Lipid-based ophthalmic emulsion

Patent metadata

Field	Value
Publication number	US-10925892-B2
Application number	US-201916281316-A
Country	US
Kind code	B2
Filing date	Feb 21, 2019
Priority date	Feb 21, 2018
Publication date	Feb 23, 2021
Grant date	Feb 23, 2021

Abstract

The present invention is directed to a lipid-based ophthalmic emulsion. The emulsion has an increased amount of a mucoadhesive galactomannan polymer that promotes a long-lasting protection against desiccation and moisture retention.

First claim

We claim:

1. An ophthalmic emulsion, the emulsion comprising:
water forming an aqueous phase;
oil forming an oil phase;
a hydrophilic surfactant having an HLB value from 10 to 18;
a hydrophobic surfactant having an HLB value from 1 to 6;
a charged phospholipid;
borate;
a mucoadhesive galactomannan polymer; and
a preservative;
wherein the mucoadhesive galactomannan polymer is present in the emulsion at a concentration of at least about 0.13 w/v % but no greater than 0.3 w/v %;
wherein the preservative is free of a benzalkonium chloride; and
wherein the ophthalmic emulsion has a hydration protection against desiccation of at least 10% higher than a control emulsion, wherein the control emulsion has the same composition of the ophthalmic emulsion except of containing 0.05 w/v % of the same galactomannan polymer used in the ophthalmic emulsion.

2. The emulsion as in claim 1 wherein the oil is a hydrocarbon selected from mineral oil, paraffin oil and petrolatum.

3. The emulsion as in claim 1 wherein the oil is at least 0.1 w/v % and no greater than 3 w/v % of the emulsion.

4. The emulsion as in claim 3 wherein the hydrophilic surfactant is present in the emulsion in an amount that is at least 0.08 w/v % and is no greater than about 0.8 w/v %.

5. The emulsion as in claim 4 wherein the hydrophilic surfactant is polyoxyethylene-40-stearate.

6. The emulsion as in claim 4 wherein the hydrophobic surfactant is at least about 0.01 w/v % and is no greater than 2.0 w/v %.

7. The emulsion as in claim 6 wherein the hydrophobic surfactant is a sorbitan tristearate.

8. The emulsion as in claim 1 wherein the mucoadhesive galactomannan polymer is selected from the group consisting of guar and hydroxypropyl guar.

9. The emulsion as in claim 8 wherein the charged phospholipid is an anionic phospholipid named dimyristoyl phosphatidylglycerol.

10. The emulsion as in claim 1 further comprising a borate/polyol buffer system.

11. The emulsion as in claim 10 wherein the preservative is a polymeric quaternary ammonium compound.

12. The emulsion as in claim 1 , wherein:
i. the oil phase is in droplets within the aqueous phase and the droplets have a D 90 diameter that is no greater than about 700 nm but is at least 10 nm; and
ii. the borate and galactomannan polymer cooperatively act to form a gel upon instillation of the emulsion in an eye of an individual.

13. The emulsion as in claim 12 , wherein the oil phase is in droplets within the aqueous phase and the droplets have a D 90 diameter that is no greater than about 500 nm but is at least 30 nm.

14. The emulsion as in claim 13 , wherein the oil phase is in droplets within the aqueous phase and the droplets have a D 90 diameter that is no greater than about 300 nm but is at least 50 nm.

Assignees

• Novartis Ag
• Alcon Inc

Inventors

• Ketelson Howard Allen
• Davis James W
• Rangarajan Rekha

Classifications

• A61K47/24

  containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids · CPC title

• A61K9/1075

  Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence) · CPC title

• A61K47/36

  Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin · CPC title

• C09K23/017

  Mixtures of compounds · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title