Esterified cellulose ethers having a specific substituent distribution
    11.
    发明授权
    Esterified cellulose ethers having a specific substituent distribution 有权
    具有特定取代基分布的酯化纤维素醚

    公开(公告)号:US09320799B2

    公开(公告)日:2016-04-26

    申请号:US14390041

    申请日:2012-10-24

    摘要: An esterified cellulose ether comprises (i) aliphatic monovalent acyl groups or (ii) groups of the formula —C(O)—R—COOA wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation or (iii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein the cellulose ether has anhydroglucose units joined by 1-4 linkages and has methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl as substituents such that the esterified cellulose ether has an MS (hydroxyalkyl) of 0.05 to 1.00, and hydroxyl groups of anhydroglucose units are substituted with methyl groups such that [s23/s26−0.2*MS(hydroxyalkyl)] is 0.36 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 3-positions of the anhydroglucose unit are substituted with a methyl group and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 6-positions of the anhydroglucose unit are substituted with a methyl group. The esterified cellulose ether is useful as an excipient for poorly water-soluble drugs.

    摘要翻译: 酯化的纤维素醚包括(i)脂族一价酰基或(ii)式-C(O)-R-COOA的基团,其中R是二价脂族或芳族烃基,A是氢或阳离子或(iii) 脂族一价酰基和式-C(O)-R-COOA基团的组合,其中纤维素醚具有通过1-4键连接并具有甲基,羟基烷基和任选的烷基的脱水葡萄糖单元, 甲基作为取代基使得酯化纤维素醚具有0.05至1.00的MS(羟烷基),脱水葡萄糖单元的羟基被甲基取代,使得[s23 / s26-0.2 * MS(羟烷基)]为0.36以下, 其中s23是脱水葡萄糖单元的摩尔分数,其中只有脱水葡萄糖单元的2-和3-位上的两个羟基被甲基取代,其中s26是脱水葡萄糖单元的摩尔分数,其中仅th 脱水葡萄糖单元的2-和6-位上的两个羟基被甲基取代。 酯化纤维素醚可用作水溶性差的药物的赋形剂。

    NOVEL HYDROXYALKYL METHYL CELLULOSE ACETATE SUCCINATES
    12.
    发明申请
    NOVEL HYDROXYALKYL METHYL CELLULOSE ACETATE SUCCINATES 审中-公开
    新型羟基乙基甲基纤维素乙酸酯

    公开(公告)号:US20150218198A1

    公开(公告)日:2015-08-06

    申请号:US14421072

    申请日:2013-08-15

    IPC分类号: C07H3/06 A61K9/48 A61K47/38

    摘要: Novel hydroxyalkyl methyl cellulose acetate succinates which a) have from 4.0 to less than 10.0 weight percent of succinoyl groups, b) have a weight average molecular weight Mw of from 80,000 Dalton to 350,000 Dalton, and c) exhibit a turbidity of up to 41 NTU as a 1.5 weight percent solution in acetone; and novel hydroxyalkyl methyl cellulose acetate succinates which a) have from 10.0 to 20.0 weight percent of succinoyl groups, b) have a weight average molecular weight Mw of from 80,000 Dalton to 350,000 Dalton, and c) exhibit a turbidity of up to 37 NTU as a 1.5 weight percent solution in acetone are useful for preparing solid dispersion of active ingredients in these hydroxyalkyl methyl cellulose acetate succinates.

    摘要翻译: 新型羟烷基甲基纤维素乙酸酯琥珀酸酯,其a)具有4.0至小于10.0重量%的琥珀酰基,b)重均分子量Mw为80,000道尔顿至350,000道尔顿,和c)表现出高达41NTU的浊度 作为1.5重量%丙酮溶液; 和新的羟烷基甲基纤维素乙酸酯琥珀酸酯,其a)具有10.0至20.0重量%的琥珀酰基,b)具有80,000道尔顿至35万道尔顿的重均分子量Mw,和c)显示高达37NTU的浊度为 丙酮中的1.5重量%溶液可用于制备活性成分在这些羟烷基甲基纤维素乙酸酯琥珀酸酯中的固体分散体。

    COMPOSITION COMPRISING AN ORGANIC DILUENT AND A CELLULOSE ETHER
    13.
    发明申请
    COMPOSITION COMPRISING AN ORGANIC DILUENT AND A CELLULOSE ETHER 有权
    包含有机稀释剂和纤维素醚的组合物

    公开(公告)号:US20150065548A1

    公开(公告)日:2015-03-05

    申请号:US14390049

    申请日:2013-04-08

    摘要: A liquid composition comprises an organic diluent and at least one cellulose ether having anhydroglucose units joined by 1-4 linkages and having methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl as substituents such that hydroxyl groups of anhydroglucose units are substituted with methyl groups such that s23/s26 is 0.29 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 3-positions of the anhydroglucose unit are substituted with a methyl group and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 6-positions of the anhydroglucose unit are substituted with a methyl group. The liquid composition can be used for preparing a solid dispersion of an active ingredient in a cellulose ether.

    摘要翻译: 液体组合物包含有机稀释剂和至少一种具有通过1-4键连接并具有甲基,羟基烷基和任选的不同于甲基作为取代基的烷基的脱水葡萄糖单元的纤维素醚,使得脱水葡萄糖单元的羟基被 甲基,使得s23 / s26为0.29以下,其中s23是脱水葡萄糖单元的摩尔分数,其中脱水葡萄糖单元的2-和3-位上的两个羟基仅被甲基取代,其中s26是 脱水葡萄糖单元的摩尔分数,其中只有脱水葡萄糖单元的2-和6-位上的两个羟基被甲基取代。 液体组合物可用于制备活性成分在纤维素醚中的固体分散体。

    NOVEL ESTERIFIED CELLULOSE ETHERS OF LOW VISCOSITY
    19.
    发明申请
    NOVEL ESTERIFIED CELLULOSE ETHERS OF LOW VISCOSITY 有权
    低粘度的新型蛋白质纤维素

    公开(公告)号:US20150374831A1

    公开(公告)日:2015-12-31

    申请号:US14766997

    申请日:2014-02-28

    IPC分类号: A61K47/38 C08B13/00

    摘要: Esterified cellulose ethers which comprise (i) aliphatic monovalent acyl groups or (ii) groups of the formula —C(O)—R—COOA, wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation, or (iii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, which have a viscosity of up to 2.33 mPa·s, measured as a 2.0 wt % solution of the esterified cellulose ether in 0.43 wt % aqueous NaOH at 20° C., and which have a viscosity of up to 13 mPao·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C. are useful for preparing solid dispersions comprising drugs.

    摘要翻译: 酯化纤维素醚,其包含(i)脂族一价酰基或(ii)式-C(O)-R-COOA的基团,其中R是二价脂族或芳族烃基,A是氢或阳离子,或( iii)脂族一价酰基和式-C(O)-R-COOA基团的组合,其粘度高达2.33mPa·s,以2.0重量%的酯化纤维素醚溶液测量为0.43 20℃下的重量%NaOH水溶液,其粘度高达13mPao·s,以20wt%的酯化纤维素醚在丙酮中的10wt%溶液测量,可用于制备包含药物的固体分散体 。