生物学的同等性とバイオアベイラビリティのジャーナル

概要

Bioavailability of Two Coated-Tablet Formulations of a Single Dose of Pantoprazole 40 mg: An Open-Label, Randomized, Two-Period Crossover, Comparison in Healthy Mexican Adult Volunteers

Juana Isabel Balderas-Acata, Esteban Patricio Ríos-Rogríguez Bueno, Sofía del Castillo-García, Clara Espinosa-Martínez, Victoria Burke-Fraga and Mario González-de la Parra

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 ng•h /ml, 5720 ± 2527 ng•h / ml); and 6097 ± 2415 ng•h /ml, 6292 ± 2548 ng•h /ml), respectively The 90% CIs for the geometric mean ratios of Cmax, AUC0–t and AUC0–8 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.