PHARMACEUTICAL COMPOSITION FOR APPLICATION TO NAIL

Abstract

Since treatment effects of conventional external preparations were not satisfactory, it is aimed to provide a novel external preparation that is excellent in drug permeability to nail, capable of fully exhibiting effects of an antifungal drug, and effective for treatments of diseases such as nail mycosis and nail candidiasis, particularly, treatments for nail tinea. The external preparation of this invention is a pharmaceutical composition for nail characterized by containing an antifungal drug, alkylpyrrolidone or a derivative thereof, and a crosslinking hydrogel.

Claims

1. A pharmaceutical composition for nails consisting essentially of an antifungal drug, alkylpyrrolidone or a derivative thereof, a crosslinking hydrogel, and optionally one or both of a polyvalent alcohol and one or more adhesion enhancers: wherein the crosslinking hydrogel is obtained by crosslinking a water-soluble crosslinking polymer using a salt of a polyvalent metal in the presence of water.

2. The pharmaceutical composition for nails according to claim 1, wherein the antifungal drug is selected from the group consisting of lanoconazole, bifonazole, neticonazole, cloconazole, clotrimazole, ketoconazole, iconazole, econazole, oxiconazole, sulconazole, miconazole, isoconazole, thioconazole, fluconazole, itraconazole, luliconazole, terbinafine, butenafine, tolnaftate, amorolfine, and nystatin or pharmacologically acceptable salts thereof.

3. The pharmaceutical composition for nails according to claim 1, wherein the antifungal drug is hardly soluble to water.

4. The pharmaceutical composition for nails according to claim 1, wherein the alkylpyrrolidone or a derivative thereof is one or more selected from the group consisting of N-methyl-2-pyrrolidone, N-(2-hydroxyethyl)pyrrolidone, N-octylpyrrolidone, N-vinyl-2-pyrrolidone, 2-pyrrolidone, and 3-pyrrolidone.

5. (canceled)

6. The pharmaceutical composition for nails according to claim 1, wherein the water-soluble crosslinking polymer is one or more selected from the group consisting of partially neutralized polyacrylate, polyacrylic acid, sodium polyacrylate, carboxymethyl cellulose sodium, and gelatin.

7. The pharmaceutical composition for nails according to claim 1, further comprising a polyvalent alcohol.

8. The pharmaceutical composition for nails according to claim 7, wherein the polyvalent alcohol is one or more selected from the group consisting of polyethyleneglycol having an average molecular weight of 200, 300, 400, 600, 1000, 1500, 1540, 4000, 6000, 20000, or 35000, propyleneglycol, dipropyleneglycol, polypropyleneglycol, 1,3-butyleneglycol, 1,4-butyleneglycol, isobutyleneglycol, glycerin, diglycerin, and sorbitol.

9. The pharmaceutical composition for nails according to claim 1, further comprising one or more adhesion enhancers selected from the group consisting of starch acrylate, polyvinyl alcohol, a carboxyvinyl polymer, hydroxypropyl cellulose, carboxymethyl cellulose, casein sodium, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, polyvinyl pyrrolidone, sodium alginate, and a methylvinylether-maleic anhydride copolymer.

10. An adhesive patch for nails comprising a pharmaceutical composition applied and spread on a support, wherein the pharmaceutical composition consists essentially of an antifungal drug, alkylpyrrolidone or a derivative thereof, and a crosslinking hydrogel, and optionally one or both of a polyvalent alcohol and one or more adhesion enhancers, wherein the crosslinking hydrogel is obtained by crosslinking a water-soluble crosslinking polymer using a salt of a polyvalent metal in the presence of water.

11. The adhesive patch for nails according to claim 10, wherein a cover sheet having an adhesive layer thereon is further attached to a surface of the support reverse to a surface on which the pharmaceutical composition for nail is applied and spread.

12. The adhesive patch for nails according to claim 10, wherein the antifungal drug is selected from the group consisting of lanoconazole, bifonazole, neticonazole, cloconazole, clotrimazole, ketoconazole, iconazole, econazole, oxiconazole, sulconazole, miconazole, isoconazole, thioconazole, fluconazole, itraconazole, luliconazole, terbinafine, butenafine, tolnaftate, amorolfine, and nystatin or pharmacologically acceptable salts thereof.

13. The adhesive patch for nails according to claim 10, wherein the antifungal drug is hardly soluble to water.

14. The adhesive patch for nails according to claim 10, wherein the alkylpyrrolidone or a derivative thereof is one or more selected from the group consisting of N-methyl-2-pyrrolidone, N-(2-hydroxyethyl) pyrrolidone, N-octylpyrrolidone, N-vinyl-2-pyrrolidone, 2-pyrrolidone, and 3-pyrrolidone.

15. The adhesive patch for nails according to claim 10, wherein the water-soluble crosslinking polymer is one or more selected from the group consisting of partially neutralized polyacrylate, polyacrylic acid, sodium polyacrylate, carboxymethyl cellulose sodium, and gelatin.

16. The adhesive patch for nails according to claim 10, wherein the pharmaceutical composition further comprises a polyvalent alcohol.

17. The adhesive patch for nails according to claim 16, wherein the polyvalent alcohol is one or more selected from the group consisting of polyethyleneglycol having an average molecular weight of 200, 300, 400, 600, 1000, 1500, 1540, 4000, 6000, 20000, or 35000, propyleneglycol, dipropyleneglycol, polypropyleneglycol, 1,3-butyleneglycol, 1,4-butyleneglycol, isobutyleneglycol, glycerin, diglycerin, and sorbitol.

18. The adhesive patch for nails according to claim 10, wherein the pharmaceutical composition further comprise one or more adhesion enhancers selected from the group consisting of starch acrylate, polyvinyl alcohol, a carboxyvinyl polymer, hydroxypropyl cellulose, carboxymethyl cellulose, casein sodium, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, polyvinyl pyrrolidone, sodium alginate, and a methylvinylether-maleic anhydride copolymer.

19. The adhesive patch for nails according to claim 10, wherein a content of water in the pharmaceutical composition is 20 to 80%.

20. The pharmaceutical composition for nails according to claim 1, wherein a content of water in the pharmaceutical composition is 20 to 80%.

Description

BRIEF DESCRIPTION OF THE DRAWINGS

[0090] FIG. 1 A diagram showing a relationship between an elapsed time and an accumulated amount of an antifungal drug permeated into the nail plate.

[0091] FIG. 2 One example of a plan view of an adhesive patch for nail of this invention with a cover sheet.

[0092] FIG. 3 One example of a sectional view of the adhesive patch for nail of this invention with a cover sheet.

[0093] FIG. 4 One example of a plan view of the adhesive patch for nail in the form of a sheet of this invention with a cover sheet.

DESCRIPTION OF REFERENCES AND SIGNS

[0094] 1: support [0095] 2: adhesive layer [0096] 3: cover sheet [0097] 4: liner [0098] 5: pharmaceutical composition for nail