Sonocrystallization Yields Monoclinic Paracetamol with Significantly Improved Compaction Behavior. Issue 1 (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 international edition. Volume 54:Issue 1(2015)
• Page Start: 249
• Page End: 253
• Publication Date: 2014-11-04
• Subjects: crystal growth -- nanostructures -- polymorphism -- powder compaction -- sonocrystallization; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201408894
• Languages: English
• ISSNs: 1433-7851

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 : Experimental compaction and finite element analysis have shown that the poor compaction properties of paracetamol can be improved through sonocrystallization. The superior tabletability is attributed to the enhanced capacity of the solid to plastically deform and the increased cohesive interactions between its particles.