A method for improving the properties of famotidine

Area of Science:

• Pharmaceutical Science
• Crystal Engineering
• Drug Delivery

Background:

• Famotidine (FMT) is a BCS Class III drug with low permeability, limiting its therapeutic efficacy.
• Crystal engineering offers strategies to modify drug properties, including permeability.
• Developing novel cocrystals is crucial for improving the bioavailability of poorly permeable drugs.

Purpose of the Study:

• To synthesize a stable salt cocrystal of famotidine (FMT) using m-nitrobenzoic acid (MNBA) as a coformer.
• To characterize the physicochemical properties of the novel FMT-MNBA cocrystal.
• To evaluate the impact of cocrystallization on the solubility and permeability of famotidine.

Main Methods:

• Cocrystallization of famotidine with m-nitrobenzoic acid.
• Characterization using scanning electron microscopy, DSC, TGA, FTIR, and XRD (powder and single crystal).
• Assessment of solubility and permeability of the synthesized cocrystal.

Main Results:

• A stable 1:1 salt cocrystal of famotidine-m-nitrobenzoic acid (FMT-MNBA) was successfully synthesized and structurally characterized.
• The FMT-MNBA cocrystal exhibited improved permeability compared to free famotidine.
• The study demonstrated the potential of crystal engineering for enhancing drug permeability.

Conclusions:

• The synthesized FMT-MNBA salt cocrystal represents a viable strategy for improving the permeability of BCS Class III drugs.
• This crystal engineering approach provides a valuable method for developing low-permeability drugs.
• Further research into cocrystal formation can advance the development of more effective pharmaceutical formulations.