Effect of food on the pharmacokinetic profile of eslicarbazepine acetate (BIA 2-093)

• Type: Article in International Scientific Journal
• Date: 2005

Authors

Maia, J (Author) Other; Vaz Da Silva, M (Author) FMUP; Almeida, L (Author) Other; Falcao, A (Author) Other; Silveira, P (Author) Other; Guimaraes, S (Author) Other; Graziela, P (Author) Other; soares-da-silva, p (Author) FMUP

Journal

The Journal is awaiting validation by the Administrative Services.

Title: Drugs in R and D

Vol. 6

Pages: 201-206

ISSN: 1174-5886

Indexing

Scopus - 46 Citations

Other information

Authenticus ID: P-007-DNT

DOI: 10.2165/00126839-200506040-00002

Abstract (EN): Objective: To investigate the effect of food on the pharmacokinetics of eslicarbazepine acetate (BIA2-093), a new voltage-gated sodium channel antagonist. Material and methods: Single-centre, open-label, randomised, two-way cross-over study in 12 healthy subjects. The study consisted of two consecutive treatment periods separated by a washout of 14 days or more. In each of the study periods subjects were administered a single dose of eslicarbazepine acetate 800mg following either a standard high-fat content meal or 10 hours of fasting. Results: Eslicarbazepine acetate was rapidly and extensively metabolised to BIA 2-005. Maximum BIA 2-005 plasma concentrations (C max) in fed (test) and fasting (reference) conditions were, respectively, 12.8 ± 1.8 ¿g/mL and 11.3 ± 1.9 ¿g/mL, and the areas under the plasma concentration time curve from 0 to infinity (AUC¿) were, respectively, 242.5 ± 32.1 ¿g ¿ h/mL and 243.6 ± 31.1 ¿g ¿ h/mL (arithmetic mean ± SD). The point estimate (PE) and 90% confidence interval (90% CI) of the test/reference Cmax geometric mean ratio were 1.14 and 1.04, 1.25, respectively; for the AUC¿ ratio, the PE and 90% CI were 1.00 and 0.95, 1.04, respectively. Bioavailability of eslicarbazepine acetate administered in fed and fasting conditions was similar and bioequivalence is accepted for both AUC¿ and Cmax because the 90% CI lies within the acceptance range of 0.80-1.25. No statistically significant differences were found in time of occurrence of C max. Conclusion: The presence of food had no significant effect on the pharmacokinetics of eslicarbazepine acetate and therefore this new voltage-gated sodium channel antagonist may be administered without regard to meals.

Language: English

Type (Professor's evaluation): Scientific