Patent Application
20090191136
The present application claims-priority under 35 U.S.C. § 119 of German Patent Application No. 10 2008 006 394.0, filed Jan. 28, 2008, the entire disclosure of which is expressly incorporated by reference herein.
1. Field of the Invention
The present invention relates to the use of certain substance complexes against pollen allergies.
2. Discussion of Background Information
Pollen from certain trees, grasses, grain types and herbs causes among those affected a running or stuffy nose, itchy eyes and constant sneezing.
The pollen or farina is formed in the anther of seed plants. It is composed of the pollen grains, the microspores. The pollen grains are surrounded by a tough cell wall, which is composed, among other things, of sporopollenin.
Pollen grains serve to bring the male spores protected to the female reproductive structure and thus to ensure the pollination and subsequently the fertilization.
Allergic reactions to plant pollen are becoming an increasing problem. Allergies and hypersensitivity can manifest themselves:
Allergy sufferers can suffer from one form of the disease, but also from mixed forms. While allergic symptoms typically tend to occur acutely on the mucous membranes, symptoms such as bronchial asthma and atopic dermatitis can take a chronic course.
First signs of pollen allergy can occur among children from the age of five to six. Hay fever is a problem for children and their parents. Children afflicted by hay fever suffer from itchy and watery eyes, running nose, breathing problems and fatigue. Because there is additionally the danger that hay fever will turn into bronchial asthma, consistent pollen protection and preventive measures are very important.
Antihistamines and cortisone can be used to alleviate acute symptoms. The new hay fever remedies with an antihistamine as active ingredient are very reliable and, in contrast to their predecessors, do not cause much fatigue. Nevertheless, adults should be careful when driving vehicles or operating machinery.
Pollen flight can furthermore trigger or intensify neurodermatitis, Allergens in the air can trigger not only asthma and hay fever, but also reactions on the skin. The latest studies using a test developed at the Technical University of Munich (Prof. Johannes Ring) showed that pollen from birch, hazel, alder, grasses and herbs triggered eczema on the skin of certain people—and neurodermatitis is ultimately an eczema. People are also thereby affected on the skin by this type of pollen allergy who do not suffer from hay fever or other allergies. It was disputed for a long time that allergies are also play a role in the development of neurodermatitis—it was assumed to be a congenital disease that is intensified by psychological factors.
It has now surprisingly been found that the use of an active substance complex comprising panthenol, glycerol, citrate and/or bisabolol for the manufacture of a cosmetic or dermatological preparation for combating or substantially preventing pollen allergies, which preparation has a pH value of from about 4.6 to about 5.4 and/or a mass ratio of panthenol to citrate of from about 25:1 to about 5:1, based on the citrate anion, and/or a mass ratio of panthenol to bisabolol of from about 5:1 to about 1:1 is suitable for avoiding or at least alleviating pollen allergies.
The present invention provides a cosmetic or dermatological preparation for combating or substantially preventing pollen allergies. The preparation comprises panthenol, glycerol and at least one of citrate and bisabolol and has at least one of (i) a pH of from about 4.6 to about 5.4, (ii) a mass ratio of panthenol to citrate of from about 25:1 to about 5:1, based on the citrate anion, and (iii) a mass ratio of panthenol to bisabolol of from about 5:1 to about 1:1.
In one aspect, the preparation may comprise citrate and the preparation may have both a pH of from about 4.6 to about 5.4 and a mass ratio of panthenol to citrate of from about 25:1 to about 5:1, based on the citrate anion.
In another aspect, the preparation may comprise bisabolol and the preparation may have both a pH of from about 4.6 to about 5.4 and a mass ratio of panthenol to bisabolol of from about 5:1 to about 1:1.
In yet another aspect of the preparation of the present invention, the mass ratio of glycerol to citrate may be from about 60:1 to about 10:1, based on the citrate anion.
In a still further aspect of the preparation, the mass ratio of glycerol to bisabolol may be from about 50:1 to about 1:1.
In yet another aspect, the preparation may be present as an emulsion and/or the preparation may comprise at least about 5% by weight of water, based on the total weight of the preparation.
In another aspect, the preparation of the present invention may be present as at least one of a solution, an anhydrous preparation, a solid stick, an ointment and an aerosol.
The present invention also provides a method of combating or substantially preventing pollen allergies. The method comprises applying to skin a cosmetic or dermatological preparation according to the present invention as set forth above, including the various aspects thereof.
The particulars shown herein are by way of example and for purposes of illustrative discussion of the embodiments of the present invention only and are presented in the cause of providing what is believed to be the most useful and readily understood description of the principles and conceptual aspects of the present invention. In this regard, no attempt is made to show structural details of the present invention in more detail than is necessary for the fundamental understanding of the present invention, the description making apparent to those skilled in the art how the several forms of the present invention may be embodied in practice. Unless stated otherwise, all amounts, fractions and percentages given are based on the weight and the total amount or on the total weight of the preparations.
Preparations of the present inventions are capable of substantially preventing or avoiding allergic reactions to pollen among the people affected and provide the patient or the user of a preparation of this type with relief from allergic reactions at an early stage.
The invention also comprises the use of the described active substance complex in a skin care preparation set at a pH value of about 5 for the protection of the skin barrier from damage caused by allergenic pollen.
The cosmetic or dermatological preparations according to the present invention can be composed as usual and be used for the treatment, the care and the cleansing of the skin and/or the hair and as a cosmetic product in decorative cosmetics.
They often will comprise from about 0.001% to about 10% by weight, preferably from about 0.05% to about 5% by weight, in particular from about 0.1% to about 2% by weight, based on the total weight of the preparation, of 3-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-propane-1-one.
Cosmetic and dermatological preparations according to the present invention can be present in various forms, They can be, for example, a solution, an anhydrous preparation, an emulsion or a microemulsion of the type water-in-oil (W/O), or the type oil-in-water (O/W), a multiple emulsion, for example of the type water-in-oil-in-water (W/O/W), a gel, a solid stick, an ointment or also an aerosol.
It is also advantageous according to the present invention to administer 3-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-propane-1-one in encapsulated form, for example, in collagen matrices and other conventional encapsulation materials such as, e.g., as cellulose encapsulations, in gelatin, wax matrices or liposomally encapsulated. In particular wax matrices such as are described in DE-OS 43 08 282, the entire disclosure whereof is incorporated by reference herein, have proven to be advantageous.
It is also possible and advantageous according to the present invention to incorporate 3-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-propane-1-one into aqueous systems or surfactant preparations for cleansing the skin and the hair.
The cosmetic and dermatological preparations according to the present invention can comprise cosmetic auxiliaries, for example, those which are customarily used in such preparations such as, e.g., preservatives, bactericides, perfumes, substances for preventing foaming, dyes, pigments that have a coloring action, thickeners, surface-active substances, emulsifiers, softening, moisturizing and/or humectant substances, fats, oils, waxes or other customary constituents of a cosmetic or dermatological formulation, such as alcohols, polyols, polymers, gel formers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
Advantageous gel formers for the preparations of the present invention include, for example, copolymers of C10-30-alkyl acrylates and one or more monomers of acrylic acid, of methacrylic acid, and/or esters thereof. The INCI name of such compounds is “Acrylates/C 10-30 Alkyl Acrylate Cross-polymer.” The PEMULEN® grades TR 1, TR 2 and TRZ from Goodrich (Noveon) are particularly advantageous.
Carbopols are also advantageous gel formers for such preparations. Carbopols are polymers of acrylic acid, in particular also acrylate-alkyl acrylate copolymers. Advantageous carbopols are, for example, the grades 980, 981, 984, 1342, 1382, 2984 and 5984, likewise the ETD grades 2001, 2020, 2050 and Carbopol Ultrez 10, PVM/MA decadiene crosspolymer (trade name STABILEZE® 06), polyglyceryl methacrylate and polyacrylamide, ammonium dimethyl tauramide/vinylformamide copolymers, copolymers or crosspolymers comprising acryloyl dimethyltaurate, polyacryloyl dimethyltauramide, polyvinylpyrrolidone, and copolymers thereof.
Further advantageous gel formers for such preparations include xanthan gum, polyvinylpyrrolidone, cellulose derivatives, in particular, cellulose ethers such as, e.g., hydroxypropyl methylcellulose, starch and starch derivatives, hyaluronic acid, carrageenan, silicon dioxide and aluminum silicates.
The quantity of antioxidants (one or more compounds) in the preparations is preferably from about 0.001% to about 30% by weight, particularly preferably from about 0.05% to about 20% by weight, in particular from about 1% to about 10% by weight, based on the total weight of the preparation.
The lipid phase can advantageously be chosen from the following substances:
The oil phase of the emulsions, oleogels or hydrodispersions or lipodispersions of the present invention is advantageously selected from the esters of saturated and/or unsaturated, branched and/or unbranched alkanecarboxylic acids with a chain length of from about 3 to about 30 carbon atoms, and saturated and/or unsaturated, branched or unbranched alcohols with a chain length from about 3 to about 30 carbon atoms, and from the esters of aromatic carboxylic acids and saturated and/or unsaturated, branched and/or unbranched alcohols with a chain length of from about 3 to about 30 carbon atoms. Such ester oils can advantageously be selected from isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononyl isononanoate, 2-ethylhexyl palmitate, 2-ethylhexyl laurate, 2-hexyldecyl stearate, 2-octyldodecyl palmitate, oleyl oleate, oleyl erucate, erucyl oleate, erucyl erucate, as well as synthetic, semisynthetic, and natural mixtures of such esters, for example, jojoba oil.
The preparations of the present invention may, for example, comprise a lipid phase which comprises one or more lipids and has a spreading coefficient of less than about 800 mm2/10 min at 25° C. and a viscosity of from about 40 to about 25,000 mPas. For example, the lipid phase may have a spreading coefficient of less than about 600 mm2/10 min at 25° C., e.g., less than about 400 mm2/10 min at 25° C. and/or the lipid phase may have a viscosity of from higher than about 80 to about 15,000 mPas, e.g., from higher than about 100 to about 8,000 mPas.
Measuring the spreading coefficient (in mm2/10 min) referred to above is carried out according to the following method. 20 μl of the substance to be tested is dripped centrally on a Rotband filter paper from Schleicher & Schüll, Germany. At the same time a stopwatch is started and after 10 min the area is measured that has been wetted by the substance during this time. The measurement is carried out in an isothermal room at 25° C.+/−1° C.
In this regard, preferred lipids include:
Persea Gratissima
Buxus Chinensis
Macadamia Ternifolia
Ricinus Communis
Cannabis Sativa Seed Oil
For example, the one or more lipids may comprise at least one lipid selected from medicinal white oils, esters of C8-C30 fatty acids and linear and branched C8-C24 alcohols, and linear silicone oils.
The viscosity of the lipid phase of a preparation of the present invention can be increased by Theological modifiers and lipid thickeners. Preferred lipid thickeners include hectorite, silicate (“Aerosil 972”), metal salts of stearic acid, hydrogenated castor oil, microwaxes having a melting point above about 42° C., paraffins having a melting point above about 42° C., native waxes having a melting point of from about 33° C. to about 78° C., glyceryl esters of isostearates, fillers with a specific surface area of at least about 0.2 m2/g, long-chain silicone oils, bentonites and/or modified bentonites.
Optionally, the aqueous phase of the preparations of the present invention advantageously comprises alcohols, diols, or polyols having a low number of carbon atoms, as well ethers thereof, preferably ethanol, isopropanol, propylene glycol, glycerin, ethyleneglycol, ethyleneglycol monoethyl or monobutyl ether, propyleneglycol mono methyl, monoethyl, or monobutyl ether, diethyleneglycol monomethyl or monoethyl ether, and analogous products, furthermore alcohols having a low number of carbon atoms, for example, ethanol, isopropanol, 1,2-propanediol, glycerin, as well as in particular one or more thickeners, which can be advantageously chosen from silicon dioxide, aluminum silicates, polysaccharides or derivatives thereof, e.g., hyaluronic acid, xanthan gum, hydroxypropyl methylcellulose, particularly preferably from the group of polyacrylates, preferably polyacrylates from the group of the so-called carbopols, for example carbopols grades 980, 981, 1382, 2984, 5984, in each case individually or in combination.
In particular mixtures of the above-referenced solvents may be used. In the case of alcoholic solvents, water can be a further constituent.
Emulsions according to the present invention are advantageous and comprise, e.g., the cited fats, oils, waxes and other fatty bodies, as well as water and one or more emulsifiers, such as, e.g., emulsifiers which are conventionally used for such a type of formulation.
Gels according to the present invention usually comprise alcohols having a low number of carbon atoms, e.g., ethanol, isopropanol, 1,2-propanediol and glycerol, and water or an above-referenced oil in the presence of a thickener that with oily alcoholic gels is preferably silicon dioxide or an aluminum silicate, and with aqueous-alcoholic or alcoholic gels is preferably a polyacrylate.
Suitable propellants for preparations of the present invention which can be sprayed from aerosol containers include the customary known readily volatile, liquefied propellants, for example hydrocarbons (propane, butane, isobutane), which can be employed individually or as mixtures. Compressed air can also advantageously be used.
Preparations according to the present invention can also advantageously comprise substances that absorb UV radiation in the UVA and/or UVB range, wherein the total concentration of the filter substances is, e.g., from about 0.1% by weight to about 30% by weight, preferably from about 0.5% to about 10% by weight, in particular from about 1.0% to about 6.0% by weight, based on the total weight of the preparation, in order to provide preparations that protect the hair or the skin from the entire range of ultraviolet radiation. They can also be used as sun block for the hair or the skin.
Preparations according to the present invention can also advantageously comprise substances that act as a stabilizer, wherein the total amount of these stabilizers is, e.g., from about 0.1% to about 30% by weight, preferably from about 0.5% to about 10% by weight, in particular from about 1.0% to about 6.0% by weight, based on the total weight of the preparation, in order to provide cosmetic preparations that render possible preparations with long-term stability.
Preferred stabilizers include substances from the group of acetyltrifluoromethylphenylvalylglycine, acrylamide ammonium acrylate copolymer, aluminum magnesium hydroxide stearate, ammonium lactate, ammonium polyacrylate, ammonium polyacryloyldimethyl taurate, arginine PCA, capryloyl salicylic acid ester, cinnamic acid, cocoglucoside, copper gluconate, diphenyldimethicone, disodium adenosine triphosphate, disodium succinate, disteardimonium hectorite, dodecene, eperua falcata, hydrogenated palm glyceride, hydrogenated palm glyceride citrate, hydrogenated palm kernel glyceride, hydrolyzed wheat protein, PG propyl methyl silanediol, hydroxyethylacrylate/sodium acryloyldimethyltaurate copolymer, isodeceth-6, linseed acid magnesium aspartate, melibiose, oxothiazolidine carboxylic acid, palmitoyl pentapeptide 4, PEG-8 laurate, phenethylalcohol, phenyl propanol, polyacrylate-13, polyacrylate-3, sarcosine, saxifraga sarmentosa extract, Scutellaria baicalensis extract, sodium metabisulfite, soybean isoflavone, tocopheryl glucoside, trideceth-6, and zinc gluconate.
The following examples are intended to illustrate the present invention without limiting it. Unless stated otherwise, all of the quantities, proportions and percentages are percentages by weight based on the weight and the total quantity or the total weight of the preparations.
While the present invention has been described with reference to an exemplary embodiment, it is understood that the words which have been used herein are words of description and illustration, rather than words of limitation. Changes may be made, within the purview of the appended claims, as presently stated and as amended, without departing from the scope and spirit of the present invention in its aspects. Although the present invention has been described herein with reference to particular means, materials and embodiments, the present invention is not intended to be limited to the particulars disclosed herein; rather, the present invention extends to all functionally equivalent structures, methods and uses, such as are within the scope of the appended claims.
| Number | Date | Country | Kind |
|---|---|---|---|
| 10 2008 006 394.0 | Jan 2008 | DE | national |
