Pharmacokinetics and absolute oral bioavailability of meloxicam in guinea pigs (Cavia porcellus)

Abstract

Objective: To investigate the pharmacokinetics and absolute oral bioavailability of meloxicam in guinea pigs.

Study design: Prospective crossover study.

Animals: A group of six healthy male Dunkin Hartley guinea pigs.

Methods: A single dose of meloxicam (1.5 mg kg^-1) was administered orally and intravenously (IV) to six healthy male guinea pigs. A wash-out period of 48 hours was taken into account between administrations (oral and IV) in the same animal. Blood was sampled through a central venous catheter before administration (t = 0 hours) and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 20, 24 and 28 hours post administration. After centrifugation, plasma concentrations of meloxicam were measured by high-performance liquid chromatography with UV detection, and pharmacokinetic parameters were calculated using noncompartmental analysis.

Results: Meloxicam in guinea pigs exhibited a moderate absorption rate after oral dosing (time to maximal plasma concentration 3.7 ± 1.7 hours) and maximal plasma concentration was 0.92 ± 0.30 μg mL^-1. After IV administration, total body clearance and volume of distribution were 0.13 ± 0.04 and 0.72 ± 0.36 L kg^-1, respectively. Terminal half-life was 3.7 ± 0.7 hours and 3.5 ± 1.1 hours after IV and oral administration, respectively. Body extraction ratio was 0.0087 and mean absorption time was 3.8 ± 1.7 hours. The absolute oral bioavailability was 0.54 ± 0.14 in unfasted guinea pigs.

Conclusions and clinical relevance: This study reported the pharmacokinetics of meloxicam in guinea pigs. Studies concerning efficacy and safety are the next step towards a rational use of this drug in guinea pigs.

Keywords: Cavia porcellus; bioavailability; guinea pig; meloxicam; nonsteroidal anti-inflammatory drug; pharmacokinetics.