Ophthalmic treatments

Abstract

Aqueous compositions suitable for topical administration to the human or animal eye contain at least one water-soluble polymeric ophthalmic lubricant, such as hyaluronate, carbomer gel or hypromellose, together with a water-soluble analgesic. The analgesic may be an opiod, particularly an opioid having an affinity for 5-HT receptors, such as tramadol. Typical tramadol levels would be in the range of 0.5% to 1.0% w/v. The aqueous compositions may for example be used as artificial tears, and as general ophthalmic lubricants for treating conditions such as dry eye or blepharitis. Further compositions combine ophthalmologically-active agents, such as pharmaceuticals, with opioids, such as tramadol in particular. These compositions may be used to treat the eye while reducing pain or discomfort that would normally be produced by administering these particular pharmaceuticals to the eye, and increasing the efficacy of the pharmaceuticals. Compositions are also disclosed, containing opioids with 5-HT receptor activity, which are of general use in alleviating pain in and around the eye.

1 . An aqueous composition topically administrable to a human or animal eye, comprising an aqueous solution of at least one water-soluble polymeric ophthalmic lubricating medium and an effective amount of tramadol or a derivative thereof. 
     
     
         2 . An aqueous composition as claimed in  claim 1 , comprising an artificial tears or ophthalmic lubricant composition, applicable to an eye in the form of drops. 
     
     
         3 - 5 . (canceled) 
     
     
         6 . An aqueous composition as claimed in  claim 1 , comprising between 0.01% and 2% w/v tramadol. 
     
     
         7 . (canceled) 
     
     
         8 . An aqueous composition as claimed in  claim 1 , wherein said water-soluble polymeric ophthalmic lubricating medium comprises a water-soluble polymer bearing a plurality of ionic or non-ionic polar groups. 
     
     
         9 . An aqueous composition as claimed in  claim 1 , wherein the water-soluble polymeric ophthalmic lubricating medium comprises at least one of sodium hyaluronate, carbomer gel (polyacrylate) and hypromellose (hydroxypropyl methyl cellulose, HPMC). 
     
     
         10 . An aqueous composition as claimed in  claim 1 , comprising at least one surfactant species adapted to reduce surface tension of the aqueous composition. 
     
     
         11 . An aqueous composition as claimed in  claim 1 , wherein the aqueous composition has a viscosity of between 1 and 20 centipoise, a pH in the range of about pH 6.5 to about pH 8.0, an osmolality in the range of about 200 to about 400 milliosmoles per kilogram of water, or any combinations thereof. 
     
     
         12 - 13 . (canceled) 
     
     
         14 . A method for treating a condition involving deficiencies in natural tears in a human or animal eye, comprising substantially simultaneously administering to a human or animal eye an aqueous solution of at least one water-soluble polymeric ophthalmic lubricating medium and an aqueous solution of tramadol or a derivative thereof. 
     
     
         15 - 16 . (canceled) 
     
     
         17 . A composition for topical application in the treatment of an eye disorder or condition of a human or animal eye, comprising an ophthalmologically-active agent adapted for the treatment of said disorder or condition or a symptom thereof, wherein the composition further comprises tramadol or a derivative of tramadol. 
     
     
         18 - 19 . (canceled) 
     
     
         20 . A composition as claimed in  claim 17 , wherein said ophthalmologically-active agent comprises a pharmaceutically-active agent that administered alone tends to cause pain, discomfort, inflammation, irritation or other undesirable sensations or reactions in or around an eye. 
     
     
         21 . A composition as claimed in  claim 17 , wherein the ophthamologically-active agent is selected from the group consisting of: aceclidine, acetazolamide, aciclovir, anecortave, apraclonidine, atropine, azapentacene, azelastine, bacitracin, befunolol, betamethasone, betaxolol, bimatoprost, brimonidine, brinzolamide, carbachol, carteolol, celecoxib, chloramphenicol, chlortetracycline, ciprofloxacin, cromoglycate, cromolyn, cyclopentolate, cyclosporin, dapiprazole, demecarium, dexamethasone, diclofenac, dichlorphenamide, dipivefrin, dorzolamide, echothiophale, emedastine, epinastine, epinephrine, erythromycin, ethoxzolamide, eucatropine, fludrocortisone, fluorometholone, flurbiprofen, fomivirsen, framycetin, ganciclovir, gatifloxacin, gentamycin, homatropine, hydrocortisone, idoxuridine, indomethacin, isoflurophate, ketorolac, ketotifen, latanoprost, levobetaxolol, levobunolol, levocabastine, levofloxacin, lodoxamide, loteprednol, medrysone, methazolamide, metipranolol, moxifloxacin, naphazoline, natamycin, nedocromil, neomycin, norfloxacin, ofloxacin, olopatadine, oxymetazoline, pemirolast, pegaptanib, phenylephrine, physostigmine, pilocarpine, pindolol, pirenoxine, polymyxin B, prednisolone, proparacaine, ranibizumab, rimexolone, scopolamine, sezolamide, squalamine, sulfacetamide, suprofen, tetracaine, tetracyclin, tetrahydrozoline, tetryzoline, timolol, tobramycin, travoprost, triamcinulone, trifluoromethazolamide, trifluridine, trimethoprim, tropicamide, unoprostone, vidarbine, xylometazoline, pharmaceutically acceptable salts thereof, and combinations thereof. 
     
     
         22 . A method for treating an eye disorder or condition of a human or animal eye, comprising the steps of (a) providing a composition comprising an ophthalmologically-active agent adapted for treatment of said disorder or condition or a symptom thereof, together with tramadol or a derivative of tramadol, and (b) administering said composition topically to a human or animal eye requiring treatment. 
     
     
         23 . (canceled) 
     
     
         24 . A topically administrable composition for use in treatment of pain associated with medical conditions of a human or animal eye, comprising tramadol or a derivative thereof, wherein the composition is formulated for topical administration. 
     
     
         25 - 27 . (canceled) 
     
     
         28 . A method of alleviating pain associated with medical conditions of a human or animal eye, comprising topically administering to or adjacent a site of said pain a composition comprising tramadol or a derivative thereof. 
     
     
         29 - 30 . (canceled)