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Sonocrystallization Yields Monoclinic Paracetamol with Significantly Improved Compaction Behavior
Author(s) -
Bučar DejanKrešimir,
Elliott James A.,
Eddleston Mark D.,
Cockcroft Jeremy K.,
Jones William
Publication year - 2015
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201408894
Subject(s) - monoclinic crystal system , materials science , compaction , micrometer , crystallization , composite material , chemical engineering , cocrystal , particle size , coating , crystallography , mineralogy , crystal structure , organic chemistry , chemistry , molecule , optics , hydrogen bond , physics , engineering
Abstract Ultrasound‐assisted crystallization (sonocrystallization) was used to prepare a mixture of nano‐ and micrometer‐sized crystals of the monoclinic form of paracetamol—a widely used analgesic known for its particularly problematic mechanical behavior under compression (i.e. poor tabletability). The nano‐ and micrometer‐sized crystals yielded a powder which exhibits elastic moduli and bulk cohesions that are significantly higher than those observed in samples consisting of macrometer‐sized crystals, thus leading to enhanced tabletability without the use of excipients, particle coating, salt, or cocrystal formation. Experimental compaction and finite element analysis were utilized to rationalize the significantly improved compaction behavior of the monoclinic form of paracetamol.