透皮促渗剂对盐酸氟西汀经皮渗透性的影响

Effects of penetration enhancers on skin permeation behavior of fluoxetine hydrochloride in vitro

目的:研究不同促渗剂及其组合对盐酸氟西汀经皮渗透性的影响,评价药物透皮给药的可行性。方法:采用Valia-Chien水平扩散池进行药物在大鼠皮肤的体外渗透性试验,用高效液相色谱进行分析检测。结果:除了丙二醇外,氮酮、水溶性氮酮、N-甲基吡咯烷酮、油酸等透皮促渗剂单用及其组合对盐酸氟西汀均有促透作用(P<0.05或P<0.01),其中氮酮联用丙二醇或氮酮联用N-甲基吡咯烷酮对盐酸氟西汀的经皮促透作用最强。结论:恰当地选取透皮促渗剂联用可使盐酸氟西汀经皮渗透起到更好的促透效果。

Objective：To study the effects of penetration enhancers and their combinations on the transdermal delivery of fluoxetine hydrochloride and to discuss the feasibility of transdermal administration of drugs. Methods： The penetration rate of fluoxetine hydrochloride through rat skin in vitro was measured using Valia-Chien diffusion cells and high pressure liquid chromatography was used for analysis. Results： Penetration enhancers, such as Azone, N-methyl-2-pyrrolidone（ NMP）, oleic acid, and their combinations all had peneration enhancing effect except for propylene glycol（PG）. Azone combined with PG or NMP had the most potent enhancing effect. Conclusion： Satisfactory penetration of fluoxetine hydrochloride through rat skin can be obtained by correct combination of enhancers.