Oral composition

The oral composition combining gallic acid and ellagic acid in a specific ratio addresses the need for effective anti-obesity and fat absorption inhibition, achieving significant body fat and BMI reduction through isomaltase and lipase inhibition.

JP7685801B1Active Publication Date: 2025-05-30TOYO SHINYAKU KK
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Patent Information

Application Number
JP2024195951
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Filing Date
2024-11-08
Publication Date
2025-05-30
Estimated Expiration
2044-11-08

AI Technical Summary

Technical Problem

There is a need for new oral compositions that effectively inhibit anti-obesity, fat absorption, triglyceride elevation, sugar absorption, blood glucose elevation, body fat reduction, and BMI reduction without the unpleasant taste of existing compounds like the pericarp of Lardizabalaceae plants.

Method used

An oral composition containing gallic acid and ellagic acid, with a specific mass ratio of gallic acid to ellagic acid ranging from 1:0.01 to 0.7, which provides isomaltase and lipase inhibitory actions, thereby offering anti-obesity and fat absorption inhibition effects.

Benefits of technology

The oral composition effectively inhibits isomaltase and lipase activities, leading to suppressed sugar and fat absorption, reduced body fat, and decreased BMI, while being palatable and effective in preventing or improving diabetes and obesity.

✦ 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, suppression of fat absorption, suppression of increase in triglyceride, suppression of sugar absorption, suppression of increase in blood glucose level, reduction of body fat or reduction of BMI. 【Solution means】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 preferably used for one or more uses selected from anti-obesity, suppression of fat absorption, suppression of increase in triglyceride, suppression of sugar absorption, suppression of increase in blood glucose level, reduction of body fat, and reduction of BMI. The oral composition preferably 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 level of physical activity has been showing a downward trend, the energy intake from diet has been relatively excessive, and there are concerns about its impact on health. Diabetes and obesity are considered to be deeply involved in the causes of such lifestyles. Diabetes and obesity were once thought to be caused by 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 disaccharide-degrading enzymes present in the digestive tract mucosa and suppress the production of glucose. Inhibition of this disaccharide-degrading enzyme 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 Lardizabalaceae plants 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 Lardizabalaceae plants. Therefore, there has been a demand for the development of new oral compositions that exhibit effects such as anti-obesity effects and suppression of an increase in neutral fat.

Prior Art Documents

Patent Document

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] An object of the present invention is to provide a new oral composition exhibiting anti-obesity, fat absorption inhibitory, triglyceride elevation inhibitory, sugar absorption inhibitory, blood glucose elevation inhibitory, body fat reduction or BMI reduction effects.

Means for Solving the Problems

[0006] The present inventors have surprisingly found 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, an oral composition excellent in functions related to anti-obesity, fat absorption inhibition, triglyceride elevation inhibition, sugar absorption inhibition, blood glucose elevation inhibition, body fat reduction or BMI reduction can be obtained.

[0007] That is, 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, an oral composition containing gallic acid and ellagic acid can be provided. In particular, it has an isomaltase inhibitory action and a lipase inhibitory action, and can provide an oral composition such as a food or drink effective for anti-obesity, fat absorption inhibition, triglyceride elevation inhibition, sugar absorption inhibition, blood glucose elevation inhibition, body fat reduction or BMI reduction.

Modes for Carrying Out the Invention

[0009] Hereinafter, preferred embodiments of the oral composition of the present invention will be described. The oral composition of the present invention contains gallic acid as an active ingredient for functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglycerides, suppression of sugar absorption, suppression of blood glucose level increase, reduction of body fat, or reduction of BMI.

[0010] 1. Gallic acid The gallic acid used in the present invention is a compound represented by C 7 H 6 O 5 and is also called 3,4,5-trihydroxybenzoic acid. Gallic acid is known to have effects such as anti-obesity, suppression of fat absorption, suppression of increase in triglycerides, suppression of sugar absorption, suppression of blood glucose level increase, reduction of body fat, and reduction of BMI, and functions as an active ingredient also in the composition of the present invention. The gallic acid used in the present invention is not particularly limited as long as it can be used as a food, and gallic acid derived from plants or those obtained by synthesis can be used. When using gallic acid derived from plants in the composition of the present invention, as the gallic acid source, plant extracts or pulverized powders may be used, or purified products thereof may be used. The pulverized powder refers to a powder obtained by drying and pulverizing a plant. When using gallic acid derived from plants, examples of the plant from which it is derived include green tea, coconut, persimmon, etc. Further, the gallic acid used in the present invention may be an anhydride or a hydrate such as a monohydrate. Gallic acid may be in the form of a salt. When using a salt of gallic acid in the present invention, 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 referred to in this specification is converted to the anhydride. In the present invention, when using a salt as gallic acid, the amount of gallic acid means the amount in terms of gallic acid conversion.

[0011] The proportion of gallic acid in the oral composition of the present invention is preferably 0.001% by mass or more and 96% by mass or less, more preferably 0.001% by mass or more and 90% by mass or less, still more preferably 0.005% by mass or more and 87% by mass or less, and particularly preferably 0.01% by mass or more and 84% by mass or less in the solid content of the composition, from the viewpoint of further enhancing the function of gallic acid related to anti-obesity, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of blood glucose level increase, reduction of body fat or reduction of BMI, and from the viewpoint of taste when orally ingested. In the present specification, when the composition is in a solid state, the solid content refers to the content in the composition, and when the composition is in a liquid or fluid state, the solid content refers to the total amount of all components excluding water in the composition.

[0012] The amount of gallic acid in the composition of the present invention can be measured by the 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% formic acid aqueous 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 device.

[0013]

Table A

[0014] Column: Imtakt Unison UK-C18 HT 3μm φ3×100 mm Column temperature: 45°C Injection volume: 2 μL Flow rate: 0.7 mL / min Measurement wavelength: 276 nm Mobile phase A: 1% formic acid aqueous solution Mobile phase B: 1% formic acid 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 H 6 O 8 . 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 ground 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 conversion.

[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 set the mass ratio of gallic acid to ellagic acid in the composition of the present invention as 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 ellagic acid with 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 glucose level increase, reduction of body fat or reduction of BMI can be effectively enhanced by setting it within the range of this ratio.

[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, 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-mentioned 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% formic acid aqueous solution for mobile phase A and 1% formic acid acetonitrile solution for mobile phase B can be used, 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 carried out as necessary to conform to the separation ability of the apparatus.

[0020]

Table B

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

[0022] 3. Chebulic acid 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 blood glucose level increase, 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 and is a compound represented by the formula. As chebulic acid, those having the following chemical structure (1) are known. The chebulic acid used in the present invention is not particularly limited as long as it can be used as a food, and plant-derived chebulic acid or those obtained by synthesis can be used. When plant-derived chebulic acid is used in the composition of the present invention, plant extracts or ground powders may be used as the chebulic acid source, or purified products thereof may be used. When the composition of the present invention contains chebulic acid, the inventor believes that chebulic acid serves as an auxiliary component that enhances the effect of gallic acid. Chebulic acid may be an anhydride or a hydrate. Also, chebulic acid may be in the form of a salt. When a salt of chebulic acid is used in the present invention, an alkali metal salt of chebulic acid can be mentioned. In the present invention, when chebulic acid is a hydrate, the amount of chebulic acid referred to in this specification is converted to the anhydride form. In the present invention, when a salt is used as chebulic acid, the amount of chebulic acid is the amount in terms of chebulic acid conversion.

[0023]

Chemical formula

[0024] When the oral composition of the present invention contains chebulic acid, the content of chebulic acid is not limited. However, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of blood glucose level increase, reduction of body fat, or reduction of BMI, it is preferable to contain 0.01 parts by mass or more of chebulic acid with respect to 1 part by mass of gallic acid, more preferably 0.02 parts by mass or more, still more preferably 0.05 parts by mass or more, and particularly preferably 0.1 parts by mass or more. Further, the oral composition of the present invention preferably contains 5 parts by mass or less of chebulic acid with respect to 1 part by mass of gallic acid, more preferably 3 parts by mass or less, still 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 chebulic acid, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of blood glucose level increase, reduction of body fat, or reduction of BMI, it is preferable to contain 0.01 parts by mass or more of chebulic acid with respect to a total of 1 part by mass of gallic acid and ellagic acid, more preferably 0.02 parts by mass or more, still more preferably 0.05 parts by mass or more, and particularly preferably 0.1 parts by mass or more. Further, the oral composition of the present invention preferably contains 5 parts by mass or less of chebulic acid with respect to a total of 1 part by mass of gallic acid and ellagic acid, more preferably 3 parts by mass or less, still 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, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of blood glucose level increase, reduction of body fat, or reduction of BMI, it 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.

[0027] The amount of chebulic acid in the composition of the present invention can be measured by LCMS method. For example, using Unison UK-C18 (HT 3μm φ3×100 mm) manufactured by Imtakt Corporation, as the liquid medium of the mobile phase, 0.1% formic acid aqueous solution for mobile phase A and acetonitrile for mobile phase B can be used, the column temperature can be 45°C, and the flow rate can be 0.7 mL / min. The ionization method can be electrospray, and the ionization mode can be negative. The gradient conditions can be as follows. In addition, when measuring, appropriate treatments such as removing impurities in the sample may be carried out as necessary to adapt to the separation ability of the apparatus.

[0028]

Table C

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

[0030] 4. Catechins From the perspective of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglycerides, suppression of sugar absorption, suppression of blood glucose level increase, 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. The content of catechins in this specification means the total amount of the above-mentioned 8 compounds. In the present invention, when catechins are hydrates, the amount of catechins referred to in this specification is converted to anhydrides.

[0031] Although not limited, from the perspective of the functionality as an auxiliary component of gallic acid, for the catechins used in the present invention, the ratio C1:C2 of the content C1 of non-gallate type catechins to the content C2 of gallate type catechins is preferably 1:0.01 to 13, more preferably 0.05 to 7. Also, in the catechins, epigallocatechin gallate (EGCG) preferably occupies 0.1 to 70% by mass, more preferably 0.5 to 60% by mass. For the catechins, the proportion occupied by the total amount of epigallocatechin (EGC) and epicatechin (EC) is preferably 20% by mass or more, more preferably 30% by mass or more. For the catechins, the content of catechin (C) preferably occupies 0.01 to 40% by mass, more preferably 0.1 to 20% by mass.

[0032] The catechins used in the present invention are not particularly limited as long as they can be used as foods, and plant-derived catechins and those obtained by synthesis can be used. When plant-derived catechins are used in the composition of the present invention, as the catechin source, plant extracts or pulverized powders may be used, or their purified products may be used. Examples of the plants from which catechins are derived include Acacia catechu, green tea, cacao beans, and apples. When the composition of the present invention contains catechins, the inventor believes that the catechins serve as an auxiliary component that enhances the effect of gallic acid.

[0033] When the oral composition of the present invention contains catechins, there is no particular limitation on the content of catechins. However, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglyceride, suppression of sugar absorption, suppression of increase in blood glucose level, reduction of body fat or reduction of BMI, it is preferable that the catechins are contained in an amount of 0.01 part by mass or more, more preferably 0.02 part by mass or more, still more preferably 0.05 part by mass or more, and particularly preferably 0.1 part by mass or more with respect to 1 part by mass of gallic acid. Further, in the oral composition of the present invention, it is preferable that the catechins are contained in an amount of 5 parts by mass or less, more preferably 3 parts by mass or less, still more preferably 2 parts by mass or less, and particularly preferably 1 part by mass or less with respect to 1 part by mass of gallic acid.

[0034] When the oral composition of the present invention contains catechins, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglyceride, suppression of sugar absorption, suppression of increase in blood glucose level, reduction of body fat or reduction of BMI, it is preferable that the catechins are contained in an amount of 0.01 part by mass or more, more preferably 0.02 part by mass or more, still more preferably 0.05 part by mass or more, and particularly preferably 0.1 part by mass or more with respect to a total of 1 part by mass of gallic acid and ellagic acid. Further, in the oral composition of the present invention, it is preferable that the catechins are contained in an amount of 5 parts by mass or less, more preferably 3 parts by mass or less, still more preferably 2 parts by mass or less, and particularly preferably 1 part by mass or less with respect to a total of 1 part by mass of gallic acid and ellagic acid.

[0035] When the oral composition of the present invention contains catechins, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of blood glucose level increase, 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 the solid content, more preferably 0.005% by mass or more, and still more preferably 0.01% by mass or more. Also, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of blood glucose level increase, reduction of body fat or reduction of BMI, it is preferable that the oral composition contains 50% by mass or less of catechins in the solid content, more preferably 40% by mass or less, still 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, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of blood glucose level increase, reduction of body fat or reduction of BMI, the oral composition of the present invention preferably contains at least chebulaic acid in addition to gallic acid and ellagic acid, and more preferably contains chebulaic acid and catechins.

[0037] The amount of catechins in the composition of the present invention can be measured by the HPLC method. For example, using L-Column ODS (3μm φ4.6×250 mm) manufactured by the Chemical Substances Evaluation and Research Foundation, as the liquid medium of the mobile phase, 0.1 M acetic acid aqueous solution for mobile phase A and 0.1 M acetic acid acetonitrile solution for mobile phase B can be used, the column temperature can be 40°C, and the flow rate can be 1.0 ml / min. The gradient conditions can be as follows. In addition, when measuring, appropriate treatment may be carried out as necessary, such as removing impurities in the sample to conform to the separation ability of the apparatus.

[0038]

Table D

[0039] Column: L-Column ODS 3 μm, 4.6×250 mm (manufactured by Chemical Substances Evaluation Research Institute, Incorporated Administrative Agency) Column temperature: 40 °C Injection volume: 10 μL Flow rate: 1.0 mL / min Measurement wavelength: 280 nm Mobile phase A solution: 0.1 M aqueous acetic acid solution Mobile phase B solution: 0.1 M acetonitrile solution of acetic acid

[0040] 5. Oral composition The oral composition of the present invention may contain components other than gallic acid, ellagic acid, chebulaic acid, and catechins, as long as it does not inhibit the expression of 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. Examples of such other components include saccharides, vitamins, minerals, proteins, dietary fibers such as insoluble dietary fibers, plants or processed plant products, yeasts, and the like. Further, if necessary, sweeteners, acidulants, colorants, thickeners, brighteners, lubricants, excipients, anti-caking agents, dietary supplements, binders, lubricants, stabilizers, diluents, bulking agents, emulsifiers, food additives, seasonings, and the like, which are usually used in the food field, may be contained.

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

[0042] Specific examples of the form of the oral composition of the present invention include pharmaceuticals (including quasi-drugs) and foods and drinks. Among them, from the viewpoint of being easily ingestible in daily life, foods and drinks are particularly preferred.

[0043] Examples of the food and drink of the present invention include so-called health foods such as general foods, functional foods, foods for specified health use whose efficacy display is approved by a specified agency, and foods with functional claims. Foods with efficacy display may be collectively referred to as "health functional foods" or "functional foods".

[0044] There is no particular limitation on the food and drink of the present invention, but examples include milk and dairy products; beverages such as soft drinks, fruit juices, milk drinks, alcoholic beverages, sports drinks, and nutritional drinks; seasonings; liquors; agricultural and forestry processed foods; confectionery and breads; cereal flours and noodles; processed fishery products; processed livestock products; fats and oil processed products; frozen cooked foods; retort foods; instant foods; food materials; supplements, etc. Examples of the form of supplements include, for example, tablet form, capsule form, powder form, granule form, liquid form, etc.

[0045] 6 . An oral composition used for applications such as suppressing fat absorption As is clear from the examples described later, the oral composition of the present invention can effectively inhibit the activity of intestinal-derived isomaltase and can also effectively inhibit 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 uses selected from (1) suppression of fat absorption, (2) suppression of increase in neutral fat, (3) suppression of sugar absorption, (4) suppression of increase in blood glucose level, (5) anti-obesity, (6) reduction of body fat, and (7) reduction of BMI (Body Mass Index). Body fat refers to the fat of the body and is a general term for visceral fat and subcutaneous fat. That is, the oral composition of the present invention can be used as (1) a composition for suppressing fat absorption, (2) a composition for suppressing increase in neutral fat, (3) a composition for suppressing sugar absorption, (4) a composition for suppressing increase in blood glucose level, (5) an anti-obesity composition, (6) a composition for reducing body fat, or (7) a composition for reducing BMI (Body Mass Index).

[0046] (1) "Suppression of fat absorption" refers to suppressing the amount of neutral fat ingested by diet absorbed into the body. (2) "Suppression of triglyceride increase" means suppressing the increase in the concentration of triglycerides in the blood after a meal or on an empty stomach. (3) "Suppression of sugar absorption" means suppressing the amount of sugar absorbed in the small intestine. (4) "Suppression of blood glucose level increase" means suppressing the increase in blood glucose level after a meal or on an empty stomach. (5) "Anti-obesity" means preventing or improving weight loss, weight gain suppression, and fat accumulation in the body, and is a concept that includes dieting for beauty purposes, etc. (6) "Reduction of body fat" means reducing the amount of body fat (visceral fat and subcutaneous fat), specifically the abdominal body fat (visceral fat and subcutaneous fat). (7) "Reduction of BMI" means reducing the value of BMI. The mechanisms by which the functions (1) to (7) are achieved according to the present invention are as follows.

[0047] By ingesting the oral composition of the present invention, the lipase activity in the body is inhibited. Lipase (pancreatic lipase) is a digestive enzyme synthesized in the pancreas and secreted into pancreatic juice to hydrolyze triglycerides. Triglycerides contained in food are decomposed by lipase into fatty acids and glycerol that are easily absorbed in the body, and the fatty acids and glycerol are absorbed by the small intestinal villus epithelial cells. The absorbed fatty acids and glycerol are resynthesized into triglycerides and transferred into the blood via lymph. As can be seen from the examples described later, when the oral composition of the present invention is ingested, the lipase activity is inhibited. Therefore, the decomposition of triglycerides in food into fatty acids and glycerol is suppressed, so the amount of fatty acids and glycerol absorbed by the small intestinal villus epithelial cells decreases, that is, (1) the absorption of fat is suppressed. In addition, since the amount of fatty acids and glycerol resynthesized into triglycerides decreases, (2) the increase in triglycerides is suppressed. As a result, (5) fat accumulation in the body is prevented (anti-obesity), and (6) body fat is reduced. As the body fat decreases, the weight decreases, and (7) the BMI also decreases.

[0048] Moreover, by ingesting the oral composition of the present invention, isomaltase activity in the body is inhibited. Isomaltase is a kind of α-glucosidase, a disaccharide-degrading enzyme that exists in the small intestine mucosa and has the function of decomposing disaccharides into monosaccharides. When the sugar contained in food reaches the small intestine, it is decomposed into easily absorbable monosaccharides (such as glucose) by the action of the degrading enzyme, absorbed from the small intestine mucosa, then transported to the liver, and transported from the liver into the bloodstream. When the concentration of glucose in the bloodstream increases, glucose is converted into neutral fat by the action of insulin, and the neutral fat is stored in fat cells. When isomaltase activity is inhibited, the decomposition of disaccharides into monosaccharides is suppressed, so the amount of easily absorbable monosaccharides decreases, and (3) the amount of sugar absorbed in the small intestine is suppressed. Also, after a meal, since the amount of glucose absorbed in the small intestine decreases, (4) the rise in blood glucose level is suppressed. When the increase in the concentration of glucose is suppressed, the conversion of glucose into neutral fat by the action of insulin is suppressed, so (5) the accumulation of fat in the body is prevented or suppressed (anti-obesity), and (6) body fat is reduced. Along with the reduction of body fat, body weight decreases, and (7) BMI also decreases.

[0049] In addition, 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 composition for lipase inhibition, a composition for α-glucosidase inhibition, and a composition for isomaltase inhibition.

[0050] From the viewpoint of reliably obtaining anti-obesity function, fat absorption inhibition function, neutral fat increase inhibition function, sugar absorption inhibition function, blood glucose level increase inhibition function, body fat reduction function, and BMI reduction function, it is preferable that the oral composition of the present invention inoculates 10 to 100 mg of gallic acid per adult per day, and more preferably inoculates 20 to 80 mg. Also, it is preferable that the total amount of gallic acid and ellagic acid inoculated is 10 to 120 mg, and more preferably inoculated orally at 20 to 100 mg.

[0051] When the oral composition of the present invention is an oral composition used for any of the functions (1) to (7) described above, it contains gallic acid and ellagic acid, and the mass ratio of gallic acid to ellagic acid is set within a specific range. In terms of being used for any of the functions (1) to (7), it is not particularly limited as long as it can be distinguished from other products as a product. For example, any of the main body, packaging, instruction manual, and promotional materials (advertising media) of the product according to the present invention that display any of the functions (1) to (7) are included in 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 an active ingredient, but it is not limited to those in which gallic acid is displayed as an active ingredient on the packaging of the product, etc. For example, it may not specify the active ingredient. Also, even general foods that are manufactured and sold with suggestions of their uses are included in the scope of the present invention. For example, foods, etc. sold with testimonials on a homepage, etc. that mention the maintenance and / or improvement of any of the functions (1) to (7) as personal impressions of the person who ingested them are also included in the scope of the present invention. Also, functional foods that use papers, etc. indicating the maintenance and / or improvement of any of the functions (1) to (7) as scientific bases for functionality, and use gallic acid as a functional-related component, and functional foods that display the functionality related to any of the functions (1) to (7) as a notification display are also included in the scope of the present invention. As described above, since components other than gallic acid in the present invention are auxiliary components for enhancing the effect of gallic acid, in functional foods or foods for specified health use that display any of the functions (1) to (7), they are usually not displayed as participating components. However, the oral composition used for any of the functions (1) to (7) in the present invention does not exclude those that display auxiliary components such as ellagic acid and chebulaic acid as participating components, and functional foods, etc. that display ellagic acid, etc. as participating components are also included in the oral composition.

[0052] As described above, the oral composition used for any of the functions (1) to (7) includes food and drink products labeled as having one or more functions selected from the group consisting of an anti-obesity function, a fat absorption inhibitory function, a neutral fat increase inhibitory function, a sugar absorption inhibitory function, a blood glucose level increase inhibitory function, a body fat reduction function, and a BMI reduction function. The method of the above labeling is preferably in the following mode (1) or (2).

[0053] (1) A food or drink product is a functional food labeled as such that has been notified to the Consumer Affairs Agency by the business operator, at its own responsibility, and based on scientific evidence, that it has an anti-obesity function, a fat absorption inhibitory function, a neutral fat increase inhibitory function, a sugar absorption inhibitory function, a blood glucose level increase inhibitory function, a body fat reduction function, and / or a BMI reduction function, and is displayed on the product package. (2) A food or drink product is a food for specified health use labeled as such that has been permitted by the Consumer Affairs Agency to display on the product package, based on scientific evidence, that it has an anti-obesity function, a fat absorption inhibitory function, a neutral fat increase inhibitory function, a sugar absorption inhibitory function, a blood glucose level increase inhibitory function, a body fat reduction function, and / or a BMI reduction function.

[0054] For example, as examples of the above labels (1) and (2), labels that appeal to target individuals who are concerned about body fat, such as those who are concerned about obesity, those who are concerned about abdominal circumference, those who are concerned about weight, those who are concerned about abdominal fat (such as visceral fat and subcutaneous fat), etc., or labels that state that it helps to reduce weight, helps to reduce abdominal fat (such as visceral fat and subcutaneous fat), helps to reduce waist circumference, supports obesity resolution, supports dieting, makes it easier to reduce fat, reduces fat absorption, helps to suppress or reduce the increase of body fat, suppresses the increase of blood glucose level, suppresses sugar absorption, moderates the increase of blood glucose level, suppresses the increase of postprandial blood glucose level, moderates the increase of postprandial blood glucose level, suppresses the absorption of neutral fat, suppresses the increase of neutral fat, moderates the increase of neutral fat, suppresses the increase of postprandial neutral fat, suppresses the absorption of sugar and fat contained in food, etc. can be mentioned.

[0055] The present invention provides the following. <1> 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 = 0.01 to 0.7. <2> The oral composition according to <1> above, which is used for one or more uses selected from anti-obesity, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of increase in blood glucose level, reduction of body fat, and reduction of BMI. <3> The oral composition according to <1> or <2> above, which further contains chebulic acid. <4> The oral composition according to at least one of <1> to <3> above, which further contains catechins. <5> The oral composition according to at least one of <1> to <4> above, which is used for one or more uses selected from anti-obesity use, fat absorption suppression use, neutral fat increase suppression use, sugar absorption suppression use, blood glucose level increase suppression use, body fat reduction function use, and BMI reduction function use. <6> The oral composition according to at least one of <1> to <5> above, which is for suppressing the increase in postprandial neutral fat or suppressing the increase in postprandial blood glucose level. <7> The oral composition according to at least one of <1> to <5> above, which is for lipase inhibition or α-glucosidase inhibition. <8> An oral composition containing gallic acid as an active ingredient, which further contains ellagic acid, wherein the mass ratio of gallic acid to ellagic acid in the composition is gallic acid:ellagic acid = 0.01 to 0.7, and which is used for one or more uses selected from anti-obesity, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of increase in blood glucose level, reduction of body fat, and reduction of BMI. <9> A food or drink product containing gallic acid as an active ingredient, which further contains ellagic acid, The mass ratio of gallic acid to ellagic acid in the food or drink is gallic acid:ellagic acid = 1:0.01 to 0.7, A food or drink that is labeled as having one or more functions selected from the group consisting of an anti-obesity function, a fat absorption inhibitory function, a neutral fat increase inhibitory function, a sugar absorption inhibitory function, a blood glucose level increase inhibitory function, a body fat reduction function, and a BMI reduction function. <10> The food or drink according to <9> above, which is a functional food or a food for specified health use.

Examples

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

[0057] In the examples and comparative examples, as gallic acid, a reagent of gallic acid (anhydrous, powdered, purity about 100% by mass) was used. As ellagic acid, a reagent of ellagic acid (anhydrous, powdered, purity about 98% by mass or more) was used. As chebulic acid, an anhydrous, powdered one with a purity of 98% by mass or more was used. As catechins, a catechin purified product derived from tea was used. As ascorbic acid, sodium L(+)-ascorbate was used. As erythorbic acid, sodium erythorbate (monohydrate) was used.

[0058] [Examples 1 to 9 and Comparative Examples 1 to 10] Using the raw materials listed in Tables 1 and 2, the test substances of Examples 1 to 9 and Comparative Examples 1 to 10 were prepared. When a plurality of raw materials were used, the test substances were prepared by mixing the plurality of raw materials. The amounts of raw materials used are as shown in Tables 1 and 2.

[0059] The following isomaltase inhibition test was conducted on the test substances of Examples 1 to 9 and Comparative Examples 1 to 10.

[0060] <Isomaltase Inhibition Test> (1) 900 μL of 56 mM maleic acid buffer (pH 6.0) was added to 100 mg of rat intestinal acetone powder (manufactured by SIGMA) and homogenized to prepare a mixed solution. The prepared mixed solution was centrifuged (3000 rpm, 10 minutes, 4 °C), and the supernatant was collected. The collected supernatant was diluted 2-fold with 56 mM maleic acid buffer (pH 6.0) to prepare an enzyme solution. (2) Isomaltose was dissolved in 56 mM maleic acid buffer (pH 6.0) to a concentration of 5 mM to prepare a substrate solution. (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 a test substance solution. (4) 15 μL of the enzyme solution was added to 15 μL of the test substance solution, and after pre-incubating at 37 °C for 5 minutes, 90 μL of the substrate solution was further added and incubated at 37 °C for 30 minutes to cause a reaction. (5) After the reaction, the mixture was treated at 98 °C for 2 minutes to stop the enzyme reaction. (6) After stopping the reaction, the absorbance at 505 nm was measured using a glucose test Wako (manufactured by Wako Pure Chemical Industries, Ltd.) to measure the isomaltase inhibitory activity of the test substance. The measured value was designated as measured value A. (7) The procedure was the same as the above procedure for measuring the isomaltase inhibitory activity, except that a 10% DMSO solution was used instead of the test substance solution, and the absorbance of the test solution was measured to obtain a measured value B. (8) The procedure was the same as the above procedure for measuring the isomaltase inhibitory activity, except that an enzyme solution heat-inactivated by treating at 98 °C for 2 minutes was used instead of the enzyme solution, and the absorbance of the test solution was measured to obtain a measured value C. (9) The procedure was the same as the above activity measurement procedure, except that a 10% DMSO solution was used instead of the test substance solution and an enzyme solution heat-inactivated by treating at 98 °C for 2 minutes was used instead of the enzyme solution, and the absorbance of the test solution was measured to obtain a measured value D. (10) From measured value A, measured value B, measured value C, and measured value D, the isomaltase inhibition rate (% of control) was calculated using the following formula (1). The results are shown in Tables 1 and 2. Isomaltase inhibition rate (% of control) = (measured value A - measured value C) / (measured value B - measured value D) × 100 (1)

[0061]

Table 1

[0062]

Table 2

[0063] As is clear from Table 1 and Table 2, in Examples 1 to 9 where the ratio of gallic acid to ellagic acid is in the range of gallic acid:ellagic acid = 1:0.01 to 0.7, the isomaltase inhibition rate was significantly higher than that of Comparative Examples 1 to 6 used individually. As a result of such an improvement effect in the present invention, the decomposition of disaccharides into monosaccharides is suppressed, so it is expected that the effects of suppressing sugar absorption, suppressing an increase in blood glucose level, anti-obesity, reducing body fat, and reducing BMI will be effectively exhibited. Such excellent effects were not achieved 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 contents of gallic acid and ellagic acid were outside the scope of the present invention. In particular, among Examples 1 to 6, the isomaltase inhibition rate varies depending on the ratio of gallic acid:ellagic acid, and it can be seen that there is a preferable range of gallic acid:ellagic acid in order to increase the isomaltase inhibition rate.

[0064] Furthermore, in Examples 7 and 8 in which chebulic acid was combined with gallic acid and ellagic acid, the mass ratio of ellagic acid to 1 part by mass of gallic acid is the same as that of Examples 3 and 4, but the isomaltase inhibition rate was even higher than that of Examples 3 and 4 that did not contain chebulic acid. Therefore, in these Examples 7 to 8, it was found that the intestinal isomaltase activity was significantly and effectively inhibited by combining chebulic acid with gallic acid and ellagic acid. Therefore, it was suggested that by this combination, the decomposition of disaccharides into monosaccharides in the intestinal tract is further suppressed, so that the effects of suppressing sugar absorption, suppressing an increase in blood glucose level, anti-obesity, reducing body fat, and reducing BMI are further significantly exhibited.

[0065] Furthermore, in Example 9 where gallic acid, ellagic acid, chebulic acid, and catechins were used in combination, the mass ratios of ellagic acid and chebulic acid to 1 part by mass of gallic acid were the same as those in Example 7. However, the isomaltase inhibition rate was even higher than that in Example 7 which did not contain catechins. Therefore, it was suggested that this combination further suppressed the decomposition of disaccharides into monosaccharides in the intestinal tract, and thus the effects of suppressing sugar absorption, suppressing the rise in blood glucose level, anti-obesity, reducing body fat, and reducing BMI were even more significantly exerted.

[0066] [Examples 10 to 16 and Comparative Examples 11 to 20] Using the raw materials described in Tables 3 and 4, the test substances of Examples 10 to 16 and Comparative Examples 11 to 20 were prepared. When multiple raw materials were used, the test substances were prepared by mixing the multiple raw materials. The usage amounts of the raw materials were as shown in Tables 3 and 4.

[0067] The following lipase inhibition test was conducted on the test substances of Examples 10 to 16 and Comparative Examples 11 to 20.

[0068] [Lipase Inhibition Activity Test] The lipase inhibition activity was measured according to the method of Lipase Kit S (manufactured by Sumitomo Bakelite Co., Ltd.). Specifically, the lipase inhibition activity of the test substance was measured by the following procedure. The substrate of Lipase Kit S is known for its high reactivity with pancreatic lipase. (1) Porcine pancreatic lipase (manufactured by SIGMA) was dissolved using 0.01 M phosphate buffer (pH 7.0) to prepare a lipase solution of 0.3 mg / mL. For the inhibition test, a lipase solution of 0.06 mg / mL obtained by diluting this 0.3 mg / mL lipase solution 5-fold with 0.01 M phosphate buffer (pH 7.0) was used. (2) The test substance was dissolved in 2.5% DMSO-containing Tris-HCl buffer (pH 8.55) to prepare a test substance solution such that the total amount of the test substance had a concentration of 0.264 mg / mL. (3) 6 μL of the test substance solution, 80 μL of the chromogenic solution in the kit, 10 μL of the lipase solution, and 1.6 μL of the esterase inhibitor solution were mixed, pre-incubated at 37°C for 5 minutes, then 8 μL of the substrate solution in the kit was added and incubation was continued at 37°C for 30 minutes. (4) Then, 160 μL of the reaction stop solution in the kit was added to the mixture and mixed. The absorbance at 412 nm was measured to determine the lipase inhibitory activity, and the measured value A was obtained. (5) The procedure for the lipase inhibitory activity measurement test described above was followed, 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 measured value B. (6) The procedure for the lipase inhibitory activity measurement test described above was followed, except that the substrate solution was added after adding the reaction stop solution. The absorbance of the test solution was measured to obtain the measured value C. (7) The procedure for the lipase inhibitory activity measurement test described above was followed, 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 adding the reaction stop solution. The absorbance of the test solution was measured to obtain the measured value D. (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) = (Measured value A - Measured value C) / (Measured value B - Measured value D) × 100 (2)

[0069]

Table 3

[0070]

Table 4

[0071] As is clear from Tables 3 to 4, in Examples 10 to 16 where the ratio of gallic acid to ellagic acid is in the range of gallic acid:ellagic acid = 1:0.01 to 0.7, the lipase inhibition rate was significantly improved compared to Comparative Examples 11 to 16 using the raw materials alone. As a result of such an improvement effect in the present invention, the decomposition of neutral fat 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 increase in neutral fat, anti-obesity, reducing body fat, and reducing BMI will be improved. Such excellent effects were not achieved in Comparative Examples 17 to 19 using gallic acid in combination with antioxidant components other than ellagic acid, and Comparative Example 20 where the content ratio of gallic acid to ellagic acid is outside the scope of the present invention. In particular, among Examples 10 to 15, the lipase inhibition rate varies depending on the ratio of gallic acid:ellagic acid, and it can be seen that there is a preferable range of gallic acid:ellagic acid to increase the lipase inhibition rate.

[0072] In particular, in Example 16 where chebulic acid was combined with gallic acid and ellagic acid, the mass ratio of ellagic acid to 1 part by mass of gallic acid is the same as that in Example 12, but the lipase inhibition rate was even higher than that in Example 12 which does not contain ellagic acid. Therefore, it was suggested that each of the above effects is more significantly exhibited by the combination.

[0073] [Examples 17 to 24] Each raw material was mixed in the ratio shown in Table 5, and using a single-punch tableting machine, tablets (swallowable tablets) with a weight of 250 mg per tablet and a tablet diameter of 8 mm were produced. The pressure for tableting was set at 3 kN. The obtained tablets exhibited anti-obesity effects, fat absorption inhibitory effects, neutral fat increase inhibitory effects, sugar absorption inhibitory effects, blood glucose level increase inhibitory effects, body fat reduction effects, and BMI reduction effects when ingested 2 tablets per day.

[0074]

Table 5

Claims

1. A food or drink containing gallic acid as an active ingredient, It also contains ellagic acid and chebulic acid, a mass ratio of gallic acid to ellagic acid in the food or drink is gallic acid:ellagic acid=1:0.1 to 0.2; A food or drink that is labeled as having one or more functions selected from the group consisting of an anti-obesity function, a function for inhibiting fat absorption, a function for inhibiting an increase in neutral fat levels, a function for inhibiting sugar absorption, a function for inhibiting an increase in blood sugar levels, a function for reducing body fat, and a function for reducing BMI.

2. The food or drink according to claim 1, which is a functional food or a food for specified health uses.

Citation Information

Patent Citations

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