DE102018206621A1 - An antiperspirant active preparation comprising alkaline earth metal salts - Google Patents

Abstract

The combination of one or more alkaline earth metal salts and one or more substances selected from the group of saccharides, polyols, carboxylic acids, polyphosphates, polyamino acids and / or astringent substances, show a synergistic antiperspirant effect.

Description

The invention is a combination of one or more alkaline earth metal salts and one or more substances that exert a synergistic antiperspirant effect with the alkaline earth metal salts.

Sweat is an aqueous secretion secreted by the skin of the human through the so-called sweat glands. There are three types of sweat glands in the skin, namely apocrine, eccrine and apoekkrine sweat glands (Int J Cosmet Sci. 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, apocrine sweat plays a role, especially in connection with emotional or stress-related sweating.

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.

The usual cosmetic deodorants are based on different active principles.

In common usage, there is not always a clear distinction between the terms "deodorant" and "antiperspirant". Rather, especially for German-speaking countries, products for use in the armpit area are referred to as deodorants or "deodorants". This is irrelevant to the question of whether an antiperspirant effect is present.

Antiperspirants (AT) are antiperspirants which, 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 addition to the actual antiperspirant active ingredients (AT-agents), AT preparations may additionally contain substances which inhibit the microbial degradation of the perspiration, such as e.g. Triclosan. Triclosan has an effect against gram-positive and gram-negative bacteria as well as against fungi and yeasts, which results in a deodorizing, but no antiperspirant effect, as no influence on the sweat secretion can be deduced from the influence on the bacterial skin flora.

In contrast to the antiperspirants pure deodorants cause no active influence on the sweat secretion, but only the control or influence of the body or underarm odor (odor control agent). Common mechanisms of action for this are antibacterial effects, such as e.g. Non-colloidal silver also shows odor neutralization (masking), influencing of bacterial metabolisms, pure perfuming as well as the use of precursors of certain perfume components, which are converted into fragrant substances by enzymatic reactions.

The effect of antiperspirants based on AI salts against thermal sweating under normal physiological conditions has been well studied.

It is believed that the sweat reduction of aluminum-containing antiperspirant actives i.a. achieved by a "blockage of the sweat gland". They work by blocking sweat gland excretions by precipitating them together with the skin's own proteins, leading to so-called plugs.

Whether this obstruction is caused by denaturation of the 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 formation of an ACH / AZG gel ( Reller HH and Luedders WL, in: Advances in Modern Toxicology, Dermatoxicology and Pharmacology, FN Marzulli and HI Maibach, Eds. Hemisphere Publishing Company, Washington and London (1977) Vol. 4: 1-5), formed by neutralization in the sweat gland duct is still open.

The thus obtained and known constipation is effective only in the short term. Heavy sweating or armpit cleaning as part of the normal body cleansing routine relieve the constipation and thus 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 the WO 2007071474 A1 It is also described that the axillary administration of aluminum-containing antiperspirants, preferably ACH, in deo / AT formulations by adding small amounts of organic solvents results in a greatly increased keratinization rate of the cells of the sweat gland duct. As a result, more horny corneocytes are released, which are released into the duct as part of the natural desquamation, clogging the duct from the inside and preventing the flow of sweat. This additional clogging mechanism is insensitive to increased sweating and / or cleaning, thus providing an additional long-term antiperspirant (AT) effect.

It is reported in the literature that calcium and magnesium salts are not effective antiperspirant agents (Reiler, Lüdders, Pharmacologic and Toxicological Effects of Topically Applied Agents on the eccrine sweat glands, Vol 4, p 18, 1975).

In the WO 2013013999 A2 However, the antiperspirant efficacy (sweat reduction) of alkaline earth metal salts is described. Compounds of polyvalent cations, such as beryllium, magnesium, calcium, strontium, barium, titanium, manganese, zinc, hafnium and aluminum, with anions from the group of the halides and carboxylic acids are listed as being AT-active and only the salts acetate, propionate , Pyrrolidonecarboxylate, sorbate, gluconate, ascorbate, pantothenate, citrate, lactate, aspartate, glutamate, bicarbonate or nitrate.

It is desirable to provide novel antiperspirant preparations which do not have the disadvantages of the known AT-active preparations. In particular, it is desirable to provide alternative AT preparations that do not include aluminum salts.

In some studies of the prior art, the cosmetically usable alkali and alkaline earth metal salts mentioned there have a sweat-reducing effect. The investigations under laboratory conditions do not always reflect the everyday use of cosmetic antiperspirants.

In addition, the consumer expects an antiperspirant, which lasts for a longer period, ideally at least one working day long.

It is therefore also desirable to provide a cosmetic formulation which, in addition to effective odor reduction, reduces the amount of sweat in the armpit for at least 24 hours and is free from aluminum salts.

It is uncertain whether or not astringent substances also have antiperspirant activity.

Due to their chemical structure, for example, tannins with protein can form stable, reticular compounds. On the skin, this then acts contracting (astringent).

On the other hand, astringent raw materials do not necessarily show any sweat-reducing properties. For example, tannins are described as astringents. However, these could not be classified as antiperspirant in studies.

Furthermore, "astringent" does not necessarily mean reducing sweat. For example, tannins are known as astringents, which in turn have no antiperspirant properties (S. Jellinek, Kosmetologie, 2nd edition, 1969 p 339).

Similarly, in the discussion of the AT mechanism of action of aluminum chlorohydrates, it is hypothesized that aluminum salts precipitate skin proteins at the exits of the sweat ducts and block the channels in this way. Against this hypothesis, however, speaks the observation of BRUN and Manuila that other protein-precipitating substances such as tannins or sulfosalicylic have, inter alia, no antiperspirant effect.

It is also known that witch hazel has an astringent effect and is even listed as an OTC active substance in the US for the treatment of pain due to its astringent action ("Skin Protectant Drug Products for Over-The-Counter Human Use; Astringent Drug Products; Final Monograph"). Hamamelis is not known for its AT effect. In addition, antiperspirant products are also OTC in the United States. However, Hamamelis is not mentioned in the FDA monograph on antiperspirants (Antiperspirant Drug Products For Over-the-Counter Human Use; Final Monograph).

In the DE 10260954 A1 is the use of arylsulfatase inhibiting substance selected from plant extracts, flavonoids, isoflavonoids, polyphenols and 6,7-disubstituted 2,2-dialkylchromans or chromenes in a cosmetic deodorant or antiperspirant composition for reducing the hydrolytic decomposition of steroid esters described body odor.

The invention is a cosmetic or dermatological preparation comprising one or more alkaline earth metal salts and one or more substances which exhibit a synergistic sweat reduction with the alkaline earth metal salts. In particular, the substances are selected from the group of saccharides, polyols, carboxylic acids, polyphosphates, polyamino acids and / or astringent substances.

Preferred preparations according to the invention have an antiperspirant activity without further antiperspirant substances, in particular aluminum salts, being present.

The use of the antiperspirant preparations according to the invention and as antiperspirants is also part of the present invention.

The preparations according to the invention are used for reducing sweat primarily in the armpit. In addition, the formulations can also be used to reduce the sweat flow on other body areas where consumers sweat undesirable. This may be, but is not limited to, the feet, the forehead, the palms or the back. Because of the advantageous freedom from aluminum, the preparations according to the invention can also be used without problem on these partially sensitive skin areas.

The formulations are applied in a form that is acceptable to the consumer, which can be advantageous, for example, pump sprays, sprays with aerosols, ball applicators, pens, tubes, soft-touch applicators, capsules.

In-depth investigations show that the combinations according to the invention exert a synergistic sweat-reducing AT-effects by z. As precipitation, gelation, complex formation, ductal changes, superficial changes (film formation), biological effects in the AT activity not simply additive but surprisingly synergistically reinforce.

The application of the composition according to the invention to the skin results in the formation of various combination products, characterized for example by precipitate formation, complex formation, etc., which lead to constriction or blockage of the sweat gland exits or at least reduce the sweat flow and thus contribute to inhibiting sweat formation.

The substances which act according to the invention in combination with the alkaline earth metal salts antiperspirant, are to be selected from the group of saccharides, polyols, carboxylic acids, polyphosphates, polyamino acids and / or astringent substances.

Preferred polysaccharides are in particular to be selected from the groups listed below:

Agar: The gelling agent derived from red algae is dominated by a galactose polymer with few sulfate groups. Agar is used as a consistency and binder.

Alginic acid (alginate) is derived from brown algae. The polysaccharide consists of varying ratios of the sugar acids (uronic acids) mannuronic acid and guluronic acid and is characterized by molecular weights of up to about 200,000 daltons. Alginic acid serves as a consistency agent, forms a moisture-binding surface film on the skin and can bind heavy metal ions that are involved in oxidative processes and radical formation.

Carrageenan (carrageenan): These polysaccharides of different composition are produced, among others, from red algae. An important building block is galactose, which is partially esterified with sulfuric acid and can therefore form sodium, potassium and calcium salts. The salts are z. B. used as a gelling agent in toothpastes. The carrageenans also include the structure-like furcelleran (from the red alga Furcellaria fastigiata), whose use is analogous.

Carrageenan is a particularly preferred combination partner with the alkaline earth metal salts, especially the magnesium and calcium chlorides.

Chitin is composed of a continuous acetyl-D-glucosamine chain. Deacetylation produces chitosan, which forms water-soluble salts with acids, which can be used to condition hair (shampoos, hair gels) and in toothpaste and mouthwashes as antibacterial components and as cationic film-forming agents in care preparations.

CM-glucan: Glucans are generally called biopolymers of glucose. The alpha-glucans include, for. As starch and glycogen, to the beta-glucans, the cellulose. CM-Glucan has skin-protecting and firming properties. It is well suited for sensitive skin as it provides some protection against UVA radiation. Fields of application are the care after exfoliation, laser treatments and shaving as well as in addition to body lotions.

CMC is the abbreviation for carboxymethylcellulose. CMC is prepared analogously to the CM glucan by chemical modification of cellulose. It forms water-soluble sodium salts, which have thickening properties and are used in detergents and detergents as an effective soil carrier.

Dextrins are made from starches under heat and acidity. The resulting fragments are in contrast to the starting material water-soluble and have depending on the production of different lengths chains. For cosmetics, especially cyclodextrins are of interest, which are formed by enzymatic degradation of starch. Cyclodextrins have a cylinder-like cavity structure and may include organic compounds whose water solubility is thereby increased. They adsorb odors, but on the other hand can also store fragrances and release them slowly. Because of these properties, they are also used as a drug carrier.

Cyclodextrins are particularly preferred combination partners with the alkaline earth metal salts, especially the magnesium and calcium chlorides.

Glycogen is a highly branched polysaccharide with a molecular mass of 1-10 megadaltons, which consists of only a small proportion of protein only from glucose and forms the body's energy reserve. Substructures correspond to the branched amylopectin.

Guar gum from guar bean (Cyamopsis tetragonoloba) is a constituent of surfactant-containing preparations, especially shampoos. It creates an antistatic effect and a good grip of the hair. The main constituent of guar gum is the polysaccharide guaran, in which mannose and galactose are present in a ratio of 2: 1. Similar composition is the locust bean gum (Ceratonia siliqua).

Gum arabic from the Arabian gum tree (Accacia senegal) consists of complex, branched polysaccharide chains containing various monosaccharides such as galactose and arabinose as well as glucuronic acid resulting from glucose. The polysaccharide comes from the juice of various African acacia species and is used in the form of its alkali and alkaline earth salts as a thickener.

Hydroxypropyl Starch Phosphate (HSP) (E 1442) is prepared by esterification of hydroxypropyl starch with phosphoric acid. Both substances are present as thickeners and emulsion stabilizers in foods and cosmetics

Hyaluronic acid is an endogenous polysaccharide consisting of alternating D-glucuronic acid and N-acetyl-D-glucosamine units. Today it is produced biotechnologically and binds a lot of water. In addition, because it adheres very well to the keratin of the skin, in contrast to many other polysaccharides, a very flexible film is formed on the skin surface, which has a cushioning and wrinkle-smoothing effect. Low molecular weight hyaluronic acid fragments are also released as signaling agents in inflammation.

Hyaluronic acid or its salts are particularly preferred combination partners with the alkaline earth metal salts, in particular the magnesium and calcium chlorides.

Hydroxyethylcellulose (HEC) is made by chemical derivatization of cellulose with ethylene oxide (EO). Together with hydroxypropylcellulose (HPC), hydroxypropylmethylcellulose (HPMC, hypromellose), it is a thickener of water-rich formulations which is frequently encountered in cosmetics.

Methylcellulose (MC) is formed by etherification of free hydroxyl groups of the cellulose. As a result, on the one hand the cellulose becomes water-dispersible and can form gels, on the other hand lipophilicity increases with the methyl groups. This gives MC emulsifying properties.

Mucopolysaccharides (glycosaminoglycans) contain amino sugar units, for example N-acetyl-D-glucosamine, which alternate with various monosaccharides or their relatives. They are important components of the connective tissue, as they are able to bind water so tightly that the tissue withstands external pressure. Hyaluronic acid, heparin and chondroitin belong to this group of substances. They are characterized by diverse biological functions.

Pectin consists of galacturonic acid chains. It comes in fruits such. For example, apples. Its composition varies depending on the crop. Pectins are gelling agents, they increase the viscosity in gels and creams.

Tragant (E 413): This gummy plant juice from the Tragantpflanze consists of the polysaccharides tragacanthine and bassorin. Whereas tragacanthin, like pectin, forms a galacturonic acid backbone consisting of the mono sugars xylose, fucose and galactose, bassorin is an elongated molecule of arabinose, galactose, rhamnose and galacturonic acid methyl ester.

Xanthan gum is a biotechnologically produced polysaccharide consisting of a main chain of glucose units, which usually carries on every second glucose molecule a side chain of mannose, glucuronic acid and ketalized pyruvic acid. Acetic acid may also be bound ester-like. Xanthan Gum has a thickening effect and increases the lubricity of gels. Similar to hyaluronic acid, xanthan gives a pleasant skin smoothing effect - combined with a moisture binding effect.

Sugar surfactants: These include synthetic alkylpolyglycosides (APG), whose chains consist of glucose molecules that are etherified with fatty alcohols at the ends. APGs have a good skin feel, especially in shampoos, and can be used in microemulsions. Coco glucoside (INCI) is z. B. a sugar with C _8-16 alkyl groups.

Fucoidan is a polysaccharide found in brown algae, consisting mainly of sulfated L-fucose in 1,2alpha glycoside compound. In addition, even smaller amounts of the monomers xylose, galactose and uronic acid may be present.

Gellan gum is a polysaccharide produced by fermentation, it is a linear molecule consisting of a basic unit of rhamnose, two glucoses and glucuronic acid, and is esterified to varying degrees by acetic acid or glyceric acid. The glucouronic acid is present as a salt. Gellan gum is widely used in food chemistry and is known as E418.

Tamarindus Indica Seed Polysaccharide is available on the market as Xilogel®.

Tamarindus indica seed polysaccharide is a particularly preferred combination partner with the alkaline earth metal salts, especially the magnesium and calcium chlorides.

Preferred saccharides according to the invention are sulfated polysaccharides such as carragenan, algae extracts such as Luminact brite, cyclic oligosaccharides, in particular cyclodextrins, polysaccharides such as Xilogel, a tamaride extract, locust bean gum (galactomannans) and / or phytic acid (hexaphosphoric acid ester).

Very particularly preferred polysaccharides and preferred oligosaccharides or derivatives thereof are carrageenans, dextrins, glycosaminoglycan and fucoidan.

Another preferred group of antiperspirant combination partners are astringents.

In cosmetics, the term astringent refers above all to the term "contraction". Through the use of astringents, the skin surface thickens and the pores are reduced in size, they contract a little.

Tannins are chemically polyhydroxyphenols. They are soluble in water, ethanol and acetone and contain sufficient ortho-phenolic hydroxyl groups to form cross-links between macromolecules such as proteins, cellulose and pectin. Such crosslinks can inhibit the activity of plant enzymes and organelles and provide durability and protection against microorganisms (tanning) in leather manufacture.

The vegetable tannins vary significantly in their chemical structure and biological activity. Tannins with strong absorption properties are generally found in the vacuoles, separated from the protoplasm of the plants. The physiological activity results from the selective binding ability of tannins to proteins, especially to large and proline-rich open-conformation molecules.

1. 1. hydrolysierbare Tannine (Gallotannine) und
2. 2. kondensierte Tannine (Catechin-Gerbstoffe); auch bekannt als kondensierte Proanthocyanidine

Tannins are divided into two groups because of their chemical properties

1. 1. hydrolyzable tannins (gallotannins) and
2. 2. condensed tannins (catechin tannins); also known as condensed proanthocyanidins

The former can be hydrolyzed to glucose, other polyhydric alcohols, gallic acid or ellagic acid. An example of a hydrolyzable tannin is the corilagin. Condensed tannin consists of co-polymerized flavonoid phenols such as catechins, epicatechin, anthocyanins, etc. They are corresponding polymers whose monomeric units consist of phenolic flavanes, mostly catechin (flavan-3-ol).

Tannic acid is a specific form of tannin, a type of polyphenol. Its weak acid (pKa around 10) is due to the numerous phenolic groups in the structure. The chemical formula for commercial tannic acid is often given as C76H52O46, which agrees with decagalloylglucose, but in fact it is a mixture of polygalloylglucoses or polygalloylquinic esters with the number of galloyl residues per molecule in the range of 2 to 12 the vegetable source used to produce the To extract tannic acid. Commercial tannic acid is usually extracted from one of the following parts of the plant: tara pods (Caesalpinia spinosa), gall-nuts from Rhus semialata or Quercus infectoria or Sicilian Sumac leaves (Rhus coriaria).

Another antiperspirant group is formed by extracts containing catechols, such as schisandrol (Schisandra chinensis fruit extract), gingko or acmella oleracea extract.

The latter includes spilanthol as an active ingredient, which shows a biological relevance in the sweat inhibition (AT effect), since it can act on the TRP channels.

Polyphenols are aromatic compounds which contain two or more hydroxy groups directly attached to an aromatic ring and which are considered to be secondary phytochemicals. Natural polyphenols are found in plants as bioactive substances such as colors, flavors and tannins.

In antiperspirant studies (see figures), surprisingly, the combination of magnesium and calcium chloride with tannic acid and castalagin showed an antiperspirant effect comparable to the known aluminum chlorohydrate.

Polyols and polyphosphates form another preferred group of antiperspirant combination partners which, in combination with alkaline earth metal salts, exhibit a surprising AT effect.

According to the invention, it is also necessary to provide at least two cosmetic or dermatological preparations, wherein in one preparation the substances, such as saccharides, carboxylic acids or astringents, and in another preparation, the alkaline earth metal salts are contained.

The application and use of these preparations is then advantageously in a 2-step application or from a 2-chamber packaging.

Here, in a first step, a preparation may be applied to the skin, which comprises, for example, the carragenan.

In the second step, a preparation is applied, which comprises the alkaline earth metal salt, such as MgCl 2.

When the two preparations on the skin come together, the described AT effect occurs due to, for example, a pore narrowing.

The application steps described above can also be carried out in reverse order or multiple times.

It is likewise according to the invention if the two preparations in which one comprises the carragenan and the other the alkaline earth metal salt are applied from a 2-chamber packaging agent. This results in a mixture of the two substances, carrageenan and salt, directly before application and can, as stated, lead to an AT effect on the skin.

Therefore, according to the invention, a preferably non-therapeutic method for sweat inhibition is also characterized by the application of a preparation according to the invention to the skin.

As stated above, a method according to the invention also comprises the sequence of application first of a preparation comprising one or more water-soluble alkaline earth metal salts or one or more of the combination partners of the water-soluble alkaline earth metal salts and then or simultaneously applying a second preparation to the same site of the skin then comprising each of the previous preparation not present combination partner or the soluble alkaline earth metal salt.

Again, the formation and / or deposition of combination products on the skin, which leads to a blockage or constriction of sweat glands and thus causes an antiperspirant effect.

The following investigations show that a process characterized by the application of a preparation according to the invention to the skin has an antiperspirant effect.

Likewise, therefore, a preferred non-therapeutic antiperspirant process according to the invention, which is characterized by the application of a preparation to the skin.

Preferred methods are non-therapeutic methods, cosmetic methods that lead to cosmetic sweat reduction or inhibition.

In particular, the methods are preferred in which are selected as alkaline earth metal salts of magnesium or calcium chlorides.

The preparations according to the invention can be prepared, for example, as follows.

The water phase and fat phase are heated and combined with stirring. Subsequently, the emulsion is cooled down with stirring and the active ingredient phase comprising the soluble alkaline earth metal salts, such as magnesium chloride, added to the emulsion at 30 ° C. Finally, the approach is homogenized.

Several comparative experiments were carried out to confirm the AT effect.

The alkaline earth metal salts used are preferably the halides, sulfates, carbonates, hydrogen phosphates, oxides, lactates, aminoates, sorbates, carboxylates and / or nitrates.

The alkaline earth metal salts used are preferably magnesium, calcium and strontium halides, in particular magnesium chloride and its hydrates, in particular hydrates to MgCl ₂ .6H ₂ O, in particular MgCl ₂ .6H ₂ O, and / or calcium chloride, and also magnesium phosphate.

The proportion of one or more alkaline earth salts is preferably selected in the range from 2 to 20% by weight, in particular in the range from 7 to 10% by weight, based on the total mass of the preparation.

In addition to the alkaline earth salts and the combination partners, no further antiperspirant active substances, in particular no aluminum salts such as aluminum chlorohydrates, are advantageously added to the preparations according to the invention.

The addition of further antiperspirant, antiperspirant substances is therefore advantageously less than 0.1 wt.%, In particular at 0 wt.%, Based on the total mass of the preparation to refer by introduction or impurities and these as free of additional AT-active ingredients ,

Preparations according to the invention are preferably O / W emulsions, W / O emulsions, aqueous-alcoholic preparations, alcoholic (ethanolic) solutions, PIT emulsions or hydrodispersions.

The results shown were particularly advantageous for both micro- and macroemulsions as well as aqueous-alcoholic and purely alcoholic formulations.

As alcoholic formulations according to the invention ethanolic solutions are used.

Advantageously, the preparations according to the invention comprise one or more lipids.

Preferably used lipids are selected from the group of the Capric / Caprylic triglyceride, cocoglyceride, PPG-14 butyl ether, PPG-9 butyl ether, PPG-12 butyl ether, PPG-14 butyl ether, PPG-15 butyl ether, PPG-16 butyl ether, PPG-17 butyl ether , PPG-18 butyl ether, PPG-2 butyl ether, PPG-20 butyl ether, PPG-22 butyl ether, PPG-24 butyl ether, PPG-26 butyl ether, PPG-30 butyl ether, PPG-33 butyl ether, PPG-40 butyl ether, PPG-52 butyl ether PPG-53 butyl ether, PPG-15 stearyl ether, coco-caprylate / caprate, dicaprylyl ether, octyldodecanol, paraffin liquidum, isododecane, isopropyl palmitate, persea gratissima, caprylyl carbonate, helianthus annuus, ethylhexyl cocoate, C12-15 alkyl benzoate, cyclomethicone and / or dimethicones, phenyltrimethicone, sunflower oil, rapeseed oil, capric / caprylic triglyceride, isopropyl myristates, isopropyl palmitate, isopropyl stearates, cetearyl ethylhexanoates, hydrogenated polydecene, glycine soya (soybean) oil, olive oil, and guerbet alcohols such as hexyldecano l, octyldodecanol and 2-ethylhexyl alcohol, and also Guerbet alcohol esters, as well as mixtures of Guerbet alcohols and Guerbetalkoholestem such. Hexyldecanol and hexyldecyl laurate.

As emulsions, one or more emulsifiers from the group of nonionic emulsifiers, such as, for example, propylene glycol isostearate (HLB 2.5), glycol stearate (HLB 2.9), glyceryl isostearate (HLB 3.5), sorbitan sesquioleate (HLB 3.7), are advantageous for the preparations according to the invention. , Glyceryl Stearate (HLB 3.8), Lecithin (HLB 4), Sorbitan Oleate (HLB 4.3), Sorbitan Monostearate NF (HLB 4.7), Sorbitan Stearate (HLB 4.7), Sorbitan Isostearate (HLB 4.7), Steareth-2 (HLB 4.9) , Oleth-2 (HLB 4.9), Glyceryl Laurate (HLB 5.2), Ceteth-2 (HLB 5.3), PEG-30 Dipolyhydroxystearate (HLB 5.5), Glyceryl Stearate SE (HLB 5.8), Sorbitan Stearate (and) Sucrose Cocoate (HLB 6), PEG-4 dilaurates (HLB 6), PEG-8 dioleates (HLB 8), sorbitan laurate (HLB 8.6), PEG-40 sorbitan peroleates (HLB 9), laureth-4 (HLB 9.7), PEG-7 glyceryl Cocoate (HLB 10), PEG-20 Almond Glycerides (HLB 10), PEG-25 Hydrogenated Castor Oil (HLB 10.8), Stearamide MEA (HLB 11), Glyceryl Stearate (and) PEG-100 Stearate (HLB 11), Polys orbate 85 (HLB 11), PEG-7 Olivate (HLB 11), Cetearyl Glucoside (HLB 11), PEG-8 Oleate (HLB 11.6), Polyglyceryl-3 Methyglucose Distearate (HLB 12), PG-10 Stearate (HLB 12) , Oleth-10 (HLB 12.4), Oleth-10 / Polyoxyl 10 Oleyl Ether NF (HLB 12.4), Ceteth-10 (HLB 12.9), PEG-8 Laurate (HLB 13), Ceteareth-12 (HLB 13.5), Cocamide MEA (HLB 13.5), Polysorbate 60 NF (HLB 14.9), Polysorbate 60 (HLB 14.9), PEG-40 Hydrogenated Castor Oil (HLB 15), Polysorbate 80 (HLB 15), Isosteareth-20 (HLB 15), PEG- 60 Almond Glycerides (HLB 15), Polysorbate 80 NF (HLB 15), PEG-150 Laurate, PEG-20 Methyl Glucose Sesquistearate (HLB 15), Ceteareth-20 (HLB 15.2), Oleth-20 (HLB 15.3), Steareth- 20 (HLB 15.3), steareth-21 (HLB 15.5), ceteth-20 (HLB 15.7), isoceteth-20 (HLB 15.7), PEG-30 glyceryl laurate (HLB 16), polysorbate 20 (HLB 16.7), polysorbate 20 NF (HLB 16.7), Laureth-23 (HLB 16.9), PEG-100 Stearate (HLB 18.8), Steareth-100 (HLB 18.8), PEG-80 Sorbitan Laurate (HLB 19.1).
The emulsions of the invention may also contain anionic or cationic emulsifiers. Preferred suitable cationic emulsifiers are to be selected from the group Cetrimonium Chloride, Palmitamidopropyltrimonium Chloride, Quaternium-87, Behentrimonium Chloride, Distearoylethyl Dimonium Chloride, Distearyldimonium Chloride, Stearamidopropyl Dimethylamine and / or Behentrimonium Methosulfate.

To stabilize the emulsions, it may be beneficial to add texturizers or thickeners.

The aqueous phase of the preparations according to the invention may advantageously comprise customary cosmetic auxiliaries, for example alcohols, in particular those of low C number such as isopropanol, diols or polyols of low C number and their ethers, preferably propylene glycol, 2-methylpropane-1,3-diol, pentane 1,2-diol, hexane-1,2-diol, octane-1,2-diol, decane-1,2-diol, 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, foam stabilizers, electrolytes, etc .. According to the invention it is preferable if the preparation according to the invention is characterized in that the preparation propylene glycol, butylene glycol, 2-methylpropane-1,3-diol, 1,2- Pentanediol, 1,2-hexanediol, 1,2-octanediol and / or 1,2-decanediol contains.

To stabilize the pH of the formulations, other acids and their buffer systems can be used with suitable alkalizing agents. Suitable acids may be citric acid, lactic acid, maleic acid, malonic acid, succinic acid, malic acid (malic acid), fumaric acid, salicylic acid, etidronic acid, phosphoric acid, hydrochloric acid and sulfuric acid.
Suitable alkalizing agents for creating a buffer system can be, for example, sodium hydroxide, potassium hydroxide, ammonia, mono-, di- and trialkylamines and the hydroxyalkylamines, aminomethylpropanol (2-amino-2-methylpropan-1-ol), ethanolamine (2-aminoethanol), triethanolamine ( 2,2 ', 2 "-nitrilotriethanol) and tetrahydroxypropylethylenediamine (1,1', 1", 1 "'- ethylenedinitrilotetrapropan-2-ol).

To demonstrate the surprising antiperspirant effect of the preparations according to the invention, the following investigations were carried out.

For the quantitative measurement of the AT-performance, the reduction of the sweat volume on the forearm and on the back was determined gravimetrically. The studies were conducted in accordance with the FDA criteria (Antiperspirants Drug Products for Over-the-Counter Human Use, Final Monograph (2003) Federal Register Vol 68, No.110, Rules and Regulations, §350.60 Guidlines for efficacy testing of antiperspirant drug products).

The sweat-reducing effect of various alkaline earth metal salt combinations was determined against an untreated control balance.

Test procedure on the forearm (AUT)

Preconditioning / behavior during the study

Study participants did not use any leave-on products (such as hand creams) or cleansers on the underarm area for at least three days prior to the start of the study, as well as during the course of the study.

Likewise during the study days the subjects are forbidden sweaty sports, sauna sessions and solarium, sun baths and swimming pool visits.

Measurement

Before application of the test substances and controls, the forearms are washed with a surfactant-containing solution. Subsequently, the test areas are recorded with the help of a template on the forearm (inside) for the recovery in the multiple application.

The application amount of preparation to be tested is adapted to the corresponding test area based on the usual amount of 500 mg. The preparation, active ingredient solution or formulation is distributed evenly on the test area after application. In order to simulate the generally moist environment of the armpit, semi-occlusive patches are pasted over the test areas 5 min after application. After another 2 or 4 hours, the patches are removed again.

At the corresponding test times (4h-96h), the sweat-reducing effect of the preparation, active substance solution or formulation on the weight gain of a liquid-absorbing matrix compared to a matrix applied over an untreated control area. Likewise, the weight of the dry matrix is determined gravimetrically before introduction into a suitable sample carrier. The subsequent uptake of water / sweat allows a direct inference to the antiperspirant efficacy of the applied sample. The antiperspirant efficacy of the formulations / drug solutions is calculated by normalization to untreated control sites.

To stimulate sweating, subjects are either placed up to their knees in a warm water bath (45 ° C), or sweating induced by physical activity (eg ergometer riding). After a quarter to half an hour, a sufficient amount of sweat can be detected.

Overall, at least 7 subjects per drug solution / formulation were always evaluated. The test was performed 4h, 24h and 48h after the last application.

Test procedure on the back (ATR)

The preconditioning / behavior during the study corresponds to that of the AUT test.

Measurement

First, the test areas are marked on the back and the formulations / drug solutions and controls based on the current amount of 500mg randomized and blinded applied. This is followed by a 5 minute drying time. Subsequently, the areas are covered with an occlusive, non-absorbent foil, which is removed after 2 hours. The application and Oclussion of the test substances is repeated several times (about 2-5 times) at intervals of about 24 h. At the appropriate test time (4-96 h), the sweat-reducing effect of the drug solution or formulation is determined by the weight gain of a water-absorbing matrix compared to an untreated control area. For this purpose, the weight of the dry matrix is determined gravimetrically before being placed in a suitable sample carrier before it is glued occlusive to the back. The test areas on the back are first wiped with a cloth, then applied the weighed pads. The measuring phase takes place horizontally in the sauna at 80 ° C for approx. 15 min. After the sweat phase, the pads are immediately weighed under standard conditions. The amount of sweat is determined by calculating the difference of the pad before and after the sweat phase. The calculated uptake of water / sweat compared to an untreated control allows a direct inference to the antiperspirant efficacy of the applied sample and thus of the drug solution / formulation.

Overall, at least 20 subjects per drug solution / formulation were evaluated. The test was performed both 24h and 48h after the last application.

As the liquid-absorbent matrix, pads, conventional cotton cosmetic pads or dressing materials such as Fixomull® can be used.

In the investigations, a total of 29 subjects were evaluated. 25 of these showed a significant reduction in sweat

In direct comparison, the untreated skin area (100% sweat volume) was compared with the treated area.

The test was carried out both 4h, after 24h and after 48h after the last application.

A sweat reduction after 4h of 40% or more can be considered significant.

A sweat reduction after 8h of 20% or more can be considered significant.

Sweat reduction after more than 10% after 24 hours is also considered significant. sweat reduction 8h 24 hours Product (recipe example no. ??) 20.9% 13.5%

This above all long-term AT effect was surprising and fulfills the stated task of providing a preparation with a sweat inhibition up to 24 hours.

In further investigation, the sweat inhibition of the combinations according to the invention was impressively confirmed, as listed in the table below. Combination in LM / Welding Reduction in% compared to untreated description 4h 24 hours 48h 20% MgCl2 * 6H20 in water A 20 10 10 15% CaCl 2 in ethanol B 20 10 10 5% carragenan in ethanol C 10 A + C 58 B + C 70 5% alpha cyclodextrin in water D 10 0 A + D 51 33 10% Maritech Bright in water e 20 0 A + E 76 27 3% Tamarindus Indica Xiloglucan in water F 20 A + F 66 2% gellan gum in water G 0 0 A + G 56 25 1% hyaluronic acid in water H 0 A + H 58 3% carob seed flour in water I 20 A + I 64 10% LaraCare J 0 A + J 48 1% tannic acid in ethanol K 19 0 A + K 58 20 B + K 60 1% castalagin in water L 20 A + L 70 1% synth. Tannin in water M 0 A + M 46 2% almond acid in water N 0 A + N 50 2% succinic acid in water O 10 A + O 57 1.8% salicylic acid in ethanol P 20 0 A + P 52 30 6% citric acid in water Q 20 A + Q 48 1% poly-L-lysine hydrochloride in water R 10 A + R 51 1% polyglyceryl-2-caprate in water S 0 A + S 56

Although individual substances show sweat reduction in the region of 20% after 4 h, this value is not considered to be sufficient (significant) for use as a cosmetic product.

Surprisingly, however, the sweat-reducing effect increased when the combinations according to the invention were used. Significant sweat reduction was also seen here after 24 and 48 h.

In the figures, the areas considered to be significant above 20% and above 40% of sweat reduction are shown in dashed lines.

and show the sweat reduction of the individual substances, which are all below 20% and 40%, respectively.

and show the significantly increased and synergistic sweat reduction of the combinations which are exemplary of the combinations according to the invention.

Carrageenan, cyclodextrins, hyaluronic acid, Tamarindus indica seed polysaccharide, luminact brite, Maritech Bright, xilogel, gellan gum, locust bean gum, phytic acid, glycosaminoglycan, fucoidan, tannic acid, castalagin, extracts are preferred as inventively preferred in combination with alkaline earth metal salts containing catechols, succinic acid, salicylic acid, mandelic acid, citric acid, poly-L-lysine hydrochloride and / or polyglyceryl-2-caprate.

In order to simultaneously allow deodorizing effects in addition to an antiperspirant effect, one or more deodorizing agents are advantageously added to the preparations according to the invention.

These deodorizing agents may preferably be selected from cationic polymers, in particular Polyquaternium-16, Polyquaternium-7, Polyquaternium-6, Polyquaternium-11 and Polyquaternium 37, polyaminopropyl biguanide and epsilon-polylysine.

Also useful as deodorizing agents are octenidine hydrochloride, alexidine dihydrochloride, benzyl alcohol, benzalkonium chloride, cetyltrimethylammonium chloride, silver citrate, triclosan, ethylhexylglycerol, triethyl citrate, 2-butyloctanoic acid, methylphenylbutanol, phenoxyethanol, zinc ricinoleate, and other drugs that reduce the number of bacteria on the skin.

The preparations according to the invention therefore preferably also comprise one or more polyquaternium polymers.

According to the invention, polyquaternium polymers are selected from the group of polyquaternium-16 polymers and polyquaternium-6 polymers. These are present in preparations according to the invention in a proportion of 0.1 to 10% by weight, in particular in a proportion of 0.15 to 5% by weight, based on the total mass of the preparation.

Polyquaternium-16 polymers (3-methyl-1-vinylimidazolium chloride-1-vinyl-2-pyrrolidinone chlorides) are preferably selected. According to the invention, the polyquaternium polymers used, and in particular PQ-16 polymers, have an additional antimicrobial activity.

In advantageous embodiments of the invention, in addition to the polyquaternium polymers used, one or more further deodorant substances may be present.

The cosmetic or dermatological preparations according to the invention may further contain cosmetic adjuvants and active ingredients such as are commonly used in such preparations, for. As agents, preservatives, preservatives, bactericides, lipids, substances for preventing foaming, dyes and color pigments, thickeners, moisturizing and / or moisturizing substances or other conventional ingredients of a cosmetic or dermatological formulation such as polyols, polymers, foam stabilizers, organic solvents or silicone derivatives if the additive does not impair or preclude the required properties in terms of stability, pH values and AT effect.

The following examples are intended to illustrate the present invention without limiting it. Unless indicated otherwise, all amounts, proportions and percentages are based on the weight and the total amount or on the total weight of the preparation.

QUOTES INCLUDE IN THE DESCRIPTION

This list of the documents listed by the applicant has been generated automatically and is included solely for the better information of the reader. The list is not part of the German patent or utility model application. The DPMA assumes no liability for any errors or omissions.

Cited patent literature

• WO 2007071474 A1 [0016]
• WO 2013013999 A2 [0018]
• DE 10260954 A1 [0029]

Claims (15)

Cosmetic or dermatological antiperspirant active composition comprising a combination of one or more alkaline earth metal salts and one or more substances selected from the group of saccharides, polyols, carboxylic acids, polyphosphates, polyamino acids and / or astringent substances. Preparation after Claim 1 characterized in that are selected as the alkaline earth metal salts of magnesium, calcium and / or strontium salts. Preparation according to one of the preceding claims, characterized in that are selected as alkaline earth metal salts halides, sulfates, carbonates, hydrogen phosphates, oxides, lactates, aminoates, sorbates, carboxylates, phosphates and / or nitrates. Preparation or preparations according to one of the preceding claims, characterized in that selected as alkaline earth metal salts calcium chloride and / or magnesium chloride and / or hydrates of Magnesiumschlorid, in particular MgCl ₂ * 6H ₂ O. Preparation according to one of the preceding claims, characterized in that the proportion of one or more alkaline earth metal salts in the range of 2 to 20 wt.%, In particular in the range of 7 to 10 wt.% Is selected, based on the total mass of the preparation. Preparation according to one of the preceding claims, characterized in that as substances, which are used in combination with one or more alkaline earth metal salts, are selected from carrageenan, cyclodextrins, hyaluronic acid, Tamarindus indica seed polysaccharide, Luminact brite, Maritech Bright, Xilogel, gellan gum, locust bean gum , Phytic acid, glycosaminoglycan, fucoidan, tannic acid, castalagin, extracts containing catechols, succinic acid, salicylic acid, mandelic acid, citric acid, poly-L-lysine hydrochloride, polyglyceryl-2-caprate. Preparation according to one of the preceding claims, characterized in that the proportion of other antiperspirant active substances in the preparation is less than 0.1 wt.%, In particular 0 wt.%, Based on the total mass of the preparation. Preparation according to one of the preceding claims, characterized in that it is in the form of a micro-, macroemulsions, aqueous-alcoholic solution or alcoholic solution. Preparation according to one of the preceding claims, characterized in that one or more deodorizing agents are contained. Preparation after Claim 9 characterized in that are selected as Deowirkstoffe cationic polymers, in particular Polyquaternium-16, Polyquaternium-7, Polyquaternium-6, Polyquaternium-11, Polyquaternium 37, Polyaminopropylbiguanid and / or epsilon-polylysine. Use of a combination formed from one or more alkaline earth metal salts and one or more substances selected from the group of saccharides, polyols, carboxylic acids, polyphosphates, polyamino acids and / or astringent substances as antiperspirant active ingredient combination in a cosmetic or dermatological preparation. Use after Claim 11 characterized in that the substances are selected from the group carrageenan, cyclodextrins, hyaluronic acid, Tamarindus indica seed polysaccharide, Luminact brite, Maritech Bright, xilogel, gellan gum, locust bean gum, phytic acid, glycosaminoglycan, fucoidan, tannic acid, castalagin, extracts containing catechols , Succinic acid, salicylic acid, mandelic acid, citric acid, poly-L-lysine hydrochloride, polyglyceryl-2-caprate. Use after Claim 11 or 12 characterized in that are selected as the alkaline earth metal salts of magnesium, calcium and / or strontium salts. Use according to one of Claims 11 to 13 characterized in that the proportion of further antiperspirant active substances in the preparation is less than 0.1% by weight, in particular 0% by weight, based on the total mass of the preparation. Non-therapeutic antiperspirant process characterized by the application of a preparation according to one of Claims 1 to 10 onto the skin.

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