Pharmaceutical composition for treatment of increased intraocular pressure

Patent metadata

Field	Value
Publication number	US-10525062-B2
Application number	US-201816017805-A
Country	US
Kind code	B2
Filing date	Jun 25, 2018
Priority date	Mar 17, 2010
Publication date	Jan 7, 2020
Grant date	Jan 7, 2020

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 method for the treatment or prophylaxis of a disease or disorder selected from increased intraocular pressure, ocular hypertension, glaucoma, or a symptom associated therewith, comprising the step of administering to a patient in need thereof, 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 method of claim 1 , wherein the active ingredient is latanoprost.

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

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

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

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

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

8. The method of claim 7 , further comprising an organic co-solvent.

9. The method of claim 8 , wherein the organic co-solvent is ethanol at a concentration of about 1.5 wt.-% or less.

10. The method of claim 9 , 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

• A61K47/06

  Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite · CPC title

• A61K31/5575 Primary

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

• A61K9/00

  Medicinal preparations characterised by special physical form {(nuclear magnetic resonance contrast preparations or magnetic resonance imaging contrast preparations A61K49/18; preparations containing radioactive substances A61K51/12)} · CPC title