Physicochemical characterization and in vivo evaluation of flurbiprofen-loaded solid dispersion without crystalline change

Title
Physicochemical characterization and in vivo evaluation of flurbiprofen-loaded solid dispersion without crystalline change
Author(s)
용철순강준혁[강준혁]오동훈[오동훈]최한곤[최한곤]박영준[박영준]
Keywords
SPRAY-DRYING TECHNIQUE; CYCLODEXTRIN INCLUSION COMPLEX; DRUG-DELIVERY SYSTEM; IBUPROFEN; RELEASE; BIOAVAILABILITY; DISSOLUTION; ENHANCEMENT; FORMULATION; SOLUBILITY
Issue Date
201101
Publisher
TAYLOR & FRANCIS INC
Citation
DRUG DELIVERY, v.18, no.1, pp.46 - 53
Abstract
To develop a novel flurbiprofen-loaded solid dispersion without crystalline change, various flurbiprofen-loaded solid dispersions were prepared with water, sodium carboxylmethyl cellulose (Na-CMC), and Tween 80. The effect of Na-CMC and Tween 80 on aqueous solubility of flurbiprofen was investigated. The physicochemical properties of solid dispersions were investigated using SEM, DSC, and X-ray diffraction. The dissolution and bioavailability in rats were evaluated compared to commercial product. Unlike conventional solid dispersion systems, the flurbiprofen-loaded solid dispersion gave a relatively rough surface and changed no crystalline form of drug. These solid dispersions were formed by attaching hydrophilic carriers to the surface of drug without crystal change, resulting in changing the hydrophobic drug to hydrophilic form. Furthermore, the flurbiprofen-loaded solid dispersion at the weight ratio of flurbiprofen/Na-CMC/Tween 80 of 6/2.5/0.5 improved similar to 60-fold drug solubility. It gave higher AUC, T(max), and C(max) compared to commercial product. The solid dispersion improved almost 1.5-fold bioavailability of drug compared to commercial product in rats. Thus, the flurbiprofen-loaded solid dispersion would be useful to deliver poorly water-soluble flurbiprofen with enhanced bioavailability without crystalline change.
URI
http://hdl.handle.net/YU.REPOSITORY/25730http://dx.doi.org/10.3109/10717544.2010.509365
ISSN
1071-7544
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약학대학 > 약학부 > Articles
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