Evaluation of comparative pharmacokinetics and bioequivalence of a new Aceclofenac formulation.

Abstract

Afenac® is a new generic formulation of aceclofenac, a commonly used nonsteroidal anti-inflammatory drug (NSAID) for treating pain of various origins, including inflammatory, degenerative, joint, and musculoskeletal diseases. We compared the pharmacokinetic (PK) properties and evaluated the bioequivalence of two formulations of aceclofenac 100 mg tablets. A single-dose, randomized, 2 × 2 crossover study was performed with 23 healthy Korean male subjects. The subjects randomly received 100 mg of either the test formulation (Afenac®, Korea Arlico Pharm, Seoul, Korea) or the reference formulation (Airtal®, Dae Woong Co., Ltd., Seoul, Korea). After a 1-week washout period, the subjects received the other formulation. Aceclofenac plasma concentrations were determined using the validated high-performance liquid chromatography coupled with tandem mass spectrometry, and pharmacokinetic (PK) parameters were calculated using a noncompartmental method. Geometric mean ratios (GMRs) of the test and reference formulations with 90% confidence intervals (90% CI) were estimated for PK parameters using a generalized linear mixed-effects model. The GMRs (with 90% CI) of the test and reference formulations for the maximum concentration of aceclofenac and the area under the plasma concentration versus time curve from 0 to the last measurable concentration were 0.994 (0.917-1.077) and 0.895 (0.859-0.932), respectively. Both formulations were well tolerated. The test formulation of aceclofenac was bioequivalent to the reference formulation and can be considered a therapeutic option for patients requiring aceclofenac treatment.