Toorisaka Eiichi, Hashida Masakazu, Kamiya Noriho, Ono Hiroshige, Kokazu Yuko, Goto Masahiro
Department of Applied Chemistry, Graduate School of Engineering, Oita University, 700 Dannoharu, Oita 870-1192, Japan.
J Control Release. 2005 Sep 20;107(1):91-6. doi: 10.1016/j.jconrel.2005.05.022.
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.
一种由表面活性剂、植物油和pH响应聚合物组成的新型胰岛素口服剂型已被开发出来。首先，制备了一种含有表面活性剂-胰岛素复合物的油包固（S/O）悬浮液。通过将S/O悬浮液与羟丙基甲基纤维素邻苯二甲酸酯（HPMCP）水溶液均质化，得到水包油包固（S/O/W）乳液。通过将S/O/W乳液挤出到酸性水溶液中，然后冻干，成功制备了一种微粒固体乳液制剂。所得干乳液中的胰岛素释放对胃肠道条件模拟的外部环境变化有响应，这表明这种新型肠溶包衣干乳液制剂有可能用于肽和蛋白质药物的口服给药。
