Characterization of Physicochemical Properties of Spray-dried Solid Dispersions Loaded with Unmodified Crystalline Fenofibrate

Title
Characterization of Physicochemical Properties of Spray-dried Solid Dispersions Loaded with Unmodified Crystalline Fenofibrate
Author(s)
용철순Abid Mehmood Yousaf[Abid Mehmood Yousaf]김동욱[김동욱]김종오장판식[장판식]백형희[백형희]임수정[임수정]조관형[조관형]최한곤[최한곤]
Keywords
WATER-SOLUBLE DRUGS; DISSOLUTION-RATE; SUPERCRITICAL ANTISOLVENT; MICRONIZED FENOFIBRATE; DOSAGE FORMS; FORMULATION; RELEASE; ENHANCEMENT; BIOAVAILABILITY; INDOMETHACIN
Issue Date
201504
Publisher
BENTHAM SCIENCE PUBL LTD
Citation
CURRENT PHARMACEUTICAL ANALYSIS, v.11, no.2, pp.139 - 144
Abstract
To accomplish a new solid dispersion providing optimized aqueous solubility and dissolution of fenofibrate without modifying the crystalline nature of the hydrophobic drug, different formulations were prepared with water, poly-vinylpyrrolidone (PVP) and sodium lauryl sulphate (SLS) using the spray-drying technique. The influence of the relative quantities of PVP and SLS on the dissolution and aqueous solubility of fenofibrate in the solid dispersion was determined. The solid dispersion exhibiting highest solubility and dissolution was subjected to scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) for physicochemical characterization. Converse to other conventional solid dispersion systems, this solid dispersion diminished the hydrophobicity of the drug by adhering hydrophilic constituents to the irregular surface of the crystalline drug during the spray drying process. In particular, the solid dispersion containing fenofibrate/PVP/SLS at a ratio of 2.5/1.5/1 (w/w/w) enormously ameliorated the aqueous solubility of fenofibrate compared to the drug powder (53.46 +/- 4.69 vs. 0.004 +/- 0.001 mu g/ml). Moreover, the dissolution was approximately 75% at 30 minutes with this solid dispersion. Thus, the solid dispersion loaded with the crystalline fenofibrate might be a promising pharmaceutical product to administer poorly water-soluble drug via the oral route.
URI
http://hdl.handle.net/YU.REPOSITORY/32730
ISSN
1573-4129
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약학대학 > 약학부 > Articles
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