Bioequivalence and pharmacokinetic evaluation of two branded formulations of aceclofenac 100 mg: a single-dose, randomized, open-label, two-period crossover comparison in healthy Korean adult volunteers.

BACKGROUND

Aceclofenac is a phenylacetic acid derivative with analgesic and anti-inflammatory properties and an improved gastrointestinal tolerance compared with other NSAIDs, such as diclofenac.

OBJECTIVE

This study was conducted to compare the bioavailability of 2 branded formulations of aceclofenac 100 mg (test and reference) marketed in Korea.

METHODS

This single-dose, randomized, open-label, 2-period crossover study in healthy Korean adult volunteers was conducted at Hanyang University Medical Center (Seoul, Republic of Korea). Subjects received 1 tablet of each aceclofenac 100-mg formulation. Study drugs were administered with 240 mL of water after a 10-hour overnight fast on each of 2 treatment days separated by a 1-week washout period. After study drug administration, serial blood samples were collected over a period of 12 hours. Plasma was analyzed for aceclofenac concentration using a validated high-performance liquid chromatography method with visible detection in the range of 0.1 to 20 microg/mL, with a lower limit of quantitation of 0.1 microg/mL. Several pharmacokinetic (PK) parameters, including C(max), T(max), t(1/2), AUC(0-t), AUC(0-infinity), and k(e), were determined from the plasma concentrations of the 2 aceclofenac formulations. C(max), AUC(0-t), and AUC(0-infinity) were used to test for bioequivalence after log-transformation of plasma data. The predetermined, regulatory range of 90% CI for bioequivalence was 0.80 to 1.25.

RESULTS

A total of 24 subjects were enrolled (20 men, 4 women; mean [SD] age, 23.5 [1.4] years; mean [SD] weight, 68.1 [11.5] kg). No significant differences were found based on analysis of variance, with mean values and 90% CIs of test/reference ratios for these parameters as follows: C(max), 10.57 versus 9.79 microg/mL (0.961-1.225); AUC(0-t), 19.95 versus 19.93 microg x h/mL (0.937-1.037); and AUC(0-infinity), 20.75 versus 20.48 microg x h/mL (0.949-1.049).

CONCLUSION

In these healthy Korean volunteers, results from the PK analysis suggested that the test and reference formulations of aceclofenac 100-mg tablets were bioequivalent, based on the regulatory definition.