JP2023172517A - tablet composition - Google Patents
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- JP2023172517A JP2023172517A JP2022084377A JP2022084377A JP2023172517A JP 2023172517 A JP2023172517 A JP 2023172517A JP 2022084377 A JP2022084377 A JP 2022084377A JP 2022084377 A JP2022084377 A JP 2022084377A JP 2023172517 A JP2023172517 A JP 2023172517A
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- 239000007916 tablet composition Substances 0.000 title claims abstract description 46
- 239000009520 bofu-tsusho-san Substances 0.000 claims abstract description 62
- 239000000284 extract Substances 0.000 claims abstract description 60
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- 235000006886 Zingiber officinale Nutrition 0.000 claims abstract description 30
- 235000008397 ginger Nutrition 0.000 claims abstract description 30
- 238000002360 preparation method Methods 0.000 claims description 28
- 229940079593 drug Drugs 0.000 claims description 27
- 239000003814 drug Substances 0.000 claims description 27
- 239000000203 mixture Substances 0.000 abstract description 15
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- 238000000034 method Methods 0.000 abstract description 7
- 238000000605 extraction Methods 0.000 abstract description 3
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- 241000555712 Forsythia Species 0.000 description 10
- 241000411851 herbal medicine Species 0.000 description 10
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- 238000001035 drying Methods 0.000 description 7
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- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 1
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- DJWYOLJPSHDSAL-UHFFFAOYSA-N Pantethine Natural products OCC(C)(C)C(O)C(=O)NCCC(=O)NCCSSCCNC(=O)CCNC(=O)C(O)C(C)(C)CO DJWYOLJPSHDSAL-UHFFFAOYSA-N 0.000 description 1
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- YKTSYUJCYHOUJP-UHFFFAOYSA-N [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] Chemical compound [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] YKTSYUJCYHOUJP-UHFFFAOYSA-N 0.000 description 1
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- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 description 1
- 239000000378 calcium silicate Substances 0.000 description 1
- 229910052918 calcium silicate Inorganic materials 0.000 description 1
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
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- 229960001681 croscarmellose sodium Drugs 0.000 description 1
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- 239000013078 crystal Substances 0.000 description 1
- 235000003373 curcuma longa Nutrition 0.000 description 1
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- HCWCAKKEBCNQJP-UHFFFAOYSA-N magnesium orthosilicate Chemical compound [Mg+2].[Mg+2].[O-][Si]([O-])([O-])[O-] HCWCAKKEBCNQJP-UHFFFAOYSA-N 0.000 description 1
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- CXHHBNMLPJOKQD-UHFFFAOYSA-N methyl hydrogen carbonate Chemical compound COC(O)=O CXHHBNMLPJOKQD-UHFFFAOYSA-N 0.000 description 1
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- DJWYOLJPSHDSAL-ROUUACIJSA-N pantethine Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCC(=O)NCCSSCCNC(=O)CCNC(=O)[C@H](O)C(C)(C)CO DJWYOLJPSHDSAL-ROUUACIJSA-N 0.000 description 1
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- Medicines Containing Plant Substances (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
本発明は、防風通聖散エキスを含む錠剤組成物に関する。より具体的には、本発明は、防風通聖散エキスを含み、製錠後における硬度、崩壊性及び耐摩損性を向上できる錠剤組成物に関する。 The present invention relates to a tablet composition containing Bofutsushosan extract. More specifically, the present invention relates to a tablet composition that contains Bofutsushosan extract and can improve hardness, disintegration properties, and abrasion resistance after tabletting.
防風通聖散は、肥満症やメタボリックシンドロームの改善を目的に服用される漢方薬である。防風通聖散のエキス製剤は、病院処方されるだけでなく、市販もされているため、その入手容易性から、市販薬が特に広く使用されている。 Bofutsushosan is a Chinese herbal medicine taken for the purpose of improving obesity and metabolic syndrome. Bofutsushosan extract preparations are not only prescribed in hospitals but also sold commercially, so commercially available drugs are particularly widely used due to their ease of availability.
防風通聖散エキス製剤は、服用をより容易にする観点から、錠剤で提供されることも多い。このため、防風通聖散エキスを含む錠剤については、硬度、崩壊性などの錠剤特性を改良する処方が様々に検討されてきた。 Bofutsushosan extract preparations are often provided in tablet form to make them easier to take. For this reason, various formulations have been investigated for improving tablet properties such as hardness and disintegration of tablets containing Bofutsushosan extract.
例えば、特許文献１には、機械的強度および崩壊性の点で優れた効果を有する漢方薬を含有する錠剤を提供する目的において、トウキ１．２（重量部、以下同じ）、シャクヤク１．２、センキュウ１．２、サンシシ１．２、レンギョウ１．２、ハッカ１．２、ショウキョウ１．２、ケイガイ１．２、ボウフウ１．２、マオウ１．２、ダイオウ１．５、ボウショウ１．５、ビャクジュツ２．０、キキョウ２．０、オウゴン２．０、カンゾウ２．０、セッコウ２．０及びカッセキ３．０からなる防風通聖散から得られるエキスにパンテチンを配合することが記載されている。 For example, in Patent Document 1, for the purpose of providing a tablet containing a Chinese herbal medicine having an excellent effect in terms of mechanical strength and disintegration, Japanese Patent Application Publication No. 2003-100001 describes Aki 1.2 (parts by weight, same hereinafter), Peony 1.2, 1.2, 1.2, 1.2, 1.2, 1.2, 1.2, 1.2, 1.2, 1.2, 1.2, 1.2, 1.5, 1.5 , it has been described that pantethine is added to the extract obtained from Bofutsushosan, which consists of Byakujutsu 2.0, Bellflower 2.0, Scutellaria 2.0, Licorice 2.0, Gypsum 2.0, and Kasseki 3.0. There is.
特許文献２には、実用的な硬度および摩損度で、べたつかず、優れた崩壊性を有する固形製剤を提供する目的において、アルプス薬品工業製の防風通聖散料エキス－Ｆに、糖類、結晶セルロース及び崩壊剤を、それぞれの成分が所定の比率となるように配合することが記載されている。 Patent Document 2 discloses that for the purpose of providing a solid preparation with practical hardness and friability, non-stickiness, and excellent disintegration properties, saccharides and crystals are added to Bofutsushosan Extract-F manufactured by Alps Pharmaceutical Industries. It is described that cellulose and a disintegrant are blended so that each component has a predetermined ratio.
特許文献３には、高濃度の生薬乾燥エキス配合の製剤であっても、打錠性に優れ、充分な製剤硬度を確保し、崩壊時間が遅延しない生薬含有製剤を提供する目的において、防風通聖散料乾燥エキス（アルプス薬品工業株式会社製、原生薬比率：キキョウ２部、ビャクジツ２部、カンゾウ２部、オウゴン２部、セッコウ２部、ダイオウ２部、トウキ１．２部、シャクヤク１．２部、センキュウ１．２部、サンシシ１．２部、レンギョウ１．２部、ハッカ１．２部、ケイガイ１．２部、ボウフウ１．２部、マオウ１．２部、ショウキョウ０．４部、カッセキ３部、ボウショウ１．５部）に、植物性のハードワックス、メタケイ酸アルミン酸マグネシウム及びセルロースの多価カルボキシメチルエーテル架橋物のナトリウム塩を配合することが記載されている。 Patent Document 3 discloses that even if the preparation contains a dried extract of a herbal medicine at a high concentration, the purpose of providing a preparation containing a herbal medicine that has excellent tableting properties, ensures sufficient hardness, and does not delay disintegration time, is Seishin dried extract (manufactured by Alps Yakuhin Kogyo Co., Ltd., raw drug ratio: 2 parts of bellflower, 2 parts of sandalwood, 2 parts of licorice, 2 parts of scutellariae, 2 parts of gypsum, 2 parts of rhubarb, 1.2 parts of Japanese trumpet, 1 part of peony) 2 parts, 1.2 parts forsythia, 1.2 parts forsythia, 1.2 parts forsythia, 1.2 parts for peppermint, 1.2 parts for snail, 1.2 parts for snail, 1.2 parts for ephedra, 0.4 part for ginger It is described that a vegetable hard wax, magnesium aluminate metasilicate, and a sodium salt of a polyvalent carboxymethyl ether cross-linked cellulose are added to the mixture (1 part, 3 parts of kaseki, 1.5 parts of boshu).
これまで、防風通聖散エキスを含有する錠剤の硬度、崩壊性、及び／又は耐摩損性といった特性の向上は、特定の添加物及びその組み合わせの選択、並びに錠剤組成物成分の比率の最適化に着眼して行われてきた。しかしながら、これまでの方法による錠剤特性の向上は限定的であるため、当該特性をより一層向上させるためには、新たな観点からの手段が求められる。 Until now, improvements in properties such as hardness, disintegration, and/or abrasion resistance of tablets containing Bofutsushosan extract have been achieved through the selection of specific additives and their combinations, as well as the optimization of the ratio of tablet composition components. It has been carried out with a focus on However, since the improvement of tablet properties by conventional methods is limited, in order to further improve the properties, means from a new perspective are required.
そこで本発明の目的は、防風通聖散エキスを含有する錠剤の硬度、崩壊性、及び耐摩損性を向上できる新たな製剤技術を提供することである。 Therefore, an object of the present invention is to provide a new formulation technology that can improve the hardness, disintegration properties, and abrasion resistance of tablets containing Bofutsushosan extract.
本発明者は鋭意検討の結果、防風通聖散の構成生薬の１つに生ショウキョウを用い、且つ、防風通聖散の全構成生薬の混合物（生薬調合物）１００重量部当たりに使用する生ショウキョウの量を３～２２重量部とすることによって得られる防風通聖散エキスが、製錠後における硬度、崩壊性及び耐摩損性を向上できることを予期せず見出した。本発明は、この知見に基づいて、更に検討を重ねることにより完成したものである。 As a result of intensive studies, the present inventor has decided to use raw ginger as one of the constituent crude drugs of Bofutsushosan, and to use it per 100 parts by weight of the mixture (crude drug formulation) of all constituent crude drugs of Bofutsushosan. It was unexpectedly discovered that a Bofutsushosan extract obtained by adjusting the amount of raw ginger to 3 to 22 parts by weight can improve the hardness, disintegration properties, and abrasion resistance after tabletting. The present invention was completed through further studies based on this knowledge.
即ち、本発明は、下記に掲げる態様の発明を提供する。
項１． 防風通聖散エキスを含む錠剤組成物であって、
前記防風通聖散エキスの抽出に使用された生薬調合物が、前記生薬調合物の１００重量部当たり生ショウキョウを３～２２重量部含む、錠剤組成物。
項２． 前記防風通聖散エキスを６５重量％以上含む、項１に記載の錠剤組成物。
項３． 項１又は２に記載の錠剤組成物を含む錠剤。
項４． 素錠である、項３に記載の錠剤。
That is, the present invention provides the inventions of the following aspects.
Item 1. A tablet composition comprising Bofutsushosan extract,
A tablet composition, wherein the crude drug preparation used to extract the Bofutsushosan extract contains 3 to 22 parts by weight of fresh ginger per 100 parts by weight of the crude drug preparation.
Item 2. Item 2. The tablet composition according to item 1, comprising 65% by weight or more of the Bofutsushosan extract.
Item 3. Item 3. A tablet comprising the tablet composition according to item 1 or 2.
Item 4. The tablet according to item 3, which is a plain tablet.
本発明によれば、防風通聖散エキスを含有する錠剤の硬度、崩壊性、及び耐摩損性を向上できる新たな製剤技術が提供される。 According to the present invention, a new formulation technique is provided that can improve the hardness, disintegration properties, and abrasion resistance of tablets containing Bofutsushosan extract.
本発明の錠剤組成物は、防風通聖散エキスを含む錠剤組成物であって、前記防風通聖散エキスの抽出に使用された生薬調合物が、前記生薬調合物の１００重量部当たり生ショウキョウを３～２２重量部含むことを特徴とする。これによって、製錠後における硬度、崩壊性及び耐摩損性を向上できる。以下、本発明の錠剤組成物について詳述する。 The tablet composition of the present invention is a tablet composition containing Bofutsushosan extract, in which the crude drug preparation used for extracting the Bofutsushosan extract contains fresh corn per 100 parts by weight of the crude drug preparation. It is characterized by containing 3 to 22 parts by weight of Kyo. This makes it possible to improve the hardness, disintegration and abrasion resistance after tabletting. The tablet composition of the present invention will be explained in detail below.
本発明の錠剤組成物は、所定の防風通聖散エキスを含む。本発明で用いられる所定の防風通聖散を構成する生薬調合物は、少なくとも生ショウキョウを上記所定比率で含む。本発明において、「生ショウキョウ」とは、生のヒネショウガを指し、日本薬局方に乾生姜として規定されている「ショウキョウ」とは異なる。つまり、本発明で用いられる所定の防風通聖散を構成する生薬調合物は、上記所定比率の「生ショウキョウ」を含む点で、「ショウキョウ」を含み「生ショウキョウ」を含まない通常の防風通聖散を構成する生薬調合物とは異なる。 The tablet composition of the present invention contains a predetermined Bofutsushosan extract. The herbal medicine preparation constituting the predetermined Bofutsushosan used in the present invention contains at least raw ginger in the above-mentioned predetermined ratio. In the present invention, "raw ginger" refers to fresh ginger, and is different from "ginger ginger", which is defined as dried ginger in the Japanese Pharmacopoeia. In other words, the herbal medicine preparation constituting the predetermined Bofutsushosan used in the present invention contains "raw ginger" in the above-mentioned predetermined ratio. It is different from the crude drug preparation that makes up Bofutsushosan.
本発明における防風通聖散を構成する生薬調合物は、上記所定比率の生ショウキョウを含むこと以外については、通常の防風通聖散を構成する生薬調合物に準じることができる。当該通常の防風通聖散については、「一般用漢方処方の手引き」（厚生省薬務局監修、日薬連漢方専門委員会編集、薬業時報社発行）によれば、トウキ、シャクヤク、センキュウ、サンシシ、レンギョウ、ハッカ、ショウキョウ、ケイガイ、ボウフウ、マオウ、ダイオウ、ボウショウ、ビャクジュツ、キキョウ、オウゴン、カンゾウ、セッコウ、及びカッセキである。書簡によっては、前記生薬の内、ビャクジュツを含まないもの（例えば「経験漢方処方分量集」、大塚敬節・矢数道明監集、医道の日本社発行）や、オウゴンを含まないもの（例えば「続漢方あれこれ」大阪読売新聞社編、浪速社発行）がある。本発明で使用される防風通聖散エキスは、これらのいずれの防風通聖散に準じてよく、「ショウキョウ」の一部又は全部が、上記所定比率の「生ショウキョウ」に置き換えられる。 The crude drug formulation constituting Bofutsushosan in the present invention can be similar to the crude drug formulation constituting ordinary Bofutsushosan, except that it contains raw ginger in the above-described predetermined ratio. According to the "Guidelines for Prescribing Traditional Chinese Herbal Medicine" (supervised by the Ministry of Health and Welfare's Pharmaceutical Affairs Bureau, edited by the Japanese Pharmaceutical Federation's Traditional Chinese Medicine Expert Committee, and published by Yakugyo Jihosha), the usual Bofutsushosan contains the following: These are forsythia, forsythia, mentha, ginger, staghorn, staghorn, ephedra, rhubarb, sardine, sandalwood, bellflower, scutellariae, licorice, gypsum, and kasseki. Depending on the letter, some of the above-mentioned herbal medicines do not contain sandalwood (for example, "Experienced Traditional Chinese Medicine Prescription Quantity Collection", edited by Keisetsu Otsuka and Michiaki Yakazu, published by Ido Nippon Sha), and others do not contain scutellariae (for example, " There is a book called ``Zoku Kanpo All Things'' (edited by Osaka Yomiuri Shimbun, published by Naniwasha). The Bofutsushosan extract used in the present invention may be similar to any of these Bofutsushosan, in which part or all of the "gingo ginger" is replaced with "raw ginger" in the above-mentioned predetermined ratio.
本発明で使用される防風通聖散エキスの製造に供される生薬調合物は、当該生薬調合物の全量１００重量部当たり、生ショウキョウを３～２２重量部含み、製錠後における硬度、崩壊性及び／又は耐摩損性をより一層向上させる観点から、生ショウキョウの比率としては、好ましくは１０～２２重量部、より好ましくは１５～２２重量部、さらに好ましくは１８～２２重量部、一層好ましくは２０～２２重量部が挙げられる。 The crude drug preparation used in the production of Bofutsushosan extract used in the present invention contains 3 to 22 parts by weight of fresh ginger per 100 parts by weight of the crude drug preparation, and has a hardness after tableting. From the viewpoint of further improving disintegration and/or abrasion resistance, the ratio of raw ginger is preferably 10 to 22 parts by weight, more preferably 15 to 22 parts by weight, even more preferably 18 to 22 parts by weight, More preferably, it is 20 to 22 parts by weight.
また、本発明において防風通聖散を構成する各生薬の具体的な分量としては、生ショウキョウ量が上記範囲内である限りにおいて限定されるものではないが、例えば、「一般用漢方処方の手引き」（厚生省薬務局監修、日薬連漢方専門委員会編集、薬業時報社発行）、「第十七改正日本薬局方」等に準じ、トウキ１．２重量部、シャクヤク１．２重量部、センキュウ１．２重量部、サンシシ１．２重量部、レンギョウ１．２重量部、ハッカ１．２重量部、生ショウキョウ３～２２重量部、ケイガイ１．２重量部、ボウフウ１．２重量部またはハマボウフウ１．２重量部、マオウ１．２重量部、ダイオウ１．５重量部、ボウショウ又は無水ボウショウ０．６～１．５重量部、ビャクジュツ２重量部、キキョウ２重量部、オウゴン２重量部、カンゾウ２重量部、セッコウ２～３重量部、及びカッセキ３～５重量部が挙げられる。また、別の書簡（例えば「明解漢方処方」、西岡一夫、高橋真太郎共著、浪速社発行）に準じ、前記分量中、１．２重量部を全て１．５重量部としてもよい。 In addition, in the present invention, the specific amount of each crude drug constituting Bofutsushosan is not limited as long as the amount of raw ginger is within the above range, but for example, According to the "Guidebook" (supervised by the Ministry of Health and Welfare's Pharmaceutical Affairs Bureau, edited by the Japanese Pharmaceutical Federation's Traditional Chinese Medicine Expert Committee, published by Yakugyo Jihosha), "17th Revised Japanese Pharmacopoeia", etc., 1.2 parts by weight of Japanese turmeric, 1.2 parts by weight of peonies. 1.2 parts by weight, 1.2 parts by weight forsythia, 1.2 parts by weight forsythia, 1.2 parts by weight forsythia, 3-22 parts by weight for fresh ginger, 1.2 parts by weight for snail, 1.2 parts by weight Parts by weight or 1.2 parts by weight of Ephedra, 1.2 parts by weight of Ephedra, 1.5 parts by weight of Rhubarb, 0.6 to 1.5 parts by weight of Rhubarb or anhydrous Rhubarb, 2 parts by weight of Sandalwood, 2 parts by weight of Bellflower, 2 parts by weight parts by weight, 2 parts by weight of licorice, 2 to 3 parts by weight of gypsum, and 3 to 5 parts by weight of gypsum. Further, in accordance with another letter (for example, "Clear Chinese Medicine Prescription", co-authored by Kazuo Nishioka and Shintaro Takahashi, published by Naniwasha), 1.2 parts by weight in the above amount may be changed to 1.5 parts by weight.
本発明で使用される防風通聖散エキスの製造に供される生薬調合物を構成する各生薬の分量の好適な例として、トウキ１．２重量部、シャクヤク１．２重量部、センキュウ１．２重量部、サンシシ１．２重量部、レンギョウ１．２重量部、ハッカ１．２重量部、ケイガイ１．２重量部、ボウフウ１．２重量部、マオウ１．２重量部、ダイオウ１．５重量部、ボウショウ又は無水ボウショウ０．６～１．５重量部、ビャクジュツ２重量部、キキョウ２重量部、オウゴン２重量部、カンゾウ２重量部、セッコウ２重量部、及びカッセキ３重量部であり、且つショウキョウが３～２２重量部、好ましくは１０～２２重量部、より好ましくは１５～２２重量部、さらに好ましくは１８～２２重量部、一層好ましくは２０～２２重量部であるものが挙げられる。 Preferred examples of the amounts of each crude drug constituting the crude drug preparation used in the production of the Bofutsushosan extract used in the present invention include 1.2 parts by weight of Angelica sp., 1.2 parts by weight of Peony, and 1.2 parts by weight of Peony. 2 parts by weight, 1.2 parts by weight of Japanese forsythia, 1.2 parts by weight of Forsythia, 1.2 parts by weight of Mentha, 1.2 parts by weight of Japanese snail, 1.2 parts by weight of Ephedra, 1.2 parts by weight of Ephedra, 1.5 parts by weight of Rhubarb Parts by weight, 0.6 to 1.5 parts by weight of sagebrush or anhydrous sagebrush, 2 parts by weight of sandalwood, 2 parts by weight of bellflower, 2 parts by weight of Scutellariae, 2 parts by weight of licorice, 2 parts by weight of gypsum, and 3 parts by weight of Kasseki, In addition, the amount of ginger is 3 to 22 parts by weight, preferably 10 to 22 parts by weight, more preferably 15 to 22 parts by weight, still more preferably 18 to 22 parts by weight, even more preferably 20 to 22 parts by weight. .
本発明で使用される防風通聖散エキスは、前記生薬調合物を公知の手法で抽出することによって得ることができる。前記生薬調合物を抽出する方法については、従来の防風通聖散エキスの抽出法と同様の方法で行えばよく、例えば、前記生薬調合物に対して、約１０～２０倍量の水を加え、８０～１００℃程度で１～３時間程度撹拌して抽出する方法が挙げられる。抽出後に、遠心分離、濾過等の固液分離に供して固形分を除去し、必要に応じて、濃縮処理や乾燥処理に供することによって防風通聖散エキスが得られる。 The Bofutsushosan extract used in the present invention can be obtained by extracting the crude drug preparation described above using a known method. The method for extracting the crude drug preparation may be the same as the conventional method for extracting Bofutsushosan extract, for example, by adding about 10 to 20 times the amount of water to the crude drug preparation. , a method of extraction by stirring at about 80 to 100°C for about 1 to 3 hours. After extraction, the solid content is removed by subjecting it to solid-liquid separation such as centrifugation or filtration, and if necessary, it is subjected to concentration treatment or drying treatment to obtain Bofutsushosan extract.
防風通聖散エキスをエキス末として得るには、固形分を除去した抽出液を、必要に応じて濃縮した後に、スプレードライ、減圧濃縮乾燥、凍結乾燥等の乾燥処理に供すればよい。また、乾燥処理(特に、スプレードライによる乾燥処理)に供する際に、必要に応じて抽出液に、賦形剤を添加してもよい。このように賦形剤を添加することにより、乾燥時間を短縮することが可能になる。添加される賦形剤の種類や添加量については、一般的な漢方エキス末を製造する場合と同様である。 In order to obtain the Bofutsushosan extract as an extract powder, the extract from which the solid content has been removed may be concentrated, if necessary, and then subjected to a drying process such as spray drying, vacuum concentration drying, freeze drying, or the like. Further, when subjecting the extract to drying treatment (particularly drying treatment by spray drying), an excipient may be added to the extract as necessary. By adding excipients in this way, it becomes possible to shorten the drying time. The type and amount of excipients to be added are the same as in the case of producing a general Chinese herbal extract powder.
本発明の錠剤組成物に含まれる防風通聖散エキスの含有量（乾燥重量換算量）としては、例えば６５重量％以上が挙げられる。本発明の錠剤組成物は、硬度、崩壊性、及び耐摩損性といった錠剤特性の向上効果に優れているため、添加剤が比較的少なくても、つまり防風通聖散エキス量が比較的多くても、効果的に当該錠剤特性を向上できる。このような観点から、本発明の錠剤組成物に含まれる防風通聖散エキスの含有量の好適な例として、好ましくは６８重量％以上、より好ましくは６９重量％以上が挙げられる。本発明の錠剤組成物に含まれる防風通聖散エキスの含有量の上限としては特に制限されず、例えば９０重量％以下が挙げられ、硬度、崩壊性、及び／又は耐摩損性をより一層高める観点から、好ましくは８０重量％以下、より好ましくは７５重量％以下、さらに好ましくは７２重量％以下が挙げられる。 The content (in terms of dry weight) of the Bofutsushosan extract contained in the tablet composition of the present invention is, for example, 65% by weight or more. The tablet composition of the present invention is excellent in improving tablet properties such as hardness, disintegration, and abrasion resistance, so even if the amount of additives is relatively small, that is, the amount of Bofutsushosan extract is relatively large. Also, the properties of the tablet can be effectively improved. From this point of view, a suitable example of the content of Bofutsushosan extract contained in the tablet composition of the present invention is preferably 68% by weight or more, more preferably 69% by weight or more. The upper limit of the content of Bofutsushosan extract contained in the tablet composition of the present invention is not particularly limited, and may be, for example, 90% by weight or less, to further improve hardness, disintegration properties, and/or abrasion resistance. From this point of view, it is preferably 80% by weight or less, more preferably 75% by weight or less, still more preferably 72% by weight or less.
その他の成分
本発明の錠剤組成物は、上記の所定の防風通聖散エキスに加え、錠剤への成形に適した他の添加剤及び／又は基剤を含んでいてもよい。
Other Components In addition to the above-described Bofutsushosan extract, the tablet composition of the present invention may contain other additives and/or bases suitable for forming into tablets.
添加剤及び基剤としては、薬学的に許容されることを限度として特に制限されないが、例えば、賦形剤、結合剤、崩壊剤、滑沢剤、等張化剤、可塑剤、分散剤、乳化剤、溶解補助剤、湿潤化剤、安定化剤、懸濁化剤、粘着剤、コーティング剤、光沢化剤、水、油脂類、ロウ類、炭化水素類、脂肪酸類、高級アルコール類、エステル類、水溶性高分子、界面活性剤、金属石鹸、低級アルコール類、多価アルコール、ｐＨ調整剤、緩衝剤、酸化防止剤、紫外線防止剤、防腐剤、矯味剤、香料、粉体、増粘剤、色素、キレート剤等が挙げられる。これらの添加剤は、１種単独で使用してもよく、また２種以上を組み合わせて使用してもよい。また、これらの添加剤及び基剤の含有量については、錠剤として成形できることを限度として、使用する添加剤及び基剤の種類等に応じて適宜設定される。 Additives and bases are not particularly limited as long as they are pharmaceutically acceptable, but include, for example, excipients, binders, disintegrants, lubricants, tonicity agents, plasticizers, dispersants, Emulsifiers, solubilizing agents, wetting agents, stabilizers, suspending agents, adhesives, coating agents, brightening 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, ultraviolet inhibitors, preservatives, flavoring agents, fragrances, powders, thickeners , dyes, chelating agents, etc. These additives may be used alone or in combination of two or more. Further, the contents of these additives and base are appropriately set depending on the types of additives and base used, etc., as long as the tablet can be formed.
添加剤及び基剤の具体例としては、デンプン（バレイショデンプン、トウモロコシデンプン等）、ステアリン酸マグネシウム、ケイ酸化合物（二酸化ケイ素（軽質無水ケイ酸等）、合成ケイ酸アルミニウム、メタケイ酸アルミン酸マグネシウム、ケイ酸カルシウム、ケイ酸マグネシウム等）、合成ハイドロタルサイト、無水リン酸水素カルシウム、カルメロース、カルメロースカルシウム、クロスカルメロースナトリウム、デンプングリコール酸ナトリウム、クロスポピドン等が挙げられ、製錠後における硬度、崩壊性及び／又は耐摩損性をより一層向上させる観点から、好ましくはデンプン（より好ましくはトウモロコシデンプン）、ステアリン酸マグネシウム、及びケイ酸化合物（好ましくは二酸化ケイ素、より好ましくは軽質無水ケイ酸、含水二酸化ケイ素）が挙げられる。 Specific examples of additives and bases include starch (potato starch, corn starch, etc.), magnesium stearate, silicic acid compounds (silicon dioxide (light anhydrous silicic acid, etc.), synthetic aluminum silicate, magnesium aluminate metasilicate, (calcium silicate, magnesium silicate, etc.), synthetic hydrotalcite, anhydrous calcium hydrogen phosphate, carmellose, carmellose calcium, croscarmellose sodium, sodium starch glycolate, crospovidone, etc. Hardness after tabletting, From the viewpoint of further improving disintegration and/or abrasion resistance, preferably starch (more preferably corn starch), magnesium stearate, and silicate compound (preferably silicon dioxide, more preferably light anhydrous silicic acid, hydrated silicon dioxide).
本発明の錠剤組成物がデンプンを含む場合のデンプンの含有量としては、例えば１０～２５重量％、好ましくは１５～２３重量％、より好ましくは１８～２１重量％が挙げられる。発明の錠剤組成物がステアリン酸マグネシウムを含む場合のステアリン酸マグネシウムの含有量としては、例えば０．２～２重量％、好ましくは０．５～１．５重量％、より好ましくは０．８～１．２重量％が挙げられる。本発明の錠剤組成物がケイ酸化合物を含む場合のケイ酸化合物の含有量としては、例えば２～２０重量％、好ましくは４～１７重量％、より好ましくは７～１３重量％が挙げられる。他の添加剤及び基材も、使用する添加剤及び基剤の種類に応じて適宜設定される。 When the tablet composition of the present invention contains starch, the starch content is, for example, 10 to 25% by weight, preferably 15 to 23% by weight, and more preferably 18 to 21% by weight. When the tablet composition of the invention contains magnesium stearate, the content of magnesium stearate is, for example, 0.2 to 2% by weight, preferably 0.5 to 1.5% by weight, more preferably 0.8 to 2% by weight. 1.2% by weight is mentioned. When the tablet composition of the present invention contains a silicic acid compound, the content of the silicic acid compound is, for example, 2 to 20% by weight, preferably 4 to 17% by weight, and more preferably 7 to 13% by weight. Other additives and base materials are also appropriately set depending on the types of additives and base materials used.
また、本発明の錠剤組成物は、防風通聖散エキスの他に、必要に応じて、他の栄養成分や薬理成分を含有していてもよい。このような栄養成分や薬理成分としては、薬学的に許容されることを限度として特に制限されないが、例えば、制酸剤、健胃剤、消化剤、整腸剤、鎮痙剤、粘膜修復剤、抗炎症剤、収れん剤、鎮吐剤、鎮咳剤、去痰剤、消炎酵素剤、鎮静催眠剤、抗ヒスタミン剤、カフェイン類、強心利尿剤、抗菌剤、血管収縮剤、血管拡張剤、局所麻酔剤、生薬エキス、ビタミン類、メントール類等が挙げられる。これらの栄養成分や薬理成分は、１種単独で使用してもよく、また２種以上を組み合わせて使用してもよい。また、これらの成分の含有量については、使用する成分の種類等に応じて適宜設定される。 Moreover, the tablet composition of the present invention may contain other nutritional components and pharmacological components in addition to the Bofutsushosan extract, if necessary. Such nutritional and pharmacological ingredients are not particularly limited as long as they are pharmaceutically acceptable, but include, for example, antacids, stomachic agents, digestive agents, intestinal regulation agents, antispasmodics, mucosal repair agents, anti-inflammatory agents, and astringents. agents, antiemetics, antitussives, expectorants, anti-inflammatory enzymes, sedative-hypnotics, antihistamines, caffeine, cardiac diuretics, antibacterial agents, vasoconstrictors, vasodilators, local anesthetics, herbal extracts, vitamins, menthol etc. These nutritional components and pharmacological components may be used alone or in combination of two or more. Further, the contents of these components are appropriately set depending on the types of components used.
製剤形態
本発明の錠剤組成物の製剤形態は、それ自体任意であり、通常、固形組成物として調製される。より具体的には、本発明の錠剤組成物の製剤形態としては、粉末及び造粒物（例えば顆粒等）が挙げられる。
Formulation The formulation form of the tablet composition of the present invention is arbitrary per se, and is usually prepared as a solid composition. More specifically, the formulation form of the tablet composition of the present invention includes powder and granules (eg, granules).
製造方法
本発明の錠剤組成物は、防風通聖散エキス、並びに必要に応じて添加される添加剤、基剤、及び／又は薬理成分を用いて、医薬分野で採用されている通常の製剤化手法に従って製造することができる。
Manufacturing method The tablet composition of the present invention can be formulated using the Bofutsushosan extract and additives, bases, and/or pharmacological ingredients added as necessary, using a conventional formulation adopted in the pharmaceutical field. It can be manufactured according to the method.
用途
本発明の錠剤組成物は、錠剤に成形される用途で用いられる。本発明の錠剤組成物から製造される錠剤（本発明の錠剤組成物を含む錠剤）の形状及び大きさ等は特に限定されない。錠剤の形状としては、円型、楕円型、三角型、四角型等が挙げられる。丸型錠の場合にあっては、直径６～１２ｍｍ、好ましくは８～１０ｍｍが挙げられる。錠剤の厚みとしては、３～８ｍｍ、好ましくは４～７ｍｍが挙げられる。一錠当たりの重量としては、２００～８００ｍｇ、好ましくは３００～６００ｍｇが挙げられる。本発明の錠剤組成物は、錠剤の硬度、崩壊性、及び耐摩損性に優れているため、一錠当たりの重量の割に厚みを薄くすることが可能である。
Applications The tablet composition of the present invention is used in applications where it is formed into tablets. The shape, size, etc. of tablets manufactured from the tablet composition of the present invention (tablets containing the tablet composition of the present invention) are not particularly limited. The shape of the tablet includes circular, oval, triangular, square, and the like. In the case of round tablets, the diameter is 6 to 12 mm, preferably 8 to 10 mm. The thickness of the tablet is 3 to 8 mm, preferably 4 to 7 mm. The weight per tablet is 200 to 800 mg, preferably 300 to 600 mg. Since the tablet composition of the present invention has excellent tablet hardness, disintegration properties, and abrasion resistance, it is possible to reduce the thickness relative to the weight of each tablet.
本発明の錠剤組成物から製造される錠剤は、素錠（裸錠）であってもよいし、薬剤の安定化、及び矯味や矯臭等の目的で表面にコーティングを施したコーティング錠であってもよい。コーティング錠としては、糖衣錠や、水溶性、腸溶性または胃溶性の高分子基剤を含むフィルムで被覆したフィルムコーティング剤（胃溶錠、腸溶錠）が挙げられる。本発明の錠剤組成物は、錠剤の硬度及び耐摩損性に優れているため、素錠であっても物理的に安定である。本発明の錠剤組成物から製造される素錠の硬度としては、例えば９０Ｎ以上、好ましくは９５Ｎ以上、より好ましくは１００Ｎ以上、さらに好ましくは１１０Ｎ以上、一層好ましくは１２０Ｎ以上、より一層好ましくは１２５Ｎ以上、特に好ましくは１３０Ｎ以上が挙げられる。 The tablets produced from the tablet composition of the present invention may be uncoated tablets (uncoated tablets) or coated tablets whose surfaces are coated for the purpose of stabilizing the drug and adding flavor or odor. Good too. Examples of coated tablets include sugar-coated tablets and film-coated tablets (gastric-coated tablets, enteric-coated tablets) coated with a film containing a water-soluble, enteric-coated, or gastric-soluble polymer base. Since the tablet composition of the present invention has excellent tablet hardness and abrasion resistance, it is physically stable even if it is a plain tablet. The hardness of the uncoated tablet produced from the tablet composition of the present invention is, for example, 90N or more, preferably 95N or more, more preferably 100N or more, even more preferably 110N or more, even more preferably 120N or more, even more preferably 125N or more. , particularly preferably 130N or more.
本発明の錠剤組成物を用いて錠剤を製造する方法は、例えば、本発明の錠剤組成物を用いて打錠する打錠工程を含み、必要に応じて、打錠工程に先立って、任意の成分を混合する混合工程、及び／又は（錠剤組成物が造粒物でない場合は）造粒工程を含むこともできる。打錠工程における打錠圧としては、例えば２００～４９０ｍｇ／錠の錠剤を製造する場合、４～２０ｋＮ、好ましくは５～１５ｋＮが挙げられる。本発明の錠剤組成物は硬度に優れているため、低い打錠圧で製造しても優れた硬度を達成することができる、従って、打錠装置への負荷を少なくすることで、打錠装置の長寿命化を図ることもできる。打錠装置への負荷を少なくする観点から、打錠圧は、より低い４～１２ｋＮとしてもよい。 The method for manufacturing a tablet using the tablet composition of the present invention includes, for example, a tableting step of compressing a tablet using the tablet composition of the present invention, and if necessary, prior to the tabletting step, an optional It may also include a mixing step to mix the ingredients and/or a granulation step (if the tablet composition is not granulated). The tableting pressure in the tableting process is, for example, 4 to 20 kN, preferably 5 to 15 kN, when producing tablets of 200 to 490 mg/tablet. Since the tablet composition of the present invention has excellent hardness, it can achieve excellent hardness even when manufactured with low tableting pressure. Therefore, by reducing the load on the tableting machine, It is also possible to extend the life of the From the viewpoint of reducing the load on the tableting device, the tableting pressure may be lower, 4 to 12 kN.
以下、本発明を実施例により具体的に説明するが、本発明はこれらの実施例に限定されるものではない。 EXAMPLES Hereinafter, the present invention will be specifically explained with reference to Examples, but the present invention is not limited to these Examples.
試験例
（１）防風通聖散エキス末の調製
表１に示す組成の原料生薬調合物を調製し、水２０倍重量を用いて約１００℃で１時間抽出し、遠心分離して抽出液を得、減圧下で濃縮してスプレードライヤーを用いて乾燥し、各防風通聖散エキス末（エキスａ～ｄ、エキスＡ～Ｄ）を得た。なお、スプレードライヤーによる乾燥は、抽出液を回転数１００００ｒｐｍのアトマイザーに落下させ、１５０℃の空気の熱風を供給して行った。
Test Example (1) Preparation of Bofutsushosan Extract Powder A raw herbal medicine preparation with the composition shown in Table 1 was prepared, extracted at about 100°C for 1 hour using 20 times the weight of water, and centrifuged to obtain the extract. The obtained extract was concentrated under reduced pressure and dried using a spray dryer to obtain each Bofutsushosan extract powder (extracts a to d, extracts A to D). Note that drying with a spray dryer was performed by dropping the extract into an atomizer with a rotational speed of 10,000 rpm, and supplying hot air at 150°C.
（２）防風通聖散エキスの錠剤組成物の調製
上記（１）で調製した防風通聖散エキス末（エキスａ～ｄ、エキスＡ～Ｄ）と、表２に示す添加物とを、表示の比率で配合し、造粒することで、顆粒状の錠剤組成物を得た。
（３）防風通聖散エキスを含む錠剤の作製
上記（２）で調製した錠剤組成物を、１２ｋＮの打圧で打錠することにより、素錠（１錠当たり重さ３００ｍｇ）を作製した。
(2) Preparation of tablet composition of Bofutsushosan extract The Bofutsushosan extract powder (extracts a to d, extracts A to D) prepared in the above (1) and the additives shown in Table 2 are labeled. A granular tablet composition was obtained by blending and granulating at the ratio of .
(3) Preparation of tablets containing Bofutsushosan extract Uncoated tablets (weighing 300 mg per tablet) were prepared by compressing the tablet composition prepared in (2) above with a compression pressure of 12 kN.
（４）錠剤特性評価
上記（３）で製造した錠剤について、以下の評価を行った。結果を表２に示す。
(4) Evaluation of tablet characteristics The tablets produced in (3) above were evaluated as follows. The results are shown in Table 2.
（４－１）硬度
ロードセル式錠剤硬度計を用いて、破断動作速度０．５ｍｍ／分で硬度（Ｎ）を測定した。
（４－２）崩壊性
日本薬局方（第十七改正）記載の崩壊試験法に従って崩壊性の評価を行った。崩壊性（分）は、錠剤６個について得られた崩壊時間（分）の平均値として導出した。
（４－３）摩損度
錠剤６個を１５ｍＬチューブ（外径１７ｍｍ）に入れ、３０分振とう（振とう幅４０ｍｍ、振とう速度１５０ｒｐｍ）した。その後、錠剤を取り出し、チューブ内壁に付着した粉体の重量を測定し、以下の式に基づいて摩損度（％）を導出した。
摩損度（％）＝チューブ内壁に付着した粉体重量（ｇ）／振とう前の錠剤６個分の重量（ｇ）×１００
(4-1) Hardness Hardness (N) was measured using a load cell tablet hardness meter at a breaking operation speed of 0.5 mm/min.
(4-2) Disintegration property Disintegration property was evaluated according to the disintegration test method described in the Japanese Pharmacopoeia (17th revision). The disintegration property (minutes) was calculated as the average value of the disintegration times (minutes) obtained for six tablets.
(4-3) Friability Six tablets were placed in a 15 mL tube (outer diameter 17 mm) and shaken for 30 minutes (shaking width 40 mm, shaking speed 150 rpm). Thereafter, the tablet was taken out, the weight of the powder adhering to the inner wall of the tube was measured, and the degree of friability (%) was derived based on the following formula.
Friability (%) = Weight of powder attached to the inner wall of the tube (g) / Weight of 6 tablets before shaking (g) x 100
表１及び表２から明らかな通り、１００重量部当たり生ショウキョウを３～２２重量部含む防風通聖散の生薬調合物から得られたエキスを含む錠剤組成物は、製錠後における硬度、崩壊性及び耐摩損性を顕著に向上できることが認められた（実施例１～４）。一方で、防風通聖散の生薬調合物１００重量部当たりの生ショウキョウの量が１．１重量部である場合（比較例３）及び生ショウキョウの量が３０．９重量部である場合（比較例４）では、実施例１～４で認められたような錠剤特性の顕著な向上効果は認められなかった。 As is clear from Tables 1 and 2, the tablet composition containing the extract obtained from the bofutsushosan crude drug formulation containing 3 to 22 parts by weight of fresh ginger per 100 parts by weight had a hardness after tableting, It was found that the disintegration properties and abrasion resistance could be significantly improved (Examples 1 to 4). On the other hand, when the amount of raw ginger is 1.1 parts by weight per 100 parts by weight of Bofutsushosan crude drug formulation (Comparative Example 3) and when the amount of raw ginger is 30.9 parts by weight In (Comparative Example 4), no significant improvement effect on tablet properties as observed in Examples 1 to 4 was observed.
さらに、防風通聖散の生薬調合物１００重量部当たりの生ショウキョウの量が１．１重量部である場合（比較例３）に対して生ショウキョウの量が４．３重量部である場合（実施例２）に錠剤特性の顕著な向上効果が認められた一方で、防風通聖散の生薬調合物１００重量部当たりのショウキョウの量が１．１重量部である場合（比較例１）に対してショウキョウの量が４．３重量部である場合（比較例２）には錠剤特性の向上が全く認められなかったことに鑑みると、実施例１～４で認められる錠剤特性の顕著な向上効果は、防風通聖散の生薬調合物において生ショウキョウを用い且つその量を１００重量部当たり３～２２重量部としたことによる特有の効果であることが判った。 Furthermore, compared to the case where the amount of raw ginger per 100 parts by weight of Bofutsushosan crude drug preparation is 1.1 parts by weight (Comparative Example 3), the amount of raw ginger is 4.3 parts by weight. In the case (Example 2), a remarkable effect of improving the tablet properties was observed, while in the case where the amount of ginger per 100 parts by weight of Bofutsushosan crude drug preparation was 1.1 parts by weight (Comparative Example) Considering that no improvement in tablet properties was observed when the amount of ginger was 4.3 parts by weight compared to 1) (Comparative Example 2), the tablet properties observed in Examples 1 to 4 were It has been found that the remarkable improvement effect of 3 to 22 parts by weight per 100 parts by weight of raw ginger is used in the herbal medicine preparation of Bofutsushosan.
処方例
試験例１で調製した防風通聖散エキス末（エキスＣ）を用い、上記試験例と同じ方法で、表３～６に示す処方の錠剤組成物の調製及び錠剤の作製を行った。いずれの錠剤も、１００重量部当たりの生ショウキョウ量が３～２２重量部でない防風通聖散の生薬調合物から得られたエキスを含む場合に比べて、硬度、崩壊性及び耐摩損性が向上していた。また、防風通聖散エキス末をエキスＡ、Ｂ、Ｄに変更したいずれの場合も、１００重量部当たりの生ショウキョウ量が３～２２重量部でない防風通聖散の生薬調合物から得られたエキスを含む場合に比べて、硬度、崩壊性及び耐摩損性が向上していた。
Formulation Example Using the Bofutsushosan extract powder (Extract C) prepared in Test Example 1, tablet compositions and tablets with the formulations shown in Tables 3 to 6 were prepared in the same manner as in the above Test Example. Both tablets had better hardness, disintegration, and abrasion resistance than those containing the extract obtained from the Bofutsushosan crude drug formulation containing less than 3 to 22 parts by weight of raw ginger per 100 parts by weight. It was improving. In addition, in any case where the Bofutsushosan extract powder is changed to Extract A, B, or D, the amount of raw ginger per 100 parts by weight is not obtained from the crude drug preparation of Bofutsushosan that is not 3 to 22 parts by weight. The hardness, disintegration properties, and abrasion resistance were improved compared to the case containing the extracted extract.
Claims (4)
前記防風通聖散エキスの抽出に使用された生薬調合物が、前記生薬調合物の１００重量部当たり生ショウキョウを３～２２重量部含む、錠剤組成物。 A tablet composition comprising Bofutsushosan extract,
A tablet composition, wherein the crude drug preparation used to extract the Bofutsushosan extract contains 3 to 22 parts by weight of fresh ginger per 100 parts by weight of the crude drug preparation.
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