微透析技术用于化疗药物——吉西他滨体内药动学的初步研究  

Pharmacokinetic reseach of anti-cancer drug-Gemcitabine in vivo model by microdialysis technique

作　　者：谢波[1] 凌家俊[2] 吴秀君[2] 付湘[2] 黄雪琴[1] 

机构地区：[1]广州军区广州总医院肿瘤科 [2]广州中医药大学中药学院

出　　处：《中国临床药理学与治疗学》2010年第9期1035-1039,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：广东省医学科研基金项目(A2007481);国家自然科学基金项目(30772791);广东省科技计划项目(2010B030700035)

摘　　要：目的:建立以微透析法(microdialysis,MD)为采样技术的肿瘤化疗药物在体检测方法,并进行药动学研究。方法:以吉西他滨(GEM)为研究对象,大鼠为实验动物,采用尾静脉注射为给药方式,通过微透析技术进行血管内取样,对血药浓度进行在线、实时、连续监测,求算相关药动学参数。结果:GEM在大鼠体内血液中的探针回收率为(11.9±2.0)%,经大鼠尾静脉给药后GEM体内过程为二室模型,其消除和分布为一级动力学过程。实验过程中大鼠未见明显副作用。结论:微透析技术可用于活体动物体内GEM浓度的连续监测,提示微透析技术可用于抗肿瘤药物的局部药动学研究。AIM：To estabalish the methodology of microdialysis technique in pharmacokinetic（PK） reseach of anticancer drugs in vivo. METHODS：Gemcitabine（GEM） was injected into mice＇s tail vein.The microdialysate samples from blood were collected after dosing in gemcitabine-treated mices.The concentration of GEM was detected real-time continuously and pharmacokinetic parameters were evaluated.RESULTS：The recovery rate of GEM in vivo was（11.9±2.0）%.It showed that the pharmacokinetics of gemcitabine was two-compartment model in vivo and the elimination and distribution of GEM meets the first kinetics.There were no serious side effects in model mice.CONCLUSION：Microdialysis can be successfully employed in living body to detect the concentration of GEM continuously,which prompts it is possible to study the PK of anticancer drugs in malignant tissues in vivo.

关 键 词：微透析 吉西他滨 肿瘤 药动学 

分 类 号：R37[医药卫生—病原生物学]