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    • 6. 发明申请
    • AQUEOUS SUSTAINED-RELEASE DRUG DELIVERY SYSTEM FOR HIGHLY WATER-SOLUBLE ELECTROLYTIC DRUGS
    • 高水溶性电解液的水溶性持续释放药物输送系统
    • WO2006135362A1
    • 2006-12-21
    • PCT/US2005/020534
    • 2005-06-09
    • UPM PHARMACEUTICALS, INC.HOLLENBECK, R., Gary
    • HOLLENBECK, R., Gary
    • A61K9/10A61K47/36A61K47/48A61K31/135
    • A61K9/0095A61K9/1635A61K9/1652A61K9/5026A61K9/5078A61K31/135A61K47/585
    • The present invention relates to liquid sustained release suspension dosage forms comprising ionized forms of water-soluble drugs. In particular, the invention encompasses a liquid form controlled release drug composition comprising a dispersed phase comprising an ion-exchange matrix drug complex comprising a pharmaceutically acceptable a ion-exchange matrix and a water-soluble electrolytic drug associated with the ion-exchange matrix, wherein the surface charge of the ion-exchange matrix is opposite that of the electrolytic drug wherein the dispersed phase further comprises a non-electrolytic, soluble component having low molecular weight and a diffusion controlling membrane and a dispersion medium substantially free of diffusible counterions, further comprising an excipient capable of associating with water and impeding water activity such that drug dissolution is inhibited prior to administration. The invention also provides methods for preparing such compositions and methods of treatment.
    • 本发明涉及包含电离形式的水溶性药物的液体缓释悬浮剂剂型。 特别地,本发明包括液体形式的控释药物组合物,其包含分散相,其包含离子交换基质药物复合物,其包含药学上可接受的离子交换基质和与离子交换基质相关的水溶性电解药物,其中 离子交换基质的表面电荷与电解药物的表面电荷相反,其中分散相还包含具有低分子量的非电解可溶性组分和扩散控制膜以及基本上不含可扩散抗衡离子的分散介质,还包含 能够与水缔合并阻碍水分活性的赋形剂,使得在施用之前药物溶解被抑制。 本发明还提供了制备这种组合物和治疗方法的方法。