COMPOSITION COMPRISING AN ORGANIC LIQUID DILUENT AND A SPECIFIC HYDROXYALKYL METHYLCELLULOSE
    13.
    发明申请
    COMPOSITION COMPRISING AN ORGANIC LIQUID DILUENT AND A SPECIFIC HYDROXYALKYL METHYLCELLULOSE 审中-公开
    包含有机液体二甲醚和特定羟基甲基甲基纤维素的组合物

    公开(公告)号:US20160235682A1

    公开(公告)日:2016-08-18

    申请号:US15023856

    申请日:2014-09-15

    Abstract: A liquid composition which comprises an organic liquid diluent and a hydroxyalkyl methylcellulose which has a certain distribution of substituted hydroxyalkoxyl groups and unsubstituted hydroxyalkoxyl groups is stable over an extended time period. In the hydroxyalkyl methylcellulose hydroxyalkoxyl groups are classified into a fraction (A) and a fraction (B), wherein fraction (A) represents the sum of all molar fractions of substituted hydroxyalkoxyl groups having hydroxyl groups substituted further with methoxyl groups and fraction (B) represents the sum of all molar fractions of unsubstituted hydroxyalkoxyl groups having hydroxyl groups not substituted further with methoxyl groups and wherein the ratio fraction (A)/fraction (B) is at least 0.30. The liquid composition is useful for preparing a solid dispersion comprising at least one active ingredient in at least one hydroxypropyl methylcellulose by spray-drying.

    Abstract translation: 包含有机液体稀释剂和羟烷基甲基纤维素的液体组合物,其具有取代的羟基烷氧基和未取代的羟基烷氧基的一定分布在延长的时间段内是稳定的。 在羟烷基甲基纤维素中,羟基烷氧基分为级分(A)和级分(B),其中级分(A)代表具有被甲氧基进一步取代的羟基的取代的羟基烷氧基的所有摩尔分数和级分(B) 表示具有未被甲氧基进一步取代的羟基的未取代的羟基烷氧基的所有摩尔分数的总和,并且其中所述比例分数(A)/分数(B)为至少0.30。 液体组合物可用于通过喷雾干燥制备包含至少一种羟丙基甲基纤维素中的至少一种活性成分的固体分散体。

    COMPOSITION FOR APPLICATION TO A MUCOSA COMPRISING A METHYLCELLULOSE
    14.
    发明申请
    COMPOSITION FOR APPLICATION TO A MUCOSA COMPRISING A METHYLCELLULOSE 审中-公开
    用于包含甲基纤维素的粘蛋白的组合物

    公开(公告)号:US20160114047A1

    公开(公告)日:2016-04-28

    申请号:US14890617

    申请日:2014-07-16

    CPC classification number: A61K47/38 A61K9/0043 A61K31/167 A61K47/02

    Abstract: A composition designed for application to a mucosa comprises a tonicity-adjusting agent, a methylcellulose, and a liquid diluent, wherein the methylcellulose has anhydroglucose units joined by 1-4 linkages wherein hydroxy groups of anhydroglucose units are substituted with methyl groups such that s23/s26 is 0.36 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 3-positions of the anhydroglucose unit are substituted with methyl groups and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 6-positions of the anhydroglucose unit are substituted with methyl groups.

    Abstract translation: 设计用于粘膜的组合物包括张力调节剂,甲基纤维素和液体稀释剂,其中甲基纤维素具有通过1-4键连接的脱水葡萄糖单元,其中脱水葡萄糖单元的羟基被甲基取代,使得s23 / s26为0.36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-位中的两个羟基仅被甲基取代,并且其中s26是脱水葡萄糖单元的摩尔分数,其中仅 脱水葡萄糖单元的2-和6-位上的两个羟基被甲基取代。

    Esterified cellulose ethers having a specific substituent distribution
    15.
    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

    Abstract: 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.

    Abstract translation: 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。

    COMPOSITION COMPRISING AN ORGANIC DILUENT AND A CELLULOSE ETHER
    16.
    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

    Abstract: 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.

    Abstract translation: 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。

    COMPOSITION FOR APPLICATION TO A MUCOSA COMPRISING A CELLULOSE ETHER
    20.
    发明申请
    COMPOSITION FOR APPLICATION TO A MUCOSA COMPRISING A CELLULOSE ETHER 审中-公开
    用于包含纤维素醚的粘蛋白的组合物

    公开(公告)号:US20160228559A1

    公开(公告)日:2016-08-11

    申请号:US15023736

    申请日:2014-09-15

    CPC classification number: A61K47/38 A61K9/0043 A61K9/08 A61K31/167 A61K47/02

    Abstract: A composition designed for application to a mucosa comprises i) a tonicity-adjusting agent, ii) an aqueous liquid diluent, and iii) 0.1 to 6 weight percent of a cellulose ether having a viscosity of up to 8000 mPa·s, 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 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.

    Abstract translation: 设计用于粘膜的组合物包括i)张力调节剂,ii)含水液体稀释剂,和iii)0.1至6重量%的粘度高达8000mPa·s的纤维素醚,其中纤维素 醚具有通过1-4键连接的脱水葡萄糖单元,并且具有甲基,羟基烷基和任选的不同于作为取代基的甲基的烷基,使得脱水葡萄糖单元的羟基被甲基取代,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,并且其中s26是脱水葡萄糖单元的摩尔分数,其中只有两个羟基在 脱水葡萄糖单元的2-位和6-位被甲基取代。

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