Ann Newman - Assessing the Performance of Amorphous Solid Dispersions

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      Publication Details (including relevant citation   information):

      A. Newman, G. Knipp, G. Zografi. J Pharm Sci   .2012,101(4), 1355-1377


      The characterization and performance of stable amorphous solid   dispersion systems were evaluated in 40 research papers reporting   active pharmaceutical ingredient (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),   and 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   centered on dissolution testing and equipment, content and amount   of dissolution media, sink or nonsink 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 versus fed conditions, and regional   differences in gastrointestinal (GI) content and volume. On the   basis of 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

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