发明名称 Sublimable sustained release delivery system and method of making same
摘要 The invention relates to compositions suitable for the delivery and/or stabilization of biologically active substances. The compositions comprise a sublimable matrix material and the biologically active agent to be delivered. The compositions can be used as drug delivery systems to treat a wide variety of diseases or as systems for the protection and stabilization of such substances. Also disclosed are methods for preparing compositions of the present invention.
申请公布号 US9301919(B2) 申请公布日期 2016.04.05
申请号 US200611615048 申请日期 2006.12.22
申请人 OAKWOOD LABORATORIES, LLC 发明人 Maskiewicz Richard
分类号 A61K9/00;A61K9/16 主分类号 A61K9/00
代理机构 Pearne & Gordon LLP 代理人 Pearne & Gordon LLP
主权项 1. A matrix biological insert or implant which is a delivery system suitable for sustained release of a biologically active agent within a mammal, said delivery system comprising: (a) at least one water insoluble sublimable matrix material that converts to vapor at a desired rate over a desired duration in the body of a mammal; and (b) a biologically active agent dispersed within said sublimable matrix material in an amount of 0.05 to 40% by weight based on a weight of said delivery system sufficient for prolonged treatment of a disease or other pathological condition in said mammal, wherein said sublimable matrix material has a sublimation enthalpy in a range of from 20 to 100 kJ/mole and is present in an amount of at least 60% by weight based on a weight of said delivery system effective to achieve a sustained release of said active agent in said mammal upon conversion of said sublimable matrix material to said vapor, and wherein said sublimable matrix material is selected from the group consisting of adamantane, perfluoroadamantane, 1-methyladamantane, perfluoro-1-methyladamantane, tetraisopropylmethane, perfluorotetraisopropylmethane, 2,2,3,3-tetramethylbutane (hexamethylethane), perfluoro-2,2,3,3-tetramethylbutane, perfluoroneopentane, perfluoro-C60fullerene, cubane, perfluorocubane, octamethylcubane, perfluorooctamethylcubane, perfluoromethyladamantane, perfluorotri-tert-butylmethane, perfluorodimethyladamantane, perfluorohexamethylethane, perfluoro-1,3-dimethyladamantane, isocamphane, tricyclene, 1-ethyladamantane,1-methyldiadamantane, perfluorodimethylbicyclo[3.3.1]nonane, diadamantane, perfluorodiadamantane, tri-tert-butylmethane, norbornane, perfluoronorbornane, cyclododecane, perfluorocyclododecane, hexamethylcyclotrisiloxane, perfluoroundecane, perfluorododecane, bicyclo[3.3.1]nonane, tetracycloheptane, tricyclohexane, dimethyl-isopropyl-perhydrophenanthrene, hexamethylprismane, prismane, tetracyclododecane, bicyclo[3.3.3]undecane, 2-methyladamantane, pentacycloundecane, tricyclodecane, bicyclodecane, bicyclo[2.2.2]octane, perfluoro-1,3,5-trimethyladamantane, perfluoro-2,2-dimethyladamantane, perfluorotetracycloheptane, perfluorotricyclohexane, perfluorohexamethylprismane, perfluoroprismane, perfluorotetracyclododecane, perfluorobicyclo[3.3.3]undecane, perfluoro-2-methyladamantane, perfluoropentacycloundecane, perfluorotricyclodecane, perfluorobicyclodecane, perfluorobicyclo[3.3.1]nonane, perfluorobicyclo[2.2.2]octane, perfluorobicyclo[2.2.1]heptane, and mixtures thereof.
地址 Oakwood Village OH US