An in-vivo-in-vitro correlation for the bioavailability of frusemide tablets

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery and Formulation

Background:

• Frusemide is a critical diuretic medication.
• Assessing oral drug bioavailability is essential for therapeutic efficacy.
• Dissolution testing serves as a surrogate for in vivo performance.

Purpose of the Study:

• To evaluate the dissolution behavior of various frusemide tablet formulations.
• To establish a correlation between in vitro dissolution and in vivo bioavailability of frusemide.
• To validate dissolution testing as a predictive tool for frusemide oral absorption.

Main Methods:

• Utilized the USP rotating basket apparatus for dissolution testing.
• Employed pH 5.0 buffer at 37°C as the dissolution medium.
• Compared dissolution profiles of four commercial and two experimental frusemide tablet formulations.

Main Results:

• A significant linear relationship was observed between the percentage of frusemide dissolved in 30 minutes and its relative bioavailability.
• The observed bioavailability range was 76-97% relative to an oral solution.
• Predicted bioavailability values showed a maximum deviation of only 2% from measured values.

Conclusions:

• In vitro dissolution testing of frusemide tablets effectively predicts in vivo bioavailability.
• The established linear correlation supports the use of dissolution profiles for quality control and formulation optimization.
• This predictive model enhances the development of bioequivalent frusemide formulations.