Clinical Pharmacology & Biopharmaceutics
Open Access

Abstract

The characterization and performance of stable amorphous solid dispersion systems were evaluated in forty research papers reporting API dissolution and bioavailability from various systems containing polymers. The results from these studies were broadly placed into three categories: amorphous dispersions that improved bioavailability (~82% of the cases); amorphous dispersions possessing lower bioavailability than the reference material (~8% of the cases), amorphous dispersions demonstrating similar bioavailabilities as the reference material (~10% of the cases). A comparative analysis of these studies revealed several in vitro and in vivo variables that could have influenced the results. The in vitro factors compared primarily centred on dissolution testing and equipment, content and amount of dissolution media, sink or non-sink conditions, agitation rates, media pH, dissolution characteristics of the polymer, and dispersion particle size. The in vivo factors included reference materials used for bioavailability comparisons, animal species utilized, fasting vs. fed conditions, and regional differences in GI content and volume. Based on these considerations, a number of recommendations were made on issues ranging from the assessment of physical stability of API-polymer dispersions to in vivo GI physiological factors that require consideration in the performance evaluation of these systems.

Biography

Email: ann.newman@SeventhStreetDev.com