公开(公告)号：US08343548B2

公开(公告)日：2013-01-01

申请号：US11888529

申请日：2007-08-01

申请人： Fumie Kusaki ,  Takafumi Hoshino ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

发明人： Fumie Kusaki ,  Takafumi Hoshino ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

IPC分类号： A61K9/14 ,  A61K9/50

CPC分类号： A61K9/1652 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/44

摘要： Provided are a solid dosage form comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising an enteric solid dispersion comprising a poorly soluble drug, an enteric polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising an enteric solid dispersion, the method comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g and serving as a disintegrant; and granulating the resultant; and drying.

摘要翻译： 提供了一种固体剂型，其包含允许制剂中的药物快速溶解而不损害固体分散体的溶解性的肠溶固体分散体及其制备方法。 更具体地，提供了包含包含难溶性药物，肠溶性聚合物和崩解剂的肠溶性固体分散体的固体剂型，其中所述崩解剂是平均粒径为10〜100μm的低取代羟丙基纤维素，比表面积 通过BET法测量为至少1.0m 2 / g。 此外，提供了一种生产包含肠溶固体分散体的固体剂型的方法，所述方法包括以下步骤：将难溶性药物已经分散或溶解的肠溶性聚合物溶液喷雾到具有 平均粒径为10〜100μm，BET法测定的比表面积为1.0m 2 / g以上，作为崩解剂; 并造成结果; 并干燥。

公开(公告)号：US08343547B2

公开(公告)日：2013-01-01

申请号：US11888445

申请日：2007-08-01

申请人： Takafumi Hoshino ,  Fumie Kusaki ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

发明人： Takafumi Hoshino ,  Fumie Kusaki ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

IPC分类号： A61K9/14 ,  A61K9/50

CPC分类号： A61K9/2054 ,  A61K31/44

摘要： Provided are a solid dosage form comprising a solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising a solid dispersion, the dispersion comprising: a poorly soluble drug, a water-soluble polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising a solid dispersion, the method comprising steps of: spraying a water-soluble polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g and serving as a disintegrant and granulating the resultant; and drying.

摘要翻译： 提供了一种固体剂型及其制备方法，该固体分散体允许制剂中的药物快速溶解而不损害固体分散体的溶解性。 更具体地，提供了包含固体分散体的固体剂型，所述分散体包含：难溶性药物，水溶性聚合物和崩解剂，其中所述崩解剂是平均粒度为10至100μm的低取代羟丙基纤维素 并且通过BET法测量的比表面积为至少1.0m 2 / g。 此外，提供了一种制备包含固体分散体的固体剂型的方法，所述方法包括以下步骤：将难溶性药物已经分散或溶解的水溶性聚合物溶液喷雾到低取代羟丙基纤维素粉末上 平均粒径为10〜100μm，BET法测定的比表面积为1.0m 2 / g以上，作为崩解剂造粒， 并干燥。

公开(公告)号：US20080038339A1

公开(公告)日：2008-02-14

申请号：US11888445

申请日：2007-08-01

申请人： Takafumi Hoshino ,  Fumie Kusaki ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

发明人： Takafumi Hoshino ,  Fumie Kusaki ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

IPC分类号： A61K9/10 ,  A61K47/30 ,  A61K47/38

CPC分类号： A61K9/2054 ,  A61K31/44

摘要： Provided are a solid dosage form comprising a solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising a solid dispersion, the dispersion comprising: a poorly soluble drug, a water-soluble polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising a solid dispersion, the method comprising steps of: spraying a water-soluble polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g and serving as a disintegrant and granulating the resultant; and drying.

摘要翻译： 提供了一种固体剂型及其制备方法，该固体分散体允许制剂中的药物快速溶解而不损害固体分散体的溶解性。 更具体地，提供了包含固体分散体的固体剂型，所述分散体包含：难溶性药物，水溶性聚合物和崩解剂，其中所述崩解剂是平均粒度为10至100μm的低取代羟丙基纤维素 并且通过BET法测量的比表面积为至少1.0m 2 / g。 此外，提供了一种制备包含固体分散体的固体剂型的方法，所述方法包括以下步骤：将难溶性药物已经分散或溶解的水溶性聚合物溶液喷雾到低取代羟丙基纤维素粉末上 平均粒径为10〜100μm，通过BET法测定的比表面积为至少1.0m 2 / g，作为崩解剂，造粒; 并干燥。

公开(公告)号：US20080038340A1

公开(公告)日：2008-02-14

申请号：US11888529

申请日：2007-08-01

申请人： Fumie Kusaki ,  Takafumi Hoshino ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

发明人： Fumie Kusaki ,  Takafumi Hoshino ,  Naosuke Maruyama ,  Yuichi Nishiyama ,  Ikuo Fukui ,  Hiroshi Umezawa

IPC分类号： A61K9/10 ,  A61K47/30 ,  A61K47/38

CPC分类号： A61K9/1652 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/44

摘要： Provided are a solid dosage form comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising an enteric solid dispersion comprising a poorly soluble drug, an enteric polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g. Moreover, provided is a method for producing a solid dosage form comprising an enteric solid dispersion, the method comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 μm and a specific surface area measured by BET method of at least 1.0 m2/g and serving as a disintegrant; and granulating the resultant; and drying.

摘要翻译： 提供了一种固体剂型，其包含允许制剂中的药物快速溶解而不损害固体分散体的溶解性的肠溶固体分散体及其制备方法。 更具体地，提供了一种固体剂型，其包含包含难溶性药物，肠溶性聚合物和崩解剂的肠溶固体分散体，其中所述崩解剂是平均粒度为10至100μm的低取代羟丙基纤维素和比表面积 通过BET法测量为至少1.0m 2 / g。 此外，提供了一种生产包含肠溶固体分散体的固体剂型的方法，所述方法包括以下步骤：将难溶性药物已经分散或溶解的肠溶性聚合物溶液喷雾到具有 平均粒径为10〜100μm，通过BET法测定的比表面积为至少1.0m 2 / g，作为崩解剂; 并造成结果; 并干燥。

公开(公告)号：US08354122B2

公开(公告)日：2013-01-15

申请号：US11736834

申请日：2007-04-18

申请人： Takafumi Hoshino ,  Fumie Kusaki ,  Ikuo Fukui

发明人： Takafumi Hoshino ,  Fumie Kusaki ,  Ikuo Fukui

IPC分类号： A61K9/20

CPC分类号： B05D1/02 ,  A61J3/005 ,  A61K9/146 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/167 ,  A61K9/2077 ,  A61K31/4422

摘要： Provided are a granule or a tablet of a solid dispersion that allows a drug in a preparation to be rapidly dissolved without impairing the dissolution of the solid dispersion, and a method for producing the same. More specifically, provided are a granule of a solid dispersion comprising a poorly soluble drug, a water-soluble polymer, an excipient and a disintegrator, wherein a content of the water-soluble polymer is 1 to 10% by weight and a content of the disintegrator is 15 to 50% by weight; a tablet of a solid dispersion comprising a poorly soluble drug, a water-soluble polymer, an excipient and a disintegrator, wherein a content of the water-soluble polymer is 1 to 5% by weight and a content of the disintegrator is 15 to 50% by weight; and a method for producing a granule or tablet of a solid dispersion comprising spraying a water-soluble polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a mixed powder of an excipient and a disintegrator, and granulating and drying a resultant.

摘要翻译： 提供一种固体分散体的颗粒或片剂，其允许制剂中的药物快速溶解而不损害固体分散体的溶解，及其制备方法。 更具体地，提供了包含难溶性药物，水溶性聚合物，赋形剂和崩解剂的固体分散体的颗粒，其中水溶性聚合物的含量为1〜10重量％，含量为 崩解剂为15〜50重量％ 包含难溶性药物，水溶性聚合物，赋形剂和崩解剂的固体分散体片剂，其中所述水溶性聚合物的含量为1〜5重量％，所述崩解剂的含量为15〜50 重量％ 以及制备固体分散体的颗粒或片剂的方法，包括将难溶性药物已经分散或溶解的水溶性聚合物溶液喷雾到赋形剂和崩解剂的混合粉末上，并将所得物 。

公开(公告)号：US20070292509A1

公开(公告)日：2007-12-20

申请号：US11764084

申请日：2007-06-15

申请人： Mutsunori Tanji ,  Tadashi Matsui ,  Shuichiro Yuasa ,  Yuichi Nishiyama ,  Yuichi Ito ,  Ikuo Fukui

发明人： Mutsunori Tanji ,  Tadashi Matsui ,  Shuichiro Yuasa ,  Yuichi Nishiyama ,  Yuichi Ito ,  Ikuo Fukui

IPC分类号： A61K9/26

CPC分类号： A61K9/1688 ,  A61K9/1652 ,  A61K9/5026 ,  A61K9/5042 ,  A61K9/5073

摘要： The present invention is an enteric coated granule having controlled dissolution in water even at a small coating amount; and a preparation method thereof. More specifically, provided are an enteric coated granule comprising a raw granule or a granule comprising a raw granule and at least one layer covering the raw granule, a first enteric layer covering the raw granule or the granule, and a second enteric layer formed over the first enteric layer, wherein the first and the second enteric layers comprise a first and a second hydroxypropylmethyl cellulose acetate succinates (HPMCASs) different in solubility pH, respectively, and the solubility pH value of the second HPMCAS of the second enteric layer is lower than that of the first enteric layer; and a preparation method comprising steps of covering a raw granule or a granule comprising a raw granule and at least one layer covering the raw granule with an enteric coating agent comprising a first HPMCAS to form a first enteric layer; and forming, over the first enteric layer, a second coating layer by using a second enteric coating agent comprising a second HPMCAS having a lower solubility pH value than that of the first HPMCAS.

摘要翻译： 本发明是即使以小的涂布量控制溶解在水中的肠溶衣颗粒剂; 及其制备方法。 更具体地，提供一种肠溶包衣颗粒，其包含原料颗粒或颗粒，其包含原料颗粒和覆盖原料颗粒的至少一层，覆盖原料颗粒或颗粒的第一肠溶层和形成在该颗粒上的第二肠溶层 第一肠溶层，其中第一和第二肠溶层分别包含溶解度pH不同的第一和第二羟丙基甲基纤维素乙酸酯琥珀酸酯（HPMCAS），第二肠溶层的第二HPMCAS的溶解度pH值低于第二肠溶层的溶解度pH值 的第一肠溶层; 以及包括以下步骤的方法，其包括用包含原料颗粒的原料颗粒或包含原料颗粒的至少一层的颗粒与包含第一HPMCAS的肠溶包衣剂一起覆盖以形成第一肠溶层; 并且通过使用包含比第一HPMCAS具有更低的溶解度pH值的第二HPMCAS的第二肠溶包衣剂，在第一肠溶层上形成第二涂层。

公开(公告)号：US09095513B2

公开(公告)日：2015-08-04

申请号：US11764084

申请日：2007-06-15

申请人： Mutsunori Tanji ,  Tadashi Matsui ,  Shuichiro Yuasa ,  Yuichi Nishiyama ,  Yuichi Ito ,  Ikuo Fukui

发明人： Mutsunori Tanji ,  Tadashi Matsui ,  Shuichiro Yuasa ,  Yuichi Nishiyama ,  Yuichi Ito ,  Ikuo Fukui

IPC分类号： A61K9/16 ,  A61K9/50

CPC分类号： A61K9/1688 ,  A61K9/1652 ,  A61K9/5026 ,  A61K9/5042 ,  A61K9/5073

摘要： The present invention is an enteric coated granule having controlled dissolution in water even at a small coating amount; and a preparation method thereof. More specifically, provided are an enteric coated granule comprising a raw granule or a granule comprising a raw granule and at least one layer covering the raw granule, a first enteric layer covering the raw granule or the granule, and a second enteric layer formed over the first enteric layer, wherein the first and the second enteric layers comprise a first and a second hydroxypropylmethyl cellulose acetate succinates (HPMCASs) different in solubility pH, respectively, and the solubility pH value of the second HPMCAS of the second enteric layer is lower than that of the first enteric layer; and a preparation method comprising steps of covering a raw granule or a granule comprising a raw granule and at least one layer covering the raw granule with an enteric coating agent comprising a first HPMCAS to form a first enteric layer; and forming, over the first enteric layer, a second coating layer by using a second enteric coating agent comprising a second HPMCAS having a lower solubility pH value than that of the first HPMCAS.

摘要翻译： 本发明是即使以小的涂布量控制溶解在水中的肠溶衣颗粒剂; 及其制备方法。 更具体地，提供一种肠溶包衣颗粒，其包含原料颗粒或颗粒，其包含原料颗粒和覆盖原料颗粒的至少一层，覆盖原料颗粒或颗粒的第一肠溶层和形成在该颗粒上的第二肠溶层 第一肠溶层，其中第一和第二肠溶层分别包含溶解度pH不同的第一和第二羟丙基甲基纤维素乙酸琥珀酸酯（HPMCAS），第二肠溶层的第二HPMCAS的溶解度pH值低于第二肠溶层的溶解度pH值 的第一肠溶层; 以及包括以下步骤的方法，其包括用包含原料颗粒的原料颗粒或包含原料颗粒的至少一层的颗粒与包含第一HPMCAS的肠溶包衣剂一起覆盖以形成第一肠溶层; 并且通过使用包含比第一HPMCAS具有更低的溶解度pH值的第二HPMCAS的第二肠溶包衣剂，在第一肠溶层上形成第二涂层。

公开(公告)号：US5583244A

公开(公告)日：1996-12-10

申请号：US551807

申请日：1995-11-07

申请人： Satoshi Uchida ,  Akira Yamamoto ,  Ikuo Fukui ,  Mikio Endo ,  Hiroshi Umezawa ,  Shigehiro Nagura ,  Tohru Kubota

发明人： Satoshi Uchida ,  Akira Yamamoto ,  Ikuo Fukui ,  Mikio Endo ,  Hiroshi Umezawa ,  Shigehiro Nagura ,  Tohru Kubota

IPC分类号： C08B37/00 ,  C08G77/42 ,  C07F7/10

CPC分类号： C08B37/0018 ,  C08G77/42

摘要： Disclosed is a novel organosilicon-containing derivative of pullulan of which an organopolysiloxane moiety having a silethylene linkage is bonded to the glucose residue of pullulan through a urethane linkage. Different from conventional organopolysiloxane-modified pullulans, the inventive derivative is stable against attack of water and exhibits unique properties as a combination of the properties inherent in pullulan and in silicones. The organosilicon-containing pullulan of the invention can be easily prepared under mild reaction conditions by reacting an isocyanato group-containing organopolysiloxane with the glucosic hydroxy groups of pullulan.

摘要翻译： 公开了一种新型含有有机硅的支链淀粉衍生物，其中具有亚硫键的有机聚硅氧烷部分通过氨基甲酸酯键与支链淀粉的葡萄糖残基结合。 与传统的有机聚硅氧烷改性的起始链不同，本发明衍生物对水的侵蚀是稳定的，并且表现出作为支链淀粉和硅氧烷中固有的性质的组合的独特性质。 本发明的含有机硅的支链淀粉可以在温和的反应条件下通过含异氰酸酯基的有机聚硅氧烷与支链淀粉的葡糖羟基反应而容易地制备。

公开(公告)号：US20100051927A1

公开(公告)日：2010-03-04

申请号：US12551205

申请日：2009-08-31

申请人： Masateru TANIGUCHI ,  Tomoji Kawai ,  Hideyuki Kawaguchi ,  Ikuo Fukui

发明人： Masateru TANIGUCHI ,  Tomoji Kawai ,  Hideyuki Kawaguchi ,  Ikuo Fukui

IPC分类号： H01L51/30 ,  H01L51/40

CPC分类号： H01L51/052 ,  H01L51/0036 ,  H01L51/004 ,  H01L51/0043 ,  H01L51/0545

摘要： An organic field effect transistor (OFET) having a structure of a conductor layer/an insulator layer/a semiconductor layer is provided. This OFET comprises an insulator layer formed by mixing a polymer compound produced by polymerizing or copolymerizing a monomer represented by the formula (1): CH2═CHCOO—(CH2)2—CN   (1) and/or a monomer represented by the formula (2): CH2═C(CH3)COO—(CH2)2—CN   (2) with a polymerizable and/or crosslinkable organic compound other than the monomer represented by the formula (1) or (2); and a semiconductor layer comprising an organic compound.

摘要翻译： 提供具有导体层/绝缘体层/半导体层的结构的有机场效应晶体管（OFET）。 该OFET包括通过将由式（1）表示的单体：CH2 = CHCOO-（CH2）2-CN（1）表示的单体和/或由式（1）表示的单体 2）：CH 2 = C（CH 3）COO-（CH 2）2 -CN（2）与除式（1）或（2）表示的单体之外的可聚合和/或可交联的有机化合物; 以及包含有机化合物的半导体层。

公开(公告)号：US20060043432A1

公开(公告)日：2006-03-02

申请号：US11199152

申请日：2005-08-09

申请人： Tomoji Kawai ,  Masateru Taniguchi ,  Ikuo Fukui

发明人： Tomoji Kawai ,  Masateru Taniguchi ,  Ikuo Fukui

IPC分类号： H01L23/58

CPC分类号： H01L51/0508 ,  H01L51/002 ,  H01L51/0036 ,  H01L51/052

摘要： In a thin-layer chemical transistor having a metal/solid electrolyte/semiconductor structure, the materials of which the solid electrolyte and semiconductor layers are made comprise organic solvent-soluble compounds. The transistor can be fabricated solely by solvent processes, typically printing techniques including ink jet printing.

摘要翻译： 在具有金属/固体电解质/半导体结构的薄层化学晶体管中，制备固体电解质和半导体层的材料包括有机溶剂可溶性化合物。 晶体管可以仅通过溶剂工艺制造，通常是印刷技术，包括喷墨印刷。