吡喹酮脂质体凝胶的研制及其体外透皮扩散研究

目的：研制吡喹酮（PQ）的脂质体凝胶（PQ—LG），并对其体外释药特性进行考察。方法：薄膜分散法制备PQ脂质体，以泊洛沙姆-407为凝胶基质，研制PQ—LG。采用均匀设计对PQ—LG的处方及制备工艺进行优化，对其体外主要性质进行考察，并采用鼠皮为吸收屏障，对其体外透皮透皮速度及程度进行评价。结果：PQ—LG的最佳处方及工艺条件为：类脂／药物为20：1，pH为6．5，蒸发温度为45℃，水化时间为30min。体外性质表明PQ—LG外形圆整，平均粒径为（866．6±18．8）nm，平均包封率（ER）为74．33±1．95％（n=3）；体外透皮实验表明PQ．LG的透皮累积透过量Q符合Higuehi方程：Q=34．15t1/2 2．76（r=0．9948），与PQ凝胶相比，Q及稳态透皮速率J均有明显提高（P〈0．05）。结论：PQ—LG具有制备简单，质量理想，透皮吸收好等特点，值得进一步进行体内研究。

Study on the Preparation and Transdermal Penetration in Vitro of Preaziquantel Lipogels

Objective： To study the preparation and transdermal penetration in vitro of preaziquantel lipogels （PQ-LG）. Method： The film dispersion method was applied to prepare PQ-LG with Poloxamer-407 as base. The formulation and preparation process was screened by the uniform design and the main properties in vitro were also studied. The Franz-diffusion cell was used to compare the permeation rates and amount of PQ-LG with those of PQ gels. Result ： The optimal formulation and preparing conditions were as the following ： lipids/PQ of 20： 1, pH of 6. 5, evaporating temperature of 45 22 and the hydration time of 30min. The mean diameter of PQ-LG was （866. 6 ± 18.8） nm and mean entrapment efficiency （ER） was （ 74. 33 ± 1.95 ） % （ n = 3 ）. The accumulation penetration amount （Q） was according to Higuchi equation：Q = 34. 15t1/2 -22. 76 （r = 0. 994 8 ）. Compared with PQ gels, Q and J were both enhanced significantly （ P 〈 0. 05 ）. Conclusion ： PQ-LG with simple preparation process, promising quality and enhanced transdermal penetration is valuable to be studied in vivo.