公开(公告)号：US09265730B2

公开(公告)日：2016-02-23

申请号：US14194050

申请日：2014-02-28

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Muneo Nonomura ,  Hiroki Ito ,  Hideo Hashimoto ,  Tadashi Urai

IPC: A61K9/16 ,  A61K9/24 ,  A61K9/48 ,  A61K31/4439 ,  A61K47/02

CPC classification number: A61K9/1676 ,  A61K9/209 ,  A61K9/4808 ,  A61K31/4439 ,  A61K47/02

Abstract: It is intended to provide a process for producing unstable amorphous benzimidazole compounds having a proton pump inhibitor function, and stable solid preparations for medicinal use containing these compounds which are produced by blending such an amorphous benzimidazole compound with a nontoxic base such as a basic inorganic salt, forming an intermediate coating layer on the layer containing the active ingredient and further forming an enteric coating layer or a release-controlling coating layer.

公开(公告)号：US09011926B2

公开(公告)日：2015-04-21

申请号：US14488823

申请日：2014-09-17

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Naoki Nagahara ,  Naoki Asakawa ,  Muneo Nonomura

IPC: A61K9/16 ,  B05D7/00 ,  A61K31/4439

CPC classification number: A61K9/1682 ,  A61J3/005 ,  A61K9/167 ,  A61K9/1676 ,  A61K9/1694 ,  A61K9/5078 ,  A61K31/4439 ,  B01J2/003

Abstract: In a production process of granules containing a biologically active substance, variation in the elution profile of the biologically active substance is reduced by heating the temperature of granules to about 50° C. or higher and maintaining the temperature for about 1 minute or longer. By setting the spray speed to about 90 mg/min or more per 1 g of cores when a spray agent for a primary agent containing the biologically active substance is sprayed while spraying a binding liquid to the cores and setting the total feeding weight per unit area for a centrifugal fluidized bed coating granulation machine to about 1.5 g/cm2 or more, the variation in the elution profile of the biologically active substance from the granules is reduced.

Abstract translation: 在含有生物活性物质的颗粒的生产方法中，通过将颗粒的温度加热至约50℃或更高并保持约1分钟或更长时间来降低生物活性物质的洗脱曲线的变化。 当喷雾含有生物活性物质的主剂的喷雾剂，同时喷涂粘合液体至核心并设定每单位面积的总进料重量时，通过将喷雾速度设定为每1g核心约90mg / min或更高 对于离心流化床包衣造粒机至约1.5g / cm 2或更高，来自颗粒的生物活性物质的洗脱曲线的变化减小。

公开(公告)号：US20130261156A1

公开(公告)日：2013-10-03

申请号：US13905090

申请日：2013-05-29

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Yasuhiro Hiraishi ,  Muneo Nonomura

IPC: A61K47/12 ,  A61K47/10 ,  A61K47/02

CPC classification number: A61K47/12 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2853 ,  A61K9/2866 ,  A61K31/4427 ,  A61K47/02 ,  A61K47/10

Abstract: The present invention provides a pharmaceutical composition or a solid preparation containing a stabilized pharmaceutically active ingredient and a stabilizing method thereof.According to the present invention, a pharmaceutical composition can be stabilized by containing a nonpeptidic pharmaceutically active ingredient having a primary or secondary amino group, an excipient and an acidic compound. In addition, a solid preparation containing a pharmaceutically active ingredient, titanium oxide, a plasticizer and a chain organic acid can enhance the stability of the pharmaceutically active ingredient during light irradiation.

Abstract translation: 本发明提供含有稳定的药物活性成分的药物组合物或固体制剂及其稳定化方法。 根据本发明，可以通过含有具有伯氨基或仲氨基的非肽类药物活性成分，赋形剂和酸性化合物来稳定药物组合物。 此外，含有药物活性成分，氧化钛，增塑剂和链状有机酸的固体制剂可以在光照射期间增强药物活性成分的稳定性。