公开(公告)号：US06753330B2

公开(公告)日：2004-06-22

申请号：US10414008

申请日：2003-04-16

申请人： Niichiro Takano ,  Hiroyuki Kawashima ,  Yasuo Shinoda ,  Toshio Inagi

发明人： Niichiro Takano ,  Hiroyuki Kawashima ,  Yasuo Shinoda ,  Toshio Inagi

IPC分类号： A61K3150

CPC分类号： A61K9/1652 ,  A61K9/146 ,  A61K9/1641 ,  A61K9/2077 ,  A61K31/50

摘要： The invention provides a solid dispersion composition containing 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H-pyridazin-3-one, hydroxypropylmethyl cellulose, and polyoxyethylene polyoxypropylene glycol. The solid dispersion composition of the present invention exhibits the excellent dissolvability of 2-benzyl-5-(4-chlorophenyl)-6-[4-(methylthio)phenyl]-2H-pyridazin-3-one in water, and enables this compound to be constant sequentially and thereby improve absorbability in blood.

摘要翻译： 本发明提供了含有2-苄基-5-（4-氯苯基）-6- [4-（甲硫基）苯基] -2H-哒嗪-3-酮，羟丙基甲基纤维素和聚氧乙烯聚氧丙烯二醇的固体分散体组合物。 本发明的固体分散体组合物表现出2-苄基-5-（4-氯苯基）-6- [4-（甲硫基）苯基] -2H-哒嗪-3-酮在水中的优异的溶解性，使该化合物 依次保持恒定，从而提高血液中的吸收性。

公开(公告)号：US08101207B2

公开(公告)日：2012-01-24

申请号：US10551901

申请日：2004-04-28

申请人： Hiroshi Miura ,  Makoto Kanebako ,  Masayuki Kanishi ,  Yasuo Shinoda ,  Toshio Inagi ,  Hirofumi Takeuchi

发明人： Hiroshi Miura ,  Makoto Kanebako ,  Masayuki Kanishi ,  Yasuo Shinoda ,  Toshio Inagi ,  Hirofumi Takeuchi

IPC分类号： A61K9/20 ,  A61K47/02 ,  A61K47/04 ,  A61K31/50

CPC分类号： A61K31/50 ,  A61K9/1611 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2095

摘要： A composition containing a very low water-soluble drug, which composition is produced by treating, with a supercritical or subcritical carbon dioxide fluid, a mixture containing a very low water-soluble drug and a porous material (exclusive of a porous silica material characterized in that the material has an average pore diameter of 1 to 20 nm, the total pore volume of the material that have a diameter falling within a range of ±40% of the average pore diameter account for 60% or more the volume of all the pores of the material, and, when subjected to X-ray diffractometry, the material exhibits one or more peaks at a diffraction angle (2θ) corresponding to d of 1 nm or more); and a method for producing the composition.The very-low-water-soluble-drug-containing composition of the present invention ensures improved dissolution of the very low water-soluble drug.

摘要翻译： 含有非常低水溶性药物的组合物，该组合物通过用超临界或亚临界二氧化碳流体处理含有非常低水溶性药物和多孔材料的混合物（不包括多孔二氧化硅材料 该材料的平均孔径为1〜20nm，直径在平均孔径的±40％范围内的材料的总孔体积占所有孔的体积的60％以上 的材料，当进行X射线衍射测定时，该材料在对应于d的衍射角（2θ）为1nm以上）表现出一个以上的峰值。 以及该组合物的制造方法。 本发明的非常低水溶性药物的组合物确保极低水溶性药物的溶出度得到改善。

公开(公告)号：US20070128273A1

公开(公告)日：2007-06-07

申请号：US10551901

申请日：2004-04-28

申请人： Hiroshi Miura ,  Makoto Kanebako ,  Masayuki Kanishi ,  Yasuo Shinoda ,  Toshio Inagi ,  Hirofumi Takeuchi

发明人： Hiroshi Miura ,  Makoto Kanebako ,  Masayuki Kanishi ,  Yasuo Shinoda ,  Toshio Inagi ,  Hirofumi Takeuchi

IPC分类号： A61K9/20

CPC分类号： A61K31/50 ,  A61K9/1611 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2095

摘要： A composition containing a very low water-soluble drug, which composition is produced by treating, with a supercritical or subcritical carbon dioxide fluid, a mixture containing a very low water-soluble drug and a porous material (exclusive of a porous silica material characterized in that the material has an average pore diameter of 1 to 20 nm, the total pore volume of the material that have a diameter falling within a range of ±40% of the average pore diameter account for 60% or more the volume of all the pores of the material, and, when subjected to X-ray diffractometry, the material exhibits one or more peaks at a diffraction angle (2θ) corresponding to d of 1 nm or more); and a method for producing the composition. The very-low-water-soluble-drug-containing composition of the present invention ensures improved dissolution of the very low water-soluble drug.

摘要翻译： 含有非常低水溶性药物的组合物，该组合物通过用超临界或亚临界二氧化碳流体处理含有非常低水溶性药物和多孔材料的混合物（不包括多孔二氧化硅材料 该材料的平均孔径为1〜20nm，直径在平均孔径的±40％范围内的材料的总孔体积占所有孔的体积的60％以上 的材料，并且当进行X射线衍射测定时，该材料在对应于d为1nm以上的衍射角（2θ）处表现出一个或多个峰）; 以及该组合物的制造方法。 本发明的非常低水溶性药物的组合物确保极低水溶性药物的溶出度得到改善。

公开(公告)号：US20050239868A1

公开(公告)日：2005-10-27

申请号：US10521958

申请日：2003-07-22

申请人： Hiroyuki Shirai ,  Tatsuya Nakai ,  Masami Serizawa ,  Yasuo Shinoda ,  Toshio Inagi

发明人： Hiroyuki Shirai ,  Tatsuya Nakai ,  Masami Serizawa ,  Yasuo Shinoda ,  Toshio Inagi

IPC分类号： A61K9/06 ,  A61K31/405 ,  A61K47/02 ,  A61K47/10 ,  A61K47/14 ,  A61K47/32 ,  A61K47/38 ,  A61K47/44 ,  A61P29/00

CPC分类号： A61K9/06 ,  A61K9/0014 ,  A61K31/405 ,  A61K47/02 ,  A61K47/10 ,  A61K47/14 ,  A61K47/32 ,  A61K47/38 ,  A61K47/44

摘要： An object of the present invention is to provide an indomethacin external preparation that has an excellent use feeling and excellent absorbability and causes no phase separation into an oil layer and an aqueous layer, thus exhibiting satisfactory stability of preparation with time. Provided is an indomethacin external preparation containing: 0.1 to 3 wt % of indomethacin; 25 to 50 wt % of alcohol; 0.01 to 5 wt % of gelling agent; 5 to 30 wt % of oil component; 20 to 50 wt % of water; and 0.01 to 10 wt % of one or more components selected from the group consisting of glyceryl monostearate, sorbitan monostearate, stearyl alcohol, and polyethylene glycol monostearate.

摘要翻译： 本发明的目的是提供具有优异的使用感和优异的吸收性的吲哚美辛外用制剂，并且不会使相分离成油层和水层，从而表现出令人满意的制备时间稳定性。 本发明提供消炎痛外用制剂，含有0.1〜3重量％的吲哚美辛; 25〜50重量％的醇; 0.01〜5重量％的胶凝剂; 5〜30重量％的油成分; 20〜50重量％的水; 和0.01〜10重量％的选自单硬脂酸甘油酯，脱水山梨糖醇单硬脂酸酯，硬脂醇和聚乙二醇单硬脂酸酯的一种或多种成分。

公开(公告)号：US07553865B2

公开(公告)日：2009-06-30

申请号：US10521958

申请日：2003-07-22

申请人： Hiroyuki Shirai ,  Tatsuya Nakai ,  Masami Serizawa ,  Yasuo Shinoda ,  Toshio Inagi

发明人： Hiroyuki Shirai ,  Tatsuya Nakai ,  Masami Serizawa ,  Yasuo Shinoda ,  Toshio Inagi

IPC分类号： A61K31/40 ,  A01N43/38 ,  C07D209/26

CPC分类号： A61K9/06 ,  A61K9/0014 ,  A61K31/405 ,  A61K47/02 ,  A61K47/10 ,  A61K47/14 ,  A61K47/32 ,  A61K47/38 ,  A61K47/44

摘要： An object of the present invention is to provide an indomethacin external preparation that has an excellent use feeling and excellent absorbability and causes no phase separation into an oil layer and an aqueous layer, thus exhibiting satisfactory stability of preparation with time. Provided is an indomethacin external preparation containing: 0.1 to 3 wt % of indomethacin; 25 to 50 wt % of alcohol; 0.01 to 5 wt % of gelling agent; 5 to 30 wt % of oil component; 20 to 50 wt % of water; and 0.01 to 10 wt % of one or more components selected from the group consisting of glyceryl monostearate, sorbitan monostearate, stearyl alcohol, and polyethylene glycol monostearate.

摘要翻译： 本发明的目的是提供具有优异的使用感和优异的吸收性的吲哚美辛外用制剂，并且不会使相分离成油层和水层，从而表现出令人满意的制备时间稳定性。 本发明提供消炎痛外用制剂，含有0.1〜3重量％的吲哚美辛; 25〜50重量％的醇; 0.01〜5重量％的胶凝剂; 5〜30重量％的油成分; 20〜50重量％的水; 和0.01〜10重量％的选自单硬脂酸甘油酯，脱水山梨糖醇单硬脂酸酯，硬脂醇和聚乙二醇单硬脂酸酯的一种或多种成分。

公开(公告)号：US06465477B1

公开(公告)日：2002-10-15

申请号：US09436789

申请日：1999-11-08

申请人： Toyojiro Muramatsu ,  Katsumi Mashita ,  Yasuo Shinoda ,  Hironori Sassa ,  Hiroyuki Kawashima ,  Yoshio Tanizawa ,  Hideatsu Takeuchi

发明人： Toyojiro Muramatsu ,  Katsumi Mashita ,  Yasuo Shinoda ,  Hironori Sassa ,  Hiroyuki Kawashima ,  Yoshio Tanizawa ,  Hideatsu Takeuchi

IPC分类号： A61K31435

CPC分类号： A61K31/44 ,  A61K31/19 ,  A61K31/435 ,  Y10S514/97

摘要： Disclosed is a pharmaceutical composition comprising (E)-3,5-dihydroxy-7-[4′-4″-fluorophenyl-2′-cyclopropyl-quinolin-3′-yl]-6-heptenoic acid, or its salt or ester, of which the aqueous solution or dispersion has pH of from 6.8 to 8. The composition has good time-dependent stability and has no change in its outward appearance even after having been stored long.

摘要翻译： 公开了一种药物组合物，其包含（E）-3,5-二羟基-7- [4'-4“ - 氟苯基-2'-环丙基 - 喹啉-3'-基] -6-庚烯酸或其盐或 酯，其水溶液或分散体的pH为6.8至8.该组合物具有良好的时间依赖性稳定性，即使在长时间储存​​后也不会改变其外观。