Pharmaceutical composition for treatment of increased intraocular pressure

Patent metadata

Field	Value
Publication number	US-10045996-B2
Application number	US-201113581396-A
Country	US
Kind code	B2
Filing date	Mar 16, 2011
Priority date	Mar 17, 2010
Publication date	Aug 14, 2018
Grant date	Aug 14, 2018

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.

First claim

The invention claimed is:

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.-%.

Assignees

• Theisinger Bastian
• Theisinger Sonja
• Guenther Bernhard
• Novaliq Gmbh

Inventors

• Theisinger Bastian
• Theisinger Sonja
• Günther Bernhard

Classifications

• A61P27/06

  Antiglaucoma agents or miotics · CPC title

• A61P27/02

  Ophthalmic agents · CPC title

• A61K9/0048

  Eye, e.g. artificial tears · CPC title

• A61K47/24

  containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids · CPC title

• A61K31/5575 Primary

  having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha · CPC title