口服抗肿瘤药赛特铂在大鼠的药动学  

Pharmacokinetics of oral antitumor drug satraplatin in rats

作　　者：李文钧[1] 彭小英[1] 马张英[2] 郑永兴[1] 

机构地区：[1]浙江省医学科学院药物研究所,杭州浙江310013 [2]浙江大学医学院附属邵逸夫医院,杭州浙江310016

出　　处：《中国新药与临床杂志》2004年第8期528-530,共3页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：目的 :观察口服抗肿瘤药赛特铂(satraplatin)在大鼠的药动学。方法 :石墨炉原子吸收分光法测定体内赛特铂的总铂浓度。结果 :剂量为 5 0mg·kg- 1和 10 0mg·kg- 1时 ,主要药动学参数分别为 :T12 β(4 3±s 34)h和 (5 8± 38)h ,Tmax(5 .0± 2 .0 )h和 (6 .0± 1.0 )h ,Cmax(12 .6± 2 .5 )mg·L- 1和 (13.4± 1.5 )mg·L- 1,AUC0 ∞(4 2 2± 12 0 )mg·h·L- 1和 (70 2± 118)mg·h·L- 1。组织分布以肝、肾最高。 4 8h后药物排出已基本完成 ,主要经粪便排出 ,约 5 5 % ,尿排出小于 6 % ,2 4h胆中排出0 .2 3%。结论 :赛特铂的药时曲线为口服一级吸收2室模型。AIM: To evaluate the pharmacokinetics of satraplatin in rats. METHODS: The drug concentration in plasma,tissues,bile,urine and feces of rats was determined by flameless atomic absorption spectrophotometry. RESULTS: The main pharmacokinetic parameters of satraplatin were: T __ 12β (43± s 34) h and (58±38) h,T _ max (5±2) h and (6±1) h,C _ max (12.6±2.5) mg·L -1 and (13.4±1.5) mg·L -1 ,AUC_ 0-∞ (422±120) mg·h·L -1 and (702±118) mg·h·L -1 for dose of 50 mg·kg -1 and 100 mg·kg -1 , respectively. The distribution process of drug to tissues was quite quicker,liver and kidney had the levels of 15-20 mg·kg -1 ,much higher than the levels of 1-5 mg·kg -1 in other tissues. More than 55 % of the drug was excreted in feces,less than 6 % in urine,0.2 % in bile. CONCLUSION: The drug concentration-time profiles of satraplatin in rats fitted to two compartment modes and show some properties of unlinear pharmacokinetics after oral administration.

关 键 词：抗肿瘤药 大鼠 药动学 赛特铂 

分 类 号：R979.1[医药卫生—药品] R969.1[医药卫生—药学]