Ophthalmic composition

Patent metadata

Field	Value
Publication number	US-2020000923-A1
Application number	US-201916565983-A
Country	US
Kind code	A1
Filing date	Sep 10, 2019
Priority date	Oct 31, 2014
Publication date	Jan 2, 2020
Grant date	—

Abstract

The present invention relates to ophthalmic compositions for treatment of conditions in the eye. More specifically, the present invention relates to ophthalmic compositions comprising a polyquaternium compound and an anionic polymer. Methods for reducing and/or preventing the incompatibility of polyquaternium compounds with anionic polymers are also disclosed.

First claim

What is claimed is:

1 . A composition comprising:
a. from about 10 ppm to about 1000 ppm of a polyquaternium compound having a weight average molecular weight of from about 150 to about 15,000 Daltons; b. from about 0.001% to about 0.5% of an anionic polymer having a weight average molecular weight of from about 250 to about 4,000,000 Daltons; and c. an effective amount of an organic acid, salts thereof or mixtures thereof, such that the organic acid binds with the polyquaternium compound at at least a 1:1 molar ratio;
wherein the composition is substantially free of cationic oligomer compounds and precipitation inhibiting compounds.

2 . The composition of claim 1 wherein the polyquaternium compound has weight average molecular weight of from about 200 to about 13,500 Daltons.

3 . The composition of claim 2 wherein the polyquaternium compound is selected from the group consisting of polyquaternium-1, polyquaternium-10, polyquaternium-42 or mixtures thereof.

4 . The composition of claim 3 wherein the polyquaternium compound is polyquaternium-42.

5 . The compositions of claim 1 wherein the anionic polymer has a weight average molecular weight of from about from about 100,000 to about 3,000,000 Daltons.

6 . The composition of claim 5 wherein the anionic polymer is selected from the group consisting of alginates; carageenans; carbomers, high molecular weight, non-linear polyacrylic acid cross-linked with polyalkenyl polyethers; sodium carboxymethylcellulose; internally cross-linked sodium carboxymethylcelluloses; gellan gum; hyaluronic acid; pectin; xanthan gum; alkylvinyl ether/maleic anhydride copolymer; and mixtures of thereof.

7 . The composition of claim 6 wherein the anionic polymer is selected from the group consisting of hyaluronic acid, gellan gum, alkylvinyl ether/maleic anhydride copolymer and mixtures thereof.

8 . The composition of claim 7 wherein the anionic polymer is hyaluronic acid.

9 . The composition of claim 7 wherein the anionic polymer is gellan gum.

10 . The composition of claim 7 wherein the anionic polymer is an alkyl vinyl ether/maleic anhydride copolymer.

11 . The composition of claim 10 wherein the anionic polymer is a free acid of alkyl vinyl ether/maleic anhydride copolymer.

12 . The composition of claim 1 wherein the organic acid is selected from the group consisting of carboxylic acids, dicarboxylic acids, tricarboxylic acids and mixtures thereof.

13 . The composition of claim 12 wherein the organic acid is a carboxylic acid.

14 . The composition of claim 13 wherein the carboxylic acid is selected from the group consisting of formic acid, acetic acid, propionic acid, salts thereof, and mixtures thereof.

15 . The composition of claim 12 wherein the organic acid is a dicarboxylic acid.

16 . The composition of claim 15 wherein the dicarboxylic acid is selected from the group consisting of glutaric acid, maleic acid, tartaric acid, salts thereof, and mixtures thereof.

17 . The composition of claim 16 wherein the dicarboxylic acid is tartaric acid.

18 . The composition of claim 12 wherein the organic acid is a tricarboxylic acid.

19 . The composition of claim 18 wherein the tricarboxylic acid is selected from the group consisting of citric acid, isocitric acid, aconitic acid, trimesic acid, propane-1,2,3-tricarboxylic acid and mixtures thereof.

20 . The composition of claim 19 wherein the tricarboxylic acid is citric acid.

21 . A method of reducing, inhibiting or preventing the precipitation of a polyquaternium compound and an anionic polymer in a composition comprising such compounds, comprising the steps of:
i) providing from about 0.001% to about 0.5% of an anionic polymer having a weight average molecular weight of from about 250 to about 4,000,000 Daltons; ii) adding an effective amount of an organic acid, salts thereof or mixtures thereof, such that the organic acid binds with the monomer units of the polyquaternium compound at at least a 1:1 molar ratio; and iii) adding from about 10 ppm to about 1000 ppm of a polyquaternium compound having a weight average molecular weight of from about 150 to about 15,000 Daltons;
wherein the composition is substantially free of cationic oligomer compounds and precipitation inhibiting compounds.

Assignees

• Johnson & Johnson Consumer Inc

Inventors

• Bai Mingqi
• Holeva Kenneth T

Classifications

• A61P27/04

  Artificial tears; Irrigation solutions · CPC title

• A61P27/02

  Ophthalmic agents · CPC title

• A61K47/18

  Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids · CPC title

• A61K9/0048 Primary

  Eye, e.g. artificial tears · CPC title

• A61K47/34

  Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence) · CPC title