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91. 发明申请

US20050106248A1 Extended release venlafaxine formulation 有权
标题翻译：延长释放文拉法辛配方
公开(公告)号：US20050106248A1
公开(公告)日：2005-05-19
申请号：US10715219
申请日：2003-11-17
申请人： Manesh Dixit , Xiu-Xiu Cheng , Avinash Nangia , Chih Chen
发明人： Manesh Dixit , Xiu-Xiu Cheng , Avinash Nangia , Chih Chen
IPC分类号： A61K20060101 , A61K9/16 , A61K9/22 , A61K9/26 , A61K9/48 , A61K9/50 , A61K31/137
CPC分类号： A61K9/48 , A61K9/1676 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5078 , A61K9/5084 , A61K31/137
摘要： A controlled release dosage form of venlafaxine that comprises an immediate release pellet and an extended release pellet.
摘要翻译：文拉法辛的控释剂型，其包含速释丸和延长释放丸。

92. 发明申请

US20050106247A1 Modified release dosage forms of skeletal muscle relaxants 有权
标题翻译：骨骼肌松弛剂的改性释放剂型
公开(公告)号：US20050106247A1
公开(公告)日：2005-05-19
申请号：US10713929
申请日：2003-11-14
申请人： Gopi Venkatesh , James Clevenger
发明人： Gopi Venkatesh , James Clevenger
IPC分类号： A61K9/50 , A61K31/5513 , A61K9/26
CPC分类号： A61K31/135 , A61K9/0053 , A61K9/1652 , A61K9/2054 , A61K9/4808 , A61K9/4866 , A61K9/5078 , A61K31/137 , A61K31/5513 , Y10T29/49826
摘要： A unit dosage form, such as a capsule or the like, for delivering a skeletal muscle relaxant, such as cyclobenzaprine hydrochloride, into the body in an extended or sustained release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed. At least one bead population exhibits a pre-designed sustained release profile. Such a drug delivery system is designed for once-daily oral administration to maintain an adequate plasma concentration—time profile, thereby providing relief of muscle spasm associated with painful musculoskeletal conditions over a 24 hour period.
摘要翻译：用于以延长或持续释放的方式将骨骼肌松弛剂（例如盐酸环苯扎林）输送到体内的单位剂型，包括一种或多种含药颗粒群（珠粒，丸粒，颗粒等）。至少一个珠粒表现出预先设计的持续释放特征。这种药物递送系统设计为每日一次口服给药以维持足够的血浆浓度 - 时间特征，从而在24小时内缓解与疼痛的肌肉骨骼病症相关的肌肉痉挛。

93. 发明申请

US20050079218A1 Matrices for the stabilizing and controlled release of problematic substances 审中-公开
标题翻译：用于稳定和控制释放有问题的物质的矩阵
公开(公告)号：US20050079218A1
公开(公告)日：2005-04-14
申请号：US10498722
申请日：2002-12-12
申请人： Achim Gopferich , Angelika Maschke
发明人： Achim Gopferich , Angelika Maschke
IPC分类号： A61K9/16 , A61K9/20 , A61K9/22 , A61K9/26 , A61K9/48 , A61K47/06 , A61K47/14 , A61K47/34 , A61K47/36 , A61K47/44 , A61K47/46
CPC分类号： A61K9/1617 , A61K9/0019 , A61K9/1694 , A61K9/2013 , A61K9/4858 , A61K47/06 , A61K47/36
摘要： The invention concerns a carrier system for stabilizing and controlled release of active substances, in particular problematic pharmaceutical substances in a biological environment. Said carrier system comprises a lipid matrix having water solubility corresponding to one part of the lipid matrix for 30 parts of water, and at least a release controlling substance, said substance being insoluble in the lipid matrix.
摘要翻译：本发明涉及用于在生物环境中稳定和控制活性物质特别是有问题的药物物质的载体系统。所述载体系统包含具有水溶性的脂质基质，其对应于30份水的脂质基质的一部分，以及至少一种释放控制物质，所述物质不溶于脂质基质。

94. 发明申请

US20050064034A1 Oral extended-release composition 有权
标题翻译：口服缓释组合物
公开(公告)号：US20050064034A1
公开(公告)日：2005-03-24
申请号：US10869497
申请日：2004-06-16
申请人： Boyong Li , Avinash Nangia , Monte Browder
发明人： Boyong Li , Avinash Nangia , Monte Browder
IPC分类号： A61K20060101 , A61K9/14 , A61K9/20 , A61K9/22 , A61K9/24 , A61K9/26 , A61K9/28 , A61K9/48 , A61K9/54
CPC分类号： A61K9/2077 , A61K9/1652 , A61K9/5084
摘要： The invention is directed to controlled release formulations containing drugs which are preferably considered sparingly soluble to insoluble and which are suitable for administration to a patient in need of treatment related thereto, and methods of manufacturing the same.
摘要翻译：本发明涉及含有药物的控制释放制剂，其优选被认为是微溶于不溶性并且适用于需要与之有关的治疗的患者的给药及其制备方法。

95. 发明申请

US20050063913A1 Novel metaxalone compositions 审中-公开
标题翻译：新颖的美他沙酮组合物
公开(公告)号：US20050063913A1
公开(公告)日：2005-03-24
申请号：US10912552
申请日：2004-08-06
申请人： John Pruitt , Tuula Ryde , H. Bosch
发明人： John Pruitt , Tuula Ryde , H. Bosch
IPC分类号： A61K9/14 , A61K9/26 , A61K9/48 , A61K9/51 , A61K31/421 , A61K49/04 , A61L9/04
CPC分类号： A61K31/421 , A61K9/145 , A61K9/146
摘要： The present invention is directed to nanoparticulate compositions comprising metaxalone. The metaxalone particles of the composition have an effective average particle size of less than about 2 microns.
摘要翻译：本发明涉及包含美他沙酮的纳米颗粒组合物。组合物的美他曲酮颗粒具有小于约2微米的有效平均粒度。

96. 发明申请

US20050058710A1 Porous drug matrices and methods of manufacture thereof 审中-公开
标题翻译：多孔药物基质及其制造方法
公开(公告)号：US20050058710A1
公开(公告)日：2005-03-17
申请号：US10928886
申请日：2004-08-27
申请人： Julie Straub , David Altreuter , Howard Bernstein , Donald Chickering , Sarwat Khattak , Greg Randall
发明人： Julie Straub , David Altreuter , Howard Bernstein , Donald Chickering , Sarwat Khattak , Greg Randall
IPC分类号： A61K9/16 , A61K9/26 , A61K9/14
CPC分类号： A61K9/1635 , A61K9/1611 , A61K9/1623 , A61K9/1688 , A61K9/1694
摘要： Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.
摘要翻译：药物，特别是低含水溶性药物以多孔基质形式提供，优选微粒，其增强药物在水性介质中的溶解。药物基质优选使用以下方法制备，所述方法包括（i）将挥发性溶剂中的药物（优选为低溶解度的药物）溶解以形成药物溶液，（ii）将至少一种成孔剂与药物溶液以形成稳定药物并抑制结晶的乳液，悬浮液或第二溶液和亲水或疏水赋形剂，和（iii）从乳液，悬浮液或第二溶液中除去挥发性溶剂和成孔剂以产生多孔基质药物。可以选择疏水性或亲水性赋形剂，以通过抑制晶体生长来稳定药物的结晶形式，或者通过防止结晶来稳定药物的无定形形式。成孔剂可以是与药物溶剂或挥发性固体化合物，优选挥发性盐不混溶的挥发性液体。在优选的实施方案中，使用喷雾干燥来除去溶剂和成孔剂。与药物的无孔基质形式相比，得到的多孔基质在给予患者后具有更快的溶解速率。在优选的实施方案中，多孔药物基质的微粒用水性介质重新配制，并肠胃外给药，或使用标准技术加工成用于口服给药的片剂或胶囊。

97. 发明申请

US20050053655A1 Rapid disintegrating tablets (RDTs) for pharmaceutical use and method for preparing the same 审中-公开
标题翻译：用于药物用途的快速崩解片（RDT）及其制备方法
公开(公告)号：US20050053655A1
公开(公告)日：2005-03-10
申请号：US10655310
申请日：2003-09-05
申请人： Chih-Chiang Yang , Wen-Che Wang , Hui-Yu Chen
发明人： Chih-Chiang Yang , Wen-Che Wang , Hui-Yu Chen
IPC分类号： A61K9/20 , A61K9/26 , A61K31/60
CPC分类号： A61K9/2081 , A61K31/60
摘要： The present invention provides a fast-disintegrating tablet (RDT) and the method of preparing the RDT. The RDT contains a plurality of microcapsules which contains an active pharmaceutical ingredient surrounded by a polymeric matrix formed by a hydrogel. The microcapsules are separated from each other by a surfactant, particularly lecithin. The RDT is particularly suitable for use as a drug delivery system for antiacid or antiulcer drugs, such as famotidine. The RDT is further characterized by their its fast disintegration time of about 3 second to 3 minutes.
摘要翻译：本发明提供快速崩解片（RDT）和RDT的制备方法。 RDT含有多个微胶囊，其包含被由水凝胶形成的聚合物基质包围的活性药物成分。微胶囊通过表面活性剂，特别是卵磷脂彼此分离。 RDT特别适合用作抗酸或抗溃疡药物如法莫替丁的药物递送系统。 RDT的特征还在于其快速崩解时间约为3秒至3分钟。

98. 发明申请

US20050048116A1 Porous drug matrices and methods of manufacture thereof 审中-公开
标题翻译：多孔药物基质及其制造方法
公开(公告)号：US20050048116A1
公开(公告)日：2005-03-03
申请号：US10924642
申请日：2004-08-24
申请人： Julie Straub , David Altreuter , Howard Bernstein , Donald Chickering , Sarwat Khattak , Greg Randall
发明人： Julie Straub , David Altreuter , Howard Bernstein , Donald Chickering , Sarwat Khattak , Greg Randall
IPC分类号： A61K9/16 , A61K9/26 , A61K9/14
CPC分类号： A61K9/1635 , A61K9/1611 , A61K9/1623 , A61K9/1688 , A61K9/1694
摘要： Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid-compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.
摘要翻译：药物，特别是低含水溶性药物以多孔基质形式提供，优选微粒，其增强药物在水性介质中的溶解。药物基质优选使用以下方法制备，所述方法包括（i）将挥发性溶剂中的药物（优选为低溶解度的药物）溶解以形成药物溶液，（ii）将至少一种成孔剂与药物溶液以形成稳定药物并抑制结晶的乳液，悬浮液或第二溶液和亲水或疏水赋形剂，和（iii）从乳液，悬浮液或第二溶液中除去挥发性溶剂和成孔剂以产生多孔基质药物。可以选择疏水性或亲水性赋形剂，以通过抑制晶体生长来稳定药物的结晶形式，或者通过防止结晶来稳定药物的无定形形式。成孔剂可以是与药物溶剂或挥发性固体化合物，优选挥发性盐不混溶的挥发性液体。在优选的实施方案中，使用喷雾干燥来除去溶剂和成孔剂。与药物的无孔基质形式相比，得到的多孔基质在给予患者后具有更快的溶解速率。在优选的实施方案中，多孔药物基质的微粒用水性介质重新配制，并肠胃外给药，或使用标准技术加工成用于口服给药的片剂或胶囊。

99. 发明申请

US20050042289A1 Tablets and methods for modified release of hydrophylic and other active agents 审中-公开
标题翻译：用于修饰释放亲水和其他活性剂的片剂和方法
公开(公告)号：US20050042289A1
公开(公告)日：2005-02-24
申请号：US10835214
申请日：2004-04-28
申请人： James Chu , Yisong Yang , Chunhong Gu , Larry Banda
发明人： James Chu , Yisong Yang , Chunhong Gu , Larry Banda
IPC分类号： A61K20060101 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/26 , A61K9/28
CPC分类号： A61K9/205 , A61K9/2031 , A61K9/204
摘要： A novel tablet and methods for making the tablet are provided. The tablet comprises at least one particle containing a pharmaceutically active agent and a gel-forming material comprising a first polymer, a second polymer, and a gelation facilitator agent, and has a sustained release profile for the active agent.
摘要翻译：提供了一种新颖的片剂和制备片剂的方法。片剂包含至少一种含有药物活性剂的颗粒和包含第一聚合物，第二聚合物和凝胶促进剂的凝胶形成材料，并且具有活性剂的持续释放特性。

100. 发明申请

US20050031668A1 Implantable polymeric device for sustained release of nalmefene 审中-公开
标题翻译：用于持续释放纳美芬的可植入聚合物
公开(公告)号：US20050031668A1
公开(公告)日：2005-02-10
申请号：US10856178
申请日：2004-05-27
申请人： Rajesh Patel , Louis Bucalo , Lauren Costantini
发明人： Rajesh Patel , Louis Bucalo , Lauren Costantini
IPC分类号： A61K9/00 , A61K9/20 , A61K9/26 , A61K9/32 , A61K31/485 , A61P25/32 , A61P25/34
CPC分类号： A61K9/0024 , A61K9/2027 , A61K9/2086 , A61K31/485
摘要： The present invention provides compositions, methods, and kits for administration of nalmefene for treatment of alcoholism, nicotine dependence, or another condition for which treatment with nalmefene is therapeutically beneficial. The invention provides a biocompatible nonerodible polymeric device which releases nalmefene continuously with generally linear release kinetics for extended periods of time. Nalmefene is released through pores that open to the surface of the polymeric matrix in which it is encapsulated. The device may be administered subcutaneously to an individual in need of continuous treatment with nalmefene.
摘要翻译：本发明提供了用于治疗酒精中毒，尼古丁依赖性的纳美芬的组合物，方法和试剂盒，或者其中用纳夫芬处理治疗有益的另一种病症。本发明提供了一种生物相容的非可溶性聚合物装置，其通过长时间的连续释放动力学连续释放纳美芬。纳美芬通过孔被释放，孔通过其被封装在其中的聚合物基质的表面。该装置可以皮下给予需要用纳美芬连续治疗的个体。

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