Oral composition

A gallic acid and ellagic acid oral composition with a specific ratio addresses the need for effective anti-obesity and diabetes prevention by inhibiting lipase and isomaltase, offering a taste-friendly solution to suppress fat and sugar absorption and glucose rise.

JP2026083809AActive Publication Date: 2026-05-20TOYO SHINYAKU KK
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
TOYO SHINYAKU KK
Filing Date
2024-11-08
Publication Date
2026-05-20

AI Technical Summary

Technical Problem

There is a demand for oral compositions that effectively inhibit fat absorption, triglyceride elevation, sugar absorption, and blood glucose rise to combat obesity and diabetes without the unpleasant taste associated with certain plant-derived ingredients.

Method used

An oral composition containing gallic acid and ellagic acid in a specific mass ratio of 1:0.01 to 0.7, optionally with chebulic acid and catechins, to inhibit lipase and isomaltase activities, thereby reducing fat and sugar absorption and blood glucose levels.

Benefits of technology

The composition effectively inhibits fat and sugar absorption, reduces body fat, and lowers BMI by suppressing triglyceride and glucose rises, providing a tasty alternative to plant-derived ingredients.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide an oral composition that can be used for anti-obesity, inhibiting fat absorption, suppressing the rise in triglycerides, inhibiting sugar absorption, suppressing the rise in blood glucose levels, reducing body fat, or reducing BMI. [Solution] An oral composition containing gallic acid and ellagic acid, wherein the mass ratio of gallic acid to ellagic acid in the composition is gallic acid:ellagic acid = 1:0.01 to 0.7. It is preferable to use it for one or more applications selected from anti-obesity, inhibition of fat absorption, inhibition of triglyceride increase, inhibition of sugar absorption, inhibition of blood glucose increase, reduction of body fat, and reduction of BMI. It is preferable that the oral composition further contains chebulic acid.
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Description

Technical Field

[0001] The present invention relates to oral compositions and food and drink products.

Background Art

[0002] In recent years, in the lives of Japanese people, while the overall amount of physical activity has tended to decline, the energy intake from diet has shown a relatively excessive tendency, and there are concerns about the impact on health. Diabetes and obesity are considered to be deeply involved in the onset of such lifestyles. Diabetes and obesity were once thought to develop due to aging, but in recent years, the onset in young people has become prominent, and subsequent investigations have revealed that lifestyles are deeply involved. Since diabetes and obesity can lead to more serious diseases such as arteriosclerosis and cancer, it is required to prevent or improve diabetes and obesity in daily diet.

[0003] Means for preventing diabetes and obesity include suppressing an increase in blood glucose and an increase in neutral fat in the blood. To suppress an increase in blood glucose level, it is effective to inhibit the action of disaccharidase present in the digestive tract mucosa and suppress the production of glucose. Inhibition of this disaccharidase can achieve suppression of an increase in blood glucose level and suppression of intestinal absorption of sugar, leading to reduction of body fat, reduction of anti-obesity, and reduction of BMI. In addition, to suppress blood neutral fat, a measure of suppressing the production of free fatty acids by inhibiting pancreatic lipase can be mentioned. As a result, the absorption of neutral fat in the intestinal tract and thus in the body is suppressed, so the amount of blood neutral fat is suppressed, leading to suppression of an increase in neutral fat, reduction of body fat, reduction of anti-obesity, and reduction of BMI. For example, Patent Document 1 describes that the pericarp of plants of the Lardizabalaceae family exhibits an anti-obesity effect and an effect of suppressing an increase in neutral fat by its lipase inhibitory action. However, there are consumers who do not like the taste of the pericarp of plants of the Lardizabalaceae family. Therefore, there has been a demand for the development of new oral compositions that exhibit effects such as an anti-obesity effect and suppression of an increase in neutral fat.

Prior Art Documents

[0004] [Patent Document 1] Japanese Patent Publication No. 2010-265182 [Overview of the project] [Problems that the invention aims to solve]

[0005] The present invention aims to provide a novel oral composition that exhibits anti-obesity effects, inhibits fat absorption, inhibits the rise in triglycerides, inhibits sugar absorption, inhibits the rise in blood glucose levels, reduces body fat, or reduces BMI. [Means for solving the problem]

[0006] The inventors have discovered that, in a composition containing gallic acid and ellagic acid, by setting the mass ratio of gallic acid to ellagic acid within a specific range, it is possible to obtain an oral composition that is remarkably effective in anti-obesity, inhibiting fat absorption, inhibiting the rise of triglycerides, inhibiting sugar absorption, inhibiting the rise of blood glucose levels, reducing body fat, or reducing BMI.

[0007] In other words, the present invention provides an oral composition containing gallic acid and ellagic acid, wherein the mass ratio of gallic acid to ellagic acid in the composition is gallic acid:ellagic acid = 1:0.01 to 0.7. [Effects of the Invention]

[0008] According to the present invention, it is possible to provide oral compositions containing gallic acid and ellagic acid, and in particular, oral compositions such as foods and beverages that have isomaltase inhibitory activity and lipase inhibitory activity and are effective for anti-obesity, suppression of fat absorption, suppression of the rise in triglycerides, suppression of sugar absorption, suppression of the rise in blood glucose levels, reduction of body fat, or reduction of BMI. [Modes for carrying out the invention]

[0009] The following describes preferred embodiments of the oral composition of the present invention. The oral composition of the present invention contains gallic acid as an active ingredient and has functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI.

[0010] 1. gallic acid The gallic acid used in this invention is a compound represented by C7H6O5 and is also called 3,4,5-trihydroxybenzoic acid. Gallic acid is known to have effects such as anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, and reduction of BMI, and functions as an active ingredient in the composition of this invention. The gallic acid used in this invention is not particularly limited as long as it can be used as a food product, and plant-derived gallic acid or synthetically obtained gallic acid can be used. When plant-derived gallic acid is used in the composition of this invention, plant extracts or pulverized powders may be used as the source of gallic acid, or purified products thereof may be used. Pulverized powder refers to powder obtained by drying and pulverizing plants. When plant-derived gallic acid is used, examples of the plants from which it may be derived include green tea, date palm, and persimmon. Furthermore, the gallic acid used in this invention may be an anhydrous form or a hydrate such as a monohydrate. Gallic acid may also be in the form of a salt. In the present invention, when a salt of gallic acid is used, examples of the salt of gallic acid include alkali metal salts. In the present invention, when gallic acid is a hydrate, the amount of gallic acid as referred to herein is on an anhydrous basis. In the present invention, when a salt is used as gallic acid, the amount of gallic acid means the amount on an anhydrous basis.

[0011] The proportion of gallic acid in the oral composition of the present invention is preferably 0.001% to 96% by mass, more preferably 0.001% to 90% by mass, even more preferably 0.005% to 87% by mass, and particularly preferably 0.01% to 84% by mass, of the solid content of the composition, from the viewpoint of further enhancing the functions of gallic acid related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat or BMI, and from the viewpoint of taste when taken orally. In this specification, solid content refers to the content in the composition if the composition is in solid form, and the total amount of all components excluding water in the composition if the composition is in liquid or fluid form.

[0012] The amount of gallic acid in the composition of the present invention can be measured by HPLC. For example, using a Unison UK-C18 (HT 3μm φ3×100mm) manufactured by Imtakt Corporation, a 1% formic acid aqueous solution can be used as the mobile phase liquid medium, and a 1% formic acid acetonitrile solution can be used as the mobile phase liquid medium, with a column temperature of 45°C and a flow rate of 0.7 ml / min. The gradient conditions can be as follows. When measuring, appropriate treatment may be performed as needed, such as removing impurities from the sample to match the separation capacity of the instrument.

[0013] [Table A]

[0014] Column: Imtakt Unison UK-C18 HT 3μm φ3×100 mm Column temperature: 45℃ Injection volume: 2μL Flow rate: 0.7 mL / min Measurement wavelength: 276 nm Mobile phase A solution: 1% formic acid aqueous solution Mobile phase B: 1% formate acetonitrile solution

[0015] 2. Ellagic acid The composition of the present invention contains ellagic acid. Ellagic acid is a kind of natural phenolic compound and is represented by C 14 H6O8. The ellagic acid used in the present invention is not particularly limited as long as it can be used as a food, and ellagic acid derived from plants or those obtained by synthesis can be used. When using ellagic acid derived from plants in the composition of the present invention, as the ellagic acid source, plant extracts or pulverized powders may be used, or purified products thereof may be used. When using ellagic acid derived from plants, examples of the plant from which it is derived include strawberries, raspberries, pomegranates, etc. Also, the ellagic acid used in the present invention may be an anhydride or a hydrate such as a monohydrate. Further, ellagic acid may be in the form of a salt. When using a salt of ellagic acid in the present invention, an alkali metal salt of ellagic acid can be mentioned. In the present invention, when ellagic acid is a hydrate, the amount of ellagic acid referred to in this specification is converted to the anhydride. In the present invention, when using a salt as ellagic acid, the amount of ellagic acid is the amount in terms of ellagic acid.

[0016] In the present invention, the inventor believes that ellagic acid is an auxiliary component that enhances the effect of gallic acid. In order to exert the effects of both components, it is necessary to make the mass ratio of gallic acid to ellagic acid in the composition of the present invention gallic acid:ellagic acid = 1:0.01 to 0.7. As shown in the examples described later, in the present invention, compared with the case of combining gallic acid without containing ellagic acid and components other than ellagic acid (for example, ascorbic acid, erythorbic acid), the function of gallic acid can be effectively enhanced by using ellagic acid. Also, in the present invention, compared with the case where the mass ratio of gallic acid to ellagic acid is outside the range of gallic acid:ellagic acid = 1:0.01 to 0.7, the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglycerides, suppression of sugar absorption, suppression of blood sugar level increase, reduction of body fat or reduction of BMI can be effectively enhanced by setting the ratio within the range.

[0017] In the present invention, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglycerides, suppression of sugar absorption, suppression of increase in blood glucose level, reduction of body fat or reduction of BMI, the mass ratio of gallic acid to ellagic acid in the composition is preferably gallic acid:ellagic acid = 1:0.03 to 0.5, more preferably 1:0.06 to 0.4, still more preferably gallic acid:ellagic acid = 1:0.07 to 0.3, particularly preferably gallic acid:ellagic acid = 1:0.08 to 0.25, and especially preferably gallic acid:ellagic acid = 1:0.1 to 0.2.

[0018] From the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglycerides, suppression of sugar absorption, suppression of increase in blood glucose level, reduction of body fat or reduction of BMI, the proportion of ellagic acid in the oral composition of the present invention is preferably 0.00001% by mass or more and 40% by mass or less, more preferably 0.00005% by mass or more and 30% by mass or less, and still more preferably 0.0001% by mass or more and 25% by mass or less in the solid content of the oral composition on the condition that the mass ratio of gallic acid to ellagic acid is within the above range.

[0019] The amounts of gallic acid and ellagic acid in the composition of the present invention can be measured by HPLC method. For example, using Unison UK-C18 (HT 3μm φ3×100mm) manufactured by Imtakt Corporation, as the liquid medium of the mobile phase, 1% aqueous formic acid solution is used for mobile phase A and 1% formic acid acetonitrile solution is used for mobile phase B, the column temperature can be 45°C, and the flow rate can be 0.7 mL / min. The gradient conditions can be as follows. In addition, when measuring, appropriate treatments such as removing impurities in the sample may be performed as necessary to adapt to the separation ability of the apparatus.

[0020]

Table B

[0021] Column: Imtakt Unison UK-C18 HT 3μm φ3×100 mm Column temperature: 45℃ Injection volume: 2μL Flow rate: 0.7 mL / min Measurement wavelength: 276 nm Mobile phase A solution: 1% formic acid aqueous solution Mobile phase B: 1% formate acetonitrile solution

[0022] 3. Chebulic acid From the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI, the oral composition of the present invention preferably further contains chebulic acid. Chebulic acid has the molecular formula: C 14 H 12 O 11 It is a compound represented by the following. As chebraic acid, those having the following chemical structure (1) are known. The chebraic acid used in the present invention is not particularly limited as long as it can be used as a food, and plant-derived chebraic acid or synthetically obtained chebraic acid can be used. When plant-derived chebraic acid is used in the composition of the present invention, plant extracts or pulverized powders may be used as the chebraic acid source, or purified products thereof may be used. When the composition of the present invention contains chebraic acid, the inventors believe that chebraic acid acts as an auxiliary component that enhances the effect of gallic acid. Chebraic acid may be an anhydrous or a hydrate. Chebraic acid may also be in the form of a salt. When a salt of chebraic acid is used in the present invention, alkali metal chebraic acid salts are mentioned. In the present invention, when chebraic acid is a hydrate, the amount of chebraic acid referred to herein is on an anhydrous basis. In the present invention, when a salt is used as chebraic acid, the amount of chebraic acid is on a chebraic acid basis.

[0023] [ka]

[0024] When the oral composition of the present invention contains chebula acid, the amount of chebula acid is not limited, but from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI, it is preferable to contain 0.01 parts by mass or more of chebula acid per 1 part by mass of gallic acid, more preferably 0.02 parts by mass or more, even more preferably 0.05 parts by mass or more, and particularly preferable 0.1 parts by mass or more. Furthermore, the oral composition of the present invention preferably contains 5 parts by mass or less of chebula acid per 1 part by mass of gallic acid, more preferably 3 parts by mass or less, even more preferably 2 parts by mass or less, and particularly preferably 1 part by mass or less.

[0025] When the oral composition of the present invention contains chebula acid, from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI, it is preferable that the composition contains 0.01 parts by mass or more of chebula acid per 1 part by mass of the total of gallic acid and ellagic acid, more preferably 0.02 parts by mass or more, even more preferably 0.05 parts by mass or more, and particularly preferably 0.1 parts by mass or more. Furthermore, the oral composition of the present invention preferably contains 5 parts by mass or less of chebula acid per 1 part by mass of the total of gallic acid and ellagic acid, more preferably 3 parts by mass or less, even more preferably 2 parts by mass or less, and particularly preferably 1 part by mass or less.

[0026] When the oral composition of the present invention contains chebulic acid, from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI, it is preferable that the amount of chebulic acid in the solid content of the oral composition be 0.00001% by mass or more and 40% by mass or less, more preferably 0.00005% by mass or more and 30% by mass or less, and even more preferably 0.0001% by mass or more and 25% by mass or less.

[0027] The amount of chebula acid in the composition of the present invention can be measured by LCMS. For example, using a Unison UK-C18 (HT 3μm φ3×100 mm) manufactured by Imtakt Corporation, a 0.1% formic acid aqueous solution can be used as the mobile phase A, and acetonitrile as the mobile phase B. The column temperature can be 45°C and the flow rate 0.7 mL / min. The ionization method can be electrospray, and the ionization mode can be negative. The gradient conditions can be as follows. When measuring, appropriate treatment may be performed as needed, such as removing impurities from the sample to match the separation capacity of the instrument.

[0028] [Table C]

[0029] Column: Imtakt Unison UK-C18 HT 3μm φ3×100 mm Column temperature: 45℃ Injection volume: 2μL Flow rate: 0.7 mL / min Ionization method: Electrospray Ionization mode: Negative Setting mass number (m / z): 355 Mobile phase A solution: 0.1% formic acid aqueous solution Mobile phase B: Acetonitrile

[0030] 4. Catechins From the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI, the composition of the present invention preferably further contains catechins. In this specification, "catechins" refers to non-gallate type catechins selected from the group consisting of catechin, gallocatechin, epicatechin, and epigallocatechin, and gallate type catechins selected from the group consisting of catechin gallate, gallocatechin gallate, epicatechin gallate, and epigallocatechin gallate. In this specification, the content of catechins means the total amount of the eight compounds described above. In the present invention, if the catechins are hydrates, the amount of catechins referred to in this specification is on an anhydrous basis.

[0031] While not limiting, in terms of functionality as an auxiliary component of gallic acid, the catechins used in this invention preferably have a ratio of non-gallate type catechin content C1 to gallate type catechin content C2 C1:C2 of 1:0.01 to 13, and more preferably 0.05 to 7. Furthermore, epigallocatechin gallate (EGCG) preferably accounts for 0.1 to 70% by mass of the catechins, and more preferably 0.5 to 60% by mass. The total amount of epigallocatechin (EGC) and epicatechin (EC) in the catechins preferably accounts for 20% by mass or more, and more preferably 30% by mass or more. The catechin (C) content of the catechins preferably accounts for 0.01 to 40% by mass, and more preferably 0.1 to 20% by mass.

[0032] The catechins used in this invention are not particularly limited as long as they can be used as food, and plant-derived catechins or those obtained by synthesis can be used. When plant-derived catechins are used in the composition of this invention, plant extracts or powders may be used as the catechin source, or purified products thereof may be used. Examples of plants from which catechins are derived include acacia catechu, green tea, cocoa beans, and apples. The inventors believe that when the composition of this invention contains catechins, the catechins act as auxiliary components that enhance the effect of gallic acid.

[0033] When the oral composition of the present invention contains catechins, there are no particular restrictions on the amount of catechins, but from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI, it is preferable to contain 0.01 parts by mass or more of catechins per 1 part by mass of gallic acid, more preferably 0.02 parts by mass or more, even more preferably 0.05 parts by mass or more, and particularly preferably 0.1 parts by mass or more. Furthermore, the oral composition of the present invention preferably contains 5 parts by mass or less of catechins per 1 part by mass of gallic acid, more preferably 3 parts by mass or less, even more preferably 2 parts by mass or less, and particularly preferably 1 part by mass or less.

[0034] When the oral composition of the present invention contains catechins, from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI, it is preferable that the composition contains 0.01 parts by mass or more of catechins per 1 part by mass of gallic acid and ellagic acid combined, more preferably 0.02 parts by mass or more, even more preferably 0.05 parts by mass or more, and particularly preferable 0.1 parts by mass or more. Furthermore, the oral composition of the present invention preferably contains 5 parts by mass or less of catechins per 1 part by mass of gallic acid and ellagic acid combined, more preferably 3 parts by mass or less, even more preferably 2 parts by mass or less, and particularly preferable 1 part by mass or less.

[0035] When the oral composition of the present invention contains catechins, from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI, it is preferable that the oral composition contains 0.001% by mass or more of catechins in its solid content, more preferably 0.005% by mass or more, and even more preferably 0.01% by mass or more. Furthermore, from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI, it is preferable that the oral composition contains 50% by mass or less of catechins in its solid content, more preferably 40% by mass or less, even more preferably 30% by mass or less, and particularly preferably 25% by mass or less.

[0036] From the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI, the oral composition of the present invention preferably contains at least chebulic acid in addition to gallic acid and ellagic acid, and more preferably contains chebulic acid and catechins.

[0037] The amount of catechins in the composition of the present invention can be measured by HPLC. For example, an L-Column ODS (3 μm φ4.6 × 250 mm) manufactured by the Chemicals Evaluation and Research Institute can be used, with 0.1 M aqueous acetic acid solution as mobile phase A and 0.1 M acetonitrile acetate solution as mobile phase B, with a column temperature of 40°C and a flow rate of 1.0 ml / min. The gradient conditions can be as follows. During measurement, appropriate treatment may be performed as needed, such as removing impurities from the sample to match the separation capacity of the instrument.

[0038] [Table D]

[0039] Column: L-Column ODS 3 μm, 4.6 × 250 mm (manufactured by the Chemicals Evaluation and Research Institute) Column temperature: 40℃ Injection volume: 10μL Flow rate: 1.0 mL / min Measurement wavelength: 280 nm Mobile phase A: 0.1 M aqueous acetic acid solution Mobile phase B: 0.1 M acetonitrile acetate solution

[0040] 5. Oral composition The oral composition of the present invention may contain other components besides gallic acid, ellagic acid, chebulic acid, and catechins, to the extent that they do not inhibit the expression of functions related to anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, or reduction of BMI. Examples of such other components include sugars, vitamins, minerals, proteins, dietary fiber such as insoluble dietary fiber, plants or plant products, and yeast. Furthermore, it may contain, if necessary, sweeteners, acidulants, colorants, thickeners, glazing agents, lubricants, excipients, anticaking agents, nutritional supplements, binders, lubricants, stabilizers, diluents, bulking agents, emulsifiers, food additives, seasonings, etc., which are commonly used in the food industry.

[0041] Examples of the oral composition of the present invention include tablets, capsules, powders, granules, liquids, granular preparations, rod-shaped preparations, plate-shaped preparations, block-shaped preparations, solid preparations, round preparations, paste-like preparations, cream-like preparations, caplet-like preparations, gel-like preparations, chewable preparations, stick-shaped preparations, and the like. Among these forms, tablets, capsules, powders, granules, and liquid preparations are preferred from the viewpoint of ease of administration.

[0042] The oral composition of the present invention can take the form of a pharmaceutical product (including quasi-drugs) or a food or beverage. Among these, a food or beverage is particularly preferred from the viewpoint of being easily consumed in daily life.

[0043] Examples of foods and beverages in this invention include general foods, foods with nutritional function claims, foods for specified health uses whose efficacy claims have been approved by designated institutions, and so-called health foods such as foods with functional claims. Foods that display efficacy claims are sometimes collectively referred to as "health functional foods" or "functional foods."

[0044] The present invention does not particularly limit the food and beverages, but examples include: milk and dairy products; beverages such as soft drinks, fruit juices, milk beverages, alcoholic beverages, sports drinks, and nutritional drinks; seasonings; alcoholic beverages; processed agricultural and forestry products; confectionery and bread; flour and noodles; processed marine products; processed livestock products; oils and fats; frozen prepared foods; retort foods; instant foods; food ingredients; and supplements. Examples of supplement forms include tablets, capsules, powders, granules, and liquids.

[0045] 6 Oral compositions used for purposes such as inhibiting fat absorption. As will be clear from the examples described later, the oral composition of the present invention can effectively inhibit intestinal isomaltase activity and lipase activity. As will be described later, isomaltase is an enzyme involved in sugar absorption, and lipase is an enzyme involved in fat absorption. Therefore, the oral composition of the present invention is suitably used for one or more of the following purposes: (1) suppression of fat absorption, (2) suppression of the rise in triglycerides, (3) suppression of sugar absorption, (4) suppression of the rise in blood glucose levels, (5) anti-obesity, (6) reduction of body fat, and (7) reduction of BMI (Body Mass Index). Body fat refers to fat in the body and is a general term for visceral fat and subcutaneous fat. In other words, the oral composition of the present invention can be used as (1) a composition for inhibiting fat absorption, (2) a composition for inhibiting the rise in triglycerides, (3) a composition for inhibiting sugar absorption, (4) a composition for inhibiting the rise in blood glucose levels, (5) an anti-obesity composition, (6) a composition for reducing body fat, or (7) a composition for reducing BMI (Body Mass Index).

[0046] (1) "Inhibition of fat absorption" refers to suppressing the amount of triglycerides ingested through food that are absorbed into the body. (2) "Suppression of triglyceride levels" means suppressing the rise in blood triglyceride levels after a meal or during fasting. (3) "Inhibition of sugar absorption" means suppressing the amount of sugar absorbed in the small intestine. (4) "Suppression of blood glucose levels" means suppressing the rise in blood glucose levels after a meal or when fasting. (5) "Anti-obesity" means reducing or suppressing weight gain, and preventing or improving the accumulation of fat in the body, and is a concept that includes diets for cosmetic purposes. (6) "Reduction of body fat" means reducing the amount of body fat (visceral fat and subcutaneous fat), specifically the amount of abdominal body fat (visceral fat and subcutaneous fat). (7) "BMI reduction" means reducing the BMI value. The mechanism by which the present invention achieves functions (1) to (7) is as follows:

[0047] Ingesting the oral composition of the present invention inhibits lipase activity in the body. Lipase (pancreatic lipase) is a digestive enzyme synthesized in the pancreas and secreted into pancreatic juice to hydrolyze triglycerides. Triglycerides in food are broken down by lipase into easily absorbed fatty acids and glycerol, which are then absorbed by the villous epithelial cells of the small intestine. The absorbed fatty acids and glycerol are then resynthesized into triglycerides and transferred into the bloodstream via the lymphatic system. As can be seen from the examples described later, ingesting the oral composition of the present invention inhibits lipase activity. Therefore, the breakdown of dietary triglycerides into fatty acids and glycerol is suppressed, reducing the amount of fatty acids and glycerol absorbed by the small intestinal villous epithelial cells, that is, (1) fat absorption is suppressed. Also, the amount of fatty acids and glycerol resynthesized into triglycerides is reduced, so (2) the rise in triglycerides is suppressed. As a result, (5) the accumulation of fat in the body is prevented (anti-obesity), and (6) body fat is reduced. With the reduction in body fat, weight decreases, and (7) BMI also decreases.

[0048] Furthermore, ingesting the oral composition of the present invention inhibits isomaltase activity in the body. Isomaltase is a type of α-glucosidase, a disaccharidase present in the small intestinal mucosa that breaks down disaccharides into monosaccharides. When sugars from food reach the small intestine, they are broken down by this enzyme into easily absorbable monosaccharides (such as glucose), absorbed through the small intestinal mucosa, transported to the liver, and then released into the bloodstream. When the concentration of glucose in the blood rises, insulin converts the glucose into triglycerides, which are then stored in fat cells. When isomaltase activity is inhibited, the breakdown of disaccharides into monosaccharides is suppressed, so the amount of easily absorbed monosaccharides decreases, and (3) the amount of sugar absorbed in the small intestine is suppressed. Also, since the amount of glucose absorbed in the small intestine after a meal decreases, (4) the rise in blood glucose levels is suppressed. When the rise in glucose concentration is suppressed, the conversion of glucose into triglycerides by insulin is suppressed, so (5) the accumulation of fat in the body is prevented or suppressed (anti-obesity), and (6) body fat is reduced. With the reduction in body fat, weight decreases, and (7) BMI also decreases.

[0049] Furthermore, the oral composition of the present invention can be suitably used for lipase inhibition, α-glucosidase inhibition, and isomaltase inhibition. That is, the oral composition of the present invention can be used as a lipase inhibitor, an α-glucosidase inhibitor, and an isomaltase inhibitor.

[0050] From the viewpoint of reliably obtaining anti-obesity function, fat absorption inhibition function, triglyceride elevation inhibition function, sugar absorption inhibition function, blood glucose elevation inhibition function, body fat reduction function, and BMI reduction function, the oral composition of the present invention preferably contains 10 to 100 mg of gallic acid per adult per day, and more preferably 20 to 80 mg. Furthermore, it is preferable to administer a total of 10 to 120 mg of gallic acid and ellagic acid, and more preferably 20 to 100 mg orally.

[0051] If the oral composition of the present invention is an oral composition used for any of the functions (1) to (7) described above, it is not particularly limited as long as it contains gallic acid and ellagic acid, the mass ratio of gallic acid to ellagic acid is set within a specific range, and it is distinguishable from other products in that it is used for any of the functions (1) to (7). For example, any product that displays any of the functions (1) to (7) on the main body, packaging, instructions, or promotional materials (advertising media) of the present invention is included within the scope of the present invention. The oral composition used for any of the functions (1) to (7) of the present invention may display gallic acid as the active ingredient, but is not limited to products that display gallic acid as the active ingredient on the packaging, etc. For example, it may not specify an active ingredient. Furthermore, even general foods that are manufactured and sold with indications of their use are included within the scope of the present invention. For example, foods that are sold with testimonials on a website, etc., mentioning the maintenance and / or improvement of any of the functions (1) to (7) as personal impressions of people who have consumed them are also included within the scope of the present invention. Furthermore, the scope of this invention also includes functional foods in which gallic acid is the functionally active ingredient, and which use papers or other documents demonstrating the maintenance and / or improvement of any of the functions (1) to (7) as the scientific basis for functionality, and which have a functional claim relating to any of the functions (1) to (7) as the notified functional claim. As stated above, in this invention, ingredients other than gallic acid are auxiliary ingredients to enhance the effect of gallic acid, and therefore are not usually listed as active ingredients in functional foods or foods for specified health uses that display any of the functions (1) to (7). However, the oral composition used for any of the functions (1) to (7) in this invention does not exclude those in which auxiliary ingredients such as ellagic acid or chebulic acid are listed as active ingredients, and functional foods that display ellagic acid, etc. as active ingredients are also included in this oral composition.

[0052] As described above, oral compositions used for any of the functions (1) to (7) include foods and beverages that are labeled as having one or more functions selected from anti-obesity function, fat absorption inhibition function, triglyceride elevation inhibition function, sugar absorption inhibition function, blood glucose elevation inhibition function, body fat reduction function, and BMI reduction function. The method of labeling is preferably in the form of (1) or (2) below.

[0053] (1) A label indicating that a food or beverage is a functional food, which has been registered with the Consumer Affairs Agency, under the responsibility of the business operator, on the product packaging, based on scientific evidence, that it has anti-obesity function, fat absorption inhibition function, triglyceride elevation inhibition function, sugar absorption inhibition function, blood glucose elevation inhibition function, and body fat reduction function and / or BMI reduction function. (2) A statement that the food or beverage is a Food for Specified Health Uses (FOSHU) which is permitted by the Consumer Affairs Agency to be displayed on the product packaging, based on scientific evidence, to indicate that it has the following functions: anti-obesity function, fat absorption inhibition function, triglyceride elevation inhibition function, sugar absorption inhibition function, blood glucose elevation inhibition function, and body fat reduction function and / or BMI reduction function.

[0054] For example, examples of the displays in (1) and (2) above include displays that appeal to people concerned about body fat, such as "For those concerned about obesity," "For those concerned about their waistline," "For those concerned about their weight," and "For those concerned about abdominal fat (visceral fat and subcutaneous fat, etc.)," ​​as well as displays that help to reduce weight, help to reduce abdominal fat (visceral fat and subcutaneous fat, etc.), help to reduce waist circumference, support for weight loss, support for dieting, make it easier to reduce fat, reduce fat absorption, help to suppress or reduce the increase of body fat, as well as displays that suppress the rise in blood sugar levels, suppress sugar absorption, moderate the rise in blood sugar levels, suppress the rise in postprandial blood sugar levels, moderate the rise in postprandial blood sugar levels, suppress the absorption of triglycerides, suppress the rise in triglycerides, moderate the rise in triglycerides, suppress the rise in postprandial triglycerides, and suppress the absorption of sugars and fats contained in food.

[0055] The present invention provides the following: <1> An oral composition containing gallic acid and ellagic acid, An oral composition in which the mass ratio of gallic acid to ellagic acid in the composition is gallic acid:ellagic acid = 0.01 to 0.7. <2> The above-mentioned product is used for one or more purposes selected from anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, and reduction of BMI. <1> The oral composition described above. <3> Furthermore, the above contains chebulic acid. <1> or <2> The oral composition described above. <4> Furthermore, the above-mentioned, which contains catechins <1> ~ <3> An oral composition according to at least one of the following, selected from: <5> The above-mentioned product is used for one or more purposes selected from the following: anti-obesity, inhibiting fat absorption, inhibiting the rise in triglycerides, inhibiting sugar absorption, inhibiting the rise in blood glucose levels, reducing body fat, and reducing BMI. <1> ~ <4> An oral composition according to at least one of the following, selected from: <6> The above-mentioned method for suppressing the rise in triglycerides after a meal or for suppressing the rise in blood glucose levels after a meal. <1> ~ <5> An oral composition according to at least one of the following, selected from: <7> The above is for lipase inhibition or α-glucosidase inhibition. <1> ~ <5> An oral composition according to at least one of the following, selected from: <8> An oral composition containing gallic acid as an active ingredient, Furthermore, it contains ellagic acid, The mass ratio of gallic acid to ellagic acid in the above composition is gallic acid:ellagic acid = 0.01 to 0.7. An oral composition used for one or more purposes selected from among anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, and reduction of BMI. <9> Food and beverages containing gallic acid as an active ingredient, Furthermore, it contains ellagic acid, The mass ratio of gallic acid to ellagic acid in the aforementioned food and beverage is gallic acid:ellagic acid = 1:0.01~0.7. Food and beverages that are labeled as having one or more functions selected from the following: anti-obesity function, fat absorption inhibition function, triglyceride elevation inhibition function, sugar absorption inhibition function, blood glucose elevation inhibition function, body fat reduction function, and BMI reduction function. <10> The above is a functional food or a food for specified health uses. <9> Food and beverages listed above. [Examples]

[0056] The present invention will be described below based on examples. However, the present invention is not limited to the following examples. Unless otherwise specified, "parts" below refers to "parts by mass" and "%" refers to "percentage by mass".

[0057] In the examples and comparative examples, gallic acid was used as a reagent for gallic acid (anhydrous, powder, purity approximately 100% by mass). Ellagic acid was used as a reagent for ellagic acid (anhydrous, powder, purity approximately 98% by mass or higher). Chebula acid was used as anhydrous, powder, purity 98% by mass or higher. Catechins were used as purified catechins derived from tea. Ascorbic acid was used, and sodium erythorbate (monohydrate) was used as the substitute for ascorbic acid.

[0058] [Examples 1-9 and Comparative Examples 1-10] The test substances for Examples 1-9 and Comparative Examples 1-10 were prepared using the raw materials listed in Tables 1 and 2. When multiple raw materials were used, the test substances were prepared by mixing the multiple raw materials. The amounts of raw materials used are shown in Tables 1 and 2.

[0059] The following isomaltase inhibition tests were performed on the test substances of Examples 1-9 and Comparative Examples 1-10.

[0060] <Isomaltase Inhibition Test> (1) 100 mg of rat intestinal acetone powder (SIGMA) was mixed with 900 μL of 56 mM maleate buffer (pH 6.0) and homogenized to prepare a mixture. The prepared mixture was centrifuged (3000 rpm, 10 minutes, 4°C), and the supernatant was collected. The collected supernatant was diluted 2-fold with 56 mM maleate buffer (pH 6.0) to prepare the enzyme solution. (2) A substrate solution was prepared by dissolving isomaltose in 56 mM maleate buffer (pH 6.0) to a concentration of 5 mM. (3) The test substance was dissolved in a 10% DMSO solution so that the total amount of the test substance was 0.32 mg / mL to prepare the test substance solution. (4) 15 μL of enzyme solution was added to 15 μL of test substance solution, and pre-incubated at 37°C for 5 minutes. Then, 90 μL of substrate solution was added and incubated at 37°C for 30 minutes to allow the reaction to proceed. (5) After the reaction, the sample was treated at 98°C for 2 minutes to stop the enzymatic reaction. (6) After the reaction was stopped, the absorbance at 505 nm was measured using a glucose tester (Wako Pure Chemical Industries, Ltd.) to determine the isomaltase inhibitory activity of the test substance. The measured value was designated as Measured Value A. (7) Except for using a 10% DMSO solution instead of the test substance solution, the procedure for measuring isomaltase inhibitory activity was carried out in the same manner as described above, and the absorbance of the test solution was measured to obtain the measurement value B. (8) Except for using an enzyme solution that had been inactivated by heat treatment at 98°C for 2 minutes instead of the enzyme solution, the procedure was the same as described above for measuring isomaltase inhibitory activity, and the absorbance of the test solution was measured to obtain the measured value C. (9) The procedure was carried out in the same manner as described above for activity measurement, except that a 10% DMSO solution was used instead of the test substance solution, and an enzyme solution that had been inactivated by heat treatment at 98°C for 2 minutes was used instead of the enzyme solution. The absorbance of the test solution was measured, and the measured value D was obtained. (10) The isomaltase inhibition rate (% of control) was calculated from measurement values ​​A, B, C, and D using the following formula (1). The results are shown in Tables 1 and 2. Isomaltase inhibition rate (% of control) = (Measurement A - Measurement C) / (Measurement B - Measurement D) × 100 (1)

[0061] [Table 1]

[0062] [Table 2]

[0063] As is clear from Tables 1 and 2, Examples 1 to 9, in which the ratio of gallic acid to ellagic acid was in the range of gallic acid:ellagic acid = 1:0.01 to 0.7, showed significantly higher isomaltase inhibition rates compared to Comparative Examples 1 to 6, in which each was used individually. As a result of this improvement effect, the breakdown of disaccharides into monosaccharides is suppressed, and therefore, the effects of suppressing sugar absorption, suppressing the rise in blood glucose levels, anti-obesity, body fat reduction, and BMI reduction are expected to be effectively achieved. Such excellent effects were not observed in Comparative Examples 7 to 9, in which gallic acid was used in combination with antioxidant components other than ellagic acid, and in Comparative Example 10, in which the gallic acid and ellagic acid content was outside the range of the present invention. In particular, among Examples 1 to 6, the isomaltase inhibition rate differed depending on the gallic acid:ellagic acid ratio, indicating that there is a preferred range for gallic acid:ellagic acid to increase the isomaltase inhibition rate.

[0064] Furthermore, in Examples 7 and 8, which used chebula acid in combination with gallic acid and ellagic acid, the mass ratio of ellagic acid to 1 part by mass of gallic acid was the same as in Examples 3 and 4, but the isomaltase inhibition rate was even higher in each case compared to Examples 3 and 4, which did not contain chebula acid. Therefore, it was found that in Examples 7 and 8, the combination of chebula acid with gallic acid and ellagic acid significantly and effectively inhibits intestinal isomaltase activity. Consequently, it was suggested that this combination further suppresses the breakdown of disaccharides to monosaccharides in the intestinal tract, resulting in even more pronounced effects such as inhibition of sugar absorption, suppression of blood glucose elevation, anti-obesity, reduction of body fat, and reduction of BMI.

[0065] Furthermore, in Example 9, which used gallic acid and ellagic acid in combination with chebulic acid and catechins, the mass ratio of ellagic acid and chebulic acid to 1 part by mass of gallic acid was the same as in Example 7, but the isomaltase inhibition rate was even higher than in Example 7, which did not contain catechins. Therefore, it was suggested that this combination further suppresses the breakdown of disaccharides to monosaccharides in the intestinal tract, resulting in even more pronounced effects such as inhibition of sugar absorption, suppression of blood glucose elevation, anti-obesity, reduction of body fat, and reduction of BMI.

[0066] [Examples 10-16 and Comparative Examples 11-20] The test substances for Examples 10-16 and Comparative Examples 11-20 were prepared using the raw materials listed in Tables 3 and 4. When multiple raw materials were used, the test substances were prepared by mixing the multiple raw materials. The amounts of raw materials used are shown in Tables 3 and 4.

[0067] The following lipase inhibition tests were performed on the test substances of Examples 10-16 and Comparative Examples 11-20.

[0068] <Lipase inhibitory activity test> The lipase inhibitory activity was measured according to the method for Lipase Kit S (manufactured by Sumitomo Bakelite Co., Ltd.). Specifically, the lipase inhibitory activity of the test substance was measured using the following procedure. The substrate of Lipase Kit S is known to have high reactivity with pancreatic lipase. (1) Porcine pancreatic lipase (manufactured by SIGMA) was dissolved in 0.01 M phosphate buffer (pH 7.0) to prepare a 0.3 mg / mL lipase solution. For the inhibition test, a 0.06 mg / mL lipase solution was used, which was obtained by diluting this 0.3 mg / mL lipase solution fivefold with 0.01 M phosphate buffer (pH 7.0). (2) The test substance was dissolved in Tris-HCl buffer (pH 8.55) containing 2.5% DMSO to prepare a test substance solution, so that the total amount of the test substance was 0.264 mg / mL. (3) Mix 6 μL of the test substance solution, 80 μL of the color development solution from the kit contents, 10 μL of the lipase solution, and 1.6 μL of the esterase inhibitor solution, pre-incubate at 37°C for 5 minutes, then add 8 μL of the substrate solution from the kit contents and incubate for a further 30 minutes at 37°C. (4) Subsequently, 160 μL of the reaction stop solution from the kit contents was added to the mixture and mixed. The absorbance at 412 nm was then measured to determine the lipase inhibitory activity, and the measured value A was obtained. (5) The procedure was the same as that for the lipase inhibitory activity measurement test described above, except that a 2.5% DMSO-containing Tris-HCl buffer (pH 8.55) was used instead of the test substance solution. The absorbance of the test solution was measured to obtain the measurement value B. (6) After adding the reaction stop solution, the procedure was carried out in the same manner as the lipase inhibitory activity measurement test described above, except that the substrate solution was added, and the absorbance of the test solution was measured to obtain the measured value C. (7) The procedure was carried out in the same manner as the lipase inhibitory activity measurement test described above, except that a 2.5% DMSO-containing Tris-HCl buffer (pH 8.55) was used instead of the test substance solution, and the substrate solution was added after the reaction stop solution was added. The absorbance of the test solution was measured, and the measured value D was obtained. (8) From the measured values ​​A, B, C, and D, the lipase inhibition rate (% of control) was calculated using the following formula (2). The results are shown in Tables 3 and 4. Lipase inhibition rate (% of control) = (Measurement A - Measurement C) / (Measurement B - Measurement D) × 100 (2)

[0069] [Table 3]

[0070] [Table 4]

[0071] As is clear from Tables 3 and 4, Examples 10 to 16, in which the ratio of gallic acid to ellagic acid was in the range of gallic acid:ellagic acid = 1:0.01 to 0.7, showed a significantly improved lipase inhibition rate compared to Comparative Examples 11 to 16, in which the raw materials were used individually. As a result of this improvement, the breakdown of triglycerides into fatty acids and glycerol is suppressed, and the absorption of fat into the body is suppressed. Therefore, it is expected that the effects of suppressing fat absorption, suppressing the rise of triglycerides, anti-obesity, reducing body fat, and reducing BMI will be improved. Such excellent effects were not observed in Comparative Examples 17 to 19, in which gallic acid was used in combination with antioxidant components other than ellagic acid, and in Comparative Example 20, in which the gallic acid to ellagic acid content ratio was outside the range of the present invention. In particular, among Examples 10 to 15, the lipase inhibition rate differed depending on the gallic acid:ellagic acid ratio, indicating that there is a preferred range for gallic acid:ellagic acid to increase the lipase inhibition rate.

[0072] In particular, in Example 16, which used chebulic acid in combination with gallic acid and ellagic acid, the mass ratio of ellagic acid to 1 part by mass of gallic acid was the same as in Example 12, but the lipase inhibition rates were even higher for each component compared to Example 12, which did not contain ellagic acid. Therefore, it was suggested that the aforementioned effects were even more pronounced with this combination.

[0073] [Examples 17-24] Each ingredient was mixed according to the proportions shown in Table 5, and tablets (for swallowing) with a tablet diameter of 8 mm and a dose of 250 mg per tablet were manufactured using a single-shot tablet press. The compression pressure was set to 3 kN. The resulting tablets, when taken at a rate of 2 tablets per day, exhibited anti-obesity effects, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, and reduction of BMI.

[0074] [Table 5]

Claims

1. An oral composition containing gallic acid and ellagic acid, An oral composition in which the mass ratio of gallic acid to ellagic acid in the composition is gallic acid:ellagic acid = 1:0.01 to 0.

7.

2. The oral composition according to claim 1, which is used for one or more purposes selected from anti-obesity, inhibition of fat absorption, inhibition of triglyceride elevation, inhibition of sugar absorption, inhibition of blood glucose elevation, reduction of body fat, and reduction of BMI.

3. The oral composition according to claim 1 or 2, further containing chebulic acid.

4. Food and beverages containing gallic acid as an active ingredient, Furthermore, it contains ellagic acid, The mass ratio of gallic acid to ellagic acid in the aforementioned food and beverage is gallic acid:ellagic acid = 1:0.01 to 0.

7. Food and beverages that are labeled as having one or more functions selected from the following: anti-obesity function, fat absorption inhibition function, triglyceride elevation inhibition function, sugar absorption inhibition function, blood glucose elevation inhibition function, body fat reduction function, and BMI reduction function.

5. Food and beverages containing gallic acid as an active ingredient, Furthermore, it contains ellagic acid and chebulic acid, The mass ratio of gallic acid to ellagic acid in the aforementioned food and beverage is gallic acid:ellagic acid = 1:0.01 to 0.

7. Food and beverages that are labeled as having one or more functions selected from the following: anti-obesity function, fat absorption inhibition function, triglyceride elevation inhibition function, sugar absorption inhibition function, blood glucose elevation inhibition function, body fat reduction function, and BMI reduction function.

6. Food or beverage according to claim 4 or 5, which is a functional food or a food for specified health uses.