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目的 研究新型重组人肿瘤坏死因子 (nrh TNFα)在小鼠体内的药代动力学 .方法 采用 1 2 5I标记的 nrh TNFα同位素法 ,观察 im和 iv后的体内过程 .结果 按 10 ,2 0和 4 0μg· kg- 1 3个剂量给小鼠 im nrh TNFα后在 1～ 2 h达到峰浓度 ,总放射性在体内消除较快 ,t1 / 2 为 4 .7～ 6 .5 h,所得结果均证明 Cmax和 AU C与剂量呈显著相关 (r=0 .95 ) ,与 iv给药 (10μg· kg- 1 )的血药浓度进行绝对生物利用度试验 ,其 im给药生物利用度为 0 .80 3.nrh TNFα在体内的分布以肾含量最高 ,脑浓度最低 ,但都低于同时间的血药浓度 .按 10 μg·kg- 1 im给药后 ,用 RA法测定尿和粪 2 4 h放射性总量 ,尿中放射性回收率为 86 .8% ,粪中回收率为 9.5 % ,总排泄量达给药剂量的 96 .3% .结论 nrh TNFα在小鼠的体内代动力学符合二室模型
Objective To study the pharmacokinetics of a novel recombinant human tumor necrosis factor (TNFα) in mice.Methods The in vivo process after im and iv was observed by the method of nrh TNFα isotope labeled with 125I.RESULTS: The results showed that the total radioactivity disappeared rapidly in vivo when the dose of 4 μg · kg -1 was given to im nrh TNFα mice at 1 ~ 2 h and the t1 / 2 was 4.7 ~ 6.5 h Cmax and AU C were significantly correlated with the dose (r = 0.95), and the absolute bioavailability of plasma drug concentration of iv (10μg · kg-1) was tested with bioavailability of 0.80 3.nrh TNFα distribution in the body with the highest content of the kidney, the brain concentration lowest, but lower than the same time plasma concentration.After administration of 10 μg · kg-1 im, RA and determination of urine and faeces 2 4 h The total radioactivity was 86.8% in urine, 9.5% in feces, and 96.3% in total excretion.Conclusion The in vivo kinetics of nrh TNFα in mice is in accordance with the second compartment model