JP6518744B2 - Oral composition - Google Patents

Description

  The present invention relates to an oral composition containing an antioxidant.

  It is possible that reactive oxygen, which is formed by partial change of oxygen taken into the living body, damages cells and tissues (oxidative stress) and causes various diseases such as arteriosclerosis, inflammatory reaction, diabetes and the like, It was known before. Also in the epidermis, it is also said that if a foundation rich in sebum and oil is left on the skin for a long time, it combines with active oxygen and becomes oxidized to become a lipid peroxide and causes smear.

  With regard to active oxygen causing the above phenomenon, it is known that about 1 to 2% of oxygen taken in by respiration by the living body becomes active oxygen in the body, but smoking, stress, etc. besides respiration. Ultraviolet rays, exhaust gases and the like are known as factors that generate active oxygen. Furthermore, in addition to this, it is said that active oxygen is also generated by oral intake of pesticides, dioxins, drugs and the like.

  Although a living body usually has a substance (antioxidant) having antioxidant activity to protect against such harmful reaction of active oxygen, such antioxidant activity is greatly affected by age and stress, The activity may be significantly reduced. Therefore, in recent years, for the purpose of improvement of antioxidant activity, development of supplements, beverages and the like having antioxidant activity has been actively carried out (for example, Patent Documents 1, 2 and the like). In addition, in the skin to which a cosmetic has been applied, various external preparations that play a role in preventing the peroxidation of sebum are blended in cosmetics such as emulsion and cosmetic liquid (for example, Patent Document 3 and the like).

  As described in Patent Document 1 and Patent Document 2 above, although various functional enhancement supplements are expected to be expected to have a health promoting effect by removing active oxygen, it is always possible to exert a stable active oxygen removing effect. In addition, functional supplements that can be provided inexpensively have not appeared yet. Therefore, there is a need for an oral composition having a high antioxidative activity effect in a small amount.

  On the other hand, in addition to the recognition that continuous intake of a single antioxidant is not good because it disrupts the body's antioxidant balance, it has been reported that combining multiple antioxidants may have a favorable effect. (Patent Documents 4 and 5).

  However, no specific guidance has been proposed as to what kind of antioxidants can be effectively combined to effectively eliminate active oxygen, and depending on the combination, they may be absorbed into the body. It has been pointed out that it causes a decrease in H., or causes deterioration of each component (Patent Document 6).

Japanese Patent Application Publication No. 07-304666 Japanese Patent Application Publication No. 08-103245 JP, 2009-269919, A JP 2000-189102 A Japanese Patent Publication No. 2004-530407 JP, 2009-062331, A

  The present invention has been made in view of the above circumstances, and an object of the present invention is to provide an oral composition which can express its antioxidant activity more efficiently.

  The inventors of the present invention have found that by taking both the black ginger processed product and vitamin E, the antioxidant action is more pronounced than when they are individually taken, and the present invention has been accomplished. More specifically, the present invention is an oral composition containing processed black ginger and vitamin E.

  ADVANTAGE OF THE INVENTION According to this invention, the antioxidant effect which a black ginger processed material and vitamin E have can be expressed more efficiently.

It is a figure which shows the antioxidant effect of the composition for oral administration of this invention.

  Hereinafter, the embodiments of the present invention will be described in detail, but the present invention is not limited to the following embodiments at all, and can be implemented with appropriate modifications within the scope of the object of the present invention. .

  The present invention is an oral composition containing a processed product of black ginger and vitamin E.

  The black ginger which is used in the present invention has a scientific name of Kaempferia parviflora, and has an alias of black turmeric or kracia dam. It is distributed in Southeast Asia and is a kind of plant of the ginger family (Zingiberaceae) genus Kaempferia. In traditional medicine such as Thailand and Laos, it is known as a health food, and it is said that it has effects such as increasing energy and nourishing. The active ingredients contained in black ginger are, for example, curcumin and polyphenol in addition to selenium and amino acids, and they are said to have the effect of suppressing arteriosclerosis and the like because they have an antioxidative effect of removing active oxygen. ing.

  In the present invention, the processed product of black ginger is a particulate substance containing a component derived from black ginger, and contains at least a component having the above-mentioned antioxidative effect derived from black ginger, and is made into powder, particles, granules There is no particular limitation on the processing method of black ginger if it is For example, a dry powder of black ginger, a powder obtained by pulverizing an extract of black ginger, a powder obtained by fractionating a component in black ginger by an arbitrary method, and the like correspond to the above. The particles do not have to be solid, and may be liquid such as liposome or microcapsule.

  As the dried powder of the above-mentioned black ginger, for example, after washing, the sliced black ginger is dried by using a sun or a dryer, and then it is cut as it is or into an appropriate shape or size, and then crushed. It can be obtained by crushing using an apparatus. As the pulverizing apparatus, those commonly used can be widely used, and, for example, a pulverizer composed of a raw material hopper, a pulverizer, a classifier, a product holder and the like can be used.

  As a powder of the above-mentioned black ginger extract, for example, the extract of black ginger is used as it is or is concentrated, and it is used in the form of liquid, concentrate, paste, or a dried product obtained by further drying these. It is possible. In addition, drying is performed by a method commonly used by those skilled in the art such as spray drying, lyophilization, reduced pressure drying, fluid drying and the like.

  The extract of the above black persimmon can be obtained by extracting black persimmon or its processed product with a suitable solvent. Examples of the solvent used for the extraction include lower alcohols such as ethanol, methanol, isopropanol and butanol, lower esters such as ethyl acetate and methyl acetate, acetone, and mixtures thereof with water. Among them, since the composition of the present invention is intended to be consumed by humans, it is preferable to use ethanol alone or a mixture with water (so-called water-containing ethanol) or hot water.

  When a mixture is used as the solvent, for example, an acetone / water (2/8 to 8/2, volume ratio) mixture, an ethanol / water (2/8 to 8/2, volume ratio) mixture, etc. can be used. . In the case of ethanol / water, it is preferable to add 2 to 20 times the mass of the solvent to the rhizome of black mustard and extract for about 10 minutes to 48 hours at room temperature or under heating.

  Further, it is also possible to obtain an extract by a method such as hot-water extraction of shredded black potato at a temperature of 95 to 100 ° C., filtering an extract having reached the highest concentration, and spray drying.

  Although there is no restriction | limiting in particular in the extraction method to be used, It is preferable to carry out on conditions as mild as possible from a viewpoint of safety | security and convenience. For example, the raw plant part or its dried material is crushed, crushed or shredded, a solvent of 2 to 20 times mass is added to this, and it is allowed to stand for 10 minutes to 48 hours in the range of 0 ° C. The extraction is carried out under any conditions such as stirring, reflux and the like. After the extraction operation, separation operation such as filtration and centrifugation is performed to remove insoluble matter. An extract is obtained by performing dilution and concentration operations on this as needed. Furthermore, the same procedure may be repeated to extract insolubles, and the extract may be used in combination with the previous extract. These extracts may be further purified and used according to the purification method commonly used by those skilled in the art.

  Further, as the particles containing the black ginger component, the above-mentioned dry powder of black ginger, the powder obtained by pulverizing the extract of black ginger, the powder which is obtained by fractionating the components in the black ginger by any method, etc. It may be used as it is, or after addition of an appropriate binder, excipients and the like, it may be used to be formed into granules by a known granulation method such as wet or dry.

  Examples of the product obtained by fractionating the components in the above black ginger by any method include curcumin, methoxyflavones, anthocyanidin and the like. Any of these may be used alone or in combination of two or more.

  It does not restrict | limit especially as a particle diameter of the particle | grains containing a black-tinted rice cake component, According to the objective, powder, particle | grains, a granule, etc. can be selected suitably. In addition, the particle size of the particles containing the black-baked silkworm component is not particularly limited, and powder, particles, granules and the like can be appropriately selected according to the purpose.

  Bark, roots, leaves, branches or the like may be used as the site of use of the black ginger to obtain particles containing the above-mentioned black ginger component. Among them, preferred is rhizome.

  By covering part or all of the particle surface containing the black ginger component with a coating agent containing fats and oils, absorption of polyphenols etc. contained in the black ginger component into the body when taken orally It is preferable because the sex is increased. By carrying out the above-mentioned oil and fat coating, oxidation of black ginger components including polyphenols can be prevented, and storage stability of the product can be enhanced. In addition, the ingredients of black ginger are strong enough to withstand extraction with organic solvents and are difficult to be denatured by exposure to gastric juice etc. However, by coating with fats and oils, it is possible to obtain more denatured prevention effect You can also.

  Vitamin E used in the present invention refers to, for example, tocopherols such as α-type, β-type, and γ-type and derivatives thereof, or mixtures thereof. These vitamins E are a kind of fat-soluble vitamins and are usually obtained in the form of oil (for example, "vitamin E oil"). These have long been known for their antioxidant activity to prevent the oxidation of lipids such as cell membranes, and in recent years, they have also been known for their action on blood lipid oxidation inhibition and blood circulation promotion based on their antioxidant activity.

  The vitamin E suitable for use in the present invention is not particularly limited as long as it has the above-mentioned function, and α-tocopherol or a derivative thereof can be widely used. The use of α-tocopherol or an ester compound of α-tocopherol such as α-tocopherol acetate is preferred from the viewpoint of the action of the antioxidant action. Among them, the use of α-tocopherol is preferred as it is the most active antioxidant biological form of vitamin E.

  The blending ratio of the above-mentioned processed product of black ginger and vitamin E in the composition for oral use varies depending on the content of the antioxidant component and the like in the processed product of black ginger, for example, dry powder of black ginger or black ginger In the combination of powdered extract and vitamin E oil, using at a weight ratio of about 1: 0.00001 to 1: 100000, the expression of the synergetic effect obtained by using both of them is more It is preferable from the point of raising.

  There are no particular restrictions on the method of intake, amount of intake, frequency of intake, timing of intake, and target of intake of the composition of the present invention, and can be appropriately selected according to the purpose. The form of the agent may be, for example, a one-part oral composition comprising a black ginger processed product and vitamin E in a single preparation, or a two-part oral composition separately containing a black ginger processed product and vitamin E It may be a thing. In the latter case, the two agents are mixed at the time of intake, or the two agents are taken simultaneously.

  The intake amount can be appropriately selected in consideration of various factors such as the age, weight, constitution and the like of the intake target individual. Also, the animal species to be ingested is preferably applied mainly to humans, but animals other than humans, for example, mice, rats, hamsters, gerbils, etc., as long as the effects are exhibited. , Ferrets, rabbits, birds, dogs, cats, sheep, goats, cows, horses, pigs, monkeys, reptiles and the like.

  The composition of the present invention is used for oral use, and as its form, food, drink, preparation and the like can be appropriately selected. As the food and drink, the composition may be used as it is, or may be used by dissolving or dispersing it in water (purified water etc.).

  In addition, various nutritional components are added within a range not impairing the effect of the composition, and a form suitable for food, for example, powder, granule, granule, liquid, paste, cream, tablet, capsule Shaped as caplet, caplet, soft capsule, rod, plate, block, gel, jelly, gummi, wafer, biscuit, chew, chewable, syrup, stick etc as food material It can also be provided.

  There is no restriction | limiting in particular as a kind of these application food-drinks, According to the objective, it can select suitably, For example, beverages, such as a soft drink, a carbonated drink, a nutrient drink, a fruit drink, a lactic acid drink; Ice cream, ice Sorbet, frozen ice, etc .; Buckwheat noodles, udon noodles, prickly potatoes, ginza skins, shumai skins, Chinese noodles, instant noodles and other noodles; candy, candy, gum, chocolate, tablets, snacks, biscuits, jellies, jams, creams , Baked goods, bread and other confectionery products; crabs, salmon, clams, tuna, sardines, shrimps, bonito, mackerel, whales, oysters, saurys, squids, mussels, scallops, abalone, sea urchin, salmon roe, tokobushi etc. marine products; , Ham and sausage processed fish and dairy products; processed milk, fermented milk and other dairy products; salad oil, tempura oil, margarine, mayonnaise , Shortening, whipped cream, dressings and other fats and oils and processed foods; sauces, saucers, and other seasonings; curry, stew, chopsticks, chopsticks, chopsticks, chopsticks, risotto, Chinese chopsticks, chopsticks, prawns, prawns, uno chopsticks, hayashi rice, oats, marbodoff Retort pouched foods such as beef bowl, meat sauce, egg soup, omelet rice, eggplant, dumplings, chumé, hamburger, meatballs, etc .; various forms of health food, dietary supplements, etc.

  There is no restriction | limiting in particular as content of the said composition contained in the food-drinks of this invention, According to the objective, it can select suitably.

  Furthermore, the preparation may contain a pharmaceutically acceptable carrier, such as tablets, granules, powders, capsules and the like. It is preferable to encapsulate to increase the amount that is allowed to reach the viscera. Furthermore, one agent of the present invention may be supplied in the form of a drink, syrup, jelly, in addition to those in the form of tablets, powders, capsules and the like.

  The method for producing the capsule may be according to a conventionally known method for producing a soft capsule except that the composition of the present invention is used as the contents. As such a production method, a method of encapsulating contents with a rotary filling machine using a capsule coating sheet and molding a capsule preparation, a method of producing a seamless capsule by a dropping method, and the like can be mentioned.

  Further, for tablets, suitable binders, excipients, disintegrants and, if necessary, lubricants can be added to the composition of the present invention, and the composition can be prepared by a known tableting method. With regard to the granules, various known wet and dry granulation methods can be applied, and they are molded with appropriate binders and excipients. Furthermore, with respect to drinks, syrups, jellies and the like, appropriate sugars, acids, flavors and the like can be added to prepare flavors, and these can be prepared according to known production methods.

  Next, the present invention will be described in more detail based on examples, but the present invention is not limited thereto.

[Confirmation of antioxidative effect promoting effect]
Thiobarbituric acid reaction product in the amount of lipid peroxide in serum when each test substance was administered by single gavage using rat oxidative stress model using iron nitrilotriacetic acid (Fe-NTA) as oxidative stress inducer The antioxidant activity of each test substance was examined by quantifying it as (TBARS) amount.

  Specifically, each test substance is orally administered at 10 mL / kg by single gavage to male Wistar rats (8 weeks old) as follows, and 1 hour after administration, Fe-NTA is intraperitoneally administered at 9 mg Fe / kg. After internal administration, blood was collected 2 hours after administration, and serum was collected to measure lipid peroxide (TBARS) in serum.

<Preparation method of test substance solution>
A test substance solution was prepared by mixing black ginger extract and / or vitamin E as a test substance in the mixing ratio shown in Table 1. The preparation method is as follows. In addition, the black ginger extract (refined powder of a black ginger extract) and vitamin E used by this case etc. used the commercial item as it was.

  The test substance was dissolved or suspended in a 1% aqueous solution of Tween 80 as a solvent to prepare a test substance solution. The comparative example 1 was prepared so that the vitamin E of the comparative example 2 might be 10 mg / mL so that the black ginger extract would be 10 mg / mL. The example was prepared so that black ginger extract and vitamin E were respectively 5 mg / mL + 5 mg / mL in the same solution.

<Method of administering test substance solution>
Fasted rats (from the day before the test) were divided into each group so that the weight value on the test day was almost uniform in each group, and was used for the test. Each test substance solution was administered by single gavage orally based on the weight value on the test day. In Control Example 1 and Control Example 2, the solvent 1% aqueous solution of Tween 80 was orally administered by single gavage. The amount of administration liquid was 10 mL / kg.

<Preparation Method of Iron Nitrilotriacetic Acid (Fe-NTA) Solution>
Dissolve ferric nitrate (III) nonahydrate and nitrilotriacetic acid disodium salt in a molar ratio of 1: 4, respectively, using distilled water as a solvent, and use sodium bicarbonate to achieve pH 7.4. It adjusted and set it as the Fe-NTA solution.

<Method of administering Fe-NTA solution>
One hour after administration of the test substance, the Fe-NTA solution was intraperitoneally administered at 9 mg Fe / kg (10 mL / kg) based on the weight value on the test day. In Control Example 1, saline was intraperitoneally administered at 10 mL / kg instead of the Fe-NTA solution.

<Blood collection method and serum collection method>
Blood was collected 2 hours after Fe-NTA administration, left at room temperature for 30 minutes or more, centrifuged, and serum was collected. The collected serum was cryopreserved at -30 ° C.

<Measurement of lipid peroxide (TBARS) in serum>
The obtained serum was used for measurement with the TBARS Assay Kit (Cayman Chemical Company).

  In FIG. 1, each group of control example 1 (normal control), control example 2 (control), comparative example 1 (black ginger extract), comparative example 2 (vitamin E), example 1 (black ginger extract + vitamin E) Shows the amount of TBARS in serum collected from

  In the black ginger extract and vitamin E single intake (comparative examples 1 and 2), almost no decrease in TBARS amount is observed, but in the combined intake (example 1), it is observed that the value decreases. It was possible to confirm the antioxidative effect of the combination of black ginger extract and vitamin E.

[Application of oral composition to beverages, granules, soft capsules]
Furthermore, using the above-mentioned black ginger extract powder and vitamin E, and the ground product of black ginger obtained in the following manner, drinks, granules and soft capsules were prepared according to the formulation shown in the following table.

(Manufacture of crushed black ginger)
After washing the rhizomes of black ginger, it was sliced to about 1 to 10 mm and dried on the sun for 1 day. Then, it dried with the oven dryer set to 40-100 degreeC for 4 to 6 hours, and after roughly crushing, sterilization was performed at 130-200 degreeC for 5 to 20 seconds. The roughly crushed paste was ground by a grinder to obtain a ground product of black ginger.

Example 2 (Production of Liquid)
Each component was compounded by the compounding ratio of Table 2, and it was set as the liquid agent.

Example 3 (Production of Granule 1)
According to Table 3, 0.3 kg of sucralose, 3 kg of citric acid, 36.9 kg of reduced maltose starch syrup, 48 kg of indigestible dextrin, 0.3 kg of licorice extract, 0.5 kg of crushed black ginger, 0.5 kg of vitamin E, 3 kg of vitamin E, 5 kg of cyclodextrin, 3 kg of shoyaku Is introduced into a flow coater NFLO-200 type fluidized bed granulator (manufactured by Freund Sangyo Co., Ltd.), and mixed with air flow for several minutes. Granulation was carried out by spraying 60 L of water at 2000 mL for 1 minute. Subsequently, the obtained granulated product is sieved with a 30-mesh sieve to obtain granules.

Example 4 (Production of Granule 2)
The components of Table 4 were blended in the same manner as in Example 3 to form granules.

Example 5 (Production of Soft Capsule 1)
The content liquid blended at the blending ratio of Table 5 was adjusted, and the capsule capsule was blended at the blending ratio of Table 6 to obtain a soft capsule. Encapsulation was carried out by casting a capsule shell liquid and forming a film, filling the inside with the content liquid and heat sealing, and drying the molded soft capsule.

Example 6 (Manufacture of Soft Capsule 2)
The content liquid compounded in the compounding ratio of Table 7 was adjusted, and filled in the capsule shell compounded in the compounding ratio of Table 8 to prepare a soft capsule in the same manner as Example 5.

Example 7 (Production of Tablet 1)
The ingredients were compounded at the blending ratio shown in Table 9 and uniformly mixed, and then they were molded into tablets 1 using a tableting apparatus.

Example 8 (Production of Tablet 2)
Tablets 2 were obtained in the same manner as in Example 7 except for blending at the blending ratio shown in Table 10.

Claims (1)

A capsule, a tablet or a liquid preparation for ameliorating and / or preventing dullness characterized by containing a black ginger processed product and vitamin E.