Pharmacokinetics of Tegoprazan and Metabolite

Plasma tegoprazan and M1 concentration–time profiles after a single oral administration were obtained from a previous comparative pharmacokinetic study comparing two formulations of tegoprazan in healthy Korean male subjects (IRB number: CUH 2015-03-007) [34 (link)]. This study was designed as a randomized, open-label, single-dose, two-sequence, and two-period crossover study. A total of 12 volunteers participated, and the mean ± standard deviation of age, height, and weight were 23.9 ± 1.3 years, 173.1 ± 7.6 cm, and 68.4 ± 8.2 kg, respectively. All subjects were administered a single tegoprazan film-coated 100 mg tablet orally of formulation type 1 or 2 (HK inno.N Corp., Seoul, Korea), and pharmacokinetic profiles were analyzed. For pharmacokinetic analysis, 8 mL of blood was collected to measure the plasma tegoprazan and M1 concentrations during each period at the following time points: pre-dose (0 h) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, and 48 h post-dose. Plasma tegoprazan and M1 concentrations were measured by liquid chromatography–tandem mass spectrometry (LC–MS/MS). Individual concentration–time profiles were used to develop and verify tegoprazan and M1 PBPK models. The PK parameters were calculated using a non-compartmental analysis (NCA) performed by Phoenix^® WinNonlin^® 6.2 (Certara, Princeton, NJ, USA).