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重组人甲状旁腺素类似物PTH(1-34)在大鼠体内药动学研究
引用本文:曾勇,姜凌,蔡永明,陈拯民,刘昌孝.重组人甲状旁腺素类似物PTH(1-34)在大鼠体内药动学研究[J].药物评价研究,2010(6):409-412.
作者姓名:曾勇  姜凌  蔡永明  陈拯民  刘昌孝
作者单位:天津药物研究院天津药代动力学与药效动力学省部共建国家重点实验室,天津300193
基金项目:国家科技支撑计划(2007BM141B04)
摘    要:目的:研究大鼠scPTH(1-34)的药动学特征。方法:用125I标记PTH(1-34)示踪法对大鼠scPTH(1-34)后的血清药物浓度进行了测定,并用3P97程序拟和分析并计算药动学参数,采用超滤离心的方法进行药物与血浆蛋白结合率的研究。结果:大鼠scPTH(1-34)10、20和40μg/kg后,药物消除符合一房室模型。平均t1/2ke为(0.92±0.04)h;平均CL为(0.56±0.05)L/(kg.h);Cmax和AUC0-8h均与剂量呈线性正相关,不同剂量药物与血浆蛋白平均结合率为13.4%。结论:大鼠scPTH(1-34)后,药物消除符合线性动力学特征。

关 键 词:重组人甲状旁腺素类似物  125↑I标记  药动学  蛋白结合

In vivo pharmacokinetics of recombinant human parathyroid hormone analogue in rats
ZENG Yong,JIANG Ling,CAI Yong-ming,CHEN Zheng-ming,LIU Chang-xiao.In vivo pharmacokinetics of recombinant human parathyroid hormone analogue in rats[J].Drug Evaluation Research,2010(6):409-412.
Authors:ZENG Yong  JIANG Ling  CAI Yong-ming  CHEN Zheng-ming  LIU Chang-xiao
Institution:(Tianjin State Key Laboratory of Pharmacokinetics and Pharmacodynamics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China)
Abstract:Objective:To study the pharmacokinetic characteristics on parathyroid hormone(PTH,1-34) after sc injection in rats.Methods:Serum drug concentration was measured by 125↑I labeled method after sc injection in rats,the pharmacokinetic model and parameters were fitted and calculated by the 3P97 program.Results:After sc injection at doses of 10,20,and 40 μg/kg in rats,the serum drug concentration-time curve was fitted to a one-compartment model.Mean t1/2ke was(0.92 ± 0.04) h and mean CL was(0.56 ± 0.05) L/(kg·h).The Cmax and AUC0-8 h were positive linear correlation with the dose.Mean binding ratio of various doses drug with plasma protein was 13.4%.Conclusion:After sc injection of PTH(1-34) to rats,the elimination of PTH(1-34) could fit to the linear kinetics.
Keywords:recombinant human parathyroid hormone analogue ( PTH  1-34)  125↑I labled  pharmacokinetics  protein binding
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