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1. 发明申请

US20050271721A1 Carvedilol-hydrophilic solutions 审中-公开
标题翻译：卡维地洛亲水溶液
公开(公告)号：US20050271721A1
公开(公告)日：2005-12-08
申请号：US11204614
申请日：2005-08-16
申请人： Rolf-Dieter Gabel , Guenter Neugebauer , Walter Preis , Alexander Wirl
发明人： Rolf-Dieter Gabel , Guenter Neugebauer , Walter Preis , Alexander Wirl
IPC分类号： A61K9/16 , A61K9/14 , A61K9/20 , A61K9/22 , A61K31/403 , A61K47/04 , A61K47/30 , A61K47/34 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12
CPC分类号： A61K9/1635 , A61K9/145 , A61K9/146 , A61K9/2027 , A61K9/205 , A61K9/2054 , A61K31/403
摘要： The present invention is concerned with pharmaceutically acceptable compositions comprising carvedilol or a pharmaceutically acceptable salt thereof distributed as a molecular dispersion in a concentration above 5% (wt./wt.), as well as pharmaceutical administration forms comprising such compositions and their use for the treatment and/or prophylaxis of illnesses such as hypertension, cardiac insufficiency or angina pectoris.
摘要翻译：本发明涉及包含卡维地洛或其药学上可接受的盐的药学上可接受的组合物，其分布为浓度高于5％（重量/重量）的分子分散体，以及包含这些组合物的药物给药形式及其用于治疗和/或预防高血压，心功能不全或心绞痛等疾病。

2. 发明授权

US06852337B2 Carvedilol-galenics 失效
标题翻译：卡维地洛
公开(公告)号：US06852337B2
公开(公告)日：2005-02-08
申请号：US10278191
申请日：2002-10-22
申请人： Rolf-Dieter Gabel , Walter Preis , Alexander Wirl
发明人： Rolf-Dieter Gabel , Walter Preis , Alexander Wirl
IPC分类号： A61K9/14 , A61K9/16 , A61K31/403 , A61K31/454
CPC分类号： A61K31/403 , A61K9/143 , A61K9/1617 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K31/454
摘要： The invention relates to a process for the preparation of fast-dissolving pharmaceutical preparations from difficultly soluble active substances, wherein an aqueous suspension is made from the active substance and one or more water-soluble adjuvants and then the resulting aqueous suspension is processed, with removal of the water, by methods conventional per se, to form solid pharmaceutical preparations. The invention also relates to fast-dissolving pharmaceutical preparations of active substances having a dissolution rate of at least 70% after 30 minutes, prepared in accordance with the process of the invention.
摘要翻译：本发明涉及从难溶性活性物质制备快速溶解药物制剂的方法，其中水性悬浮液由活性物质和一种或多种水溶性佐剂制成，然后将所得水性悬浮液加工，除去的水，通过本身的方法形成固体药物制剂。本发明还涉及根据本发明的方法制备的30分钟后溶解速率至少为70％的活性物质的快速溶解药物制剂。

3. 发明申请

US20060148878A1 Pseudopolymorphic forms of carvedilol 审中-公开
公开(公告)号：US20060148878A1
公开(公告)日：2006-07-06
申请号：US11325754
申请日：2006-01-05
申请人： Andre Bubendorf , Rolf-Dieter Gabel , Michael Hennig , Siegfried Krimmer , Guenter Neugebauer , Walter Preis , Alexander Wirl
发明人： Andre Bubendorf , Rolf-Dieter Gabel , Michael Hennig , Siegfried Krimmer , Guenter Neugebauer , Walter Preis , Alexander Wirl
IPC分类号： A61K31/403 , C07D209/88
CPC分类号： C07D209/88
摘要： The present invention is concerned with pseudopolymorphic forms of 1-(4-carbazolyloxy)-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanole (carvedilol) or of optically active forms or pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them.

4. 发明授权

US06689755B1 Method of stabilizing biologically active substances 有权
标题翻译：稳定生物活性物质的方法
公开(公告)号：US06689755B1
公开(公告)日：2004-02-10
申请号：US09184866
申请日：1998-11-03
申请人： Rolf-Dieter Gabel , Markus Mattern , Gerhard Winter , Alexander Wirl , Heinrich Woog
发明人： Rolf-Dieter Gabel , Markus Mattern , Gerhard Winter , Alexander Wirl , Heinrich Woog
IPC分类号： C08B3000
CPC分类号： A61K9/1617 , A61K9/1623 , A61K47/183 , B01D1/18 , F26B3/02 , Y10S435/81 , Y10S514/911 , Y10S514/97
摘要： The present invention relates to a rapid and readily reproducible process for stabilizing biologically active substances by combining the biologically active substance witha a stabilizingmixture and drying the resulting mixture into a dry, amorphous product by means of convection drying. The invention also relates to the amorphous, microscopically homogeneous products which are obtained by this process, are in the form of powders and have a uniform geometric, in particular spherical, shape. The invention furthermore relates to the use of substance mixtures for stabilizing biologically active material, in particular proteins by means of spray drying.
摘要翻译：本发明涉及通过将生物活性物质与稳定混合物组合并通过对流干燥将所得混合物干燥成干燥的无定形产物来稳定生物活性物质的快速和容易重现的方法。本发明还涉及通过该方法获得的无定形，微观均匀的产品，其为粉末形式并且具有均匀的几何形状，特别是球形的形状。本发明还涉及物质混合物用于通过喷雾干燥来稳定生物活性物质，特别是蛋白质的用途。

5. 发明授权

US06521262B2 Solid instant-release forms of administration and process for producing the same 失效
标题翻译：固体即时释放形式的施用和其制备方法
公开(公告)号：US06521262B2
公开(公告)日：2003-02-18
申请号：US09117170
申请日：1998-07-27
申请人： Rolf-Dieter Gabel , Alexander Wirl , Heinrich Woog
发明人： Rolf-Dieter Gabel , Alexander Wirl , Heinrich Woog
IPC分类号： A61K914
CPC分类号： A61K9/2081 , A61K9/0056
摘要： The present invention concerns solid instant-release forms of administration (IR form of administration) comprising therapeutic active substances or active substance concentrates in particular lipid conjugates of nucleosides which have gel-forming properties in aqueous media as well as processes for their production.
摘要翻译：本发明涉及包含在含水介质中具有凝胶形成性质的核苷的特定脂质缀合物的治疗活性物质或活性物质浓缩物的固体即时释放形式的施用（IR给药形式）及其制备方法。

6. 发明授权

US4828839A Method for making a guar flour chewable dosage unit 失效
标题翻译：制造瓜尔豆粉咀嚼剂量单位的方法
公开(公告)号：US4828839A
公开(公告)日：1989-05-09
申请号：US149901
申请日：1988-01-29
申请人： Berthold Stemmle , Alexander Wirl , Fritz Demmer
发明人： Berthold Stemmle , Alexander Wirl , Fritz Demmer
IPC分类号： A61K9/20 , A61K31/715
CPC分类号： A61K31/715 , A61K9/2004 , A61K9/2009
摘要： The present invention provides a composition containing guar flour in the form of tablets for oral administration, said tablets having been produced by dry pressing guar flour with a particle size of 60 to 500 .mu.m. in admixture with 5 to 30% of highly dispersed silica gel.
摘要翻译：本发明提供一种含有用于口服给药的片剂形式的瓜尔豆粉的组合物，所述片剂是通过干燥粒径为60-500μm的瓜耳粉制成的。与5至30％的高度分散的硅胶混合。

7. 发明授权

US5840330A Process for the preparation of shaped, compressed controlled-release unit-dosage forms, and the compressed unit-dosage forms thus obtained 失效
标题翻译：用于制备成形压缩的控释单元剂型的方法以及由此获得的压缩的单位剂型
公开(公告)号：US5840330A
公开(公告)日：1998-11-24
申请号：US357143
申请日：1994-12-15
申请人： Berthold Stemmle , Klaus Budde , Alexander Wirl , Fritz Demmer
发明人： Berthold Stemmle , Klaus Budde , Alexander Wirl , Fritz Demmer
IPC分类号： A61K9/22 , A61K20060101 , A61K9/20 , A61K31/19 , A61K47/00 , A61P3/06
CPC分类号： A61K9/2095 , A61K9/2077
摘要： Process for the preparation of shaped, compressed controlled-release unit-dosage forms from a therapeutic active substance exhibiting a self-retarding release that depends on the magnitude of the force used for the compression. The process gives unit-dosage forms for which the release of the active substance is highly uniform, reproducibly identical and largely linear. To achieve this, the active substance and an additive charge that inhibits or compensates for the self-retardation of its release are processed into particles in the first stage of production, so that the preliminary compressed objects made from these particles without any further additives exhibit a rapid release (in comparison with the required controlled release) over the range of the force of compression envisaged for the production of the unit-dosage form in question, after which the particles are compressed in the second stage of production with a release-retarding agent to obtain the unit-dosage forms. The invention also relates to the unit-dosage forms thus obtained.
摘要翻译：从治疗活性物质制备成形的，压缩的控制释放单位剂型的方法，其表现出取决于用于压缩的力的大小的自我缓解释放。该方法给出了单位剂型，其中活性物质的释放是高度均匀的，可重复地相同的并且在很大程度上是线性的。为了达到这个目的，在生产的第一阶段，抑制或补偿其释放的自我延迟的活性物质和添加剂被加工成颗粒，使得由这些颗粒制成的预先压制的物体没有任何其它添加剂显示出在生产所述单位剂量形式的压缩力的范围内快速释放（与所需的控制释放相比），然后在第二阶段用释放阻滞剂压缩颗粒以获得单位剂型。本发明还涉及由此获得的单位剂型。

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