AU2019259322A1 - Anti-perspirant 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 containing saccharides, polyols, carboxylic acids, polyphosphates, polyamino acids and/or from astringent substances exhibits a synergistic anti-perspirant action.

Description

Description

Antiperspirant preparation comprising alkaline earth metal salts

The invention relates to a combination of one or more alkaline earth metal salts and one or more substances which have a synergistic sweat-inhibiting effect with the alkaline earth metal salts.

Sweat is a watery secretion exuded from human skin via what are referred to as sweat glands. There are three types of sweat glands in the skin, namely apocrine, eccrine and apoeccrine sweat glands (Int J Cosmet Sci. 2007 Jun; 29(3):169-79).

In humans, the eccrine sweat glands are distributed over virtually all of the body and can produce considerable amounts of a clear, odorless secretion consisting of over 99% water. By contrast, the apocrine sweat glands are found only in the areas of the body that have hair, namely the armpit and genital regions and the nipples. The apocrine sweat glands produce small amounts of a milky secretion that contains proteins and lipids and is chemically neutral.

Sweating, also referred to as perspiration, is an effective mechanism for releasing excess heat and thus regulating body temperature. This function is fulfilled in particular by the high-volume, watery secretion from the eccrine glands, which can produce up to 2-4 liters per hour or 10 14 liters per day in adults.

Sweat, in particular the secretion from the apocrine sweat glands, is also said to have a signaling effect via the sense of smell. In humans, apocrine sweat plays a role in particular in connection with emotional or stress-related sweating.

Cosmetic antiperspirants or deodorants are used to eliminate body odor or to reduce the development thereof. Body odor arises when the odorless, fresh sweat is broken down by microorganisms such as staphylococci and corynebacteria.

Conventional cosmetic deodorants are based on various active principles.

In common usage, there is not always a clear distinction between the terms "deodorant" and "antiperspirant." Instead, especially also in German-speaking countries, all products for use in the armpit region are referred to as "deodorants" or "deos." This is the case regardless of whether there is also an antiperspirant effect.

Antiperspirants (AP) are sweat-inhibiting or sweat-preventing agents which-by contrast with deodorants, which generally prevent sweat which has already formed from being broken down microbially-are intended to prevent sweat from being exuded at all.

In addition to the actual sweat-inhibiting active ingredients (AP active ingredients), AP preparations can also contain substances that inhibit the microbial breakdown of sweat, such as triclosan. Triclosan acts against gram-positive and gram-negative germs as well as against fungi and yeasts, which results in a deodorizing, but not antiperspirant effect, since no influence on sweat secretion can be derived from the influence on the bacterial skin flora.

By contrast with antiperspirants, pure deodorants do not actively influence sweat secretion, but rather only control or influence body or armpit odor (odor-improving agents). Common mechanisms of action for this purpose are the following antibacterial effects, as demonstrated, for example, by non-colloidal silver: odor neutralization (masking), influence on bacterial metabolisms, pure perfuming and the use of precursors of certain perfume components which are converted to fragrant substances by enzymatic reactions.

The effect of antiperspirants based on Al salts against thermal sweating under normal physiological conditions has been very well researched.

It is assumed that sweat reduction in aluminum-containing antiperspirant active ingredients is achieved, inter alia, by "clogging of the sweat gland." They work by clogging sweat gland ducts by precipitating in place together with the skin's own proteins, and thus result in what are referred to as plugs.

The question still remains as to whether this clogging is caused 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 formation of an ACH/AZG gel (Reller HH and Luedders WL, in: Advances in Modern Toxicology, Dermatoxicology and Pharmocology, F.N. Marzulli and H.I. Maibach, Eds. Hemisphere Publishing Company, Washington and London (1977) vol. 4: 1 5), which is formed by neutralization in the sweat gland duct.

The known clogging thus achieved is, however, only effective for a short period of time. Heavy sweating or armpit cleansing as part of a normal body cleansing routine removes the clogging and thus also the antiperspirant effect. The consequent need to apply antiperspirant (AP) products at least once a day, however, may lead to skin irritation, especially after shaving or in or on previously damaged areas of the skin.

WO 2007071474 Al also describes that the axillary administration of aluminum-containing antiperspirants, preferably ACH, in deodorant/AP 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, increasingly cornified corneocytes are formed, which are released into the duct as part of natural desquamation, thus clogging the duct from the inside and preventing the flow of sweat. This additional clogging mechanism is resistant to increased sweating and/or cleansing and thus constitutes an additional long-term antiperspirant (AP) effect.

The literature reports that calcium and magnesium salts are not effective antiperspirant active ingredients (Reller, LOdders, Pharmacologic and Toxicologic Effects of topically applied agents on the eccrine sweat glands, Vol 4, p 18, 1975).

WO 2013013999 A2 describes, however, the antiperspirant effectiveness (sweat reduction) of alkaline earth metal salts. Said document mentions compounds of polyvalent cations, such as beryllium, magnesium, calcium, strontium, barium, titanium, manganese, zinc, hafnium and aluminum, with anions from the group of halides and carboxylic acids, specifically only the salts acetate, propionate, pyrrolidone carboxylate, sorbate, gluconate, ascorbate, pantothenate, citrate, lactate, aspartate, glutamate, bicarbonate or nitrate, as having an AP effect.

It is desirable to provide new preparations having an antiperspirant effect that do not have the disadvantages of the known preparations having an AP effect. In particular, it is desirable to provide alternative AP preparations that do not comprise aluminum salts.

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

Furthermore, the consumer expects a sweat-inhibiting effect that lasts for a longer period of time, ideally at least one working day.

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

It is not certain whether or not substances having an astringent effect also have antiperspirant effectiveness.

Due to their chemical structure, tannins, for example, can form stable, network-like connections with protein. This then has a contracting (astringent) effect on the skin.

Conversely, astringent starting materials do not necessarily have sweat-reducing properties. For example, tannins are described as astringents. In studies, however, tannins could not be classified as sweat-inhibiting.

Furthermore, "astringent" does not necessarily mean sweat-reducing. For example, tannins are known as astringents, which in turn do not have any sweat-inhibiting properties (S. Jellinek, Kosmetologie, 2nd edition, 1969, page 339).

Likewise, in the discussion of the AP mechanism of action of aluminum chlorohydrate, the hypothesis is put forward that aluminum salts precipitate skin proteins at the outlets of the sweat ducts and thereby block the ducts. This hypothesis is contradicted, however, by the observation by BRUN and Manuila that other protein-precipitating substances such as tannins or sulfosalicylic acid do not have, inter alia, a sweat-inhibiting effect.

It is also known that witch hazel has an astringent effect and is even listed as an OTC active ingredient for pain treatment in the USA due to its astringent effect ("Skin Protectant Drug Products for Over-The-Counter Human Use; Astringent Drug Products; Final Monograph"). However, witch hazel is not known for its AP effect. In addition, antiperspirant products are also classified as OTC active ingredients in the USA, but witch hazel is not mentioned in the FDA monograph for antiperspirants (Antiperspirant Drug Products For Over-the-Counter Human Use; Final Monograph).

DE 10260954 Al describes the use of arylsulfatase inhibitors 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 body odor caused by hydrolytic decomposition of steroid esters.

The invention relates to a cosmetic or dermatological preparation comprising one or more alkaline earth metal salts and one or more substances which have a synergistic sweat-reducing effect 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 substances having an astringent effect.

Preferred preparations according to the invention have an antiperspirant effect without the presence of further sweat-inhibiting substances, in particular aluminum salts.

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

The preparations according to the invention are used primarily to reduce sweat in the armpit. In addition, the formulations can also be used to reduce the sweat flow on other areas of the body where consumers sweat undesirably. These can include, but without being limited thereto, the feet, forehead, palms of the hands or back. Since aluminum is advantageously not present, the preparations according to the invention can also be used without issue on these partially sensitive areas of the skin.

The formulations are applied in a form which is acceptable to the consumer, which can advantageously be, for example, pump sprays, sprays containing a propellant, ball applicators, sticks, tubes, soft-touch applicators or capsules.

In-depth tests show that the combinations according to the invention have a synergistic sweat-reducing AP effect as a result of their AP effectiveness being strengthened not only additively, but surprisingly also synergistically, by a wide range of interactions, e.g. precipitation, gel formation, complex formation, ductal changes, superficial changes (film formation) and biological effects.

As a result of the preparation according to the invention being applied to the skin, various combination products are formed, characterized for example by the formation of precipitates, the formation of complexes, etc., which result in narrowing or clogging of the sweat gland outlets or at least reduce the flow of sweat and thus contribute to the inhibition of sweat formation.

The substances which have, according to the invention, a sweat-inhibiting effect in combination with the alkaline earth metal salts can be selected from the group of saccharides, polyols, carboxylic acids, polyphosphates, polyamino acids and/or substances having an astringent effect.

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

Agar: A galactose polymer having few sulfate groups is dominant in the gelling agent originating from red algae. Agar is used as a consistency and binding agent.

Alginic acid (algin) is obtained from brown algae. The polysaccharide consists of changing ratios of the sugar acids (uronic acids) mannuronic acid and guluronic acid and is distinguished by molecular weights of up to approx. 200,000 daltons. Alginic acid is used as a consistency agent, forms a moisturizing surface film on the skin and can bind heavy metal ions involved in oxidative processes and formation of radicals.

Carrageen (carrageenan): These polysaccharides of varying composition are produced, inter alia, from red algae. An important component is galactose, which is partially esterified with sulfuric acid and can therefore form sodium, potassium and calcium salts. The salts are used as gelling agents in toothpastes, for example. The carrageenans also include the structurally similar furcellaran (from the red alga Furcellaria fastigiata), the use of which is similar.

Carrageenan is a particularly preferred combination partner of the alkaline earth metal salts, in particular magnesium and calcium chlorides.

Chitin is made up of a continuous acetyl-D-glucosamine chain. Chitosan is produced by deacetylation, which chitosan forms water-soluble salts with acids, which salts can be used to condition hair (shampoos, hair gel) and can be used in toothpastes and mouthwashes as bacteria-inhibiting components and in care products as cationic film-forming agents.

CM-Glucan: Biopolymers of glucose are generally referred to as glucans. Alpha-glucans include, for example, starch and glycogen, and beta-glucans include cellulose. CM-Glucan has skin-protecting and skin-firming properties. It is well suited to sensitive skin as it provides some protection against UVA radiation. Fields of application include care after peeling, laser treatments and shaving, and use as an additive to body lotions.

CMC is the abbreviation of carboxymethyl cellulose. Similarly to CM-Glucan, CMC is produced from cellulose by chemical modification. It forms water-soluble sodium salts that have thickening properties and are used in cleaning and washing agents as effective anti-redeposition agents.

Dextrins are produced from starches under the influence of heat and acids. In contrast to the starting material, the resulting fragments are water-soluble and have chains of different lengths depending on the production process. Cyclodextrins, which are produced from starch by enzymatic degradation, are of particular interest for cosmetics. Cyclodextrins have a cylindrical cavity structure and can encapsulate organic compounds, the water solubility of which being thereby increased. They adsorb odors, but can also store and slowly release fragrances. Owing to these properties, cyclodextrins are also used as active ingredient carriers.

Cyclodextrins are particularly preferred combination partners of the alkaline earth metal salts, in particular magnesium and calcium chlorides.

Glycogen is a highly branched polysaccharide having a molar mass of 1-10 megadaltons, which, in addition to having a low protein content, consists only of glucose and forms the body's own energy reserve. Partial structures correspond to the branched amylopectin.

Guar gum produced from the guar bean (Cyamopsis tetragonoloba) is a component of surfactant-containing preparations, in particular shampoos. It creates an antistatic effect and makes hair more manageable. The main component of guar gum is the polysaccharide guaran, in which mannose and galactose are present in a ratio of 2:1. The composition of carob gum (Ceratonia siliqua) is similar.

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

Hydroxypropyl starch phosphate (HSP) (E 1442) is produced by esterifying hydroxypropyl starch with phosphoric acid. Both substances are used as thickeners and emulsion stabilizers in food and cosmetics.

Hyaluronic acid is a polysaccharide produced naturally in the body that consists alternately of D-glucuronic acid and N-acetyl-D-glucosamine units. Today, it is produced biotechnologically and binds an enormous amount of water. Since hyaluronic acid also adheres very well to the keratin of the skin, in contrast to many other polysaccharides, a very flexible film is formed on the surface of the skin, which film has plumping and smoothing effects. Low-molecular-weight hyaluronic acid fragments are also released as signal substances for inflammation.

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

Hydroxyethyl cellulose (HEC) is produced by chemically derivatizing cellulose with ethylene oxide (EO). Together with hydroxypropyl cellulose (HPC) and hydroxypropyl methylcellulose (HPMC, hypromellose), hydroxyethyl cellulose is a thickener for aqueous formulations that is widely used in cosmetics.

Methyl cellulose (MC) is produced by the etherification of free hydroxyl groups in cellulose. This makes the cellulose water-dispersible and able to form gels, and the lipophilicity increases with the methyl groups. This also gives MC emulsifying properties.

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

Pectin consists of galacturonic acid chains. It is found in fruits such as apples. Its composition varies depending on the type of fruit. Pectins are gelling agents; they increase the viscosity of gels and creams.

Tragacanth (E 413): This gum-like sap from the tragacanth plant consists of the polysaccharides tragacanthin and bassorin. While tragacanthin, like pectin, forms a galacturonic acid main chain with branches consisting of the monosugars xylose, fucose and galactose, bassorin is an elongate molecule consisting of arabinose, galactose, rhamnose and galacturonic acid methyl ester.

Xanthan gum is a biotechnologically produced polysaccharide that consists of a main chain of glucose units, which usually has a side chain of mannose, glucuronic acid and ketalized pyruvic acid at every second glucose molecule. Acetic acid can also be bonded in the manner of an ester. Xanthan gum has a thickening effect and increases the lubricity of gels. Similarly to hyaluronic acid, xanthan has a gentle skin-smoothing effect combined with a moisturizing effect.

Sugar surfactants: These include synthetic alkyl polyglycosides (APGs), the chains of which consist of glucose molecules that are etherified at the ends with fatty alcohols. APGs are distinguished by a pleasant feeling on the skin, in particular in shampoos, and can be used in microemulsions. Coco-glucoside (INCI) is, for example, a sugar having C8-16 alkyl groups.

Fucoidan is a polysaccharide found in brown algae, and consists mainly of sulfated L-fucose in a 1,2-alpha glycoside bond. Smaller amounts of the monomers xylose, galactose and uronic acid may also be present.

Gellan gum is a polysaccharide produced by fermentation. It is a linear molecule that consists of a basic unit of rhamnose, two glucoses and glucuronic acid, and is esterified to varying degrees by acetic acid or glyceric acid. The glucuronic acid is present as a salt. Gellan gum is often used in food chemistry and is known as E 418.

Tamarindus indica seed polysaccharide is commercially available as Xilogel@.

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

Saccharides preferred according to the invention are sulfated polysaccharides such as carrageenan, algae extracts such as Luminact Brite, cyclic oligosaccharides, in particular cyclodextrins, polysaccharides such as Xilogel, a tamarind extract, carob 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.

Astringents are another preferred group of sweat-inhibiting combination partners.

In cosmetics, the term "astringent" relates primarily to the term "contraction." As a result of using astringent agents, the surface of the skin thickens and the pores shrink, i.e. they contract to some extent.

From a chemical point of view, tannins are polyhydroxyphenols. They are soluble in water, ethanol and acetone and contain sufficient ortho-positioned phenolic hydroxy groups for forming cross links between macromolecules such as proteins, cellulose and pectin. Cross links of this kind can inhibit the activity of plant enzymes and organelles and ensure durability and protection against microorganisms in leather production (tanning).

Vegetable tannins vary significantly in terms of chemical structure and biological activity. Tannins which have strong absorption properties are generally found in vacuoles, separate from the protoplasm of the plants. The physiological activity results from the selective binding of the tannins to proteins, in particular to large and proline-rich molecules having an open conformation.

Tannins are divided into two groups based on their chemical properties:

1. hydrolyzable tannins (gallotannins) and 2. condensed tannins (catechin tanning agents), also known as condensed proanthocyanidins.

The first type can be hydrolyzed to glucose, other polyhydric alcohols, gallic acid or ellagic acid. Corilagin is an example of a hydrolyzable tannin. Condensed tannin consists of flavonoid phenols polymerized with one another, such as catechins, epicatechin, anthocyanins, etc. They are correspondingly polymers of which the monomer units consist of phenolic flavans, mostly catechin (flavan-3-ol).

Tannic acid is a specific form of tannin, namely a type of polyphenol. Its weak acidity (pKa of approx. 10) is due to the numerous phenol groups in the structure. The chemical formula for commercial tannic acid is often given as C76H52046, which corresponds to decagalloyl glucose; however, in reality, it is a mixture of polygalloyl glucoses or polygalloyl quinic acid esters, with the number of galloyl groups per molecule ranging from 2 to 12 using the plant source to extract the tannic acid. Commercial tannic acid is usually extracted from any of the following plant parts: tara pods (Caesalpinia spinosa), gallnuts from Rhus semialata or Quercus infectoria or Sicilian sumac leaves (Rhus coriaria).

Another sweat-inhibiting group are extracts containing catechin tanning agents such as schisandrol (Schisandra Chinensis fruit extract), Gingko or Acmella Oleracea extract. Acmella Oleracea extract comprises spilanthol as an active ingredient, which has biological relevance in the inhibition of sweat (AP effect), as it can act on the TRP channels.

Polyphenols are aromatic compounds that contain two or more hydroxy groups bonded directly to an aromatic ring and are classified as secondary plant substances. Natural polyphenols occur in plants as bioactive substances such as dyes, flavors and tannins.

Sweat inhibition tests (see the figures) surprisingly demonstrated that the combination of magnesium and calcium chloride with tannic acid and castalagin has an antiperspirant effect comparable to that of the known aluminum chlorohydrate.

Polyols and polyphosphates constitute another preferred group of sweat-inhibiting combination partners which have a surprising AP effect in combination with alkaline earth metal salts.

The invention also relates to at least two cosmetic or dermatological preparations, the substances such as saccharides, carboxylic acids or astringents being contained in one preparation and the alkaline earth metal salts being contained in another preparation.

These preparations are in turn applied and used advantageously in a two-step application process or from dual-chamber packaging.

In a first step, a preparation comprising the carrageenan, for example, can be applied to the skin.

In the second step, a preparation comprising the alkaline earth metal salt, such as MgCl2, is applied.

When the two preparations meet on the skin, the described AP effect occurs due to the narrowing of pores, for example.

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

The invention also covers the situation whereby the two preparations, one of which comprises the carrageenan and the other of which comprises the alkaline earth salt, are applied from dual-chamber packaging. This results in a mixture of the two substances, namely the carrageenan and the salt, directly before application and, as stated, can thus lead to an AP effect on the skin.

The invention also relates to a preferably non-therapeutic method for inhibiting sweat 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 first applying 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 subsequently or simultaneously applying, to the same area of the skin, a second preparation comprising the combination partners or the soluble alkaline earth metal salt not in the previous preparation.

In this case too, combination products are formed and/or deposited on the skin, which leads to sweat glands being blocked or narrowed, and thus brings about an antiperspirant effect.

The following tests demonstrate that a method characterized by the application of a preparation according to the invention to the skin results in a sweat-inhibiting effect.

The invention therefore also relates to a preferably non-therapeutic sweat-inhibiting method characterized by the application of a preparation to the skin.

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

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

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

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

Several comparative tests were carried out which confirm the AP effect.

Halides, sulfates, carbonates, hydrogen phosphates, oxides, lactates, aminoates, sorbates, carboxylates and/or nitrates are preferably selected as alkaline earth metal salts.

Magnesium, calcium and strontium halides, in particular magnesium chloride and its hydrates, in particular hydrates up to MgCl 2*6H 20, in particular MgCl 2 *6H 2 0, and/or calcium chloride and magnesium phosphate are preferably used as alkaline earth salts.

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

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

Further antiperspirant, sweat-inhibiting substances are therefore advantageously added in an amount of less than 0.1 wt.%, in particular 0 wt.%, based on the total mass of the preparation, so that said preparation can also be referred to as being free of additional AP active ingredients caused by infiltration or contamination.

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

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

According to the invention, ethanolic solutions are used as alcoholic formulations.

The preparations according to the invention advantageously comprise one or more lipids.

Preferably used lipids are selected from the group of 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, paraffinum liquidum, isododecane, isopropyl palmitate, persea gratissima, caprylyl carbonate, helianthus annuus, ethylhexyl cocoate, C12-15 alkyl benzoate, cyclomethicone and/or dimethicone, phenyl trimethicone, sunflower oil, rapeseed oil, capric/caprylic triglyceride, isopropyl myristate, isopropyl palmitate, isopropyl stearate, cetearyl ethylhexanoate, hydrogenated polydecene, glycine soy (soybean) oil, olive oil and also Guerbet alcohols such as hexyldecanol, octyldodecanol and 2-ethylhexyl alcohol, as well as Guerbet alcohol esters, and mixtures of Guerbet alcohols and Guerbet alcohol esters, such as hexyldecanol and hexyldecyl laurate.

One or more emulsifiers from the group of nonionic emulsifiers are advantageous, as emulsions, for the preparations according to the invention, such as propylene glycol isostearate

(HLB 2.5), glycol stearate (HLB 2.9), glyceryl isostearate (HLB 3.5), sorbitan sesquioleate (HLB 3.7), 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 dilaurate (HLB 6), PEG-8 dioleate (HLB 8), sorbitan laurate (HLB 8.6), PEG-40 sorbitan peroleate (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), polysorbate 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-1O/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 according to the invention can also contain anionic or cationic emulsifiers. Preferred suitable cationic emulsifiers can be selected from the group of 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 structuring agents or thickeners.

The water phase of the preparations according to the invention can advantageously contain conventional cosmetic auxiliaries, such as alcohols, in particular those having a low C number such as isopropanol, diols or polyols having a low C number, and also 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 similar products, foam stabilizers, electrolytes, etc. It is preferable according to the invention for the preparation according to the invention to be characterized in that the preparation contains propylene glycol, butylene glycol, 2-methylpropane-1,3-diol, 1,2 pentanediol, 1,2-hexanediol, 1,2-octanediol and/or 1,2-decanediol.

To stabilize the pH of the formulations, further acids and their buffer systems having suitable alkalizing agents can be used. Suitable acids can be citric acid, lactic acid, maleic acid, malonic acid, succinic acid, hydroxy succinic 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 as well as hydroxyalkylamines, aminomethyl propanol (2-amino-2-methylpropan-1-ol), ethanolamine (2-aminoethanol), triethanolamine (2,2',2"-nitrilotriethanol) and tetrahydroxypropyl ethylenediamine(1,1',1",1"' ethylenedinitrilotetrapropan-2-ol).

The following tests were carried out to demonstrate the surprising sweat-inhibiting effect of the preparations according to the invention.

The reduction in the amount of sweat on the forearm and on the back was determined gravimetrically so as to quantitatively measure the AP power. The studies were carried out following 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 Guidelines for effectiveness testing of antiperspirant drug products).

The sweat-reducing effect of various alkaline earth metal salt combinations was determined with reference to an untreated control area.

Test procedure for the forearm (AFT)

Preconditioninq/behavior during the study For at least three days prior to the start of the study, the study participants do not use any leave-on products (e.g. hand creams) or washing substances on the forearm test area, nor do they use such products during the course of the study.

During the days of the study, the test persons are also prohibited from taking part in sweaty sports, going to the sauna and solarium, sunbathing, and going to the swimming pool.

Measurement

Before applying the test substances and control substances, the forearms are washed with a surfactant-containing solution. The test areas are then marked using a template on the forearm (inside) so that they can be located again in the case of multiple applications.

The application amount of the preparation which is the subject of the test is adapted to the corresponding test area based on the standard amount of 500 mg. The preparation, active ingredient solution or formulation is evenly distributed on the test area after application. In order to simulate the generally moister environment of the armpit, semi-occlusive plasters are stuck over the test areas 5 minutes after application. After a further 2 or 4 hours, the plasters are removed.

At the corresponding test times (4h-96h), the sweat-reducing effect of the preparation, active ingredient solution or formulation is determined using the weight increase of a liquid-absorbing matrix by comparison with a matrix that was applied over an untreated control area. The weight of the dry matrix is also determined gravimetrically before it is placed in a suitable sample carrier. The subsequent absorption of water/sweat allows a direct conclusion to be drawn about the antiperspirant effectiveness of the applied sample. The antiperspirant effectiveness of the formulations/active ingredient solutions is calculated by normalization to untreated control areas.

To stimulate sweating, either the test persons are placed up to their knees in a warm water bath (45°C) or sweating is induced accordingly through physical activities (e.g. using an ergometer). A sufficient amount of sweat can be detected after a quarter to half an hour.

A total of at least 7 test persons per active ingredient solution/formulation were always tested. The test was carried out 4 hours, 24 hours and 48 hours after the last application.

Test procedure for the back (ABT)

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

Measurement First, the test areas on the back are marked and the formulations/active ingredient solutions and control substances are applied randomly and blindly based on the standard amount of 500 mg. Then, there is a drying period of 5 minutes. The areas are then covered with an occlusive, non-absorbent film, which is removed after 2 hours. The application and occlusion of the test substances is repeated several times (approx. 2-5 times) at intervals of approx. 24 hours. At the corresponding test times (4-96 h), the sweat-reducing effect of the active ingredient solution or formulation is determined using the weight increase of a water-absorbing matrix by comparison with an untreated control area. For this purpose, the weight of the dry matrix is determined gravimetrically before it is placed in a suitable sample carrier, before it is occlusively affixed to the back. The test areas on the back are first wiped with a towel, and then the weighed pads are applied. The measurement phase takes place with the test person lying down in the sauna at 80°C for approx. 15 minutes. After the sweating phase, the pads are immediately weighed again under standard conditions. The amount of sweat is determined by calculating the difference between the pad before and after the sweating phase. The calculated absorption of water/sweat by comparison with an untreated control allows a direct conclusion to be drawn about the antiperspirant effectiveness of the applied sample and thus the active ingredient solution/formulation.

A total of at least 20 test persons per active ingredient solution/formulation were tested. The test was carried out 24 hours and 48 hours after the last application.

Conventional cosmetic pads made of cotton wool or bandages such as Fixomull@ can be used as the liquid-absorbing matrix.

A total of 29 test persons were tested during the tests. There was found to be a significant sweat reduction for 25 of these test persons.

By direct comparison, the untreated area of the skin (100% sweat amount) was compared with the treated area.

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

A sweat reduction of 40% or more after 4 hours can be classified as significant.

A sweat reduction of 20% or more after 8 hours can be classified as significant.

A sweat reduction of more than 10% after 24 hours can also be considered significant.

Sweat reduction 8h 24h

Product (formulation example no.??) 20.9% 13.5%

This especially long-term AP effect was surprising and solves the problem addressed of providing a preparation having a sweat-inhibiting effect for up to 24 hours.

In further tests, the sweat inhibition of the combinations according to the invention was impressively confirmed, as shown in the following table.

Combination in solvent / sweat reduction in % by comparison with untreated Designation 4h 24h 48h 20% MgCl2*6H20 in water A 20 10 10 15% CaC12 in ethanol B 20 10 10

% carrageenan in ethanol C 10 A+C 58 B+C 70

% 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 xyloglucan 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 gum in water 1 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% synthetic tanning agent in water M 0 A+M 46

2% mandelic acid in water N 0 A+N 50

2% succinic acid in water 0 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

Individual substances produce a sweat reduction in the range of 20% after 4 hours, but this value cannot be considered sufficient (significant) for use as a cosmetic product.

Surprisingly, however, the sweat-reducing effect increased when the combinations according to the invention were used. There was a significant sweat reduction even after 24 hours and 48 hours.

In the figures, the regions above 20% and above 40% sweat reduction that can be considered significant are shown by dashed lines.

Figures 1 and 2 show the sweat reduction of the individual substances, all of which substances produce a sweat reduction below 20% or 40%.

Figures 3 and 4 show the significantly increased and synergistic sweat reduction of the combinations that act as examples of the combinations according to the invention.

Substances preferred according to the invention which can preferably be selected in combination with alkaline earth metal salts are carrageenan, cyclodextrins, hyaluronic acid, tamarindus indica seed polysaccharide, Luminact Brite, Maritech Bright, Xilogel, gellan gum, carob gum, phytic acid, glycosaminoglycan, fucoidan, tannic acid, castalagin, extracts containing catechin tanning agents, succinic acid, salicylic acid, mandelic acid, citric acid, poly L-lysine hydrochloride and/or polyglyceryl-2 caprate.

In order to enable deodorizing effects at the same time as an antiperspirant effect, one or more deodorizing active ingredients are advantageously added to the preparations according to the invention.

These deodorizing active ingredients can preferably be selected from cationic polymers, in particular polyquaternium-16, polyquaternium-7, polyquaternium-6, polyquaternium-11 and polyquaternium 37, polyaminopropyl biguanide and epsilon-polylysine.

Octenidine hydrochloride, alexidine dihydrochloride, benzyl alcohol, benzalkonium chloride, cetyltrimethylammonium chloride, silver citrate, triclosan, ethylhexylglycerin, triethyl citrate, 2 butyloctanoic acid, methyl phenyl butanol, phenoxyethanol, zinc ricinoleate, and other active ingredients which reduce the number of bacteria on the skin can also be advantageously used as deodorizing active ingredients.

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 contained in preparations according to the invention in a proportion of from 0.1 to 10 wt.%, in particular in a proportion of from 0.15 to 5 wt.%, based on the total mass of the preparation.

Polyquaternium-16 polymers (3-methyl--vinylimidazolium chloride-1-vinyl-2-pyrrolidinone chloride) 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 substances having a deodorizing effect can be contained.

The cosmetic or dermatological preparations according to the invention can also contain cosmetic auxiliaries and active ingredients such as those conventionally used in preparations of this kind, e.g. active ingredients, preservatives, preservation aids, bactericides, lipids, substances for preventing foaming, dyes and color pigments, thickeners, hydrating and/or moisturizing substances or other conventional components of a cosmetic or dermatological formulation such as polyols, polymers, foam stabilizers, organic solvents or silicone derivatives, provided that the addition of these substances does not impair or exclude the required properties with regard to stability, pH and AP effect.

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

Claims (15)

Claims

1. Cosmetic or dermatological antiperspirant preparation 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 substances having an astringent effect.

2. Preparation according to claim 1, characterized in that magnesium, calcium and/or strontium salts are selected as the alkaline earth metal salts.

3. Preparation according to either of the preceding claims, characterized in that halides, sulfates, carbonates, hydrogen phosphates, oxides, lactates, aminoates, sorbates, carboxylates, phosphates and/or nitrates are selected as the alkaline earth metal salts.

4. Preparation or preparations according to any of the preceding claims, characterized in that calcium chloride and/or magnesium chloride and/or hydrates of magnesium chloride, in particular MgCl 2 *6H 2 0, are selected as the alkaline earth metal salts.

5. Preparation according to any of the preceding claims, characterized in that the proportion of one or more alkaline earth metal salts is selected from the range of 2 to 20 wt.%, in particular from the range of 7 to 10 wt.%, based on the total mass of the preparation.

6. Preparation according to any of the preceding claims, characterized in that carrageenan, cyclodextrins, hyaluronic acid, tamarindus indica seed polysaccharide, Luminact Brite, Maritech Bright, Xilogel, gellan gum, carob gum, phytic acid, glycosaminoglycan, fucoidan, tannic acid, castalagin, extracts containing catechin tanning agents, succinic acid, salicylic acid, mandelic acid, citric acid, poly-L-lysine hydrochloride, polyglyceryl-2 caprate are selected as the substances used in combination with one or more alkaline earth metal salts.

7. Preparation according to any of the preceding claims, characterized in that the proportion of further antiperspirant substances in the preparation is less than 0.1 wt.%, in particular 0 wt.%, based on the total mass of the preparation.

8. Preparation according to any of the preceding claims, characterized in that it is in the form of a microemulsion, macroemulsion, aqueous-alcoholic solution or alcoholic solution.

9. Preparation according to any of the preceding claims, characterized in that one or more deodorizing active ingredients are contained.

10. Preparation according to claim 9, characterized in that cationic polymers, in particular polyquaternium-16, polyquaternium-7, polyquaternium-6, polyquaternium-11, polyquaternium 37, polyaminopropyl biguanide and/or epsilon-polylysine, are selected as the deodorizing active ingredients.

11. Use of a combination formed 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 substances having an astringent effect as a sweat-inhibiting active ingredient combination in a cosmetic or dermatological preparation.

12. Use according to claim 11, characterized in that the substances are selected from the group of carrageenan, cyclodextrins, hyaluronic acid, tamarindus indica seed polysaccharide, Luminact Brite, Maritech Bright, Xilogel, gellan gum, carob gum, phytic acid, glycosaminoglycan, fucoidan, tannic acid, castalagin, extracts containing catechin tanning agents, succinic acid, salicylic acid, mandelic acid, citric acid, poly-L-lysine hydrochloride and polyglyceryl-2 caprate.

13. Use according to either claim 11 or claim 12, characterized in that magnesium, calcium and/or strontium salts are selected as the alkaline earth metal salts.

14. Use according to any of claims 11 to 13, characterized in that the proportion of further antiperspirant substances in the preparation is less than 0.1 wt.%, in particular 0 wt.%, based on the total mass of the preparation.

15. Non-therapeutic, sweat-inhibiting method, characterized by a preparation according to any of claims 1 to 10 being applied to the skin.