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    Binding agent which is stable in storage and used for pharmaceutical applications
    1.
    发明申请
    Binding agent which is stable in storage and used for pharmaceutical applications 审中-公开
    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。

    Injection molding method for (meth)acrylate copolymers having tertiary ammonium groups
    2.
    发明授权
    Injection molding method for (meth)acrylate copolymers having tertiary ammonium groups 失效
    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。

    Adhesive binders for dermal or transdermal therapy systems
    5.
    发明授权
    Adhesive binders for dermal or transdermal therapy systems 失效
    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％。

    Dermal therapeutic system made of a meltable poly (meth) acrylate
    6.
    发明授权
    Dermal therapeutic system made of a meltable poly (meth) acrylate 失效
    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。

    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
    7.
    发明申请
    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
    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％。

    Multilayer pharmaceutical dosage form containing a substance that acts in a modulatory manner with regard to the release of active substances
    8.
    发明申请
    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
    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。

    Aqueous film coating agent for solid medicaments
    10.
    发明授权
    Aqueous film coating agent for solid medicaments 失效
    固体药物水性膜包衣剂

    公开(公告)号：US5292522A

    公开(公告)日：1994-03-08

    申请号：US998882

    申请日：1992-12-28

    申请人： Hans-Ulrich Petereit ,  Manfred Assmus ,  Klaus Lehmann

    发明人： Hans-Ulrich Petereit ,  Manfred Assmus ,  Klaus Lehmann

    IPC分类号： A61K9/28 ,  A61K9/50 ,  A61K9/16

    CPC分类号： A61K9/5073 ,  A61K9/28 ,  A61K9/282 ,  A61K9/2846 ,  A61K9/5015 ,  A61K9/5026

    摘要： A water insoluble lipophilic emulsifier having a hydrophile-lipophile balance (HLB) of 3.5 to 7, added to an aqueous dispersion containing a polymer comprising acrylic acid, methacrylic acid, their alkyl esters, and/or their alkylaminoalkyl esters, acts as a lubricant and parting agent when the resulting mixture is used for coating pharmaceutical dosage forms and prevents the pharmaceutical dosage forms being coated from sticking to one another and to the walls of the coating apparatus used.

    摘要翻译： 将亲水 - 亲油平衡（HLB）为3.5至7的水不溶性亲脂性乳化剂加入到含有丙烯酸，甲基丙烯酸，它们的烷基酯和/或它们的烷基氨基烷基酯的聚合物的水性分散体中，起润滑作用， 当所得到的混合物用于涂覆药物剂型并防止药物剂型被涂覆时彼此粘附和使用的涂覆装置的壁分离剂。