Enhancing bioavailability through thermal processing

Formulation intervention, through the application of processing technologies, is a requirement for enabling therapy for the vast majority of drugs. Without these enabling technologies, poorly soluble drugs may not achieve therapeutic concentrations in the blood or tissue of interest. Conversely, freely soluble and/or rapidly cleared drugs may require frequent dosing resulting in highly cyclic tissue concentrations. During the last several years, thermal processing techniques, such as melt mixing, spray congealing, sintering, and hot-melt extrusion, have evolved rapidly and several new technologies, specifically dry powder coating, injection molding, and KinetiSol® dispersing, have been adapted to the pharmaceutical arena. An examination of the contemporary literature is reported in this review to summarize the variety and utility of thermal processing technologies employed for solubility enhancement and controlled release. In particular, the impact of these processing technologies on bioavailability, considered in terms of both rate and extent, has been reviewed.

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