Oral composition

An oral composition with gallic acid and catechins in a specific ratio, enhanced by ellagic and chebulic acid, addresses the need for effective fat and sugar absorption inhibition, triglyceride and glucose level control, and body fat reduction, offering a palatable solution.

JP2026083813AActive 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, suppress triglyceride and blood glucose levels, reduce body fat, and lower BMI without the unpleasant taste associated with certain plant-derived ingredients.

Method used

A specific oral composition containing gallic acid and catechins in a mass ratio of 1:0.1 to 5, optionally with ellagic acid and chebulic acid, which inhibits lipase and isomaltase activities to achieve anti-obesity and blood glucose regulation effects.

Benefits of technology

The composition effectively inhibits fat and sugar absorption, reduces triglycerides and blood glucose levels, and decreases body fat and BMI, providing a tasteful alternative to traditional 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 catechins, An oral composition wherein the mass ratio in the composition is gallic acid:catechins = 1:0.1 to 5. The oral composition preferably further contains ellagic acid. It is also preferable to use it for 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.
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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 food has been relatively excessive. Concerns have been raised about the impact on health, and diabetes and obesity, which are considered to be deeply involved in the cause of such lifestyles, are thought to be closely related to these lifestyle habits. 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 a deep involvement of lifestyle habits. Since diabetes and obesity lead to arteriosclerosis, cancer, etc., it is required to prevent or improve diabetes and obesity in daily dietary life.

[0003] One of the measures for preventing diabetes and obesity is to suppress an increase in blood glucose and an increase in neutral fat in the blood. In order 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, in order 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, since the absorption of neutral fat in the intestinal tract and thus in the body is suppressed, 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

Patent 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, by using a specific composition, such as a specific ratio of gallic acid and catechins, it is possible to obtain a composition that exhibits improved functions in terms of 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 compared to conventional compositions.

[0007] In other words, the present invention relates to an oral composition containing gallic acid and catechins, The present invention provides an oral composition in which the mass ratio of gallic acid to catechins is 1:0.1 to 5. [Effects of the Invention]

[0008] According to the present invention, it is possible to provide useful oral compositions containing gallic acid and catechins, 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 triglyceride increase, suppression of sugar absorption, suppression of blood glucose increase, 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 plants from which it may be derived include green tea, date palm, and persimmon. Furthermore, the gallic acid used in this invention may be anhydrous or a hydrate such as a monohydrate. In addition, gallic acid may 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 80% by mass, and particularly preferably 0.01% to 70% 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 reduction of BMI, and from the viewpoint of taste when taken orally. In this specification, "solid content" refers to the amount contained in the composition if the composition is in solid form, and refers to 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. 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 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 the general term for 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 kinds of compounds. In the present invention, when catechins are hydrates, the amount of catechins referred to in this specification is in terms of anhydride conversion.

[0016] 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 using plant-derived catechins in the composition of the present invention, as a catechin source, plant extracts or pulverized powders may be used, or purified products thereof may be used. Examples of plants from which catechins are derived include Acacia catechu, green tea, cacao beans, and apples.

[0017] In the present invention, the inventor believes that catechins are auxiliary components that enhance 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 catechins in the composition of the present invention as gallic acid:catechins = 1:0.1 to 5. As shown in the examples described later, in the present invention, the function of gallic acid can be effectively enhanced by using catechins as compared with the case of combining gallic acid without catechins with components other than catechins (for example, ascorbic acid, erythorbic acid). Also, as compared with the case where the mass ratio of gallic acid to catechins is outside the range of gallic acid:catechins = 1:0.1 to 5, 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 the ratio within this range.

[0018] In the present invention, 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 mass ratio of gallic acid to catechins in the composition is preferably gallic acid:catechins = 1:0.2 to 2.5, more preferably gallic acid:catechins = 1:0.2 to 2.0, still more preferably 0.3 to 1.5, and particularly preferably 0.4 to 1.0.

[0019] 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, 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, and more preferably 0.05 to 7.

[0020] 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, in the catechins, gallocatechin (GC) preferably occupies 0 to 20% by mass, and more preferably 0 to 10% by mass. In the catechins, epigallocatechin (EGC) is 0.01 to It is preferable that it accounts for 95% by mass, and more preferably 0.1 to 90% by mass. Furthermore, among the catechins, it is preferable that catechin (C) accounts for 0.01 to 40% by mass, and more preferably 0.1 to 20% by mass. In addition, among the catechins, it is preferable that epicatechin gallate (ECG) accounts for 0.01 to 40% by mass, and more preferably 0.1 to 20% by mass. Among the catechins, it is preferable that epigallocatechin gallate (EGCG) accounts for 0.1 to 70% by mass, and more preferably 0.5 to 60% by mass. Among the catechins, it is preferable that gallocatechin gallate (GCG) accounts for 0.01 to 30% by mass, and more preferably 0.1 to 20% by mass. Among the catechins, it is preferable that epicatechin (EC) accounts for 0.01 to 95% by mass, and more preferably 0.1 to 90% by mass. In the catechins, catechin gallate (CG) preferably accounts for 0 to 40% by mass, and more preferably 0 to 20% by mass. Furthermore, in the catechins used in this invention, the total amount of epigallocatechin (EGC) and epicatechin (EC) preferably accounts for 20% by mass or more, and more preferably 30% by mass or more.

[0021] 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 85% by mass or less of catechins in its solid content, more preferably 70% by mass or less, even more preferably 60% by mass or less, and particularly preferably 40% by mass or less.

[0022] 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.

[0023] [Table B]

[0024] 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

[0025] 3. Ellagic 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 contains at least ellagic acid in addition to gallic acid and catechins, and more preferably contains ellagic acid and chebulic acid.

[0026] The composition of the present invention preferably contains ellagic acid. Ellagic acid is a type of natural phenolic compound, C 14 It is represented as H6O8. The ellagic acid used in this invention is not particularly limited as long as it is suitable for use in food, and plant-derived ellagic acid or synthetically obtained ellagic acid can be used. When plant-derived ellagic acid is used in the composition of this invention, plant extracts or powders may be used as the ellagic acid source, or purified products thereof may be used. When plant-derived ellagic acid is used, examples of the plants from which it may be derived include strawberries, raspberries, and pomegranates. Furthermore, the ellagic acid used in this invention may be in the form of an anhydrous form or a hydrate such as a monohydrate. Ellagic acid may also be in the form of a salt. When a salt of ellagic acid is used in this invention, alkali metal ellagic acid salts are examples. In this invention, when ellagic acid is in the form of a hydrate, the amount of ellagic acid referred to herein is on an anhydrous basis. In this invention, when a salt is used as ellagic acid, the amount of ellagic acid is on an ellagic acid basis.

[0027] When the oral composition of the present invention contains ellagic 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 0.001 parts by mass or more of ellagic acid per 1 part by mass of gallic acid, more preferably 0.003 parts by mass or more, even more preferably 0.006 parts by mass or more, particularly preferably 0.008 parts by mass or more, and especially preferably 0.01 parts by mass or more. Furthermore, the oral composition of the present invention preferably contains 0.7 parts by mass or less of ellagic acid per 1 part by mass of gallic acid, more preferably 0.5 parts by mass or less, even more preferably 0.9 parts by mass or less, particularly preferably 0.8 parts by mass or less, and especially preferably 0.7 parts by mass or less.

[0028] When the oral composition of the present invention contains ellagic 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 0.005 parts by mass or more of ellagic acid per 1 part by mass of the total amount of gallic acid and catechins, more preferably 0.008 parts by mass or more, even more preferably 0.04 parts by mass or less, particularly preferably 0.08 parts by mass or more, and especially preferably 0.11 parts by mass or more. Furthermore, the oral composition of the present invention preferably contains 0.7 parts by mass or less of ellagic acid per 1 part by mass of the total amount of gallic acid and catechins, more preferably 0.5 parts by mass or less, even more preferably 0.4 parts by mass or less, particularly preferably 0.3 parts by mass or less, and especially preferably 0.2 parts by mass or less.

[0029] 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 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 even more preferably 0.0001% by mass or more and 25% by mass or less, in the solid content of the oral composition.

[0030] The amount of ellagic 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.

[0031] [Table C]

[0032] 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

[0033] 4. 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.

[0034] [ka]

[0035] 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.

[0036] 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 catechins, 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 catechins, 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.

[0037] 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.

[0038] 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.

[0039] [Table D]

[0040] 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

[0041] 5. Oral Composition The oral composition of the present invention may contain other components besides gallic acid, catechins, ellagic acid, and chebulic acid, 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.

[0042] 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.

[0043] 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.

[0044] 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."

[0045] 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.

[0046] 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. Therefore, the oral composition of the present invention is suitably used for one or more applications selected from (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). Fat refers to body fat 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 suppressing fat absorption, (2) a composition for suppressing the rise in triglycerides, (3) a composition for suppressing sugar absorption, (4) a composition for suppressing 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).

[0047] (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 glucose 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:

[0048] 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.

[0049] 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.

[0050] 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.

[0051] 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 ingest a total of 10 to 400 mg of gallic acid and catechins, and more preferably 20 to 380 mg orally.

[0052] 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 catechins, the mass ratio of gallic acid to catechins 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 publications 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 catechins or ellagic acid are listed as active ingredients, and functional foods that display catechins etc. as active ingredients are also included in this oral composition.

[0053] 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.

[0054] (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.

[0055] For example, the aforementioned displays include those 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.)." Other displays indicate that the product helps to reduce weight, helps to reduce abdominal fat (visceral fat and subcutaneous fat, etc.), helps to reduce waist circumference, supports weight loss, supports dieting, makes it easier to reduce fat, reduces fat absorption, helps to suppress or reduce the increase of body fat, and also indicate that the product helps to 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.

[0056] The present invention provides the following: <1> An oral composition containing gallic acid and catechins, An oral composition in which the mass ratio of gallic acid to catechins is 1:0.1 to 5. <2> Furthermore, the above contains ellagic acid. <1> or <2> The oral composition described above. <3> The ellagic acid content is 0.01 parts by mass or more and 0.7 parts by mass or less per 1 part by mass of gallic acid, <1> or <2> The oral composition described above. <4> Furthermore, the above contains chebulic acid. <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 catechins, The mass ratio of gallic acid to catechins in the above composition is gallic acid:catechins = 1:0.1~5. 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 catechin acid, The mass ratio of gallic acid to catechins in the aforementioned food and beverage is gallic acid:catechins = 1:0.1~5. 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]

[0057] 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".

[0058] In the examples and comparative examples, gallic acid was used as a reagent for gallic acid (anhydrous, powder, purity approximately 100% by mass). For catechins, purified catechin derived from tea was used. For ellagic acid, a reagent for ellagic acid (anhydrous, powder, purity 98% by mass or higher) was used. For chebula acid, anhydrous, powder, purity 98% by mass or higher was used. Ascorbic acid was used, and sodium erythorbate (monohydrate) was used as the substitute for ascorbic acid.

[0059] [Comparative Examples 1-9 and Examples 1-12: Isomaltase Inhibition Test] The test substances for Comparative Examples 1-9 and Examples 1-12 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.

[0060] The following isomaltase inhibition tests were performed on the test substances of Comparative Examples 1-9 and Examples 1-12.

[0061] <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 1-3. Isomaltase inhibition rate (% of control) = (Measurement A - Measurement C) / (Measurement B - Measurement D) × 100 (1)

[0062] [Table 1]

[0063] [Table 2]

[0064] [Table 3]

[0065] As is clear from Tables 1 to 3, Examples 1 to 12, in which the ratio of gallic acid to catechins was in the range of gallic acid:catechins = 1:0.1 to 5, showed significantly higher isomaltase inhibition rates compared to Comparative Examples 1 to 6, in which the raw materials were 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 synergistic effects were not observed in Comparative Examples 7 to 9, in which gallic acid was used in combination with antioxidant components other than catechins. In particular, the isomaltase inhibition rate differed depending on the gallic acid:catechin ratio in Examples 1 to 8, indicating that there is a preferred range for the gallic acid:catechin ratio to increase the isomaltase inhibition rate.

[0066] Furthermore, in Examples 9, 10, and 11, which used ellagic acid in combination with gallic acid and catechins, the isomaltase inhibition rate was even higher compared to Examples 2 and 7, which did not contain ellagic acid, although the mass ratio of catechins to 1 part by mass of gallic acid was the same. Therefore, it was suggested that this combination further suppresses the breakdown of disaccharides into 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.

[0067] Furthermore, in Example 12, which used gallic acid and catechins in combination with ellagic acid and chebulic acid, the mass ratio of catechins and ellagic acid to 1 part by mass of gallic acid was the same as in Example 9, but the isomaltase inhibition rate was even higher than in Example 9, which did not contain chebulic acid. 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 level rise, anti-obesity, reduction of body fat, and reduction of BMI.

[0068] [Comparative Examples 10-18 and Examples 13-22: Lipase Inhibitory Activity Tests] The test substances for Comparative Examples 10-15 and Examples 13-22 were prepared using the raw materials listed in Tables 4-6. 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 4-6.

[0069] The following lipase inhibition tests were performed on the test substances of Comparative Examples 10-18 and Examples 13-22.

[0070] <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 4 to 6. Lipase inhibition rate (% of control) = (Measurement A - Measurement C) / (Measurement B - Measurement D) × 100 (2)

[0071] [Table 4]

[0072] [Table 5]

[0073] [Table 6]

[0074] As is clear from Tables 4 to 6, Examples 13 to 16, in which the ratio of gallic acid to catechins was in the range of gallic acid:catechins = 1:0.1 to 5, showed a significantly improved lipase inhibition rate compared to Comparative Examples 10 to 15, 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 16 to 18, in which gallic acid was used in combination with antioxidant components other than catechins, and in Comparative Example 19, in which the content of gallic acid and catechins was outside the range of the present invention. However, it was not performed. In particular, among Examples 13 to 18, the lipase inhibition rate differed depending on the gallic acid:catechin ratio, indicating that there is a preferred range for the gallic acid:catechin ratio to increase the lipase inhibition rate.

[0075] In particular, in Examples 19-21, which used gallic acid, catechins, and ellagic acid in combination, the mass ratio of catechins to 1 part by mass of gallic acid was the same, but the lipase inhibition rate was even higher compared to Examples 13 and 17, which did not contain ellagic acid. Therefore, it was found that in Examples 19-21, the combination of gallic acid, catechins, and ellagic acid significantly and effectively inhibited lipase activity. This suggests that the aforementioned effects are even more pronounced with this combination.

[0076] Furthermore, in Example 22, which used a combination of gallic acid, catechins, ellagic acid, and chebulic acid, the mass ratio of catechins and ellagic acid to 1 part by mass of gallic acid was the same as in Example 19, but the lipase inhibition rate was even higher than in Example 19, which did not contain chebulic acid. It was found that these four components significantly and effectively inhibited lipase activity, such as pancreatic lipase activity. Therefore, it was suggested that the aforementioned effects were even more pronounced with this combination.

[0077] [Examples 23-34] The raw materials were mixed in the proportions shown in Tables 7 and 8, 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.

[0078] [Table 7]

[0079] [Table 8]

Claims

1. An oral composition containing gallic acid and catechins, An oral composition in which the mass ratio of gallic acid to catechins in the composition is gallic acid:catechins = 1:0.1 to 5.

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. Furthermore, the oral composition according to claim 1 or 2, further containing ellagic acid.

4. Food and beverages containing gallic acid as an active ingredient, Furthermore, it contains catechins, The mass ratio of gallic acid to catechins in the aforementioned food and beverage is gallic acid:catechins = 1:0.1 to 5. Food and beverages that display a claim that they have one or more functions selected from the following: anti-obesity, inhibition of fat absorption, inhibition of triglyceride increase, inhibition of sugar absorption, inhibition of blood glucose level increase, reduction of body fat, and reduction of BMI.

5. Food and beverages containing gallic acid as an active ingredient, Furthermore, it contains catechins and chebulic acid, The mass ratio of gallic acid to catechins in the aforementioned food and beverage is gallic acid:catechins = 1:0.1 to 5. Food and beverages that display a claim that they have one or more functions selected from the following: anti-obesity, inhibition of fat absorption, inhibition of triglyceride increase, inhibition of sugar absorption, inhibition of blood glucose level increase, reduction of body fat, and reduction of BMI.

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