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本文报告~3H-三尖杉酯碱在正常及肿瘤鼠体内的吸收、分布和排泄。静脉注射~3H-三尖杉酯碱后,大鼠血中放射性迅速降低,快、慢两相的生物半衰期分别为3.5分钟和50分钟。给大鼠静脉注射~3H-三尖杉酯硷,注射后15分钟时,药物在各组织中的分布以肾脏为最高,肝、骨髓、肺、心脏、胃肠、脾、肌肉次之,睾丸、血及脑较低。两小时后各组织中的药物浓度均迅速下降,但骨髓的下降较慢,在所有组织中药物浓度居于首位。24小时后则在所测组织中药物浓度均降到相当低的水平。~3H-三尖杉酯碱在肿瘤小鼠体内的分布情况与正常大鼠的分布趋势大致相仿。~3H-三尖杉酯碱在静脉注射后24小时自大鼠体内排出的总放射性,在尿相当于注射剂量的30.2％,在粪相当于16.6％,其中原型药共占14.5％。此外胆汁也是一条重要排泄途径。静脉注射后24小时可自胆汁排出剂量的24.5％,其中原型药占17.1％。该硷口服给药可迅速吸收入血,但吸收不完全。
This article reports ~ 3H-harringtonine absorption, distribution and excretion in normal and tumor mice. After intravenous administration of ~ 3H-harringtonine, the radioactivity in rat blood decreased rapidly, and the biological half-lives of fast and slow phases were 3.5 and 50 minutes, respectively. The rats were intravenously injected with ~ 3H-harringtonine. At 15 minutes after injection, the distribution of the drugs in each tissue was highest in the kidney, followed by the liver, bone marrow, lung, heart, stomach, spleen, muscle, testis Lower blood and brain. Two hours later, the concentration of the drug in each tissue decreased rapidly, but the decline in bone marrow was slower and drug concentration was highest in all tissues. After 24 hours the concentration of the drug in the tested tissue dropped to a very low level. The distribution of ~ 3H-harringtonine in tumor mice is roughly the same as that in normal rats. ~ 3H-harringtonine The total radioactivity discharged from rats 24 hours after intravenous injection was equivalent to 30.2% of the injected dose in urine and 16.6% in feces, with a total of 14.5% of the prototype drug. In addition, bile is also an important excretion route. 24 hours after intravenous injection of bile from the discharge of 24.5%, of which 17.1% of prototype drugs. The base oral administration can quickly absorbed into the blood, but the absorption is not complete.