TOPICAL FORMULATION FOR A JAK INHIBITOR
This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.
1 - 82 . (canceled)
83 . A pharmaceutical composition suitable for topical skin application comprising:
an oil-in-water emulsion comprising:
water
an oil component,
an emulsifier component,
a solvent component, and
a means for inhibiting JAK1 and/or JAK2,
wherein the oil-in-water emulsion in the composition is a solubilized cream for topical application.
84 . The composition of claim 83 , wherein the solubilized cream is suitable for application to the skin for up to 84 consecutive days.
85 . The composition of claim 83 , further comprising a stabilizing agent component.
86 . The composition of claim 83 , wherein the water is present in an amount ranging from about 40% to about 60% by weight of the composition, and the oil component is present in an amount ranging from about 17% to about 27% by weight of the composition.
87 . The composition of claim 86 , further comprising a stabilizing agent component present in an amount ranging from about 0.3% to about 0.5% by weight of the composition.
88 . The composition of claim 83 , wherein the means for inhibiting JAK1 and/or JAK2 is present in an amount ranging from about 0.5% to about 1.5% by weight of the composition.
89 . A method of treating a skin disorder in a human patient in need thereof, comprising:
applying to the patient's skin a pharmaceutically acceptable composition according to claim 83 ; wherein treating is one or more of inhibiting the skin disorder and ameliorating the skin disorder; and wherein the skin disorder is an autoimmune skin disorder.
90 . The method of claim 89 , wherein the applying step comprises application up to 84 consecutive days to the patient's skin.
91 . The method of claim 89 , wherein the autoimmune skin disorder is psoriasis or atopic dermatitis.
92 . The method of claim 89 , wherein the water is present in an amount ranging from about 40% to about 60% by weight of the composition, and the oil component is present in an amount ranging from about 17% to about 27% by weight of the composition.
93 . The method of claim 92 , wherein the composition further comprises a stabilizing agent component.
94 . The method of claim 89 , the means for inhibiting JAK1 and/or JAK2 is present in an amount ranging from about 0.5% to about 1.5% by weight of the composition.
95 . A method of inhibiting JAK1 and/or JAK2 in a human patient suffering from a skin disorder, comprising:
applying to the patient's skin a pharmaceutically acceptable composition according to claim 83 .
96 . The method of claim 95 , wherein the applying step comprises application up to 84 consecutive days to the patient's skin.
97 . The method of claim 95 , wherein the skin disorder is an autoimmune skin disorder.
98 . The method of claim 98 , wherein the skin disorder is atopic dermatitis.
99 . The method of claim 95 , wherein the water is present in an amount ranging from about 40% to about 60% by weight of the composition, and the oil component is present in an amount ranging from about 17% to about 27% by weight of the composition.
100 . The method of claim 99 , wherein the composition further comprises a stabilizing agent component.
101 . The method of claim 95 , wherein the means for inhibiting JAK1 and/or JAK2 is present in an amount ranging from about 0.5% to about 1.5% by weight of the composition.
102 . A method of treating atopic dermatitis in a human patient, comprising:
applying to the patient's skin a pharmaceutically acceptable composition according to claim 83 ; and wherein treating is one or more of inhibiting atopic dermatitis and ameliorating atopic dermatitis.
103 . The method of claim 102 , wherein the applying step comprises application up to 84 consecutive days to the patient's skin.
104 . The method of claim 102 , wherein the water is present in an amount ranging from about 40% to about 60% by weight of the composition, and the oil component is present in an amount ranging from about 17% to about 27% by weight of the composition.
105 . The method of claim 102 , wherein the composition further comprises a stabilizing agent component.
106 . The method of claim 102 , wherein treating is ameliorating atopic dermatitis.
107 . The method of claim 102 , wherein the means for inhibiting JAK1 and/or JAK2 is present in an amount ranging from about 0.5% to about 1.5% by weight of the composition.