【摘要】 为测定r -Sak在大鼠体内的药代动力学参数及给药一个剂量后的分布和排泄。用12 5I标记法研究大鼠单剂量静脉注射12 5I -r -Sak的药物动力学参数及体内分布和排泄情况。结果表明 ,12 5I -r-sak按 70 μg/kg及 84 0 μg/kg两种剂量静脉给药后 ,在大鼠体内均可以二室模型拟合。低、高两种剂量的T1/2 (α) 分别为 5 .4 7± 2 .13、8.4 5± 4 .5 0min ,T1/2 ( β) 分别为 96.15± 2 2 .2 9、5 8.78± 3 2 .79min ,AUC分别为 0 .895± 0 .4 5 5、3 8.3 6± 5 .181μg·min·mL- 1,经统计分析 ,T1/2 (α) 、T1/2 ( β) 在两剂量组间无显著性差异 (P >0 .0 5 ) ,AUC随剂量增加而显著增加 (P <0 .0 5 )。12 5I -r -Sak在大鼠体内的分布以肾脏中放射活性为最高 ,其次为血浆、肝脏、肺脏、脾脏、心脏 ,在脑内也有很高浓度。排泄试验表明 ,在给药后 96h ,累计的尿和粪排泄的放射性以及被甲状腺组织富集的放射性碘已近 80 %。更多还原

【Abstract】 The purpose of this work is to measure the pharmacokinetic parameters of r-Sak in rats as well as the biodistribution and the excretion of r-Sak in rats. 125 I-r-Sak was applied for the purpose. The results showed that the pharmacokinetics of 125 I-r-Sak following intravenous injection with two doses (70μg/kg and 840μg/kg) in rats was in correspondence with 2-compartment-model. The T 1/2(α) were 5.47±2.13 and 8.45±4.50min and T 1/2(β) were 96.15±22.29 and 58.78±32.79min for the two dose groups. AUC were 0.895±0.455 and 38.36±5.181μg·min·mL -1 . There were no marked differences of T 1/2(α) and T 1/2(β) between the two dose groups ( P >0.05), but the AUC increased markedly with the dose increase ( P <0.05). The biodistribution of 125 I-r-Sak was wide in rats. Radioactivity was highest in kidney, followed in order by plasma, liver, lung, spleen, heart and brain. Excretion experiment showed that the sum of the accumulative excretion of the radio-material plus the enrichment of the radio-material in thyroid was approximately 80% in 96h.更多还原