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    Novel Polymorphic Form Of Imatinib Mesylate And A Process For Its Preparation
    3.
    发明申请
    Novel Polymorphic Form Of Imatinib Mesylate And A Process For Its Preparation 有权
    伊马替尼甲磺酸的新型多态性及其制备方法

    公开(公告)号：US20080255138A1

    公开(公告)日：2008-10-16

    申请号：US10585702

    申请日：2004-11-16

    申请人： Kompella Amala ,  Thungathurthi Srinivasa Rao ,  Bhujanga rao Adibhatla Kali Satya ,  Sreenivas Rachakonda ,  Nannapaneni Venkaiah Chowdary ,  Khadgapathi Podili

    发明人： Kompella Amala ,  Thungathurthi Srinivasa Rao ,  Bhujanga rao Adibhatla Kali Satya ,  Sreenivas Rachakonda ,  Nannapaneni Venkaiah Chowdary ,  Khadgapathi Podili

    IPC分类号： A61K31/497 ,  C07D401/14

    CPC分类号： C07D401/04

    摘要： This invention discloses a novel stable crystal form of imatinib mesylate, designated by us as α2 Form, which is stable at room temperature and even at higher temperatures up to 120° C. and accelerated stress conditions and, freely soluble in water. This invention also discloses a pharmaceutical composition containing the novel stable α2 form of Imatinib mesylate and other usually employed excipients, useful in the treatment of Chronic Myelogenous Leukemia (CML). This new α2 Form of imatinib mesylate is prepared by slurrying Imatinib base in isopropanol at room temperature followed by addition of methane sulfonic acid and maintaining 50-60 ° C. followed by filtration. This invention also discloses another process for the preparation of the novel, stable α2 crystalline form of Imatinib Mesylate by the conversion of Imatinib mesylate β-polymorphic modification by suspending it in water and organic solvents, distilling off water azeotropically, cooling and filtering to obtain the α2 crystal form.

    摘要翻译： 本发明公开了一种新颖的稳定的甲磺酸伊马替尼结晶形式，由我们指定为α2 H 2 O形式，其在室温下甚至在高达120℃的较高温度下是稳定的，并且加速的应激条件， 易溶于水。 本发明还公开了一种药物组合物，其含有可用于治疗慢性骨髓性白血病（CML）的新颖的甲磺酸伊马替尼和其它通常使用的赋形剂的稳定的α2 N形式。 通过在室温下将伊马替尼碱分散在异丙醇中，然后加入甲磺酸并保持50-60℃，然后过滤，制备这种新的甲磺酸伊马替尼形式。 本发明还公开了通过将甲磺酸伊马替尼β-多晶型修饰物悬浮在水和有机溶剂中，蒸馏除去水来制备新型稳定的α2结晶形式的伊马替尼甲磺酸盐的另一种方法 共沸，冷却和过滤以获得α2 H 2结晶形式。

    Enteric Soft Gelatin Capsule Containing Esomerpazole And Method Of Preparation
    4.
    发明申请
    Enteric Soft Gelatin Capsule Containing Esomerpazole And Method Of Preparation 审中-公开
    含有Esomerpazole的肠溶软明胶胶囊及其制备方法

    公开(公告)号：US20070196463A1

    公开(公告)日：2007-08-23

    申请号：US10572984

    申请日：2004-09-25

    申请人： Khadgapathi Podili ,  Venkaiah Nannapaneni

    发明人： Khadgapathi Podili ,  Venkaiah Nannapaneni

    IPC分类号： A61K31/4439 ,  A61K9/64

    CPC分类号： A61K9/4825 ,  A61K9/4891 ,  A61K31/4439

    摘要： The present invention relates to an improved pharmaceutical composition, in the form of a soft gel capsule resistant to digestive juice. The composition of the present invention is made up of gelatin and an enteric polymer in the form of free acid or its salt, containing used in the treatment of duodenal ulcers, solublised and/or suspended in a liquid or semisolid medium, comprising the enantiomers of omeprazole such as esomeprazole or rabeprazole or other enantiomers of omeprazole or its salts or derivatives or their mixtures, a hydrophobic carrier, an alkaline inert reacting material and a surface active agent and/or a solublising agent wherein the resulting capsules being insoluble in aqueous medium up to a pH of 5.5 but quickly dissolving above pH of 6.0. The present invention also relates to a process of preparing the above said pharmaceutical composition.

    摘要翻译： 本发明涉及一种抗消化液的软胶囊形式的改进药物组合物。 本发明的组合物由明胶和游离酸或其盐形式的肠溶性聚合物组成，其包含用于治疗十二指肠溃疡，溶解和/或悬浮在液体或半固体培养基中，包括对映异构体 奥美拉唑如奥美拉唑或雷贝拉唑或奥美拉唑或其盐或衍生物或其混合物的其它对映异构体，疏水载体，碱性惰性反应物质和表面活性剂和/或溶解剂，其中所得胶囊不溶于水性介质中 至5.5的pH，但快速溶解于pH6.0以上。 本发明还涉及制备上述药物组合物的方法。

    Polymorphic form of imatinib mesylate and a process for its preparation
    5.
    发明授权
    Polymorphic form of imatinib mesylate and a process for its preparation 有权
    伊马替尼甲磺酸多形态及其制备方法

    公开(公告)号：US08048883B2

    公开(公告)日：2011-11-01

    申请号：US10585702

    申请日：2004-11-16

    申请人： Kompella Amala ,  Thungathurthi Srinivasa Rao ,  Bhujanga rao Adibhatla Kali Satya ,  Sreenivas Rachakonda ,  Nannapaneni Venkaiah Chowdary ,  Khadgapathi Podili

    发明人： Kompella Amala ,  Thungathurthi Srinivasa Rao ,  Bhujanga rao Adibhatla Kali Satya ,  Sreenivas Rachakonda ,  Nannapaneni Venkaiah Chowdary ,  Khadgapathi Podili

    IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D239/02

    CPC分类号： C07D401/04

    摘要： This invention discloses a novel stable crystal form of imatinib mesylate, designated by us as α2 Form, which is stable at room temperature and even at higher temperatures up to 120° C. and accelerated stress conditions and, freely soluble in water. This invention also discloses a pharmaceutical composition containing the novel stable α2 form of Imatinib mesylate and other usually employed excipients, useful in the treatment of Chronic Myelogenous Leukemia (CML). This new α2 Form of imatinib mesylate is prepared by slurrying Imatinib base in isopropanol at room temperature followed by addition of methane sulfonic acid and maintaining 50-60 ° C. followed by filtration. This invention also discloses another process for the preparation of the novel, stable α2 crystalline form of Imatinib Mesylate by the conversion of Imatinib mesylate β-polymorphic modification by suspending it in water and organic solvents, distilling off water azeotropically, cooling and filtering to obtain the α2 crystal form.

    摘要翻译： 本发明公开了一种新颖的甲磺酸伊马替尼结晶形式，由我们称为α2形式，其在室温下甚至在高达120℃的较高温度下是稳定的，并且加速应激条件并且易溶于水。 本发明还公开了一种药物组合物，其含有可用于治疗慢性骨髓性白血病（CML）的新型稳定α2形式的甲磺酸伊马替尼和其它通常使用的赋形剂。 这种新的α2甲磺酸伊马替尼形式是通过在室温下将伊马替尼碱分散在异丙醇中制备的，然后加入甲磺酸并保持50-60℃，然后过滤。 本发明还公开了通过将甲磺酸伊马替尼和bgr-多晶型修饰物悬浮在水和有机溶剂中，通过共沸蒸馏除去水，冷却和过滤来制备新型稳定的α2结晶形式的伊马替尼甲磺酸盐的另一种方法，以获得 α2晶体形式。