CAJ | 학술논문

测定R-hap在健康Wistar大鼠体内的组织分布,排泄及药动学参数.R-hap采用IODO-GEN标记,测定单次推注给药后125-ⅠR-hap的组织分布,尿、粪及胆汁的排泄情况.125Ⅰ-R-hap药动学参数也是在单次推注给药后测定.R-hap在体内广泛分布,在大部分器官中快速消除.其中.肾的含量最高,脂肪的含量最低.累计排泄率为71.81%±2.15%(48小时)及94.71%±1.50%(120小时).经尿排泄为主要的排泄途径,给药后120小时,尿及粪的累计排泄率分别为80.64%±1.47%,14.07%±0.95%.平均给药时曲线下面积为(8818.4±576.1)Bq/h/mL.R-hap的组织分布,排泄及药动学参数的结果为未来的临床试验设计提供了参考依据.
측정R-hap재건강Wistar대서체내적조직분포,배설급약동학삼수.R-hap채용IODO-GEN표기,측정단차추주급약후125-ⅠR-hap적조직분포,뇨、분급담즙적배설정황.125Ⅰ-R-hap약동학삼수야시재단차추주급약후측정.R-hap재체내엄범분포,재대부분기관중쾌속소제.기중.신적함량최고,지방적함량최저.루계배설솔위71.81%±2.15%(48소시)급94.71%±1.50%(120소시).경뇨배설위주요적배설도경,급약후120소시,뇨급분적루계배설솔분별위80.64%±1.47%,14.07%±0.95%.평균급약시곡선하면적위(8818.4±576.1)Bq/h/mL.R-hap적조직분포,배설급약동학삼수적결과위미래적림상시험설계제공료삼고의거.
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 excre- tion 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 trichloroaeetic acid (TCA) precipitated radioactivity was widely dis- trihuted and rapidly 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 dis- tribution, excretion and phaxmacokinetics of R-hap in rats provided biopharmaceutical basis for the design of future clinical trials.