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KMID : 0369820160460060583
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Jorunal of Korean Pharmaceutical Sciences
2016 Volume.46 No. 6 p.583 ~ p.592
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Employing an optimized spray-drying process to produce ezetimibe tablets with an improved dissolution profile
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Kim Sung-Yub
Gupta Biki
Moon Cheol
Oh Eui-Chaul
Jeong Jee-Heon
Yong Chul-Soon
Kim Jong-Oh
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Abstract
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Ezetimibe is a low-density lipoprotein cholesterol-lowering agent with poor aqueous solubility. There is therefore a need to increase the aqueous solubility of ezetimibe in order to improve its dissolution profile, and thereby, enhance its bioavailability. The purpose of this study was to produce a solid dispersion of ezetimibe with improved physicochemical characteristics, which could be then be used to prepare ezetimibe tablets with improved dissolution characteristics. The ezetimibe solid dispersion was prepared by an optimized spray-drying process. Product characteristics, namely, yield, moisture content, solubility, and Hausner ratio, were optimized by controlling process parameters, namely, inlet temperature, pump feed rate, and solid contents, by applying the Box-Behnken design and the desirability functions approach. The physicochemical characteristics of the optimized solid dispersion were in close agreement with the predicted characteristics. The tablets formulated using the optimized solid dispersion exhibited an excellent dissolution profile, which was remarkably better than that of tablets formulated from free ezetimibe or a physical mixture of the drug and the excipients. Therefore, ezetimibe tablets with improved solubility and dissolution characteristics were produced using an optimized spray-drying technique.
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KEYWORD
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Ezetimibe, Solid dispersion, Spray-drying, Solubility, Design of experiment, Box-Behnken design
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