EP3328502A1

EP3328502A1 - Antiperspirant

Info

Publication number: EP3328502A1
Application number: EP16736494.2A
Authority: EP
Inventors: Elke Grotheer; Franz STÄB; Thomas Schmidt-Rose; Michael Seet; Robert Klauck; Frank Lehmbeck
Original assignee: Beiersdorf AG
Current assignee: Beiersdorf AG
Priority date: 2015-07-27
Filing date: 2016-07-11
Publication date: 2018-06-06
Also published as: US20200078276A1; BR112018001791A2; DE102015214143A1; AU2016299197A1; WO2017016858A1; JP2018521096A; CN107921297A

Abstract

The use of low-molecular weight polysilicic acids in combination with one or more stabilizers in cosmetic or dermatological preparations leads to a reduction or prevention of apoeccrine perspiration.

Description

antiperspirant

The invention is the use of low molecular weight, highly amorphous silicic acids in combination with one or more stabilizers in cosmetic or dermatological preparations for reducing or preventing apoekrine perspiration.

As sweat becomes one of the skin of humans over so-called sweat glands

designated secreted aqueous secretion. There are three types of sweat glands in the skin, namely, apocrine, eccrine, and apoekrine sweat glands (Int J Cosmet Sei. 2007 Jun;

29 (3): 169-79). The eccrine sweat glands in humans are distributed practically throughout the body and can produce significant amounts of a clear, odorless secretion that is over 99% water. In contrast, the apocrine sweat glands occur only in the hairy body areas of the armpit and genital region and on the nipples. They produce small amounts of a milky secretion that contains proteins and lipids and is chemically neutral.

Sweating, also known as transpiration, is an effective mechanism to release excess heat and thereby regulate body temperature. The volume-rich aqueous secretion of the eccrine glands, which can produce up to 2-4 liters per hour or 10-14 liters a day in adults, is used for this purpose. The sweat - especially the secretion of apocrine sweat glands - is also signaled by the sense of smell. In humans, the apocrine sweat plays in particular in connection with the emotional or stress related

Sweating matter.

Cosmetic antiperspirants or deodorants / deodorants are used to eliminate body odor or to reduce their formation. Body odor arises when the per se odorless fresh sweat by microorganisms such. Staphylococci and

Corynebacteria is decomposed.

In general parlance is not always a clear separation of concepts

"Deodorant" and "antiperspirant". Rather, especially in German-speaking countries, products for use in the armpit area are referred to as deodorants or "deodorants", irrespective of the question of whether an antiperspirant effect is also present. Antiperspirants (AT) are antiperspirants that, in contrast to the deodorants which generally prevent microbial decomposition of already formed perspiration, are said to prevent the secretion of sweat at all.

In contrast to the antiperspirants pure deodorants cause no active

Influencing the sweat secretion, but only the control or influence of the body or armpit odor (odor control agent). The usual cosmetic deodorants are based on different active principles.

Common mechanisms of action for this are antibacterial effects, such as e.g. The non-colloidal silver also shows odor neutralization (masking), influencing of bacterial metabolisms, the pure perfuming as well as the use of precursors of certain perfume components, which are converted by enzymatic reactions to fragrant substances.

Sweat odor consists to a large extent of branched-chain fatty acids, which are released by bacterial enzymes from odorless sweat. Classic deodorizing agents counteract this by reducing the growth of bacteria. Frequently, however, the substances used for this purpose also act nonselectively against useful skin germs and can lead to skin irritations in sensitive individuals.

The classic antiperspirants used are, in particular, aluminum salts or aluminum / zirconium salts. These inhibit the flow of sweat by obstructing the excretory ducts of the sweat glands by precipitating them together with the skin's own proteins and thus leading to so-called plugs. Therefore, there may be a congestion of sweat within the gland.

The effect of antiperspirants based on AI salts against thermal sweating under normal physiological conditions has been well studied. Whether this obstruction by denaturation of keratin or by clumping of

Corneocytes in the sweat gland duct (Shelley WB and Hurley HJ, Acta, Derm. Venereol. (1975) 55: 241-60), or by the emergence of an ACH / AZG gel (Reiler HH and Luedders WL, in: Advances in Modern Hemisphere Publishing Company, Washington and London (1977) Vol. 4: 1-5), which is formed by neutralization in the sweat gland duct, remains open.

The thus obtained and known constipation is effective only in the short term. strong

Sweat or clean the armpit as part of the normal body cleansing routine lift the blockage again and thus also the antiperspirant effect. However, the resulting need to apply antiperspirant (AT) products at least once a day may cause skin irritation, especially after shaving or in or on previously damaged areas of the skin. In addition, such aluminum salts as aluminum hydroxychlorides can cause skin damage if used frequently and on sensitive persons. In addition, the use of the aluminum salts can cause discoloration of textiles which come into contact with the antiperspirant.

The additional use of antimicrobial substances in cosmetic antiperspirants can reduce the bacterial flora on the skin. Ideally, only the odor causing microorganisms should be effectively reduced. The sweat flow itself is not affected, in the ideal case, only the microbial decomposition of the sweat is temporarily stopped.

Usually antiperspirants (AT) and deodorants (Deo) are offered in a variety of product forms, with scooters, pump sprayers and aerosols dominating in Europe, and deodorant sticks ("sticks") in the US, Central and South America. There are both anhydrous (suspensions) and hydrous products (hydro-alcoholic formulations,

Emulsions).

A satisfactory deodorant means the following conditions are met: 1)

Protection of the natural biology of the skin 2) Fragrance neutrality 3) Activity only with respect to deodorization, i. only avoidance and / or elimination of body odor 4) prevention of the formation of resistant bacterial strains 5) avoidance of accumulation of the active ingredients on the skin 6) harmlessness in case of overdose or other improper use 7) good cosmetic application 8) easy handling (eg as liquid) and universal usability in a wide variety of cosmetic and external preparations. 9) Excellent skin and mucous membrane compatibility 10) Use of environmentally friendly substances

Apart from the liquid deodorants and antiperspirants, solid preparations, for example powders, powder sprays, are also known and customary as intimate cleaners.

A disadvantage of the aluminum salts used hitherto for sweat inhibition is the currently not yet fully understood long-term toxicity. Aluminum has been suspected for a long time to promote or trigger neurodegenerative diseases such as dementia, in particular Alzheimer's disease. Also, aluminum is associated with the development of breast cancer. So far, there is no verified evidence that works over the skin aluminum-containing AT agents are involved. If the skin is intact, the maximum admissible intake levels can not be achieved.

In view of the data, however, the move away from aluminum-containing AT agents is advantageous, so that the industry is desperately looking for aluminum-free alternatives. Because of this problem, it is desirable to provide products that achieve an antiperspirant effect without the use of Al salts.

An alternative to Al salts are short-chain silicates in the form of silicic acids, which can reliably suppress sweat formation.

Silica acids are the oxygen acids of silicon. The easiest

Silica is monosilicic acid (orthosilicic acid) Si (OH) ₄ . It is a weak acid (pKsl = 9.51, pKs2 = 11, 74) and tends to condense. Dehydration leads to compounds such as silicic acid (pyrosilicic acid) (HO) 3Si-0-Si (OH) ₃ and tri-silica (HO) ₃ Si-O-Si (OH) ₂ -O-Si (OH) ₃ . Cyclic (annular) silicas are z. B.

Cyclotric acid and cyclotetravelic acid with the general empirical formula [Si (OH) 2-0-] _n . Polymers are sometimes referred to as meta-silicic acid (H2S1O3, [-Si (OH) 2-0-] _n ). If these low-molecular-weight silicic acids continue to condense, amorphous colloids (silica sol) are formed. The general empirical formula of all silicas is H2n + 2Si _n 03n + i. The empirical formula is often S1O2 ^■ n H2O; However, the water is not with silicas

Water of crystallization, but can be cleaved only by a chemical reaction and forms from constitutionally bound hydroxy groups.

Generally, the lower-water products of orthosilicic acid are termed

Polysilicic acids summarized. Formal end product of dehydration is

Silica, the anhydride of silicic acid. The salts of acids are called silicates.

Technically used or prepared alkali metal salts are often called water glasses. The esters of silicic acids are called silicic acid esters.

As low molecular weight, highly amorphous silicic acids are within the meaning of the invention, only the

Silica acids are understood to have an extension of 1 to 100 nm, measured by dynamic light scattering. These low molecular weight, highly amorphous silicas are also known as low molecular weight polysilicic acids and are referred to below as NPK.

NPK can be represented as follows: a) Preparation of an alkaline silicate solution with a pH> = 10 b) lowering the pH by adding an acid to a pH <= 1, wherein the polysilicic acid is formed and wherein the lowering of the pH occurs within less than 60 seconds

c) raising the pH to a physiologically acceptable pH of at least 3.5 by adding a base

However, the silicas prepared by this method are stable only at these very low pH levels. From a pH of 3.5 condensation occurs, which is noticeable by precipitation gelation. These precipitates of high molecular weight silicic acids no longer have an AT effect. Since pH values below 3.5 are physiologically incompatible, formulations must be found in which the pH is at least 3.5 and in which there is no gelation or precipitation of amorphous colloids (silica sol).

It would therefore be desirable to provide an antiperspirant which does not show the abovementioned disadvantages and side effects, in particular ACH-containing preparations.

It would also be desirable to provide an antiperspirant preparation which enriches the state of the art and represents an alternative to the known preparations, in particular ACH-containing preparations.

In particular, it is also desirable to provide an antiperspirant active which allows for the widest possible possibilities of galenic incorporation into cosmetically acceptable and attractive formulary systems.

A further object of the present invention was thus to develop AT agents / preparations which are suitable as a basis for cosmetic deodorants or antiperspirants and which do not have the disadvantages of the prior art. Furthermore, it was therefore an object of the invention to develop cosmetic bases for cosmetic Antritranspirantien, which are characterized by good skin compatibility.

The object of the invention is the use of physiologically compatible

Antiperspirant preparations containing low molecular weight polysilicic acids (NPK) in

Combination with one or more stabilizers to reduce or prevent apogex sweat formation.

After all this it was surprising and unpredictable that siliceous

Preparations having a pH of at least 3.5, containing NPK and one or more Stabilizers for use as hypoallergenic antiperspirants, ie to reduce or prevent apoekkrinen sweat formation, and eliminate the disadvantages of the prior art.

It was surprising that the preparations used according to the invention are not only outstandingly suitable for cosmetic purposes, but moreover are more effective and gentler than the use of prior art compositions.

The invention is the use of NPK in combination with one or more stabilizers - hereinafter referred to as stabilized NPK, in cosmetic or dermatological formulations having a pH of at least 3.5 for reducing or preventing apoecraine perspiration.

The invention accordingly comprises the use of NPK, as antiperspirant active, preferably in topically administrable, in particular cosmetic and / or dermatological, preparations, wherein the pH of the preparation is not less than 3.5.

Precipitation at pH values above 3.5 can be reliably achieved by adding

Stabilizers are prevented during the preparation of the preparations to be used according to the invention.

The stabilizers are selected from group A:

Hexenol ice 3 (CAS 928-96-1), terpineol (CAS 8000-41 -7), linalool (CAS 78-70-6),

Tetrahydrolinalool (CAS 78-69-3), triethyl citrate (CAS 77-93-0), 2-isobutyl-4-hydroxy-4-methyltetrahydropyran (CAS 63500-71-0), hexyl salicylate (CAS 6259-76-3 ), Phenylethyl alcohol (CAS 60-12-8), 3-methyl-5-phenyl-1-pentanol (CAS 55066-48-3), 2,6-dimethyl-7-octene-2-o (CAS 18479 -58-8), benzyl salicylate (CAS 1 18-58-1), geraniol (CAS 106-24-1), citronellol (CAS 106-22-9) and ethyllinalool (CAS 10339-55-6); group B: alcohols and diols and group C: substances with at least three hydroxyl groups.

Particularly advantageous stabilizers from group A are: linalool (CAS 78-70-6), benzyl salicylate (CAS 1 18-58-1), geraniol (CAS 106-24-1) and citronellol (CAS 106-22-9.

Particularly advantageous group B stabilizers are: ethanol, 2-propanol, PEG 8, triethylene glycol, methylphenylbutanol, decanediol, polyglyceryl-2-caprate, oxalic acid. Particularly advantageous stabilizers from group C are: sucrose (mannose, mannitol), glycerol, pentaerythritol, threitol, erythritol, hyaluronic acid

The topical application of preparations - ie the use of cosmetic or dermatological preparations on the skin - containing NPK in combination with one or more stabilizers chosen from the group A, B and / or C allows the reduction or prevention of stress sweating.

In the context of the invention, the possibility of reducing or preventing perspiration is understood as an antiperspirant effect. That NPK act as a sweat inhibitor and reduce the formation of sweat and thus indirectly also the smell of sweat. By stabilizing the NPK with the stabilizers mentioned above, preparations are possible which have a high physiological compatibility.

The combination of NPK with the stabilizers according to the invention in cosmetic or dermatological preparations offers a more effective use against perspiration.

The combination of NPK with the stabilizers according to the invention is provided in cosmetic or dermatological preparations, in particular for topical application.

Use of stabilized NPK according to the invention allows antiperspirant activity on the order of known and proven antiperspirant active ingredients, the required concentration of NPK being much lower than when using ACH.

This also leads to the elimination of the disadvantages listed, such as skin irritation, in particular due to low pH of unstabilized silicas and the toxicity of aluminum compounds under discussion.

In addition to the NPK, preferably cosmetic preparations suitable for use according to the invention therefore comprise no further antiperspirant active substances, in particular no aluminum salts, in particular no ACH and / or AACH (activated aluminum chlorohydrate). A significant advantage of the use according to the invention is, moreover, that there is no discoloration on the skin or clothing as compared with the AT agents based on aluminum salts. The so-called white is omitted as well as the

Repeated use and washing in directly on the underarm skin overlying textiles to be observed residues. The stabilized silicas can be easily incorporated into the products according to the invention

Be incorporated using suitable compositions. They are preferred as NPK suspension added to the other constituents of the formulations. The proportion of NPK suspension can make up to 98% of the total amount of the formulation. In the simplest case, only a thickener and a perfume are added to the NPK suspension, perfume meaning a mixture comprising one or more olfactorily detectable individual substances.

Silica acids stabilized for use according to the invention can be e.g. Produce according to the following methods on a laboratory scale:

Method I:

1. Preparation of a dilute aqueous Na silicate solution having a pH> 1 1 2. Reduction of the pH from> 1 1 to <1 by adding an appropriate amount of one or more strong acids within 5-10sec.

3. Increase the pH to a cosmetically acceptable level of at least 3.5 by adding one or more bases

4. Addition of the Stabilizer The acid used in step 2 for pH reduction is particularly suitable

Mineral acids such as hydrochloric acid, sulfuric acid or phosphoric acid, their anions

Physiologically compatible and to keep well in solution. However, the pH reduction can also be carried out any other acids, as long as they a) can reduce the pH accordingly and b) their salts, in particular sodium salt, are physiologically acceptable or cause no skin irritation. Preference is given to pH reduction

Hydrochloric acid used.

The fast pH reduction is crucial for the successful formation of the NPK.

If the pH reduction is too slow, form very high molecular weight silica, which have no antiperspirant activity, to gelation. Increasing the pH in step 3 to a cosmetically acceptable level may be accomplished with caustic soda, caustic potash, or with weaker bases. Useful bases include: 2-aminobutanol, 2- (2-aminoethoxy) ethanol, aminoethyl propanediol, aminomethyl propanediol, aminomethyl propanol, aminopropanediol, bis-hydroxyethyl tromethamine, butyl diethanolamine, butylethanolamine, dibutyl ethanolamine, diethanolamine, diethyl

Ethanolamines, diisopropanolamines, dimethylamino methylpropanol, dimethyl

Isopropanolamines, dimethyl MEA, ethanolamines, ethyl ethanolamines, isopropanolamines, Methyl Diethanolamine, Methylethanolamine, Triethanolamine, Triisopropanolamine,

Tromethamines, polyethylenimines, tetrahydroxypropylethylenediamine, ammonia.

The increase in pH can also be carried out with buffer systems, which is also considered in the context of the invention as a base, which are added either in aqueous solution or anhydrous. The buffer systems can consist of the abovementioned bases and cosmetically acceptable acids and have a pH of from 3 to 11, preferably from 7 to 9.

Examples of acids which are particularly suitable for the production of buffers are citric acid, lactic acid, tartaric acid, fatty acids, phosphoric acid, phosphonic acids, polyacrylic acids, succinic acid, malic acid, oxalic acid, amino acids.

Particularly suitable for the base used in step 3 for pH increase

Alkali hydroxides whose cations are physiologically compatible and easy to keep in solution. In particular, sodium and / or potassium hydroxide solution are suitable for raising the pH. The pH increase can be advantageously carried out in stages, with a more concentrated base, e.g. 5N NaOH, and only to adjust the final pH, a less concentrated base, e.g. 0.5N NaOH, is used.

It is advantageous to first bring the pH to pH 2 with 5N NaOH and then further increase to at least pH 3.5 with 0.5N NaOH.

Particularly suitable stabilizers for this preparation method are ethanol, glycerol, 2-propanol, PEG 8, triethylene glycol, urea, oxalic acid, hyaluronic acid, ethylhexylglycerol, pentaerythritol, threitol, erythritol, methylphenylbutanol, polyglyceryl 2-caprate, decanediol

Method II:

1 . Preparation of a dilute aqueous Na silicate solution with a pH> 1 1

2. Addition of at least one stabilizer 3. Reduction of the pH from> 1 to <1 by addition of an appropriate amount of one or more strong acids within 5-10 seconds.

4. Increase the pH to a cosmetically acceptable level of 3.5 by adding one or more bases

The same conditions apply to the pH reduction (step 3) and the pH increase (step 4) as to step 2 and step 3 of method I. Suitable stabilizers for this stabilized NPK preparation process are sucrose, mannose and / or mannitol.

Particularly preferred is a use of glycerol and ethanol in a ratio of 1: 10 to 6:10, in particular 5 to 30 wt .-% glycerol and 30 wt .-% EtOH based on the total amount of sodium silicate solution prepared in step 1.

Method III:

1. Preparation of a dilute Na silicate solution having a pH> 1 1, wherein the or

Simultaneously, stabilizers as part of the solvent 2. Reduction of the pH from> 1 1 to <1 by adding an appropriate amount of one or more strong acids within 5-10sec.

The same conditions apply to the pH reduction (step 2) and the pH increase (step 3) as to step 2 and step 3 of method I.

Suitable stabilizers for this stabilized NPK preparation process are glycerol.

In particular, at very high glycerol concentrations of over 70%, the pH increase with 0.1 to 0.5 M sodium hydroxide in glycerol is advantageous, as this possible, pH peaks' can be prevented. Decisive in the production of NPK is the step of exothermic pH reduction in all three cases. This pH reduction must be very fast, so that no condensation of the monomers can take place.

For a required rapid, erratic and uniform change in the pH in the batch volume, a high stirring speed with very good mixing of the required. Slow or incomplete mixing leads to a reduction in stability and, if necessary, a reduction in AT performance.

On a larger scale, this rapid pH reduction can no longer be handled as a 'batch' process due to the high amount of heat to be removed. On a large scale, rapid pH reduction is therefore only possible in a continuous process in which step 2 (method I and III) or step 3 (method II) by combining the reactants

Sodium silicate solution and acid in a flow reactor, possible.

The obtained according to the methods I to III stabilized NPK solutions are at

Room temperature sufficiently stable for use in antiperspirant formulations which can be used according to the invention. The stability increases with decreasing temperature, so that storage in the refrigerator (at 5 to 8 degrees Celsius) is advantageous.

According to the use according to the invention, the cosmetic preparations (antiperspirants) containing stabilized NPK in the form of aerosols, ie

Aerosol containers, squeeze bottles or sprayable by a pumping device

Or in the form of by means of roll-on devices (application over

Movement body, for example ball or roller) can be applied to liquid compositions to be applied. Also as AT-sticks and in the form of W / O or O / W emulsions which can be applied from normal bottles and containers, e.g. Creams or lotions.

A good method is also the spreading or rubbing by means of flat applicators, in particular applicators with flocked and / or textile surface, since they have a low tendency to clog.

Furthermore, the cosmetic antiperspirants containing stabilized NPK may advantageously be present in the form of tinctures, intimate cleansers, shampoos, shower or bath preparations, powders or powder sprays. The preferred form of application for antiperspirants with stabilized NPK are hydrous aerosols which come on the market in lacquered aluminum cans (protective lacquer to prevent corrosion on the inside of the container). In the hydrous aerosols, especially the W / O emulsions are mentioned. This form of application is preferred, since it represents the most common form in the world of deodorant / AT. It is advantageous with respect to aluminum chlorohydrate-containing AT sprays that the stabilized NPK is present dissolved in the preparation and does not have to be resuspended by shaking before using the spray. The clogging probability of the nozzles is thereby reduced.

Furthermore, it is possible and advantageous to use the stabilized NPK in O / W emulsions in roll-ons and pump sprays.

Like the aerosol sprays, pump sprays offer a contactless application of the AT preparation to the skin. For pump sprays, however, pressure-resistant containers can be dispensed with. pump Sprays can be made metal-free, especially aluminum-free. For example, containers made of PE, PP or PET, which are closed with a metal-free atomizing pump, are advantageous, wherein metal-free means that the pumped preparation does not come into contact with metallic components. Due to the very good packaging compatibility is also a use in hydrous

Formulations of AT sticks recommended, since even after storage at + 40 ° C over a period of 6 months hardly changes in packaging material.

The preparation can be advantageously used according to the invention as impregnation medium for a plaster or cloth. For this reason, patches and wipes soaked with the preparation according to the invention are also suitable application forms for the purposes of the use according to the invention.

Aerosol Spray:

The stabilized NPK are in the antiperspirant according to the invention preferably in an amount of 0, 1 to 10 wt .-%, content of NPK based on the

Total mass of the preparation, i. including the possibly existing propellants used. Particularly advantageous are concentrations of 0.5 to 3 wt .-%.

As a drug solution, the sum of all ingredients without the propellant gas is called, since the propellant usually added only at the bottling.

AT roller: The proportion of one or more stabilizers can advantageously be selected up to 85% by weight, in particular up to 30% by weight, based on the total mass of the preparation.

The proportion of SiO 2 equivalents is advantageously selected in the range from 0.1 to 6% by weight, preferably 0.5 to 3% by weight, based on the total mass of the preparation.

Pump spray: The proportion of one or more stabilizers can advantageously be selected up to 85% by weight, in particular up to 30% by weight, based on the total mass of the preparation.

The proportion of NPK is advantageously selected in the range from 0.1 to 6% by weight, preferably 0.5 to 3% by weight, based on the total mass of the preparation. Cosmetic and dermatological preparations comprising the NPKs stabilized according to the invention may contain cosmetic adjuvants such as are conventionally used in such preparations, for example preservatives, preserving auxiliaries,

Bactericides, perfumes, UV filters, antioxidants, water-soluble vitamins, minerals, suspended solid particles, foaming inhibitors, dyes, pigments having a coloring effect, thickeners, moisturizing and / or moisturizing substances or other common ingredients of a cosmetic or dermatological Formulation such as electrolytes, organic solvents, alcohols, polyols, emulsifiers, polymers, foam stabilizers or silicone derivatives. The preparations are preferably produced and used in an optically appealing transparent manner.

The cosmetic preparation according to the invention is advantageously characterized in that it is in the form of an aqueous or aqueous-alcoholic solution, an emulsion (W / O, O / W, W / Si, Si / W or multiple emulsion, macro-, micro- or nanoemulsion ), a dispersion, a Pickering emulsion, a gel, a hydrodispersion gel or anhydrous

Preparation is present.

According to the invention, the preparation may also be present in the form of a low-viscosity, sprayable aqueous or aqueous-alcoholic solution, in the form of a gel, in a wax matrix, a stick form, as an ointment, cream or lotion (possibly sprayable). Advantageously, preparations according to the invention may also be added with deodorants. The usual cosmetic deodorants are based on different active principles. By using antimicrobial substances as cosmetic deodorants, the bacterial flora on the skin can be reduced. Ideally, only the odor causing microorganisms should be effectively reduced. The sweat flow itself is not affected, in the ideal case, only the microbial decomposition of the sweat is temporarily stopped. The combination of astringents with antimicrobial substances in one and the same composition is also common.

All agents which are common as deodorants can advantageously be used, for example odor maskers such as the common perfume ingredients, odor absorbers, for example the phyllosilicates described in DE 40 09 347, of these in particular montmorillonite, kaolinite, mit, beidellite, nontronite, saponite, hectorite, bentonite, smectite , Further, for example, zinc salts of ricinoleic acid. Germ-inhibiting agents are also suitable for incorporation into the preparations according to the invention. Advantageous substances are, for example, 2,4,4'-trichloro-2'-hydroxydiphenyl ether (Irgasan), 1, 6-di- (4-chlorphenylbiguanido) hexane (Chlorhexidine), 3,4,4'-trichlorocarbanilide, quaternary ammonium compounds, clove oil, mint oil, thyme oil, triethyl citrate, farnesol (3,7,1-trimethyl-2,6,10-dodecatriene-1-ol),

Ethylhexylglycerin, phenoxyethynol, Pirocton olamine, caffeine and in DE 37 40 186, DE 39 38 140, DE 42 04 321, DE 42 29 707, DE 42 29 737, DE 42 37 081, DE 43 09 372, DE 43 24 219 described effective agents. Also, sodium bicarbonate is advantageous to use.

Likewise, an antimicrobial silver citrate complex, as described in DE 202008014407, can preferably be used as a deodorizing component in conjunction with NPK. Preferred cosmetic preparations which can be used according to the invention may also contain polymers. The polymers preferably originate from the range of celluloses and / or polystyrenes. They are advantageously hydrophobic or hydrophilic modified.

Usable polymers therefore include celluloses, polystyrenes and / or alkyl-acrylic

Crosspolymers and may optionally be added to the NPK preparations.

In addition to water, ethanol and isopropanol, glycerol and propylene glycol, skin-care fat or fat-like substances and also oils such as oleic acid decyl ester, cetyl alcohol, cetylstearyl alcohol and 2-octyldodecanol, which are customary for such preparations, can be used as customary cosmetic ingredients of the NPK-containing preparations for use according to the invention

Quantity ratios are used and slime-forming substances and thickeners, e.g. Hydroxyethyl or hydroxypropyl cellulose, polyacrylic acid, polyvinylpyrrolidone and waxes. The emulsifiers known for cosmetic preparations have proven to be advantageous for the preparations which can be used according to the invention.

Polyoxyethylene (20) sorbitan monolaurate, polyoxyethylene (20) sorbitan monopalmitate,

Polyoxyethylene (20) sorbitan monostearate, polyoxyethylene (20) sorbitan monooleate, sorbitan trioleates, polyglyceryl-10 stearates, polyglyceryl-4 caprates, lauryl glucosides, polyglyceryl-2 dipolyhydroxyl stearates, polyglyceryl-10 laurates, polyglyceryl-4 laurates, decyl

Glucoside, Propylene Glycol Isostearate, Glycol Stearate), Glyceryl Isostearate), Sorbitan Sesquioleate, Glyceryl Stearate, Lecithin, Sorbitan Oleate, Sorbitan Monostearate NF, Sorbitan Stearate, Sorbitan Isostearate, Steareth-2, Oleth-2, Glyceryl Laurate, Ceteth-2, PEG-30 Dipolyhydroxystearates, Glyceryl Stearate SE, Sorbitan Stearate (and) Sucrose Cocoate, PEG-4 Dilaurate, PEG-8 Dioleate, Sorbitan Laurate, PEG-40 Sorbitan Peroleate, Laureth-4, PEG-7 Glyceryl Cocoate, PEG-20 Almond Glycerides, PEG-25 Hydrogenated Castor Oil, Stearamide MEA, Glyceryl Stearate + PEG-100 Stearate, Polysorbate 85, PEG-7 Olivate, Cetearyl Glucoside, PEG-8 Oleate, Polyglyceryl-3 Methyglucose Distearate, PG-10 Stearate, Oleth-10 . Oleth-10 / Polyoxyl 10 Oleyl Ether NF, Ceteth-10, PEG-8 Laurate, Ceteareth-12, Cocamide MEA, Polysorbate 60 NF, Polysorbate 60, PEG-40 Hydrogenated Castor Oil, Polysorbate 80, isosteareth-20, PEG-60 Almond Glycerides, Polysorbate 80 NF, PEG-150 Laurate, PEG-20 Methyl Glucose Sesquistearate, Ceteareth-20, Oleth-20, Steareth-20, Steareth-21, Ceteth-20, Isoceteth-20, PEG-30 Glyceryl Laurate, Polysorbates 20, Polysorbate 20 NF, Laureth-23, PEG-100 Stearate, Steareth-100, PEG-80 Sorbitan Laurate.

Preference is given to using glyceryl isostearates, glyceryl stearates, steareth-2, ceteareth-20, steareth-21, PEG-40 hydrogenated castor oil, PG-10 stearates, isoceteth-20, isosteareth-20 and ceteareth-12. Also known as solubilizers but useful as emulsifiers for the formulations useful in the present invention are PEG-40 Hydrogenated Castor Oil, Polysorbate 80, Laureth-23, PEG-150 Laurate and PEG-30 Glyceryl Laurate.

In addition to or instead of nonionic emulsifiers and cationic emulsifiers are suitable to create stable formulations with the invention Poylquaternium polymers. Preferred suitable cationic emulsifiers are from the group Cetrimonium Chloride, Palmitamidopropyltrimonium Chloride, Quaternium-87, Behentrimonium Chloride, Distearoylethyl Dimonium Chloride, Distearyldimonium Chloride, Stearamidopropyl

Dimethylamine and / or Behentrimonium methosulfate.

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 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 ,

If, within the meaning of the present invention, the cosmetic or dermatological preparation is a solution or emulsion or dispersion, the solvent,

Bodying agents and / or main care agents are used:

- water or aqueous solutions

- Oils, such as triglycerides of capric or caprylic and alkyl benzoate, but preferably cyclic silicone oils or volatile hydrocarbons;

- fats, waxes and other natural and synthetic fatty substances, preferably esters of fatty acids with alcohols of low C number, for example with isopropanol, propylene glycol or Glycerol, or esters of fatty alcohols with alkanoic acids of low C number or with fatty acids; Vegetable oils such as avocado oil, meadowfoam seed oil, olive oil, sunflower oil, rapeseed oil, almond oil, evening primrose oil, coconut oil. Palm oil, linseed oil, shea

Butter.

Alcohols, diols or polyols of low C number, and their ethers, in particular 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.

Skin care substances such as e.g. Panthenol, allantoin, urea, urea derivatives,

Guanidine, ascorbic acid, glyceryl glucose,

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

Suitable propellants for cosmetic and / or dermatological preparations which can be sprayed from aerosol containers in the context of the present invention are the customary known volatile volatile liquefied propellants, for example hydrocarbons (propane, butane, isobutane), which can be used alone or mixed with one another. Also

Dimethyl ether, nitrous oxide, carbon dioxide, nitrogen and compressed air are advantageous to use.

Of course, the person skilled in the art knows that there are per se nontoxic propellant gases which would in principle be suitable for the realization of the present invention in the form of aerosol preparations, but which should nevertheless be dispensed with because of a harmful effect on the environment or other accompanying circumstances, in particular fluorohydrocarbons and chlorofluorocarbons (US Pat. CFC).

In aerosol preparations oils are often added, which are miscible in the drug solution with the propellant gas (propane, butane, isobutane), as an oil that is immiscible, too

Rainfall leads, which lead in the glass aerosol that the drug particles are not aufzuschütteln more.

Cosmetic preparations within the meaning of the present invention may also be present as gels which, in addition to an effective content of the active ingredient according to the invention and solvents usually used for it, preferably water, also organic thickeners (thickeners), e.g. Tamarind flour, Konjakmannan, Guaran, Hydroxypropylguar,

Locust bean gum, gum arabic, xanthan gum, sodium alginate, cellulose derivatives, preferably methylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose or a mixture of Polyethylene glycol and polyethylene glycol stearate or distearate. The

Thickener is included in the formulation e.g. in an amount of between 0.1 and 40% by weight, preferably between 0.5 and 25% by weight.

Otherwise, the usual measures for putting together cosmetic

Observe formulations that are familiar to the expert.

Following are advantageous embodiments of the present invention.

The following examples illustrate the preparations according to the invention which serve to reduce or prevent perspiration. The numbers represent parts by weight, based on the total mass of the preparation.

Alcoholic-aqueous roll-on data in% by weight

1 2 3 4 5 6

Sodium silicate 11,12 11,12 11,12 11,12 11,12 11,12

Water (demineralized) 51,32 40,32 40,32 51,32 46,47 51,37

Ethanol 30 30 20 10 30 30

Glycerol 11 21 5

PEG-200 (Sigma) 20

HCl, 37% 1.76 1.76 1.76 1.76 1.76 1.76

Sodium hydroxide 0.3 0.3 0.3 0.3 0.3 0.3

Persea Gratissima Oil (IMCD 0.1 0.1 0.1 0.1 0.1 0.1 Germany)

PEG-40 Hydrogenated Castor Oil 2 2 2 2 2 2 (Eumulgin CO 40, BASF)

Perfume 1 1 1 1 1 1

Citric Acid (Citric Acid Monohydrate, 0.05 0.05 0.05 0.05 0.05 0.05 Jungbunzlauer)

Hydroxyethylcellulose (Natrosol 250 HHX 0.35 0.35 0.35 0.35 0.2

pharm; Ashland)

Xanthan gum (Keltrol CG-F, Rahn) 0.3

PEG-8 (Kollisolv PEG 400, BASF) 2 2 2 2 2 2 Total 100 100 100 100 100 100

Alcoholic-aqueous spray in% by weight

1 2 3 4 5 6

Sodium silicate 11,12 11,12 11,12 11,12 11,12 11,12

Water (demineralised) 51,67 40,67 40,32 51,32 46,67 51,67

Ethanol 30 30 20.35 10.35 30 20

Glycerol 11 21 5

PEG-200 (Sigma) 20 10

HCl, 37% 1.76 1.76 1.76 1.76 1.76 1.76

Sodium hydroxide 0.3 0.3 0.3 0.3 0.3 0.3

Persea Gratissima Oil (IMCD 0.1 0.1 0.1 0.1 0.1 0.1 Germany)

PEG-40 Hydrogenated Castor Oil 2 2 2 2 2 2 (Eumulgin CO 40, BASF)

Perfume 1 1 1 1 1 1

PEG-8 (Kollisolv PEG 400, BASF) 2 2 2 2 2 2

Total 100 100 100 100 100 100

O / W emulsion (roll-on) (cold data in% by weight

produced)

1 2 3 4 5

Water 50.89 40.89 39.89 44.62 45.89

Ethanol 23,68 13,68 23,68 30,00 23,68

Sodium Silicate 11,12 11,12 11,12 11,12 11,12

HCl, 37% 1.76 1.76 1.76 1.76 1.76

NaOH 0.30 0.30 0.30 0.30 0.30

Glycerine 11.00 5.00

PEG-200 (Sigma) 20.00

Benzyl alcohol 0.30 0.30 0.30 0.30 0.30

Phenoxyethanol 0.50 0.50 0.50 0.50 0.50

Cocamidopropylamine oxides 10.00 10.00 10.00 10.00 10.00 (Amphoteric surfactant COX / C, Zschimmer &

Black)

Persea Gratissima Oil 0,10 0,10 0,10 0,10 0,10

Hydroxyethylcellulose 0.35 0.35 0.35 0.00 0.35

Xanthan gum (Keltrol CG-F, Rahn) 0.30

Perfume 1.00 1.00 1.00 1.00 1.00

100.00 100.00 100.00 100.00 100.00

When filled as an aerosol, the propellant is a hydrocarbon mixture, eg. B. butane, isobutane, propane with a pressure of 2.7 bar in a filling ratio of emulsion to propellant from 5:95 to 40:60 weight percent. Examples 3 and 4 of the table are advantageously filled 20:80.

Preparation of a cosmetic or dermatological preparation for use according to the invention from a stabilized NPK solution prepared according to Methods I to III and a pre-emulsion:

1. Preparation of a pre-emulsion in which the water-soluble constituents are heated to 75 ° C together with the stated amount of water. The oil components and emulsifiers are heated separately to 75 ° C. The phases are combined and homogenized. The emulsion is cooled to room temperature with stirring.

2. Preparation of a Solution of Stabilized NPK by Method I to III (Silica Pre-Solution)

3. The cooled pre-emulsion is added to the silica pre-solution with continuous stirring. It is stirred until completely mixed.

The pre-emulsion can be mixed in various proportions with the silica precursor with stirring. The mixing ratio of pre-emulsion to silica pre-solution is 10:90 to 90:10.

Silica precursor data in% by weight

1 b 2b 3b 4b 5b

Sodium Silicate 15.9 15.9 15.9 15.9 15.9

Water (demineralized) 42.6 35.5 42.6 42.6 39.7

Ethanol 17, 1 0.0 10.0 7, 1 7, 1

Glycerol 21, 4 28.6 28.6 7, 1 17.1 PEG-200 (Sigma) 0.0 17, 1 0.0 24.3 17.1

Hydrochloric acid (conc. 37%) 2.5 2.5 2.5 2.5 2.5

Sodium hydroxide 0.4 0.4 0.4 0.4 0.4

Total 100 100 100 100 100

Tests and evidence

To demonstrate the antiperspirant efficacy or sweat inhibition, the sweat-reducing effect of 0.5 M silica was measured gravimetrically in the sauna test design.

Sauna Testdesgin:

The axillary sweat volume is determined gravimetrically by cotton pads are balanced in the sauna after a 15min sweat phase.

Subjects (N = 24, 12 female + 12 male) refrain from using aluminum-containing products for at least 14 days before the start of the test. For each armpit 500mg of product are applied right / left randomized and encrypted.

6h after application of the test products (10% ACH aq and 0.5M silica + 30% EtOH) cotton pads are placed in the armpits and the perspiration is stimulated in the sauna (75 ° C / 30% relative humidity) for a period of 15min.

The relative axillary sweat volume is normalized to the baseline sweat level recorded under identical experimental conditions prior to product application (= 100%). The relative sweat reduction for the silica compared to the untreated area is 54, 1%. The efficacy is therefore at the level of 10% ACH (see table). sample baseline after application rel. Reduction significance

[g] [g] [%] P

"ACH" 0.75 ± 0.45 0.35 ± 0.24 53.3 <0.001 "Silica" 0.74 ± 0.48 0.34 ± 0.29 54, 1 <0.001

Claims

claims

1. Use of low molecular weight polysilicic acids (NPK) in combination with one or more stabilizers in cosmetic and / or dermatological preparations for reducing or preventing perspiration, wherein the pH of the preparation is not less than 3.5.

2. Use according to claim 1, characterized in that the preparation is thickened with a thickener and having at least one perfume.

3. Use according to at least one of claims 1 or 2, characterized in that the stabilizer (s) are selected from the group hexenol ice 3 (CAS 928-96-1), terpineol (CAS 8000-41 -7), Linalool (CAS 78-70-6), tetrahydrolinalool (CAS 78-69-3), triethyl citrate (CAS 77-93-0), 2-isobutyl-4-hydroxy-4-methyltetrahydropyran (CAS 63500-71-0) , Hexyl salicylate (CAS 6259-76-3), phenylethyl alcohol (CAS 60-12-8), 3-methyl-5-phenyl-1-pentanol (CAS 55066-48-3), 2,6-dimethyl-7 octo-2-ol (CAS 18479-58-8), benzyl salicylate (CAS 1 18-58-1), geraniol (CAS 106-24-1), citronellol (CAS 106-22-9) and ethyllinalool (CAS 10339-55-6), in particular from the group linalool (CAS 78-70-6), benzyl salicylate (CAS 1 18-58-1), geraniol (CAS 106-24-1) and citronellol (CAS 106-22- 9th

4. Use according to at least one of claims 1 or 2, characterized in that the stabilizer (s) are selected from the group of alcohols and diols, in particular from the group: ethanol, 2-propanol, PEG 8, triethylene glycol,

Methylphenylbutanol, decanediol, polyglyceryl-2-caprate, oxalic acid.

5. Use according to at least one of claims 1 or 2, characterized in that the stabilizer (s) are selected from the group of substances having at least three hydroxyl groups, in particular from the group: sucrose (mannose, mannitol), glycerol, pentaerythritol , Threitol, erythritol, hyaluronic acid.

6. Use according to at least one of the preceding claims 2 to 5, characterized in that the thickener is selected from the group tamarind flour,

Konjakmannan, guar gum, hydroxypropyl guar, locust bean gum, gum arabic,

Xanthan gum, sodium alginate, cellulose derivatives, preferably methylcellulose,

Hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose,

Hydroxypropylmethylcellulose, carboxymethylcellulose or a mixture of polyethylene glycol and polyethylene glycol stearate or distearate.

7. Use according to at least one of the preceding claims 1 to 6, characterized in that the cosmetic and / or dermatological preparation less than 0, 1 Wt .-% of aluminum compounds, in particular less than 0.05 mol / l of aluminum ions, particularly preferably free of aluminum chlorohydrate.

8. Use according to at least one of the preceding claims 1 to 7, characterized in that the pH value of the cosmetic and / or dermatological preparation is greater than 4, in particular 5.

9. Use according to at least one of the preceding claims 1 to 8, characterized in that the cosmetic and / or dermatological preparation contains at least one physiologically acceptable and / or cosmetic oil and at least one physiologically acceptable and / or cosmetic emulsifier.

10. Use according to at least one of the preceding claims 1 to 9, characterized in that the cosmetic and / or dermatological preparation is applied topically as an aerosol or by means of a movement body.

1 1. Use according to at least one of the preceding claims 1 to 10, characterized in that the cosmetic and / or dermatological preparation is applied topically by rubbing or Versteichen.