Solid dispersions are a useful approach to improve the dissolution rate and\nbioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). The aim of\nthis study was to improve the physicochemical properties and bioavailability of a poorly\nwater-soluble aprepitant by preparation of solid dispersions. The solid dispersions were\ncharacterized by dissolution, FTIR, XRPD, DSC, SEM and pharmacokinetic studies in rats.\nThe dissolution rate of the aprepitant was significantly increased by solid dispersions, and\nXRD, DSC, and SEM analysis indicated that the aprepitant existed in an amorphous form\nwithin the solid dispersions. The result of dissolution study showed that the dissolution rate\nof SDs was nearly five-fold faster than aprepitant. FTIR spectrometry suggested the presence\nof intermolecular hydrogen bonds between the aprepitant and polymer. Pharmacokinetic\nstudies in rats indicated that the degree drug absorption was comparable with that of\nEmendÃ?®. Aprepitant exists in an amorphous state in solid dispersions and the solid\ndispersions can markedly improve the dissolution and oral bioavailability of the aprepitant.\nThe AUC0ââ?¬â??t of the SDs was 2.4-fold that of the aprepitant. In addition, the method and its\nassociated techniques are very easy to carry out.
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