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公开(公告)号：US10959959B2
公开(公告)日：2021-03-30
申请号：US15667307
申请日：2017-08-02
发明人： Yasuyuki Hirama , Naosuke Maruyama
摘要： Provided is low-substituted hydroxypropyl cellulose from which a granulation product having an adequate particle size can be obtained in a wet granulation method and a tablet having excellent compactibility and disintegrability can be obtained. More specifically, provided is low-substituted hydroxypropyl cellulose having a hydroxypropoxyl content of from 5 to 16% by weight and a water-soluble content of less than 2% by weight, wherein a weight ratio of water to the low-substituted hydroxypropyl cellulose giving a maximum torque is from 3 to 5 as determined while adding one part by weight of water per minute to one part by weight of the low-substituted hydroxypropyl cellulose under mixing with biaxial mixing blades. Also provided are a solid preparation including the low-substituted hydroxypropyl cellulose, and the like.
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公开(公告)号：US20210024656A1
公开(公告)日：2021-01-28
申请号：US17066543
申请日：2020-10-09
IPC分类号： C08B13/00 , A61K47/38 , A61K9/28 , A61K9/50 , A61K31/525
摘要： Provided are HPMCAS powder having high solubility when dissolved in a solvent and being capable of suppressing generation of undissolved materials; and a method for producing the powder. More specifically, provided is hypromellose acetate succinate powder having an average ratio of L to D of from 2.0 to 3.0, wherein L and D mean maximum and minimum diameters of each particle, respectively. Also provided is a method for producing a hypromellose acetate succinate, comprising the steps of: dissolving hypromellose powder in a solvent, esterifying the dissolved hypromellose with succinic anhydride and acetic anhydride in the presence of a catalyst to obtain a reaction mixture, and mixing the reaction mixture with water to precipitate hypromellose acetate succinate, wherein the reaction mixture just before being mixed with the water has a viscosity of from 100 to 200 Pa·s.
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公开(公告)号：US20200181291A1
公开(公告)日：2020-06-11
申请号：US16789598
申请日：2020-02-13
IPC分类号： C08B13/00 , A61K31/525 , A61K9/50 , A61K9/28 , A61K47/38
摘要： Provided are HPMCAS powder having high solubility when dissolved in a solvent and being capable of suppressing generation of undissolved materials; and a method for producing the powder. More specifically, provided is hypromellose acetate succinate powder having an average ratio of L to D of from 2.0 to 3.0, wherein L and D mean maximum and minimum diameters of each particle, respectively. Also provided is a method for producing a hypromellose acetate succinate, comprising the steps of: dissolving hypromellose powder in a solvent, esterifying the dissolved hypromellose with succinic anhydride and acetic anhydride in the presence of a catalyst to obtain a reaction mixture, and mixing the reaction mixture with water to precipitate hypromellose acetate succinate, wherein the reaction mixture just before being mixed with the water has a viscosity of from 100 to 200 Pa·s.
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公开(公告)号：US20170283514A1
公开(公告)日：2017-10-05
申请号：US15471224
申请日：2017-03-28
IPC分类号： C08B13/00 , A61K9/28 , A61K31/525 , A61K9/50
CPC分类号： C08B13/00 , A61K9/2866 , A61K9/5042 , A61K9/5089 , A61K31/525 , A61K47/38
摘要： Provided are HPMCAS powder having high solubility when dissolved in a solvent and being capable of suppressing generation of undissolved materials; and a method for producing the powder. More specifically, provided is hypromellose acetate succinate powder having an average ratio of L to D of from 2.0 to 3.0, wherein L and D mean maximum and minimum diameters of each particle, respectively. Also provided is a method for producing a hypromellose acetate succinate, comprising the steps of: dissolving hypromellose powder in a solvent, esterifying the dissolved hypromellose with succinic anhydride and acetic anhydride in the presence of a catalyst to obtain a reaction mixture, and mixing the reaction mixture with water to precipitate hypromellose acetate succinate, wherein the reaction mixture just before being mixed with the water has a viscosity of from 100 to 200 Pa·s.
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5.发明申请Composition for Hot-Melt Extrusion and Method for Producing Hot-Melt Extrusion Product Using Same 有权用于热熔体挤出的组合物和使用它的热熔体挤出产物的生产方法公开(公告)号：US20140357681A1
公开(公告)日：2014-12-04
申请号：US14294258
申请日：2014-06-03
发明人： Shogo Warashina , Fumie Kusaki , Kazuki Kikuchi , Sakae Obara , Naosuke Maruyama
IPC分类号： A61K31/4422
CPC分类号： A61K47/38 , A61K9/146 , A61K31/4422 , A61K31/496 , C08B11/193 , C08B11/20 , C08B13/00 , C08J3/201 , C08J2301/32 , C08L1/32
摘要： Provided are a composition for hot-melt extrusion which can be hot-melt extruded at a temperature lower than a conventional temperature and therefore free of heat-induced deactivation of a drug; and a method for producing a hot-melt extrusion product which is simpler than a spray-drying method. More specifically, provided is a composition for hot-melt extrusion including a drug and hypromellose acetate succinate (HPMCAS) having a hydroxypropoxy molar substitution of 0.40 or more. Also provided is a method for producing a hot-melt extrusion product including a step of hot-melt extruding a composition for hot-melt extrusion including a drug and hypromellose acetate succinate having a hydroxypropoxy molar substitution of 0.40 or more at a hot-melt temperature of melting temperature of the hypromellose acetate succinate or higher, or at a hot-melt temperature equal to or higher than a temperature at which both the hypromellose acetate succinate and the drug become melted.
摘要翻译： 提供一种用于热熔挤出的组合物，其可以在比常规温度低的温度下进行热熔挤出，因此不导致药物的热诱导失活; 以及比喷雾干燥法简单的热熔挤出制品的制造方法。 更具体地，提供了包含药物和乙氧基甲基纤维素乙酸琥珀酸酯（HPMCAS）的组合物，其具有0.40或更高的羟丙氧基摩尔取代度。 本发明还提供一种热熔挤出产品的制造方法，其特征在于，包括将热熔融挤出用组合物热熔融挤出的步骤，所述组合物包括药物和醋酸羟丙甲纤维素琥珀酸酯，所述组合物的羟丙氧基摩尔取代度为0.40以上， 或者在等于或高于乙酸琥珀酸羟丙甲纤维素和药物熔化的温度的热熔融温度下进行。
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公开(公告)号：US11052051B2
公开(公告)日：2021-07-06
申请号：US14151205
申请日：2014-01-09
IPC分类号： A61K9/50 , A61K9/00 , A61K9/20 , C09D101/32
摘要： Provided are a drug-containing particle capable of suppressing dissolution of a drug in the oral cavity to suppress an unpleasant taste thereof and having excellent dissolution of the drug in the digestive tract after passing through the oral cavity; a method for preparing the drug-containing particle; a coating composition used for preparing the drug-containing particle; and a solid preparation having the drug-containing particle. More specifically, provided are a coating composition having 100 parts by weight of a cellulose-based enteric base and 50 parts by weight or less of a water-soluble cellulose ether; a drug-containing particle having a drug-containing core and a coat portion obtained by coating the core with the coating composition; a solid preparation having the drug-containing particle; and a method for preparing a drug-containing particle having a step of coating the drug-containing core with the coating composition.
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公开(公告)号：US11021628B2
公开(公告)日：2021-06-01
申请号：US15450511
申请日：2017-03-06
IPC分类号： C09D101/00 , C09D101/28 , C09D7/40 , A61K9/50 , C08B11/02
摘要： Regarding coating of fine particles or the like, provided are a coating composition containing methyl cellulose having small adhesiveness, resistance to generation of lumps, ability to form uniform coating, and ability to form a coating composition easily with water of normal temperature; a method for producing the coating composition; and a solid preparation. More specifically provided are a coating composition including methyl cellulose having such a viscosity that a viscosity at 20° C. of a 2% by weight aqueous solution of the methyl cellulose is 1 to 15 mPa·s and having such a dissolution start temperature that a dissolution start temperature of a 12% by weight aqueous liquid of the methyl cellulose is 10 to 25° C. and a solvent; a solid preparation obtained by coating of the coating composition; and the like.
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公开(公告)号：US10888525B2
公开(公告)日：2021-01-12
申请号：US15797876
申请日：2017-10-30
IPC分类号： C08B3/16 , A61K9/28 , A61K47/38 , C08B13/00 , A61K31/525
摘要： There are provided HPMCAS (hypromellose acetate succinate) having such a property that a solution of the HPMCAS in a solvent has a controlled viscosity; and a method for producing the HPMCAS. More specifically, provided are HPMCAS having such property that a solution of 10 parts by weight of the HPMCAS in 100 parts by weight of a mixed solvent having a weight ratio of methylene chloride to methanol of 1:1 has a viscosity at 20° C. of 135 mPa·s or less; and a method for producing the HPMCAS including an esterification step of adding acetic anhydride and succinic anhydride to a solution of hypromellose in glacial acetic acid in the presence of sodium acetate to obtain a reaction product mixture, wherein the succinic anhydride is added intermittently, and a precipitation step of mixing the reaction product mixture with water to precipitate the HPMCAS.
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公开(公告)号：US20180333361A1
公开(公告)日：2018-11-22
申请号：US16047531
申请日：2018-07-27
发明人： Takuya Yokosawa , Naosuke Maruyama
IPC分类号： A61K9/20 , C08B11/20 , A61K31/167 , C08B11/02
CPC分类号： A61K9/2054 , A61K9/2095 , A61K31/167 , C08B11/02 , C08B11/20
摘要： Provided are an alkyl cellulose excellent in formability when added even in a small amount and not causing marked delay in disintegration; a solid preparation comprising it; and a method for producing the solid preparation. More specifically, provided are an alkyl cellulose for use in tableting, the alkyl cellulose having a specific surface area of from 0.5 to 10.0 m2/g as measured by BET method and a solid preparation comprising the alkyl cellulose. Also provided is a method for producing the alkyl cellulose, comprising the steps of: bringing pulp into contact with an alkali metal hydroxide solution to obtain alkali cellulose, reacting the alkali cellulose with an etherifying agent to obtain a first alkyl cellulose, pulverizing the first alkyl cellulose, and depolymerizing the pulverized first alkyl cellulose through hydrolysis with an acid catalyst or through oxidative decomposition with an oxidant to obtain a second alkyl cellulose.
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10.发明授权公开(公告)号：US10016508B2
公开(公告)日：2018-07-10
申请号：US14294258
申请日：2014-06-03
发明人： Shogo Warashina , Fumie Kusaki , Kazuki Kikuchi , Sakae Obara , Naosuke Maruyama
IPC分类号： A61K31/4422 , A61K47/38 , C08B11/193 , C08B11/20 , C08B13/00 , C08L1/32 , A61K9/14 , C08J3/20 , A61K31/496
CPC分类号： A61K47/38 , A61K9/146 , A61K31/4422 , A61K31/496 , C08B11/193 , C08B11/20 , C08B13/00 , C08J3/201 , C08J2301/32 , C08L1/32
摘要： Provided are a composition for hot-melt extrusion which can be hot-melt extruded at a temperature lower than a conventional temperature and therefore free of heat-induced deactivation of a drug; and a method for producing a hot-melt extrusion product which is simpler than a spray-drying method. More specifically, provided is a composition for hot-melt extrusion including a drug and hypromellose acetate succinate (HPMCAS) having a hydroxypropoxy molar substitution of 0.40 or more. Also provided is a method for producing a hot-melt extrusion product including a step of hot-melt extruding a composition for hot-melt extrusion including a drug and hypromellose acetate succinate having a hydroxypropoxy molar substitution of 0.40 or more at a hot-melt temperature of melting temperature of the hypromellose acetate succinate or higher, or at a hot-melt temperature equal to or higher than a temperature at which both the hypromellose acetate succinate and the drug become melted.
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