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1. 发明申请

US20080050446A1 Fast Release Dosage Forms for Antibiotics 有权
标题翻译：快速释放抗生素剂型
公开(公告)号：US20080050446A1
公开(公告)日：2008-02-28
申请号：US11767228
申请日：2007-06-22
申请人： Iris Ziegler , Johannes Bartholomaeus , Jessica Redmer
发明人： Iris Ziegler , Johannes Bartholomaeus , Jessica Redmer
IPC分类号： A61K9/14 , A61K33/42 , A61P43/00
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。

3. 发明授权

US08722086B2 Dosage form with impeded abuse 有权
标题翻译：剂量形式与滥用滥用
公开(公告)号：US08722086B2
公开(公告)日：2014-05-13
申请号：US12044586
申请日：2008-03-07
申请人： Elisabeth Arkenau-Marić , Johannes Bartholomaeus , Iris Ziegler , Marcel Haupts
发明人： Elisabeth Arkenau-Marić , Johannes Bartholomaeus , Iris Ziegler , Marcel Haupts
IPC分类号： A61K9/20 , A61K9/50 , A61K9/16
CPC分类号： A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/4808 , A61K9/4866 , A61K31/137
摘要： A multiparticulate dosage form formulated to make misuse more difficult containing least one active substance with potential for misuse (A), at least one synthetic or natural polymer (C), optionally at least one natural, semi-synthetic or synthetic wax (D), at least one disintegrant (E) and optionally one or more additional physiologically compatible excipients (B), wherein the individual particles of the dosage form display a breaking strength of at least 500 N and a release of active substance of at least 75% after 45 minutes measured according to Ph.Eur. in the paddle mixer with sinker in 600 ml of aqueous buffer solution with a pH value of 1.2 at 37° C. and 75 rpm.
摘要翻译：配制成使滥用更加困难的多颗粒剂型，其含有至少一种具有误用潜力（A）的活性物质，至少一种合成或天然聚合物（C），任选至少一种天然的，半合成的或合成的蜡（D），至少一种崩解剂（E）和任选的一种或多种另外的生理相容性赋形剂（B），其中剂型的各个颗粒在45以后显示出至少500N的断裂强度和至少75％的活性物质释放分钟根据Ph.Eur测量。在具有沉降片的桨式混合器中，在37℃和75rpm下，pH值为1.2的600ml缓冲水溶液中。

4. 发明申请

US20050136110A1 Delayed release pharmaceutical composition containing 1-dimethy-lamino-3(3-methoxyl-phenyl)-2-methyl-pentan-3-ol 失效
标题翻译：含有1-二甲基 - 氨基-3（3-甲氧基 - 苯基）-2-甲基 - 戊-3-醇的延迟释放药物组合物
公开(公告)号：US20050136110A1
公开(公告)日：2005-06-23
申请号：US10998159
申请日：2004-11-29
申请人： Johannes Bartholomaeus , Iris Ziegler
发明人： Johannes Bartholomaeus , Iris Ziegler
IPC分类号： A61K9/20 , A61K31/13 , A61K31/138 , A61K9/22
CPC分类号： A61K31/13 , A61K9/2054
摘要： A delayed release pharmaceutical formulation containing 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol or a pharmaceutically acceptable salt thereof in a matrix; said matrix containing from 1 to 80 wt. % of at least one pharmaceutically acceptable, matrix-forming, hydrophilic or hydrophobic polymer and having the following in vitro dissolution rate relative to 100 wt. % of the 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol contained in the formulation: 3-35 wt. % released after 0.5 hour, 5-50 wt. % released after 1 hour, 10-75 wt. % released after 2 hours, 15-82 wt. % released after 3 hours, 30-97 wt. % released after 6 hours, more than 50 wt. % released after 12 hours, more than 70 wt. % released after 18 hours, and more than 80 wt. % released after 24 hours.
摘要翻译：含有1-二甲基氨基-3-（3-甲氧基苯基）-2-甲基戊-3-醇或其药学上可接受的盐的基质中的延迟释放药物制剂; 所述基质含有1至80wt。至少一种药学上可接受的，基质形成的，亲水的或疏水的聚合物的％，并且相对于100重量％具有以下体外溶出速率。制剂中所含的1-二甲基氨基-3-（3-甲氧基苯基）-2-甲基戊-3-醇的％：3-35重量％ 0.5小时后释放％，5-50重量％ 1小时后释放％，10-75重量％ 2小时后释放％，15-82wt。 3小时后释放％，30-97重量％ 6小时后释放％，超过50重量％ 12小时后释放％，超过70wt。 18小时后释放％，超过80重量％。 24小时后释放％。

5. 发明申请

US20050003002A1 Sustained-release, oral pharmaceutical formulations and methods of making and using same 失效
标题翻译：持续释放，口服药物制剂及其制备和使用方法
公开(公告)号：US20050003002A1
公开(公告)日：2005-01-06
申请号：US10837755
申请日：2004-05-04
申请人： Iris Ziegler , Johannes Bartholomaeus
发明人： Iris Ziegler , Johannes Bartholomaeus
IPC分类号： A61K9/16 , A61K9/20 , A61K9/22 , A61K9/28 , A61K9/30 , A61K9/50 , A61K9/52 , A61K31/135 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/428 , A61K31/60 , A61K31/616 , A61K47/12 , A61K47/20 , A61K47/22 , A61P1/04 , A61P1/12 , A61P9/00 , A61P11/00 , A61P11/14 , A61P13/00 , A61P13/02 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/24 , A61P25/30 , A61P25/32 , A61P25/36 , A61P29/00 , A61P37/08 , A61K9/00 , A61K31/137
CPC分类号： A61K31/19 , A61K9/1617 , A61K9/1623 , A61K9/1652 , A61K9/2081 , A61K9/2846 , A61K9/5015 , A61K9/5026 , A61K9/5047 , A61K31/135 , A61K31/137 , A61K31/195 , A61K31/196 , A61K31/428 , A61K31/60 , A61K2300/00
摘要： A sustained-release, oral pharmaceutical formulation of tramadol comprising a compound formed in situ of tramadol or a tramadol salt and a pharmaceutically acceptable acidic substance. The compound formed in situ has a desired water solubility. Also provided are methods of treatment using the pharmaceutical formulations. Method for preparing such formulations are also provided. The preparation method comprises repeatedly mixing tramadol or its salt with the acidic substance, and moistening the mixture and formulating the mixture under an energy input, such as heat or pressure. Optionally, drying, repeated granulating, extrudation and pelleting may also be included.
摘要翻译：曲马多的缓释口服药物制剂，其包含由曲马多或曲马多盐和药学上可接受的酸性物质原位形成的化合物。原位形成的化合物具有所需的水溶性。还提供了使用药物制剂的治疗方法。还提供了制备这些制剂的方法。制备方法包括将曲马多或其盐与酸性物质重复混合，并在能量输入如热或压力下润湿混合物并配制该混合物。任选地，还可以包括干燥，重复造粒，挤出和造粒。

6. 发明授权

US08173164B2 Oral administration forms for administering a fixed tramadol and diclofenac combination 失效
标题翻译：用于施用固定的曲马多和双氯芬酸组合的口服给药形式
公开(公告)号：US08173164B2
公开(公告)日：2012-05-08
申请号：US10665552
申请日：2003-09-22
申请人： Johannes Bartholomaeus , Iris Ziegler
发明人： Johannes Bartholomaeus , Iris Ziegler
IPC分类号： A61K9/14 , A61K9/20 , A61K9/48
CPC分类号： A61K9/5084 , A61K9/1652 , A61K9/5026 , A61K9/5036 , A61K31/195 , A61K2300/00
摘要： An oral administration unit containing the active substances Tramadol and Diclofenac and/or physiologically acceptable salts thereof, in which both active substances are contained in the same administration unit as two separately formulated subunits.
摘要翻译：含有活性物质曲马多和双氯芬酸的口服给药单元和/或其生理学上可接受的盐，其中两种活性物质都包含在与两个单独配制的亚基相同的给药单位中。

7. 发明申请

US20120034304A1 Prolonged Release Pharmaceutical Composition Containing 3-(3-Dimethylamino-1-Ethyl-2-Methyl-Propyl)Phenol 审中-公开
标题翻译：含有3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚的长期释放药物组合物
公开(公告)号：US20120034304A1
公开(公告)日：2012-02-09
申请号：US13242800
申请日：2011-09-23
申请人： Johannes BARTHOLOMAEUS , Iris Ziegler
发明人： Johannes BARTHOLOMAEUS , Iris Ziegler
IPC分类号： A61K9/00 , A61P25/00 , A61K31/135
CPC分类号： A61K31/137 , A61K9/0053 , A61K9/2054 , A61K9/5047 , A61K31/135 , A61K31/136
摘要： A pharmaceutical formulation for prolonged release of the active ingredient 3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol or a pharmaceutically acceptable salt thereof in a matrix containing between 1 and 80 wt. % of at least one pharmaceutically acceptable hydrophilic or hydrophobic polymer as a matrix forming agent and exhibiting in vivo the following release rate: 3 to 35% by weight (based on 100% by weight active ingredient) 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 0.5 hours; 5 to 50% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 1 hour; 10 to 75% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 2 hours; 15 to 82% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 3 hours; 30 to 97% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 6 hours; more than 50% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 12 hours; more than 70% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 18 hours, and more than 80% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 24 hours.
摘要翻译：一种药物制剂，用于将活性成分3-（3-二甲基氨基-1-乙基-2-甲基丙基）苯酚或其药学上可接受的盐在含有1-80重量％％至少一种药学上可接受的亲水或疏水性聚合物作为基质形成剂，并且体内呈现以下释放速率：3-35重量％（基于100重量％活性成分）3-（3-二甲基氨基-1- 乙基-2-甲基 - 丙基）酚在0.5小时后释放; 1小时后，5〜50重量％的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚释放出来; 在2小时后释放10〜75重量％的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚; 在3小时后释放出15〜82重量％的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚; 6小时后释放30〜97重量％的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚; 12小时后释放出大于50重量％的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚; 18小时后释放的70重量％以上的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚和大于80重量％的3-（3-二甲基氨基-1-乙基-2-甲基丙基）苯酚在24小时后释放。

8. 发明授权

US07572463B2 Oral dosage forms 失效
公开(公告)号：US07572463B2
公开(公告)日：2009-08-11
申请号：US10084674
申请日：2002-02-28
申请人： Johannes Bartholomaeus , Iris Ziegler
发明人： Johannes Bartholomaeus , Iris Ziegler
IPC分类号： A61K9/22
CPC分类号： C07D275/06 , A61K9/0056 , A61K9/0058 , A61K9/0095 , A61K9/1652 , A61K9/2054 , A61K9/2081 , A61K9/2846 , A61K9/5015 , A61K9/5026 , A61K9/5047 , A61K31/135 , A61K31/137 , A61K31/19 , A61K31/195 , A61K31/205 , A61K31/428 , A61K31/54 , A61K31/60 , C07C217/74 , C07C307/02 , C07C2601/14 , C07D291/06 , A61K2300/00
摘要： A controlled-release oral dosage formulation of a salt-forming active ingredient, wherein the active ingredient is present as at least two different salts in a solid aggregation state, wherein the two different salts have different water solubility and release the active ingredient in-vitro at different release rates, provided that oral dosage formulations are excluded which comprise a resin carrying a sulfonate group and a resin carrying a carboxyl group and which contain an active ingredient in a form fixed to these resins.

9. 发明申请

US20090004267A1 Dosage Form with Impeded Abuse 有权
标题翻译：滥用药物的剂量
公开(公告)号：US20090004267A1
公开(公告)日：2009-01-01
申请号：US12044586
申请日：2008-03-07
申请人： Elisabeth Arkenau-Maric , Johannes Bartholomaeus , Iris Ziegler , Marcel Haupts
发明人： Elisabeth Arkenau-Maric , Johannes Bartholomaeus , Iris Ziegler , Marcel Haupts
IPC分类号： A61K9/20 , A61K9/14
CPC分类号： A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/4808 , A61K9/4866 , A61K31/137
摘要： A multiparticulate dosage form formulated to make misuse more difficult containing least one active substance with potential for misuse (A), at least one synthetic or natural polymer (C), optionally at least one natural, semi-synthetic or synthetic wax (D), at least one disintegrant (E) and optionally one or more additional physiologically compatible excipients (B), wherein the individual particles of the dosage form display a breaking strength of at least 500 N and a release of active substance of at least 75% after 45 minutes measured according to Ph.Eur. in the paddle mixer with sinker in 600 ml of aqueous buffer solution with a pH value of 1.2 at 37° C. and 75 rpm.
摘要翻译：配制成使滥用更加困难的多颗粒剂型，其含有至少一种具有误用潜力（A）的活性物质，至少一种合成或天然聚合物（C），任选至少一种天然的，半合成的或合成的蜡（D），至少一种崩解剂（E）和任选的一种或多种另外的生理相容性赋形剂（B），其中剂型的各个颗粒在45以后显示出至少500N的断裂强度和至少75％的活性物质释放分钟根据Ph.Eur测量。在具有沉降片的桨式混合器中，在37℃和75rpm下，pH值为1.2的600ml缓冲水溶液中。

10. 发明申请

US20050058706A1 Delayed release pharmaceutical composition containing 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol 审中-公开
标题翻译：含有3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚的延迟释放药物组合物
公开(公告)号：US20050058706A1
公开(公告)日：2005-03-17
申请号：US10831368
申请日：2004-04-26
申请人： Johannes Bartholomaeus , Iris Ziegler
发明人： Johannes Bartholomaeus , Iris Ziegler
IPC分类号： A61K47/30 , A61K9/20 , A61K9/22 , A61K9/50 , A61K31/135 , A61K31/136 , A61K31/137 , A61K47/38 , A61P25/04
CPC分类号： A61K31/137 , A61K9/0053 , A61K9/2054 , A61K9/5047 , A61K31/135 , A61K31/136
摘要： A pharmaceutical formulation for delayed release of the active ingredient 3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol or a pharmaceutically acceptable salt thereof in a matrix containing between 1 and 80 wt. % of at least one pharmaceutically acceptable hydrophilic or hydrophobic polymer as a matrix forming agent and exhibiting in vivo the following release rate: 3 to 35% by weight (based on 100% by weight active ingredient) 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 0.5 hours; 5 to 50% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 1 hour; 10 to 75% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 2 hours; 15 to 82% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 3 hours; 30 to 97% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 6 hours; more than 50% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 12 hours; more than 70% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 18 hours, and more than 80% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 24 hours.
摘要翻译：用于将活性成分3-（3-二甲基氨基-1-乙基-2-甲基丙基）苯酚或其药学上可接受的盐延迟释放在含有1-80重量％％至少一种药学上可接受的亲水或疏水性聚合物作为基质形成剂，并且体内呈现以下释放速率：3-35重量％（基于100重量％活性成分）3-（3-二甲基氨基-1- 乙基-2-甲基 - 丙基）酚在0.5小时后释放; 1小时后，5〜50重量％的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚释放出来; 在2小时后释放10〜75重量％的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚; 在3小时后释放出15〜82重量％的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚; 6小时后释放30〜97重量％的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚; 12小时后释放出大于50重量％的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚; 18小时后释放的70重量％以上的3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基）苯酚和大于80重量％的3-（3-二甲基氨基-1-乙基-2-甲基丙基）苯酚在24小时后释放。

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