Rapid Development of Amorphous Solid Dispersions (ASDs) for Improved Bioavailability

26 September 2022 12:15 - 12:45

  • Learn how oncology pipelines are dominated by poorly water-soluble compounds
  • Understand how ASD drug products can enhance bioavailability and overcome pH effects of poorly soluble weak base drugs
  • Learn how knowledge of key drug, polymer, and gastrointestinal properties can be combined with in vitro and in silico tools to develop ASD drug products without the need for reformulation or multiple studies
  • Describe key considerations driving effective selection of ASD formulations

Pharmaceutical pipelines are dominated by oncology indications. However, many oncology drugs are poorly soluble in gastrointestinal fluids, often resulting in drug-drug or food-drug interactions that limit oral bioavailability. Amorphous solid dispersion (ASD) is a leading technology for overcoming oral bioavailability issues. This talk will provide a background to the advantages in ASDs for delivering oncology drugs, and a background to using spray drying to develop ASDs. The talk further describes a case study of an ASD tablet of a weak base drug, acalabrutinib, that removed the pH effect observed with commercially marketed Calquence® at the human dose in dogs. ASD tablets outperformed Calquence 2.4-fold at high gastric pH with a 60% smaller dosage form size.

David Lyon, Sr. Fellow, Global Research, Lonza, Small Molecules