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1. 发明申请

WO2013174752A3 SYSTEM COMPOSED OF INHALER AND CAPSULE 审中-公开
标题翻译：系统吸入剂和胶囊
公开(公告)号：WO2013174752A3
公开(公告)日：2014-03-20
申请号：PCT/EP2013060272
申请日：2013-05-17
申请人： BOEHRINGER INGELHEIM INT
发明人： HOLAKOVSKY HOLGER , FRENTZEL-BEYME JESSICA , DUNNE STEPHEN TERENCE , BESSELER JENS , WEILER CLAUDIUS
IPC分类号： A61M15/00 , A61J3/07 , A61K9/00 , A61K9/48 , B65D47/28
CPC分类号： A61K9/0075 , A61J3/071 , A61K9/4808 , A61M15/0028 , A61M15/0043 , A61M2202/064 , B65D47/283
摘要： System composed of an inhaler and a capsule (71). The capsule contains a pharmaceutical preparation, preferably in powder form, which escapes for inhalation from the capsule (71) in the inhaler via at least one hole (72). As capsule elements, the capsule has a capsule cap (1) and a capsule body (2), at least one of which has at least one prefabricated hole. The prefabricated hole in the capsule is sealed in the transport state and is exposed in the application state. The hole is exposed by actuating a tension mechanism. Beforehand, the hole is covered by a capsule receptacle or a film. In one embodiment, the capsule can exist in two different states, e.g. in different insertion positions of the capsule elements. In the first state, the prefabricated hole is closed; in the second state, it is exposed. An inhaler produced from deep-drawn parts or a blister roll and is suitable as a disposable product is also specified.
摘要翻译：从吸入器和胶囊（71）的系统。所述胶囊优选地包括离开所述吸入器在从所述胶囊（71），用于吸入至少一个孔（72）的粉末状药物制剂。胶囊包括在胶囊帽（1）和一个胶囊主体（2），其中的至少一个具有至少一个预制的孔中的胶囊的元件。在胶囊中的预制孔被密封在该系统的传送状态，并且在应用前打开的状态。通过拉动机制的运行中，孔被释放。此前，该孔由胶囊保持器或膜封闭。在一个实施方案中，胶囊可以是在两个不同的状态，例如在不同Einsteckstellungen胶囊元件存在。在预制孔被封闭在第一状态下，第二是它自由。此外，示出了适合作为由深拉部分或从泡罩片的一次性产品吸入器。

2. 发明申请

WO2008061873A3 STABLE POWDER FORMULATION CONTAINING A NOVEL ANTICHOLINERGIC AGENT 审中-公开
标题翻译：稳定粉末配方，包含新的抗胆碱能
公开(公告)号：WO2008061873A3
公开(公告)日：2008-07-10
申请号：PCT/EP2007061910
申请日：2007-11-06
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA , TRUNK MICHAEL , WEILER CLAUDIUS , PIEROTH WERNER
发明人： TRUNK MICHAEL , WEILER CLAUDIUS , PIEROTH WERNER
IPC分类号： A61K9/16 , A61K31/00
CPC分类号： A61K9/0075
摘要： The invention relates to a spray-dried powder formulation comprising particles that contain the following components i) to iii): i) a compound of formula 1, in which A represents a group selected from (I), (II) or (III), R and R' each representing hydrogen or in combination form a group selected from a single bond, -CH 2 - and -O-, and in which X - represents a negatively charged anion, ii) at least one embedding material selected from the group consisting of mono- or disaccharides, oligosaccharides, polymers, sugar alcohols and cholesterol, iii) an organic, physiologically acceptable, sterically demanding acid, selected from the group consisting of ascorbic acid, a monovalent, divalent or trivalent carboxylic acid, preferably fumaric acid, oxalic acid, diacetic acid or a sterically demanding amino acid and a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, a-hydroxycaprylic acid or gluconic acid. The invention also relates to a method for producing said formulation and to the use of an organic, physiologically acceptable, sterically demanding acid, from the group consisting of ascorbic acid, a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, a-hydroxycaprylic acid or gluconic acid and a monovalent, divalent or trivalent carboxylic acid, preferably fumaric acid, oxalic acid, diacetic acid or a sterically demanding amino acid, for stabilising a powder formulation produced by spray-drying containing the aforementioned compound i) of formula 1 and a suitable embedding material ii).
摘要翻译：本发明涉及一种喷雾干燥的粉末制剂，其包含含有以下组分i）至iii粒子）：i）式1的化合物，其中A是选自其中R和R“各自为氢或一起选择的基团形成的基团（1），（2）和（3）选自单键选自，-CH _{2 - 和-O-，并且X ^{- 表示带负电的阴离子，ii）至少选自单糖或二糖，寡糖，聚合物，糖醇和胆甾醇的组中选择的包埋材料，ⅲ）选自抗坏血酸，羧酸单，二或三价的组中的有机的，生理上可接受的，空间要求的酸，优选富马酸，草酸，琥珀酸，或空间要求的氨基酸和水果或可食用的酸，优选Citronensä？重新，酒石酸，苹果酸，MIL chsäure，乙酸，α-hydroxycaprylic或Glucx）甲酸叔中，用于它们的制备方法和使用有机的，生理上可接受的，空间要求的由抗坏血酸，水果或可食用的酸，优选柠檬酸，酒石酸，Äpfetsäure，乳酸，乙酸酸的，S-羟基辛酸或葡糖酸和单 - ，或三价羧酸二 - 优选富马酸，草酸，琥珀酸，或位苛刻氨基酸，用于稳定通过喷雾干燥制备的粉末制剂，含有式1的上述化合物i）和一个合适的嵌入材料ⅱ），}}

3. 发明申请

WO2008061874A2 STABLE POWDER FORMULATION CONTAINING AN ANTICHOLINERGIC AGENT 审中-公开
标题翻译：含有抗胆碱能STABLE粉末制剂
公开(公告)号：WO2008061874A2
公开(公告)日：2008-05-29
申请号：PCT/EP2007061911
申请日：2007-11-06
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA , TRUNK MICHAEL , WEILER CLAUDIUS , PIEROTH WERNER
发明人： TRUNK MICHAEL , WEILER CLAUDIUS , PIEROTH WERNER
CPC分类号： A61K31/5375 , A61K9/0075 , A61K9/1617 , A61K9/1623 , A61K9/1647 , A61K9/1652 , A61K9/1682 , A61K9/4858 , C07D451/12
摘要： The invention relates to a spray-dried powder formulation comprising particles that contain the following components i) to iii): i) anticholinergic agents, in particular at least one compound of formula 1, in which X - represents a negatively charged anion, ii) at least one embedding material selected from the group consisting of mono- or disaccharides, oligosaccharides, polymers, sugar alcohols and cholesterol, iii) an organic, physiologically acceptable, sterically demanding acid, selected from the group consisting of ascorbic acid, a monovalent, divalent or trivalent carboxylic acid, with the exception of amino carboxylic acids, preferably fumaric acid, oxalic acid, or diacetic acid, and a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, a-hydroxycaprylic acid or gluconic acid. The invention also relates to a method for producing said formulation and to the use of an organic, physiologically acceptable, sterically demanding acid from the group consisting of ascorbic acid, a monovalent, divalent or trivalent carboxylic acid, with the exception of amino carboxylic acids, preferably fumaric acid, oxalic acid, or diacetic acid, and a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, a-hydroxycaprylic acid or gluconic acid, for stabilising a powder formulation produced by spray-drying containing the aforementioned compound of formula 1 according to i) and a suitable embedding material ii).
摘要翻译：本发明涉及一种喷雾干燥的粉末制剂，其包含颗粒，含有下列组分i）至iii）：ⅰ）抗胆碱能药，式特别是至少一种化合物（1），其中X ^{- 是带负电荷的阴离子，选自单糖或二糖，寡糖，聚合物，糖醇和胆固醇的组中选择ii）至少一个掩埋材料，ⅲ））是有机的，生理上可接受的，空间要求的选自抗坏血酸，单 - ，二 - 的组中选择的酸或三价羧酸与氨基羧酸，优选富马酸，草酸或琥珀酸，和水果或可食用的酸，优选柠檬酸，酒石酸，苹果酸，乳酸，醋酸，α-羟基辛酸或葡糖酸，它们的制备方法，以及使用有机的例外生理unbedenklic 母鸡，空间要求的酸选自抗坏血酸，单，二或三元羧酸的组中选择，其中的氨基羧酸外，优选富马酸，草酸或琥珀酸，和水果或可食用的酸，优选柠檬酸，酒石酸，苹果酸，乳酸，乙酸，α-羟基辛酸或葡糖酸，用于稳定通过喷雾干燥制备的粉末制剂，含有式的上述化合物（1）根据i）和一个合适的嵌入材料ⅱ）。}

4. 发明申请

WO2005018603A3 SPRAY-DRIED AMORPHOUS BIBN 4096 METHOD FOR PRODUCTION AND USE THEREOF AS INHALANT 审中-公开
标题翻译：喷雾干燥，无定形BIBN 4096，工艺用于生产相同，其作为INHALATIVUM
公开(公告)号：WO2005018603A3
公开(公告)日：2005-07-21
申请号：PCT/EP2004009012
申请日：2004-08-12
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA , TRUNK MICHAEL , WEILER CLAUDIUS
发明人： TRUNK MICHAEL , WEILER CLAUDIUS
IPC分类号： A61K9/00 , A61K31/517 , A61K9/12
CPC分类号： A61K9/0075 , A61K31/517
摘要： The invention relates to the CGRP antagonist 1-[N -[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine (A), or the physiologically-acceptable salts thereof, which are stable in the amorphous state under normal conditions (T
摘要翻译：本发明涉及CGRP拮抗剂1 [N <2> - [3,5-二溴-N - [[4-（3,4-二氢-2（1H）-oxochinazolin -3-基）-1-哌啶基] 羰基] -D-酪氨酰] -L-赖氨酰基] -4-（4-吡啶基） - 哌嗪（A）或它的在无定形状态下在正常条件下生理学上可接受的盐（T <50℃，相对湿度<75％）是稳定的和在微粒的形式，用于制备这些物质的微粒以及用于制备给药吸入粉末的药物形式用于肺和鼻吸入，尤其是对于对头痛，偏头痛和丛集性头痛的治疗的药物的制备中的用途，这些颗粒的方法。

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