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    • 6. 发明申请
    • COMPOSITION COMPRISING AN ORGANIC LIQUID DILUENT AND A SPECIFIC HYDROXYALKYL METHYLCELLULOSE
    • 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
    • WO2015047763A1
    • 2015-04-02
    • PCT/US2014/055574
    • 2014-09-15
    • DOW GLOBAL TECHNOLOGIES LLC
    • BRACKHAGEN, MeinolfADDEN, RolandKNARR, Matthias
    • A61K9/08A61K9/48A61K47/10A61K47/38
    • A61K9/4866A61K9/08A61K9/10A61K9/4808A61K9/4816A61K9/4891A61K47/10A61K47/38C08L1/284
    • 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.
    • 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。
    • 8. 发明申请
    • NOVEL SUSTAINED RELEASE DOSAGE FORMS
    • 新的持续释放剂型
    • WO2013154977A1
    • 2013-10-17
    • PCT/US2013/035589
    • 2013-04-08
    • DOW GLOBAL TECHNOLOGIES LLC
    • BRACKHAGEN, MeinolfADDEN, RolandPETERMANN, OliverSAMMLER, Robert, L.WALLICK, David, E.
    • A61K47/26A61K9/20C08B11/08C08B11/193C08L1/28
    • A61K31/167A61K9/2018A61K9/2054A61K9/2095C08B11/08C08B11/193C08L1/284
    • A sustained release dosage form comprises an active ingredient blended with a polymeric matrix. At least a portion of the polymeric matrix is formed by a cellulose ether having an onset dissolution temperature of at least 40°C, 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 the 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 0.31 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.
    • 持续释放剂型包含与聚合物基质共混的活性成分。 聚合物基质的至少一部分由具有至少40℃的起始溶解温度的纤维素醚形成,其具有通过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纤维素醚具有0.05至1.00的MS(羟烷基),并且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0.31或更小,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,其中只有 脱水葡萄糖单元的2-位和6-位被甲基取代。
    • 9. 发明申请
    • ESTERIFIED CELLULOSE ETHERS HAVING A SPECIFIC SUBSTITUENT DISTRIBUTION
    • 具有特殊替代品分销的蛋白质酯类化合物
    • WO2013154607A1
    • 2013-10-17
    • PCT/US2012/061586
    • 2012-10-24
    • DOW GLOBAL TECHNOLOGIES LLC
    • SCHMITT, Robert, L.SAMMLER, Robert, L.BRACKHAGEN, MeinolfPETERMANN, OliverADDEN, RolandGRASMAN, Nicholas, S.GUILLAUDEU, Steven, J.
    • A61K9/20A61K47/38C08B11/08C08B13/00
    • A61K47/38A61K9/08A61K9/145A61K9/146A61K9/4816A61K9/4858A61K9/4866A61K31/343A61K31/4166A61K47/10C08B11/193C08B13/00
    • 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.
    • 酯化纤维素醚包括(i)脂族一价酰基或(ii)式-C(O)-R-COOA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),并且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 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。