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1. 发明申请

US20080206324A1 PELLETS HAVING AN ACTIVE COMPOUND MATRIX AND A POLYMER COATING, AND A PROCESS FOR THE PRODUCTION OF THE PELLETS 审中-公开
标题翻译：具有活性化合物基质和聚合物涂料的片剂以及生产小片剂的方法
公开(公告)号：US20080206324A1
公开(公告)日：2008-08-28
申请号：US12030377
申请日：2008-02-13
申请人： Andreas Gryczke , Hans-Ulrich Petereit , Christian Meier , Kathrin Nollenberger , Christian Brunnengraber , Andreas Klosendorf , Reinhard Menzel
发明人： Andreas Gryczke , Hans-Ulrich Petereit , Christian Meier , Kathrin Nollenberger , Christian Brunnengraber , Andreas Klosendorf , Reinhard Menzel
IPC分类号： A61K9/48 , A61K9/14 , A61K9/32
CPC分类号： A61K9/1635 , A61K9/5026 , A61K31/52
摘要： An active compound-containing pellet has a polymer coating of an anionic (meth)acrylate copolymer and a pharmaceutically active substance, embedded in a polymer matrix of one or more polymers, a particle size in the range from 300 to 1100 μm, a friability of at most 0.1%, measured using 200 g of pellets in a screening machine having a 200 μm screen, a screening diameter of 20 cm and 1.5 mm shaking amplitude at a shaking frequency of 50 l/sec for 10 min in the presence of six rubber cubes having a 1.8 cm edge length, with the proviso that the pellet releases no more than 10% of the active compound in a release test according to USP in artificial gastric juice at pH 1.2 after 120 min.
摘要翻译：含活性化合物的颗粒具有嵌入在一种或多种聚合物的聚合物基质中的阴离子（甲基）丙烯酸酯共聚物和药物活性物质的聚合物涂层，粒度在300至1100μm的范围内，脆性在具有200μm筛网的筛选机中使用200g粒料测量，至少0.1％，筛选直径为20cm和1.5mm，振荡频率为50l / sec，在六个橡胶存在下摇动10分钟具有1.8厘米边缘长度的立方体，条件是在120分钟后pH 1.2的人造胃液中，根据USP的释放试验中，颗粒释放不超过10％的活性化合物。

2. 发明申请

US20130071475A1 Method For Producing An Oral Pharmaceutical Form With Immediate Disintegration And Active Ingredient Release 审中-公开
标题翻译：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。

3. 发明申请

US20050197434A9 Granulate or powder for producing coating or binding agents for medicaments 有权
标题翻译：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。

4. 发明授权

US09050256B2 Oral dosage form, comprising at least one biologically active agent, formulation auxiliary substances and magnetizable particles 有权
标题翻译：口服剂型，包含至少一种生物活性剂，制剂辅助物质和可磁化颗粒
公开(公告)号：US09050256B2
公开(公告)日：2015-06-09
申请号：US13390353
申请日：2010-08-30
申请人： Benedikt Hartwig , Norbert Windhab , Melanie Liefke , Juan Tome Alcalde , Michael Damm , Rosario Lizio , Michael Gottschalk , Angela Olf , Christian Meier , Andreas Gryczke
发明人： Benedikt Hartwig , Norbert Windhab , Melanie Liefke , Juan Tome Alcalde , Michael Damm , Rosario Lizio , Michael Gottschalk , Angela Olf , Christian Meier , Andreas Gryczke
IPC分类号： A61B5/055 , A61K9/20 , A61K9/28 , A61K9/48 , A61K9/50 , A61K9/00
CPC分类号： A61K9/2072 , A61K9/0009 , A61K9/0053 , A61K9/2095 , A61K9/2813 , A61K9/2846 , A61K9/2866 , A61K9/4808 , A61K9/4816 , A61K9/4833 , A61K9/4883 , A61K9/5094
摘要： The invention relates to an oral dosage form, comprising at least one biologically active agent, formulation auxiliary substances and magnetizable particles, wherein the dosage form has an at least two phase composition, wherein the phases can dissolve in the body after oral administration due to their formulation and the magnetizable particles are bound in formulation auxiliary substances and are present in a magnetized state, wherein the magnetized particles are present in at least two phases of the dosage form and generate magnetic fields, wherein these phases dissolve at different times in the body after oral administration, and wherein the magnetic field strength with respect to time, position and movement in the body is acquired using a detection system and can be evaluated using a computer-based evaluation system.
摘要翻译：本发明涉及口服剂型，其包含至少一种生物活性剂，制剂辅助物质和可磁化颗粒，其中所述剂型具有至少两相组合物，其中所述相可以在口服给药后溶于体内，因为它们制剂和可磁化颗粒结合在制剂辅助物质中并以磁化状态存在，其中磁化颗粒存在于剂型的至少两个相中并产生磁场，其中这些相在体内不同时间溶解在体内并且其中使用检测系统获取相对于身体中的时间，位置和运动的磁场强度，并且可以使用基于计算机的评估系统进行评估。

5. 发明申请

US20080206350A1 PELLETS HAVING A GASTRIC JUICE-RESISTANT ACTIVE COMPOUND MATRIX 有权
标题翻译：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。

6. 发明授权

US08642089B2 Melt extrusion of salts of active ingredients 有权
标题翻译：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。

7. 发明申请

US20130142877A1 PHARMACEUTICAL DOSAGE FORM COMPRISING ONE OR MORE ANTIRETROVIRAL ACTIVE INGREDIENTS 审中-公开
标题翻译：包含一种或多种抗血小板活性成分的药物剂型
公开(公告)号：US20130142877A1
公开(公告)日：2013-06-06
申请号：US13696746
申请日：2011-03-03
申请人： Pravin Nalawade , Smitha Shetty , Hema Ravishankar , Shripad Gadhinglajkar , Andreas Gryczke , Hans-Ulrich Petereit , Kathrin Nollenberger
发明人： Pravin Nalawade , Smitha Shetty , Hema Ravishankar , Shripad Gadhinglajkar , Andreas Gryczke , Hans-Ulrich Petereit , Kathrin Nollenberger
IPC分类号： A61K47/32 , A61K31/427 , A61K31/513
CPC分类号： A61K31/513 , A61K9/145 , A61K9/146 , A61K9/1635 , A61K9/4866 , A61K31/427
摘要： The invention relates to a pharmaceutical dosage form comprising one or more antiretroviral active ingredients in the form of a solid dispersion or solid solution in a matrix, wherein said matrix comprises an amino(meth)acrylate copolymer, characterized in that the matrix does not contain any essential amounts of pharmaceutically acceptable surfactants with an HLB value from 12 to 18 and in that the matrix comprises a mono carboxylic acid or an alcohol with 12 to 22 carbon atoms or both.
摘要翻译：本发明涉及药物剂型，其包含一种或多种基质中固体分散体或固体溶液形式的抗逆转录病毒活性成分，其中所述基质包含氨基（甲基）丙烯酸酯共聚物，其特征在于所述基质不含任何必需量的HLB值为12至18的药学上可接受的表面活性剂，并且基质包含单羧酸或具有12至22个碳原子的醇或两者。

8. 发明授权

US08216613B2 Pellets having a gastric juice-resistant active compound matrix 有权
标题翻译：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。

9. 发明授权

US08343542B2 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.

10. 发明申请

US20120143039A1 ORAL DOSAGE FORM, COMPRISING AT LEAST ONE BIOLOGICALLY ACTIVE AGENT, FORMULATION AUXILIARY SUBSTANCES AND MAGNETIZABLE PARTICLES 有权
标题翻译：口服剂型，包含至少一种生物活性剂，配方辅助物质和可磁化颗粒
公开(公告)号：US20120143039A1
公开(公告)日：2012-06-07
申请号：US13390353
申请日：2010-08-30
申请人： Benedikt Hartwig , Norbert Windhab , Melanie Liefke , Juan Tome Alcalde , Michael Damm , Rosario Lizio , Michael Gottschalk , Angela Olf , Christian Meier , Andreas Gryczke
发明人： Benedikt Hartwig , Norbert Windhab , Melanie Liefke , Juan Tome Alcalde , Michael Damm , Rosario Lizio , Michael Gottschalk , Angela Olf , Christian Meier , Andreas Gryczke
IPC分类号： A61B5/05 , A61J3/07
CPC分类号： A61K9/2072 , A61K9/0009 , A61K9/0053 , A61K9/2095 , A61K9/2813 , A61K9/2846 , A61K9/2866 , A61K9/4808 , A61K9/4816 , A61K9/4833 , A61K9/4883 , A61K9/5094
摘要： The invention relates to an oral dosage form, comprising at least one biologically active agent, formulation auxiliary substances and magnetizable particles, wherein the dosage form has an at least two phase composition, wherein the phases can dissolve in the body after oral administration due to their formulation and the magnetizable particles are bound in formulation auxiliary substances and are present in a magnetized state, wherein the magnetized particles are present in at least two phases of the dosage form and generate magnetic fields, wherein these phases dissolve at different times in the body after oral administration, and wherein the magnetic field strength with respect to time, position and movement in the body is acquired using a detection system and can be evaluated using a computer-based evaluation system.
摘要翻译：本发明涉及口服剂型，其包含至少一种生物活性剂，制剂辅助物质和可磁化颗粒，其中所述剂型具有至少两相组合物，其中所述相可以在口服给药后溶于体内，因为它们制剂和可磁化颗粒结合在制剂辅助物质中并以磁化状态存在，其中磁化颗粒存在于剂型的至少两个相中并产生磁场，其中这些相在体内不同时间溶解在体内并且其中使用检测系统获取相对于身体中的时间，位置和运动的磁场强度，并且可以使用基于计算机的评估系统进行评估。

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