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

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.

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 ${\text{AUC}}_{0-\infty }$ fell within the predefined range of 80%-125%.

Seventy of the 72 enrolled subjects completed the study. Under fasting conditions, the GMRs (90% CIs) for C_max, AUC_0-t, and ${\text{AUC}}_{0-\infty }$ 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 ${\text{AUC}}_{0-\infty }$ . 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.

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.

https://www.chinadrugtrials.org.cn/clinicaltrials.searchlistdetail.dhtml, identifier CTR20233597.