PHARMACEUTICAL COMPOSITION FOR TREATMENT OF INCREASED INTRAOCULAR PRESSURE

• US 20130046014A1
• Filed: 03/16/2011
• Published: 02/21/2013
• Est. Priority Date: 03/17/2010
• Status: Active Grant

• Current Assignee: Novaliq GmbH
• Original Assignee: Novaliq GmbH
• Inventors: Theisinger, Bastian
• Granted Patent: US 10,045,996 B2
• Time in Patent Office: Days
• US Class Current: 514/530
• 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 poorly water-soluble prostaglandin analogue useful in the management of increased intraocular pressure or a symptom associated therewith , and

(b) a liquid vehicle comprising a semifluorinated alkane.

2. The composition of claim 1, wherein the active ingredient is a PGF2a analogue, a prostamide, or a prodrug thereof, and preferably selected from the group consisting of latanoprost, bimatoprost, tafluprost, travoprost and unoprostone.

3. The composition of claim 1, wherein the active ingredient exhibits a water solubility of less than about 1 mg per ml, as measured at room temperature and neutral pH.

4. The composition of claim 3, wherein the active ingredient is latanoprost.

5. The composition of claim 4, wherein the concentration of latanoprost is from about 0.001 wt.-% to about 0.01 wt.-%.

6. The composition of claim 1, wherein the semifluorinated alkane is a compound of formula RFRH

or of formula

RFRHRF

wherein RF is a perfluorinated hydrocarbon segment with 20 or less carbon atoms, and wherein RH is a non-fluorinated hydrocarbon segment with 3 to 20 carbon atoms.

7. The composition of claim 6, wherein the semifluorinated alkane is a compound of formula

RFRH

wherein RF is a linear perfluorinated hydrocarbon segment with 3 to 10 carbon atoms,

and

wherein RH is a linear alkyl group with 3 to 10 carbon atoms.

8. The composition of claim 7, wherein the semifluorinated alkane is selected from F4H5, F4F6, F6H6 and F6H8.

9. The composition of claim 1, being formulated as a solution, emulsion or suspension.

10. The composition of claim 1, being substantially free of water.

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

12. The composition of claim 11, comprising ethanol at a concentration of about 1.5 wt.-% or less, or of about 1.0 wt.-% or less.

13. The use of a pharmaceutical composition of claim 1 for the prevention or therapy of increased intraocular pressure, ocular hypertension, glaucoma, or a symptom associated therewith.

14. The use of claim 13, wherein the composition is adapted for topical administration to the eye of a patient.

15. 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.