Homogeneity of amorphous solid dispersions - an example with KinetiSol^®

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Drug Delivery

Background:

• KinetiSol® is a solvent-free, high-shear technology for amorphous solid dispersions (ASDs).
• It addresses limitations of traditional methods like hot melt extrusion and spray drying for challenging drugs.
• Characterization of ASD homogeneity is crucial for process understanding.

Purpose of the Study:

• To evaluate the homogeneity and molecular miscibility of KinetiSol®-processed amorphous solid dispersions.
• To assess the KinetiSol® process's capability for uniform drug dispersion at low concentrations.
• To investigate the use of advanced analytical techniques for ASD characterization.

Main Methods:

• Utilized meloxicam, a BCS class II drug, processed with KinetiSol® at 1%, 5%, and 10% w/w.
• Assessed powder blend homogeneity and content uniformity.
• Employed SEM/EDS, Raman spectroscopy, and ssNMR for characterization.

Main Results:

• All KinetiSol® samples showed excellent content uniformity (≤2.0% RSD).
• SEM/EDS confirmed material homogeneity at a 25 µm² scale.
• Raman spectroscopy verified amorphous content, and ssNMR demonstrated high molecular miscibility (~200 nm scale) at 1% drug load.

Conclusions:

• The KinetiSol® process effectively produces homogeneous amorphous solid dispersions.
• Molecular-level drug-in-polymer dispersion is achieved even at low drug concentrations (1% w/w).
• KinetiSol® offers a viable solvent-free method for creating stable ASDs from challenging compounds.