目的 研究新型钠–葡萄糖协同转运蛋白2抑制剂tianagliflozin与L-脯氨酸的共结晶，制备一种稳定的可供药用的共结晶。方法 在乙醇中共结晶制备tianagliflozin与L-脯氨酸的共结晶，并采用核磁共振氢谱、粉末X衍射、热重/差热分析及红外光谱测定共结晶物的特征。初步考察了共结晶对光、温度和湿度的稳定性。结果 制备了tianagliflozin与L-脯氨酸稳定的1∶1共结晶，初步稳定性考察表明该共结晶对光照、高温和低中湿稳定，高湿条件下发生分解。结论 tianagliflozin与L-脯氨酸的共结晶在稳定性和制备重现性方面较好，为其成药性研究提供了参考。

Objective To investigate the cocrystallization of tianagliflozin, a new inhibitor on sodium-dependent glucose co-transporter 2, and L-proline and to prepare a stable modality of medicinal cocrystallization. Methods The cocrystallization of tianagliflozin and L-proline was prepared from ethanol cocrystallization, and characterized by 1H-NMR, PXRD, TG/DTA, and IR methods. Preliminary stability tests of cocrystallization to light, temperature, and moisture were performed. Results The cocrystallization of tianagliflozin and L-proline in a molecular ratio of 1∶1 was prepared. The stability test demonstrated that the cocrystallization was stable to light, high temperature, and low to medium moisture, but unstable to high moisture, which could decompose the cocrystallization to its individual components. Conclusion The cocrystallization of tianagliflozin and L-proline is stable and reproducible, which provide reference for its druggablitiy.

国家自然科学基金资助项目(21302141)；天津市科技计划项目(10ZCKFSH01300)