公开(公告)号：US20180134811A1

公开(公告)日：2018-05-17

申请号：US15574496

申请日：2016-05-26

Applicant: Dow Global Technologies LLC

Inventor： Roland Adden ,  Tirtha Chatterjee ,  Matthias Knarr ,  Meinolf Brackhagen

IPC: C08B11/02 ,  C08J3/12

CPC classification number: C08B11/02 ,  C08J3/12 ,  C08J3/122 ,  C08J3/14 ,  C08J2301/26 ,  C08J2301/28 ,  G01N23/20

Abstract: Provided is a composition in powder form comprising methylcellulose, wherein said composition has a powder x-ray diffraction spectrum at source x-ray wavelength of 1.789 Å showing a peak at a 2θ value between 14.5 and 16.5 degrees having intensity level Ipeak and a trough at a 2θ value between 16.51 and 20 degrees having intensity level Itrough, wherein a peak index PIndex is defined as PIndex=(Ipeak−Itrough)/Itrough and wherein said PIndex is 0.01 or greater.

公开(公告)号：US09937258B2

公开(公告)日：2018-04-10

申请号：US14890617

申请日：2014-07-16

Applicant: Dow Global Technologies LLC

Inventor： Jaime L. Curtis-Fisk ,  Susan L. Jordan ,  True L. Rogers ,  Matthias Knarr ,  Meinolf Brackhagen ,  Roland Adden

IPC: A61K47/38 ,  A61K47/02 ,  A61K31/167 ,  A61K9/00

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.

公开(公告)号：US09890220B2

公开(公告)日：2018-02-13

申请号：US14766609

申请日：2014-02-28

Applicant: Dow Global Technologies LLC

Inventor： Oliver Petermann ,  Meinolf Brackhagen ,  Matthias Sprehe

IPC: C08B13/00 ,  C08B11/20 ,  C08L1/32 ,  A61K9/48 ,  A61K9/14 ,  A61K9/28

CPC classification number: C08B13/00 ,  A61K9/146 ,  A61K9/2866 ,  A61K9/4816 ,  C08B11/20 ,  C08L1/32

Abstract: Esterified cellulose ethers which comprise (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 divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation, which have a viscosity of up 50 mPa·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C., and a weight average molecular weight Mw of at least 220,000 Dalton, or which have a viscosity of up 100 mPa·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C., and a weight average molecular weight Mw of at least 310,000 Dalton are useful for preparing solid dispersions comprising drugs.

公开(公告)号：US20160347866A1

公开(公告)日：2016-12-01

申请号：US15113921

申请日：2015-01-27

Applicant: DOW GLOBAL TECHNOLOGIES LLC

Inventor： Oliver Petermann ,  Matthias Sprehe ,  Meinolf Brackhagen

IPC: C08B13/00 ,  A61K9/10 ,  A61K9/48 ,  A61K47/38

CPC classification number: C08B13/00 ,  A61K9/10 ,  A61K9/146 ,  A61K9/2866 ,  A61K9/4816 ,  A61K47/38 ,  C08B11/20

Abstract: Esterified cellulose ethers which have i) as ester groups aliphatic monovalent acyl groups 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, ii) a weight average molecular weight Mw of from 80,000 Dalton to 220,000 Dalton, iii) a Polydispersity Mw/Mn of from 1.3 to 4.0, and iv) an Mz/Mn of not more than 18.5, when the weight average molecular weight Mw, the number average molecular weight Mn and the z-average molecular weight Mz are measured by SEC-MALLS using as mobile phase a mixture produced from 40 parts by volume of acetonitrile and 60 parts by volume of aqueous buffer containing 50 mM NaH2—PO4 and 0.1 M NaNO3. are useful as enteric polymers for pharmaceutical dosage forms.

Abstract translation: 酯化纤维素醚，其具有i）酯基脂族一价酰基或脂族一价酰基的组合和式-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，ii）重均分子量Mw为80,000道尔顿至220,000道尔顿，iii）多分散性Mw / Mn为1.3至4.0，以及iv）Mz / Mn不大于18.5，当重量 平均分子量Mw，数均分子量Mn和z平均分子量Mz通过SEC-MALLS使用由40体积份乙腈和60体积份含有50mM NaH2-PO4和0.1M NaNO3。 可用作药物剂型的肠溶性聚合物。

公开(公告)号：US20150202301A1

公开(公告)日：2015-07-23

申请号：US14421064

申请日：2013-08-15

Applicant: Dow Global Technologies LLC

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

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

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

Abstract: 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.

Abstract translation: 酯化纤维素醚，其具有i）脂族一价酰基和式-C（O）-R-COOA基团的组合，其中R是二价脂族或芳族烃基，A是氢或阳离子，ii）重量 平均分子量Mw为80,000道尔顿至350,000道尔顿，iii）多分散性Mw / Mn为1.3至4.1，以及iv）粘度高达4.0mPa·s，以2.0wt％的酯化纤维素醚溶液 在20℃下0.43重量％的NaOH水溶液可用作药物剂型的肠溶性聚合物。

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。

公开(公告)号：US20140024723A1

公开(公告)日：2014-01-23

申请号：US13942775

申请日：2013-07-16

Applicant: Dow Global Technologies LLC

Inventor： Meinolf Brackhagen ,  Robert L. Schmitt ,  Matthias Knarr

IPC: A61K47/38

CPC classification number: A61K47/38 ,  A61K9/146 ,  A61K9/2866 ,  A61K9/5047 ,  A61K9/5089

Abstract: A liquid composition which comprises an organic liquid diluent and at least one hydroxypropyl methylcellulose having 28 to 30 weight percent of methoxyl groups, 7 to 12 weight percent of hydroxypropoxyl groups and a sum of methoxyl groups and hydroxypropoxyl groups of from 38.5 to 42 weight percent 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 hydroxypropyl methylcellulose by spray-drying.Alternatively a solid dispersion can be produced by blending and extruding at least one active ingredient, at least one hydroxypropyl methylcellulose described above and optionally one or more adjuvants.

Abstract translation: 一种液体组合物，其包含有机液体稀释剂和至少一种羟甲基纤维素，其具有甲氧基28-30重量％，羟丙氧基7-12重量％，甲氧基和羟丙氧基之和为38.5至42重量％ 在延长的时间内稳定。 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。 或者，可以通过共混和挤出至少一种活性成分，至少一种上述羟丙基甲基纤维素和任选的一种或多种佐剂来制备固体分散体。

公开(公告)号：US10759873B2

公开(公告)日：2020-09-01

申请号：US15113921

申请日：2015-01-27

Applicant: Dow Global Technologies LLC

Inventor： Oliver Petermann ,  Matthias Sprehe ,  Meinolf Brackhagen

IPC: C08B13/00 ,  A61K9/10 ,  A61K47/38 ,  A61K9/48 ,  C08B11/20 ,  A61K9/14 ,  A61K9/28

Abstract: Esterified cellulose ethers which have i) as ester groups aliphatic monovalent acyl groups 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, ii) a weight average molecular weight Mw of from 80,000 Dalton to 220,000 Dalton, iii) a Polydispersity Mw/Mn of from 1.3 to 4.0, and iv) an Mz/Mn of not more than 18.5, when the weight average molecular weight Mw, the number average molecular weight Mn and the z-average molecular weight Mz are measured by SEC-MALLS using as mobile phase a mixture produced from 40 parts by volume of acetonitrile and 60 parts by volume of aqueous buffer containing 50 mM NaH2—PO4 and 0.1 M NaNO3. are useful as enteric polymers for pharmaceutical dosage forms.

公开(公告)号：US10577432B2

公开(公告)日：2020-03-03

申请号：US15574497

申请日：2016-05-26

Applicant: Dow Global Technologies LLC

Inventor： Roland Adden ,  Tirtha Chatterjee ,  Matthias Knarr ,  Meinolf Brackhagen

IPC: C08B11/20 ,  B01J2/04

Abstract: Provided is a method of making methylcellulose-type ether in powder form, said method comprising (a) providing a solution of said methylcellulose-type ether in water, and (b) then separating said methylcellulose-type ether from said water to produce dried methylcellulose-type ether, with the proviso that either (i) step (b) produces said methylcellulose-type ether in powder form, or (ii) after step (b), said method additionally comprises a step (c) of subjecting said dried methylcellulose-type ether to mechanical stress to produce said methylcellulose-type ether in powder form.

公开(公告)号：US10450424B2

公开(公告)日：2019-10-22

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: A61K47/38 ,  C08J3/07 ,  C08B13/00 ,  C09D101/32 ,  C08L1/32 ,  A61K9/10 ,  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.