Investigation into mixing capability and solid dispersion preparation using the DSM Xplore Pharma Micro Extruder

Area of Science:

• Pharmaceutical Technology
• Materials Science

Background:

• Hot-melt extrusion (HME) is crucial for developing solid dispersion formulations.
• Early-stage formulation screening requires efficient and scalable methods.

Purpose of the Study:

• To evaluate the DSM Xplore Pharma Micro Extruder as a tool for early-stage formulation screening in hot-melt extrusion.
• To assess the extruder's capability for dispersive and distributive mixing using various polymers and sodium chloride (NaCl).

Main Methods:

• Investigated dispersive and distributive mixing using Soluplus, copovidone, or basic butylated methacrylate copolymer with NaCl in 5g batches.
• Prepared eleven types of solid dispersions using diverse drugs and carriers in 5g batches, following established literature protocols.

Main Results:

• Particle size reduction was rapid (1 min) and independent of polymer type, influenced by screw speed and recirculation time.
• Specific mechanical energy (SME) showed an inverse relationship with particle size, with higher SME values compared to large-scale extruders.
• Achieved European Pharmacopoeia uniformity criteria for NaCl content after 1 min recirculation at 200 rpm, indicating successful distributive mixing.
• Differential scanning calorimetry, powder X-ray diffractometry, and in-vitro dissolution confirmed successful preparation of all solid dispersion systems.

Conclusions:

• The DSM Xplore Pharma Micro Extruder is validated as a valuable small-scale tool for screening solid dispersion formulations.
• The extruder effectively characterizes material properties and formulation performance at an early stage of development.