Relative bioavailability study of a generic effervescent tablet formulation of dexketoprofen and thiocolchicoside versus the originator 25 mg film coated tablet (dexketoprofen) and 8 mg capsule (thiocolchicoside)

Abstract

Aims: The aim of this study was to evaluate the pharmacokinetic profiles and the relative bioavailability of dexketoprofen and thiocolchicoside of the test preparation (dexketoprofen / thiocolchicoside 25 mg / 8 mg effervescent tablet) in comparison with the reference preparations (Keral 25 mg film coated tablet, containing dexketoprofen trometamol equivalent to 25 mg dexketoprofen (Menarini International Operations Luxembourg S.A.) (R1) and Muscoril 8 mg capsule, containing 8 mg thiocolchicoside (Sanofi Aventis İlaçları Ltd. Şti.) (R2) under fasting conditions. Methods: 25 healthy male subjects were enrolled in the study. Volunteers were hospitalised from the evening before drug administration (Day 0) until after the 24-hour blood sampling time on Day 2. Results: 24 subjects completed the study. Relative bioavailability (AUCT/AUCR1) of dexketoprofen from the test preparation was 100.99 %; (AUCT/AUCR2) of 3-O-glucuronide of thiocolchicoside (aglycone) from the test preparation was 100.47 %; (Cmax,T/Cmax,R1) of dexketoprofen from the test preparation was 122.59 %; (Cmax,T/Cmax,R2) of 3-O-glucuronide of thiocolchicoside (aglycone) from the test preparation was 111.43 %. Conclusions: The relative bioavailability AUCT /AUCR of the test preparation compared with both reference preparations is comparable, as shown by the geometric mean ratios of 100.59 % (dexketoprofen) and of 98.20 % (3-O-glucuronide of thiocolchicoside (aglycone).