Sonocrystallization Yields Monoclinic Paracetamol with Significantly Improved Compaction Behavior. (4th November 2014)

• Record Type: Journal Article
• Authors: Bučar, Dejan‐Krešimir; Elliott, James A.; Eddleston, Mark D.; Cockcroft, Jeremy K.; Jones, William
• Is Part Of: Angewandte Chemie. Volume 127:Number 1(2015)
• Page Start: 251
• Page End: 255
• Publication Date: 2014-11-04
• Subjects: Kristallwachstum -- Nanostrukturen -- Polymorphie -- Pulverkompaktierung -- Sonokristallisation; Chemistry -- Periodicals; 540
• DOI: 10.1002/ange.201408894
• Languages: English
• ISSNs: 0044-8249

Abstract

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. Abstract : Compact Discs : Experimentelle Studien und eine Finite‐Elemente‐Analyse belegen, dass das schlechte Kompaktierungsverhalten von Paracetamol durch Sonokristallisation verbessert werden kann. Die leichtere Tablettenpressung wird einer einfacheren plastischen Verformung des Feststoffs und einer verstärkten Kohäsion zwischen einzelnen Partikeln zugeschrieben.