Non-aqueous formulations for ram and screen extrusion-spheronisation.

Area of Science:

• Pharmaceutical Technology
• Materials Science

Background:

• Extrusion-spheronisation (E-S) is a key pharmaceutical process for pellet production.
• Non-aqueous formulations offer advantages but require specific binders.
• Cellulose derivatives are widely used in pharmaceutical formulations.

Purpose of the Study:

• To investigate non-aqueous cellulose-based formulations for extrusion-spheronisation (E-S).
• To identify suitable sticky liquid binders for non-aqueous paste preparation.
• To evaluate pellet quality using different extrusion methods and active pharmaceutical ingredient loading.

Main Methods:

• Preparation of non-aqueous pastes using hydroxypropyl cellulose (HPC) in isopropyl alcohol (IPA).
• Testing pastes with ram and laboratory roller screen extruders to simulate batch and manufacturing conditions.
• Incorporation of calcium carbonate as a model active pharmaceutical ingredient (API).

Main Results:

• A 10 wt% HPC/IPA solution was identified as an effective sticky liquid binder.
• Pellets with acceptable size and shape distributions were achieved using Avicel® HFE-102 NF/HPC/IPA (ram E-S) and Avicel® RC-591/HPC/IPA (screen E-S).
• Both formulations successfully produced pellets with up to 50 wt% calcium carbonate loading.

Conclusions:

• Non-aqueous cellulose-based formulations are viable for extrusion-spheronisation.
• Specific Avicel® grades combined with HPC/IPA binder are suitable for producing pharmaceutical pellets.
• Further optimization is needed to improve yields for high API loading.