Relative Bioavailability of Ticagrelor from Hard Capsules and Film-Coated Tablets in Healthy Caucasian Volunteers

Le résumé fourni par la source

Ticagrelor is an active pharmaceutical ingredient of the first oral medicinal product inhibiting adenosine diphosphate-induced platelet aggregation by reversibly binding to P2Y12 receptor. It is co-administered with acetylsalicylic acid in patients with acute coronary syndromes or a history of myocardial infarction with high risk of cardiovascular events. The aim of study was to evaluate relative bioavailability of ticagrelor from two oral pharmaceutical forms hard capsules (Tikozek, test product) vs. film-coated tablets (Brilique®, reference product) after a single 90 mg dose administration. A randomized, 2-period, crossover, open-label, and laboratory-blinded study was conducted in healthy Caucasian male and female volunteers in Poland. Ticagrelor in human plasma was quantified by a validated LC-MS/MS method using isotope labelled internal standard. Two pharmaceutical forms were considered bioequivalent when 90% confidence intervals (CI) of the log-transformed geometric mean ratios (hard capsules over film-coated tablets) for both AUC(0-t) and Cmax were within 80.00-125.00%. Adverse events, values of laboratory parameters, and vital signs were recorded during the study. Among 40 volunteers enrolled, 37 completed the study. Geometric mean ratios for the primary pharmacokinetic parameter were 100.51% (90% CI 95.00-106.34%) for AUC(0-t), and 92.43% (90% CI 84.11-101.58%) for Cmax. Ticagrelor administered in both pharmaceutical forms was well tolerated. No serious adverse events were recorded. Results of the clinical trial indicate that hard capsules (Tikozek) are bioequivalent to the film-coated tablets (Brilique®).

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