Controlled precipitation for enhanced dissolution rate of flurbiprofen: Development of rapidly disintegrating tablets.

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Controlled precipitation for enhanced dissolution rate of flurbiprofen: Development of rapidly disintegrating tablets.

Drug Dev Ind Pharm. 2017 Apr 12;:1-34

Authors: Essa EA, Elmarakby AO, Donia AM, El Maghraby GM

Abstract
OBJECTIVE: The aim of this work was to investigate the potential of controlled precipitation of flurbiprofen on solid surface, in presence or absence of hydrophilic polymers, as a tool for enhnaced dissolution rate of the drug. The work was extended to develop rapidly disintegrated tablets.
SIGNIFICANCE: This strategy provide simple technique for dissolution enhancement of slowly dissolving drugs with high scaling up potential.
METHOD: Aerosil was dispersed in ethanolic solution of flurbiprofen in presence and absence of hydrophilic polymers. Acidified water was added as antisolvent to produce controlled precipitation. The resultant particles were centrifuged and dried at ambient temperature before monitoring the dissolution pattern. The particles were also subjected to FTIR spectroscopic, X-ray diffraction and thermal analysis.
RESULTS: The FTIR spectroscopy excluded any interaction between flurbiprofen and excipients. The thermal analysis reflected possible change in the crystalline structure and or crystal size of the drug after controlled precipitation in presence of hydrophilic polymers. This was further confirmed by X-ray diffraction. The modulation in the crystalline structure and size was associated with a significant enhancement in the dissolution rate of flurbiprofen. Optimum formulations were successfully formulated as rapidly disintegrating tablet with subsequent fast dissolution.
CONCLUSION: Precipitation on a large solid surface area is a promising strategy for enhanced dissolution rate with the presence of hydrophilic polymers during precipitation process improving the efficiency.

PMID: 28402193 [PubMed - as supplied by publisher]

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