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https://doi.org/10.2478/acph-2014-0001

Comparative bioavailability of two oral formulations of clopidogrel: Determination of clopidogrel and its carboxylic acid metabolite (SR26334) under fasting and fed conditions in healthy subjects

NINA BRVAR ; Krka, d.d., 8501 Novo mesto, Slovenia
SYLVAIN LACHANCE ; inVentiv Health Clinical, Québec, Québec, Canada
ANN LÉVESQUE ; inVentiv Health Clinical, Québec, Québec, Canada
MARJANCA BREZNIK ; Krka, d.d., 8501 Novo mesto, Slovenia
LEA CVITKOVIČ-MARIČIČ ; Krka, d.d., 8501 Novo mesto, Slovenia
MATEJA MERSLAVIČ ; Krka, d.d., 8501 Novo mesto, Slovenia
IZTOK GRABNAR ; University of Ljubljana, Faculty of Pharmacy, 1000 Ljubljana, Slovenia
TATJANA MATEOVIĆ-ROJNIK ; Krka, d.d., 8501 Novo mesto, Slovenia


Puni tekst: engleski pdf 184 Kb

str. 45-62

preuzimanja: 1.543

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Sažetak

Two randomized, single dose, 2-period, 2-sequence crossover studies were conducted to evaluate the comparative bioavailability of two clopidogrel formulations under fasting and fed conditions. Assessment of bioequivalence was based upon measurement of plasma concentrations of the parent drug, clopidogrel, and its major (inactive) metabolite, clopidogrel carboxylic acid, using improved methanol-free extraction.
Bioequivalence of Krka’s formulation to the innovator’s formulation was demonstrated under both fasting and fed conditions on 205 volunteers. Confidence intervals for AUC0-t, AUC0-inf and Cmax of clopidogrel and its main metabolite were well within the acceptance range of 80.00 to 125.00 %. Food substantially increased the bioavailability of clopidogrel from both formulations, while no effect of food on the extent and rate of exposure to the metabolite was observed. The effect of food was comparable between the two formulations, as indicated by the same direction and rank of food impact on the bioavailability of both formulations.

Ključne riječi

bioavailability, food effect, clopidogrel, clopidogrel carboxylic acid

Hrčak ID:

113579

URI

https://hrcak.srce.hr/113579

Posjeta: 2.078 *