EP1104295A1 - Use of quaternary nitrogen compounds for prophylaxis or treatment of superinfected atopic eczema - Google Patents

Use of quaternary nitrogen compounds for prophylaxis or treatment of superinfected atopic eczema

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Publication number
EP1104295A1
EP1104295A1 EP99938370A EP99938370A EP1104295A1 EP 1104295 A1 EP1104295 A1 EP 1104295A1 EP 99938370 A EP99938370 A EP 99938370A EP 99938370 A EP99938370 A EP 99938370A EP 1104295 A1 EP1104295 A1 EP 1104295A1
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EP
European Patent Office
Prior art keywords
acid
sodium
derivatives
oil
advantageously
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.)
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Application number
EP99938370A
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German (de)
French (fr)
Inventor
Gunhild Hamer
Bernd Traupe
Florian Wolf
Heiner Max
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Beiersdorf AG
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Beiersdorf AG
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Publication of EP1104295A1 publication Critical patent/EP1104295A1/en
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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/74Synthetic polymeric materials
    • A61K31/785Polymers containing nitrogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/14Quaternary ammonium compounds, e.g. edrophonium, choline

Definitions

  • Atopic eczema generally begins with itching, reddening, scaling, oozing and crusting, whereby the areas of the skin that are affected, depending on the age of the patient, assume certain characteristic accumulations. Complications in the appearance of atopic eczema are often superinfections with various pathogens men, especially Staphylococcus aureus, which affects approximately 90% of all atopics with eczematous manifestation.
  • Conventional treatment methods therefore include, in addition to anti-inflammatory agents (e.g. hydrocortisone), also external substances such as various antibiotics in the narrower sense or agents with antimicrobial or antimycotic properties in the broader sense (e.g. gentian violet).
  • anti-inflammatory agents e.g. hydrocortisone
  • external substances such as various antibiotics in the narrower sense or agents with antimicrobial or antimycotic properties in the broader sense (e.g. gentian violet).
  • the conventionally used active ingredients usually have the disadvantage that they either have more or less serious side effects, resistance or intolerance, or that they have an unsanitary appearance (e.g. severe skin discoloration with gentian violet).
  • antibiotics In individual cases, it is easily possible to fight superinfections with antibiotics, but mostly such substances have the disadvantage of unpleasant side effects. For example, patients are often allergic to penicillins, which is why appropriate treatment would be prohibited in such a case. Furthermore, topically administered antibiotics have the disadvantage that they not only free the skin flora from the secondary pathogen, but also severely impair the physiological skin flora and the natural healing process is slowed down again in this way.
  • the object of the present invention was to eliminate the disadvantages of the prior art and to make available substances and preparations containing such substances, the use of which can cure superinfections, the physiological skin flora not suffering any appreciable losses.
  • quaternary ammonium compounds is sometimes used synonymously for “quaternary nitrogen compounds”.
  • quaternary ammonium compounds or preparations containing quaternary ammonium compounds are extremely suitable for reducing superinfected atopic eczema or for alleviating the symptoms of superinfected eczema.
  • Quaternary ammonium compounds with at least one long alkyl chain such as distearyldimethylammonium chloride (DSDMA)
  • DSDMA distearyldimethylammonium chloride
  • Predominantly short-chain quaternary ammonium compounds have microbicidal properties and are therefore used in fungicidal and bactericidal disinfectants or as algicides.
  • the quaternary ammonium compounds used according to the invention can advantageously be selected from the group of quaternary surfactants.
  • alkyl betaine, alkyl amidopropyl betaine and alkyl amidopropyl hydroxysulfain are advantageous.
  • the cationic surfactants used in the invention can be furthermore preferably selected from the group of quaternary ammonium compounds, especially benzyltrialkylammonium chlorides or bromides, such as benzyl zyldimethylstearylammoniumchlorid, further Alkyltriaikylammoniumsalze, for example cetyltrimethylammonium chloride or bromide, xyethylammoniumchloride Alkyldimethylhydro- or bromides, dialkyldimethylammonium chlorides or - bromides , Alkylamidethyltrimethylammonium ether sulfates, alkylpyridinium salts, for example lauryl or cetylpyrimidinium chloride, imidazoline derivatives and compounds with a cationic character such as amine
  • the preparations according to the invention are particularly advantageously characterized in that the quaternary nitrogen compounds are present in concentrations of 0.001-99.00% by weight, preferably 0.01-50.00% by weight, particularly preferably 0.1-10.00% by weight .-%, each based on the total weight of the composition.
  • Dermatological preparations according to the invention can be in the form of aerosols, that is to say from aerosol containers, squeeze bottles or preparations sprayable by a pump device, or in the form of liquid compositions that can be applied by means of roll-on devices, but also in the form of W / O that can be applied from normal bottles and containers. or O / W emulsions, e.g. Creams or lotions.
  • the preparations can advantageously be in the form of tinctures, shampoos, washing, showering or bathing preparations or powders.
  • ethanol and isopropanol, glycerol and propylene glycol, skin-caring fat or fat-like substances, such as oleic acid decyl ester, cetyl alcohol, cetylstearyl alcohol and 2-octyldodecanol can be used as conventional cosmetic carriers for the production of the dermatological preparations according to the invention in such a way
  • Preparations customary proportions are used as well as Schieimbiidigen substances and thickeners, such as hydroxyethyl or hydroxypropyl cellulose, polyacrylic acid, polyvinylpyrrolidone, but also in small amounts cyclic silicone oils (polydimethylsiloxanes) and liquid polymethylphenylsiloxanes of low viscosity.
  • the lipid phase can advantageously be selected from the following group of substances: mineral oils, mineral waxes
  • Oils such as triglycerides of capric or caprylic acid, but preferably castor oil;
  • Fats, waxes and other natural and synthetic fat bodies preferably esters of fatty acids with alcohols of low C number, e.g. with isopropanol, propylene glycol or glycerin, or esters of fatty alcohols with low C number alkanoic acids or with fatty acids; Alkyl benzoates;
  • Silicone oils such as dimethylpolysiloxanes, diethylpolysiloxanes, diphenylpolysiioxanes and mixed forms thereof.
  • the oil phase of preparations according to the invention in the form of oils, emulsions, oleogels or hydrodispersions or lipodispersions is advantageously selected from the group of esters from saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 3 to 30 carbon atoms. Atoms and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 to 30 carbon atoms, from the group of esters from aromatic carboxylic acids and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 to 30 carbon atoms.
  • ester oils can then advantageously be selected from the group of isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononylisononanoate, 2-xyl-ethylhexyl palmitate Hexyldecyl stearate, 2-octyldodecyl palmitate, oleyl oleate, olerlerucate, erucyl oieate, erucylerucate and synthetic, semisynthetic and natural mixtures of such esters, for example Jojoba oil.
  • the oil phase can advantageously be selected from the group of branched and unbranched hydrocarbons and waxes, silicone oils, dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols, and also fatty acid triglycerides, in particular the triglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 8 to 24, in particular 12-18 C atoms.
  • the fatty acid triglycerides can, for example, advantageously be selected from the group of synthetic, semisynthetic and natural oils, for example olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm kernel oil and the like, in particular evening primrose oil and borage oil.
  • synthetic, semisynthetic and natural oils for example olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm kernel oil and the like, in particular evening primrose oil and borage oil.
  • any mixtures of such oil and wax components can also be used advantageously for the purposes of the present invention. It may also be advantageous to use waxes, for example cetyl palmitate, as the sole lipid component of the oil phase.
  • the oil phase is advantageously selected from the group consisting of 2-ethylhexyl isostearate, octyldodanol, isotridecyl isononanoate, isoeicosane, 2-ethylhexyl cocoate, C 12-1 alkyl benzoate, caprylic capric acid triglyceride, dicaprylyl ether.
  • hydrocarbons paraffin oil, squaian and squaien can be used advantageously for the purposes of the present invention.
  • the oil phase can advantageously also contain cyclic or linear silicone oils or consist entirely of such oils, although it is preferred to use an additional content of other oil phase components in addition to the silicone oil or the silicone oils.
  • Cyclomethicone (octamethylcyclotetrasiloxane) is advantageously used as the silicone oil to be used according to the invention.
  • other silicone oils can also be used advantageously for the purposes of the present invention, for example hexamethylcyclotrisiloxane, polydimethylsiloxane, poly (methylphenylsiloxane).
  • Mixtures of cyclomethicone and isotridecyl isononanoate, cyclomethicone and 2-ethylhexyl isostearate are also particularly advantageous.
  • the aqueous phase of the preparations according to the invention advantageously advantageously contains alcohols, diols or polyols of low C number, and their ethers, preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or mono - Butyl ether, diethylene glycol monomethyl or monoethyl ether and similar products, furthermore alcohols with a low C number, for example Ethanol, isopropanol, 1, 2-propanediol, glycerol and in particular one or more thickening agents, which one or more can advantageously be selected from the group consisting of silicon dioxide, aluminum silicates, polysaccharides or their derivatives, e.g.
  • Hyaluronic acid, xanthan gum, hydroxypropyl methyl cellulose particularly advantageously from the group of the polyacrylates, preferably a polyacrylate from the group of the so-called carbopoles, for example carbopoles of the types 980, 981, 1382, 2984, 5984, each individually or in combination.
  • Solid pins used in the present invention contain e.g. natural or synthetic waxes, fatty alcohols or fatty acid esters.
  • Suitable propellants for dermatological preparations according to the invention which can be sprayed from aerosol containers are the customary, known volatile, liquefied propellants, for example hydrocarbons (propane, butane, isobutane), which can be used alone or in a mixture with one another. Compressed air can also be used advantageously.
  • hydrocarbons propane, butane, isobutane
  • Non-ionogenic types such as polyoxyethylene fatty alcohol ethers, for example cetylstearyl alcohol polyethylene glycol ethers with 12 or 20 attached ethylene oxide units per molecule, cetostearyl alcohol and sorbitan esters and sorbitan ester and ethylene oxide compounds (for example sorbitan ethyl monostearate and monostearate) and long-chain, high molecular weight waxy polyglycol ethers have been found to be suitable.
  • polyoxyethylene fatty alcohol ethers for example cetylstearyl alcohol polyethylene glycol ethers with 12 or 20 attached ethylene oxide units per molecule
  • cetostearyl alcohol and sorbitan esters and sorbitan ester and ethylene oxide compounds for example sorbitan ethyl monostearate and monostearate
  • long-chain, high molecular weight waxy polyglycol ethers have been found to be suitable.
  • Cleaning agents can also be advantageous embodiments of the present invention. This is particularly advantageous since some quaternary nitrogen compounds have surfactant properties.
  • Surfactants are amphiphilic substances that can dissolve organic, non-polar substances in water. Due to their specific molecular structure with at least one hydrophilic and one hydrophobic part of the molecule, they ensure a reduction in the surface tension of the water, wetting of the skin, facilitating the removal and removal of dirt, easy rinsing and, if desired, foam regulation.
  • hydrophilic parts of a surfactant molecule are mostly polar functional groups, for example -COO " , -OSO 3 2" , -SO 3 " , while the hydrophobic parts generally represent non-polar hydrocarbon residues.
  • Surfactants are generally of type and charge of the hydrophilic part of the molecule. There are four groups:
  • B + any cation, eg Na +
  • Non-ionic surfactants do not form ions in an aqueous medium.
  • Anionic surfactants to be used advantageously are acylamino acids (and their salts), such as
  • acylglutamates for example sodium acylglutamate, di-TEA-palmitoylaspartate and sodium caprylic / capric glutamate,
  • acyl peptides for example palmitoyl-hydrolyzed milk protein, sodium cocoyl-hydrolyzed soy protein and sodium / potassium cocoyl-hydrolyzed collagen,
  • Sarcosinates for example myristoyl sarcosin, TEA-lauroyl sarcosinate, sodium lauroyl sarcosinate and sodium cocoyl sarcosinate,
  • taurates for example sodium lauroyl taurate and sodium methyl cocoyl taurate
  • carboxylic acids for example lauric acid, aluminum stearate, magnesium alkanolate and zinc undecyienate,
  • ester carboxylic acids for example calcium stearoyl lactylate, laureth-6 citrate and sodium PEG-4 lauramide carboxylate,
  • ether carboxylic acids for example sodium laureth-13 carboxylate and sodium PEG-6 cocamide carboxylate,
  • Phosphoric acid esters and salts such as, for example, DEA-oleth-10-phosphate and di-laureth-4 phosphate, Sulfonic acids and salts such as
  • acyl isethionates e.g. Sodium / ammonium cocoyl isethionate
  • alkyl sulfonates for example sodium coconut monoglyceride sulfate, sodium C ⁇ 2-14 olefin sulfonate, sodium lauryl sulfoacetate and magnesium PEG-3 cocamide sulfate,
  • Sulfosuccinates for example dioctyl sodium sulfosuccinate, disodium laureth sulfosuccinate, disodium lauryl sulfosuccinate and disodium undecylenamido MEA sulfosuccinate
  • sulfuric acid esters such as
  • alkyl ether sulfate for example sodium, ammonium, magnesium, MIPA, TIPA laureth sulfate, sodium myreth sulfate and sodium C ⁇ 2-13 pareth sulfate,
  • Alkyl sulfates for example sodium, ammonium and TEA lauryl sulfate.
  • the large remaining group of quaternary nitrogen surfactants is represented by the group of active substances on which the invention is based.
  • acyl- / dialkylethylenediamine for example sodium acylamphoacetate, disodium acylamphodipropionate, disodium alkylamphodiacetate, sodium acylamphohydroxypropylsulfonate, disodium acylamphodiacetate and sodium acylamphopropionate,
  • N-alkylamino acids for example aminopropylalkylglutamide, alkylaminopropionic acid, sodium alkylimidodipropionate and lauroamphocarboxyglycinate.
  • Non-ionic surfactants to be used advantageously 1. alcohols,
  • alkanolamides such as cocamides MEA / DEA / MIPA
  • amine oxides such as cocoamidopropylamine oxide
  • esters which are formed by esterification of carboxylic acids with ethyl oxide, glycerol, sorbitol or other alcohols,
  • ethers for example ethoxylated / propoxylated alcohols, ethoxyated / propoxylated esters, ethoxyated / propoxylated glycerol esters, ethoxyated / propoxylated cholesterols, ethoxylated / propoxylated triglyceride esters, ethoxylated propoxylated lanolin, ethoxylated / propoxylated polysiloxanes and propoxylated POs Lauryl glucoside, decyl glycoside and cocoglycoside.
  • compositions according to the invention can be up to 80% by weight, based on the total weight of the preparations.
  • the dermatological preparations according to the invention the pH of which is preferably e.g. is adjusted to 4.0 to 7.5, in particular 5.0 to 6.5, by customary buffer mixtures, perfume, dyes, antioxidants, suspending agents, buffer mixtures or other customary cosmetic or dermatological base materials are added.
  • antioxidants suitable or customary for cosmetic and / or dermatological applications can be used as favorable antioxidants.
  • antioxidants are advantageously selected from the group consisting of Amino acids (eg glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (eg urocanic acid) and their derivatives, peptides such as D, L-carnosine, D-carnosine, L-carnosine and their derivatives (eg anserine), carotenoids , Carotenes (e.g. ⁇ -carotene, ß-carotene, lycopene) and their derivatives, chlorogenic acid and their derivatives, liponic acid and their derivatives (e.g.
  • Amino acids eg glycine, histidine, tyrosine, tryptophan
  • imidazoles eg urocanic acid
  • peptides such as D, L-carnosine, D-carnosine, L-carnosine and their derivatives (eg anserine)
  • carotenoids e.g.
  • thiols e.g. thioredoxin, glutathione, cysteine, cystine, Cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, paimitoyl, oleyl, ⁇ -linoleyl, cholesteryl and glyceryl esters
  • salts dilaurylthiodi - propionate, distearyl thiodipropionate, thiodipropionic acid and their derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) as well as sulfoximine compounds (eg buthioninsulfoximines, homocysteine sulfoximine, buthioninsulfones, penta
  • thiols e.g. thioredoxin, glutathione, cysteine
  • ⁇ -hydroxy fatty acids e.g. cftronic acid, lactic acid, malic acid
  • humic acid e.g. bile acid, bile extracts, bilirubin, biliverdin, EDTA, EGTA and their derivatives
  • unsaturated fatty acids and their derivatives eg ⁇ -linolenic acid, linoleic acid, oleic acid
  • folic acid and their derivatives ubiquinone and ubiquinol and their derivatives
  • vitamin C and derivatives eg ascorbyl palmitate, Mg-ascorbyl phosphate, as - corby acetate
  • tocopherols and derivatives eg vitamin E acetate
  • vitamin A and derivatives vitamin A and derivatives (vitamin A palmitate) as well as coniferyl benzoate of benzoin
  • the amount of the antioxidants (one or more compounds) in the preparations is preferably 0.001 to 30% by weight, particularly preferably 0.05-20% by weight, in particular 1-10% by weight, based on the total weight of the preparation .
  • vitamin E and / or its derivatives represent the antioxidant (s)
  • vitamin A or vitamin A derivatives or carotenes or their derivatives represent the antioxidant or antioxidants, it is advantageous to have their respective concentrations in the range from 0.001-10% by weight, based on the total weight of the formulation, to choose.
  • the pH of the dermatological preparations according to the invention is less than 8. pH values that are slightly higher than 7 but less than 7.5 can generally be tolerated. In any case, it is easy to determine for a given fatty acid mixture by simply trying it out, without inventive step, which exact upper pH limit is to be observed.
  • the pH of the formulations according to the invention is advantageously adjusted to less than 8 in the acidic to very weakly alkaline range, preferably from 4.0 to 7.5, particularly preferably from 5.0 to 6.5.
  • auxiliary additives and carriers and possibly perfume to be used can easily be determined by a person skilled in the art by simply trying them out, depending on the type of product in question.
  • the dermatological preparations according to the invention are prepared in a customary manner, usually simply by mixing with stirring, optionally with gentle heating. It has no difficulties.
  • fat phase and water phase e.g. prepared separately, optionally with heating and then emulsified.
  • the suspension bases for this can advantageously be selected from the group Silicic acid gels (eg those available under the trade name Aerosil®), kieselguhr, talc, modified starch, titanium dioxide, silk powder, nylon powder, polyethylene powder and related substances.
  • Titanium dioxide 1.00

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Abstract

The invention relates to the use of quaternary nitrogen compounds for the prophylaxis or treatment of superinfected atopic eczema.

Description

Beschreibung description
Verwendung quaternärer Stickstoffverbindungen zur Prophylaxe und Behandlung des superinfizierten atopischen EkzemsUse of quaternary nitrogen compounds for the prophylaxis and treatment of superinfected atopic eczema
Die gesunde menschliche Haut ist mit einer Vielzahl nichtpathogener Mikroorganismen besiedelt. Diese sogenannte Mikroflora der Haut ist nicht nur unschädlich, sie stellt einen wichtigen Schutz zur Abwehr opportunistischer oder pathogener Keime dar.Healthy human skin is populated with a large number of non-pathogenic microorganisms. This so-called microflora of the skin is not only harmless, it is an important protection for the defense against opportunistic or pathogenic germs.
Bei bestehendem Primärinfekt, d.h., der normalen Keimbesiedeiung der Haut, eintretende Neuinfektion mit hohen Keimzahlen eines oder mehrerer oft physiologischer Erreger, beispielsweise Staphylokokken, oft aber auch unphysiologischer Erreger, beispielsweise Candida albicans, kann bei Zusammentreffen ungünstiger Einflüssen eine "Superinfektion" der befallenen Haut auftreten. Die normale Mikroflora der Haut (oder eines anderen Körperorgans) wird dabei von dem Sekundärerreger regelrecht überwuchert.In the case of an existing primary infection, that is, the normal microbial colonization of the skin, new infection with high bacterial counts of one or more often physiological pathogens, for example staphylococci, but often also unphysiological pathogens, for example Candida albicans, a "superinfection" of the affected skin can occur when adverse influences come together . The normal microflora of the skin (or another body organ) is literally overgrown by the secondary pathogen.
Solche Superinfektionen können sich, in Abhängigkeit vom betreffenden Keim, in günstig verlaufenden Fällen in unangenehmen Hauterscheinungen (Juckreiz, unschönes äußeres Erscheinungsbild) äußern. In ungünstig verlaufenden Fällen können sie aber zu großflächiger Zerstörung der Haut führen, im schlimmsten Falle sogar im Tode des Patienten gipfeln.Depending on the germ in question, such superinfections can manifest themselves in unpleasant skin symptoms (itching, unattractive external appearance) in favorable cases. In unfavorable cases, however, they can lead to extensive destruction of the skin, in the worst case even culminating in the death of the patient.
Derartige Superinfektionen werden bei einer Vielzahl dermatologischer Erkrankungen wie insbesondere dem atopischem Ekzem, auch Neurodermitis beobachtet. Das ato- pische Ekzem beginnt im allgemeinen mit Juckreiz, Rötung, Schuppung, Nässen und Krustenbildung, wobei der Befall der Hautpartien je nach Lebensalter des Patienten gewisse charakteristische Häufungen annimmt. Komplikationen beim Erscheinungsbild des atopischen Ekzems stellen oftmals Superinfektionen mit verschiedenen Kei- men dar, insbesondere Staphylococcus aureus, von denen ca. 90 % aller Atopiker mit ekzematöser Ausprägung betroffen sind.Superinfections of this kind are observed in a large number of dermatological diseases, in particular atopic eczema, including neurodermatitis. Atopic eczema generally begins with itching, reddening, scaling, oozing and crusting, whereby the areas of the skin that are affected, depending on the age of the patient, assume certain characteristic accumulations. Complications in the appearance of atopic eczema are often superinfections with various pathogens men, especially Staphylococcus aureus, which affects approximately 90% of all atopics with eczematous manifestation.
Herkömmliche Behandlungsmethoden umfassen daher neben entzündungshemmenden Wirkstoffen (z.B. Hydrocortison) auch Externa wie verschiedene Antibiotika im engeren Sinne oder Wirkstoffe mit antimikrobiellen bzw. antimycotischen Eigenschaften im weiteren Sinne (z.B. Gentianaviolett).Conventional treatment methods therefore include, in addition to anti-inflammatory agents (e.g. hydrocortisone), also external substances such as various antibiotics in the narrower sense or agents with antimicrobial or antimycotic properties in the broader sense (e.g. gentian violet).
Die herkömmlich verwendeten Wirkstoffe haben aber zumeist den Nachteil, daß sie entweder mehr oder weniger schwerwiegende Nebenwirkungen, Resistenzbildung oder Unverträglichkeiten zeitigen, oder daß sie unkosmetische Anmutungen mit sich bringen (z.B. starke Hautverfärbung mit Gentianaviolett).However, the conventionally used active ingredients usually have the disadvantage that they either have more or less serious side effects, resistance or intolerance, or that they have an unsanitary appearance (e.g. severe skin discoloration with gentian violet).
So ist es im Einzelfalle ohne weiteres möglich, Superinfektionen mit Antibiotika zu bekämpfen, meistens haben solche Substanzen aber den Nachteil unangenehmer Nebenwirkungen. Oft sind Patienten beispielsweise gegen Penicilline allergisch, weswegen eine entsprechende Behandlung sich in einem solchen Falle verbieten würde. Ferner haben topisch verabreichte Antibiotika den Nachteil, daß sie die Hautflora nicht nur vom Sekundärerreger befreien, sondern auch die an sich physiologische Hautflora stark beeinträchtigen und der natürliche Heilungsprozeß auf diese Weise wieder gebremst wird.In individual cases, it is easily possible to fight superinfections with antibiotics, but mostly such substances have the disadvantage of unpleasant side effects. For example, patients are often allergic to penicillins, which is why appropriate treatment would be prohibited in such a case. Furthermore, topically administered antibiotics have the disadvantage that they not only free the skin flora from the secondary pathogen, but also severely impair the physiological skin flora and the natural healing process is slowed down again in this way.
Die Reduktion eines klinisch ausgeprägten atopischen Ekzems indes war mit Wirkstoffen und Zubereitungen des Standes der Technik bisher - wenn überhaupt erreichbar - stets mit erheblichen Unannehmlichkeiten verbunden.The reduction of clinically pronounced atopic eczema, however, has so far always been associated with considerable inconvenience, if at all, with active substances and preparations of the prior art.
Aufgabe der vorliegenden Erfindung war, die Nachteile des Standes der Technik zu beseitigen und Substanzen und Zubereitungen, solche Substanzen enthaltend, zur Verfügung zu stellen, durch deren Verwendung Superinfektionen geheilt werden können, wobei die physiologische Hautflora keine nennenswerte Einbußen erleidet.The object of the present invention was to eliminate the disadvantages of the prior art and to make available substances and preparations containing such substances, the use of which can cure superinfections, the physiological skin flora not suffering any appreciable losses.
Darüberhinaus war es Aufgabe der vorliegenden Erfindung, Substanzen und kosmetische bzw. dermatologische Zubereitungen, solche Substanzen enthaltend, zur Verfügung zu steilen, die prophylaktisch gegen Superinfektionen wirken. Es wurde überraschend gefunden, und darin liegt die Lösung dieser Aufgabe, daß die Verwendung quaternärer Stickstoffverbindungen zur Prophylaxe und Behandlung des superinfizierten atopischen Ekzems den Nachteilen des Standes der Technik abhilft.Furthermore, it was an object of the present invention to provide substances and cosmetic or dermatological preparations containing such substances which have a prophylactic effect against superinfections. It has surprisingly been found, and this is the solution to this problem that the use of quaternary nitrogen compounds for the prophylaxis and treatment of superinfected atopic eczema remedies the disadvantages of the prior art.
Im Rahmen der Offenbarung zur vorliegenden Erfindung wird der Begriff „quaternäre Ammoniumverbindungen" gelegentlich synonym für „quaternäre Stickstoffverbindungen" angewandt.In the context of the disclosure of the present invention, the term “quaternary ammonium compounds” is sometimes used synonymously for “quaternary nitrogen compounds”.
Gemäß der Erfindung sind quaternäre Ammoniumverbindungen bzw. Zubereitungen, quaternäre Ammoniumverbindungen enthaltend, hervorragend geeignet, superinfizierte atopische Ekzeme zu reduzieren bzw. die Symptome superinfizierter Ekzeme zu lindern.According to the invention, quaternary ammonium compounds or preparations containing quaternary ammonium compounds are extremely suitable for reducing superinfected atopic eczema or for alleviating the symptoms of superinfected eczema.
Quaternäre Ammonium-Verbindungen zeichnen sich durch mindestens ein quaternä- res Stickstoff-Atomen aus und folgen den nachstehenden Grundschemata:Quaternary ammonium compounds are characterized by at least one quaternary nitrogen atom and follow the basic schemes below:
(1) (2) (3)(1) (2) (3)
(1) Alkylammonium-Verbindungen(1) alkyl ammonium compounds
(2) Imidazolinium-Verbindungen(2) Imidazolinium compounds
(3) Pyridinium-Verbindungen.(3) pyridinium compounds.
Quaternäre Ammoniumverbindungen mit mindestens einer langen Alkyl-Kette, wie beispielsweise das Distearyldimethylammoniumchlorid (DSDMA), besitzen oberflächenaktive Eigenschaften und werden daher als Kationtenside, z. B. als Netzmittel, Emulgatoren, Antistatika und als Weichmacher eingesetzt. Vorwiegend kurzkettige quaternäre Ammoniumverbindungen weisen mikrobizide Eigenschaften auf und finden daher Verwendung in fungiziden und bakteriziden Desinfektionsmitteln oder als Algizide. Die erfindungsgemäß verwendeten quaternären Ammoniumverbindungen können vorteilhaft aus der Gruppe der quaternären Tenside gewählt werden. Vorteilhaft sind beispielsweise Alkylbetain, Alkylamidopropylbetain und Alkyl-amidopropylhydroxy- sulfain. Die erfindungsgemäß verwendeten kationischen Tenside können femer bevorzugt gewählt werden aus der Gruppe der quaternären Ammoniumverbindungen, insbesondere Benzyltrialkylammoniumchloride oder -bromide, wie beispielsweise Ben- zyldimethylstearylammoniumchlorid, ferner Alkyltriaikylammoniumsalze, beispielsweise beispielsweise Cetyltrimethylammoniumchlorid oder -bromid, Alkyldimethylhydro- xyethylammoniumchloride oder -bromide, Dialkyldimethylammoniumchloride oder - bromide, Alkylamidethyltrimethylammoniumethersulfate, Alkylpyridiniumsalze, beispielsweise Lauryl- oder Cetylpyrimidiniumchiorid, Imidazolinderivate und Verbindungen mit kationischem Charakter wie Aminoxide, beispielsweise Alkyldimethylaminoxi- de oder Alkyiaminoethyldimethyiaminoxide. Vorteilhaft sind insbesondere Cetyltrime- thylammoniumsalze zu verwenden, wie auch Polyaminoalkylbiguanide, z.B. Poly- aminopropylbiguanid.Quaternary ammonium compounds with at least one long alkyl chain, such as distearyldimethylammonium chloride (DSDMA), have surface-active properties and are therefore used as cationic surfactants, e.g. B. used as wetting agents, emulsifiers, antistatic agents and as plasticizers. Predominantly short-chain quaternary ammonium compounds have microbicidal properties and are therefore used in fungicidal and bactericidal disinfectants or as algicides. The quaternary ammonium compounds used according to the invention can advantageously be selected from the group of quaternary surfactants. For example, alkyl betaine, alkyl amidopropyl betaine and alkyl amidopropyl hydroxysulfain are advantageous. The cationic surfactants used in the invention can be furthermore preferably selected from the group of quaternary ammonium compounds, especially benzyltrialkylammonium chlorides or bromides, such as benzyl zyldimethylstearylammoniumchlorid, further Alkyltriaikylammoniumsalze, for example cetyltrimethylammonium chloride or bromide, xyethylammoniumchloride Alkyldimethylhydro- or bromides, dialkyldimethylammonium chlorides or - bromides , Alkylamidethyltrimethylammonium ether sulfates, alkylpyridinium salts, for example lauryl or cetylpyrimidinium chloride, imidazoline derivatives and compounds with a cationic character such as amine oxides, for example alkyldimethylaminoxides or alkyiaminoethyldimethylamine oxides. Cetyltrimethylammonium salts are particularly advantageous, as are polyaminoalkyl biguanides, for example polyaminopropyl biguanide.
Die erfindungsgemäßen Zubereitungen sind besonders vorteilhaft dadurch gekennzeichnet, daß die die quaternären Stickstoffverbindungen in Konzentrationen von 0,001 - 99,00 Gew.-%, bevorzugt 0,01 - 50,00 Gew.-%, besonders bevorzugt 0,1 - 10,00 Gew.-%, jeweils bezogen auf das Gesamtgewicht der Zusammensetzung, vorliegen.The preparations according to the invention are particularly advantageously characterized in that the quaternary nitrogen compounds are present in concentrations of 0.001-99.00% by weight, preferably 0.01-50.00% by weight, particularly preferably 0.1-10.00% by weight .-%, each based on the total weight of the composition.
Erfindungsgemäße dermatologische Zubereitungen können in Form von Aerosolen, also aus Aerosolbehältern, Quetschflaschen oder durch eine Pumpvorrichtung versprühbaren Präparaten vorliegen oder in Form von mittels Roll-on-Vorrichtungen auftragbaren flüssigen Zusammensetzungen, jedoch auch in Form von aus normalen Flaschen und Behältern auftragbaren W/O- oder O/W-Emulsionen, z.B. Cremes oder Lotionen. Weiterhin können die Zubereitungen vorteilhaft in Form von Tinkturen, Shampoos, Wasch-, Dusch- oder Badezubereitungen oder Pudern vorliegen.Dermatological preparations according to the invention can be in the form of aerosols, that is to say from aerosol containers, squeeze bottles or preparations sprayable by a pump device, or in the form of liquid compositions that can be applied by means of roll-on devices, but also in the form of W / O that can be applied from normal bottles and containers. or O / W emulsions, e.g. Creams or lotions. Furthermore, the preparations can advantageously be in the form of tinctures, shampoos, washing, showering or bathing preparations or powders.
Als übliche kosmetische Trägerstoffe zur Herstellung der erfindungsgemäßen dermatologischen Zubereitungen können neben Wasser, Ethanol und Isopropanol, Glycerin und Propylenglykol hautpflegende Fett- oder fettähnliche Stoffe, wie Ölsäure- decylester, Cetylalkohol, Cetylstearylalkohol und 2-Octyldodecanol, in den für solche Präparate üblichen Mengenverhältnissen eingesetzt werden sowie schieimbiidende Stoffe und Verdickungsmittel, z.B. Hydroxyethyl- oder Hydroxypropylcellulose, Polyacrylsäure, Polyvinylpyrrolidon, daneben aber auch in kleinen Mengen cyclische Silikonöle (Polydimethylsiloxane) sowie flüssige Polymethylphenylsiloxane niedriger Viskosiät.In addition to water, ethanol and isopropanol, glycerol and propylene glycol, skin-caring fat or fat-like substances, such as oleic acid decyl ester, cetyl alcohol, cetylstearyl alcohol and 2-octyldodecanol, can be used as conventional cosmetic carriers for the production of the dermatological preparations according to the invention in such a way Preparations customary proportions are used as well as Schieimbiidigen substances and thickeners, such as hydroxyethyl or hydroxypropyl cellulose, polyacrylic acid, polyvinylpyrrolidone, but also in small amounts cyclic silicone oils (polydimethylsiloxanes) and liquid polymethylphenylsiloxanes of low viscosity.
Die Lipidphase kann vorteilhaft gewählt werden aus folgender Substanzgruppe: Mineralöle, MineralwachseThe lipid phase can advantageously be selected from the following group of substances: mineral oils, mineral waxes
Öle, wie Triglyceride der Caprin- oder der Caprylsäure, vorzugsweise aber Rizinusöl;Oils, such as triglycerides of capric or caprylic acid, but preferably castor oil;
Fette, Wachse und andere natürliche und synthetische Fettkörper, vorzugsweise Ester von Fettsäuren mit Alkoholen niedriger C-Zahl, z.B. mit Isopropanol, Propylenglykol oder Glycerin, oder Ester von Fettalkoholen mit Alkansäuren niedriger C-Zahl oder mit Fettsäuren; Alkylbenzoate;Fats, waxes and other natural and synthetic fat bodies, preferably esters of fatty acids with alcohols of low C number, e.g. with isopropanol, propylene glycol or glycerin, or esters of fatty alcohols with low C number alkanoic acids or with fatty acids; Alkyl benzoates;
Silikonöle wie Dimethylpolysiloxane, Diethylpolysiloxane, Diphenylpolysiioxane sowie Mischformen daraus.Silicone oils such as dimethylpolysiloxanes, diethylpolysiloxanes, diphenylpolysiioxanes and mixed forms thereof.
Die Ölphase von als Ölen, Emulsionen, Oleogelen bzw. Hydrodispersionen oder Lipo- dispersionen vorliegenden Zubereitungen gemäß der Erfindung wird vorteilhaft gewählt aus der Gruppe der Ester aus gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkancarbonsäuren einer Kettenlänge von 3 bis 30 C-Atomen und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C-Atomen, aus der Gruppe der Ester aus aromatischen Carbonsäuren und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C-Atomen. Solche Esteröle können dann vorteilhaft gewählt werden aus der Gruppe Isopropylmyristat, Isopropyl- palmitat, Isopropylstearat, Isopropyloleat, n-Butylstearat, n-Hexyllaurat, n-Decyloleat, Isooctylstearat, Isononylstearat, isononylisononanoat, 2-Ethylhexylpalmitat, 2-Ethylhe- xyllaurat, 2-Hexyldecylstearat, 2-Octyldodecylpalmitat, Oleyloleat, Oleylerucat, Erucyl- oieat, Erucylerucat sowie synthetische, halbsynthetische und natürliche Gemische solcher Ester, z.B. Jojobaöl.The oil phase of preparations according to the invention in the form of oils, emulsions, oleogels or hydrodispersions or lipodispersions is advantageously selected from the group of esters from saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 3 to 30 carbon atoms. Atoms and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 to 30 carbon atoms, from the group of esters from aromatic carboxylic acids and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 to 30 carbon atoms. Such ester oils can then advantageously be selected from the group of isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononylisononanoate, 2-xyl-ethylhexyl palmitate Hexyldecyl stearate, 2-octyldodecyl palmitate, oleyl oleate, olerlerucate, erucyl oieate, erucylerucate and synthetic, semisynthetic and natural mixtures of such esters, for example Jojoba oil.
Ferner kann die Ölphase vorteilhaft gewählt werden aus der Gruppe der verzweigten und unverzweigten Kohlenwasserstoffe und -wachse, der Silkonöle, der Dialkylether, der Gruppe der gesättigten oder ungesättigten, verzweigten oder unverzweigten Alkohole, sowie der Fettsäuretriglyceride, namentlich der Triglycerinester gesättigter und/oder ungesättigter, verzweigter und/oder unverzweigter Alkancarbonsäuren einer Kettenlänge von 8 bis 24, insbesondere 12 - 18 C-Atomen. Die Fettsäuretriglyceride können beispielsweise vorteilhaft gewählt werden aus der Gruppe der synthetischen, halbsynthetischen und natürlichen Öle, z.B. Olivenöl, Sonnenblumenöl, Sojaöl, Erdnußöl, Rapsöl, Mandelöl, Palmöl, Kokosöl, Palmkernöl und dergleichen mehr, insbesondere Nachtkerzenöl und Borretschöl.Furthermore, the oil phase can advantageously be selected from the group of branched and unbranched hydrocarbons and waxes, silicone oils, dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols, and also fatty acid triglycerides, in particular the triglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 8 to 24, in particular 12-18 C atoms. The fatty acid triglycerides can, for example, advantageously be selected from the group of synthetic, semisynthetic and natural oils, for example olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm kernel oil and the like, in particular evening primrose oil and borage oil.
Auch beliebige Abmischungen solcher Öl- und Wachskomponenten sind vorteilhaft im Sinne der vorliegenden Erfindung einzusetzen. Es kann auch gegebenenfalls vorteilhaft sein, Wachse, beispielsweise Cetylpalmitat, als alleinige Lipidkomponente der Ölphase einzusetzen.Any mixtures of such oil and wax components can also be used advantageously for the purposes of the present invention. It may also be advantageous to use waxes, for example cetyl palmitate, as the sole lipid component of the oil phase.
Vorteilhaft wird die Ölphase gewählt aus der Gruppe 2-Ethylhexylisostearat, Octyldo- decanol, Isotridecylisononanoat, Isoeicosan, 2-Ethylhexylcocoat, C12-1 -Alkylbenzoat, Capryl-Caprinsäure-triglycerid, Dicaprylylether.The oil phase is advantageously selected from the group consisting of 2-ethylhexyl isostearate, octyldodanol, isotridecyl isononanoate, isoeicosane, 2-ethylhexyl cocoate, C 12-1 alkyl benzoate, caprylic capric acid triglyceride, dicaprylyl ether.
Besonders vorteilhaft sind Mischungen aus Cι2-ιs-Alkylbenzoat und 2-Ethylhexyliso- stearat, Mischungen aus Cι2-ιs-Alkylbenzoat und Isotridecylisononanoat sowie Mischungen aus C12-i5-Alkylbenzoat, 2-Ethylhexylisostearat und Isotridecylisononanoat.Mixtures of C 2 -is alkyl benzoate and 2-ethylhexyl isostearate, mixtures of C 2 -is alkyl benzoate and isotridecyl isononanoate and mixtures of C 12 i5 alkyl benzoate, 2- ethyl hexyl isostearate and isotridecyl isononanoate are particularly advantageous.
Von den Kohlenwasserstoffen sind Paraffinöl, Squaian und Squaien vorteilhaft im Sinne der vorliegenden Erfindung zu verwenden.Of the hydrocarbons, paraffin oil, squaian and squaien can be used advantageously for the purposes of the present invention.
Vorteilhaft kann die Ölphase ferner einen Gehalt an cyclischen oder linearen Silikonölen aufweisen oder vollständig aus solchen Ölen bestehen, wobei allerdings bevorzugt wird, außer dem Silikonöl oder den Silikonölen einen zusätzlichen Gehalt an anderen Ölphasenkomponenten zu verwenden.The oil phase can advantageously also contain cyclic or linear silicone oils or consist entirely of such oils, although it is preferred to use an additional content of other oil phase components in addition to the silicone oil or the silicone oils.
Vorteilhaft wird Cyclomethicon (Octamethylcyclotetrasiloxan) als erfindungsgemäß zu verwendendes Silikonöl eingesetzt. Aber auch andere Silikonöle sind vorteilhaft im Sinne der vorliegenden Erfindung zu verwenden, beispielsweise Hexamethylcyclotrisi- loxan, Polydimethylsiloxan, Poly(methylphenylsiloxan). Besonders vorteilhaft sind ferner Mischungen aus Cyclomethicon und Isotridecylisononanoat, aus Cyclomethicon und 2-Ethylhexylisostearat.Cyclomethicone (octamethylcyclotetrasiloxane) is advantageously used as the silicone oil to be used according to the invention. However, other silicone oils can also be used advantageously for the purposes of the present invention, for example hexamethylcyclotrisiloxane, polydimethylsiloxane, poly (methylphenylsiloxane). Mixtures of cyclomethicone and isotridecyl isononanoate, cyclomethicone and 2-ethylhexyl isostearate are also particularly advantageous.
Die wäßrige Phase der erfindungsgemäßen Zubereitungen enthält gegebenenfalls vorteilhaft Alkohole, Diole oder Polyole niedriger C-Zahl, sowie deren Ether, vorzugsweise Ethanol, Isopropanol, Propylenglykol, Glycerin, Ethylenglykol, Ethylenglykolmo- noethyl- oder -monobutylether, Propylenglykolmonomethyl, -monoethyl- oder -mono- butylether, Diethylenglykolmonomethyl- oder -monoethylether und analoge Produkte, ferner Alkohole niedriger C-Zahl, z.B. Ethanol, Isopropanol, 1 ,2-Propandiol, Glycerin sowie insbesondere ein oder mehrere Verdickungsmrttel, welches oder welche vorteilhaft gewählt werden können aus der Gruppe Siiiciumdioxid, Aluminiumsilikate, Poly- saccharide bzw. deren Derivate, z.B. Hyaluronsäure, Xanthangummi, Hydroxypro- pylmethylcellulose, besonders vorteilhaft aus der Gruppe der Polyacrylate, bevorzugt ein Polyacrylat aus der Gruppe der sogenannten Carbopole, beispielsweise Car- bopole der Typen 980, 981 , 1382, 2984, 5984, jeweils einzeln oder in Kombination.The aqueous phase of the preparations according to the invention advantageously advantageously contains alcohols, diols or polyols of low C number, and their ethers, preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or mono - Butyl ether, diethylene glycol monomethyl or monoethyl ether and similar products, furthermore alcohols with a low C number, for example Ethanol, isopropanol, 1, 2-propanediol, glycerol and in particular one or more thickening agents, which one or more can advantageously be selected from the group consisting of silicon dioxide, aluminum silicates, polysaccharides or their derivatives, e.g. Hyaluronic acid, xanthan gum, hydroxypropyl methyl cellulose, particularly advantageously from the group of the polyacrylates, preferably a polyacrylate from the group of the so-called carbopoles, for example carbopoles of the types 980, 981, 1382, 2984, 5984, each individually or in combination.
Erfindungsgemäß verwendete feste Stifte enthalten z.B. natürliche oder synthetische Wachse, Fettalkohole oder Fettsäureester.Solid pins used in the present invention contain e.g. natural or synthetic waxes, fatty alcohols or fatty acid esters.
Als Treibmittel für erfindungsgemäße, aus Aerosolbehältern versprühbare dermatologische Zubereitungen sind die üblichen bekannten leichtflüchtigen, verflüssigten Treibmittel, beispielsweise Kohlenwasserstoffe (Propan, Butan, Isobutan) geeignet, die allein oder in Mischung miteinander eingesetzt werden können. Auch Druckluft ist vorteilhaft zu verwenden.Suitable propellants for dermatological preparations according to the invention which can be sprayed from aerosol containers are the customary, known volatile, liquefied propellants, for example hydrocarbons (propane, butane, isobutane), which can be used alone or in a mixture with one another. Compressed air can also be used advantageously.
Natürlich weiß der Fachmann, daß es an sich nichttoxische Treibgase gibt, die grundsätzlich für die vorliegende Erfindung geeignet wären, auf die aber dennoch wegen bedenklicher Wirkung auf die Umwelt oder sonstiger Begleitumstände verzichtet werden sollte, insbesondere Fluorchlorkohlenwasserstoffe (FCKW).Of course, the person skilled in the art knows that there are non-toxic propellant gases per se which would in principle be suitable for the present invention, but which should nevertheless be dispensed with, in particular chlorofluorocarbons (CFCs), because of their harmful effects on the environment or other associated circumstances.
Als Emulgatoren zur Herstellung der erfindungsgemäßen dermatologischen Zubereitungen, haben sich nichtionogene Typen, wie Polyoxyethylen-Fettalkoholether, z.B. Cetylstearylalkoholpolyethylengiykolether mit 12 bzw. 20 angelagerten Ethylenoxid- Einheiten pro Molekül, Cetostearylalkohol sowie Sorbitanester und Sorbrtanester- Ethylenoxid-Verbindungen (z.B. Sorbitanmonostearat und Polyoxyethylensorbitan- monostearat) und langkettige höhermolekulare wachsartige Polyglykolether als geeignet erwiesen.Non-ionogenic types such as polyoxyethylene fatty alcohol ethers, for example cetylstearyl alcohol polyethylene glycol ethers with 12 or 20 attached ethylene oxide units per molecule, cetostearyl alcohol and sorbitan esters and sorbitan ester and ethylene oxide compounds (for example sorbitan ethyl monostearate and monostearate) and long-chain, high molecular weight waxy polyglycol ethers have been found to be suitable.
Auch Reingungsmittel können vorteihafte Verkörperungen der vorliegenden Erfindung darstellen. Dies ist insbesondere daher vorteilhaft, da manche quaternäre Stickstoffverbindungen tensidische Eigenschaften aufweisen.Cleaning agents can also be advantageous embodiments of the present invention. This is particularly advantageous since some quaternary nitrogen compounds have surfactant properties.
Tenside sind amphiphile Stoffe, die organische, unpolare Substanzen in Wasser lösen können. Sie sorgen, bedingt durch ihren spezifischen Molekülaufbau mit mindestens einem hydrophilen und einem hydrophoben Molekülteil, für eine Herabsetzung der Oberflächenspannung des Wassers, die Benetzung der Haut, die Erleichterung der Schmutzentfernung und -lösung, ein leichtes Abspülen und -je nach Wunsch - für Schaumregulierung.Surfactants are amphiphilic substances that can dissolve organic, non-polar substances in water. Due to their specific molecular structure with at least one hydrophilic and one hydrophobic part of the molecule, they ensure a reduction in the surface tension of the water, wetting of the skin, facilitating the removal and removal of dirt, easy rinsing and, if desired, foam regulation.
Bei den hydrophilen Anteilen eines Tensidmoleküls handelt es sich meist um polare funktioneile Gruppen, beispielweise -COO", -OSO3 2", -SO3 ", während die hydrophoben Teile in der Regel unpolare Kohlenwasserstoffreste darstellen. Tenside werden im allgemeinen nach Art und Ladung des hydrophilen Molekülteils klassifiziert. Hierbei können vier Gruppen unterschieden werden:The hydrophilic parts of a surfactant molecule are mostly polar functional groups, for example -COO " , -OSO 3 2" , -SO 3 " , while the hydrophobic parts generally represent non-polar hydrocarbon residues. Surfactants are generally of type and charge of the hydrophilic part of the molecule. There are four groups:
• anionische Tenside,Anionic surfactants,
• kationische Tenside,Cationic surfactants,
• amphotere Tenside und• amphoteric surfactants and
• nichtionische Tenside.• nonionic surfactants.
Anionische Tenside weisen als funktionelle Gruppen in der Regel Carboxylat-, Sulfatoder Sulfonatgruppen auf. In wäßriger Lösung bilden sie im sauren oder neutralen Milieu negativ geladene organische Ionen. Kationische Tenside sind beinahe ausschließlich durch das Vorhandensein einer quarternären Ammoniumgruppe gekennzeichnet. In wäßriger Lösung bilden sie im sauren oder neutralen Milieu positiv geladene organische Ionen. Amphotere Tenside enthalten sowohl anionische als auch kationische Gruppen und verhalten sich demnach in wäßriger Lösung je nach pH- Wert wie anionische oder kationische Tenside. Im stark sauren Milieu besitzen sie eine positive und im alkalischen Milieu eine negative Ladung. Im neutralen pH-Bereich hingegen sind sie zwitterionisch, wie das folgende Beispiel verdeutlichen soll: RNH2 +CH2CH2COOH X" (bei pH=2) X' = beliebiges Anion, z.B. Cl" Anionic surfactants generally have carboxylate, sulfate or sulfonate groups as functional groups. In an aqueous solution they form negatively charged organic ions in an acidic or neutral environment. Cationic surfactants are characterized almost exclusively by the presence of a quaternary ammonium group. In aqueous solution they form positively charged organic ions in an acidic or neutral environment. Amphoteric surfactants contain both anionic and cationic groups and accordingly behave like anionic or cationic surfactants in aqueous solution depending on the pH. They have a positive charge in a strongly acidic environment and a negative charge in an alkaline environment. In the neutral pH range, however, they are zwitterionic, as the following example should illustrate: RNH 2 + CH 2 CH 2 COOH X " (at pH = 2) X ' = any anion, for example Cl "
RNH2 +CH2CH2COO" (bei pH=7)RNH 2 + CH 2 CH 2 COO " (at pH = 7)
RNHCH2CH2COO" B+ (bei pH=12) B+ = beliebiges Kation, z.B. Na+ RNHCH 2 CH 2 COO " B + (at pH = 12) B + = any cation, eg Na +
Typisch für nicht-ionische Tenside sind Polyether-Ketten. Nicht-ionische Tenside bilden in wäßrigem Medium keine Ionen.Polyether chains are typical of non-ionic surfactants. Non-ionic surfactants do not form ions in an aqueous medium.
A. Anionische TensideA. Anionic surfactants
Diese sind in der Regel schwer kompatibel mit kationischen Tensiden, weswegen ihre Mitverwendung gemäß der vorliegenden Erfindung erschwert, wenngleich, z.B. in geringen Mengen, nicht ausgeschlossen ist. Vorteilhaft zu verwendende anionische Tenside sind Acylaminosäuren (und deren Salze), wieAs a rule, these are difficultly compatible with cationic surfactants, which makes their use according to the present invention difficult, although, e.g. in small quantities, is not excluded. Anionic surfactants to be used advantageously are acylamino acids (and their salts), such as
1. Acylglutamate, beispielsweise Natriumacylglutamat, Di-TEA-palmitoylaspartat und Natrium Caprylic/ Capric Glutamat,1. acylglutamates, for example sodium acylglutamate, di-TEA-palmitoylaspartate and sodium caprylic / capric glutamate,
2. Acylpeptide, beispielsweise Palmitoyl-hydrolysiertes Milchprotein, Natrium Coco- yl-hydrolysiertes Soja Protein und Natrium-/ Kalium Cocoyl-hydrolysiertes Kollagen,2. acyl peptides, for example palmitoyl-hydrolyzed milk protein, sodium cocoyl-hydrolyzed soy protein and sodium / potassium cocoyl-hydrolyzed collagen,
3. Sarcosinate, beispielsweise Myristoyl Sarcosin, TEA-Iauroyl Sarcosinat, Natri- umlauroylsarcosinat und Natriumcocoylsarkosinat,3. Sarcosinates, for example myristoyl sarcosin, TEA-lauroyl sarcosinate, sodium lauroyl sarcosinate and sodium cocoyl sarcosinate,
4. Taurate, beispielsweise Natriumlauroyltaurat und Natriummethylcocoyltaurat,4. taurates, for example sodium lauroyl taurate and sodium methyl cocoyl taurate,
5. AcylLactylate, lauroyllactylat, Caproyllactylat5. Acyl lactylates, lauroyl lactylate, caproyl lactylate
6. Alaninate Carbonsäuren und Derivate, wie6. Alaninate carboxylic acids and derivatives such as
1. Carbonsäuren, beispielsweise Laurinsäure, Aluminiumstearat, Magnesiumalka- nolat und Zinkundecyienat,1. carboxylic acids, for example lauric acid, aluminum stearate, magnesium alkanolate and zinc undecyienate,
2. Ester-Carbonsäuren, beispielsweise Calciumstearoyllactylat, Laureth-6 Citrat und Natrium PEG-4 Lauramidcarboxylat,2. ester carboxylic acids, for example calcium stearoyl lactylate, laureth-6 citrate and sodium PEG-4 lauramide carboxylate,
3. Ether-Carbonsäuren, beispielsweise Natriumlaureth-13 Carboxylat und Natrium PEG-6 Cocamide Carboxylat,3. ether carboxylic acids, for example sodium laureth-13 carboxylate and sodium PEG-6 cocamide carboxylate,
Phosphorsäureester und Salze, wie beispielsweise DEA-Oleth-10-Phosphat und Di- laureth-4 Phosphat, Sulfonsäuren und Salze, wiePhosphoric acid esters and salts, such as, for example, DEA-oleth-10-phosphate and di-laureth-4 phosphate, Sulfonic acids and salts such as
1. Acyl-isethionate, z.B. Natrium-/ Ammoniumcocoyl-isethionat,1. acyl isethionates, e.g. Sodium / ammonium cocoyl isethionate,
2. Alkylarylsulfonate,2. alkylarylsulfonates,
3. Alkylsulfonate, beispielsweise Natriumcocosmonoglyceridsulfat, Natrium Cι2-14 Olefin-sulfonat, Natriumlaurylsulfoacetat und Magnesium PEG-3 Cocamidsulfat,3. alkyl sulfonates, for example sodium coconut monoglyceride sulfate, sodium Cι 2-14 olefin sulfonate, sodium lauryl sulfoacetate and magnesium PEG-3 cocamide sulfate,
4. Sulfosuccinate, beispielsweise Dioctylnatriumsulfosuccinat, Dinatriumlaurethsul- fosuccinat, Dinatriumlaurylsulfosuccinat und Dinatriumundecylenamido MEA- Sulfosuccinat4. Sulfosuccinates, for example dioctyl sodium sulfosuccinate, disodium laureth sulfosuccinate, disodium lauryl sulfosuccinate and disodium undecylenamido MEA sulfosuccinate
sowie Schwefelsäureester, wieas well as sulfuric acid esters, such as
1. Alkylethersulfat, beispielsweise Natrium-, Ammonium-, Magnesium-, MIPA-, TIPA- Laurethsulfat, Natriummyrethsulfat und Natrium Cι2-13 Parethsulfat,1. alkyl ether sulfate, for example sodium, ammonium, magnesium, MIPA, TIPA laureth sulfate, sodium myreth sulfate and sodium Cι 2-13 pareth sulfate,
2. Alkylsulfate, beispielsweise Natrium-, Ammonium- und TEA- Laurylsulfat.2. Alkyl sulfates, for example sodium, ammonium and TEA lauryl sulfate.
B. Kationische TensideB. Cationic surfactants
Vorteilhaft zu verwendende kationische Tenside sindCationic surfactants to be used advantageously
1. Alkylamine,1. alkylamines,
2. Alkylimidazole,2. alkylimidazoles,
3. Ethoxylierte Amine.3. Ethoxylated amines.
Die große verbleibende Gruppe der quaternären Stickstofftenside wird durch die der Erfindung zugrundeliegende Wirkstoffgruppe repräsentiert.The large remaining group of quaternary nitrogen surfactants is represented by the group of active substances on which the invention is based.
C. Amphotere TensideC. Amphoteric surfactants
Vorteilhaft zu verwendende amphotere Tenside sindAmphoteric surfactants to be used advantageously
1. Acyl-/dialkylethylendiamin, beispielsweise Natriumacylamphoacetat, Dinatrium- acylamphodipropionat, Dinatriumalkylamphodiacetat, Natriumacylamphohydro- xypropylsulfonat, Dinatriumacylamphodiacetat und Natriumacylamphopropionat,1. acyl- / dialkylethylenediamine, for example sodium acylamphoacetate, disodium acylamphodipropionate, disodium alkylamphodiacetate, sodium acylamphohydroxypropylsulfonate, disodium acylamphodiacetate and sodium acylamphopropionate,
2. N-Alkylaminosäuren, beispielsweise Aminopropylalkylglutamid, Alkylaminopropi- onsäure, Natriumalkylimidodipropionat und Lauroamphocarboxyglycinat.2. N-alkylamino acids, for example aminopropylalkylglutamide, alkylaminopropionic acid, sodium alkylimidodipropionate and lauroamphocarboxyglycinate.
D. Nicht-ionische TensideD. Non-ionic surfactants
Vorteilhaft zu verwendende nicht-ionische Tenside sind 1. Alkohole,Non-ionic surfactants to be used advantageously 1. alcohols,
2. Alkanolamide, wie Cocamide MEA/ DEA/ MIPA,2. alkanolamides, such as cocamides MEA / DEA / MIPA,
3. Aminoxide, wie Cocoamidopropylaminoxid,3. amine oxides, such as cocoamidopropylamine oxide,
4. Ester, die durch Veresterung von Carbonsäuren mit Ethyienoxid, Glycerin, Sor- bitan oder anderen Alkoholen entstehen,4. esters which are formed by esterification of carboxylic acids with ethyl oxide, glycerol, sorbitol or other alcohols,
5. Ether, beispielsweise ethoxylierte/propoxylierte Alkohole, ethoxyiierte/ propoxy- lierte Ester, ethoxyiierte/ propoxylierte Glycerinester, ethoxyiierte/ propoxylierte Cholesterine, ethoxyiierte/ propoxylierte Triglyceridester, ethoxyliertes propoxy- liertes Lanolin, ethoxyiierte/ propoxylierte Polysiloxane, propoxylierte POE-Ether und Alkylpolyglycoside wie Laurylglucosid, Decylglycosid und Cocoglycosid.5. ethers, for example ethoxylated / propoxylated alcohols, ethoxyated / propoxylated esters, ethoxyated / propoxylated glycerol esters, ethoxyated / propoxylated cholesterols, ethoxylated / propoxylated triglyceride esters, ethoxylated propoxylated lanolin, ethoxylated / propoxylated polysiloxanes and propoxylated POs Lauryl glucoside, decyl glycoside and cocoglycoside.
6. Sucroseester, -Ether6. sucrose esters, ether
7 Polyglycerinester, Diglycerinester, Monoglycerinester 8. Methylglucosester, Ester von Hydroxysäuren7 polyglycerol esters, diglycerol esters, monoglycerol esters 8. methyl glucose esters, esters of hydroxy acids
Vorteilhaft ist erfindungsgemäß insbesondere die Verwendung einer Kombination von quaternären Stickstoffverbindungen mit einem oder mehreren amphoteren Tensiden und/oder mit einem oder mehreren nicht-ionischen Tensiden.According to the invention, it is particularly advantageous to use a combination of quaternary nitrogen compounds with one or more amphoteric surfactants and / or with one or more nonionic surfactants.
Je nach Kompatibilität der nicht-kationischen Tenside mit den erfindungsgemäßen quaternären Stickstoffverbindung kann ihre Konzentration in Zubereitungen gemäß der Erfindung bis zu 80 Gew.-% betragen, bezogen auf das Gesamtgewicht der Zubereitungen.Depending on the compatibility of the non-cationic surfactants with the quaternary nitrogen compound according to the invention, their concentration in preparations according to the invention can be up to 80% by weight, based on the total weight of the preparations.
Zusätzlich zu den genannten Bestandteilen können den erfindungsgemäßen dermatologischen Zubereitungen, deren pH-Wert vorzugsweise z.B. durch übliche Puffergemische auf 4,0 bis 7,5 insbesondere 5,0 bis 6,5, eingestellt wird, Parfüm, Farbstoffe, Antioxidantien, Suspendiermittel, Puffergemische oder andere übliche kosmetische oder dermatologische Grundstoffe beigemischt werden.In addition to the ingredients mentioned, the dermatological preparations according to the invention, the pH of which is preferably e.g. is adjusted to 4.0 to 7.5, in particular 5.0 to 6.5, by customary buffer mixtures, perfume, dyes, antioxidants, suspending agents, buffer mixtures or other customary cosmetic or dermatological base materials are added.
Erfindungsgemäß können als günstige Antioxidantien alle für kosmetische und/oder dermatologische Anwendungen geeigneten oder gebräuchlichen Antioxidantien verwendet werden.According to the invention, all the antioxidants suitable or customary for cosmetic and / or dermatological applications can be used as favorable antioxidants.
Es ist auch von Vorteil, den erfindungsgemäßen Zubereitungen Antioxidantien zuzusetzen. Vorteilhaft werden die Antioxidantien gewählt aus der Gruppe bestehend aus Aminosäuren (z.B. Glycin, Histidin, Tyrosin, Tryptophan) und deren Derivate, Imida- zole (z.B. Urocaninsäure) und deren Derivate, Peptide wie D,L-Carnosin, D-Carnosin, L-Carnosin und deren Derivate (z.B. Anserin), Carotinoide, Carotine (z.B. α-Carotin, ß- Carotin, Lycopin) und deren Derivate, Chlorogensäure und deren Derivate, Lipon- säure und deren Derivate (z.B. Dihydroliponsäure), Aurothioglucose, Propylthiouracil und andere Thiole (z.B. Thioredoxin, Glutathion, Cystein, Cystin, Cystamin und deren Glycosyl-, N-Acetyl-, Methyl-, Ethyl-, Propyl-, Amyl-, Butyl- und Lauryl-, Paimitoyl-, Oleyl-, γ-Linoleyl-, Cholesteryl- und Glycerylester) sowie deren Salze, Dilaurylthiodi- propionat, Distearylthiodipropionat, Thiodipropionsäure und deren Derivate (Ester, Ether, Peptide, Lipide, Nukleotide, Nukleoside und Salze) sowie Sulfoximinverbindun- gen (z.B. Buthioninsulfoximine, Homocysteinsulfoximin, Buthioninsulfone, Penta-, Hexa-, Heptathioninsulfoximin) in sehr geringen verträglichen Dosierungen (z.B. pmol bis μmol/kg), ferner (Metall)-Chelatoren (z.B. α-Hydroxyfettsäuren, Palmitinsäure, Phytinsäure, Lactoferrin), α-Hydroxysäuren (z.B. Cftronensäure, Milchsäure, Apfelsäure), Huminsäure, Gallensäure, Gallenextrakte, Bilirubin, Biliverdin, EDTA, EGTA und deren Derivate, ungesättigte Fettsäuren und deren Derivate (z.B. γ-Linolensäure, Li- nolsäure, Ölsäure), Folsäure und deren Derivate, Ubichinon und Ubichinol und deren Derivate, Vitamin C und Derivate (z.B. Ascorbylpalmitat, Mg-Ascorbylphosphat, As- corbylacetat), Tocopherole und Derivate (z.B. Vitamin-E-acetat), Vitamin A und Derivate (Vitamin-A-palmitat) sowie Koniferylbenzoat des Benzoeharzes, Rutinsäure und deren Derivate, α-Glycosylrutin, Ferulasäure, Furfurylidenglucitol, Carnosin, Butylhy- droxytoluol, Butylhydroxyanisol, Nordihydroguajakharzsäure, Nordihydroguajaretsäu- re, Trihydroxybutyrophenon, Harnsäure und deren Derivate, Mannose und deren Derivate, Zink und dessen Derivate (z.B. ZnO, ZnSO4) Selen und dessen Derivate (z.B. Selenmethionin), Stiibene und deren Derivate (z.B. Stilbenoxid, Trans-Stilbenoxid) und die erfindungsgemäß geeigneten Derivate (Salze, Ester, Ether, Zucker, Nukleotide, Nukleoside, Peptide und Lipide) dieser genannten Wirkstoffe.It is also advantageous to add antioxidants to the preparations according to the invention. The antioxidants are advantageously selected from the group consisting of Amino acids (eg glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (eg urocanic acid) and their derivatives, peptides such as D, L-carnosine, D-carnosine, L-carnosine and their derivatives (eg anserine), carotenoids , Carotenes (e.g. α-carotene, ß-carotene, lycopene) and their derivatives, chlorogenic acid and their derivatives, liponic acid and their derivatives (e.g. dihydroliponic acid), aurothioglucose, propylthiouracil and other thiols (e.g. thioredoxin, glutathione, cysteine, cystine, Cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, paimitoyl, oleyl, γ-linoleyl, cholesteryl and glyceryl esters) and their salts, dilaurylthiodi - propionate, distearyl thiodipropionate, thiodipropionic acid and their derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) as well as sulfoximine compounds (eg buthioninsulfoximines, homocysteine sulfoximine, buthioninsulfones, penta-, hexa-, heptathioninsulfoximine doses) in very low dosages (e.g. pmol to μmol / kg), also (metal) chelators (e.g. α-hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), α-hydroxy acids (e.g. cftronic acid, lactic acid, malic acid), humic acid, bile acid, bile extracts, bilirubin, biliverdin, EDTA, EGTA and their derivatives, unsaturated fatty acids and their derivatives (eg γ-linolenic acid, linoleic acid, oleic acid), folic acid and their derivatives, ubiquinone and ubiquinol and their derivatives, vitamin C and derivatives (eg ascorbyl palmitate, Mg-ascorbyl phosphate, as - corby acetate), tocopherols and derivatives (eg vitamin E acetate), vitamin A and derivatives (vitamin A palmitate) as well as coniferyl benzoate of benzoin, rutinic acid and its derivatives, α-glycosyl rutin, ferulic acid, furfurylidene glucitol, carnosine, butyl hyroxroxy toluene , Butylated hydroxyanisole, nordihydroguajak resin acid, nordihydroguajaretic acid, trihydroxybutyrophenone, uric acid and its derivatives, mannose and its derivatives, zinc and its derivatives (eg ZnO, ZnSO 4 ) selenium and its derivatives (for example selenium methionine), stiibenes and their derivatives (for example stilbene oxide, trans-stilbene oxide) and the derivatives (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids) of these active substances which are suitable according to the invention.
Die Menge der Antioxidantien (eine oder mehrere Verbindungen) in den Zubereitungen beträgt vorzugsweise 0,001 bis 30 Gew.-%, besonders bevorzugt 0,05 - 20 Gew.- %, insbesondere 1 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitung.The amount of the antioxidants (one or more compounds) in the preparations is preferably 0.001 to 30% by weight, particularly preferably 0.05-20% by weight, in particular 1-10% by weight, based on the total weight of the preparation .
Sofern Vitamin E und/oder dessen Derivate das oder die Antioxidantien darstellen, ist vorteilhaft, deren jeweilige Konzentrationen aus dem Bereich von 0,001 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Formulierung, zu wählen. Sofern Vitamin A, bzw. Vitamin-A-Derivate, bzw. Carotine bzw. deren Derivate das oder die Antioxidantien darstellen, ist vorteilhaft, deren jeweilige Konzentrationen aus dem Bereich von 0,001 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Formulierung, zu wählen.If vitamin E and / or its derivatives represent the antioxidant (s), it is advantageous to choose their respective concentrations from the range of 0.001-10% by weight, based on the total weight of the formulation. If vitamin A or vitamin A derivatives or carotenes or their derivatives represent the antioxidant or antioxidants, it is advantageous to have their respective concentrations in the range from 0.001-10% by weight, based on the total weight of the formulation, to choose.
Es ist für die vorliegende Erfindung vorteilhaft, daß der pH-Wert der erfindungsgemäßen dermatologischen Zubereitungen kleiner als 8 ist. pH-Werte, die leicht höher sind als 7, aber kleiner als 7,5 können dabei im allgemeinen toleriert werden. Jedenfalls ist für ein gegebenes Fettsäuregemisch im Einzelfalle durch einfaches Ausprobieren, ohne erfinderisches Dazutun, leicht zu ermitteln, welche exakte obere pH-Grenze zu beachten ist.It is advantageous for the present invention that the pH of the dermatological preparations according to the invention is less than 8. pH values that are slightly higher than 7 but less than 7.5 can generally be tolerated. In any case, it is easy to determine for a given fatty acid mixture by simply trying it out, without inventive step, which exact upper pH limit is to be observed.
Vorteilhaft wird der pH-Wert der erfindungsgemäßen Formulierungen im sauren bis sehr schwach alkalischen Bereich kleiner als 8 eingestellt, bevorzugt von 4,0 - 7,5 , besonders bevorzugt von 5,0 - 6,5.The pH of the formulations according to the invention is advantageously adjusted to less than 8 in the acidic to very weakly alkaline range, preferably from 4.0 to 7.5, particularly preferably from 5.0 to 6.5.
Die jeweils einzusetzenden Mengen an Hilfs- Zusatz- und Trägerstoffen und gegebenenfalls Parfüm können in Abhängigkeit von der Art des jeweiligen Produktes vom Fachmann durch einfaches Ausprobieren leicht ermittelt werden.The amounts of auxiliary additives and carriers and possibly perfume to be used can easily be determined by a person skilled in the art by simply trying them out, depending on the type of product in question.
Die Herstellung der erfindungsgemäßen dermatologischen Zubereitungen erfolgt, abgesehen von speziellen Zubereitungen, die in den Beispielen jeweils gesondert vermerkt sind, in üblicher Weise, zumeist durch einfaches Vermischen unter Rühren, gegebenenfalls unter leichter Erwärmung. Sie bietet keine Schwierigkeiten. Für Emulsionen werden Fettphase und die Wasserphase z.B. separat, gegebenenfalls unter Erwärmen hergestellt und dann emulgiert.With the exception of special preparations, each of which is noted separately in the examples, the dermatological preparations according to the invention are prepared in a customary manner, usually simply by mixing with stirring, optionally with gentle heating. It has no difficulties. For emulsions fat phase and water phase e.g. prepared separately, optionally with heating and then emulsified.
Ansonsten sind die üblichen Maßregeln für das Zusammenstellen von galenischen Formulierungen zu beachten, die dem Fachmann geläufig sind.Otherwise, the usual measures for compiling galenic formulations, which are familiar to the person skilled in the art, must be observed.
Sollen die erfindungsgemäßen Kombinationen in Puder eingearbeitet werden, so können die Suspensionsgrundlagen dafür vorteilhaft gewählt werden aus der Gruppe Kieselsäuregele (z.B. solche die unter dem Handelsnamen Aerosil® erhältlich sind), Kieselgur, Talkum, modifizierte Stärke, Titandioxid, Seidenpulver, Nylonpulver, Poly- ethylenpulver und verwandten Stoffen.If the combinations according to the invention are to be incorporated into powder, the suspension bases for this can advantageously be selected from the group Silicic acid gels (eg those available under the trade name Aerosil®), kieselguhr, talc, modified starch, titanium dioxide, silk powder, nylon powder, polyethylene powder and related substances.
Es folgen vorteilhafte Ausführungsbeispiele der vorliegenden Erfindung. Die Mengenangaben beziehen sich stets auf Gewichts-%, wenn nichts Anderes angegeben wird. Advantageous exemplary embodiments of the present invention follow. The quantities always relate to% by weight, unless otherwise stated.
Beispiel 1example 1
W/O CremeW / O cream
Gew.%% By weight
Paraffinöl (DAB 9) 10,00Paraffin oil (DAB 9) 10.00
Petrolatum 4,00Petrolatum 4.00
Wollwachsalkohol 1,00Wool wax alcohol 1.00
PEG-7-Hydriertes Ricinusöl 3,00PEG-7 hydrogenated castor oil 3.00
Aluminiumstearat 0,40Aluminum stearate 0.40
Polyaminopropylbiguanid 0,20Polyaminopropyl biguanide 0.20
Glycerin 2,00Glycerin 2.00
Konservierungsmittel, Farbstoffe, Parfüm q.s.Preservatives, dyes, perfume q.s.
Wasser ad 100,00Water ad 100.00
Beispiel 2Example 2
W/O LotionW / O lotion
Gew.-%% By weight
Paraffinöl (DAB 9) 20,00Paraffin oil (DAB 9) 20.00
Petrolatum 4,00Petrolatum 4.00
Glucosesesquiisostearat 2,00Glucose sesquiisostearate 2.00
Aluminiumstearat 0,40Aluminum stearate 0.40
Cetyltrimethylammoniumchlorid 0,10 α-Tocopherylacetat 1 ,00Cetyltrimethylammonium chloride 0.10 α-tocopheryl acetate 1.00
Glycerin 5,00Glycerin 5.00
Konservierungsmittel, Farbstoffe, Parfüm q.s.Preservatives, dyes, perfume q.s.
Wasser ad 100,00 Beispiel 3Water ad 100.00 Example 3
O/W LotionO / W lotion
Gew.-%% By weight
Paraffinöl (DAB 9) 8,00Paraffin oil (DAB 9) 8.00
Isopropylpalmrtat 3,00Isopropyl palmate 3.00
Petrolatum 4,00Petrolatum 4.00
Cetylstearylalkohol 2,00Cetylstearyl alcohol 2.00
PEG-40 Ricinusöl 0,50PEG-40 castor oil 0.50
Natriumcetylstearylsulfat 0,50Sodium cetyl stearyl sulfate 0.50
Natrium Carbomer 0,40Sodium carbomer 0.40
Polyaminopropylbiguanid 0,20Polyaminopropyl biguanide 0.20
Glycerin 3,00 α-Tocopherol 0,20Glycerin 3.00 α-tocopherol 0.20
Octylmethoxycinnamat 5,00Octyl methoxycinnamate 5.00
Butylmethoxydibenzoylmethan 1,00Butyl methoxydibenzoyl methane 1.00
Konservierungsmittel, Farbstoffe, Parfüm q.s.Preservatives, dyes, perfume q.s.
Wasser ad 100,00Water ad 100.00
Beispiel 4Example 4
O/W CremeO / W cream
Gew.-%% By weight
Paraffinöl (DAB 9) 7,00Paraffin oil (DAB 9) 7.00
Avocadoöl 4,00Avocado oil 4.00
Glycerylmonostearat 2,00Glyceryl monostearate 2.00
Cetyltrimethylammoniumchlorid 0,10Cetyltrimethylammonium chloride 0.10
Titandioxid 1 ,00Titanium dioxide 1.00
Natriumlactat 3,00Sodium lactate 3.00
Glycerin 3,00Glycerin 3.00
Konservierungsmittel, Farbstoffe, Parfüm q.s.Preservatives, dyes, perfume q.s.
Wasser ad 100,00 Beispiel 5Water ad 100.00 Example 5
O/W-CremeO / W cream
Gew.-%% By weight
Quartβrnium-5 3,50Quartzrnium-5 3.50
Paraffinöl, subliquidum 10,00Paraffin oil, subliquidum 10.00
Cetearylalkohol 2,00Cetearyl alcohol 2.00
Hydrierte Kokosfettsäureglyceride 0,50Hydrogenated coconut fatty acid glycerides 0.50
Dimethicone 0,75Dimethicone 0.75
Glycerin 20,00Glycerin 20.00
Tocopherolacetat 0,50Tocopherol acetate 0.50
Polyaminopropylbiguanid 0,20Polyaminopropyl biguanide 0.20
Konservierungsmittel, Farbstoffe, Parfüm q.s. Wasser ad 100,00Preservatives, dyes, perfume q.s. Water ad 100.00
Beispiel 6Example 6
O/W-CremeO / W cream
Gew.-%% By weight
Quarternium-5 3,50Quarternium-5 3.50
Paraffinöl, subliquidum 10,00Paraffin oil, subliquidum 10.00
Cetearylalkohol 2,00Cetearyl alcohol 2.00
Hydrierte Kokosfettsäureglyceride 0,50Hydrogenated coconut fatty acid glycerides 0.50
Dimethicone 0,75Dimethicone 0.75
Glycerin 20,00Glycerin 20.00
Tocopherolacetat 0,50Tocopherol acetate 0.50
Konservierungsmittel, Farbstoffe, Parfüm q.s.Preservatives, dyes, perfume q.s.
Wasser ad 100,00 Beispiel 7Water ad 100.00 Example 7
Liposomenhaltiges GelGel containing liposomes
Gew.-%% By weight
Lecithin 6,00Lecithin 6.00
Schibutter 3,00Ski butter 3.00
Cetyltrimethylammoniumchlorid 0,10 α-Tocopherol 0,20Cetyltrimethylammonium chloride 0.10 α-tocopherol 0.20
Biotin 0,08Biotin 0.08
Natriumeitrat 0,50Sodium citrate 0.50
Glycin 0,20Glycine 0.20
Harnstoff 0,20Urea 0.20
Natrium PCA 0,50Sodium PCA 0.50
Hydrolysiertes Kollagen 2,00Hydrolyzed collagen 2.00
Xanthan Gummi 1,40Xanthan gum 1.40
Sorbrtol 3,00Sorbrtol 3.00
Konservierungsmittel, Farbstoffe, Parfüm q.s.Preservatives, dyes, perfume q.s.
Wasser ad 100,00Water ad 100.00
Beispiel 8Example 8
Gelgel
Gew.-%% By weight
Carbopol 934 P 2,00Carbopol 934 P 2.00
Triethanolamin 3,00Triethanolamine 3.00
Polyaminopropylbiguanid 0,20 α-Tocopherylacetat 0,20Polyaminopropyl biguanide 0.20 α-tocopheryl acetate 0.20
Polyoxyethylensorbitanfettsäureester (Tween 20) 0,50Polyoxyethylene sorbitan fatty acid ester (Tween 20) 0.50
Glycerin 2,00Glycerin 2.00
Natrium PCA 0,50Sodium PCA 0.50
Hydrolysiertes Kollagen 2,00Hydrolyzed collagen 2.00
Konservierungsmittel, Farbstoffe, Parfüm q.s.Preservatives, dyes, perfume q.s.
Wasser ad 100,00 Water ad 100.00

Claims

Patentansprüche: Claims:
1. Verwendung quaternärer Stickstoffverbindungen zur Prophylaxe und Behandlung des superinfizierten atopischen Ekzems.1. Use of quaternary nitrogen compounds for the prophylaxis and treatment of superinfected atopic eczema.
2. Verwendung nach Anspruch 1, dadurch gekennzeichnet, daß die quaternären Stickstoffverbindungen in Konzentrationen von 0,01 - 99,00 Gew.-%, bevorzugt 0,05 - 50,00 Gew.-%, besonders bevorzugt 0,1 - 10,00 Gew.-%, jeweils bezogen auf das Gesamtgewicht der Zusammensetzung, vorliegen. 2. Use according to claim 1, characterized in that the quaternary nitrogen compounds in concentrations of 0.01-99.00% by weight, preferably 0.05-50.00% by weight, particularly preferably 0.1-10, 00 wt .-%, based in each case on the total weight of the composition.
EP99938370A 1998-08-19 1999-07-29 Use of quaternary nitrogen compounds for prophylaxis or treatment of superinfected atopic eczema Withdrawn EP1104295A1 (en)

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DE19918324A1 (en) * 1999-04-22 2000-10-26 Mann Gerhard Chem Pharm Fab Bactericidal, virucidal, fungicidal and antiprotozoal pharmaceutical composition, especially for ophthalmological use, contains benzalkonium salt
DE10140361B4 (en) * 2001-08-17 2009-07-16 Rüdiger Bode Use of a preparation containing biguanides for hoof care
DE10147186A1 (en) * 2001-09-25 2003-04-24 Beiersdorf Ag Synergistic antimicrobial composition, useful e.g. as cosmetic preservative and for treating skin disorders, comprises polyhexamethylene biguanide and distearyldimethylammonium chloride
WO2006054312A1 (en) * 2004-11-16 2006-05-26 Munisekhar Medasani Ammonium compounds for treating psoriasis and eczema
US20190125734A1 (en) * 2016-05-09 2019-05-02 Nanoegg Research Laboratories, Inc. Composition for treating or preventing atopic dermatitis

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JPS62126121A (en) * 1985-11-26 1987-06-08 Kiyoshi Nakajima Remedy for athlete's foot
DE3603859A1 (en) * 1986-02-07 1987-08-13 Roehm Pharma Gmbh WASHABLE TOPICAL PREPARATION FOR THERAPY OF PSORIASIS
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