title: Formulation optimization of solid dispersion of mosapride hydrochloride.
abstract: Mosapride citrate (MSP) is a gastroprokinetic agent that acts as a selective 5-HT(4) 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.
authors: College of Pharmacy, Sookmyung Women's University, Seoul 140-742, Korea.
authors: Hye Jin
authors: HJ
authors: Kim
authors: Su Hyun
authors: SH
authors: Lee
authors: Eun Ah
authors: EA
authors: Lim
authors: Jin-Seok
authors: JS
authors: Kim
mesh_terms: D001549:Benzamides / Q000737:chemistry* / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding; D005765:Gastrointestinal Agents / Q000737:chemistry* / Q000494:pharmacology; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D015394:Molecular Structure; D009025:Morpholines / Q000737:chemistry* / Q000494:pharmacology; D011109:Polymethacrylic Acids / Q000737:chemistry; D011145:Polyvinyls / Q000737:chemistry; D011759:Pyrrolidines / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D001549:Benzamides; D003692:Delayed-Action Preparations; D004337:Drug Carriers; C496966:Eudragit RSPO; D005765:Gastrointestinal Agents; D009025:Morpholines; D011109:Polymethacrylic Acids; D011145:Polyvinyls; D011759:Pyrrolidines; C505150:poly(N-vinylpyrrolidine); D065347:Hypromellose Derivatives; D008747:Methylcellulose; C062720:mosapride