Enabling or Not? – A Journey of FIH Formulation Development for a Poorly Water-Soluble Deuterated Weak Basic Development Candidate

Bioperformance driven and physico-chemical properties-based formulation development
Spring effect in conventional formulation - Evaluation and selection of acidic excipients to provide a micro-environment to offer higher solubility in gastric fluid
Parachute effect in conventional formulation - Evaluation and selection of polymers to sustain the dissolved molecules in intestine fluid
Prototype formulation development using pentagastrin treated dog exposures to help select the best performer
Enabling formulation, Amorphous solid dispersion formulation, development to be a backup option
Stability evaluation using ASAPprime® for shelf-life determination and packaging configuration selection