基于微透析技术的苦参碱凝胶经皮给药的药动学研究

目的 建立同步测定经皮给药制剂在皮肤、血液中药动学的方法，研究苦参碱凝胶在体内的药动学行为。方法 应用经体外和体内回收率校正建立的基于微透析探针的皮肤血液双位点同步微透析系统，通过在皮肤和颈静脉植入探针，在大鼠腹部脱毛部位给予苦参碱凝胶，连续收集探针中12 h的透析液，并采用LC-MS微量检测技术测定探针透析液中的药物浓度。结果 本研究成功构建了双位点同步微透析药动学评价系统，大鼠皮肤给予苦参碱凝胶后，皮肤中的药物浓度、AUC值、半衰期均显著高于血液中药物浓度。结论 本研究建立的微透析结合LC-MS的取样及检测技术为经皮给药制剂的药动学研究提供了新的技术平台。

Pharmacokinetics study on matrine gels based on micro dialysis

Objective To establish a pharmacokinetic method for simultaneous determination the drug concentration in the skin and blood for transdermal formulations,and to study the absorption and metabolism of matrine gel in vivo.Methods A micro dialysis probe-based skin-blood synchronous micro dialysis system was established.After the probe was implanted into the skin and jugular vein,the matrine gel was administered.The dialysate in the probe was continuously collected for 12 h.The concentration of the drug in the probe dialysate was determined by LC-MS.Results In this study,a two-site synchronous micro dialysis pharmacokinetic evaluation system was successfully established.After given matrine gel,the concentration,AUC and half-life of the drug in skin were significantly higher than that in blood.Conclusion The established micro dialysis system combined with LC-MS could provide a new technology platform for the pharmacokinetic study on transdermal formulations.