公开(公告)号：US20150376299A1

公开(公告)日：2015-12-31

申请号：US14766786

申请日：2014-02-28

Applicant: DOW GLOBAL TECHNOLOGIES LLC

Inventor： Oliver Petermann ,  Robert B. Appell ,  Meinolf Brackhagen

IPC: C08B13/00 ,  A61K47/38

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

Abstract: An esterified cellulose ether which 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, and which has a) a viscosity of from 1.2 to 1.8 mPaos, measured as a 2.0 wt % solution of the esterified cellulose ether in 0.43 wt % aqueous NaOH at 20° C., or b) a viscosity of up to 5 mPa·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C., or c) a combination of the viscosities of a) and b), is useful for preparing solid dispersions comprising drugs.

Abstract translation: 酯化纤维素醚，其包含（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，其具有a）粘度为1.2至1.8mPaos，以2.0wt％的酯化纤维素溶液 醚，在20℃下在0.43wt％NaOH水溶液中，或b）粘度高达5mPa·s，以20wt％的酯化纤维素醚在丙酮中的10wt％溶液测量，或c） a）和b）的粘度的组合可用于制备包含药物的固体分散体。

公开(公告)号：US20150374831A1

公开(公告)日：2015-12-31

申请号：US14766997

申请日：2014-02-28

Applicant: DOW GLOBAL TECHNOLOGIES LLC

Inventor： Meinolf Brackhagen ,  Steven J. Guillaudeu ,  Nicholas S. Grasman ,  Oliver Petermann ,  Robert L. Schmitt ,  Matthias Sprehe

IPC: A61K47/38 ,  C08B13/00

CPC classification number: A61K47/38 ,  A61K9/2866 ,  A61K9/4891 ,  C08B13/00

Abstract: Esterified cellulose ethers which comprise (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, which have a viscosity of up to 2.33 mPa·s, measured as a 2.0 wt % solution of the esterified cellulose ether in 0.43 wt % aqueous NaOH at 20° C., and which have a viscosity of up to 13 mPao·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C. are useful for preparing solid dispersions comprising drugs.

Abstract translation: 酯化纤维素醚，其包含（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，其粘度高达2.33mPa·s，以2.0重量％的酯化纤维素醚溶液测量为0.43 20℃下的重量％NaOH水溶液，其粘度高达13mPao·s，以20wt％的酯化纤维素醚在丙酮中的10wt％溶液测量，可用于制备包含药物的固体分散体 。

公开(公告)号：US11000594B2

公开(公告)日：2021-05-11

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

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：US10272156B2

公开(公告)日：2019-04-30

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

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：US20180282526A1

公开(公告)日：2018-10-04

申请号：US15764498

申请日：2016-09-29

Applicant: Dow Global Technologies LLC

Inventor： Oliver Petermann ,  Matthias Knarr ,  Meinolf Brackhagen

IPC: C08L1/32 ,  C08B13/00 ,  A61K47/38 ,  A61K9/48 ,  A23L33/10 ,  A23P10/30 ,  B29C41/14

Abstract: An aqueous composition which is useful for producing coatings and capsule shells comprises a) dispersed particles of 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 divalent hydrocarbon group and A is hydrogen or a cation, and the total degree of ester substitution is more than 0.70, and b) an esterified cellulose ether comprising aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOH, R being a divalent hydrocarbon group, wherein 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 0.70, and III) the esterified cellulose ether b) has a solubility in water of at least 2.0 weight percent at 2° C.

公开(公告)号：US09617351B2

公开(公告)日：2017-04-11

申请号：US14766786

申请日：2014-02-28

Applicant: Dow Global Technologies LLC

Inventor： Oliver Petermann ,  Robert B. Appell ,  Meinolf Brackhagen

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

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

Abstract: An esterified cellulose ether which 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, and which has a) a viscosity of from 1.2 to 1.8 mPaos, measured as a 2.0 wt % solution of the esterified cellulose ether in 0.43 wt % aqueous NaOH at 20° C., or b) a viscosity of up to 5 mPa·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C., or c) a combination of the viscosities of a) and b), is useful for preparing solid dispersions comprising drugs.

公开(公告)号：US09486532B2

公开(公告)日：2016-11-08

申请号：US14766997

申请日：2014-02-28

Applicant: Dow Global Technologies LLC

Inventor： Meinolf Brackhagen ,  Steven J. Guillaudeu ,  Nicholas S. Grasman ,  Oliver Petermann ,  Robert L. Schmitt ,  Matthias Sprehe

IPC: A61K47/38 ,  C08B13/00 ,  A61K9/28 ,  A61K9/48

CPC classification number: A61K47/38 ,  A61K9/2866 ,  A61K9/4891 ,  C08B13/00

Abstract: Esterified cellulose ethers which comprise (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, which have a viscosity of up to 2.33 mPa·s, measured as a 2.0 wt % solution of the esterified cellulose ether in 0.43 wt % aqueous NaOH at 20° C., and which have a viscosity of up to 13 mPao·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C. are useful for preparing solid dispersions comprising drugs.

Abstract translation: 酯化纤维素醚，其包含（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，其粘度高达2.33mPa·s，以2.0重量％的酯化纤维素醚溶液测量为0.43 20℃下的重量％NaOH水溶液，其粘度高达13mPao·s，以20wt％的酯化纤维素醚在丙酮中的10wt％溶液测量可用于制备包含药物的固体分散体 。

公开(公告)号：US20150368365A1

公开(公告)日：2015-12-24

申请号：US14766569

申请日：2014-02-28

Applicant: DOW GLOBAL TECHNOLOGIES LLC

Inventor： Oliver Petermann ,  Meinolf Brackhagen ,  Matthias Sprehe ,  Robert B. Appell

IPC: C08B13/00 ,  A61K47/38

CPC classification number: C08B13/00 ,  A61K9/2866 ,  A61K9/4816 ,  A61K47/38

Abstract: Esterified cellulose ethers which comprise (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, which have a viscosity of up 19 mPa·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C., and which have a weight average molecular weight Mw of at least 90,000 Dalton, are useful for preparing solid dispersions comprising drugs.

Abstract translation: 酯化纤维素醚，其包含（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，其粘度为19mPa·s，以酯化纤维素醚在丙酮中的10wt％溶液测量 20℃，其重均分子量Mw至少为90,000道尔顿，可用于制备包含药物的固体分散体。

公开(公告)号：US20150320869A1

公开(公告)日：2015-11-12

申请号：US14804489

申请日：2015-07-21

Applicant: Dow Global Technologies LLC

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

IPC: A61K47/38 ,  A61K9/50

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乙基甲基纤维素，其具有甲氧基28-30重量％，羟丙氧基7-12重量％，甲氧基和羟基丙氧基之和为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：US20150057356A1

公开(公告)日：2015-02-26

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: A61K47/38 ,  B29C47/00 ,  A61K9/20 ,  A61K31/192

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。