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Pharmacokinetics and bioavailability of tildipirosin following intravenous and subcutaneous administration in horses
Author(s) -
AbuBasha Ehab A.,
Bani Ismail Zuhair,
Ababneh Mohammed M.,
Hamzeh Eyad,
Gehring Ronette
Publication year - 2021
Publication title -
journal of veterinary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.527
H-Index - 60
eISSN - 1365-2885
pISSN - 0140-7783
DOI - 10.1111/jvp.12958
Subject(s) - pharmacokinetics , bioavailability , volume of distribution , distribution (mathematics) , adverse effect , drug administration , body weight , medicine , plasma concentration , pharmacology , chemistry , oral administration , zoology , biology , mathematics , mathematical analysis
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.