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1. 发明申请

US20080260814A1 INJECTION MOULDING PROCESS FOR NEUTRAL AND ACID-GROUP-CONTAINING (METH)ACRYLATE COPOLYMERS 审中-公开
标题翻译：用于中性和含酸基（甲基）丙烯酸酯共聚物的注射成型工艺
公开(公告)号：US20080260814A1
公开(公告)日：2008-10-23
申请号：US12106669
申请日：2008-04-21
申请人： Hans-Ulrich PETEREIT , Thomas Beckert , Manfred Assmus , Werner Hoess , Wolfgang Fuchs , Hartmut Schikowsky
发明人： Hans-Ulrich PETEREIT , Thomas Beckert , Manfred Assmus , Werner Hoess , Wolfgang Fuchs , Hartmut Schikowsky
IPC分类号： A61K47/32 , C08L33/08 , C08L33/10 , A61K9/48 , B29C45/46
CPC分类号： A61K9/2095 , A61J3/077 , A61K9/2027 , A61K9/4816 , B29C45/0001
摘要： Processes for producing moldings by injection moulding, include melting a mixture made from a (meth)acrylate copolymer and a release agent, devolatilizing the mixture, injecting the molten and devolatilized mixture into a mold cavity of an injection mold, cooling the molten mixture, and removing the resultant molding from the mold.
摘要翻译：通过注射成型制造模制品的方法包括熔融由（甲基）丙烯酸酯共聚物和脱模剂制成的混合物，使混合物脱挥发分，将熔融和脱挥发分的混合物注入注模的模腔中，冷却熔融混合物，以及从模具中取出所得模制品。

2. 发明授权

US06576255B1 Injection molding method for (meth)acrylate copolymers having tertiary ammonium groups 失效
标题翻译：具有叔铵基的（甲基）丙烯酸酯共聚物的注射成型方法
公开(公告)号：US06576255B1
公开(公告)日：2003-06-10
申请号：US09889565
申请日：2001-07-30
申请人： Hans-Ulrich Petereit , Thomas Beckert , Manfred Assmus , Werner Hoess , Wolfgang Fuchs , Hartmut Schikowsky
发明人： Hans-Ulrich Petereit , Thomas Beckert , Manfred Assmus , Werner Hoess , Wolfgang Fuchs , Hartmut Schikowsky
IPC分类号： A61K948
CPC分类号： A61K9/1635 , A61J3/071
摘要： The invention relates to a process for making molded articles by means of injection molding with the process steps of a) melting of a (meth)acrylate copolymer, which is composed of 30 to 80 wt % of radical-polymerized C1 to C4 alkyl esters of acrylic or methacrylic acid and 70 to 20 wt % of (meth)acrylate monomers with a tertiary ammonium group in the alkyl residue, wherein the (meth)acrylate copolymer is present in a mixture with 1 to 70 wt % of a plasticizer and a desiccant in the ratio of 1:1 to 1:20 and also with 0.05 to 5 wt % of a release agent, and further standard additives or adjuvants and if necessary even a pharmaceutical active principle can also be present in the mixture, and before the mixture is melted it has a content of more than 0.5 wt % of low-boiling constituents with a vapor pressure of at least 1.9 bar at 120° C., b) degassing of the mixture in the thermoplastic condition at temperatures of at least 120° C., whereby the content of low-boiling constituents with a vapor pressure of at least 1.9 bar at 120° C. is lowered to at most 0.5 wt % and c) injection of the melted and degassed mixture into the mold cavity of an injection-molding die, wherein the mold cavity has a temperature which lies at least 10° C. below the glass transition temperature of the (meth)acrylate copolymer, cooling of the melt mixture and removal of the obtained molded article from the mold.
摘要翻译：本发明涉及一种通过注射成型制备模塑制品的方法，其工艺步骤为：a）熔融（甲基）丙烯酸酯共聚物，其由30至80重量％的自由基聚合的C1至C4烷基酯组成丙烯酸或甲基丙烯酸和70〜20重量％的烷基残基中具有叔铵基的（甲基）丙烯酸酯单体，其中（甲基）丙烯酸酯共聚物与1至70重量％的增塑剂和干燥剂以1:1至1:20的比例和0.05至5重量％的脱模剂，并且进一步的标准添加剂或佐剂，并且如果需要甚至药物活性成分也可以存在于混合物中，并且在混合物之前熔化，其含量大于0.5重量％的低沸点成分，蒸气压在120℃下至少为1.9巴，b）在热塑性条件下，在至少120℃的温度下脱气混合物，其中低沸点成分含量为a 在120℃下至少1.9巴的蒸汽压降低至至多0.5重量％，和c）将熔融和脱气的混合物注射到注射成型模具的模腔中，其中模腔具有位于在（甲基）丙烯酸酯共聚物的玻璃化转变温度以下至少10℃，冷却熔融混合物并从模具中除去得到的模塑制品。

3. 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。

4. 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。

5. 发明申请

US20050019381A1 Binding agent which is stable in storage and used for pharmaceutical applications 审中-公开
标题翻译：在储存中稳定并用于制药应用的结合剂
公开(公告)号：US20050019381A1
公开(公告)日：2005-01-27
申请号：US10239187
申请日：2001-01-29
申请人： Hans-Ulrich Petereit , Manfred Assmus , Thomas Beckert , Guenther Bergmann , Stephanie Zacharias
发明人： Hans-Ulrich Petereit , Manfred Assmus , Thomas Beckert , Guenther Bergmann , Stephanie Zacharias
IPC分类号： A61K47/32 , A61K9/70 , A61K47/12 , A61K47/14 , C09J133/14
CPC分类号： A61K9/7023 , C08L2666/34 , C09J133/14
摘要： The invention relates to an adhesive and binder for dermal or transdermal therapy systems, consisting of (a) a (meth)acrylate copolymer composed of radically polymerized C1 to C4 alkyl esters of acrylic or methacrylic acid and (meth)acrylate monomers with a cationic ammonium group in the alkyl radical, containing (b) 0.1-45 wt.-% with reference to (a) of an organic dicarboxylic or tricarboxylic acid or an acrylate or (meth)acrylate polymer or copolymer containing an acid group, as well as (c) 20-80 wt.-% with reference to (a) of a plasticizer, and (d) if necessary, a pharmaceutically active substance and/or pharmaceutically usual additives, characterized in that dibutyl sebacate is contained as the 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，其由（a）由丙烯酸或甲基丙烯酸的自由基聚合的C1至C4烷基酯和（甲基）丙烯酸酯单体与阳离子铵组成的（甲基）丙烯酸酯共聚物在（a）有机二羧酸或三羧酸或丙烯酸酯或（甲基）丙烯酸酯或含有酸基团的共聚物或共聚物中，（a）为（a）为0.1-45重量％ c）相对于（a）增塑剂为20-80重量％，和（d）如果需要，药物活性物质和/或药学上通常的添加剂，其特征在于包含癸二酸二丁酯作为增塑剂。

6. 发明授权

US6063399A Adhesive binders for dermal or transdermal therapy systems 失效
标题翻译：用于皮肤或透皮治疗系统的粘合剂粘合剂
公开(公告)号：US6063399A
公开(公告)日：2000-05-16
申请号：US995986
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 , C09J133/14 , A61F13/02
CPC分类号： A61K9/7061 , C09J133/14
摘要： An adhesive binder for dermal or transdermal therapy systems consists of the following components:(a1) 55-99.9 wt. % of a (meth)acrylate copolymer of a structural (meth)acrylate or a functional (meth)acrylate monomer, wherein the functional monomer has a tertiary or quaternary amino group,(a2) 0.1-45 wt. % of an acid group-containing acrylate or (meth)acrylate polymer or copolymer, and(b) 25-80 wt. % of a plasticizer, based on the sum of (a1) and (a2).
摘要翻译：用于皮肤或透皮治疗系统的粘合剂粘合剂由以下组分组成：（a1）55-99.9wt。％的结构（甲基）丙烯酸酯或官能（甲基）丙烯酸酯单体的（甲基）丙烯酸酯共聚物，其中官能单体具有叔或季氨基，（a2）0.1-45重量％％的含酸基的丙烯酸酯或（甲基）丙烯酸酯聚合物或共聚物，和（b）25-80重量％基于（a1）和（a2）的总和的增塑剂的％。

7. 发明授权

US5730999A Dermal therapeutic system made of a meltable poly (meth) acrylate 失效
标题翻译：由可熔融的聚（甲基）丙烯酸酯混合物制成的皮肤治疗系统
公开(公告)号：US5730999A
公开(公告)日：1998-03-24
申请号：US650025
申请日：1996-05-17
申请人： Klaus Lehmann , Hans-Ulrich Petereit , Manfred Assmus
发明人： Klaus Lehmann , Hans-Ulrich Petereit , Manfred Assmus
IPC分类号： A61K9/70 , A61L15/44 , A61L15/58 , A61P17/00
CPC分类号： A61K9/7061 , A61L15/44 , A61L15/58 , A61L2300/40 , A61L2300/418 , A61L2300/434 , A61L2300/602
摘要： A dermal therapeutic system which exhibits a prolonged release of a drug comprising at least one pharmaceutical agent combined with poly(meth)acrylates in the form of at least one layer of the therapeutic system, the poly(meth)acrylates being a mixture, which is produced from a melt, comprising (1) at least one (meth)acrylic polymer containing functional groups and (2) at least one (meth)acrylic polymer which regulates the flow behavior of the poly(meth)acrylate mixture and which contains no functional groups or only insignificant amounts of functional groups.
摘要翻译：显示药物延长释放的真皮治疗系统，其包含至少一种药物剂，其与至少一层治疗系统形式的聚（甲基）丙烯酸酯组合，所述聚（甲基）丙烯酸酯是混合物，其为由（1）至少一种含有官能团的（甲基）丙烯酸聚合物和（2）调节聚（甲基）丙烯酸酯混合物的流动行为的至少一种（甲基）丙烯酸类聚合物，其不含功能性组或仅有微量的官能团。

8. 发明申请

US20110033530A1 COATING COMPOSITION FOR THE DIP COATING OF CAPSULE HALVES 有权
标题翻译：涂料组合物用于胶囊的浸涂
公开(公告)号：US20110033530A1
公开(公告)日：2011-02-10
申请号：US12845994
申请日：2010-07-29
申请人： Brigitte SKALSKY , Manfred Assmus , Odette Hensel , Hans-Ulrich Petereit
发明人： Brigitte SKALSKY , Manfred Assmus , Odette Hensel , Hans-Ulrich Petereit
IPC分类号： A61K9/48 , A61K47/32 , B05D5/00 , A23P1/08
CPC分类号： A23P1/04 , A23P10/30 , A61K9/4891 , A61K47/32
摘要： A coating composition for the enteric coating of capsule halves made of water-soluble or water-swellable polymer material in a dipping process is provided. The composition is an aqueous dispersion or solution, containing a polymer mixture of at least one first (meth)acrylate copolymer, which is enteric, and at least one further (meth)acrylate copolymer, which is enteric or water-insoluble, and also auxiliaries which influence the viscosity of the dispersion and the elasticity of the dried polymer film. The solids content of the dispersion or solution is more than 25% by weight and the viscosity is 150 to 1500 mPa·s and a dried film produced from the dispersion or solution has an elongation at break of at least 200%. Also provided is a capsule composed of two capsule halves coated with the dispersion or solution in a dipping process does. The enteric capsule does not dissolve in 0.1 N HCl at pH 1.2 after two hours, but completely dissolves in buffer at pH 6.8 in less than 30 minutes. A method to prepare enteric coated capsule halves is also provided.
摘要翻译：提供了一种用于在浸渍过程中由水溶性或水溶胀性聚合物材料制成的胶囊半部的肠溶衣涂料组合物。该组合物是含有至少一种肠溶性的至少一种第一（甲基）丙烯酸酯共聚物和至少一种其它（甲基）丙烯酸酯共聚物的聚合物混合物的水性分散体或溶液，其为肠溶或水不溶性的，以及辅助剂这影响了分散体的粘度和干燥的聚合物膜的弹性。分散体或溶液的固体成分大于25重量％，粘度为150〜1500mPa·s，由分散液或溶液制得的干燥膜的断裂伸长率为200％以上。还提供了由在浸渍过程中涂覆有分散体或溶液的两个胶囊半部组成的胶囊。肠溶胶囊在pH2.2后2小时内不溶于0.1N HCl，但在不到30分钟内完全溶于pH 6.8的缓冲液中。还提供了制备肠溶衣胶囊半部的方法。

9. 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％。

10. 发明申请

US20060269605A1 Multilayer pharmaceutical dosage form containing a substance that acts in a modulatory manner with regard to the release of active substances 审中-公开
标题翻译：含有在活性物质释放方面以调节方式起作用的物质的多层药物剂型
公开(公告)号：US20060269605A1
公开(公告)日：2006-11-30
申请号：US10572963
申请日：2004-09-15
申请人： Rosario Lizio , Hans-Ulrich Petereit , Manfred Assmus , Hema Ravishankar
发明人： Rosario Lizio , Hans-Ulrich Petereit , Manfred Assmus , Hema Ravishankar
IPC分类号： A61K9/24
CPC分类号： A61K9/5078 , A61K9/5026
摘要： The invention relates to a multilayer pharmaceutical dosage form for the controlled release of active substances, containing: a) a core layer containing a substance that acts in a modulatory manner with regard to the release of active substances, optionally a neutral core and/or an active substance; b) an inner control layer that influences the release of the substance that acts in a modulatory manner and of the optionally contained active substance from the core layer, containing pharmaceutically useable polymers, waxes, resins and/or proteins; c) an active substance layer containing a pharmaceutical active substance and, optionally, a substance that acts in a modulatory manner; d) an outer control layer containing a (meth)acrylate copolymer or a mixture consisting of a number of (meth)acrylate copolymers comprised of 98 to 85 C1-C4 alkyl esters of (meth)acrylic acid and 2 to 15% by weight of methacrylate monomers with a quaternary ammonium group in the alkyl radical and optionally containing pharmaceutically useable polymers that are insoluble in water, whereby the layers can contain, in addition and in a known manner, pharmaceutically conventional adjuvants.
摘要翻译：本发明涉及用于控制释放活性物质的多层药物剂型，其包含：a）核心层，其含有相对于活性物质的释放以调节方式起作用的物质，任选的中性核和/或活性物质 b）内部控制层，其影响以调节方式起作用的物质的释放，以及含有药学上可用的聚合物，蜡，树脂和/或蛋白质的核心层中任选地含有的活性物质; c）含有药物活性物质和任选的以调节方式作用的物质的活性物质层; d）包含（甲基）丙烯酸酯共聚物的外部控制层或由多个（甲基）丙烯酸酯共聚物组成的混合物，所述（甲基）丙烯酸酯共聚物包含98至85℃1〜（甲基）丙烯酸的烷基酯和2至15重量％的在烷基中具有季铵基团的甲基丙烯酸酯单体，并且任选地含有不溶于水的药学上可用的聚合物，其中所述层还可以包含已知的方式，药学上常规的佐剂。

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