EP1244416A2 - Preparations cosmetiques ou dermatologiques du type huile dans l'eau - Google Patents

Preparations cosmetiques ou dermatologiques du type huile dans l'eau

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Publication number
EP1244416A2
EP1244416A2 EP00987407A EP00987407A EP1244416A2 EP 1244416 A2 EP1244416 A2 EP 1244416A2 EP 00987407 A EP00987407 A EP 00987407A EP 00987407 A EP00987407 A EP 00987407A EP 1244416 A2 EP1244416 A2 EP 1244416A2
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EP
European Patent Office
Prior art keywords
density
oil
cosmetic
acid
phase
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
EP00987407A
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German (de)
English (en)
Inventor
Anja MÜLLER
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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Filing date
Publication date
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Publication of EP1244416A2 publication Critical patent/EP1244416A2/fr
Withdrawn legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/06—Emulsions
    • A61K8/062—Oil-in-water emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/06—Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier 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
    • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations

Definitions

  • the present invention relates to cosmetic and dermatological preparations of the oil-m-water type, in particular free-flowing O / emulsions, very particularly sprayable O / W emulsions which have a viscosity of less than 2000 mPa s, and a method for stabilization O / W formulations using density adjustment of the phases
  • Cosmetic preparations are mainly used to care for the skin.
  • Human skin as the largest human organ, performs numerous vital functions. With an average surface area of around 2 m 2 in adults, it has an outstanding role as a protective and sensory organ. Among its many functions (The barrier function, which prevents the skin (and ultimately the entire organism) from drying out, is the most important factor.
  • the skin acts as a protective device against the penetration and absorption of external substances (e.g. dirt, chemicals, microorganisms) ) It also has an important role as a regulatory and target organ in human metabolism
  • Cosmetic skin care primarily serves to strengthen or restore the natural function of the skin as a barrier against environmental influences and against the loss of the body's own substances (in addition to water also natural fats, electrolytes etc.)
  • 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 particularly important when the natural regeneration capacity is not sufficient Protect environmental influences, especially from the sun and wind, and delay skin aging
  • UV-C radiation with a wavelength that is less than 290 nm is known from the Ozone layer absorbs in the earth's atmosphere and has no physiological significance.
  • UV-B range causes erythema, simple sunburn or even more or less severe burns of UV-A radiation (320 up to 400 nm) is far more dangerous than UV-B radiation with regard to the triggering of photodynamic, especially phototoxic reactions and chronic changes in the skin.
  • UV-A radiation is sufficient under normal everyday conditions to collagen within a short time - and elastin fibers can also be damaged by the damaging influence of UV-B radiation
  • UV-A radiation can be intensified
  • Medical topical compositions usually contain one or more drugs in effective concentration.
  • cosmetic and medical use e.g. cosmetics regulation, food and drug law.
  • Emulsions are disperse two- or multi-phase systems, whereby cosmetic emulsions consist of at least one fat phase (fats and mineral oils, fatty acid esters, fatty alcohols etc) and at least one water phase (water, glycols, glycols) etc.), which are distributed with the help of emulsifiers in the form of very fine droplets.
  • the oil phase is finely distributed in the water phase, it is an OI- ⁇ n-water emulsion (O / W emulsion, e.g. milk)
  • O / W emulsion e.g. milk
  • the basic character of an O / W emulsion is characterized by the water, ie it has a less greasy effect on the skin, is rather matting and is absorbed into the skin faster than a W / 0 emulsion
  • emulsions are unstable from a thermodynamic point of view, it is possible to produce cosmetic emulsions that have been stable for years.
  • An emulsion is said to be stable if there are no measurable changes in the temporal and local distribution of the droplet size distribution over a given period of time
  • the stability or instability of emulsions depends on various factors. For example, the water phase of a W / O emulsion tends to sediment because the water and oil phases have different densities. The oil phase of an O / W emulsion accordingly tends to cream
  • droplet aggregation can occur, with the individual droplets of an aggregate initially being separated from one another by a thin film of continuous phase.
  • the original droplet size distribution only changes apparently and can in this case be changed Ruhren or Schuttein can be restored
  • auxiliaries are accordingly required which prevent the two phases from segregating, but at least delay until the emulsion has fulfilled its purpose
  • these aids are intended to stabilize the interface by preventing the droplets of the disperse phase from flowing together.
  • these substances also cause the droplets to be repelled, which prevents them from approaching each other, so that aggregation can be avoided
  • auxiliary substances are used to counteract the creaming or sedimentation of the phases
  • Emulsifiers are surface-active substances that are able to reduce the interfacial tension between the oil and water phase by preferentially attaching to the interface between these two. This is made possible by their amphiphilic molecular structure.
  • Emulsifiers have at least one polar (hydrophilic) group and at least a non-polar (lipophilic) group They are soluble in both the hydrophilic and the lipophilic phase. The part that is more soluble in the corresponding phase protrudes into it and thereby reduces the interfacial tension between the two phases
  • emulsifiers also stabilize emulsions by forming interface films and thus, so to speak, "physical" barriers, thereby preventing the formation of aggregates and the coalescence of the emulsified particles.
  • the droplets are either deposited on the interface by the emulsifier. load so that they repel each other, or a stable, often highly viscous or even solid protective layer is formed around the droplets
  • the emulsifier system must therefore usually contain, in addition to the actual emulsifier, another component which is referred to as a co-emulsifier, stabilizer or, depending on the mode of action, also as a consistency agent, thickener or protective colloid, etc.
  • Stabilizers need not be surface-active but can be amphiphilic compounds
  • the viscosity of the outer phase can be increased, for example, by adding thickeners, which, for example, form gels and / or lamellar liquid crystals.
  • Emulsifiers are also in principle able to increase the viscosity of a liquid through the formation of emulsifier gel networks a comparatively high amount of emulsifier is required for this since gel networks are only formed when the entire interface between the phases is occupied by emulsifier molecules
  • an emulsion as a system of metal balls of the same diameter (inner phase) and a liquid (outer phase). Sedimentation or creaming can - in In this simple model - no longer take place when the entire liquid is filled with metal balls. This is - one assumes a densest packing of balls as a distribution - especially at a ratio of 1 2, ie if the emulsion is 2/3 full inner phase exists It is evident that the viscosity of an emulsion increases with increasing proportion of inner phase, since this limits the mobility of the dispersed droplets
  • O / W emulsions are generally stabilized by thickeners which increase the viscosity of the aqueous phase.
  • Polyacrylates (carbomer) and other organic thickeners are suitable for this purpose.
  • a disadvantage of this method of improving stability is the sensitivity of these formulations to electrolytes to produce naturally high-viscosity formulations (such as creams or ointments)
  • the stabilization of O / W emulsions via the phase volume ratio also leads to viscous formulations according to what has been said
  • emulsifiers like ultimately every chemical substance - in individual cases allergic reactions or reactions based on hypersensitivity of the user cause (although the use of the usual cosmetic emulsifiers is of course completely harmless), it is desirable to keep the emulsifier content of a cosmetic or dermatological formulation as low as possible
  • Emulsions with a very low viscosity have so far been very difficult to formulate, if at all, according to what has been said above. Accordingly, the range of such formulations is extremely low. Nevertheless, such formulations were able to offer the consumer previously unknown cosmetic services
  • Type DMA 45 from chempro / PA at 25 ° C) is not larger than 0.01 g cm "3 and, if desired, contains conventional cosmetic or dermatological auxiliaries, additives and / or active ingredients
  • the preparations according to the invention are extremely satisfactory preparations, which are not limited to a restricted selection of raw materials. Accordingly, they are particularly suitable to serve as the basis for preparation forms with a wide variety of uses.
  • the preparations according to the invention have excellent stability against disintegration into Oil and water phases and show very good sensory properties, such as spreadability on the skin or the ability to be absorbed into the skin
  • the O ⁇ / V-formulations according to the invention are stabilized by adjusting the density of the oil phase and the water phase. It was particularly surprising that the preparations according to the invention were also provided without the addition of further stabilizers, such as, for example, consistency agents, thickeners or protective colloids, etc. are stable. This was in no way predictable, especially for flowable or sprayable formulations
  • the preparations according to the invention are in every respect an enrichment of the prior art with regard to O / W emulsions, in particular with regard to flowable or sprayable O / W emulsions
  • the preparations contain significantly less than 1% by weight (based on the total weight of the preparations) of one or more emulsifiers
  • the average diameter of the oil droplets of the formulations according to the invention is less than 50 ⁇ m.
  • formulations are also preferred whose total density is greater than 0.9 g 3, in particular greater than 0.95 g cm 3
  • the O / W formulations according to the invention may furthermore be advantageous if the O / W formulations according to the invention, although it is not necessary, also contain stabilizers which are advantageously chosen from the group of thickeners. It is advantageous to adjust the content of the thickener (s) from the range 0. 05% by weight to 0 15% by weight to choose based on the total weight of the preparations
  • Advantageous UV filter substances in the sense of the present invention are substances which absorb UV radiation in the UV-A and / or UV-B range
  • cosmetic and dermatological preparations which are in the form of a sunscreen for the hair and / or the skin.
  • the total amount of the filter substances is, for example, 0.1% by weight to 30% by weight, preferably 0.5 to 20% by weight. , in particular 1.0 to 15.0% by weight, based on the total weight of the preparations, in order to provide cosmetic preparations which protect the hair or the skin from the entire range of ultraviolet radiation. It is also advantageous for the purposes of the present invention to produce cosmetic and dermatological preparations whose main purpose is not to protect against sunlight
  • UV-A filter substances for the purposes of the present invention are dibenzoyl methande ⁇ vate, in particular 4- (tert-butyl) -4'-methoxyd ⁇ benzoylmethan (CAS No. 70356-09-1), marketed by Givaudan under the trade name Parsol ® 1789 and is sold by Merck under the trade name Eusolex® 9020
  • UV-A filter substances are the phenylene-1,4-b ⁇ s- (2-benz ⁇ m ⁇ dazyl) - 3,3'-5,5'-tetrasulfonic acid
  • salts especially the corresponding sodium, potassium or tnethanolammonium salts, in particular phenylene-1,4-b ⁇ s- (2-benzimidazyl) -3,3'-5,5'-tetrasulfonic acid-bis- nat ⁇ umsalz
  • UV filter substances in the sense of the present invention are also so-called broadband filters, that is filter substances which absorb both UV-A and UV-B radiation
  • Advantageous broadband filters or UV-B filter substances are, for example, bis-resorcinyltinazine pvates with the following structure
  • R 1 , R 2 and R 3 are selected independently of one another from the group of branched and unbranched alkyl groups having 1 to 10 carbon atoms or a single hydrogen atom.
  • Particularly preferred are 2,4-B ⁇ s - ⁇ [4- (2- Ethyl-hexyloxy) -2-hydroxy] -phenyl ⁇ -6- (4-methoxyphenyl) -1, 3,5-t ⁇ az ⁇ n (INCI Aniso Tnazin), which is available under the trade name Tinosorb® S from CIBA-Chemicals GmbH is, and the 4,4 ', 4 "- (1, 3,5-Tr ⁇ az ⁇ n-2.4 l 6-tr ⁇ ylt ⁇ m ⁇ no) -tr ⁇ s-benzoesaure- tr ⁇ s (2-ethylhexyl ester), synonymous 2,4,6-T ⁇ s- [an ⁇ l ⁇ no- (p-carbo-2'-ethyl-1'-hexyl
  • UV filter substances which describe the structural motif are also described are advantageous UV filter substances in the sense of the present invention, for example the s-Tnazinden ⁇ vate described in the European published patent application EP 570 838 A1, the chemical structure of which by the gene formula
  • R represents a branched or unbranched CrC ⁇ 8 alkyl radical, a C 5 -C 2 cycloalkyl radical, optionally substituted by one or more CC 4 alkyl groups,
  • X represents an oxygen atom or an NH group
  • Rt is a branched or unbranched C 8 alkyl radical, a C 5 -C 2 cycloalkyl radical, optionally substituted with one or more C 1 -C 4 alkyl groups, or a hydrogen atom, an alkali metal atom, an ammonium group or a group of the formula means in which
  • A represents a branched or unbranched C 1 -C 8 -alkyl radical, a C 5 -C 2 -cycloalkyl or aryl radical, optionally substituted by one or more C 1 -C 4 alkyl groups
  • R 3 represents a hydrogen atom or a methyl group
  • n represents a number from 1 to 10
  • X represents the NH-- Represents group
  • A represents a branched or unbranched C 8 alkyl radical, a C 5 -C 2 cycloalkyl or aryl radical, optionally substituted by one or more CC alkyl groups,
  • R 3 represents a hydrogen atom or a methyl group
  • n represents a number from 1 to 10 when X represents an oxygen atom
  • a particularly preferred UV filter substance in the sense of the present invention is also an asymmetrically substituted s-Tnazine, the chemical structure of which is represented by the formula
  • Also advantageous for the purposes of the present invention are the 2,4-bis - ⁇ [4- (3-sulfonato) - 2-hydroxy-propyloxy) -2-hydroxy] phenyl ⁇ -6- (4-methoxyphenyl) -1, 3,5-Tr ⁇ az ⁇ n sodium salt, the 2,4-B ⁇ s - ⁇ [4- (3- (2-propyloxy) -2-hydroxypropyloxy) -2-hydroxy] phenyl ⁇ -6- (4-methoxyphenyl ) -1, 3,5-tr ⁇ az ⁇ n, the 2,4-B ⁇ s - ⁇ [4- (2-ethylhexyloxy) -2-hydroxy] phenyl ⁇ -6- [4- (2-meth-oxyethyl-carboxyl ) -phenylam ⁇ no] -1, 3,5-tr ⁇ az ⁇ n, the 2,4-B ⁇ s - ⁇ [4- (3- (2-propyloxy) -2-
  • An advantageous broadband filter for the purposes of the present invention is 2,2'-methylene-b ⁇ s- (6- (2H-benzot ⁇ azol-2-yl) -4- (1, 1, 3,3-tetramethylbutyl) phenol) , which is characterized by the chemical structural formula
  • Tinosorb® M is marked and is available under the trade name Tinosorb® M from CIBA-Chemika en GmbH
  • Another advantageous broadband filter for the purposes of the present invention is 2- (2H-benzot ⁇ azol-2-yl) -4-methyl-6- [2-methyl-3- [1, 3,3,3-tetramethyl-1 - [( t ⁇ methyls ⁇ lyl) oxy] d ⁇ - s ⁇ loxanyl] propyl] -phenol (CAS No. 155633-54-8) with the INCI name Dromet ⁇ zole T ⁇ siloxane, which is characterized by the chemical structural formula
  • UV-B filters can be batch-soluble or water-soluble.
  • Advantageous oil-soluble UV-B filter substances are, for example
  • 3-benzyl camphor derivatives preferably 3- (4-methylbenzyl) camphor, 3-benzylidene camphor, ⁇ 4-aminobenzoic acid derivatives, preferably 4- (dimethylamino) benzoic acid (2-ethylhexyl) esters, 4- (dimethylamino), benzoate.
  • esters of benzalmalonic acid preferably 4-methoxybenzalmalonic acid (2-ethylhexyl) ester
  • esters of cinnamic acid preferably 4-methoxycinnamic acid (2-ethylhexyl) ester
  • 4-methoxycinnamic acid isopentyl ester
  • benzophenone preferably 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone, 2,2'-dihydroxy-4-methoxybenzophenone
  • Advantageous water-soluble UV-B filter substances are, for example
  • Salts of 2-phenylbenzimidazole-5-sulfonic acid such as its sodium-potassium or T ⁇ -ethanolammonium salt, and the sulfonic acid itself,
  • sulfonic acid derivatives of 3-benzyl-iodide camphor such as 4- (2-oxo-3-bornyl-iodomethyl) benzenesulfonic acid, 2-methyl-5- (2-oxo-3-bornyl-iodomethyl) sulfonic acid and their salts
  • Another advantageous light protection filter substance according to the invention is ethylhexyl-2-cyano-3,3-diphenylacrylate (octocrylene), which is available from BASF under the name UvinuP N 539 and is distinguished by the following structure
  • the UV filter substances can be liquid or solid at room temperature
  • UV filter substances which are liquid at room temperature and which can be used for the purposes of the invention are, preferably, homomenthyl salicylate, 2-ethyl-hexyl-2-cyano-3,3-diphenylacrylate, 2-ethylhexyl-2-hydroxybenzoate and esters of cinnamic acid 4-Methoxyz ⁇ mtsaure (2-ethy! Hexyl) ester and 4-Methoxyz ⁇ mtsaure- isopentyl ester
  • Homomenthyl salicylate (INCI homosalate) is characterized by the following structure
  • 2-Ethylhexyl-2-hydroxybenzoate (2-Ethylhexylsal ⁇ cylat, Octylsa cylat, INCI Octyl Sahcy- late) is available for example from Haarmann & Reimer under the trade name Neo Heliopan OS and is characterized by the following structure
  • the oil phase of the O / W formulations according to the invention advantageously has a high content of UV filter substances according to the invention or can even consist entirely of such substances.
  • the cosmetic and dermatological preparations according to the invention can accordingly also contain oil components as are customarily used in such preparations
  • UV filter substances according to the invention which are liquid or solid at room temperature, are dissolved, for example, in the oil phase of the formulations, as a result of which the density of the oil phase is adjusted to the density of the water phase
  • the subject of the invention is also a
  • O / W formulations obtainable by this process are also the subject of the present invention
  • the present invention further relates to a method for stabilizing O / W formulations, which in turn is based on inventive activity, the density of the water phase being the density of the oil phase, which contains at least one UV filter substance, by adding electrolytes and / or polyols are adjusted in such a way that the density difference of the two phases (determinable with a computing digital density meter of the type DMA 45 from chempro / PA at 25 ° C.) is not greater than 0.01 g cm "3
  • the present invention also relates to O / W formulations which can be obtained by this process
  • Very stable O / W formulations for example sprayable formulations with a high sun protection factor, can be obtained by the processes according to the invention in a surprisingly simple manner, it being possible for elegantly incorporated polar oils into the preparations
  • the electrolyte or electrolytes are advantageously selected from the following groups
  • water-soluble UV filter substances mostly present as alkali salts, in particular those which have one or more sulfonic acid groups or sulfonate groups on their molecular structure
  • Advantageous water-soluble UV filter substances are, for example
  • ⁇ Salts of 2-phenylbenz ⁇ m ⁇ dazol-5-sulfonic acid such as their sodium-potassium or their t ⁇ ethanolammonium-Saiz, especially the phenylene-1, 4-b ⁇ s- (2-benz ⁇ m ⁇ dazyl) - 3 3'-5,5'-tetrasulfonic acid b ⁇ s -nat ⁇ umsalz and the sulfonic acid itself, ⁇ sulfonic acid derivatives of the 3-Benzyl ⁇ dencamphers such as 4- (2-Oxo-3-bornyl ⁇ den- methyl) benzenesulfonic acid and / or 2-methyl-5- (2-oxo-3-bornyl ⁇ denmethyl) sulfonic acid and its salts, for example the corresponding sodium, potassium or tnethanolammonium salt, Sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and its salts, for example the
  • Chlorides also inorganic oxo-element anions, of these in particular sulfates, carbonates, phosphates, borates and aluminates. Electrolytes based on organic anions are also advantageous, for example lactates, acetates, benzoates, propionates, tartrates, citrates, amino acids and their salts and others Comparable effects can also be achieved with ethylenediaminetetraacetic acid and its salts
  • Cations of these salts are preferably ammonium, alkylammonium, alkali metal, alkaline earth metal, magnesium, iron or zinc ions. There is no need to mention that only physiologically acceptable electrolytes should be used in cosmetics. Potassium chloride is particularly preferred. Table salt, magnesium sulfate, zinc sulfate and mixtures thereof
  • Amino acids are a component of the natural moisture factor (the so-called natural moisturing factor).
  • the addition of amino acids, in particular essential amino acids, is to be regarded as advantageous since hydration processes can bind moisture in the skin
  • Amino acids with a particularly advantageous cosmetic or dermatological effect are glycine, alanine, valine, leucm, isoleucine, phenylalanine, tyrosine, proline, hydroxyprohn, senn, threonine, cysteine, methionine, tryptophan, arginine
  • R '- C - COOH where R' and R "are selected independently of one another from the groups
  • Forms ring atoms and where the ⁇ -hydroxycarboxylic acids or the ⁇ -hydroxycarboxylic acids or the ⁇ -ketocarboxylic acids may be present in the form of their physiologically acceptable salts
  • ⁇ -hydroxycarboxylic acids according to the invention are advantageously chosen from the following classes of substances (these also being representative of their salts or anions)
  • ⁇ -hydroxy fatty acids which in turn are particularly advantageously selected from the group of C 10- ⁇ s-alkyl carboxylic acids, especially ⁇ -hydroxy carboxylic acids, according to the formula
  • n represents a number less than 7, ⁇ -hydroxy sugar acids, aliphatic ⁇ -hydroxy fruit acids, especially malic acid, lactic acid, citric acid, tartaric acid,
  • mixtures of aliphatic ⁇ -hydroxycarboxylic acids in particular in the form of wool wax acid mixtures, in which the content of ⁇ -hydroxycarboxylic acids is 20 to 30% by weight, based on the total composition
  • Preferred ⁇ -ketocarboxylic acid is pyruvic acid ( ⁇ -oxopropanoic acid)
  • the total amount of one or more electrolytes in the finished cosmetic or dermatological preparations is chosen so that the density of the water phase is adjusted to the density of the UV filter phase in such a way that the density difference of the two phases (determinable with a computing digital density meter of type DMA 45 from the company chempro / PA at 25 ° C) is not larger than 0.01 g cm "3. This amount can be easily determined without trial and error without own inventive step
  • Advantageous polyols in the sense of the present invention are low C number polyols, for example glycene, ethylene glycol, propylene glycol and / or butylene glycol and the like
  • O / W formulations according to the present invention are to contain emulsifiers, it is advantageous to use those emulsifiers which are suitable for producing O / W emulsions, which may be present either individually or in any combination with one another
  • the emulsifier or emulsifiers are particularly preferably selected from the group of fatty acids which are wholly or partly neutralized with customary alkalis (such as sodium and potassium hydroxide, sodium and potassium carbonate and mono- and tetrahanolamine).
  • customary alkalis such as sodium and potassium hydroxide, sodium and potassium carbonate and mono- and tetrahanolamine.
  • stearic acid and stearates are particularly advantageous , Isostea ⁇ nsaure and Isostearate, Palmitmsaure and Palmitate as well as My ⁇ stinsaure and My ⁇ state
  • the emulsifiers are furthermore preferably selected from the group of saturated and / or unsaturated, branched and / or unbranched fatty alcohols having 10 to 40 carbon atoms, butyl octanol, butyl decanol, hexyl octanol, hexyl decanol, ethyl dodecanol, behenyl alcohol (C 22 H 5 OH), cetearyl alcohol [a mixture of cetyl alcohol (C 16 H 33 OH) and stearyl alcohol (C ⁇ 8 H 37 OH)], cetylarachidol [2-hexadecyl-1-ecoscosanol (C 36 H 73 ⁇ H),], lanohn alcohols (wool wax alcohols, which represent the unsaponifiable alcohol fraction of the wool wax which is obtained after the saponification of wool wax) and / or 2-tetradecyloctadecanol (C 32 H 65 ).
  • Hydrocolloids are macromolecules that are largely linear in shape and have intermolecular interaction forces that enable secondary and main valence bonds between the individual molecules and thus the formation of a network-like structure. They are partially water-soluble natural or synthetic polymers that form gels or in water-based systems Viscous solutions increase the viscosity of the water either by binding water molecules (hydration) or by absorbing and enveloping the water in their intertwined macromolecules, while at the same time restricting the mobility of the water
  • the group of hydrocolloids can be divided into the following. organic, natural compounds, such as agar agar, carrageenan, tragacanth, acacia, alginates, pectins, polyoses, guar flour, locust bean gum, starch, dextrins, gelatin, casein,. organic, modified natural substances, such as, for example, carboxymethyl cellulose and other cellulose ethers, hydroxyethyl and propyl cellulose and the like,. organic, fully synthetic compounds, such as polyacrylic and polymethacrylic compounds, vinyl polymers, polycarboxylic acids, polyethers, polyimines, polyamides,. inorganic compounds, such as, for example, polysilicic acids, clay minerals such as montmolononites, zeolites, silicas
  • Hydrocolloids preferred according to the invention are, for example, methyl celluloses, as the methyl ethers of cellulose are referred to. They are distinguished by the following structural formula
  • R can represent a hydrogen or a methyl group
  • cellulose mixed ethers which are generally also referred to as methyl celluloses and which, in addition to a dominant content of methyl, additionally contain 2-hydroxyethyl, 2-hydroxypropyl or 2-hydroxybutyl groups.
  • Particularly preferred (hydroxypropyl) methyl celluloses for example those available under the trade name Methocel E4M from Dow Chemical Compute.
  • sodium carboxymethyl cellulose the sodium salt of the glycolic acid ether of cellulose, for which R in structural formula I can be a hydrogen and / or CH 2 COONa.
  • R in structural formula I can be a hydrogen and / or CH 2 COONa.
  • Particularly preferred is the cellulose gum available from Aqualon under the trade name Natrosol Plus 330 CS designated sodium carboxymethyl cellulose
  • xanthan (CAS No. 11138-66-2), also known as xanthan gum, which is an anionic heteropolysaccharide which is generally formed from corn sugar by fermentation and is isolated as the potassium salt. It is obtained from Xanthomonas campest ⁇ s and some other species under aerobic conditions with a molecular weight of 2 * 10 5 to 24 * 10 6 produces xanthan is formed from a chain with ß-1, 4-bound glucose (cellulose) with side chains
  • the structure of the subgroups (“repeated units” ) consists of glucose mannose, glucuronic acid, acetate and pyruvate
  • Hydrocolloids which are advantageous according to the invention are also polymers of acrylic acid, in particular those selected from the group of the so-called carbomers or carbopoles (Carbopol® is actually a registered trademark of the BF Goodrich Company). Carbopols are compounds of the general structural formula
  • the carbopole group also includes acrylate-alkyl acrylate copolymers, for example those which are distinguished by the following structure
  • R ' represents a long-chain alkyl radical and x and y numbers which symbolize the respective stochiometric portion of the respective comonomers.
  • carbopole 981 is particularly preferred , 1382 and 5984 (both individually and in combination with other hydrocolloids)
  • copolymers of C ⁇ o comparable to the acrylate-alkyl acrylate copolymers.
  • the INCl designation for such compounds is "Acrylates / C 10-30 Alkyl Acrylate Crosspolymer”.
  • Pemulen TR1 and Pemulen TR2 are particularly advantageous available from the BF Goodrich Company
  • the total amount of one or more hydrocolloids in the finished cosmetic or dermatological preparations is advantageously chosen to be less than 1.0% by weight, preferably between 0.01 and 0.5% by weight, based on the total weight of the preparations
  • the aqueous phase of the preparations according to the invention optionally advantageously contains polyol ethers, such as, for example, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether, diethylene glycol monomethyl or monoethyl ether and analogous products, furthermore alcohols or diols of lower C numbers - preferably ethanol, isopropanol and 1, 2-propanediol
  • antioxidants are used as additives or active ingredients.
  • the preparations advantageously contain one or more antioxidants. All the antioxidants suitable or customary for cosmetic and / or dermatological applications can be used as inexpensive but nevertheless optional antioxidants
  • the antioxidants are advantageously selected from the group consisting of amino acids (for example glycine, histidine, tyrosine, tryptophan) and their derivatives, tmidazoles (for example urocanic acid) and their derivatives, peptides such as D, L-carnosine, D-carnosine, L-carnosine and its derivatives (e.g. Anse ⁇ n), carotmoids, carotenes (e.g. ⁇ -carotene, ß-carotene, lycopene) and their derivatives, lipoic acid and their derivatives (e.g. dihydroponic acid), aurothioglucose, propylthiouracil and other thiols (e.g.
  • amino acids for example glycine, histidine, tyrosine, tryptophan
  • tmidazoles for example urocanic acid
  • peptides such as D, L-carnosine, D-carnosine,
  • buthionine sulfoximines in see r low contractual dosages (e.g. pmol to ⁇ mol / kg), also (metal) chelators (e.g. ⁇ -hydroxy fatty acids, palmitic acid, phytic acid, lactofer ⁇ n), ⁇ -hydroxy acids (e.g. citric acid, lactic acid, malic acid), humic acid, bile acid , Bile extracts, bihrubin, biliverdin, EDTA, EGTA and their derivatives, unsaturated fatty acids and their derivatives (e.g.
  • ⁇ -oleolic acid linoleic acid, oleic acid
  • folic acid and their derivatives ubiquinone and ubichmol and their derivatives
  • vitamin C and derivatives e.g. Ascorbyl palmitate, Mg - ascorbyl phosphate, ascorbylacetate
  • tocopherols and derivatives e.g.
  • vitamin E acetate
  • vitamin A and derivatives vitamin A palmitate
  • konyferyl benzoate of benzoin resin rutinic acid and its derivatives, ferulic acid and its derivatives, butylhydroxy toluene, Nordihydroxy toluene, Nordihydroxy - Guaiac resin acid, Nordihydroguajaretsaure, T ⁇ hydroxybutyrophenon, uric acid and their derivatives, mannose and their derivatives, zinc and its derivatives (eg ZnO, ZnS ⁇ 4) selenium and its derivatives (eg selenium methionm), stilbenes and their derivatives (eg 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
  • preparations according to the invention are very good vehicles for cosmetic or dermatological active ingredients in the skin, preferred active ingredients being antioxidants which can protect the skin from oxidative stress.
  • preferred active ingredients being antioxidants which can protect the skin from oxidative stress.
  • Preferred antioxidants are vitamin E and its derivatives and Vitamin A and its derivatives
  • 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 0.1 to 10% by weight, based on the total weight of the preparation
  • vitamin E and / or its derivatives represent the antioxidant (s)
  • vitamin A or vitamin A derivatives or carotenes or their derivatives represent the antioxidant (s)
  • the cosmetic and dermatological preparations according to the invention can also contain cosmetic auxiliaries as are customarily used in such preparations, for example consistency agents, fillers, preservatives, Perfumes, anti-foaming substances, dyes, other surface-active Substances, softening, moisturizing and / or moisturizing substances, anti-inflammatory substances, additional active substances such as vitamins or proteins, light stabilizers, insect repellents, bactericides, virucides, water, salts, antimicrobial, proteolytically or keratolytically active substances, medicines or other common components of a cosmetic or dermatological formulation such as alcohols, polyols, polymers, foam stabilizers, organic solvents or electrolytes
  • the O / W emulsions according to the invention can serve as the basis for cosmetic or dermatological formulations. These can be composed as usual and, for example, for the treatment and care of the skin and / or the hair, as a lip care product, as a de-product and as a make-up or make-up removal product in the Decorative cosmetics or used as a sunscreen preparation
  • the cosmetic and dermatological preparations according to the invention are applied to the skin and / or the hair in a sufficient amount in the manner customary for cosmetics or dermatics
  • cosmetic or topical dermatological compositions in the sense 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 is possibly possible and advantageous to use the compositions according to the invention as the basis for pharmaceuticals Use wording
  • the low-viscosity cosmetic or dermatological agents according to the invention can be present, for example, as preparations sprayable from aerosol containers, squeeze bottles or by a pump device or in the form of a liquid composition that can be applied by means of roll-on devices, but also in the form of an emulsion that can be applied from normal bottles and containers
  • Suitable blowing agents for cosmetic or dermatological preparations which can be sprayed from aerosol containers in the sense of the present invention are the customary known volatile, liquefied blowing agents, for example hydrocarbons (propane butane, isobutane), which can be used alone or in a mixture with one another. Compressed air can also be used advantageously

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Abstract

L'invention concerne des préparations cosmétiques ou dermatologiques du type huile dans l'eau, qui contiennent une phase huileuse, dans laquelle est incorporée au moins une substance filtrant les UV, et une phase aqueuse. La différence de densité entre la phase huileuse et la phase aqueuse (pouvant être déterminée avec un densimètre numérique calculateur, du type DMA 45 de la société chempro/PA, à 25 DEG C) ne dépasse pas 0,01 g.cm<-3>. L'invention concerne également un procédé pour stabiliser des formulations huile dans l'eau.
EP00987407A 2000-01-05 2000-12-15 Preparations cosmetiques ou dermatologiques du type huile dans l'eau Withdrawn EP1244416A2 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10000209 2000-01-05
DE10000209A DE10000209A1 (de) 2000-01-05 2000-01-05 Kosmetische oder dermatologische Zubereitungen vom Typ Öl-in-Wasser
PCT/EP2000/012822 WO2001049253A2 (fr) 2000-01-05 2000-12-15 Preparations cosmetiques ou dermatologiques du type huile dans l'eau

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EP1244416A2 true EP1244416A2 (fr) 2002-10-02

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US (1) US20030049214A1 (fr)
EP (1) EP1244416A2 (fr)
JP (1) JP2003526636A (fr)
DE (1) DE10000209A1 (fr)
WO (1) WO2001049253A2 (fr)

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JP2003526636A (ja) 2003-09-09
DE10000209A1 (de) 2001-07-12
US20030049214A1 (en) 2003-03-13
WO2001049253A2 (fr) 2001-07-12

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