Pharmacokinetics and bioavailability of tildipirosin following intravenous and subcutaneous administration in horses.

Autor: Abu-Basha EA; Department of Basic Medical Veterinary Sciences, Faculty of Veterinary Medicine, Jordan University of Science and Technology, Irbid, Jordan., Bani Ismail Z; Department of Veterinary Clinical Sciences, Faculty of Veterinary Medicine, Jordan University of Science and Technology, Irbid, Jordan., Ababneh MM; Department of Veterinary Clinical Sciences, Faculty of Veterinary Medicine, Jordan University of Science and Technology, Irbid, Jordan., Hamzeh E; Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan., Gehring R; Department of Population Health Sciences, Faculty of Veterinary Medicine, Utrecht University, Utrecht, The Netherlands.
Jazyk: angličtina
Zdroj: Journal of veterinary pharmacology and therapeutics [J Vet Pharmacol Ther] 2021 Jul; Vol. 44 (4), pp. 544-551. Date of Electronic Publication: 2021 Feb 20.
DOI: 10.1111/jvp.12958
Abstrakt: This study was designed to investigate the safety and pharmacokinetic (PK) profile of tildipirosin in horses after intravenous (i.v.) and subcutaneous (s.c.) injection of a single dose at 4 mg/kg of body weight (b.w.). A total of 12 healthy mixed breed horses were used in the study. Horses were monitored for systemic and local adverse effects, and whole blood samples were collected for hematology and plasma biochemistry analysis at time (0) and at 6, 24, and 72 h after drug administration. For PK analysis, blood samples were collected at pre-determined times before and after tildipirosin administration. Plasma concentrations of tildipirosin were determined using ultra-high-performance liquid chromatography-ultraviolet detection method (UHPLC-UV). All horses tolerated the i.v. injection of tildipirosin without showing any systemic adverse effects. However, a non-painful, soft swelling appeared at the s.c. injection site in 5 horses (41.7%). On average, tildipirosin reached a maximum plasma concentration (C max ) of 1257 ng/ml (geometric mean) between 0.5 and 1.5 h after s.c. administration (T max ). The geometric mean values for total body clearance (Cl), the apparent volume of distribution based on the terminal phase (V z ), and the apparent volume of distribution at steady-state (V ss ) were 0.52 L/kg·h, 22 L/kg, and 10.0 L/kg, respectively. Data collected in this study suggests that tildipirosin can be used safely in horses with caution.
(© 2021 John Wiley & Sons Ltd.)
Databáze: MEDLINE
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