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    • 1. 发明授权
    • Basic drug compositions with enhanced bioavailability
    • 具有增强的生物利用度的基本药物组合物
    • US06548555B1
    • 2003-04-15
    • US09495438
    • 2000-01-31
    • William J. CuratoloJames A. S. NightingaleRavi M. ShankerSteven C. Sutton
    • William J. CuratoloJames A. S. NightingaleRavi M. ShankerSteven C. Sutton
    • A61K4732
    • A61K47/38A61K9/146A61K9/1652A61K9/2054A61K9/4866Y10S977/915
    • A composition comprising a basic drug, a drug which forms a zwitterion, or a salt of either entity, admixed with a polymer selected from hydroxypropylmethylcellulose acetate succinate (HPMCAS), cellulose acetate trimellitate (CAT), cellulose acetate phthalate (CAP), hydroxypropylcellulose acetate phthalate (HPCAP), hydroxypropylmethylcellulose acetate phthalate (HPMCAP), and methylcellulose acetate phthalate (MCAP). The compositions having improved solubility, hence bioavailability, in the small intestine; Processes for testing such compositions, and methods of using such compositions. The compositions comprise the basic drug, zwitterion, or salt and one or more of the aforementioned polymers. The invention further relates to a method for increasing the bioavailability of a basic or a zwitterionic drug comprising co-administering the basic drug, the zwitterionic drug, or the salt, with one or more of the aforementioned polymers.
    • 包含碱性药物,形成两性离子的药物或任一实体的盐,与选自羟丙基甲基纤维素乙酸酯琥珀酸酯(HPMCAS),醋酸偏苯三酸纤维素(CAT),乙酸邻苯二甲酸纤维素(CAP),羟丙基纤维素乙酸酯 邻苯二甲酸酯(HPCAP),羟丙基甲基纤维素乙酸邻苯二甲酸酯(HPMCAP)和甲基纤维素乙酸邻苯二甲酸酯(MCAP)。 所述组合物在小肠中具有改善的溶解度,因此具有生物利用度; 用于测试这些组合物的方法,以及使用这些组合物的方法。 组合物包含碱性药物,两性离子或盐和一种或多种上述聚合物。 本发明还涉及增加碱性或两性离子药物的生物利用度的方法,包括将一种或多种上述聚合物共同给予碱性药物,两性离子药物或盐。