tablet

Abstract

The purpose of this disclosure is to provide tablets in which the sustained-release properties of extracts from plants of the genus Salacia are improved. [Solution] The tablets of this disclosure contain (A) an extract of a plant of the genus Salacia, and (B) an extract of Gymnema.

Description

Technical Field

[0006] , ,

[0001] The present disclosure relates to tablets with improved sustained release of extracts from plants of the genus Salacia.

Background Art

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

[0003] In oral ingestion of plants of the genus Salacia, extracts from parts such as stems, roots, and bark are concentrated and formulated into food and drink products, thereby achieving efficient ingestion of 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 with 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 formulation form because they can be ingested by drinking with water or the like without causing the taste of functional components to be felt. In addition, in order to reduce the frequency of taking tablets, there may be a need to slowly release functional components and make them act in the body for a long time.

[0006] To date, there has been no study on how to sustainably release the extract of Salacia plants in tablets containing Salacia extracts so that they can act in the body for an extended period.

[0007] Therefore, the purpose of this disclosure is to provide tablets in which the sustained release properties of the extract of Salacia plants are improved. [Means for solving the problem]

[0008] The inventors conducted diligent research to solve the aforementioned problems and unexpectedly discovered that by combining Gymnema extract with tablets containing Salacia plant extract, the sustained release of Salacia plant extract is improved. This disclosure was completed by further research based on this finding.

[0009] In other words, this disclosure provides inventions in the following embodiments. Item 1: Tablets containing (A) an extract of a plant of the genus Salacia, and (B) an extract of Gymnema. 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 sustained release of the extract of a plant of the genus Salacia in a tablet containing an extract of a plant of the genus Salacia, A method for improving sustained release, comprising (A) adding a tablet containing an extract of a plant of the genus Salacia, and (B) adding a Gymnema extract. [Effects of the Invention]

[0010] The tablets of this disclosure have improved sustained-release properties of the Salacia plant extract, allowing the Salacia plant extract to act in the body for a longer period, thus reducing the frequency of administration. [Modes for carrying out the invention]

[0011] 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) a Gymnema extract (hereinafter also referred to as "Component (B)"). The tablets of this disclosure are 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.

[0012] (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). Conventional tablets containing extracts of plants of the genus Salacia do not have sufficient sustained release properties of the extract. However, the tablets of this disclosure have improved sustained release properties of the extract of plants of the genus Salacia due to the inclusion of component (B), which extends the dissolution time of the extract and allows it to act in the body for a longer period.

[0013] 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.

[0014] 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.

[0015] 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.

[0016] 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.

[0017] 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.

[0018] 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 preferred, water, ethanol, and mixed solvents thereof are more preferred, and water is particularly preferred.

[0019] 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.

[0020] The solvent extraction treatment can be carried out by immersing the extraction target part of the Salacia plant (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 extraction target part of the Salacia plant and carrying out the treatment for about 0.5 to 24 hours.

[0021] Also, 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.

[0022] By removing solids through solid-liquid separation after extraction treatment, an extract of Salacia plants can be obtained. The extract obtained by the extraction treatment may, if necessary, be subjected to a purification treatment by adsorption treatment such as various chromatographies using a column filled with a carrier such as a filtration treatment; a polystyrene gel (such as a polystyrene-divinylbenzene copolymer), an 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 a dry extract.

[0023] In the extract of Salacia plants used in the present disclosure, the content (in terms of dry weight) of neokotalanol is not particularly limited. However, from the viewpoint of gently absorbing sugar and improving the effect of suppressing the rise in postprandial blood glucose level, it is preferably 0.2% by weight or more, more preferably 0.25% by weight or more, and 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. From the viewpoint of reducing the unpleasant aftertaste after taking tablets, it is preferably 0.45% by weight or less, and 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, and still more preferably 0.3 to 0.4% by weight.

[0024] 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. From the viewpoints of improving the blood glucose level-rising inhibitory effect and appetite inhibitory effect, etc., and reducing the unpleasant aftertaste after taking 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.

[0025] (B) Gymnema extract The tablets of this disclosure contain Gymnema extract as component (B). Surprisingly, by combining Gymnema extract with tablets containing extracts of Salacia plants, the sustained release properties of the Salacia plant extract are improved.

[0026] Gymnema extract is an extract of the leaves and stems of Gymnema sylvestre or Gymnema inodorum, a plant of the Asclepidaceae family that is native to India and grows widely in Southeast Asia, including Thailand, Indonesia, and southern China. Its main component is gymnemic acid, one of the triterpenoid saponins.

[0027] For obtaining Gymnema extract, 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".

[0028] In Gymnema extracts, the extraction solvent used in the solvent extraction process is preferably water, a lower monohydric alcohol, or a mixture thereof, more preferably a lower monohydric alcohol, and particularly preferably ethanol.

[0029] After the extraction process, solid matter is removed by solid-liquid separation to obtain a Gymnema extract. The extract obtained from the extraction process may be purified as needed, by filtration and adsorption. The obtained extract is concentrated and used as Gymnema extract. Specific forms of Gymnema extract include soft extract and dry extract, with dry extract being preferred.

[0030] In the tablets of this disclosure, the content of component (B) can be appropriately set according to the desired degree to which the sustained release effect of the extract of Salacia plants is improved. 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 sustained release of the extract of Salacia plants, it is preferably 0.05 to 15 parts by weight, more preferably 0.1 to 10 parts by weight, even more preferably 0.15 to 7 parts by weight, and even more preferably 0.2 to 5 parts by weight.

[0031] Furthermore, in the tablets of this disclosure, the content of component (B) can be appropriately set according to the desired degree of improvement in the sustained release of the extract of Salacia plants, 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 sustained release of the extract of Salacia plants, 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.

[0032] 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.

[0033] 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.

[0034] Physical properties of tablets The tablets of this disclosure possess a sustained-release property that allows the extract of Salacia plants to act in the body for an extended period after ingestion. Specifically, the sustained-release property of the tablets of this disclosure is such that, when the time required for disintegration (disintegration time) is measured according to the "6.09 Disintegration Test Method" of the "General Test Methods" of the "Seventeenth Edition of the Japanese Pharmacopoeia," the disintegration time is 40 minutes or more, preferably 45 minutes or more, more preferably 50 minutes or more, even more preferably 55 minutes or more, and particularly preferably 60 minutes or more.

[0035] 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.

[0036] Tablet shape and product classification The tablets described herein 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.

[0037] The weight per tablet of the tablets disclosed herein can be set appropriately depending on the dosage per dose, the amount of component (A) contained, etc., but for example, it can be around 200 to 400 mg.

[0038] 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).

[0039] 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.

[0040] 2. Method for improving the sustained release properties of extracts from Salacia plants. This disclosure provides a method for improving the sustained release of a Salacia plant extract in tablets containing a Salacia plant extract. Specifically, the improvement method is characterized by (A) adding a Gymnema extract to a tablet containing a Salacia plant extract. The types and amounts of ingredients used in this improvement method, the method of forming the tablets, etc., are as described in section "1. Tablets" above.

[0041] In this disclosure, improving the sustained release properties of the Salacia plant extract means that the disintegration time of a tablet containing components (A) and (B) is longer than the disintegration time of a tablet without component (B). The disintegration time is measured according to "6.09 Disintegration Test Method" of "General Test Methods" in the "Seventeenth Edition of the Japanese Pharmacopoeia". [Examples]

[0042] The present disclosure will be described in more detail below with reference to examples, but the present disclosure is not limited to these examples.

[0043] 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 • Gymnema extract: This is a powdered extract obtained by solvent extraction of the leaves and stems of Gymnema sylvestre with ethanol (containing 9% by weight of Gymnema saponins).

[0044] 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).

[0045] 2. Evaluation of the sustained-release properties of Salacia extract The sustained-release properties of Salacia extract were evaluated by the disintegration time of the tablets. 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. A longer disintegration time indicates superior sustained-release properties of the Salacia extract. The results are shown in Table 1.

[0046] [Table 1]

[0047] As shown in Table 1, the tablets of Comparative Examples 1 or 2, which contained either component (A) or component (B) alone, had short disintegration times, and the tablet of Comparative Example 1 exhibited inferior sustained release of the Salacia extract. However, as shown in Examples 1 to 3, the tablets containing a combination of component (A) and component (B) showed significantly longer disintegration times compared to the tablets of Comparative Examples 1 or 2, which contained either component (A) or component (B) alone, and significantly improved sustained release of the Salacia extract, yielding unexpected results.

[0048] Prescription examples Tablets with the composition shown in Table 2 were manufactured. When the disintegration time was measured using the same method as in the test examples, all tablets showed a significantly longer disintegration time, indicating a significant improvement in the sustained release of Salacia extract.

[0049] [Table 2]

Claims

1. Tablets containing (A) an extract of a plant of the genus Salacia, and (B) an extract of Gymnema.

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 sustained release of the extract of a plant of the genus Salacia in a tablet containing an extract of a plant of the genus Salacia, A method for improving sustained release, comprising (A) adding a tablet containing an extract of a plant of the genus Salacia, and (B) adding a Gymnema extract.

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