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    • 3. 发明申请
    • PHARMACEUTICAL COMPOSITIONS AND METHODS FOR STABILIZING THE SAME
    • 药物组合物及其稳定化方法
    • US20120322836A1
    • 2012-12-20
    • US13600083
    • 2012-08-30
    • Gopal KrishnaRajeshwar MotheramMin Ding
    • Gopal KrishnaRajeshwar MotheramMin Ding
    • A61K31/4418A61P9/12C07D213/80
    • A61K31/519A61K9/0019A61K9/10A61K31/435A61K31/4418A61K2300/00
    • Pharmaceutical compositions, and a method of stabilizing pharmaceutical compositions having clevidipine, or any pharmaceutically acceptable salt thereof, as the active ingredient is described. The method includes the slowing down or inhibiting of the oxidation pathway of clevidipine. This can be accomplished by reducing the amount the pharmaceutical composition is exposed to oxygen and/or light during the manufacturing and storing processes. According to this method, oxygen must be removed or replaced, or light must be sufficiently blocked such that light energy cannot reach the active ingredient of the composition, or is reduced to a level that the light-induced oxidation reaction converting clevidipine to H324/78 is minimized, such that the total detectable level of H324/78 in a given composition sample does not exceed about 0.2% on a weight-by-weight basis, or the ratio of clevidipine to H324/78 is equal to or greater than about 450 to 1 on a weight-to-weight basis.
    • 描述了药物组合物和稳定具有氯维地平的药物组合物或其任何药学上可接受的盐作为活性成分的方法。 该方法包括减缓或抑制氯维地平的氧化途径。 这可以通过在制造和储存过程中减少药物组合物暴露于氧和/或光的量来实现。 根据该方法,必须除去或更换氧气,或者必须充分阻挡光,使得光能不能达到组合物的活性成分,或者降低到光诱导的氧化反应将氯维地平转化为H324 / 78 被最小化,使得给定组合物样品中H324 / 78的总可检测水平以重量计不超过约0.2%,或者氯维地平与H324 / 78的比例等于或大于约450 至1,以重量为基准。
    • 4. 发明申请
    • Pharmaceutical compositions and methods for stabilizing the same
    • 药物组合物及其稳定方法
    • US20100105743A1
    • 2010-04-29
    • US12462147
    • 2009-07-30
    • Gopal KrishnaRajeshwar MotheramMin Ding
    • Gopal KrishnaRajeshwar MotheramMin Ding
    • A61K31/44A61P9/12
    • A61K31/519A61K9/0019A61K9/10A61K31/435A61K31/4418A61K2300/00
    • Pharmaceutical compositions, and a method of stabilizing pharmaceutical compositions having clevidipine, or any pharmaceutically acceptable salt thereof, as the active ingredient is described. The method includes the slowing down or inhibiting of the oxidation pathway of clevidipine. This can be accomplished by reducing the amount the pharmaceutical composition is exposed to oxygen and/or light during the manufacturing and storing processes. According to this method, oxygen must be removed or replaced, or light must be sufficiently blocked such that light energy cannot reach the active ingredient of the composition, or is reduced to a level that the light-induced oxidation reaction converting clevidipine to H324/78 is minimized, such that the total detectable level of H324/78 in a given composition sample does not exceed about 0.2% on a weight-by-weight basis, or the ratio of clevidipine to H324/78 is equal to or greater than about 450 to 1 on a weight-to-weight basis.
    • 描述了药物组合物和稳定具有氯维地平的药物组合物或其任何药学上可接受的盐作为活性成分的方法。 该方法包括减缓或抑制氯维地平的氧化途径。 这可以通过在制造和储存过程中减少药物组合物暴露于氧和/或光的量来实现。 根据该方法,必须除去或更换氧气,或者必须充分阻挡光,使得光能不能达到组合物的活性成分,或者降低到光诱导的氧化反应将氯维地平转化为H324 / 78 被最小化,使得给定组合物样品中H324 / 78的总可检测水平以重量计不超过约0.2%,或者氯维地平与H324 / 78的比例等于或大于约450 至1,以重量为基准。