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41. 发明申请

US20080166416A1 Multiparticle Pharmaceutical Dosage Form for a Low-Soluble Active Substances and Method for Producing Said Pharmaceutical Dosage Form 有权
标题翻译：用于制备低剂量活性物质的多药物药物剂型及生产所述药物剂型的方法
公开(公告)号：US20080166416A1
公开(公告)日：2008-07-10
申请号：US11572720
申请日：2005-07-08
申请人： Rosario Lizio , Hans-Ulrich Petereit , Peter Langguth , Marcus Knoll
发明人： Rosario Lizio , Hans-Ulrich Petereit , Peter Langguth , Marcus Knoll
IPC分类号： A61K9/14 , A61K31/513 , A61K31/4439 , A61K31/55
CPC分类号： A61K31/506 , A61K9/1617 , A61K9/1652 , A61K9/5026 , A61K9/5078 , A61K31/427 , A61K31/55
摘要： The invention relates to an oral multiparticle pharmaceutical dosage form in the form of a receptacle reducing the pH values of stomach, containing a plurality of pellets, particles, granules or agglomerates whose mean diameter ranges from 50 to 2500 μn substentially consisting of a) an internal matrix layer containing an active agent which is neither peptide or protein, nor the derivatives or conjugates thereof, a lipophilic matrix whose melting point is greater than 37° C. and a polymer with mucoadhesive effect, b) an external film coating substentially consisting of a polymer or an anionic copolymer which is optionally formulated with conventional pharmaceutical additives, wherein the active agent has a water solubility according to DAB 10, of at least 30 volume parts of water for one part by weight of the active agent and is coated with the lipophilic matrix and said active agent-containing lipophilic matrix is coated with a matrix made of a polymer with mucoadhesive effect. A method for producing the inventive multiparticle pharmaceutical dosage is also disclosed.
摘要翻译：本发明涉及呈容器形式的口服多颗粒药物剂型，其减少胃的pH值，其含有多个颗粒，颗粒，颗粒或附聚物，其平均直径范围为50至2500个，其特征在于a）内部含有不是肽或蛋白质的活性剂的基质层，也不是其衍生物或共轭物，其熔点大于37℃的亲脂基质和具有粘膜粘附作用的聚合物，b）由聚合物或阴离子共聚物，其任选地与常规药物添加剂配制，其中活性剂具有根据DAB 10的水溶性，至少30体积份的水用于1重量份的活性剂，并且用亲脂性基质和所述含活性剂的亲脂基质涂覆有由具有粘膜粘附作用的聚合物制成的基质。还公开了用于生产本发明的多颗粒药物剂量的方法。

42. 发明授权

US07264943B2 Method for producing cephalexin 失效
标题翻译：生产头孢氨苄的方法
公开(公告)号：US07264943B2
公开(公告)日：2007-09-04
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： C07D501/22 , C12P35/04
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。

43. 发明申请

US20050079216A1 Pharmaceutical dosage form and method for the production thereof 有权
标题翻译：药物剂型及其制备方法
公开(公告)号：US20050079216A1
公开(公告)日：2005-04-14
申请号：US10502648
申请日：2003-01-30
申请人： Hans-Ulrich Petereit , Thomas Suefke , Christian Meier , Michael Schnabel , Ingrid Blesing , Stefan Grimm
发明人： Hans-Ulrich Petereit , Thomas Suefke , Christian Meier , Michael Schnabel , Ingrid Blesing , Stefan Grimm
IPC分类号： A61J3/06 , A61K9/02 , A61K9/08 , A61K9/20 , A61K9/28 , A61K9/32 , A61K9/48 , A61K9/50 , A61K9/52 , A61K31/49 , A61K47/20 , A61K47/32 , A61P9/06 , A61K9/14
CPC分类号： A61K9/5026 , A61K9/2846 , Y02A50/473
摘要： The invention relates to a method for producing a pharmaceutical dosage form as tablets, pellets and/or in the form of an active ingredient-containing matrix, whereby the tablets, pellets and/or active ingredient-containing matrix contain a pharmaceutical active ingredient and a copolymer serving as a coating agent and/or binding agent, and optionally contain a core and pharmaceutically common additives. According to the invention, the copolymer, the pharmaceutical active ingredient, the optionally present core and/or the pharmaceutically common additives are processed using known techniques by melting, injection molding, extrusion, wet granulation, casting, dipping, spreading out, spraying on, or pressing to form tablets, pellets and/or an active ingredient-containing matrix. The inventive method is characterized in that a copolymer is used that consists of 20 to 34 wt. % methacrylic acid, 20 to 69 wt. % methylacrylate and 0 to 40 wt. % ethylacrylate and, optionally, of 0 to 10 wt. % of additional vinylically copolymerizable monomers with the provision that the glass transition temperature of the copolymer is no higher than 60° C. according to ISO 11357-2, Item 3.3.3. The invention also relates to the pharmaceutical dosage form produced according to this method, said copolymer and the use thereof.
摘要翻译：本发明涉及用于制备药物剂型作为片剂，丸粒和/或含有活性成分的基质形式的方法，由此所述片剂，丸剂和/或含活性成分的基质含有药物活性成分和共聚物作为包衣剂和/或粘合剂，并且任选地含有核心和药学上常用的添加剂。根据本发明，共聚物，药物活性成分，任选存在的核心和/或药学上常用的添加剂使用已知技术通过熔融，注射成型，挤出，湿法制粒，浇铸，浸渍，扩散，喷涂，或压制以形成片剂，丸剂和/或含活性成分的基质。本发明的方法的特征在于使用由20〜34重量％％甲基丙烯酸，20〜69重量％％甲基丙烯酸酯和0至40wt。％丙烯酸乙酯和任选地0至10wt。％的额外的乙烯基共聚单体，其规定，根据ISO 11357-2，项目3.3.3，共聚物的玻璃化转变温度不高于60℃。本发明还涉及根据该方法生产的药物剂型，所述共聚物及其用途。

44. 发明申请

US20050065224A1 Macroporous material in the form of plastic pearls 失效
标题翻译：大孔材料以塑料珍珠的形式
公开(公告)号：US20050065224A1
公开(公告)日：2005-03-24
申请号：US10498971
申请日：2003-08-25
申请人： Stefan Menzler , Hans-Ulrich Petereit , Christian Meier , Thomas Boller , Thomas Suefke , Klaus Schultes , Roger Recktenwald
发明人： Stefan Menzler , Hans-Ulrich Petereit , Christian Meier , Thomas Boller , Thomas Suefke , Klaus Schultes , Roger Recktenwald
IPC分类号： C08F220/28 , C08F246/00 , C08J9/00 , C08F118/02
CPC分类号： C08F220/28 , C08F246/00 , Y10S530/815
摘要： The invention relates to a macroporous plastics bead material with an average particle diameter from 10 to 1000 μm, containing a copolymer of a) 5-60 wt. % vinylically polymerizable monomers with a water solubility of at least 1% at 20° C., b) 1-40 wt. % vinylically polymerizable monomers with an additional functional group, which can enter into covalent bonds with the nucleophilic groups of the ligands in a polymer-like reaction, c) 10-40 wt. % hydrophilic, crosslinking radical-polymerizable monomers with two or more ethylenically unsaturated polymerizable groups and d) 10-60 wt. % vinylically polymerizable monomers with a water solubility of at most 1% at 20° C. are contained, as a rule with the monomers a) to d) adding up to 100%.
摘要翻译：本发明涉及平均粒径为10-1000μm的大孔塑料珠粒材料，其含有a）5-60wt。％乙烯基聚合性单体，水溶性在20℃下至少为1％，b）1-40wt。具有另外的官能团的具有可与聚合物样反应中的配体的亲核基团共价键的乙烯基聚合性单体的％，c）10-40wt。具有两个或更多个烯属不饱和可聚合基团的亲水性交联自由基聚合单体，和d）10-60wt。在20℃下水溶解度最多为1％的％乙烯基聚合性单体的含量通常与单体a）至d）相加至100％。

45. 发明授权

US06632454B2 Multilayer pharmaceutical product for release in the colon 有权
标题翻译：多层药物在结肠中释放
公开(公告)号：US06632454B2
公开(公告)日：2003-10-14
申请号：US09926567
申请日：2001-11-19
申请人： Thomas Beckert , Hans-Ulrich Petereit , Vishal K. Gupta
发明人： Thomas Beckert , Hans-Ulrich Petereit , Vishal K. Gupta
IPC分类号： A61K958
CPC分类号： A61K9/5073 , A61K9/2846 , A61K9/2886 , A61K9/5026
摘要： The invention relates to the use of a multilayer pharmaceutical product that substantially comprises a) a core containing a pharmaceutically active substance, b) an inner coating consisting of a copolymer or a mixture of copolymers that are composed of 85 to 98 wt.- % of radically polymerized C1 to C4 alkyl esters of the acrylic or methacrylic acid and 15 to 2 wt.- % of (meth)acrylate monomers with a quaternary ammonium group in the alkyl group, and c) an outer coating consisting of a copolymer that is composed of 75 to 95 wt.- % of radically polymerized C1 to C4 alkyl esters of the acrylic or methacrylic acid and 5 to 25 wt.- % of (meth)acrylate monomers with an anionic group in the alkyl group. The inventive product is used for producing a pharmaceutical product that releases the active substance contained therein according to the USP release test, at pH 1.2 during 2 hours and subsequent rebuffering to pH 7.0, by less than 5% after 2.0 hours after start of the test and by 30 to 80% after eight hours after start of the test.
摘要翻译：本发明涉及多层药物产品的应用，其基本上包括a）含有药物活性物质的核心，b）由共聚物或共聚物混合物组成的内涂层，其由85-98wt。％的丙烯酸或甲基丙烯酸的自由基聚合的C1-C4烷基酯和在烷基中具有季铵基团的15至2重量％的（甲基）丙烯酸酯单体，和c）由共聚物组成的外涂层， 75至95重量％的丙烯酸或甲基丙烯酸的自由基聚合的C1至C4烷基酯和5至25重量％的在（甲基）丙烯酸烷基酯中具有阴离子基团的（甲基）丙烯酸酯单体。本发明产品用于生产一种药物产品，根据USP的释放试验，在pH2.2的时间内释放其中所含的活性物质，并在试验开始后的2.0小时内，随后的反渗透至pH 7.0，小于5％并且在开始测试后八小时后，再增加30到80％

46. 发明授权

US5708021A Debittered ranitidine preparation 失效
标题翻译：取代雷尼替丁制剂
公开(公告)号：US5708021A
公开(公告)日：1998-01-13
申请号：US574340
申请日：1995-12-18
申请人： Manfred Assmus , Hans-Ulrich Petereit
发明人： Manfred Assmus , Hans-Ulrich Petereit
IPC分类号： A61K9/08 , A61K9/00 , A61K31/34 , A61K47/32 , A61K47/48 , A61P1/00
CPC分类号： A61K9/0095 , A61K31/34 , A61K47/48176
摘要： Ranitidine salts with polycarboxylic acids, such as copolymers of acrylic and/or methacrylic acid with their lower alkyl esters, are water-soluble salts with a very reduced bitter taste. The salts are suitable as liquid gastritis preparations.
摘要翻译：与多羧酸的雷尼替丁盐如丙烯酸和/或甲基丙烯酸与其低级烷基酯的共聚物是具有非常降低的苦味的水溶性盐。这些盐适合作为液体胃炎制剂。

47. 发明授权

US5292522A Aqueous film coating agent for solid medicaments 失效
标题翻译：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。

48. 发明授权

US10113050B2 Powdery or granulated composition comprising a copolymer, a dicarboxylic acid and a fatty monocarboxylic acid 有权
公开(公告)号：US10113050B2
公开(公告)日：2018-10-30
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： 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).

49. 发明授权

US09597293B2 Solid dosage forms comprising an enteric coating with accelerated drug release 有权
公开(公告)号：US09597293B2
公开(公告)日：2017-03-21
申请号：US12598138
申请日：2007-05-07
申请人： Fang Liu , Abdul W. Basit , Rosario Lizio , Hans-Ulrich Petereit , Christian Meier , Michael Damm
发明人： Fang Liu , Abdul W. Basit , Rosario Lizio , Hans-Ulrich Petereit , Christian Meier , Michael Damm
IPC分类号： A61K9/32 , A61K47/12 , A61K47/32 , A61K47/34 , A61K47/38 , A61K9/50
CPC分类号： A61K9/5073 , A61K9/5026
摘要： The present invention provides a solid dosage form including an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating; wherein the inner coating includes a partially neutralized anionic polymeric material, and at least a carboxylic acid having 2 to 16 carbon atoms the salts thereof or mixtures of the acid and its salt; wherein the outer coating includes an anionic polymeric material which is less or not at all neutralized than the material of the inner coating.

50. 发明申请

US20110033530A1 COATING COMPOSITION FOR THE DIP COATING OF CAPSULE HALVES 有权
标题翻译：涂料组合物用于胶囊的浸涂
公开(公告)号：US20110033530A1
公开(公告)日：2011-02-10
申请号：US12845994
申请日：2010-07-29
申请人： Brigitte SKALSKY , Manfred Assmus , Odette Hensel , Hans-Ulrich Petereit
发明人： Brigitte SKALSKY , Manfred Assmus , Odette Hensel , Hans-Ulrich Petereit
IPC分类号： A61K9/48 , A61K47/32 , B05D5/00 , A23P1/08
CPC分类号： A23P1/04 , A23P10/30 , A61K9/4891 , A61K47/32
摘要： A coating composition for the enteric coating of capsule halves made of water-soluble or water-swellable polymer material in a dipping process is provided. The composition is an aqueous dispersion or solution, containing a polymer mixture of at least one first (meth)acrylate copolymer, which is enteric, and at least one further (meth)acrylate copolymer, which is enteric or water-insoluble, and also auxiliaries which influence the viscosity of the dispersion and the elasticity of the dried polymer film. The solids content of the dispersion or solution is more than 25% by weight and the viscosity is 150 to 1500 mPa·s and a dried film produced from the dispersion or solution has an elongation at break of at least 200%. Also provided is a capsule composed of two capsule halves coated with the dispersion or solution in a dipping process does. The enteric capsule does not dissolve in 0.1 N HCl at pH 1.2 after two hours, but completely dissolves in buffer at pH 6.8 in less than 30 minutes. A method to prepare enteric coated capsule halves is also provided.
摘要翻译：提供了一种用于在浸渍过程中由水溶性或水溶胀性聚合物材料制成的胶囊半部的肠溶衣涂料组合物。该组合物是含有至少一种肠溶性的至少一种第一（甲基）丙烯酸酯共聚物和至少一种其它（甲基）丙烯酸酯共聚物的聚合物混合物的水性分散体或溶液，其为肠溶或水不溶性的，以及辅助剂这影响了分散体的粘度和干燥的聚合物膜的弹性。分散体或溶液的固体成分大于25重量％，粘度为150〜1500mPa·s，由分散液或溶液制得的干燥膜的断裂伸长率为200％以上。还提供了由在浸渍过程中涂覆有分散体或溶液的两个胶囊半部组成的胶囊。肠溶胶囊在pH2.2后2小时内不溶于0.1N HCl，但在不到30分钟内完全溶于pH 6.8的缓冲液中。还提供了制备肠溶衣胶囊半部的方法。

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