DE102010055770A1 - Preparing cosmetic and/or dermatological emulsion comprises adding one or more glucosylglycerides to an aqueous phase and/or an oil phase at a specified temperature, and combining the oil and aqueous phases - Google Patents

Abstract

Preparing cosmetic and/or dermatological emulsion comprises adding one or more glucosylglycerides to an aqueous phase and/or an oil phase at = 40[deg] C, and combining the oil and aqueous phases.

Description

The present invention relates to a process for the preparation of cosmetic and / or dermatological emulsions with one or more glucosylglycerides The outermost layer of the epidermis, the stratum corneum (horny layer), as an important barrier layer of particular importance and u. a. for protection against environmental influences and dehydration. The horny layer is constantly worn in contact with the environment and must therefore be renewed continuously.

A skin model widely used today in the art understands the stratum corneum as a two-component system, similar to a brick wall (brick-mortar model). In this model, the corneocytes (horny cells) correspond to the bricks, the complex composite lipid membrane in the intercellular spaces corresponds to the mortar.

In addition to their barrier effect against external chemical and physical influences, the epidermal lipids also contribute to the cohesion of the horny layer and have an influence on the skin smoothness. In contrast to the sebaceous gland lipids, which do not form a closed film on the skin, the epidermal lipids are distributed over the entire horny layer.

The extremely complex interaction of the moisture-binding substances and the lipids of the upper skin layers is very important for the regulation of skin moisture. Therefore, cosmetics usually contain, in addition to balanced lipid mixtures and water, water-binding substances. These include u. a. Polyols such as glycerol, sorbitol and xylitol, ethoxylated polyols and hydrolyzed proteins. Further application find the substances contained in the natural moisturizing factor (so-called Natural Moisturizing Factor = NMF), such as. Urea, carbohydrates (eg glucose) and amino acids (eg serine). These substances are therefore of particular importance for the care performance of a cosmetic product, in particular because of their relatively good skin and mucous membrane compatibility.

Cosmetic and pharmaceutical products must be fast and inexpensive to produce.

The "hardware", ie mixing and stirring systems are fixed and can not be adapted for each new recipe. The "software" for each production is then the phase divisions, in which the individual raw materials are summarized according to their solubility, temperature sensitivity and percentage of the total formulation.

Known batch processes are characterized in that the individual phases are metered simultaneously into a high-performance emulsifier. There, the emulsification and homogenization process takes place with high energy input, with high shear forces occurring. However, the occurrence of high shear forces can damage polymers contained in the formulations. The simultaneous dosing of all components exposes them to higher temperatures for longer periods of time. As a result, the use of temperature-sensitive substances is limited. Such substances are, for example, cosmetic active ingredients and functional substances such as fragrances, vitamins, coenzymes, peptides, enzymes, nucleic acids, plant extracts, preservatives such as, for example, 1,2-dibromo-2,4-dicyanobutane and 2-phenoxyethanol.

Such substances must be provided as a separate phase (s). These phases were prepared in different variations, depending on the active ingredient:

Version 1:

• Preservative 0.5%
• Water, demineralized 3-8%

Variant 2:

• Thickener polyacrylic acid 0.2%
• Lipid 3-8%

Variant 3:

• Perfume oil 0.4-1.2%
• Ethanol 3-10%

Variant 4:

• Heat-sensitive drug z. B. α-tocopherol, panthenol 0.5-10%
• Vegetable oil 3-10%

For water-in-oil emulsions are additional active substance / resp. Perfume phases are always critical because it interferes with the process of adding (sucking in, stirring in) the pre-emulsion. When water-soluble and temperature-sensitive constituents have to be added, it is particularly critical because these substances must enter the water droplets through the "lipid layer" outer phase without destroying or enlarging these droplets.

For other emulsion types, as well as hydrodispersion gels, the addition of extraphases is less critical because the outer phases are usually the coherent phase (aqueous phase). Due to the other stabilization principle (gel network, formation of a polymer matrix), extravasases are easy to add. However, the distribution is often hampered by these networks, so that as a last step in the production of O / W emulsions usually a Homogenisierungsschritt takes place. This is the actually critical process step, because here the built up gelnetzwerkt is partly destroyed again and must build new ones.

There is therefore a need for preparations which overcome the disadvantages of the prior art.

• (i) ein oder mehrere Glucosylglyceriden einer Wasserphase oder
• (ii) ein oder mehrere Glucosylglyceriden einer Ölphase oder
• (iii) ein oder mehrere Glucosylglyceriden einer Wasser- und einer Ölphase

zugegeben wird oder werden und diese bei Temperaturen, die 40°C nicht überschreiten

• (i) die Wasserphase mit einer Ölphase vereinigt oder
• (ii) die Ölphase mit mit einer Wasserphase vereinigt wird oder
• (iii) beide Phasen miteinander vereinigt werden.

It was after all this surprising and unpredictable that a process for the preparation of cosmetic and / or dermatological emulsions, characterized in that

• (i) one or more glucosylglycerides of a water phase or
• (ii) one or more glucosylglycerides of an oil phase or
• (iii) one or more glucosylglycerides of a water and an oil phase

is or are added and these at temperatures not exceeding 40 ° C.

• (i) the water phase is combined with an oil phase or
• (ii) the oil phase is combined with a water phase or
• (iii) combining both phases.

The addition of glyceryl glucoside to active ingredients, perfume oils or other volatile raw materials improves the absorption capacity of this phase in the overall preparation. Heating the phase can often be avoided because the glyceryl glucoside improves the solubility of many drugs. Glyceryl glucoside can be used as a "filler" to give these phases a larger volume so that they can be sucked in and an immediate mixing and emulsification / stabilization can take place.

Such additional phases contain preservative or polyacrylic acid or drug or perfume oil and glyceryl glucose 3-10%.

und/oder der allgemeinen Formel

und/oder der allgemeinen Formel

und/oder der allgemeinen Formel

werden erfindungsgemäß bevorzugt.For the purposes of the present invention, glucosylglycerides of the general formula are advantageous

and / or the general formula

and / or the general formula

and / or the general formula

are preferred according to the invention.

Particularly preferred glucosylglyceride is (2-O-β-D-glucopyranosyl) -sn-glycerol.

According to the process of the invention, the preparations are particularly advantageously characterized in that the glucosylglyceride or in the water and / or oil phase in concentrations of 0.01-40.00 wt .-%, preferably 0.05-15.00 wt. -%, particularly preferably 0.1-6.00 wt .-%, each based on the total weight of the composition present.

In addition to water, ethanol and isopropanol, glycerol and propylene glycol skin-care fat or fat-like substances, such as oleic acid, cetyl alcohol, cetylstearyl alcohol and 2-octyldodecanol, can be used in the usual proportions for such preparations as conventional cosmetic excipients for the preparation of the preparations according to the invention as well as slime-forming substances and thickeners, eg. As hydroxyethyl or hydroxypropyl cellulose, polyacrylic acid, polyvinylpyrrolidone, but also in small quantities cyclic silicone oils (polydimethylsiloxanes) and liquid Polymethylphenylsiloxane low Viskosiät.

It is likewise advantageous to add conventional antioxidants to the preparations for the purposes of the present invention. According to the invention, all antioxidants which are suitable or customary for cosmetic and / or dermatological applications can be used as favorable antioxidants.

The amount of the antioxidants (one or more compounds) in the preparations is preferably from 0.001 to 30% by weight, particularly preferably from 0.05 to 20% by weight, in particular from 1 to 10% by weight, based on the total weight of the preparation ,

• – Wasser oder wäßrige Lösungen
• – Öle, wie Triglyceride der Caprin- oder der Caprylsäure, vorzugsweise aber Rizinusöl;
• – Fette, Wachse und andere natürliche und synthetische Fettkörper, vorzugsweise Ester von Fettsäuren mit Alkoholen niedriger C-Zahl, z. B. mit Isopropanol, Propylenglykol oder Glycerin, oder Ester von Fettalkoholen mit Alkansäuren niedriger C-Zahl oder mit Fettsäuren;
• – Alkohole, Diole oder Polyole niedriger C-Zahl, sowie deren Ether, vorzugsweise Ethanol, Isopropanol, Propylenglykol, Glycerin, Ethylenglykol, Ethylenglykolmonoethyl- oder -monobutylether, Propylenglykolmonomethyl, -monoethyl- oder -monobutylether, Diethylenglykolmonomethyl- oder -monoethylether und analoge Produkte.

If the cosmetic or dermatological preparation in the sense of the present invention is a solution or emulsion or dispersion, it is possible to use as solvent:

• - water or aqueous solutions
• - Oils, such as triglycerides of capric or caprylic, but preferably castor oil;
• Fats, waxes and other natural and synthetic fats, preferably esters of fatty acids with lower C-number alcohols, e.g. With isopropanol, propylene glycol or glycerol, or esters of fatty alcohols with alkanoic acids of low C number or with fatty acids;
• Alcohols, diols or polyols of low C number, and their ethers, preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether, diethylene glycol monomethyl or monoethyl ether and analogous products.

In particular, mixtures of the abovementioned solvents are used. For alcoholic solvents, water can be another ingredient.

• – Wasser oder wäßrige Lösungen
• – Öle, wie Triglyceride der Caprin- oder der Caprylsäure, vorzugsweise aber Rizinusöl;
• – Fette, Wachse und andere natürliche und synthetische Fettkörper, vorzugsweise Ester von Fettsäuren mit Alkoholen niedriger C-Zahl, z. B. mit Isopropanol, Propylenglykol oder Glycerin, oder Ester von Fettalkoholen mit Alkansäuren niedriger C-Zahl oder mit Fettsäuren;
• – Alkohole, Diole oder Polyole niedriger C-Zahl, sowie deren Ether, vorzugsweise Ethanol, Isopropanol, Propylenglykol, Glycerin, Ethylenglykol, Ethylenglykolmonoethyl- oder -monobutylether, Propylenglykolmonomethyl, -monoethyl- oder -monobutylether, Diethylenglykolmonomethyl- oder -monoethylether und analoge Produkte.

If the cosmetic or dermatological preparation in the sense of the present invention is a solution or emulsion or dispersion, it is possible to use as solvent:

• - water or aqueous solutions
• - Oils, such as triglycerides of capric or caprylic, but preferably castor oil;
• Fats, waxes and other natural and synthetic fats, preferably esters of fatty acids with lower C-number alcohols, e.g. With isopropanol, propylene glycol or glycerol, or esters of fatty alcohols with alkanoic acids of low C number or with fatty acids;
• Alcohols, diols or polyols of low C number, and their ethers, preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether, diethylene glycol monomethyl or monoethyl ether and analogous products.

In particular, mixtures of the abovementioned solvents are used. For alcoholic solvents, water can be another ingredient.

Suitable propellants for sprayable from aerosol containers cosmetic and / or dermatological preparations in the context of the present invention, the usual known volatile, liquefied propellants, such as hydrocarbons (propane, butane, isobutane) are suitable, which can be used alone or in mixture with each other. Also, compressed air is advantageous to use.

Of course, those skilled in the art will recognize that there are inherently nontoxic propellants which would be useful in the practice of the present invention in the form of aerosol preparations, but which should be avoided due to adverse environmental effects or other attendant circumstances, especially fluorocarbons and chlorofluorocarbons (US Pat. CFC).

Cosmetic preparations according to the present invention may also be present as gels, in addition to an effective content of the active ingredient according to the invention and solvents commonly used for this, preferably water, or organic thickening agents, for. Gum arabic, xanthan gum, sodium alginate, cellulose derivatives, preferably methylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose or inorganic thickening agents, e.g. For example, aluminum silicates such as bentonites, or a mixture of polyethylene glycol and polyethylene glycol stearate or distearate. The thickener is in the gel z. B. in an amount between 0.1 and 30 wt .-%, preferably between 0.5 and 15 wt .-%.

Following are advantageous embodiments of the present invention. The data relate to% by weight, based on the total weight of the preparations. W / O emulsions, 1 2 3 4 5 fat phase Wool alcohol 3.0 - - - 3.0 Polyglyceryl-3 diisostearate - 3.5 1.43 2.5 - PEG-40 sorbitan isostearate 3.0 2.5 1.77 3.5 3.0 Medical white oil 12.5 10.0 10.0 5.0 17.5 isopropyl 8.0 6.0 - 12.0 2.5 Caprylic / capric 2.0 2.5 - 5.0 0.5 almond oil 2.0 - 0.01 - - microcrystalline wax 2.0 1.0 2.0 5.0 0.25 isopropyl palmitate 0.5 1.0 3.0 3.0 0.25 Perfume phase Glycerylglucose 2.5 7.5 0.5 22.5 8.0 Perfume q, s, q, s, q, s, q, s, q, s, water phase potassium sorbate 0.05 0.1 0,125 0.75 0.25 magnesium sulfate 0.5 0.6 0.7 0.7 1.0 glycerin 3.0 5.0 4.8 15.0 1.5 lactic acid 0.2 0.09 0.086 0.3 1.0 sodium lactate 0.4 0.18 0.174 0.6 2.0 water ad 100 ad 100 ad 100 ad 100 ad 100

Production process for producing a W / O emulsion on a 500 kg Beco mixer:

The fat phase is heated in the boiler 2 with stirring at 1 meter / second to 80 ° C until all raw materials are clearly dissolved. The water phase is also heated in boiler 1 with stirring at 1 meter / second to 80 ° C. When all phases have reached 80 ° C, a vacuum of at least -0.5 bar is applied.

The fat phase is sucked into the boiler 1, into the water phase. The circulation homogenizer is switched on at 14 meters / second to achieve a homogeneous emulsion. After 6 minutes, the homogenizer is switched off and the cooling is made with a capacity of 8600 liters / hour. After 25 minutes 35 ° C are reached and the perfume phase is sucked. After another 25 minutes 28 ° C are reached and the circulation homogenizer, the final viscosity is set. It is homogenised at 25 meters / second for 10 minutes. It is then cooled for a further 10 minutes, until the finished emulsion can be pumped into a storage container or to the filling line. O / W emulsion 6 7 8th 9 10 fat phase Glycerylsterat 1.0 - - 0.5 0.25 Polyethylene glycol (40) stearate 10.0 - 5 - - Triglycerinmethylglucosedistearat - 5.5 - - 2.5 sorbitan - 1.5 3 - - hydrogenated polyisobutene 0.5 0.75 1.0 2.0 0.25 octyldodecanol 0.5 1.0 0.75 3.0 0.25 cyclomethicone 12.5 15 28.0 25.0 17.5 dimethicone 5.0 13.0 5.0 12.0 15.0 behenyl 1 - 2 1 - stearyl - 1 - 1 - carbomer Carbomer - 0.5 0.75 0.15 - Glycerylglucose - 10 15 20 - Perfume phase Glycerylglucose 2.5 - - - 8.0 Perfume q, s, - - - q, s, water phase methylparaben 0.4 0.1 0.05 0.3 0.4 Propylparaben 0.3 0.4 0.25 0.15 - glycerin 5 10 3 15 7.5 water ad 100 ad 100 ad 100 ad 100 ad 100

Production process for the production of an O / W emulsion on a 500 kg Beco mixer:

The fat phase is heated in the boiler 2 with stirring at 1 meter / second to 80 ° C until all raw materials are clearly dissolved. The water phase is also heated in boiler 1 with stirring at 1 meter / second to 80 ° C. When all phases have reached 80 ° C, a vacuum of at least -0.5 bar is applied.

The fat phase is sucked into the boiler 1, into the water phase. The circulation homogenizer is switched on at 14 meters / second to achieve a homogeneous emulsion. After phase combination of the water and fat phase, the thickener phase is sucked in while the homogenizer is running. After 8 minutes, the homogenizer is switched off and the cooling is made with a capacity of 8600 liters / hour. After 30 minutes 35 ° C are reached and the perfume phase or further Extraphasen be sucked. After another 30 minutes 28 ° C are reached and with the circulation homogenizer the final viscosity is set. It is homogenised at 25 meters / second for 8 minutes. It is then cooled for a further 10 minutes, until the finished emulsion can be pumped into a storage container or to the filling line.

Claims (2)

Process for the preparation of cosmetic and / or dermatological emulsions, characterized in that (i) one or more glucosylglycerides of a water phase or (ii) one or more glucosylglycerides of an oil phase or (iii) one or more glucosylglycerides of a water and an oil phase is added or and at temperatures not exceeding 40 ° C, (i) the water phase is combined with an oil phase or (ii) the oil phase is combined with a water phase or (iii) both phases are combined. A method according to claim 1, characterized in that the glucosylglyceride or in the water and / or oil phase in concentrations of 0.01-40.00 wt .-%, preferably 0.05-15.00 wt .-%, especially preferably 0.1-6.00 wt .-%, each based on the total weight of the composition.