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：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：US06602995B2

公开(公告)日：2003-08-05

申请号：US09758898

申请日：2001-01-11

申请人： Naosuke Maruyama ,  Hiroshi Umezawa

发明人： Naosuke Maruyama ,  Hiroshi Umezawa

IPC分类号： C08B1100

CPC分类号： C08B11/20 ,  C08B11/08

摘要： An object of the present invention is to provide a process for the production of low-substituted hydroxypropyl cellulose wherein, in the formation of low-substituted hydroxypropyl cellulose particles, a granular material obtained by granulating the reaction product is neutralized with an acid to form neutralization-precipitated particles of low-substituted hydroxypropyl cellulose which can reduce the treating time as compared with conventional processes and, moreover, permit its ash content to be easily decreased in a subsequent washing step. Specifically, the reaction product of an alkali cellulose with a hydroxypropylating agent is granulated, and the resulting granular material is neutralized with an acid.

摘要翻译： 本发明的目的是提供一种生产低取代羟丙基纤维素的方法，其中在形成低取代羟丙基纤维素颗粒时，将通过制粒反应产物得到的颗粒物质用酸中和以形成中和 与常规方法相比可以降低处理时间的低取代羟丙基纤维素的沉淀颗粒，此外，在随后的洗涤步骤中允许其灰分含量容易降低。 具体地说，将碱纤维素与羟丙基化剂的反应产物造粒，得到的颗粒状物质用酸中和。

公开(公告)号：US06525192B2

公开(公告)日：2003-02-25

申请号：US09309532

申请日：1999-05-11

申请人： Sakae Obara ,  Hiroshi Umezawa ,  Naosuke Maruyama ,  Fumie Tanno

发明人： Sakae Obara ,  Hiroshi Umezawa ,  Naosuke Maruyama ,  Fumie Tanno

IPC分类号： C08B1120

CPC分类号： A61K9/2054 ,  C08B11/08

摘要： The present invention provides a low-substituted hydroxypropyl cellulose having a loose bulk density of not less than 0.40 g/mL and a tap bulk density of not less than 0.60 g/mL and a process for producing the same.

摘要翻译： 本发明提供松散堆积密度不低于0.40g / mL，堆积密度不小于0.60g / mL的低取代羟丙基纤维素及其制备方法。

公开(公告)号：US08519120B2

公开(公告)日：2013-08-27

申请号：US11888375

申请日：2007-08-01

申请人： Naosuke Maruyama ,  Hiroshi Umezawa

发明人： Naosuke Maruyama ,  Hiroshi Umezawa

IPC分类号： C08B11/20 ,  C08B11/08

CPC分类号： C08B11/08 ,  A61K9/2054 ,  Y10T428/2982

摘要： Provided are a low-substituted hydroxypropylcellulose powder having high compressibility, good flowability and excellent disintegration, and a method for producing the same. More specifically, provided is a method for producing a low-substituted hydroxypropylcellulose powder having a molar substitution number per anhydrous glucose unit of 0.05 to 1.0, which is insoluble in water and swollenable by absorbing water, comprising the steps of: adding an aqueous sodium hydroxide solution to powdered pulp in such a manner that weight ratio of sodium hydroxide with respect to anhydrous cellulose is 0.1 to 0.3 so as to produce alkali cellulose; etherifying the obtained alkali cellulose to obtain a crude product; neutralizing the sodium hydroxide contained in the obtained crude reaction product; washing the resultant; drying; and pulverizing using by compaction-grinding.

摘要翻译： 提供具有高压缩性，良好流动性和优异崩解性的低取代羟丙基纤维素粉末及其制造方法。 更具体地说，提供了一种生产低取代度羟丙基纤维素粉末的方法，所述低取代羟丙基纤维素粉末的无水葡萄糖单元的摩尔取代数为0.05-1.0，其不溶于水并通过吸收水可膨胀，包括以下步骤：加入氢氧化钠水溶液 粉末纸浆的溶液，使氢氧化钠相对于无水纤维素的重量比为0.1〜0.3，制成碱纤维素; 将得到的碱性纤维素醚化得到粗产物; 中和所得粗反应产物中所含的氢氧化钠; 洗涤结果; 烘干; 并通过压实研磨进行粉碎。

公开(公告)号：US20080039621A1

公开(公告)日：2008-02-14

申请号：US11888375

申请日：2007-08-01

申请人： Naosuke Maruyama ,  Hiroshi Umezawa

发明人： Naosuke Maruyama ,  Hiroshi Umezawa

IPC分类号： C08B11/20

CPC分类号： C08B11/08 ,  A61K9/2054 ,  Y10T428/2982

摘要： Provided are a low-substituted hydroxypropylcellulose powder having high compressibility, good flowability and excellent disintegration, and a method for producing the same. More specifically, provided is a method for producing a low-substituted hydroxypropylcellulose powder having a molar substitution number per anhydrous glucose unit of 0.05 to 1.0, which is insoluble in water and swollenable by absorbing water, comprising the steps of: adding an aqueous sodium hydroxide solution to powdered pulp in such a manner that weight ratio of sodium hydroxide with respect to anhydrous cellulose is 0.1 to 0.3 so as to produce alkali cellulose; etherifying the obtained alkali cellulose to obtain a crude product; neutralizing the sodium hydroxide contained in the obtained crude reaction product; washing the resultant; drying; and pulverizing using by compaction-grinding.

摘要翻译： 提供具有高压缩性，良好流动性和优异崩解性的低取代羟丙基纤维素粉末及其制造方法。 更具体地说，提供了一种生产低取代度羟丙基纤维素粉末的方法，所述低取代羟丙基纤维素粉末的无水葡萄糖单元的摩尔取代数为0.05-1.0，其不溶于水并通过吸收水可膨胀，包括以下步骤：加入氢氧化钠水溶液 粉末纸浆的溶液，使氢氧化钠相对于无水纤维素的重量比为0.1〜0.3，制成碱纤维素; 将得到的碱性纤维素醚化得到粗产物; 中和所得粗反应产物中所含的氢氧化钠; 洗涤结果; 烘干; 并通过压实研磨进行粉碎。

公开(公告)号：US07009046B2

公开(公告)日：2006-03-07

申请号：US10315324

申请日：2002-12-10

申请人： Naosuke Maruyama ,  Hiroshi Umezawa

发明人： Naosuke Maruyama ,  Hiroshi Umezawa

IPC分类号： C08B11/20

CPC分类号： C08B11/20 ,  A61K9/2054 ,  C08B11/08 ,  C08L1/284

摘要： Provided is an agent serving as a binder and a disintegrant for dry direct compression having a high binding property and fluidity. More specifically, provided are low-substituted hydroxypropyl cellulose having coiled fibers; an agent serving both as a binder and a disintegrant for dry direct compression and a solid preparation, each comprising the low-substituted hydroxypropyl cellulose; and a process for producing the low-substituted hydroxypropyl cellulose having coiled fibers.

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。