Mathur P P, Smyth R D
Res Commun Chem Pathol Pharmacol. 1979 Jul;25(1):23-31.
The physiologic disposition and subcellular tissue localization of 14C-fenclorac was studied in rats receiving single and multiple oral doses of the drug. The drug was primarily excreted via renal and fecal routes. The 24-hour urinary and fecal elimination rates were 41 and 17% respectively, of the administered dose. The daily elimination rates of drug/drug metabolites were not altered when the treatment period was extended to seven days, suggesting that the processes for the renal and fecal clearance of drug were not affected by this treatment schedule. Studies on the distribution of 14C-fenclorac in slected tissues revealed that hepatic, renal and splenic tissue to plasma ratio of the label twenty-four hours after a single dose was 1.53, 3.88 and 0.11, respectively. Similar results were observed in rats receiving multiple doses of 14C-fenclorac. The 14C-label was distributed throughout the subcellular organelles with the highest concentration in the cytosol and lower levels in the mitochondria and microsomes. Furthermore, these experiments demonstrated that both metabolic (hepatic) and excretory (kidney) organs do not accumulate fenclorac in animals receiving the drug up to seven days.
在接受单次和多次口服剂量该药物的大鼠中，研究了14C-芬氯那酸的生理处置及亚细胞组织定位。该药物主要通过肾脏和粪便途径排泄。给药剂量的24小时尿液和粪便消除率分别为41%和17%。当治疗期延长至7天时，药物/药物代谢物的每日消除率未改变，这表明该治疗方案不影响药物经肾脏和粪便清除的过程。对14C-芬氯那酸在选定组织中的分布研究表明，单次给药24小时后，肝脏、肾脏和脾脏组织与血浆的标记物比值分别为1.53、3.88和0.11。在接受多次剂量14C-芬氯那酸的大鼠中也观察到了类似结果。14C标记物分布于整个亚细胞细胞器中，胞质溶胶中浓度最高，线粒体和微粒体中浓度较低。此外，这些实验表明，在接受该药物长达7天的动物中，代谢（肝脏）和排泄（肾脏）器官均不会蓄积芬氯那酸。
