Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/34—Alcohols
  • A61K8/345—Alcohols containing more than one hydroxy group
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
  • A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/55—Phosphorus compounds
  • A61K8/553—Phospholipids, e.g. lecithin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders

Definitions

• the invention relates to lecithin and essential fatty acids containing cosmetic and / or dermatological formulations which ensure maximum hydration of the skin with a simultaneous acceleration of metabolic processes, so that the healing process of damaged skin is supported.
• the formulations according to the invention give a remarkably pleasant feeling on the skin.
• a cosmetic and / or dermatological formulation achieves the stated object if this formulation contains lecithin, as lipid phase a native oil with a defined, preferably high, content of fatty acids, in particular essential fatty acids, e.g.
• Sunflower oil and glycerol (and / or ethylene glycol, 1, 3-propanediol and / or tert-butyl alcohol), propylene glycol (and / or polyethylene glycol), benzyl alcohol (and / or benzylacetone and / or benzaldehyde), phenylethyl alcohol (and / or 2-phenylacetate ), Benzyl alcohol (and / or phenylethyl alcohol) and purified water.
• Lecithin belongs to the group of phosphoglycerides, which are also called phosphatides or phospholipids. These compounds are fat-like triglycerides with two long-chain fatty acids and one Phosphoric acid residue, to which an ammonium radical is attached, as shown below:
• Lecithin is not a pure substance but a mixture of different fatty acid esters depending on their origin. Particularly preferred is the use of lecithin from chicken eggs and / or soybeans. Another source is e.g. Rape.
• the lecithin from soya is obtained by extraction of the soya with ethanol and the lecithin purified by chromatography is then hydrogenated.
• the phosphatidylcholine (lecithin) thus obtained contains 80% to 90% stearic acid, preferably about 85% stearic acid and 10% by weight to 20% by weight palmitic acid, preferably about 15% palmitic acid, as fatty acid residues.
• a particularly suitable lecithin is the Phospholipon available from PHOSPHOLIPID GmbH, Cologne, Germany ® 80 H and the Phospholipon ® 90 H.
• Lecithin is widely used in cosmetic formulations. As a component of ointments and creams it promotes the permeation of active ingredients into the skin and significantly improves the water retention capacity of the stratum corneum in gel preparations. Due to the increase in moisture absorption of the skin, the roughness of the skin is lowered. As an emulsifier, lecithin has a very low irritation potential (no washout effect). With lecithin W / O emulsions with high water content can be produced. Lecithin is a natural antioxidant and is used as an emulsifier in bath oils. Hydrogenated lecithin is suitable as a gelling and thickening agent in cosmetic preparations.
• Another essential component of the formulations according to the invention are essential fatty acids which are preferably added to the formulation in the form of suitable oils.
• suitable oils include sunflower oil, olive oil, corn oil, linseed oil, cod liver oil and fish oil.
• These oils of native origin are added to the formulations of the present invention in an amount of 3.0-20.0 wt%, preferably 6.0-16.0 wt%, more preferably 7-14 wt% preferably 8.0-12.0% by weight, more preferably still 9-11% by weight, and especially preferably 10.0% by weight.
• oils of natural origin are selected according to their content and composition of fatty acids, including essential fatty acids, dermatologically and their technological suitability.
• the refined sunflower oil in pharm. EUR. Quality is preferred for the formulations of the invention.
• This refined sunflower oil (Helianthi annui oleum raffinatum) is obtained from the seed of Helianthus annuus C., has a specific gravity of 0.921 and a refractive index of 1.474, an acid value of at most 0.5 (determined with 10 g of substance), a peroxide value !
• fatty acid composition palmitic acid 4% by weight - 9% by weight, stearic acid 1% by weight - 7% by weight, oleic acid 14% by weight - 40% by weight and linoleic acid 48% by weight. -% - 74 wt .-%.
• sunflower oil (Helianthus annuus L) consists of 39 wt .-% oleic acid, 34 wt .-% ⁇ -linoleic acid, 13 wt .-% ß-linoleic acid, about 4 wt .-% glycerol, about 9 wt .-% saturated fatty acids (palmitic, stearic, arachic and linoceric), carotenoids and lecithin.
• the fatty acid fraction of the sunflower oils used preferably contains 15-35% by weight of oleic acid, 50-72% by weight of linoleic acid.
• Oleic acid is also known as Acidum oleinicum, cis-9-octadecenoic acid, oleic acid or oleic acid.
• EFAs Essential fatty acids
• Essential fatty acids always exist in the cis and not in the trans configuration and are characterized by two or more unsaturated carbon atoms, ie by at least one double bond. Characteristic is the position at which the first double bond in the fatty acid chain, as seen from the end of the methyl end (omega end), is positioned.
• omega-6 derived from cis-linolenic acid
• omega-3 derived from alpha-linolenic acid.
• the most important groups of omega fatty acids are omega-3, -6 and -9 fatty acids.
• the omega-3 fatty acids include ⁇ -linolenic acid, eicosapentaenoic acid and docohexaenoic acid.
• Omega-6 fatty acids include ⁇ -linolenic acid, linoleic acid, arachidonic acid, delta-is-cis-cis-docosadienoic acid (22: 2), delta-11-cis, 14-cis-eicosa- / icosadienoic acid (20: 2) and delta-7-cis, 10-cis-hexadecadienoic acid (16: 2).
• the omega-9 fatty acids include oleic acid (delta-9-octadecenoic acid, 18: 1), gondoic acid (delta-11-cis-eicosenic / icosenoic acid, 20: 1), erucic acid (delta-13-cis-docosenoic acid, 22 : 1) as well as nervonic acid (delta-15-cis-tetracenoic acid, 24: 1).
• linoleic acid The highest content of linoleic acid is found in vegetable oils such as safflower or safflower oil, sunflower hemp and soybean oil, and vegetable margarine.
• the threefold unsaturated alpha-linolenic acid (9,12,15-octadecatrienoic acid) is mainly present in linseed oil (55%), walnut oil (14%), rapeseed oil (11%) and hemp oil (7%).
• Table 1 shows important omega-3 and 6-fatty acids, their chain length and position as well as their occurrence.
• unsaturated fatty acids are preferably selected from the group comprising oleic acid, eicosapentaenoic acid, timnodonic acid, docosahexaenoic acid, arachidonic acid, linoleic acid, ⁇ -linolenic acid, ⁇ -1-nolinic acid and mixtures of the abovementioned fatty acids. These mixtures comprise in particular mixtures of the pure unsaturated compounds.
• oils are preferably used as component b which contain at least 20%, preferably at least 25%, more preferably at least 30% and especially preferably at least 35% of omega fatty acids.
• omega fatty acids especially the omega-9 fatty acids are preferred and among the omega-9 fatty acids in particular the oleic acid. Furthermore, the omega-6 fatty acids are particularly suitable for the production of the formulation according to the invention and the linoleic acid among the omega-6 fatty acids.
• the oils used as component b according to the invention preferably contain more than 78% by weight of oleic and linoleic acid, more preferably more than 86% by weight and more preferably more than 93% by weight of oleic and linoleic acid.
• the oils used as component b preferably contain more than 13% by weight of oleic acid, more preferably more than 24% by weight of oleic acid and more preferably more than 34% by weight of oleic acid.
• oils as component b contain more than 38% by weight of linoleic acid ( ⁇ -linoleic acid + ⁇ -linoleic acid), preferably more than 47% by weight of linoleic acid, more preferably more than 57% by weight of linoleic acid and particularly preferably more than 67% by weight of linoleic acid.
• Another particularly suitable oil is a sunflower oil (Helianthus annuus L.) containing 39% by weight of oleic acid, 34% by weight of ⁇ -linoleic acid and 13% by weight of ⁇ -linoleic acid,
• oils are linseed oil, hemp oil, corn oil, walnut oil, rapeseed oil, soybean oil, sunflower oil, poppy seed oil, safflower oil, wheat germ oil, thistle oil, grape seed oil, evening primrose oil, borage oil, black cumin oil, algae oil, fish oil, cod liver oil and / or mixtures of the aforementioned oils , Particularly suitable is sunflower oil. It is also possible to add one or more essential fatty acids to the oils to provide the necessary amount of essential fatty acids.
• Fish oil and cod liver oil mainly contain eicosapentaenoic acid (EPA C20: 5) and docosahexaenoic acid (DHA C22: 6) in addition to low alpha-linolenic acid (ALA C18: 3).
• Omega-3 fatty acids are found not only in fish oil but also in vegetable oils. Table 2 below shows a list of fatty acid components in various oils.
• Tables 3, 4 and 5 show a list of monoolefinic, polyunsaturated and acetylenic fatty acids which are preferably used in the present invention.
• Non-essential fatty acids or trans-fatty acids may also be added to the formulation according to the invention together with the essential fatty acids, the abovementioned weight percentage being at least 30% by weight, preferably 40% by weight and in particular at least 50% by weight of essential Fatty acids should not fall below.
• the maximum amount by weight of essential fatty acids should not exceed 25 g per 100 g formulation
• the cosmetic and / or dermatological formulations according to the invention contain glycerol as an 85% solution in water, propylene glycol or polyethylene glycol as bodying agent, benzyl alcohol, benzylacetone and / or benzaldehyde and also phenylethyl alcohol and / or 2-phenylacetate.
• the glycerol used can have a water content of up to 20%.
• ethylene glycol, 1, 3-propanediol, tert-butyl alcohol! and / or alcohols having boiling points above 125 ° C preferably above 15O 0 C and preferably diols or triols are used.
• Benzyl alcohol, benzylacetone and / or benzaldehyde are added as permeability enhancers to accelerate metabolic processes in the skin as well as stabilizing agents for the formulation.
• Phenylethyl alcohol and 2-phenylacetate also serve as permeability enhancers for accelerating metabolic processes in the skin and also stabilize the formulation.
• benzylic alcohol and phenylethyl alcohol also lead to an unexpected synergistic effect between the components of the cosmetic and / or dermatological formulation according to the invention, which As a result, with very good moisturizing of the skin, metabolic processes in the skin are stimulated and accelerated and, in addition, a support of the lipid barrier takes place. As a result, the formulations according to the invention are suitable both for the treatment of damaged skin and for the smoothing of wrinkles with prolonged use.
• formulations which are not only suitable for dermatological use, for example in acne, atopic dermatitis and / or dermatitis, but at the same time also achieve a cosmetic effect, for example the smoothing of wrinkles by the support of the structure as well as the regeneration of the lipid barrier and / or the stimulation as well as acceleration of metabolic processes in the skin.
• a cosmetic effect for example the smoothing of wrinkles by the support of the structure as well as the regeneration of the lipid barrier and / or the stimulation as well as acceleration of metabolic processes in the skin.
• Particularly advantageous is the addition of benzyl alcohol and / or phenylethyl alcohol, which also contribute to a marked increase in viscosity in addition to a pronounced synergistic effect.
• This significant spontaneous increase in viscosity achieved in particular by benzyl alcohol is essential for the matrix or gel skeleton formation and thus for the dermatological / cosmetic function of the formulations according to the invention.
• propylene glycol which is preferably present in weight percentages of at least 8 wt%, more preferably 9 wt%, 10 wt%, 11 wt%, 12 wt%, 13 wt%. -%, And particularly preferably 14 wt .-% is used.
• the function of propylene glycol in the formation of the special framework structure of the formulations according to the invention has not yet been clarified, but an effect on the consistency of the formulation is clearly detectable.
• the cosmetic and / or dermatological formulations according to the invention contain lecithin in an amount of 0.5-20.0% by weight, preferably 2.0-10.0% by weight, more preferably 3.0-5.0% by weight. -%, and more preferably 4.0 wt .-%.
• Glycerol is added as an 85% solution in water in an amount of 0.5-30.0% by weight, preferably 3.0-10.0% by weight, more preferably 5.0-7.0% by weight. -%, even more preferably 4.5 to 6.0 wt .-% and particularly preferably 5.0 wt .-% used.
• the amount of propylene glycol and / or polyethylene glycol used is 0.5-50.0 wt%, preferably 6-35 wt%, 7-30 wt%, 7.5-28 wt%, 8 - 26 wt .-%, 8.5 - 25 wt .-%, 9 - 24 wt .-%, 9.5 - 23 wt .-%, more preferably 10.0 - 22.0 wt .-%, further preferably 11-21% by weight, 12-20% by weight, 13-19% by weight, even more preferably 14.0-18.0% by weight, furthermore preferably 15-17% by weight. % and most preferably 16.0 wt .-%.
• the aforementioned weight percentages are only for propylene glycol, i.
• Polyethylene glycol is not present.
• Benzyl alcohol, benzylacetone and / or benzaldehyde are used in an amount of 0.1-15.0% by weight, preferably 1.0-10.0% by weight, more preferably 2.0-4.0% by weight. and particularly preferably used of 3.0 wt .-%.
• the cosmetic and / or dermatological formulations according to the invention comprise phenylethyl alcohol and / or 2-phenylacetate in an amount of 0.1-15.0% by weight, preferably 0.2-5.0% by weight, furthermore preferably 0.3 - 1, 5 wt .-% and particularly preferably 0.5 wt .-%.
• Purified water is added to the above ingredients in an amount to supplement the formulation to 100% by weight (ad 100% by weight).
• lecithin preferably a formulation of the following ingredients: lecithin, native oil with a defined content of essential fatty acids, such as e.g. Sunflower oil and glycerin, propylene glycol, benzyl alcohol, phenylethyl alcohol and purified water.
• essential fatty acids such as e.g. Sunflower oil and glycerin
• propylene glycol propylene glycol
• benzyl alcohol benzyl alcohol
• phenylethyl alcohol preferably purified water.
• compositions according to the invention may also be supplemented with customary odorants or perfumes, dyes, preservatives, viscosity-increasing substances and / or UV filters.
• customary odorants or perfumes are used in particular to increase the color, light and / or perfume stability of Formulations or shelf life or consistency.
• Such additives are present in total in not more than 10 wt .-%, preferably 8 wt .-%, more preferably 6 wt .-% and particularly preferably 4 wt .-% in the formulation.
• the cosmetic and / or dermatological formulations according to the invention can advantageously be used for the treatment of all forms from impure to damaged skin. From blemished to damaged skin, for example, all forms of acne, atopic dermatitis or atypical dermatitis are to be understood.
• Cosmetic and / or dermatological formulations are, in particular, skin creams, skin lotions, milks, ointments, oils and balms and all other formulations suitable for topical application.
• Example 1 Example 4: Example 7: Example 10:
• Detection of the viscosity increase A suspension of 100 g of lecithin (phosphatidylcholine 8OH, Fa. Lipoid) and 900 g of water is mixed with 20 g of benzyl alcohol at 30 - 4O 0 C.
• the viscosity before the addition of the benzyl alcohol was about 2180 mPas (Haake RV / 7 (Brookfield) immersion R3, 30 up / m, 38 ° C) after the addition of benzyl alcohol but about 54790 mPas (immersion R5, 4 up / m , 34 ° C).
• the viscosity increase is permanent.

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• 2004
  • 2004-06-28 DE DE102004031210A patent/DE102004031210A1/de not_active Withdrawn
• 2005
  • 2005-06-22 BR BRPI0505988-7A patent/BRPI0505988A/pt not_active IP Right Cessation
  • 2005-06-22 US US10/569,770 patent/US20060257352A1/en not_active Abandoned
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  • 2005-06-22 WO PCT/DE2005/001112 patent/WO2006000196A1/de active Application Filing
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  • 2005-06-22 EP EP05759725A patent/EP1763335A1/de not_active Withdrawn
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