9-硝基喜树碱单次灌胃给药后大鼠体内的分布与排泄  

Disposition of 9-nitrocamptothecin after sigle oral dose in rats

作　　者：张春燕[1] 殷琦[2] 李玉珍[1] 李长龄[3] 

机构地区：[1]北京大学人民医院药剂科,北京100044 [2]卫生部北京医院药剂科,北京100730 [3]北京大学药学院药理系,北京100083

出　　处：《中国新药杂志》2006年第3期193-196,共4页Chinese Journal of New Drugs

摘　　要：目的:建立测定生物样品中9-硝基喜树碱的反相高效液相色谱法,研究其在大鼠体内处置的规律及特点。方法:SD大鼠单次灌胃9-硝基喜树碱3．0 mg·kg^(-1)后摘取组织,收集粪、尿、胆汁,用HPLC方法测定药物浓度,计算累积排泄率。结果:9-硝基喜树碱单次灌胃后在各组织广泛分布,24h内原形药从尿及粪中排泄量24066．3ng,占给药量的1．814%,给药后12h原形药从胆汁中排泄13253．7ng,占给药量的1．62%。结论:9-硝基喜树碱原形药累积排泄率约为3．43%,可能主要以代谢物形式排出体外。Objective：To investigate the disposition of 9-nitrocamptothecin in rats. Methods：Following after a single oral dose of 9-nitrocamptothecin （3.0 mg·kg^-1 ） to SD rats, the feces and urine of the rats were collected. Subsequently, the rats were euthanized to collect tissues and bile. The concentrations of 9-nitrocamptothecin were measured by HPLC, followed by the calculation of the accumulate excretion ratio of 9-nitrocamptothecin. Results：The 9-nitrocamptothecin distributed all tissues wide after oral administration. The urine and feces excretion ratio of the raw 9-nitrocamptothecin was 1. 814% in 24 hours, and bile excretion ratio was 1.62% in 12 hours. Conclusion ：The accumulate excretion ratio of the raw 9-nitrocamptothecin is about 3.43% ,so 9-nitrocamptothecin is eliminated mainly by its metabolites.

关 键 词：9-硝基喜树碱 大鼠 处置 

分 类 号：R965.1[医药卫生—药理学] R979.1[医药卫生—药学]