The use of excipients other than polymers for enhancing the physical stability of amorphous active pharmaceutical ingredients (APIs) has largely been unexplored. We investigated several organic acids (oxalic, tartaric, citric and succinic acid) for the purpose of stabilizing a weakly basic API, ketoconazole (KTZ), in the amorphous state.
Extruded milled griseofulvin (GF, drug) suspensions along with additional polymers.
• Formed HPC-based nano composite and Soluplus-based amorphous solid dispersion (ASD).
• Compared dissolution response under non-supersaturating conditions (low drug dose).
• Drug nanocrystal in the nano composite dissolved faster than amorphous drug in ASD.
• Showed the impact of drug particle size and extrudate (matrix) size on dissolution.