盐酸拓扑替康脂质体的制备及影响因素考察  

Studies on the preparation of liposomal topotecan hydrochloride and the influencing factors

作　　者：郝艳丽[1] 邓英杰[1] 陈妍[1] 王秀敏[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《中国药学杂志》2004年第8期602-604,共3页Chinese Pharmaceutical Journal

基　　金：国家新药研究基金项目(94-97-20)辽宁省教育厅重大项目计划(202043233)

摘　　要：目的 进行新型抗癌药物盐酸拓扑替康的脂质体制备研究,以期得到具有较高包封率的制备方法。方法采用薄膜分散法、乙醇注入法、反相蒸发法等传统的脂质体制备方法,以及新的主动载药方法制备盐酸拓扑替康脂质体,筛选出最佳的制备盐酸拓扑替康脂质体的方法,并且考察不同的影响因素对制备过程的影响。结果 通过主动载药方法--硫酸铵梯度法制备的盐酸拓扑替康脂质体,可以获得较高包封率(90％以上)和较大的药脂比,并且药物在脂质体内水相中可保持其内酯结构不发生转变,从而活性不受到影响。结论 硫酸铵梯度法作为主动载药方法--pH梯度法的一种,可以用于两亲性药物盐酸拓朴替康脂质体的制备,磷脂的组成、空白脂质体的粒径大小、硫酸铵的浓度、药脂比是影响包封率的主要因素。OBJECTIVE: To study the best preparation method of liposomal topotecan(TPT) hydrochloride by comparing the entrapment efficiencies of different methods. METHODS: TPT liposomes were prepared by thin-film dispersion, ethanol injection, reverse-phase evaporation vesicles, and active remote loading i.e. ammonium sulfate gradient. The effects of different preparation methods on drug loading and the different influencing factors in preparation of liposomal TPT by active loading were also studied. RESULTS: By the method of ammonium sulfate gradient, the encapsulation efficiency was over 90% and a high ratio of drug to lipid was got. Liposome-encapsulated TPT was more stable under physiological conditions. CONCLUSION: As a kind of active remote loading, the ammonium sulfate gradient method can be used to prepare TPT liposome and get satisfactory results.

关 键 词：盐酸拓扑替康 脂质体 制备 影响因素 抗癌药 

分 类 号：R979.1[医药卫生—药品]