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    • 10. 发明申请
    • Injectable compositions for the controlled delivery of pharmacologically active compound
    • 用于控制递送药理学活性化合物的可注射组合物
    • US20030130211A1
    • 2003-07-10
    • US10274445
    • 2002-10-18
    • Yerramilli V.S.N. MurthyRobert H. Suva
    • A61K031/704A61K031/496A61K031/202A61K031/65A61K031/63A61K031/24A61K031/205
    • A61K31/00A61K9/0019A61K9/0024A61K31/24A61K31/496A61K31/65A61K31/7034A61K31/7048A61K47/10A61K47/12A61K47/14A61K47/20A61K47/22A61K47/26A61K2300/00
    • The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer. Many compounds can be administered according to the present invention including, but not limited to, tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine.
    • 本发明提供用于延长释放时间并降低药理活性化合物的毒性的组合物和方法。 化合物包含药理活性化合物的盐与亲脂性抗衡离子和药学上可接受的水溶性溶剂组合在一起形成可注射组合物。 亲油抗衡离子可以是饱和或不饱和的C 8 -C 22脂肪酸,优选可以是饱和或不饱和的C 10 -C 18脂肪酸。 当注射到哺乳动物中时,组合物的至少一部分随时间沉淀并释放活性化合物。 因此,组合物在哺乳动物中形成缓慢释放活性化合物的药物贮库。 因此,本发明使得能够提供活性化合物的受控剂量给药长达15天甚至更长时间。 根据本发明可以施用许多化合物,包括但不限于替米考星,土霉素,美托洛尔,氟西汀,罗红霉素和头孢噻吩。