The effect of food and antacids on lansoprazole absorption and disposition.
Bioavailability of lansoprazole, a new gastric proton pump inhibitor, was investigated in 12 healthy subjects. Each subject received in random order, lansoprazole (30 mg) alone or associated with standard meal or with antacids (aluminium and magnesium hydroxides) or one hour later than antacids. Lansoprazole and metabolite (sulfone (AG 1813), sulfide (AG 1777) and hydroxylated (AG 1908) metabolites) plasma concentrations were determined using a specific high pressure liquid chromatographic assay procedure, with a limit of detection of 2 ng/ml. The time to peak was significantly later with food (p less than 0.001) and its magnitude was significantly decreased (600 +/- 330 ng/ml vs 1151 +/- 344 ng/ml, p less than 0.001). The bioavailability of lansoprazole was significantly decreased by food, about 27%, (p less than 0.05) and slightly decreased by concomitant administration of antacids (NS), the effect was more pronounced in male subjects (p less than 0.05). Lansoprazole is presented as an enteric-coated granules, the concomitant administration of antacids, increasing the gastric pH, increased the absorption rate of lansoprazole. When antacids were administered one hour before lansoprazole, no effect was observed on lansoprazole bioavailability. This study showed that lansoprazole must be administered in fasting state and not simultaneously with antacids.
Delhotal-Landes
B
B
Laboratory of Toxicology and Pharmacokinetics, Ambroise Paré Hospital, Boulogne-Billancourt, France.
Cournot
A
A
Vermerie
N
N
Dellatolas
F
F
Benoit
M
M
Flouvat
B
B
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D000328:Adult; D000536:Aluminum Hydroxide / Q000494:pharmacology; D000863:Antacids / Q000494:pharmacology*; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D004338:Drug Combinations; D005260:Female; D005502:Food; D006207:Half-Life; D006801:Humans; D064747:Lansoprazole; D008276:Magnesium Hydroxide / Q000494:pharmacology; D008297:Male; D009853:Omeprazole / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D013608:Tablets, Enteric-Coated
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D000863:Antacids; D000897:Anti-Ulcer Agents; D004338:Drug Combinations; D013608:Tablets, Enteric-Coated; D064747:Lansoprazole; C013591:aluminum hydroxide, magnesium hydroxide, drug combination; D000536:Aluminum Hydroxide; D009853:Omeprazole; D008276:Magnesium Hydroxide