公开(公告)号：US20210008060A1

公开(公告)日：2021-01-14

申请号：US16939717

申请日：2020-07-27

申请人： Orexo AB

发明人： Jonas Sävmarker ,  Robert Rönn ,  Andreas Fischer

IPC分类号： A61K31/485 ,  A61K9/16 ,  A61K9/00

摘要： According to the invention, there is provided a solid pharmaceutical composition formulation for nasal delivery of an opioid antagonist, comprising a pharmacologically-effective amount of an opioid antagonist and a pharmaceutically-acceptable carrier. Said compositions are preferably in the form of a powder produced by spray-drying, which are subsequently loaded into single use nasal applicators. Preferred pharmaceutically-acceptable carriers in this regard include disaccharides (e.g. lactose or trehalose) and dextrins (e.g. cyclodextrins or maltodextrins), preferably spray-dried together in combination. Compositions may further comprise an alkyl saccharide, preferably a sucrose ester, such as sucrose monolaurate. Said compositions and applicators may be employed in the treatment of opioid overdose in subjects.

公开(公告)号：US20170071927A1

公开(公告)日：2017-03-16

申请号：US15138570

申请日：2016-04-26

申请人： Orexo AB

发明人： Anders Pettersson ,  Barbro Johansson ,  Emil Schwan

IPC分类号： A61K31/454 ,  A61K9/20 ,  A61K9/00

CPC分类号： A61K31/454 ,  A61K9/0056 ,  A61K9/006 ,  A61K9/1623 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2077

摘要： There is provided pharmaceutical compositions for the treatment of pain e.g. short-term pain, which compositions comprise a mixture comprising: (a) microparticles of alfentanil, or a pharmaceutically acceptable salt thereof, which microparticles are presented on the surfaces of larger carrier particles; (b) a water-soluble weak base; and (c) a compound which is a weak acid, which acid is presented in intimate mixture with the microparticles of alfentanil or salt thereof. The composition may further comprise a disintegrant. The acid is preferably citric acid.

摘要翻译： 组合物还可以包含崩解剂。 酸优选为柠檬酸。

公开(公告)号：US09408843B2

公开(公告)日：2016-08-09

申请号：US14577823

申请日：2014-12-19

申请人： Orexo AB

发明人： Andreas Fischer

IPC分类号： A61K31/4748 ,  A61K9/14 ,  A61K31/485 ,  A61K9/20 ,  A61K9/00

摘要： There is provided pharmaceutical compositions for the treatment of e.g. opioid dependency comprising microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof, in associative admixture with particles comprising a weak acid, or particles comprising weakly-acidic buffer forming materials. The composition may further comprise a disintegrant and/or particles of a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof. The compositions are useful in the treatment of opioid dependency/addiction and/or pain.

公开(公告)号：US20150238482A1

公开(公告)日：2015-08-27

申请号：US14699889

申请日：2015-04-29

申请人： Orexo AB

发明人： Andreas Fischer

IPC分类号： A61K31/485 ,  A61K9/20

CPC分类号： A61K31/485 ,  A61K9/0056 ,  A61K9/006 ,  A61K9/14 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/2095 ,  A61K31/4748

摘要： There is provided pharmaceutical compositions for the treatment of e.g. opioid dependency comprising microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof, in associative admixture with particles comprising a weak acid, or particles comprising weakly-acidic buffer forming materials. The composition may further comprise a disintegrant and/or particles of a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof. The compositions are useful in the treatment of opioid dependency/addiction and/or pain.

摘要翻译： 提供了用于治疗例如药物的药物组合物。 包含药理学有效量的丁丙诺啡或其药学上可接受的盐的微粒与包含弱酸的微粒或包含弱酸性缓冲液形成材料的颗粒的缔合混合物中的阿片样物质依赖性。 组合物还可以包含崩解剂和/或药理学有效量的纳洛酮或其药学上可接受的盐的颗粒。 该组合物可用于治疗阿片依赖性/成瘾和/或疼痛。

公开(公告)号：US08815911B2

公开(公告)日：2014-08-26

申请号：US13874762

申请日：2013-05-01

申请人： Orexo AB

发明人： Anders Pettersson ,  Barbro Johansson ,  Emil Schwan

IPC分类号： A61K31/445 ,  A61K9/20

CPC分类号： A61K31/454 ,  A61K9/0056 ,  A61K9/006 ,  A61K9/1623 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2077

摘要： There is provided pharmaceutical compositions for the treatment of pain e.g. short-term pain, which compositions comprise a mixture comprising: (a) microparticles of alfentanil, or a pharmaceutically acceptable salt thereof, which microparticles are presented on the surfaces of larger carrier particles; (b) a water-soluble weak base; and (c) a compound which is a weak acid, which acid is presented in intimate mixture with the microparticles of alfentanil or salt thereof. The composition may further comprise a disintegrant. The acid is preferably citric acid.

摘要翻译： 提供了用于治疗疼痛的药物组合物。 短期疼痛，所述组合物包含混合物，所述混合物包含：（a）微球呈现在较大载体颗粒表面上的阿芬太尼微粒或其药学上可接受的盐; （b）水溶性弱碱; 和（c）作为弱酸的化合物，该酸与阿芬太尼或其盐的微粒紧密混合存在。 组合物还可以包含崩解剂。 酸优选为柠檬酸。

公开(公告)号：US20140030336A1

公开(公告)日：2014-01-30

申请号：US13954141

申请日：2013-07-30

申请人： Orexo AB

发明人： Anders Pettersson ,  Christer Nystrom

IPC分类号： A61K9/00 ,  A61K38/22 ,  A61K9/14 ,  A61K31/196 ,  A61K31/4468 ,  A61K31/635 ,  A61K31/4439

CPC分类号： A61K9/006 ,  A61K9/0056 ,  A61K9/145 ,  A61K9/146 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2866 ,  A61K31/136 ,  A61K31/19 ,  A61K31/196 ,  A61K31/34 ,  A61K31/341 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/4745 ,  A61K31/485 ,  A61K31/4985 ,  A61K31/5415 ,  A61K31/5513 ,  A61K31/635 ,  A61K36/84 ,  A61K38/00 ,  A61K38/2242

摘要： A pharmaceutical composition for the treatment or acute disorders is described. The composition comprises an essentially water-free, ordered mixture of at least one pharmaceutically active agent in the form of microparticles which are adhered to the surfaces of carrier particles which are substantially larger than the particles of the active agent or agents, and are essentially water-soluble, in combination with the bioadhesion and/or mucoadhesion promoting agent. The invention also relates to a method for preparing the composition and to the use of the composition for the treatment of acute disorders.

摘要翻译： 描述了用于治疗或急性疾病的药物组合物。 该组合物包含至少一种呈微粒形式的至少一种药物活性剂的基本上无水的有序混合物，所述药物活性剂粘附到载体颗粒的表面上，其基本上大于活性剂或试剂的颗粒，并且基本上为水 与生物粘附和/或粘膜粘附促进剂组合。 本发明还涉及一种制备组合物的方法以及用于治疗急性疾病的组合物的用途。

公开(公告)号：US20140005223A1

公开(公告)日：2014-01-02

申请号：US13874762

申请日：2013-05-01

申请人： Orexo AB

发明人： Anders Pettersson ,  Barbro Johansson ,  Emil Schwan

IPC分类号： A61K31/454

CPC分类号： A61K31/454 ,  A61K9/0056 ,  A61K9/006 ,  A61K9/1623 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2077

摘要： There is provided pharmaceutical compositions for the treatment of pain e.g. short-term pain, which compositions comprise a mixture comprising: (a) microparticles of alfentanil, or a pharmaceutically acceptable salt thereof, which microparticles are presented on the surfaces of larger carrier particles; (b) a water-soluble weak base; and (c) a compound which is a weak acid, which acid is presented in intimate mixture with the microparticles of alfentanil or salt thereof. The composition may further comprise a disintegrant. The acid is preferably citric acid.

摘要翻译： 提供了用于治疗疼痛的药物组合物。 短期疼痛，所述组合物包含混合物，所述混合物包含：（a）微球呈现在较大载体颗粒表面上的阿芬太尼微粒或其药学上可接受的盐; （b）水溶性弱碱; 和（c）作为弱酸的化合物，该酸与阿芬太尼或其盐的微粒紧密混合存在。 组合物还可以包含崩解剂。 酸优选为柠檬酸。

公开(公告)号：US20230355552A1

公开(公告)日：2023-11-09

申请号：US18323101

申请日：2023-05-24

申请人： OREXO AB

发明人： Jonas SÄVMARKER ,  Robert RÖNN

IPC分类号： A61K31/137 ,  A61M15/08 ,  A61K9/16 ,  A61K9/00

CPC分类号： A61K31/137 ,  A61K9/0043 ,  A61K9/1652 ,  A61M15/08 ,  A61M2209/06

摘要： Disclosed is a pharmaceutically-acceptable composition in the form of a solid, amorphous, mono-particulate powder comprising a mixture of:

(a) a pharmacologically-effective dosage amount of an adrenergic receptor modulator, or a pharmaceutically-acceptable salt thereof; and
(b) a pharmaceutically-acceptable carrier material, which carrier material comprises a maltodextrin with a dextrose equivalent (DE) that is above 15.

Compositions are suitable for transmucosal drug delivery, including nasal delivery, by which said compositions may be loaded into a single-use nasal applicator. Compositions are preferably made by way of spray drying and may further include a disaccharide, such as lactose or trehalose which, along with the active ingredient and maltodextrin, may be spray-dried together in combination. Compositions may further comprise one or more alkyl saccharides. Preferred alkyl saccharides include sucrose esters, such as sucrose monolaurate. Preferred adrenergic receptor modulators include epinephrine (adrenaline). The compositions are thus particularly useful in the treatment of allergic reactions, including anaphylaxis.

公开(公告)号：US11433066B2

公开(公告)日：2022-09-06

申请号：US17032882

申请日：2020-09-25

申请人： Orexo AB

发明人： Andreas Fischer

IPC分类号： A61K31/485 ,  A61K9/14 ,  A61K9/20 ,  A61K9/00 ,  A61K31/4748

摘要： There is provided pharmaceutical compositions for the treatment of e.g. opioid dependency comprising microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof, in associative admixture with particles comprising a weak acid, or particles comprising weakly-acidic buffer forming materials. The composition may further comprise a disintegrant and/or particles of a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof. The compositions are useful in the treatment of opioid dependency/addiction and/or pain.

公开(公告)号：US10898480B1

公开(公告)日：2021-01-26

申请号：US16939660

申请日：2020-07-27

申请人： Orexo AB

发明人： Jonas Sävmarker ,  Robert Rönn

IPC分类号： A61K9/16 ,  A61K31/70 ,  A61P25/36 ,  A61K31/485 ,  A61K9/00

摘要： According to the invention, there is provided a solid pharmaceutical composition formulation for nasal delivery of an opioid antagonist, comprising a pharmacologically-effective amount of an opioid antagonist and a pharmaceutically-acceptable carrier. The compositions are preferably in the form of a powder produced by spray-drying, which are subsequently loaded into single use nasal applicators. Preferred pharmaceutically-acceptable carriers in this regard include disaccharides (e.g. lactose or trehalose) and dextrins (e.g. cyclodextrins or maltodextrins), preferably spray-dried together in combination. Compositions may further comprise an alkyl saccharide, preferably a sucrose ester, such as sucrose monolaurate. The compositions and applicators may be employed in the treatment of opioid overdose in subjects.