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    • 专利摘要:
    A topical cosmetic agent is provided for use in preventing hair graying and / or caring for hair that has recovered in color and / or for returning gray hair to its original hair color, comprising melatonin and optionally at least one first cosmetically active substance, the conjugated double bonds contains and at least one other cosmetically active substance.
    公开号:CH716867A2
    申请号:CH01482/20
    申请日:2020-11-20
    公开日:2021-05-31
    发明作者:Karrer Lukas
    申请人:Karrer Lukas；
    IPC主号:
    专利说明:

    The invention relates to the use of topical cosmetic preparations, in particular care products, against graying hair, for the care of grayed hair and for returning grayed hair to the original hair color, the preparations melatonin and at least one first and at least one further cosmetically active substance include. It preferably relates to the additional use of other substances in combination with melatonin, in particular of polyunsaturated fatty acids with conjugated double bonds and their derivatives for the production of cosmetic care products that prevent graying of the hair, to return grayed hair to its original color, to strengthen the hair, in particular for hair that has recovered in color and for protection against the effects of UV light and against hair loss.
    State of the art
    Melatonin is an endogenous hormone that is responsible for the human circadian rhythm. However, it has also been shown that melatonin can be used to care for the skin and to prevent hair loss, see CA1292947, or as an antioxidant, see WO2007 / 099172, in the form of a topical preparation. Melatonin is available inexpensively. In addition, apart from a moderate tendency to initiate the sleep cycle, it is largely free of side effects. US4746674 describes that after a treatment with melatonin, the hair pigmentation does not appear to be affected and the hair retains its color.
    It is also known (Fischer et al. Abstract P19 in EHRS Conference Marburg, 2000) that melatonin has different effects with regard to cell proliferation. It has been shown to both inhibit and stimulate keratinocyte proliferation. The influence of melatonin on the length and proliferation of hair follicles was investigated. Melatonin inhibited hair growth compared to the control at concentrations of 1 to 3 mmol. In contrast, 30 µmol melatonin resulted in increased growth compared to the control over the first 2 days. Melatonin and its antagonist 4-PDOT (30 µmol each) lead to a significant inhibition of hair follicle growth over 6 days. Melatonin therefore has a strong dose-dependent effect on the inhibition or promotion of hair follicle growth.
    Graying of hair is essentially pigment loss and is not just an aesthetic problem. The lack of pigment in the hair also reduces the UV shielding to the scalp. Particularly at an advanced age, when the hair is thinning, the UV protection provided by the hair decreases and the risk of malignant skin changes increases. It is therefore desirable to stop or delay this physiological process.
    The graying could be countered by coloring the hair. The disadvantage of treating hair with hair dyes, however, is that the effects are only temporary and usually do not have the same effect in terms of appearance as natural hair. Often, hair dyes also degrade the quality of the hair because they are mixed with oxidizing agents or reducing agents.
    The pigments of the hair are the so-called melanins, which are produced in the melanocytes. Melanocytes are found in the basal layer of the epidermis and in the hair follicles. The pigment produced is generically called melanin and is phenotypically determined. Melanins are complex polymer compounds derived from tyrosine and levodopa on the one hand and cysteine on the other. The biosynthetic route takes place with eumelanin, the essentially black pigment, starting from tyrosine via dopa to dopaquinone via the intermediate indolquinone, which is polymerized to eumelanin, including further reactions with proteins etc. to the target pigment. In the biosynthesis of pheomelanin, the red pigment, cysteine is involved in the production of dopaquinone, whereby cysteine dopa is formed, which is then polymerized by oxidation and at the same time or subsequently built up with proteins, peptides, etc. to form the target pigment. The essential enzyme involved in this biosynthesis is tyrosinase. Tyrosinase is an enzyme that contains copper, which the body produces to a greater extent, for example when there is increased UVB radiation. The pigment production is increased for a protective reaction of the body against the radiation.
    Classical studies have shown that the cessation of pigment production and therefore the graying of the hair is an age-related process that cannot be treated with medication, see Herzberg and Gusek Arch. exp. Derm. 236, 368-384 (1970). Nevertheless, in the past there have been reports of preparations that can at least delay the graying process. The reasons for this are discussed in different ways. The basis of an interpretation for these results, which contradict the classical view, is usually the complexity of the actual processes involved in pigment formation, which should not only be limited to the action of the tyrosinase. Thus, blood circulation-promoting agents, mostly vasodilatory plant extracts, agonists or antagonists for the enzymes, hormones and their receptors and antioxidants involved in the melanin formation process are proposed as radical scavengers. Due to the extremely complex pathology of the hair-pigment-producing apparatus, also with the most varied of phenotypes and accompanying conditions as well as their medications, it is not surprising that unconventional approaches have often led to the goal, the actual effect of which, if at all, was only understood much later .
    Main hair and body hair are subject to a cycle. This cycle includes a growth phase (anagen phase), a degenerative phase (catagen phase) and a resting phase (telogen phase), after which a new anagen phase develops. Because of this hair cycle and in contrast to the epidermal pigmentation unit, the follicular pigmentation unit must also be renewed cyclically.
    Melanocytes are involved in these pigmentation processes of the skin and / or skin appendages.
    Hair and skin pigment show some morphological differences. The pigment granules of the hair are larger, do not occur in melanosome complexes, are also localized in individual cells and reveal two forms that are characteristic of black and blonde hair and basically correspond to eumelanin and / or pheomelanin.
    The melanin pigment thus determines the hair color and is synthesized from tyrosine biochemically by the melanosome in melanocytes, which are present in the upper region of the matrix cell and supply the hair.
    In the course of life, melanocytes are still produced, but increasingly no longer produce melanin. This process can be continuous or intermittent.
    Melanin synthesis begins, it is believed, in the cisterns of the endoplasmic beticulum or in the Golgi apparatus. From these membrane systems approx. 0.05 µm large vesicles constrict, which slowly become larger, take on more elongated shapes and later have inner membranes. These premelanosomes can also be detected in amelanotic melanocytes, e.g. in albinism. They are usually 0.25 X 0.08 µm in size. The melanin is said to be deposited in the form of small granules on the inner membranes of the premelanosomes.
    Where exactly the melanin monomer is formed is not yet completely clear. In part, the endoplasmic reticulum, on the other hand, the (pre-) - melanosomes themselves are made responsible for it. The mitochondria tend not to be involved in melanin synthesis. The premelanosomes are converted into melanosomes by the deposited melanin, which have a finely grained, longitudinal or transverse striate internal structure. Further melanin storage and polymerisation of the melanin monomer within the melanosomes result in the mature, almost homogeneous melanin granules. The individual melanin granules of epidermal melanocytes are usually 0.45-0.7 × 0.45-0.3 µm in size in Europeans. How the melanin granules are smuggled from the melanocytes into the keratinocytes is not yet known in detail. There they are usually detectable in groups as melanosome complexes. It is possible that parts of the melanodendrites are phagocytosed by the keratinocytes. The melanosome complexes of normal and pathologically altered skin are extremely polymorphic, but show no significant qualitative differences.
    It has been shown that during the telogen-anagen transition, some of the inactive melanocytes contained in the telogen capsule multiply, arrange themselves around the dermal papilla of the nascent bulb and begin to express enzymes that are responsible for the synthesis of melanins are required. This population of melanocytes corresponds to the active melanocytes of the globe. At the same time, the other part of the melanocytes in the uppermost region of the hair follicle remains inactive. This population of melanocytes corresponds to the silent melanocytes of the uppermost region of the hair follicle.
    It has been shown that the enzyme dopachrome tautomerase (DCT), which converts dopachrome to 5,6-dihydroxyindole-2-carboxylate (DHICA), is involved in the synthesis of melanin. This reaction step is part of one of two metabolic pathways for the production of the pigment melanin. Mutations in the DCT gene can affect hair color. DCT is similar to tyrosinase and DHICA oxidase, but instead of copper it has two zinc atoms as a catalytic center. DCT is over-dominant in Europeans. DCT is not only a marker for melanoblasts, but it also regulates the sprouting of neuronal progenitor cells.
    Black hair contains approximately 0.35-1.0 μm oval granules with a homogeneous internal structure (type A, eumelanin). Blonde hair, on the other hand, has smaller, approx. 0.2-0.7 µm, more elongated granules with a layered internal structure (type B, pheomelanin). The hair color (black or blonde) depends on the type of pigment granules it contains. The color intensity, on the other hand, (brown, brownish, dark or light blond) is determined by the number of pigment granules.
    There are some similarities between the immature black hair pigment granules and the mature blonde hair pigment granules. However, there are some arguments against the assumption that the blonde pigment is only a preliminary stage of the black.
    The pigment of blonde hair is constructed differently in some respects than the pigment of black hair.
    The pigment of the hair differs in morphological terms from the pigment of the skin. The melanin granules in the cortex of mature human hair are larger than the epidermal ones, occur not only intracellularly but occasionally also extracellularly and finally occur individually or in groups, but not in melanosome complexes, as in the cells of the Stratum Malpighi. Furthermore, the pigment granules of black and blonde hair show clear structural differences that are apparently not present between light and dark pigmented skin.
    It is known that the “black” pigment also appears layered during its ripening, in a similar way to the “blonde” pigment. However, when fully developed, there are very noticeable structural differences.
    In mature hair, pigment granules occur only in the cortex. The cuticle is pigment-free. The distribution of pigment granules within the cortex is largely regular. No particular layer is preferred.
    As a rule, the pigment granules are localized individually or in groups in the cortical cells, much less often in the intercellular spaces. Occasionally, individual granules are found in the peripheral parts of the cortical cells, enclosed in spaces that are in communication with the intercellular space. In the vicinity of extracellular pigment granules, the intercellular lamellae appear interrupted or severely narrowed.
    In the cortex cells, the pigment granules are embedded between the keratin fibrils, but not between the keratin filaments.
    The distribution of the melanin granules in the cortex cells is not subject to any strict rule and is apparently of no importance for the hair color. Without a doubt, there is a qualitative difference between the pigment granules of blonde and black hair.
    Whether or not the previous metabolic path before the formation of eumelanin and pheomelanin is different cannot be decided with certainty. Much is still unclear about the nature of these pigments and their relationships with one another. In addition to the morphological structure described, their behavior towards various noxae, e.g. alkalis, pharmaceuticals (chloroquine, etc.) is certainly different.
    The melanocytes of the hair bulb are, during the anagen phase, not only dopa-, but also tyrosinase-positive. The intracellular localization of the hair pigment exclusively in the spaces that were previously occupied by the cytoplasm, i.e. between the keratin fibrils, is an indication that the pigment granules are only taken up by the cortical cells after the filaments have condensed into fibrils. The mechanism of infiltration is also unknown in the hair, as in the skin. Morphologically, it appears possible in the hair material that individual or several pigment granules are absorbed in indentations in the cortex cell cytoplasm, the walls of which later stick together (Swift, 1964) and sometimes disappear.
    Graying or whitening of the hair is different from hair to hair, neither simultaneous, uniform, nor gradual loss of melanocytes occurring from gray to white. There is a similar, mosaic-like behavior in pigment depletion as in growth.
    It is believed that the graying of hair due to aging or stress, etc., for example, leads to a decrease in melanocytes or melanosomes, or abnormalities in these cells or organs that result in a decrease in the amount or activity of tyrosinase, inhibition transport of melanosomes, etc., but the mechanism for this is still unclear.
    The color intensity gradually decreases, so that a gray color impression on the transition from black to white is quite conceivable. White hair and pigmented hair are next to each other. In addition, there will be gray hair, especially in older black-haired people, which contains a residual proportion of color pigment. The pigment degradation does not occur abruptly because it does not affect all granules at the same time.
    It is assumed that the more superficial granules disappear faster or earlier than the deeper ones. Exogenous factors, such as sunlight, could be partly responsible for the preferential disintegration of the superficial granules.
    The "whitening" of hair in old age is not based on a corpuscular color, but rather a color impression that is created by the natural color of the hair keratin and by the reflection at the interfaces and the islands of the interfibrillary matrix.
    The color impression of the hair is essentially determined by: color content: type of pigment granules contained in the hair color density: number of pigment granules in the hair and grain size distribution intrinsic color of the keratin: arises from opalescence and clouding phenomena structural features: interfibrillary matrix, nucleus and cytoplasmic Remnants and small vacuoles
    It was assumed early on that the reduced blood flow to the scalp and hormonal influences in old age disrupted melanin synthesis in the sensitive melanoblasts of the hair bulb.
    Due to the lack of the pigment, the light in aging hair is no longer selectively absorbed, but reflected from the interfaces, the nuclear and cytoplasmic residues, and from the islands of the interfibrillary matrix, the spectral distribution being preserved. It is assumed that, in addition to missing or very inadequate pigment granules, particularly with white hair, there are vacuoles, presumably filled with air, on which the light is refracted.
    The whitening of the hair is probably not always based on the same pathomechanism. The hair becomes white if a) there are no active melanocytes in the hair bulbs and therefore no melanin is formed (this is probably the case in poliosis, b) if premelanosomes but no melanin monomers are synthesized in the melanocytes, as in albinism and finally c) if the melanocytes produce no or only a few, apparently inferior pigment granules that are easily broken down or broken down, as in the white hair of older people.
    The etiology of premature graying is also not yet fully known. Most likely, melanocytes within the hair follicles stop producing melanin and this can be compared to the pathophysiology of vitiligo, which in some cases is mediated by an autoimmune mechanism. Premature melanocyte failure is inherited in an autosomal dominant manner. For this and other clinical reasons in premature graying, such as damaging anemia and Graves disease, it has been suggested that the gene coding for premature graying may be linked to one or more genes that control the expression of other traits and diseases. This explains the complexity of the process and constant examinations in order to record the processes more reliably.
    It is known from US2013108564A that 2,4,6-octatrienoic acid is a promoter of melanogenesis in normal human melanocytes. A process via PPAR-y activation is discussed as a mechanism.
    An object of the present invention is to provide further cosmetic care agents for use against the process of graying, in particular for returning grayed hair to its original hair color
    A further object is to provide the use of cosmetic care agents which are able to protect and promote the melanocytes of the hair follicles.
    Against this background, further subtasks of the invention are therefore to provide the use of melatonin-containing topical cosmetic agents for inducing the expression of DOPAchrom tautomerase, fighting the disappearance of the melanocytes of the hair follicles by maintaining and / or regenerating the population of the active melanocytes Globe and silent melanocytes of the upper and uppermost regions of the hair follicles. Increasing the number of hair follicles, increasing the number of melanocytes, improving the differentiation and migration of melanocytes from the hair sheath to the hair matrix and / or increasing the multiplication of hair cells, increasing the amount of melanin, lengthening the hair growth phase and shortening the hair rest period. Phase, to prevent or prevent graying or to restore or maintain the natural hair color, to positively influence melanogenesis and stimulate melanin production, especially in the hair follicle. to increase the expression of tyrosinase in melanocytes, for measures against a gradual decrease in tyrosinase activity, for the prevention and / or treatment of pigmentation diseases, prevention and / or treatment of graying of previously damaged hair, simultaneous prevention and / or treatment of hair thinning, for the promotion of Repigmentation of gray hair, promoting the thickening of vellus hair, inhibiting the senescence of cells that make up or surrounding the hair roots, disturbances in the formation of hair follicles or in the cycle of hair follicle formation, to reduce the occurrence and slow down the progress of Folliculitis, for a more even coloring, smoother hair, and a more even texture of the hair, to favor the differentiation of the melanocytes, i.e. favor the production of more mature or better differentiated melanosomes in melanocytes, for the largely complete remelanization, the strengthening of the hair and hair chaftes, the provision of an agent promoting tyrosinase activity, the stimulating effect on the proliferation of melanocytes and a stimulating effect on the migration of melanocytes, an effect for maintaining or promoting the mitotic reproductive activity of follicle cells or the hair growth activity of head hair, as the growth phase extends, the overall activity of the hair increases.
    The object is achieved according to the main claim by providing a topical cosmetic agent for use in the prevention of graying hair and / or care of color recovered hair and / or the return of gray hair to the original hair color, comprising melatonin and a first and possibly at least one further cosmetically active substance.
    Further preferred embodiments are defined in the subclaims.
    It has now been found, surprisingly, that the use according to the invention of the agents also partially or completely solve the aforementioned subtasks.
    It is assumed that melatonin derivatives which have an effect similar to melatonin are also suitable for the agents used according to the invention.
    Melatonin can be used as a base, hydrochloride or other physiologically acceptable salt.
    The first cosmetically active substance is defined by the following formula 1:R- (CH = CH) n-R '- (CO) XR "(1)where R is a linear or branched alkyl radical having 1 to 20 carbon atoms, R 'is a bond or an alkylene radical having 1 to 5 carbon atoms, X is a bond, an alkylene radical having 1 to 5 carbon atoms, O or S, and R' 'is H , NR1R2, an alkyl radical with 1 to 20 carbon atoms, which optionally contains one double bond or more than two conjugated double bonds, where R1 and R2 are a linear or branched alkyl radical with 1 to 6 carbon atoms or a cycloalkyl ring with 2 to 6 carbon atoms, the can optionally be interrupted by one or two heteroatoms selected from N, O or S, and n = 2 to 7, preferably 5.
    The first substance is preferably a conjugated unsaturated fatty acid or its derivative.
    The derivative is preferably the derived alcohol, the COOH group of the conjugated unsaturated fatty acid being replaced by an OH group, the derived optionally mono- or disubstituted alkyl-substituted amide, the COOH group of the conjugated unsaturated fatty acid being replaced by a group -NR1 (R2) has been replaced, in which R1 and R1, H or a linear or branched alkyl group with 1 to 6 carbon atoms, or a cycloalkyl ring with 2 to 6 carbon atoms, optionally with one or two heteroatoms selected from N, O or S can be interrupted, mean the derived ketone, the COOH group of the conjugated unsaturated fatty acid having been replaced by a group - (C = O) R, in which RH or a linear or branched alkyl group with 1 to 20 carbon atoms, the optionally contains a double bond or more than two conjugated double bonds, or the derived ester, wherein the COOH group of the conjugated unsaturated fatty acid through a group - (C = O) OR has been replaced, in which R is a linear or branched alkyl group with 1 to 20 carbon atoms, which optionally contains one double bond or more than two conjugated double bonds.
    Particularly preferred as substances with conjugated double bonds are octatriene, nonatriene, decatriene, undecatriene, dodecatriene, parinar, Bosseopentaen, punic, catalpine, eleostearic, jacarin, calendula or rumenic acid, or Octatrien-, nonatrien-, decatrien-, undecatrien-, dodecatrien-, parinar-, Bosseopentaen-, Punic-, Catalpin-, Eleostearic-, Jacarin-, Calendula- or Rumenic acid and their derivatives as defined above.
    The agents can also contain at least some further, preferably 5, more preferably 4, more preferably 3, especially 2 substances and particularly preferably one further cosmetically active substance: A) Natural compounds or compounds derived from natural compounds a) Amines, amides or amino acids, such as hexamethylene-bis-acetamide (HMBA), 5-aminolevulinic acid, putrescine, allantoin, capronium chloride, berberine, taurine b) terpenes, diterpenes or triterpenes, such as glycyrrhizin, steviol, isosteviol, isocembrol, carnosol, sclareolid, hesperidin, hesperidin, hesperidin, hesperidin methyl chalcone, chromone, astaxanthin, aesculin, abietic acid, labdan, beta-sitosterol, 17α-estradiol, progesterone c) polyphenol, chromone, xanthonone and flavanone compounds, such as kaempferol, apigenin, gambogic acid, gambogic acid amide, 2 ', 3 ', 4', 3,4-pentahydroxychalcone (okanine), aureusidin, 3,3 ', 4', 5,7-pentahydroxyflavone-3-O-rutinoside (rutin), dihydroquercetin, rheosmin, taxifolin, resveratrol, baicalin d ) Xanthines, such as caffeine, theophylline, theobromine e) Vitamins and provitamins, such as niacinamide, panthenol, folates, folic acid, pantothenates, pyridoxines, riboflavin, thiamine, biotin, ascorbic acid, B) active ingredients8-Benzyl-1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione, naloxone, naloxonazine, 2,3-dimethoxy-5-methylhydroquinone, acitazanolast, iralukast, montelukast, Pranlukast, Velukast, Zafirlukast, Zileuton, bisphosphonate derivatives, pyrimidine derivatives, aminocyclohexane derivatives, piperidine derivatives, retenoids, roxithromycin, finasteride, bimatoprost, cAMP derivatives, dopa derivatives, 3,4-dihydroxyphenyl, 5-trihydroxyphenylalanine, 2-methyl-3- (3,4-dihydroxyphenylalanine) methoxytyrosine, cAMP-Na C) extracts from plantsExtracts, extracts or other preparations from Camellia, Camellia sinensis, Betulaceae, Hamamelis, Tanacetum parthenium, Petroselinum crispum, Broussonetia papyrifera, Castanea sativa, Curcuma angustifolia, Polygonum multiflorum, Panax quinquefolius, Ciper nigrum baccirum, Fiperus nigrum, Unbuscichulum vulgare, malva sylvestris, Ageratum, Valeriana officinalis, Paullinia cupana, Catalpa speciosa, Calendula officinalis, Eryngium foetidum, Rheum rhabarbarum, Syzygium aromaticum, Quassia amara, Areca catechu, Gossypium herbaceum, Aloe vera, Emarinus officinalus, Aloe vera, Emarinus verniana , Ziziphus spina-christi, Fallopia multiflora, Carum carvi, Commiphora mukul, Impatiens, Hibiscus syriacus, Ballota nigra, Cyperus rotundus, Bidens torta, borage oil, evening primrose oil, D) Inorganic compoundsIron salts, iron citrates, iron phosphates, iron EDTA, copper salts such as copper-peptide complexes, manganese salts such as chlorine [N, N'-ethylenbis (salicylidenaminato)] manganese (EUK-8), zinc salts, E) peptides / proteinsNLys-Pro-Valc, NLys-Pro-Thrc, NpGlu-His-Proc, Lys-d-Pro-Thr, thymulin, thymosin alpha-1, thymosin beta-4, insulin, triiodothyronine, thyroxine, extracts of bacteria such as from Beggiatoa, Vitreoscilla, Flexithrix or Leucothrix
    The agents used according to the invention preferably contain at least one further substance selected from: a) amines, amides and amino acids, b) terpenes, diterpenes and triterpenes, c) polyphenol, chromone, xanthone and flavanone compounds, d) xanthines , and e) vitamins and provitamins.
    The substance from group a) is preferably taurine, HMBA, capronium chloride and / or berberine, in particular taurine
    The substance from group b) is preferably glycyrrhizin, carnosol, beta-sitosterol and / or progesterone, in particular beta-sitosterol.
    The substance from group c) is preferably kaempferol, gambogic acid, rutin, rheosmin and / or resveratrol, in particular rheosmin and / or resveratrol.
    The substance from group d) is preferably caffeine
    The substance from group e) is preferably niacinamide, folate, thiamine and / or biotin, in particular biotin.
    In the case of more than 2 further substances, these can be selected from the same group, preferably from different groups a) to e).
    As a further substance, caffeine and / or biotin are particularly preferred. Caffeine is particularly preferred.
    If a substance from group B) is used, it can be used instead of a substance from group A) or one or more substances from group B) can be used with melatonin.
    If a substance from group C) is used, it can be used instead of a substance from group A) and / or B) or one or more substances from group C) can be used with melatonin.
    If a substance from group D) is used, it can be used instead of a substance from group A), B) and / or C) or one or more substances from group D) can be used with melatonin.
    If a substance from group E) is used, it can be used instead of a substance from group A), B), C) and / or E) or one or more substances from group E) can be used with melatonin .
    Preferred substances of group B) are cAMP-Na, dopa derivatives, retenoids and / or finasteride, especially finasteride.
    Preferred substances of group C) are extracts, extracts or other preparations of Camellia sinensis, Rosmarinus officinalis, borage oil, evening primrose oil and / or Calendula officinalis, in particular Camellia sinensis, borage oil and / or evening primrose oil.
    Preferred substances of group D) are iron salts, copper salts, zinc salts, in particular zinc and / or copper salts.
    Preferred substances of group E) are Lys-d-Pro-Thr, thymulin, thymosin alpha-1, thymosin beta-4 and / or thyroxine, in particular Lys-d-Pro-Thr, thymulin and / or thyroxine.
    The agents used according to the invention can be formulated as creams, hair treatments, hair packs, hair lotions, hair gels, lotions or tinctures for hair for application by spray or pen applicators or with pipettes, swabs, sponges, tissues or the like.
    The agents used according to the invention are also particularly suitable for long-term use with a prophylactic effect. For example, a leave-on hair tonic based on ethanol is preferred.
    In a first embodiment of the agents used according to the invention, the preparations used according to the invention contain 0.0001 to 5.0 mg melatonin, preferably 0.001 to 1.0 mg melatonin, more preferably 0.005 to 0.2 mg per ml of preparation.
    The first cosmetically active substance (s) that may be present and the further cosmetically active substance (s) that may be present ( e) is / t (s) in a weight ratio of melatonin to the further substance in the range from 0.001: 1000 to 1000: 0.001. Preferred ranges are 0.01: 100 to 100: 0.01; 0.05: 80 to 80: 0.05; 0.1: 50 to 50: 0.1, or 0.5: 30 to 30: 0.5.
    The agents used according to the invention can 1 to three times a day, preferably once a day, preferably in the evening by spraying, dripping and / or rubbing, brushing with an applicator, such as a brush or a sponge, by applying a damp cloth to the scalp or can also be applied as a shampoo by foaming.
    For a successful treatment, at least 4 weeks, preferably at least 8 weeks, of treatment are required. The care agent used according to the invention can be designed as a cure or administered as a long-term treatment.
    The aforementioned formulations of the agents used according to the invention can contain auxiliaries and additives such as those explained below: A surfactant in the agent used according to the invention can be selected from any known surfactant which is suitable for topical application to the human body. Mild surfactants, i.e. surfactants that do not damage the stratum corneum, the outer layer of the skin, are particularly preferred. Because of their foaming properties, anionic surfactants are very preferred components of the compositions used according to the invention. When the composition contains an anionic surfactant, it is advantageous that the composition also contains a co-surfactant, which can be an anionic, cationic or zwitterionic surfactant. The surfactant can be present in the composition in an amount of from 0.5 to 15% by weight.
    The surfactants can be a fatty acyl isethionate, alkyl ether sulfate, alkyl glyceryl ether sulfate, sulfosuccinates, taurates, sarcosinates, sulfoacetates, alkyl phosphate, alkyl phosphate esters and lactic acid acyl esters, glutamic acid alkyl esters and mixtures thereof.
    Suitable nonionic surfactants include alkyl polysaccharides, lactobionamides, ethylene glycol esters, glycerol monoethers, polyhydroxyamides (glucamide), primary and secondary alcohol ethoxylates, especially the C8-20 aliphatic alcohols ethoxylated with an average of 1 to 20 moles of ethylene oxide per mole of alcohol.
    It is also preferred that the composition include 0.5 to 15% by weight of a cosurfactant agent having skin mildness benefits. Suitable materials are zwitterionic detergents which have an alkyl or alkenyl group with 7 to 18 carbon atoms, and these are also betaines or sulfobetaines. Surfactants and cosurfactants are particularly suitable for formulations used according to the invention, such as shampoos.
    Cationic polymers suitable for the purpose used according to the invention include, for example, copolymers of vinyl monomers with cationic amine or quaternary ammonium functionalities with water-soluble space monomers, such as (meth) acrylamide, alkyl and dialkyl (meth) acrylamides, alkyl (meth) acrylate, vinyl caprolactone and Vinyl pyrrolidine. The alkyl and dialkyl substituted monomers preferably have C1-C7 alkyl groups, more preferably C1-C3 alkyl groups. Other suitable spacer groups include vinyl esters, vinyl alcohol, maleic anhydride, propylene glycol and ethylene glycol. Cationic polymers can be used in an amount from 0.1 to 10% by weight of the formulation.
    [0079] The compositions according to the invention may further myristyl myristate, myristyl palmitate, myristyl stearate, Myristylisostearat, myristyl, Myristylbehenat, Myristylerucat, cetyl myristate, cetyl palmitate, cetyl stearate, Cetylisostearat, cetyl oleate, cetyl behenate, Cetylerucat, Stearylmyristat, stearyl palmitate, stearyl stearate, Stearylisostearat, stearyl oleate, stearyl behenate, Stearylerucat , isostearyl, isostearyl palmitate, Isostearylstearat, isostearyl isostearate, Isostearyloleat, isostearyl behenate, Isostearyloleat, oleyl myristate, oleyl palmitate, oleyl stearate, oleyl isostearate, oleyl oleate, Oleylbehenat, oleyl erucate, behenyl myristate, behenyl palmitate, behenyl, Behenylisostearat, behenyl oleate, behenyl behenate, behenyl erucate, erucyl myristate, erucyl, erucyl, erucyl , Erucyl oleate, erucyl behenate and erucyl eucate. The fatty acid esters can be used in an amount from 0.1 to 10% by weight of the formulation.
    The combined use of fatty alcohol materials and cationic surfactants in conditioning compositions is believed to be particularly advantageous because it leads to the formation of a lamellar phase in which the cationic surfactant is dispersed. Representative fatty alcohols comprise 8 to 22 carbon atoms, more preferably 16 to 20. Examples of suitable fatty alcohols include cetyl alcohol, stearyl alcohol, and mixtures thereof. The use of these materials is also advantageous in that they contribute to the overall conditioning properties of the compositions used according to the invention. The proportion of fatty alcohol material in agents used according to the invention is suitably from 0.01 to 10%, preferably from 0.1 to 5% by weight of the composition. The weight ratio of cationic surfactant to fatty alcohol is suitably 10: 1 to 1:10, preferably 4: 1 to 1: 8, optimally 1: 1 to 1: 4.
    The agents used according to the invention can also contain emulsifiers. Examples are ethoxylated fatty alcohols, ethoxylated fatty amines, ethoxylated fatty acids, ethoxylated alkylphenols, ethoxylated oils, e.g. hardened ethoxylated castor oil, ethoxylated polyols, ethoxylated mono-, di- and trialkyl phosphates, ethoxylated wool wax alcohols, ethoxylated poly-poly-polyether derivatives, ethoxylated poly-poly-siloxane derivatives. etc. Instead of ethoxylation, propoxylation or mixed etoxylation / propoxylation can also be carried out.
    [0082] Due agents used in this invention may also contain partial glycerides, such as hydroxystearic, hydroxystearic acid diglyceride, isostearic acid, Isostearinsäurediglycerid, oil-resistant acid monoglyceride, oleic acid diglyceride, Ricinolsäuremoglycerid, Ricinolsäurediglycerid, Linolsäuremonoglycerid, Linolsäurediglycerid, Linolensäuremonoglycerid, Linolensäurediglycerid, Erucasäuremonoglycerid, Erucasäurediglycerid, Weinsäuremonoglycerid, Weinsäurediglycerid, Citronensäuremonoglycerid, Citronendiglycerid , Malic acid monoglyceride, malic acid diglyceride and mixtures thereof. Ethoxylation products of 1 to 30, preferably 5 to 10, mol of ethylene oxide on the partial glycerides mentioned are also suitable. These materials can be used in an amount from 0.1 to 10% by weight of the formulation.
    [0083] As an additional sorbitan can also be used, such as sorbitan, sorbitan sesquiisostearate, Sorbitan, sorbitan triisostearate, sorbitan monooleate, sorbitan, sorbitan, Sorbitanmonoerucat, Sorbitansesquierucat, Sorbitandierucat, Sorbitantrierucat, Sorbitanmonoricinoleat, Sorbitansesquiricinoleat, Sorbitandiricinoleat, Sorbitantriricinoleat, Sorbitanmonohydroxystearat, Sorbitansesquihydroxystearat, Sorbitandihydroxystearat , Sorbitan trihydroxystearate, sorbitan monotartrate, sorbitan sesqui-tartrate, sorbitan ditartrate, sorbitan trite tartrate, sorbitan monocitrate, sorbitan sesquicitrate, sorbitan citrate, sorbitan tricitrate, sorbitan monantomaleate, sorbitan quantum maleate, sorbitan sorbitan, sorbitan, sorbitan, technical, sorbitan ses. Ethoxylation products of 1 to 30, preferably 5 to 10, mol of ethylene oxide onto the sorbitan esters mentioned are also suitable. These materials can be used in an amount from 0.1 to 10% by weight of the formulation.
    The agents used according to the invention can also contain silicone compounds, such as dimethylpolysiloxanes, methylphenylpolysiloxanes, cyclic silicones and amino, fatty acid, alcohol, polyether, epoxy, fluorine, glycoside and / or alkyl-modified silicone compounds, which at room temperature can be both liquid and resinous. Simethicones, which are mixtures of dimethicones with an average chain length of 200 to 300 dimethylsiloxane units and hydrogenated silicates, are also suitable.
    Suitable silicones include polydiorganosiloxanes, especially polydimethylsiloxanes, which have the CTFA designation dimethicone. Also suitable for use in compositions used according to the invention (in particular shampoos and conditioners) are polydimethylsiloxanes with hydroxyl end groups, which have the CTFA designation dimethiconol. Silicone rubbers with a low degree of crosslinking are also suitable for use in the compositions used according to the invention. These materials can also add body, volume, and manageability to hair as well as good wet and dry conditioning.
    Examples of suitable pre-formed emulsions include emulsions DC2 <®> -1766, DC2 <®> -1784, and microemulsions DC2 <®> -1865 and DC2 <®> -1870, all available from Dow Corning. These are all emulsions / microemulsions from Dimethiconol. Crosslinked silicone gums are also available in pre-emulsified form, which is advantageous for easy formulation. A preferred example is the material available from Dow Corning as DC <®> X2-1787, which is an emulsion of crosslinked dimethiconol gum. Another preferred example is the material available from Dow Corning as DC <®> X2-1391, which is a microemulsion of crosslinked dimethiconol gum.
    Since the agents used according to the invention for aged scalps are provided with their disadvantages, such as higher UV sensitivity, it is advantageous to additionally add UV light protection factors, such as, for example, organic substances (light protection filters) present in liquid or crystalline form at room temperature to understand the are able to absorb ultraviolet rays and to release the absorbed energy in the form of longer-wave radiation, e.g. heat. UVB filters can be oil-soluble or water-soluble. Examples of oil-soluble substances are: 3-benzylidene camphor or 3-benzylidene norcamphor and its derivatives, e.g. 3- (4-methylbenzylidene) camphor; 4-aminobenzoic acid derivatives, preferably 4- (dimethylamino) benzoic acid 2-ethylhexyl ester, 4- (dimethylamino) benzoic acid 2-octyl ester and 4- (dimethylamino) benzoic acid amyl ester; Esters of cinnamic acid, preferably 2-ethylhexyl 4-methoxycinnamate, propyl 4-methoxycinnamate, isoamyl 4-methoxycinnamate, 2-cyano-3,3-phenylcinnamic acid-2-ethylhexyl ester (octocrylene); Esters of salicylic acid, preferably 2-ethylhexyl salicylate, 4-isopropylbenzyl salicylate, homomenthyl salicylate; Derivatives of benzophenone, preferably 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone, 2,2'-dihydroxy-4-methoxybenzophenone; Esters of benzalmalonic acid, preferably 4-methoxybenzmalonic acid di-2-ethylhexyl ester; Triazine derivatives, such as 2,4,6-trianilino- (p-carbo-2'-ethyl-1'-hexyloxy) -1,3,5-triazine and octyl triazon, or dioctyl butamido triazone (Uvasorb (R) HEB) ; Propane-1,3-diones such as 1- (4-tert, butylphenyl) -3- (4'-methoxyphenyl) propane-1,3-dione; Ketotricyclo (5.2.1.0) decane derivatives.
    Film formers in the agents used according to the invention can be helpful, for example chitosan, microcrystalline chitosan, quaternized chitosan, polyvinylpyrrolidone, vinylpyrrolidone-vinyl acetate copolymers, polymers of the acrylic acid series, quaternary cellulose derivatives, collagen, hyaluronic acid and its salts .
    Anti-dandruff active ingredients can also prepare the scalp for the action of the agents used according to the invention.
    The agents used according to the invention can optionally also contain perfume oils and preservatives.
    The preferred base is an alcoholic or aqueous-alcoholic base which may contain other auxiliaries, e.g. as mentioned above. C2-C4-alkanols are preferred, preferably ethanol and / or isopropanol. If desired, dimethyl sulfoxide (DMSO) can be contained as a penetration enhancer in an amount of 0.1 to 30% by weight.
    example
    A solution of 0.1 mg melatonin in 1 ml 50% ethanol was prepared. 2 mg of sodium octatrienoate, a perfume (0.01% by weight) and a coloring agent were also added to the solution.
    The agent obtained in this way was applied as uniformly as possible to affected areas of the scalp by spraying to a test person with sections of slightly graying hair in an amount of about 3 ml once a day in the evening. As a control, only 50% of the ethanol was sprayed onto other affected areas of the scalp.
    It was observed that the hair follicles became darker again, and it was further observed that the hair stump grew out of the follicle as a hair shaft of darker color. This did not occur at a control point. After a treatment time of 6 weeks, parts of a section with slightly graying hair had regained the original hair color. After 8 weeks, clear changes were observed over almost all treated areas, with the exception of the control areas.
    Although the details of the mechanism for preventing graying hair or restoring gray hair to its natural color with the agents used in the present invention have not yet been found, it is believed that when applied topically, the melanocytes that are present in the scalp Radix pilii are present and the melanoblasts, which represent the precursors of melanocytes, are activated by the agents used according to the invention in order to promote the formation of melanin and the melanin granules obtained are built into the mother cells of the hair.
    On the basis of these measures, the progress of the graying of hair is stopped and / or slowed down and / or, surprisingly, a return of grayed hair to the original hair color is also achieved.
    权利要求:
    Claims (14)
    [1]
    1. Topical cosmetic agent for use in the prevention of graying hair and / or the care of hair that has recovered in color and / or the return of gray hair to its original hair color, comprising melatonin and a first and optionally at least one further cosmetically active substance.
    [2]
    2. Topical cosmetic agent for use according to claim 1, wherein the first substance is defined by the following formula 1:R- (CH = CH) n-R '- (CO) XR ". (1)where R is a linear or branched alkyl radical having 1 to 20 carbon atoms, R 'is a bond or an alkylene radical having 1 to 5 carbon atoms, X is a bond, an alkylene radical having 1 to 5 carbon atoms, O or S, and R' 'is H , NR1R2, or an alkyl radical with 1 to 10 carbon atoms, which optionally contains one double bond or more than two conjugated double bonds, where R1 and R2 are a linear or branched alkyl radical with 1 to 6 carbon atoms or a cycloalkyl ring with 2 to 6 carbon atoms, the can optionally be interrupted by one or two heteroatoms selected from N, O or S, and n = 2 to 7.
    [3]
    3. Topical cosmetic agent for use according to claim 1 or 2, wherein the first substance is a conjugated unsaturated fatty acid or its derivative.
    [4]
    4. Topical cosmetic agent for use according to claim 3, wherein the derivative is the derived alcohol, wherein the COOH group of the conjugated unsaturated fatty acid has been replaced by an OH group, the derived optionally mono- or disubstituted alkyl-substituted amide, the COOH -Group of the conjugated unsaturated fatty acid has been replaced by a group -NR1 (R2), in which R1 and R1, H or a linear or branched alkyl group with 1 to 6 carbon atoms, or a cycloalkyl ring with 2 to 6 carbon atoms, optionally with one or two heteroatoms selected from N, O or S may be interrupted, mean the derived ketone, the COOH group of the conjugated unsaturated fatty acid having been replaced by a group - (C = O) R, in which RH or a linear or branched alkyl group with 1 to 20 carbon atoms, which optionally contains one double bond or more than two conjugated double bonds, or the derived ester, where the COOH group is the conjugated unsaturated fatty acid has been replaced by a group - (C = O) OR, where R is a linear or branched alkyl group with 1 to 20 carbon atoms, which optionally contains one double bond or more than two conjugated double bonds.
    [5]
    5. Topical cosmetic agent for use according to one of the preceding claims, wherein the at least one further substance is selected from:a) amines, amides and amino acids,b) terpenes, diterpenes and triterpenes,c) Polyphenol, chromone, xanthone and flavanone compounds,d) xanthines, ande) vitamins and provitamins.
    [6]
    6. Topical cosmetic agent for use according to one of the preceding claims, wherein the at least one further substance is selected from the compounds: caffeine, theobromine, 5-aminolevulinic acid, capronium chloride, carnosol, taxifolin, rheosmin, resveratrol, niacinamide and / or panthenol.
    [7]
    7. Topical cosmetic agent for use according to one of the preceding claims, wherein the at least one further substance is selected from:8-Benzyl-1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione, naloxone, naloxonazine, 2,3-dimethoxy-5-methylhydroquinone, acitazanolast, iralukast, montelukast, Pranlukast, Velukast, Zafirlukast, Zileuton, bisphosphonate derivatives, pyrimidine derivatives, aminocyclohexane derivatives, piperidine derivatives, retenoids, ascorbic acid, panthenol, roxithromycin, finasteride, bimatoprost, tafluprost, cAMP derivatives, 3,4 dihydroxyphenylserine, 2,4,5-trihydroxyphenylalanine, 2-methyl-3- (3,4-dihydroxyphenylalanine) methoxytyrosine and cAMP-Na.
    [8]
    8. Topical cosmetic agent for use in one of the preceding claims, wherein the at least one further substance is selected from an extract, extract or another preparation made from the following species:Camellia, Camellia sinensis, Betulaceae, Hamamelis, Tanacetum parthenium, Petroselinum crispum, Broussonetia papyrifera, Castanea sativa, Curcuma angustifolia, Polygonum multiflorum, Panax quinquefolius, Piper nigrum, Uncoenaria gambirata, vulgarium bacciryl, Cichorium baccybus, Taxus gambirata, Cichorium baccirata Valeriana officinalis, Paullinia cupana, Catalpa speciosa, Calendula officinalis, Eryngium foetidum, Rheum rhabarbarum, Syzygium aromaticum, Quassia amara, Areca catechu, Gossypium herbaceum, Aloe vera, Rosmarinus officinalis, Gentiana vernia, Eucalyptus, Christulus-Humlopina multiflora, Carum carvi, Commiphora mukul, Impatiens, Hibiscus syriacus, Ballota nigra, Cyperus rotundus and Bidens torta.
    [9]
    9. Topical cosmetic agent for use according to one of the preceding claims, wherein the at least one further substance is selected from inorganic compounds:Iron salts, iron citrates, iron phosphates, iron EDTA, copper salts, such as copper-peptide complexes, manganese salts, such as chlorine [N, N'ethylenbis (salicylidenaminato)] manganese (EUK-8).
    [10]
    10. Topical cosmetic agent for use according to one of the preceding claims, wherein the at least one further substance is selected from peptides or proteins:NLys-Pro-Valc, NLys-Pro-Thrc, NpGlu-His-Proc, thymulin, thymosin alpha-1, thymosin beta-4, insulin, triiodothyronine, thyroxine, extracts from bacteria such as from Beggiatoa, Vitreoscilla, Flexithrix and Leucothrix.
    [11]
    11. Topical cosmetic agent for use according to one of the preceding claims, wherein melatonin is used in an amount of 0.0001 to 5.0 mg.
    [12]
    12. Topical cosmetic agent for use according to one of the preceding claims, wherein the weight ratio of melatonin to the first cosmetically active substance and / or the further cosmetically active substance is in the range from 0.001: 1000 to 1000: 0.001.
    [13]
    13. Topical cosmetic agent for use according to one of the preceding claims, wherein the agent is applied at least once a day.
    [14]
    14. Topical cosmetic agent for use according to one of the preceding claims, wherein the agent is applied in the evening.
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    同族专利:
    公开号 | 公开日
    DE102019131415A1|2021-05-27|
    AT523300A2|2021-06-15|
    引用文献:
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    DE102019131415.1A|DE102019131415A1|2019-11-21|2019-11-21|Cosmetic care for graying hair and returning gray hair to its original hair color|
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