US2020237651A1PendingUtilityA1
Topical montelukast for treatment of atopic dermatitis
Est. expiryMay 4, 2036(~9.8 yrs left)· nominal 20-yr term from priority
A61K 9/0014A61K 31/495A61K 31/47A61K 31/00A61K 9/06A61K 45/06A61K 47/42A61K 47/20A61K 9/1075
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Claims
Abstract
A topical formulation comprising Montelukast or a pharmaceutically acceptable salt thereof, a gelling agent and water for the treatment of atopic dermatitis.
Claims
exact text as granted — not AI-modified1 . A topical formulation comprising Montelukast or a pharmaceutically acceptable salt thereof, a gelling agent and water for the treatment of atopic dermatitis.
2 . The topical formulation of claim 1 , wherein the concentration of Montelukast tor its pharmaceutically acceptable salt is between about 0.5% w/w to about 5% w/w or between about 5% w/w to about 10% w/w.
3 . The topical formulation of claim 1 , wherein the concentration of montelukast or a pharmaceutically acceptable salt is 5% w/w.
4 . The topical formulation of claim 1 , wherein between about 0.5% to about 1% of Montelukast is deposited within the skin following topical application.
5 . The topical formulation of claim 1 , wherein the pH of the formulation is less than 6
6 . The topical formulation of claim 1 , wherein the pH is in the range 5 to 6.
7 . The topical formulation of claim 1 , wherein the formulation further comprises a water miscible organic solvent.
8 . The topical formulation of claim 1 , wherein the formulation further comprises a penetration enhancer.
9 . The topical formulation of claim 1 , wherein the formulation further comprises an antioxidant.
10 . The topical formulation of claim 1 , wherein the formulation further comprises a preservative.
11 . The topical formulation of claim 1 comprising:
a)
Category
Ingredient
Active
Montelukast sodium
Water miscible
Alcohol 96%
organic solvent
Penetration
DMSO
enhancer
Antioxidant
BHT
Chelating Agent
EDTA
Water
Purified water
Preservative
Methyl paraben
Preservative
Propyl paraben
Gelling agent
Hydroxyethylcellulose
(M w 90,000 to 1,300,000)
pH adjusting
HCl (10% solution)
agent
b)
Category of ingredient
Example of Ingredient
Occlusive ingredient
Dimethicone
Occlusive ingredient
Cyclomethicone
Active
Montelukast sodium
Emulsifier
Silicone Glycerol emulsifier
Occlusive ingredient
Cetearyl Ethylhexanoate
Water miscible
Glycerin
organic solvent
Solvent
Water
Gelling agent
Sodium Carbomer
Lubricant
Sodium Hyaluronate
c)
Category of ingredient
Example of Ingredient
Active
Montelukast sodium
Water miscible
Alcohol
organic solvent
Antioxidant
BHT
Water
Purified water
Penetration
DMSO
enhancer
Preservative
Methyl paraben
Preservative
Propyl paraben
Gelling agent
Carbopol 947P(polymers of acrylic acid)
Chelating agent
EDTA
Emulsifier/
Sepineo 600(Acrylamide/Sodium
Thickener/Stabilizer
Acryloyldimethyl Taurate copolymer/
isohexadecane and Polysorbate 80)
d)
Category of ingredient
Example of Ingredient
Active
Montelukast sodium
Water miscible
Alcohol
organic solvent
Antioxidant
BHT
Water
Purified water
Penetration
DMSO
enhancer
Preservative
Methyl paraben
Preservative
Propyl paraben
Gelling agent
Carbopol 947P(polymers of acrylic acid)
Chelating agent
EDTA
Emulsifier/
Sepineo 600(Acrylamide/Sodium
Thickener/Stabilizer
Acryloyldimethyl Taurate copolymer/
isohexadecane and Polysorbate 80)
pH adjusting
Phosphate or citric acid Buffer
agent
12 . A topical formulation as in claim 11 selected from any one of the following
a)
Category
Ingredient
% W/W
Active
Montelukast sodium
5.00
Water miscible
Alcohol 96%
25.00
organic solvent
Penetration
DMSO
10.00
enhancer
Antioxidant
BHT
0.10
Chelating Agent
EDTA
0.10
Water
Purified water
57.90
Preservative
Methyl paraben
0.30
Preservative
Propyl paraben
0.10
Gelling agent
Hydroxyethylcellulose
1.50
(M w 90,000 to 1,300,000)
pH adjusting
HCl (10% solution)
q.s.
agent
b)
Category of ingredient
Ingredient
% W/W
Occlusive ingredient
Dimethicone
1
Occlusive ingredient
Cyclomethicone
4
Active
Montelukast sodium
3
Emulsifier
Silicone Glycerol emulsifier
1.5
Occlusive ingredient
Cetearyl Ethylhexanoate
2.5
Water miscible
Glycerin
3.0
organic solvent
Solvent
Water
Up to 100
Gelling agent
Sodium Carbomer
2.5
Lubricant
Sodium Hyaluronate
1.0
c)
Category of ingredient
Ingredient
% W/W
Active
Montelukast sodium
1%
Water miscible
Alcohol
25%
organic solvent
Antioxidant
BHT
0.10%
Water
Purified water
60.00
Penetration
DMSO
10.00%
enhancer
Preservative
Methyl paraben
0.30%
Preservative
Propyl paraben
0.10%
Gelling agent
Carbopol 947P (polymers of acrylic
0.40%
acid)
Chelating agent
EDTA
0.10%
Emulsifier/
Sepineo 600(Acrylamide/Sodium
3%
Thickener/Stabilizer
Acryloyldimethyl Taurate copolymer/
isohexadecane and Polysorbate 80
d)
Category of ingredient
Ingredient
% W/W
Active
Montelukast sodium
1%
Water miscible organic solvent
Alcohol
25%
Antioxidant
BHT
0.10%
Water
Purified water
60.00
Penetration enhancer
DMSO
10.00%
Preservative
Methyl paraben
0.30%
Preservative
Propyl paraben
0.10%
Gelling agent
Carbopol 947P
0.40%
(polymers of acrylic
acid)
Chelating agent
EDTA
0.10%
Emulsifier/Thickener/Stabilizer
Sepineo 600
3%
(Acrylamide/Sodium
Acryloyldimethyl
Taurate copolymer/
isohexadecane and
Polysorbate 80
pH adjusting agent
Phosphate Buffer
pH 5.6
13 . The topical formulation of claim 1 , wherein the montelukast is homogeneously suspended in the formulation or wherein montelukast crystals are present in the formulation.
14 . A topical formulation comprising Montelukast or a pharmaceutically acceptable salt thereof and at least one oil for the treatment of atopic dermatitis wherein the formulation is waterless.
15 . A topical formulation as in claim 14 wherein the formulation further comprises a topically acceptable solvent, and an amphiphilic compound and further an occlusive ingredient
16 . A topical formulation as in claim 15 selected from any of the following:
a solution comprising
Category of ingredient
Example
Topically acceptable solvent
Alcohol (Dehydrated)
Amphiphilic compound
Poloxylhydrogenated Castor oil
Active
Montelukast sodium
Oil
Fractionated Coconut oil
or a gel formulation comprising
Category of ingredient
Example of ingredient
Topically acceptable solvent
Alcohol (Dehydrated)
Amphiphilic compound
Poloxylhydrogenated Castor oil
Active
Montelukast sodium
Oil
Fractionated Coconut oil
Gelling agent
Hydroxypropylcellulose
or an ointment comprising
Category of ingredient
Example of Ingredient
Active
Montelukast sodium
Occlusive ingredient
Petroleum jelly/white petrolatum
Oil
Trihydroxystearin
Oil
Olive oil
or an ointment comprising
Category of ingredient
Example of Ingredient
Active
Montelukast sodium
Water miscible organic solvent
Glycerine
Oil
Medium chain triglycerides
Antioxidant
Antioxidant
or an ointment comprising
Category of ingredient
Example of Ingredient
Active
Montelukast Sodium
Antioxidant
BHT
Occlusive ingredient
Cyclomethicone 5, NF
Occlusive ingredient
Cyclomethicone and Dimethicone 5225C
or an ointment comprising
Category of ingredient
Example of Ingredient
Active
Montelukast Sodium
Antioxidant
BHT
Occlusive ingredient
Petrolatum White USP
Amphiphilic compound
Propylene Glycol-15 Stearyl Ether
Oil
Medium Chain Triglycerides
Amphiphilic compound
Monosteol(propylene glycol
monostearate)
or an ointment comprising
Category of ingredient
Example of Ingredient
Active
Montelukast Sodium
Antioxidant
BHT
Occlusive ingredient/
Petrolatum White USP
Oil
Mineral Oil
17 . A topical formulation as in claim 16 selected from any one of the following:
a solution comprising
Category of Ingredient
Ingredient
% W/W
Topically acceptable
Alcohol (Dehydrated)
34.5
Amphiphilic compound
Poloxylhydrogenated Castor
2.5
Active
Montelukast sodium
3
oil
Fractionated Coconut oil
60
or a gel formulation comprising
Category of ingredient
Ingredient
% W/W
Topically acceptable solvent
Alcohol (Dehydrated)
31
Amphiphilic compound
Poloxylhydrogenated Castor
2.5
Active
Montelukast sodium
3
oil
Fractionated Coconut oil
60
Gelling agent
Hydroxy propyl cellulose
3.5
or an ointment comprising
Category of
ingredient
Ingredient
% W/W
Active
Montelukast sodium
0.5-5
Occlusive
Petroleum jelly/white
80
ingredient
petrolatum
Oil
Trihydroxystcarin
1-3
oil
Olive oil
12-18.5
or an ointment comprising
Category of
ingredient
Ingredient
% W/W{grave over ( )}
Active
Montelukast sodium
0.5-5
Water miscible
Glycerine
65-75
organic solvent
Oil
Medium chain
20
triglycerides
Antioxidant
Antioxidant
0-0.5
or an ointment comprising
Category of
ingredient
Ingredient
% W/W{grave over ( )}
Active
Montelukast Sodium
5
Antioxidant
BHT
0.08
Occlusive
Cyclomethicone
94.52
ingredient
Amphiphilic
Cyclomethicone and
0.40
compound
Dimethicone
or an ointment comprising
Category of
ingredient
Ingredient
% W/W{grave over ( )}
Active
Montelukast Sodium
5
Antioxidant
BHT
0.08
Occlusive
Petrolatum White
55.92
ingredient
Amphiphilic
PPG-15 Stearyl Ether
16
compound
Oil
Medium Chain Triglycerides
20
Amphiphilic
Monosteol
3
compound
or an ointment comprising
Category of
ingredient
Ingredient
% W/W{grave over ( )}
Active
Montelukast Sodium
5
Antioxidant
BHT
0.08
Occlusive
Petrolatum White
49.92
ingredient/
Oil
Mineral Oil
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