摘要
本文采用高压液相分析法分别测定了氟脲嘧啶(5-FU) 快速静脉滴注,灌胃及灌肠给药后消化道肿瘤患者门静脉(Portal)和末梢静脉(Systemic)血中的药物浓度和癌组织、正常组织、淋巴结及脂肪组织中的药物浓度,并对5-FU的体内动力学参数进行了计算。结果表明5-FU体内动力学呈二室开放模型,血中消除半衰期t1/2(β)por=11.5min,t1/2(β)sys=13.6min. 灌胃给药显示5-FU在门静脉中的血药浓度明显高于末梢静脉。肝对5-FU的提取率达76%,说明5-FU口服给药后将有较多的药物首先进入到肝脏,提示此种给药途径对于治疗肝癌和消化道癌肝转移可能为简便有效的途径之一。并能减少5-FU的毒性,灌肠给药门静脉和末梢静脉血药浓度都很低,二者浓度没有显著差异。组织浓度测定结果表明三种途径给药后,5-FU在脂肪组织中的分布均很少,相同时间5-FU在癌组织中的浓度明显高于癌旁正常组织,虽然灌胃及灌肠给药没有出现象静脉给药那么高的血药浓度,但5-FU在淋巴结及癌组织中的分布并不低于静脉给药。
The concentrations of 5-FU in portal and systemic blood andin cancer tissue, normal tissue, adipose tissue as well as lymph nodes weredetermined by HPLC method after administration by rapid intravenousinfusion or by oral or rectal route. The pharmacokinetic parameters throughrapid intravenous infusion were calculated and fitted a two-compartmentopen model. The half life of elimination were 11 .5 min in portal and 13.6min in systemic blood respectively. After oral administration, the concentration of 5-FU in portal blood wassignificantly higher than that in systemic blood, The hepatic extraction ratio was 76% This result showed that more 5-FU in portal and systemicblood were low and no significant difference observed. The result of concentrations of 5-FU in various tissues after threeroutes of administration showed that the distribution of 5-FU was low inadipose tissue. The concentrations of 5-FU in cancer tissues were higherthan that in normal tissues at the same time. Although the blood concentration of 5-FU after oral and rectal admini-stration was not as high as that after intravenous infection the concentrationsof 5-FU in lymph nodes and cancer tissues after oral and rectal administra-tion were not lower than that after rapid intravenous infusion.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1990年第2期92-99,共8页
The Chinese Journal of Clinical Pharmacology
关键词
氟脲嘧啶
药代动力学
给药途径
5-fluorouracil
pharmacokinetics
portal vein
systemic vein
cancer
lymph node
