盐酸丁螺环酮透皮促渗剂选择及其透皮机制的研究

目的研究透皮促渗剂对盐酸丁螺环酮体外经皮渗透的影响以及盐酸丁螺环酮的透皮机制。方法采用改良Franz扩散池,比较不同促渗剂种类、浓度、配比对盐酸丁螺环酮的促渗效果,同时通过改变扩散池的介质pH及皮肤的状态,研究药物的透皮机制。结果采用3%氮酮为透皮促渗剂时药物透过量最大。盐酸丁螺环酮随着分子型浓度的升高透过量也随之增加,皮肤去除角质层后,药物的透过量显著大于完整皮肤,而完整皮肤的贮库效应大于去角质皮肤。结论药物透皮以3%氮酮为透皮促进剂促渗效果最佳。盐酸丁螺环酮主要是以分子型透过皮肤,药物的透皮屏障与贮库效应发生的主要部位是皮肤的角质层。

Optimization of Transdermal Penetration Enhancer for Buspirone Hydrochloride and Study on in Vitro Permeation Mechanism

OBJECTIVE To study the effect of penetration enhancers for buspirone hydrochloride on drug permeation of rats skin in vitro and the percutaneous mechanism of buspirone hydrochloride. METHODS The Franz diffusion chamber was applied for evaluating the different kinds, concentration and proportion of penetration enhancer on the buspirone hydrochloride permeability in vitro. By inspecting the effect of medium pH and skin condition on the permeation to study the percutaneous mechanism. RESULTS It was discovered that drug had favorable permeation with 3% Azone as the enhancer of buspirone hydrochloride. With increase of molecular pattern concentration, the steady permeation speed of buspirone hydrochloride was elevated. The barrier effect of stripped stratum corneum was less than that of whole skin, and the deposit function of whole skin was more significant than that of stripped stratum corneum skin. CONCLUSION The effect of promoting penetration of 3% Azone is the best, the drug permeates easily with molecular pattern. Stratum corneum is the leading barrier and reservoir site when medicine is permeating through the skin.