Pharmacokinetics of rabeprazole following single intravenous and oral administration to healthy subjects

Int J Clin Pharmacol Ther. 2005 Jan;43(1):37-42. doi: 10.5414/cpp43037.


The study was designed to determine the absolute bioavailability of 20 mg rabeprazole tablets in normal, healthy subjects in comparison with intravenous administration of 20 mg rabeprazole. Twenty-eight healthy subjects were enrolled in this study. The study was a randomized, balanced, open-label, 2-period crossover study. Each subject was randomized at the beginning of the study to receive either a single 20 mg dose of rabeprazole intravenously or orally during Period 1. Following a 7-day washout period, all subjects received the alternate formulation during Period 2. Intravenous dose was given in constant infusion over five minutes. The absolute bioavailability of rabeprazole was 51.8%. The elimination half-life of rabeprazole sodium (1.47 +/- 0.82 h) after oral administration was significantly longer than the elimination half-life after intravenous administration (1.02 +/- 0.63 h), probably due to slower rate of absorption than that of elimination. The mean total body clearance was 283 +/- 98 ml/minutes following a 20 mg intravenous dose. The administration of rabeprazole sodium was safe as evidenced by the lack of serious adverse events and the rapid resolution of the mostly mild adverse events that occurred during the study. Both treatments were well-tolerated throughout the study. Rabeprazole was well-absorbed after oral administration.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • 2-Pyridinylmethylsulfinylbenzimidazoles
  • Absorption
  • Administration, Oral
  • Adult
  • Benzimidazoles / administration & dosage*
  • Benzimidazoles / pharmacokinetics*
  • Biological Availability
  • Cross-Over Studies
  • Enzyme Inhibitors / administration & dosage*
  • Enzyme Inhibitors / pharmacokinetics*
  • Female
  • Humans
  • Infusions, Intravenous
  • Male
  • Middle Aged
  • Omeprazole / administration & dosage*
  • Omeprazole / analogs & derivatives*
  • Omeprazole / pharmacokinetics*
  • Rabeprazole


  • 2-Pyridinylmethylsulfinylbenzimidazoles
  • Benzimidazoles
  • Enzyme Inhibitors
  • Rabeprazole
  • Omeprazole