[1-~(14)C]-已酰乙醛亚硫酸氢钠在小鼠体内的药代动力学研究

用巳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4小时后大部分组织的放射性分布广泛,给药4小时后大部分组织的放射性巳降至较低水平,瘤组织的放射性分布较低,血清、尿和肝肾组织匀浆薄层层析(TLC)实验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3小时从呼吸道以~(14)CO_2形式和24小时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％.

THE PHARMACOKINETIC STUDIES OF THE [1-~(14)C]-HAXANOYL ALDEHYDE SODIUM BISULFITE IN THE MOUSE

Haxanoyl aldehyde sodium bisulfite (HASB) was synthesized by the department of chemistry, Sun Yat-Sen University of Medical Sciences. It is an analogue of Houttuynium (Decanoyl Acetalde-hyde). The results of pharmacoklnetic research of C14 -HASB showed that the logarithm of drug concentration in blood versus time curve after intravenous administration was fitted to a two - compartment open model with first order elimination. In the distribution studies the results revealed that radioactivity distributed widely in the body. The concentrations in the liver and kidney were markedly higher than those in the blood and other tissues at 2 and 24 hour time points studied. Except for kidney and liver, radioactivity in tissues observed decreased to quite low levels 4 hours after administration ; the levels of radioactivity in the tumor were comparatively low. Thin layer chromatographic (TLC) analyses of serum urine and homogenates of liver and kidney indicated that most of radioactivity in serum was in the form unchanged C14 - HASB and that the drug could be metabolized rapidly after pass-Ing into some tissue cells in vivo. In excretion studies, the major routes of elimination were found to be via the expiration with 26. 76 % of the C14 as carbon dioxide recovered in 3 hours and via urine with 14. 60% of the C14mainly in the form of metabolites recovered in 24 hours.