代谢
在雄性Sprague-Dawley大鼠和两种性别恒河猴单次肌肉注射随机三氚标记的硫化羟钴胺酸盐后,血液和组织中达到峰值水平的时间大约在给药后30-60分钟,所用剂量是人类治疗推荐范围(3毫克/千克体重)之内。除了在大鼠肝脏中迅速转化为羟钴胺磺氧化物,在猴子的肝脏中转化为N-脱乙基代谢物之外,血液和组织中发现了未改变的药物。
In male Sprague-Dawley rats and in rhesus monkeys of both sexes receiving single im injections of randomly tritiated hycanthone mesylate at doses in the range of those therapeutically recommended for man (3 mg/kg bw), peak blood and tissue levels were found about 30-60 minutes after administration. ... Unchanged drug was found in blood and tissues, except in the liver where rapid conversion to hycanthone sulphoxide occured in rats and to the N-de-ethylated metabolite in monkeys.
来源:Hazardous Substances Data Bank (HSDB)