Abstract

Pharmacokinetics and urinary excretion of an intravenous dose of 5 mg.kg-1 ofloxacin were investigated in water buffalo calves. Plasma concentrations of ofloxacin were determined by high-performance liquid chromatography. Ofloxacin was rapidly distributed from the central to the peripheral compartment as evidenced by a short distribution half-life (0.09 h ± 0.003 h) and high K12 (4.7 h(-1) ± 0.1 h(-1)), and was detected in plasma for 8 h. The large volume of distribution (2.48 L.kg(-1) ± 0.18 L.kg(-1)) obtained in this study indicated high distribution of ofloxacin in water buffalo calves. The elimination half-life, the area under the plasma drug concentration-time curve and total body clearance were 2.11 h ± 0.13 h, 6.20 µg.mL(-1) ± 0.23 µg.mL(-1).h and 0.81 mL.kg(-1).h(-1) ± 0.03 mL.kg(-1).h(-1), respectively. About 18.7% of administered drug was bound to plasma proteins and approximately 32.5% of the administered dose was recovered in urine within 48 h. The results of the study indicated a favourable pharmacokinetic profile of ofloxacin in water buffalo calves, which suggests that ofloxacin may be effective against urinary pathogens in this species.

Highlights

  • Fluoroquinolones have gained widespread acceptance in veterinary medicine thanks to their broad spectrum of activity against Gram-positive and Gram-negative aerobes, mycoplasma and rickettsia (Brown 1996)

  • Pharmacokinetic studies of ofloxacin after intravenous administration have been conducted in humans (Bethell et al 1996), dogs (Yoshida et al 1998), swine (Son et al 2000), goats (Baruah et al 2004), cattle (Gaur et al 2004), chicken (Kalaiselvi et al 2006) and rabbits (Ahmad et al 2008)

  • Evaluation of the results revealed that plasma disposition of ofloxacin followed a two-compartment open model, which is adequately described by the bi-exponential equation: Cp = Ae–at + Be–bt

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Summary

Introduction

Fluoroquinolones have gained widespread acceptance in veterinary medicine thanks to their broad spectrum of activity against Gram-positive and Gram-negative aerobes, mycoplasma and rickettsia (Brown 1996) These antibacterials are currently used for the treatment of invasive and systemic bacterial infections, such as upper and lower respiratory infections, gonorrhoea, bacterial gastroenteritis, skin and soft tissue infections and urinary tract infections that occur in humans and animals (Duan & Yuan 2001). Ofloxacin, (±)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4 benzoxazine-6 carboxylic acid (Lode et al 1987), a synthetic fluoroquinolone, was introduced in the late 1980s (Andersson & MacGowan 2003). It possesses a broad spectrum of activity against a variety of Gram-positive and Gram-negative bacteria, including some anaerobes. In view of the marked variation in the kinetic behaviour of antimicrobial drugs amongst species, the present study was undertaken to determine the pharmacokinetics, in vitro plasma protein binding and urinary excretion following a single intravenous administration of ofloxacin in water buffalo calves

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