EP1100455A1 - Cosmetic and dermatological preparations comprising an effective content of bile acids, their salts and/or their derivatives - Google Patents

Cosmetic and dermatological preparations comprising an effective content of bile acids, their salts and/or their derivatives

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Publication number
EP1100455A1
EP1100455A1 EP99938295A EP99938295A EP1100455A1 EP 1100455 A1 EP1100455 A1 EP 1100455A1 EP 99938295 A EP99938295 A EP 99938295A EP 99938295 A EP99938295 A EP 99938295A EP 1100455 A1 EP1100455 A1 EP 1100455A1
Authority
EP
European Patent Office
Prior art keywords
salts
derivatives
acid
skin
preparations
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP99938295A
Other languages
German (de)
French (fr)
Inventor
Ghita LANZENDÖRFER
Volker Schreiner
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Beiersdorf AG
Original Assignee
Beiersdorf AG
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Filing date
Publication date
Application filed by Beiersdorf AG filed Critical Beiersdorf AG
Publication of EP1100455A1 publication Critical patent/EP1100455A1/en
Withdrawn legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04Dispersions; Emulsions
    • A61K8/06Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55Phosphorus compounds
    • A61K8/553Phospholipids, e.g. lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/02Preparations containing skin colorants, e.g. pigments
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/02Preparations containing skin colorants, e.g. pigments
    • A61Q1/04Preparations containing skin colorants, e.g. pigments for lips
    • A61Q1/06Lipsticks
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q15/00Anti-perspirants or body deodorants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/001Preparations for care of the lips
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/10Washing or bathing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • A61Q5/02Preparations for cleaning the hair

Definitions

  • the present invention relates to cosmetic and dermatological preparations with an effective content of bile acids, their salts and / or their derivatives and the use thereof for strengthening the barrier function of the skin.
  • the skin is the largest human organ. Among its many functions (for example for heat regulation and as a sensory organ), the barrier function that prevents the skin (and ultimately the entire organism) from drying out is probably the most important. At the same time, the skin acts as a protective device against the penetration and absorption of substances coming from outside. This barrier function is brought about by the epidermis, which as the outermost layer forms the actual protective cover against the environment. At around a tenth of the total thickness, it is also the thinnest layer of the skin.
  • the epidermis is a stratified tissue in which the outer layer, the horny layer (stratum corneum), is the important part for the barrier function. It is worn away in contact with the environment and is therefore in a constant renewal process, with fine flakes being continuously released to the outside and corneal and lipid material horned from the inside being reproduced.
  • the skin model of Elias (PM Elias, Structure and Function of the Stratum Corneum Permeability Barrier, Drug Dev. Res. 13, 1988, 97-105), which is recognized by experts today, describes the horny layer as a two-component system, similar to a brick wall ( Brick-mortar model).
  • the horny cells (corneocytes) correspond to the bricks
  • the complex lipid membrane in the intercellular spaces corresponds to the mortar.
  • This system essentially represents a physical barrier against hydrophilic substances, but due to its narrow and more-
  • the regulation of water and moisture content is one of the most important functions of the epidermal lipid membrane. However, it not only has a barrier effect against external chemical and physical influences, but also contributes to the cohesion of the horny layer.
  • the lipids of the horny layer essentially consist of ceramides, free fatty acids, cholesterol and cholesterol sulfate and are distributed over the entire horny layer.
  • the composition of these lipids is of crucial importance for the intact function of the epidermal barrier and thus for the water impermeability of the skin.
  • the barrier effect of the skin can be quantified by determining the transepidermal water loss (TEWL - transepidermal water ioss). This is the evaporation of water from the inside of the body without taking into account the loss of water when sweating.
  • the determination of the TEWL value has proven to be extremely informative and can be used to diagnose cracked or chapped skin, to determine the compatibility of chemically differently structured surfactants and the like.
  • the water content in the top layer of skin is of the utmost importance. It can be influenced to a limited extent by introducing moisture regulators.
  • Anionic surfactants which are generally components of cleaning preparations, can increase the pH value in the horny layer for a long time, which greatly hinders regenerative processes that serve to restore and renew the barrier function of the skin. In this case, a new, often very unfavorable state of equilibrium occurs in the horny layer between regeneration and the loss of essential substances through regular extraction, which significantly affects the external appearance of the skin and the physiological functioning of the horny layer.
  • Skin care in the sense of the present invention is to be understood primarily as meaning that the natural function of the skin acts as a barrier against environmental influences (e.g. dirt, chemical potassium, microorganisms) and against the loss of the body's own substances (e.g. water, lipids, electrolytes) is strengthened or restored.
  • environmental influences e.g. dirt, chemical potassium, microorganisms
  • loss of the body's own substances e.g. water, lipids, electrolytes
  • the effect of ointments and creams on the barrier function and the hydration of the horny layer is based essentially on the covering (occlusion) of the treated skin areas.
  • the ointment or cream is, so to speak, a (second) artificial barrier that is supposed to prevent water loss from the skin.
  • This physical barrier can be removed correspondingly easily, for example with cleaning agents, as a result of which the original, impaired state is reached again.
  • the skin care effect can decrease with regular treatment. After stopping the application of the product, the skin quickly returns to the condition before the start of treatment. With certain products, the condition of the skin may even temporarily deteriorate. A sustainable product effect is therefore generally not achieved or only to a limited extent.
  • the effect of nourishing cleaning products essentially consists in an efficient regreasing with sebum lipid-like substances.
  • the damage to the horny layer barrier can be further limited.
  • the prior art lacks preparations which have a positive effect on the barrier function and hydration of the horny layer and which strengthen or even restore the physicochemical properties of the horny layer and in particular the lamellae made of intercellular lipids.
  • the object of the present invention was therefore to eliminate the disadvantages of the prior art.
  • skin-care preparations and preparations for cleaning the skin should be made available which maintain or restore the barrier properties of the skin, especially when the natural regeneration of the skin is insufficient. They should also be suitable for the treatment and prophylaxis of consequential damage to skin drying out, for example fissures or inflammatory or allergic processes or also neurodermatitis.
  • barrier strengthening or “strengthening the barrier function of the skin” is to be understood in particular to mean the following effect: the active compounds according to the invention interact with the lipids of the horny layer in such a way that the arrangement of these lipids in the horny layer at the molecular level is improved. This means that the natural function of the skin as a barrier against environmental influences and against the loss of the body's own substances is strengthened or restored.
  • Bile is the exocrine secretion of the liver, the main components of which are water (86.7%), bile acids (9.1%), bile pigments (3%), cholesterol (0.3%) and fatty acids, pro teine and inorganic substances.
  • the function of the bile in the context of fat digestion consists in the emulsification of water-insoluble food components in the intestinal tract and in the conversion of water-insoluble compounds into the resorbable cholic acids.
  • the bile acids which occur in the bile as salts, keep the cholesterol in solution and facilitate its excretion.
  • Bile acids are predominantly substituted cholanic acids conjugated with glycine (glycocholic acid) or taurine (taurocholic acid), which have the following structural motif:
  • dehydrocholic acid which is characterized by the following structure, and its salts:
  • lithocholic acid which is characterized by the following structure, and its salts:
  • Cholic acid which is characterized by the following structure, and its salts are also advantageous:
  • Glycocholic acid which is characterized by the following structure, and its salts are also advantageous:
  • taurolithocholic acid which is characterized by the following structure, and its salts, in particular its sodium salt:
  • deoxycholic acid which is characterized by the following structure, and its salts:
  • ursodeoxycholic acid (chenodeoxycholic acid), which is characterized by the following structure, and its salts:
  • taurocholic acid which is characterized by the following structure, and its salts, in particular its sodium salt:
  • esters and ethers of bile acids are also advantageous in the sense of the present invention.
  • Bile acid ethers can be obtained by etherification of at least one of the alcohol functions in the 3-, 7- or 12-position of the cholane ring. Bile acid ethers which are obtainable by etherification of the alcohol function in the 3-position are particularly preferred.
  • bile acid ethers which are obtainable by etherification with ethylene oxide, saturated and / or unsaturated, branched and / or unbranched alcohols having a chain length of 2 to 22 carbon atoms are advantageous.
  • Bile acid esters can be obtained by esterifying at least one of the alcohol functions in the 3-, 7- or 12-position of the cholane ring and by esterifying the terminal acid functions.
  • Advantageous in the sense of the present invention are bile acid esters, which by esterification with saturated and / or unsaturated, branched and / or unbranched acids with a chain length of 2 to 22 carbon atoms are available.
  • bile acid esters which can be obtained by esterifying the terminal acid function with ethylene oxide, saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 2 to 22 carbon atoms.
  • the salts of bile acids are also particularly advantageous in the sense of the present invention.
  • the sodium, potassium and / or triethanolamine salts of bile acids are particularly preferred according to the invention.
  • the cosmetic or dermatological preparations or formulations according to the invention can be composed as usual and can be used for the treatment, care and cleaning of the skin and / or hair and as a make-up product in decorative cosmetics. Correspondingly, depending on their structure, they can be used, for example, as a skin protection cream, cleansing milk, sunscreen lotion, nutritional cream, day or night cream, etc. It may be possible and advantageous to use the preparations according to the invention as the basis for pharmaceutical formulations.
  • the preparations according to the invention contain z. B.
  • 0.001 to 10 wt .-% preferably 0.01 wt .-% to 1 wt .-%, but especially 0.01 wt .-% to 0.5 wt .-%, each based on the total weight of the preparations on the active substances according to the invention.
  • Cosmetic and dermatological preparations which are in the form of a sunscreen are also favorable.
  • these preferably contain at least one UV-A filter substance and / or at least one UV-B filter substance and / or at least one inorganic pigment.
  • the cosmetic and dermatological preparations according to the invention can contain cosmetic auxiliaries, as are usually used in such preparations, e.g. B. preservatives, bactericides, perfumes, anti-foaming substances, dyes, pigments that have a coloring effect, thickeners, surface-active substances, emulsifiers, softening, moisturizing and / or moisturizing substances, fats, oils, waxes or other common components of a cosmetic or dermatological formulation such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
  • cosmetic auxiliaries e.g. B. preservatives, bactericides, perfumes, anti-foaming substances, dyes, pigments that have a coloring effect, thickeners, surface-active substances, emulsifiers, softening, moisturizing and / or moisturizing substances, fats, oils, waxes or other common components of a cosmetic or dermatological formulation such as alcohols, polyo
  • Preparations for the treatment and care of the skin are particularly preferred.
  • the cosmetic and dermatological preparations according to the invention are applied to the skin and / or the hair in a sufficient amount in the manner customary for cosmetics.
  • Cosmetic and dermatological preparations according to the invention can be in various forms. So you can z. B. a solution, an anhydrous preparation, an emulsion or microemulsion of the water-in-oil (W / O) or oil-in-water (O / W) type, a multiple emulsions, for example of the water-in-oil type Oil-in-water (W / O / W), a gel, a solid stick, an ointment or an aerosol. It is also advantageous to present the active compounds according to the invention in encapsulated form, e.g. B. in collagen matrices and other common encapsulation materials, e.g. B.
  • the cosmetic and dermatological preparations according to the invention can also contain antioxidants.
  • all the antioxidants suitable or customary for cosmetic and / or dermatological applications can be used as favorable antioxidants.
  • the antioxidants are advantageously selected from the group consisting of amino acids (e.g. glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (e.g. urocanic acid) and their derivatives, peptides such as D, L-camosine, D-carnosine, L-carnosine and their derivatives (e.g. anserine), carotenoids, carotenes (e.g. ⁇ -carotene, ß-carotene, lycopene) and their derivatives, chlorogenic acid and its derivatives, lipoic acid and its derivatives ( e.g.
  • amino acids e.g. glycine, histidine, tyrosine, tryptophan
  • imidazoles e.g. urocanic acid
  • peptides such as D, L-camosine, D-carnosine, L-carnosine and their derivatives (e.g. anserine)
  • thiols e.g. thioredoxin, glutathione, cysteine, cystine, cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl , Butyl and lauryl, palmitoyl, oleyl, ⁇ -linoleyl, cholesteryl and glyceryl esters
  • salts dilauryl thiodipropionate, distearyl thiodipropionate, thiodipropionic acid and their derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) as well as sulfoximine compounds (e.g.
  • buthionine sulfoximines in very low tolerable doses (e.g. B. pmol to ⁇ mol / kg), further (metal) chelators (e.g. ⁇ -hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), ⁇ -hydroxy acids (e.g.
  • crtronic acid lactic acid, malic acid
  • humic acid bile acid
  • Bile extracts bilirubin, biliverdin, EDTA, EGTA and their derivatives
  • unsaturated fatty acids and their derivatives e.g. ⁇ -linolenic acid, linoleic acid, oleic acid
  • folic acid and their derivatives ubiquinone and ubiquinol and their derivatives
  • vitamin C and derivatives e.g. B. Ascorbyl palmitate, Mg ascorbyl phosphate, ascorbyl acetate), tocopherols and derivatives (e.g.
  • vitamin E acetate
  • vitamin A and derivatives vitamin A palmitate
  • Derivatives e.g. stilbene oxide, trans-stilbene oxide
  • derivatives suitable according to the invention te (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids) of these active ingredients.
  • the amount of the aforementioned antioxidants (one or more compounds) in the preparations according to the invention 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 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 use their respective concentrations in the range from 0.001-10% by weight, based on the total weight of the formulation, to choose.
  • Color pigments Color lacquers, titanium dioxide q, p.
  • Glycerol monostearate 1 00
  • Titanium dioxide 2.50

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Dermatology (AREA)
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  • Toxicology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
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Abstract

The invention relates to cosmetic and dermatological preparations comprising an effective content of bile acids, their salts and/or their derivatives, whereby said active ingredients can be provided both individually and in a mixture.

Description

Beschreibung description
Kosmetische und dermatologische Zubereitungen mit einem wirksamen Gehalt an Gallensäuren, ihren Salzen und/oder ihren DerivatenCosmetic and dermatological preparations with an effective content of bile acids, their salts and / or their derivatives
Die vorliegende Erfindung betrifft kosmetische und dermatologische Zubereitungen mit einem wirksamen Gehalt an Gallensäuren, ihren Salzen und/oder ihren Derivaten sowie die Verwendung derselben zur Stärkung der Barrierefunktion der Haut.The present invention relates to cosmetic and dermatological preparations with an effective content of bile acids, their salts and / or their derivatives and the use thereof for strengthening the barrier function of the skin.
Die Haut ist das größte Organ des Menschen. Unter ihren vielen Funktionen (beispielsweise zur Wärmeregulation und als Sinnesorgan) ist die Barrierefunktion, die das Austrocknen der Haut (und damit letzlich des gesamten Organismus) verhindert, die wohl wichtigste. Gleichzeitig wirkt die Haut als Schutzeinrichtung gegen das Eindringen und die Aufnahme von außen kommender Stoffe. Bewirkt wird diese Barrierefunktion durch die Epidermis, welche als äußerste Schicht die eigentliche Schutzhülle gegenüber der Umwelt bildet. Mit etwa einem Zehntel der Gesamtdicke ist sie gleichzeitig die dünnste Schicht der Haut.The skin is the largest human organ. Among its many functions (for example for heat regulation and as a sensory organ), the barrier function that prevents the skin (and ultimately the entire organism) from drying out is probably the most important. At the same time, the skin acts as a protective device against the penetration and absorption of substances coming from outside. This barrier function is brought about by the epidermis, which as the outermost layer forms the actual protective cover against the environment. At around a tenth of the total thickness, it is also the thinnest layer of the skin.
Die Epidermis ist ein stratifiziertes Gewebe, in dem die äußere Schicht, die Hornschicht (Stratum corneum), den für die Barrierefunktion bedeutenden Teil darstellt. Sie wird im Kontakt mit der Umwelt abgenutzt und befindet deshalb sich in einem ständigen Emeuerungs- prozess, wobei nach außen kontinuierlich feine Schuppen abgegeben und von innen verhorntes Zeil- und Lipidmaterial nachproduziert wird.The epidermis is a stratified tissue in which the outer layer, the horny layer (stratum corneum), is the important part for the barrier function. It is worn away in contact with the environment and is therefore in a constant renewal process, with fine flakes being continuously released to the outside and corneal and lipid material horned from the inside being reproduced.
Das heute in der Fachwelt anerkannte Hautmodell von Elias (P. M. Elias, Structure and Function of the Stratum Corneum Permeability Barrier, Drug Dev. Res. 13, 1988, 97-105) beschreibt die Hornschicht als Zwei-Komponenten-System, ähnlich einer Ziegelsteinmauer (Ziegelstein-Mörtel-Modell). In diesem Modell entsprechen die Hornzellen (Korneozyten) den Ziegelsteinen, die komplex zusammengesetzte Lipidmembran in den Interzellularräumen entspricht dem Mörtel. Dieses System stellt im wesentlichen eine physikalische Barriere gegen hydrophile Substanzen dar, kann aber aufgrund seiner engen und mehr-The skin model of Elias (PM Elias, Structure and Function of the Stratum Corneum Permeability Barrier, Drug Dev. Res. 13, 1988, 97-105), which is recognized by experts today, describes the horny layer as a two-component system, similar to a brick wall ( Brick-mortar model). In this model, the horny cells (corneocytes) correspond to the bricks, the complex lipid membrane in the intercellular spaces corresponds to the mortar. This system essentially represents a physical barrier against hydrophilic substances, but due to its narrow and more-
Q \USER\HEINDO-R\PAT-RS\97-179 DOC schichtigen Struktur gleichermaßen auch von lipophilen Substanzen nur schwer passiert werden. Die besondere Struktur der Hornschicht schützt einerseits die Haut und stabilisiert andererseits ihre eigene Flexibilität durch Bindung einer definierten Wassermenge.Q \ USER \ HEINDO-R \ PAT-RS \ 97-179 DOC layered structure is equally difficult for lipophilic substances to pass through. The special structure of the horny layer protects the skin on the one hand and on the other hand stabilizes its own flexibility by binding a defined amount of water.
Auch mechanische Belastungen, wie beispielsweise Druck-, Stoß- oder Scherkräfte, können in erstaunlichem Maße durch die Hornschicht allein oder im Verbund mit den tieferen Hautschichten abgefangen werden. Größere Druck-, Dreh- oder Scherkräfte werden über die Verzahnung der Epidermis mit dem Corium an tiefere Hautschichten weitergegeben.Mechanical loads such as pressure, impact or shear forces can also be absorbed to an astonishing extent by the horny layer alone or in combination with the deeper skin layers. Greater pressure, torsional or shear forces are passed on to the deeper layers of the skin through the interlocking of the epidermis with the corium.
Die Regulation des Wasser- und Feuchtigkeitsgehaltes ist eine der wichtigsten Funktionen der epidermalen Lipidmembran. Allerdings hat sie nicht nur eine Barrierewirkung gegen externe chemische und physikalische Einflüsse, sondern trägt auch zum Zusammenhalt der Hornschicht bei.The regulation of water and moisture content is one of the most important functions of the epidermal lipid membrane. However, it not only has a barrier effect against external chemical and physical influences, but also contributes to the cohesion of the horny layer.
Die Lipide der Hornschicht bestehen im wesentlichen aus Ceramiden, freien Fettsäuren, Cholesterin und Cholesterinsulfat und sind über die gesamte Hornschicht verteilt. Die Zusammensetzung dieser Lipide ist für die intakte Funktion der epidermalen Barriere und damit für die Wasserundurchlässigkeit der Haut von entscheidender Bedeutung.The lipids of the horny layer essentially consist of ceramides, free fatty acids, cholesterol and cholesterol sulfate and are distributed over the entire horny layer. The composition of these lipids is of crucial importance for the intact function of the epidermal barrier and thus for the water impermeability of the skin.
Bereits bei einer Reinigung der Haut mit Hilfe eines einfachen Wasserbads - ohne Zusatz von Tensiden - kommt es zunächst zu einer Quellung der Hornschicht der Haut. Der Grad dieser Quellung hängt u. a. von der Dauer des Bads und dessen Temperatur ab. Gleichzeitig werden wasserlösliche Stoffe ab- bzw. ausgewaschen, wie z. B. wasserlösliche Schmutzbestandteile, aber auch hauteigene Stoffe, die für das Wasserbindungsvermögen der Hornschicht verantwortlich sind. Durch hauteigene oberflächenaktive Stoffe werden außerdem auch Hautfette in gewissem Ausmaß gelöst und ausgewaschen. Dies bedingt nach anfänglicher Quellung eine nachfolgende Austrocknung der Haut, die durch waschaktive Zusätze noch deutlich verstärkt werden kann.When the skin is cleaned with the help of a simple water bath - without the addition of surfactants - the skin's horny layer swells. The degree of this swelling depends on a. on the duration of the bath and its temperature. At the same time, water-soluble substances are washed off or washed out, e.g. B. water-soluble dirt components, but also the skin's own substances, which are responsible for the water retention capacity of the horny layer. Skin oils are also dissolved and washed out to a certain extent by the skin's own surface-active substances. After initial swelling, this causes the skin to subsequently dry out, which can be significantly enhanced by washing-active additives.
Bei gesunder Haut sind diese Vorgänge im allgemeinen belanglos, da die Schutzmechanismen der Haut solche leichten Störungen der oberen Hautschichten ohne weiteres kompensieren können. Aber bereits im Fall nichtpathologischer Abweichungen vom Normalstatus, z. B. durch umweltbedingte Abnutzungsschäden bzw. Irritationen, Lichtschäden, Altershaut usw., ist der Schutzmechanismus an der Hautoberfläche gestört. Bei alter Haut beispielsweise erfolgt die regenerative Erneuerung verlangsamt, wobei insbesondere das Wasserbindungsvermögen der Hornschicht nachläßt. Sie wird deshalb inflexibel, trocken und rissig ("physiologisch" trockene Haut). Ein Barriereschaden ist die Folge. Die Haut wird anfällig für negative Umwelteinflüsse wie die Invasion von Mikroorganismen, Toxinen und Allergenen. Als Folge kann es sogar zu toxischen oder allergischen Hautreaktionen kommen.These processes are generally irrelevant for healthy skin, since the protective mechanisms of the skin can easily compensate for such slight disorders of the upper layers of the skin. But already in the case of non-pathological deviations from normal status, e.g. B. by environmental wear and tear or irritation, light damage, aging skin, etc., the protective mechanism on the skin surface is disturbed. In the case of old skin, for example, the regenerative renewal is slowed down, the water-binding capacity of the horny layer in particular diminishing. It therefore becomes inflexible, dry and cracked ("physiologically" dry skin). Barrier damage is the result. The skin becomes susceptible to negative environmental influences such as the invasion of microorganisms, toxins and allergens. As a result, there may even be toxic or allergic skin reactions.
Bei pathologisch trockener und empfindlicher Haut liegt ein Barriereschaden a priori vor. Epidermale Interzellularlipide werden offenbar fehlerhaft oder in ungenügender Menge bzw. Zusammensetzung gebildet. Die Konsequenz ist eine erhöhte Durchlässigkeit der Hornschicht und ein unzureichender Schutz der Haut vor Verlust an hygroskopischen Substanzen und Wasser.In the case of pathologically dry and sensitive skin, there is a priori barrier damage. Epidermal intercellular lipids appear to be defective or in insufficient quantity or composition. The consequence is increased permeability of the horny layer and inadequate protection of the skin against loss of hygroscopic substances and water.
Die Barrierewirkung der Haut kann über die Bestimmung des transepidermalen Wasserverlustes (TEWL - transepidermal water ioss) quantifiziert werden. Dabei handelt es sich um die Abdunstung von Wasser aus dem Körperinneren ohne Einbeziehung des Wasserverlustes beim Schwitzen. Die Bestimmung des TEWL-Wertes hat sich als außerordentlich informativ erwiesen und kann zur Diagnose rissiger oder schrundiger Haut, zur Bestimmung der Verträglichkeit chemisch verschiedenartig aufgebauter Tenside und dergleichen mehr herangezogen werden.The barrier effect of the skin can be quantified by determining the transepidermal water loss (TEWL - transepidermal water ioss). This is the evaporation of water from the inside of the body without taking into account the loss of water when sweating. The determination of the TEWL value has proven to be extremely informative and can be used to diagnose cracked or chapped skin, to determine the compatibility of chemically differently structured surfactants and the like.
Für die Schönheit und Gepflegtheit der Haut ist der Wasseranteil in der obersten Hautschicht von größter Bedeutung. Man kann ihn in einem begrenzten Umfang durch Einbringen von Feuchtigkeitsregulatoren günstig beeinflussen.For the beauty and care of the skin, the water content in the top layer of skin is of the utmost importance. It can be influenced to a limited extent by introducing moisture regulators.
Anionische Tenside, welche im allgemeinen Bestandteile von Reinigungszubereitungen sind, können den pH-Wert in der Hornschicht langanhaltend erhöhen, was regenerative Prozesse, die der Wiederherstellung und Erneuerung der Barrierefunktion der Haut dienen, stark behindert. In diesem Fall stellt sich in der Hornschicht zwischen Regeneration und dem Verlust essentieller Substanzen durch regelmäßige Extraktion ein neuer, häufig sehr ungünstiger Gleichgewichtszustand ein, der das äußere Erscheinungsbild der Haut und die physiologische Funktionweise der Hornschicht entscheidend beeinträchtigt.Anionic surfactants, which are generally components of cleaning preparations, can increase the pH value in the horny layer for a long time, which greatly hinders regenerative processes that serve to restore and renew the barrier function of the skin. In this case, a new, often very unfavorable state of equilibrium occurs in the horny layer between regeneration and the loss of essential substances through regular extraction, which significantly affects the external appearance of the skin and the physiological functioning of the horny layer.
Unter Hautpflege im Sinne der vorliegenden Erfindung ist in erster Linie zu verstehen, daß die natürliche Funktion der Haut als Barriere gegen Umwelteinflüsse (z. B. Schmutz, Chemi- kalien, Mikroorganismen) und gegen den Verlust von körpereigenen Stoffen (z. B. Wasser, Lipide, Elektrolyte) gestärkt oder wiederhergestellt wird.Skin care in the sense of the present invention is to be understood primarily as meaning that the natural function of the skin acts as a barrier against environmental influences (e.g. dirt, chemical potassium, microorganisms) and against the loss of the body's own substances (e.g. water, lipids, electrolytes) is strengthened or restored.
Produkte zur Pflege, Behandlung und Reinigung trockener und strapazierter Haut sind an sich bekannt. Allerdings ist ihr Beitrag zur Regeneration einer physiologisch intakten, hydra- tisierten und glatten Hornschicht umfangmäßig und zeitlich begrenzt.Products for the care, treatment and cleaning of dry and stressed skin are known per se. However, their contribution to the regeneration of a physiologically intact, hydrated and smooth horny layer is limited in scope and time.
Die Wirkung von Salben und Cremes auf die Barrierefunktion und die Hydratation der Hornschicht beruht im wesentlichen auf der Abdeckung (Okklusion) der behandelten Hautbezirke. Die Salbe oder Creme stellt sozusagen eine (zweite) künstliche Barriere dar, die den Wasserverlust der Haut verhindern soll. Entsprechend leicht kann diese physikalische Barriere - beispielsweise mit Reinigungsmitteln - wieder entfernt werden, wodurch der ursprüngliche, beeinträchtigte Zustand wieder erreicht wird. Darüber hinaus kann die Hautpflegewirkung bei regelmäßiger Behandlung nachlassen. Nach dem Absetzen der Produktanwendung kehrt die Haut sehr schnell wieder in den Zustand vor Behandlungsbeginn zurück. Bei bestimmten Produkten verschlechtert sich der Zustand der Haut unter Umständen sogar vorübergehend. Eine nachhaltige Produktwirkung wird in der Regel also nicht oder nur in einem eingeschränkten Maße erreicht.The effect of ointments and creams on the barrier function and the hydration of the horny layer is based essentially on the covering (occlusion) of the treated skin areas. The ointment or cream is, so to speak, a (second) artificial barrier that is supposed to prevent water loss from the skin. This physical barrier can be removed correspondingly easily, for example with cleaning agents, as a result of which the original, impaired state is reached again. In addition, the skin care effect can decrease with regular treatment. After stopping the application of the product, the skin quickly returns to the condition before the start of treatment. With certain products, the condition of the skin may even temporarily deteriorate. A sustainable product effect is therefore generally not achieved or only to a limited extent.
Die Wirkung einiger pharmazeutischer Zubereitungen auf die Barrierefunktion der Haut besteht sogar in einer selektiven Barriereschädigung, die ermöglichen soll, daß Wirkstoffe in bzw. durch die Haut in den Körper eindringen können. Ein gestörtes Erscheinungsbild der Haut wird dabei als Nebenwirkung teilweise billigend in Kauf genommen.The effect of some pharmaceutical preparations on the barrier function of the skin even consists in selective barrier damage, which is intended to enable active substances to penetrate into or through the skin into the body. A disturbed appearance of the skin is sometimes accepted as a side effect.
Die Wirkung von pflegenden Reinigungsprodukten besteht im wesentlichen in einer effizienten Rückfettung mit Sebumlipid-ähnlichen Substanzen. Durch die gleichzeitige Verminderung des Tensidgehalts solcher Zubereitungen läßt sich der Schaden an der Hornschicht- barriere weiter begrenzen.The effect of nourishing cleaning products essentially consists in an efficient regreasing with sebum lipid-like substances. By simultaneously reducing the surfactant content of such preparations, the damage to the horny layer barrier can be further limited.
Dem Stand der Technik mangelt es allerdings an Zubereitungen, welche die Barrierefunktion und die Hydratation der Hornschicht positiv beeinflussen und die physikalisch-chemischen Eigenschaften der Hornschicht und insbesondere der Lamellen aus Interzellularlipiden stärken bzw. sogar wiederherstellen. Aufgabe der vorliegenden Erfindung war es also, die Nachteile des Standes der Technik zu beseitigen. Insbesondere sollten hautpflegende Zubereitungen und Zubereitungen zur Reinigung der Haut zur Verfügung gestellt werden, welche die Barriereeigenschaften der Haut erhalten oder wiederherstellen, zumal dann, wenn die natürliche Regeneration der Haut nicht ausreicht. Sie sollen femer zur Behandlung und Prophylaxe von Folgeschäden der Hautaustrocknung, beispielsweise Fissuren oder inflammatorischen oder allergischen Prozessen oder auch der Neurodermitis, geeignet sein. Aufgabe der vorliegenden Erfindung war es auch, stabile hautpflegende kosmetische und/oder dermatologische Mittel zur Verfügung zu stellen, welche die Haut vor Umwelteinflüssen wie Sonne und Wind schützen. Insbesondere sollte die Wirkung der Zubereitungen physiologisch, schnell und nachhaltig sein.However, the prior art lacks preparations which have a positive effect on the barrier function and hydration of the horny layer and which strengthen or even restore the physicochemical properties of the horny layer and in particular the lamellae made of intercellular lipids. The object of the present invention was therefore to eliminate the disadvantages of the prior art. In particular, skin-care preparations and preparations for cleaning the skin should be made available which maintain or restore the barrier properties of the skin, especially when the natural regeneration of the skin is insufficient. They should also be suitable for the treatment and prophylaxis of consequential damage to skin drying out, for example fissures or inflammatory or allergic processes or also neurodermatitis. It was also an object of the present invention to provide stable skin-care cosmetic and / or dermatological agents which protect the skin from environmental influences such as sun and wind. In particular, the effect of the preparations should be physiological, quick and sustainable.
Diese Aufgaben werden überraschend und für den Fachmann nicht vorhersehbar gelöst durch kosmetische und dermatologische Zubereitungen mit einem wirksamen Gehalt an Gal- iensäuren, ihren Salzen und/oder ihren Derivaten, wobei die genannten Wirkstoffe sowohl einzeln als auch im Gemisch vorliegen können.These objects are surprisingly and unpredictably achieved for the person skilled in the art by cosmetic and dermatological preparations with an effective content of bile acids, their salts and / or their derivatives, it being possible for the active substances mentioned to be present both individually and in a mixture.
Unter „Barrierestärkung" bzw. „Stärkung der Barrierefunktion der Haut" ist im Sinne der vorliegenden Erfindung insbesondere der folgende Effekt zu verstehen: Die erfindungsgemäßen Wirkstoffe interagieren mit den Lipiden der Hornschicht in der Art, daß die Anordnung dieser Lipide in der Hornschicht auf molekularer Ebene verbessert wird. Dies führt dazu, daß die natürliche Funktion der Haut als Barriere gegen Umwelteinflüsse und gegen den Verlust von körpereigenen Stoffen gestärkt oder wiederhergestellt wird.For the purposes of the present invention, “barrier strengthening” or “strengthening the barrier function of the skin” is to be understood in particular to mean the following effect: the active compounds according to the invention interact with the lipids of the horny layer in such a way that the arrangement of these lipids in the horny layer at the molecular level is improved. This means that the natural function of the skin as a barrier against environmental influences and against the loss of the body's own substances is strengthened or restored.
Die erfindungsgemäßen Zubereitungen sind in jeglicher Hinsicht überaus befriedigende Präparate. Es war für den Fachmann nicht vorauszusehen gewesen, daß die erfindungsgemäßen ZubereitungenThe preparations according to the invention are extremely satisfactory preparations in every respect. It was not foreseeable for the person skilled in the art that the preparations according to the invention
- besser die Barriereeigenschaften der Haut erhalten oder wiederherstellen,- better maintain or restore the skin's barrier properties,
- besser der Hautaustrocknung entgegenwirken,- counteract dehydration better,
- besser gegen die Hautalterung wirken und- work better against aging and
- die Haut besser vor Umwelteinflüssen schützen als die Zubereitungen des Standes der Technik.- protect the skin better from environmental influences than the preparations of the prior art.
Die Galle ist das exokrine Sekret der Leber, dessen Hauptbestandteile Wasser (86,7 %), Gallensäuren (9,1 %), Gallenfarbstoffe (3 %), Cholesterin (0,3 %) sowie Fettsäuren, Pro- teine und anorganische Substanzen sind. Die Funktion der Gallenflüssigkeit im Rahmen der Fettverdauung besteht in der Emulgation wasserunlöslicher Nahrungsbestandteile im Darmtrakt und in der Überführung wasserunlöslicher Verbindungen in die resorbierbaren Cholein- säuren. Zudem halten die Gallensäuren, welche in der Galle als Salze vorkommen, das Cholesterin in Lösung und erleichtern dessen Ausscheidung. Gallensäuren sind überwiegend mit Glycin (Giykocholsäure) oder Taurin (Taurocholsäure) konjugierte, substituierte Cholansäuren, die das folgende Strukturmotiv aufweisen:Bile is the exocrine secretion of the liver, the main components of which are water (86.7%), bile acids (9.1%), bile pigments (3%), cholesterol (0.3%) and fatty acids, pro teine and inorganic substances. The function of the bile in the context of fat digestion consists in the emulsification of water-insoluble food components in the intestinal tract and in the conversion of water-insoluble compounds into the resorbable cholic acids. In addition, the bile acids, which occur in the bile as salts, keep the cholesterol in solution and facilitate its excretion. Bile acids are predominantly substituted cholanic acids conjugated with glycine (glycocholic acid) or taurine (taurocholic acid), which have the following structural motif:
Vorteilhaft im Sinne der vorliegenden Erfindung sind beispielsweise Dehydrocholsäure, welche durch folgende Struktur gekennzeichnet ist, und ihre Salze:Advantageous for the purposes of the present invention are, for example, dehydrocholic acid, which is characterized by the following structure, and its salts:
Femer vorteilhaft sind Lithocholsäure, welche durch folgende Struktur gekennzeichnet ist, und ihre Salze:Also advantageous are lithocholic acid, which is characterized by the following structure, and its salts:
Femer vorteilhaft sind Cholsäure, welche durch folgende Struktur gekennzeichnet ist, und ihre Salze: Cholic acid, which is characterized by the following structure, and its salts are also advantageous:
Ferner vorteilhaft sind Giykocholsäure, welche durch folgende Struktur gekennzeichnet ist, und ihre Salze:Glycocholic acid, which is characterized by the following structure, and its salts are also advantageous:
Ferner vorteilhaft sind Taurolithocholsäure, welche durch folgende Struktur gekennzeichnet ist, und ihre Salze, insbesondere ihr Natriumsalz:Also advantageous are taurolithocholic acid, which is characterized by the following structure, and its salts, in particular its sodium salt:
Besonders bevorzugt im Sinne der vorliegenden Erfindung sind Desoxycholsäure, welche durch folgende Struktur gekennzeichnet ist, und ihre Salze:For the purposes of the present invention, particular preference is given to deoxycholic acid, which is characterized by the following structure, and its salts:
Ebenfalls besonders bevorzugt sind Ursodesoxycholsäure (Chenodesoxycholsäure), welche durch folgende Struktur gekennzeichnet ist, und ihre Salze: Also particularly preferred are ursodeoxycholic acid (chenodeoxycholic acid), which is characterized by the following structure, and its salts:
Werterhin besonders bevorzugt sind Taurocholsäure, welche durch folgende Struktur gekennzeichnet ist, und ihre Salze, insbesondere ihr Natriumsalz:Further particularly preferred are taurocholic acid, which is characterized by the following structure, and its salts, in particular its sodium salt:
Weiterhin vorteilhaft im Sinne der voriiegenden Erfindung sind auch die Ester und Ether der Gallensäuren, insbesondere die Ester und Ether der vorgenannten Gallensäuren.Also advantageous in the sense of the present invention are the esters and ethers of bile acids, in particular the esters and ethers of the aforementioned bile acids.
Gallensäureether sind durch eine Veretherung mindestens einer der Alkoholfunktionen in 3-, 7- oder 12-Position des Cholanringes erhältlich. Besonders bevorzugt sind Gallensäureether, die durch Veretherung der Alkoholfunktion in 3-Position erhältlich sind.Bile acid ethers can be obtained by etherification of at least one of the alcohol functions in the 3-, 7- or 12-position of the cholane ring. Bile acid ethers which are obtainable by etherification of the alcohol function in the 3-position are particularly preferred.
Vorteilhaft im Sinne der vorliegenden Erfindung sind Gallensäureether, welche durch eine Veretherung mit Ethylenoxid, gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen mit einer Kettenlänge von 2 bis 22 Kohlenstoffatomen erhältlich sind.For the purposes of the present invention, bile acid ethers which are obtainable by etherification with ethylene oxide, saturated and / or unsaturated, branched and / or unbranched alcohols having a chain length of 2 to 22 carbon atoms are advantageous.
Gallensäureester sind durch Veresterung mindestens einer der Alkoholfunktionen in 3-, 7- oder 12-Position des Cholanringes sowie durch Veresterung der endständigen Säurefunktionen erhältlich. Vorteilhaft im Sinne der vorliegenden Erfindung sind Gallensäureester, welche durch Veresterung mit gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Säuren mit einer Kettenlänge von 2 bis 22 Kohlenstoffatomen erhältlich sind.Bile acid esters can be obtained by esterifying at least one of the alcohol functions in the 3-, 7- or 12-position of the cholane ring and by esterifying the terminal acid functions. Advantageous in the sense of the present invention are bile acid esters, which by esterification with saturated and / or unsaturated, branched and / or unbranched acids with a chain length of 2 to 22 carbon atoms are available.
Ferner vorteilhaft sind Gallensäureester, welche durch Veresterung der endständigen Säurefunktion mit Ethylenoxid, gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen mit einer Kettenlänge von 2 bis 22 Kohlenstoffatomen erhältlich sind.Also advantageous are bile acid esters which can be obtained by esterifying the terminal acid function with ethylene oxide, saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 2 to 22 carbon atoms.
Weiterhin vorteilhaft im Sinne der vorliegenden Erfindung sind insbesondere auch die Salze der Gallensäuren, insbesondere die Alkali- und/oder Erdalkalisalze sowie die Salze der ein- oder zweiwertigen Kationen von Elementen der Nebengruppen sowie der Lanthanide und/oder Actinide. Desweiteren vorteilhaft sind auch Gallensäuresalze von Ammonium (-NH3), Alkanolammoniumderivaten mit 2 bis 9 C-Atomen insgesamt, Alkyl- oder Alkenyl- ammoniumderivaten mit 1 bis 22 C-Atomen insgesamt, Pyridin, welches mit einer Alkyl- oder Alkenylgruppe substituiert sein kann, die 1 bis 18 C-Atome hat, und basischer Aminosäuren. Erfindungsgemäß besonders bevorzugt sind die Natrium-, Kalium- und/oder Triethanolaminsalze der Gallensäuren.The salts of bile acids, in particular the alkali and / or alkaline earth metal salts, and the salts of the mono- or divalent cations of elements of the subgroups and of the lanthanides and / or actinides, are also particularly advantageous in the sense of the present invention. Also advantageous are bile acid salts of ammonium (-NH 3 ), alkanolammonium derivatives with 2 to 9 carbon atoms in total, alkyl or alkenylammonium derivatives with 1 to 22 carbon atoms in total, pyridine, which can be substituted with an alkyl or alkenyl group , which has 1 to 18 carbon atoms, and basic amino acids. The sodium, potassium and / or triethanolamine salts of bile acids are particularly preferred according to the invention.
Die erfindungsgemäßen kosmetischen oder dermatologischen Zubereitungen oder Formulierungen können wie üblich zusammengesetzt sein und zur Behandlung, der Pflege und der Reinigung der Haut und/oder der Haare und als Schminkprodukt in der dekorativen Kosmetik dienen. Entsprechend können sie, je nach ihrem Aufbau, beispielsweise verwendet werden als Hautschutzcreme, Reinigungsmilch, Sonnenschutzlotion, Nährcreme, Tages- oder Nachtcreme usw. Es ist gegebenenfalls möglich und vorteilhaft, die erfindungsgemäßen Zubereitungen als Grundlage für pharmazeutische Formulierungen zu verwenden. Die erfindungsgemäßen Zubereitungen enthalten z. B. 0,001 bis 10 Gew.-%, bevorzugt 0,01 Gew.-% bis 1 Gew.-%, insbesondere aber 0,01 Gew.-% bis 0,5 Gew.-%, jeweils bezogen auf das Gesamtgewicht der Zubereitungen an den erfindungsgemäßen Wirkstoffen.The cosmetic or dermatological preparations or formulations according to the invention can be composed as usual and can be used for the treatment, care and cleaning of the skin and / or hair and as a make-up product in decorative cosmetics. Correspondingly, depending on their structure, they can be used, for example, as a skin protection cream, cleansing milk, sunscreen lotion, nutritional cream, day or night cream, etc. It may be possible and advantageous to use the preparations according to the invention as the basis for pharmaceutical formulations. The preparations according to the invention contain z. B. 0.001 to 10 wt .-%, preferably 0.01 wt .-% to 1 wt .-%, but especially 0.01 wt .-% to 0.5 wt .-%, each based on the total weight of the preparations on the active substances according to the invention.
Günstig sind auch solche kosmetischen und dermatologischen Zubereitungen, die in der Form eines Sonnenschutzmittels vorliegen. Vorzugsweise enthalten diese neben einem oder mehreren erfindungsgemäßen Wirkstoffen mindestens eine UV-A-Filtersubstanz und/oder mindestens eine UV-B-FiKersubstanz und/oder mindestens ein anorganisches Pigment. Es ist aber auch vorteilhaft im Sinne der vorliegenden Erfindung, solche kosmetischen und dermatologischen Zubereitungen zu erstellen, deren hauptsächlicher Zweck nicht der Schutz vor Sonnenlicht ist, die aber dennoch einen Gehalt an UV-Schutzsubstanzen enthalten. So werden z. B. in Tagescremes gewöhnlich UV-A- bzw. UV-B-Filtersubstanzen eingearbeitet.Cosmetic and dermatological preparations which are in the form of a sunscreen are also favorable. In addition to one or more active substances according to the invention, these preferably contain at least one UV-A filter substance and / or at least one UV-B filter substance and / or at least one inorganic pigment. However, it is also advantageous for the purposes of the present invention to produce cosmetic and dermatological preparations whose main purpose is not protection against sunlight, but which nevertheless contain UV protection substances. So z. B. usually incorporated into day creams UV-A or UV-B filter substances.
Die erfindungsgemäßen kosmetischen und dermatologischen Zubereitungen können kosmetische Hilfsstoffe enthalten, wie sie üblicherweise in solchen Zubereitungen verwendet werden, z. B. Konservierungsmittel, Bakterizide, Parfüme, Substanzen zum Verhindern des Schäumens, Farbstoffe, Pigmente, die eine färbende Wirkung haben, Verdickungsmittel, oberflächenaktive Substanzen, Emulgatoren, weichmachende, anfeuchtende und/oder feuchthaltende Substanzen, Fette, Öle, Wachse oder andere übliche Bestandteile einer kosmetischen oder dermatologischen Formulierung wie Alkohole, Polyole, Polymere, Schaumstabilisatoren, Elektrolyte, organische Lösemittel oder Silikonderivate.The cosmetic and dermatological preparations according to the invention can contain cosmetic auxiliaries, as are usually used in such preparations, e.g. B. preservatives, bactericides, perfumes, anti-foaming substances, dyes, pigments that have a coloring effect, thickeners, surface-active substances, emulsifiers, softening, moisturizing and / or moisturizing substances, fats, oils, waxes or other common components of a cosmetic or dermatological formulation such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
Die jeweils einzusetzenden Mengen an kosmetischen, dermatologischen oder medizinischen Trägerstoffen und Parfüm können in Abhängigkeit von der Art des jeweiligen Produktes vom Fachmann durch einfaches Ausprobieren leicht ermittelt werden.The amounts of cosmetic, dermatological or medical carriers and perfume to be used in each case can easily be determined by a person skilled in the art depending on the type of product in question by simply trying them out.
Zubereitungen zur Behandlung und Pflege der Haut werden besonders bevorzugt.Preparations for the treatment and care of the skin are particularly preferred.
Zur Anwendung werden die erfindungsgemäßen kosmetischen und dermatologischen Zubereitungen in der für Kosmetika üblichen Weise auf die Haut und/oder die Haare in ausreichender Menge aufgebracht.For use, the cosmetic and dermatological preparations according to the invention are applied to the skin and / or the hair in a sufficient amount in the manner customary for cosmetics.
Erfindungsgemäße kosmetische und dermatologische Zubereitungen können in verschiedenen Formen vorliegen. So können sie z. B. eine Lösung, eine wasserfreie Zubereitung, eine Emulsion oder Mikroemulsion vom Typ Wasser-in-ÖI (W/O) oder vom Typ Öl-in-Wasser (O/W), eine multiple Emulsionen, beispielsweise vom Typ Wasser-in-ÖI-in-Wasser (W/O/W), ein Gel, einen festen Stift, eine Salbe oder auch ein Aerosol darstellen. Es ist auch vorteilhaft, die erfindungsgemäßen Wirkstoffe in verkapselter Form darzureichen, z. B. in Kollagenmatrices und anderen üblichen Verkapselungsmaterialien, z. B. als Cellulosever- kapselungen, in Gelatine, Wachsmatrices oder liposomal verkapselt. Es ist auch möglich und vorteilhaft im Sinne der vorliegenden Erfindung, die erfindungsgemäßen Wirkstoffe in wäßrige Systeme bzw. Tensidzubereitungen zur Reinigung der Haut und der Haare einzufügen.Cosmetic and dermatological preparations according to the invention can be in various forms. So you can z. B. a solution, an anhydrous preparation, an emulsion or microemulsion of the water-in-oil (W / O) or oil-in-water (O / W) type, a multiple emulsions, for example of the water-in-oil type Oil-in-water (W / O / W), a gel, a solid stick, an ointment or an aerosol. It is also advantageous to present the active compounds according to the invention in encapsulated form, e.g. B. in collagen matrices and other common encapsulation materials, e.g. B. as cellulose encapsulation, encapsulated in gelatin, wax matrices or liposomal. It is also possible and advantageous for the purposes of the present invention to insert the active compounds according to the invention into aqueous systems or surfactant preparations for cleaning the skin and hair.
Insbesondere können die erfindungsgemäßen kosmetischen und dermatologischen Zubereitungen auch Antioxidantien enthalten. Erfindungsgemäß können als günstige Antioxidantien alle für kosmetische und/oder dermatologische Anwendungen geeigneten oder gebräuchlichen Antioxidantien verwendet werden.In particular, the cosmetic and dermatological preparations according to the invention can also contain antioxidants. According to the invention, all the antioxidants suitable or customary for cosmetic and / or dermatological applications can be used as favorable antioxidants.
Vorteilhaft werden die Antioxidantien gewählt aus der Gruppe bestehend aus Aminosäuren (z. B. Glycin, Histidin, Tyrosin, Tryptophan) und deren Derivate, Imidazole (z. B. Urocanin- säure) und deren Derivate, Peptide wie D,L-Camosin, 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, Liponsäure und deren Derivate (z. B. Dihydroliponsäure), Aurothioglucose, Propylthiouracil und andere Thiole (z. B. Thioredoxin, Glutathion, Cystein, Cystin, Cystamin und deren Glykosyl-, N-Acetyl-, Methyl-, Ethyl-, Pro- pyl-, Amyl-, Butyl- und Lauryl-, Palmitoyl-, Oleyl-, γ-Linoleyl-, Cholesteryl- und Glycerylester) sowie deren Salze, Dilaurylthiodipropionat, Distearylthiodipropionat, Thiodipropionsäure und deren Derivate (Ester, Ether, Peptide, Lipide, Nukleotide, Nukleoside und Salze) sowie Sulf- oximinverbindungen (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. Crtronensäure, Milchsäure, Apfelsäure), Huminsäure, Gallensäure, Gallenextrakte, Bilirubin, Biliverdin, EDTA, EGTA und deren Derivate, ungesättigte Fettsäuren und deren Derivate (z. B. γ-Linolensäure, Linolsäure, Ölsäure), Folsäure und deren Derivate, Ubichinon und Ubichinol und deren Derivate, Vitamin C und Derivate (z. B. Ascorbylpalmitat, Mg-Ascorbylphosphat, Ascorbylacetat), Tocopherole und Derivate (z. B. Vitamin-E-acetat), Vitamin A und Derivate (Vitamin-A-pal- mitat) sowie Koniferylbenzoat des Benzoeharzes, Rutinsäure und deren Derivate, α- Glykosylrutin, Ferulasäure, Furfurylidenglucitol, Carnosin, Butylhydroxytoluol, Butylhydroxy- anisol, Nordihydroguajakharzsäure, Nordihydroguajaretsäure, Trihydroxybutyrophenon, Harnsäure und deren Derivate, Mannose und deren Derivate, Zink und dessen Derivate (z. B. ZnO, ZnSθ4), Selen und dessen Derivate (z. B. Selenmethionin), Stilbene und derenThe antioxidants are advantageously selected from the group consisting of amino acids (e.g. glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (e.g. urocanic acid) and their derivatives, peptides such as D, L-camosine, D-carnosine, L-carnosine and their derivatives (e.g. anserine), carotenoids, carotenes (e.g. α-carotene, ß-carotene, lycopene) and their derivatives, chlorogenic acid and its derivatives, lipoic acid and its 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, palmitoyl, oleyl, γ-linoleyl, cholesteryl and glyceryl esters) and their salts, dilauryl thiodipropionate, distearyl thiodipropionate, thiodipropionic acid and their derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) as well as sulfoximine compounds (e.g. buthionine sulfoximines, homocysteine sulfoximine, buthioni nsulfones, penta-, hexa-, heptathioninsulfoximine) in very low tolerable doses (e.g. B. pmol to μmol / kg), further (metal) chelators (e.g. α-hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), α-hydroxy acids (e.g. crtronic acid, lactic acid, malic acid), humic acid, bile acid, Bile extracts, bilirubin, biliverdin, EDTA, EGTA and their derivatives, unsaturated fatty acids and their derivatives (e.g. γ-linolenic acid, linoleic acid, oleic acid), folic acid and their derivatives, ubiquinone and ubiquinol and their derivatives, vitamin C and derivatives (e.g. B. Ascorbyl palmitate, Mg ascorbyl phosphate, ascorbyl acetate), tocopherols and derivatives (e.g. vitamin E acetate), vitamin A and derivatives (vitamin A palmitate) and coniferyl benzoate of benzoin, rutinic acid and its derivatives, α-Glycosylrutin, ferulic acid, furfurylidene glucitol, carnosine, butylated hydroxytoluene, butylated hydroxy anisole, nordihydroguajak resin acid, nordihydroguajaretic acid, trihydroxybutyrophenone, uric acid and its derivatives, mannose and their derivatives, zinc and its derivatives, e.g. Zn 4), selenium and its derivatives (e.g. B. selenomethionine), stilbene and their
Derivate (z. B. Stilbenoxid, Trans-Stilbenoxid) und die erfindungsgemäß geeigneten Deriva- te (Salze, Ester, Ether, Zucker, Nukleotide, Nukleoside, Peptide und Lipide) dieser genannten Wirkstoffe.Derivatives (e.g. stilbene oxide, trans-stilbene oxide) and the derivatives suitable according to the invention te (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids) of these active ingredients.
Die Menge der vorgenannten Antioxidantien (eine oder mehrere Verbindungen) in den erfindungsgemäßen 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 aforementioned antioxidants (one or more compounds) in the preparations according to the invention 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 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 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.
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 A or vitamin A derivatives or carotenes or their derivatives represent the antioxidant or antioxidants, it is advantageous to use their respective concentrations in the range from 0.001-10% by weight, based on the total weight of the formulation, to choose.
Die nachfolgenden Beispiele sollen die vorliegende Erfindung verdeutlichen, ohne sie einzuschränken. Die Zahlenwerte in den Beispielen bedeuten Gewichtsprozente, bezogen auf das Gesamtgewicht der jeweiligen Zubereitungen. The following examples are intended to illustrate the present invention without restricting it. The numerical values in the examples mean percentages by weight, based on the total weight of the respective preparations.
Beispielrezepturen:Example recipes:
1. Lecithin-Fluid1. Lecithin fluid
Gew.-%% By weight
Lecithin 5,00Lecithin 5.00
Ursodesoxycholsäure 0,50Ursodeoxycholic acid 0.50
Cetearylalkohol 1 ,00Cetearyl alcohol 1.00
Glycerin 3,00Glycerin 3.00
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Wasser ad 100Water ad 100
2. Hvdrodispersionsgel2. Hvdrodispersion gel
Gew.-%% By weight
Stearylalkohol 2,00Stearyl alcohol 2.00
Behenylalkohol 2,00Behenyl alcohol 2.00
Ceramid 3 0,20Ceramide 3 0.20
Taurodesoxycholsäure 0,10Taurodeoxycholic acid 0.10
Carbopol 0,30Carbopol 0.30
Hydroxyethylcellulose 0,40Hydroxyethyl cellulose 0.40
Glycerin 3,00Glycerin 3.00
Panthenol 1 ,00Panthenol 1, 00
Caprylic / Capric Triglycerid 3,00Caprylic / Capric Triglyceride 3.00
Isopropylpalmitat 3,00Isopropyl palmitate 3.00
Shea Butter 2,00Shea Butter 2.00
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s.Antioxidants, preservatives, neutralizing agents, q.s.
Parfüm, FarbstoffePerfume, dyes
Wasser ad 100 3. Leichtes GelWater ad 100 3. Light gel
Gew.-%% By weight
Sucrosestearat 3,00Sucrose stearate 3.00
Cetearylalkohol 2,00Cetearyl alcohol 2.00
Desoxycholsäure 0,02Deoxycholic acid 0.02
Carbopol 0,50Carbopol 0.50
Glycerin 3,00Glycerin 3.00
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Wasser ad 100Water ad 100
4. O/W Creme4. O / W cream
Gew.-%% By weight
Sucrosestearat 4,00Sucrose stearate 4.00
Sucroselaurat 2,00Sucroselaurate 2.00
Taurolithocholsäure 0,02Taurolithocholic acid 0.02
Cetearylalkohol 3,00Cetearyl alcohol 3.00
Glycerin 3,00Glycerin 3.00
Dimethicone 2,00Dimethicone 2.00
Mineralöl 5,00Mineral oil 5.00
Isopropylpalmitat 3,00Isopropyl palmitate 3.00
Sonnenblumenöl 3,00Sunflower oil 3.00
Hydrierte Kokosfettsäureglyceride 2,50Hydrogenated coconut fatty acid glycerides 2.50
Süßholzwurzelextrakt 2,00Liquorice root extract 2.00
Carbomer 0,20Carbomer 0.20
NaOH 45%ig 0,10NaOH 45% 0.10
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Wasser ad 100 5. O/W-LotionWater ad 100 5. O / W lotion
Gew.-%% By weight
Stearinsäure 1 ,50Stearic acid 1, 50
Sorbitanmonostearat 0,50Sorbitan monostearate 0.50
U rsodesoxycholsäu re 0,05U rsodeoxycholic acid 0.05
Myristylalkokol 1,00Myristyl alcohol 1.00
Glycerinmonostearat 0,50Glycerol monostearate 0.50
Paraffinöl, subliquidum 10,00Paraffin oil, subliquidum 10.00
Dimethicone 1 ,00Dimethicone 1, 00
Octyldodecanol 2,00Octyldodecanol 2.00
Hydrierte Kokosfettsäureglyceride 0,50Hydrogenated coconut fatty acid glycerides 0.50
Carbomer 0,10Carbomer 0.10
Serin 0,50Serine 0.50
Glycerin 5,00Glycerin 5.00
Tocopherolacetat 0,50Tocopherol acetate 0.50
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s.Antioxidants, preservatives, neutralizing agents, q.s.
Parfüm, FarbstoffePerfume, dyes
Wasser ad 100Water ad 100
6. W/O-Lotion6. W / O lotion
Gew.-%% By weight
PEG-7-hydriertes Ricinusöl 4,00PEG-7 hydrogenated castor oil 4.00
Giykocholsäure 0,01Glycocholic acid 0.01
Bienenwachs 3,00Beeswax 3.00
Vaseline 4,00Vaseline 4.00
Ozokerit 4,00Ozokerite 4.00
Paraffinöl, subliquidum 10,00Paraffin oil, subliquidum 10.00
Glycerin 5,00Glycerin 5.00
Octyl Methoxycinnamat 2,50Octyl methoxycinnamate 2.50
Methylbenzyliden Campher 2,50Methylbenzylidene camphor 2.50
Tocopherolacetat 1 ,00Tocopherol acetate 1.00
Magnesiumsulfat 7 H2O 0,70Magnesium sulfate 7 H 2 O 0.70
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s.Antioxidants, preservatives, neutralizing agents, q.s.
Parfüm, FarbstoffePerfume, dyes
Wasser ad 100 Gew.-%Water ad 100 % By weight
PEG-7-hydriertes Ricinusöl 4,00PEG-7 hydrogenated castor oil 4.00
Wollwachsalkohol 1 ,50Wool wax alcohol 1, 50
Desoxycholsäure 0,05Deoxycholic acid 0.05
Vaseline 9,00Vaseline 9.00
Ozokerit 4,00Ozokerite 4.00
Paraffinöl, subliquidum 10,00Paraffin oil, subliquidum 10.00
Urea 10,00Urea 10.00
Magnesiumsulfat 7 H2O 0,70Magnesium sulfate 7 H 2 O 0.70
Milchsäure 0.30Lactic acid 0.30
Natriumiaktat 2,50Sodium lactate 2.50
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Wasser ad 100Water ad 100
8. Silikonemulsion8. Silicone emulsion
Gew.-%% By weight
Dimethicone Copolyol 2,00Dimethicone copolyol 2.00
Cylomethicone 5,00Cylomethicone 5.00
Dimethicone 3,00Dimethicone 3.00
Paraffinöl, subliquidum 8,00Paraffin oil, subliquidum 8.00
Weizenkeimöl 4,00Wheat germ oil 4.00
Dehydrocholsäure 0,02Dehydrocholic acid 0.02
Glycerin 10,00Glycerin 10.00
Natriumchlorid 1 ,00Sodium chloride 1.00
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Wasser ad 100 9. SalbeWater ad 100 9. Ointment
Gew.-%% By weight
Vaseline 36,00Vaseline 36.00
Ceresin 10,00Ceresin 10.00
Zinkoxid 4,00Zinc oxide 4.00
Weizenkeimöl 20,00Wheat germ oil 20.00
Taurocholsäure 0,02Taurocholic acid 0.02
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Paraffinöl ad 100Paraffin oil ad 100
10. Hautöl10. Skin oil
Gew.-%% By weight
Cetylpalmitat 3,00Cetyl palmitate 3.00
C12-15 Alkylbenzoat 2,00C12-15 alkyl benzoate 2.00
Polyisobuten 10,00Polyisobutene 10.00
Squalan 2,00Squalane 2.00
Ursodesoxycholsäure 0,05Ursodeoxycholic acid 0.05
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Paraffinöl ad 100Paraffin oil ad 100
11. Badeöl11. Bath oil
Gew.-%% By weight
Paraffinöl 20,00Paraffin oil 20.00
PEG-40 Hydrogeniertes Ricinusöl 5,00PEG-40 Hydrogenated castor oil 5.00
Desoxycholsäure 0,50Deoxycholic acid 0.50
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Sojaöl ad 100 12. LippenpflegestiftSoybean oil ad 100 12. Lip care stick
Gew.-%% By weight
Caprylic/Capric Triglycerid 25,00Caprylic / Capric triglyceride 25.00
Octyldodecanol 25,00Octyldodecanol 25.00
Ceramid 3 0,50Ceramide 3 0.50
Ursodesoxycholsäure 0,20Ursodeoxycholic acid 0.20
Bienenwachs 20,00Beeswax 20.00
Cetylpalmitat 8,00Cetyl palmitate 8.00
Jojoba Öl 5,00Jojoba oil 5.00
Carnauba Wachs 4,00Carnauba wax 4.00
Tocopherolacetat 0,75Tocopherol acetate 0.75
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s.Antioxidants, preservatives, neutralizing agents, q.s.
Parfüm, FarbstoffePerfume, dyes
Squalan ad 100Squalane ad 100
13. Emulsions-Lippenpfleqestift13. Emulsion lip care stick
Gew.-%% By weight
Caprylic/Capric Triglyceride 30,00Caprylic / Capric Triglyceride 30.00
Octyldodecanol 20,00Octyldodecanol 20.00
Polyglyceryl-3 Dioleat 3,50Polyglyceryl-3 dioleate 3.50
Bienenwachs 10,00Beeswax 10.00
Dehydrocholsäure 0,10Dehydrocholic acid 0.10
C2(Mo Alkylstearat 5,00C 2 (M o alkyl stearate 5.00
Jojoba Öl 5,00Jojoba oil 5.00
Carnauba Wachs 2,00Carnauba wax 2.00
Tocopherolacetat 0,75Tocopherol acetate 0.75
Wasser 5,00Water 5.00
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Squalan ad 100 14. LippenstiftSqualane ad 100 14. Lipstick
Gew.-%% By weight
Caprylic/Capric Triglycerid 22,00Caprylic / Capric triglyceride 22.00
Octyldodecanol 22,00Octyldodecanol 22.00
Ursodesoxycholsäure 0,20Ursodeoxycholic acid 0.20
PEG-5 Soyasterol 0,50PEG-5 soyasterol 0.50
Bienenwachshydrolysat 5,00Beeswax hydrolyzate 5.00
Bienenwachs 15,00Beeswax 15.00
Cetylpalmitat 2,00Cetyl palmitate 2.00
Jojoba Öl 5,00Jojoba oil 5.00
Carnauba Wachs 2,00Carnauba wax 2.00
Tocopherolacetat 0,75Tocopherol acetate 0.75
Farbpigmente, Farblacke.Titandioxid q,s.Color pigments, color lacquers, titanium dioxide q, p.
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q,s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q, s. Perfume, dyes
Squalan ad 100 Squalane ad 100
15. Emulsions-Make-up15. Emulsion makeup
Gew.-%% By weight
Sorbitanmonostearat 1,50Sorbitan monostearate 1.50
Sorbitanmonooleat 1 ,00Sorbitan monooleate 1.00
Glycerinmonostearat 1 ,00Glycerol monostearate 1, 00
Taurocholsäure 0,20Taurocholic acid 0.20
Glyceryllanolat 1,00Glyceryl alcoholate 1.00
Paraffinöl, subliquidum 7,00Paraffin oil, subliquidum 7.00
Octyldodecanol 7,00Octyldodecanol 7.00
Hydrierte Kokosfettsäureglyceride 4,00Hydrogenated coconut fatty acid glycerides 4.00
Octyl Methoxycinnamat 2,00Octyl methoxycinnamate 2.00
Butylmethoxydibenzoylmethan 1 ,00Butyl methoxydibenzoyl methane 1.00
Carbomer 0,10Carbomer 0.10
Glycerin 5,00Glycerin 5.00
1 ,3 Butylenglycol 2,001, 3 butylene glycol 2.00
Tocopherolacetat 1 ,00Tocopherol acetate 1.00
Stärke Natriumoctenylsuccinat (Amiogum® von der American 2,50Strength Natriumoctenylsuccinat (Amiogum ® from the American 2.50
Maize-Products Company / CERSTAR)Maize-Products Company / CERSTAR)
Magnesiumsilikat 1,00Magnesium silicate 1.00
Glimmer 1 ,00Mica 1, 00
Eisenoxide 1 ,00Iron oxides 1, 00
Titandioxid 2,50Titanium dioxide 2.50
Talkum 5,00Talc 5.00
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s.Antioxidants, preservatives, neutralizing agents, q.s.
Parfüm, FarbstoffePerfume, dyes
Wasser ad 100 Water ad 100
16. Haarpflegemittel16. Haircare products
Gew.-%% By weight
TEA - Cocoyl hydrolysiertes Kollagen 30,00TEA - Cocoyl hydrolyzed collagen 30.00
Monoethanolaminlaurylsulfat 25,00Monoethanolamine lauryl sulfate 25.00
Mandelöl 2,00Almond oil 2.00
PEG-25 Sojasterol 2,00PEG-25 Soyasterol 2.00
Desoxycholsäure 0,20Deoxycholic acid 0.20
Natrium Chlorid 1 ,00Sodium chloride 1.00
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Wasser ad 100Water ad 100
17. Pflegeshampoo17.Care shampoo
Gew.-%% By weight
Natriumlaurylsulfat 34,00Sodium lauryl sulfate 34.00
Dinatriumlauryisulfosuccinat 6,00Disodium lauryl sulfosuccinate 6.00
Cocoamidopropylbetain 10,00Cocoamidopropyl betaine 10.00
Lithocholsäure 0,02Lithocholic acid 0.02
Glykoldistearat 5,00Glycol distearate 5.00
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Wasser ad 100 Water ad 100
18. Pumpsprav18. Pumpsprav
Gew.-%% By weight
PEG-40 Hydriertes Ricinusöl 2,00PEG-40 hydrogenated castor oil 2.00
Glycerin 1 ,00Glycerin 1, 00
PEG-25 Sojasterol 2,00PEG-25 Soyasterol 2.00
Giykocholsäure 0,02Glycocholic acid 0.02
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Wasser ad 100Water ad 100
19. Roll-on Emulsion19. Roll-on emulsion
Gew.-%% By weight
Tricetearethphosphat 0,30Triceteareth phosphate 0.30
Octyldodecanol 2,00Octyldodecanol 2.00
C12-1S Alkylbenzoat 2,00C1 2 -1S alkyl benzoate 2.00
C10-30 Alkylacrylat 0,15C 1 0-30 alkyl acrylate 0.15
Taurolithocholsäure 0,05Taurolithocholic acid 0.05
Antioxidantien, Konservierungsmittel, Neutralisationsmittel, q.s. Parfüm, FarbstoffeAntioxidants, preservatives, neutralizing agents, q.s. Perfume, dyes
Wasser ad 100 Water ad 100

Claims

Patentansprüche: Claims:
1. Kosmetische und dermatologische Zubereitungen mit einem wirksamen Gehalt an Gallensäuren, ihren Salzen und/oder ihren Derivaten, wobei die genannten Wirkstoffe sowohl einzeln als auch im Gemisch vorliegen können.1. Cosmetic and dermatological preparations with an effective content of bile acids, their salts and / or their derivatives, it being possible for the active substances mentioned to be present both individually and in a mixture.
2. Zubereitungen nach Anspruch 1, dadurch gekennzeichnet, daß zusätzlich kosmetische oder dermatologische Hilfs-, Zusatz- und/oder Wirkstoffe enthalten sind.2. Preparations according to claim 1, characterized in that additional cosmetic or dermatological auxiliaries, additives and / or active ingredients are included.
3. Zubereitungen nach einem der vorhergehenden Ansprüche, dadurch gekennzeichnet, daß der Gehalt an einer oder mehreren Gallensäuren, ihren Salzen und/oder ihren Derivaten in den kosmetischen oder dermatologischen Zubereitungen aus dem Bereich 0,001 bis 10 Gew.-%, bevorzugt 0,01 Gew.-% bis 1 Gew.-%, insbesondere aber 0,01 Gew.-% bis 0,5 Gew.-%, jeweils bezogen auf das Gesamtgewicht der Zubereitungen, gewählt wird.3. Preparations according to one of the preceding claims, characterized in that the content of one or more bile acids, their salts and / or their derivatives in the cosmetic or dermatological preparations from the range 0.001 to 10 wt .-%, preferably 0.01 wt % to 1% by weight, but in particular 0.01% by weight to 0.5% by weight, in each case based on the total weight of the preparations.
4. Zubereitungen nach einem der vorhergehenden Ansprüche, dadurch gekennzeichnet, daß der oder die Wirkstoffe gewählt werden aus der Gruppe Desoxycholsäure, Ursodesoxycholsäure, Taurocholsäure und/oder deren Salze und/oder deren Derivate.4. Preparations according to one of the preceding claims, characterized in that the active ingredient or ingredients are selected from the group deoxycholic acid, ursodeoxycholic acid, taurocholic acid and / or their salts and / or their derivatives.
5. Zubereitungen nach einem der vorhergehenden Ansprüche, dadurch gekennzeichnet, daß der oder die Wirkstoffe gewählt werden aus der Gruppe der Ester und Ether der Galiensäuren.5. Preparations according to one of the preceding claims, characterized in that the active ingredient or ingredients are selected from the group of esters and ethers of galienic acids.
6. Zubereitungen nach einem der vorhergehenden Ansprüche, dadurch gekennzeichnet, daß der oder die Wirkstoffe gewählt werden aus der Gruppe der Salze der Gallensäuren, insbesondere der Alkali- und Erdalkalisalze, der Salze der ein- oder zweiwertigen Kationen von Elementen der Nebengruppen sowie der Lanthanide und Actinide, der Salze von Ammonium (-NH3), Alkanolammoniumderivaten mit 2 bis 9 C-Atomen insgesamt, Alkyl- und Alkenylammoniumderivaten mit 1 bis 22 C-Atomen insgesamt, Pyridin, welches mit einer Alkyl- oder Alkenylgruppe substituiert sein kann, die 1 bis 18 C-Atome hat sowie der Salze basischer Aminosäuren.6. Preparations according to one of the preceding claims, characterized in that the active ingredient or ingredients are selected from the group consisting of the salts of bile acids, in particular the alkali and alkaline earth metal salts, the salts of the mono- or divalent cations of elements of the subgroups and the lanthanides and Actinides, the salts of ammonium (-NH 3 ), alkanolammonium derivatives with 2 to 9 carbon atoms in total, alkyl and alkenylammonium derivatives with 1 to 22 carbon atoms in total, pyridine, which can be substituted with an alkyl or alkenyl group, the 1st has up to 18 carbon atoms and the salts of basic amino acids.
7. Verwendung von Zubereitungen nach einem der Ansprüche 1 bis 6 zur Stärkung der Barrierefunktion der Haut. 7. Use of preparations according to one of claims 1 to 6 for strengthening the barrier function of the skin.
EP99938295A 1998-08-01 1999-07-20 Cosmetic and dermatological preparations comprising an effective content of bile acids, their salts and/or their derivatives Withdrawn EP1100455A1 (en)

Applications Claiming Priority (3)

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DE19834814A DE19834814A1 (en) 1998-08-01 1998-08-01 Cosmetic and dermatological preparations with an effective content of bile acids, their salts and / or their derivatives
DE19834814 1998-08-01
PCT/EP1999/005157 WO2000007557A1 (en) 1998-08-01 1999-07-20 Cosmetic and dermatological preparations comprising an effective content of bile acids, their salts and/or their derivatives

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EP1100455A1 true EP1100455A1 (en) 2001-05-23

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DE19834814A1 (en) 2000-02-03
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WO2000007557A1 (en) 2000-02-17

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