Influence of Drug Properties, Formulation Composition, and Processing Parameters on the Stability and Dissolution...

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Polymeric amorphous solid dispersions (ASDs) are crucial for improving oral bioavailability of poorly water-soluble drugs.
• Successful ASD tablet formulation demands optimization of composition and compaction parameters.

Purpose of the Study:

• To investigate the performance of polymeric-based ASD tablets using model drugs with different glass-forming abilities.
• To evaluate the impact of formulation variables and compaction on mechanical properties, disintegration, and supersaturation.

Main Methods:

• Prepared ASDs with indomethacin (good glass former) and carbamazepine (poor glass former) at various API-to-polyvinylpyrrolidone ratios.
• Formulated tablets with different ASD loadings and assessed compaction effects on physical and dissolution properties.
• Evaluated performance immediately after preparation and after storage under controlled conditions.

Main Results:

• Solid-state analysis confirmed amorphous state and API-polymer interactions.
• Dissolution was influenced by drug loading, polymer content, and compaction; carbamazepine showed faster release but reduced stability.
• Indomethacin and carbamazepine ASD tablets exhibited distinct responses to formulation and storage conditions.

Conclusions:

• API physicochemical properties, particularly glass-forming ability, critically influence ASD tablet physical stability and dissolution performance.
• Tailored formulation and processing strategies are essential for developing robust ASD-based drug delivery systems.