Scintigraphic assessment of the intragastric distribution and gastric emptying of an encapsulated drug: the effect of feeding and of a proton pump inhibitor.
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.
Atherton
J C
JC
Division of Gastroenterology, University Hospital, Nottingham, UK.
Washington
N
N
Bracewell
M A
MA
Sutton
L J
LJ
Greaves
J L
JL
Perkins
A C
AC
Hawkey
C J
CJ
Spiller
R C
RC
D000328:Adult; D000658:Amoxicillin / Q000008:administration & dosage / Q000493:pharmacokinetics; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002214:Capsules; D018592:Cross-Over Studies; D004044:Dietary Proteins / Q000008:administration & dosage; D004311:Double-Blind Method; D004337:Drug Carriers; D004435:Eating / Q000502:physiology*; D005260:Female; D005502:Food; D005746:Gastric Emptying / Q000187:drug effects* / Q000502:physiology*; D005753:Gastric Mucosa / Q000378:metabolism*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007205:Indium Radioisotopes; D008297:Male; D009853:Omeprazole / Q000494:pharmacology*; D004369:Pentetic Acid / Q000493:pharmacokinetics; D054328:Proton Pump Inhibitors; D011877:Radionuclide Imaging; D013270:Stomach / Q000000981:diagnostic imaging* / Q000187:drug effects; D013667:Technetium
D000900:Anti-Bacterial Agents; D002214:Capsules; D004044:Dietary Proteins; D004337:Drug Carriers; D007205:Indium Radioisotopes; D054328:Proton Pump Inhibitors; D013667:Technetium; D004369:Pentetic Acid; D000658:Amoxicillin; D009853:Omeprazole