PREPARATIONS CONSISTING OF PHOSPHINIC ACID OR ITS SALTS AND CARRIER SYSTEMS, AND ORAL CARE PRODUCTS CONTAINING THESE PREPARATIONS

Abstract

The invention relates to a composition comprising phosphinic acid or its salts, and a carrier system, and an oral care product, specifically a toothpaste or mouthwash, comprising such composition.

Description

[0001] Composition comprising phosphinic acid or a salt thereof and a carrier system

[0002] The present invention relates to a composition comprising phosphinic acid or a salt thereof and a carrier system, an oral care product, in particular a toothpaste or a mouthwash, comprising the composition, and their uses.

[0003] Dental care is becoming increasingly important, if only because of the increasingly carbohydrate-rich diet worldwide. In addition to aesthetic considerations, greater emphasis is being placed on preventative care, with the main focus being on reducing or even preventing plaque, tooth decay, and / or halitosis (bad breath), as well as healthy gums.

[0004] Healthy gums are characterized, among other things, by their cervical surroundings. The gums surround the neck of the tooth, sealing the point where the tooth enters the jawbone of the oral cavity. The gums thus serve, among other things, to protect and support the tooth.

[0005] The different parts of a natural tooth are the crown, neck, and root, each of which is made up of several layers. Of these layers, only the outer enamel is visible in a healthy tooth, which encloses the dentin and other layers. In order to be able to bite or grind food, for example, without damaging the teeth, the enamel is very hard. It consists of approximately 97% by weight of hydroxyapatite (HAP), which has the molecular formula Cas(PO4)3(OH). Dentin is also considered the hard substance of the tooth and is also made up of about two-thirds hydroxyapatite. In addition to hydroxyapatite, dentin also contains proteins (e.g. collagen) and water and is therefore softer than enamel.

[0006] It is documented that saliva, due to its supersaturation of Ca 2+ - and PO4 3'-ions in bioavailable form has a remineralizing effect. However, the remineralizing effect induced by saliva is not only slow but also apparently insufficient to protect individuals from caries and / or remineralize existing dental lesions without the addition of mineralization-enhancing additives.

[0007] Dental diseases such as caries can be caused by the formation of bacterial microfilms and / or bacterial inflammation. Although often preventable through preventive care, caries remains one of the most common chronic diseases in children and adults worldwide, and there is a great global need for products to prevent and treat caries-affected teeth.

[0008] Caries is considered a multifactorial disease, particularly affecting tooth enamel and dentin, involving microorganisms. In the initial stage, a precipitate, also called a pellicle, can form on the tooth surface. It consists of saliva protein, among other substances. The rougher the tooth surface, the easier it is for this precipitate to form and adhere to it. Over time, this pellicle then forms a film a few micrometers thick covering the tooth surface. Bacteria can then multiply and spread on this film. This film can be considered a biofilm.

[0009] The bacteria can produce organic acids, such as gluconic and lactic acid, from low-molecular-weight carbohydrates commonly found in today's diet. Both these organic acids produced by bacteria and acids ingested through food, such as fruit acids, can cause erosion of tooth structure.

[0010] This process dissolves, among other things, calcium phosphates from the tooth enamel. If this process is not stopped, or preferably even reversed, demineralization of the tooth enamel and possibly also of the dentin can occur over time. A defect in the tooth structure caused in this way is referred to as a carious lesion. Carious lesions in the dentin layer, for example, can be recognized by a yellow to brown discoloration of the affected area of ​​the tooth. While carious lesions in the enamel alone can often be reduced or eliminated by re-mineralization of the enamel, in the case of carious lesions that affect other layers in addition to the enamel, the damaged part of the tooth is usually removed and the resulting hole (caries lesion) is closed with a filling material.

[0011] In summary, caries formation can be promoted by the interaction of the following factors:

[0012] - special bacteria that adhere to the pellicle

[0013] - poor tooth quality or mineral quality of the tooth - plaque

[0014] - food containing low molecular weight carbohydrates

[0015] - Time.

[0016] One possible approach to caries prevention could therefore be the administration of calcium phosphate compounds, particularly hydroxyapatite, to improve tooth quality. Furthermore, there are various approaches, all aimed at preventing caries in order to avoid the aforementioned treatments. Caries prevention with fluoride-containing dental care products can be considered the current standard. J.M. ten Cate: "Contemporary perspective on the use of fluoride products in caries prevention", British Dental Journal, February 23, 2013, vol. 214, no. 4, pp. 161-167, describes in a review the use and effectiveness of fluoride-containing dental care products such as toothpaste and mouthwash.

[0017] It is particularly noted that the reduction of caries is achieved through regular use of such fluoride-containing dental care products. The model assumes that fluoride accelerates natural remineralization from saliva.

[0018] Various fluoride compounds, such as sodium fluoride, stannous fluoride, amine fluorides, and sodium monofluorophosphate, are suitable as fluoride sources in the aforementioned dental care products. J.M. ten Cate: “The Need for Antibacterial Approaches to Improve Caries Control," Adv Dent Res 21:8-12, August 2009, pp. 8-12, describes that fluoride provision alone may not be sufficient to achieve adequate caries prevention, since, as mentioned above, bacteria also play a crucial role in caries formation. For this reason, caries prophylactic compositions are being considered that contain one or more antimicrobial substances in addition to fluoride. One example is chlorhexidine (CHX), whose antimicrobial effect in the oral cavity has been investigated in many studies.

[0019] The use of fluorides in dental care products is controversial, however, due to concerns about negative side effects. One example is dental fluorosis, which occurs due to excessive fluoride intake during tooth formation. Acute toxic effects include nausea, vomiting, and diarrhea. Other examples are bone fluorosis, which is characterized by thickening of the outer bone layer and the associated loss of elasticity and resilience, and enamel fluorosis, which is recognizable by the appearance of whitish enamel spots on the tooth surface. Furthermore, it has been reported that swallowing high-dose dental care products, especially in children, can trigger acute fluoride poisoning, which can occasionally even be fatal. In a recent evaluation of in vivo human studies by the National Toxicology Program of the USDepartments of Health and Human Services have clearly established that the higher the mother's fluoride exposure during pregnancy, the lower the IQ score of her children.

[0020] Furthermore, the WHO is not yet able to establish a value for daily fluoride requirements, as fluoride is not an essential trace element. Therefore, there are no diagnostic parameters and no corresponding evidence for the existence of clinical symptoms of "fluoride deficiency."

[0021] The use of an antimicrobial substance such as chlorhexidine in dental care, especially for caries prevention, is also controversial. It has been reported that a relevant effect for caries prevention is not always reproducible and only occurs in a portion of the studied cases. Furthermore, the antimicrobial effect of chlorhexidine is not limited to the bacteria in the mouth that contribute to caries formation, but also includes beneficial bacteria. Furthermore, long-term treatment with products containing chlorhexidine leads to undesirable side effects, such as tooth discoloration and impaired taste.

[0022] Biomimetic tooth and mouthwashes with artificial enamel, which may contain the active ingredient hydroxyapatite, are also known. Hydroxyapatite-based products can reduce initial bacterial colonization on the enamel surface without possessing antimicrobial properties that can disrupt the oral cavity's ecological balance. Furthermore, these products are said to remineralize and repair microscopic defects in the enamel, as well as form a protective layer.

[0023] Biomimetic dental care products based on the use of hydroxyapatite are also known. For example, WO 2018 / 024649 A1, DE 10 2017 009 626 A1, and DE 10 2018 102 365 describe oral care compositions containing synthetic hydroxyapatite. Hydroxyapatite, as indicated above, is a bioactive and biocompatible material with a similar chemical composition to the hydroxyapatite of human tooth enamel.

[0024] However, due to the above-mentioned limitations of both the homeostatic mechanism of the body's own saliva and the fluoride-based approaches to caries prevention and remineralization, there is a need for alternative compositions and oral care products that are at least equivalent to the efficiency of fluoride supplementation in mineralization, but without the corresponding undesirable side effects.

[0025] Furthermore, there continues to be a need for compositions and oral care products for the treatment or prevention of various diseases affecting the teeth.

[0026] Furthermore, the use of the compositions and oral care products provided should not significantly disturb the ecological balance in the oral area and / or risk tooth discoloration or taste disturbance.

[0027] The object of the invention is therefore to provide a composition and in particular an oral care product, in particular a toothpaste or a mouthwash, with one or more biomimetic or bioinspired active ingredients, in particular for the prophylaxis of caries, which avoids the disadvantages of the prior art described above.

[0028] In particular, a composition or an oral care product, in particular a toothpaste or mouthwash, is to be provided that mineralizes existing, minor caries lesions and / or repairs microfine defects in the tooth enamel. Furthermore, a protective layer should be applied to the tooth and / or open dentin tubules should be able to be closed. To this end, the aforementioned effects should be achieved while avoiding the disadvantages that can accompany the use of fluoride. Furthermore, the adhesion of bacteria to the tooth enamel should be advantageously reduced without significantly disturbing the ecological balance in the oral cavity and / or risking tooth discoloration or taste disturbance. Furthermore, the composition and, in particular, the oral care product should not have any mucosal irritating effects.These objects are achieved by the composition according to the invention and in particular the oral care product according to the invention comprising phosphinic acid and / or a salt of phosphinic acid, in particular calcium hypophosphite (Ca(H2PO2)2). In addition, at least one compound selected from the group comprising remineralizing substances, antibacterial substances, moisturizing or conditioning substances, desensitizing substances, and abrasive agents may be included.

[0029] A first aspect of the invention therefore relates to a composition, in particular an oral care product comprising

[0030] (A) Phosphinic acid and / or a salt of phosphinic acid, in particular calcium hypophosphite (Ca(H2PO2)2), and

[0031] (B) a carrier system having a pH between 3.0 and 9.0.

[0032] Phosphinic acid, also known as hypophosphorous acid, is one of the acids of phosphorus and has the molecular formula H3PO2. Its salts are called phosphinates or hypophosphites. Salts of phosphinic acid are preferred according to the invention. Divalent salts of phosphinic acid are particularly preferred, with calcium hypophosphite (Ca(H2PO2)2) being particularly preferred.

[0033] The composition according to the invention preferably contains phosphinate and in particular calcium hypophosphite in an amount of 0.00001 to 40.0 percent by weight (wt%), preferably from 0.0001 to 20.0 wt%, more preferably 0.001 to 15 wt%, more preferably 0.01 to 15 wt%, particularly preferably 0.1 to 8 wt% and in particular 2.5 wt%, in each case based on the total weight of the composition.

[0034] In the composition according to the invention, calcium hypophosphite is preferably present in dissolved or predominantly dissolved form, more preferably completely dissolved. It is known that the solubility of calcium hypophosphite in water is approximately 154 g / l (Robertson, DS Magnesium or calcium hypophosphite could be a treatment for obesity in humans. Med. Hypotheses 2006, 66, 439-440). It is therefore preferred that all calcium hypophosphite in the composition according to the invention is present in dissolved form up to a concentration of 154 g / l. The composition according to the invention preferably contains dissolved calcium hypophosphite, in particular in a concentration of 0.0001 to 154 g / l, more preferably from 0.001 to 154 g / l, even more preferably 0.01 to 150 g / l, even more preferably 0.1 to 150 g / l, particularly preferably 1 to 80 g / l and in particular 25 g / l.The carrier system according to the invention contains at least one substance selected from remineralizing substances, antibacterial substances, moisturizing or conditioning substances, desensitizing substances, and abrasive agents. Furthermore, any mixtures of these substances can be included in the carrier system according to the invention.

[0035] The carrier system particularly preferably comprises at least one calcium phosphate. Generally, calcium phosphate, also known as tricalcium orthophosphate or tricalcium phosphate (Ca3(PC>4)2), refers to a calcium salt of orthophosphoric acid and belongs to the phosphates. The term tricalcium phosphate is occasionally used for the very similar compound pentacalcium hydroxytriphosphate (Cas(PO4)3-OH) (=hydroxyapatite).

[0036] It is preferred according to the invention that, in addition to calcium hypophosphite, at least one calcium phosphate compound is preferably present in particulate form and is selected from the group consisting of monocalcium phosphate monohydrate (MCPM), monocalcium phosphate anhydrate (MCPA), dicalcium phosphate dihydrate (DCPD, brushite), dicalcium phosphate anhydrate (DCPA, monetite), octacalcium phosphate (OCP), α-tricalcium phosphate (α-TCP), β-tricalcium phosphate (β-TCP), amorphous calcium phosphate (ACP; also known as CPP-ACP complex = casein phosphopeptide - amorphous calcium phosphate), amorphous calcium phosphate (ACP), calcium-deficient hydroxyapatite (CDHA), hydroxyapatite (HA or HAP), tetracalcium phosphate (TTCP) and calcium pyrophosphate, preferably from the group consisting of monocalcium phosphate monohydrate (MCPM), monocalcium phosphate anhydrate (MCPA), Dicalcium phosphate dihydrate (DCPD, brushite), dicalcium phosphate anhydrate (DCPA, monetite), octacalcium phosphate (OCP),Amorphous calcium phosphate (ACP; also known as CPP-ACP complex = casein phosphopeptide - amorphous calcium phosphate), amorphous calcium phosphate (ACP), calcium-deficient hydroxyapatite (CDHA), hydroxyapatite (HA or HAP), and tetracalcium phosphate (TTCP), and any mixtures of these compounds. Hydroxyapatite is particularly preferred. The at least one calcium phosphate compound can be present in different crystal forms, including mixtures of these crystal forms, with round crystal forms being preferred over pointed crystal forms (e.g., needle-shaped crystals). They can also have different crystal and aggregate sizes, including mixed forms, and different crystallinities.also in mixed form. Hydroxyapatite is particularly preferred according to the invention. However, depending on the use of the compositions described herein, embodiments may also be preferred according to the invention which, in addition to calcium hypophosphite, contain no further calcium phosphate compound, and in particular no hydroxyapatite.

[0037] Hydroxyapatite is also known as hydroxyapatite. Accordingly, the terms are used interchangeably herein. It is a mineral from the phosphate mineral class that crystallizes in a hexagonal crystal system. Hydroxyapatite is also a member of the apatite group and forms a continuous mixed series with chloroapatite and fluorapatite.

[0038] A Cas(PO4)3(OH) suitable for the invention is described, for example, in DE 102016 114 189.5. The Cas(PO4)3(OH) used according to the invention is preferably produced synthetically. This means that the Cas(PO4)3(OH) used according to the invention is preferably not obtained by cauterizing the organic components from animal material, such as bone.

[0039] According to the invention, a composition or an oral care product comprising calcium hypophosphite and hydroxyapatite is particularly preferred.

[0040] The calcium phosphate compounds used according to the invention can be present in pure form as well as in the form of substituted compounds and as mixtures thereof. A pure form is present according to the invention when the ions contained in the respective calcium phosphate compound are each substituted by one or more other ions to an extent of less than 1%, preferably less than 0.5%, even more preferably less than 0.1%. For example, in pure hydroxyapatite, the Ca 2+ -ions by, for example, Mg 2+ or Zn 2+ substituted to less than 1%, preferably less than 0.5%, even more preferably less than 0.1%.

[0041] Furthermore, the calcium phosphate compounds preferably do not contain any doping, such as zinc carbonate doping. However, doped calcium phosphate compounds can also be used.

[0042] The X50 value of the volume-based particle size distribution of the calcium phosphate compounds is 1.0 nm to 100.0 pm, preferably 10 nm to 10.0 pm, more preferably 50 nm to 1 pm, particularly preferably 100 nm to 5500 nm, wherein the X50 value of the volume-based particle size distribution is measured by laser diffraction. The maximum aspect ratio of the particles of the calcium phosphate compounds, determined by transmission electron microscopy (TEM) images, is preferably in the range 1-20, more preferably 2-15, and even more preferably 4-10.

[0043] For this purpose, a sample of calcium phosphate compounds is first subjected to ultrasonic irradiation in an ultrasonic homogenizer with an energy output of 96 W for 9 minutes, followed by a further 3 minutes in a sample preparation device. The subsequent particle size distribution measurement (laser diffraction) is performed in a particle size determination instrument at a temperature of 25 °C ± 0.3 °C, and the corresponding values ​​are calculated according to Mie theory. All measuring instruments used are commercially available.

[0044] In a preferred embodiment of the invention, the calcium phosphate compound is Cas(PO4)3(OH) and has a hexagonal crystal lattice in which the length of the a-axis is 0.930 to 0.950 nm, preferably 0.933 to 0.948 nm, particularly preferably 0.936 to 0.945 nm, and the length of the c-axis is 0.680 to 0.700 nm, preferably 0.682 to 0.696 nm, particularly preferably 0.685 to 0.692 nm. The lengths of the a-axis and the c-axis are determined by a Rietveld analysis of the corresponding X-ray powder diffractograms.

[0045] X-ray powder diffractograms themselves are obtained by measuring with a conventional powder diffractometer at routine settings.

[0046] In a preferred embodiment of the invention, the at least one calcium phosphate compound is present in aggregated form. Aggregation in this case refers to the aggregation of molecules or particles into a larger structure, the aggregate. This aggregation or aggregate is caused and held together by various forces and / or bonding types, such as ionic bonding, van der Waals forces, intermolecular forces, or other chemical bonding types. The degree of aggregation and also the size of the aggregate can be determined using scanning electron microscopy.

[0047] The composition or oral care product according to the invention comprises calcium phosphate compounds in an amount of 0.01 to 80 wt.%, preferably 0.1 to 20 wt.%, particularly preferably 1 to 10 wt.%, and in particular 1 to 5 wt.%, based on the total weight of the oral care product. For mouthwashes, the preferred amount of calcium phosphate compounds is 1 to 5 wt.%, and for toothpastes, 10 to 20 wt.%, each based on the total weight.

[0048] The composition according to the invention or the oral care product according to the invention can contain, in addition to calcium hypophosphite and / or hydroxyapatite, at least one further calcium compound, which is preferably selected from the group consisting of calcium carbonate, calcium chloride, calcium bromide, calcium nitrate, calcium acetate, calcium gluconate, calcium lactate, calcium tartrate and their hydrates and mixtures thereof, preferably calcium carbonate.

[0049] The carrier system according to the invention preferably has a viscosity between 0 and 150,000 mP sec (mPas).

[0050] In embodiments of the invention relating to pastes and in particular toothpastes, the viscosity is preferably in the range 0 - 150,000 mPas, more preferably between 5,000 - 120,000 mPas and particularly preferably in the range 10,000 - 90,000 mPas (in each case determined 0-4 days after production).

[0051] In embodiments according to the invention relating to solutions and in particular mouthwashes, the viscosity is preferably in the range 0 - 1,000 mPas, more preferably between 0 - 500 mPas and particularly preferably in the range 10 - 150 mPas (in each case determined 0-4 days after production).

[0052] All viscosity data are based on measurements according to DIN 53019-1:2008-09 using a Haake RheoStressl rheometer (ThermoFisher Scientific) at 20 °C and a gravity velocity of 10 / s (toothpaste) and 50 / s (mouthwash) in plate-plate geometry.

[0053] The carrier system according to the invention has a pH between 3.0 and 9.0. The pH is preferably in the range from 4.0 to 8.0, in particular between 5.0 and 7.0.

[0054] The pH can be adjusted using pH regulators. pH regulators are substances that can adjust a specific pH range, preferably a range from pH 5.5 to 8.0. Examples of pH regulators are acetic acid, acetates, lactic acid, lactates, malic acid, malates, fumaric acid, citric acid, citrates, tartaric acid, tartrates, orthophosphates, di-, tri-, and polyphosphates, hydrochloric acid, chlorides, sulfuric acid, sulfates, hydroxides, oxides, adipic acid, adipates, gluconic acid, gluconates, phosphoric acid, calcium carbonate, or a hydrate thereof. A preferred example of a pH regulator that can be added when a lower pH is desired is phosphoric acid (H3PO4).

[0055] Within the scope of the invention, it has surprisingly been shown that calcium hypophosphite effectively remineralizes tooth enamel and dentin and protects against caries. In particular, chalky teeth and / or teeth affected by fluorosis are also effectively remineralized. The remineralizing effect is surprisingly significantly higher than that of other calcium compounds. Furthermore, it was unexpectedly discovered that calcium hypophosphite has pronounced antimicrobial properties against bacteria that cause caries and periodontitis, and also effectively prevents sensitive teeth.

[0056] In combination with hydroxyapatite, a surprising synergistic effect was observed. The addition of calcium hypophosphite unexpectedly significantly increased the remineralization performance of the active ingredient hydroxyapatite.

[0057] A composition comprising calcium hypophosphite, hydroxyapatite and an additional antibacterial substance is particularly preferred.

[0058] A composition comprising calcium hypophosphite, hydroxyapatite and moisturizing or caring substances as described herein represents a preferred embodiment of the invention.

[0059] A composition comprising calcium hypophosphite, hydroxyapatite and abrasive particles as described herein represents a preferred embodiment of the invention.

[0060] During the tooth cleaning process, abrasives, usually together with the toothbrush, remove plaque and harmful bacteria from the tooth surface and can provide a whitening effect. Abrasives or abrasives are contained in toothpastes in quantities of up to 15% by weight, or more, based on the total weight of the toothpaste. Examples of abrasives are whiting, marble powder, and / or silicate compounds such as silica. Polysilicic acids (hydrated silica) and calcium carbonate are the most commonly used. The disadvantage is that, with the exception of calcium phosphate compounds (e.g., hydroxyapatite), all types of abrasives are foreign to the body and do not correspond to the natural tooth mineral (hydroxyapatite). For example, abrasives with a high relative hardness can cause irreparable damage to the tooth structure.If the abrasive body is too hard, the cleaning performance of the overall toothpaste formulation may be too low to effectively remove plaque during brushing (increased risk of caries and periodontitis).

[0061] A composition comprising calcium hypophosphite, hydroxyapatite and gingival care substances as described herein represents a preferred embodiment of the invention.

[0062] The above-mentioned active ingredients and groups of active ingredients can be combined freely and independently with calcium hypophosphite, and in particular calcium hypophosphite and hydroxyapatite.

[0063] Anionic, non-ionic, cationic, and zwitterionic surfactants can be used as surfactants. Non-ionic surfactants are often avoided due to their adverse effects on the antibacterial compound. Likewise, cationic and zwitterionic surfactants are often avoided because they can stain or darken teeth. Accordingly, anionic surfactants are preferred as the cleansing component in the composition or oral care product. Sodium lauryl sulfate and other higher alkyl sulfates containing 10 to 18 carbon atoms in the alkyl group are preferred, although other known sulfated and sulfonated surfactants can also be used partially or entirely as such.

[0064] Preferably, the composition or oral care product contains at least one surfactant selected from the group consisting of taurates, glycinates, sarcosinates and quaternary ammonium compounds, preferably sodium methyl cocoyl taurate, sodium cocoyl glycinate, sodium lauroyl sarcosinate, benzalkonium chloride,

[0065] Cetylpyridinium chloride or any mixtures thereof.

[0066] Preferably, the composition or oral care product contains less than 10 wt.% poloxamers, also called pluronic acid, a non-ionic surfactant. More preferably, the composition or oral care product is substantially free of pluronic acid. "Substantially free" within the meaning of the present application means "< (less than) 10 ppm."

[0067] Preferably, the composition or oral care product contains no more than 10.0% by weight of calcium gluconate.

[0068] In a preferred embodiment of the invention, the composition or oral care product contains peroxide, preferably in an amount of 0.00001-40 wt.%, more preferably 0.0001-6 wt.%, and particularly preferably 0.001-0.1 wt.%. In this case, the peroxide is preferably selected from the group consisting of hydrogen peroxide, carbamide peroxide, sodium percarbonate, and calcium peroxide, and any mixtures thereof; particularly preferably, the peroxide is hydrogen peroxide or carbamide peroxide.

[0069] In a preferred embodiment of the invention, the composition or oral care product contains about 0.1% by weight, particularly preferably 0.1% by weight, of hydrogen peroxide.

[0070] In another preferred embodiment of the invention, the composition or oral care product contains less than 0.1% hydrogen peroxide and is more preferably substantially free of hydrogen peroxide.

[0071] One aspect of the invention, as described, relates to an oral care product comprising the composition described herein. The oral care product is preferably a toothpaste, an oral gel, or a mouthwash. As long as the composition according to the invention is intended for oral application, the terms "composition according to the invention" and "oral care product" can be used interchangeably herein.

[0072] The composition according to the invention is preferably intended for topical application, in particular in the oral cavity.

[0073] A toothpaste, also known as tooth cream, can be used in combination with a toothbrush for the mechanical cleaning of teeth and gums and is a soft or semi-solid composition for oral application. An oral gel is used in the same way but has a gel-like composition. A mouthwash, also known as a mouth rinse, is a liquid formulation that can be used, among other things, for the prevention of caries and other diseases in the oral cavity. The oral care product according to the invention can accordingly be intended to remain on the teeth and / or to be rinsed out. The composition according to the invention can also be in the form of a tooth varnish or polishing paste.

[0074] Since sodium lauryl sulfate can also be irritating to the mucous membranes at concentrations above 1.0% by weight, the oral care product according to the invention can also be free of sodium lauryl sulfate and instead be surfactant-free or contain other surfactants that cause less mucous membrane irritation than sodium lauryl sulfate, such as taurates, preferably sodium methyl cocoyl taurate, glycinates, preferably sodium cocoyl glycinate, sarcosinates, preferably sodium lauroyl sarcosinate or quaternary ammonium compounds, preferably benzalkonium chloride or cetylpyridinium chloride. The information about the respective surfactants also includes all variants thereof (different alkyl chains, branches in the alkyl chains, counterions, etc.). Surfactants are important for a toothpaste because they help distribute the active ingredients in the oral cavity while brushing. Surfactants are also important for consumer convenience.

[0075] Furthermore, it was unexpectedly found that the oral care product according to the invention advantageously mineralizes smaller caries lesions and / or repairs microfine defects in the tooth enamel, particularly in patients with dry mouth / low saliva production. Furthermore, the composition according to the invention can be used to apply a protective layer to the tooth, and it was also found that the tooth enamel exhibits advantageous solubility and resistance to acid after application of the composition according to the invention. Furthermore, the present composition eliminates the need for antimicrobial substances (such as chlorhexidine) as excipients. This ensures excellent caries prophylaxis without, for example, disturbing / destroying the bacterial balance in the oral cavity and without risking unpleasant side effects.

[0076] Furthermore, it was unexpectedly discovered that the oral care product according to the invention prevents caries and can also remineralize lesions down to deeper layers of the tooth, particularly the enamel. Furthermore, the oral care product according to the invention can apply a protective layer to the tooth and over exposed dentin, and in particular, can close open dentin tubules. Furthermore, it was found that the tooth enamel exhibits significantly reduced or no longer detectable structural damage after application. Furthermore, the present oral care product can completely dispense with the use of fluoride. Thus, the aforementioned positive aspects can be ensured without, for example, disturbing / destroying the bacterial balance in the oral cavity and without risking undesirable side effects that can occur, for example, when using fluoride-containing oral care products (see above).The subject of the present invention is an oral care product for the mineralization and remineralization of teeth, in particular enamel and dentin, but also non-mineralized tooth components in cases of so-called mineralization defects. These include, for example, "molar incisor hypomineralization" (MIH, also called "chalky teeth"). Alternatively, chalky teeth are also referred to in the professional world as "molar hypomineralization" (MH). Accordingly, the terms can be used interchangeably herein.

[0077] The oral care product according to the invention is intended for daily use with 1-3 applications per day.

[0078] If the oral care product is in the form of an oral gel, it does not need to be spit out, but can be absorbed over a longer period of time of more than 3 minutes, preferably between 5 minutes and 12 hours, particularly preferably between 10 minutes and 1 hour. Due to the gel-like composition, the adhesion of the calcium hypophosphite directly to the tooth (enamel, dentin, cementum) is supported, so that the calcium hypophosphite is in direct contact with it over a longer period of time, thereby achieving a high remineralization rate. The oral gel according to the invention is preferably used 1-3 times daily, particularly preferably once daily. Use in the evening is then again preferred. In other embodiments, application can also be made once a week.

[0079] It is also possible for the oral care product to be substantially free, preferably free, of fluorides and / or tin salts and / or chlorhexidine and / or triclosan. "Free" in the context of the present invention means that the composition according to the invention may contain unavoidable impurities of the substance designated "free from." "Substantially free" in the context of the present application means "< (less than) 10 ppm."

[0080] The oral care product according to the invention can be used for remineralization and protection of teeth.

[0081] It has been found that the oral care product according to the invention can be used in the treatment and / or prevention of numerous dental diseases.

[0082] In a preferred embodiment of the invention, the oral care product according to the invention can be used for the treatment of (dental) diseases / conditions selected from caries, tooth erosion, tooth abrasion, attrition, bruxism, molar-incisor hypomineralization (MIH; chalky teeth), amelogenesis imperfecta, dentinogenesis imperfecta and fluorosis.

[0083] The term "caries" is familiar to experts. It is generally understood as a destructive disease of the hard dental tissue, enamel, and dentin.

[0084] Tooth erosion refers to damage to the hard tooth substance caused by acids, in other words defects in the tooth enamel and / or dentin caused by dental erosion, which, if treated too late, can lead to irreversible damage.

[0085] (Tooth) abrasion refers to the loss of tooth substance due to friction. Attrition is a subtype of abrasion, namely the loss of tooth substance due to reflexive contact of the teeth.

[0086] Bruxism is the unconscious grinding or clenching of teeth, usually at night but also during the day, which can result in the wear and tear of not only the teeth but also the periodontal ligament and chewing muscles.

[0087] Molar-incisor hypomineralization (MIH), also known as “chalky teeth,” is a disorder of the enamel, i.e. structural damage to the tooth enamel.

[0088] Amelogenesis imperfecta is considered a genetic disorder that disrupts tooth enamel formation. As a result, teeth are at increased risk of caries and are particularly sensitive to temperature.

[0089] Dentinogenesis imperfecta is an autosomal dominant inherited maldevelopment / structural disorder of the dental dentition that occurs in approximately 1 in 8,000 people and results in severe tooth abrasion.

[0090] Dental fluorosis (also known as dental fluorosis) is a non-inflammatory disease ("speckled teeth") caused by excessive fluoride intake, particularly during the ontogenetic development of the teeth. It has been found that the use according to the invention can prevent the above-mentioned dental diseases and / or at least significantly slow their progression and / or achieve complete restoration of the tooth substance, particularly the hard tooth substance. In particular, it has been found that the use according to the invention, or after its application, significantly reduces or no longer detects structural damage to the tooth enamel.

[0091] In a preferred embodiment, the oral care product according to the invention can be used for both cosmetic and medicinal purposes. This means that it can be used, for example, not only for the treatment of the aforementioned (dental) diseases, but also for cosmetic purposes such as improving the appearance of teeth.

[0092] In a preferred embodiment, the oral care product according to the invention is used in persons of all age groups, including children, in the case of children preferably in children aged 6 months to 14 years, in particular in children aged 10 months to 12 years.

[0093] In a preferred embodiment, the Cas(PO4)3(OH) contained in the oral care product according to the invention is the only apatite component of the oral care product.

[0094] In a preferred embodiment, the oral care product according to the invention comprises 0.01 to 80 wt.%, preferably 0.2 to 40 wt.%, more preferably 0.5 to 30 wt.%, in particular 1.0 to 20 wt.% calcium phosphate compounds. In a preferred embodiment of the invention, the oral care product according to the invention can comprise 1 wt.%, 2 wt.%, 3 wt.%, 4 wt.%, 5 wt.%, 6 wt.%, 7 wt.%, 8 wt.%, 9 wt.%, 10 wt.%, 11 wt.%, 12 wt.%, 13 wt.%, 14 wt.%, 15 wt.%, 20 wt.% or 25 wt.% calcium phosphate compounds.

[0095] Preferably, the composition comprises one or more pharmaceutical or cosmetic ingredients such as xylitol, antimicrobial substances, pH regulators, abrasives, flavorings and humectants, in particular xylitol, pH regulators, abrasives and flavorings.

[0096] Xylitol can minimize the number of caries bacteria and inhibit their growth. Furthermore, xylitol can stimulate saliva flow. The increased amount of saliva produces an increased amount of phosphate. This phosphate can react with the calcium (ions) of the oral care product according to the invention to form hydroxyapatite. The oral care product according to the invention can contain xylitol in an amount of 0.01 to 15 wt.%, preferably 1.0 to 10.0 wt.%, in particular about 7.0 wt.%, based on the total weight of the oral care product. In addition to xylitol, the oral care product according to the invention can contain other sugar alcohols such as sorbitol.

[0097] Antimicrobial substances are substances that can kill microorganisms, such as bacteria, or significantly reduce their proliferation. In addition to antimicrobial substances that provide non-specific defense against bacteria and fungi, there are also antimicrobial substances that, for example, only act against specific bacteria. The use of antimicrobial substances can also be used to combat bad breath, for example. Antimicrobial substances can preferably be contained in the oral care product according to the invention in an amount of 0.01 to 2.0 wt.%, more preferably 0.05 to 1.0 wt.%.

[0098] In a further preferred embodiment, the oral care product according to the invention contains a pH regulator in an amount of 0.05 to 3.0 percent by weight, more preferably 0.1 to 2.5 percent by weight, particularly preferably 0.2 to 1.5 percent by weight, in each case based on the total weight of the oral care product.

[0099] In a preferred embodiment, the oral care product according to the invention contains one or more flavoring agents that can impart the desired taste. This one or more flavoring agents can be natural, nature-identical, synthetic flavoring agents, and / or mixtures thereof.

[0100] Flavorings may be contained in the oral care product according to the invention preferably in an amount of 0 to 5% by weight, preferably 0.1 to 3% by weight, based on the total weight of the oral care product according to the invention.

[0101] Humectants are additives that prevent the inventive oral care product from drying out by binding water added during production (i.e., preventing evaporation) or by attracting atmospheric moisture during storage. Examples of humectants are glycerin, propane-1,2-diol, hexane-1,2-diol, egg yolk, aloe vera gel, honey, molasses, especially glycerin and hexane-1,2-diol. Humectants can be present in the inventive oral care product preferably in an amount of 0 to 25 wt.%, preferably 0.1 to 20 wt.%, based on the total weight of the inventive oral care product.

[0102] In a preferred embodiment, the oral care product according to the invention contains

[0103] - 0.01 to 80 wt.%, preferably 0.2 to 40 wt.%, more preferably 0.5 to 30 wt.%, in particular 1.01 to 20 wt.% calcium phosphate compounds, preferably hydroxyapatite,

[0104] - 0.00001 to 30.0 wt.%, preferably from 0.0001 to 10.0 wt.% and particularly preferably from 0.0005 to 5.0, in particular 2.5 wt.% calcium hypophosphite,

[0105] - 0.3 to 3 wt.% surfactants, preferably about 1.0 wt.% sodium cocoyl glycinate or sodium methyl cocoyl taurate,

[0106] - 0.5 to 15% by weight, preferably 1 to 10% by weight, in particular about 7.0% by weight of xylitol,

[0107] - 0 to 2.0 wt.%, preferably 0.01 to 2.0 wt.%, more preferably 0.05 to 1.0 wt.% antimicrobial substance, in particular cetylpyridinium chloride and / or zinc chloride,

[0108] - 0 to 5 wt.%, preferably 0.3 to 2.0 wt.%, pH regulator, in particular phosphoric acid,

[0109] - 0 to 5% by weight, preferably 0.1 to 3% by weight, flavoring,

[0110] - From 0 to 25% by weight, preferably 0.1 to 20% by weight, of humectant, in particular glycerin and / or hexane-1,2-diol, where the percentages in weight refer to the total weight of the oral care product. The remainder is optionally distilled water.

[0111] If the oral care product is in the form of an oral gel, it contains gelling agents, whereby the gelling agent consists of synthetic and / or natural polymer materials.

[0112] It is advantageous for the gelling agent to be selected from the group comprising cellulose and cellulose derivatives such as methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, agarose, agar, pectins, sclerotium gum, xanthan gum, guar gum, carrageenan, alginic acid, polyvinyl alcohol, polyvinylpyrrolidone, and mixtures thereof. Such an oral gel preferably contains gelling agent in an amount of 1.0 to 4.0 percent by weight, particularly preferably 1.5 to 3.0 percent by weight, and in particular approximately 2.0 percent by weight, based in each case on the total weight of the oral gel.

[0113] A further aspect of the invention relates to the use of the composition described herein for dermatological treatment. In this embodiment, the composition according to the invention particularly preferably comprises a divalent salt of phosphinic acid, in particular calcium hypophosphite (Ca(H2PO2)2), but not hydroxyapatite.

[0114] It is particularly preferred for the treatment of diseases of the skin, but also of the mucous membranes, hair and / or nails.

[0115] Topical application is preferred here. Topical application can be in the form of ointments, creams, solutions, or drops.

[0116] This is particularly true for topical treatment of skin and scalp.

[0117] Examples

[0118] The invention is explained below using examples.

[0119] Examples of the composition of oral care products according to the invention in the form of toothpastes (in wt.%):

[0120] Study 1: Remineralization of tooth enamel with toothpastes (in situ)

[0121] Analogous experimental design:

[0122] K. Najibfard, K. Ramalingam, I. Chedjieu, BT Amaechi, Remineralization of early caries by a nano-hydroxyapatite dentifrice, J. Clin. Dent. 22 (2011) 139-43. Results:

[0123] Study 2: Remineralization of tooth enamel with mouthwashes (in vitro)

[0124] Analogous experimental design:

[0125] P. Tschoppe, DL Zandim, P. Martus, AM Kielbassa, Enamel and dentine remineralization by nano-hydroxyapatite toothpastes, J. Dent. 39 (2011) 430-437.

[0126] (Modification of the literature reference: Instead of toothpastes, different mouthwashes were tested here.)

[0127] Results:

[0128] Study 3: Remineralization of chalky teeth (MIH) with toothpastes (in vitro)

[0129] Analogous experimental design:

[0130] BT Amaechi, R Farah, JA Liu, TS Phillips, Bl Perozo, Y Kataoka, F Meyer, J Enax, Remineralization of molar incisor hypomineralization (MIH) with a hydroxyapatite toothpaste: an in-situ study, BDJ Open 8 (2022) 33. Results:

[0131] Study 4: Effectiveness against sensitive teeth with toothpastes (in vivo)

[0132] Analogous experimental design:

[0133] G. Orsini, M. Procaccini, L. Manzoli, F. Giuliodori, A. Lorenzini, A. Putignano, A double-blind randomized-controlled trial comparing the desensitizing efficacy of a new dentifrice containing carbonate / hydroxyapatite nanocrystals and a sodium fluoride / potassium nitrate dentifrice, J. Clin. Periodontol. 37 (2010) 510-517.

[0134] Results:

[0135] The following items summarize the invention:

[0136] 1. Composition comprehensive

[0137] (A) phosphinic acid and / or at least one salt of phosphinic acid, and

[0138] (B) a carrier system having a pH between 3.0 and 9.0.

[0139] 2. Composition according to Item 1, wherein the carrier system (B) has a viscosity between 0 and 150,000 mP.sec.

[0140] 3. Composition according to item 1 or 2, wherein the carrier system (B) contains at least one calcium phosphate.

[0141] 4. Composition according to one of the preceding items, wherein the carrier system (B) contains hydroxyapatite.

[0142] 5. Composition according to one of the preceding items, with a pH value in the range between 4 and 7.

[0143] 6. Composition according to one of the preceding items, wherein the salt of phosphinic acid (A) is divalent.

[0144] 7. Composition according to one of the preceding items, wherein the salt of phosphinic acid (A) is the calcium salt, ie calcium hypophosphite, in particular dissolved calcium hypophosphite.

[0145] 8. Composition according to one of the preceding items, wherein the composition contains 0.00001 to 40.0 wt.%, in particular 0.001 to 20 wt.%, preferably 0.01 to 15 wt.%, particularly preferably 0.1 to 8 wt.% calcium hypophosphite.

[0146] 9. Composition according to one of the preceding items, where the

[0147] Composition designed for topical application.

[0148] 10. Composition according to one of the preceding items, wherein the

[0149] Carrier system (B) contains a gelling agent, in particular celluloses and / or xanthans or corresponding derivatives. Composition according to one of the preceding items, which is intended for rinsing after use. Composition according to one of the preceding items, which is intended to remain on the teeth after use. Composition according to one of the preceding items, which contains one or more organic acids. Composition according to one of the preceding items, which contains xylitol. Composition according to one of the preceding items, which contains at least one surfactant from the group of taurates, sarcosinates, glycinates and alkyl sulfates or mixtures thereof. Composition according to one of the preceding items, which is substantially free of fluorides. Composition according to one of the preceding items, which contains menthol and / or menthol derivatives.Composition according to one of the preceding items, which contains silica abrasive particles, calcium carbonates, and / or calcium phosphates. Composition according to one of the preceding items, which contains antibacterial substances. Composition according to one of the preceding items, which contains gum-care additives. Use of the composition according to one of the preceding items for the prevention and / or treatment of tooth and / or gum diseases. Use of the composition according to item 21 for the treatment of chalky teeth and / or fluorosis. Use of the composition according to item 21 or 22 for the prevention and / or treatment of caries. Use of the composition according to one of the preceding items for the prevention and / or treatment of sensitive teeth. Use of the composition according to one of the preceding items for whitening teeth. Use of the composition according to one of the preceding items for remineralizing teeth.Use of the composition according to any one of the preceding items for protecting teeth from erosion, particularly due to exposure to acid(s). Use of the composition according to any one of items 1 to 20 for dermatological treatment, particularly topical treatment of skin and scalp. Oral care product comprising a composition according to any one of items 1 to 20. Oral care product according to item 29, wherein the oral care product is a toothpaste, a mouthwash, an oral gel, a dental varnish, or a polishing paste.

Claims

Patent claims 1. Composition comprehensive (A) phosphinic acid and / or at least one salt of phosphinic acid, and (B) a carrier system having a pH between 3.0 and 9.

0.

2. Composition according to claim 1, wherein the carrier system (B) has a viscosity between 0 and 150,000 mP see.

3. Composition according to claim 1 or 2, wherein the carrier system (B) contains at least one calcium phosphate and / or hydroxyapatite.

4. Composition according to one of the preceding claims, wherein the pH is in the range between 4 and 7.

5. Composition according to one of the preceding claims, wherein the salt of phosphinic acid (A) is divalent and the salt of phosphinic acid (A) is preferably the calcium salt, ie calcium hypophosphite, in particular dissolved calcium hypophosphite.

6. Composition according to one of the preceding claims, wherein the composition contains 0.00001 to 40.0 wt.%, in particular 0.001 to 20 wt.%, preferably 0.01 to 15 wt.%, particularly preferably 0.1 to 8 wt.% calcium hypophosphite.

7. Composition according to one of the preceding claims, wherein the composition is designed for topical application and is preferably intended for rinsing after application or for remaining on the teeth.

8. Composition according to one of the preceding claims, wherein the carrier system (B) contains a gelling agent, in particular celluloses and / or xanthans or corresponding derivatives, and / or wherein the composition contains one or more organic acids and / or xylitol and / or at least one surfactant from the group of taurates, sarcosinates, glycinates and alkyl sulfates or mixtures thereof.

9. A composition according to any one of the preceding claims which is substantially free of fluorides.

10. Composition according to one of the preceding claims, which contains menthol and / or menthol derivatives, Contains silica abrasives, calcium carbonates and / or calcium phosphates, antibacterial substances and / or gum care additives.

11. Use of the composition according to any one of the preceding claims for the prevention and / or treatment of dental and / or gum diseases.

12. Use of the composition according to claim 11 for the treatment of chalky teeth and / or fluorosis and / or for the prevention and / or treatment of caries and / or sensitive teeth.

13. Use of the composition according to any one of the preceding claims for remineralizing and / or whitening teeth and / or protecting teeth from erosion, in particular due to exposure to acid(s).

14. Use of the composition according to any one of claims 1 to 10 for dermatological treatment, in particular the topical treatment of skin and scalp.

15. An oral care product comprising a composition according to any one of claims 1 to 10, wherein the oral care product is preferably a toothpaste, a mouthwash, an oral gel, a dental varnish or a polishing paste.