黄芩素-羟丙基-γ-环糊精包合物制备工艺研究  

Preparation of inclusion complex of Baicalein-Hydroxypropyl-γ-Cyclodextrin

作　　者：周秋娜[1,2,3,4] 尉小慧[1,2,3,4] 王峥涛[1,2,3,4] 

机构地区：[1]上海中医药大学中药研究所中药标准化教育部重点实验室,上海201210 [2]上海中医药大学中药研究所中药新资源与质量标准综合评价国家中医药管理局重点研究室,上海201210 [3]上海中医药大学中药研究所上海市复方中药重点实验室,上海201210 [4]上海中药标准化研究中心,上海201203

出　　处：《上海中医药杂志》2013年第8期82-85,共4页Shanghai Journal of Traditional Chinese Medicine

基　　金：上海市教委预算内资助项目(2011JW21)

摘　　要：目的优化羟丙基-γ-环糊精(HP-γ-CD)包合黄芩素的工艺条件。方法采用冷冻干燥法,以包合物的得率、包封率和载药率为考察指标,通过L9(3)4正交设计优选黄芩素(Ba)与HP-γ-CD摩尔比、包合温度、包合时间、包合溶剂比(水∶无水乙醇),综合评价确定最佳制备工艺;采用X射线衍射分析和差示扫描量热分析验证包合物。结果最优包合条件:Ba与HP-γ-CD摩尔比为1∶3,温度45℃,包合时间4 h,包合溶剂比(水∶无水乙醇)2∶3;采用最优包合条件制备的Ba-HP-γ-CD包合物得率为93.97%,包封率为95.96%,载药率为5.20%,其粉末经鉴定已形成包合物;Ba-HP-γ-CD包合物能够显著提高Ba的溶解度。结论优选的包合工艺合理可行,为黄芩素制备成各种剂型奠定了良好基础。Objective To select the optimum prepared process of inclusion complex of baicalein with HP-γ-CD. Methods The inclusion yield, encapsulation efficiency and drug loading were investigated by freeze-drying method. The molar ratio of baicalein and HP-γ-CD, reaction temperature, reaction time and solvent ratio （ water ： ethanol） were designed by L9 （ 3 ） 4 orthogonal experiment. Analyzed and verified the inclusion complex by X-ray diffraction and differential scanning calorimetry. Results The best ratio of baiealein and HP-γ-CD was 1 ： 3, the reaction temperature was 45 ℃, the reaction time was 4 h and the solvent ratio （ water： ethanol） was 2 ： 3. The best inclusion yield was 93.97% , the encapsulation efficiency was 95.96% and drug loading was 5.20%. The inclusion in the powder was formed ; the inclusion complex of Ba-HP-γ-CD can improve the solubility of Ba. Conclusion The optimum preparation conditions were reasonable and feasible, which provided a good foundation for a variety of dosage forms.

关 键 词：黄芩素 羟丙基-γ-环糊精 包合物 工艺条件 

分 类 号：TQ461[化学工程—制药化工]