The applications of the crystallization technique in the pharmaceutical industry as a purification and separation process for the isolation and synthesis of pure active pharmaceutical ingredients(API),co-crystals,cont...The applications of the crystallization technique in the pharmaceutical industry as a purification and separation process for the isolation and synthesis of pure active pharmaceutical ingredients(API),co-crystals,controlled release pulmonary drug delivery,and separation of chiral isomers are briefly discussed using a few case studies.The effect of process variables and solvent on the polymorphism and morphology of stavudine is discussed.The implementation of external control in the form of feedback and real-time optimal control using cooling and antisolvent crystallization of paracetamol in water-isopropyl alcohol is introduced.Two methods to prepare micronsized drug particles,namely,micro-crystallization and polymer-coated API-loaded magnetic nanoparticles for pulmonary drug delivery,are discussed.The significance of co-crystals in drug administration is highlighted using the theophylline-nicotinamide co-crystal system.Resolution of chloromandelic acid derivatives,a racemic compound,is achieved using direct crystallization and diastereomeric salts crystallization.The crystal structures of diastereomeric salts of chloromandelic acid and phenylethylamine are determined.The structure comparison between the less soluble and more soluble salts shows that weak interactions such as CH/πinteractions and van der Waals forces contribute to chiral recognition when the hydrogen bonding patterns are similar.展开更多
基金The financial support of Natural Sciences and Engineering Council Canada(NSERC)Canada Foundation for Innovation(CFI)。
文摘The applications of the crystallization technique in the pharmaceutical industry as a purification and separation process for the isolation and synthesis of pure active pharmaceutical ingredients(API),co-crystals,controlled release pulmonary drug delivery,and separation of chiral isomers are briefly discussed using a few case studies.The effect of process variables and solvent on the polymorphism and morphology of stavudine is discussed.The implementation of external control in the form of feedback and real-time optimal control using cooling and antisolvent crystallization of paracetamol in water-isopropyl alcohol is introduced.Two methods to prepare micronsized drug particles,namely,micro-crystallization and polymer-coated API-loaded magnetic nanoparticles for pulmonary drug delivery,are discussed.The significance of co-crystals in drug administration is highlighted using the theophylline-nicotinamide co-crystal system.Resolution of chloromandelic acid derivatives,a racemic compound,is achieved using direct crystallization and diastereomeric salts crystallization.The crystal structures of diastereomeric salts of chloromandelic acid and phenylethylamine are determined.The structure comparison between the less soluble and more soluble salts shows that weak interactions such as CH/πinteractions and van der Waals forces contribute to chiral recognition when the hydrogen bonding patterns are similar.
