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NO813931L - ANTIMYCOTIC AGENT WITH HIGH EFFICIENT SUBSTANCE RELEASE IN THE FORM OF ELASTIC LIQUID PLASTERS - Google Patents

ANTIMYCOTIC AGENT WITH HIGH EFFICIENT SUBSTANCE RELEASE IN THE FORM OF ELASTIC LIQUID PLASTERS

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Publication number
NO813931L
NO813931L NO813931A NO813931A NO813931L NO 813931 L NO813931 L NO 813931L NO 813931 A NO813931 A NO 813931A NO 813931 A NO813931 A NO 813931A NO 813931 L NO813931 L NO 813931L
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Prior art keywords
antimycotic agent
agent according
effect
high efficient
active substance
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NO813931A
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Norwegian (no)
Inventor
Miklos Von Bittera
Karl Heinz Buechel
Manfred Plempel
Erik Regel
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Bayer Ag
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Publication of NO813931L publication Critical patent/NO813931L/en

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    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • 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
    • A61P31/04—Antibacterial agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Dispersion Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Materials For Medical Uses (AREA)
  • Body Structure For Vehicles (AREA)
  • Catching Or Destruction (AREA)
  • Stereophonic Arrangements (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Antimykotisk middel med hyere frigjøring av de virksomme stoffer og inneholdende azolderivater og vanlige formuleringshjelpestoffer, idet de inneholder 2 - 10% spredemidler, 1-8% oppløsningsformidler og som filmdanner celluloseetere. Det antimykotiske middel kan fore-ligge i form av oppløsning eller spray. Ved hjelp av det nye middel oppnås en hyere biodisponerbarhet av det virksomme stoff og derved muliggjøres en korttidsterapi.Antifungal agent with higher release of the active substances and containing azole derivatives and common formulation auxiliaries, containing 2 - 10% dispersants, 1-8% solvents and film-forming cellulose ethers. The antifungal agent may be in the form of a solution or spray. With the help of the new agent, a higher biodiscibility of the active substance is achieved and thereby a short-term therapy is made possible.

Description

Oppfinnelsen vedrører nye formuleringer av de kjente antimykotiske azolderivater som har en depot-virkning på tross av filmdannelse og en høyere biodisponerbarhet av de virksomme stoffer og derved muliggjør en korttidsterapi. The invention relates to new formulations of the known antifungal azole derivatives which have a depot effect despite film formation and a higher bioavailability of the active substances and thereby enable a short-term therapy.

For behandling av mykoser hos menneske fremfor alt hudmykoser er det allerede blitt kjent tilberedninger av antimykotiske derivater. Med disse tilberedninger krevdes for en fullstendig sanering over 21 dagers terapitid. Preparations of antifungal derivatives are already known for the treatment of mycoses in humans, above all skin mycoses. With these preparations, a complete remediation is required over 21 days of therapy.

For å komme til en nedsettelse av terapivarigheten krever man spesielt for eliminering av kimene respektiv for å oppnå en mykologisk sanering en viss depot-virkning og en høyere biodisponerbarhet av de virksomme stoffer. Hertil er de kjente formuleringer bare begrenset egnet, fordi det fra det tilstedeværende virksomme stofftilbud bare oppløser seg en liten del i væskevolumene på infeksjonsstedet. Når man nu uten ytterligere økning av den virksomme stoffkonsentra-sjon vil oppnå en nedsettelse av terapivarigheten, f.eks. til 1 dag ved en gangs applikasjon må man sørge for en optimal biodisponerbarhet av det virksomme stoff. In order to achieve a reduction in the duration of therapy, a certain depot effect and a higher bioavailability of the active substances are required especially for the elimination of the germs respectively to achieve a mycological remediation. The known formulations are only suitable to a limited extent for this, because only a small part of the active substance present dissolves in the liquid volumes at the site of infection. When you now want to achieve a reduction in the duration of therapy without further increasing the active substance concentration, e.g. to 1 day with a single application, one must ensure optimal bioavailability of the active substance.

Det er nu funnet at slike formuleringer av antimykotisk virksomme stoffer som inneholder 2-10% spredemiddel, 1-8% oppløsningsformidler og som filmdanner en celluloseeter, spesielt hydroksypropylcellulose som såvel er oppløselig i vann som også i organiske oppløsningsmidler og dessuten inneholder de vanlige formuleringshjelpestoffer, muliggjør en optimal frigjøring av det virksomme stoff og dermed en til en dag forkortet terapivarighet ved oppnåelse av høye konsentrasjoner av det virksomme stoff. Denne effekt oppnås ved at virkningen av de i formuleringene inneholdte virksomme stoffer økes ved spredeoljer og oppløsningsfor-midlere og adhererende filmdanner-tilsetning og derved kan den virksomme stoff-frigjøring økes inntil 10 ganger. It has now been found that such formulations of antifungally active substances which contain 2-10% dispersing agent, 1-8% solubilizer and which film-forms a cellulose ether, especially hydroxypropyl cellulose which is soluble in water as well as in organic solvents and also contains the usual formulation aids, enables an optimal release of the active substance and thus shortens the duration of therapy by one to one day when high concentrations of the active substance are achieved. This effect is achieved by the fact that the effect of the active substances contained in the formulations is increased by the addition of dispersing oils and dissolving agents and adhering film formers, and thereby the active substance release can be increased up to 10 times.

De ifølge oppfinnelsen elastiske flytende plaster-formuler inger er et nytt applikasjonsprinsipp til dermal behandling av mykoser som ved siden av en meget god virkning ved lukning av infeksjonsstedet danner en infeksjonsbeskyttelse for om-givelsen. Spesielt godt egnet er formuleringene ifølge oppfinnelsen for behandling av neglmykoser. The elastic liquid patch formulas according to the invention are a new application principle for the dermal treatment of mycoses which, in addition to a very good effect when closing the site of infection, forms an infection protection for the environment. The formulations according to the invention are particularly suitable for the treatment of nail mycoses.

Formuleringen ifølge oppfinnelsen kan såvel være oppløsninger som også sprays. The formulation according to the invention can be both solutions and sprays.

Virksomme stoffer som kan formuleres på denne måte er alle antimykotisk virksomme derivater, spesielt imidazol- og triazolderivater. De er tilstede i midlene ifølge oppfinnelsen i mengder på 0,05-1%, fortrinnsvis 0,1-1%. Active substances that can be formulated in this way are all antifungally active derivatives, especially imidazole and triazole derivatives. They are present in the agents according to the invention in amounts of 0.05-1%, preferably 0.1-1%.

Eksempelvis skal det nevnes forbindelsene med følgende formler: For example, the compounds with the following formulas should be mentioned:

Tallrike ytterligere antimykotisk virksomme azolderivater er kjent fra DE-OS 24 30 039. De kan likeledes tjene som virksomme stoffer i midlene ifølge oppfinnelsen. Numerous further antifungally active azole derivatives are known from DE-OS 24 30 039. They can likewise serve as active substances in the agents according to the invention.

Med spredemidler forstås oljeaktige væsker som fordeler seg spesielt godt på huden (R.Keymer, Pharm.Ind.32 (1970), side 77-81). For midlene ifølge oppfinnelsen egner det seg som spredemidler spesielt følgende: Dispersants mean oily liquids which distribute particularly well on the skin (R.Keymer, Pharm.Ind.32 (1970), pages 77-81). For the agents according to the invention, the following are particularly suitable as dispersants:

Silikonoljer av forskjellig viskositet.Silicone oils of different viscosities.

Fettsyreestere, som etylstearat, di-n-butyl-adipat, laurin-syreheksylester, dipropylen-glykolpelargonat, estere av en forgrenet fettsyre av midlere kjedelengde med mettede fettalkoholer c±£~ ciq' isopropylmyristat, isopropylpalmitat, capryl/caprinsyreester av umettede fettalkoholer av kjedelengde ci2~ ClS'<i>soProPYlstearat'oljesyreoleylester, olje-syredecylester, etyloleat, melkesyreetylester, voksaktige fettsyreestere som kunstig andegumkjertelfett, bibutylftalat, adipinsyrediisopropylester, til sistnevnte beslektede ester-blandinger og lignende. Fatty acid esters, such as ethyl stearate, di-n-butyl adipate, lauric acid hexyl ester, dipropylene glycol pelargonate, esters of a branched fatty acid of medium chain length with saturated fatty alcohols c±£~ ciq' isopropyl myristate, isopropyl palmitate, caprylic/capric acid esters of unsaturated fatty alcohols of chain length ci2~ ClS'<i>soProPYlstearate'oleic acid oleyl ester, oleic acid decyl ester, ethyl oleate, lactic acid ethyl ester, waxy fatty acid esters such as artificial duck gum fat, bibutyl phthalate, adipic acid diisopropyl ester, to the latter related ester mixtures and the like.

Triglycerider, som capryl/caprinsyretriglycerid, triglycetid-blandinger med plantefettsyrer av kjedelengder C0-C,~eller andre spesielt utvalgte naturlige fettsyrer, partialglycerin-blandinger av mettede eller umettede eventuelt også hydroksyl-gruppeholdige fettsyrer, monoglycerider av C0/C,_-fettsyrer Triglycerides, such as caprylic/capric acid triglyceride, triglyceride mixtures with plant fatty acids of chain lengths C0-C,~ or other specially selected natural fatty acids, partialglycerin mixtures of saturated or unsaturated fatty acids possibly also containing hydroxyl groups, monoglycerides of C0/C,_ fatty acids

o lu oh lol

og lignende.and such.

Fettalkoholer, som isotridecylalkohol, cetylstearylalkohol, oleylalkohol. Fatty alcohols, such as isotridecyl alcohol, cetylstearyl alcohol, oleyl alcohol.

Fettsyrer, som f.eks. oljesyre.Fatty acids, such as oleic acid.

Spesielt godt egnede spredende oljer er følgende: isopropylmyristat, isopropylpalmitat, isopropylstearat, capryl/caprin- syreestere av umettede fettalkoholer av kjedelengder C-,~-C,0, Particularly suitable spreading oils are the following: isopropyl myristate, isopropyl palmitate, isopropyl stearate, caprylic/capric acid esters of unsaturated fatty alcohols of chain lengths C-,~-C,0,

LZ. lo voksaktige fettsyreestere som kunstig andegumpkjertelfett, silikonolje, isopropylmyristat-isopropylpalmitat-isopropyl-stearatblanding og kokosfettsyreisopropylester. LZ. waxy fatty acid esters such as artificial duck fat, silicone oil, isopropyl myristate-isopropyl palmitate-isopropyl stearate blend, and coconut fatty acid isopropyl ester.

Som oppløsningsformidlere egner det seg for midlene ifølge oppfinnelsen fremfor alt: Benzylalkohol, 2-octyl-dodecanol, polyetylenglykoler,ftalater, adipater, propylenglykol, glycerol, di- og tripropylenglykol, vokser etc, og andre i kosmetikken anvendte tilsetnings-stoffer • As solubilizers, the agents according to the invention are suitable above all: Benzyl alcohol, 2-octyl-dodecanol, polyethylene glycols, phthalates, adipates, propylene glycol, glycerol, di- and tripropylene glycol, waxes, etc., and other additives used in cosmetics •

Som gel- og filmdannere kommer det på tale cellyloseetere som vel kan oppløses eller respektiv svelle seg i vann som også As gel and film formers, we are talking about cellulose ethers which can well dissolve or respectively swell in water which also

i organiske oppløsningsmidler og etter tørkningen danner en filmtype. in organic solvents and after drying forms a film type.

Spesielt egnet er hydroksypropylcellulose.Hydroxypropyl cellulose is particularly suitable.

Ytterligere egnede celluloseetere er f.eks. metylcellulose, etylcellulose samt oppløselige stivelser. Further suitable cellulose ethers are e.g. methyl cellulose, ethyl cellulose and soluble starches.

Som oppløsningsmidler er egnet vann også alle med vann blandbare oppløsningsmidler. I betraktning kommer f.eks. alkanoler som etanol og isopropylalkohol, propylenglykol, metylcellulosesolv, cellosolv, estere, morfoliner, dioksan, dimetylsulfoksyd, dimetylformamid, tetrahydrofuran, cyklo-heksanon etc. Suitable solvents are water and all water-miscible solvents. Taking into account e.g. alkanols such as ethanol and isopropyl alcohol, propylene glycol, methylcellulose solv, cellosolv, esters, morpholines, dioxane, dimethylsulfoxide, dimethylformamide, tetrahydrofuran, cyclohexanone etc.

Det kan ved fremstillingen av formuleringen ifølge oppfinnelsen anvendes et eller flere oppløsningsmidler. In the preparation of the formulation according to the invention, one or more solvents may be used.

Ved forsøkene til å fastslå en optimal formulering kan det bl.a. anvendes følgende hjelpestoffer: Glycerol, tyktflytende parafin, tyntflytende parafin, tri-etanolamin. collagen, allantoin, novantisolsyre, parfymeolje. In the attempts to determine an optimal formulation, it can i.a. the following excipients are used: Glycerol, viscous paraffin, thin paraffin, tri-ethanolamine. collagen, allantoin, novantisolic acid, perfume oil.

Som ytterligere hjelpemidler er det egnet:As additional aids, the following are suitable:

a. Stoffer som f.eks. kan stabilisere en suspensjon,a. Substances such as can stabilize a suspension,

f.eks. kolloidal kiselsyre, montmorillonitter o.l.e.g. colloidal silicic acid, montmorillonites etc.

b. Tensider (omfattende emulgatorer og fuktemidler),b. Surfactants (including emulsifiers and wetting agents),

f.eks.e.g.

1. anionaktive, som Na-laurylsulfat, fettalkoholetersulfat, mono/dialkylpolyglykoleterortofosforsyreester-mono-etanolaminsalt; 2. kationaktive, som cetyltrimetylammoniumklorid; 3. amf olyttiske , som di-Na-N-lauryl-(3-ininodipropionat eller lecitin; 4. ikke ionogene, f.eks. polyoksyetilert rizinusolje, polyoksyetilert sorbitan-monooleat, sorbitan-monostearat, cetylalkohol, glycerol-monostearat, polyoksyetylenstearat, alkylfenolpolyglykoleter. c. Stabilisatorer for å hindre den ved noen viksomme stoffer inntredende kjemiske avbygning som anti-oksydanter, f.eks. tocoferoler, butylhydroksyanisol. d. Surt innstilte vandige oppløsninger kan stabiliseres ved tilsetningen av i kosmetikk vanlige konserverings-midler, f.eks. p-hydroksybenzosyreester. 1. anionic, such as Na-lauryl sulfate, fatty alcohol ether sulfate, mono/dialkyl polyglycol ether orthophosphoric acid ester mono-ethanolamine salt; 2. cation active, such as cetyltrimethylammonium chloride; 3. ampholytic, such as di-Na-N-lauryl-(3-ininodipropionate or lecithin; 4. non-ionic, e.g. polyoxyethylated castor oil, polyoxyethylated sorbitan monooleate, sorbitan monostearate, cetyl alcohol, glycerol monostearate, polyoxyethylene stearate, alkylphenol polyglycol ether. c. Stabilizers to prevent the chemical degradation that occurs with some volatile substances such as antioxidants, e.g. tocopherols, butylhydroxyanisole. d. Acidic aqueous solutions can be stabilized by the addition of preservatives common in cosmetics, e.g. p-Hydroxybenzoic acid ester.

Viksomhetsundersøkelse av midlene ifølge oppfinnelsen på tricofyton-infiserte marsvin. Viability study of the agents according to the invention on trichophyton-infected guinea pigs.

Som prøvemodell til sammenlignende virksomhetsundersøkelse av midlene ifølge oppfinnelsen ble det anvendt tricopyton-infiserte Pirbright-hvite-marsvin med en gjennomsnittlig vekt på 6 00 g. Dyrene ble på ryggen barbert med en elektrisk hårklippemaskin således at det forble stående ca. 1/10 mm lange hårstumper. Tricopyton-infected Pirbright white guinea pigs with an average weight of 600 g were used as a test model for a comparative business study of the agents according to the invention. The animals were shaved on their backs with an electric hair clipper so that approx. 1/10 mm long hair stubs.

Infeksjonen med tritricofyton metagrofytes foregikk ved lett utrivning av en 24 timer, i Sabouraud-næringsoppløsning kim-dannet sporesuspensjon av frembringeren på en ca. 2 x 2 cm stor flate av den barberte rygg av dyrene. Det ble påført pr. dyr 0,5 ml kimsuspensjon som inneholdt 1 - 3 x 10^ infektiøse soppartikler. The infection with Tritricophyton metagrophytes took place by lightly pulling out a 24 hour, in Sabouraud nutrient solution germ-formed spore suspension of the producer on an approx. 2 x 2 cm large area of the shaved back of the animals. It was applied per animals 0.5 ml of germ suspension which contained 1 - 3 x 10^ infectious fungal particles.

Ved denne infeksjonsmodus viste det seg 2-3 dager postinfek-sjonem de første symptomer av dermatofytose som røddannelse og skorpedannelse på huden. Ved ubehandlede dyr er ca. 14 dager p-i- dermatofytosen maksimalt utpreget. Håravfall-plater og blodige integument-defekter innen en betent endret, skårpet kantsone. With this mode of infection, the first symptoms of dermatophytosis appeared 2-3 days post-infection, such as redness and crusting on the skin. In untreated animals, approx. 14 days p-i- the dermatophytosis maximally pronounced. Alopecia plaques and bloody integument defects within an inflamed altered, sharpened edge zone.

De formuleringer som skulle undersøkes appliseres en gangThe formulations to be examined are applied once

på 2. dag post infeksjonum lokalt på de røde infeksjons-steder på dyrene. Det ble hver gang påført 0,5 ml av formuleringene = 5 mg virksomt stoff (1 %ig formulering). Vurderingene av infeksjonsforløpet foregikk daglig inntil on the 2nd day post infection locally on the red infection sites on the animals. 0.5 ml of the formulations = 5 mg of active substance (1% formulation) was applied each time. The assessments of the course of the infection took place daily until

20. dag p.i.20th day p.i.

Resultatene er angitt ved eksempelene. ( + = svak virkning, ++ er like virkning, +++ = god virkning, ++++ = meget god: virkning). The results are indicated by the examples. ( + = weak effect, ++ is equal effect, +++ = good effect, ++++ = very good: effect).

I de følgende eksempler er det angitt reseptorer for midlene ifølge oppfinnelsen. De enkelte komponenter blandes med hverandre ved værelsetemperatur og går derved i oppløsning. In the following examples, receptors are indicated for the agents according to the invention. The individual components are mixed with each other at room temperature and thereby dissolve.

M.G. betyr molekylvekt.M. G. means molecular weight.

Anvender man istedenfor formuleringen ifølge oppfinnelsen slike som i stedenfor celluloseetere inneholder vannuopp-løselige polymerer, f.eks. metacrylater, så blir mykosen verre. If one uses instead of the formulation according to the invention those which contain water-insoluble polymers instead of cellulose ethers, e.g. methacrylates, then the mycosis gets worse.

Anvender man slike formuleringer som ved siden av det virksomme stoff bare inneholder vannoppløselige celluloseetere, men hverken spredemiddel eller oppløsningsformidlere oppnår man bare en svak virkning. If such formulations are used which, in addition to the active substance, only contain water-soluble cellulose ethers, but neither dispersants nor dissolution agents, only a weak effect is achieved.

Eksempel 1Example 1

Virkning på marsvinprøve ++++ = meget god virkning. Effect on guinea pig test ++++ = very good effect.

Eksempel 2Example 2

Virkning i marsvinprøve +++ = god virkning. Effect in guinea pig test +++ = good effect.

Eksempel 3Example 3

Virkning i marsvinprøve +++ = god virkning. Effect in guinea pig test +++ = good effect.

Eksempel 4 Example 4

Virkning i marsvinprøve +++ = god virkning. Effect in guinea pig test +++ = good effect.

Eksempel 5Example 5

Virkning i marsvinprøve +++ = god virkning. Effect in guinea pig test +++ = good effect.

Eksempel 6Example 6

Virkning i marsvinprøve ++++ meget god virkning. Effect in guinea pig test ++++ very good effect.

Eksempel 7Example 7

eks. 7 forts... e.g. 7 cont...

Virkning i marsvinprøve +++ = god virkning. Effect in guinea pig test +++ = good effect.

Eksempel 8Example 8

Virkning i marsvinprøve +++ = god virkning. Effect in guinea pig test +++ = good effect.

SpraysSprays

De ifølge eksempelene 1-8 fremstilte virksomme stoffopp-løsninger kan også forarbeides til sprays. For dette formål blander man f.eks. 60 - 90 % virksom stoffopp-løsning med 20 - 40 % av de vanlige drivmidler, f.eks. N2, N20, C02, propan, butan, halogenhydrokarbon osv. The active substance solutions prepared according to examples 1-8 can also be processed into sprays. For this purpose, you mix e.g. 60 - 90% active substance solution with 20 - 40% of the usual propellants, e.g. N2, N20, C02, propane, butane, halohydrocarbon, etc.

Claims (8)

1. Antimykotisk middel med høyere frigjøring av de virksomme stoffer inneholdende azolderivater og vanlige formuleringshjelpestoffer, karakterisert ved at de inneholder 2-10% spredemiddel, 1-8% oppløsningsformidler og som filmdanner celluloseeter.1. Antimycotic agent with higher release of the active substances containing azole derivatives and common formulation aids, characterized in that they contain 2-10% dispersant, 1-8% solubilizer and film-forming cellulose ether. 2. Antimykotisk middel ifølge krav 1, karakterisert ved at det som virksomt stoff inneholder clotrimazol med formel: 2. Antimycotic agent according to claim 1, characterized in that the active substance contains clotrimazole with the formula: 3. Antomykotisk middel ifølge krav 1, karakterisert ved at det som virksomt stoff inneholder trifon-azol med formel: 3. Antomycotic agent according to claim 1, characterized in that the active ingredient contains trifonazole with the formula: 4. Antimykotisk middel ifølge krav 1, karakterisert ved at det som virksomt stoff inneholder lombazol med formel: 4. Antimycotic agent according to claim 1, characterized in that the active ingredient contains lombazole with the formula: 5. Antimykotisk middel ifølge krav 1, karakterisert ved at det inneholder de antimykotiske azolderivater i mengder på 0,05-1%, fortrinnsvis på 0,1-1%. 5. Antimycotic agent according to claim 1, characterized in that it contains the antifungal azole derivatives in quantities of 0.05-1%, preferably of 0.1-1%. 6. Antimykotisk middel ifølge krav 1, karakterisert ved at det som filmdanner inneholder hydroksypropylcellulose.6. Antimycotic agent according to claim 1, characterized in that the film former contains hydroxypropyl cellulose. 7. Antimykotisk middel ifølge krav 1, karakterisert ved at det er en oppløsning.7. Antimycotic agent according to claim 1, characterized in that it is a solution. 8. Antimykotisk middel ifølge krav 1, karakterisert ved at det er en spray.8. Antimycotic agent according to claim 1, characterized in that it is a spray.
NO813931A 1980-12-05 1981-11-19 ANTIMYCOTIC AGENT WITH HIGH EFFICIENT SUBSTANCE RELEASE IN THE FORM OF ELASTIC LIQUID PLASTERS NO813931L (en)

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DE19803045915 DE3045915A1 (en) 1980-12-05 1980-12-05 ANTIMYCOTIC AGENTS WITH HIGH ACTIVE SUBSTANCE RELEASE IN THE FORM OF ELASTIC LIQUID PLASTERS

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NO813931L true NO813931L (en) 1982-06-07

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EP (1) EP0055396B1 (en)
JP (1) JPS57122016A (en)
AT (1) ATE11369T1 (en)
AU (1) AU546450B2 (en)
CA (1) CA1175354A (en)
DE (2) DE3045915A1 (en)
DK (1) DK538381A (en)
FI (1) FI813884L (en)
IL (1) IL64435A (en)
NO (1) NO813931L (en)
PH (1) PH17277A (en)
ZA (1) ZA818432B (en)

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DE3243546A1 (en) * 1982-11-25 1984-05-30 Bayer Ag, 5090 Leverkusen ANTIMYCOTIC AGENTS IN GEL FOR TREATING FUNGAL INFECTIONS OF THE ORAL CAVES
EP0117811A3 (en) * 1983-02-23 1987-06-03 Sanofi S.A. Fungicidal pharmaceutical compositions for oral administration
FR2541114B1 (en) * 1983-02-23 1986-04-11 Sanofi Sa ANTIFUNGAL PHARMACEUTICAL COMPOSITIONS FOR ORAL USE CONTAINING OMOCONAZOLE
DE3311701A1 (en) * 1983-03-30 1984-10-04 Bayer Ag ANTIMYCOTIC AGENTS WITH HIGH ACTIVE SUBSTANCE RELEASE IN THE FORM OF CREAM
DE3311700A1 (en) * 1983-03-30 1984-10-04 Bayer Ag ANTIMYCOTIC AGENTS WITH HIGH ACTIVE SUBSTANCE RELEASE IN THE FORM OF SOLUTION AND SPRAY
JPS6058914A (en) * 1983-09-12 1985-04-05 Shionogi & Co Ltd Antimycotic gel preparation for external use containing imidazoles
CA1241602A (en) * 1984-02-23 1988-09-06 Ortho Pharmaceutical Corporation Antifungal aerosol solution
JPS61151117A (en) * 1984-12-25 1986-07-09 Bayer Yakuhin Kk Gelatinous antimycotic preparation
EP0215072A4 (en) * 1985-03-13 1990-01-08 Gluck Bruno A Antiseptic fluids.
HU200914B (en) * 1987-03-09 1990-09-28 Horvath Gyoengyi Lengyelne Process for producing new medical dosage unit suitable for local treatment of fungus infection of nails
JPH0725675B2 (en) * 1989-05-08 1995-03-22 ホーユー株式会社 Liquid mycosis agent
JP2555555B2 (en) * 1991-07-03 1996-11-20 武田薬品工業株式会社 Antifungal topical formulation
GB9408545D0 (en) * 1994-04-29 1994-06-22 Zyma Sa Compositions
FR2732223B1 (en) * 1995-03-30 1997-06-13 Sanofi Sa PHARMACEUTICAL COMPOSITION FOR TRANSDERMAL ADMINISTRATION
PT1150661E (en) * 1999-02-05 2004-02-27 Cipla Ltd PRODUCT FOR SPRAYING FOR TOPIC APPLICATION
US6962691B1 (en) 1999-05-20 2005-11-08 U & I Pharmaceuticals Ltd. Topical spray compositions
US8697753B1 (en) 2013-02-07 2014-04-15 Polichem Sa Method of treating onychomycosis

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US3476853A (en) * 1965-04-13 1969-11-04 Colgate Palmolive Co Sprayed opaque bandage composition
DE2333335A1 (en) * 1973-06-29 1975-01-23 Siemens Ag Spring wire contact for cross-bar switches - has contact element at free end of spring contact in wire axial direction
JPS50129728A (en) * 1974-04-05 1975-10-14
DE2430039C2 (en) * 1974-06-22 1983-11-10 Bayer Ag, 5090 Leverkusen Climbazole in cosmetic products
DE2461406C2 (en) * 1974-12-24 1984-06-14 Bayer Ag, 5090 Leverkusen Azolyl- (1) -methanes and their salts, processes for their preparation and medicaments containing them
DE2628421A1 (en) * 1976-06-24 1978-01-05 Bayer Ag ANTIMICROBIAL AGENTS
JPS53139719A (en) * 1977-05-12 1978-12-06 Terumo Corp Antibacterial coating composition
DE2811916A1 (en) * 1978-03-18 1979-09-27 Bayer Ag Antimycotic 1-phenoxy-1-azolyl-4-halo-2-acyloxy-butane derivs. - prepd. by acylation of corresp. 1-imidazolyl-or 1-triazolyl-2-butanol derivs.

Also Published As

Publication number Publication date
ATE11369T1 (en) 1985-02-15
IL64435A0 (en) 1982-03-31
PH17277A (en) 1984-07-06
DE3045915A1 (en) 1982-07-08
ZA818432B (en) 1982-11-24
DE3168543D1 (en) 1985-03-07
FI813884A7 (en) 1982-06-06
EP0055396A1 (en) 1982-07-07
AU7826281A (en) 1982-06-10
JPS57122016A (en) 1982-07-29
CA1175354A (en) 1984-10-02
FI813884L (en) 1982-06-06
IL64435A (en) 1985-03-31
EP0055396B1 (en) 1985-01-23
DK538381A (en) 1982-06-06
AU546450B2 (en) 1985-09-05

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