Abstract：
:Piroxicam crystallises into two polytypes, α1 and α2, with crystal structures that contain identical molecular layers but differ in the way that these layers are stacked. In spite of having close structural similarity, the polytypes have significantly different powder tabletting behaviour: α2 forms only weak tablets at low pressures accompanied by extensive capping and lamination, which make it impossible to form intact tablets above 100 MPa, while α1 exhibits superior tabletability over the investigated pressure range (up to 140 MPa). The potential structural origin of the different behaviour is sought using energy-vector models, produced from pairwise intermolecular interaction energies calculated using the PIXEL method. The analysis reveals that the most stabilising intermolecular interactions define columns in both crystal structures. In α2, a strongly stabilising interaction between inversion-related molecules links these columns into a 2-D network, while no comparable interaction exists in α1. The higher dimensionality of the energy-vector model in α2 may be one contributor to its inferior tabletability. A consideration of probable slip planes in the structures identifies regions where the benzothiazine groups of the molecules meet. The energy-vector models in this region are geometrically similar for both structures, but the interactions are more stabilising in α2 compared to α1. This feature may also contribute to the inferior tabletability of α2.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Upadhyay PP,Sun CC,Bond ADdoi
10.1016/j.ijpharm.2018.03.040subject
Has Abstractpub_date
2018-05-30 00:00:00pages
46-51issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(18)30187-Xjournal_volume
543pub_type
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