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    Solid bulk compositions containing quinolone carboxylic acids or naphthyridine carboxylic acids in free base form
    1.
    发明授权
    Solid bulk compositions containing quinolone carboxylic acids or naphthyridine carboxylic acids in free base form 失效
    含有游离碱形式的喹诺酮羧酸或萘啶羧酸的固体本体组合物

    公开(公告)号：US5783585A

    公开(公告)日：1998-07-21

    申请号：US723797

    申请日：1996-09-30

    申请人： Gary Jay Dozeman ,  Kenneth Thomas Porter ,  James Norton Wemple

    发明人： Gary Jay Dozeman ,  Kenneth Thomas Porter ,  James Norton Wemple

    IPC分类号： C07D401/04 ,  A61K31/47 ,  A61P31/04 ,  C07D215/56 ,  C07D471/04 ,  A61K31/435

    CPC分类号： C07D215/56 ,  C07D471/04

    摘要： The present invention provides a method of making quinolone carboxylic acids or naphthyridine carboxylic acids in free base form, the method comprising dissolving a quinolone carboxylic acid salt or naphthyridine carboxylic acid salt in a solvent system to form a solution; combining the solution containing the quinolone carboxylic acid salt or naphthyridine carboxylic acid salt with a calcium salt in an amount in the range of about 0.01% to about 5.0% by weight of the quinolone carboxylic acid salt or naphthyridine carboxylic acid salt and a base, the combination resulting in the formation of a precipitate; and collecting the precipitate. Also provided is a solid bulk pharmaceutical chemical composition comprising 7-(3-amino-1-pyrrolidinyl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or 7-�3-S-(2-S-aminopropionylamino)pyrrolidin-1-yl!-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid; and calcium in an amount in the range of 0.001% to about 1.0% by weight of the 7-(3-amino-1-pyrrolidinyl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or 7-�3-S-(2-S-aminopropionylamino) pyrrolidin-1-yl!-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid.

    摘要翻译： 本发明提供以游离碱形式制备喹诺酮羧酸或萘啶羧酸的方法，所述方法包括将喹诺酮羧酸盐或萘啶羧酸盐溶解在溶剂体系中以形成溶液; 将含有喹诺酮羧酸盐或萘啶羧酸盐的溶液与喹啉酮羧酸盐或萘啶羧酸盐和碱的重量比为约0.01％至约5.0％的钙盐组合， 组合导致沉淀物的形成; 并收集沉淀物。 还提供了包含7-（3-氨基-1-吡咯烷基）-8-氯-1-环丙基-6-氟-1,4-二氢-4-氧代喹啉-3-羧酸或7 - [3-S-（2-S-氨基丙酰基氨基）吡咯烷-1-基] -1-环丙基-6-氟-1,4-二氢-4-氧代-1,8-二氮杂萘-3-羧酸; 和以重量计为0.001％至约1.0％的量的7-（3-氨基-1-吡咯烷基）-8-氯-1-环丙基-6-氟-1,4-二氢-4 - 氧代喹啉-3-羧酸或7- [3-S-（2-S-氨基丙酰基氨基）吡咯烷-1-基] -1-环丙基-6-氟-1,4-二氢-4-氧代-1,8 - 萘啶-3-羧酸。