Pharmacokinetics of pantoprazole following single intravenous and oral administration to healthy male subjects.
The plasma pharmacokinetics of pantoprazole have been investigated following single intravenous infusion and single oral administration at a dose of 40 mg to 12 healthy male subjects in a randomised cross-over study. Both treatments were generally well tolerated and no relevant compound-related adverse events were noted. The plasma pharmacokinetics of pantoprazole following intravenous infusion in this group of subjects were characterised by a total plasma clearance of 0.13 l.h-1 x kg-1 and apparent terminal elimination half-life 1.9 h. The apparent volume of distribution estimated at steady state (0.17 l.kg-1) was compatible with the localization of a major fraction of the compound in extracellular water. Following oral administration as an enteric-coated tablet formulation, a variable onset of absorption was followed by rapid attainment of maximum plasma concentrations of pantoprazole. Pantoprazole was well absorbed following oral administration; the absolute systemic bioavailability of the compound was estimated as 77% (95% CI, 67 to 89%).
Pue
M A
MA
SmithKline Beecham, Department of Drug Metabolism and Pharmacokinetics, Welwyn, UK.
Laroche
J
J
Meineke
I
I
de Mey
C
C
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D000251:Adenosine Triphosphatases / Q000037:antagonists & inhibitors; D000284:Administration, Oral; D000328:Adult; D001562:Benzimidazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D004334:Drug Administration Schedule; D006207:Half-Life; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D008657:Metabolic Clearance Rate; D009853:Omeprazole / Q000031:analogs & derivatives; D000077402:Pantoprazole; D013454:Sulfoxides / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D013608:Tablets, Enteric-Coated
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D001562:Benzimidazoles; D013454:Sulfoxides; D013608:Tablets, Enteric-Coated; D000077402:Pantoprazole; D000251:Adenosine Triphosphatases; D009853:Omeprazole