蛇床子素脂质体的处方优化及其体外释放度.pdf

· 728 · 中国医药工业杂志 Chinese Journal of Pharmaceuticals 2016, 47(6) 蛇床子素脂质体的处方优化及其体外释放度 张成龙1，张 季1，康 聪2，孟宪勇2，董晓华1* (1. 河北北方学院药学系，河北张家口 075000；2. 河北北方学院附属第一医院骨科，河北张家口 075000) 摘要 ：采用薄膜 - 超声分散法制备蛇床子素脂质体，以包封率为评价指标，采用单因素考察和正交试验优化蛇床子素脂 质体的处方和工艺条件。所得优化工艺为 ：胆固醇与蛋黄卵磷脂质量比为 1 ∶ 2，药脂比为 3 ∶ 20，Tris 缓冲液 pH 值为 8.2，成膜温度为 40 ℃。优化后 3 批脂质体的平均粒径和 ? 电位为 260 nm 和-28.1 mV，包封率为 88％。与蛇床子素溶液相比， 蛇床子素脂质体的体外释放呈现出一定的缓释特征。 关键词：蛇床子素；脂质体；处方优化；体外释放 中图分类号：R944.9 文献标志码：A 文章编号：1001-8255(2016)06-0728-04 DOI：10.16522/ki.cjph.2016.06.013 Formulation Optimization and in vitro Release of Osthole Liposomes ZHANG Chenglong1, ZHANG Ji1, KANG Cong2, MENG Xianyong2, DONG Xiaohua1* (1. Pharmacy Dept. of Heibei North University, Zhangjiakou 075000; 2. Dept. of Orthopaedics of the First Af? liated Hospital of Heibei North University, Zhangjiakou 075000) ABSTRACT: The osthole liposomes were prepared by film-ultrasonic dispersion method. The formulation was optimized by single factor test and orthogonal design with entrapment ef? ciency as the index. The optimal parameters were as follows: the ratio of cholesterol to yolk lecithin was 1∶2, drug-to-lipid ratio was 3∶20, pH value of Tris buffer was 8.2 and hydration temperature was 40 ℃. The average particle size, ? potential and entrapment ef? ciency of three batches of optimal liposomes were 260 nm, -28.1 mV and 88％, respectively. Compared with osthole solution, the in vitro release behavior of osthole from the liposomes demonstrated a sustained-release property. Key Words: osthole; liposome; formulation optimization; in vitro release 蛇床子素 (osthole，1) 是从中药蛇床子中提取 溶性和水溶性药物，增加药物在水相中的溶解度， 得到的单体物质，属香豆素类化合物，也是蛇床子