Amorphous solid dispersions (ASDs) have emerged over the past decade as the leading formulation technology for low solubility compounds because they enhance bioavailability through two primary mechanisms: 1) increasing concentration of solvated drug, and 2) formation of drug-polymer colloids, which lead to increased rates of diffusion through the unstirred water layer and a rapid resupply of solvated drug at the epithelial surface.
In this work, we characterized colloids formed in biorelevant by polymers typically used in ASDs media and identified intrinsic differences in size and density. Based on these results, we evaluated the degree to which four model compounds partition into polymer colloids and consider their effect on the colloidal species.
Finally, we produced spray dried dispersion and hot melt extrusion formulations for one of the model compounds and compared the extent of solubilization and colloidal species formation as both neat ASD powders and as formulated tablets in biorelevant dissolution.
Learning Objectives:
Upon completion, participants will understand how polymer choice and manufacturing technology can affect speciation of amorphous solid dispersions.
Upon completion, participants will understand how particle properties can affect the performance of amorphous solid dispersion oral dosage forms.
Upon completion, participants will gain insight into the interplay between the development of drug product intermediates and drug products
