An enteric-coated dry emulsion formulation for oral insulin delivery.
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.
Toorisaka
Eiichi
E
Department of Applied Chemistry, Graduate School of Engineering, Oita University, 700 Dannoharu, Oita 870-1192, Japan.
Hashida
Masakazu
M
Kamiya
Noriho
N
Ono
Hiroshige
H
Kokazu
Yuko
Y
Goto
Masahiro
M
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
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