Preservative containing compositions

Patent metadata

Field	Value
Publication number	US-2020206355-A1
Application number	US-202016808566-A
Country	US
Kind code	A1
Filing date	Mar 4, 2020
Priority date	Mar 4, 2016
Publication date	Jul 2, 2020
Grant date	—

Abstract

The present invention relates to compositions providing improved preservative efficacy. The present invention further relates to polyquaternium compound containing compositions having improved the antifungal activity. In certain embodiments, the present invention relates to ophthalmic compositions comprising a polyquaternium compound, a polyol or combination of polyols, borate compound, and an antimicrobial mixture comprising electrolytes and nutrients.

First claim

What is claimed is:

1 . A composition, comprising:
a) from about 0.0005% w/v to about 0.1000% w/v, of the total composition, of a polyquaternium compound; b) optionally, from about 0.2% w/v to about 2.0% w/v, of the total composition, of an amount of a polyol or combination polyols; c) from about 0.02% w/v to about 1.5% w/v, of the total composition, of a borate; and e) an antimicrobial mixture comprising:
iii. one or more nutrients; and
iv. optionally, one or more electrolytes
such that:
a. the total nutrient concentration, in the total composition, is from about 1.0 mMol/L to about 4.0 mMol/L of the composition; and
b. when present, the total electrolyte concentration, in the total composition, is from about 20.0 mMol/L to about 80.0 mMol/L of the composition.

2 . The composition of claim 1 wherein the polyquaternium compound has a weight average molecular weight of from about 150 to about 15,000 Daltons.

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

4 . The composition of claim 3 , wherein the polyquaternium compound has a weight average molecular weight of from about about 250 to about 12,000 Daltons.

5 . The composition of claim 1 , wherein the composition comprises from about 0.0010% w/v to about 0.0200% w/v, of the total composition, of the polyquaternium compound.

6 . The composition of claim 5 , wherein the composition comprises from about 0.0010% w/v to about 0.0050% w/v, of the total composition, of the polyquaternium compound.

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

8 . The composition of claim 7 , wherein the polyquaternium compound is polyquaternium-42.

9 . The composition of claim 1 , wherein the composition comprises from about 0.2% w/v to about 1.7% w/v, of the total composition, of the polyol.

10 . The composition of claim 9 , wherein the composition comprises from about 0.4% w/v to about 1.5% w/v, of the total composition, of the polyol.

11 . The composition of claim 1 , wherein the polyol is selected from the group consisting of sugars, sugar alcohols, sugar acids, uronic acids and mixtures thereof.

12 . The composition of claim 11 , wherein the polyol is selected from the group consisting of sugars, sugar alcohols, sugar acids and mixtures thereof.

13 . The composition of claim 12 , wherein the polyol is selected from the group consisting of mannitol, glycerin, polysorbate 80, propylene glycol, polyethylene glycol, sorbitol and mixtures thereof.

14 . The composition of claim 1 , wherein the composition comprises from about 0.04% w/v to about 1.0% w/v, of the total composition, of the borate.

15 . The composition of claim 14 , wherein the composition comprises from about 0.06% w/v to about 0.60% w/v, of the total composition, of the borate.

16 . The composition of claim 1 , wherein the borate is selected from the group consisting of sodium borate, potassium borate, calcium borate, magnesium borate, manganese borate; and mixtures thereof.

17 . The composition of claim 1 , wherein the total nutrient concentration, in the total composition, is from about 2.0 mMol/L to about 3.0 mMol/L of the composition.

18 . The composition of claim 17 , wherein the total nutrient concentration, in the total composition, is from about 2.8 mMol/L to about 3.0 mMol/L of the composition.

19 . The composition of claim 1 , wherein the total nutrient concentration of the composition comprises one or more of:
a. lactate at a concentration of from about 0 mMol/L to about 10.0 mMol/L of the total composition; b. citrate at a concentration of from about 0 mMol/L to about 0.5 mMol/L of the total composition; c. phosphate at a concentration of from about 0 mMol/L to about 10 mMol/L of the total composition d. glucose at a concentration of from about 0.1 mMol/L to about 25 mMol/L of the total composition; e. ascorbic acid at a concentration of from about 0.0003 mMol/L to about 0.0010 mMol/L of the total composition.

20 . The composition of claim 1 , wherein the total electrolyte concentration, in the total composition, is from about 30 mMol/L to about 70 mMol/L of the total composition.

21 . The composition of claim 20 , wherein the total electrolyte concentration, in the total composition, is from about 40 mMol/L to about 60 mMol/L of the composition.

22 . The composition of claim 1 , wherein the total electrolyte concentration comprises one or more of:
a. potassium at a concentration of from about 24 mMol/L to about 28 mMol/L of the total composition; b. sodium at a concentration of from about 5 mMol/L to about 10 mMol/L of the total composition; c. magnesium at a concentration of from about 0.50 mMol/L to about 0.80 mMol/L of the total composition; and d. chloride at a concentration of from about 23 mMol/L to about 28 mMol/L of the total composition.

23 . A method for treating or preventing dry eye comprising the step of applying the composition of claim 1 to a subject in need of such treatment or prevention.

24 . A method for treating or preventing minor eye irritation comprising the step of applying the composition of claim 1 to a subject in need of such treatment or prevention.

25 . A method for treating or preventing eye allergy comprising the step of applying the composition of claim 1 to a subject in need of such treatment or prevention.

26 . A method for improving overall preservative efficacy of a liquid composition, comprising the step of combining:
a) from about 0.0005% w/v to about 0.1000% w/v, of the total composition, of a polyquaternium compound; b) optionally, from about 0.2% w/v to about 2.0% w/v, of the total composition, of an amount of a polyol or combination polyols; c) from about 0.02% w/v to about 1.5% w/v, of the total composition, of a borate; and d) an antimicrobial mixture comprising:
i. one or more nutrients; and
ii. optionally, one or more electrolytes
such that:
a. the total nutrient concentration, in the total composition, is from about 1.0 mMol/L to about 4.0 mMol/L of the composition; and
c. when present, the total electrolyte concentration, in the total composition, is from about 20.0 mMol/L to about 80.0 mMol/L of the composition.

27 . The method of claim 26 , wherein the preservative efficacy of the liquid composition satisfies the criteria of the EP B Criteria described in the Specification.

28 . The method of claim 27 , wherein the liquid composition is an aqueous liquid preparation.

29 . A method for improving antifungal activity of a liquid composition, comprising the step of combining:
a) from about 0.0005% w/v to about 0.1000% w/v, of the total composition, of a polyquaternium compound; b) optionally, from about 0.2% w/v to about 2.0% w/v, of the total composition, of an amount of a polyol or combination polyols; c) from about 0.02% w/v to about 1.5% w/v, of the total composition, of a borate; and d) an antimicrobial mixture comprising:
i. one or more nutrients; and
ii. optionally, one or more electrolytes
such that:
a. the total nutrient concentration, in the total composition, is from about 1.0 mMol/L to about 4.0 mMol/L of the composition; and
c. when pre

Assignees

• Johnson & Johnson Consumer Inc

Inventors

• Bai Mingqi
• Holeva Kenneth T

Classifications

• A61P31/10

  Antimycotics · CPC title

• A61P29/02

  without antiinflammatory effect · CPC title

• A61K47/38 Primary

  Cellulose; Derivatives thereof · CPC title

• A61K33/22

  Boron compounds · CPC title

• A61K33/14

  Alkali metal chlorides; Alkaline earth metal chlorides · CPC title