Comparative bioavailability study with two pantoprazole delayed-released tablet formulations administered with and without food in healthy subjects.
OBJECTIVE
To assess the comparative bioavailability of two formulations (40 mg delayed-released [DR] tablet; test and reference) of pantoprazole (CAS 102625-70-7) in healthy volunteers of both sexes, with and without food.


METHODS
The study was conducted using an open, randomized, two-period crossover design with a 1-week washout interval, in two groups, with and without food. Plasma samples were obtained for up to 24 h post dose. Plasma pantoprazole concentrations were analyzed by liquid chromatography coupled to tandem mass spectrometry (LC-MS-MS) with positive ion electrospray ionization using multiple reactions monitoring (MRM). From the pantoprazole plasma concentration vs. time curves, the pharmacokinetic parameters AUC(last) and C(max) were obtained, with and without food.


RESULTS
The limit of quantification was 5 ng/mL for plasma pantoprazole analysis. The geometric mean and 90% confidence interval CI of test/reference percent ratios were, without and with food, respectively: 104.6540% (90.8616%-120.5401%) and 99.9708% (90.9987%-109.8275%) for C(max), 95.6634% (85.2675%-107.3267%) and 89.3500% (83.6630%-95.4237%) for AUC(last).


CONCLUSIONS
Since the 90% CI for AUC(last) and C(max) ratios were within the 80-125% interval proposed by the US FDA, it was concluded that pantoprazole 40 mg DR tablet (test formulation) with and without food was bioequivalent to the reference 40 mg DR tablet for both the rate and extent of absorption.
Mendes
Fabiana D
FD
Department of Internal Medicine, Faculty of Medical Sciences, State University of Campinas (UNICAMP), Campinas, SP, Brazil.
Patni
Anil K
AK
Reyer
Simrit
S
Monif
Tausif
T
Moreira
Leonard D
LD
Ilha
Jaime O
JO
Mendes
Gustavo D
GD
De Nucci
Gilberto
G
D053799:2-Pyridinylmethylsulfinylbenzimidazoles / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000293:Adolescent; D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D005215:Fasting / Q000378:metabolism; D005260:Female; D018565:Food-Drug Interactions; D006207:Half-Life; D006801:Humans; D008297:Male; D008875:Middle Aged; D000077402:Pantoprazole; D054328:Proton Pump Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D015203:Reproducibility of Results
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D003692:Delayed-Action Preparations; D054328:Proton Pump Inhibitors; D000077402:Pantoprazole