摘要
荷S_(180)肉瘤小鼠iv[~3H]CMCa后,血药-时曲线呈二相指数函数关系,符合开放型二室模型,并计算了各药代动力学参数。其t_(1/2)α=9min38s,结果表明药物从中央室向周边室分布极为迅速;半减期(t_(1/2)β=37h)较长;该药在肿瘤内含量最高,代谢速率也最慢。此药有浓集于肿瘤的作用;在服内含量低,降低了神经的毒副作用;其在血液和肌肉内代谢速率较快,有利于临床诊治肿瘤使用。药后24h尿液经TLC分析和液闪测定结果,表明约占尿总放射性的80％呈原形药排出,并有7％以其水解产物灭滴灵排出。上述结果基本与该药在正常小鼠体内代谢相似。
The blood radioactivity-time curve after iv [3H] CMCa in S180 bearing mice was found to be diexponential model.Pharmacokinetic parameters; t1/2 α=9.6min, t1/2 P=37 h.It was quite rapidly distributed from the central compartment to the peripheral compartment.The highest radioactivity and the slowest metabolic rate were found in tumor.It further confirmed our foregoing result that this drug could concentrate in tumor,and was lower in brain with decreased neurotoxicity.The metabolic rates of the drug in blood and muscle were quite rapid, indicating it might be useful for clinical diagnosis and therapy of tumor.The results analyzed by TLC and scintillation counting of urine taken 24 h after iv [3H] CMCa to S180 bearing mice indicated that approximately 80% of urine total radioactivity was excreted as original drug in unchanged form and 7% as its hydrolyzate metronidazol.These results were similar to those in normal mice.
出处
《第二军医大学学报》
CAS
CSCD
北大核心
1989年第2期115-118,共4页
Academic Journal of Second Military Medical University
基金
国家自然科学基金
关键词
甲硝唑氨酸
肿瘤
药物代谢
灭滴灵
[3~H]CMCa
metronidazole
sarcoma 180
tissue distribution
drug metabolism
