公开(公告)号：US20070270500A1

公开(公告)日：2007-11-22

申请号：US10578765

申请日：2004-11-05

申请人： Mahendra Dedhiya ,  Shashank Mahashabde ,  Yan Yang ,  Anshu Goel ,  Erhard Seiller ,  Bernhard Hauptmeier

发明人： Mahendra Dedhiya ,  Shashank Mahashabde ,  Yan Yang ,  Anshu Goel ,  Erhard Seiller ,  Bernhard Hauptmeier

IPC分类号： A61K31/136 ,  A61K31/13 ,  A61P25/00

CPC分类号： A61K31/13 ,  A61K9/0063 ,  Y02A50/411

摘要： The invention is directed to formulations of pharmaceutical compounds, such as the Cyclohexylamines and Aminoadamantanes which have antimicrobial properties. In particular, it is directed to aqueous based formulations with reduced amounts of preservatives which allow safe and convenient administration and flexible dosing and which, in the case of oral formulations, are easy to swallow. Optionally, the compositions contain components that provide the requisite stability and shelf life while reducing or avoiding incrustation of the composition around the container closure which leads to leaks and difficulty in opening the container.

摘要翻译： 本发明涉及药物化合物的制剂，例如具有抗微生物性质的环己胺和氨基金刚烷。 特别地，其涉及具有减少量的防腐剂的含水基制剂，其允许安全和方便的施用和柔性给药，并且在口服制剂的情况下，易于吞咽。 任选地，组合物包含提供必要的稳定性和保质期的组分，同时减少或避免组合物围绕容器封闭物的结垢，这导致泄漏和难以打开容器。

公开(公告)号：US20120238631A1

公开(公告)日：2012-09-20

申请号：US13456751

申请日：2012-04-26

申请人： Mahendra G. Dedhiya ,  Shashank Mahashabde ,  Yan Yang ,  Anshu Goel ,  Erhard Seiller ,  Bernhard Hauptmeier

发明人： Mahendra G. Dedhiya ,  Shashank Mahashabde ,  Yan Yang ,  Anshu Goel ,  Erhard Seiller ,  Bernhard Hauptmeier

IPC分类号： A61K31/13 ,  A61P25/00 ,  A61P31/00

CPC分类号： A61K31/13 ,  A61K9/0063 ,  Y02A50/411

摘要： The invention is directed to formulations of pharmaceutical compounds, such as the Cyclohexylamines and Aminoadamantanes which have antimicrobial properties. In particular, it is directed to aqueous based formulations with reduced amounts of preservatives which allow safe and convenient administration and flexible dosing and which, in the case of oral formulations, are easy to swallow. Optionally, the compositions contain components that provide the requisite stability and shelf life while reducing or avoiding incrustation of the composition around the container closure which leads to leaks and difficulty in opening the container.

摘要翻译： 本发明涉及药物化合物的制剂，例如具有抗微生物性质的环己胺和氨基金刚烷。 特别地，其涉及具有减少量的防腐剂的含水基制剂，其允许安全和方便的施用和柔性给药，并且在口服制剂的情况下，易于吞咽。 任选地，组合物包含提供必要的稳定性和保质期的组分，同时减少或避免组合物围绕容器封闭物的结垢，这导致泄漏和难以打开容器。

公开(公告)号：US20100035995A1

公开(公告)日：2010-02-11

申请号：US12587885

申请日：2009-10-14

申请人： Mahendra G. Dedhiya ,  Shashank Mahashabde ,  Yan Yang ,  Anshu Goel ,  Erhard Seiller ,  Bernhard Hauptmeier

发明人： Mahendra G. Dedhiya ,  Shashank Mahashabde ,  Yan Yang ,  Anshu Goel ,  Erhard Seiller ,  Bernhard Hauptmeier

IPC分类号： A61K31/13

CPC分类号： A61K31/13 ,  A61K9/0063 ,  Y02A50/411

摘要： The invention is directed to formulations of pharmaceutical compounds, such as the Cyclohexylamines and Aminoadamantanes which have antimicrobial properties. In particular, it is directed to aqueous based formulations with reduced amounts of preservatives which allow safe and convenient administration and flexible dosing and which, in the case of oral formulations, are easy to swallow. Optionally, the compositions contain components that provide the requisite stability and shelf life while reducing or avoiding incrustation of the composition around the container closure which leads to leaks and difficulty in opening the container.

摘要翻译： 本发明涉及药物化合物的制剂，例如具有抗微生物性质的环己胺和氨基金刚烷。 特别地，其涉及具有减少量的防腐剂的含水基制剂，其允许安全和方便的施用和柔性给药，并且在口服制剂的情况下，易于吞咽。 任选地，组合物包含提供必要的稳定性和保质期的组分，同时减少或避免组合物围绕容器封闭物的结垢，这导致泄漏和难以打开容器。

公开(公告)号：US20060002999A1

公开(公告)日：2006-01-05

申请号：US11155319

申请日：2005-06-16

申请人： Yan Yang ,  Rajiv Janjikhel ,  Niranjan Rao ,  Antonia Periclou ,  Wattanaporn Abramowitz ,  Mahendra Dedhiya ,  Erhard Seiller ,  Bernhard Hauptmeier

发明人： Yan Yang ,  Rajiv Janjikhel ,  Niranjan Rao ,  Antonia Periclou ,  Wattanaporn Abramowitz ,  Mahendra Dedhiya ,  Erhard Seiller ,  Bernhard Hauptmeier

IPC分类号： A61K9/20 ,  A61K31/13

CPC分类号： A61K31/13 ,  A61K9/28 ,  A61K9/2846 ,  A61K9/2866 ,  A61K47/38 ,  Y02A50/411

摘要： The present invention relates to an immediate release solid oral dosage form containing 1-aminocyclohexanes, preferably memantine or neramexane, and optionally a pharmaceutically acceptable coating, wherein the active ingredient exhibits dose proportionality and is released at a dissolution rate of more than about 80% within about the first 60 minutes following entry of said form into a use environment. The dosage form is direct compressed and has a hardness within the range of between about 3 and about 40 Kp, exhibits an average Tmax within the range of about 2 to about 8 hours with an active ingredient load within the range of about 2.5 to about 150 mg. The formulation allows for dose-proportional compositions for once daily or b.i.d. dosing, while maintaining a steady average range of Tmax.

公开(公告)号：US20060198884A1

公开(公告)日：2006-09-07

申请号：US11304976

申请日：2005-12-14

申请人： Yan Yang ,  Rajiv Janjikhel ,  Niranjan Rao ,  Antonia Periclou ,  Wattanaporn Abramowitz ,  Mahendra Dedhiya ,  Erhard Seiller ,  Bernhard Hauptmeier

发明人： Yan Yang ,  Rajiv Janjikhel ,  Niranjan Rao ,  Antonia Periclou ,  Wattanaporn Abramowitz ,  Mahendra Dedhiya ,  Erhard Seiller ,  Bernhard Hauptmeier

IPC分类号： A61K31/13 ,  A61K9/20

CPC分类号： A61K31/13 ,  A61K9/28 ,  A61K9/2846 ,  A61K9/2866 ,  A61K47/38 ,  Y02A50/411

摘要： The present invention relates to an immediate release solid oral dosage form containing 1-aminocyclohexanes, preferably memantine or neramexane, and optionally a pharmaceutically acceptable coating, wherein the active ingredient exhibits dose proportionality and is released at a dissolution rate of more than about 80% within about the first 60 minutes following entry of said form into a use environment. The dosage form is direct compressed and has a hardness within the range of between about 3 and about 40 Kp, exhibits an average Tmax within the range of about 2 to about 8 hours with an active ingredient load within the range of about 2.5 to about 150 mg. The formulation allows for dose-proportional compositions for once daily or b.i.d. dosing, while maintaining a steady average range of Tmax.

摘要翻译： 本发明涉及含有1-氨基环己烷，优选美金刚或奈拉美生和任选的药学上可接受的包衣的立即释放的固体口服剂型，其中活性成分表现出剂量比例，并以大于约80％的溶解速率释放 大约在所述表格进入使用环境后的前60分钟。 该剂型是直接压制的并且具有在约3至约40Kp范围内的硬度，在约2至约8小时的范围内显示平均T max max，活性成分负载在 约2.5至约150mg的范围。 该制剂允许剂量比例组合物每天一次或b.i.d。 同时保持T max的稳定平均范围。

公开(公告)号：US20110236439A1

公开(公告)日：2011-09-29

申请号：US13134467

申请日：2011-06-08

申请人： Yan Yang ,  Rajiv Janjikhel ,  Niranjan Rao ,  Antonia Periclou ,  Wattanaporn Abramowitz ,  Mahendra G. Dedhiya ,  Erhard Seiller ,  Bernhard Hauptmeier

发明人： Yan Yang ,  Rajiv Janjikhel ,  Niranjan Rao ,  Antonia Periclou ,  Wattanaporn Abramowitz ,  Mahendra G. Dedhiya ,  Erhard Seiller ,  Bernhard Hauptmeier

IPC分类号： A61K9/00 ,  A61K31/13 ,  A61K31/205 ,  A61P25/28 ,  A61P25/16 ,  A61P25/04 ,  A61P25/08 ,  A61P27/06 ,  A61P25/24 ,  A61P31/14 ,  A61P33/06 ,  A61P1/16 ,  A61P25/00

CPC分类号： A61K31/13 ,  A61K9/28 ,  A61K9/2846 ,  A61K9/2866 ,  A61K47/38 ,  Y02A50/411

摘要： The present invention relates to an immediate release solid oral dosage form containing 1-aminocyclohexanes, preferably memantine or neramexane, and optionally a pharmaceutically acceptable coating, wherein the active ingredient exhibits dose proportionality and is released at a dissolution rate of more than about 80% within about the first 60 minutes following entry of said form into a use environment. The dosage form is direct compressed and has a hardness within the range of between about 3 and about 40 Kp, exhibits an average Tmax within the range of about 2 to about 8 hours with an active ingredient load within the range of about 2.5 to about 150 mg. The formulation allows for dose-proportional compositions for once daily or b.i.d. dosing, while maintaining a steady average range of Tmax.

摘要翻译： 本发明涉及含有1-氨基环己烷，优选美金刚或奈拉美生和任选的药学上可接受的包衣的立即释放的固体口服剂型，其中活性成分表现出剂量比例，并以大于约80％的溶解速率释放 大约在所述表格进入使用环境后的前60分钟。 剂型是直接压制的并且硬度在约3至约40Kp之间的范围内，平均Tmax在约2至约8小时的范围内，活性成分负载在约2.5至约150的范围内 mg。 该制剂允许剂量比例组合物每天一次或b.i.d。 同时保持Tmax的稳定平均范围。

公开(公告)号：US20100028427A1

公开(公告)日：2010-02-04

申请号：US12410224

申请日：2009-03-24

申请人： Yan Yang ,  Rajiv Janjikhel ,  Niranjan Rao ,  Antonia Periclou ,  Wattanaporn Abramowitz ,  Mahendra G. Dedhiya ,  Erhard Seiller ,  Bernhard Hauptmeier

发明人： Yan Yang ,  Rajiv Janjikhel ,  Niranjan Rao ,  Antonia Periclou ,  Wattanaporn Abramowitz ,  Mahendra G. Dedhiya ,  Erhard Seiller ,  Bernhard Hauptmeier

IPC分类号： A61K9/22 ,  A61K31/13

CPC分类号： A61K31/13 ,  A61K9/28 ,  A61K9/2846 ,  A61K9/2866 ,  A61K47/38 ,  Y02A50/411

摘要： The present invention relates to an immediate release solid oral dosage form containing 1-aminocyclohexanes, preferably memantine or neramexane, and optionally a pharmaceutically acceptable coating, wherein the active ingredient exhibits dose proportionality and is released at a dissolution rate of more than about 80% within about the first 60 minutes following entry of said form into a use environment. The dosage form is direct compressed and has a hardness within the range of between about 3 and about 40 Kp, exhibits an average Tmax within the range of about 2 to about 8 hours with an active ingredient load within the range of about 2.5 to about 150 mg. The formulation allows for dose-proportional compositions for once daily or b.i.d. dosing, while maintaining a steady average range of Tmax.

摘要翻译： 本发明涉及含有1-氨基环己烷，优选美金刚或奈拉美生和任选的药学上可接受的包衣的立即释放的固体口服剂型，其中活性成分表现出剂量比例，并以大于约80％的溶解速率释放 大约在所述表格进入使用环境后的前60分钟。 剂型是直接压制的并且硬度在约3至约40Kp之间的范围内，平均Tmax在约2至约8小时的范围内，活性成分负载在约2.5至约150的范围内 mg。 该制剂允许剂量比例组合物每天一次或b.i.d。 同时保持Tmax的稳定平均范围。

公开(公告)号：US08834924B2

公开(公告)日：2014-09-16

申请号：US13134467

申请日：2011-06-08

申请人： Yan Yang ,  Rajiv Janjikhel ,  Niranjan Rao ,  Antonia Periclou ,  Wattanaporn Abramowitz ,  Mahendra G. Dedhiya ,  Erhard Seiller ,  Bernhard Hauptmeier

发明人： Yan Yang ,  Rajiv Janjikhel ,  Niranjan Rao ,  Antonia Periclou ,  Wattanaporn Abramowitz ,  Mahendra G. Dedhiya ,  Erhard Seiller ,  Bernhard Hauptmeier

IPC分类号： A61K9/20 ,  A61K9/28 ,  A61K31/13

CPC分类号： A61K31/13 ,  A61K9/28 ,  A61K9/2846 ,  A61K9/2866 ,  A61K47/38 ,  Y02A50/411

摘要： The present invention relates to an immediate release solid oral dosage form containing 1-aminocyclohexanes, preferably memantine or neramexane, and optionally a pharmaceutically acceptable coating, wherein the active ingredient exhibits dose proportionality and is released at a dissolution rate of more than about 80% within about the first 60 minutes following entry of said form into a use environment. The dosage form is direct compressed and has a hardness within the range of between about 3 and about 40 Kp, exhibits an average Tmax within the range of about 2 to about 8 hours with an active ingredient load within the range of about 2.5 to about 150 mg. The formulation allows for dose-proportional compositions for once daily or b.i.d. dosing, while maintaining a steady average range of Tmax.

摘要翻译： 本发明涉及含有1-氨基环己烷，优选美金刚或奈拉美生和任选的药学上可接受的包衣的立即释放的固体口服剂型，其中活性成分表现出剂量比例，并以大于约80％的溶解速率释放 大约在所述表格进入使用环境后的前60分钟。 剂型是直接压制的并且硬度在约3至约40Kp之间的范围内，平均Tmax在约2至约8小时的范围内，活性成分负载在约2.5至约150的范围内 mg。 该制剂允许剂量比例组合物每天一次或b.i.d。 同时保持Tmax的稳定平均范围。

公开(公告)号：US5288501A

公开(公告)日：1994-02-22

申请号：US905036

申请日：1992-06-26

申请人： Eberhard Nurnberg ,  Erhard Seiller ,  Bernd Kuhn

发明人： Eberhard Nurnberg ,  Erhard Seiller ,  Bernd Kuhn

IPC分类号： A61J3/06 ,  A61K9/14 ,  A61K9/20 ,  A61K9/32 ,  A61K9/36 ,  A61K9/50

CPC分类号： A61K9/2095 ,  A61K9/5026 ,  A61K9/5042 ,  A61K9/5078

摘要： The application discloses a process for the manufacture of mechanically-stable, readily-disintegratable tablets made of small preformed, preferably rounded, particles or pellets containing a high percentage of active ingredient in which--prior to compression--the particles are coated with an aqueous or aqueous/organic suspension containing water-soluble polyvinyl alcohol having an ester content of 19.4 to 6.7%, a disintegrant, and finely-divided cellulose, the remainder being excipients such as additional colloids, adjuvants, dyes, and/or flavors and the suspending liquid, and dried, the stable but readily-friable tablet product thus-produced, and a method of delivering an active ingredient by the employment of such a tablet for oral ingestion.

摘要翻译： 本申请公开了一种用于制造机械稳定的，易于崩解的片剂的方法，其由预先形成的，优选圆形的颗粒或丸粒制成，其含有高百分比的活性成分，其中 - 在压缩之前，将颗粒用水或 含有酯含量为19.4至6.7％的水溶性聚乙烯醇的水/有机悬浮液，崩解剂和细碎纤维素，其余为赋形剂，例如附加胶体，助剂，染料和/或香料，以及悬浮液 并干燥，如此生产的稳定但易碎的片剂，以及通过使用这种用于口服摄取的片剂递送活性成分的方法。

公开(公告)号：US08877814B2

公开(公告)日：2014-11-04

申请号：US12733645

申请日：2008-09-10

申请人： Barbara Ellers-Lenz ,  Tanja Rosenberg ,  Erhard Seiller ,  Hagen Kruger ,  Michael Althaus

发明人： Barbara Ellers-Lenz ,  Tanja Rosenberg ,  Erhard Seiller ,  Hagen Kruger ,  Michael Althaus

IPC分类号： A61K31/13 ,  A61P27/16 ,  C07C211/35 ,  A61K9/20

CPC分类号： A61K31/13 ,  A61K9/2054 ,  A61K45/06

摘要： The present invention relates to a titration scheme for the administration of a 1-amino-alkylcyclohexane derivative which allows for quick attainment of an effective dose of a 1-amino-alkylcyclohexane derivative while minimizing side effects. The present invention further relates to a titration package for providing a 1-amino-alkylcyclohexane derivative (e.g., neramexane or a pharmaceutically acceptable salt thereof) in at least two different dosages. The present titration scheme/titration package may be useful in the treatment of various diseases, including tinnitus.

摘要翻译： 本发明涉及一种用于施用1-氨基 - 烷基环己烷衍生物的滴定方案，其允许快速获得有效剂量的1-氨基 - 烷基环己烷衍生物，同时尽量减少副作用。 本发明还涉及用于以至少两种不同剂量提供1-氨基 - 烷基环己烷衍生物（例如奈拉美生或其药学上可接受的盐）的滴定包装。 本滴定方案/滴定包可用于治疗各种疾病，包括耳鸣。