Amorphous solid dispersion is a powerful approach for delivering poorly water soluble drugs. However, high drug loading of ASDs are challenging with respect to physical stability and drug release, which limits the maximum dose and the achievement of the desirable high exposure. In this work, counterions were incorporated with API model compound indomethacin (IMC), to ionize the API and influence the pH of the diffusion layer. Improvement of dissolution rate was systemically studied to show the facilitating effect of counterions in high drug load ASDs. These findings can help better design high drug load ASD using counterions for ionizable drugs.
Upon completion, participants will be able to understand the concept using counterions to facilitate the dissolution limited high drug loading amorphous solid dispersion of an ionizable compound.
Upon completion, participants will be able to carry out a rational designing of amorphous solid dispersion with counterions including selection of counterions and the desired amount.
Upon completion, participants will be able to interpret the chemical mechanism why the counterions facilitate the dissolution of amorphous solid dispersion.