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Home / Equine Research Bank / J Vet Intern Med / Pharmacokinetics of meloxicam after oral administration of a...
Journal of veterinary internal medicine2019; 33(2); 961-967; doi: 10.1111/jvim.15433

Pharmacokinetics of meloxicam after oral administration of a granule formulation to healthy horses.

Abstract: Nonsteroidal anti-inflammatory drugs are administered in horses for several systemic diseases. Selective cyclooxygenase-2 inhibitors are preferred because of lower risk of adverse effects. Several meloxicam formulations have been tested in horses, but a recently marketed granule oral formulation has not been studied. Objective: To characterize the pharmacokinetics of a novel granule meloxicam formulation in fasted and fed horses, and to compare pharmacokinetic features with oral suspension and tablets. Methods: Seven healthy adult horses. Methods: Meloxicam was administered at 0.6 mg/kg in fasted or fed horses. Blood samples were collected for pharmacokinetic analysis, and vital signs, hematology, and biochemistry variables were monitored for 72 hours. Results: No adverse effects were detected. Volume of distribution and clearance after intravenous administration of meloxicam were 0.36 L/kg and 29.12 mL/h/kg, respectively, with a 12.39 hours of terminal half-life. Protein binding was of 97%. Bioavailability was high for every oral formulation, ranging 70%-110%, without feed effect. Because of a slower absorption, meloxicam after administration of granules had a longer half-life (24 and 34 hours, fasted and fed, respectively) and mean residence time (31 and 47 hours), than suspension and tablets (ranging 10-13 and 13-15 hours, respectively). In addition, the time above therapeutic concentration was higher for the granule formulation than other formulations. Conclusions: Granule formulation has different PK parameters compared to other oral formulations, which could enable this formulation to be used for different dosage regimens in order to reach a desired clinical effect or decrease the risk of adverse effects.
© 2019 The Authors. Journal of Veterinary Internal Medicine published by Wiley Periodicals, Inc. on behalf of the American College of Veterinary Internal Medicine.
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Publication Date: 2019-02-15 PubMed ID: 30768821PubMed Central: PMC6430890DOI: 10.1111/jvim.15433Google Scholar: Lookup
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Summary

This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.

The research paper explores the pharmacokinetics, or the way the drug moves within the body, of a granule formulation of a nonsteroidal anti-inflammatory drug named Meloxicam given orally to healthy horses. The research uncovers that the granule formulation when compared to oral suspension and tablet forms of the drug has a distinct pharmacokinetic profile that could potentially be used for changing dosage routines to achieve desired clinical outcomes or lessen the risk of side effects.

Study Overview

  • The objective of the study was to understand the pharmacokinetics of a new granulated formulation of Meloxicam in both fasted and fed horses, comparing it with the drug’s oral suspension and tablet forms.
  • The study was carried out on seven healthy adult horses. The horses either fasted or were fed and Meloxicam was administered at a dosage of 0.6 mg/kg.
  • Blood samples were collected for pharmacokinetic analysis, while vital signs, hematology, and biochemistry variables were tracked for 72 hours.

Results

  • No adverse effects were detected during the course of this study.
  • The volume of distribution and clearance rates after intravenous administration of Meloxicam were determined to be 0.36 L/kg and 29.12 mL/h/kg, respectively, with a terminal half-life of 12.39 hours. Protein binding was observed at 97%.
  • Across all oral formulations, an unexpectedly high bioavailability (the percentage of the administered drug that reaches the bloodstream and can have an active effect) was noted, ranging from 70% to 110%. Importantly, in contrast to many drugs, the presence or absence of food seemed to have no effect on Meloxicam’s pharmacokinetics.
  • However, the granule formulation of Meloxicam, because of slower absorption, showed both a longer half-life (24 and 34 hours for fasted and fed horses respectively) and mean residence time (31 and 47 hours) compared to the suspension and tablet forms (ranging 10-13 and 13-15 hours respectively).
  • Besides, the time for which the therapeutic concentration of Meloxicam remained in the body was significantly higher for the granule formulation compared to other forms.

Conclusion

  • The study concludes that the granulated formulation of Meloxicam displays a different pharmacokinetic profile compared to other oral formulation such as suspension and tablets.
  • This distinct profile, particularly the longer half-life and residence time, might allow veterinarians to modify dosage regimens as suited to individual horses or specific conditions, which can aim at either maximizing the desired clinical effect or minimizing potential adverse effects.

Cite This Article

APA
Mendoza FJ, Serrano-Rodriguez JM, Perez-Ecija A. (2019). Pharmacokinetics of meloxicam after oral administration of a granule formulation to healthy horses. J Vet Intern Med, 33(2), 961-967. https://doi.org/10.1111/jvim.15433

Publication

Journal of veterinary internal medicine
ISSN: 1939-1676
NlmUniqueID: 8708660
Country: United States
Language: English
Volume: 33
Issue: 2
Pages: 961-967

Researcher Affiliations

Mendoza, Francisco Javier
  • Department of Animal Medicine and Surgery, University of Cordoba, Cordoba, Spain.
Serrano-Rodriguez, Juan Manuel
  • Department of Pharmacology, Toxicology and Legal and Forensic Medicine, University of Cordoba, Cordoba, Spain.
Perez-Ecija, Alejandro
  • Department of Animal Medicine and Surgery, University of Cordoba, Cordoba, Spain.

MeSH Terms

  • Administration, Oral
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / blood
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Biological Availability
  • Fasting
  • Female
  • Horses / metabolism
  • Male
  • Meloxicam / administration & dosage
  • Meloxicam / blood
  • Meloxicam / pharmacokinetics
  • Tablets

Grant Funding

  • AGR-277 / Plan Andaluz de Investigacion from the Consejeria de Salud de la Junta de Andalucia, Spain
  • Virbac SL

Conflict of Interest Statement

None of the authors has a financial or personal relationship with other people or organizations that could inappropriately influence or bias the content of this study. The authors would like to emphasize that both experimental trial and results analysis were not biased or manipulated by Virbac S.L.

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Citations

This article has been cited 5 times.
  1. Mercer MA, Davis JL, McKenzie HC. The Clinical Pharmacology and Therapeutic Evaluation of Non-Steroidal Anti-Inflammatory Drugs in Adult Horses. Animals (Basel) 2023 May 10;13(10).
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  2. Martinez MN, Papich MG, Fahmy R. Impact of gastrointestinal differences in veterinary species on the oral drug solubility, in vivo dissolution, and formulation of veterinary therapeutics. ADMET DMPK 2022;10(1):1-25.
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  3. Plummer C, White PJ, Kimble B, Govendir M, Van der Saag D. Preliminary Investigation into a Novel Sustained-Release Formulation of Meloxicam in Sheep (Ovis aries)-Pharmacokinetic Profile. Animals (Basel) 2021 Aug 24;11(9).
    doi: 10.3390/ani11092484pubmed: 34573450google scholar: lookup
  4. Small A, Fisher AD, Lee C, Colditz I. Analgesia for Sheep in Commercial Production: Where to Next?. Animals (Basel) 2021 Apr 14;11(4).
    doi: 10.3390/ani11041127pubmed: 33920025google scholar: lookup
  5. Nateghi Baygi M, Metcalf LN, Kimble B, Lomax S. When Pain Outlasts Our Drugs: The Case for Sustained-Release Analgesia in Sheep. Animals (Basel) 2026 Feb 5;16(3).
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