喷雾干燥法制备斑蝥素壳聚糖生物黏附微球的处方工艺研究  

Formula and Preparation of Cantharidin Chitosan Bioadhesive Microspheres by Spray Drying

作　　者：吕琳[1] 何晓明[2] 曹德英[2] 杜青[2] 党云洁[2] 

机构地区：[1]天津泰达国际心血管病医院药剂科,天津300270 [2]河北医科大学药学院

出　　处：《中国药师》2017年第8期1344-1348,共5页China Pharmacist

基　　金：国家科技重大专项(编号:2014ZX09507001);河北省自然科学基金项目(编号:H2016206584);河北医科大学2013科研骨干人才培育计划项目

摘　　要：目的:优选斑蝥素壳聚糖生物黏附微球的最佳处方工艺。方法:采用喷雾干燥法制备微球,运用单因素试验考察不同壳聚糖分子量对微球胃黏膜黏附率的影响,不同药载比、壳聚糖醋酸溶液浓度和蠕动泵速度对斑蝥素包封率的影响。采用效应面法,以斑蝥素的包封率为考察指标,进一步优化药载比、壳聚糖醋酸溶液浓度和蠕动泵流速3个因素。结果:斑蝥素壳聚糖生物黏附微球的最佳处方工艺为:斑蝥素和壳聚糖的重量比为19.83%,壳聚糖醋酸溶液浓度为0.77%,蠕动泵流速为9.225 ml·min^(-1)。以最佳处方工艺制得的斑蝥素壳聚糖生物黏附微球包封率为90.14%。结论:采用喷雾干燥法制备微球,具有工艺稳定、可重复等优点,制备的斑蝥素壳聚糖生物黏附微球具备较好的包封率和生物黏附性能。Objective： To optimize the formula and preparation technology of cantharidin chitosan bioadhesive microspheres. Methoils ： The microspheres were prepared by a spray drying method. A single-factor experiment was used to study the effect of chitosan with different molecular weight on the gastric mucosa adhesion rate were also studied, and the effects of different drug loading ratio, concen- tration of chitosan acetic acid solution and speed of peristaltic pump on the loading rate were also studied. The cantharidin entrapment efficiency as the studying index, a response surface method was used to further optimize the formula. Results： The best formula and preparation process of cantharidin chitosan bioadhesive mierospheres were as follows： the concentration ratio of antharidin to chitosan was 19.83%, the concentration of chitosan acetic acid solution was 0.77%, and the peristaltic pump flow rate was 9. 225 ml min -1. With the best formula, the entrapment efficiency of eantharidin chitosan bioadhesive microspheres was 90.14%. Conclusion： The mi- crosphere preparation by the spray drying method is stable and repeatable. Cantharidin chitosan bioadhesive microspheres have high en- trapment efficiency and promising biological adhesion.

关 键 词：斑蝥素 壳聚糖微球 生物黏附 效应面法 

分 类 号：R944.9[医药卫生—药剂学]