Pharmaceutical tetracycline composition for dermatological use
Provided herein is a topical composition and related methods for making and using the composition. In a first aspect, the topical composition comprises minocycline, a magnesium salt, and a sulfite compound in a non-aqueous solvent. In yet another aspect, the topical composition comprises a tetracycline-class drug, a source of magnesium, a monohydric aliphatic alcohol, and a polyol, wherein (i) the ratio between the monohydric aliphatic alcohol and the propylene glycol is in the range of 1:1 to 99:1 by weight and (ii) the tetracycline-class drug is dissolved in the topical composition.
1. A topical composition, comprising:
between about 0.7% to about 2.5% by weight minocycline,
between about 0.8% to about 2.6% by weight of a divalent cation, selected from the group consisting of a magnesium cation, a calcium cation, an aluminum cation, and a zinc cation,
between about 0.1% to about 0.3% by weight of a sulfite compound, selected from the group consisting of a sulfite salt, a metabisulfite salt, and a bisulfite salt, and
a solvent system comprising ethanol, propylene glycol, and cineole;
wherein the minocycline is dissolved in the composition.
2. The topical composition of claim 1 , wherein the divalent cation is magnesium chloride.
3. The topical composition of claim 1 , wherein the sulfite compound is sodium meta-bisulfite.
4. The topical composition of claim 1 , wherein the composition comprises about 1.1% by weight of the minocycline.
5. The topical composition of claim 1 , wherein
the divalent cation is a magnesium cation, and
the composition comprises less than 5% water as measured by Karl Fischer titration.
6. The topical composition of claim 1 , wherein the composition comprises about 2.2% by weight of minocycline.
7. The topical composition of claim 2 , wherein the composition comprises about 1.2% by weight of magnesium chloride.
8. The topical composition of claim 1 , wherein the molar ratio of the divalent cation to the minocycline is in a range of about 2:1 to 100:1.
9. The topical composition of claim 2 , wherein the composition comprises about 2.3% by weight of magnesium chloride.
10. The topical composition of claim 1 , wherein the composition comprises about 76% by weight of ethanol.
11. The topical composition of claim 1 , wherein the composition comprises between about 72-77% by weight of ethanol.
12. The topical composition of claim 3 , wherein the composition comprises about 0.2% by weight of sodium meta-bisulfite.
13. The topical composition of claim 1 , wherein the composition comprises between about 18-21% by weight of propylene glycol.
14. The topical composition of claim 1 , wherein the composition comprises between about 0.9-1.3% by weight of cineole.
15. The topical composition of claim 1 , comprising about 1% by weight of minocycline; about 1.2% by weight of magnesium chloride; about 0.2% by weight of sodium meta-bisulfite; about 76% by weight of ethanol; about 20% by weight of propylene glycol; about 1% by weight of cineole; and further comprising about 0.6% by weight hydroxypropyl cellulose.
16. The topical composition of claim 1 , comprising about 2.2% by weight of minocycline; about 2.3% by weight of magnesium chloride; about 0.2% by weight of sodium meta-bisulfite; about 73% by weight of ethanol; about 20% by weight of propylene glycol; about 1% by weight of cineole; and further comprising about 0.6% by weight hydroxypropyl cellulose.
17. The topical composition of claim 1 , further comprising hydroxypropyl cellulose.
18. A method for treating an active dermatological inflammation or infection comprising applying the topical composition of claim 1 to an inflamed or infected area of skin of a human at least once daily for a period of at least 1 month.
19. The method of claim 18 wherein the active dermatological inflammation or infection is acne or rosacea.