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    PHARMACEUTICAL COMPOSITIONS AND METHODS FOR STABILIZING THE SAME
    3.
    发明申请
    PHARMACEUTICAL COMPOSITIONS AND METHODS FOR STABILIZING THE SAME 审中-公开
    药物组合物及其稳定化方法

    公开(公告)号：US20120322836A1

    公开(公告)日：2012-12-20

    申请号：US13600083

    申请日：2012-08-30

    申请人： Gopal Krishna ,  Rajeshwar Motheram ,  Min Ding

    发明人： Gopal Krishna ,  Rajeshwar Motheram ,  Min Ding

    IPC分类号： A61K31/4418 ,  A61P9/12 ,  C07D213/80

    CPC分类号： A61K31/519 ,  A61K9/0019 ,  A61K9/10 ,  A61K31/435 ,  A61K31/4418 ,  A61K2300/00

    摘要： 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.

    摘要翻译： 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。

    Pharmaceutical compositions and methods for stabilizing the same
    4.
    发明申请
    Pharmaceutical compositions and methods for stabilizing the same 审中-公开
    药物组合物及其稳定方法

    公开(公告)号：US20100105743A1

    公开(公告)日：2010-04-29

    申请号：US12462147

    申请日：2009-07-30

    申请人： Gopal Krishna ,  Rajeshwar Motheram ,  Min Ding

    发明人： Gopal Krishna ,  Rajeshwar Motheram ,  Min Ding

    IPC分类号： A61K31/44 ,  A61P9/12

    CPC分类号： A61K31/519 ,  A61K9/0019 ,  A61K9/10 ,  A61K31/435 ,  A61K31/4418 ,  A61K2300/00

    摘要： 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.

    摘要翻译： 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。

    Ready-to-use bivalirudin compositions
    5.
    发明授权
    Ready-to-use bivalirudin compositions 有权

    公开(公告)号：US07803762B1

    公开(公告)日：2010-09-28

    申请号：US12545036

    申请日：2009-08-20

    申请人： Nagesh Palepu ,  Rajeshwar Motheram ,  Praful Shah ,  Gopal Krishna

    发明人： Nagesh Palepu ,  Rajeshwar Motheram ,  Praful Shah ,  Gopal Krishna

    IPC分类号： A61K38/00

    CPC分类号： A61K38/58

    摘要： Ready-to-use bivalirudin compositions, methods of using the ready-to-use bivalirudin compositions, and methods of preparing the ready-to-use bivalirudin compositions. The ready-to-use bivalirudin compositions comprise bivalirudin and one or more stabilizing agents. The one or more stabilizing agents may be buffering agents having a pKa of about 2.5 to about 6.5, pH-adjusting agents, polymers, preservatives, antioxidants, sugars or polyols, or a combination thereof. The ready-to-use bivalirudin compositions may also comprise [9-10]-cycloimido bivalirudin, [11-12]-cycloimido bivalirudin, or a combination thereof. The method of using the ready-to-use bivalirudin compositions comprises administering the ready-to-use compositions to a patient in need thereof. Further, the method of preparing the ready-to-use bivalirudin compositions comprises mixing bivalirudin with one or more stabilizing agents.

    Ready-to-use bivalirudin compositions
    6.
    发明授权
    Ready-to-use bivalirudin compositions 有权
    即用型比伐卢定组合物

    公开(公告)号：US07713928B1

    公开(公告)日：2010-05-11

    申请号：US12563821

    申请日：2009-09-21

    申请人： Nagesh Palepu ,  Rajeshwar Motheram ,  Praful Shah ,  Gopal Krishna

    发明人： Nagesh Palepu ,  Rajeshwar Motheram ,  Praful Shah ,  Gopal Krishna

    IPC分类号： A61K38/00

    CPC分类号： A61K38/58

    摘要： Ready-to-use bivalirudin compositions, methods of using the ready-to-use bivalirudin compositions, and methods of preparing the ready-to-use bivalirudin compositions. The ready-to-use bivalirudin compositions comprise bivalirudin and one or more stabilizing agents. The one or more stabilizing agents may be buffering agents having a pKa of about 2.5 to about 6.5, pH-adjusting agents, polymers, preservatives, antioxidants, sugars or polyols, or a combination thereof. The ready-to-use bivalirudin compositions may also comprise [9-10]-cycloimido bivalirudin, [11-12]-cycloimido bivalirudin, or a combination thereof. The method of using the ready-to-use bivalirudin compositions comprises administering the ready-to-use compositions to a patient in need thereof. Further, the method of preparing the ready-to-use bivalirudin compositions comprises mixing bivalirudin with one or more stabilizing agents.

    摘要翻译： 即用比伐卢定组合物，使用即用比伐卢定组合物的方法，以及制备即用型比伐卢定组合物的方法。 即用型比伐卢列组合物包含比伐卢定和一种或多种稳定剂。 一种或多种稳定剂可以是pKa为约2.5至约6.5的缓冲剂，pH调节剂，聚合物，防腐剂，抗氧化剂，糖或多元醇或其组合。 即用型比伐卢定组合物还可以包含[9-10] - 环亚氨基比伐卢定，[11-12] - 环亚氨基比伐卢定或其组合。 使用即用比伐卢定组合物的方法包括将即用组合物给予有需要的组合物。 此外，制备即用型比伐卢定组合物的方法包括将比伐卢定与一种或多种稳定剂混合。

    Propofol formulation with enhanced microbial characteristics
    10.
    发明授权
    Propofol formulation with enhanced microbial characteristics 失效
    丙泊酚配方具有增强的微生物特性

    公开(公告)号：US6100302A

    公开(公告)日：2000-08-08

    申请号：US286159

    申请日：1999-04-05

    申请人： Satish K. Pejaver ,  Rajeshwar Motheram ,  Barrett E. Rabinow ,  Josben C. dela Rosa

    发明人： Satish K. Pejaver ,  Rajeshwar Motheram ,  Barrett E. Rabinow ,  Josben C. dela Rosa

    IPC分类号： A61K9/107 ,  A61K31/05 ,  A61K47/10 ,  A61K47/24 ,  A61K47/44 ,  A61K47/46 ,  A61P23/00

    CPC分类号： A61K31/05 ,  A61K9/1075 ,  Y10S514/816 ,  Y10S514/938

    摘要： Formulations of intravenous anesthetic propofol emulsions are provided which contain sufficiently low concentrations of soybean oil to produce a stable emulsion and simultaneously provide reduced nutrients, which inhibit microbial growth thereby providing protection against accidental microbial contamination during long-term IV infusions. In addition to the inhibition of microbial growth due to a reduction of nutrients, the formulation exhibits unanticipated additional microbial inhibition due to an increased availability of propofol. The low concentration of soybean oil also provides a formulation that reduces the chances of fat overload when administered over an extended period of time to chronically ill patients.

    摘要翻译： 提供静脉麻醉丙泊酚乳剂的制剂，其含有足够低浓度的大豆油以产生稳定的乳液，同时提供减少的营养物质，其抑制微生物生长，从而在长期IV输注期间提供防止意外的微生物污染的保护。 除了由于营养物质的减少而抑制微生物生长之外，由于异丙酚的可用性的增加，该制剂表现出意外的另外的微生物抑制。 低浓度的大豆油也提供了一种配方，可以在延长的时间内长期服用长期患者时，减少脂肪过量的机会。