公开(公告)号：US20060280789A1

公开(公告)日：2006-12-14

申请号：US11317897

申请日：2005-12-27

申请人： Yosuke Ueki ,  Satoshi Fujioka ,  Shigeru Aoki ,  Susan Abu-Shakra ,  J. Carter ,  Gary Dorough

发明人： Yosuke Ueki ,  Satoshi Fujioka ,  Shigeru Aoki ,  Susan Abu-Shakra ,  J. Carter ,  Gary Dorough

IPC分类号： A61K31/445 ,  A61K9/20

CPC分类号： A61K9/2054 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2027 ,  A61K31/445

摘要： The invention provides sustained release formulations of basic drugs, stereoisomers of basic drugs, pharmaceutically acceptable salts of basic drugs, and pharmaceutically acceptable salts of stereoisomers of basic drugs. The basic drugs may be anti-dementia drugs, such as cholinesterase inhibitors or memantine. In one embodiment, the cholinesterase inhibitor is donepezil.

摘要翻译： 本发明提供碱性药物的缓释制剂，碱性药物的立体异构体，碱性药物的药学上可接受的盐，以及碱性药物的立体异构体的药学上可接受的盐。 碱性药物可能是抗痴呆药物，如胆碱酯酶抑制剂或美金刚。 在一个实施方案中，胆碱酯酶抑制剂是多奈哌齐。

公开(公告)号：US20070129402A1

公开(公告)日：2007-06-07

申请号：US11475255

申请日：2006-06-27

申请人： Yosuke Ueki ,  Satoshi Fujioka ,  Shigeru Aoki

发明人： Yosuke Ueki ,  Satoshi Fujioka ,  Shigeru Aoki

IPC分类号： A61K31/445

CPC分类号： A61K9/1635 ,  A61K9/1652 ,  A61K9/2027 ,  A61K9/2054 ,  A61K31/445

摘要： The invention provides sustained release formulations comprising donepezil, stereoisomers of donepezil, pharmaceutically acceptable salts of donepezil, or pharmaceutically acceptable salts of stereoisomers of donepezil. The formulations have desirable pharmacokinetic characteristics. Examples include AUC, Tmax, Cmax, dosage-corrected AUC, and dosage-corrected Cmax.

摘要翻译： 本发明提供包含多奈哌齐，多奈哌齐的立体异构体，多奈哌齐的药学上可接受的盐或多奈哌齐的立体异构体的药学上可接受的盐的缓释制剂。 制剂具有所需的药代动力学特征。 实例包括AUC，Tmax，Cmax，剂量校正的AUC和剂量校正的C max。

公开(公告)号：US20110045074A1

公开(公告)日：2011-02-24

申请号：US12910313

申请日：2010-10-22

申请人： Yosuke Ueki ,  Satoshi Fujioka

发明人： Yosuke Ueki ,  Satoshi Fujioka

IPC分类号： A61K9/10 ,  A61K31/445 ,  A61K31/13 ,  A61P25/28

CPC分类号： A61K31/445 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2095 ,  A61K31/13

摘要： A matrix type sustained-release preparation and a manufacturing method therefor are provided wherein dissolution with low pH dependence of a basic drug or a salt thereof at the early stage of dissolution can be ensured in a dissolution test, and wherein as the dissolution test proceeds, a ratio of a dissolution rate of the basic drug or the salt thereof in an acidic test solution to a dissolution rate of the basic drug or the salt thereof in a neutral test solution (dissolution rate in the acidic test solution/dissolution rate in the neutral test solution) decreases with dissolution time at the late stage of dissolution, as compared to the early stage of dissolution. According to the present invention, the matrix type sustained-release preparation contains a basic drug or a salt thereof and at least one enteric polymer, in which solubility of the basic drug or the salt thereof in a 0.1 N hydrochloric acid solution and a neutral aqueous solution, pH 6.0 is higher than in a basic aqueous solution, pH 8.0.

摘要翻译： 提供了一种基质型缓释制剂及其制备方法，其中在溶出试验中可以确保溶解初期碱性药物或其盐的低pH依赖性的溶解性，并且其中随着溶出试验的进行， 碱性药物或其盐在酸性试验溶液中的溶解速率与碱性药物或其盐在中性试验溶液中的溶解速率的比例（酸性试验溶液中的溶解速率/中性溶解速度 测试溶液）与溶解的早期相比在溶解后期的溶解时间下降。 根据本发明，基质型缓释制剂含有碱性药物或其盐和至少一种肠溶性聚合物，其中碱性药物或其盐在0.1N盐酸溶液和中性水溶液中的溶解度 溶液pH 6.0比碱性水溶液pH 8.0高。

公开(公告)号：US08481565B2

公开(公告)日：2013-07-09

申请号：US11793722

申请日：2005-12-27

申请人： Yosuke Ueki ,  Yasuyuki Suzuki ,  Satoshi Fujioka

发明人： Yosuke Ueki ,  Yasuyuki Suzuki ,  Satoshi Fujioka

IPC分类号： A01N43/42 ,  A61K9/14

CPC分类号： A61K9/2054 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2027 ,  A61K31/445

摘要： The present invention provides a method for stabilizing an anti-dementia drug in a pharmaceutical composition containing the anti-dementia drug and a high molecular weight basic substance by adding a high molecular weight acidic substance to said pharmaceutical composition. Further, the present invention provides a pharmaceutical composition containing an anti-dementia drug and a high molecular basic substance in which a high molecular weight acidic substance is contained for stabilizing the anti-dementia drug. Furthermore, the present invention provides a method for manufacturing a pharmaceutical composition which comprises steps wherein a solution or suspension containing a high molecular weight acidic substance is added to a mixture of an anti-dementia drug and a high molecular weight basic substance for the sake of stabilizing the anti-dementia drug.

公开(公告)号：US20060160852A1

公开(公告)日：2006-07-20

申请号：US11317238

申请日：2005-12-27

申请人： Susumu Kimura ,  Yosuke Ueki ,  Satoshi Fujioka

发明人： Susumu Kimura ,  Yosuke Ueki ,  Satoshi Fujioka

IPC分类号： A61K31/445 ,  A61K31/13

CPC分类号： A61K45/06 ,  A61K9/2018 ,  A61K9/209 ,  A61K31/13 ,  A61K31/445 ,  A61K2300/00

摘要： An object of the present invention is to provide, for the case of implementing a therapeutic method in which at least two kinds of anti-dementia drugs are used together, a composition that has a good therapeutic effect on the dementia, and also gives excellent compliance. Another object of the present invention is to provide a composition containing at least two kinds of the anti-dementia drugs, for which release of the anti-dementia drugs from the composition is controlled, whereby a combined effect of the anti-dementia drugs can be achieved well. Still another object of the present invention is to provide: a composition, for which the frequency of administration and the amount taken are reduced, and hence compliance can be improved; and a method of manufacturing such a composition. According to the present invention, there are provided a composition containing at least two kinds of the anti-dementia drugs; such a composition containing at least one sustained release portion containing an anti-dementia drug; and such a composition containing at least one cholinesterase inhibitor, and at least one N-methyl-D-aspartate receptor antagonist.

摘要翻译： 本发明的目的是提供一种治疗方法，其中至少两种抗痴呆药物一起使用，具有对痴呆具有良好治疗效果的组合物，并且还具有优异的依从性 。 本发明的另一个目的是提供一种含有至少两种抗痴呆药物的组合物，其中控制抗痴呆药物从组合物中的释放，由此抗痴呆药物的组合效果可以是 做得很好 本发明的另一个目的是提供：给药频率和使用量减少的组合物，从而可以提高顺应性; 以及制造这种组合物的方法。 根据本发明，提供含有至少两种抗痴呆药物的组合物; 这种组合物含有至少一种含有抗痴呆药物的持续释放部分; 和含有至少一种胆碱酯酶抑制剂和至少一种N-甲基-D-天冬氨酸受体拮抗剂的组合物。

公开(公告)号：US08507527B2

公开(公告)日：2013-08-13

申请号：US12712959

申请日：2010-02-25

申请人： Yosuke Ueki ,  Yasuyuki Suzuki ,  Satoshi Fujioka

发明人： Yosuke Ueki ,  Yasuyuki Suzuki ,  Satoshi Fujioka

IPC分类号： A01N43/42 ,  A61K9/14

CPC分类号： A61K9/2054 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2027 ,  A61K31/445

摘要： The present invention provides a method for stabilizing an anti-dementia drug in a pharmaceutical composition containing the anti-dementia drug and a high molecular weight basic substance by adding a high molecular weight acidic substance to said pharmaceutical composition. Further, the present invention provides a pharmaceutical composition containing an anti-dementia drug and a high molecular basic substance in which a high molecular weight acidic substance is contained for stabilizing the anti-dementia drug. Furthermore, the present invention provides a method for manufacturing a pharmaceutical composition which comprises steps wherein a solution or suspension containing a high molecular weight acidic substance is added to a mixture of an anti-dementia drug and a high molecular weight basic substance for the sake of stabilizing the anti-dementia drug.

摘要翻译： 本发明提供了通过向所述药物组合物中加入高分子量酸性物质，在含有抗痴呆药物和高分子量碱性物质的药物组合物中稳定抗痴呆药物的方法。 此外，本发明提供含有抗痴呆药物和高分子碱性物质的药物组合物，其中含有高分子量酸性物质以稳定抗痴呆药物。 此外，本发明提供了一种制备药物组合物的方法，其包括以下步骤：将含有高分子量酸性物质的溶液或悬浮液加入到抗痴呆药物和高分子量碱性物质的混合物中， 稳定抗痴呆药物。

公开(公告)号：US20080213368A1

公开(公告)日：2008-09-04

申请号：US11793722

申请日：2005-12-27

申请人： Yosuke Ueki ,  Yasuyuki Suzuki ,  Satoshi Fujioka

发明人： Yosuke Ueki ,  Yasuyuki Suzuki ,  Satoshi Fujioka

IPC分类号： A61K9/10 ,  A61K31/445

CPC分类号： A61K9/2054 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2027 ,  A61K31/445

摘要： The present invention provides a method for stabilizing an anti-dementia drug in a pharmaceutical composition containing the anti-dementia drug and a high molecular weight basic substance by adding a high molecular weight acidic substance to said pharmaceutical composition. Further, the present invention provides a pharmaceutical composition containing an anti-dementia drug and a high molecular basic substance in which a high molecular weight acidic substance is contained for stabilizing the anti-dementia drug. Furthermore, the present invention provides a method for manufacturing a pharmaceutical composition which comprises steps wherein a solution or suspension containing a high molecular weight acidic substance is added to a mixture of an anti-dementia drug and a high molecular weight basic substance for the sake of stabilizing the anti-dementia drug.

摘要翻译： 本发明提供了通过向所述药物组合物中加入高分子量酸性物质，在含有抗痴呆药物和高分子量碱性物质的药物组合物中稳定抗痴呆药物的方法。 此外，本发明提供含有抗痴呆药物和高分子碱性物质的药物组合物，其中含有高分子量酸性物质以稳定抗痴呆药物。 此外，本发明提供了一种制备药物组合物的方法，其包括以下步骤：将含有高分子量酸性物质的溶液或悬浮液加入到抗痴呆药物和高分子量碱性物质的混合物中， 稳定抗痴呆药物。

公开(公告)号：US20060159753A1

公开(公告)日：2006-07-20

申请号：US11317898

申请日：2005-12-27

申请人： Yosuke Ueki ,  Satoshi Fujioka

发明人： Yosuke Ueki ,  Satoshi Fujioka

IPC分类号： A61K9/22

CPC分类号： A61K9/2027 ,  A61K9/2054

摘要： A matrix type sustained-release preparation and a manufacturing method therefor are provided wherein dissolution with low pH dependence of a basic drug or a salt thereof at the early stage of dissolution can be ensured in a dissolution test, and wherein as the dissolution test proceeds, a ratio of a dissolution rate of the basic drug or the salt thereof in an acidic test solution to a dissolution rate of the basic drug or the salt thereof in a neutral test solution (dissolution rate in the acidic test solution/dissolution rate in the neutral test solution) decreases with dissolution time at the late stage of dissolution, as compared to the early stage of dissolution. According to the present invention, the matrix type sustained-release preparation contains a basic drug or a salt thereof and at least one enteric polymer, in which solubility of the basic drug or the salt thereof in a 0.1 N hydrochloric acid solution and a neutral aqueous solution, pH 6.0 is higher than in a basic aqueous solution, pH 8.0.

摘要翻译： 提供了一种基质型缓释制剂及其制备方法，其中在溶出试验中可以确保溶解初期碱性药物或其盐的低pH依赖性的溶解性，并且其中随着溶出试验的进行， 碱性药物或其盐在酸性试验溶液中的溶解速率与碱性药物或其盐在中性试验溶液中的溶解速率的比例（酸性试验溶液中的溶解速率/中性溶解速度 测试溶液）与溶解的早期相比在溶解后期的溶解时间下降。 根据本发明，基质型缓释制剂含有碱性药物或其盐和至少一种肠溶性聚合物，其中碱性药物或其盐在0.1N盐酸溶液和中性水溶液中的溶解度 溶液pH 6.0比碱性水溶液pH 8.0高。

公开(公告)号：US20100152164A1

公开(公告)日：2010-06-17

申请号：US12712959

申请日：2010-02-25

申请人： Yosuke Ueki ,  Yasuyuki Suzuki ,  Satoshi Fujioka

发明人： Yosuke Ueki ,  Yasuyuki Suzuki ,  Satoshi Fujioka

IPC分类号： A61K31/445 ,  A61K31/27 ,  A61K31/55 ,  A61K31/454 ,  A61P25/28

CPC分类号： A61K9/2054 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2027 ,  A61K31/445

摘要： The present invention provides a method for stabilizing an anti-dementia drug in a pharmaceutical composition containing the anti-dementia drug and a high molecular weight basic substance by adding a high molecular weight acidic substance to said pharmaceutical composition. Further, the present invention provides a pharmaceutical composition containing an anti-dementia drug and a high molecular basic substance in which a high molecular weight acidic substance is contained for stabilizing the anti-dementia drug. Furthermore, the present invention provides a method for manufacturing a pharmaceutical composition which comprises steps wherein a solution or suspension containing a high molecular weight acidic substance is added to a mixture of an anti-dementia drug and a high molecular weight basic substance for the sake of stabilizing the anti-dementia drug.

摘要翻译： 本发明提供了通过向所述药物组合物中加入高分子量酸性物质，在含有抗痴呆药物和高分子量碱性物质的药物组合物中稳定抗痴呆药物的方法。 此外，本发明提供含有抗痴呆药物和高分子碱性物质的药物组合物，其中含有高分子量酸性物质以稳定抗痴呆药物。 此外，本发明提供了一种制备药物组合物的方法，其包括以下步骤：将含有高分子量酸性物质的溶液或悬浮液加入到抗痴呆药物和高分子量碱性物质的混合物中， 稳定抗痴呆药物。

公开(公告)号：US20090208579A1

公开(公告)日：2009-08-20

申请号：US11794212

申请日：2005-12-12

申请人： Yosuke Ueki ,  Satoshi Fujioka

发明人： Yosuke Ueki ,  Satoshi Fujioka

IPC分类号： A61K9/14 ,  A61K31/445 ,  A61K31/13 ,  A61P25/28

CPC分类号： A61K31/445 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2095 ,  A61K31/13

摘要： A matrix type sustained-release preparation and a manufacturing method therefor are provided wherein dissolution with low pH dependence of a basic drug or a salt thereof at the early stage of dissolution can be ensured in a dissolution test, and wherein as the dissolution test proceeds, a ratio of a dissolution rate of the basic drug or the salt thereof in an acidic test solution to a dissolution rate of the basic drug or the salt thereof in a neutral test solution (dissolution rate in the acidic test solution/dissolution rate in the neutral test solution) decreases with dissolution time at the late stage of dissolution, as compared to the early stage of dissolution. According to the present invention, the matrix type sustained-release preparation contains a basic drug or a salt thereof and at least one enteric polymer, in which solubility of the basic drug or the salt thereof in a 0.1 N hydrochloric acid solution and a neutral aqueous solution, pH 6.0 is higher than in a basic aqueous solution, pH 8.0.

摘要翻译： 提供了一种基质型缓释制剂及其制备方法，其中在溶出试验中可以确保溶解初期碱性药物或其盐的低pH依赖性的溶解性，并且其中随着溶出试验的进行， 碱性药物或其盐在酸性试验溶液中的溶解速率与碱性药物或其盐在中性试验溶液中的溶解速率的比例（酸性试验溶液中的溶解速率/中性溶解速度 测试溶液）与溶解的早期相比在溶解后期的溶解时间下降。 根据本发明，基质型缓释制剂含有碱性药物或其盐和至少一种肠溶性聚合物，其中碱性药物或其盐在0.1N盐酸溶液和中性水溶液中的溶解度 溶液pH 6.0比碱性水溶液pH 8.0高。