Corum Orhan, Yildiz Ramazan, Ider Merve, Altan Feray, Ok Mahmut, Uney Kamil
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Kastamonu, Kastamonu, Turkey.
Department of Internal Medicine, Faculty of Veterinary Medicine, University of Mehmet Akif Ersoy, Burdur, Turkey.
J Vet Pharmacol Ther. 2019 Nov;42(6):632-639. doi: 10.1111/jvp.12789. Epub 2019 Jun 14.
The aim of this study was to evaluate the pharmacokinetics and bioavailability of cefquinome (CFQ) and ceftriaxone (CTX) following intravenous (IV) and intramuscular (IM) administrations in premature calves. Using a parallel design, 24 premature calves were randomly divided into the two antibiotic groups. Each of the six animals in the first group received CFQ (2 mg/kg) through IV or IM administration. The second group received CTX (20 mg/kg) via the same administration route. Plasma concentrations of the drugs were analyzed by high-performance liquid chromatography and noncompartmental methods. Mean pharmacokinetic parameters of CFQ and CTX following IV administration were as follows: elimination half-life (t ) 1.85 and 3.31 hr, area under the plasma concentration-time curve (AUC ) 15.74 and 174 hr * μg/ml, volume of distribution at steady-state 0.37 and 0.45 L/kg, and total body clearance 0.13 and 0.12 L hr kg , respectively. Mean pharmacokinetic parameters of CFQ and CTX after IM injection were as follows: peak concentration 4.56 and 25.04 μg/ml, time to reach peak concentration 1 and 1.5 hr, t 4.74 and 3.62 hr, and AUC 22.75 and 147 hr * μg/ml, respectively. The bioavailability of CFQ and CTX after IM injection was 141% and 79%, respectively. IM administration of CFQ (2 mg/kg) and CTX (20 mg/kg) can be recommended at 12-hr interval for treating infections caused by susceptible bacteria, with minimum inhibitory concentration values of ≤0.5 and ≤4 μg/ml, respectively, in premature calves. However, further research is indicated to assess the pharmacokinetic parameters following multiple doses of the drug in premature calves.
本研究的目的是评估在早产犊牛中静脉注射（IV）和肌肉注射（IM）头孢喹肟（CFQ）和头孢曲松（CTX）后的药代动力学和生物利用度。采用平行设计，将24头早产犊牛随机分为两个抗生素组。第一组的六只动物分别通过静脉注射或肌肉注射接受CFQ（2mg/kg）。第二组通过相同的给药途径接受CTX（20mg/kg）。通过高效液相色谱法和非房室方法分析药物的血浆浓度。静脉注射后CFQ和CTX的平均药代动力学参数如下：消除半衰期（t）分别为1.85和3.31小时，血浆浓度-时间曲线下面积（AUC）分别为15.74和174小时μg/ml，稳态分布容积分别为0.37和0.45L/kg，全身清除率分别为0.13和0.12L·小时-1·kg-1。肌肉注射后CFQ和CTX的平均药代动力学参数如下：峰值浓度分别为4.56和25.04μg/ml，达到峰值浓度的时间分别为1和1.5小时，t分别为4.74和3.62小时，AUC分别为分别为22.75和147小时μg/ml。肌肉注射后CFQ和CTX的生物利用度分别为141%和79%。对于治疗由敏感细菌引起的感染，建议在早产犊牛中以≤0.5和≤4μg/ml的最低抑菌浓度值分别以12小时间隔肌肉注射CFQ（2mg/kg）和CTX（20mg/kg）。然而，需要进一步研究以评估在早产犊牛中多次给药后的药代动力学参数。
