Pharmacokinetics

PROTONIX Delayed-Release Tablets are prepared as enteric-coated tablets so that absorption of pantoprazole begins only after the tablet leaves the stomach. Peak serum concentration (Cmax) and area under the serum concentration time curve (AUC) increase in a manner proportional to oral and intravenous doses from 10 mg to 80 mg. Pantoprazole does not accumulate and its pharmacokinetics are unaltered with multiple daily dosing. Following oral or intravenous administration, the serum concentration of pantoprazole declines biexponentially with a terminal elimination half-life of approximately one hour. In extensive metabolizers (see CLINICAL PHARMACOLOGY, Pharmacokinetics, Metabolism) with normal liver function receiving an oral dose of the enteric-coated 40 mg pantoprazole tablet, the peak concentration (Cmax) is 2.5μg/mL, the time to reach the peak concentration (tmax) is 2.5 h and the total area under the plasma concentration versus time curve (AUC) is 4.8μg·hr/mL. When pantoprazole is given with food, its tmax is highly variable and may increase significantly. Following intravenous administration of pantoprazole to extensive metabolizers, its total clearance is 7.6-14.0 L/h and its apparent volume of distribution is 11.0-23.6 L.

PROTONIX® (pantoprazole sodium) For Delayed-Release Oral Suspension has been shown to be comparable to PROTONIX® (pantoprazole sodium) Delayed-Release Tablets in suppressing pentagastrin-stimulated maximum acid output (MAO) in patients with gastroesophageal reflux disease (GERD) and a history of erosive esophagitis (EE) (see CLINICAL PHARMACOLOGY, Pharmacodynamics).

PROTONIX For Delayed-Release Oral Suspension is bioequivalent when administered orally in applesauce or apple juice, or mixed in apple juice and administered through a nasogastric tube. The plasma pharmacokinetic parameters from a crossover study in healthy subjects are summarized in the table below. In this study, a single oral 40 mg dose of Protonix For Delayed-Release Oral Suspension was administered to healthy subjects (N = 22) as granules sprinkled over a teaspoonful of applesauce, as granules mixed with apple juice and, mixed with apple juice followed by administration through a nasogastric tube.

Pharmacokinetics parameters (mean ± SD) of Pantoprazole with Administration of Protonix For Delayed-Release Oral Suspension Sprinkled on Applesauce, Mixed with Apple Juice, Mixed with Apple Juice and Administered through a Nasogastric Tube

Absorption

The absorption of pantoprazole is rapid, with a Cmax of 2.5 g/mL that occurs approximately 2.5 hours after administration of single or multiple 40 mg doses of PROTONIX® (pantoprazole sodium) Delayed-Release Tablets. Pantoprazole is well absorbed; it undergoes little first-pass metabolism resulting in an absolute bioavailability of approximately 77%. Pantoprazole absorption is not affected by concomitant administration of antacids.

Administration of PROTONIX® (pantoprazole sodium) Delayed-Release Tablets with food may delay its absorption up to 2 hours or longer; however, the Cmax and the extent of pantoprazole absorption (AUC) are not altered. Thus, PROTONIX® (pantoprazole sodium) Delayed-Release Tablets may be taken without regard to timing of meals.

PROTONIX® (pantoprazole sodium) For Delayed-Release Oral Suspension should be taken approximately 30 minutes before a meal.

Distribution

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