Development of a rebamipide solid dispersion system with improved dissolution and oral bioavailability

Title
Development of a rebamipide solid dispersion system with improved dissolution and oral bioavailability
Author(s)
김종오로샨프라단트란탄힙최주연최임순최한곤[최한곤]용철순
Keywords
SPRAY-DRYING TECHNIQUE; IN-VIVO EVALUATION; ENHANCED BIOAVAILABILITY; SOLUBLE DRUGS; BETA-CYCLODEXTRIN; SALT FORM; ABSORPTION; RELEASE; PH; INCLUSION
Issue Date
201504
Publisher
PHARMACEUTICAL SOC KOREA
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.38, no.4, pp.522 - 533
Abstract
The purpose of this study was to improve the gastric solubility and bioavailability of rebamipide (RBM) by preparing the RBM solid dispersion tablet (RBM-SDT) from solid dispersion powder prepared by spray-drying technique. For preparation of rebamipide solid dispersions (RBM-SDs), solubility study was performed in various hydrophilic carriers and alkalizers, among which sodium alginate and sodium carbonate were selected as the hydrophilic polymer and alkalizer, respectively. Different combinations of drug-polymer-alkalizer were dissolved in aqueous solution and spray-dried in order to obtain solid dispersions. Noticeable improvement in aqueous solubility (approximately 200 times) and in vitro dissolution rate was observed by RBM-SDs, compared to RBM powder. The optimized formulation of RBM-SD powder consisted of RBM powder/sodium alginate/sodium carbonate at the weight ratio of 1/2/2. The transformation of crystalline RBM to amorphous RBM-SD powder was clearly demonstrated by powder X-ray diffraction, differential scanning calorimetry (DSC) and scanning electron microscopy. The optimized RBM-SD was formulated in tablet dosage form, containing approximately 2 % sodium lauryl sulphate and poloxamer F68 as wetting agents. The RBM-SDT exhibited enhanced dissolution in hydrochloric acid buffer (pH 1.2) and distilled water. Moreover, pharmacokinetic study in rats showed higher AUC and C-max for RBM-SDT than those for RBM powder and commercial product. Thus, the developed RBM-SDT formulation can be more efficacious for improving oral bioavailability of RBM.
URI
http://hdl.handle.net/YU.REPOSITORY/32832http://dx.doi.org/10.1007/s12272-014-0399-0
ISSN
0253-6269
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약학대학 > 약학부 > Articles
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