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    • 6. 发明专利
    • Process for manufacturing tigecycline
    • 制造TIGECYCLINE的方法
    • JP2009191083A
    • 2009-08-27
    • JP2009136753
    • 2009-06-05
    • WyethワイスWyeth
    • CHANANA GURMUKHVENTURA DOMINICSAUNDERS RICHARDFAWZI MAHDI B
    • A61K31/65A61P31/04
    • A61K9/19A61K9/0019A61K31/58C07C231/12C07C231/22C07C2603/46C07C237/26
    • PROBLEM TO BE SOLVED: To provide a process for manufacturing the preparation of tigecycline suitable for intravenous infusion.
      SOLUTION: The process for manufacturing tigecycline as a reconstitutable powder having less than 0.9% of the total degradants comprises the steps: a. reducing and maintaining the oxygen level in WFI water to less than or equal to 0.5 ppm while maintaining the temperature at about 2°C to about 8°C; b. forming a solution of tigecycline in the water of step a at a concentration of about 10 to 50 mg/ml while maintaining the temperature and oxygen level; c. filling vials with the solution of step b; d. lyophilizing the solution of step c to form 25 mg to 150 mg of a reconstitutable powder in a vial; and e. sealing the vial under nitrogen atmosphere.
      COPYRIGHT: (C)2009,JPO&INPIT
    • 要解决的问题:提供一种制备适于静脉输注的替加环素的制备方法。 解决方案:将替加环素制造成具有小于总降解物的0.9%的可重构粉末的方法包括以下步骤:a。 将WFI水中的氧含量降低并维持在小于或等于0.5ppm,同时将温度保持在约2℃至约8℃; b。 在步骤a的水中以约10至50mg / ml的浓度形成替加环素的溶液,同时保持温度和氧气水平; C。 用步骤b的溶液填充小瓶; d。 将步骤c的溶液冻干以在小瓶中形成25mg至150mg的可重组粉末; 和e。 在氮气氛下密封小瓶。 版权所有(C)2009,JPO&INPIT