盐酸伊立替康脂质体的制备  

The Preparation of Liposome of the CPT-11

作　　者：韩婷 

机构地区：[1]辽宁省沈阳陆军总院,110016

出　　处：《中国医药指南》2008年第17期36-38,共3页Guide of China Medicine

摘　　要：目的结合脂质体这种新型给药载体的特征将盐酸伊利替康(Irinotecan,OPT-11)制备成脂质体以解决喜树碱类药物在生理条件下其结果中的内酯环易发生水解反应转变为羟酸盐形式,从而失去活性这个难问题.方法以包封率为主要评价指标,比较了传统的脂质体制备方法(薄膜分散法、乙醇注入法、反向蒸发法等)与主动载药方法-硫酸铵梯度法对伊立替康脂质体制备的影响.结果采用硫酸铵梯度法制备伊立替康脂质体可以获得较高的包封率、较大的药酯比.结论硫酸铵溶液的浓度、孵育时间和温度空白脂质体的粒径大小等是影响伊立替康脂质体包封率的主要因素.Objective Based on the characteristics of liposome a new drug carrier,CPT-11 is prepared for a liposome so that it can solve the problem that the lactone structur of camptothecine easily hydrolyses to be inactive carboxylate form at physiology condition. Method Compare the methods of preparation of the liposomal CPT-11,which cotain thin film dispersion,ethanol infection,reverse- phase evaporation and active remote loading ammonium sulfate gradient through studying the encapsulation efficiency.Resunts The results showed that higher encapsulation efficiency and drug-to-lipid ratio were got by ammonium gradent method.Conclusion The lipids to drug and vesicle size of blank liposome were the main factors influencing the encapsulation efficiency of CPT-11 liposomes by ammonium sulfate gradient method.

关 键 词：伊主替康 脂质体 主动载药 硫酸铵梯度法 

分 类 号：R979.1[医药卫生—药品]