Yang Fang, Sun Long-Ji, Yang Fan, Li Shi-Hao, Chen Yu-Xin, Wang Wen-Rui
College of Animal Science and Technology, Henan University of Science and Technology, Luoyang, China.
J Vet Pharmacol Ther. 2025 Jan;48(1):30-36. doi: 10.1111/jvp.13478. Epub 2024 Aug 16.
The objective of this study was to determine the pharmacokinetics of enrofloxacin and its metabolite, ciprofloxacin, in Nanyang cattle after a single intravenous (IV), and intramuscular (IM) administration of enrofloxacin at 2.5 mg/kg body weight (BW). Blood samples were collected at predetermined time points. Enrofloxacin and ciprofloxacin concentrations in plasma were simultaneously determined using a high-performance liquid chromatography (HPLC) assay method and subjected to a non-compartmental analysis. After IV administration, enrofloxacin had a mean (±SD) volume of distribution at steady state (V ) of 1.394 ± 0.349 L/kg, a terminal half-life (t ) of 3.592 ± 1.205 h, and a total body clearance (Cl) of 0.675 ± 0.16 L/h/kg. After IM administration, enrofloxacin was absorbed relatively slowly but completely, with a mean absorption time (MAT) of 6.051 ± 1.107 h and a bioavailability of 99.225 ± 7.389%. Both compounds were detected simultaneously in most plasma samples following both routes of administration, indicating efficient biotransformation of enrofloxacin to ciprofloxacin. After IV injection, the peak concentration (C ) of ciprofloxacin was 0.315 ± 0.017 μg/mL, observed at 0.958 ± 0.102 h. Following IM injection, the corresponding values were 0.071 ± 0.006 μg/mL and 3 ± 1.095 h, respectively. Following IV and IM administration, the conversion ratio of enrofloxacin to ciprofloxacin was calculated as 59.2 ± 9.6% and 31.2 ± 7.7%, respectively. The present results demonstrated favorable pharmacokinetic profiles for enrofloxacin, characterized by complete absorption with relatively slow kinetics, extensive distribution, efficient biotransformation to ciprofloxacin, and prolonged elimination in Nanyang cattle.
本研究的目的是在以2.5毫克/千克体重(BW)对南阳牛单次静脉注射(IV)和肌肉注射(IM)恩诺沙星后,测定恩诺沙星及其代谢物环丙沙星的药代动力学。在预定时间点采集血样。使用高效液相色谱(HPLC)测定法同时测定血浆中恩诺沙星和环丙沙星的浓度,并进行非房室分析。静脉注射后,恩诺沙星在稳态时的平均(±标准差)分布容积(V )为1.394±0.349升/千克,终末半衰期(t )为3.592±1.205小时,全身清除率(Cl)为0.675±0.16升/小时/千克。肌肉注射后,恩诺沙星吸收相对缓慢但完全,平均吸收时间(MAT)为6.051±1.107小时,生物利用度为99.225±7.389%。在两种给药途径后的大多数血浆样本中均同时检测到这两种化合物,表明恩诺沙星向环丙沙星的有效生物转化。静脉注射后,环丙沙星的峰浓度(C )为0.315±0.017微克/毫升,在0.958±0.102小时观察到。肌肉注射后,相应的值分别为0.071±0.006微克/毫升和3±1.095小时。静脉注射和肌肉注射后,恩诺沙星向环丙沙星的转化率分别计算为59.2±9.6%和31.2±7.7%。目前的结果表明恩诺沙星具有良好的药代动力学特征,其特点是吸收完全但动力学相对缓慢、分布广泛、向环丙沙星的有效生物转化以及在南阳牛体内消除时间延长。