依帕司他共晶的制备、表征及性质研究

Preparation, Characterization and Property Research of Epalrestat Co-crystal

摘要:
目的制备依帕司他药物共晶，提高依帕司他水溶性。
方法以依帕司他为原料，4,4’-联吡啶为共晶前驱体，采用溶剂挥发法，制备得到依帕司他共晶。应用¹H-NMR分析、X射线单晶衍射法、粉末X射线衍射法、差示扫描量热法、热重法等对制备得到的共晶进行表征。对共晶溶解性及引湿性进行了研究。
结果相较依帕司他原料药，共晶在水中的溶解度提高近40倍。
结论依帕司他共晶水溶性提升显著。

Abstract:
OBJECTIVE To prepare the eutectic of epalrestat and improve its water solubility.
METHODS Using epalrestat as starting material and 4,4'-bipyridine as eutectic precursor, the epalrestat co-crystal was obtained by solvent volatilization. The structure of prepared co-crystal was characterized by ¹H-NMR, X-ray single-crystal diffraction, power X-ray diffraction, differential scanning calorimetry and thermal gravimetric analysis respectively. The solubility and hygroscopicity of the co-crystal were also studied.
RESULTS The solubility of epalrestat co-crystal in water was increased to nearly 40 times as compared with epalrestat raw materials.
CONCLUSION The solubility of epalrestat co-crystal increased significantly.