Comparative Bioavailability Study with Two Chlorpropamide Tablet Formulations in Healthy Volunteers

 

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Summary

Objective: The aim of this study was the assessment of the bioequivalence of two formulations (250 mg tablet) of chlor-propamide (CAS 94-20-2) in 36 healthy volunteers of both sexes.

Methods: The study was conducted using an open, randomized, two-period crossover design with a 3-week washout interval. Plasma samples were obtained over a 72-h period. Plasma chlorprop-amide concentrations were analyzed by liquid chromatography coupled to tandem mass spectrometry (LC-MS-MS) with positive ion electrospray ionization using multiple reaction monitoring (MRM). From the chlorpropamide plasma concentration vs time curves, the following pharmacokinetic parameters were obtained: AUC_0–72h, AUC_inf and C_max.

Results: The limit of quantification was 0.1 µg/mL for plasma chlorpropamide analysis. The geometric mean and respective 90 % confidence interval (CI) of Test/ Reference percent ratios were 93.99 % (87.11 %–101.41 %) for C_max, 92.45 % (85.96 %–99.44 %) for AUC_0–72h and 90.30 % (83.35 %–97.82 %) for AUC_0–inf.

Conclusion: Since the 90 % CI for AUC_0–72h, AUC_0–inf and C_max ratios were within the 80–125 % interval proposed by the US FDA, it was concluded that chlor-propamide 250 mg tablet (test formulation) was bioequivalent to the reference 250 mg tablet for of both the rate and extent of absorption.