PVP solid dispersions for the controlled release of furosemide from a floating multiple-unit system

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Biopharmaceutics

Background:

• Poor oral bioavailability of furosemide (FUR) is attributed to its limited residence time in the upper gastrointestinal tract.
• Furosemide's low water solubility further complicates achieving effective therapeutic concentrations.
• Developing advanced drug delivery systems is crucial for enhancing the efficacy of poorly soluble drugs.

Purpose of the Study:

• To develop and optimize an in vitro multiple-unit floating system for furosemide.
• To increase the gastric residence time of furosemide for improved oral absorption.
• To overcome the challenges of incomplete drug release due to furosemide's low solubility.

Main Methods:

• Formulation of multiple-unit floating systems incorporating furosemide.
• Preparation and evaluation of furosemide/polyvinylpyrrolidone (FUR/PVP) solid dispersions.
• Inclusion of solid dispersion in both core and membrane of floating units.
• Physicochemical characterization to assess drug state and dissolution.

Main Results:

• A 1:5 FUR/PVP solid dispersion in both core and membrane achieved complete drug release over 8 hours.
• The amorphous state of furosemide in the solid dispersion significantly enhanced drug solubility and dissolution rate.
• The developed system demonstrated a desired release profile suitable for extended gastric residence.

Conclusions:

• The optimized multiple-unit floating system effectively enhances furosemide's dissolution and release profile.
• Utilizing solid dispersion technology is a viable strategy to improve the bioavailability of poorly soluble drugs like furosemide.
• This approach offers a promising strategy for developing advanced oral drug delivery systems with prolonged gastric residence time.