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公开(公告)号：US20100305179A1
公开(公告)日：2010-12-02
申请号：US12855226
申请日：2010-08-12
IPC分类号： A61K31/4174 , A61P13/00
CPC分类号： A61K9/2054 , A61K31/4174
摘要： (Object) An oral sustained-release tablet is provided, which does not cause initial rapid increases in the bloodlevels of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide (KRP-197) and can maintain constant the blood levels.(Solving means) An oral sustained-release tablet comprises a pharmaceutical composition and a gel-forming material, the pharmaceutical composition containing KRP-197 as an active ingredient.
摘要翻译： （对象）提供口服持续释放片剂，其不会引起4-（2-甲基-1-咪唑基）-2,2-二苯基丁基酰胺（KRP-197）的血液水平的初始快速增加，并且可以保持恒定 血液水平。 （解决方案）口服缓释片剂包含药物组合物和凝胶形成材料，所述药物组合物含有KRP-197作为活性成分。
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2.发明申请Multiple Unit Oral Sustained Release Preparation and Production Method Thereof 审中-公开多单位口服缓释制剂及其制备方法公开(公告)号：US20080107727A1
公开(公告)日：2008-05-08
申请号：US11795792
申请日：2006-01-30
IPC分类号： A61K31/417 , A61K9/24 , A61K9/52 , A61K9/16
CPC分类号： A61K9/1652 , A61K9/1617 , A61K9/2077 , A61K9/5078 , A61K31/4164
摘要： A multiple-unit oral sustained release preparation is provided which allows controlled release of imidafenacin [4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide]. The preparation serves to ensure a prolonged effect of imidafenacin and prevent rapid elevation in the blood levels of imidafenacin.Specifically, granules or powders comprising imidafenacin dispersed in a water-insoluble polymer or a higher alcohol are used in the preparation. These preparations achieve sustained release of imidafenacin since the molecular network structure that the water-insoluble polymer or the higher alcohol forms during the preparation of the granules or powders serves to control the rate of diffusion of imidafenacin in water. Granules comprising a core granule having two layers of an inner imidafenacin coating and an outer water-insoluble polymer coating are used in the preparation. The water-insoluble polymer coating serves to control the rate of diffusion of imidafenacin in water and ensure sustained release of imidafenacin. The multiple-unit oral sustained release preparation is provided in the forms of capsules and tablets containing the granules or powders that allow controlled release of imidafenacin. The preparation achieves controlled release of imidafenacin over a prolonged period of time.
摘要翻译： 提供多单位口服持续释放制剂，其允许控制释放咪达那新[4-（2-甲基-1-咪唑基）-2,2-二苯基丁基酰胺]。 该制剂用于确保咪达达敏的长期作用，并防止咪达那新的血液水平迅速升高。 具体地，在制剂中使用包含分散在水不溶性聚合物或高级醇中的咪达那新的颗粒或粉末。 由于在制备颗粒或粉末期间水不溶性聚合物或高级醇形成的分子网络结构用于控制咪达那新在水中的扩散速率，因此这些制剂实现咪达那新的持续释放。 在制剂中使用包含具有两层内亚胺多沙星涂层和外部水不溶性聚合物涂层的核心颗粒的颗粒。 水不溶性聚合物涂层用于控制咪达那新在水中的扩散速率，并确保咪达那新的持续释放。 多单位口服持续释放制剂以含有允许控制释放咪达那新的颗粒或粉末的胶囊和片剂的形式提供。 该制剂在长时间内实现了咪达那新的控制释放。
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公开(公告)号：US20100102474A1
公开(公告)日：2010-04-29
申请号：US12514330
申请日：2007-11-12
申请人： Katashi Nakashima , Kazuo Kazama
发明人： Katashi Nakashima , Kazuo Kazama
CPC分类号： A61J3/10 , A61K9/2077
摘要： Herein provided is a method for easily preparing a sustained release tablet which contains an orally administrable medicinal component, while maintaining the uniformity of the content of the medicinal component.The method comprises mixing (1) a granulated product A obtained by granulating an excipient and an enteric coating agent while spraying thereon with a solution or a suspension containing an orally administrable medicinal component, with (2) a composition B containing a hydrogel-forming substance; and then compressing the resulting mixture into a tablet.
摘要翻译： 本发明提供一种容易地制备含有可口服给药的药物成分的缓释片剂的方法，同时保持药物成分的含量的均匀性。 该方法包括混合（1）通过使赋形剂和肠溶包衣剂制粒而得到的造粒产品A，同时用含有口服药物组分的溶液或悬浮液喷雾，和（2）含有水凝胶形成物质的组合物B ; 然后将所得混合物压片成片剂。
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公开(公告)号：US20070092566A1
公开(公告)日：2007-04-26
申请号：US10566503
申请日：2004-08-03
IPC分类号： A61K31/4172 , A61K9/22
CPC分类号： A61K9/2054 , A61K31/4174
摘要： An oral sustained-release tablet is provided, which does not cause initial rapid increases in the bloodlevels of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide (KRP-197) and can maintain constant the blood levels. (Solving means) An oral sustained-release tablet comprises a pharmaceutical composition and a gel-forming material, the pharmaceutical composition containing KRP-197 as an active ingredient.
摘要翻译： 提供口服持续释放片剂，其不引起4-（2-甲基-1-咪唑基）-2,2-二苯基丁基酰胺（KRP-197）的血液水平的初步快速增加，并且可以保持血液水平恒定。 （解决方案）口服缓释片剂包含药物组合物和凝胶形成材料，所述药物组合物含有KRP-197作为活性成分。
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公开(公告)号：US08343544B2
公开(公告)日：2013-01-01
申请号：US12855226
申请日：2010-08-12
IPC分类号： A61K9/22
CPC分类号： A61K9/2054 , A61K31/4174
摘要： (Object) An oral sustained-release tablet is provided, which does not cause initial rapid increases in the bloodlevels of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide (KRP-197) and can maintain constant the blood levels.(Solving means) An oral sustained-release tablet comprises a pharmaceutical composition and a gel-forming material, the pharmaceutical composition containing KRP-197 as an active ingredient.
摘要翻译： （对象）提供口服持续释放片剂，其不会引起4-（2-甲基-1-咪唑基）-2,2-二苯基丁基酰胺（KRP-197）的血液水平的初始快速增加，并且可以保持恒定 血液水平。 （解决方案）口服缓释片剂包含药物组合物和凝胶形成材料，所述药物组合物含有KRP-197作为活性成分。
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公开(公告)号：US08202456B2
公开(公告)日：2012-06-19
申请号：US12514330
申请日：2007-11-12
申请人： Katashi Nakashima , Kazuo Kazama
发明人： Katashi Nakashima , Kazuo Kazama
IPC分类号： B29C43/02
CPC分类号： A61J3/10 , A61K9/2077
摘要： Herein provided is a method for easily preparing a sustained release tablet which contains an orally administrable medicinal component, while maintaining the uniformity of the content of the medicinal component.The method comprises mixing (1) a granulated product A obtained by granulating an excipient and an enteric coating agent while spraying thereon with a solution or a suspension containing an orally administrable medicinal component, with (2) a composition B containing a hydrogel-forming substance; and then compressing the resulting mixture into a tablet.
摘要翻译： 本发明提供一种容易地制备含有可口服给药的药物成分的缓释片剂的方法，同时保持药物成分的含量的均匀性。 该方法包括混合（1）通过使赋形剂和肠溶包衣剂制粒而得到的造粒产品A，同时用含有口服药物组分的溶液或悬浮液喷雾，和（2）含有水凝胶形成物质的组合物B ; 然后将所得混合物压片成片剂。
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公开(公告)号：US20070154543A1
公开(公告)日：2007-07-05
申请号：US10552889
申请日：2004-04-14
IPC分类号： A61K31/325 , A61K31/27 , A61K9/20
CPC分类号： A61K31/195 , A61K9/2866
摘要： Upon performing the clinical study of (S)-2-[3-[N-[4-(4-fluorophenoxy)benzyl]carbamoyl]-4-methoxybenz yl]butanoic acid (hereinafter abbreviated as KRP-101), of which improvement in the lipidmetabolism is expected in a microdose, no oral solid dosage form that allows KRP-101 to be administered quantitatively has been embodied. After mixing KRP-101 with additives (excipient, disintegrator and lubricant), the mixture is granulated, pressed into tablets and coated with coating agent, thereby film-coated tablets uniformly containing a small amount of KRP-101 are obtained, making it possible to administer amicrodose of KRP-101 quantitatively on clinical study.
摘要翻译： 在进行（S）-2- [3- [N- [4-（4-氟苯氧基）苄基]氨基甲酰基] -4-甲氧基苄基]丁酸（以下简称为KRP-101）的临床研究中， 在微剂量中预期脂代谢，已经体现了允许定量施用KRP-101的口服固体剂型。 将KRP-101与添加剂（赋形剂，崩解剂和润滑剂）混合后，将混合物造粒，压制成片剂并用包衣剂涂布，得到均匀含有少量KRP-101的薄膜包衣片剂， 在临床研究中定量地施用KRP-101的微量。
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公开(公告)号：US20060188554A1
公开(公告)日：2006-08-24
申请号：US10566502
申请日：2004-08-03
IPC分类号： A61K31/445 , A61K31/4164 , A61F13/02
CPC分类号： A61K9/7053 , A61K9/7076 , A61K31/4174
摘要： (Object) A transdermal preparation is provided, which ensures stable and effective absorption of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide (KRP-197) which has a low skin absorption and is a bladder-selective muscarinic M3 and M1 receptor antagonist, into body through the skin while causing little side effects and providing sustained pharmacological effect with less skin irritancy. (Solving means) A composition comprising KRP-197 and an external preparation base is deposited and dried onto a structural body or a small pool of the composition is deposited on the structural body to obtain a single adhesive layer-type transdermal preparation or a reservoir-type transdermal preparation. These preparations can ensure high permeation of KRP-197 through the skin and sustained absorption of KRP-197 into body while causing decreased skin irritancy.
摘要翻译： （对象）提供透皮制剂，其确保具有低皮肤吸收性并且是膀胱选择性的4-（2-甲基-1-咪唑基）-2,2-二苯基丁基酰胺（KRP-197）的稳定和有效的吸收 毒蕈碱M3和M1受体拮抗剂通过皮肤进入体内，同时引起少量副作用，并提供持久的药理作用，皮肤刺激性较小。 （解决方法）将包含KRP-197和外部制剂基质的组合物沉积并干燥到结构体上，或将组合物的小池沉积在结构体上，以获得单一粘合剂层型透皮制剂或储液器 - 型透皮制剂。 这些制剂可以确保KRP-197通过皮肤的高渗透和KRP-197持续吸收到体内，同时引起皮肤刺激性降低。
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