微透析技术-同位素示踪法联用进行青藤碱贴剂的皮肤局部药代动力学研究

目的: 进行青藤碱贴剂的皮肤局部药动学研究。 方法: 微透析技术与同位素示踪法联用,以HPLC-UV和液闪计数仪为检测工具,以微透析探针为采样手段,将线性微透析探针植入大鼠皮下组织,采用释放量法测定青藤碱皮肤相对损失率,实时、活体、动态监测青藤碱皮下组织浓度。皮肤微透析样品浓度经相对损失率校正后进行房室和非房室模型拟合。 结果: 房室模型拟合不佳。非房室模型参数显示皮肤药物浓度达峰时间约6.3 h,平均滞留时间MRT约18 h。 结论: 微透析法较好的采集了青藤碱贴剂经皮给药的皮肤局部药动学特征,是局部药动学良好的研究手段。

Local Pharmacokinetics Study of Sinomenine Patch by Using Microdialysis Technology Combined with Isotope Tracer Method

Objective: To study the skin local pharmacokinetics of Sinomenine Patch. Method: The microdialysis technology was used as sampling tool combined with isotope tracer method. The HPLC-UV detector and liquid scintillation counter was selected as detection tool. The relative loss(RL) was determined by using delivery method. The liner probes were implanted into the subcutaneous tissue to determine the real-time, in vivo concentration of sinomenine. The skin microdialysis sample was calibrated by relative loss and fitted with compartment and non-compartment model. Result: The compartmennt model was not the good model. The non-compartment parameters showed that the maximum skin concentration appeared at about 6 h after drug administration and the mean residence time (MRT) was about 18 h. Conclusion: The microdialysis technology could collecte the local skin pharmacokinetics characteristics of transdermal administration and of sinomenine was the appropriate study tool.