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KMID : 0043320110340091467
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Archives of Pharmacal Research
2011 Volume.34 No. 9 p.1467 ~ p.1475
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Formulation optimization of solid dispersion of mosapride hydrochloride
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Kim Hye-Jin
Lee Su-Hyun
Lim Eun-Ah
Kim Jin-Seok
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Abstract
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Mosapride citrate (MSP) is a gastroprokinetic agent that acts as a selective 5-HT4 agonist and accelerates the gastric emptying, and is used for the treatment of acid reflux, irritable bowel syndrome, and functional dyspepsia. The purpose of this study is to investigate the solid dispersion formulations of MSP with controlled release characteristic using various polymers, elucidate the release mechanism, and characterize the interaction patterns between MSP and polymers. Solid dispersions of MSP with different drug-to-polymer ratios were prepared by a solvent evaporation method and characterized in comparison with the simple physical mixtures. Eudragit RSPO, Eudragit RLPO, hydroxypropylmethylcellulose (HPMC) or Kollidon SR® was used as a controlled-release polymer along with polyvinylpyrrolidone (PVP) as a carrier. Characterization of MSP solid dispersion was performed using thermal analysis (DSC), powder X-ray diffraction (XRD), Fourier transform-infrared (FT-IR) spectroscopy, where the drug was converted from the crystalline state to amorphous state in all polymeric carriers used. In vitro dissolution studies showed that the drug release has been extended up to 24 h by using Eudragit RSPO or HPMC. Moreover, the formulations containing higher polymer content ratio showed better slow-release profile. These results indicate that the solid dispersion formulation containing PVP/Eudragit RSPO or HPMC mixture could serve as a good controlled-release system for MSP.
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KEYWORD
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Mosapride citrate (MSP), Solid dispersion, Polyvinylpyrrolidone (PVP), Controlled-release solid dispersion
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