苏艳莹 雷小小 桂卉 夏新华 周莉莉

    中图分类号 R350.35 文献标志码 A 文章编号 1001-0408(2018)19-2612-05

    DOI 10.6039/j.issn.1001-0408.2018.19.05

    摘 要 目的：优化山茱萸总环烯醚萜苷脂质体的制备工艺，并对其进行表征。方法：采用逆相蒸发法制备山茱萸总环烯醚萜苷脂质体。采用高效液相色谱法测定山茱萸总环烯醚萜苷脂质体中马钱苷和莫诺苷含量。以总皂苷(以马钱苷和莫诺苷总和计)包封率为指标，通过单因素试验筛选制备山茱萸总环烯醚萜苷脂质体的主要工艺因素后，采用星点设计-效应面法优化药物与磷脂的质量比(药脂比)、胆固醇与磷脂的质量比(胆脂比)和水合介质pH值。利用达尔文激光粒径测定仪测定最优处方下所制脂质体的Zeta电位和粒径，并在透射电镜下观察其形态。结果：确定最优处方的药脂比为0.026、胆脂比为0.107、水合介质pH为5.78。所制3批脂质体的平均包封率为11.63%(n=3)，与预测值11.48%的相对误差为1.29%；平均粒径为(80.87±0.27) nm，Zeta电位为(-13.60±5.32) mV，脂质体外观呈球形或类球形。结论：优化后山茱萸总环烯醚萜苷脂质体制备工艺简单，所制脂质体粒径较小。

    关键词 星点设计-效应面法；山茱萸总环烯醚萜苷；脂质体；逆相蒸发法；制备工艺

    ABSTRACT OBJECTIVE： To optimize the preparation technology of Total iridoid glycosides liposome of Cornus officinalis， and to characterize it. METHODS： Total iridoid glycosides liposome of C. officinalis was prepared by reverse phase evaporation method. The contents of loganin and morroniside in Total iridoid glycosides liposome of C. officinalis were determined by HPLC. Using encapsulation rate of total saponins (total contents of loganin and morroniside) as index， main technology factors for the preparation of Total glycosides liposome of C. officinalis were screened by single factor test； the ratio of drug to phospholipid (drug-lipid ratio) ......