Compositions and methods for treating diseases of the nail

• US 9,877,955 B2
• Filed: 10/24/2016
• Issued: 01/30/2018
• Est. Priority Date: 01/03/2008
• Status: Active Grant

• Current Assignee: Bausch Health Ireland Limited (Bausch Health Cos., Inc.)
• Original Assignee: Dow Pharmaceutical Sciences Incorporated (Bausch Health Cos., Inc.)
• Inventors: Winckle, Gareth, Fieldson, Gregory T.
• Primary Examiner(s): Stevens, Mark V
• Application Number:
  US15/332,909
• Publication Number:
  US 20170165249A1
• Time in Patent Office: 463 Days
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/454 containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• CPC Class Codes: A61K 8/34 Alcohols
• CPC Class Codes: A61K 8/496 Triazoles or their condensed derivatives, e.g. benzotriazoles
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/10 Antimycotics

Abstract

Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, and which composition is effective in treating a disorder of the nail or nail bed.

Claims

1. A method for the treatment of onychomycosis comprising topically applying to the surface of the nail of an individual suffering from onychomycosis a pharmaceutical composition comprising:

50% w/w to 70% w/w ethanol,

8% w/w to 15% w/w diisopropyl adipate,

8% w/w to 15% w/w C12-15 alkyl lactate,

10% w/w to 15% w/w cyclomethicone, and

2% w/w to 15% w/w (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidine-1-yl)-1-(1H-1,2,4-triazole-1-yl)butane-2-ol;

wherein the composition is formulated as a solution; and

wherein the application of the composition is in an amount and for a time sufficient to ameliorate the symptoms of the onychomycosis.

2. The method of claim 1, wherein the pharmaceutical composition comprises about 12% w/w diisopropyl adipate, about 10% w/w C12-15 alkyl lactate, and about 13% w/w cyclomethicone.

3. The method of claim 2, wherein the pharmaceutical composition comprises about 10% w/w (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidine-1-yl)-1-(1H-1,2,4-triazole-1-yl)butane-2-ol.

4. The method of claim 1, wherein the pharmaceutical composition comprises about 57% w/w ethanol.

5. The method of claim 4, wherein the pharmaceutical composition comprises about 10% w/w (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidine-1-yl)-1-(1H-1,2,4-triazole-1-yl)butane-2-ol.

6. The method of claim 1, wherein the pharmaceutical composition does not comprise a polymeric film forming compound.

7. The method of claim 2, wherein the pharmaceutical composition does not comprise a polymeric film forming compound.

8. The method of claim 3, wherein the pharmaceutical composition does not comprise a polymeric film forming compound.

9. The method of claim 4, wherein the pharmaceutical composition does not comprise a polymeric film forming compound.

10. The method of claim 5, wherein the pharmaceutical composition does not comprise a polymeric film forming compound.

11. The method of claim 1, wherein the pharmaceutical composition is administered twice daily to the surface of the nail.

12. The method of claim 1, wherein the pharmaceutical composition is administered once daily to the surface of the nail.

13. The method of claim 1, wherein the pharmaceutical composition is administered one weekly to the surface of the nail.

14. A method for the treatment of onychomycosis comprising topically applying to the surface of the nail of an individual suffering from onychomycosis a pharmaceutical composition comprising:

50% w/w to 70% w/w ethanol,

about 12% w/w diisopropyl adipate,

about 10% w/w C12-15 alkyl lactate,

about 13% w/w cyclomethicone, and

about 10% w/w (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidine-1-yl)-1-(1H-1,2,4-triazole-1-yl)butane-2-ol;

wherein the composition is formulated as a solution; and

wherein the application of the composition is in an amount and for a time sufficient to ameliorate the symptoms of the onychomycosis.