金花止咳巴布剂的离体小鼠经皮渗透动力学研究

目的:研究金花止咳巴布剂的离体小鼠的透皮性能及其体外经皮渗透动力学行为。方法:采用改良的Franz扩散池,以离体小鼠皮肤为屏障,采用HPLC法分别测定金花止咳巴布剂处方君药金银花中有效成分绿原酸、异绿原酸A、异绿原酸C透过离体皮肤的含量,计算体外经皮渗透动力学拟合方程。结果:金花止咳巴布剂中绿原酸、异绿原酸A、异绿原酸C在24 h后的体外经皮渗透速率分别为33.44%,31.32%,27.33%,体外经皮渗透动力学拟合度最高的方程分别为:(1)绿原酸:Higuchi方程,Q=2.546 6t^1/2+3.625 1,拟合度=0.971;(2)异绿原酸A:Higuchi方程,Q=1.455 5t^1/2+1.787 2,拟合度=0.973;(3)异绿原酸C:Higuchi方程,Q=0.307 4t^1/2+0.363 1,拟合度=0.948。结论:金花止咳巴布剂的离体小鼠体外经皮渗透行为以符合Higuchi方程拟合为优,拟合度最高,表明金花止咳巴布剂中有效成分逐步释放,释放速度平缓,释放曲线不会发生时滞现象,具有骨架型缓释制剂的特性。

In vitro percutaneous permeation kinetics of Jinhua Zhike Cataplasm in mice

OBJECTIVE To study the transdermal properties of Jinhua Zhike Cataplasm in vitro and its permeation kinetics in vitro.METHODS The modified Franz diffusion cell was used, and the isolated mouse skin was used as a barrier. The transdermal contents of chlorogenic acid, isochlorogenic acid A and isochlorogenic acid C in flos lonicerae, monarch drug of the preparation, were determined by HPLC.RESULTS The transdermal permeation rates of chlorogenic acid, isochlorogenic acid a and isochlorogenic acid C in Jinhua Zhike Cataplasm were 33.44% , 31.32% and 27.33%, respectively in 24 hours, the equations with the highest fitting degree were as follows: chlorogenic acid, Higuchi equation, Q=2.546 6t^1/2+3.625 1, fitting degree=0.971; chlorogenic acid A, Higuchi equation, Q=1.455 5t^1/2+1.787 2, fitting degree=0.973; chlorogenic acid C, Higuchi equation, Q=0.307 4t^1/2+0.363 1, fitting degree=0.948.CONCLUSION Higuchi equation is the best fit for the permeation behavior of Jinhua Zhike Cataplasm in vitro, which indicates that the effective components in Jinhua Zhike Cataplasm are released gradually with gentle release rates. There is no time lag in the release curves, and the release curves have the characteristics of matrix sustained-release preparation.