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1. 发明申请

WO2013025442A3 CONCENTRATED FELBAMATE FORMULATIONS FOR PARENTERAL ADMINISTRATION 审中-公开
标题翻译：浓缩的膳食配方用于住院管理
公开(公告)号：WO2013025442A3
公开(公告)日：2013-04-25
申请号：PCT/US2012050148
申请日：2012-08-09
申请人： PEROSPHERE INC , BAKHRU SASHA H , LAULICHT BRYAN E , MATHIOWITZ EDITH , STEINER SOLOMON S
发明人： BAKHRU SASHA H , LAULICHT BRYAN E , MATHIOWITZ EDITH , STEINER SOLOMON S
IPC分类号： A61K31/55 , A61K9/14 , A61K9/16 , A61K31/27 , A61P25/00
CPC分类号： A61K31/27 , A61K9/0019 , A61K9/08 , A61K9/10 , A61K9/145 , A61K31/55 , A61K47/10 , A61K47/20
摘要： Formulations of a neuroprotective agent for parenteral administration are described herein. The formulation is in the form of a concentrated (supersaturated) solution or a concentrated suspension of microparticles. The suspension medium or the solution solvent carrier may also contain dissolved neuroprotective agent. For the supersaturated solutions, the agent is dissolved at high concentrations of at least about 1% by weight, 5% by weight, 10% by weight, 15% by weight, or 20% by weight in a solvent suitable for parenteral administration. For the concentrated suspension, the microparticles have an effective particle size from about 100 nm to about 5 microns, preferably from about 50 nm to about 3 microns, more preferably from about 10 nm to about 2 microns. The formulations described herein can be used to treat a variety of neurological diseases/disorders and/or neurological injury or trauma.
摘要翻译：本文描述了用于肠胃外给药的神经保护剂的制剂。制剂是浓缩（过饱和）溶液或微粒浓缩悬浮液的形式。悬浮介质或溶剂溶剂载体也可以含有溶解的神经保护剂。对于过饱和溶液，在适于肠胃外给药的溶剂中，该试剂以至少约1重量％，5重量％，10重量％，15重量％或20重量％的高浓度溶解。对于浓缩悬浮液，微粒具有约100nm至约5微米，优选约50nm至约3微米，更优选约10nm至约2微米的有效粒度。本文描述的制剂可用于治疗各种神经疾病/障碍和/或神经损伤或创伤。

2. 发明申请

WO2013033400A9 METHODS FOR EFFECTIVELY AND RAPIDLY DESENSITIZING ALLERGIC PATIENTS 审中-公开
公开(公告)号：WO2013033400A9
公开(公告)日：2013-03-07
申请号：PCT/US2012/053145
申请日：2012-08-30
申请人： PEROSPHERE INC. , LAULICHT, Bryan, E. , BAKHRU, Sasha, H. , STEINER, Solomon, S. , MATHIOWITZ, Edith
发明人： LAULICHT, Bryan, E. , BAKHRU, Sasha, H. , STEINER, Solomon, S. , MATHIOWITZ, Edith
IPC分类号： A61K39/35 , A61K9/50 , A61K9/48 , A61K47/30 , A61P37/00

3. 发明申请

WO2012100002A1 DEPLOYABLE BARBED MICRONEEDLE ARRAY AND USES THEREOF 审中-公开
标题翻译：可配置的BARBED MICRONEEDLE ARRAY及其用途
公开(公告)号：WO2012100002A1
公开(公告)日：2012-07-26
申请号：PCT/US2012/021778
申请日：2012-01-18
申请人： MASSACHUSETTS INSTITUTE OF TECHNOLOGY , THE BRIGHAM AND WOMEN'S HOSPITAL, INC. , KARP, Jeffrey, M. , CHO, Woo, Kyung , LAULICHT, Bryan , ANKRUM, James, A. , KARNIK, Rohit, N. , LANGER, Robert
发明人： KARP, Jeffrey, M. , CHO, Woo, Kyung , LAULICHT, Bryan , ANKRUM, James, A. , KARNIK, Rohit, N. , LANGER, Robert
IPC分类号： A61M5/32
CPC分类号： A61B17/205 , A61M37/0015 , A61M2037/0046 , A61M2037/0053 , A61M2037/0061
摘要： The present disclosure provides devices and uses thereof. A devices disclosed herein comprises one or more tips, wherein the one or more tips are designed and constructed to initiate penetration by the device; and one or more protrusions in a region adjacent to each tip. In some embodiments, one or more protrusions can be constructed and arranged so that the required penetration force is reduced as compared with that observed for an otherwise identical device lacking the one or more protrusions. Additionally or alternatively, one or more protrusions can be constructed and arranged such that the required pull-out force is increased as compared with that observed for an otherwise identical device lacking the one or more protrusions.
摘要翻译：本公开提供了其设备及其用途。本文公开的装置包括一个或多个尖端，其中所述一个或多个尖端被设计和构造成启动所述装置的穿透; 以及与每个尖端相邻的区域中的一个或多个突起。在一些实施例中，可以构造和布置一个或多个突起，使得与对于缺少一个或多个突起的其它相同的装置观察到的相比，所需的穿透力减小。附加地或替代地，可以构造和布置一个或多个突起，使得与对于缺少一个或多个突起的其它相同的装置观察到的相比，所需的拉出力增加。

4. 发明申请

WO2006125074A1 DRUG DELIVERY FORMULATIONS FOR TARGETED DELIVERY 审中-公开
标题翻译：用于指定交货的药物递送配方
公开(公告)号：WO2006125074A1
公开(公告)日：2006-11-23
申请号：PCT/US2006/019229
申请日：2006-05-17
申请人： BROWN UNIVERSITY RESEARCH FOUNDATION , MORELLO, Arthur, Peter, III , REINEKE, Joshua , CHEIFETZ, Peter, Matthew , LAULICHT, Bryan , MATHIOWITZ, Edith
发明人： MORELLO, Arthur, Peter, III , REINEKE, Joshua , CHEIFETZ, Peter, Matthew , LAULICHT, Bryan , MATHIOWITZ, Edith
IPC分类号： A61K9/20
CPC分类号： A61K9/0004 , A61K9/0009
摘要： The size and location of microsphere uptake/delivery are important determinants of the final biodistribution of oral microsphere systems. Formulations, kits, methods of administering the formulations, and using the kits are described herein. The formulations are oral dosage formulations. In one embodiment, the formulations contain microparticles and/or nanoparticles having a homogenous size range selected to optimize uptake in a specific region of the GI tract and target drug delivery to specific organs. In some embodiments, the dosage formulation contains an enteric coating and/or a magnetic material. In a preferred embodiment, the formulation contains a magnetic material and an active agent to be delivered, optionally the active agent is in the form of micro- or nano-particles. In some embodiments metallomucoadhesive materials and/or magnetic materials are employed as magnetic and/or mucoadhesive sources. Formulations containing magnetic materials can be localized using the kits and methods disclosed herein. In one embodiment, the method includes orally administering the formulation and applying an extracorporeal magnet to a site on the outside surface of the patient's body in an area that closely apposes the location in the gastrointestinal tract to which delivery of the formulation is desired. The extracorporeal magnet is applied for a suitable time period to allow for the drug to be released from the formulation and/or to allow for the formulation to adhere to the site. Both magnetic and mucoadhesive forces may be utilized to site-direct and retain the dosage fonn in the region of the gastrointestinal (GI) tract most suitable for the desired delivery.
摘要翻译：微球吸收/释放的大小和位置是口腔微球系统最终生物分布的重要决定因素。本文描述了制剂，试剂盒，施用制剂的方法和使用试剂盒。制剂是口服剂型。在一个实施方案中，制剂包含具有选择的均匀尺寸范围的微粒和/或纳米颗粒，以优化GI道的特定区域中的摄取并将靶向药物递送至特定器官。在一些实施方案中，剂量制剂含有肠溶衣和/或磁性材料。在优选的实施方案中，制剂含有磁性材料和待递送的活性剂，任选的活性剂是微粒或纳米颗粒的形式。在一些实施方案中，金属粘着粘附材料和/或磁性材料用作磁性和/或粘膜粘附源。可以使用本文公开的试剂盒和方法来定位含有磁性材料的制剂。在一个实施方案中，该方法包括口服施用该制剂并将一个体外磁体施加到患者身体的外表面上的一个位置，该区域紧密地形成需要递送制剂的胃肠道中的位置。施用体外磁体合适的时间段以允许药物从制剂中释放和/或允许制剂粘附到部位。可以利用磁性和粘膜粘附力来定位直接并将剂量保留在最适合于期望递送的胃肠道（GI）区域中。

5. 发明申请

WO2013025442A2 CONCENTRATED FELBAMATE FORMULATIONS FOR PARENTERAL ADMINISTRATION 审中-公开
标题翻译：用于肠胃外给药的浓缩的佛氨酸盐制剂
公开(公告)号：WO2013025442A2
公开(公告)日：2013-02-21
申请号：PCT/US2012/050148
申请日：2012-08-09
申请人： PEROSPHERE INC. , BAKHRU, Sasha, H. , LAULICHT, Bryan, E. , MATHIOWITZ, Edith , STEINER, Solomon, S.
发明人： BAKHRU, Sasha, H. , LAULICHT, Bryan, E. , MATHIOWITZ, Edith , STEINER, Solomon, S.
IPC分类号： A61K31/55 , A61K31/27 , A61K9/16 , A61K9/14 , A61P25/00
CPC分类号： A61K31/27 , A61K9/0019 , A61K9/08 , A61K9/10 , A61K9/145 , A61K31/55 , A61K47/10 , A61K47/20
摘要： Formulations of a neuroprotective agent for parenteral administration are described herein. The formulation is in the form of a concentrated (supersaturated) solution or a concentrated suspension of microparticles. The suspension medium or the solution solvent carrier may also contain dissolved neuroprotective agent. For the supersaturated solutions, the agent is dissolved at high concentrations of at least about 1% by weight, 5% by weight, 10% by weight, 15% by weight, or 20% by weight in a solvent suitable for parenteral administration. For the concentrated suspension, the microparticles have an effective particle size from about 100 nm to about 5 microns, preferably from about 50 nm to about 3 microns, more preferably from about 10 nm to about 2 microns. The formulations described herein can be used to treat a variety of neurological diseases/disorders and/or neurological injury or trauma.
摘要翻译：本文描述了用于肠胃外给药的神经保护剂的制剂。该制剂为浓缩（过饱和）溶液或微粒浓缩悬浮液的形式。悬浮介质或溶液溶剂载体也可含有溶解的神经保护剂。对于过饱和溶液，试剂以适合非肠道给药的溶剂中以至少约1重量％，5重量％，10重量％，15重量％或20重量％的高浓度溶解。对于浓缩悬浮液，微粒具有约100nm至约5微米，优选约50nm至约3微米，更优选约10nm至约2微米的有效粒度。本文所述的制剂可用于治疗多种神经疾病/病症和/或神经损伤或创伤。

6. 发明申请

WO2007009023A3 CHEMICALLY CROSS-LINKED ELASTOMERIC MICROCAPSULES 审中-公开
标题翻译：化学交联的弹性微球
公开(公告)号：WO2007009023A3
公开(公告)日：2009-04-09
申请号：PCT/US2006027163
申请日：2006-07-12
申请人： ENGINEERED RELEASE SYSTEMS INC , LAULICHT BRYAN E , BAKHRU SASHA
发明人： LAULICHT BRYAN E , BAKHRU SASHA
IPC分类号： A61K9/14
CPC分类号： A61K9/5031
摘要： The present invention relates to the fields of stably encapsulating oral care, skin care, scented, flavoring agents for cued release, and therapeutic agents for extended and sustained release. The invention relates to the stable microencapsulation of these agents for incorporation into dentifrices, topical ointments, microwavable food products, dryer sheets and chewing gums to be released during brushing, applying, heating, tumbling, and masticating respectively. Additionally, the invention encompasses extended and sustained release formulations that achieve reservoir-type delivery of therapeutic agents. The invention discloses methods for manufacturing and post-processing populations of chemically cross-linked elastomeric microcapsules allowing for the incorporation of encapsulated agents into a wide range of formulations without significantly altering their physio-chemical properties while providing for the cued delivery of the encapsulated agent upon the reception of a single or multiple mechanical or thermo-mechanical cues, or extended delivery via diffusion.
摘要翻译：本发明涉及稳定包封口腔护理，皮肤护理，香味，调理释放的调味剂以及用于延长和持续释放的治疗剂的领域。本发明涉及这些试剂稳定的微胶囊化，用于掺入洁牙剂，局部软膏，微波加工食品，干燥片和口香糖中，分别在刷牙，涂抹，加热，翻滚和咀嚼过程中释放。另外，本发明包括实现治疗剂的储库型递送的延长和持续释放制剂。本发明公开了用于制造和后处理化学交联的弹性体微胶囊的种群的方法，其允许将包封的试剂掺入到宽范围的制剂中，而不显着改变其生理化学性质，同时提供包封的药剂的提供递送接收单个或多个机械或热机械线索，或通过扩散延长传送。

7. 发明申请

WO2005041884A9 POLYMER-BASED MICROSTRUCTURES 审中-公开
标题翻译：聚合物基微结构
公开(公告)号：WO2005041884A9
公开(公告)日：2005-06-23
申请号：PCT/US2004036158
申请日：2004-10-29
申请人： ENGINEERED RELEASE SYSTEMS INC , LAULICHT BRYAN E , BAKHRU SASHA
发明人： LAULICHT BRYAN E , BAKHRU SASHA
IPC分类号： A61K20060101 , B01J13/08 , B01J13/14 , A61K
CPC分类号： B01J13/14 , B01J13/08
摘要： The present invention relates to the fields of controlled release of drugs, proteins, nucleic acids, and other pharmaceuticals. It also relates to delivery systems for these agents and other compounds. The invention also relates to stable encapsulation of cells and molecules. The invention provides a population of microstructures comprising a permeable polymer shell, wherein the standard variance in the volume of the microstructures is usually less than or equal to 20 % , preferably 10 % , of the mean, and wherein the diffusion characteristics of the polymer shell vary within the population of microstructures. It also provides for an apparatus and a method of forming a population of microstructures, which method for making microstructures by introducing drops of a polymer solution into a receiving solution under conditions that permit cross-linking of the polymer in the receiving solution. Microstructures of calcium-cross-linked alginate with a chitosin capsule are disclosed.
摘要翻译：本发明涉及药物，蛋白质，核酸和其他药物的控制释放领域。它还涉及这些药剂和其他化合物的递送系统。本发明还涉及细胞和分子的稳定包封。本发明提供了包含可渗透聚合物壳的微结构群，其中微结构体积的标准变化通常小于或等于平均值的20％，优选10％，并且其中聚合物壳的扩散特征在微观结构的人口中变化。本发明还提供了一种形成微结构群体的设备和方法，该设备和方法通过在允许接收溶液中的聚合物交联的条件下通过将聚合物溶液液滴引入接收溶液来制造微结构。公开了用壳聚糖胶囊交联钙交联藻酸盐的微结构。

8. 发明申请

WO2013033400A2 METHODS FOR EFFECTIVELY AND RAPIDLY DESENSITIZING ALLERGIC PATIENTS 审中-公开
标题翻译：有效和快速降解过敏性患者的方法
公开(公告)号：WO2013033400A2
公开(公告)日：2013-03-07
申请号：PCT/US2012053145
申请日：2012-08-30
申请人： PEROSPHERE INC , LAULICHT BRYAN E , BAKHRU SASHA H , STEINER SOLOMON S , MATHIOWITZ EDITH
发明人： LAULICHT BRYAN E , BAKHRU SASHA H , STEINER SOLOMON S , MATHIOWITZ EDITH
IPC分类号： A61K39/35 , A61K9/48 , A61K9/50 , A61K47/30 , A61P37/00
CPC分类号： A61K39/35 , A61K31/43 , A61K31/60 , A61K39/36 , A61K2039/54 , A61K2039/55511 , A61K2039/55555 , A61K2039/55583 , A61K2039/577 , A61M37/0015 , A61M2037/0023 , A61M2037/003 , A61M2037/0061
摘要： Methods and compositions for delivering antigens to the lymphatic system in doses that desensitize patients to future exposure to antigens have been developed. Rapid desensitization is achieved by introducing small quantities of antigen into the lymphatic system. In preferred embodiments, the compositions are administered to yield therapeutically effective levels of antigen within the lymph, where macrophages reside in the greatest concentration, by intradermal administration, using for example, microneedles or microparticles, oral administration, using for example, enteric coated capsules or tablets, or autologous transfusion. In some embodiments, the methods and compositions for delivering antigens orally achieve uptake by the Peyer's patches of the small intestines.
摘要翻译：已经开发了用于将患者未来接触抗原脱敏的剂量将抗原递送至淋巴系统的方法和组合物。通过将少量抗原引入淋巴系统来实现快速脱敏。在优选的实施方案中，施用组合物以通过皮内给药，使用例如微针或微粒，口服给药，使用例如肠溶衣胶囊或淋巴细胞，以产生治疗有效水平的淋巴内的抗原，其中巨噬细胞以最大浓度存在片剂或自体输血。在一些实施方案中，用于递送抗原的方法和组合物通过小肠的派尔氏贴片摄取。

9. 发明申请

WO2012170547A1 BIOADHESIVE DRUG DELIVERY COMPOSITIONS 审中-公开
标题翻译： BIOADHESIVE药物输送组合物
公开(公告)号：WO2012170547A1
公开(公告)日：2012-12-13
申请号：PCT/US2012/041120
申请日：2012-06-06
申请人： PEROSPHERE, INC. , MATHIOWITZ, Edith , STEINER, Solomon S. , LAULICHT, Bryan, E. , BAKHRU, Sasha
发明人： MATHIOWITZ, Edith , STEINER, Solomon S. , LAULICHT, Bryan, E. , BAKHRU, Sasha
IPC分类号： A61K9/48
CPC分类号： A61K47/34 , A61K9/4858 , A61K47/32
摘要： Compositions containing one or more active agents, one or more bioadhesives elements, and one or more charge masking agents are described herein. In some embodiments, the one or more active agents are biomolecules or macromolecules, such as polysaccharides, proteins, peptides, or nucleic acids, which are charged at physiological pH. The one or more charge masking agents are selected based on the nature of the charge on the active agent. The compositions may also contain one or more controlled release materials, such as extended or sustained release materials or delayed release materials, in order to modify release of the active agent.
摘要翻译：本文描述了包含一种或多种活性剂，一种或多种生物粘合剂元件和一种或多种电荷掩蔽剂的组合物。在一些实施方案中，一种或多种活性剂是在生理pH下加入的生物分子或大分子，例如多糖，蛋白质，肽或核酸。基于活性剂上的电荷的性质来选择一种或多种电荷掩蔽剂。为了改变活性剂的释放，组合物还可以含有一种或多种受控释放材料，例如延长或持续释放材料或延迟释放材料。

10. 发明申请

WO2005041884A2 POLYMER-BASED MICROSTRUCTURES 审中-公开
标题翻译：聚合物微结构
公开(公告)号：WO2005041884A2
公开(公告)日：2005-05-12
申请号：PCT/US2004/036158
申请日：2004-10-29
申请人： ENGINEERED RELEASE SYSTEMS, INC , LAULICHT, Bryan, E. , BAKHRU, Sasha
发明人： LAULICHT, Bryan, E. , BAKHRU, Sasha
IPC分类号： A61K
CPC分类号： B01J13/14 , B01J13/08
摘要： The present invention relates to the fields of controlled release of drugs, proteins, nucleic acids, and other pharmaceuticals. It also relates to delivery systems for these agents and other compounds. The invention also relates to stable encapsulation of cells and molecules. The invention provides a population of microstructures comprising a permeable polymer shell, wherein the standard variance in the volume of the microstructures is usually less than or equal to 20 % , preferably 10 % , of the mean, and wherein the diffusion characteristics of the polymer shell vary within the population of microstructures. It also provides for an apparatus and a method of forming a population of microstructures, which method for making microstructures by introducing drops of a polymer solution into a receiving solution under conditions that permit cross-linking of the polymer in the receiving solution. Microstructures of calcium-cross-linked alginate with a chitosin capsule are disclosed.
摘要翻译：本发明涉及药物，蛋白质，核酸和其他药物的控制释放领域。它还涉及这些试剂和其它化合物的递送系统。本发明还涉及细胞和分子的稳定包封。本发明提供了包含可渗透聚合物壳的微观组织群，其中微结构体积的标准差异通常小于或等于平均值的20％，优选10％，并且其中聚合物壳的扩散特性在微观结构的群体内变化。它还提供了一种形成微观结构群的装置和方法，该方法通过在允许聚合物在接收溶液中交联的条件下将聚合物溶液的液滴引入接收溶液来制备微结构。公开了钙交联藻酸盐与壳聚糖胶囊的微结构。

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