环维黄杨星D透皮贴剂体外释放度与经皮渗透实验∗

摘要

Objective To explore the release and percutaneous penetration of cyclovirobuxine D patches at different concentrations in vitro. Methods The release curves of cyclovirobuxine D patch in vitro were fitted by ritger-peppas mathematical model, and the patch release mechanism was discussed according to the fitting parameters. At the same time, compared the percutaneous permeability characteristics of 0.25,0.5,1.0,2.0 mg.( cm2 )-1 of cyclovirobuxine D patch by using a modified Franz diffusion cell, with isolated rat skin serving as transdermal barrier. Results Ritger-Peppas model fitting equation for cyclovirobuxine D patch [1.00 mg.(cm2)-1]was: Mt/M=0.964 6 t1.621 6.And the percutaneous penetration curve was best fitted to Higuchi kinetics equation.The drug release rate from the patch matrix was greater than the rate of penetration through the skin, indicating the patch at the time through rat′s skin was a passive diffusion process, and transdermal process was rate-limited by skin. Conclusion Kinetics equation fitting is an effective method for analyzing drug release and permeation behavior of cyclovirobuxine D patch in vitro.%目的：探讨不同浓度环维黄杨星D透皮贴剂的体外释放与经皮渗透行为。方法将环维黄杨星D透皮贴剂的体外释放曲线与Ritger-Peppas数学模型进行拟合,根据拟合参数判断该贴剂的释药机制。同时采用改良Franz扩散池,以离体大鼠皮肤为透皮屏障,比较0.25,0.5,1.0,2.0 mg.(cm2)－1环维黄杨星D透皮贴剂的经皮渗透特性。结果药物浓度为1.00 mg.(cm2)－1的贴剂体外释放度数据Ritger-Peppas模型拟合方程为：Mt/M＝0.9646t1.6216,四个药物浓度环维黄杨星D透皮贴剂在20 h内体外经皮渗透曲线均以Higuchi动力学方程拟合较优,且药物从贴剂基质中释放速率均大于渗透通过皮肤的速率,该贴剂属于骨架溶蚀型释药系统,其透皮过程主要以皮肤限速方式进行。结论动力学方程拟合方法可有效分析环维黄杨星D贴剂的体外释药与经皮渗透行为。