TOPICAL COMPOSITIONS WITH STABLE SOLUBILIZED SELECTIVE RETINOIDS AND/OR TETRACYCLINE-CLASS ANTIBIOTICS
Topical compositions for dermatological use are described. The topical compositions generally comprise a selective retinoid, such as tazarotene or adapalene, and/or a tetracycline-class antibiotic, such as minocycline or doxycycline, and a monohydric aliphatic alcohol. The compositions may further comprise a divalent cation, such as magnesium, calcium, or zinc, and an antioxidant, such as a sulfite or a thiosulfate. The composition may further comprise a carboxylate ester solvent.
1 . A topical composition, comprising:
a drug selected from a selective retinoid, a tetracycline-class drug, and a combination of a selective retinoid and a tetracycline-class drug,
a monohydric aliphatic alcohol, and
a carboxylate ester with a ratio of ester groups to carbon atoms of at least 0.05.
2 . The topical composition of claim 1 , wherein the drug is dissolved in the composition.
3 . The topical composition of claim 1 , further comprising a salt of a divalent cation.
4 . The topical composition of claim 1 , further comprising an antioxidant selected from a sulfite, a thiosulfate, and a combination thereof.
5 . The topical composition of claim 4 , wherein the antioxidant is a divalent cation.
6 . The topical composition of claim 5 , wherein the antioxidant with a divalent cation is magnesium sulfite, magnesium thiosulfate, or a combination thereof.
7 . A topical composition, comprising:
a selective retinoid, a tetracycline-class drug, or both a selective retinoid and a tetracycline-class drug,
a monohydric aliphatic alcohol,
a salt of a divalent cation, and
an antioxidant.
8 . The topical composition of claim 7 , wherein the molar ratio of the divalent cation to the tetracycline-class drug in the topical composition is at least about 4:1.
9 . The topical composition claim 7 , further comprising a carboxylate ester with a ratio of ester groups to carbon atoms of at least 0.05.
10 . The topical composition of claim 9 , wherein the concentration of the carboxylate ester in the topical composition is between about 1-30% by weight.
11 . The topical composition of claim 9 , wherein the carboxylate ester is selected from the group consisting of isopropyl myristate, medium-chain triglycerides, diisopropyl adipate, ethyl acetate, triacetin, dimethyl succinate, propyl acetate, and combinations thereof.
12 . The topical composition of claim 7 , wherein the salt of a divalent cation is a magnesium salt.
13 . The topical composition of claim 12 , wherein the magnesium salt is magnesium chloride, magnesium sulfite, or magnesium thiosulfate.
14 . The topical composition of claim 7 , wherein the monohydric aliphatic alcohol is selected from the group consisting of ethanol, isopropanol, propyl alcohol, tert-butyl alcohol, and combinations thereof.
15 . The topical composition of claim 14 , wherein the concentration of the monohydric aliphatic alcohol in the topical composition is between about 50-99% by weight.
16 . The topical composition of claim 7 , wherein the selective retinoid is dissolved in the composition.
17 . The topical composition of claim 16 , wherein the tetracycline class drug is dissolved in the composition.
18 . The topical composition of claim 7 , wherein the tetracycline-class drug is minocycline or doxycycline.
19 . The topical composition of claim 7 , wherein the selective retinoid is tazarotene or adapalene.
20 . The topical composition of claim 7 , further comprising a polyol.
21 . The topical composition of claim 20 , wherein the polyol is a C3-C8 diol or a triol.
22 . The topical composition of claim 20 , wherein the polyol is selected from the group consisting of propylene glycol, glycerol and glycerin.
23 . The topical composition of claim 20 , wherein the concentration of the polyol in the topical composition is between about 2-40% by weight.
24 . The topical composition of claim 7 , further comprising a sulfite, a thiosulfate, or both.
25 . The topical composition of claim 24 , wherein the sulfite is sodium bisulfite, sodium metabisulfite, magnesium sulfite, or a combination thereof, and the thiosulfate is sodium thiosulfate, ammonium thiosulfate, magnesium thiosulfate or a combination thereof.
26 . A method for treatment of a dermatological condition or disease, comprising:
applying the topical composition of claim 1 to an exterior epithelial surface of a mammalian body at least once daily for a period of at least 4 weeks.
27 . The method of claim 26 , wherein the dermatological condition or disease is selected from the group consisting of acne, rosacea, and psoriasis.
28 . The method of claim 26 , wherein the dermatological condition or disease is an orphan disease selected from Hidradenitis suppurativa, Hailey Hailey disease, and Darier's disease.
29 . A method for treatment of a dermatological condition or disease, comprising:
applying the topical composition of claim 7 to an exterior epithelial surface of a mammalian body at least once daily for a period of at least 4 weeks.
30 . The method of claim 29 , wherein the dermatological condition or disease is selected from the group consisting of acne, rosacea, and psoriasis.
31 . The method of claim 29 , wherein the dermatological condition or disease is an orphan disease selected from Hidradenitis suppurativa, Hailey Hailey disease, and Darier's disease.