Pharmacokinetics and relative bioavailability of meloxicam oil suspension in pigs after intramuscular administration

J Vet Pharmacol Ther. 2020 Mar;43(2):189-196. doi: 10.1111/jvp.12826. Epub 2019 Dec 27.

Abstract

This study aimed to develop one novel meloxicam (MEL) oil suspension for sustained-release and compare the pharmacokinetic characteristics of it with MEL conventional formulation in pigs after a single intramuscular administration. Six healthy pigs were used for the study by a crossover design in two periods with a withdrawal interval of 14 days. Plasma concentrations of MEL were measured by ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). Pharmacokinetic parameters were calculated by noncompartmental methods. The difference was statistically significant (p < .05) between MEL oil suspension and MEL conventional formulation in pharmacokinetic parameters of mean residence time (6.16 ± 4.04) hr versus (2.66 ± 0.55) hr, peak plasma concentration (Cmax ) (0.82 ± 0.12) µg/ml versus (1.12 ± 0.22) µg/ml, time needed to reach Cmax (Tmax ) (2.33 ± 0.82) hr versus (0.59 ± 0.18) hr, and terminal elimination half-life (t1/2λz ) (3.74 ± 2.66) hr versus (1.55 ± 0.37) hr. The mean area under the concentration-time curve (AUC0-∝ ) of MEL oil suspension and MEL conventional formulation was 5.35 and 3.43 hr µg/ml, respectively, with a relative bioavailability of 155.98%. Results of the present study demonstrated that the MEL oil suspension could prolong the effective time of drugs in blood, thereby reducing the frequency of administration on a course of treatment. Therefore, the novel MEL oil suspension seems to be of great value in veterinary clinical application.

Keywords: meloxicam oil suspension; pharmacokinetics; pigs; relative bioavailability; sustained-release.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
  • Area Under Curve
  • Biological Availability
  • Half-Life
  • Injections, Intramuscular
  • Meloxicam / administration & dosage
  • Meloxicam / pharmacokinetics*
  • Suspensions
  • Swine / blood*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Suspensions
  • Meloxicam