二黄凝胶贴膏的制备及体外评价

Preparation and in vitro evaluation of Erhuang Gel Paste

目的:制备二黄凝胶贴膏并进行体外释放与透皮特性研究。方法:采用正交实验设计,以初黏力、持黏力、剥离强度及主药独活的有效成分蛇床子素为指标,制备二黄凝胶贴膏,并采用改进的Franz扩散池及Strat-M膜分别进行二黄凝胶贴膏、二黄软膏的体外释放、透皮试验,采用高效液相色谱法定量分析接受液中蛇床子素含量,测定新、老两种剂型的体外释放度、透皮量及透皮率,对体外释放及透皮试验结果进行回归分析,并进行二黄凝胶贴膏的过敏性实验。结果:二黄凝胶贴膏的最佳处方为NP700∶卡波姆∶甘油∶甘羟铝∶酒石酸∶水(2∶0.8∶30∶0.1∶0.1∶61),其体外累积释放度、透皮量、透皮率分别为62.90%、0.0672mg/g、20.82%,二黄软膏的体外累积释放度、透皮量、透皮率分别为77.64%、0.0131mg/g、9.36%,二黄凝胶贴膏不会引起动物皮肤过敏反应。结论:经正交实验设计优化的处方稳定可行,制备的二黄凝胶贴膏外观美观,黏附性能优异,其体外释放速率大于透皮速率,透皮过程主要受皮肤屏障的限制,透皮量及透皮率均较原剂型为好,应用前景广阔。

Objective： To prepare Erhuang Gel Paste and do release and transdermal behavior researches in vitro. Methods： To prepare Erhuang Gel Paste by the orthogonal test, with the adhesive force, the holding adhesive power, the peeling strength and the osthole, the the effective component of the key herb Angelica, as the indicators. Strat-M membrane and advanced Franz diffusion cell were chosen in the release and transdermal experiments of the Erhuang Gel Paste and its ointment in vitro and to do regression analysis on these statistics. The content of osthole, the effective component of the key herb Angelica of the preparation was quantitatively determined by HPLC method to determine the release rate, penetration quantity and penetration rate of the two forms. The skin susceptibility test was done too. Results： The best formula is NP700 2, carbomer 0.8, glycerol 30, glycinate aluminum 0.1, tartaric acid 0.1 and water 61. The cumulative release rate, penetration quantity and penetration rate of the gel paste and the ointment in vitro were respectively 62.90%, 0.0672mg/g, 20.82%, and 77.64%, 0.0131mg/g, 9.36%. The Conclusion： The preparation optimized by orthogonal test is stable. The Erhuang Gel Paste looks nice, adheres goog, and the transdermal procedure of it is restricted by skin barrier as release speed is faster than the penetration speed. Erhuang Gel Paste might be widely used as the quantity and rate of penetration are both better than its ointment.