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公开(公告)号：SK279964B6
公开(公告)日：1999-06-11
申请号：SK76994
申请日：1992-12-18
Applicant: RORK GERALD S. , PIPKIN JAMES D.
Inventor： RORK GERALD S , PIPKIN JAMES D
Abstract: A device for the controlled delivery of a beneficial agent as a gelatinous dispersion consisting of (i) a core which contains a beneficial agent, a polymer which forms gelatinous microscopic particles upon hydration and if desired an agent to modulate the hydration of the polymer; and (ii) an impermeable, insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of a dispersion comprising gelatinous microscopic particles.
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公开(公告)号：WO2008005692A3
公开(公告)日：2008-01-10
申请号：PCT/US2007/071758
申请日：2007-06-21
Applicant: CYDEX PHARMACEUTICALS, 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.
Abstract: An inhalable formulation containing SAE-γ-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-γ-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- γ-CD is especially useful for solubilizing esterified corticosteroids.
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3.发明申请INHALANT FORMULATION CONTAINING SULFOALKYL ETHER CYCLODEXTRIN AND CORTICOSTEROID PREPARED FROM A UNIT DOSE SUSPENSION 审中-公开含有来自单体剂量悬浮液的硫酸环己酮和角质醇的吸入制剂
公开(公告)号：WO2005065651A1
公开(公告)日：2005-07-21
申请号：PCT/US2005/000084
申请日：2004-12-31
Applicant: CYDEX, INC. , ZIMMERER, Rupert, O. , PIPKIN, James, D. , THOMPSON, Diane, O. , MOSHER, Gerold, L.
Inventor： ZIMMERER, Rupert, O. , PIPKIN, James, D. , THOMPSON, Diane, O. , MOSHER, Gerold, L.
IPC: A61K9/12
CPC classification number: A61K9/0078 , A61K9/0075 , A61K9/08 , A61K31/137 , A61K31/167 , A61K31/46 , A61K31/56 , A61K31/573 , A61K31/58 , A61K47/40 , A61K47/6951 , B82Y5/00 , A61K31/16 , A61K2300/00 , A61K31/57 , A61K31/715
Abstract: An inhalable unit dose liquid 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 aqueóus 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 corticosteroid, such as budesonide. A method of administering the formulation by inhalation is provided. The formulation can also be administered by conventional nasal delivery apparatus. The formulation is prepared by mixing SAE-CD, in solid or liquid (dissolved) form, with an inhalable suspension-based unit dose formulation.
Abstract translation: 提供含有SAE-CD和皮质类固醇的可吸入单位剂量液体制剂。 该制剂适于用任何已知的喷雾器通过雾化给予受试者。 制剂可以包含在试剂盒中。 该制剂作为水溶液或浓缩组合物施用。 该制剂用于通过吸入施用皮质类固醇的改进的雾化系统。 配方中的SAE-CD显着提高了皮质类固醇（如布地奈德）的化学稳定性。 提供了通过吸入给药该制剂的方法。 制剂也可以通过常规的鼻输送装置来施用。 通过将固体或液体（溶解）形式的SAE-CD与可吸入悬浮液的单位剂量制剂混合来制备制剂。
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4.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。
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公开(公告)号：WO1996012478A1
公开(公告)日：1996-05-02
申请号：PCT/US1995013693
申请日：1995-10-19
Applicant: MERCK & CO., INC. , RORK, Gerald, S. , PIPKIN, James, D.
Inventor： MERCK & CO., INC.
IPC: A61K09/24
CPC classification number: A61K9/2027 , A61K9/0004 , A61K9/2072 , A61K31/4422
Abstract: A device for the controlled delivery of a beneficial agent as a gelatinous dispersion consisting of (i) a core which contains a beneficial agent, a polymer which forms microscopic gel beads upon hydration and the core may also contain an agent to modulate the hydration of the polymer; and (ii) an impermeable, insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of the microscopic gel beads.
Abstract translation: 用于作为凝胶状分散体受控输送有益剂的装置，其包含（i）含有有益试剂的核心，在水合时形成微细凝胶珠粒的聚合物和核心，还可含有调节水合作用的试剂 聚合物; 和（ii）不渗透的不溶性涂层，其粘附并包围芯并且包含提供用于微细凝胶珠的水合和释放的区域的孔。
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Patent Agency Ranking
公开(公告)号：WO2005065435A3
公开(公告)日：2005-07-21
申请号：PCT/US2005/000082
申请日：2004-12-31
Applicant: CYDEX, INC. ET AL. , 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: A61K9/12
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.
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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
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。
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8.发明申请CAPSULES CONTAINING AQUEOUS FILL COMPOSITIONS STABILIZED WITH DERIVATIZED CYCLODEXTRIN 审中-公开含有用衍生环糊精稳定的含水填充组合物的胶囊
公开(公告)号：WO2004024126A1
公开(公告)日：2004-03-25
申请号：PCT/US2003/030960
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
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: 包含水，填充组合物的胶囊，所述填充组合物包含水，衍生化的环糊精如磺烷基醚环糊精（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 在储存过程中更多的赋形剂稳定免于其壳的降解，侵蚀，溶胀或溶解。 衍生的环糊精以足以减少，消除或抑制填充组合物中存在的水对壳的降解，侵蚀，溶胀和/或溶解的量存在。 或者，衍生环糊精和另一种壳稳定材料一起使壳稳定化，防止存在于填充组合物中的水发生降解，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性。
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9.发明申请INJECTABLE MELPHALAN COMPOSITIONS COMPRISING A CYCLODEXTRIN DERIVATIVE AND METHODS OF MAKING AND USING THE SAME 审中-公开包含环糊精衍生物的可注射的MELPHALAN组合物及其制备和使用方法
公开(公告)号：WO2010138920A1
公开(公告)日：2010-12-02
申请号：PCT/US2010/036736
申请日：2010-05-28
Applicant: CYDEX PHARMACEUTICALS, INC. , PIPKIN, James, D. , MACHATHA, Stephen, G.
Inventor： PIPKIN, James, D. , MACHATHA, Stephen, G.
IPC: A01N43/04
CPC classification number: A61K31/198 , A61K9/0019 , A61K47/40 , A61K47/6951 , B82Y5/00 , C08B37/0015 , C08L5/16
Abstract: The present invention is directed to pharmaceutical compositions comprising melphalan and a cyclodextrin derivative, and methods of making and using the same.
Abstract translation: 本发明涉及包含美法仑和环糊精衍生物的药物组合物及其制备和使用方法。
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公开(公告)号：WO2009003199A8
公开(公告)日：2010-03-25
申请号：PCT/US2008068872
申请日：2008-06-30
Applicant: CYDEX PHARMACEUTICALS INC , PIPKIN JAMES D , ZIMMERER RUPERT O , SIEBERT JOHN M
Inventor： PIPKIN JAMES D , ZIMMERER RUPERT O , SIEBERT JOHN M
IPC: A01N43/04 , A61K31/715
CPC classification number: A61K31/55 , A61K9/0043 , A61K9/0048 , A61K9/08 , A61K31/335 , A61K31/506 , A61K31/56 , A61K31/57 , A61K31/58 , A61K31/715 , A61K31/724 , A61K45/06 , A61K47/40 , A61M31/00 , A61K2300/00
Abstract: The present invention is directed to methods of treating nasal and/or ophthalmic diseases, symptoms, or disorders that are therapeutically responsive to corticosteroid therapy by delivering aqueous solution formulations comprising a corticosteroid to nasal and ophthalmic tissues. The invention is also directed to methods, systems, devices, and compositions for delivering aqueous solution formulations comprising a corticosteroid and an antihistamine to nasal and ophthalmic tissues. watering eyes
Abstract translation: 本发明涉及通过将包含皮质类固醇的水溶液制剂递送至鼻和眼组织来治疗对皮质类固醇治疗有治疗反应的鼻和/或眼部疾病，症状或病症的方法。 本发明还涉及用于将包含皮质类固醇和抗组胺药物的水溶液制剂递送至鼻和眼组织的方法，系统，装置和组合物。 浇水眼睛
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