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    Powder formulation disintegrating system and method for dry powder inhalers
    1.
    发明授权
    Powder formulation disintegrating system and method for dry powder inhalers 有权
    粉末制剂粉碎系统和干粉吸入器的方法

    公开(公告)号：US06681768B2

    公开(公告)日：2004-01-27

    申请号：US10177433

    申请日：2002-06-21

    申请人： Anne Haaije de Boer ,  Henderik Willem Frijlink ,  Doetie Gjaltema ,  Joachim Goede ,  Paul Hagedoorn

    发明人： Anne Haaije de Boer ,  Henderik Willem Frijlink ,  Doetie Gjaltema ,  Joachim Goede ,  Paul Hagedoorn

    IPC分类号： A61M1500

    CPC分类号： A61M15/0086 ,  A61M2202/064 ,  A61M2206/16

    摘要： A disperser for dry powders which can be used with different dose systems, dose weights ranging from 2 to 25 mg and different types of powder formulation. In one embodiment, the disperser acts both as a de-agglomeration (disintegration; aerosolization) means and as an air classifier for especially adhesive mixtures. Only fine drug particles are emitted whereas the larger agglomerates and carrier crystals are retained by the disperser. Another embodiment enables time controlled release of carrier crystals in these mixtures. Yet another embodiment has optimized performance with spherical pellets, containing no carrier crystals. Other possible embodiments of the invention make it possible to control the total inhaler resistance and the powder deposition in the upper respiratory tract by means of the addition of a so-called sheath flow of clean air. Modifications also enable carrier retainment in the mouthpiece and elimination of the tangential flow component of the discharge cloud.

    摘要翻译： 用于干粉的分散机，可用于不同剂量系统，​​剂量重量范围为2至25 mg和不同类型的粉末制剂。 在一个实施方案中，分散器既作为去附聚（崩解，雾化）装置，又作为特别是粘合剂混合物的空气分级器。 只有细小的药物颗粒被排出，而较大的附聚物和载体晶体被分散器保留。 另一个实施方案允许在这些混合物中载体晶体的时间控制释放。 另一个实施方案具有不含载体晶体的球形颗粒的优化性能。 本发明的其它可能的实施方案使得可以通过添加所谓的干净空气的鞘流来控制上呼吸道中的总吸入器阻力和粉末沉积。 修改还使得容器保持在接口中并消除排出云的切向流分量。

    Dry powder inhaler and method for pulmonary inhalation of dry powder
    2.
    发明授权
    Dry powder inhaler and method for pulmonary inhalation of dry powder 有权
    干粉吸入器和肺部吸入干粉的方法

    公开(公告)号：US07617822B2

    公开(公告)日：2009-11-17

    申请号：US10561410

    申请日：2004-06-16

    申请人： Anne Haaije De Boer ,  Paul Hagedoorn ,  Henderik Willem Frijlink

    发明人： Anne Haaije De Boer ,  Paul Hagedoorn ,  Henderik Willem Frijlink

    IPC分类号： B05D7/14 ,  B65D83/06 ,  A61M15/00 ,  A61M16/10 ,  A61M15/08

    CPC分类号： A61M15/0091 ,  A61M15/0003 ,  A61M15/0028 ,  A61M15/0043 ,  A61M15/0045 ,  A61M2202/064 ,  A61M2206/16

    摘要： A breath actuated dry powder inhaler, comprising a substantially disc shaped air circulation chamber for de-agglomeration of entrained powdered medicament using the energy of the inspiratory air stream. The chamber has a substantially circular or polygonal sidewall extending about a central axis between top and bottom walls of the chamber so that the height of the chamber is smaller than its diameter. A plurality of air supply channels disposed about the circumference of the chamber, which channels extend from joint or separate air inlets and which channels enter the chamber substantially tangentially to its sidewall. At least one of the supply channels extends through a powder dose supply region of the inhaler. The chamber further comprises an air outlet axially extending from a discharge opening in the centre of the top or bottom wall of the chamber and connects to a discharge channel that extends to a mouthpiece. The inhaler comprises at least one further air circulation chamber for de-agglomeration of entrained powdered medicament, the chambers being connected to the mouthpiece in parallel.

    摘要翻译： 一种呼吸致动的干粉吸入器，包括基本盘形的空气循环腔，用于使用吸气空气流的能量使夹带的粉末状药物脱附。 腔室具有围绕室的顶壁和底壁之间的中心轴线延伸的大致圆形或多边形的侧壁，使得腔室的高度小于其直径。 多个空气供应通道围绕室的周边设置，该通道从接头或单独的空气入口延伸，并且哪个通道基本上相对于其侧壁进入腔室。 至少一个供应通道延伸穿过吸入器的粉末剂量供应区域。 所述室还包括从所述室的顶壁或底壁的中心的排出口轴向延伸的空气出口，并且连接到延伸到接口管的排出通道。 吸入器包括至少一个另外的空气循环室，用于夹带的粉末药物的去附聚，这些腔室平行连接到接口管。

    Peptide Formulations and Uses Thereof
    5.
    发明申请
    Peptide Formulations and Uses Thereof 审中-公开
    肽配方及其用途

    公开(公告)号：US20110237508A1

    公开(公告)日：2011-09-29

    申请号：US13062484

    申请日：2009-09-09

    申请人： Jean-Pierre Amorij ,  Christina Avanti ,  Henderik Willem Frijlink ,  Wouter Leonardus Joseph Hinrichs

    发明人： Jean-Pierre Amorij ,  Christina Avanti ,  Henderik Willem Frijlink ,  Wouter Leonardus Joseph Hinrichs

    IPC分类号： A61K38/11 ,  A61P7/12 ,  A61P7/04 ,  A61P9/00

    CPC分类号： A61K38/095

    摘要： The present invention relates to the field of preventive and therapeutic medicine, in particular to peptide formulations. Provided is a pH-buffered aqueous formulation comprising oxytocin, vasopressin or an analogue thereof and at least one non-toxic source of divalent metal ions in a concentration of at least 2 mM, and the use of the formulation for the manufacture of a medicament for therapeutic and/or prophylactic treatments. Also provided is a method for treating or preventing haemorrhage in a subject in need thereof, comprising administering to said subject an effective dosage amount of an oxytocin formulation according to the invention. Further provided is a method for treating or preventing diabetes insipidus or vasodilatory shock in a subject in need thereof, comprising administering to said subject an effective dosage amount of a vasopressin formulation according to the invention.

    摘要翻译： 本发明涉及预防和治疗药物领域，特别涉及肽制剂。 本发明提供了包含催产素，加压素或其类似物和浓度至少为2mM的至少一种无毒二价金属离子源的pH缓冲水性制剂，以及该制剂用于制备药物的用途 治疗和/或预防性治疗。 还提供了治疗或预防有此需要的受试者的出血的方法，包括向所述受试者施用有效剂量的根据本发明的催产素制剂。 还提供了在有需要的受试者中治疗或预防尿崩症或血管扩张性休克的方法，包括向所述受试者施用有效剂量的根据本发明的加压素制剂。

    PH-Controlled Pulsatile Delivery System, Methods for Preparation and Use Thereof
    6.
    发明申请
    PH-Controlled Pulsatile Delivery System, Methods for Preparation and Use Thereof 审中-公开
    PH控制脉冲递送系统，其制备和使用方法

    公开(公告)号：US20090181089A1

    公开(公告)日：2009-07-16

    申请号：US11989112

    申请日：2005-07-29

    申请人： Reinout Cornelus Andreas Schellekens ,  Henderik Willem Frijlink

    发明人： Reinout Cornelus Andreas Schellekens ,  Henderik Willem Frijlink

    IPC分类号： A61K9/10 ,  A61K9/00

    CPC分类号： A61K9/4891 ,  A61K9/2846 ,  A61K9/286 ,  A61K9/2866 ,  A61K31/00

    摘要： The invention relates to delivery systems that allow for the pulsatile release of a substance, such as a drug, in response to a change in pH. More specifically, it relates to drug administration to the GI tract, in particular to site-specific intestinal drug delivery via the oral route. Provided is a pH-controlled pulsatile release system (PPRS) comprising a core surrounded by a coating layer, wherein said core comprises an active substance and wherein said coating layer comprises a pH-sensitive coating material wherein a swellable agent is embedded. Said swellable agent is capable of taking up at least 1.1 times, preferably at least 5 times, more preferably at least 10 times its weight in water. Also provided is a pharmaceutical composition comprising a PPRS, in particular a colon-specific PPRS.

    摘要翻译： 本发明涉及允许物质（例如药物）响应于pH变化而脉动释放的递送系统。 更具体地说，它涉及到胃肠道的药物给药，特别是通过口服途径给药到特定地点的药物递送。 提供了一种pH控制的脉冲释放系统（PPRS），其包括被涂层包围的芯，其中所述芯包含活性物质，并且其中所述涂层包含其中嵌入有溶胀剂的pH敏感性涂料。 所述可溶胀剂能够在水中占据其重量的至少1.1倍，优选至少5倍，更优选至少10倍。 还提供了包含PPRS，特别是结肠特异性PPRS的药物组合物。