Taylor A, King L J, Marks V
Xenobiotica. 1985 Mar;15(3):221-6. doi: 10.3109/00498258509045352.
In rats injected intramuscularly with sodium aurothio[1,4-14C]malate, 80% of the 14C was excreted in the urine, mostly in 24 h, 2% in the faeces and 10% as 14CO2 in the expired air during the first six hours with none thereafter. Urinary and faecal gold represented 5% and 2.5% of the dose, respectively. In rats given thio[1,4-14C]malic acid, 50% of the 14C was excreted in the urine, 10% in the expired air as 14CO2 and 2% in the faeces. Radioactivity was found in all tissues with distribution similar for the two compounds, the major sites of accumulation being bone, kidney and liver. Significantly higher amounts of 14C were found in the 14C-aurothiomalate-dosed animals, notably in bone and kidney. Gold was located principally in kidney, liver, lung and spleen with smaller amounts elsewhere. At least seven radioactive metabolites (including sodium aurothiomalate and thiomalic acid) were present in the urine of rats given 14C-aurothiomalate. Urine from 14C-thiomalic acid-treated rats contained at least five radiolabelled compounds, one of which was thiomalic acid. Results show that most of the gold was removed from the thiomalate moiety, however, the 14C distribution and the radioactive metabolites in urine demonstrated that some intact aurothiomalate remains.
给大鼠肌肉注射硫代苹果酸金钠[1,4 - 14C]后,14C的80%经尿液排出,大部分在24小时内排出,2%经粪便排出,在最初6小时内有10%以14CO2形式经呼出气体排出,之后不再有。尿金和粪金分别占给药剂量的5%和2.5%。给大鼠注射硫代[1,4 - 14C]苹果酸后,14C的50%经尿液排出,10%以14CO2形式经呼出气体排出,2%经粪便排出。在所有组织中均发现有放射性,两种化合物的分布相似,主要蓄积部位为骨骼、肾脏和肝脏。在注射14C - 硫代苹果酸金钠的动物中发现14C的含量显著更高,尤其是在骨骼和肾脏中。金主要分布在肾脏、肝脏、肺和脾脏,其他部位含量较少。给注射14C - 硫代苹果酸金钠的大鼠的尿液中至少存在七种放射性代谢物(包括硫代苹果酸金钠和硫代苹果酸)。注射14C - 硫代苹果酸的大鼠的尿液中至少含有五种放射性标记化合物,其中一种是硫代苹果酸。结果表明,大部分金从硫代苹果酸部分去除,然而,14C的分布和尿液中的放射性代谢物表明仍有一些完整的硫代苹果酸金钠存在。