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目的:比较半乳糖化重组人生长激素(Gal-rhGH)和重组人生长激素(rhGH)在小鼠体内的药物动力学特征.方法:用~(125)I标记Gal-rhGH和rhGH,通过小鼠尾静脉iv,测定血和肝中相对放射性随时间的变化,以3P87药物动力学程序进行模型拟合和参数求算.结果:~(125)I-rhGH-Gal在血中的相对放射性呈现双峰,其体内药物动力学特征与~(125)I-rhGH明显不同,进一步证实了Gal-rhGH的肝靶向性.结论:以放射性同位素标记示踪法成功比较了Gal-rhGH和rhGH的药物动力学特征.
Objective: To compare the pharmacokinetics of Gal-rhGH and recombinant human growth hormone (rhGH) in mice.Methods: Gal-rhGH and rhGH were labeled with ~ (125) I, The rat tail vein iv was used to determine the changes of relative radioactivity in blood and liver over time, and the model fitting and parameter calculation were performed by the 3P87 pharmacokinetic program.Results: The relative radioactivity of ~ (125) I-rhGH-Gal in blood appeared The bimodal pharmacokinetic characteristics in vivo were significantly different from those of ~ (125) I-rhGH, which further confirmed the liver targeting of Gal-rhGH.Conclusion: The results of Gal-rhGH and rhGH were successfully compared by radioisotope labeling Pharmacokinetic characteristics.