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.