公开(公告)号：US08859004B2

公开(公告)日：2014-10-14

申请号：US13561106

申请日：2012-07-30

申请人： Lijuan Zhang ,  Li Ling ,  Li Ying Zhou ,  Zhi Min Wu ,  Xin Dong Guo ,  Wei Jiang ,  Qian Luo ,  Yu Qian

发明人： Lijuan Zhang ,  Li Ling ,  Li Ying Zhou ,  Zhi Min Wu ,  Xin Dong Guo ,  Wei Jiang ,  Qian Luo ,  Yu Qian

IPC分类号： A61K9/51 ,  A61K38/28

CPC分类号： A61K9/5153 ,  A61K9/5161 ,  A61K9/5192 ,  A61K38/28 ,  Y10S977/906

摘要： The present invention discloses the pH-sensitive nanoparticles composed of pH-sensitive polymer, hydrophobic material, internal stabilizer, external stabilizer content and insulin drug. The present invention also includes a method for preparation of pH-sensitive nanoparticles, in particular, a multiple emulsions solvent evaporation method. The pH-sensitive nanoparticles of the present invention show good pH-sensitive property with 100-300 nanometer particle size. Significant decrease in blood glucose level is observed in streptozotocin (STZ)-induced diabetic rats and the bioavailability of insulin is more than 10% after oral administration of the insulin-loaded pH-sensitive nanoparticles.

摘要翻译： 本发明公开了由pH敏感聚合物，疏水材料，内部稳定剂，外部稳定剂含量和胰岛素药物组成的pH敏感纳米颗粒。 本发明还包括用于制备pH敏感性纳米颗粒的方法，特别是多重乳液溶剂蒸发法。 本发明的pH敏感纳米颗粒具有100-300纳米粒度的良好的pH敏感性质。 在链脲佐菌素（STZ）诱导的糖尿病大鼠中观察到血糖水平的显着降低，并且口服施用负载胰岛素的pH敏感纳米颗粒后胰岛素的生物利用度大于10％。

公开(公告)号：US09101547B2

公开(公告)日：2015-08-11

申请号：US13561105

申请日：2012-07-30

申请人： Yu Qian ,  Li Juan Zhang ,  Zhi Min Wu ,  Li Ying Zhou ,  Wei Jiang ,  Li Ling ,  Qian Luo ,  Xin Dong Guo

发明人： Yu Qian ,  Li Juan Zhang ,  Zhi Min Wu ,  Li Ying Zhou ,  Wei Jiang ,  Li Ling ,  Qian Luo ,  Xin Dong Guo

IPC分类号： A61K9/50 ,  A61K38/28 ,  A61K9/16 ,  A61K9/48 ,  B82Y5/00

CPC分类号： A61K9/5026 ,  A61K9/1635 ,  A61K9/1647 ,  A61K9/4891 ,  A61K38/28 ,  B82Y5/00

摘要： The invention relates to an enteric-coated capsule containing cationic nanoparticles for oral insulin delivery, in particular to a type of cationic nanoparticle including a polycationic and mucoadhesive polymer and a biodegradable polymer, wherein each of the nanoparticles has positive surface charge and enhanced permeability for paracellular insulin delivery; the enteric-coated capsule further includes a pH-sensitive polymer as the coating. The enteric-coated capsule containing cationic nanoparticles, when being orally administered to a subject, are configured to prevent the acidic degradation of the active substance such as insulin before being released from said cationic nanoparticles to a specific absorption site along the gastrointestinal tract.

摘要翻译： 本发明涉及含有用于口服胰岛素递送的阳离子纳米颗粒的肠溶衣胶囊，特别涉及一种阳离子纳米颗粒，包括聚阳离子和粘膜粘附聚合物和可生物降解的聚合物，其中每种纳米颗粒具有正表面电荷并且增加细胞旁通道的渗透性 胰岛素分泌 肠溶衣胶囊还包括作为涂层的pH敏感聚合物。 包含阳离子纳米颗粒的肠溶衣胶囊当被口服给药时被配置成防止活性物质如胰岛素在从所述阳离子纳米颗粒释放到沿着胃肠道的特定吸收部位之前的酸性降解。