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1. 发明授权

EP0656776B1 MULTILAYER CONTROLLED RELEASE TABLETS CONTAINING BOTH NAPROXEN AND NAPROXEN SODIUM SALT 失效
标题翻译：多层片剂具有受控现役同时含有萘普生和萘普生钠SALT
公开(公告)号：EP0656776B1
公开(公告)日：1996-03-20
申请号：EP92923137.1
申请日：1992-11-02
申请人： G.D. Searle & Co.
发明人： DESAI, Subhash
IPC分类号： A61K31/19 , A61K9/20
CPC分类号： A61K9/209 , A61K9/2077 , A61K31/19 , A61K31/192
摘要： The present invention relates to controlled release dosage forms composed of a naproxen layer which contains a delayed release granulate of naproxen compressed with an immediate release granulate of naproxen and an immediate release naproxen sodium layer compressed with the naproxen layer, designed to promptly exert a therapeutic effect while also maintaining the therapeutic blood concentration for a prolonged duration of 24 hours.

2. 发明授权

EP0744947B1 MODIFIED-RELEASE METRONIDAZOLE COMPOSITIONS AND METHODS FOR MAKING AND USING SAME 失效
标题翻译：随着对生产和使用释放和方法METRONIDAZOLPRÄPARATE
公开(公告)号：EP0744947B1
公开(公告)日：2002-04-17
申请号：EP95907963.3
申请日：1995-01-04
申请人： G.D. SEARLE & CO.
发明人： DESAI, Subhash , MANCINI, Alan Mark , SCHUMANN, Steven Charles
IPC分类号： A61K31/415 , A61K9/20
CPC分类号： A61K9/2027 , A61K9/2077 , A61K31/415 , A61K31/4164
摘要： Pharmaceutical compositions having a modified release profile for once daily dosing of metronidazole, methods for making the pharmaceutical compositions, and methods for treating a microbial infection with once daily dosing of the pharmaceutical compositions of the invention are provided. The compositions given once daily exhibit substantial bioequivalence to immediate release metronidazole given three times per day. The compositions of the invention comprise: (a) a first portion of metronidazole which is about 59 wt.% to about 79 wt.% metronidazole; (b) about 1.5 wt.% to about 3.0 wt.% of an aqueous insoluble poly(meth)acrylic acid ester copolymer which is aqueous permeable, aqueous expandable and pH- independent; (c) about 0.1 wt.% to about 2.0 wt.% detackifier; (d) 0 to about 23 wt.% of a first aqueous soluble pharmaceutical diluent; (e) 0 to about 23 wt.% of a second aqueous soluble diluent which is suitable for forming a pharmaceutical tablet when compressed with the granules of (a), the second aqueous soluble diluent being the same as or different from the first aqueous soluble diluent; (f) 0 to about 20 wt.% of a second portion of metronidazole; (g) 0 to about 0.2 wt.% glidant; and (h) 0 to about 2 wt.% lubricant; wherein the composition comprises metronidazole containing granules comprising (a), (b), (c) and (d), wherein the sum of the weight percentages of metronidazole provided by (a) and (f) is between about 72 wt.% and about 79 wt.%, and wherein the sum of the weight percentages of the aqueous soluble diluent provided by (d) and (e) is between about 16 wt.% and about 23 wt.%.

3. 发明公开

EP1165136A1 COMBINATION THERAPY OF ANGIOTENSIN CONVERTING ENZYME INHIBITOR AND EPOXY-STEROIDAL ALDOSTERONE ANTAGONIST FOR TREATMENT OF CARDIOVASCULAR DISEASE 有权
标题翻译：血管紧张素转换酶抑制剂和环氧基的甾体醛固酮拮抗剂用于治疗心血管疾病的治疗的组合疗法
公开(公告)号：EP1165136A1
公开(公告)日：2002-01-02
申请号：EP00912174.0
申请日：2000-03-03
申请人： G.D. SEARLE & CO.
发明人： ALEXANDER, John, C. , RONIKER, Barbara , DESAI, Subhash
IPC分类号： A61K45/06 , A61K38/55 , A61P9/00
CPC分类号： C12Q1/48 , A61K31/585 , A61K38/556 , A61K45/06 , A61K2300/00
摘要： Combinations of an ACE inhibitor and an epoxy-steroidal aldosterone receptor antagonist are described for use in treatment of circulatory disorders. Of particular interest are therapies using epoxy-steroidal-type aldosterone receptor antagonist compounds, such as eplerenone, in combination with an angiotensin converting enzyme inhibitor. This co-therapy would be particularly useful to treat congestive heart failure while avoiding or reducing aldosterone-antagonist-induced side effects such as hyperkalemia.

4. 发明公开

EP0656776A1 MULTILAYER CONTROLLED RELEASE TABLETS CONTAINING BOTH NAPROXEN AND NAPROXEN SODIUM SALT 失效
标题翻译：多层片剂具有受控现役同时含有萘普生和萘普生钠的盐。
公开(公告)号：EP0656776A1
公开(公告)日：1995-06-14
申请号：EP92923137.0
申请日：1992-11-02
申请人： G.D. Searle & Co.
发明人： DESAI, Subhash
IPC分类号： A61K9 , A61K31 , A61P25 , A61P29
CPC分类号： A61K9/209 , A61K9/2077 , A61K31/19 , A61K31/192

5. 发明公开

EP0901372A1 POTASSIUM, SODIUM AND TRIS OXAPROZIN SALT PHARMACEUTICAL FORMULATIONS 失效
标题翻译：含有奥沙普秦钠盐，钾盐，或三药物（羟甲基）氨基甲烷
公开(公告)号：EP0901372A1
公开(公告)日：1999-03-17
申请号：EP97925466.0
申请日：1997-05-14
申请人： G.D. SEARLE & CO.
发明人： ADAMS, Mark, E. , DESAI, Subhash , KARIM, Aziz , PAUL, Kalidas , SCHAAF, Douglas, J. , ZOLD, David, J.
IPC分类号： C07D263 , A61K9 , A61K31 , A61P29
CPC分类号： A61K9/2018 , A61K9/2004 , A61K9/2009 , A61K9/2013 , A61K9/2031 , A61K9/2054 , A61K9/2059 , A61K31/421 , Y10S514/886
摘要： The present invention provides a pharmaceutical formulation for oral administration which is pharmaceutically acceptable, and which produces a desired therapeutic response, in tablet, caplet or other compressed form which comprises the potassium, sodium or Tris salt of oxaprozin, the tablet, caplet or other compressed form of the pharmaceutical formulation generally becoming about 75 % dissolved in phosphate buffer media within about 30 minutes.

6. 发明公开

EP0744947A1 MODIFIED-RELEASE METRONIDAZOLE COMPOSITIONS AND METHODS FOR MAKING AND USING SAME 失效
标题翻译：随着对生产和使用释放和方法METRONIDAZOLPRÄPARATE
公开(公告)号：EP0744947A1
公开(公告)日：1996-12-04
申请号：EP95907963.0
申请日：1995-01-04
申请人： G.D. SEARLE & CO.
发明人： DESAI, Subhash , MANCINI, Alan Mark , SCHUMANN, Steven Charles
IPC分类号： A61K9 , A61K31 , A61K47
CPC分类号： A61K9/2027 , A61K9/2077 , A61K31/415 , A61K31/4164
摘要： Pharmaceutical compositions having a modified release profile for once daily dosing of metronidazole, methods for making the pharmaceutical compositions, and methods for treating a microbial infection with once daily dosing of the pharmaceutical compositions of the invention are provided. The compositions given once daily exhibit substantial bioequivalence to immediate release metronidazole given three times per day. The compositions of the invention comprise: (a) a first portion of metronidazole which is about 59 wt.% to about 79 wt.% metronidazole; (b) about 1.5 wt.% to about 3.0 wt.% of an aqueous insoluble poly(meth)acrylic acid ester copolymer which is aqueous permeable, aqueous expandable and pH- independent; (c) about 0.1 wt.% to about 2.0 wt.% detackifier; (d) 0 to about 23 wt.% of a first aqueous soluble pharmaceutical diluent; (e) 0 to about 23 wt.% of a second aqueous soluble diluent which is suitable for forming a pharmaceutical tablet when compressed with the granules of (a), the second aqueous soluble diluent being the same as or different from the first aqueous soluble diluent; (f) 0 to about 20 wt.% of a second portion of metronidazole; (g) 0 to about 0.2 wt.% glidant; and (h) 0 to about 2 wt.% lubricant; wherein the composition comprises metronidazole containing granules comprising (a), (b), (c) and (d), wherein the sum of the weight percentages of metronidazole provided by (a) and (f) is between about 72 wt.% and about 79 wt.%, and wherein the sum of the weight percentages of the aqueous soluble diluent provided by (d) and (e) is between about 16 wt.% and about 23 wt.%.

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