~3H—藻酸双酯钠的药物动力学研究

A STUDY ON THE PHARMACOKINETICS OF ~3H-POLY SACHARIDE SULPHATE 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％。PSS0.8％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 adsorption,distribution exception and pharmacokinetic parameters of 1H-polysaccharide sulphate(PSS) in mice and rats is reported.The blood concentration time obtained after introvenous injection of 2H-PSS to mice was shown to fit a three-compartment open model,after oral is shown to fit a two-compartment open model.The drug concentration was 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 following iv the total radioactivity excreted in urine and feces was 59.52% and 20.23% of dose,after oral 12h excres in bile was 15.3% in rats.The bioavailability was 75.6%,the drugplasms protin binding of 3H-PSS was found to be 97.6% in human and 98.1% in mice.