JP4437319B2 - Preventing lactic acid production during exercise - Google Patents

Description

The present invention relates to a preventive agent for lactic acid production during exercise. In the present invention, “exercise” exercise means an activity in which metabolic energy production is performed under anaerobic conditions such as overloaded work and intense sports.

In order for a living organism to maintain life activity, it needs biogenic energy, which is produced in the following process. In other words, ingested food is digested, absorbed, transferred to cells, and accumulated glucose (glucose) and glycogen stored mainly in the liver and muscles through glucose 6-phosphate by glycolytic enzyme reaction, pyrubin ATP (adenosine triphosphate), NADH and NAD (nicotine) produced in a series of metabolic processes that are converted into acetyl-CoA in the mitochondria of cells and further converted into citric acid, oxaloacetate, etc. in the TCA cycle Amide adenine dinucleotide reduced and oxidized forms) are used as direct energy sources. In addition, fat undergoes a β-oxidation reaction of fatty acid, passes through acetyl CoA, is similarly metabolized in the TCA cycle, and participates in bioenergy production.

In normal mental and physical activities, aerobic glycolysis is prioritized due to the presence of sufficient oxygen, and glucose and glycogen are mainly used as bioenergy sources, and the pyruvic acid produced is sequentially released in the TCA cycle. It is metabolized and does not produce lactic acid. On the other hand, in an intense activity that requires a large amount of bioenergy (overloading work, sports exercise, etc.), anaerobic glycolysis occurs in an oxygen-deficient state, and the metabolic energy production reaction in the TCA circuit occurs. It becomes rate-determining with respect to the pyruvic acid production reaction in the previous stage, so that an excess of pyruvic acid is generated, and a part of this is converted into lactic acid by lactate dehydrogenase. Will be accumulated.

Lactic acid has traditionally been considered to be a muscle fatigue substance together with ammonia production during exercise, scorching glucose, and the like, and has been considered to be a major factor in muscle pain caused by fatigue. However, lactic acid is converted to acetyl-CoA and converted to TCA. Although it may be interpreted as a substance that relieves fatigue rather than being metabolized into the circuit (Non-patent Document 1), in general, lactic acid accumulates in the muscle as fatigue occurs. There is a theory that lactic acid is interpreted as one of fatigue-related substances because it increases the acidity of muscle tissue, reduces the activity of enzymes, and suppresses the production of bioenergy necessary for muscle exercise. Influential.

In order to alleviate fatigue, daily intake of carbohydrates and B vitamins, which are bioenergy sources in the diet, is recommended to compensate for the lack of energy, and nutritional balance can be achieved as an easy way to relieve fatigue. Taking a fresh meal, taking a bath and massage to improve blood circulation, and taking sufficient rest. In addition, from the viewpoint of fatigue prevention and recovery, physical strength enhancement, a specific amino acid mixture (Patent Document 1), beef-degrading peptide (Patent Document 2), a combination of mineral yeast, dolomite, heme iron and seaweed (Patent Document 3), Ingestion of a reishi component (Patent Document 4), coenzyme Q10, a combination of carnitine and an organic acid (Patent Document 5), milk whey protein (Patent Document 6) and the like has been proposed. However, when these are taken orally, there are some which are difficult to digest and absorb, and there are few that are sufficiently satisfactory in practical use.

By the way, the following things are known about the thioctic acid mentioned later. Thioctic acid is α-lipoic acid, 1,2-diethylene-3-pentanoic acid, 1,2-diethylene-3-valeric acid, 1,2-dithiolane-6-pentanoic acid or 1,2-dithiacyclopentane. It is also called -3-valeric acid. Pale yellow to yellow crystal or crystalline powder with specific odor, melting point: racemic: 60-61 ° C, R: 46-48 ° C, S: 45-48 ° C, slightly in water Dissolves and dissolves in organic solvents such as ethanol and acetone and dilute alkaline water. Thioctic acid is synthesized in vivo by plants, animals / humans, and microorganisms, and is bioavailable as one of various coenzymes such as pyruvate dehydrogenase complex and 2-oxoglutarate dehydrogenase complex, and catalyzes acyl transfer reaction. It is known to do.

In recent years, research on the function of thioctic acid and its reduced form dihydrothioctic acid (6,8-dimercapto-octanoic acid) has progressed, and these have attracted attention as having strong antioxidant power, superoxide radicals, It reacts easily with reactive oxygen species such as hydroxy radical, peroxy radical, singlet oxygen, etc., easily reacting to lose the action of the active oxygen species, reducing damage to living tissues, and interacting with vitamin C and glutathione. It is said that it has the effect of protecting cell membranes by action and regenerating vitamin E (Non-patent Document 1). The pharmacological action of thioctic acid has been reported to be effective for pathological models of oxidative stress such as tissue damage during ischemic reperfusion, diabetes, cataracts, neurodegeneration, radiation damage, inflammatory diseases, etc. ( Non-patent document 2). However, there are no reports on the action of thioctic acid and its derivatives to sustain a long operation requiring a large amount of bioenergy, to prevent fatigue, or to recover early.

In general, the technology of coating powders and particles as a core substance and surrounding the surface with a hydrophobic substance such as a polymer substance or lipid has been known, and the coating process stabilizes the taste and aroma of the core substance. It is proposed to prevent the leakage of the component when the core substance is a water-soluble component, or to prevent moisture absorption, to prevent powder absorption, or when the core substance is a water-soluble component (Patent Document 7, 8 and 9). However, the protective action of the core material by such coating treatment aims at improving physical properties such as maintaining the quality of flavor components, moisture resistance, and preventing leakage of water-soluble components .

JP-A-8-198748 JP-A-10-113147 Japanese Patent Laid-Open No. 2003-198 JP-A-5-124974 JP-A-2005-97161 Japanese Patent Laid-Open No. 2005-289861 JP 63-226250 A JP-A-9-70285 Japanese Patent No. 3512238 Thomas H.M. Pedersen et al., “Intracellular Acidity enhancement the Working Mus.” (USA), 2004, Science, 305, August 20, pp. 1144-147. Indani Maitra et al., “Α-lipoic acid presents basicion sulfoximine-induced catalyst formation in newborn rats.” (Netherlands), p. 8, M

In view of the current situation, the present inventors have made it an object to provide a material and method that can prevent the production of lactic acid during exercise .

In order to solve the above-mentioned problems, the present inventors have conducted extensive studies on the relationship between various raw materials and bioenergy production ability, sustainability of activity, prevention and recovery of fatigue, nutritional supplementation, etc. The present inventors have found that thioctic acids have extremely remarkable effects and that they can be effectively used in the fields of foods and drinks, feeds, cosmetics, pharmaceuticals, etc., and have completed the present invention.

That is, according to the present invention, prevention of lactic acid production during exercise, which is a composition for preventing lactic acid production during exercise , comprising thioctic acids and creatine or a derivative thereof as active ingredients An agent is provided.

In the composition, the thioctic acids are selected from the group consisting of thioctic acid, dihydrothioctic acid which is a reduced form thereof, optical isomers thereof, salts, esters and amides of the respective substances, and cyclodextrin inclusion products thereof. It is desirable that they are one or more types.

Further, the thioctic acid is selected from the group consisting of thioctic acid, dihydrothioctic acid which is a reduced form thereof, optical isomers thereof, salts, esters and amides of the respective substances, and cyclodextrin inclusions thereof. It is more desirable to coat the outer surface of seeds or two or more crystals, powders and / or particles with lipids. Further, the thioctic acid is one kind selected from the group consisting of thioctic acid, dihydrothioctic acid which is a reduced form thereof, optical isomers thereof, salts, esters and amides of the respective substances, and cyclodextrin inclusion products thereof. Alternatively, it is more preferable that the outer surface of two or more kinds of crystals, powders and / or particles is coated with lipids and the outer surface is further coated with a hydrophilic substance. The thioctic acids are preferably racemic in optical isomers.

According to the present invention, the thioctic acid, caffeine, creatine and derivatives thereof, glucosamine, chondroitin, chondroitin sulfate, collagen hydrolyzate, choline, choline salt, phosphatidylcholine, serine, phosphatidylserine, methylsulfonylmethane, whey Protein, L-carnitine and its salt, D-ribose, amino acid, branched chain amino acid, taurine, coenzyme Q10, vitamin B1, vitamin B2, nicotinic acid, pantothenic acid, lactoferrin, conjugated linoleic acid, citric acid, malic acid and mineral yeast A prophylactic agent for lactic acid production during exercise is provided which is used in combination with at least one selected from the group consisting of :

In the above combination composition, the raw material component used in combination is one or two selected from the group consisting of creatine and / or a derivative thereof, L-carnitine and / or a salt thereof, coenzyme Q10, vitamin B1, vitamin B2, and phosphatidylserine. The above is more desirable, and creatine and / or its derivatives are most desirable. As the creatine derivative, it is preferable to use one or more selected from the group consisting of creatine salt, creatine monohydrate, creatine citrate, creatine pyruvate and phosphocreatine.

According to the present invention, there is further provided a food or drink for preventing lactic acid production during exercise , characterized by comprising any one of the above compositions. Furthermore, there is provided a method for preventing lactic acid production during exercise , characterized by orally ingesting any one of the above-described compositions or food and drink before exercise .

The composition of the present invention has excellent quality stability, and when taken orally, the active ingredient is efficiently absorbed without being digested and decomposed in the body, and a large amount of bioenergy is required continuously. It has a remarkable effect on the enhancement of endurance, and is extremely effective in preventing fatigue and / or early recovery, in particular, preventing fatigue, and also beneficial for nutritional tonic. For this reason, the composition of the present invention can be effectively used as it is in the above-mentioned composition or in a form blended with various conventional products in the fields of foods and drinks, feeds, pharmaceuticals and the like.

The present invention is described in detail below. An embodiment of the composition according to the present invention is for preventing lactic acid production during exercise , and is characterized by containing thioctic acids and creatine or a derivative thereof as active ingredients.

Here, the origin and type of thioctic acids are not particularly limited, and natural product extracts of organs such as livers of cattle and pigs, and chemical synthetic products starting from ethylene and adipic acid esters are known. It may be collected and manufactured by the method described above. In addition, since thioctic acid has an asymmetric carbon, optically enantiomers ((R) -enantiomer and (S) -enantiomer) exist, but any one of these thioctic acids according to the present invention can be used in any proportion. Or a racemic mixture or a racemate. In the industrial production level, it is easy to use a commercially available racemate that is inexpensive and easily available, and it is desirable to use the racemate because the desired effect of the present invention is more strongly expressed.

As the thioctic acid used in the composition according to the present invention, various derivatives in addition to the thioctic acid can be appropriately used. Among them, a reduced form of thioctic acid, optical isomers thereof, more preferably racemates, salts, esters and amides of the respective substances, and one or more selected from the group consisting of these cyclodextrin inclusions or Two or more types are desirable. Specific examples of the reduced form of thioctic acid include dihydrothioctic acid, dihydrolipoic acid, 6,8-dimercapto-octanoic acid and the like. Similarly, optical isomers include (R) -thioctic acid and (S) -thiocto (R), (S) -thioctic acid, (R) -dihydrothioctic acid, (S) -dihydrothioctic acid, (R), (S) -dihydrothioctic acid, etc. (R) , (S) -thioctic acid, (R), (S) -dihydrothioctic acid, and the like, (R) -thioctic acid, (S) -thioctic acid, (R), (S) -thioctic acid, ( Potassium salts such as R) -dihydrothioctic acid, (S) -dihydrothioctic acid, (R), (S) -dihydrothioctic acid, sodium salts, calcium salts, magnesium salts, etc., and (R) -thioctic acid as an ester , (S) Thioctic acid, (R), (S) -thioctic acid, (R) -dihydrothioctic acid, (S) -dihydrothioctic acid, (R), (S) -dihydrothioctic acid and the like and polyhydric alcohols (ethylene glycol, Partial ester or complete ester or glycerides (monoglyceride, diglyceride, triglyceride) with propylene glycol, butanediol, neopentyl glycol, glycerin, erythritol, polyglycerin or the like, or higher alcohols having 10 to 22 carbon atoms Monoesters with (decanol, lauryl alcohol, myristyl alcohol, cetanol, stearyl alcohol, isostearyl alcohol, behenyl alcohol, etc.), amides as (R) -thioctic acid, (S) -thioctic acid, (R) (S) - thioctic acid, (R) - Dihydrothiazol octoate, (S) - Dihydrothiazol octoate, (R), (S) - can be exemplified amides such dihydrothiazoles octoate. Examples of cyclodextrin inclusions include inclusions of the thioctic acids with α-, β-, γ- and / or δ-cyclodextrin. In the present invention, α- or γ-cyclo Dextrin inclusions are preferred. In addition, this invention is not limited by these illustrations.

Thioctic acids that can be used in the composition according to the present invention include those obtained by coating the outer surface of one or more crystals, powders and / or particles of the thioctic acids with lipids. Is more desirable from the viewpoints of suppressing thermal alteration (decomposition, polymerization, discoloration, etc.), moisture absorption or oxidative modification of thioctic acids, improving flavor and taste, and slow release of active ingredients after ingestion. Is.

The lipids that coat the outer surface of the thioctic acid crystals, powder, and / or particles may be acceptable as long as they are acceptable in the industrial field in which the composition of the present invention is used. Fats and oils, fatty acid glycerides, fatty acids, fatty acid esters, fatty acid amides, higher alcohols, waxes, sterols, glycolipids, phospholipids and the like can be used alone or in combination. Of these, lipids having a melting point of about 30 ° C. or higher are preferable in consideration of coating workability and physical properties of the coating (stability, solidification, fluidity, meltability, solubility, etc.). More preferred forms are lipids having a melting point of about 40 ° C. to about 70 ° C., and most preferred forms are lipids having a melting point of about 40 ° C. to about 60 ° C. When the melting point is less than about 30 ° C., the coating may not be able to maintain a solid state during use, and may form a lump or impair flowability. On the other hand, when the temperature exceeds about 70 ° C., the thioctic acids themselves may be deteriorated due to the influence of heat treatment and mechanical energy when producing the composition according to the present invention.

Specific examples of such lipids include soybean oil, rapeseed oil, corn oil, sunflower oil, cottonseed oil, wheat germ oil, rice oil, sesame oil, olive oil, safflower oil, palm oil, palm kernel oil, coconut oil, linseed oil , Vegetable oils such as peanut oil, animal fats such as beef tallow, lard, fish oil, processed oils and fats that have been subjected to one or more of such treatments as fractionation, transesterification, decolorization, deodorization, etc., partially or completely Various hydrogenated hydrogenated oils, saturated fatty acids having 2 to 22 carbon atoms (acetic acid, butyric acid, caproic acid, caprylic acid, capric acid, lauric acid, myristic acid, pentadecanoic acid, palmitic acid, stearic acid, 12-hydroxystearic acid , Isostearic acid, arachidic acid, behenic acid, etc.) or unsaturated fatty acids (palmitoleic acid, oleic acid, elaidic acid, linoleic acid, α-linolenic acid) , Γ-linolenic acid, ricinoleic acid, arachidonic acid, icosapentaenoic acid (EPA), erucic acid, docosahexaenoic acid (DHA), etc., salts of these arbitrary fatty acids (sodium salt, potassium salt, calcium salt, magnesium salt, etc.) Partial or complete with esters with monohydric alcohols (methanol, ethanol, propanol, butanol, etc.), polyhydric alcohols (monomers or polymers such as ethylene glycol, propylene glycol, butanediol, neopentyl glycol, glycerin, erythritol, etc.) Esters or glycerides (monoglyceride, diglyceride, triglyceride), higher alcohols having 10 to 22 carbon atoms (decanol, lauryl alcohol, myristyl alcohol, cetanol, stearyl alcohol, Sostearyl alcohol, behenyl alcohol, etc.), waxes (carnauba wax, rice wax (rice bran wax), candelilla wax and other plant-derived waxes, beeswax, whale wax, shellac wax and other animal-derived waxes, paraffin wax, microcrystalline Petroleum-derived waxes such as wax, waxes derived from minerals such as montan wax, ozokerite, polyethylene wax, synthetic waxes such as esters of the above fatty acids and higher alcohols, sterols (animal cholesterol, vegetable campesterol, Stigmasterol, sitosterol, and other fungal ergosterols and their derivatives), phospholipids (animal and plant-derived lecithin, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinos , Phosphatidylserine, phosphatidic acid, sphingomyelin, etc.), glycolipids (monoglucosyl diglyceride, monogalactosyl diglyceride, diglucosyl monoglyceride, digalactosyl monoglyceride, monoglucosyl diglyceride, digalactosyl diglyceride, sucrose fatty acid ester, etc.) be able to. In addition, this invention is not limited at all by these illustrations.

In the present invention, any one or a mixture of two or more of the above-mentioned various lipids can be used. Suitable types of lipids include the above edible oils or industrial fats, fatty acid glycerides, fatty acid esters and Waxes, more preferably edible fats and oils and fatty acid glycerides, and these and one or more selected from fatty acids, higher alcohols, sterols, glycolipids or phospholipids The combination is a more desirable embodiment from the viewpoint of adjusting the melting point of the coated lipid, reinforcing the coating film, and the like.

A known method can be used to coat the outer surface of the thioctic acid crystals, powder and / or particles with lipids. That is, ball mill, flash blender (powder granule mixer), V-type mixer, high-speed mixer, high-speed paddle mixer, heat-melt mixer, ultrasonic super-humidified liquid-type mixer, tumbler mixer, pressure extruder, etc. The thioctic acid crystals, powder and / or particles and the heated and melted lipids are uniformly mixed, cooled and solidified, and then pulverized. A method of coating by spraying or dripping the lipids which have been formed, and stirring and mixing the thioctic acids of the above-mentioned form and particulate lipids at high speed, and bringing them into contact or colliding with each other, thereby producing crystals, powders and / or thioctic acids. Alternatively, a method in which particulate lipids are uniformly attached to the entire surface of the particle and coated is possible. In the present invention, among these, thioctic acid crystals, powders and / or particles and particulate lipids having a specific melting point or higher are mixed with high-speed stirring, and both are brought into contact with or collided with each other to obtain the thioctic acid of the above form. A method of uniformly coating particulate lipids on the entire surface of acids is desirable.

In the above-described coating treatment, the ratio of thioctic acid crystals, powders and / or particles to lipids, thioctic acid crystals, powder and particle shapes and sizes, lipid types and melting points, coating film thickness and Although it is difficult to define uniformly depending on factors such as properties, about 0.05 parts by weight to about 10 parts by weight, preferably about 0 parts by weight of lipids are generally added to 1 part by weight of crystals, powders and / or particles of thioctic acids. .1 part by weight to about 5 parts by weight. If the lipids are less than about 0.05 parts by weight, the coating state is not sufficient and it is difficult to achieve the desired effect. Conversely, if the lipids exceed about 10 parts by weight, the thioctic acid content in the coating is low, In the scene where it is used, the blending rate and the like are limited, and the practical value may be impaired.

The above-described coating of thioctic acids with lipids is more desirable in that the outer surface is further coated with a hydrophilic substance, including the case where it is applied to an aqueous composition such as a beverage. . Here, the hydrophilic substance means a substance that further coats the outer surface of the coating with lipids and has a coating film-forming ability having an affinity with an aqueous substance. Specific examples include polysaccharides (xanthan gum, guar gum, Tamarind seed gum, psyllium seed gum), starch and modified starch, yeast cell wall components, glucan, mannan, shellac, sodium alginate, gelatin, carrageenan, pullulan, carboxymethylcellulose, soybean protein, whey protein, zein, etc. Can do. More preferably, it is one or more selected from the group consisting of polysaccharides, starch, yeast cell wall components, shellac, gelatin, soybean protein, zein and mannan, and more preferably yeast cell wall components, shellac and gelatin. is there.

In order to coat such a hydrophilic substance, a method according to the above-described method for coating lipids may be employed. That is, the hydrophilic substance is appropriately dissolved in water, ethanol, or other solvent to form a liquid, and this is attached to the outer surface of thioctic acid previously coated with lipids and dried to coat the hydrophilic substance. A film can be formed. The coating thus obtained becomes a double-coated structure having a hydrophilic substance as the outermost layer. When this is used for foods, drinks, feeds, cosmetics, pharmaceuticals, etc., the affinity with aqueous raw materials and ingredients is increased, It becomes easy to prepare a homogeneous composition of thioctic acids with low water solubility.

In the above-described coating of thioctic acids with lipids and the double coating in which the coating is further coated with a hydrophilic substance, these include Garcinia camphor peel, red pepper rhizome, guava leaf and extracts thereof (water And / or one or two selected from the group consisting of an extract with a hydrophilic organic solvent (e.g., a lower monohydric alcohol such as ethanol, acetone, its fraction, a solvent fraction or a purified product), and carnitine. More preferably, the presence of red pepper rhizome extract and / or carnitine, and most preferably carnitine, allows further suppression of thermal and / or oxidative denaturation and degradation of thioctic acids and contains thioctic acids with excellent stability. Such a thioctic acid is more desirable since a coating is obtained.

In order to allow these combined raw materials to coexist in the aforementioned thioctic acid-containing coating, (i) the combined raw material is mixed with a coating in which lipids are coated on thioctic acid crystals, powder and / or particles, (ii) ) A lipid is coated on a mixture of the thioctic acid crystals, powders and / or particles and the combination raw material. (Iii) A part of the combination raw material is dispersed in the thioctic acid crystals, powder and / or particles. Or (iv) a solution obtained by coating the lipids on the thioctic acid crystals, powder and / or particles, and a solution, dispersion or emulsification containing the combined raw material and the hydrophilic substance. Any of attaching and drying and coating the liquid is possible, and a combination of these embodiments may be used. In the present invention, the aspects (i) and (iv) have the desired effects of the present invention, the production is simple, and the handling workability of the coating is good, but the aspects (ii) and (iii) are desirable. It is easy to express the effect more powerfully.

In such an embodiment, the mixing ratio of the coating material obtained by coating the crystals, powders and / or particles of thioctic acid with lipids or lipids and a hydrophilic substance and the coexisting raw material is the coexistence with respect to 1 part by weight of the coating material. The raw material is about 0.01 parts by weight to about 10 parts by weight, more preferably about 0.1 parts by weight to about 1 part by weight. When the amount is less than about 0.01 part by weight, the desired effect cannot be improved by mixing the coexisting raw materials. When the amount exceeds about 10 parts by weight, the content of thioctic acid in the coating and further in the composition using the same As a result, the thioctic acid content in various products containing the thioctic acid-containing composition is limited, and the desired effect of thioctic acid itself cannot be expected in the product stage.

In the embodiment of the composition according to the present invention, the aforementioned thioctic acids, that is, thioctic acid, dihydrothioctic acid, optical isomers thereof (preferably racemates), salts, esters and amides of the respective substances, and One or two or more selected from the group consisting of cyclodextrin inclusions, lipid coatings obtained by coating the outer surface of these crystals, powders and / or particles with lipids, or the lipid coatings Single or multiple double coatings whose outer surface is further coated with a hydrophilic substance, caffeine, creatine and its derivatives, glucosamine, chondroitin, chondroitin sulfate, collagen hydrolyzate, choline, choline salt, phosphatidylcholine, serine Phosphatidylserine, methylsulfonylmethane, whey protein, L-carnitine and its salts, D-ribo And at least one selected from the group consisting of amino acids, branched chain amino acids, taurine, coenzyme Q10, vitamin B1, vitamin B2, nicotinic acid, pantothenic acid, lactoferrin, conjugated linoleic acid, citric acid, malic acid and mineral yeast It is also possible to use a composition comprising a combination of

In the present invention, among the combined raw material components, one or two selected from the group consisting of creatine and / or a derivative thereof, L-carnitine and / or a salt thereof, coenzyme Q10, vitamin B1, vitamin B2, and phosphatidylserine. Species are more desirable and creatine and / or its derivatives are most desirable. Here, as the creatine derivative, it is preferable to use one or more selected from the group consisting of creatine salt, creatine monohydrate, creatine citrate, creatine pyruvate and phosphocreatine.

As described above, in the embodiment of the composition according to the present invention, the thioctic acid and at least one of the combined raw material components , particularly creatine and / or a derivative thereof , are included. Although it is difficult to uniformly define the ratio with the combination raw material component depending on the type and form, thioctic acids: combination raw material component = 90 to 10:10 to 90 (weight ratio) is preferable, and 70 to 50:30 to 50 Is more preferable.

The composition according to the present invention can be used as a variety of products in food and drink products, pharmaceutical products, cosmetics, feeds, and other industrial fields, or can be used in a form used as a part of blended raw materials of the various products. In particular, food and drink applications are suitable. Examples of these are described below, but the present invention is not limited thereby.

Specific examples of foods and drinks to which the composition according to the present invention can be applied include vegetable juices, fruit juice beverages, soft drinks, beverages such as tea, soups, jelly, pudding, yogurt, cake premix products, confectionery, Sprinkles, miso, soy sauce, sauce, dressing, mayonnaise, vegetable cream, miso, seasonings such as yakiniku sauce and noodle soup, noodles, udon, soba noodles, spaghetti, ham and sausage and other processed meat and fish meat products, hamburger, croquette , Sprinkles, boiled simmered, jam, milk, cream, butter, spread and cheese powders, solid or liquid dairy products, margarine, bread, cakes, cookies, chocolate, candy, gummi, gum and other general processed foods Or powder, granule, pill, tablet, soft capsule, hard capsule, paste or liquid Dietary supplements, and food for specified health use, functional foods, mention may be made of health food products, the concentrated liquid diet and dysphagia for food diet and the like.

In order to produce these foods and drinks, a known raw material and the composition according to the present invention may be used, or a part of the known raw material may be replaced with the composition of the present invention and produced by a known method. For example, the composition according to the present invention and, if necessary, glucose (dextrose), dextrin, lactose, starch or processed product thereof, excipients such as cellulose powder, vitamins, minerals, fats and oils of animals and plants and seafood, protein (Proteins derived from animals and plants and yeast, hydrolysates thereof, etc.), sugars, pigments, fragrances, antioxidants, other edible additives, mixed with edible materials such as powders and extracts containing various nutritional functional ingredients Capsules can be processed into powders, granules, pellets, tablets, etc., processed into general foods of the above examples by conventional methods, or mixed with a liquid such as gelatin, sodium alginate, carboxymethylcellulose, etc. It is preferable to use it as a dietary supplement or health food after being molded or processed into a beverage (drink) form. In particular, tablets, capsules and drinks are desirable.

The ratio in the case of blending the composition according to the present invention into a food or drink is the form of the food or drink, the type and content of thioctic acids and concomitant raw material components in the composition according to the present invention, the types and ingredients of other blended raw materials Although it is difficult to define uniformly because of the difference in the above, the thioctic acid content in the food and drink is about 0.01% to about 90% by weight, more preferably about 1% to about 50% by weight. Thioctic acids, lipid coatings and double coatings thereof, and further coexisting raw materials appropriately selected from Garcinia Cambodian peel, red pepper rhizome, guava leaves, extracts thereof and carnitine, creatine and / or derivatives thereof, Concomitant ingredients selected from L-carnitine and / or its salt, coenzyme Q10, vitamin B1, vitamin B2, phosphatidylserine, etc., and other food and beverage products Feed design the appropriate combination prescribe, the present invention according to a conventional method may be prepared food products of interest. In foods and beverages with a thioctic acid content of less than about 0.01% by weight, in order to expect the desired effect of thioctic acids, a large amount of the foods and beverages must be ingested. From the practical aspect of the considered food or drink, the most thioctic acid content in the food or drink according to the present invention is about 95% by weight. The food / beverage product according to the present invention is about 10 mg to about 1000 mg, preferably about 30 mg to about 500 mg, more preferably about 50 mg to about 200 mg per day, for example, in the case of humans. It can be taken into the body by a method such as tube administration.

The composition and the food and drink according to the present invention are desirably taken orally prior to various activities in accordance with the object of the present invention. According to this use aspect, the desired effect of the present invention, that is, the production of lactic acid during exercise is achieved. Effective in prevention . From this point of view, in the present invention, there is no restriction that the combination raw material components such as thioctic acids, thioctic acids, and creatine are included in the same composition, and they are prepared as a plurality of compositions or foods and drinks separately containing them. However, it is within the technical scope of the present invention to ingest such a composition or food or drink almost simultaneously.

Next, although an Example is given and this invention is demonstrated in detail, this invention is not limited by this. In each example, all the percentages, parts and ratios are based on weight.

(Production Example 1)
(1) Thioctic acid lipid coating Crystal powder of thioctic acid (manufactured by Degussa, Germany, trade name: ALIPURE (registered trademark), racemic body) heat-melted rapeseed oil (manufactured by Kawaken Fine Chemical Co., Ltd.) (Melting point: 67 ° C., flake shape) 200 g was added, mixed well and dispersed uniformly, and then cooled and solidified to room temperature. Next, the solidified product was pulverized with a high-speed mixer, and sieved with 100 mesh (Tyler mesh; the same applies hereinafter) to obtain a thioctic acid lipid coating (sample 1) having a particle size of 150 μm or less.

200 g of thioctic acid and 200 g of creatine monohydrate (manufactured by Degussa, Germany, trade name: CREAPURE (registered trademark)) and powdered rapeseed oil (manufactured by Kawaken Fine Chemical Co., Ltd., melting point: 60 ° C., average particle size) 200g) was charged into a fine particle coating granulator (Powrec Co., Ltd., model: MP-25SFP), stirred and mixed with a fan blade rotating at 1000 rpm for 30 minutes, and both raw materials were brought into contact and collided. Thus, a thioctic acid lipid coating (sample 2) having an average particle diameter of about 100 μm was obtained.

In the production example of the thioctic acid lipid coating (sample 2), 200 g of thioctic acid and 200 g of creatine were mixed into 150 g of thioctic acid and 50 g of guava leaf extract (manufactured by BN Co., Ltd., trade name: guava leaf extract powder-S). A treatment was performed in the same manner except that the thioctic acid lipid coating (Sample 3) was obtained.

In the production example of the thioctic acid lipid coating (sample 2), 200 g of thioctic acid was charged into a coating granulator and stirred and flowed, soybean oil: 40 parts, carnauba wax: 40 parts and soy sterol: 20 parts Lipid mixture 100 g, L-carnitine-L-tartrate (manufactured by Lonza Japan Co., Ltd.) and creatine (same as sample 2), and sucrose behenate (Mitsubishi Chemical Foods Co., Ltd., Ryoto) (Registered trademark) Sugar ester, HLB: 1-2) 20 g of a homogeneous liquid material heated, melted and mixed at 70 ° C. is sprayed from the spray nozzle to coat the thioctic acid surface, and the thioctic acid lipid coating (sample 4) Got.

(Production Example 2)
(2) Double coating of thioctic acid Coating granulation using a part of any of the above thioctic acid lipid coatings (sample 1, sample 3) in the production example of the thioctic acid lipid coating (sample 2) A dispersion (made by Kirin Brewery Co., Ltd., trade name: East Wrap (registered trademark)) containing 8.0% yeast cell wall is charged into an apparatus (provided by the company, model: MP-01SFP), and stirred and flowed. It sprayed and the surface of each thioctic acid lipid coating particle was coat | covered with the hydrophilic material, and the thioctic acid double coating (sample 5, sample 7) was obtained. In addition, the thioctic acid lipid coating (sample 2 and sample 4) was treated in the same manner except that the dispersion containing 8.0% yeast cell wall was replaced with an aqueous ethanol solution containing 20% shellac. Coatings (Sample 6, Sample 8) were obtained.

(Test Example 1)
The effects of the composition according to the present invention on endurance, fatigue and the like during exercise were examined by the method described below. That is, the test substances are thioctic acid, thioctic acid lipid coating (sample 1 and sample 3), thioctic acid double coating (sample 5 and sample 7), thioctic acid and creatine. Mixture (1: 1), lipid coating of thioctic acid and creatine mixture (sample 2 and sample 4), double coating of thioctic acid and creatine mixture (sample 6 and sample 8), and comparative test substance as creatine It was. Here, thioctic acid was manufactured by Degussa, Germany, trade name: ALIPURE (registered trademark), creatine was manufactured by Degussa, Germany, trade name: CREAPURE (registered trademark), and creatine monohydrate.

4-week-old male Wistar rats (average body weight: 110 g) were preliminarily raised for 1 week, and 10 rats per group were used as a control group, test substance administration group (10 animals for each test substance), and comparative test substance administration group. divided. As shown in Table 1, the control group had a standard diet (AIN-76A), the test substance administration group and the comparative test substance administration group had a thioctic acid content of 0.5% in the diet and a creatine content in the standardized diet. The feed containing each test substance was ingested so as to be 1.0%, and was bred for 2 weeks. During this period, water was freely consumed, and in order to get used to the swimming exercise in the load swimming exercise test described later, it was allowed to swim freely for 30 minutes every day without applying a load. After breeding under the above conditions, attach a weight equivalent to 6% of the body weight to the trunk of each rat, swim in the water tank, and measure the time (swimming duration) until the face is not exposed to the water surface after 7 days of fatigue. did. Moreover, the lactic acid level in the blood immediately after swimming exercise was measured. These results are shown in Table 2.

From Table 2, when the thioctic acid-containing feed was raised for 2 weeks, the swimming time was significantly prolonged and the blood lactic acid concentration was also low compared to the control group. In addition, a synergistic effect was observed with the combined use of thioctic acids and creatine. Based on this, it was determined that thioctic acids have the effect of preventing fatigue by enhancing endurance during exercise and suppressing the production of lactic acid, which is considered to be one of the fatigue substances. Since creatine conventionally transports ATP energy produced in mitochondria in the form of creatine phosphate and stores it in muscles, creatine phosphate can re-synthesize ATP without requiring oxygen, so it can be instantaneous It is said to be a bioenergy source of so-called, and so to speak, a substance having a rapid-acting bioenergy production promoting effect. On the other hand, thioctic acids show an endurance-extending effect that exceeds that of creatine, and a synergistic effect is observed when used in combination with creatine, and the same effect is evident in terms of inhibiting lactic acid production. Became.

In this test example, data are omitted, but from the results of weight gain, dietary intake, and dietary efficiency during breeding, a significant decrease was observed when thioctic acids or a mixture of thioctic acids and creatine were fed. In addition, the weight of the abdominal fat tissue and the weight of the abdominal fat tissue per body weight of each rat sacrificed after the exercise decreased significantly when a mixture of octoic acids, thioctic acids and creatine was fed. Serum glucose concentration and serum triglyceride concentration at the time of sacrifice were significantly lower when fed with a mixture of thioctic acids, thioctic acids and creatine compared to the control group. The effect by was remarkable. Furthermore, the serum lipid peroxide concentration and liver lipid peroxide concentration at the time of slaughter were significantly lower in the case of serum compared to the target group in the intake of thioctic acids, and this tendency was also observed in the case of the liver. Admitted. From these facts, the anti-obesity effect and the antioxidant effect were confirmed when thioctic acids or a mixture of thioctic acids and creatine were fed.

(Test Example 2)
Ten volunteer female adults (21-54 years old, average age: 32.3 years old) were filled with gelatin capsules filled with 67 mg of thioctic acid and 130 mg of indigestible dextrin used in Test Example 1 (3 days a day). Per thioctic acid intake: 200 mg) was divided into 3 portions and was taken after each meal, and this was continued for 2 weeks. The control group (10 persons) received a gelatin capsule filled with 200 mg of indigestible dextrin in the same manner. Two weeks after the start of taking the capsule, a bicycle ergo loaded with a heart rate that is 50% intensity of the maximum heart rate (heart rate is (maximum heart rate-resting heart rate) / 2 + resting heart rate) Meter exercise was performed for 30 minutes, after which the lactic acid concentration in the blood was measured.

As a result, in the control group, before exercise: 1.45 ± 0.41 (unit: nanomol / liter. Mean value ± standard error; the same applies hereinafter), after exercise: 9.12 ± 2.23, capsule containing thioctic acid In the intake group, before exercise: 1.52 ± 0.44 and after exercise: 6.03 ± 1.47. This reveals that thioctic acid has an effect of suppressing the production of lactic acid produced by exercise even in humans, and this effect is due to ingestion of thioctic acid prior to exercise. It is effective and is considered useful for early recovery from fatigue because the amount of lactic acid produced in the body is suppressed.

(Prototype example 1: Food and drink)
Thioctic acid (manufactured by Degussa, Germany, trade name: ALIPURE (registered trademark), racemic) 170 parts, beeswax 30 parts and medium-chain fatty acid triglyceride (Nisshin Eulio Co., Ltd., trade name: ODO (registered trademark) 50 parts) The mixture was heated and mixed to about 50 ° C. to be homogenized, and then subjected to a capsule filling machine, and a gelatin-coated soft capsule preparation having an internal volume of 300 mg per tablet was prepared by a conventional method. Available as

(Prototype example 2: food and drink)
In Example 1, 170 parts of thioctic acid was replaced with 100 parts of thioctic acid and 70 parts of creatine monohydrate (manufactured by Degussa, Germany, trade name: CREAPURE (registered trademark)). Prototype.

(Prototype example 3: food and drink)
In Example 1, 170 parts of thioctic acid was replaced with 170 parts of a mixture of thioctic acid and guava leaf extract (sample 3) to prepare a dietary supplement.

(Prototype example 4: food and drink)
150 parts of a lipid coating (sample 4) containing thioctic acid, creatine and L-carnitine-L-tartrate, 20 parts of red pepper extract powder (manufactured by BN Co., Ltd.), 30 parts of beeswax and 50 parts of evening primrose oil The mixture was thoroughly mixed at about 45 ° C. to obtain a homogeneous state, and then subjected to a capsule filling machine to prepare a gelatin-coated capsule preparation having an inner volume of 250 mg per grain by a conventional method. This capsule preparation can be taken orally as a dietary supplement.

(Prototype example 5: Food and drink)
47 parts of thioctic acid lipid coating (sample 1), 20 parts of grape seed extract (manufactured by Kikkoman Corporation, “Grabinol”), 25 parts of cystine, 20 parts of lotus germ extract powder (manufactured by Maruzen Pharmaceutical Co., Ltd.), creatine ( Germany Degussa, same as above.) 25 parts, Riboflavin (DSM Nutrition Japan Co., Ltd.) 7 parts, Maltitol (Towa Kasei Co., Ltd.) 105 parts, Tricalcium phosphate (Yoneyama Chemical Industries) 105 parts and Cellulose 26 parts were charged in a mixer and stirred and mixed for 10 minutes. This mixture was subjected to a direct compression tableting machine to prepare uncoated tablets having a diameter of 7 mm, a height of 4 mm, and a weight of 150 mg / piece, and then a shellac film was formed by the coating machine to produce a tablet-shaped food.

(Prototype 6: Food and drink)
20 g of the thioctic acid double coating (sample 5) of the present invention was added to 1 L of commercially available orange juice and mixed well to produce a homogeneous orange flavored beverage. Even if this was stored for 1 week in the refrigerator, no abnormality or discomfort was observed in the appearance and flavor.

The composition comprising the thioctic acid or thioctic acid and creatine of the present invention has the effect of preventing lactic acid production during exercise by ingesting it orally or tube, so sports exercise and overload In performing the work, it can be effectively used in the form of food and drink, pharmaceuticals, feeds, and the like.

Claims (6)

It contains thioctic acids and creatine or creatine salt, creatine monohydrate, creatine citrate, creatine citrate, creatine pyruvate and phosphocreatine as active ingredients. A preventive agent for lactic acid production during exercise under anaerobic conditions where metabolic energy production is characterized.   The thioctic acid is one or more selected from the group consisting of thioctic acid, dihydrothioctic acid, optical isomers thereof, salts, esters and amides of the respective substances, and cyclodextrin inclusion products thereof. 1. The preventive agent according to 1.   Thioctic acid is thioctic acid, dihydrothioctic acid, optical isomers thereof, salts, esters and amides of the respective substances, and one or more crystals or powders selected from the group consisting of these cyclodextrin inclusions 2. The preventive agent according to claim 1, wherein the outer surface of the particle is coated with lipids.   Thioctic acid is thioctic acid, dihydrothioctic acid, optical isomers thereof, salts, esters and amides of the respective substances, and one or more crystals or powders selected from the group consisting of these cyclodextrin inclusions 2. The preventive agent according to claim 1, wherein the outer surface of the particles coated with lipids is further coated with a hydrophilic substance.   The preventive agent according to any one of claims 1 to 4, wherein the thioctic acid is a racemic thioctic acid.   The preventive agent according to any one of claims 1 to 5, wherein the creatine derivative is creatine monohydrate.