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1. WO2020109192 - COMPOSITIONS D'ALCANES SEMI-FLUORÉS COMPORTANT DES ESTERS ÉTHYLIQUES D'ACIDES GRAS OMÉGA -3

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]

Claims

1. A stable liquid ophthalmic pharmaceutical composition comprising:

a) at least one omega-3 fatty acid ethyl ester in a total amount of up to 5 wt% based on the total weight of the composition;

b) a liquid paraffin in a total amount of up to 1 wt% based on the total weight of the composition;

wherein the at least one omega-3 fatty acid ethyl ester and the liquid paraffin are dissolved in a liquid vehicle comprising a semifluorinated alkane selected from 1-perfluorohexyl-octane (F6H8) or 1-perfluorobutyl-pentane (F4H5).

2. The composition according to any one of the preceding claims, wherein the total amount of liquid paraffin in wt% does not exceed the total amount of omega-3 fatty acid ethyl ester in wt%.

3. The composition according to claim 1 or 2, wherein the at least one omega 3 fatty acid ethyl ester is eicosapentaenoic acid ethyl ester, docosahexaenoic ethyl ester or a mixture thereof.

4. The composition according to any one of the preceding claims, wherein the liquid paraffin is light liquid paraffin.

5. The composition according to any one of the preceding claims, wherein the composition substantially consists of at least one omega- 3 fatty acid ethyl ester and a liquid paraffin dissolved in a semifluorinated alkane and optionally an antioxidant.

6. The composition according to any one of the claims 1 to 5, comprising or

consisting of up to 0.2 wt% of an omega- 3 fatty acid ethyl ester selected from docosahexaenoic acid ethyl ester, eicosapentaenoic acid ethyl ester or mixtures thereof, 0.2 wt% light liquid paraffin, dissolved in a liquid vehicle comprising a semifluorinated alkane selected from F4H5, F6H8 and mixtures thereof and optionally up to 0.1 wt% of antioxidant.

7. The composition according to any of the claims 1 to 5, comprising up to 0.2 wt% docosahexaenoic acid ethyl ester, 0.2 wt% light liquid paraffin, at least 99 wt% of a semifluorinated alkane selected from F4H5, F6H8 and mixtures thereof, and optionally up to 0.1 wt% of antioxidant.

8. The composition according to any of the claims 1 to 5, essentially consisting of 0.2 wt% docosahexaenoic acid ethyl ester, 0.2 wt% light liquid paraffin, dissolved in a semifluorinated alkane selected from F4H5, F6H8 and mixtures thereof and optionally up to 0.1 wt% of antioxidant.

9. The composition according to any of the claims 1 to 5, essentially consisting of 0.2 wt% docosahexaenoic acid ethyl ester, 0.2 wt% light liquid paraffin, 0.0133 wt% butylhydroxyanisol, and 0.0067 wt% butylhydroxytoluene dissolved in F6H8.

10. The composition according to any one of the preceding claims, wherein the composition retains more than 75 wt% for 3 months of omega-3 ethyl ester upon storage at 40°c at a relative humidity of 75%.

11. The composition according to any preceding claim, wherein the oxygen content of the composition is below 0.90 pg/ml.

12. The composition according to any one of the preceding claims for use as a

medicament.

13. The composition for use according to claim 12, wherein the composition is topically administered, preferably the composition is topically administered to the eye, to an eye surface, to the lacrimal sac, to the upper or lower eyelid or to an ophthalmic tissue.

14. The composition for use according to claim 12 or 13, for use in the prevention or treatment of dry eye disease (keratoconjunctivitis sicca), evaporative dry eye disease, dry eye disease associated with Meibomian Gland Dysfunction, Meibomian Gland Dysfunction or a symptom or condition associated therewith.

15. A kit comprising a container comprising the ophthalmic composition according to any one of claims 1 to 11, a dispensing means, and optionally instructions for use.

16. A method for stabilizing a composition comprising one or more omega-3 fatty acid ethyl esters as defined in any of the claims 1 to 11, comprising a step of mixing the one or more omega-3 fatty acid ethyl esters, a liquid paraffin and optionally one or more antioxidants, with a semifluorinated alkane to form a stable clear and colorless solution.