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1. 发明授权

US06355270B1 Particles for oral delivery of peptides and proteins 有权
标题翻译：用于口服肽和蛋白质的颗粒
公开(公告)号：US06355270B1
公开(公告)日：2002-03-12
申请号：US09479389
申请日：2000-01-06
申请人： Mauro Ferrari , Peter J. Dehlinger , Francis J. Martin , Carl F. Grove , David R. Friend
发明人： Mauro Ferrari , Peter J. Dehlinger , Francis J. Martin , Carl F. Grove , David R. Friend
IPC分类号： A61K914
CPC分类号： G03F7/00 , A61K9/0097 , A61K9/1676 , A61K9/1694 , A61K9/4891
摘要： Microfabricated, asymmetrical, reservoir-containing particles for use in the oral delivery of biopolymer therapeutic agents such as peptides, proteins and oligonucleotides are disclosed. The particles are encapsulated in enteric-coated capsules or tablets to provide passage through the stomach and release of a suspension of the particles in the intestinal lumen. The particles have a selected shape, and uniform dimensions preferably in the 100 &mgr;m to 1 mm range. The reservoirs open to the face of the particle and are filled with a therapeutic agent and selected excipients. The excipients are selected to delay the dissolution/release of the agent from the particle reservoirs for 5-60 minutes after the particle is released in the intestinal lumen. Alternatively, the pore is plugged with an erodable material. The face of the particle is grafted with a layer of muco-adhesive ligands designed to quickly bind the particle to the intestinal mucosa for several minutes to several hours after release of the particles from the enteric-coated carrier.
摘要翻译：公开了用于生物聚合物治疗剂例如肽，蛋白质和寡核苷酸的口服递送的微制造的，不对称的，含储层的颗粒。将颗粒包封在肠溶衣胶囊或片剂中以提供穿过胃的通道并释放颗粒在肠腔中的悬浮液。颗粒具有选定的形状，并且尺寸均匀，优选在100μm至1mm范围内。储存器对颗粒的表面开放并填充有治疗剂和选定的赋形剂。选择赋形剂以在颗粒在肠腔中释放后延迟药剂从颗粒储存器中溶解/释放5-60分钟。或者，孔被可侵蚀的材料堵塞。该颗粒的表面用一层粘膜 - 粘合剂配体接枝，其设计用于在从肠溶衣载体上释放颗粒之后将颗粒快速结合至肠粘膜数分钟至数小时。

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