TOPICAL PHARMACEUTICAL COMPOSITIONS FOR TREATING SKIN CONDITIONS
Topical pharmaceutical compositions for treating a skin condition or disorder are provided. The topical pharmaceutical compositions can be formulated as lotions containing a therapeutically effective amount of an active agent, such as tretinoin, a viscosity increasing agent, and advantageously small amounts of both a polymeric emulsifier and an oil component. The topical compositions of the present invention are tolerated exceptionally well by subjects to whom the compositions are administered.
1 . A topical pharmaceutical composition for treating a skin condition or disorder, comprising:
a therapeutically effective amount of an active agent that is useful for treating the skin condition or disorder;
a viscosity increasing agent;
a polymeric emulsifier, wherein the polymeric emulsifier is present in an amount ranging from about 0.01% to about 0.095% by weight of the composition; and
an oil component, wherein the oil component is present in an amount ranging from about 0.1% to about 5% by weight of the composition.
2 . The topical pharmaceutical composition of claim 1 , wherein the active agent is a retinoid, a corticosteroid, an antibiotic, or an anti-inflammatory agent.
3 . The topical pharmaceutical composition of claim 2 , wherein the active agent is a retinoid.
4 . The topical pharmaceutical composition of claim 3 , wherein the retinoid is tretinoin.
5 . The topical pharmaceutical composition of any one of claims 1 to 4 , wherein the active agent is present in an amount ranging from about 0.001% to about 1% by weight of the composition.
6 . The topical pharmaceutical composition of claim 1 , comprising tretinoin in an amount of about 0.05% by weight of the composition.
7 . The topical pharmaceutical composition of any one of claims 1 to 6 , wherein the polymeric emulsifier comprises a cross-linked copolymer of acrylic acid and C10-C30 alkyl acrylate.
8 . The topical pharmaceutical composition of any one of claims 1 to 7 , wherein the polymeric emulsifier is present in an amount ranging from about 0.04% to about 0.06% by weight of the composition.
9 . The topical pharmaceutical composition of any one of claims 1 to 8 , wherein the oil component comprises mineral oil.
10 . The topical pharmaceutical composition of any one of claims 1 to 9 , wherein the oil component is present in an amount ranging from about 1% to about 3% by weight of the composition.
11 . The topical pharmaceutical composition of any one of claims 1 to 10 , wherein the viscosity increasing agent comprises a cross-linked homopolymer of an acrylic acid.
12 . The topical pharmaceutical composition of any one of claims 1 to 11 , wherein the viscosity increasing agent is present in an amount ranging from about 0.1% to about 2% by weight of the composition.
13 . The topical pharmaceutical composition of claim 12 , wherein the viscosity increasing agent is present in an amount ranging from about 0.6% to about 1% by weight of the corn position.
14 . The topical pharmaceutical composition of any one of claims 1 to 13 , further comprising one or more preservatives.
15 . The topical pharmaceutical composition of any one of claims 1 to 14 , further comprising one or more moisturizing agents.
16 . The topical pharmaceutical composition of any one of claims 1 to 15 , further comprising one or more antioxidants.
17 . The topical pharmaceutical composition of any one of claims 1 to 16 , further comprising one or more humectants.
18 . The topical pharmaceutical composition of any one of claims 1 to 17 , further comprising a neutralizing agent that maintains the pH of the composition at a pH from about 5 to about 6.
19 . The topical pharmaceutical composition of claim 1 , comprising:
tretinoin in an amount ranging from about 0.001% to about 1% by weight of the composition;
a viscosity increasing agent in an amount ranging from about 0.6% to about 1% by weight of the composition;
a polymeric emulsifier in an amount ranging om about 0.04% to about 0.06% by weight of the composition;
mineral oil in an amount ranging from about 1% to about 5% by weight of the composition;
one or more humectants, moisturizing agents, antioxidants, preservatives, wetting agents, and/or neutralizing agents; and
water.
20 . A topical pharmaceutical composition for treating a skin condition or disorder, comprising:
tretinoin in an amount ranging from about 0.01% to about 1% by weight of the composition;
a polymeric emulsifier, wherein the polymeric emulsifier comprises a cross-linked copolymer of acrylic acid and C10-C30 alkyl acrylate and wherein the polymeric emulsifier is present in an amount ranging from to about 0.01% to about 0.095% by weight of the composition;
a viscosity increasing agent, wherein the viscosity increasing agent comprises a cross-linked homopolymer of an acrylic acid; and
an oil component, wherein the oil component is present in an amount ranging from about 0.1% to about 5% by weight.
21 . The topical pharmaceutical composition of claim 20 , comprising tretinoin in an amount of about 0.05% by weight of the composition.
22 . The topical pharmaceutical composition of claim 20 or 21 , wherein the polymeric emulsifier is a carbomer copolymer type B.
23 . The topical pharmaceutical composition of any one of claims 20 to 22 , wherein the polymeric emulsifier is present in an amount ranging from about 0.04% to about 0.06% by weight of the composition.
24 . The topical pharmaceutical composition of a any one of claims 20 to 23 , wherein the oil component comprises mineral oil.
25 . The topical pharmaceutical composition of any one of claims 20 to 24 , wherein the oil component is present in an amount ranging from about 1% to about 3% by weight of the composition.
26 . The topical pharmaceutical composition of any one of claims 20 to 25 , wherein the viscosity increasing agent is a carbomer homopolymer type A.
27 . The topical pharmaceutical composition of any one of claims 20 to 26 , wherein the viscosity increasing agent is present in an amount ranging from about 0.1% to about 2% by weight of the composition.
28 . The topical pharmaceutical composition of claim 27 , wherein the viscosity increasing agent is present in an amount ranging from about 0.6% to about 1% by weight of the composition.
29 . The topical pharmaceutical composition of any one of claims 20 to 28 , further comprising one or more preservatives; moisturizing agents, antioxidants; and/or humectants.
30 . The topical pharmaceutical composition of any one of claims 20 to 29 , further comprising a neutralizing agent that maintains the pH of the composition at a pH from about 5 to about 6.
31 . The topical pharmaceutical composition of claim 20 , comprising:
tretinoin in an amount of about 0.05% by weight of the composition;
a polymeric emulsifier in an amount ranging from about 0.04% to about 0.06% by weight of the composition, wherein the polymeric emulsifier is a carbomer copolymer type B;
a viscosity increasing agent in an amount ranging from about 0.6% to about 1% by weight of the composition; wherein the viscosity increasing agent is carbomer homopolymer type A;
an oil component in an amount ranging from about 0.1% to about 5% (e.g., from about 2% to about 4%, or from about 1% to about 3%) by weight of the composition, wherein the oil component is a mineral oil;
one or more moisturizing agents in an amount ranging from about 5% to about 20% by weight of the composition, wherein the moisturizing agents are sodium hyaluronate, soluble collagen, or a combination thereof;
a humectant in an amount ranging from about 5% to about 20% by weight of the composition, wherein the humectant is glycerin;
an antioxidant in an amount ranging from about 0.1% to about 2% by weight of the composition, wherein the antioxidant is butylated hydroxytoluene;
a wetting agent in an amount ranging from about 0.05% to about 0.5% by weight of the composition, wherein the wetting agent is octoxynol-9;
optionally, one or more preservatives in an amount ranging from about 0.25% to about 5% by weight of the composition, wherein the preservatives are benzyl alcohol, methyl paraben, or a combination thereof;
optionally, a neutralizing agent, wherein the neutralizing agent is trolamine; and
water.
32 . A topical pharmaceutical composition for treating a skin condition or disorder, wherein the topical pharmaceutical composition comprises:
tretinoin in an amount of about 0.05% by weight of the composition;
a carbomer copolymer type B in an amount ranging from about 0.04% to about 0.06% by weight of the composition;
a carbomer homopolymer type A in an amount ranging from about 0.2% to about 1% by weight of the composition;
mineral oil in an amount ranging from about 2% to about 4% by weight of the composition;
one or more preservatives, moisturizing agents, antioxidants, humectants, wetting agents, and/or neutralizing agents; and
water.
33 . The topical pharmaceutical composition of any one of claims 1 to 32 , wherein the composition has a viscosity from about 2,500 cP to about 18,000 cP.
34 . The topical pharmaceutical composition of any one of claims 1 to 32 , wherein the composition has a viscosity of less than about 15,000 cP.
35 . The topical pharmaceutical composition of claim 34 , wherein the composition has a viscosity from about 8,000 cP to about 12,000 cP.
36 . A kit comprising the topical pharmaceutical composition of any one of claims 1 to 35 .
37 . A method for treating a skin condition or disorder, comprising administering the topical pharmaceutical composition of any one of claims 1 to 35 to a subject in need thereof.
38 . The method of claim 37 , wherein the skin condition or disorder is acne vulgaris.
39 . The method of claim 37 or 38 , wherein the topical pharmaceutical composition is applied once daily to an affected area of skin.
40 . A method for treating acne vulgaris, the method comprising applying to the skin of a subject having acne vulgaris the topical pharmaceutical composition of any one of claims 1 to 35 .