Davison C, Scrime M, Edelson J
Arch Int Pharmacodyn Ther. 1977 Nov;230(1):4-18.
The rate of excretion of labelled hycanthone has been determined in bile and urine from three strains of rats (Sprague-Dawley, hooded and Gunn), and from dogs, cats, rabbits and monkeys. Bile was the major route of excretion in all species; the half-life for excretion of total radioactivity ranged from 1.6 to 3.0 hours. Relatively little of the radioactivity was found in the urine, except in the monkey and notably in the cat. Most of the radioactivity in the bile and urine was found in conjugated form, or as polar metabolites; cat urine, however contained a high percentage of hycanthone and less polar metabolites. Some fifteen metabolites have been seen in bile, and/or urine, and nine from in vitro incubations with microsomal preparations. Five of these, including hycanthone, have been chemically characterized, and two others tentatively identified.
已测定了三种品系大鼠(斯普拉格-道利大鼠、带帽大鼠和冈恩大鼠)以及狗、猫、兔和猴的胆汁和尿液中标记海恩酮的排泄率。胆汁是所有物种的主要排泄途径;总放射性排泄的半衰期为1.6至3.0小时。除了猴,尤其是猫,尿液中发现的放射性相对较少。胆汁和尿液中的大部分放射性以结合形式或极性代谢物形式存在;然而,猫尿中含有高比例的海恩酮和极性较小的代谢物。在胆汁和/或尿液中已发现约十五种代谢物,在与微粒体制剂的体外温育中发现了九种。其中五种,包括海恩酮,已进行了化学表征,另外两种已初步鉴定。