Novel Polymorph of Atorvastatin Calcium and Use Thereof for the Preparation of Amorphous Atorvastatin Calcium
申请人:Dixit Girish
公开号:US20100260851A1
公开(公告)日:2010-10-14
The present invention provides a novel polymorphic form of atorvastatin calcium, designated as form Al, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention further provides a process for the preparation of highly pure amorphous atorvastatin calcium using the novel atorvastatin calcium form Al. The present invention also relates to novel amorphous form of atorvastatin tert-butyl ester, chemically known as [R-(R*,R*)]-2-(4-fluorophenyl)-[β],[δ]-dihydroxy -5-(1-methylethyl)-3-phenyl-4-(phenylcarbamoyl-1H-pyrrole-1-heptanoicacid tert-butyl ester, process for the preparation, and its application for preparing highly pure atorvastatin and its pharmaceutically acceptable salts thereof. The present invention also relates to use of the novel amorphous atorvastatin tert-butyl ester and novel atorvastatin calcium form al for preparing amorphous atorvastatin calcium.
本发明提供了阿托伐他汀钙的一种新的多晶形式,称为Al型,制备方法、制药组合物和治疗方法。本发明还提供了一种使用新的阿托伐他汀钙Al型制备高纯非晶态阿托伐他汀钙的方法。本发明还涉及阿托伐他汀叔丁基酯的新非晶态形式,化学名称为[R-(R*,R*)]-2-(4-氟苯基)-[β],[δ]-二羟基-5-(1-甲基乙基)-3-苯基-4-(苯基羰氨基)-1H-吡咯烷-1-庚酸叔丁基酯,制备方法及其应用于制备高纯阿托伐他汀及其药用盐。本发明还涉及使用新的非晶态阿托伐他汀叔丁基酯和新的阿托伐他汀钙Al型制备非晶态阿托伐他汀钙。