癌光啉在兔体内的药代动力学及生物利用度  

A study of pharmacokinetics and the absolute bioavailability of PSD-007 in rabbits

作　　者：郑立卿[1,2] 阴慧娟[1] 李迎新[1] 陈洪丽[1] 

机构地区：[1]中国医学科学院.北京协和医学院生物医学工程研究所激光医学实验室,天津300192 [2]河北北方学院药理学教研室,河北张家口075000

出　　处：《中国药理学通报》2012年第4期573-577,共5页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 60678047);2010中央公益性院所基本科研业务费资助项目

摘　　要：目的研究癌光啉在兔体内的药代动力学及生物利用度特点,为药物进一步研究提供依据。方法兔腹腔注射或静脉注射10 mg.kg-1癌光啉,于给药后的10 min、30 min、1h、2 h、4 h、8 h、24 h、48 h、72 h耳缘静脉采血,以全波长酶标仪荧光法测定兔血浆中癌光啉浓度,用3P97处理血药浓度-时间数据,分析房室模型,得到最佳房室模型和药代动力学参数。结果家兔腹腔注射癌光啉10 mg.kg-1的时量曲线符合一室开放模型,静脉注射时的时量曲线符合三室模型,但其消除快于ip。主要药代动力学参数:ip给药组,T12Ke=11.6 h,Cmax=2.312 mg.L-1,AUC=43.177 mg.L-1.h,CL=0.232 L.kg-1.h-1,V/F(c)=3.888 L.kg-1;iv给药组,Vc=0.75 L.kg-1,T12α=2.824 h,T 12β=40.632 h,AUC=65.161 mg.L-1.h,CL(s)=0.153 L.kg-1.h-1。腹腔给药后绝对生物利用度是66.2%。结论癌光啉在兔体内吸收快、起效快、消除快,无蓄积现象,给药方式不同,药代动力学特点不同。Aim To investigate the pharmacokinetic characteristics and the absolute bioavailability of PSD-007 in rabbits.Methods The blood of rabbits was collected from the blink of the ears after ip/iv administration of PSD-007,and the plasma drug concentrations at different times were determined by ultraviolet visible spectrophotometer.The best compartment model and the pharmacokinetic parameters were calculated by the software of 3P97.Results The elimination process of PSD-007 fitted one-compartment model after ip administration of 10 mg·kg-1 of PSD-007,but fitted three-compartment open model after iv administration,the eliminate rate of which was faster.The principal pharmacokinetic parameters were T12Ke=11.6 h,Cmax=2.312 mg·L-1,AUC=43.177 mg·L-1·h,CL=0.232 L·kg-1·h-1,V/F（c）=3.888 L·kg-1;Vc=0.75 L·kg-1,T12α=2.824 h,T12β=40.632 h,AUC=65.161 mg·L-1·h,CL（s）=0.153 L·kg-1·h-1.The absolute bioavailability was 66.2%.Conclusions PSD-007 has fast absorption,quick effect and elimination,without accumulation phenomenon,and pharmacokinetic characteristics were different based on different ways of giving medicine.

关 键 词：药代动力学 癌光啉 新西兰兔 荧光 血浆 生物利用度 

分 类 号：R452[医药卫生—治疗学] R453[医药卫生—临床医学]