DE202008006708U1 - Combination of tocotrienols with long-chain fatty acids for health maintenance, pain relief and anti-inflammatory - Google Patents

Abstract

medium consisting of a mixture of tocotrienols with gamma-linolenic acid (GLA 18: 3 omega-6) or dihomogammalinolenic acid or from substances that can deliver these substances, for the purpose of contraception or relieving symptoms such as pain, soreness, fatigue, Itching, redness or swelling especially on muscles, joints, cartilage or the skin, improve the immune status, improve the skin Well-being, for health maintenance, for reduction or regression of arteriosclerosis or for improved wound healing.

Description

Patent to obtain a utility model with reference to the priority date of Patent Application 10 2007 046 202.8

These Patent describes a product with the property of production from "evil" (Series 2, inflammatory, from the arachidonic acid stemming) eicosanoids, while at the same time the "good" (Series 1 and Series 3, anti-inflammatory) Eicosanoids promoted become. Furthermore are through it beyond the health benefits of the components used to be expected, especially by the antioxidants contained.

One such remedy is of fundamental importance for medical purposes of the Maintaining health over the treatment of illnesses to "feel-good" treatments.

Technical background

By Nobel Prizes in 1986 became known as the body Eicosanoids essential parameters such as inflammation / healing, blood clotting / blood liquefaction, Pain sensation that regulates functions of the immune system and others.

in this connection acts the arachidonic acid (AA) as a substrate for the generation of the series-2 eicosanoids as well as the gamma-linolenic acid (GLA) and eicosapentaenoic acid (EPA) as a substrate for the respective opponents.

in the Generally, the eicosanoids derived from arachidonic acid become as undesirable considered, as they give reactions in the emergence of the "civilasasic diseases", as well as in all pain play an important role.

Painkiller such as As the Acatylsalicylsäure ("Aspirin") or cortisone in that they are the expression the pain-enhancing Prevent eicosanoids.

These However, funds represent a relatively strong intervention in biochemistry of the body and are associated with many side effects.

By the present invention will be the expression of the series-2 eicosanoids slowed down while at the same time the expression the positive-acting opponent is supported.

operation

• 1. Tocotrienolen
• 2. langkettigen (omega-6) Fettsäuren Gammalinolensäure oder Dihomogammalinolensäure (GLA oder DGLA)
• 3. sowie optional die langkettigen (omega-3) Fettsäuren Eicosapentaensäure (EPA) und/oder Docosahexaensäure (DHA) und/oder Alpha-Linolensäure (18:3, omega-3). Letztere kann durch die Pflanzenstoffe Curcumin oder Sesamin (vorhanden in Gelbwurz/Turmerik bzw. Sesam) ergänzt oder ersetzt werden.

The present invention is based on the synergistic effect of

• 1. tocotrienols
• 2. long-chain (omega-6) fatty acids gammalinolenic acid or dihomogammalinolenic acid (GLA or DGLA)
• 3. and optionally the long chain (omega-3) fatty acids eicosapentaenoic acid (EPA) and / or docosahexaenoic acid (DHA) and / or alpha-linolenic acid (18: 3, omega-3). The latter can be supplemented or replaced by the plant substances curcumin or sesamin (present in turmeric / turmeric or sesame).

By Collaboration of these substances arises one another reinforcing Effect that over the expected effect of the individual substances significantly.

Empirical experiments

tries with test persons have revealed that the mixture described in its analgesic property of the action of cortisone preparations or some analgesics without having side effects.

• 1. Sonnenbrand/Rötung nach Sonnenbädern: auch recht starke Rötungen wurden nach kurzer Zeit gelindert, die Haut machte nach kurzer Zeit einen gesunden Eindruck, schnelle Bräunung wurde erzielt
• 2. „Hexenschuss" einige Stunden nach Auftragen in Gegend der Lendenwirbelsäule trat eine deutliche Linderung ein.
• 3. Schmerz an überlasteten Sehnen (Karpaltunnel): nach 2–3 maligem Auftragen trat eine deutliche Linderung und schneller Heilungsverlauf ein.
• 4. Schmerz an der Wirbelsäule bei Morbus Bechterev: nach wenigen Stunden trat deutliche Linderung ein.
• 5. Verbrennungen: nach Kühlung sofortiges Auftragen des Mittels auf die verletzte Stelle bewirkte eine ungewöhnlich schnelle und schmerzfreie Heilung
• 6. kleinere Wunden: die Wundheilung ohne Narbenbildung scheint verbessert zu sein
• 7. Haarwuchs: nach einigen Wochen täglichen Auftragens der hochkonzentrierten Mischung auf die Kopfhaut schien sich Haarflaum zu bilden

In the following tests easily comprehensible impressive effects of the desired kind were achieved:

• 1. Sunburn / redness after sunbathing: also quite strong redness was relieved after a short time, the skin made after a short time a healthy impression, fast tanning was achieved
• 2. "lumbago" a few hours after application in the area of the lumbar spine occurred a significant relief.
• 3. Pain on overloaded tendons (carpal tunnel): after 2-3 applications, clear relief and faster healing occurred.
• 4. Pain in the spinal column in ankylosing spondylitis: after a few hours clear relief occurred.
• 5. Burns: immediate application of the product to the injured area after cooling caused an unusually fast and painless healing
• 6. minor wounds: wound healing without scarring seems to be improved
• 7. Hair Growth: After a few weeks of daily application of the highly concentrated mixture to the scalp, hair follicles appeared to form

These Experiments should be done by placebo-controlled double-blind studies corroborated become.

Discussion of the substances

1. Tocotrienols

The fat-soluble Vitamin E occurs in nature in eight forms, namely alpha, beta, gamma, and delta-tocopherol, as well as alpha, beta, gamma, and delta-tocotrienol. In nature, tocotrienols are found in red palm oil, in rice oil and in Coconut oil in to a significant extent.

Compared to the often Tocopherols used in (eg, in cosmetics) have tocotrienols a polyunsaturated Side chain up. Presumably, this can Tocotrienols considerably better penetrate into tissues and cell membranes around there their effect to unfold.

In The research has shown a 40-60-fold higher antioxidant effect on the cell membrane of tocotrienols compared to tocopherols. These Extraordinary antioxidant effect may be the result of inflammation arising and the inflammation reinforcing neutralize free radicals. In addition, tocotrienols act directly on the genesis of the mentioned "unwanted" eicosanoids as well the genesis of cholesterol.

2. Omega-6 fatty acids (GLA and DGLA)

The DGLA (and its precursor GLA) provide the basic substance for production the (anti-inflammatory) Serie-1 Eicosanoide dar. For this reason, the supply of these fatty acids promotes the Production of Series 1 Eicosanoids.

In Nature's Gamma Linolenic Acid (GLA) in borage oil, Evening primrose oil and hemp oil contained to a significant extent.

Indeed becomes the dihomogammalinolenic acid (DLGA) in the body converted into the dreaded arachidonic acid by only one enzyme step (D5D).

Out This reason is longer term Application, a limitation of this enzyme step desirable. Serve this purpose omega-3 fatty acids and some natural substances (sesamin curcumin).

3. Omega-3 fatty acids eicosapentaenoic acid (EPA) and or docosahexaenoic acid (DHA)

These both long-chain fatty acids come naturally in a relatively high concentration in the body, especially in nerve tissue and in the brain.

she are the most important in fish oil contained ingredients.

she can the release of arachidonic acid inhibit and are the basis for the anti-inflammatory Series 3 Eicosanoids.

4. Omega-3 fatty acid alpha-linolenic acid (LNA)

The alpha-linolenic acid and the resulting fatty acids can inhibit the formation of new arachidonic acid, since they are around the key enzyme (D5D) compete.

at all ingredients are substances that in some Foods are found in quite high concentration.

• 1. eine Nahrungsmittelergänzung oder "functional food" mit den genannten Eigenschaften hergestellt werden kann
• 2. keine Substanz einer lebensmitteltechnischen Prüfung unterzogen werden muss
• 3. durch jahrhunderte- oder jahrtausende langen Verzehr durch den Menschen eine sehr geringe Neigung zu Unverträglichkeiten oder Giftigkeit besteht.

This has the advantage that

• 1. a food supplement or "functional food" can be produced with the said properties
• 2. no substance must undergo a food testing
• 3. is a very low tendency to intolerance or toxicity due to human consumption for centuries or thousands of years.

Dosage of ingredients

1. Dosage of tocotrienols

The amounts used in scientific studies on tocotrienols are in the range of 80 to 120 mg tocotrienol when administered orally. The dosage should be such that in typical use (cholesterol, chronic discomfort) in about this amount is achieved. In acute Complaints should be about 5 to 10 times the concentration, with long term Spa treatment can be applied about 1/10 of this amount.

tocotrienols be over The skin is even better absorbed than oral.

Deßhalb can the amount of tocotrienol when applied topically to 1/2 to 1/5 of said area can be reduced.

at oral administration, the tocotrienol must be distributed throughout the body, which distributes the local concentrations approximately over the entire body weight.

At the topical application over an affected body site can the corresponding local concentration with only 1/10 to 1/100 the amount of active ingredient can be achieved.

On the basis of these specifications, it is easy to obtain a table of the concentrations of tocotrienols For typical application (eg 0.5 g to 5 g for application), limitation of the effective range (eg 1/10 on the lumbar spine, 1/1 in arteriosclerosis) and reason for use (eg. B. 10 times in acute conditions) leads to the amount corresponding to 100 mg oral administration. (Example: lumbar spine application 5 g, factor 10% due to topical application, factor 10 due to acute case and factor 50% due to administration via the skin gives 100 mg × 10 × 10 × 50 = 50 mg administration T3 would add a concentration of 5000 mg 50 mg = 1%).

I Beat in preparations for topical application to the skin T3 concentrations from 0.1 to 25 percent ago.

2. Dosage of omega-6 fatty acids

The Daily requirements of long-chain omega-6 fatty acids are associated with a "few Grams "of science only very vague and uncertain indicated. For the desired effect of the increased Production of Series 1 Eicosanoids are the mixing ratios with the other fat classes that matter per individual difficult to assess.

The Amount of GLA (or DGLA) should be adjusted in proportion to other oils used be that they are in place after penetrating the skin Application results in a measurable concentration, that of the intended Enzymes (cyclooxygenase etc) transformed into the beneficial eicosanoids can be. I suggest a concentration with local application from 1-50% GLA ago.

3. Dosage of omega-3 fatty acid LNA (Alpha-linolenic acid)

purpose alpha-linolenic acid in the preparation it is the further processing of the DGLA in arachidonic acid by Compete to limit the enzyme d5d (delta-5-desaturase).

The Enzyme d5d has an approximately 4-fold higher affinity for omega-3 fatty acids, in comparison with omega-6 fatty acids.

I therefore suggest a concentration of 1/4 of the amount of GLA / DGLA in front.

at sufficient consumption of LNA over the nutrition could to the enclosure be omitted from LNA in the preparation described.

4. Dosage of long-chain omega-3 Fatty acids EPA and DHA

The Dosage of EPA and DHA when given orally in commercial Containers are around 500 mg / day. For topical application and under consideration of the synergy effect I hit a concentration of 1/10 to 1/100 of before, so z. B. 1 percent.

Side effects, toxicity and maximum doses

1. Tocotrienols

at Tocotrienols is a fat-soluble vitamin.

It can however over Liver and kidney are also excreted.

• – eine Menge von 12–14 mg Vitamin E entspricht der empfohlenen Tagesaufnahme
• – eine Europäische Behörde für Lebensmittelsicherheit (EFSA) definiert als tolerierbare Höchstaufnahmemenge (die Menge, die ein gesunder Erwachsener lebenslang täglich verzehren kann, ohne dass gesundheitliche Risiken zu befürchten sind) die Aufnahme von 300 mg täglich
• – eine Menge von 800 mg Vitamin E wird als nebenwirkungsfreie regelmäßige Tagesaufnahme angesehen
• – nach Angabe von Herstellern von Vitamin E Präparaten treten bei Dosierung von 1200 mg alpha-Tocopherolacetat "sehr selten" (1 oder weniger aus 10000 Behandelten), oral eingenommen, Magen und Darm-Beschwerden auf.

For vitamin E, there are approximately the following dosage guidelines:

• - An amount of 12-14 mg of vitamin E corresponds to the recommended daily intake
• - A European Food Safety Authority (EFSA) defines the maximum tolerable intake (the amount that a healthy adult can consume lifelong daily without any risk to health) of 300 mg daily
• - An amount of 800 mg of vitamin E is considered a side-effect-free regular daily intake
• - According to manufacturers of vitamin E preparations occur at a dosage of 1200 mg alpha-tocopherol "very rarely" (1 or less from 10000 treated people), taken orally, stomach and intestinal complaints.

2. GLA and DGLA and LNA

These fatty acids come in in nature, in food (vegetable oils, animal fat) and in the body in large quantities. The body It produces itself from linoleic acid in the range of a few grams on Day.

3. eicosapentaenoic acid (EPA) and or docosahexaenoic acid (DHA)

These fatty acids come in in nature, in food (fish, brain) and in the body in relatively large quantities. The body produces it itself from the alpha-linolenic acid in the range to a few + grams a day.

In summary It can be said that all components of the invention described can be considered highly harmless.

Advantages of this invention

• 1. Vermeidung von Nebenwirkungen. Alle Bestandteile sind ungiftig und weisen als natürlich im Körper vorkommende Substanzen ein sehr geringes Allergie-Potential auf. Alle Bestandteile können direkt Naturprodukten entnommen werden.
• 2. durch topische Anwendung über die Haut kann eine lokale Konzentration erreicht werden, die weit über die Konzentrationen bei oraler Gabe und die Verteilung über den Blutkreislauf hinaus geht.
• 3. Es steht ein schmerzlindernes und entzündungsreduzierendes Mittel zur Verfügung, das dank seiner Ungiftigkeit und Freiheit von Nebenwirkungen auch für die Selbstanwendung oder im Wellness-Bereich verwendet werden kann.

Particular advantages of the present invention are

• 1. Avoiding side effects. All ingredients are non-toxic and have a very low allergy potential as naturally occurring substances in the body. All ingredients can be taken directly from natural products.
• 2. By topical application through the skin, a local concentration can be achieved that goes far beyond the levels of oral administration and distribution across the bloodstream.
• 3. A pain-relieving and anti-inflammatory agent is available which, thanks to its non-toxicity and freedom from side-effects, can also be used for self-care or in the wellness sector.

applications

• As a sports gel
• To remedy (inflammatory) pain on cartilage, muscles, joints, skin
• For the improvement of allergic symptoms
• To prevent cancer by eliminating free radicals and improving of immune status
• For health care the heart / circulatory system by improving blood circulation
• In eczema
• As a hair restorer
• As a sexual enhancer (by improving blood circulation and increasing the Testosterone)
• As a skin soothing cream, skin freshener

Claims (8)

Agent consisting of a mixture of tocotrienols with gamma-linolenic acid (GLA 18: 3 omega-6) or dihomogammalinolenic acid or from substances that can deliver these substances, for the purpose of contraception or relieving symptoms such as pain, soreness, fatigue, Itching, redness or swelling especially on muscles, joints, cartilage or the skin, to improve the immune status, to improve the well-being, for health maintenance, for the reduction or regression of arteriosclerosis or for improved wound healing. complement of the composition according to claim 1 with the omega-3 fatty acid alpha-linolenic acid (LNA) or one of his derivatives in the body on the way to eicosapentaenoic acid, being the fatty acid as a triglyceride or as a free fatty acid or in another binding is present. The LNA can be supplemented by sesamin or curcumin or be replaced. complement of the agent according to claim 1 or 2 with the omega-3 fatty acids eicosapentaenoic acid, docohexaenoic acid (EPA, DHA) being the fatty acid as Triglyceride or as free fatty acid or in another bond. shaping of the agent according to claim 1 to 3 as a fatty substance for topical Apply to the body. shaping of the agent according to claim 1 to 3 as a fatty substance for oral Taking in the form of capsules, spreads or the like, even as a combination of such topically applied ingredients. shaping the agent of claim 1 to 3 using a textile or other protective skin (plaster) with the added benefit of a long-term delivery the active ingredients, avoiding losses due to blurring, as well as ease of use under clothing or for extended periods of time. shaping the agent according to one of the preceding claims, consisting of an extract from natural red palm oil or rice oil with a total tocotrienol content of 0.06 to 25% by weight; as well as evening primrose oil or borage oil with a total content of 1% to 50% of gamma-linolenic acid; such as from linseed oil with a total content of 0.25% to 25%; as well as a lipophilic Carrier. shaping the agent according to any one of the preceding claims as a food ("functional food")