon oils) or the waxes (such as paraffin hydrocarbon waxes) through their Consistency favorable affect the adhesive effect. Included in a special form the adhesive composition at least one aliphatic hydrocarbon resin and at least one aromatic hydrocarbon resin. As a plasticizer find medium or long-chain fatty acids and / or their esters use. These accessories These are the setting of the adhesive properties and stability. Possibly Further stabilizers and other auxiliaries are used.

One To fill the cohesive Adhesive with mineral fillers, Fibers, micro hollow or solid balls is possible.

optional can additionally also up to 15 wt .-% of a permeation-promoting excipient as lipophilic solubilizers such as oleic acid decyl ester or isopropyl myristate and palmitate (IPM and IPP).

The Production of the matrix is preferably carried out by means of methods which all components of the pressure-sensitive matrix waiving the addition of solvents be homogenized in the melt.

Especially All components are preferred in a continuous or discontinuous process a temperature below 100 ° C processed.

damp self-adhesive polymer film for the delivery of essential oils to the respiratory air, comprising a homogeneous mixture of polyvinyl alcohol with an average Molar weight of 20,000 to 100,000 g / mol, preferably 28,000 to 40 000 g / mol, and a degree of hydrolysis of 80 to 95%, preferably 85 to 90%, and polyacrylic acid with an average molecular weight of 450,000 to 4,000,000 g / mol, preferably 1 300 000 to 4 000 000 g / mol, wherein the weight ratio of polyvinyl alcohol to polyacrylic acid in the polymer film in the range 10: 1 to 1: 1.

In an advantageous embodiment contains the moist self-adhesive polymer film 0.1 - 20% essential oils.

The polymer film of the invention is a solvent-free matrix system of the synthetic polymers polyvinyl alcohol and polyacrylic acid, which adheres only to moisturized skin, which automatically and painlessly detached after drying of the skin / matrix and with simple technical means is inexpensive to produce.

When Particularly suitable polymer films have been shown in which the weight ratio Polyvinyl alcohol to polyacrylic acid in the film in the range 5: 1 to 3: 1.

The moist self-adhesive polymer film can continue with other active substances equipped for skin treatment become. For example, with pharmaceutical and / or cosmetic active ingredients doped for continuous release into the skin or wound be. Preferred pharmaceutical active ingredients are dexpanthenol, Lidocaine and urea called, as preferred cosmetic agents For example, the groups of flavonoids and sericosides may be mentioned. The proportion of active ingredients in the polymer film is advantageously 0.01 to 10% by weight. The active ingredient becomes weaker during polymer formation introduced known processes in the polymer matrix.

In the simplest embodiment Can the wound dressing as thin Apply film on moistened skin.

to increase the internal strength of the polymer film can be one or two sides embossed be. Similarly, by an inserted grid of synthetic or natural Tissue be made reinforced polymer film. Suitable fabrics include, for example, cotton mesh fabrics a mesh size of 1 to 2 mm or a perforated fleece of 67% Viscose and 33% polyester in question.

In a further embodiment the polymer matrix is unilaterally coated with a carrier material (fabric, nonwovens, mousses, Plastics, etc.) covered and applied as a composite film. ever after used carrier material can thereby the water vapor permeability, the release rate of the essential oils, the padding against pressure and other physical properties of the polymer film to be controlled.

Of the Decisive advantage of the polymer film is its on moist Basic self-adhesive property, which is an additional application of an adhesive layer on the matrix, to fix the film in the area of the skin, superfluous. this leads to et al for a cheap and easy method of production.

The special property of the moist adhesive property of the polymer film according to the invention explained from the finely divided incorporation of the hydrophilic polyacrylic acid into a only moderately hydrophilic Polyvinylalkoholnetzwerk. Polyacrylates according to the invention have due their carboxylate function a strong charge affinity to water. The superficial Moisturizing the skin is this for the adhesive properties necessary moisture present and the Polymer film thus absorbs under gel formation on the skin. The significantly lower hydrophilicity of Polyviniylalkohols provides for a uniform distribution the moisture in the polymer matrix. Due to the poor gelation capacity of the Polyvinyl alcohol, however, remains the strength of the matrix receive. As soon as due to progressive permeation in the Foil and evaporation from the surface insufficient moisture is more, the proportion of polyacrylic acid gel dries out and the matrix loses its grip.

According to the invention advantageous Polyacrylates are acrylate-alkyl acrylate copolymers as mentioned previously.

to Preparation of the film containing moist adhesives containing essential oils a film-forming polymer of high cohesiveness, e.g. polyvinyl alcohol (Mowiol 18/88, Fa. Hoechst) with an average molecular weight from 20,000 to 100,000 g / mol, preferably 28,000 to 40,000 g / mol, and a degree of hydrolysis of 80 to 95%, preferably 85 to 90%, with a gel-forming polyacrylic acid polymer, such as. Carbopol 980 of the company Goodrich, with an average Molecular weight of 450,000 - 4 000 000 g / mol, preferably 1 300 000 to 4 000 000 g / mol wherein the weight ratio Polyvinyl alcohol to polyacrylic acid in the range 10: 1 to 1: 1, combined.

Both Polymers are used in water as a solvent at 60 to 90 ° C in a forced mixing mixer, such as. a kneader, solved or swollen and homogeneously mixed together. Subsequently, will the resulting viscous mass flat and then dried to the foil. It is important to note that due to the manufacturing process, only such essential oils in the Feuchklebende polymer matrix are incorporated, the boiling point is significantly higher than that of the water.

to change the physical properties of the film, e.g. the elasticity can during the Kneading appropriate additions such as polyethylene glycol (Lutrol E400, Fa.BASF), etc. are incorporated.

When Pharmaceutical / cosmetic agents may additionally wound healing-de Agents e.g. Dexpanthenol and / or other substances in the matrix be incorporated.

thermal sensitive active ingredients which incorporation into the matrix at 60 to 90 ° C can not let that happen be incorporated by first preparing the matrix without active ingredient and dry. These temperature-sensitive agents can subsequently be used in dissolved in a slightly hydrophilic medium, absorbed by the matrix become.

to Adjustment of a particularly skin-friendly pH of the moist adhesive polymer film, and / or for influencing the gel properties the moist polyacrylic acid can also appropriate pH corrigents such as trometamol, triethanolamine etc. are incorporated into the matrix.

optional For production in a kneader, the polymer film can also be continuous be prepared in an extruder.

self-adhesive Comprising polymer matrix of a water-gelling polymer preferably at least one polyacrylic acid polymer, water, seaweed extract and alcohol, as well as essential oils for delivery to the breath.

The Matrix consists of one of a water-gelling polymer, preferably polyacrylic acid gel, as adhesion-determining component. As a seaweed extract is preferably used agar-agar. In particular, alcohol is a or polyhydric alcohols, preferably glycerol, used as Consistency factors act.

Prefers Seaweed extract to be used is agar agar and carrageenan. Carrageenan is a hydrophilic polysaccharide of high molecular weight, from various red algae, notably Chondrus crispus Hot water extraction, subsequent freezing and subsequent purification is obtained. The structure of carrageenan consists mainly of repetitive ones Galactose and 3.6 anhydrogalactose units, both in sulfated like unsulfated form. The most important difference between kappa, iota and lambda carrageenan is the number and position of ester sulfate groups at the repeating galactose units.

A Gelation of carrageenan is possible only in the presence of cations. According to the invention preferred are kappa and iota carrageenan, which in the presence of calcium (kappa and iota), potassium and ammonium ions (kappa only) gels. Especially advantageous is the use of appropriate cation hydroxides, since also for the preparation of gel matrix systems according to the invention used polyacrylic acid for Training stable gels must be neutralized.

Industrial Carrageenan is offered e.g. by Lehmann & Voss & Co. under the names Gelcarin, Viscarin and Seaspen.

Seaweed extract, as according to the invention especially preferably agar-agar, is a hydrophilic colloid of polysaccharide structure consisting of the gelling agarose and the non-gelling agaropectin, the from different sea algae of the Rhodophyceen class by hot water extraction, subsequent freezing and subsequent purification is obtained. Agar-agar is offered industrially, e.g. from the Riedel de Haen AG.

Of the Extract, especially agar-agar or carrageenan, is preferred in an amount of 0.1-15% by weight, more preferably between 0.5 and 5% by weight. All Percentages are based on parts by weight of the polymer matrix unless otherwise stated.

One- or polyhydric alcohols, e.g. Glycerol (1,2,3-propanetriol), are among others as a solubilizer or humectants widely used adjuvants of pharmaceutical industry.

One- or polyhydric alcohols, e.g. Glycerol are preferred according to the invention in an amount of 1 - 85 % By weight, more preferably between 5 and 45% by weight. Of the Proportion of water-gelling polymer, e.g. Polyacrylic acid gel in The matrix regulates the adhesion. Unlike agar-agar, however, polyacrylic acid forms with both water as well as with alcohols gels, so that adjusted by the proportion of polyacrylic acid adhesiveness independently remains constant from the respective alcohol content. The proportion of essential oils in the Matrix is preferably 0.1 - 20 %.

According to the invention advantageous Polyacrylates are acrylate-alkyl acrylate copolymers as previously mentioned.

The gelling polymer in water, in particular polyacrylic acid and / or their copolymers are preferably used in an amount of 2 to 55% by weight, more preferably between 5 - 30 % By weight used.

The Preparation of the polymer matrices is carried out without using organic Solvents preferably at 40 - 95 ° C, in commercial Mixers / kneaders or continuously in suitable extruders.

When Water-gelling polymer is useful i.a. also monkey bread tree flour.

On This way can only be done using water in water gel-forming polymer, seaweed extract and monovalent or polyvalent Alcohol as starting materials targeted soft, supple, self-adhesive Hydrogel matrices as a basis for preparation and use as essential oils containing Make plasters, TTS, cataplasms or pads.

to Execution of special application properties can be the Polymer matrices with corresponding plasticizers, solubilizers, Penetration enhancers, neutralizing agents, e.g. tromethamol (2-amino-2- (hydroxymethyl) -1,3-propanediol), Triethanolamine (2,2 ', 2' '- nitrilotriethanol) or NaOH, fillers and / or other known additives be added, but the addition is not mandatory.

The Gel matrix can thus with hydrophilic, with suitable solubilizer also hydrophobic, drugs for wound healing or skin care doped become. When incorporating hydrophobic active ingredients, it may be of Be useful to use cyclodextrins for encapsulation.

cyclodextrins (Cycloamyloses, cycloglucans) are in cosmetic and pharmaceutical Preparations known per se.

The Improvement of solubility sparingly Substances in the presence of cyclodextrins in aqueous medium is for individual Substances are described. Advantageously, both the inclusion compounds a substance, also called guest, with a cyclodextrin species, where both 1: 1 or 1: 2 complexes, as well as complexes with others molar ratios (Guest: cyclodextrin) possible are as well as their physical mixture.

It The cyclodextrins are cyclic oligosaccharides consisting of α-1,4 linked Glucose units. As a rule, six to eight glucose units (α-, ⎕-, or γ-cyclodextrin) connected with each other.

cyclodextrins are obtained on starch when exposed to Bacillus macerans. They have a hydrophobic interior and a hydrophilic exterior. Cyclodextrins and their derivatives may be due to their structure Include inclusion complexes. They are the "molecular encapsulation" of drugs suitable (for example as protective wrapping sensitive molecules in cosmetic and pharmaceutical formulations).

These applications are also described in a number of patents (eg: WO 98/55148, EP 0 579 435 . EP 0 392 608 ). In these publications, however, usually only one active ingredient is complexed by the cyclodextrin (derivative). Although multicomponent inclusion complexes are included in EP 0756 493 but, on closer examination, it is a salt rather than a two-component mixture of acid and base.

With "cyclodextrin and / or a derivative thereof " in the following both cyclodextrins with different numbers of Glucose building blocks in the ring molecule as well as derivatives of these compounds.

According to the invention the cyclodextrin (s) are preferred in cosmetic or dermatological Compositions used in a concentration of 0.0005 to 20.0% by weight, especially 0.01 to 10% by weight, and more preferably in a concentration of 0.1 to 5.0 wt .-%.

It is advantageous according to the invention use native, polar and / or nonpolar-substituted cyclodextrins. These include preferably but not exclusively methyl, especially random methyl-β-cyclodextrin, Ethyl and hydroxypropyl cyclodextrins, for example HP-⎕-cyclodextrin or HP-⎕-cyclodextrin.

The particularly according to the invention preferred cyclodextrin species are γ-cyclodextrin and hydroxypropyl-β-cyclodextrin.

• K. Uekama et al., Chemical Reviews, 1998, 98, 2045 – 2076, "Cyclodextrin drug carrier systems"
• T. Loftsson, Int. J. Dermatology, 1998, 37, 241 – 246, "Cyclodextrins: new drugdelivery systems in dermatology".
• J. Zatz et al. Cosmetics & Toiletries, 1997, 112, Juli, S. 39ff, "Applications of cyclodextrins in skin products.
• U. Citernesi, Cosmetics & Toiletries, 1995, 110, März, S. 53 ff, Cyclodextrins in functional dermocosmetics.

Another prior art is contained in the following documents:

• K. Uekama et al., Chemical Reviews, 1998, 98, 2045-2076, "Cyclodextrin drug carrier system"
• T. Loftsson, Int. J. Dermatology, 1998, 37, 241-246, "Cyclodextrins: new drug delivery systems in dermatology".
• J. Zatz et al. Cosmetics & Toiletries, 1997, 112, July, p. 39ff, "Applications of cyclodextrins in skin products.
• Citernesi, Cosmetics & Toiletries, 1995, 110, March, p. 53 et seq., Cyclodextrins in functional dermocosmetics.

The used according to the invention Cyclodextrins or cyclodextrin-guest inclusion complexes or the cyclodextrin substance Mixtures can be without difficulty in the polymer matrix incorporated.

Next Polyurethane, polyisobutylene or polyacrylic acid matrices is also a metallocene polyethylene nonwoven fabric as a carrier material suitable for the essential oils.

• • ein Flächengewicht von 40 bis 200 g/m², insbesondere von 60 bis 120 g/m², und/oder
• • eine Dicke von 0,1 bis 0,6 mm, insbesondere von 0,2 bis 0,5, und/oder
• • eine Höchstzugkraft-Dehnung längs von 400 bis 700% und/oder
• • eine Höchstzugkraft-Dehnung quer von 250 bis 550%.

The metallocene polyethylene nonwoven fabric preferably has the following properties:

• A basis weight of 40 to 200 g / m ² , in particular of 60 to 120 g / m ² , and / or
• A thickness of 0.1 to 0.6 mm, in particular of 0.2 to 0.5, and / or
• A maximum tensile elongation of 400 to 700% and / or
• • a maximum elongation at break of 250 to 550%.

thereupon can as carrier materials known nonwovens are used, which are mechanically solidified, namely by oversewing with separate threads or by meshing.

In the first case, the nonwoven-Faden-Nähgewirke arise. To produce this, a non-woven fabric is presented, which may be, for example, cross-paneled and by means of separate threads in fringe or Trikotle is sewn.

These Nonwovens are under the name "Maliwatt" (by the company Malimo) or Arachne known.

at The second type of solidification is also preferably one quergetäfeltes Fleece submitted. While of the solidification process draw needles from the web itself fibers out and form them into stitches, where in fringe seams arise. This nonwoven sewing knit is under the name "Malivlies", also from the Company Malimo, spread.

An overview of the various types of mechanically bonded nonwoven fabrics is the article "Lamination of car-upholstery fabrics with non-woven fabrics "by G. Schmidt, Melliand Textilberichte 6/1992, pages 479-486.

In summary can be found that all rigid as substrates and elastic sheets made of synthetic and natural Raw materials are suitable. Preferred are support materials used in this way can be that they meet the characteristics of a functional association. exemplary are textiles such as fabrics, knitted fabrics, nonwovens, nonwovens, laminates, nets, Foils, foams and papers listed. Next you can these materials are pre- or post-treated. Common pretreatments are corona-treated and hydrophobic; common aftertreatments are Calendering, tempering, laminating, punching and covering.

When Barrier layer for a matrix according to the invention all films impermeable to essential oils are suitable, that will not be attacked or destroyed by the Matrix over time. Appropriate barrier layers can while simple polymer films such. be made of polyester as well as composites chemically or physically different films or metallic barrier layers, e.g. a vapor-deposited aluminum layer, as well as composites of films with metal layers. According to the invention preferred is a polyethylene terephthalate film. (Hostaphan RN MED 8.0; Mitsubishi Polyester film) is particularly advantageous if that the carrier material and a gfs. used barrier layer sterilizable, preferably γ- (gamma) sterilizable, is.

By a variation of the outer shape, as in 5 is shown, the described drug delivery systems, the application is made possible at different points of the body. The following sizes are defined for the individual shapes:

The 1 to 6 explain the use according to the invention and the structure of the drug delivery systems.

1 : While the 1a describes the matrix diffusion controlled release of the essential oils into the air, describes the 1b the membrane permeation controlled release of the oils for diffusion through the skin. It means:

1

active substance-permeable carrier material with or without padding layer,

2

matrix with drug reservoir,

3

drug-impermeable film and adhesive layer,

4

layer for controlling drug release,

5

Skin surface,

6

drug-impermeable film, Barrier layer, with or without upholstery.

2 : Application area of drug delivery systems with active ingredients that change to gaseous state at body temperature.

3 : Drug delivery system with simultaneous application by the air and by transdermal diffusion.

4 : Description of the preparation of essential oil-containing drug delivery systems made of polyurethane. It means

A, B and C

the Components base, reactor and activator;

1

mixing chamber the three components;

2

application site the homogeneous mixture of A, B, C and the essential oils or their

components;

3

Polypropylene film;

4

siliconized Polyester film;

5

Hot press;

6

Polypropylene film;

7

fleece-like Polymer;

8th

Press;

9

ready Product;

10

treadmill

5 : Different forms of drug delivery systems that allow adaptation to the site of application.

6 : Possibilities for application of essential oils from differently designed drug delivery systems. It means:

1

fleece-like Polymer,

2

polyurethane or polyisobutylene matrix with essential oils,

3

Protector,

4

Blocking layer, the no penetration capacity for essential oils shows

5

permeationskontrollierende Membrane for the release of the essential oils.

6a

diffusion-controlled Release by transdermal and per inhalation application,

6b

diffusion-controlled Release by inhalation,

6c

membranpermeationskontrollierte Release in transdermal Applikatipon and

diffusion-controlled Release by inhalation,

6d

diffusion-controlled Release for transdermal administration,

6e

membranpermeationskontrollierte Release for transdermal administration,

6f

membranpermeationskontrollierte Release for application by inhalation,

6g

membranpermeationskontrollierte Release for application by inhalation,

6h

membranpermeationskontrollierte Release for transdermal and per inhalation

Application.

in the The following are examples of preferred embodiments of the subject invention described without wishing to limit the invention unnecessarily. The specified Percentages refer to percentages by weight, based on the Total mass of polymer matrix, unless otherwise specified.

Example 1:

Production of a Drug Delivery System made of Polyurethane, which contains 4.5% Oleum Pini Pumilionis as an effective component. Due to the expectorant properties of the oil, it is used in bronchitis, asthma and paranasal sinusitis. Other indications include muscle and joint pain associated with sore muscles, arthritis, rheumatism and muscle spasms. Initial weight [%] polyether polyol 76.9 superabsorbent 9.0 Oleum Pini Pumilionis 4.6 hexamethyldiisocyanate 7.7 Bismuth compound 10% 1.8

 Example 2:

Production of a Drug Delivery System made of Polyurethane, which contains 6.6% Oleum Caryophylli as active substance. As an indication of the essential oil is given its local anesthetic and disinfecting effect, which is used in particular in dentistry. In addition, the oil has an anti-inflammatory effect, which is used for pain in the muscles or joints. Initial weight [%] polyether polyol 70.2 α-tocopherol 4.4 superabsorbent 8.8 Oleum Caryophylli 6.6 hexamethyldiisocyanate 7.4 Bismuth compound 10% 2.6

Example 3:

manufacturing of drug delivery systems by incorporation of Oleum Aurantii or Oleum Citri in a polyurethane matrix. The essential oils were with a concentration of 2.2% and 4.5% incorporated into the polyurethane matrix. The resulting product can be used as a deodorant or to improve indoor air be used.

Example 4:

Production of a drug delivery system made of polyurethane, which contains 12.9% Oleum Lavendulae as an effective component. The essential oil is used as a mild-acting antidepressant and sedative in restlessness, nervous exhaustion and sleep disorders. Its action is due to a calming of the central nervous system by the release of the neurotransmitter serotonin. Initial weight [%] polyether polyol 69.0 superabsorbent 8.6 Oleum Lavendulae 12.9 hexamethyldiisocyanate 7.3 Bismuth compound 10% 2.2

 Example 5:

Production of a drug delivery system made of polyurethane, which contains 19.1% Oleum Rosmarini as an effective component. The rosemary oil is suitable for the treatment of muscle pain and muscle cramps. While the oil acts as a balancing agent for nervous tensions even in small doses, a high dose must be used to compensate for fatigue and increase self-confidence Initial weight [%] polyether polyol 65.9 superabsorbent 7.8 Oleum rosemary 19.6 hexamethyldiisocyanate 5.2 Bismuth compound 10% 1.5

 Example 6:

Production of a drug delivery system of polyurethane, which contains as effective components Oleum Eucalypti, Oleum Pini pumilionis and Oleum Menthae piperitae. The essential oil is used to treat diseases of the bronchial area or in migraine attacks with tension headaches. Weighing (%) polyether polyol 68.1 α-tocopherol 4.6 superabsorbent 9.1 Oleum Eucalypti 2.1 Oleum Menthae piperitae 2.3 Oleum Pini pumilionis 4.6 hexamethyldiisocyanate 6.9 bismuth compound 2.3

Example 7:

Production of a drug delivery system made of polyurethane, which contains Oleum Thymi in proportion A as an effective component. The essential oil is used to treat infections and diseases of the bronchial area. It is also possible to use Oleum Thymi for the treatment of headache and muscle pain. Initial weight [%] polyether polyol 78.6 superabsorbent 9.0 Oleum Thymi 2.3 hexamethyldiisocyanate 8.3 bismuth compound 1.8

 Example 8:

For the preparation of a perfume, which was incorporated into a delivery system, a recipe was selected, which contains in addition to Oleum Bergamottae, Oleum Aurantii, Oleum Citri and Oleum Lavendulae. Due to the delayed release of the essential oils, the fragrance of the perfume is maintained over a much longer period compared to a normal perfume. Initial weight [%] polyether polyol 69.0 α-tocopherol 6.3 Oleum Bergamottae 10.9 Oleum Aurantii 1.2 Oleum Citri 1.2 Oleum Lavendulae 2.3 hexamethyldiisocyanate 6.8 bismuth compound 2.3

 Example 9:

The following drug delivery system is based on polyisobutylene and is due to the active ingredient Oleum Menthae used for the treatment of migraine attacks, with a combination with paracetamol leads to a meaningful improvement in therapy. The application of the drug delivery systems takes place in the area of the lateral end sections. [%] Vistanex LM MH 27,20 Vistanex MM L80 16.60 Elastoflex Pls E1003D 14,20 Elcema P 020 22,75 Cetiol V 7.50 Oleum Pini Pumilionis 11.75

 Example 10:

The following recipe describes a system based on polyisobutylene, which can be used to aromatize the air. [%] Vistanex LM MH 32.50 Vistanex MM L80 12.60 Elastoflex Pls E1003D 10.40 Elcema P 020 22,50 castor oil 5.00 Oleum Citri 6.00 Oleum Bergamottae 8.00 Oleum Aurantii 3.00

 Example 11:

manufacturing a drug delivery system of polyisobutylene, which is effective as Component Oleum Pini Pumilionis contains. Pine needle oil is added Diseases are used in the respiratory tract, whose Cause infections, asthma, sinusitis and bronchitis are. Besides these indications, pine oil can be used to treat muscle and joint pain with sore muscles, arthritis, and rheumatism following muscle spasms be used. Furthermore is the pine needle oil like the peppermint oil able to stimulate circulation and blood pressure during hypotension to increase.

Example 12:

manufacturing a drug delivery system of polyisobutylene, which is effective as Component Oleum Aurantii contains. As indications of the essential oil can be physical Tension, pain in the area of the musculature and production called an optimistic mood and calming nervousness become. Furthermore, the oil has an appetizing and digestive effect and it will in the field of cosmetics for dry and chapped skin, for softening dryness and keratinized skin and used in the treatment of orange peel.

Example 13:

In the following polyisobutylene-based drug delivery system, essential oils are processed DE 3540515 cause swelling of the nasal mucosa, thereby reducing snoring. The drug delivery system is applied before sleeping in the area of the upper lip. [%] Vistanex LM MH 25,00 Vistanex MM L80 16.60 Elastoflex Pls E1003D 13.10 Elcema P 020 27,30 Cetiol V 7.50 Oleum Menthae 2.50 Oleum Eucalyptus 5.00 Oleum Pini Pumilionis 3.00

Example 14

The preparation of these polyacrylic acid matrices containing essential oils is carried out solvent-free, preferably at room temperature, in commercially available kneaders or suitable extruders. [%] polyacrylic acid 22.5% by weight Polyvinylpyrrolidone, PVP 25 3.5% by weight propanediol 30.5% by weight polyethylene glycol 12.0% by weight silica 11.5% by weight dexpanthenol 5.0% by weight eucalyptus oil 15.0% by weight

 Example 15

Silicone matrices containing eucalyptus oil Carbopol 32.0% by weight Q7-9600 A 23.4% by weight Q7-9600 B 13.9% by weight Silicone PSA 29.7% by weight eucalyptus oil 1.0% by weight

 Example 16

Kutschukmatrix containing peppermint oil. peppermint oil 3,000% Colan 46 2.099% Keromet MD 100 0.262% Filler IR 13.120% Crepe 11.546% Ameripol 1011 21.591% Natsyn 2200 8.397% Resin 115 11.021% Resin 95 9,971% Resin SE 10 8.922% yellow oil 5.377% Wool wax DAB 4,724%

Example 17

SBC hotmelt matrix containing peppermint oil Kraton D-1113, Kraton: 43.87% by weight Escorez 5380, Exxon: 24.54% by weight Sylvares TR 7115, Arizona 21.90% by weight Whitemor WOM 14, Castrol 3.84% by weight Cetiol V, Henkel 4.35% by weight Irganox 1010, Ciba-Geigy 0.78% by weight peppermint oil 0.72% by weight

 Example 18

Moisture-adhesive polymer film based on PVA / PAS with eucalyptus oil Mowiol 18/88 73.40% Carbopol 980 16.00% dexpanthenol 5.00% Lutrol E 400 5.00% Euklyptusöl 0.60%

Claims (12)

Use of a polymer matrix containing essential oils for the production of drug delivery systems for transdermal and / or per inhalation application of essential oils in aromatherapy, characterized in that the system is composed of a - comprising polymer matrix - polyisobutylene containing Cetiol V or castor oil, - Polyurethane, polyacrylic acid containing PVP, silicone, rubber or SBC hotmelt matrices, PVA / PAS-based wet-adhesive polymer film or agar / PAS-based gel matrix, wherein one or more essential oils are present in the matrix or their constituents are distributed homogeneously, and - a carrier layer, - optionally a blockade layer impermeable to essential oils, - optionally one or more permeation-controlling membranes, - optionally a pressure-sensitive adhesive layer and - a peelable protective layer. Use according to claim 1, characterized that the essential oils or their constituents in a concentration range of 0.1-20.0% by weight, preferably from 5 to 10 wt.%, Based on the polymer matrix used become. Use according to claim 1 or 2, characterized that in the polymer matrix at least one additive for improvement the cohesiveness of the matrix and / or to increase the solubility of the essential oil in the Matrix is included Use according to claim 1, 2 or 3, characterized that is chosen as the matrix polyisobutylene and the polyisobutylene matrix is composed of 5 - 30 % By weight, preferably 10-20 % By weight, high molecular weight polyisobutylene, 20-60% by weight, preferably 25-40% by weight, low molecular weight polyisobutylene, 5 to 30% by weight, preferably 5 to 20% by weight, amorphous poly-α-olefin, 5 - 50 % By weight, preferably 10 - 40 % By weight, hydrophilic filler, 2.5 - 20 % By weight, preferably 5 - 15 Wt.% Cetiol V or castor oil and 0.1 - 20 % By weight, preferably 2.5-15 % By weight, essential oils or their components. Use according to claim 1, 2, 3 or 4, characterized in that as a peelable protective layer coated with silicone, polyethylene or polytetrafluoroethylene Paper, polypropylene, polyester or aluminum coated films is used. Use according to one the preceding claims, characterized in that as a blocking layer polycarbonate, polyamide, Polyethylene, polyester or an aluminum-coated film is used. Use according to one the preceding claims, characterized in that as permeation-controlling membrane Polyethylene terephthalate, polypropylene, ethylene vinyl acetate, polyethylene, Polyurethane or ethylene-vinyl copolymers membranes is used. Use according to one the preceding claims, characterized in that as a pressure-sensitive adhesive layers of Polyurethane, polyisobutylene or acrylate-based polymers used become. Use according to one the preceding claims, characterized in that in the polymer matrix superabsorbent are included. Use according to one the preceding claims, characterized in that in the polymer matrix α-tocopherol is included. Use of the drug delivery system according to one of the preceding claims as a deodorant or perfume dispenser to improve the room air. Use of the drug delivery systems according to one of claims 1 to 10 for application to the Dress.