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二氟沙星在鸽子体内单次静脉注射、口服和肌肉注射后的药代动力学

Pharmacokinetics of difloxacin after single intravenous, oral and intramuscular administration in pigeons.

作者信息

Jin Yang-Guang, Liu Yue, Zhang Yan-Ni, Chen Yu-Xin, Sun Long-Ji, Li Shi-Hao, Wang Wen-Rui, Yang Fan

机构信息

College of Animal Science and Technology, Henan University of Science and Technology, Luoyang 471023, PR China.

出版信息

Poult Sci. 2025 Feb;104(2):104800. doi: 10.1016/j.psj.2025.104800. Epub 2025 Jan 9.

Abstract

This study aimed to investigate the pharmacokinetics of difloxacin in pigeons following oral (PO), intramuscular (IM), and intravenous (IV) administration. Thirty pigeons were randomly divided into three groups (IM, IV, and PO; n = 10 per group). Difloxacin was administered at 10 mg/kg body weight (BW) via each route. Blood samples were collected at various intervals from 0 to 48 h, and plasma was analyzed for difloxacin concentrations using a validated high-performance liquid chromatography (HPLC) method. Pharmacokinetic parameters were determined using Phoenix software and a non-compartmental analysis (NCA) approach. After PO and IM administration, peak plasma concentrations (C) were observed as 1.81 ± 0.47 and 6.52 ± 1.62 μg/mL, occurring at 2.60 ± 0.97 and 0.63 ± 0.24 h, respectively. Bioavailability (F) was 38.35 % ± 10.45 % for PO and 90.25 % ± 26.14 % for IM administration. Following IV administration, difloxacin was widely distributed, with a volume of distribution (V) of 2.52 ± 0.65 L/kg and a steady-state volume of distribution (V) of 1.87 ± 0.27 L/kg. Difloxacin exhibited slow elimination, with elimination half-lives (ts) of 1.61 ± 0.3, 2.64 ± 0.64, and 4.27 ± 1.14 h after IM, PO, and IV administration, respectively. Based on the AUC/MIC ratios calculated here, the current IM or IV administration at 10 mg/kg BW is effective against bacterial infections with MIC values ≤ 0.1 μg/mL, while the current oral dose (10 mg/kg BW) may be insufficient, particularly for infections caused by pathogens with MIC values exceeding 0.1 μg/mL.

摘要

本研究旨在调查二氟沙星经口服(PO)、肌肉注射(IM)和静脉注射(IV)给药后在鸽子体内的药代动力学。30只鸽子被随机分为三组(IM组、IV组和PO组;每组n = 10)。通过各给药途径以10 mg/kg体重(BW)给予二氟沙星。在0至48小时的不同时间间隔采集血样,并使用经过验证的高效液相色谱(HPLC)方法分析血浆中二氟沙星的浓度。使用Phoenix软件和非房室分析(NCA)方法确定药代动力学参数。口服和肌肉注射给药后,血浆峰浓度(C)分别为1.81±0.47和6.52±1.62μg/mL,分别在2.60±0.97和0.63±0.24小时出现。口服给药的生物利用度(F)为38.35%±10.45%,肌肉注射给药的生物利用度为90.25%±26.14%。静脉注射给药后,二氟沙星分布广泛,分布容积(V)为2.52±0.65 L/kg,稳态分布容积(V)为1.87±0.27 L/kg。二氟沙星消除缓慢,肌肉注射、口服和静脉注射给药后的消除半衰期(t₁/₂)分别为1.61±0.3、2.64±0.64和4.27±1.14小时。根据此处计算的AUC/MIC比值,当前以10 mg/kg BW进行肌肉注射或静脉注射给药对MIC值≤0.1μg/mL的细菌感染有效,而当前口服剂量(10 mg/kg BW)可能不足,特别是对于由MIC值超过0.1μg/mL的病原体引起的感染。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8425/11770492/a74a375dff13/gr1.jpg

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