tablet

Combining Salacia plant extracts with specific compounds enhances tablet disintegration, ensuring easier absorption and effective physiological function.

JP2026067266APending Publication Date: 2026-04-20KOBAYASHI PHARMA CO LTD
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
KOBAYASHI PHARMA CO LTD
Filing Date
2024-10-08
Publication Date
2026-04-20

AI Technical Summary

Technical Problem

Tablets containing Salacia plant extracts face disintegration issues, leading to poor absorption in the body.

Method used

Combining Salacia plant extracts with γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract improves disintegration properties.

Benefits of technology

The tablets exhibit enhanced disintegration, allowing easier absorption of Salacia plant extracts and effective physiological function exertion.

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Abstract

The purpose of this disclosure is to provide tablets containing an extract of a plant of the genus Salacia, with improved disintegration properties. [Solution] The tablets of the present disclosure contain (A) an extract of a plant of the genus Salacia, and (B) at least one selected from the group consisting of γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract.
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Description

Technical Field

[0001] The present disclosure relates to tablets containing an extract of plants of the genus Salacia and having improved disintegrability.

Background Art

[0002] Plants of the genus Salacia are vine-like perennial plants of the family Celastraceae that grow in India, Sri Lanka, Thailand, Vietnam, and southern China. Components of plants of the genus Salacia are known to have an α-glucosidase activity inhibitory effect and an effect of increasing GLP-1 production, and are ingested in the form of foods and beverages in order to obtain an effect of suppressing an increase in blood glucose level and an appetite-suppressing effect based on these effects.

[0003] In oral ingestion of plants of the genus Salacia, an extract of parts such as stems, roots, and bark is concentrated and blended into foods and beverages to efficiently ingest useful components of plants of the genus Salacia. For example, in Patent Document 1, a food in the form of a tablet or capsule containing an extract of a plant of the genus Salacia having a 50% inhibitory concentration (IC50 value) of sucrase of 300 μg / ml or less has been proposed.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] Among foods and pharmaceuticals, tablets are a highly convenient and consumer-preferred dosage form because they can be ingested by drinking with water or the like without causing a feeling of the taste of functional components or the like. However, when an extract of a plant of the genus Salacia is formed into a tablet, there is a drawback that the disintegration time of the tablet becomes long and it becomes difficult to be absorbed in the body.

[0006] Therefore, the purpose of this disclosure is to provide a tablet containing an extract of a plant of the genus Salacia and having improved disintegration properties. [Means for solving the problem]

[0007] The inventors of the present invention conducted diligent research to solve the aforementioned problems and unexpectedly discovered that when an extract of a Salacia plant, which reduces the disintegration properties of tablets, is combined with at least one substance selected from the group consisting of γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract, which also reduce the disintegration properties of tablets, the disintegration properties of the tablets are improved. This disclosure was completed by further research based on this finding.

[0008] In other words, this disclosure provides inventions in the following embodiments. Item 1: A tablet containing (A) an extract of a plant of the genus Salacia, and (B) at least one selected from the group consisting of γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract. Item 2 The tablet according to Item 1, wherein, on a dry weight basis, it contains 0.01 to 20 parts by weight of component (B) per 1 part by weight of component (A). Item 3 A tablet according to item 1 or 2, wherein the content of component (A) is 1 to 80% by weight on a dry weight basis. Item 4 A tablet according to any one of items 1 to 3, wherein the content of component (B) is 0.01 to 80% by weight on a dry weight basis. Item 5 (A) A method for improving the disintegration properties of tablets containing an extract of a plant of the genus Salacia, A method for improving disintegration, comprising (A) a tablet containing an extract of a plant of the genus Salacia, and (B) at least one selected from the group consisting of γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract. [Effects of the Invention]

[0009] The tablets of this disclosure, even though they contain extracts from Salacia plants, have improved disintegration properties, making them easily absorbed in the body and allowing the physiological functions of the Salacia plant extracts to be effectively exerted. [Modes for carrying out the invention]

[0010] 1. Tablets The tablets of this disclosure contain (A) an extract of a plant of the genus Salacia (hereinafter also referred to as "component (A)") and (B) at least one selected from the group consisting of γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract (hereinafter also referred to as "component (B)"). The tablets of this disclosure will be described in detail below. In this specification, numerical ranges indicated by two numbers and "~" include those two numbers as the lower and upper limits. For example, the notation 2-15% by weight means 2% by weight or more and 15% by weight or less.

[0011] (A) Extracts from plants of the genus Salacia The tablets of this disclosure contain an extract of a plant of the genus Salacia as component (A). Tablets containing extracts of plants of the genus Salacia have the disadvantage of poor disintegration, but the tablets of this disclosure have surprisingly improved disintegration due to the inclusion of component (B).

[0012] There are no particular restrictions on the types of plants in the genus Salacia, but examples include Salacia chinensis, Salacia reticulata, Salacia oblonga, Salacia prinoides, Salacia latifolia, Salacia burunoniana, Salacia grandiflora, and Salacia macrosperma. Among these Salacia plants, Salacia chinensis is preferred.

[0013] Neocotalanol, an active ingredient found in plants of the Salacia genus, has recently attracted attention as an ingredient that slows down sugar absorption and suppresses the rise in blood glucose levels after meals. To enhance this effect, it is preferable to incorporate an extract of Salacia plants rich in neocotalanol into the tablets.

[0014] It is known that the neocotalanol content of Salacia plants varies depending on their origin. For example, Salacia plants from India and Sri Lanka typically contain around 0.1 mg / g of neocotalanol, which is a small amount. Therefore, extracts obtained using Salacia plants from India and Sri Lanka as raw materials and employing general extraction methods contain at most about 0.1% by weight of neocotalanol. However, Salacia plants from Thailand typically contain around 0.6 mg / g of neocotalanol, which is about six times more than Salacia plants from India and Sri Lanka. Therefore, using Salacia plants from Thailand as raw materials makes it easier to obtain extracts rich in neocotalanol. In this disclosure, it is preferable to use Salacia plants from Thailand as raw materials in order to obtain an extract of Salacia plants rich in neocotalanol using general extraction methods.

[0015] The part of the Salacia plant used as the raw material for component (A) in this disclosure is not particularly limited, but examples include rhizomes, leaves, fruits, bark, etc., preferably stems, roots, and bark, and more preferably stems and roots.

[0016] For the extraction process to obtain an extract from a Salacia plant, any common extraction method used in the production of plant extracts is acceptable, such as solvent extraction, supercritical fluid extraction, or steam distillation. Among these, solvent extraction is preferred.

[0017] Examples of the extraction solvent used in the solvent extraction treatment include water; lower monohydric alcohols having 1 to 4 carbon atoms such as methanol, ethanol, n-propanol, isopropanol, and n-butanol; polyhydric alcohols such as propylene glycol and 1,3-butylene glycol; hydrophilic solvents such as acetone; and mixed solvents thereof. Among these extraction solvents, water, lower monohydric alcohols, and mixed solvents thereof are preferable, water, ethanol, and mixed solvents thereof are more preferable, and water is particularly preferable.

[0018] When a mixed solvent of water and a lower monohydric alcohol is used as the extraction solvent, the content of the lower monohydric alcohol in the mixed solvent is, for example, 10 to 90% by volume, preferably 20 to 80% by volume, more preferably 20 to 60% by volume, and still more preferably 25 to 55% by volume.

[0019] The solvent extraction treatment can be carried out by immersing a part of the plant of the genus Salacia to be extracted (for example, rhizome, leaf, fruit, bark, etc.; preferably stem, root, bark; more preferably stem, root), which has been subjected to treatments such as drying, cutting, and pulverization as necessary to enhance the extraction efficiency, in the extraction solvent and stirring as necessary. The solvent extraction treatment can be carried out, for example, by immersing it in about 0.3 to 1.5 L of the extraction solvent per 100 g of the part of the plant of the genus Salacia to be extracted and performing the treatment for about 0.5 to 24 hours.

[0020] Further, the solvent extraction treatment can be carried out by heating, and the heating temperature is, for example, 60 to 110°C, preferably 80 to 100°C.

[0021] By removing solids through solid-liquid separation after extraction, an extract of Salacia plants can be obtained. The extract obtained by the extraction process may, if necessary, be subjected to a purification process by subjecting it to adsorption processes such as various chromatographies using columns filled with carriers such as filtration treatment; polystyrene gel (polystyrene-divinylbenzene copolymer, etc.), ion exchange resin, activated carbon, etc. The obtained extract is concentrated and used as the component (A). Specific forms of the component (A) include soft extract and dry extract, and preferably dry extract.

[0022] In the extract of Salacia plants used in the present disclosure, the content (in terms of dry weight) of neokotalanol is not particularly limited, but from the viewpoint of gently reducing sugar absorption and improving the effect of suppressing the rise in postprandial blood glucose levels, it is preferably 0.2% by weight or more, more preferably 0.25% by weight or more, still more preferably 0.3% by weight or more. In the extract of Salacia plants used in the present disclosure, the upper limit value of the content (in terms of dry weight) of neokotalanol is not particularly limited, but it is usually 0.5% by weight or less, and from the viewpoint of reducing the unpleasant aftertaste after taking tablets, it is preferably 0.45% by weight or less, more preferably 0.4% by weight or less. Specifically, the content (in terms of dry weight) of neokotalanol in the extract of Salacia plants used in the present disclosure is preferably 0.2 to 0.5% by weight, more preferably 0.25 to 0.45% by weight, still more preferably 0.3 to 0.4% by weight.

[0023] In the tablets of the present disclosure, the content of the component (A) may be appropriately set according to the intake amount per time, etc. For example, in terms of dry weight, it is usually 1 to 95% by weight, and from the viewpoints of improving the blood glucose level-rising inhibitory effect and appetite-suppressing effect, etc., and further improving the disintegration property of the tablets, it is preferably 1 to 80% by weight, more preferably 2 to 70% by weight, still more preferably 3 to 60% by weight, even more preferably 4 to 50% by weight, and particularly preferably 5 to 40% by weight. Since the tablets of the present disclosure contain the component (B), even if the content of the component (A) is relatively large, they have excellent disintegration properties.

[0024] (B) γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract The tablets of this disclosure contain, as component (B), at least one selected from the group consisting of γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract. Component (B) may be used alone or in combination of two or more. Although component (B) itself reduces the disintegration properties of the tablet, when combined with component (A), the disintegration properties of the tablet are surprisingly improved.

[0025] [γ-aminobutyric acid] Gamma-aminobutyric acid, also known as GABA, is a component known to exert a blood pressure-lowering effect by promoting parasympathetic nervous system activity.

[0026] The γ-aminobutyric acid used in this disclosure is not particularly limited and may be obtained by any of the following methods: extraction from plants containing γ-aminobutyric acid, microbial fermentation, enzymatic synthesis, chemical synthesis, etc.

[0027] Furthermore, the γ-aminobutyric acid used in this disclosure may be in a purified state, or it may be in the form of a plant extract containing γ-aminobutyric acid, a fermented product from which γ-aminobutyric acid has been produced, or an extract thereof.

[0028] [Equol] Equol is a substance produced when daidzein, a type of isoflavone, is metabolized by intestinal bacteria and digestive enzymes in the body. Specifically, it refers to 7-hydroxy-3-(4′-hydroxyphenyl)-chroman. Equol is known as a component that possesses estrogen-like activity.

[0029] Equol may be synthetic equol produced by the chemical reduction of daidzeins (daidzein glycosides, daidzein, and / or dihydrodaidzein), or it may be a metabolite produced by equol-producing bacteria from raw materials containing daidzeins (daidzein glycosides, daidzein, and / or dihydrodaidzein).

[0030] The raw materials containing daidzeins are not particularly limited and include, for example, plants (specifically, soybeans, kudzu, kudzu root, red globe grapes, alfalfa, etc.), processed products thereof (specifically, soybean flour, boiled soybeans, tofu, fried tofu, soy milk, soybean hypocotyls, soybean hypocotyl extracts, etc.), and fermented preparations thereof (specifically, natto, soy sauce, miso, tempeh, fermented soy beverages, etc.). Furthermore, the equol-producing bacteria can be any microorganism capable of utilizing daidzeins to produce equol, such as microorganisms belonging to the genera Lactococcus, Streptococcus, and Bacteroides.

[0031] For obtaining an extract containing equol, the general extraction methods described in the section on "Extracts from Salacia Plants" are used, but solvent extraction is preferred. The specific solvent extraction process is as described in the section on "Extracts from Salacia Plants".

[0032] In extracts containing equol, the extraction solvent used in the solvent extraction process is preferably water, a lower monohydric alcohol, or a mixture thereof, more preferably a mixture of water and a lower monohydric alcohol, and particularly preferably a mixture of water and ethanol. In the case of a mixture of water and a lower monohydric alcohol, the content of the lower monohydric alcohol is, for example, 10 to 90% by volume, preferably 20 to 80% by volume, more preferably 20 to 60% by volume, and even more preferably 25 to 55% by volume.

[0033] After the extraction process, solid matter is removed by solid-liquid separation to obtain an extract containing equol. The extract obtained from the extraction process may be purified as needed, by filtration and adsorption. The obtained extract is concentrated and used as an extract containing equol. Specific forms of the extract containing equol include soft extracts and dry extracts, with dry extracts being preferred.

[0034] In this disclosure, as equol, a product obtained by fermenting a raw material containing daidzeins with equol-producing bacteria may be used, or equol, which is a metabolite, may be isolated and purified from the fermented culture.

[0035] [Carnitine and its salts] Carnitine is a vitamin-like substance synthesized from lysine and methionine.

[0036] In this disclosure, any of L-carnitine, D-carnitine, levocarnitine, and DL-carnitine may be used as carnitine, but L-carnitine, DL-carnitine, and more preferably L-carnitine are used.

[0037] Carnitine salts are not particularly limited as long as they are edible, but examples include chloride salts; metal salts such as sodium salts, potassium salts, calcium salts, magnesium salts, and zinc salts; ammonium salts; organic acid salts such as acetate, propionate, lactate, tartrate, citrate, succinate, maleate, and fumarate; and inorganic acid salts such as hydrochloride, sulfate, and phosphate.

[0038] [Pine bark extract, Ginkgo biloba extract] Pine bark extract contains proanthocyanidins, a type of polyphenol, and is a known component that has effects such as improving blood lipid levels, antihypertensive effects, suppressing blood glucose level increases, protecting blood vessels, improving the efficiency of vitamin C utilization, and improving blood fluidity, due to the antioxidant effects of proanthocyanidins.

[0039] The type of pine tree from which pine bark is derived is not particularly limited, but examples include French maritime pine (Pinus pinaster), Finnish pine, and New Zealand pine.

[0040] As the pine bark extract, you may use one that you have prepared yourself using a known extraction method, or you may use a commercially available product. Examples of commercially available French maritime pine bark extracts include the trade names "Pycnogenol" (manufactured by Hoffer Research, Switzerland) and "Flavanogenol" (distributed by Toyo Shinyaku Co., Ltd.). An example of a commercially available Finnish pine bark extract is the trade name "Fingenol". An example of a commercially available New Zealand pine bark extract is the trade name "Enzogenol".

[0041] Examples of pine bark extracts include, specifically, sap, solvent extracts, and fractions of solvent extracts containing proanthocyanidins.

[0042] Ginkgo biloba extract is a known component obtained by extracting ginkgo leaves (Ginkgo biloba L.).

[0043] For obtaining pine bark extract and ginkgo leaf extract, the general extraction methods described in the "Extracts from Salacia Plants" section above are used, but solvent extraction is preferred. The specific solvent extraction process is as described in the "Extracts from Salacia Plants" section above.

[0044] In pine bark extract and ginkgo leaf extract, the extraction solvent used in the solvent extraction process is preferably water, a lower monohydric alcohol, or a mixture thereof; more preferably a mixture of water and a lower monohydric alcohol; and particularly preferably a mixture of water and ethanol. In the case of a mixture of water and a lower monohydric alcohol, the content of the lower monohydric alcohol is, for example, 10 to 90% by volume, preferably 20 to 80% by volume, more preferably 20 to 60% by volume, and even more preferably 25 to 55% by volume.

[0045] After the extraction process, solid matter is removed by solid-liquid separation to obtain an extract of pine bark or ginkgo leaves. The extract obtained from the extraction process may be purified as needed, by filtration and adsorption. The obtained extract is concentrated and used as pine bark extract and ginkgo leaf extract. Specific forms of pine bark extract and ginkgo leaf extract include soft extract and dried extract, with dried extract being preferred.

[0046] [Content of component (B)] In the tablets of this disclosure, the content of component (B) (total content if two or more are included) can be set appropriately according to the desired degree of improvement in disintegration, but on a dry weight basis, the content of component (B) per 1 part by weight of component (A) is usually 0.01 to 20 parts by weight, and from the viewpoint of further improving the disintegration of the tablets, it is preferably 0.03 to 15 parts by weight, more preferably 0.05 to 10 parts by weight, even more preferably 0.07 to 7 parts by weight, and even more preferably 0.08 to 5 parts by weight.

[0047] In one embodiment of the tablets of this disclosure, when component (B) is γ-aminobutyric acid, the amount of γ-aminobutyric acid per 1 part by weight of component (A) on a dry weight basis is preferably 0.03 to 15 parts by weight, more preferably 0.05 to 10 parts by weight, even more preferably 0.07 to 5 parts by weight, and even more preferably 0.08 to 3 parts by weight, from the viewpoint of further improving the disintegration properties of the tablets.

[0048] In another embodiment of the tablets of this disclosure, when component (B) is pine bark extract, the amount of pine bark extract per 1 part by weight of component (A) on a dry weight basis is preferably 0.05 to 15 parts by weight, more preferably 0.1 to 10 parts by weight, even more preferably 0.15 to 6 parts by weight, and even more preferably 0.2 to 3 parts by weight, from the viewpoint of further improving the disintegrability of the tablets.

[0049] In another embodiment of the tablets of this disclosure, when component (B) is equol, the equol content per 1 part by weight of component (A) is preferably 0.05 to 10 parts by weight, more preferably 0.08 to 8 parts by weight, even more preferably 0.1 to 5 parts by weight, and even more preferably 0.15 to 2 parts by weight, on a dry weight basis, from the viewpoint of further improving the disintegration properties of the tablets.

[0050] In another embodiment of the tablets of this disclosure, when component (B) is carnitine or a salt thereof, the amount of carnitine or a salt thereof per 1 part by weight of component (A) on a dry weight basis is preferably 0.05 to 15 parts by weight, more preferably 0.1 to 10 parts by weight, even more preferably 0.2 to 6 parts by weight, and even more preferably 0.3 to 4 parts by weight, from the viewpoint of further improving the disintegrability of the tablets.

[0051] In another embodiment of the tablets of this disclosure, when component (B) is ginkgo biloba extract, the amount of ginkgo biloba extract per 1 part by weight of component (A) on a dry weight basis is preferably 0.05 to 15 parts by weight, more preferably 0.1 to 10 parts by weight, even more preferably 0.2 to 7 parts by weight, and even more preferably 0.3 to 4 parts by weight, from the viewpoint of further improving the disintegrability of the tablets.

[0052] Furthermore, in the tablets of this disclosure, the content of component (B) (total content if two or more are included) can be appropriately set according to the desired degree of improvement in disintegration, but for example, on a dry weight basis, it is usually 0.01 to 90% by weight, and from the viewpoint of further improving the disintegration of the tablets, it is preferably 0.01 to 80% by weight, more preferably 0.1 to 70% by weight, even more preferably 0.5 to 60% by weight, even more preferably 1 to 50% by weight, and particularly preferably 2 to 40% by weight.

[0053] In one embodiment of the tablets of the present disclosure, when component (B) is γ-aminobutyric acid, the content of γ-aminobutyric acid in the tablets of the present disclosure is preferably 0.01 to 70% by weight, more preferably 0.1 to 60% by weight, even more preferably 0.5 to 50% by weight, even more preferably 1 to 40% by weight, and particularly preferably 1 to 30% by weight on a dry weight basis, from the viewpoint of further improving the disintegration properties of the tablets.

[0054] In another embodiment of the tablets of the present disclosure, if component (B) is pine bark extract, the content of pine bark extract in the tablets of the present disclosure is preferably 0.1 to 70% by weight, more preferably 0.5 to 60% by weight, even more preferably 1 to 50% by weight, even more preferably 2 to 40% by weight, and particularly preferably 3 to 30% by weight on a dry weight basis, from the viewpoint of further improving the disintegration of the tablets.

[0055] In another embodiment of the tablets of the present disclosure, where component (B) is equol, the equol content in the tablets of the present disclosure is preferably 0.1 to 70% by weight, more preferably 0.5 to 60% by weight, even more preferably 1 to 50% by weight, even more preferably 2 to 40% by weight, and particularly preferably 3 to 30% by weight on a dry weight basis, from the viewpoint of further improving the disintegration of the tablets.

[0056] In another embodiment of the tablets of the present disclosure, where component (B) is carnitine or a salt thereof, the content of carnitine or a salt thereof in the tablets of the present disclosure is preferably 0.1 to 80% by weight, more preferably 0.5 to 70% by weight, even more preferably 1 to 60% by weight, even more preferably 2 to 50% by weight, and particularly preferably 3 to 40% by weight on a dry weight basis, from the viewpoint of further improving the disintegration of the tablets.

[0057] In another embodiment of the tablets of the present disclosure, if component (B) is ginkgo biloba extract, the content of ginkgo biloba extract in the tablets of the present disclosure is preferably 0.1 to 80% by weight, more preferably 0.5 to 70% by weight, even more preferably 1 to 60% by weight, even more preferably 2 to 50% by weight, and particularly preferably 3 to 40% by weight on a dry weight basis, from the viewpoint of further improving the disintegration of the tablets.

[0058] Other ingredients In addition to the components described above, the tablets of this disclosure may contain other additives necessary for formulation into tablets, etc., to the extent that they do not interfere with the effects of this disclosure. Examples of such additives include excipients, binders, fluidizers, lubricants, disintegrants, acidulants, sweeteners, flavorings, and colorants. Specific examples of such additives include lactose, maltose, crystalline cellulose, hydroxymethylcellulose, hydroxypropylmethylcellulose, silicon dioxide, sucrose fatty acid esters, calcium stearate, and magnesium stearate. These additives may be used individually or in combination of two or more. The content of these additives may be appropriately determined depending on the type of additive used.

[0059] Furthermore, the tablets of this disclosure may contain nutritional components and pharmacological components in addition to the components described above. The nutritional components and pharmacological components are not particularly limited as long as they are usable in food and pharmaceuticals, but examples include antacids, stomachic agents, digestive agents, intestinal regulators, antispasmodics, mucosal repair agents, anti-inflammatory agents, astringents, antiemetics, antitussives, expectorants, anti-inflammatory enzymes, sedatives, antihistamines, caffeine, cardiotonic and diuretic agents, antibacterial agents, vasoconstrictors, vasodilators, local anesthetics, herbal medicines, herbal medicine extracts, amino acids, vitamins, menthol, etc. These nutritional components and pharmacological components may be used individually or in combination of two or more. The content of these components may be appropriately determined depending on the type of component used.

[0060] Physical properties of tablets The tablets of this disclosure have excellent disintegration properties, and the extract of Salacia plants is easily absorbed in the body. Specifically, the disintegration properties of the tablets of this disclosure include those in which, when the time required for disintegration (disintegration time) is measured according to "6.09 Disintegration Test Method" of "General Test Methods" in "The Seventeenth Edition of the Japanese Pharmacopoeia", the disintegration time is 28 minutes or less, preferably 25 minutes or less, more preferably 20 minutes or less, even more preferably 18 minutes or less, and particularly preferably 15 minutes or less.

[0061] The tablets of this disclosure have a moderate hardness that prevents breakage during packaging and transportation. The hardness of the tablets of this disclosure is sufficient to prevent breakage during packaging and transportation, but specifically, the hardness measured by a load cell type tablet hardness tester is 80N or higher, preferably 85N or higher, more preferably 90N or higher, and even more preferably 90-350N.

[0062] Tablet shape and product classification The tablets of this disclosure may be used in their uncoated state, but may also be used as coated tablets by applying a coating such as sugar coating or film coating as needed.

[0063] The weight per tablet of the tablets disclosed herein can be set appropriately depending on the single dose, the amount of component (A) contained, etc., but for example, it can be around 200 to 400 mg.

[0064] The product classification of tablets in this disclosure is not particularly limited and may be any of the following: food and beverages (including foods for special dietary uses and health functional foods (nutrient function foods, foods with functional claims, foods for specified health uses, etc.), and general foods (nutritional supplements, health supplements, fortified foods, nutritional adjustment foods, supplements, etc.)) and oral pharmaceuticals (including quasi-drugs for oral use).

[0065] Manufacturing method The tablets of this disclosure are manufactured by compressing a raw material mixture containing components (A) and (B), and other components added as needed. The method of compressing is not particularly limited, but can be carried out using equipment such as a single-shot tablet press, a rotary tablet press, or a high-speed rotary tablet press. The compression pressure during tableting is not particularly limited as long as tablet formation is possible, but can usually be set to about 0.5 to 2.0 t, preferably about 0.8 to 1.8 t, and more preferably about 1.0 to 1.5 t. In addition, at least a portion of the raw material mixture to be used for tableting may be granulated in advance as needed.

[0066] 2. Method for improving the disintegration properties of tablets This disclosure provides a method for improving the disintegration properties of tablets containing extracts of Salacia plants. Specifically, the method is characterized by (A) including in a tablet containing an extract of Salacia plant (B) at least one selected from the group consisting of γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract. The types and amounts of ingredients used in this method, the method of forming the tablets, etc., are as described in section "1. Tablets" above. [Examples]

[0067] The present disclosure will be described in more detail below with reference to examples, but the present disclosure is not limited to these examples.

[0068] The details of the ingredients used in the following test examples and formulation examples are as follows: (A) component • Salacia extract: This is a dried powder of a hot water extract of the stems of Salacia chinensis from Thailand (containing 0.22% by weight of neocotaranol). Specifically, 1 kg of crushed Salacia chinensis stems from Thailand was mixed with 7 L of water, extracted at 98°C for 2 hours, and then concentrated under reduced pressure and spray-dried to obtain the Salacia extract. (B) Component • GABA-containing barley lactic acid fermentation extract: This is a dried powder (containing 90% by weight of γ-aminobutyric acid) obtained by separating and concentrating microbial cells from the alcohol fermentation product of barley shochu lees. • Pine bark extract: French pine bark extract Pycnogenol®, 1000x concentrate, containing 65% by weight of procyanidins. • Equol: A powder obtained by solvent extraction of soybean hypocotyls with aqueous ethanol (containing 5% by weight of S-equol). • Carnitine: Contains 67.2% L-carnitine by weight. Ginkgo biloba leaf extract: This is a powdered extract (containing 6% by weight of terpene lactones) obtained by solvent extraction of ginkgo leaves with aqueous ethanol.

[0069] Test example 1. Manufacturing of tablet samples Tablet samples with the composition shown in Table 1 were prepared. Specifically, predetermined amounts of the components shown in Table 1 were mixed, and the resulting mixed powder was compressed into tablets using a hydraulic tablet press (TB-20N, NPA System Co., Ltd.) at a pressure of 100N to obtain tablet samples of 306 mg each (9 mm in diameter, disc shape).

[0070] 2. Assessment of disintegration potential For each tablet sample obtained, the disintegration time was measured using a disintegration tester (NT-1HM, Toyama Sangyo Co., Ltd.) in accordance with the disintegration test method specified in the 17th edition of the Japanese Pharmacopoeia. The disintegration time was taken as the average of six tablet samples. The results are shown in Table 1.

[0071] [Table 1]

[0072] As shown in Table 1, the tablets of Comparative Examples 1 to 6, which contained either component (A) or component (B) alone, had a very long disintegration time. However, as shown in Examples 1 to 15, the tablets containing a combination of component (A) and component (B) had a shorter disintegration time compared to the tablets of Comparative Examples 1 to 6, which contained either component (A) or component (B) alone, yielding an unexpected result.

[0073] Prescription examples Tablets with the compositions shown in Table 2 were manufactured. When the disintegration time was measured using the same method as in the test examples, all tablets showed shorter disintegration times and improved disintegrability.

[0074] [Table 2]

Claims

1. A tablet containing (A) an extract of a plant of the genus Salacia, and (B) at least one selected from the group consisting of γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract.

2. The tablet according to claim 1, wherein, on a dry weight basis, it contains 0.01 to 20 parts by weight of component (B) per 1 part by weight of component (A).

3. The tablet according to claim 1, wherein the content of component (A) is 1 to 80% by weight on a dry weight basis.

4. The tablet according to claim 1, wherein the content of component (B) is 0.01 to 80% by weight on a dry weight basis.

5. (A) A method for improving the disintegration properties of tablets containing an extract of a plant of the genus Salacia, A method for improving disintegration, comprising (A) a tablet containing an extract of a plant of the genus Salacia, and (B) at least one selected from the group consisting of γ-aminobutyric acid, equol, carnitine and its salts, pine bark extract, and ginkgo leaf extract.

Citation Information

Patent Citations

  • Foodstuff containing extract of plant of genus salacia and flavonoid

    JP2013027403A