Hot Melt Extrusion: Meeting The Solubility Challenge

By David B. Hedden and Monthira Reodacha, UPM Pharmaceuticals

The formulation of poorly soluble compounds for oral delivery is a growing and often daunting challenge in drug development. As innovator pipelines of developmental drugs become richer, there is a strong trend toward candidates with low aqueous solubility. Approximately 90% of drug candidates today fall into two low aqueous solubility categories of the Biopharmaceutics Classification System (BCS), Class II and Class IV.¹ Low solubility has the consequent risk of low intrinsic bioavailability, requiring additional formulation efforts that can delay the overall development process.

A specialized technology, such as hot melt extrusion (HME), presents new opportunities to improve bioavailability through solubility enhancement. Interest in HME is growing rapidly for developing bio-enhanced formulations that increase the efficacy of these compounds. We shall discuss how development-stage pharma companies can quickly evaluate the feasibility of processes such as HME for improving compound solubility and bioavailability.