Oral Compositions

The oral composition of charcoal and iron, potentially with barley grass, addresses the limitations of existing bile acid excretion promoters by enhancing bile acid excretion, fat absorption inhibition, and blood cholesterol suppression, providing effective anti-obesity and disease prevention.

JP7618292B2Active Publication Date: 2025-01-21TOYO SHINYAKU KK
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Patent Information

Application Number
JP2023194855
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Filing Date
2023-11-16
Publication Date
2025-01-21
Estimated Expiration
2038-07-31

AI Technical Summary

Technical Problem

Existing bile acid excretion promoters, such as those made from immature persimmon fruit, are limited by restrictive timing and ingredient proportion requirements, necessitating a more flexible and effective composition.

Method used

An oral composition containing charcoal and iron, optionally with barley grass, to enhance bile acid excretion, fat absorption inhibition, and blood cholesterol suppression.

Benefits of technology

The composition effectively adsorbs and excretes bile acids, inhibiting fat absorption and reducing blood cholesterol levels, offering anti-obesity benefits and preventing lifestyle-related diseases.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide a new oral composition having a high bile acid excretion effect.SOLUTION: An oral composition contains charcoal, iron, and barley young leaves.SELECTED DRAWING: Figure 1
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Description

[Technical field]

[0001] The present invention relates to an oral composition having a high bile acid excretion effect. [Background technology]

[0002] Conventionally, persimmons have been known to have a bile acid excretion effect, and for example, a bile acid excretion promoter containing unripe persimmon fruit has been proposed (see Patent Document 1).

[0003] However, the bile acid excretion promoter described in Patent Document 1 is made from unripe persimmon fruit (meaning persimmon fruit picked between flowering and two weeks before ripening) as a raw material, and is characterized by a composition made by drying and powdering unripe persimmon fruit, which contains 5.5 to 10% moisture and 3.3 to 15% tannic acid.Since the picking time and part of the persimmon used, as well as the proportions of the ingredients contained, are limited, its preparation was not easy. Therefore, there is a need for new compositions that have such bile acid excretion effects. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Patent Publication No. 2008-063332 Summary of the Invention [Problem to be solved by the invention]

[0005] An object of the present invention is to provide a novel oral composition having a high bile acid excretion effect. [Means for solving the problem]

[0006] In searching for a composition having a bile acid excretion effect, the present inventors discovered that a composition containing charcoal and iron has a high bile acid excretion effect, and thus completed the present invention.

[0007] That is, the present invention is as follows. [1] An oral composition comprising charcoal and iron. [2] The oral composition according to [1] above, further comprising young barley leaves. [3] The oral composition according to [1] or [2] above, which is used for excretion of bile acids. [4] The oral composition according to any one of the above [1] to [3], which is used for inhibiting fat absorption. [5] The oral composition according to any one of the above [1] to [4], which is used for suppressing an increase in blood cholesterol. [6] The oral composition according to any one of the above [1] to [5], which is used for anti-obesity (dieting). Effect of the Invention

[0008] The oral composition of the present invention has a high bile acid excretion effect.

[0009] Furthermore, the oral composition of the present invention has a high fat absorption inhibiting effect. That is, while bile acids promote fat absorption in the intestine, the oral composition of the present invention adsorbs to bile acids in the intestine and excretes the bile acids, thereby suppressing fat absorption in the intestine.

[0010] Furthermore, the oral composition of the present invention has a high effect of suppressing an increase in blood cholesterol. That is, bile acids are produced in the liver through catabolism of cholesterol, and although some are excreted from the body in the intestines, most are reabsorbed and returned to the liver. The oral composition of the present invention adsorbs bile acids in the intestines and excretes them, thereby reducing the amount of bile acids returning from the intestines to the liver, thereby increasing the production of bile acids from cholesterol in the liver and suppressing an increase in blood cholesterol.

[0011] Furthermore, the oral composition of the present invention has a high anti-obesity effect due to the above-mentioned bile acid excretion effect, fat absorption inhibitory effect, and blood cholesterol increase inhibitory effect. [Brief description of the drawings]

[0012] [Figure 1] FIG. 2 is a graph showing the amount of bile acid adsorbed by the composition of the present invention. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0013] The oral composition of the present invention is characterized by containing charcoal and iron. In the oral composition of the present invention, charcoal and iron are used in combination, so bile acids can be effectively adsorbed and excreted. In addition, based on this bile acid excretion effect, it is possible to suppress an increase in cholesterol (LDL cholesterol) in the blood and fat absorption in the intestine. Therefore, the oral composition of the present invention is useful for preventing and / or improving obesity, as well as preventing and / or improving lifestyle-related diseases such as hyperlipidemia, arteriosclerosis, fatty liver, and cardiovascular disease.

[0014] The charcoal contained in the oral composition of the present invention is not particularly limited as long as it is edible, and examples thereof include rice husk charcoal, coconut husk charcoal, walnut husk charcoal, charcoal, bamboo charcoal, pure charcoal, activated charcoal, etc. These charcoals can be obtained, for example, by burning and carbonizing rice husks, coconut husks, walnut husks, trees such as pine, oak, Japanese oak, bamboo, cellulose extracted from these, and synthesized cellulose, and then pulverizing them. As the charcoal, rice husk charcoal, coconut husk charcoal, charcoal, bamboo charcoal, pure charcoal, and activated charcoal are preferred, and rice husk charcoal, coconut husk charcoal, pine charcoal, bamboo charcoal, and activated charcoal are particularly preferred. Activated charcoal is a porous carbon material obtained by carbonizing and activating carbonaceous materials such as rice husks, coconut husks, trees, and bamboo by heat treatment.

[0015] The iron contained in the oral composition of the present invention is not particularly limited as long as it is a compound containing iron, and examples thereof include sodium iron chlorophyllin, iron citrate, and iron pyrophosphate.

[0016] In the oral composition of the present invention, it is preferable to contain young barley leaves in addition to charcoal and iron. By containing young barley leaves, the bile acid excretion effect can be further enhanced. In addition, it becomes possible to easily take it as green juice.

[0017] Barley (Hordeum vulgare L.) is an annual or biennial herb belonging to the family Poaceae, said to be native to Central Asia, and is roughly classified into two-row barley, six-row barley, etc., depending on the panicle shape. The young barley leaves used in the oral composition of the present invention are not particularly limited as long as they are normally available, and any young barley leaves, such as two-row barley or six-row barley leaves, may be used. Any variety of young barley leaves may be used. The young barley leaves may contain young barley leaves, and may also contain other parts such as stems.

[0018] Furthermore, young barley leaves can be used as pulverized material, juice, extract, etc. Examples of pulverized material include powder and granules. The juice and extract may be in liquid form, but can also be used in paste form or as dry powder. The extract can be obtained by extraction using a suitable solvent, and examples of the solvent that can be used include water (warm water, hot water), ethanol, and aqueous ethanol.

[0019] The oral composition of the present invention may contain other green juice ingredients together with or instead of young barley leaves, such as kale, angelica tree, kumazasa, and chou-mei-so.

[0020] The oral composition of the present invention can be prepared by adding other ingredients other than those mentioned above as necessary and by a known method such as mixing. Examples of other ingredients include vitamins such as water-soluble vitamins (vitamins B1, B2, B3, B5, B6, B12, B13, B15, B17, biotin, choline, folic acid, inositol, PABA, vitamin C, vitamin P) and oil-soluble vitamins (vitamins A, D, E, K); minerals such as calcium, magnesium, phosphorus; sulfur-containing compounds contained in taurine, garlic, etc.; flavanoids or flavonoids such as hesperidin and quercetin; proteins such as collagen; peptides; amino acids; animal fats and oils; vegetable fats and oils; crushed products or extracts of animals and plants, etc.

[0021] The oral composition of the present invention has a bile acid excretion effect, a fat absorption inhibitory effect and a blood cholesterol increase inhibitory effect based on this bile acid excretion effect, and further an anti-obesity (diet) effect based on this bile acid excretion effect, fat absorption inhibitory effect, and blood cholesterol increase inhibitory effect, and can be used, for example, as so-called health foods such as pharmaceuticals (including quasi-drugs), functional foods such as specified health foods, nutrient functional foods, and functional food with functional labeling, whose efficacy has been approved by a designated organization, as well as general foods, food additives, feed, etc.

[0022] The oral composition of the present invention can be used as a composition for inhibiting fat absorption, and there is no particular limitation on such a composition for inhibiting fat absorption, so long as it contains charcoal and iron and can be distinguished from other products in terms of being used to inhibit fat absorption, and for example, the scope of the present invention includes a product that displays on the product itself, packaging, instructions, or advertising materials that it has a fat absorption inhibitory function. Note that the composition for inhibiting fat absorption of the present invention is not limited to a product that displays the combined components of the present invention (charcoal and iron) as the active ingredient for inhibiting fat absorption on the product packaging, etc., and may be one in which the active ingredient is not specified, for example.

[0023] Specifically, examples of the composition for inhibiting fat absorption of the present invention include pharmaceuticals (including quasi-drugs) and so-called health foods. Examples of so-called health foods include those labeled "inhibits fat absorption," "reduces fat absorption," "for those who want to inhibit fat absorption," etc.

[0024] The oral composition of the present invention can be used as a composition for suppressing an increase in blood cholesterol, and the composition for suppressing an increase in blood cholesterol is not particularly limited as long as it contains charcoal and iron and can be distinguished from other products in terms of being used to suppress an increase in blood cholesterol, and for example, the scope of the present invention includes a product that indicates that the product has an effect of suppressing an increase in blood cholesterol on the main body, packaging, instruction manual, or advertising material of the product of the present invention. Note that the composition for suppressing an increase in blood cholesterol of the present invention is not limited to a product that indicates on the packaging etc. of the product that the combined components of the present invention (charcoal and iron) are the active ingredients for suppressing an increase in blood cholesterol, and may be a product that does not specify the active ingredient, for example.

[0025] Specifically, examples of the composition of the present invention for suppressing an increase in blood cholesterol include pharmaceuticals (including quasi-drugs) and so-called health foods. Examples of so-called health foods include those labeled with claims such as "suppresses the increase in cholesterol," "for those concerned about cholesterol," "suppresses cholesterol absorption," and "for those with high cholesterol."

[0026] In addition, the oral composition of the present invention can be used as an anti-obesity composition for anti-obesity, and such anti-obesity composition is not particularly limited as long as it contains charcoal and iron and can be distinguished from other products as a product in that it is used for anti-obesity, and for example, the scope of the present invention includes a product that displays the function of anti-obesity on the main body, packaging, instructions, or promotional materials of the product of the present invention. Note that the anti-obesity composition of the present invention is not limited to a product that displays the combined components of the present invention (charcoal and iron) as the active ingredient for anti-obesity on the product packaging, etc., and may be a product that does not specify the active ingredient, for example.

[0027] Specifically, examples of the anti-obesity composition of the present invention include pharmaceuticals (including quasi-drugs) and so-called health foods. Examples of so-called health foods include those labeled with claims such as "for those concerned about body fat," "for those who are prone to obesity," "for those concerned about weight (BMI)," "reduce weight and abdominal fat (visceral fat and subcutaneous fat)," and "reduce waist circumference."

[0028] Examples of the form of the oral composition of the present invention include tablets, capsules, powders, granules, liquids, granules, rods, plates, blocks, solids, rounds, pastes, creams, caplets, gels, chewables, and sticks. Among these, tablets, capsules, powders, granules, and liquids are particularly preferred. Specific examples include supplements, containerized beverages filled in PET bottles, cans, bottles, etc., powders to be dissolved in water (hot water), milk, fruit juice, green juice, etc., and food additives. These are preferred because they are easy to drink during meals and can increase palatability.

[0029] The contents of charcoal and iron (the two components of the present invention) in the oral composition of the present invention may be appropriately determined within the range in which the effects thereof are exhibited.

[0030] In general, when the oral composition of the present invention is a pharmaceutical product such as a tablet or a supplement, the two components of the present invention are contained in an amount of 0.01 to 100 mass%, more preferably 0.03 to 85 mass%, and even more preferably 0.05 to 70 mass%, of the total composition calculated on a dry mass basis.

[0031] When the oral composition of the present invention is a packaged beverage, the two components of the present invention are preferably contained in an amount of 0.0001 to 50 mass%, more preferably 0.0005 to 40 mass%, and even more preferably 0.001 to 30 mass%, of the total composition.

[0032] Furthermore, when the oral composition of the present invention is a powdered beverage, the two components of the present invention are preferably contained in an amount of 0.0001 to 80 mass%, more preferably 0.0005 to 70 mass%, and even more preferably 0.001 to 60 mass%, of the total composition calculated on a dry mass basis.

[0033] Furthermore, when the oral composition of the present invention contains charcoal, iron and young barley leaves, in the case of a pharmaceutical product such as a tablet or a supplement, the three components of the present invention are preferably contained in an amount of 0.05 to 100 mass%, more preferably 0.075 to 85 mass%, and even more preferably 0.1 to 70 mass%, of the total composition calculated as a dry mass.

[0034] When the oral composition of the present invention is a packaged beverage, the three components of the present invention are preferably contained in an amount of 0.0001 to 50 mass%, more preferably 0.0005 to 40 mass%, and even more preferably 0.001 to 30 mass%, of the total composition.

[0035] Furthermore, when the oral composition of the present invention is a powdered beverage, the three components of the present invention are preferably contained in an amount of 0.0005 to 90 mass%, more preferably 0.001 to 80 mass%, and even more preferably 0.005 to 70 mass%, of the total composition calculated on a dry mass basis.

[0036] In order to more effectively exert the effects of the present invention, the three components of the present invention are preferably contained in an amount of 0.1 mass % or more of the total composition, calculated on a dry mass basis, more preferably 1 mass % or more, even more preferably 5 mass % or more, and particularly preferably 10 mass % or more.

[0037] The intake amount of the oral composition of the present invention is not particularly limited, but from the viewpoint of more significantly exerting the effect of the present invention, it is preferable to take the two components of the present invention in an amount of 5 mg / day or more, more preferably 10 mg / day or more, and even more preferably 20 mg / day or more. The oral composition of the present invention can be stored as a daily amount in one container or divided into, for example, 2 to 3 multiple containers so that the daily intake amount is the above-mentioned intake amount.

[0038] The blending mass ratio of charcoal and iron, calculated on a dry mass basis, is preferably 0.01 to 2000: 1, more preferably 0.05 to 1000: 1, and even more preferably 0.1 to 100: 1. The blending mass ratio of charcoal and iron, and young barley leaves, calculated on a dry mass basis, is preferably in the range of 0.01 to 2000: 1, more preferably 0.05 to 1000: 1, and even more preferably 0.1 to 100: 1. EXAMPLES

[0039] The present invention will be described below with reference to examples.

[0040] <Bile acid adsorption test> (Preparation of test substances) The raw materials (charcoal, iron, and young barley leaf powder) were mixed as shown in Table 1 to prepare the test substances of Comparative Examples 1 to 3 and Examples 1 and 2.

[0041] [Table 1]

[0042] (Sample preparation) The test substance was added at a concentration of 0.05% (W / V) to 6 mL of postprandial artificial intestinal fluid (FeSSIF: 15 mL of 100 mM sodium taurocholate, 284.3 mg of lecithin, 14.4 mL of 1 M acetic acid, 10.1 mL of 1 M sodium hydroxide, 17.3 mL of 1 M sodium chloride, pH 5.0) warmed to 37°C, and vortexed. The mixture was then warmed in a 37°C incubator while shaking at 100 rpm for 30 minutes. As a control, 6 mL of postprandial artificial intestinal fluid was warmed in a 37°C incubator while shaking at 100 rpm for 30 minutes.

[0043] After warming for 30 minutes, the mixture was centrifuged at 2000 rpm for 10 minutes.

[0044] 3 mL of the supernatant was taken without sucking up the precipitate (test substance), and an equal volume of ethyl acetate was added to the supernatant, vortexed for 30 seconds, and then centrifuged at 2000 rpm for 10 minutes.

[0045] The upper layer (1.5 mL) of the liquid was transferred to a new centrifuge tube and evaporated to dryness using a centrifugal evaporator.

[0046] 600 μL of 2-propanol was added to the dried product, which was then vortexed for 10 seconds, and then suspended by ultrasonication for 10 minutes.

[0047] Thereafter, the mixture was centrifuged at 800 rpm for 3 minutes, and the supernatant was collected in a 1.5 mL tube to obtain a sample.

[0048] (Measurement of bile acid concentration) The bile acid concentration in the sample was measured using a Wako Total Bile Acid Test in the following manner.

[0049] 62.5 μL of enzyme solution was added to 25 μL of sample, mixed thoroughly, and then heated at 37° C. for 10 minutes. 62.5 μL of reaction stop solution was then added, mixed thoroughly, and the absorbance at 560 nm was measured. In addition, 62.5 μL of blank enzyme solution was added to 25 μL of sample, and reacted in the same manner to serve as a sample blank.

[0050] 62.5μL of enzyme solution was added to 25μL of 2-propanol solution in which the concentration of glycocholic acid was adjusted to 10, 20, 30, 40, or 50μmol / L, and the mixture was mixed well and then heated at 37℃ for 10 minutes. Then, 62.5μL of reaction stop solution was added, mixed well, and the absorbance at 560nm was measured to create a calibration curve. In addition, 62.5μL of blank enzyme solution with no activity was added to 25μL of 2-propanol solution in which the concentration of glycocholic acid was adjusted to 10μmol / L, and the mixture was reacted in the same manner as above, and this was used as the blank standard solution.

[0051] The bile acid concentration (μmol / L) of the sample was determined from the calibration curve and converted into a relative value (%) with the control taken as 100%, and the amount of adsorption was calculated from the relative value.

[0052] The results are shown in Figure 1.

[0053] As shown in Figure 1, it was found that the combination of charcoal and iron improved the amount of bile acid adsorption compared to the addition of charcoal or iron alone. Also, as shown in Figure 1, it was found that the combination of charcoal and iron with young barley leaves synergistically increased the adsorption of bile acids.

[0054] [Production Example 1] (Production of tablets) Tablets were prepared from the following ingredients: The resulting composition was expected to have bile acid adsorption properties.

[0055] Charcoal powder (from bamboo) 0.08% Iron Chlorophyll 0.0001% Barley grass powder 0.04% Vitamin 5% Silicon dioxide 6% Maltose 55.5799% Reduced maltose 0.3% Hydroxypropyl cellulose 15% Calcium stearate 3% Hydroxypropyl methylcellulose 15%

[0056] [Production Example 2] (Production of Granules) Granules containing the following ingredients were prepared. The resulting composition was expected to have bile acid adsorption properties.

[0057] Charcoal powder (derived from coconut shells) 70% Iron Chlorophyll 20% Barley grass powder 2.25% Calcium stearate 1.5% Dolomite 6.25% [Production Example 3] (Production of powdered beverage) A powdered beverage was prepared from the following ingredients: The resulting composition was expected to have bile acid adsorption properties.

[0058] Charcoal powder (derived from rice husk) 0.02% Iron Chlorophyll 0.16% Barley leaf extract powder 1% Vitamin 3% Reduced maltose 35.82% Resistant dextrin 60% [Industrial Applicability]

[0059] INDUSTRIAL APPLICABILITY The oral composition of the present invention has a high bile acid excretion effect and is therefore industrially useful.

Claims

[Claim 1] An oral composition for anti-obesity comprising charcoal, iron and young barley leaves.

Citation Information

Patent Citations

  • Immature persimmon fruit powder composition and method for producing the same

    JP2008063332A

  • JPP6999175B

  • JPP7393026B