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21. 发明授权

US08663683B2 Sustained-release formulations of topiramate 有权
公开(公告)号：US08663683B2
公开(公告)日：2014-03-04
申请号：US13595103
申请日：2012-08-27
申请人： Likan Liang , Hua Wang , Padmanabh P. Bhatt , Michael L. Vieira
发明人： Likan Liang , Hua Wang , Padmanabh P. Bhatt , Michael L. Vieira
IPC分类号： A61K31/35 , A61K9/24 , A61K9/54 , A61P3/10 , A61P25/02 , A61P25/06
CPC分类号： A61K9/5042 , A61K9/1652 , A61K9/1676 , A61K9/209 , A61K9/5047 , A61K9/5078 , A61K9/5084 , A61K31/357 , A61K31/7048 , A61K45/06 , A61K47/48969 , A61K47/6951 , B82Y5/00 , Y02A50/465
摘要： Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.

22. 发明授权

US08598191B2 Controlled release compositions of gamma-hydroxybutyrate 有权
标题翻译： γ-羟基丁酸酯的控制释放组合物
公开(公告)号：US08598191B2
公开(公告)日：2013-12-03
申请号：US13476369
申请日：2012-05-21
申请人： Likan Liang , Niraj Shah , Padmanabh P. Bhatt , Scott Ibrahim
发明人： Likan Liang , Niraj Shah , Padmanabh P. Bhatt , Scott Ibrahim
IPC分类号： A61K9/20 , A61K9/24 , A61K9/28
CPC分类号： A61K9/5031 , A61K9/1635 , A61K9/1652 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5073 , A61K9/5084 , A61K31/19
摘要： The present invention is directed to oral pulse-release pharmaceutical dosage form containing an immediate release component of gamma-hydroxybutyric acid, and one or more delayed/controlled release components of gamma-hydroxybutyric acid.
摘要翻译：本发明涉及含有γ-羟基丁酸的即时释放组分和γ-羟基丁酸的一种或多种延迟/控制释放组分的口服脉冲释放药物剂型。

23. 发明授权

US08535650B2 Stabilized reverse micelle compositions and uses thereof 有权
标题翻译：稳定的反胶束组合物及其用途
公开(公告)号：US08535650B2
公开(公告)日：2013-09-17
申请号：US10497775
申请日：2002-12-03
申请人： Panayiotis P. Constantinides , Likan Liang , Eun-Hyun Jang
发明人： Panayiotis P. Constantinides , Likan Liang , Eun-Hyun Jang
IPC分类号： A61K9/107 , A61K31/727
CPC分类号： A61K31/727 , A61K8/0291 , A61K9/107 , A61K9/1075 , A61K9/4891 , A61K38/09 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61Q19/00
摘要： The invention relates to compositions and methods for drug delivery suitable for promoting the transmucosal absorption of drugs, especially drugs with poor intrinsic bioavailability, such as peptides, proteins, vaccines, and nucleic acids. The delivery system of this invention preferably comprises fatty acid esters and their hydrophilic derivatives that associate with water and other polar solvents to form reverse micelles that are physically stabilized in the presence of gastrointestinal fluid, water, and other hydrophilic solvents. Such stable reverse micelles are formed by suitable mixtures of polymeric or non-polymeric compounds with amphiphiles. Micelles made using these methods undergo phase transformation more slowly resulting in delayed drug release profiles and sustained absorption. When administered as a pharmaceutical to mucosal surfaces following oral ingestion or intranasal administration, therapeutic molecules principally solubilized in the aqueous phase are protected from digestion by mucosal enzymes and other mucosal degradative processes and are taken up by absorptive cell mechanisms and reach appropriate body compartments. The reverse micelle compositions may comprise mono-, di-glycerides and/or their transesterified products containing C6-C12 fatty acids chains, wherein the transester groups consist of hydrophilic moieties.
摘要翻译：本发明涉及用于药物递送的组合物和方法，其适用于促进药物，特别是具有差的内在生物利用度的药物（例如肽，蛋白质，疫苗和核酸）的经粘膜吸收。本发明的递送系统优选包括与水和其它极性溶剂缔合的脂肪酸酯及其亲水性衍生物，以形成在胃肠液，水和其它亲水溶剂存在下物理稳定的反胶束。这种稳定的反胶束由聚合物或非聚合物与两亲物的合适混合物形成。使用这些方法制备的胶束进行相变更慢，导致延迟的药物释放曲线和持续吸收。当口服摄取或鼻内给药后作为药物施用于粘膜表面时，主要溶解在水相中的治疗分子被保护不被粘膜酶和其它粘膜降解过程消化，并被吸收细胞机制吸收并达到适当的身体隔室。反胶束组合物可以包含含有C 6 -C 12脂肪酸链的单 - ，二 - 甘油酯和/或其酯交换产物，其中所述酯基组由亲水部分组成。

24. 发明申请

US20120231085A1 CONTROLLED RELEASE COMPOSITIONS OF GAMMA-HYDROXYBUTYRATE 有权
标题翻译：游离羟基丁酸的控制释放组合物
公开(公告)号：US20120231085A1
公开(公告)日：2012-09-13
申请号：US13476369
申请日：2012-05-21
申请人： Likan Liang , Niraj Shah , Padmanabh P. Bhatt , Scott Ibrahim
发明人： Likan Liang , Niraj Shah , Padmanabh P. Bhatt , Scott Ibrahim
IPC分类号： A61K31/19 , A61P25/00 , A61P25/18 , A61P25/30 , A61P25/16 , A61P9/12 , A61P9/10 , A61P7/00 , A61P35/00 , A61P23/00 , A61P5/06 , A61P15/00 , A61P3/04 , A61P21/02 , A61P21/06 , A61K9/14
CPC分类号： A61K9/5031 , A61K9/1635 , A61K9/1652 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5073 , A61K9/5084 , A61K31/19
摘要： The present invention is directed to oral pulse-release pharmaceutical dosage form containing an immediate release component of gamma-hydroxybutyric acid, and one or more delayed/controlled release components of gamma-hydroxybutyric acid.
摘要翻译：本发明涉及含有γ-羟基丁酸的即时释放组分和γ-羟基丁酸的一种或多种延迟/控制释放组分的口服脉冲释放药物剂型。

25. 发明授权

US08193211B2 Controlled release compositions of gamma-hydroxybutyrate 有权
标题翻译： γ-羟基丁酸酯的控制释放组合物
公开(公告)号：US08193211B2
公开(公告)日：2012-06-05
申请号：US11239638
申请日：2005-09-30
申请人： Likan Liang , Niraj Shah , Padmanabh P. Bhatt , Scott Ibrahim
发明人： Likan Liang , Niraj Shah , Padmanabh P. Bhatt , Scott Ibrahim
IPC分类号： A61K31/44 , A61K47/00
CPC分类号： A61K9/5031 , A61K9/1635 , A61K9/1652 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5073 , A61K9/5084 , A61K31/19
摘要： The present invention is directed to oral pulse-release pharmaceutical dosage form containing an immediate release component of gamma-hydroxybutyric acid, and one or more delayed/controlled release components of gamma-hydroxybutyric acid.
摘要翻译：本发明涉及含有γ-羟基丁酸的即时释放组分和γ-羟基丁酸的一种或多种延迟/控制释放组分的口服脉冲释放药物剂型。

26. 发明申请

US20110287099A1 Sustained-release formulations of topiramate 有权
标题翻译：托吡酯的缓释制剂
公开(公告)号：US20110287099A1
公开(公告)日：2011-11-24
申请号：US12926931
申请日：2010-12-17
申请人： Likan Liang , Hua Wang , Padmanabh P. Bhatt , Michael L. Vieira
发明人： Likan Liang , Hua Wang , Padmanabh P. Bhatt , Michael L. Vieira
IPC分类号： A61K9/22 , A61K9/14 , A61P25/00 , A61K31/357
CPC分类号： A61K9/5042 , A61K9/1652 , A61K9/1676 , A61K9/209 , A61K9/5047 , A61K9/5078 , A61K9/5084 , A61K31/357 , A61K31/7048 , A61K45/06 , A61K47/48969 , A61K47/6951 , B82Y5/00 , Y02A50/465
摘要： Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.
摘要翻译：提供了托吡酯每日一次口服给药的药物组合物。制剂包含缓释组分和任选的快速释放组分，其组合物可分别选择性地调节以沿预定释放曲线释放活性成分。还提供了治疗或预防哺乳动物受试者中包括施用本文公开的新型制剂的病理学障碍的方法。

27. 发明申请

US20110251198A1 METHODS FOR PRODUCING VILOXAZINE SALTS AND NOVEL POLYMORPHS THEREOF 有权
标题翻译：生产维生素SALTS及其新型聚合物的方法
公开(公告)号：US20110251198A1
公开(公告)日：2011-10-13
申请号：US13084612
申请日：2011-04-12
申请人： Likan Liang , Padmanabh P. Bhatt , David Dain , Jean-Philippe Taquet , Aleksandr Pechenov , Alexei Tchesnokov , Reynold Mariaux
发明人： Likan Liang , Padmanabh P. Bhatt , David Dain , Jean-Philippe Taquet , Aleksandr Pechenov , Alexei Tchesnokov , Reynold Mariaux
IPC分类号： A61K31/535 , C07C215/20 , A61P25/00 , A61P25/24 , A61P25/32 , C07D265/30 , C07D265/32
CPC分类号： C07D265/30 , C07C215/08 , C07C217/34 , C07D265/32
摘要： Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.
摘要翻译：本文提供了维罗他嗪及其各种盐的制备方法，以及与维甲内酯相关的化合物，例如新的中间体反应产物及其多晶型物。特别地，该方法提供基本上纯的维罗他嗪HCl的API，同时避免不期望的杂质。该方法进一步提供了分离，鉴定和表征viloxazine的新型多晶型物。还提供了用于合成和鉴定和描述维罗他嗪的新型中间体的方法，以及一些重要的代谢产物和维罗他嗪代谢物的前体。

28. 发明申请

US20060078618A1 Lipid particles and suspensions and uses thereof 审中-公开
标题翻译：脂质颗粒和悬浮液及其用途
公开(公告)号：US20060078618A1
公开(公告)日：2006-04-13
申请号：US10498572
申请日：2002-12-11
申请人： Panayiotis Constantinides , Reena Patil , Likan Liang
发明人： Panayiotis Constantinides , Reena Patil , Likan Liang
IPC分类号： A61K9/14
CPC分类号： A61K9/1075 , A61K9/0019 , A61K9/127
摘要： The present invention relates to formulations and methods for the mucosal and parenteral administration of lipid particles an suspensions. The formulations of this invention are stable lipid particles useful for oral delivery of water-insoluble therapeutic agents, vaccines and diagnostics. The compositions of this invention promote the mucosal absorption of biologically active molecules across mucosal epithelial barriers. Stabilization of lipid particles is achieved by coating the hydrophobic central core with a polymer shell. The polymer shell can include bioadhesive agents, ligands, and absorption promoting agents. This invention relates to oral drug delivery systems for hydrophobic drugs, and in particular is concerned with improving the bioavailability of hydrophobic drugs from such systems. Using this system, anticancer drugs such as taxanes are orally effective.
摘要翻译：本发明涉及用于粘膜和肠胃外给予脂质颗粒悬浮液的制剂和方法。本发明的制剂是用于口服递送水不溶性治疗剂，疫苗和诊断的稳定的脂质颗粒。本发明的组合物促进生物活性分子穿过粘膜上皮屏障的粘膜吸收。脂质颗粒的稳定通过用聚合物壳涂覆疏水性中心核来实现。聚合物壳可以包括生物粘附剂，配体和吸收促进剂。本发明涉及用于疏水药物的口服药物递送系统，并且特别涉及提高来自这种系统的疏水性药物的生物利用度。使用该系统，抗癌药如紫杉烷是口服有效的。

29. 发明授权

US06511677B1 Polymerizable fatty acids, phospholipids and polymerized liposomes therefrom 失效
公开(公告)号：US06511677B1
公开(公告)日：2003-01-28
申请号：US09714103
申请日：2000-11-17
申请人： Robert N Brey , Likan Liang
发明人： Robert N Brey , Likan Liang
IPC分类号： A61K9127
CPC分类号： C07C69/587 , A61K9/1271 , A61K9/1273 , C11C3/00
摘要： The invention relates to an oral drug delivery system which delivers biologically active substances to the mucosal tissue of the intestine utilizing novel polymerized liposomes. Novel polymerizable fatty acids having a polymerizable group, a surfactant group, and a functional group, and optionally coupled to ligands which target mucosal tissue in the intestine are disclosed. Novel negatively charged polymerizable lipids which have phosphatidyl inositol (PI), phosphatidyl glycerol (PG) or phosphatidyl serine (PS) groups on a polymerizable backbone are also described.

30. 发明授权

US06500453B2 Polymerizable fatty acids, phospholipids and polymerized liposomes therefrom 失效
标题翻译：可聚合的脂肪酸，磷脂和聚合的脂质体
公开(公告)号：US06500453B2
公开(公告)日：2002-12-31
申请号：US10013689
申请日：2001-12-13
申请人： Robert N Brey , Likan Liang
发明人： Robert N Brey , Likan Liang
IPC分类号： A61K9127
CPC分类号： C07C69/587 , A61K9/1271 , A61K9/1273 , C11C3/00
摘要： The invention relates to an oral drug delivery system which delivers biologically active substances to the mucosal tissue of the intestine utilizing novel polymerized liposomes. Novel polymerizable fatty acids having a polymerizable group, a surfactant group, and a functional group, and optionally coupled to ligands which target mucosal tissue in the intestine are disclosed. Novel negatively charged polymerizable lipids which have phosphatidyl inositol (PI), phosphatidyl glycerol (PG) or phosphatidyl serine (PS) groups on a polymerizable backbone are also described.
摘要翻译：本发明涉及使用新型聚合脂质体将生物活性物质输送到肠粘膜组织的口服药物递送系统。公开了具有可聚合基团，表面活性剂组和官能团的新型可聚合脂肪酸，并且任选地与靶向肠内粘膜组织的配体偶联。还描述了在可聚合主链上具有磷脂酰肌醇（PI），磷脂酰甘油（PG）或磷脂酰丝氨酸（PS）基团的新型带负电荷的可聚合脂质。

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