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    • 1. 发明授权
    • Aerosol compositions
    • 气溶胶成分
    • US06524556B2
    • 2003-02-25
    • US09994702
    • 2001-11-28
    • Saburo MurataFumio ShiomojoYuji TokunagaTakehisa Hata
    • Saburo MurataFumio ShiomojoYuji TokunagaTakehisa Hata
    • A61K912
    • A61K9/008A61K9/12A61K31/4433
    • The use of a medium-chain fatty acid triglyceride as the dispersant in the preparation of a medicinal aerosol composition comprising tricyclic compound (I) dispersed in a liquefied hydrofluoroalkane propellant is described. When a liquefied hydrofluoroalkane is added to a kneaded premix of the tricyclic compound (I) and a medium-chain fatty acid triglyceride, the active ingredient is evenly dispersed in the liquefied hydrofluoroalkane. Therefore, by distributing a dispenser first with the kneaded premix and, then, with a liquefied hydrofluoroalkane under cooling or elevated pressure, there can be provided a medicinal aerosol composition an improved uniformity of content of the active ingredient.
    • 描述了使用中链脂肪酸甘油三酸酯作为分散剂来制备包含分散在液化氢氟烷烃推进剂中的三环化合物(I)的药用气溶胶组合物。当将液化氢氟烷烃加入到三环化合物的捏合预混物中时 (I)和中链脂肪酸甘油三酸酯,活性成分均匀分散在液化氢氟烷烃中。因此,首先通过在搅拌的预混物中分配分配器,然后在冷却或升高的压力下用液化氢氟烷烃分配分配器, 提供药物气溶胶组合物,改善活性成分含量的均匀性。
    • 5. 发明授权
    • Sustained release medicinal preparation
    • 持续释放药用制剂
    • US5601844A
    • 1997-02-11
    • US424498
    • 1995-05-18
    • Akira KagayamaSumihisa KimuraSaburo MurataSachiyo TanimotoTakehisa Hata
    • Akira KagayamaSumihisa KimuraSaburo MurataSachiyo TanimotoTakehisa Hata
    • A61K9/16A61K9/52A61K31/436C07D498/18A61K9/48A61K9/50A61K31/44
    • C07D498/18A61K31/436A61K9/1647
    • A sustained release medicinal preparation is produced by enclosing a macrocyclic compound represented by 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl)-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone or 17-ethyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone, into the fine particles generally called microspheres which arc made of biodegradable polymer. This preparation, when, for example, given by injection, appreciably improves the transferance of said macrocyclic compound into the blood. Further, this is also used as an agent suitable for topical administration.
    • PCT No.PCT / JP93 / 01672 Sec。 371日期1995年5月18日 102(e)日期1995年5月18日PCT提交1993年11月11日PCT公布。 公开号WO94 / 10981 日期1994年5月26日缓释药物制剂是通过将由17-烯丙基-1,14-二羟基-12- [2-(4-羟基-3-甲氧基环己基)-1-甲基乙烯基)-23表示的大环化合物, 25-二甲氧基-13,19,21,27-四甲基-11,28-二氧杂-4-氮杂三环[22.3.1.04,9]二十八-18-烯-2,3,10,16-四酮或17-乙基 - 1,14-二羟基-12- [2-(4-羟基-3-甲氧基环己基)-1-甲基乙烯基] -23,25-二甲氧基-13,19,21,27-四甲基-11,28-二氧杂-4- 氮杂三环[22.3.1.04,9]二十八烷-18-烯-2,3,10,16-四酮,形成由可生物降解的聚合物制成的通常称为微球的细颗粒。 当通过注射给予时,该制剂明显地改善了所述大环化合物向血液中的转移。 此外,这也用作适合局部给药的药剂。
    • 6. 发明授权
    • Aerosol compositions
    • 气溶胶成分
    • US06361760B1
    • 2002-03-26
    • US09029863
    • 1998-04-22
    • Saburo MurataFumio ShiomojoYuji TokunagaTakehisa Hata
    • Saburo MurataFumio ShiomojoYuji TokunagaTakehisa Hata
    • A61K912
    • A61K9/008A61K9/12A61K31/4433
    • The use of a medium-chain fatty acid triglyceride as the dispersant in the preparation of a medicinal aerosol composition comprising tricyclic compound (I) dispersed in a liquefied hydrofluoroalkane propellant is described. When a liquefied hydrofluoroalkane is added to a kneaded premix of the tricyclic compound (I) and a medium-chain fatty acid triglyceride, the active ingredient is evenly dispersed in the liquefied hydrofluoroalkane. Therefore, by distributing a dispenser first with the kneaded premix and, then, with a liquefied hydrofluoroalkane under cooling or elevated pressure, there can be provided a medicinal aerosol composition having an improved uniformity of content of the active ingredient.
    • 描述了使用中链脂肪酸甘油三酸酯作为分散剂来制备包含分散在液化氢氟烷烃推进剂中的三环化合物(I)的药用气溶胶组合物。 当将液化氢氟烷烃加入到三环化合物(I)和中链脂肪酸甘油三酯的捏合预混物中时,活性成分均匀分散在液化氢氟烷烃中。 因此,首先通过在搅拌的预混物中分配分配器,然后在冷却或升高的压力下用液化氢氟烷烃分配分配器,可以提供具有改善的活性成分含量均匀性的药用气溶胶组合物。