JP6010482B2 - Oral composition - Google Patents

Description

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

  Active oxygen produced by changing some of the oxygen taken into the body can damage cells and tissues (oxidative stress) and cause various diseases such as arteriosclerosis, inflammatory reaction, diabetes, It has been known for some time. Also, in the epidermis, if a foundation rich in sebum or oil is left on the skin for a long time, it is said that it binds with active oxygen and oxidizes to become lipid peroxide and dullness.

  About the active oxygen that causes the above phenomenon, it is known that about 1-2% of the oxygen taken in by the living body breathing becomes active oxygen in the body, but in addition to breathing, smoking, stress, Ultraviolet rays, exhaust gas, and the like are known as factors that generate active oxygen. In addition, it is said that active oxygen is also generated by ingestion of agricultural chemicals, dioxins, drugs, and the like.

  A living body usually has a substance having an antioxidant activity (antioxidant) to prevent such an adverse reaction of active oxygen, but such an antioxidant activity is greatly influenced by age and stress. Activity may be significantly reduced. Therefore, in recent years, for the purpose of improving the antioxidant activity, supplements, beverages and the like having an antioxidant action have been actively developed (for example, Patent Documents 1 and 2). In addition, various external preparations that play a role of preventing peroxidation of sebum in skin to which cosmetics are applied are blended in cosmetics such as milky lotion and cosmetic liquid (for example, Patent Document 3).

  As shown in Patent Document 1 and Patent Document 2 above, various types of function-enhanced supplements that are expected to promote health by removing active oxygen have been studied, but can always exhibit stable removal of active oxygen. Moreover, functionally enhanced supplements that can be provided at low cost have not yet appeared. Therefore, there is a demand for oral compositions that have a high antioxidant 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 destroys the antioxidant balance in the body, it has been reported that a combination of multiple antioxidants may give a favorable effect. (Patent Documents 4 and 5).

  However, no effective guideline has been proposed regarding what kind of antioxidants can be combined to make the elimination of active oxygen more efficient. Depending on the combination, absorption into the body is rather difficult. It has been pointed out that this also causes a decrease in the amount of water and deterioration of each component (Patent Document 6).

Japanese Patent Application Laid-Open No. 07-304666 Japanese Patent Laid-Open No. 08-103245 JP 2009-269919 A JP 2000-189102 A Special table 2004-530407 gazette JP 2009-062331 A

  This invention is made | formed in view of the said situation, and aims at provision of the composition for oral administration which can express an antioxidant effect | action more efficiently.

  The present inventors have found that by taking both black ginger processed products and vitamin E, the antioxidant effect appears stronger than when they are taken alone, and the present invention has been completed. 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 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 use of this invention.

  Hereinafter, embodiments of the present invention will be described in detail. However, the present invention is not limited to the following embodiments, 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 black ginger and vitamin E.

  The black ginger used in the present invention is called Kaempferia parviflora and has an alias of black turmeric or Krachaidam. It is a kind of plant belonging to the genus Zingiberaceae Kaempferia distributed in Southeast Asia. It is known as a health food in traditional medicine such as Thailand and Laos, and is said to have effects such as energy enhancement and nutrition and tonic. In addition to selenium and amino acids, there are, for example, curcumin and polyphenols as active ingredients contained in black ginger, and these are said to have an effect of suppressing arteriosclerosis and the like because they have an antioxidant action to remove active oxygen. ing.

  The processed black ginger in the present invention refers to a granular material containing components derived from black ginger, and includes at least the above-described antioxidant effect derived from black ginger, and is powdered, granulated, granulated There is no particular limitation on the processing method of the black ginger as long as it has been converted to a standard. For example, dry powder of black ginger, powdered black ginger extract, and powder obtained by fractionating components in black ginger by any method are applicable. The particles do not need to be solid, and may be liquids such as liposomes and microcapsules.

  As the dry powder of the black ginger, for example, after washing, the sliced black ginger is dried using the sun or a dryer, and then processed as it is or cut into an appropriate shape and size. It can be obtained by grinding using an apparatus. As the pulverizer, those that are usually used can be widely used. For example, a pulverizer composed of a raw material hopper, a pulverizer, a classifier, a product holder and the like can be used.

  As the powdered black ginger extract, for example, the black ginger extract is used as it is or in a concentrated form in the form of a liquid, a concentrated product, a paste, or a dried product obtained by drying these. It is possible. The drying is performed by a method commonly used by those skilled in the art such as spray drying, freeze drying, reduced pressure drying, fluidized drying and the like.

  The black ginger extract is obtained by extracting black ginger or a processed product thereof with a suitable solvent. Examples of the solvent used for extraction include lower alcohols such as ethanol, methanol, isopropanol, and butanol, lower esters such as ethyl acetate and methyl acetate, acetone, and a mixture of these with water. Among them, since the composition of the present invention is supposed to be ingested by humans, it is preferable to use ethanol alone or a mixture with water (so-called hydrous 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, or the like can be used. . In the case of ethanol / water, it is preferable to add a solvent having a mass of 2 to 20 times the mass of black ginger rhizome and extract it at room temperature or under heating for about 10 minutes to 48 hours.

  It is also possible to extract the black ginger by hot water extraction at a temperature of 95-100 ° C., filter the extract reaching the maximum concentration, and then spray-dry it.

  There are no particular limitations on the extraction method to be used, but it is preferable to perform the extraction method under as mild conditions as possible from the viewpoint of safety and convenience. For example, pulverize, crush or shred the raw material plant part or its dried product, add 2 to 20 times the mass of the solvent, and leave it at 0 ° C. to the reflux temperature of the solvent for 10 minutes to 48 hours. The extraction is performed under any conditions such as stirring or refluxing. After the extraction operation, separation operations such as filtration and centrifugation are performed to remove insoluble matters. An extract is obtained by diluting and concentrating as necessary. Further, the same operation may be repeated for insoluble matter, and the extract may be used in combination with the previous extract. These extracts may be used after further purification by a purification method commonly used by those skilled in the art.

  Further, as the particles containing black ginger components, the above-mentioned black ginger dry powder, those obtained by pulverizing black ginger extract, those obtained by fractionating the components in black ginger and pulverizing by any method, etc. You may use as it is, and after adding a suitable binder, an excipient | filler, etc., you may use what was shape | molded by the granulation method of well-known wet and dry granulation.

  Examples of products obtained by fractionating the components in the black ginger by any method include curcumin, methoxyflavones, and anthocyanidins. Any one of these powders may be used, or two or more may be mixed and used.

  The particle diameter of the particles containing the black ginger component is not particularly limited, and powders, particles, granules and the like can be appropriately selected according to the purpose. The particle size of the particles containing the black ginger component is not particularly limited, and powders, particles, granules, and the like can be appropriately selected according to the purpose.

  Bark, roots, leaves, branches, or the like can be used as the part where black ginger is used to obtain particles containing the above-described black ginger component. Among them, preferred is a rhizome.

  When part or all of the particle surface containing the black ginger component is coated with a coating agent containing fats and oils, it is absorbed into the body, especially polyphenols contained in the black ginger component, when taken orally. This is preferable because of increased properties. By performing the oil-and-fat coating, oxidation of black ginger components including polyphenols can be prevented, and the storage stability of the product can be improved. In addition, the components of black ginger are strong enough to withstand extraction with organic solvents and are not easily denatured by exposure to gastric juice, etc. 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 a mixture thereof. These vitamin Es are a kind of fat-soluble vitamins and are usually obtained in oil form (for example, “vitamin E oil”). These have long been known for their antioxidant activity that prevents the oxidation of lipids such as cell membranes. In recent years, they have also been known to have functions such as blood lipid oxidation-inhibiting activity and blood circulation promoting activity based on antioxidant activity.

  The appropriate vitamin E used in the present invention is not particularly limited as long as it has the above-described function, and α-tocopherol or a derivative thereof can be widely used. From the viewpoint of the action of antioxidant action, α-tocopherol or an ester compound of α-tocopherol, for example, α-tocopherol acetate is preferably used. Among these, the use of α-tocopherol is preferred because it is the most active antioxidant biological form of vitamin E.

  The blending ratio of the black ginger processed product and vitamin E in the composition for oral use varies depending on the content of the antioxidant component in the processed black ginger processed product, for example, black ginger dry powder or black ginger In the combination of the powdered extract of extract and vitamin E oil, the weight ratio is about 1: 0.00001 to 1: 100,000. It is preferable from the point of increasing.

There is no restriction | limiting in particular as an ingestion method of the composition of this invention, an ingestion amount, the frequency | count of ingestion, an ingestion time, and an ingestion object, According to the objective, it can select suitably. The form of the agent may be, for example, a one-part oral composition containing black ginger processed product and vitamin E in one agent, or a two-part oral composition containing black ginger processed product and vitamin E separately. It is good also as a thing. In the latter case, the two drugs are mixed at the time of ingestion, or the two drugs are taken at the same time.

  The intake amount can be appropriately selected in consideration of various factors such as the age, weight and constitution of the individual to be ingested. In addition, the animal species to be ingested are mainly suitably applied to humans, but animals other than humans, such as mice, rats, hamsters, gerbils, etc., as long as their effects are exerted. , 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, foods and drinks, preparations and the like can be appropriately selected. As said food-drinks, the said composition may be used as it is, and you may use it melt | dissolving thru | or disperse | distributing only with water (purified water etc.).

  Further, various nutritional ingredients are added within a range not impairing the effect of the composition, and the form suitable for edible use, for example, powder, granule, granule, liquid, paste, cream, tablet, capsule , Caplet, soft capsule, rod, plate, block, gel, jelly, gummy, wafer, biscuit, bowl, chewable, syrup, stick, etc. It can also be provided.

  There is no restriction | limiting in particular as kind of these applicable food-drinks, According to the objective, it can select suitably, For example, drinks, such as a soft drink, a carbonated drink, a nutrition drink, a fruit drink, a lactic acid drink; Ice cream, ice Frozen confectionery such as sorbet and shaved ice; noodles such as buckwheat, udon, harusame, gyoza skin, sushi mai, Chinese noodles and instant noodles; rice cake, candy, gum, chocolate, tablet confectionery, snack confectionery, biscuits, jelly, jam, cream , Baked confectionery, bakery and other confectionery; crab, salmon, clam, tuna, sardine, shrimp, bonito, mackerel, whale, oyster, saury, squid, red scallop, scallop, abalone, sea urchin, crabs, tocobushi, etc .; Processed fishery and livestock products such as ham, sausage; dairy products such as processed milk and fermented milk; salad oil, tempura oil, margarine, mayonnaise , Shortening, whipped cream, dressing and other fats and oils processed foods; sauces, sauces and other seasonings; curry, stew, oyakodon, rice bowl, miscellaneous cooking, Chinese rice bowl, bowl, tempura, eel rice, hayashi rice, oden, mabodorf Retort pouch foods such as beef bowl, meat sauce, egg soup, omelet rice, dumplings, shumai, hamburger, meatballs; various forms of health foods, dietary supplements and the like.

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

  Furthermore, the preparation may contain a pharmacologically acceptable carrier, and examples thereof include tablets, granules, powders, capsules and the like. It is preferable to encapsulate and increase the amount that reaches the internal organs as it is. Furthermore, one agent of the present invention can be supplied in the form of drinks, syrups, and jelly, in addition to those having dosage forms such as tablets, powders, and capsules.

  As a method for producing capsules, a conventionally known method for producing soft capsules may be used except that the composition of the present invention is used as the contents. Examples of such a production method include a method of encapsulating contents with a rotary filling machine using a capsule film sheet and molding a capsule preparation, or a method of producing seamless capsules by a dropping method.

  The tablet can be prepared by a known tableting method by adding an appropriate binder, excipient, disintegrant and, if necessary, a lubricant to the composition of the present invention. As for the granule, known various wet and dry granulation methods can be applied, and it is molded together with an appropriate binder and excipient. Furthermore, drinks, syrups, jellies and the like can be prepared by adding known sugars, acids, fragrances and the like to prepare flavors and preparing them by 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 antioxidant effect]
Using a rat oxidative stress model using iron nitrilotriacetic acid (Fe-NTA) as an oxidative stress inducer, the amount of lipid peroxide in serum when a single oral gavage was administered to each test substance was a thiobarbituric acid reaction product The antioxidant action of each test substance was examined by quantifying the amount as (TBARS).

  Specifically, in the following manner, male Wistar rats (8-week-old) were subjected to a single oral gavage of each test substance at 10 mL / kg, and 1 hour after administration, Fe-NTA was intraperitoneally injected at 9 mg Fe / kg. Then, blood was collected 2 hours after administration, serum was collected, and serum lipid peroxide (TBARS) was measured.

<Method for preparing test substance solution>
As a test substance, black ginger extract and / or vitamin E were mixed at a blending ratio shown in Table 1 to prepare a test substance solution. The preparation method is as follows. In addition, as for the black ginger extract (purified powder of black ginger extract) and vitamin E used in this case, commercially available products were used as they were.

  A test substance solution was prepared by dissolving or suspending the test substance using a 1% Tween 80 aqueous solution as a solvent. Comparative Example 1 was prepared so that the black ginger extract was 10 mg / mL, and Comparative Example 2 was prepared so that vitamin E was 10 mg / mL. The examples were prepared so that black ginger extract and vitamin E were 5 mg / mL + 5 mg / mL, respectively, in the same solution.

<Method of administration of test substance solution>
The fasted rats (from the day before the test) were divided into groups so that the weight values on the test day were almost uniform in each group, and were subjected to the test. Each test substance solution was administered by single oral gavage based on the body weight on the test day. In Control Example 1 and Control Example 2, a 1% Tween 80 aqueous solution as a solvent was administered by single oral gavage. The administration liquid volume was 10 mL / kg.

<Preparation method of iron nitrilotriacetic acid (Fe-NTA) solution>
Using distilled water as a solvent, iron (III) nitrate nonahydrate and nitrilotriacetic acid disodium salt are dissolved in a molar ratio of 1: 4, respectively, and adjusted to pH 7.4 using sodium bicarbonate. It adjusted and it was set as the Fe-NTA solution.

<Method of administration of Fe-NTA solution>
One hour after administration of the test substance, the Fe-NTA solution was intraperitoneally administered at 9 mgFe / kg (10 mL / kg) based on the body weight value on the test day. In Control Example 1, physiological 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 the administration of Fe-NTA and allowed to stand at room temperature for 30 minutes or more, and then centrifuged to collect serum. The collected serum was stored frozen at −30 ° C.

<Measurement of serum lipid peroxide (TBARS)>
Using the obtained serum, TBARS Assay Kit (Cayman
The measurement was carried out at the Chemical Company.

  FIG. 1 shows groups of Control Example 1 (normal control), Control Example 2 (control), Comparative Example 1 (black ginger extract), Comparative Example 2 (vitamin E), and Example 1 (black ginger extract + vitamin E). Shows the amount of TBARS in the serum collected from.

  Ingestion of black ginger extract and vitamin E alone (Comparative Examples 1 and 2) shows almost no decrease in the amount of TBARS, but it is observed that the value decreases when ingested in combination (Example 1). In addition, the enhancement effect of the antioxidant effect by the combination of black ginger extract and vitamin E was confirmed.

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

(Manufacture of crushed black ginger)
After washing the black ginger rhizome, it was sliced to about 1 to 10 mm and dried in the sun for one day. Then, it dried for 4 to 6 hours with the oven dryer set to 40-100 degreeC, and sterilized at 130-200 degreeC for 5 to 20 second after coarse grinding. The sterilized coarsely pulverized product was pulverized by a pulverizer to obtain a black ginger pulverized product.

Example 2 (Manufacture of a liquid agent)
Each component was blended at the blending ratio in Table 2 to obtain a liquid.

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

Example 4 (Production of granules 2)
In the same manner as in Example 3, the ingredients shown in Table 4 were blended to prepare granules.

Example 5 (Production of soft capsule 1)
The content liquid blended at the blending ratio shown in Table 5 was prepared, and the capsule film blended at the blending ratio shown in Table 6 was filled into soft capsules. Encapsulation was performed by casting a capsule coating solution to form a film, filling the content solution inside, heat-sealing, and drying the formed soft capsule.

Example 6 (Production of soft capsule 2)
The content liquid blended at the blending ratio shown in Table 7 was prepared, and the capsule film blended at the blending ratio shown in Table 8 was filled into soft capsules as in Example 5.

Example 7 (Production of tablet 1)
Each component was blended at a blending ratio shown in Table 9 and mixed uniformly, and then formed into a tablet 1 using a tableting device.

Example 8 (Production of tablet 2)
A tablet 2 was prepared in the same manner as in Example 7 except that it was blended at the blending ratio shown in Table 10.

Claims (3)

A composition for enhancing oral antioxidant effect, comprising black ginger processed product and vitamin E. A composition for promoting blood circulation comprising vitamin E as an active ingredient, further comprising a processed product of black ginger (however, excluding granules). A composition for preventing lipid oxidation in the body, comprising vitamin E as an active ingredient, and further containing a processed product of black ginger (except for granules).

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