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1. 发明授权

US07834201B2 Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base 有权
标题翻译：依他普仑和包含依他普仑碱的分散片的结晶基
公开(公告)号：US07834201B2
公开(公告)日：2010-11-16
申请号：US11425522
申请日：2006-06-21
申请人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
发明人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
IPC分类号： C07D307/87
CPC分类号： C07D307/81
摘要： The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
摘要翻译：本发明涉及众所周知的抗抑郁药物依他普仑S-1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃甲腈的结晶碱，所述制剂为碱，使用碱，草酸盐的纯化盐的制备方法，通过所述方法获得的盐和含有这些盐的制剂的方法，以及制备纯化的依他普仑游离碱或依他普仑的盐的方法，例如草酸盐，使用氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂。最后，本发明涉及硬度至少为22N，口服崩解时间小于120秒的可分散片剂，其包含吸附在水溶性填料上的活性药物成分，其中活性药物成分的熔点为 40-100℃的范围，以及制造这种可分散片剂的方法。

2. 发明授权

US07723533B2 Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base 有权
标题翻译：依他普仑和包含依他普仑碱的分散片的结晶基
公开(公告)号：US07723533B2
公开(公告)日：2010-05-25
申请号：US12046999
申请日：2008-03-12
申请人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
发明人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
IPC分类号： C07D307/87
CPC分类号： C07D307/81
摘要： The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
摘要翻译：本发明涉及众所周知的抗抑郁药物依他普仑S-1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的结晶碱，其制剂的所述碱的方法，使用碱，通过所述方法获得的盐以及含有这些盐的制剂来制备依他普仑的纯化盐如草酸盐的方法，以及制备纯化的依他普仑游离碱或其盐的方法使用氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂，例如草酸盐。最后，本发明涉及硬度至少为22N，口服崩解时间小于120秒的可分散片剂，其包含吸附在水溶性填料上的活性药物成分，其中活性药物成分的熔点为 40-100℃的范围，以及制造这种可分散片剂的方法。

3. 发明申请

US20080161388A1 CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 有权
标题翻译：包括ESCITALOPRAM基板的晶圆和可折叠片
公开(公告)号：US20080161388A1
公开(公告)日：2008-07-03
申请号：US12046984
申请日：2008-03-12
申请人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
发明人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
IPC分类号： A61K31/343 , C07D307/87
CPC分类号： C07D307/81
摘要： The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
摘要翻译：本发明涉及众所周知的抗抑郁药物依他普仑S-1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的结晶碱，其制剂的所述碱的方法，使用碱，通过所述方法获得的盐以及含有这些盐的制剂来制备依他普仑的纯化盐如草酸盐的方法，以及制备纯化的依他普仑游离碱或其盐的方法使用氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂，例如草酸盐。最后，本发明涉及硬度至少为22N，口服崩解时间小于120秒的可分散片剂，其包含吸附在水溶性填料上的活性药物成分，其中活性药物成分的熔点为 40-100℃的范围，以及制造这种可分散片剂的方法。

4. 发明申请

US20110046218A1 CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 审中-公开
标题翻译：包括ESCITALOPRAM基板的晶圆和可折叠片
公开(公告)号：US20110046218A1
公开(公告)日：2011-02-24
申请号：US12916750
申请日：2010-11-01
申请人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
发明人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
IPC分类号： A61K31/343 , C07D307/87 , A61P25/24
CPC分类号： C07D307/81
摘要： The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
摘要翻译：本发明涉及众所周知的抗抑郁药物依他普仑S-1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃甲腈的结晶碱，所述制剂为碱，使用碱，草酸盐的纯化盐的制备方法，通过所述方法获得的盐和含有这些盐的制剂的方法，以及制备纯化的依他普仑游离碱或依他普仑的盐的方法，例如草酸盐，使用氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂。最后，本发明涉及硬度至少为22N，口服崩解时间小于120秒的可分散片剂，其包含吸附在水溶性填料上的活性药物成分，其中活性药物成分的熔点为 40-100℃的范围，以及制造这种可分散片剂的方法。

5. 发明申请

US20070021499A1 CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 有权
标题翻译：包括ESCITALOPRAM基板的晶圆和可折叠片
公开(公告)号：US20070021499A1
公开(公告)日：2007-01-25
申请号：US11425522
申请日：2006-06-21
申请人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Rock , Helle Eliasen , Ken Liljegren
发明人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Rock , Helle Eliasen , Ken Liljegren
IPC分类号： A61K31/343 , C07D307/02
CPC分类号： C07D307/81
摘要： The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
摘要翻译：本发明涉及众所周知的抗抑郁药物依他普仑S-1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃甲腈的结晶碱，所述制剂为碱，使用碱，草酸盐的纯化盐的制备方法，通过所述方法获得的盐和含有这些盐的制剂的方法，以及制备纯化的依他普仑游离碱或依他普仑的盐的方法，例如草酸盐，使用氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂。最后，本发明涉及硬度至少为22N，口服崩解时间小于120秒的可分散片剂，其包含吸附在水溶性填料上的活性药物成分，其中活性药物成分的熔点为 40-100℃的范围，以及制造这种可分散片剂的方法。

6. 发明授权

US07560576B2 Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base 有权
标题翻译：依他普仑和包含依他普仑碱的分散片的结晶基
公开(公告)号：US07560576B2
公开(公告)日：2009-07-14
申请号：US12046984
申请日：2008-03-12
申请人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
发明人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
IPC分类号： C07D307/00 , A61K31/34
CPC分类号： C07D307/81
摘要： The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
摘要翻译：本发明涉及众所周知的抗抑郁药物依他普仑S-1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的结晶碱，其制剂的所述碱的方法，使用碱，通过所述方法获得的盐以及含有这些盐的制剂来制备依他普仑的纯化盐如草酸盐的方法，以及制备纯化的依他普仑游离碱或其盐的方法使用氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂，例如草酸盐。最后，本发明涉及硬度至少为22N，口服崩解时间小于120秒的可分散片剂，其包含吸附在水溶性填料上的活性药物成分，其中活性药物成分的熔点为 40-100℃的范围，以及制造这种可分散片剂的方法。

7. 发明申请

US20080161584A1 CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 有权
公开(公告)号：US20080161584A1
公开(公告)日：2008-07-03
申请号：US12046999
申请日：2008-03-12
申请人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
发明人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
IPC分类号： C07D307/87
CPC分类号： C07D307/81
摘要： The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.

8. 发明申请

US20060115524A1 Method for preparation of an agglomerate using melt agglomeration 审中-公开
标题翻译：使用熔融聚集制备团块的方法
公开(公告)号：US20060115524A1
公开(公告)日：2006-06-01
申请号：US10543789
申请日：2004-02-18
申请人： Helle Eliasen
发明人： Helle Eliasen
IPC分类号： A61K9/48 , A61K9/20 , B27N3/00
CPC分类号： A61K9/1611 , A61K9/143 , A61K9/1617 , A61K9/1641 , A61K9/1694 , A61K9/2009 , A61K9/2013 , A61K9/2031
摘要： Melt agglomeration for the preparation of an agglomerated material is performed us-ing a vehicle that can be melted at a suitable temperature, an active compound and silicon dioxide as filler. Using silicon dioxide as a filler in melt agglomeration has the benefit that a high ratio of melt to filler may be used. Agglomerates prepared by the process proved to be readily compressible into tablets using common equipment. Melt agglomeration for the preparation of an agglomerated material is performed us-ing a vehicle that can be melted at a suitable temperature, an active compound and silicon dioxide as filler. Using silicon dioxide as a filler in melt agglomeration has the benefit that a high ratio of melt to filler may be used. Agglomerates prepared by the process proved to be readily compressible into tablets using common equipment.
摘要翻译：使用可在合适温度下熔化的载体，活性化合物和二氧化硅作为填料进行用于制备团聚材料的熔融聚集。在熔体团聚中使用二氧化硅作为填料具有可以使用高比例的熔体与填料的益处。通过该方法制备的团块被证明可以使用普通设备容易地压缩成片剂。使用可在合适温度下熔化的载体，活性化合物和二氧化硅作为填料进行用于制备团聚材料的熔融聚集。在熔体团聚中使用二氧化硅作为填料具有可以使用高比例的熔体与填料的益处。通过该方法制备的团块被证明可以使用普通设备容易地压缩成片剂。

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