# US 2013/0156867 A1 · Artificial Tear Emulsion

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- Number: US 2013/0156867 A1
- Document ID: US20130156867A1
- Status: Published application
- Kind: A1
- Application number: 13/642,580
- Filed: 2011-04-21
- Published: 2013-06-20
- Earliest claimed: 2010-04-21
- Assignees: Horus Pharma
- Inventors: Claude Claret; Martine Claret; Carole Gard; Nicola Lamprecht-Weissenborn
- Web page: https://patentgrep.com/patent/US20130156867A1

## CPC

- A61K 31/726: Glycosaminoglycans, i.e. mucopolysaccharides (chondroitin sulfate, dermatan sulfate A61K31/737)
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)}
- A61K 31/728: Hyaluronic acid
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/34: 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)
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 27/02: Ophthalmic agents
- A61P 27/04: Artificial tears; Irrigation solutions
- A61P 27/14: Decongestants or antiallergics
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to an oil-in-water emulsion comprising at least one mucomimetic polymer, at least one lipid of phospholipid type, at least one lipid other than the phospholipid, at least one stabilizing polymer, and a hydrophilic liquid, to an emulsion comprising an aqueous phase that contains at least one stabilizing polymer and at least one mucomimetic polymer, and an oily phase that contains at least one lipid of phospholipid type and a lipid other than the phospholipid, to a medicament comprising one of these emulsions, and to the use of one of these emulsions as an agent for restoring and/or replacing the lachrimal film or as a carrier for an active compound.

## Claims

### Claim at position 1

1-24. (canceled)

### Claim 25

An eye lotion being an oil-in-water emulsion, said oil-in-water emulsion comprising:
at least one mucomimetic polymer selected from glycosaminoglycans and hyaluronic acids,
at least one phospholipid,
at least one lipid other than the phospholipid,
at least one stabilizing polymer selected from polyvinyl alcohol polymers, polysorbates and cellulose polymers,
water.

### Claim 26 (depends on 25)

The eye lotion according to claim 25 wherein said eye lotion has a viscosity lower than or equal to 10−1 Pa·s.

### Claim 27 (depends on 25)

The eye lotion according to claim 25 wherein said eye lotion has an osmolarity ranging from 100 to 300 mOsm/l.

### Claim 28 (depends on 25)

The eye lotion according to claim 25 wherein said eye lotion has a turbidity of 0 to 5,000 NTU.

### Claim 29 (depends on 25)

The eye lotion according to claim 25 wherein said composition comprises from 0 to 0.1% by weight of surfactant in relation to the total weight of the eye lotion.

### Claim 30 (depends on 25)

The eye lotion according to claim 25 wherein said eye lotion comprises from 0 to 10 ppm of preservatives and/or EDTA.

### Claim 31 (depends on 25)

The eye lotion according to claim 25 wherein said phospholipid is present in a concentration of 0.01% to 3% by weight in relation to the total weight of the composition and wherein said phospholipid is selected from phosphoacylglycerides, phosphosphingolipids, phosphonosphingolipids, phosphoglycolipids and phosphosaccharolipids.

### Claim 32 (depends on 25)

The eye lotion according to claim 25 wherein said phospholipid is selected from lecithins.

### Claim 33 (depends on 25)

The eye lotion according to claim 25 wherein said eye lotion comprises a lipid other than the phospholipid in a concentration of 0.01% to 5% by weight in relation to the total weight of the composition and wherein said lipid other than the phospholipid is a glyceride.

### Claim 34 (depends on 25)

The eye lotion according to claim 25 wherein said eye lotion comprises a stabilizing polymer in a concentration of 0.01% to 5% by weight in relation to the total weight of the composition.

### Claim 35 (depends on 25)

The eye lotion according to claim 25 wherein said cellulose polymer is carboxymethylcellulose.

### Claim 36 (depends on 25)

The eye lotion according to claim 25 wherein said mucomimetic polymer is present in a concentration of 0.01% to 5% by weight in relation to the total weight of the composition.

### Claim 37 (depends on 25)

The eye lotion according to claim 25 wherein said eye lotion has a pH of 5.5 to 8.

### Claim 38 (depends on 25)

The eye lotion according to claim 25 further comprising an active agent selected from the group consisting of antiseptics, antibiotics, antivirals, anti-inflammatories, anti-allergy agents, anti-glaucoma agents, anti-dryness agents, vasoconstrictors, anesthetics, mydriatics, miotics, diagnostic products, products for treating retinal diseases and combinations thereof.

### Claim 39 (depends on 25)

The eye lotion according to claim 25 further comprising a substance helping to restore the composition of the lacrimal film's aqueous layer selected from the group consisting of vitamin A, vitamin B, vitamin B12, albumin, sodium, potassium, calcium, chloride, bicarbonate ions, buffer composition and combinations thereof.

### Claim 40

An eye lotion being an oil-in-water emulsion comprising:
0.01 to 5% by weight of at least one mucomimetic polymer, said mucomimetic polymer being selected from glycosaminoglycans and hyaluronic acids,
01 to 3% by weight of at least one phospholipid, said phospholipid being selected from phosphoacylglycerides, phosphosphingolipids, phosphonosphingolipids, phosphoglycolipids and phosphosaccharolipids,
0.01 to 5% by weight of at least one lipid other than the phospholipid, said lipid other than the phospholipid being a glyceride,
0.01% to 5% by weight of at least one stabilizing polymer, said stabilizing polymer being selected from polyvinyl alcohol polymers, polysorbates and cellulose polymers,
from 0 to 0.1% by weight of surfactant in relation to the total weight of the eye lotion,
from 0 to 10 ppm of preservatives and/or EDTA,
water.

### Claim 41 (depends on 40)

The eye lotion according to claim 40 wherein said eye lotion has a viscosity lower than or equal to 10−1 Pa·s.

### Claim 42 (depends on 40)

The eye lotion according to claim 40 wherein said eye lotion has an osmolarity ranging from 100 to 300 mOsm/l.

### Claim 43 (depends on 40)

The eye lotion according to claim 40 further comprising an active agent selected from the group consisting of antiseptics, antibiotics, antivirals, anti-inflammatories, anti-allergy agents, anti-glaucoma agents, anti-dryness agents, vasoconstrictors, anesthetics, mydriatics, miotics, diagnostic products, products for treating retinal diseases and combinations thereof.

### Claim 44 (depends on 25)

A method for treating or preventing ophthalmic diseases comprising administering in the eye(s) of a patient in need thereof an efficient amount of the eye lotion according to claim 25.

### Claim 45 (depends on 25)

A method for treating or preventing ocular dryness, allergies and/or inflammation of the eye comprising administering in the eye(s) of a patient in need thereof an efficient amount of the eye lotion according to claim 25.

### Claim 46 (depends on 25)

A method for preparing an eye lotion according to claim 25, said method comprising the following steps:
a) mix a phospholipid and a lipid other than the phospholipid,
b) dissolve a mucomimetic polymer in a buffer,
c) dissolve a stabilizing polymer in the aqueous phase of step b),
d) disperse the oily phase of step a) in the aqueous phase of step c) by agitation,
e) control and adjust the pH, notably by adding respectively a base or an acid and/or control and adjust the osmolarity, and
f) sterilize the emulsion.

### Claim 47 (depends on 46)

The method of claim 46, wherein the eye lotion is sterilized by filtration.

### Claim 48 (depends on 46)

The method of claim 46, wherein the eye lotion is filtered on a 0.22 μm filter.
