Scintigraphic assessment of the intragastric distribution and gastric emptying of an encapsulated drug: the effect of feeding and of a proton pump inhibitor

Aliment Pharmacol Ther. 1994 Oct;8(5):489-94. doi: 10.1111/j.1365-2036.1994.tb00320.x.

Abstract

Background: Local delivery of therapeutic agents to the stomach may be a useful strategy in the treatment of Helicobacter pylori infection. We aimed to see whether the intragastric distribution and gastric retention of a therapeutic agent could be improved, either by giving omeprazole or by dosing after a meal.

Methods: Twelve healthy volunteers took part in this double-blind placebo-controlled crossover study comparing the effects of omeprazole 20 mg twice daily for 5 days with placebo, and the fasted with the fed state, on the gastric emptying and intragastric distribution of a soluble scintigrapic marker contained in a drug capsule.

Results: Dosing after food profoundly prolonged gastric residence of the drug label, prolonging mean time to 50% emptying (T50) from 0.5 +/- 0.1 h in the fasted state to 2.0 +/- 0.2 h when given after food. Food also improved intragastric distribution by increasing delivery to the body and fundus. Omeprazole enhanced the effect of food, prolonging T50 to 2.9 +/- 0.3 h, but had no effect in fasted subjects.

Conclusions: Dosing after food markedly improves the aspects of local drug delivery to the stomach investigated in this study, and omeprazole enhances this effect. Post-prandial dosing may, therefore, be useful for improving delivery of some anti-Helicobacter agents.

Publication types

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

MeSH terms

  • Adult
  • Amoxicillin / administration & dosage
  • Amoxicillin / pharmacokinetics
  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / pharmacokinetics*
  • Capsules
  • Cross-Over Studies
  • Dietary Proteins / administration & dosage
  • Double-Blind Method
  • Drug Carriers
  • Eating / physiology*
  • Female
  • Food
  • Gastric Emptying / drug effects*
  • Gastric Emptying / physiology*
  • Gastric Mucosa / metabolism*
  • Humans
  • Hydrogen-Ion Concentration
  • Indium Radioisotopes
  • Male
  • Omeprazole / pharmacology*
  • Pentetic Acid / pharmacokinetics
  • Proton Pump Inhibitors
  • Radionuclide Imaging
  • Stomach / diagnostic imaging*
  • Stomach / drug effects
  • Technetium

Substances

  • Anti-Bacterial Agents
  • Capsules
  • Dietary Proteins
  • Drug Carriers
  • Indium Radioisotopes
  • Proton Pump Inhibitors
  • Technetium
  • Pentetic Acid
  • Amoxicillin
  • Omeprazole