硫酸铵梯度法制备盐酸表阿霉素长循环脂质体  

Preparation of epirubicin hydrochloride long circulating liposome by a method of ammonium sulfate trasmembrane gradients

作　　者：尹飞[1] 贺霞[2] 姜伟化[2] 杨磊[2] 刘慧[2] 闫笑笑[2] 邱立朋[2] 王东凯[2] 周晖[3] 

机构地区：[1]辽宁省肿瘤医院药学部,沈阳110042 [2]沈阳药科大学药学院,沈阳110016 [3]中国医科大学附属第一医院药剂科,沈阳110001

出　　处：《中国新药杂志》2013年第19期2296-2300,2313,共6页Chinese Journal of New Drugs

基　　金：沈阳市科学技术计划项目(F13-316-1-25)

摘　　要：目的:用硫酸铵梯度法制备盐酸表阿霉素长循环脂质体。方法:以包封率为评价指标,通过单因素-正交试验设计优化脂质体处方及工艺。结果:大豆磷脂浓度2.5%,药物磷脂比1∶12.5,磷脂胆固醇比例4∶1,硫酸铵浓度200 mmol·L-1,载药孵育温度50℃,载药时间30 min,PEG2000-DSPE摩尔比4%,药物包封率达97.84%。结论:用优化后的处方制备的盐酸表阿霉素长循环脂质体包封率高,粒度分布范围较窄,平均粒径较小。Objective： To prepare epirubiein hydrochloride-loaded long circulating liposome by a method of ammonium sulfate trasmembrane gradients. Methods： A single faetor-orthogonal test design was employed to opti- mize the prescription and process. The entrapment efficiency （EE） of the liposomes was used as the assessment cri- teria. Results： The optimized prescription and preparing process were as follows： the concentration of soybean phospholipid was 2.5 %, the ratio of drug to lipid （w/w） was 1 ： 12.5, the ratio of cholesterol to lipid （w/w） was 1 ： 4, the concentration of ammonium sulfate was 200 mmol. L- 1 and the incubation condition was 50 ℃ for 30 min, and the molar ratio of PEG2000-DSPE was 4%. The EE of liposomes was 97.84%. Conclusions ： Liposomes pre- pared by the optimized preparation have high EE and low particle size distribution index.

关 键 词：盐酸表阿霉素 长循环脂质体 硫酸铵梯度法 包封率 

分 类 号：R943.4[医药卫生—药剂学] R979.14[医药卫生—药学]