芪嘧啶的药代动力学  

Pharmacokinetics of stilbenemidine in experimental animals

作　　者：刘昌孝[1] 张振伦[1] 叶燕辉 温启珍 李洛生[3] 胡建程[3] 

机构地区：[1]国家医药管理局天津药物研究院,天津300193 [2]广州医药工业研究所,广州510250 [3]湖南医药工业研究所,长沙410005

出　　处：《中国药理学与毒理学杂志》1990年第4期289-292,共4页Chinese Journal of Pharmacology and Toxicology

摘　　要：本文报告芪嘧啶在大鼠(150 mg/kg)和家兔(100mg/kg)一次ig的药代动力学研究结果。采用分光光度法测定生物样品中的药物浓度,用3P87实用药代动力学程序处理药物浓度数据,并自动算出各项动力学参数和C-T曲线图。主要参数t_(1/2ke),t_(peak),C_(max),CL和V_d在大鼠分别为6.55 h,1.32 h,9.5μg/ml,1.46 L·kg^1·h^1和13.8 L/kg,家兔分别为1.98h,1.00h,7.1μg/ml,4.09L·kg^1·h^(-1)和11.7 L/kg。结果表明药物在大鼠肝中达峰时间短,峰浓度高,清除较慢,在肝、肾含量高于其它组织。由尿粪排泄量小,72 h累计量仅为给药量的11.5％,而且排泄速度慢,一次给药后72 h仍有一定量药物由粪尿排泄。Stilbenemidine is a new antitumor compound.This paper reports the pharmacokinetics of Stilbenemidine in rats and rabbits after single oral administration.The concentrations in biological samples were detected by spectrophotometry.The concentration-time data were fitted by using a practical pharmacokinetic program(3P87).The t1/2,tpeak,Cmax,Cl and Vd in rat were 6.55 h,1.32 h,9.5μg/ml,1.46 L*·kg-1·h-1 and 13.8 L/kg,respectively; those in rabbits 1.98 h,1.00 h,7.1μg/ml,4.09 L·kg-1·h1 and 11.7L/kg,respectively.The result of elimination kinetics in rat liver showed that tpeak was shorter,Cmax was higher and ke was lower.The concentrations in liver and kidneys were more than those in other tissues.The excreted amount from urine and faeces was very small,and the accumulated amount for 72 h was only 11.5 % of the administered dosage.

关 键 词：芪嘧啶 抗癌药 药代动力学 

分 类 号：R979.1[医药卫生—药品]