Relative bioavailability and pharmacokinetic comparison of two different enteric formulations of omeprazole.

In order to comply with the requirements for a drug listed in China, the study was developed to compare the pharmacokinetics and relative bioavailability of two different enteric formulations of omeprazole (OPZ) in healthy Chinese subjects. A total of 32 volunteers participated in the study. Plasma concentrations were analyzed by nonstereospecific liquid chromatography/tandem mass spectrometric (LC-MS/MS) method. After administration of a single 40-mg dose of the two OPZ formulations, the comparative bioavailability was assessed by calculating individual AUC(0‒t) (the area under the concentration-time curve from time zero to the last measurable concentration), AUC(0‒∞) (the area under the concentration-time curve extrapolated to infinity), C(max) (the maximum observed concentration), and T(peak) (the time to C(max)) values of OPZ, 5-hydroxyomeprazole (OH-OPZ), and omeprazole sulfone (OPZ-SFN), respectively. The 90% confidence intervals (CIs) of AUC(0‒t), AUC(0‒∞), and C(max) were 85.4%‒99.0%/88.8%‒98.6%/87.6%‒99.4%, 85.5%‒99.2%/89.0%‒98.6%/88.5%‒101.3%, and 72.3%‒87.6%/79.6%‒91.1%/88.4%‒99.1% for OPZ/OH-OPZ/OPZ-SFN, respectively, and T(peak) values did not differ significantly. In this study, the test formulation of OPZ in fasting healthy Chinese male volunteers met the Chinese bioequivalance standard to the reference formulation based on AUC, C(max), and T(peak).