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1. 发明授权

US08802145B2 Highly porous, fast-disintegrating solid dosage form and its way of manufacturing comprising the preparation of a powder and a freezedrying step 有权
标题翻译：高度多孔，快速崩解的固体剂型及其制备方法，包括制备粉末和自由干燥步骤
公开(公告)号：US08802145B2
公开(公告)日：2014-08-12
申请号：US11666434
申请日：2005-10-27
申请人： Kurt Heinz Bauer
发明人： Kurt Heinz Bauer
IPC分类号： A61K9/00 , A61K31/60 , A61K31/451 , A61K31/606 , A61K31/192 , A61K31/341 , A61K9/46
CPC分类号： A61K9/0056 , A61K9/0007
摘要： The invention relates to a method of manufacture of fast-disintegrating solid dosage forms, characterized in that one or more structure building components in mixed solid powder form are dosed into cavities of blister packs or moulds, the remaining components dissolved in water dosed and added to the powder to form a moistened, plasticized mass, frozen to below −20° C., and the water sublimed in high vacuum. In this way solid dosage forms are obtained with a similar porous structure as usually result from freeze drying processes, but the process requires much less water, which means considerably less time and less energy.
摘要翻译：本发明涉及一种快速崩解固体剂型的制造方法，其特征在于将一种或多种混合固体粉末形式的结构构造成分加入到泡罩包装或模具的空腔中，其余组分溶解于水中并加入粉末形成湿润的塑化块，冷冻至-20℃以下，水在高真空中升华。以这种方式获得通常由冷冻干燥过程产生的类似的多孔结构的固体剂型，但是该方法需要更少的水，这意味着更少的时间和更少的能量。

2. 发明授权

US06331294B1 Use of copolymers of monoethylenically unsaturated carboxylic acids as solubilizers 有权
标题翻译：使用单烯属不饱和羧酸的共聚物作为增溶剂
公开(公告)号：US06331294B1
公开(公告)日：2001-12-18
申请号：US09268720
申请日：1999-03-17
申请人： Helmut Meffert , Axel Sanner , Gunther Berndl , Folker Ruchatz , Karl Kolter , Kurt Heinz Bauer
发明人： Helmut Meffert , Axel Sanner , Gunther Berndl , Folker Ruchatz , Karl Kolter , Kurt Heinz Bauer
IPC分类号： A61K3174
CPC分类号： A61K8/8158 , A61K8/8152 , A61K9/0014 , A61K9/0019 , A61K9/1075 , A61K9/2027 , A61K9/4866 , A61K47/32 , A61Q13/00 , A61Q17/04 , C08F220/04
摘要： The invention relates to the use of copolymers comprising a) 82 to 99.9 mol % of at least one monoethylenically unsaturated C3-C8-carboxylic acid; b) 0.1 to 18 mol % of at least one monomer selected from the group b1) N—C8-C30-alkyl-substituted amides of monoethylenically unsaturated C3-C8-carboxylic acids, b2) N,N—C8-C30-dialkyl-substituted amides of monoethylenically unsaturated C3-C8-carboxylic acids, b3) C8-C30-alkyl esters of monoethylenically unsaturated C3-C8-carboxylic acids; c) 0 to 17.9 mol % of at least one monomer selected from the group of c1) vinyl esters of aliphatic C8-C30-carboxylic acids, c2) C8-C30-alkylvinyl ethers, mol % data for the individual components adding up to 100%, as solubilizer.
摘要翻译：本发明涉及包含a）82-99.9摩尔％的至少一种单烯属不饱和C 3 -C 8 - 羧酸的共聚物的用途; b）0.1至18摩尔％的至少一种选自b 1）N-C 8 -C 30 烷基取代的单烯属不饱和C3-C8-羧酸的酰胺，b2）单烯属不饱和C3-C8-羧酸的N，N-C8-C30-二烷基取代的酰胺，b3）单烯属不饱和的C 3 -C 30 - 烷基酯 C 3 -C 8 - 羧酸; c）0至17.9mol％的至少一种选自以下的单体：c1）脂肪族C 8 -C 30 - 羧酸的乙烯基酯，c 2）C 8 -C 30烷基乙烯基醚，mol％个别成分加起来可达100％，作为增溶剂。

3. 发明授权

US5739122A Dextran esters, the preparation thereof and the use thereof for coating or embedding drugs 失效
标题翻译：葡聚糖酯，其制备方法及其用于涂覆或包埋药物的用途
公开(公告)号：US5739122A
公开(公告)日：1998-04-14
申请号：US612975
申请日：1996-03-11
申请人： Volker Schehlmann , Kurt Heinz Bauer , Jan-Frederic Kesselhut
发明人： Volker Schehlmann , Kurt Heinz Bauer , Jan-Frederic Kesselhut
IPC分类号： A61K9/20 , A61K9/28 , A61K38/00 , A61K47/36 , C08B37/02 , A61K31/72
CPC分类号： A61K9/286 , A61K9/205 , C08B37/0021 , Y10S514/964
摘要： Dextran esters with a molecular weight of 10,000-10,000,000 and ester side chains which are derived from acids with 6-18 carbon atoms, where the degree of esterification is adjusted, depending on the number of carbon atoms in the side chains and the molecular weight, to a value of 0.04-1.1 so that the dextran esters are insoluble in water at room temperature and are broken down by colonic bacteria, and their use for coating and/or embedding pharmaceutical active ingredients or drug formulations.
摘要翻译： PCT No.PCT / EP94 / 02988 Sec。 371日期：1996年3月11日 102（e）1996年3月11日PCT 1994年9月7日PCT PCT。出版物WO95 / 07936 日期1995年3月23日分子量为10,000-10,000,000的葡聚糖酯和衍生自具有6-18个碳原子的酸的酯侧链，其中调节酯化度取决于侧链中的碳原子数和分子量为0.04-1.1，使得葡聚糖酯在室温下不溶于水，并被结肠细菌分解，以及它们用于涂覆和/或包埋药物活性成分或药物制剂的用途。

4. 发明授权

US4567161A Liquid active ingredient concentrates for preparation of microemulsions 失效
标题翻译：液体活性成分浓缩液用于制备微乳液
公开(公告)号：US4567161A
公开(公告)日：1986-01-28
申请号：US508664
申请日：1983-06-28
申请人： Ulrich Posanski , Miklos Ghyczy , Kurt-Heinz Bauer , Armin Wendel
发明人： Ulrich Posanski , Miklos Ghyczy , Kurt-Heinz Bauer , Armin Wendel
IPC分类号： A01N25/04 , A01N25/02 , A61K9/107 , B01F17/00 , B01J13/00 , A61K31/70 , A61K31/685
CPC分类号： A01N25/02 , A61K9/1075 , B01F17/0085
摘要： Liquid, active substance formulations containing an active substance insoluble or poorly soluble in water, or a mixture, a phospholipid, a special co-emulsifier (glycerinester in which the 1 or 2 OH groups have been esterized with hydrocarbon atoms of 8-16, preferably 8-10, C atoms by means of fatty acids and the 3 or remaining OH group of the glycerin body has been etherized with polyethyleneglycol, specifically, with 6-30, preferably 6-15 ethyleneoxide units) and a liquid carrier, the molar ratio of phospholipid to co-emulsifier being from 1:1 to 1:4, and the formulations being such that when added to water they form a transparent liquid system in the form of a microemulsion, with a degree of fineness of 10-200 nm in the lipid phase.
摘要翻译：包含不溶于水或难溶于水的活性物质的液体活性物质制剂，或混合物，磷脂，特殊助乳化剂（其中1或2个OH基已经被烃基原子8-16酯化的甘油酯，优选如图8-10所示，通过脂肪酸的C原子和甘油体的3个或剩余的OH基已经用聚乙二醇醚化，具体地，用6-30，优选6-15个环氧乙烷单元）和液体载体，摩尔比的磷脂与共乳化剂的比例为1:1至1:4，并且制剂使得当加入到水中时，它们形成微乳液形式的透明液体体系，其细度为10-200nm 脂质相。

5. 发明授权

US06497867B2 Use of copolymers of monoethylenically unsaturated carboxylic acids as solubilizers 有权
标题翻译：使用单烯属不饱和羧酸的共聚物作为增溶剂
公开(公告)号：US06497867B2
公开(公告)日：2002-12-24
申请号：US09953683
申请日：2001-09-18
申请人： Helmut Meffert , Axel Sanner , Gunther Berndl , Folker Ruchatz , Karl Kolter , Kurt Heinz Bauer
发明人： Helmut Meffert , Axel Sanner , Gunther Berndl , Folker Ruchatz , Karl Kolter , Kurt Heinz Bauer
IPC分类号： A61K3174
CPC分类号： A61K8/8158 , A61K8/8152 , A61K9/0014 , A61K9/0019 , A61K9/1075 , A61K9/2027 , A61K9/4866 , A61K47/32 , A61Q13/00 , A61Q17/04 , C08F220/04
摘要： The invention relates to the use of copolymers comprising a) 82 to 99.9 mol % of at least one monoethylenically unsaturated C3-C8-carboxylic acid; b) 0.1 to 18 mol % of at least one monomer selected from the group b1) N—C8-C30-alkyl-substituted amides of monoethylenically unsaturated C3-C8-carboxylic acids, b2) N,N—C8-C30-dialkyl-substituted amides of monoethylenically unsaturated C3-C8-carboxylic acids, b3) C8-C30-alkyl esters of monoethylenically unsaturated C3-C8-carboxylic acids; c) 0 to 17.9 mol % of at least one monomer selected from the group of c1) vinyl esters of aliphatic C8-C30-carboxylic acids, c2) C8-C30-alkylvinyl ethers, the mol % data for the individual components adding up to 100%, as solubilizer.
摘要翻译：本发明涉及包含a）82-99.9摩尔％的至少一种单烯属不饱和C 3 -C 8 - 羧酸的共聚物的用途; b）0.1至18摩尔％的至少一种选自b 1）N-C 8 -C 30 烷基取代的单烯属不饱和C3-C8-羧酸的酰胺，b2）单烯属不饱和C3-C8-羧酸的N，N-C8-C30-二烷基取代的酰胺，b3）单烯属不饱和的C 3 -C 30 - 烷基酯 C 3 -C 8 - 羧酸; c）0至17.9mol％的至少一种选自以下的单体：c1）脂族C 8 -C 30羧酸的乙烯基酯，c 2）C 8 -C 30烷基乙烯基醚，mol％数据为各成分加起来可达100％，作为增溶剂。

6. 发明授权

US5688776A Crosslinked polysaccharides, process for their preparation and their use 失效
标题翻译：交联多糖，其制备方法及其用途
公开(公告)号：US5688776A
公开(公告)日：1997-11-18
申请号：US302831
申请日：1994-09-16
申请人： Kurt Heinz Bauer , Juergen Betzing
发明人： Kurt Heinz Bauer , Juergen Betzing
IPC分类号： A61K9/16 , A61K9/20 , A61K9/22 , A61K9/28 , A61K9/36 , A61K9/52 , C08B37/00 , A61K31/715 , C08B37/02 , C08B37/06
CPC分类号： C08B37/0087 , A61K9/1652 , A61K9/205 , A61K9/286 , C08B37/00
摘要： The invention relates to polysaccharides which are crosslinked with bifunctional crosslinkers and are no longer water-soluble but are still biodegradable, have a swelling of from 100 to 1000%, where the swelling, which means the percentage gain in weight, is determined by the following equation: ##EQU1## in which A is the percentage gain in weight, W.sub.o is the weight of the dry polymer and W.sub.t is the weight of the swollen polymer saturated with water. It likewise relates to a process for preparing the crosslinked polysaccharides and to the use of the crosslinked polysaccharides for coating and/or embedding medicinal active substances or drug compositions. The invention furthermore relates to a drug which contains an active substance which acts in the large intestine or an active substance which is broken down on passing through the stomach or small intestine, coated with or embedded in one of the crosslinked polysaccharides.
摘要翻译： PCT No.PCT / EP93 / 00225 Sec。 371日期1994年9月16日 102（e）日期1994年9月16日PCT提交1993年2月1日PCT公布。第WO93 / 19095号公报日期1993年9月30日本发明涉及与双功能交联剂交联并且不再是水溶性但仍可生物降解的多糖，具有100至1000％的溶胀，其中溶胀，这意味着重量增加百分比，由以下等式确定：其中A是重量增益百分比，Wo是干聚合物的重量，Wt是用水饱和的溶胀聚合物的重量。它同样涉及制备交联多糖的方法，以及交联多糖用于涂覆和/或包埋药物活性物质或药物组合物的用途。本发明还涉及一种药物，其含有作用于大肠中的活性物质或活性物质，所述活性物质在穿过胃或小肠时分解，涂覆或嵌入其中一种交联多糖中。

7. 发明申请

US20090062241A1 Highly porous, fast-disintegrating solid dosage form and its way of manufacturing comprising the preparation of a powder and a freezedrying step 有权
标题翻译：高度多孔，快速崩解的固体剂型及其制备方法，包括制备粉末和自由干燥步骤
公开(公告)号：US20090062241A1
公开(公告)日：2009-03-05
申请号：US11666434
申请日：2005-10-27
申请人： Kurt Heinz Bauer
发明人： Kurt Heinz Bauer
IPC分类号： A61K31/60 , A61K31/451 , A61K31/606 , A61P43/00 , A61K31/192 , A61K31/341
CPC分类号： A61K9/0056 , A61K9/0007
摘要： The invention relates to a method of manufacture of fast-disintegrating solid dosage forms, characterized in that one or more structure building components in mixed solid powder form are dosed into cavities of blister packs or moulds, the remaining components dissolved in water dosed and added to the powder to form a moistened, plasticized mass, frozen to below −20° C. , and the water sublimed in high vacuum. In this way solid dosage forms are obtainable with a similar porous structure as usually result from freeze-drying processes, but the process requires much less water, which means considerably less time and less energy.
摘要翻译：本发明涉及一种快速崩解固体剂型的制造方法，其特征在于将一种或多种混合固体粉末形式的结构构造成分加入到泡罩包装或模具的空腔中，其余组分溶解于水中并加入粉末形成湿润的塑化块，冷冻至-20℃以下，水在高真空中升华。以这种方式，可以用通常由冷冻干燥过程产生的类似的多孔结构获得固体剂型，但是该方法需要少得多的水，这意味着显着更少的时间和更少的能量。

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