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1. 发明授权

US07550628B2 Process for preparing phenolic acid salts of gabapentin 失效
标题翻译：加巴喷丁酚酸盐的制备方法
公开(公告)号：US07550628B2
公开(公告)日：2009-06-23
申请号：US10806022
申请日：2004-03-22
申请人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
发明人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
IPC分类号： C07C61/08 , A61K31/195
CPC分类号： A61K31/7024 , A61K31/195 , C07C229/28 , C07H13/08
摘要： The present invention provides a novel process for preparation of the tannate salt of gabapentin for human and veterinary pharmaceutical use. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. However, the prior art neither discloses nor suggests the preparation of gabapentin tannate. The process for preparing gabapentin tannate includes the mixing of gabapentin and tannic acid together in the presence of one or more solvents. The method may further include the step of selecting the one or more solvents from a group consisting of purified water, ethanol, glycerin, propylene glycol, diethylether, methylene chloride, acetone, isopropyl alcohol and mixtures thereof. The process may also include the steps of isolating and purifying the tannate salt. This may be accomplished by filtration, drying, centrifugation and lyophilization. The process may utilize either natural or synthetic tannic acid.
摘要翻译：本发明提供了用于人和兽药用途的加巴喷丁的鞣酸盐的制备新方法。活性药物成分的鞣酸盐用于持续释放应用，并改善某些感官特性如味道。然而，现有技术既没有公开也没有提出加巴喷丁丹宁酸盐的制备。加巴喷丁鞣酸盐的制备方法包括在一种或多种溶剂的存在下将加巴喷丁和单宁酸混合在一起。该方法还可以包括从由纯水，乙醇，甘油，丙二醇，二乙醚，二氯甲烷，丙酮，异丙醇及其混合物组成的组中选择一种或多种溶剂的步骤。该方法还可以包括分离和纯化鞣酸盐的步骤。这可以通过过滤，干燥，离心和冻干来完成。该方法可以使用天然或合成的单宁酸。

2. 发明授权

US07094429B2 Process for preparing tannate liquid and semi-solid dosage forms 有权
公开(公告)号：US07094429B2
公开(公告)日：2006-08-22
申请号：US10921438
申请日：2004-08-19
申请人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
发明人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
IPC分类号： A61K9/14 , A01N33/02 , A01N43/40
CPC分类号： A61K31/205 , A61K9/007 , A61K9/2004 , A61K9/4858 , A61K9/4866 , A61K31/7024 , Y10S514/849 , Y10S514/85 , Y10S514/853 , Y10S514/855 , Y10S514/937
摘要： An active ingredient from the group of an antihistamine, a decongestant, an antitussive or anticholinergic is dissolved in a suitable solvent and added to a dispersion of tannic acid in water to form the tannate salt complex of the active ingredient. The active ingredient tannate salt complex without isolation or purification is then added to a liquid or semi-solid medium composed of thickening, suspending, coloring, sweetening and flavoring agents, with stirring. Thereafter, preservatives, pH-adjusting and anti-caking agents in a suitable solvent are mixed with the liquid or semi-solid medium to generate a therapeutic dosage form.

3. 发明授权

US06869618B2 Process for preparing tannate liquid and semi-solid dosage forms 失效
标题翻译：制备鞣酸液体和半固体剂型的方法
公开(公告)号：US06869618B2
公开(公告)日：2005-03-22
申请号：US10119285
申请日：2002-04-09
申请人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
发明人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
IPC分类号： A61K9/00 , A61K9/20 , A61K9/48 , A61K31/205 , A61K31/7024 , A61K9/14 , A01N25/00 , A01N33/02 , A01N43/40
CPC分类号： A61K31/205 , A61K9/007 , A61K9/2004 , A61K9/4858 , A61K9/4866 , A61K31/7024 , Y10S514/849 , Y10S514/85 , Y10S514/853 , Y10S514/855 , Y10S514/937
摘要： An active ingredient from the group of an antihistamine, a decongestant, an antitussive or anticholinergic is dissolved in a suitable solvent and added to a dispersion of tannic acid in water to form the tannate salt complex of the active ingredient. The active ingredient tannate salt complex without isolation or purification is then added to a liquid or semi-solid medium composed of thickening, suspending, coloring, sweetening and flavoring agents, with stirring. Thereafter, preservatives, pH-adjusting and anti-caking agents in a suitable solvent are mixed with the liquid or semi-solid medium to generate a therapeutic dosage form.
摘要翻译：将抗组胺剂，减充血剂，镇咳药或抗胆碱能药物的活性成分溶解在合适的溶剂中，并加入到鞣酸在水中的分散体中以形成活性成分的鞣酸盐复合物。然后将不分离或纯化的活性成分单宁盐复合物在搅拌下加入到由增稠剂，悬浮剂，着色剂，甜味剂和调味剂组成的液体或半固体培养基中。然后，将合适溶剂中的防腐剂，pH调节剂和抗结块剂与液体或半固体培养基混合以产生治疗剂型。

4. 发明授权

US07786168B2 Phenolic acid salts of gabapentin in solid dosage forms and methods of use 失效
标题翻译：加巴喷丁的酚酸盐在固体剂型和使用方法中的用途
公开(公告)号：US07786168B2
公开(公告)日：2010-08-31
申请号：US12138945
申请日：2008-06-13
申请人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
发明人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
IPC分类号： A61K31/196 , C07C61/08
CPC分类号： A61K9/2009 , A61K9/2018 , A61K9/2054 , A61K9/485 , A61K9/4858 , A61K31/195 , A61K31/7024
摘要： The present invention relates to pharmaceutical compositions of gabapentin tannate in solid dosage form, processes for production of those compositions and methods of use of those compositions. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. The process may utilize either natural or synthetic tannic acid.
摘要翻译：本发明涉及固体剂型中的加巴喷丁鞣酸盐的药物组合物，这些组合物的制备方法和这些组合物的使用方法。活性药物成分的鞣酸盐用于持续释放应用，并改善某些感官特性如味道。该方法可以使用天然或合成的单宁酸。

5. 发明授权

US07390922B2 Phenolic acid salts of gabapentin in liquid and/or semi-solid dosage forms and methods of use 失效
标题翻译：加巴喷丁在液体和/或半固体剂型中的酚酸盐和使用方法
公开(公告)号：US07390922B2
公开(公告)日：2008-06-24
申请号：US10806260
申请日：2004-03-22
申请人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
发明人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
IPC分类号： C07C229/28
CPC分类号： C07H5/04 , A61K31/7024
摘要： The present invention relates to pharmaceutical compositions of gabapentin tannate, processes for production of those compositions and methods of use of those compositions. The present invention provides a novel process for preparation of the tannate salt of gabapentin in liquid or semi-solid dosage form for human and veterinary pharmaceutical use. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. The process may utilize either natural or synthetic tannic acid.
摘要翻译：本发明涉及鞣酸加巴喷丁的药物组合物，这些组合物的制备方法和这些组合物的使用方法。本发明提供了用于人和兽用药物用途的液体或半固体剂型中加巴喷丁的鞣酸盐的新方法。活性药物成分的鞣酸盐用于持续释放应用，并改善某些感官特性如味道。该方法可以使用天然或合成的单宁酸。

6. 发明授权

US07273623B2 Process for preparing tannate tablet, capsule or other solid dosage forms 有权
标题翻译：制备鞣酸盐片剂，胶囊或其他固体剂型的方法
公开(公告)号：US07273623B2
公开(公告)日：2007-09-25
申请号：US10269027
申请日：2002-10-10
申请人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
发明人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
IPC分类号： A61K9/14 , A61K9/20 , A61K9/48
CPC分类号： C07H5/06 , A61K9/2004 , A61K9/4858 , A61K9/4866 , A61K31/7024 , A61K45/06 , A61K2300/00
摘要： An active pharmaceutical ingredient is combined with tannic acid to form a tannate salt complex of the active ingredient. The active ingredient tannate salt complex without isolation or purification is then blended with pharmaceutically acceptable excipients to form a granulate which is processed into a tablet or capsule to generate a therapeutic solid dosage form.
摘要翻译：将活性药物成分与丹宁酸混合以形成活性成分的鞣酸盐复合物。然后将分离或纯化的活性成分鞣酸盐复合物与药学上可接受的赋形剂混合以形成颗粒，其被加工成片剂或胶囊以产生治疗性固体剂型。

7. 发明申请

US20030077321A1 Process for preparing tannate tablet, capsule or other solid dosage forms 有权
标题翻译：制备鞣酸盐片剂，胶囊或其他固体剂型的方法
公开(公告)号：US20030077321A1
公开(公告)日：2003-04-24
申请号：US10269027
申请日：2002-10-10
申请人： KIEL LABORATORIES, INC.
发明人： Jeffrey S. Kiel , H. Greg Thomas , Narasimhan Mani
IPC分类号： C07H005/06 , A61K031/7024 , A61K009/48 , A61K009/20
CPC分类号： C07H5/06 , A61K9/2004 , A61K9/4858 , A61K9/4866 , A61K31/7024 , A61K45/06 , A61K2300/00
摘要： An active pharmaceutical ingredient is combined with tannic acid to form a tannate salt complex of the active ingredient. The active ingredient tannate salt complex without isolation or purification is then blended with pharmaceutically acceptable excipients to form a granulate which is processed into a tablet or capsule to generate a therapeutic solid dosage form.
摘要翻译：将活性药物成分与丹宁酸混合以形成活性成分的鞣酸盐复合物。然后将分离或纯化的活性成分鞣酸盐复合物与药学上可接受的赋形剂混合以形成颗粒，其被加工成片剂或胶囊以产生治疗性固体剂型。

8. 发明申请

US20090062191A1 Composition for maintaining gastrointestinal homeostasis 审中-公开
标题翻译：用于维持胃肠道稳态的组合物
公开(公告)号：US20090062191A1
公开(公告)日：2009-03-05
申请号：US11897156
申请日：2007-08-29
申请人： Jeffrey S. Kiel , H. Gregory Thomas , Richard Andrew Todebush
发明人： Jeffrey S. Kiel , H. Gregory Thomas , Richard Andrew Todebush
IPC分类号： A61K31/19 , A61K38/00 , A61P1/12
CPC分类号： A61K31/05 , A61K31/7024 , A61K38/38 , A61K2300/00
摘要： The invention relates to a suspension of albumin and tannic acid for maintaining gastrointestinal homeostasis.
摘要翻译：本发明涉及白蛋白和丹宁酸用于维持胃肠体内平衡的悬浮液。

9. 发明申请

US20080015260A1 Pharmaceutical compositions having improved stability and methods for preparation and use 审中-公开
标题翻译：药物组合物具有改进的稳定性和制备和使用方法
公开(公告)号：US20080015260A1
公开(公告)日：2008-01-17
申请号：US11827363
申请日：2007-07-11
申请人： Jeffrey Kiel , H. Thomas , Richard Todebush , Amy Barish
发明人： Jeffrey Kiel , H. Thomas , Richard Todebush , Amy Barish
IPC分类号： A61K31/133
CPC分类号： A61K31/133 , A61K9/0056 , A61K9/0095 , A61K9/2009 , A61K47/02
摘要： The present invention relates to novel compositions having improved stability during storage over extended periods of time. The compositions of the present invention comprise an active pharmaceutical ingredient combined with a synthetic form of magnesium aluminum silicate. The present invention also relates to novel compositions that comprise active pharmaceutical ingredients as tannate complexes combined with a synthetic form of magnesium aluminum silicate wherein the compositions have an increased weight percent of insoluble active pharmaceutical ingredient. The present invention also relates to a method for preparing the novel compositions.
摘要翻译：本发明涉及在长时间储存期间具有改进的稳定性的新型组合物。本发明的组合物包含与合成形式的硅酸镁铝组合的活性药物成分。本发明还涉及包含与合成形式的硅酸镁铝组合的鞣酸复合物的活性药物成分的新型组合物，其中所述组合物具有增加的不溶性活性药物成分的重量百分数。本发明还涉及一种制备新型组合物的方法。

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