Publication: Pharmacokinetics of Metformin in Combination With Sitagliptin in Adult Horses
After Enteral Administration
Authors
Cárceles-Rodríguez, Carlos M. ; Fernández-Varón, Emilio ; Martín-Gimenez, Tamara ; Aguirre, Carla ; Arion, Alexandra ; Rodríguez, María J. ; Ayala de la Peña, Ignacio
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Publisher
Elsevier
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DOI
https://doi.org/10.1016/j.jevs.2018.10.017
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info:eu-repo/semantics/article
Description
© 2019. Elsevier. This document is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0
This document is the accepted version of a published work that appeared in final form in
Journal of Equine Veterinary Science (JEVS)
To access the final work, see DOI: https://doi.org/10.1016/j.jevs.2018.10.017
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 HPLC methods. The t½λz for metformin
was 2.9 hours and for sitagliptin 21 hours. The Cmax 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.
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Citation
Journal of Equine Veterinary Science. Volume 72, January 2019, Pages 84-88
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