多柔比星海藻酸钙微球的制备及其载药、释药性质的研究  

Preparation and characteristics of doxorubicin alginate microspheres

作　　者：刘丹[1] 王鹏程[1] 刘昕[1] 李明光[1] 齐宪荣[1] 

机构地区：[1]北京大学药学院药剂学研究室,北京100083

出　　处：《中国新药杂志》2006年第15期1260-1264,共5页Chinese Journal of New Drugs

基　　金：国家高科技研究发展计划(836计划)基金资助(2003AA326020)

摘　　要：目的:考察多柔比星海藻酸钙微球的制备工艺及载药、释药性质。方法:考察不同处方微球的粒径、机械强度、降解等性质,筛选出最佳处方;以多柔比星为模型药物研究其对药物的承载能力及体外释药特性。结果:制备的微球圆整且分散性好,粒径均匀。多柔比里海藻酸钙微球的载药量达30％以上,包封率在90％以上;在体外37℃生理氯化钠溶液中释放显示具有缓释作用。结论:该微球对多柔比星具有较高的承载能力,并有较好的缓释作用,可满足临床治疗动脉栓塞需要。Objective： To investigate the preparation, inclusion rate and dissolution of doxorubicin-alginate microspheres. Methods： The formulation of alginate microspheres was optimized based on the size, distribution, strength to withstand the mechanical stress and degradation in vitro of microspheres. Doxorubicin was encapsulated into the alginate microspheres. The inclusion rate and dissolution of the microspheres were assessed. Results： The doxorubicin-alginate microspheres looked spherical, homogeneous and well distributive, contained 〈 30% doxorubicin and possessed an entrapment rate of more than 90%. The microsphere released drug gradually for prolonged action in vitro. Conclusion： The doxorubicin-alginate microspheres with higher loading amount featured sustained-release of drug substance.

关 键 词：海藻酸钙微球 多柔比星 包封率 动脉栓塞 

分 类 号：R943.41[医药卫生—药剂学] R979.14[医药卫生—药学]