LAURETH-4 CONTAINING TOPICAL FORMULATIONS
The present invention is a method and composition comprising laureth-4 in topical formulations, wherein the laureth-4 increases the penetration of active ingredients across the skin. In a particularly preferred embodiment, the active ingredient is SHR0302.
1 . A topical pharmaceutical composition comprising SHR0302, laureth-4, and a solvent.
2 . The topical pharmaceutical composition of claim 1 , wherein the SHR0302 is present in an amount of about 0.1 to about 1.0% w/w.
3 . The topical pharmaceutical composition of claim 1 , wherein the laureth-4 is present in an amount of about 0.5 to about 5% w/w.
4 . The topical pharmaceutical composition of claim 1 , further comprising dimethyl sulfoxide.
5 . The topical pharmaceutical composition of claim 1 , further comprising an antioxidant, a preservative, an emulsifier, a moisturizer, or a thickener.
6 . The topical pharmaceutical composition of claim 1 , wherein said composition is selected from the group consisting of an oil-in-water emulsion, a water-in-oil emulsion, a microemulsion, a nanoemulsion, a foam, a spray, a hydrophilic ointment, or a hydrophobic ointment.
7 . The topical pharmaceutical composition of claim 1 , further comprising a corticosteroid, timolol, methotrexate, or cyclosporine.
8 . The topical pharmaceutical composition of claim 1 , wherein skin penetration of the topical pharmaceutical composition is enhanced by 5-fold to 30-fold relative to the same topical pharmaceutical formulation without laureth-4 as measured by in vitro permeation testing in excised human cadaver skin dermatomed to a target thickness of 500 microns.
9 . A method of treating an inflammatory skin disease, disorder, or condition in a subject in need thereof, comprising:
topically administering to the subject a pharmaceutical composition comprising SHR0302, laureth-4, and a solvent.
10 . The method of claim 9 , wherein said inflammatory skin disease, disorder, or condition is atopic dermatitis, rosacea, psoriasis, seborrheic dermatitis, vitiligo, eczema, or alopecia areata.
11 . The method of claim 9 , wherein the pharmaceutical compositions is administered to the subject one or more times per day.
12 . The method of claim 9 , wherein the SHR0302 is present in the pharmaceutical composition in an amount of about 0.1 to about 1.0% w/w.
13 . The method of claim 9 , wherein the laureth-4 is present in the pharmaceutical composition in an amount of about 0.5 to about 5% w/w.
14 . The method of claim 9 , wherein the pharmaceutical composition further dimethyl sulfoxide.
15 . The method of claim 9 , wherein the pharmaceutical composition further comprising a corticosteroid, timolol, methotrexate, or cyclosporine.
16 . The method of claim 9 , wherein skin penetration of the topical pharmaceutical composition is enhanced by 5-fold to 30-fold relative to the same topical pharmaceutical formulation without laureth-4 as measured by in vitro permeation testing in excised human cadaver skin dermatomed to a target thickness of 500 microns.
17 . A method for enhancing the skin penetration in a human subject of a topical pharmaceutical formulation comprising:
preparing a formulation comprising SHR0302, laureth-4 and a solvent,
wherein the skin penetration of the topical pharmaceutical composition is enhanced by 5-fold to 30-fold relative to the same topical pharmaceutical formulation without laureth-4 in the subject.
18 . The topical pharmaceutical composition of claim 17 , wherein the SHR0302 is present in an amount of about 0.1 to about 1.0% w/w.
19 . The topical pharmaceutical composition of claim 17 , wherein the laureth-4 is present in an amount of about 0.5 to about 5% w/w.
20 . The topical pharmaceutical composition of claim 17 , further comprising dimethyl sulfoxide.