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Journal of veterinary pharmacology and therapeutics2006; 29(3); 191-197; doi: 10.1111/j.1365-2885.2006.00737.x

The pharmacokinetics of orbifloxacin in the horse following oral and intravenous administration.

Abstract: The purpose of this study was to determine the pharmacokinetics and physicochemical characteristics of orbifloxacin in the horse. Six healthy adult horses were administered oral and intravenous orbifloxacin at a dose of 2.5 mg/kg. Plasma samples were collected and analyzed by high-pressure liquid chromatography with ultraviolet detection. Plasma protein binding and lipophilicity were determined in vitro. Following i.v. administration, orbifloxacin had a terminal half-life (t1/2) of 5.08 h and a volume of distribution (V(d(SS))) of 1.58 L/kg. Following oral administration, the average maximum plasma concentration (Cmax) was 1.25 microg/mL with a t1/2 of 3.42 h. Systemic bioavailability was 68.35%. Plasma protein binding was 20.64%. The octanol:water partition coefficient (pH 7.4) was 0.2 +/- 0.11. No adverse reactions were noted during this study. Dosage regimens were determined from the pharmacokinetic-pharmacodynamic parameters established for fluoroquinolone antibiotics. For susceptible bacteria, an oral dose of approximately 5 mg/kg once daily will produce plasma concentrations within the suggested range. This dose is suggested for further studies on the clinical efficacy of orbifloxacin for treatment of susceptible bacterial infections in the horse.
Publication Date: 2006-05-04 PubMed ID: 16669863DOI: 10.1111/j.1365-2885.2006.00737.xGoogle Scholar: Lookup
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  • Clinical Trial
  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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The research is a study on the characteristics and effects of orbifloxacin, a medical drug, administered to horses both orally and through intravenous methods. The study determines the pharmacokinetics, protein binding, and lipophilicity of the drug when ingested and intravenously injected, in order to establish effective dosage regimens for treating bacterial infections.

Methodology

  • The research employed a sample size of six healthy adult horses. The horses were given orbifloxacin through two means: orally and through intravenous injection. In both cases, the dose of the drug was 2.5 mg/kg.
  • Plasma samples from these subjects were then collected for further analysis. The researchers used high-pressure liquid chromatography coupled with ultraviolet detection for the said analysis.
  • Furthermore, the plasma protein binding and lipophilicity were determined in vitro, or through the laboratory methods outside the living organism.

Results and Findings

  • The research found out that after intravenous administration, orbifloxacin had a terminal half-life (the time required for the concentration of the drug to reach half its original value) of 5.08 hours. The volume of distribution (a parameter to describe how a drug is distributed in the body) was found out to be 1.58 L/kg.
  • Oral administration led to an average maximum plasma concentration of 1.25 micrograms/mL with a half-life of 3.42 hours. Moreover, systemic bioavailability, which means how much of the drug reaches the circulation to have an active effect, was found to be 68.35%.
  • Plasma protein binding, which determines how drugs are distributed within the body and how they interact with their target proteins, was recorded at 20.64%. The octanol:water partition coefficient, a measure of how the drug distributes between organic and water phases, at pH 7.4, was noted to be 0.2 +/- 0.11.
  • No adverse reactions were noted during the study, implying the drug administration did not lead to any severe or negative responses from the sample subjects.

Conclusions and Recommendations

  • The pharmacokinetic and pharmacodynamic parameters of fluoroquinolone antibiotics, i.e., the behavior of the drug in the body and the drug’s effects on the body, respectively, were used to determine the dosage. The study concludes that an oral dose of approximately 5 mg/kg once daily would result in suitable plasma concentrations for treatment purposes.
  • Based on these findings, the researchers suggest further studies on the clinical efficacy of orbifloxacin for the treatment of susceptible bacterial infections in the horse.

Cite This Article

APA
Davis JL, Papich MG, Weingarten A. (2006). The pharmacokinetics of orbifloxacin in the horse following oral and intravenous administration. J Vet Pharmacol Ther, 29(3), 191-197. https://doi.org/10.1111/j.1365-2885.2006.00737.x

Publication

ISSN: 0140-7783
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 29
Issue: 3
Pages: 191-197

Researcher Affiliations

Davis, J L
  • Clinical Pharmacology Laboratory, Department of Molecular and Biomedical Sciences, College of Veterinary Medicine, North Carolina State University, Raleigh, NC 27606, USA. jennifer_davis@ncsu.edu
Papich, M G
    Weingarten, A

      MeSH Terms

      • Administration, Oral
      • Animals
      • Anti-Infective Agents / administration & dosage
      • Anti-Infective Agents / blood
      • Anti-Infective Agents / pharmacokinetics
      • Area Under Curve
      • Ciprofloxacin / administration & dosage
      • Ciprofloxacin / analogs & derivatives
      • Ciprofloxacin / blood
      • Ciprofloxacin / pharmacokinetics
      • Cross-Over Studies
      • Drug Administration Schedule
      • Female
      • Horses / metabolism
      • Infusions, Intravenous / veterinary
      • Male
      • Protein Binding

      Citations

      This article has been cited 3 times.
      1. Cazedey EC, Salgado HR. Development and validation of a microbiological agar assay for determination of orbifloxacin in pharmaceutical preparations. Pharmaceutics 2011 Aug 29;3(3):572-81.
        doi: 10.3390/pharmaceutics3030572pubmed: 24310597google scholar: lookup
      2. Gebru E, Lee JS, Chang ZQ, Hwang MH, Cheng H, Park SC. Integration of pharmacokinetic and pharmacodynamic indices of orbifloxacin in beagle dogs after a single intravenous and intramuscular administration. Antimicrob Agents Chemother 2009 Jul;53(7):3024-9.
        doi: 10.1128/AAC.01346-08pubmed: 19398644google scholar: lookup
      3. Zhong LG, Tang SJ, Liang LY, Yao X, Sun LW, Sun J, Liao XP, Zhou YF. In vivo pharmacokinetic and pharmacodynamic profiles of orbifloxacin against Staphylococcus aureus in a neutropenic murine thigh infection model. BMC Vet Res 2025 Aug 29;21(1):531.
        doi: 10.1186/s12917-025-04974-8pubmed: 40883777google scholar: lookup