促渗剂对青蒿琥酯贴剂体外经皮吸收的影响

目的考察几种促渗剂对青蒿琥酯体外经皮吸收的影响,为青蒿琥酯贴剂的开发提供参考。方法采用TK-6A型透皮扩散仪,以SD大鼠腹部皮肤为透皮屏障,测定含有不同浓度促渗剂的青蒿琥酯贴剂的累计透过量和经皮渗透速率。结果各促渗剂对青蒿琥酯促渗作用大小依次为：油酸（OA）〉N-甲基吡咯烷酮（NMP）〉丙二醇（PG）〉氮酮（Azone）〉己二酸二异丙酯（IPA）。NMP和OA的促渗作用呈浓度依赖性,IPA和PG的促渗效果不随浓度的升高而增强,处方中高浓度的IPA和PG反而会抑制青蒿琥酯的透皮吸收。结论10%OA对青蒿琥酯的促渗作用最显著。

Effect of Permeation Enhancers on the Percutaneous Absorption of Artesunate in Vitro

Objective To investigate the effect of penetration enhancers on the percutaneous absorption of artesunate,and provide a reference for the development of artesunate transdermal delivery systems.Methods Penetration enhancers（in different concentrations） were incorporated into a 25% w/w artesunate matrix patch formulation.Modified Franz diffusion chambers and SD rat abdominal skin were used for in vitro skin permeation studies,the transdermal flux and permeation rate of artesunate in vitro were determined by HPLC. Result The enhancing effectiveness of the enhancers decreased in the order： OA〉NMP 〉 PG 〉 Azone 〉 IPA. Skin permeation was significantly enhanced by increasing the loading concentration of OA or NMP, larger IPA amount （8%） or PG amount （20%） could inhibit the permeation of artesunate. Conclusion Oleic acid was found to be the most efficient enhancer for artesunate, 10% is the most effective concentration.