Semifluorinated alkane compositions

Patent metadata

Field	Value
Publication number	US-10576154-B2
Application number	US-201816041317-A
Country	US
Kind code	B2
Filing date	Jul 20, 2018
Priority date	Sep 12, 2012
Publication date	Mar 3, 2020
Grant date	Mar 3, 2020

Abstract

The invention provides novel compositions comprising semifluorinated alkanes and at least one compound sensitive or prone to oxidation. The compositions can be used as medicines that are topically administered to an eye or ophthalmic tissue. The invention further provides kits comprising such compositions.

First claim

The invention claimed is:

1. A method of treating a disease or disorder of the eye wherein the disease or disorder is either (a) meibomian gland dysfunction and symptoms or conditions associated therewith or (b) keratoconjunctivitis sicca (dry eye) and symptoms or conditions associated therewith, in a patient in need of such treatment, comprising topically administering an effective amount of a stable liquid composition to an eye or ophthalmic tissue of the patient,
wherein the composition consists of a semifluorinated alkane of the formula F(CF 2 )n(CH 2 )mH, wherein n is an integer from 3 to 8 and m is an integer from 3 to 10, and optionally one or more excipients.

2. The method according to claim 1 , wherein the semifluorinated alkane is selected from F(CF 2 ) 4 (CH 2 ) 5 H, F(CF 2 ) 4 (CH 2 ) 6 H, F(CF 2 ) 4 (CH 2 ) 8 H, F(CF 2 ) 6 (CH 2 ) 4 H, F(CF 2 ) 6 (CH 2 ) 6 H, F(CF 2 ) 6 (CH 2 ) 8 H, and F(CF 2 ) 6 (CH 2 ) 10 H.

3. The method according to claim 1 , wherein the semifluorinated alkane is F(CF 2 ) 6 (CH 2 ) 8 H.

4. The method according to claim 1 , wherein the composition consists of F(CF 2 ) 6 (CH 2 ) 8 H.

5. The method according to claim 1 , wherein the disease or disorder is meibomian gland dysfunction and wherein the symptom associated with meibomian gland dysfunction is selected from itchiness, redness, swelling, pain or soreness, discharge accumulation or crusting at the lid margins.

6. The method according to claim 1 , wherein the disease or disorder is meibomian gland dysfunction and wherein the meibomian gland dysfunction is characterized by gland duct obstructions and/or qualitative and/or quantitative changes to the secretions of the glands.

7. The method according to claim 1 , wherein the composition is topically administered to the cornea, the conjunctiva or to the upper or lower eye lid margins, meibomian gland ducts, eye lashes or any area of the eye or eye lid anatomy.

8. The method according to claim 1 , wherein the disease or disorder is keratoconjunctivitis sicca and the condition associated with keratoconjunctivitis sicca is selected from Sjogren syndrome, lacrimal gland insufficiency, meibomian gland disease and meibomian gland dysfunction.

9. The method according to claim 1 , wherein the disease or disorder is keratoconjunctivitis sicca and the symptom associated with keratoconjunctivitis sicca is selected from dry, scratchy, gritty, or sandy feeling in the eye; foreign body sensation; pain or soreness; stinging or burning; itching; increased blinking; eye fatigue; photophobia; blurry vision; redness; mucus discharge; contact lens intolerance; excessive reflex tearing.

10. The method according to claim 1 , wherein the disease or disorder is keratoconjunctivitis sicca and the condition associated with keratoconjunctivitis sicca is meibomian gland dysfunction and wherein the composition consists of F(CF 2 ) 6 (CH 2 ) 8 H.

11. The method according to claim 1 , wherein the disease or disorder is meibomian gland dysfunction and the composition consists of F(CF 2 ) 6 (CH 2 ) 8 H.

12. The method according to claim 1 , wherein the disease or disorder is keratoconjunctivitis sicca and the composition consists of F(CF 2 ) 6 (CH 2 ) 8 H.

13. The method according to claim 1 , wherein the composition consists of the semifluorinated alkane and one or more excipients selected from the group consisting of lipids, oils, lubricants, lipophilic vitamins, viscosity agents, antioxidants, surfactants, and mixtures thereof.

14. The method according to claim 13 , wherein the one or more excipients are selected from triglyceride oils, mineral oil, medium chain triglycerides (MCT), oily fatty acids, isopropyl myristate, oily fatty alcohols, esters of sorbitol and fatty acids, oily sucrose esters, oily cholesterol esters, oily wax esters, glycerophospholipids, sphingolipids, and any oily substance which is physiologically tolerated by the eye.

15. The method according to claim 14 , wherein the triglyceride oils are selected from soybean oil, olive oil, sesame oil, cotton seed oil, castor oil, and sweet almond oil, and wherein the mineral oil is selected from petrolatum and liquid paraffin.

16. The method according to claim 1 , wherein the disease or disorder is keratoconjunctivitis sicca, and wherein the direct or indirect cause of the keratoconjunctivitis sicca is meibomian gland dysfunction.

17. The method according to claim 1 , wherein the disease or disorder is keratoconjunctivitis sicca, and wherein the symptom or condition associated therewith is selected from aqueous deficient dry eye disease or evaporative dry eye disease.

18. The method according to claim 1 , wherein the disease or disorder is meibomian gland dysfunction and wherein the meibomian gland dysfunction is characterized by abnormal, reduced or increased delivery of lipids to the tear film.

19. The method according to claim 1 , wherein the disease or disorder is keratoconjunctivitis sicca and wherein the keratoconjunctivitis sicca is characterized by abnormal, reduced or increased delivery of lipids to the tear film.

Assignees

• Novaliq Gmbh

Inventors

• Günther Bernhard
• Scherer Dieter
• Pettigrew Anthony
• Theisinger Bastian
• Theisinger Sonja

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P37/02

  Immunomodulators · CPC title

• A61P5/38

  of the suprarenal hormones · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title