Effect of crystal habit on intrinsic dissolution behavior of celecoxib due to differential wettability

Sameer R. Modi, Ajay K.R. Dantuluri, Sathyanarayana R. Perumalla, Changquan Calvin Sun, Arvind K. Bansal

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50 Scopus citations


Intrinsic dissolution rate (IDR) is a useful technique to differentiate the solid forms of a drug. In the present study, the impact of crystal habit and crystal size on IDR of celecoxib (CEL) in different media was assessed. The IDR of plate-shaped CEL crystals (CEL-P) (53.4 ± 6.7 μg/min/cm2) was 46.3% higher than that of acicular crystals (CEL-A) (36.5 ± 1.7 μg/min/cm2) in pH 12 phosphate buffer. Contact angle experiments and values of dispersive and polar components of surface free energy indicated better wettability of CEL-P compacts than CEL-A. Higher IDR and better wettability of CEL-P were attributed to favorable exposure of hydrophilic crystal facets on compact surface, due to preferred orientation during compaction. In contrast to native samples, milled CEL-A (MCEL-A) and milled CEL-P (MCEL-P) showed similar IDR. Interestingly, IDR of CEL-A (36.5 ± 1.7 μg/min/cm2) and MCEL-A (35.64 ± 5.09 μg/min/cm2) did not show any significant difference (p > 0.05). However, IDR of CEL-P (53.4 ± 6.7 μg/min/cm2) was significantly higher (p < 0.05) than that of MCEL-P (39.15 ± 2.48 μg/min/cm2). This was ascribed to (i) differential cleavage behavior of CEL-A and CEL-P during milling and (ii) reduced degree of preferred orientation of hydrophilic facets in MCEL-P compacts. This work provides an interesting case study of the impact of particle level properties and surface molecular environment on IDR.

Original languageEnglish (US)
Pages (from-to)5283-5292
Number of pages10
JournalCrystal Growth and Design
Issue number10
StatePublished - Oct 1 2014

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© 2014 American Chemical Society.


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