Composition for oral hygiene products containing n-cetylpyridinium chloride, a flavonoid and a polymer

Abstract

A composition, in particular for the prophylaxis and / or treatment of caries, gingivitis, halitosis and / or arteriosclerosis, comprises N-cetylpyridinium chloride, at least one flavonoid, at least one polymer, in particular a homopolymer comprising at least one monomer having a polar functional group, in particular polylysine, and optionally chlorhexidine, wherein the weight ratio of chlorhexidine to N-cetylpyridinium chloride is between 0 and 7, in particular between 0.01 and 6, especially between 0.1 and 5, more especially between 0.2 and 4, for example between 0.4 and 3.2.

Description

[0001] Composition for oral hygiene products

[0002] Technical field

[0003] The invention relates to a composition, in particular for the prophylaxis and / or treatment of caries, gingivitis, halitosis and / or arteriosclerosis. The invention further relates to mouthwash, toothpaste, dental chewing gum, tablets, dental floss and / or dental cleaning gel comprising the composition, as well as the composition for use in the prophylaxis and / or treatment of caries, gingivitis, halitosis and / or arteriosclerosis, and the composition for use as a medicinal product.

[0004] State of the art

[0005] Oral hygiene is an essential part of a daily health routine, and numerous products are available to support oral health. Toothpaste, mouthwash, and dental floss are among the best-known aids that promise to effectively prevent cavities, gingivitis, and halitosis. Particular attention is paid to ingredients such as fluoride, which is specifically designed to combat the cavity-causing bacterium Streptococcus mutans (S. mutans).

[0006] WO 99 / 18999 (Pharmaceutical Biotechnologies, Inc.) concerns a formulation primarily for plaque prophylaxis and the prevention of periodontal diseases such as caries by increasing the retention time of corresponding active ingredients in the oral cavity. The bacterial species S. mutans is considered one of the causes of these diseases. The formulation comprises polysaccharide-degrading enzymes and anchor molecules coupled to these enzymes, resulting in an enzyme-anchor molecule complex. The anchor molecules allow the enzyme-anchor molecule complex to adhere better to the oral cavity, thus prolonging the enzyme's activity. The enzyme-anchor molecule complex binds to the side of the anchor molecule, for example, to existing plaque, thereby reducing potential substrate sites for the attachment of pathogenic bacterial colonies. Preferred enzymes include, for example...Esterases or enzymes are used to cleave glycolytic, ether, or carbon-nitrogen bonds. The formulation can be used, for example, in mouthwashes. WO 99 / 18999 also mentions proteins, protein fragments, and polypeptides, such as Lys-Lys-Glu-Lys-Lys, as examples of anchor molecules. EP 0 737 470 Al (Quest International BV) describes an anti-plaque formulation in which the anti-plaque active ingredient is present in colloidal form and encapsulated by a polymer. The polymer can contain antibodies, carbohydrate, or peptide structures that are recognized by plaque-producing bacteria, thus transporting the active ingredient, e.g., zinc oxide, directly to the bacteria. At acidic pH values, zinc ions, for example, can then be released. EP 0 737 470 Al also mentions, by way of example, that optional antibacterial agents, such as chlorhexidine or cetylpyridinium chloride (CPC), can be used.

[0007] WO 99 / 20239 (Novo Nordisk A / S) describes a composition for the prevention or treatment of plaque, including that caused by S. mutans. This composition utilizes starch-hydrolyzing and / or starch-modifying enzymes. The latter group includes, for example, CGTAse, mutanase, and / or dextranase. The composition can be an ingredient in toothpaste or mouthwash and may contain additives such as surfactants, sweeteners, flavorings, or antibacterial agents like chlorhexidine or zinc ions.

[0008] However, conventional oral hygiene products have proven unsatisfactory. While they may offer short-term freshness and a clean feeling, they don't always achieve the desired long-term effect. In many cases, chemical ingredients can cause irritation, and using oral hygiene products with insufficient antibacterial properties can even increase the risk of dental problems. Furthermore, while antibacterial agents in some oral hygiene products may reduce bacterial counts in the short term, their long-term effectiveness is often questionable.

[0009] Therefore, there is a need for improved solutions.

[0010] Description of the invention

[0011] The object of the invention is therefore to provide a solution that at least reduces the disadvantages present in the prior art. In particular, it is an object of the invention to provide a composition that inhibits the growth of harmful microorganisms in the oral cavity, protects the salivary biome, and has a long-lasting effect. Furthermore, it is an object of the invention to provide uses for the composition.

[0012] These problems are solved by the features of independent claim 1 and independent claims 14 and 15. The invention therefore relates to a composition, in particular for the prophylaxis and / or treatment of caries, gingivitis, halitosis and / or arteriosclerosis, comprising

[0013] (i) N-Cetylpyridinium chloride,

[0014] (ii) at least one flavonoid,

[0015] (iii) at least one polymer, in particular a homopolymer, comprising at least one monomer with a polar functional group, in particular polylysine,

[0016] (iv) and optionally chlorhexidine,

[0017] (v) wherein the weight ratio between chlorhexidine and N-cetylpyridinium chloride is between 0 and 7, in particular between 0.01 and 6, specifically between 0.1 and 5, and in particular between 0.2 and 4, for example between 0.4 and 3.2.

[0018] Tooth decay, also known as caries, is a progressive disease of the teeth caused by the destruction of tooth structure. It develops when bacteria in the mouth ferment sugars and other carbohydrates, producing acids. These acids attack the enamel, leading to demineralization and ultimately to cavities (holes or holes) in the tooth. If left untreated, tooth decay can cause pain, inflammation, and even tooth loss.

[0019] Gingivitis is an inflammation of the gums, usually caused by a buildup of plaque (bacterial deposits). It is the earliest form of periodontal disease and typically manifests as symptoms such as redness, swelling, and bleeding of the gums, especially when brushing or flossing. Gingivitis is usually reversible if treated early, primarily through improved oral hygiene. However, if left untreated, it can lead to more serious forms of periodontal disease, such as periodontitis.

[0020] Halitosis, also known colloquially as bad breath, is an unpleasant odor emanating from the mouth that can be caused by various factors. Common causes include bacteria in the mouth that decompose food particles, inadequate oral hygiene, certain foods (such as garlic or onions), smoking, dry mouth, or underlying health problems. Halitosis can be either temporary or chronic. Good oral hygiene and regular dental checkups can help prevent or treat halitosis. Atherosclerosis is a condition in which the walls of the arteries thicken and harden, leading to restricted blood flow. These changes are usually caused by deposits of fat, cholesterol, calcium, and other substances that form plaque.Arteriosclerosis can affect various blood vessels in the body and is a major risk factor for cardiovascular diseases such as heart attack and stroke.

[0021] N-Cetylpyridinium chloride (CPC) is a chemical compound used, among other things, as an antiseptic. It is frequently used in mouthwashes, toothpastes, and other oral hygiene products to regulate the oral flora and inhibit bacterial growth. CPC has antibacterial properties and can help reduce plaque and bad breath.

[0022] Flavonoids are a large group of secondary plant compounds found in many fruits and vegetables. They belong to the polyphenol family and are responsible for the color, taste, and aroma of plants. Flavonoids possess antioxidant properties and can help reduce cell damage caused by free radicals. They are also known for their potential health benefits, including supporting the cardiovascular system, reducing inflammation, and improving immune function.

[0023] By reducing oxidative stress and inflammation, flavonoids can improve endothelial function and inhibit the formation of atherosclerotic plaques. This can at least reduce the risk of arteriosclerosis.

[0024] A "polar functional group" is a functional group in a molecule that exhibits a charge distribution due to an unequal distribution of electrons among the atoms within the group. This results in a partial positive and a partial negative charge within the group. Examples of polar functional groups include the hydroxyl group (-OH), carbonyl group (C=O), amino group (-NH₂), carboxyl group (-COOH), nitro group (-NO₂), sulfhydryl group (-SH), amide group (-CONH₂), and phosphate group (-PO₄). 3 ), peroxide group (-OO-) and / or the cyano group (-CN).

[0025] In particular, the monomers of the at least one polymer exhibit one or more of the above-mentioned polar functional groups in the non-polymerized monomer and / or the above-mentioned polar functional groups are a component of the polymer, having been formed, for example, by the polymerization of the monomers.

[0026] Specifically, the at least one monomer with a polar functional group comprises an amino acid, specifically an amino acid which, in its unpolymerized state, has two amine groups and one carboxyl group. Most preferred is the at least one monomer with a polar functional group being lysine.

[0027] According to an advantageous embodiment, the at least one polymer is based on polymerized amino acids. This means that at least 50%, specifically at least 75%, for example at least 90%, and most specifically at least 99% or 100%, of all monomers in the polymer are amino acids or polymerized amino acids.

[0028] Homopolymers are polymers composed of only one type of monomer. This means that the repeating units in the polymer are made up of the same molecules. Homopolymers often have relatively uniform physical and chemical properties because they have a consistent structure. Examples of homopolymers include polyethylene (PE), which consists only of ethylene monomers, and polypropylene (PP), which consists only of propylene monomers.

[0029] Some homopolymers, such as polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), polyacrylic acid (PAA), and / or polyethylene glycol (PEG), have the advantage of improving the viscosity of oral hygiene products, resulting in a pleasant and stable consistency. Furthermore, some homopolymers, such as PVA, PVP, and / or PAA, have the ability to adhere to tooth surfaces, which can prolong the effectiveness of oral hygiene products. They also exhibit antimicrobial properties and the ability to bind water, which can be particularly beneficial in cases of dry mouth. Some homopolymers, such as PVA, PVP, and / or PAA, can also enable the controlled release of active ingredients such as fluoride or other substances, leading to a longer duration of action and improving the effectiveness of oral hygiene products.

[0030] Polylysine is generally a homopolymer composed of repeated units of the amino acid lysine. It consists exclusively of lysine monomers linked by peptide bonds. Polylysine is positively charged because the side chains of the lysine units contain amino groups that are protonated at physiological pH. It is frequently used in biological applications, including cell culture, because it promotes cell adhesion.

[0031] Chlorhexidine is an antiseptic and disinfectant commonly used to kill bacteria, fungi, and some viruses. It works by disrupting the cell membranes of microorganisms, thus preventing their growth and reproduction. Chlorhexidine is used as a preservative in various medical and cosmetic applications, such as in mouthwashes, wound disinfectants, and for skin disinfection before surgical procedures. It is known for its long-lasting effect and is often used in dentistry to reduce plaque and gum inflammation.

[0032] A "salivary biome" refers to the entirety of microbial communities and their biological components found in saliva. This includes bacteria, viruses, fungi, proteins, enzymes, and other molecules detectable in saliva. The salivary biome plays an important role in oral health and can provide clues about overall health, as it can be linked to various conditions such as gum disease, tooth decay, or even systemic illnesses.

[0033] Surprisingly, it has been shown that the composition according to the invention leads to a more effective inhibition of the growth of S. mutans, affects the salivary biome less and has a longer lasting effect than known compositions.

[0034] The compositions according to the invention are characterized, for example, by the fact that an inhibitory effect on the growth of S. mutans is achieved at higher dilutions compared to compositions from the prior art. A further advantage is that the compositions according to the invention only affect the salivary biome at a lower dilution than is known from the prior art.

[0035] Due to the aforementioned advantages, a smaller quantity of the composition is required to inhibit S. mutans than is known in the prior art. This leads, on the one hand, to a reduced intake of chemical substances into the body while maintaining the same effectiveness of the oral hygiene products, and on the other hand, to lower consumption of ingredients for the production of the composition according to the invention. The latter protects the environment and reduces production costs.

[0036] Furthermore, another advantage is that a higher quantity of the composition is required to affect the salivary biome than with known prior art. This helps to protect the salivary biome, so that impairment is only observed at larger quantities of the composition.

[0037] An impaired salivary biome means that the natural balance of microorganisms and biochemical components in saliva is disrupted. A healthy salivary biome consists of a variety of bacteria, fungi, viruses, and other microbes that live together in a harmonious balance and contribute to oral health. Impairment can lead to the following consequences:

[0038] - Increased risk of oral diseases: An imbalance, such as an increase in pathogenic bacteria, can lead to gum inflammation (gingivitis), caries, periodontitis or halitosis;

[0039] - Reduced protective function: Saliva contains antimicrobial substances that help control harmful microbes. A disruption in the salivary biome can impair this protective function and promote infections;

[0040] - Possible systemic effects: Since the salivary biome is connected to the entire body, a disruption can also provide clues to systemic diseases such as diabetes or heart disease.

[0041] The composition according to the invention thus has the advantage that it can at least reduce, and in particular prevent, oral diseases and protect the salivary biome. Furthermore, it exhibits a high degree of persistence.

[0042] "Remanence" refers to the lingering effect of a condition over a longer period, even after the direct influence has ceased. In this context, remanence therefore refers to the long-term effect of the composition, which persists even after the composition has been introduced into the oral cavity, for example, through a mouthwash or toothpaste.

[0043] "Dilution" refers to the reduction of the concentration of a composition by adding a diluent such as water and / or another solvent. A "higher dilution" means the composition is more diluted, while a "lower dilution" means the composition is less diluted.

[0044] Without being bound by the theory, it is also assumed that the composition according to the invention can have a positive effect on the prophylaxis and / or treatment of arteriosclerosis. Since chronic inflammation plays an important role in the development of arteriosclerosis, the anti-inflammatory properties of the composition according to the invention could indirectly help to slow the progression of the disease.

[0045] Furthermore, although not bound to the theory, there are indications that a connection between oral bacteria and arteriosclerosis may exist. Oral bacteria could enter the arteries via the bloodstream and trigger inflammatory processes there, promoting the formation of atherosclerotic plaques. By reducing harmful oral bacteria, particularly through the composition according to the invention, the risk of such inflammation, and thus arteriosclerosis, could therefore be indirectly reduced, at least to some extent.

[0046] Tests have shown that the components of the composition according to the invention interact functionally and synergistically.

[0047] The weight ratio of chlorhexidine to N-cetylpyridinium chloride is between 0 and 7, in particular between 0.01 and 6, specifically between 0.1 and 5, and in particular between 0.2 and 4, for example between 0.4 and 3.2.

[0048] If chlorhexidine is present, the weight ratio between chlorhexidine and N-cetylpyridinium chloride is between >0 and 7, in particular between 0.01 and 6, specifically between 0.1 and 5, and in particular between 0.2 and 4, for example between 0.4 and 3.2.

[0049] In a particular embodiment, the weight ratio of chlorhexidine to N-cetylpyridinium chloride is < 0.1, in particular < 0.01.

[0050] There

[0051] The inventive weight ratio of chlorhexidine to N-cetylpyridinium chloride leads to a particularly effective inhibition of S. mutans and a particularly high degree of protection of the salivary biome.

[0052] In particular, the proportion of chlorhexidine is a maximum of 0.08 wt. - %, more specifically a maximum of 0.07 wt. - %, more preferably a maximum of 0.06 wt. - %, in particular a maximum of 0.05 wt. - %, most preferably a maximum of 0.01 wt. - %, based on the total weight of the composition.

[0053] The inventive components of chlorhexidine can reduce side effects of chlorhexidine, such as tooth discoloration, taste disturbances, dry mouth, changes in oral flora, allergic reactions, or increased blood pressure.

[0054] In a particularly preferred embodiment, the composition according to the invention does not include chlorhexidine. In this case, the ratio of chlorhexidine to N-cetylpyridinium chloride is zero. This has the advantage that the aforementioned undesirable side effects of chlorhexidine can at least be reduced, and in particular, completely eliminated.

[0055] Another advantage is that by reducing, and especially by eliminating, chlorhexidine, the effect of CPC can be enhanced.

[0056] It has therefore been found that by reducing, and especially by eliminating, chlorhexidine, less of the other components, i.e., CPC, flavonoids and / or polymers comprising at least one monomer with a polar functional group, is needed without reducing the effect of the composition.

[0057] In a particular embodiment, the composition according to the invention comprises, in particular instead of the at least one flavonoid, the oral antiseptic CITROX®. CITROX® comprises, among other things, polylysine, bioflavonoids, citric acid, glycerin and water.

[0058] In particular, the composition according to the invention comprises at least one fruit acid, in particular citric acid, and / or glycerin.

[0059] Specifically, the proportion of N-cetylpyridinium chloride is 0.005 to 0.045 wt. - %, in particular 0.015 to 0.035 wt. - %, and specifically 0.02 to 0.03 wt. - %, based on the total weight of the composition.

[0060] This leads to a particularly effective inhibition of S. mutans and a particularly high degree of preservation of the salivary biome.

[0061] The flavonoids are preferably derived from the plant Citrus aurantium amara.

[0062] These flavonoids have the beneficial properties of inhibiting inflammatory processes and thus helping to alleviate inflammation. This is particularly advantageous in the prevention of diseases such as arthritis and other inflammatory disorders.

[0063] Furthermore, the flavonoids from bitter orange (Citrus aurantium amara) can support heart health by lowering blood pressure, improving blood lipid levels (e.g., cholesterol), and promoting endothelial function. The antioxidant and anti-inflammatory effects of these flavonoids may help reduce the risk of cardiovascular disease.

[0064] Furthermore, these flavonoids can inhibit the growth of certain bacteria and viruses, thus contributing to a strengthened immune system. However, it is also possible that the flavonoids originate from other plants, such as sweet oranges (Citrus sinensis), blueberries, currants, strawberries or blackcurrants, apples, onions, grapes, wine, soybeans, buckwheat, broccoli, cabbage, parsley, thyme, ginkgo biloba, red clover, chili peppers, and / or bell peppers.

[0065] Flavonoids, especially glycosylated and / or non-glycosylated flavanones, are particularly favored.

[0066] Flavanones belong to the group of flavonoids, are widespread in citrus fruits and have antioxidant and anti-inflammatory properties due to their structure.

[0067] Glycosylated flavanones are flavanones that are linked to a sugar molecule. This allows them to exhibit better water solubility, which can increase their bioavailability.

[0068] Furthermore, the sugar molecules can increase the stability of flavanones in the blood, which can prolong their half-life and potentially lead to a prolonged effect in the body.

[0069] Non-glycosylated flavanones do not have sugar molecules bound to them. This allows them to have a simpler structure, which can lead to easier uptake into cells and enhance their antioxidant and anti-inflammatory properties. This can be particularly helpful in cases of acute inflammation.

[0070] In a further preferred embodiment, the flavanones comprise naringin, neohesperidin, neoriocitrin, isinarinagin, hesperidin, poncirin, rhiofolin, naringenin, hesperetin and / or neodiosmin.

[0071] These flavanones have the advantage of being able to exhibit a particularly anti-inflammatory effect.

[0072] In particular, the proportion of flavonoids is 0.02 to 0.2 wt. - %, especially 0.04 to 0.17 wt. - %, in particular 0.06 to 0.15 wt. - %, particularly preferably 0.08 to 0.12 wt. - %, based on the total weight of the composition.

[0073] This leads to a particularly effective inhibition of S. mutans and a particularly high degree of preservation of the salivary biome. In a particularly preferred embodiment, the polymer comprising at least one monomer with a polar functional group is a homopolymer, specifically polylysine.

[0074] The advantage of polylysine is that it has a strong antimicrobial effect, reduces plaque, inhibits biofilms, acts as a preservative, has a gentle effect on the gums and can promote oral health without resistance, while being biodegradable and non-toxic to humans.

[0075] Polylysine can destabilize the cell membrane of microorganisms, such as S. mutans, thus inhibiting their growth. This can at least minimize the formation of plaque, caries, gingivitis, halitosis, and / or arteriosclerosis.

[0076] Since polylysine can act as a preservative, it can inhibit the growth of harmful microorganisms in the product formulation itself, thus contributing to a longer shelf life of the product.

[0077] In contrast to antibiotics, polylysine can also promote oral health without the risk of bacteria in the mouth becoming resistant to treatment.

[0078] Furthermore, polylysine exhibits high cationicity, meaning it contains positively charged groups that readily adhere to the negatively charged surfaces of teeth and gums. This electrostatic attraction promotes adhesion to the tooth surface.

[0079] In particular, the polymer comprises at least one monomer with a polar functional group, e-poly-L-lysine. e-Poly-L-lysine has the advantage of exhibiting strong antimicrobial properties, high heat stability and water solubility, good biodegradability, and being non-toxic in the quantities used.

[0080] However, it is also possible that other polymers, individually or in combination with polylysine, are used, e.g. polyvinyl alcohol, chitosan, guar hydroxypropyltrimonium chloride and / or carboxymethylcellulose.

[0081] Specifically, the proportion of the at least one polymer comprising at least one monomer with a polar functional group is 0.002 to 0.045 wt. %, in particular 0.015 to 0.035 wt. %, and specifically 0.02 to 0.03 wt. %, based on the total weight of the composition.

[0082] In a further specific embodiment, the composition comprises levulinic acid and / or salts of levulinic acid. This is particularly in addition to preservatives commonly used in oral hygiene products, such as sorbates and / or benzoates, especially individually or in combination with their acid(s).

[0083] This has the advantage of improving the effectiveness of oral hygiene products, as levulinic acid and / or levulinic acid salts have antimicrobial and anti-inflammatory properties, contribute to wound healing and the regeneration of oral tissue, or help regulate pH, and / or can be used as preservatives or sweeteners. Furthermore, levulinic acid and / or levulinic acid salts pose a low risk of toxic reactions.

[0084] However, it is also possible that neither levulinic acid nor salts of levulinic acid are present in the composition according to the invention, and in particular that only conventional preservatives are present.

[0085] In particular, the proportion of levulinic acid and / or salts of levulinic acid is 0.001 to 1.5 wt. - %, especially 0.005 to 1.3 wt. - %, and specifically 0.010 to 1.0 wt. - %, based on the total weight of the composition.

[0086] Particularly preferably, the composition comprises a proportion of at least one flavonoid, especially from the plant Citrus aurantium amara, of 0.02 to 0.2 wt. %, a proportion of at least one polymer comprising at least one monomer with a polar functional group, especially polylysine, in particular E-poly-L-lysine, of 0.002 to 0.045 wt. %, a proportion of N-cetylpyridinium chloride of 0.005 to 0.045 wt. %, based on the total weight of the composition, and no chlorhexidine is present.

[0087] Specifically, the composition contains 0.1% w / w of at least one flavonoid, particularly from the plant Citrus aurantium amara; 0.025% w / w of at least one polymer comprising at least one monomer with a polar functional group, particularly polylysine, specifically E-poly-L-lysine; and 0.025% w / w of N-cetylpyridinium chloride, based on the total weight of the composition. Chlorhexidine is not present. This results in particularly effective inhibition of S. mutans and exceptional preservation of the salivary microbiome.

[0088] In another preferred embodiment, the composition comprises magnolol and / or a structural isomer thereof, such as honokiol, and / or a lignan, in particular a lignan-containing extract. In a particular embodiment, the lignan is magnolol.

[0089] Magnolol is a naturally occurring chemical compound and is found as the main component in magnolia bark.

[0090] The advantages of magnolol and honokiol are their antimicrobial properties, especially against bacteria associated with oral diseases, such as S. mutans, as well as their anti-inflammatory and antioxidant effects.

[0091] However, it is also possible that the composition does not include magnolol and / or a structural isomer thereof and / or a lignan.

[0092] In particular, the proportion of magnolol and / or its structural isomer, such as honokiol, and / or the lignan is 0.005 to 0.1 wt. %, especially 0.006 to 0.09 wt. %, and specifically 0.007 to 0.08 wt. %, based on the total weight of the composition.

[0093] Specifically, the composition includes fluorides.

[0094] Fluorides have the advantage of strengthening tooth enamel by being incorporated into the mineral structure of the teeth. This makes teeth more resistant and reduces the risk of cavities. Furthermore, fluorides can stabilize teeth and attract minerals such as calcium and phosphate, thus helping to treat early cavities. Additionally, fluorides have an antibacterial effect against bacteria in the mouth, such as S. mutans, which can help reduce plaque.

[0095] However, it is also possible that the composition according to the invention does not include fluorides.

[0096] In particular, the fluoride content is 0.01 to 0.2 wt.%, more specifically 0.02 to 0.1 wt.%, in particular 0.03 to 0.09 wt.%, and most specifically 0.04 to 0.06 wt.%, based on the total weight of the composition. The present invention relates in particular to mouthwash, toothpaste, dental chewing gum, tablets, dental floss and / or dental cleaning gel comprising a composition as described above.

[0097] This simplifies the application of the composition according to the invention, as it can be applied via the aforementioned oral hygiene products to where it can be most effective, i.e. in the oral cavity.

[0098] However, it is also possible that other products may include the composition according to the invention, e.g. interdental brushes, tongue cleaners and / or teeth whitening products.

[0099] A second aspect of the invention relates to a composition as described above for use in the prophylaxis and / or treatment of caries, gingivitis, halitosis and / or arteriosclerosis.

[0100] In a third aspect, the invention relates to a composition as described above for use as a medicinal product.

[0101] Brief description of the drawings

[0102] Fig. 1 A graphical representation of the minimum inhibitory concentration of two compositions according to the invention, "PZN" and "PZN 3", as well as a composition of a commercially available mouthwash, "HM", with respect to the growth of S. mutans. The minimum inhibitory concentration is the highest dilution of the sample (l: value of the vertical axis) that visibly inhibits the growth of S. mutans.

[0103] Fig. 2 A graphical representation of the minimum inhibitory concentration of two compositions according to the invention, "PZN" and "PZN 3", as well as a composition of commercially available mouthwash "HM", with regard to the impairment of the salivary biome. The minimum inhibitory concentration is the highest dilution of the sample (λ: value of the vertical axis) that visibly impairs the growth of the salivary biome.

[0104] Experiments

[0105] The effects of the invention claimed herein are supported by the following experimental data. The efficacy of S. mutans inhibition and the impairment of the salivary biome were measured for three different compositions, "PZN", "PZN3", and "HM". All three compositions are based on the following components in equal parts:

[0106] Propylene glycol, sodium gluconate, xylitol, polyglyceryl-3 caprate, sodium hyaluronate, polysorbate 20, sodium chloride, sodium hydroxide, trisodium ethylenediamine disuccinate, cyclodextrin, VP / VA copolymer, Givaudan Top Noch flavor, sucralose, guar hydroxypropyltrimonium chloride, anhydrous citric acid, sodium phosphate buffer and sodium benzoate.

[0107] "PZN", "PZN3" and "HM" differ in their variable components according to the table below. The percentages given by weight refer to the total weight of the respective composition.

[0108] For dilution of the compositions (each consisting of base components + variable components), water was used as the solvent for all three compositions, and a dilution series was prepared. "PZN" and "PZN 3" correspond to embodiments of the present invention. "HM" corresponds to a composition of a commercially available mouthwash.

[0109] Figure 1 shows the minimum inhibitory concentration (MIC) for the three compositions "PZN", "PZN3", and "HM" with respect to the inhibition of S. mutans growth. "HM" corresponds to a commercially available chlorhexidine-containing mouthwash. The minimum inhibitory concentration, or the lowest concentration in a dilution series, is the lowest concentration of an antimicrobial agent required to inhibit the growth of a specific microorganism under standardized conditions. In other words, it is the smallest amount of an antibiotic or antiseptic needed to prevent the multiplication of bacteria, fungi, or other microorganisms.

[0110] Figure 1 shows on the x-axis the respective compositions "PZN", "PZN3" and "HM" and on the y-axis the dilution values ​​with which the dilution solutions described above were further diluted with water in the ratio l:"dilution value".

[0111] Figure 1 shows that "PZN 3" visibly impairs the growth of S. mutans even at a dilution of 1:316, followed by "PZN" at a dilution of 1:177. The commercially available composition "HM," on the other hand, performs worst, showing visible impairment of S. mutans growth only at a dilution of 1:100. Thus, the compositions according to the invention, "PZN" and "PZN 3," inhibit the growth of S. mutans even at high dilutions and entirely without chlorhexidine, meaning that a smaller quantity of each composition is required to achieve the desired effect compared to "HM."

[0112] Figure 2 shows the minimum inhibitory concentration for the three compositions "PZN", "PZN3" and "HM" with respect to the impairment of the growth of the salivary biome.

[0113] Figure 2 shows on the x-axis the respective compositions "PZN", "PZN3" and "HM" and on the y-axis the dilution values ​​with which the dilution solutions described above were further diluted with water in the ratio l:"dilution value".

[0114] Figure 2 shows that "PZN 3" only visibly impairs the growth of the salivary biome at a dilution of 1:3.2, followed by "PZN" at a dilution of 1:17.8. The commercially available composition "HM," on the other hand, performs worst, showing a visible impairment of salivary biome growth even at a dilution of 1:100. Thus, the compositions according to the invention, "PZN" and "PZN 3," only inhibit the growth of the salivary biome at low dilutions or higher concentrations, in contrast to "HM," which already produces the undesirable effect, i.e., impairs the salivary biome, at a higher dilution or lower concentration. The experimental results described above suggest that the absence of chlorhexidine reduces the effectiveness of the composition in preventing the growth of S. mutans and preserving the salivary biome.The residual effect is increased (compare "PZN" and "PZN 3" without chlorhexidine with "HM" including chlorhexidine). A further conclusion is that "PZN" and "PZN 3" are more selective against harmful bacteria such as S. mutans than "HM".

Claims

1. Patent claims 1. A composition, in particular for the prophylaxis and / or treatment of caries, gingivitis, halitosis and / or arteriosclerosis, comprising: (i) N-Cetylpyridinium chloride, (ii) at least one flavonoid, (iii) at least one polymer, in particular a homopolymer, comprising at least one monomer with a polar functional group, in particular polylysine, and (iv) optional chlorhexidine, (v) wherein the weight ratio between chlorhexidine and N-cetylpyridinium chloride is between 0 and 7, in particular between 0.01 and 6, specifically between 0.1 and 5, and in particular between 0.2 and 4, for example between 0.4 and 3.

2.

2. The composition according to claim 1, wherein the proportion of chlorhexidine is a maximum of 0.08 wt. %, in particular a maximum of 0.07 wt. %, particularly preferably a maximum of 0.06 wt. %, in particular a maximum of 0.05 wt. %, most preferably a maximum of 0.01 wt. %, based on the total weight of the composition.

3. The composition according to any of the preceding claims, wherein the proportion of N-cetylpyridinium chloride is 0.005 to 0.045 wt. %, in particular 0.015 to 0.035 wt. %, and in particular 0.02 to 0.03 wt. %, based on the total weight of the composition.

4. The composition according to any of the preceding claims, wherein the flavonoids are derived from the plant Citrus aurantium amara.

5. The composition according to any of the preceding claims, wherein the flavonoids are flavanones, in particular glycosylated and / or non-glycosylated flavanones.

6. The composition according to claim 5, wherein the flavanones comprise naringin, neohesperidin, neoriocitrin, isinarinagin, hesperidin, poncirin, rhiofolin, naringenin, hesperetin and / or neodiosmin.

7. The composition according to one of the preceding claims, wherein a proportion of flavonoids is 0.02 to 0.2 wt. - %, in particular 0.04 to 0.17 wt. - %, in particular 0.06 to 0.15 wt. - %, particularly preferably 0.08 to 0.12 wt. - %, based on the total weight of the composition.

8. The composition according to one of the preceding claims, wherein the at least one polymer comprising at least one monomer with a polar functional group is E-poly-L-lysine.

9. The composition according to one of the preceding claims, wherein a proportion of the at least one polymer comprising at least one monomer with a polar functional group is 0.002 to 0.045 wt. %, in particular 0.015 to 0.035 wt. %, in particular 0.02 to 0.03 wt. %, based on the total weight of the composition.

10. The composition according to any of the preceding claims, wherein the composition comprises levulinic acid and / or salts of levulinic acid.

1. The composition according to one of the preceding claims, wherein a proportion of levulinic acid and / or salts of levulinic acid is 0.001 to 1.5 wt. - %, in particular 0.005 to 1.3 wt. - %, in particular 0.010 to 1.0 wt. - %, based on the total weight of the composition.

12. The composition of one of the preceding claims, wherein a proportion of the at least one flavonoid, in particular from the plant Citrus aurantium amara, is 0.02 to 0.2 wt. %, a proportion of the at least one polymer comprising at least one monomer with a polar functional group, in particular polylysine, specifically E-poly-L-lysine, is 0.002 to 0.045 wt. %, a proportion of the N-cetylpyridinium chloride is 0.005 to 0.045 wt. %, based on the total weight of the composition, and no chlorhexidine is present.

13. The composition according to any of the preceding claims, wherein the composition contains magnolol and / or a structural isomer thereof, such as honokiol, and / or a lignan, in particular a lignan-containing extract.

14. Mouthwash, toothpaste, dental care chewing gum, tablets, dental floss and / or dental cleaning gel comprising a composition according to any one of claims 1-13.

15. Composition according to any one of claims 1-13 for use in the prophylaxis and / or treatment of caries, gingivitis, halitosis, and / or arteriosclerosis.

16. Composition according to any one of claims 1-13 for use as a medicament.

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