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公开(公告)号：US20090028939A1
公开(公告)日：2009-01-29
申请号：US12086700
申请日：2006-12-21
IPC分类号： A61K9/14 , A61K31/4439 , A61K9/20 , A61P3/00
CPC分类号： A61K9/209 , A61K9/1623 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/2077 , A61K31/366 , A61K31/4439 , A61K31/64
摘要： The present invention intends to provide a solid preparation which contains an insulin sensitizer and an active ingredient other than an insulin sensitizer, and exhibits dissolution behavior of an insulin sensitizer similar to that of an insulin sensitizer from “a solid preparation containing only an insulin sensitizer as an active ingredient”. The solid preparation comprises “a part containing coated particles in which the particles containing an insulin sensitizer are coated with lactose or a sugar alcohol” and “a part containing an active ingredient other than an insulin sensitizer”.
摘要翻译： 本发明提供一种固体制剂，其含有胰岛素敏化剂和胰岛素敏化剂以外的活性成分，并且表现出胰岛素敏化剂与胰岛素敏化剂类似的胰岛素敏化剂的溶解行为，其来自“仅含胰岛素敏化剂的固体制剂如 活性成分“。 固体制剂包括“含有包含胰岛素敏化剂的颗粒的包衣颗粒的部分用乳糖或糖醇包衣的部分”和“含有胰岛素敏化剂以外的活性成分的部分”。
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公开(公告)号：US08071130B2
公开(公告)日：2011-12-06
申请号：US12086700
申请日：2006-12-21
CPC分类号： A61K9/209 , A61K9/1623 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/2077 , A61K31/366 , A61K31/4439 , A61K31/64
摘要： The present invention intends to provide a solid preparation which contains an insulin sensitizer and an active ingredient other than an insulin sensitizer, and exhibits dissolution behavior of an insulin sensitizer similar to that of an insulin sensitizer from “a solid preparation containing only an insulin sensitizer as an active ingredient”. The solid preparation comprises “a part containing coated particles in which the particles containing an insulin sensitizer are coated with lactose or a sugar alcohol” and “a part containing an active ingredient other than an insulin sensitizer”.
摘要翻译： 本发明提供一种固体制剂，其含有胰岛素敏化剂和胰岛素敏化剂以外的活性成分，并且表现出胰岛素敏化剂与胰岛素敏化剂类似的胰岛素敏化剂的溶解行为，其来自“仅含胰岛素敏化剂的固体制剂如 活性成分“。 固体制剂包括“含有包含胰岛素敏化剂的颗粒的包衣颗粒的部分用乳糖或糖醇包衣的部分”和“含有胰岛素敏化剂以外的活性成分的部分”。
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公开(公告)号：US08637077B2
公开(公告)日：2014-01-28
申请号：US10451922
申请日：2001-12-26
CPC分类号： A61K9/5031 , A61K9/0019 , A61K9/10 , A61K9/1647 , A61K38/27 , A61K47/18 , A61K47/183 , A61K47/186 , A61K47/26 , A61K47/36 , A61K47/42
摘要： Sustained release preparations, which show suppressed initial release of a physiologically active substance and can release a constant amount of the physiologically active substance over a long period of time, and dispersion vehicle thereof can be obtained by adding a cationic substance or polyols to the outside of a matrix or dispersion vehicle thereof. Thus, sustained release preparations, which show suppressed initial release of a physiologically active substance immediately after the administration and can release a constant amount of the physiologically active substance over a long period of time and dispersion vehicle thereof can be provided.
摘要翻译： 持续释放制剂显示抑制生理活性物质的初始释放并且可以长时间释放一定量的生理活性物质，并且其分散载体可以通过将阳离子物质或多元醇加入到 其基质或分散载体。 因此，可以提供在施用后立即抑制生理活性物质的初次释放并能够长时间释放一定量的生理活性物质及其分散载体的缓释制剂。
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公开(公告)号：US06267981B1
公开(公告)日：2001-07-31
申请号：US09571728
申请日：2000-05-15
IPC分类号： A61F200
CPC分类号： A61K38/27 , A61K9/1647 , A61K9/5031 , A61K38/28
摘要： This invention provides a sustained-release preparation comprising a biodegradable polymer metal salt and broactive polypeptide, with enhanced entrapment of the bioactive polypeptides, a suppression of initial burst, and a constant long-term release of the bioactive polypeptides.
摘要翻译： 本发明提供包含可生物降解的聚合物金属盐和活性多肽的持续释放制剂，其具有增强的生物活性多肽捕获，抑制初始爆发以及生物活性多肽的恒定长期释放。
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公开(公告)号：US20130115292A1
公开(公告)日：2013-05-09
申请号：US13695366
申请日：2011-04-28
申请人： Masafumi Misaki , Yuki Tsushima , Masahiro Niwa
发明人： Masafumi Misaki , Yuki Tsushima , Masahiro Niwa
IPC分类号： A61K9/28
CPC分类号： A61K9/2027 , A61K9/2018 , A61K9/2813 , A61K9/2846 , A61K9/2866 , A61K9/2886 , A61K31/495
摘要： The present invention relates to an enteric tablet with improved bioavailability, which is rapidly disintegrated after reaching the intestine to allow dissolution of the active ingredient, and which characteristically reduces the amount of talc to be used and is free of an alkali component.
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6.发明授权公开(公告)号：US06482864B1
公开(公告)日：2002-11-19
申请号：US09319023
申请日：1999-05-28
申请人： Yutaka Yamagata , Masafumi Misaki , Susumu Iwasa
发明人： Yutaka Yamagata , Masafumi Misaki , Susumu Iwasa
IPC分类号： A61K4732
CPC分类号： A61K9/1647 , A61K38/27 , Y10S514/964
摘要： A method for producing a sustained-release preparation, which comprises dispersing a physiologically active polypeptide into an organic solvent solution of a biodegradable polymer and removing the organic solvent, wherein the polypeptide is a powder obtained by lyophilizing an aqueous solution of the polypeptide which solution has a water-miscible organic solvent and/or a volatile salt; which improves the ease of handling of the physiologically active polypeptide powder in the process for producing the preparation; which makes it possible to industrially produce the sustained-release preparation in large scale; which provides a sustained-release preparation showing high and stable concentration of the active component in blood in long term, low initial release ratio of the physiologically active polypeptide, and high entrapment ratio of the polypeptide into the sustained-release preparation.
摘要翻译： 一种缓释制剂的制备方法，其包括将生理活性多肽分散到生物可降解聚合物的有机溶剂溶液中并除去有机溶剂，其中所述多肽是通过将多肽溶液冻干得到的粉末 水混溶性有机溶剂和/或挥发性盐; 这提高了在制备该制剂的过程中易于处理生理活性多肽粉末; 这使得可以大规模地工业生产缓释制剂; 其提供持续释放制剂，其显示出高生产活性多肽的长期，低的初始释放比例以及所述多肽进入缓释制剂的高滞留比，从而高效稳定血液中活性成分的浓度。
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公开(公告)号：US20150157609A1
公开(公告)日：2015-06-11
申请号：US14009277
申请日：2012-03-29
申请人： Wataru Hoshina , Masafumi Misaki
发明人： Wataru Hoshina , Masafumi Misaki
IPC分类号： A61K31/4188 , A61K47/02
CPC分类号： A61K9/2009 , A61K9/2018 , A61K9/2054 , A61K9/28 , A61K31/4188 , A61K47/02
摘要： The present invention provides a solid preparation wherein variation in weight is suppressed, a solid preparation wherein the active ingredient is stabilized, and a stabilization method thereof. A solid preparation containing (1) an active ingredient, (2) D-mannitol and (3) an alkaline earth metal salt selected from magnesium aluminometasilicate and calcium silicate. A method of stabilizing the. active ingredient, including adding an alkaline earth metal salt selected from magnesium aluminometasilicate and calcium silicate.
摘要翻译： 本发明提供了其中抑制重量变化的固体制剂，其中活性成分稳定的固体制剂及其稳定化方法。 一种固体制剂，其含有（1）活性成分，（2）D-甘露糖醇和（3）选自硅铝酸镁和硅酸钙的碱土金属盐。 一种稳定的方法。 包括加入选自硅酸铝镁和硅酸钙的碱土金属盐。
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公开(公告)号：US20130115291A1
公开(公告)日：2013-05-09
申请号：US13695220
申请日：2011-04-28
申请人： Masafumi Misaki , Yuki Tsushima , Masahiro Niwa
发明人： Masafumi Misaki , Yuki Tsushima , Masahiro Niwa
IPC分类号： A61K9/28
CPC分类号： A61K9/2077 , A61K9/2813 , A61K9/2846 , A61K9/2886 , A61K31/4465
摘要： The present invention relates to an enteric tablet with improved bioavailability, which is rapidly disintegrated after reaching the intestine to allow dissolution of the active ingredient, and which characteristically reduces the amount of talc to be used and is free of an alkali component.
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公开(公告)号：US06706732B1
公开(公告)日：2004-03-16
申请号：US09980391
申请日：2001-11-28
IPC分类号： A61K3147
CPC分类号： C07D215/38 , A61K9/0043 , A61K31/47
摘要： A nasal preparation comprising a compound represented by the formula: wherein Ring A is an optionally substituted 5- or 6-membered aromatic heterocyclic ring, Ring B is an optionally substituted 5- or 6-membered aromatic homocyclic or heterocyclic ring, R1 is a hydrogen atom, a hydroxyl group or a lower alkyl group, and n is 0 or 1, which has an Na—H exchange inhibiting activity, or a salt thereof exhibits excellent bioabsorbability and an Na—H exchange inhibiting activity superior to that of an oral preparation, thus being useful as a prophylactic and/or therapeutic agent for ischemic heart diseases such as myocardial infarct and arrhythmia.
摘要翻译： 一种鼻制剂，其包含由下式表示的化合物：其中环A是任选取代的5元或6元芳族杂环，环B是任选取代的5或6元芳族碳环或杂环，R 1， 是氢原子，羟基或低级烷基，n为0或1，其具有Na-H交换抑制活性，或其盐表现出优于生物吸收性和Na-H交换抑制活性优于 口服制剂，因此可用作缺血性心脏病例如心肌梗塞和心律失常的预防和/或治疗剂。
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公开(公告)号：US06429296B2
公开(公告)日：2002-08-06
申请号：US09767144
申请日：2001-01-23
申请人： Yutaka Yamagata , Masafumi Misaki , Susumu Iwasa
发明人： Yutaka Yamagata , Masafumi Misaki , Susumu Iwasa
IPC分类号： A61K3827
CPC分类号： A61K9/1647 , A61K38/27 , C07K14/61 , Y10S530/839
摘要： The present invention provides a complex of human growth hormone and zinc containing human growth hormone and zinc at a molar ratio of about 1:1.6 to about 1:2.4, and a sustained-release preparation which comprises the complex of human growth hormone and zinc and a biodegradable polymer and which has a high entrapment ratio of human growth hormone and exhibits a stable sustained-release suppressing the initial burst.
摘要翻译： 本发明提供人体生长激素和含锌人体生长激素和锌的复合物，其摩尔比为约1:1.6至约1:2.4，以及包含人生长激素和锌的复合物的缓释制剂和 可生物降解的聚合物，并且其具有高的人生长激素的截留比并表现出稳定的持续释放，抑制了初始爆发。
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