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恩诺沙星及其代谢产物环丙沙星在南阳牛体内的药代动力学

Pharmacokinetics of Enrofloxacin and Its Metabolite Ciprofloxacin in Nanyang Cattle.

作者信息

Yang Fang, Sun Long-Ji, Yang Fan, Li Shi-Hao, Chen Yu-Xin, Wang Wen-Rui

机构信息

College of Animal Science and Technology, Henan University of Science and Technology, Luoyang, China.

出版信息

J Vet Pharmacol Ther. 2025 Jan;48(1):30-36. doi: 10.1111/jvp.13478. Epub 2024 Aug 16.

Abstract

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.

摘要

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。

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