公开(公告)号：EP2174660A1

公开(公告)日：2010-04-14

申请号：EP08790688.9

申请日：2008-06-27

申请人： Asubio Pharma Co., Ltd.

发明人： KONDOH, Masuo ,  UCHIDA, Hiroshi ,  HANADA, Takeshi ,  HOSHINO, Masato

IPC分类号： A61K38/22 ,  A61K47/42 ,  A61P43/00

CPC分类号： A61K38/29 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0073 ,  A61K38/164 ,  A61K38/2214 ,  A61K38/25 ,  A61K47/42 ,  A61K2300/00

摘要： A mucosal absorption-enhancing agent is provided that enables oral, nasal or pulmonary administration of peptide drugs whose administration route has heretofore been limited to the injections due to their poor absorption from the mucosa. Specifically, the mucosal absorption of peptide drugs via intestinal, pulmonary or nasal route can be enhanced by allowing the peptide drugs with the C-terminal fragment (C-CPE) of an enterotoxin (CPE) produced by the bacterium Clostridium perfringens of the genus Clostridium, in particular with the C-CPE or its mutants resulting from the substitution and/or deletion of one or several amino acid residues of the C-CPE to act thereon. The composition for mucosal administration of the present invention significantly enhances absorption of peptide drugs, such as human parathyroid hormone hPTH(1-34), human ghrelin and human motilin, through the mucosa of small intestine, lung, nasal cavity and other mucosa. Also, unlike any of the conventional mucosal absorption-enhancers, the composition for mucosal administration of the present invention does not cause tissue damage and is therefore highly safe for use.

摘要翻译： 本发明提供一种粘膜吸收增强剂确实允许口服，经鼻或肽药物谁的给药途径迄今限于由于它们从粘膜吸收差注射肺给药。 具体而言，通过肠道，肺或鼻途径的肽类药物的粘膜吸收可通过使由梭菌属的细菌产气荚膜梭菌产生的肽药物的肠毒素（CPE）的C端片段（C-CPE）来增强 特别是与C-CPE或及其突变体来自一个的取代和/或缺失或C-CPE以在其上作用的几个氨基酸残基得到的。 用于本发明的粘膜给药的组合物显着提高了的肽类药物，：诸如人副甲状腺激素的hPTH（1-34），人生长素释放肽和人促胃动素的吸收，通过小肠，肺，鼻腔和其他粘膜的粘膜。 因此，与任何常规的粘膜吸收促进剂的，用于本发明的粘膜给予的组合物不会引起组织损伤，因此对于使用高度安全的。