The combination of Tegoprazan in a 1:1 ratio formulation of immediate-release and delayed-release provides more potent gastric acid suppression both during the day and at night, surpassing the effects of the traditional immediate-release formulation.

A three-period, six-sequence, three-treatment, single-dose, randomized, open-label, three-cohort,  crossover study aimed to investigate the pharmacodynamics (PD) and pharmacokinetics (PK) of different combinations of Tegoprazan with delayed-release (DR) and immediate-release (IR)  formulations.

Oral administration of different doses (50, 75, or 100 mg) of Tegoprazan IR and DR formulations was carried out once during each study period. The intragastric pH was monitored for 24 hours pre and post each administration, and blood samples for PK were collected up to 48 hours. The PK and PD profiles were contrasted among the different intervention groups.

The study involved 18 healthy participants who successfully completed the trial. Following the administration of Tegoprazan, all intervention groups exhibited an intragastric pH >4 after approximately one hour. Comparing different combinations, the 1:1 ratio of IR and DR formulations resulted in higher suppression of gastric acid (%Time pH ≥ 4) compared to IR alone in each dose group.

This effect was observed over a 24-hour period (50 mg; 59% vs. 52%, 100 mg; 85% vs. 70%) and during the night (50 mg; 27% vs. 16%, 100 mg; 77% vs. 49%), while systemic exposure remained comparable.

Compared to the standard IR formulation, the combination of Tegoprazan in a 1:1 ratio of IR and DR formulation demonstrated enhanced suppression of gastric acid levels both during the day and at night.