依达拉奉软膏的处方筛选及体外透皮性能研究

    Prescription Screening and in Vitro Permeation of Edaravone Transdermal Ointment

    • 摘要: 目的 考察依达拉奉软膏体外皮肤渗透性,筛选软膏剂最佳处方。方法 以大鼠离体皮肤作为渗透屏障,采用Valin-Chien双室渗透扩散池,以HPLC测定依达拉奉的浓度,考察依达拉奉含量、环糊精的型号和含量以及月桂氮卓酮用量对依达拉奉软膏剂经皮渗透性的影响。结果 软膏剂处方的最佳组合为6.0%依达拉奉,8.0%月桂氮卓酮,3.0%β-环糊精,依达拉奉12 h累积渗透量平均值可达(1 215.88±27.59)μg·cm-2,平均渗透速率为(103.69±7.39)μg·cm-2·h-1结论 软膏剂具有较好的皮肤渗透特性,有望成为依达拉奉新的给药剂型。

       

      Abstract: OBJECTIVE To investigate the in vitro skin permeability of edaravone ointment and screen its best prescription. 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, so as to investigate the effect of edaravone content, cyclodextrin type, cyclodextrin content, and azone dosage on its skin permeation ability. RESULTS The best combination of ointment prescription was composed with 6.0% edaravone, 8.0% azone and 3.0% β-cyclodextrin. The accumulative permeation amount of the ointment was (1 215.88±27.59)μg·cm-2 in 12 h, and the permeation rate was (103.69±7.39)μg·cm-2·h-1. CONCLUSION Ointment has good skin penetration properties and is expected to be a new dosage form for edaravone.

       

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