Manufacturing and Bioprocessing
2019 PharmSci 360
Andrei Winkler, MSc, MBA
Thermo Fisher Scientific, New Jersey
Solubility enhancement is the main challenge in pharmaceutical development. Stabilizing the active pharmaceutical ingredient (API) in an amorphous state is one possibility to enhance its solubility. Co-milling of drug and highly porous silica with defined pore sizes proved to reach amorphous state and improve solubility of the drug (F. Monsuur et al., Int. J. Pharm., vol. 511, 2016.).
In this study a pharmaceutical twin-screw extruder is used to process the model drug itraconazole with mesoporous silica. Different screw configurations and process parameters were tested. The products were analyzed by DSC, XRD and SEM to confirm the amorphous state. The results show that a twin-screw extruder can successfully process the materials to reach amorphous state of API. Throughput, screw speed, temperature and screw configuration are key process parameters for this solvent-free amorphization technology.