Likun Wang
Jiangsu Hengrui Medical Co. Ltd, China
Title: Small molecule enabling formulation development: A super-saturation perspective
Biography
Biography: Likun Wang
Abstract
Over 90% of small molecule NMEs are poorly water soluble and supersaturation drug delivery systems, i.e. amorphous solid dispersions, Nanosuspensions and lipid based drug delivery systems, are the main strategy to enhance bioavailability. Supersaturation can also be included due to pH change during GI transition for both free form and pharmaceutical salt. Supersaturation can also increase flux rate by creating higher API concentration gradient in the GI tract. Therefore, it is critical to obtain a good understanding of the kinetics of supersaturation process both in-vitro and in-vivo. As supersturation can occur rapidly and it can be very sensitive to pH, hydrodynamics, a real-time concentration monitoring, multi-channel and miniaturized setup was used to investigate the kinetics of supersaturation. The results were also compared with HPLC analysis for validation purpose. The in-vitro data was also used to model and simulation supersaturation process by GastroPlus to further understand the impact of supersaturation on biopharmaceutics. Case studies of how supersaturation studies can help with formulation design to enhance bioavailability in different situations were given. Finally, the future direction of supersaturation investigations and applications was also shared.