Eslicarbazepine Acetate (BIA 2-093)Relative Bioavailability and Bioequivalence of 50 mg/mL Oral Suspension and 200mg and 800mg Tablet Formulations
作者:
Carlos Fontes-Ribeiro,
Teresa Nunes,
Amilcar Falcão,
Carla Neta,
Ricardo Lima,
Susana Tavares,
Luis Almeida,
Tice Macedo,
Patricio Soares-da-Silva,
期刊:
Drugs in R & D
(ADIS Available online 2005)
卷期:
Volume 6,
issue 5
页码: 253-260
ISSN:1174-5886
年代: 2005
出版商: ADIS
关键词: Antiepileptic drugs, pharmacokinetics;Bioavailability;Bioequivalence;Eslicarbazepine, pharmacokinetics;Sodium channel antagonists, pharmacokinetics
数据来源: ADIS
摘要:
PurposeTo investigate the bioavailability and bioequivalence of three different formulations of eslicarbazepine acetate (BIA 2-093): 50 mg/mL oral suspension (test 1), 200mg tablets (test 2) and 800mg tablets (reference).Design, subjects and methodsSingle-centre, open-label, randomised, three-way crossover study in 18 healthy subjects. The study consisted of three consecutive periods separated by a washout period of 7 days or more. Each subject received a single dose of eslicarbazepine acetate 800mg on three different occasions: 16mL of oral 50 mg/mL suspension, four 200mg tablets or one 800mg tablet.ResultsEslicarbazepine acetate was rapidly and extensively metabolised to BIA 2-005. Maximum BIA 2-005 plasma concentrations (Cmax) and area under the plasma concentration-time curve from time 0 to infinity (AUC∞) were, respectively (arithmetic mean ± SD), 18.0 ± 4.6 µg/mL and 325.7 ± 64.9 μg · h/mL for test 1, 16.0 ± 4.0 µg/mL and 304.2 ± 66.0 μg · h/mL for test 2, and 17.0 ± 4.1 µg/mL and 301.1 ± 60.0 μg · h/mL for the reference formulation. Point estimate (PE) and 90% confidence intervals (CIs) for AUC∞test 1/reference geometric mean ratio were 1.09 and 1.01, 1.15; for Cmaxratio, PE and 90% CI were 1.07 and 0.97, 1.15. When test 2 and the reference formulations were compared, the PE and 90% CI were 0.99 and 0.94, 1.07 for the AUC∞ratio, and 0.94 and 0.86, 1.02 for the Cmaxratio. Bioequivalence of test versus reference formulations is thus accepted for both AUC∞and Cmaxbecause the 90% CIs lie within the acceptance range of 0.80–1.25.ConclusionThe pharmacokinetic profiles of eslicarbazepine acetate oral 50 mg/mL suspension, 200mg tablet and 800mg tablet formulations were essentially similar, and the formulations can be considered bioequivalent.
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