Abstract

Aim: The objective of the present study was to study the disposition kinetics and dosage regimens of long acting moxifloxacin following intravenous administration at the dose rate of 7.5 mg/kg-1 b. wt. in six male sheep and to calculate dosage regimens of the same in sheep. Materials and Methods: The study was conducted using six healthy male sheep. Long acting Moxifloxacin solution (10 % moxifloxacin in solution with L- arginine, N-butyl alcohol and benzyl alcohol) was injected in jugular vein and periodical blood samples were collected from contra-lateral jugular vein in test tubes containing 30-50 IU heparin (anticoagulant) at 0.083 (5 min), 0.166 (10 min), 0.5, 1, 2, 4, 8, 12, 24, 36, 48, 60, 72 and up to 96 h post administration of drug. Drug concentration in plasma was determined using High Performance Liquid Chromatography (HPLC) with Fluorescence Detector. The blood concentrations versus time data were analyzed using software. Results: After single dose intravenous administration of long acting moxifloxacin the plasma concentration of 0.016 ± 0.001 μg/ml-1 was maintained for up to 72 h. Distribution half-life (t ) and elimination half-life (t ) were 1.637 ± 0.053 h, and 1/2 1/2 12.130 ± 0.202 h, following IV administration. The mean values of apparent volume of distribution V 5.436 ± 0.135 L/kg-1 d(area) as well as mean residence time 10.02 ± 4.787 minute were detected with IV administration. Conclusion: The long acting Moxifloxacin @ the dose 7.5 mg/kg IV maintains the effective therapeutic concentration in the plasma of sheep for up to 72 hours. The long acting Moxifloxacin at this dose rate can be used to treat sensitive bacteria causing infectious diseases in sheep.

Highlights

  • Moxifloxacin is a new 8-methoxy-quinolone with a broad spectrum of antibacterial activity against Gram-positive and Gram-negative bacteria, anaerobes and atypical organisms such as Mycoplasma and Chlamydia spp

  • Pharmacokinetics studies of moxifloxacin would be of great use as it provides a basis for the determination of satisfactory dosage regimen in sheep under our tropical climate

  • As the effectiveness of an antibacterial agent depends on its efficacy, safety and pharmacokinetic disposition in the target animal, the aim of the present study was to investigate the plasma pharmacokinetics of long acting moxifloxacin in sheep after single intravenous (IV) administration

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Summary

Introduction

Moxifloxacin is a new 8-methoxy-quinolone with a broad spectrum of antibacterial activity against Gram-positive and Gram-negative bacteria, anaerobes and atypical organisms such as Mycoplasma and Chlamydia spp. The MIC of moxifloxacin for Mycobacterium ulcerans ranged from 0.015-0.5 μg/ml-1 [3], for S. aureus from 0.03-0.12 μg/ml-1 [4]. Pharmacokinetics studies of moxifloxacin would be of great use as it provides a basis for the determination of satisfactory dosage regimen in sheep under our tropical climate. These have been studied exclusively by in various animals species like lactating goats [7], lactating ewes [8], camel [9], rabbits [4], Mice [10] and Horse [11]. As the effectiveness of an antibacterial agent depends on its efficacy, safety and pharmacokinetic disposition in the target animal, the aim of the present study was to investigate the plasma pharmacokinetics of long acting moxifloxacin in sheep after single intravenous (IV) administration

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