Abstract
ENHANCEMENT OF DISSOLUTION RATE OF EBASTINE FOR THE PREPARATION OF ORODISPERSIBLE TABLETS

*Marwa A. Shama, Ebtessam A. Essa and Mona F. Arafa

ABSTRACT

The aim of this work was to explore solid dispersion strategy as a tool to enhance the dissolution rate of the hydrophobic drug, Ebastine. The drug was allowed to co-precipitate from its organic solvent with a hydrophilic polymer. polyvinyl pyrrolidone (PVP 40T), hydroxypropylmethylcellulose (HPMC E5) and polyethylene glycol (PEG 6000) were selected as the hydrophilic polymers. The effect of presence of carrierof large surface area during the precipitation step was also investigated. Aerosil 200 was used as carrier upon which the drug would deposit. Coprecipitation was achieved by solvent evaporation method. The prepared formulations were evaluated regarding their in vitro drug release. Solid state characterization was also evaluated for selected formulations. Unprocessed ebastine showed no release during the experiment time course. Precipitated ebastine in presence of hydrophilic polymers significantly improved the dissolution compared to control, with ebastine-PVP40T co-precipitate being superior to the other two polymers. Addition of Aerosil during the recrystallization step improved further the dissolution parameters. The Thermal behavior and X-ray powder diffraction results indicated reduced drug crystalinity. Infra-red spectroscopy alleviate any possible drug-excipient interaction. This strategy thus provided a simple technique for dissolution enhancement of low soluble drugs. Optimum formulations were successfully formulated as orally disintegrating tablets with subsequent fast dissolution.

Keywords: Ebastine, Aerosil 200, solid dispersion, enhance dissolution rate, fast dissolving tablets.


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