H^3-藻酸双酯钠的药物动力学研究

A STUDY ON THE PHARMACOKINETICS OF ~3H-POLY SACCHARIDE SUIPHATE(PSS) IN MICE AND RATS

研究了不同剂量~3H-藻酸双酯钠(PSS)在小鼠及大鼠体内的吸收、分布,排泄及药物代谢动力学参数.无论口服或静注小鼠组织分布较广,12h 以肝、肾最高,脑,脂肪、骨骼较低,大脑、小脑、脑干放射性分布未见明显差异.静注72h 自小鼠尿排泄60%,粪排泄20%.大鼠口服24h 由胆汁排泄15.3%.小鼠及人血血浆蛋白结合率24h 为98%.PSS 0.8%CMC 混悬液口服的绝对生物利用度为75.6%,具有吸收好,分布广,排泄快等特点.

A study on absorption,distribution excertion and pharmaco- kinetic parameters of ~3H-poly saccharide suiphate(PSS) in mice and rats is reported.The blood concentration-time obtained after introvenous injection of ~3H-PSS to mice is shown to fit a tree-comparment open model,after oral is shown to fit a two-compartment open model.The drug concentration is found to be highest in liver and kidney,moderate in lung,spleen,intestine, stomach,heart,muscle and lower in bone,brain and fat.Within 72h follow- ing iv the total radioactivity excreted in urine and feces is 59.52% and 20.23% of dose,after oral 12h excred in bile is 15.3% in rats.The bioava- liability is 75.6%,the drug-plasms protin binding of ~3H-PSS is found to be 97.6% in human and 98.1% in mice.