Pharmacokinetics of Tildipirosin in Ewes after Intravenous, Intramuscular and Subcutaneous Administration

A single-dose disposition kinetics for tildipirosin was evaluated in clinically healthy ewes (<i>n</i> = 6) after intravenous (IV), intramuscular (IM), and subcutaneous (SC) administration of a commercial formulation. Tildipirosin concentrations were determined by high-performance liquid...

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Main Authors: Juan Sebastián Galecio, Elisa Escudero, José Joaquín Cerón, Giuseppe Crescenzo, Pedro Marín
Format: Article
Language:English
Published: MDPI AG 2020-08-01
Series:Animals
Subjects:
Online Access:https://www.mdpi.com/2076-2615/10/8/1332
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author Juan Sebastián Galecio
Elisa Escudero
José Joaquín Cerón
Giuseppe Crescenzo
Pedro Marín
author_facet Juan Sebastián Galecio
Elisa Escudero
José Joaquín Cerón
Giuseppe Crescenzo
Pedro Marín
author_sort Juan Sebastián Galecio
collection DOAJ
description A single-dose disposition kinetics for tildipirosin was evaluated in clinically healthy ewes (<i>n</i> = 6) after intravenous (IV), intramuscular (IM), and subcutaneous (SC) administration of a commercial formulation. Tildipirosin concentrations were determined by high-performance liquid chromatography with ultraviolet detection. Plasma concentration-time data was calculated by non-compartmental pharmacokinetic methods. The apparent volume of distribution (Vz) of tildipirosin after IV administration was 5.36 ± 0.57 L/kg suggesting a wide distribution in tissues and inside the cells. The elimination half-life (t½λz) was 17.16 ± 2.25, 23.90 ± 6.99 and 43.19 ± 5.17 h after IV, IM and SC administration, respectively. Following IM administration, tildipirosin was rapidly absorbed (tmax = 0.62 ± 0.10 h) even to a greater extent than after SC administration. Time to reach peak concentration (tmax) and peak plasma concentrations (Cmax) differed significantly, but both parameters showed a more significant variability after SC than after IM administration. Bioavailabilities after extravascular administration were high (>70%). Therefore, given general adverse reactions that were not observed in any ewe and favourable pharmacokinetics, tildipirosin could be effective in treating bacterial infections in sheep.
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spelling doaj.art-89c0989dbec34577a24d53108fb1c1b02023-11-20T08:46:04ZengMDPI AGAnimals2076-26152020-08-01108133210.3390/ani10081332Pharmacokinetics of Tildipirosin in Ewes after Intravenous, Intramuscular and Subcutaneous AdministrationJuan Sebastián Galecio0Elisa Escudero1José Joaquín Cerón2Giuseppe Crescenzo3Pedro Marín4Department of Pharmacology, Faculty of Veterinary Medicine, University of Murcia, 30100 Murcia, SpainDepartment of Pharmacology, Faculty of Veterinary Medicine, University of Murcia, 30100 Murcia, SpainInterdisciplinary Laboratory of Clinical Pathology, Interlab–UMU, University of Murcia, 30100 Murcia, SpainDepartment of Veterinary Medicine, University of Bari Aldo Moro, 70010 Valenzano, BA, ItalyDepartment of Pharmacology, Faculty of Veterinary Medicine, University of Murcia, 30100 Murcia, SpainA single-dose disposition kinetics for tildipirosin was evaluated in clinically healthy ewes (<i>n</i> = 6) after intravenous (IV), intramuscular (IM), and subcutaneous (SC) administration of a commercial formulation. Tildipirosin concentrations were determined by high-performance liquid chromatography with ultraviolet detection. Plasma concentration-time data was calculated by non-compartmental pharmacokinetic methods. The apparent volume of distribution (Vz) of tildipirosin after IV administration was 5.36 ± 0.57 L/kg suggesting a wide distribution in tissues and inside the cells. The elimination half-life (t½λz) was 17.16 ± 2.25, 23.90 ± 6.99 and 43.19 ± 5.17 h after IV, IM and SC administration, respectively. Following IM administration, tildipirosin was rapidly absorbed (tmax = 0.62 ± 0.10 h) even to a greater extent than after SC administration. Time to reach peak concentration (tmax) and peak plasma concentrations (Cmax) differed significantly, but both parameters showed a more significant variability after SC than after IM administration. Bioavailabilities after extravascular administration were high (>70%). Therefore, given general adverse reactions that were not observed in any ewe and favourable pharmacokinetics, tildipirosin could be effective in treating bacterial infections in sheep.https://www.mdpi.com/2076-2615/10/8/1332macrolidespharmacokineticssheepewestildipirosin
spellingShingle Juan Sebastián Galecio
Elisa Escudero
José Joaquín Cerón
Giuseppe Crescenzo
Pedro Marín
Pharmacokinetics of Tildipirosin in Ewes after Intravenous, Intramuscular and Subcutaneous Administration
Animals
macrolides
pharmacokinetics
sheep
ewes
tildipirosin
title Pharmacokinetics of Tildipirosin in Ewes after Intravenous, Intramuscular and Subcutaneous Administration
title_full Pharmacokinetics of Tildipirosin in Ewes after Intravenous, Intramuscular and Subcutaneous Administration
title_fullStr Pharmacokinetics of Tildipirosin in Ewes after Intravenous, Intramuscular and Subcutaneous Administration
title_full_unstemmed Pharmacokinetics of Tildipirosin in Ewes after Intravenous, Intramuscular and Subcutaneous Administration
title_short Pharmacokinetics of Tildipirosin in Ewes after Intravenous, Intramuscular and Subcutaneous Administration
title_sort pharmacokinetics of tildipirosin in ewes after intravenous intramuscular and subcutaneous administration
topic macrolides
pharmacokinetics
sheep
ewes
tildipirosin
url https://www.mdpi.com/2076-2615/10/8/1332
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