~3H-米托蒽醌在动物体内的药代动力学研究

A Study on Pharmacokinetics of ~3H-mitoxantrone in Experimental Animals

作者用3H-米托蒽醌给大鼠和小鼠作静脉和肌肉注射。按二室模型计算该药在其体内的药代谢动力学参数。结果表明:该药肌肉注射吸收迅速而完全,组织分布广,以肝脏分布最高,其次,依次为肠、肾、肺、心脏、肌肉及脑。该药排泄缓慢,T1/2为42.56小时。在给药72小时内,从尿中排出约为给药量的7％,主要是该药的代谢产物。从粪便中排出为给药量的43％。

Mitoxantrone (DHAQ) we studied isa new semisynthetic antitumor drug pre-pared in China. This paper reports thepharmacokinetic studies of ~3H--mitoxan-trone in mice by liquid scintillation. Theresults showed that the decline of radioac-tivity in the plasma was a biphasic curveafter intramuscular and intravenous injec-tion in rats. The adsorption of ~3H--DHAQwas ready and complete after intramuscu-lar injection. it was widely distributed inbody tissues. The concentration order ofvarious organs was liver>intestine>kid-ney>lung>heart>muscles>brain.The eli-mination of tho drug was slow, T_(1/2) was42.56 h. In 72 h after administration thecumulative excretion of radioactivity inurine was 7％ of the total dose, while thatin feces was 43％. The main forms of thedrug in urine were its metabolites.