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Home / Equine Research Bank / J Vet Pharmacol Ther / Pharmacokinetics and bioavailability of tildipirosin followi...
Journal of veterinary pharmacology and therapeutics2021; 44(4); 544-551; doi: 10.1111/jvp.12958

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

Abstract: 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 ) of 1257 ng/ml (geometric mean) between 0.5 and 1.5 h after s.c. administration (T ). The geometric mean values for total body clearance (Cl), the apparent volume of distribution based on the terminal phase (V ), and the apparent volume of distribution at steady-state (V ) 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.
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Publication Date: 2021-02-20 PubMed ID: 33609061DOI: 10.1111/jvp.12958Google Scholar: Lookup
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  • Journal Article

Summary

This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.

The research article discusses a study on the safety and pharmacokinetics (drug absorption, distribution, and elimination processes) of a drug called tildipirosin in horses, delivered via intravenous and subcutaneous methods.

Research Methodology

  • The study was conducted on 12 healthy mixed breed horses. These horses were given tildipirosin at a dosage of 4 milligrams per kilogram of body weight. The drug was administered either intravenously (i.v.) or subcutaneously (s.c.).
  • The researchers monitored the horses for any systemic and local side effects. Whole blood samples were taken at certain intervals (0, 6, 24, and 72 hours) after the drug administration. These samples were used for hematological and plasma biochemistry analysis.
  • Additionally, blood samples were collected for Pharmacokinetic (PK) analysis at specific times before and after the administration of tildipirosin.

Results and Findings

  • All the horses tolerated the intravenous injection of the drug without showing any systemic side effects. However, five of the horses showed non-painful, soft swelling at the site of the subcutaneous injection.
  • Plasma concentrations of the drug were measured using a detection method called ultra-high-performance liquid chromatography-ultraviolet (UHPLC-UV).
  • The researchers found that the average maximum plasma concentration (Cmax) of tildipirosin was 1257 ng/ml. This peak was reached between 0.5 and 1.5 hours after subcutaneous administration.
  • The values for total body clearance (Cl), the apparent volume of distribution based on the terminal phase (Vz), and the apparent volume of distribution at steady-state (Vss) were also measured. The geometric mean values for these parameters were 0.52 L/kg·h, 22 L/kg, and 10.0 L/kg, respectively.

Conclusion of the Study

  • The study concludes that tildipirosin can be used safely in horses, but with some caution, particularly when choosing the method of administration. Given that some horses developed a non-painful swelling at the subcutaneous injection site, the intravenous route might be preferable despite it involving a more invasive procedure.

Cite This Article

APA
Abu-Basha EA, Bani Ismail Z, Ababneh MM, Hamzeh E, Gehring R. (2021). Pharmacokinetics and bioavailability of tildipirosin following intravenous and subcutaneous administration in horses. J Vet Pharmacol Ther, 44(4), 544-551. https://doi.org/10.1111/jvp.12958

Publication

Journal of veterinary pharmacology and therapeutics
ISSN: 1365-2885
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 44
Issue: 4
Pages: 544-551

Researcher Affiliations

Abu-Basha, Ehab A
  • Department of Basic Medical Veterinary Sciences, Faculty of Veterinary Medicine, Jordan University of Science and Technology, Irbid, Jordan.
Bani Ismail, Zuhair
  • Department of Veterinary Clinical Sciences, Faculty of Veterinary Medicine, Jordan University of Science and Technology, Irbid, Jordan.
Ababneh, Mohammed M
  • Department of Veterinary Clinical Sciences, Faculty of Veterinary Medicine, Jordan University of Science and Technology, Irbid, Jordan.
Hamzeh, Eyad
  • Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.
Gehring, Ronette
  • Department of Population Health Sciences, Faculty of Veterinary Medicine, Utrecht University, Utrecht, The Netherlands.

MeSH Terms

  • Administration, Oral
  • Animals
  • Area Under Curve
  • Biological Availability
  • Horses
  • Injections, Intravenous / veterinary
  • Tylosin / analogs & derivatives

Grant Funding

  • 298/2019 / Jordan University of Science and Technology

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Citations

This article has been cited 1 times.
  1. Galecio JS, Marín P, Hernandis V, Botía M, Escudero E. Pharmacokinetics of Tildipirosin in Plasma, Milk, and Somatic Cells Following Intravenous, Intramuscular, and Subcutaneous Administration in Dairy Goats.. Pharmaceutics 2022 Apr 13;14(4).
    doi: 10.3390/pharmaceutics14040860pubmed: 35456694google scholar: lookup
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