Topical treatment or prevention of ocular infections

Abstract

The topical application of an azalide antibiotic such as azithromycin to the eye is useful in treating or preventing ocular infections. In one embodiment, the azalide antibiotic is supplied to the eye in a depot for sustained release. A more convenient dosing regimen can also be provided by the use of an appropriate depot. Furthermore, a composition containing a combination of medicaments is also provided.

1 . A process for treating an eye, which comprises:
 topically applying an aqueous polymeric suspension of an azalide antibiotic, wherein said suspension comprises water, 0.01% to 1.0% of an azalide antibiotic, and 0.1 to 10% of a polymeric suspending agent.   
     
     
         2 . The process according to  claim 1 , wherein said polymeric suspending agent is a water-swellable water-insoluble crosslinked carboxy-vinyl polymer. 
     
     
         3 . The process according to  claim 2 , wherein the polymer comprises at least 90% acrylic acid monomers and 0.1% to 5% crosslinking agent. 
     
     
         4 . The process according to  claim 3 , wherein the crosslinking agent comprises a difunctional crosslinking agent. 
     
     
         5 . The process according to  claim 4 , wherein said crosslinking agent is selected from the group consisting of divinyl glycol, 2,3-dihydroxyhexa-1,5-diene, 2,5-dimethyl-1,5-hexadiene, divinylbenzene, N,N-diallylacrylamide, N,N-diallymethacrylamide, and mixtures thereof. 
     
     
         6 . The process according to  claim 3 , wherein said polymer comprises a polycarbophil. 
     
     
         7 . The process according to  claim 3 , wherein said polymeric suspending agent is contained in an amount of from about 0.5 to 1.2%. 
     
     
         8 . The process according to  claim 7 , wherein said polymer has a monodisperse particle size distribution. 
     
     
         9 . The process according to  claim 8 , wherein said azalide antibiotic comprises azithromycin. 
     
     
         10 . The process according to  claim 9 , wherein said azalide antibiotic comprises azithromycin dihydrate. 
     
     
         11 . A process for treating an eye, comprising: topically applying an azalide antibiotic to an eye in an amount effective to treat infection in a tissue of the eye, wherein said topically applying comprises supplying a depot of a composition containing said azalide antibiotic on the eye. 
     
     
         12 . The process according to  claim 11 , wherein said eye is suffering from at least one condition selected from the group consisting of conjunctivitis, ophthalmia neonatorum, trachoma, corneal ulcers, keratitis, keratoconjunctivitis, endophthalmitis, infectious uveitis and combinations thereof, and said amount of said azalide antibiotic is therapeutically effective to treat said condition. 
     
     
         13 . The process according to  claim 11 , wherein said azalide antibiotic is a compound of formula (I): 
       
         
           
           
               
               
           
         
       
       wherein R 1  and R 2  each independently represent a hydrogen atom or methyl group. 
     
     
         14 . The process according to  claim 13 , wherein said azalide antibiotic is azithromycin. 
     
     
         15 . The process according to  claim 13 , wherein said applying provides a therapeutically effective concentration of azalide antibiotic within a tissue of the eye for at least 8 hours. 
     
     
         16 . The process according to  claim 15 , wherein said applying provides a therapeutically effective concentration of azalide antibiotic within a tissue of the eye for at least 12 hours. 
     
     
         17 . The process according to  claim 16 , wherein said applying provides a therapeutically effective concentration of azalide antibiotic within a tissue of the eye for at least 18 hours. 
     
     
         18 . The process according to  claim 11 , wherein said depot is an aqueous polymeric suspension of said azalide antibiotic. 
     
     
         19 . The process according to  claim 18 , wherein said aqueous polymeric suspension further comprises an additional medicament. 
     
     
         20 . The process according to  claim 19 , wherein said additional medicament is selected from the group consisting of amikacin, gentamycin, tobramycin, streptomycin, netilmycin, kanamycin ciprofloxacin, norfloxacin, ofloxacin, trovafloxacin, lomefloxacin, levofloxacin, enoxacin, sulfonamides, polymyxin, chloramphenicol, neomycin, paramomomycin, colistimethate, bacitracin, vancomycin, tetracyclines, rifampins, cycloserine, beta-lactams, cephalosporins, amphotericins, fluconazole, flucytosine, natamycin, miconazole, ketoconazole, corticosteroids, diclofenac, flurbiprofen, ketorolac, suprofen, comolyn, lodoxamide, levocabastin, naphazoling, antazoline, and. pheniramimane.