[1-^(14)C]-己酰乙醛亚硫酸氢钠药代动力学研究

A study on the pharmacokinetics of [1-^(14)C]-hexanoyl aldehyde sodium bisulfite (14C-HASB) in mice

用[1-^(14)C]-己酰乙醛亚硫酸氢钠静注给药在小鼠体内作了药代动力学研究。结果表明:血药浓度改变符合开放式二房室模型;体内放射性分布广泛,给药4h后大部分组织的放射性已降至较低水平,瘤组织的放射性分布较低;血清、尿和肝、肾组织匀浆TLC显示大部分血清的放射性来自原形药物,而尿的放射性来自代谢物:肝、肾组织内放射性以代谢物为主,给药3h从呼吸道以^(14)CO_2形式和24h从尿排出的放射性分别占注入放射性总剂量的26.76％和14.60％。

After a single intravenous injection of [1-14C]-hexanoyl aldehyde sodium bisulfite (HASB), the blood radioactivity time course curve fitted well a two-compartment open model. The radioactivity distributed widely in the body, with the concentrations in liver and kidneys markedly higher than in blood and other tissues. Except in kidneys and liver, the radioactivities in tissues decreased to quite low levels 4h after administration. The ra dioactivity in tumors were relatively low. Thin layer chromatographic (TLC) analyses indi-cated that most of radioactivity in serum was in the form of unchanged 14C-HASB and the drug was metabolized rapidly after passing into some tissue cells in vivo. The major routes of elimination were found to be via expiration with 26.76% of the 14C recovered as carbon dioxide in 3h and via urine with 14.6% of the 14C recovered in 24h mainly in the form of metabolites.