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

Crystal structure and crystal form stability of trelagliptin succinate

  • 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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