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公开(公告)号：EP1505072A3
公开(公告)日：2006-06-21
申请号：EP04020121.2
申请日：2000-12-04
发明人： Barton, Kathleen , Borchardt, Thomas B. , Carlos, Marlon, V. , Desai, Subhash , Ferro, Leonard, J. , Gaud, Henry, T. , Ganser, Scott , Little, Clay, R. , Mudipalli, Partha S. , Pietz, Mark, A. , Pilipauskas, Daniel R. , Sing, Yuen-Lung, L. , Stahl, Glenn, L. , Wieczorek, Joseph, J. , Yan, Chris Y.
CPC分类号： C07J71/0015
摘要： A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
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公开(公告)号：EP1580193A2
公开(公告)日：2005-09-28
申请号：EP04030774.6
申请日：2000-12-04
发明人： Barton, Kathleen P. , Gaud, Henry T. , Ganser, Scott , Little, Clay R. , Mudipalli, Partha S. , Borschardt, Thomas B. , Carlos, Marlon V. , Desai, Subhash , Ferro, Leonard J. , Pietz, Mark A. , Sing, Yuen-Lung L. , Stahl, Glenn L. , Wieczorek, Joseph J. , Yan, Chris Y.
CPC分类号： C07J71/0015
摘要： A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.
摘要翻译： 提供醛固酮受体拮抗剂药物依普利酮的新型结晶形式（形式L），其在常规储存和使用温度下具有较高的物理稳定性。 还提供药物组合物，其包含任选伴随有一种或多种其它固体形式的依普利酮的甲基泼尼龙，总单位剂量为约10至约1000mg的依普利酮，并且还包含一种或多种药学上可接受的赋形剂。 提供了用于制备L-赖康孕酮的方法和用于制备包含L型依普利酮形式的组合物。 还提供了用于预防和/或治疗醛固酮介导的病症或病症的方法，其包括向受试者施用治疗有效量的依普利酮，其中至少一部分所述的依普利酮是L-赖康孕酮。
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公开(公告)号：EP1580193A3
公开(公告)日：2010-06-23
申请号：EP04030774.6
申请日：2000-12-04
发明人： Barton, Kathleen P. , Gaud, Henry T. , Ganser, Scott , Little, Clay R. , Mudipalli, Partha S. , Borschardt, Thomas B. , Carlos, Marlon V. , Desai, Subhash , Ferro, Leonard J. , Pietz, Mark A. , Sing, Yuen-Lung L. , Stahl, Glenn L. , Wieczorek, Joseph J. , Yan, Chris Y.
CPC分类号： C07J71/0015
摘要： A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.
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公开(公告)号：EP1527782A1
公开(公告)日：2005-05-04
申请号：EP04030120.2
申请日：2000-12-04
IPC分类号： A61K31/565 , A61K31/57 , A61K9/14 , A61K9/51 , A61K31/585
CPC分类号： A61K9/2018 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/2054 , A61K9/4858 , A61K31/565 , A61K31/57 , A61K31/585
摘要： There is provided a pharmaceutical composition comprising eplerenone in solid particulate form, wherein at least 90% of the eplerenone particles are smaller than about 15 µm, for example about 0.01 to about 1 µm, in diameter. The composition can be adapted for oral administration, for example as a tablet or capsule comprising eplerenone in a unit dosage amount of about 10 to about 1000 mg and one or more excipients.
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