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    • 13. 发明申请
    • PHARMACEUTICAL FORMULATIONS FOR SUSTAINED DRUG DELIVERY
    • 用于持续输送药物的药物制剂
    • WO2007022254A2
    • 2007-02-22
    • PCT/US2006/031967
    • 2006-08-15
    • PRAECIS PHARMACEUTICALS, INC.GEFTER, Malcolm, L.BARKER, NicholasMUSSO, Gary, F.MOLINEAUX, Christopher, J.
    • GEFTER, Malcolm, L.BARKER, NicholasMUSSO, Gary, F.MOLINEAUX, Christopher, J.
    • A61K47/48
    • A61K38/09A61K47/61
    • Sustained delivery formulations comprising a water-insoluble complex of a peptidic compound (e.g., a peptide, polypeptide, protein, peptidomimetic or the like) and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptidic compound in a small volume and for delivery of a pharmaceutically active peptidic compound for prolonged periods, e.g. , one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptidic compound of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.
    • 公开了包含肽化合物(例如肽,多肽,蛋白质,拟肽等)和载体大分子的水不溶性络合物的持续递送制剂。 本发明的制剂允许以小体积装载高浓度的肽化合物并延长药物活性的肽化合物,例如用于递送。 ,一个月后,复杂的管理。 本发明的络合物可以研磨或粉碎成细粉末。 以粉末形式,络合物形成稳定的水性悬浮液和分散体,适于注射。 在优选的实施方案中,复合物的肽化合物是LHRH类似物,优选LHRH拮抗剂,载体大分子是阴离子聚合物,优选羧甲基纤维素。 还公开了制备本发明复合物的方法,以及使用含LHRH类似物的复合物治疗可用LHRH类似物治疗的病症的方法。