盐酸尼卡地平贴剂的制备及体外透皮释药

Study on the preparation and penetration of nicardipine hydrochloride

目的 :制备盐酸尼卡地平透皮贴剂 ,研究其释药影响因素。方法 :利用Franz扩散池 ,进行离体皮肤体外渗透实验 ,通过改变皮肤的状态 ,研究其体外透皮释药。结果 :盐酸尼卡地平贴剂中药物的渗透可用Higuchi方程来表达。去除角质层皮肤的药物渗透远大于完整皮肤 ,而完整皮肤的贮库效应大于去角质层皮肤。结论 :盐酸尼卡地平在经皮渗透过程中存在贮库效应 ,渗透的主要屏障为角质层。

OBJECTIVE:To prepare nicardipine hydrochloride transdermal therapeutic system and study penetration mechanism. METHODS:Nicardipine permeation tests in vitro through rat skin in franz diffusion cells were performed to study the penetration mechanism of nicardipine by changing rat skin condition. RESULTS:The penetration rate of drug from hydrogel formulations could be described by Higichi's equation. The nicardipine permeation coefficient of stripped stratum corneum skin was higher than that of whole skin, and the deposit function of whole skin was more effecting than that of stripped stratum corneum skin. CONCLUSIONS:The barrier of nicardipine penetration is in the stratum corneum, and nicardipime permeating has the deposit function also in the stratum corneum. [