Pharmaceutical composition for treatment of increased intraocular pressure

• US 10,045,996 B2
• Filed: 03/16/2011
• Issued: 08/14/2018
• Est. Priority Date: 03/17/2010
• Status: Active Grant

• Current Assignee: Novaliq GmbH
• Original Assignee: Novaliq GmbH
• Inventors: Theisinger, Bastian, Theisinger, Sonja, Gunther, Bernhard
• Primary Examiner(s): Lundgren, Jeffrey S
• Assistant Examiner(s): Springer, Stephanie K
• Application Number:
  US13/581,396
• Publication Number:
  US 20130046014A1
• Time in Patent Office: 2,708 Days
• Field of Search: None
• CPC Class Codes: A61K 31/5575 having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
• 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: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics

Abstract

The invention provides novel pharmaceutical compositions for the treatment of increased intraocular pressure based on semifluorinated alkanes which are useful as carriers for a broad range of active ingredients. Preferred active ingredients include poorly water-soluble prostaglandin analogues. The compositions can be administered topically into the eye. The invention further provides kits comprising such compositions.

Claims

1. A pharmaceutical composition comprising:

(a) a therapeutically effective amount of a poorly water-soluble prostaglandin analogue selected from the group consisting of latanoprost, bimatoprost, tafluprost, travoprost and unoprostone, and

(b) a liquid vehicle comprising a semifluorinated alkane selected from F4H5, F4H6, F6H6 and F6H8;

wherein the composition is substantially free of water and free of a preservative and is adapted for topical administration to the conjunctiva or the corneal surface of an eye of a patient; and

wherein the composition is formulated as a solution, emulsion or suspension.

2. The composition of claim 1, wherein the active ingredient is latanoprost.

3. The composition of claim 2, wherein the concentration of latanoprost is from about 0.001 wt.-% to about 0.01 wt.-%.

4. The composition of claim 1, wherein the composition is formulated as a solution.

5. The composition of claim 1, further comprising an organic cosolvent.

6. The composition of claim 5, comprising ethanol at a concentration of about 1.5 wt.-% or less, or of about 1.0 wt.-% or less.

7. A pharmaceutical kit comprising the composition of claim 1 and a container holding the composition, wherein the container has a dispensing means adapted for topically administering the composition to the eye of a patient.

8. The composition of claim 2, wherein the semifluorinated alkane is F4H5, being formulated as a solution.

9. The composition of claim 8, further comprising an organic co-solvent.

10. The composition of claim 9, wherein the organic co-solvent is ethanol at a concentration of about 1.5 wt.-% or less.

11. The composition of claim 10, wherein the concentration of latanoprost is from about 0.001 wt.-% to about 0.01 wt.-%.