title: Preparation of solid dispersion of dronedarone hydrochloride with Soluplus(®) by hot melt extrusion technique for enhanced drug release.
abstract: In order to enhance the dissolution rate of dronedarone hydrochloride (DRN), a novel Soluplus(®) (polyethyleneglycol-polyvinyl caprolactam-polyvinyl acetate grafted copolymer)-based solid dispersion (SD) was formulated using a hot melt extrusion technique. The physical characteristics determined using scanning electron microscopy and X-ray powder diffraction, revealed that the active compound was molecularly dispersed in the amphiphilic polymer in a stable amorphous form. The dissolution rate of DRN from the tablet dosage form of SD extrudate consisted of the drug and Soluplus(®) in a weight ratio of 1 : 1, and was obviously more rapid and higher than that of the intact drug and marketed product (Multaq(®), Sanofi, U.S.A.) at pH 1.2, 4.0 and 6.8. This suggests that Soluplus(®)-based SD formula can be a promising approach for enhancing the dissolution and oral absorption of DRN with a simple preparation process.
authors.affiliation: Dong-A Pharmaceutical Co., Ltd.
authors.forename: Sang Duk
authors.initials: SD
authors.lastname: Han
authors.forename: Sang Won
authors.initials: SW
authors.lastname: Jung
authors.forename: Sun Woo
authors.initials: SW
authors.lastname: Jang
authors.forename: Hyuck Jun
authors.initials: HJ
authors.lastname: Jung
authors.forename: Miwon
authors.initials: M
authors.lastname: Son
authors.forename: Byoung Moon
authors.initials: BM
authors.lastname: Kim
authors.forename: Myung Joo
authors.initials: MJ
authors.lastname: Kang
mesh_terms: D000638:Amiodarone / Q000031:analogs & derivatives* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D000077764:Dronedarone; D065546:Drug Liberation; D006358:Hot Temperature; D006863:Hydrogen-Ion Concentration; D015394:Molecular Structure; D011092:Polyethylene Glycols / Q000737:chemistry*; D011145:Polyvinyls / Q000737:chemistry*; D052616:Solid Phase Extraction; D013678:Technology, Pharmaceutical
chemical_list: D011145:Polyvinyls; C572167:polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; D011092:Polyethylene Glycols; D000077764:Dronedarone; D000638:Amiodarone