The Bioequivalence Study of Two Dexketoprofen 25 mg Film-Coated Tablet Formulations in Healthy Males Under Fasting Conditions

INTRODUCTION: Dexketoprofen is a non-steroidal analgesic/anti-inflammatory drug and its’ trometamol salt is extensively preferred in mild or moderate pain due to its rapid onset of relief. A new formulation of 36.9 mg of dexketoprofen trometamol (equivalent to 25 mg of dexketoprofen) tablet has been developed and its bioequivalence to the reference product was proven.
METHODS: An open-label, single-dose, randomized, two-period, cross-over bioequivalence study was conducted with healthy males under fasting conditions for two different tablet formulations of 25 mg of dexketoprofen. In order to prove the bioequivalence of the test product with the reference product, the comparison study has been performed in compliance with regulations in force under Good Clinical Practice principles. A single-center clinical study was run and blood samples of the participants have been withdrawn at specified time points, before and after dosing, to measure the plasma concentrations of dexketoprofen trometamol. A validated analytical method has been developed by using an LC-MS/MS instrument to assess the plasma concentrations of the test and reference products.
RESULTS: 47 volunteers completed the clinical phase of the study. For the test and reference products, the mean ± SD of Cmax were found 2543.82 ± 655.42 ng/mL and 2539.11 ± 662.57 ng/mL, and the mean ± SD of AUC0-tlast were found 3483.49 ± 574.42 h.ng/mL and 3560.75 ± 661.83 h.ng/mL, respectively. The primary target variables data demonstrate the bioequivalence of test and reference products with regard to 90% CI for Cmax of 92.45 – 108.53 and for AUC0-tlast of 95.57 – 100.87. The geometric mean ratios were found as 100.16% and 98.18% for Cmax and AUC0-tlast, respectively. There were no serious adverse events or adverse reactions reported throughout the study.
DISCUSSION AND CONCLUSION: After statistical evaluation of the analytical results, the test and reference products were considered to be bioequivalent. Both products were well tolerated and considered as safe.