Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q3/00—Manicure or pedicure preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/19—Carboxylic acids, e.g. valproic acid
  • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/275—Nitriles; Isonitriles
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/74—Synthetic polymeric materials
  • A61K31/745—Polymers of hydrocarbons
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/74—Synthetic polymeric materials
  • A61K31/785—Polymers containing nitrogen
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
  • A61K9/7015—Drug-containing film-forming compositions, e.g. spray-on
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/10—Antimycotics

Definitions

• the present invention relates to treatment of nail fungi and, more particularly, this invention relates to a novel, effective topical treatment of toenail fungi.
• Fungi includes yeasts, molds, rusts and mushrooms. Of the 100,000 known species, only 150 regularly cause disease. Dermatophytes which include tinea Mguium are the main cause of onychomycosis the detachment of the nail from its bed at its distal or lateral attachments especially in the dark, sweaty environment of toenails. The fungi create micropores in the nails. They also cause unsightly discoloration and thickening of the nails and attack the tissue in the nailbed under the nails. Continued presence of the fungi can lead to secondary bacterial infections in subjects having poor circulation in the extremities, such as diabetes and eventually to gangrene and amputation of the toes.
• Topical antifungals used for treatment of toe fungus disease are not nearly as effective against tinea copitis and tinea unguium. The following older topical treatments are still available over the counter (OTC).
• Systematic antifungals such as griseofulvin, Amphotericin B, imidazoles, triazoles, flucytosine or terbinafine must be taken for several months while closely monitoring liver enzymes since there is risk of damage to the liver.
• the selling price of typical nail fungus medicines is as follows:
• Medication Amount Cost Lamasil (terbinafine) 90 tablets $971.66 Sporanox (traconazole) 84 tablets $797.71 Penlac (cyclopiox 8% laquer) 6.6 ml $147.00
• Nail lacquers may induce side effects such as sensitization and allergic contact dermatitis (European Journal of Dermatology, Volume 10, Number 3, 223-5, Avril-Mai 2000.
• ECA Ethylcyanoacrylate
• Liquids containing Cyanoarcrylate ester such as Cyanoacrylate ethyl have chemical properties capable of effectively controlling fungal nail disease.
• these chemicals can penetrate beneath the nail surface and coat or fill the micro pores created by fungi.
• the liquid solidifies. Nails treated with the liquid harden.
• the nail/hardened plastic is sufficiently durable to maintain its condition for up to six weeks. The hardened plastic effectively forms a moisture barrier. Without moisture, onychomycosis is incapable of further nail degradation and the disease is controlled or even eliminated.
• Cyanoacrylate ester such as Cyanoacrylate ethyl have high absorbing ability; they are good vehicles for delivery of other antifungal medications such as Clotrimazole, Nystatin Griseofulvin, Ketoconazole, Terbinafine, Itraconazole and others. Therefore, mixing a cyanoacrylate ester with one of the antifungal medications may have an enhanced treatment effect on Onychomycosis fungi. Addition of 1-12%, preferably 2-10% of undecylenic acid has been shown to inhibit the spread of infection and to remove the yellow-color of infected nails as does the presence of a small amount of hydroquine.
• the fungus infected nail becomes microporus.
• the viscosity of the coating solution is selected such that the solution enters the pores and progresses through the thickness of the nail to the nail bed.
• the compound that provides the popular cyanoacrylate, SUPERGLUE with adhesive properties is methyl cyanoacrylate.
• esters of alkenoic acids have the general formula:
• R is a hydrocarbon group having 1 to 12 carbon atoms, preferable an alkyl group having 2-8 carbon atoms.
• the preferred ester is ethylcyanoacrylate (ECA) through many of the other commercially available esters where R is ethyl, propyl, butyl octyl, or their mixtures, are available and will form impervious, films.
• ECA ethylcyanoacrylate
• cyanoacrylate does not air dry.
• cyanoacrylates cure (convert from liquid to solid) in the prescense of weak bases such as water, alcohol, and blood.
• weak bases such as water, alcohol, and blood.
• a thin layer of water is present on almost all surfaces. This accounts for many unintended adhesions involving appendages and/or expensive tools.
• the curing process involves the anionic chain polymerization reaction, which occurs as follows:
• the weak base (X) donates an electron pair to a cyanoacrylate monomer.
• the CH 2 group is highly electropositive as a result of the electron-withdrawing properties of the cyanide and ester groups; therefore, the electron pair is attracted to this region.
• the attraction alters the carbon-carbon double bond to create bonding sites of both ends of the reactant group.
• one free falling drop covers one square inch of nail area with a thickness of approximately 002′′ for best results.
• Fixture time and full cure rates are dependent upon temperature, relative humidity, thickness, and surfaces being bonded.
• Cyanoalkenoic ester adhesives are actually a solution of prepolymers of the ester in the ester monomer. Viscosity is adjusted by the degree of polymerization of the ester. Preferred viscosity of an ECA is 5 cP to 10 cP which will fill micropores from 0.002′′ to 0.005′′. Cure rate is affected by the amount of an intribitor cush as 100-2000 ppm of hydroquinone or methyl-ethyl hydroquinone (MEHQ).
• the monomer can also act as a solvent for other antifungals, such as 0.01 to 5% of preferably 0.1 to 5% undecylenic acid.
• An additional film forms such as below 10% by weight, suitably 1 to 9% of a compatible acrylic polymer which dissolves in the cynoacrylate monomer such as polymethylmethacrylate may also be present.
• the nail area infected with Onychomycosis fungi should be removed to the extent reasonably possible preferably by first mechanically grinding away the infected nail down to the level of the normal nail, and then secondly applying a small amount of the composition. Care should be taken to make certain the composition covers the infected area and also that sufficient amounts are used to saturate as well and to produce a thin coating on the infected area of nail.
• Applications can be with or without a brush, while not accidentally spilling onto the skin. Skin application can cause a bonding with keratin in skin in a matter of seconds and may be difficult to remove.
• Grinding and recoating can be repeated from at least 3 days to 6 weeks, preferably, every one to three weeks for a total of three to four months.
• the coating usually starts to lift at edges after 1 week.
• Further treatment can be assigned to the patient to do further debridment with an emery board or other tool at home and using a drop or brush application for the composition.
• composition for the treatment of onychomycosis was prepared:
• Pretreatment diagnosis clinical, KOH, PAS-D of nail clippings and cultures on Sabaround's agar.
• Negative cultures at 9 months in toenails reflects the slow growth of these nails and the layer by layer removal of infected keratin by successive debridement.
• Cyanoacrylate glues used in securing artificial nails deteriorate over time and water permeated between the natural and artificial nail allowing fungus to attack the natural nail.
• composition comprising cyanoacrylate with hydroquinone and undecylenic acid (in low concentration) combined with periodic debridement provides a less expensive, effective, safe non oral alternative for the treatment of nail fungus.
• Onychomycosis can be treated with a composition of cyanoacrylate and hydroquinone, optionally including unrdecylenic acid.
• Cyanoacrylate binds to keratin of skin and nails blocking these essential needs.
• Hydroquinone helps bleach yellow color of infected nails.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Epidemiology (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Birds (AREA)
• Communicable Diseases (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Oncology (AREA)
• Medicinal Preparation (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Agricultural Chemicals And Associated Chemicals (AREA)

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Citations (15)

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• 2006
  • 2006-02-22 US US11/816,389 patent/US20090036531A1/en not_active Abandoned
  • 2006-02-22 MX MX2007010147A patent/MX2007010147A/es not_active Application Discontinuation
  • 2006-02-22 WO PCT/US2006/006767 patent/WO2006091908A2/en active Application Filing
  • 2006-02-22 CA CA002598445A patent/CA2598445A1/en not_active Abandoned
• 2007
  • 2007-08-09 US US11/836,300 patent/US8409558B2/en not_active Expired - Fee Related

Patent Citations (15)

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