Pharmacokinetic and Bioequivalence Evaluation of Febuxostat 40 mg Tablets in Healthy Chinese Subjects Under Fasting and Fed Conditions.

The objective of the current study was to evaluate the rate and extent of absorption, and confirm the bioequivalence of a test formulation and a reference formulation of febuxostat 40 mg tablets in healthy Chinese subjects under both fasting and fed conditions. An open-label, randomized, single-dose, single-center, two-sequence, two-period crossover Phase I study was implemented to assess the pharmacokinetic bioequivalence of the two formulations in 64 healthy volunteers (32 for fasting group, 32 for fed group). Subjects received a single oral dose of either the test or reference febuxostat 40 mg tablet under the corresponding condition, with a 7-day washout period between cycles. The geometric mean ratios and their 90% confidence intervals (CIs) of the peak plasma concentration ( C max ), area under the plasma concentration-time curve from time 0 to the last quantifiable time point ( AU C 0 - t ), and area under the plasma concentration-time curve from time 0 to infinity ( AU C 0 - ∞ ) for the test versus reference formulation were calculated for bioequivalence evaluation. All 90% CIs fell within the pharmacokinetic bioequivalence acceptance range of 80%-125%. A total of 12 adverse events (AEs) were reported in 10 subjects in the fasting group and nine AEs in eight subjects in the fed group, all of which were mild in severity with no serious AEs observed. The test formulation of febuxostat 40 mg tablets was bioequivalent to the reference formulation in healthy Chinese subjects under both fasting and fed conditions, and both formulations were well tolerated.