125I示踪法研究rhPTH(1~34)在大鼠体内的药代动力学
Study on the Pharmacokinetics of rhPTH1-34 in Sprague-Dawley
Rats by 125I Tracing
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摘要: 采用125I标记重组人甲状旁腺素(1~34)肽(Recombinant Human Parathyroid hormone(1~34),rhPTH(1~34))示踪技术,研究rhPTH(1~34)在SD大鼠体内的药代动力学。结果显示,SD大鼠单次皮下给予1.8和3.6μg/kg剂量的rhPTH1-34后,其主要药代动力学参数为:达峰时间Tmax为0.26±0.07 h和0.25±0.0 h,血浆峰浓度为1.30±0.17 μg/L和3.20±1.12μg/L,末端消除半衰期T1/2el为1.70±0.56 h和1.58±0.70 h,药物浓度-时间曲线下面积AUC(0-∞)为3.1±0.7 μg•h /L和6.7±0.7 μg•h /L。表明大鼠单次皮下给予rhPTH(1~34)后,在给药后大约0.25 h血药浓度达到峰值,随后出现一个较快的消除过程,其药代动力学特征符合非静脉给药线性一房室模型一级动力学。Abstract: 125I tracing method is used to observe the pharmacokinetic parameters of the recombinant human parathyroid hormone (1-34) (rhPTH1-34) in adults Sprague-Dawley rats. The results show that when adults SD rats is given a dosing regimens of 1.8 and 3.6μg/kg rhPTH1-34 by single dose subcutaneous, the main pharmacokinetic parameters of rhPTH1-34 including Tmax, Cmax, T1/2el and AUC is 0.26±0.07h, 0.25±0.0h; 1.30±0.17 μg/L, 3.20±1.12μg/L; 1.70±0.56h, 1.58±0.70h and 3.1±0.7 μg•h /L,6.7±0.7μg•h /L, respectively. It shows that the pharmacokinetic characteristics of rhPTH1-34 in SD rats is accord with linear one-compartment model and eliminate with mono-phase kinetics.