66. Sanganwar, Ganesh P.; Gupta, Ram B.. Dissolution-rate enhancement of fenofibrate by adsorption onto silica using supercritical carbon dioxide. International Journal of Pharmaceutics (2008), 360(1-2), 213-218.
Abstract
Dissoln. rate of a
poorly water-sol. drug, fenofibrate, is increased by
adsorbing the drug onto silica. The
adsorption is achieved by first dissolving the drug in supercrit.
carbon dioxide and then depressurizing the soln. onto silica.
Loadings of up to 27.5 wt.% drug onto silica
are obtained. Since solvents are not
used in the loading process, the fenofibrate/silica
formulation is free of any residual solvent, and carbon dioxide is freely
removed upon depressurization. The
formulation is characterized using IR spectroscopy, UV spectroscopy, X-ray
diffraction, differential scanning calorimetry and
SEM. Based on in vitro
dissoln. study, a
significant increase in the dissoln. rate (.apprx.80% drug release in 20 min) of drug-silica
formulation is obsd. as
compared to micronized fenofibrate
(.apprx.20% drug release in 20 min), which can be attributed to increase in the
surface area and decrease in the crystallinity of
drug after adsorption onto silica. Two
different formulations are compared: (A) amorphous fenofibrate/silica
and (B) slightly cryst. fenofibrate/silica. The second formulation is found to be more
stable on storage.
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