Development and scale-up of bio-enhanced formulation via hot melt extrusion for toxicology study and phase I clinical trials: a case study
To address the challenges posed by new drug candidates showing unfavourable bio-pharmaceutical characteristics such as poor water solubility and/or low permeability, the development of advanced drug delivery systems must be taken into consideration not only for clinical trials but also much earlier in preclinical studies.
This study presents the adopted strategy to develop and scale-up an amorphous solid dispersion of a poorly soluble and low permeable drug (Compound A) enabling to conduct the toxicology studies in dog and the formulation development for first time in human (FTIH).
The optimisation of hot melt extrusion (HME) formulation composition and process and the scale-up were performed to achieve the following objectives:
- Assessment of drug load and physicochemical stabilisation of extrudate
- Preparation of HME formulation at larger scale to support enabling Phase 1 general toxicology studies in dog
- Providing HME formulation composition and process suitable to be used for FTIH
Recently presented at AAPS 2017 by our expert Cesare Di Palma, in collaboration with Sunesis, download your copy of this scientific poster and learn more.