Screening for pharmaceutical cocrystals using the supercritical fluid enhanced atomization process

PAT-based design of agrochemical co-crystallization processes: A case-study for the selective crystallization of 1:1 and 3:2 co-crystals of p-toluenesulfonamide/triphenylphosphine oxide

“…Co-crystallization can be an effective crystal engineering approach for modifying the crystal structure and properties of an active ingredient [8], [9]. However, many of the current methods used to isolate co-crystal forms such as neat and liquid assisted grinding [10], [11], slurry conversion [12], [13], supercritical fluid enhanced atomization [14], and evaporative co-crystallization [13], [15], [16] cannot be scaled to industrial production capacity. Cooling crystallization is perhaps the most viable route to scale-up, yet there are only a few studies that have explored this method to isolate co-crystals [17]- [19].…”

Pharmaceutical Cocrystals: An Overview

“…Grinding methods are of two types: neat grinding and solvent drop grinding [85,86] . Some newly emerging methods used for the formation of cocrystals are ultrasound assisted solution method [87,88] , supercritical fluid atomization technique [46,89] , spray drying technique [90,91] , hot melt extrusion technique [92,93] .…”

“…In relative humidity stress, automated water sorption/desorption studies are performed to determine the effect of water on the formulation. Several researchers studied the behaviour of cocrystals under relative humidity stress conditions [41,[45][46][47] . Cocrystals of glutaric acid and 2-[4-(4-chloro-2-fluorphenoxy)phenyl]pyrimidine-4-carboxamide showed 0.08% moisture at high 95% RH and cocrystals were found stable at different conditions [41] .…”

“…Cocrystals are prepared by atomizing this solution with the help of atomizer. In supercritical antisolvent (SAS) method, the cocrystals are prepared from solution by the antisolvent effect of supercritical fluid [46,89,105] .…”

“…Scanning electron microscope is the instrument used to determine the particle size and morphological analysis of cocrystals. A high energy electron beams scan the atoms that provide the information about the sample surface's topography [12,45,46] . Dissolution study is used to determine the amount of drug release with time in dissolution medium and predict the in vivo performance of the formulation.…”