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

BMC Pharmacol Toxicol. 2020 Jul 25;21(1):54. doi: 10.1186/s40360-020-00433-2.


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 Tmax and decreased AUC and Cmax), pantoprazole (increased Tmax and decreased AUC), and rabeprazole (increased Tmax, Cmax and half-life). Food increased variability in Tmax 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).

Keywords: Food; Omeprazole; Pantoprazole; Pharmacokinetics; Proton pump inhibitors; Rabeprazole.

Publication types

  • Clinical Trial, Phase I
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Anti-Ulcer Agents / blood
  • Anti-Ulcer Agents / pharmacokinetics*
  • Cross-Over Studies
  • Cytochrome P-450 CYP2C19 / genetics
  • Dietary Fats / administration & dosage*
  • Fasting / metabolism
  • Female
  • Food-Drug Interactions*
  • Genotype
  • Humans
  • Male
  • Omeprazole / blood
  • Omeprazole / pharmacokinetics*
  • Pantoprazole / blood
  • Pantoprazole / pharmacokinetics*
  • Proton Pump Inhibitors / blood
  • Proton Pump Inhibitors / pharmacokinetics*
  • Rabeprazole / blood
  • Rabeprazole / pharmacokinetics*
  • Young Adult


  • Anti-Ulcer Agents
  • Dietary Fats
  • Proton Pump Inhibitors
  • Rabeprazole
  • Pantoprazole
  • CYP2C19 protein, human
  • Cytochrome P-450 CYP2C19
  • Omeprazole

Associated data

  • EudraCT/2004–003863-59
  • EudraCT/2006–001162-17
  • EudraCT/2007–002489-37
  • EudraCT/2007–002490-31
  • EudraCT/2010–024029-19