雷公藤甲素在大鼠体内过程的研究

雷公藤甲素具有抗肿瘤、抗炎和免疫抑制作用,能迅速由胃肠道吸收,但并不完全。本实验研究了该药口服和静注给药途径的分布和排泄,结果表明:口服和静注后,药物在体内的分布和消除速率大体相似,均以肝中浓度为最高,依次为脾、肺、肾、肠、心和脑,体内消除较缓慢。血浆蛋白结合率为64.7%。24d内,口服后尿粪总排泄量为给药量的67.5% ,其中粪占52.4%;静注后为61.9%,粪占25%。24h内胆汁排泄为6.73%。提取尿、粪和胆汁经TLC、放射性测定及放射自显影分析,表明以原药排泄为主和部分代谢物。

THE PHYSIOLOGICAL DISPOSITIONS OF TRIPTOLIDE IN RATS

Triptolide possesses antitumor, anti-inflammatory and immuno-supression activity. 3H-triptolide given intragastrically to rats was rapidly but not totally absorbed. After ig and iv administration of 3H-triptolide to rats, the highest radioactivity level was found in the liver, followed by spleen, lung, kidney, intestine, heart and brain. The radioactivity in organs disappeared slowly. 3H-triptolide in plasma was found to be 64.7% bound to plasma protein. In 21d, the cumulative excretion of radioactivity in urine and feces after ig and iv 3H-triptolide to rats was 67.5% and 61.9% of the total dose, respectively. Among that, the radioactivity was 52.4% and 25.3% of the total dose in feces, respectively. The radioactivity excreted by bile in 24h was 6.73 ± 1.9%. The radioactivity in urine, feces and bile measured by TLC, autoradiography and liquid scintillation count indicated that 3H-triptolide excreted in urine, feces and bile was mainly in unchanged form and a few metabolites was found in urine and feces