Comparative bioavailability study with two gemfibrozil tablet formulations in healthy volunteers.
OBJECTIVE
To assess the bioequivalence of gemfibrozil (CAS 25812-30-0) 900 mg tablet formulation from EMS Farmaceutica as test formulation versus a 900 mg tablet formulation as reference in 36 healthy volunteers of both sexes.


METHODS
The study was conducted using an open, randomized, two-period crossover design with a 1-week washout interval. Plasma samples were obtained over a 24-h period. Plasma gemfibrozil concentrations were analyzed by liquid chromatography coupled to tandem mass spectrometry (LC-MS-MS) with negative ion electrospray ionization using multiple reaction monitoring (MRM). From the gemfibrozil plasma concentration vs time curves, the following pharmacokinetic parameters were obtained: AUClast, AUC(0-inf) and Cmax.


RESULTS
The limit of quantification was 0.05 microg/mL for plasma gemfibrozil analysis. The geometric mean and respective 90% confidence interval (CI) of Test/Reference percent ratios were 90.29 (81.39-100.17) for Cmax, 96.26 (90.33-102.59) for AUClast, 96.04 (90.21-102.23) for AUC(0-24 h) and 96.62 (90.82-102.78) for AUC(0-infinity).


CONCLUSIONS
Since the 90% CI for AUClast, AUC(0-inf) and Cmax, ratios were within the 80-125% interval proposed by the U.S. FDA, it was concluded that gemfibrozil 900 mg tablet (test formulation) was bioequivalent to the 900 mg tablet reference formulation for both rate and extent of absorption.
Borges
Ney Carter do C
NC
Department of Pharmacology, State University of Campinas, Campinas, SP, Brazil.
Mendes
Gustavo Duarte
GD
Barrientos-Astigarraga
Rafael E
RE
Zappi
Eduardo
E
Mendes
Fabiana Duarte
FD
De Nucci
Gilberto
G
D000293:Adolescent; D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D005260:Female; D015248:Gemfibrozil / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D013058:Mass Spectrometry; D008875:Middle Aged; D013607:Tablets
D000960:Hypolipidemic Agents; D013607:Tablets; D015248:Gemfibrozil