匹莫范色林晶型C的结晶工艺研究  

Crystallization Process Study of Crystal Form C of Pimavanserin

作　　者：郝晓锋[1] 侯权 曾霞 严峻[1] 柯潇[1] HAO Xiaofeng;HOU Quan;ZENG Xia;YAN Jun;KE Xiao(Chengdu Kanghong Pharmaceutical Group Co.,Ltd.,Chengdu 610036)

机构地区：[1]成都康弘药业集团股份有限公司,四川成都610036

出　　处：《中国医药工业杂志》2022年第12期1788-1795,共8页Chinese Journal of Pharmaceuticals

摘　　要：开发了一种无需添加晶种的匹莫范色林晶型C放大制备方法。通过溶解度的考察、结晶方式的筛选,结合生产设备的选型,研究了工业结晶条件;利用在线-离线监控相结合的方式探索了其结晶过程及原理;并采用X射线粉末衍射(PXRD)法、差示扫描量热(DSC)法、热重分析(TGA)法对成品晶型质量进行了研究与控制。结果表明,在丁酮中通过悬浮转晶的方法制备晶型C的工艺操作简单,晶型质量稳定且可控,适合工业化生产。A crystallization process of crystal form C of pimavanserin is developed without adding crystal seeds.The industrial crystallization conditions were studied through the investigation of solubility,the selection of crystallization methods and production equipment.The crystallization process and mechanism were explored by combination of in-line and off-line monitoring.X-Ray powder diffraction(PXRD),differential scanning calorimetry(DSC)and thermogravimetric analysis(TGA)were used to investigate and control the crystal quality of the final product.The results showed that the process(suspension crystallization in butanone)was suitable for industrial production with a simple operation procedure,and the obtained crystal form C was stable and controllable.

关 键 词：匹莫范色林 晶型C 结晶工艺 晶型质量 

分 类 号：O782.1[理学—晶体学] R971.4[医药卫生—药品]