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
- *Corresponding Author:
- Dr. Ney Carter C. Borges
24 Cesar Bierrenbach
Street Campinas, SP, Brazil
Postal Code: 13015-025
Phone : 55 19 3234-2834
Fax : 55 19 3234-2834
E-mail : [email protected]
Received Date: September 21, 2009; Accepted Date: October 31, 2009; Published Date: November 02, 2009
Citation: Moreira RF, Rigato HM, Borges BC, Sverdloff CE, Oliveira RA, et al. (2009) Effect of Hyperl ipemic 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.
A specific, fast and sensitive LC–MS/MS assay was d e- veloped for the determination of bupropion and its me- tabolite hydroxybupropion in human plasma using lidocaine as the internal standard. The limit of qu antifica- tion was 3.13 ng/ml for bupropion and 7.81 ng/ml fo r hydroxybupropion. The method was linear in the stud ied range of 3.13 – 400.00 ng/ml for bupropion and 7.81 – 1000 ng/ml for hydroxybupropion. This analytical me thod was applied to a comparative pharmacokinetic study, in which seventy eight volunteers (39 men and 39 femal e) aged between 18 and 50 years received a single oral dose of 150 mg of reference and test bupropion formulati on, in an open, two-period, balanced randomized, crossover pro- tocol. Group 1 received the medication without any addi- tional meal. Group two received a hyperlipemic meal 30 min before the medication. Based on the 90% confide nce interval of the individual ratios for C max and AUC 0-inf , it was concluded that the test formulation is bioequiv alent to the reference formulation with respect to the ra te and extent of absorption of both bupropion and hydroxybupropion and that food intake before the dr ug administration had no effect in the relative pharma coki- netic parameters. However, the hyperlipemic meal si gnifi- cantly increased the bupropion absorption.