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1. 发明授权

US08361506B2 Fast release dosage forms for antibiotics 有权
标题翻译：抗生素快速释放剂型
公开(公告)号：US08361506B2
公开(公告)日：2013-01-29
申请号：US11767228
申请日：2007-06-22
申请人： Iris Ziegler , Johannes Bartholomäus , Jessica Redmer
发明人： Iris Ziegler , Johannes Bartholomäus , Jessica Redmer
IPC分类号： A61K9/14 , A61K33/42
CPC分类号： A61K9/1623 , A61K9/0095 , A61K9/1611 , A61K9/1652 , A61K9/5026 , A61K9/5073 , A61K31/43 , A61K31/545 , A61K31/546 , A61K31/7048 , A61K31/7052
摘要： A multiparticulate, pharmaceutical dosage form containing at least one antibiotic which is sparingly wettable with aqueous media or sparingly soluble in aqueous media and a combination of carrageenan and tricalcium phosphate and optionally sucrose ester. Also, an administration system having this dosage form arranged in a drinking straw with at least one barrier device for single administration, optionally together with a conveying liquid.
摘要翻译：含有至少一种抗微生物剂的多颗粒药物剂型，其可用水性介质微溶或微溶于水性介质，以及角叉菜胶和磷酸三钙与任选的蔗糖酯的组合。此外，具有这种剂型的给药系统布置在具有至少一个用于单次给药的阻隔装置的饮用吸管中，任选地与输送液体一起。

2. 发明申请

US20120107250A1 ABUSE-PROOFED DOSAGE FORM 有权
标题翻译：避免使用的剂型
公开(公告)号：US20120107250A1
公开(公告)日：2012-05-03
申请号：US13346257
申请日：2012-01-09
申请人： Johannes Bartholomäus , Heinrich Kugelmann , Elisabeth Arkenau-Maric
发明人： Johannes Bartholomäus , Heinrich Kugelmann , Elisabeth Arkenau-Maric
IPC分类号： A61K31/135 , A61P25/00 , A61K31/485
CPC分类号： A61K31/135 , A61K9/0053 , A61K9/20 , A61K9/2013 , A61K9/2027 , A61K9/2031 , A61K9/205 , A61K9/2054 , A61K9/2068 , A61K9/2095 , A61K31/485 , A61K31/515 , A61K31/5513 , A61K47/10
摘要： An abuse-proofed, thermoformed dosage form containing, in addition to one or more active ingredients with abuse potential optionally together with physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N and to a process for the production thereof.
摘要翻译：除了一种或多种具有滥用潜力的活性成分，任选地与生理学上可接受的辅助物质一起，还包含至少一种具有至少500N的断裂强度的合成或天然聚合物，以及一种抗过氧化物其生产。

3. 发明申请

US20120059066A1 PHARMACEUTICAL SALTS 审中-公开
标题翻译：制药销售
公开(公告)号：US20120059066A1
公开(公告)日：2012-03-08
申请号：US13295242
申请日：2011-11-14
申请人： JOHANNES BARTHOLOMÄUS , Heinrich Kugelmann
发明人： JOHANNES BARTHOLOMÄUS , Heinrich Kugelmann
IPC分类号： A61K31/137 , C07C217/74 , A61P13/00 , A61K31/135 , A61P29/00 , C07C215/54 , C07C215/64
CPC分类号： C07C215/54 , A61K9/0056 , A61K9/0058 , A61K9/0095 , C07B2200/07 , C07C215/62 , C07C215/64 , C07C217/68 , C07C217/74 , C07C2601/14 , C07D275/06 , C07D291/06 , C07D489/04
摘要： The invention relates to pharmaceutical salts comprised of a pharmaceutical active substance and of at least one sugar substitute, to medicaments containing these salts, and to the use of these salts for producing medicaments.
摘要翻译：本发明涉及由药物活性物质和至少一种糖替代物组成的药物盐，含有这些盐的药物，以及这些盐用于制备药物的用途。

4. 发明申请

US20120039963A1 3-(2-Dimethlaminomethyl Cyclohexyl)Phenol Retard Formulation 审中-公开
标题翻译： 3-（2-二甲基氨基甲基环己基）酚酚制剂
公开(公告)号：US20120039963A1
公开(公告)日：2012-02-16
申请号：US13282005
申请日：2011-10-26
申请人： Tobias JUNG , Johannes BARTHOLOMÄUS
发明人： Tobias JUNG , Johannes BARTHOLOMÄUS
IPC分类号： A61K9/00 , A61K31/135 , A61P29/00 , C07C215/64
CPC分类号： A61K9/286 , A61K9/2018 , A61K9/2054 , A61K31/133 , A61K47/38 , A61K2300/00
摘要： A pharmaceutical dosage form for controlled release of the active substance 3-(2-dimethylaminomethylcyclohexyl)-phenol, preferably (1R,2R)-3-(2-dimethylaminomethylcyclohexyl)-phenol, or a pharmaceutically acceptable salt thereof, which dosage form (i) in vivo produces a peak plasma level of the active substance after 2 to 10 hours, and/or (ii) in vitro releases 3.0 to 37 percent by weight of the active substance originally contained in the dosage form after one-half hour, 5.0 to 56 percent by weight after one hour, 10 to 77 percent by weight after two hours, 15 to 88 percent by weight after 3 hours, at least 30 percent by weight after six hours, at least 50 percent by weight after 12 hours, at least 70 percent by weight after 18 hours, and at least 80 percent by weight after 24 hours when measured according to the European pharmacopoeia using a blade mixer in preferably 900 ml of a buffer solution at a pH value of 6.9, a temperature of 37° C., and 75 rpm.
摘要翻译：用于控制释放活性物质3-（2-二甲基氨基甲基环己基） - 苯酚的药物剂型，优选（1R，2R）-3-（2-二甲基氨基甲基环己基） - 苯酚或其药学上可接受的盐）在2至10小时后产生活性物质的峰值血浆水平，和/或（ii）体外释放半个小时后原始含有的活性物质的3.0至37重量％，5.0 1小时后的56重量％，2小时后10〜77重量％，3小时后15〜88重量％，6小时后至少30重量％，12小时后至少50重量％，12小时后至少50重量％ 18小时后至少70重量％，24小时后至少80重量％，根据欧洲药典使用叶片式混合器，优选900ml缓冲溶液，pH值为6.9，温度为37° C.和75rpm。

5. 发明授权

US10160719B2 Pharmaceutical salts 有权
公开(公告)号：US10160719B2
公开(公告)日：2018-12-25
申请号：US13295242
申请日：2011-11-14
申请人： Johannes Bartholomäus , Heinrich Kugelmann
发明人： Johannes Bartholomäus , Heinrich Kugelmann
IPC分类号： A61K31/137 , A61K31/135 , A61P13/00 , A61P29/00 , C07C215/54 , C07C215/64 , C07C217/74 , A61K9/00 , A61K9/68 , C07C215/62 , C07C217/68 , C07D275/06 , C07D291/06 , C07D489/04
摘要： The invention relates to pharmaceutical salts comprised of a pharmaceutical active substance and of at least one sugar substitute, to medicaments containing these salts, and to the use of these salts for producing medicaments.

6. 发明授权

US08323889B2 Process for the production of an abuse-proofed solid dosage form 有权
标题翻译：生产滥用防腐固体剂型的方法
公开(公告)号：US08323889B2
公开(公告)日：2012-12-04
申请号：US12140496
申请日：2008-06-17
申请人： Elisabeth Arkenau-Maric , Johannes Bartholomäus , Heinrich Kugelmann
发明人： Elisabeth Arkenau-Maric , Johannes Bartholomäus , Heinrich Kugelmann
IPC分类号： C12Q1/68 , A61K49/00
CPC分类号： A61K9/2095 , A61K9/1635
摘要： The present invention relates to a process for the production of an abuse-proofed solid dosage form containing at least one active ingredient with potential for abuse and a synthetic or natural polymer with a breaking strength of =500 N, characterized in that a corresponding mixture is processed by melt extrusion with the assistance of a planetary-gear extruder.
摘要翻译：本发明涉及生产含有至少一种具有滥用潜力的活性成分和具有= 500N的断裂强度的合成或天然聚合物的抗滥用固体剂型的方法，其特征在于相应的混合物为在行星齿轮挤出机的帮助下通过熔融挤出加工。

7. 发明申请

US20120065220A1 Tamper Resistant Dosage Form Comprising An Anionic Polymer 有权
标题翻译：包含阴离子聚合物的防篡改剂型
公开(公告)号：US20120065220A1
公开(公告)日：2012-03-15
申请号：US13223384
申请日：2011-09-01
申请人： Lutz BARNSCHEID , Sebastian SCHWIER , Johannes BARTHOLOMÄUS
发明人： Lutz BARNSCHEID , Sebastian SCHWIER , Johannes BARTHOLOMÄUS
IPC分类号： A61K31/485 , A61K31/135 , A61P25/04 , A61K47/34
CPC分类号： A61K9/2031 , A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2095 , A61K31/137
摘要： A pharmaceutical dosage form and method of using same, the pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, said dosage form containing a pharmacologically active ingredient (A); a physiologically acceptable polymer (B) obtainable by polymerization of a monomer composition comprising an ethylenically unsaturated monomer bearing an anionic functional group, in protonated form or a physiologically acceptable salt thereof; a polyalkylene oxide (C) having a weight average molecular weight of at least 200,000 g/mol, wherein the content of the polyalkylene oxide (C) is at least 20 wt.-%, based on the total weight of the dosage form; wherein the pharmacologically active ingredient (A) is present in a controlled-release matrix comprising the polymer (B) and the polyalkylene oxide (C).
摘要翻译：一种药物剂型及其使用方法，所述药物剂型具有至少500N的断裂强度，所述剂型含有药理活性成分（A）; 通过聚合包含具有阴离子官能团的烯属不饱和单体，质子化形式的单体组合物或其生理学上可接受的盐得到的生理上可接受的聚合物（B）重均分子量至少为200,000g / mol的聚环氧烷（C），其中聚环氧烷（C）的含量为至少20重量％，基于剂型的总重量; 其中药理活性成分（A）存在于包含聚合物（B）和聚环氧烷（C）的控释基质中。

8. 发明授权

US08114383B2 Abuse-proofed dosage form 有权
标题翻译：滥用药剂
公开(公告)号：US08114383B2
公开(公告)日：2012-02-14
申请号：US10718112
申请日：2003-11-20
申请人： Johannes Bartholomäus , Heinrich Kugelmann , Elisabeth Arkenau-Marić
发明人： Johannes Bartholomäus , Heinrich Kugelmann , Elisabeth Arkenau-Marić
IPC分类号： A61K49/00
CPC分类号： A61K31/135 , A61K9/0053 , A61K9/20 , A61K9/2013 , A61K9/2027 , A61K9/2031 , A61K9/205 , A61K9/2054 , A61K9/2068 , A61K9/2095 , A61K31/485 , A61K31/515 , A61K31/5513 , A61K47/10
摘要： The present invention relates to an abuse-proofed, thermoformed dosage form containing, in addition to one or more active ingredients with abuse potential optionally together with physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N and to a process for the production thereof.
摘要翻译：本发明涉及一种防滥用热成型剂型，除了一种或多种具有滥用潜力的活性成分以外，还含有生理上可接受的辅助物质，至少一种具有至少500N的断裂强度的合成或天然聚合物以及其生产方法。

9. 发明授权

US07776314B2 Abuse-proofed dosage system 有权
标题翻译：滥用药物剂量系统
公开(公告)号：US07776314B2
公开(公告)日：2010-08-17
申请号：US11007887
申请日：2004-12-09
申请人： Johannes Bartholomäus , Heinrich Kugelmann
发明人： Johannes Bartholomäus , Heinrich Kugelmann
IPC分类号： A61K49/00 , A61K9/48 , A61K9/20 , A61K9/14 , A61K9/16
CPC分类号： A61K9/2054 , A61K9/0053 , A61K9/2009 , A61K9/2013 , A61K9/205 , A61K9/4866 , A61K31/137 , A61K31/485 , A61K31/5513 , A61K45/06 , A61K47/38 , A61K2300/00
摘要： The invention relates to a solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid.
摘要翻译：本发明涉及一种固体给药形式，除了一种或多种具有肠胃外滥用潜力的活性物质外，还可防止肠胃外滥用，并含有至少一种增粘剂。基于从给药形式获得的提取物，当加入必要的最少量的含水液体时，该试剂形成当引入另一量的水性液体时保持视觉上不同的优选可注射的凝胶。

10. 发明授权

US09066888B2 Plaster causing reduced skin irritation 有权
标题翻译：石膏导致皮肤刺激性降低
公开(公告)号：US09066888B2
公开(公告)日：2015-06-30
申请号：US11509612
申请日：2006-08-25
申请人： Heinrich Kugelmann , Johannes Bartholomäus , Rasoul Sedaghat Kerdar
发明人： Heinrich Kugelmann , Johannes Bartholomäus , Rasoul Sedaghat Kerdar
IPC分类号： A61F13/00 , A61K9/70 , A61L15/44 , A61K47/34
CPC分类号： A61K9/7084 , A61F13/00 , A61F13/00063 , A61F2013/00387 , A61K47/34 , A61L15/44
摘要： A plaster containing an active ingredient for the transdermal administration of a pharmaceutical active ingredient, having a removable protective film and an adhesive layer. The plaster includes at least one compound that is contained in the adhesive layer or lies adjacent the adhesive layer between the adhesive layer and the removable protective film and that can be applied to the skin to at least reduce skin irritation.
摘要翻译：含有用于透皮给药药用活性成分的活性成分的石膏，其具有可除去的保护膜和粘合剂层。石膏包括至少一种化合物，其包含在粘合剂层中或邻近粘合剂层和可移除的保护膜之间的粘合剂层并且可以施用于皮肤以至少减少皮肤刺激。

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