Artificial tear emulsion

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

1. An eye lotion being a stable oil-in-water emulsion, without surfactants other than phospholipid, having an osmolarity of 110 to 180 mOsm/1 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, which is a triglyceride whose three hydroxyl groups are esterified by fatty acids comprising from 8 to 12 carbon atoms, at least one stabilizing polymer selected from cellulose polymers, water, and a salt selected from potassium chloride, sodium chloride or potassium and/or sodium carbonate.

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

3. The eye lotion according to claim 1 wherein said eye lotion has a turbidity of 0 to 5,000 NTU.

4. The eye lotion according to claim 1 wherein said eye lotion comprises from 0 to 10 ppm of preservatives and/or EDTA.

5. The eye lotion according to claim 1 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.

6. The eye lotion according to claim 1 wherein said phospholipid is selected from lecithins.

7. The eye lotion according to claim 1 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.

8. The eye lotion according to claim 1 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.

9. The eye lotion according to claim 1 wherein said cellulose polymer is carboxymethylcellulose.

10. The eye lotion according to claim 1 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.

11. The eye lotion according to claim 1 wherein said eye lotion has a pH of 5.5 to 8.

12. The eye lotion according to claim 1 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.

13. The eye lotion according to claim 1 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.

14. An eye lotion being a stable oil-in-water emulsion, without surfactants other than phospholipid, having an osmolarity of 110 to 180 mOsm/1, and comprising: 0.01 to 5% by weight of at least one mucomimetic polymer, said mucomimetic polymer being selected from glycosaminoglycans and hyaluronic acids, 0.01 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 which is a triglyceride whose three hydroxyl groups are esterified by fatty acids comprising from 8 to 12 carbon atoms, 0.01% to 5% by weight of at least one stabilizing polymer, said stabilizing polymer being selected from cellulose polymers, from 0 to 10 ppm of preservatives and/or EDTA, and a salt selected from potassium chloride, sodium chloride or potassium and/or sodium carbonate water.

15. The eye lotion according to claim 14 wherein said eye lotion has a viscosity lower than or equal to 10.sup.−1 Pa.Math.s.

16. The eye lotion according to claim 14 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.

17. The eye lotion of claim 1 further including at least one buffer selected from the group consisting of phosphate buffer, acetate buffer and citrate buffer.

18. The eye lotion of claim 14 further including at least one buffer selected from the group consisting of phosphate buffer, acetate buffer and citrate buffer.

19. The eye lotion of claim 1 having a weight ratio of lipid other than phospholipid to phospholipid between 0.2 to 5.0.

20. The eye lotion of claim 14 having a weight ratio of lipid other than phospholipid to phospholipid between 0.2 to 5.0.

21. A method for treating ophthalmic diseases comprising administering in the eye(s) of a patient in need thereof an efficient amount of the eye lotion according to claim 1.

22. A method for treating 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 1.

23. A method for preparing an eye lotion according to claim 1, said method comprising the following steps: a) mix the at least one phospholipid and the at least one lipid other than the phospholipid which is a triglyceride whose three hydroxyl groups are esterified by fatty acids comprising from 8 to 12 carbon atoms, b) dissolve the at least one mucomimetic polymer in a buffer, c) dissolve the at least one 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 by adding respectively a base or an acid and/or control and adjust the osmolarity, and f) sterilize the emulsion.

24. The method of claim 23, wherein the eye lotion is sterilized by filtration.

25. The method of claim 24, wherein the eye lotion is filtered on a 0.22 μm filter.

Description

EXAMPLES

(1) The examples below are eye lotions containing an oil-in-water emulsion and a mucomimetic polymer, intended in particular for restoring the various layers of the lacrimal film in patients suffering from dry eye syndrome. They are prepared with the following ingredients given for a centesimal composition. These formulas have a pH of roughly 7.1 and are hypotonic to tears.

Example 1

(2) TABLE-US-00001 Oily phase: Triglycerides 0.05% Lecithin 0.1% Aqueous phase: Chondroitin sulfate 0.2% Polyvinyl alcohol 0.2% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 2

(3) TABLE-US-00002 Oily phase: Triglycerides 0.2% Lecithin 0.1% Aqueous phase: Sodium hyaluronate 0.2% Polysorbate 0.2% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 3

(4) TABLE-US-00003 Oily phase: Triglycerides 0.05% Lecithin 0.1% Aqueous phase: Dextran sulfate 0.2% Sodium hydroxypropylmethylcellulose 0.2% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 4

(5) TABLE-US-00004 Oily phase: Triglycerides 0.05% Lecithin 0.1% Aqueous phase: Heparin 0.2% Polyvinylpyrrolidone 0.1% Sodium carboxymethylcellulose 0.1% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 5

(6) TABLE-US-00005 Oily phase: Triglycerides 0.05% Lecithin 0.1% Aqueous phase: Sodium alginate 0.1% Polyvinyl alcohol 0.1% Sodium carboxymethylcellulose 0.2% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 6

(7) TABLE-US-00006 Oily phase: Triglycerides 0.1% Lecithin 0.1% Aqueous phase: Sodium hyaluronate 0.2% Sodium carboxymethylcellulose 0.1% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 7

(8) TABLE-US-00007 Oily phase: Triglycerides 0.1% Lecithin 0.1% Aqueous phase: Sodium hyaluronate 0.2% Sodium carboxymethylcellulose 0.05% Polyvinyl alcohol 0.1% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 8

(9) TABLE-US-00008 Oily phase: Triglycerides 0.05% Lecithin 0.1% Aqueous phase: Sodium hyaluronate 0.2% Polyvinyl alcohol 0.2% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 9

(10) TABLE-US-00009 Oily phase: Triglycerides 0.2% Lecithin 0.1% Aqueous phase: Sodium hyaluronate 0.2% Polysorbate 0.1% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 10

(11) TABLE-US-00010 Oily phase: Triglycerides 0.05% Lecithin 0.1% Aqueous phase: Sodium hyaluronate 0.2% Sodium hydroxypropylmethylcellulose 0.2% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 11

(12) TABLE-US-00011 Oily phase: Triglycerides 0.1% Lecithin 0.1% Aqueous phase: Sodium hyaluronate 0.2% Sodium carboxymethylcellulose 0.1% Sodium hydroxypropylmethylcellulose 0.1% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 12

(13) TABLE-US-00012 Oily phase: Triglycerides 0.05% Lecithin 0.1% Aqueous phase: Sodium hyaluronate 0.2% Sodium carboxymethylcellulose 0.1% Polyvinylpyrrolidone 0.1% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.

Example 13

(14) TABLE-US-00013 Oily phase: Triglycerides 0.05% Lecithin 0.1% Aqueous phase: Sodium hyaluronate 0.2% Sodium carboxymethylcellulose 0.1% Polyvinyl alcohol 0.1% Citric acid 0.05M Sodium citrate 0.05M Sodium chloride q.s. Distilled water q.s.