抗晕动姜贴的处方优化及体外经皮渗透性实验

Optimization of Zingiber patch formula and its percutaneous permeability in vitro

目的:制备抗晕动姜贴,优化其处方并考察其离体皮肤经皮渗透特性。方法:建立姜贴中指标成分6-姜酚的分析方法,比较干姜的提取工艺并制备姜贴,采用全自动体外透皮扩散实验仪进行处方筛选并研究其经皮渗透特征。结果:干姜经超临界CO2(SFE-CO2)萃取的提取物中6-姜酚的含量高于渗漉提取所得提取物。处方③[超临界CO2萃取姜油、进口聚丙烯酸压敏胶(德国罗姆公司)和1%氮酮]体外经皮渗透性较好。除处方③2 h内具有较强透过外,其他处方均呈零级释放。结论:超临界CO2萃取法提取干姜优于乙醇渗漉法,将超临界提取姜油采用进口聚丙烯酸压敏胶加入1%氮酮制成400 mg/贴的贴剂,能有效通透过皮肤,为抗晕动药效的发挥奠定了基础。

Objective ： To prepare the antimotion sickness drug of Zingiber patch, to optimize its formula and study its percutaneous permeability in vitro. Methods： 6-gingerol was determined to compare two extractive of Zingiber. The formula was optimized and its permeability in vitro was measured. Results：The supercritical CO2 extractive contented a higher concentration of 6-Gingerol than percolate extractive. The extraction with supercritical CO2 , import polyacrylic acid glue and 1% azone improved the permeability with a high transit through skin after two hours. Others showed a zero order release. Conclusion：Supcrcritical CO： extraction of Zingiber is superior to percolate extraction, and the 400 mg patch by Supcrcritical CO2 extractive, imported polyacrylic acid glue and 1% azone, can permeate skin efficiently.