公开(公告)号：US20180072820A1

公开(公告)日：2018-03-15

申请号：US15550109

申请日：2016-03-08

Applicant: Dow Global Technologies LLC

Inventor： Oliver Petermann ,  Matthias Knarr

IPC: C08B13/00 ,  A61K47/38 ,  A61K9/48 ,  A61K9/10 ,  A23L33/125 ,  A23P10/30

Abstract: An esterified cellulose comprising aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOH, R being a divalent hydrocarbon group, has the following properties: i) the degree of neutralization of the groups —C(O)—R—COOH is not more than 0.4, ii) the total degree of ester substitution is from 0.03 to 0.38, and iii) the esterified cellulose ether has a solubility in water of at least 2.0 weight percent at 20° C.

公开(公告)号：US20180072819A1

公开(公告)日：2018-03-15

申请号：US15550097

申请日：2016-03-08

Applicant: Dow Global Technologies LLC

Inventor： Oliver Petermann ,  Matthias Knarr ,  Robert B. Appell

IPC: C08B13/00 ,  A61K9/48 ,  A23L33/125

CPC classification number: C08B13/00 ,  A23L33/125 ,  A23V2002/00 ,  A61K9/4816 ,  A61K9/4866 ,  A61K47/38 ,  C08B11/20

Abstract: An esterified cellulose ether comprising aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOH, R being a divalent hydrocarbon group, has the following properties: i) the degree of neutralization of the groups —C(O)—R—COOH is not more than 0.4, ii) the total degree of ester substitution is from 0.10 to 0.70, and iii) the esterified cellulose ether has a solubility in water of at least 2.0 weight percent at 2 C.

公开(公告)号：US20180030157A1

公开(公告)日：2018-02-01

申请号：US15549858

申请日：2016-03-08

Applicant: Dow Global Technologies LLC

Inventor： Oliver Petermann ,  Matthias Knarr ,  Meinolf Brackhagen ,  Matthias Sprehe

IPC: C08B11/20 ,  C08B13/00 ,  C08L1/26

CPC classification number: C08B11/20 ,  A61K9/146 ,  C08B13/00 ,  C08L1/26

Abstract: A process for fractionating an esterified cellulose ether comprising groups of the formula —C(O)—R—COOH, wherein R is a divalent hydrocarbon group, comprises the steps of a) blending the esterified cellulose ether comprising groups of the formula —C(O)—R—COOH with an aqueous liquid and setting the temperature of the resulting blend to less than 10° C. to dissolve a portion of the esterified cellulose ether in the aqueous liquid, b) separating the non-dissolved portion of the esterified cellulose ether from the remainder of the blend, and c) recovering or disposing of the esterified cellulose ether that is dissolved in the aqueous liquid.

公开(公告)号：US20170355782A1

公开(公告)日：2017-12-14

申请号：US15541642

申请日：2016-01-04

Applicant: Dow Global Technologies LLC

Inventor： Roland Bayer ,  Oliver Petermann

IPC: C08B11/20 ,  C08B13/00 ,  C08B11/193

Abstract: A process for producing a water-soluble cellulose derivative of a reduced content of water-insoluble particles comprises the steps of a) reacting cellulose with an alkaline material to produce alkali cellulose, b) reacting the produced alkali cellulose with one or more derivatizing agents to produce a water-soluble cellulose derivative, c) washing the produced cellulose derivative with an aqueous liquid once or several times to provide a moist cellulose derivative having a water content of 25 to 85 percent, based on the total weight of the moist cellulose derivative, d) subjecting the moist cellulose derivative to homogenization to form the moist cellulose derivative to a paste, and e) pressing the paste through a filter of a pore size of up to 200 μm.

公开(公告)号：US20170240654A1

公开(公告)日：2017-08-24

申请号：US15503600

申请日：2015-08-18

Applicant: Dow Global Technologies LLC

Inventor： Oliver Petermann ,  Matthias Knarr ,  Matthias Sprehe

IPC: C08B13/00 ,  C09D101/32 ,  A61K9/48

CPC classification number: C08B13/00 ,  A61K9/146 ,  A61K9/2054 ,  A61K9/4816 ,  A61K47/38 ,  C08L1/32 ,  C09D101/32

Abstract: Esterified cellulose ethers which have i) as ester groups aliphatic monovalent acyl groups or 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 ii) a content of not more than 0.85 weight percent acetone-insoluble esterified cellulose ether particles, when the esterified cellulose ether is present in a mixture of 12.5 weight parts of esterified cellulose ether and 87.5 weight parts of acetone at 21° C., the weight percent acetone-insoluble esterified cellulose ether particles being based on the total weight of the esterified cellulose ether, wherein iii) not more than 14 percent of the acetone-insoluble esterified cellulose ether particles have a particle size of more than 90 micrometers.

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。

公开(公告)号：US20150218198A1

公开(公告)日：2015-08-06

申请号：US14421072

申请日：2013-08-15

Applicant: Dow Global Technologies LLC

Inventor： Oliver Petermann ,  Matthias Sprehe ,  Steven J. Guillaudeu

IPC: C07H3/06 ,  A61K9/48 ,  A61K47/38

CPC classification number: C07H3/06 ,  A61K9/1652 ,  A61K9/4891 ,  A61K47/38 ,  C08B11/20 ,  C08B13/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20150218197A1

公开(公告)日：2015-08-06

申请号：US14420921

申请日：2013-08-15

Applicant: DOW GLOBAL TECHNOLOGIES LLC

Inventor： Oliver Petermann ,  Matthias Sprehe ,  Robert L. Schmitt ,  Andrew C. Arthur ,  Warren K. Miller ,  David K. Lyon

IPC: C07H3/06

CPC classification number: C07H3/06 ,  C08B11/20 ,  C08B13/00

Abstract: Two or more esters of a cellulose ether, each having the same ether and ester substituents but different weight average molecular weights are prepared in a process which comprises the steps of esterifying a cellulose ether with (i) an aliphatic monocarboxylic acid anhydride or (ii) a dicarboxylic acid anhydride or (iii) a combination of an aliphatic monocarboxylic acid anhydride and a dicarboxylic acid anhydride in the presence of an aliphatic carboxylic acid as a reaction diluent in two or more separate reactions, wherein in each reaction a different molar ratio [aliphatic carboxylic acid/anhydroglucose units of cellulose ether] is used to produce esters of the cellulose ether of different weight average molecular weights.

Abstract translation: 在包括以下步骤的方法中制备两种或更多种纤维素醚的酯，它们各自具有相同的醚和酯取代基但不同的重均分子量，该方法包括以下步骤：（i）脂肪族单羧酸酐或（ii） 二羧酸酐或（iii）脂肪族单羧酸酐和二羧酸酐在脂肪族羧酸作为反应稀释剂的存在下在两个或更多个分开的反应中的组合，其中在每个反应中不同的摩尔比[脂族 纤维素醚的羧酸/脱水葡萄糖单元]用于生产不同重均分子量的纤维素醚的酯。

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。

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。