Bioequivalence study of vonoprazan fumarate tablets in healthy Chinese subjects: a randomized, open-label, two-period crossover trial

Objectives To evaluate the bioequivalence and safety of a test formulation (Vonoprazan Fumarate Tablets, 20 mg, T) compared with the reference product (Takecab®, 20 mg, R) in healthy Chinese subjects under both fasting and fed conditions. Methods This was a single-center, randomized, open-label, single-dose, two-sequence, two-period, crossover study. Seventy-two healthy subjects were enrolled and assigned to either a fasting (n = 32) or a fed (n = 40) cohort. In each period, subjects received a single dose of either the test (T) or reference (R) formulation, separated by a 5-day washout period before crossing over to the alternate treatment. Plasma vonoprazan concentrations were quantified using a validated high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method. Pharmacokinetic parameters were calculated using non-compartmental analysis. Bioequivalence was assessed by determining whether the 90% confidence intervals (CIs) for the geometric mean ratios (GMRs, T/R) of C max , AUC 0-t , and AUC 0 ‐ ∞ fell within the predefined range of 80%–125%. Results Seventy of the 72 enrolled subjects completed the study. Under fasting conditions, the GMRs (90% CIs) for C max , AUC 0-t , and AUC 0 ‐ ∞ were 95.45% (88.96%–102.41%), 98.15% (93.93%–102.56%), and 98.53% (94.41%–102.83%), respectively. Under fed conditions, the corresponding values were 105.00% (94.35%–116.85%) for C max , 101.96% (98.10%–105.97%) for AUC 0-t , and 102.31% (98.58%–106.17%) for AUC 0 ‐ ∞ . All 90% CIs fell within the accepted bioequivalence limits. Adverse events (AEs) were infrequent, with incidence rates of 28.1% and 25.6% in the fasting and fed groups, respectively; no serious adverse events occurred. Conclusion The test formulation of vonoprazan fumarate is bioequivalent to the reference formulation and is well tolerated in healthy Chinese subjects under fasting and fed conditions. Clinical trial registration https://www.chinadrugtrials.org.cn/clinicaltrials.searchlistdetail.dhtml , identifier CTR20233597.