Evaluation of amorphous solid dispersion properties using thermal analysis techniques.

ABSTRACT

Amorphous solid dispersions are an increasingly important formulation approach to improve the dissolution rate and apparent solubility of poorly water soluble compounds. Due to their complex physicochemical properties, there is a need for multi-faceted analytical methods to enable comprehensive characterization, and thermal techniques are widely employed for this purpose. Key parameters of interest that can influence product performance include the glass transition temperature (T(g)), molecular mobility of the drug, miscibility between the drug and excipients, and the rate and extent of drug crystallization. It is important to evaluate the type of information pertaining to the aforementioned properties that can be extracted from thermal analytical measurements, in addition to considering any inherent assumptions or limitations of the various analytical approaches. Although differential scanning calorimetry (DSC) is the most widely used thermal analytical technique applied to the characterization of amorphous solid dispersions, there are many established and emerging techniques which have been shown to provide useful information. Comprehensive characterization of fundamental material descriptors will ultimately lead to the formulation of more robust solid dispersion products.