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 AUC_0–24, 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).

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，吨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，吨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。