EP2222319A2 - Médicaments topiques pour le traitement antimycotique - Google Patents

Médicaments topiques pour le traitement antimycotique

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Publication number
EP2222319A2
EP2222319A2 EP08850735A EP08850735A EP2222319A2 EP 2222319 A2 EP2222319 A2 EP 2222319A2 EP 08850735 A EP08850735 A EP 08850735A EP 08850735 A EP08850735 A EP 08850735A EP 2222319 A2 EP2222319 A2 EP 2222319A2
Authority
EP
European Patent Office
Prior art keywords
group
topical
combination
dexpanthenol
antifungal
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP08850735A
Other languages
German (de)
English (en)
Inventor
Marianne Petersen-Braun
Sabine GLÄSER
Norbert-Heinz Becker
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Consumer Care AG
Original Assignee
Bayer Consumer Care AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bayer Consumer Care AG filed Critical Bayer Consumer Care AG
Priority to EP08850735A priority Critical patent/EP2222319A2/fr
Publication of EP2222319A2 publication Critical patent/EP2222319A2/fr
Withdrawn legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • 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
    • A61K31/095—Sulfur, selenium, or tellurium compounds, e.g. thiols
    • A61K31/10—Sulfides; Sulfoxides; Sulfones
    • 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
    • A61K31/16—Amides, e.g. hydroxamic 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/164—Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin

Definitions

  • the present invention relates to topical drugs with fixed drug combinations for the antifungal therapy of dermatological diseases.
  • the invention further relates to the use of the active compound combinations according to the invention for the topical treatment of mycoses of the skin or mucous membranes.
  • Mycoses are infectious diseases caused by fungi, the pathogens belonging to the group of dermatophytes (eg Trichophyton spp., Microsporum spp., Epidermophyton spp.), Yeasts (eg Candida spp., Trichosporon spp., Cryptococcus neoformans) or molds (eg Aspergillus spp., Mucor spp., Penicillium spp.).
  • the term dermatomycoses refers essentially to mycoses of the skin, skin appendages (hair, nails) and mucous membranes.
  • Common symptoms include itchy skin, burning pain, dandruff, skin maceration, erythema, rhagades, mucosal lining, knots, papules, pustules, abscesses, hair loss and pigmentation of the skin.
  • antifungal agents are available in various topically applicable dosage forms.
  • the antimycotic agents are essentially active substances from the classes of azole derivatives (in particular triazoles and imidazoles), polyenes, thiocarbamates, allylamines, morpholine derivatives and hydroxypyridones.
  • mycotic diseases of the skin or mucous membranes often occur inflammatory reactions that lead to a worsening of the symptoms. Furthermore, cracks in the skin or even open wounds may occur during the course of the disease, resulting in secondary infections, e.g. bacterial infections, are favored.
  • An anti-inflammatory (i.e., antiphlogistic) effect is not or only insufficiently present in the antifungal drugs known in the art.
  • Some antifikyotic agents from the group of azoles eg clotrimazole, bifonazole
  • Some antifikyotic agents from the group of azoles are known to have a weak or even stronger antifungal activity have an anti-inflammatory effect.
  • this "intrinsic" antiphlogistic effect only occurs in certain antifungal agents from the drug group of azoles, and since the intrinsic antiphlogistic effect may be present to varying degrees, the therapeutic utility of this intrinsic effect is only small.
  • the skin or mucous membrane areas affected by a mycosis usually already have tissue damage at the beginning of the antifungal therapy. For a successful healing process, therefore, the regeneration of the damaged tissue is of central importance. In general, after the killing of the mycotic pathogens a period of several weeks is needed until the skin structure damaged by the infection is repaired again by the process of natural regeneration. During this period, the affected skin or mucous membrane region is particularly susceptible to other infection germs (eg, superinfections or secondary infections by fungi or bacteria).
  • topical drugs used according to the prior art in the antifungal therapy are not suitable to promote skin regeneration and thereby accelerate the healing process. As a result, there is a high risk of the occurrence of secondary infections in the use of these known drugs.
  • the object underlying the present invention was to provide topically applicable drugs for antifungal therapy, which are not associated with the disadvantages mentioned above.
  • the object was to provide medicaments of the type mentioned, which are characterized by an additional anti-inflammatory (anti-inflammatory) effect and / or by a skin or mucous membrane regeneration-promoting effect.
  • this object could be achieved according to the present invention by providing a topical drug containing at least one antifungal agent and additionally at least one selected from the pantothenic acid and pantothenic acid group group selected drug, in particular dexpanthenol, in a fixed combination.
  • the topical administration of said fixed active ingredient combination not only an anti-infective effect, but also an anti-inflammatory and skin regeneration-promoting effect is achieved. This will make a - im Comparison to known antifungal agents - allows more favorable and faster healing with a reduced risk of secondary or superinfections.
  • pantothenic acid and pantothenic acid derivatives in particular dexpanthenol
  • an antifungal agent according to the present invention it is possible to synergistically enhance the intrinsic antiphlogistic action of this antifungal agent.
  • inventive antifungal drug combinations which contain one or more active ingredients from the group of azole derivatives.
  • the anti-inflammatory and synergistic enhancement of the anti-inflammatory activity of the drug combinations and drugs of the present invention can be demonstrated by known standard experimental models and methods in vitro and in vivo (e.g., transendothelial leukocyte migration test or UV erythema test). Likewise, the aforementioned improvement in skin regeneration can be detected by known in vivo test models.
  • a further advantage of the medicaments according to the invention is that the occurrence of side effects caused by the topical application of antifungal agents is suppressed or reduced. This is obviously due to the additional presence of the drug selected from the pantothenic acid and pantothenic acid derivatives group.
  • antifungal agents are for the purposes of the present invention, in principle, all pharmacological agents into consideration, which act fungistatic or fungicidal against fungal diseases.
  • these are antifungal agents which are selected from the drug classes of azole derivatives, in particular triazole and imidazole derivatives, and the allylamines, thiocarbamates, thiocarbanilates, substituted pyridones, polyene antibiotics, morpholines, hydroxypyridones and Glukansynthesehemmer.
  • a topical medicament according to the invention contains at least one antifungal active ingredient from the group of allylamines, preferably selected from the group comprising terbinafine and naftifine, in fixed combination with at least one group comprising pantothenic acid and pantothenic acid derivatives selected drug, with dexpanthenol being particularly preferred.
  • the above medicines are particularly useful in the treatment of dermatophytoses of the skin and mucous membranes.
  • a topical medicament according to the invention contains at least one antimycotic active ingredient from the group of the azole derivatives, in particular the imidazole derivatives and triazole derivatives, in a fixed combination with at least one active ingredient comprising pantothenic acid and pantothenic acid derivatives, with dexpanthenol being particularly preferred.
  • the group of azole derivatives includes in particular miconazole, miconazole nitrate, ketoconazole, fluconazole, itraconazole, bifonazole, clotrimazole, econazole, clomidazole, isoconazole, Tiabendazol, tioconazole, ketoconazole, sulconazole, oxiconazole, fenticonazole, omoconazole, sertaconazole, flutrimazole, croconazole, voriconazole and posaconazole.
  • Azole derivatives are generally characterized by a broad spectrum of activity and can be applied to dermal or mucosal mycoses by dermatophytes, yeasts and molds.
  • a topical medicament according to the invention contains at least one antifungal active ingredient from the group of thiocarbamates and thiocarbanilates, tolnaftate and tolciclate being particularly preferred.
  • a topical medicament according to the invention contains at least one antifungal active ingredient from the group of morpholines, with amorolfine being particularly preferred.
  • a topical medicament according to the invention contains at least one antifungal active ingredient from the group of glucan synthesis inhibitors (echinocandins), with caspofungin being particularly preferred.
  • a topical medicament according to the invention contains at least one antifungal active ingredient from the group of polyene antibiotics, preferably from the group comprising nystatin, natamycin, amphotericin B, hachimycin and pecilocin. Preference is further macrolide antibiotics with fungicidal or fungistatic action, such as Mepartricin, and other antimycotic antibiotics of bacterial origin, such as pyrrolitrite or griseofulvin; as well as inhibitors of DNA, RNA or protein synthesis, such as flucytosine.
  • a topical medicament according to the invention contains at least one antimycotic active ingredient from the group of hydroxypyridones, with ciclopirox and ciclopiroxolamine being particularly preferred.
  • antifungal agents are also all other antimicrobial or antiseptic substances with fungistatic or fungicidal effect into consideration, which may belong to different classes. These include in particular the following active ingredients: quinoline derivatives, in particular diiodo-hydroxyquinoline, clioquinol, chlorquinaldol, broxyquinoline, oxyquinoline; antiseptic agents such as dequalinium, clodantoin, bromochlorosalicylanilide (Multifungin), bromsalicylisopropylamide, methylrosaniline, tribromometacresol, policicules, benzalkonium chloride, povidone-iodine, hexetidine, octenidine, polynoxylin, 2- (4-chlorophenoxy) -ethanol, chlorphenesin, ticlaton, sulbentin, fenticlor, Bithionol, ethyl hydroxybenzoate, haloprogin, salicylic acid
  • a pharmaceutical composition of the invention may contain one, two or more antifungal agents in fixed combination with a drug selected from the group consisting of pantothenic acid and pantothenic acid derivatives, preferably dexpanthenol.
  • the group of pantothenic acid derivatives comprises in particular dexpanthenol, DL-panthenol, salts of pantothenic acid (eg Na-pantothenate, Ca-pantothenate), esters of pantothenic acid (eg ethyl, methyl ester), panthenol-ether (eg ethyl or methyl ether), panthenol- Thioether and Panthenyltriacetat includes.
  • a topical medicament according to the invention contains one of the following active ingredient combinations:
  • one or more antifungal agents from the group of azoles preferably from the group comprising clotrimazole, bifonazole, fluconazole, miconazole, econazole, tioconazole, fenticonazole, oxiconazole and ketoconazole, in combination with dexpanthenol;
  • amorolfol in combination with dexpanthenol d) amorolfol in combination with dexpanthenol; e) caspofiingin in combination with dexpanthenol;
  • one or more antifungal agents from the mepartricin, pyrrolnitrin, griseofulvin and flucytosine group in combination with dexpanthenol g) one or more antifungal agents from the mepartricin, pyrrolnitrin, griseofulvin and flucytosine group in combination with dexpanthenol.
  • the medicaments according to the invention additionally comprise at least one further active substance, which is preferably selected from the group comprising topical antihistamines, topical glucocorticoids, local anesthetics and antipruritinosa.
  • the active substance class of the topical antihistamines comprises in particular the following active ingredients: ketotifen, thonzylamine, mepyramine, thenalidine, tripelennamine, chloropyramine, promethazine, tolpropamine, dimetindene, clemastine, bamipine,
  • Particularly preferred antihistamines are: bamipin, clemastine, chlorphenoxamine, azelastine, terfenadine, loratadine.
  • the class of topical glucocorticoids includes in particular hydrocortisone, hydrocortisone acetate, hydrocortisone butyrate, methylprednisolone, methylprednisolone acetate, clobetasone butyrate, fluocinolone acetonide, fluocortolone, prednicarbate, beclomethasone dipropionate, betamethasone 17-valerate, betamethasone 17,21 dipropionate, budesonide, desonide,
  • the class of drugs of local anesthetics includes in particular lidocaine, tetracaine and benzocaine.
  • the drug class of Antipruritinosa includes in particular crotamiton, bufexamac, isoprenaline, camphor, tar preparations, topical antihistamines, Avenathramid and its synthetic or natural derivatives, glycyrrhetinic acid, glycyrrhizinic acid or its potassium salts and tannins.
  • the medicaments according to the invention additionally contain at least one extract from the plant Centella asiatica, preferably a titrated extract from Centella asiatica.
  • Extracts of Centella asiatica preferably contain active ingredients of the group consisting of the acid of asiatic acid, asiaticoside, madecassid acid, madecassoside and terminoloside and can be obtained as described in WO2004 / 062678.
  • the medicaments according to the invention contain the extracts from the plant Centella asiatica, preferably a titered extract from Centella asiatica, particularly preferably the active substances from the group comprising asiatic acid, asiaticoside, madecassid acid, madecassoside and terminoloside in a content of 0.5 to 1.5%. % By weight based on the total weight of the drug.
  • the extract of Centella asiatica preferably contains the active ingredients madecassoside and / or terminoloside and / or asiaticoside in a content of more than 75% by weight, preferably more than 85% by weight, based on the total weight of the extract.
  • the extract of Centella asiatica particularly preferably contains the active ingredients madecassoside and / or terminoloside in a content of more than 75% by weight, preferably more than 85% by weight, particularly preferably more than 95% by weight, based on the total weight of the extract.
  • the medicaments of the invention may contain vitamins and / or minerals.
  • Vitamins include, for example, vitamin A, beta-carotene, vitamin C (ascorbic acid), vitamin D3 (cholecalcipherol), vitamin E (tocopherol acetate), vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinamide), vitamin B6 (pyridoxine), Folic acid, vitamin B12 (cyanocobalamin), vitamin K and biotin.
  • Minerals include, for example, iron salts, copper salts, calcium salts such as calcium carbonate, calcium phosphate, calcium glycerophosphate; Magnesium salts such as magnesium phosphates, magnesium sulfate (dihydrate) or magnesium oxide; Zinc salts such as zinc citrate; Strontium salts such as strontium ranelate, selenium or its salts such as sodium selenate; potassium iodide; Magansalts such as manganese sulfate; Molybdenum salts such as sodium molybdate; Chromium salts such as chromium chloride; Sodium chloride or potassium chloride. Alkaline earth metal salts can be added against itching, such.
  • the salts may be, for example, carbonates, bicarbonates, sulfates, glycerophosphates, borates, chlorides, nitrates, acetates, hydroxides and persulfates and salts of ⁇ -hydroxy acids (citrates, tartrates, lactates, malates) or fruit acids, salts of amino acids (aspartate , Arginate, glycocholate, fumarate) or salts of fatty acids (palmitate, oleate, caseinate, behenate).
  • the salt is, for example, calcium nitrate, magnesium nitrate, calcium borate, magnesium borate, calcium chloride, magnesium chloride, calcium sulfate, magnesium sulfate, calcium acetate or Magnesium acetate selected.
  • the salt is a magnesium salt or even better a strontium salt and in particular a chloride or nitrate.
  • Active ingredient groups are used in the context of the invention.
  • the active substances according to the invention can also be used in the form of their pharmaceutically acceptable salts.
  • Suitable salts are, for example, the following:
  • Hydrochloride hydrobromide, sodium salts, phosphate, nitrate, sulfate, acetate, fumarate, citrate, propionate, oxalate, succinate, lactate, butyrate, methanesulfonate, aspartate, decanoate, maleate, tartrate,
  • the medicaments according to the invention contain a combination of the named active ingredients in the form of a "fixed combination"; This means that all active substances which form the respective active ingredient combination are present together in a dosage form and are administered together.
  • the active substances can be present in the medicaments in particular in particulate, dispersed, dissolved, suspended or emulsified form.
  • the total active ingredient content of the medicaments according to the invention is preferably in the range of 0.05 to 90 wt .-%, preferably in the range of 0.1 to 50 wt .-%, particularly preferably 0.5 to 20 wt .-%, each based on the total weight of the drug.
  • the proportion of active ingredient is determined in a manner known to the person skilled in the art, depending on the respectively selected dosage form, of the selected active ingredient (s) and the dose suitable for the respective therapeutic purpose.
  • the therapeutically suitable dosages of the individual active ingredients are known to the person skilled in the art.
  • the daily dose is in the range of about 5 to 50 mg.
  • the proportion of the antimycotic active ingredient (s) is preferably 0.01 to 85 wt .-%, preferably 0.05 to 45 wt .-%, particularly preferably 0.1 to 15 wt .-%, each based on the total Drug.
  • pantothenic acid derivative preferably dexpanthenol
  • pantothenic acid derivative preferably dexpanthenol
  • the dexpanthenol content is preferably from 0.01 to 85% by weight, in particular from 0.05 to 45% by weight, particularly preferably from 0.1 to 15% by weight, in each case based on the total drug.
  • the weight ratio of dexpanthenol (or the pantothenic acid derivative or pantothenic acid) to said at least one antifungal active ingredient is in the range from 1: 100 to 100: 1, preferably in the range from 50: 1 to 1 : 50, more preferably in the range of 1:10 to 10: 1.
  • the proportion of said at least one further active ingredient is preferably from the group comprising topical antihistamines, topical glucocorticoids, local anesthetics and antipruriticosa, is preferably from 0.05 to 50% by weight, in particular from 0.1 to 20% by weight, in each case based on the drug.
  • the medicaments according to the invention additionally comprise one or more dermatological and / or cosmetic ingredients.
  • these substances are preferably selected from the group consisting of zinc containing agents (eg, zinc oxide, zinc sulfate), silicone-containing agents (eg, dimethicone, phenylmethylpolysiloxane, polysiloxane), petrolatum, fatty agents (eg, linoleic acid, ethyl linolate, paraffin, vaseline), urea-containing agents (eg, urea , Carbamide peroxide, allantoin), salicylic acid-containing preparations (eg acetylsalicylic acid, salicylic acid, bromosalicylic acid), skin protection agents (eg guaiaculas, sulfur-containing agents, glycerol, glucose, thymol), emollients (eg mineral oils or paraffins in the form of oil-in-water emulsions), Moisturi
  • the medicaments according to the invention are formulated as topical medicaments which are particularly suitable for use on the skin, on the hairy skin, on mucous membranes (for example of the oral, nose, pharynx or vagina) and on the skin appendages (eg finger or toenails) .
  • the medicaments according to the invention can be formulated as solid, semi-solid or liquid dosage forms, preferably as powder, powder, granules, tablet, lozenge, lozenge, suppository, patch or patch, solution, foam, gel, lotion, emulsion, cream, ointment, paste, Oil, shampoo, nail polish, film, aerosol, dust aerosol or spray.
  • ⁇ for the therapeutic treatment of mycoses of the skin and skin appendages are preferably the following dosage forms into consideration: powder, powder, granules, patch or patch, solution, foam, gel, lotion, emulsion, cream, ointment, paste, oil, shampoo, nail polish, film , Aerosol, dust aerosol or spray.
  • ⁇ dosage forms into consideration: powder, powder, granules, tablet, lozenge, lozenge, suppositories, patch or patch, solution, foam, gel, lotion, emulsion, suspension, cream, ointment, paste , Oil, film, aerosol, dust aerosol or spray.
  • Vaginal mycoses - are preferably the following dosage forms into consideration: powder, powder, solution, foam, gel, lotion, emulsion, cream, ointment, paste, oil, aerosol, dust aerosol, spray, vaginal tablets, vaginal suppositories, vaginal capsules, vaginal gel, vaginal suppositories.
  • auxiliaries are, for example, the following: particulate carriers (for example talc, zinc oxide, starch, starch derivatives, kieselguhr); gel-forming substances (e.g., gelatin, tragacanth, cellulose derivatives, alginates, polyacrylic acid); Humectants (e.g., urea, glycerin, propylene glycol), pressure-sensitive adhesives (e.g., polyacrylates, as well as tackifier resins); Ointment bases (e.g., vaselin, fats, cellulose derivatives, polyacrylic acid, polyethylene glycols); Emulsifiers (e.g., wool wax, sorbitan esters, monoglycerides); Preservatives (e.g., benzalkonium chloride), antioxidants (e.g., butylhydroxyanisole), thickening agents (e.g.
  • particulate carriers for example talc, zinc oxide, starch, starch derivatives, kieselg
  • Binders for example polyvinylpyrrolidone, starch, hydroxypropylmethylcellulose, polyethylene glycols), fillers (eg microcrystalline cellulose, sorbitol), dyes, flavorings, sweeteners (eg sorbitol, aspartame); Solvents (eg water, ethanol, ethanol-water mixtures); Solubilizers (eg glycerol, propylene glycol); Skin penetration enhancers (eg, propylene glycol); Plasticizers (eg sorbitol, glycerol, phthalic acid esters); Wetting agents (eg, sodium lauryl sulfate, polysorbates); synthetic and natural oils (eg medium chain triglycerides); Propellants for aerosol or foam sprays (eg norflurane, cryoflurane, dichlorofluoromethane, trichlorofluoromethane, propane, butane, isobutan
  • the invention further relates to the use of a combination of active substances which, as described in the preceding paragraphs, contains at least one antimycotic active ingredient and at least one active ingredient selected from the pantothenic acid and pantothenic acid derivatives, in particular dexpanthenol, for the topical treatment of mycoses of the skin (including subcutaneous mycoses) and cutaneous appendages or mycoses of the mucous membranes.
  • mycoses essentially includes dermatophytoses, mold mycoses and yeast mycoses.
  • the treatment is generally carried out in such a way that the antimycotic agents contained in the drug combination as a mixture of active ingredients, optionally together with one or more excipients, are applied locally to the diseased body sites.
  • a suitable antifungal agent or a combination of antifungal agents generally depends on the type of mycosis to be treated, the type of pathogen involved and the spectrum of action of the active ingredient.
  • the spectrum of action of the various antimycotic agents are known in the art.
  • the drug combinations of the invention and medicaments containing them can be used to treat mycoses caused by dermatophytes, molds or yeasts.
  • the invention further relates to the use of a fixed combination of active ingredients which, as described above, contains at least one antimycotic active ingredient and at least one active ingredient selected from the pantothenic acid and pantothenic acid derivatives, in particular dexpanthenol, for the preventive topical treatment of mycoses of the skin and skin appendages or mycoses mucous membranes.
  • Preventive treatment is particularly contemplated in those patients at high risk for fungal infections, e.g. in immunocompromised patients or diabetics.
  • the invention further extends to the use of a combination of active substances according to the invention for the reinfection prophylaxis against mycosis of the skin and skin appendages or mycoses of the mucous membranes.
  • Such treatment is particularly useful in people who suffer from common recurrent fungal diseases such as athlete's foot, genital mycoses, especially vaginal mycoses, or bran fungus (pityriasis versicolor).
  • active compound combinations according to the invention can be used for the topical treatment of dermal or mucosal mycoses which occur during or after radiation or chemotherapy, during or after an immunosuppressive therapy, during or following systemic antibiotic therapy or skin or mucosal damage caused by chemical or physical agents (eg, injuries, burns).
  • active ingredient combinations and topical medicaments according to the invention can advantageously be used to improve the active ingredient combinations and topical medicaments according to the invention.
  • the active compound combinations and medicaments according to the invention are particularly suitable for the topical treatment of inflammatory or eczematous dermatomycoses.
  • the active compound combinations and medicaments according to the invention can preferably be used for the topical treatment of the following mycotic disorders:
  • Tinea especially tinea pedis, tinea manuum, tinea capitis, tinea barbae, tinea favosa, tinea corporum, tinea faciei.
  • these are infections caused by Epidermophyton, Microsporum and Trichophyton species.
  • Pityriasis in particular pityriasis versicolor (bran fungus);
  • subcutaneous tissue subcutaneous mucous
  • the active compound combinations according to the invention and topical medicaments are thus suitable for the treatment of cutaneous or mucosal mycoses of very different etiology and localization.
  • the drug combinations and drugs of the invention are used in the field of human medicine, i. for the treatment of persons suffering from dermatomycosis or mucosal mycosis.
  • the invention also extends to the use of the active ingredient combinations and veterinary medicaments according to the invention, i. for the treatment of animals, in particular livestock or domestic animals suffering from dermatomycosis or mucosal mycosis.
  • the invention further encompasses a method for the therapeutic treatment of a person suffering from a mycosis of the skin, appendages or mucous membrane, and who requires a therapeutic treatment.
  • a therapeutic method has at least one treatment step in which a combination of active substances according to the invention in a therapeutically effective dose (or a erf ⁇ ndungsdorfes drug containing such drug combination) administered topically, i. is applied to the areas affected by the mycosis body regions.
  • Particularly suitable body regions to be treated are the following: skin, scalp, hands, fingers, fingernails, feet, toes, toenails, mucous membranes, lips, oral cavity, tongue, gums, skin folds, body folds, inguinal region, genital area, anal area, eyelid, conjunctiva.
  • the invention also extends to the use of a fixed active ingredient combination, as described above, for the preparation of topical medicaments for the therapeutic treatment of mycoses of the skin, mucous membranes or skin appendages in humans or in animals.
  • a fixed active ingredient combination as described above, for the preparation of topical medicaments for the therapeutic treatment of mycoses of the skin, mucous membranes or skin appendages in humans or in animals.
  • the cream is used for the topical treatment of dermatomycoses caused by dermatophytes, yeasts, molds or other fungi. It is particularly suitable for the treatment of tinea pedis, tinea manuum or pityriasis versicolor.
  • the cream is applied once a day to the diseased skin surfaces and rubbed.
  • the gel is used for the topical treatment of dermatomycoses caused by dermatophytes, yeasts, molds or other fungi. It is particularly suitable for the treatment of fungal diseases of the feet and hands (tinea pedum, tinea manuum), fungal skin diseases and skin folds (tinea corporis, tinea inguinalis), Pityriasis versicolor (bran fungus), as well as for the treatment of superficial candidoses.
  • the gel is applied once a day to the diseased skin surfaces and rubbed.
  • Excipients fumed silica, crospovidone, calcium lactate pentahydrate, lactose monohydrate, magnesium stearate, corn starch, hypromellose, microcrystalline cellulose and lactic acid.
  • the tablets are used to treat vaginal yeast infections (dosage: 1 tablet daily).
  • dexpanthenol in a cream preparation of benzyl alcohol, polyoxyethylene (20) sorbitan monostearate, stearyl alcohol, cetyl alcohol, cetyl palmitate, sorbitan stearate, isopropyl myristate, sodium hydroxide, ethanol and purified water.
  • the cream is applied once a day to the diseased skin and rubbed in lightly.
  • the ointment is used to treat Candida infections of the skin, mucous membranes and finger or toenails.
  • the ointment is applied 1 to several times daily to the affected body regions.
  • the cream can be used to treat inflammatory dermatomycoses caused by dermatophytes, yeasts (especially Candida), molds or other fungi. It is also useful in the treatment of diaper dermatitis, vulvitis, balanitis and intertrigo, if these infections involve Candida yeasts.
  • the ointment is applied two to several times daily to the affected body regions.
  • the solution can be used in particular for the treatment of dermatomycoses and onychomycoses caused by dermatophytes, yeasts or molds.

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  • Health & Medical Sciences (AREA)
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Abstract

L'invention concerne des médicaments topiques pour le traitement antimycotique qui contiennent, en association fixe : au moins un principe actif antimycotique; et au moins un principe actif sélectionné dans le groupe comprenant l'acide pantothénique et des dérivés de l'acide pantothénique.
EP08850735A 2007-11-17 2008-11-15 Médicaments topiques pour le traitement antimycotique Withdrawn EP2222319A2 (fr)

Priority Applications (1)

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EP08850735A EP2222319A2 (fr) 2007-11-17 2008-11-15 Médicaments topiques pour le traitement antimycotique

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EP07022353 2007-11-17
EP08850735A EP2222319A2 (fr) 2007-11-17 2008-11-15 Médicaments topiques pour le traitement antimycotique
PCT/EP2008/009686 WO2009062746A2 (fr) 2007-11-17 2008-11-15 Médicaments topiques pour le traitement antimycotique

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EP2222319A2 true EP2222319A2 (fr) 2010-09-01

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AU (1) AU2008323165A1 (fr)
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EP2166840B1 (fr) 2007-06-20 2017-01-11 The Trustees of Columbia University in the City of New York Surfaces résistantes à la formation de biofilm
US9981069B2 (en) 2007-06-20 2018-05-29 The Trustees Of Columbia University In The City Of New York Bio-film resistant surfaces
US9687429B2 (en) 2007-06-20 2017-06-27 The Trustees Of Columbia University In The City Of New York Antimicrobial compositions containing low concentrations of botanicals
US9511040B2 (en) 2007-06-20 2016-12-06 The Trustees Of Columbia University In The City Of New York Skin and surface disinfectant compositions containing botanicals
JP2012532141A (ja) * 2009-06-30 2012-12-13 ザ トラスティース オブ コロンビア ユニバーシティ イン ザ シティ オブ ニューヨーク 植物性成分を含有する抗微生物／防腐組成物
IT1400726B1 (it) * 2009-07-24 2013-07-02 Vi Rus S R L Composizione di un'emulsione ad uso topico a base di clotrimazolo, clorexidina digluconato,acido salicilico,allantoina,pantenolo,zinco,acido glicirretico,olio di mandorle dolci,olio di riso,mentile lattato indicata nel trattamento delle infezioni micotiche della cute e dei suoi annessi.
WO2011061155A1 (fr) * 2009-11-17 2011-05-26 Bayer Consumer Care Ag Formulations antifongiques et leur utilisation
GB201107176D0 (en) * 2011-04-28 2011-06-15 Cxr Biosciences Ltd Pyrrolnitrin derivatives
ES2762405T3 (es) 2011-11-03 2020-05-25 Univ Columbia Composición con actividad antimicrobiana sostenida
US9968101B2 (en) 2011-11-03 2018-05-15 The Trustees Of Columbia University In The City Of New York Botanical antimicrobial compositions
WO2013086094A1 (fr) 2011-12-06 2013-06-13 The Trustees Of Columbia University In The City Of New York Composition d'agent de conservation naturelle à large spectre
EP2906946A1 (fr) 2012-10-09 2015-08-19 The Procter & Gamble Company Procédé d'identification ou d'évaluation de principes actifs bénéfiques, et compositions contenant ces derniers
EP2906197A1 (fr) 2012-10-09 2015-08-19 The Procter & Gamble Company Procédé d'identification de combinaisons cosmétiques synergiques
US9138393B2 (en) 2013-02-08 2015-09-22 The Procter & Gamble Company Cosmetic compositions containing substituted azole and methods for improving the appearance of aging skin
US9144538B2 (en) 2013-02-08 2015-09-29 The Procter & Gamble Company Cosmetic compositions containing substituted azole and methods for alleviating the signs of photoaged skin
CN108472272A (zh) * 2015-08-17 2018-08-31 俄亥俄州国家创新基金会 用于ar-12的增强的透甲递送的方法和组合物
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KR102217617B1 (ko) * 2020-08-14 2021-02-19 비엘엔에이치 주식회사 백선의 예방 또는 치료용 약학적 조성물
CN113440483B (zh) * 2021-06-30 2023-04-07 佛山市南海东方澳龙制药有限公司 一种犬用盐酸特比萘芬喷剂及其制备方法

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WO2009062746A2 (fr) 2009-05-22
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WO2009062746A3 (fr) 2009-08-13
CA2705815A1 (fr) 2009-05-22

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