JP2006137730A - Anti-fatigue agent or stamina enhancing agent, functional food or cosmetic - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain an anti-fatigue agent or a stamina enhancing agent, or to provide a functional food having anti-fatigue action or stamina enhancing action. <P>SOLUTION: This invention relates to the anti-fatigue agent or the stamina enhancing agent containing coenzyme Q10 and an α-lipoic acid as active components, a functional food containing the compounds as active components and having anti-fatigue action or stamina enhancing effect, the use of coenzyme Q10 and α-lipoic acid for the preparation of a composition for anti-fatigue action or stamina enhancing use, and a method for attaining anti-fatigue action or stamina enhancing effect by taking the composition containing the compounds as active components. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

  The present invention relates to an anti-fatigue agent and / or endurance enhancer containing coenzyme Q10 and α-lipoic acid as active ingredients, or an anti-fatigue action or endurance enhancement containing coenzyme Q10 and α-lipoic acid as active ingredients Use of coenzyme Q10 and α-lipoic acid for the preparation of functional foods, cosmetics, and compositions having anti-fatigue activity or endurance enhancing activity, and coenzyme Q10 and α-lipoic acid as active ingredients It is related with the anti-fatigue effect | action or endurance enhancement method characterized by ingesting or apply | coating the composition contained as.

  Coenzyme Q10 is a benzoquinone derivative and is widely distributed in the living world, so it was named ubiquinone (oxidized coenzyme Q10). A hydroquinone form obtained by reducing this by two electrons is ubiquinol (reduced coenzyme Q10). Although many homologues exist depending on the length (n) of the isoprenoid side chain (n = 1 to 12), the main homologue is determined by the species because it is biosynthesized. In mammals, n = 9 and 10 are mainly used. For example, n = 9 is often used in mice and rats, and n = 10 is often used in rabbits. For humans, n = 10.

  Coenzyme Q10 is a physiological component that exists as a constituent component of the mitochondrial electron transfer system in cells in the living body, and plays a role as a transfer component in the electron transfer system by repeating oxidation and reduction in the living body. Since coenzyme Q10 exhibits energy production and antioxidant activity in vivo, its usefulness is widely known. Coenzyme Q10 is a molecule that is biosynthesized in the human body, but it has been reported that the amount of biosynthesis decreases with age, or that the amount of coenzyme Q10 in the body in various diseases is decreased. In such diseases, external supply of coenzyme Q10 has yielded good results. Furthermore, it is considered that coenzyme Q10 needs to be replenished not only at the time of illness but also at normal times such as when the elderly or physically fatigued.

  Oxidized coenzyme Q10 is used for pharmaceutical use as a congestive heart failure drug. In addition to vitamins, as with vitamins, nutritional supplements, nutritional supplements, senile diseases such as dementia, usefulness for allergic diseases, and increased exercise capacity have also been reported, and their safety It can be said that it is a useful means of nutrition because it is high.

  Further, α-lipoic acid (thioctic acid, 1,2-dithiolane-3-pentanoic acid) exists as a natural product in plant or animal cells at a low concentration in the form of its R-enantiomer. Α-Lipoic acid, first discovered as a growth factor, acts as a coenzyme for the oxidative decarboxylase of α-ketocarboxylic acids, such as pyruvate, in physiologically hydrophilic and lipophilic media. In recent years, it is a substance that has attracted attention for its strong antioxidative effect.

  In recent years, with increasing health consciousness, development of functional foods with various effects using various natural materials has been promoted. On the other hand, sports are becoming increasingly popular for the purpose of actively maintaining health and improving physical fitness. Against this backdrop, research on the way of sports life and the influence of dietary habits, sports nutrition studies on people aiming for health is progressing, and interest is also increasing.

  However, at present, none of the various functional foods has the purpose of enhancing anti-fatigue and / or endurance and supporting the effect. For example, there are known fatigue improving agents (Patent Document 1) containing coenzyme Q10 and carnitine, and nutritional supplements (Patent Document 2) containing coenzyme Q10, cyanocobalamin, folic acid and pyridoxine hydrochloride. Does not clearly describe the effects of improving fatigue and endurance. From such a background, development of a novel anti-fatigue agent and / or endurance enhancer, functional food, or cosmetic has been strongly desired.

JP-A-7-330584 Japanese Patent Application No. 2003-169633

  An object of the present invention is to provide a pharmaceutical, a functional food, and a cosmetic that are superior to conventionally known pharmaceuticals, functional foods, and cosmetics that have anti-fatigue and / or endurance enhancing effects. It is in.

  As a result of intensive studies to solve the above-mentioned problems, the present inventors have found that when coenzyme Q10 and α-lipoic acid are simultaneously ingested, the effect is enhanced more than ingestion alone. The present invention has been completed by finding that a pharmaceutical, a functional food or a cosmetic containing sucrose as an active ingredient has an anti-fatigue action or an endurance enhancing action.

That is, the present invention
(1) an anti-fatigue agent and / or endurance enhancer comprising coenzyme Q10 and α-lipoic acid as active ingredients,
(2) The anti-fatigue agent and / or endurance enhancer according to (1) above, which contains at least coenzyme Q10, α-lipoic acid, and a water-soluble substance,
(3) In order to ingest and / or apply coenzyme Q10 and α-lipoic acid simultaneously, an anti-fatigue agent and / or endurance enhancer containing coenzyme Q10 as an active ingredient, and α-lipoic acid as an active ingredient A kit containing an anti-fatigue agent and / or an endurance enhancer,
(4) A functional food having anti-fatigue action and / or endurance enhancing action containing coenzyme Q10 and α-lipoic acid as active ingredients,
(5) Use of coenzyme Q10 and α-lipoic acid for preparing a composition having an anti-fatigue action and / or endurance enhancing action,
(7) An anti-fatigue action and / or endurance enhancement method characterized by ingesting and / or applying a composition containing coenzyme Q10 and α-lipoic acid as active ingredients,
(8) Cosmetics containing coenzyme Q10 and α-lipoic acid as active ingredients,
About.

  According to the present invention, an anti-fatigue agent and / or endurance enhancer containing coenzyme Q10 and α-lipoic acid as active ingredients, or an anti-fatigue action and / or endurance containing coenzyme Q10 and α-lipoic acid as active ingredients Use of coenzyme Q10 and α-lipoic acid for the preparation of functional foods, cosmetics, and compositions having anti-fatigue and / or endurance enhancing activity, and coenzyme Q10 and α-lipo An anti-fatigue action and / or endurance enhancement method characterized by ingesting and / or applying a composition containing an acid as an active ingredient can be provided.

  The present invention will be specifically described below.

  Coenzyme Q10 used in the present invention is not limited in its origin and production method as long as it is coenzyme Q10 that can be taken or edible as a medicine or food, but a commercially available product is preferred. Further, it may be a compound that converts to coenzyme Q10 in vivo.

  The content of coenzyme Q10 in medicine and food is not limited as long as the anti-fatigue action and / or endurance enhancing action is obtained, but the daily intake of coenzyme Q10 is 1 to 2000 mg. The amount is preferably 10 to 500 mg, more preferably 30 to 300 mg.

  Coenzyme Q10 is a lipophilic solid having a low melting point, and is known to have low absorbability in oral administration due to poor solubility in water. For this reason, it is preferable to improve stability of properties such as dispersion stability of coenzyme Q10 in pharmaceutical preparations and foods, and prevention of crystal precipitation, and bioabsorbability. In the present invention, a stabilized product of coenzyme Q10 may be used. For example, by blending coenzyme Q10 with animal protein such as chicken egg protein, milk protein, meat protein, vegetable protein such as soybean protein or soybean peptide, or hydrolyzate thereof, or further blending with carbohydrates Coenzyme Q10 may be used after stabilization and further improvement of bioabsorbability.

  When coenzyme Q10 is used as an emulsified composition, for example, coenzyme Q10 is dissolved in a sucrose fatty acid ester such as sucrose acetate isobutyrate, a medium chain fatty acid ester or the like as an oil phase component, and a polyhydric alcohol and an emulsifier are used. Water-soluble such as gum arabic, agar, water-soluble corn fiber, starch, gelatin, xanthan gum, casein, dextrin, carmelol sodium, polyvinyl pyrrolidone in the presence or absence of additives such as organic acids The coenzyme Q10 may be used after improving the stability and bioabsorbability of the properties by dispersing and emulsifying coenzyme Q10 in the substance. The α-lipoic acid used in the present invention is not limited in any way as long as it is α-lipoic acid that can be taken or edible as a medicine or food, but a commercially available one is preferable. The content of α-lipoic acid in pharmaceuticals and foods is not limited as long as it provides an anti-fatigue effect and / or endurance enhancing effect, but the daily intake of α-lipoic acid Is such that the amount becomes 1 to 2000 mg, preferably 10 to 1000 mg, more preferably 50 to 500 mg.

  The kit for simultaneously ingesting and / or applying Coenzyme Q10 and α-lipoic acid of the present invention includes an anti-fatigue agent and / or endurance enhancer containing coenzyme Q10 as an active ingredient, and α-lipoic acid. Anti-fatigue agent and / or endurance enhancer containing as active ingredient is included in kit or anti-fatigue agent and / or endurance enhancement containing coenzyme Q10 and α-lipoic acid as active ingredients The kit is not limited as long as it is a kit composed of an agent.

The composition containing coenzyme Q10 and α-lipoic acid as an active ingredient of the present invention has an anti-fatigue action obtained by ingestion and / or application, coenzyme Q10 alone, or α-lipoic acid alone and / or application. What is necessary is just a composition which shows a synergistic anti-fatigue effect and / or endurance enhancement effect compared with the endurance enhancement effect. That is, it is a composition for improving fatigue and / or endurance, which contains coenzyme Q10 and α-lipoic acid and has an effect of improving fatigue and / or endurance. The content of coenzyme Q10 and α-lipoic acid in pharmaceuticals and foods is not limited as long as the anti-fatigue effect and / or endurance enhancing effect is obtained, but the daily coenzyme Q10 / α -An amount such that the intake amount of lipoic acid is 1 to 2000/1 to 2000 mg, preferably 10 to 500/10 to 200 mg, and more preferably 30 to 300/50 to 500 mg is good.
An anti-fatigue action and / or endurance enhancing action characterized by ingesting and / or applying the composition is also within the scope of the present invention. Ingestion includes both oral and parenteral, and parenteral includes injection, infusion, and nasal administration.

  The use of coenzyme Q10 and α-lipoic acid of the present invention is not particularly limited as long as it is used for preparing the anti-fatigue action or endurance enhancing composition of the present invention. Examples of compositions effective for anti-fatigue action and / or endurance enhancement include pharmaceuticals for anti-fatigue action and / or endurance enhancement, functional foods having anti-fatigue action and / or endurance enhancement, cosmetics, etc. Is mentioned.

  The medicament containing coenzyme Q10 and α-lipoic acid of the present invention is not limited in any way as long as an anti-fatigue action and / or endurance enhancing effect is obtained. The pharmaceutical dosage forms include scattered, granule, soft capsule, hard capsule, tablet, chewable tablet, quick-disintegrating tablet, syrup, solution, suspension, suppository, ointment, cream, gel, sticky, inhalation Agents, injections and the like. These preparations are prepared according to conventional methods. However, since Coenzyme Q10 is hardly soluble in water, it can be dissolved in a non-hydrophilic organic solvent such as vegetable oil or animal oil, or an emulsifier, dispersed or surfactant It is used after being dispersed and emulsified in an aqueous solution using an agent or the like. Further, in order to increase the absorbability of coenzyme Q10, the average particle system can be finely pulverized to about 1 micron.

  Additives that can be used for formulation include animal oils such as soybean oil, safflower oil, olive oil, germ oil, sunflower oil, beef tallow, sardine oil, polyethylene glycol, propylene glycol, glycerin, sorbitol, etc. Surfactant such as polyhydric alcohol, sorbitan fatty acid ester, sucrose fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, purified water, lactose, starch, crystalline cellulose, D-mannitol, lecithin, gum arabic, sorbitol solution, sugar Examples thereof include excipients such as liquid, sweeteners, colorants, pH adjusters, and fragrances. The liquid preparation may be dissolved or suspended in water or other appropriate medium when taken. Tablets and granules may be coated by a known method.

  The functional food containing coenzyme Q10 and α-lipoic acid of the present invention is not limited in any way as long as an anti-fatigue action and / or endurance enhancing effect can be obtained, but coenzyme Q10 and α- It is a food containing lipoic acid, characterized by having an effect of improving fatigue and / or endurance, and having a label indicating that it is used for improving fatigue and / or endurance It is preferable. Examples of the food include coenzyme Q10 and α-lipoic acid-containing supplements (dispersed, granules, soft capsules, hard capsules, tablets, chewable tablets, quick-disintegrating tablets, syrups, liquids, etc.), coenzyme Q10 and α-lipoic acid-containing beverages ( Tea, carbonated drink, sports drink, etc.), coenzyme Q10 and α-lipoic acid-containing confectionery (gummy, jelly, gum, chocolate, cookies, candy, etc.), coenzyme Q10 and α-lipoic acid-containing oil, coenzyme Q10 and α-lipo Acid-containing oil and fat foods (mayonnaise, dressing, butter, cream, margarine, etc.), coenzyme Q10 and α-lipoic acid-containing ketchup, coenzyme Q10 and α-lipoic acid-containing sauce, coenzyme Q10 and α-lipoic acid-containing liquid food, coenzyme Q10 And α-lipoic acid-containing dairy products (cow , Yogurt, cheese, etc.), coenzyme Q10 and α-lipoic acid-containing breads, coenzyme Q10 and α-lipoic acid-containing noodles (noodles, soba, ramen, pasta, yakisoba, kishimen, somen, hiyamugi, rice noodles, etc.) Is mentioned.

  The functional food containing coenzyme Q10 and α-lipoic acid used in the present invention includes various nutrients and various vitamins as necessary (vitamin A, vitamin B1, vitamin B2, vitamin B6, vitamin C, vitamin E, etc. ), Minerals, dietary fiber, polyunsaturated fatty acids, other nutrients (β-carotene, lycopene, astaxanthin and other carotenoids, carnitine, sesamin), dispersing agents, stabilizers such as emulsifiers, sweeteners, taste ingredients (Citric acid, malic acid, etc.), flavor, royal jelly, propolis, agarics and the like can be blended. Moreover, you may mix | blend herbs, such as peppermint, bergamot, camomile meal, and lavender. Examples of the cosmetic of the present invention include creams, emulsions, lotions, microemulsion essences, bathing agents, and the like, and fragrances and the like may be mixed.

The present invention will be described based on Examples, Formulation Examples, Food Production Examples, Cosmetic Production Examples, and Test Examples, but the present invention is not limited to the following.
[Example 1]
Coenzyme Q10 (120 g) and α-lipoic acid (120 g) were mixed to obtain a composition.
[Formulation Example 1]
<Tablets>
Coenzyme Q10 120g
α-Lipoic acid 120g
Crystalline cellulose 330g
Carmellose-calcium 15g
Hydroxypropylcellulose 10g
60 ml of purified water
After blending and drying the above composition by a usual method, 10 g of magnesium stearate was added and tableted to obtain 100 mg tablets each containing 20 mg of coenzyme Q10 and α-lipoic acid. .
[Formulation Example 2]
<Soft capsule>
200 g of coenzyme Q10 and 200 g of α-lipoic acid were added to 400 g of olive oil, dissolved at about 60 ° C., stirred uniformly, and then cooled to obtain a coenzyme Q10-containing material. Gelatin 70% and glycerin 30% were mixed and swollen to prepare a dissolved gelatin sheet. This gelatin sheet was filled with a coenzyme Q10-containing material as an internal solution so as to have an internal volume of 300 mg per capsule and dried to obtain soft capsules containing 100 mg of coenzyme Q10 and α-lipoic acid per capsule.
[Kit example]
In the same manner as the tablet described in Formulation Example 1 or the soft capsule described in Formulation Example 2 except that it contains coenzyme Q10 alone or α-lipoic acid alone instead of containing coenzyme Q10 and α-lipoic acid (tablet (Or soft capsule). 1-5 each of the coenzyme Q10-containing tablets (or soft capsules) and the α-lipoic acid-only tablets (or soft capsules) were packed to prepare a coenzyme Q10 and α-lipoic acid bundling kit.
[Food Production Example 1]
<Beverage>
500 g of coenzyme Q10 and 2500 g of α-lipoic acid were dissolved in 10 g of glycerin fatty acid ester heated to 60 ° C. and 30 g of glycerin. Water was added to the mixed solution to make 100 ml, and the mixture was emulsified using an emulsifier (pressure homogenizer) to obtain an emulsified composition. Water was added to 1 g of this emulsified composition to make 100 ml, and stirred to obtain a beverage containing coenzyme Q10 (50 mg / 100 ml) and α-lipoic acid (250 mg / 100 ml).
[Food Production Example 2]
<Bread>
1 g of coenzyme Q10, 1 g of α-lipoic acid, 15 g of sugar, 2 g of sodium chloride, and 5 g of fat milk powder were dissolved in 70 g of hot water, and 2 eggs were added and mixed well. This was added to a mixture of 130 g of wheat flour and 2 g of dry yeast, kneaded by hand, then kneaded with about 30 g of butter to make 30 roll bread dough. Next, after fermenting, a beaten egg was applied to the surface and baked in an oven at 180 ° C. for 15 minutes to obtain a roll.
[Food Production Example 3]
<Udon>
To 400 g of wheat flour, 2 g of coenzyme Q10, 2 g of α-lipoic acid and 20 g of sodium chloride were added to 200 g of water and kneaded well. Thereafter, the dough was stretched and cut into widths of about 6 mm to produce udon.
[Cosmetics Production Example 1]
<Cream>
Coenzyme Q10, α-lipoic acid, stearyl alcohol, propylene glycol, sorbitol, paraben, vitamin E, fragrance, and purified water were blended in appropriate amounts according to a conventional method to obtain a cream.
[Test Example 1] Anti-fatigue effect and endurance enhancing effect test of coenzyme Q10 and α-lipoic acid-containing foods Using 5-week-old male ddY mice, after 6 days of preliminary breeding, divided into 4 groups of 10 per group It was. The group composition is a control group (water administration group), Comparative Example 1 (Coenzyme Q10 10 mg / kg single beverage containing group), Comparative Example 2 (α-lipoic acid 50 mg / kg single beverage containing group), and Test Example (Coenzyme Q10 10 mg / kg and α-lipoic acid 50 mg / kg-containing beverage administration group; coenzyme Q10 and α-lipoic acid-containing beverage described in Food Production Example 1 were used), and oral gavage was performed 5 days a week . From the first week after the administration, a weight of 9.5% of the body weight was added to the mouse and forced swimming was performed. The time until the head was completely submerged in water for 7 seconds was measured. The results are shown in Table 1. Mean values (seconds) ± standard error are shown and tested by Student's t-test. (Test example at 2 weeks vs control group: p <0.0006, Test example at 2 weeks vs Comparative example 1: p <0.049, Test example at 2 weeks vs Comparative example 2: p <0.0009 )

  As shown in Table 1, in the coenzyme Q10 and α-lipoic acid-containing food administration group, a significant prolongation effect of swimming time was recognized as compared with the control group and CoQ10 or α-lipoic acid alone administration group.

The anti-fatigue agent or endurance enhancer of the present invention or the functional food having an anti-fatigue effect or endurance enhancement effect can be suitably used in the field of medicine and / or food.

Claims (8)

  An anti-fatigue agent and / or endurance enhancer comprising coenzyme Q10 and α-lipoic acid as active ingredients.   2. The anti-fatigue agent and / or endurance enhancer according to claim 1, comprising at least coenzyme Q10, α-lipoic acid, and a water-soluble substance.   In order to simultaneously ingest and / or apply coenzyme Q10 and α-lipoic acid, an anti-fatigue agent and / or endurance enhancer containing coenzyme Q10 as an active ingredient, and an anti-fatigue agent containing α-lipoic acid as an active ingredient A kit containing a fatigue agent and / or endurance enhancer.   A functional food having anti-fatigue action and / or endurance enhancing action containing coenzyme Q10 and α-lipoic acid as active ingredients.   Use of coenzyme Q10 and α-lipoic acid for preparing a composition having an anti-fatigue action and / or endurance enhancing action.   A method for enhancing anti-fatigue action and / or endurance, comprising simultaneously ingesting and / or applying coenzyme Q10 and α-lipoic acid.   A method for enhancing anti-fatigue action and / or endurance, comprising ingesting and / or applying a composition containing coenzyme Q10 and α-lipoic acid as active ingredients.   Cosmetics containing coenzyme Q10 and α-lipoic acid as active ingredients.