Comparative bioavailability of cefuroxime axetil suspension formulations administered with food in healthy subjects

Abstract

Objective:

To assess the comparative bioavailability of two formulations (250 mg/5 mL suspension) of cefuroxime axetil (CAS 64544-07-6), administered with food, 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 12 h post dose. Plasma cefuroxime axetil concentrations were analyzed by liquid chromatography coupled with tandem mass spectrometry (LC-MS-MS) with negative ion electrospray ionization using multiple reactions monitoring (MRM). From the cefuroxime axetil plasma concentration vs. time curves, the following pharmacokinetic parameters were obtained: AUC_last and C_max.

Results:

The limit of quantification was 0.1 μg/mL for plasma cefuroxime axetil analysis. The geometric mean and 90 % confidence interval CI of test/reference product percent ratios were: 106.1 %(100.8%–111.8%) for C_max, 109.4%(104.8 %–114.2%) for AUC_last.

Conclusion:

Since the 90% CI for AUC_lastand C_max ratios were within the 80–125%interval proposed by the US FDA, it was concluded that cefuroxime axetil (test formulation, 250 mg/5 mL suspension) was bioequivalent to a reference formulation under fed conditions, for both the rate and extent of absorption.

Key words

Antibacterial - CAS 64544-07-6 - Cefuroxime axetil, bioavailability, administration with food, pharmacokinetics - Tandem mass spectrometry, LC/MS/MS

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