Claims for Patent: 9,662,394

Summary for Patent: 9,662,394

Title:	Stabilized efinaconazole compositions
Abstract:	The present invention provides compositions containing efinaconazole, butylated hydroxytoluene, a salt of ethylenediaminetetraacetic acid, and optional citric acid. The compositions exhibit stable color profiles and are useful in the treatment of fungal infections.
Inventor(s):	Bhatt; Varsha (San Francisco, CA), Desai; Nayan (Santa Rosa, CA), Pillai; Radhakrishnan (Santa Rosa, CA)
Assignee:	Dow Pharmaceutical Sciences, Inc. (Petaluma, CA)
Application Number:	14/505,379
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,662,394
Patent Claims:	1. A composition comprising about 8% to about 12% efinaconazole by weight, water, C12-15 alkyl lactate, diisopropyl adipate, cyclomethicone, ethanol, butylated hydroxytoluene (BHT), a salt of ethylenediaminetetraacetic acid (EDTA), and citric acid, wherein the amount of BHT is in the range of about 0.01% (w/w) to about 2% (w/w), wherein the amount of the salt of EDTA is in the range of about 0.0001% (w/w) to about 1.5% (w/w), wherein the amount of citric acid is in the range of about 0.05% (w/w) to about 0.25% (w/w), wherein the composition is formulated as a solution, and wherein the amounts of BHT and the salt of EDTA are sufficient to ensure the composition is (i) colorless upon initial formulation and (ii) colorless or pale yellow after storage for three weeks at a temperature of about 40.degree. C. 2. The composition of claim 1, wherein the amount of efinaconazole is about 10% (w/w). 3. The composition of claim 1, wherein the amount of the salt of EDTA is in the range of about 0.0001% (w/w) to about 0.0005% (w/w). 4. The composition of claim 3, wherein the amount of the salt of EDTA is about 0.00025% (w/w) and the amount of BHT is about 0.1% (w/w). 5. The composition of claim 1, wherein the amount of the salt of EDTA is in the range of about 0.01% (w/w) to about 1% (w/w). 6. The composition of claim 5, wherein the amount of the salt of EDTA is about 0.1% (w/w) and the amount of BHT is about 0.1% (w/w). 7. The composition of claim 1, wherein the composition comprises from about 0.075% citric acid (w/w) to about 0.15% citric acid (w/w). 8. The composition of claim 1, wherein the color of the composition is determined by visual inspection. 9. The composition of claim 1, wherein the color is determined by assessing UV-vis absorbance values. 10. The composition of claim 9, wherein after storage for one month at 65.degree. C. the composition exhibits UV-vis absorbance values of 0.4 absorbance units (AU) or less at 400 nm; 0.1 AU or less at 500 nm; and/or 0.1 AU or less at 600 nm. 11. The composition of claim 1, wherein the composition is a pharmaceutically acceptable formulation that is effectively absorbed in the treatment of the nail. 12. The composition of claim 1, comprising: ethanol in an amount ranging from 50% to 70% by weight, cyclomethicone in an amount ranging from 10% to 15% by weight, diisopropyl adipate in an amount ranging from 8% to 15% by weight, and C12-15 alkyl lactate in an amount ranging from 8% to 15% by weight. 13. The composition of claim 12, wherein the amount of the salt of EDTA is about 0.00025% (w/w) and the amount of BHT is about 0.1% (w/w). 14. The composition of claim 12, wherein the amount of citric acid is in the range of about 0.075% (w/w) to about 0.15% (w/w). 15. The composition of claim 13, wherein the amount of citric acid is in the range of about 0.075% (w/w) to about 0.15% (w/w). 16. A method of treating a fungal infection comprising administering a therapeutically effective amount of a formulation according to claim 11 to a patient in need of such treatment.