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Journal of veterinary pharmacology and therapeutics2014; 38(2); 130-136; doi: 10.1111/jvp.12169

Pharmacokinetics of intravenous, plain oral and enteric-coated oral omeprazole in the horse.

Abstract: The objectives were to document the pharmacokinetics of intravenous, enteric-coated oral and plain oral omeprazole in fasted horses and to investigate the impact of feeding on the bioavailability of an enteric-coated omeprazole. Twelve horses received four treatments: intravenous omeprazole (0.5 mg/kg) in the fasted state (IV-Fasted), enteric-coated omeprazole (4 mg/kg) orally in the fasted state (ECO-Fasted), enteric-coated omeprazole (4 mg/kg) orally in the fed state (ECO-Fed) and plain omeprazole (4 mg/kg) orally in the fasted state (PL-Fasted). Plasma omeprazole concentrations were determined by UHPLC-MS. Bioavailability was higher (P = 0.038) in the ECO-Fasted group (21.5 [9.0-27.7]%) than the PL-Fasted group (10.1 [7.7-13.3]%). Similarly, AUC0-∞ was higher in the ECO-Fasted group than the PL-Fasted group (P = 0.027). No significant differences were present between the ECO-Fasted and ECO-Fed groups with regards to bioavailability, Cmax , Tmax or AUC0-∞ . When the half-life data from the oral formulations was pooled, it was longer than that observed in the IV-Fasted group (100 [73-118] min) and 35 [34-39] min, respectively; P < 0.0001). Bioavailability of enteric-coated omeprazole was higher than previously reported and feeding had minimal impact. Bioavailability of plain omeprazole was approximately half that of enteric-coated omeprazole. The longer half-life observed following oral administration was consistent with the flip-flop effect and has not previously been described for omeprazole in the horse.
Publication Date: 2014-10-01 PubMed ID: 25271390DOI: 10.1111/jvp.12169Google Scholar: Lookup
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  • Journal Article
  • Randomized Controlled Trial
  • Research Support
  • Non-U.S. Gov't

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 article is about a study that explored the pharmacokinetics of omeprazole administered in different forms and conditions in horses. It was found that enteric-coated oral omeprazole, particularly when the horses were fasted, had a higher bioavailability compared to the other methods of administration.

Study Design

  • The goal of the study was to understand how omeprazole, a medication often used for gastric ulcers in horses, behaves in the horse’s body and how its rate of absorption and overall availability can be influenced by different methods of administration.
  • Twelve horses served as the subjects of the experiment, which consisted of four different treatment groups: fasted state intravenous omeprazole (IV-Fasted), fasted state enteric-coated oral omeprazole (ECO-Fasted), fed state enteric-coated oral omeprazole (ECO-Fed), and fasted state plain oral omeprazole (PL-Fasted).
  • The respective pharmacokinetic properties of these different applications were then tracked and recorded, using UHPLC-MS (Ultra High-Performance Liquid Chromatography-Mass Spectrometry) to determine plasma omeprazole concentrations.

Results and Findings

  • Higher rates of bioavailability (the amount of the drug that is able to be absorbed and used by the body) were discovered among the horses in the ECO-Fasted group, in relation to those in the PL-Fasted group.
  • Similarly, the area under the curve or AUC, representing the total drug exposure over time, was higher in the ECO-Fasted group compared to the PL-Fasted group.
  • There were no consequential differences found between the ECO-Fasted and ECO-Fed groups in terms of bioavailability, peak concentration (Cmax), time to reach peak concentration (Tmax), or AUC.
  • When the half-life data from the oral formulations was combined, it was discovered to be longer than the half-life found in the IV-Fasted group. This indicates the drug stayed in the horse’s system longer when administered orally.

Conclusions

  • The study concluded that enteric-coated omeprazole showed higher bioavailability than previously believed, with feeding having minor effects.
  • The bioavailability of plain omeprazole was about half that of the enteric-coated form, emphasizing the advantage of the enteric-coating.
  • The longer half-life found following oral administration is in line with a common pharmacokinetic phenomenon known as the “flip-flop effect”, which hadn’t been previously reported for omeprazole in horses.

Cite This Article

APA
Sykes BW, Underwood C, McGowan CM, Mills PC. (2014). Pharmacokinetics of intravenous, plain oral and enteric-coated oral omeprazole in the horse. J Vet Pharmacol Ther, 38(2), 130-136. https://doi.org/10.1111/jvp.12169

Publication

ISSN: 1365-2885
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 38
Issue: 2
Pages: 130-136

Researcher Affiliations

Sykes, B W
  • School of Veterinary Sciences, The University of Queensland, Gatton, Qld, Australia.
Underwood, C
    McGowan, C M
      Mills, P C

        MeSH Terms

        • Administration, Oral
        • Animals
        • Anti-Ulcer Agents / administration & dosage
        • Anti-Ulcer Agents / pharmacokinetics
        • Area Under Curve
        • Cross-Over Studies
        • Female
        • Half-Life
        • Horses / blood
        • Horses / metabolism
        • Injections, Intravenous
        • Male
        • Omeprazole / administration & dosage
        • Omeprazole / pharmacokinetics

        Citations

        This article has been cited 9 times.
        1. Harding C, Viljanto M, Hincks P, Habershon-Butcher J, Paine SW. Plasma and Urine Pharmacokinetics of Long-Acting Injectable Omeprazole Following Intramuscular Administrations to Healthy Thoroughbred Horses. J Vet Pharmacol Ther 2025 May;48(3):155-162.
          doi: 10.1111/jvp.13494pubmed: 39921577google scholar: lookup
        2. Vokes J, Lovett A, Sykes B. Equine Gastric Ulcer Syndrome: An Update on Current Knowledge. Animals (Basel) 2023 Apr 5;13(7).
          doi: 10.3390/ani13071261pubmed: 37048517google scholar: lookup
        3. Song Y, Day CM, Afinjuomo F, Tan JE, Page SW, Garg S. Advanced Strategies of Drug Delivery via Oral, Topical, and Parenteral Administration Routes: Where Do Equine Medications Stand?. Pharmaceutics 2023 Jan 4;15(1).
          doi: 10.3390/pharmaceutics15010186pubmed: 36678815google scholar: lookup
        4. Hewetson M, Tallon R. Equine Squamous Gastric Disease: Prevalence, Impact and Management. Vet Med (Auckl) 2021;12:381-399.
          doi: 10.2147/VMRR.S235258pubmed: 35004264google scholar: lookup
        5. Wise JC, Hughes KJ, Edwards S, Jacobson GA, Narkowicz CK, Raidal SL. Pharmacokinetic and pharmacodynamic effects of 2 registered omeprazole preparations and varying dose rates in horses. J Vet Intern Med 2021 Jan;35(1):620-631.
          doi: 10.1111/jvim.15971pubmed: 33340169google scholar: lookup
        6. Gough S, Hallowell G, Rendle D. A study investigating the treatment of equine squamous gastric disease with long-acting injectable or oral omeprazole. Vet Med Sci 2020 May;6(2):235-241.
          doi: 10.1002/vms3.220pubmed: 31945806google scholar: lookup
        7. Cook EK, Satake N, Sykes BW, Bennett EL, Mills PC. Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs. Vet Med (Auckl) 2016;7:123-131.
          doi: 10.2147/VMRR.S112643pubmed: 30050845google scholar: lookup
        8. Sykes BW, Hewetson M, Hepburn RJ, Luthersson N, Tamzali Y. European College of Equine Internal Medicine Consensus Statement--Equine Gastric Ulcer Syndrome in Adult Horses. J Vet Intern Med 2015 Sep-Oct;29(5):1288-99.
          doi: 10.1111/jvim.13578pubmed: 26340142google scholar: lookup
        9. Chee EL, Lim AY, Modamio P, Fernandez-Lastra C, Segarra I. Sunitinib tissue distribution changes after coadministration with ketoconazole in mice. Eur J Drug Metab Pharmacokinet 2016 Jun;41(3):309-19.
          doi: 10.1007/s13318-015-0264-7pubmed: 25656737google scholar: lookup