目的：研究制备澳洲茄边碱脂质体的最佳工艺，并建立起包封率的测定方法。方法：采用pH 梯度法制备澳洲茄边碱脂质体，以包封率为指标进行工艺优化，通过SephadexG-50 葡聚糖凝胶柱分离脂质体，高效液相色谱法测定澳洲茄边碱的包封率。结果：制备澳洲茄边碱脂质体的最佳条件，药物与卵磷脂的质量比为1颐30，胆固醇与卵磷脂质量比为1颐4，脂质体外水相pH 值最终调至6.5，孵育温度为55益，此时的包封率可以达到70%以上。结论：用pH梯度法能制备包封率较高的澳洲茄边碱脂质体。

The study was aimed to find the best method of detecting entrapment efficiency, the formula and preparation process of solamargine liposomes with pH-gradient method. Orthogonal design was used in the selection of optimum formulation. Unloaded solamargine were separated by Sephadex G-50 chromatography and HPLC method. Entrapment efficiency of solamargine 1iposomes was determined. The result showed that the optimal formulation is that drug/PC (mass ratio) is 1∶30; cholesterol/PC (mass ratio) is 1∶4; liposomes were pH 6.5 outside and incubated at 55℃. The encapsulation rate of solamargine liposomes was above 70%. It is concluded that liposomes were prepared with good entrapment efficiency by pH-gradient method.

科学技术部国家科技重大专项课题重大新药创制项目（2009ZX09103-389）；中药制药过程新技术国家重点实验室，负责人：萧伟。