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公开(公告)号：US07666876B2
公开(公告)日：2010-02-23
申请号：US10508336
申请日：2002-03-19
IPC分类号： A01N43/42 , A61K31/35 , A61K31/715 , A61F13/00 , C07D498/00 , C07D513/00 , C07D515/00
CPC分类号： A61K31/407 , A61K9/0043 , A61K31/195 , A61K31/196 , A61K31/405 , A61K31/485 , A61K31/54 , A61K31/5415 , A61K47/34 , A61K47/36 , A61K47/38
摘要： Aqueous formulations suitable for intranasal administration comprise buprenorphine or a physiologically acceptable salt or ester thereof and (a) a pectin having a degree of esterification of less than 50%, (b) chitosan and a polyoxyethylene-polyoxypropylene copolymer (poloxamer) or (c) chitosan and hydroxypropylmethylcellulose. Such formulations can induce rapid and prolonged analgesia when delivered intranasally to a patient. The buprenorphine or buprenorphine salt or ester may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration of buprenorphine, Cther, of 0.2 ng/ml or greater which is maintained for a duration Tmaint of at least 2 hours.
摘要翻译： 适用于鼻内给药的水性制剂包括丁丙诺啡或其生理上可接受的盐或酯，和（a）酯化度小于50％的果胶，（b）壳聚糖和聚氧乙烯 - 聚氧丙烯共聚物（泊洛沙姆）或（c） 壳聚糖和羟丙基甲基纤维素。 当向患者鼻内递送时，这样的制剂可以诱导快速和延长的止痛。 丁丙诺啡或丁丙诺啡盐或酯可以在30分钟内输送至0.2ng / ml或更高的丁丙诺啡（Cther）的治疗血浆浓度，其维持持续至少2小时的持续时间。
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公开(公告)号：US20110105551A1
公开(公告)日：2011-05-05
申请号：US12929279
申请日：2011-01-12
IPC分类号： A61K31/485 , A61P25/04 , A61K31/4468 , A61M11/00
CPC分类号： A61K31/407 , A61K9/0043 , A61K31/195 , A61K31/196 , A61K31/405 , A61K31/485 , A61K31/54 , A61K31/5415 , A61K47/34 , A61K47/36 , A61K47/38
摘要： An analgesic and a delivery agent are combined in a pharmaceutical composition such that, on introduction into the nasal cavity of a patient to be treated, the analgesic may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration, Cther, of 0.2 ng/ml or greater which is maintained for a duration Tmaint of at least 2 hours. The analgesic may be an opioid analgesic or a non-steroidal anti-inflammatory drug.
摘要翻译： 将镇痛剂和递送剂组合在药物组合物中，使得在引入待治疗的患者的鼻腔中时，止痛剂可以在30分钟内递送到血流中，治疗血浆浓度Cther为0.2 ng / ml或更高，其保持持续至少2小时的Tmaint。 止痛剂可以是阿片样镇痛药或非甾体抗炎药。
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公开(公告)号：US20100041624A1
公开(公告)日：2010-02-18
申请号：US12588528
申请日：2009-10-19
IPC分类号： A61K31/722 , A61K31/4355
CPC分类号： A61K31/407 , A61K9/0043 , A61K31/195 , A61K31/196 , A61K31/405 , A61K31/485 , A61K31/54 , A61K31/5415 , A61K47/34 , A61K47/36 , A61K47/38
摘要： Aqueous formulations suitable for intranasal administration comprise buprenorphine or a physiologically acceptable salt or ester thereof and (a) a pectin having a degree of esterification of less than 50%, (b) chitosan and a polyoxyethylene-poly-oxypropylene copolymer (poloxamer) or (c) chitosan and hydroxypropylmethylcellulose. Such formulations can induce rapid and prolonged analgesia when delivered intranasally to a patient. The buprenorphine or buprenorphine salt or ester may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration of buprenorphine, Cther, of 0.2 ng/ml or greater which is maintained for a duration Tmaint of at least 2 hours.
摘要翻译： 适用于鼻内给药的水性制剂包括丁丙诺啡或其生理上可接受的盐或酯，和（a）酯化度小于50％的果胶，（b）壳聚糖和聚氧乙烯 - 聚氧化丙烯共聚物（泊洛沙姆）或（ c）壳聚糖和羟丙基甲基纤维素。 当向患者鼻内递送时，这样的制剂可以诱导快速和延长的止痛。 丁丙诺啡或丁丙诺啡盐或酯可以在30分钟内输送至0.2ng / ml或更高的丁丙诺啡（Cther）的治疗血浆浓度，其维持持续至少2小时的持续时间。
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公开(公告)号：US09078814B2
公开(公告)日：2015-07-14
申请号：US13541325
申请日：2012-07-03
IPC分类号： A61F13/00 , A61K31/445 , A01N43/40 , A01N43/16 , A61K31/35 , A61K9/00 , A61K31/4468
CPC分类号： A61K31/4468 , A61K9/0043 , A61K47/26 , A61K47/36 , A61M11/00 , A61M15/08
摘要： An intrasnal spray device contains a composition for the intranasal delivery of fentanyl or a pharmaceutically acceptable salt thereof to an animal includes an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable additive selected from (i) a pectin and (ii) a poloxamer and chitosan or a salt or derivative thereof; provided that when the composition comprises a pectin it is substantially free of divalent metal ions; and which, in comparison to a simple aqueous solution of fentanyl administered intranasally at the same dose, provides a peak plasma concentration of fentanyl (Cmax) that is from 10 to 80% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose. A method for treating or managing pain by intranasally administering the composition is also disclosed.
摘要翻译： 包含用于将芬太尼或其药学上可接受的盐鼻内递送给动物的组合物包括芬太尼或其药学上可接受的盐的水溶液和选自以下的药学上可接受的添加剂：（i）果胶和（ii） 泊洛沙姆和壳聚糖或其盐或衍生物; 条件是当组合物包含果胶时，其基本上不含二价金属离子; 并且与以相同剂量鼻内施用的芬太尼的简单水溶液相比，提供了芬太尼（C max）的峰值血浆浓度，其为使用芬太尼简单的水溶液，其在鼻内给药时的10至80％ 芬太尼剂量相同。 还公开了通过鼻内施用组合物治疗或治疗疼痛的方法。
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公开(公告)号：US08216604B2
公开(公告)日：2012-07-10
申请号：US12047388
申请日：2008-03-13
IPC分类号： A61F13/00 , A61K31/445 , A61K31/35 , A01N43/40 , A01N43/16
CPC分类号： A61K31/4468 , A61K9/0043 , A61K47/26 , A61K47/36 , A61M11/00 , A61M15/08
摘要： A composition for the intranasal delivery of fentanyl or a pharmaceutically acceptable salt thereof to an animal includes an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable additive selected from (i) a pectin and (ii) a poloxamer and chitosan or a salt or derivative thereof; provided that when the composition comprises a pectin it is substantially free of divalent metal ions; and which, in comparison to a simple aqueous solution of fentanyl administered intranasally at the same dose, provides a peak plasma concentration of fentanyl (Cmax) that is from 10 to 80% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose. A method for treating or managing pain by intranasally administering the composition is also disclosed.
摘要翻译： 用于向动物鼻内递送芬太尼或其药学上可接受的盐的组合物包括芬太尼或其药学上可接受的盐的水溶液和选自以下的药学上可接受的添加剂：（i）果胶和（ii）泊洛沙姆和壳聚糖或 其盐或衍生物; 条件是当组合物包含果胶时，其基本上不含二价金属离子; 并且与以相同剂量鼻内施用的芬太尼的简单水溶液相比，提供了芬太尼（C max）的峰值血浆浓度，其为使用芬太尼简单的水溶液在10％至80％ 芬太尼剂量相同。 还公开了通过鼻内施用组合物治疗或治疗疼痛的方法。
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公开(公告)号：US08889176B2
公开(公告)日：2014-11-18
申请号：US13541314
申请日：2012-07-03
IPC分类号： A61F13/00 , A61K31/445 , A01N43/40 , A01N43/16 , A61K31/35
CPC分类号： A61K31/4468 , A61K9/0043 , A61K47/26 , A61K47/36 , A61M11/00 , A61M15/08
摘要： A composition for the intranasal delivery of fentanyl or a pharmaceutically acceptable salt thereof to an animal includes an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable additive selected from (i) a pectin and (ii) a poloxamer and chitosan or a salt or derivative thereof; provided that when the composition comprises a pectin it is substantially free of divalent metal ions; and which, in comparison to a simple aqueous solution of fentanyl administered intranasally at the same dose, provides a peak plasma concentration of fentanyl (Cmax) that is from 10 to 80% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose. A method for treating or managing pain by intranasally administering the composition is also disclosed.
摘要翻译： 用于向动物鼻内递送芬太尼或其药学上可接受的盐的组合物包括芬太尼或其药学上可接受的盐的水溶液和选自以下的药学上可接受的添加剂：（i）果胶和（ii）泊洛沙姆和壳聚糖或 其盐或衍生物; 条件是当组合物包含果胶时，其基本上不含二价金属离子; 并且与以相同剂量鼻内施用的芬太尼的简单水溶液相比，提供了芬太尼（C max）的峰值血浆浓度，其为使用芬太尼简单的水溶液在10％至80％ 芬太尼剂量相同。 还公开了通过鼻内施用组合物治疗或治疗疼痛的方法。
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公开(公告)号：US08034371B2
公开(公告)日：2011-10-11
申请号：US10596817
申请日：2004-12-23
CPC分类号： B82Y5/00 , A61K9/0043 , A61K9/1623 , A61K9/1652 , A61K31/4184 , A61K47/36 , A61K47/40 , A61K47/6951 , Y10S514/923
摘要： The present invention provides compositions for the intranasal administration of zolpidem or a pharmaceutically acceptable salt thereof. Preferred compositions of the invention are in the form of aqueous solutions. Optionally the compositions of the invention comprise a cyclodextrin and/or chitosan, a salt or derivative thereof or a salt of a derivative of chitosan. The compositions can be used for the treatment or prevention insomnia or the treatment of neurological disorders such as those arising from brain trauma, stroke and spinocerebellar ataxia or in the treatment of Parkinson's disease.
摘要翻译： 本发明提供了用于鼻内施用唑吡旦或其药学上可接受的盐的组合物。 本发明的优选组合物是水溶液的形式。 任选地，本发明的组合物包含环糊精和/或壳聚糖，其盐或衍生物或壳聚糖衍生物的盐。 该组合物可用于治疗或预防失眠或治疗诸如由脑创伤，中风和脊髓小脑共济失调引起的神经障碍或治疗帕金森病。
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公开(公告)号：US20080153879A1
公开(公告)日：2008-06-26
申请号：US12047388
申请日：2008-03-13
IPC分类号： A61K31/445 , A61P29/00
CPC分类号： A61K31/4468 , A61K9/0043 , A61K47/26 , A61K47/36 , A61M11/00 , A61M15/08
摘要： A composition for the intranasal delivery of fentanyl or a pharmaceutically acceptable salt thereof to an animal includes an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable additive selected from (i) a pectin and (ii)a poloxamer and chitosan or a salt or derivative thereof; provided that when the composition comprises a pectin it is substantially free of divalent metal ions; and which, in comparison to a simple aqueous solution of fentanyl administered intranasally at the same dose, provides a peak plasma concentration of fentanyl (Cmax) that is from 10 to 80% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose. A method for treating or managing pain by intranasally administering the composition is also disclosed.
摘要翻译： 用于向动物鼻内递送芬太尼或其药学上可接受的盐的组合物包括芬太尼或其药学上可接受的盐的水溶液和选自以下的药学上可接受的添加剂：（i）果胶和（ii）泊洛沙姆和壳聚糖或 其盐或衍生物; 条件是当组合物包含果胶时，其基本上不含二价金属离子; 并且与相同剂量的鼻内施用的芬太尼的简单水溶液相比，提供芬太尼（C max max）的峰值血浆浓度为10至80％，其使用简单的 芬太尼水溶液以相同的芬太尼剂量鼻内给药。 还公开了通过鼻内施用组合物治疗或治疗疼痛的方法。
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