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1. 发明申请

US20100210506A1 INTRANASAL ADMINISTRATION OF RAPID ACTING INSULIN 审中-公开
标题翻译：快速行动胰岛素的管理管理
公开(公告)号：US20100210506A1
公开(公告)日：2010-08-19
申请号：US12672478
申请日：2006-10-20
申请人： Steven C. Quay , Annemarie Stoudt Cohen , Henry R. Costantino , Shu-Chih Chen Quay , Anthony P. Sileno , Mary S. Kleppe
发明人： Steven C. Quay , Annemarie Stoudt Cohen , Henry R. Costantino , Shu-Chih Chen Quay , Anthony P. Sileno , Mary S. Kleppe
IPC分类号： A61K38/28 , A61P3/10
CPC分类号： A61K9/0043 , A61K38/28 , A61K47/40
摘要： What is described are pharmaceutical compositions, formulations, and uses thereof, for medicaments for intranasal delivery of insulin to a patient, comprising an aqueous mixture of human insulin, a solubilizing agent, and a surface active agent, wherein the human insulin may be rapid actin insulin.
摘要翻译：所描述的是药物组合物，制剂及其用途，用于向患者鼻内递送胰岛素的药物，包括人胰岛素的水性混合物，增溶剂和表面活性剂，其中人胰岛素可以是快速肌动蛋白胰岛素。

2. 发明申请

US20090220435A1 TIGHT JUNCTION MODULATING PEPTIDE COMPONENTS FOR ENHANCING MUCOSAL DELIVERY OF THERAPEUTIC AGENTS 审中-公开
标题翻译：用于增强治疗药物的粘膜递送的轻度结节调节肽组分
公开(公告)号：US20090220435A1
公开(公告)日：2009-09-03
申请号：US11997132
申请日：2006-07-27
申请人： Steven C. Quay , Shu-Chih Chen Quay , Kunyuan Cui , Anthony P. Sileno , Paul Hickok Johnson , Michael E. Houston , Henry R. Costantino , Michael V. Templin
发明人： Steven C. Quay , Shu-Chih Chen Quay , Kunyuan Cui , Anthony P. Sileno , Paul Hickok Johnson , Michael E. Houston , Henry R. Costantino , Michael V. Templin
IPC分类号： A61K9/12 , A61K38/21 , A61K38/20 , A61K39/395 , A61K39/00 , A61K38/28 , A61K38/10 , A61K38/16 , A61K31/7088 , A61K31/60 , A61K31/56 , A61K31/485 , C07K14/00 , C07K7/00
CPC分类号： C07K14/00 , A61K9/0043 , A61K31/55 , A61K38/12 , A61K38/22 , A61K38/23 , A61K45/06 , A61K47/42 , A61K47/60 , A61K2300/00
摘要： Compounds and components including sequences for mucosal epithelial transport of an active agent are given. Tight junction modulating peptide components are described for use in transport and delivery. Permeability can be enhanced with reversibility. Compounds and components for enhanced delivery may be peptide or protein variants, conjugates, or other analog types and structures.
摘要翻译：给出了包括活性剂粘膜上皮转运序列的化合物和组分。描述了紧密连接调节肽组分用于运输和递送。渗透性可以提高可逆性。用于增强递送的化合物和组分可以是肽或蛋白质变体，缀合物或其它类似物和结构。

3. 发明授权

US09993425B2 Compositions for intranasal delivery of human insulin and uses thereof 有权
公开(公告)号：US09993425B2
公开(公告)日：2018-06-12
申请号：US13314080
申请日：2011-12-07
申请人： Henry R. Costantino , Annemarie Stoudt Cohen , Anthony P. Sileno
发明人： Henry R. Costantino , Annemarie Stoudt Cohen , Anthony P. Sileno
IPC分类号： A61K38/28 , A61K9/00 , A61K47/40
CPC分类号： A61K9/0043 , A61K38/28 , A61K47/40
摘要： What is described is a pharmaceutical formulation for intranasal delivery of insulin to a patient, comprising an aqueous mixture of human insulin, a solubilizing agent, a surface active agent, and a thickening agent, wherein said formulation provides a ultra-rapid acting profile to regular human insulin.

4. 发明申请

US20120094903A1 COMPOSITIONS FOR INTRANASAL DELIVERY OF HUMAN INSULIN AND USES THEREOF 有权
标题翻译：人胰岛素输送的组合物及其用途
公开(公告)号：US20120094903A1
公开(公告)日：2012-04-19
申请号：US13314080
申请日：2011-12-07
申请人： Henry R. Costantino , Annemarie Stoudt Cohen , Anthony P. Sileno
发明人： Henry R. Costantino , Annemarie Stoudt Cohen , Anthony P. Sileno
IPC分类号： A61K38/28 , A61P3/08 , A61P3/10
CPC分类号： A61K9/0043 , A61K38/28 , A61K47/40
摘要： What is described is a pharmaceutical formulation for intranasal delivery of insulin to a patient, comprising an aqueous mixture of human insulin, a solubilizing agent, a surface active agent, and a thickening agent, wherein said formulation provides a ultra-rapid acting profile to regular human insulin.
摘要翻译：描述的是用于向患者鼻内递送胰岛素的药物制剂，其包含人胰岛素，增溶剂，表面活性剂和增稠剂的水性混合物，其中所述制剂提供超快速作用轮廓至规则人胰岛素

5. 发明申请

US20090325860A1 COMPOSITIONS FOR INTRANASAL DELIVERY OF HUMAN INSULIN AND USES THEREOF 审中-公开
标题翻译：人胰岛素输送的组合物及其用途
公开(公告)号：US20090325860A1
公开(公告)日：2009-12-31
申请号：US12376205
申请日：2007-04-19
申请人： Henry R. Costantino , Annemarie Stoudt Cohen , Anthony P. Sileno
发明人： Henry R. Costantino , Annemarie Stoudt Cohen , Anthony P. Sileno
IPC分类号： A61K38/28
CPC分类号： A61K9/0043 , A61K38/28 , A61K47/40
摘要： What is described is a pharmaceutical formulation for intranasal delivery of insulin to a patient, comprising an aqueous mixture of human insulin, a solubilizing agent, a surface active agent, and a thickening agent, wherein said formulation provides a ultra-rapid acting profile to regular human insulin.
摘要翻译：描述的是用于向患者鼻内递送胰岛素的药物制剂，其包含人胰岛素，增溶剂，表面活性剂和增稠剂的水性混合物，其中所述制剂提供超快速作用轮廓至规则人胰岛素

6. 发明申请

US20090054326A1 FORMULATIONS FOR ENHANCED MUCOSAL DELIVERY OF PYY 审中-公开
标题翻译：用于增强PYY的粘膜递送的配方
公开(公告)号：US20090054326A1
公开(公告)日：2009-02-26
申请号：US11995315
申请日：2006-07-10
申请人： Henry R. Costantino , Mary S. Kleppe , Annemarie S. Cohen , Anthony P. Sileno
发明人： Henry R. Costantino , Mary S. Kleppe , Annemarie S. Cohen , Anthony P. Sileno
IPC分类号： A61K38/00 , A61P3/00
CPC分类号： A61K38/22 , A61K9/0043 , A61K47/10 , A61K47/183
摘要： Pharmaceutical formulations are described for enhancing mucosal delivery of peptide YY (PYY) to a mammal. A PYY dosage form is described that is suitable for multi-use administration. The PYY dosage form comprises a bottle containing an aqueous pharmaceutical formulation and an actuator effective intranasal administration of the formulation. The formulation comprises a therapeutically effective amount of PYY, a buffer to control pH, a water-miscible polar organic solvent and a chelating agent for cations. The PYY dosage form exhibits at least 90% PYY recovery after storage as used for greater than about five days.
摘要翻译：描述了用于增强对哺乳动物的肽YY（PYY）的粘膜递送的药物制剂。描述了适用于多用途给药的PYY剂型。 PYY剂型包含含有水性药物制剂的瓶子和有效地鼻内施用该制剂的致动器。该制剂包含治疗有效量的PYY，用于控制pH的缓冲液，与水可混溶的极性有机溶剂和用于阳离子的螯合剂。 PYY剂型在储存后显示至少90％的PYY回收率，大于约5天。

7. 发明授权

US09023793B2 Intranasal carbetocin formulations and methods for the treatment of autism 有权
标题翻译：鼻内卡贝缩胆制剂和治疗自闭症的方法
公开(公告)号：US09023793B2
公开(公告)日：2015-05-05
申请号：US13204485
申请日：2011-08-05
申请人： Alexis Kays Leonard , Joshua Orion Sestak , Henry R. Costantino , Anthony P. Sileno , Lalit Raj Peddakota , Kayvon Emile Sharghi , Garland M. Bellamy , Jason Philip Gesty , Steven C. Quay
发明人： Alexis Kays Leonard , Joshua Orion Sestak , Henry R. Costantino , Anthony P. Sileno , Lalit Raj Peddakota , Kayvon Emile Sharghi , Garland M. Bellamy , Jason Philip Gesty , Steven C. Quay
IPC分类号： A61K38/11 , A61P5/10 , A61K9/00 , A61K45/06 , A61K31/337 , A61K9/08
CPC分类号： A61K9/0043 , A61K9/08 , A61K31/337 , A61K45/06 , A61K2300/00
摘要： Methods and compositions containing oxytocin or an oxytocin analog, such as carbetocin, are provided for the prevention and treatment of autism spectrum disorders, related disorders and symptoms of such disorders. The methods and compositions of this disclosure are effective in the treatment of social withdrawal, eye contact avoidance, repetitive behaviors, anxiety, attention deficit, hyperactivity, depression, loss of speech, verbal communication difficulties, aversion to touch, visual difficulties, comprehension difficulties, and sound and light sensitivity. Additional compositions and methods are provided which employ oxytocin or an oxytocin analog in combination with a secondary or adjunctive therapeutic agent to yield more effective treatment tools against autism spectrum disorders and related disorders.
摘要翻译：提供含有催产素或催产素类似物（例如卡贝缩略）的方法和组合物用于预防和治疗自闭症谱系障碍，相关疾病和此类病症的症状。本公开的方法和组成有效地用于治疗社会戒断，避免眼睛接触，重复行为，焦虑，注意力缺陷，多动，抑郁，言语失调，口头沟通困难，厌恶触觉，视力困难，理解困难，声光灵敏度。提供了额外的组合物和方法，其使用催产素或催产素类似物与次要或辅助治疗剂组合以产生针对孤独症谱系障碍和相关病症的更有效的治疗工具。

8. 发明申请

US20120142592A1 NASAL CALCITONIN FORMULATIONS CONTAINING CHLOROBUTANOL 有权
标题翻译：包含氯丁醇的纳卡尔钙钙配方
公开(公告)号：US20120142592A1
公开(公告)日：2012-06-07
申请号：US13371037
申请日：2012-02-10
申请人： Steven C. Quay , Jorge C. de Meireles , Arati A. Deshpande , Zenaida O. Go , Anthony P. Sileno
发明人： Steven C. Quay , Jorge C. de Meireles , Arati A. Deshpande , Zenaida O. Go , Anthony P. Sileno
IPC分类号： A61K38/23 , A61P5/18
CPC分类号： A61K9/0043 , A61K38/23
摘要： An aqueous solution of calcitonin suitable for intranasal administration comprised of calcitonin, chlorobutanol at a concentration of less than 0.4% weight/weight, and water and having a pH of less than 4 with the proviso that benzalkonium chloride is not present in the solution. The aqueous solution of calcitonin can be used to treat osteoporosis, Paget's bone disease and hypercalcemia.
摘要翻译：适于鼻内给药的降钙素水溶液包含浓度小于0.4重量％的降钙素，氯丁醇和水，pH小于4，条件是溶液中不存在苯扎氯铵。降钙素水溶液可用于治疗骨质疏松症，佩吉特骨病和高钙血症。

9. 发明授权

US08003353B2 Cyanocobalamin low viscosity aqueous formulations for intranasal delivery 有权
公开(公告)号：US08003353B2
公开(公告)日：2011-08-23
申请号：US12142240
申请日：2008-06-19
申请人： Steven C. Quay , Peter C. Aprile , Zenaida O. Go , Anthony P. Sileno
发明人： Steven C. Quay , Peter C. Aprile , Zenaida O. Go , Anthony P. Sileno
IPC分类号： C12P19/42 , A61K31/70 , A01N43/04 , C07H19/20
CPC分类号： A61K9/0043 , A61K9/08 , A61K31/7056 , A61K31/714 , A61K47/10 , A61K47/12 , A61K47/186
摘要： A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.1 comprising intranasally administering an aqueous solution of a cyanocobalamin, wherein said solution of cyanocobalamin has a bioavailability of at least 7% relative to an intramuscular injection of a cyanocobalamin.

10. 发明申请

US20120190640A1 CYANOCOBALAMIN LOW VISCOSITY AQUEOUS FORMULATIONS FOR INTRANASAL DELIVERY 有权
标题翻译：氰钴胺低粘度水性配方
公开(公告)号：US20120190640A1
公开(公告)日：2012-07-26
申请号：US13189061
申请日：2011-07-22
申请人： Steven C. QUAY , Peter C. Aprile , Zenaida O. Go , Anthony P. Sileno
发明人： Steven C. QUAY , Peter C. Aprile , Zenaida O. Go , Anthony P. Sileno
IPC分类号： A61K31/714 , A61P3/02
CPC分类号： A61K9/0043 , A61K9/08 , A61K31/7056 , A61K31/714 , A61K47/10 , A61K47/12 , A61K47/186
摘要： A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering, intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.1 comprising intranasally administering an aqueous solution of a cyanocobalamin, wherein said solution of cyanocobalamin has a bioavailability of at least 7% relative to an intramuscular injection of a cyanocobalamin.
摘要翻译：一种由氰钴胺素和水组成的稳定的药用无汞水溶液，其中所述氰钴胺溶液适合于鼻内给药，其粘度小于约1000cPs，其中所述氰钴胺溶液在鼻内给药时具有氰钴胺素的生物利用度相对于肌内注射氰钴胺素至少约7％，条件是溶液基本上不含汞和含汞化合物。本发明还涉及提高脑脊髓液（CSF）中的维生素B12水平的方法，其包括鼻内施用足量的无水银氰钴胺溶液，以增加CSF中维生素B12的平均比例与血液中的血清（B12 CSF / B12血清×100）相比至至少约1.1，其包括鼻内施用氰钴胺水溶液，其中所述氰钴胺溶液相对于肌内注射的生物利用度为至少7％氰钴胺素

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