茶碱微乳经皮吸收及药代动力学研究  

Transdermal absorption and pharmacokinetics of theophylline microemulsion

作　　者：赵鑫[1] 刘建平[1] 朱家壁[1] 

机构地区：[1]中国药科大学药物制剂研究所,南京210009

出　　处：《中国药科大学学报》2006年第1期28-32,共5页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.30371699);江苏省自然科学基金资助项目(No.BK2001081)~~

摘　　要：目的:研究茶碱微乳在家兔不同皮肤部位给药后的经皮吸收及药代动力学。方法:采用HPLC测定血浆中茶碱的浓度,应用基于Guass-Newton-Zhu原理设计的NLFTZ计算机程序对实验数据进行解析。结果:茶碱微乳经背部肺腧穴给药后的血药浓度高于非穴位给药,有极显著性差异(P<0.01);茶碱经皮吸收符合两个独立的具不同时滞的零级吸收、一级消除的一室模型迭加形成的复合模型,血药浓度平稳,可以维持24 h以上。结论:茶碱微乳经皮吸收均具有双通道、双过程复合的特征;穴位经皮给药的两种通道中存在特殊的加速通道,而药物经穴位周围皮肤的穿透表现为慢吸收过程。Aim：To investigate the transdermal absorption and pharmacokinetics of theophylline microemulsions on the acupuncture points of rabbits. Methods： Theophylline concentration in plasma was determined by HPLC. The pharmacokinetic parameters were estimated by application of NLFTZ program based on the principle of Guass-NewtonZhu. Results： The plasma concentrations of theophylline following administration via Feishu point were statistically significantly higher than those via conventional application （ P 〈 0.01 ）. The plasma level-time profile of theophyllines- rIDS was better fitted to a complex model consisting of two independent zero-order absorption processes with no lagtimes and first-order elimination process. Conclusion： The transdermal delivery of theophylline microemulsian showed characteristics, i.e. double-path ways and double processes. ＂Special transport route＂ might exist in the double-path ways of penetration through acupuncture point while slow transport occurs through non-point.

关 键 词：茶碱 微乳 经皮给药系统 肺腧穴 药代动力学 

分 类 号：R96[医药卫生—药理学]