Cosmetic preparation comprising pulverized hydrophilic substances

Abstract

A substance, which is in principle insoluble in a cosmetic or dermatological anhydrous preparation is converted into a powdery product by absorption onto a carrier, the powdery product being soluble in the preparation. The anhydrous preparations comprise one or more hydrophilic substances or substance mixtures which are liquid, pasty at room temperature and/or meltable up to a temperature of 150 C. and which are absorbed on one or more particulate carriers. The hydrophilic substance or substance mixture in itself is insoluble or sparingly soluble in the preparation and the carriers are characterized by a particle size ranging from 5 nm to 2 mm, a tamped density of between 50 kg/m.sup.3 and 1400 kg/m.sup.3 and a spherical, fibrous, flocculated and/or sponge-like particulate form.

Claims

1. A cosmetic or dermatological preparation, wherein the preparation is anhydrous and comprises an organic medium which has incorporated therein one or more powdery materials comprising or consisting of (i) one or more hydrophilic substances or substance mixtures which are liquid or pasty at room temperature and/or meltable up to a temperature of 150 C. and on their own are insoluble or sparingly soluble in a remainder of the preparation, bound by at least one of adhesion, impregnation, agglomeration to (ii) one or more particulate carriers having an average particle size in a range of from 5 nm to 2 mm and a tamped density of from 50 kg/m.sup.3 to 1400 kg/m.sup.3, and being of a spherical, fibrous, flocculated and/or sponge-like form.

2. The preparation of claim 1, wherein (i) has been bound to (ii) by a Concentrated Powder Form (CPF) process.

3. The preparation of claim 1, wherein (ii) comprises a polysaccharide.

4. The preparation of claim 3, wherein (ii) comprises cellulose and/or a cellulose derivative.

5. The preparation of claim 3, wherein (ii) comprises a starch.

6. The preparation of claim 1, wherein (ii) comprises one or more of silica and a silicate.

7. The preparation of claim 1, wherein (ii) comprises one or more of a nylon and lauroyl lysine.

8. The preparation of claim 1, wherein the one or more powdery materials consist of (i) and (ii).

9. The preparation of claim 1, wherein the one or more powdery materials are free of emulsifiers and stabilizers.

10. The preparation of claim 1, wherein the organic medium comprises at least one of dimethicone, cyclomethicone, C12-15 alkyl benzoate, ricinus communis seed oil, lanolin oil, octyldodecanol, microcrystalline wax, candellila wax, cetyl palmitate, hydrogenated polydecene.

11. The preparation of claim 1, wherein (i) comprises one or more of an antibacterial, antiperspirant, anti-aging, skin-calming and/or moisturizing active ingredient.

12. The preparation of claim 11, wherein (i) comprises at least one of Q10, bisabolol, panthenol, calcium pantothenate, niacinamide, piroctone olamine.

13. The preparation of claim 11, wherein (i) comprises at least one of glycerol and a glycol.

14. The preparation of claim 1, wherein (i) comprises at least one deodorant active ingredient.

15. The preparation of claim 14, wherein the at least one deodorant active ingredient comprises at least one of methyl phenyl butanol, butyloctanoic acid, polyglyceryl-2 caprate, polyaminopropyl biguanide, octenidine HCl, silver citrate.

16. The preparation of claim 1, wherein (i) comprises at least one water-soluble UV filter.

17. The preparation of claim 1, wherein (i) comprises at least one plant extract.

18. The preparation of claim 17, wherein the at least one plant extract comprises one or more extracts of one or more of Cymbopogon citratus, Maris limus, Ostrea shell, cucumber.

19. The preparation of claim 1, wherein the preparation is present as an aerosol.

20. The preparation of claim 1, wherein the preparation is present as an antiperspirant or a lip product.

Description

(1) The invention is therefore a cosmetic or dermatological anhydrous preparation comprising one or more powdery products, comprising or consisting of one or more hydrophilic substances or substance mixtures that are liquid or pasty at room temperature and/or meltable up to a temperature of 150 C. (a.), which are absorbed on one or more particulate carriers (b.). The substance or substance mixture (a.) is by itself insoluble or sparingly soluble in the preparation. The substance or substance mixture (a.) is considered to be soluble if it is present in completely and homogeneously dissolved form in the surrounding medium, i.e. the preparation, without further auxiliaries such as emulsifiers or solubilizers. By itself means here that the substance is not absorbed on the carrier (b.).

(2) The carriers (b.) are characterized by an average particle size in the range from 5 nm to 2 mm, a tamped density of from 50 kg/m.sup.3 to 1400 kg/m.sup.3 and a spherical, fibrous, flocculated and/or sponge-like particulate form.

(3) The carriers used are powders which have minimum 5 nm and maximum 2 mm in the average particle size.

(4) A particularly decisive factor for selecting the carrier material is its tamped density. The tamped density is 50 kg/m.sup.3 to 1400 kg/m.sup.3. The tamped density is ascertained by determining the volume, the tamped volume being the smallest volume of a released amount of filler material which is present after tamping or compacting according to standardized conditions (see also ISO 787/11). The porosity of the carrier can be freely selected from nonporous to highly porous.

(5) The particulate form of the carrier is spherical, fibrous, flocculated or sponge-like.

(6) The carrier substances are powder substances customarily used in cosmetics. They are preferably selected from the group of polysaccharides and silicas and derivatives thereof, but powder substances as are used in decorative cosmetics as filler and sensory additive are also possible. The list below of carrier materials that can be used advantageously should in no way be limiting:

(7) Polysaccharides: starches from different plant sources, e.g. corn starch, potato starch, rice starch, wheat starch, and derivatives thereof (e.g. trade names: Amylogum CLS from Avebe, C*EmCap from Cerestar, DryFlo grades from Akzo Nobel celluloses and derivatives, e.g. Avicel grades from FMC Biopolymer, Arbocel, Vitacel, Vivapur grades from J. Rettenmaier & Shne GmbH.

(8) Further fillers such as lauroyl lysine (Amihope LL), nylon grades (e.g. Orgasol grades from Arkema) or silicates such as calcium silicate (Hubersorb from Huber) can be used. In the case of the silicas, preferably grades from the series of Aerosils from Evonik Degussa can be used.

(9) The powdery products include the hydrophilic substances or substance mixtures (a.) and the particulate carriers (b.) on which they are absorbed, or preferably they consist only of these two constituents a.) and b.).

(10) It is possible to dispense with the addition of emulsifiers or stabilizers in the powdery products.

(11) A further preferred criterion is that the powdery products are produced according to the CPF process.

(12) According to the invention, the hydrophilic substance or the substance mixture is characterized in that, by itself, it is insoluble or sparingly soluble in the preparation. The hydrophilic substance or a hydrophilic substance mixture is characterized in that it is miscible with water. Solubility is the property of a substance to dissolve homogeneously in a liquid or melt.

(13) Substance or substance mixtures which can be dissolved in the solvent incompletely or only inhomogeneously are referred to as insoluble or sparingly soluble.

(14) As a result of pulverizing the hydrophilic substances or substance mixtures, also referred to as active ingredients or active solutions, it is now possible according to the invention to incorporate these without further auxiliaries such as solubilizers or emulsifiers into formulations in which they are not soluble in a homogeneous manner, i.e. without phase separation.

(15) I.e. a substance that is in principle insoluble in a cosmetic or dermatological preparation is converted to a powdery product as a result of absorption on a carrier, where the substance insoluble in the hydrophobic formulation is bonded as hydrophilic solution to the carrier. The powder laden with active ingredients does not dissolve here in the preparation, but is present in the formulation such as a sensory additive as powder, only additionally laden with liquid.

(16) Pulverization advantageously takes place according to the CPF process. Reference is hereby expressly made to the CPF processes described in documents WO 99 17868 A1, EP 1 021 241 A1 and EP 0 744 992 A1. The disclosures made therein are in their entirety also part of the present application.

(17) The CPF process makes it possible to produce powdery solids from liquids. The process principle consists in dissolving a gas in the liquid to be pulverized under elevated pressure, preferably until a gas-saturated solution is obtained. Compared to pure liquid, such a solution has a series of favorable properties: thus, normally, the viscosity of this solution is lowered by several orders of magnitude compared to the pure liquid at the same temperature, and the interfacial tension is also considerably reduced.

(18) The pressurized liquid/gas solution is then fed to a decompression element and rapidly decompressed therein. Before the decompression element, in the decompression element or after it, in particular shortly after the decompression element, a solid, powdery auxiliary, the particulate carrier, is admixed with the liquid substance or substance mixture to be pulverized or the liquid/gas solution.

(19) The gas used can in principle be any gas which is sufficiently soluble in the liquid substance or substance mixture to be pulverized. For example, the gas that can be used is carbon dioxide, a hydrocarbon, in particular methane, ethane, propane, butane, ethene, propene or a halogenated hydrocarbon, an ether, an inert gas, in particular nitrogen, helium or argon, a gaseous oxide, in particular dinitrogen oxide or sulfur dioxide, and ammonia. A mixture of two or more of the aforementioned gases can also be used. The increased pressure under which the gas is dissolved in the liquid substance or substance mixture can be in the range from 5 bar to 800 bar, although preferably the pressure is in the range from 10 bar to 350 bar and particularly preferably in the range from 20 bar to 250 bar.

(20) Preferably, the dissolution of the gas in the liquid substance or substance mixture is accelerated by mixing the gas with the liquid substance or substance mixture. This mixing can be achieved for example by shaking or rolling the pressurized container in which the liquid to be pulverized has been introduced. Alternatively, the solution that is formed in the pressurized container can be stirred using a stirrer. Another option of achieving thorough mixing of the liquid to be pulverized with the gas consists in recirculating the liquid phase present in the pressurized container and/or the gas phase, i.e. pumping it/them from the pressurized container and introducing it/them again to the pressurized container in the region of the respective other phase. A further option is the use of a static mixer. The aforementioned procedures can of course also be combined.

(21) The CPF process functions in principle with any solid, powdery carrier.

(22) The substance to be pulverized, the active solution, is bound here to the carrier particle by adhesion, impregnation and/or agglomeration. Surprisingly, the CPF process does not lead to a closed coating being formed. Capsules are not formed. Consequently, the active solution can dissolve from the particulate carrier as soon as the laden particles come into an environment in which the active solution is soluble and/or to which there exists an affinity. Thus, for example, the hydrophilic substances can bind with the perspiration on the skin and thus spread themselves on the skin. The release then takes place also with a time delay and thus leads to a long-lasting effect.

(23) On account of the special production technology with CPF technology, the substance, active ingredient on the particles is already present in predissolved form at the site of action and can be very rapidly released. The thus improved solubility is comparable with that of instant coffee compared to coffee powder.

(24) According to the invention, hydrophilic substance, substance mixture, active ingredient or active solution to be pulverized are to be understood as meaning all substances that are liquid or pasty at room temperature and/or meltable up to a temperature of 150 C.

(25) Substance mixtures or active solutions include, for example, solutions such as e.g. aqueous surfactant solutions which optionally comprise further ingredients, or water-dissolved plant extracts or dissolved active ingredients, such as e.g. antibacterial and antiperspirant active ingredients.

(26) The substance to be pulverized can be present as pure substance (without solvents) or dissolved in a suitable solvent, e.g. in the case of hydrophilic active ingredients water or propylene glycol.

(27) From the group of polar solvents, mention is to be made in particular of: water, volatile alcohols (e.g. ethanol, isopropanol), and also humectants (polyhydric alcohols, such as glycerol, propylene glycol, butylene glycol), generally alkanediols, as are used as preservative aids (e.g. caprylyl glycol, pentylene glycol) and low molecular weight PEGs (e.g. PEG-8).

(28) The active solution is preferably liquid at room temperature, but can also be pasty to solid if it is then meltable at a temperature up to 150 C. The viscosity of the active solution can also be adjusted via hydrophilic thickeners customarily used in cosmetics, such as, for example, polymers.

(29) Preferred cosmetic active ingredients which can be present in the preparation and are preferably pulverized by means of CPF are to be selected from the group of antibacterial, antiperspirant, anti-aging, skin-calming and/or moisturizing active ingredients.

(30) Deodorant active ingredients such as methyl phenyl butanol, butyloctanoic acid, polyglyceryl-2 caprate, polyaminopropyl biguanide, octenidine HCl, silver citrate or other active ingredients, such as Q10, panthenol, bisabolol, calcium pantothenate, niacinamide, and/or piroctone olamine, can likewise be selected.

(31) Furthermore, water-soluble UV filters can be used, e.g. disodium phenyl dibenzimidazole tetrasulfonate.

(32) Suitable humectants are glycerol and glycols. These substances require then in particular no solvent and can be pulverized directly as hydrophilic substances on the carrier and then be added to the water-free or hydrophobic preparation.

(33) Further active ingredients can be selected from the group of extracts, such as e.g. from Cymbopogon citratus, Maris limus, Ostrea shell, cucumber.

(34) According to the invention, now hydrophilic deodorant active ingredients can for example be incorporated into anhydrous formulations (oil-based), such as e.g. into aerosols.

(35) It is likewise now possible to provide hydrophilic skin moisturizers such as glycerol in anhydrous formulas, such as e.g. in lip products.

(36) Preferably, the preparations according to the invention are anhydrous. A residual fraction of water can be present in the preparation according to the invention, however, as a consequence of raw materials and may therefore be unavoidable. Within the context of the invention, anhydrous is therefore the term used to refer to compositions which comprise less than 5% by weight of water (water of crystallization not included), preferably less than 2% by weight and in particular less than 1% by weight, of water, based on the total mass of the preparation.

(37) The substances, active ingredients or active solutions to be incorporated are insoluble or only sparingly soluble in the preparation. The solubility is the property of a substance to dissolve homogeneously in a liquid. Substance or substance mixtures which cannot dissolve completely in the solvent or can only dissolve inhomogeneously in solvents are referred to as insoluble or sparingly soluble, respectively.

(38) Thus, aerosol preparations for perspiration reduction can also advantageously be provided. The preparation according to the invention is applied to the skin, for example in the armpits. The perspiration encounters the pulverized substances or substance mixtures, such as, for example, an active-ingredient-containing emulsion, and leads to its rehydration. The perspiration is absorbed and at the same time any active ingredients present are released which serve for perspiration inhibition or skin care.

(39) The cosmetic and dermatological preparations according to the invention can also comprise cosmetic auxiliaries and further active ingredients, as are customarily used in such preparations, e.g. preservatives, preservation aids, bactericides, perfumes, substances for preventing foaming, dyes and colored pigments, thickeners, moisturizing and/or humectant substances, fats, oils, waxes or other customary constituents of a cosmetic or dermatological formulation, such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives, provided the addition does not adversely affect the required properties as regards solubility.

(40) The examples below are intended to describe the invention in more detail without limiting it.

(41) The fraction data refer to fractions by weight, based on the total mass of the preparation, unless disclosed otherwise.

(42) Demonstration of the deodorant effect of water-soluble deodorant actives in anhydrous aerosols

(43) TABLE-US-00001 Example 1 Cyclomethicone 39.75 Disteardimonium Hectorite 4.00 C12-15 Alkyl benzoate 30.00 Calcium carbonate 10.00 Perfume 6.25 Carrier particles (microcrystalline cellulose) 6.60 Deodorant active ingredient on carrier particles 3.40 (polyaminopropyl biguanide) Filling with a mixture of propane, isobutane, butane in a ratio of 15% by weight active solution and 85% by weight propellant gas Sniff* Score untreated vs. product with CPF powder 0.92 after 4 h (preparation Example 1) 0.83 after 24 h *To test the deodorant effectiveness, a SNIFF test was carried out in which trained people tested by smelling how the deodorized armpit smelled compared to the others which remained without deodorant for comparison purposes. The preconditioning time is 10 days. In this time, the subjects must use no deodorant products of any kind in the armpits and wash only with unperfumed soap. The first odor value (t0) is ascertained 24 h after the subjects have washed with unperfumed soap. After rewashing, the product is applied in one armpit (application amount approx. 1000 mg), the other armpit remains untreated. 4 h (t1) and 24 h (t2) afterwards, the armpit odor is assessed on a five-point scale (0 no odor, 5 very strong odor). To assess the deodorant performance, the SNIFF scores from both armpits for time points t1 and t2 are compared. The greater the difference, the better the deodorant performance.

(44) For the sniff scores shown in Example 1, this means that a deodorant performance was able to be demonstrated after 4 h and after 24 h. The hydrophilic deodorant active ingredient polyaminopropyl biguanide was thus released from the hydrophobic preparation and could therefore be effective.

(45) TABLE-US-00002 Example 2 Example 3 Example 4 Cyclomethicone 60.95 55.15 39.25 Disteardimonium Hectorite 3.5 4 4.5 Dipropylene glycol 0.65 Triethyl citrate 0.65 Persea gratissima oil 0.8 Octyldodecanol 0.8 Dimethicone 3 C12-15 Alkyl benzoate 40 Calcium carbonate 20 20 Carrier particles Avivel PH 101 4.4 (microcrystalline cellulose) Deodorant active ingredient on 3.6 carrier particles (polyaminopropyl biguanide) Carrier particles Vivapur 105 6.4 6.4 (microcrystalline cellulose) Deodorant active ingredient on 3.6 3.6 carrier particles (propylene glycol + ethylhexylglycerine + octenidine HCl) Perfume 6.25 6.25 6.25 Filling with a mixture of propane, isobutane, butane in a ratio of 15% by weight active solution and 85% by weight propellant gas

(46) Examples of Lip Products

(47) TABLE-US-00003 INCI Example 5 Example 6 Tocopheryl acetate 1.00 1.00 Ricinus communis seed oil + CI 77492 + BHT 4.50 4.50 CI 77499 + Ricinus communis seed oil + BHT 0.32 0.32 Ricinus communis seed oil + CI 77891 + BHT 5.86 5.86 Ricinus communis seed oil + CI 15850 + BHT 2.53 2.53 Mica + CI 77891 1.00 1.00 Octyldodecanol 8.00 8.00 Hydrogenated polydecene 6.00 6.00 Copernicia cerifera cera 2.25 2.25 Ricinus communis seed oil 13.72 12.13 Cera microcristallina 3.15 3.15 Vitis vinifera seed oil 0.50 0.50 Simmondsia chinensis seed oil 2.00 2.00 Persea gratissima oil 3.00 3.00 Lanolin oil 9.00 7.28 Lauryl PCA 3.00 3.00 Bis-diglyceryl polyacyladipate-2 5.00 5.00 Myristyl lactate 5.00 5.00 Isopropyl palmitate 3.00 3.00 Candelilla cera 5.40 5.40 Cera microcristallina 2.70 2.70 Lecithin 0.50 0.50 Lanolin alcohol (Eucerit) 0.81 0.81 Nylon-12 0.50 0.50 VP/hexadecene copolymer 1.50 1.50 Propyl paraben 0.10 0.10 Propylene carbonate 0.12 0.12 Disteardimonium hectorite 0.50 0.50 BHT 0.03 0.03 Perfume 0.20 0.20 Hydrophilic active ingredient on carrier particles 3.00 3.37 (Glycerin) Carrier particles Vivapur 105 (microcrystalline 5.82 cellulose) Carrier particles lauroyl lysine 8.76

(48) TABLE-US-00004 Example 7 Example 8 Example 9 Cera microcristallina 19.35 21.50 19.35 Panthenol 0.13 0.13 0.13 Cetearyl alcohol 2.25 2.50 2.25 Cocoglycerides 2.00 2.00 2.00 Cetyl palmitate 9.00 10.00 9.00 Pentaerythrityl tetraisostearate 2.00 2.00 2.00 Octyldodecanol 17.75 18.61 16.05 Butyrospermum parkii butter 1.80 2.00 1.80 Hydrogenated polydecene 15.00 15.00 15.00 Myristyl myristate 3.42 3.80 3.42 Cera alba 0.45 0.50 0.45 Copernica cerifera cera 1.08 1.20 1.08 Ricinus communis seed oil 8.00 8.00 8.00 Cera microcristallina 0.81 0.90 0.81 Vitis vinifera seed oil 0.10 0.10 0.10 C20-40 Alkyl stearate 1.62 1.80 1.62 Simmondsia chinensis seed oil 1.00 1.00 1.00 VP/eicosene copolymer 2.00 2.00 2.00 VP/hexadecene copolymer 3.00 3.00 3.00 Perfume 0.15 0.15 0.15 Hydrophilic active ingredient on 3.09 3.00 3.00 carrier particles (glycerin) Carrier particles Vivapur 105 6.01 (microcrystalline cellulose) Carrier particles silica dimethyl 0.82 silylate Carrier particles lauroyl lysine 7.79