公开(公告)号：US20130273163A1

公开(公告)日：2013-10-17

申请号：US13648846

申请日：2012-10-10

申请人： Matthias SEILER ,  Norbert Windhab ,  Manfred Stickler ,  Hans-Ulrich Petereit

发明人： Matthias SEILER ,  Norbert Windhab ,  Manfred Stickler ,  Hans-Ulrich Petereit

IPC分类号： A61K9/14

CPC分类号： A61K9/146 ,  A61K9/1641 ,  A61K47/34 ,  A61K47/59 ,  A61K47/595 ,  A61K47/62

摘要： The invention relates to novel particulate drug-delivery systems based on a polymer support containing at least one linear, branched or cross-linked polymer in a fraction of over 50 percent by weight in relation to the total weight of the support. The system is characterised in that at least one signal substance for transport through a biological barrier and at least one active ingredient are stored, the support, signal substance and active ingredient having no covalent links and no active-ingredient specific and signal substance specific coordinative links between one another.

摘要翻译： 本发明涉及基于聚合物载体的新型颗粒药物递送系统，其包含至少一种相对于载体总重量超过50重量％的直链，支链或交联聚合物。 该系统的特征在于，存储用于传输通过生物屏障和至少一种活性成分的至少一种信号物质，所述载体，信号物质和没有共价连接并且没有活性成分特异性和信号物质特异性协调链接的信号物质和活性成分 在彼此之间

公开(公告)号：US20100291202A1

公开(公告)日：2010-11-18

申请号：US12742945

申请日：2008-02-01

申请人： Hema Ravishankar ,  Shradda Bodinge ,  Hans-Ulrich Petereit

发明人： Hema Ravishankar ,  Shradda Bodinge ,  Hans-Ulrich Petereit

IPC分类号： A61K47/32 ,  A61K9/22 ,  A61K9/52 ,  A61P43/00

CPC分类号： A61K9/5078 ,  A61K9/2081

摘要： The present invention relates to a pharmaceutical or nutraceutical preparation comprising a) a core containing a pharmaceutically or nutraceutically active substance and a substance that acts in a modulatory manner with regard of the release of pharmaceutically or nutraceutically active substances; and b) a controlling layer surrounding the core comprising i) 55 to 92% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of 80 to 98% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from C1 to C4 alkyl esters of (meth)acrylic acid and 2 to 20% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from (meth)acrylate monomers with a quaternary ammonium group in the alkyl radical; and ii) 8 to 45% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of more than 5 to 59% by weight based on the weight of the copolymer of structural units derived from acrylic acid or methacrylic acid and to tablets or capsules comprising same.

摘要翻译： 本发明涉及一种药物或营养制剂，其包含a）含有药学上或营养活性物质的核心和在释放药学或营养活性物质方面以调节方式起作用的物质; 和b）围绕芯的控制层，其包含i）55至92重量％，基于存在于由80重量份组成的多个（甲基）丙烯酸酯共聚物的一种或多种混合物的层中的（甲基）丙烯酸共聚物的总重量 至（甲基）丙烯酸共聚物的重量比为基于（甲基）丙烯酸的C1至C4烷基酯的结构单元的（甲基）丙烯酸共聚物的重量计为98重量％，基于（甲基）丙烯酸共聚物的重量为2至20重量％ 衍生自烷基中具有季铵基团的（甲基）丙烯酸酯单体的结构单元; 和ii）8至45重量％，基于存在于由多于5至59重量％组成的多个（甲基）丙烯酸酯共聚物的一种或多种（甲基）丙烯酸酯共聚物的层中的（甲基）丙烯酸共聚物）的总重量，基于 衍生自丙烯酸或甲基丙烯酸的结构单元的共聚物与包含其的片剂或胶囊的重量。

公开(公告)号：US20100247639A1

公开(公告)日：2010-09-30

申请号：US12742842

申请日：2008-02-01

申请人： Hema Ravishankar ,  Shradda Bodinge ,  Hans-Ulrich Petereit

发明人： Hema Ravishankar ,  Shradda Bodinge ,  Hans-Ulrich Petereit

IPC分类号： A61K9/00 ,  A61K9/32 ,  A61K9/48 ,  A61K31/606

CPC分类号： A23P10/30 ,  A23L27/72 ,  A61K9/5078

摘要： The present invention relates to a pharmaceutical or nutraceutical preparation comprising a) a core containing a pharmaceutically or nutraceutically active substance; and b) an inner controlling layer surrounding the core comprising i) one or a mixture of a plurality of (meth)acrylate copolymers bearing a cationic group or a group that can be converted to a cationic group; and ii) one or a mixture of a plurality of polymers or copolymers bearing an anionic group or group that can be converted to an anionic group; and c) an outer controlling layer comprising one or a mixture of a plurality of polymers or copolymers bearing an anionic group or group that can be converted to an anionic group and to tablets or capsules comprising same.

摘要翻译： 本发明涉及药物或营养制剂，其包含a）含有药学或营养活性物质的核心; 和b）围绕所述芯的内部控制层，包括i）一个或多个带有阳离子基团的甲基丙烯酸酯共聚物或可转化为阳离子基团的基团的混合物; 和ii）可以转化成阴离子基团的多个带有阴离子基团或基团的聚合物或共聚物的一种或多种混合物; 和c）包含一个或多个带有阴离子基团的聚合物或共聚物的混合物或可以转化成阴离子基团的外部控制层和包含其的片剂或胶囊的外部控制层。

公开(公告)号：US20100221324A1

公开(公告)日：2010-09-02

申请号：US12678429

申请日：2007-09-25

申请人： Hans-Ulrich Petereit ,  Hema Ravishankar ,  Ashwini Samel

发明人： Hans-Ulrich Petereit ,  Hema Ravishankar ,  Ashwini Samel

IPC分类号： A61K9/14 ,  A61K9/00 ,  A61K31/138 ,  A61K9/22 ,  A61K9/58

CPC分类号： A61K9/5078 ,  A61K9/501 ,  A61K9/5026

摘要： The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising at least one pharmaceutical active ingredient, with the exception of opioids, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer or copolymer, and ii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0. characterized in that the coating layer further contains 110 to 250% by weight, calculated on dry weight of the polymer mixture, of a non-porous inert lubricant and the is present in an amount of at least 60% by weight calculated on the weight of core.

摘要翻译： 本发明涉及pH依赖性控释药物组合物，其包含除阿片样物质以外的至少一种药物活性成分，其中核心至少涂覆一层涂层，以控制药物组合物的释放，其中涂层 至少一种不溶于水的基本上中性的乙烯基聚合物或共聚物，和ii）5-60重量％，基于干燥的聚合物混合物，i）40-95重量％，基于聚合物混合物的干重， 聚合物混合物的至少一种阴离子聚合物或共聚物的重量，其不溶于低于pH 4.0的缓冲介质并且可溶于至少在7.0至8.0的范围内。 其特征在于，所述涂层还包含110-250重量％，以聚合物混合物的干重计算的非多孔惰性润滑剂，并且其含量以至少60重量％的量存在，以重量计 核心。

公开(公告)号：US20090041842A1

公开(公告)日：2009-02-12

申请号：US11815632

申请日：2005-12-15

申请人： Rosario Lizio ,  Hans-Ulrich Petereit ,  Erna Roth ,  Michael Damm ,  Ruediger Alexowsky

发明人： Rosario Lizio ,  Hans-Ulrich Petereit ,  Erna Roth ,  Michael Damm ,  Ruediger Alexowsky

IPC分类号： A61K9/16 ,  C08L33/08 ,  A61K9/20 ,  A61K47/32

CPC分类号： C08F220/18 ,  A61K9/2846 ,  A61K9/5026

摘要： The invention relates to a partly neutralised anionic (meth)acrylate copolymer consisting of radically polymerised units containing 25-95% by weight (meth)acrylic acid C1 to C4 alkylesters and 5-75% by weight (meth)acrylate monomer with an anionic group, wherein 0.1 to 25% contained anionic groups are neutralised by a base. Said invention is characterised in that said base is embodied in the form of an cationic organic base whose molecular weight is greater than 150. A medical form containing said partly neutralised anionic (meth)acrylate copolymer and the use of said partly neutralised anionic (meth)acrylate copolymer for producing a medical form rapidly releasing an active substance having a determined pH value are also disclosed.

摘要翻译： 本发明涉及部分中和的阴离子（甲基）丙烯酸酯共聚物，其由含有25-95重量％（甲基）丙烯酸C1至C4烷基酯和5-75重量％（甲基）丙烯酸酯单体的自由基聚合单元组成，具有阴离子基团 ，其中0.1〜25％的阴离子基团被碱中和。 所述发明的特征在于所述碱以分子量大于150的阳离子有机碱的形式实施。含有所述部分中和的阴离子（甲基）丙烯酸酯共聚物的医用形式以及所述部分中和的阴离子（甲基）丙烯酸酯共聚物的用途， 丙烯酸酯共聚物，用于制备快速释放具有确定的pH值的活性物质的医用形式。

公开(公告)号：US07438929B2

公开(公告)日：2008-10-21

申请号：US10949323

申请日：2004-09-27

申请人： Thomas Beckert ,  Hans-Ulrich Petereit ,  Jennifer Dressman ,  Markus Rudolph

发明人： Thomas Beckert ,  Hans-Ulrich Petereit ,  Jennifer Dressman ,  Markus Rudolph

IPC分类号： A61K9/52 ,  A61K9/14

CPC分类号： A61K31/58 ,  A61K9/2081 ,  A61K9/5026 ,  A61K9/5073 ,  A61K9/5084 ,  A61K31/573 ,  A61K31/606 ,  A61K31/635

摘要： The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.

摘要翻译： 本发明涉及适于在小肠和大肠中均匀释放活性药物成分的多颗粒药物形式，其包含至少两种形式的颗粒A和B，其包含芯中的活性药物成分并具有不同的聚合物 确定在不同pH值下释放活性成分的涂层，其特征在于，颗粒形式A具有能够连续释放活性成分的内部聚合物涂层，并且具有快速溶解在约pH 5.5以上的外部肠溶衣，以及 颗粒形式B具有聚合物涂层，其在USP释放试验中在6小时内在pH 6.8下释放少于20％的活性成分，并在6小时内在pH 7.2下释放超过50％的活性成分。 本发明还涉及生产多颗粒药物形式的方法以及用于制备药物形式的颗粒形式A和B的用途。

公开(公告)号：US20080152719A1

公开(公告)日：2008-06-26

申请号：US11815677

申请日：2006-03-03

申请人： Hans-Ulrich Petereit ,  Rosario Lizio ,  Hema Ravishankar ,  Ashwini Samel

发明人： Hans-Ulrich Petereit ,  Rosario Lizio ,  Hema Ravishankar ,  Ashwini Samel

IPC分类号： A61K9/16

CPC分类号： A61K9/5078 ,  A61K9/2081 ,  A61K9/5015 ,  A61K9/5026

摘要： The invention relates to a multiparticulate pharmaceutical form, comprising pellets with a multilayer structure for controlled active ingredient release, comprising a) optionally a neutral core (nonpareilles), b) an inner controlling layer comprising a substance having a modulating effect, which is embedded in a matrix which influences the delivery of the modulatory substance and which comprises pharmaceutically usable polymers, waxes, resins and/or proteins, and where appropriate an active ingredient, c) an active ingredient layer comprising an active pharmaceutical ingredient and, where appropriate, a substance having a modulating effect, d) an outer controlling layer comprising at least 60% by weight of one or a mixture of a plurality of (meth) acrylate copolymers where the outer controlling layer has a thickness from 20 to less than 55 μm and contains 0,1 to 10% by weight of glycerol monostearate, where the multiparticulate pharmaceutical form contains 20 to 60% by weight of the pellets, which are compressed in mixture with 80 to 40% by weight of an outer phase which consists from 50 to 100% by weight of a cellulose or a derivate of cellulose and optionally 0 to 50% by weight of further pharmaceutical excipients.

摘要翻译： 本发明涉及多颗粒药物形式，其包含具有用于受控活性成分释放的多层结构的颗粒，其包含a）任选的中性核心（非矫正剂），b）包含调节作用的物质的内部控制层，其嵌入 影响调节物质递送的基质，其包含药学上可用的聚合物，蜡，树脂和/或蛋白质，以及适当的活性成分，c）包含活性药物成分和适当的物质的活性成分层 具有调节作用，d）包含至少60重量％的多个（甲基）丙烯酸酯共聚物中的一种或多种（甲基）丙烯酸酯共聚物的混合物的外部控制层，其中外部控制层具有20至小于55μm的厚度并且包含0 ，1至10重量％的甘油单硬脂酸酯，其中多颗粒药物形式包含20至60重量％的p 它们与80至40重量％的外相一起被压制，所述外相由50-100重量％的纤维素或纤维素衍生物和任选的0至50重量％的其它药用赋形剂组成。

公开(公告)号：US20070026082A1

公开(公告)日：2007-02-01

申请号：US10564096

申请日：2004-07-15

申请人： Rosario Lizio ,  Hans-Ulrich Petereit ,  Erna Roth ,  Ines Andres ,  Michael Damm

发明人： Rosario Lizio ,  Hans-Ulrich Petereit ,  Erna Roth ,  Ines Andres ,  Michael Damm

IPC分类号： A61K9/50 ,  A61K9/16

CPC分类号： A61K9/5026 ,  A61K9/1629 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/5078 ,  A61K38/00

摘要： The invention relates to an oral, multiparticle pharmaceutical dosage form containing pellets, the size of which ranges from 50 to 2500 μm and which essentially consist of: a) an inner matrix layer containing an active substance which is a peptide or a protein, including the derivatives or conjugates thereof, and which is embedded in a matrix consisting of a polymer with mucoadhesive effect, and b) an outer film coating essentially consisting of an anionic polymer or copolymer, which can be optionally formulated with pharmaceutically conventional adjuvants, more particularly softening agents.

摘要翻译： 本发明涉及含有丸粒的口服多颗粒药物剂型，其粒径范围为50-2500μm，其基本上由以下组成：a）包含肽或蛋白质的活性物质的内基质层，包括 衍生物或共轭物，并且其嵌入由具有粘膜粘附作用的聚合物组成的基质中，以及b）基本上由阴离子聚合物或共聚物组成的外膜包衣，其可以任选地与药学上常规的佐剂配制，更特别的是软化剂 。

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。

公开(公告)号：US20060078610A1

公开(公告)日：2006-04-13

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： A61K9/28 ,  A61K9/20 ,  A61K8/49 ,  B05D3/00

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。