title: An enteric-coated dry emulsion formulation for oral insulin delivery.
abstract: A novel oral dosage formulation of insulin consisting of a surfactant, a vegetable oil, and a pH-responsive polymer has been developed. First, a solid-in-oil (S/O) suspension containing a surfactant-insulin complex was prepared. Solid-in-oil-in-water (S/O/W) emulsions were obtained by homogenizing the S/O suspension and the aqueous solution of hydroxypropylmethylcellulose phthalate (HPMCP). A microparticulate solid emulsion formulation was successfully prepared from the S/O/W emulsions by extruding them to an acidic aqueous solution, followed by lyophilization. The insulin release from the resultant dry emulsion responded to the change in external environment simulated by gastrointestinal conditions, suggesting that the new enteric-coated dry emulsion formulation is potentially applicable for the oral delivery of peptide and protein drugs.
authors.affiliation: Department of Applied Chemistry, Graduate School of Engineering, Oita University, 700 Dannoharu, Oita 870-1192, Japan.
authors.forename: Eiichi
authors.initials: E
authors.lastname: Toorisaka
authors.forename: Masakazu
authors.initials: M
authors.lastname: Hashida
authors.forename: Noriho
authors.initials: N
authors.lastname: Kamiya
authors.forename: Hiroshige
authors.initials: H
authors.lastname: Ono
authors.forename: Yuko
authors.initials: Y
authors.lastname: Kokazu
authors.forename: Masahiro
authors.initials: M
authors.lastname: Goto
mesh_terms: D000284:Administration, Oral; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D004655:Emulsions / Q000737:chemistry* / Q000627:therapeutic use; D016650:Fluorescein-5-isothiocyanate; D005456:Fluorescent Dyes; D006863:Hydrogen-Ion Concentration; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000737:chemistry* / Q000627:therapeutic use; D007328:Insulin / Q000008:administration & dosage* / Q000737:chemistry* / Q000627:therapeutic use; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D008856:Microscopy, Fluorescence; D010938:Plant Oils / Q000737:chemistry; D012996:Solutions; D013501:Surface-Active Agents / Q000737:chemistry; D014867:Water / Q000737:chemistry
chemical_list: D002214:Capsules; D004655:Emulsions; D005456:Fluorescent Dyes; D007004:Hypoglycemic Agents; D007328:Insulin; D010938:Plant Oils; D012996:Solutions; D013501:Surface-Active Agents; D014867:Water; D008747:Methylcellulose; D016650:Fluorescein-5-isothiocyanate