Effects of crystal habit on the sticking propensity of ibuprofen—A case study

[Display omitted] This study demonstrates the effect of active pharmaceutical ingredient (API) particle habit on the sticking propensity of ibuprofen. Four diverse crystal habits with similar physico chemical properties are reported and the sticking propensity was found to increase with shape regula...

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Bibliographic Details
Published in:International journal of pharmaceutics 2017-10, Vol.531 (1), p.266-275
Main Authors: Hooper, D., Clarke, F.C., Docherty, R., Mitchell, J.C, Snowden, M.J.
Format: Article
Language:English
Subjects:
Chemistry, Pharmaceutical
Crystal chemistry
Ibuprofen - analysis
Particle shape
Particle Size
Punch sticking
Surface energy
Surface Properties
Tablets
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Summary:[Display omitted] This study demonstrates the effect of active pharmaceutical ingredient (API) particle habit on the sticking propensity of ibuprofen. Four diverse crystal habits with similar physico chemical properties are reported and the sticking propensity was found to increase with shape regularity. The surface energy of the extreme habits were shown to be different where particles that were more regular in shape exhibited surface energies of 9mJ/m2 higher than those that were needle-like in habit. Computational and experimental data reveals that the increase in surface energy of the regular shaped particles can be attributed to the increase in the specific (polar) component, which is due to greater presence of faces which contain the carboxylic acid functionality at the surface. The increase in the specific energy component is shown to correlate with the sticking propensity of ibuprofen. It is proposed that investigation of the chemical causality of sticking, for this API and others, using the techniques demonstrated in this paper will be of increasing importance.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2017.08.091