盐酸伊立替康脂质体的制备及体外释药特性研究  

Preparation and in Vitro Release of Irinotecan Hydrochloride Liposome

作　　者：张俭俭[1] 张佳佳[2] 杨建坤[3] 李华建[4] 王世霞[5] 曹德英[5] 

机构地区：[1]中国人民武装警察部队学院医院药剂科,廊坊市065000 [2]北京朝阳医院京西院区,北京市100043 [3]河北大学附属医院药剂科,保定市071000 [4]河北廊坊市人民医院检验科,廊坊市065000 [5]河北医科大学药学院,石家庄市050017

出　　处：《中国药房》2008年第10期762-764,共3页China Pharmacy

摘　　要：目的:制备盐酸伊立替康脂质体并考察其体外释药特性。方法:采用硫酸铵梯度法,通过正交试验进行盐酸伊立替康脂质体处方筛选和制备工艺研究;采用透析法考察体外释放度。结果:制备的盐酸伊立替康脂质体包封率较高,达到75·4%;通过正交设计确定最佳处方为磷脂与胆固醇质量比为2:1,硫酸铵溶液浓度为0·20mol·mL-1,孵育温度为50℃,药脂比为1:10;脂质体中药物1h释放8·09%,9h释放64·2%。结论:制备的盐酸伊立替康脂质体具有较高包封率和缓释特性。OBJECTIVE： To prepare irinotecan hydrochloride liposome and study its drug release profile in vitro. METHODS： Irinotecan hydrochloride liposome was prepared by ammonium sulfate gradient method, Orthogonal test was conducted to optimize the formula and preparation techniques of irinotecan hydrochloride liposome, and the release of it in vitro was investigated by dialysis method. RESULTS： The entrapment efficiency（EE） of the prepared liposome was as high as 75,4%, The optimized formula was as follows： the ratio of lipid to cholesterol was 2 ： 1; the concentrations of ammonium sulfate was 0.20 mol· mL^-1 the incubation temperature was 50℃and the ratio of drug to lipid was 1 ： 10, The study proved that the liposome could retard drug release in vitro, at a release rate of 8.09% at 1 h and 64.2% at 9 h, CONCLUSION： The irinotecan hydrochloride liposome had high EE and characterized by slow drug release.

关 键 词：盐酸伊立替康 脂质体 体外释药 

分 类 号：R979.1[医药卫生—药品] TQ460.6[医药卫生—药学]