Abstract
Solid dispersions of poorly water-soluble drug, sibutramine, were prepared with hydrophilic polymer, poly-N-vinylpyrrolidone (PVP), hydroxypropylmethylcellulose (HPMC) and organic acid, citric acid, to improve the solubility of drug. Physicochemical variation and shape of microsphere were characterized by scanning electron microscopy (SEM), differential scanning calorimeter (DSC) and Fourier-transform infrared spectroscopy (FT-IR). Microspheres containing additives showed more spherical shape than non additive microspheres. In vitro release behavior of microspheres presented at simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The solid dispersion form transformed the drug into an amorphous state and dramatically improved its dissolution rate. These data suggest that the solid dispersion technique is an effective approach for developing the appetite depressant drug products and various pharmaceutical excipients are able to control the release behaviors.
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