Effect of the characteristics of raw material ibuprofen on roller compaction and dissolution

Abstract

Ibuprofen is an oral analgesic usually processed by wet granulation. In this manuscript a new roller compaction process for ibuprofen is reported. The low melting point of ibuprofen is a critical point to be considered during processing. Melting of ibuprofen and its posterior solidification leads to a lower soluble form. The hypothesis of this work is that crystallinity of ibuprofen may be a good indicator of the quality for both raw material selection and the granules obtained during roller compaction. To test the hypothesis two batches of ibuprofen raw material with different crystallinity degree were used. Crystallinity was studied by X ray powder diffraction (XRPD), molecular modelling and differential scanning calorimetry (DSC). Ibuprofen was mixed with sodium croscarmellose and then compacted in a refrigerated roller compactor at five different compaction forces (KN) between 45 and 70 KN. Particle size, moisture content and dissolution rate of the granules were also studied. As it was expected, roller compaction decreased the crystallinity degree of ibuprofen. Interestingly, differences on the crystal morphology of the raw material batches were related to the dissolution behavior of the granules. Therefore, crystallinity characterization of the raw material is proposed as a critical requirement on roller compaction.