反溶剂重结晶法制备多晶型比卡鲁胺

季华;乐园;沈志刚;陈建峰*

北京化工大学学报(自然科学版) ›› 2008, Vol. 35 ›› Issue (4) : 14-17.

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北京化工大学学报(自然科学版) ›› 2008, Vol. 35 ›› Issue (4) : 14-17.
化学与化学工程

反溶剂重结晶法制备多晶型比卡鲁胺

  • 季华;乐园;沈志刚;陈建峰*
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Preparation of bicalutamide polymorphs by mixed solvents induced precipitation

  • JI Hua;LE Yuan;SHEN ZhiGang;CHEN JianFeng*
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摘要

采用反溶剂重结晶法制备多晶型比卡鲁胺,通过改变重结晶过程中所使用的溶剂,对比单一溶剂和共溶剂对所制得晶体的晶型和颗粒形貌差别,探索最优化的共溶剂类型和体积比参数,以达到将比卡鲁胺原料药进行晶型纯化的目的。在反溶剂重结晶过程中采用共溶剂制备比卡鲁胺晶体发现:共溶剂(二甲基亚砜+乙醇)以及(丙酮+乙醇)可制备比卡鲁胺晶型I,并通过调节共溶剂中乙醇的用量可得到粒度均一,分散性好的I型比卡鲁胺。

Abstract

The polymorphism of bicalutamide and the factors affecting its crystal formation have been studied. The standard forms of bicalutamide were prepared by evaporat ion and meltingcooling processes. Two crystalline forms of bicalutamide were o btained by antisolvent precipitation and their structures were determined by c omparing their X-ray powder diffraction patterns with those of the standard for ms. A range of mixed solvents were screened in order to determine the optimum sy stem. It was shown that changing the volume ratio of two solvents can induce cry stallization of different polymorphs. 

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季华;乐园;沈志刚;陈建峰*. 反溶剂重结晶法制备多晶型比卡鲁胺[J]. 北京化工大学学报(自然科学版), 2008, 35(4): 14-17
JI Hua;LE Yuan;SHEN ZhiGang;CHEN JianFeng*. Preparation of bicalutamide polymorphs by mixed solvents induced precipitation[J]. Journal of Beijing University of Chemical Technology, 2008, 35(4): 14-17

参考文献

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