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1. 发明授权

US5980947A Process for producing drug-containing microspheres by oil-in-water evaporation process 失效
标题翻译：通过水包油蒸发法生产含药微球的方法
公开(公告)号：US5980947A
公开(公告)日：1999-11-09
申请号：US352188
申请日：1994-12-01
申请人： Ichiro Yamakawa , Ryoichi Machida , Sumio Watanabe
发明人： Ichiro Yamakawa , Ryoichi Machida , Sumio Watanabe
IPC分类号： A61K9/16 , A61K9/50 , B01J13/12 , A61K9/14
CPC分类号： A61K9/1694 , A61K9/1617 , A61K9/1647
摘要： Formation of a drug into microspheres by an oil-on-water solvent evaporation process in which a mixed solvent of at least one water-insoluble solvent and at least one water-miscible solvent is used as a solvent of an oil phase. A fatty acid or a salt thereof or at least one glycerin fatty acid ester and/or at least one propylene glycol fatty acid ester are added to the mixed solvent. The oil phase may also comprise the mixed solvent; a fatty acid or a salt thereof; and at least one glycerin fatty acid ester and/or at least one propylene glycol fatty acid ester. This oil phase is mixed and emulsified with an aqueous phase to form an oil-in-water emulsion. The emulsion with a drug contained therein is then subjected to an oil-in water solvent evaporation to produce the microspheres. The resulting drug-containing microspheres contain the drug at a high concentration and slowly release from the initial stage after administration.
摘要翻译：通过油包水溶剂蒸发方法将药物形成为微球，其中使用至少一种水不溶性溶剂和至少一种与水相混溶的溶剂的混合溶剂作为油相的溶剂。向混合溶剂中加入脂肪酸或其盐或至少一种甘油脂肪酸酯和/或至少一种丙二醇脂肪酸酯。油相也可以包含混合溶剂; 脂肪酸或其盐; 和至少一种甘油脂肪酸酯和/或至少一种丙二醇脂肪酸酯。将该油相与水相混合并乳化以形成水包油乳液。然后将其中含有药物的乳液进行油包水溶剂蒸发以产生微球体。所得含药微球含有高浓度的药物，并在给药后从初始阶段缓慢释放。

2. 发明授权

US4397951A Elastase-containing composition permitting elastase to be absorbed in increased amount 失效
标题翻译：含弹性蛋白酶的组合物允许弹性蛋白酶以增加的量被吸收
公开(公告)号：US4397951A
公开(公告)日：1983-08-09
申请号：US343333
申请日：1982-01-27
申请人： Kazuo Taki , Ryoichi Machida , Kouichi Katayama
发明人： Kazuo Taki , Ryoichi Machida , Kouichi Katayama
IPC分类号： A61K38/46 , A61K38/00 , A61K38/43 , A61K47/26 , A61P3/06 , A61P9/10 , C12N9/66 , C12N9/96 , A61K37/48
CPC分类号： C12N9/6448 , A61K47/26 , A61K38/00
摘要： An elastase-containing composition containing 0.5 to 50 parts by weight of sucrose fatty acid ester per part by weight of pure elastase, which composition permits elastase, useful as medicine for arterioscloerosis and hyperlipemia, to be absorbed in increased amount through intenstine.
摘要翻译：含有0.5〜50重量份蔗糖脂肪酸酯的重量份纯弹性蛋白酶组合物，该组合物允许弹性蛋白酶用作动脉硬化和高脂血症的药物，以通过内脏吸收增加的量。

3. 发明授权

US5254545A Injectable preparations containing cephalosporin medicament 失效
标题翻译：含有头孢菌素药物的注射剂
公开(公告)号：US5254545A
公开(公告)日：1993-10-19
申请号：US589922
申请日：1990-09-28
申请人： Yasuo Ishibashi , Isamu Hasegawa , Masanori Kayano , Ryoichi Machida , Masahiro Kawahara , Sumio Watanabe
发明人： Yasuo Ishibashi , Isamu Hasegawa , Masanori Kayano , Ryoichi Machida , Masahiro Kawahara , Sumio Watanabe
IPC分类号： A61K9/08 , A61K9/00 , A61K31/545 , A61K31/546 , A61K47/00 , A61K47/02 , A61K47/12 , A61K47/18 , A61K47/26
CPC分类号： A61K9/0019 , A61K31/545
摘要： A preparation containing a cephalosporin medicament is disclosed. The preparation comprises a cephalosporin derivative represented by the following formula: ##STR1## namely, 7.beta.-{2-(5-amino-1,2,4-thiadiazol-3-yl)-(Z)-2-fluoromethoxyiminoacetamido}-3-{(E)-3-(carbamoylmethylethylmethylammonio) -1-propen-1-yl}-3-cephem-4-carboxylate or a pharmaceutically acceptable salt thereof salt, lactose, citric acid or a sodium salt thereof, and arginine or a hydrochloride thereof; or the cephalosporin derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof, lactose, citric acid or a sodium salt thereof, and sodium chloride.

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