Topical administration method

Patent metadata

Field	Value
Publication number	US-RE50060-E
Application number	US-201717899610-A
Country	US
Kind code	E1
Filing date	Jun 21, 2017
Priority date	Jun 23, 2016
Publication date	Jul 30, 2024
Grant date	Jul 30, 2024

Abstract

The present invention relates to a method for topical administration of ophthalmic compositions in a dropwise manner, preferably for topical administration of ophthalmic compositions comprising semifluorinated alkanes (SFAs). Further, the present invention relates to the use of said methods in the prevention or treatment of ocular diseases or disorders or any symptoms or conditions associated therewith. In a further aspect, the present invention relates to a kit comprising a drop dispenser at least partially filled with a liquid composition for the use in such a method and directions for use of said drop dispenser.

First claim

The invention claimed is:

1. A method for dropwise topical administration of a liquid composition ( 2 ), comprising the steps of:
a) providing a drop dispenser ( 1 ), comprising:
a container part ( 1 B) with an interior volume partially filled with the liquid composition ( 2 ) and a gaseous phase ( 3 ) filling the remainder of the interior volume at ambient pressure, the container part ( 1 B) having a displaceable section ( 1 C) and optionally a substantially stationary section, and
a dropper part ( 1 A) in physical connection and in fluid communication with the interior volume of the container part ( 1 B), comprising an outflow channel ( 5 ), connecting the interior volume of the container part ( 1 B) to the environment;

b) exerting a first force to the displaceable section ( 1 C) of the container part ( 1 B) of the drop dispenser ( 1 ) while holding the drop dispenser ( 1 ) in an upright position in which the outflow channel ( 5 ) is not in contact with the liquid composition ( 2 ), thereby reducing the interior volume of the container part ( 1 B) and forcing the gaseous phase ( 3 ) of the interior volume at least partially out of the drop dispenser ( 1 ) into the environment;
c) inverting the drop dispenser ( 1 ) to an inverted position in which the liquid composition ( 2 ) is in contact with the outflow channel ( 5 );
d) releasing said first force from the displaceable section ( 1 C) of the container part ( 1 B) at least partly, thereby reducing the pressure inside the container part ( 1 B) below ambient pressure; and
e) exerting a second force to the displaceable section ( 1 C) of the container part ( 1 B), while still holding the drop dispenser in the inverted position in which the liquid composition ( 2 ) is in contact with the outflow channel ( 5 ), thereby raising the pressure inside the interior volume of the container part ( 1 B) above ambient pressure and releasing the liquid composition ( 2 ) dropwise from the dropper part ( 1 A) of the drop dispenser ( 1 ).

2. The method according to claim 1 , wherein the drop dispenser ( 1 ) is a dropper bottle with a dropper part ( 1 A) and a container part ( 1 B), the container part ( 1 B) comprising the displaceable section ( 1 C).

3. The method according to claim 1 , wherein the inversion of the drop dispenser ( 1 ) to the inverted position according to step (c) and the release of the first force according to step (d) is performed at least partly simultaneously.

4. The method according to claim 1 , wherein the liquid composition ( 2 ) is an ophthalmic composition.

5. The method according to claim 1 , wherein the liquid composition ( 2 ) comprises a liquid semifluorinated alkane.

6. The method according to claim 1 , wherein the liquid composition ( 2 ) further comprises water.

7. The method according to claim 1 , wherein the reduced pressure generated inside the interior volume of the container part ( 1 B) prevents unintended release of the liquid composition ( 2 ).

8. The method according to claim 1 , wherein the liquid composition ( 2 ) has a density measured at 25° C. in the range of 1.0 to 1.7 g/cm 3 .

9. The method according to claim 1 , wherein the liquid composition ( 2 ) has a viscosity measured at 25° C. in air in the range of 0.9 to 4.0 mPa s.

10. The method according to claim 1 , wherein the liquid composition ( 2 ) has a surface tension in air measured at 25° C. in the range of 15 to 30 mN/m.

11. The method according to claim 1 , wherein the liquid composition ( 2 ) comprises a liquid linear or branched semifluorinated alkane having one perfluorinated segment and one non-fluorinated hydrocarbon segment.

12. The method according to claim 1 , wherein the liquid composition ( 2 ) further comprises one or more pharmaceutical active ingredients.

13. The method according to claim 1 , further comprising the step:
f) dropwise administering the liquid composition (2) to the eye, eye lid, eye sac or an ophthalmic tissue of a subject in need thereof.

14. A method of treating an ocular disease or disorder, or any symptoms or conditions associated therewith, comprising dropwise administration of a liquid ophthalmic composition according to the method of claim 1 .

15. The method according to claim 14 , wherein the ocular disease or disorder is dry eye disease.

16. The method according to claim 14 , wherein the ocular disease or disorder is a disease or disorder of the eyelid, lacrimal system, orbit, conjunctiva, sclera, cornea, iris, ciliary body, lens, choroid and/or retina.

17. The method according to claim 11 , wherein each segment independently has a number of carbon atoms selected from the range of 3 to 10 .

18. The method according to claim 5 , wherein the liquid semifluorinated alkane is selected from the group consisting of F4H5, F4H6, F5H6, F5H7, F6H6, F6H7, and F6H8.

19. The method according to claim 18 , wherein the liquid semifluorinated alkane is F4H5.

20. The method according to claim 18 , wherein the liquid semifluorinated alkane is F6H8.

21. The method according to claim 1 , wherein the liquid composition (2) is an ophthalmic composition comprising 1-perfluorohexyloctane (F6H8).

22. The method according to claim 1 , wherein the liquid composition (2) is an ophthalmic composition comprising 1 mg/ml Ciclosporine A and 1 wt-% ethanol in 1-perfluorobutyl-pentane (F4H5).

23. The method according to claim 22 , wherein the liquid composition (2) is an ophthalmic composition consisting essentially of 1 mg/ml Ciclosporine A and 1 wt-% ethanol in 1-perfluorobutyl-pentane (F4H5).

24. The method according to claim 21 , wherein the ophthalmic composition is administered to treat dry eye disease.

25. The method according to claim 22 , wherein the ophthalmic composition is administered to treat dry eye disease.

26. The method according to claim 13 , wherein the administering of the liquid composition (2) is carried out up to once per week, or up to once per day or up to 8, 7, 6, 5, 4, 3 or up to 2 times per day.

27. The method according to claim 1 , wherein the outflow channel (5) narrows from a proximal dropper mouth (7) to a distal duct opening (4).

28. The method according to claim 27 , wherein the drops to be released are formed at the dropper mouth (7) at the proximal end of the outflow channel (5).

29. The method according to claim 27 , wherein the duct opening (4) is circular.

30. The method according to claim 29 , wherein the duct opening (4) has a diameter in the range of from 0.15 to 1.2 mm, or in the range of from 0.18 to 0.5 mm, or in the range of from 0.2 to 0.3 mm.

31. The method according to claim 27 , wherein the diameter of the dropper mouth (7) is between 1 and 5 mm, or is between 2 and 3 mm, or is between 2.0 and 2.6 mm, or is about 2.0 to 2.4 mm.

32. The method according to claim 1 , wherein displaceable section (1C) comprises a deformable wall which is manually deformable.

33. The method according to claim 32 , wherein the displaceable section (1C) comprises a deformable wall having a wall thickness of between 0.4 and 1.6 mm, or between 0.5 and 1.0 mm, or between 0.6 and 0.8 mm.

34. The method according to claim 1 , wherein the exerting a first force of step (b), and the exerting a second force of step (e), are each provided by manually compressing or squeezing t

Assignees

• Novaliq Gmbh

Inventors

• Graf Gesche
• Ahmed Yasin
• Legner Stephanie
• Kemp Philip

Classifications

• A61F2230/0067

  conical · CPC title

• A61F2230/0023

  triangular · CPC title

• A61F9/0026 Primary

  Ophthalmic product dispenser attachments to facilitate positioning near the eye · CPC title

• A61P27/02

  Ophthalmic agents · CPC title

• A61K31/02

  Halogenated hydrocarbons · CPC title