DE10223925B4 - Antiperspirant composition - Google Patents

Abstract

A water-containing antiperspirant composition consisting exclusively of aluminum chloride with glycerol as a skin-friendly carrier and a cellulose ether which is selected from methylhydroxypropylcellulose and / or methylhydroxyethylcellulose, wherein the cellulose ether in a proportion of 0.1 to 10 wt .-%, the aluminum chloride in a proportion of 10 to 30% by weight, and the glycerol in a proportion of 1 to 20% by weight in the composition and optionally perfume oils, dyes, panthenol or allantoin.

Description

The This invention relates generally to a hydrous antiperspirant composition consisting of aluminum chloride with glycerol as a skin-friendly Carrier.

such Antiperspirant compositions are in the art in many ways embodiments known. They serve to promote perspiration on the skin surface, in particular under the armpits, to prevent or at least control.

The Transpiration is mainly used to thermoregulate the body and is therefore for indispensable to man. scope and intensity transpiration depends on individual factors. For this System, the sweat glands act similar to one Thermostat, as they come into action as soon as the human body is affected by external heat or is heated up as a result of physical or mental exertion, to cool the organism To provide.

Especially with excessive sweat production, For example, in hyperhidrosis, there is a need that Control production of sweat glands and / or reduce it to at least an average value.

On available on the market are predominantly antiperspirant products, containing astringent substances, such as aluminum and / or Zirconium salts.

In Compounds with perfumes and / or perfumes are antiperspirant compositions Further embodiments used as deodorants, in addition to the When you sweat you should often neutralize odor.

antiperspirants and deodorants are commercially available, for example, as creams, sprays, Pens or so-called roll-on preparations available.

in the Trade available For example, water-free pens or sprays are particularly useful to the user a dry skin feeling to convey after application. A disadvantage of these preparations is, however, that the astringent substances are often water-soluble and therefore in these anhydrous formulations are difficult to be released. Further These formulations give the user an inadequate Fresh feeling.

Of Further, anhydrous compositions are known, the volatile silicone oils as an ingredient have, however, have the disadvantage of leaving on the skin product residues and clothes to discolor.

One significant disadvantage of antiperspirants and deodorants is often their skin intolerance. Not infrequently, the skin reacts after application of the antiperspirants and / or deodorants irritates, itches or even forms an allergic Rash. these can by the carriers contained in the compositions, such as For example, silicones or ethanol, or by the active ingredients themselves, such as z. As aluminum chloride, triggered become. To avoid such negative effects, is usually the Proportion of active ingredient in the composition diminished or its Tried to reduce penetration into the skin. However, it is getting straight through these measures In turn, the performance of an antiperspirant composition is greatly reduced.

In spite of of the manifold However, a wide range of compositions is generally known that this Problem of excessive sweating not complete solved is. The commercially available Products are neither capable of segregating sweat or the Formation of odors permanently prevent.

Especially Strong sweating and hyperhidrosis often cause astringents, which are slightly tanning agents or preparations, the pores contract.

From the EP 0 781 780 A2 Cosmetic compositions are known which have as thickening agents, inter alia, hydroxyethyl cellulose or hydroxypropyl cellulose, or derivatives thereof.

From the WO 01/60329 A1 For example, cosmetic compositions are known which comprise a silicone (dimethicone copolyol ester), a thickening agent such as, for example, hydroxypropylcellulose, sorbitol and, for example, an antiperspirant active substance.

The WO 02/49590 A2 discloses an antiperspirant comprising a salt and a water-soluble polymer wherein the polymer has Bronsted acid groups and does not come into contact with the salt until applied to the skin.

In the WO 02/47621 A2 there are disclosed antiperspirant compositions which, in addition to an antiperspirant active, further comprise a silicone coupling agent.

In the US 3,198,708 B1 there is described an antiperspirant composition comprising aluminum chlorhydroxide, glycerol, cellulose ether, neomycin and ethanol. Also in the publication by Fiedler, "The sweat", Arzneimittelforschung 18. Supplement, Editio Cantor, 1968, p 310-320, such a composition is described.

In the common ones Antiperspirant compositions are nowadays mostly astringent Salts of metals, e.g. B. aluminum chloride used. In the conventional Means these drugs are usually not stable and / or sufficiently distributed before, so that she often - before they get to the sweat glands - washed off or sweat and can not exert their effect.

Furthermore there is a risk that through an insufficient one Dispersion and the resulting concentration of eg. Aluminum chloride in certain areas of the composition Applying allergic skin reactions are triggered.

task The invention therefore provides a novel aluminum chloride antiperspirant composition in which the aluminum chloride is stable and dispersed present and at the same time by an optimal drug release sweat secretion greatly reduced.

According to the invention Task solved by that the Composition further comprises at least one cellulose ether, the selected is from methylhydroxypropylcellulose and / or methylhydroxyethylcellulose, the cellulose ether being present in a proportion of 0.1 to 10% by weight, the aluminum chloride in a proportion of 10 to 30 wt .-%, and the glycerol in a proportion of 1 to 20% by weight in the composition and, if appropriate, Perfume oils, dyes, panthenol or allantoin is included.

Further the task is solved by using a composition exclusively Aluminum chloride with glycerol as a skin-compatible carrier and with a cellulose ether, as antiperspirant Skin-applying agent as defined in the claims.

The Inventors have recognized that it especially by the galenics of the antiperspirant composition possible is, the sweat production clearly to reduce. Skin irritations could be beneficial at the same time be avoided.

By the formulation is achieved by passing the aluminum chloride through the various layers of skin are delivered through to the sweat glands which allows the antiperspirant composition to target its action can unfold.

By the cellulose ether as gelling agent may be the antiperspirant composition be formulated as a gel. The cellulose ether may be particulate or powdered and natural or be of synthetic origin.

Of the Cellulose ether gives the composition a skin-friendly Character, whereby the composition is easy to apply and feels pleasant on the skin.

The The inventors were able to show in their own studies that the invention formulated Antiperspirant composition extremely effective is, so she not more often than every two days must be applied to the sweat production significantly reduce.

Especially Due to the special galenics it is achieved that the strongly reactive active ingredient Aluminum chloride in the interaction of skin-friendly carrier and cellulose ether over a longer Stable period and optimally released at the site of action. This is v. a. across from usual Antiperspirant compositions advantageous since in these aluminum chloride often insufficiently dispersed present and less stable in the formulation is incorporated.

glycerol, A trivalent alcohol has been used in cosmetics in particular as a skin care product, which in cosmetic products the Function of skin moisturizing perceives. Glycerol as hygroscopic liquid supports the skin's own moisture balance. The use of glycerol has about that addition, the advantage that by its use the astringent agent aluminum chloride the Skin layers can penetrate and so the sweat glands better reached.

methylhydroxypropylcellulose is for example as "Methocel" in the Company Synopharm, Hamburg available, Methylhydroxyethylcellulose as Tylose MH 300 from Kalle, Wiesbaden. These ethers have already proven to be good in cosmetics compatible proved.

In a preferred embodiment is the cellulose ether in a proportion of 0.5 to 1.5 wt .-% contained in the composition.

Further it is preferred that the aluminum chloride in the composition is contained in a proportion of 15 to 25 wt .-%.

Farther It is preferred that the glycerol as a skin-friendly carrier in a proportion of 5 to 15 Wt .-% is contained in the composition.

Farther it is preferred that 85% glycerol be used.

In particular, the compound of cellulose ether and glycerol ensures that aluminum chloride is finely dispersed in the gelatinous composition and is to be supported by glycerol is conducted to a desired site of action, where it leads to a constriction of the glands. This swelling of the sweat glands removes less sweat.

In In comparative studies, the inventors were able to show that the composition according to the invention because of her galenic skin was more permanent and thus was able to exert its effect more effectively on the sweat glands than with conventional sweat glands Means was the case.

Farther proved the composition of the invention as hypoallergenic and hypoallergenic, because of that the special galenics - among others Preservatives can be dispensed with.

The In addition, composition can also contain other ingredients usually included in cosmetic products, such as, for example, perfume oils, dyes, etc., and anti-inflammatory Substances such as panthenol or allantoin.

• (a) Vermengen des Cellulose-Ethers mit dem hautverträglichen Träger Glycerol,
• (b) Lösen und Aufquellen der sich in Schritt (a) gebildeten Mischung unter Einsatz von Wasser und
• (c) portionsweises Hinzufügen von Aluminiumchlorid.

To prepare the antiperspirant composition, a method can be used with the following steps:

• (a) mixing the cellulose ether with the skin-compatible carrier glycerol,
• (b) dissolving and swelling the mixture formed in step (a) using water and
• (c) adding aluminum chloride in portions.

• (a) Lösen und Aufquellen des Cellulose-Ethers unter Einsatz von Wasser,
• (b) Einrühren des hautverträglichen Trägers Glycerol, in die unter (a) gebildete Mischung und
• (c) portionsweises Hinzufügen von Aluminiumchlorid.

Another possible method comprises the steps:

• (a) dissolving and swelling the cellulose ether using water,
• (B) Stirring the skin-friendly carrier glycerol, in the mixture formed under (a) and
• (c) adding aluminum chloride in portions.

With the procedures it is possible a clear, low-viscosity gel in a simple and inexpensive way manufacture.

The Gel prepared by the method can be portioned, for example, in glass "deodorant", through which the composition is then simply applied can.

By the procedures are achieved so that the gelatinous composition can optimally dissolve and swell and that continues the aluminum chloride in the swollen gel mixture particularly finely dispersed becomes. As a result, a stable incorporation of the drug in the composition and its optimal release from the composition guaranteed.

The Add in portions of aluminum chloride has about it addition, the advantage that thereby the hydrate shell of the cellulose gel not disturbed becomes. Too fast stirring or adding huge Amounts the cellulose hydrate shell through the aluminum and Destroys chloride ions, whereby the cellulose derivatives can precipitate out. By the limited supply of aluminum chloride - preferably at low temperature - remains the hydrate shell intact, which is why the gel stays clear.

alternative can be a highly concentrated aluminum chloride solution with well-defined Drip speed or pumping and conveying speed up to desired Final concentration to be supplied.

In a preferred possible Execution of the Procedure, the release takes place and swelling the prepared mixture over a period of about 1 up to 24 hours, preferably about 12 hours.

This Period has proven in trials to be particularly favorable to the composition the optimal properties for to provide storage and release of the active substance aluminum chloride.

In a preferred possible Execution done also the release and swelling the prepared mixture at a temperature of about 2 to 10 ° C, in particular from about 4 to 8 ° C.

The Use of these conditions favors efficient production the composition and contributes continue to their conservation at.

The Manufacturing process can also carried out without problems sterile be made under laminar air flow conditions of the heat-sterilized cellulose solution a adequate Amount of sterilized or sterile filtered aluminum chloride solution is supplied.

The The invention further relates to the use of the antiperspirant composition according to the invention as antiperspirant Means for applying to the skin.

in this connection is preferred when the antiperspirant composition of the invention especially in the evening is applied.

This use provides a particularly good antiperspirant effect and makes another application the next morning liquid.

By this use is guaranteed, also because of Of the long period the aluminum chloride as an astringent to its place of action, namely the sweat glands, enter can to unfold its effect there. This avoids that one for example, in the morning applied composition due to excessive sweating is "sweated out" again, without the active ingredients have reached their destination. The active ingredients only get here into the upper areas of the excretory ducts, thereby They do not affect their action on the secreting part of the sweat glands exercise can.

The Composition according to the invention makes it possible continue to be used only every other evening, thanks galenics are extremely effective Effect can be achieved.

This is particularly advantageous over conventional means, since these often one to two times a day Application need, an antiperspirant Effect.

It understands that the mentioned above and the features to be explained below not only in the specified combination, but also in other combinations or alone, without to leave the scope of the present invention.

embodiments of the invention are in the following example and the drawing and are explained in more detail in the following description. It shows:

1 a schematic representation of a cross section through the uppermost skin layers.

In 1 is total with 10 the epidermis indicated, with the basal membrane attached to the dermis 12 borders. Through the so-called papillae 14 is the connective tissue of the dermis 12 with the epidermis 10 toothed. Furthermore, the dermis includes 12 the so-called network layer, which contains a dense network of collagen fibers.

To the dermis 12 borders the subcutis 16 in, in the fat cells 17 available. At the border between dermis 12 and subcutis 16 is with 18 Overall, a sweat gland is represented, which is a secretion part 20 and an outgoing gear 22 having. The secretion part 20 is twisted in itself and goes into the execution passage 22 over to the skin surface 24 leads and ends there in a pore. The excretory duct 22 leads spirally through the dermis 12 and the epidermis 10 ,

In sweat production, the sweat secretion in the secretion part 20 the sweat gland 18 formed and over the excretory duct 22 through the dermis 12 and the epidermis 10 to the skin surface 24 directed, where it forms small welding droplets.

In one application, the composition of the invention with aluminum chloride, with the skin-friendly carrier glycerol and with a cellulose ether on the skin surface 24 applied. The aluminum chloride penetrates under the action of the carrier glycerol, the epidermis 10 and large parts of the dermis 12 and enters the secretion part 20 the sweat gland 18 ,

In this case, an application in the evening is particularly advantageous, which allows the aluminum chloride over a relatively long period of time to get to the sweat glands. When applied in the morning, there is a risk that patients sweat a lot after getting up and starting to move, whereby the astringent substance of the previously applied composition is sweated out before the secretion part 20 the sweat gland 18 has reached.

The to the skin surface 24 leading gear 22 (or channel) or the sweat gland 18 Overall, it is lined with mucopolysaccharides. The negatively charged mucopolysaccharides have as counterion sodium, which is exchanged when using the inventive composition by aluminum ions. The trivalent aluminum ions lead to larger aggregates of aluminum mucopolysaccharides, whereby the sweat flow is inhibited and partially completely inhibited.

The astringent substance thus causes contraction of the sweat gland 18 , which inhibits overall sweat production.

example

manufacturing

1.0 g methylhydroxypropylcellulose (Synopharm, Hamburg) or optionally Tylose MH 300 (Kalle, Wiesbaden) were weighed into a beaker and 10.0 g of glycerol (85%). The cellulose was with glycerol carefully mixed and moistened. Subsequently, the approach was under stir made up to 100 ml with ice-cold distilled water. The Gel was completely dissolved and Swelled for several hours. Then followed Optionally the further steps or the gel was for further 12 h at 4 to 8 ° C stored.

To another mixing step was 20.0 g of aluminum chloride hexahydrate added in small portions to the cellulose gel. Care was taken that one further aluminum chloride portion was added only when had already dissolved the previously added aluminum chloride portion. The addition was carried out with stirring with a magnetic or propeller stirrer at approx. 600 rpm. Subsequently was the clear gel in glass deodorant (Zscheile-Klinger, Hamburg) with every 50 ml filled.

application

In front The gel was shaken in the glass deodorant rollers until application the gel composition beaded. Then the gel was in the evening of Patients with hyperhidrosis applied. The next morning was none further application, also no other deodorant. The gel was applied on the second day in the evening, the application at least over a week away.

in the Comparison with conventional Means showed that at Patients with hyperhidrosis already after one week a good success could be achieved, which showed that the gel sweating prevented or at least reduced to a normal level. Conventional means had at a similar Application comparatively worse antiperspirant properties, since here the aluminum chloride was sweated out before it at his The site of action was reached.

Claims (7)

Hydrous antiperspirant composition consisting exclusively of aluminum chloride with glycerol as a skin-friendly carrier and a cellulose ether the selected is from methylhydroxypropylcellulose and / or methylhydroxyethylcellulose, the cellulose ether being present in a proportion of 0.1 to 10% by weight, the aluminum chloride in a proportion of 10 to 30 wt .-%, and the Glycerol in a proportion of 1 to 20 wt .-% in the composition and optionally perfume oils, dyes, panthenol or allantoin are included. Composition according to Claim 1, characterized that the cellulose ether in a proportion of 0.5 to 1.5 wt .-% is included. Composition according to Claim 1 or 2, characterized that the aluminum chloride contained in a proportion of 15 to 25 wt .-% is. A composition according to any one of claims 1 to 3, characterized in that the glycerol in a proportion of 5 to 15 wt .-% is included. A composition according to any one of claims 1 to 4, characterized in that contains the following components: - 10 to 25% by weight of aluminum chloride hexahydrate 5 to 15% by weight of glycerol 85% - 0.1 to 5% by weight of methylhydroxypropylcellulose - 65 to 75 wt .-% water Use of a composition according to any one of claims 1 to 5 as antiperspirant to apply on skin. Use according to claim 6, characterized that the composition is applied in the evening.