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1.发明授权公开(公告)号：US10646573B2
公开(公告)日：2020-05-12
申请号：US14892421
申请日：2014-06-03
发明人： Shogo Warashina , Fumie Kusaki , Sakae Obara , Kazuki Kikuchi , Naosuke Maruyama
IPC分类号： A61K47/38 , A61K9/14 , A61K31/4422 , C08J3/20 , C08B11/193 , C08B11/20 , C08B13/00 , C08L1/32 , A61K31/496
摘要： 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 and a mole ratio of an acetyl group to a succinyl group of less than 1.6. Further, provided is a method for producing a hot melt extrudate including the step of hot melt-extruding a composition for hot melt extrusion including a drug and hypromellose acetate succinate having a molar hydroxypropoxy substitution of 0.40 or more and a mole ratio of an acetyl group to a succinyl group of less than 1.6, at a hot melt temperature of not lower than a melting temperature of the hypromellose acetate succinate or of not lower than a temperature at which both the hypromellose acetate succinate and the drug are melted.
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公开(公告)号：US11090295B2
公开(公告)日：2021-08-17
申请号：US14453935
申请日：2014-08-07
发明人： Naosuke Maruyama , Shogo Warashina , Fumie Kusaki , Sakae Obara , Kazuki Kikuchi
IPC分类号： A61K31/4422 , A61K9/14 , A61K47/38 , A61K9/20
摘要： Provided are hypromellose acetate succinates (HPMCAS) for use as a hot-melt extrusion carrier having a volume average particle size (D50) of from 70 to 300 as measured by dry laser diffraction and a loose bulk density of from 0.25 to 0.40 g/cm3; and a hot-melt extrusion composition comprising the HPMCAS and a drug. Also provided is a method for producing a hot-melt extrudate including the steps of: hot-melting the hot-melt extrusion composition at a hot-melt temperature equal to or higher than a melting temperature of the HPMCAS, or at a hot-melt temperature equal to or higher than a temperature at which both of the HPMCAS and the drug become melt; and extruding the hot-melted composition.
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公开(公告)号：US10604588B2
公开(公告)日：2020-03-31
申请号：US15471224
申请日：2017-03-28
IPC分类号： C08B13/00 , A61K9/28 , A61K31/525 , A61K9/50 , 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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4.发明申请HYPROMELLOSE ACETATE SUCCINATE FOR USE AS HOT-MELT EXTRUSION CARRIER, HOT-MELT EXTRUSION COMPOSITION, AND METHOD FOR PRODUCING HOT-MELT EXTRUDATE 审中-公开用作高熔体挤出载体的丙烯酸乙酯酯，热熔融挤出组合物，以及用于生产高熔点挤出物的方法公开(公告)号：US20150044289A1
公开(公告)日：2015-02-12
申请号：US14453935
申请日：2014-08-07
发明人： Naosuke Maruyama , Shogo Warashina , Fumie Kusaki , Sakae Obara , Kazuki Kikuchi
IPC分类号： A61K31/4422 , A61K9/14
CPC分类号： A61K31/4422 , A61K9/146 , A61K9/20 , A61K47/38 , Y10T428/2982
摘要： Provided are hypromellose acetate succinates (HPMCAS) for use as a hot-melt extrusion carrier having a volume average particle size (D50) of from 70 to 300 as measured by dry laser diffraction and a loose bulk density of from 0.25 to 0.40 g/cm3; and a hot-melt extrusion composition comprising the HPMCAS and a drug. Also provided is a method for producing a hot-melt extrudate including the steps of: hot-melting the hot-melt extrusion composition at a hot-melt temperature equal to or higher than a melting temperature of the HPMCAS, or at a hot-melt temperature equal to or higher than a temperature at which both of the HPMCAS and the drug become melt; and extruding the hot-melted composition.
摘要翻译： 提供了用作通过干激光衍射测量的体积平均粒径（D50）为70至300的热熔体挤出载体的乙酸纤维素乙酸酯琥珀酸酯（HPMCAS），以及0.25至0.40g / cm 3的松散堆积密度 ; 和包含HPMCAS和药物的热熔挤出组合物。 还提供了一种生产热熔挤出物的方法，包括以下步骤：在等于或高于HPMCAS的熔融温度的热熔融温度下热熔融该热熔挤出组合物，或在热熔体 温度等于或高于HPMCAS和药物两者融化的温度; 并挤出热熔融组合物。
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5.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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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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9.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：US10934367B2
公开(公告)日：2021-03-02
申请号：US15683222
申请日：2017-08-22
摘要： Provided is a method for producing HPMCAS capable of reducing the average particle size of HPMCAS particles to an intended range without a pulverization step. Specifically provided is a method for producing hypromellose acetate succinate, comprising an esterification step of reacting hypromellose with an esterification agent in the presence of a catalyst to obtain a reaction solution containing crude hypromellose acetate succinate, a precipitation step of mixing the reaction solution with water to precipitate the crude hypromellose acetate succinate, thereby obtaining a hypromellose acetate succinate suspension, a liquid removal step of removing a liquid from the hypromellose acetate succinate suspension with a centrifugal decanter to obtain liquid-removed hypromellose acetate succinate, and a drying step of drying the liquid-removed hypromellose acetate succinate.
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