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    • 6. 发明申请
    • NOVEL POLYMORPHS OF FOSAMPRENAVIR CALCIUM
    • FOSAMPRENAVIR钙的新型聚合物
    • US20150025040A1
    • 2015-01-22
    • US14125386
    • 2012-05-21
    • HETERO RESEARCH FOUNDATION
    • Bandi Parthasaradhi ReddyKura Rathnakar ReddyDasari Muralidhara ReddyKesireddy Subash Chander ReddyBandi Vamsi Krishna
    • C07F9/655
    • C07F9/65515C07B2200/13
    • Crystalline Forms of fosamprenavir calcium are disclosed, processes for its preparation and pharmaceutical compositions therefrom. The process for the preparation of fosamprenavir calcium crystalline Form H1, comprises: a) suspending fosamprenavir calcium in a nitrile solvent; b) heating the suspension obtained in step (a) at reflux; c) optionally adding a solvent to the reaction mass obtained in step (b); d) cooling the reaction mass at below 35 degrees Centigrade; and e) isolating fosamprenavir calcium crystalline Form H1. Another process for the preparation of substantially pure amorphous fosamprenavir calcium, which comprises: a) dissolving fosamprenavir calcium in an ester solvent; b) a portion of solvent from the solution obtained in step (a) until at least separation of fosamprenavir calcium as solid occurs; and c) isolating substantially pure amorphous fosamprenavir calcium. The pharmaceutical composition may comprse substantially pure amorphous fosamprenavir calcium and pharmaceutically acceptable excipients.
    • 披露了福沙那韦钙的结晶形式,其制备方法及其药物组合物。 制备福沙那韦钙晶体形式H1的方法包括:a)将福沙那韦钙悬浮在腈溶剂中; b)将在步骤(a)中获得的悬浮液加热回流; c)任选地向步骤(b)中获得的反应物料中加入溶剂; d)将反应物料冷却至35摄氏度以下; 和e)分离福桑那韦钙晶体形式H1。 制备基本上纯的无定形福桑那韦钙的另一种方法,其包括:a)将福沙那韦钙溶于酯溶剂中; b)将来自步骤(a)中获得的溶液的一部分溶剂直至至少分离作为固体的福沙那韦钙; 和c)分离基本上纯的无定形福桑那韦。 药物组合物可以包括基本上纯的无定形福桑那韦钙和药学上可接受的赋形剂。