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左氧氟沙星在杂种犬单次静脉注射和口服给药后的药代动力学及其与硫糖铝的相互作用。

Pharmacokinetics of levofloxacin after single intravenous and oral administration, and its interaction with sucralfate in mixed-breed dogs.

作者信息

Urzúa Natalia, Messina María Jimena, Caverzan Matías, Prieto Guillermo, Lüders Carlos, Errecalde Carlos

机构信息

Departamento de Clínica Animal, Universidad Nacional de Río Cuarto, Río Cuarto, Argentina.

Departamento de Patología Animal, Facultad de Agronomía y Veterinaria, Universidad Nacional de Río Cuarto, Río Cuarto, Argentina.

出版信息

Xenobiotica. 2020 Dec;50(12):1490-1493. doi: 10.1080/00498254.2020.1793031. Epub 2020 Jul 13.

DOI:10.1080/00498254.2020.1793031
PMID:32628058
Abstract

The study aims to establish the plasma pharmacokinetic parameters of levofloxacin in mixed-breed dogs, at a single dose of 5 mg/kg, intravenously, orally only and orally with sucralfate pre-treatment (1 g per animal), to evaluate its influence on antimicrobial absorption. Concentrations of levofloxacin in plasma were determined using high-performance liquid chromatography (HPLC) with fluorescence detection. After iv of levofloxacin, the mean (±SD) of AUC, Vz, ½λz and MRT, was 19.05 ± 6.4 µg-h/ml, 2.43 ± 0.5 L/kg, 7.93 ± 1.41 hours and 8.7 ± 1.5 hours, respectively. After oral administration, the , ½λz and bioavailability were 1.95 ± 0.7 µg/ml, 7.65 ± 1.38 hours and 71.93 ± 9.75%, respectively. In animals given an oral dose of levofloxacin with sucralfate pre-treatment, there was a significant decrease ( < 0.05) in (0.57 ± 0.23 µg/ml), AUC (5.73 ± 2.26 µg-h/ml) and bioavailability (31.92 ± 14.19%). In the dogs studied, it is suggested that the dose 5 mg/kg of levofloxacin for both routes is inadequate to meet PK-PD targets for susceptible bacteria using breakpoints established by the Institute of Clinical and Laboratory Standards (CLSI).

摘要

本研究旨在确定左氧氟沙星在杂种犬体内的血浆药代动力学参数,分别采用单剂量5mg/kg静脉注射、仅口服以及口服并预先给予硫糖铝(每只动物1g)的方式,以评估其对抗菌药物吸收的影响。采用高效液相色谱法(HPLC)结合荧光检测法测定血浆中左氧氟沙星的浓度。静脉注射左氧氟沙星后,AUC、Vz、½λz和MRT的平均值(±标准差)分别为19.05±6.4μg·h/ml、2.43±0.5L/kg、7.93±1.41小时和8.7±1.5小时。口服给药后,Cmax、½λz和生物利用度分别为1.95±0.7μg/ml、7.65±1.38小时和71.93±9.75%。在预先给予硫糖铝后口服左氧氟沙星的动物中,Cmax(0.57±0.23μg/ml)、AUC(5.73±2.26μg·h/ml)和生物利用度(31.92±14.19%)均显著降低(P<0.05)。在所研究的犬中,建议对于两种给药途径,5mg/kg的左氧氟沙星剂量均不足以达到临床和实验室标准协会(CLSI)制定的针对敏感细菌的PK-PD目标。

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