JP7752893B1 - Oral Composition - Google Patents

Abstract

The present invention provides an oral composition that can be used for anti-obesity, suppressing fat absorption, suppressing increases in neutral fat levels, suppressing sugar absorption, suppressing increases in blood sugar levels, reducing body fat, or reducing BMI.
An oral composition containing gallic acid and catechins,
An oral composition having a mass ratio of gallic acid to catechins of 1:0.1 to 5. The oral composition preferably further contains ellagic acid. It is also preferably used for anti-obesity, suppression of fat absorption, suppression of an increase in neutral fat, suppression of sugar absorption, suppression of an increase in blood glucose level, reduction of body fat, or reduction of BMI.
[Selection diagram] None

Description

The present invention relates to oral compositions and food and beverage products.

In recent years, the overall level of physical activity in the lives of Japanese people has tended to decline, while dietary energy intake has tended to be relatively excessive. Diabetes and obesity, which are of concern for their impact on health, 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, their incidence among young people has become more prevalent, and subsequent research has revealed that lifestyle habits are deeply involved. Because diabetes and obesity can lead to arteriosclerosis, cancer, and other conditions, it is necessary to prevent or improve diabetes and obesity through daily eating habits.

One of the strategies for preventing diabetes and obesity is to suppress elevated blood glucose levels and elevated blood triglycerides. To suppress elevated blood glucose levels, it is effective to inhibit the activity of disaccharidases present in the gastrointestinal mucosa and suppress the production of glucose. Inhibition of disaccharidases can suppress elevated blood glucose levels and inhibit intestinal sugar absorption, leading to reduced body fat, reduced obesity, and a lower BMI. Another strategy for suppressing blood triglycerides is to inhibit pancreatic lipase, thereby suppressing the production of free fatty acids. This suppresses the absorption of triglycerides in the intestine and, ultimately, the body, thereby suppressing blood triglyceride levels, leading to reduced elevated triglycerides, reduced body fat, reduced obesity, and a lower BMI.
For example, Patent Document 1 describes that the pericarp of plants of the Akebia family exhibits anti-obesity effects and neutral fat elevation suppression effects due to its lipase inhibitory activity. However, some consumers dislike the taste of the pericarp of plants of the Akebia family. Therefore, there has been a demand for the development of a new oral composition that exhibits effects such as anti-obesity effects and neutral fat elevation suppression.

JP 2010-265182 A

The present invention aims to provide a new oral composition that exhibits anti-obesity effects, inhibits fat absorption, inhibits increases in triglyceride levels, inhibits sugar absorption, inhibits increases in blood glucose levels, and reduces body fat or BMI.

The inventors have surprisingly discovered that by using a specific composition containing gallic acid and catechins, such as a specific ratio of gallic acid and catechins, it is possible to obtain a composition with improved functions compared to conventional compositions in terms of anti-obesity, suppression of fat absorption, suppression of increases in triglyceride levels, suppression of sugar absorption, suppression of increases in blood glucose levels, reduction of body fat, and reduction of BMI.

That is, the present invention provides 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 1:0.1-5.

The present invention provides a useful oral composition containing a composition 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, suppressing fat absorption, suppressing increases in triglyceride levels, suppressing sugar absorption, suppressing increases in blood sugar levels, reducing body fat, or reducing BMI.

Preferred embodiments of the oral composition of the present invention will be described below.
The oral composition of the present invention contains gallic acid as an active ingredient for its functions of anti-obesity, inhibiting fat absorption, inhibiting increases in triglyceride levels, inhibiting sugar absorption, inhibiting increases in blood glucose levels, reducing body fat, or reducing BMI.

1. Gallic Acid The gallic acid used in the present invention is a compound represented _{by C7H6O5} and is also known as 3,4,5-trihydroxybenzoic acid. Gallic acid is known to have effects such as anti-obesity, suppression of _fat absorption, suppression of increases in neutral fat levels, suppression of increases in sugar absorption, suppression of increases in blood glucose levels, reduction of body fat, and reduction of BMI, and also functions as an active ingredient in the composition of the present invention. The gallic acid used in the present invention is not particularly limited as long as it is suitable for use 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 the present invention, plant extracts or pulverized powders may be used as the gallic acid source, or purified products thereof may also be used. "Pulverized powder" refers to powder obtained by drying and pulverizing a plant. When plant-derived gallic acid is used, examples of the plant from which it is derived include green tea, dates, and persimmons. Furthermore, the gallic acid used in the present invention may be anhydrous or a hydrate, such as a monohydrate. Gallic acid may also be in the form of a salt. When a salt of gallic acid is used in the present invention, examples of the salt of gallic acid include alkali metal salts. When gallic acid is a hydrate in the present invention, the amount of gallic acid referred to in this specification is calculated as an anhydrous form. When a salt is used as gallic acid in the present invention, the amount of gallic acid refers to the amount calculated as gallic acid.

From the perspective of further enhancing the functions of gallic acid in anti-obesity, suppressing fat absorption, suppressing increases in triglyceride levels, suppressing sugar absorption, suppressing increases in blood glucose levels, and reducing body fat or BMI, as well as from the perspective of taste when orally ingested, the proportion of gallic acid in the oral composition of the present invention is preferably from 0.001% to 96% by mass of the solid content of the composition, more preferably from 0.001% to 90% by mass, even more preferably from 0.005% to 80% by mass, and particularly preferably from 0.01% to 70% by mass. Note that, in this specification, the term "solid content" refers to the content in the composition when the composition is solid, and refers to the total amount of all components in the composition excluding water when the composition is liquid or fluid.

The amount of gallic acid in the composition of the present invention can be measured by HPLC. For example, a Unison UK-C18 (HT 3 μm φ3 × 100 mm) manufactured by Imtakt Ltd. can be used, with a 1% formic acid aqueous solution as mobile phase A and a 1% formic acid acetonitrile solution as mobile phase B, a column temperature of 45°C, and a flow rate of 0.7 ml/min. The gradient conditions can be as follows. Note that, during measurement, appropriate treatments, such as removing impurities from the sample, may be performed as needed to match the resolution of the instrument.

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

2. Catechins The composition of the present invention further contains catechins in order to further enhance the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglyceride levels, suppression of increase in sugar absorption, suppression of increase in blood glucose levels, reduction of body fat, or reduction of BMI. As used herein, "catechins" collectively refers to non-gallate catechins selected from the group consisting of catechin, gallocatechin, epicatechin, and epigallocatechin, as well as gallate catechins selected from the group consisting of catechin gallate, gallocatechin gallate, epicatechin gallate, and epigallocatechin gallate. The content of catechins in this specification refers to the total amount of the above-mentioned eight types of compounds. In the present invention, when catechins are hydrates, the amount of catechins referred to in this specification is calculated on an anhydrous basis.

The catechins used in the present invention are not particularly limited as long as they are suitable for use in food products, and plant-derived catechins or synthetic catechins can be used. When plant-derived catechins are used in the composition of the present invention, plant extracts or crushed powders may be used as the catechin source, or purified products thereof may also be used. Examples of plants from which catechins can be derived include acacia catechu, green tea, cocoa beans, and apples.

In the present invention, the inventors believe that catechins are auxiliary ingredients that enhance the effects of gallic acid. In order for both ingredients to exert their effects, the mass ratio of gallic acid to catechins in the composition of the present invention must be 1:0.1-5 (gallic acid:catechins). As shown in the examples described below, in the present invention, the use of catechins can effectively enhance the functions of gallic acid compared to a combination of gallic acid and a component other than catechins (e.g., ascorbic acid, erythorbic acid) without the inclusion of catechins. Furthermore, by maintaining the mass ratio of gallic acid to catechins within this range (gallic acid:catechins = 1:0.1-5), compared to a ratio outside this range, functions related to anti-obesity, suppression of fat absorption, suppression of increases in triglyceride levels, suppression of sugar absorption, suppression of increases in blood glucose levels, reduction of body fat, and reduction of BMI can be effectively enhanced.

In the present invention, from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of increases in triglyceride levels, inhibition of sugar absorption, inhibition of increases in blood glucose levels, reduction of body fat, and reduction of BMI, the mass ratio of gallic acid to catechins in the composition is preferably gallic acid:catechins = 1:0.2-2.5, more preferably gallic acid:catechins = 1:0.2-2.0, even more preferably 0.3-1.5, and particularly preferably 0.4-1.0.

From the perspective of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increases in triglyceride levels, suppression of sugar absorption, suppression of increases in blood glucose levels, and reduction of body fat or BMI, the catechins used in the present invention preferably have a ratio C1:C2 of the non-gallate catechin content C1 to the gallate catechin content C2 of 1:0.01-13, more preferably 0.05-7.

From the viewpoint of further enhancing the functions of 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 or reduction of BMI, gallocatechin (GC) preferably accounts for 0 to 20% by mass, more preferably 0 to 10% by mass, of the catechins.
It is preferable that the catechins account for 95% by mass, and more preferably 0.1 to 90% by mass. Furthermore, among the catechins, catechin (C) preferably accounts for 0.01 to 40% by mass, and more preferably 0.1 to 20% by mass. Furthermore, among the catechins, epicatechin gallate (ECG) preferably accounts for 0.01 to 40% by mass, and more preferably 0.1 to 20% by mass. Among the catechins, epigallocatechin gallate (EGCG) preferably accounts for 0.1 to 70% by mass, and more preferably 0.5 to 60% by mass. Among the catechins, gallocatechin gallate (GCG) preferably accounts for 0.01 to 30% by mass, and more preferably 0.1 to 20% by mass. Among the catechins, epicatechin (EC) preferably accounts for 0.01 to 95% by mass, and more preferably 0.1 to 90% by mass. Of the catechins, catechin gallate (CG) preferably accounts for 0 to 40% by mass, more preferably 0 to 20% by mass. In addition, the catechins used in the present invention preferably have a total content of epigallocatechin (EGC) and epicatechin (EC) of 20% by mass or more, more preferably 30% by mass or more.

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 increases in triglyceride levels, suppression of sugar absorption, suppression of increases in blood glucose levels, reduction of body fat, or reduction of BMI, the oral composition preferably contains 0.001% by mass or more of catechins, more preferably 0.005% by mass or more, and even more preferably 0.01% by mass or more of catechins based on the solid content of the oral composition. Furthermore, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increases in triglyceride levels, suppression of sugar absorption, suppression of increases in blood glucose levels, reduction of body fat, or reduction of BMI, the oral composition preferably contains 85% by mass or less of catechins, more preferably 70% by mass or less, even more preferably 60% by mass or less, and particularly preferably 40% by mass or less of catechins.

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 Chemicals Evaluation and Research Institute, Japan can be used, with 0.1 M aqueous acetic acid as mobile phase A and 0.1 M acetic acid/acetonitrile as mobile phase B, at a column temperature of 40°C and a flow rate of 1.0 ml/min. The gradient conditions can be as follows: During measurement, samples may be treated as needed, such as by removing impurities, to match the resolution of the instrument.

Column: L-Column ODS 3 μm, 4.6 × 250 mm (Chemicals Evaluation and Research Institute, Japan)
Column temperature: 40°C
Injection volume: 10μL
Flow rate: 1.0 mL/min
Measurement wavelength: 280 nm
Mobile phase A: 0.1 M acetic acid solution Mobile phase B: 0.1 M acetic acid solution in acetonitrile

3. Ellagic Acid From the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increase in triglyceride levels, suppression of sugar absorption, suppression of increase in blood glucose levels, and reduction of body fat or BMI, the oral composition of the present invention preferably contains at least ellagic acid, more preferably ellagic acid and chebulic acid, in addition to gallic acid and catechins.

The composition of the present invention preferably contains ellagic acid. Ellagic acid is a natural _phenolic compound and is represented _{by C14H6O8} .
The ellagic acid used in the present invention is not particularly limited as long as it is suitable for use as a food product, and plant-derived ellagic acid or synthetic ellagic acid can be used. When plant-derived ellagic acid is used in the composition of the present invention, the ellagic acid source may be a plant extract or pulverized powder, or a purified product thereof. When plant-derived ellagic acid is used, examples of the plant from which it is derived include strawberry, raspberry, and pomegranate. Furthermore, the ellagic acid used in the present invention may be an anhydride or a hydrate such as a monohydrate. Furthermore, ellagic acid may be in the form of a salt. When a salt of ellagic acid is used in the present invention, examples include alkali metal ellagic acid salts. Note that, in the present invention, when ellagic acid is a hydrate, the amount of ellagic acid referred to in this specification is calculated as an anhydride. In the present invention, when a salt is used as ellagic acid, the amount of ellagic acid referred to in this specification is calculated as an ellagic acid equivalent.

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 increases in triglyceride levels, inhibition of sugar absorption, inhibition of increases in blood glucose levels, reduction of body fat, or reduction of BMI, the oral composition of the present invention preferably 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.

When the oral composition of the present invention contains ellagic acid, from the viewpoint of further enhancing the functions related to anti-obesity, suppression of fat absorption, suppression of increases in triglyceride levels, suppression of sugar absorption, suppression of increases in blood glucose levels, and reduction of body fat or BMI, the oral composition of the present invention preferably 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 more, 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.

From the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of increases in triglyceride levels, inhibition of sugar absorption, inhibition of increases in blood glucose levels, and reduction of body fat or BMI, the proportion of ellagic acid in the oral composition of the present invention is preferably from 0.00001% to 40% by mass, more preferably from 0.00005% to 30% by mass, and even more preferably from 0.0001% to 25% by mass, of the solid content of the oral composition.

The amount of ellagic acid in the composition of the present invention can be measured by HPLC. For example, a Unison UK-C18 (HT 3 μm φ3 × 100 mm) manufactured by Imtakt Corporation can be used, with a 1% formic acid aqueous solution as mobile phase A and a 1% formic acid acetonitrile solution as mobile phase B, a column temperature of 45°C, and a flow rate of 0.7 mL/min. The gradient conditions can be as follows. Note that, during measurement, appropriate treatments, such as removing impurities from the sample, may be performed as needed to match the resolution of the instrument.

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

4. Chebulic Acid: The oral composition of the present invention preferably further contains chebulic acid to further enhance its functions related to anti-obesity, suppression of fat absorption, suppression of increases in triglyceride levels, suppression of increases in sugar absorption, suppression of increases in blood glucose levels, and reduction of body fat or _BMI . Chebulic acid is a compound represented by the molecular formula _C14H12O11 . Known chebulic acids have the following chemical structure (1). The chebulic acid used in _the present invention is not particularly limited as long as it is suitable for use as a food product, and plant-derived chebulic acid or synthetically obtained chebulic acid can be used. When plant-derived chebulic acid is used in the composition of the present invention, plant extracts or crushed powders may be used as the chebulic acid source, or purified products thereof may also be used. The inventors believe that when the composition of the present invention contains chebulic acid, chebulic acid serves as an auxiliary ingredient that enhances the effects of gallic acid. Chebulic acid may be anhydrous or hydrated. Chebulic acid may also 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 may be used. In the present invention, when chebulic acid is a hydrate, the amount of chebulic acid referred to in this specification is calculated as an anhydride. In the present invention, when a salt is used as chebulic acid, the amount of chebulic acid referred to in this specification is calculated as a chebulic acid.

When the oral composition of the present invention contains chebulic acid, the amount of chebulic acid is not limited, but from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of increases in triglyceride levels, inhibition of sugar absorption, inhibition of increases in blood glucose levels, reduction of body fat, or reduction of BMI, it is preferable that the oral composition of the present invention contain 0.01 parts by mass or more of chebulic 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 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 chebulic 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.

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 increases in triglyceride levels, inhibition of sugar absorption, inhibition of increases in blood glucose levels, reduction of body fat, or reduction of BMI, it preferably contains 0.01 part by mass or more of chebulic acid per 1 part by mass of the total of gallic acid and catechins, more preferably 0.02 part by mass or more, even more preferably 0.05 part by mass or more, and particularly preferably 0.1 part by mass or more. Furthermore, the oral composition of the present invention preferably contains 5 parts by mass or less of chebulic 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.

When chebulic acid is contained in the oral composition of the present invention, from the viewpoint of further enhancing the functions related to anti-obesity, inhibition of fat absorption, inhibition of increase in triglyceride levels, inhibition of sugar absorption, inhibition of increase in blood glucose levels, reduction of body fat, or reduction of BMI, the content of chebulic acid 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, of the solid content of the oral composition.

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

Column: Imtakt Unison UK-C18 HT 3 μm φ3 × 100 mm
Column temperature: 45°C
Injection volume: 2μL
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

5. Oral Composition The oral composition of the present invention may contain components other than gallic acid, catechins, ellagic acid, and chebulic acid, to the extent that the components do not inhibit the expression of functions related to anti-obesity, suppression of fat absorption, suppression of increases in triglyceride levels, suppression of sugar absorption, suppression of increases in blood glucose levels, reduction of body fat, or reduction of BMI. Examples of such components include sugars, vitamins, minerals, proteins, dietary fiber such as insoluble dietary fiber, plants or processed plant products, and yeast. If necessary, the oral composition may further contain sweeteners, acidulants, colorants, thickeners, glazing agents, lubricants, excipients, anti-caking agents, nutritional supplements, binders, lubricants, stabilizers, diluents, bulking agents, emulsifiers, food additives, seasonings, and the like, which are commonly used in the food industry.

Examples of the oral composition of the present invention include tablets, capsules, powders, granules, liquids, granules, rods, plates, blocks, solids, pills, pastes, creams, caplets, gels, chewable tablets, and sticks. Among these, tablets, capsules, powders, granules, and liquids are preferred from the standpoint of ease of administration.

Specific examples of the oral composition of the present invention include pharmaceuticals (including quasi-drugs) and food and beverage products. Among these, food and beverage products are particularly preferred, as they can be easily ingested in daily life.

The foods and beverages of the present invention include so-called health foods, such as general foods, foods with nutrient function claims, foods for specified health uses that have been approved by designated organizations for efficacy claims, and foods with functional claims. Foods that display efficacy claims are sometimes collectively referred to as "health functional foods" or "functional foods."

The foods and beverages of the present invention are not particularly limited, but examples include milk and dairy products; beverages such as soft drinks, fruit juice drinks, dairy drinks, alcoholic drinks, sports drinks, and energy drinks; seasonings; alcoholic beverages; processed agricultural and forestry products; confectioneries and breads; flour and noodles; processed seafood products; processed livestock products; oils and fats; cooked frozen foods; retort foods; instant foods; food ingredients; and supplements. Examples of the form of supplements include tablets, capsules, powders, granules, and liquids.

6. Oral Compositions Used for Inhibiting Fat Absorption, etc. As will be apparent from the Examples below, 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 suitable for one or more applications selected from (1) inhibition of fat absorption, (2) inhibition of an increase in triglyceride levels, (3) inhibition of sugar absorption, (4) inhibition of an increase 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. That is, the oral composition of the present invention can be used as (1) a composition for inhibiting fat absorption, (2) a composition for inhibiting an increase in triglyceride levels, (3) a composition for inhibiting sugar absorption, (4) a composition for inhibiting an increase 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).

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

By ingesting the oral composition of the present invention, 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 neutral fats. Dietary neutral fats are broken down by lipase into fatty acids and glycerol, which are easily absorbed by the body. The fatty acids and glycerol are then absorbed by the small intestinal villus epithelial cells. The absorbed fatty acids and glycerol are then resynthesized into neutral fats, which are then transported into the bloodstream via the lymph.
As will be seen from the examples described below, ingestion of the oral composition of the present invention inhibits lipase activity. Therefore, the breakdown of dietary triglycerides into fatty acids and glycerol is suppressed, thereby reducing the amounts of fatty acids and glycerol absorbed by small intestinal villus epithelial cells. In other words, (1) fat absorption is suppressed. Furthermore, the amounts of fatty acids and glycerol resynthesized into triglycerides are reduced, thereby (2) suppressing the rise in triglyceride levels. As a result, (5) fat accumulation in the body is prevented (anti-obesity), and (6) body fat is reduced. As body fat is reduced, weight loss is achieved, and (7) BMI is also reduced.

Furthermore, by taking the oral composition of the present invention, isomaltase activity in the body is inhibited.
Isomaltase is a type of α-glucosidase, a disaccharidase present in the small intestinal mucosa that breaks down disaccharides into monosaccharides. When sugars contained in food reach the small intestine, they are broken down by the action of enzymes into easily absorbed monosaccharides (such as glucose), which are then absorbed through the small intestinal mucosa and transported to the liver, from which they are transported into the blood. When the concentration of glucose in the blood rises, insulin converts glucose into triglycerides, which are then stored in fat cells.
When isomaltase activity is inhibited, the breakdown of disaccharides into monosaccharides is suppressed, thereby reducing the amount of easily absorbed monosaccharides, (3) suppressing the amount of sugar absorbed in the small intestine. Furthermore, the amount of glucose absorbed in the small intestine after a meal is reduced, (4) suppressing the rise in blood glucose levels. Suppressing the rise in glucose concentration inhibits the conversion of glucose to neutral fats by the action of insulin, (5) preventing or suppressing the accumulation of fat in the body (anti-obesity), and (6) reducing body fat. The reduction in body fat leads to weight loss, and (7) a reduction in BMI.

Furthermore, the oral composition of the present invention can be suitably used for inhibiting lipase, α-glucosidase, and isomaltase. That is, the oral composition of the present invention can be used as a lipase inhibitory composition, an α-glucosidase inhibitory composition, or an isomaltase inhibitory composition.

From the standpoint of reliably achieving the anti-obesity effects, the fat absorption inhibitory effect, the triglyceride increase inhibitory effect, the sugar absorption inhibitory effect, the blood glucose increase inhibitory effect, the body fat reduction effect, and the BMI reduction effect, 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, the total amount of gallic acid and catechins that is orally ingested is preferably 10 to 400 mg, and more preferably 20 to 380 mg.

When 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 the product can be distinguished from other products in that it is used for any of the functions (1) to (7). For example, the scope of the present invention includes a product in which any of the functions (1) to (7) is indicated on the product itself, packaging, instructions, or promotional materials (advertising media). Oral compositions used for any of the functions (1) to (7) of the present invention may indicate gallic acid as an active ingredient, but are not limited to products in which gallic acid is indicated as an active ingredient on the product packaging, etc. For example, products in which the active ingredient is not specified may also be used. Furthermore, even general foods that are manufactured and sold with a suggested use are included within the scope of the present invention. For example, foods sold with personal testimonials from people who have taken the food, mentioning the maintenance and/or improvement of any of the functions (1) to (7) as their personal impressions, posted on a website, etc., are also included within the scope of the present invention. The scope of the present invention also includes functional foods that use papers or other documents demonstrating the maintenance and/or improvement of any of the functions (1) to (7) as scientific evidence of their functionality, contain gallic acid as a functional component, and notify the public of the functionality related to any of the functions (1) to (7). As mentioned above, in the present invention, components other than gallic acid are supplementary components used to enhance the effects of gallic acid, and therefore are not generally listed as components involved in functional foods or foods for specified health uses that claim any of the functions (1) to (7). However, oral compositions used for any of the functions (1) to (7) in the present invention do not exclude those that list supplementary components such as catechins or ellagic acid as components involved, and functional foods that list catechins or other components as components involved are also included in such oral compositions.

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

(1) A label indicating that a food or beverage is a functional food that has been notified to the Consumer Affairs Agency and that the business operator is responsible for displaying on the product packaging, based on scientific evidence, that the food or beverage has anti-obesity properties, fat absorption inhibitory properties, neutral fat increase inhibitory properties, sugar absorption inhibitory properties, blood sugar increase inhibitory properties, and body fat reduction properties and/or BMI reduction properties.
(2) A statement that the food or beverage is a food for specified health use that has been approved by the Consumer Affairs Agency to display on the product package, based on scientific evidence, that it has anti-obesity properties, fat absorption inhibitory properties, neutral fat increase inhibitory properties, sugar absorption inhibitory properties, blood sugar increase inhibitory properties, and body fat reduction properties and/or BMI reduction properties.

Examples of such claims include claims that appeal to people concerned about body fat, such as those concerned about obesity, those concerned about their stomach area, those concerned about their weight, and those concerned about abdominal fat (visceral fat, subcutaneous fat, etc.); claims that help lose weight, help reduce abdominal fat (visceral fat and subcutaneous fat, etc.), help reduce waist circumference, support obesity reduction, support dieting, make fat reduction easier, reduce fat absorption, help reduce or inhibit the increase of body fat, and claims that suppress blood sugar rise, suppress sugar absorption, moderate blood sugar rise, suppress postprandial blood sugar rise, moderate postprandial blood sugar rise, suppress triglyceride absorption, suppress triglyceride rise, moderate triglyceride rise, suppress postprandial triglyceride rise, suppress the absorption of sugar and fat contained in food, etc.

The present invention provides the following:
<1>
An oral composition containing gallic acid and catechins,
An oral composition, wherein the mass ratio of gallic acid to catechins in the composition is 1:0.1-5.
<2>
The oral composition according to <1> or <2>, further comprising ellagic acid.
<3>
The oral composition according to <1> or <2>, wherein the content of ellagic acid is 0.01 parts by mass or more and 0.7 parts by mass or less per 1 part by mass of gallic acid.
＜4＞
The oral composition according to at least one of the above items <1> to <3>, further comprising chebulic acid.
<5>
The oral composition according to at least one of the above items <1> to <4>, which is used for one or more purposes 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.
<6>
The oral composition according to at least one of the above items <1> to <5>, which is for suppressing postprandial increase in neutral fat or postprandial increase in blood glucose level.
＜７＞
The oral composition according to at least one of the above items <1> to <5>, which is for inhibiting lipase or α-glucosidase.
＜8＞
An oral composition containing gallic acid as an active ingredient,
It also contains catechins,
a mass ratio of gallic acid to catechins in the composition is gallic acid:catechins=1:0.1 to 1:5;
An oral composition used for one or more purposes selected from anti-obesity, inhibition of fat absorption, inhibition of increase in neutral fat, inhibition of sugar absorption, inhibition of increase in blood sugar level, reduction of body fat, and reduction of BMI.
＜９＞
A food or drink containing gallic acid as an active ingredient,
It also contains catechin acid,
a mass ratio of gallic acid to catechins in the food or drink is gallic acid:catechins=1:0.1 to 5;
A food or drink that is labeled as having one or more functions selected from the group consisting of anti-obesity function, fat absorption suppression function, neutral fat increase suppression function, sugar absorption suppression function, blood sugar level increase suppression function, body fat reduction function, and BMI reduction function.
<10>
The food or drink according to <9>, which is a functional food or a food for specified health uses.

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 mean "parts by mass" and "%" means "% by mass."

In the examples and comparative examples, a gallic acid reagent (anhydrous, powdery, purity of approximately 100% by mass) was used as the gallic acid. A purified tea-derived catechin was used as the catechin. An ellagic acid reagent (anhydrous, powdery, purity of 98% by mass or more) was used as the ellagic acid. An anhydrous, powdery, purity of 98% by mass or more was used as the chebulic acid.
As the ascorbic acid, L(+)-sodium ascorbate was used, and as the erythorbic acid, sodium erythorbate (monohydrate) was used.

[Comparative Examples 1 to 9 and Examples 1 to 12: Isomaltase Inhibition Test]
Test substances in Comparative Examples 1 to 9 and Examples 1 to 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 the raw materials used are as shown in Tables 1 and 2.

The following isomaltase inhibition tests were conducted on the test substances in Comparative Examples 1 to 9 and Examples 1 to 12.

<Isomaltase inhibition test>
(1) 100 mg of rat intestinal acetone powder (manufactured by SIGMA) was mixed with 900 μL of 56 mM maleic acid buffer (pH 6.0) and homogenized to prepare a mixture. The mixture 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) A substrate solution was prepared by dissolving isomaltose in 56 mM maleic acid buffer (pH 6.0) to a concentration of 5 mM.
(3) A test substance solution was prepared by dissolving the test substance in a 10% DMSO solution so that the total amount of the test substance was 0.32 mg/mL.
(4) 15 μL of the enzyme solution was added to 15 μL of the test substance solution, and the mixture was pre-incubated at 37° C. for 5 minutes. Then, 90 μL of the substrate solution was added, and the mixture was incubated at 37° C. for 30 minutes to allow the reaction to proceed.
(5) After the reaction, the enzyme reaction was stopped by treating at 98°C for 2 minutes.
(6) After the reaction was stopped, the absorbance at 505 nm was measured using Glucose Test Wako (manufactured by 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 the isomaltase inhibitory activity was repeated, and the absorbance of the test solution was measured to obtain a measurement value B.
(8) The procedure for measuring the isomaltase inhibitory activity described above was repeated, except that an enzyme solution heat-inactivated by treatment at 98°C for 2 minutes was used instead of the enzyme solution, and the absorbance of the test solution was measured to obtain the measurement value C.
(9) The procedure was the same as that for measuring activity described above, except that a 10% DMSO solution was used instead of the test substance solution and an enzyme solution heat-inactivated by treatment at 98°C for 2 minutes was used instead of the enzyme solution, and the absorbance of the test solution was measured to obtain the measurement value D.
(10) The isomaltase inhibition rate (% of control) was calculated using the following formula (1) from the measured values A, B, C, and D. The results are shown in Tables 1 to 3.

Isomaltase inhibition rate (% of control) = (measured value A - measured value C) / (measured value B - measured value D) × 100 (1)

As is clear from Tables 1 to 3, Examples 1 to 12, in which the ratio of gallic acid to catechins was gallic acid:catechins = 1:0.1 to 5, had significantly higher isomaltase inhibition rates than Comparative Examples 1 to 6, in which the raw materials were used alone. As a result of this improved effect, the decomposition of disaccharides to monosaccharides is suppressed in the present invention, and it is expected that the effects of suppressing sugar absorption, suppressing increases in blood glucose levels, anti-obesity, reducing body fat, and reducing BMI will be effectively achieved. Such a synergistic effect was not achieved in Comparative Examples 7 to 9, in which gallic acid was used in combination with antioxidant components other than catechins.
In particular, it can be seen that the isomaltase inhibition rate differs depending on the ratio of gallic acid to catechins among Examples 1 to 8, and that there is a preferred range of gallic acid to catechins for increasing the isomaltase inhibition rate.

Furthermore, Examples 9, 10, and 11, which used a combination of gallic acid, catechins, and ellagic acid, had a similar mass ratio of catechins to 1 part by mass of gallic acid, but had a higher isomaltase inhibition rate than Examples 2 and 7, which did not contain ellagic acid. This suggests that this combination further suppresses the breakdown of disaccharides into monosaccharides in the intestinal tract, thereby providing even more pronounced effects such as suppressing sugar absorption, preventing increases in blood sugar levels, preventing obesity, reducing body fat, and reducing BMI.

Furthermore, in Example 12, which used a combination of gallic acid and catechins with ellagic acid and chebulic acid, the mass ratio of catechins and the mass ratio of ellagic acid to 1 part by mass of gallic acid were 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, this combination further suppresses the breakdown of disaccharides into monosaccharides in the intestinal tract, suggesting that the effects of suppressing sugar absorption, suppressing blood sugar level increases, anti-obesity, reducing body fat, and reducing BMI are even more pronounced.

[Comparative Examples 10 to 18 and Examples 13 to 22: Lipase Inhibitory Activity Test]
Test substances in Comparative Examples 10 to 15 and Examples 13 to 22 were prepared using the raw materials listed in Tables 4 to 6. When multiple raw materials were used, the test substances were prepared by mixing the multiple raw materials. The amounts of the raw materials used are as shown in Tables 4 to 6.

The following lipase inhibition tests were conducted on the test substances in Comparative Examples 10-18 and Examples 13-22.

<Lipase inhibitory activity test>
Lipase inhibitory activity was measured according to the method of Lipase Kit S (Sumitomo Bakelite Co., Ltd.). Specifically, the lipase inhibitory activity of the test substance was measured according to the following procedure. The substrate of Lipase Kit S is known to be highly reactive 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, this 0.3 mg/mL lipase solution was diluted 5-fold with 0.01 M phosphate buffer (pH 7.0) to prepare a 0.06 mg/mL lipase solution.
(2) A test substance solution was prepared by dissolving the test substance in Tris-HCl buffer (pH 8.55) containing 2.5% DMSO so that the total amount of the test substance was 0.264 mg/mL.
(3) 6 μL of the test substance solution, 80 μL of the color-developing solution included in the kit, 10 μL of the lipase solution, and 1.6 μL of the esterase inhibitor solution were mixed and pre-incubated at 37°C for 5 minutes. After that, 8 μL of the substrate solution included in the kit was added and further incubated at 37°C for 30 minutes.
(4) Then, 160 μL of the reaction stop solution included in the kit was added to the mixture and mixed. After that, the absorbance at 412 nm was measured to determine the lipase inhibitory activity, and a measurement value A was obtained.
(5) The procedure was the same as that of the above-mentioned lipase inhibitory activity measurement test, except that 2.5% DMSO-containing Tris-HCl buffer (pH 8.55) was used instead of the test substance solution, and the absorbance of the test solution was measured to obtain a measurement value B.
(6) After the addition of the reaction stopping solution, the procedure was the same as that of the above-mentioned lipase inhibitory activity measurement test, except that the substrate solution was added, and the absorbance of the test solution was measured to obtain a measurement value C.
(7) The procedure was the same as that of the above-mentioned lipase inhibitory activity measurement test, except that a 2.5% DMSO-containing Tris-HCl buffer solution (pH 8.55) was used instead of the test substance solution, and the substrate solution was added after the addition of the reaction stop solution. The absorbance of the test solution was measured, and the measurement value D was obtained.
(8) The lipase inhibition rate (% of control) was calculated using the following formula (2) from the measured values A, B, C, and D. The results are shown in Tables 4 to 6.

Lipase inhibition rate (% of control) = (measured value A - measured value C) / (measured value B - measured value D) × 100 (2)

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 significantly improved lipase inhibition rates compared to Comparative Examples 10 to 15, in which the raw materials were used alone. As a result of this improved effect, the decomposition of triglycerides into fatty acids and glycerol is inhibited, suppressing fat absorption into the body. This is expected to result in improved effects such as suppression of fat absorption, suppression of increases in triglyceride levels, anti-obesity, body fat reduction, and BMI reduction. Such excellent effects were not achieved in Comparative Examples 16 to 18, in which gallic acid was used in combination with antioxidant components other than catechins, or in Comparative Example 19, in which the gallic acid and catechin contents were outside the ranges of the present invention.
It was not performed.
In particular, among Examples 13 to 18, the lipase inhibition rate differs depending on the ratio of gallic acid to catechins, and it is clear that there is a preferred range of gallic acid to catechins for increasing the lipase inhibition rate.

In particular, Examples 19 to 21, which used a combination of gallic acid, catechins, and ellagic acid, had a higher lipase inhibition rate than Examples 13 and 17, which did not contain ellagic acid, despite the same mass ratio of catechins to 1 part by mass of gallic acid. Therefore, it was found that Examples 19 to 21 showed that the combination of gallic acid, catechins, and ellagic acid significantly and effectively inhibited lipase activity. This suggests that the above-mentioned effects are more pronounced with this combination.

Furthermore, Example 22, which used a combination of gallic acid, catechins, ellagic acid, and chebulic acid, had the same mass ratio of catechins and ellagic acid to 1 part by mass of gallic acid as Example 19, but had a higher lipase inhibition rate than Example 19, which did not contain chebulic acid, demonstrating that these four components significantly and effectively inhibit lipase activity, including pancreatic lipase activity. This suggests that this combination exerts the aforementioned effects even more significantly.

[Examples 23 to 34]
The raw materials were mixed to obtain the proportions shown in Tables 7 and 8, and tablets (tablets for swallowing) each weighing 250 mg and having a tablet diameter of 8 mm were produced using a single punch tablet press. The punching force was 3 kN. Taking two tablets per day provided anti-obesity effects, a fat absorption inhibitory effect, an inhibitory effect on the increase in neutral fat, an inhibitory effect on the absorption of sugar, an inhibitory effect on the increase in blood glucose levels, a body fat reducing effect, and a BMI reducing effect.

Claims (2)

A food or drink containing gallic acid as an active ingredient,
It also contains catechins and chebulic acid,
a mass ratio of gallic acid to catechins in the food or drink is gallic acid:catechins=1:0.1 to 5;
Food and beverage products (excluding Triphala Rasayana) that are labeled as having one or more functions selected from the group consisting of anti-obesity, suppression of fat absorption, suppression of increase in neutral fat, suppression of sugar absorption, suppression of increase in blood sugar level, reduction of body fat, and reduction of BMI. The food or drink according to claim 1, which is a functional food or a food for specified health uses.