Liquid pharmaceutical composition for the treatment of a posterior eye disease

Patent metadata

Field	Value
Publication number	US-2016101178-A1
Application number	US-201514973461-A
Country	US
Kind code	A1
Filing date	Dec 17, 2015
Priority date	Nov 11, 2010
Publication date	Apr 14, 2016
Grant date	—

Abstract

The invention provides pharmaceutical compositions based on liquid vehicles whose density is substantially higher than that of aqueous physiological fluids. The compositions are useful as medicines in ophthalmology, in particular for the treatment of conditions affecting the posterior segment of an eye. They may be administered topically into the eye or in a minimally invasive manner by periocular injection. Preferred liquid carriers are selected from semifluorinated alkanes.

First claim

1 . A pharmaceutical composition for the treatment of a tissue associated with the posterior segment of an eye of a patient, wherein the composition comprises a non-aqueous, physiologically tolerable, liquid vehicle having a density of at least 1.2 g/ml, and wherein the treatment comprises topical administration to the surface of the eye and/or periocular injection.

2 . The pharmaceutical composition of claim 1 , wherein the treatment further includes a time period subsequent to the administration of the composition during which period the patient is in a supine position facing upwards, said period being sufficient to allow the composition to migrate from the site of administration to a site in the posterior segment of the eye.

3 . The pharmaceutical composition of claim 1 or 2 , wherein the patient is affected by a disease or condition selected from age-related macular degeneration, diabetic retinopathy, glaucoma, retinitis pigmentosa, and cytomegalovirus retinitis.

4 . The pharmaceutical composition of any preceding claim, wherein the liquid vehicle is selected from perfluorocarbons, semifluorinated alkanes, polysiloxanes, and mixtures thereof.

5 . The composition of claim 4 , wherein liquid vehicle comprises a semifluorinated alkane according to the 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.

6 . The composition of claim 5 , 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.

7 . The composition of claim 6 , wherein the semifluorinated alkane is selected from F4H5, F6H6 and F6H8.

8 . The pharmaceutical composition of any preceding claim, wherein the liquid vehicle has a density of at least about 1.35 g/ml.

9 . The pharmaceutical composition of any preceding claim, wherein the liquid vehicle has a boiling point of at least about 120° C.

10 . The pharmaceutical composition of any preceding claim, having a dynamic viscosity of not more than about 5 mPas.

11 . The pharmaceutical composition of any preceding claim, wherein the liquid vehicle has a refractive index in the range from 1.29 to 1.35 at 20° C.

12 . The pharmaceutical composition of any preceding claim, comprising an active pharmaceutical ingredient in dissolved or dispersed form, which active ingredient is optionally selected from latanoprost, bimatoprost, tafluprost, travoprost, unoprostone, triamcinolone, dexamethasone, fluorometholone, hydrocortisone, prednisolone, rimexolone, aureomycin, azithromycin, gentamycin, ciprofloxacin, ofloxacin, fusidic acid, kanamycin, levofloxacin, lomefloxacin, oxytetracyclin, tobramycin, natamycin, gentamycin, moxifloxacin, carteolol, timolol, metipranolol, betaxolol, pindolol, levobunolol, brimonidine, clonidine, dipivefrine, apraclonidine, carbachol, pilocarpine, brinzolamide, dorzolamide, aciclovir, trifluridine, ganciclovir, diclofenac, bromfenac, ketorolac, flurbiprofen, and indometacin, including any salts and solvates thereof.

13 . The pharmaceutical composition of any preceding claim, further comprising one or more excipients selected from co-solvents, surfactants, stabilisers, antioxidants, preservatives, and colouring agents.

14 . The pharmaceutical composition of any preceding claim, being formulated so as to provide for the sustained release of the active ingredient over a period of at least about 24 hours.

15 . A method for treating a disease or condition of a tissue associated with the posterior segment of an eye of a patient, comprising (a) administering a pharmaceutical composition comprising a non-aqueous, physiologically tolerable, liquid vehicle having a density of at least 1.2 g/ml by topical administration to the surface of the eye and/or periocular injection, and subsequently (b) bringing the patient into a supine position facing upwards for a sufficiently long time period to allow the composition to migrate from the site of administration to a site in the posterior segment of the eye.

Assignees

• Wilson Clive G
• Novaliq Gmbh

Inventors

• Wilson Clive G

Classifications

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P31/12

  Antivirals · CPC title

• A61P31/04

  Antibacterial agents · CPC title