JP2012224581A - Pharmaceutical composition - Google Patents
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- JP2012224581A JP2012224581A JP2011093799A JP2011093799A JP2012224581A JP 2012224581 A JP2012224581 A JP 2012224581A JP 2011093799 A JP2011093799 A JP 2011093799A JP 2011093799 A JP2011093799 A JP 2011093799A JP 2012224581 A JP2012224581 A JP 2012224581A
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- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000000284 extract Substances 0.000 claims abstract description 82
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- JAUGGEIKQIHSMF-UHFFFAOYSA-N dialuminum;dimagnesium;dioxido(oxo)silane;oxygen(2-);hydrate Chemical compound O.[O-2].[O-2].[Mg+2].[Mg+2].[Al+3].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O.[O-][Si]([O-])=O JAUGGEIKQIHSMF-UHFFFAOYSA-N 0.000 abstract 1
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- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
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- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 1
- 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
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 150000004645 aluminates Chemical class 0.000 description 1
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- 229940084030 carboxymethylcellulose calcium Drugs 0.000 description 1
- 235000005607 chanvre indien Nutrition 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 239000008726 choto-san Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000000748 compression moulding Methods 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
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- 239000003205 fragrance Substances 0.000 description 1
- 235000008434 ginseng Nutrition 0.000 description 1
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 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
- 239000000391 magnesium silicate Substances 0.000 description 1
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- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
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Landscapes
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Description
本発明は、漢方エキスを高濃度で含有する組成物に関する。さらに詳しくは、漢方エキスを８７重量％以上含有する錠剤に関する。 The present invention relates to a composition containing a Kampo extract at a high concentration. More specifically, the present invention relates to a tablet containing 87% by weight or more of Kampo extract.
漢方エキスを含む錠剤を製造する場合、錠剤中のエキス濃度が増加するに伴って崩壊時間が著しく延長するため、エキスの含有量には限界があることが知られている。また、油脂成分含量の高いエキスの場合には、エキス含有量が一定濃度以下でないと錠剤に実用的な強度を与えることが難しい（非特許文献１参照）。このような事情から、エキスを高濃度に含有する錠剤の設計には課題が多く、１錠あたりの漢方エキス含有量を減らした錠剤を設計することが多い。しかし、この場合、患者が必要量の漢方エキスを服用するためには多量の添加剤（賦形剤、崩壊剤、結合剤など）も共に服用することになり、１回当たりの服用量が増大する。このため、漢方エキスを錠剤として服用する場合には、多数の錠剤を服用するか、あるいは、１錠あたりのサイズが大きい（１錠あたりの重量が大きい）錠剤を服用しなければならず、患者に負担が生じることになる。また、漢方エキス含有量を減らした錠剤を製造するには添加剤の原体を多量に用いることとなり、錠剤の製造に時間を要するなど生産効率が悪くなる。 When manufacturing a tablet containing a Kampo extract, it is known that the content of the extract is limited because the disintegration time is remarkably prolonged as the extract concentration in the tablet increases. Moreover, in the case of an extract with a high fat content, it is difficult to give the tablet practical strength unless the extract content is below a certain level (see Non-Patent Document 1). Under such circumstances, there are many problems in designing a tablet containing an extract at a high concentration, and tablets having a reduced Kampo extract content per tablet are often designed. However, in this case, in order for the patient to take the necessary amount of Kampo extract, a large amount of additives (excipients, disintegrants, binders, etc.) must be taken together, increasing the dose per dose. To do. For this reason, when taking Kampo extract as a tablet, you must take a large number of tablets or take tablets with a large size per tablet (heavy weight per tablet) Will be burdened. Moreover, in order to produce a tablet with a reduced amount of Kampo extract, a large amount of the active ingredient of the additive is used, and the production efficiency is deteriorated because it takes time to produce the tablet.
これに対して、例えば、特許文献１、２では、漢方薬の抽出液もしくはその濃縮液に、多孔性無水ケイ酸等の水不溶性超微粒子を添加して噴霧乾燥した粉末を用いることにより、崩壊性が向上した錠剤が得られることが報告されている。このようにして得られる錠剤のうち最もエキス配合量が多いものとしては、具体的には、当帰芍薬エキスに多孔性無水ケイ酸を添加して得られた、漢方エキス濃度が８５％である錠剤（特許文献１の実施例５）が開示されている。 On the other hand, for example, in Patent Documents 1 and 2, by using a powder obtained by adding water-insoluble ultrafine particles such as porous silicic acid to a herbal medicine extract or a concentrated solution thereof, It has been reported that improved tablets can be obtained. Specifically, among the tablets obtained in this way, the extract containing the most amount is specifically, the Kampo extract concentration obtained by adding porous anhydrous silicic acid to Toki's extract is 85%. A tablet (Example 5 of Patent Document 1) is disclosed.
特許文献３では、安中散を含有する混合末に軽質無水ケイ酸及び低置換度ヒドロキシプロピルセルロースを添加混合したものを圧縮成型後、破砕して得られた顆粒に、さらに軽質無水ケイ酸を混合して圧縮成型することで、圧縮成型性に優れ、かつ、崩壊時間の遅延が抑制された安中散含有錠剤が得られることが報告されている。かかる方法によれば、安中散は錠剤全体に対して２０〜８０重量％配合することができ、例えば、実施例１では、安中散末と芍薬甘草湯エキス末の漢方エキス末を合計６８％含有する錠剤が開示されている。 In Patent Document 3, light anhydrous silicic acid and low-substituted hydroxypropylcellulose added to and mixed with powder containing Anchu-san are compression-molded and then crushed into granules obtained by further adding light anhydrous silicic acid. It has been reported that by mixing and compression molding, an anchu-san containing tablet with excellent compression moldability and suppressed delay of disintegration time can be obtained. According to this method, Anchu-san can be blended in an amount of 20 to 80% by weight based on the whole tablet. For example, in Example 1, a total of 68 Kampo extract powders including Anchu-san powder and Shakuyakukanzoto extract powder are obtained. % Containing tablets are disclosed.
特許文献４では、漢方エキス粉末や生薬エキス粉末にケイ酸カルシウムを特定の重量比で混合したものを湿式造粒することにより得られた顆粒を用いることで、崩壊時間の短い漢方含有錠剤を製造する技術が開示されている。例えば、第１実施形態では、前記方法により製造した漢方エキス含有量が５０〜８０％の各種漢方含有錠剤について崩壊時間が長くとも１５分以内であることが確認されている。 In Patent Document 4, a Kampo-containing tablet with a short disintegration time is produced by using granules obtained by wet granulation of Kampo extract powder or herbal extract powder mixed with calcium silicate at a specific weight ratio. Techniques to do this are disclosed. For example, in the first embodiment, it is confirmed that the disintegration time is 15 minutes or less at the longest for various Kampo-containing tablets having a Kampo extract content of 50 to 80% produced by the above method.
特許文献５では、漢方エキス粉末もしくはその造粒品に、約２０〜１００メッシュに造粒した崩壊剤を配合することにより、崩壊性の良好な漢方エキス錠剤を製造する技術が開示されている。崩壊剤としては、クロスカルメロースナトリウム、カルボキシメチルセルロースなど一般に崩壊剤として用いられているものが用いられると記載されており、例えば、実施例１〜５では、桂枝茯苓丸料エキス粉末８５重量％に、合成ケイ酸アルミニウム８重量％、ステアリン酸マグネシウム１％、種々の粒度を有するカルボキシメチルセルロースカルシウム６重量％を配合した錠剤が開示されている。 Patent Document 5 discloses a technique for producing a Kampo extract tablet with good disintegration by blending a disintegrant granulated to about 20 to 100 mesh into a Kampo extract powder or a granulated product thereof. As a disintegrating agent, it is described that what is generally used as a disintegrating agent, such as croscarmellose sodium and carboxymethylcellulose, is used. Discloses a tablet containing 8% by weight of synthetic aluminum silicate, 1% of magnesium stearate and 6% by weight of carboxymethyl cellulose calcium having various particle sizes.
しかし、いずれの先行技術においても、１錠あたりに８７重量％以上もの漢方エキスを含有する場合については、一切開示されていおらず、さらなる高含量化が望まれている。 However, in any of the prior arts, the case of containing 87% by weight or more of Kampo extract per tablet is not disclosed at all, and further higher content is desired.
本発明の課題は、漢方エキス含有量が８７重量％以上であっても、崩壊性及び成形性に優れる錠剤を提供することにある。 The subject of this invention is providing the tablet which is excellent in disintegration and a moldability, even if a Kampo extract content is 87 weight% or more.
本発明者らが検討を重ねた結果、漢方エキスに、メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムを配合することにより、漢方エキス含有量が８７重量％以上である錠剤を成形性良く製造することができ、かつ、得られた錠剤の崩壊性が良好であることを見出し、本発明を完成するに至った。 As a result of repeated studies by the present inventors, by adding magnesium aluminate metasilicate and / or magnesium aluminate silicate to a Kampo extract, a tablet having a Kampo extract content of 87% by weight or more has good moldability. It has been found that the tablet can be manufactured and the disintegration property of the obtained tablet is good, and the present invention has been completed.
即ち、本発明は、（Ａ）漢方エキス、ならびに、（Ｂ）メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムを含有してなる錠剤であって、漢方エキス含有量が８７重量％以上である錠剤、に関する。 That is, the present invention is a tablet comprising (A) a Chinese medicine extract and (B) magnesium metasilicate aluminate and / or magnesium aluminate silicate, wherein the Kampo extract content is 87% by weight or more. Related to a tablet.
本発明の錠剤は、漢方エキスを８７重量％以上の割合で含有していても、成形性よく製造することができ、かつ、崩壊性も良好であるという優れた効果を奏する。また、漢方エキスを高濃度で含有する錠剤を製造することができるため、配合される添加剤の量が少量となり、１回あたりの添加剤の服用量を減らすことが可能となる。ひいては、１回あたりの服用錠数を減らしたり、１錠の大きさを小さくしたりすることが可能となる。また、本発明の錠剤は、煩雑な工程を必要としないため、効率よく製造することが可能である。 Even if the tablet of the present invention contains a Kampo extract in a proportion of 87% by weight or more, it has an excellent effect that it can be produced with good moldability and has good disintegration. In addition, since a tablet containing a high concentration of Kampo extract can be produced, the amount of the additive to be blended becomes small, and the dose of the additive per time can be reduced. As a result, it is possible to reduce the number of tablets taken at one time or to reduce the size of one tablet. Moreover, since the tablet of this invention does not require a complicated process, it can be manufactured efficiently.
本発明の錠剤は、（Ａ）漢方エキス、ならびに、（Ｂ）メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムを含有してなる錠剤であって、漢方エキス含有量が８７重量％以上であることに特徴を有する。 The tablet of the present invention is a tablet comprising (A) Chinese medicine extract and (B) magnesium aluminate metasilicate and / or magnesium aluminate, wherein the Kampo extract content is 87% by weight or more. It is characterized by being.
従来、メタケイ酸アルミン酸マグネシウム及びケイ酸アルミン酸マグネシウムは、滑沢剤、吸着剤、結合剤、安定化剤、流動化剤等として医薬品に配合されている。本願発明では、メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムを、漢方エキスを高濃度に含有する場合にでも少量配合するだけで、驚くべきことに、圧縮成形性が飛躍的に高まることを見出した。また、これを錠剤にした時にその崩壊性が大きく改善されることを見出した。即ち、漢方エキスを１錠中に高濃度配合できることを見出した。 Conventionally, magnesium aluminate metasilicate and magnesium aluminate silicate are blended in pharmaceuticals as lubricants, adsorbents, binders, stabilizers, fluidizing agents, and the like. In the present invention, surprisingly, the compression moldability is remarkably increased only by blending a small amount of magnesium aluminate metasilicate and / or magnesium aluminate silicate even when the Kampo extract is contained in a high concentration. I found. Moreover, when this was made into the tablet, it discovered that the disintegration was improved greatly. That is, it has been found that a Kampo extract can be blended at a high concentration in one tablet.
このメタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムによる効果のメカニズムは不明であるが、他の添加物を配合した場合、例えば、一般的な流動化剤等を配合した場合には、漢方エキス含有錠の圧縮成形性も崩壊性も劣るものであったり、圧縮成形性を高めることが可能であったとしても崩壊性が劣るものであったが、メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムを配合した場合には圧縮成形性と崩壊性という相反する特性の両立が可能となり、メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムに特異的な作用であると考えられる。 The mechanism of the effect of this magnesium metasilicate aluminate and / or magnesium aluminate silicate is unknown, but when other additives are blended, for example, when general fluidizing agents are blended, The extract-containing tablets are inferior in compression moldability and disintegration, and even if it is possible to improve compression moldability, the disintegration is inferior, but magnesium metasilicate and / or silicic acid When magnesium aluminate is blended, it is possible to achieve both contradictory properties of compression moldability and disintegration, and this is considered to be an action specific to magnesium aluminate metasilicate and / or magnesium aluminate silicate.
本発明に用いられる（Ａ）漢方エキスとしては、医薬上、薬理学的に又は生理学的に許容されるものであればよく、構成する生薬の組合せやその配合比率についても特に制限されない。例えば、「改訂 一般用漢方処方の手引き」〔財団法人 日本公定書協会監修、日本漢方生薬製剤協会編集、じほう発行、平成21年〕や「改訂 一般用漢方処方の手引き 平成22年4月1日通知（加減方追加）対応追補版」〔財団法人 日本公定書協会監修、日本漢方生薬製剤協会編集、じほう発行、平成22年〕に記載されている漢方処方をエキス化、即ち、漢方処方の生薬を用いて日本薬局方 エキス剤の製法等に従って得ることが出来る。漢方処方の具体例としては、防風通聖散、安中散、安中散加茯苓、胃風湯、胃苓湯、茵チン蒿湯、茵チン五苓散、温経湯、温清飲、温胆湯、延年半夏湯、黄耆建中湯、黄ゴン湯、応鐘散、黄連阿膠湯、黄連解毒湯、黄連湯、乙字湯、乙字湯去大黄、化食養脾湯、カッ香正気散、葛根黄連黄ゴン湯、葛根紅花湯、葛根湯、葛根湯加川キュウ辛夷、加味温胆湯、加味帰脾湯、加味解毒湯、加味逍遙散、加味逍遙散加川キュウ地黄、加味平胃散、乾姜人参半夏丸、甘草瀉心湯、甘草湯、甘麦大棗湯、帰耆建中湯、桔梗湯、帰脾湯、キュウ帰膠艾湯、キュウ帰調血飲、キュウ帰調血飲第一加減、響声破笛丸、杏蘇散、苦参湯、駆風解毒散、荊芥連翹湯、鶏肝丸、桂枝湯、桂枝加黄耆湯、桂枝加葛根湯、桂枝加厚朴杏仁湯、桂枝加芍薬生姜人参湯、桂枝加芍薬大黄湯、桂枝加芍薬湯、桂枝加朮附湯、桂枝加竜骨牡蛎湯、桂枝加苓朮附湯、桂枝人参湯、桂枝茯苓丸、桂枝茯苓丸料加ヨク苡仁、啓脾湯、荊防敗毒散、桂麻各半湯、鶏鳴散加茯苓、堅中湯、甲字湯、香砂平胃散、香砂養胃湯、香砂六君子湯、香蘇散、厚朴生姜半夏人参甘草湯、五虎湯、牛膝散、五積散、牛車腎気丸、呉茱萸湯、五物解毒散、五淋散、五苓散、柴陥湯、柴胡加竜骨牡蛎湯、柴胡桂枝乾姜湯、柴胡桂枝湯、柴胡清肝湯、柴芍六君子湯、柴朴湯、柴苓湯、左突膏、三黄散、三黄瀉心湯、酸棗仁湯、三物黄ゴン湯、滋陰降火湯、滋陰至宝湯、紫雲膏、四逆散、四君子湯、滋血潤腸湯、七物降下湯、柿蒂湯、四物湯、炙甘草湯、芍薬甘草湯、鷓鴣菜湯、蛇床子湯、十全大補湯、十味敗毒湯、潤腸湯、蒸眼一方、生姜瀉心湯、小建中湯、小柴胡湯、小柴胡湯加桔梗石膏、小承気湯、小青竜湯、小青竜湯加杏仁石膏、小青龍湯加石膏、椒梅湯、小半夏加茯苓湯、消風散、升麻葛根湯、逍遙散、四苓湯、辛夷清肺湯、秦キュウ姜活湯、秦キュウ防風湯、参蘇飲、神秘湯、参苓白朮散、清肌安蛔湯、清湿化痰湯、清暑益気湯、清上ケン痛湯、清上防風湯、清心蓮子飲、清肺湯、折衝飲、川キュウ茶調散、千金鶏鳴散、銭氏白朮散、疎経活血湯、蘇子降気湯、大黄甘草湯、大黄牡丹皮湯、大建中湯、大柴胡湯、大柴胡湯去大黄、大半夏湯、竹茹温胆湯、治打撲一方、治頭瘡一方、治頭瘡一方去大黄、中黄膏、調胃承気湯、丁香柿蒂湯、釣藤散、猪苓湯、猪苓湯合四物湯、通導散、桃核承気湯、当帰飲子、当帰建中湯、当帰散、当帰四逆湯、当帰四逆加呉茱萸生姜湯、当帰芍薬散、当帰湯、当帰貝母苦参丸、独活葛根湯、独活湯、二朮湯、二陳湯、女神散、人参養栄湯、人参湯、排膿散、排膿湯、麦門冬湯、八味地黄丸、半夏厚朴湯、半夏瀉心湯、半夏白朮天麻湯、白虎湯、白虎加桂枝湯、白虎加人参湯、不換金正気散、伏竜肝湯、茯苓飲、茯苓飲加半夏、茯苓飲合半夏厚朴湯、茯苓沢瀉湯、分消湯、平胃散、防已黄耆湯、防已茯苓湯、補気健中湯、補中益気湯、補肺湯、麻黄湯、麻杏甘石湯、麻杏ヨク甘湯、麻子仁丸、揚柏散、ヨク苡仁湯、抑肝散、抑肝散加陳皮半夏、六君子湯、立効散、竜胆瀉肝湯、苓姜朮甘湯、苓桂甘棗湯、苓桂朮甘湯、六味丸、麻黄附子細辛湯、黄耆桂枝五物湯、解労散、加味四物湯、枳縮二陳湯、杞菊地黄丸、紫胡疎肝湯、柴蘇飲、芍薬甘草附子湯、沢瀉湯、竹葉石膏湯、知柏地黄丸、中建中湯、定悸飲、当帰芍薬散加黄耆釣藤、当帰芍薬散加人参、当帰芍薬散加附子、排膿散及湯、八解散、附子理中湯、味麦地黄丸、明朗飲、抑肝散加芍薬黄連、連珠飲等が例示される。 The Chinese medicine extract (A) used in the present invention is not particularly limited as long as it is a pharmaceutical, pharmacologically or physiologically acceptable one, and the combination of herbal medicines and the blending ratio thereof are not particularly limited. For example, “Guideline for Revised Kampo Prescription” (supervised by the Japan Standards Association, edited by the Japan Herbal Medicine Association, published by Jiho, 2009) and “Guideline for Revised Kampo Prescription April 1, 2010 An expanded version of the Kampo prescription described in “Notification (addition and subtraction added) Supplementary edition” (supervised by the Japan Association of Standards Association, edited by the Japanese Herbal Medicine Association, published by Jiho, 2010) Can be obtained according to the manufacturing method of the Japanese Pharmacopoeia extract. Specific examples of Kampo prescriptions include Fufutsu Seiki, Anchu-san, Annaka-san, Ganfu-to, Gabuchi-yu, Sakai Chin-to, Sakai Chin Go-san, Unkei-to, Warm-and-drink, Hot-boiled hot water, Ennenhan summer hot water, Huanglong Jianchu hot water, Huang-gon hot water, Okansan, Hokuren Aji hot water, Huangren detoxifying hot water, Houren hot water, Otsuji hot water, Otsuji hot water leaving Daihyo, Kayaku no Splenic hot water, Kasaka Sankisan, Kakkon Houren Huang-Gon, Kakkon Benkahana-yu, Kakkon-yu, Kakone-yu Kagawa Spicy Hot Spring, Kami Hot-boiled Hot Spring, Kami Kaitou-yu, Kami Detoxification Hot Water, Kami-Sanyu, Kami-San Kagawa Kyu Ji-Huang, Kamiheigasakusan, Inui-Ginseng Hanatsumaru, Liquorice Hot Spring, Licorice Hot Spring, Sweet Barley Hot Spring, Kikai Kenchu Hot Spring, Kikyo Hot Spring, Kisui Hot Spring, Kyu Ki-Gai Hot Spring, Kyu Kisei Blood Drink, Kyu Home First adjustment of blood-drinking, Hibiki-fu-Fuemaru, Anzu-san, Nana-san, Kaifu-to-doku-san, Kureren-yu, Chicken liver-maru, Katsue-yu, Keishika-kao-yu, Keishika-kakatsu-yu , Katsueka Atsu Park Anjinyu, Katsueka Ginseng Ginseng Hot Spring, Katsueda Shakuyaku Daioyu, Keishika Kayakuyu, Katsueka Kayutsuyu, Katsueka Dragon Bone Oysteryu, Keishika Katsukiyuyu, Keishijinjin-yu, Keishi Karasuma, Keishi Karasuma Yokajin , Keisyu-to, Tsumugi detoxification powder, Katsura-han Hanyu, Chicken narcissus hot water, Kenchu-yu, Ko-ji-yu, Kosa-hiragashira-san, Kosa-no-yaku-to, Kosa-Rokukimiko-to, Kosa-san , Kopak Ginger Hanatsu Ginseng Amakusa-yu, Gotora-yu, Gyu-Kyo-san, Gokan-san, Ushizura-Ken-maru, Kureyu-yu, Gomono-detox-san, Gojo-san, Gojo-san, Goka-san Keel oyster bath, Saiko katsushi dry bath, Saiko katsushi hot water, Saiko Seiki liver bath, Saiko rikkunshiyu, Sabak hot water, Sakai hot water, left plaster, Sankosan, Sankoshinshin hot water, Suijin hot water, Three Monogon Gon-yu, Shi-in Furu-yu, Shi-in Zouho-yu, Shiun-gyo, Shikaku-san, Shikinko-yu, Shige-Jun-yu, Shichi-jyu-sen-yu, Tsuku-yu, Yotsumono-yu, Tsuga-kanzo-to, Glaze Licorice hot water, beef hot spring, snake bed child hot water, Juzen Daiyu hot water, Jumi-detoxicated hot water, Jun-in hot water, steamed eye, ginger heart hot water, small Nakayu, Shosaikoyu, Shosaikoyu Kyokyo-gypsum, Kojoki-yu, Shosei-ryu, Shosei-ryu-ka-anjin-gypsum, Shosei-ryu-ka-gypsum, Ume-yu, Shohanka-ka-yu, Shoufu-san Hakone, Yusan, Shijonawate, Karin Kiyoku-yu, Sakai Kyu Kou Hot Spring, Sakai Kyu Fengyu, Sansou Drinking, Mystic Hot Spring, Sanraku Hakuensan, Kiyohisa Antoyu, Kiyozuka Tokuyu , Kiyotaka Kouki, Kiyokami Ken-to, Kiyokami Fudo-yu, Seishin Renko Drinking, Kiyo-no-yu, Negoti Drinking, Kawa Kyu-cha-san, Senkin-Chicken-san, Qianji Haku-san Kogeki-to, Dai-kokanzo-yu, Dai-ko peony-skin-yu, Daikenchu-yu, Dai-saiko-yu, Dai-saiko-yu-de-dai-o-ko, most summer bath, bamboo-boiled hot-boiled hot water, bruise one, juniper one, head Azalea Daiochi, Chuo-Otsuka, Toki-gaki-to, Choko-san, Choto-san, Tsuga-to, Tsuyu-yu Gomono-yu, Tsutsu-san, Toukoku-jo-ki-to, Toki Dinko , Tokikenchu, Tokisan, Toki Yotsukato, Toki Shikaka-Gyu Gyoyu, Toki Seiyaku, Toki-yu, Tokaikai Mother Nansen-maru, Tokiwa Kakkon-yu, Tokiwa-yu, Futaba-yu, Ni-Cen-yu, Megami-san, Ninjin-yoei-yu, Ginseng-yu, Dyu-yu-san, Dyu-yu-yu, Bakumon-toyu , Hachimi-jio-maru, Semi-summer Koboku-yu, Hanka-shashinshin-yu, Hanka-white birch Tenma-yu, Shira-Tora-yu, Shira-Toraka-Katsura-yu, Shira-Tora-Kinjin-yu, Insane-money-sanity Kahan Summer, Sakai Drinking Midsummer Koboku Hot Spring, Serizawa Hot Spring, Minsoku Hot Spring, Hiragasaku, Hakusen Houyu, Hohagi Hot Spring, Reiki Kenchu Hot Spring, Hochuekki Hot Spring, Hyukan Hot Spring, Mao Hot water, maso kanishi-yu, maso yoku amyu, asako jinmaru, gangesan, yoku jinninyu, yokukansan, yokukansanka chinsatsu summer, rikkunshiyu, tachi-san , 苓 姜 朮 甘 湯, 苓 桂 甘 棗湯, 苓 桂 朮 甘 湯, Rokumi Maru, Mao-bushi Shokuyu, Huangguo Katsura Gotoyu, Kano-san, Kami four-boiled hot water, Kageri-jenyu, 杞 gikuchi Huang Maru, Shikouhato, Shiso-drinking, Shakuyaku licorice-boiled hot water, Sawa-yu, Takeba gypsum, Chichiji Houmaru, Chukenchu , Sadagomi, Tokiyaku Sanka Houen Choto, Tokiyaku Sanka Ginseng, Toki Sakuyaku Sanka Tsuke, Dyuyu Syuyu, Hachi-San, Tsukeri Richu-yu, Ajimu-jio-maru, Akira Drink Examples include Yokukansan Gakuyaku Huangren, Renju Drinking, etc.
上記「一般用漢方処方の手引き」には、漢方エキスを構成する生薬の組合せやその配合量が記載されているが、構成する生薬やその配合比率を適宜変更して得られる漢方エキスであっても、本発明に使用することができる。例えば、防風通聖散エキスは、防風１．２重量部、黄ごん２．０重量部、大黄１．５重量部、芒硝１．５重量部、麻黄１．２重量部、石膏２〜３重量部、白朮２．０重量部、荊芥１．２重量部、連翹１．２重量部、桔梗２．０重量部、山梔子１．２重量部、芍薬１．２重量部、当帰１．２重量部、川きゅう１．２重量部、薄荷１．２重量部、滑石３〜５重量部、生姜１．２重量部、及び甘草２．０重量部からなる混合原料の抽出物として知られているが、白朮を含まないもの、配合比率を適宜変更したもの等であってもよい。抽出溶媒は特に限定されないが、水やエタノールが好ましい。 The above-mentioned “Guide for general-purpose Kampo prescription” describes the combination of herbal medicines constituting the Kampo extract and the blending amount thereof, but is a Kampo extract obtained by appropriately changing the constituting herbal medicine and its blending ratio. Can also be used in the present invention. For example, the windproof tsushosan extract is 1.2 parts by weight of windproof, 2.0 parts by weight of yellow rice, 1.5 parts by weight of large yellow, 1.5 parts by weight of mirabilite, 1.2 parts by weight of hemp, 2-3 gypsum. Parts by weight, white birch 2.0 parts by weight, firewood 1.2 parts by weight, ream 1.2 parts by weight, bellflower 2.0 parts by weight, yam 1.2 parts by weight, glaze 1.2 parts by weight, Toki 1.2 Known as an extract of mixed raw materials consisting of parts by weight, 1.2 parts by weight of river cucumber, 1.2 parts by weight of light load, 3-5 parts by weight of talc, 1.2 parts by weight of ginger, and 2.0 parts by weight of licorice However, it may be one that does not contain white birch or one that has been appropriately changed in the blending ratio. The extraction solvent is not particularly limited, but water and ethanol are preferable.
これらの漢方エキスは、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。好適な例としては、防風通聖散エキス、防已黄耆湯エキス、当帰飲子エキス、柴胡加竜骨牡蛎湯エキス、補中益気湯エキス、加味帰脾湯エキス、牛車腎気丸エキス、及び独活葛根湯エキスからなる群より選ばれる少なくとも１種のエキスが挙げられる。 These Chinese medicine extracts may be used alone or in combination of two or more. Preferable examples include Fufutsu Seisaku Extract, Hosei Koreiyu Extract, Toki Dinzi Extract, Saiko Karyu Bone Oyster Extract, Hochuekki-to Extract, Kamiki-Shiki-to Extract, Ushisha Renkimaru Examples thereof include at least one extract selected from the group consisting of an extract and an independent Kakkonto extract.
本発明で用いられる（Ｂ）メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムは、医薬上、薬理学的に又は生理学的に許容されるものであればよく、特に制限されない。例えば、比表面積は５０〜５００ｍ２／ｇが好ましく、１００〜３００ｍ２／ｇがより好ましい。また、粒子の形状は、粉末もしくは球形顆粒が好ましく、粉末がより好ましい。本発明で用いられる（Ｂ）メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムは、市販品を用いることができ、例えば、日本薬局方、日本薬局方外医薬品規格等に適合するものが使用される。また、好適な市販品としては、富士化学工業社製「ノイシリン（登録商標）」シリーズ、富田製薬社製「ネオアルミンＳ（登録商標）」等が挙げられる。 The (B) magnesium aluminate metasilicate and / or magnesium aluminate used in the present invention is not particularly limited as long as it is pharmaceutically and pharmacologically or physiologically acceptable. For example, the specific surface area is preferably 50~500m 2 / g, 100~300m 2 / g is more preferable. The particle shape is preferably powder or spherical granules, and more preferably powder. As the (B) magnesium aluminate metasilicate and / or magnesium aluminate used in the present invention, commercially available products can be used, for example, those complying with Japanese Pharmacopoeia, Japanese Pharmacopoeia Pharmaceutical Standards, etc. Is done. Moreover, as a suitable commercial item, "Neosilin (registered trademark)" series manufactured by Fuji Chemical Industry Co., Ltd., "Neoalumin S (registered trademark)" manufactured by Tomita Pharmaceutical Co., Ltd. and the like can be mentioned.
本発明の錠剤における（Ａ）漢方エキスの含有量は、該錠剤の総量１００重量％に対して、８７重量％以上であり、９０重量％以上が好ましく、９２重量％以上がより好ましく、９２〜９６重量％がさらに好ましい。 The content of the Chinese medicine extract (A) in the tablet of the present invention is 87% by weight or more, preferably 90% by weight or more, more preferably 92% by weight or more, with respect to 100% by weight of the total amount of the tablet. More preferred is 96% by weight.
本発明の錠剤における（Ｂ）メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムの含有量は、該錠剤の総量１００重量％に対して、１３重量％以下であり、１０重量％以下が好ましく、８重量％以下がより好ましく、２〜８重量％がさらに好ましく、３〜６重量％がよりさらに好ましい。なお、本明細書において、「メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムの含有量」又は「メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムの重量」とは、メタケイ酸アルミン酸マグネシウム及びケイ酸アルミン酸マグネシウムの合計重量のことを意味する。 The content of (B) magnesium aluminate metasilicate and / or magnesium aluminate in the tablet of the present invention is 13% by weight or less, preferably 10% by weight or less, with respect to 100% by weight of the total amount of the tablet. 8 wt% or less is more preferable, 2 to 8 wt% is more preferable, and 3 to 6 wt% is still more preferable. In the present specification, “content of magnesium aluminate metasilicate and / or magnesium aluminate silicate” or “weight of magnesium aluminate metasilicate and / or magnesium aluminate silicate” refers to aluminate metasilicate. It means the total weight of magnesium and magnesium aluminate silicate.
また、従来、錠剤を製造するためには、結合剤や滑沢剤等種々の添加剤を組み合わせて用いるが、本願発明では、錠剤の成形性及び崩壊性を改善する効果を得るために、（Ｂ）メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムの含有量は、（Ａ）漢方エキス以外の成分、即ち、錠剤から（Ａ）漢方エキスを除いた残余成分の総量１００重量％に対して、好ましくは３５重量％以上、より好ましくは４０〜９５重量％、さらに好ましくは４５〜９５重量％、さらに好ましくは５０〜９５重量％である。 Conventionally, in order to produce tablets, various additives such as binders and lubricants are used in combination. In the present invention, in order to obtain the effect of improving the moldability and disintegration of tablets, The content of B) magnesium aluminate metasilicate and / or magnesium aluminate silicate is 100% by weight of the total amount of the components other than (A) Kampo extract, that is, (A) the remaining component excluding Kampo extract from the tablet. Thus, it is preferably 35% by weight or more, more preferably 40 to 95% by weight, still more preferably 45 to 95% by weight, still more preferably 50 to 95% by weight.
本発明の錠剤において、（Ａ）漢方エキスの重量は、良好な成形性及び崩壊性を有し、かつ、服用可能な量とするために、（Ｂ）メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムの重量に対して、好ましくは７倍以上、より好ましくは１０倍以上、さらに好ましくは１２．５倍以上、さらに好ましくは１５倍以上である。また、好ましくは２００倍以下、より好ましくは１５０倍以下、さらに好ましくは１００倍以下、さらに好ましくは５０倍以下である。従って、（Ａ）漢方エキスと（Ｂ）メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムの重量比〔（Ａ）／（Ｂ）〕は、７〜２００が好ましく、１０〜１５０がより好ましく、１２．５〜１００がさらに好ましく、１５〜５０がさらに好ましい。 In the tablet of the present invention, (B) the weight of the Chinese medicine extract has good moldability and disintegration, and can be taken in an amount (B) magnesium aluminate metasilicate and / or silicic acid. Preferably it is 7 times or more with respect to the weight of magnesium aluminate, More preferably, it is 10 times or more, More preferably, it is 12.5 times or more, More preferably, it is 15 times or more. Further, it is preferably 200 times or less, more preferably 150 times or less, further preferably 100 times or less, and further preferably 50 times or less. Accordingly, the weight ratio [(A) / (B)] of (A) Kampo extract and (B) magnesium aluminate metasilicate and / or magnesium silicate is preferably 7 to 200, more preferably 10 to 150. 12.5-100 are more preferable and 15-50 are more preferable.
本発明の錠剤は、上記成分以外に、賦形剤、結合剤、崩壊剤、滑沢剤、甘味剤、矯味剤、防腐剤、キレート剤、抗酸化剤、清涼化剤、コーティング剤、安定化剤、流動化剤、粘稠剤、溶解補助剤、増粘剤、緩衝剤、香料、着色剤、吸着剤、湿潤剤、防湿剤、帯電防止剤、可塑剤、消泡剤、界面活性剤等の添加剤を含有することができる。添加剤の例としては、乳糖、白糖等の糖類；結晶セルロース、ヒドロキシプロピルセルロース等のセルロース類；ステアリン酸マグネシウム、夕ルク、酸化チタン等の無機物質等が挙げられる。 In addition to the above components, the tablet of the present invention includes excipients, binders, disintegrants, lubricants, sweeteners, flavoring agents, preservatives, chelating agents, antioxidants, cooling agents, coating agents, and stabilization agents. Agent, fluidizer, thickener, solubilizer, thickener, buffer, fragrance, colorant, adsorbent, wetting agent, moisture-proofing agent, antistatic agent, plasticizer, antifoaming agent, surfactant, etc. The additive may be contained. Examples of the additive include saccharides such as lactose and sucrose; celluloses such as crystalline cellulose and hydroxypropyl cellulose; inorganic substances such as magnesium stearate, evening lime, and titanium oxide.
本発明の錠剤は、（Ａ）漢方エキス、（Ｂ）メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムを含有し、かつ、漢方エキスの含有量が８７重量％以上であれば特に限定はなく、直接粉末圧縮法や顆粒圧縮法など当業者に公知の方法に従って、調製することができる。また、錠剤の形状や大きさも特に限定はなく、公知の方法に従って、糖衣やフィルムコート等のコーティング処理がされてもよい。 The tablet of the present invention contains (A) Kampo extract, (B) magnesium aluminate metasilicate and / or magnesium aluminate silicate, and the content of Kampo extract is 87% by weight or more. And can be prepared according to methods known to those skilled in the art such as direct powder compression method and granule compression method. Further, the shape and size of the tablet are not particularly limited, and coating treatment such as sugar coating or film coating may be performed according to a known method.
具体的には、例えば、漢方エキスに、メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウム、必要により、その他の添加剤を混合することにより得られた混合物を、そのまま、或いは公知の方法に従って造粒後に、打錠機に投入して成型加工する方法により調製することができる。本発明においては、造粒により成形性を向上させなくても効果が得られることから、漢方エキスに、メタケイ酸アルミン酸マグネシウム及び／又はケイ酸アルミン酸マグネシウムを配合し、漢方エキスの含有量が８７重量％以上となる混合物をそのまま直接打錠することができる。 Specifically, for example, a mixture obtained by mixing magnesium aluminate metasilicate and / or magnesium aluminate with other additives, if necessary, according to a known method. After granulation, it can be prepared by a method in which it is put into a tableting machine and molded. In the present invention, the effect can be obtained without improving the moldability by granulation. Therefore, the Kampo extract is blended with magnesium aluminate metasilicate and / or magnesium aluminate silicate, and the content of the Kampo extract is The mixture of 87% by weight or more can be directly tableted as it is.
以下、本発明を実施例に基づいて説明するが、本発明はこれらの実施例等によりなんら限定されるものではない。 EXAMPLES Hereinafter, although this invention is demonstrated based on an Example, this invention is not limited at all by these Examples.
実施例１〜３及び比較例１〜５
表１に示す防風通聖散エキスとステアリン酸マグネシウム以外の原料とを混合した後に、さらにステアリン酸マグネシウムを添加して混合後、５００μｍの篩で混合粉を篩過したものを打錠用混合末とした。これを打錠機を用いて、２００ｋＮの予圧を負荷後に表２に示す５００〜１５００ｋＮの本圧をかけて打錠した。なお、メタケイ酸アルミン酸マグネシウム「ノイシリンＦＬ１」（比表面積１５０ｍ２／ｇ）、「ノイシリンＦＨ２」（比表面積１１０ｍ２／ｇ）、「ノイシリンＵＦＬ２」（比表面積３００ｍ２／ｇ）はいずれも富士化学工業社製である。
Examples 1-3 and Comparative Examples 1-5
After mixing the windproof Tsushosan extract shown in Table 1 and raw materials other than magnesium stearate, magnesium stearate was further added and mixed, and then the mixed powder was sieved with a 500 μm sieve and mixed powder for tableting It was. This was tableted using a tableting machine after applying a preload of 200 kN and applying a main pressure of 500 to 1500 kN shown in Table 2. The magnesium aluminate metasilicate “Neusilin FL1” (specific surface area 150 m 2 / g), “Neusilin FH2” (specific surface area 110 m 2 / g), “Neusilin UFL2” (specific surface area 300 m 2 / g) are all Fuji Chemical. It is made by an industrial company.
得られた錠剤について、硬度計（ＰＨＡＲＭＡ ＴＥＳＴ社製、ＰＴＴＢ３１１Ｅ）を使用して硬度を測定した（ｎ＝５）。また、打錠圧が８００、１２００ｋＮの錠剤については、打錠終了時のキャッピング、スティッキングを調べ、成形性を評価した。硬度の平均値、及び、キャッピング、スティッキングの「あり」「なし」について、結果を表２に示す。なお、錠剤硬度は６〜２０ｋｐ程度のものが取り扱い性に優れることから好ましい。 About the obtained tablet, hardness was measured using a hardness meter (manufactured by PHARMA TEST, PTTB311E) (n = 5). For tablets with a tableting pressure of 800, 1200 kN, capping and sticking at the end of tableting were examined to evaluate moldability. The results are shown in Table 2 for the average value of hardness, and “with” and “without” capping and sticking. In addition, the tablet hardness of about 6 to 20 kp is preferable because of excellent handleability.
また、第十五改正日本薬局方 崩壊試験法に従って、崩壊試験装置（富山産業社製、ＮＴ−２ＨＦ）を用いて崩壊時間を測定し、崩壊性を評価した。測定試料としては、硬度が約１０ｋｐのものを６錠用いた。崩壊時間の最長値、最短値、そして６錠の平均崩壊時間を表２に示す。なお、各錠剤について、第十五改正日本薬局方 崩壊試験法 （１）即放性製剤の記載に従って、崩壊性の適否を併せて判定した。 Moreover, according to the 15th revision Japanese Pharmacopoeia disintegration test method, disintegration time was measured using the disintegration test apparatus (NT-2HF by Toyama Sangyo Co., Ltd.), and disintegration was evaluated. As a measurement sample, 6 tablets having a hardness of about 10 kp were used. The longest and shortest disintegration times and the average disintegration time for 6 tablets are shown in Table 2. For each tablet, the suitability of disintegration was also determined according to the description of the Fifteenth Revised Japanese Pharmacopoeia Disintegration Test Method (1) Immediate release preparation.
表２より、結晶セルロース等の一般的な錠剤で汎用される添加剤を用いて漢方エキス含有量が高い錠剤を製造した場合には、十分な硬度の錠剤を得ることが出来ない上、キャッピングが見られ、成形性が悪かった（比較例１〜比較例３）。また、従来の漢方エキスを含有する錠剤に配合されているケイ酸カルシウム（比較例４）、軽質無水ケイ酸（比較例５）を用いた場合、漢方エキス含有量が８７重量％以上という高い含有量でも、十分な硬度が得られ、キャッピングやスティッキングもなく、成形性は良好であったが、十分な崩壊性を得ることが出来なかった。一方、メタケイ酸アルミン酸マグネシウムの場合（実施例１〜３）には、漢方エキス含有量が８７重量％以上であっても、成形性よく製造することができ、また、十分な硬度を有しながらも崩壊性にも優れることが明らかである。 From Table 2, when a tablet with a high Kampo extract content is produced using an additive commonly used in general tablets such as crystalline cellulose, a tablet with sufficient hardness cannot be obtained, and capping It was seen and the moldability was bad (Comparative Examples 1 to 3). Further, when calcium silicate (Comparative Example 4) and light anhydrous silicic acid (Comparative Example 5) blended in a tablet containing a traditional Chinese medicine extract is used, the Kampo extract content is as high as 87% by weight or more. Even in the amount, sufficient hardness was obtained, there was no capping or sticking, and the moldability was good, but sufficient disintegration property could not be obtained. On the other hand, in the case of magnesium metasilicate aluminate (Examples 1 to 3), even if the Kampo extract content is 87% by weight or more, it can be produced with good moldability and has sufficient hardness. However, it is clear that it is excellent in disintegration.
実施例４
表３に示す防已黄耆湯エキスとステアリン酸マグネシウム以外の原料とを混合した後に、さらにステアリン酸マグネシウムを添加して混合後、５００μｍの篩で混合粉を篩過したものを打錠用混合末とした。これを打錠機を用いて、２００ｋＮの予圧を負荷後に８００〜１０００ｋＮの本圧をかけて打錠した。なお、メタケイ酸アルミン酸マグネシウムは、「ノイシリンＵＦＬ２ 」（比表面積３００ｍ２／ｇ、富士化学工業社製）を使用した。
Example 4
After mixing the anti-Kojito extract shown in Table 3 and raw materials other than magnesium stearate, magnesium stearate was further added and mixed, and then the mixed powder was sieved with a 500 μm sieve and mixed for tableting. The end. This was tableted by applying a main pressure of 800 to 1000 kN after loading with a preload of 200 kN using a tableting machine. As the magnesium aluminate metasilicate, “Neucillin UFL2” (specific surface area 300 m 2 / g, manufactured by Fuji Chemical Industry Co., Ltd.) was used.
得られた錠剤について、前記と同様にして、硬度を測定し、成形性と崩壊性についても評価した。なお、崩壊時間の測定には、硬度が約１０ｋｐのものを６錠用いた。結果を表４に示す。 About the obtained tablet, hardness was measured in the same manner as described above, and moldability and disintegration were also evaluated. For the measurement of the disintegration time, 6 tablets having a hardness of about 10 kp were used. The results are shown in Table 4.
表４より、漢方エキスの種類が異なる場合にも、成形性よく、十分な硬度を有しながらも崩壊性に優れ、８７重量％以上の漢方エキスを含有する錠剤を製造することが可能であることが明らかである。 From Table 4, even when the types of Chinese herbal extracts are different, it is possible to produce tablets with good moldability, excellent hardness and excellent disintegration, and containing 87% by weight or more of Chinese herbal extracts. It is clear.
以下に処方例を挙げるが、本発明はこれらの実施例に限られるものではない。 Formulation examples are given below, but the present invention is not limited to these examples.
製造例１〜７
表５及び表６に記載の処方について、公知の技術を用いて錠剤を製造する。
Production Examples 1-7
About the prescription of Table 5 and Table 6, a tablet is manufactured using a well-known technique.
本発明の錠剤は、漢方エキスを８７重量％以上含有したものであっても、成形性及び崩壊性が改善された錠剤を簡便に製造することができる。また、本技術を用いることで、漢方エキスを高濃度含む錠剤を作ることができる、すなわち、添加剤の配合量を減らすことが可能となるため、１回あたりに服用する錠剤の量を減らしたり、１錠の大きさを小さくしたりすることが出来る。 Even if the tablet of the present invention contains 87% by weight or more of Kampo extract, a tablet with improved moldability and disintegration can be easily produced. In addition, by using this technology, it is possible to make tablets containing a high concentration of Kampo extract, that is, it is possible to reduce the amount of additives, so the amount of tablets to be taken at one time can be reduced. The size of one tablet can be reduced.
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|---|---|---|---|---|
| JP2015081238A (en) * | 2013-10-22 | 2015-04-27 | ポーラ化成工業株式会社 | Oral composition |
| CN111505196A (en) * | 2020-06-12 | 2020-08-07 | 上海中医药大学 | Quality control method for soup material reference in large-scale construction |
| JP7335730B2 (en) | 2019-06-26 | 2023-08-30 | 小林製薬株式会社 | Female hormone booster |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5711911A (en) * | 1980-06-25 | 1982-01-21 | Tsumura Juntendo Inc | Preparation of herb medicine tablet |
| JPH01258625A (en) * | 1988-04-08 | 1989-10-16 | Kanebo Ltd | Production of chinese medicine extract tablet |
| JP2012087055A (en) * | 2010-10-15 | 2012-05-10 | Sakamoto Kanpo Seiyaku:Kk | Pharmaceutical formulation containing crude drug |
| JP2014031333A (en) * | 2012-08-03 | 2014-02-20 | Rohto Pharmaceut Co Ltd | Kampo formulation |
-
2011
- 2011-04-20 JP JP2011093799A patent/JP5718714B2/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5711911A (en) * | 1980-06-25 | 1982-01-21 | Tsumura Juntendo Inc | Preparation of herb medicine tablet |
| JPH01258625A (en) * | 1988-04-08 | 1989-10-16 | Kanebo Ltd | Production of chinese medicine extract tablet |
| JP2012087055A (en) * | 2010-10-15 | 2012-05-10 | Sakamoto Kanpo Seiyaku:Kk | Pharmaceutical formulation containing crude drug |
| JP2014031333A (en) * | 2012-08-03 | 2014-02-20 | Rohto Pharmaceut Co Ltd | Kampo formulation |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015081238A (en) * | 2013-10-22 | 2015-04-27 | ポーラ化成工業株式会社 | Oral composition |
| JP7335730B2 (en) | 2019-06-26 | 2023-08-30 | 小林製薬株式会社 | Female hormone booster |
| CN111505196A (en) * | 2020-06-12 | 2020-08-07 | 上海中医药大学 | Quality control method for soup material reference in large-scale construction |
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|---|---|
| JP5718714B2 (en) | 2015-05-13 |
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