高良姜素的体外透皮吸收特性研究

Study on the in vitro Transdermal Absorption Properties of Galangin

目的:考察高良姜素的体外透皮吸收特性及不同促透剂对其透皮行为的影响,为开发以高良姜素为原料药的治疗白癜风的皮肤给药制剂提供参考。方法:采用高效液相色谱法测定高良姜素的含量。以高良姜素的累积透过量(Q)和透皮速率(J)为指标,考察接收液[20%、40%聚乙二醇400(PEG400)溶液和30%乙醇溶液]、转速(200、300、400 r/min)对高良姜素在小鼠完整皮肤中吸收的影响,考察氮酮(1%、3%、5%)、丙二醇(10%、20%、40%)单用或者联用对其促透作用。同时,考察高良姜素在大鼠和小鼠的完整皮肤、去角质层皮肤、真皮层皮肤的透过特性。结果:以接收液为40%PEG400溶液、转速为300 r/min、5%氮酮单用时,高良姜素在小鼠完整皮肤中的透过性最好,J为3.257 0μg/(cm2·h)。小鼠完整皮肤、去角质层皮肤、真皮层皮肤的J分别为2.7199、34.016、33.874μg/(cm2·h),大鼠3种皮肤的J分别为0.499 6、9.512 4、17.406μg/(cm2·h)。结论:高良姜素可以透过小鼠和大鼠的完整皮肤,但是透过量远低于去角质层皮肤和真皮层皮肤。

OBJECTIVE：To investigate the in vitro transdermal absorption properties of galangin and effects of different penetration enhancers on its transdermal behaviors,and provide reference for developing skin preparations using galangin as APIs in the treatment of vitiligo. METHODS：HPLC was used to determine the galangin content. Using cumulative permeation rate（Q） and the transdermal rate（J）of galangin as indexes,the effect of absorption of receiving solution [20%,40% polyethylene glycol 400（PEG400）solution and 30% ethanol solution] and rotating rate（200,300,400 r/min）on galangin in complete skin of mice were investigated,as well as the azone（1%,3%,5%）and propylene glycol（10%,20%,40%）alone or combination on its penetration promotion. And the transdermal properties of galangin in complete skin,exfoliating skin,dermis skin of rats and mice were detected. RESULTS：The best permeability of complete skin of mice showed in 40% PEG400 solution at rotating speed of 300 r/minwith 5% azone alone,J was 3.257 0 μg（/cm^2·h）. Js of complete skin,exfoliating skin,dermis skin of mice were 2.719 9,34.016,33.874 μg（/cm^2·h）,respectively;and those of rats were 0.499 6,9.512 4,17.406 μg（/cm^2·h）. CONCLUSIONS：Galangin can penetrate the complete skin of mice and rats,however,the penetration quantity is far lower than exfoliating skin and dermis skin.