南阳牛体内恩诺沙星及其代谢物环丙沙星的药代动力学。

IF 1.5 4区 农林科学 Q3 PHARMACOLOGY & PHARMACY
Fang Yang, Long-Ji Sun, Fan Yang, Shi-Hao Li, Yu-Xin Chen, Wen-Rui Wang
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引用次数: 0

摘要

本研究的目的是测定南阳牛在一次静脉注射(IV)和肌肉注射(IM)2.5 毫克/千克体重的恩诺沙星后,恩诺沙星及其代谢物环丙沙星的药代动力学。在预定的时间点采集血液样本。采用高效液相色谱法同时测定血浆中恩诺沙星和环丙沙星的浓度,并进行非室分析。静脉给药后,恩诺沙星的平均(±SD)稳态分布容积(VSS)为 1.394 ± 0.349 L/kg,终末半衰期(t1/2λz)为 3.592 ± 1.205 h,全身清除率(Cl)为 0.675 ± 0.16 L/h/kg。用药后,恩诺沙星的吸收相对缓慢但完全,平均吸收时间(MAT)为 6.051 ± 1.107 h,生物利用度为 99.225 ± 7.389%。两种给药途径后的大多数血浆样本中都能同时检测到这两种化合物,这表明恩诺沙星能有效地生物转化为环丙沙星。静脉注射后,环丙沙星的峰值浓度(Cmax)为 0.315 ± 0.017 μg/mL,观察时间为 0.958 ± 0.102 h;IM 注射后,相应值分别为 0.071 ± 0.006 μg/mL和 3 ± 1.095 h。经计算,静脉注射和注射后,恩诺沙星与环丙沙星的转化率分别为 59.2 ± 9.6% 和 31.2 ± 7.7%。本研究结果表明,恩诺沙星在南阳牛体内具有良好的药代动力学特征,即吸收完全、动力学相对缓慢、分布广泛、高效生物转化为环丙沙星以及消除时间较长。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pharmacokinetics of Enrofloxacin and Its Metabolite Ciprofloxacin in Nanyang Cattle.

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 (VSS) of 1.394 ± 0.349 L/kg, a terminal half-life (t1/2λz) 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 (Cmax) 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.

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来源期刊
CiteScore
3.10
自引率
15.40%
发文量
69
审稿时长
8-16 weeks
期刊介绍: The Journal of Veterinary Pharmacology and Therapeutics (JVPT) is an international journal devoted to the publication of scientific papers in the basic and clinical aspects of veterinary pharmacology and toxicology, whether the study is in vitro, in vivo, ex vivo or in silico. The Journal is a forum for recent scientific information and developments in the discipline of veterinary pharmacology, including toxicology and therapeutics. Studies that are entirely in vitro will not be considered within the scope of JVPT unless the study has direct relevance to the use of the drug (including toxicants and feed additives) in veterinary species, or that it can be clearly demonstrated that a similar outcome would be expected in vivo. These studies should consider approved or widely used veterinary drugs and/or drugs with broad applicability to veterinary species.
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