Powdery or granulated composition comprising a copolymer, a dicarboxylic acid and a fatty monocarboxylic acid

Patent metadata

Field	Value
Publication number	US-10113050-B2
Application number	US-200913322159-A
Country	US
Kind code	B2
Filing date	Jul 30, 2009
Priority date	Jul 30, 2009
Publication date	Oct 30, 2018
Grant date	Oct 30, 2018

Abstract

A powdery or granulated composition, containing: (a) a copolymer containing, in polymerized form, a C1- to C4-alkyl ester of acrylic or methacrylic acid and an alkyl(meth)acrylate monomer containing a tertiary amino group in an alkyl radical; (b) 0.5 to 10% by weight based on (a) of a dicarboxylic acid having 3 to 10 carbon atoms; and (c) 5 to 20% by weight based on (a) of a fatty monocarboxylic acid having 8 to 18 carbon atoms, where the composition contains at least by 30% by weight of (a), (b), and (c).

First claim

The invention claimed is:

1. A powdery or granulated composition, comprising at least 30% by weight of a mixture comprising:
(a) a copolymer comprising, in polymerized form, a C 1 - to C 4 -alkyl ester of acrylic or methacrylic acid and an alkyl(meth)acrylate monomer comprising a tertiary amino group in an alkyl radical;
(b) 0.5 to 10% by weight based on (a) of a dicarboxylic acid comprising 4 to 10carbon atoms; and
(c) 5 to 20% by weight based on (a) of a linear, saturated fatty monocarboxylic acid comprising 8 to 18 carbon atoms;
wherein
a molar ratio of the dicarboxylic acid to the tertiary amino groups of copolymer (a) is from 0.8/100 to 17/100,
a molar ratio of the fatty monocarboxylic acid to the tertiary amino groups of copolymer (a) is from 5/100 to 45/100, and
a dispersion or solution preparation time of the composition is less than 3 hours.

2. The composition of claim 1 , wherein the copolymer (a) comprises in polymerized form, 30 to 80% by weight of the C 1 - to C 4 -alkyl ester of acrylic or methacrylic acid and 70 to 20% by weight of the alkyl(meth)acrylate monomer comprising a tertiary amino group in the alkyl radical.

3. The composition of claim 1 , wherein the copolymer (a) comprises in polymerized form, 20 - 30% by weight of methyl methacrylate, 20 - 30% by weight of butyl methacrylate and 60 - 40% by weight of dimethylaminoethyl methacrylate.

4. The composition of claim 1 , wherein the dicarboxylic acid (b) is at least one selected from the group consisting of fumaric acid, malic acid, tartaric acid, and succinic acid.

5. The composition of claim 1 , wherein the fatty monocarboxylic acid (c) is at least one selected from the group consisting of caprylic acid, capric acid, lauric acid, palmitic acid, and stearic acid.

6. The composition of claim 1 , further comprising up to 200% by weight based on a total weight of (a), (b), and (c) of a pharmaceutical, a nutraceutical, or a cosmetical excipient which are different from (a), (b), and (c).

7. The composition of claim 6 , wherein the pharmaceutical, nutraceutical, or cosmetical excipient is at least one selected from the group consisting of an antioxidant, a brightener, a flavouring agent, a flow aid, a fragrance, a glidant (release agent), a penetration-promoting agent, a pigment, a plasticizer, a pore-forming agent, and a stabilizer.

8. The composition of claim 1 , wherein the composition is comprised in an aqueous dispersion,
wherein the aqueous dispersion is in a dispersed or dissolved form and has a dry weight content of 5 to 40% (weight/volume).

9. An aqueous dispersion or solution comprising the composition of claim 1 , obtained by a process comprising:
combining a dry powdery or granular mixture of (a), (b), and (c) with water;
stirring the dry powdery or granulate mixture into water at room temperature; and
further stirring and thereby dissolving the dry powdery or granulate mixture, to obtain a clear aqueous dispersion or solution, respectively,
wherein the aqueous dispersion or solution is obtained in less than 3 hours from beginning the stirring.

10. A process for preparing a composition of claim 1 , the process comprising:
combining (a), (b), and (c), wherein the combining is carried out by powder mixing, dry granulation, wet granulation, or melt granulation.

11. The process of claim 10 , wherein the combining is carried out by wet granulation, and wherein (a), (b), and (c) are in the form of an organic solution.

12. A process for coating a pharmaceutical, nutraceutical, or cosmetical composition, the process comprising:
contacting a composition of claim 1 with a pharmaceutical, nutraceutical, or cosmetical composition.

13. A process for binding a pharmaceutical, nutraceutical, or cosmetical composition, the process comprising:
contacting a binding agent comprising a composition of claim 1 with a pharmaceutical, nutraceutical, or cosmetical composition.

14. The powdery or granulated composition according to claim 1 , wherein the preparation time is the time point when substantially no particles are observed in a fluid under a polarization microscope with a magnification of 100-fold with the support of a phase filter when a less than 35% by weight of the composition is stirred in water at room temperature.

15. The powdery or granulated composition according to claim 2 , wherein the preparation time is the time point when substantially no particles are observed in a fluid under a polarization microscope with a magnification of 100-fold with the support of a phase filter when a less than 35% by weight of the composition is stirred in water at room temperature.

Assignees

• Roth Erna
• Alexowsky Ruediger
• Petereit Hans Ulrich
• Meier Christian
• Evonik Roehm Gmbh

Inventors

• Roth Erna
• Alexowsky Ruediger
• Petereit Hans-Ulrich
• Meier Christian

Classifications

• C08K5/09 Primary

  Carboxylic acids; Metal salts thereof; Anhydrides thereof · CPC title

• C08K5/092

  Polycarboxylic acids · CPC title

• C08J3/12

  Powdering or granulating · CPC title

• A61K47/30

  Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates · CPC title

• C08F20/10

  Esters · CPC title