公开(公告)号：US20180215880A1

公开(公告)日：2018-08-02

申请号：US15746207

申请日：2016-07-08

Applicant: Dow Global Technologies LLC

Inventor： Meinolf Brackhagen ,  Neal J. Fetner ,  Matthias Knarr ,  Jin Zhao

IPC: C08J3/07 ,  C09D101/32 ,  C08J3/12

Abstract: A process for producing an aqueous composition comprising a dispersed esterified cellulose ether comprises the steps of grinding, in the presence of an aqueous diluent an esterified cellulose ether comprising (i) groups of the formula —C(O)—R—COOA or (ii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein R is a N divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation, blending a salt of a fatty acid with the esterified cellulose ether and choosing the amounts of aqueous diluent, esterified cellulose ether and salt of a fatty acid that the produced aqueous composition comprises at least 20 percent of the dispersed esterified cellulose ether and heating the aqueous composition to a temperature of from 37 to 80 C during or after the grinding step.

公开(公告)号：US09616036B2

公开(公告)日：2017-04-11

申请号：US14390046

申请日：2013-04-08

Applicant: Dow Global Technologies LLC

Inventor： Meinolf Brackhagen ,  Roland Adden ,  Oliver Petermann ,  Robert L. Sammler ,  David E. Wallick

IPC: A61K31/167 ,  A61K9/20 ,  C08B11/08 ,  C08B11/193 ,  C08L1/28

CPC classification number: A61K31/167 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2095 ,  C08B11/08 ,  C08B11/193 ,  C08L1/284

Abstract: 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.

公开(公告)号：US09364546B2

公开(公告)日：2016-06-14

申请号：US14389838

申请日：2013-04-08

Applicant: Dow Global Technologies LLC

Inventor： Nicholas S. Grasman ,  True L. Rogers ,  Oliver Petermann ,  Meinolf Brackhagen ,  Roland Adden

IPC: A61K9/14 ,  A61K47/38 ,  C08B11/193 ,  C08L1/28 ,  A61K9/16 ,  A61K9/20 ,  A61K31/192 ,  B29C47/00 ,  B29K1/00 ,  B29K105/00

CPC classification number: A61K47/38 ,  A61K9/1652 ,  A61K9/2095 ,  A61K31/192 ,  B29C47/004 ,  B29C47/0066 ,  B29C2793/009 ,  B29K2001/08 ,  B29K2105/0035 ,  C08B11/193 ,  C08L1/28 ,  C08L1/284

Abstract: A melt-extruded polymer composition comprising a) at least one cellulose ether, b) one or more active ingredients and c) one or more optional additives, wherein said at least one cellulose ether has an MS (hydroxyalkyl) of 0.05 to 0.55 and hydroxyl groups of anhydroglucose units are substituted with methyl groups such that [s23/s26−0.2*MS(hydroxyalkyl)] is 0.32 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: 一种熔融挤出的聚合物组合物，其包含a）至少一种纤维素醚，b）一种或多种活性成分和c）一种或多种任选的添加剂，其中所述至少一种纤维素醚具有0.05至0.55的MS（羟烷基）和羟基 脱水葡萄糖单元的基团被甲基取代，使得[s23 / s26-0.2 * MS（羟烷基）]为0.32以下，其中s23是脱水葡萄糖单元的摩尔分数，其中只有2位和3位的两个羟基， 脱水葡萄糖单元的位置被甲基取代，其中s26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6-位上的两个羟基仅被甲基取代。

公开(公告)号：US20150209436A1

公开(公告)日：2015-07-30

申请号：US14413080

申请日：2013-07-12

Applicant: Dow Global Technologies LLC

Inventor： Meinolf Brackhagen ,  Nicholas S. Grasman ,  Mark J. Hall ,  Steven J. Guillaudeu ,  Robert L. Schmitt ,  Matthias Knarr

IPC: A61K47/38 ,  A61K31/343 ,  A61K31/4166 ,  A61K9/14

CPC classification number: A61K47/38 ,  A61K9/10 ,  A61K9/146 ,  A61K9/1652 ,  A61K9/2866 ,  A61K31/343 ,  A61K31/4166 ,  C08L1/284

Abstract: A liquid composition which comprises an organic liquid diluent and at least one non-ionic cellulose ether having a viscosity of up to 2.33 mPa·s, measured as a 2 wt.-% solution in water at 20° C., is stable over an extended time period. The liquid composition is useful for preparing a solid dispersion comprising at least one active ingredient in at least one cellulose ether by spray-drying. Alternatively a solid dispersion can be produced by blending and extruding at least one active ingredient, at least one cellulose ether having a viscosity of up to 2.33 mPa·s and optionally one or more adjuvants.

Abstract translation: 包含有机液体稀释剂和至少一种具有高达2.33mPa·s的非离子纤维素醚的非离子纤维素醚的液体组合物，其在20℃下以2重量％的水溶液测量，在 延长时间 液体组合物可用于通过喷雾干燥制备包含至少一种纤维素醚中的至少一种活性成分的固体分散体。 或者，可以通过共混和挤出至少一种活性成分，至少一种粘度高达2.33mPa·s的纤维素醚和任选的一种或多种佐剂来制备固体分散体。

公开(公告)号：US20150057358A1

公开(公告)日：2015-02-26

申请号：US14390046

申请日：2013-04-08

Applicant: Dow Global Technologies LLC

Inventor： Meinolf Brackhagen ,  Roland Adden ,  Oliver Petermann ,  Robert L. Sammler ,  David E. Wallick

IPC: A61K31/167 ,  A61K9/20

CPC classification number: A61K31/167 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2095 ,  C08B11/08 ,  C08B11/193 ,  C08L1/284

Abstract: 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 anhydrogluclose 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.

Abstract translation: 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起始溶解温度为至少40℃的纤维素醚形成，其具有通过1-4键连接且具有甲基，羟基烷基和任选的烷基不同的脱水葡萄糖单元 由甲基作为取代基，使得纤维素醚具有0.05至1.00的MS（羟基烷基），并且脱甲羟基化单元的羟基被甲基取代，使得[s23 / s26-0.2 * MS（羟烷基）]为0.31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。

公开(公告)号：US20190209693A1

公开(公告)日：2019-07-11

申请号：US16357687

申请日：2019-03-19

Applicant: Dow Global Technologies LLC

Inventor： Meinolf Brackhagen ,  Nicholas S. Grasman ,  Mark J. Hall ,  Steven J. Guillaudeu ,  Robert L. Schmitt ,  Matthias Knarr

IPC: A61K47/38 ,  A61K9/10 ,  A61K31/4166 ,  A61K31/343 ,  A61K9/16 ,  C08L1/28 ,  A61K9/28 ,  A61K9/14

CPC classification number: A61K47/38 ,  A61K9/10 ,  A61K9/146 ,  A61K9/1652 ,  A61K9/2866 ,  A61K31/343 ,  A61K31/4166 ,  C08L1/284

Abstract: A liquid composition which comprises an organic liquid diluent and at least one non-ionic cellulose ether having a viscosity of up to 2.33 mPa·s, measured as a 2 wt.-% solution in water at 20° C., is stable over an extended time period. The liquid composition is useful for preparing a solid dispersion comprising at least one active ingredient in at least one cellulose ether by spray-drying. Alternatively a solid dispersion can be produced by blending and extruding at least one active ingredient, at least one cellulose ether having a viscosity of up to 2.33 mPa»s and optionally one or more adjuvants.

公开(公告)号：US20190184020A1

公开(公告)日：2019-06-20

申请号：US16281700

申请日：2019-02-21

Applicant: Dow Global Technologies LLC

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

IPC: A61K47/38 ,  A61K9/10 ,  C08B11/20 ,  C08B13/00

CPC classification number: A61K47/38 ,  A61K9/10 ,  C08B11/20 ,  C08B13/00

Abstract: A process for making esterified cellulose ethers which have i) 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, ii) a weight average molecular weight Mw of from 80,000 Dalton to 350,000 Dalton, iii) a Polydispersity Mw/Mn of from 1.3 to 4.1, and iv) a viscosity of up to 4.0 mPa·s, measured as a 2.0 wt % solution of the esterified cellulose ether in 0.43 wt % aqueous NaOH at 20° C., are useful as enteric polymers for pharmaceutical dosage forms.

公开(公告)号：US09757465B2

公开(公告)日：2017-09-12

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: A01N43/50 ,  A61K31/415 ,  A61K47/38 ,  A61K9/08 ,  C08B11/193 ,  C08B11/20 ,  C09D101/28 ,  C08L1/28 ,  A61K9/16 ,  A61K31/343 ,  A61K31/4166 ,  A61K47/10

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.

公开(公告)号：US09745387B2

公开(公告)日：2017-08-29

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 ,  A61K9/28 ,  A61K9/14

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.

公开(公告)号：US20170028069A1

公开(公告)日：2017-02-02

申请号：US15292914

申请日：2016-10-13

Applicant: Dow Global Technologies LLC

Inventor： Meinolf Brackhagen ,  Nicholas S. Grasman ,  Mark J. Hall ,  Steven J. Guillaudeu ,  Robert L. Schmitt ,  Matthias Knarr

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

CPC classification number: A61K47/38 ,  A61K9/10 ,  A61K9/146 ,  A61K9/1652 ,  A61K9/2866 ,  A61K31/343 ,  A61K31/4166 ,  C08L1/284

Abstract: A liquid composition which comprises an organic liquid diluent and at least one non-ionic cellulose ether having a viscosity of up to 2.33 mPa·s, measured as a 2 wt.-% solution in water at 20° C., is stable over an extended time period.The liquid composition is useful for preparing a solid dispersion comprising at least one active ingredient in at least one cellulose ether by spray-drying.Alternatively a solid dispersion can be produced by blending and extruding at least one active ingredient, at least one cellulose ether having a viscosity of up to 2.33 mPa·s and optionally one or more adjuvants.

Abstract translation: 或者，可以通过共混和挤出至少一种活性成分，至少一种粘度高达2.33mPa·s的纤维素醚和任选的一种或多种佐剂来制备固体分散体。