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EP2453868A2 - Concentrés liquides ou fluides pour le bain ou la douche formant des protéasomes, formes galéniques de ces concentrés et leur utilisation - Google Patents

Concentrés liquides ou fluides pour le bain ou la douche formant des protéasomes, formes galéniques de ces concentrés et leur utilisation

Info

Publication number
EP2453868A2
EP2453868A2 EP10732867A EP10732867A EP2453868A2 EP 2453868 A2 EP2453868 A2 EP 2453868A2 EP 10732867 A EP10732867 A EP 10732867A EP 10732867 A EP10732867 A EP 10732867A EP 2453868 A2 EP2453868 A2 EP 2453868A2
Authority
EP
European Patent Office
Prior art keywords
mixtures
weight
bath
protein
fatty
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP10732867A
Other languages
German (de)
English (en)
Inventor
Rolf Beutler
Karl Heinz Schmidt
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.)
Merz Pharma GmbH and Co KGaA
Original Assignee
Merz Pharma GmbH and Co KGaA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merz Pharma GmbH and Co KGaA filed Critical Merz Pharma GmbH and Co KGaA
Publication of EP2453868A2 publication Critical patent/EP2453868A2/fr
Withdrawn legal-status Critical Current

Links

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
    • A61Q19/10—Washing or bathing preparations
    • 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
    • A61K8/14—Liposomes; Vesicles
    • 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
    • A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
    • A61K8/645—Proteins of vegetable origin; Derivatives or degradation products 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
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

  • the present invention relates to balneological preparations, in particular
  • Bath and shower preparations which, as a flowable or liquid premix concentrate, comprise liposome-forming components such as phospholipids in addition to natural and / or synthetic lipids, and furthermore are present as mixtures with predominantly vegetable proteins, surfactants and optionally additives.
  • liposome-forming components such as phospholipids in addition to natural and / or synthetic lipids, and furthermore are present as mixtures with predominantly vegetable proteins, surfactants and optionally additives.
  • These stable systems on contact with an excess of water form directly skin-active proteoliposomes with catalytic activity for improved drug delivery into the skin. They can be used directly or in diluted or solid forms of application (such as lipid proteosome shower preparation, proteosome bath powder, etc.).
  • Balneological preparations such as soaps, oils, etc.
  • Balneological preparations are well known to those skilled in various compositions and dosage forms since ancient times and the Middle Ages as components of a bath culture highly developed in many countries.
  • fundamental scientific findings and systematic studies on specific effects of balneological preparations such as cleansing, care or treatment of the skin, have only become available in recent decades.
  • cosmetic preparations such as creams or lotions, which can be applied to the skin in concentrated form and remain there for longer periods
  • balneological preparations are used by the bath or shower water in highly diluted form and the contact time on the Skin is relatively short during bathing or showering.
  • balneological preparations are usually offered in the form of concentrates in the prior art.
  • a special form of balneological preparations are premix concentrates which are designed so that the active balneological system is formed only after introduction into an excess of water.
  • DE 42 05 548 A1 describes, for example, certain stabilizing water-dispersible oil-soluble polyoxyethylated surfactants having an HLB value of 6 to 13 together with vesicle-forming agents such as phospholipids in an oil base as such a balneological preparation which forms bath liposomes after introduction into an excess of water. which have favorable skin-active balneological effects.
  • vesicle-forming agents such as phospholipids in an oil base as such a balneological preparation which forms bath liposomes after introduction into an excess of water. which have favorable skin-active balneological effects.
  • lipoproteins which are capable of binding and transporting lipids.
  • DE 103 24 256 A1 discloses proteins as a vehicle for lipids which catalyze effective lipid transport. In the process, energy barriers of lipid exchange are lowered and the transfer of lipophilic active substances in aqueous media is made possible or increased. Criticism of the prior art
  • balneological preparations which on the one hand contain the favorable properties of liposomal systems from premixes and on the other hand offer the advantage of catalytic drug delivery by lipoproteins.
  • balneological preparations in particular bath and shower preparations, which, after contact with an excess of water, develop skin-active protein-containing liposomal systems (nano-proteosomes) from premixes, which enable additional catalytic transport of the active substance.
  • balneological premix basic concentrates for the formation of proteo (lipo) somenae with lipophilic components, comprising 25 to 95% by weight of lipids selected from vegetable, animal or synthetic lipids or mixtures thereof, 0.1 to 15% by weight one or more liposome-forming substances selected from phospholipids, sphingolipids or mixtures thereof, 0.5 to 70 percent by weight of one or more surfactants, such as ethoxylated fatty alcohols, ethoxylated fatty acids, ethoxylated sugar esters or sugar ethers of fatty acids, fatty alcohol sulfates or their ethoxylated derivatives, 0.05 to 15% by weight of one or more proteins selected from vegetable proteins with a mean molecular mass of 4 kD to 30 kD, milk proteins with a mean molecular weight of 2.5 kD to 18 kD, quaternized milk proteins having an average molecular weight of 2.5 kD to 12 kD and optional
  • the liposome-forming component (s) such as phospholipids
  • the protein component or components of 10 to 1 to 1 to 1, especially 3 to 1 to 1 to 1 an equilibrium can be achieved, so that on the one hand the liposomal Vehicle structure and on the other hand, the protein-catalyzed Drug delivery can be used.
  • the liposome-forming component (s) such as phospholipids
  • an equilibrium can be achieved, so that on the one hand the liposomal Vehicle structure and on the other hand, the protein-catalyzed Drug delivery can be used.
  • the balneological preparations it is possible to obtain the proteoliposomal structures after dilution in the bathing bath or during the showering process. This also favors an increased drug delivery into the skin in the case of rinse-off applications, as is the rule with cosmetic leave-on applications.
  • FIGS. 1a, b and 2a, b show the improvement of the epidermal oxygen supply and the cutaneous microcirculation after bathing or showering with balneological preparations according to the invention of a corresponding base formulation as described in Examples 1 and 4, respectively.
  • FIG. 3 shows an electron micrograph of the formed proteoliposomal structures after entry of a balneological preparation according to the invention according to Example 2 into an excess of water.
  • the balneological preparations according to the invention contain as the first active ingredient one or more lipids which are selected in particular from vegetable oils or mixtures of vegetable oils with glycerides or fatty acid esters, fatty alcohols, fatty acids or optionally also with hydrocarbons such as paraffins.
  • These include, in particular, olive oil, sunflower oil, soya oil, rapeseed oil, peach kernel oil, apricot kernel oil, grape seed oil, castor oil, peanut oil, almond oil, wheat germ oil, sesame oil, thistle oil, avocado oil, shea butter, illipe butter, coconut oil, borage oil, corn oil, Walnut oil, palm oil, macadamia nut oil, palm kernel oil, hazelnut oil, rose hip kernel oil, cottonseed oil, papaya oil, rosewood oil, rosemary oil, eucalyptus oil, thyme oil, pine needle oil, cardamom oil, turpentine oil, jojoba oil or its substitute oleyl erucate.
  • Particularly preferred vegetable oils are soybean oil, sunflower oil, wheat germ oil, almond oil, olive oil or mixtures thereof.
  • Liposome-forming component is soybean oil, sunflower oil, wheat germ oil, almond oil, olive oil or mixtures thereof.
  • liposome-forming components are particularly suitable phospholipids, e.g. Egg, soya, oilseed rape, cottonseed, such as phosphatidylcholine from soy or yolk, mixtures with phosphatidylcholine in various ratios, such as NAT products, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol from soy, yolk, rape, cottonseed, lecithin from soya, egg yolk, rapeseed, cottonseed.
  • phospholipids e.g. Egg, soya, oilseed rape, cottonseed
  • phosphatidylcholine from soy or yolk mixtures with phosphatidylcholine in various ratios, such as NAT products, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol from soy, yolk, rape, cottonseed, lecithin from soya
  • sphingolipids such as ceramides, cerebrosides, spingomyelin, etc.
  • the total proportion of liposome-forming components is above all 0.2 to 10 percent by weight, in particular 0.4 to 5 percent by weight, preferably 1 to 3 percent by weight ,
  • protein (s) or, depending on the molecular mass, protein hydrolyzates vegetable proteins, such as those from cereals, seafood, milk, are used according to the invention.
  • Wheat, oats, soya, buckwheat, tapioca, corn, barley, rice, beans, millet, spelled, or mixtures thereof are preferred cereals.
  • the proteins or hydrolyzates have an average molecular weight of 4000 to 30,000 D 1, preferably> 10,000 D to 30,000 D, especially 11,000 D to 25,000 D.
  • the average molecular weight of the plants, especially cereal proteins e.g.
  • Oat, wheat, barley, soy between 4000 and 9900 D, in other embodiments between> 10000 D to 25000 D, preferably to 19000 D.
  • rice, bean or sugar Corn, millet, soy wheat oat protein, or mixtures thereof, or rice, bean or corn, millet, soy wheat oat protein with an average molecular weight of 12,500 to 18,000 D in particular also mixtures of soybean and oat protein, soybean and corn protein, barley and millet protein, in the ratio 1: 1 to 1: 5.
  • those having an average molecular weight of 25,000 to 45,000 D are especially 41,000 D to 45,000 D.
  • animal proteins or protein hydrolysates such as those from milk with an average molecular weight of 2500 D to 18000 D, especially 2500 to 8500 D, or even 2500 to 3500 D, or in other embodiments also especially 9000 to 15000 D, in particular 9000 to 12000 D.
  • animal proteins or protein hydrolysates such as those from milk with an average molecular weight of 2500 D to 18000 D, especially 2500 to 8500 D, or even 2500 to 3500 D, or in other embodiments also especially 9000 to 15000 D, in particular 9000 to 12000 D.
  • quaternized milk proteins or hydrolyzates thereof such as cocodimium hydroxypropyl milk protein.
  • Preferred proteins are plant proteins, in particular selected from the abovementioned cereal proteins or mixtures thereof.
  • the proteins or hydrolyzates to be used according to the invention can be prepared from the starting materials by suspension in water, if appropriate, reaction with acids or bases, further workup such as centrifugation, optionally separation of accompanying substances by precipitation z. For example, with acid, salts (such as ammonium sulfate), degreasing with organic solvents, purification by dialysis, gel filtration, chromatography, etc. are obtained. Processes for this purpose are known in the prior art and described, for example, in DE 38 15 473 C1, see also US Pat. No. 5,777,640, US Pat. No. 6,077,529.
  • the amount of protein (s) is preferably 0.2 to 15% by weight, in particular 0.2 to 4% by weight, especially 0.3 to 1.1% by weight.
  • Particularly preferred proteins or protein hydrolysates can be selected from plant proteins (average molecular mass, for example, 4500 to 9000 D, or especially 11000 to 23000 D), especially from oats, soybeans, buckwheat, rice, millet; or mixtures thereof; Milk protein (average molecular weight 2500 to 3500, in particular 9500 to 15000 D), quaternised milk protein or mixtures thereof, such as mixtures of plant or mixtures of plant and milk proteins such as: buckwheat / oats; Oats / millet; Rice / milk; Buckwheat / milk; Oats / milk, oats / quaternized milk protein with the respectively indicated, in particular the particularly preferred molecular masses.
  • surfactants are examples of surfactants:
  • Particularly suitable surfactants are sugar esters or sugar ethers of glucose, sucrose, methylglucose of C 2 -C 8 saturated, unsaturated, partially saturated fatty acids; or polyoxyethylated and / or medium-polyoxypropylated telkettigen and higher-chain (C 2 -C 22 -) fatty acids (esters); or of C 8 -C 20 saturated, unsaturated, partially saturated or such polyoxyethylated and / or polyoxypropylated fatty alcohols (ethers).
  • the EO (PEG products) or PO (PPG products) degree may be between 8 and 40, preferably 8-25. It is also possible to use mixed polyoxylated products.
  • Particularly suitable sugars are glucose, sucrose, methyl glucose.
  • fatty acids or fatty alcohols are especially organic aliphatic Ci 2 -Ci 8 .
  • Known oxylated (ethoxylated, propoxylated, mixed-alkoxylated) sugar surfactants are, for. PEG-20 methyl glucose sesquistearate, PEG-120 methyl glycose dioleate or methyl gluceth-10, methyl gluceth-20, PPG-10 methyl glucose ether, PPG-20 methyl glucose ether.
  • sucrose palmitate / stearate methyl glucose stearate, decyl glucoside and mixtures thereof.
  • fatty acid or fatty alcohol nonionic surfactants such as nonionic ethoxylated and / or propoxylated fatty alcohols (fatty alcohol ethers), nonionic ethoxylated and / or propoxylated fatty acids (esters) or their amides such as.
  • B. mono- or diethanolamides are used, wherein the fatty alcohol or the fatty acid has a chain length C 8 to C 20 , or Ci 2 to C 22 ; especially Ci 2 to Ci 8 has.
  • Ci-C 8 - alkyl-Cio-Ci 8 fatty alcohol ethoxylates such as polyoxyethylene (1 to 4 EO, Laureth 1-4), polyoxyethylene (5) - oleyl ether, polyoxyethylene (7) palmitylether, polyoxyethylene (15) stearyl.
  • Such surfactants preferably have an HLB value of 6 to 16; preferably 7-13 (alone or mixed).
  • anionic fatty alcohol surfactant derivatives in particular in combination with nonionic surfactants, such as the abovementioned fatty acid or fatty alcohol derivatives (ethoxylated or propoxylated, preferably ethoxylated derivatives) or nonionic fatty acid amides.
  • Suitable anilines ontensid- Fettalkoholdrivaten mainly include Ce to C20, especially C1 0 to Ci 8 fatty alcohol sulfates or sulfate salts, such as amine salts, in particular Monoisopro- panolamin- sulfate salts, optionally ethoxylated derivatives thereof with a degree of EO 0 to 4, especially 1-4. These include z.
  • MIPA laureth sulfate dioisopropanolamine (E01-4) lauryl sulfate.
  • surfactants selected from ethoxylated C 10 to C 20 fatty alcohols, ethoxylated C 12 to C 20 fatty acids having an EO or PO degree of 1 to 5, especially 1 to 4; or C 2 to C 20 - fatty acid amides hereof, in particular mono- or diethanolamides or mixtures thereof or mixtures with anionic fatty alcohol sulfate salts, z.
  • the nonionic surfactants may be mixtures of said fatty alcohol or fatty acid derivatives (in particular the abovementioned ethoxylated) and the abovementioned fatty acid amides, in particular ethoxylated products, for. B. in the ratio 2: 1 to 1: 2.
  • surfactant at least one surfactant selected from the group comprising ethoxylated and / or propoxylated C 10 to C 2 o fatty alcohols, ethoxylated and / or propoxylated C 12 to C 2 o fatty acids with an EP or PO or EO_PO grade from 1-5, CI 0 to C 20 - (optionally ethoxylated) fatty alcohol (ether) sulfate salts - sulphate monoisopropanolamines having an EO degree of 0.4; or mixtures.
  • the surfactants may be present in amounts of preferably from 4 to 65%, especially from 8 to 65% by weight, especially from 10 to 65% by weight.
  • a higher or lower amount of surfactant such as B. 8-20% by weight to achieve a proteoliposomal oil bathing effect, or z. B. 40 to 65 wt.%, In particular 57 to 63 wt% surfactant content, to achieve a proteoliposomal Schaumbadeskyes.
  • additives in total, for example, in an amount of 0 to 30%, especially 0.01-30%, especially 0.01 to 20%, especially also 0.1 to 15% by weight or 1 to 10 wt .%
  • conventional active ingredients such as khaki strictn, mango, figs, lavender oil, cedar, lotus, chamomile flowers, ylang ylang, gingko, pine needle, cypress, birch leaf extract, aloe Vera extract, marigold, hibiscus, burdock root witch hazel, aquamarine, algae, quince, water lily, cinnamon extract, thyme, mint, lime, orange, grapefruit, mandarin, juniper, valerian, lemon balm extract, Eucalyptus, thyme, palmarosa, rosemary, lavender, rosewood, lemongrass, wild rose, spruce needle, pine needle, ginger, currant, lime blossom, marigold, magnolia, pineapple, guava, echin
  • extracts are prepared in a known manner, such as by steam distillation. This results in e.g. get essential oils from the said plants, which are particularly preferred.
  • the extracts may also be e.g. obtained by solvent extraction (with alcohols, triglycerides or hydrocarbons, water, mixtures thereof) and then used as such.
  • Examples of analogously synthesized substances are terpenes and terpenoids, such as camphor, menthol, cineol or mixtures thereof.
  • agents may, for.
  • vitamins such as vitamin A 1 E, or other or suitable derivatives thereof such as esters such as palmitate, acetate or phosphate.
  • Other agents are z.
  • Nicotinic acid derivatives such as methyl or tocopheryl nicotinate, alpha- and Betahydroxys ⁇ ren and their derivatives, eg. As glycolic, malic, citric, tartaric, lactic acid, salicylic acid, isopropylbenzyl salicylates, C12-13 alkyl lactates (Cosmacol ® ELI) or anti-inflammatory and antibacterial substances such as triterpenes, z.
  • Stearyl glycyrrhetinates potassium glycyrrhinate; Pantothenic acid derivatives, e.g. As D-panthenol, panthenyl triacetate or polyphenols, flavonoids, z.
  • Pantothenic acid derivatives e.g. As D-panthenol, panthenyl triacetate or polyphenols, flavonoids, z.
  • rutin ferulic acid and their esters or isoflavones such as soy isoflavones or coenzyme Q 10 can be used.
  • Preferred active ingredients are selected from essential oils, plant extracts, vitamins or mixtures thereof, in particular also mixtures thereof with glycerol or solvents such as ethanol.
  • suitable additives can be selected from conditioning agents, preservatives, dyes, perfumes, care substances or mixtures thereof. These may be present in particular in amounts of 0.01 to 8%, preferably 0.1 to 5%.
  • conditioning agents in suitable amounts include, for example, acrylamides (polyacrylamide or polyacrylamide-containing mixtures), starch such as hypromellose or starch glycola, rice, wheat, corn and potato starch, as well as hydrophobically modified starches, and the like. Furthermore, polysaccharides (for example xanthan gum) or silicates such as magnesium aluminum silicate may also be mentioned here. As conditioning agents, it is also possible to use granular Plextruckner such as EDTA Na-SaIz, means for pH adjustment, eg citric acid, sodium hydroxide, solvents such as propylene glycol, ethanol, glycerol, polyethylene glycol such. B. PEG 400 u. ⁇ ., Polypropylene glycol, salts such as NaCl, or mixtures thereof. Further conditioning agents are in particular mono- and dialkyl phosphates or glyceryl stearate, optionally colloids.
  • humectants such as glycerol, propylene glycol or polyethylene glycols, polypropylene glycol, butylene glycol, sorbitol or polymers, e.g. Polyquaternium types such as Polyquaternium -39, collagen or its hydrolysates, amino acids, urea, polysaccharides, or commercial humectants such as inositol, sodium lactate, DL-2-pyrrolidone-5-carboxylic acid, Na salt.
  • humectants such as glycerol, propylene glycol or polyethylene glycols, polypropylene glycol, butylene glycol, sorbitol or polymers, e.g. Polyquaternium types such as Polyquaternium -39, collagen or its hydrolysates, amino acids, urea, polysaccharides, or commercial humectants such as inositol, sodium lactate, DL-2-pyrrolidone-5-car
  • Coloring and preservatives are known in the art for such products and are selected in particular from water-soluble products.
  • premix bases described above can be used as such (premix
  • Concentrates such as bath oils, shower concentrates with lipid or high lipid content, also as indication products such as sports shower concentrate, relaxation oil bath, refreshment shower / bath, etc.) are used.
  • solid baths such as bath tablets, bath pearls may be prepared from the premix concentrates using suitable formulatory agents.
  • suitable solvents in particular water, dilute products such as cream baths, creamed foam baths, cream showers or foam showers are obtained.
  • from the above concentrates z.
  • one or more galenic adjuvants selected from solid builders, tabletting agents, solid gas / foam generators, salt crystals, organic pellets or liquid solvents especially water, galenic preparations are obtained.
  • Suitable galenic formulation agents are z.
  • salts such as sodium chloride, sodium carbonate / bicarbonate, calcium magnesium carbonate / bicarbonate (so-called CO 2 generators for effervescent tablets or powders) or colloids, especially organic, for pearls; furthermore also tableting agents, explosives, colloidal auxiliaries for solid forms.
  • auxiliaries are known to the person skilled in the art.
  • Solvents are especially selected from water or water mixed with compatible organic solvents.
  • Lipid-rich cream baths or lipid-containing foam baths Lipid-rich cream baths or lipid-containing foam baths:
  • lipid 8-35% lipid (cream shower), 25-62% lipid (lipid-rich foam shower), 5-25% lipids (lipid-containing foam shower); 0.2 to 8% transfer protein proteins; 0.2 to 8% liposome-forming substance; 15 to 59% surfactants; Remainder if available additives (especially active ingredients).
  • Preferred concentrate preparations comprise the following combinations: Balneological preparations comprising 25 to 95% lipids, especially 25 to 50% by weight, in particular 25 to 30% by weight; or even 70 to 90 wt% and selected from vegetable lipids, 2 C1 - 22 fatty acid glycerides, C 2 - ⁇ -C12 alcohol - 22 - Fettklareestern, C ⁇ - 22 fatty alcohols or mixtures thereof.
  • one or more liposome-forming substances selected from phospholipids, especially lecithins, and sphingolipids, especially sphingosine; or mixtures thereof; 5 to 65% by weight, especially 5 to 65% by weight or else 57 to 65% by weight or 5 to 15% by weight (in each case in correlation with the above-mentioned corresponding lipid content) of one or more surfactants selected from polyoxyethylated and / or Ce polyoxyproyl believing -C ⁇ oFett alcohols, polyoxyethylenated and / or polyoxyproyl believing C 12 -C ⁇ fatty acids having an EO / PO ratio of 1-4, optionally ethoxylated C 8 -C 22 fatty acid amides; optionally anionic ethoxylated C 8 -C 2 oFett- acid alcohol sulfate salts, or mixtures thereof; 0.5 to 3% by weight of one or more proteins, from
  • the amount of water is less than 5% by weight, in particular less than 1% by weight.
  • the protein (s) is / are cereal protein (s) selected from rice, bean or corn, millet, soybean wheat oat protein or hydrolyzates having a mean molecular weight of 11,000 - 19000 D or mixtures thereof; or milk protein having an average molecular weight of 8500 to 15000 D; or a mixture of said milk protein with one or more of said grain protein (s), e.g. B. in a total amount of 0.1 to 3 wt.%, Preferably 0.5 to 1.5 wt.% "Exists.
  • Preparations are also suitable in which one or more plant proteins, in particular one or more cereal proteins (for example rice, bean or maize, millet, soya wheat oat protein or hydrolyzates), having an average molecular mass of 11000 D to 25000 D in a mixture with quaternised milk protein having an average molecular weight of 2500, especially 4000 to 12000 D, z. B. in a total amount of 0.1 to 3 wt.%, Preferably 0.5 to 1, 5 wt.%, Is contained.
  • cereal proteins for example rice, bean or maize, millet, soya wheat oat protein or hydrolyzates
  • a further advantageous embodiment comprises preparations in which as protein (e) one or more plant proteins, in particular rice, bean or maize, millet, soy wheat oat protein or hydrolyzates having an average molecular weight of 4000 to 9500 D. , or mixtures thereof, or milk protein or quaternized milk protein, having an average molecular weight of 2500 to 3500 or 8500 to 15000 D, or mixtures of said milk protein or quaternised milk protein, with one or more of said grain proteins.
  • protein e
  • plant proteins in particular rice, bean or maize, millet, soy wheat oat protein or hydrolyzates having an average molecular weight of 4000 to 9500 D. , or mixtures thereof, or milk protein or quaternized milk protein, having an average molecular weight of 2500 to 3500 or 8500 to 15000 D, or mixtures of said milk protein or quaternised milk protein, with one or more of said grain proteins.
  • Particularly suitable as plant lipids in preparations according to the invention are jojoba oil, almond oil, soybean oil, sunflower oil, olive oil or mixtures thereof or with caprylic-capric triglyceride, glyceryl stearate.
  • the protein or proteins are preferably present in a (total) amount of from 0.5 to 3, especially up to 1.5,% by weight.
  • surfactant or surfactants are selected from polyoxyethylated Zuckerestern of and / or polyoxypropylated (Ce -C 18 -) fatty acids (esters); Sugar ethers of polyoxyethylated and / or polyoxypropylated C 8 -C 20 fatty alcohols having a PO or EO degree 3 and 16, in particular 4-8.
  • Ciobis Ci ⁇ fatty alcohols ethoxylated and / or propoxylated C 12 to C 16 fatty acids, each having an EO or PO degree from 1 to 5, especially 2 to 4; Ci 2 to Ci 8 - fatty acid amides, or mixtures thereof.
  • anionic optionally ethoxylated C 8 to C 2 o fatty alcohols - sulfate salts such as amine salts, especially substituted amine salts such as mono / diethanolamine / Monoisopropylamin- especially salts; in particular in combination with nonionic ethoxylated C 8 to C 20 fatty alcohol ethers, (ethoxylated) or C 12 to C 20 fatty acid amides, or mixtures of the latter two.
  • the weight ratio of liposome-forming substance (s) to protein (s) is 1: 1 to 5: 1, in particular 2.5: 1 to 1.3: 1.
  • 0.1 to 20 especially up to 18, wt.%, In particular 0.1 to 10 wt.%
  • Additives selected from active ingredients, consistency regulators, care agents, preservatives, dyes, perfume or mixtures thereof contain.
  • Particularly preferred active ingredients are essential oils, plant extracts, vitamins or mixtures thereof.
  • balneologi- rule preparations of the invention comprise 75 to 90 wt% lipids, selected from vegetable Lipi- to, C. 12 - 22 fatty acid glycerides, C 2 - C 6 alcohol ⁇ - Fettklareestern, C ⁇ -22 - Fatty alcohols or mixtures thereof, in particular selected from jojoba oil, caprylic capric triglyceride, glyceryl stearate, soybean oil, sunflower linolenic acid, olive oil, or mixtures thereof, furthermore 5-10% by weight of surfactants selected from ethoxylated and / or propoxylated C 8 to C 20 Fatty alcohols or sulfate salts thereof, ethoxylated and / or propoxylated C 12 to C 22 fatty acids, having an EO or PO or EO-PO degree of from 1 to 5, especially 1 to 4; or mixtures thereof, C 12 to C 22 fatty acid amides, or mixtures thereof; 2 to 4% by weight of one
  • cereal proteins such as oats, soybeans, wheat, buckwheat (average molecular mass, for example, 4000-9500 D), milk protein (2500-8000 D), or mixtures thereof (oat / soybean, buckwheat / soybean / oat Buckwheat / milk; oats / wheat / milk).
  • balneological preparations which have the following components:
  • vegetable oils preferably selected from soybean oil, wheat germ oil, especially in admixture with C12-22 triglycerides,
  • lecithin soya egg lecithin
  • sphingosine or mixtures thereof.
  • 0.5 to 1.5% protein component in particular selected from wheat protein (hydrolyzate), MW 11000-19000 D, oat protein (hydrolyzate) (MW 11500-20000 D), barley protein (hydrolyzate) (MW 11000 to 21000 D), Milk protein (hydrolyzate) (MW 9000 to 15000 D), quaternised milk protein (Z: b: 4000 to 12000 D), MW or mixtures of such proteins, such as wheat milk; Barley + oats; Milk + oats;
  • additives selected from consistency regulators; Conditioners, dyes, perfumes, preservatives; Active ingredients, such as. As essential oils, plant extracts, vitamins.
  • balneological premix preparations are provided with the following components:
  • lipids selected from vegetable lipids, C1. 2 - 22 fatty acid glycerides, C 2 -6-C12 alcohol 2 2 fatty acid esters, fatty alcohols or mixtures C ⁇ - thereof 22, further
  • surfactants selected from ethoxylated and / or propoxylated C 8 to C 2 o fatty alcohols or their sulfate salts, ethoxylated and / or propoxylated C 12 to C 22 fatty acids having an EO or PO degree of 1 to 5, especially 1 to 4 (wherein EO derivatives are preferred), C 12 to C 22 - fatty acid amides, optionally anionic ethoxylated (0-4 EO) C 8 to C 2 o fatty alcohol sulphate salts, especially Sulfatmonoisopropanolaminen; or mixtures of such surfactants; 1 to 4% by weight of one or more phospholipids such as lecithins; Sphinolipids or mixtures thereof; 0.05 to 3 wt.% Of one or more proteins or protein hydrolysates selected from rice, bean or corn, millet, soy wheat oat protein with an average molecular weight of (each) 11000 to 19000 D,
  • Fatty acid amides one or more Ci to Ci 0 8 - - (optionally ethoxylated.)
  • Fatty alcohol are preferably used in such preparations as a surfactant one or more ethoxylated C 10 to C 8 - one or more C 2 to C 18 fatty alcohols, (ether) sulfate salts, especially sulfate monoisopropanolamines; or mixtures of said oxylated fatty alcohol (s), fatty acid amide (s) and said fatty alcohol sulfate salt (s).
  • the preparation concentrates are prepared by mixing the lipid (s) with the surfactant (s), by stirring, and subsequently adding the liposome-forming substance together with optionally present (temperature-stable) additives, if appropriate at elevated temperature, eg. B. mixed to 56 ° C and then at room temperature, the protein (s) and, if present, temperature-labile additives by stirring u. ⁇ . incorporated.
  • optionally present (temperature-stable) additives if appropriate at elevated temperature, eg. B. mixed to 56 ° C and then at room temperature, the protein (s) and, if present, temperature-labile additives by stirring u. ⁇ . incorporated.
  • the preparations of the invention are designed especially for the balneo-cosmetic application, z. B. as a relaxation aroma refreshing skin care bath (oil bath), foot bath, oil bath, or shower room u. ⁇ .
  • the corresponding active ingredients can be transported very effectively, as can be seen from Figures 1a, b and 2a, b.
  • indication baths such as rheumatism bath, detoxification bath, cold bath and, relaxation bath, refreshing bath / shower.
  • Particularly suitable for this purpose are the concentrates or the solid preparations such as salts.
  • dilute preparations can also be used.
  • balneological concentrates Examples 1 to 4, Table 1
  • galenic preparations thereof Tables 2 to 4, Examples 5 to 22
  • Table 1 Liquid Bath Concentrates with Proteosomes
  • a bath concentrate (Verum 2, Example 23) (Skin Tightening Bath Concentrate) analogously to Example 12, comprising 25% water and 75% of the concentrate according to Example 1 with the following modifications * with respect to the lipids or replacement of the active ingredients and additives as follows: Paraffin oil: 25%, soybean oil: 24%; 5% rosemary oil, 6% pine needle oil, 1, 5% ivy leaf extract, 1, 5% niacin, 0.5% tocopheryl acetate, 1, 5% methyl nicotinate were tested. After the procedure according to E. Nuremberg, T.
  • a preparation (skin tightening shower concentrate) (Verum 2, Example 24) according to Example 18, with 46% water and 54% concentrate according to Example 4 with the following modifications * with regard to the lipids, proteins or replacement of the additives / active ingredients as indicated : 22% glycerol monostearate, 0.5% wheat protein hydrolyzate as indicated; 30% Laureth-3; 3% rosemary, 1% tocopheryl nicotinate, 1.5% ivy leaf extract, 3% pine needle oil, 1% niacin, 1.5% methyl nicotinylate, 3% exfoliating body (without perfume dye) were tested.
  • the epidermal oxygen supply was determined by polarographic measurement of the oxygen partial pressure (platinum electrode) and determination of the measurement current produced as a result of dermal O 2 diffusion by the O 2 reduction carried out at the electrode.
  • a, b the respective result (Verum 2) in comparison to water and the analogous preparation, without protein (Verum 1) is shown. As can be seen, carried out with the application according to Verum preparation 2 an unexpected improvement over Verum 1.
  • Variations means: Change in the amount of the specified component while retaining the remaining (not listed) components of the respective substance group - in the area set for replacement.
  • a preparation according to Example 2 was introduced into a bathing liquor (in an amount of more than 100 times as much water) and the forming structure (TEM image) was determined by electron microscopy.
  • the recording according to Fig. 3 shows the case surprisingly trained multi-layer structures.

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Abstract

L'invention concerne des préparations balnéologiques, en particulier des préparations pour le bain et la douche, qui sous forme de concentrés prémélangés coulants ou liquides présentent des constituants formant des liposomes tels que des phospholipides en plus de lipides naturels et/ou synthétiques et qui sont également disponibles sous forme de mélanges comprenant principalement des protéines végétales, des tensio-actifs et éventuellement des additifs. En contact avec un excès d'eau, ces systèmes stables forment directement des protéoliposomes à activité catalytique agissant sur la peau pour un meilleur transport des principes actifs dans la peau. Ils peuvent être mis en oeuvre directement ou sous des formes galéniques solides ou diluées (notamment préparation lipidique pour la douche contenant des protéasomes, poudre pour le bain contenant des protéasomes).
EP10732867A 2009-07-15 2010-07-07 Concentrés liquides ou fluides pour le bain ou la douche formant des protéasomes, formes galéniques de ces concentrés et leur utilisation Withdrawn EP2453868A2 (fr)

Applications Claiming Priority (2)

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DE102009033109A DE102009033109A1 (de) 2009-07-15 2009-07-15 Flüssige oder fließfähige proteosomenbildende Bade- und Dusch-Konzentrate, galenische Anwendungsprodukte hiervon und deren Verwendung
PCT/EP2010/004142 WO2011006616A2 (fr) 2009-07-15 2010-07-07 Concentrés liquides ou fluides pour le bain ou la douche formant des protéasomes, formes galéniques de ces concentrés et leur utilisation

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DE102010054461A1 (de) * 2010-12-14 2012-06-14 Merz Pharma Gmbh & Co. Kgaa Liposomenbildende wässrige Badezubereitungen mit hohem Wirkstoffanteil und deren kosmetische / dermatologische / medizinische Anwendung
US8859549B2 (en) 2011-05-13 2014-10-14 Abbvie, Inc. Potassium channel modulators
DE102012007734A1 (de) 2012-04-18 2013-10-24 Merz Pharma Gmbh & Co. Kgaa Stabile, einfach aus 2 Phasen herstellbare feste Ölbadesalzzubereitungen mit anwendungsbezogener Einsatzflexibilität
EP2671615A1 (fr) 2012-06-05 2013-12-11 Merz Pharma GmbH & Co. KGaA Additif solide de bain avec un profil de dissémination visuel et olfactoric à l'effect retardé
DE202012005506U1 (de) 2012-06-05 2012-08-28 Merz Pharma Gmbh & Co. Kgaa Fester Badezusatz mit retardiertem olfaktorischem und visuellem Freisetzungswirkungsprofil
CN104768523B (zh) 2012-10-29 2017-08-15 宝洁公司 10℃下具有0.30或更大损耗角正切值的个人护理组合物
EP2808059A1 (fr) 2013-05-29 2014-12-03 Merz Pharma GmbH & Co. KGaA Additif de bain comprenant 2 composants avec un delai de liberation retardee d'un colorant dependant de la matrice
WO2018008235A1 (fr) * 2016-07-07 2018-01-11 パナソニックＩｐマネジメント株式会社 Dispositif de traitement de l'eau
RU2732128C1 (ru) * 2020-01-10 2020-09-11 Цзинь, Гэ Состав для приготовления изоосмотических ванн для детоксикации и восстановления жизненных функций организма человека

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WO2011006616A2 (fr) 2011-01-20
US20120101172A1 (en) 2012-04-26
DE102009033109A1 (de) 2011-02-03
RU2012105276A (ru) 2013-11-20

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