[^(14)C]乙双吗啉在小鼠体内的药代动力学研究

The Study of the pharmacokinetics of(^(14)C)bimolane in mice

[^(14)C]乙双吗啉给动物iv后,血中放射性一时间曲线符合二房室开放模型,药代动力学参数T1/2α=0.16±0.03h,T1/2β=15.1±0.7h,生物利用度为87.3±7.7%。给动物ig后,胃肠道吸收较慢,分布广,以胃、肝脏及肺组织中放射性为最高,其次为肠道、食道、肿瘤、淋巴结及皮肤等组织。连续ig 3天后,放射性主要分布在胸腺。48h 内iv自尿排泄为41.7±4.6%,大便排泄为7.5±1.0%;ig后自尿排泄为52.5±3.1%,大便排泄为7.9±0.3%。

After (^(14)C) bimolane had been given intravenously to mice,the decline of rad-ioactivity in the plasma appeared as two-compartment open model. Pharmacokine-tic parameters were T_(1/2)α= 0.16±0.03h, T_(1/2)β= 15.1±0.7 h. Bioavailability was87. 3±7.7%.After ig administration of the medicine,it was absorbed and taken upslowly by various organs in mice but its distribution is wide. The highest radioac-tivity was found in the stomach, the liver and the lung; the radioactivity in the in-testine, the esophagus,the tumor the lymph nodes and the skin took the seco-ndplace. After continuous ig. administration of the medicine for 3 days in mice,the highest radioactivity was found in the thymus. In 48 h, the iv cumulative ex-cretion of radioactivity was 41.7±4.6% of the total dose in urine and 7.5±1.0 % infeces while the ig cumulative excretion of radioactivity was 52.5±3.1% of the totaldose in urine and 7.9±0.3% in feces.