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Comparative bioavailability study with two chlorpropamide tablet formulations in healthy volunteers
Marcia Aparecida da Silva1, Fabiana D Mendes, Rogério Antonio de Oliveira
1Department of Pharmacology, Faculty of Medical Sciences, State University of Campinas, Campinas, SP, Brazil.
Arzneimittel-Forschung
|October 31, 2007
Summary
This study assessed the bioequivalence of two chlorpropamide 250 mg tablets in healthy volunteers. The test formulation was found to be bioequivalent to the reference, meeting FDA standards for absorption.
Area of Science:
- Pharmacokinetics
- Drug formulation analysis
- Clinical pharmacology
Background:
- Chlorpropamide is an oral hypoglycemic agent used in type 2 diabetes management.
- Bioequivalence studies are crucial for generic drug approval and ensuring therapeutic equivalence.
- Assessing the pharmacokinetic profile of different chlorpropamide formulations is essential for patient safety and efficacy.
Purpose of the Study:
- To evaluate the bioequivalence of a 250 mg chlorpropamide tablet (test formulation) compared to a reference product.
- To determine if the rate and extent of absorption of the test chlorpropamide formulation are comparable to the reference formulation.
- To provide data supporting the interchangeability of the two chlorpropamide tablet formulations.
Main Methods:
- An open-label, randomized, two-period crossover study was conducted in 36 healthy adult volunteers.
- Plasma chlorpropamide concentrations were measured over 72 hours using liquid chromatography-tandem mass spectrometry (LC-MS-MS).
- Key pharmacokinetic parameters including AUC(0-72h), AUC(inf), and C(max) were analyzed.
Main Results:
- The limit of quantification for plasma chlorpropamide was 0.1 microg/mL.
- Geometric mean ratios (Test/Reference) for C(max), AUC(0-72h), and AUC(inf) were 93.99%, 92.45%, and 90.30%, respectively.
- The 90% confidence intervals (CI) for these ratios fell within the 80-125% bioequivalence range.
Conclusions:
- The 250 mg chlorpropamide tablet (test formulation) demonstrated bioequivalence to the reference product.
- The study concluded that both the rate and extent of absorption are comparable between the two formulations.
- The findings support the use of the test formulation as a therapeutically equivalent alternative to the reference chlorpropamide tablet.
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