Ophthalmic compositions comprising F6H8

Patent metadata

Field	Value
Publication number	US-12569452-B2
Application number	US-202418439258-A
Country	US
Kind code	B2
Filing date	Feb 12, 2024
Priority date	Oct 4, 2017
Publication date	Mar 10, 2026
Grant date	Mar 10, 2026

Abstract

The present disclosure provides methods of treatment using ophthalmic compositions comprising semifluorinated alkanes for keratoconjunctivitis sicca and/or Meibomian gland dysfunction, which methods provide for the enrichment of an ophthalmic tissue in the semifluorinated alkane, and optionally methods of delayed release of the semifluorinated alkane from the enriched ophthalmic tissue to the surface of the cornea and/or conjunctiva, and/or to the Meibomian gland.

First claim

The invention claimed is:

1 . A method of providing delayed ophthalmic release of a semifluorinated alkane, wherein the method comprises the steps of (a) administering to the eye of a patient in need thereof an amount of an ophthalmic composition consisting of a mixture of F(CF 2 ) 6 (CH 2 ) 8 H and 2-perfluorohexyloctane, wherein the amount is effective to enrich an ophthalmic tissue in F(CF 2 ) 6 (CH 2 ) 8 H, and (b) delayed release of F(CF 2 ) 6 (CH 2 ) 8 H from the enriched ophthalmic tissue;
wherein the ophthalmic composition is administered to the surface of the cornea and/or the conjunctiva in the form of liquid drops; wherein the patient suffers from keratoconjunctivitis sicca (dry eye disease); and wherein the patient is non-responsive to physical methods of treating Meibomian Gland Dysfunction.

2 . A method of treating keratoconjunctivitis sicca (dry eye disease) due to Meibomian gland dysfunction, wherein the method comprises the steps of (a) administering to the eye of a patient in need thereof an amount of an ophthalmic composition consisting of a mixture of F(CF 2 ) 6 (CH 2 ) 8 H and 2-perfluorohexyloctane, wherein the amount is effective to enrich an ophthalmic tissue in F(CF 2 ) 6 (CH 2 ) 8 H, and optionally (b) delayed release of F(CF 2 ) 6 (CH 2 ) 8 H from the enriched ophthalmic tissue;
wherein the ophthalmic composition is administered to the surface of the cornea and/or the conjunctiva in the form of liquid drops; wherein the patient suffers from keratoconjunctivitis sicca (dry eye disease); and wherein the patient is non-responsive to physical methods of treating Meibomian Gland Dysfunction.

3 . The method according to claim 2 , wherein the composition consists of F(CF 2 ) 6 (CH 2 ) 8 H and up to 3 wt % of 2-perfluorohexyloctane, based on the total weight of the composition.

4 . The method according to claim 2 , wherein the physical methods of treating Meibomian Gland Dysfunction are selected from heat compresses, eye lid massaging, and forced expression of the Meibomian glands.

5 . The method according to claim 2 , wherein the composition is administered in a dose of a single drop per eye less than four times per day.

6 . The method according to claim 2 , wherein the composition is administered in a dose of a single drop of 10-12 μl per eye two times per day.

7 . The method of claim 2 , wherein the patient is characterized by at least 2 of the criteria selected from the group consisting of:
(i) a total ocular surface disease index (OSDI) of higher than 25; (ii) a total corneal fluorescein staining (NEI scale) between 4 and 11; (iii) a Schirmer's Test I greater than 5 mm; and (iv) an MGD score of higher than 3.

8 . The method according to claim 2 , wherein the composition consists of F(CF 2 ) 6 (CH 2 ) 8 H and up to 1 wt % of 2-perfluorohexyloctane, based on the total weight of the composition.

9 . A method of treating keratoconjunctivitis sicca (dry eye disease), wherein the method comprises the steps of (a) administering to the eye of a patient in need thereof an amount of an ophthalmic composition consisting of a mixture of F(CF 2 ) 6 (CH 2 ) 8 H and 2-perfluorohexyloctane, wherein the amount is effective to enrich an ophthalmic tissue in F(CF 2 ) 6 (CH 2 ) 8 H, and optionally (b) delayed release of F(CF 2 ) 6 (CH 2 ) 8 H from the enriched ophthalmic tissue;
wherein the ophthalmic composition is administered to the surface of the cornea and/or the conjunctiva in the form of liquid drops; wherein the patient suffers from keratoconjunctivitis sicca (dry eye disease); and wherein the patient is non-responsive to physical methods of treating Meibomian Gland Dysfunction.

10 . The method according to claim 9 , wherein the composition consists of F(CF 2 ) 6 (CH 2 ) 8 H and up to 3 wt % of 2-perfluorohexyloctane, based on the total weight of the composition.

11 . The method according to claim 9 , wherein the physical methods of treating Meibomian Gland Dysfunction are selected from heat compresses, eye lid massaging, and forced expression of the Meibomian glands.

12 . The method according to claim 9 , wherein the composition is administered in a dose of a single drop per eye less than four times per day.

13 . The method according to claim 9 , wherein the composition is administered in a dose of a single drop of 10-12 μl per eye two times per day.

14 . The method of claim 9 , wherein the patient is characterized by at least 2 of the criteria selected from the group consisting of:
(i) a total ocular surface disease index (OSDI) of higher than 25; (ii) a total corneal fluorescein staining (NEI scale) between 4 and 11; (iii) a Schirmer's Test I greater than 5 mm; and (iv) an MGD score of higher than 3.

15 . The method according to claim 9 , wherein the composition consists of F(CF 2 ) 6 (CH 2 ) 8 H and up to 1 wt % of 2-perfluorohexyloctane, based on the total weight of the composition.

16 . The method according to claim 1 , wherein the composition consists of F(CF 2 ) 6 (CH 2 ) 8 H and up to 1 wt % of 2-perfluorohexyloctane, based on the total weight of the composition.

17 . The method according to claim 1 , wherein the composition consists of F(CF 2 ) 6 (CH 2 ) 8 H and up to 3 wt % of 2-perfluorohexyloctane, based on the total weight of the composition.

18 . The method according to claim 1 , wherein the physical methods of treating Meibomian Gland Dysfunction are selected from heat compresses, eye lid massaging, and forced expression of the Meibomian glands.

19 . The method according to claim 1 , wherein the composition is administered in a dose of a single drop per eye less than four times per day.

20 . The method according to claim 1 , wherein the composition is administered in a dose of a single drop of 10-12 μl per eye two times per day.

21 . The method of claim 1 , wherein the patient is characterized by at least 2 of the criteria selected from the group consisting of:
(i) a total ocular surface disease index (OSDI) of higher than 25; (ii) a total corneal fluorescein staining (NEI scale) between 4 and 11; (iii) a Schirmer's Test I greater than 5 mm; and (iv) an MGD score of higher than 3.

Assignees

• Novaliq Gmbh

Inventors

• Günther Bernhard
• LÖSCHER Frank
• Voss Hartmut
• Krösser Sonja
• Eickhoff Kirsten
• Willen Daniela
• Beier Markus
• Schlüter Thomas

Classifications

• A61K9/0048

  Eye, e.g. artificial tears · CPC title

• A61P27/04

  Artificial tears; Irrigation solutions · CPC title

• A61P27/02

  Ophthalmic agents · CPC title

• A61K31/02 Primary

  Halogenated hydrocarbons · CPC title