Polymorphic forms of dihydrochloride salts of cetirizine and processes for preparation thereof
    7.
    发明申请
    Polymorphic forms of dihydrochloride salts of cetirizine and processes for preparation thereof 审中-公开
    西替利嗪的二盐酸盐的多晶型形式及其制备方法

    公开(公告)号:US20040186112A1

    公开(公告)日:2004-09-23

    申请号:US10729856

    申请日:2003-12-04

    CPC classification number: C07D295/088 A61K31/495

    Abstract: The present invention relates to crystalline and amorphous forms of dextrorotatory dihydrochloride salt of cetirizine, the process for the preparation thereof and compositions containing the same. The invention also relates to the crystalline and amorphous forms of levorotatory dihydrochloride salt of cetirizine, the process for the preparation thereof and compositions containing the same. Both crystalline and amorphous salt forms of cetirizine dihydrochloride are suitable for pharmaceutical purposes in the treatment of allergies, including ailments such as chronic and acute allergic rhinitis, allergic conjunctivitis, pruritus, urticaria and the like.

    Abstract translation: 本发明涉及西替立嗪的右旋二盐酸盐的结晶和无定形形式,其制备方法和含有它们的组合物。 本发明还涉及西替利嗪的左旋二盐酸盐的结晶和无定形形式,其制备方法和含有它的组合物。 西替立嗪二盐酸盐的结晶盐和无定形盐形式适用于治疗过敏症的药物用途,包括慢性和急性过敏性鼻炎,过敏性结膜炎,瘙痒症,荨麻疹等疾病。

    Novel anhydrous crystalline form of Levofloxacin and process for preparation there of
    9.
    发明申请
    Novel anhydrous crystalline form of Levofloxacin and process for preparation there of 审中-公开
    左氧氟沙星的新型无水结晶形式及其制备方法

    公开(公告)号:US20040152701A1

    公开(公告)日:2004-08-05

    申请号:US10716207

    申请日:2003-11-18

    CPC classification number: C07D498/04

    Abstract: The present invention is directed to novel anhydrous crystalline form of Levofloxacin is depicted as Formula (I), further more its process for preparation thereof. The process for the preparation of novel anhydrous crystalline form of Levofloxacin comprises the condensation of N-Methyl piperazine with S(null)-9,10-difluoro-7-oxo 2,3-dihydro 7H-pyridonull1,2,3-DEnull null1,4null Benzoxazine-6-carboxylic acid in Acetonitrile followed by distillation of solvent to afford the residue, the resultant residue is refluxed with toluene and the solid is filtered at room temperature to afford the Levofloxacin. Thus resulted Levofloxacin is further refluxed in Acetonitrile and filtered the Novel anhydrous crystalline form of Levofloxacin as undissolved material. The anhydrous crystalline form of Levofloxacin is characterized by X-ray diffractogram, Differential Scanning Calorimetry thermogram and Infrared Spectra. 1

    Abstract translation: 本发明涉及左氧氟沙星的新型无水结晶形式如式(I)所示,其进一步制备其制备方法。 制备新型无水结晶形式的左氧氟沙星的方法包括N-甲基哌嗪与S( - ) - 9,10-二氟-7-氧代2,3-二氢-7-吡啶并[1,2,3- DE] [1,4]苯并恶嗪-6-羧酸,然后蒸馏除去溶剂,得到残留物,所得残余物与甲苯一起回流,固体在室温下过滤,得到左氧氟沙星。 由此导致左氧氟沙星在乙腈中进一步回流,并以新溶剂的形式过滤了左氧氟沙星的新型无水结晶形式。 无水结晶形式的左氧氟沙星的特征在于X射线衍射图,差示扫描量热法和红外光谱。

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