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Pharmacokinetics of levofloxacin after single intravenous and oral administration, and its interaction with sucralfate in mixed-breed dogs.
Xenobiotica ( IF 1.3 ) Pub Date : 2020-07-13 , DOI: 10.1080/00498254.2020.1793031
Natalia Urzúa 1 , María Jimena Messina 1 , Matías Caverzan 2 , Guillermo Prieto 1 , Carlos Lüders 3 , Carlos Errecalde 1
Affiliation  

Abstract

  1. 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.

  2. Concentrations of levofloxacin in plasma were determined using high-performance liquid chromatography (HPLC) with fluorescence detection.

  3. After iv of levofloxacin, the mean (±SD) of AUC0–24, Vz, t½λz 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 C max, t½λz and bioavailability were 1.95 ± 0.7 µg/ml, 7.65 ± 1.38 hours and 71.93 ± 9.75%, respectively.

  4. In animals given an oral dose of levofloxacin with sucralfate pre-treatment, there was a significant decrease (p < 0.05) in C max (0.57 ± 0.23 µg/ml), AUC (5.73 ± 2.26 µg-h/ml) and bioavailability (31.92 ± 14.19%).

  5. 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).



中文翻译:

左氧氟沙星单次静脉内和口服给药后的药代动力学及其与硫糖铝的相互作用。

摘要

  1. 这项研究旨在建立左氧氟沙星在混合犬中的血浆药代动力学参数,单次剂量为5 mg / kg,仅静脉内,口服和硫糖铝预处理(每只动物1 g),以评估其对左氧氟沙星的影响。抗菌吸收。

  2. 使用具有荧光检测功能的高效液相色谱(HPLC)测定血浆中左氧氟沙星的浓度。

  3. AUC的左氧氟沙星的平均(±SD)的IV后0-24,1/2,½λz和MRT,为19.05±6.4微克小时/毫升,2.43±0.5升/千克,7.93±1.41小时,8.7±1.5小时, 分别。口服给药后,Ç 最大值½λz和生物利用度分别为1.95±0.7微克/毫升,7.65±1.38小时和71.93±9.75%,分别。

  4. 在给定的与硫糖铝预处理左氧氟沙星的口服剂量的动物,有一个显著减少(p 在<0.05)Ç 最大(0.57±0.23微克/毫升),AUC(5.73±2.26微克小时/ ml)和生物利用度( 31.92±14.19%)。

  5. 在研究的狗中,建议使用临床和实验室标准协会(CLSI)确定的断点,两种途径的左氧氟沙星剂量5 mg / kg不足以满足易感细菌的PK–PD目标。

更新日期:2020-07-13
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