Oral composition, absorption enhancer for ascorbic acid or salts thereof, and cell permeability enhancer for ascorbic acid or salts thereof

Abstract

To provide an oral composition that enhances the absorption of ascorbic acid or salts thereof.SOLUTION: Prepared is an oral composition containing (A) Centella asiatica or Centella asiatica extract and (B) ascorbic acid or salts thereof. Also prepared are an absorption enhancer for ascorbic acid or salts thereof, as well as a cell permeability enhancer for ascorbic acid or salts thereof, containing Centella asiatica or Centella asiatica extract as an active ingredient. These agents can also serve as an oral composition.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to an oral composition containing Centella asiatica and / or an extract thereof. More specifically, the present invention relates to an oral composition containing an absorption enhancer for ascorbic acid or a salt thereof, an agent for improving the cell permeability of ascorbic acid or a salt thereof, and ascorbic acid or a salt thereof. [Background technology]

[0002] Ascorbic acid is known to have various effects, such as anti-inflammatory effects, acne treatment, whitening effects, anti-aging effects, antioxidant effects, cell activation effects by promoting the synthesis of biological components such as collagen, and suppression of cell damage and DNA damage caused by ultraviolet rays in epidermal keratinocytes. For these reasons, it is widely used as a topical skin preparation and supplement.

[0003] Preparations aimed at promoting the absorption of ascorbic acid for oral administration have also been proposed (Patent Document 1). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Application Laid-Open No. 2013-49670 Summary of the Invention [Problem to be solved by the invention]

[0005] An object of the present invention is to provide a means for improving the absorption and cellular permeation of ascorbic acid or a salt thereof. [Means for solving the problem]

[0006] For ascorbic acid or a salt thereof, absorption into the intestinal tract, particularly the small intestine, is an essential issue for an oral composition.

[0007] As a result of extensive research, the present inventors have discovered that the absorbability and cell permeability of ascorbic acid or a salt thereof can be increased by preparing an agent or composition containing Centella asiatica and / or an extract thereof, and have thus completed the present invention.

[0008] That is, the present invention provides the oral compositions or agents listed below. [1] An oral composition comprising (A) Centella asiatica and / or an extract thereof and (B) ascorbic acid or a salt thereof. [2] The composition for oral administration according to [1], wherein the total content of the component (B) is 10 to 1000 parts by mass per part by mass of the component (A). [3] An absorption enhancer for ascorbic acid or its salts, which contains Centella asiatica and / or its extract. [4] A cell permeation enhancer for ascorbic acid or its salts containing Centella asiatica and / or its extract. [5] The agent according to [3] or [4], which is an oral composition. [Effects of the Invention]

[0009] According to the present invention, it is possible to provide an agent or oral composition having good absorbability and cell permeability of ascorbic acid or a salt thereof, particularly an agent or oral composition having good absorbability into the intestinal tract and small intestine and good permeability into intestinal cells. DETAILED DESCRIPTION OF THE INVENTION

[0010] In this specification, examples of salts include salts with organic bases (e.g., salts with tertiary amines such as trimethylamine salts, triethylamine salts, monoethanolamine salts, triethanolamine salts, and pyridine salts; basic ammonium salts such as arginine); salts with inorganic bases (e.g., alkali metal salts such as ammonium salts, sodium salts, and potassium salts; alkaline earth metal salts such as calcium salts and magnesium salts; and aluminum salts).

[0011] [Oral composition] One aspect of the present invention relates to an oral composition containing (A) Centella asiatica and / or an extract thereof and (B) at least one member selected from the group consisting of ascorbic acid and salts of ascorbic acid.

[0012] ((A) Centella asiatica and / or its extract) Centella asiatica is a plant of the genus Centella in the family Apiaceae, and is used as a raw material for herbal medicines. When Centella asiatica and / or an extract thereof is used, it is preferably at least one selected from the group consisting of the whole plant, fruit, pericarp, flower (petals, ovary, etc.), seed, leaf, stem, and root, or an extract thereof. Of these, the whole plant, leaf, and / or stem, or an extract thereof, is more preferred, and a leaf extract is even more preferred.

[0013] The extract can be obtained by a conventional extraction method used for plant extraction. Examples of solvents that can be used include water; alcohols such as methanol, ethanol, propanol, isopropanol, and butanol; polyhydric alcohols such as ethylene glycol, propylene glycol, 1,2-butylene glycol, 1,3-butylene glycol, 1,4-butylene glycol, and 2,3-butylene glycol; ketones such as acetone and methyl ethyl ketone; and esters such as methyl acetate and ethyl acetate. While not limited to these, ethanol and water are preferred. Commercially available Centella asiatica extracts may also be used.

[0014] To achieve the effects of the present invention more effectively, when a Centella asiatica extract is used, its content is, for example, preferably 0.001% by mass or more, more preferably 0.005% by mass or more, and particularly preferably 0.01% by mass or more, based on the total amount of the composition. The content of the Centella asiatica extract may be 0.0001% by mass or more, 0.0005% by mass or more, 0.003% by mass or more, 0.05% by mass or more, or 0.1% by mass or more. The content of the Centella asiatica extract is preferably 50% by mass or less, more preferably 20% by mass or less, and particularly preferably 10% by mass or less. It may also be 70% by mass or less, 60% by mass or less, 30% by mass or less, 5% by mass or less, or 1% by mass or less.

[0015] To achieve the effects of the present invention more significantly, when Centella asiatica is used, its content is, for example, preferably 0.01% by mass or more, more preferably 0.05% by mass or more, and particularly preferably 0.1% by mass or more, based on the total amount of the composition. The Centella asiatica content may be 0.001% by mass or more, 0.005% by mass or more, 0.03% by mass or more, 0.5% by mass or more, or 1% by mass or more. The Centella asiatica content is preferably 95% by mass or less, more preferably 40% by mass or less, and particularly preferably 20% by mass or less. It may also be 70% by mass or less, 60% by mass or less, 30% by mass or less, 10% by mass or less, or 2% by mass or less.

[0016] Here, the contents of Centella asiatica and / or its extract are all dry solid contents. In the case of Centella asiatica extract, the ratio of crude drug to crude drug is usually 1 to 100:1, preferably 5 to 50:1, more preferably 7 to 20:1, and even more preferably 10 to 15:1 (1 kg of extract can be produced from 10 kg to 15 kg of leaves). Furthermore, the total content of asiatic acid, madecassic acid, madecassoside, and asiaticoside is preferably 5% by mass or more, more preferably 10% by mass or more, even more preferably 20% by mass or more, even more preferably 30% by mass or more, and particularly preferably 45% by mass or more.

[0017] The daily intake of Centella asiatica extract may vary depending on the condition of the individual taking it (body weight, age, sex, etc.), the formulation of the composition, etc., but from the viewpoint of significantly achieving the effects of the present invention, it is, for example, preferably 0.01 mg or more, more preferably 0.1 mg or more, and even more preferably 0.5 mg or more. It may be 1 mg or more, 5 mg or more, 10 mg or more, etc. It may also be 500 mg or less, preferably 300 mg or less, more preferably 100 mg or less, and may be 70 mg or less, 50 mg or less, 20 mg or less, or 10 mg or less.

[0018] The daily intake of Centella asiatica varies depending on the condition of the individual taking it (body weight, age, sex, etc.), the formulation of the composition, etc., but from the viewpoint of significantly achieving the effects of the present invention, it is, for example, preferably 0.1 mg or more, more preferably 1 mg or more, and even more preferably 5 mg or more. It may be 10 mg or more, 50 mg or more, 100 mg or more, etc. It may also be 5000 mg or less, preferably 3000 mg or less, and even more preferably 1000 mg or less. It may also be 500 mg or less, 200 mg or less, or 100 mg or less.

[0019] ((B) At least one selected from the group consisting of ascorbic acid and salts of ascorbic acid) The ascorbic acid used in the present invention can be ascorbic acid commercially available as a component of pharmaceuticals, quasi-drugs, or external skin preparations in the cosmetic field, and these generally refer to the L-isomer.

[0020] Salts of ascorbic acid can also be used. Particularly preferred salts of ascorbic acid are sodium salts, potassium salts, and magnesium salts. Specific examples include sodium ascorbate, sodium ascorbic acid monophosphate, sodium ascorbic acid diphosphate, sodium ascorbic acid triphosphate, sodium ascorbic acid 2-sulfate, and magnesium L-ascorbyl phosphate. Furthermore, liposomal ascorbic acid or a salt thereof, or oil-coated ascorbic acid or a salt thereof can also be used.

[0021] (liposomal ascorbic acid or its salt) The ascorbic acid and / or a salt thereof used in the present invention may be encapsulated in a liposome (ascorbic acid encapsulated in a liposome may be referred to herein as liposomal ascorbic acid). A liposome is a monolayer or multilayer closed endoplasmic reticulum of phospholipids, and ascorbic acid or a salt thereof may be encapsulated in the internal aqueous or lipid layer. The term "encapsulated" of a desired component in a liposome may refer to any of the following: being encapsulated in the space within the liposome membrane, being present together with components of the liposome membrane, being present between the multiple membranes constituting the liposome, or being bound to or attached to the surface of the outermost membrane constituting the liposome.

[0022] The size of liposomal ascorbic acid or a salt thereof is usually about 30 to 1000 nm, preferably 30 to 600 nm, and more preferably 50 to 200 nm.

[0023] Liposomes containing ascorbic acid or a salt thereof can be produced by a conventional method. For example, lecithin and optionally a sterol are solubilized in a solvent such as ethanol, the solvent is removed under reduced pressure to prepare membrane lipids, and then a solution containing ascorbic acid or a salt thereof is added to the membrane lipids and stirred to prepare a liposome suspension, thereby obtaining liposomes containing the components.

[0024] In addition to these methods, liposomes can also be obtained by dissolving lecithin and, optionally, a sterol in a small amount of ethanol, dispersing the lecithin in an aqueous solution or a buffer solution to pre-emulsify the solution, and dispersing the solution under high pressure to form a lipid bilayer to prepare a liposome suspension.

[0025] For example, commercially available liposomes containing ascorbic acid include "Vitamin C Zeal" (manufactured by Aurea Biolabs) and "Lypo-C [lipocapsule] Vitamin C" (manufactured by Spic).

[0026] (Oil-coated ascorbic acid or its salt) The ascorbic acid and / or its salt used in the present invention may be coated with an oil or fat. This may be, but is not limited to, an animal-derived oil or vegetable oil coated on ascorbic acid and / or its salt. Preferred examples of the oil or fat include hydrogenated oil and fat. Examples include vegetable oils such as hydrogenated soybean oil, rice bran wax, and hydrogenated seed oil, and animal oils such as hydrogenated beef tallow oil. These oils and fats may be powdered oils whose surfaces have been coated with a hydrophilic material in advance.

[0027] The oil or fat coating for ascorbic acid and / or a salt thereof can be produced by a conventionally known method, for example, a conventional coating method such as tumbling granulation, extrusion granulation, compression granulation, fluidized bed granulation, pulverization granulation, stirring granulation, or melt mixing.

[0028] Commercially available products of ascorbic acid and / or a salt thereof coated with oil or fat can also be used. Commercially available liposomes encapsulating ascorbic acid include "VC-80R" (manufactured by NOF Corporation), "Ascorbic Acid-95R" (manufactured by NOF Corporation), and "Vitacoat C-95" (manufactured by Yokohama Oil & Fat Industries Co., Ltd.).

[0029] In the present invention, ascorbic acid or a salt thereof can be used alone or in combination of two or more kinds.

[0030] In the oral composition of the present invention, the total content of component (B) relative to the total amount of the composition is appropriately determined based on the balance with other components. The total content of component (B) relative to the total amount of the composition is 1% by mass or more, preferably 5% by mass or more, and even more preferably 10% by mass or more. It may be 20% by mass or more, 30% by mass or more, 40% by mass or more, etc. The total content of component (B) relative to the total amount of the composition is 95% by mass or less, preferably 80% by mass or less, and even more preferably 70% by mass or less. It may be 60% by mass or less, 50% by mass or less, or 40% by mass or less. The total content of component (B) relative to the total amount of the composition is 1% by mass to 95% by mass, preferably 10% by mass to 80% by mass, and even more preferably 20% by mass to 70% by mass. It may be 30% by mass to 60% by mass, etc.

[0031] The daily intake of ascorbic acid may vary depending on the condition of the individual taking it (body weight, age, sex, etc.), the formulation of the composition, etc., but from the viewpoint of significantly achieving the effects of the present invention, it is, for example, preferably 10 mg or more, more preferably 100 mg or more, even more preferably 200 mg or more, and even more preferably 300 mg or more. It may also be 3000 mg or less, preferably 2500 mg or less, and more preferably 2000 mg or less. It may also be 400 mg or more, 500 mg or more, 600 mg or more, 1000 mg or more, 1500 mg or more, or 2000 mg or more.

[0032] In the oral composition of the present invention, from the viewpoint of more significantly achieving the effects of the present invention, the ratio of (B) ascorbic acid or a salt thereof to (A) Centella asiatica extract (also referred to as Centella asiatica extract) is, for example, preferably 0.1 parts by mass or more, more preferably 1 part by mass or more, even more preferably 10 parts by mass or more, even more preferably 20 parts by mass or more, particularly preferably 50 parts by mass or more, and most preferably 100 parts by mass or more, per 1 part by mass of the content of component (A). It may also be 0.001 parts by mass or more, 0.01 parts by mass or more, etc. Furthermore, the content of Centella asiatica extract per 1 part by mass of the content of component (A) is preferably 10,000 parts by mass or less, more preferably 5,000 parts by mass or less, even more preferably 3,000 parts by mass or less, even more preferably 1,000 parts by mass or less, particularly preferably 500 parts by mass or less, and most preferably 300 parts by mass or less. It may also be 100,000 parts by mass or less, 50,000 parts by mass or less.

[0033] In the oral composition of the present invention, from the viewpoint of more significantly achieving the effects of the present invention, the ratio of (B) ascorbic acid or a salt thereof to (A) Centella asiatica is, for example, preferably 0.01 parts by mass or more, more preferably 0.1 parts by mass or more, even more preferably 1 part by mass or more, even more preferably 2 parts by mass or more, particularly preferably 5 parts by mass or more, and most preferably 10 parts by mass or more, per 1 part by mass of the content of component (A). It may also be 0.0001 parts by mass or more, 0.001 parts by mass or more, etc. Furthermore, the content of Centella asiatica extract per 1 part by mass of the content of component (A) is preferably 1,000 parts by mass or less, more preferably 500 parts by mass or less, even more preferably 300 parts by mass or less, even more preferably 100 parts by mass or less, particularly preferably 50 parts by mass or less, and most preferably 30 parts by mass or less. It may also be 10,000 parts by mass or less, or 5,000 parts by mass or less.

[0034] (Other ingredients) The oral composition of the present invention may contain pharmacologically or physiologically active ingredients other than the components (A) and (B) to the extent that the effects of the present invention are not impaired. The pharmacologically or physiologically active ingredients may be used alone or in combination of two or more. Such ingredients include, but are not limited to, various vitamins and peptides.

[0035] Examples of vitamins include vitamin A [e.g., retinal, retinol, retinoic acid, carotene, dehydroretinal, lycopene, etc.], vitamin B [e.g., thiamine, thiamine disulfide, dicethiamine, octotiamine, shikotiamine, bis-ibutiamine, bis-bentiamine, prosultiamine, benfotiamine, fursultiamine, riboflavin, flavin adenine dinucleotide, pyridoxine, pyridoxal, hydroxocobalamin, cyanocobalamin, methylcobalamin, deoxyadenocobalamin, folic acid, tetrahydrofolic acid, dihydrofolic acid, nicotinic acid, nicotinamide, nicotinyl alcohol, pantothenic acid, panthenol, biotin, choline, inositol, etc.], vitamin Ds [e.g., ergocalciferol, cholecalciferol, hydroxycholecalciferol, dihydroxycholecalciferol, dihydrotachysterol, etc.], vitamin Es [e.g., tocopherol and its derivatives, ubiquinone derivatives, etc.], other vitamins [e.g., hesperidin, carnitine, ferulic acid, γ-oryzanol, orotic acid, rutin, eriocitrin, etc.], etc. Among these, water-soluble vitamins are preferred, and water-soluble vitamins including vitamin Bs are more preferred.

[0036] The oral composition of the present invention may contain additives to the extent that the effects of the present invention are not impaired. Specific examples of such additives include sugar alcohols, oils and fats, binders, flavorings, excipients, disintegrants, lubricants, colorants, flavoring agents, odorants, sugars, polyhydric alcohols, high-intensity sweeteners, emulsifiers, thickeners, acidulants, fruit juices, etc.

[0037] Examples of sugar alcohols include lactose, maltose, fructose, sorbitol, maltitol, mannitol, xylitol, and trehalose.

[0038] Examples of fats and oils include vegetable fats and oils such as castor oil, cottonseed oil, soybean oil, camellia oil, olive oil, sesame oil, peanut oil, corn oil, coconut oil, rapeseed oil, wheat germ oil, safflower oil, sunflower oil, safflower oil, perilla oil, hardened oil, and cacao butter; animal fats and oils such as lard stabilized by hydrogenating coconut oil, beef tallow, milk fat, and cod liver oil; mineral fats and oils such as silicone oil; and functional fats and oils such as medium-chain fatty acid triglycerides and long-chain fatty acid triglycerides.

[0039] Examples of functional oils and fats include compounds in which short-chain fatty acids having 2 to 4 carbon atoms, medium-chain fatty acids having 5 to 12 carbon atoms, or fatty acids having a chain longer than 12 carbon atoms are ester-bonded to mono- to decaglycerin. Examples of short-chain fatty acids include butyric acid, etc. Examples of medium-chain fatty acids include valeric acid, caproic acid, enanthic acid, caprylic acid, pelargonic acid, capric acid, and lauric acid, and examples of long-chain fatty acids include myristic acid, pentadecylic acid, palmitic acid, palmitoleic acid, margaric acid, stearic acid, oleic acid, vaccenic acid, linoleic acid, linolenic acid, arachidic acid, arachidonic acid, behenic acid, lignoceric acid, nervonic acid, cerotic acid, montanic acid, and melissic acid.

[0040] Examples of binders include cellulose derivatives such as methyl cellulose, ethyl cellulose, hydroxypropyl cellulose, and hydroxypropylmethyl cellulose, polyvinylpyrrolidone, polyvinyl alcohol, acrylic acid polymers, gelatin, gum arabic, pullulan, pregelatinized starch, agar, tragacanth, sodium alginate, and propylene glycol alginate.

[0041] Among these, the additives are preferably, but not limited to, a combination of sugar alcohol, fat, binder, and / or flavoring.

[0042] [Absorption composition of ascorbic acid or its salt] One aspect of the present invention relates to (A) a composition for absorbing ascorbic acid or a salt thereof, containing Centella asiatica and / or an extract thereof. The content of Centella asiatica and / or an extract thereof in the composition for absorbing ascorbic acid or a salt thereof is not limited, and can be, for example, 1% by mass or more, 10% by mass or more, 50% by mass or more, 60% by mass or more, or 70% by mass or more. The content of Centella asiatica and / or an extract thereof in the composition for absorbing ascorbic acid or a salt thereof is preferably 100% by mass or less, more preferably 90% by mass or less, and even more preferably 80% by mass or less. The content of the components and other conditions can be similar to those described under [Composition].

[0043] Another aspect of the present invention relates to a composition for absorbing ascorbic acid or a salt thereof, which contains (A) Centella asiatica and / or an extract thereof and (B) at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid. Specifically, the presence of (A) Centella asiatica and / or an extract thereof and (B) at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid improves the absorption of ascorbic acid in the composition compared to the absence of Centella asiatica and / or an extract thereof. The content of each component and other conditions are the same as those described under "Oral Composition."

[0044] [Absorption enhancer of ascorbic acid or its salts] One aspect of the present invention relates to an absorption enhancer for ascorbic acid or a salt thereof, which contains Centella asiatica and / or an extract thereof. The absorption enhancer for ascorbic acid or a salt thereof of the present invention has the effect of promoting the absorption of ascorbic acid or a salt thereof and increasing the amount or rate of absorption when used in combination with ascorbic acid or a salt thereof.

[0045] Here, the content of Centella asiatica and / or an extract thereof relative to the absorption enhancer of ascorbic acid or a salt thereof is not limited, and when used as a raw material for foods or supplements, for example, it can be 1% by mass or more, 10% by mass or more, 50% by mass or more, 60% by mass or more, or 70% by mass or more. The content of Centella asiatica and / or an extract thereof relative to the absorption enhancer of ascorbic acid or a salt thereof is preferably 100% by mass or less, more preferably 90% by mass or less, and even more preferably 80% by mass or less.

[0046] The daily intake of Centella asiatica or its extract should conform to the content described in [Oral Composition].

[0047] When Centella asiatica and / or an extract thereof is present together with ascorbic acid or a salt thereof in the absorption enhancer of ascorbic acid or a salt thereof of the present invention, the contents of each component and other conditions are the same as those described in [Oral composition].

[0048] The absorption enhancer for ascorbic acid or a salt thereof can also be formulated as an oral composition as is.

[0049] [Cell permeation enhancer of ascorbic acid or its salt] Another aspect of the present invention relates to a cell permeation enhancer for ascorbic acid or a salt thereof, containing Centella asiatica and / or an extract thereof as an active ingredient. The cell permeation enhancer for ascorbic acid or a salt thereof of the present invention has the effect of improving the cell permeability of ascorbic acid or a salt thereof when coexisting with ascorbic acid or a salt thereof, thereby increasing the amount or rate of permeation into cells. Here, the cells refer to, but are not limited to, intestinal cells, for example. Therefore, the cell permeation enhancer for ascorbic acid or a salt thereof of the present invention can increase the amount, rate, or rate of absorption of ascorbic acid or a salt thereof in the digestive tract.

[0050] The content of Centella asiatica and / or an extract thereof relative to the cell permeation enhancer of ascorbic acid or a salt thereof is not limited, and when used as a raw material for foods or supplements, it can be 50% by mass or more, 60% by mass or more, or 70% by mass or more. The content of Centella asiatica and / or an extract thereof relative to the absorption enhancer of ascorbic acid or a salt thereof is preferably 100% by mass or less, more preferably 90% by mass or less, and even more preferably 80% by mass or less.

[0051] The daily intake of Centella asiatica or its extract is as described in [Composition].

[0052] When Centella asiatica and / or an extract thereof is present together with ascorbic acid or a salt thereof in the cell permeation enhancer of ascorbic acid or a salt thereof of the present invention, the contents of each component and other conditions are in accordance with those described in [Composition].

[0053] The cell permeation enhancer of ascorbic acid or a salt thereof can also be formulated as an oral composition as is.

[0054] [Manufacturing method] The method for producing the composition or agent of the present invention is not particularly limited, and any known method can be used. Specifically, a method in which the components are stirred while being heated as necessary to dissolve or disperse them, mixed, stirred while being cooled, and then allowed to stand at room temperature can be mentioned, but the method is not particularly limited thereto.

[0055] [Form of formulation] The oral composition or agent of the present invention may be an oral preparation suitable for oral administration. The absorption enhancer and cell permeation enhancer for ascorbic acid or a salt thereof may be an oral composition itself, or may be used as a raw material for an oral composition. The form of the oral composition or agent is not particularly limited, and examples include solid preparations such as tablets (including orally disintegrating tablets, chewable tablets, lozenges, etc.), granules, powders, soft capsules, hard capsules, lozenges, and jellies, or liquid preparations (including suspensions, emulsions, syrups, etc.). Among these, from the viewpoint of ease of handling and further enhancing the effects of the present invention, solid preparations are preferred, and tablets or granules are more preferred.

[0056] [Use and dosage] The oral composition or agent of the present invention can be used, for example, as an ingredient in pharmaceuticals, quasi-drugs, cosmetics, and food and beverages (drinks, foods). Furthermore, the oral composition or agent according to this embodiment can also be used, for example, as a food or an ingredient thereof, such as a specified health food, a nutrient-functional food, a food for the elderly, a special-use food, a food with functional claims, a health supplement (supplement), or a food preparation (e.g., confectionery tablets), in addition to pharmaceutical preparations and quasi-drug preparations.

[0057] When the oral composition or agent of the present invention is used as a food or beverage, the food may be a general food containing component (A) alone, a combination of components (A) and (B), or components (A) and (B) and, if necessary, other components. Examples of such foods and beverages include solid foods such as cookies, biscuits, snacks, jellies, gummies, chocolates, chewing gum, candies, and cheese; and liquid foods such as nutritional drinks, juices, tea drinks, coffee drinks, and dairy drinks.

[0058] The amount of the oral composition of the present invention to be incorporated into pharmaceutical preparations, quasi-drug preparations, foods for specified health uses, foods with nutrient function claims, foods for the elderly, foods for special dietary uses, foods with functional claims, health supplements (supplements), and food preparations (e.g., confectionery tablets) is not particularly limited, but the daily dose of the composition of the present invention for an adult can be, for example, 0.01 to 500 g, preferably 0.1 to 100 g, more preferably 0.5 to 50 g, and most preferably 1 to 10 g.

[0059] The oral composition of the present invention can be stored and / or sold in a known container (packaging material) in an amount to be administered for, but not limited to, one week or more, 10 days or more, 14 days or more, 20 days or more, or 30 days or more. [Example]

[0060] Next, the present invention will be specifically explained using examples and test examples, but the present invention is not limited to the following examples and test examples. The unit of the amount of each component in the tables is mass % unless otherwise specified. The following reagents were used: Ascorbic acid (product name: L-ascorbic acid: Tokyo Chemical Industry Co., Ltd.) Centella asiatica extract (product name: Centevita, Indena Japan Co., Ltd.) Ao Mikan Extract (Product Name: Ao Mikan Extract PSW: Nikken Food Co., Ltd.) Caco-2 (DSP ECACC cells)

[0061] [Test Example 1. Permeability Test] Compositions of Examples and Comparative Examples having the formulations shown in Table 1 below were prepared. For each of these compositions, the permeability of ascorbic acid into cells was examined using Caco-2 cells, a human small intestine-like cell line.

[0062] Caco-2 cells were placed in the upper layer (chamber) of a Transwell (Transwell®, 24-well, pore size: 5 μm, Corning, product number 3421) insert at 2.0 × 10 5A suspension of 500 μL of medium was seeded at 16 cells / well. 1.5 mL of the same medium was added to the lower layer, and pre-culture was carried out for 2 weeks. During the culture period, the medium was changed every 2-3 days.

[0063] After 2 weeks of culture, the media in the upper and lower layers were completely removed, 500 μl of media containing each composition was added to the upper layer, and 1.5 ml of the same medium as in the pre-culture was added to the lower layer, followed by culture at 37°C and 5% CO. Simultaneously, media containing each composition (hereinafter referred to as blanks) were also cultured at 37°C and 5% CO.

[0064] After 24 hours, the upper and lower layers of the medium were collected and the remaining amount of ascorbic acid in the medium was quantified using HPLC. The ascorbic acid concentration in each blank was also quantified, and the resulting concentration was used as the average concentration in the medium for each test example. The medium used in the test was DMEM (ThermoFisher, product number 11995065) supplemented with 10% FBS.

[0065] The rate of increase in ascorbic acid permeability was calculated as follows: Transmittance (%) = average concentration of ascorbic acid in the lower layer (μg / mL) × [{volume of lower layer (μL) / volume of upper layer (μL)} / average concentration in the medium (μg / mL)] × 100 Transmittance improvement rate (%) = (transmittance of each test example / transmittance of reference example) × 100 The results are shown in Table 1.

[0066] [Table 1] In the composition of the example containing ascorbic acid and Centella asiatica extract (Centevita), the cell permeability of ascorbic acid was improved compared to the formulation containing ascorbic acid alone (Reference Example 1).

[0067] In the comparative composition containing ascorbic acid and Citrus unshiu extract, the cell permeability of ascorbic acid was reduced compared to the formulation containing ascorbic acid alone (Reference Example 1).

Claims

1. An oral composition comprising (A) Centella asiatica and / or an extract thereof and (B) ascorbic acid or a salt thereof.

2. The composition for oral administration according to claim 1, wherein the total content of the component (B) is 10 to 1,000 parts by mass per part by mass of the component (A).

3. An agent for enhancing absorption of ascorbic acid or a salt thereof, comprising Centella asiatica and / or an extract thereof as an active ingredient.

4. A cell permeation enhancer for ascorbic acid or its salts, comprising Centella asiatica and / or an extract thereof as an active ingredient.

5. The agent according to claim 3 or 4, which is an oral composition.

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