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恩诺沙星/甲氧苄啶组合在大鼠单剂量腹腔注射和口服给药后的药代动力学相互作用

Pharmacokinetic interaction of enrofloxacin/trimethoprim combination following single-dose intraperitoneal and oral administration in rats.

作者信息

Choi Myung-Jin, Yohannes Sileshi Belew, Lee Seung-Jin, Damte Dereje, Kim Jong-Choon, Suh Joo-Won, Park Seung-Chun

机构信息

Veterinary Clinical Pharmacology Laboratory, College of Veterinary Medicine, Kyungpook National University, Daegu, 702-701, South Korea.

出版信息

Eur J Drug Metab Pharmacokinet. 2014 Mar;39(1):11-6. doi: 10.1007/s13318-013-0142-0. Epub 2013 Jun 8.

DOI:10.1007/s13318-013-0142-0
PMID:23749586
Abstract

The pharmacokinetic interaction of enrofloxacin and trimethoprim was evaluated after single-dose intraperitoneal or oral co-administration in rats. Plasma concentrations of the two drugs were determined by high-performance liquid chromatography. Following intraperitoneal combination, a significant (P < 0.05) increase in mean values of plasma half-life (t 1/2) and maximum plasma concentration (C max) was observed for enrofloxacin and trimethoprim, respectively. There was a significant (P < 0.05) increase in mean values of area under the plasma drug concentration versus time from time zero to infinity (AUC0-∞) and C max between combined oral doses (10, 30 and 100 mg/kg) of both antibacterial drugs. Also, after oral conjugation a significant difference in mean values of MRT0-∞ was observed between lower (10 mg/kg) and higher (100 mg/kg) doses of both drugs. A significant increase in pharmacokinetic parameters of both drugs in combined intraperitoneal and oral doses indicated pharmacokinetic interaction of enrofloxacin and trimethoprim. Further study is recommended in other species of animals.

摘要

在大鼠中单次腹腔内或口服联合给药后,评估了恩诺沙星和甲氧苄啶的药代动力学相互作用。通过高效液相色谱法测定两种药物的血浆浓度。腹腔内联合给药后,恩诺沙星和甲氧苄啶的血浆半衰期(t1/2)和最大血浆浓度(Cmax)平均值分别显著(P < 0.05)增加。两种抗菌药物联合口服剂量(10、30和100 mg/kg)之间,血浆药物浓度-时间曲线下面积从时间零至无穷大(AUC0-∞)和Cmax的平均值显著(P < 0.05)增加。此外,口服联合给药后,两种药物较低剂量(10 mg/kg)和较高剂量(100 mg/kg)之间的平均滞留时间(MRT0-∞)平均值存在显著差异。联合腹腔内和口服剂量时两种药物的药代动力学参数显著增加,表明恩诺沙星和甲氧苄啶存在药代动力学相互作用。建议在其他动物物种中进行进一步研究。

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