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    Method For Producing An Oral Pharmaceutical Form With Immediate Disintegration And Active Ingredient Release
    2.
    发明申请
    Method For Producing An Oral Pharmaceutical Form With Immediate Disintegration And Active Ingredient Release 审中-公开
    生产具有立即崩解和活性成分释放的口服药物形式的方法

    公开(公告)号：US20130071475A1

    公开(公告)日：2013-03-21

    申请号：US13677740

    申请日：2012-11-15

    申请人： Hans-Ulrich PETEREIT ,  Christian MEIER ,  Andreas GRYCZKE

    发明人： Hans-Ulrich PETEREIT ,  Christian MEIER ,  Andreas GRYCZKE

    IPC分类号： A61J3/10 ,  A61K31/192 ,  A61K9/14

    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.

    摘要翻译： 本发明涉及一种生产口服给药方法，该方法立即分解并释放口腔内的活性成分。 根据所述方法，（a）阴离子药物活性成分与（b）由丙烯酸或甲基丙烯酸的自由基聚合的C1-C4酯和含有官能叔氨基的其它（甲基）丙烯酸酯单体组成的共聚物强烈混合， 和（c）5-50wt。 ％的（b）相对于熔融物质中的C 12 -C 22羧酸; 将混合物固化并研磨形成含有平均粒径为200μm以下的活性成分的粉末; 并将粉末包封在由药学上标准的佐剂组成的水溶性基质中，条件是不超过3wt。 相对于共聚物，HLB值至少为14的乳化剂的％必须包含在其中。 本发明还涉及含有活性成分的粉末及其用途。

    Granulate or powder for producing coating or binding agents for medicaments
    3.
    发明申请
    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：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。

    PELLETS HAVING A GASTRIC JUICE-RESISTANT ACTIVE COMPOUND MATRIX
    5.
    发明申请
    PELLETS HAVING A GASTRIC JUICE-RESISTANT ACTIVE COMPOUND MATRIX 有权
    具有耐胃肠阻遏活性化合物矩阵的片剂

    公开(公告)号：US20080206350A1

    公开(公告)日：2008-08-28

    申请号：US12034943

    申请日：2008-02-21

    申请人： Andreas Gryczke

    发明人： Andreas Gryczke

    IPC分类号： A61K9/50

    CPC分类号： A61K31/522 ,  A61K9/1635 ,  A61K9/1694

    摘要： A pellet contains a pharmaceutically active substance embedded in a polymer matrix of one or more water-insoluble polymers; wherein said polymer matrix comprises 10 to 90% by weight of an anionic polymer; with the proviso that the pellet a) releases no more than 10% of said active compound in a release test according to USP in artificial gastric juice at pH 1.2 after 120 min, and b) releases at least 50% of the active compound after altogether a further 300 min at pH 6.8 and/or pH 7.5; wherein said pellet has a particle size in the range from 300 to 1100 μm.

    摘要翻译： 颗粒含有嵌入在一种或多种水不溶性聚合物的聚合物基质中的药物活性物质; 其中所述聚合物基质包含10至90重量％的阴离子聚合物; 条件是在120分钟后，在pH 1.2的人造胃液中，丸剂a）在根据USP的释放试验中释放不超过10％的所述活性化合物，和b）总共释放出至少50％的活性化合物 在pH 6.8和/或pH7.5下再进行300分钟; 其中所述颗粒具有在300至1100μm的范围内的粒度。

    Melt extrusion of salts of active ingredients
    6.
    发明授权
    Melt extrusion of salts of active ingredients 有权
    熔融挤出活性成分的盐

    公开(公告)号：US08642089B2

    公开(公告)日：2014-02-04

    申请号：US10498829

    申请日：2003-01-30

    申请人： Hans-Ulrich Petereit ,  Christian Meier ,  Andreas Gryczke

    发明人： Hans-Ulrich Petereit ,  Christian Meier ,  Andreas Gryczke

    IPC分类号： A61K9/16 ,  A61K9/00 ,  A61K9/14 ,  A61K9/50 ,  A61K47/32

    CPC分类号： A61K9/2027 ,  A61K9/1694

    摘要： The invention relates to a method for producing active ingredient-containing granules or powders involving the following steps: a) melting a mixture consisting of a pharmaceutical active ingredient and of a (meth)acrylate copolymer, which is comprised of 40 to 75 wt. % of radically polymerized C1 to C4 alkyl esters of acrylic acid or of methacrylic acid and can be comprised of 25 to 60 wt. % (meth)acrylate monomers having an anionic group in the alkyl radial; b) extruding the mixture, and; c) comminuting the extrudate to form a granule or powder. The inventive method is characterized in that the active ingredient is the salt of an alkaline substance, and in that the pH value, which can be measured on the obtained powder or granule, is equal to or less than pH 7.0. The invention also relates to pharmaceutical dosage forms or precursors thereof, which can be produced using the inventive method.

    摘要翻译： 本发明涉及生产含有活性成分的颗粒或粉末的方法，其包括以下步骤：a）熔化由药物活性成分和（甲基）丙烯酸酯共聚物组成的混合物，其由40至75重量％ ％的丙烯酸或甲基丙烯酸的自由基聚合的C1至C4烷基酯，并且可以包含25至60重量％ 具有阴离子基团的（甲基）丙烯酸酯单体在烷基的径向上; b）挤出混合物， c）粉碎挤出物以形成颗粒或粉末。 本发明的方法的特征在于活性成分是碱性物质的盐，并且可以在所得粉末或颗粒上测量的pH值等于或小于pH7.0。 本发明还涉及可以使用本发明方法制备的药物剂型或其前体。

    Pellets having a gastric juice-resistant active compound matrix
    8.
    发明授权
    Pellets having a gastric juice-resistant active compound matrix 有权
    具有抗胃酸活性化合物基质的颗粒

    公开(公告)号：US08216613B2

    公开(公告)日：2012-07-10

    申请号：US12034943

    申请日：2008-02-21

    申请人： Andreas Gryczke

    发明人： Andreas Gryczke

    IPC分类号： A61K9/16 ,  A61K47/32 ,  A61K47/38

    CPC分类号： A61K31/522 ,  A61K9/1635 ,  A61K9/1694

    摘要： A pellet or pellets having an average particle size in the range from 300 to 1,100 μm, comprising a pharmaceutically active substance embedded in a polymer matrix of one or more water-insoluble polymers, wherein the polymer matrix additionally contains 10 to 90% by weight of an anionic polymer and with the proviso that the pellets release no more than 10% of the active compound contained in the release test according to USP in artificial gastric juice at pH 1.2 after 120 min and release at least 50% of the active compound contained after altogether a further 300 min at pH 6.8 and/or pH 7.5.

    摘要翻译： 平均粒度在300至1100μm范围内的丸粒或丸粒，其包含嵌入一种或多种水不溶性聚合物的聚合物基质中的药物活性物质，其中所述聚合物基质另外含有10至90重量％ 阴离子聚合物，条件是在120分钟后，在pH 1.2的人造胃液中，根据USP释放试验中释放不超过10％的活性化合物，并释放至少50％的活性化合物 在pH6.8和/或pH7.5下再进行300分钟。

    Method for producing an immediately decomposing oral form of administration which releases active ingredients
    9.
    发明授权
    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.