叶佳丽, 周新波, 吴素香, 孙梦莹, 顾建明, 胡秀荣. 曲格列汀琥珀酸盐晶体结构和晶型稳定性研究J. 药学学报, 2016,51(11): 1759-1764. doi: 10.16438/j.0513-4870.2016-0452
引用本文: 叶佳丽, 周新波, 吴素香, 孙梦莹, 顾建明, 胡秀荣. 曲格列汀琥珀酸盐晶体结构和晶型稳定性研究J. 药学学报, 2016,51(11): 1759-1764. doi: 10.16438/j.0513-4870.2016-0452
YE Jia-li, ZHOU Xin-bo, WU Su-xiang, SUN Meng-ying, GU Jian-ming, HU Xiu-rong. Crystal structure and crystal form stability of trelagliptin succinateJ. Acta Pharmaceutica Sinica, 2016,51(11): 1759-1764. doi: 10.16438/j.0513-4870.2016-0452
Citation: YE Jia-li, ZHOU Xin-bo, WU Su-xiang, SUN Meng-ying, GU Jian-ming, HU Xiu-rong. Crystal structure and crystal form stability of trelagliptin succinateJ. Acta Pharmaceutica Sinica, 2016,51(11): 1759-1764. doi: 10.16438/j.0513-4870.2016-0452

曲格列汀琥珀酸盐晶体结构和晶型稳定性研究

Crystal structure and crystal form stability of trelagliptin succinate

  • 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。

     

    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 by solvent, especially by polar solvent, namely trelagliptin hemi-succinate is more stable than trelagliptin succinate in solution.

     

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