Comparative Pharmacokinetics and Safety of Orally Disintegrating and Conventional Tablet Formulations of Zastaprazan in Healthy Subjects.

Zastaprazan, a potassium-competitive acid blocker, has been developed as an orally disintegrating tablet (ODT) to improve administration flexibility. This study evaluated the pharmacokinetics and safety of a single 20 mg dose of Zastaprazan ODT administered with or without water compared with the conventional tablet in healthy volunteers. In this open-label, randomized, single-dose, 6-sequence, 3-period crossover study, 54 healthy volunteers received a conventional tablet with water, an ODT with water, and an ODT without water. Serial blood samples were collected up to 36 h post-dose, and pharmacokinetic parameters were calculated using a non-compartmental method. Safety was assessed through adverse events, laboratory tests, vital signs, and electrocardiograms. Fifty-one subjects completed all periods. The geometric mean ratios (90% confidence intervals) of Cmax and AUCt were 95.05% (88.38%-102.21%) and 108.00% (100.50%-116.06%) for ODT without water versus the conventional tablet, and 90.85% (84.96%-97.16%) and 101.88% (96.69%-107.36%) for ODT with water versus the conventional tablet, respectively. All 90% confidence intervals were within the predefined bioequivalence range. Ka and Tmax showed similar patterns across treatments, and no apparent additional early systemic exposure was observed within 30 min following ODT administration. Two mild adverse events were reported in one subject, with no serious adverse events. Zastaprazan ODT administered either with or without water was pharmacokinetically equivalent to the conventional tablet, with no apparent additional early systemic exposure and no clinically meaningful safety concerns. Trial Registration: ClinicalTrials.gov: NCT07181538.