COMPOSITIONS COMPRISING MIXTURES OF SEMIFLUORINATED ALKANES

• US 20150224064A1
• Filed: 09/12/2013
• Published: 08/13/2015
• Est. Priority Date: 09/12/2012
• Status: Active Grant

• Current Assignee: Novaliq GmbH
• Original Assignee: Novaliq GmbH
• Inventors: Gnther, Bernhard, Theisinger, Bastian, Theisinger, Sonja, Scherer, Dieter
• Granted Patent: US 10,449,164 B2
• Time in Patent Office: Days
• US Class Current: 1/1
• CPC Class Codes: A61K 31/02 Halogenated hydrocarbons
• CPC Class Codes: A61K 47/06 Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/00 Drugs for disorders of the senses
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/04 Artificial tears; Irrigation solutions

Abstract

The invention provides novel compositions comprising at least two or more semifluorinated alkanes. The compositions can be used as medicines that are topically administered to an eye or ophthalmic tissue, such as for use in the treatment of keratoconjunctivitis sicca (dry eye) and/or meibomian gland dysfunction and symptoms associated therewith. The invention further provides kits comprising such compositions.

Claims

1. A composition comprising:

a first semifluorinated alkane of the formula F(CF₂)_n(CH₂)_mH, wherein n is an integer from the range of 3 to 8 and m is an integer from the range of 3 to 10, and

a second semifluorinated alkane of the formula F(CF₂)_n(CH₂)_mH, wherein n is an integer from the range of 6 to 20 and m is an integer from the range of 10 to 20.

2. The composition according to claim 1, consisting of said first semifluorinated alkane, said second semifluorinated alkane, and optionally one or more further excipients.

3. The composition of claim 1, wherein the first semifluorinated alkane is selected from a group consisting of F(CF₂)₄(CH₂)₅H, F(CF₂)₄(CH₂)₆H, F(CF₂)₆(CH₂)₆H, F(CF₂)₆(CH₂)₈H, and F(CF₂)₆(CH₂)₁₀H, and/or wherein the second semifluorinated alkane is selected from a group consisting of F(CF₂)₈(CH₂)₁₀H and F(CF₂)₁₀(CH₂)₁₂H.

4. The composition of claim 1, wherein the weight ratio of the first semifluorinated alkane to the second semifluorinated alkane is at least about 3:

1.

5. The composition of claim 1, comprising one or more excipients selected from lipids, oils, omega-3 fatty acids, omega-6 fatty acids and lipophilic vitamins or any derivatives or mixtures thereof.

6. The composition of claim 1, further comprising a semifluorinated alkane of the general formula F(CF₂)_n(CH₂)_mH and/or the general formula F(CF₂)_n(CH₂)_m(CF₂)_oF.

7. The composition of claim 1, wherein the composition is a liquid solution, gel, emulsion, microemulsion, suspension or spray.

9. A method of treating a disease or condition of a patient in need of such treatment, comprising administering an effective amount of the composition of claim 1 to the patient, wherein the composition is topically administered to an eye or ophthalmic tissue.

10. The method of claim 9, wherein the disease or condition of the patient is keratoconjunctivitis sicca (dry eye) or a symptom or condition associated therewith.

11. The method of claim 9, wherein the disease or condition of the patient is meibomian gland dysfunction or a symptom or condition associated therewith.

12. The method of claim 9 in the palliative treatment and care of an eye or ophthalmic tissue.

14. The composition of claim 1, wherein the composition is a cleansing solution for the eye or ophthalmic tissue.

15. A kit comprising the composition claim 1 and a container for holding the composition, wherein the container has a dispensing means adapted for topical administration of the composition to an eye or ophthalmic tissue.

8. (canceled)

13. (canceled)