胆酸-羟丙基-β-环糊精包合物的制备工艺及相溶解度研究  

Preparation and phase solubility of inclusion complex of cholic acid-hydroxypropyl-β-cyclodextrin

作　　者：苏柘僮[1] 杨明[1] 吴品江[1] 许润春[1] 高亚男[1] 欧水平[1] 

机构地区：[1]成都中医药大学,四川成都610075

出　　处：《中成药》2009年第3期380-382,共3页Chinese Traditional Patent Medicine

摘　　要：目的:考察胆酸-羟丙基-β-环糊精包合物的最佳制备工艺以及溶解性。方法:采用正交设计试验,以包合率为评价标准,对药物与羟丙基-β-环糊精的投料比例、包合温度、搅拌时间、药液滴加速度进行了考察,以确定胆酸-羟丙基-β-环糊精包合物的最佳制备工艺;采用高效液相色谱法测定胆酸-羟丙基-β-环糊精包合物的包合率;采用相溶解度试验对增溶效应进行了评价。结果:确定了胆酸-羟丙基-β-环糊精包合物最佳制备工艺,即药物投料比例为1:3,温度为60℃,搅拌时间60 min,药液滴加速度1.6 mL/min;相溶解度曲线为AL型,包合常数K=564.30 L/mol,增溶11.81倍。结论:以最佳制备工艺制备包合物,包合率达到97.1%,工艺稳定,合理可行;胆酸适宜用HP-β-CD包合,增溶效应明显。AIM： To optimize the preparation of cholic acid-hydroxypropy-β-cyclodextrin inclusion complex, and its phase solubility analysis. METHODS： Orthogonal test, including molar ratio, inclusion temperature, mixing time and liquid dropping rate of cholic acid-HP-β-CD, was adopted to screen the optimal preparation, based on the inclusion efficiency by HPLC method. The solubilization effect was evaluated by using phase solubility. RESULTS ： The optimal preparation consisted of the molar ratio of cholic acid-HP-β-CD was 1 ： 3, 60℃ inclusion temperature, 60 min mixing time, 1.6 mL/min liquid dropping rate ; AL type of phase solubility curve, K = 564.30 L/mol,and 11.81 times solubilization. CONCLUSION： The optimal preparation is stable, reasonable and practicable with the encapsulation efficiency of 97.1%. Inclusing cholic acid with HP-β-CD is feasible, and the solubilization effect is significant.

关 键 词：胆酸-羟丙基-β-环糊精包合物 HPLC 制备工艺 相溶解度 

分 类 号：R944[医药卫生—药剂学]