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    • 1. 发明申请
    • PROCESSES FOR PREPARATION OF AMORPHOUS CEFEPIME ACID ADDITION SALTS
    • 制备非晶形磷酸添加剂的方法
    • WO2006109324A3
    • 2007-04-05
    • PCT/IN2006000125
    • 2006-04-12
    • LUPIN LTDTYAGI OM DUTTMEHARE KISHOR GULABRAODESHMUKH SANJAY
    • TYAGI OM DUTTMEHARE KISHOR GULABRAODESHMUKH SANJAY
    • C07D501/00A61K31/545
    • C07D501/00C07D501/56
    • The present invention provides processes for the preparation amorphous form of Cefepime acid addition salt in high purity which exhibits very good thermal stability on storage. The processes are simple and cost-effective. The selective solvent precipitation method comprises of: (a) dissolving cefepime acid addition salt or solvates thereof in a polar solvent, (b) addition of less polar solvent to the solution obtained in step (a) to precipitate out cefepime acid addition salt followed by isolation of solid by filtration and drying or alternatively, (a) dissolving cefepime acid addition salt or solvates thereof in a polar solvent, (b) addition of the solution obtained in step (a) to less polar solvent to precipitate out cefepime acid addition salt followed by isolation of solid by filtration and drying. The further method involves spray drying of solution of cefepime acid addition salt or solvates thereof prepared in a polar solvent.
    • 本发明提供了高纯度制备非晶态Cefepime酸加成盐的方法,其在储存时表现出非常好的热稳定性。 流程简单,成本效益高。 选择性溶剂沉淀法包括:(a)将头孢吡肟酸加成盐或溶剂合物溶解在极性溶剂中,(b)向步骤(a)获得的溶液中加入极性极少的溶剂,沉淀出头孢吡肟酸加成盐, 通过过滤和干燥分离固体,或者(a)将头孢吡肟酸加成盐或溶剂合物溶解在极性溶剂中,(b)将步骤(a)中获得的溶液加入到极性较小的溶剂中以沉淀出头孢吡肟酸加成盐 然后通过过滤和干燥分离固体。 另外的方法包括喷雾干燥在极性溶剂中制备的头孢吡肟酸加成盐或溶剂合物溶液。