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

In 30 seconds

This open-label, randomized, single-dose, three-period crossover study compared the pharmacokinetics and safety of 20 mg zastaprazan orally disintegrating tablets (ODTs), taken with or without water, with the conventional tablet in healthy volunteers. Of 54 participants, 51 completed all periods. For both ODT conditions, the 90% confidence intervals for the geometric mean ratios of Cmax and AUCt versus the conventional tablet fell within the predefined bioequivalence range. No additional early systemic exposure was apparent within 30 minutes, and two mild adverse events were reported in one participant.

Key findings

• For ODT without water versus conventional tablet, Cmax and AUCt geometric mean ratios were 95.05% (88.38%-102.21%) and 108.00% (100.50%-116.06%), respectively.
• For ODT with water versus conventional tablet, Cmax and AUCt geometric mean ratios were 90.85% (84.96%-97.16%) and 101.88% (96.69%-107.36%), respectively; all 90% confidence intervals met the predefined bioequivalence range.
• No apparent additional early systemic exposure was observed within 30 min after ODT administration.
• Two mild adverse events occurred in one subject; no serious adverse events were reported.

Why it matters

The findings indicate that, after a single dose in healthy volunteers, zastaprazan ODT produced pharmacokinetic exposure comparable to the conventional tablet whether taken with or without water. This supports administration flexibility without an observed increase in early systemic exposure. The safety observations were limited to this single-dose study and do not establish safety with repeated use or in patient populations.

What to keep in mind

The study assessed a single dose in healthy volunteers, and 51 of 54 participants completed all periods; it does not establish repeated-dose safety or effects in patients.