盐酸绿卡色林多晶型与稳定性研究  

Research on Polymorphic Form and Stability of Lorcaserin Hydrochloride

作　　者：刘松[1] 陈晓丽 吴淑阳 周梦青 皋海涛 顾佳丽[1] 张朝霞[1] 张国庆[1] 

机构地区：[1]浙江理工大学先进纺织材料与制备技术教育部重点实验室,杭州310018 [2]浙江普洛家园药业有限公司,浙江金华322118

出　　处：《浙江理工大学学报（自然科学版）》2016年第4期625-629,共5页Journal of Zhejiang Sci-Tech University(Natural Sciences)

基　　金：国家自然科学基金项目(51073142)

摘　　要：研究盐酸绿卡色林在不同条件下3种晶型间的相互转化关系及其机理，及其优势药物晶型Ⅲ的稳定性。运用粉末X射线衍射仪、差示扫描量热仪、热重分析仪和扫描电子显微镜对药物进行测试分析。盐酸绿卡色林存在2种亚稳态晶型（晶型Ⅰ和Ⅱ）和1种稳定晶型（晶型Ⅲ）；晶型Ⅱ在433．15K左右存在一转晶吸热峰；晶型Ⅰ、晶型Ⅱ和晶型Ⅲ的熔点皆为473．15K ，另外，晶型Ⅲ在368．22K处有一失结晶水的吸热峰，热焓值为64．57J／g ；优势药物晶型Ⅲ在高温高湿条件下晶型保持不变，稳定性好。在不同的实验条件下，盐酸绿卡色林的3种晶型间可以相互转化，通过热分析技术分析了药物的多晶型以及热稳定性，再结合其他分析技术可以有效和准确地表征药物的晶型、形貌和稳定性。T his paper aims to study mutual transformation relations of lorcaserin hydrochloride among three polymorphic forms under different conditions ,the mechanism and the stability of the dominant FormⅢ . The drugs had been analyzed by using powder X‐ray diffraction （PXRD ） , differential scanning calorimetry （DSC） ,thermal gravimetric analysis （TGA） ,and scanning electron microscopy （SEM ） .The lorcaserin hydrochloride has two metastable state forms （FormⅠand FormⅡ） and one stable form （FormⅢ） .There is a crystal transformation endothermic peak at 433 .15K for Form Ⅱ ;FormⅠ ,Form Ⅱ and FormⅢ show the same melt point ,i .e .473 .15K and there is endothermic peak at 368 .22K and the enthalpy value is 64 .57J/g ;FormⅢ can keep the form stabilization at high temperature and high humidity . Under different experimental conditions ,the three forms of lorcaserin hydrochloride can inter‐convert . The polymorphic form of drugs and their thermal stability are analyzed by using thermal analysis technology .By combining other analysis technologies ,crystal form ,morphology and stability of drugs can be effectively and accurately characterized .

关 键 词：盐酸绿卡色林 多晶型 热分析 X射线粉末衍射 电镜 

分 类 号：TQ460.1[化学工程—制药化工]