The application of twin screw extrusion (TSE) as a scalable and green process for the manufacture of cocrystals was investigated. Four model cocrystal forming systems, Caffeine-Oxalic acid, Nicotinamide-trans cinnamic acid, Carbamazepine-Saccharin, and Theophylline-Citric acid, were selected for the study. The parameters of the extrusion process that influenced cocrystal formation were examined. TSE was found to be an effective method to make cocrystals for all four systems studied. It was demonstrated that temperature and extent of mixing in the extruder were the primary process parameters that influenced extent of conversion to the cocrystal in neat TSE experiments. In addition to neat extrusion, liquid-assisted TSE was also demonstrated for the first time as a viable process for making cocrystals. Notably, the use of catalytic amount of benign solvents led to a lowering of processing temperatures required to form the cocrystal in the extruder. TSE should be considered as an efficient, scalable, and environmentally friendly process for the manufacture of cocrystals with little to no solvent requirements.
The application of twin screw extrusion (TSE) in the scale-up of cocrystal production was investigated by using AMG 517-sorbic acid as a model system. Extrusion parameters that influenced conversion to the cocrystal such as temperature, feed rate and screw speed were investigated. Extent of conversion to the cocrystal was found to have a strong dependence on temperature and a moderate dependence on feed rate and screw speed. Cocrystals made by the TSE process were found to have superior mechanical properties than solution grown cocrystals. Additionally, moving to a TSE process eliminated the need for solvent.
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