DE102007046202A1 - Medium for preventing or relieving pain, muscular strain particularly in muscle, for improvement of immune condition, wound healing or for reduction or recovery of arteriosclerosis, has mixture of tocotrienols and gamma linolenic acid - Google Patents

Abstract

The medium has a mixture of tocotrienols and gamma-linolenic acid (GLA, 18:3 omega 6) or dihomo-gamma-linolenic acid or other substances. Omega-3-fatty acid alpha-linolenic acid (LNA), which form eicosapentaenoic acid in the body, and docohexaenoic acid are also provided, where the fatty acid is present as triglyceride or as free fatty acid or in another compound. The LNA is supplemented or replaced by sesamin or curcumin. ACTIVITY : Analgesic; Antipruritic; Immunomodulator; Vulnerary; Antiarteriosclerotic. MECHANISM OF ACTION : None given.

Description

described becomes a remedy in the sense of maintaining health (wellness) of skin, muscles, joints and cartilage preventative or for the shortening of recovery periods can be used. Through the medical effects described in the research tocotrienols are also becoming a number of medical applications in cancer, cardiovascular diseases or arteriosclerosis.

Technical background

in the Daily life is subject to skin, muscles, cartilage and Joints or other body parts often heavy-duty, symptoms such as pain, soreness, fatigue, Itching, redness and in need of long recovery periods demonstrate. Addressed here are stresses z. Through sports, Cold, sun exposure, cigarette smoke, wet or normal functioning immune defense, which normally man overcomes automatically can, for but support the body functions in the sense of the wellness idea is desirable.

All related pain, redness or swelling etc. Reactions are caused by the series-2 eicosanoids (eicosanoids, the arising from the arachidonic acid) modulated. The eicosanoids are usually subdivided into prostaglandins, thromboxanes, and leucotrienes.

Farther damage occurs in biological systems (cells) the life-sustaining components (genetic material, enzymes, other molecules) by "free radicals." Free radicals are molecules, by their chemical aggressiveness, especially their oxidizing power, life-sustaining components of cells or body fluids destroying or weakening in their function or new, generate harmful substances. Free radicals are created by many influences, including through tissue penetrating Radiation (UV, light, ionizing radiation) and chemical influences like cigarette smoke or others through the lungs or the digestive system absorbed substances. Free radicals are also caused by the "normal" Functions of the cell, such as energy production (cellular respiration), especially during sports.

It would not be an exaggeration, considering any cell aging as an effect of free radicals. That is why in the Nutrition also the intake of radical scavengers (Antioxidants) such. As Vitamin C or Vitamin E recommended, the can neutralize free radicals.

It seems puzzling, why the organism often in excess Serie-2 Eicosanoids produced (eg pain-enhancing). These Reactions appear useful in a biological environment of collectors and hunters, in which the genetic evolution of man by far predominantly took place.

possibly Free radicals also cause a stronger turn towards Series 2 Eicosanoids. So should the fight against free radicals not just serve the wellness idea of maintaining health, but could also be the mentioned unpleasant reactions Contain.

State of the art

One large part of the pharmaceutical industry focuses on medicines, slow or block the formation of eicosanoids - best known example: "Aspirin" or cortisone. These drugs usually focus on inactivation or attenuation of those involved in eicosanoid synthesis Molecules (enzymes).

Free Radicals are considered extreme in nutritional science recognized important parameters of health, especially with regard to on cardiovascular diseases and cancer. From this follows the recommendation the intake of various antioxidants in the diet, namely vitamin E, vitamin C, selenium, carotenes and many other.

By the patent DE000069534536T2 and other related patents in other countries have patented the topical use of tocotrienols for the purpose of improving the cosmetic appearance of the skin or hair.

Summary

By the present invention (working name Wunder-Ghee) is a means before, according to the above-described causal relationships a clear alleviation of symptoms such as pain, sore muscles, Tiredness, itching, redness or swelling let assume. This has already been empirical in experiments approved.

It is a mixture of components that can influence both the free radicals and the production of unwanted eicosanoids. This mixture works by applying to the skin throughout the body, but especially in subcutaneous organs, such as the muscles (soreness), cartilage and bone (lumbar spine) and on the skin itself. It could also be expressed in an equal composition as an edible food supplement who the.

Composition:

• 1. ein Antioxidans
• 2. Komponenten, die die Genese von Dihomogammalinolensäure (und damit Serie-1 Eicosanoide) heraufsetzen
• 3. (optional) Komponenten, die die Genese von Arachidonsäure (und damit Serie-2 Eicosanoide) herabsetzen
• 4. (optional) eine hautpflegene Trägersubstanz mit bestimmten Eigenschaften
• 5. weitere Bestandteile, die nicht ausdrücklich aufgeführt sind, sondern gemäß dem Stand der Technik zugefügt werden können, zum Zweck der verbesserten Haltbarkeit, des verbesserten Geschmacks oder Geruchs, der Verdünnung oder zur Erzielung eines nach dem Stand der Technik erreichbaren weiteren Zusatznutzens.

The present invention is based on the following components:

• 1. an antioxidant
• 2. Components that increase the genesis of dihomogammalinolenic acid (and thus Series 1 eicosanoids)
• 3. (optional) components that lower the genesis of arachidonic acid (and thus series-2 eicosanoids)
• 4. (optional) a skin-care carrier with certain properties
• 5. other ingredients which are not expressly listed, but may be added according to the prior art, for the purpose of improved shelf life, flavor or odor, dilution or to achieve a further benefit which can be achieved according to the prior art.

These are in accordance with the present invention by applied topically to the skin.

Description of components:

antioxidant

• 1. Tocotrienole (Teil der Vitamin-E Stoffgruppe) diese haben die Eigenschaft besonders gut durch die Haut einzudringen, außerdem existiert eine Vielzahl von Forschungsergebnissen, die ihnen neben außergewöhnlich starker Aktivität als Antioxidans auch eine entzündungshemmende Aktivität bescheinigen. Als Tocotrienole im Sinne dieser Erfindung werden die natürlich vorkommenden Tocotrienole (alpha-, beta-, gamme-, delta-) sowie deren Derivate bezeichnet.
• 2. Tocopherole (Teil der Vitamin-E Stoffgruppe)
• 3. Lycopin – dieses hat den Vorteil sich bei der Entschärfung der freien Radikale (Quenchingreaktion) nicht zu verbrauchen
• 4. andere Carotene
• 5. Ascorbinsäure oder deren Derivate, besonders fettlösliche

For application and penetration into the skin are various, mainly lipophilic antioxidants. Particularly suitable

• 1. Tocotrienols (part of the vitamin E substance group) have the ability to penetrate through the skin particularly well, also there is a variety of research results, which certify them in addition to exceptionally strong activity as an antioxidant and anti-inflammatory activity. As tocotrienols in the context of this invention, the naturally occurring tocotrienols (alpha-, beta-, gamme-, delta-) and their derivatives are referred to.
• 2. Tocopherols (part of the vitamin E substance group)
• 3. Lycopene - this has the advantage not to consume in the defusing of the free radicals (quenching reaction)
• 4. other carotene
• 5. ascorbic acid or its derivatives, especially fat-soluble

Components that determine the genesis of dihomogammalinolenic acid (and thus series-1 eicosanoids):

The Gammalinolenic acid (GLA) is a polyunsaturated omega-6 fatty acid, which, inter alia, in evening primrose oil, Borage oil or hemp oil occurs. This fatty acid is first produced by the enzyme D6D (delta-6-desaturase) converted into DGLA (DiHomoGammalinolenic acid), which in turn Series 2 Eicosanoide Anti-inflammatory Antagonists arise. If more DGLA is available, more of produced such desired tissue hormones. This explains the anti-inflammatory properties of oils, which contain GLA.

Components that determine the genesis of arachidonic acid (and so that series-2 eicosanoids) minimize:

• 1. The omega-3 fatty acid alpha-linolenic acid: The Conversion of the mentioned omega-6 fatty acid DGLA in Arachidonic acid is produced by the enzyme D5D (delta-5-desaturase). By but the same enzyme is also an omega-3 fatty acid in converts the (very beneficial) fatty acid EPA (eicosapentaenoic acid). Here, the omega-3 fatty acids compete with the omega-6 fatty acids same chain length. By introducing a short-chain omega-3 fatty acid such as LNA (alpha-linolenic acid) is So also the D5D activity braked and thus less Arachidonic acid is produced. The addition of alpha-linolenic acid can be done in the form of flaxseed oil that too over 60 percent of it is. The addition of alpha-linolenic acid can also be done as an oral addition, z. B. in the form of linseed oil.
• 2. D5D inhibitors - By the enzyme D5D (delta-5-desaturase) In turn, the beneficial DGLA will be in the utmost converted unwanted arachidonic acid. It is known that the sesamin contained in sesame seeds, as well the turmeric contained in turmeric (turmeric) the activity inhibit from D5d. The addition of sesamin and / or curcumin can also be done as an oral addition

The vehicle

There above components are fat-soluble to be medicated to the skin, in a lipophilic substance be solved, in an oil, a fat, a Cream, a gel, a lotion, or the like. Preferably This percentage of the mediator should be a particularly easy on the skin penetrating substance, as these accelerate the absorption can and also a thinning of the attached Prevents substances on the skin surface. By suitable Choice of the receiving medium can also be a depot effect with constant slow delivery of the attached substances can be achieved.

As a carrier medium, we propose in particular a composition containing the medium-chain fatty acid caprylic acid and / or lauric acid. Caprylic acid (octanoic acid) is used in diet preppa used as a remedy for fungal infections in the intestine. Capric acid, as well as lauric acid, are said to have fungicidal, bactericidal and antiviral properties. The addition of these components relieves the immune system and promotes by their good penetration into the skin, the Aufnahhe other substances used. Caprylic acid and lauric acid are contained as triglyceride in coconut oil, MCT oil (medium chain extract of coconut oil) in very high concentration. But they are also contained in milk fat, even in human breast milk.

Other benefits that come from applying the to be expected described invention:

• 1. Vorbeugung gegen Alterung (Anti-Aging)
• 2. Vorbeugung gegen Krebsgefahren – freie Radikale haben auch mutagene (krebserzeugende) Eigenschaften. Durch die Einbringung von Radikalfängern (Antioxidantien) in den Körper kann dieses Gefahrenpotential reduziert werden. Dies trifft auf innere und äußere Anwendung zu, wobei bei äußerer Anwendung eine bessere Konzentration von Radikalfängern an der Stelle des lokalen Auftragens zu erwarten ist.
• 3. Vorbeugung gegen Herz-Kreislaufkrankheiten: Durch Verringerung der Serie-2 Eicosanoide und Erhöhung der Serie-1 Eicosanoide werden eine Vielzahl von Parameter im Körper positiv im Sinne der Gesunderhaltung gegen Herz- und Kreislauf- Erkrankungen gesteuert. Hierzu gehören die Neigung zu Blutzusammenklumpung (Platalet Aggregation), die Blutdurchlässigkeit der Kapilaren, die Produktion von Cholesterin. Durch Antioxidantien kann die gefürchtete Oxidation von Cholesterin in bei Arteriosklerose herabgesetzt werden.
• 4. Vorbeugung gegen Wasseransammlungen: Durch Verringerung der Serie-2 Eicosanoide und Erhöhung der Serie-1 Eicosanoide wird auch die Neigung zur Ansammlung von Wasser im Körper herabgesetzt.

Besides the already described desired effects of this invention as a wellness agent, the following positive effects are to be expected:

• 1. Prevention of aging (anti-aging)
• 2. Prevention of cancer hazards - free radicals also have mutagenic (carcinogenic) properties. The introduction of radical scavengers (antioxidants) into the body can reduce this risk potential. This applies to internal and external application, with a better concentration of radical scavengers at the site of local application being expected when used externally.
• 3. Preventing Cardiovascular Disease: Reducing Series-2 eicosanoids and increasing Series-1 eicosanoids positively regulate a variety of parameters in the body to help maintain good health against cardiovascular disease. These include the tendency to clumping (Platalet aggregation), the blood permeability of capillaries, the production of cholesterol. Antioxidants can reduce the dreaded oxidation of cholesterol in arteriosclerosis.
• 4. Preventing water retention: Reducing Series-2 eicosanoids and increasing Series-1 eicosanoids also reduces the tendency for water to accumulate in the body.

QUOTES INCLUDE IN THE DESCRIPTION

This list The documents listed by the applicant have been automated generated and is solely for better information recorded by the reader. The list is not part of the German Patent or utility model application. The DPMA takes over no liability for any errors or omissions.

Cited patent literature

• - DE 000069534536 T2 [0010]

Claims (14)

The application of a remedy for the topical application to the skin, consisting of a mixture of the one or more antioxidants selected from a group consisting of tocotrienols, tocopherols, lycopene or others Carotenes, as well as gamma-linolenic acid (GLA 18: 3 omega-6) in an amount of more than 0.5% by weight, for the purpose of preventing or alleviating phenomena like pain, sore muscles, tiredness, itching, redness or swelling especially on muscles, joints, cartilage or of the skin. Use according to one of the preceding claims being alpha-linolenic acid (LNA 18: 3 omega-3) or one of these containing triglyceride in an amount of more than 1% or by the oral addition of linseed oil or other carriers is supplemented by alpha-linolenic acid. Use according to one of the preceding claims wherein caprylic acid or lauric acid or a these containing triglyceride in an amount of more than 4% by weight are included. Use according to one of the preceding claims wherein curcumin or sesamin are added, or by oral supplementation. The use according to any one of the preceding claims the agent being a mixture of coconut oil or extracts from it, evening primrose oil or borage oil or extracts from it, red palm oil or extracts thereof or Lycopene, in addition to possible other ingredients contains. The use according to any one of the preceding claims, wherein the agent is expressed as edible (food supplement). Use according to one of the preceding claims, For the purpose of tumor formation (cancer) to prevent or unlikely or prevent tumors from enlarging, or to promote their regression Use according to one of the preceding claims 1 to 5, with the possible omission of GLA, for the purpose of the formation of arteriosclerosis or other cardiovascular diseases to prevent, slow or reverse their regression promote. Use according to one of the preceding claims 1 to 5, with the possible omission of GLA, wherein the active ingredient is provided in a composition and wherein the composition causes the release of tocotrienol amount, those in research as a daily amount for avoidance or treatment of cardiovascular diseases is proposed (currently about 100-200 mg daily). Use according to one of the preceding claims 1 to 5, with the possible omission of GLA, wherein the active ingredient is provided in a composition and wherein the composition causes the release of tocotrienol amount, those in research as a dose to prevent or treat Cancer diseases is proposed. Use according to one of the preceding claims 1 to 6, with the possible omission of the addition of GLA, wherein the active ingredient is provided in a composition and wherein the composition is the daily dose of tocotrienol causes the recommended in nutritional research Daily dose of the intake of vitamin E includes (currently about 12-20 mg daily). Use according to one of the preceding claims 1 to 5, with the possible omission of GLA, for the purpose of slowing down aging processes (anti-aging). Use according to one of the preceding claims 1 to 5, with the possible omission of GLA, for topical application to the skin or hair, for the purpose, the cosmetic appearance of the skin or hair, but with the use of Tocotrienols is omitted. Use according to one of the preceding claims using a textile or other protective skin (plaster) with the added benefit of a long-term delivery of the active substances, Avoiding losses through blurring, as well as the lighter ones Applicability under clothing or over longer Periods.