发明名称 ACTIVE AGENT TRANSPORT SYSTEMS
摘要 Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of: a) providing a biologically active agent which can exist in a native conformational state, a denatured conformational state, and an intermediate conformational state which is reversible to the native state an d which is conformationally between the native and denatured states; b) exposing the biologically active agent to a complexing perturbant to reversibly transform the biologically active agent to the intermediate state and to forth a transportable supramolecular complex; and c) exposing the membrane or bilayer to the supramolecular complex, to transport the biologically active agent across the membrane or bilayer. The perturbant has a molecular weight between about 150 and about 600 daltons, and contains at least one hydrophilic moiety and at least one hydrophobic moiety. The supramolecular complex comprises the perturbant non-covalently bound or completed with the biologically active agent. In the present invention, the biologically active agent does not form a microsphere after interacting with the perturbant. A method for preparing an orally administrable biologically active agent comprising steps (a) and (b) above is also provided as are oral delivery compositions. Additionally, mimetics and methods for preparing mimetics are contemplated.
申请公布号 CA2202300(C) 申请公布日期 2007.04.10
申请号 CA19952202300 申请日期 1995.10.24
申请人 EMISPHERE TECHNOLOGIES, INC. 发明人 MILSTEIN, SAM J.;BARANTSEVITCH, EVGUENI;LEONE-BAY, ANDREA;WANG, NAI FANG;SARUBBI, DONALD J.;SANTIAGO, NOEMI B.
分类号 A61K9/16;A61K9/50 主分类号 A61K9/16
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