依达拉奉凝胶的制备及体外透皮性能研究

Preparation and in Vitro Permeation of Edaravone Gel

目的考察依达拉奉凝胶体外经皮渗透性,筛选凝胶剂最佳处方。方法采用Valin-Chien双室渗透扩散池,以大鼠离体皮肤为渗透屏障,以HPLC测定依达拉奉的浓度,考察含药量、月桂氮?酮用量、环糊精的型号和含量对依达拉奉凝胶剂经皮渗透性的影响。结果凝胶剂最佳处方为6%依达拉奉、10%月桂氮?酮、10%β-环糊精、2%羧甲基纤维素钠,依达拉奉12 h累积渗透量平均值为(501.95±27.59)μg·cm?2,渗透速率平均值为(42.25±7.39)μg·cm?2·h?1。结论依达拉奉凝胶剂具有较好的经皮渗透特性,有望成为新的给药制剂。

OBJECTIVE To prepare edaravone transdermal gel and to study its permeation ability in vitro. METHODS The skin permeation ability was evaluated by Valian-Chien permeation cells with isolated rat skin. The concentration of edaravone in samples was determined by HPLC to study the effect of different drug content, laurocapram amount, type and content of the cyclodextrin. RESULTS The optimal form ulation was composed with 6% edaravone, 10% laurocapram, 10% β-cyclodextrin, and 2% sodium carboxymethyl cellulose. The accumulative permeation amount of the gel was（501.95±27.59）μg·cm^-2 in 12 h, and the permeation rate was（42.25±7.39）μg·cm^-2·h^-1. CONCLUSION Edaravone gel prepared in the study would be developed as a novel transdermal preparation.