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1. 发明申请

US20120065404A1 Process for Preparing Ethyl (s)-2-Ethoxy-4-[N-[1-(2-Piperidinophenyl)-3-Methyl-1-Butyl]Aminocarbonyl Methyl]Benzoate and Use Thereof for the Preparation of Repaglinide 审中-公开
标题翻译：制备乙基-2-乙氧基-4- [N- [1-（2-哌啶基苯基）-3-甲基-1-丁基]氨基羰基甲基]苯甲酸酯的方法，用于制备瑞格列奈
公开(公告)号：US20120065404A1
公开(公告)日：2012-03-15
申请号：US13301068
申请日：2011-11-21
申请人： Venkata Sasidhar Balla , Madhubabu Alapharthi , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Venkata Sasidhar Balla , Madhubabu Alapharthi , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： C07D295/155
CPC分类号： C07D295/135
摘要： Described herein is an improved, commercially viable and industrially advantageous process for the preparation of Repaglinide intermediate, ethyl (S)-2-ethoxy-4-[N-(1-(2-piperidino-phenyl)-3-methyl-1-butyl)-aminocarbonylmethyl]-benzoate. The process provides the Repaglinide intermediate in higher yield and purity compared to the previously disclosed processes, thereby providing for production of Repaglinide and its pharmaceutically acceptable salts in high purity and in high yield.
摘要翻译：本文描述了一种改进的，商业上可行的和工业上有利的制备瑞格列奈中间体，（S）-2-乙氧基-4- [N-（1-（2-哌啶子基 - 苯基）-3-甲基-1- 丁基） - 氨基羰基甲基] - 苯甲酸酯。与先前公开的方法相比，该方法以更高的产率和纯度提供了瑞格列奈中间体，从而提供了以高纯度和高产率生产瑞格列奈及其药学上可接受的盐。

2. 发明授权

US07955622B2 Controlled-release galantamine formulations 失效
标题翻译：对照释放加兰他敏制剂
公开(公告)号：US07955622B2
公开(公告)日：2011-06-07
申请号：US11870444
申请日：2007-10-11
申请人： Sunil Vandse
发明人： Sunil Vandse
IPC分类号： A61K9/16 , A61K9/00 , A61P25/34
CPC分类号： A61K9/167 , A61K9/209 , A61K9/5073
摘要： Controlled-release galantamine formulations, including controlled-release particles, pellets, granules, and spheres are described. Controlled-release particles, pellets, granules, and spheres with immediate release top-coat are also described. Method of preparing such formulations and method of treating a variety of disorders are also disclosed.
摘要翻译：描述了控制释放加兰他敏制剂，包括控制释放颗粒，颗粒，颗粒和球体。还描述了具有立即释放顶部涂层的控制释放颗粒，颗粒，颗粒和球体。还公开了制备这些制剂的方法和治疗多种疾病的方法。

3. 发明申请

US20080200684A1 Process for Preparing Ethyl (s)-2-Ethoxy-4-[N-[1-(2-Piperidinophenyl)-3-Methyl-1-Butyl]Aminocarbonyl Methyl]Benzoate and Use Thereof for the Preparation of Repaglinide 失效
标题翻译：制备乙基-2-乙氧基-4- [N- [1-（2-哌啶基苯基）-3-甲基-1-丁基]氨基羰基甲基]苯甲酸酯的方法，用于制备瑞格列奈
公开(公告)号：US20080200684A1
公开(公告)日：2008-08-21
申请号：US12031184
申请日：2008-02-14
申请人： Venkata Sasidhar Balla , Madhubabu Alapharthi , Nitin Sharadchandra Pradhan , Jon Valgeirsson
发明人： Venkata Sasidhar Balla , Madhubabu Alapharthi , Nitin Sharadchandra Pradhan , Jon Valgeirsson
IPC分类号： C07D211/32
CPC分类号： C07D295/135
摘要： Described herein is an improved, commercially viable and industrially advantageous process for the preparation of Repaglinide intermediate, ethyl (S)-2-ethoxy-4-[N-(1-(2-piperidino-phenyl)-3-methyl-1-butyl)-aminocarbonylmethyl]-benzoate. The process provides the Repaglinide intermediate in higher yield and purity compared to the previously disclosed processes, thereby providing for production of Repaglinide and its pharmaceutically acceptable salts in high purity and in high yield.
摘要翻译：本文描述了一种改进的，商业上可行的和工业上有利的制备瑞格列奈中间体，（S）-2-乙氧基-4- [N-（1-（2-哌啶子基 - 苯基）-3-甲基-1- 丁基） - 氨基羰基甲基] - 苯甲酸酯。与先前公开的方法相比，该方法以更高的产率和纯度提供了瑞格列奈中间体，从而提供了以高纯度和高产率生产瑞格列奈及其药学上可接受的盐。

4. 发明申请

US20070243252A1 Oral Dosage Formulations and Methods of Preparing the Same 审中-公开
标题翻译：口服制剂及其制备方法
公开(公告)号：US20070243252A1
公开(公告)日：2007-10-18
申请号：US11736048
申请日：2007-04-17
申请人： Grant Wayne Heinicke
发明人： Grant Wayne Heinicke
IPC分类号： A61K9/62
CPC分类号： A61K9/5026 , A61K9/2866 , A61K9/5073 , A61K9/5078 , A61K9/5084 , A61K31/00
摘要： Disclosed herein are methods and compositions suitable for providing zero-order release of active agents. Disclosed herein is a multiparticulate oral dosage form comprising a plurality of pulsed-release pellets, wherein the dosage form releases the active agent at a substantially constant rate following a lag time. The dosage form comprises a combination ensemble of pellets produced by combining 2 to 8 individual ensembles of pulsed-release pellets having a particular T50 and dissolution profile.
摘要翻译：本文公开了适用于提供活性剂零次释放的方法和组合物。本文公开了包含多个脉冲释放丸粒的多颗粒口服剂型，其中剂型在滞后时间之后以基本恒定的速率释放活性剂。剂型包括通过组合具有特定T 50和溶出曲线的2至8个单独的脉冲释放丸粒组合产生的丸粒的组合组合。

5. 发明申请

US20070243250A1 Oral Dosage Formulations and Methods of Preparing the Same 审中-公开
标题翻译：口服制剂及其制备方法
公开(公告)号：US20070243250A1
公开(公告)日：2007-10-18
申请号：US11736113
申请日：2007-04-17
申请人： Grant Wayne Heinicke
发明人： Grant Wayne Heinicke
IPC分类号： A61K9/24
CPC分类号： A61K9/5026 , A61K9/2866 , A61K9/5073 , A61K9/5078 , A61K9/5084 , A61K31/00
摘要： A method of optimizing a dissolution profile for a selected active agent dosage form, comprises combining a first amount of a first ensemble of pulsed-release pellets having a first dissolution profile with a first T50 and a second amount of a second ensemble of pulsed-release pellets having a second dissolution profile with a second T50 to produce a combination ensemble of pellets having a combination dissolution profile of a combination slope, wherein the combination slope corresponds to a single phase release, and wherein the combination slope is greater than 10% lower than the slope of the first dissolution profile and greater than 10% lower than the slope of the second dissolution profile, and wherein the first ensemble of pellets and the second ensemble of pellets comprise a core having disposed thereon a core composition layer, the core composition layer comprising the active agent, and a pulsed-release coating disposed on the core composition layer.
摘要翻译：优化选择的活性剂剂型的溶出曲线的方法包括将具有第一溶出曲线的第一量的第一组脉冲释放颗粒与第一T50和第二量的第二组脉冲释放具有第二溶解曲线的颗粒具有第二T50以产生具有组合斜率的组合溶出曲线的颗粒的组合组合，其中组合斜率对应于单相释放，并且其中组合斜率大于所述第一溶出曲线的斜率比所述第二溶解曲线的斜率低大10％，并且其中所述第一团粒和所述第二团粒组合包括其上设置有芯组合物层的芯，所述芯组合物层包括活性剂和设置在芯组合物层上的脉冲释放涂层。

6. 发明申请

US20070243245A1 Oral Dosage Formulations, Methods of Preparing the Same, and Methods of Reducing Food Effects on Drug Release 审中-公开
标题翻译：口服制剂，其制备方法以及减少食物对药物释放的影响的方法
公开(公告)号：US20070243245A1
公开(公告)日：2007-10-18
申请号：US11736081
申请日：2007-04-17
申请人： Grant Wayne Heinicke
发明人： Grant Wayne Heinicke
IPC分类号： A61K9/62
CPC分类号： A61K9/5026 , A61K9/2081 , A61K9/5078
摘要： A multi-particulate oral dosage form, comprising a plurality of pellets, the pellets comprising a core having disposed thereon a core composition layer, the core composition layer comprising an active agent, and a sustained-release coating disposed on the core composition layer, wherein the sustained-release coating comprises a first polymer comprising a copolymer of acrylic and methacrylic esters comprising quaternary ammonium groups and having a ratio of quaternary ammonium groups to neutral meth(acrylic) esters of 1:40 and optionally a second polymer comprising a copolymer of acrylic and methacrylic esters comprising quaternary ammonium groups and having a ratio of quaternary ammonium groups to neutral meth(acrylic) esters of 1:20, wherein the ratio of the first polymer to the second polymer is about 50:50 to about 100:0, and wherein the first and second polymer comprise about 20 wt % to about 90 wt % of the total weight of the sustained-release coating; and about 10 wt % to about 50 wt % of colloidal silicon dioxide, based on the total weight of the alcohol-soluble material in the sustained-release coating. Methods of making the dosage form and methods of reducing food effects by administering the dosage form to a human subject are also disclosed.
摘要翻译：一种多颗粒口服剂型，包括多个丸粒，所述丸粒包含其上设置有核心组合物层的核心，所述核心组合物层包含活性剂，以及设置在所述核心组合物层上的缓释涂层，其中缓释涂层包括第一聚合物，其包含丙烯酸和甲基丙烯酸酯的共聚物，其包含季铵基团并且具有1:40的中性甲基（丙烯酸）酯的季铵基团的比例和任选地包含丙烯酸共聚物的第二聚合物和含有季铵基并且季铵基与中性甲基（丙烯酸）酯的比例为1:20的甲基丙烯酸酯，其中第一聚合物与第二聚合物的比例为约50:50至约100:0，和其中所述第一和第二聚合物占所述缓释涂层总重量的约20重量％至约90重量％; 和约10重量％至约50重量％的胶体二氧化硅，基于持续释放涂层中的醇可溶材料的总重量。还公开了通过将剂型给予受试者来制备剂型和降低食物效果的方法。

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