EP1418884A2 - Cosmetic and dermatological preparations in the form of o/w emulsions containing sterols and/or c12-c40 fatty acids - Google Patents

Cosmetic and dermatological preparations in the form of o/w emulsions containing sterols and/or c12-c40 fatty acids

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Publication number
EP1418884A2
EP1418884A2 EP02762429A EP02762429A EP1418884A2 EP 1418884 A2 EP1418884 A2 EP 1418884A2 EP 02762429 A EP02762429 A EP 02762429A EP 02762429 A EP02762429 A EP 02762429A EP 1418884 A2 EP1418884 A2 EP 1418884A2
Authority
EP
European Patent Office
Prior art keywords
preparations
group
saturated
branched
fatty acids
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Application number
EP02762429A
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German (de)
French (fr)
Inventor
Jens Nielsen
Thomas Raschke
Heidi Riedel
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
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Beiersdorf AG
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Application filed by Beiersdorf AG filed Critical Beiersdorf AG
Publication of EP1418884A2 publication Critical patent/EP1418884A2/en
Withdrawn legal-status Critical Current

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Classifications

    • 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
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/361Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04Dispersions; Emulsions
    • A61K8/06Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04Dispersions; Emulsions
    • A61K8/06Emulsions
    • A61K8/062Oil-in-water emulsions
    • 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
    • A61K8/34Alcohols
    • A61K8/342Alcohols having more than seven atoms in an unbroken chain
    • 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
    • A61K8/37Esters of carboxylic acids
    • A61K8/375Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
    • 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
    • A61K8/39Derivatives containing from 2 to 10 oxyalkylene groups
    • 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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K8/67Vitamins
    • A61K8/671Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
    • 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
    • A61K8/67Vitamins
    • A61K8/678Tocopherol, i.e. vitamin E
    • 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
    • A61K8/68Sphingolipids, e.g. ceramides, cerebrosides, gangliosides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures

Definitions

  • the present invention relates to cosmetic and dermatological emulsions, in particular skin-care cosmetic and dermatological emulsions.
  • the present invention relates to an application which makes it possible to increase the stability of preparations containing fatty acids, in particular emulsions, preferably O / W emulsions.
  • the skin is the largest human organ. Among its many functions (for example for heat regulation and as a sensory organ), the most important is the barrier function that prevents the skin (and ultimately the entire organism) from drying out. At the same time, the skin acts as a protective device against the penetration and absorption of substances coming from outside. This barrier function is brought about by the epidermis, which as the outermost layer forms the actual protective cover against the environment. At around a tenth of the total thickness, it is also the thinnest layer of the skin.
  • the epidermis is a stratified tissue in which the outer layer, the horny layer (stratum corneum), is the important part for the barrier function.
  • the skin model of Elias (PM Elias, Structure and Function of the Stratum Corneum Permeability Barrier, Drug Dev. Res. 13, 1988, 97-105), which is recognized by experts today, describes the horny layer as a two-component system, similar to a brick wall ( Brick-mortar model).
  • the horny cells corneocytes
  • the complex lipid membrane in the intercellular spaces corresponds to the mortar.
  • This system essentially represents a physical barrier against hydrophilic substances, but due to its narrow and multilayer structure it is equally difficult for lipophilic substances to pass through.
  • the present invention relates to cosmetic or pharmaceutical preparations with a reduced feeling of stickiness, to processes for their preparation and to the use of active ingredients for reducing the stickiness of cosmetic preparations.
  • the epidermal lipids In addition to their barrier effect against external chemical and physical influences, the epidermal lipids also contribute to the cohesion of the homolayer and influence the smoothness of the skin. In contrast to the sebum lipids, which do not form a closed film on the skin, the epidermal lipids are distributed over the entire homolayer.
  • Cosmetic skin care is primarily understood to mean that the natural function of the skin as a barrier against environmental influences (e.g. dirt, chemicals, microorganisms) and against the loss of the body's own substances (e.g. water, natural fats, electrolytes) is strengthened or restored.
  • environmental influences e.g. dirt, chemicals, microorganisms
  • loss of the body's own substances e.g. water, natural fats, electrolytes
  • 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 rain generation capacity is not sufficient.
  • skin care products are intended to protect against environmental influences, particularly sun and wind, and to delay skin aging.
  • Medical topical compositions usually contain one or more drugs in effective concentration.
  • drugs 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.
  • emulsions This is generally understood to mean a heterogeneous system composed of two liquids which are immiscible or only miscible with one another, which are usually referred to as phases. One is in the form of droplets (dispere or inner phase), while the other liquid forms a continuous (coherent or inner phase). More rare forms of administration are multiple emulsions, i.e. those which themselves contain droplets of a further dispersed phase in the droplets of the dispersed (or discontinuous) phase, e.g. W / O / W emulsions and O / W / O emulsions.
  • emulsifiers In order to guarantee the metastability of emulsions, surface-active substances, i.e. emulsifiers, are generally necessary. In itself, the use of the usual cosmetic emulsifiers is completely harmless. Nevertheless, emulsifiers, like any chemical substance, can cause allergic or hypersensitive reactions in individual cases. It is known, for example, that in certain particularly sensitive people certain light dermatoses are triggered by certain emulsifiers and simultaneous exposure to sunlight.
  • emulsifier-free preparations which, for example, have oil droplets dispersed in an aqueous phase, similar to an O / W emulsion. Ahead- The reason for this may be that the continuous aqueous phase has a gel structure which stabilizes the dispersed phase and other circumstances.
  • Such systems are sometimes called hydrodispersions or oleodispersions, depending on which is the disperse phase and which is the continuous phase.
  • a further object of the present invention was to provide preparations which significantly improve the condition of the skin, in particular reduce the roughness of the skin.
  • stearate emulsions that is to say those in which stearic acid and / or palmitic acid or alkali metal salts of stearic acid and / or palmitic acid are effective as emulsifiers.
  • These preparations can advantageously be present as O / V emulsions and are notable for good
  • fatty acids tend to crystallize in a pH range from 3.5 to 8.0 (in particular in a pH range below 7.0), so that the pleasant skin feel, the skin care performance and the external appearance of a corresponding preparation can be severely impaired.
  • low-viscosity preparations of the prior art frequently have the disadvantage that they are unstable, are limited to a narrow application range or a limited choice of starting materials.
  • Low-viscosity products in which, for example, strongly polar oils - such as the vegetable oils commonly used in commercial products - are sufficiently stabilized, are currently not available on the market.
  • viscosity means the property of a liquid to oppose the mutual laminar displacement of two adjacent layers with resistance (toughness, internal friction).
  • is a substance constant with the Sl unit Pascal second (Pa s) at a given temperature.
  • the quotient v ⁇ / p from the dynamic viscosity ⁇ and the density p of the liquid is referred to as the kinematic viscosity v and is given in the SI unit m 2 / s.
  • the use value is determined, among other things, by the so-called ness.
  • the speed of an ointment or ointment base or the like means its property of pulling threads of different lengths when tapping; accordingly, a distinction is made between short and long-lasting fabrics.
  • the falling body viscometry is only suitable for the investigation of Newtonian liquids and gases. It is based on the Stokes law, according to which the dynamic viscosity ⁇ for a ball falling through a liquid flowing around it
  • O / W emulsions with a low viscosity which have a storage stability, as is required for marketable products, can only be formulated with great effort using the prior art. Accordingly, the range of such formulations is extremely small. Nevertheless, such formulations could offer the consumer previously unknown cosmetic services.
  • (I) 1 to 5% by weight, based on the total weight of the preparations, one or more substances selected from the group of sterols, branched or unbranched, saturated or unsaturated C 12 -C 0 fatty acids,
  • the preparations according to the invention act better than moisturizing preparations, better promote smoothing of the skin, are distinguished by better care effects, serve better as a vehicle for cosmetic and medical-dermatological active ingredients have higher stability towards the crystallization of the fatty acids used and would be characterized by better biocompatibility would be characterized by a better skin feel and by higher cosmetic elegance would be characterized by a wide cosmetic variability and by a wide range Consistency and viscosity ranges from 400 mPas to> 20,000 mPas would be formulated as the preparations of the prior art.
  • the preparations according to the invention are both sprayable, flowable and cream-like, can be formulated, have very good cosmetic properties, in particular with regard to stickiness, and have very good skin tolerance and skin care performance.
  • Sterols are steroids that only have a hydroxyl group in the 3-position, but do not have a functional group otherwise, formally represent alcohols. Therefore, the more logical name sterols is sometimes used.
  • the sterols containing 27 to 30 carbon atoms generally have a double bond in the 5/6 position, more rarely also / or in 7/8, 8/9 and other positions (for example 22/23).
  • the sterols are widespread in nature as lipids - mostly in the form of esters (formerly called steroids).
  • the sterols found in the animal kingdom are called zoosterols. The most important representative is cholesterol. Further zoosterols were found in wool fat (lanosterol, dihydrolanosterol), in the silkworm, in sponges (spongosterol), starfish, sea urchins, oysters etc.
  • the plant sterols are called phytosterols. Its main representatives are ergosterol, stigmasterol and sitosterol. You can find some in cosmetics. Products use. Occasionally, the sterols from fungi and yeast are separated from the group of phytosterols as mycosterols (e.g. ergosterol, fungister, stellasterin and zymosterol).
  • mycosterols e.g. ergosterol, fungister, stellasterin and zymosterol.
  • phytosterols examples are:
  • phytosterols to be used according to the invention have a more or less large number of optical isomers, which are not to be listed in detail here, but which have proven to be advantageous insofar as their cosmetic safety is beyond question.
  • Preferred sterols are cholesterol and lanosterol.
  • Preferred fatty acids are stearic acid and / or palmitic acid (stearin) and lignoceric acid.
  • glyceryl monostearate, glyceryl distearate, propylene glycol monostearate examples: glyceryl isostearate, glyceryl alcoholate, glyceryl myristate,
  • (III) 0.1 up to 1.5% by weight of one or more sorbitan esters, selected from the group of the mono-, sesqui-, di and triesters of the sorbitan ( monoanhydrosorbites or 1.5- Anhydro-D-sorbitol) with fatty acids of chain length C 12 - C 40 (even, saturated, unsaturated and branched) and optionally a degree of ethoxylation of 10 - 100).
  • (V) 0.5-7% by weight, based on the total weight of the preparations, of one or more fatty alcohols selected from the group consisting of myristyl alcohol, cetyl alcohol, isocetyl alcohol, cetylstearyl alcohol, stearyl alcohol, isostearyl alcohol, behenyl alcohol and mixtures thereof.
  • the total amount of branched and unbranched alkyl alcohols having 12 to 40 carbon atoms in the finished cosmetic or dermatological preparations is advantageously chosen from the range from 0.1 to 7.0% by weight, preferably 0.5 to 5.0% by weight , based on the total weight of the preparations.
  • Wool wax alcohols represent the unsaponifiable alcohol fraction of the wool wax that is obtained after the saponification of the wool wax. They consist of approximately 25.2% cholesterol, 2.7% lanosterol, 2.2% dihydrolanosterol and approximately 29.5% aliphatic monohydric C 6 -C 32 alcohols. Wool wax alcohols are therefore used for the production of ointment bases, from which mostly W / O emulsions are made. Advantageous embodiments of the present invention therefore relate to preparations according to
  • these wool wax alcohols contain, in addition to the aliphatic alcohols, also one or more sterols, for example cholesterol, lanosterol, dihydrolanosterol.
  • sterols for example cholesterol, lanosterol, dihydrolanosterol.
  • Advantageous embodiments of the present invention relate, for example, to cosmetic and dermatological preparations in the form of O / W emulsions, containing 3% liquid lipids (preferably selected from (a) Guerbet alcohols, (b) saturated triglycerides and (c) ethers of medium-chain fatty alcohols, (d) non-polar lipids, (e) silicone oils, (f) dialkyl carbonates or mixtures thereof.
  • liquid lipids preferably selected from (a) Guerbet alcohols, (b) saturated triglycerides and (c) ethers of medium-chain fatty alcohols, (d) non-polar lipids, (e) silicone oils, (f) dialkyl carbonates or mixtures thereof.
  • lipids is sometimes used as a generic term for fats, oils, waxes and the like, as is well known to the person skilled in the art.
  • oil phase and “lipid phase” are also used synonymously.
  • Oils and fats differ among other things in their polarity, which is difficult to define. It has already been proposed to take the interfacial tension against water as a measure of the polarity index of an oil or an oil phase. The polarity of the oil phase in question is greater, the lower the interfacial tension between this oil phase and water. According to the invention, the interfacial tension is viewed as a possible measure of the polarity of a given oil component.
  • the interfacial tension is the force that acts on an imaginary line of one meter in length that lies in the interface between two phases.
  • the physical unit for this interfacial tension is calculated classically according to the force / length relationship and is usually given in mN / m (millinewtons divided by meters). It has a positive sign if it tries to reduce the size of the interface. In the opposite case, it has a negative sign.
  • mN / m millinewtons divided by meters
  • Polar oils are, for example, those from the group of lecithins and fatty acid triglycerides, namely the triglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 8 to 24, in particular 12 to 18, carbon atoms.
  • the fatty acid triglycerides can, for example, advantageously be selected from the group of synthetic, semi-synthetic and natural oils, such as e.g. Olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, castor oil, wheat germ oil, grape seed oil, safflower oil, evening primrose oil, macadamia nut oil and the like.
  • Further polar oil components can be selected from the group of esters from saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 3 to 30 carbon atoms and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 up to 30 carbon atoms and 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 carbon atoms.
  • ester oils can then advantageously be selected from the group of isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononylisononanoate, 2-ethylhexyl urethane Hexyldecyl stearate, 2-octyldodecyl palmitate, oleyl oleate, olerlerucate, erucyl oleate, erucylerucate as well as synthetic, semi-synthetic and natural mixtures of such esters, such as Jojoba oil.
  • the oil phase can advantageously be chosen from the group of dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols. It is particularly advantageous if the oil phase of the W / O emulsions according to the invention has a C 2-15 alkyl benzoate content or consists entirely of this.
  • the oil phase can advantageously be selected from the group of Guerbet alcohols.
  • Guerbet alcohols are named after Marcel Guerbet, who described their production for the first time. They arise according to the reaction equation R
  • Guerbet alcohols are liquid even at low temperatures and practically do not cause skin irritation. They can advantageously be used as greasing, over-greasing and also moisturizing components in skin and hair care products.
  • R 1 and R 2 generally mean unbranched alkyl radicals.
  • the Guerbet alcohol or alcohols are advantageously selected from the group in which
  • Ri propyl, butyl, pentyl, hexyl, heptyl or octyl and
  • R 2 hexyl, heptyl, octyl, nonyl, decyl, undecyl, dodecyl, tridecyl or tetradecyl.
  • Guerbet alcohols preferred according to the invention are 2-butyl octanol - it has the chemical structure
  • Guerbet alcohols according to the invention can also be used advantageously according to the invention.
  • Mixtures of 2-butyl octanol and 2-hexyl decanol are available, for example, under the trade name Isofol® 14 from Condea Chemie GmbH.
  • the total amount of Guerbet alcohols in the finished cosmetic or dermatological preparations is advantageously selected from the range up to 25.0% by weight, preferably 0.5-15.0% by weight, based on the total weight of the preparations.
  • any mixtures of such oil and wax components can also be used advantageously for the purposes of the present invention. It may also be advantageous to use waxes, for example cetyl palmitate, as the sole lipid component of the oil phase.
  • Nonpolar oils are, for example, those which are selected from the group of branched and unbranched hydrocarbons and waxes, in particular petroleum jelly (petrolatum), paraffin oil, squalane and squalene, polyolefins and hydrogenated polyisobutenes.
  • polyolefins polydecenes are the preferred substances.
  • Table 1 below lists lipids which are advantageous according to the invention as individual substances or as a mixture with one another. The relevant interfacial tensions against water are given in the last column. However, it is also advantageous to use mixtures of higher and lower polar and the like.
  • the following can be used as basic components of the preparations according to the invention: water or aqueous solutions, aqueous ethanolic solutions, natural oils and / or chemically modified natural oils and / or synthetic oils; Fats, waxes and other natural and synthetic fat bodies, preferably esters of fatty acids with alcohols with a low C number, for example with isopropanol, propylene glycol or glycerol, or esters of fatty alcohols with alkanoic acids with a low C number or with fatty acids;
  • 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, diethylene glycol monomethyl or monoethyl ether and analog products.
  • the oil phase of the emulsions preferably consists predominantly of components of the type listed under point (4), although it is possible to accept up to 50% by weight, preferably up to 40, without major disadvantages % By weight of the total weight of the oil components from the group of other oil components.
  • 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 up to 30 carbon 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 carbon atoms.
  • ester oils can then advantageously be selected from the group of isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononylisononanoate, 2-ethyl-2-ethylhexyl palatate 2-octyldodecyl palmitate, oleyl oleate, olerlerucate, erucyl oleate, erucylerucate as well as synthetic, semisynthetic and natural mixtures of such esters, for example Jojoba oil.
  • the oil phase can advantageously be chosen from the group of branched and unbranched hydrocarbons and waxes, the dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols, and also the fatty acid triglycerides, especially the triglycerol esters saturated and / or unsaturated, 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, semi-synthetic 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, provided that the conditions specified in the main claim are met.
  • synthetic, semi-synthetic 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, provided that the conditions specified in the main claim are met.
  • Fat and / or wax components to be used advantageously according to the invention can be selected from the group of vegetable waxes, animal waxes, mineral waxes and petrochemical waxes.
  • Favorable according to the invention are, for example, candelilla wax, carnauba wax, japan wax, esparto grass wax, cork wax, guaruma wax, rice germ oil wax, sugar cane wax, berry wax, ouricury wax, montan wax, jojoba wax, shea butter, beeswax, shellac wax, walnut, lanolin (wool wax), pretzel fat, ceresin Ozokerite (earth wax), paraffin waxes and micro waxes, provided the conditions specified in the main claim are met.
  • fat and / or wax components are chemically modified waxes and synthetic waxes such as those sold under the tradenames Syncrowax HRC (glyceryl tribehenate), Syncrowax HGLC (C 16-3 6-fatty acid triglyceride) (. CI8 36 fatty acid) and Syncrowax AW 1C available from CRODA GmbH as well as montan ester waxes, sasol waxes, hydrogenated jojoba waxes, synthetic or modified beeswaxes (e.g.
  • the fat and / or wax components can be present both individually and in a mixture.
  • the oil phase is advantageously selected from the group 2-ethylhexyl isostearate, octyldodecanol, isotridecylisononanoate, isoeicosane, 2-ethylhexyl cocoate, C ⁇ 2- i 5 alkyl benzoate, caprylic capric acid triglyceride, dicaprylyl ether as long as the conditions are met.
  • Mixtures of octyldodecanol, caprylic-capric acid triglyceride, dicaprylyl ether or mixtures of d 2 are particularly advantageous.
  • hydrocarbons paraffin oil, cycloparaffin, squalane, squalene, hydrogenated polyisobutene or polydecene are to be used advantageously for the purposes of the present invention, provided the conditions specified in the main claim are met.
  • O / W emulsions according to the invention can advantageously be prepared with the aid of the usual O / V emulsifiers, if desired with the aid of W / O emulsifiers or other co-emulsifiers.
  • O / W emulsions according to the present invention further contain one or more emulsifiers, if desired advantageously selected from the group of the following substances, which generally act as W / O emulsifiers:
  • O / W emulsions according to the present invention contain one or more emulsifiers, particularly advantageously selected from the group of the following substances, which generally act as O / W emulsifiers:
  • Emulsions according to the invention in the sense of the present invention are advantageous and contain, for example, fats, oils, waxes and / or other fat bodies, as well as water and one or several emulsifiers, as are usually used for such a type of formulation.
  • the preparations according to the invention can also be sprayable cleansing preparations (“cleaning sprays”) which, for example, for removing make-up and / or make-up or as a mild washing lotion - if appropriate also for impure skin.
  • cleaning sprays Such cleaning preparations can also advantageously be used as so-called “rinse-off preparations" which are rinsed off the skin after use
  • Medical topical compositions in the sense of the present invention generally contain one or more medicaments in an effective concentration.
  • medicaments in an effective concentration.
  • cosmetic or topical dermatological compositions within the meaning of the present invention, depending on their structure, can be used, for example, as skin protection cream, cleansing milk, sunscreen lotion, nutritional cream, day or night cream, etc. It may be possible and advantageous to use the compositions according to the invention as a basis for pharmaceuticals Use wording.
  • compositions according to the invention are also advantageous.
  • Cosmetic and dermatological preparations which are in the form of a sunscreen are also favorable.
  • these preferably additionally contain at least one UVA filter substance and / or at least one UVB filter substance and / or at least one inorganic pigment.
  • UV-A or UV-B filter substances are usually incorporated into day creams.
  • Preparations according to the invention can 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, in particular 1 to 6% by weight, based on the total weight of the preparations.
  • the UVB filters can be oil-soluble or water-soluble.
  • oil-soluble substances e.g. to call:
  • 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;
  • Esters of benzalmalonic acid preferably 4-methoxybenzalmalonic acid di (2-ethylhexyl) ester;
  • 2-phenylbenzimidazole-5-sulfonic acid and its salts for example sodium, potassium or triethanolammonium salts
  • Sulfonic acid derivatives of benzophenones preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and its salts;
  • Sulfonic acid derivatives of 3-benzylidene camphor e.g. 4- (2-oxo-3-bornylidene-methyl) benzenesulfonic acid, 2-methyl-5- (2-oxo-3-bomylidene-methyl) sulfonic acid and their
  • UVB filters which can be used according to the invention, is of course not intended to be limiting.
  • UVA filters in the preparations according to the invention, which are usually contained in cosmetic and / or dermatological preparations.
  • Such filter 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. Preparations containing these combinations are also the subject of the invention.
  • the same amounts of UVA filter substances that were mentioned for UVB filter substances can be used.
  • Cosmetic and / or dermatological preparations in the sense of the present invention can also contain inorganic pigments which are usually used in cosmetics to protect the skin from UV rays. These are oxides of titanium, zinc, iron, zirconium, silicon, manganese, aluminum, cerium and mixtures thereof, as well as modifications in which the oxides are the active agents. It is particularly preferred to use pigments based on titanium dioxide. The amounts given for the above combinations can be used.
  • the cosmetic and dermatological preparations according to the invention can contain cosmetic active ingredients, auxiliaries and / or additives, as are usually used in such preparations, for example antioxidants, preservatives, bactericides, perfumes, substances for preventing foaming, dyes, pigments, the coloring effect have thickeners, surface-active substances, emulsifiers, softening, moisturizing and / or moisturizing substances, fats, oils, waxes or other usual components of a cosmetic or dermatological formulation such as alcohols, Polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
  • cosmetic active ingredients for example antioxidants, preservatives, bactericides, perfumes, substances for preventing foaming, dyes, pigments, the coloring effect have thickeners, surface-active substances, emulsifiers, softening, moisturizing and / or moisturizing substances, fats, oils, waxes or other usual components of a cosmetic or dermatological formulation such as alcohols, Polyols
  • batyl alcohol ⁇ -octadecylglyceryl ether
  • selachyl alcohol ⁇ -9-octadecenylglyceryl ether
  • chimyl alcohol ⁇ -hexadecylglyceryl ether
  • bisabolol ⁇ -hexadecylglyceryl ether
  • antioxidants it is also advantageous to add customary antioxidants to the preparations for the purposes of the present invention. According to the invention, all the antioxidants suitable or customary for cosmetic and / or dermatological applications can be used as favorable antioxidants.
  • the antioxidants are advantageously selected from the group consisting of amino acids (eg glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (eg urocanic acid) and their derivatives, peptides such as D, L-carnosine, D-carnosine, L- Camosin and its derivatives (e.g. anserine), carotenoids, carotenes (e.g. ⁇ -carotene, ß-carotene, ⁇ -lycopene) and their derivatives, chlorogenic acid and their derivatives, aurothioglucose, propylthiouracil and other thiols (e.g.
  • amino acids eg glycine, histidine, tyrosine, tryptophan
  • imidazoles eg urocanic acid
  • peptides such as D, L-carnosine, D-carnosine, L- Camosin and its derivatives (e
  • thioredoxin glutathione, cysteine, cystine , Cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl, ⁇ -linoleyl, cholesterol and glyceryl esters) as well as their salts, dilaurylthiodipropionate, distearylthiodipropionate, thiodipropionic acid and their derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) as well as sulfoximine compounds (for example buthioninsulfoximines, homocystinsulfoximine, buthioninsulfones), pentathione sulfoximine, penta-, hexa-, hexa-, hexa- very low vert conventional dosages (eg
  • the amount of the antioxidants (one or more compounds) in the preparations is preferably 0.001 to 30% by weight, particularly preferably 0.05 to 20% by weight, in particular 1 to 10% by weight, based on the total weight of the preparation ,
  • vitamin E and / or its derivatives represent the antioxidant (s)
  • Preparations according to the present invention can also be used as a basis for cosmetic or dermatological deodorants or antiperspirants.
  • All active ingredients common to deodorants or antiperspirants can be used advantageously, for example odor maskers such as the common perfume components, odor absorbers, for example the layered silicates described in patent application DE-P 40 09 347, of which in particular montmorillonite, kaolinite, llite, beidellite, nontronite, Sa. - ponite, hectorite, bentonite, smectite, furthermore, for example, zinc salts of ricinoleic acid.
  • odor maskers such as the common perfume components
  • odor absorbers for example the layered silicates described in patent application DE-P 40 09 347, of which in particular montmorillonite, kaolinite, llite, beidellite, nontronite, Sa. - ponite, hectorite, bentonite, smectite, further
  • Germ-inhibiting agents are also suitable for being incorporated into the preparations according to the invention.
  • advantageous substances are 2,4,4'-trichloro-2'-hydroxydiphenyl ether (irgasane), 1,6-di- (4-chlorophenylbiguanido) hexane (chlorhexidine), 3,4,4'-tri- chlorocarbanilide, quaternary ammonium compounds, clove oil, mint oil, thyme oil, triethyl citrate, farnesol (3,7,11-trimethyl-2,6,10-dodecatrien-1-ol) and those described in the patent documents DE-37 40 186, DE-39 38 140, DE-42 04 321, DE-42 29 707, DE-43 09 372, DE-44 11 664, DE-195 41 967, DE-195 43 695, DE-195 43 696, DE- 195 47 160, DE-196 02 108, DE-196 02 110, DE-196 02 111, DE-196 31
  • Sodium hydrogen carbonate can also be used advantageously.
  • the amount of such active substances (one or more compounds) in the preparations according to the invention is preferably 0.001 to 30% by weight, particularly preferably 0.05-20% by weight, in particular 1-10% by weight, based on the Total weight of the preparation.
  • the water phase of the cosmetic preparations in the sense of the present invention can also have a gel character which, in addition to an effective content of the substances used according to the invention and solvents usually used for this purpose, preferably water, also further organic thickeners, e.g. Gum arabic, xanthan gum, sodium alginate, starch and starch derivatives (e.g. distarch phosphate), cellulose, cellulose derivatives, preferably methyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose or inorganic thickeners, e.g. B.
  • organic thickeners e.g. Gum arabic, xanthan gum, sodium alginate, starch and starch derivatives (e.g. distarch phosphate)
  • cellulose, cellulose derivatives preferably methyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose
  • aluminum silicates such as organically modified or unmodified hectorites, bentonites, or the like, or a mixture of polyethylene glycol and polyethylene glycol stearate or distearate.
  • the thickener is in the gel e.g. in an amount between 0.1 and 30% by weight, preferably between 0.5 and 15% by weight.
  • cationic emulsifiers such as, in particular, quaternary surfactants.
  • Quaternary surfactants contain at least one N atom, which is linked 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 according to the invention can furthermore preferably be selected from the group of the quaternary ammonium compounds, in particular benzyltrialkylammonium chlorides or bromides, such as, for example, benzyldimethylstearylammonium chloride, and furthermore alkyltrialkylammonium salts, for example, for example cetyltrimethylammonium chloride or bromide, or alkyldimbromide, alkylammonium bromide or dimethylammonium chlorides or bromides, alkylamidethyltrimethylammonium ether sulfates, alkylpyridinium salts, for example lauryl or cetylpyrimidinium chloride, imidazoline derivatives and compounds with a cationic character such as amine oxides, for example alkyldimethylamineoxides or alkylaminoethyldimethylamine oxides.
  • Cetyltrimethylammonium salts are particularly advantageous to use. It is also advantageous to use cationic polymers (for example Jaguar® C 162 [hydroxypropyl guar hydroxypropyltrimonium chloride) or modified magnesium aluminum silicates (for example Quatemium-18-hectorite, which is available, for example, from Rheox under the trade name Bentone® 38) or stearalkonium hectorite, which is available, for example, under the trade name Softisan® Gel from Hüls AG).
  • cationic polymers for example Jaguar® C 162 [hydroxypropyl guar hydroxypropyltrimonium chloride) or modified magnesium aluminum silicates (for example Quatemium-18-hectorite, which is available, for example, from Rheox under the trade name Bentone® 38) or stearalkonium hectorite, which is available, for example, under the trade name Softisan® Gel from Hüls AG).
  • Preparations according to the invention can advantageously also contain oil thickeners in order to improve the tactile properties of the emulsion and the stick consistency.
  • Oil thickeners for the purposes of the present invention are, for example, other solids, such as, for. B. hydrophobic silicon oxides of the type Aerosil®, which are available from Degussa AG.
  • Aerosil® grades are Aerosil® OX50, Aerosil® 130, Aerosil® 150, Aerosil® 200, Aerosil® 300, Aerosil® 380, Aerosil® MOX 80, Aerosil® MOX 170, Aerosil® COK 84, Aerosil® R 202 , Aerosil® R 805, Aerosil® R 812, Aerosil® R 972, Aerosil® R 974 and / or Aerosil® R976.
  • metal soaps i.e. the salts of higher fatty acids with the exception of the alkali salts
  • oil thickeners for the purposes of the present invention, such as, for example, aluminum stearate, zinc stearate and / or magnesium stearate.
  • amphoteric or zwitterionic surfactants e.g. cocoamidopropyl betaine
  • moisturizers e.g. betaine
  • Amphoteric surfactants to be used advantageously are, for example, acyl / dialkylethylenediamine, for example sodium acylamphoacetate, disodium acylamphodipropionate, disodium alkylamphodiacetate, sodium acylamphohydroxypropylsulfonate, disodium acylamphodiacetate and sodium triumacylamphopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropylate aminopropyl aminopropylate aminopropyl aminopropylate, for example
  • the amount of surface-active or surface-active substances (one or more compounds) in the preparations according to the invention is preferably 0.001 to 30% by weight, particularly preferably 0.05-20% by weight, in particular 1-10% by weight. %, based on the total weight of the preparation.
  • An astonishing property of the preparations according to the invention is that they are very good vehicles for cosmetic or dermatological active ingredients in the skin, preferred active ingredients being the aforementioned antioxidants, which can protect the skin against oxidative stress.
  • the active ingredients can also be selected very advantageously from the group of lipophilic active ingredients, in particular from the following group:
  • vitamin F essential fatty acids
  • ® ® for example Purcellinöl, Eucerit and Neocerit.
  • the active ingredient (s) are particularly advantageously selected from the group of NO synthase inhibitors, in particular if the preparations according to the invention are intended 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 ,
  • the preferred NO synthase inhibitor is nitroarginine.
  • the active ingredient (s) are also advantageously selected from the group comprising catechins and bile esters of catechins and aqueous or organic extracts from plants or parts of plants which contain catechins or bile esters of catechins, such as, for example, the leaves of the Theaceae plant family, in particular of the species Camellia sinensis (green tea).
  • catechins and bile esters of catechins such as, for example, the leaves of the Theaceae plant family, in particular of the species Camellia sinensis (green tea).
  • Their are particularly advantageous typical ingredients such as polyphenols or catechins, caffeine, vitamins, sugar, minerals, amino acids, lipids).
  • Catechins are a group of compounds which are to be regarded as hydrogenated flavones or anthocyanidins and derivatives of "catechins” (catechol, 3,3 ', 4', 5,7-flavanpentaol, 2- (3,4- Dihydroxyphenyl) -chroman-3,5,7-triol)
  • Catatechin ((2R, 3R) -3,3 ', 4', 5,7-flavanpentaol) is also an advantageous active substance in the sense of the present invention.
  • Plant extracts containing catechins in particular extracts of green tea, such as. B. extracts from leaves of the plants of the species Camellia spec, especially the teas Camellia sinenis, C. .assamica, C. taliensis or C. irrawadiensis and crosses of these with, for example, Camellia japonica
  • Preferred active substances are also polyphenols or catechins from the group (-) - catechin, (+) - catechin, (-) - catechin gallate, (-) - Ga ⁇ locatechin gallate, (+) - epicatechin, (-) - epicatechin, (-) - epicatechin gallate, (-) - epigallocatechin, (-) - epigallocatechin gallate.
  • Flavon and its derivatives are advantageous active substances in the sense of the present invention. They are characterized by the following basic structure (substitution positions specified):
  • flavones usually occur in glycosidated form.
  • the flavonoids are preferably chosen from the group of substances of the generic structural formula
  • Z ⁇ to Z 7 are independently selected from the group H, OH, alkoxy and hydroxyalkoxy, where the alkoxy or hydroxyalkoxy groups can be branched and unbranched and can have 1 to 18 carbon atoms, and wherein Gly is selected from the group of mono- and oligoglycoside residues.
  • the flavonoids can also be advantageously selected from the group of substances of the generic structural formula
  • Z ⁇ to Z 6 are selected independently of one another from the group H, OH, alkoxy and hydroxyalkoxy, where the alkoxy or hydroxyalkoxy groups are branched and unbranched and can have 1 to 18 carbon atoms, and where Gly is selected from the group of mono- and oligoglycoside residues.
  • Such structures can preferably be selected from the group of substances of the generic structural formula
  • Glyi, Gly 2 and Gly 3 independently of one another represent monoglycoside residues or. Gly 2 or Gly 3 can also represent, individually or together, saturations by hydrogen atoms.
  • Glyi, Gly 2 and Gly 3 are preferably selected independently of one another from the group of the hexosyl radicals, in particular the rhamnosyl radicals and glucosyl radicals.
  • hexosyl residues for example allosyl, altrosyl, galactosyl, gulosyl, idosyl, mannosyl and talosyl, can also be used advantageously if appropriate. It can also be advantageous according to the invention to use pentosyl residues.
  • Z ⁇ to Z 5 are advantageously selected independently of one another from the group H, OH, methoxy, ethoxy and 2-hydroxyethoxy, and the flavone glycosides have the structure
  • Glyi, Gly 2 and Gly 3 independently of one another represent monoglycoside residues or. Gly 2 or Gly 3 can also represent, individually or together, saturations by hydrogen atoms.
  • Glyi, Gly 2 and Gly 3 are preferably selected independently of one another from the group of the hexosyl radicals, in particular the rhamnosyl radicals and glucosyl radicals.
  • hexosyl residues for example allosyl, altrosyl, galactosyl, gulosyl, idosyl, mannosyl and talosyl, can also be used advantageously if appropriate. It can also be advantageous according to the invention to use pentosyl residues.
  • flavone glycoside (s) from the group ⁇ -glucosyl rutin, ⁇ -glucosyl myrcetin, ⁇ -glucosyl isoquercitrin, ⁇ -glucosyl iso quercetin and ⁇ -glucosyl quercitrin.
  • ⁇ -glucosylrutin is particularly preferred.
  • Naringin (aurantiin, naringenin-7-rhamnoglucoside), hesperidin (3 ', 5,7-trihydroxy-4'-methoxyflavanon-7-rutinoside, hesperidoside, hesperetin-7-o-rutinoside) are also advantageous according to the invention.
  • Rutin (3,3 ', 4', 5,7-pentahydroxyflyvon-3-rutinosid, quercetin-3-rutinosid, sophorin, birutan, rutabion, taurutin, phytomelin, melin), troxerutin (3,5-dihydroxy-3 ', 4 ', 7-tris (2-hydroxyethoxy) flavone-3- (6-O- (6-deoxy- ⁇ -L-mannopyranosyl) -ß-D-glucopyranoside)), monoxurutin (3,3', 4 ', 5-tetrahydroxy-7- (2-hydroxyethoxy) flavon-3- (6-O- (6-deoxy- ⁇ -L-mannopyrano-syl) -ß-D-glucopyranoside)), dihydrorobinetin (3, 3 ', 4', 5 ', 7-pentahydroxyflavanone), taxifolin (3,3', 4 ', 5,7-penta
  • the active ingredient (s) from the group of ubiquinones and plastoquinones.
  • Coenzyme Q10 which is characterized by the following structural formula, is particularly advantageous:
  • Creatine and / or creatine derivatives are also preferred active substances for the purposes of the present invention. Creatine is characterized by the following structure:
  • Preferred derivatives are creatine phosphate and creatine sulfate, creatine acetate, creatine ascorbate and the derivatives esterified on the carboxyl group with mono- or polyfunctional alcohols.
  • acyl-carnitine which is selected from the group of substances of the following general structural formula %
  • R is selected from the group of branched and unbranched alkyl radicals having up to 10 carbon atoms are advantageous active substances in the sense of the present invention.
  • Propionylcarnitine and in particular acetylcamitine are preferred.
  • Both entantiomers (D- and L-form) can be used advantageously for the purposes of the present invention. It can also be advantageous to use any mixture of enantiomers, for example a racemate of D and L form.
  • the list of the active substances or combinations of active substances mentioned which can be used in the preparations according to the invention is of course not intended to be limiting.
  • the active ingredients can be used individually or in any combination with one another.
  • the amount of such active substances (one or more compounds) in the preparations according to the invention is preferably 0.001 to 30% by weight, particularly preferably 0.05-20% by weight, in particular 1-10% by weight, based on the Total weight of the preparation.
  • Preparations according to the invention are produced under the conditions familiar to the person skilled in the art.
  • the components of the oil phase or the water phase are combined separately and heated, and then with stirring and, particularly advantageously, with homogenization, very particularly advantageously with stirring with medium to high energy input, advantageously with the aid of a gear rim dispersion machine with a speed of up to a maximum of 10,000 rpm, preferably from 2500 to 7700 rpm, combined with one another.
  • Example 1 (O / W cream):
  • the constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization, with the aid of a gear rim dispersing machine at a speed of 5000 rpm.
  • the constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 7000 rpm.
  • the constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 3200 rpm.
  • the components of the oil phase or the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 5000 rpm.
  • Titanium dioxide 2.50
  • Example 7 (O / W lotion):
  • the constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 3000 rpm.
  • the constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 5,200 rpm.
  • the components of the oil phase or the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 3500 rpm.

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Abstract

The invention relates to cosmetic or dermatological preparations in the form of an O/W emulsion containing the following: (I) Between 1 and 5 wt %, in relation to the total weight of the preparations, of one or more substances, selected from the group of sterols and branched or unbranched, saturated or unsaturated C12-C40 fatty acids. (II) Between 0.1 and 1.5 wt %, in relation to the total weight of the preparations, of one or more monoesters, sesquiesters, diesters or triesters of saturated or unsaturated, straight-chain or branched-chain fatty acids of glycerol and/or propylene glycol and/or glycol, comprising a chain length of C14-C40. (III) Between 0.1 and 1.5 wt. %, in relation to the total weight of the preparation of one or more monoesters, sesquiesters, diesters or triesters of saturated or unsaturated, straight-chain or branched-chain fatty acids of sorbitan, comprising a chain length of C14-C40 and optionally with a polyethoxylation degree of 0-100. (IV) Between 0.1 and 1.5 wt. %, in relation to the total weight of the preparations, of one or more ethoxylated fatty acid esters, comprising fatty acids with a chain length of C12-C40 and an ethoxylation degree of up to 100, preferably of between 5 and 100. (V) Between 0.5 and 7 wt. %, in relation to the total weight of the preparations, of one or more fatty alcohols, selected from the group of branched and unbranched, saturated and unsaturated alkyl alcohols comprising between 12 and 40 carbon atoms. According to the invention, (VI) the ratio from (II):(III):(IV) is preferably selected as a: b: c, whereby a, b and c independently of one another represent rational numbers from 1 to 5, preferably from 1 to 3, (VII) the ratio from (II)+(III)+(IV) to (V) lies preferably in the range 5:1 to 1:5, (VIII) the sum of (I), (II), (III), (IV) and (V) amounts to a maximum 25 wt. %, (IX) and the preparations preferably lie in a pH range of 3.5-8.0, preferably having pH values of 4.5-6.5.

Description

Beschreibung description
Kosmetische und dermatologische Zubereitungen in Form von O/W-Emulsionen mit einem Gehalt an Sterinen und/oder Cι2-C40-FettsäurenCosmetic and dermatological preparations in the form of O / W emulsions containing sterols and / or C 2 -C 40 fatty acids
Die vorliegende Erfindung betrifft kosmetische und dermatologische Emulsionen, insbesondere hautpflegende kosmetische und dermatologische Emulsionen. In einer vorteilhaften Ausführungsform betrifft die vorliegende Erfindung eine Anwendung, welche es erlaubt, die Stabilität von fettsäurehaltigen Zubereitungen, insbesondere Emulsionen, bevorzugt von O/W-Emulsionen, zu steigern.The present invention relates to cosmetic and dermatological emulsions, in particular skin-care cosmetic and dermatological emulsions. In an advantageous embodiment, the present invention relates to an application which makes it possible to increase the stability of preparations containing fatty acids, in particular emulsions, preferably O / W emulsions.
Die Haut ist das größte Organ des Menschen. Unter ihren vielen Funktionen (beispielsweise zur Wärmeregulation und als Sinnesorgan) ist die Barrierefunktion, die das Austrocknen der Haut (und damit letztlich des gesamten Organismus) verhindert, die wohl wichtigste. Gleichzeitig wirkt die Haut als Schutzeinrichtung gegen das Eindringen und die Aufnahme von außen kommender Stoffe. Bewirkt wird diese Barrierefunktion durch die Epidermis, welche als äußerste Schicht die eigentliche Schutzhülle gegenüber der Umwelt bildet. Mit etwa einem Zehntel der Gesamtdicke ist sie gleichzeitig die dünnste Schicht der Haut.The skin is the largest human organ. Among its many functions (for example for heat regulation and as a sensory organ), the most important is the barrier function that prevents the skin (and ultimately the entire organism) from drying out. At the same time, the skin acts as a protective device against the penetration and absorption of substances coming from outside. This barrier function is brought about by the epidermis, which as the outermost layer forms the actual protective cover against the environment. At around a tenth of the total thickness, it is also the thinnest layer of the skin.
Die Epidermis ist ein stratifiziertes Gewebe, in dem die äußere Schicht, die Hornschicht (Stratum corneum), den für die Barrierefunktion bedeutenden Teil darstellt. Das heute in der Fachwelt anerkannte Hautmodell von Elias (P. M. Elias, Structure and Function of the Stratum Corneum Permeability Barrier, Drug Dev. Res. 13, 1988, 97-105) beschreibt die Hornschicht als Zwei-Komponenten-System, ähnlich einer Ziegelsteinmauer (Ziegelstein-Mörtel- Modell). In diesem Modell entsprechen die Hornzellen (Korneozyten) den Ziegelsteinen, die komplex zusammengesetzte Lipidmembran in den Interzellularräumen entspricht dem Mörtel. Dieses System stellt im wesentlichen eine physikalische Barriere gegen hydrophile Substanzen dar, kann aber aufgrund seiner engen und mehrschichtigen Struktur gleichermaßen auch von lipophilen Substanzen nur schwer passiert werden. Die vorliegende Erfindung betrifft in einer besonderen Ausführungsform kosmetische oder pharmazeutische Zubereitungen mit vermindertem Klebrigkeitsgefühl, Verfahren zu ihrer Herstellung sowie die Verwendung von Wirkstoffen zur Herabminderung des Klebrigkeitsge- fühles kosmetischer Zubereitungen.The epidermis is a stratified tissue in which the outer layer, the horny layer (stratum corneum), is the important part for the barrier function. The skin model of Elias (PM Elias, Structure and Function of the Stratum Corneum Permeability Barrier, Drug Dev. Res. 13, 1988, 97-105), which is recognized by experts today, describes the horny layer as a two-component system, similar to a brick wall ( Brick-mortar model). In this model, the horny cells (corneocytes) correspond to the bricks, the complex lipid membrane in the intercellular spaces corresponds to the mortar. This system essentially represents a physical barrier against hydrophilic substances, but due to its narrow and multilayer structure it is equally difficult for lipophilic substances to pass through. In a particular embodiment, the present invention relates to cosmetic or pharmaceutical preparations with a reduced feeling of stickiness, to processes for their preparation and to the use of active ingredients for reducing the stickiness of cosmetic preparations.
Außer ihrer Barrierewirkung gegen externe chemische und physikalische Einflüsse tragen die epidermalen Lipide auch zum Zusammenhalt der Homschicht bei und haben Einfluß auf die Hautglätte. Im Gegensatz zu den Talgdrüsenlipiden, die keinen geschlossenen Film auf der Haut ausbilden, sind die epidermalen Lipide über die gesamte Homschicht verteilt.In addition to their barrier effect against external chemical and physical influences, the epidermal lipids also contribute to the cohesion of the homolayer and influence the smoothness of the skin. In contrast to the sebum lipids, which do not form a closed film on the skin, the epidermal lipids are distributed over the entire homolayer.
Das äußerst komplexe Zusammenwirken der feuchtigkeitsbindenden Substanzen und der Lipide der oberen Hautschichten ist für die Regulation der Hautfeuchte sehr wichtig. Daher enthalten Kosmetika in der Regel, neben ausgewogenen Lipidabmischungen und Wasser, wasserbindende Substanzen.The extremely complex interaction of the moisture-binding substances and the lipids of the upper skin layers is very important for the regulation of skin moisture. Therefore, in addition to balanced lipid blends and water, cosmetics usually contain water-binding substances.
Neben der chemischen Zusammensetzung ist jedoch auch das physikalische Verhalten dieser Substanzen von Bedeutung. Daher ist die Entwicklung von sehr gut bioverträglichen E- mulgatoren bzw. Tensiden wünschenswert. Damit formulierte Produkte unterstützen die flüssigkristalline Organisation der Interzellularlipide des Stratum Corneums und verbessern so die Barriereeigenschaften der Homschicht. Besonders vorteilhaft ist es, wenn deren Molekülbestandteile aus natürlicherweise in der Epidermis vorkommenden Substanzen bestehen.In addition to the chemical composition, the physical behavior of these substances is also important. Therefore, the development of very well biocompatible emulsifiers or surfactants is desirable. Products formulated in this way support the liquid-crystalline organization of the intercellular lipids of the stratum corneum and thus improve the barrier properties of the homolayer. It is particularly advantageous if their molecular components consist of substances that occur naturally in the epidermis.
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, Elektrolyte) gestärkt oder wiederhergestellt wird.Cosmetic skin care is primarily understood to mean that the natural function of the skin as a barrier against environmental influences (e.g. dirt, chemicals, microorganisms) and against the loss of the body's own substances (e.g. 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.
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 Rege- nerationsvermögen nicht ausreicht. Außerdem sollen Hautpflegeprodukte vor Umwelteinflüssen, insbesondere vor Sonne und Wind, schützen und die Hautalterung verzögern.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 rain generation capacity is not sufficient. In addition, skin care products are intended to protect against environmental influences, particularly sun and wind, and to delay skin aging.
Medizinische topische Zusammensetzungen enthalten in der Regel ein oder mehrere Medikamente in wirksamer Konzentration. Der Einfachheit 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 usually contain one or more drugs in 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.
Übliche kosmetische Darreichungsformen sind Emulsionen. Darunter versteht man im allgemeinen ein heterogenes System aus zwei miteinander nicht oder nur begrenzt mischbaren Flüssigkeiten, die üblicherweise als Phasen bezeichnet werden. Die eine liegt dabei in Form von Tröpfchen vor (dispere oder innere Phase), während die andere Flüssigkeit eine kontinuierliche (kohärente oder innere Phase ) bildet. Seltenere Darreichungsformen sind multiple Emulsionen, also solche, welche in den Tröpfchen der dispergierten (oder diskontinuierlichen) Phase ihrerseits Tröpfchen einer weiteren dispergierten Phase enthalten, z.B. W/O/W- Emulsionen und O/W/O-Emulsionen.Common cosmetic dosage forms are emulsions. This is generally understood to mean a heterogeneous system composed of two liquids which are immiscible or only miscible with one another, which are usually referred to as phases. One is in the form of droplets (dispere or inner phase), while the other liquid forms a continuous (coherent or inner phase). More rare forms of administration are multiple emulsions, i.e. those which themselves contain droplets of a further dispersed phase in the droplets of the dispersed (or discontinuous) phase, e.g. W / O / W emulsions and O / W / O emulsions.
Neuere Erkenntnisse führten in letzter Zeit zu einem besseren Verständnis praxisrelevanter kosmetischer Emulsionen. Dabei geht man davon aus, daß die im Überschuß eingesetzten Emulgatorgemische iamellare flüssigkristalline Phasen bzw. kristalline Gelphasen ausbilden. In der Gelnetzwerktheorie werden Stabilität und physikochemische Eigenschaften solcher Emulsionen auf die Ausbildung von viskoelastischen Gelnetzwerden zurückgeführt.Recent findings have led to a better understanding of practical cosmetic emulsions. It is assumed that the emulsifier mixtures used in excess form iamellar liquid-crystalline phases or crystalline gel phases. In gel network theory, the stability and physicochemical properties of such emulsions are attributed to the formation of viscoelastic gel networks.
Um die Metastabilität von Emulsionen gewährleisten zu können, sind in der Regel grenzflächenaktive Substanzen, also Emulgatoren, nötig. An sich ist die Verwendung der üblichen kosmetischen Emulgatoren völlig unbedenklich. Dennoch können Emulgatoren, wie letztlich jede chemische Substanz, im Einzelfalle allergische oder auf Überempfindlichkeit des Anwenders beruhende Reaktionen hervorrufen. So ist bekannt, daß bei manchen besonders empfindlichen Personen bestimmte Lichtdermatosen durch gewisse Emulgatoren und gleichzeitige Einwirkung von Sonnenlicht ausgelöst werden.In order to guarantee the metastability of emulsions, surface-active substances, i.e. emulsifiers, are generally necessary. In itself, the use of the usual cosmetic emulsifiers is completely harmless. Nevertheless, emulsifiers, like any chemical substance, can cause allergic or hypersensitive reactions in individual cases. It is known, for example, that in certain particularly sensitive people certain light dermatoses are triggered by certain emulsifiers and simultaneous exposure to sunlight.
Es ist möglich, emulgatorfreie Zubereitungen herzustellen, welche beispielsweise in einer wäßrigen Phase dispergierte Öltröpfchen, ähnlich einer O/W-Emulsion, aufweisen. Voraus- setzung dafür kann sein, daß die kontinuierliche wäßrige Phase ein die dispergierte Phase stabilisierendes Gelgerüst aufweist und andere Umstände mehr. Solche Systeme werden gelegentlich Hydrodispersionen oder Oleodispersionen genannt, je nachdem, welches die disperse und welches die kontinuierliche Phase darstellt.It is possible to prepare emulsifier-free preparations which, for example, have oil droplets dispersed in an aqueous phase, similar to an O / W emulsion. Ahead- The reason for this may be that the continuous aqueous phase has a gel structure which stabilizes the dispersed phase and other circumstances. Such systems are sometimes called hydrodispersions or oleodispersions, depending on which is the disperse phase and which is the continuous phase.
Es ist für die kosmetische Galenik aber weder nötig noch möglich, auf Emulgatoren ganz zu verzichten, zumal eine gewisse Auswahl an besonders milden Emulgatoren existiert. Allerdings besteht ein Mangel des Standes der Technik an einer befriedigend großen Vielfalt solcher Emulgatoren, welche dann auch das Anwendungsspektrum entsprechend milder und hautverträglicher kosmetischer Zubereitungen deutlich verbreitern würde.However, it is neither necessary nor possible for cosmetic galenics to completely dispense with emulsifiers, especially since there is a certain selection of particularly mild emulsifiers. However, there is a lack of the prior art in a satisfactorily large variety of such emulsifiers, which would then also significantly broaden the range of applications corresponding to mild and skin-compatible cosmetic preparations.
So war eine Aufgabe der vorliegenden Erfindung, kosmetische bzw. dermatologische Zubereitungen mit hervorragenden hautpflegenden Eigenschaften zur Verfügung zu stellen.It was an object of the present invention to provide cosmetic or dermatological preparations with excellent skin-care properties.
Ferner war eine Aufgabe der vorliegenden Erfindung, Zubereitungen zur Verfügung zu stellen, welche den Zustand der Haut deutlich verbessern, insbesondere die Hautrauhigkeit vermindern.A further object of the present invention was to provide preparations which significantly improve the condition of the skin, in particular reduce the roughness of the skin.
Es ist zwar bekannt, durch Hinzufügen bestimmter Substanzen, beispielsweise einiger ausgewählter Puderrohstoffe, insbesondere Talkum, ein Klebrigkeitsgefühl oder auch Schmie- rigkeitsgefühl zu reduzieren. Davon abgesehen, daß dieses nur selten vollständig gelingt, wird durch einen solchen Zusatz auch die Viskosität des betreffenden Produktes verändert und die Stabilität verringert.It is known to reduce a feeling of stickiness or also a feeling of slowness by adding certain substances, for example some selected powder raw materials, in particular talc. Apart from the fact that this is rarely completely successful, such an addition also changes the viscosity of the product in question and reduces the stability.
Aufgabe war daher, all diesen den Nachteilen des Standes der Technik Abhilfe zu schaffen. Insbesondere sollten Produkte mit verringerter Klebrigkeit bzw. Schmierigkeit zur Verfügung gestellt werden. Produkte auf dem Gebiete der pflegenden Kosmetik, der dekorativen Kosmetik und der pharmakologischen Galenik sollten gleichermaßen von den geschilderten Nachteilen des Standes der Technik befreit werden.The task was therefore to remedy all of these disadvantages of the prior art. In particular, products with reduced stickiness or greasiness should be made available. Products in the fields of care cosmetics, decorative cosmetics and pharmacological galenics should equally be freed from the disadvantages of the prior art described.
Weiterhin war es eine Aufgabe der Erfindung, kosmetische Grundlagen für kosmetische Zubereitungen zu entwickeln, die sich durch gute Hautverträglichkeit auszeichnen. Bekannte kosmetische Zubereitungen sind sogenannte „Stearatemulsionen", also solchen, in welchen Stearinsäure und/oder Palmitinsäure bzw. Alkalisalze der Stearinsäure und/oder der Palmitinsäure als Emulgator wirksam sind. Diese Zubereitungen können vorteilhaft als OΛ/V- Emulsionen vorliegen und zeichnen sich durch gutes Hautgefühl und sehr gute Hautpflegeleistung aus. Nachteilig ist jedoch, daß Fettsäuren in einem pH-Bereich von 3,5 - 8,0 zur Kristallisation neigen (insbesondere in einem pH-Bereich unterhalb 7,0), wodurch das angenehme Hautgefühl, die Hautpflegeleistung sowie das äußere Erscheinungsbild einer entsprechenden Zubereitung stark beeinträchtigt werden.Furthermore, it was an object of the invention to develop cosmetic bases for cosmetic preparations which are notable for good skin tolerance. Known cosmetic preparations are so-called “stearate emulsions”, that is to say those in which stearic acid and / or palmitic acid or alkali metal salts of stearic acid and / or palmitic acid are effective as emulsifiers. These preparations can advantageously be present as O / V emulsions and are notable for good It is disadvantageous, however, that fatty acids tend to crystallize in a pH range from 3.5 to 8.0 (in particular in a pH range below 7.0), so that the pleasant skin feel, the skin care performance and the external appearance of a corresponding preparation can be severely impaired.
Natürlich ist dem Fachmann eine Vielzahl von Möglichkeiten bekannt, stabile O/W- Zubereitungen zur kosmetischen oder dermatologischen Anwendung zu formulieren, beispielsweise in Form von Cremes und Salben, die im Bereich von Raum- bis Hauttemperatur streichfähig sind, oder als Lotionen und Milche, die in diesem Temperaturbereich eher fließfähig sind. Der Stand der Technik kennt allerdings nur wenige Formulierungen, die so dünnflüssig sind, daß sie beispielsweise sprühbar wären.Of course, a multitude of possibilities is known to the person skilled in the art to formulate stable O / W preparations for cosmetic or dermatological use, for example in the form of creams and ointments which are spreadable in the range from room temperature to skin temperature, or as lotions and milks tend to flow in this temperature range. However, the prior art knows only a few formulations which are so thin that they would be sprayable, for example.
Zudem haben dünnflüssige Zubereitungen des Standes der Technik häufig den Nachteil, daß sie instabil, auf einen engen Anwendungsbereich oder eine begrenzte Einsatzstoffauswahl begrenzt sind. Dünnflüssige Produkte, in denen beispielsweise stark polare Öle - wie die in handelsüblichen Produkten sonst häufig verwendeten Pflanzenöle - ausreichend stabilisiert sind, gibt es daher zur Zeit auf dem Markt nicht.In addition, low-viscosity preparations of the prior art frequently have the disadvantage that they are unstable, are limited to a narrow application range or a limited choice of starting materials. Low-viscosity products, in which, for example, strongly polar oils - such as the vegetable oils commonly used in commercial products - are sufficiently stabilized, are currently not available on the market.
Unter dem Begriff „Viskosität" versteht man die Eigenschaft einer Flüssigkeit, der gegenseitigen laminaren Verschiebung zweier benachbarter Schichten einen Widerstand (Zähigkeit, innere Reibung) entgegenzusetzen. Man definiert heute diese sogenannte dynamische Viskosität nach η=t/D als das Verhältnis der Schubspannung zum Geschwindigkeitsgradienten senkrecht zur Strömungsrichtung. Für newtonsche Flüssigkeiten ist η bei gegebener Temperatur eine Stoffkonstante mit der Sl-Einheit Pascalsekunde (Pa s).The term "viscosity" means the property of a liquid to oppose the mutual laminar displacement of two adjacent layers with resistance (toughness, internal friction). Today, this so-called dynamic viscosity according to η = t / D is defined as the ratio of the shear stress to the velocity gradient perpendicular to the direction of flow For Newtonian liquids η is a substance constant with the Sl unit Pascal second (Pa s) at a given temperature.
Der Quotient v=η/p aus der dynamischen Viskosität η und der Dichte p der Flüssigkeit wird als kinematische Viskosität v bezeichnet und in der Sl-Einheit m2/s angegeben.The quotient v = η / p from the dynamic viscosity η and the density p of the liquid is referred to as the kinematic viscosity v and is given in the SI unit m 2 / s.
Als Fluidität (φ) bezeichnet man den Kehrwert der Viskosität (φ=1/η). Bei Salben und dergleichen wird der Gebrauchswert unter anderem mitbestimmt von der sogenannten Zügig- keit. Unter der Zügigkeit einer Salbe oder Salbengrundlage oder dergleichen versteht man deren Eigenschaft, beim Abstechen verschieden lange Fäden zu ziehen; dementsprechend unterscheidet man kurz- und langzügige Stoffe.Fluidity (φ) is the reciprocal of viscosity (φ = 1 / η). In the case of ointments and the like, the use value is determined, among other things, by the so-called ness. The speed of an ointment or ointment base or the like means its property of pulling threads of different lengths when tapping; accordingly, a distinction is made between short and long-lasting fabrics.
Während die graphische Darstellung des Fließverhaltens Newtonscher Flüssigkeiten bei gegebener Temperatur eine Gerade ergibt, zeigen sich bei den sogenannten nichtnewtonschen Flüssigkeiten in Abhängigkeit vom jeweiligen Geschwindigkeitsgefälle D (Schergeschwindigkeit γ ) bzw. der Schubspannung τ oft erhebliche Abweichungen. In diesen Fällen läßt sich die sogenannte scheinbare Viskosität bestimmen, die zwar nicht der Newtonschen Gleichung gehorcht, aus der sich jedoch durch graphische Verfahren die wahren Viskositätswerte ermitteln lassen.While the graphic representation of the flow behavior of Newtonian liquids at a given temperature gives a straight line, so-called non-Newtonian liquids often show considerable deviations depending on the respective speed gradient D (shear rate γ) or the shear stress τ. In these cases the so-called apparent viscosity can be determined, which does not obey Newton's equation, but from which the true viscosity values can be determined by graphic methods.
Die Fallkörperviskosimetrie ist lediglich zur Untersuchung newtonscher Flüssigkeiten sowie von Gasen geeignet. Sie basiert auf dem Stokes-Gesetz, nach dem für das Fallen einer Kugel durch eine sie umströmende Flüssigkeit die dynamische Viskosität η ausThe falling body viscometry is only suitable for the investigation of Newtonian liquids and gases. It is based on the Stokes law, according to which the dynamic viscosity η for a ball falling through a liquid flowing around it
2r2(pκ - pR)-g η 9 v bestimmbar ist, wobei r = Radius der Kugel, v = Fallgeschwindigkeit, pκ = Dichte der Kugel, pF, = Dichte der Flüssigkeit und g = Fallbeschleunigung.2r 2 (p κ - p R ) -g η 9 v can be determined, where r = radius of the sphere, v = falling speed, p κ = density of the sphere, p F , = density of the liquid and g = acceleration of gravity.
O/W-Emulsionen mit einer geringen Viskosität, die eine Lagerstabilität aufweisen, wie sie für marktgängige Produkte gefordert wird, sind nach dem Stand der Technik nur sehr aufwendig zu formulieren. Dementsprechend ist das Angebot an derartigen Formulierungen äußerst gering. Gleichwohl könnten derartige Formulierungen dem Verbraucher bisher nicht gekannte kosmetische Leistungen bieten.O / W emulsions with a low viscosity, which have a storage stability, as is required for marketable products, can only be formulated with great effort using the prior art. Accordingly, the range of such formulations is extremely small. Nevertheless, such formulations could offer the consumer previously unknown cosmetic services.
Ferner war eine Aufgabe der vorliegenden Erfindung, Produkte mit einer möglichst breiten Anwendungsvielfalt zur Verfügung zu stellen. Beispielsweise sollten Grundlagen für Zubereitungsformen wie Reinigungsemulsionen, Gesichts- und Körperpflegezubereitungen, aber auch ausgesprochen medizinisch-pharmazeutische Darreichungsformen geschaffen werden, zum Beispiel Zubereitungen gegen Akne und andere Hauterscheinungen. Es hat sich überraschend gezeigt, und darin liegt die Lösung dieser Aufgaben, daß kosmetische oder dermatologische Zubereitungen in Form einer OΛΛ/-Emulsion enthaltendIt was also an object of the present invention to provide products with the widest possible range of applications. For example, the basis for preparation forms such as cleaning emulsions, face and body care preparations, but also very medicinal-pharmaceutical forms of administration should be created, for example preparations for acne and other skin symptoms. It has been shown to be surprising, and this is the solution to these problems that cosmetic or dermatological preparations in the form of an OΛΛ / emulsion
(I) 1 bis zu 5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, einer o- der mehrerer Substanzen, gewählt aus der Gruppe der Sterine, verzweigten oder unverzweigten, gesättigten oder ungesättigten C12-C 0-Fettsäuren,(I) 1 to 5% by weight, based on the total weight of the preparations, one or more substances selected from the group of sterols, branched or unbranched, saturated or unsaturated C 12 -C 0 fatty acids,
(II) 0,1 bis zu 1 ,5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, eines oder mehrerer Mono-, Sesqui-, Di-, Triestem von gesättigten oder ungesättigten, geradkettigten oder verzweigtkettigen Fettsäuren mit einer Kettenlänge von Cι4 - C40 des Glycerols und/oder des Propylenglycols und/oder des Glykols,(II) 0.1 to 1.5% by weight, based on the total weight of the preparations, of one or more mono-, sesqui-, di-, trieste of saturated or unsaturated, straight-chain or branched-chain fatty acids with a chain length of Cι 4 - C 40 of glycerol and / or propylene glycol and / or glycol,
(III) 0,1 bis zu 1 ,5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitung eines o- der mehrerer Mono-, Sesqui-, Di-, Triester von gesättigten oder ungesättigten, geradkettigten oder verzweigtkettigen Fettsäuren mit einer Kettenlänge von C14 - C40 des Sorbitans, optional mit einem Polyethoxylierungsgrad von 0-100,(III) 0.1 to 1.5% by weight, based on the total weight of the preparation of one or more mono-, sesqui-, di-, triesters of saturated or unsaturated, straight-chain or branched-chain fatty acids with a chain length of C 14 - C 40 of sorbitan, optionally with a degree of polyethoxylation of 0-100,
(IV) 0,1 bis zu 1,5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, eines oder mehrerer ethoxylierter Fettsäureester, mit Fettsäuren der Kettenlänge Cι2 - C40 und einem Ethoxylierungsgrad bis zu 100, bevorzugt von 5 - 100,(IV) 0.1 to 1.5% by weight, based on the total weight of the preparations, of one or more ethoxylated fatty acid esters, with fatty acids of chain length C 2 -C 40 and a degree of ethoxylation up to 100, preferably from 5 to 100 .
(V) 0,5 - 7 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, einer oder mehrere Fettalkohole, gewählt aus der Gruppe der verzweigten und unverzweigten, gesättigten und ungesättigten Alkylalkohole mit 12 bis 40 Kohlenstoff atomen(V) 0.5 - 7 wt .-%, based on the total weight of the preparations, one or more fatty alcohols selected from the group of branched and unbranched, saturated and unsaturated alkyl alcohols with 12 to 40 carbon atoms
(VI) wobei das Verhältnis aus (II): (III) : (IV) vorzugsweise gewählt wie a : b : c wird, wobei a, b und c unabhängig voneinander rationale Zahlen von 1 bis 5, bevorzugt von 1 bis 3 darstellen.(VI) where the ratio of (II): (III): (IV) is preferably chosen as a: b: c, where a, b and c independently of one another represent rational numbers from 1 to 5, preferably from 1 to 3.
(VII) sowie das Verhältnis aus (II)+(|||)+(IV) zu (V) vorzugsweise im Bereich 5:1 bis 1:5 liegt,(VII) and the ratio of (II) + (|||) + (IV) to (V) is preferably in the range 5: 1 to 1: 5,
(VIII) wobei die Summe aus (I), (II), (III), (IV) und (V) maximal 25 Gew.-% beträgt,(VIII) the sum of (I), (II), (III), (IV) and (V) being at most 25% by weight,
(IX) und wobei die Zubereitungen vorteilhaft in einem pH-Bereich von 3,5 - 8,0, vorzugsweise bei pH-Werten von 4,5 -6,5, vorliegen, den Nachteilen des Standes der Technik abhelfen.(IX) and where the preparations are advantageously present in a pH range from 3.5 to 8.0, preferably at pH values from 4.5 to 6.5, remedy the disadvantages of the prior art.
Es war für den Fachmann daher nicht vorauszusehen gewesen, daß die erfindungsgemäßen Zubereitungen besser als feuchtigkeitsspendende Zubereitungen wirken, besser die Hautglättung fördern, sich durch bessere Pflegewirkung auszeichnen, besser als Vehikel für kosmetische und medizinisch-dermatologische Wirkstoffe dienen höhere Stabilität gegenüber der Kristallisation der eingesetzten Fettsäuren aufweisen und sich durch bessere Bioverträglichkeit auszeichnen würden sich durch ein besseres Hautgefühl und durch höhere kosmetische Eleganz auszeichnen würden sich über eine breite kosmetische Variabilität auszeichnen würden und über breite Konsistenz- und Viskositätsbereiche von 400 mPas bis > 20.000 mPas formulieren lassen würden als die Zubereitungen des Standes der Technik.It was therefore not foreseeable for the person skilled in the art that the preparations according to the invention act better than moisturizing preparations, better promote smoothing of the skin, are distinguished by better care effects, serve better as a vehicle for cosmetic and medical-dermatological active ingredients have higher stability towards the crystallization of the fatty acids used and would be characterized by better biocompatibility would be characterized by a better skin feel and by higher cosmetic elegance would be characterized by a wide cosmetic variability and by a wide range Consistency and viscosity ranges from 400 mPas to> 20,000 mPas would be formulated as the preparations of the prior art.
Die erfindungsgemäßen Zubereitungen sind sowohl sprühbar, fließfähig als auch cremeartig formulierbar, besitzen sehr gute kosmetische Eigenschaften, insbesondere was die Klebrigkeit betrifft, und weisen eine sehr gute Hautverträglichkeit sowie Hautpflegeleistung auf.The preparations according to the invention are both sprayable, flowable and cream-like, can be formulated, have very good cosmetic properties, in particular with regard to stickiness, and have very good skin tolerance and skin care performance.
Sterine sind Steroide, die nur in der 3-Position eine Hydroxy-Gruppe, sonst aber keine funk- tionelle Gruppe tragen, stellenalso formal Alkohole dar. Daher wird gelegentlich die logischere Bez. Sterole benutzt. Zusätzlich besitzen die 27 bis 30 C-Atome enthaltenden Sterine im allgemeinen eine Doppelbindung in 5/6-Stellung, seltener auch/oder in 7/8, 8/9 und anderen Positionen (z. B. 22/23).Sterols are steroids that only have a hydroxyl group in the 3-position, but do not have a functional group otherwise, formally represent alcohols. Therefore, the more logical name sterols is sometimes used. In addition, the sterols containing 27 to 30 carbon atoms generally have a double bond in the 5/6 position, more rarely also / or in 7/8, 8/9 and other positions (for example 22/23).
Die Sterine sind als Lipide - zumeist in Form von Estern (früher Steride genannt) - in der Natur weit verbreitet. Die im Tierreich vorkommenden Sterine nennt man Zoosterine. Wichtigster Vertreter ist das Cholesterin. Weitere Zoosterine fand man im Wollfett (Lanosterin, Dihydrolanosterin), in der Seidenraupe, in Schwämmen (Spongosterin), Seesternen, Seeigeln, Austern usw.The sterols are widespread in nature as lipids - mostly in the form of esters (formerly called steroids). The sterols found in the animal kingdom are called zoosterols. The most important representative is cholesterol. Further zoosterols were found in wool fat (lanosterol, dihydrolanosterol), in the silkworm, in sponges (spongosterol), starfish, sea urchins, oysters etc.
Cholesterin ist durch folgende Struktur gekennzeichnet: Cholesterol is characterized by the following structure:
Lanosterin ist durch folgende Struktur gekennzeichnet:Lanosterin is characterized by the following structure:
Dihydrolanosterin ist durch folgende Struktur gekennzeichnet:Dihydrolanosterol is characterized by the following structure:
Die pflanzlichen Sterine werden Phytosterine genannt. Ihre wichtigsten Vertreter sind Er- gosterin, Stigmasterin und Sitosterin. Sie finden teilweise in kosmet. Produkten Verwendung. Gelegentlich trennt man von der Gruppe der Phytosterine die Sterine aus Pilzen und Hefen als Mykosterine (z. B. Ergosterin, Fungisterin, Stellasterin und Zymosterin) ab.The plant sterols are called phytosterols. Its main representatives are ergosterol, stigmasterol and sitosterol. You can find some in cosmetics. Products use. Occasionally, the sterols from fungi and yeast are separated from the group of phytosterols as mycosterols (e.g. ergosterol, fungister, stellasterin and zymosterol).
Beispiele für Phytosterole sind: Examples of phytosterols are:
(Ergosterol),(Ergosterol),
(Stigmasterol),(Stigmasterol),
(Sitosterol), (Sitosterol),
(Fucosterol),(Fucosterol)
(Brassicasterol),(Brassicasterol),
(Fungisterol), (Fungisterol)
(Campesterol).(Campesterol).
Alle erfindungsgemäß zu verwendenden Phytosterole besitzen eine mehr oder weniger große Anzahl an optischen Isomeren, welche hier im einzelnen nicht aufgeführt werden sollen, welche sich aber als vorteilhaft erwiesen haben, sofern ihre kosmetische Unbedenklichkeit außer Frage steht.All phytosterols to be used according to the invention have a more or less large number of optical isomers, which are not to be listed in detail here, but which have proven to be advantageous insofar as their cosmetic safety is beyond question.
Bevorzugte Sterine sind Cholesterol und Lanosterol.Preferred sterols are cholesterol and lanosterol.
Bevorzugte Fettsäuren sind Stearinsäure und/oder Palmitinsäure (Stearin) sowie Lignocerin- säure.Preferred fatty acids are stearic acid and / or palmitic acid (stearin) and lignoceric acid.
Vorteilhafte Ausführungsformen der vorliegenden Erfindung betreffen kosmetische und dermatologische Zubereitungen, enthaltendAdvantageous embodiments of the present invention relate to cosmetic and dermatological preparations containing
(II) 0,1 bis zu 1,5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, einer oder mehrerer Glycol- bzw. Glycerylester gewählt aus der Gruppe der Mono-, Sesqui- Di- und Triester der Glycole (= vic-Diole bzw. 1,2-Diole) bzw. des Glycerols (1,2,3- Trihydroxypropane) mit Fettsäuren der Kettenlänge Cι2 - C 40 (geradzahlig, gesättigt, ungesättigt und verzweigt) Beispiele: Glycerylmonostearat, Glyceryldistearat, Propy- lenglycolmonostearat, Glycerylisostearat, Glyceryllanolat, Glycerylmyristat, Glyceryl- laurat, Glyceryloleat, Glycerylstearatcitrat.(II) 0.1 to 1.5% by weight, based on the total weight of the preparations, of one or more glycol or glyceryl esters selected from the group of the mono-, sesqui-di- and triesters of the glycols (= vic Diols or 1,2-diols) or of glycerol (1,2,3-trihydroxypropane) with fatty acids of chain length C 2 - C 40 (even, saturated, unsaturated and branched) Examples: glyceryl monostearate, glyceryl distearate, propylene glycol monostearate , Glyceryl isostearate, glyceryl alcoholate, glyceryl myristate, glyceryl laurate, glyceryl oleate, glyceryl stearate citrate.
Vorteilhafte Ausführungsformen der vorliegenden Erfindung betreffen kosmetische und dermatologische Zubereitungen, enthaltendAdvantageous embodiments of the present invention relate to cosmetic and dermatological preparations containing
(III) 0,1 bis zu 1 ,5 Gew.-% eines oder mehrere Sorbitanester, gewählt aus der Gruppe der Mono-, Sesqui-, Di und Triester der Sorbitane (= Monoanhydrosorbite bzw. 1 ,5- Anhydro-D-Sorbit) mit Fettsäuren der Kettenlänge C12 - C 40 (geradzahlig, gesättigt, ungesättigt und verzweigt) sowie optional einem Ethoxylierungsgrad von 10 - 100). Beispiele: Sorbitanstearat, Sorbitandistearat, Sorbitanisostearat, Sorbitanoleat, PEG- 40-Sorbitanperoleat, PEG-40-Sorbitanperisostearat, Sorbitansesquioleat.(III) 0.1 up to 1.5% by weight of one or more sorbitan esters, selected from the group of the mono-, sesqui-, di and triesters of the sorbitan (= monoanhydrosorbites or 1.5- Anhydro-D-sorbitol) with fatty acids of chain length C 12 - C 40 (even, saturated, unsaturated and branched) and optionally a degree of ethoxylation of 10 - 100). Examples: sorbitan stearate, sorbitan distearate, sorbitan isostearate, sorbitan oleate, PEG-40 sorbitan peroleate, PEG-40 sorbitan perisostearate, sorbitan sesquioleate.
Vorteilhafte Ausführungsformen der vorliegenden Erfindung betreffen ferner kosmetische und dermatologische Zubereitungen, enthaltendAdvantageous embodiments of the present invention also relate to cosmetic and dermatological preparations containing
(III) 0,1 bis zu 1 ,5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, eines oder mehrerer ethoxylierter Fettsäureester, mit Fettsäuren der Kettenlänge Cι2 - C o und einem Ethoxylierungsgrad von 5 - 100, insbesondere gewählt aus der Gruppe PEG-20 Stearat, PEG-30 Stearat, PEG-40-Stearat, PEG-100 Stearat(III) 0.1 to 1.5% by weight, based on the total weight of the preparations, of one or more ethoxylated fatty acid esters, with fatty acids of chain length C 2 -C o and a degree of ethoxylation of 5-100, in particular selected from Group PEG-20 stearate, PEG-30 stearate, PEG-40 stearate, PEG-100 stearate
Vorteilhafte Ausführungsformen der vorliegenden Erfindung betreffen ferner kosmetische und dermatologische Zubereitungen, enthaltendAdvantageous embodiments of the present invention also relate to cosmetic and dermatological preparations containing
(V) 0,5 - 7 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, einer oder mehrere Fettalkohole, gewählt aus der Gruppe Myristylalkohol, Cetylalkohol, Isocetylalko- hol, Cetylstearylalkohol, Stearylalkohol, Isostearylalkohol, Behenylalkohol und Mischungen daraus.(V) 0.5-7% by weight, based on the total weight of the preparations, of one or more fatty alcohols selected from the group consisting of myristyl alcohol, cetyl alcohol, isocetyl alcohol, cetylstearyl alcohol, stearyl alcohol, isostearyl alcohol, behenyl alcohol and mixtures thereof.
Die Gesamtmenge an verzweigten und unverzweigten Alkylalkohole mit 12 bis 40 Kohlenstoffatomen in den fertigen kosmetischen oder dermatologischen Zubereitungen wird vorteilhaft aus dem Bereich von 0,1 - 7,0 Gew.-%, bevorzugt 0,5 - 5,0 Gew.-% gewählt, bezogen auf das Gesamtgewicht der Zubereitungen.The total amount of branched and unbranched alkyl alcohols having 12 to 40 carbon atoms in the finished cosmetic or dermatological preparations is advantageously chosen from the range from 0.1 to 7.0% by weight, preferably 0.5 to 5.0% by weight , based on the total weight of the preparations.
Wollwachsalkohole (CAS-Nr. 8027-33-6) stellen die unverseifbare Alkoholfraktion des Wollwachses dar, die nach der Verseifung des Wollwachses erhalten wird. Sie bestehen zu ca. 25,2 % aus Cholesterol, zu 2,7 % aus Lanosterol, zu 2,2 % aus Dihydrolanosterol und zu ca. 29,5 % aliphatischen einwertigen Cι6-C32- Alkoholen. Wollwachsalkohole werden daher zur Herstellung von Salbengrundlagen, aus denen meist W/O-Emulsionen gefertigt werden, verwendet. Vorteilhafte Ausführungsformen der vorliegenden Erfindung betreffen daher Zubereitungen nachWool wax alcohols (CAS No. 8027-33-6) represent the unsaponifiable alcohol fraction of the wool wax that is obtained after the saponification of the wool wax. They consist of approximately 25.2% cholesterol, 2.7% lanosterol, 2.2% dihydrolanosterol and approximately 29.5% aliphatic monohydric C 6 -C 32 alcohols. Wool wax alcohols are therefore used for the production of ointment bases, from which mostly W / O emulsions are made. Advantageous embodiments of the present invention therefore relate to preparations according to
(V) wobei die aus der Gruppe der verzweigten und unverzweigten, gesättigten und ungesättigten Alkylalkohole mit 12 bis 40 Kohlenstoffatomen aus der Gruppe der Wollwachsalkohole gewählt werden,(V) where those from the group of branched and unbranched, saturated and unsaturated alkyl alcohols having 12 to 40 carbon atoms are selected from the group of wool wax alcohols,
(I) wobei diese Wollwachsalkohole neben den aliphatischen Alkoholen auch ein oder mehrere Sterine, beispielsweise Cholesterol, Lanosterol, Dihydrolanosterol, enthalten.(I) these wool wax alcohols contain, in addition to the aliphatic alcohols, also one or more sterols, for example cholesterol, lanosterol, dihydrolanosterol.
Vorteilhafte Ausführungsformen der vorliegenden Erfindung betreffen zum Beispiel kosmetische und dermatologische Zubereitungen in Form von O/W-Emulsionen, enthaltend 3% flüssige Lipide (vorzugsweise ausgewählt aus (a) Guerbetalkoholen, (b) gesättigten Triglyceri- den und (c) Ethern mittelkettiger Fettalkohole, (d) unpolare Lipide, (e) Silikonölen, (f) Dialkyl- carbonaten oder Abmischungen daraus.Advantageous embodiments of the present invention relate, for example, to cosmetic and dermatological preparations in the form of O / W emulsions, containing 3% liquid lipids (preferably selected from (a) Guerbet alcohols, (b) saturated triglycerides and (c) ethers of medium-chain fatty alcohols, (d) non-polar lipids, (e) silicone oils, (f) dialkyl carbonates or mixtures thereof.
Im Rahmen der vorliegenden Offenbarung wird als Oberbegriff für Fette, Öle, Wachse und dergleichen gelegentlich der Ausdruck „Lipide" verwendet, wie dem Fachmanne durchaus geläufig ist. Auch werden die Begriffe „Ölphase" und „Lipidphase" synonym angewandt.In the context of the present disclosure, the term “lipids” is sometimes used as a generic term for fats, oils, waxes and the like, as is well known to the person skilled in the art. The terms “oil phase” and “lipid phase” are also used synonymously.
Öle und Fette unterscheiden sich unter anderem in ihrer Polarität, welche schwierig zu definieren ist. Es wurde bereits vorgeschlagen, die Grenzflächenspannung gegenüber Wasser als Maß für den Polaritätsindex eines Öls bzw. einer Ölphase anzunehmen. Dabei gilt, daß die Polarität der betreffenden Ölphase umso größer ist, je niedriger die Grenzflächenspannung zwischen dieser Ölphase und Wasser ist. Erfindungsgemäß wird die Grenzflächenspannung als ein mögliches Maß für die Polarität einer gegebenen Ölkomponente angesehen.Oils and fats differ among other things in their polarity, which is difficult to define. It has already been proposed to take the interfacial tension against water as a measure of the polarity index of an oil or an oil phase. The polarity of the oil phase in question is greater, the lower the interfacial tension between this oil phase and water. According to the invention, the interfacial tension is viewed as a possible measure of the polarity of a given oil component.
Die Grenzflächenspannung ist diejenige Kraft, die an einer gedachten, in der Grenzfläche zwischen zwei Phasen befindlichen Linie der Länge von einem Meter wirkt. Die physikalische Einheit für diese Grenzflächenspannung errechnet sich klassisch nach der Beziehung Kraft/Länge und wird gewöhnlich in mN/m (Millinewton geteilt durch Meter) wiedergegeben. Sie hat positives Vorzeichen, wenn sie das Bestreben hat, die Grenzfläche zu verkleinern. Im umgekehrten Falle hat sie negatives Vorzeichen. Als polar im Sinne der vorliegenden Erfin- dung werden Lipide angesehen, deren Grenzflächenspannung gegen Wasser weniger als 30 mN/m beträgt.The interfacial tension is the force that acts on an imaginary line of one meter in length that lies in the interface between two phases. The physical unit for this interfacial tension is calculated classically according to the force / length relationship and is usually given in mN / m (millinewtons divided by meters). It has a positive sign if it tries to reduce the size of the interface. In the opposite case, it has a negative sign. As polar in the sense of the present invention Lipids whose interfacial tension against water is less than 30 mN / m are considered.
Polare Öle, sind beispielsweise solche aus der Gruppe der Lecithine und der Fettsäuretrigly- ceride, namentlich der Triglycerinester gesättigter und/oder ungesättigter, verzweigter und/oder unverzweigter Alkancarbonsäuren einer Kettenlänge von 8 bis 24, insbesondere 12 bis 18 C-Atomen. Die Fettsäuretriglyceride können beispielsweise vorteilhaft gewählt werden aus der Gruppe der synthetischen, halbsynthetischen und natürlichen Öle, wie z.B. Olivenöl, Sonnenblumenöl, Sojaöl, Erdnußöl, Rapsöl, Mandelöl, Palmöl, Kokosöl, Rizinusöl, Wei- zenkeimöl, Traubenkernöl, Distelöl, Nachtkerzenöl, Macadamianußöl und dergleichen mehr.Polar oils are, for example, those from the group of lecithins and fatty acid triglycerides, namely the triglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 8 to 24, in particular 12 to 18, carbon atoms. The fatty acid triglycerides can, for example, advantageously be selected from the group of synthetic, semi-synthetic and natural oils, such as e.g. Olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, castor oil, wheat germ oil, grape seed oil, safflower oil, evening primrose oil, macadamia nut oil and the like.
Weitere polare Ölkomponenten können gewählt werden aus der Gruppe der Ester aus gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkancarbonsäuren einer Kettenlänge von 3 bis 30 C-Atomen und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C-Atomen sowie 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-Decyl- oleat, Isooctylstearat, Isononylstearat, Isononylisononanoat, 2-Ethylhexylpalmitat, 2-Ethylhe- xyllaurat, 2-Hexyldecylstearat, 2-Octyldodecylpalmitat, Oleyloleat, Oleylerucat, Erucyloleat, Erucylerucat sowie synthetische, halbsynthetische und natürliche Gemische solcher Ester, wie z.B. Jojobaöl.Further polar oil components can be selected from the group of esters from saturated and / or unsaturated, branched and / or unbranched alkane carboxylic acids with a chain length of 3 to 30 carbon atoms and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 up to 30 carbon atoms and 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 carbon atoms. Such ester oils can then advantageously be selected from the group of isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononylisononanoate, 2-ethylhexyl urethane Hexyldecyl stearate, 2-octyldodecyl palmitate, oleyl oleate, olerlerucate, erucyl oleate, erucylerucate as well as synthetic, semi-synthetic and natural mixtures of such esters, such as Jojoba oil.
Ferner kann die Ölphase vorteilhaft gewählt werden aus der Gruppe der Dialkylether, der Gruppe der gesättigten oder ungesättigten, verzweigten oder unverzweigten Alkohole. Es ist insbesondere vorteilhaft, wenn die Ölphase der erfindungsgemäßen W/O-Emulsionen einen Gehalt an Cι2-15-Alkylbenzoat aufweist oder vollständig aus diesem besteht.Furthermore, the oil phase can advantageously be chosen from the group of dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols. It is particularly advantageous if the oil phase of the W / O emulsions according to the invention has a C 2-15 alkyl benzoate content or consists entirely of this.
Ferner kann die Ölphase vorteilhaft gewählt werden aus der Gruppe der Guerbetalkohole. Guerbetalkohole sind benannt nach Marcel Guerbet, der ihre Herstellung erstmalig beschrieb. Sie entstehen nach der Reaktionsgleichung RFurthermore, the oil phase can advantageously be selected from the group of Guerbet alcohols. Guerbet alcohols are named after Marcel Guerbet, who described their production for the first time. They arise according to the reaction equation R
R— CH2-CH2— OH ► R_CH_CH2— OHR— CH2-CH2— OH ► R _ CH _CH2— OH
Katalysatorcatalyst
durch Oxidation eines Alkohols zu einem Aldehyd, durch Aldol-Kondensation des Aldehyds, Abspaltung von Wasser aus dem Aldol- und Hydrierung des Allylaldehyds. Guerbetalkohole sind selbst bei niederen Temperaturen flüssig und bewirken praktisch keine Hautreizungen. Vorteilhaft können sie als fettende, überfettende und auch rückfettend wirkende Bestandteile in Haut- und Haarpflegemitteln eingesetzt werden.by oxidation of an alcohol to an aldehyde, by aldol condensation of the aldehyde, elimination of water from the aldol and hydrogenation of the allyl aldehyde. Guerbet alcohols are liquid even at low temperatures and practically do not cause skin irritation. They can advantageously be used as greasing, over-greasing and also moisturizing components in skin and hair care products.
Die Verwendung von Guerbet-Alkoholen in Kosmetika ist an sich bekannt. Solche Species zeichnen sich dann meistens durch die StrukturThe use of Guerbet alcohols in cosmetics is known per se. Such species are usually characterized by their structure
HH
R1 — C — CH2 — OHR 1 - C - CH 2 - OH
R2 aus. Dabei bedeuten R1 und R2 in der Regel unverzweigte Alkylreste.R 2 off. R 1 and R 2 generally mean unbranched alkyl radicals.
Erfindungsgemäß vorteilhaft werden der oder die Guerbet-Alkohole gewählt aus der Gruppe, bei denenAccording to the invention, the Guerbet alcohol or alcohols are advantageously selected from the group in which
Ri = Propyl, Butyl, Pentyl, Hexyl, Heptyl oder Octyl undRi = propyl, butyl, pentyl, hexyl, heptyl or octyl and
R2 = Hexyl, Heptyl, Octyl, Nonyl, Decyl, Undecyl, Dodecyl, Tridecyl oder Tetradecyl.R 2 = hexyl, heptyl, octyl, nonyl, decyl, undecyl, dodecyl, tridecyl or tetradecyl.
Erfindungsgemäß bevorzugte Guerbet-Alkohole sind das 2-Butyloctanol - es hat die chemische StrukturGuerbet alcohols preferred according to the invention are 2-butyl octanol - it has the chemical structure
und ist beispielsweise unter der Handelsbezeichnung Isofol® 12 von der Gesellschaft Con- dea Chemie GmbH erhältlich - und das 2-Hexyldecanol - es hat die chemische Struktur H and is available, for example, under the trade name Isofol ® 12 from Conde Chemie GmbH - and the 2-hexyldecanol - it has the chemical structure H
H'oCß — C CH2 OHH'oC ß - C CH 2 OH
C10H21 und ist beispielsweise unter der Handelsbezeichnung Isofol® 16 von der Gesellschaft Con- dea Chemie GmbH erhältlich.C10H21 and is available, for example, under the trade name Isofol® 16 from Condeda Chemie GmbH.
Auch Mischungen von erfindungsgemäßen Guerbet-Alkoholen sind erfindungsgemäß vorteilhaft zu verwenden. Mischungen aus 2-Butyloctanol und 2-Hexyldecanol sind beispielsweise unter der Handelsbezeichnung Isofol® 14 von der Gesellschaft Condea Chemie GmbH erhältlich.Mixtures of Guerbet alcohols according to the invention can also be used advantageously according to the invention. Mixtures of 2-butyl octanol and 2-hexyl decanol are available, for example, under the trade name Isofol® 14 from Condea Chemie GmbH.
Die Gesamtmenge an Guerbet-Alkoholen in den fertigen kosmetischen oder dermatologischen Zubereitungen wird vorteilhaft aus dem Bereich bis 25,0 Gew.-%, bevorzugt 0,5 - 15,0 Gew.-% gewählt, bezogen auf das Gesamtgewicht der Zubereitungen.The total amount of Guerbet alcohols in the finished cosmetic or dermatological preparations is advantageously selected from the range up to 25.0% by weight, preferably 0.5-15.0% by weight, based on the total weight of the preparations.
Auch beliebige Abmischungen solcher Öl- und Wachskomponenten sind vorteilhaft im Sinne der vorliegenden Erfindung einzusetzen. Es kann auch gegebenenfalls vorteilhaft sein, Wachse, beispielsweise Cetylpalmitat, als alleinige Lipidkomponente der Ölphase einzusetzen.Any mixtures of such oil and wax components can also be used advantageously for the purposes of the present invention. It may also be advantageous to use waxes, for example cetyl palmitate, as the sole lipid component of the oil phase.
Unpolare Öle sind beispielsweise solche, welche gewählt werden aus der Gruppe der verzweigten und unverzweigten Kohlenwasserstoffe und -wachse, insbesondere Vaseline (Pe- trolatum), Paraffinöl, Squalan und Squalen, Polyolefine und hydrogenierte Polyisobutene. Unter den Polyolefinen sind Polydecene die bevorzugten Substanzen. Die nachfolgende Tabelle 1 führt Lipide auf, die als Einzelsubstanzen oder auch im Gemisch untereinander erfindungsgemäß vorteilhaft sind. Die betreffenden Grenzflächenspannungen gegen Wasser sind in der letzten Spalte angegeben. Es ist jedoch auch vorteilhaft, Gemische aus höher- und niederpolaren und dergleichen zu verwenden. Nonpolar oils are, for example, those which are selected from the group of branched and unbranched hydrocarbons and waxes, in particular petroleum jelly (petrolatum), paraffin oil, squalane and squalene, polyolefins and hydrogenated polyisobutenes. Among the polyolefins, polydecenes are the preferred substances. Table 1 below lists lipids which are advantageous according to the invention as individual substances or as a mixture with one another. The relevant interfacial tensions against water are given in the last column. However, it is also advantageous to use mixtures of higher and lower polar and the like.
Als Grundbestandteile der erfindungsgemäßen Zubereitungen können verwendet werden: Wasser oder wäßrige Lösungen wäßrige ethanolische Lösungen natürliche Öle und/oder chemisch modifizierte natürliche Öle und/oder synthetische Öle; Fette, Wachse und andere natürliche und synthetische Fettkörper, vorzugsweise Ester von Fettsäuren mit Alkoholen niedriger C-Zahl, z.B. mit Isopropanol, Propylengly- kol oder Glycerin, oder Ester von Fettalkoholen mit Alkansäuren niedriger C-Zahl o- der mit Fettsäuren;The following can be used as basic components of the preparations according to the invention: water or aqueous solutions, aqueous ethanolic solutions, natural oils and / or chemically modified natural oils and / or synthetic oils; Fats, waxes and other natural and synthetic fat bodies, preferably esters of fatty acids with alcohols with a low C number, for example with isopropanol, propylene glycol or glycerol, or esters of fatty alcohols with alkanoic acids with a low C number or with fatty acids;
Alkohole, Diole oder Polyole niedriger C-Zahl, sowie deren Ether, vorzugsweise Etha- nol, Isopropanol, Propylenglykol, Glycerin, Ethylenglykol, Ethylenglykolmonoethyl- o- der -monobutylether, Propylenglykolmonomethyl, -monoethyl- oder -monobutylether, Diethylenglykolmonomethyl- oder -monoethylether und analoge Produkte.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, diethylene glycol monomethyl or monoethyl ether and analog products.
Insbesondere werden Gemische der vorstehend genannten Lösungsmittel verwendet.Mixtures of the abovementioned solvents are used in particular.
Die Ölphase der Emulsionen im Sinne der vorliegenden Erfindung besteht erfindungsgemäß vorzugsweise vorwiegend aus Komponenten der unter Punkt (4) aufgeführten Art, wobei es allerdings möglich ist, ohne große Nachteile in Kauf zu nehmen, bis zu 50 Gew.-%, vorzugsweise bis zu 40 Gew.-% des Gesamtgewichtes der Olkomponenten aus der Gruppe anderer Olkomponenten zu wählen. Diese können dann vorteilhaft gewählt werden aus der Gruppe der Ester aus gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkancarbonsäuren einer Kettenlänge von 3 bis 30 C-Atomen und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C-Atomen, aus der Gruppe der Ester aus aromatischen Carbonsäuren und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C-Atomen. Solche Esteröle können dann vorteilhaft gewählt werden aus der Gruppe Isopropylmyristat, Isopropylpalmitat, Isopropylstearat, Isopropyloleat, n-Butylstearat, n-Hexyllaurat, n-Decyloleat, Isooctylstearat, Isononylstearat, Isononylisononanoat, 2-Ethyl- hexylpalmitat, 2-Ethylhexyllaurat, 2-Hexyldecylstearat, 2-Octyldodecylpalmitat, Oleyloleat, Oleylerucat, Erucyloleat, Erucylerucat sowie synthetische, halbsynthetische und natürliche Gemische solcher Ester, z.B. Jojobaöl.According to the invention, the oil phase of the emulsions preferably consists predominantly of components of the type listed under point (4), although it is possible to accept up to 50% by weight, preferably up to 40, without major disadvantages % By weight of the total weight of the oil components from the group of other oil components. These can then advantageously be 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 up to 30 carbon 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 carbon atoms. Such ester oils can then advantageously be selected from the group of isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononylisononanoate, 2-ethyl-2-ethylhexyl palatate 2-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 Dialkylether, der Gruppe der gesättigten oder ungesättigten, verzweigten oder unverzweigten Alkohole, sowie der Fettsäuretriglyce- ride, namentlich der Triglycerinester gesättigter und/oder ungesättigter, verzweigter und/oder unverzweigter Alkancarbonsäuren einer Kettenlänge von 8 bis 24, insbesondere 12 - 18 C- Atomen. Die Fettsäuretriglyceride können beispielsweise vorteilhaft gewählt werden aus der Gruppe der synthetischen, halbsynthetischen und natürlichen Öle, z.B. Olivenöl, Sonnenblumenöl, Sojaöl, Erdnußöl, Rapsöl, Mandelöl, Palmöl, Kokosöl, Palmkernöl und dergleichen mehr, sofern die im Hauptanspruch geforderten Bedingungen eingehalten werden.Furthermore, the oil phase can advantageously be chosen from the group of branched and unbranched hydrocarbons and waxes, the dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols, and also the fatty acid triglycerides, especially the triglycerol esters saturated and / or unsaturated, 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, semi-synthetic 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, provided that the conditions specified in the main claim are met.
Erfindungsgemäß vorteilhaft zu verwendende Fett- und/oder Wachskomponenten können aus der Gruppe der pflanzlichen Wachse, tierischen Wachse, Mineralwachse und petroche- mischen Wachse gewählt werden. Erfindungsgemäß günstig sind beispielsweise Candelilla- wachs, Carnaubawachs, Japanwachs, Espartograswachs, Korkwachs, Guarumawachs, Reiskeimölwachs, Zuckerrohrwachs, Beerenwachs, Ouricurywachs, Montanwachs, Jojoba- wachs, Shea Butter, Bienenwachs, Schellackwachs, Walrat, Lanolin (Wollwachs), Bürzelfett, Ceresin, Ozokerit (Erdwachs), Paraffinwachse und Mikrowachse, sofern die im Hauptanspruch geforderten Bedingungen eingehalten werden.Fat and / or wax components to be used advantageously according to the invention can be selected from the group of vegetable waxes, animal waxes, mineral waxes and petrochemical waxes. Favorable according to the invention are, for example, candelilla wax, carnauba wax, japan wax, esparto grass wax, cork wax, guaruma wax, rice germ oil wax, sugar cane wax, berry wax, ouricury wax, montan wax, jojoba wax, shea butter, beeswax, shellac wax, walnut, lanolin (wool wax), pretzel fat, ceresin Ozokerite (earth wax), paraffin waxes and micro waxes, provided the conditions specified in the main claim are met.
Weitere vorteilhafte Fett- und/oder Wachskomponenten sind chemisch modifzierte Wachse und synthetische Wachse, wie beispielsweise die unter den Handelsbezeichnungen Syncrowax HRC (Glyceryltribehenat), Syncrowax HGLC (C16-36-Fettsäuretriglycerid) und Syncrowax AW 1C (Ci8.36 -Fettsäure) bei der CRODA GmbH erhältlichen sowie Montanesterwachse, Sasolwachse, hydrierte Jojobawachse, synthetische oder modifizierte Bienenwachse (z. B. Dimethicon Copolyol Bienenwachs und/oder C30-so -Alkyl Bienenwachs), Polyalkylenwachse, Polyethylenglykolwachse, aber auch chemisch modifzierte Fette, wie z. B. hydrierte Pflanzenöle (beispielsweise hydriertes Ricinusöl und/oder hydrierte Cocosfettglyceride), Triglyce- ride, wie beispielsweise Trihydroxystearin, Fettsäuren, Fettsäureester und Glykolester, wie beispielsweise C20. o-Alkylstearat, C2o^to-Alkylhydroxystearoylstearat und/oder Glykol- montanat. Weiter vorteilhaft sind auch bestimmte Organosiliciumverbindungen, die ähnliche physikalische Eigenschaften aufweisen wie die genannten Fett- und/oder Wachskomponenten, wie beispielsweise Stearoxytrimethylsilan sofern die im Hauptanspruch geforderten Bedingungen eingehalten werden.Further advantageous fat and / or wax components are chemically modified waxes and synthetic waxes such as those sold under the tradenames Syncrowax HRC (glyceryl tribehenate), Syncrowax HGLC (C 16-3 6-fatty acid triglyceride) (. CI8 36 fatty acid) and Syncrowax AW 1C available from CRODA GmbH as well as montan ester waxes, sasol waxes, hydrogenated jojoba waxes, synthetic or modified beeswaxes (e.g. dimethicone copolyol beeswax and / or C 30 -so-alkyl beeswax), polyalkylene waxes, polyethylene glycol waxes, but also chemically modified fats such as B. hydrogenated vegetable oils (for example hydrogenated castor oil and / or hydrogenated coconut fat glycerides), triglycerides such as trihydroxystearin, fatty acids, fatty acid esters and glycol esters such as C 20 . o-alkyl stearate, C 2 o ^ to-alkyl hydroxystearoyl stearate and / or glycol montanate. Also particularly advantageous are certain organosilicon compounds which have similar physical properties to the fat and / or wax components mentioned, such as stearoxytrimethylsilane, provided the conditions specified in the main claim are met.
Erfindungsgemäß können die Fett- und/oder Wachskomponenten sowohl einzeln als auch im Gemisch vorliegen.According to the invention, the fat and / or wax components can be present both individually and in a mixture.
Auch beliebige Abmischungen solcher Öl- und Wachskomponenten sind vorteilhaft im Sinne der vorliegenden Erfindung einzusetzen. Vorteilhaft wird die Ölphase gewählt aus der Gruppe 2-Ethylhexylisostearat, Octyldodecanol, Isotridecylisononanoat, Isoeicosan, 2-Ethylhexylcocoat, Cι2-i5-Alkylbenzoat, Capryl-Caprin- säure-triglycerid, Dicaprylylether sofern die im Hauptanspruch geforderten Bedingungen eingehalten werden.Any mixtures of such oil and wax components can also be used advantageously for the purposes of the present invention. The oil phase is advantageously selected from the group 2-ethylhexyl isostearate, octyldodecanol, isotridecylisononanoate, isoeicosane, 2-ethylhexyl cocoate, Cι 2- i 5 alkyl benzoate, caprylic capric acid triglyceride, dicaprylyl ether as long as the conditions are met.
Besonders vorteilhaft sind Mischungen aus Octyldodecanol, Capryl-Caprinsäure-triglycerid, Dicaprylylether oder Mischungen aus d2.15-Alkybenzoat und 2-Ethylhexylisostearat, Mischungen aus Cι2-i5-Alkybenzoat und Isotridecylisononanoat sowie Mischungen aus Cι2-ιs- Alkybenzoat, 2-Ethylhexylisostearat und Isotridecylisononanoat sofern die im Hauptanspruch geforderten Bedingungen eingehalten werden.Mixtures of octyldodecanol, caprylic-capric acid triglyceride, dicaprylyl ether or mixtures of d 2 are particularly advantageous. 15 -Alkylbenzoate and 2-ethylhexyl isostearate, mixtures of Cι 2- i5-alkylbenzoate and isotridecyl isononanoate and mixtures of Cι 2- ιs alkylbenzoate, 2-ethylhexyl isostearate and isotridecyl isononanoate provided that the conditions specified in the main claim are met.
Von den Kohlenwasserstoffen sind Paraffinöl, Cycloparaffin, Squalan, Squalen, hydriertes Polyisobuten bzw. Polydecen vorteilhaft im Sinne der vorliegenden Erfindung zu verwenden, sofern die im Hauptanspruch geforderten Bedingungen eingehalten werden.Of the hydrocarbons, paraffin oil, cycloparaffin, squalane, squalene, hydrogenated polyisobutene or polydecene are to be used advantageously for the purposes of the present invention, provided the conditions specified in the main claim are met.
Erfindungsgemäße O/W-Emulsionen können vorteilhaft mit Hilfe der üblichen OΛ/V-Emulga- toren, gewünschtenfalls unter Zuhilfenahme von W/O-Emulgatoren bzw. weiteren Coemulga- toren hergestellt werden.O / W emulsions according to the invention can advantageously be prepared with the aid of the usual O / V emulsifiers, if desired with the aid of W / O emulsifiers or other co-emulsifiers.
O/W-Emulsionen entsprechend der vorliegenden Erfindung enthalten gewünschtenfalls ferner einen oder mehrere Emulgatoren, gewünschtenfalls vorteilhaft gewählt aus der Gruppe der folgenden Substanzen, die in der Regel als W/O-Emulgatoren wirken:If desired, O / W emulsions according to the present invention further contain one or more emulsifiers, if desired advantageously selected from the group of the following substances, which generally act as W / O emulsifiers:
Lecithin, Lanolin, mikrokristallines Wachs (Cera microcristallina) im Gemisch mit Paraffinöl (Paraffinum liquidum), Ozokerit, hydriertem Ricinusöl, Polyglyceryl-3-Oleat, Wollwachssäure- gemische, Wollwachsalkoholgemische, Pentaerythrithylisostearat, Polyglyceryl-3-Diisostea- rat, Bienenwachs (Cera alba) und Stearinsäure, Natriumdihydroxycetylphosphat im Gemisch mit Isopropylhydroxycetylether, Methylglucosedioleat, Methylglucosedioleat im Gemisch mit Hydroxystearat und Bienenwachs, Mineralöl im Gemisch mit Petrolatum und Ozokerit und Glyceryloleat und Lanolinalkohol, Petrolatum im Gemisch mit Ozokerit und hydriertem Ricinusöl und Glycerylisostearat und Polyglyceryl-3-oleat, PEG-7-hydriertes Ricinusöl, Ozokerit und hydriertem Ricinusöl, Polyglyceryl-4-isostearat, Polyglyceryl-4-isostearat im Gemisch mit Cetyldimethiconcopolyol und Hexyllaurat, Laurylmethiconcopolyol, Cetyldimethiconcopolyol, Acrylat/ Cιo-3o-Alkylacrylat-Crosspolymer, Poloxamer 101, Polyglyceryl-2-dipolyhydroxystea- rat, Polyglyceryl-3-Diisostearat, Polyglyceryl-4-dipolyhydroxystearat, PEG-30-dipolyhydroxy- stearat, Diisostearoylpolyglyceryl-3-diisostearat, Polyglyceryl-2-dipolyhydroxystearat, Po- lyglyceryl-3-dipolyhydroxystearat, Polyglyceryl-4-dipolyhydroxystearat, Polyglyceryl-3-dioleat.Lecithin, lanolin, microcrystalline wax (Cera microcristallina) in a mixture with paraffin oil (Paraffinum liquidum), ozokerite, hydrogenated castor oil, polyglyceryl-3-oleate, wool wax acid mixtures, wool wax alcohol mixtures, pentaerythrithyl isostearate, polyglyceryl-3-dibaostearate (c ) and stearic acid, sodium dihydroxycetyl phosphate in a mixture with isopropylhydroxycetyl ether, methyl glucose dioleate, methyl glucose dioleate in a mixture with hydroxystearate and beeswax, mineral oil in a mixture with petrolatum and ozokerite and glyceryl oleate and lanolin alcohol, petrolatum in a mixture with ozokerite and hydrogenated polyglycerol, glycine oleate and glyceryl glyceryl pearlyl, and glyceryl oleate, and hydrogenated ricinostearate -7-hydrogenated castor oil, ozokerite and hydrogenated castor oil, polyglyceryl-4-isostearate, polyglyceryl-4-isostearate in a mixture with cetyldimethicone copolyol and hexyllaurate, laurylmethicone copolyol, cetyldimethicone copolyol, acrylate / Cιo-3o-alkylacrylcrylglyceryl, 101-polyacrylate, dipolyhydroxyst ea- rat, polyglyceryl-3-diisostearate, polyglyceryl-4-dipolyhydroxystearate, PEG-30-dipolyhydroxy-stearate, diisostearoylpolyglyceryl-3-diisostearate, polyglyceryl-2-dipolyhydroxystearate, polyglyceryl-3-dipolyhydroxystearate, polyglyceryl 3 dioleate.
O/W-Emulsionen entsprechend der vorliegenden Erfindung enthalten gewünschtenfalls einen oder mehrere Emulgatoren, insbesondere vorteilhaft gewählt aus der Gruppe der folgenden Substanzen, die in der Regel als O/W-Emulgatoren wirken:If desired, O / W emulsions according to the present invention contain one or more emulsifiers, particularly advantageously selected from the group of the following substances, which generally act as O / W emulsifiers:
Glycerylstearat im Gemisch mit Ceteareth-20, Ceteareth-25, Ceteareth-6 im Gemisch mit Stearylalkohol, Cetylstearylalkohol im Gemisch mit PEG-40-Ricinusöl und Natriumcetylstea- rylsulfat, Triceteareth-4 Phosphat, Natriumcetylstearylsulfat, Lecithin Trilaureth-4 Phosphat, Laureth-4 Phosphat, Stearinsäure, Propylenglycolstearat SE, PEG-25-hydriertes Ricinusöl, PEG-54-hydriertes Ricinusöl, PEG-6 Caprylsäure/Caprinsäureglyceride, Glyceryloleat im Gemisch mit Propylenglycol, Ceteth-2, Ceteth-20, Polysorbat 60, Glycerylstearat im Gemisch mit PEG-100 Stearat, Laureth-4, Ceteareth-3, Isostearylglycerylether, Cetylstearylalkohol im Gemisch mit Natrium Cetylstearylsulfat, Laureth-23, Steareth-2, Glycerylstearat im Gemisch mit PEG-30 Stearat, PEG-40-Stearat, Glycol Distearat, PEG-22-Dodecyl Glycol Copolymer, Polyglyceryl-2-PEG-4-Stearat, Ceteareth-20, Methylglucosesesquistearat, Steareth-10, PEG- 20-Stearat, Steareth-2 im Gemisch mit PEG-8 Distearat, Steareth-21, Steareth-20, Isostea- reth-20, PEG-45/ Dodecylglycol-Copolymer, Methoxy-PEG-22/Dodecylglycol-Copolymer, PEG-20-Glycerylstearat, PEG-20-Glycerylstearat, PEG-8-Bienenwachs, Polyglyceryl-2-lau- rat, Isostearyldiglycerylsuccinat, Stearamidopropyl-PG-dimoniumchloridphosphat, Glycerylstearat SE, Ceteth-20, Triethylcitrat, PEG-20-Methylglucosesesquistearat, Ceteareth-12, Gly- cerylstearatcitrat, Cetylphosphat, Triceteareth-4-Phosphat, Trilaureth-4-Phosphat, Polygly- cerylmethylglucosedistearat, Kaliumcetylphosphat, lsosteareth-10, Polyglyceryl-2-sesquiiso- stearat, Ceteth-10, Oleth-20, lsoceteth-20, Glycerylstearat im Gemisch mit Ceteareth-20, Ceteareth-12, Cetylstearylalkohol und Cetylpalmitat, Cetylstearylalkohol im Gemisch mit PEG- 20 Stearat, PEG-30-Stearat, PEG-40-Stearat, PEG-100-Stearat.Glyceryl stearate in a mixture with ceteareth-20, ceteareth-25, ceteareth-6 in a mixture with stearyl alcohol, cetylstearyl alcohol in a mixture with PEG-40 castor oil and sodium cetylstearylsulfate, triceteareth-4 phosphate, sodium cetylstearylsulfate, 4-phosphate, lecithin, lecithin Phosphate, stearic acid, propylene glycol stearate SE, PEG-25 hydrogenated castor oil, PEG-54 hydrogenated castor oil, PEG-6 caprylic acid / capric acid glycerides, glyceryl oleate in a mixture with propylene glycol, ceteth-2, ceteth-20, polysorbate 60, with a mixture of glyceryl stearate -100 stearate, laureth-4, ceteareth-3, isostearylglyceryl ether, cetylstearyl alcohol mixed with sodium cetylstearyl sulfate, laureth-23, steareth-2, glyceryl stearate mixed with PEG-30 stearate, PEG-40 stearate, glycol distearate, PEG-22 -Dodecyl glycol copolymer, polyglyceryl-2-PEG-4 stearate, ceteareth-20, methylglucose sesquistearate, steareth-10, PEG-20 stearate, steareth-2 in a mixture with PEG-8 distearate, steareth-21, steareth-20, Isosteareth-2 0, PEG-45 / dodecyl glycol copolymer, methoxy-PEG-22 / dodecyl glycol copolymer, PEG-20 glyceryl stearate, PEG-20 glyceryl stearate, PEG-8 beeswax, polyglyceryl-2-laurate, isostearyl diglyceryl succinate, stearamidopropyl PG-dimonium chloride phosphate, glyceryl stearate SE, ceteth-20, triethyl citrate, PEG-20 methyl glucose sesquistearate, ceteareth-12, glyceryl stearate citrate, cetyl phosphate, triceteareth-4-phosphate, trilaureth-4-phosphate, polyglyceryl stearate , Polyglyceryl-2-sesquiiso stearate, ceteth-10, oleth-20, isoceteth-20, glyceryl stearate in a mixture with ceteareth-20, ceteareth-12, cetyl stearyl alcohol and cetyl palmitate, cetyl stearyl alcohol in a mixture with PEG-20 stearate, PEG Stearate, PEG-40 stearate, PEG-100 stearate.
Erfindungsgemäße Emulsionen im Sinne der vorliegenden Erfindung, z.B. in Form einer Hautschutzcreme, einer Hautlotion, einer kosmetischen Milch, beispielsweise in Form einer Sonnenschutzcreme oder einer Sonnenschutzmilch, 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. Ebenso wie Emulsionen von flüssiger und fester Konsistenz als kosmetische Reinigungslotionen oder Reinigungscremes Verwendung finden, können auch die erfindungsgemäßen Zubereitungen versprühbare Reinigungszubereitungen („Reinigungssprays") darstellen, welche beispielsweise zum Entfernen von Schminken und/oder Make-up oder als milde Waschlotion - ggf. auch für unreine Haut - verwendet werden. Derartige Reinigungszubereitungen können vorteilhaft femer als sogenannte „rinse-off-Präparate" angewendet werden, welche nach der Anwendung von der Haut abgespült werdenEmulsions according to the invention in the sense of the present invention, for example in the form of a skin protection cream, a skin lotion, a cosmetic milk, for example in the form of a sun protection cream or a sun protection milk, are advantageous and contain, for example, fats, oils, waxes and / or other fat bodies, as well as water and one or several emulsifiers, as are usually used for such a type of formulation. Just as emulsions of liquid and solid consistency are used as cosmetic cleansing lotions or cleansing creams, the preparations according to the invention can also be sprayable cleansing preparations (“cleaning sprays”) which, for example, for removing make-up and / or make-up or as a mild washing lotion - if appropriate also for impure skin. Such cleaning preparations can also advantageously be used as so-called "rinse-off preparations" which are rinsed off the skin after use
Es ist dem Fachmanne natürlich bekannt, daß anspruchsvolle kosmetische Zusammensetzungen zumeist nicht ohne die üblichen Hilfs- und Zusatzstoffe denkbar sind. Darunter zählen beispielsweise Konsistenzgeber, Füllstoffe, Parfüm, Farbstoffe, Emulgatoren, zusätzliche Wirkstoffe wie Vitamine oder Proteine, Lichtschutzmittel, Stabilisatoren, Insektenrepellentien, Alkohol, Wasser, Salze, antimikrobiell, proteolytisch oder keratolytisch wirksame Substanzen usw.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. These include, for example, consistency agents, fillers, perfumes, dyes, emulsifiers, additional active ingredients such as vitamins or proteins, light stabilizers, stabilizers, insect repellents, alcohol, water, salts, antimicrobial, proteolytic or keratolytically active substances, etc.
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 der Regel ein oder mehrere Medikamente in wirksamer Konzentration. Der Einfachheit 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 in the sense 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.
Entsprechend können kosmetische oder topische dermatologische Zusammensetzungen im Sinne der vorliegenden Erfindung, je nach ihrem Aufbau, beispielsweise verwendet werden als Hautschutzcreme, Reinigungsmilch, Sonnenschutzlotion, Nährcreme, Tages- oder Nachtcreme usw. Es ist gegebenenfalls möglich und vorteilhaft, die erfindungsgemäßen Zusammensetzungen als Grundlage für pharmazeutische Formulierungen zu verwenden.Accordingly, cosmetic or topical dermatological compositions within the meaning of the present invention, depending on their structure, can be used, for example, as skin protection cream, cleansing milk, sunscreen lotion, nutritional cream, day or night cream, etc. It may be possible and advantageous to use the compositions according to the invention as a basis for pharmaceuticals Use wording.
Es ist ebenfalls von Vorteil, von den erfindungsgemäßen Eigenschaften in Form von dekorativen Kosmetika (Make-Up-Formulierungen) Gebrauch zu machen. Günstig sind auch solche kosmetischen und dermatologischen Zubereitungen, die in der Form eines Sonnenschutzmittels vorliegen. Vorzugsweise enthalten diese neben dem erfindungsgemäß verwendeten Wirkstoff zusätzlich mindestens eine UVA-Filtersubstanz und/oder mindestens eine UVB-Filtersubstanz und/oder mindestens ein anorganisches Pigment.It is also advantageous to make use of the properties according to the invention in the form of decorative cosmetics (make-up formulations). Cosmetic and dermatological preparations which are in the form of a sunscreen are also favorable. In addition to the active ingredient used according to the invention, these preferably additionally contain at least one UVA filter substance and / or at least one UVB filter substance and / or at least one inorganic pigment.
Es ist aber auch vorteilhaft im Sinne der vorliegenden Erfindungen, solche kosmetischen und dermatologischen Zubereitungen zu erstellen, deren hauptsächlicher Zweck nicht der Schutz vor Sonnenlicht ist, die aber dennoch einen Gehalt an UV-Schutzsubstanzen enthalten. So werden beispielsweise in Tagescremes gewöhnlich UV-A- bzw. UV-B-Filtersubstanzen eingearbeitet.However, it is also advantageous in the sense of the present inventions to create cosmetic and dermatological preparations whose main purpose is not protection against sunlight, but which nevertheless contain UV protection substances. For example, UV-A or UV-B filter substances are usually incorporated into day creams.
Vorteilhaft können erfindungsgemäße Zubereitungen 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 bis 6 Gew.-% beträgt, bezogen auf das Gesamtgewicht der Zubereitungen.Preparations according to the invention can 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, in particular 1 to 6% by weight, based on the total weight of the preparations.
Die UVB-Filter können öllöslich oder wasserlöslich sein. Als öllösliche Substanzen sind z.B. zu nennen:The UVB filters can be oil-soluble or water-soluble. As oil-soluble substances e.g. to call:
3-Benzylidencampher und dessen Derivate, z.B. 3-(4-Methylbenzyliden)campher,3-benzylidene camphor and its derivatives, e.g. 3- (4-methylbenzylidene) camphor,
4-Aminobenzoesäure-Derivate, vorzugsweise 4-(Dimethylamino)-benzoesäure(2-ethyl- hexyl)ester, 4-(Dimethylamino)benzoesäureamylester;4-aminobenzoic acid derivatives, preferably 4- (dimethylamino) benzoic acid (2-ethyl-hexyl) ester, 4- (dimethylamino) benzoic acid amyl ester;
Ester der Zimtsäure, vorzugsweise 4-Methoxyzimtsäure(2-ethylhexyl)ester, 4-Meth- oxyzimtsäureisopentylester;Esters of cinnamic acid, preferably 4-methoxycinnamic acid (2-ethylhexyl) ester, 4-methoxycinnamic acid isopentyl ester;
Ester der Salicylsäure, vorzugsweise Salicylsäure(2-ethylhexyl)ester, Salicylsäure(4- isopropylbenzyl)ester, Salicylsäurehomomenthylester;Esters of salicylic acid, preferably salicylic acid (2-ethylhexyl) ester, salicylic acid (4-isopropylbenzyl) ester, salicylic acid homomethyl ester;
Derivate des Benzophenons, vorzugsweise 2-Hydroxy-4-methoxybenzophenon, 2-Derivatives of benzophenone, preferably 2-hydroxy-4-methoxybenzophenone, 2-
Hydroxy-4-methoxy-4'-methylbenzophenon, 2,2'-Dihydroxy-4-methoxybenzophenon;Hydroxy-4-methoxy-4'-methylbenzophenone, 2,2'-dihydroxy-4-methoxybenzophenone;
Ester der Benzalmalonsäure, vorzugsweise 4-Methoxybenzalmalonsäuredi(2-ethyl- hexyl)ester;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-triazin2,4,6-trianilino- (p-carbo-2'-ethyl-1 , -hexyloxy) -1,3,5-triazine
Als wasserlösliche Substanzen sind vorteilhaft: 2-Phenylbenzimidazol-5-sulfonsäure und deren Salze, z.B. Natrium-, Kalium- oder Tri- ethanolammonium-Salze,The following are advantageous as water-soluble substances: 2-phenylbenzimidazole-5-sulfonic acid and its salts, for example sodium, potassium or triethanolammonium salts,
Sulfonsäure-Derivate von Benzophenonen, vorzugsweise 2-Hydroxy-4-methoxyben- zophenon-5-sulfonsäure und ihre Salze;Sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and its salts;
Sulfonsäure-Derivate des 3-Benzylidencamphers, wie z.B. 4-(2-Oxo-3-bornyliden- methyl)benzolsulfonsäure, 2-Methyl-5-(2-oxo-3-bomylidenmethyl)sulfonsäure und ihreSulfonic acid derivatives of 3-benzylidene camphor, e.g. 4- (2-oxo-3-bornylidene-methyl) benzenesulfonic acid, 2-methyl-5- (2-oxo-3-bomylidene-methyl) sulfonic acid and their
Salze.Salts.
Die Liste der genannten UVB-Filter, die erfindungsgemäß Verwendung finden können, soll selbstverständlich nicht limitierend sein.The list of UVB filters mentioned, which can be used according to the invention, is of course not intended to be limiting.
Es kann auch von Vorteil sein, in erfindungsgemäßen Zubereitungen UVA-Filter einzusetzen, die üblicherweise in kosmetischen und/oder dermatologischen Zubereitungen enthalten sind. Bei solchen Filtersubstanzen handelt es sich vorzugsweise um Derivate des Dibenzoylme- thans, insbesondere um 1-(4'-tert.Butylphenyl)-3-(4'-methoxyphenyl)propan-1 ,3-dion und um 1-Phenyl-3-(4'-isopropylphenyl)propan-1,3-dion. Auch Zubereitungen, die diese Kombinationen enthalten, sind Gegenstand der Erfindung. Es können die gleichen Mengen an UVA- Filtersubstanzen verwendet werden, welche für UVB-Filtersubstanzen genannt wurden.It can also be advantageous to use UVA filters in the preparations according to the invention, which are usually contained in cosmetic and / or dermatological preparations. Such filter 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. Preparations containing these combinations are also the subject of the invention. The same amounts of UVA filter substances that were mentioned for UVB filter substances can be used.
Kosmetische und/oder dermatologische Zubereitungen im Sinne der vorliegenden Erfindung können auch anorganische Pigmente enthalten, die üblicherweise in der Kosmetik zum Schütze der Haut vor UV-Strahlen verwendet werden. Dabei handelt es sich um Oxide des Titans, Zinks, Eisens, Zirkoniums, Siliciums, Mangans, Aluminiums, Cers und Mischungen davon, sowie Abwandlungen, bei denen die Oxide die aktiven Agentien sind. Besonders bevorzugt handelt es sich um Pigmente auf der Basis von Titandioxid. Es können die für die vorstehenden Kombinationen genannten Mengen verwendet werden.Cosmetic and / or dermatological preparations in the sense of the present invention can also contain inorganic pigments which are usually used in cosmetics to protect the skin from UV rays. These are oxides of titanium, zinc, iron, zirconium, silicon, manganese, aluminum, cerium and mixtures thereof, as well as modifications in which the oxides are the active agents. It is particularly preferred to use pigments based on titanium dioxide. The amounts given for the above combinations can be used.
Die erfindungsgemäßen kosmetischen und dermatologischen Zubereitungen können kosmetische Wirk-, Hilfs- und/oder Zusatzstoffe enthalten, wie sie üblicherweise in solchen Zubereitungen verwendet werden, z.B. Antioxidationsmittel, Konservierungsmittel, Bakterizide, Parfüme, Substanzen zum Verhindern des Schäumens, Farbstoffe, Pigmente, die färbende Wirkung haben, Verdickungsmittel, oberflächenaktive Substanzen, Emulgatoren, weichmachende, anfeuchtende und/oder feuchthaltende Substanzen, Fette, Öle, Wachse oder andere übliche Bestandteile einer kosmetischen oder dermatologischen Formulierung wie Alkohole, Polyole, Polymere, Schaumstabilisatoren, Elektrolyte, organische Lösungsmittel oder Silikonderivate.The cosmetic and dermatological preparations according to the invention can contain cosmetic active ingredients, auxiliaries and / or additives, as are usually used in such preparations, for example antioxidants, preservatives, bactericides, perfumes, substances for preventing foaming, dyes, pigments, the coloring effect have thickeners, surface-active substances, emulsifiers, softening, moisturizing and / or moisturizing substances, fats, oils, waxes or other usual components of a cosmetic or dermatological formulation such as alcohols, Polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
Es ist vorteilhaft, den Zubereitungen im Sinne der vorliegenden Erfindung weitere antiirritati- ve oder antientzündliche Wirkstoffe zuzugeben, insbesondere Batylalkohol (α-Octadecylgly- cerylether), Selachylalkohol (α-9-Octadecenylglycerylether), Chimylalkohol (α-Hexadecylgly- cerylether), Bisabolol und/oder Panthenol.For the purposes of the present invention, it is advantageous to add further anti-irritant or anti-inflammatory active ingredients, in particular batyl alcohol (α-octadecylglyceryl ether), selachyl alcohol (α-9-octadecenylglyceryl ether), chimyl alcohol (α-hexadecylglyceryl ether), bisabolol and / or panthenol.
Es ist ebenfalls vorteilhaft, den Zubereitungen im Sinne der vorliegenden Erfindung übliche Antioxidantien zuzufügen. Erfindungsgemäß können als günstige Antioxidantien alle für kosmetische und/oder dermatologische Anwendungen geeigneten oder gebräuchlichen Antioxidantien verwendet werden.It is also advantageous to add customary antioxidants to the preparations for the purposes of the present invention. According to the invention, all the antioxidants suitable or customary for cosmetic and / or dermatological applications can be used as favorable antioxidants.
Vorteilhaft werden die Antioxidantien gewählt aus der Gruppe bestehend aus Aminosäuren (z.B. Glycin, Histidin, Tyrosin, Tryptophan) und deren Derivate, Imidazole (z.B. Urocaninsäu- re) und deren Derivate, Peptide wie D,L-Carnosin, D-Carnosin, L-Camosin und deren Derivate (z.B. Anserin), Carotinoide, Carotine (z.B. α-Carotin, ß-Carotin, ψ-Lycopin) und deren Derivate, Chlorogensäure und deren Derivate, Aurothioglucose, Propylthiouracil und andere Thiole (z.B. Thioredoxin, Glutathion, Cystein, Cystin, Cystamin und deren Glycosyl-, N-Ace- tyl-, Methyl-, Ethyl-, Propyl-, Amyl-, Butyl- und Lauryl-, Palmitoyl-, Oleyl-, γ-Linoleyl-, Cho- lesteryl- und Glycerylester) sowie deren Salze, Dilaurylthiodipropionat, Distearylthiodipropio- nat, Thiodipropionsäure und deren Derivate (Ester, Ether, Peptide, Lipide, Nukleotide, Nukleoside und Salze) sowie Sulfoximinverbindungen (z.B. Buthioninsulfoximine, Homocy- steinsulfoximin, Buthioninsulfone, Penta-, Hexa-, Heptathioninsulfoximin) in sehr geringen verträglichen Dosierungen (z.B. pmol bis μmol/kg), ferner (Metall)-Chelatoren (z.B. α-Hy- droxyfettsäuren, Palmitinsäure, Phytinsäure, Lactoferrin), α-Hydroxysäuren (z.B. Citro- nensäure, Milchsäure, Apfelsäure), Huminsäure, Gallensäure, Gallenextrakte, Bilirubin, Bili- verdin, EDTA, EGTA und deren Derivate, ungesättigte Fettsäuren und deren Derivate (z.B. γ- Linolensäure, Linolsäure, Ölsäure), Folsäure und deren Derivate, Furfurylidensorbitol und dessen 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), sowie Koniferylbenzoat des Benzoeharzes, Ferulasäure, Furfurylidenglu- citol, Carnosin, Butylhydroxytoluol, Butylhydroxyanisol, Nordihydroguajakharzsäure, Nordihy- droguajaretsäure, Trihydroxybutyrophenon, Harnsäure und deren Derivate, Mannose und deren Derivate, Zink und dessen Derivate (z.B. ZnO, ZnSO4) Selen und dessen Derivate (z.B. Selenmethionin), Stilbene und deren Derivate (z.B. Stilbenoxid, Trans-Stilbenoxid) und die erfindungsgemäß geeigneten Derivate (Salze, Ester, Ether, Zucker, Nukleotide, Nukleo- side, Peptide und Lipide) dieser genannten Wirkstoffe.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- Camosin and its derivatives (e.g. anserine), carotenoids, carotenes (e.g. α-carotene, ß-carotene, ψ-lycopene) and their derivatives, chlorogenic acid and their derivatives, aurothioglucose, propylthiouracil and other thiols (e.g. thioredoxin, glutathione, cysteine, cystine , Cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl, γ-linoleyl, cholesterol and glyceryl esters) as well as their salts, dilaurylthiodipropionate, distearylthiodipropionate, thiodipropionic acid and their derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) as well as sulfoximine compounds (for example buthioninsulfoximines, homocystinsulfoximine, buthioninsulfones), pentathione sulfoximine, penta-, hexa-, hexa-, hexa- very low vert conventional dosages (eg pmol to μmol / kg), also (metal) chelators (eg α-hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), α-hydroxy acids (eg citric acid, lactic acid, malic acid), humic acid, bile acid, Bile extracts, bilirubin, biliquin, EDTA, EGTA and their derivatives, unsaturated fatty acids and their derivatives (eg γ-linolenic acid, linoleic acid, oleic acid), folic acid and their derivatives, furfurylidene sorbitol and its derivatives, ubiquinone and ubiquinol and their derivatives, vitamin C and derivatives (e.g. ascorbyl palmitate, Mg ascorbyl phosphate, ascorbylacetate), tocopherols and derivatives (e.g. vitamin E acetate), as well as coniferyl benzoate of benzoin, ferulic acid, furfurylidene glucitolol, carnosine, butylated hydroxytoluene, butylated hydroxyanidic acid, northern dihydrogenated acid, nordihyduated hydroxy acid, nordihyduated hydroxy acid, nordihyduated hydroxychloride, Uric acid and its derivatives, mannose and their derivatives, zinc and their derivatives (for example ZnO, ZnSO 4 ) selenium and their derivatives (for example selenium methionine), stilbenes and their derivatives (for example stilbene oxide, trans-stilbene oxide) and the derivatives suitable according to the invention (salts, esters, ethers, sugars, nucleotides) , Nucleosides, peptides and lipids) of these active ingredients.
Die Menge der Antioxidantien (eine oder mehrere Verbindungen) in den Zubereitungen beträgt vorzugsweise 0,001 bis 30 Gew.-%, besonders bevorzugt 0,05 - 20 Gew.-%, insbesondere 1 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitung.The amount of the antioxidants (one or more compounds) in the preparations is preferably 0.001 to 30% by weight, particularly preferably 0.05 to 20% by weight, in particular 1 to 10% by weight, based on the total weight of the preparation ,
Sofern Vitamin E und/oder dessen Derivate das oder die Antioxidantien darstellen, ist vorteilhaft, deren jeweilige Konzentrationen aus dem Bereich von 0,001 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Formulierung, zu wählen.If vitamin E and / or its derivatives represent the antioxidant (s), it is advantageous to choose their respective concentrations from the range of 0.001-10% by weight, based on the total weight of the formulation.
Zubereitungen gemäß der vorliegenden Erfindung können auch Verwendung als Grundlage für kosmetische oder dermatologische Desodorantien bzw. Antitranspirantien finden. Alle für Desodorantien bzw. Antitranspirantien gängigen Wirkstoffe können vorteilhaft genutzt werden, beispielsweise Geruchsüberdecker wie die gängigen Parfümbestandteile, Geruchsabsorber, beispielsweise die in der Patentoffenlegungsschrift DE-P 40 09 347 beschriebenen Schichtsilikate, von diesen insbesondere Montmorillonit, Kaolinit, llit, Beidellit, Nontronit, Sa- ponit, Hectorit, Bentonit, Smectit, ferner beispielsweise Zinksalze der Ricinolsäure.Preparations according to the present invention can also be used as a basis for cosmetic or dermatological deodorants or antiperspirants. All active ingredients common to deodorants or antiperspirants can be used advantageously, for example odor maskers such as the common perfume components, odor absorbers, for example the layered silicates described in patent application DE-P 40 09 347, of which in particular montmorillonite, kaolinite, llite, beidellite, nontronite, Sa. - ponite, hectorite, bentonite, smectite, furthermore, for example, zinc salts of ricinoleic acid.
Keimhemmende Mittel sind ebenfalls geeignet, in die erfindungsgemäßen Zubereitungen eingearbeitet zu werden. Vorteilhafte Substanzen sind zum Beispiel 2,4,4'-Trichlor-2'-hydra- xydiphenylether (Irgasan), 1 ,6-Di-(4-chlorphenylbiguanido)-hexan (Chlorhexidin), 3,4,4'-Tri- chlorcarbanilid, quatemäre Ammoniumverbindungen, Nelkenöl, Minzöl, Thymianöl, Triethylci- trat, Farnesol (3,7,11-Trimethyl-2,6,10-dodecatrien-1-ol) sowie die in den Patentoffenle- gungsschriften DE-37 40 186, DE-39 38 140, DE-42 04 321, DE-42 29 707, DE-43 09 372, DE-44 11 664, DE-195 41 967, DE-195 43 695, DE-195 43 696, DE-195 47 160, DE-196 02 108, DE-196 02 110, DE-196 02 111, DE-196 31 003, DE-196 31 004 und DE-196 34 019 und den Patentschriften DE-42 29 737, DE-42 37 081 , DE-43 24 219, DE-44 29 467, DE-44 23 410 und DE-195 16 705 beschriebenen Wirkstoffe bzw. Wirkstoffkombinationen. Auch Natriumhydrogencarbonat ist vorteilhaft zu verwenden. Die Menge solcher Wirkstoffe (eine oder mehrere Verbindungen) in den Zubereitungen gemäß der Erfindung beträgt vorzugsweise 0,001 bis 30 Gew.-%, besonders bevorzugt 0,05 - 20 Gew.-%, insbesondere 1 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitung.Germ-inhibiting agents are also suitable for being incorporated into the preparations according to the invention. Examples of advantageous substances are 2,4,4'-trichloro-2'-hydroxydiphenyl ether (irgasane), 1,6-di- (4-chlorophenylbiguanido) hexane (chlorhexidine), 3,4,4'-tri- chlorocarbanilide, quaternary ammonium compounds, clove oil, mint oil, thyme oil, triethyl citrate, farnesol (3,7,11-trimethyl-2,6,10-dodecatrien-1-ol) and those described in the patent documents DE-37 40 186, DE-39 38 140, DE-42 04 321, DE-42 29 707, DE-43 09 372, DE-44 11 664, DE-195 41 967, DE-195 43 695, DE-195 43 696, DE- 195 47 160, DE-196 02 108, DE-196 02 110, DE-196 02 111, DE-196 31 003, DE-196 31 004 and DE-196 34 019 and the patents DE-42 29 737, DE- 42 37 081, DE-43 24 219, DE-44 29 467, DE-44 23 410 and DE-195 16 705 described active ingredients or combinations of active ingredients. Sodium hydrogen carbonate can also be used advantageously. The amount of such active substances (one or more compounds) in the preparations according to the invention is preferably 0.001 to 30% by weight, particularly preferably 0.05-20% by weight, in particular 1-10% by weight, based on the Total weight of the preparation.
Die Wasserphase der kosmetischen Zubereitungen im Sinne der vorliegenden Erfindung kann auch Gelcharakter aufweisen, die neben einem wirksamen Gehalt am erfindungsgemäß eingesetzten Substanzen und dafür üblicherweise verwendeten Lösungsmitteln, bevorzugt Wasser, noch weitere organische Verdickungsmittel, z.B. Gummiarabikum, Xanthan- gummi, Natriumalginat, Stärke und Stärkederivate (z.B. Distärkephosphat), Cellulose, Cellu- lose-Derivate, vorzugsweise Methylcellulose, Hydroxymethylcellulose, Hydroxyethylcellulose, Hydroxypropylcellulose, Hydroxypropylmethylcellulose oder anorganische Verdickungsmittel, z. B. Aluminiumsilikate wie beispielsweise organisch modifizierte oder auch unmodifizierte Hectorite, Bentonite, oder dergleichen, oder ein Gemisch aus Polyethylenglykol und Poly- ethylenglykolstearat oder -distearat, enthalten. Das Verdickungsmittel ist in dem Gel z.B. in einer Menge zwischen 0,1 und 30 Gew.-%, bevorzugt zwischen 0,5 und 15 Gew.-%, enthalten.The water phase of the cosmetic preparations in the sense of the present invention can also have a gel character which, in addition to an effective content of the substances used according to the invention and solvents usually used for this purpose, preferably water, also further organic thickeners, e.g. Gum arabic, xanthan gum, sodium alginate, starch and starch derivatives (e.g. distarch phosphate), cellulose, cellulose derivatives, preferably methyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose or inorganic thickeners, e.g. B. aluminum silicates such as organically modified or unmodified hectorites, bentonites, or the like, or a mixture of polyethylene glycol and polyethylene glycol stearate or distearate. The thickener is in the gel e.g. in an amount between 0.1 and 30% by weight, preferably between 0.5 and 15% by weight.
Ferner kann es von Vorteil sein, Zubereitungen gemäß der Erfindung grenz- bzw. oberflächenaktive Agentien zuzufügen, beispielsweise kationische Emulgatoren wie insbesondere quatemäre Tenside.It may also be advantageous to add surface-active or surface-active agents to preparations according to the invention, for example cationic emulsifiers such as, in particular, quaternary surfactants.
Quatemäre Tenside enthalten mindestens ein N-Atom, das mit 4 Alkyl- oder Arylgruppen ko- valent 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 Benzyltrialkyl- ammoniumchloride oder -bromide, wie beispielsweise Benzyldimethylstearylammoniumchlo- rid, ferner Alkyltrialkylammoniumsalze, beispielsweise beispielsweise Cetyltrimethylammoni- umchlorid oder -bromid, Alkyldimethylhydroxyethylammoniumchloride oder -bromide, Dialkyl- dimethylammoniumchloride oder -bromide, Alkylamidethyltrimethylammoniumethersulfate, Alkylpyridiniumsalze, beispielsweise Lauryl- oder Cetylpyrimidiniumchlorid, Imidazolinderiva- te und Verbindungen mit kationischem Charakter wie Aminoxide, beispielsweise Alkyldime- thyla inoxide oder Alkylaminoethyldimethylaminoxide. Vorteilhaft sind insbesondere Cetyltri- methylammoniumsalze zu verwenden. Vorteilhaft ist auch, kationische Polymere (z.B. Jaguar® C 162 [Hydroxypropyl Guar Hydro- xypropyltrimonium Chloride] bzw. modifizierten Magnesiumaluminiumsilikaten (z.B. Qua- temium-18-Hectorit, welches z. B. unter der Handelsbezeichnung Bentone® 38 bei der Firma Rheox erhältlich ist, oder Stearalkonium Hectorit, welches z. B. unter der Handelsbezeichnung Softisan® Gel bei der Hüls AG erhältlich ist), einzusetzen.Quaternary surfactants contain at least one N atom, which is linked 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 according to the invention can furthermore preferably be selected from the group of the quaternary ammonium compounds, in particular benzyltrialkylammonium chlorides or bromides, such as, for example, benzyldimethylstearylammonium chloride, and furthermore alkyltrialkylammonium salts, for example, for example cetyltrimethylammonium chloride or bromide, or alkyldimbromide, alkylammonium bromide or dimethylammonium chlorides or bromides, alkylamidethyltrimethylammonium ether sulfates, alkylpyridinium salts, for example lauryl or cetylpyrimidinium chloride, imidazoline derivatives and compounds with a cationic character such as amine oxides, for example alkyldimethylamineoxides or alkylaminoethyldimethylamine oxides. Cetyltrimethylammonium salts are particularly advantageous to use. It is also advantageous to use cationic polymers (for example Jaguar® C 162 [hydroxypropyl guar hydroxypropyltrimonium chloride) or modified magnesium aluminum silicates (for example Quatemium-18-hectorite, which is available, for example, from Rheox under the trade name Bentone® 38) or stearalkonium hectorite, which is available, for example, under the trade name Softisan® Gel from Hüls AG).
Erfindungsgemäße Zubereitungen können vorteilhaft auch Ölverdickungsmittel enthalten, um die taktilen Eigenschaften der Emulsion und die Stiftkonsistenz zu verbessern. Vorteilhafte Ölverdickungsmittel im Sinne der vorliegenden Erfindung sind beispielsweise weitere Feststoffe, wie z. B. hydrophobe Siliciumoxide des Typs Aerosil®, welche von der Degussa AG erhältlich sind. Vorteilhafte Aerosil®-Typen sind beispielsweise Aerosil® OX50, Aerosil® 130, Aerosil® 150, Aerosil® 200, Aerosil® 300, Aerosil® 380, Aerosil® MOX 80, Aerosil® MOX 170, Aerosil® COK 84, Aerosil® R 202, Aerosil® R 805, Aerosil® R 812, Aerosil® R 972, Aerosil® R 974 und/oder Aerosil® R976.Preparations according to the invention can advantageously also contain oil thickeners in order to improve the tactile properties of the emulsion and the stick consistency. Advantageous oil thickeners for the purposes of the present invention are, for example, other solids, such as, for. B. hydrophobic silicon oxides of the type Aerosil®, which are available from Degussa AG. Examples of advantageous Aerosil® grades are Aerosil® OX50, Aerosil® 130, Aerosil® 150, Aerosil® 200, Aerosil® 300, Aerosil® 380, Aerosil® MOX 80, Aerosil® MOX 170, Aerosil® COK 84, Aerosil® R 202 , Aerosil® R 805, Aerosil® R 812, Aerosil® R 972, Aerosil® R 974 and / or Aerosil® R976.
Ferner sind auch sogenannte Metallseifen (d. h. die Salze höherer Fettsäuren mit Ausnahme der Alkalisalze) vorteilhafte Ölverdickungsmittel im Sinne der vorliegenden Erfindung, wie beispielsweise Aluminium-Stearat, Zink-Stearat und/oder Magnesium-Stearat.Furthermore, so-called metal soaps (i.e. the salts of higher fatty acids with the exception of the alkali salts) are also advantageous oil thickeners for the purposes of the present invention, such as, for example, aluminum stearate, zinc stearate and / or magnesium stearate.
Ebenfalls vorteilhaft ist, Zubereitungen gemäß der Erfindung amphotere bzw. zwitterionische Tenside (z.B. Cocoamidopropylbetain) und Moisturizer (z.B. Betain) zuzusetzen. Vorteilhaft zu verwendende amphotere Tenside sind beispielsweise Acyl-/dialkylethylendiamin, beispielsweise Natriumacylamphoacetat, Dinatriumacylamphodipropionat, Dinatriumalkylam- phodiacetat, Natriumacylamphohydroxypropylsulfonat, Dinatriumacylamphodiacetat und Na- triumacylamphopropionat, N-Alkylaminosäuren, beispielsweise Aminopropylalkylglutamid, Al- kylaminopropionsäure, Natriumalkylimidodipropionat und Lauroamphocarboxyglycinat.It is also advantageous to add amphoteric or zwitterionic surfactants (e.g. cocoamidopropyl betaine) and moisturizers (e.g. betaine) to preparations according to the invention. Amphoteric surfactants to be used advantageously are, for example, acyl / dialkylethylenediamine, for example sodium acylamphoacetate, disodium acylamphodipropionate, disodium alkylamphodiacetate, sodium acylamphohydroxypropylsulfonate, disodium acylamphodiacetate and sodium triumacylamphopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropyl aminopropylate aminopropyl aminopropylate aminopropyl aminopropylate, for example
Die Menge der ober- bzw. grenzflächenaktiven Substanzen (eine oder mehrere Verbindungen) in den Zubereitungen gemäß der Erfindung beträgt vorzugsweise 0,001 bis 30 Gew.-%, besonders bevorzugt 0,05 - 20 Gew.-%, insbesondere 1 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitung. Eine erstaunliche Eigenschaft der erfindungsgemäße Zubereitungen ist, daß diese sehr gute Vehikel für kosmetische oder dermatologische Wirkstoffe in die Haut sind, wobei bevorzugte Wirkstoffe die vorab erwähnten Antioxidantien sind, welche die Haut vor oxidativer Beanspruchung schützen können.The amount of surface-active or surface-active substances (one or more compounds) in the preparations according to the invention is preferably 0.001 to 30% by weight, particularly preferably 0.05-20% by weight, in particular 1-10% by weight. %, based on the total weight of the preparation. An astonishing property of the preparations according to the invention is that they are very good vehicles for cosmetic or dermatological active ingredients in the skin, preferred active ingredients being the aforementioned antioxidants, which can protect the skin against oxidative stress.
Erfindungsgemäß können die Wirkstoffe (eine oder mehrere Verbindungen) auch sehr vorteilhaft gewählt werden aus der Gruppe der lipophilen Wirkstoffe, insbesondere aus folgender Gruppe:According to the invention, the active ingredients (one or more compounds) can also be selected very advantageously from the group of lipophilic active ingredients, in particular from the following group:
Acetylsalicylsäure, Atropin, Azulen, Hydrocortison und dessen Derivaten, z. B. Hydrocor- tison-17-valerat, Vitamine der B- und D-Reihe, sehr günstig das Vitamin B-i, das Vitamin Bι2 das Vitamin Di, aber auch Bisabolol, ungesättigte Fettsäuren, namentlich die essentiellen Fettsäuren (oft auch Vitamin F genannt), insbesondere die gamma-Linolensäure, Ölsäure, Eicosapentaensäure, Docosahexaensäure und deren Derivate, Chloramphenicol, Coffein, Prostaglandine, Thymol, Campher, Extrakte oder andere Produkte pflanzlicher und tierischer Herkunft, z. B. Nachtkerzenöl, Borretschöl oder Johannisbeerkernöl, Fischöle, Lebertran aber auch Ceramide und cera idähnliche Verbindungen und so weiter.Acetylsalicylic acid, atropine, azulene, hydrocortisone and its derivatives, e.g. B. Hydrocortisone-17-valerate, vitamins of the B and D series, very cheap the vitamin Bi, the vitamin Bι 2, the vitamin Di, but also bisabolol, unsaturated fatty acids, especially the essential fatty acids (often called vitamin F) ), in particular gamma-linolenic acid, oleic acid, eicosapentaenoic acid, docosahexaenoic acid and its derivatives, chloramphenicol, caffeine, prostaglandins, thymol, camphor, extracts or other products of plant and animal origin, e.g. B. evening primrose oil, borage oil or currant seed oil, fish oils, cod liver oil but also ceramides and cera-like compounds and so on.
Vorteilhaft ist es auch, die Wirkstoffe aus der Gruppe der rückfettenden Substanzen zuIt is also advantageous to add the active ingredients from the group of refatting substances
® ® wählen, beispielsweise Purcellinöl, Eucerit und Neocerit .Choose ® ®, for example Purcellinöl, Eucerit and Neocerit.
Besonders vorteilhaft werden der oder die Wirkstoffe ferner gewählt aus der Gruppe der NO- Synthasehemmer, insbesondere wenn die erfindungsgemäßen Zubereitungen zur Behandlung und Prophylaxe der Symptome der intrinsischen und/oder extrinsischen Hautalterung sowie zur Behandlung und Prophylaxe der schädlichen Auswirkungen ultravioletter Strahlung auf die Haut dienen sollen.The active ingredient (s) are particularly advantageously selected from the group of NO synthase inhibitors, in particular if the preparations according to the invention are intended 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 ,
Bevorzugter NO-Synthasehemmer ist das Nitroarginin.The preferred NO synthase inhibitor is nitroarginine.
Weiter vorteilhaft werden der oder die Wirkstoffe gewählt aus der Gruppe, welche Catechine und Gallensäureester von Catechinen und wäßrige bzw. organische Extrakte aus Pflanzen oder Pflanzenteilen umfaßt, die einen Gehalt an Catechinen oder Gallensäureestem von Catechinen aufweisen, wie beispielsweise den Blättern der Pflanzenfamilie Theaceae, insbesondere der Spezies Camellia sinensis (grüner Tee). Insbesondere vorteilhaft sind deren typische Inhaltsstoffe (wie z. B. Polyphenole bzw. Catechine, Coffein, Vitamine, Zucker, Mineralien, Aminosäuren, Lipide).The active ingredient (s) are also advantageously selected from the group comprising catechins and bile esters of catechins and aqueous or organic extracts from plants or parts of plants which contain catechins or bile esters of catechins, such as, for example, the leaves of the Theaceae plant family, in particular of the species Camellia sinensis (green tea). Their are particularly advantageous typical ingredients (such as polyphenols or catechins, caffeine, vitamins, sugar, minerals, amino acids, lipids).
Catechine stellen eine Gruppe von Verbindungen dar, die als hydrierte Flavone oder An- thocyanidine aufzufassen sind und Derivate des „Catechins" (Catechol, 3,3',4',5,7-Fla- vanpentaol, 2-(3,4-Dihydroxyphenyl)-chroman-3,5,7-triol) darstellen. Auch Epicatechin ((2R,3R)-3,3',4',5,7-Flavanpentaol) ist ein vorteilhafter Wirkstoff im Sinne der vorliegenden Erfindung.Catechins are a group of compounds which are to be regarded as hydrogenated flavones or anthocyanidins and derivatives of "catechins" (catechol, 3,3 ', 4', 5,7-flavanpentaol, 2- (3,4- Dihydroxyphenyl) -chroman-3,5,7-triol) Epicatechin ((2R, 3R) -3,3 ', 4', 5,7-flavanpentaol) is also an advantageous active substance in the sense of the present invention.
Vorteilhaft sind ferner pflanzliche Auszüge mit einem Gehalt an Catechinen, insbesondere Extrakte des grünen Tees, wie z. B. Extrakte aus Blättern der Pflanzen der Spezies Camellia spec, ganz besonders der Teesorten Camellia sinenis, C. .assamica, C. taliensis bzw. C. irrawadiensis und Kreuzungen aus diesen mit beispielsweise Camellia japonicaPlant extracts containing catechins, in particular extracts of green tea, such as. B. extracts from leaves of the plants of the species Camellia spec, especially the teas Camellia sinenis, C. .assamica, C. taliensis or C. irrawadiensis and crosses of these with, for example, Camellia japonica
Bevorzugte Wirkstoffe sind ferner Polyphenole bzw. Catechine aus der Gruppe (-)-Catechin, (+)-Catechin, (-)-Catechingallat, (-)-GaΙlocatechingallat, (+)-Epicatechin, (-)-Epicatechin, (-)- Epicatechin Gallat, (-)-Epigallocatechin, (-)-Epigallocatechingallat.Preferred active substances are also polyphenols or catechins from the group (-) - catechin, (+) - catechin, (-) - catechin gallate, (-) - GaΙlocatechin gallate, (+) - epicatechin, (-) - epicatechin, (-) - epicatechin gallate, (-) - epigallocatechin, (-) - epigallocatechin gallate.
Auch Flavon und seine Derivate (oft auch kollektiv „Flavone" genannt) sind vorteilhafte Wirkstoffe im Sinne der vorliegenden Erfindung. Sie sind durch folgende Grundstruktur gekennzeichnet (Substitutionspostitionen angegeben):Flavon and its derivatives (often also collectively called "flavones") are advantageous active substances in the sense of the present invention. They are characterized by the following basic structure (substitution positions specified):
Einige der wichtigeren Flavone, welche auch bevorzugt in erfindungsgemäßen Zubereitungen eingesetzt werden können, sind in der nachstehenden Tabelle 2 aufgeführt: Some of the more important flavones, which can also preferably be used in preparations according to the invention, are listed in Table 2 below:
In der Natur kommen Flavone in der Regel in glycosidierter Form vor.In nature, flavones usually occur in glycosidated form.
Erfindungsgemäß werden die Flavonoide bevorzugt gewählt gewählt aus der Gruppe der Substanzen der generischen StrukturformelAccording to the invention, the flavonoids are preferably chosen from the group of substances of the generic structural formula
wobei Z^ bis Z7 unabhängig voneinander gewählt werden aus der Gruppe H, OH, Alkoxy- sowie Hydroxyalkoxy-, wobei die Alkoxy- bzw. Hydroxyalkoxygruppen verzweigt und unverzweigt sein und 1 bis 18 C-Atome aufweisen können, und wobei Gly gewählt wird aus der Gruppe der Mono- und Oligoglycosidreste. Erfindungsgemäß können die Flavonoide aber auch vorteilhaft gewählt werden aus der Gruppe der Substanzen der generischen Strukturformel where Z ^ to Z 7 are independently selected from the group H, OH, alkoxy and hydroxyalkoxy, where the alkoxy or hydroxyalkoxy groups can be branched and unbranched and can have 1 to 18 carbon atoms, and wherein Gly is selected from the group of mono- and oligoglycoside residues. According to the invention, the flavonoids can also be advantageously selected from the group of substances of the generic structural formula
wobei Z\ bis Z6 unabhängig voneinander gewählt werden aus der Gruppe H, OH, Alkoxy- sowie Hydroxyalkoxy-, wobei die Alkoxy- bzw. Hydroxyalkoxygruppen verzweigt und unverzweigt sein und 1 bis 18 C-Atome aufweisen können, und wobei Gly gewählt wird aus der Gruppe der Mono- und Oligoglycosidreste. where Z \ to Z 6 are selected independently of one another from the group H, OH, alkoxy and hydroxyalkoxy, where the alkoxy or hydroxyalkoxy groups are branched and unbranched and can have 1 to 18 carbon atoms, and where Gly is selected from the group of mono- and oligoglycoside residues.
Bevorzugt können solche Strukturen gewählt werden aus der Gruppe der Substanzen der generischen StrukturformelSuch structures can preferably be selected from the group of substances of the generic structural formula
wobei Glyi, Gly2 und Gly3 unabhängig voneinander Monoglycosidreste oder darstellen. Gly2 bzw. Gly3 können auch einzeln oder gemeinsam AbSättigungen durch Wasserstoffatome darstellen. wherein Glyi, Gly 2 and Gly 3 independently of one another represent monoglycoside residues or. Gly 2 or Gly 3 can also represent, individually or together, saturations by hydrogen atoms.
Bevorzugt werden Glyi, Gly2 und Gly3 unabhängig voneinander gewählt aus der Gruppe der Hexosylreste, insbesondere der Rhamnosylreste und Glucosylreste. Aber auch andere He- xosylreste, beispielsweise Allosyl, Altrosyl, Galactosyl, Gulosyl, Idosyl, Mannosyl und Talosyl sind gegebenenfalls vorteilhaft zu verwenden. Es kann auch erfindungsgemäß vorteilhaft sein, Pentosylreste zu verwenden. Vorteilhaft werden Z^ bis Z5 unabhängig voneinander gewählt aus der Gruppe H, OH, Me- thoxy-, Ethoxy- sowie 2-Hydroxyethoxy-, und die Flavonglycoside haben die StrukturGlyi, Gly 2 and Gly 3 are preferably selected independently of one another from the group of the hexosyl radicals, in particular the rhamnosyl radicals and glucosyl radicals. However, other hexosyl residues, for example allosyl, altrosyl, galactosyl, gulosyl, idosyl, mannosyl and talosyl, can also be used advantageously if appropriate. It can also be advantageous according to the invention to use pentosyl residues. Z ^ to Z 5 are advantageously selected independently of one another from the group H, OH, methoxy, ethoxy and 2-hydroxyethoxy, and the flavone glycosides have the structure
Besonders vorteilhaft werden die erfindungsgemäßen Flavonglycoside aus der Gruppe, welche durch die folgende Struktur wiedergegeben werden:The flavone glycosides according to the invention from the group which are represented by the following structure are particularly advantageous:
wobei Glyi, Gly2 und Gly3 unabhängig voneinander Monoglycosidreste oder darstellen. Gly2 bzw. Gly3 können auch einzeln oder gemeinsam AbSättigungen durch Wasserstoffatome darstellen. wherein Glyi, Gly 2 and Gly 3 independently of one another represent monoglycoside residues or. Gly 2 or Gly 3 can also represent, individually or together, saturations by hydrogen atoms.
Bevorzugt werden Glyi, Gly2 und Gly3 unabhängig voneinander gewählt aus der Gruppe der Hexosylreste, insbesondere der Rhamnosylreste und Glucosylreste. Aber auch andere He- xosylreste, beispielsweise Allosyl, Altrosyl, Galactosyl, Gulosyl, Idosyl, Mannosyl und Talosyl sind gegebenenfalls vorteilhaft zu verwenden. Es kann auch erfindungsgemäß vorteilhaft sein, Pentosylreste zu verwenden. Besonders vorteilhaft im Sinne der vorliegenden Erfindung ist, das oder die Flavonglycoside zu wählen aus der Gruppe α-Glucosylrutin, α-Glucosylmyricetin, α-Glucosylisoquercitrin, α- Glucosylisoquercetin und α-Glucosylquercitrin.Glyi, Gly 2 and Gly 3 are preferably selected independently of one another from the group of the hexosyl radicals, in particular the rhamnosyl radicals and glucosyl radicals. However, other hexosyl residues, for example allosyl, altrosyl, galactosyl, gulosyl, idosyl, mannosyl and talosyl, can also be used advantageously if appropriate. It can also be advantageous according to the invention to use pentosyl residues. For the purposes of the present invention, it is particularly advantageous to select the flavone glycoside (s) from the group α-glucosyl rutin, α-glucosyl myrcetin, α-glucosyl isoquercitrin, α-glucosyl iso quercetin and α-glucosyl quercitrin.
Erfindungsgemäß besonders bevorzugt ist α-Glucosylrutin.According to the invention, α-glucosylrutin is particularly preferred.
Erfindungsgemäß vorteilhaft sind auch Naringin (Aurantiin, Naringenin-7-rhamnoglucosid), Hesperidin (3',5,7-Trihydroxy-4'-methoxyflavanon-7-rutinosid, Hesperidosid, Hesperetin-7-O- rutinosid). Rutin (3,3',4',5,7-Pentahydroxyflyvon-3-rutinosid, Quercetin-3-rutinosid, Sophorin, Birutan, Rutabion, Taurutin, Phytomelin, Melin), Troxerutin (3,5-Dihydroxy-3',4',7-tris(2- hydroxyethoxy)-flavon-3-(6-O-(6-deoxy-α-L-mannopyranosyl)-ß-D-glucopyranosid)), Monoxe- rutin (3,3',4',5-Tetrahydroxy-7-(2-hydroxyethoxy)-flavon-3-(6-O-(6-deoxy-α-L-mannopyrano- syl)-ß-D-glucopyranosid)), Dihydrorobinetin (3,3',4',5',7-Pentahydroxyflavanon), Taxifolin (3,3',4',5,7-Pentahydroxyflavanon), Eriodictyol-7-glucosid (3',4',5,7-Tetrahydroxyflavanon-7- glucosid), Flavanomareϊn (3',4',7,8-Tetrahydroxyflavanon-7-glucosid) und Isoquercetin (3,3',4',5,7-Pentahydroxyflavanon-3-(ß-D-Glucopyranosid).Naringin (aurantiin, naringenin-7-rhamnoglucoside), hesperidin (3 ', 5,7-trihydroxy-4'-methoxyflavanon-7-rutinoside, hesperidoside, hesperetin-7-o-rutinoside) are also advantageous according to the invention. Rutin (3,3 ', 4', 5,7-pentahydroxyflyvon-3-rutinosid, quercetin-3-rutinosid, sophorin, birutan, rutabion, taurutin, phytomelin, melin), troxerutin (3,5-dihydroxy-3 ', 4 ', 7-tris (2-hydroxyethoxy) flavone-3- (6-O- (6-deoxy-α-L-mannopyranosyl) -ß-D-glucopyranoside)), monoxurutin (3,3', 4 ', 5-tetrahydroxy-7- (2-hydroxyethoxy) flavon-3- (6-O- (6-deoxy-α-L-mannopyrano-syl) -ß-D-glucopyranoside)), dihydrorobinetin (3, 3 ', 4', 5 ', 7-pentahydroxyflavanone), taxifolin (3,3', 4 ', 5,7-pentahydroxyflavanone), eriodictyol-7-glucoside (3', 4 ', 5,7-tetrahydroxyflavanone-7 - Glucoside), Flavanomareϊn (3 ', 4', 7,8-tetrahydroxyflavanon-7-glucoside) and Isoquercetin (3,3 ', 4', 5,7-pentahydroxyflavanon-3- (ß-D-glucopyranoside).
Vorteilhaft ist es auch, dem oder die Wirkstoffe aus der Gruppe der Ubichinone und Plasto- chinone zu wählen.It is also advantageous to choose the active ingredient (s) from the group of ubiquinones and plastoquinones.
Ubichinone zeichnen sich durch die StrukturformelUbiquinones are characterized by the structural formula
aus und stellen die am weitesten verbreiteten und damit am besten untersuchten Biochinone dar. Ubichinone werden je nach Zahl der in der Seitenkette verknüpften Isopren-Einheiten als Q-1, Q-2, Q-3 usw. oder nach Anzahl der C-Atome als U-5, U-10, U-15 usw. bezeichnet. Sie treten bevorzugt mit bestimmten Kettenlängen auf, z. B. in einigen Mikroorganismen und Hefen mit n=6. Bei den meisten Säugetieren einschließlich des Menschen überwiegt Q10. Besonders vorteilhaft ist Coenzym Q10, welches durch folgende Strukturformel gekennzeichnet ist:and represent the most widespread and thus the best studied bioquinones. Depending on the number of isoprene units linked in the side chain, ubiquinones are called as Q-1, Q-2, Q-3 etc. or according to the number of C atoms as U-5, U-10, U-15 and so on. They preferably occur with certain chain lengths, e.g. B. in some microorganisms and yeasts with n = 6. Q10 predominates in most mammals, including humans. Coenzyme Q10, which is characterized by the following structural formula, is particularly advantageous:
Plastochinone weisen die allgemeine StrukturformelPlastoquinones have the general structural formula
auf. Plastoschinone unterscheiden sich in der Anzahl n der Isopren-Reste und werden endsprechend bezeichnet, z. B. PQ-9 (n=9). Ferner existieren andere Plastochinone mit unterschiedlichen Substituenten am Chinon-Ring. on. Plastoquinones differ in the number n of isoprene residues and are named accordingly, e.g. B. PQ-9 (n = 9). There are also other plastoquinones with different substituents on the quinone ring.
Auch Kreatin und/oder Kreatinderivate sind bevorzugte Wirkstoffe im Sinne der vorliegenden Erfindung. Kreatin zeichnet sich durch folgende Struktur aus:Creatine and / or creatine derivatives are also preferred active substances for the purposes of the present invention. Creatine is characterized by the following structure:
Bevorzugte Derivate sind Kreatinphosphat sowie Kreatinsulfat, Kreatinacetat, Kreatin- ascorbat und die an der Carboxylgruppe mit mono- oder polyfunktionalen Alkoholen ver- esterten Derivate.Preferred derivatives are creatine phosphate and creatine sulfate, creatine acetate, creatine ascorbate and the derivatives esterified on the carboxyl group with mono- or polyfunctional alcohols.
Ein weiterer vorteilhafter Wirkstoff ist L-Camitin [3-Hydroxy-4-(trimethylammonio)-butter- säurebetain]. Auch Acyl-Carnitine, welche gewählt aus der Gruppe der Substanzen der folgenden allgemeinen Strukturformel %Another advantageous active ingredient is L-camitin [3-hydroxy-4- (trimethylammonio) -butter-acid-betaine]. Also acyl-carnitine, which is selected from the group of substances of the following general structural formula %
+ I+ I
(H3C)3N— CH2— C— CH2— COO-(H 3 C) 3 N - CH 2 - C - CH 2 - COO-
H wobei R gewählt wird aus der Gruppe der verzweigten und unverzweigten Alkylreste mit bis zu 10 Kohlenstoffatomen sind vorteilhafte Wirkstoffe im Sinne der vorliegenden Erfindung. Bevorzugt sind Propionylcarnitin und insbesondere Acetylcamitin. Beide Entantiomere (D- und L-Form) sind vorteilhaft im Sinne der vorliegenden Erfindung zu verwenden. Es kann auch von Vorteil sein, beliebige Enantiomerengemische, beispielsweise ein Racemat aus D- und L-Form, zu verwenden.H where R is selected from the group of branched and unbranched alkyl radicals having up to 10 carbon atoms are advantageous active substances in the sense of the present invention. Propionylcarnitine and in particular acetylcamitine are preferred. Both entantiomers (D- and L-form) can be used advantageously for the purposes of the present invention. It can also be advantageous to use any mixture of enantiomers, for example a racemate of D and L form.
Weitere vorteilhafte Wirkstoffe sind Sericosid, Pyridoxol, Vitamin K, Biotin und Aromastoffe.Other advantageous active ingredients are sericoside, pyridoxol, vitamin K, biotin and flavorings.
Die Liste der genannten Wirkstoffe bzw. Wirkstoffkombinationen, die in den erfindungsgemäßen Zubereitungen verwendet werden können, soll selbstverständlich nicht limitierend sein. Die Wirkstoffe können einzelnen oder in beliebigen Kombinationen miteinander verwendet werden.The list of the active substances or combinations of active substances mentioned which can be used in the preparations according to the invention is of course not intended to be limiting. The active ingredients can be used individually or in any combination with one another.
Die Menge solcher Wirkstoffe (eine oder mehrere Verbindungen) in den Zubereitungen gemäß der Erfindung beträgt vorzugsweise 0,001 bis 30 Gew.-%, besonders bevorzugt 0,05 - 20 Gew.-%, insbesondere 1 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitung.The amount of such active substances (one or more compounds) in the preparations according to the invention is preferably 0.001 to 30% by weight, particularly preferably 0.05-20% by weight, in particular 1-10% by weight, based on the Total weight of the preparation.
Die Herstellung erfindungsgemäßer Zubereitungen erfolgt unter den dem Fachmanne geläufigen Bedingungen. Es werden in der Regel die Bestandteile der Ölphase bzw. der Wasserphase gesondert zusammengegeben und erwärmt, und sodann unter Rühren und, besonders vorteilhaft, unter Homogenisieren, ganz besonders vorteilhaft unter Rühren mit mittlerem bis hohen Energieeintrag, vorteilhaft mit Hilfe einer Zahnkranzdispergiermaschine mit einer Umdrehungszahl bis maximal 10000 U/min, vorzugsweise von 2500 bis 7700 U/min, miteinander vereinigt.Preparations according to the invention are produced under the conditions familiar to the person skilled in the art. As a rule, the components of the oil phase or the water phase are combined separately and heated, and then with stirring and, particularly advantageously, with homogenization, very particularly advantageously with stirring with medium to high energy input, advantageously with the aid of a gear rim dispersion machine with a speed of up to a maximum of 10,000 rpm, preferably from 2500 to 7700 rpm, combined with one another.
Die nachfolgenden Beispiele sollen die vorliegende Erfindung verdeutlichen. Beispiel 1 (O/W-Creme):The following examples are intended to illustrate the present invention. Example 1 (O / W cream):
Gew.-%Wt .-%
Stearinsäure 2,00Stearic acid 2.00
Lignocerinsäure 1 ,00Lignoceric acid 1.00
Cetylalkohol 5,00Cetyl alcohol 5.00
PEG-20 Stearat 1 ,00PEG-20 stearate 1, 00
Sorbitanstearat 1,00Sorbitan stearate 1.00
Caprylsäure-/Caprinsäuretriglyceride 3,00Caprylic acid / capric acid triglycerides 3.00
Glycerylstearat 1,00Glyceryl stearate 1.00
Octyldodecanol 6,00Octyldodecanol 6.00
Isopropylpalmitate 1 ,00Isopropyl palmitate 1, 00
Octylstearate 1,00Octyl stearate 1.00
Cyclomethicone 3,00Cyclomethicone 3.00
Myristylmyristat 3,00Myristyl myristate 3.00
Glycerin 3,00Glycerin 3.00
Carbomer 0,10Carbomer 0.10
Ceramide III 0,50Ceramide III 0.50
Natriumhydroxid q.s.Sodium hydroxide q.s.
Konservierung q.s.Conservation q.s.
Parfüm q.s.Perfume q.s.
Wasser.demineralisiert ad 100,00 pH-Wert eingestellt auf 5.0-6,5Water demineralized ad 100.00 pH adjusted to 5.0-6.5
Die Bestandteile der Ölphase bzw. der Wasserphase werden gesondert zusammengegeben und erwärmt, und sodann unter Homogenisieren, mit Hilfe einer Zahnkranzdispergiermaschine mit einer Umdrehungszahl von 5000 U/min miteinander vereinigt. The constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization, with the aid of a gear rim dispersing machine at a speed of 5000 rpm.
Beispiel 2 (O/W-Lotion):Example 2 (O / W lotion):
Gew.-%Wt .-%
Cholesterol 2,50Cholesterol 2.50
Lanosterol 0,50Lanosterol 0.50
Lanolin 0,50Lanolin 0.50
Myristylalcohol 1 ,00Myristyl alcohol 1, 00
Cetylstearylalcohol 2,00Cetylstearyl alcohol 2.00
PEG-100 Stearat 1,00PEG-100 stearate 1.00
Sorbitanstearat 1,00Sorbitan stearate 1.00
Glycerylstearat 1 ,00Glyceryl stearate 1, 00
Propylenglycoldicaprylat/dicaprat 3,00Propylene glycol dicaprylate / dicaprate 3.00
Octylpalmitat 5,00Octyl palmitate 5.00
Hydriertes Polyisobuten 2,00Hydrogenated polyisobutene 2.00
Glycerin 3,00Glycerin 3.00
Carbomer 0,15Carbomer 0.15
Alpha-Glucosylrutin 0,50Alpha-glucosylrutin 0.50
Retinol 0,20Retinol 0.20
Kaliumhydroxid q.s.Potassium hydroxide q.s.
Konservierung q.s.Conservation q.s.
Parfüm q.s.Perfume q.s.
Wasser.demineralisiert ad 100,00 pH-Wert eingestellt auf 5,0Water demineralized from 100.00 pH adjusted to 5.0
Die Bestandteile der Ölphase bzw. der Wasserphase werden gesondert zusammengegeben und erwärmt, und sodann unter Homogenisieren mit einer Zahnkranzdispergiermaschine mit einer Umdrehungszahl von 7000 U/min miteinander vereinigt. The constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 7000 rpm.
Beispiel 3 (O/W-Lotion):Example 3 (O / W lotion):
Gew.-%Wt .-%
Stearinsäure 3,00Stearic acid 3.00
Myristylalcohol 1 ,00Myristyl alcohol 1, 00
Cetylstearylalcohol 1,00Cetylstearylalcohol 1.00
PEG-100 Stearat 1,00PEG-100 stearate 1.00
Sorbitanstearat 1,00Sorbitan stearate 1.00
Glycerylstearat 1,00Glyceryl stearate 1.00
Propylenglycoldicaprylat/dicaprat 3,00Propylene glycol dicaprylate / dicaprate 3.00
Paraffinöl 5,00Paraffin oil 5.00
Glycerin 3,00Glycerin 3.00
Carbomer 0,15Carbomer 0.15
Alpha-Glucosylrutin 0,50Alpha-glucosylrutin 0.50
Retinol 0,20Retinol 0.20
Kaliumhydroxid q.s.Potassium hydroxide q.s.
Konservierung q.s.Conservation q.s.
Parfüm q.s.Perfume q.s.
Wasser, demineralisiert ad 100,00 pH-Wert eingestellt auf 5,0Water, demineralized ad 100.00 pH adjusted to 5.0
Die Bestandteile der Ölphase bzw. der Wasserphase werden gesondert zusammengegeben und erwärmt, und sodann unter Homogenisieren mit einer Zahnkranzdispergiermaschine mit einer Umdrehungszahl von 3200 U/min miteinander vereinigt. The constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 3200 rpm.
Beispiel 4 (O/W-Creme):Example 4 (O / W cream):
Gew.-%Wt .-%
PEG-40 Stearat 0,50PEG-40 stearate 0.50
Stearinsäure 3,00Stearic acid 3.00
Cholesterol 1 ,00Cholesterol 1.00
Cetylstearylalkohol 4,00Cetylstearyl alcohol 4.00
Glycerylstearat 1 ,00Glyceryl stearate 1, 00
Sorbitanstearat 0,50Sorbitan stearate 0.50
Caprylsäure-/Caprinsäuretriglyceride 3,00Caprylic acid / capric acid triglycerides 3.00
Dimethicone 4,00Dimethicone 4.00
Dicaprylylether 2,00Dicaprylyl ether 2.00
Hydrierte Kokosfettsäureglyceride 5,00Hydrogenated coconut fatty acid glycerides 5.00
Ceramide II 0,07Ceramide II 0.07
Xanthangummi 0,10Xanthan gum 0.10
Citronensäure 0,10Citric acid 0.10
Glycerin 3,00 Parfüm, Konservierungsmittel,Glycerin 3.00 perfume, preservative,
Farbstoffe usw. q.s.Dyes etc. q.s.
Wasser ad 100,00 pH-Wert eingestellt auf 5.0-7.0Water ad 100.00 pH set to 5.0-7.0
Die Bestandteile der Ölphase bzw. der Wasserphase werden gesondert zusammengegeben und erwärmt, und sodann unter Homogenisieren mit einer Zahnkranzdispergiermaschine mit einer Umdrehungszahl von 5000 U/min miteinander vereinigt. The components of the oil phase or the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 5000 rpm.
Beispiel 5 (O/W-Emulsions-Make-up):Example 5 (O / W emulsion make-up):
Gew.-%Wt .-%
PEG-40 Stearat 1 ,00PEG-40 stearate 1, 00
Stearinsäure 3,00Stearic acid 3.00
Lanolin 0,50Lanolin 0.50
Cholesterol 0,25Cholesterol 0.25
Lignocerinsäure 0,25Lignoceric acid 0.25
Cetylalkohol 2,00Cetyl alcohol 2.00
Glycerylstearat 1 ,00Glyceryl stearate 1, 00
Sorbitanstearat 1 ,00Sorbitan stearate 1, 00
Caprylsäure-/Caprinsäuretriglyceride 3,00Caprylic acid / capric acid triglycerides 3.00
Cetylstearylisononanoate 2,00Cetylstearylisononanoate 2.00
Hexyldecanol 5,00Hexyl decanol 5.00
Glycerin 3,00Glycerin 3.00
Carbomer 0,15Carbomer 0.15
Glimmer 1 ,00Mica 1, 00
Magnesiumsilikat 1 ,00Magnesium silicate 1.00
Eisenoxide 1 ,00Iron oxides 1, 00
Titandioxid 2,50Titanium dioxide 2.50
Talkum 5,00Talc 5.00
Retinol 0,20Retinol 0.20
Natriumhydroxid q.s.Sodium hydroxide q.s.
Konservierung q.s.Conservation q.s.
Parfüm q.s.Perfume q.s.
Wasser, demineralisiert ad 100,00 pH-Wert eingestellt auf 6.5Water, demineralized to 100.00 pH adjusted to 6.5
Die Bestandteile der Ölphase bzw. der Wasserphase werden gesondert zusammengegeben und erwärmt, und sodann unter Homogenisieren mit einer Zahnkranzdispergiermaschine mit einer Umdrehungszahl von 6000 U/min miteinander vereinigt. Beispiel 6 (O/W-Creme):The constituents of the oil phase or the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 6000 rpm. Example 6 (O / W cream):
Gew.-%Wt .-%
PEG-100 Stearat 1,00PEG-100 stearate 1.00
Lignocerinsäure 1,00Lignoceric acid 1.00
Cholesterol 1,00Cholesterol 1.00
Lanolin 1,00Lanolin 1.00
Cetylalkohol 4,00Cetyl alcohol 4.00
Sorbitanstearat 1,00Sorbitan stearate 1.00
Glyceryldistearat 1,00Glyceryl distearate 1.00
Octyldodecylmyristat 3,00Octyldodecyl myristate 3.00
Octyldodecanol 3,00Octyldodecanol 3.00
Paraffinöl 2,00Paraffin oil 2.00
Butyleneglycolcaprylat/caprat 2,00Butylene glycol caprylate / caprate 2.00
Dimethicone 2,00Dimethicone 2.00
Cyclomethicone 1,00Cyclomethicone 1.00
Ceramide 0,50Ceramides 0.50
Vitamin E Acetate 1,00Vitamin E Acetate 1.00
Xanthangummi 0,10Xanthan gum 0.10
Glycerin 3,00Glycerin 3.00
BHT 0,02BHT 0.02
Disodium EDTA 0,10Disodium EDTA 0.10
Parfüm, Konservierungsmittel,Perfume, preservative,
Farbstoffe q.s.Dyes q.s.
Wasser ad 100,00 pH-Wert eingestellt auf 5,0-6,5Water ad 100.00 pH adjusted to 5.0-6.5
Die Bestandteile der Ölphase bzw. der Wasserphase werden gesondert zusammengegeben und erwärmt, und sodann unter Homogenisieren mit einer Zahnkranzdispergiermaschine mit einer Umdrehungszahl von 2800 U/min miteinander vereinigt. Beispiel 7 (O/W-Lotion):The constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 2800 rpm. Example 7 (O / W lotion):
Gew.-%Wt .-%
PEG-100 Stearate 0,50PEG-100 stearate 0.50
Stearinsäure 2,00Stearic acid 2.00
Cetylalkohol 2,00Cetyl alcohol 2.00
Sorbitan Stearate 0,50Sorbitan stearate 0.50
Glyceryl Stearate 0,50Glyceryl stearate 0.50
2-ι5Alkylbenzoate 4,002- ι 5 alkyl benzoates 4.00
Caprylsäure-/Caprinsäuretriglycerid 3,00Caprylic acid / capric acid triglyceride 3.00
Paraffinöl 2,00Paraffin oil 2.00
Tocopherylacetat 2,00Tocopheryl acetate 2.00
Natriumcarbomer 0,10Sodium carbomer 0.10
Ceramide III 0,50Ceramide III 0.50
Glycerin 3,00Glycerin 3.00
Parfüm, Konservierungsmittel,Perfume, preservative,
Farbstoffe usw. q.s.Dyes etc. q.s.
Wasser ad 100,00 pH-Wert eingestellt auf 5,0-7,0Water ad 100.00 pH adjusted to 5.0-7.0
Die Bestandteile der Ölphase bzw. der Wasserphase werden gesondert zusammengegeben und erwärmt, und sodann unter Homogenisieren mit einer Zahnkranzdispergiermaschine mit einer Umdrehungszahl von 3000 U/min miteinander vereinigt. The constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 3000 rpm.
Beispiel 8 (O/W-Creme)Example 8 (O / W cream)
Gew.-%Wt .-%
PEG-100 Stearate 0,50PEG-100 stearate 0.50
Stearinsäure 3,00Stearic acid 3.00
Cetylalkohol 5,00Cetyl alcohol 5.00
Sorbitan Stearate 0,50Sorbitan stearate 0.50
Glyceryl Stearate 0,50Glyceryl stearate 0.50
Dimethicone 1 ,00Dimethicone 1, 00
Paraffinöl 3,00Paraffin oil 3.00
Myristyl Myristat 2,00Myristyl myristate 2.00
Hydrierte Kokosfettsäureglyceride 4,00Hydrogenated coconut fatty acid glycerides 4.00
Tocopherylacetat 2,00Tocopheryl acetate 2.00
Natriumcarbomer 0,10Sodium carbomer 0.10
Ceramide III 0,50Ceramide III 0.50
Glycerin 3,00Glycerin 3.00
Parfüm, Konservierungsmittel,Perfume, preservative,
Farbstoffe usw. q.s.Dyes etc. q.s.
Wasser ad 100,00 pH-Wert eingestellt auf 5,0-7,0Water ad 100.00 pH adjusted to 5.0-7.0
Die Bestandteile der Ölphase bzw. der Wasserphase werden gesondert zusammengegeben und erwärmt, und sodann unter Homogenisieren mit einer Zahnkranzdispergiermaschine mit einer Umdrehungszahl von 5200 U/min miteinander vereinigt. The constituents of the oil phase and the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 5,200 rpm.
Beispiel 9 (Sonnenschutz-Creme):Example 9 (sun protection cream):
Gew.-%Wt .-%
PEG-100 Stearat 1 ,00PEG-100 stearate 1, 00
Stearinsäure 2,00Stearic acid 2.00
Cholesterol 1,00Cholesterol 1.00
Lignocerinsäure 1,00Lignoceric acid 1.00
Cetylalkohol 4,00Cetyl alcohol 4.00
Sorbitanstearat 1 ,00Sorbitan stearate 1, 00
Glycerylstearat 1 ,50Glyceryl stearate 1, 50
Octyldodecanol 2,00Octyldodecanol 2.00
Paraffinöl 6,00Paraffin oil 6.00
Butyloctanol 1,00Butyl octanol 1.00
Xanthangummi 0,10Xanthan gum 0.10
Natriumcarbomer 0,10Sodium carbomer 0.10
Glycerin 3,00Glycerin 3.00
Ceramide III 0,20Ceramide III 0.20
BHT 0,02BHT 0.02
Na2H2EDTA 0,10Na 2 H 2 EDTA 0.10
Parfüm, Konservierungsmittel,Perfume, preservative,
Farbstoffe, usw. q.s.Dyes, etc. q.s.
Wasser ad 100,00 pH-Wert eingestellt auf 5,0-5.5Water ad 100.00 pH adjusted to 5.0-5.5
Die Bestandteile der ölphase bzw. der Wasserphase werden gesondert zusammengegeben und erwärmt, und sodann unter Homogenisieren mit einer Zahnkranzdispergiermaschine mit einer Umdrehungszahl von 3500 U/min miteinander vereinigt. The components of the oil phase or the water phase are combined separately and heated, and then combined with one another with homogenization using a gear rim dispersing machine at a speed of 3500 rpm.

Claims

Patentansprüche: claims:
1. Kosmetische oder dermatologische Zubereitungen in Form einer O/W-Emulsion enthaltend1. Containing cosmetic or dermatological preparations in the form of an O / W emulsion
(I) 1 bis zu 5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, einer oder mehrerer Substanzen, gewählt aus der Gruppe der Sterine, verzweigten o- der unverzweigten, gesättigten oder ungesättigten Cι2-C40-Fettsäuren,(I) 1 to 5% by weight, based on the total weight of the preparations, of one or more substances selected from the group of sterols, branched or unbranched, saturated or unsaturated C 2 -C 40 fatty acids,
(II) 0,1 bis zu 1 ,5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, eines oder mehrerer Mono-, Sesqui-, Di-, Triestem von gesättigten oder ungesättigten, geradkettigten oder verzweigtkettigen Fettsäuren mit einer Kettenlänge von Cι4 - C 0 des Glycerols und/oder des Propylenglycols und/oder des Glykols.(II) 0.1 to 1.5% by weight, based on the total weight of the preparations, of one or more mono-, sesqui-, di-, trieste of saturated or unsaturated, straight-chain or branched-chain fatty acids with a chain length of Cι 4 - C 0 of the glycerol and / or the propylene glycol and / or the glycol.
(III) 0,1 bis zu 1 ,5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitung eines o- der mehrerer Mono-, Sesqui-, Di-, Triester von gesättigten oder ungesättigten, geradkettigten oder verzweigtkettigen Fettsäuren mit einer Kettenlänge von Cι4 - C 0 des Sorbitans und optional mit einem Polyethoxylierungsgrad von 0-100.(III) 0.1 to 1.5% by weight, based on the total weight of the preparation of one or more mono-, sesqui-, di-, triesters of saturated or unsaturated, straight-chain or branched-chain fatty acids with a chain length of Cι 4 - C 0 of sorbitan and optionally with a degree of polyethoxylation of 0-100.
(IV) 0,1 bis zu 1 ,5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, eines oder mehrerer ethoxylierter Fettsäureester, mit Fettsäuren der Kettenlänge Cι2 - C 0 und einem Ethoxylierungsgrad bis zu 100, bevorzugt von 5 - 100,(IV) 0.1 to 1.5% by weight, based on the total weight of the preparations, of one or more ethoxylated fatty acid esters, with fatty acids of chain length C 2 -C 0 and a degree of ethoxylation of up to 100, preferably from 5 to 100 .
(V) 0,5 - 7 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, einer oder mehrere Fettalkohole, gewählt aus der Gruppe der verzweigten und unverzweigten, gesättigten und ungesättigten Alkylalkohole mit 12 bis 40 Kohlenstoffatomen(V) 0.5 - 7 wt .-%, based on the total weight of the preparations, one or more fatty alcohols selected from the group of branched and unbranched, saturated and unsaturated alkyl alcohols having 12 to 40 carbon atoms
(VI) wobei das Verhältnis aus (II): (III) : (IV) vorzugsweise gewählt wie a : b : c wird, wobei a, b und c unabhängig voneinander rationale Zahlen von 1 bis 5, bevorzugt von 1 bis 3 darstellen.(VI) where the ratio of (II): (III): (IV) is preferably chosen as a: b: c, where a, b and c independently of one another represent rational numbers from 1 to 5, preferably from 1 to 3.
(VII) sowie das Verhältnis aus (ll)+(lll)+(IV) zu (V) vorzugsweise im Bereich 5:1 bis 1 :5 liegt,(VII) and the ratio of (II) + (III) + (IV) to (V) is preferably in the range 5: 1 to 1: 5,
(VIII) wobei die Summe aus (I), (II), (III), (IV) und (V) maximal 25 Gew.-% beträgt,(VIII) the sum of (I), (II), (III), (IV) and (V) being at most 25% by weight,
(IX) und wobei die Zubereitungen vorteilhaft in einem pH-Bereich von 3,5 - 8,0, vorzugsweise bei pH-Werten von 4,5 -6,5, vorliegen.(IX) and wherein the preparations are advantageously present in a pH range from 3.5 to 8.0, preferably at pH values from 4.5 to 6.5.
2. Zubereitungen nach Anspruch 1 , enthaltend2. Preparations according to claim 1, containing
(II) 0,1 bis zu 1 ,5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, einer oder mehrerer Glycol- bzw. Glycerylester gewählt aus der Gruppe der Mono-, Sesqui- Di- und Triester der Glycole (= vic-Diole bzw. 1,2-Diole) bzw. des Glycerols (1,2,3- Trihydroxypropane) mit Fettsäuren der Kettenlänge Cι2 - C 40 (geradzahlig, gesättigt, ungesättigt und verzweigt).(II) 0.1 to 1.5% by weight, based on the total weight of the preparations, of one or more glycol or glyceryl esters selected from the group of the mono-, sesqui-di- and triesters of the glycols (= vic -Diols or 1,2-diols) or glycerol (1,2,3- Trihydroxypropane) with fatty acids of chain length Cι 2 - C 40 (even, saturated, unsaturated and branched).
3. Zubereitungen nach Anspruch 1 , enthaltend3. Preparations according to claim 1, containing
(IV) 0,1 bis zu 1 ,5 Gew.-% eines oder mehrere Sorbitanester, gewählt aus der Gruppe der Mono-, Sesqui-, Di und Triester der Sorbitane (= Monoanhydrosorbite bzw. 1 ,5- Anhydro-D-Sorbit) mit Fettsäuren der Kettenlänge Cι2 - C 40 (geradzahlig, gesättigt, ungesättigt und verzweigt) sowie optional einem Ethoxylierungsgrad von 10 - 100).(IV) 0.1 up to 1.5% by weight of one or more sorbitan esters, selected from the group of the mono-, sesqui-, di and triesters of sorbitans (= monoanhydrosorbites or 1,5-anhydro-D-sorbitol ) with fatty acids of chain length Cι 2 - C 40 (even, saturated, unsaturated and branched) and optionally a degree of ethoxylation of 10 - 100).
4. Zubereitungen nach Anspruch 1 , enthaltend4. Preparations according to claim 1, containing
(V) 0,1 bis zu 1 ,5 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, eines oder mehrerer ethoxylierter Fettsäureester, mit Fettsäuren der Kettenlänge C12 - C 40 und einem Ethoxylierungsgrad von 5 - 100, gewählt aus der Gruppe PEG-20-Stearat, PEG-30 Stearat PEG-40-Stearat, PEG-100 Stearat(V) 0.1 to 1.5% by weight, based on the total weight of the preparations, of one or more ethoxylated fatty acid esters, with fatty acids of chain length C 12 -C 40 and a degree of ethoxylation of 5-100, selected from the group PEG-20 stearate, PEG-30 stearate PEG-40 stearate, PEG-100 stearate
5. Zubereitungen nach Anspruch 1 , enthaltend5. Preparations according to claim 1, containing
(V) 0,5 - 7 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, einer oder mehrere verzweigter oder unverzweigter, gesättigter oder ungesättigter Fettalkohole, gewählt aus der Gruppe Myristylalkohol, Cetylalkohol, Isocetylalkohol, Cetylstearylalkohol, Stearylalkohol, Isostearylalkohol, Behenylalkohol und Mischungen daraus.(V) 0.5 - 7 wt .-%, based on the total weight of the preparations, one or more branched or unbranched, saturated or unsaturated fatty alcohols, selected from the group myristyl alcohol, cetyl alcohol, isocetyl alcohol, cetylstearyl alcohol, stearyl alcohol, isostearyl alcohol, behenyl alcohol and Mixtures of these.
6. Zubereitungen nach Anspruch 1,6. Preparations according to claim 1,
(VI) wobei die aus der Gruppe der verzweigten und unverzweigten, gesättigten und ungesättigten Alkylalkohole mit 12 bis 40 Kohlenstoffatomen aus der Gruppe der Wollwachsalkohole gewählt werden,(VI) where those from the group of branched and unbranched, saturated and unsaturated alkyl alcohols having 12 to 40 carbon atoms are selected from the group of wool wax alcohols,
(II) die neben den aliphatischen Alkoholen auch ein oder mehrere Sterine enthalten können.(II) which can also contain one or more sterols in addition to the aliphatic alcohols.
7. Zubereitungen nach Anspruch 1, enthaltend mindestens 2% flüssige Lipide vorzugsweise ausgewählt aus (a) Guerbetalkoholen, (b) gesättigten Triglyceriden, (c) Ethern mittelkettiger Fettalkohole, (d) unpolaren Lipiden, (e) Silikonölen, (f) Dialkylcarbonaten oder Abmischungen daraus. 7. Preparations according to claim 1, containing at least 2% liquid lipids, preferably selected from (a) Guerbet alcohols, (b) saturated triglycerides, (c) ethers of medium-chain fatty alcohols, (d) non-polar lipids, (e) silicone oils, (f) dialkyl carbonates or Mixtures from it.
EP02762429A 2001-08-10 2002-08-06 Cosmetic and dermatological preparations in the form of o/w emulsions containing sterols and/or c12-c40 fatty acids Withdrawn EP1418884A2 (en)

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DE10139580 2001-08-10
DE10139580A DE10139580A1 (en) 2001-08-10 2001-08-10 O/W emulsions useful e.g. cleansing, skin-care or anti-acne agents comprise a combination of steroids or fatty acids with optionally ethoxylated esters
PCT/EP2002/008743 WO2003013460A2 (en) 2001-08-10 2002-08-06 Cosmetic and dermatological preparations in the form of o/w emulsions containing sterols and/or c12-c40 fatty acids

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EP1418884A2 true EP1418884A2 (en) 2004-05-19

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