Improved dissolution and anti-inflammatory effect of ibuprofen by solid dispersion

Abstract

The purpose of this study was to improve the dissolution rate and anti-inflammatory effect of ibuprofen by a solid dispersion (SD) method. Initial screening was developed based on drug solubility in carriers in the liquid state to select a suitable water-soluble carrier system for the preparation of SDs. The dissolution of ibuprofen in urea was higher than in PEG4000 or mannitol. Thus, urea was selected as the carrier for the preparation of SDs. SDs were characterized in terms of dissolution, differential scanning calorimetry (DSC), X-ray diffraction (XRD), scanning electron microscopy (SEM), and Fourier transform infrared (FTIR) spectroscopy. Solid dispersion-based (SDBT) and conventional (CT) tablets were prepared by the wet granulation method. The anti-inflammatory effect of SDBT was evaluated using the mouse ear edema test with xylene. In vitro release results indicated that the ibuprofen dissolution rate was improved by the SD. SD characterization results suggested that ibuprofen partly precipitates in crystalline and amorphous forms after SD preparation and that ibuprofen and urea do not interact. SDBT displayed more significant anti-inflammatory effects than CT. The dissolution rate and anti-inflammatory effect of ibuprofen were significantly enhanced by the ibuprofen-urea SD.

Keywords

ibuprofen / solid dispersion / physical mixture / dissolution / anti-inflammatory effect

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Acknowledgements

The authors acknowledge International S&T Cooperation Program of China (ISTCP, 2011DFA31270), National Natural Science Foundation of China &βKorea Science and Engineering Foundation (NSFC-KOSEF, 40911140282) and the Fundamental Research Funds for the Central Universities (841111042, 201213006) for their financial support.

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2014 Higher Education Press and Springer-Verlag Berlin Heidelberg