Origin of deteriorated crystal plasticity and compaction properties of a 1:1 cocrystal between piroxicam and saccharin

Sayantan Chattoraj, Limin Shi, Miles Chen, Amjad Alhalaweh, Sitaram Velaga, Changquan Calvin Sun

Research output: Contribution to journalArticlepeer-review

59 Scopus citations

Abstract

The 1:1 cocrystal between piroxicam and saccharin exhibits significantly deteriorated powder compaction properties compared to both coformers. The molecular origin of this effect is revealed by a systematic investigation of crystal mechanical properties, probed with nanoindentation, and crystal structure analysis. The order of bulk powder tabletability of the three materials is identical to that of single crystal plasticity (saccharin > piroxicam > cocrystal). The lowest plasticity of the cocrystal is confirmed by its highest crystal hardness and the highest yield strength. The low plasticity of the cocrystal is attributed to structural packing features that discourage plastic deformation. This work demonstrates that cocrystallization, even though it may be useful to improve pharmaceutically relevant properties, must be carefully evaluated to avoid unexpected problems in formulation and drug product manufacturing due to compromised mechanical properties.

Original languageEnglish (US)
Pages (from-to)3864-3874
Number of pages11
JournalCrystal Growth and Design
Volume14
Issue number8
DOIs
StatePublished - Aug 6 2014

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