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    Coating and binding agent for pharmaceutical formulations with improved storage stability
    1.
    发明授权
    Coating and binding agent for pharmaceutical formulations with improved storage stability 有权
    具有改善储存稳定性的药物制剂的涂层和粘合剂

    公开(公告)号：US07160558B2

    公开(公告)日：2007-01-09

    申请号：US10239634

    申请日：2001-02-27

    申请人： Hans-Ulrich Petereit ,  Christian Meier ,  Erna Roth

    发明人： Hans-Ulrich Petereit ,  Christian Meier ,  Erna Roth

    IPC分类号： A61K9/14 ,  A61K9/16

    CPC分类号： A61K9/282 ,  A61K9/2846 ,  A61K47/10 ,  A61K47/12 ,  A61K47/20 ,  A61K47/32

    摘要： The invention relates to a process for the preparation of a coating and binding agent for oral or dermal pharmaceutical forms, essentially consisting 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 ammonium groups, the coplymer being present in powdered form having an average particle size of 1–40 μm, (b) 3 to 15% by weight, based on (a), of an emulsifier having an HLB of at least 14 and (c) 5 to 50% by weight, based on (a), of a C12—to C18-monocarboxylic acid or a C12—to C18-hydroxyl compound, the components (a), (b) and (c) being blended or mixed with one another with or without addition of water and if appropriate with addition of a pharmaceutical active compound and further customary additives and the coating and binding agent being produced from the mixture by melting, casting, spreading or spraying. The invention further relates to the coating and binding agent itself.

    摘要翻译： 本发明涉及一种制备用于口服或皮肤药物形式的包衣和粘合剂的方法，其基本上由（a）由丙烯酸或甲基丙烯酸的自由基聚合的C1至C4酯和（甲基）丙烯酸酯组成的共聚物 ）丙烯酸酯单体，所述共聚物以平均粒径为1-40μm的粉末形式存在，（b）基于（a）的3至15重量％的具有HLB的乳化剂 至少14和（c）5至50重量％，基于（a）的C 12 - C 18 C 18 - 单羧酸或C < 将组分（a），（b）和（c）在或不加入水中彼此混合或混合，如果 适当地添加药物活性化合物和进一步的常规添加剂，并且通过熔融，浇铸，铺展或喷涂由混合物制备涂层和粘合剂。 本发明还涉及涂层和粘合剂本身。

    Method for producing coated pharmaceuticals and food supplements with concentration gradients in the coating thereof
    3.
    发明申请
    Method for producing coated pharmaceuticals and food supplements with concentration gradients in the coating thereof 审中-公开
    用于在其涂层中生产具有浓度梯度的包衣药物和食品添加剂的方法

    公开(公告)号：US20050271778A1

    公开(公告)日：2005-12-08

    申请号：US10539614

    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： A23L1/275 ,  A23L1/308 ,  A61K9/28 ,  A61K9/48 ,  A61K9/50 ,  A23B4/00

    CPC分类号： A61K9/4891 ,  A23L5/42 ,  A23L33/24 ,  A23L33/25 ,  A61K9/2846 ,  A61K9/2866 ,  A61K9/2893 ,  A61K9/5026 ,  A61K9/5047 ,  A61K9/5089

    摘要： The invention relates to a method for producing pharmaceuticals or parts thereof or food supplements or parts thereof, by coating substrates for pharmaceutical uses or for using as food supplements for humans or animals, with a film-forming coating agent mixed with at least one other substance suitable for the cited purposes. The film-forming coating agent and the other substance first constitute separate liquid, sprayable individual portions, and are sprayed by means of at least one spray device which are provided, individually or together, with at least two separate nozzles for liquids, and have overlapping spray jets—in such a way that the individual portions sprayed out of the separate nozzles mix during the spraying process and the mixture forms a continuous film coating on the substrate, forming the food supplement, the pharmaceutical or the part thereof. The invention is characterized in that the coating agent and the other substance are in a concentration gradient from the inside to the outside.

    摘要翻译： 本发明涉及一种制备药物或其部分或食品添加剂或其部分的方法，其通过将药物用途的基质或用作人或动物的食品添加剂，与至少一种其它物质混合的成膜包衣剂 适合引用的用途。 成膜涂层剂和其它物质首先构成单独的液体，可喷雾的单独部分，并且通过至少一个喷射装置喷射，所述喷射装置单独地或一起设置有用于液体的至少两个单独的喷嘴，并且具有重叠 喷射喷嘴 - 以这样的方式，使喷射出单独喷嘴的各个部分在喷涂过程中混合，并且混合物在基材上形成连续的膜涂层，形成食品补充剂，药物或其部分。 本发明的特征在于涂层剂和其它物质的浓度梯度是从内向外。

    Coating and excipient agent for oral or dermal dosage forms
    6.
    发明授权
    Coating and excipient agent for oral or dermal dosage forms 有权
    用于口服或皮肤剂型的包衣和赋形剂

    公开(公告)号：US06624210B1

    公开(公告)日：2003-09-23

    申请号：US09764993

    申请日：2001-01-23

    申请人： Hans-Ulrich Petereit ,  Christian Meier ,  Erna Roth

    发明人： Hans-Ulrich Petereit ,  Christian Meier ,  Erna Roth

    IPC分类号： C08K904

    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 ammonium 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, casting, 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 &mgr;m.

    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 具有功能性叔铵基团的另外的（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，其中组分（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，并且通过熔融，浇铸，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。

    PROCESS FOR CONVERTING A SOLID (METH)ACRYLATE COPOLYMER INTO A DISPERSED FORM BY MEANS OF A DISPERSING AGENT
    7.
    发明申请
    PROCESS FOR CONVERTING A SOLID (METH)ACRYLATE COPOLYMER INTO A DISPERSED FORM BY MEANS OF A DISPERSING AGENT 有权
    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

    POWDERY OR GRANULATED COMPOSITION COMPRISING A COPOLYMER, A DICARBOXYLIC ACID AND A FATTY MONOCARBOXYLIC ACID
    8.
    发明申请
    POWDERY OR GRANULATED COMPOSITION COMPRISING A COPOLYMER, A DICARBOXYLIC ACID AND A FATTY MONOCARBOXYLIC ACID 审中-公开
    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 ）。

    Granulate or powder for producing coating or binding agents for medicaments
    9.
    发明授权
    Granulate or powder for producing coating or binding agents for medicaments 有权
    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。

    Coating and binding agent for oral or dermal pharmaceutical forms
    10.
    发明授权
    Coating and binding agent for oral or dermal pharmaceutical forms 有权
    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。