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公开(公告)号：US20090169604A1
公开(公告)日：2009-07-02
申请号：US12097260
申请日：2006-12-13
IPC分类号： A61K9/70 , A61K31/135 , A61P9/00
CPC分类号： A61K9/7053 , A61K31/138 , A61K47/10 , A61K47/32
摘要： In the adhesive pharmaceutical preparation of the invention containing bisoprolol, a pressure-sensitive adhesive layer is laminated on one side of the backing. The pressure-sensitive adhesive layer contains a branched monoalcohol having from 12 to 28 carbon atoms, a free base of bisoprolol and a polyisobutylene pressure-sensitive adhesive. Accordingly, compatibility of the polyisobutylene pressure-sensitive adhesive with the free base of bisoprolol can be specifically increased. As a result, not only it becomes possible to increase blending amount of the free base of bisoprolol but also bleed of the free base of bisoprolol from the pressure-sensitive adhesive layer can be suppressed and, what is more, the pressure-sensitive adhesion characteristics sufficient from the practical point of view can be obtained.
摘要翻译： 在含有比索洛尔的本发明的粘合剂药物制剂中，在背衬的一侧层压压敏粘合剂层。 压敏粘合剂层含有具有12至28个碳原子的支链一元醇，比索洛尔的游离碱和聚异丁烯压敏粘合剂。 因此，可以特异性地增加聚异丁烯压敏粘合剂与比索洛尔的游离碱的相容性。 结果，可以抑制比索洛尔的游离碱的混合量的增加，而且可以抑制比索洛尔的游离碱从压敏粘合剂层的渗出，而且还可以抑制压敏粘合特性 从实用的角度来看可以获得足够的。
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公开(公告)号：US08298572B2
公开(公告)日：2012-10-30
申请号：US12097260
申请日：2006-12-13
IPC分类号： A61K9/70 , A61K47/10 , A61K47/32 , A61K31/045 , A61K31/138
CPC分类号： A61K9/7053 , A61K31/138 , A61K47/10 , A61K47/32
摘要： In the adhesive pharmaceutical preparation of the invention containing bisoprolol, a pressure-sensitive adhesive layer is laminated on one side of the backing. The pressure-sensitive adhesive layer contains a branched monoalcohol having from 12 to 28 carbon atoms, a free base of bisoprolol and a polyisobutylene pressure-sensitive adhesive. Accordingly, compatibility of the polyisobutylene pressure-sensitive adhesive with the free base of bisoprolol can be specifically increased. As a result, not only it becomes possible to increase blending amount of the free base of bisoprolol but also bleed of the free base of bisoprolol from the pressure-sensitive adhesive layer can be suppressed and, what is more, the pressure-sensitive adhesion characteristics sufficient from the practical point of view can be obtained.
摘要翻译： 在含有比索洛尔的本发明的粘合剂药物制剂中，在背衬的一侧层压压敏粘合剂层。 压敏粘合剂层含有具有12至28个碳原子的支链一元醇，比索洛尔的游离碱和聚异丁烯压敏粘合剂。 因此，可以特异性地增加聚异丁烯压敏粘合剂与比索洛尔的游离碱的相容性。 结果，可以抑制比索洛尔的游离碱的混合量的增加，而且可以抑制比索洛尔的游离碱从压敏粘合剂层的渗出，而且还可以抑制压敏粘合特性 从实用的角度来看可以获得足够的。
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3.发明授权Proline ester and preparation containing the same for percutaneous administration 失效脯氨酸酯和含有相同用于经皮给药的制剂公开(公告)号：US07323489B2
公开(公告)日：2008-01-29
申请号：US10527062
申请日：2003-09-08
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： A61K9/7053 , A61K9/0014 , A61K9/7076 , A61K38/00 , C07K5/0222 , C07K5/06026
摘要： A proline ester represented by the following formula (I): wherein R1 represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.
摘要翻译： 由下式（I）表示的脯氨酸酯：其中R 1表示羟基 - 低级烷基，低级烷氧基 - 低级烷基或低级烷氧基 - 低级烷氧基 - 低级烷基，或 其药学上可接受的盐。 本发明的脯氨酸酯（I）及其药学上可接受的盐可用作依那普利的前药，它是可用于预防或治疗诸如高血压，心脏疾病（例如心脏肥大，心脏衰竭， 和心肌梗塞），肾炎和中风。 因此，从药物活性和用途的观点出发，优选将含有酯或其盐的药剂配制成经皮制剂，特别是贴剂。
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公开(公告)号：US20100098747A1
公开(公告)日：2010-04-22
申请号：US12528194
申请日：2008-03-06
IPC分类号： A61K9/70 , A61K31/138 , A61P9/00
CPC分类号： A61K31/138 , A61K9/7053 , A61K9/7061
摘要： The present invention relates to a percutaneous administration device of bisoprolol, which includes a backing; and a pressure-sensitive adhesive layer containing bisoprolol, which is laminated on one surface of the backing, wherein the maximum value of a release rate of bisoprolol during a period of from immediately after the application on skin until a lapse of 24 hours is 30 μg/cm2/hr or less; and wherein the release rate of bisoprolol at the time of a lapse of 24 hours after the application on skin is 10 μg/cm2/hr or less. The percutaneous administration device of the present invention is reduced in the skin irritation during the application, especially at the time of peeling, and is capable of persistently administrating a therapeutically or preventively effective amount of bisoprolol into a living body.
摘要翻译： 本发明涉及比索洛尔的经皮给药装置，其包括背衬; 以及层压在背衬的一个表面上的含有比索洛尔的压敏粘合剂层，其中在施用于皮肤上直到24小时之后的期间，比索洛尔的释放速率的最大值为30μg / cm 2 / hr以下; 并且其中在皮肤上施用后24小时时比索洛尔的释放速率为10μg/ cm 2 / hr以下。 本发明的经皮给药装置，特别是剥离时，皮肤刺激性降低，能够将治疗或预防有效量的比索洛尔施用于生物体。
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5.发明申请Proline ester and preparation containing the same for percutaneous administration 失效脯氨酸酯和含有相同用于经皮给药的制剂公开(公告)号：US20050288232A1
公开(公告)日：2005-12-29
申请号：US10527062
申请日：2003-09-08
申请人： Takayuki Furuishi , Kunihiro Minami
发明人： Takayuki Furuishi , Kunihiro Minami
IPC分类号： A61K9/00 , A61K9/70 , A61K38/00 , A61P9/04 , A61P9/12 , A61P43/00 , C07K5/02 , C07K5/062 , A61K38/04 , C07K5/04
CPC分类号： A61K9/7053 , A61K9/0014 , A61K9/7076 , A61K38/00 , C07K5/0222 , C07K5/06026
摘要： A proline ester represented by the following formula (I): wherein R1 represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.
摘要翻译： 由下式（I）表示的脯氨酸酯：其中R 1表示羟基 - 低级烷基，低级烷氧基 - 低级烷基或低级烷氧基 - 低级烷氧基 - 低级烷基，或 其药学上可接受的盐。 本发明的脯氨酸酯（I）及其药学上可接受的盐可用作依那普利的前药，它是可用于预防或治疗诸如高血压，心脏疾病（例如心脏肥大，心脏衰竭， 和心肌梗塞），肾炎和中风。 因此，从药物活性和用途的观点出发，优选将含有酯或其盐的药剂配制成经皮制剂，特别是贴剂。
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公开(公告)号：US08808731B2
公开(公告)日：2014-08-19
申请号：US12066095
申请日：2006-09-07
IPC分类号： A61K9/70 , A61P9/12 , A61K31/135
CPC分类号： A61K31/138 , A61K9/7053
摘要： An adhesive pharmaceutical preparation which has a less irritation to the skin surface, keeps excellent stability of bisoprolol in the preparation, and allows continuous administration of a pharmacologically effective amount of bisoprolol into the living body, is provided. The adhesive preparation 10 comprises a support 1, an adhesive layer 2 laminated on one surface of the support 1. The adhesive layer 2 is characterized by containing bisoprolol, polyisobutylene, tackifier, and an organic liquid ingredient compatible to polyisobutylene and tackifier. Thus, an adhesive pharmaceutical preparation which has a good adhesiveness with less irritation to the skin and which gives almost no pain at peel-off or removal from the skin surface with leaving almost no paste, can be provided. In addition, bisoprolol is very stably maintained in the preparation and a pharmacologically effective amount of bisoprolol can be administered continuously into the living body through the skin surface.
摘要翻译： 具有对皮肤表面刺激性低的粘合性药物制剂，在制剂中保持比索洛尔优异的稳定性，并且允许将药理学有效量的比索洛尔连续给予生物体。 粘合剂制剂10包括支撑体1，层压在载体1的一个表面上的粘合剂层2.粘合剂层2的特征在于含有比索洛尔，聚异丁烯，增粘剂和与聚异丁烯和增粘剂相容的有机液体成分。 因此，可以提供粘合性药物制剂，其具有良好的粘附性，对皮肤的刺激性较差，并且几乎不会留下剥离或从皮肤表面除去而几乎不产生疼痛，几乎没有糊剂。 此外，比索洛尔在制剂中非常稳定地保持，并且可以通过皮肤表面连续向生物体中施用药理学有效量的比索洛尔。
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公开(公告)号：US08703178B2
公开(公告)日：2014-04-22
申请号：US12528194
申请日：2008-03-06
IPC分类号： A61K9/70 , A61K31/138 , A61P9/00
CPC分类号： A61K31/138 , A61K9/7053 , A61K9/7061
摘要： The present invention relates to a percutaneous administration device of bisoprolol, which includes a backing; and a pressure-sensitive adhesive layer containing bisoprolol, which is laminated on one surface of the backing, wherein the maximum value of a release rate of bisoprolol during a period of from immediately after the application on skin until a lapse of 24 hours is 30 μg/cm2/hr or less; and wherein the release rate of bisoprolol at the time of a lapse of 24 hours after the application on skin is 10 μg/cm2/hr or less. The percutaneous administration device of the present invention is reduced in the skin irritation during the application, especially at the time of peeling, and is capable of persistently administrating a therapeutically or preventively effective amount of bisoprolol into a living body.
摘要翻译： 本发明涉及比索洛尔的经皮给药装置，其包括背衬; 以及层压在背衬的一个表面上的含有比索洛尔的压敏粘合剂层，其中在施用于皮肤上直到24小时之后的期间，比索洛尔的释放速率的最大值为30μg / cm 2 / hr以下; 并且其中在皮肤上施用后24小时时比索洛尔的释放速率为10μg/ cm 2 / hr以下。 本发明的经皮给药装置，特别是剥离时，皮肤刺激性降低，能够将治疗或预防有效量的比索洛尔施用于生物体。
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公开(公告)号：US20090291126A1
公开(公告)日：2009-11-26
申请号：US12066095
申请日：2006-09-07
IPC分类号： A61K9/70 , A61P9/12 , A61K31/135
CPC分类号： A61K31/138 , A61K9/7053
摘要： An adhesive pharmaceutical preparation which has a less irritation to the skin surface, keeps excellent stability of bisoprolol in the preparation, and allows continuous administration of a pharmacologically effective amount of bisoprolol into the living body, is provided. The adhesive preparation 10 comprises a support 1, an adhesive layer 2 laminated on one surface of the support 1. The adhesive layer 2 is characterized by containing bisoprolol, polyisobutylene, tackifier, and an organic liquid ingredient compatible to polyisobutylene and tackifier. Thus, an adhesive pharmaceutical preparation which has a good adhesiveness with less irritation to the skin and which gives almost no pain at peel-off or removal from the skin surface with leaving almost no paste, can be provided. In addition, bisoprolol is very stably maintained in the preparation and a pharmacologically effective amount of bisoprolol can be administered continuously into the living body through the skin surface.
摘要翻译： 具有对皮肤表面刺激性低的粘合性药物制剂，在制剂中保持比索洛尔优异的稳定性，并且允许将药理学有效量的比索洛尔连续给予生物体。 粘合剂制剂10包括支撑体1，层压在载体1的一个表面上的粘合剂层2.粘合剂层2的特征在于含有比索洛尔，聚异丁烯，增粘剂和与聚异丁烯和增粘剂相容的有机液体成分。 因此，可以提供粘合性药物制剂，其具有良好的粘附性，对皮肤的刺激性较差，并且几乎不会留下剥离或从皮肤表面除去而几乎不产生疼痛，几乎没有糊剂。 此外，比索洛尔在制剂中非常稳定地保持，并且可以通过皮肤表面连续向生物体中施用药理学有效量的比索洛尔。
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