One-step continuous extrusion process for the manufacturing of solid dispersions.

Area of Science:

• Materials Science
• Pharmaceutical Technology
• Drug Delivery Systems

Background:

• Amorphous solid dispersions are crucial for improving the bioavailability of poorly soluble drugs.
• Hot melt extrusion (HME) is a promising technique for manufacturing amorphous solid dispersions.
• Novel inorganic carriers are needed to enhance the stability and performance of amorphous solid dispersions.

Purpose of the Study:

• To evaluate synthetic magnesium aluminometasilicate (MAS) as a novel inorganic carrier for indomethacin (IND) solid dispersions.
• To investigate the performance of MAS in hot melt extrusion (HME) processing.
• To assess the physicochemical properties and stability of IND/MAS solid dispersions.

Main Methods:

• Hot melt extrusion (HME) using a twin-screw extruder with varying IND/MAS ratios (20%, 30%, 40%).
• Physicochemical characterization including SEM, DSC, XRPD, AFM, and FTIR.
• Dissolution rate studies and accelerated stability testing (40°C, 75% RH).

Main Results:

• SEM, DSC, and XRPD confirmed amorphous IND within the porous MAS network in all formulations.
• AFM and FTIR indicated a single-phase amorphous system with intermolecular hydrogen bonding.
• IND/MAS extrudates exhibited enhanced dissolution rates (100% release within 1 hour) and maintained physical stability for 12 months under accelerated conditions.

Conclusions:

• Synthetic MAS is a highly effective inorganic carrier for developing stable amorphous solid dispersions of indomethacin via HME.
• MAS enhances the dissolution rate of indomethacin, improving its bioavailability.
• The developed solid dispersions demonstrate excellent physical stability, even at high drug loadings.