Antiprostaglandins for the treatment of ocular pathologies
First Claim
1. A formulation for the treatment of ocular neovascularization comprising an antiprostaglandin in a concentration and dose suitable for treating ocular neovascularization, characterized in that said antiprostaglandin is in a pharmaceutically acceptable form suitable for delivery to the eye and optionally, said antiprostaglandin is at a substantially neutral pH, wherein optionally (a) the antiprostaglandin is selected from the group consisting of flurbiprofen, indomethacin, ketorolac, tromethamine, meclofenamate, flurbiprofen, and compounds in the pyrrolo-pyrrole group of non-steroidal anti-inflammatory drugs or (b) the antiprostaglandin is flurbiprofen or (c) the antiprostaglandin is in a concentration from about 0.001%w/v to about 0.5%w/v, characterized in that said compound is at a substantially neutral pH in a pharmaceutically acceptable form suitable for delivery to the eye to reduce ocular neovascularization or (d) the antiprostaglandin is present in a concentration range of about about 0.01%w/v to about 0.1%w/v or (e) the antiprostaglandin is present in a concentration range of about 0.01%w/v to about 0.05%w/v or (f) the formulation formulation also includes heparin in a concentration and dose sufficient to reduce ocular neovascularization, and wherein the heparin is low molecular weight heparin or is from about 0.01 pg/ml to about 30 mg/ml or the low molecular weight heparin is present in a concentration of 0.03%w/v or (g) the formulation also includes an antimicrobial in a concentration from about 20 μ
- g/ml to about 200 μ
g/ml, wherein the antimicrobial is a macrolide antibiotic or (h) the macrolide antibiotic of (g) is selected from the group consisting of tacrolimus, cyclosporine, sirolimus, everolimus, ascomycin, erythromycin, azithromycin, clarithromycin, clindamycin, lincomycin, dirithromycin, josamycin, spiramycin, diacetyl-midecamycin, tylosin, roxithromycin, ABT-773, telithromycin, leucomycins, and lincosamide or (i) the macrolide antibiotic of (g) is ascomycin.
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Accused Products
Abstract
Formulations and methods useful to treat ocular neovascularization (new blood vessel growth in the cornea, retina, conjunctiva, and/or choroid) are disclosed. According to the invention there is provided a formulation suitable for the treatment of ocular neovascularization that may comprise flurbiprofen in a concentration and dose suitable for treating ocular neovascularization, characterized in that said flurbiprofen may be at a substantially neutral pH in a pharmaceutically acceptable form suitable for delivery to the eye.
24 Citations
16 Claims
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1. A formulation for the treatment of ocular neovascularization comprising an antiprostaglandin in a concentration and dose suitable for treating ocular neovascularization, characterized in that said antiprostaglandin is in a pharmaceutically acceptable form suitable for delivery to the eye and optionally, said antiprostaglandin is at a substantially neutral pH, wherein optionally
(a) the antiprostaglandin is selected from the group consisting of flurbiprofen, indomethacin, ketorolac, tromethamine, meclofenamate, flurbiprofen, and compounds in the pyrrolo-pyrrole group of non-steroidal anti-inflammatory drugs or (b) the antiprostaglandin is flurbiprofen or (c) the antiprostaglandin is in a concentration from about 0.001%w/v to about 0.5%w/v, characterized in that said compound is at a substantially neutral pH in a pharmaceutically acceptable form suitable for delivery to the eye to reduce ocular neovascularization or (d) the antiprostaglandin is present in a concentration range of about about 0.01%w/v to about 0.1%w/v or (e) the antiprostaglandin is present in a concentration range of about 0.01%w/v to about 0.05%w/v or (f) the formulation formulation also includes heparin in a concentration and dose sufficient to reduce ocular neovascularization, and wherein the heparin is low molecular weight heparin or is from about 0.01 pg/ml to about 30 mg/ml or the low molecular weight heparin is present in a concentration of 0.03%w/v or (g) the formulation also includes an antimicrobial in a concentration from about 20 μ - g/ml to about 200 μ
g/ml, wherein the antimicrobial is a macrolide antibiotic or(h) the macrolide antibiotic of (g) is selected from the group consisting of tacrolimus, cyclosporine, sirolimus, everolimus, ascomycin, erythromycin, azithromycin, clarithromycin, clindamycin, lincomycin, dirithromycin, josamycin, spiramycin, diacetyl-midecamycin, tylosin, roxithromycin, ABT-773, telithromycin, leucomycins, and lincosamide or (i) the macrolide antibiotic of (g) is ascomycin. - View Dependent Claims (2, 3, 4, 7, 8, 9, 10, 12, 13, 14, 15)
- g/ml to about 200 μ
-
5. An ocular pharmaceutically acceptable formulation comprising:
- an antiprostaglandin in a concentration from about 0.001%w/v to about 0.5%w/v, characterized in that said antiprostaglandin is at a substantially neutral pH in a pharmaceutically acceptable form suitable for delivery to the eye to reduce ocular neovascularization and
(a) a steroid such as triamcinolone acetonide at a concentration from about 0.1 mg/ml to about 40 mg/ml and a tetracycline or a derivative thereof (including CMTs which inhibit MMP activity) such as doxycycline at a concentration from about 0.01 pg/ml to about 30 mg/ml or (b) a steroid such as triamcinolone acetonide at a concentration from about 0.1 mg/ml to about 40 mg/ml and a heparin or low molecular weight heparin in a concentration from about 0.01 pg/ml to about 100 mg/ml or (c) a heparin or low molecular weight heparin in a concentration from about 0.01 pg/ml to about 100 mg/ml and a macrolide antibiotic such as ascomycin at a concentration from about 20 μ
g/ml to about 200 μ
g/ml or(d) a heparin or low molecular weight heparin in a concentration from about 0.01 pg/ml to about 100 mg/ml and a tetracycline or a derivative thereof (including CMTs which inhibit MMP activity) such as doxycycline at a concentration from about 0.01 pg/ml to about 30 mg/ml or (e) a heparin or low molecular weight heparin in a concentration from about 0.01 pg/ml to about 100 mg/ml and an inhibitor of a metalloproteinase in a concentration and dose to reduce ocular neovascularization or (f) a steroid such as triamcinolone acetonide at a concentration from about 0.1 mg/ml to about 40 mg/ml and an inhibitor of a metalloproteinase in a concentration and dose to reduce ocular neovascularization or (g) a steroid such as triamcinolone acetonide at a concentration from about 0.1 mg/ml to about 40 mg/ml and a macrolide antibiotic such as ascomycin at a concentration from about 20 μ
g/ml to about 200 μ
g/ml or(h) a tetracycline or a derivative thereof (including CMTs which inhibit MMP activity) such as doxycycline at a concentration from about 0.01 pg/ml to about 30 mg/ml and an inhibitor of a metalloproteinase in a concentration and dose to reduce ocular neovascularization or (i) a macrolide antibiotic such as ascomycin at a concentration from about 20 μ
g/ml to about 200 μ
g/ml and an inhibitor of a metalloproteinase in a concentration and dose to reduce ocular neovascularization or(j) a tetracycline or a derivative thereof (including CMTs which inhibit MMP activity) such as doxycycline at a concentration from about 0.01 pg/ml to about 30 mg/ml, a steroid such as triamcinolone acetonide at a concentration from about 0.1 mg/ml to about 40 mg/ml and a heparin or low molecular weight heparin in a concentration from about 0.01 pg/ml to about 100 mg/ml or (k) a tetracycline or a derivative thereof (including CMTs which inhibit MMP activity) such as doxycycline at a concentration from about 0.01 pg/ml to about 30 mg/ml, a steroid such as triamcinolone acetonide at a concentration from about 0.1 mg/ml to about 40 mg/ml and a macrolide antibiotic such as ascomycin at a concentration from about 20 μ
g/ml to about 200 μ
g/ml or(l) a tetracycline or a derivative thereof (including CMTs which inhibit MMP activity) such as doxycycline at a concentration from about 0.01 pg/ml to about 30 mg/ml, a steroid such as triamcinolone acetonide at a concentration from about 0.1 mg/ml to about 40 mg/ml, a heparin or low molecular weight heparin in a concentration from about 0.01 pg/ml to about 100 mg/ml and a macrolide antibiotic such as ascomycin at a concentration from about 20 μ
g/ml to about 200 μ
g/ml. - View Dependent Claims (11, 16)
- an antiprostaglandin in a concentration from about 0.001%w/v to about 0.5%w/v, characterized in that said antiprostaglandin is at a substantially neutral pH in a pharmaceutically acceptable form suitable for delivery to the eye to reduce ocular neovascularization and
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6. A method for treating ocular neovascularization comprising the step of administering to a patient an antiprostaglandin in a concentration from about 0.001%w/v to about 0.5%w/v, characterized in that said antiprostaglandin is at a substantially neutral pH in a pharmaceutically acceptable form suitable for delivery to the eye to reduce ocular neovascularization.
Specification