DE19837549A1 - Use of quaternary nitrogen compounds for treatment and prevention of atopic eczema - Google Patents
Use of quaternary nitrogen compounds for treatment and prevention of atopic eczemaInfo
- Publication number
- DE19837549A1 DE19837549A1 DE1998137549 DE19837549A DE19837549A1 DE 19837549 A1 DE19837549 A1 DE 19837549A1 DE 1998137549 DE1998137549 DE 1998137549 DE 19837549 A DE19837549 A DE 19837549A DE 19837549 A1 DE19837549 A1 DE 19837549A1
- Authority
- DE
- Germany
- Prior art keywords
- acid
- sodium
- derivatives
- oil
- esters
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 229910017464 nitrogen compound Inorganic materials 0.000 title claims abstract description 10
- 150000002830 nitrogen compounds Chemical group 0.000 title claims abstract description 10
- 206010012438 Dermatitis atopic Diseases 0.000 title claims abstract description 8
- 201000008937 atopic dermatitis Diseases 0.000 title claims abstract description 8
- 238000011282 treatment Methods 0.000 title claims abstract description 6
- 208000010668 atopic eczema Diseases 0.000 title abstract description 9
- 230000002265 prevention Effects 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 claims description 16
- 238000011321 prophylaxis Methods 0.000 claims description 2
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- -1 ether sulfates Chemical class 0.000 description 26
- 238000002360 preparation method Methods 0.000 description 22
- 239000011734 sodium Substances 0.000 description 17
- 229910052708 sodium Inorganic materials 0.000 description 16
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 15
- 239000003921 oil Substances 0.000 description 13
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- 150000003856 quaternary ammonium compounds Chemical class 0.000 description 8
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- WAYINTBTZWQNSN-UHFFFAOYSA-N 11-methyldodecyl 3,5,5-trimethylhexanoate Chemical compound CC(C)CCCCCCCCCCOC(=O)CC(C)CC(C)(C)C WAYINTBTZWQNSN-UHFFFAOYSA-N 0.000 description 3
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- CQOVPNPJLQNMDC-ZETCQYMHSA-N carnosine Chemical compound [NH3+]CCC(=O)N[C@H](C([O-])=O)CC1=CNC=N1 CQOVPNPJLQNMDC-ZETCQYMHSA-N 0.000 description 3
- RLGQACBPNDBWTB-UHFFFAOYSA-N cetyltrimethylammonium ion Chemical compound CCCCCCCCCCCCCCCC[N+](C)(C)C RLGQACBPNDBWTB-UHFFFAOYSA-N 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
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- REZZEXDLIUJMMS-UHFFFAOYSA-M dimethyldioctadecylammonium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCCC[N+](C)(C)CCCCCCCCCCCCCCCCCC REZZEXDLIUJMMS-UHFFFAOYSA-M 0.000 description 3
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- QAOJADINKLMTRR-UHFFFAOYSA-N octan-3-yl 16-methylheptadecanoate Chemical compound CCCCCC(CC)OC(=O)CCCCCCCCCCCCCCC(C)C QAOJADINKLMTRR-UHFFFAOYSA-N 0.000 description 3
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- REZOIPSCCRVWNN-UHFFFAOYSA-N tetratriacontan-17-ol Chemical compound CCCCCCCCCCCCCCCCCC(O)CCCCCCCCCCCCCCCC REZOIPSCCRVWNN-UHFFFAOYSA-N 0.000 description 1
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- ZCIHMQAPACOQHT-ZGMPDRQDSA-N trans-isorenieratene Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/c1c(C)ccc(C)c1C)C=CC=C(/C)C=Cc2c(C)ccc(C)c2C ZCIHMQAPACOQHT-ZGMPDRQDSA-N 0.000 description 1
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- 229940040064 ubiquinol Drugs 0.000 description 1
- QNTNKSLOFHEFPK-UPTCCGCDSA-N ubiquinol-10 Chemical compound COC1=C(O)C(C)=C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)C(O)=C1OC QNTNKSLOFHEFPK-UPTCCGCDSA-N 0.000 description 1
- 229940035936 ubiquinone Drugs 0.000 description 1
- GAAKLDANOSASAM-UHFFFAOYSA-N undec-10-enoic acid;zinc Chemical compound [Zn].OC(=O)CCCCCCCCC=C GAAKLDANOSASAM-UHFFFAOYSA-N 0.000 description 1
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- OENHQHLEOONYIE-JLTXGRSLSA-N β-Carotene Chemical compound CC=1CCCC(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C OENHQHLEOONYIE-JLTXGRSLSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/74—Synthetic polymeric materials
- A61K31/785—Polymers containing nitrogen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/14—Quaternary ammonium compounds, e.g. edrophonium, choline
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Cosmetics (AREA)
Abstract
Description
Die gesunde menschliche Haut ist mit einer Vielzahl nichtpathogener Mikroorganis men besiedelt. Diese sogenannte Mikroflora der Haut ist nicht nur unschädlich, sie stellt einen wichtigen Schutz zur Abwehr opportunistischer oder pathogener Keime dar.The healthy human skin is made up of a variety of non-pathogenic microorganisms populated. This so-called microflora of the skin is not only harmless to them provides important protection against opportunistic or pathogenic germs represents.
Bei bestehendem Primärinfekt, d. h., der normalen Keimbesiedelung der Haut, eintre tende Neuinfektion mit hohen Keimzahlen eines oder mehrerer oft physiologischer Er reger, beispielsweise Staphylokokken, oft aber auch unphysiologischer Erreger, bei spielsweise 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 über wuchert.In case of primary infection, d. h., the normal germ colonization of the skin, eintre tende new infection with high germ counts of one or more often physiological Er such as staphylococci, but often also unphysiological pathogens For example, Candida albicans, when encountering unfavorable influences, a "Superinfection" of the affected skin occur. The normal microflora of the skin (or of another body organ) is thereby literally over from the secondary exciter overgrown.
Solche Superinfektionen können sich, in Abhängigkeit vom betreffenden Keim, in günstig verlaufenden Fällen in unangenehmen Hauterscheinungen (Juckreiz, unschö nes 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.Such superinfections can, depending on the germ concerned, in favorable cases in unpleasant skin conditions (itching, unschö external appearance). In unfavorable cases they can but lead to extensive destruction of the skin, in the worst case even in the Culminate 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 Erscheinungs bild 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.Such superinfections are found in a variety of dermatological diseases especially atopic eczema, also neurodermatitis observed. The ato Eczema generally begins with itching, redness, scaling, and oozing Crust formation, wherein the infestation of the skin parts depending on the age of the patient assumes certain characteristic accumulations. Complications of appearance Pictures of atopic eczema often present superinfections with different kei in particular Staphylococcus aureus, of which approximately 90% of all Atopiker with eczematous expression are affected.
Herkömmliche Behandlungsmethoden umfassen daher neben entzündungshemmen den Wirkstoffen (z. B. Hydrocortison) auch Externa wie verschiedene Antibiotika im engeren Sinne oder Wirkstoffe mit antimikrobiellen bzw. antimycotischen Eigen schaften im weiteren Sinne (z. B. Gentianaviolett).Conventional treatments therefore include in addition to anti-inflammatory the active ingredients (eg hydrocortisone) also Externa as various antibiotics in the narrower sense or agents with antimicrobial or antimycotic properties in the wider sense (eg 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).The conventionally used agents but usually have the disadvantage that they either more or less serious side effects, resistance formation or incompatibilities, or that they have non-cosmetic sensations (eg 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.So it is in some cases easily possible to super infections with antibiotics too combat, but usually such substances have the disadvantage unpleasant Side effects. For example, patients are often allergic to penicillins, Therefore, such treatment is prohibited in such a case would. Furthermore, topically administered antibiotics have the disadvantage that they Relieve skin flora not only from the secondary pathogen, but also in itself physiological skin flora severely impair and the natural healing process on this way is slowed down again.
Die Reduktion eines klinisch ausgeprägten atopischen Ekzems indes war mit Wirk stoffen und Zubereitungen des Standes der Technik bisher - wenn überhaupt erreich bar - stets mit erheblichen Unannehmlichkeiten verbunden.The reduction of clinically pronounced atopic eczema, however, was with Wirk so far, if at all achievable, prior art materials and preparations bar - always associated with significant inconvenience.
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 overcome the disadvantages of the prior art and substances and preparations containing such substances, to To make superinfections cured by using them can, wherein the physiological skin flora suffers no significant loss.
Darüberhinaus war es Aufgabe der vorliegenden Erfindung, Substanzen und kosme tische bzw. dermatologische Zubereitungen, solche Substanzen enthaltend, zur Ver fügung zu stellen, die prophylaktisch gegen Superinfektionen wirken. Moreover, it was an object of the present invention, substances and kosme tables or dermatological preparations containing such substances, for Ver to provide prophylactic against superinfections.
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.It has surprisingly been found, and therein lies the solution of this problem that the Use of quaternary nitrogen compounds for the prophylaxis and treatment of Superinfected atopic dermatitis remedies the disadvantages of the prior art.
Im Rahmen der Offenbarung zur vorliegenden Erfindung wird der Begriff "quaternäre Ammoniumverbindungen" gelegentlich synonym für "quaternäre Stickstoffverbindun gen" angewandt.In the context of the disclosure of the present invention, the term "quaternary Ammonium compounds "occasionally synonymous with" quaternary nitrogen compounds "applied.
Gemäß der Erfindung sind quaternäre Ammoniumverbindungen bzw. Zubereitungen, quaternäre Ammoniumverbindungen enthaltend, hervorragend geeignet, superinfi zierte atopische Ekzeme zu reduzieren bzw. die Symptome superinfizierter Ekzeme zu lindern.According to the invention, quaternary ammonium compounds or preparations, containing quaternary ammonium compounds, excellently suited, superinfi reduced atopic eczema or the symptoms of superinfected eczema to alleviate.
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 following basic schemes:
Quaternäre Ammoniumverbindungen mit mindestens einer langen Alkyl-Kette, wie beispielsweise das Distearyldimethylammoniumchlorid (DSDMA), besitzen oberflä chenaktive 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 fin den daher Verwendung in fungiziden und bakteriziden Desinfektionsmitteln oder als Algizide. Quaternary ammonium compounds having at least one long alkyl chain, such as for example distearyldimethylammonium chloride (DSDMA) have oberflä chenaktiven properties and are therefore used as cationic surfactants, eg. B. as a wetting agent, Emulsifiers, antistatic agents and used as a plasticizer. Mainly short-chain Quaternary ammonium compounds have microbicidal properties and fin Therefore, use in fungicidal and bactericidal disinfectants or as Algaecides.
Die erfindungsgemäß verwendeten quatemären 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 ferner bevorzugt gewählt werden aus der Gruppe der quaternären Ammoniumverbindungen, insbesondere Benzyltrialkylammoniumchloride oder -bromide, wie beispielsweise Ben zyldimethylstearylammoniumchlorid, ferner Alkyltrialkylammoniumsalze, beispielswei se beispielsweise Cetyltrimethylammoniumchlorid oder -bromid, Alkyldimethylhydro xyethylammoniumchloride oder -bromide, Dialkyldimethylammoniumchloride oder -bromide, Alkylamidethyltrimethylammoniumethersulfate, Alkylpyridiniumsalze, bei spielsweise Lauryl- oder Cetylpyrimidiniumchlorid, Imidazolinderivate und Verbindun gen mit kationischem Charakter wie Aminoxide, beispielsweise Alkyldimethylaminoxi de oder Alkylaminoethyldimethylaminoxide. Vorteilhaft sind insbesondere Cetyltrime thylammoniumsalze zu verwenden, wie auch Polyaminoalkylbiguanide, z. B. Poly aminopropylbiguanid.The quaternary ammonium compounds used according to the invention can are advantageously selected from the group of quaternary surfactants. Are advantageous for example, alkylbetaine, alkylamidopropylbetaine and alkyl-amidopropylhydroxy sulfain. The cationic surfactants used according to the invention can furthermore are preferably selected from the group of quaternary ammonium compounds, in particular Benzyltrialkylammoniumchloride or bromides, such as Ben cyldimethylstearylammonium chloride, further Alkyltrialkylammoniumsalze, beispielswei For example, cetyltrimethylammonium chloride or bromide, alkyldimethylhydro xyethylammonium chlorides or bromides, dialkyldimethylammonium chlorides or bromides, alkylamidoethyltrimethylammonium ether sulfates, alkylpyridinium salts For example, lauryl or cetylpyrimidinium chloride, imidazoline derivatives and Verbindun with cationic character such as amine oxides, for example Alkyldimethylaminoxi de or alkylaminoethyldimethylamine oxides. Cetyl trimes are particularly advantageous to use thylammonium salts, as well as polyaminoalkylbiguanides, z. B. poly aminopropylbiguanid.
Die erfindungsgemäßen Zubereitungen sind besonders vorteilhaft dadurch gekenn zeichnet, daß die die quatemären 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, vor liegen.The preparations according to the invention are particularly advantageously characterized records that the quaternary nitrogen compounds in concentrations of 0.001-99.00 wt%, preferably 0.01-50.00 wt%, more preferably 0.1-10.00 wt .-%, each based on the total weight of the composition before lie.
Erfindungsgemäße dermatologische Zubereitungen können in Form von Aerosolen, also aus Aerosolbehältern, Quetschflaschen oder durch eine Pumpvorrichtung ver sprühbaren 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. Crèmes 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 may be in the form of aerosols, So from aerosol containers, squeeze bottles or by a pumping ver sprayable preparations or in the form of by means of roll-on devices Applicable liquid compositions, but also in the form of normal For bottles and containers, W / O or O / W emulsions, eg. B. creams or Lotions. Furthermore, the preparations may advantageously be in the form of tinctures, Shampoos, washing, shower or bath preparations or powders are present.
Als übliche kosmetische Trägerstoffe zur Herstellung der erfindungsgemäßen derma tologischen 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 schleimbildende Stoffe und Verdickungsmittel, z. B. Hydroxyethyl- oder Hydroxypropylcellulose, Polyacrylsäure, Polyvinylpyrrolidon, daneben aber auch in kleinen Mengen cyclische Silikonöle (Polydimethylsiloxane) sowie flüssige Polymethylphenylsiloxane niedriger Viskosiät.As usual cosmetic carriers for the preparation derma the invention In addition to water, ethanol and isopropanol, glycerol may also be used for tological preparations and propylene glycol skin-care fat or fat-like substances, such as oleic acid decyl esters, cetyl alcohol, cetylstearyl alcohol and 2-octyldodecanol, in those for such Preparations are used in customary proportions and slime-forming Substances and thickeners, eg. Hydroxyethyl or hydroxypropyl cellulose, Polyacrylic acid, polyvinylpyrrolidone, but also in small quantities cyclic Silicone oils (polydimethylsiloxanes) as well as liquid polymethylphenylsiloxanes lower Viskosiät.
Die Lipidphase kann vorteilhaft gewählt werden aus folgender Substanzgruppe:
The lipid phase can advantageously be selected from the following substance group:
- - Mineralöle, Mineralwachse- mineral oils, mineral waxes
- - Öle, wie Triglyceride der Caprin- oder der Caprylsäure, vorzugsweise aber Ri zinusöl;- Oils, such as triglycerides of capric or caprylic, but preferably Ri zinusöl;
- - Fette, Wachse und andere natürliche und synthetische Fettkörper, vorzugs weise Ester von Fettsäuren mit Alkoholen niedriger C-Zahl, z. B. mit lsopro panol, Propylenglykol oder Glycerin, oder Ester von Fettalkoholen mit Alkan säuren niedriger C-Zahl oder mit Fettsäuren;- Fats, waxes and other natural and synthetic fats, preferably example, esters of fatty acids with alcohols of low C number, z. B. with isopro panol, propylene glycol or glycerol, or esters of fatty alcohols with alkane acids of low C number or with fatty acids;
- - Alkylbenzoate;- alkyl benzoate;
- - Silikonöle wie Dimethylpolysiloxane, Diethylpolysiloxane, Diphenylpolysiloxane sowie Mischformen daraus.- Silicone oils such as dimethylpolysiloxanes, diethylpolysiloxanes, diphenylpolysiloxanes and mixed forms thereof.
Die Ölphase von als Ölen, Emulsionen, Oleogelen bzw. Hydrodispersionen oder Lipo dispersionen vorliegenden Zubereitungen gemäß der Erfindung wird vorteilhaft ge wählt 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 Alkoho len einer Kettenlänge von 3 bis 30 C-Atomen, aus der Gruppe der Ester aus aromati schen 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 oleat, Erucylerucat sowie synthetische, halbsynthetische und natürliche Gemische sol cher Ester, z. B. Jojobaöl.The oil phase of as oils, emulsions, oleogels or hydrodispersions or lipo dispersions present compositions according to the invention is advantageous ge selects from the group of esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids of a chain length of 3 to 30 carbon atoms and saturated and / or unsaturated, branched and / or unbranched alcohol len of a chain length of 3 to 30 carbon atoms, from the group of esters of aromati carboxylic acids and saturated and / or unsaturated, branched and / or unbranched alcohols of a chain length of 3 to 30 carbon atoms. Such ester oils can then be advantageously selected from the group isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, Isooctyl stearate, isononyl stearate, isononyl isononanoate, 2-ethylhexyl palmitate, 2-ethylhe xyl laurate, 2-hexyldecyl stearate, 2-octyl dodecyl palmitate, oleyl oleate, oleyl erucate, erucyl oleate, erucyl erucate and synthetic, semi-synthetic and natural mixtures sol cher ester, z. B. jojoba oil.
Ferner kann die Ölphase vorteilhaft gewählt werden aus der Gruppe der verzweigten und unverzweigten Kohlenwasserstoffe und -wachse, der Silikonöle, der Dialkylether, der Gruppe der gesättigten oder ungesättigten, verzweigten oder unverzweigten Alko hole, 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, Erd nußöl, Rapsöl, Mandelöl, Palmöl, Kokosöl, Palmkernöl und dergleichen mehr, insbesondere Nachtkerzenöl und Borretschöl.Furthermore, the oil phase can be advantageously selected from the group of branched and unbranched hydrocarbons and waxes, the silicone oils, the dialkyl ether, the group of saturated or unsaturated, branched or unbranched alkoxy as well as the fatty acid triglycerides, namely the triglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids of a Chain length of 8 to 24, in particular 12-18 C atoms. The fatty acid triglycerides For example, they can be advantageously selected from the group of synthetic, semisynthetic and natural oils, e.g. As olive oil, sunflower oil, soybean oil, earth nut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm kernel oil and the like more, especially 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 vorteil haft sein, Wachse, beispielsweise Cetylpalmitat, als alleinige Lipidkomponente der Öl phase einzusetzen.Any mixtures of such oil and wax components are advantageous in Use of the present invention. It may also benefit if necessary be liable, waxes, such as 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, C12-15-Alkylbenzoat, Capryl-Caprinsäure-triglycerid, Dicaprylylether.Advantageously, the oil phase is selected from the group consisting of 2-ethylhexyl isostearate, octyldodanol, isotridecyl isononanoate, isoeicosane, 2-ethylhexyl cocoate, C 12-15 alkyl benzoate, caprylic capric acid triglyceride, dicaprylyl ether.
Besonders vorteilhaft sind Mischungen aus C12-15-Alkylbenzoat und 2-Ethylhexyliso stearat, Mischungen aus C12-15-Alkylbenzoat und lsotridecylisononanoat sowie Mi schungen aus C12-15-Alkylbenzoat, 2-Ethylhexylisostearat und lsotridecylisononanoat.Particularly advantageous are mixtures of C 12-15 alkyl benzoate and 2-Ethylhexyliso stearate, mixtures of C 12-15 alkyl benzoate and isotridecyl isononanoate and Mi mixtures of C 12-15 alkyl benzoate, 2-Ethylhexylisostearat and isotridecyl isononanoate.
Von den Kohlenwasserstoffen sind Paraffinöl, Squalan und Squalen vorteilhaft im Sin ne der vorliegenden Erfindung zu verwenden.Of the hydrocarbons, paraffin oil, squalane and squalene are beneficial in the sin ne of the present invention.
Vorteilhaft kann die Ölphase ferner einen Gehalt an cyclischen oder linearen Silikon ölen aufweisen oder vollständig aus solchen Ölen bestehen, wobei allerdings bevor zugt wird, außer dem Silikonöl oder den Silikonölen einen zusätzlichen Gehalt an an deren Ölphasenkomponenten zu verwenden.Advantageously, the oil phase may further contain cyclic or linear silicone have oils or consist entirely of such oils, although before is added, except the silicone oil or silicone oils to an additional content of to use their oil phase components.
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). Advantageously, cyclomethicone (octamethylcyclotetrasiloxane) is used as the invention used silicone oil. But other silicone oils are also beneficial For purposes of the present invention, for example Hexamethylcyclotrisi loxan, polydimethylsiloxane, poly (methylphenylsiloxane).
Besonders vorteilhaft sind ferner Mischungen aus Cyclomethicon und Isotridecyliso nonanoat, aus Cyclomethicon und 2-Ethylhexylisostearat.Furthermore, mixtures of cyclomethicone and isotridecyliso are particularly advantageous nonanoate, from cyclomethicone and 2-ethylhexyl isostearate.
Die wäßrige Phase der erfindungsgemäßen Zubereitungen enthält gegebenenfalls vorteilhaft Alkohole, Diole oder Polyole niedriger C-Zahl, sowie deren Ether, vorzugs weise 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 Verdickungsmittel, welches oder welche vorteil haft gewählt werden können aus der Gruppe Siliciumdioxid, 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 optionally contains advantageous alcohols, diols or polyols low C number, and their ethers, preferably Example, ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol Mo noethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or mono butyl ether, diethylene glycol monomethyl or monoethyl ether and analogous products, furthermore lower C number alcohols, e.g. As ethanol, isopropanol, 1,2-propanediol, glycerol and in particular one or more thickening agents, which or which advantage can be selected from the group silicon dioxide, aluminum silicates, poly saccharides or their derivatives, for. Hyaluronic acid, xanthan gum, hydroxypropene pylmethylcellulose, particularly advantageous from the group of polyacrylates, preferred a polyacrylate from the group of so-called carbopols, for example Car bopols of 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 according to the invention contain z. Natural or synthetic Waxes, fatty alcohols or fatty acid esters.
Als Treibmittel für erfindungsgemäße, aus Aerosolbehältern versprühbare dermatolo gische 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.As a propellant for inventive dermatolo sprayable from aerosol containers gische preparations are the usual known volatile, liquefied Propellants, for example hydrocarbons (propane, butane, isobutane) suitable, which can be used alone or mixed with each other. Also compressed air is advantageous to use.
Natürlich weiß der Fachmann, daß es an sich nichttoxische Treibgase gibt, die grund sätzlich 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 expert knows that there are nontoxic propellants per se, the reason addition would be suitable for the present invention, but because of questionable effect on the environment or other accompanying circumstances especially chlorofluorocarbons (CFCs).
Als Emulgatoren zur Herstellung der erfindungsgemäßen dermatologischen Zubere itungen, haben sich nichtionogene Typen, wie Polyoxyethylen-Fettalkoholether, z. B. Cetylstearylalkoholpolyethylenglykolether mit 12 bzw. 20 angelagerten Ethylenoxid- Einheiten pro Molekül, Cetostearylalkohol sowie Sorbitanester und Sorbitanester- Ethylenoxid-Verbindungen (z. B. Sorbitanmonostearat und Polyoxyethylensorbitan monostearat) und langkettige höhermolekulare wachsartige Polyglykolether als geeignet erwiesen.As emulsifiers for the preparation of dermatological Zubere invention nonionic types such as polyoxyethylene fatty alcohol ethers, e.g. B. Cetylstearyl alcohol polyethylene glycol ethers with 12 or 20 attached ethylene oxide Units per molecule, cetostearyl alcohol and sorbitan esters and sorbitan esters Ethylene oxide compounds (e.g., sorbitan monostearate and polyoxyethylene sorbitan monostearate) and long-chain higher molecular weight waxy polyglycol ethers as proved suitable.
Auch Reinigungsmittel können vorteilhafte Verkörperungen der vorliegenden Erfindung darstellen. Dies ist insbesondere daher vorteilhaft, da manche quaternäre Stickstoff verbindungen tensidische Eigenschaften aufweisen.Cleaning agents may also be advantageous embodiments of the present invention represent. This is particularly advantageous because some quaternary nitrogen compounds have surfactant properties.
Tenside sind amphiphile Stoffe, die organische, unpolare Substanzen in Wasser lö sen können. Sie sorgen, bedingt durch ihren spezifischen Molekülaufbau mit minde stens einem hydrophilen und einem hydrophoben Molekülteil, für eine Herabsetzung der Oberflächenspannung des Wassers, die Benetzung der Haut, die Erleichterung der Schmutzentfemung und -lösung, ein leichtes Abspülen und - je nach Wunsch - für Schaumregulierung.Surfactants are amphiphilic substances that dissolve organic, nonpolar substances in water sen. They provide, due to their specific molecular structure with minde at least one hydrophilic and one hydrophobic moiety, for a reduction the surface tension of the water, the wetting of the skin, the relief Dirt removal and solution, a gentle rinse and - as desired - for foam regulation.
Bei den hydrophilen Anteilen eines Tensidmoleküls handelt es sich meist um polare
funktionelle Gruppen, beispielweise -COO-, -OSO32-, -SO3 -, während die hydropho
ben 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 portions of a surfactant molecule are usually polar functional groups, for example -COO - , -OSO3 2- , -SO 3 - , while the hydropho ben parts are generally nonpolar hydrocarbon radicals. Surfactants are generally classified according to the nature and charge of the hydrophilic part of the molecule. Here four groups can be distinguished:
- - anionische Tenside,- anionic surfactants,
- - kationische Tenside,- cationic surfactants,
- - amphotere Tenside undAmphoteric surfactants and
- - nichtionische Tenside.- nonionic surfactants.
Anionische Tenside weisen als funktionelle Gruppen in der Regel Carboxylat-, Sulfat-
oder Sulfonatgruppen auf. In wäßriger Lösung bilden sie im sauren oder neutralen Mi
lieu negativ geladene organische Ionen. Kationische Tenside sind beinahe aus
schließlich durch das Vorhandensein einer quarternären Ammoniumgruppe gekenn
zeichnet. In wäßriger Lösung bilden sie im sauren oder neutralen Milieu positiv gela
dene 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:
Anionic surfactants generally have carboxylate, sulfate or sulfonate groups as functional groups. In aqueous solution, they form negatively charged organic ions in the acidic or neutral state. Cationic surfactants are almost exclusively characterized by the presence of a quaternary ammonium group. In aqueous solution they form positive gela dene organic ions in an acidic or neutral medium. Amphoteric surfactants contain both anionic and cationic groups and therefore behave in aqueous solution depending on the pH as anionic or cationic surfactants. 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 is intended to illustrate:
RNH2 +CH2CH2COOH X- (bei pH=2) X = beliebiges Anion, z. B. Cl-
RNH2 +CH2CH2COO- (bei pH=7)
RNHCH2CH2COO- B+ (bei pH=12) B+ = beliebiges Kation, z. B. Na+ RNH 2 + CH 2 CH 2 COOH X - (at pH = 2) X = any anion, e.g. B. Cl -
RNH 2 + CH 2 CH 2 COO - (at pH = 7)
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 bil den in wäßrigem Medium keine Ionen.Typical of non-ionic surfactants are polyether chains. Nonionic surfactants bil no ions in aqueous medium.
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), wie
These are usually difficult to be compatible with cationic surfactants, therefore their co-use according to the present invention difficult, although, z. B. in small quantities, is not excluded. Advantageously used anionic surfactants 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-palmitoyl aspartate and sodium caprylic / capric glutamate,
- 2. Acylpeptide, beispielsweise Palmitoyl-hydrolysiertes Milchprotein, Natrium Coco yl-hydrolysiertes Soja Protein und Natrium-/Kalium Cocoyl-hydrolysiertes Kolla gen,2. Acyl peptides, for example palmitoyl-hydrolyzed milk protein, sodium coco yl-hydrolyzed soy protein and sodium / potassium cocoyl-hydrolyzed collagen gene,
- 3. Sarcosinate, beispielsweise Myristoyl Sarcosin, TEA-lauroyl Sarcosinat, Natri umlauroylsarcosinat und Natriumcocoylsarkosinat,3. sarcosinates, for example myristoyl sarcosine, TEA lauroyl sarcosinate, Natri umlauroyl 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, Iauroyllactylat, Caproyllactylat5. Acyl lactylate, lauroyl lactylate, caproyl lactylate
- 6. Alaninate6. alaninates
Carbonsäuren und Derivate, wie
Carboxylic acids and derivatives, such as
- 1. Carbonsäuren, beispielsweise Laurinsäure, Aluminiumstearat, Magnesiumalka nolat und Zinkundecylenat,1. Carboxylic acids, for example lauric acid, aluminum stearate, magnesium alka nolate and zinc undecylenate,
- 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,
Phosphorsäureester und Salze, wie beispielsweise DEA-Oleth-10-Phosphat und Di laureth-4 Phosphat,3. Ether carboxylic acids, for example sodium laureth-13 carboxylate and sodium PEG-6 cocamide carboxylate,
Phosphoric acid esters and salts such as DEA-oleth-10-phosphate and di-laureth-4-phosphate,
Sulfonsäuren und Salze, wieSulfonic acids and salts, such as
- 1. Acyl-isethionate, z. B. Natrium-/Ammoniumcocoyl-isethionat,1. Acyl-isethionates, z. B. sodium / ammonium cocoyl isethionate,
- 2. Alkylarylsulfonate,2. alkylarylsulfonates,
- 3. Alkylsulfonate, beispielsweise Natriumcocosmonoglyceridsulfat, Natrium C12-14 Olefin-sulfonat, Natriumlaurylsulfoacetat und Magnesium PEG-3 Cocamidsulfat,3. alkyl sulfonates, for example sodium coconut monoglyceride sulfate, sodium C 12-14 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 laurethsul fosuccinate, disodium lauryl sulphosuccinate and disodium undecylenamido MEA sulfosuccinate
sowie
Schwefelsäureester, wie
such as
Sulfuric acid esters, such as
- 1. Alkylethersulfat, beispielsweise Natrium-, Ammonium-, Magnesium-, MIPA-, TIPA-Laurethsulfat, Natriummyrethsulfat und Natrium C12-13 Parethsulfat,1. alkyl ether sulfate, for example sodium, ammonium, magnesium, MIPA, TIPA laureth sulfate, sodium myreth sulfate and sodium C 12-13 pareth sulfate,
- 2. Alkylsulfate, beispielsweise Natrium-, Ammonium- und TEA- Laurylsulfat.2. Alkyl sulfates, for example sodium, ammonium and TEA lauryl sulfate.
Vorteilhaft zu verwendende kationische Tenside sind
Advantageously to use cationic surfactants
- 1. Alkylamine,1. alkylamines,
- 2. Alkylimidazole,2. Alkylimidazoles,
- 3. Ethoxylierte Amine.3. Ethoxylated amines.
Die große verbleibende Gruppe der quatemären Stickstofftenside wird durch die der Erfindung zugrundeliegende Wirkstoffgruppe repräsentiert.The large remaining group of quaternary nitrogen surfactants is characterized by the Represents invention underlying drug group.
Vorteilhaft zu verwendende amphotere Tenside sind
Advantageously used amphoteric surfactants
- 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 acylamphohydro xypropylsulfonate, disodium acylamphodiacetate and sodium acylamphopropionate,
- 2. N-Alkylaminosäuren, beispielsweise Aminopropylalkylglutamid, Alkylaminopropi onsäure, Natriumalkylimidodipropionat und Lauroamphocarboxyglycinat.2. N-alkyl amino acids, for example Aminopropylalkylglutamid, Alkylaminopropi onsäure, Natriumalkylimidodipropionat and Lauroamphocarboxyglycinat.
Vorteilhaft zu verwendende nicht-ionische Tenside sind
Advantageously used nonionic surfactants are
- 1. Alkohole,1. Alcohols,
- 2. Alkanolamide, wie Cocamide MEA/DEA/MIPA,2. alkanolamides, such as cocamide MEA / DEA / MIPA,
- 3. Aminoxide, wie Cocoamidopropylaminoxid,3. amine oxides, such as cocoamidopropylamine oxide,
- 4. Ester, die durch Veresterung von Carbonsäuren mit Ethylenoxid, Glycerin, Sor bitan oder anderen Alkoholen entstehen,4. Esters obtained by esterification of carboxylic acids with ethylene oxide, glycerol, Sor bitane or other alcohols,
- 5. Ether, beispielsweise ethoxylierte/propoxylierte Alkohole, ethoxylierte/propoxy lierte Ester, ethoxyliertel propoxylierte Glycerinester, ethoxylierte/propoxylierte Cholesterine, ethoxyliertel propoxylierte Triglyceridester, ethoxyliertes propoxy liertes Lanolin, ethoxylierte/propoxylierte Polysiloxane, propoxylierte POE-Ether und Alkylpolyglycoside wie Laurylglucosid, Decylglycosid und Cocoglycosid.5. Ethers, for example ethoxylated / propoxylated alcohols, ethoxylated / propoxy esters, ethoxylated propoxylated glycerol esters, ethoxylated / propoxylated esters Cholesterols, ethoxylated propoxylated triglyceride esters, ethoxylated propoxy lanolin, ethoxylated / propoxylated polysiloxanes, propoxylated POE ethers and alkyl polyglycosides such as lauryl glucoside, decyl glycoside and cocoglycoside.
- 6. Sucroseester, -Ether6. sucrose ester, ether
- 7. Polyglycerinester, Diglycerinester, Monoglycerinester7. Polyglycerol esters, diglycerol esters, monoglycerol esters
- 8. Methylglucosester, Ester von Hydroxysäuren8. 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 Zube reitungen.Depending on the compatibility of the non-cationic surfactants with the inventive Quaternary nitrogen compound can be used in accordance with their concentration in preparations of the invention up to 80 wt .-%, based on the total weight of the Zube TION.
Zusätzlich zu den genannten Bestandteilen können den erfindungsgemäßen derma tologischen Zubereitungen, deren pH-Wert vorzugsweise z. B. durch übliche Puf fergemische auf 4,0 bis 7,5 insbesondere 5,0 bis 6,5, eingestellt wird, Parfüm, Farb stoffe, Antioxidantien, Suspendiermittel, Puffergemische oder andere übliche kosmeti sche oder dermatologische Grundstoffe beigemischt werden.In addition to the ingredients mentioned derma the invention tological preparations whose pH preferably z. B. by conventional Puf Fememic to 4.0 to 7.5, in particular 5.0 to 6.5, is adjusted, perfume, color substances, antioxidants, suspending agents, buffer mixtures or other conventional cosmeti or basic dermatological substances.
Erfindungsgemäß können als günstige Antioxidantien alle für kosmetische und/oder dermatologische Anwendungen geeigneten oder gebräuchlichen Antioxidantien ver wendet werden.According to the invention as cheap antioxidants all for cosmetic and / or dermatological applications suitable or common antioxidants ver be used.
Es ist auch von Vorteil, den erfindungsgemäßen Zubereitungen Antioxidantien zuzu setzen. 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, β- 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-, Palmitoyl-, 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. Citronensäure, Milchsäure, Apfelsäu re), 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 Deri vate (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 Deri vate, Zink und dessen Derivate (z. B. ZnO, ZnSO4) Selen und dessen Derivate (z. B. Selenmethionin), Stilbene und deren Derivate (z. B. Stilbenoxid, Trans-Stilbenoxid) und die erfindungsgemäß geeigneten Derivate (Salze, Ester, Ether, Zucker, Nukleoti de, 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 urocaninic acid) and derivatives thereof, peptides such as D, L-carnosine, D Carnosine, L-carnosine and their derivatives (eg anserine), carotenoids, carotenes (eg α-carotene, β-carotene, lycopene) and derivatives thereof, chlorogenic acid and its derivatives, lipoic acid and derivatives thereof ( eg dihydrolipoic acid), aurothioglucose, propylthiouracil and other thiols (eg thioredoxin, glutathione, cysteine, cystine, cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl, γ-linoleyl, cholesteryl and glyceryl esters) and their salts, dilauryl thiodi propionate, distearyl thiodipropionate, thiodipropionic acid and derivatives thereof (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) and Sulfoximine compounds (eg, buthionine sulfoximines, homocysteine sulfoximine, buthioni sulfones, penta, hexa, heptathionine sulfoximine) in very low tolerated dosages (eg. Pmol to μmol / kg), furthermore (metal) chelators (for example α-hydroxyfatty acids, palmitic acid, phytic acid, lactoferrin), α-hydroxy acids (for example citric 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 its derivatives, ubiquinone and ubiquinol and their derivatives, vitamin C and derivatives (For example, ascorbyl palmitate, Mg-ascorbyl phosphate, As corbylacetat), tocopherols and derivatives (eg., Vitamin E acetate), vitamin A and Deri vate (vitamin A palmitate) and Koniferylbenzoat of Benzoeharzes, rutinic acid and their Derivatives, α-glycosylrutin, ferulic acid, furfurylideneglucitol, carnosine, butylhydroxytoluene, butylhydroxyanisole, nordihydroguaiacetic acid, nordihydroguajaric acid, trihydroxybutyrophenone, uric acid and its derivatives, mannose and its derivatives, zinc and its derivatives (eg ZnO, ZnS O 4 ) selenium and its derivatives (e.g. B. selenium methionine), stilbenes and their derivatives (eg stilbene oxide, trans-stilbene oxide) and the inventively suitable derivatives (salts, esters, ethers, sugars, Nukleoti de, nucleosides, peptides and lipids) of these drugs.
Die Menge der Antioxidantien (eine oder mehrere Verbindungen) in den Zubereitun gen 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 antioxidants (one or more compounds) in the preparation is preferably from 0.001 to 30% by weight, particularly preferably from 0.05 to 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. If vitamin E and / or its derivatives are the antioxidant (s) advantageous, their respective concentrations in the range of 0.001-10 wt .-%, based on the total weight of the formulation to choose.
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 Formulie rung, zu wählen.If vitamin A, or vitamin A derivatives, or carotenes or their derivatives the or which are antioxidants is advantageous, their respective concentrations of in the range of 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 erfindungsgemä ßen 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 inventive dermatological preparations is less than 8. pH values that are slightly higher as 7, but smaller than 7.5 can be tolerated in general. Anyway for a given fatty acid mixture in a particular case by simple trial and error, without inventive effort, easy to determine which exact upper pH limit to note is.
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.Advantageously, the pH of the formulations of the invention in the acid to very weakly alkaline range less than 8, preferably 4.0-7.5, more preferably from 5.0 to 6.5.
Die jeweils einzusetzenden Mengen an Hilfs- Zusatz- und Trägerstoffen und gegebe nenfalls Parfüm können in Abhängigkeit von der Art des jeweiligen Produktes vom Fachmann durch einfaches Ausprobieren leicht ermittelt werden.The amounts to be used in each case auxiliary auxiliaries and carriers and give Perfume may vary depending on the type of product Professional can be easily determined by simple trial and error.
Die Herstellung der erfindungsgemäßen dermatologischen Zubereitungen erfolgt, ab gesehen von speziellen Zubereitungen, die in den Beispielen jeweils gesondert ver merkt 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.The production of the dermatological preparations according to the invention takes place from seen from special preparations which in the examples separately ver are noticed in the usual way, usually by simply mixing with stirring, optionally with slight warming. It offers no difficulties. For Emulsions become fat phase and the water phase z. B. separately, if necessary prepared 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 putting together galenic Observe formulations that are familiar to the expert.
Sollen die erfindungsgemäßen Kombinationen in Puder eingearbeitet werden, so kön nen 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 in powder, then Kings NEN the suspension bases are advantageously selected from the group Silica gels (eg those available under the tradename Aerosil®), Diatomaceous earth, talc, modified starch, titanium dioxide, silk powder, nylon powder, poly ethylene powder and related substances.
Es folgen vorteilhafte Ausführungsbeispiele der vorliegenden Erfindung. Die Mengen angaben beziehen sich stets auf Gewichts-%, wenn nichts Anderes angegeben wird. Following are advantageous embodiments of the present invention. The quantities Information always refers to% by weight, unless stated otherwise.
Claims (2)
Priority Applications (3)
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DE1998137549 DE19837549A1 (en) | 1998-08-19 | 1998-08-19 | Use of quaternary nitrogen compounds for treatment and prevention of atopic eczema |
EP99938370A EP1104295A1 (en) | 1998-08-19 | 1999-07-29 | Use of quaternary nitrogen compounds for prophylaxis or treatment of superinfected atopic eczema |
PCT/EP1999/005425 WO2000010556A1 (en) | 1998-08-19 | 1999-07-29 | Use of quaternary nitrogen compounds for prophylaxis or treatment of superinfected atopic eczema |
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DE1998137549 DE19837549A1 (en) | 1998-08-19 | 1998-08-19 | Use of quaternary nitrogen compounds for treatment and prevention of atopic eczema |
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DE1998137549 Withdrawn DE19837549A1 (en) | 1998-08-19 | 1998-08-19 | Use of quaternary nitrogen compounds for treatment and prevention of atopic eczema |
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DE (1) | DE19837549A1 (en) |
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
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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 |
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 |
DE10140361B4 (en) * | 2001-08-17 | 2009-07-16 | Rüdiger Bode | Use of a preparation containing biguanides for hoof care |
Families Citing this family (2)
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WO2006054312A1 (en) * | 2004-11-16 | 2006-05-26 | Munisekhar Medasani | Ammonium compounds for treating psoriasis and eczema |
WO2017195783A1 (en) * | 2016-05-09 | 2017-11-16 | 株式会社ナノエッグ | 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 |
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JPH0812572A (en) * | 1994-07-01 | 1996-01-16 | Kosakai:Kk | Therapeutic agent for dermatomycosis |
IT1295974B1 (en) * | 1996-11-04 | 1999-05-28 | Claudio Risicato | DISINFECTANT COMPOSITION IN PARTICULAR FOR THE PREVENTION OF DERMATITIS FROM NAP |
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1998
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- 1999-07-29 WO PCT/EP1999/005425 patent/WO2000010556A1/en not_active Application Discontinuation
- 1999-07-29 EP EP99938370A patent/EP1104295A1/en not_active Withdrawn
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DE3337026A1 (en) * | 1983-10-12 | 1985-04-25 | Henkel KGaA, 4000 Düsseldorf | Amine oxide sulphonates |
DE3528209A1 (en) * | 1984-08-07 | 1986-04-24 | Fresenius AG, 6380 Bad Homburg | Disinfectant |
DE3603859A1 (en) * | 1986-02-07 | 1987-08-13 | Roehm Pharma Gmbh | WASHABLE TOPICAL PREPARATION FOR THERAPY OF PSORIASIS |
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Cited By (3)
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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 |
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WO2000010556A1 (en) | 2000-03-02 |
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