Pharmacokinetics, Bioequivalence, and Safety Evaluation of Two Formulations of 0.2‐g Ibuprofen Granules

Abstract Ibuprofen is a nonsteroidal anti‐inflammatory agent. In this study, we compared the pharmacokinetic properties, bioequivalence, and safety of a newly developed generic formulation (test) and a branded formulation (reference) of 0.2 g ibuprofen granules in healthy Chinese participants in fasting and fed arms. The randomized, single‐dose, open‐label, two‐preparation, two‐sequence, two‐period crossover study had a washout period of 7 days between each period. It was conducted in 72 participants, 24 in the fasting arm and 48 in the fed arm. The concentration of ibuprofen in the plasma was determined using high‐performance liquid chromatography‐tandem mass spectroscopy. The primary pharmacokinetic parameters were calculated using a noncompartmental model. Safety assessments were performed throughout the study. The mean values of C max , AUC 0‐t , and AUC 0‐∞ for the test and reference preparations of ibuprofen were 19 295 and 21 101 ng/mL, 70 795 and 70 558 ng * h/mL, and 72 023 and 71 647 ng * h/mL, respectively, in the fasting arm and 11 299 and 11 605 ng/mL, 70 983 and 69 157 ng * h/mL, and 73 279 and 71 267 ng * h/mL, respectively, in the fed arm. For all parameters, bioequivalence was within acceptable limits. No serious adverse reactions were reported in this study. This study demonstrated that the 2 formulations of ibuprofen granules were bioequivalent in healthy Chinese volunteers under fasting and fed conditions.