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    CAPSULES CONTAINING AQUEOUS FILL COMPOSITIONS STABILIZED WITH DERIVATIZED CYCLODEXTRIN
    2.
    发明申请
    CAPSULES CONTAINING AQUEOUS FILL COMPOSITIONS STABILIZED WITH DERIVATIZED CYCLODEXTRIN 审中-公开
    含有稳定的环糊精的水性填充物组合物的胶囊

    公开(公告)号：WO2004024126B1

    公开(公告)日：2004-07-22

    申请号：PCT/US0330960

    申请日：2003-09-12

    Applicant: CYDEX INC ,  THOMPSON DIANE O ,  ZIMMERER RUPERT O ,  PIPKIN JAMES D

    Inventor： THOMPSON DIANE O ,  ZIMMERER RUPERT O ,  PIPKIN JAMES D

    IPC: A61K9/48 ,  A61K9/52 ,  A61K31/724

    CPC classification number: A61K31/724 ,  A61K9/4866 ,  A61K9/4891

    Abstract: A capsule containing an aqueous fill composition that comprises water, a derivatized cyclodextrin, such as sulfoalkyl ether cyclodextrin (SAE-CD) or hydroxypropyl cyclodextrin (HPCD), optionally one or more active agents and optionally one or more excipients is stabilized from degradation, erosion, swelling or dissolution of its shell during storage. The derivatized cyclodextrin is present in an amount sufficient to reduce, eliminate or inhibit degradation, erosion, swelling and/or dissolution of the shell by water present in the fill composition. Alternatively, the derivatized cyclodextrin and another shell-stabilizing material together stabilize the shell from degradation, erosion, swelling and/or dissolution by water present in the fill composition. The derivatized cyclodextrin can reduce the water activity of the fill composition.

    Abstract translation: 包含含水的水性填充组合物的胶囊，衍生的环糊精，例如磺基烷基醚环糊精（SAE-CD）或羟丙基环糊精（HPCD），任选的一种或多种活性剂和任选的一种或多种赋形剂，其稳定性降低，侵蚀 ，储存期间其壳体溶胀或溶解。 衍生化的环糊精以足以减少，消除或抑制由填充组合物中存在的水引起的壳的降解，侵蚀，溶胀和/或溶解的量存在。 或者，衍生化的环糊精和另一种壳稳定材料一起使壳体不会因存在于填充组合物中的水分而降解，侵蚀，溶胀和/或溶解。 衍生化的环糊精可以降低填充组合物的水分活度。

    USE OF SULFOALKYL ETHER CYCLODEXTRIN AS A PRESERVATIVE
    3.
    发明申请
    USE OF SULFOALKYL ETHER CYCLODEXTRIN AS A PRESERVATIVE 审中-公开
    以维生素C作为防腐剂使用

    公开(公告)号：WO03080079B1

    公开(公告)日：2004-07-15

    申请号：PCT/US0308348

    申请日：2003-03-19

    Applicant: CYDEX INC ,  MOSHER GEROLD L ,  PIPKIN JAMES D ,  ZIMMERER RUPERT O ,  FULK CHRISTINA M ,  THOMPSON DIANE O

    Inventor： MOSHER GEROLD L ,  PIPKIN JAMES D ,  ZIMMERER RUPERT O ,  FULK CHRISTINA M ,  THOMPSON DIANE O

    IPC: A61K9/00 ,  A61K31/05 ,  A61K31/724 ,  A61K47/32 ,  A61K47/34 ,  A61K47/40 ,  A61K47/46 ,  A61K47/48

    CPC classification number: B82Y5/00 ,  A61K9/0019 ,  A61K31/05 ,  A61K31/724 ,  A61K47/40 ,  A61K47/6951 ,  A61K2300/00

    Abstract: A method of preserving formulations is provided. The method includes the step of including a derivatized cyclodextrin in a formulation capable of sustaining microbial growth. One embodiment of the formulation employs a sulfoalkyl ether cyclodextrin as a preservative and optionally as a solubilizing and complexing agent. A suitable cyclodextrin is the CAPTISOL" brand cyclodextrin (sulfobutyl ether R-cyclodextrin). Whether or not the formulation includes a conventional preservative, the formulation will remain preserved for at least a minimum predetermined period. Specific embodiments of the invention include a carrier, a derivatized cyclodextrin and optionally one or more active agents, one or more water activity-reducing agents, and/or one or more complexation-enhancing agents. The derivatized cyclodextrin reduces the water activity of the formulation. A liquid formulation can be lyophilized or otherwise dried to yield a solid formulation that is optionally reconstitutable.

    Abstract translation: 提供了一种保存制剂的方法。 该方法包括将衍生化的环糊精包含在能够维持微生物生长的制剂中的步骤。 制剂的一个实施方案采用磺基烷基醚环糊精作为防腐剂，任选地作为增溶剂和络合剂。 合适的环糊精是CAPTISOL“品牌的环糊精（磺丁基醚R-环糊精），无论制剂是否含有常规的防腐剂，制剂将保持至少保持至少最小的预定时间。本发明的具体实施方案包括载体， 衍生化的环糊精和任选的一种或多种活性剂，一种或多种水活性降低剂和/或一种或多种络合增强剂。衍生化的环糊精降低制剂的水活性。液体制剂可以冻干或以其它方式干燥 以产生任选可重构的固体制剂。

    INHALANT FORMULATION CONTAINING SULFOALKYL ETHER ?-CYCLODEXTRIN AND CORTICOSTEROID
    4.
    发明申请
    INHALANT FORMULATION CONTAINING SULFOALKYL ETHER ?-CYCLODEXTRIN AND CORTICOSTEROID 审中-公开
    含磺酰基醚-β-环糊精和皮质类固醇的含氟制剂

    公开(公告)号：WO2008005692A2

    公开(公告)日：2008-01-10

    申请号：PCT/US2007071758

    申请日：2007-06-21

    Applicant: CYDEX INC ,  PIPKIN JAMES D ,  ZIMMERER RUPERT O ,  THOMPSON DIANE O ,  MOSHER GEROLD L

    Inventor： PIPKIN JAMES D ,  ZIMMERER RUPERT O ,  THOMPSON DIANE O ,  MOSHER GEROLD L

    IPC: A61K31/724 ,  A61K31/573

    CPC classification number: A61K31/573 ,  A61K9/0078 ,  A61K9/19 ,  A61K31/724 ,  A61K45/06 ,  A61K47/40 ,  A61K2300/00

    Abstract: An inhalable formulation containing SAE-?-CD and corticosteroid is provided. The formulation is adapted for administration to a subject by nebulization with any known nebulizer. The formulation can be included in a kit. The formulation is administered as an aqueous solution, however, it can be stored as a dry powder, ready-to-use solution, or concentrated composition. The formulation is employed in an improved nebulization system for administering corticosteroid by inhalation. SAE-?-CD present in the formulation significantly enhances the chemical stability of budesonide. A method of administering the formulation by inhalation is provided. The formulation can also be administered by conventional nasal delivery apparatus. The formulation can include one or more additional therapeutic agents for use in combination with the corticosteroid. SAE- ?-CD is especially useful for solubilizing esterified corticosteroids.

    Abstract translation: 提供含有SAE-β-CD和皮质类固醇的可吸入制剂。 该制剂适于通过用任何已知的雾化器雾化来施用于受试者。 该制剂可以包含在试剂盒中。 该制剂作为水溶液施用，然而，其可以作为干粉，即用溶液或浓缩组合物储存。 该制剂用于通过吸入施用皮质类固醇的改进的雾化系统。 存在于制剂中的SAE-β-CD显着增强了布地奈德的化学稳定性。 提供了通过吸入给药制剂的方法。 该制剂也可以通过常规的鼻输送装置给药。 该制剂可以包括一种或多种与皮质类固醇组合使用的其他治疗剂。 SAE-β-CD对溶解酯化皮质类固醇特别有用。

    DPI FORMULATION CONTAINING SULFOALKYL ETHER CYCLODEXTRIN
    7.
    发明申请
    DPI FORMULATION CONTAINING SULFOALKYL ETHER CYCLODEXTRIN 审中-公开
    含有硫代环戊二烯的DPI配方

    公开(公告)号：WO2005104712A3

    公开(公告)日：2007-06-07

    申请号：PCT/US2005014010

    申请日：2005-04-22

    Applicant: CYDEX INC ,  PIPKIN JAMES D ,  ZIMMERER RUPERT O ,  HICKEY ANTHONY J ,  THOMPSON DIANE O ,  SMYTH HUGH D C

    Inventor： PIPKIN JAMES D ,  ZIMMERER RUPERT O ,  HICKEY ANTHONY J ,  THOMPSON DIANE O ,  SMYTH HUGH D C

    IPC: A61K9/00 ,  A61K9/12 ,  A61K9/14 ,  A61K47/40 ,  C08B37/16

    CPC classification number: A61K47/40 ,  A61K9/0075 ,  Y10T428/2982

    Abstract: An inhalable dry powder formulation containing SAE-CD and an active agent is provided. The formulation is adapted for administration by DPI. The SAE-CD serves as a carrier rather than as an absorption enhancer. The average particle size of the SAE-CD is large enough to preclude (for the most part) pulmonary deposition thereof. Following release from the DPI device, the SAE-CD-containing particles dissociate from the active agent-containing particles in the buccal cavity or throat, after which the active agent-containing particles continue deeper into the respiratory tract. The physicochemical and morphological properties of the SAE-CD are easily modified to permit optimization of active agent and carrier interactions. Drugs having a positive, neutral or negative electrostatic charge can be delivered by DPI when SAE-CD is used as a carrier.

    Abstract translation: 提供含有SAE-CD和活性剂的可吸入干粉配方。 该制剂适用于DPI的给药。 SAE-CD作为载体而不是吸收增强剂。 SAE-CD的平均粒径足够大以排除（大部分）肺沉积。 从DPI装置释放后，含有SAE-CD的颗粒从颊腔或咽喉中的含活性剂颗粒分离，之后含活性剂的颗粒继续深入呼吸道。 SAE-CD的物理化学和形态学特性易于修饰，可以优化活性剂和载体的相互作用。 当使用SAE-CD作为载体时，具有正，中性或负静电电荷的药物可由DPI递送。

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