Therapeutic anti-fungal nail preparation

• US 6,159,977 A
• Filed: 11/16/1998
• Issued: 12/12/2000
• Est. Priority Date: 11/16/1998
• Status: Expired due to Term

• Current Assignee: Astan Incorporated
• Original Assignee: Astan Incorporated
• Inventors: Reeves, Stanley Forrest
• Primary Examiner(s): Dees, Jose' G.
• Assistant Examiner(s): PRYOR, ALTON NATHANIEL
• Application Number:
  US09/193,073
• Time in Patent Office: 757 Days
• Field of Search: 514/946, 514/252, 514/359, 514/570, 514/345, 514/723, 514/396, 514/397, 514/272, 514/479
• US Class Current: 514/254.07
• 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 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 31/20 having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
• CPC Class Codes: A61K 31/22 of acyclic acids, e.g. pravastatin
• CPC Class Codes: A61K 31/27 of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
• CPC Class Codes: A61K 31/415 1,2-Diazoles
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 31/47 Quinolines; Isoquinolines
• CPC Class Codes: A61K 31/495 having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazinesA61K31/48 takes precedence ; with three nitrogen atoms A61K31/53
• CPC Class Codes: A61K 31/505 Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• CPC Class Codes: A61K 31/70 Carbohydrates; Sugars; Derivatives thereof sorbitol A61K31/047
• 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 47/20 containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• 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 31/10 Antimycotics

Abstract

A therapeutic solution and application procedure for curing Nail fungus infections or Onychomycosis comprising a combination of an anti-fungal agent with DMSO in a anhydrous solution of Polyglycol, and including a secondary anti-inflammatory agent. The DMSO acts as a delivery vehicle so that active anti-fungal agents such as Miconazole in combination with an anti-inflammatory compound such as ibuprofen can be delivered directly to fungal infected areas under and around the nail. The DMSO, Miconazole, and ibuprofen are dissolved in a viscous solution of Polyglycol so that the combined ingredients may be applied directly to the affected nails with superior penetration. The therapeutic solution is formulated by dissolving the Miconazole into the Polyglycol over heat and adding the ibuprofen and DMSO over additional heat in a timed process. Repeated applications of the resulting solution on Onychomycosis infected nails over one 4-6 week period yields satisfactory result rates as high as 85-90% without augmenting the therapy with systemic drugs. Most versions of the therapeutic solution are anticipated to not require a prescription.

Claims

1. A topical solution effective in inhibiting the growth of micro-organisms causing Onychomycosis, consisting essentially of:

a. a pharmacological agent for killing micro-organisms causing Onychomycosis;

b. an anti-inflammatory;

c. a polyglycol base into which said agent and said anti-inflammatory are dissolved; and

,

d. a solution of DMSO mixed with said polyglycol base.

2. A topical solution as recited in claim 1, wherein said pharmacological agent is an antifungal agent selected from the group consisting of Miconazole, Clotrimazole, Tioconazole, Nystatin, Terconazole, Butoconazole Nitrate, Unecylenic Acid, Clioquinol, Ciclopirox Olamine, Econazole Nitrate, Triacetin, Tolnaftate, Flucytosine, and Ketoconazole.

3. A topical solution as recited in claim 2, wherein said anti-inflammatory is ibuprofen.

4. A topical solution as recited in claim 3, wherein said ibuprofen is 4% by volume.

5. A topical solution as recited in claim 2, wherein said polyglycol is of the molecular weight of 300.

6. A topical solution as recited in claim 1, wherein said topical solution contains 40% by volume DMSO.

7. A topical solution as recited in claim 1, wherein said pharmacological agent is between 1-30% by volume of said solution.

8. A topical solution as recited in claim 1, wherein said pharmacological agent is Miconazole.

9. A pharmaceutical composition for enhancing penetration of a pharmaceutically active antifungal substance, consisting essentially of:

a. an antifungal agent selected from the group consisting of Miconazole, Clotrimazole, Tioconazole, Nystatin, Terconazole, Butoconazole Nitrate, Unecylenic Acid, Clioquinol, Ciclopirox Olamine, Econazole Nitrate, Triacetin, Tolnaftate, Flucytosine, and Ketoconazole;

b. ibuprofen;

c. a polyglycol base into which said agent and said ibuprofen are dissolved; and

,

d. a solution of DMSO mixed with said polyglycol base.

10. A pharmaceutical composition for enhancing penetration of a therapeutic agent through unguis, consisting essentially of:

a. an antifungal agent for killing said micro-organisms causing Onychomycosis;

b. an anti-inflammatory agent for enhancing efficacy of said killing means;

c. an anhydrous base into which said antifungal agent and said anti-inflammatory agent are dissolved; and

,

d. a solution of DMSO mixed with said anhydrous base for enhancing penetration of said antifungal agent into said unguis.

11. A Pharmaceutical composition as recited in claim 10, wherein said anhydrous base comprises polyglycol.

12. A composition for enhancing transdermal and transcutinel penetration of a pharmaceutically active substance, consisting essentially of:

a. from about 1 to 30% by volume of an antifungal agent;

b. from about 1 to 40% by volume of ibuprofen;

c. from about 10 to 80% by volume of a polyglycol base into which said agent and said ibuprofen are dissolved; and

,

d. from about 10 to 80% solution of DMSO mixed with said polyglycol base and in an inverse proportion by volume with said polyglycol base .

13. A method of making a therapeutic solution for inhibiting the growth of micro-organisms causing Onychomycosis, comprising the steps of:

a. heating and maintaining 40 ml of Polyglycol liquid at 45°

C.;

b. slowly stirring in 4 grams of Miconazole into said heated Polyglycol until dissolved;

c. adding 4 grams of ibuprofen to said Polyglycol and stirring until uniform;

d. slowly adding 40 ml of 99% pure DMSO liquid to said Polyglycol; and

,

e. allowing said solution to cool to room temperature while stirring until all ingredients are uniform.

14. The method as recited in claim 13, wherein said Miconazole is sifted into said heated Polyglycol base.

15. The method as recited in claim 13, wherein said ibuprofen is sifted into said heated Polyglycol base.

16. The method as recited in claim 13, wherein said method of making a therapeutic solution includes the additional step of filtering said solution after said cooling step.

17. The method as recited in claim 13, wherein said step of stirring in Miconazole comes after said step of adding ibuprofen.

18. A method of killing micro-organisms causing nail fungus, comprising the step of applying to a nail a solution effective in eliminating fungi, said solution consisting essentially of:

a. an anti-fungal agent selected from the group consisting of Miconazole, Clotrimazole, Tioconazole, Nystatin, Terconazole, Butoconazole Nitrate, Unecylenic Acid, Clioquinol, Ciclopirox Olamine, Econazole Nitrate, Triacetin, Tolnaftate, Flucytosine, and Ketoconazole;

b. ibuprofen;

c. a polyglycol base into which said agent and said ibuprofen are dissolved; and

,

d. a solution of DMSO mixed with said polyglycol base.