曲格列汀琥珀酸盐晶体结构和晶型稳定性研究Crystal-药学学报.PDFVIP

药学学报 Acta Pharmaceutica Sinica 20 16, 51 ( 11): 1759 1764 ·1759 · 格列汀琥珀酸盐晶体结构和晶型稳定性研究 1, 2 1 1 1 2 2* 叶佳丽 , 周新波 , 吴素香 , 孙梦莹 , 顾建明 , 胡秀荣 (1. 浙江中医药大学药学院, 浙江 杭州 3 10053; 2. 浙江大学化学系, 浙江 杭州 310028) 摘要: 采用重结晶方法和混悬方法研究曲格列汀琥珀酸盐在极性溶剂 (水和95% 乙醇) 中的转晶情况。采用 X 射线单晶衍射、X 射线多晶衍射和热分析等多种分析方法, 对曲格列汀琥珀酸盐转晶前后的结晶形式进行了结 构表征。结果表明, 曲格列汀琥珀酸盐在溶剂介导下特别是极性溶剂介导下容易转化成曲格列汀半琥珀酸盐。 关键词: 曲格列汀半琥珀酸盐; 曲格列汀琥珀酸盐; 晶体结构; 稳定性; 转晶 中图分类号: R9 17 文献标识码: A 文章编号: 0513-4870 (20 16) 11-1759-06 Crystal structure and crystal form stability of trelagliptin succinate 1, 2 1 1 1 2 2* YE Jia-li , ZHOU Xin-bo , WU Su-xiang , SUN Meng-ying , GU Jian-ming , HU Xiu-rong (1. College of Pharmaceutical Science, Zhej iang Chinese Medical University, Hangzhou 310053, China; 2. Dep artment of Chemistry, Zheji ang University, Hangzhou 310028, China ) Abstract : In order to investigate trelagliptin succinate ’s stability in solution, recrystallization and suspension methods in polar solvent (mainly in water and 95% alcohol) were used to study the crystal form transformation of trelagliptin succinate. Single crystal X-ray diffraction, powder X-ray diffraction and thermalgravimetric analysis, and differential scanning calorimetry were used to characterize the structure of the solid state form before and after transformation. The results showed that trelagliptin succinate can easily convert to trelagliptin hemi-succinate mediated