Toma S, Hirai Y, Sugimoto C, Shoji M, Oguni Y, Morishita S, Ito C, Horie M
Research Laboratories of Kyushin Pharmaceutical Co., Ltd., Tokyo, Japan.
Yakugaku Zasshi. 1991 Nov;111(11):676-86. doi: 10.1248/yakushi1947.111.11_676.
In an attempt to evaluate the metabolic fate of "Kyushin", which is a traditional medicine containing Toad venom, a 3H-labeled compound of bufalin, which is one of the main active components, has been synthesized. The metabolic fate of the 3H-bufalin was studied after its single and repeated oral administration in rats. After a single administration of the 3H-bufalin (20 micrograms/kg), the radioactivity in the blood reached a maximum level at 15 min. The radioactivity in the blood declined in a triphasic manner with half-life times of 18 min, 2.6 and 86 h. Within 24 h after the single administration, the excretion of the radioactivity into the urine and feces amounted to 1.3% and 81% of the administered dose, respectively. Tissue radioactivity was higher in the stomach, small intestine, liver, lung, kidney and pancreas, while the radioactivity in other tissues was lower than that in blood. Radioactivity disappeared rapidly from any tissues. In case of repeated administration for 14 d, the disposition of radioactivity was almost same as the result after a single dosing, and radioactivity scarcely remained in any tissues after the last administration.
为了评估含有蟾蜍毒液的传统药物“救心”的代谢命运，已合成了一种主要活性成分之一蟾毒灵的3H标记化合物。在大鼠单次和重复口服3H-蟾毒灵后，研究了其代谢命运。单次给予3H-蟾毒灵（20微克/千克）后，血液中的放射性在15分钟时达到最高水平。血液中的放射性以三相方式下降，半衰期分别为18分钟、2.6小时和86小时。单次给药后24小时内，放射性进入尿液和粪便的排泄量分别占给药剂量的1.3%和81%。胃、小肠、肝脏、肺、肾脏和胰腺中的组织放射性较高，而其他组织中的放射性低于血液中的放射性。放射性从任何组织中迅速消失。在重复给药14天的情况下，放射性的处置与单次给药后的结果几乎相同，最后一次给药后几乎没有放射性残留在任何组织中。
