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1. 发明申请

US20050197434A9 Granulate or powder for producing coating or binding agents for medicaments 有权
标题翻译：用于生产药物的涂层或粘合剂的颗粒或粉末
公开(公告)号：US20050197434A9
公开(公告)日：2005-09-08
申请号：US10489856
申请日：2003-07-08
申请人： Hans-Ulrich Petereit , Christian Meier , Erna Roth , Andreas Gryczke
发明人： Hans-Ulrich Petereit , Christian Meier , Erna Roth , Andreas Gryczke
IPC分类号： A61K9/16 , A61K9/28 , A61K9/50 , A61K47/10 , A61K47/12 , A61K47/32 , B29C39/14 , C08J3/00 , C08J5/00 , C08K5/04
CPC分类号： A61K9/1694 , A61K9/1635 , A61K9/1682 , A61K9/2846 , A61K9/5026
摘要： The invention relates to a process for the production of granules or powders, suitable as coating agents and binders for oral or dermal pharmaceutical forms, for cosmetics or food supplements, consisting essentially of (a) a copolymer, consisting of free radical- polymerized C1- to C4-esters of acrylic or methacrylic acid and further (meth)acrylate monomers which contain functional tertiary amino groups, (b) 3 to 25% by weight, based on (a), of an emulsifier having an HLB of at least 14, (c) 5 to 50% by weight, based on (a), of a C12- to C18-monocarboxylic acid or of a C12- to C18- hydroxyl compound, where the components (a), (b) and (c) are simultaneously or successively blended or mixed with one another, optionally with addition of a pharmaceutical active compound and/or further customary additives, fused in a heatable mixer, mixed, the melt is cooled and comminuted to give granules or powders.
摘要翻译：本发明涉及一种用于生产用于化妆品或食品补充剂的适合作为口服或皮肤药物形式的包衣剂和粘合剂的颗粒或粉末的方法，其基本上由（a）共聚物组成，所述共聚物由游离基聚合的C1- 丙烯酸或甲基丙烯酸的C 4 - 酯和另外（甲基）丙烯酸酯单体，其中含有官能叔氨基，（b）3-25重量％，基于（a）的HLB为至少14的乳化剂，（c）5至50重量％，基于（a），C 12 - 12 - C 18 - 单羧酸或C 12 - 其中组分（a），（b）和（c）同时或相继地彼此混合或混合，任选地加入药物活性物质化合物和/或其它常规添加剂，在可加热混合器中熔融混合，将熔体冷却并粉碎以产生颗粒或粉末。

2. 发明授权

US07175857B2 Granulate or powder for producing coating or binding agents for medicaments 有权
标题翻译：用于生产药物的涂层或粘合剂的颗粒或粉末
公开(公告)号：US07175857B2
公开(公告)日：2007-02-13
申请号：US10489856
申请日：2003-07-08
申请人： Hans-Ulrich Petereit , Christian Meier , Erna Roth , Andreas Gryczke
发明人： Hans-Ulrich Petereit , Christian Meier , Erna Roth , Andreas Gryczke
IPC分类号： A61K9/14 , A61K9/16
CPC分类号： A61K9/1694 , A61K9/1635 , A61K9/1682 , A61K9/2846 , A61K9/5026
摘要： The invention relates to a process for the production of granules or powders, suitable as coating agents and binders for oral or dermal pharmaceutical forms, for cosmetics or food supplements, consisting essentially of (a) a copolymer, consisting of free radical-polymerized C1- to C4-esters of acrylic or methacrylic acid and further (meth)acrylate monomers which contain functional tertiary amino groups, (b) 3 to 25% by weight, based on (a), of an emulsifier having an HLB of at least 14, (c) 5 to 50% by weight, based on (a), of a C12- to C18-monocarboxylic acid or of a C12- to C18-hydroxyl compound, where the components (a), (b) and (c) are simultaneously or successively blended or mixed with one another, optionally with addition of a pharmaceutical active compound and/or further customary additives, fused in a heatable mixer, mixed, the melt is cooled and comminuted to give granules or powders.
摘要翻译：本发明涉及一种用于生产用于化妆品或食品补充剂的适合作为口服或皮肤药物形式的包衣剂和粘合剂的颗粒或粉末的方法，其基本上由（a）共聚物组成，所述共聚物由游离基聚合的C1- 丙烯酸或甲基丙烯酸的C 4 - 酯和另外（甲基）丙烯酸酯单体，其中含有官能叔氨基，（b）3-25重量％，基于（a）的HLB为至少14的乳化剂，（c）5至50重量％，基于（a），C 12 - 12 - C 18 - 单羧酸或C 12 - 其中组分（a），（b）和（c）同时或相继地彼此混合或混合，任选地加入药物活性物质化合物和/或其它常规添加剂，在可加热混合器中熔融混合，将熔体冷却并粉碎以产生颗粒或粉末。

3. 发明申请

US20080206324A1 PELLETS HAVING AN ACTIVE COMPOUND MATRIX AND A POLYMER COATING, AND A PROCESS FOR THE PRODUCTION OF THE PELLETS 审中-公开
标题翻译：具有活性化合物基质和聚合物涂料的片剂以及生产小片剂的方法
公开(公告)号：US20080206324A1
公开(公告)日：2008-08-28
申请号：US12030377
申请日：2008-02-13
申请人： Andreas Gryczke , Hans-Ulrich Petereit , Christian Meier , Kathrin Nollenberger , Christian Brunnengraber , Andreas Klosendorf , Reinhard Menzel
发明人： Andreas Gryczke , Hans-Ulrich Petereit , Christian Meier , Kathrin Nollenberger , Christian Brunnengraber , Andreas Klosendorf , Reinhard Menzel
IPC分类号： A61K9/48 , A61K9/14 , A61K9/32
CPC分类号： A61K9/1635 , A61K9/5026 , A61K31/52
摘要： An active compound-containing pellet has a polymer coating of an anionic (meth)acrylate copolymer and a pharmaceutically active substance, embedded in a polymer matrix of one or more polymers, a particle size in the range from 300 to 1100 μm, a friability of at most 0.1%, measured using 200 g of pellets in a screening machine having a 200 μm screen, a screening diameter of 20 cm and 1.5 mm shaking amplitude at a shaking frequency of 50 l/sec for 10 min in the presence of six rubber cubes having a 1.8 cm edge length, with the proviso that the pellet releases no more than 10% of the active compound in a release test according to USP in artificial gastric juice at pH 1.2 after 120 min.
摘要翻译：含活性化合物的颗粒具有嵌入在一种或多种聚合物的聚合物基质中的阴离子（甲基）丙烯酸酯共聚物和药物活性物质的聚合物涂层，粒度在300至1100μm的范围内，脆性在具有200μm筛网的筛选机中使用200g粒料测量，至少0.1％，筛选直径为20cm和1.5mm，振荡频率为50l / sec，在六个橡胶存在下摇动10分钟具有1.8厘米边缘长度的立方体，条件是在120分钟后pH 1.2的人造胃液中，根据USP的释放试验中，颗粒释放不超过10％的活性化合物。

4. 发明授权

US08343542B2 Method for producing an immediately decomposing oral form of administration which releases active ingredients 有权
公开(公告)号：US08343542B2
公开(公告)日：2013-01-01
申请号：US10542283
申请日：2003-11-21
申请人： Hans-Ulrich Petereit , Christian Meier , Andreas Gryczke
发明人： Hans-Ulrich Petereit , Christian Meier , Andreas Gryczke
IPC分类号： A61K9/20 , B27N3/00
CPC分类号： A61J3/10 , A61K9/0056 , A61K9/146 , A61K9/1647 , A61K9/2054 , A61K31/192
摘要： The invention relates to a method for producing an oral form of administration which decomposes immediately and releases active ingredients in the mouth. According to said method, (a) an anionic pharmaceutical active ingredient is intensively mixed with (b) a copolymer consisting of radically polymerized C1-C4 esters of the acrylic acid or methacrylic acid and other (meth)acrylate monomers containing functional tertiary amino groups, and (c) between 5 and 50 wt. %, in relation to (b), of a C12-C22 carboxylic acid in the melted mass; the mixture is solidified and ground to form a powder containing active ingredients having an average particle size of 200 μm or less; and the powder is encapsulated in a water-soluble matrix consisting of pharmaceutically standard adjuvants, on the condition that no more than 3 wt. %, in relation to the copolymer, of emulsifiers with an HLB value of at least 14 must be contained therein. The invention also relates to the powder containing active ingredients and the uses of the same.

5. 发明申请

US20090011007A1 Pharmaceutical Compositions Containing Mixtures of Polymers and Active Agents Poorly Soluble in Water 审中-公开
标题翻译：含有聚合物和活性剂混合物的药物组合物难溶于水
公开(公告)号：US20090011007A1
公开(公告)日：2009-01-08
申请号：US12159538
申请日：2007-01-17
申请人： Christian Meier , Kathrin Nollenberger , Andreas Gryczke , Hans-Ulrich Petereit , Jennifer Dressman
发明人： Christian Meier , Kathrin Nollenberger , Andreas Gryczke , Hans-Ulrich Petereit , Jennifer Dressman
IPC分类号： A61K9/48 , A61K47/00 , A61K47/38 , A61K31/4418 , A61K9/14 , A61K9/20
CPC分类号： A61K9/2027 , A61K9/1635 , A61K9/1652 , A61K9/2054 , A61K9/2077 , A61K9/5084
摘要： The invention relates to a pharmaceutical composition comprising a mixture of at least one cationic, water-soluble (meth)acrylate copolymer, at least one water-insoluble polymer and at least one active ingredient having a solubility in demineralized water of 3.3 g/l or less, characterized in that the water-insoluble polymer and the active ingredient are present in a ratio of at most 3.5 to 1 parts by weight, and the pharmaceutical composition has the property of releasing the active ingredient present in a medium buffered to pH 1.2 in dissolved form in a concentration which, after 2 hours at pH 1.2, corresponds to at least sixteen times the solubility value of the active ingredient alone at pH 1.2.
摘要翻译：本发明涉及药物组合物，其包含至少一种阳离子，水溶性（甲基）丙烯酸酯共聚物，至少一种水不溶性聚合物和在软化水中溶解度为3.3g / l的至少一种活性成分的混合物或其特征在于，水不溶性聚合物和活性成分以至多3.5至1重量份的比例存在，并且药物组合物具有释放缓冲至pH 1.2的培养基中存在的活性成分的性质溶解形式的浓度，其在pH2.2下2小时后对应于在pH1.2下单独的活性成分的溶解度值的至少十六倍。

6. 发明申请

US20120208832A1 PROCESS FOR CONVERTING A SOLID (METH)ACRYLATE COPOLYMER INTO A DISPERSED FORM BY MEANS OF A DISPERSING AGENT 有权
标题翻译：通过分散剂将固体（甲基）丙烯酸酯共聚物转化成分散形式的方法
公开(公告)号：US20120208832A1
公开(公告)日：2012-08-16
申请号：US13504527
申请日：2009-11-16
申请人： Erna Roth , Ruediger Alexowsky , Hans-Ulrich Petereit , Kathrin Nollenberger , Christian Meier
发明人： Erna Roth , Ruediger Alexowsky , Hans-Ulrich Petereit , Kathrin Nollenberger , Christian Meier
IPC分类号： A61K47/32 , C08K5/11 , C08K5/1535 , A61P11/00 , C08K5/41 , C09D105/00 , A61K31/522 , C08L5/00 , C08K5/06
CPC分类号： C08J3/03 , A61K9/284 , A61K9/5026 , A61K9/5089 , C08J3/05 , C08J2333/14
摘要： The present invention provides a process for converting a solid (meth)acrylate copolymer into a dispersed form by preparing an aqueous dispersion comprising the components (a) a (meth)acrylate copolymer which is composed of free-radical polymerized methyl methacrylate, ethylacrylate and a salt of 2-trimethylammoniumethyl methacrylate, present in solid form as a powder or as a granulate, (b) up to 50% by weight calculated on the (meth)acrylate copolymer (a) of a dispersing agent selected from the groups of (b) i) plasticizers in combination with emulsifiers and/or (b) ii) pharmaceutically acceptable carbohydrates having 6 to 18 carbon atoms with a functional group and (c) water by mixing the components (a), (b) and (c) to give a suspension which becomes an aqueous dispersion during the conversion of the solid (meth)acrylate copolymer into the dispersed form, characterized in that, the (meth)acrylate copolymer is converted into the dispersed form by means of the presence of the dispersing agent at a temperature of less than 50° C.
摘要翻译：本发明提供了一种将固体（甲基）丙烯酸酯共聚物转化成分散形式的方法，其中制备含有（a）（甲基）丙烯酸酯共聚物的组分的水性分散体，该组分由自由基聚合的甲基丙烯酸甲酯，丙烯酸乙酯和以甲基丙烯酸2-三甲基铵乙酯为盐，粉末形式为固体形式，或以颗粒形式存在，（b）按（b）所示的分散剂的（甲基）丙烯酸酯共聚物（a）计算的至多50重量％）i）与乳化剂组合的增塑剂和/或（b）ii）具有官能团的具有6至18个碳原子的药学上可接受的碳水化合物和（c）通过将组分（a），（b）和（c）得到在将固体（甲基）丙烯酸酯共聚物转化成分散形式时成为水分散体的悬浮液，其特征在于，通过存在分散体将（甲基）丙烯酸酯共聚物转化为分散形式 g试剂在低于50℃的温度下

7. 发明申请

US20120071565A1 POWDERY OR GRANULATED COMPOSITION COMPRISING A COPOLYMER, A DICARBOXYLIC ACID AND A FATTY MONOCARBOXYLIC ACID 审中-公开
标题翻译：包含共聚物，二羧酸和脂肪单羧酸的粉末或成粒组合物
公开(公告)号：US20120071565A1
公开(公告)日：2012-03-22
申请号：US13322159
申请日：2009-07-30
申请人： Erna Roth , Ruediger Alexowsky , Hans-Ulrich Petereit , Christian Meier
发明人： Erna Roth , Ruediger Alexowsky , Hans-Ulrich Petereit , Christian Meier
IPC分类号： A61K47/32 , B02C23/18 , A61K8/81
CPC分类号： C08K5/09 , C08K5/092 , C08L33/14
摘要： A powdery or granulated composition, containing: (a) a copolymer containing, in polymerized form, a C1- to C4-alkyl ester of acrylic or methacrylic acid and an alkyl(meth)acrylate monomer containing a tertiary amino group in an alkyl radical; (b) 0.5 to 10% by weight based on (a) of a dicarboxylic acid having 3 to 10 carbon atoms; and (c) 5 to 20% by weight based on (a) of a fatty monocarboxylic acid having 8 to 18 carbon atoms, where the composition contains at least by 30% by weight of (a), (b), and (c).
摘要翻译：一种粉状或粒状组合物，其含有：（a）以聚合形式含有丙烯酸或甲基丙烯酸的C 1至C 4烷基酯和在烷基中含有叔氨基的（甲基）丙烯酸烷基酯单体的共聚物; （b）相对于（a）碳原子数为3〜10的二羧酸为0.5〜10重量％和（c）基于（a）具有8至18个碳原子的脂肪一元羧酸的5至20重量％，其中所述组合物含有至少30重量％的（a），（b）和（c ）。

8. 发明授权

US06846891B2 Coating and binding agent for oral or dermal pharmaceutical forms 有权
标题翻译：用于口服或皮肤药物形式的涂层和粘合剂
公开(公告)号：US06846891B2
公开(公告)日：2005-01-25
申请号：US10463539
申请日：2003-06-18
申请人： Hans-Ulrich Petereit , Christian Meier , Erna Roth
发明人： Hans-Ulrich Petereit , Christian Meier , Erna Roth
IPC分类号： A61K47/32 , A61K9/02 , A61K9/28 , A61K9/32 , A61K9/70 , C08K5/00 , C08L33/08 , C08L33/10 , C08L33/14 , C08F220/52
CPC分类号： A61K9/2846 , Y10S524/904
摘要： The invention relates to a method for the production of a coating and excipient agent for oral or dermal dosage forms, consisting of (a) 35-98% by weight of a copolymer consisting of radically polymerized C1-C4 esters of acrylic or methacrylic acid and additional (meth)acrylate monomers having functional tertiary amino groups and (b) 1-50% by weight of a softener and 1-15% by weight of an emulgator with an HLB value of less than 14, wherein constituents (a), (b) and (c) are mixed with or without adding water and optionally adding a pharmaceutical active substance and other conventional additives and the coating and excipient agent is produced by melting, casing, spreading or spraying. The invention is characterized in that the copolymer (a) is applied in powder form with a mean particle size of 1-40 μm.
摘要翻译：本发明涉及一种生产用于口服或皮肤剂型的包衣和赋形剂的方法，由（a）35-98重量％的由丙烯酸或甲基丙烯酸的自由基聚合的C1-C4酯组成的共聚物和具有官能叔氨基的另外的（甲基）丙烯酸酯单体和（b）1-50重量％的软化剂和1-15重量％的HLB值小于14的乳化剂，其中（a），（ b）和（c）与或不加入水混合，并且任选地加入药物活性物质和其它常规添加剂，并且通过熔化，套管，铺展或喷涂制备涂层和赋形剂。本发明的特征在于共聚物（a）以平均粒径为1-40μm的粉末形式施用。

9. 发明授权

US10113050B2 Powdery or granulated composition comprising a copolymer, a dicarboxylic acid and a fatty monocarboxylic acid 有权
公开(公告)号：US10113050B2
公开(公告)日：2018-10-30
申请号：US13322159
申请日：2009-07-30
申请人： Erna Roth , Ruediger Alexowsky , Hans-Ulrich Petereit , Christian Meier
发明人： Erna Roth , Ruediger Alexowsky , Hans-Ulrich Petereit , Christian Meier
IPC分类号： C08K5/09 , C08K5/092 , C08L33/14
摘要： A powdery or granulated composition, containing: (a) a copolymer containing, in polymerized form, a C1- to C4-alkyl ester of acrylic or methacrylic acid and an alkyl(meth)acrylate monomer containing a tertiary amino group in an alkyl radical; (b) 0.5 to 10% by weight based on (a) of a dicarboxylic acid having 3 to 10 carbon atoms; and (c) 5 to 20% by weight based on (a) of a fatty monocarboxylic acid having 8 to 18 carbon atoms, where the composition contains at least by 30% by weight of (a), (b), and (c).

10. 发明授权

US07494690B2 Method of producing pharmaceuticals or food supplements comprising pigmented polymer coatings 失效
标题翻译：制备包含着色聚合物涂层的药物或食品补充剂的方法
公开(公告)号：US07494690B2
公开(公告)日：2009-02-24
申请号：US10539808
申请日：2003-10-18
申请人： Hans-Ulrich Petereit , Christian Meier , Erna Roth
发明人： Hans-Ulrich Petereit , Christian Meier , Erna Roth
IPC分类号： B05D3/00 , B05D7/00 , B32B5/16
CPC分类号： A61K9/5089 , A23L5/42 , A23L33/25 , A61K9/2846 , A61K9/2893 , A61K9/4891 , A61K9/5026 , Y10T428/2998
摘要： The invention relates to a method for producing pharmaceuticals or parts thereof or food supplements or parts thereof, by coating substrates with a film-forming coating agent containing a pigment which is incompatible with the coating agent. The invention also relates to appliances for carrying out said method, especially a drum coater, a mushroom mixer, a fluidised bed appliance or a spray sifter comprising multiple spray devices.
摘要翻译：本发明涉及通过用含有与涂布剂不相容的颜料的成膜包衣剂涂布基材来制备药物或其部分或食品添加剂或其部分的方法。本发明还涉及用于执行所述方法的设备，特别是鼓式涂布机，蘑菇式混合器，流化床装置或包括多个喷射装置的喷雾筛分机。

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