EP1696903A1 - Combination of 2,3-dibenzylbutyrolactone and licochalcone-a - Google Patents

Combination of 2,3-dibenzylbutyrolactone and licochalcone-a

Info

Publication number
EP1696903A1
EP1696903A1 EP04819609A EP04819609A EP1696903A1 EP 1696903 A1 EP1696903 A1 EP 1696903A1 EP 04819609 A EP04819609 A EP 04819609A EP 04819609 A EP04819609 A EP 04819609A EP 1696903 A1 EP1696903 A1 EP 1696903A1
Authority
EP
European Patent Office
Prior art keywords
skin
preparations
polyethylene glycol
weight
acid
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Withdrawn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
EP04819609A
Other languages
German (de)
French (fr)
Inventor
Stefan Gallinat
Ludger Kolbe
Christopher Mummert
Rainer Wolber
Franz STÄB
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
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Beiersdorf AG filed Critical Beiersdorf AG
Publication of EP1696903A1 publication Critical patent/EP1696903A1/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Withdrawn legal-status Critical Current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
    • A61Q19/08Anti-ageing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • A61K31/121Ketones acyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/48Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/484Glycyrrhiza (licorice)
    • 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
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/35Ketones, e.g. benzophenone
    • 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
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • 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
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/18Antioxidants, e.g. antiradicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61Q17/04Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
    • 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
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/004Aftersun preparations

Definitions

  • the present invention relates to cosmetic or dermatological preparations containing active ingredients for the care and protection of the skin, in particular sensitive skin, and very particularly in the foreground of skin aged or aging due to intrinsic and / or extrinsic factors, and the use of such active ingredients and combinations of such active ingredients in the field of cosmetic and dermatological skin care.
  • Cosmetic skin care is primarily to be understood as meaning that the natural function of the skin as a barrier against environmental influences (eg dirt, chemicals, microorganisms) and against the loss of the body's own substances (eg water, natural fats, electrolytes) is strengthened or restored ,
  • the barrier effect of the skin can be quantified by determining the transepidermal water loss (TEWL - transepidermal water loss). 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 uppermost skin layer is of the greatest importance for the beauty and care of the skin. 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 skin's barrier function. In this case, a new, often very unfavorable 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.
  • the changes in the lipid pattern of the very dry, non-eczematous skin of patients with atopic eczema represent an extreme case for the deviations that are found in the dry skin of healthy people.
  • ceramides which are greatly reduced in their quantity and are also composed differently.
  • the deficit in ceramides 1 and 3 is particularly striking, it being known in particular for ceramide 1 that it increases the order of the lipids in the intercellular membrane systems in a special way.
  • Adverse changes in the lipid membranes of the type described above may be due to miscontrolled lipid biosynthesis and also ultimately increase transepidermal water loss. Long-lasting barrier weakness, in turn, makes healthy skin more sensitive and in individual cases can contribute to the development of eczematous processes in the diseased skin.
  • the effect of ointments and creams on the barrier function and hydration of the horny layer usually does not consist in restoring or strengthening the physicochemical properties of the lamellae made of intercellular lipids.
  • a major partial effect is due to the mere covering of the treated skin areas and the resulting water retention in the underlying horny layer.
  • Co-applied hygroscopic Substances bind the water so that there is a measurable increase in the water content in the horny layer.
  • this purely physical barrier can be removed relatively easily.
  • the skin care effect can diminish with regular treatment, so that the status quo is finally reached again even during treatment.
  • the condition of the skin may temporarily worsen after discontinuation.
  • a sustainable product effect is not achieved or only to a limited extent.
  • the aim of the present invention was therefore to find ways to avoid the disadvantages of the prior art.
  • the effects of skin care products should be physiological, quick and sustainable.
  • 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, chemicals, 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, chemicals, microorganisms
  • the loss of the body's own substances e.g. water, lipids
  • Electrolytes e.g. water, lipids
  • 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 easily for example with cleaning agents - are removed again, whereby 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 state before the start of treatment. With certain products, the condition of the skin may even temporarily deteriorate. As a rule, a sustainable product effect is not achieved or only to a limited extent.
  • the effect of nourishing cleansing products is essentially an efficient regreasing with sebum lipid-like substances.
  • the damage to the homolayer 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 of the lamellae from 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 skin's barrier properties, especially when the natural regeneration of the skin is not sufficient. 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.
  • the effect of the preparations should be physiological, quick and sustainable.
  • the invention relates to preparations with extremely low so-called "stinging potential".
  • Typical reactions of "stinging" to sensitive skin are reddening, tension and burning of the skin as well as itching.
  • Cutting 'phenomena can be regarded as disorders to be treated cosmetically.
  • severe itching particularly severe itching in the case of atopy, can also be described as a more serious dermatological disorder.
  • Typical disturbing neurosensory phenomena associated with the terms "stinging” or “sensitive skin” are reddening of the skin, tingling, tingling, tension and burning of the skin and itching.
  • PJFrosch and AMKligman describe a method for estimating the "stinging potential" of topically administered substances.
  • Lactic acid and pyruvic acid for example, are used here as positive substances.
  • amino acids, in particular glycine were also found to be neurosensory active (such substances are called “Stinger”). According to previous knowledge, such a sensitivity to very specific substances occurs individually in different ways. This means that a person who experiences “stinging effects" when in contact with a substance is very likely to experience it repeatedly with each subsequent contact. Contact with other "Stingers" can just as easily be without any reaction.
  • Sensitive skin affects a growing number of adults and children. Sensitive skin is a combination of various symptoms, such as hyper-reactive and intolerant skin. But atopic skin can also be summed up. These skin conditions are often affected by those affected, not entirely correct, referred to as "allergic" skin. Although an allergic disease can lead to symptoms of sensitive skin, the appearance of "sensitive skin” is not limited to allergy sufferers
  • Erythematous skin symptoms also appear as a side effect with certain skin diseases or irregularities. For example, the typical rash in the appearance of acne is usually more or less reddened.
  • active substances and preparations containing such active substances should be made available for the cosmetic and dermatological treatment and / or prophylaxis of erythematous, inflammatory, allergic or autoimmune-reactive symptoms, in particular dermatoses, but also the appearance of the "stinging".
  • active substances or preparations containing such active substances should be made available which can be used for immune stimulation of the skin, advantageously also for immune stimulation in the sense of the effect promoting wound healing.
  • the present invention relates to cosmetic and dermatological preparations for the prophylaxis and treatment of cosmetic or dermatological skin changes such as, for example, the undesired pigmentation, for example local hyper- and deficient pigmentations (for example liver spots, freckles), but also for purely cosmetic lightening of larger, the individual skin type of adequately pigmented skin areas.
  • Melanocytes are responsible for the pigmentation of the skin. They can be found in the bottom layer of the epidermis, the stratum basale, next to the basal cells as - depending on the skin type, either isolated or more or less frequently occurring pigment-forming cells.
  • melanocytes contain melanosomes which, when stimulated by UV radiation, form increased melanin. This is transported into the keratinocyte and causes a more or less pronounced brown or brown skin color.
  • Melanin is formed as the final stage of an oxidative process in which tyrosine with the help of the enzyme tyrosinase via 3,4-dihydroxyphenylalanine (dopa), dopa-quinone, leucodopachrome, dopachrome, 5,6-dihydroxyindole and indole-5,6-quinone finally in Melanin is converted.
  • UV radiation e.g. freckles, ephe- lides
  • genetic disposition e.g. incorrect pigmentation of the skin during wound healing or scarring or skin aging (e.g. Lentigines seniles).
  • the object of the present invention was also to remedy these shortcomings.
  • the aim of skin care is also to compensate for the loss of fat and water in the skin caused by daily washing. This is especially important when the natural regeneration ability is insufficient.
  • skin care products are intended to protect against environmental influences, especially sun and wind, and to delay skin aging.
  • Chronological skin aging is caused, for example, by endogenous, genetically determined factors. The following structural damage and functional disorders occur in the epidermis and dermis due to aging, which can also fall under the term "senile xerosis":
  • Exogenous factors such as UV light and chemical pollutants can be cumulative and e.g. accelerate or complement the endogenous aging processes.
  • exogenous factors e.g. the following structural damage and functional disorders in the skin that go beyond the extent and quality of the damage with chronological aging:
  • the present invention relates in particular to products for the care of naturally aged skin and for the treatment of the consequential damage caused by light aging, in particular the phenomena listed under a) to g).
  • Products for the care of aged skin are known per se. They contain e.g. Retinoids (vitamin A acid and / or its derivatives) or vitamin A and / or its derivatives.
  • Retinoids vitamin A acid and / or its derivatives
  • their effect on structural damage is limited in scope.
  • the use of products containing vitamin A acid often causes severe erythematous skin irritation. Retinoids can therefore only be used in low concentrations.
  • the present invention relates to cosmetic preparations with effective protection against harmful oxidation processes in the skin, but also for protection cosmetic preparations themselves or to protect the components of cosmetic preparations from harmful oxidation processes.
  • the present invention further relates to antioxidants, preferably those which are used in skin-care cosmetic or dermatological preparations.
  • the invention also relates to cosmetic and dermatological preparations containing such antioxidants.
  • the present invention relates to cosmetic and dermatological preparations for the prophylaxis and treatment of cosmetic or dermatological skin changes such as e.g. skin aging, especially skin aging caused by oxidative processes.
  • the present invention further relates to active substances and preparations containing such active substances for cosmetic and dermatological treatment or prophylaxis of erythematous, inflammatory, allergic or autoimmune-reactive symptoms, in particular dermatoses.
  • the present invention relates to active substance combinations and preparations which are used for the prophylaxis and treatment of light-sensitive skin, in particular photodermatoses.
  • UVC range rays with a wavelength shorter than 290 nm
  • UVB range rays in the range between 290 nm and 320 nm, the so-called UVB range, cause an erythema simple sunburn or even more or less severe burns.
  • the narrower range around 308 nm is given as a maximum of the erythema effectiveness of sunlight.
  • UVB radiation which are derivatives of 3-benzylidene camphor, 4-aminobenzoic acid, cinnamic acid, salicylic acid, benzophenone and also 2-phenylbenzimidazole. It is also important to have filter substances available for the range between about 320 nm and about 400 nm, the so-called UVA range, since their rays can cause reactions in light-sensitive skin. It has been proven that UVA radiation damages the elastic and collagen fibers of the connective tissue, which causes the skin to age prematurely, and that it can be seen as the cause of numerous phototoxic and photoallergic reactions. The damaging influence of UVB radiation can be intensified by UVA radiation.
  • UV radiation can also lead to photochemical reactions, in which case the photochemical reaction products interfere with the skin's metabolism.
  • Such photochemical reaction products are predominantly free radical compounds, for example hydroxyl radicals, singlet oxygen.
  • Undefined radical photo products which are created in the skin itself, can also display uncontrolled subsequent reactions due to their high reactivity.
  • singlet oxygen a non-radical excited state of the oxygen molecule can occur with UV radiation, just as short-lived epoxies and many others.
  • Singlet oxygen for example, is characterized by increased reactivity compared to the triplet oxygen (radical ground state) that is normally present. However, there are also excited, reactive (radical) triplet states of the oxygen molecule.
  • UV radiation also belongs to ionizing radiation. There is therefore a risk that ionic species also develop when exposed to UV, which in turn can then oxidatively intervene in the biochemical processes.
  • antioxidants and / or free radical scavengers can be incorporated into the cosmetic or dermatological formulations.
  • vitamin E a substance with a known antioxidant effect, in light protection formulations, but the efficacy achieved here still remains. kung far behind the hoped for.
  • the object of the invention was therefore also to provide cosmetic, dermatological and pharmaceutical active substances and preparations and light protection formulations which are used for the prophylaxis and treatment of light-sensitive skin, in particular photodermatoses, preferably PLD.
  • Antioxidants are mainly used as protective substances against the spoilage of the preparations containing them. Nevertheless, it is known that undesirable oxidation processes can also occur in human and animal skin. Such processes play an essential role in skin aging.
  • antioxidants and / or free radical scavengers can be incorporated into cosmetic or dermatological formulations.
  • antioxidants and radical scavengers are known. It has already been proposed in US Pat. Nos. 4,144,325 and 4,248,861 and from numerous other documents to use vitamin E, a substance with a known antioxidant effect in sunscreen formulations, but the effect achieved here also falls far short of the hoped-for effect.
  • the object of the present invention was therefore to find ways which avoid the disadvantages of the prior art.
  • the effect of repairing the damage associated with endogenous, chronological and exogenous skin aging and the Prophylaxis to be permanent, sustainable and without the risk of side effects.
  • active ingredient combinations according to the invention or cosmetic or topical dermatological preparations with an effective content of active ingredient combinations according to the invention surprisingly offers effective treatment, but also prophylaxis of deficient, sensitive or hypoactive skin conditions or deficit, sensitive or hypoactive conditions of skin appendages of signs of premature aging the skin (eg wrinkles, age spots, telangiectasia) and / or the appendages of the skin, of environmental ones (smoking, smog, reactive oxygen species, free radicals) and in particular light-related negative changes in the skin and appendages, of light-related skin damage - t from pigmentation disorders, from sensitive, irritated and itchy skin, from dry skin conditions and barrier layer disorders, from hair loss and for improved hair growth - from inflammatory skin conditions as well as atopic eczema, seborrheic eczema, polymorphic light dermatosis, psoriasis, vitiligo
  • the active ingredient according to the invention or cosmetic or topical dermatological preparations with an effective content of the active ingredient according to the invention also surprisingly serves to calm sensitive or irritated skin to stimulate collagen, hyaluronic acid, elastin synthesis to stimulate ceramide synthesis of the skin - to stimulate the skin intracellular DNA synthesis, especially for deficient or hypoactive skin conditions.
  • to increase cell renewal and regeneration of the skin to increase the skin's own protection and repair mechanisms (e.g. for dysfunctional enzymes, DNA, lipids, proteins) - for pre-treatment and post-treatment with topical application of laser and abrasive treatments, e.g. B. serve the reduction of skin folds and scars to counteract the resulting skin irritation and to promote the regeneration processes in the injured skin.
  • the 2,3-dibenzylbutyrolactone derivatives and licochalcone A are preferably present in the active compound combinations according to the invention in ratios of 50: 1 to 1:50, preferably 10: 1 to 1:10, particularly preferably 2: 1 to 1: 2.
  • the 2,3-dibenzylbutyrolactone derivatives according to the invention and / or their glycosides are derived from the 2,3-dibenzylbutyrolactone also according to the invention, which is characterized by the following structure:
  • 2,3-dibenzylbutyrolactone, 2,3-dibenzylbutyrolactone derivatives and / or their glycosides in all their stereoisomeric forms which can be present both as a racemate and in enantiomerically pure form, and also in racemic mixtures with different enantiomeric proportions.
  • the formulation comprises 2,3-dibenzylbutyrolactone derivatives and / or their glycosides also the 2,3-dibenzylbutyrolactone.
  • the 2,3-dibenzylbutyrolactone derivatives according to the invention and / or their glycosides can advantageously be added to the preparation according to the invention in the form of plant extracts.
  • Aqueous-alcoholic extracts from plants have proven particularly useful.
  • extracts and distillates obtained with other forms of extraction and methods for example extracts obtained with carbon dioxide as extracting agent and steam distillates, can also be advantageously formulated into the preparations according to the invention.
  • Arctiin, arctigenin, Prestegan B, matairesinol, tracheloside and / or trachelogenin are used as 2,3-dibenzylbutyrolactone derivatives preferred according to the invention and / or their glycosides.
  • the derivatives with the following stereochemical structure are particularly preferred:
  • Arctiin and prestegan B are very particularly preferred according to the invention.
  • the 2,3-dibenzylbutyrolactone derivatives and / or their glycosides according to the invention can be easily incorporated into conventional cosmetic and / or dermatological preparations, such as sunscreen preparations, skin care preparations, anti-wrinkle preparations, but also other preparations, for example pharmaceutical preparations.
  • Preparations according to the invention advantageously contain 0.01-25% by weight of one or more 2,3-dibenzylbutyrolactone derivatives, preferably 0.1-20% by weight, in particular 1-10% by weight, in each case based on the total weight of the preparations.
  • the plant species Glycyrrhiza inflata like the licorice Glycyrrhiza glabra, which belongs to Europe, belongs to the genus Glycyrrhiza, which belongs to the Fabaceae (pea family) plant family.
  • the drug Radix Glycyrrhizae inflatae i.e. the root of the plant, is used, for example, in Far Eastern medicine. The use of the drug as an anti-inflammatory is also known.
  • a component of the aqueous extract from Radix Glycyrrhizae inflatae is the licochalcon
  • the preparations contain 0.0001 to 5% by weight, in particular 0.001 to 1% by weight, very particularly 0.005 to 0.15% by weight of licochalcone A, based on the total weight of the preparation. It is also advantageous according to the invention in particular if the preparations contain 0.001 to 10% by weight, in particular 0.05 to 5% by weight, very particularly 0.01 to 2% by weight, of one or more polyols, based on the total weight of the Preparation.
  • the preparations contain licocalchon as a constituent of plant extracts, in particular of Radix Glycyrrhizae inflatae.
  • licochalcone is in the form of an aqueous extract in which - licochalcone A water, if appropriate, one or more polyols are present.
  • the cosmetic or dermatological preparations 0.001 to 10% by weight, in particular 0.05 to 5% by weight, very particularly 0.01 to 2% by weight, of an aqueous extract from Radix Glycyrrhizae inflatae included, based on the total weight of the preparation.
  • the cosmetic or dermatological preparations contain 0.001 to 10% by weight, in particular 0.05 to 5% by weight, very particularly 0.01 to 2% by weight, of one or more polyols, based on the total weight of the preparation.
  • Licochalcone A in other vehicle systems in a concentration of 0.0001 to 5% by weight, in particular 0.001 to 1% by weight, very particularly 0.005-0.05% by weight. Accordingly, the use of active substance combinations according to the invention for the prophylaxis and treatment of inflammatory skin conditions - including atopic eczema - and / or for skin protection in the case of sensitive, determined dry skin is accordingly also according to the invention.
  • Cosmetic or dermatological preparations according to the invention preferably contain 0.001-1.0% by weight, particularly preferably 0.01-1% by weight, of active compound combinations according to the invention, based on the total composition of the preparations.
  • antioxidants are advantageously selected from the group consisting of amino acids (eg glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (eg urocanic acid) and their derivatives, peptides such as D, L-carnosine, D-carnosine, L- Carnosine and its derivatives (eg anserine), carotenoids, carotenes (eg ⁇ -carotene, ⁇ -carotene, lycopene) and their derivatives, chlorogenic acid and their derivatives, lipoic acid and their derivatives (eg dihydrolipoic acid), aurothioglucose, propylthiouracil and other thiols (eg thioredoxin, glutathione, cysteine, cystine, cystamine and their glycosyl, N-acetyl, methyl,
  • amino acids eg glycine, histidine, tyrosine, tryptophan
  • buthioninsulfoxinsulfoximine, homocystone, homocystone pent ⁇ -, hexa-, heptathioninsulfoximine) in very low tolerable doses e.g. pmol to ⁇ mol / kg
  • metal chelators e.g. ⁇ -hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), ⁇ -hydroxy acids (e.g. 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 (e.g.
  • ⁇ -linolenic acid linoleic acid, oleic acid
  • folic acid and its derivatives Ubiquinone and ubiquinol and their derivatives
  • vitamin C and derivatives e.g. ascorbyl palmitate, Mg ascorbyl phosphate, ascorbyl acetate
  • tocopherols and derivatives e.g.
  • vitamin E acetate
  • vitamin A and derivatives vitamin A palmitate
  • coniferyl benzoate Benzoin, rutinic acid and its derivatives, ⁇ -glycosyl rutin, ferulic acid, furfurylidene glucitol, carnosine, butylated hydroxytoluene, butylated hydroxyanisole, nordihydroguajak resin acid, nordihydroguajaretic acid, trihydroxybutyrophenone, uric acid and its derivative e, mannose and its derivatives, zinc and its derivatives (for example ZnO, ZnS0 4 ) selenium and its derivatives (for example selenium methionine), stilbenes and their derivatives (for example stilbene oxide, trans-stilbene oxide) and which are suitable according to the invention Derivatives (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids) of these active ingredients.
  • the amount of the antioxidants (one or more compounds) in the preparations is preferably 0.001 to 30% by weight, particularly preferably 0.05-20% by weight, in particular 1-10% by weight, based on the total weight the preparation.
  • the prophylaxis or the cosmetic or dermatological treatment with the active ingredient used according to the invention or with the cosmetic or topical dermatological Tological preparations with an effective content of active ingredient used according to the invention are carried out in the usual way, in such a way that the active ingredient used according to the invention or the cosmetic or topical dermatological preparations with an effective content of active ingredient used according to the invention is applied to the affected skin areas.
  • the active ingredient used according to the invention can advantageously be incorporated into customary cosmetic and dermatological preparations, which can be in various forms. So you can e.g. a solution, an emulsion of the type water-in-oil (W / O) or of the type oil-in-water (O / W), or a multiple emulsions, for example of the type water-in-oil-in-water (W / O / W) or oil-in-water-in-oil (O / W / O), a hydrodispersion or lipodispersion, a gel, a solid stick or an aerosol.
  • Emulsions according to the invention in the sense of the present invention are advantageous and contain e.g. Fats, oils, waxes and / or other fat bodies, as well as water and one or more emulsifiers, as are usually used for such a type of formulation.
  • the active ingredient used according to the invention into aqueous systems or surfactant preparations for cleaning the skin and hair.
  • the cosmetic preparations according to the invention can therefore contain cosmetic auxiliaries as are usually used in such preparations, e.g. Preservatives, bactericides, deodorising substances, antiperspirants, insect repellents, vitamins, anti-foaming agents, dyes, pigments with a coloring effect, thickeners, softening substances, moisturizing and / or moisturizing substances, fats, oils, waxes or other common components a cosmetic formulation such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
  • cosmetic auxiliaries as are usually used in such preparations, e.g. Preservatives, bactericides, deodorising substances, antiperspirants, insect repellents, vitamins, anti-foaming agents, dyes, pigments with a coloring effect, thickeners, softening substances, moisturizing and / or moisturizing substances, fats, oils, waxes or other common components a cosmetic formulation such as alcohols, polyols
  • Medical topical compositions within the meaning of the present invention generally contain one or more medicaments in an effective concentration.
  • Preparations according to the invention can also advantageously contain substances which absorb UV radiation in the UVB range, the total amount of filter substances e.g. 0.1% by weight to 30% by weight, preferably 0.5 to 10% by weight. is in particular 1.0 to 6.0% by weight, based on the total weight of the preparations, in order to provide cosmetic preparations which protect the hair or the skin from the entire range of ultraviolet radiation. They can also serve as a sunscreen for the hair.
  • the total amount of filter substances e.g. 0.1% by weight to 30% by weight, preferably 0.5 to 10% by weight. is in particular 1.0 to 6.0% by weight, based on the total weight of the preparations, in order to provide cosmetic preparations which protect the hair or the skin from the entire range of ultraviolet radiation. They can also serve as a sunscreen for the hair.
  • Oil-soluble UVB filters which are advantageous according to the invention are, for example: 3-benzylidene camphor derivatives, preferably 3- (4-methylbenzylidene) camphor, 3-benzylidene camphor; 4-aminobenzoic acid derivatives, preferably 4- (dimethylamino) benzoic acid (2-ethyl-hexyl) ester, 4- (dimethylamino) benzoic acid amyl ester; Esters of cinnamic acid, preferably 4-methoxycinnamic acid (2-ethylhexyl) ester, 4-methoxycinnamic acid isopentyl ester; Esters of salicylic acid, preferably salicylic acid (2-ethylhexyl) ester, salicylic acid (4-isopropylbenzyl) ester, salicylic acid homomethyl ester, derivatives of benzophenone
  • Examples of advantageous water-soluble UVB filters are: Salts of 2-phenylbenzimidazole-5-sulfonic acid such as its sodium, potassium or triethanolammonium salt, and also the sulfonic acid itself; Sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and its salts; Sulfonic acid derivatives of 3-benzylidene camphor, such as 4- (2-oxo-3-bomylidene-methyl) benzenesulfonic acid, 2-methyl-5- (2-oxo-3-bomylidene-methyl) sulfonic acid and their salts and 1,4- di (2-oxo-10-sulfo-3-bornylidenemethyl) -benzene and its salts (the corresponding 10-sulfato compounds, for example the corresponding sodium, potassium or triethanolammonium salt), also as benzene-1 , 4-di (2-oxo-3-bornyliden
  • UVB filters which can be used in combination with the active compound combinations according to the invention, is of course not intended to be limiting.
  • UVA filters that are usually contained in cosmetic preparations.
  • These substances are preferably derivatives of dibenzoylmethane, in particular 1- (4'-tert-butylphenyl) -3- (4'-methoxyphenyl) propane-1, 3-dione and 1-phenyl-3 - (4'-Isopropylphenyl) propane-1,3-dione.
  • the quantities used for the UVB combination can be used.
  • Cosmetic and dermatological preparations according to the invention advantageously also contain inorganic pigments based on metal oxides and / or other metal compounds which are sparingly soluble or insoluble in water, in particular the oxides of titanium (Ti0 2 ), zinc (ZnO), iron (eg Fe 2 0 3 ), zirconium (Zr0 2 ), silicon (Si0 2 ), manganese (eg MnO), aluminum (Al 2 0 3 ), cerium (eg Ce 2 0 3 ), mixed oxides of the corresponding metals and mixtures of such oxides. It is particularly preferably pigments based on TiO 2 .
  • the inorganic pigments are in hydrophobic form, ie that they have been treated to be water-repellent on the surface.
  • This surface treatment can consist in that the pigments are provided with a thin hydrophobic layer by methods known per se. Such a method consists, for example, in that the hydrophobic surface layer according to a direction
  • n and m are stoichiometric parameters to be used at will, R and R 'are the desired organic radicals.
  • hydrophobized pigments shown in analogy to DE-OS 33 14 742 are advantageous.
  • Advantageous Ti0 2 pigments are available, for example, under the trade names MT 100 T from TAYCA, M 160 from Kemira and T 805 from Degussa.
  • Preparations according to the invention can also contain anionic, nonionic and / or amphoteric surfactants, especially if crystalline or microcrystalline solids, for example inorganic micropigments, are to be incorporated into the preparations according to the invention.
  • Surfactants are amphiphilic substances that can dissolve organic, non-polar substances in water.
  • hydrophilic parts of a surfactant molecule are mostly polar functional groups, for example -COO " , -OS0 3 2" , -S0 3 " , while the hydrophobic parts generally represent non-polar hydrocarbon residues.
  • Surfactants are generally of type and charge of the hydrophilic part of the molecule. Four groups can be distinguished here:
  • Anionic surfactants generally have carboxylate, sulfate or sulfonate groups as functional groups. In aqueous solution they form negatively charged organic ions in an acidic or neutral environment. Cationic surfactants are almost exclusively due to that Labeled presence of a quaternary ammonium group. In aqueous solution, they form positively charged organic ions in an acid or neutral environment. Amphoteric surfactants contain both anionic and cationic groups and accordingly behave in aqueous solution like anionic or cationic surfactants depending on the pH. They have a positive charge in a strongly acidic environment and a negative charge in an alkaline environment. In the neutral pH range, however, they are zwitterionic, as the following example should illustrate:
  • Non-ionic surfactants do not form ions in an aqueous medium.
  • acylglutamates for example sodium acylglutamate, di-TEA-palmitoylaspartate and sodium caprylic / capric glutamate,
  • acyl peptides for example palmitoyl-hydrolyzed milk protein, sodium cocoyl-hydrolyzed soy protein and sodium / potassium cocoyl-hydrolyzed collagen,
  • sarcosinates for example myristoyl sarcosin, TEA-lauroyl sarcosinate, sodium lauroyl sarcosinate and sodium cocoyl sarcosinate
  • taurates for example sodium lauroyl taurate and sodium methyl cocoyl taurate
  • carboxylic acids for example lauric acid, aluminum stearate, magnesium alkenolate and zinc undecylenate,
  • ester carboxylic acids for example calcium stearoyl lactylate, laureth-6 citrate and sodium PEG-4 lauramide carboxylate,
  • ether carboxylic acids for example sodium laureth-13 carboxylate and sodium PEG-6 cocamide carboxylate, Phosphoric acid esters and salts, such as DEA-oleth-10-phosphate and dilaureth-4-phosphate,
  • acyl isethionates e.g. Sodium / ammonium cocoyl isethionate
  • alkyl sulfonates for example sodium cocosmonoglyceride sulfate, sodium C 12-1 olefin sulfonate, sodium lauryl sulfoacetate and magnesium PEG-3 cocamide sulfate, 4.
  • sulfosuccinates for example dioctyl sodium sulfosuccinate, disodium laureth sulfosuccinate, disodium lauryl sulfyl succinate sulfosuccinate aminosulfinate sulfosuccinate aminosulfinate sulfosuccinate disodium aminosulfinate sulfate succinate disodium aminosulfinate sulfate succinate disodium aminosulfinate sulfate and
  • alkyl ether sulfate for example sodium, ammonium, magnesium, MIPA, TIPA laureth sulfate, sodium and sodium C12 - 1 3 pareth
  • alkyl sulfates for example sodium, ammonium and TEA lauryl sulfate.
  • Cationic Surfactants Cationic surfactants to be used advantageously are
  • Quaternary surfactants contain at least one N atom which is covalently bonded to 4 alkyl or aryl groups. Regardless of the pH value, this leads to a positive charge.
  • Alkyl betaine, alkyl amidopropyl betaine and alkyl amidopropyl hydroxysulfain are advantageous.
  • the cationic surfactants used in the invention can be also preferably selected from the group of quaternary ammonium compounds, in particular benzene zyltrialkylammoniumchloride or bromides, such as Benzyldimethylstea- rylammoniumchlorid, also alkyltrialkylammonium, such as for example Ce tyltrimethylammoniumchlorid or bromide, alkyldimethylhydroxyethylammonium chlorides or bromides, dialkyldimethylammonium chlorides or -bromides, alkylamidethyltrimethylam- monium ether sulfates, alkylpyridinium salts, for example lauryl or cetylpyrimidinium chloride, imidazoline derivatives and compounds with a cationic character such as amine oxides, for example alkyldimethylamine oxides or alkylaminoethyldimethylamine oxides. Cetylt methylam
  • acyl / dialkyl ethylenediamine for example sodium acyl amphoacetate, disodium acyl amphodipropionate, disodium alkyl amphodiacetate, sodium acylamphohydroxypropyl sulfonate, disodium acylamphodiacetate and sodium acylamphopropionate,
  • N-alkylamino acids for example aminopropylalkylglutamide, alkylaminopropionic acid, sodium alkylimidodipropionate and lauroamphocarboxyglycinate.
  • Non-ionic surfactants are non-ionic surfactants that can be used advantageously
  • alkanolamides such as cocamides MEA / DEA / MIPA
  • amine oxides such as cocoamidopropylamine oxide
  • esters which are formed by esterification of carboxylic acids with ethylene oxide, glycerol, sorbitan or other alcohols,
  • ethers for example ethoxylated / propoxylated alcohols, ethoxylated / propoxylated esters, ethoxylated / propoxylated glycerol esters, ethoxylated / propoxylated cholesterols, ethoxylated / propoxylated triglyceride esters, ethoxylated propoxylated lanolin, ethoxylated / propoxylated polysiloxanes, propoxylated POE ethers and alkylpolyglycosides such as lauryl polyglycosides cocoglycoside.
  • the surface-active substance can be present in the preparations according to the invention in a concentration between 1 and 95% by weight, based on the total weight of the preparations.
  • the lipid phase of the cosmetic or dermatological emulsions according to the invention can advantageously be selected from the following group of substances: mineral oils, mineral wax oils, such as triglycerides of capric or caprylic acid, and also natural oils such as e.g. Castor oil; Fats, waxes and other natural and synthetic fat bodies, preferably esters of fatty acids with alcohols of low C number, e.g.
  • the oil phase of the emulsions of the present invention is advantageously selected from the group of the esters from saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 3 to 30 carbon atoms and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 to 30 C atoms, from the group of esters of aromatic carboxylic acids and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 to 30 C atoms.
  • ester oils can then advantageously be selected from the group of isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyistearate, isononylisononanoate, 2-ethylhexyl-2-ethylhexyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethylhexyl-2-ethyl-2-ethyl-2-ethyl-2-ethylhexyl-2-ethyl-2-ethyl-2-
  • the oil phase can advantageously be selected from the group of branched and unbranched hydrocarbons and waxes, the silicone oils, the dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols, and also the fatty acid triglycerides, especially the triglycerol esters of saturated and / or unsaturated, comparable branched and / or unbranched alkane carboxylic acids with a chain length of 8 to 24, in particular 12 - 18 carbon atoms.
  • the fatty acid triglycerides can, for example, advantageously be selected from the group of synthetic, semisynthetic and natural oils, for example olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm kernel oil and the like.
  • any mixtures of such oil and wax components can also be used advantageously for the purposes of the present invention. It may also be advantageous, where appropriate, to use waxes, for example cetyl palmitate, as the sole lipid component of the oil phase.
  • the oil phase is advantageously selected from the group 2-ethylhexyl isostearate, octyldodecanol, isotridecylisononanoate, isoeicosane, 2-ethylhexyl cocoate, C ⁇ 2- ⁇ 5 alkyl benzoate, caprylic capric acid re-trig lyceride, dicaprylyl ether.
  • C 12 are particularly advantageous. 5 alkyl benzoate and 2-ethylhexyl isostearate, mixtures of C 2-15 alkyl benzoate and isotridecyl isononanoate and mixtures of C 1 . 15 alkyl benzoate, 2-ethylhexyl isostearate and isotridecyl isononanoate.
  • hydrocarbons paraffin oil, squalane and squalene can be used advantageously for the purposes of the present invention.
  • the oil phase can advantageously also have a content of cyclic or linear silicone oils or consist entirely of such oils, although it is preferred to use an additional content of other oil phase components in addition to the silicone oil or the silicone oils.
  • Such silicones or silicone oils can be present as monomers, which are generally characterized by structural elements, as follows:
  • Linear silicones with a plurality of siloxyl units which can advantageously be used according to the invention are generally characterized by structural elements as follows: wherein the silicon atoms can be substituted with the same or different alkyl radicals and / or aryl radicals, which are generally represented by the radicals R 1 - R 4 (to say that the number of different radicals is not necessarily limited to up to 4), m can assume values from 2 - 200,000.
  • n assume values from 3/2 to 20.
  • broken values for n take into account that there may be odd numbers of siloxyl groups in the cycle.
  • Cyclomethicone e.g. decamethylcyclopentasiloxane
  • silicone oils can also be used advantageously for the purposes of the present invention, for example undecamethylcyclotrisiloxane, polydimethylsiloxane, poly (methylphenylsiloxane), cetyldimethicone, behenoxydimethicone.
  • silicone oils of a constitution similar to the above-mentioned compounds, the organic side chains of which are derivatized, for example polyethoxylated and / or polypropoxylated.
  • silicone oils include, for example, polysiloxane-polyalkyl-polyether copolymers such as the cetyl-dimethicone copolyol, the (cetyl-dimethicone copolyol (and) polyglyceryl-4-isostearate (and) hexyl laurate)
  • the aqueous phase of the preparations according to the invention advantageously advantageously contains alcohols, diols or polyols of low C number, and their ethers, preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether , Diethy- glycol monomethyl or monoethyl ether and analog products, furthermore alcohols of low C number, for example Ethanol, isopropanol, 1, 2-propanediol, glycerol and in particular one or more thickeners, which one or more can advantageously be selected from the group consisting of silicon dioxide and aluminum silicates.
  • alcohols, diols or polyols of low C number, and their ethers preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol,
  • Preparations according to the invention which are present as emulsions particularly advantageously contain one or more hydrocolloids.
  • hydrocolloids can advantageously be selected from the group consisting of gums, polysaccharides, cellulose derivatives, layered silicates, polyacrylates and / or other polymers.
  • Preparations according to the invention which are present as hydrogels contain one or more hydrocolloids. These hydrocolloids can advantageously be selected from the aforementioned group.
  • Gums include plant or tree sap that harden in the air and form resins or extracts from aquatic plants. Gum arabic, locust bean gum, tragacanth, karaya, guar gum, pectin, gellan gum, carrageenan, agar, algine, chondrus, xanthan gum can advantageously be selected from this group for the purposes of the present invention.
  • derivatized gums such as hydroxypropyl guar (Jaguar® HP 8) is also advantageous.
  • polysaccharides and derivatives are e.g. Hyaluronic acid, chitin and chitosan, chondroitin sulfates, starch and starch derivatives.
  • cellulose derivatives are e.g. Methyl cellulose, carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose.
  • Layered silicates contain naturally occurring and synthetic clays such as Montmorillonite, bentonite, hectorite, laponite, magnesium aluminum silicates such as Vegegum®. These can be used as such or in a modified form such as e.g. Stearylalkonium hectorite.
  • silica gels can also advantageously be used.
  • the polyacrylates include e.g. Carbopol types from Goodrich (Carbopol 980, 981, 1382, 5984, 2984, EDT 2001 or Pemulen TR2).
  • polymers e.g. Polyacrylamides (Seppigel 305), polyvinyl alcohol, PVP, PVP / VA copolymers, polyglycols.
  • Preparations according to the invention in the form of emulsions contain one or more emulsifiers.
  • emulsifiers can advantageously be selected from the group of nonionic, anionic, cationic or amphoteric emulsifiers.
  • nonionic emulsifiers are a) partial fatty acid esters and fatty acid esters of polyhydric alcohols and their ethoxylated derivatives (e.g. glyceryl monostearates, sorbitan stearates, glyceryl stearyl citrates, sucrose stearates) b) ethoxylated fatty alcohols and fatty acids c) ethoxylated fatty amides, fatty acid glycol amides, fatty acid glycol amides, fatty acid glycol amides, fatty acid glycol amides, e.g. Triton X)
  • the anionic emulsifiers include a) soaps (e.g. sodium stearate) b) fatty alcohol sulfates c) mono-, di- and trialkylphosphonic acid esters and their ethoxylates
  • the cationic emulsifiers include a) quaternary ammonium compounds with a long-chain aliphatic radical, e.g. Distearyldimonium Chloride
  • amphoteric emulsifiers include: a) alkylamininoalkane carboxylic acids b) betaines, sulfobetaines c) imidazoline derivatives
  • emulsifiers which include beeswax, wool wax, lecithin and sterols.
  • O / V emulsifiers can, for example, advantageously be selected from the group of the polyethoxylated or polypropoxylated or polyethoxylated and polypropoxylated products, for example: the fatty alcohol ethoxylates of the ethoxylated wool wax alcohols, the polyethylene glycol ethers of the general formula R-0 - (- CH 2 -CH 2 -0-) n -R ', the fatty acid ethoxylates of the general formula R-COO - (- CH 2 -CH 2 -0-) n -H, the etherified fatty acid ethoxylates of the general formula R-C00 - (- CH 2 -CH 2 -0-) n -R ', the esterified fatty acid ethoxylates of the general formula R-C00 - (- CH 2 -CH 2 -0-) n -C (0) -R', - the polyethylene glycol glycerol
  • the polyethoxylated or polypropoxylated or polyethoxylated and polypropoxylated O / W emulsifiers used are particularly advantageously selected from the group of substances with HLB values of 11-18, very particularly advantageously with HLB values of 14.5 - 15.5, provided the O / W emulsifiers have saturated residues R and R '. If the O / W emulsifiers have unsaturated radicals R and / or R ', or if isoalkyl derivatives are present, the preferred HLB value of such emulsifiers can also be lower or higher.
  • fatty alcohol ethoxylates from the group of the ethoxylated stearyl alcohols, cetyl alcohols, cetylstearyl alcohols (cetearyl alcohols).
  • cetyl alcohols cetylstearyl alcohols
  • cetearyl alcohols cetearyl alcohols
  • Polyethylene glycol (12) lauryl ether (Laureth-12), polyethylene glycol (12) isolauryl ether (Isolureth-12).
  • the sodium laureth-11 carboxylate can advantageously be used as the ethoxylated alkyl ether carboxylic acid or its salt.
  • Sodium laureth 1-4 sulfate can advantageously be used as alkyl ether sulfate.
  • Polyethylene glycol (30) cholesteryl ether can advantageously be used as the ethoxylated cholesterol derivative.
  • Polyethylene glycol (25) soyasterol has also proven itself.
  • polyethylene glycol glycerol fatty acid esters from the group polyethylene glycol (20) glyceryl laurate, polyethylene glycol (21) glyceryl laurate, polyethylene glycol (22) glyceryl laurate, polyethylene glycol (23) glyceryl laurate, polyethylene glycol (6) glyceryl caprolate caprinate, polyethylene glycol
  • polyethylene glycol (20) glyceryl isostearate polyethylene glycol (18) glyceryl oleate / cocoat.
  • sorbitan esters from the group consisting of polyethylene glycol (20) sorbitan monolaurate, polyethylene glycol (20) sorbitan monostearate, polyethylene glycol (20) sorbitan monoisostearate, polyethylene glycol (20) sorbitan monopalmitate, polyethylene glycol (20) sorbitan monooleate.
  • W / O emulsifiers that can be used are: fatty alcohols with 8 to 30 carbon atoms, monoglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 8 to 24, in particular 12 to 18 carbon atoms, diglycerol esters saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 8 to 24, in particular 12 to 18 carbon atoms, monoglycerol ethers saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 8 to 24, in particular 12 to 18 C atoms, diglycerine ethers of saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 8 to 24, in particular 12-18 C atoms, propylene glycol esters of saturated and / or unsaturated, branched and / or unbranche
  • W / O emulsifiers are glyceryl stearate Glycerylmonoiso-, glyceryl monomyristate, glyceryl, diglyceryl monostearate, Diglycerylmono- isostearate, propylene glycol caprylate, propylene glycol monoisostearate, propylene glycol, Propylengiycolmonolaurat, sorbitan, sorbitan, sorbitan monocaprylate, Sorbitanmonoisooleat, sucrose, cetyl alcohol, stearyl alcohol, Arachidyl alcohol, behenyl alcohol, isobehenyl alcohol, selachyl alcohol, chimyl alcohol, polyethylene glycol (2) stearyl ether (Steareth-2), glyceryl monolaurate, glyceryl monocaprinate, glyceryl monocaprylate.

Abstract

The invention relates to active agent combinations of (a) one or more 2,3-dibenzylbutyrolactone derivatives and (b) licochalcone-A, or an aqueous extract of Radix Glycyrrhizae inflatae, containing licochalcone-A.

Description

KOMBIHATION VON 2, 3-DIBEΪIZY BUTYROLACTON UND LICOCHALCON A COMBINATION OF 2, 3-DIBEΪIZY BUTYROLACTONE AND LICOCHALCON A
Beschreibungdescription
Wirkstoffkombinationen aus 2,3-Dibenzylbutyrolactoπen und ücochalcon A oder einem wässrigen Extrakt aus Radix Glycyrrhizae inflatae, enthaltend Licochaicon AActive ingredient combinations of 2,3-dibenzylbutyrolactoπen and ücochalcon A or an aqueous extract from Radix Glycyrrhizae inflatae, containing Licochaicon A
Die vorliegende Erfindung betrifft kosmetische bzw. dermatologische Zubereitungen, enthaltend Wirkstoffe zur Pflege und zum Schütze der Haut, insbesondere der empfindlichen Haut wie auch ganz besonders im Vordergrunde stehend der durch intrinsische und/oder extrinsi- sche Faktoren gealterten oder alternden Haut sowie die Verwendung solcher Wirkstoffe und Kombinationen solcher Wirkstoffe auf dem Gebiete der kosmetischen und dermatologischeπ Hautpflege.The present invention relates to cosmetic or dermatological preparations containing active ingredients for the care and protection of the skin, in particular sensitive skin, and very particularly in the foreground of skin aged or aging due to intrinsic and / or extrinsic factors, and the use of such active ingredients and combinations of such active ingredients in the field of cosmetic and dermatological skin care.
Unter kosmetischer Hautpflege ist in erster Linie zu verstehen, dass die natürliche Funktion der Haut als Barriere gegen Umwelteinflüsse (z.B. Schmutz, Chemikalien, Mikroorganismen) und gegen den Verlust von körpereigenen Stoffen (z.B. Wasser, natürliche Fette, Elek- trolyte) gestärkt oder wiederhergestellt wird.Cosmetic skin care is primarily to be understood as meaning that the natural function of the skin as a barrier against environmental influences (eg dirt, chemicals, microorganisms) and against the loss of the body's own substances (eg water, natural fats, electrolytes) is strengthened or restored ,
Wird diese Funktion gestört, kann es zu verstärkter Resorption toxischer oder allergener Stoffe oder zum Befall von Mikroorganismen und als Folge zu toxischen oder allergischen Hautreaktionen kommen.If this function is disturbed, there may be an increased absorption of toxic or allergenic substances or an infestation of microorganisms and, as a result, toxic or allergic skin reactions.
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. Bei pathologisch trockener und empfindlicher Haut liegt ein Barriereschaden a priori vor. Epidermale Interzellularlipide werden 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 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. In the case of pathologically dry and sensitive skin, there is a priori barrier damage. Epidermal intercellular lipids are formed incorrectly or in insufficient quantity or composition. The consequence is an 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 loss) 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 loss). 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 Haut- schicht von größter Bedeutung. Man kann ihn in einem begrenzten Umfang durch Einbringen von Feuchtigkeitsregulatoren günstig beeinflussen.The water content in the uppermost skin layer is of the greatest importance for the beauty and care of the skin. 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 lang anhaltend erhöhen, was regenerative Prozes- se, 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 Funktionsweise 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 skin's barrier function. In this case, a new, often very unfavorable 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.
Schon bei einem einfachen Wasserbade ohne Zusatz von Tensiden kommt es zunächst zu einer Quellung der Hornschicht d er H aut, w obei d er G rad d ieser Q uellung b eispielsweise von der Dauer des Bades und dessen Temperatur abhängt. Zugleich werden wasserlösliche Stoffe, z.B. wasserlösliche Schmutzbestandteile, aber auch hauteigene Stoffe, die für das Wasserbindungsvermögen der Hornschicht verantwortlich sind, ab- bzw. ausgewaschen. Durch hauteigene oberflächenaktive Stoffe werden zudem auch Hautfette in gewissem Ausmaße gelöst und ausgewaschen. Dies bedingt nach anfänglicher Quellung eine nachfolgende deutliche Austrocknung d er H aut, d ie d urch waschaktive Zusätze noch verstärkt werden kann. 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 Falle nichtpathologischer Abweichungen vom Normalstatus, z.B. durch u mweltbedingte Abnutzungsschäden bzw. I rritationen, L ichtschäden, Altershaut usw., ist der Schutzmechanismus der Hautoberfläche gestört. Unter Umständen ist er dann aus eigener Kraft nicht mehr imstande, seine Aufgabe zu erfüllen und muss durch externe Maßnahmen regeneriert werden.Even a simple water bath without the addition of surfactants initially causes swelling of the horny layer of the skin, while the degree of this swelling depends, for example, on the duration of the bath and its temperature. At the same time, water-soluble substances, such as water-soluble dirt components, but also skin's own substances, which are responsible for the water-binding capacity of the horny layer, are washed off or washed out. To a certain extent, skin fats are also dissolved and washed out by the skin's own surface-active substances. After initial swelling, this requires a subsequent significant drying out of the skin, which can be reinforced by washing-active additives. In healthy skin, these processes are generally irrelevant, since the protective mechanisms of the skin can easily compensate for such slight disorders of the upper layers of the skin. But even in the case of non-pathological deviations from normal status, for example due to environmental wear and tear or irritation, light damage, aging skin, etc., the protective mechanism of the skin surface is disrupted. Under certain circumstances, he may no longer be able to fulfill his task on his own and must be regenerated by external measures.
Darüber hinaus ist bekannt, dass Lipidzusammensetzung und -menge der Hornschicht der pathologisch veränderten, trockenen und der trockenen, jedoch nicht erkrankten Haut jüngerer und älterer Menschen vom Normalzustand abweicht, der in der gesunden, normal hydrierten Haut einer gleich alten Altersgruppe vorgefunden wird. Dabei stellen die Veränderungen im Lipidmuster der sehr trockenen, nicht-ekzematösen Haut von P atienten m it atopi- schem Ekzem einen Extremfall für die Abweichungen dar, die in der trockenen Haut hautgesunder Menschen vorgefunden werden.In addition, it is known that the lipid composition and amount of the horny layer of the pathologically changed, dry and dry, but not diseased skin of younger and older people deviate from the normal condition found in healthy, normally hydrated skin of an age group of the same age. The changes in the lipid pattern of the very dry, non-eczematous skin of patients with atopic eczema represent an extreme case for the deviations that are found in the dry skin of healthy people.
Diese Abweichungen betreffen dabei ganz besonders die Ceramide, die in ihrer Menge stark reduziert und zusätzlich anders zusammengesetzt sind. Auffallend ist dabei in beson- derer Weise das Defizit an den Ceramiden 1 und 3, wobei insbesondere für das Ceramid 1 bekannt ist, dass es in besonderer Weise die Ordnung der Lipide in den Interzellularmembransystemen steigert.These deviations particularly affect the ceramides, which are greatly reduced in their quantity and are also composed differently. The deficit in ceramides 1 and 3 is particularly striking, it being known in particular for ceramide 1 that it increases the order of the lipids in the intercellular membrane systems in a special way.
Nachteilige Veränderungen in den Lipidmembranen der vorab geschilderten Art beruhen möglicherweise auf fehlgesteuerter Lipidbiosynthese und erhöhen ebenfalls im Endeffekt den transepidermalen Wasserverlust. Eine langanhaltende Barriereschwäche wiederum macht die an sich gesunde Haut empfindlicher und kann im Einzellfalle zum Entstehen ek- zematöser Vorgänge in der kranken Haut beitragen.Adverse changes in the lipid membranes of the type described above may be due to miscontrolled lipid biosynthesis and also ultimately increase transepidermal water loss. Long-lasting barrier weakness, in turn, makes healthy skin more sensitive and in individual cases can contribute to the development of eczematous processes in the diseased skin.
Die Wirkung von Salben und Cremes auf Barrierefunktion und Hydratation der Hornschicht besteht in der Regel nicht in einer Wiederherstellung bzw. Stärkung der physikalisch-chemischen Eigenschaften der Lamellen aus Interzellularlipiden. Ein wesentlicher Teileffekt beruht auf der bloßen Abdeckung der behandelten Hautbezirke und dem daraus resultierenden Wasserstau in der darunterliegenden Hornschicht. Coapplizierte hygroskopische Substanzen binden das Wasser, so dass es zu einer messbaren Zunahme des Wassergehaltes in der Hornschicht kommt. Diese rein physikalische Barriere kann jedoch relativ leicht wieder entfernt werden. Nach dem Absetzen des Produktes kehrt die Haut dann sehr schnell wieder den Zustand vor Behandlungsbeginn zurück. Darüber hinaus kann die Hautpflegewirkung bei regelmäßiger Behandlung nachlassen, so dass schließlich sogar während der Behandlung der Status quo wieder erreicht wird. Bei bestimmten Produkten verschlechtert sich der Zustand der Haut nach Absetzen unter Umständen 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 hydration of the horny layer usually does not consist in restoring or strengthening the physicochemical properties of the lamellae made of intercellular lipids. A major partial effect is due to the mere covering of the treated skin areas and the resulting water retention in the underlying horny layer. Co-applied hygroscopic Substances bind the water so that there is a measurable increase in the water content in the horny layer. However, this purely physical barrier can be removed relatively easily. After stopping the product, the skin quickly returns to the state before the start of treatment. In addition, the skin care effect can diminish with regular treatment, so that the status quo is finally reached again even during treatment. With certain products, the condition of the skin may temporarily worsen after discontinuation. As a rule, a sustainable product effect is not achieved or only to a limited extent.
Um die defizitäre Haut bei ihrer natürlichen Regeneration zu unterstützen und ihre physiologische Funktion zu stärken, werden topischen Präparaten in neuerer Zeit zunehmend Interzellularlipidmischungen zugesetzt, die von der Haut zum Wiederaufbau der natürlichen Barriere verwendet werden sollen. Allerdings handelt es sich bei diesen Lipiden, insbesonde- re aber den Ceramiden, um sehr teure Rohstoffe. Zudem ist ihre Wirkung meist sehr viel geringer als erhofft.In order to support the deficient skin in its natural regeneration and to strengthen its physiological function, intercellular lipid mixtures, which are to be used by the skin to rebuild the natural barrier, are increasingly being added to topical preparations. However, these lipids, especially the ceramides, are very expensive raw materials. In addition, their effect is usually much less than expected.
Ziel der vorliegenden Erfindung war es somit, Wege zu finden, die Nachteile des Standes der Technik zu vermeiden. Insbesondere sollte die Wirkung der Hautpflegeprodukte physio- logisch, schnell und nachhaltig sein.The aim of the present invention was therefore to find ways to avoid the disadvantages of the prior art. In particular, the effects of skin care products should be physiological, quick and sustainable.
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, Chemikalien, 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, chemicals, 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 easily for example with cleaning agents - are removed again, whereby 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 state before the start of treatment. With certain products, the condition of the skin may even temporarily deteriorate. As a rule, a sustainable product effect is not achieved or only to a limited extent.
Die Wirkung einiger pharmazeutischer Zubereitungen auf die Barrierefunktion der Haut be- steht 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 Reinigungsprödukten besteht im wesentlichen in einer effizien- ten Rückfettung mit Sebumlipid-ähnlichen Substanzen. Durch die gleichzeitige Verminderung des Tensidgehalts solcher Zubereitungen lässt sich der Schaden an der Homschicht- barriere weiter begrenzen.The effect of nourishing cleansing products is essentially an efficient regreasing with sebum lipid-like substances. By simultaneously reducing the surfactant content of such preparations, the damage to the homolayer 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 Interzelluiarlipiden stärken bzw. sogar wiederherstellen.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 of the lamellae from intercellular lipids.
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 ferner 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. Darüber hinaus betrifft die Erfindung Zubereitungen mit extrem niedrigem sogenanntem "Stinging Potential". Bei Menschen mit sensibler, empfindlicher oder verletzlicher Haut kann ein mit "Stinging" (<engl.> "to sting" = verletzen, brennen, schmerzen) bezeichnetes neurosensorisches Phänomen beobachtet werden. Diese "sensible Haut" unterscheidet sich grundsätzlich von "trockener Haut" mit verdickten und verhärteten Hornschichten.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 skin's barrier properties, especially when the natural regeneration of the skin is not sufficient. 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. In addition, the invention relates to preparations with extremely low so-called "stinging potential". In people with sensitive, sensitive or vulnerable skin, a neurosensory phenomenon called "stinging"(<engl.>"Tosting" = injure, burn, pain) can be observed. This "sensitive skin" differs fundamentally from "dry skin" with thickened and hardened horny layers.
Typische Reaktionen des "Stinging" bei sensibler Haut sind Rötung, Spannen und Brennen der Haut sowie Juckreiz.Typical reactions of "stinging" to sensitive skin are reddening, tension and burning of the skin as well as itching.
Als neurosensorisches Phänomen ist der Juckreiz bei atopischer Haut anzusehen, sowie Juckreiz bei Hauterkrankungen.Itching in atopic skin and itching in skin diseases are to be regarded as a neurosensory phenomenon.
"Stinging'-Phänomene können als kosmetisch zu behandelnde Störungen angesehen werden. Starker Juckreiz dagegen, insbesondere bei Atopie auftretendes starkes Hautjucken, kann auch als schwerwiegendere dermatologische Störung bezeichnet werden."Stinging 'phenomena can be regarded as disorders to be treated cosmetically. In contrast, severe itching, particularly severe itching in the case of atopy, can also be described as a more serious dermatological disorder.
Typische, mit den Begriffen "Stinging" oder "empfindlicher Haut" in Verbindung gebrachte, störende neurosensorische Phänomene sind Hautrötung, Kribbeln, Prickeln, Spannen und Brennen der Haut und Juckreiz. Sie können durch stimulierende Umgebungsbedingungen z.B. Massage, Tensideinwirkung, Wettereinfiuss wie Sonne, Kälte, Trockenheit, aber auch feuchte Wärme, Wärmestrahlung und UV-Strahlung, z.B. der Sonne, hervorgerufen werden.Typical disturbing neurosensory phenomena associated with the terms "stinging" or "sensitive skin" are reddening of the skin, tingling, tingling, tension and burning of the skin and itching. You can e.g. by stimulating environmental conditions Massage, exposure to surfactants, weather influences such as sun, cold, dryness, but also moist heat, heat radiation and UV radiation, e.g. the sun.
In "Journal of the Society of Cosmetic Chemists" 28, S.197 - 209 (Mai 1977) beschreiben P.J.Frosch und A.M.Kligman eine Methode zur Abschätzung des "Stinging-Potentials" to- pisch verabreichter Substanzen. Als positive Substanzen werden hier z.B. Milchsäure und Brenztraubensäure eingesetzt. Bei Messung nach dieser Methode wurden aber auch Aminosäuren, insbesondere Glycin, als neurosensorisch aktiv ermittelt (solche Substanzen werden "Stinger" genannt). Nach bisherigen Erkenntnissen tritt eine derartige Empfindlichkeit gegenüber ganz bestimmten Substanzen individuell unterschiedlich auf. Dies bedeutet, eine Person, die bei Kontakt mit einer Substanz "Stingingeffekte" erlebt, wird sie mit hoher Wahrscheinlichkeit bei jedem weiteren Kontakt wiederholt erleben. Der Kontakt mit anderen "Stingern" kann aber ebensogut ohne jede Reaktion verlaufen. Das Problem „ sensible Haut" betrifft eine wachsende Anzahl Erwachsenen und Kindern. Mit Sensibler Haut bezeichnet man eine Kombination verschiedener Symptome, wie hyperreaktive und intolerante Haut. Aber auch atopische Haut kann darunter s ubsummiert werden. Diese H autzustände werden von d en Betroffenen oftmals, n icht g anz k orrekt, a ls „allergische" Haut bezeichnet. Obwohl eine allergische Erkrankung zu Symptomen der sensiblen Haut führen kann, ist die Erscheinung „sensible Haut" nicht auf Allergiker beschränktIn "Journal of the Society of Cosmetic Chemists" 28, pp. 197-209 (May 1977), PJFrosch and AMKligman describe a method for estimating the "stinging potential" of topically administered substances. Lactic acid and pyruvic acid, for example, are used here as positive substances. When measured by this method, however, amino acids, in particular glycine, were also found to be neurosensory active (such substances are called "Stinger"). According to previous knowledge, such a sensitivity to very specific substances occurs individually in different ways. This means that a person who experiences "stinging effects" when in contact with a substance is very likely to experience it repeatedly with each subsequent contact. Contact with other "Stingers" can just as easily be without any reaction. The problem of "sensitive skin" affects a growing number of adults and children. Sensitive skin is a combination of various symptoms, such as hyper-reactive and intolerant skin. But atopic skin can also be summed up. These skin conditions are often affected by those affected, not entirely correct, referred to as "allergic" skin. Although an allergic disease can lead to symptoms of sensitive skin, the appearance of "sensitive skin" is not limited to allergy sufferers
Viele mehr oder weniger empfindliche Personen haben auch bei Verwendung mancher de- sodorierenden oder antitranspirierend wirkenden Zubereitungen unter erythematösen Hauterscheinungen zu leiden.Many more or less sensitive people also suffer from erythematous skin symptoms when using some deodorizing or antiperspirant preparations.
Erythematöse Hauterscheinungen treten auch als Begleiterscheinungen bei gewissen Hauterkrankungen oder -Unregelmäßigkeiten auf. Beispielsweise ist der typische Hautausschlag beim Erscheinungsbild der Akne regelmäßig mehr oder weniger stark gerötet.Erythematous skin symptoms also appear as a side effect with certain skin diseases or irregularities. For example, the typical rash in the appearance of acne is usually more or less reddened.
Es war also die Aufgabe der vorliegenden Erfindung, den Nachteilen des Standes der Technik abzuhelfen.It was therefore the object of the present invention to remedy the disadvantages of the prior art.
Insbesondere sollten Wirkstoffe und Zubereitungen, solche Wirkstoffe enthaltend, zur kos- metischen und dermatologischen Behandlung und/oder Prophylaxe erythematöser, entzündlicher, allergischer oder autoimmunreaktiver Erscheinungen, insbesondere Dermatosen, aber auch des Erscheinungsbildes des "Stingings" zur Verfügung gestellt werden.In particular, active substances and preparations containing such active substances should be made available for the cosmetic and dermatological treatment and / or prophylaxis of erythematous, inflammatory, allergic or autoimmune-reactive symptoms, in particular dermatoses, but also the appearance of the "stinging".
Ferner sollten solche Wirkstoffe, bzw. Zubereitungen, solche Wirkstoffe enthaltend, zur Ver- fügung g estellt werden, welche zur Immunstimulation der Haut, dabei vorteilhaft auch zur Immunstimulation im Sinne der die Wundheilung fördernden Wirkung, verwendet werden können.Furthermore, such active substances or preparations containing such active substances should be made available which can be used for immune stimulation of the skin, advantageously also for immune stimulation in the sense of the effect promoting wound healing.
In einer weiteren bevorzugten Ausführungsform betrifft die vorliegende Erfindung kosmeti- sehe und dermatologische Zubereitungen zur Prophylaxe und Behandlung kosmetischer oder dermatologischer Hautveränderungen wie z.B. der unerwünschten Pigmentierung, beispielsweise lokale Hyper- und Fehlpigmentierungen (beispielsweise Leberflecken, Sommersprossen), aber auch zur rein kosmetischen Aufhellung größerer, dem individuellen Hauttyp an sich durchaus angemessen pigmentierter Hautflächen. Für die Pigmentierung der Haut verantwortlich sind die Melanozyten, welche in der untersten Schicht der Epidermis, dem Stratum basale, neben den Basalzellen als - je nach Hauttyp entweder vereinzelt oder aber mehr oder weniger gehäuft auftretende pigmentbildende Zel- len vorzufinden sind. Melanozyten enthalten als charakteristische Zellorganellen Melanoso- men, die bei Anregung durch UV-Strahlung verstärkt Melanin bilden. Dieses wird in die Ke- ratinozyteπ transportiert und ruft eine mehr oder weniger ausgeprägte bräunliche oder braune Hautfarbe hervor.In a further preferred embodiment, the present invention relates to cosmetic and dermatological preparations for the prophylaxis and treatment of cosmetic or dermatological skin changes such as, for example, the undesired pigmentation, for example local hyper- and deficient pigmentations (for example liver spots, freckles), but also for purely cosmetic lightening of larger, the individual skin type of adequately pigmented skin areas. Melanocytes are responsible for the pigmentation of the skin. They can be found in the bottom layer of the epidermis, the stratum basale, next to the basal cells as - depending on the skin type, either isolated or more or less frequently occurring pigment-forming cells. As characteristic cell organelles, melanocytes contain melanosomes which, when stimulated by UV radiation, form increased melanin. This is transported into the keratinocyte and causes a more or less pronounced brown or brown skin color.
Melanin wird als Endstufe eines oxidativen Prozesses gebildet, in welchem Tyrosin unter Mitwirkung des Enzymes Tyrosinase über 3,4-Dihydroxyphenylalanin (Dopa), Dopa-Chinon, Leucodopachrom, Dopachrom, 5,6-Dihydroxyindol und lndol-5,6-chinon schließlich in Melanin umgewandelt wird.Melanin is formed as the final stage of an oxidative process in which tyrosine with the help of the enzyme tyrosinase via 3,4-dihydroxyphenylalanine (dopa), dopa-quinone, leucodopachrome, dopachrome, 5,6-dihydroxyindole and indole-5,6-quinone finally in Melanin is converted.
Probleme mit Hyperpigmentierung der Haut haben vielfältige Ursachen bzw. sind Begleiterscheinungen vieler biologischer Vorgänge, z.B. UV-Strahlung (z.B. Sommersprossen, Ephe- lides), genetische Disposition, Fehlpigmentierung der Haut bei der Wundheilung bzw. -vernarbung oder der Hautalterung (z.B. Lentigines seniles).Problems with hyperpigmentation of the skin have various causes or are side effects of many biological processes, e.g. UV radiation (e.g. freckles, ephe- lides), genetic disposition, incorrect pigmentation of the skin during wound healing or scarring or skin aging (e.g. Lentigines seniles).
Es sind Wirkstoffe und Zubereitungen bekannt, welche der Hautpigmentierung e ntgegen- wirken. Im praktischen Gebrauch sind im wesentlichen Präparate auf der Grundlage von Hydrochinon, welche aber einesteils erst nach mehrwöchiger Anwendung ihre Wirkung zeigen, deren übertrieben lange Anwendung andererseits aus toxikologischen Gründen bedenklich ist. Auch die Inhibierung der Tyrosinase mit Substanzen wie Kojisäure, Ascorbin- säure und Azelainsäure sowie deren Derivaten ist geläufig, hat aber kosmetische und dermatologische Nachteile.Active substances and preparations are known which counteract skin pigmentation. Preparations based on hydroquinone are essentially in practical use, but some of them only show their effect after several weeks of use, the excessive use of which is also of concern for toxicological reasons. The inhibition of tyrosinase with substances such as kojic acid, ascorbic acid and azelaic acid and their derivatives is also common, but has cosmetic and dermatological disadvantages.
Auch diesen Übelständen abzuhelfen, war Aufgabe der vorliegenden Erfindung.The object of the present invention was also to remedy these shortcomings.
Ziel der Hautpflege ist es ferner, den durch tägliche Waschen verursachten Fett- und Wasserverlust der Haut auszugleichen. Dies ist gerade dann wichtig, wenn das natürliche Regenerationsvermögen nicht ausreicht. Außerdem sollen Hautpflegeprodukte vor Umwelteinflüssen, insbesondere vor Sonne und Wind, schützen und die Hautalterung verzögern. Die chronologische Hautalterung wird z.B. durch endogene, genetisch determinierte Faktoren verursacht. In Epidermis und Dermis kommt es alterungsbedingt z.B. zu folgenden Strukturschäden und Funktionsstörungen, die auch unter den Begriff „Senile Xerosis" fallen können:The aim of skin care is also to compensate for the loss of fat and water in the skin caused by daily washing. This is especially important when the natural regeneration ability is insufficient. In addition, skin care products are intended to protect against environmental influences, especially sun and wind, and to delay skin aging. Chronological skin aging is caused, for example, by endogenous, genetically determined factors. The following structural damage and functional disorders occur in the epidermis and dermis due to aging, which can also fall under the term "senile xerosis":
a) Trockenheit, Rauhigkeit und Ausbildung von Trockenheitsfältchen, b) Juckreiz und c) verminderte Rückfettung durch Talgdrüsen (z.B. nach Waschen).a) Dryness, roughness and the formation of wrinkles due to dryness, b) itching and c) reduced regreasing due to sebum glands (e.g. after washing).
Exogene Faktoren, wie UV-Licht und chemische Noxen, können kumulativ wirksam sein und z.B. die endogenen Alterungsprozesse beschleunigen bzw. sie ergänzen. In Epidermis und Dermis kommt es i nsbesondere d urch exogene Faktoren z .B. zu folgenden Strukturschäden- und Funktionsstörungen in der Haut, die über Maß und Qualität der Schäden bei chronologischer Alterung hinausgehen:Exogenous factors such as UV light and chemical pollutants can be cumulative and e.g. accelerate or complement the endogenous aging processes. In the epidermis and dermis, there are especially exogenous factors, e.g. the following structural damage and functional disorders in the skin that go beyond the extent and quality of the damage with chronological aging:
d) Sichtbare Gefäßerweiterungen (Teleangiektasien, Cuperosis); e) Schlaffheit und Ausbildung von Falten; f) lokale Hyper-, Hypo- und Fehlpigmentierungen (z.B. Altersflecken) und g) vergrößerte Anfälligkeit gegenüber mechanischem Stress (z.B. Rissigkeit).d) visible vasodilation (telangiectasia, cuperosis); e) flaccidity and wrinkling; f) local hyper-, hypo- and incorrect pigmentations (e.g. age spots) and g) increased susceptibility to mechanical stress (e.g. cracking).
Die vorliegende Erfindung betrifft insbesondere Produkte zur Pflege der auf natürliche Weise gealterten Haut, sowie zur Behandlung der Folgeschäden der Lichtalterung, insbesondere der unter a) bis g) aufgeführten Phänomene.The present invention relates in particular to products for the care of naturally aged skin and for the treatment of the consequential damage caused by light aging, in particular the phenomena listed under a) to g).
Produkte zur Pflege gealterter Haut sind an sich bekannt. Sie enthalten z.B. Retinoide (Vitamin A-Säure und/oder deren Derivate) bzw. Vitamin A und/oder dessen Derivate. Ihre Wirkung auf die Strukturschäden ist allerdings umfangsmäßig begrenzt. Daüber hinaus gibt es bei der Produktentwicklung erhebliche Schwierigkeiten, die Wirkstoffe in ausreichendem Maße gegen oxidativen Zerfall zu stabilisieren. Die Verwendung Vitamin A-Säure-haltiger Produkte bedingt darüber hinaus oft starke erythematöse Hautreizungen. Retinoide sind daher nur in geringen Konzentrationen einsetzbar.Products for the care of aged skin are known per se. They contain e.g. Retinoids (vitamin A acid and / or its derivatives) or vitamin A and / or its derivatives. However, their effect on structural damage is limited in scope. In addition, there are considerable difficulties in product development to sufficiently stabilize the active ingredients against oxidative decay. The use of products containing vitamin A acid often causes severe erythematous skin irritation. Retinoids can therefore only be used in low concentrations.
Insbesondere betrifft die vorliegende Erfindung kosmetische Zubereitungen mit einem wirksamen S chutz vor schädlichen O xidationsprozessen i n der Haut, aber auch zum Schütze kosmetischer Zubereitungen selbst bzw. zum Schütze der Bestandteile kosmetischer Zubereitungen vor schädlichen Oxidationsprozessen.In particular, the present invention relates to cosmetic preparations with effective protection against harmful oxidation processes in the skin, but also for protection cosmetic preparations themselves or to protect the components of cosmetic preparations from harmful oxidation processes.
Die vorliegende Erfindung betrifft ferner Antioxidantien, bevorzugt solche, welche in hautpfle- genden kosmetischen oder dermatologischen Zubereitungen eingesetzt werden. Insbesondere betrifft die Erfindung auch kosmetische und dermatologische Zubereitungen, solche Antioxidantien enthaltend. In einer bevorzugten Ausführungsform betrifft die vorliegende Erfindung kosmetische und dermatologische Zubereitungen zur Prophylaxe und Behandlung kosmetischer oder dermatologischer Hautveränderungen wie z.B. der Hautalterung, insbe- sondere der durch oxidative Prozesse hervorgerufenen Hautalterung.The present invention further relates to antioxidants, preferably those which are used in skin-care cosmetic or dermatological preparations. In particular, the invention also relates to cosmetic and dermatological preparations containing such antioxidants. In a preferred embodiment, the present invention relates to cosmetic and dermatological preparations for the prophylaxis and treatment of cosmetic or dermatological skin changes such as e.g. skin aging, especially skin aging caused by oxidative processes.
Weiterhin betrifft die vorliegende Erfindung Wirkstoffe und Zubereitungen, solche Wirkstoffe enthaltend, zur kosmetischen und dermatologischen Behandlung oder Prophylaxe erythematöser, entzündlicher, allergischer oder autoimmunreaktiver Erscheinungen, insbesondere Dermatosen.The present invention further relates to active substances and preparations containing such active substances for cosmetic and dermatological treatment or prophylaxis of erythematous, inflammatory, allergic or autoimmune-reactive symptoms, in particular dermatoses.
Die vorliegende Erfindung betrifft in einer weiteren vorteilhaften Ausführungsform Wirkstoffkombinationen und Zubereitungen, die zur Prophylaxe und Behandlung der lichtempfindlichen Haut, insbesondere von Photodermatosen, dienen.In a further advantageous embodiment, the present invention relates to active substance combinations and preparations which are used for the prophylaxis and treatment of light-sensitive skin, in particular photodermatoses.
Die schädigende Wirkung des ultravioletten Teils der Sonnenstrahlung auf die Haut ist allgemein bekannt. Während Strahlen mit einer Wellenlänge, die kleiner als 290 nm ist (der sogenannte UVC-Bereich), von der Ozonschicht in der Erdatmosphäre absorbiert werden, verursachen Strahlen im Bereich zwischen 290 nm und 320 nm, dem sogenannten UVB- Bereich, ein Erythem, einen einfachen Sonnenbrand oder sogar mehr oder weniger starke Verbrennungen.The damaging effect of the ultraviolet part of solar radiation on the skin is well known. While rays with a wavelength shorter than 290 nm (the so-called UVC range) are absorbed by the ozone layer in the earth's atmosphere, rays in the range between 290 nm and 320 nm, the so-called UVB range, cause an erythema simple sunburn or even more or less severe burns.
Als ein Maximum der Erythemwirksamkeit des Sonnenlichtes wird der engere Bereich um 308 nm angegeben.The narrower range around 308 nm is given as a maximum of the erythema effectiveness of sunlight.
Zum Schutz gegen UVB-Strahlung sind zahlreiche Verbindungen bekannt, bei denen es sich um Derivate des 3-Benzylidencamphers, der 4-Aminobenzoesäure, der Zimtsäure, der Sali- cylsäure, des Benzophenons sowie auch des 2-Phenylbenzimidazols handelt. Auch für den Bereich zwischen etwa 320 nm und etwa 400 nm, des sogenannten UVA- Bereich, ist es wichtig, Filtersubstanzen zur Verfügung zu haben, da dessen Strahlen Reaktionen bei lichtempfindlicher Haut hervorrufen können. Es ist erwiesen, dass UVA-Strahlung zu einer Schädigung der elastischen und kollagenen Fasern des Bindegewebes führt, was die Haut vorzeitig altern lässt, und dass sie als Ursache zahlreicher phototoxischer und photoallergischer Reaktionen zu sehen ist. Der schädigende Einfluss der UVB-Strahlung kann durch UVA-Strahlung verstärkt werden.Numerous compounds are known for protection against UVB radiation, which are derivatives of 3-benzylidene camphor, 4-aminobenzoic acid, cinnamic acid, salicylic acid, benzophenone and also 2-phenylbenzimidazole. It is also important to have filter substances available for the range between about 320 nm and about 400 nm, the so-called UVA range, since their rays can cause reactions in light-sensitive skin. It has been proven that UVA radiation damages the elastic and collagen fibers of the connective tissue, which causes the skin to age prematurely, and that it can be seen as the cause of numerous phototoxic and photoallergic reactions. The damaging influence of UVB radiation can be intensified by UVA radiation.
Zum Schutz gegen die Strahlen des UVA-Bereichs werden daher gewisse Derivate des Di- benzoylmethans verwendet, deren Photostabilität (Int. J. Cosm. Science 10, 53 (1988)), nicht in ausreichendem Maße gegeben ist.To protect against the rays of the UVA range, certain derivatives of di-benzoylmethane are therefore used, the photostability (Int. J. Cosm. Science 10, 53 (1988)) of which is insufficient.
Die UV-Strahlung kann aber auch zu photochemischen Reaktionen führen, wobei dann die photochemischen Reaktionsprodukte in den Hautmetabolismus eingreifen.However, UV radiation can also lead to photochemical reactions, in which case the photochemical reaction products interfere with the skin's metabolism.
Vorwiegend handelt es sich bei solchen photochemischen Reaktionsprodukten um radikalische Verbindungen, beispielsweise Hydroxylradikale, Singulettsauerstoff. Auch Undefinierte radikalische Photoprodukte, welche in der Haut selbst entstehen, können aufgrund ihrer hohen Reaktivität unkontrollierte Folgereaktionen an den Tag legen. Aber auch Singulettsauer- Stoff, ein nichtradikalischer angeregter Zustand des Sauerstoffmoleküls kann bei UV- Bestrahlung auftreten, ebenso kurzlebige Epoxide und viele andere. Singulettsauerstoff beispielsweise zeichnet sich gegenüber dem normalerweise vorliegenden Triplettsauerstαff (radikalischer Grundzustand) durch gesteigerte Reaktivität aus. Allerdings existieren auch angeregte, reaktive (radikalische) Triplettzustände des Sauerstoffmoleküls.Such photochemical reaction products are predominantly free radical compounds, for example hydroxyl radicals, singlet oxygen. Undefined radical photo products, which are created in the skin itself, can also display uncontrolled subsequent reactions due to their high reactivity. But also singlet oxygen, a non-radical excited state of the oxygen molecule can occur with UV radiation, just as short-lived epoxies and many others. Singlet oxygen, for example, is characterized by increased reactivity compared to the triplet oxygen (radical ground state) that is normally present. However, there are also excited, reactive (radical) triplet states of the oxygen molecule.
Ferner zählt UV-Strahlung zur ionisierenden Strahlung. Es besteht also das Risiko, dass auch ionische Spezies bei UV-Exposition entstehen, welche dann ihrerseits oxidativ in die biochemischen Prozesse einzugreifen vermögen.UV radiation also belongs to ionizing radiation. There is therefore a risk that ionic species also develop when exposed to UV, which in turn can then oxidatively intervene in the biochemical processes.
Um diesen Reaktionen vorzubeugen, können den kosmetischen bzw. dermatologischen Formulierungen zusätzliche Antioxidantien und/oder Radikalfänger einverleibt werden.In order to prevent these reactions, additional antioxidants and / or free radical scavengers can be incorporated into the cosmetic or dermatological formulations.
Es ist bereits vorgeschlagen worden, Vitamin E, eine Substanz mit bekannter antioxidativer Wirkung in Lichtschutzformulierungen einzusetzen, dennoch bleibt auch hier die erzielte Wir- kung weit hinter der erhofften zurück.It has already been proposed to use vitamin E, a substance with a known antioxidant effect, in light protection formulations, but the efficacy achieved here still remains. kung far behind the hoped for.
Aufgabe der Erfindung war es daher auch, kosmetische, dermatologische und pharmazeutische Wirkstoffe und Zubereitungen sowie Lichtschutzformulierungen zu schaffen, die zur Prophylaxe und Behandlung lichtempfindlicher Haut, insbesondere Photodermatosen, bevorzugt PLD dienen.The object of the invention was therefore also to provide cosmetic, dermatological and pharmaceutical active substances and preparations and light protection formulations which are used for the prophylaxis and treatment of light-sensitive skin, in particular photodermatoses, preferably PLD.
Weitere Bezeichnungen für die polymorphe Lichtdermatose sind PLD, PLE, Mallorca-Akne und eine Vielzahl von weiteren Bezeichnungen, wie sie in der Literatur (z.B. A. Voelckel et al, Zentralblatt Haut- und Geschlechtskrankheiten (1989), 156, S.2), angegeben sind.Other names for polymorphic light dermatosis are PLD, PLE, Mallorca acne and a variety of other names, such as those in the literature (e.g. A. Voelckel et al, Zentralblatt Haut- und Sexually Diseases (1989), 156, p.2), are specified.
Hauptsächlich werden Antioxidantien als Schutzsubstanzen gegen den Verderb der sie enthaltenden Zubereitungen verwendet. Dennoch ist bekannt, dass auch in der menschlichen und tierischen Haut unerwünschte Oxidationsprozesse auftreten können. Solche Prozesse spielen eine wesentliche Rolle bei der Hautalterung.Antioxidants are mainly used as protective substances against the spoilage of the preparations containing them. Nevertheless, it is known that undesirable oxidation processes can also occur in human and animal skin. Such processes play an essential role in skin aging.
Im Aufsatz "Skin Diseases Associated with Oxidative Injury" in "Oxidative Stress in Der- matology", S. 323 ff. (Marcel Decker Inc., New York, Basel, Hong Kong, Herausgeber: Jürgen Fuchs, Frankfurt, und Lester Packer, Berkeley/Californien), werden oxidative Schäden der Haut und ihre näheren Ursachen aufgeführt.In the article "Skin Diseases Associated with Oxidative Injury" in "Oxidative Stress in Dermatology", p. 323 ff. (Marcel Decker Inc., New York, Basel, Hong Kong, publisher: Jürgen Fuchs, Frankfurt, and Lester Packer, Berkeley / California), oxidative damage to the skin and its closer causes are listed.
Auch aus dem Grunde, solchen Reaktionen vorzubeugen, können kosmetischen oder dermatologischen Formulierungen zusätzlich Antioxidantien und/oder Radikalfänger einverleibt werden.Also for the reason of preventing such reactions, additional antioxidants and / or free radical scavengers can be incorporated into cosmetic or dermatological formulations.
Zwar sind einige Antioxidantien und Radikalfänger bekannt. So ist bereits in den US-Patentschriften 4,144,325 und 4,248,861 sowie aus zahlreichen anderen Dokumenten vorgeschlagen worden, Vitamin E, eine Substanz mit bekannter antioxidativer Wirkung in Lichtschutzformulierungen e inzusetzen, d ennoch b leibt auch hier die erzielte Wirkung weit hinter der erhofften zurück.Some antioxidants and radical scavengers are known. It has already been proposed in US Pat. Nos. 4,144,325 and 4,248,861 and from numerous other documents to use vitamin E, a substance with a known antioxidant effect in sunscreen formulations, but the effect achieved here also falls far short of the hoped-for effect.
Aufgabe der vorliegenden Erfindung war es somit, Wege zu finden, die die Nachteile des Standes der Technik vermeiden. Insbesondere soll die Wirkung der Behebung der mit der endogenen, chronologischen u nd exogenen H autalterung verbundenen S chäden u nd d ie Prophylaxe dauerhaft, nachhaltig und ohne das Risiko von Nebenwirkungen sein.The object of the present invention was therefore to find ways which avoid the disadvantages of the prior art. In particular, the effect of repairing the damage associated with endogenous, chronological and exogenous skin aging and the Prophylaxis to be permanent, sustainable and without the risk of side effects.
Erfindungsgemäß werden die Übelstände des Standes der Technik beseitigt durch Wirk- stoffkombinationen aus (a) einem oder mehreren 2,3-Dibenzylbutyrolactonderivaten undAccording to the invention, the deficiencies of the prior art are eliminated by combinations of active ingredients from (a) one or more 2,3-dibenzylbutyrolactone derivatives and
(b) Licochalcon A oder einem wässrigen Extrakt aus Radix Glycyrrhizae inflatae, enthaltend Licochalcon A(b) Licochalcon A or an aqueous extract from Radix Glycyrrhizae inflatae, containing Licochalcon A
bzw. kosmetische oder dermatologische Zubereitungen, solche Wirkstoffkombinationen enthaltend.or cosmetic or dermatological preparations containing such active ingredient combinations.
Zubereitungen gemäß der Erfindung bzw. kosmetische oder dermatologische Zubereitungen, sind in jeglicher Hinsicht überaus befriedigende Präparate. Es war für den Fachmann nicht vorauszusehen, dass die Zubereitungen gemäß der Erfindung - besser die Barriereeigenschaften der Haut erhalten oder wiederherstellen,Preparations according to the invention or cosmetic or dermatological preparations 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 - better maintain or restore the barrier properties of the skin,
- besser der Hautaustrocknung entgegenwirken,- counteract dehydration better,
- besser gegen Pigmentstörungen wirken,- work better against pigment disorders,
- besser gegen entzündliche Hautzustände wirken- work better against inflammatory skin conditions
- besser gegen die Hautalterung wirken und - die Haut besser vor Umwelteinflüssen schützen als die Zubereitungen des Standes der Technik.- work better against skin aging and - protect the skin better from environmental influences than the preparations of the prior art.
Die Verwendung erfindungsgemäßer Wirkstoffkombinationen bzw. kosmetischer oder topischer dermatologischer Zubereitungen mit einem wirksamen Gehalt an erfindungsgemäßen Wirkstoffkombinationen bietet in überraschender Weise eine wirksame Behandlung, aber auch eine Prophylaxe von defizitären, sensitiven oder hypoaktiven Hautzuständen oder defizitären, sensitiven oder hypoaktiven Zustände von Hautanhangsgebilden von Erscheinungen vorzeitiger Alterung der Haut (z.B. Falten, Altersflecken, Telean- giektasien) und/oder der Hautanhangsgebilde, von umweltbedingten (Rauchen, Smog, reaktive Sauerstoffspecies, freie Radikale) und insbesondere lichtbedingten negativen Veränderungen der Haut und der Hautanhangsgebilde, von lichtbedingten Hautschäden - t von Pigmentierungsstörungen, von empfindlicher, gereizter und juckender Haut, von trockenen Hautzuständen und Homschichtbarrierestörungen, von Haarausfall und für verbessertes Haarwachstum - von entzündlichen Hautzuständen sowie atopischem Ekzem, seborrhoischem Ekzem, polymorpher Lichtdermatose, Psöriasis, VitiligoThe use of active ingredient combinations according to the invention or cosmetic or topical dermatological preparations with an effective content of active ingredient combinations according to the invention surprisingly offers effective treatment, but also prophylaxis of deficient, sensitive or hypoactive skin conditions or deficit, sensitive or hypoactive conditions of skin appendages of signs of premature aging the skin (eg wrinkles, age spots, telangiectasia) and / or the appendages of the skin, of environmental ones (smoking, smog, reactive oxygen species, free radicals) and in particular light-related negative changes in the skin and appendages, of light-related skin damage - t from pigmentation disorders, from sensitive, irritated and itchy skin, from dry skin conditions and barrier layer disorders, from hair loss and for improved hair growth - from inflammatory skin conditions as well as atopic eczema, seborrheic eczema, polymorphic light dermatosis, psoriasis, vitiligo
möglich. Der erfindungsgemäße Wirkstoffes bzw. kosmetischer oder topischer dermatologischer Zubereitungen mit einem wirksamen Gehalt an erfindungsgemäßem Wirkstoff dient aber auch in überraschender Weise zur Beruhigung von empfindlicher oder gereizter Haut zur Stimulation der Kollagen-, Hyaluronsäure-, Elastinsynthese zur Stimulation der Ceramidsynthese der Haut - zur Stimulation der intrazellulären DNA-Synthese, insbesondere bei defizitären oder hypoaktiven Hautzuständen. zur Steigerung der Zellerneuerung und Regeneration der Haut zur Steigerung der hauteigenen Schutz- und Reparaturmechanismen (beispielsweise für dysfunktionelle Enzyme, DNA, Lipide, Proteine) - zur Vor- und Nachbehandlung bei topischer Anwendung von Laser- und Abschleifbehandlungen, die z. B. der Reduzierung von Hautfalten und Narben dienen, um den resultierenden Hautreizungen entgegenzuwirken und die Regenerationsprozesse in der verletzten Haut zu fördern.possible. The active ingredient according to the invention or cosmetic or topical dermatological preparations with an effective content of the active ingredient according to the invention also surprisingly serves to calm sensitive or irritated skin to stimulate collagen, hyaluronic acid, elastin synthesis to stimulate ceramide synthesis of the skin - to stimulate the skin intracellular DNA synthesis, especially for deficient or hypoactive skin conditions. to increase cell renewal and regeneration of the skin to increase the skin's own protection and repair mechanisms (e.g. for dysfunctional enzymes, DNA, lipids, proteins) - for pre-treatment and post-treatment with topical application of laser and abrasive treatments, e.g. B. serve the reduction of skin folds and scars to counteract the resulting skin irritation and to promote the regeneration processes in the injured skin.
Vorzugsweise liegen in den erfindungsgemäßen Wirkstoffkombinationen das oder die 2,3- Dibenzylbutyrolactonderivate und Licochalcon A in Verhältnissen von 50 : 1 bis 1 : 50, bevorzugt 10 : 1 bis 1 : 10, besonders bevorzugt 2 : 1 bis 1 : 2 vor.The 2,3-dibenzylbutyrolactone derivatives and licochalcone A are preferably present in the active compound combinations according to the invention in ratios of 50: 1 to 1:50, preferably 10: 1 to 1:10, particularly preferably 2: 1 to 1: 2.
Die erfindungsgemäßen 2,3-Dibenzylbutyrolactonderivate und/oder deren Glycoside leiten sich von dem ebenfalls erfindungsgemäßen 2,3-Dibenzylbutyrolacton ab, welches durch die folgende Struktur gekennzeichnet ist: The 2,3-dibenzylbutyrolactone derivatives according to the invention and / or their glycosides are derived from the 2,3-dibenzylbutyrolactone also according to the invention, which is characterized by the following structure:
2,3-Dibenzylbutyrolacton 2,3-Dibenzylbutyrolacton
Erfindungsgemäß sind 2,3-Dibenzylbutyrolactoπ, 2,3-Dibenzylbutyrolactondehvate und/oder deren Glycoside in all ihren stereoisomeren Formen, die sowohl als Racemat als auch in e- nantiomerenreiner Form, sowie in racemischen Gemischen mit unterschiedlichen Enantiome- renanteilen vorliegen können. Erfindungsgemäß umfasst die Formulierung 2,3- Dibenzylbutyrolactonderivate und/oder deren Glycoside auch das 2,3-Dibenzylbutyrolacton.According to the invention, 2,3-dibenzylbutyrolactone, 2,3-dibenzylbutyrolactone derivatives and / or their glycosides in all their stereoisomeric forms, which can be present both as a racemate and in enantiomerically pure form, and also in racemic mixtures with different enantiomeric proportions. According to the invention, the formulation comprises 2,3-dibenzylbutyrolactone derivatives and / or their glycosides also the 2,3-dibenzylbutyrolactone.
Die erfindungsgemäßen 2,3-Dibenzylbutyrolactonderivate und/oder deren Glycoside können der erfindungsgemäßen Zubereitung vorteilhaft in Form von Pflanzenextrakten zugesetzt werden. Dabei haben sich wässrig-alkoholische Extrakte aus Pflanzen besonders bewährt. Jedoch sind auch mit anderen Extraktionsformen u nd M ethoden g ewonnene Extrakte u nd Destillate, beispielsweise mit Kohlendioxid als Extraktionsmittel gewonnene Extrakte sowie Wasserdampfdestillate, erfindungsgemäß vorteilhaft in die Zubereitungen einzuformulieren.The 2,3-dibenzylbutyrolactone derivatives according to the invention and / or their glycosides can advantageously be added to the preparation according to the invention in the form of plant extracts. Aqueous-alcoholic extracts from plants have proven particularly useful. However, extracts and distillates obtained with other forms of extraction and methods, for example extracts obtained with carbon dioxide as extracting agent and steam distillates, can also be advantageously formulated into the preparations according to the invention.
Es ist dabei erfindungsgemäß besonders vorteilhaft, Pflanzenextrakte von Arctium lappa L (Große Klette) und/oder Steganotaenia araliacea (Karottenbaum) einzusetzen.It is particularly advantageous according to the invention to use plant extracts of Arctium lappa L (large burdock) and / or Steganotaenia araliacea (carrot tree).
Als erfindungsgemäß bevorzugte 2,3-Dibenzylbutyrolactonderivate und/oder deren Glycoside werden Arctiin, Arctigenin, Prestegan B, Matairesinol, Trachelosid und/oder Trachelogenin eingesetzt.Arctiin, arctigenin, Prestegan B, matairesinol, tracheloside and / or trachelogenin are used as 2,3-dibenzylbutyrolactone derivatives preferred according to the invention and / or their glycosides.
Erfindungsgemäß besonders bevorzugt sind dabei die Derivate mit dem folgenden stereochemischen Aufbau: According to the invention, the derivatives with the following stereochemical structure are particularly preferred:
Trachelo genin TrachelosidTrachelo genin tracheloside
Matairesinol Prestegan B Matairesinol Prestegan B
Erfindungsgemäß ganz besonders bevorzugt ist das Arctiin und das Prestegan B. Die erfindungsgemäßen 2,3-Dibenzylbutyrolactonderivate und/oder d eren G lycoside I assen sich problemlos üblichen kosmetischen und/oder dermatologischen Zubereitungen, wie Lichtschutzzubereitungen, Hautpflegezubereitungen, Antifalten-Zubereitungen, aber auch an- deren Zubereitungen, beispielsweise pharmazeutischen Zubereitungen einverleiben.Arctiin and prestegan B are very particularly preferred according to the invention. The 2,3-dibenzylbutyrolactone derivatives and / or their glycosides according to the invention can be easily incorporated into conventional cosmetic and / or dermatological preparations, such as sunscreen preparations, skin care preparations, anti-wrinkle preparations, but also other preparations, for example pharmaceutical preparations.
Vorteilhaft enthalten erfindungsgemäße Zubereitungen 0,01 - 25 Gew.-% eines oder mehrerer 2,3-Dibenzylbutyrolactonderivate, bevorzugt 0,1 - 20 Gew.-%, insbesondere 1 - 10 Gew.- %, jeweils bezogen auf das Gesamtgewicht der Zubereitungen.Preparations according to the invention advantageously contain 0.01-25% by weight of one or more 2,3-dibenzylbutyrolactone derivatives, preferably 0.1-20% by weight, in particular 1-10% by weight, in each case based on the total weight of the preparations.
Die Pflanzenart Glycyrrhiza inflata gehört wie das in Europa offizineile Süßholz Glycyrrhiza glabra der Gattung Glycyrrhiza an, die zur Pflanzenfamilie der Fabaceae (Erbsengewächse) gehört. Die Droge Radix Glycyrrhizae inflatae, d.h., die Wurzel der Pflanze, ist, beispielsweise in der fernöstlichen Medizin, gebräuchlich. Die Verwendung der Droge als Entzündungshemmer ist ebenfalls bekannt.The plant species Glycyrrhiza inflata, like the licorice Glycyrrhiza glabra, which belongs to Europe, belongs to the genus Glycyrrhiza, which belongs to the Fabaceae (pea family) plant family. The drug Radix Glycyrrhizae inflatae, i.e. the root of the plant, is used, for example, in Far Eastern medicine. The use of the drug as an anti-inflammatory is also known.
Ein Bestandteil des wässrigen Auszugs aus Radix Glycyrrhizae inflatae ist das LicochalconA component of the aqueous extract from Radix Glycyrrhizae inflatae is the licochalcon
A, welches sich durch die folgende Strukturformel auszeichnet:A, which is characterized by the following structural formula:
Es w ird a ngenommen, d ass d iese S ubstanz, m öglicherweise i n S ynergie mit den übrigen Bestandteilen des Extraktes, Anteil an der erfindungsgemäßen Wirkung besitzt. It is assumed that this substance, possibly in synergy with the other constituents of the extract, has a share in the effect according to the invention.
Vorteilhaft ist erfindungsgemäß insbesondere, wenn die Zubereitungen 0,0001 bis 5 Gew.- %, insbesondere 0,001 bis 1 Gew.-%, ganz besonders 0,005 bis 0,15 Gew.-% Licochalcon A enthalten, bezogen auf das Gesamtgewicht der Zubereitung. Vorteilhaft ist erfindungsgemäß ferner insbesondere wenn die Zubereitungen 0,001 bis 10 Gew.-%, insbesondere 0,05 bis 5 Gew.-%, ganz besonders 0,01 bis 2 Gew.-% an einem oder mehreren Polyolen enthalten, bezogen auf das Gesamtgewicht der Zubereitung.It is particularly advantageous according to the invention if the preparations contain 0.0001 to 5% by weight, in particular 0.001 to 1% by weight, very particularly 0.005 to 0.15% by weight of licochalcone A, based on the total weight of the preparation. It is also advantageous according to the invention in particular if the preparations contain 0.001 to 10% by weight, in particular 0.05 to 5% by weight, very particularly 0.01 to 2% by weight, of one or more polyols, based on the total weight of the Preparation.
Vorteilhaft ist erfindungsgemäß femer wenn die Zubereitungen Licocalchon als Bestandteil von pflanzlichen Extracten, insbesondere von Radix Glycyrrhizae inflatae, enthalten.It is also advantageous according to the invention if the preparations contain licocalchon as a constituent of plant extracts, in particular of Radix Glycyrrhizae inflatae.
Erfindungsgemäß ist ferner vorteilhaft, wenn Licochalcon in Form eines wässrigen Auszugs vorliegt, in welchem - Licochalcon A Wasser gegebenenfalls ein oder mehrere Polyole vorliegen.It is also advantageous according to the invention if licochalcone is in the form of an aqueous extract in which - licochalcone A water, if appropriate, one or more polyols are present.
Es ist erfindungsgemäß vorteilhaft, wenn die kosmetischen oder dermatolog ischen Zubereitungen 0,001 bis 10 Gew.-%, insbesondere 0,05 bis 5 Gew.-%, ganz besonders 0,01 bis 2 Gew.-% an einem wässrigen Extrakt aus Radix Glycyrrhizae inflatae enthalten, bezogen auf das Gesamtgewicht der Zubereitung.It is advantageous according to the invention if the cosmetic or dermatological preparations 0.001 to 10% by weight, in particular 0.05 to 5% by weight, very particularly 0.01 to 2% by weight, of an aqueous extract from Radix Glycyrrhizae inflatae included, based on the total weight of the preparation.
Es ist erfindungsgemäß vorteilhaft, wenn die kosmetischen oder dermatologischen Zubereitungen 0,001 bis 10 Gew.-%, insbesondere 0,05 bis 5 Gew.-%, ganz besonders 0,01 bis 2 Gew.-% an einem oder mehreren Polyolen enthalten, bezogen auf das Gesamtgewicht der Zubereitung.It is advantageous according to the invention if the cosmetic or dermatological preparations contain 0.001 to 10% by weight, in particular 0.05 to 5% by weight, very particularly 0.01 to 2% by weight, of one or more polyols, based on the total weight of the preparation.
Insbesondere ist vorteilhaft, als Polyol das Butylenglycol zu wählen. IIt is particularly advantageous to choose butylene glycol as the polyol. I
Ganz besonders vorteilhaft ist es, von einem Extrakt auszugehen, der unter der Bezeichnung Polyol Soluble Licorice Extract P-U von der Firma Maruzen vertrieben wird.It is particularly advantageous to start with an extract that is marketed by the Maruzen company under the name Polyol Soluble Licorice Extract P-U.
Ferner ist es vorteilhaft, Licochalcone A in anderen Vehikelsystemen in einer Konzentration von 0,0001 bis 5 Gew.-%, insbesondere 0,001 bis 1 Gew.-%, ganz besonders 0,005 - 0,05 Gew.-% zu verwenden. Erfindungsgemäß ist demnach auch die Verwendung erfindungsgemäßer Wirkstoffkombinationen zur Prophylaxe und Behandlung von entzündlichen Hautzuständen - auch dem atopi- schen Ekzem - und/oder zum Hautschutz bei empfindlich determinierter trockener Haut.It is also advantageous to use Licochalcone A in other vehicle systems in a concentration of 0.0001 to 5% by weight, in particular 0.001 to 1% by weight, very particularly 0.005-0.05% by weight. Accordingly, the use of active substance combinations according to the invention for the prophylaxis and treatment of inflammatory skin conditions - including atopic eczema - and / or for skin protection in the case of sensitive, determined dry skin is accordingly also according to the invention.
Erfindungsgemäß ist demnach auch die Verwendung erfindungsgemäßer Wirkstoffkombinationen zur Herstellung von kosmetischen oder dermatologischen Zubereitungen zur Herstellung von kosmetischen oder dermatologischen Zubereitungen zur Behandlung und/oder Prophylaxe von Pigmentierungsstörungen.Accordingly, the use of active compound combinations according to the invention for the production of cosmetic or dermatological preparations for the production of cosmetic or dermatological preparations for the treatment and / or prophylaxis of pigmentation disorders is also in accordance with the invention.
Erfindungsgemäß ist demnach auch die Verwendung erfindungsgemäßer Wirkstoffkombina- tionen zur Herstellung von kosmetischen oder dermatologischen Zubereitungen zur Behandlung und/oder Prophylaxe der Symptome der intrinsischen und/oder extrinεischen Hautalterung sowie zur Behandlung und Prophylaxe der schädlichen Auswirkungen ultravioletter Strahlung auf die HautAccordingly, the use of active substance combinations according to the invention for the production of cosmetic or dermatological preparations for the treatment and / or prophylaxis of the symptoms of intrinsic and / or extrinsic skin aging and for the treatment and prophylaxis of the harmful effects of ultraviolet radiation on the skin is accordingly also according to the invention
Erfindungsgemäß ist demnach auch die Verwendung erfindungsgemäßer Wirkstoffkombinationen zur Herstellung von kosmetischen oder dermatologischen Zubereitungen zur Steigerung der Ceramidbiosynthese.Accordingly, the use of active compound combinations according to the invention for the production of cosmetic or dermatological preparations for increasing ceramide biosynthesis is also in accordance with the invention.
Erfindungsgemäß ist demnach auch die Verwendung erfindungsgemäßer Wirkstoffkombinationen zur Herstellung von kosmetischen oder dermatologischen Zubereitungen zur Stärkung der Barrierefunktion der Haut.Accordingly, the use of active substance combinations according to the invention for the production of cosmetic or dermatological preparations for strengthening the barrier function of the skin is also in accordance with the invention.
Bevorzugt enthalten kosmetische oder dermatologische Zubereitungen gemäß der Erfindung 0,001 - 1 0 G ew.-%, besonders bevorzugt 0 ,01 - 1 Gew.-%, an erfindungsgemäße Wirkstoffkombinationen, bezogen auf die Gesamtzusammensetzung der Zubereitungen.Cosmetic or dermatological preparations according to the invention preferably contain 0.001-1.0% by weight, particularly preferably 0.01-1% by weight, of active compound combinations according to the invention, based on the total composition of the preparations.
Es ist erfindungsgemäß insbesondere äußerst vorteilhaft, erfindungsgemäße Wirkstoffkombinationen bzw. kosmetische oder topische dermatologische Zubereitungen mit einem wirk- samen Gehalt an erfindungsgemäßen Wirkstoffkombinationen zur kosmetischen oder dermatologischen Behandlung oder Prophylaxe unerwünschter Hautzustände zu verwenden.It is particularly advantageous according to the invention to use active ingredient combinations according to the invention or cosmetic or topical dermatological preparations with an effective content of active ingredient combinations according to the invention for cosmetic or dermatological treatment or prophylaxis of undesirable skin conditions.
Erfindungsgemäß können Zubereitungen welche erfindungsgemäße Wirkstoffkombinationen enthalten, übliche Antioxidantien eingesetzt werden. Vorteilhaft werden die Antioxidantien gewählt aus der Gruppe bestehend aus Aminosäuren (z.B. Glycin, Histidin, Tyrosin, Tryptophan) und deren Derivate, Imidazole (z.B. Urocaninsäu- re) und deren Derivate, Peptide wie D,L-Carnosin, D-Carnosin, L-Carnosin und deren Der- ivate (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. Dihydroli- ponsäure), Aurothioglucose, Propylthiouracil und andere Thiole (z.B. Thioredoxin, Gluta- thion, Cystein, Cystin, Cystamin und deren Glycosyl-, N-Acetyl-, Methyl-, Ethyl-, Propyl-, Amyl-, Butyl- und Lauryl-, Palmitoyl-, Oleyl-, γ-Linoleyl-, Cholesteryl- und Glycerylester) so- wie deren Salze, Dilaurylthiodipropionat, Distearylthiodipropionat, Thiodipropionsäure und deren Derivate (Ester, Ether, Peptide, Lipide, Nukleotide, Nukleoside und Salze) sowie Sul- foximinverbindungen (z.B. Buthioninsulfoximine, Homocysteinsulfoximin, Buthioninsulfone, Penta-, Hexa-, Heptathioninsulfoximin) in sehr geringen verträglichen Dosierungen (z.B. pmol bis μmol/kg), ferner (Metali)-Chelatoren (z.B. α-Hydroxyfettsäuren, Palmitinsäure, Phy- tinsäure, Lactoferrin), α-Hydroxysäuren (z.B. Citronensäure, Milchsäure, Apfeisäure), Hu- minsäure, Gallensäure, Gallenextrakte, Bilirubin, Biliverdin, EDTA, EGTA und deren Derivate, u ngesättigte Fettsäuren u nd d eren D erivate (z.B. γ-Linolensäure, L inolsäure, 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-palmitat) sowie Konife- rylbenzoat des Benzoeharzes, Rutinsäure und deren Derivate, α-Glycosylrutin, Ferulasäure, Furfurylidenglucitol, Carnosin, Butylhydroxytoluol, Butylhydroxyanisol, Nordihydroguajakharz- säure, Nordihydroguajaretsäure, Trihydroxybutyrophenon, Harnsäure und deren Derivate, Mannose und deren Derivate, Zink und dessen Derivate (z.B. ZnO, ZnS04) Selen und des- sen Derivate (z.B. Selenmethionin), Stilbene und deren Derivate (z.B. Stilbenoxid, Trans-Stil- benoxid) und d ie e rfindungsgemäß g eeigneten D erivate ( Salze, E ster, E ther, Z ucker, N u- kleotide, Nukleoside, Peptide und Lipide) dieser genannten Wirkstoffe.According to the invention, preparations containing active substance combinations according to the invention, customary antioxidants can be used. The antioxidants are advantageously selected from the group consisting of amino acids (eg glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (eg urocanic acid) and their derivatives, peptides such as D, L-carnosine, D-carnosine, L- Carnosine and its derivatives (eg anserine), carotenoids, carotenes (eg α-carotene, β-carotene, lycopene) and their derivatives, chlorogenic acid and their derivatives, lipoic acid and their derivatives (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) as well as 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. buthioninsulfoxinsulfoximine, homocystone, homocystone pent α-, hexa-, heptathioninsulfoximine) in very low tolerable doses (e.g. pmol to μmol / kg), also (metal) chelators (e.g. α-hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), α-hydroxy acids (e.g. 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 (e.g. γ-linolenic acid, linoleic acid, oleic acid), folic acid and its derivatives, Ubiquinone and ubiquinol and their derivatives, vitamin C and derivatives (e.g. 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 Benzoin, rutinic acid and its derivatives, α-glycosyl rutin, ferulic acid, furfurylidene glucitol, carnosine, butylated hydroxytoluene, butylated hydroxyanisole, nordihydroguajak resin acid, nordihydroguajaretic acid, trihydroxybutyrophenone, uric acid and its derivative e, mannose and its derivatives, zinc and its derivatives (for example ZnO, ZnS0 4 ) selenium and its derivatives (for example selenium methionine), stilbenes and their derivatives (for example stilbene oxide, trans-stilbene oxide) and which are suitable according to the invention Derivatives (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids) of these active ingredients.
Die Menge der Antioxidantien (eine oder mehrere Verbindungen) in den Zubereitungen be- trägt vorzugsweise 0,001 bis 30 Gew.-%, besonders bevorzugt 0,05 - 20 Gew.-%, insbesondere 1 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitung.The amount of the antioxidants (one or more compounds) in the preparations is preferably 0.001 to 30% by weight, particularly preferably 0.05-20% by weight, in particular 1-10% by weight, based on the total weight the preparation.
Die Prophylaxe bzw. die kosmetische oder dermatolog ische Behandlung mit dem erfindungsgemäß verwendeten Wirkstoff bzw. mit den kosmetischen oder topischen derma- tologischen Zubereitungen mit einem wirksamen Gehalt an erfindungsgemäß verwendetem Wirkstoff erfolgt in der üblichen Weise, und zwar dergestalt, dass der erfindungsgemäß verwendete Wirkstoff bzw. die kosmetischen oder topischen dermatologischen Zubereitungen mit einem wirksamen Gehalt an erfindungsgemäß verwendetem Wirkstoff auf die betroffe- nen Hautstellen aufgetragen wird.The prophylaxis or the cosmetic or dermatological treatment with the active ingredient used according to the invention or with the cosmetic or topical dermatological Tological preparations with an effective content of active ingredient used according to the invention are carried out in the usual way, in such a way that the active ingredient used according to the invention or the cosmetic or topical dermatological preparations with an effective content of active ingredient used according to the invention is applied to the affected skin areas.
Vorteilhaft kann der erfindungsgemäß verwendete Wirkstoff eingearbeitet werden in übliche kosmetische und dermatologische Zubereitungen, welche in verschiedenen Formen vorliegen können. So können sie z.B. eine Lösung, eine Emulsion vom Typ Wasser-in-ÖI (W/O) oder vom Typ Öl-in-Wasser (O/W), oder eine multiple Emulsionen, beispielsweise vom Typ Wasser-in-ÖI-in-Wasser (W/O/W) oder Öl-in-Wasser-in-ÖI (O/W/O), eine Hydrodispersion oder Lipodispersion, ein Gel, einen festen Stift oder auch ein Aerosol darstellen.The active ingredient used according to the invention can advantageously be incorporated into customary cosmetic and dermatological preparations, which can be in various forms. So you can e.g. a solution, an emulsion of the type water-in-oil (W / O) or of the type oil-in-water (O / W), or a multiple emulsions, for example of the type water-in-oil-in-water (W / O / W) or oil-in-water-in-oil (O / W / O), a hydrodispersion or lipodispersion, a gel, a solid stick or an aerosol.
Erfindungsgemäße Emulsionen im Sinne der vorliegenden Erfindung, z.B. in Form einer Creme, einer Lotion, einer kosmetischen Milch sind vorteilhaft und enthalten z.B. Fette, Öle, Wachse und/oder andere Fettkörper, sowie Wasser und einen oder mehrere Emulgatoren, wie sie üblicherweise für einen solchen Typ der Formulierung verwendet werden.Emulsions according to the invention in the sense of the present invention, e.g. in the form of a cream, a lotion, a cosmetic milk are advantageous and contain e.g. Fats, oils, waxes and / or other fat bodies, as well as water and one or more emulsifiers, as are usually used for such a type of formulation.
Es ist auch möglich und vorteilhaft im Sinne der vorliegenden Erfindung, den erfindungsge- maß verwendeten Wirkstoff in wässrige Systeme bzw. Tensidzubereitungen zur Reinigung der Haut und der Haare einzufügen.For the purposes of the present invention, it is also possible and advantageous to insert the active ingredient used according to the invention into aqueous systems or surfactant preparations for cleaning the skin and hair.
Es ist dem Fachmanne natürlich bekannt, dass anspruchsvolle kosmetische Zusammensetzungen zumeist nicht ohne die üblichen Hilfs- und Zusatzstoffe denkbar sind. Die erfin- dungsgemäßen kosmetischen Zubereitungen können daher kosmetische Hilfsstoffe enthalten, wie sie üblicherweise in solchen Zubereitungen verwendet werden, z.B. Konservierungsmittel, Bakterizide, desodorierend wirkende Substanzen, Antitranspirantien, Insektenrepel- lentien, Vitamine, Mittel zum Verhindern des Schäumens, Farbstoffe, Pigmente mit färbender Wirkung, Verdickungsmittel, weichmachende Substanzen, anfeuchtende und/oder feuchthaltende Substanzen, Fette, Öle, Wachse oder andere übliche Bestandteile einer kosmetischen Formulierung wie Alkohole, Polyole, Polymere, Schaumstabilisatoren, Elektrolyte, organische Lösungsmittel oder Silikonderivate.It is of course known to the person skilled in the art that sophisticated cosmetic compositions are usually inconceivable without the customary auxiliaries and additives. The cosmetic preparations according to the invention can therefore contain cosmetic auxiliaries as are usually used in such preparations, e.g. Preservatives, bactericides, deodorising substances, antiperspirants, insect repellents, vitamins, anti-foaming agents, dyes, pigments with a coloring effect, thickeners, softening substances, moisturizing and / or moisturizing substances, fats, oils, waxes or other common components a cosmetic formulation such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
Mutatis mutandis gelten entsprechende Anforderungen an die Formulierung medizinischer Zubereitungen.Mutatis mutandis, corresponding requirements apply to the formulation of medical Preparations.
Medizinische topische Zusammensetzungen im Sinne der vorliegenden Erfindung enthalten in d er Regel ein oder m ehrere Medikamente i n wirksamer Konzentration. D er E infachheit halber wird zur sauberen Unterscheidung zwischen kosmetischer und medizinischer Anwendung und entsprechenden Produkten auf die gesetzlichen Bestimmungen der Bundesrepublik Deutschland verwiesen (z.B. Kosmetikverordnung, Lebensmittel- und Arzneimittelgesetz).Medical topical compositions within the meaning of the present invention generally contain one or more medicaments in an effective concentration. For the sake of simplicity, reference is made to the legal provisions of the Federal Republic of Germany (e.g. cosmetics regulation, food and drug law) for a clear distinction between cosmetic and medical use and corresponding products.
Vorteilhaft können erfindungsgemäße Zubereitungen außerdem Substanzen enthalten, die UV-Strahlung im UVB-Bereich absorbieren, wobei die Gesamtmenge der Filtersubstanzen z.B. 0,1 Gew.-% bis 30 Gew.-%, vorzugsweise 0,5 bis 10 Gew.-%,. insbesondere 1,0 bis 6,0 Gew.-% beträgt, bezogen auf das Gesamtgewicht der Zubereitungen, um kosmetische Zubereitungen zur Verfügung zu stellen, die das Haar bzw. die Haut vor dem gesamten Be- reich der ultravioletten Strahlung schützen. Sie können auch als Sonnenschutzmittel fürs Haar dienen.Preparations according to the invention can also advantageously contain substances which absorb UV radiation in the UVB range, the total amount of filter substances e.g. 0.1% by weight to 30% by weight, preferably 0.5 to 10% by weight. is in particular 1.0 to 6.0% by weight, based on the total weight of the preparations, in order to provide cosmetic preparations which protect the hair or the skin from the entire range of ultraviolet radiation. They can also serve as a sunscreen for the hair.
Enthalten die erfindungsgemäßen Zubereitungen UVB-Filtersubstanzen, können diese öl- löslich oder wasserlöslich sein. Erfindungsgemäß vorteilhafte öllösliche UVB-Filter sind z.B.: - 3-Benzylidencampher-Derivate, vorzugsweise 3-(4-Methylbenzyliden)campher, 3- Benzylidencampher; 4-Aminobenzoesäure-Derivate, vorzugsweise 4-(Dimethylamino)-benzoesäure(2-ethyl- hexyl)ester, 4-(Dimethylamino)benzoesäureamylester; Ester der Zimtsäure, vorzugsweise 4-Methoxyzimtsäure(2-ethylhexyl)ester, 4-Methoxy- zimtsäureisopentylester; Ester der Salicylsäure, vorzugsweise Salicylsäure(2-ethylhexyl)ester, Salicylsäure(4- isopropylbenzyl)ester, Salicylsäurehomomenthylester, Derivate des Benzophenons, vorzugsweise 2-Hydroxy-4-methoxybenzophenon, 2-Hy- droxy-4-methoxy-4'-methylbenzophenon, 2,2'-Dihydroxy-4-methoxybenzophenon; - Ester der Benzalmalonsäure, vorzugsweise 4-Methoxybenzalmalonsäuredi(2-ethylhe- xyl)ester, 2,4,6-Trianilino-(p-carbo-2'-ethyl-1'-hexyloxy)-1 ,3,5-triazin.If the preparations according to the invention contain UVB filter substances, they can be oil-soluble or water-soluble. Oil-soluble UVB filters which are advantageous according to the invention are, for example: 3-benzylidene camphor derivatives, preferably 3- (4-methylbenzylidene) camphor, 3-benzylidene camphor; 4-aminobenzoic acid derivatives, preferably 4- (dimethylamino) benzoic acid (2-ethyl-hexyl) ester, 4- (dimethylamino) benzoic acid amyl ester; Esters of cinnamic acid, preferably 4-methoxycinnamic acid (2-ethylhexyl) ester, 4-methoxycinnamic acid isopentyl ester; Esters of salicylic acid, preferably salicylic acid (2-ethylhexyl) ester, salicylic acid (4-isopropylbenzyl) ester, salicylic acid homomethyl ester, derivatives of benzophenone, preferably 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone , 2,2'-dihydroxy-4-methoxybenzophenone; - Esters of benzalmalonic acid, preferably 4-methoxybenzalmalonic acid di (2-ethylhexyl) ester, 2,4,6-trianilino- (p-carbo-2'-ethyl-1'-hexyloxy) -1, 3,5-triazine.
Vorteilhafte wasserlösliche UVB-Filter sind z.B.: Salze der 2-Phenylbenzimidazol-5-sulfonsäure wie ihr Natrium-, Kalium- oder ihr Tri- ethanolammonium-Salz, sowie die Sulfonsäure selbst; Sulfonsäure-Derivate von Benzophenonen, vorzugsweise 2-Hydroxy-4-methoxybenzo- phenon-5-sulfonsäure und ihre Salze; Sulfonsäure-Derivate des 3-Benzylidencamphers, wie z.B. 4-(2-Oxo-3-bomyliden- methyl)benzolsulfonsäure, 2-Methyl-5-(2-oxo-3-bomylidenmethyl)sulfonsäure und ihre Salze sowie das 1 ,4-di(2-oxo-10-Sulfo-3-bornylidenmethyl)-Benzol u nd dessen Salze (die entprehenden 10-Sulfato-verbindungen, beispielsweise das entsprechende Natri- um-, Kalium- oder Triethanolammonium-Salz), auch als Benzol-1 ,4-di(2-oxo-3-bornyli- denmethyl-10-Sulfonsäure bezeichnetExamples of advantageous water-soluble UVB filters are: Salts of 2-phenylbenzimidazole-5-sulfonic acid such as its sodium, potassium or triethanolammonium salt, and also the sulfonic acid itself; Sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and its salts; Sulfonic acid derivatives of 3-benzylidene camphor, such as 4- (2-oxo-3-bomylidene-methyl) benzenesulfonic acid, 2-methyl-5- (2-oxo-3-bomylidene-methyl) sulfonic acid and their salts and 1,4- di (2-oxo-10-sulfo-3-bornylidenemethyl) -benzene and its salts (the corresponding 10-sulfato compounds, for example the corresponding sodium, potassium or triethanolammonium salt), also as benzene-1 , 4-di (2-oxo-3-bornylidenemethyl-10-sulfonic acid)
Die Liste der genannten UVB-Filter, die in Kombination mit den erfindungsgemäßen Wirk- stoffkombinationen verwendet werden können, soll selbstverständlich nicht limitierend sein.The list of UVB filters mentioned, which can be used in combination with the active compound combinations according to the invention, is of course not intended to be limiting.
Es kann auch von Vorteil sein, UVA-Filter einzusetzen, die üblicherweise in kosmetischen Zubereitungen enthalten sind. Bei diesen Substanzen handelt es sich vorzugsweise um Derivate d es Dibenzoylmethans, i nsbesondere u m 1-(4'-tert.Butylphenyl)-3-(4'-methoxyphenyl)- propan-1 ,3-dion und um 1-Phenyl-3-(4'-isopropylphenyl)propan-1 ,3-dion. Es können die für die UVB-Kombination verwendeten Mengen eingesetzt werden.It can also be advantageous to use UVA filters that are usually contained in cosmetic preparations. These substances are preferably derivatives of dibenzoylmethane, in particular 1- (4'-tert-butylphenyl) -3- (4'-methoxyphenyl) propane-1, 3-dione and 1-phenyl-3 - (4'-Isopropylphenyl) propane-1,3-dione. The quantities used for the UVB combination can be used.
Erfindungsgemäße kosmetische und dermatologische Zubereitungen enthalten vorteilhaft außerdem anorganische Pigmente auf Basis von Metalloxiden und/oder anderen in Wasser schwerlöslichen oder unlöslichen Metallverbindungen, insbesondere der Oxide des Titans (Ti02), Zinks (ZnO), Eisens (z.B. Fe203), Zirkoniums (Zr02), Siliciums (Si02), Mangans (z.B. MnO), Aluminiums (Al203), Cers (z.B. Ce203), Mischoxiden der entsprechenden Metalle sowie Abmischungen aus solchen Oxiden. Besonders bevorzugt handelt es sich um Pigmente auf der Basis von Ti02.Cosmetic and dermatological preparations according to the invention advantageously also contain inorganic pigments based on metal oxides and / or other metal compounds which are sparingly soluble or insoluble in water, in particular the oxides of titanium (Ti0 2 ), zinc (ZnO), iron (eg Fe 2 0 3 ), zirconium (Zr0 2 ), silicon (Si0 2 ), manganese (eg MnO), aluminum (Al 2 0 3 ), cerium (eg Ce 2 0 3 ), mixed oxides of the corresponding metals and mixtures of such oxides. It is particularly preferably pigments based on TiO 2 .
Es ist besonders vorteilhaft im Sinne der vorliegenden Erfindung, wenngleich nicht zwingend, wenn die anorganischen Pigmente in hydrophober Form vorliegen, d.h., dass sie oberflächlich wasserabweisend behandelt sind. Diese Oberflächenbehandlung kann darin bestehen, dass die Pigmente nach an sich bekannten Verfahren mit einer dünnen hydrophoben Schicht versehen werden. Eines solcher Verfahren besteht beispielsweise darin, dass die hydrophobe Oberflächenschicht nach einer Rektion gemäßFor the purposes of the present invention, it is particularly advantageous, although not essential, if the inorganic pigments are in hydrophobic form, ie that they have been treated to be water-repellent on the surface. This surface treatment can consist in that the pigments are provided with a thin hydrophobic layer by methods known per se. Such a method consists, for example, in that the hydrophobic surface layer according to a direction
n Ti02+ m (RO)3 Si-R' -> n Ti02 (oberfl.)n Ti0 2 + m (RO) 3 Si-R '-> n Ti0 2 (surface)
erzeugt wird, n und m sind dabei nach Belieben einzusetzende stöchiometrische Parameter, R und R' die gewünschten organischen Reste. Beispielsweise in Analogie zu DE-OS 33 14 742 dargestellte hydrophobisierte Pigmente sind von Vorteil.is generated, n and m are stoichiometric parameters to be used at will, R and R 'are the desired organic radicals. For example, hydrophobized pigments shown in analogy to DE-OS 33 14 742 are advantageous.
Vorteilhafte Ti02-Pigmente sind beispielsweise unter den Handelsbezeichnungen MT 100 T von der Firma TAYCA, ferner M 160 von der Firma Kemira sowie T 805 von der Firma Degussa erhältlich.Advantageous Ti0 2 pigments are available, for example, under the trade names MT 100 T from TAYCA, M 160 from Kemira and T 805 from Degussa.
Erfindungsgemäße Zubereitungen können, zumal wenn kristalline oder mikrokristalline Festkörper, beispielsweise anorganische Mikropigmente in die erfindungsgemäßen Zubereitungen eingearbeitet werden sollen, auch anionische, nichtionische und/oder amphotere Tenside enthalten. Tenside sind amphiphile Stoffe, die organische, unpolare Substanzen in Wasser lösen können.Preparations according to the invention can also contain anionic, nonionic and / or amphoteric surfactants, especially if crystalline or microcrystalline solids, for example inorganic micropigments, are to be incorporated into the preparations according to the invention. Surfactants are amphiphilic substances that can dissolve organic, non-polar substances in water.
Bei den hydrophilen Anteilen eines Tensidmoleküls handelt es sich meist um polare funktionelle Gruppen, beispielsweise -COO", -OS03 2", -S03 ", während die hydrophoben Teile in der Regel unpolare Kohlenwasserstoffreste darstellen. Tenside werden im allgemeinen nach Art und Ladung des hydrophilen Molekülteils klassifiziert. Hierbei können vier Gruppen un- terschieden- werden:The hydrophilic parts of a surfactant molecule are mostly polar functional groups, for example -COO " , -OS0 3 2" , -S0 3 " , while the hydrophobic parts generally represent non-polar hydrocarbon residues. Surfactants are generally of type and charge of the hydrophilic part of the molecule. Four groups can be distinguished here:
• anionische Tenside,Anionic surfactants,
• kationische Tenside,Cationic surfactants,
• amphotere Tenside und • nichtionische Tenside.• amphoteric surfactants and • 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 Milieu negativ geladene organische Ionen. Kationische Tenside sind beinahe ausschließlich durch das Vorhandensein einer quatemären Ammoniumgruppe gekennzeichnet. In wässriger Lösung bilden sie i m sauren o der neutralen Milieu positiv geladene organische Ionen. Amphotere Tenside enthalten sowohl anionische als auch kationische Gruppen und verhalten sich demnach in wässriger Lösung je nach pH-Wert wie anionische oder kationische Tenside. Im stark sauren M ilieu besitzen s ie e ine 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 an acidic or neutral environment. Cationic surfactants are almost exclusively due to that Labeled presence of a quaternary ammonium group. In aqueous solution, they form positively charged organic ions in an acid or neutral environment. Amphoteric surfactants contain both anionic and cationic groups and accordingly behave in aqueous solution like anionic or cationic surfactants depending on the pH. They have a positive charge in a strongly acidic environment and a negative charge in an alkaline environment. In the neutral pH range, however, they are zwitterionic, as the following example should illustrate:
RNH2 +CH2CH2COOH X" (bei pH=2) X" = beliebiges Anion, z.B. Cf RNH2 +CH2CH2COO" (bei pH=7)RNH 2 + CH 2 CH 2 COOH X " (at pH = 2) X " = any anion, e.g. Cf RNH 2 + CH 2 CH 2 COO " (at pH = 7)
RNHCH2CH2COO_ B+ (bei pH=12) B+ = beliebiges Kation, z.B. Na+ RNHCH 2 CH 2 COO _ B + (at pH = 12) B + = any cation, e.g. Na +
Typisch für nicht-ionische Tenside s ind Polyether-Ketten. N icht-ionische Tenside b ilden i n wässrigem Medium keine Ionen.Typical of non-ionic surfactants and polyether chains. Non-ionic surfactants do not form ions in an aqueous medium.
A. Anionische TensideA. Anionic surfactants
Vorteilhaft zu verwendende anionische Tenside sindAnionic surfactants to be used advantageously
Acylaminosäuren (und deren Salze), wieAcylamino acids (and their salts), such as
1. Acylglutamate, beispielsweise Natriumacylglutamat, Di-TEA-palmitoylaspartat und Na- trium Caprylic/ Capric Glutamat,1. acylglutamates, for example sodium acylglutamate, di-TEA-palmitoylaspartate and sodium caprylic / capric glutamate,
2. Acylpeptide, beispielsweise Palmitoyl-hydrolysiertes Milchprotein, Natrium Cocoyl- hydrolysiertes Soja Protein und Natrium-/ Kalium Cocoyl-hydrolysiertes Kollagen,2. acyl peptides, for example palmitoyl-hydrolyzed milk protein, sodium cocoyl-hydrolyzed soy protein and sodium / potassium cocoyl-hydrolyzed collagen,
3. Sarcosinate, beispielsweise Myristoyl Sarcosin, TEA-Iauroyl Sarcosinat, Natrium- lauroylsarcosinat und Natriumcocoylsarkosinat, 4. Taurate, beispielsweise Natriumlauroyltaurat und Natriummethylcocoyltaurat,3. sarcosinates, for example myristoyl sarcosin, TEA-lauroyl sarcosinate, sodium lauroyl sarcosinate and sodium cocoyl sarcosinate, 4. taurates, for example sodium lauroyl taurate and sodium methyl cocoyl taurate,
5. AcylLactylate, lauroyllactylat, Caproyliactylat5. Acyl lactylate, lauroyl lactylate, caproyl octylate
6. Alaninate Carbonsäuren und Derivate, wie6. Alaninate carboxylic acids and derivatives, such as
1. Carbonsäuren, beispielsweise Laurinsäure, Aluminiumstearat, Magnesiumalkänolat und Zinkundecylenat,1. carboxylic acids, for example lauric acid, aluminum stearate, magnesium alkenolate 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 Dilaureth-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 dilaureth-4-phosphate,
Sulfonsäuren und Salze, wieSulfonic acids and salts such as
1. Acyl-isethionate, z.B. Natrium-/ Ammoniumcocoyl-isethionat,1. acyl isethionates, e.g. Sodium / ammonium cocoyl isethionate,
2. Alkylarylsulfonate,2. alkylarylsulfonates,
3. Alkylsulfonate, beispielsweise Natriumcocosmonoglyceridsulfat, Natrium C12-1 Olefin- sulfonat, Natriumlaurylsulfoacetat und Magnesium PEG-3 Cocamidsulfat, 4. Sulfosuccinate, beispielsweise Dioctylnathumsulfosuccinat, Dinatriumlaurethsulfosuc- cinat, Dinatriumlaurylsulfosuccinat und Dinatriumundecylenamido MEA-Sulfosuccinat3. alkyl sulfonates, for example sodium cocosmonoglyceride sulfate, sodium C 12-1 olefin sulfonate, sodium lauryl sulfoacetate and magnesium PEG-3 cocamide sulfate, 4. sulfosuccinates, for example dioctyl sodium sulfosuccinate, disodium laureth sulfosuccinate, disodium lauryl sulfyl succinate sulfosuccinate aminosulfinate sulfosuccinate aminosulfinate sulfosuccinate disodium aminosulfinate sulfate succinate disodium aminosulfinate sulfate succinate disodium aminosulfinate sulfate succinate disulfate and
sowiesuch as
Schwefelsäureester, wie 1. Alkylethersulfat, beispielsweise Natrium-, Ammonium-, Magnesium-, MIPA-, TIPA- Laurethsulfat, Natriummyrethsulfat und Natrium C12-13 Parethsulfat, 2. Alkylsulfate, beispielsweise Natrium-, Ammonium- und TEA- Laurylsulfat.Schwefelsäureester as 1. alkyl ether sulfate, for example sodium, ammonium, magnesium, MIPA, TIPA laureth sulfate, sodium and sodium C12 - 1 3 pareth, 2. alkyl sulfates, for example sodium, ammonium and TEA lauryl sulfate.
B. Kationische Tenside Vorteilhaft zu verwendende kationische Tenside sindB. Cationic Surfactants Cationic surfactants to be used advantageously are
1. Alkylamine,1. alkylamines,
2. Alkylimidazole,2. alkylimidazoles,
3. Ethoxylierte Amine und3. Ethoxylated amines and
4. Quatemäre Tenside. 5. Esterquats4. Quaternary surfactants. 5. Esterquats
Quaternäre Tenside enthalten mindestens ein N -Atom, d as m it 4 Alkyl- oder Arylgruppen kovaient verbunden ist. Dies führt, unabhängig vom pH Wert, zu einer positiven Ladung. Vorteilhaft sind, Alkylbetain, Alkylamidopropylbetain und Alkyl-amidopropylhydroxysulfain. Die erfindungsgemäß verwendeten kationischen Tenside können ferner bevorzugt gewählt werden aus der Gruppe der quaternären Ammoniumverbindungen, insbesondere Ben- zyltrialkylammoniumchloride oder -bromide, wie beispielsweise Benzyldimethylstea- rylammoniumchlorid, ferner Alkyltrialkylammoniumsalze, beispielsweise beispielsweise Ce- tyltrimethylammoniumchlorid oder -bromid, Alkyldimethylhydroxyethylammoniumchloride oder -bromide, Dialkyldimethylammoniumchloride oder -bromide, Alkylamidethyltrimethylam- moniumethersulfate, Alkylpyridiniumsalze, beispielsweise Lauryl- oder Cetylpyrimidinium- chlorid, Imidazolinderivate und Verbindungen mit kationischem Charakter wie Aminoxide, beispielsweise Alkyldimethylaminoxide oder Alkylaminoethyldimethylaminoxide. Vorteilhaft sind insbesondere Cetylt methylammoniumsalze zu verwenden.Quaternary surfactants contain at least one N atom which is covalently bonded to 4 alkyl or aryl groups. Regardless of the pH value, this leads to a positive charge. Alkyl betaine, alkyl amidopropyl betaine and alkyl amidopropyl hydroxysulfain are advantageous. The cationic surfactants used in the invention can be also preferably selected from the group of quaternary ammonium compounds, in particular benzene zyltrialkylammoniumchloride or bromides, such as Benzyldimethylstea- rylammoniumchlorid, also alkyltrialkylammonium, such as for example Ce tyltrimethylammoniumchlorid or bromide, alkyldimethylhydroxyethylammonium chlorides or bromides, dialkyldimethylammonium chlorides or -bromides, alkylamidethyltrimethylam- monium ether sulfates, alkylpyridinium salts, for example lauryl or cetylpyrimidinium chloride, imidazoline derivatives and compounds with a cationic character such as amine oxides, for example alkyldimethylamine oxides or alkylaminoethyldimethylamine oxides. Cetylt methylammonium salts are particularly advantageous.
C. Amphotere TensideC. Amphoteric surfactants
Vorteilhaft zu verwendende amphotere Tenside sindAmphoteric surfactants to be used advantageously
1. Acyl-/dialkylethylendiamin, beispielsweise Natriumacylamphoacetat, Dinatriumacyl- amphodipropionat, Dinatriumalkylamphodiacetat, Natriumacylamphohydroxypropylsul- fonat, Dinatriumacylamphodiacetat und Natriumacylamphopropionat,1. acyl / dialkyl ethylenediamine, for example sodium acyl amphoacetate, disodium acyl amphodipropionate, disodium alkyl amphodiacetate, sodium acylamphohydroxypropyl sulfonate, disodium acylamphodiacetate and sodium acylamphopropionate,
2. N-Alkylaminosäuren, beispielsweise Aminopropylalkylglutamid, Alkylaminopropion- säure, Natriumalkylimidodipropionat und Lauroamphocarboxyglycinat.2. N-alkylamino acids, for example aminopropylalkylglutamide, alkylaminopropionic acid, sodium alkylimidodipropionate and lauroamphocarboxyglycinate.
D. Nicht-ionische Tenside Vorteilhaft zu verwendende nicht-ionische Tenside sindD. Non-ionic surfactants are non-ionic surfactants that can be used advantageously
1. Alkohole,1. alcohols,
2. Alkanolamide, wie Cocamide MEA/ DEA/ MIPA,2. alkanolamides, such as cocamides MEA / DEA / MIPA,
3. Aminoxide, wie Cocoamidopropylaminoxid,3. amine oxides, such as cocoamidopropylamine oxide,
4. Ester, die durch Veresterung von Carbonsäuren mit Ethylenoxid, Glycerin, Sorbitan oder anderen Alkoholen entstehen,4. esters which are formed by esterification of carboxylic acids with ethylene oxide, glycerol, sorbitan or other alcohols,
5. Ether, beispielsweise ethoxylierte/propoxylierte Alkohole, ethoxylierte/ propoxylierte Ester, ethoxylierte/ propoxylierte Glycerinester, ethoxylierte/ propoxylierte Cholesterine, ethoxylierte/ propoxylierte Triglyceridester, ethoxyliertes propoxyliertes Lanolin, ethoxylierte/ propoxylierte Polysiloxane, propoxylierte POE-Ether und Alkylpolyglycoside wie Laurylglucosid, Decylglycosid und Cocoglycosid.5. ethers, for example ethoxylated / propoxylated alcohols, ethoxylated / propoxylated esters, ethoxylated / propoxylated glycerol esters, ethoxylated / propoxylated cholesterols, ethoxylated / propoxylated triglyceride esters, ethoxylated propoxylated lanolin, ethoxylated / propoxylated polysiloxanes, propoxylated POE ethers and alkylpolyglycosides such as lauryl polyglycosides cocoglycoside.
6. Sucroseester, -Ether6. sucrose esters, ether
7 Polyglycerioester, Diglycerinester, Monoglycerinester 8. Methylglucosester, Ester von Hydroxysäuren7 polyglycerio esters, diglycerol esters, monoglycerol esters 8. methyl glucose esters, esters of hydroxy acids
Vorteilhaft ist ferner die Verwendung einer Kombination von anionischen und/oder ampho- teren Tensiden mit einem oder mehreren nicht-ionischen Tensiden. Die oberflächenaktive Substanz kann in einer Konzentration zwischen 1 und 95 Gew.-% in den erfindungsgemäßen Zubereitungen vorliegen, bezogen auf das Gesamtgewicht der Zubereitungen.It is also advantageous to use a combination of anionic and / or amphoteric surfactants with one or more nonionic surfactants. The surface-active substance can be present in the preparations according to the invention in a concentration between 1 and 95% by weight, based on the total weight of the preparations.
Die Lipidphase der erfindungsgemäßen kosmetischen oder dermatologischen Emulsionen kann vorteilhaft gewählt werden aus folgender Substanzgruppe: Mineralöle, Mineralwächse Öle, wie Triglyceride der Caprin- oder der Caprylsäure, ferner natürliche Öle wie z.B. Rizinusöl; - Fette, Wachse und andere natürliche und synthetische Fettkörper, vorzugsweise Ester von Fettsäuren mit Alkoholen niedriger C-Zahl, z.B. mit Isopropanol, Propylen- glykol oder Glycerin, oder Ester von Fettalkoholen mit Alkansäuren niedriger C-Zahl oder mit Fettsäuren; Alkylbenzoate; - Silikonöle wie Dimethylpolysiloxane, Diethylpolysiloxane, Diphenylpolysiloxane sowie Mischformen daraus.The lipid phase of the cosmetic or dermatological emulsions according to the invention can advantageously be selected from the following group of substances: mineral oils, mineral wax oils, such as triglycerides of capric or caprylic acid, and also natural oils such as e.g. Castor oil; Fats, waxes and other natural and synthetic fat bodies, preferably esters of fatty acids with alcohols of low C number, e.g. with isopropanol, propylene glycol or glycerin, or esters of fatty alcohols with low C number alkanoic acids or with fatty acids; benzoates; - Silicone oils such as dimethylpolysiloxanes, diethylpolysiloxanes, diphenylpolysiloxanes and mixed forms thereof.
Die Ölphase der Emulsionen der vorliegenden Erfindung wird vorteilhaft gewählt aus der Gruppe der Ester aus gesättigten und/oder ungesättigten, verzweigten und/oder unverzweig- ten Alkancarbonsäuren einer Kettenlänge von 3 bis 30 C-Atomen und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C-Atomen, aus der Gruppe der Ester aus aromatischen Carbonsäuren und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C-Atomen. Solche Esteröle können dann vorteilhaft gewählt werden aus der Gruppe Isopropylmyristat, Isopropylpalmitat, Isopropylstearat, Isopropyloleat, n-Butylstearat, n-Hexyllaurat, n-Decyloleat, Isooctylstearat, Isononyistearat, Isononylisononanoat, 2- Ethylhexylpalmitat, 2-Ethylhexyllaurat, 2-Hexyldecylstearat, 2-Octyldodecylpalmitat, Oleyl- oleat, Oleylerucat, Erucyloleat, Erucylerucat sowie synthetische, halbsynthetische und natürliche Gemische solcher Ester, z.B. Jojobaöl.The oil phase of the emulsions of the present invention is advantageously selected from the group of the esters from saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 3 to 30 carbon atoms and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 to 30 C atoms, from the group of esters of aromatic carboxylic acids and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 to 30 C atoms. Such ester oils can then advantageously be selected from the group of isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyistearate, isononylisononanoate, 2-ethylhexyl-2-ethylhexyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethyl-2-ethylhexyl-2-ethyl-2-ethyl-2-ethylhexyl-2-ethyl-2-ethyl-2-ethyl-2-ethylhexyl-2-ethyl-2-ethylhexyl-2-ethyl-2-ethylhexyl Octyldodecyl palmitate, oleyl oleate, olerlerucate, erucyl oleate, erucylerucate as well as synthetic, semisynthetic and natural mixtures of such esters, for example Jojoba oil.
Ferner kann die Ölphase vorteilhaft gewählt werden aus der Gruppe der verzweigten und unverzweigten Kohlenwasserstoffe und -wachse, der Silkonöle, der Dialkylether, der Gruppe der gesättigten oder ungesättigten, verzweigten oder unverzweigten Alkohole, sowie der Fettsäuretriglyceride, namentlich der Triglycerinester gesättigter und/oder ungesättigter, ver- zweigter und/oder unverzweigter Alkancarbonsäuren einer Kettenlänge von 8 bis 24, insbesondere 12 - 18 C-Atomen. Die Fettsäuretriglyceride können beispielsweise vorteilhaft gewählt werden aus der Gruppe der synthetischen, halbsynthetischen und natürlichen Öle, z.B. Olivenöl, Sonnenblumenöl, Sojaöl, Erdnußöl, Rapsöl, Mandelöl, Palmöl, Kokosöl, Palm- kernöl und dergleichen mehr.Furthermore, the oil phase can advantageously be selected from the group of branched and unbranched hydrocarbons and waxes, the silicone oils, the dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols, and also the fatty acid triglycerides, especially the triglycerol esters of saturated and / or unsaturated, comparable branched and / or unbranched alkane carboxylic acids with a chain length of 8 to 24, in particular 12 - 18 carbon atoms. The fatty acid triglycerides can, for example, advantageously be selected from the group of synthetic, semisynthetic and natural oils, for example olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm kernel oil and the like.
Auch beliebige Abmischungen solcher Öl- und Wachskomponenten sind vorteilhaft im Sinne der vorliegenden Erfindung einzusetzen. Es kann auch gegebenenfalls vorteilhaft sein, Wachse, beispielsweise Cetylpalmitat, als alleinige Lipidkomponente der Ölphase einzuset- zen.Any mixtures of such oil and wax components can also be used advantageously for the purposes of the present invention. It may also be advantageous, where appropriate, to use waxes, for example cetyl palmitate, as the sole lipid component of the oil phase.
Vorteilhaft wird die Ölphase gewählt aus der Gruppe 2-Ethylhexylisostearat, Octyldodecanol, Isotridecylisononanoat, Isoeicosan, 2-Ethylhexylcocoat, Cι2-ι5-Alkylbenzoat, Capryl-Caprin- säu re-trig lycerid , Dicaprylylether.The oil phase is advantageously selected from the group 2-ethylhexyl isostearate, octyldodecanol, isotridecylisononanoate, isoeicosane, 2-ethylhexyl cocoate, Cι 2- ι 5 alkyl benzoate, caprylic capric acid re-trig lyceride, dicaprylyl ether.
Besonders vorteilhaft sind Mischungen aus C12. 5-Alkylbenzoat und 2-Ethylhexylisostearat, Mischungen aus Cι2-15-Alkylbenzoat und Isotridecylisononanoat sowie Mischungen aus C1 . 15-Alkylbenzoat, 2-Ethylhexylisostearat und Isotridecylisononanoat.Mixtures of C 12 are particularly advantageous. 5 alkyl benzoate and 2-ethylhexyl isostearate, mixtures of C 2-15 alkyl benzoate and isotridecyl isononanoate and mixtures of C 1 . 15 alkyl benzoate, 2-ethylhexyl isostearate and isotridecyl isononanoate.
Von den Kohlenwasserstoffen sind Paraffinöl, Squalan und Squalen vorteilhaft im Sinne der vorliegenden Erfindung zu verwenden.Of the hydrocarbons, paraffin oil, squalane and squalene can be used advantageously for the purposes of the present invention.
Vorteilhaft kann die Ölphase ferner einen Gehalt an cyclischen oder linearen Silikonölen aufweisen oder vollständig aus solchen Ölen bestehen, wobei allerdings bevorzugt wird, außer dem Silikonöl oder den Siiikonölen einen zusätzlichen Gehalt an anderen Ölphasenkom- ponenten zu verwenden. Solche Silicone oder Siliconöle können als Monomere vorliegen, welche in der Regel durch Strukturelemente charakterisiert sind, wie folgt:The oil phase can advantageously also have a content of cyclic or linear silicone oils or consist entirely of such oils, although it is preferred to use an additional content of other oil phase components in addition to the silicone oil or the silicone oils. Such silicones or silicone oils can be present as monomers, which are generally characterized by structural elements, as follows:
Als erfindungsgemäß vorteilhaft einzusetzenden linearen Silicone mit mehreren Siloxyl- einheiten werden im allgemeinen durch Strukturelemente charakterisiert wie folgt: wobei die Siliciumatome mit gleichen oder unterschiedlichen Alkylresten und/oder Arylresten substituiert werden können, welche ήier verallgemeinernd durch die Reste R1 - R4 dargestellt sind (will sagen, dass die Anzahl der unterschiedlichen Reste nicht notwendig auf bis zu 4 beschränkt ist), m kann dabei Werte von 2 - 200.000 annehmen.Linear silicones with a plurality of siloxyl units which can advantageously be used according to the invention are generally characterized by structural elements as follows: wherein the silicon atoms can be substituted with the same or different alkyl radicals and / or aryl radicals, which are generally represented by the radicals R 1 - R 4 (to say that the number of different radicals is not necessarily limited to up to 4), m can assume values from 2 - 200,000.
Erfindungsgemäß vorteilhaft einzusetzende cyclische Silicone werden im allgemeinen durch Strukturelemente charakterisiert, wie folgtCyclic silicones to be used advantageously according to the invention are generally characterized by structural elements as follows
wobei die Siliciumatome mit gleichen oder unterschiedlichen Alkylresten und/oder Arylresten substituiert werden können, welche hier verallgemeinernd durch die Reste R1 - R dargestellt sind (will sagen, dass die Anzahl der unterschiedlichen Reste nicht notwendig auf bis zu 4 beschränkt ist), n kann dabei Werte von 3/2 bis 20 annehmen. Gebrochene Werte für n berücksichtigen, dass ungeradzahlige Anzahlen von Siloxylgruppen im Cyclus vorhanden sein können. wherein the silicon atoms can be substituted with the same or different alkyl radicals and / or aryl radicals, which are generally represented here by the radicals R 1 - R (to say that the number of different radicals is not necessarily limited to up to 4), n assume values from 3/2 to 20. Broken values for n take into account that there may be odd numbers of siloxyl groups in the cycle.
Vorteilhaft wird Cyclomethicon (z.B. Decamethylcyclopentasiloxan) als erfindungsgemäß zu verwendendes Silikonöl eingesetzt. Aber auch andere Silikonöle sind vorteilhaft im Sinne der vorliegenden E rfindung zu verwenden, beispielsweise Undecamethylcyclotrisiloxan, Polydi- methylsiloxan, Poly(methylphenylsiloxan), Cetyldimethicon, Behenoxydimethicon.Cyclomethicone (e.g. decamethylcyclopentasiloxane) is advantageously used as the silicone oil to be used according to the invention. However, other silicone oils can also be used advantageously for the purposes of the present invention, for example undecamethylcyclotrisiloxane, polydimethylsiloxane, poly (methylphenylsiloxane), cetyldimethicone, behenoxydimethicone.
Vorteilhaft sind ferner Mischungen aus Cyclomethicon und Isotridecylisononanoat, sowie solche aus Cyclomethicon und 2-Ethylhexylisostearat. Es ist aber auch vorteilhaft, Silikonöle ähnlicher Konstitution wie der v orstehend b ezeich- neten Verbindungen zu wählen, deren organische Seitenketten derivatisiert, beispielsweise polyethoxyliert und/oder polypropoxyliert sind. Dazu zählen beispielsweise Polysiloxan- polyalkyl-polyether-copolymere wie das Cetyl-Dimethicon-Copolyol, das (Cetyl-Dimethicon- Copolyol (und) Polyglyceryl-4-lsostearat (und) Hexyllaurat)Mixtures of cyclomethicone and isotridecyl isononanoate and those of cyclomethicone and 2-ethylhexyl isostearate are also advantageous. However, it is also advantageous to choose silicone oils of a constitution similar to the above-mentioned compounds, the organic side chains of which are derivatized, for example polyethoxylated and / or polypropoxylated. These include, for example, polysiloxane-polyalkyl-polyether copolymers such as the cetyl-dimethicone copolyol, the (cetyl-dimethicone copolyol (and) polyglyceryl-4-isostearate (and) hexyl laurate)
Besonders vorteilhaft sind ferner Mischungen aus Cyclomethicon und Isotridecylisononanoat, aus Cyclomethicon und 2-Ethylhexylisostearat.Mixtures of cyclomethicone and isotridecyl isononanoate, cyclomethicone and 2-ethylhexyl isostearate are also particularly advantageous.
Die wässrige Phase der erfindungsgemäßen Zubereitungen enthält gegebenenfalls vorteilhaft Alkohole, Diole oder Polyole niedriger C-Zahl, sowie deren Ether, vorzugsweise Ethanol, Isopropanol, Propylenglykol, Glycerin, Ethylenglykol, Ethylenglykolmonoethyl- oder -mo- nobutylether, Propylenglykolmonomethyl, -monoethyl- oder -monobutylether, Diethy- lenglykolmonomethyl- 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 vorteilhaft gewählt werden können aus der Gruppe Siliciumdioxid, Aluminiumsilikate.The aqueous phase of the preparations according to the invention advantageously advantageously contains alcohols, diols or polyols of low C number, and their ethers, preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether , Diethy- glycol monomethyl or monoethyl ether and analog products, furthermore alcohols of low C number, for example Ethanol, isopropanol, 1, 2-propanediol, glycerol and in particular one or more thickeners, which one or more can advantageously be selected from the group consisting of silicon dioxide and aluminum silicates.
Erfindungsgemäße als Emulsionen vorliegenden Zubereitungen enthalten insbesondere vorteilhaft ein oder mehrere Hydrocolloide. Diese Hydrocolloide können vorteilhaft gewählt werden aus der Gruppe der Gummen, Polysaccharide, Cellulosederivate, Schichtsilikate, Polyacrylate und/oder anderen Polymeren.Preparations according to the invention which are present as emulsions particularly advantageously contain one or more hydrocolloids. These hydrocolloids can advantageously be selected from the group consisting of gums, polysaccharides, cellulose derivatives, layered silicates, polyacrylates and / or other polymers.
Erfindungsgemäße als Hydrogele vorliegenden Zubereitungen enthalten ein oder mehrere Hydrocolloide. Diese Hydrocolloide können vorteilhaft aus der vorgenannten Gruppe gewählt werden.Preparations according to the invention which are present as hydrogels contain one or more hydrocolloids. These hydrocolloids can advantageously be selected from the aforementioned group.
Zu den Gummen zählt man Pflanzen- oder Baumsäfte, die an der Luft erhärten und Harze bilden oder Extrakte aus Wasserpflanzen. Aus dieser Gruppe können vorteilhaft im Sinne der vorliegenden Erfindung gewählt werden beispielsweise Gummi Arabicum, Johannisbrotmehl, Tragacanth, Karaya, Guar Gummi, Pektin, Gellan Gummi, Carrageen, Agar, Algine, Chondrus, Xanthan Gummi. Weiterhin vorteilhaft ist die Verwendung von derivatisierten Gummen wie z.B. Hydroxypropyl Guar (Jaguar® HP 8).Gums include plant or tree sap that harden in the air and form resins or extracts from aquatic plants. Gum arabic, locust bean gum, tragacanth, karaya, guar gum, pectin, gellan gum, carrageenan, agar, algine, chondrus, xanthan gum can advantageously be selected from this group for the purposes of the present invention. The use of derivatized gums such as hydroxypropyl guar (Jaguar® HP 8) is also advantageous.
Unter den Polysacchariden und -derivaten befinden sich z.B. Hyaluronsäure, Chitin und Chitosan, Chondroitinsulfate, Stärke und Stärkederivate.Among the polysaccharides and derivatives are e.g. Hyaluronic acid, chitin and chitosan, chondroitin sulfates, starch and starch derivatives.
Unter den Cellulosederivaten befinden sich z.B. Methylcellulose, Carboxymethylcellulose, Hydroxyethylcellulose, Hydroxypropylmethylcellulose.Among the cellulose derivatives are e.g. Methyl cellulose, carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose.
Unter den Schichtsilikaten befinden sich natürlich vorkommende und synthetische Tonerden wie z.B. Montmorillonit, Bentonit, Hektorit, Laponit, Magnesiumaluminiumsilikate wie Vee- gum®. Diese können als solche oder in modifizierter Form verwendet werden wie z.B. Stea- rylalkonium Hektorite.Layered silicates contain naturally occurring and synthetic clays such as Montmorillonite, bentonite, hectorite, laponite, magnesium aluminum silicates such as Vegegum®. These can be used as such or in a modified form such as e.g. Stearylalkonium hectorite.
Weiterhin können vorteilhaft auch Kieselsäuregele verwendet werden.Furthermore, silica gels can also advantageously be used.
Unter den Polyacrylaten befinden sich z.B. Carbopol Typen der Firma Goodrich (Carbopol 980, 981 , 1382, 5984, 2984, EDT 2001 oder Pemulen TR2).The polyacrylates include e.g. Carbopol types from Goodrich (Carbopol 980, 981, 1382, 5984, 2984, EDT 2001 or Pemulen TR2).
Unter den Polymeren befinden sich z.B. Polyacrylamide (Seppigel 305), Polyvinylalkohoie, PVP, PVP / VA Copolymere, Polyglycole.Among the polymers are e.g. Polyacrylamides (Seppigel 305), polyvinyl alcohol, PVP, PVP / VA copolymers, polyglycols.
Erfindungsgemäße als Emulsionen vorliegenden Zubereitungen enthalten einen oder mehrere Emulgatoren. Diese Emulgatoren können vorteilhaft gewählt werden aus der Gruppe der nichtionischen, anionischen, kationischen oder amphoteren Emulgatoren.Preparations according to the invention in the form of emulsions contain one or more emulsifiers. These emulsifiers can advantageously be selected from the group of nonionic, anionic, cationic or amphoteric emulsifiers.
Unter den nichtionischen Emulgatoren befinden sich a) Partialfettsäureester und Fettsäureester mehrwertiger Alkohole und deren ethoxylierte Derivate (z. B. Glycerylmonostearate, Sorbitanstearate, Glycerylstearylcitrate, Sucrose- stearate) b) ethoxylierte Fettalkohole und Fettsäuren c) ethoxilierte Fettamine, Fettsäureamide, Fettsäurealkanolamide d) Alkylphenolpolyglycolether (z.B. Triton X) Unter den anionischen Emulgatoren befinden sich a) Seifen (z. B. Natriumstearat) b) Fettalkoholsulfate c) Mono-, Di- und Trialkylphosphosäureester und deren EthoxylateAmong the nonionic emulsifiers are a) partial fatty acid esters and fatty acid esters of polyhydric alcohols and their ethoxylated derivatives (e.g. glyceryl monostearates, sorbitan stearates, glyceryl stearyl citrates, sucrose stearates) b) ethoxylated fatty alcohols and fatty acids c) ethoxylated fatty amides, fatty acid glycol amides, fatty acid glycol amides, fatty acid glycol amides, fatty acid glycol amides, e.g. Triton X) The anionic emulsifiers include a) soaps (e.g. sodium stearate) b) fatty alcohol sulfates c) mono-, di- and trialkylphosphonic acid esters and their ethoxylates
Unter den kationischen Emulgatoren befinden sich a) quaternäre Ammoniumverbindungen mit einem langkettigen aliphatischen Rest z.B. Distearyldimonium Chloride Unter den amphoteren Emulgatoren befinden sich , a) Alkylamininoalkancarbonsäuren b) Betaine, Sulfobetaine c) Imidazolinderivate Weiterhin gibt es natürlich vorkommende Emulgatoren, zu denen Bienenwachs, Wollwachs, Lecithin und Sterole gehören.The cationic emulsifiers include a) quaternary ammonium compounds with a long-chain aliphatic radical, e.g. Distearyldimonium Chloride Among the amphoteric emulsifiers are: a) alkylamininoalkane carboxylic acids b) betaines, sulfobetaines c) imidazoline derivatives There are also naturally occurring emulsifiers, which include beeswax, wool wax, lecithin and sterols.
OΛ/V-Emulgatoren können beispielsweise vorteilhaft gewählt werden aus der Gruppe der po- lyet oxylierten bzw. polypropoxylierten bzw. polyethoxylierten und polypropoxylierten Pro- dukte, z.B.: der Fettal koholethoxylate der ethoxylierten Wollwachsalkohole, der Polyethylenglycolether der allgemeinen Formel R-0-(-CH2-CH2-0-)n-R', der Fettsäureethoxylate der allgemeinen Formel R-COO-(-CH2-CH2-0-)n-H, der veretherten Fettsäureethoxylate der allgemeinen Formel R-C00-(-CH2-CH2-0-)n -R', der veresterten Fettsäureethoxylate der allgemeinen Formel R-C00-(-CH2-CH2-0-)n -C(0)-R', - der Polyethylenglycolglycerinfettsäureester der ethoxylierten Sorbitanester der Cholesterinethoxylate der ethoxylierten Triglyceride der Alkylethercarbonsäuren der allgemeinen Formel R-0-(-CH2-CH2-0-)n-CH2-COOH nd n eine Zahl von 5 bis 30 darstellen, der Polyoxyethylensorbitolfettsäureester, der Alkylethersulfate der allgemeinen Formel R-0-(-CH2-CH2-0-)n-S03-H der Fettalkoholpropoxylate der allgemeinen Formel R-0-(-CH2-CH(CH3)-0-)n-H, der Polypropylenglycolether der allgemeinen Formel R-0-(-CH2-CH(CH3)-0-)π-R', der propoxylierten Wollwachsalkohole, der veretherten Fettsäurepropoxylate R-COO-(-CH2-CH(CH3)-0-)π-R', der veresterten Fettsäurepropoxylate der allgemeinen Formel R-COO-(-CH2-CH(CH3)-0-)π-C(0)-R', der Fettsäurepropoxylate der allgemeinen Formel R-COO-(-CH2-CH(CH3)-0-)n-H, - der Polypropylenglycolglycerinfettsäureester der propoxylierten Sorbitanester der Cholesterinpropoxylate der propoxylierten Triglyceride der Alkylethercarbonsäuren der allgemeinen Formel R-0-(-CH2-CH(CH3)0-)π-CH2-COOH der Alkylethersulfate bzw. die diesen Sulfaten zugrundeliegenden Säuren der allgemeinen Formel R-0-(-CH2-CH(CH3)-0-)n-S03-H der Fettalkoholethoxylate/propoxylate der allgemeinen Formel R-0-Xn-Ym-H, - der Polypropylenglycolether der allgemeinen Formel R-0-Xn-Ym-R', der veretherten Fettsäurepropoxylate der allgemeinen Formel R-COO-Xn-YπrR', der Fettsäureethoxylate/propoxylate der allgemeinen Formel R-COO-Xn-Ym-H,.O / V emulsifiers can, for example, advantageously be selected from the group of the polyethoxylated or polypropoxylated or polyethoxylated and polypropoxylated products, for example: the fatty alcohol ethoxylates of the ethoxylated wool wax alcohols, the polyethylene glycol ethers of the general formula R-0 - (- CH 2 -CH 2 -0-) n -R ', the fatty acid ethoxylates of the general formula R-COO - (- CH 2 -CH 2 -0-) n -H, the etherified fatty acid ethoxylates of the general formula R-C00 - (- CH 2 -CH 2 -0-) n -R ', the esterified fatty acid ethoxylates of the general formula R-C00 - (- CH 2 -CH 2 -0-) n -C (0) -R', - the polyethylene glycol glycerol fatty acid ester of the ethoxylated Sorbitan esters of cholesterol ethoxylates of ethoxylated triglycerides of alkyl ether carboxylic acids of the general formula R-0 - (- CH 2 -CH 2 -0-) n -CH 2 -COOH and n represent a number from 5 to 30, the polyoxyethylene sorbitol fatty acid esters, the alkyl ether sulfates of the general formula R-0 - (- CH 2 -CH 2 -0-) n -S0 3 -H of the fatty alcohol propoxylates of the general formula R-0 - (- CH 2 -CH (CH 3 ) -0-) n -H, the polypropylene glycol ether of the general formula R-0 - (- CH 2 -CH (CH 3 ) -0-) π -R ', the propoxylated wool wax alcohols, the etherified fatty acid propoxylates R-COO - (- CH 2 -CH (CH 3 ) -0-) π -R', the esterified fatty acid propoxylates of the general Formula R-COO - (- CH 2 -CH (CH 3 ) -0-) π -C (0) -R ', the fatty acid propoxylates of the general formula R-COO - (- CH 2 -CH (CH 3 ) -0 -) n -H, - the polypropylene glycol glycerol fatty acid ester of the propoxylated sorbitan esters of the cholesterol propoxylates of the propoxylated triglycerides of the alkyl ether carboxylic acids of the general formula R-0 - (- CH 2 -CH (CH 3 ) 0-) π -CH 2 -COOH of the alkyl ether sulfates or the acids of the general formula R-0 - (- CH 2 - CH (CH 3 ) -0-) n -S0 3 -H of the fatty alcohol ethoxylates / propoxylates of the general formula R-0-X n -Y m -H, - the polypropylene glycol ether of the general formula R-0-X n -Y m - R ', the etherified fatty acid propoxylates of the general formula R-COO-X n -Y π rR', the fatty acid ethoxylates / propoxylates of the general formula R-COO-X n -Y m -H ,.
Erfindungsgemäß besonders vorteilhaft werden die eingesetzten polyethoxylierten bzw. polypropoxylierten bzw. polyethoxylierten und polypropoxylierten O/W-Emulgatoren gewählt aus der Gruppe der Substanzen mit HLB-Werten von 11 - 18, ganz besonders vorteilhaft mit mit HLB-Werten von 14,5 - 15,5, sofern die O/W-Emulgatoren gesättigte Reste R und R' aufweisen. Weisen die O/W-Emulgatoren u ngesättigte Reste R und/oder R ' auf, oder liegen Isoalkylderivate vor, so kann der bevorzugte HLB-Wert solcher Emulgatoren auch niedriger oder darüber liegen.According to the invention, the polyethoxylated or polypropoxylated or polyethoxylated and polypropoxylated O / W emulsifiers used are particularly advantageously selected from the group of substances with HLB values of 11-18, very particularly advantageously with HLB values of 14.5 - 15.5, provided the O / W emulsifiers have saturated residues R and R '. If the O / W emulsifiers have unsaturated radicals R and / or R ', or if isoalkyl derivatives are present, the preferred HLB value of such emulsifiers can also be lower or higher.
Es ist von Vorteil, die Fettalkoholethoxylate aus der Gruppe der ethoxylierten Stearylal- kohole, Cetylalkohole, Cetylstearylalkohole (Cetearylalkohole) zu wählen. Insbesondere bevorzugt sind:It is advantageous to choose the fatty alcohol ethoxylates from the group of the ethoxylated stearyl alcohols, cetyl alcohols, cetylstearyl alcohols (cetearyl alcohols). The following are particularly preferred:
Polyethylenglycol(13)stearylether (Steareth-13), Polyethylenglycol(14)stearylether (Steareth- 14), Polyethylenglycol(15)stearylether (Steareth-15), Polyethylenglycol(16)stearylether (Steareth-16), Polyethylenglycol(17)stearylether (Steareth-17), Polyethylenglycol(18)stearyl- ether (Steareth-18), Polyethylenglycol(19)stearylether (Steareth-19), Polyethylenglycol(20)- stearylether (Steareth-20),Polyethylene glycol (13) stearyl ether (steareth-13), polyethylene glycol (14) stearyl ether (steareth-14), polyethylene glycol (15) stearyl ether (steareth-15), polyethylene glycol (16) stearyl ether (steareth-16), polyethylene glycol (17) stearyl ether ( Steareth-17), polyethylene glycol (18) stearyl ether (Steareth-18), polyethylene glycol (19) stearyl ether (Steareth-19), polyethylene glycol (20) - stearyl ether (Steareth-20),
Polyethylenglycol(12)isostearylether (lsosteareth-12), Polyethylenglycol(13)isostearylether (lsosteareth-13), Polyethylenglycol(14)isostearylether (lsosteareth-14), Polyethyleπglycol- (15)isostearylether (lsosteareth-15), Polyethylenglycol(16)isostearylether (lsosteareth-16), Polyethylenglycol(17)isostearylether (lsosteareth-17), Polyethylenglycol(18)isostearylether (lsosteareth-18), Polyethylenglycol(19)isostearylether (lsosteareth-19), Polyethylenglycol- (20)isostearylether (lsosteareth-20),Polyethylene glycol (12) isostearyl ether (isosteareth-12), polyethylene glycol (13) isostearyl ether (isosteareth-13), polyethylene glycol (14) isostearyl ether (isosteareth-14), polyethylene glycol (15) isostearyl ether (isosteareth-15), polyethyleneostearyl (16 (isosteareth-16), polyethylene glycol (17) isostearyl ether (isosteareth-17), polyethylene glycol (18) isostearyl ether (isosteareth-18), polyethylene glycol (19) isostearyl ether (isosteareth-19), polyethylene glycol (20) isostearyl ether (isosteareth-20 .
Polyethylenglycol(13)cetylether (Ceteth-13), Polyethylenglycol(14)cetylether (Ceteth- 4), Polyethylenglycol(15)cetylether (Ceteth-15), Polyethylenglycol(16)cetylether (Ceteth-16), Polyethylenglycol(17)cetylether (Ceteth-17), Polyethylenglycol(18)cetylether (Ceteth-18), Polyethylenglycol(19)cetylether (Ceteth-19), Polyethylenglycol(20)cetylether (Ceteth-20),Polyethylene glycol (13) cetyl ether (ceteth-13), polyethylene glycol (14) cetyl ether (ceteth-4), polyethylene glycol (15) cetyl ether (ceteth-15), polyethylene glycol (16) cetyl ether (ceteth-16), polyethylene glycol (17) cetyl ether ( Ceteth-17), polyethylene glycol (18) cetyl ether (ceteth-18), polyethylene glycol (19) cetyl ether (ceteth-19), polyethylene glycol (20) cetyl ether (ceteth-20),
Polyethylenglycol(13)isocetylether (lsoceteth-13), Polyethylenglycol(14)isocetylether (Iso- ceteth-14), Polyethylenglycol(15)isocetylether (lsoceteth-15), Polyethylenglycol(16)- isocetylether (lsoceteth- 6), Polyethylenglycol(17)isocetylether (lsoceteth-17), Polyethylen- glycol(18)isocetylether (lsoceteth-18), Polyethylenglycol(19)isocetylether (lsoceteth-19), Polyethylenglycol(20)isocetylether (lsoceteth-20), Polyethylenglycol(12)oleylether (Oleth-12), Polyethylenglycol(13)oleylether (Oleth-13), Poly- ethylenglycol(14)oleylether (Oleth-14), Polyethylenglycol(15)oleylether (Oleth-15),Polyethylene glycol (13) isocetyl ether (isoceteth-13), polyethylene glycol (14) isocetyl ether (isoceteth-14), polyethylene glycol (15) isocetyl ether (isoceteth-15), polyethylene glycol (16) - isocetyl ether (isoceteth-6), polyethylene glycol (17 ) isocetyl ether (isoceteth-17), polyethylene glycol (18) isocetyl ether (isoceteth-18), polyethylene glycol (19) isocetyl ether (isoceteth-19), polyethylene glycol (20) isocetyl ether (isoceteth-20), Polyethylene glycol (12) oleyl ether (oleth-12), polyethylene glycol (13) oleyl ether (oleth-13), polyethylene glycol (14) oleyl ether (oleth-14), polyethylene glycol (15) oleyl ether (oleth-15),
Polyethylenglycol(12)laurylether (Laureth-12), Polyethylenglycol(12)isolaurylether (Isolau- reth-12).Polyethylene glycol (12) lauryl ether (Laureth-12), polyethylene glycol (12) isolauryl ether (Isolureth-12).
Polyethylenglycol(13)cetylstearylether (Ceteareth-13), Polyethylenglycol(14)cetylstearylether (Ceteareth-14), Polyethylenglycol(15)cetylstearylether (Ceteareth-15), Polyethylenglycol(16)- cetylstearylether (Ceteareth- 6), Polyethylenglycol(17)cetylstearylether (Ceteareth-17), Poly- ethylenglycol(18)cetylstearylether (Ceteareth-18), Polyethylenglycol(19)cetylstearylether (Ceteareth-19), Polyethylenglycol(20)cetylstearylether (Ceteareth-20),Polyethylene glycol (13) cetyl stearyl ether (ceteareth-13), polyethylene glycol (14) cetyl stearyl ether (ceteareth-14), polyethylene glycol (15) cetyl stearyl ether (ceteareth-15), polyethylene glycol (16) - cetyl stearyl ether (ceteareth-6), polyethylene glycol (Ceteareth-17), polyethylene glycol (18) cetyl stearyl ether (Ceteareth-18), polyethylene glycol (19) cetyl stearyl ether (Ceteareth-19), polyethylene glycol (20) cetyl stearyl ether (Ceteareth-20),
Es ist ferner von Vorteil, die Fettsäureethoxylate aus folgender Gruppe zu wählen:It is also advantageous to choose the fatty acid ethoxylates from the following group:
Polyethylenglycol(20)stearat, Polyethylenglycol(21)stearat, Polyethylenglycol(22)stearat, Polyethylenglycol(23)stearat, Polyethylenglycol(24)stearat, Polyethylenglycol(25)stearat,Polyethylene glycol (20) stearate, polyethylene glycol (21) stearate, polyethylene glycol (22) stearate, polyethylene glycol (23) stearate, polyethylene glycol (24) stearate, polyethylene glycol (25) stearate,
Polyethylenglycol(12)isostearat, Polyethylenglycol(13)isostearat, Polyethylenglycol(14)iso- stearat, Polyethylenglycol(15)isostearat, Polyethylenglycol(16)isostearat, Polyethylenglycol- (17)isostearat, Polyethylenglycol(18)isostearat, Polyethylenglycol(19)isostearat, Polyethylen- glycol(20)isostearat, Polyethylenglycol(21 )isostearat, Polyethylenglycol(22)isostearat, Poly- ethylenglycol(23)isostearat, Polyethylenglycol(24)isostearat, Polyethylenglycol(25)isostearat,Polyethylene glycol (12) isostearate, polyethylene glycol (13) isostearate, polyethylene glycol (14) isostearate, polyethylene glycol (15) isostearate, polyethylene glycol (16) isostearate, polyethylene glycol (17) isostearate, polyethylene glycol (18) isostearate, polyethylene glycol (19) isostearate , Polyethylene glycol (20) isostearate, polyethylene glycol (21) isostearate, polyethylene glycol (22) isostearate, polyethylene glycol (23) isostearate, polyethylene glycol (24) isostearate, polyethylene glycol (25) isostearate,
Polyethylenglycol(12)oleat, Polyethylenglycol(13)oleat, Polyethylenglycol(14)oleat, Polyethy- lenglycol(15)oleat, Polyethylenglycol(16)oleat, Polyethylenglycol(17)oleat, Polyethylenglycol- (18)oleat, Polyethylenglycol(19)oleat, Polyethylenglycol(20)oleatPolyethylene glycol (12) oleate, polyethylene glycol (13) oleate, polyethylene glycol (14) oleate, polyethylene glycol (15) oleate, polyethylene glycol (16) oleate, polyethylene glycol (17) oleate, polyethylene glycol (18) oleate, polyethylene glycol (19) oleate , Polyethylene glycol (20) oleate
Als ethoxylierte Alkylethercarbonsäure bzw. deren Salz kann vorteilhaft das Natriumlaureth- 11-carboxylat verwendet werden. .The sodium laureth-11 carboxylate can advantageously be used as the ethoxylated alkyl ether carboxylic acid or its salt. ,
Als Alkylethersulfat kann Natrium Laureth 1-4 sulfat vorteilhaft verwendet werden.Sodium laureth 1-4 sulfate can advantageously be used as alkyl ether sulfate.
Als ethoxyliertes Cholesterinderivat kann vorteilhaft Polyethylenglycol(30)Cholesterylether verwendet werden. Auch Polyethylenglycol(25)Sojasterol hat sich bewährt. Als ethoxylierte Triglyceride können vorteilhaft die Polyethylenglycol(60) Evening Primrose Glycerides verwendet werden (Evening Primrose = Nachtkerze)Polyethylene glycol (30) cholesteryl ether can advantageously be used as the ethoxylated cholesterol derivative. Polyethylene glycol (25) soyasterol has also proven itself. Polyethylene glycol (60) evening primrose glycerides can advantageously be used as ethoxylated triglycerides (evening primrose = evening primrose)
Weiterhin ist von Vorteil, die Polyethylenglycolglycerinfettsäureester aus der Gruppe Poly- ethylenglycol(20)glyceryllaurat, Polyethylenglycol(21 )glyceryllaurat, Polyethylenglycol(22)gly- ceryllaurat, Polyethylenglycol(23)glyceryllaurat, Polyethylenglycol(6)glycerylcaprat caprinat, Polyethylenglycol(20)glyceryloleat, Polyethylenglycol(20)glycerylisostearat, Polyethylengly- col(18)glyceryloleat/cocoat zu wählen.It is also advantageous to use the polyethylene glycol glycerol fatty acid esters from the group polyethylene glycol (20) glyceryl laurate, polyethylene glycol (21) glyceryl laurate, polyethylene glycol (22) glyceryl laurate, polyethylene glycol (23) glyceryl laurate, polyethylene glycol (6) glyceryl caprolate caprinate, polyethylene glycol To choose polyethylene glycol (20) glyceryl isostearate, polyethylene glycol (18) glyceryl oleate / cocoat.
Es ist ebenfalls günstig, die Sorbitanester aus der Gruppe Polyethylenglycol(20)sorbitanmo- nolaurat, Polyethylenglycol(20)sorbitanmonostearat, Polyethylenglycol(20)sorbitanmonoiso- stearat, Polyethylenglycol(20)sorbitanmonopalmitat, Polyethylenglycol(20)sorbitanmonooleat zu wählen.It is also favorable to select the sorbitan esters from the group consisting of polyethylene glycol (20) sorbitan monolaurate, polyethylene glycol (20) sorbitan monostearate, polyethylene glycol (20) sorbitan monoisostearate, polyethylene glycol (20) sorbitan monopalmitate, polyethylene glycol (20) sorbitan monooleate.
Als vorteilhafte W/O-Emulgatoren können eingesetzt werden: Fettalkohole mit 8 bis 30 Kohlenstoffatomen, Monoglycerinester gesättigter und/oder ungesättigter, verzweigter und/oder unverzweigter Alkancarbonsäuren einer Kettenlänge von 8 bis 24, insbesondere 12 - 18 C- Atomen, Diglycerinester gesättigter und/oder ungesättigter, verzweigter und/oder unver- zweigter Alkancarbonsäuren einer Kettenlänge von 8 bis 24, insbesondere 12 - 18 C-Atomen, Monoglycerinether gesättigter und/oder ungesättigter, verzweigter und/oder unverzweigter Alkohole einer Kettenlänge von 8 bis 24, insbesondere 12 - 18 C-Atomen, Diglyce- rinether gesättigter und/oder ungesättigter, verzweigter und/oder unverzweigter Alkohole einer Kettenlänge von 8 bis 24, insbesondere 12 - 18 C-Atomen, Propylenglycolester gesättig- ter und/oder ungesättigter, verzweigter und/oder unverzweigter Alkancarbonsäuren einer Kettenlänge von 8 bis 24, insbesondere 12 - 18 C-Atomen sowie Sorbitanester gesättigter und/oder ungesättigter, verzweigter und/oder unverzweigter Alkancarbonsäuren e iner Kettenlänge von 8 bis 24, insbesondere 12 - 18 C-Atomen.Advantageous W / O emulsifiers that can be used are: fatty alcohols with 8 to 30 carbon atoms, monoglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 8 to 24, in particular 12 to 18 carbon atoms, diglycerol esters saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 8 to 24, in particular 12 to 18 carbon atoms, monoglycerol ethers saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 8 to 24, in particular 12 to 18 C atoms, diglycerine ethers of saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 8 to 24, in particular 12-18 C atoms, propylene glycol esters of saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids Chain length of 8 to 24, in particular 12 - 18 carbon atoms and sorbitan esters saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids in a chain length of 8 to 24, in particular 12 - 18 carbon atoms.
Insbesondere vorteilhafte W/O-Emulgatoren sind Glycerylmonostearat, Glycerylmonoiso- stearat, Glycerylmonomyristat, Glycerylmonooleat, Diglycerylmonostearat, Diglycerylmono- isostearat, Propylenglycolmonostearat, Propylenglycolmonoisostearat, Propylenglycolmono- caprylat, Propylengiycolmonolaurat, Sorbitanmonoisostearat, Sorbitanmonolaurat, Sorbitan- monocaprylat, Sorbitanmonoisooleat, Saccharosedistearat, Cetylalkohol, Stearylalkohol, Arachidylalkohol, Behenylalkohol, Isobehenylalkohol, Selachylalkohol, Chimylalkohol, Poly- ethylenglycol(2)stearylether (Steareth-2), Glycerylmonolaurat, Glycerylmonocaprinat, Glyce- rylmonocaprylat.Particularly advantageous W / O emulsifiers are glyceryl stearate Glycerylmonoiso-, glyceryl monomyristate, glyceryl, diglyceryl monostearate, Diglycerylmono- isostearate, propylene glycol caprylate, propylene glycol monoisostearate, propylene glycol, Propylengiycolmonolaurat, sorbitan, sorbitan, sorbitan monocaprylate, Sorbitanmonoisooleat, sucrose, cetyl alcohol, stearyl alcohol, Arachidyl alcohol, behenyl alcohol, isobehenyl alcohol, selachyl alcohol, chimyl alcohol, polyethylene glycol (2) stearyl ether (Steareth-2), glyceryl monolaurate, glyceryl monocaprinate, glyceryl monocaprylate.
Die folgenden Beispiele sollen die Erfindung erläutern, aber nicht einschränken. Die Zahlenangaben beziehen sich auf Gew.-%, sofern nichts Anderes angegeben ist. The following examples are intended to illustrate, but not limit, the invention. The figures relate to% by weight, unless stated otherwise.
Beispiel Nr. 1 Gew.-%Example No. 1% by weight
O/W-CremeO / W cream
Glycerylsterat selbstemulgierend 4,00Self-emulsifying glyceryl sterate 4.00
PEG-40-Stearat 1 ,00PEG-40 stearate 1, 00
Cetylalkohol 3,00Cetyl alcohol 3.00
Caprylsäure-/Caprinsäuretriglyceride 5,00Caprylic acid / capric acid triglycerides 5.00
Paraffinum liquidum 5,00Paraffinum liquidum 5.00
Licochalcon A 0,05Licochalcon A 0.05
Arctiin 0,1Arctiin 0.1
Tocopherol 0,1Tocopherol 0.1
Na3HEDTA 0,1Na 3 HEDTA 0.1
Konservierungsmittel, Parfüm q.s.Preservative, perfume q.s.
Polyacrylsäure 3,00Polyacrylic acid 3.00
Natronlauge 45% q.sCaustic soda 45% q.s
Glycerin 5,00Glycerin 5.00
Wasser ad100 Water ad100
Beispiel Nr. 2 Gew.-%Example No. 2% by weight
O/W-CremeO / W cream
Glycerylsterat selbstemulgierend 3,00Self-emulsifying glyceryl sterate 3.00
Stearinsäure 1 ,00Stearic acid 1, 00
Cetylalkohol 2,00Cetyl alcohol 2.00
Caprylsäure-/Caprinsäuretriglyceride 3,00Caprylic acid / capric acid triglycerides 3.00
Dicaprylylether 4,00Dicaprylyl ether 4.00
Paraffinum liquidum 2,00Paraffinum liquidum 2.00
Licochalcon A 0,01Licochalcon A 0.01
Arctiin 0,50Arctiin 0.50
Konservierungsmittel, Parfüm q.s.Preservative, perfume q.s.
Polyacrylsäure 0,10Polyacrylic acid 0.10
Natronlauge 45% q.s.Caustic soda 45% q.s.
Glycerin 3,00Glycerin 3.00
Butylenglycol 3,00Butylene glycol 3.00
Wasser ad 100Water ad 100
Beispiel Nr. 3 Gew.-%Example No. 3% by weight
O/W-CremeO / W cream
Glycerylstearatcitrat 2,00Glyceryl stearate citrate 2.00
Stearylalkohol 2,00Stearyl alcohol 2.00
Lanolinalkohol 1 ,00Lanolin alcohol 1.00
Caprylsäure-/Caprinsäuretriglyceride 4,00Caprylic acid / capric acid triglycerides 4.00
Paraffinum liquidum 8,00Paraffinum liquidum 8.00
Dimethicon 1 ,00Dimethicone 1.00
Licochalcon A 0,04Licochalcon A 0.04
Arctiin 2,00Arctiin 2.00
Konservierungsmittel, Parfüm q.s.Preservative, perfume q.s.
Natronlauge 45% q.s.Caustic soda 45% q.s.
Glycerin 7,50Glycerin 7.50
Wasser ad100 Beispiel Nr. 4 Gew.-%Water ad100 Example No. 4% by weight
W/O-CremeW / O Cream
Polyglyceryl-3-Diisostearat 3,50Polyglyceryl-3-diisostearate 3.50
Glycerin 3,00Glycerin 3.00
Polyglyceryl-2-Dipolyhydroxystearat 3,50Polyglyceryl-2-dipolyhydroxystearate 3.50
Licochalcon A 0,1Licochalcon A 0.1
Arctiin 1 ,00Arctiin 1, 00
Konservierungsmittel q.s.Preservatives q.s.
Parfüm q.s.Perfume q.s.
Magnesiumsulfat 0,6Magnesium sulfate 0.6
Isopropylstearat 2,0Isopropyl stearate 2.0
Caprylylether 8,0Caprylyl ether 8.0
Cetearylisononanoat 6,0Cetearyl isononanoate 6.0
Wasser ad 100 Water ad 100
Beispiel Nr. 5 Gew.-%Example No. 5% by weight
W/O-EmulsionW / O emulsion
Triceteareth-4-Phosphat 0,80Triceteareth-4-phosphate 0.80
Butylhydroxytoluol 0,05Butylated hydroxytoluene 0.05
Glyceryllanolat 1,70Glyceryl alcoholate 1.70
Cyclomethicon 2,20Cyclomethicone 2.20
Isopropylpalmitat 1,00Isopropyl palmitate 1.00
Licochalcon A 0,10Licochalcon A 0.10
Arctiin 1,00Arctiin 1.00
Polyacrylsäure 0,50Polyacrylic acid 0.50
Ethylendiamintetraessigsäure 1 ,00Ethylenediaminetetraacetic acid 1.00
Natriumhydroxid q.s.Sodium hydroxide q.s.
Zitronensäure 0,01Citric acid 0.01
Konservierungsmittel q.s.Preservatives q.s.
Parfüm q.s.Perfume q.s.
Wasser ad 100 Water ad 100

Claims

Patentansprüche: claims:
1. Wirkstoffkombinationen aus1. Active ingredient combinations
(a) einem oder mehreren 2,3-Dibenzylbutyrolactonderivaten und (b) Licochalcon A oder einem wässrigen Extrakt aus Radix Glycyrrhizae inflatae, enthaltend Licochalcon A(a) one or more 2,3-dibenzylbutyrolactone derivatives and (b) licochalcon A or an aqueous extract from Radix Glycyrrhizae inflatae, containing licochalcon A
2. Wirkstoffkombinationen nach Anspruch 1 , dadurch gekennzeichnet, dass das oder die 2,3-Dibenzylbutyrolactonderivate und Licochalcon A in Verhältnissen von 100 : 1 bis 1 : 50, bevorzugt 80 : 1 bis 1 : 10, besonders bevorzugt 20 : 1 vorliegen2. Active substance combinations according to claim 1, characterized in that the 2,3-dibenzylbutyrolactone derivative and licochalcone A are present in ratios of 100: 1 to 1:50, preferably 80: 1 to 1:10, particularly preferably 20: 1
3. Wirkstoffkombinationen nach Anspruch 1, dadurch gekennzeichnet, dass als 2,3- Dibenzylbutyrolactonderivat das Arctiin gewählt wird.3. Active ingredient combinations according to claim 1, characterized in that the arctiin is chosen as the 2,3-dibenzylbutyrolactone derivative.
4. Kosmetische oder dermatologische Zubereitungen, enthaltend Wirkstoffkombinationen nach Anspruch 1 oder 2.4. Cosmetic or dermatological preparations containing active ingredient combinations according to claim 1 or 2.
5. Zubereitungen nach Anspruch 3, enthaltend 0,01 - 25 Gew.-% eines oder mehrerer 2,3- Dibenzylbutyrolactonderivate, bevorzugt 0,1 - 20 Gew.-%, insbesondere 1 - 10 Gew.-%, je- weils bezogen auf das Gesamtgewicht der Zubereitungen.5. Preparations according to claim 3, containing 0.01-25% by weight of one or more 2,3-dibenzylbutyrolactone derivatives, preferably 0.1-20% by weight, in particular 1-10% by weight, in each case based on the total weight of the preparations.
6. Zubereitungen nach Anspruch 2 oder 3, enthaltend 0,0001 bis 5 Gew.-%, insbesondere 0,001 b is 1 Gew.-%, ganz b esonders 0,005 bis 0,15 Gew.-% Licochalcon A, bezogen auf das Gesamtgewicht der Zubereitung.6. Preparations according to claim 2 or 3, containing 0.0001 to 5% by weight, in particular 0.001 to 1% by weight, very particularly 0.005 to 0.15% by weight of licochalcone A, based on the total weight of the Preparation.
7. Zubereitungen nach Anspruch 2, 3 oder 4, enthaltend 0,001 bis 10 Gew.-%, insbesondere 0,05 bis 5 Gew.-%, ganz besonders 0,01 bis 2 Gew.-% an einem oder mehreren Polyolen, bezogen auf das Gesamtgewicht der Zubereitung.7. Preparations according to claim 2, 3 or 4, containing 0.001 to 10 wt .-%, in particular 0.05 to 5 wt .-%, very particularly 0.01 to 2 wt .-% of one or more polyols, based on the total weight of the preparation.
8. Verwendung von Wirkstoffkombinationen oder Zubereitungen nach einem oder mehreren der vorstehenden Ansprüche zur Prophylaxe und/oder Behandlung von entzündlichen Hautzuständen und/oder zum Hautschutz bei empfindlich determinierter und trockener Haut. 8. Use of active substance combinations or preparations according to one or more of the preceding claims for the prophylaxis and / or treatment of inflammatory skin conditions and / or for skin protection in the case of sensitive, determined and dry skin.
9. Verwendung von Wirkstoffkombinationen oder Zubereitungen nach einem oder mehreren der vorstehenden Ansprüche zur Behandlung und Prophylaxe der Symptome der intrinsi- schen und/oder extrinsischen Hautalterung sowie zur Behandlung und Prophylaxe der schädlichen Auswirkungen ultravioletter Strahlung auf die Haut.9. Use of active substance combinations or preparations according to one or more of the preceding claims for the treatment and prophylaxis of the symptoms of intrinsic and / or extrinsic skin aging and for the treatment and prophylaxis of the harmful effects of ultraviolet radiation on the skin.
10. Verwendung von Wirkstoffkombinationen oder Zubereitungen nach einem oder mehreren der vorstehenden Ansprüche zur Behandlung und/oder Prophylaxe von Pigmentie- rungsstörungen.10. Use of active substance combinations or preparations according to one or more of the preceding claims for the treatment and / or prophylaxis of pigmentation disorders.
11. Verwendung von Wirkstoffkombinationen oder Zubereitungen nach einem oder mehreren der vorstehenden Ansprüche zur Steigerung der Ceramidbiosynthese .11. Use of active ingredient combinations or preparations according to one or more of the preceding claims to increase ceramide biosynthesis.
12. Verwendung von Wirkstoffkombinationen oder Zubereitungen nach einem oder mehreren der vorstehenden Ansprüche zur Stärkung der Barrierefunktion der Haut .12. Use of active ingredient combinations or preparations according to one or more of the preceding claims for strengthening the barrier function of the skin.
13. Verwendung von Wirkstoffkombinationen oder Zubereitungen nach einem oder mehreren der vorstehenden Ansprüche zur Behandlung und/oder Prophylaxe von funktionellen Störungen der Hautanhangsgebilde . 13. Use of active substance combinations or preparations according to one or more of the preceding claims for the treatment and / or prophylaxis of functional disorders of the skin appendages.
EP04819609A 2003-12-03 2004-11-22 Combination of 2,3-dibenzylbutyrolactone and licochalcone-a Withdrawn EP1696903A1 (en)

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