Effect of food on the pharmacokinetics of omeprazole, pantoprazole and rabeprazole

BACKGROUND: The pharmacokinetics of proton pump inhibitors (PPIs) may be affected by food intake. We aimed to evaluate the effect of food on the pharmacokinetics of omeprazole, rabeprazole, and pantoprazole. SETTING: The study population comprised 186 healthy volunteers participating in 6 bioequivalence clinical trials. METHOD: Subjects were evaluated to determine the effect of a high-fat breakfast on the pharmacokinetics of omeprazole (n = 36), rabeprazole (n = 69), and pantoprazole (n = 81). MAIN OUTCOME MEASURE: Drug plasma concentrations were measured using high-performance liquid chromatography coupled to mass spectrometry. RESULTS: Food affected the pharmacokinetics of omeprazole (increased T(max) and decreased AUC and C(max)), pantoprazole (increased T(max) and decreased AUC), and rabeprazole (increased T(max), C(max) and half-life). Food increased variability in T(max) for all 3 drugs, delaying absorption around 3 to 4 h and until 20 h in some subjects. CONCLUSION: As food delays the absorption of PPIs and increases their variability, it would be better to administer these drugs under fasting conditions. TRIAL REGISTRATION: European Union Drug Regulating Authorities Clinical Trials Database: EudraCT: 2004–003863-59 (registration date 05/MAR/2004), EudraCT 2006–001162-17 (registration date 17-MAR-2006), EudraCT: 2007–002489-37 (registration date 12-JUN-2007), EudraCT: 2007–002490-31 (registration date 12-JUN-2007), EudraCT: 2010–024029-19 (registration date 23-NOV-2010).