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. |