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Green production of cocrystals using a new solvent-free approach by spray congealing
Pharmaceutical cocrystals are used as a strategy to overcome poor physicochemical properties of drugs.聽The use of cocrystals in the pharmaceutical industry remains to be fully exploited due, in part, to the scarcity of suitable large-鈥媠cale production methods and lack of robust and cost-鈥媏ffective processes.聽To overcome these challenges, spray congealing was used for the first time in the preparation of cocrystals.聽The work considered a feasibility study, followed by a design of experiments to assess the impact of varying atomization and cooling-鈥媟elated process parameters on cocrystal formation, purity, particle size, shape and bulk powder flow properties.聽It was demonstrated that spray congealing could be used to produce cocrystals.聽The thermal analysis and X-鈥媟ay results of the spray-鈥媍ongealed products were different from the pure components or physical mixtures and were aligned with those reported for the same cocrystals systems produced by other techniques.聽Cocrystal particles were compact and spherical consisting of aggregates of individual cocrystals entangled or adhered with each other.聽
From the design of experiments, the results demonstrated that varying the process parameters did not influence cocrystal formation, but had an impact on cocrystal purity.聽Moreover, it was demonstrated that cocrystal particle properties can be adjusted, in situ, by varying atomization and cooling efficiency, in order to produce particles more suited for incorporation in final dosage forms such as tablets.