US2021252020A1PendingUtilityA1
Methods and compositions for the treatment of ophthalmic conditions
Est. expirySep 1, 2037(~11.1 yrs left)· nominal 20-yr term from priority
Inventors:Yosuf El-Shabrawi
A61K 47/40A61P 27/02A61K 31/5383A61K 31/196A61K 31/58A61K 31/573A61K 47/32A61K 45/06A61K 9/06A61K 9/0048
61
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Claims
Abstract
Compositions comprising at least two of a corticosteroid, a non-steroidal anti-inflammatory drug (NSAID), and an antibiotic find use in treating or preventing eye conditions in subjects in need thereof. Methods of treatment or prevention of eye conditions comprise administering an effective amount of the disclosed compositions to the affected eye(s). Methods of preparing a composition comprising an NSAID and antibiotic comprise separately complexing the NSAID and antibiotic with cyclodextrin.
Claims
exact text as granted — not AI-modifiedThat which is claimed:
1 . A composition comprising a non-steroidal anti-inflammatory drug (NSAID) and a corticosteroid.
2 . The composition of claim 1 , wherein the concentration of the NSAID is between 0.05% and 0.5% (weight/volume) of the total volume of the composition.
3 . The composition of claim 1 or 2 , wherein the NSAID is one or more of diclofenac, ketorolac tromethamine, bromfenac, nepafenac, derivatives thereof, and salts thereof.
4 . The composition of claim 1 , wherein the NSAID is diclofenac, a salt thereof, and/or a combination thereof.
5 . The composition of claim 4 , wherein the concentration of diclofenac is between 0.05% and 0.2% (weight/volume) of the total volume of the composition.
6 . The composition of claim 4 , wherein the concentration of diclofenac is about 0.1% (weight/volume) of the total volume of the composition.
7 . The composition of claim 1 , wherein the NSAID is bromfenac, a salt thereof, and/or a combination thereof.
8 . The composition of claim 7 , wherein the concentration of bromfenac is between 0.05% and 0.2% (weight/volume) of the total volume of the composition.
9 . The composition of claim 7 , wherein the concentration of bromfenac is about 0.09% (weight/volume) of the total volume of the composition.
10 . The composition of claim 1 , wherein the concentration of the corticosteroid is between 0.05% and 2% (weight/volume) of the total amount of the composition.
11 . The composition of claim 1 , wherein the corticosteroid is one or more of prednisolone, dexamethasone, difluprednate, loteprednol etabonate, fluorometholone, derivatives thereof, and salts thereof.
12 . The composition of claim 1 , wherein the corticosteroid is prednisolone or a salt or derivative thereof.
13 . The composition of claim 12 , wherein the prednisolone salt is prednisolone acetate.
14 . The composition of claim 12 or 13 , wherein the concentration of prednisolone or prednisolone acetate is between 0.25% and 1% (weight/volume) of the total amount of the composition.
15 . The composition of claim 12 or 13 , wherein the concentration of prednisolone or prednisolone acetate is about 0.5% (weight/volume) of the total amount of the composition.
16 . The composition of claim 1 , wherein the corticosteroid is dexamethasone or a salt or derivative thereof.
17 . The composition of claim 16 , wherein the concentration of dexamethasone or a salt or derivative thereof is between 0.05% and 0.5% (weight/volume) of the total amount of the composition.
18 . The composition of claim 16 or 17 , wherein the concentration of dexamethasone or a salt or derivative thereof is about 0.1% (weight/volume) of the total amount of the composition.
19 . The composition of any one of claims 1 - 18 , wherein the composition further comprises an antibiotic.
20 . The composition of claim 19 , wherein the concentration of the antibiotic is between 0.1% and 1% (weight/volume) of the total volume of the composition.
21 . The composition of claim 19 or 20 , wherein the antibiotic is a broad spectrum antibiotic.
22 . The composition of claim 19 or 20 , wherein the antibiotic is a fluoroquinolone.
23 . The composition of claim 19 or 20 , wherein the antibiotic is one or more of ofloxacin, moxifloxacin, ciprofloxacin, levofloxacin, besifloxacin, fluoroquinolone, derivatives thereof, and salts thereof
24 . The composition of claim 19 , wherein the antibiotic is ofloxacin.
25 . The composition of claim 24 , wherein the concentration of ofloxacin is between 0.2% and 0.5% (weight/volume) of the total volume of the composition.
26 . The composition of claim 24 , wherein the concentration of ofloxacin is about 0.3% (weight/volume) of the total volume of the composition.
27 . The composition of any one of claims 1 - 26 , wherein the composition further comprises a complexing agent.
28 . The composition of claim 27 , wherein the complexing agent is cyclodextrin or a derivative thereof.
29 . The composition of claim 27 , wherein the complexing agent is 2-Hydroxypropyl-gamma-cyclodextrin.
30 . The composition of any one of claims 1 - 29 , wherein the composition further comprises a viscosifying agent.
31 . The composition of claim 1 , wherein the composition is formulated as viscous eye drops, an eye gel, eye cream, or eye ointment.
32 . The composition of claim 1 , wherein the composition is formulated as an eye gel.
33 . The composition of claim 30 , wherein the viscosifying agent is a viscoelastic polymer.
34 . The composition of claim 33 , wherein the viscoelastic polymer is one or more of polymeric cellulose, polysaccharides, polyacrylic acid, polymeric alcohol, hyaluronic acid, derivatives thereof, and salts thereof.
35 . The composition of claim 34 , wherein the polymeric alcohol is polyvinylalcohol.
36 . The composition of claim 30 , wherein the viscosifying agent is methylcellulose.
37 . The composition of claim 36 , wherein the concentration of methylcellulose is between 1% and 5% (weight/volume) of the total volume of the composition.
38 . The composition of claim 36 , wherein the concentration of methylcellulose is between 2% and 4% (weight/volume) of the total volume of the composition.
39 . A composition comprising a corticosteroid, a non-steroidal anti-inflammatory drug (NSAID), an antibiotic, and optionally a viscosifying agent, wherein the composition is formulated as an eye gel.
40 . The composition of claim 39 , wherein the concentration of the corticosteroid is between 0.05% and 2% (weight/volume) of the total amount of the composition.
41 . The composition of claim 39 or 40 , wherein the corticosteroid is one or more of prednisolone, dexamethasone, difluprednate, loteprednol etabonate, fluorometholone, derivatives thereof, and salts thereof.
42 . The composition of claim 41 , wherein the corticosteroid is prednisolone, a derivative thereof, and/or a salt thereof.
43 . The composition of claim 42 , wherein the prednisolone salt is prednisolone acetate.
44 . The composition of claim 42 or 43 , wherein the concentration of the prednisolone, derivative thereof, and salt thereof is between 0.25% and 1% (weight/volume) of the total volume of the composition.
45 . The composition of claim 42 , wherein the concentration of the prednisolone, derivative thereof, and salt thereof, is about 0.5% (weight/volume) of the total volume of the composition.
46 . The composition of any one of claims 39 - 45 , wherein the concentration of the NSAID is between 0.05% and 0.5% (weight/volume) of the total volume of the composition.
47 . The composition of any one of claims 39 - 46 , wherein the NSAID is one or more of diclofenac, ketorolac tromethamine, bromfenac, nepafenac, derivatives thereof, and salts thereof.
48 . The composition of claim 47 , wherein the NSAID is diclofenac, a derivative thereof, or a salt thereof.
49 . The composition of claim 48 , wherein the concentration of the diclofenac, derivative thereof, and salt thereof, is between 0.05% and 0.2% (weight/volume) of the total volume of the composition.
50 . The composition of claim 48 , wherein the concentration of the diclofenac, derivative thereof, and salt thereof, is about 0.1% (weight/volume) of the total volume of the composition.
51 . The composition of any one of claims 39 - 50 , wherein the concentration of the antibiotic is between 0.1% and 1% (weight/volume) of the total volume of the composition.
52 . The composition of any one of claims 39 - 51 , wherein the antibiotic is a broad spectrum antibiotic.
53 . The composition of any one of claims 39 - 51 , wherein the antibiotic is a fluoroquinolone.
54 . The composition of any one of claims 39 - 51 , wherein the antibiotic is one or more of ofloxacin, moxifloxacin, ciprofloxacin, levofloxacin, besifloxacin, derivatives thereof, and salts thereof.
55 . The composition of claim 54 , wherein the antibiotic is ofloxacin, a derivate thereof, and/or a salt thereof.
56 . The composition of claim 55 , wherein the concentration of the ofloxacin, a derivate thereof, and a salt thereof, is between 0.2% and 0.5% (weight/volume) of the total volume of the composition.
57 . The composition of claim 55 , wherein the concentration of the ofloxacin, a derivate thereof, and a salt thereof, is about 0.3% (weight/volume) of the total volume of the composition.
58 . The composition of any one of claims 39 - 57 , wherein the viscosifying agent is a viscoelastic polymer.
59 . The composition of claim 58 , wherein the viscoelastic polymer is one or more of polymeric cellulose, polysaccharides, polyacrylic acid, polymeric alcohol, hyaluronic acid, derivatives thereof, and salts thereof.
60 . The composition of claim 59 , wherein the polymeric alcohol is polyvinylalcohol.
61 . The composition of any one of claims 39 - 59 , wherein the viscosifying agent is methylcellulose.
62 . The composition of claim 61 , wherein the concentration of methylcellulose is between 1% and 5% (weight/volume) of the total volume of the composition.
63 . The composition of claim 62 , wherein the concentration of methylcellulose is between 2% and 4% (weight/volume) of the total volume of the composition.
64 . The composition of any one of claims 1 - 63 , wherein the composition further comprises a pharmaceutically acceptable carrier.
65 . The composition of any one of claims 1 - 64 , wherein the composition is substantially preservative-free.
66 . The composition of any one of claims 1 - 65 , wherein the composition is provided as a single dose unit.
67 . The composition of any one of claims 1 - 65 , wherein the composition is provided in a multi-dose container.
68 . A method of treating and/or preventing an ophthalmic condition in a subject, the method comprising topically administering an effective amount of the composition of any one of claims 1 - 67 to an eye of a subject in need thereof.
69 . The method of claim 68 , wherein the ophthalmic condition is at least one of ocular inflammation and ocular infection.
70 . The method of claim 68 or 69 , wherein the composition is administered at least one of peri- and post-operative to ocular surgery.
71 . The method of claim 70 , wherein the ocular surgery is cataract surgery.
72 . The method of any one of claims 69 - 71 , wherein the ophthalmic condition comprises one or more of cystoid macula edema (CME), ocular pain after surgery, ocular discomfort after surgery, and both ocular pain and ocular discomfort after surgery.
73 . The method of claim 68 , wherein the subject is at risk of at least one of CME and ocular inflammation.
74 . The method of claim 73 , wherein the subject:
a) has had a prolonged surgery; b) has had a previous surgery; c) is younger than 50 years; d) was previously diagnosed with, or had symptoms of, CME; e) was previously diagnosed with, or had symptoms of, diabetes mellitus; f) was previously diagnosed with, or had symptoms of, uveitis; g) was previously diagnosed with, or had symptoms of, intraocular inflammation; h) was previously diagnosed with, or had symptoms of, additional ocular diseases; i) was previously diagnosed with, or had symptoms of, diabetic retinopathy; and/or j) was previously diagnosed with, or had symptoms of, retinal venocclusion.
75 . The method of any one of claims 69 - 74 , wherein the composition is administered at a dose of one drop 1 to 6 times per day.
76 . The method of claim 75 , wherein the dose is one drop 1 to 3 times pre-operatively.
77 . The method of claim 75 , wherein the dose is one drop 1 to 6 times per day post-operatively.
78 . The method of claim 75 , wherein the dose is one drop 1 to 3 times per day post-operatively.
79 . The method of any one of claims 69 to 78 , wherein the composition is administered concurrently with at least one other medication.
80 . The method of any one of claims 69 to 78 , wherein the composition is administered concurrently with a subconjunctival injection of triamcinolone acetonide.
81 . The method of claim 80 , wherein the triamcinolone acetonide is administered at a dose of 40 mg.
82 . The method of claim 79 , wherein the composition is administered concurrently with an intravitreal injection of bevacizumab.
83 . The method of claim 82 , wherein the bevacizumab is administered at a dose of 1.25 mg.
84 . The method of claim 79 , wherein the composition is administered concurrently with a subconjunctival injection of triamcinolone acetonide and an intravitreal injection of bevacizumab.
85 . The method of claim 84 , wherein the triamcinolone acetonide is administered at a dose of 40 mg and the bevacizumab is administered at a dose of 1.25 mg.
86 . A method for preparing a composition comprising prednisolone, diclofenac, and ofloxacin in a gel formulation, the method comprising:
producing a methylcellulose gel to form Solution 1; complexing ofloxacin with gamma-cyclodextrin to form Solution 2; complexing diclofenac with gamma-cyclodextrin to form Solution 3; combining Solutions 2 and 3 to form Solution 4; adding mannitol to Solution 4 to form Solution 5; Solutions 1 and 5 to form Solution 6; and adding prednisolone acetate to Solution 6, thereby forming the composition, wherein steps a)-c) can be performed in any order, and wherein step a) can be performed before, simultaneously, or after any one of steps b)-f).
87 . The method of claim 86 , wherein the method further comprises distributing the composition into container and overlaying the composition with an inert gas to exclude oxygen.Join the waitlist — get patent alerts
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