公开(公告)号：US20100255092A1

公开(公告)日：2010-10-07

申请号：US12742263

申请日：2008-02-01

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

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

IPC分类号： A61K9/32 ,  A61K9/00 ,  A61K31/522 ,  A61P43/00

CPC分类号： A61K9/5026 ,  A61K9/5078

摘要： The present invention relates to pharmaceutical or nutraceutical preparations comprising a) a core containing a pharmaceutically or nutraceutically active substance; 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 Ci 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 and capsules containing same.

摘要翻译： 本发明涉及药物或营养制剂，其包含a）含有药学或营养物质活性物质的核心; 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C 1〜C 4烷基酯的结构单元的（甲基）丙烯酸共聚物的重量为98重量％，基于（甲基）丙烯酸共聚物的重量为2〜20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的重量，以及含有它们的片剂和胶囊的重量。

公开(公告)号：US20100151010A1

公开(公告)日：2010-06-17

申请号：US11569731

申请日：2005-05-18

申请人： Hans-Ulrich Petereit ,  Christian Meier

发明人： Hans-Ulrich Petereit ,  Christian Meier

IPC分类号： A61K9/14 ,  A61K31/606 ,  A61K31/196 ,  A61K31/573 ,  A61K31/58 ,  A61K38/43 ,  A61K38/00 ,  A61K39/00 ,  A61K39/395 ,  A61K38/54 ,  A61K38/28 ,  A61K38/22 ,  A61K31/7088 ,  A61K38/23 ,  A61K38/21 ,  A61K38/20 ,  A61K38/29 ,  A61K38/26 ,  A61K31/352 ,  A61K38/08 ,  A61K38/11 ,  A61K9/20 ,  A61K9/48 ,  B05D3/02

CPC分类号： A61K9/2846 ,  A61K9/284 ,  A61K9/2886

摘要： The invention relates to a medicament in a multilayer form, containing a) a core with a pharmaceutical agent, b) an inner coating, 50 to 95 percent by weight of which arc composed of a (co)polymer comprising 95 to 100 percent by weight of radically polymerized vinylic monomers with neutral side groups and 0 to 5 percent by weight of monomers with anionic side groups, c) an outer coaling made of a copolymer comprising 75 to 95 percent by weight of radically polymerized C1 to C4 alkyl esters of acrylic acid or methacrylic acid and 5 to 25 percent by weight of (meth)acrylate monomers with an anionic group in the alkyl radical. Said medicament further contains 5 to 30 percent by weight of common pharmaceutical auxiliaries, particularly emollients. The inventive medicament is characterized in that the inner coaling contains 5 to 50 percent by weight of common pharmaceutical auxiliaries which are no expanding agents while the amount of expanding agents provided is less than 5 percent by weight.

摘要翻译： 本发明涉及一种多层形式的药物，其包含a）具有药剂的芯，b）内涂层，其包含50-95重量％的由包含95-100重量％的（共）聚合物组成的电弧 具有中性侧基的自由基聚合的乙烯基单体和0至5重量％的具有阴离子侧基的单体，c）由包含75至95重量％的丙烯酸的自由基聚合的C1至C4烷基酯的共聚物制成的外部共聚物 或甲基丙烯酸和5至25重量％的（甲基）丙烯酸酯单体在烷基中具有阴离子基团。 所述药物还包含5-30重量％的常见药用助剂，特别是润肤剂。 本发明的药物的特征在于，内部包衣含有5至50重量％的不是发泡剂的常规药物助剂，而所提供的发泡剂的量小于5重量％。

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。

公开(公告)号：US20090011038A1

公开(公告)日：2009-01-08

申请号：US12090754

申请日：2006-10-25

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：US20080044470A1

公开(公告)日：2008-02-21

申请号：US11695848

申请日：2007-04-03

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

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

IPC分类号： A61K47/08 ,  A61K47/12 ,  A61K9/28 ,  A61K9/48

CPC分类号： A61K9/5078 ,  A61K9/5026

摘要： A pharmaceutical preparation comprising: a) a core with an active ingredient and with an organic acid and/or the salt of an organic acid; and b) a coating which envelops the core and which comprises a polymer content of (meth)acrylate copolymers which have not more than 15% by weight of cationic or anionic groups, and which comprises at least 60% by weight of a (meth)acrylate copolymer which is composed of free-radically polymerized units of 93 to 98% by weight C1- to C4-alkyl esters of acrylic or of methacrylic acid and 7 to 2% by weight (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, wherein the active ingredient has a solubility in water of at least 10 g/l at 20° C. and the coating comprises silicon dioxide particles having an average particle size in the range from 1 to 50 μm.

摘要翻译： 一种药物制剂，其包含：a）具有活性成分和有机酸和/或有机酸盐的核心; 和b）包封芯的涂层，其包含具有不超过15重量％的阳离子或阴离子基团的（甲基）丙烯酸酯共聚物的聚合物含量，并且其包含至少60重量％的（甲基）丙烯酸酯共聚物， 丙烯酸酯共聚物，其由93至98重量％的C 1〜C 4 - 丙烯酸或甲基丙烯酸的C 4 - 烷基酯的自由基聚合单元和7至 2重量％的在烷基中具有季铵基团的（甲基）丙烯酸酯单体，其中活性成分在20℃下在水中的溶解度至少为10g / l，并​​且涂层包含具有平均值的二氧化硅颗粒 粒径在1〜50μm的范围内。

公开(公告)号：US20070231397A1

公开(公告)日：2007-10-04

申请号：US11570050

申请日：2005-07-09

申请人： Hans-Ulrich Petereit ,  Wolfgang Weisbrod ,  Hans Bar

发明人： Hans-Ulrich Petereit ,  Wolfgang Weisbrod ,  Hans Bar

IPC分类号： A61K9/00

CPC分类号： A61K9/5089 ,  A61K9/5026

摘要： The invention relates to methods for producing drugs having a stable profile for the release of active ingredients, said drugs exhibiting a controlled release characteristic as a result of the coating of vinyl (co)polymers. The inventive methods are characterised in that the coated drugs are conditioned in a fluidised bed coating appliance or a drum coating appliance for at least 10 minutes until a stable profile for the release of active ingredients is reached at a temperature of between 30 and 70° C. A humidity of between 5 and 30% is regulated during the conditioning process.

摘要翻译： 本发明涉及用于生产具有稳定的释放活性成分的药物的药物的方法，所述药物由于乙烯基（共）聚合物的涂覆而表现出控制释放特征。 本发明的方法的特征在于，将涂覆的药物在流化床包衣器具或鼓包衣器中调理至少10分钟，直到在30至70℃的温度下达到用于释放活性成分的稳定曲线 在调理过程中调节5至30％的湿度。

公开(公告)号：US20060051412A1

公开(公告)日：2006-03-09

申请号：US10542283

申请日：2003-11-21

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

发明人： Hans-Ulrich Petereit ,  Christian Meier ,  Adreas 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.

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）由丙烯酸的自由基聚合的C 1 -C 4 -C 4酯的共聚物密集混合 或甲基丙烯酸和其它含有官能叔氨基的（甲基）丙烯酸酯单体，和（c）5-50wt。 ％）相对于（b）相对于熔融物质中的C 12 -C 22 -C 22羧酸; 将混合物固化并研磨形成含有平均粒径为200μm或更小的活性成分的粉末; 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。

公开(公告)号：US20050084925A1

公开(公告)日：2005-04-21

申请号：US10501140

申请日：2003-10-16

申请人： Stefan Menzler ,  Thomas Boller ,  Hans-Ulrich Petereit ,  Christian Meier

发明人： Stefan Menzler ,  Thomas Boller ,  Hans-Ulrich Petereit ,  Christian Meier

IPC分类号： C12P35/04 ,  C12P35/00 ,  C07D501/14

CPC分类号： C12P35/04

摘要： The invention relates to a process for the preparation of cephalexin with the aid of a penicillin amidase immobilized on a crosslinked hydrophilic copolymer which has binding activity for ligands having nucleophilic groups and is in bead form.

摘要翻译： 本发明涉及一种借助于固定在交联的亲水共聚物上的青霉素酰胺酶来制备头孢氨苄的方法，所述交联的亲水共聚物对具有亲核基团的配体具有结合活性且呈珠粒形式。

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。

公开(公告)号：US06306428B1

公开(公告)日：2001-10-23

申请号：US09058951

申请日：1998-04-13

申请人： Klaus Lehmann ,  Hans-Ulrich Petereit

发明人： Klaus Lehmann ,  Hans-Ulrich Petereit

IPC分类号： A61K900

CPC分类号： A61K9/2095 ,  A61K9/2072 ,  A61K9/2086 ,  A61K9/7007

摘要： A time-release laminar pharmaceutical composition, comprised of rolled or folded layers of a polymer film, that contain a pharmaceutically active substance, in which the outer surface area of the polymer film which contains the active substance, and which is accessible to the digestive juices, amounts to at most 25% of the entire surface area in the rolled or folded state, and the rolled or folded layers adhere to one another in such a way that the laminar form of medication maintains its rolled or folded form for a period of at least one hour in the release test according to USP 23, Method A, apparatus 2, at 37° C. and 50 rpm, in artificial gastric juice, and at least 30% of the active substance contained in it is released in the rolled or folded state.

摘要翻译： 包含聚合物膜的卷曲或折叠层的时间释放层状药物组合物，其含有药物活性物质，其中含有活性物质的聚合物膜的外表面积并且可被消化液接触 相当于轧制或折叠状态下整个表面积的至多25％，并且卷起或折叠的层彼此粘合，使得层状形式的药物保持其卷曲或折叠形式一段时间 根据USP 23，方法A，装置2在37℃和50rpm，在人造胃液中的释放试验中至少1小时，其中含有的至少30％的活性物质被释放在轧制或 折叠状态。