Dermatological products

Abstract

The present invention provides products for treating or preventing human hair or skin disorders or for skin or hair care. The present invention discloses a composition comprising niacinamide in combination with a sugar alcohol, or a combination of a sugar alcohol and a Tetraselmis extract, or either of the former.

Description

[Technical Field]

[0001] The present invention provides a method for treating or preventing hair or skin dysfunction in humans. Sugar alcohols, or sugar alcohols and tetrahydroxybenzoates, as cosmetic or skin or hair care products Tetraselmis extract combination, or either the former and Compositions containing combined niacinamide are disclosed. [Background technology]

[0002] Prior art US2010143267A1 (Symrise) states, inter alia, For example, levels of cornified membrane protein components such as filaggrin and / or involucrin The present invention describes the use of an extract obtained from Tetraselmis species to stimulate the immune system. hexane, ethyl acetate, ethanol, water, methanol, isopropanol and A liquid extractant selected from the group consisting of a mixture of two or more extractants at a temperature of 50°C or less Tetraselmis species, preferably Tetraselmis suesica (Tetra Extracting freeze-dried or dried viable cells of S. selmis suecica According to Examples 33 to 40 and 41 to 48, continuous enzyme activity at 5 μg / mL was obtained. Alcohol extraction increases involucrin and filaggrin in human skin ex vivo This is the most effective extraction.

[0003] Official document EP2193785A2 concerns the extraction of Tetraselmis suecica. The present invention discloses a composition containing an extract of Tetraselmis suecica. These compositions differ in the sugar alcohols present.

[0004] Compositions using Tetraselmis extract in combination with high levels of sugar alcohols are at the forefront of the technology. are not known to affect the skin treatment properties of topical applications using the compositions of the present invention. do. Summary of the Invention

[0005] The object of the present invention is therefore to provide a new composition of active ingredients suitable for reducing sebum production. The purpose is to provide.

[0006] Another problem to be solved by the present invention is the function of human hair and / or skin. To obtain new cosmetic or dermatological compositions and products for treating or preventing disorders. and the use of these compositions for cosmetic and therapeutic applications.

[0007] The problem related to the present invention is solved by the following: a composition comprising sugar alcohols and Tetraselmis extract, wherein the total sugar alcohol content is calculated based on the dry weight of the extract and is the total sugar alcohol content of the entire composition. 16% by weight or more The amount of Tetraselmis extract is based on the dry weight of the extract as follows: 10% by weight or more The total minerals of the Tetraselmis extract composition are further included. 3% by weight or more of total galactose of the entire Tetraselmis extract composition 2% by weight or more of total glucose of the entire Tetraselmis extract composition 3% by weight or more and the total amino acids of the Tetraselmis extract composition 2% by weight or more of total nitrogen.

[0008] The subject of the present invention is further to provide a method for producing a tetraselmis extract containing both sugar alcohols and tetraselmis extract, and containing niacin. The problem is solved by a combination composition further comprising acinamide.

[0009] The present invention further relates to a composition comprising 0.5 to 80% by weight of the composition or combination composition of the present invention. The present invention also includes concentrates containing 0.5 to 90% by weight of water and 0.5 to 90% by weight of The formulation contains a carrier and 0.1 to 5% by weight of one or more preservatives or preservative systems. All calculations are based on the dry weight of Tetraselmis extract.

[0010] In particular, the present invention also provides a method for preparing a soluble fiber containing one or more sugar alcohols, preferably mannitol, or niacin. A combination of one or more sugar alcohols, preferably mannitol, together with cinnamide These medicines and cosmetics are used to treat skin diseases. It is useful. DETAILED DESCRIPTION OF THE INVENTION

[0011] Surprisingly, sugar alcohols themselves or extracts from the microalga Tetraselmis suecica It has now been discovered that sugar alcohol combinations are highly effective in reducing sebum production .

[0012] Furthermore, surprisingly, sugar alcohols, either by themselves or in combination with Tetraselmis extract, Sugar alcohols are involved in cell-cell adhesion, e.g., desmosomal ("mechanical") bonds, The integrity of epidermal junctions and tissues such as tight junctions, adherens junctions, and gap junctions as well as adjacent cells Many involved in permitting the exchange of ions, second messengers, and small molecule metabolites between cells It was found to strongly upregulate genes.

[0013] Furthermore, sugar alcohols alone or in combination with Tetraselmis extracts were surprisingly Importantly, these proteins are involved in processes such as wound healing, tissue regeneration and barrier formation. It regulates genes related to differentiation and re-epithelialization.

[0014] Furthermore, we have surprisingly found that sugar alcohols and in particular those of formula (I) Mannitol itself was found to significantly reduce sebum production. [ka]

[0015] Mannitol, CAS 69-65-8(I), is a sugar alcohol. It is an isomer of glycerin, and today it is usually formed from starch or sucrose (common sugar). It is produced by hydrogenating fructose, which is a sugar that is poorly absorbed from the intestinal tract. It is often used as a sweetener in diabetic diets because it is not easily absorbed. It is primarily used as a humectant, but also as a carrier / diluent, binder, suspending agent, masking agent, Moisturizers, osmolytes, hydrophilic antioxidants and / or flavoring agents (e.g., in lip balms) Mannitol may also be found to be useful in preventing the hyperlipidemia seen in, for example, glaucoma. It is also used as a drug to reduce low intraocular pressure and high intracranial pressure.

[0016] Thus, in a first aspect, the present invention relates to a composition comprising a sugar alcohol and a Tetraselmis extract, wherein the total sugar alcohol content is calculated based on the dry weight of the extract and is the total sugar alcohol content of the entire composition. 16% by weight or more The Tetraselmis extract further comprises the following based on the dry weight of the extract: 10% by weight or more The total minerals in the Tetraselmis extract composition are 3% by weight or more of total galactose of the entire Tetraselmis extract composition 2% by weight or more of total glucose of the entire Tetraselmis extract composition 3% by weight or moreand the total amino acids of the Tetraselmis extract composition 2% by weight or more Preferably, the Tetraselmis extract as described herein is a Tetraselmis suecica extract.

[0017] Tetraselmis biomass was grown in a photobioreactor or a large tank under sunlight or artificial light. It can be obtained by culturing in polyethylene bags or tanks of the same type. Cultivation can occur indoors or outdoors. Once the microalgae biomass reaches a suitable cell density, by centrifugation or sedimentation or flocculation or other technique suitable to preserve the integrity of the cellular material. The harvested biomass is then fresh (viable) and can be harvested. ) or dried, for example, by freeze-drying or spray-drying, and The raw material for extraction has so far been unextracted biomass. from the mass or previous extraction, or from e.g. ethyl acetate, hexane, cyclohexane San, acetone, carbon dioxide, methanol, ethanol, propanol, isopropanol ethanol, 1-butanol, 2-butanol, tert-butanol, or a mixture of organic solvents Residual biomass resulting from treatment with organic solvents such as cellulose can be used.

[0018] The method for obtaining Tetraselmis extract is to extract Tetraselmis cells with a liquid extractant. wherein the extraction comprises (a) exposing the cellular material to an extractant for up to 8 hours; and (b) ) removal of cellular material to obtain an extract.

[0019] The Tetraselmis extract is preferably prepared by extracting Tetraselmis cells with a liquid extractant. Preferably, the extraction is carried out at a temperature above 60°C. The cells of the culture are preferably used fresh (viable), e.g., freeze-dried or spray-dried. It is dried by fog drying or processed by suitable techniques.

[0020] Suitable liquid extractants for extraction are polar solvents, i.e., solvents with a dielectric constant greater than 15. Preferably, the extraction of Tetraselmis suecica cells is carried out using a solvent such as 2-propanone, ethanol, or the like. , water, methanol, isopropanol, and mixtures of two or more of these solvents. This is carried out by the polar solvent selected.

[0021] The ratio of extractant to tetraselmis matrix is ​​preferably between 80:1 and 3:1. More preferably, it is 20:1 to 8:1. This relatively low ratio is due to the small amount of extractant. leads to improved depigmenting effect.

[0022] Particularly preferred common extraction processes are maceration, remaceration, digestion, agitation maceration, and vortex extraction. Extraction, ultrasonic extraction, countercurrent extraction, permeation, re-permeation, evaporation (vacuum extraction), subcritical or supercritical fluid extraction, diacollation, and solid / liquid extraction under continuous reflux. Osmosis is even more preferred and has been found to have advantageous scalability properties.

[0023] In some preferred cases, extraction is performed twice or three times with Tetraselmis biomass cellular material. The liquid extracts are combined after removal of cellular material.

[0024] Extraction preferably involves exposing the cellular material to an extractant at a temperature above 60°C for up to 8 hours. An exposure time of 0.5 to 4 hours is preferred. Even more preferred The exposure time of the cellular material to the extractant is 1 to 3 hours.

[0025] After the extraction of Tetraselmis cells is complete, the cellular material is removed to obtain the extract. In most cases, the extract is a dried Tetraselmis extract. In this case, the extracting agent is the extractant. Removed from emitted material.

[0026] In the present invention, the Tetraselmis extract is preferably partially or completely extracted with an extractant. Preferably, the dried Tetraselmis extract is obtained by completely removing If the extractant is partially removed, then the remaining extractant is 0.5 to 10 wt. % of the extract.

[0027] Most preferred is a Tetraselmis extract as described throughout this specification. The substance is Tetraselmis suecica extract. Tetraselmis suecica algae has been cultivated in Italy for some time, e.g. in Orbetello In addition, Tetraselmis of different origins were cultivated in Italian hatcheries. Six strains of S. suesica are collected from the CCAP (Culture Collection of Algal and Protozoan Cultures), e.g., CC AP66 / 4, CCAP66 / 22A, CCAP66 / 22B, CCAP66 / 22C, Available from CCAP66 / 22D and CCAP66 / 38. Other sources of biological material for this invention, such as the Lasselmis suesica algae culture collection, are also available. can be considered a potential source of income.

[0028] The resulting extract also does not show a strong dark green color, but the resulting Tetraselmis extract is exhibiting a pleasing beige color when applied in pharmaceutical and / or cosmetic and / or other compositions (See Procedure Example 1).

[0029] Furthermore, the Tetraselmis extract thus provided significantly reduces sebum production in the skin. (See Procedural Example 3).

[0030] Furthermore, temperatures above 70°C are preferred for extraction. It was found that Tetraselmis extract beneficially affected the sebum-reducing ability of the extract. It also provided a pleasing color.

[0031] Even more preferred is a temperature during exposure of 75°C or higher, and most preferred is 75-9 5°C. This temperature is sufficient to provide the above-named color benefits and sebum-reducing properties. as well as epidermal junctions, antimicrobial peptides, and water / glycerol transport in the skin. A specific gene involved in the regulation of COX-2 surprisingly affects the gene expression. Tetraselmis extracts are also provided.

[0032] In the present application, as indicated above and throughout the present application, Tetraselmis extract is preferably obtained by partially or preferably completely removing the extracting agent. The resulting dried Tetraselmis extract is obtained. If so, then the remaining extractant is present in the extract in an amount of 0.5 to 10% by weight.

[0033] In some cases, Tetraselmis extract in its liquid, native form without undergoing a drying process Alternatively, prior to partial drying, a solvent such as glycerin may be used. In such cases, the active ingredient is usually dissolved in it. A stable aqueous glycerin solvent system is achieved.

[0034] Preferably, the extract is a dried Tetraselmis suecica extract; in this case, The above-described method further comprises the step of (c) removing the extracting agent.

[0035] The composition of the Tetraselmis extract obtained by extraction at 80°C and room temperature is specified in Table 2. do.

[0036] Tetraselmis extract, especially Tetraselmis suecica extract, has been shown to reduce sebum production. It was found to be highly efficient at 10-14 wt.% mannite. This suggests that the sebum-reducing effect of such extracts is particularly This is supported by the procedure described in Example 3. Preferably, the extract is 15 to 30 It is also preferred that the extract contains 7 to 20% by weight of total minerals. The amount of galactose within the preferred range thereby increases the shelf life of the extract. Furthermore, it is preferred that the extract contains 5 to 13% by weight of total glucose, Increase the shelf life of the extract. Furthermore, the extract is at least 6% by weight, but not more than 16% by weight. It is also preferred that the extract contains 3 to 7 percent by weight or less of total amino acids. It is preferred that the total nitrogen content be 100% by weight.

[0037] One method for obtaining the composition of the present invention is to utilize the Tetraselmis extract in a liquid extractant obtained by extraction according to the method mentioned above, and to obtain a total amount of sugar alcohols in the entire composition. 16% by weight or more , preferably 18% by weight or moreThe sugar alcohol is added to the Tetraselmis extract material in the liquid extractant in an amount such that the sugar alcohol is added to the Tetraselmis extract material in the liquid extractant. Subsequently, it is then preferred to remove the extractant to obtain a dried product. In some preferred cases, extraction is performed twice or three times on the Tetraselmis biomass cellular material, and the liquid extracts are combined before further addition of the sugar alcohol. Typically, the sugar alcohol added in this manner is preferably mannitol.

[0038] Another alternative method for obtaining the composition of the present invention utilizes a dried Tetraselmis suecica extract obtained by extraction according to the method mentioned above, wherein the total amount of sugar alcohols in the entire composition is 16% by weight or more , preferably 18% by weight or more The sugar alcohol added to the dried Tetraselmis extract is preferably mannitol.

[0039] Preferably, the Tetraselmis extract in the composition of the present invention contains 10-14% by weight of mannitol. Contains 15-30% by weight of total minerals and 7-20% by weight of total galactose. It is also preferred that the sugars contain more than 8% by weight of total galactose. The amount of galactose in the low range increases the shelf life of the extract. The content of total glucose is 5 to 13% by weight, and more preferably more than 4% by weight. It is further preferred that the extract contains at least 6% by weight, but not more than 16% by weight. It is also preferred that the extract contains 3 to 7% by weight of the total amino acids. It is preferred that the total nitrogen content is:

[0040] Preferably, the Tetraselmis extract comprises 6 to 12% of the total composition based on the dry weight of the extract. % by weight of the total composition, and even more preferably 8 to 11% by weight of the total composition of free galactose and bound galactose. It has a total galactose content, which is the sum of lactose and galactose. This leads to improved skin hydration properties of Esica extract-based cosmetics and drugs.

[0041] Preferably, the Tetraselmis extract comprises 4 to 10% of the total composition based on the dry weight of the extract. % by weight of free glucose and bound glucose, and even more preferably between 6 and 9% by weight of the total composition. It has a total glucose content which is the sum of the courses. This leads to improved skin hydration properties of extract-based cosmetics and drugs.

[0042] Preferably, the Tetraselmis extract comprises 0.1 to 1.5% of the total composition based on the dry weight of the extract. 1.5% by weight, and even more preferably between 0.6 and 1.0% by weight of the total composition. The total arginine content is the sum of arginine and bound arginine.

[0043] Preferably, the Tetraselmis extract comprises 0.1 to 1.5% of the total composition based on the dry weight of the extract. 1.0% by weight, even more preferably between 0.3 and 0.5% by weight of the total composition of free asparagus It has a total asparagine content which is the sum of asparagine and bound asparagine.

[0044] Preferably, the Tetraselmis extract comprises 0.8 parts by weight of the total composition based on the dry weight of the extract. Free asparagus less than 0.2% by weight of the total composition, and even more preferably between 0.2 and 0.3% by weight of the total composition. The total aspartic acid content is the sum of phosphate and bound aspartic acid.

[0045] Preferably, the Tetraselmis extract comprises 1.5 parts of the total composition based on the dry weight of the extract. less than 0.4-0.6% by weight of the total composition, and even more preferably between 0.4-0.6% by weight of the total composition and bound ornithine.

[0046] Preferably, the Tetraselmis extract is Tetraselmis suecica extract.

[0047] Sugar alcohols are polysaccharides that result from the reduction of carbonyl groups in monosaccharides to hydroxyl groups. Sugar alcohols derived from disaccharides require only one aldehyde group for reduction. It is not entirely hydrogenated because it is not available.

[0048] In a first preferred variant of the first aspect, the sugar alcohol is a C4, C5, C6 or C7 The sugar alcohol is selected from one or more of a sugar alcohol or a disaccharide sugar alcohol.

[0049] Tetraselmis synergistically combined with a sugar alcohol according to the first variant of the first aspect. Suecia extract has been found to have a particularly pronounced sebum-reducing effect.

[0050] In a second preferred variant of the first aspect, the sugar alcohol is threitol (a C4 sugar alcohol). Erythritol (C4 sugar alcohol), ribitol (C5 sugar alcohol), xylitol (C5 sugar alcohol), sorbitol (C 6 sugar alcohol), mannitol (C6 sugar alcohol), dulcitol (galactitol fucitol (C6 sugar alcohol), iditol (C6 sugar alcohol) alcohol), inositol (cyclic C6 sugar alcohol), volemitol (C7 sugar alcohol) ), lactitol (4-O-β-D-galactopyranosyl-D-glucitol; C12 Sugar alcohol), maltitol (4-O-α-glucopyranosyl-D-sorbitol) ;C12 disaccharide sugar alcohols) and their related enantiomers. can be.

[0051] In a more preferred version of the second variant, the sugar alcohol is threitol, erythritol , xylitol, sorbitol, mannitol, inositol, lactitol and multi Preferably the sugar alcohol is selected from one or more of mannitol, most preferably mannitol.

[0052] The sugar alcohols according to this variant of the first embodiment are thereby, apart from mannitol, in particular Thritol, erythritol, xylitol, sorbitol, inositol, lactose It has been found that tallow and maltitol have a high sebum-reducing effect.

[0053] By adding a sugar alcohol to the composition of the present invention, the sugar alcohol in the composition The total content exceeds the natural sugar alcohol content of the Tetraselmis extract present in the composition.

[0054] As a result, in the composition of the present invention thus obtained, the ratio of the total sugar alcohol content to the sugar alcohol content in the Tetraselmis extract based on the dry weight of the extract is 1.1:1 or higher , preferably 1.3:1 or higher , even more preferably 1.5:1 or more is.

[0055] Tetraselmis extract in synergistic combination with additional sugar alcohols reduces sebum production It has been found to be highly efficient in reducing the total weight of the composition. % or more, even more preferably 18% or more by weight of the total composition, and most preferably 25% or more by weight of the total composition. This was particularly effective for compositions containing a sugar alcohol, preferably mannitol, at % by weight or more. This is supported by Procedural Example 2, which describes the sebum-reducing effect of such an extract. It is attached.

[0056] Niacinamide, also known as nicotinamide, is a B vitamin with formula (II). It is a water-soluble vitamin in the vitamin B family, especially the vitamin B3 complex, and is found in food. It is used as a dietary supplement and as a cosmetic ingredient in skin and hair care. [ka]

[0057] It is a known sebum-reducing agent (ZD Draelos, et al., J. Cosmet .Laser Ther.2006,8(2),96-101), a potent anti-inflammatory and anti- Acne medication (FM Walocko, et al., Dermatol. Ther. 20 17,30(5).doi:10.1111 / dth.12481). Mido also improves the epidermal permeability barrier in vivo.

[0058] According to the present invention, a second aspect of the invention is a glycoside according to the present invention as described herein. A combination composition containing both alcohol and tetraselmis extract, and also containing niacinamide Preferably, the Tetraselmis extract as described herein is a tetraselmis extract. Cermis suecica extract.

[0059] Sugar alcohols and tetraselmis extract in combination with niacinamide are particularly effective in reducing sebum Surprisingly, the Tetraselmis extract of the present invention exhibited anti-inflammatory activity. Sugar alcohols and niacinamide together contribute to the total lipid content in the sebaceous glands, i.e. It has been found that sugar alcohols and tetrahydroxybenzoates synergistically reduce sebum levels. The enhancing effect of Selmis extract in combination with niacinamide is unexpected.

[0060] Particularly effective were the sugar alcohols and niacinamide in Tetraselmis extract. The weight ratio range of the Preferably, the ratio is 1:500 to 1:10, and most preferably 1:400 to 1:300. All combinations were calculated based on the dry weight of the extract.

[0061] Preferred are one or more sugar alcohols, tetraselmis extract, and niacinamide. a sebum-reducing composition comprising or containing the following, wherein the total amount of the final (skin care) product is The combined sugar alcohol and Tetraselmis extract are 0.01 to 3% by weight. , preferably used in an amount of 0.1 to 1% by weight, niacinamide in an amount of 0.5 to 5% by weight, Preferably, it is used in an amount of 1 to 2% by weight, calculated based on the dry weight of the extract. do.

[0062] The sugar alcohols, Tetraselmis extract, and niacin in the preparations prepared by this method It has been found that the amount of mide synergistically enhances sebum-reducing ability.

[0063] Additionally, sugar alcohols and Tetraselmis extract (preferably Tetraselmis suecica ) can be used in the form of a concentrate. Preferably, according to the third aspect of the present invention, The concentrate is 0.5 to 80% by weight of the first aspect calculated based on the dry weight of the extract. or the combination composition according to the second aspect, 0.5 to 90% by weight of water, and 0.5 ~90% by weight of a carrier and optionally 0.1-5% by weight of one or more preservatives or preservative systems Includes:

[0064] More preferably, the sugar alcohols are present in an amount of 0.5 to 30% by weight, as described above. The content of Tetraselmis extract or the combined composition is 10 to 80% by weight. A water content of 15 to 70% by weight of the carrier is more preferably used. stomach.

[0065] Preferably, the concentrate further comprises 0.1 to 5% by weight of one or more preservatives or preservative complexes. In another preferred form, the concentrate also includes a stabilizer.

[0066] Even more preferably, this amount of preservative or preservative system or stabilizer is prepared. without negatively affecting the beneficial properties of the concentrate, such as its sebum-cleansing ability. It has been shown to have a positive effect on the shelf life of extract concentrates such as It has been found that 0.5 to 2% by weight of one or more preservatives or preservative systems or The use of stabilizers.

[0067] The amount of each ingredient is determined based on whether it complies with Cosmetics Regulation 76 / 768 EEC and EU Regulation 95 / 17 EC. Preferably, the preservative is selected so as to comply with Annex 6 of Cosmetics Regulation 76 / 768 EEC. Parts A and B are employed according to the classes and compounds listed. Preservatives include benzoic acid, sodium benzoate, sorbic acid, lactic acid, potassium sorbate, phenoxyethanol, or a combination thereof. Lactic acid is preferred. Most preferred The preservative booster is preferably hydroxyacetophenone, 1 ,2-pentanediol, 1,2-hexanediol, 1,2-octanediol or However, 1,2-pentanediol is used as a secondary liquid carrier. However, even larger amounts may be used.

[0068] In the concentrate according to the third aspect of the present invention, which comprises sugar alcohols and a Tetraselmis extract (preferably Tetraselmis suecica), the ratio of the total sugar alcohol content to the sugar alcohol content in the Tetraselmis extract based on the dry weight of the extract is 1.1:1 or higher , more preferably 1.3:1 or higher , even more preferably 1.5:1 or more The sugar alcohols originally derived from the extract may be only about 11% by weight based on the dry weight of the extract. However, for the present invention, a high sugar alcohol content in the composition of 16% by weight or greater is preferred. To achieve this, sugar alcohols are added to the composition. Whether the composition is subsequently diluted or concentrated into a liquid or solid concentrate, the total sugar alcohols in either the composition or concentrate will be higher than those derived from the extract alone. Thus, the ratio of total sugar alcohol content to native sugar alcohols derived from the extract is always greater than 1:1. Thus, the above ratio distinguishes between added sugar alcohols and native sugar alcohols derived from the extract to obtain the total sugar alcohol content.

[0069] More preferably, the concentrate is either a liquid concentrate or a solid concentrate. If the product is a liquid concentrate, it should contain 1 to 70% by weight of water, more preferably 30 to 60% by weight of water. % of water.

[0070] More preferably, the concentrate comprises: (a) 0.5 to 20% by weight, preferably 0.5 to 10% by weight, of the composition of the present invention; is a combination composition; (b) 1 to 70% by weight of water; (c) 0.5 to 85% by weight of a liquid carrier, preferably glycerin; (d) a liquid concentrate optionally comprising 0.1 to 5% by weight of one or more preservatives or preservative systems. The weight ratio is calculated based on the dry weight of the Tetraselmis extract.

[0071] The concentrate is (a) 0.5 to 20% by weight (preferably 0.5 to 10% by weight) of the composition according to the present invention, or is a combination composition; (b) 40 to 65% by weight of water (c) 25 to 55% by weight of glycerin; (d) 0.1 to 1% by weight of potassium sorbate; (e) 0.1 to 1% by weight of sodium benzoate; (f) It is particularly preferred if the liquid concentrate contains 0.1 to 5% by weight of lactic acid. Weight ratios are calculated based on the dry weight of Tetraselmis extract.

[0072] In a liquid concentrate containing sugar alcohols and a Tetraselmis extract (preferably Tetraselmis suecica), the ratio of the total sugar alcohol content to the sugar alcohol content in the Tetraselmis extract based on the dry weight of the extract is 1.1:1 or higher , more preferably 1.3:1 or higher , even more preferably 1.5:1 or more is.

[0073] The liquid concentrate is preferably a fraction of the extractant after extraction and separation of the biomass from the extraction solution. Partial or complete removal and use of, for example, glycerin, propylene glycol, butyl Glycol, 1,3-propanediol, 1,2-pentanediol, 1,2-hexane a liquid carrier such as benzoyl alcohol, preferably glycerin, or a mixture of two or more thereof; and optionally with the addition of a preservative or preservative system. Such systems may optionally contain 0.1 to 5% by weight of a preservative.

[0074] It is also preferred that the concentrate (a) 1 to 30% by weight (preferably 1 to 10% by weight) of the composition or combination of the present invention a composition; (b) 0.5 to 8 wt. % water (c) a solid concentrate comprising 50 to 98% by weight of a solid carrier, preferably maltodextrin; The weight ratio is calculated based on the dry weight of the Tetraselmis extract.

[0075] In a solid concentrate containing sugar alcohols and a Tetraselmis extract (preferably Tetraselmis suecica), the ratio of the total sugar alcohol content to the sugar alcohol content in the Tetraselmis extract based on the dry weight of the extract is 1.1:1 or higher , more preferably 1.3:1 or higher , even more preferably 1.5:1 or more is.

[0076] In another preferred form, the solid concentrate includes a preservative or preservative system.

[0077] The solid concentrate may be used in the extraction and extraction solution, with or without prior partial removal of the extractant. After separation of the derived biomass and, for example, maltodextrin, dextrin or Modified starches such as cyclodextrin, lactose, modified cellulose, xanthan gum gum, gellan gum, guar gum, gum arabic, gum ghatti, gum tragacanth or laurel gums such as castor bean gum, silicon dioxide, preferably maltodextrin or After optional addition of a solid carrier such as a mixture of two or more of these, the mixture may be dried by, for example, spray drying, freeze drying or The polymer is advantageously prepared by drying using a suitable process such as vacuum drying.

[0078] The liquid or solid concentrates described above may be present in an amount of 0.0001 to 10% by weight of the final product, preferably In an amount of 0.001 to 5% by weight, most preferably 0.005 to 3% by weight, the hand of the skin and hair Use in cosmetic and / or dermatological and / or pharmaceutical products for cleaning and rinsing can be done.

[0079] These liquid or solid concentrates exhibit good storage properties, are easy to handle and administer. It has been found to be easy to use and easy to formulate.

[0080] In a further fourth aspect of the invention, particularly preferred are those for treating skin-related diseases and conditions. The composition according to the first aspect or the composition according to the second aspect, which is used as a medicament for treating A pharmaceutical composition comprising a combination composition or a concentrate according to the third aspect of the invention.

[0081] In a first preferred variant of the fourth aspect, the sugar alcohol of the pharmaceutical composition is threitol ( C4 sugar alcohol), erythritol (C4 sugar alcohol), ribitol (C5 sugar alcohol) arabitol (C5 sugar alcohol), xylitol (C5 sugar alcohol), sol Bitol (C6 sugar alcohol), mannitol (C6 sugar alcohol), dulcitol ( Galactitol (C6 sugar alcohol), fucitol (C6 sugar alcohol), iditol (C6 sugar alcohol), inositol (cyclic C6 sugar alcohol), volemitol (C7 Sugar alcohol), lactitol (4-O-β-D-galactopyranosyl-D-glucitol) C12 disaccharide sugar alcohol), maltitol (4-O-α-glucopyranosyl-D- Sorbitol (C12 disaccharide sugar alcohol) and one or more of their related enantiomers From the top, preferably threitol, erythritol, xylitol, sorbitol, mannitol and most preferably selected from one or more of: nitritol, inositol, lactitol and maltitol. Preferably, it is selected from mannitol.

[0082] In a preferred variant of the fourth aspect, the sugar alcohol, preferably mannitol, in the pharmaceutical composition The amount of thiamin is 0.0001 to 5% by weight, preferably 0.005 to 3% by weight of the total pharmaceutical composition. The quantity.

[0083] Particularly preferred are functional disorders of human hair and / or skin, seborrheic dermatitis (seborrhea) , acne vulgaris, wound healing, tissue regeneration, post-inflammatory hyperpigmentation, inflammation-related diseases, dandruff, or The compounds described herein are used as medicaments for treating or preventing tinea versicolor. The pharmaceutical composition is preferably a composition for treating tinea versicolor, which is a fungus that causes Malassezia. This is achieved by reducing

[0084] Thereby, the pharmaceutical composition as described according to the present fourth aspect can be applied to human hair and and / or to treat or prevent skin disorders, inflammation-related diseases, acne and dandruff It is further preferred that the pharmaceutical composition is used as a medicament for the treatment of a steroid or steroid-related condition, and the pharmaceutical composition is a saccharide or steroid-related condition according to the previously described embodiment. Most preferred is a combination of alcohol or sugar alcohol with niacinamide. It's nice.

[0085] Interestingly, pharmaceutical compositions, more preferably compositions according to the first inventive aspect of the present invention Alternatively, the combination composition according to the second aspect of the present invention may be used to improve the function of human hair and / or skin. Used as a drug to treat or prevent skin disorders, inflammation-related diseases, acne and dandruff This is particularly effective when

[0086] Furthermore, particularly preferred are those for treating human hair and / or skin disorders, seborrheic dermatitis ( Seborrhea), acne vulgaris, wound healing, tissue regeneration, post-inflammatory hyperpigmentation, inflammation-related diseases, dandruff or a drug for treating or preventing tinea versicolor. The treatment of tinea versicolor is preferably a combination composition as described in the literature. This is achieved by reducing the ssezia.

[0087] Even more preferred is a compound that is useful in treating hair and / or skin disorders in humans, such as acne vulgaris or Use of a compound according to the third aspect of the invention as a medicament for treating or preventing seborrheic dermatitis. Use of a Tetraselmis extract according to any one of the above-described embodiments. Most preferably, it is an extract obtained from Sueca.

[0088] In the fifth aspect, particularly preferred is one or more sugar alcohols, preferably mannitol. or a combination of one or more sugar alcohols and niacinamide.

[0089] In a preferred version of the fifth embodiment, the sugar alcohol is a C4, C5, C6, or C7 sugar alcohol. The sugar alcohols are selected from one or more of: disaccharide and disaccharide sugar alcohols. In a second preferred variant of the fifth aspect, the sugar alcohol is threitol (a C4 sugar alcohol ), erythritol (C4 sugar alcohol), ribitol (C5 sugar alcohol), arabitol C5 sugar alcohol, xylitol (C5 sugar alcohol), sorbitol (C6 sugar alcohol) Alcohol), Mannitol (C6 sugar alcohol), Durcitol (galactitol ) (C6 sugar alcohol), fucitol (C6 sugar alcohol), iditol (C6 sugar alcohol) inositol (cyclic C6 sugar alcohol), volemitol (C7 sugar alcohol), Lactitol (4-O-β-D-galactopyranosyl-D-glucitol; C12 disaccharide) Sugar alcohol), maltitol (4-O-α-glucopyranosyl-D-sorbitol; C 12 disaccharide sugar alcohols) and their related enantiomers. .

[0090] In a more preferred version of the second variant, the sugar alcohol is threitol, erythritol , xylitol, sorbitol, mannitol, inositol, lactitol and multi Preferably the sugar alcohol is selected from one or more of mannitol, most preferably mannitol.

[0091] The sugar alcohol according to the fifth aspect is therefore known to have a particularly significant sebum-reducing effect. It has been shown (see Procedure Examples 6 and 7). Furthermore, sugar alcohols have the potential to reduce sebum production. Despite its anti-aging effect, its water-holding capacity is thought to enhance epidermal skin hydration. Additionally, mannitol provides the named benefit in terms of sebum-reducing ability (see Example 4). ) as well as epidermal junctions, antimicrobial peptides, water / glycerol in the skin. Surprisingly, this effect was also seen in the gene expression of genes involved in COX-2 regulation, as well as in steroid transport. (See Procedural Example 5). In addition to the effects named above, the fifth aspect Such sugar alcohols improve the shelf life and compatibility of the composition.

[0092] According to the present invention, a third variant of the fifth aspect is provided, in particular by providing one or more of the above-described This combination of sugar alcohol and niacinamide. The combination enhances skin hydration and is particularly suitable for moisturizing the skin.

[0093] Sugar alcohols in combination with niacinamide exhibit particularly effective sebum-reducing activity Surprisingly, the combination of sugar alcohols and niacinamide Our experiments have shown that the total lipid content of the sebaceous glands, i.e., the sebum level, is highly synergistically reduced. (See Procedure Example 8.) The potentiating effect of the combination of benzodiazepines is unexpected.

[0094] Particularly effective was the combination in the composition, where sugar alcohols, preferably The weight ratio of mannitol to niacinamide ranges from 1:10,000 to 1:1. , preferably 1:2500 to 1:1, more preferably 1:500 to 1:10, and most preferably Or 1:400 to 1:300. Alternatively, niacinamide, a sugar alcohol component, The weight ratio in the pharmaceutical composition is 1:100 to 1:1, preferably 1:50 to It's 1:1.

[0095] The sugar alcohols in the preparations prepared in this way, especially mannitol, may be present. The amount of niacinamide along with the alcohol component was found to have synergistic sebum-reducing properties. It was served.

[0096] Particularly preferred are functional disorders of human hair and / or skin, seborrheic dermatitis (seborrhea) , acne vulgaris, wound healing, tissue regeneration, post-inflammatory hyperpigmentation, inflammation-related diseases, dandruff, or The compounds described herein are used as a drug for treating or preventing tinea versicolor. The treatment of tinea versicolor is preferably a drug containing Malassezia. This is achieved by reducing

[0097] Thereby, the pharmaceutical product as described by the present fifth aspect can be applied to human hair and and / or for treating or preventing skin disorders, inflammation-related diseases, acne and dandruff It is further preferred that the pharmaceutical is used as a drug, and the pharmaceutical is a sugar alcohol according to the previously described embodiment. Most preferably, the composition comprises a combination of a sugar alcohol or sugar alcohol with niacinamide.

[0098] Surprisingly, it has been found that niacinamide as described by the previous invention embodiment and one or more The combination with the above sugar alcohol is particularly preferred when the sugar alcohol contained is the first or second sugar alcohol of the present invention. If the second variant is involved, functional disorders of human hair and / or skin, acne vulgaris or is particularly effective when used as a drug to treat or prevent seborrheic dermatitis is.

[0099] In another preferred variant of the fourth or fifth aspect, a pharmaceutical composition or medicament according to the invention The amount of sugar alcohol, preferably mannitol, in the product or pharmaceutical product is Alternatively, the amount is 0.0001 to 5% by weight, preferably 0.005 to 3% by weight, of the entire pharmaceutical product.

[0100] Preferred are those consisting of one or more sugar alcohols in combination with niacinamide or It is a medicine that reduces sebum, containing sugar alcohol and niacinamide. The combination is used in an amount of 0.5 to 5% by weight based on the total weight of the final product.

[0101] Furthermore, the weight ratio range of niacinamide in the pharmaceutical composition according to the fourth aspect or The weight ratio range of niacinamide in the pharmaceutical product according to the fifth aspect is or skin dysfunction, seborrheic dermatitis (seborrhea), acne vulgaris, wound healing, tissue regeneration, inflammation Medications to treat or prevent post-symptom hyperpigmentation, inflammatory-related diseases, dandruff, or tinea versicolor 0.0001 to 5 wt.% of the total pharmaceutical composition or drug product is particularly preferably used as a pharmaceutical product. %, preferably 0.005 to 3% by weight. The treatment of tinea versicolor is preferably carried out using Malassezia (M This is achieved by reducing the amount of vasopressin (vasopressin) released from the blood.

[0102] Sugar alcohols as described in the previous aspects of the present invention can be used to treat human hair and / or is used as a drug to treat or prevent skin dysfunction, inflammation-related diseases, or acne. It has been found that the second aspect of the fourth embodiment is effective when used in the same manner. The sugar alcohols related to the above-mentioned transformations are known to cause functional disorders of human hair and / or skin, inflammation-related diseases, or It is highly preferred that the compound be used as a medicament for treating or preventing acne.

[0103] Furthermore, the present invention relates to a pharmaceutical composition according to the present invention for use in treating a skin disease. or dermatological products or therapeutic agents containing pharmaceuticals and optionally auxiliary substances.

[0104] The formulation may also contain up to 99% by weight, preferably 5 to 80% by weight, based on the total weight of the formulation. This allows the formulation of the present invention to be, for example, W / O (water-in-oil) emulsion, O / W (oil-in-water) emulsion, W / O / W (water-in-oil-in-water) emulsion Emulsions, even more preferably O / W / O (oil-in-water) emulsions .

[0105] Auxiliary substances and additives may be present in an amount of 0.1 to 99% by weight, preferably 1 to 9% by weight, based on the total weight of the formulation. It may be included in an amount of 0% by weight, preferably 60 to 80% by weight.

[0106] Auxiliary substances and / or additives include coolants, film-forming substances, antioxidants, vitamins, 2-hydroxybenzoates, hydroxycarboxylic acids, skin colorants, skin moisturizers, fats / fatty acids, waxy substances or cosmetic preparations or conventional constituents of dermatological formulations, such as alcohols, polyols, polymers, Foam stabilizer, electrolyte, organic solvent, silicone derivative or chelating agent, fragrance, foaming agent substances with anti-bacterial properties, dyes, pigments with coloring action, thickeners, surface-active substances, emulsifiers, plant parts and and plant extracts, animal extracts, propolis, proteins, protein hydrolysates and yeast extracts Preferably, the compound is selected from one or more of the following groups:

[0107] This allows the film-forming material to be, for example, polyvinylpyrrolidone or chitosan or the like. being selected from derivatives of Vitamins include, for example, vitamin C and derivatives, tocopherol and derivatives, vitamin A and derivatives thereof; The 2-hydroxycarboxylic acid may be, for example, citric acid, malic acid, L-, D- or dl- being selected from lactic acid; the skin colorant is selected from walnut extract or dihydroxyacetone; the skin moisturizer is selected from, for example, glycerol or urea; The fatty acid may be a monounsaturated or polyunsaturated fatty acid or an α-hydroxy acid or a polyhydroxy acid. hydroxy fatty acids or their derivatives, such as linoleic acid, α-linolenic acid, γ-linolenic acid, from carboxylic or arachidonic acids and their natural or synthetic esters, is selected from a combination of these subgroups, the chelating agent is selected from, for example, ethylenediaminetetraacetic acid and derivatives; The thickener may be silicon dioxide, aluminum silicate, e.g., bentonite, polysaccharides or Derivatives such as hyaluronic acid, guar gum, xanthan gum, hydroxypropyl methylcellulose, cellulose or allulose derivatives, particularly preferably polyacrylates, e.g. being selected from Lubopol or polyurethane; Plant parts and plant extracts include, for example, arnica, aloe, usnea, ivy, and iracle. , ginseng, henna, chamomile, marigold, rosemary, sage, from or containing horsetail, oats, ginger, hops, wheat or thyme The fact that the compounds are selected from these combinations means that the compounds are used as auxiliary substances and / or additives. It is particularly preferred when employed as a

[0108] In a further sixth aspect of the invention, we provide a composition or combination composition or one or more sugar alcohols, preferably mannitol, one or more sugar alcohols and niacin The present invention provides a cosmetic composition comprising a cosmetic product containing a combination of the present invention and a The composition or combination composition or concentrate or cosmetic product according to the invention, optionally containing auxiliary substances and / or and a fragrance, wherein the cosmetic composition or cosmetic is applied to human skin. and / or hair care products.

[0109] In a first preferred variant of the sixth aspect, the sugar alcohol is a C4, C5, C6, or C7 sugar alcohol. The sugar alcohol is selected from the group consisting of alcohols and disaccharide sugar alcohols.

[0110] The sugar alcohol according to the first variant of the sixth aspect thereby exhibits a particularly significant sebum-reducing effect. It has been found that it has.

[0111] In a second preferred variant of the sixth aspect, the sugar alcohol is threitol (a C4 sugar alcohol). Erythritol (C4 sugar alcohol), ribitol (C5 sugar alcohol), xylitol (C5 sugar alcohol), sorbitol (C 6 sugar alcohol), mannitol (C6 sugar alcohol), dulcitol (galactitol fucitol (C6 sugar alcohol), iditol (C6 sugar alcohol) alcohol), inositol (cyclic C6 sugar alcohol), volemitol (C7 sugar alcohol) ), lactitol (4-O-β-D-galactopyranosyl-D-glucitol; C12 Sugar alcohol), maltitol (4-O-α-glucopyranosyl-D-sorbitol) ;C12 disaccharide sugar alcohols) and their related enantiomers. can be.

[0112] In a more preferred version of the second variant, the sugar alcohol is threitol, erythritol , xylitol, sorbitol, mannitol, inositol, lactitol and multi Preferably the sugar alcohol is selected from one or more of mannitol, most preferably mannitol.

[0113] The sugar alcohol according to the second variant of the sixth aspect has a strong sebum-reducing effect.

[0114] According to the present invention, a third variant of the sixth aspect is a composition comprising one or more sugar alcohols and niacinamide. This combination with niacinamide has enhanced skin hydration. It is particularly suitable for moisturizing the skin.

[0115] Sugar alcohols in combination with niacinamide have been shown to exhibit particularly good sebum-reducing activity. Surprisingly, sugar alcohols, especially sorbitol and mannitol, and niacinamide synergistically reduce the total lipid content of the sebaceous glands, i.e., sebum levels. It was found in our experiments that the sugar alcohol reduces the amount of sugar (see Procedure Example 8). The enhancing effect of the combination of niacinamide with ethanol is unexpected.

[0116] Particularly effective are sugar alcohol to niacinamide weight ratios in the range of 1:10 000 to 1:1, preferably 1:2500 to 1:1, more preferably 1:500 to 1: 10, and most preferably 1:400 to 1:300. Alternatively, the sugar alcohol niacinamide in pharmaceutical or cosmetic compositions The weight ratio range is 1:100 to 1:1, preferably 1:50 to 1:1.

[0117] The amount of sugar alcohol and niacinamide in the formulation prepared by this method is synergistic with the sebum It was found that it has the ability to reduce

[0118] Preferably, the sebum is composed of or contains a sugar alcohol and niacinamide. In this case, the combination of sugar alcohol and niacinamide is It is used in an amount of 0.1 to 5% by weight based on the total weight of the cosmetic (skin care) product.

[0119] Further preferred are dermatological products or treatments as previously mentioned according to the present invention. wherein the amount of the composition, combination composition, or concentrate in the product is 0.0001 to 10 % by weight, preferably 0.005 to 3% by weight, or a sugar alcohol, preferably mannitol The amount of nitril is 0.0001 to 5% by weight of the total dermatological product or therapeutic agent, preferably It is 0.005 to 3% by weight.

[0120] Also preferred are cosmetic compositions or cosmetics according to the invention, wherein the product The amount of the cosmetic composition or cosmetic in the or the amount of sugar alcohol, preferably mannitol, is up to 3% by weight of the total cosmetic composition. 0.0001 to 5% by weight, preferably 0.005 to 3% by weight of the total body or cosmetic product .

[0121] Furthermore, dermatological products or therapeutic agents as previously mentioned or cosmetic compositions according to the invention In the case of cosmetics or cosmetics, the composition in the product, the combination composition, the concentrate, the cosmetic composition or the chemical The amount of cosmetic product is 0.000 of the total amount of the dermatological product or therapeutic agent or cosmetic composition or cosmetic product. 1 to 3 ppm, preferably 0.005 to 3 ppm. In the present invention, the amount of sugar alcohol, preferably mannitol, is 0.0001 to 5 ppm, preferably 0.005 to 3 ppm of the total product composition or cosmetic product m or more.

[0122] In another preferred variant, the present invention provides a method for treating, cleansing or treating the skin and / or hair. or non-therapeutic application of the cosmetic composition or cosmetic product according to the invention for the purpose of protecting Or refers to cosmetic use.

[0123] Preferably, the cosmetic composition or cosmetic product according to the invention is for the treatment of skin and / or hair. Wearable or washable products for protection, care and cleaning or as cosmetic products Preferably, the product is selected from the group of products as a flushing product, most preferably as a leave-on product.

[0124] The formulation according to the invention is preferably in the form of an emulsion.

[0125] Thus, the formulation of the present invention can be, for example, a W / O (water-in-oil) emulsion, an O / W (oil-in-water) emulsion, W / O / W (water-in-oil-in-water) emulsion, O / W / O (oil-in-water) emulsion Oil-in-water emulsion, PIT emulsion, Pickering emulsion, oil content low emulsions, microemulsions or nanoemulsions, e.g. Oils (fatty oils or fatty acid esters, especially C6-C) depending on the method and ingredients 32 -Fatty acids, C 2~C 30 -solutions, dispersions, suspensions, creams in esters or silicone oils, Lotions or milks, gels (including hydrogels, hydrodispersed gels, and oleogels), Sprays (e.g., pump sprays or propellant sprays) or cosmetic wipes foams or soaking solutions for cleaning, surfactants, e.g., soaps, synthetic surfactants, liquid Cleansers, shower and bath preparations, bath products (capsules, oils, tablets, salt, bath salts, soaps, etc.), foaming preparations, skin care products, e.g. emulsions (as described above), (as listed above), ointments, pastes, gels (as listed above), oils, balsams , serums, powders (e.g., face powders, body powders), tonics, masks, pens, sticks , roll-on, pump, aerosol (foaming, non-foaming or post-foaming), deodorant and / or antiperspirants, mouthwashes and rinses, foot care products (including keratolytics and deodorants), Insecticides, sunscreens, after-sun preparations, shaving products, after-shave balms, pre-shave and after-shave products Lotions, depilatories, hair care products, such as shampoos (two-ingredient shampoos) - Includes anti-dandruff shampoo, baby shampoo, scalp shampoo, and concentrated shampoo ), conditioner, hair tonic, hair water, hair rinse, styling cream Hair conditioners, pomades, lotions for perms and settings, hairsprays, styling aids ( For example, gel or wax), hair smoothing agents (agents that detangle hair, hair straighteners), hair dyes, such as temporary direct hair dyes and semi-permanent hair dyes , permanent hair dyes, hair conditioners, hair mousses, eye care products, cosmetics, chemicals Even more preferably, it is a makeup remover or a baby product.

[0126] The formulations according to the invention are particularly preferably in the form of emulsions, in particular W / O, O / W, W O / W, O / W / O emulsion form, PIT emulsion, Pickering emulsion emulsions, emulsions with low oil content, microemulsions or nanoemulsions gels (including hydrogels, hydrodisperse gels, and oleogels), surfactants (e.g., soaps, synthetic surfactants, liquid cleansers), solutions (e.g., tonics, facial toners or as an impregnation solution for wet tissues), sprays (e.g., pump sprays or high-pressure sprays), spray with compressed gas) or shampoo (two-ingredient shampoo, anti-dandruff shampoo) , baby shampoo, shampoo for sensitive scalp, concentrated shampoo), conditioner - in the form of a hair tonic, hair mask or hair water.

[0127] Another seventh aspect of the present invention is a cosmetic composition or cosmetic product according to the present invention for reducing sebum. This is the cosmetic use of the product.

[0128] A further eighth aspect of the present invention is a method for producing a medicament for use in a pharmaceutical composition comprising: (a) Irritation of the skin junction, (b) stimulation of antimicrobial peptides in the skin; (c) reduction of COX-2 gene expression and prostaglandin-mediated effects; (d) reduction of post-inflammatory hyperpigmentation; (e) Stimulation of filaggrin The present invention also relates to the use of a pharmaceutical composition or a medicament according to the present invention for the treatment of

[0129] Preferably, the cosmetic composition or cosmetic product according to the present invention comprises: (a) for improving the epidermal integrity of the skin, (b) To prevent external stimuli, such as air pollution or particulate matter-induced effects. For (c) To prevent skin barrier dysfunction Used cosmetically.

[0130] An even more preferred variation is one that contains one or more of the following: other sebum-reducing agents and / or anti-acne agents The pharmaceutical composition or drug or cosmetic composition or cosmetic according to the present invention further comprises do.

[0131] Alternative preferred variations are: other sebum reducing agents, anti-acne agents, anti-dandruff agents, other anti-inflammatory agents. agents, TRPV1 antagonists, antipruritic agents, antimicrobial agents, especially anti-acne agents, anti-malassezia agents A pharmaceutical composition or medicament according to the invention further comprising one or more thia fungicides.

[0132] In the formulation, sugar alcohol or sugar alcohols (of the total composition) 16% by weight or more ) and Tetraselmis extract (dried) or sugar alcohol and niacinamide, preferably mannitol, may be used in combination with other sebum-reducing and / or anti-acne agents, especially if they act via a different pathway, which would be expected to result in even more pronounced activity.Since a seborrheic condition of the skin is an ideal nutrient medium for the growth of bacteria and fungi and, consequently, for example, for the development of impure skin or acne, compositions for the prevention and / or treatment of oily skin are likewise preferred compositions for the prevention and / or treatment of impure skin or acne. Suitable active substances are, for example, retinoids such as 13-cis-retinoic acid (isotretinoin), all-trans-retinoic acid, adapalene, its salts or derivatives, androgen inhibitors such as spironolactone and cyproterone, antibiotics, preferably clindamycin, erythromycin and tetracycline, zinc or zinc salts, and antiandrogens, 5-α-reductase inhibitors, D-panthenol, α-hydroxy acids such as salicylic acid and lactic acid, pyruvic acid (α-keto acid), aliphatic dicarboxylic acids such as azelaic acid, L-carnitine, bakuchiol, 1,2-decanediol, senkyunolide-A and senkyunolide-A-containing Apium graveolens seed oil, Quillaja saponaria extract, Enantia chlorantha bark extract, Spiraea ulmaria extract, butyl avocate, vitamin B6 (also known as pyridoxine) or a salt or derivative thereof, vitamin B3 (also known as niacin or nicotinic acid) or a salt or derivative thereof, benzoyl peroxide, phloretin, Camellia sinensis extract and polyphenols contained therein, such as epigallocatechin-3-gallate, red clover (Trifolium pretense) extract, soybean (Glycine soja) seed extract, isoflavonoids or isoflavonoid-containing extracts, preferably biochanin A, genistein, daidzein, genistin and daidzin.

[0133] Preferred auxiliary substances, additives and / or activators for formulations for reducing the sebum concentration on the skin The aforementioned products, preferably in combination with the above-mentioned compound, are useful for preventing oily skin, impure skin or acne and and / or as a formulation for treatment.

[0134] We now have the ability to identify drugs and methods for treating diseases such as those described herein according to the present invention. The present invention relates to the previously described embodiments and variations thereof for use in treating skin diseases, in particular for skin disorders. Also disclosed are pharmaceutical compositions or medicaments containing the compound.

[0135] We currently have a number of compounds for use in non-therapeutic applications such as those described herein in accordance with the present invention. Also disclosed is a cosmetic composition or cosmetic product as mentioned above, in particular for skin protection. are.

[0136] Preferred cosmetic or therapeutic dermatological formulations for topical application contain the following components or the following as a whole composition: 16% by weight or more The formulations comprise one or more sugar alcohols and Tetraselmis, particularly Tetraselmis suecica, or one or more sugar alcohols or one or more sugar alcohols and niacinamide in amounts of 0.01 to 0.01%. Preferably, the sugar alcohol is mannitol, sufficient to reduce sebum levels in the skin. More preferably, the formulations contain a combination of two, three, or four active compounds.

[0137] Preferably, the active compounds are from the following groups: antiandrogens, isoflavonoid-containing extracts, Retinoids, vitamins, organic peroxides, organic ethers, organic acids or alcohols The compounds are selected from one or more of the classes of compounds in

[0138] More preferably, the active compound is 1,2-decanediol, bakuchiol, salicylic acid, acid, lactic acid, azelaic acid, retinoids, preferably 13-cis-retinoic acid (isothreonine), tinoin), all-trans-retinoic acid, adapalene, its salts or derivatives, benzoyl Peroxide, D-Panthenol, Vitamin B6 (also known as pyridoxine) or its salts, such as pyridoxine HCl or derivatives, vitamin B3 (niacin or or nicotinic acid) or its salts or derivatives, butyl avocado, Lunesol, phenoxyethanol, red clover (Trifolium preten se) extracts, isoflavonoids or isoflavonoid-containing extracts, preferably bio Okanin A, genistein, daidzein, genistin and daidzin, and antiandrogens , preferably selected from 5-α-reductase inhibitors.

[0139] Even more preferably, the one or more active compounds are 1,2-decanediol, salicylic acid , Lactic Acid, Azelaic Acid, Benzoyl Peroxide, D-Panthenol, 13-cis-Retinoic Acid retinoic acid (isotretinoin), all-trans-retinoic acid, adapalene, its salts or Derivatives, bakuchiol, erythromycin, sulfur, butyl avocate, farnesol , Phenoxyethanol, Pyridoxine HCl, Red Clover (Trifolium pretense) extract, Biochanin A, genistein, daidzein, genistin, daidzin, and 5-α-reductase inhibitors.

[0140] Even more preferably, the one or more active compounds are 1,2-decanediol, salicylic acid, benzoyl alcohol, benzoyl benzoate ... Zelic acid, benzoyl peroxide, D-panthenol, 13-cis-retinoic acid ( isotretinoin), all-trans-retinoic acid, adapalene, its salts or derivatives, Quchiol, erythromycin, butyl avocado, phenoxyethanol, pyridoxy HCl, Red Clover (Trifolium pretense) Extract, Bioka daidzein, genistein, daidzein, and 5-α-reductase inhibitors. can be.

[0141] Most preferably, the one or more active compounds are 1,2-decanediol, salicylic acid, azelaic acid, Acid, Benzoyl Peroxide, D-Panthenol, Adapalene, Bakuchiol, Erythritol From the group consisting of thromycin, butyl avocado, pyridoxine HCl and biocanin A are selected.

[0142] Additionally, it is highly preferred to include niacin as an active compound.

[0143] Preferably, one or more active compounds are combined with an anti-dandruff active. If they act through different biological pathways, a more pronounced overall effect may be found. Antidandruff agents include azoles, such as climbazole, ketoconazole, itraconazole, hydroxypyridones such as octopyrrole, econazole and elubiol; (piroctone olamine), ciclopirox, rilopirox and MEA-hydro hydroxyoctyloxypyridinone; keratolytic agents such as salicylic acid and other hydroxypropyl ... acids; strobilurins such as azoxystrobin and metal chelating agents such as 1,10-phenanthroline, Good too.

[0144] In embodiments, the azole antimicrobial agent is a benzimidazole, a benzothiazole, a biphenyl, butaconazole nitrate, climbazole, clotrimazole, cloconazole le, eberconazole, econazole, elubiol, fenticonazole, fluconazole flutimazole, isoconazole, ketoconazole, lanoconazole, metronidazole azole, miconazole, neticonazole, omoconazole, oxiconazole nitrate, sebenzyl nitrate Rutaconazole, sulconazole nitrate, tioconazole, thiazole, and mixtures thereof The azole antimicrobial is an imidazole selected from the group consisting of terco a triazole selected from the group consisting of benzodiazepine, benzocaine, benzotriazole ... is.

[0145] In an embodiment, preferred anti-dandruff agents are present in an amount of 0.1% to 10% by weight. In some embodiments, the amount is from 0.25% to 8% by weight, and in yet further embodiments, from 0.5% to 6% by weight. It may be present in an amount of % by weight.

[0146] The compositions and products of the present invention comprise a sugar alcohol and a Tetraselmis extract, or one or more The above sugar alcohols, either by themselves or in combination with niacinamide, also include: Preferably, the active ingredient is an agent that inhibits acne-related P. acnes and / or dandruff. COX-2 / PGE2 and related Malassezia sp. and / or act via a different pathway than anti-acne and / or antimicrobial agents, May be combined with anti-inflammatory or anti-irritant agents. Intended for use on oily skin or sensitive oily skin with acne or sensitive oily scalp or dandruff If so, these combinations are particularly beneficial.

[0147] The compositions and products of the present invention contain anti-inflammatory ingredients and / or ingredients that improve redness and / or itching. In particular, the composition may contain an active ingredient having an anti-inflammatory effect or an active ingredient that relieves redness and itching. It is advantageously used as a component of anti-inflammatory drugs, the list of which can be expanded by the addition of other steroidal anti-inflammatory drugs. Hydrocortisone, dexamethasone, dexamethasone phosphate, methyl A corticosteroid-type steroid selected from the group consisting of prednisolone, or cortisone. Non-steroidal anti-inflammatory agents may also be used. Examples that can be cited here are oxicams, such as piroxicam or tenoxicam. xicam; salicylates, such as aspirin, disalcid, solprin or phen Dosal; acetic acid derivatives, such as diclofenac, fenclofenac, indomethacin , sulindac, tolmetin or clindanac; fenamates, for example, mefena meclofenamic, flufenamic, or niflumic; propionic acid derivatives ibuprofen, naproxen, benoxaprofen or pyrazoles , for example, phenylbutazone, oxyphenylbutazone, febrazone or azapro Anthranilic acid derivatives, in particular those described in WO2004047833A1, Avenanthramide, which is present in the present invention, is a preferred anti-itch ingredient in the compositions of the present invention.

[0148] Also useful are natural or naturally occurring mixtures of anti-inflammatory / anti-irritant substances. or a mixture of substances that relieve inflammation and / or redness and / or itching, in particular chamomile Aloe vera, Commiphora species, Rubia species, willow, willow- Herbs, oats, calendula, arnica, St. John's wort, honeysuckle La, rosemary, Passiflora incarnata, witch hazel, ginger or Echinacea; preferably chamomile, A. Loe vera, oat, calendula, arnica, honeysuckle, rosemary extracts or fractions derived from Lee, Witch Hazel, Ginger or Echinacea, and / or pure substances, natural α-bisabolol, synthetic bisabolol, apigenin, api Genin-7-glucoside, gingerol, shogaol, gingerdiol, dehydrogenase Gingerion, paradols, especially natural or synthetic 6-paradol, naturally occurring avenanthramides, preferably avenanthramide A, avenanthramide B, avenanthramide Avenanthramide C, Avenanthramide D, Avenanthramide E, Non-natural or non-naturally occurring Avenanthramide, preferably dihydroavenanthramide D, dihydroavenanthramide E, tranilast, boswellic acid, phytosterol, glycyrrhizin, glabridin, sclareolide and licochalcone A; preferably the naturally occurring α- Bisabolol, synthetic bisabolol, natural avenanthramide, non-natural avenanthramide dihydroavenanthramide D (described in WO2004047833A1) (such as), ginger extract, gingerol, shogaol, gingerdiol, Dehydrogingerione, paradols, especially natural or synthetic 6-paradol, bos valeric acid, phytosterols, glycyrrhizin, and licorice A, and / or Lanthin, sclareolide, panthenol, (pseudo-)ceramide [preferably ceramide 2 , Hydroxypropyl Bispalmitamide M EA, Cetyloxypropyl Glyceryl Methacrylate N-(l-hexadecanoyl)-4-hydroxy-L-propyl myristamide Phosphorus (1-hexadecyl) ester, hydroxyethyl palmityloxyhydroxypropyl pyrpalmitamide], phytosterols, chitosan, and beta-glucans, especially oat The glucan is selected from the group consisting of 1,3-1,4-glucans derived from

[0149] The total amount of anti-irritant or anti-inflammatory substance in the formulation or product according to the invention is preferably are each 0.0001 to 20% by weight based on the total weight of the formulation or product, preferably The range is 0.0001 to 10% by weight, particularly 0.001 to 5% by weight.

[0150] Transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist Gonist

[0151] Suitable compounds that can be combined with the products of the present invention are TRPV1 antagonists These are based on the effects of reducing the hypersensitivity of the skin nerves, Preferably, a transformer such as that described in WO2009087242A1 is used. -4-tert-butylcyclohexanol, or TRPV via μ-receptor activation 1, indirect modulators of acetyl tetrapeptide-15. do.

[0152] The overall composition of the formulation of the present invention 16% by weight or moreThe sugar alcohol and Tetraselmis extract (preferably Tetraselmis suecica) in an amount of 0.01 to 0.01, or one or more sugar alcohols by themselves, such as mannitol, or one or more sugar alcohols and niacinamide, may also be used in combination with an anti-dandruff agent. Suitable anti-dandruff agents include piroctone olamine (1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)-2-(1H)-pyridinone monoethanolamine salt), bipival (climbazole), Ketoconazol® (2RS,4SR)-1-(4-{4-[-2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-ylmethoxy]phenyl}piperazin-1-yl)ethanone, ketoconazol® ... The active ingredients are: elubiol, selenium disulfide, colloidal sulfur, sulfur polyethylene glycol sorbitan monooleate, sulfur ricinol polyethoxylate, sulfur tal distillate, salicylic acid (or in combination with hexachlorophene), undecylenic acid, sulfosuccinic acid monoethanolamide sodium salt, Ramepon S (protein / undecylenic acid condensate), zinc pyrithione, aluminum pyrithione, and magnesium pyrithione / dipyrithione magnesium sulfate.

[0153] Further preferred cosmetic formulations for topical application comprise or consist of the following components: - Preferably the sugar alcohol is mannitol, in an amount sufficient to reduce the sebum concentration in the skin, of the entire composition 16% by weight or more Sugar alcohols and Tetraselmis extract (preferably Tetraselmis suecica) 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or more, preferably 2 or more, more preferably 3 or more cleaning adjuvants; - optionally one or more further auxiliary substances and / or additives. Such cosmetic formulations are particularly suitable for cleansing greasy, oily and / or impure skin.

[0154] Another preferred cosmetic formulation for topical application comprises or contains the following components: Consists of: - Niacinamide and one or more sugar alcohols sufficient to reduce the sebum concentration in the skin, Preferably mannitol, - 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or more, preferably 2 or more, more preferably or 3 or more cleaning aids; - optionally one or more further auxiliary substances and / or additives. Such cosmetic preparations have a particularly long shelf life.

[0155] Even more preferred cosmetic formulations for topical application include or comprise the following components: It consists of: one or more sugar alcohols, preferably mannitol, sufficient to reduce the sebum concentration in the skin Lu, - 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or more, preferably 2 or more, more preferably or 3 or more cleaning aids; - optionally one or more further auxiliary substances and / or additives. Such cosmetic preparations have particularly good availability.

[0156] The formulations include the sugar alcohol of the present invention together with Tetraselmis extract, or niacin. one or more sugar alcohols, preferably mannitol, with amides, or one or more sugar alcohols ethanol, preferably mannitol, itself an additional topical agent, particularly a film-forming agent, which protects the skin. They may also be combined with film-forming agents to provide a physical barrier. This will enhance the epidermal integrity improving effect of extracts such as PM. It has been shown that external stimuli increase sebum production, leading to barrier dysfunction, especially It is beneficial.

[0157] Typical film-forming agents include, for example, chitosan, microcrystalline chitosan, quaternized chitosan, polyvinyl alcohol, and the like. vinylpyrrolidone, vinylpyrrolidone / vinyl acetate copolymer, acrylic acid series polymers , quaternary cellulose derivatives, collagen, hyaluronic acid and its salts, 1, derived from oat 3-1,4-glucan or 1,3-1,6-glucan derived from yeast or mushrooms β-glucans and similar compounds.

[0158] Both sugar alcohols and niacinamide are colorless and odorless compounds; Its high water solubility allows for wide application in various types of cosmetic formulations. Alcohol and niacinamide are solids that are usually available in powder form.

[0159] In order to formulate the pharmaceutical composition or cosmetic composition or drug or cosmetic according to the present invention, To more easily synergistically combine them for this purpose, they are used in a liquid carrier system. To prepare such a liquid formulation of alcohol and niacinamide, the solid ingredients, i.e. That is, sugar alcohol and niacinamide are mixed in a liquid carrier system at room temperature (20-30°C) under stirring. The liquid carrier is preferably glycerin, 1,3-butylene, or the like, to give a colorless solution. glycol, 1,3-propanediol, 1,2-pentanediol or water or A mixture of these is used.

[0160] Thus, in a still further aspect, the present invention provides a pharmaceutical or cosmetic composition according to the invention. one or more sugar alcohols used in the preparation of pharmaceuticals or cosmetics; Liquid formulations containing a combination of one or more sugar alcohol(s) and niacinamide do.

[0161] In particular, such liquid formulations (a) 0.5 to 25% by weight, preferably 1 to 20% by weight, of a sugar alcohol; (b) optionally 1 to 35% by weight, preferably 2 to 20% by weight, of niacinamide; (c) 5 to 55% by weight, preferably 10 to 50% by weight, of a liquid carrier; (d) optionally 0.1 to 5% by weight of one or more preservatives or preservative systems.

[0162] Particularly preferred are: (a) Mannitol, sorbitol, xylitol, erythritol, maltitol, 1 to 20% by weight of a sugar alcohol selected from inositol and mixtures thereof; (b) optionally 2 to 20% by weight of niacinamide; (c) Glycerin, 1,3-butylene glycol, 1,3-propanediol, 1,2- 10 to 50% by weight of a liquid carrier selected from pentanediols and mixtures thereof; (d) optionally 0.1 to 5% by weight of one or more preservatives or preservative systems. is.

[0163] The composition of the liquid formulation is set forth in Table 9 below.

[0164] One or more sugar alcohol(s) or one or more sugar alcohol(s) and niacin Liquid formulations containing the amide combination are suitable for use in pharmaceutical, cosmetic or dermatological preparations according to the present invention. Used in the preparation of pharmaceutical or therapeutic drugs. [Example]

[0165] Experimental Section

[0166] Example 1: Preparation of Tetraselmis suecica extract

[0167] 3 g of freeze-dried Tetraselmis suecica biomass was mixed with 30 g of water. The mixture was stirred at 80°C for 2 hours. The liquid extract was separated from the biomass, and the extracted biomass was added with 3 0 g of water was added and the mixture was stirred for an additional 2 h at 80°C. The extracts were separated from the oat mass, and both extract solutions were combined and the water was removed by freeze-drying. Three different batches of biomass were performed.

[0168] For comparison, the aqueous extract described in US2010143267A1 was added to the same three It was prepared from a batch of biomass and the water was removed by freeze-drying. [Table 1]

[0169] Heated extractions have comparable, if not slightly higher, extraction yields compared to room temperature extractions. However, surprisingly, a much lighter extract was obtained, which was It is particularly advantageous for use as a cosmetic ingredient as consumers prefer less pigmented products. The treatment has the added benefit of inactivating enzymes in the biomass, which It is particularly advantageous if viable or non-inactivated biomass is used. This is particularly challenging for extraction with water at low temperatures or with extractant systems with high water content. Microbial contamination by certain bacteria, fungi or yeasts can be eliminated by extraction at high temperatures (>50°C). and is prevented. [Table 2]

[0170] Example 2: Preparation of liquid form of Tetraselmis suecica extract

[0171] 4.6 g of Tetraselmis suecica extract obtained by extraction at 80 °C according to Example 1 The dry matter of the product was mixed with 97g of water, 46g of glycerin, 18% by weight of mannitol, and 0.5g of glycerin. % sodium benzoate and 0.2% potassium sorbate (both by total weight of the liquid mixture) (based on) and adjust the pH of the mixture to 4.5 with the help of lactic acid. A light brown solution was obtained.

[0172] Example 3: Effect of Tetraselmis suecica extract (dried) on the total lipid content of ex vivo human sebaceous glands The effect of dried

[0173] Organ culture of human sebaceous glands finely dissected from human skin explants was performed as described in Example 1. The regulatory activity of Tetraselmis suecica extract prepared according to the method described in [1] on sebum levels was evaluated. The extract is employed in dry form.

[0174] After removing the epidermis of the full-thickness skin samples, carefully remove the sebaceous glands using fine scissors and a scalpel. The finely dissected sebaceous glands were then pooled into groups of eight and placed in 500 μL of modified Wiley®. The cells were cultured in 24-well plates in Illiam's E medium for up to 6 days. After 3 days of culture, the culture medium was changed and replaced with medium containing the extract to be investigated. The medium was refreshed on day 6. Glands were harvested on day 6 and used for lipid and protein quantification. To equate the estimated productivity of glands that vary in biomass, we estimated their total sebum content. , divided by the protein extracted from the glandular tissue, and the ratio between the produced sebum and tissue protein was calculated. (i.e. mg lipid / mg protein) was obtained.

[0175] To do this, the sebaceous glands were homogenized in 100 μL of isopropyl alcohol. After centrifugation, the lipids were extracted and the proteins were insoluble. The supernatant was collected and analyzed. The remaining pellet was dried using a vacuum dry evaporator. The cells were then dissociated in the presence of 50 μL of protein lysis buffer. After the time, the extraction mixture was centrifuged and the supernatant was collected and analyzed. Infrared spectroscopy using a Millipore The dissolved lipids and proteins dissolved in the dissolution buffer were quantified. Total lipids were obtained by normalizing the lipids quantified in the above manner (i.e., mg lipid / tan Normalized lipids produced by each group of sebaceous glands from the treatment groups. That is, the amount of sebum was compared with that of the untreated control group, and the regulating activity was calculated as a ratio. As a control, 5 μM capsaicin treatment was included in the experimental setup. Capsaicin inhibits sebum production. It is an active ingredient of chili peppers suitable for treating rheumatoid arthritis [Toth et al., J. Invest. Derm. (2009), 129:329-339]. For statistical analysis, Differences between groups were confirmed by one-way analysis of variance followed by Dunnett's permutation test. The differences were evaluated.

[0176] To better understand the response to the extract, viability was assessed at days 1 and 6 of organ culture. Resazurin was added to the wells (1:11) and incubated for 2 hours. At the end of the incubation, an equal volume of medium was measured in a fluorometer (excitation: 560 nm, emission: 590 nm). To eliminate residual resazurin, the medium was then placed in normal medium for 2 hours. After this, the medium was replaced again with medium containing the test sample. Survival was measured as the difference in ratio between day 6 and day 1.

[0177] To assess donor responsiveness and inter-individual variability, skin samples from three different donors were used. The extract was tested on sebaceous glands obtained from In this cell test, biological tests are performed in vitro and in vitro, and generally, Tetracell By using a dried form of the extract, side effects arising from the solvent, glycerin or preservative system can be prevented. Avoid use. [Table 3]

[0178] The results were obtained by extracting Tetraselmis suecica water extract (dried) at 80 °C. Surprisingly, the normalized total volume of human sebaceous glands was significantly increased without affecting their viability. It has been shown to be a highly effective reducer of lipid, i.e., sebum content. It is more effective than its rival, capsaicin, even at concentrations five times lower. Sebaceous glands from all human donors responded to the extract (donor responsiveness: 100%).

[0179] A similar effect was observed with mannitol and Tetraselmis extract as prepared according to Example 2. This was also achieved by comparing the combination of mannitol and Tetraselmis suae. Combination with deer water extract (dried) was shown to inhibit the growth of rhesus monkeys without affecting their viability. It is a particularly highly effective reducer of the normalized total lipids of the sebaceous glands, i.e., sebum. is more effective than the positive control, capsaicin. The addition of this product shows a good skin moisturizing effect.

[0180] Example 4: Effect of mannitol (alone) on the total lipid content of human sebaceous glands in vitro

[0181] Organ culture of human sebaceous glands, finely dissected from human skin explants, was performed to assess the effect of sebum levels. The regulatory activity of mannitol was evaluated.

[0182] After removing the epidermis of the full-thickness skin samples, carefully remove the sebaceous glands using fine scissors and a scalpel. The finely dissected sebaceous glands were then pooled into groups of eight and placed in 500 μL of modified Wiley®. The cells were cultured in 24-well plates in Illiam's E medium for up to 6 days. After 3 days, the culture medium was changed and replaced with medium containing the sample to be examined. The medium was refreshed every 6 days. On day 6, the glands were harvested and used for lipid and protein quantification. To equate the estimated productivity of glands that vary in biomass, their total sebum content was estimated. Divide by the protein extracted from the glandular tissue to determine the ratio between the produced sebum and tissue protein ( i.e. mg lipid / mg protein) was obtained.

[0183] To do so, homogenize each sebaceous gland group in 100 μL of isopropyl alcohol. After centrifugation, the lipids were extracted and the proteins were insoluble. The supernatant was collected and analyzed. The remaining pellet was dried using a vacuum dry evaporator. The cells were then dissociated in the presence of 50 μL of protein lysis buffer. After this time, the extraction mixture was centrifuged and the supernatant was collected and analyzed by direct detection IR spectroscopy. Infrared spectroscopy using a chromatograph (Millipore) determined that isopropyl alcohol The dissolved lipids and proteins dissolved in the lysis buffer were quantified. The total amount of lipid was obtained by normalizing the quantified lipids (i.e., mg of lipid / tablet). Normalized lipids produced by each group of sebaceous glands from the treatment groups. That is, the amount of sebum was compared with that of the untreated control group, and the regulating activity was calculated as a ratio. As a control, 5 μM capsaicin treatment was included in the experimental setup. Capsaicin inhibits sebum production. It is the active ingredient in chili peppers that is suitable for damaging the Derm. (2009), 129:329-339]. For statistical analysis, One-way ANOVA with a variance test followed by Dunnett's permutation test confirmed the intergroup differences. The differences were assessed.

[0184] To better understand the response to the extract, viability was assessed at days 1 and 6 of organ culture. Resazurin was added to the wells (1:11) and incubated for 2 hours. At the end of the incubation, an equal volume of medium was measured in a fluorometer (excitation: 560 nm, emission: 590 nm). To eliminate residual resazurin, the medium was then placed in normal medium for 2 hours. After this, the medium was replaced again with medium containing the test sample. Survival was measured as the difference in ratio between day 6 and day 1.

[0185] [Table 4]

[0186] The results surprisingly showed that mannitol significantly reduced the lipid content of human sebaceous glands in vitro. It clearly shows that.

[0187] According to Example 1, the water extract of Tetraselmis suecica (dried) had a concentration of 11.8±0 Contains 0.9% by weight of mannitol. The extract significantly reduces the total lipid content at 0.3 ppm. and was consistently more effective than 5 μM capsaicin when tested in three separate experiments ( Example 3).

[0188] 0.03 ppm of mannitol was added to 0.3 ppm of Tetraselmis suecica water extract ( The mannitol content of 0.03 ppm corresponds to the mannitol content of the skin. It significantly reduced the fat content, but was less effective than 5 μM capsaicin. Mannitol is one of the active ingredients in Tetraselmis suecica extract. However, this indicates that it is not entirely responsible for the observed sebum-reducing effect of the extract. Other extract components may additively or synergistically enhance the observed sebum-reducing efficacy of the extract. Strengthen the system.

[0189] Example 5: Effect of mannitol on gene expression of claudin-7 EpiLife medium containing HKGS kit (Gibco) according to the supplier's instructions Neonatal human epidermal keratinocytes (nHEK) were cultured in a Gibco culture medium at 5% CO2 and 37°C. Ta.

[0190] 0.025% Tetraselmis tetracycline obtained according to Example 1 by extraction at 80 °C The cells were treated with the water extract of Sueca or medium as a solvent control for 24 hours. The expression levels of the target genes in the genome of the cells treated with the extracts were analyzed by RT-qPCR. and measured.

[0191] RNA isolation was performed using the RNeasy® Mini Kit, Qiagen By measuring the absorbance at 260 nm, the μCuvette G1.0 and BioP Total RNA concentration was measured using a thermometer (Eppendorf). Purity control values ​​such as E280 and E260 / 230 were calculated simultaneously. Therefore, the high-performance RNA-to-cDNA kit, Applied Biosystems Reverse transcription was performed using the PCR thermocycler Biometra. Ta.

[0192] For rapid real-time PCR, use RNase-free water and TaqMan™ Fast Universal PCR Master Mix, Applied b cDNA was diluted with StepOne Plus Fast Reagents. al Time PCR Instrument, Applied biosystem Quantitative real-time PCR was performed using StepOne software and 2 -ΔCT method (normalized to the expression of endogenous control HTRP1).

[0193] Regarding upregulation 2.0 or higher Regarding RG values ​​and downregulation of Less than 0.5 RQ values ​​of are considered appropriate. [Table 5]

[0194] The results showed that mannitol alone or in combination with Tetraselmis extract containing mannitol Surprisingly, the combination also upregulated the claudin 7 gene, which is involved in tight junctions. This indicates that

[0195] Furthermore, proteins involved in tight junctions, such as claudin 1, occludin or cingulin Other genes, such as phosphorus, were also found in combination with Tetraselmis extract containing mannitol. Therefore, the effects of treatment with Tetraselmis extract on the expression of mannitol and mannitol are synergistically upregulated. The differential effect of treatment with nitrite is shown.

[0196] Example 6: Effect of erythritol, xylitol, and erythritol on the total lipid content of ex vivo human sebaceous glands The effects of sorbitol

[0197] Human sebaceous gland organs microdissected from human skin explants as described in Example 4 Cultivation produces erythritol (C4 sugar alcohol) and xylitol (C5 sugar alcohol). The sebum level-regulating activity of sorbitol (C6 sugar alcohol) was evaluated. Capsaicin from M was examined in parallel as a reference / positive control. [Table 6]

[0198] The results showed that erythritol, xylitol, and sorbitol surprisingly inhibited in vitro hives. All three sugar alcohols have been shown to reduce the lipid content of the sebaceous glands. More active than the positive control / reference capsaicin.

[0199] None of the test samples had any significant effect on sebaceous gland viability.

[0200] Example 7: Effect of threitol, inositol, and lactose on the total lipid content of ex vivo human sebaceous glands Effects of maltitol and maltitol

[0201] Human sebaceous gland organs microdissected from human skin explants as described in Example 4 Culture was performed to detect threitol, inositol, lactitol, and maltitol in the sebaceous gland. The modulatory activity against the bell was evaluated. 5 μM capsaicin was administered in parallel as a reference / positive control. I looked it up. [Table 7]

[0202] The results showed that threitol, inositol, lactitol, and maltitol were surprisingly The results clearly show that the four sugars significantly reduce the lipid content of human sebaceous glands in vitro. All of the alcohols are more active than the positive control / reference capsaicin.

[0203] None of the test samples had any significant effect on sebaceous gland viability.

[0204] Example 8: Effect of sugar alcohols and niacinamide on the total lipid content of ex vivo human sebaceous glands Synergy

[0205] The synergistic activity of sugar alcohols was investigated using the same experimental setup as described in Example 4. Combinations of niacinamide were evaluated. 5 μM capsaicin was used as a reference / positive control. were investigated in parallel.

[0206] The synergy index (SI) is calculated using the Kull equation: SI=C×D / A+C×E / B was used, At that time, A = lipid reduction by sorbitol at concentration x B = lipid reduction by niacinamide at concentration y C = combination of sorbitol at concentration x / 2 and niacinamide at concentration y / 2 Lipid reduction D = coefficient ≥ 0.5 for sorbitol (due to half the concentration tested in the combination) E = ≥ 0.5 for niacinamide (due to half the concentration tested in combination) coefficient.

[0207] For additive activity of two combined components, SI=1 is obtained, whereas S<1 is Antagonistic activity (observed efficacy is less than additive), SI > 1 indicates synergistic activity (observed efficacy is less than additive). The results of this experiment are summarized in Table 8. [Table 8]

[0208] SI=15×0.5 / 11+15×0.5 / 2=4.43

[0209] The resulting SI of 4.43 indicates that the combination of sugar alcohol and niacinamide is surprising. The results showed that the total lipid content of human sebaceous glands, i.e., sebum levels, was highly synergistically reduced. It is clearly proven.

[0210] Niacinamide alone does not exhibit relevant lipid-lowering activity when tested in human sebaceous glands in vitro. Sorbitol showed efficacy in the expected range compared to capsaicin. The combination led to unexpectedly strong enhanced efficacy.

[0211] Cosmetic ingredients ideally have no color or odor of their own, so that the final cosmetic It has no effect of its own on the appearance and odor of the formulation. Both amides are colorless and odorless compounds; moreover, they are both readily soluble in water and can be found in a variety of species. This allows for a wide range of applications in cosmetic formulations.

[0212] Additionally, sugar alcohols and niacinamide are solids that are usually available in powder form. To make synergistic combinations even easier to formulate typical cosmetic formulations, These can be used in liquid carrier systems. To prepare a liquid combination, a solid The ingredients, namely sugar alcohol and niacinamide, are mixed at room temperature (20-30°C) under stirring. The mixture is dissolved in the liquid carrier at 70° C. to give a colorless solution. [Table 9]

[0213] The liquid formulation may further contain 0.1 to 5% by weight of one or more preservative(s) or preservative system. may include:

[0214] One or more sugar alcohol(s) or one or more sugar alcohol(s) and niacin The liquid formulation containing the combination of the amide and the pharmaceutical or cosmetic or dermatological preparation according to the present invention is Used in the preparation of products or therapeutic agents.

[0215] Example 9: Formulation Examples

[0216] In formulations 1 to 22, the following two perfume oils, PFO1 and PFO2, were used as fragrances. (DPG = dipropylene glycol) was used. [Table 10] [Table 11] [Table 12-1] [Table 12-2] [Table 12-3]

Table 12-4

Table 12-5

Table 12-6

Table 12-7

Table 12-8

Table 12-9

Table 12-10

Table 12-11

Table 12-12

Table 12-13

Table 13-1

Table 13-2

Table 13-3

Table 13-4

Table 13-5

Table 13-6

Table 13-7

Table 13-8

Table 13-9

Table 13-10

Table 13-11

Claims

1. 1. A composition comprising sugar alcohols and a Tetraselmis suecica extract, wherein the total content of the sugar alcohols is 16% or more by weight based on the dry weight of the composition, and the Tetraselmis suecica extract has the following compositional values ​​based on the dry weight of the extract: (a) 10% by weight or more of total minerals in the Tetraselmis suecica extract; (b) 3% or more by weight of total galactose in the Tetraselmis suecica extract; (c) 4% or more by weight of total glucose of the Tetraselmis suecica extract; (d) 3% by weight or more of total amino acids in the Tetraselmis suecica extract; (e) 2% or more by weight of total nitrogen of the Tetraselmis suecica extract; The composition, wherein the Tetraselmis suecica extract is obtained by extracting Tetraselmis suecica cells with a liquid extractant consisting of water at a temperature above 60°C.

2. 2. The composition of claim 1, wherein the sugar alcohol is selected from one or more of a C4, C5, C6, C7 sugar alcohol and a disaccharide sugar alcohol.

3. 3. The composition of claim 1, wherein the sugar alcohol is selected from one or more of threitol (a C4 sugar alcohol), erythritol (a C4 sugar alcohol), ribitol (a C5 sugar alcohol), arabitol (a C5 sugar alcohol), xylitol (a C5 sugar alcohol), sorbitol (a C6 sugar alcohol), mannitol (a C6 sugar alcohol), dulcitol (galactitol) (a C6 sugar alcohol), inositol (a cyclic C6 sugar alcohol), volemitol (a C7 sugar alcohol), lactitol (4-O-β-D-galactopyranosyl-D-glucitol; a disaccharide sugar alcohol), maltitol (4-O-α-glucopyranosyl-D-sorbitol; a disaccharide sugar alcohol) and their associated enantiomers.

4. 1. A composition, which is a cosmetic or pharmaceutical composition, comprising sugar alcohols and a Tetraselmis suecica extract, wherein the total content of the sugar alcohols is in an amount of 16% by weight or more based on the dry weight of the composition, and the Tetraselmis extract has the following content based on the dry weight of the extract: (a) 10% by weight or more of total minerals in the Tetraselmis suecica extract; (b) 3% or more by weight of total galactose in the Tetraselmis suecica extract; (c) 4% or more by weight of total glucose of the Tetraselmis suecica extract; (d) 3% by weight or more of total amino acids in the Tetraselmis suecica extract; (e) 2% or more by weight of total nitrogen of the Tetraselmis suecica extract; The Tetraselmis suecica extract is obtained by extracting cells of Tetraselmis suecica with a liquid extractant consisting of water at a temperature above 75°C; the Tetraselmis suecica extract has a total arginine content, which is the sum of free arginine and bound arginine, of between 0.6 and 1.0% by weight of the total composition based on the dry weight of the extract; A composition, wherein the ratio of the total sugar alcohol content based on the dry weight of the composition to the sugar alcohol content in the Tetraselmis suecica extract is 1.1 or more.

5. A combination composition comprising the composition according to any one of claims 1 to 4 and further comprising niacinamide.

6. 6. The combination composition according to claim 5, wherein the weight ratio of the sugar alcohol and Tetraselmis suecica extract combined to niacinamide ranges from 1:10,000 to 1:1, calculated based on the dry weight of the extract.

7. (a) 0.5 to 80% by weight, calculated on the dry weight of the concentrate, of the composition according to any one of claims 1 to 4 or the combination composition according to claim 5 or 6; (b) 0.5 to 90 wt. % water; (c) 0.5 to 90 wt. % of a carrier; A concentrate comprising: The concentrate, wherein the ratio of the total sugar alcohol content based on the dry weight of the composition to the sugar alcohol content in the Tetraselmis suecica extract is 1.1 or more.

8. (a) 0.5 to 10% by weight, calculated based on the weight of the liquid concentrate, of the composition according to any one of claims 1 to 4 or the combination composition according to claim 5 or 6; (b) 1 to 70 wt. % water; (c) 0.5 to 85 wt. % of a liquid carrier; A liquid concentrate comprising: The liquid concentrate, wherein the ratio of the total sugar alcohol content based on the dry weight of the composition to the sugar alcohol content in the Tetraselmis suecica extract is 1.1 or more.

9. (a) 1 to 10% by weight, calculated on the dry weight of the solid concentrate, of the composition according to any one of claims 1 to 4 or the combination composition according to claim 5 or 6; (b) 0.5 to 10 wt. % water; (c) 50 to 98 wt. % of a solid carrier; A solid concentrate comprising: The solid concentrate, wherein the ratio of the total content of sugar alcohols based on the dry weight of the composition to the sugar alcohol content in the Tetraselmis suecica extract is 1.1 or more.

10. A pharmaceutical composition comprising the composition of any one of claims 1 to 4 or the combination composition of claim 5 or 6 or the concentrate of any one of claims 7 to 9 for use as a medicament for treating or preventing functional disorders of human hair and / or skin, skin diseases, seborrheic dermatitis, acne vulgaris, wound healing, tissue regeneration, post-inflammatory hyperpigmentation, inflammation-related diseases, dandruff, or tinea versicolor.

11. The pharmaceutical composition according to claim 10, wherein the sugar alcohol is present in an amount of 0.0001 to 5% by weight of the total pharmaceutical composition.

12. A therapeutic agent for use in treating a skin disorder, comprising the pharmaceutical composition of claim 10 or 11.

13. The therapeutic agent according to claim 12, The therapeutic agent, wherein the amount of the composition according to any one of claims 1 to 4, the combination composition according to claim 5 or 6, or the concentrate according to any one of claims 7 to 9 in the product is 0.0001 to 10% by weight of the total amount of the therapeutic agent, or the amount of the sugar alcohol is 0.0001 to 5% by weight of the total amount of the therapeutic agent.

14. A cosmetic composition comprising a composition according to any one of claims 1 to 4, a combination composition according to claims 5 or 6, or a concentrate according to any one of claims 7 to 9, The cosmetic composition, wherein the cosmetic composition is a skin and / or hair care product.

15. The cosmetic composition according to claim 14, wherein the amount of the composition according to claims 1 to 4, the combination composition according to claims 5 or 6, or the concentrate according to claims 7 to 9 is 0.0001 to 10% by weight of the total cosmetic composition, or the amount of the sugar alcohol is 0.0001 to 5% by weight of the total cosmetic composition.

16. Use for the manufacture of a cosmetic composition according to claim 14 or 15 for application in caring for, cleaning or protecting the skin or for reducing sebum.

17. (a) skin junction irritation; (b) stimulation of antimicrobial peptides in the skin; (c) reducing COX-2 gene expression and prostaglandin-mediated effects; (d) reduction of post-inflammatory hyperpigmentation, or (e) Stimulation of filaggrin 14. The pharmaceutical composition according to claim 10 or 11 for the treatment of a rheumatoid arthritis or the use thereof for the manufacture of a therapeutic agent according to claim 12 or 13.

18. (a) for improving the epidermal integrity of the skin, (b) to protect against external stimuli, or (c) to prevent skin barrier dysfunction, Use for the preparation of a cosmetic composition according to claim 14 or 15.

19. 16. The pharmaceutical composition of claim 10 or 11, or the therapeutic agent of claim 12 or 13, or the cosmetic composition of claim 14 or 15, further comprising an additional sebum-reducing agent.

20. Additionally: Anti-acne agents, anti-dandruff agents, anti-inflammatory agents, TRPV1 antagonists, Antipruritic, antimicrobial agents, Anti-Malassezia agents 16. A pharmaceutical composition according to claim 10 or 11, or a therapeutic agent according to claim 12 or 13, or a cosmetic composition according to claim 14 or 15, comprising one or more of:

21. 21. A pharmaceutical composition or therapeutic agent according to claim 20 for use as a medicament in the prevention or treatment of a disease according to claim 10.

22. Use according to claim 16 or use for the manufacture of a cosmetic composition according to claim 20 in the care of skin or hair.

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