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

Abstract

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.

Development and validation of a high‐performance liquid chromatography–tandem mass spectrometric method for simultaneous determination of bupropion, quetiapine and escitalopram in human plasma

“…Various analytical methods have been reported in the literature to detect each medication separately with their metabolites and/or in combination with other medications in rat and human plasma as well as urine samples. These include gas chromatography (GC; da Fonseca et al, 2013), capillary electrophoresis (CE; Deng et al, 2012), thin-layer chromatography (TLC; Soliman and Youssef, 2011), high-performance liquid chromatography (HPLC; Belal et al, 2008;Yeniceli and Dogrukol-Ak, 2010;Suryakant and Sadhana, 2012), liquid chromatography-mass spectrometry (LC/MS; Zhou et al, 2004;Raman et al, 2010;Choong et al, 2011), gas chromatography-mass spectrometry (GC/MS; Kakde et al, 2013), liquid chromatography-tandem mass spectrometry (LC/MS/MS; Moreira et al, 2009;Suresh et al, 2010;Fisher et al, 2012;Pan et al, 2012;Parekh et al, 2012) and ultra-performance liquid chromatographytandem mass spectrometry (UPLC/MS/MS) (Li et al, 2007;Tu et al, 2008;Denooz et al, 2010). However, no method has been reported to simultaneously determine BUP, ESC and QUE in plasma.…”

Recent Trends in Analytical Techniques for the Development of Pharmaceutical Drugs

“…• The purpose of this study was to develop a single-laboratory validated (SLV) method using high-performance liquid chromatography with different detectors. The method does not require any sample cleanup/preconcentration steps except centrifugation and filtration [46].…”

Role of Novel Hole Technology in Fast Dissolving Tablets

“…Post compression parameters: All the prepared tablets were subjected to various physical characteristics like Crushing strength, Friability, Thickness, Diameter, Hole depth, Disintegration time, Wetting time, Weight variation, Drug content [17][18][19][20][21][22][23][24][25][26][27][28][29][30][31][32][33][34][35].…”