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Journal of equine veterinary science2018; 72; 84-88; doi: 10.1016/j.jevs.2018.10.017

Pharmacokinetics of Metformin in Combination With Sitagliptin in Adult Horses After Enteral Administration.

Abstract: Insulin dysregulation (ID) is a common metabolic disorder in horses. Recently, incretin hormone release has been suggested to be involved in ID in horses. In human medicine, metformin and sitagliptin are commonly used in combination for metabolic syndrome. This combination could be useful in treating ID in horses. However, no pharmacokinetics data have been reported in this species. The objective of the present study was to establish the plasma concentration-time profile and to derive pharmacokinetics data for a combination of metformin and sitagliptin in horses after enteral administration. Six healthy adult Purebred Spanish horses were used. A metformin (15 mg/kg) plus sitagliptin (1.5 mg/kg) preparation was administered by intragastric route (IG) as an enteral solution. Blood samples were collected from 0 to 48 hours after IG drug administration. Plasma concentrations of metformin and sitagliptin were measured using high performance liquid chromatography methods. The t for metformin was 2.9 hours and for sitagliptin 21 hours. The C was 442 ± 84 mg/L within 0.9 hours for metformin and 94 ± 14 mg/L within 1.3 hours for sitagliptin. No adverse effects were observed, and the combination of metformin and sitagliptin was well tolerated. Therefore, these results suggest that metformin plus sitagliptin might be a combination to consider in horses with ID. Additional studies are needed to establish the effectiveness and tolerance in equids affected by endocrine disorders.
Publication Date: 2018-11-02 PubMed ID: 30929789DOI: 10.1016/j.jevs.2018.10.017Google Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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The research article discusses the study focused on the impacts of a metformin and sitagliptin combination on horses with insulin dysregulation when administered orally and suggests that it might be a suitable medication combo for treating ID in horses.

Objective of the Research

  • The main objective of this study was to determine the concentration over time and derive the pharmacokinetics (how the body metabolizes, distributes, and excretes the drugs) for a combination of metformin and sitagliptin in horses after their oral administration.

Study Methodology

  • For the study, six healthy mature Purebred Spanish horses were selected. Metformin and sitagliptin were given to these horses via an enteral (oral) solution.
  • The dosage of metformin was 15 mg/kg and of sitagliptin was 1.5 mg/kg.
  • The concentration of both drugs in the horse’s plasma was monitored from 0 to 48 hours after administering the drug combo. This was done using a technique called high performance liquid chromatography.

Results of the Study

  • The researchers found that the half-life (the time required for the concentration of the drug to reduce to half its initial value) for metformin was 2.9 hours and for sitagliptin was 21 hours.
  • The maximum concentration (C) after which the drug concentration in the blood begins declining was recorded as 442 ± 84 mg/L within 0.9 hours for metformin and 94 ± 14 mg/L within 1.3 hours for sitagliptin.
  • No negative effects were observed after the medication was administered. The combination of metformin and sitagliptin was shown to be well tolerated by the horses, suggesting its potential to be used as a treatment for horses with insulin dysregulation.

Conclusion and Future Scope

  • The research does caution that while the results are promising, more comprehensive studies are needed to establish the effectiveness and tolerance levels against horses suffering from endocrine disorders.

Cite This Article

APA
Cárceles-Rodríguez CM, Fernández-Varón E, Martín-Gimenez T, Aguirre C, Arion A, Rodríguez MJ, Ayala I. (2018). Pharmacokinetics of Metformin in Combination With Sitagliptin in Adult Horses After Enteral Administration. J Equine Vet Sci, 72, 84-88. https://doi.org/10.1016/j.jevs.2018.10.017

Publication

ISSN: 0737-0806
NlmUniqueID: 8216840
Country: United States
Language: English
Volume: 72
Pages: 84-88
PII: S0737-0806(18)30130-8

Researcher Affiliations

Cárceles-Rodríguez, Carlos M
  • Department of Pharmacology, Faculty of Veterinary Medicine, University of Murcia, Murcia, Spain.
Fernández-Varón, Emilio
  • Department of Pharmacology, Faculty of Veterinary Medicine, University of Murcia, Murcia, Spain. Electronic address: emiliofv@um.es.
Martín-Gimenez, Tamara
  • Department of Animal Medicine and Surgery, Faculty of Veterinary Medicine, University of Murcia, Murcia, Spain.
Aguirre, Carla
  • Department of Animal Medicine and Surgery, Faculty of Veterinary Medicine, University of Murcia, Murcia, Spain.
Arion, Alexandra
  • Department of Pharmacology, Faculty of Veterinary Medicine, University of Murcia, Murcia, Spain.
Rodríguez, María J
  • Department of Animal Medicine and Surgery, Faculty of Veterinary Medicine, University of Murcia, Murcia, Spain.
Ayala, Ignacio
  • Department of Animal Medicine and Surgery, Faculty of Veterinary Medicine, University of Murcia, Murcia, Spain.

MeSH Terms

  • Animals
  • Horses / metabolism
  • Hypoglycemic Agents / pharmacokinetics
  • Incretins
  • Insulin / metabolism
  • Metformin / pharmacokinetics
  • Sitagliptin Phosphate

Citations

This article has been cited 1 times.
  1. Bouriche S, Alonso-García A, Cárceles-Rodríguez CM, Rezgui F, Fernández-Varón E. An in vivo pharmacokinetic study of metformin microparticles as an oral sustained release formulation in rabbits. BMC Vet Res 2021 Sep 25;17(1):315.
    doi: 10.1186/s12917-021-03016-3pubmed: 34563196google scholar: lookup