Preparation and evaluation of famotidine polymorphs

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Pharmacology

Background:

• Drug polymorphism significantly impacts bioavailability and therapeutic efficacy.
• Famotidine, a widely used H2 receptor antagonist, exists in various polymorphic forms.
• Understanding famotidine polymorph behavior is crucial for optimizing drug delivery and therapeutic outcomes.

Purpose of the Study:

• To compare the drug release behavior of famotidine polymorphs prepared with different additives and solvents.
• To evaluate the stability, solubility, and in vivo antiulcer activity of selected famotidine polymorphs.
• To elucidate the impact of additives and solvents on famotidine polymorph characteristics and therapeutic performance.

Main Methods:

• Famotidine polymorphs were prepared using the solvent evaporation method with polyvinyl pyrrolidone (PVP), Tween 80, polyethylene glycol, and methanol.
• Physicochemical characterization involved Differential Scanning Calorimetry (DSC), Fourier-Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM), and X-ray Diffraction (XRD).
• Drug release kinetics were analyzed using zero-order, first-order, and Hixon-Crowel equations, followed by in vivo antiulcer activity assessment using the pylorus ligation model and antioxidant parameter estimation.

Main Results:

• Famotidine polymorphs prepared with 1% PVP exhibited optimal drug release and solubility.
• DSC indicated superior stability for PVP polymorphs, while FTIR confirmed the absence of drug-additive interactions in PVP formulations.
• In vivo studies revealed that famotidine PVP polymorphs demonstrated significantly better antiulcer and antioxidant activities compared to pure famotidine and famotidine methanol polymorphs.

Conclusions:

• Famotidine PVP polymorphs possess favorable dissolution behavior, enhanced stability, and lack of drug-additive interactions.
• The superior in vivo antiulcer and antioxidant activities of famotidine PVP polymorphs confirm their enhanced therapeutic efficacy.
• This study highlights the critical role of excipient selection in developing improved famotidine formulations with better bioavailability and therapeutic outcomes.