促进剂对青蒿琥酯体外经皮渗透的影响

Effect of Penetration Enhancers on the in vitro [WT2”,3FZ]Permeability of Artesunate through Excised Mouse Skin

以离体小鼠皮肤为渗透屏障，采用预处理法研究了多种促进剂对青蒿琥酯经皮渗透的增强作用，结果表明，药物经皮渗透符合零级动力学过程，几种渗透促进剂的促进作用大小依次为：薄荷油＞氮酮＞氮酮－丙二醇（１∶１）＞桉叶油＞松节油＞油酸＞桉叶油－丙二醇（１∶１）＞二甲基亚砜＞吐温－８０＞二甲基甲酰胺。各促进剂在实际处方中的作用效能有所下降，但作用大小次序不变。氮酮的促渗作用呈现浓度依赖性，其最佳浓度为３％

The effect of penetration enhancers on the in vitro permeability of artesunate through excised mouse skin was examined using the standing type diffusion apparatus. The results showed that the drug penetration rate decreased in the following order:pepermint oil, Azone,Azone propyleneglycol(PG)(1∶1), eucalyptus oil, turpentine oil, oleic acid(OA), eucalyptus PG(1∶1), dimethyl sulfoxide(DMSO), polysorbate 80(Tween 80), and dimethyl formamide(DMF). For all cases the drug penetration process could be described by zero order kinetic mechanism. Azone showed maximum penetration efficacy at 3% concentration.