Topical formulations for the treatment of nail fungal diseases
AssigneeBertek Pharmaceuticals, Inc.
InventorsBhaskar Chaudhuri, Ming Fai Chim, Daniel Bucks
Life of this patent
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Abstract
Stable, topical formulations useful for treating a nail fungal disease are disclosed. The compositions comprise an antifungal compound and at least one pharmaceutically acceptable excipient sufficient to form a gel. The antifungal compound is represented by the formula ##STR1## where R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen or lower alkyl; X is --(CH.sub.2).sub.n -- in which n is 0, 1 or 2; Y is aryl or heteroaryl; and Ar is aryl or heteroaryl. The composition is applied to the afflicted nail for once a day until the fungal disease is cured.
Claims22
A topical antifungal composition for treating a nail fungal disease in a mammal, which composition comprises:
- (a) about 1% by weight to about 10% by weight of an antifungal compound, or a pharmaceutically acceptable salt thereof, wherein the antifungal compound is represented by the formula ##STR5## wherein:
- R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen or lower alkyl;
- X is --(CH.sub.2).sub.n -- in which n is 0, 1 or 2;
- Y is aryl or heteroaryl;
- and Ar is aryl or heteroaryl;
- and
- (b) about 30% by weight to about 70% by weight of a pharmaceutically-acceptable solvent,
- (c) about 0.5% by weight to about 15% by weight of a gelling agent,
- (d) about 0.5% by weight to about 10% by weight of an adhesion-promoting agent,
- (e) about 0.1% by weight to about 3% by weight of a film-forming agent,
- (f) about 0.5% by weight to about 5% by weight of a surfactant,
- (g) about 0% by weight to about 20% by weight of a keratolytic agent, and
- (h) water in an amount sufficient to bring the composition to 100%;
- wherein said composition is capable of adhering to the surface of a human nail and delivering the antifungal compound through the nail barrier.
A method of treating a nail fungal disease in a human, which method comprises
- (a) applying a therapeutically-effective amount of a topical antifungal gel composition to the surface of the nail to be treated,
- (b) maintaining the composition on the nail for at least about 4 hours to about 12 hours,
- (c) removing the composition from the nail for about 4 to 12 hours, and
- (d) repeating steps (a) through (c) until the nail fungal disease has been successfully treated, wherein the composition comprises
- (i) about 1% by weight to about 10% by weight of an antifungal compound represented by the formula ##STR6## wherein:
- R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen or lower alkyl;
- X is --(CH.sub.2).sub.n -- in which n is 0, 1 or 2;
- Y is aryl or heteroaryl;
- and Ar is aryl or heteroaryl and
- (ii) about 30% by weight to about 70% by weight of a pharmaceutically-acceptable solvent,
- (iii) about 0.5% by weight to about 15% by weight of a gelling agent,
- (iv) about 0.5% by weight to about 10% by weight of an adhesion-promoting agent,
- (v) about 0.1% by weight to about 3% by weight of a film-forming agent,
- (vi) about 0.5% by weight to about 5% by weight of a surfactant,
- (vii) about 0% by weight to about 20% by weight of a keratolytic agent, and
- (viii) water in an amount sufficient to bring the composition to 100%;
- wherein said composition is capable of adhering to the surface of the nail to deliver the antifungal compound through the nail barrier.
Dependencies are inferred from the claim text.