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51. 发明授权

US5993849A Hydrophilic adhesive and binder for medications 失效
标题翻译：亲水性粘合剂和药物粘合剂
公开(公告)号：US5993849A
公开(公告)日：1999-11-30
申请号：US995974
申请日：1997-12-22
申请人： Manfred Assmus , Thomas Beckert , Guenter Bergmann , Stephanie Kaehler , Hans-Ulrich Petereit
发明人： Manfred Assmus , Thomas Beckert , Guenter Bergmann , Stephanie Kaehler , Hans-Ulrich Petereit
IPC分类号： A61K9/70 , A61L15/44 , A61L15/58 , C08F8/00 , C09J133/14 , A61M37/00
CPC分类号： A61K9/7061 , A61L15/44 , A61L15/58 , C08F8/00 , C08F8/10 , C09J133/14 , A61L2300/00 , C08F2800/20
摘要： The invention relates to an adhesive and binder for dermal or transdermal therapy systems, that includes (a) 85-99.9 weight % of (meth)acrylate copolymer of structural and functional monomers, where the functional monomers have tertiary or quaternary amino groups, (b) 0.1-15 weight % of an organic dicarboxylic or tricarboxylic acid, and (c) 40-70 weight %, relative to the total of (a) and (b), of a plasticizer.
摘要翻译：本发明涉及用于皮肤或透皮治疗系统的粘合剂和粘合剂，其包括（a）85-99.9重量％的结构和功能单体的（甲基）丙烯酸酯共聚物，其中官能单体具有叔或季氨基，（b ）0.1-15重量％的有机二羧酸或三羧酸，和（c）相对于（a）和（b）的总量为40-70重量％的增塑剂。

52. 发明授权

US5296512A Water-soluble pressure-sensitive skin adhesive, its use, and agents provided with it 失效
标题翻译：水溶性压敏皮肤粘合剂，其用途和代理商提供
公开(公告)号：US5296512A
公开(公告)日：1994-03-22
申请号：US896790
申请日：1992-06-09
申请人： Helmut Beier , Hans-Ulrich Petereit , Gunter Bergmann
发明人： Helmut Beier , Hans-Ulrich Petereit , Gunter Bergmann
IPC分类号： A61K9/70 , A61L15/58 , C09J133/02 , C09J133/04 , C08L31/02 , C08L33/10
CPC分类号： C09J133/02 , A61L15/58 , C09J2201/606 , Y10S514/944 , Y10S514/953
摘要： A salt of an uncrosslinked copolymer of a monoethylenically unsaturated mono- or dicarboxylic acid and an alkyl ester of acrylic or methacrylic acid is suitable as a pressure-sensitive skin adhesive for plasters, for transdermal pharmaceutical forms, or for fastening bandages, which is permanently flexible and can be washed off with water, for which the proportion of carboxylic acid has to be sufficient to make the copolymer water-soluble in the salt form.
摘要翻译：单烯键式不饱和单羧酸或二羧酸与丙烯酸或甲基丙烯酸的烷基酯的未交联共聚物的盐适合作为膏药的压敏皮肤粘合剂，用于经皮药物形式或用于紧固绷带，其是永久柔性的并且可以用水洗涤，羧酸的比例必须足以使共聚物以盐形式溶于水。

53. 发明授权

US09011907B2 Coated pharmaceutical or nutraceutical preparation with enhanced pulsed active substance release 有权
标题翻译：具有增强脉冲活性物质释放的涂层药物或营养制剂
公开(公告)号：US09011907B2
公开(公告)日：2015-04-21
申请号：US12742945
申请日：2008-02-01
申请人： Hema Ravishankar , Shradda Bodinge , Hans-Ulrich Petereit
发明人： Hema Ravishankar , Shradda Bodinge , Hans-Ulrich Petereit
IPC分类号： A61K9/64 , A61K9/20 , A61K9/50
CPC分类号： A61K9/5078 , A61K9/2081
摘要： The present invention relates to a pharmaceutical or nutraceutical preparation comprising a) a core containing a pharmaceutically or nutraceutically active substance and a substance that acts in a modulatory manner with regard of the release of pharmaceutically or nutraceutically active substances; and b) a controlling layer surrounding the core comprising i) 55 to 92% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of 80 to 98% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from C1 to C4 alkyl esters of (meth)acrylic acid and 2 to 20% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from (meth)acrylate monomers with a quaternary ammonium group in the alkyl radical; and ii) 8 to 45% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of more than 5 to 59% by weight based on the weight of the copolymer of structural units derived from acrylic acid or methacrylic acid and to tablets or capsules comprising same.
摘要翻译：本发明涉及一种药物或营养制剂，其包含a）含有药学上或营养活性物质的核心和在释放药学或营养活性物质方面以调节方式起作用的物质; 和b）围绕芯的控制层，其包含i）55至92重量％，基于存在于由80重量份组成的多个（甲基）丙烯酸酯共聚物的一种或多种混合物的层中的（甲基）丙烯酸共聚物的总重量至（甲基）丙烯酸共聚物的重量比为基于（甲基）丙烯酸的C1至C4烷基酯的结构单元的（甲基）丙烯酸共聚物的重量计为98重量％，以及（甲基）丙烯酸共聚物的重量为2至20重量％衍生自烷基中具有季铵基团的（甲基）丙烯酸酯单体的结构单元; 和ii）8至45重量％，基于存在于由多于5至59重量％组成的多个（甲基）丙烯酸酯共聚物的一种或多种的（甲基）丙烯酸酯共聚物的层中的（甲基）丙烯酸共聚物的总重量）衍生自丙烯酸或甲基丙烯酸的结构单元的共聚物与包含其的片剂或胶囊的重量。

54. 发明授权

US08951558B2 Aqueous carbonated medium containing an amino(meth)acrylate polymer or copolymer 有权
标题翻译：包含氨基（甲基）丙烯酸酯聚合物或共聚物的含水碳酸酯介质
公开(公告)号：US08951558B2
公开(公告)日：2015-02-10
申请号：US13322530
申请日：2009-07-30
申请人： Rosario Lizio , Michael Damm , Hans-Ulrich Petereit
发明人： Rosario Lizio , Michael Damm , Hans-Ulrich Petereit
IPC分类号： A61K9/48 , A61K9/32 , A61K9/16 , A61K9/50 , A23G3/02 , A23L1/30 , A23L3/015 , A23P1/00 , B29D22/00 , B29D23/00 , B32B1/08 , B32B27/08 , A61K47/32 , C08F8/30 , C08L39/00 , A61K47/08
CPC分类号： A61K47/08 , Y10T428/13 , Y10T428/1352
摘要： The invention relates to an aqueous medium containing an amino(meth)acrylate polymer or copolymer which is not soluble in dematerialised water, characterized in that the medium has a content of an aqueous phase of at least 60% by weight and a content of up to 40% by weight of solids comprising the amino(meth)acrylate polymer or copolymer, whereby the aqueous phase is charged by a sufficient amount of carbon dioxide that effects the amino(meth)acrylate polymer or copolymer to be present in solute form in the medium. The aqueous medium may be used beneficially as a coating or binding solution for the spray coating or binding of pharmaceutical compositions or nutraceutical compositions or cosmetical compositions.
摘要翻译：本发明涉及含有不溶于非物质化水的氨基（甲基）丙烯酸酯聚合物或共聚物的水性介质，其特征在于该介质的含水量至少为60重量％，含量至多 40重量％的包含氨基（甲基）丙烯酸酯聚合物或共聚物的固体，由此通过足够量的二氧化碳装入水相，使得氨基（甲基）丙烯酸酯聚合物或共聚物以溶质形式存在于介质中。有利地，水性介质可用作药物组合物或营养组合物或美容组合物的喷涂或结合的包衣或结合溶液。

55. 发明授权

US08313778B2 Drug-delivery systems 有权
标题翻译：给药系统
公开(公告)号：US08313778B2
公开(公告)日：2012-11-20
申请号：US12090754
申请日：2006-10-25
申请人： Matthias Seiler , Norbert Windhab , Manfred Stickler , Hans-Ulrich Petereit
发明人： Matthias Seiler , Norbert Windhab , Manfred Stickler , Hans-Ulrich Petereit
IPC分类号： A61K9/14
CPC分类号： A61K9/146 , A61K9/1641 , A61K47/34 , A61K47/59 , A61K47/595 , A61K47/62
摘要： The invention relates to novel particulate drug-delivery systems based on a polymer support containing at least one linear, branched or cross-linked polymer in a fraction of over 50 percent by weight in relation to the total weight of the support. The system is characterized in that at least one signal substance for transport through a biological barrier and at least one active ingredient are stored, the support, signal substance and active ingredient having no covalent links and no active-ingredient specific and signal substance specific coordinative links between one another.
摘要翻译：本发明涉及基于聚合物载体的新型颗粒药物递送系统，其包含至少一种相对于载体总重量超过50重量％的直链，支链或交联聚合物。该系统的特征在于，存储用于传输通过生物屏障和至少一种活性成分的至少一种信号物质，所述载体，信号物质和没有共价连接并且没有活性成分特异性和信号物质特异性协调链接的信号物质和活性成分在彼此之间

56. 发明申请

US20100239666A1 Process for producing mouldings from (meth) acrylate copolymers by means of injection moulding 审中-公开
标题翻译：通过注射成型由（甲基）丙烯酸酯共聚物制备模制品的方法
公开(公告)号：US20100239666A1
公开(公告)日：2010-09-23
申请号：US12793549
申请日：2010-06-03
申请人： Hans-Ulrich Petereit , Thomas Beckert , Manfred Assmus , Wemer Hoess , Wolfgang Fuchs , Hartmut Schikowsky
发明人： Hans-Ulrich Petereit , Thomas Beckert , Manfred Assmus , Wemer Hoess , Wolfgang Fuchs , Hartmut Schikowsky
IPC分类号： A61K9/52 , A61K47/32 , A61K31/60 , A61K31/34 , A61K31/35 , A61K31/40 , A61K31/44 , A61K31/43 , A61K31/135 , A61K31/496 , A61K31/52 , A61K38/22 , A61K31/4525 , A61K31/12 , A61K31/439 , A61K31/4164 , A61K31/519 , A61K31/5415 , A61K31/277 , A61K31/16 , A61K31/4353 , A61P43/00 , A61P5/00
CPC分类号： B29C45/0001 , B29C48/06 , B29C48/09 , B29C48/395 , B29C48/76 , B29K2033/00 , B29K2105/0035
摘要： The invention relates to a process for producing mouldings by injection moulding the steps in the process being a) melting and mixing of a (meth)acrylate copolymer composed of from 85 to 98% by weight of C1-C4-alkyl (meth)acrylates capable of free-radical polymerization and from 15 to 2% by weight of (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, with from 10 to 25% by weight of a plasticizer, and also from 10 to 50% by weight of a dryers [sic] and/or from 0.1 to 3% by weight of a release agent, and, where appropriate, with other conventional pharmaceutical additives or auxiliaries and/or with an active pharmaceutical ingredient, b) devolatilizing the mixture at temperatures of at least 120° C., thus reducing the content of the low-boiling constituents with a vapour pressure of at least 1.9 bar at 120° C. to not more than 0.5% by weight, and c) injecting the devolatilized mixture at a temperature of from 80 to 160° C. into the mould of an injection moulding system and removing the resultant moulding from the mould.
摘要翻译：本发明涉及一种通过注射成型制备模制品的方法，该方法为：a）熔融和混合由（甲基）丙烯酸酯共聚物组成的（甲基）丙烯酸酯共聚物，其由85至98重量％的（甲基）丙烯酸C 1 -C 4烷基酯的自由基聚合和15至2重量％的在烷基中具有季铵基团的（甲基）丙烯酸酯单体，10至25重量％的增塑剂，以及10至50重量％的干燥剂和/或0.1至3重量％的脱模剂，以及在适当情况下与其它常规药物添加剂或助剂和/或与活性药物成分的混合物，b）在温度为至少120℃，从而将低沸点组分的含量以120℃至少1.9巴的蒸汽压降低至不超过0.5重量％，和c）将脱挥发分混合物在温度从80至160℃进入注射模具模制系统，并从模具中取出所得模制品。

57. 发明申请

US20100226978A1 PH-DEPENDENT CONTROLLED RELEASE PHARMACEUTICAL OPIOID COMPOSITION WITH RESISTANCE AGAINST THE INFLUENCE OF ETHANOL 有权
标题翻译： PH依赖性控释药物抗药性组合物对乙醇的影响
公开(公告)号：US20100226978A1
公开(公告)日：2010-09-09
申请号：US12678406
申请日：2007-09-25
申请人： Hans-Ulrich Petereit , Hema Ravishankar , Ashwini Samel
发明人： Hans-Ulrich Petereit , Hema Ravishankar , Ashwini Samel
IPC分类号： A61K9/56 , A61K9/00 , A61K9/46 , A61K9/22 , A61K9/52 , A61K31/55 , A61K31/5377 , A61K31/485 , A61P25/04
CPC分类号： A61K9/5078 , A61K9/501 , A61K9/5026
摘要： The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, comprising at least one pharmaceutical active ingredient, which is an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further contains 110 to 250% by weight, calculated on dry weight of the polymer mixture, of a non-porous inert lubricant and the coating layer is present in an amount of at least 60% by weight calculated on the weight of core.
摘要翻译：本发明涉及pH依赖性控释药物组合物，其包含核心，其包含至少一种药物活性成分，其为阿片样物质，其中核心至少涂覆一层涂层，控制药物组合物的释放，其中所述涂层包含以下混合物：i）基于所述聚合物混合物的干重为40-95重量％的至少一种水不溶性基本中性乙烯基聚合物的混合物，以及ii）5-60重量％，基于聚合物混合物的干重，至少一种阴离子聚合物或共聚物，其不溶于低于pH 4.0的缓冲介质中并且可溶于至少在pH 7.0至pH 8.0的范围内，其特征在于，所述涂层还包含110至以聚合物混合物的干重计，250重量％的无孔惰性润滑剂和涂层的含量以核心重量计算为至少60重量％。

58. 发明申请

US20080220080A1 Multiparticulate Pharmaceutical form Comprising Pellets with a Substance Having a Modular Effect in Relation to Active Ingredient Release 审中-公开
标题翻译：包含颗粒与具有与活性成分释放有关的模块效应的物质的多颗粒药物形式
公开(公告)号：US20080220080A1
公开(公告)日：2008-09-11
申请号：US11816372
申请日：2006-03-03
申请人： Hans-Ulrich Petereit , Rosario Lizio , Hema Ravishankar , Ashwini Samel
发明人： Hans-Ulrich Petereit , Rosario Lizio , Hema Ravishankar , Ashwini Samel
IPC分类号： A61K9/14 , A61K31/135
CPC分类号： A61K9/209 , A61K9/2886 , A61K9/5026 , A61K9/5078
摘要： The invention relates to a multiparticulate pharmaceutical form, comprising pellets with a multilayer structure for controlled active ingredient release, comprising a) a core layer comprising a substance having a modulating effect, b) an inner controlling layer which influences the delivery of the substance having a modulating effect, consisting of pharmaceutically usable polymers, waxes, resins and/or proteins, c) an active ingredient layer comprising an active pharmaceutical ingredient and, where appropriate, a substance having a modulating effect, d) an outer controlling layer comprising at least 60% by weight of one or a mixture of a plurality of (meth)acrylate copolymers where the layers may additionally and in a manner known per se comprise pharmaceutically usual excipients, where the outer controlling layer d) has a thickness from 20 to less than 55 μm and contains 0.1 to 10% by weight of glycerol monostearate, where the multiparticulate pharmaceutical form contains 20 to 60% by weight of the pellets, which are compressed in mixture with 80 to 40% by weight of an outer phase which consists from 50 to 100% by weight of a cellulose or a derivate of cellulose and optionally 0 to 50% by weight of further pharmaceutical excipients.
摘要翻译：本发明涉及一种多颗粒药物形式，其包含具有用于受控活性成分释放的多层结构的颗粒，其包含a）包含具有调节作用的物质的芯层，b）影响具有调节作用，由药学上可用的聚合物，蜡，树脂和/或蛋白质组成，c）活性成分层，其包含活性药物成分和适当时具有调节作用的物质，d）外部控制层，其包含至少60 重量％的一种或多种（甲基）丙烯酸酯共聚物的混合物，其中层可以另外地以本身已知的方式包含药学上通常的赋形剂，其中外部控制层d）的厚度为20至小于55 并含有0.1至10重量％的单硬脂酸甘油酯，其中多颗粒药物形式含有20至60％的b 的颗粒重量，其与80至40重量％的外相以80至40重量％的混合物压缩，所述外相由50至100重量％的纤维素或纤维素衍生物和任选的0至50重量％的进一步的药物赋形剂。

59. 发明申请

US20080200482A1 Use of a Partially Neutralized, Anionic (Meth)Acrylate Copolymer as a Coating for the Production of a Medicament Releasing Active Substance at Reduced Ph Values 有权
标题翻译：使用部分中和的阴离子（甲基）丙烯酸酯共聚物作为用于生产降低Ph值的药物释放活性物质的涂层
公开(公告)号：US20080200482A1
公开(公告)日：2008-08-21
申请号：US11994440
申请日：2006-04-05
申请人： Hans-Ulrich Petereit , Manfred Assmus
发明人： Hans-Ulrich Petereit , Manfred Assmus
IPC分类号： A61K31/522
CPC分类号： A61K9/5026 , A61K9/2081 , A61K9/2846
摘要： (EN) The invention relates to the use of a partially neutralized, anionic (meth)acrylate copolymer comprising radically polymerized units of 25 to 95 percent by weight of C1 to C4 alkyl esters of acrylic or methacrylic acid and 5 to 75 percent by weight of (meth)acrylate monomers with an anionic group, at least 4 percent of which are neutralized by means of a base, for producing a medicament that is provided with an active substance-containing core and is coated with the partially neutralized, anionic (meth)acrylate copolymer. Said medicament releases at least 30 percent of the active substance contained therein in 30 minutes at a pH at which the active substance is sufficiently soluble and stable and at which the corresponding medicament that is coated with the non-neutralized anionic (meth)acrylate polymer releases less than 10 percent of the active substance contained therein.
摘要翻译：（EN）本发明涉及部分中和的阴离子（甲基）丙烯酸酯共聚物的用途，其包括25至95重量％的C 1至C 4的自由基聚合单元丙烯酸或甲基丙烯酸的烷基酯和5至75重量％的具有阴离子基团的（甲基）丙烯酸酯单体，其中至少4％通过碱中和，用于生产具有活性物质的药物并含有部分中和的阴离子（甲基）丙烯酸酯共聚物。所述药物在活性物质足够可溶和稳定的pH下在30分钟内释放其中所含活性物质的至少30％，其中涂覆有未中和的阴离子（甲基）丙烯酸酯聚合物的相应药物释放少于其中含有的活性物质的10％。

60. 发明申请

US20080166416A1 Multiparticle Pharmaceutical Dosage Form for a Low-Soluble Active Substances and Method for Producing Said Pharmaceutical Dosage Form 有权
标题翻译：用于制备低剂量活性物质的多药物药物剂型及生产所述药物剂型的方法
公开(公告)号：US20080166416A1
公开(公告)日：2008-07-10
申请号：US11572720
申请日：2005-07-08
申请人： Rosario Lizio , Hans-Ulrich Petereit , Peter Langguth , Marcus Knoll
发明人： Rosario Lizio , Hans-Ulrich Petereit , Peter Langguth , Marcus Knoll
IPC分类号： A61K9/14 , A61K31/513 , A61K31/4439 , A61K31/55
CPC分类号： A61K31/506 , A61K9/1617 , A61K9/1652 , A61K9/5026 , A61K9/5078 , A61K31/427 , A61K31/55
摘要： The invention relates to an oral multiparticle pharmaceutical dosage form in the form of a receptacle reducing the pH values of stomach, containing a plurality of pellets, particles, granules or agglomerates whose mean diameter ranges from 50 to 2500 μn substentially consisting of a) an internal matrix layer containing an active agent which is neither peptide or protein, nor the derivatives or conjugates thereof, a lipophilic matrix whose melting point is greater than 37° C. and a polymer with mucoadhesive effect, b) an external film coating substentially consisting of a polymer or an anionic copolymer which is optionally formulated with conventional pharmaceutical additives, wherein the active agent has a water solubility according to DAB 10, of at least 30 volume parts of water for one part by weight of the active agent and is coated with the lipophilic matrix and said active agent-containing lipophilic matrix is coated with a matrix made of a polymer with mucoadhesive effect. A method for producing the inventive multiparticle pharmaceutical dosage is also disclosed.
摘要翻译：本发明涉及呈容器形式的口服多颗粒药物剂型，其减少胃的pH值，其含有多个颗粒，颗粒，颗粒或附聚物，其平均直径范围为50至2500个，其特征在于a）内部含有不是肽或蛋白质的活性剂的基质层，也不是其衍生物或共轭物，其熔点大于37℃的亲脂基质和具有粘膜粘附作用的聚合物，b）由聚合物或阴离子共聚物，其任选地与常规药物添加剂配制，其中活性剂具有根据DAB 10的水溶性，至少30体积份的水用于1重量份的活性剂，并且用亲脂性基质和所述含活性剂的亲脂基质涂覆有由具有粘膜粘附作用的聚合物制成的基质。还公开了用于生产本发明的多颗粒药物剂量的方法。

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