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KMID : 0380020090240060533
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Korean Journal of Biotechnology and Bioengineering
2009 Volume.24 No. 6 p.533 ~ p.540
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Preparation of Solid Dispersions of a Poorly Water-soluble Drug Using Supercritical Fluid
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Kim Seok-Yun
Lee Jung-Min
Jung In-Il
Lim Kyo-Bin
Ryu Jong-Hoon
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Abstract
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In this work, 5’-nitroindirubinoxime (5’-NIO) has been prepared as solid dispersions using a supercritical aerosol solvent extraction system (ASES) process in order to enhance its water solubility and dissolution rate. Solid dispersions of 5’-NIO and poly(vinyl pyrrolidone) (PVP) were prepared in various weight percent ratios. Three-component solid dispersions consisting of 5’-NIO, PVP, and poloxamer 188 (P188) were also prepared to study the influence of P188 level on their morphology, crystallinity, and dissolution behavior. All samples were prepared at 35℃ and 180 bar using supercritical carbon dioxide. The particle morphology and size of the two-component solid dispersions were found to be nearly spherical and much smaller (100-200 nm) compared with the original 5’-NIO. The morphology of three-component solid dispersions became more agglomerated as the level of P188 increased. The crystallinity of the original 5’-NIO was not observed in the solid dispersions prepared by the ASES process. Faster dissolution rates were observed for the three-componet solid dispersions because the arrangement of ethylene oxide and propylene oxide blocks of the poloxamer 188 enabled the formation of micelles in an aqueous phase.
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KEYWORD
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5’-NIO, supercritical fluid, solid dispersion, ASES
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