Between 70% and 90% of new chemical entities in development, and approximately 40% of currently marketed drugs, fall into either Class II or IV of the Biopharmaceutics/Developability Classification System (BCS/DCS), where poor aqueous solubility limits oral bioavailability.1,2
The cause of this problem is that discovery strategies for new drugs favour molecules that are larger, more complex and lipophilic.
Poor solubility equates to drugs with low and variable absorption, a higher food-effect risk potential and unpredictable pharmacokinetics that can delay first-in-human studies or force late-stage formulation rework.
Amorphous solid dispersions (ASDs), in which a crystalline drug substance is converted to a higher-energy amorphous form and dispersed within a polymer carrier, have become the default strategy for these molecules.
Hibreniguss Terefe, PhD, Director of Product Development at Ardena, reports.
The two most popular manufacturing strategies to create ASDs are hot-melt extrusion (HME) and spray drying — although new particle-engineering and coprocessing approaches are emerging that continue to expand the development toolkit for difficult molecules.
Not yet a Subscriber?
This is a small extract of the full article which is available ONLY to premium content subscribers. Click below to get premium content on Manufacturing Chemist.
Subscribe now Already a subscriber? Sign in here.
