鼻用人参皂苷Rg3壳聚糖微球的制备  

Preparation of Ginsenoside Rg3-loaded chitosan microspheres for intranasal administration

作　　者：唐文燕[1] 高静[1] 丁雪鹰[1] 高申[1] 

机构地区：[1]第二军医大学药学院药剂学教研室,上海200433

出　　处：《第二军医大学学报》2008年第7期817-821,共5页Academic Journal of Second Military Medical University

基　　金：全军医药卫生科研基金(2006172006)~~

摘　　要：目的:以壳聚糖为载体材料,人参皂苷Rg3为模型药物,制备鼻腔给药微球。方法:采用复乳化化学交联技术制备人参皂苷Rg3鼻用微球。利用Statistic软件进行多元线性回归和二项式拟合,求得方程。以载药量,包封率及40～60μm微球所占比例为指标,用星点设计-效应面优化法选取较佳工艺条件,扫描电镜观察微球表面形态。结果:据效应面优选的较佳处方范围为:投药比为0.4～0.5;有机相与水相之比为0.4～0.6;初乳与油相比为0.13～0.17。以此优选处方制备的三批微球形态良好,球形圆整,平均粒径为(44.99±12.59)μm,载药量为(10.25±0.08)%,包封率为(30.61±1.46)%。结论:所优化的制备工艺稳定,适于鼻用人参皂苷Rg3壳聚糖微球的制备。Objective：To prepare ginsenoside Rg3-loaded chitosan microspheres for intranasal administration. Methods： The chitosan microspheres were prepared by the O/W/O combined with multiple emulsification chemical crosslink technique. Quadratic polynomial equation and linear regression equation were fitted by the statistic software, and the resulting equations were used to produce response surface graphs. The best experiment conditions were screened by central composite design （CCD） using drug load,encapsulation efficiency, and the proportions of microspheres （with diameter of 40-60 μm） as variables. The shape of microspheres was observed by scanning electron microscope. Results： The best ranges of the prescription included：drug to carrier material ratio：0.4-0.5;organic phase and water phase ratio：0.4-0.6;and first emulsion and oil phase ratio：0.13-0.17. The 3 batches of microspheres prepared according to the above condition were well-shaped （full sphere）, with the mean drug loading capacity being （10.25±0.08）% and the encapsulation efficiency being （30. 61±1.46）%. Conclusion： The optimized technique has a good reproducibility and can be used for preparation of Rg3-loaded chitosan microspheres for intranasal administration.

关 键 词：人参皂苷 壳聚糖 微球体 药物制备 药物设计 

分 类 号：R943.43[医药卫生—药剂学]