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11.发明公开AQUEOUS DISPERSION COMPRISING STABLE NANOPARTICLES OF A WATER-INSOLUBLE THIAZOLE DERIVATIVE AND EXCIPIENTS LIKE MIDDLE CHAIN TRIGLYCERIDES 审中-公开水分散体的稳定的纳米颗粒水噻唑和代理人中链甘油三酯CONTAIN
公开(公告)号：EP1592403A1
公开(公告)日：2005-11-09
申请号：EP04707262.4
申请日：2004-02-02
申请人： AstraZeneca AB
发明人： LINDFORS, Lennart
IPC分类号： A61K9/16 , A61K9/10 , C07D277/56 , C07D417/12 , C07D417/04
CPC分类号： C07D417/04 , A61K9/145 , C07D277/56
摘要： A process for the preparation of a stable dispersion of solid particles, in an aqueous medium comprising combining (a) a first solution comprising a substantially water-insoluble substance which is a thiazole compound of Formula I, a water-miscible organic solvent and an inhibitor with (b) an aqueous phase comprising water and optionally a stabiliser, thereby precipitating solid particles comprising the inhibitor and the substantially water-insoluble substance; and optionally removing the water-miscible organic solvent; wherein the inhibitor is a non-polymeric hydrophobic organic compound as defined in the description. Also claimed are stable dispersions obtainable by the process, solid particles obtainable by the process and use of such particles. The process provides a dispersion of solid particles in an aqueous medium, which particles exhibit reduced or substantially no particle growth mediated by Ostwald ripening. The process is particlularly suitable for the preparation of small (sub-micron) aqueous dispersions of a substantially water-insoluble pharmacologically active substance.
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公开(公告)号：EP1015022B1
公开(公告)日：2004-12-15
申请号：EP97926326.6
申请日：1997-05-28
申请人： AstraZeneca AB
CPC分类号： A61K9/4858 , A61K9/1274 , A61K38/55 , Y10S514/946
摘要： A new pharmaceutical formulation comprising the thrombin inhibitor HOOC-CH2-(R)-Cgl-Aze-Pab in combination with medium chain glycerides, a process for the preparation of such a pharmaceutical formulation, the use of such formulation in the treatment of thromboembolism as well as a method of treating a patient in need of such a treatment by using said formulation.
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公开(公告)号：EP1015022A1
公开(公告)日：2000-07-05
申请号：EP97926326.6
申请日：1997-05-28
申请人： AstraZeneca AB
CPC分类号： A61K9/4858 , A61K9/1274 , A61K38/55 , Y10S514/946
摘要： A new pharmaceutical formulation comprising the thrombin inhibitor HOOC-CH2-(R)-Cgl-Aze-Pab in combination with medium chain glycerides, a process for the preparation of such a pharmaceutical formulation, the use of such formulation in the treatment of thromboembolism as well as a method of treating a patient in need of such a treatment by using said formulation.
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