title: Solid-state characterization of Felodipine-Soluplus amorphous solid dispersions.
abstract: The aim of the current study is to develop amorphous solid dispersion (SD) via hot melt extrusion technology to improve the solubility of a water-insoluble compound, felodipine (FEL). The solubility was dramatically increased by preparation of amorphous SDs via hot-melt extrusion with an amphiphilic polymer, Soluplus® (SOL). FEL was found to be miscible with SOL by calculating the solubility parameters. The solubility of FEL within SOL was determined to be in the range of 6.2-9.9% (w/w). Various techniques were applied to characterize the solid-state properties of the amorphous SDs. These included Fourier Transform Infrared Spectrometry spectroscopy and Raman spectroscopy to detect the formation of hydrogen bonding between the drug and the polymer. Scanning electron microscopy was performed to study the morphology of the SDs. Among all the hot-melt extrudates, FEL was found to be molecularly dispersed within the polymer matrix for the extrudates containing 10% drug, while few small crystals were detected in the 30 and 50% extrudates. In conclusion, solubility of FEL was enhanced while a homogeneous SD was achieved for 10% drug loading.
authors.affiliation: a Department of Pharmaceutics and Drug Delivery , School of Pharmacy, the University of Mississippi, University , MS , USA .
authors.forename: Jiannan
authors.initials: J
authors.lastname: Lu
authors.affiliation: b Department of Chemistry and Biochemistry , The University of Mississippi, University , MS , USA .
authors.forename: Kristina
authors.initials: K
authors.lastname: Cuellar
authors.affiliation: b Department of Chemistry and Biochemistry , The University of Mississippi, University , MS , USA .
authors.forename: Nathan I
authors.initials: NI
authors.lastname: Hammer
authors.affiliation: a Department of Pharmaceutics and Drug Delivery , School of Pharmacy, the University of Mississippi, University , MS , USA .
authors.forename: Seongbong
authors.initials: S
authors.lastname: Jo
authors.affiliation: c BASF SE, Global Development and Technical Marketing , Ludwigshafen , Germany .
authors.forename: Andreas
authors.initials: A
authors.lastname: Gryczke
authors.affiliation: d BASF SE, R&D Product Management Excipients , Ludwigshafen , Germany .
authors.forename: Karl
authors.initials: K
authors.lastname: Kolter
authors.affiliation: e BASF Corporation , Tarrytown , NY , USA , and.
authors.forename: Nigel
authors.initials: N
authors.lastname: Langley
authors.affiliation: a Department of Pharmaceutics and Drug Delivery , School of Pharmacy, the University of Mississippi, University , MS , USA .|f Pii Center for Pharmaceutical Technology, School of Pharmacy, the University of Mississippi, University , MS , USA.
authors.forename: Michael A
authors.initials: MA
authors.lastname: Repka
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015736:Felodipine / Q000032:analysis / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000032:analysis / Q000737:chemistry*; D011145:Polyvinyls / Q000032:analysis / Q000737:chemistry*
chemical_list: D011145:Polyvinyls; C572167:polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; D011092:Polyethylene Glycols; D015736:Felodipine
keywords: Amorphous solid dispersion; felodipine; hot-melt extrusion; miscibility/solubility; solid-state characterization