Tissue distribution,excretion and pharmacokinetics of R-hap in rats

作     者：周佳雨 孟志云 窦桂芳 付守廷 华子春 杨翔 刘军 韦利军 张笋华 Jia-Yu Zhou;Zhi-Yun Meng;Gui-Fang Dou;Shou-Ting Fu;Zi-Chun Hua;Xiang Yang;Jun Liu;Li-Jun Wei;Sun-Hun Zhang

作者机构：沈阳药科大学辽宁沈阳110016 北京输血研究所药物代谢与药代动力学实验室北京100850 南京大学医药生物技术国家重点实验室江苏南京210093 常州千红生化制药有限公司江苏常州213032 

基　　金：National Natural Sciences Foundation of China(Grant No.30371669) National High Technology Research and Development Program of China(863 Program,Grant No.2003AA2Z347B) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2008年第17卷第2期

页      码：106-112页

摘      要：The purpose of this study is to characterize the tissue distribution, excretion and pharmacokinetics profiles of R-hap in healthy Wistar rats. R-hap was radiolabeled by the IODO-GEN method. Tissue distribution and urinary, fecal and biliary excretion patterns of ^125I-R-hap were investigated following a single i.v. bolus injection. Pharmacokinetics properties of ^125I-R-hap were also examined after a single i.v. bolus injection. The trichloroacetic acid （TCA） precipitated radioactivity was widely distributed and rapiclly diminished in most tissues. Kidney contained the highest radioactivity among all organs and the distribution of ^125I-R-hap to fat was minimal. The cumulative excretion of ^125I-R-hap reached 71.81% ± 2.15% of the administered radioactivity at 48 h and 94.71% ± 1.50% at 120 h. Urinary excretion was the dominant route of elimination following i.v. administration, as 80.64% ± 1.47% and 14.07% ± 0.95% of administered radioactivity were recovered in urine and feces, respectively, in intact rats over 120 h. The mean areas under the plasma concentration-time curve was （8818.4 ± 576.1） Bq/h/mL. The results of tissue distribution, excretion and pharmacokinetics of R-hap in rats provided biopharmaceutical basis for the design of future clinical trials.

主 题 词：R-hap Tissue distribution Excretion Pharmacokinetics 

学科分类：1007[医学-药学类] 1006[医学-中西医结合类] 100706[100706] 100602[100602] 10[医学] 

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