Abstract
Pantoprazole is a proton pump inhibitor indicated for the treatment of acid-related gastrointestinal diseases such as reflux esophagitis, duodenal and gastric ulcers. The aims of this study were to compare the bioavailability and to determine the bioequivalence of a test and reference formulation of oral pantoprazole 40 mg, administered as a coated tablet, and to generate data regarding the oral bioavailability of this drug in the Mexican population. This single-dose, randomized-sequence, open-label, 2-period crossover study was conducted on a total 34 healthy Mexican adult subjects of both genders, with a 7-days washout period. Study formulations were administered after a 10-hour overnight fast. For pharmacokinetic analysis, blood samples were drawn at 0 (baseline), 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2.0, 2.5, 3, 3.5, 4, 5, 6, 8, and 10 hours after administration. Plasma concentrations of pantoprazole were determined using HPLC coupled to a UV detector. The test and reference formulations were to be considered bioequivalent if the 90% CIs for the geometric mean test/reference ratios were within a predetermined range of 80% to 125%. The estimated pharmacokinetic parameters of pantoprazole for the reference (Pantozol ® ) and test (Prazolan ® ) formulations were Cmax (3448 ± 1214 ng/ml, 3610 ± 1344 ng/ml); AUC0-t, (5521± 2454 ngh /ml, 5720 ± 2527 ngh / ml); and 6097 ± 2415 ngh /ml, 6292 ± 2548 ngh /ml), respectively The 90% CIs for the geometric mean ratios of C max , AUC 0-t and AUC 0-∞ were 90.13% to 117.04%, 92.45% to 113.18%, and 94.50% to 108.16%, respectively. In this study a single dose of the test formulation met the regulatory requirements to assume bioequivalence, based on the rate and extent of absorption.
Highlights
Pantoprazole, (R,S)-6-(difluoromethoxy)-2-[(3,4-dimethoxypyridin-2yl)methylsulfinyl]-1H-benzo[d]imidazole, is a proton pump inhibitor [11,5] indicated for the treatment of acid-related gastrointestinal diseases such as reflux esophagitis, duodenal and gastric ulcers [8,2].Its absolute bioavailability is 77% and it is not affected by multiple dosing
The bioavailability of pantoprazole is not affected by the concomitant intake of food [7]
Pantozol® was selected as the reference formulation [9] because it is included in the list of Drug Reference Medications issued by the Mexican Federal Commission for the Protection Against Sanitary Risks [4]
Summary
Pantoprazole, (R,S)-6-(difluoromethoxy)-2-[(3,4-dimethoxypyridin-2yl)methylsulfinyl]-1H-benzo[d]imidazole, is a proton pump inhibitor [11,5] indicated for the treatment of acid-related gastrointestinal diseases such as reflux esophagitis, duodenal and gastric ulcers [8,2].Its absolute bioavailability is 77% and it is not affected by multiple dosing. Pantoprazole shows lineal pharmacokinetics after both i.v. and oral administration. It is extensively metabolized in the liver, has a total serum clearance of 0.1 l/h/kg, an elimination half life of approximately 1.1 hour, and an apparent volume of distribution of 0.15 l/kg. It is important to point out that the reference medications (formulations) indicated in this list are mandatory for the bioequivalence studies performed in Mexico.
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