Effect of Hyperlipemic Food on the Comparative Bioavailability of Two Bupropion Formulations after Administration of a Single Oral Dose of 150 mg in Healthy Human Volunteers

A specific, fast and sensitive LC–MS/MS assay was developed for the determination of bupropion and its metabolite hydroxybupropion in human plasma using lidocaine as the internal standard. The limit of quantification was 3.13 ng/ml for bupropion and 7.81 ng/ml for hydroxybupropion. The method was linear in the studied range of 3.13 – 400.00 ng/ml for bupropion and 7.81 – 1000 ng/ml for hydroxybupropion. This analytical method was applied to a comparative pharmacokinetic study, in which seventy eight volunteers (39 men and 39 female) aged between 18 and 50 years received a single oral dose of 150 mg of reference and test bupropion formulation, in an open, two-period, balanced randomized, crossover protocol. Group 1 received the medication without any additional meal. Group two received a hyperlipemic meal 30 min before the medication. Based on the 90% confidence interval of the individual ratios for C max and AUC 0-inf , it was concluded that the test formulation is bioequivalent to the reference formulation with respect to the rate and extent of absorption of both bupropion and hydroxybupropion and that food intake before the drug administration had no effect in the relative pharmacokinetic parameters. However, the hyperlipemic meal significantly increased the bupropion absorption. *Corresponding author: Ney Carter C. Borges, 24 Cesar Bierrenbach Street Campinas, SP, Brazil, Postal Code: 13015-025, Tel/Fax: 55 19 3234-2834; E-mail: [email protected] Received September 21, 2009; Accepted October 31, 2009; Published November 02, 2009 Citation: Moreira RF, Rigato HM, Borges BC, Sverdloff CE, Oliveira RA, et al. (2009) Effect of Hyperlipemic Food on the Comparative Bioavailability of Two Bupropion Formulations after Administration of a Single Oral Dose of 150 mg in Healthy Human Volunteers. J Bioequiv Availab 1: 103-111. doi:10.4172/jbb.1000016 Copyright: © 2009 Moreira RF, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Effect of Hyperlipemic Food on the Comparative Bioavailability of Two Bupropion Formulations after Administration of a Single Oral Dose of 150 mg in Healthy Human Volunteers Roberto F. Moreira, Hamilton M. Rigato, Bruno C. Borges, Carlos E. Sverdloff, Rogério A. Oliveira, Ronilson A. Moreno, Ney C. Borges* Department of Medical Clinic, State University of Campinas, Campinas/SP, Brazil College of Medicine, Pontificia Universidade Católica, 290 Dr. José Ermirio de Moraes Sq., Sorocaba, SP, Brazil Synchrophar Assessoria e Desenvolvimento de Projetos Clínicos, Campinas, SP, Brazil Department of Pharmacology, State University of Campinas, Campinas/SP, Brazil