[~3H]二甲基左旋筒箭毒碱双氯甲盐(海轮碱Ⅱ)在小鼠体内的药代动力学及整体放射自显影研究

• 作 者: 李水兴 高汝劦 蒋建强 肖玉媛 潘咸新
• 机 构: 上海医药工业研究院,上海医药工业研究院,上海医药工业研究院,上海医药工业研究院,上海医药工业研究院
• 出 处: 核技术
• 发表日期: 1984年02期
• 关键词: 筒箭毒碱 药代动力学 放射自显影 左旋 三室开放模型 药-时曲线 [~3H]海轮碱Ⅰ 内排 代谢产物 肌松作用

615小鼠iV[~3H]海轮碱Ⅱ730μCi/kg,血清药-时曲线呈三项指数函数关系,按三室开放模型计算药代动力学参数,结果表明本品在体内分布非常迅速,但消除较缓慢。给药后2min,组织内放射性以肾为最高,肝、肺、膈肌、心肌、脾、腹肌、肠壁依次递减,脑最低。尿粪内未找到代谢产物。至96h,尿内排出放射性为注入剂量的28.3±4.2％,粪内排出放射性为注入剂量的36.7±6.2％。

The pharmacokinetic parameters of 615 iV [~ 3H] pyritinⅡ730μCi / kg and serum drug-time curve showed three exponential functions. The pharmacokinetic parameters were calculated according to the three-compartment open model. The results showed that the product was very rapidly distributed in the body, slow. 2min after administration, the radioactivity in the tissue was the highest in the kidney, followed by decreasing in the liver, lung, diaphragm, myocardium, spleen, abdominal muscle and intestine, and the lowest in the brain. No metabolites found in the urine. By 96h, the radioactivity in the urine was 28.3 ± 4.2% of the injected dose and that in the feces was 36.7 ± 6.2% of the injected dose.