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    • 4. 发明申请
    • Amorphous Besifloxacin Solid
    • 无定形贝西沙星固体
    • US20110144329A1
    • 2011-06-16
    • US12956009
    • 2010-11-30
    • Mohannad ShawerEric PhillipsHarry M. King, JR.
    • Mohannad ShawerEric PhillipsHarry M. King, JR.
    • C07D223/12
    • C07D401/04C07D223/12
    • Amorphous solid-state form of (R)-(+)-7-(3-amino-2,3,4,5,6,7-hexahydro-1H-azepin-1-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid is characterized by at least one of: (a) an X-ray powder diffraction (“XRPD”) spectrum that comprises peaks at 2θ angles of 6.9-7.1, 9.4, 10.6-10.7, and 13.4-13.7°±0.2°, and a diffuse halo pattern at 11-30°; and (b) a DSC (differential scanning calorimetry) melting peak at about 267-272° C. The amorphous solid is prepared by rapid precipitation from a saturated or supersaturated solution of besifloxacin free base in a solvent comprising at least benzyl alcohol.
    • (R) - (+) - 7-(3-氨基-2,3,4,5,6,7-六氢-1H-吖庚因-1-基)-1,4-二氢 - 4-氧代喹啉-3-羧酸的特征在于以下中的至少一种:(a)包含在2θ处的峰的X射线粉末衍射(“XRPD”)光谱; 角度为6.9-7.1,9.4,10.6-10.7和13.4-13.7°±0.2°,扩散晕图案为11-30°; 在约267-272℃下的DSC(差示扫描量热法)熔融峰。(b)在约267-272℃下的DSC(差示扫描量热法)熔融峰。通过在至少含有苄醇的溶剂中从饱和或过饱和的贝沙沙星游离碱溶液快速沉淀制备无定形固体。