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    • 1. 发明申请
    • COMPOSITIONS CONTAINING PRODRUGS OF FLORFENICOL AND METHODS OF USE
    • 含有氟虫腈的组合物及其使用方法
    • US20080306152A1
    • 2008-12-11
    • US12143097
    • 2008-07-28
    • Yerramilli V.S.N. MurthyRobert H. Suva
    • Yerramilli V.S.N. MurthyRobert H. Suva
    • A61K31/22A61P31/04
    • A61K31/222A61K9/0019A61K9/0024A61K31/205A61K31/23A61K49/0004C07C317/32A61K2300/00
    • The present invention provides compositions and methods for administering florfenicol to mammals. The compositions contain a prodrug of florfenicol in a pharmaceutically acceptable carrier. In one embodiment the prodrug is an esterized form of florfenicol. Examples of suitable prodrugs include one or a combination of one or a combination of the following: florfenicol acetate, florfenicol propionate, florfenicol butyrate, florfenicol pentanoate, florfenicol hexanoate, florfenicol heptanoate, florfenicol octanoate, florfenicol nanoate, florfenicol decanoate, florfenicol undecanoate, florfenicol dodecanoate, and florfenicol phthalate. In another embodiment the prodrug is converted into the florfenicol in vivo by the action of one or more endogenous esterases. The invention also provides new compounds, pharmaceutical compositions containing the compounds, and methods for their administration.
    • 本发明提供了用于向哺乳动物施用氟苯尼考的​​组合物和方法。 组合物在药学上可接受的载体中含有氟苯尼考的​​前药。 在一个实施方案中,前药是氟苯尼考的​​酯化形式。 合适的前药的实例包括以下的一种或组合的一种或其组合:氟苯尼考乙酸酯,氟苯尼考丙酸酯,氟苯尼考丁酸酯,氟苯尼考戊酸酯,氟苯尼考己酸酯,氟苯尼考辛酸酯,氟苯尼考辛酸酯,氟苯尼考羧酸酯,氟苯尼考十一酸酯,氟苯尼考十二酸酯 和氟苯尼考邻苯二甲酸酯。 在另一个实施方案中,前体药物通过一种或多种内源性酯酶的作用在体内转化成氟苯尼考。 本发明还提供新的化合物,含有这些化合物的药物组合物及其给药方法。
    • 3. 发明授权
    • 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
    • US07404964B2
    • 2008-07-29
    • US11088922
    • 2005-03-25
    • Yerramilli V.S.N. MurthyRobert H. Suva
    • Yerramilli V.S.N. MurthyRobert H. Suva
    • A61K9/00
    • 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 12 -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。