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。

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。

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。

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。

公开(公告)号：US06406562B1

公开(公告)日：2002-06-18

申请号：US09572699

申请日：2000-05-16

申请人： Yucheng Lu ,  Michael Brian Ives

发明人： Yucheng Lu ,  Michael Brian Ives

IPC分类号： C23C2282

CPC分类号： C23C22/56 ,  C23C22/48 ,  C23C22/50 ,  C23C22/52 ,  C23C22/68

摘要： There is provided a method for treating the surface of metals such as nickel based or high alloy steels, austenitic and ferritic stainless steels, copper and aluminum alloys to increase their corrosion resistance by modification of the metal surfaces to inhibit cathodic corrosion processes. In a single step treatment process the metals are immersed into a heated aqueous composition containing a rare earth salt substantially free of any halide compound. Increased corrosion resistance is obtained using nitrates of yttrium, gadolinium, cerium, europium, terbium, samarium, neodymium, praseodymium, lanthanum, holmium, ytterbium, dysprosium, and erbium nitrates. The rare earth salt is present in the range from about 2% by weight to saturation of the solution. The composition includes a pH-modifying substance such as nitric acid to adjust the pH in the range 0.5 to about 6.5 to attack the surface to remove oxides facilitating deposition of the rare earth.

摘要翻译： 提供了一种用于处理镍基或高合金钢，奥氏体和铁素体不锈钢，铜和铝合金等金属表面的方法，通过改变金属表面以抑制阴极腐蚀过程来提高其耐腐蚀性。 在单步处理工艺中，将金属浸入含有基本上不含任何卤化物的稀土盐的加热含水组合物中。 使用钇，钆，铈，铕，铽，钐，钕，镨，镧，钬，镱，镝和硝酸铒的硝酸盐可以获得提高的耐腐蚀性。 稀土盐以约2重量％至溶液饱和的范围存在。 组合物包括pH调节物质如硝酸，以将pH调节在0.5至约6.5的范围内以侵蚀表面以除去促进稀土沉积的氧化物。

公开(公告)号：US6068711A

公开(公告)日：2000-05-30

申请号：US863935

申请日：1997-05-27

申请人： Yucheng Lu ,  Michael Brian Ives

发明人： Yucheng Lu ,  Michael Brian Ives

IPC分类号： C23C22/48 ,  C23C22/50 ,  C23C22/52 ,  C23C22/56 ,  C23C22/68

CPC分类号： C23C22/56 ,  C23C22/48 ,  C23C22/50 ,  C23C22/52 ,  C23C22/68

摘要： There is provided a method for treating the surface of metals such as nickel based or high alloy steels, austenitic and ferritic stainless steels, copper and aluminum alloys to increase their corrosion resistance by modification of the metal surfaces to inhibit cathodic corrosion processes. In a single step treatment process the metals are immersed into a heated aqueous composition containing a rare earth salt substantially free of any halide compound. Increased corrosion resistance is obtained using nitrates of yttrium, gadolinium, cerium, europium, terbium, samarium, neodymium, praseodymium, lanthanum, holmium, ytterbium, dysprosium, and erbium nitrates. The rare earth salt is present in the range from about 2% by weight to saturation of the solution. The composition includes a pH-modifying substance such as nitric acid to adjust the pH in the range 0.5 to about 6.5 to attack the surface to remove oxides facilitating deposition of the rare earth. For aluminum alloys the pH is maintained between 4.5 to 6.5, for nickel based alloys and austenitic stainless steels the pH is maintained between 0.5 to 3.5 and between pH 2.0 to 4.5 for ferritic stainless steels. The surface can also be conditioned by abrasion before or during immersion in the composition. Increased corrosion resistance is achieved by immersion for time periods in the range of a few minutes up to one hour with the composition maintained between 60 to 95.degree. C. Cerium, gadolinium, neodymium and praseodymium nitrate when used alone produced the greatest degree of corrosion resistance compared to the other rare earth nitrates. Significant synergistic effects are observed when combinations of two or more rare earth nitrates are used in the compositions. Aqueous treatment solutions based on combinations of cerium nitrate, gadolinium nitrate and lanthanum nitrate are very effective in reducing crevice corrosion.