目的将青风藤在电致孔电离巴布剂条件下透皮给药,用房室模型法初步分析考察电致孔巴布剂透皮给药的药动学特点。方法制备青风藤电离巴布剂,以所含青藤碱为检测指标,采用双室扩散池、高效液相色谱法测定血药浓度,采用AIC法判断药动学房室模型。结果青风藤电离巴布剂在电致孔条件下透皮给药符合线性乳突型单室开放模型,其模型参数K=0.056,Ka=0.232,体内药物浓度与时间的关系方程为C=2.884×(e^-0.056t-e^-0.232t);单纯被动扩散的模型参数K=0.058,Ka=0.149,体内药物浓度与时间的关系方程为C=2.512×(e^-0.058t-e^-0.149t)。结论可以用一级吸收、一级消除的线性乳突型单室开放模型分析青风藤电离巴布剂电致孔技术透皮给药的体内药物浓度随时间的变化规律。电致孔技术与被动扩散比较,能够提高透皮给药的生物利用度。

Objective To study the effects on electroporation of Qingfengteng cataplasma transdermal absorption and describe the characteristics of animal pharmacokinetics of it.Methods Two-chamber diffusion cell was used and the plasma drug concentration was determined by HPLC.The application of AIC theory to analysis of the compartmentally based model of sinomenine transdermal delivery by electroporation.Results The Cmax,Ka,and AUC0→∞ of electroporation was larger than those of passive diffusion;t1/2(Ka)and tmax of electroporation were reduced compared with passive diffusion.The drug concentration-curve equation were C=2.884×(e^{-0.056 t}-e^{-0.232 t})and C=2.512×(e^{-0.058 t}-e^{-0.149 t})for electroporation and passive diffusion,respectively.Conclusion The change of in vivo drug concentration of Qingfengteng calaplasma transdermal absorption by electroporation could be analized in accordance with mammillary one-compartment open model.The etrectroporation technology could sharply enhance the bioavalibility compared with the passive diffusion.