Tablet Composition

Abstract

To provide an Eppikajutsubuto extract formulation having excellent formulation properties.SOLUTION: A tablet composition contains Eppikajutsubuto extract, so that it has excellent hardness.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to an extract preparation of Eppikajutsubuto. [Background technology]

[0002] Eppikajutsubuto is a Kampo medicine made by adding Busi to Eppikajutsuto, and is used in cases of severe symptoms such as edema, chills, and difficulty urinating, in patients with Eppikajutsuto symptoms. Eppikajutsubuto was added to the approval standards for general-use Kampo preparations relatively recently (Non-Patent Document 1).

[0003] Eppikajutsuto contains 6g of Ephedra, 8g of Sekko, 3g of Ginger, and 2g of Licorice. It is commercially available as a herbal medicine mixture consisting of 4 g of Atractylodes orbiculatus, 3 g of Taiso, and 1 g of Bushi, and is taken by decoction (Non-patent Document 2). [Prior art documents] [Non-patent literature]

[0004] [Non-Patent Document 1] Approval Standards for General Kampo Preparations, Reference Material 2-2, Ministry of Health, Labor and Welfare, Pharmaceuticals and Food Safety Bureau, April 15, 2011 [Non-Patent Document 2] Eppikajutsubuto, a convenient decoction for 5 days (15 packets), for swelling, eczema, arthritis, pharmacy preparation, [online], Akao Kampo Pharmacy, [searched on March 20, 2021], Internet<URL:https: / / store.shopping.yahoo.co.jp / akaokanpou / eppikajutu-kpc5.html> Summary of the Invention [Problem to be solved by the invention]

[0005] Currently, Eppikajutsubuto is only available as a decoction of a mixture of herbs, and there is no extract preparation available. Furthermore, the pharmaceutical properties of Eppikajutsubuto extract preparations have not yet been investigated.

[0006] Therefore, an object of the present invention is to provide an Eppikajutsubuto extract preparation having excellent formulation properties. [Means for solving the problem]

[0007] As a result of intensive research, the present inventors have found that tablets with excellent hardness can be obtained by tableting Ekpi-ka-jutsu-to extract. Moreover, the hardness of Ekpi-ka-jutsu-to extract tablets is improved compared to Ekpi-ka-jutsu-to extract, which has the same herbal composition except for the presence or absence of 'bushi', and such an effect of improving hardness was unexpected in view of the fact that no technical relationship between 'bushi' and tablet hardness is known. Furthermore, it has been unexpectedly found that in the herbal medicine mixture used for extracting Ekpi-ka-jutsu-to extract, by further increasing the amount of 'bushi' relative to 'ginger', the hardness can be further improved and disintegration can be improved in some cases. The present invention was completed based on these findings and through further research.

[0008] That is, the present invention provides the following aspects. Item 1. A tablet composition containing an extract of Eppikajutsubuto. Item 2. The tablet composition according to Item 1, wherein the herbal medicine mixture used for extracting the Eppikajutsufuto extract contains 0.3 to 1 part by weight of Bupleurum per part by weight of Zingiber officinale. Item 3. The tablet composition according to claim 1, wherein the herbal medicine mixture used for extracting the Eppikajutsufuto extract contains 0.7 to 1 part by weight of Bupleurum per part by weight of Zingiber officinale. Item 4. The tablet composition according to any one of Items 1 to 3, comprising 60 to 95% by weight of the Eppikajutsubuto extract. Item 5. The tablet composition according to any one of Items 1 to 4, comprising 5 to 40% by weight of a disintegrant. Item 6. The tablet composition according to Item 5, wherein the disintegrant is light anhydrous silicic acid, carmellose calcium, and / or starch. Effect of the Invention

[0009] According to the present invention, it is possible to provide an Eppikajutsubuto extract tablet having excellent hardness. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0010] The tablet composition of the present invention is characterized by containing an extract of Eppikajutsufuto. The tablet composition of the present invention will be described in detail below.

[0011] The constituent herbal medicines of Eppikajutsubuto are Ephedra, Sekko, Atractylodes Root, Bouquet, Zingiber officinale, Licorice, and Taiso. As Atractylodes Root, Byaku-Atractylodes Root and / or Souquetylodes Root can be used, and from the viewpoint of further improving tablet hardness or from the viewpoint of improving disintegration in addition to said viewpoint, Souquetylodes Root is preferably used. As Bouquetyl Root, Bouquetyl Root powder and / or processed Bouquetyl Root can be used, and from the viewpoint of further improving tablet hardness or from the viewpoint of improving disintegration in addition to said viewpoint, processed Bouquetyl Root is preferably used.

[0012] The amount of each herb in the herb preparation used in the production of the Eppikajutsubuto extract of the present invention is not particularly limited, but the content of Bushi per 1 part by weight of Zingiber officinale is, for example, 0.3 to 1 part by weight, and from the viewpoint of further improving tablet hardness, preferably 0.6 to 1 part by weight. Furthermore, from the viewpoint of further improving tablet hardness and disintegrability, more preferably 0.7 to 1 part by weight, even more preferably 0.8 to 1 part by weight, even more preferably 0.9 to 1 part by weight, and even more preferably 0.95 to 1 part by weight.

[0013] The specific composition of the herbal medicine preparation used in the production of the Eppikajutsubuto extract used in the present invention includes, for example, 4 to 6 parts by weight of Ephedra, 8 to 10 parts by weight of Gypsum, 3 to 4 parts by weight of Atractylodes Root, 0.3 to 1 part by weight of Atractylodes Root, 1 part by weight of Zingiber officinale, 1.5 to 2 parts by weight of Licorice Root, and 3 to 4 parts by weight of Atractylodes Root; from the viewpoint of further improving tablet hardness, or from the viewpoint of improving disintegrability as well as the tablet hardness, preferably, 5 to 6 parts by weight of Ephedra, 8 to 9 parts by weight of Gypsum, 3.5 to 4 parts by weight of Atractylodes Root, 0.6 to 1 part by weight of Atractylodes Root, 1 part by weight of Zingiber officinale, 1.8 to 2 parts by weight of Licorice Root, and 3 to 3.5 parts by weight of Atractylodes Root; From the viewpoint of further improving the tablet hardness and disintegrability, more preferred are 5 to 6 parts by weight of Ephedra, 8 to 9 parts by weight of Gypsum, 3.5 to 4 parts by weight of Atractylodes Root, 0.7 to 1 part by weight of Bougainvillea, 1 part by weight of Zingiber officinale, 1.8 to 2 parts by weight of Licorice Root, and 3 to 3.5 parts by weight of Trifolium Pratense; from the viewpoint of further improving the tablet hardness and disintegrability, even more preferred are 6 parts by weight of Ephedra, 8 parts by weight of Gypsum, 4 parts by weight of Atractylodes Root, 0.8 to 1 part by weight of Bougainvillea (even more preferably 0.9 to 1 part by weight, even more preferably 0.95 to 1 part by weight, particularly preferably 1 part by weight), 1 part by weight of Zingiber officinale, 2 parts by weight of Licorice Root, and 3 parts by weight of Trifolium Pratense.

[0014] The Eppikajutsubuto extract used in the present invention can be obtained by extracting the herbal preparation by a known method. For example, the method of extracting the herbal preparation includes adding water in an amount of about 10 to 20 times, preferably 13 to 18 times, the amount of the herbal preparation, and stirring and extracting at about 80 to 100°C, preferably 95 to 100°C, for about 0.5 to 3 hours, preferably 0.5 to 1.5 hours. After extraction, the solid content is removed by solid-liquid separation such as centrifugation and filtration, and if necessary, by concentration or drying, to obtain the Eppikajutsubuto extract.

[0015] To obtain Eppikajutsuto extract as an extract powder, the extract from which the solids have been removed may be concentrated as necessary and then subjected to drying treatment such as spray drying, reduced pressure concentration drying, freeze drying, etc. When subjected to drying treatment (particularly drying treatment by spray drying), an excipient may be added to the extract as necessary.

[0016] The content of the Eppikajutsubuto extract in the tablet composition of the present invention is not particularly limited, but may be 60 to 95% by weight. The Eppikajutsubuto extract itself of the tablet composition of the present invention is obtained from a herbal preparation containing Busi, and thus serves to improve tablet hardness. Therefore, unlike general herbal extract tablets, the tablet composition of the present invention can have high hardness even if the content of the Eppikajutsubuto extract itself is high. Therefore, suitable examples of the Eppikajutsubuto extract in the tablet composition of the present invention include 70 to 95% by weight, more preferably 72 to 95% by weight, even more preferably 74 to 95% by weight, even more preferably 76 to 95% by weight, and even more preferably 78 to 95% by weight.

[0017] Other Ingredients The tablet composition of the present invention may contain additives and / or bases as components other than the Eppii Ka Sutsubu To extract, as long as the effects of the present invention are not impaired.

[0018] The additives and bases are not particularly limited as long as they are pharma- ceutically acceptable, and examples thereof include excipients, binders, disintegrants, lubricants, isotonicity agents, plasticizers, dispersants, emulsifiers, solubilizers, wetting agents, stabilizers, suspending agents, adhesives, coating agents, glossing agents, water, oils and fats, waxes, hydrocarbons, fatty acids, higher alcohols, esters, water-soluble polymers, surfactants, metal soaps, lower alcohols, polyhydric alcohols, pH adjusters, buffers, antioxidants, UV inhibitors, preservatives, flavorings, fragrances, powders, thickeners, dyes, and chelating agents. These additives may be used alone or in combination of two or more. The content of these additives and bases is appropriately set according to the type of additives and bases used, etc., as long as they can be molded into tablets.

[0019] Among these additives and bases, preferred are disintegrants (e.g., light anhydrous silicic acid, synthetic aluminum silicate, magnesium aluminometasilicate, anhydrous calcium hydrogen phosphate, carmellose, carmellose sodium, carmellose calcium, croscarmellose sodium, low-substituted hydroxypropylcellulose, low-substituted carboxymethylstarch, crystalline cellulose, starch, sodium starch glycolate, crospovidone, etc.), magnesium stearate, calcium stearate, calcium silicate, magnesium silicate, synthetic hydrotalcite, etc. Of these, from the viewpoint of further improving tablet hardness or, in addition to said viewpoint, from the viewpoint of improving disintegrability, more preferred are light anhydrous silicic acid, carmellose calcium, starch, and magnesium stearate.

[0020] Since the tablet composition of the present invention can form tablets with high hardness without impairing disintegrability, even if the amount of disintegrant used is small, tablets with high hardness can be effectively formed. From this viewpoint, the suitable amount of disintegrant used is, for example, 5 to 40% by weight, preferably 5 to 30% by weight, more preferably 5 to 25% by weight, and even more preferably 5 to 20% by weight. From the viewpoint of achieving both excellent hardness and disintegrability, the more suitable amount of disintegrant used is, for example, 10 to 20% by weight, even more preferably 15 to 20% by weight, and particularly preferably 17 to 20% by weight.

[0021] Furthermore, when light anhydrous silicic acid, carmellose calcium, and starch are used as disintegrants in the tablet composition of the present invention, the blending weight ratio thereof (light anhydrous silicic acid:carmellose calcium:starch) is preferably [1-3]:[0.6-1]:1, more preferably [1.5-2.5]:[0.7-0.9]:1, and even more preferably [1.8-2.2]:[0.75-0.85]:1, from the viewpoint of obtaining excellent hardness and / or disintegrability.

[0022] In addition, the tablet composition of the present invention may contain other nutritional components or pharmacological components as necessary, in addition to the Eppikajutsufuto extract. Such nutritional components and pharmacological components are not particularly limited as long as they are pharmacologic acceptable, and examples thereof include antacids, stomachic agents, digestive agents, intestinal regulators, antispasmodics, mucosal repair agents, anti-inflammatory agents, astringents, antiemetics, antitussives, expectorants, anti-inflammatory enzymes, sedatives, hypnotics, antihistamines, caffeine, cardiac diuretics, antibacterial agents, vasoconstrictors, vasodilators, local anesthetics, herbal extracts, vitamins, and menthols. These nutritional components and pharmacological components may be used alone or in combination. The content of these components is appropriately set according to the type of components used.

[0023] Formulation The tablet composition of the present invention is formed into a tablet. The shape and size of the tablet are not particularly limited. Examples of tablet shapes include round, oval, triangular, and rectangular. In the case of round tablets, the diameter is 6 to 12 mm, preferably 8 to 10 mm. The weight per tablet is 200 to 600 mg, preferably 300 to 400 mg.

[0024] The tablet produced from the tablet composition of the present invention may be a plain tablet (bare tablet), or may be a coated tablet with a coating applied to the surface for the purpose of stabilizing the drug and masking the taste and odor. Examples of coated tablets include sugar-coated tablets and film-coated tablets (stomach-soluble tablets, enteric-coated tablets) coated with a film containing a water-soluble, enteric or gastrosoluble polymer base. The tablet composition of the present invention has excellent tablet hardness, so that even if it is a plain tablet, it is physically stable. The hardness of the plain tablet produced from the tablet composition of the present invention is 180N or more, preferably 185N or more, more preferably 200N or more, even more preferably 210N or more, even more preferably 220N or more, even more preferably 230N or more, and particularly preferably 235N or more. The upper limit of the hardness is not particularly limited, and examples thereof include 250N or less, 245N or less, or 240N or less.

[0025] Manufacturing method The tablet composition of the present invention can be manufactured according to a conventional formulation method adopted in the pharmaceutical field using the Eppii Ka Zhuo Tang extract, and additives, base materials, and pharmacological ingredients added as necessary. Preferably, the manufacturing method of the tablet composition of the present invention includes a granulation step of granulating the Eppii Ka Zhuo Tang extract or an Eppii Ka Zhuo Tang extract mixture mixed with additives, base materials, other nutritional ingredients, and / or other pharmacological ingredients as necessary, and a tableting step of tableting the granulated product. The tableting pressure in the tableting step is, for example, 4 to 20 kN, preferably 6 to 20 kN, and more preferably 8 to 15 kN. Since the tablet composition of the present invention has excellent tablet hardness, a tablet with high hardness can be effectively formed even with a relatively small tableting pressure. From this viewpoint, a suitable example of the tableting pressure in the tableting step is 8 to 13 kN, more preferably 8 to 11 kN, and even more preferably 8 to 10 kN.

[0026] Purpose The tablet composition of the present invention is used for applications in which it is formed into tablets, and furthermore, tablets produced from the tablet composition of the present invention may be used for any application in which the efficacy of Eppii Ka Sutsubu Tang extract is expected. EXAMPLES

[0027] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples.

[0028] Test Example 1. Manufacturing of Eppikajutsubuto extract powder A herbal preparation with the composition shown in Table 1 (processed bush was used as bush in the table) was used as the raw herbal material and extracted with 15 times its weight of normal water at about 100°C for 1 hour, followed by hot solid-liquid separation and filtration to obtain an extract. The extract was concentrated under reduced pressure and dried using a spray dryer to obtain Eppikajutsuto extract powder (Eppikajutsuto extract powder for Comparative Example 1). Drying using a spray dryer was performed by dropping the extract into an atomizer rotating at 10,000 rpm and supplying hot air at 150°C.

[0029] [Table 1]

[0030] 2. Preparation of tablet composition The Eppikajutsubutou extract powder obtained in 1 above was mixed with the ingredients shown in Table 2 in the composition shown in the table, granulated, and then compressed with a pressure of 9 kN to produce tablets (plain tablets, weight 360 mg, diameter 9.5 mm).

[0031] 3. Hardness and Friability The hardness (N) of the produced tablets (plain tablets) was measured using a load cell type tablet hardness tester (breaking speed 0.5 mm / min), and the disintegration properties (min) were evaluated according to the disintegration test method described in the Japanese Pharmacopoeia (17th edition). The disintegration time was the average value of three tablets. The results are shown in Table 2.

[0032] [Table 2]

[0033] As is clear from Table 2, tablets containing Eppikajutsubuto extract showed improved hardness (Examples 1 to 3). In particular, when the weight ratio of Bushi to Ginger in the herbal mixture used to manufacture Eppikajutsubuto extract was set to a specified ratio or higher, improved hardness and disintegration properties were also observed (Examples 1 and 2), demonstrating that the tablets had particularly excellent tablet properties.

Claims

1. A tablet composition containing Eppikajutsubutou extract.

2. The tablet composition according to claim 1, wherein the herbal preparation used for extracting the Eppikajutsufuto extract contains 0.3 to 1 part by weight of Bupleurum per part by weight of Zingiber officinale.

3. The tablet composition according to claim 1, wherein the herbal preparation used for extracting the Eppikajutsufuto extract contains 0.7 to 1 part by weight of Bupleurum per part by weight of Zingiber officinale.

4. The tablet composition according to any one of claims 1 to 3, comprising 60 to 95% by weight of the Eppikajutsufuto extract.

5. The tablet composition according to any one of claims 1 to 4, comprising 5 to 40% by weight of a disintegrant.

6. The tablet composition according to claim 5, wherein the disintegrant is light anhydrous silicic acid, calcium carmellose, and / or starch.

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