公开(公告)号：US5972373A

公开(公告)日：1999-10-26

申请号：US945822

申请日：1997-10-31

申请人： Toshio Yajima ,  Kuniaki Ishii ,  Shigeru Itai ,  Masami Nemoto ,  Kouji Suetake ,  Nobuyoshi Tsukui

发明人： Toshio Yajima ,  Kuniaki Ishii ,  Shigeru Itai ,  Masami Nemoto ,  Kouji Suetake ,  Nobuyoshi Tsukui

IPC分类号： A61K9/00 ,  A61K9/16 ,  A61K9/10 ,  A61K47/26 ,  A61K47/32

CPC分类号： A61K9/0095 ,  A61K9/1617 ,  A61K9/1635 ,  Y10S514/974

摘要： [Object] To provide a composition for oral administration which is excellent in masking a taste of an unpleasant tasting drug and in bioavailability.[Constitution] A composition for oral administration comprising an unpleasantly tasting drug, a high polymer soluble in the stomach and a monoglyceride in the .beta.-crystal form.

摘要翻译： PCT No.PCT / JP96 / 01179 Sec。 371日期1997年10月31日 102（e）日期1997年10月31日PCT 1996年4月30日PCT PCT。 出版物WO96 / 34628 PCT 日期：1996年11月7日[目的]提供一种口服给药的组合物，该组合物在掩蔽不愉快的品尝药物的味道和生物利用度方面是优异的。 [组成]口服给药的组合物，其包含不愉快的品尝药物，可溶于胃的高聚物和β-晶型的单甘油酯。

公开(公告)号：US5328903A

公开(公告)日：1994-07-12

申请号：US016576

申请日：1993-02-10

申请人： Kuniaki Ishii ,  Yumiko Toriumi ,  Shigeru Itai ,  Hidefumi Hayashi ,  Masami Nemoto

发明人： Kuniaki Ishii ,  Yumiko Toriumi ,  Shigeru Itai ,  Hidefumi Hayashi ,  Masami Nemoto

IPC分类号： A61K9/16 ,  A61K9/20 ,  A61K31/59 ,  A61K47/26 ,  A61K47/32 ,  A61K47/38 ,  A61P3/02 ,  A61K31/595 ,  A61K9/36 ,  A61K31/58

CPC分类号： A61K31/59 ,  A61K9/2018 ,  A61K9/2054 ,  Y10S514/96 ,  Y10S514/961

摘要： A composition for solid pharmaceutical preparations containing a vitamin D.sub.3 derivative capable of permitting the derivative to be uniformly distributed in the composition while being stabilized. The composition contains an excipient consisting of mannitol and sugar, a degradative agent consisting of hydroxypropyl cellulose, and a binder consisting of polyvinyl pyrrolidone and hydroxypropylmethyl cellulose.

摘要翻译： 一种含有维生素D3衍生物的固体药物制剂的组合物，其能够使该衍生物均匀地分布在组合物中，同时稳定。 该组合物含有由甘露糖醇和糖组成的赋形剂，由羟丙基纤维素组成的降解剂和由聚乙烯吡咯烷酮和羟丙基甲基纤维素组成的粘合剂。

公开(公告)号：US08231899B2

公开(公告)日：2012-07-31

申请号：US10758233

申请日：2004-01-13

申请人： Poul Egon Bertelsen ,  Niels Gjørløv Hansen ,  Hermann Ruckendorfer ,  Shigeru Itai

发明人： Poul Egon Bertelsen ,  Niels Gjørløv Hansen ,  Hermann Ruckendorfer ,  Shigeru Itai

IPC分类号： A61K9/20 ,  A61K9/14

CPC分类号： A61K9/1617 ,  A61K9/1611 ,  A61K9/1652

摘要： The present invention relates to an oral modified release pharmaceutical composition for the administration of a therapeutically and/or prophylactically effective amount of an active substance (a drug substance) to obtain a relatively fast or quick onset of the therapeutic and/or prophylactic effect. The drug substances contained in a modified release pharmaceutical composition according to the invention are suitably a drug substance which has a very low solubitity under acidic conditions, i.e. under conditions similar to those present in the stomach and/or drug substances which have a pKa value below about 5.5 such as in a range of from about 4 to about 5. The composition is based on a powder comprising a therapeutically and/or prophylactically active substance and has such a particle size that: when the powder is subjected to a sieve analysis, then at least about 90% w/w of the particles passes through sieves 180 μm and the powder is contacted with an aqueous medium to form a particulate composition, which has such a particle size that when the particulate composition is subjected to a sieve analysis, then at least about 50% w/w of the particles passes through sieve 180 μm. Furthermore, the composition, when tested in accordance with the dissolution method (I) defined herein employing 0.07 N hydrochloric acid as dissolution medium, releases at least about 50% w/w of the active substance within the first 20 min of the test.

摘要翻译： 本发明涉及用于给予治疗和/或预防有效量的活性物质（药物物质）以获得治疗和/或预防效果相对快速或快速发作的口服释放药物组合物。 包含在根据本发明的调释释放药物组合物中的药物物质合适地是在酸性条件下具有非常低的溶解度的药物物质，即在与pKa值低于pKa值的胃和/或药物物质中存在的条件相似的条件下 约5.5，例如在约4至约5的范围内。该组合物基于包含治疗和/或预防活性物质的粉末，并且具有如下的粒径：当粉末进行筛分分析时，则 至少约90％w / w的颗粒通过180μm的筛子，并且粉末与水性介质接触以形成颗粒组合物，其具有这样的颗粒尺寸，即当颗粒组合物进行筛分分析时， 颗粒的至少约50％w / w通过筛180μm。 此外，当根据本文定义的溶解方法（I）使用0.07N盐酸作为溶解介质测试时，组合物在试验的最初20分钟内释放至少约50％w / w的活性物质。

公开(公告)号：US20050147668A1

公开(公告)日：2005-07-07

申请号：US10758233

申请日：2004-01-13

申请人： Poul Bertelsen ,  Niels Hansen ,  Hermann Ruckendorfer ,  Shigeru Itai

发明人： Poul Bertelsen ,  Niels Hansen ,  Hermann Ruckendorfer ,  Shigeru Itai

IPC分类号： A61K9/16 ,  A61K9/20

CPC分类号： A61K9/1617 ,  A61K9/1611 ,  A61K9/1652

摘要： The present invention relates to an oral modified release pharmaceutical composition for the administration of a therapeutically and/or prophylactically effective amount of an active substance (a drug substance) to obtain a relatively fast or quick onset of the therapeutic and/or prophylactic effect The drug substances contained in a modified release pharmaceutical composition according to the invention are suitably a drug substance which has a very low solubitity under acidic conditions, i.e. under conditions similar to those present in the stomach and/or drug substances which have a pKa value below about 5.5 such as in a range of from about 4 to about 5. The composition is based on a powder comprising a therapeutically and/or prophylactically active substance and has such a particle size that when the powder is subjected to a sieve analysis, then at least about 90% w/w of the particles passes through sieves 180 μm and the powder is contacted with an aqueous medium to form a particulate composition, which has such a particle size that when the particulate composition is subjected to a sieve analysis, then at least about 50% w/w of the particles passes through sieve 180 μm. Furthermore, the composition, when tested in accordance with the dissolution method (1) defined herein employing 0.07 N hydrochloric acid as dissolution medium, releases at least about 50% w/w of the active substance within the first 20 min of the test

摘要翻译： 本发明涉及一种用于给予治疗和/或预防有效量的活性物质（药物）以获得相对快速或快速起效的治疗和/或预防效果的口服释放药物组合物。该药物 根据本发明的改性释放药物组合物中所含的物质适宜地是在酸性条件下具有非常低的溶解性的药物物质，即在与胃和/或药物物质中存在pK < 低于约5.5，例如在约4至约5的范围内。该组合物基于包含治疗和/或预防活性物质的粉末，并且具有这样的粒径，即当粉末经受 进行筛分分析，然后至少约90％w / w的颗粒通过筛子180μm，粉末与水性介质接触以形成 颗粒组合物具有这样的颗粒尺寸，当颗粒组合物进行筛分分析时，至少约50％w / w的颗粒通过筛子180μm。 此外，当根据本文定义的溶解方法（1）使用0.07N盐酸作为溶解介质测试时，组合物在试验的最初20分钟内释放至少约50％w / w的活性物质

公开(公告)号：US06713089B1

公开(公告)日：2004-03-30

申请号：US09786864

申请日：2001-07-10

申请人： Poul Bertelsen ,  Niels Gjørløv Hansen ,  Hermann Ruckendorfer ,  Shigeru Itai

发明人： Poul Bertelsen ,  Niels Gjørløv Hansen ,  Hermann Ruckendorfer ,  Shigeru Itai

IPC分类号： A61K914

CPC分类号： A61K9/2009 ,  A61K9/1611

摘要： The present invention relates to an oral modified release pharmaceutical composition for the administration of a therapeutically and/or prophylactically effective amount of an active substance (a drug substance), to obtain a relatively fast or quick onset of the therapeutic and/or prophylactic effect. The drug substances contained in a modified release pharmaceutical composition according to the invention are suitably a drug substance which has a pKa value below about 5, such as in a range of from about 4 to about 5. The composition is based on a powder comprising a therapeutically and/or prophylactically active substance and has such a particle size that: when the powder is subjected to a sieve analysis, then at least about 90% w/w of the particles pass through a 180 micron sieve, and when the powder is contacted with an aqueous medium to form a particulate composition, which as such a particle size that when the particulate composition is subjected to a sieve analysis, then at least about 50% w/w of the particles passes through a 180 micron sieve. Further more, the composition, when tested in accordance with the dissolution method (I) defines herein, employing 0.07 HCl as dissolution medium, release at least about 50% w/w of the active substance within the first 20 minutes of the test.

摘要翻译： 本发明涉及用于给予治疗和/或预防有效量的活性物质（药物物质）的口服释放药物组合物，以获得治疗和/或预防效果的相对快速或快速的发作。 包含在根据本发明的改性释放药物组合物中的药物物质合适地是pKa值低于约5，例如在约4至约5范围内的药物。该组合物基于包含 治疗和/或预防活性物质，并且具有这样的粒度：当粉末进行筛分分析时，然后至少约90％w / w的颗粒通过180微米筛，并且当粉末接触时 与水性介质形成颗粒组合物，其颗粒大小使得当颗粒组合物进行筛分分析时，至少约50％w / w的颗粒通过180微米筛。 此外，当根据本文的溶解方法（I）测试时，组合物使用0.07HCl作为溶解介质，在测试的前20分钟内释放至少约50％w / w的活性物质。

公开(公告)号：US5707646A

公开(公告)日：1998-01-13

申请号：US295672

申请日：1994-09-09

申请人： Toshio Yajima ,  Kuniaki Ishii ,  Nobuo Umeki ,  Shigeru Itai ,  Hidefumi Hayashi ,  Kimihide Shimano ,  Ikuo Koyama

发明人： Toshio Yajima ,  Kuniaki Ishii ,  Nobuo Umeki ,  Shigeru Itai ,  Hidefumi Hayashi ,  Kimihide Shimano ,  Ikuo Koyama

IPC分类号： A61K9/14 ,  A61K20060101 ,  A61K9/00 ,  A61K9/10 ,  A61K9/16 ,  A61K31/70 ,  A61K31/7048 ,  A61K47/02 ,  A61K47/04 ,  A61K47/10 ,  A61K47/30 ,  A61K47/32 ,  A61K47/44

CPC分类号： A61K9/1617 ,  A61K9/0095 ,  A61K9/1635 ,  Y10S514/974

摘要： A composition for oral preparations, having a complex formed by dispersing or dissolving an unpleasantly tasting basic drug and a functional polymer compound in a substance having a low melting point, 10 to 70% by weight, based on the composition, of sugar alcohol and 0.1 to 7% by weight, based on the composition, of basic oxide. The composition for oral preparation is excellent in masking unpleasantly tasting basic drugs and has excellent performance in biological use.

摘要翻译： PCT No.PCT / JP93 / 00291 Sec。 371日期1994年9月9日 102（e）1994年9月9日PCT 1993年3月10日PCT公布。 公开号WO93 / 17667 日本1993年9月16日一种口服制剂的组合物，其具有通过将不愉快的品尝碱性药物和功能性高分子化合物分散或溶解在基于组合物的10〜70重量％的低熔点物质中形成的复合物， 的糖醇和0.1〜7重量％，基于组成，碱性氧化物。 用于口服制剂的组合物在掩蔽令人不愉快的基本药物中具有优异的性能，并且在生物学应用中具有优异的性能。