Abstract
Objective:
To assess the comparative bioavailability of two formulations (16 mg tablet) of betahistine
(CAS 5579-84-0) in 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 for up to 36 h post dose.
Plasma 2-pyridylacetic acid concentrations were analyzed by liquid chromatography
coupled with tandem mass spectrometry (LC-MS-MS) with positive ion electrospray ionization
using multiple reaction monitoring (MRM). From the 2-pyridylacetic acid plasma concentration
vs. time curves, the following pharmacokinetic parameters were obtained for AUClast and Cmax.
Results:
The limit of quantification was 4 ng/mL for plasma 2-pyridylacetic acid analysis.
The geometric mean and 90% confidence interval (CI) of test/reference percent ratios
were: 98.94% (92.21% −106.16%) for Cmax( 95.42% (91.74% −99.25%) for AUClast.
Conclusion:
Since the 90% CI for Cmax and AUCs ratios were all within the 80–125% interval proposed by the US Food and
Drug Administration Agency, it was concluded that the test formulation is bioequivalent
to the reference for both the rate and the extent of absorption.
Key words
Betahistine, bioequivalence, pharmacokinetics - CAS 5579-84-0 - LC-MS/MS - 2-Pyridylacetic
acid
