Nova Patents
EP0306984A1

Preservative system for ophtalmic formulations.

Abstract

Stable, clear, antimicrobially effective, ophthalmic formulations include an ophthalmologically effective amount of a drug, especially a -COOH group-containing drug or a NSAID, and a preservative system formed of a quaternary ammonium preservative and a nonionic surfactant, all in an aqueous vehicle. These formulations are useful for treating diseases that are either caused by, associated with or accompanied by inflammatory processes, including, among others, glaucoma, cystoid macular edema, uveitis, diabetic retinopathy, and conjunctivitis, or any trauma caused by eye surgery or eye injury.

Term

Term ended

Projected expiry passed 9 September 2008, 18 years ago.

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18 claims: 12 independent, 6 dependent

  1. 1
    An ophthalmic NSAID formulation comprising:a NSAID in an effective amount for ophthalmic treatment, a quaternary ammonium preservative, a stabilizing amount of a nonionic ethoxylated octylphenol surfactant, and an aqueous vehicle.
  2. 3
    The ophthalmic NSAID formulation of any one of Claims 1 and 2 wherein said nonionic ethoxylated oc­tylphenol surfactant is an octylphenoxypoly(ethyleneoxy)-­ethanol with a mole ratio of ethylene oxide to octylphe­nol of between 3:1 and 40:1.
  3. 4
    The ophthalmic NSAID formulation of any one of Claims 1 to 3 wherein said nonionic ethoxylated octyl­phenol surfactant is Octoxynol 40.
  4. 5
    The ophthalmic NSAID formulation of any one of Claims 1 to 4 including disodium edetate.
  5. 6
    The ophthalmic NSAID formulation of any one of Claims 1 to 5 wherein said NSAID is selected from the group:ketorolac, indomethacin, flurbiprofen, and diclo­fenac, or their isomers, pharmaceutically acceptable salts, or esters.
  6. 7
    The ophthalmic NSAID formulation of any one of Claims 1 to 6 wherein said NSAID is Ketorolac Trometh­amine.
  7. 8
    The ophthalmic NSAID formulation of any one of Claims 1 to 6 wherein said NSAID is the (1)-isomer of ketorolac or one of its pharmaceutically acceptable salts.
  8. 9
    The ophthalmic NSAID formulation of any one of Claims 1 to 8 comprising:NSAID      0.001% to 10.0% wt/vol.;Preservative      0.001% to 1.0% wt/vol.;Surfactant      0.001% to 1.0% wt/vol.;and Purified Water      q.s. to 100%.
  9. 13
    An antimicrobially effective preservative system for ophthalmologically acceptable, carboxyl group-containing drugs, said preservative system comprising a quaternary ammonium preservative and a stabilizing amount of anonionic ethoxylated octylphenol surfactant.
  10. 15
    The use of a formulation of any one of Claims 1 to 12 for the manufacture of a medicament for the treatment or prevention of ophthalmic diseases, particu­larly ocular inflammatory diseases.
  11. 16
    The use of a preservative system of any one of Claims 13 and 14 for manufacture of a medicament for the treatment or prevention of ophthalmic diseases, particularly ocular inflammatory diseases.
  12. 17
    A process for the preparation of an ophthalmic NSAID formulation which comprises mixing 0.001% to 10.0% wt/vol. of an NSAID, 0.001% to 1.0% wt/vol. of a preservative, 0.001% to 1.0% wt/vol. of a nonionic ethoxylated octylphenol surfactant, and Purified Water q.s. to 100%.
Independent claims12