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    ESTERIFIED CELLULOSE ETHERS HAVING A SPECIFIC SUBSTITUENT DISTRIBUTION
    3.
    发明申请
    ESTERIFIED CELLULOSE ETHERS HAVING A SPECIFIC SUBSTITUENT DISTRIBUTION 有权
    具有特殊取代分布的蛋白质酯

    公开(公告)号：US20150065547A1

    公开(公告)日：2015-03-05

    申请号：US14390041

    申请日：2012-10-24

    Applicant: Dow Global Technologies LLC

    Inventor： Robert L. Schmitt ,  Robert L. Sammler ,  Meinolf Brackhagen ,  Oliver Petermann ,  Roland Adden ,  Nicholas S. Grasman ,  Steven J. Guillaudeu

    IPC: A61K47/38 ,  A61K47/10 ,  A61K9/48 ,  A61K31/4166 ,  A61K9/14 ,  C08B13/00 ,  A61K31/343

    CPC classification number: A61K47/38 ,  A61K9/08 ,  A61K9/145 ,  A61K9/146 ,  A61K9/4816 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/343 ,  A61K31/4166 ,  A61K47/10 ,  C08B11/193 ,  C08B13/00

    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。

    Esterified cellulose ethers having a specific substituent distribution
    4.
    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

    Applicant: Dow Global Technologies LLC

    Inventor： Robert L. Schmitt ,  Robert L. Sammler ,  Meinolf Brackhagen ,  Oliver Petermann ,  Roland Adden ,  Nicholas S. Grasman ,  Steven J. Guillaudeu

    IPC: A61K31/343 ,  A61K31/4166 ,  A61K47/10 ,  A61K47/38 ,  A61K9/14 ,  A61K9/48 ,  C08B13/00 ,  C08B11/193 ,  A61K9/08

    CPC classification number: A61K47/38 ,  A61K9/08 ,  A61K9/145 ,  A61K9/146 ,  A61K9/4816 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/343 ,  A61K31/4166 ,  A61K47/10 ,  C08B11/193 ,  C08B13/00

    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。

    PARTIALLY CROSS-LINKED ESTERIFIED CELLULOSE ETHERS
    5.
    发明申请
    PARTIALLY CROSS-LINKED ESTERIFIED CELLULOSE ETHERS 有权
    部分交联的蛋白质酯

    公开(公告)号：US20150203597A1

    公开(公告)日：2015-07-23

    申请号：US14420985

    申请日：2013-08-15

    Applicant: Dow Global Technologies LLC

    Inventor： Meinolf Brackhagen ,  Nicholas S. Grasman ,  Yongfu Li ,  David M. Meunier ,  Oliver Petermann ,  Matthias Sprehe

    IPC: C08B13/00 ,  C08B11/20 ,  A61K9/10

    CPC classification number: C08B13/00 ,  A61K9/10 ,  A61K9/146 ,  A61K9/2866 ,  C08B11/20

    Abstract: A partially cross-linked esterified cellulose ether having A) groups of the formula —C(O)—R—COOA or a combination of aliphatic monovalent acyl groups and 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, and B) having a molecular weight distribution such that [Wf(>100 k)−Wf(>100 k)XL]/Wf(>100 k)XL is at least 0.20, wherein Wf(>100 k) is the total weight fraction of the esterified cellulose ether that exceeds 100,000 g/mol, and Wf(>100 k)XL is the weight fraction that exceeds 100,000 g/mol of the methylated esterified cellulose ether is useful as enteric polymer for pharmaceutical dosage forms.

    Abstract translation: 具有A）基团的式-C（O）-R-COOA或脂族一价酰基和式-C（O）-R-COOA基团的部分交联的酯化纤维素醚，其中R为 二价脂族或芳族烃基，A是氢或阳离子，B）分子量分布使得[Wf（> 100k）-Wf（> 100k）XL] / Wf（> 100k）XL为 至少0.20，其中Wf（> 100k）是超过100,000g / mol的酯化纤维素醚的总重量分数，Wf（> 100k）XL是甲基化酯化的超过100,000g / mol的重量分数 纤维素醚可用作药物剂型的肠溶性聚合物。

    COMPOSITION COMPRISING AN ORGANIC DILUENT AND A CELLULOSE ETHER
    6.
    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

    Applicant: Dow Global Technologies LLC

    Inventor： Roland Adden ,  Robert L. Sammler ,  Meinolf Brackhagen ,  Nicholas S. Grasman ,  Oliver Petermann ,  Steven J. Guillaudeu

    IPC: A61K47/38 ,  A61K31/4166 ,  A61K31/343 ,  A61K47/10 ,  A61K9/16

    CPC classification number: A61K47/38 ,  A61K9/08 ,  A61K9/16 ,  A61K9/1617 ,  A61K9/1652 ,  A61K31/343 ,  A61K31/4166 ,  A61K47/10 ,  C08B11/193 ,  C08B11/20 ,  C08L1/28 ,  C08L1/284 ,  C09D101/28 ,  C09D101/284

    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。

    METHOD OF CONTROLLING THE RELEASE OF AN ACTIVE INGREDIENT FROM A DOSAGE FORM
    7.
    发明申请
    METHOD OF CONTROLLING THE RELEASE OF AN ACTIVE INGREDIENT FROM A DOSAGE FORM 有权
    控制从剂量形式释放活性成分的方法

    公开(公告)号：US20150018420A1

    公开(公告)日：2015-01-15

    申请号：US14476203

    申请日：2014-09-03

    Applicant: Dow Global Technologies LLC

    Inventor： Yvonne M. Goerlach-Doht ,  Juergen Hermanns ,  Nicholas S. Grasman

    IPC: A61K9/20 ,  A61K31/192

    CPC classification number: A61K9/2054 ,  A61K9/146 ,  A61K31/192

    Abstract: A method of controlling or adjusting release of an active ingredient from a dosage form comprising the active ingredient and a polysaccharide derivative has been found. The method comprises the steps of a) providing a composition comprising a polysaccharide derivative and a controlled amount of a liquid diluent, based on the dry weight of the polysaccharide derivative, b) subjecting the composition to a dry-grinding operation to provide a dry-ground polysaccharide derivative, and c) incorporating the dry-ground polysaccharide derivative and an active ingredient into a dosage form.

    Abstract translation: 已经发现了从包含活性成分和多糖衍生物的剂型中控制或调节活性成分释放的方法。 该方法包括以下步骤：a）基于多糖衍生物的干重，提供包含多糖衍生物和受控量的液体稀释剂的组合物，b）使组合物进行干磨操作以提供干 - 研磨多糖衍生物，和c）将干地多糖衍生物和活性成分掺入剂型中。

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