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公开(公告)号：EP3816191A1
公开(公告)日：2021-05-05
申请号：EP20204429.3
申请日：2020-10-28
摘要： There is provided a method for producing hydroxypropyl methyl cellulose phthalate (HPMCP), including an esterification step of reacting hydroxypropyl methyl cellulose with a carboxybenzoylating agent in the presence of an aliphatic carboxylic acid in a kneader reactor equipped with two or more stirring blades rotating around their own axes and orbitally revolving, to obtain a reaction product solution containing HPMCP; a precipitation step of precipitating the HPMCP by mixing the reaction product solution with water to obtain a suspension of the precipitated HPMCP; and a washing and recovery step of washing the HPMCP in the suspension and recovering the washed HPMCP. Further, there is provided HPMCP having yellowness at 20°C of 10.0 or less, as determined in a 10% by mass solution of the HPMCP in acetone.
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公开(公告)号：EP3567058A1
公开(公告)日：2019-11-13
申请号：EP19172187.7
申请日：2019-05-02
IPC分类号： C08B13/00
摘要： There is provided a method for producing hypromellose phthalate (HPMCP) which exhibits an excellent solubility when dissolved in a solvent, while suppressing formation of undissolved matter. More specifically, there is provided a method for producing HPMCP, including an esterification step of esterifying hypromellose dissolved in glacial acetic acid with phthalic anhydride in the presence of sodium acetate at a temperature of from 75 to 100 °C to obtain a reaction product solution; a cooling step of cooling the reaction product solution to 70 °C or lower; and a precipitation step of mixing the cooled reaction product solution with water of from 0 to 40 °C to obtain a suspension of precipitated HPMCP.
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公开(公告)号：EP3228324A1
公开(公告)日：2017-10-11
申请号：EP17164369.5
申请日：2017-03-31
IPC分类号： A61K47/38 , A61K9/28 , A61K31/525
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.
摘要翻译： 提供了当溶解在溶剂中时具有高溶解度并且能够抑制不溶物质产生的HPMCAS粉末; 和生产该粉末的方法。 更具体地，提供具有平均比率L与D的2.0-3.0的醋酸羟丙甲纤维素琥珀酸酯粉末，其中L和D分别表示每个颗粒的最大直径和最小直径。 本发明还提供一种琥珀酸羟丙甲纤维素琥珀酸酯的制造方法，其包括以下步骤：将羟丙甲纤维素粉末溶解在溶剂中，在催化剂存在下，将溶解的羟丙甲纤维素与琥珀酸酐和乙酸酐酯化，得到反应混合物， 与水混合以沉淀醋酸羟丙甲纤维素琥珀酸酯，其中恰好在与水混合之前的反应混合物具有100-200Pa·s的粘度。
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4.发明公开HYPROMELLOSE ACETATE SUCCINATE, METHOD FOR PRODUCING THE SAME AND COMPOSITION CONTAINING THE SAME 审中-公开醋酸胞壁琥珀酸钠，其制备方法和含有该化合物的组合物
公开(公告)号：EP3216808A1
公开(公告)日：2017-09-13
申请号：EP17159962.4
申请日：2017-03-08
发明人： KIKUCHI, Kazuki , YOSHIDA, Mitsuhiro , MATSUBARA, Junichi , YAMASHITA, Tatsuya , KITAMURA, Akira , MARUYAMA, Naosuke
IPC分类号： C08B13/00
CPC分类号： C08B13/00 , C09D7/20 , C09D7/65 , C09D101/32
摘要： Provided are hypromellose acetate succinate (HPMCAS) which exhibits high solubility and can suppress generation of undissolved materials when dissolved in a solvent; an HPMCAS-containing composition; and a method for producing the HPMCAS. More specifically, provided are HPMCAS having a ratio of 2-position MS to 3-position MS of 1.2 or less, wherein the 2-position MS means a molar substitution of hydroxypropyl group by which a hydrogen atom of a hydroxyl group on 2-position carbon of each glucose unit of the HPMCAS has been directly replaced, and the 3-position MS means a molar substitution of hydroxypropyl group by which a hydrogen atom of a hydroxyl group on 3-position carbon of each glucose unit of the HPMCAS has been directly replaced; a composition comprising the HPMCAS and a solvent; and the method for producing the HPMCAS.
摘要翻译： 本发明提供乙酸羟丙甲纤维素琥珀酸酯（HPMCAS），其显示出高溶解度并且当溶解在溶剂中时可抑制不溶物质的生成; 含有HPMCAS的组合物; 以及生产HPMCAS的方法。 更具体地说，提供具有1.2或更低的2-位MS与3-位MS的比率的HPMCAS，其中2-位MS是指2-羟基上的氢原子在2-位上的羟丙基的摩尔取代 直接取代HPMCAS的每个葡萄糖单元的碳原子，并且3位MS表示HPMCAS的每个葡萄糖单元的3位碳上的羟基的氢原子直接被羟丙基取代的羟基基团 更换; 包含HPMCAS和溶剂的组合物; 以及制造HPMCAS的方法。
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公开(公告)号：EP3816192A1
公开(公告)日：2021-05-05
申请号：EP20204427.7
申请日：2020-10-28
摘要： There is provided a method for producing hydroxypropyl methyl cellulose acetate succinate (HPMCAS), including an esterification step of reacting hydroxypropyl methyl cellulose with an acetylating agent and a succinoylating agent in the presence of an aliphatic carboxylic acid in a kneader reactor equipped with two or more stirring blades rotating around their own axes and orbitally revolving, to obtain a reaction product solution containing HPMCAS; a precipitation step of precipitating the HPMCAS by mixing the reaction product solution with water to obtain a suspension of the precipitated HPMCAS; and a washing and recovery step of washing the HPMCAS in the suspension and recovering the washed HPMCAS. Further, there is provided HPMCAS having yellowness at 20°C of 15.0 or less, as determined in a 2% by mass solution of the HPMCAS in a mixed solvent of dichloromethane, methanol and water in a mass ratio of 44:44:10.
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6.发明授权
公开(公告)号：EP3216808B1
公开(公告)日：2018-10-03
申请号：EP17159962.4
申请日：2017-03-08
发明人： KIKUCHI, Kazuki , YOSHIDA, Mitsuhiro , MATSUBARA, Junichi , YAMASHITA, Tatsuya , KITAMURA, Akira , MARUYAMA, Naosuke
IPC分类号： C08B13/00
CPC分类号： C08B13/00 , C09D7/20 , C09D7/65 , C09D101/32
摘要： Provided are hypromellose acetate succinate (HPMCAS) which exhibits high solubility and can suppress generation of undissolved materials when dissolved in a solvent; an HPMCAS-containing composition; and a method for producing the HPMCAS. More specifically, provided are HPMCAS having a ratio of 2-position MS to 3-position MS of 1.2 or less, wherein the 2-position MS means a molar substitution of hydroxypropyl group by which a hydrogen atom of a hydroxyl group on 2-position carbon of each glucose unit of the HPMCAS has been directly replaced, and the 3-position MS means a molar substitution of hydroxypropyl group by which a hydrogen atom of a hydroxyl group on 3-position carbon of each glucose unit of the HPMCAS has been directly replaced; a composition comprising the HPMCAS and a solvent; and the method for producing the HPMCAS.
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7.发明公开
公开(公告)号：EP3318283A1
公开(公告)日：2018-05-09
申请号：EP17199574.9
申请日：2017-11-01
CPC分类号： A61K9/2866 , A61K31/525 , A61K47/38 , C08B13/00
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.
摘要翻译： 提供具有这样性质的HPMCAS（羟丙甲纤维素琥珀酸酯）：HPMCAS在溶剂中的溶液具有可控的粘度; 以及生产HPMCAS的方法。 更具体地说，提供具有如下性质的HPMCAS：10重量份的HPMCAS在100重量份的具有1：1的二氯甲烷与甲醇的重量比的混合溶剂中的溶液具有20℃时的粘度 135 mPa·s以下; 以及制造HPMCAS的方法，其包括酯化步骤，在乙酸钠存在下将羟基甲
纤维素溶于羟乙基纤维素的溶液中加入乙酸酐和琥珀酸酐以获得反应产物混合物，其中间歇地加入琥珀酸酐， 将反应产物混合物与水混合以沉淀HPMCAS的沉淀步骤。-
8.发明公开HYPROMELLOSE PHTHALATE AND METHOD FOR PRODUCING HYPROMELLOSE PHTHALATE 审中-公开邻苯二甲酸氢酯和生产邻苯二甲酸邻苯二甲酸酯的方法
公开(公告)号：EP3290443A1
公开(公告)日：2018-03-07
申请号：EP17187784.8
申请日：2017-08-24
IPC分类号： C08B13/00
摘要： Provided is a method for producing HPMCP capable of reducing the average particle size of HPMCP particles to an intended range without a pulverization step. Specifically provided is a method for producing hypromellose phthalate, 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 phthalate, a precipitation step of mixing the reaction solution with water to precipitate the crude hypromellose phthalate, thereby obtaining a hypromellose phthalate suspension, a liquid removal step of removing a liquid from the hypromellose phthalate suspension with a centrifugal decanter to obtain liquid-removed hypromellose phthalate, and a drying step of drying the liquid-removed hypromellose phthalate.
摘要翻译： 本发明提供一种HPMCP的制造方法，其能够在不进行粉碎工序的情况下将HPMCP粒子的平均粒径缩小至目标范围。 具体而言，提供一种羟丙甲纤维素邻苯二甲酸酯的制造方法，其包括使羟丙甲纤维素与酯化剂在催化剂的存在下反应而得到含有粗邻苯二甲酸羟丙甲纤维素的反应溶液的酯化工序，将该反应溶液与水混合， 从而获得邻苯二甲酸羟丙甲纤维素悬浮液，用离心倾析器从邻苯二甲酸羟丙甲纤维素悬浮液中除去液体以获得除去液体的羟丙甲纤维素邻苯二甲酸酯的液体除去步骤以及干燥除去液体的羟丙甲纤维素邻苯二甲酸酯的干燥步骤。
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