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1. 发明申请

US20080292685A1 Transdermal Patch Containing Isosorbide Dinitrate and Bisoprolol 有权
标题翻译：含有硝酸异山梨酯和比索洛尔的透皮贴剂
公开(公告)号：US20080292685A1
公开(公告)日：2008-11-27
申请号：US12096545
申请日：2005-12-09
申请人： Shuming Wang , Li Wang , Xiaoling Fan , Huiyong Xue , Shuang Zhang , Enhong Zhang , Xuying Zhong , Yucheng Lu , Chun Li , Li Song
发明人： Shuming Wang , Li Wang , Xiaoling Fan , Huiyong Xue , Shuang Zhang , Enhong Zhang , Xuying Zhong , Yucheng Lu , Chun Li , Li Song
IPC分类号： A61K9/70 , A61K31/343 , A61P9/00
CPC分类号： A61K9/7061 , A61K31/138 , A61K31/724
摘要： This invention relates to a transdermal patch in the form of a layer complex, comprising a backing layer, a drug-reservoir layer comprising pharmacologically active ingredients and pharmaceutically acceptable adjuvants, and a release liner covering the drug-reservoir layer, characterized in that the drug-reservoir layer comprises isosorbide dinitrate and Bisoprolol at a ratio of 1:3 to 3:1 by weight, as the pharmacologically active ingredients. Animal tests show that said patch can reduce the elevation of T wave of cardiogram, the increase of the level of myocardial enzyme in blood serum, and the extension of the range of myocardial infarction caused by ligating the coronary artery in animals. Results show that said patch exhibits a considerable synergistic effect in the treatment of cardiovascular diseases and has good preventive and therapeutic effects on several adverse events on heart. In addition, the animal tests show that the patch according to the invention has a better pressure-reducing effect than the application of the patch containing only one of isosorbide dinitrate and Bisoprolol, and does not worsen the arrhythmia that is easily caused by the application of the patch containing only isosorbide dinitrate or Bisoprolol.
摘要翻译：本发明涉及层复合物形式的透皮贴剂，其包含背衬层，包含药理活性成分和药学上可接受的佐剂的药物储库层，以及覆盖药物储库层的释放衬垫，其特征在于药物作为药理活性成分，含有硝酸异山梨酯和比索洛尔，比例为1:3〜3:1。动物试验表明，所述贴片可以降低心电图T波的升高，血清中心肌酶水平的升高，以及通过在动物中连接冠状动脉引起的心肌梗塞范围的延长。结果表明，所述贴片在治疗心血管疾病方面具有相当大的协同效应，对心脏上的几种不良事件具有良好的预防和治疗作用。此外，动物试验表明，根据本发明的贴剂具有比仅含有硝酸异山梨酯和比洛维罗之一的贴剂的施用更好的减压效果，并且不会使应用容易引起的心律失常恶化该补丁仅含有硝酸异山梨酯或比索洛尔。

2. 发明授权

US08071125B2 Transdermal patch containing isosorbide dinitrate and bisoprolol 有权
标题翻译：透皮贴剂含有硝酸异山梨酯和比索洛尔
公开(公告)号：US08071125B2
公开(公告)日：2011-12-06
申请号：US12096545
申请日：2005-12-09
申请人： Shuming Wang , Li Wang , Xiaoling Fan , Huiyong Xue , Shuang Zhang , Enhong Zhang , Xuying Zhong , Yucheng Lu , Chun Li , Li Song
发明人： Shuming Wang , Li Wang , Xiaoling Fan , Huiyong Xue , Shuang Zhang , Enhong Zhang , Xuying Zhong , Yucheng Lu , Chun Li , Li Song
IPC分类号： A61F13/00
CPC分类号： A61K9/7061 , A61K31/138 , A61K31/724
摘要： This invention relates to a transdermal patch in the form of a layer complex, comprising a backing layer, a drug-reservoir layer comprising pharmacologically active ingredients and pharmaceutically acceptable adjuvants, and a release liner covering the drug-reservoir layer, characterized in that the drug-reservoir layer comprises isosorbide dinitrate and Bisoprolol at a ratio of 1:3 to 3:1 by weight, as the pharmacologically active ingredients. Animal tests show that said patch can reduce the elevation of T wave of cardiogram, the increase of the level of myocardial enzyme in blood serum, and the extension of the range of myocardial infarction caused by ligating the coronary artery in animals. Results show that said patch exhibits a considerable synergistic effect in the treatment of cardiovascular diseases and has good preventive and therapeutic effects on several adverse events on heart. In addition, the animal tests show that the patch according to the invention has a better pressure-reducing effect than the application of the patch containing only one of isosorbide dinitrate and Bisoprolol, and does not worsen the arrhythmia that is easily caused by the application of the patch containing only isosorbide dinitrate or Bisoprolol.
摘要翻译：本发明涉及层复合物形式的透皮贴剂，其包含背衬层，包含药理活性成分和药学上可接受的佐剂的药物储库层，以及覆盖药物储库层的释放衬垫，其特征在于药物作为药理活性成分，含有硝酸异山梨酯和比索洛尔，比例为1:3〜3:1。动物试验表明，所述贴片可以降低心电图T波的升高，血清中心肌酶水平的升高，以及通过在动物中连接冠状动脉引起的心肌梗塞范围的延长。结果表明，所述贴片在治疗心血管疾病方面具有相当大的协同效应，对心脏上的几种不良事件具有良好的预防和治疗作用。此外，动物试验表明，根据本发明的贴剂具有比仅含有硝酸异山梨酯和比洛维罗之一的贴剂的施用更好的减压效果，并且不会使应用容易引起的心律失常恶化该补丁仅含有硝酸异山梨酯或比索洛尔。

3. 发明授权

US09265752B2 Transdermal patch containing Rotigotine 有权
标题翻译：含有罗替高汀的透皮贴剂
公开(公告)号：US09265752B2
公开(公告)日：2016-02-23
申请号：US12667915
申请日：2008-07-03
申请人： Shuming Wang , Huiyong Xue , Li Wang , Enhong Zhang , Hongjun Lian , Xiaoyan Shi , Guohua Chi , Yucheng Lu , Xiquan Liu , Li Song , Xuying Zhong , Hongguang Du
发明人： Shuming Wang , Huiyong Xue , Li Wang , Enhong Zhang , Hongjun Lian , Xiaoyan Shi , Guohua Chi , Yucheng Lu , Xiquan Liu , Li Song , Xuying Zhong , Hongguang Du
IPC分类号： A61K9/70 , A61K31/381 , A61P25/16
CPC分类号： A61K9/7023 , A61K9/7053 , A61K9/7061 , A61K9/7069 , A61K31/381
摘要： A Rotigotine-containing composition having a matrix mixture system formed from a polyvinylpyrrolidone and a combination of an acrylic pressure-sensitive adhesive with a silicone pressure-sensitive adhesive. The polyvinylpyrrolidone may be present in an amount of about 1-10% by weight in matrix mixture system. The acrylic pressure-sensitive adhesive may be present in an amount of about 1-25% by weight in the matrix mixture system. The silicone pressure-sensitive adhesive may be present in an amount of about 65-98% by weight in the matrix mixture system. The composition further includes 1-40% of Rotigotine on the basis of the total weight of the composition. The composition provides improved properties in the solubility, release and initial penetration level of Rotigotine. Also disclosed is a transdermal patch that includes the Rotigotine-containing composition, as well as methods of manufacturing and using the Rotigotine-containing composition.
摘要翻译：一种含有罗替那定的组合物，其具有由聚乙烯吡咯烷酮形成的基质混合物体系和丙烯酸类压敏粘合剂与硅氧烷压敏粘合剂的组合。聚乙烯吡咯烷酮的存在量可以在基质混合体系中约1-10％（重量）。丙烯酸类压敏粘合剂可以在基质混合物体系中以约1-25重量％的量存在。在基质混合物体系中，硅氧烷压敏粘合剂可以以约65-98重量％的量存在。该组合物还包括基于组合物总重量的1-40％的罗替戈汀。该组合物提供了罗替戈汀的溶解度，释放和初始渗透水平的改善的性质。还公开了包括含有罗替多汀的组合物的透皮贴剂，以及制造和使用含有罗替尼汀的组合物的方法。

4. 发明申请

US20110027345A1 COMPOSITION CONTAINING ROTIGOTINE AND USE THEREOF AND TRANSDERMAL PATCH CONTAINING THE COMPOSITION 有权
标题翻译：含有ROTIGOTINE的组合物及其用途及含有组合物的透皮贴剂
公开(公告)号：US20110027345A1
公开(公告)日：2011-02-03
申请号：US12667915
申请日：2008-07-03
申请人： Shuming Wang , Huiyong Xue , Li Wang , Enhong Zhang , Hongjun Lian , Xiaoyan Shi , Guohua Chi , Yucheng Lu , Xiquan Liu , Li Song , Xuying Zhong , Hongguang Du
发明人： Shuming Wang , Huiyong Xue , Li Wang , Enhong Zhang , Hongjun Lian , Xiaoyan Shi , Guohua Chi , Yucheng Lu , Xiquan Liu , Li Song , Xuying Zhong , Hongguang Du
IPC分类号： A61K31/381 , A61K9/00 , A61K9/70 , A61P25/16
CPC分类号： A61K9/7023 , A61K9/7053 , A61K9/7061 , A61K9/7069 , A61K31/381
摘要： The present invention relates to a composition containing Rotigotine and the use thereof in the manufacture of a Rotigotine-containing transdermal patch, wherein said composition is based on a matrix mixture system formed from a combination of an acrylic pressure-sensitive adhesive with a silicone pressure-sensitive adhesive, and polyvinylpyrrolidone which are present in a particular weight ratio, wherein (1) the acrylic pressure-sensitive adhesive is present in an amount of about 1-25% by weight in the matrix mixture system, (2) the silicone pressure-sensitive adhesive is present in an amount of about 65-98% by weight in the matrix mixture system, and (3) the polyvinylpyrrolidone is present in an amount of about 1-10% by weight in the matrix mixture system, and comprises 1-40% of Rotigotine on the basis of the total weight of the composition. The present invention further relates to an improved transdermal patch containing Rotigotine comprising said composition. Said patch has improved properties in the solubility, release and initial penetration level of Rotigotine.
摘要翻译：本发明涉及含有罗替高汀的组合物及其在制造含罗替尼汀的透皮贴剂中的用途，其中所述组合物是基于由丙烯酸压敏粘合剂与硅氧烷压敏粘合剂组合形成的基质混合物体系，敏感性粘合剂和聚乙烯吡咯烷酮，其特征在于：（1）所述丙烯酸类压敏粘合剂在所述基质混合物体系中以约1-25％（重量）的量存在，（2）在基质混合体系中，敏感粘合剂的存在量为约65-98重量％，（3）在基质混合体系中，聚乙烯吡咯烷酮的存在量为约1-10重量％，并且包含1- 基于组合物总重量的罗替高汀为40％。本发明还涉及包含所述组合物的含有罗替高汀的改良透皮贴剂。所述贴剂具有改善的罗替戈汀的溶解度，释放和初始渗透水平的性质。

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