西罗莫司脂质体的制备及处方因素考察.pdfVIP

中国抗生素杂志2010年2月第35卷第2期 . 119 . 文章编号：1001-8689 （2010 ）02-0119-04 西罗莫司脂质体的制备及处方因素考察 1 2 1 1 1 1,* 王晓宇 苗志林 陈超 董晓东 崔丽莉 邓英杰 （1 沈阳药科大学，沈阳110016；2 辽宁省人民医院，沈阳110016 ） 摘要： 目的 制备西罗莫司脂质体并对处方进行筛选, 以期得到高包封率的脂质体制剂。方法 选用乙醇注入法制备西罗莫 司脂质体，微柱离心-HPLC法测定包封率，以包封率为评价指标, 考察磷脂浓度、磷脂胆固醇质量比、药脂比、水相介质pH等 因素对脂质体的影响,在此基础上运用正交设计对处方进行优化。结果 正交试验结果表明磷脂浓度为4% ，磷脂与胆固醇质量比 例为8:1，药物磷脂质量比为1:20，水相pH为7.4为最佳处方，制得的脂质体包封率为（82.11±2.13 ）% 。结论 优选出最佳处方， 制得的西罗莫司脂质体包封率高，重现性好。 关键词： 西罗莫司；脂质体；包封率；单因素考察：正交设计 中图分类号： R979.5 文献标识码： A Preparation and study on formulation of sirolimus liposomes 1 2 1 1 1 1* Wang Xiao-yu , Miao Zhi-lin , Chen Chao , Dong Xiao-dong , Cui Li-li and Deng Ying-jie (1 Shenyang Pharmaceutical University,Liaoning, Shenyang 110016; 2 Liaoning Provincial People′s Hospital, Liaoning ,Shenyang 110016) Abstract Objective To optimize the formulation of prepared sirolimus liposomes with high encapsulation effi ciency ( EE% ). Methods Sirolimus liposomes were prepared by ethanol injection method and the encapsulation efficiency was determindated by the minicolumn centrifugation-HPLC method.The single factors such as the concentration of PC,the ratio of PC to cholesterol,the ratio of drug to PC and the pH value of aqueous phase were studied. And the orthogonal design was adopted to obtain the optimized prescription, the main index was entrapment effi ciency. Results The best prescription is as follows: the concentration of PC was 4%, the ratio of PC to cholesterol was 8:1, the ratio