Vergin H, Strobel K
Eur J Drug Metab Pharmacokinet. 1982;7(3):197-202. doi: 10.1007/BF03189566.
The pharmacokinetics and metabolism of the newly developed antibacterial tetroxoprim (TXP) were investigated in four male beagle dogs using a 2-(14C)-labelled drug. TXP was administered intravenously and orally at doses of 5 mg/kg bodyweight. Counting of the total 14C-radioactivity shows that the drug was absorbed completely and eliminated almost exclusively by the kidneys. The quantitative absorption of TXP from the canine gastro-intestinal tract was ascertained by comparison of the AUC-values and the renal recoveries of unchanged drug following i.v. and oral dosage. The terminal half-lives of non-metabolized compound in plasma were 4.64 and 4.83 for i.v. and oral dosing respectively. Following either i.v. or oral TXP administration, the major route of excretion was renal elimination of the compound as its major metabolite U-1 (81-82.2% of dose) and as unchanged mother substance (11.4-12.3% of dose).
使用一种2-(14C)标记的药物，在四只雄性比格犬中研究了新开发的抗菌药物四氧普明（TXP）的药代动力学和代谢情况。TXP以5mg/kg体重的剂量静脉注射和口服给药。对总14C放射性进行计数表明，该药物被完全吸收，几乎完全通过肾脏消除。通过比较静脉注射和口服给药后AUC值以及未变化药物的肾脏回收率，确定了TXP从犬胃肠道的定量吸收情况。静脉注射和口服给药后，血浆中非代谢化合物的终末半衰期分别为4.64和4.83。静脉注射或口服TXP后，排泄的主要途径是肾脏消除该化合物，以其主要代谢物U-1（占剂量的81-82.2%）和未变化的母体物质（占剂量的11.4-12.3%）的形式排出。
