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 Different Tablet Formulations of Telmisartan of Two Different Strengths (40 mg and 80 mg) in Healthy Male Mexican Volunteers

Daniel Ponce-Navarrete, Armando Cortés-Mendoza, Ericka López-Bojórquez, Jessica González-Bañuelos, Victoria Burke-Fraga and Mario González-de la Parra

Telmisartan is a non-peptide angiotensin II receptor antagonist. In Mexico, it is indicated for the treatment of arterial hypertension and for the prevention of morbidity and mortality of patients ≥ 55 years old with high risk of cardiovascular disease. The aim of these two studies was to compare the bioavailability and to determine the bioequivalence of two test formulations containing 40 mg and 80 mg of oral telmisartan. Two separate, singledose, single-blind, randomized, two-period, crossover studies were conducted. For each study a different set of 30 male subjects completed both studies with a 14-day washout period. In both studies, the study formulations were administered after a 10-hour overnight fast. For pharmacokinetic analysis, blood samples were drawn at baseline, 0.25, 0.5, 0.75, 1, 1.33, 1.67, 2, 3, 4, 6, 8, 12, 24, 48 and 72 hours after administration. Plasma concentrations of telmisartan were determined using HPLC coupled with a fluorescence detector. The test and reference formulations were considered bioequivalent if the 90% CI for the geometric mean test/reference ratios were within the predetermined ranges of 80% to 125%.for AUC0-t and AUC0-∞; and 75% to 133% for Cmax. In the study with telmisartan 40 mg, the 90% CI were 81.23%; 104.94% for Cmax, 92.61%; 115.41% for AUC0-t, 91.83%; and 115.05% for AUC0-∞. In the study with telmisartan 80 mg the 90% CI were 86.84%; 121.07% for Cmax, 90.51%; 110.38% for AUC0-t, 90.58%; and 110.96% for AUC0-∞. In both studies, a single dose of the test formulation met the regulatory requirements to assume bioequivalence, based on the rate and extent of absorption.