萜烯类化合物对吲哚美辛脂质体凝胶透皮吸收的影响

发布时间：2018-05-25 10:11

本文选题：吲哚美辛 + 脂质体凝胶　；参考：《中国新药杂志》2017年16期

【摘要】：目的:制备吲哚美辛脂质体凝胶,考察不同吸收促进剂对其体外透皮吸收的影响。方法:以卡波姆作为凝胶基质,采用薄膜分散法制备脂质体,分别考察磷脂和胆固醇的比例、药物和磷脂的比例对吲哚美辛包封率的影响,优化并选择最佳处方;采用立式改良Franz扩散池,研究萜烯类化合物对吲哚美辛脂质体凝胶体外透皮吸收的影响。结果:磷脂/胆固醇(SPC/CH)及药物/磷脂的最佳比例分别为6∶1和1∶30。凝胶基质为4%卡波姆,最佳透皮吸收促进剂为2.5%葑酮,吲哚美辛脂质体凝胶的累积渗透量Q24达到(198.36±15.78)μg·cm~(-2),稳态透皮速率(JS)为(7.93±3.01)μg·cm~(-2)·h~(-1)。结论:2.5%葑酮对吲哚美辛脂质体凝胶的促渗作用良好,为今后开发经皮给药制剂提供理论基础。
[Abstract]:Aim: to prepare indomethacin liposome gel and investigate the effect of different absorption enhancers on its transdermal absorption in vitro. Methods: liposomes were prepared by membrane dispersion method with Carbomer as gel matrix. The effects of the ratio of phospholipid to cholesterol and the ratio of drug to phospholipid on the entrapment efficiency of indomethacin were investigated. The effect of terpenes on the transdermal absorption of indomethacin liposome gel in vitro was studied by using a vertical modified Franz diffusion cell. Results: the optimum ratios of phospholipid / cholesterol SPC / Ch and drug / phospholipid were 6:1 and 1: 30 respectively. The gel matrix was 4% carbomer, the optimal transdermal absorption promoter was 2.5% fenchone, the cumulative permeation capacity Q24 of indomethacin liposome gel was up to 198.36 卤15.78 渭 g / cm ~ (-2) C ~ (-2), and the steady-state penetration rate was 7.93 卤3.01 渭 g 路cm ~ (-2) 路h ~ (-1) 路h ~ (-1). Conclusion the effect of 2.5% fenchone on the permeation of indomethacin liposome gel is good, which provides a theoretical basis for the development of transdermal drug delivery preparations in the future.
【作者单位】：吉林医药学院;
【基金】：国家自然科学基金项目(31572262) 吉林省科技发展计划项目(20160414050GH):吲哚美辛凝胶的微针制备研究
【分类号】：R943

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