One Step In Situ Co-Crystallization of Dapsone and Polyethylene Glycols during Fluidized Bed Granulation

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Chemical Engineering

Background:

• In situ co-crystallization is feasible in pharmaceutical processes like spray drying and hot melt extrusion.
• Previous research has not explored in situ co-crystallization for formulations where a polymer acts as a coformer.
• Co-crystal-in-excipient formulations offer enhanced drug properties.

Purpose of the Study:

• To investigate the use of fluidized bed granulation (FBG) for one-step in situ co-crystallization of dapsone (DAP) with polyethylene glycols (PEGs).
• To evaluate the pharmaceutical properties of the resulting co-crystal granules.
• To compare FBG with solvent evaporation (SE) for producing API-polymer co-crystals.

Main Methods:

• Dapsone-PEG co-crystals were initially prepared using solvent evaporation (SE) at a 55:45 w/w ratio.
• Fluidized bed granulation (FBG) was employed to produce co-crystal granules using microcrystalline cellulose and hydroxypropyl methyl cellulose.
• The purity, flow properties, and tableting properties of the FBG-produced granules were analyzed and compared to SE-produced co-crystals.

Main Results:

• FBG successfully produced dapsone-PEG co-crystal granules, achieving higher purity than SE.
• Granules containing dapsone-PEG 400 co-crystals could be prepared using FBG without an additional binder.
• FBG-produced DAP-PEG co-crystal granules exhibited superior flow and tableting properties compared to SE-produced counterparts.

Conclusions:

• In situ co-crystallization via FBG is an effective method for producing API-polymer co-crystals.
• FBG enhances the purity and pharmaceutical properties of co-crystal formulations.
• This approach offers a promising one-step process for advanced drug delivery systems.