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1. 发明申请

US20090012150A1 Stablized Pharmaceutical Composition Comprising an Amorphous Active Substance 审中-公开
标题翻译：包含无定形活性物质的稳定药物组合物
公开(公告)号：US20090012150A1
公开(公告)日：2009-01-08
申请号：US11923059
申请日：2007-10-24
申请人： Rok Grahek , Andrej Bastarda , Mateja Salobir
发明人： Rok Grahek , Andrej Bastarda , Mateja Salobir
IPC分类号： A61K31/40
CPC分类号： A61K31/40 , A61K9/2013 , A61K9/2018 , A61K9/2054
摘要： The invention relates to the pharmaceutical composition comprising the amorphous active substance which is atorvastatin calcium. The process of stabilization of the pharmaceutical composition comprising the pharmaceutical formulation with amorphous atorvastatin calcium, the process of stabilization of the pharmaceutical formulation comprising amorphous atorvastatin calcium and the process of stabilization of atorvastatin calcium in an amorphous form is described.
摘要翻译：本发明涉及包含阿托伐他汀钙的无定形活性物质的药物组合物。描述了包含药物制剂与无定形阿托伐他汀钙的药物组合物的稳定化过程，包含无定形阿托伐他汀钙的药物制剂的稳定化过程和以无定形形式稳定阿托伐他汀钙的方法。

2. 发明授权

US09149460B2 Coated particles and pharmaceutical dosage forms 有权
标题翻译：涂层颗粒和药物剂型
公开(公告)号：US09149460B2
公开(公告)日：2015-10-06
申请号：US11862470
申请日：2007-09-27
申请人： Vlasta Humar , Mateja Burjak , Rok Grahek , Mateja Salobir , Janez Kerc , Klemen Kocevar
发明人： Vlasta Humar , Mateja Burjak , Rok Grahek , Mateja Salobir , Janez Kerc , Klemen Kocevar
IPC分类号： A61K9/24 , A61K31/225 , A61K31/40 , A61K9/20 , A61K9/28
CPC分类号： A61K9/5047 , A61K9/2009 , A61K9/2018 , A61K9/2054 , A61K9/2866 , A61K31/40
摘要： The present invention relates to coated particles and pharmaceutical dosage forms comprising the active substances sensitive to environmental influences. The coating of the present invention provides stability and protection of the active substance to environmental influences and in particular from oxidation and/or environmental humidity by coating.
摘要翻译：本发明涉及包含对环境影响敏感的活性物质的包衣颗粒和药物剂型。本发明的涂层提供活性物质对于环境影响的稳定性和保护，特别是通过涂覆从氧化和/或环境湿度。

3. 发明申请

US20080138429A1 Coated Particles and Pharmaceutical Dosage Forms 有权
标题翻译：涂层颗粒和药物剂型
公开(公告)号：US20080138429A1
公开(公告)日：2008-06-12
申请号：US11862470
申请日：2007-09-27
申请人： Vlasta HUMAR , Mateja Burjak , Rok Grahek , Mateja Salobir , Janez Kerc , Klemen Kocevar
发明人： Vlasta HUMAR , Mateja Burjak , Rok Grahek , Mateja Salobir , Janez Kerc , Klemen Kocevar
IPC分类号： A61K9/50 , A61K31/401
CPC分类号： A61K9/5047 , A61K9/2009 , A61K9/2018 , A61K9/2054 , A61K9/2866 , A61K31/40
摘要： The present invention relates to coated particles and pharmaceutical dosage forms comprising the active substances sensitive to environmental influences. The coating of the present invention provides stability and protection of the active substance to environmental influences and in particular from oxidation and/or environmental humidity by coating.
摘要翻译：本发明涉及包含对环境影响敏感的活性物质的包衣颗粒和药物剂型。本发明的涂层提供活性物质对于环境影响的稳定性和保护，特别是通过涂覆从氧化和/或环境湿度。

4. 发明申请

US20060093680A1 Coated particles and pharmaceutical dosage forms 审中-公开
公开(公告)号：US20060093680A1
公开(公告)日：2006-05-04
申请号：US10544920
申请日：2004-02-11
申请人： Vlasta Humar , Mateja Burjak , Rok Grahek , Mateja Salobir , Janez Kerc , Klemen Kocevar
发明人： Vlasta Humar , Mateja Burjak , Rok Grahek , Mateja Salobir , Janez Kerc , Klemen Kocevar
IPC分类号： A61K31/401 , A61K9/50 , A61K9/16
CPC分类号： A61K9/5047 , A61K9/2009 , A61K9/2018 , A61K9/2054 , A61K9/2866 , A61K31/40
摘要： The present invention relates to coated particles and pharmaceutical dosage forms comprising the active substances sensitive to environmental influences. The coating of the present invention provides stability and protection of the active substance to environmental influences and in particular from oxidation and/or environmental humidity by coating.

5. 发明授权

US06696086B1 Solid pharmaceutical formulation containing lovastatin and simvastatin, respectively, and its preparation 失效
标题翻译：分别含有洛伐他汀和辛伐他汀的固体药物制剂及其制备方法
公开(公告)号：US06696086B1
公开(公告)日：2004-02-24
申请号：US09657853
申请日：2000-09-08
申请人： Zlatko Pflaum , Mateja Salobir , Zdenka Jerala , Aleksander Resman
发明人： Zlatko Pflaum , Mateja Salobir , Zdenka Jerala , Aleksander Resman
IPC分类号： A61K920
CPC分类号： A61K9/1688
摘要： The present invention relates to a novel solid pharmaceutical formulation containing lovastatin and simvastatin, respectively, with a particle size D(0.9) between 15 and 100 &mgr;m and a specific particle surface area between 1 and 4 m2/g, and to the process for its preparation. The present invention also relates to the method for production of lovastatin and simvastatin with the size of crystals which are suitable for the preparation of the pharmaceutical formulation of the present invention. The novel solid pharmaceutical formulation is useful for treating hypercholesterolemia and hyperlipidemia.
摘要翻译：本发明涉及分别含有粒径D（0.9）在15-100μm之间的洛伐他汀和辛伐他汀的新型固体药物制剂，特异性颗粒表面积在1至4m 2 / g之间，而对于其准备过程。本发明还涉及适用于制备本发明的药物制剂的具有晶体尺寸的洛伐他汀和辛伐他汀的生产方法。新型固体药物制剂可用于治疗高胆固醇血症和高脂血症。

6. 发明申请

US20060159741A1 Pharmaceutical compositions comprising amoxicillin and clavulanic acid 审中-公开
标题翻译：包含阿莫西林和克拉维酸的药物组合物
公开(公告)号：US20060159741A1
公开(公告)日：2006-07-20
申请号：US10536543
申请日：2003-11-25
申请人： Janez Kerc , Mateja Salobir
发明人： Janez Kerc , Mateja Salobir
IPC分类号： A61K9/48 , A61K9/26 , B27N3/02
CPC分类号： A61K31/424 , A61K9/1635 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K31/43 , A61K2300/00
摘要： The present invention relates to the formed particles comprising amoxicillin and clavulanic acid, the particles being obtained wet granulation. The invention also relates to the procedure for the preparation of these particles and to the pharmaceutical compositions comprising them.
摘要翻译：本发明涉及形成的包含阿莫西林和克拉维酸的颗粒，该颗粒获得湿法制粒。本发明还涉及制备这些颗粒的方法以及包含它们的药物组合物。

7. 发明授权

US07030151B2 Atorvastatin calcium in a pharmaceutical form composition thereof and pharmaceutical formulation comprising atorvastatin calcium 有权
标题翻译：阿托伐他汀钙，其药物形式组合物和包含阿托伐他汀钙的药物制剂
公开(公告)号：US07030151B2
公开(公告)日：2006-04-18
申请号：US10471906
申请日：2002-03-13
申请人： Janez Ker{hacek over (c)} , Mateja Salobir , Sa{hacek over (s)}a Bavec
发明人： Janez Ker{hacek over (c)} , Mateja Salobir , Sa{hacek over (s)}a Bavec
IPC分类号： A61K209/04 , C07D31/4035
CPC分类号： A61K9/1611 , A61K9/1617 , A61K9/1652 , A61K9/2077 , A61K31/40 , A61K47/02 , A61K47/18
摘要： Atorvastatin calcium, the substance known by the chemical name (R—(R*,R*))-2-(4-fluorophenyl)-β, δ-dihydroxy-5-(1-methylethyl)-3-phenyl-((phenylamino)carbonyl)-1H-pyrrole-1-heptanoic acid hemi calcium salt is known as HMG-CoA reductase inhibitor and is used as an antihypercholesterolemic agent. Atorvastatin in the pharmaceutical compositions available in the market, is usually prepared as its calcium salt since it enables atorvastatin to be conveniently formulated in the pharmaceutical formulations, for example, in tablets, capsules, powders and the like for oral administration. Atorvastatin calcium can exist in an amorphous form or in one of the at least four known crystalline forms (Form I, Form II, Form III and Form IV). Atorvastatin calcium is the substance which is sparingly soluble in water, with pKa 4,5, and it has been found that the crystalline forms are less soluble than the amorphous form, which may cause problems in bioavailability of atorvastatin in the body. The present invention solves the problem of providing therapeutic equivalence of atorvastatin pharmaceutical formulation regardless the form (crystalline, amorphous, mixture of both) of atorvastatin calcium used for its preparation.
摘要翻译：阿托伐他汀钙，化学名称（R-（R *，R *））-2-（4-氟苯基） - ，δ-二羟基-5-（1-甲基乙基）-3-苯基 - （（苯基氨基）羰基）-1H-吡咯-1-庚酸半钙盐被称为HMG-CoA还原酶抑制剂，并用作抗高胆固醇血药剂。市售的药物组合物中的阿托伐他汀通常制备为其钙盐，因为其可使阿托伐他汀方便地配制在药物制剂中，例如用于口服给药的片剂，胶囊，粉末等。阿托伐他汀钙可以以无定形形式或至少四种已知结晶形式之一（形式I，形式II，形式III和形式IV）存在。阿托伐他汀钙是微溶于水的物质，其中pKa为4,5，并且已经发现结晶形式比无定形形式更易溶解，这可能导致阿托伐他汀在体内的生物利用度问题。本发明解决了提供阿托伐他汀药物制剂的治疗等效性的问题，而不管用于其制备的阿托伐他汀钙的形式（两者的结晶，无定形，混合物）。

8. 发明授权

US06984399B2 Solid pharmaceutical formulation containing lovastatin and simvastatin respectively, and its preparation 失效
标题翻译：分别含有洛伐他汀和辛伐他汀的固体药物制剂及其制备方法
公开(公告)号：US06984399B2
公开(公告)日：2006-01-10
申请号：US10742367
申请日：2003-12-19
申请人： Zlatko Pflaum , Mateja Salobir , Zdenka Jerala , Aleksander Resman
发明人： Zlatko Pflaum , Mateja Salobir , Zdenka Jerala , Aleksander Resman
IPC分类号： A61K9/28 , A61K9/20 , A61K9/48 , A61K9/14
CPC分类号： A61K9/1688
摘要： The present invention relates to a novel solid pharmaceutical formulation containing lovastatin and simvastatin, respectively, with a particle size D(0.9) between 15 and 100 μm and a specific particle surface area between 1 and 4 m2/g, and to the process for its preparation. The present invention also relates to the method for production of lovastatin and simvastatin with the size of crystals which are suitable for the preparation of the pharmaceutical formulation of the present invention. The novel solid pharmaceutical formulation is useful for treating hypercholesterolemia and hyperlipidemia.
摘要翻译：本发明涉及一种含有分别具有15至100μm的粒径D（0.9）和1至4μm2的特定颗粒表面积的洛伐他汀和辛伐他汀的新型固体药物制剂， g，以及其准备过程。本发明还涉及适用于制备本发明的药物制剂的具有晶体尺寸的洛伐他汀和辛伐他汀的生产方法。新型固体药物制剂可用于治疗高胆固醇血症和高脂血症。

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