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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)I-R-hap的组织分布,尿、粪及胆汁的排泄情况。~(125)I-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。
Tissue distribution, excretion and pharmacokinetic parameters of R-hap in healthy Wistar rats were determined. R-hap was labeled with IODO-GEN to determine tissue distribution, urine, feces and bile excretion of ~ (125) I-R-hap after a single bolus dose. ~ (125) I-R-hap The pharmacokinetic parameters were also determined after a single bolus dose. R-hap is widely distributed in the body and rapidly eliminated in most organs. The highest content of kidney, the lowest fat content. The cumulative excretion rate was 71.81% ± 2.15% (48 hours) and 94.71% ± 1.50% (120 hours). Urinary excretion as the main excretion pathway, 120 hours after administration, excretion rate of urine and excrement were 80.64% ± 1.47%, 14.07% ± 0.95%. The average area under the curve at the time of administration was (8818.4 ± 576.1) Bq / h / mL. R-hap tissue distribution, excretion and pharmacokinetic parameters of the results for the future clinical trial design provides a reference.