DE102017009626A1 - Oral composition with citrus extract and hydroxyapatite - Google Patents

Abstract

The present invention relates to an oral composition comprising hydroxyapatite and citrus extract, and their use in particular in oral biofilm control.

Description

The present invention relates to an oral composition comprising hydroxyapatite and citrus extract, and their use in particular in oral biofilm control.

In terms of carbohydrate and sugar diet, oral care is gaining importance in many countries. Thus, in addition to esthetic aspects, particular emphasis is placed on precautionary measures, whereby the reduction or even prevention of plaque, tooth decay and / or halitosis (halitosis) as well as healthy gums are the focus here.

Among other things, the gum is characterized by the fact that it surrounds the teeth cervically. The gum surrounds the neck of the tooth, thereby sealing the entry point of the tooth into the jawbone of the oral cavity. The gum thus serves, inter alia, the protection and as a holder of the tooth.

The different parts of a natural tooth are the tooth crown, the tooth neck and the tooth root, which are composed of several layers. Of these layers, one usually only sees the outer enamel, which surrounds the dentin and other layers. For example, to bite or grind food, the enamel is very hard. It consists of about 97% by weight of hydroxyapatite, which has the following empirical formula: Ca ₅ (PO ₄ ) ₃ (OH). The dentin is also considered hard tooth substance and consists of about two thirds also of hydroxyapatite. Dentin contains proteins and water in addition to hydroxyapatite and is therefore not as hard as the enamel.

Common dental and gum diseases such as tooth decay and periodontitis may be due to the formation of bacterial microfilms and / or due to bacterial inflammation.

Caries is considered to be a multi-influential disease, especially of enamel and dentin, with the involvement of microorganisms such as bacteria. Thus, in a first step on the tooth surface, a precipitate, also called pellicle, can be formed, among other things, from saliva protein. The rougher the tooth surface, the easier the precipitate can form on it or adhere to it. From this pellicle is then formed after a time a tooth surface covering, a few microns thick film. Bacteria can then multiply and spread on this film, this film being called a biofilm. Furthermore, said bacteria can produce organic acids, such as gluconic and lactic acids, from low molecular weight carbohydrates commonly present in food today.

Both these organic acids produced by bacteria and the dietary acids, such as fruit acids, can cause erosion of the hard tooth substance. Among other things, calcium phosphates are dissolved out of the enamel. If this process is not halted, or preferably vice versa, demineralization of the enamel and possibly also of the dentin may occur after some time. A defect in the hard tooth tissue is called a carious lesion. For example, carious lesions on the dentin layer can be identified as having a yellow to brown colouration of the corresponding part of the tooth. So while carious lesions on the enamel alone often can be reduced or eliminated by re-mineralizing the enamel, is carious lesions that affect in addition to the enamel also other layers, usually the damaged part of the tooth removed and the resulting hole with a Filling material closed.

Periodontal disease, which is also colloquially referred to as "periodontal disease", is a bacterial inflammation of the gums, which can show in an irreversible destruction of the periodontium apparatus. Periodontitis is triggered by a bacterial plaque, also known as plaque. Similar to what has been described above for caries, this usually tough adherent bacterial plaque or film may also be referred to as a biofilm. One feature of periodontal disease is the detectable bone loss, which is reported to be triggered by enzymes destined to destroy the bacterial biofilm, but among others these enzymes also lead to the destruction of native tissue. This can lead to the loss of connective tissue and bones.

Halitosis, also known as halitosis, is an unpleasant odor of exhaled air. Halitosis may have local causes, including inflammation of the periodontium (see Periodontitis), Lack of oral or tongue hygiene, inflammation of the oral mucosa and / or gums, infections (eg candidosis) and poor dental status (caries, root remnants).

In summary, it can be said that the formation of bacterial biofilms is a crucial factor for dental and gum diseases such as caries and periodontitis. Since tooth decay and / or periodontal disease can be among other causes of bad breath, it is therefore considered that the formation of biofilms can also be an important factor in halitosis.

For this reason, different active ingredients are currently used to reduce and avoid biofilms (oral biofilm control / oral biofilm management).

Chlorhexidine has proven to be particularly effective in reducing and avoiding biofilms. On the one hand, chlorhexidine has anti-adherent properties with regard to biofilms. This means that by chlorhexidine the initial bacterial colonization of a surface such as the tooth surface can be reduced or even prevented. Furthermore, chlorhexidine has antimicrobial properties, so that by using it already existing biofilms can be reduced. Overall, therefore, a good oral biofilm control can be achieved by the use of chlorhexidine in principle.

However, the use of chlorhexidine involves some significant disadvantages. It is known that a relevant effect for caries prophylaxis in chlorhexidine is not always reproducible and occurs only in a part of the investigated cases. Furthermore, the antimicrobial effect of chlorhexidine is not limited to the oral bacteria involved in caries formation, but also includes the control of beneficial bacteria. Furthermore, chlorhexidine should be used only in a short-term application, as long-term treatment with chlorhexidine-containing products may lead to undesirable side effects such as discoloration of the tooth surfaces or impairment of the taste sensation. From the cosmetic point of view, the use of chlorhexidine alone is not very beneficial in everyday dental care, simply because of the discoloration of the tooth surfaces.

An alternative biofilm control measure could be (synthetic) hydroxyapatite particles. Preliminary investigations indicate that both hydroxyapatite particles, which have been obtained by tooth wear and, in particular, oral care products, can interfere with biofilm management. However, in this application areas are problematic, which are already covered with plaque, which in particular the molars and / or interdental spaces are mentioned.

Thus, biomimetic tooth and mouthwashes can be treated with "artificial enamel" e.g. Containing zinc carbonate hydroxyapatite. Zinc carbonate hydroxyapatite based products can reduce initial bacterial colonization on the enamel surface without having antimicrobial properties, i. they have the anti-adherent properties described above, while not disturbing the environmental balance of the oral cavity. In addition, these products are designed to remineralise and repair microfine defects in the enamel and dentin, as well as to form a protective layer. As mentioned above, however, problems could arise in this context with poorly accessible and / or plaque-covered areas.

Thus, there continues to be a significant need for oral care products to effectively treat (i.e., reduce and prevent) oral biofilms.

Therefore, it is the object of the present invention to provide a product for oral care and in particular for dental care, with which oral biofilms can be effectively reduced and / or prevented.

For this purpose, in particular the initial adhesion of bacteria on both the tooth and in the interstices and the transition to the gums should be advantageously reduced.

Furthermore, a control or reduction of existing biofilms, especially in the hard to reach areas of teeth and gums to be achieved.

A biofilm control is to be achieved without significantly disrupting the ecological balance in the oral cavity and / or risking tooth discoloration or taste disorder.

These objects are surprisingly achieved by the present application according to the claims.

In particular, it has unexpectedly been found that the oral composition according to the invention achieves both a favorable reduction of initial bacterial colonization and the control of already existing biofilms in regions of the oral cavity which are difficult to access and thus tooth and gum diseases can be effectively counteracted.

Furthermore, a protective layer can be applied to the tooth by the composition according to the invention. In addition, it was found that the enamel has a higher resistance to acid after the application of the composition according to the invention. Finally, the addition of chlorhexidine can be dispensed with in the present composition.

Thus, a good biofilm management including an excellent caries and / or periodontitis prophylaxis can be ensured even in hard to reach places such as the interdental spaces as well as preventing or reducing the bad breath without disturbing or destroying the bacterial balance in the oral cavity, for example.

The subject of the present invention is an oral composition comprising hydroxyapatite Ca ₅ (PO ₄ ) ₃ (OH) and citrus extract.

Within the scope of the present application, the oral composition according to the invention may also comprise oral cosmetic and / or medical care products.

Ca ₅ (PO ₄ ) ₃ (OH) is also known as hydroxyapatite and more rarely hydroxyapatite. It is a mineral from the mineral class of phosphates, which crystallizes in a hexagonal crystal system. In addition, hydroxyapatite is a member of the apatite group and forms a complete mixed series with chlorapatite and fluorapatite.

The Ca ₅ (PO ₄ ) ₃ (OH) comprised in the present oral composition is preferably prepared synthetically. This means that the Ca ₅ (PO ₄ ) ₃ (OH) used is preferably not obtained by burning out the organic constituents from animal material, such as, for example, bones.

In a preferred embodiment, Ca ₅ (PO ₄ ) ₃ (OH) is present in pure form. According to the invention, a pure form exists if the ions containing Ca ₅ (PO ₄ ) ₃ (OH) (Ca ²⁺ , PO ₄ ^3- and OH ^- ) are each less than 1%, preferably less than 0.5%. even more preferably less than 0.1% are substituted by one or more other ions. For example, in pure hydroxyapatite, the Ca ²⁺ ions are exemplified by Mg ²⁺ or Zn ²⁺ and the OH ^- ions are less than 1%, preferably less than 0.5%, more preferably less than, for example, fluoride or chloride 0.1% substituted.

Thus, the composition according to the invention comprises (pure) Ca ₅ (PO ₄ ) ₃ (OH), hydroxyapatite, as the only apatite component.

It has been shown that by the use of Ca ₅ (PO ₄ ) ₃ (OH) as Apatitkomponente on the addition of fluorides such as CaF ₂ and / or fluoroapatite, which were previously used, for example, for hardening the enamel and fighting tooth decay, in the present oral compositions can be dispensed with. Thus, the negative effects that are currently being discussed in the context of fluoride-containing dental care and oral products can be avoided in any case. One of these negative effects is the so-called fluorosis, which is caused by excessive fluoride intake and causes symptoms such as nausea, vomiting and diarrhea. Other examples are bone fluorosis, which is manifested by thickening of the outer bone layer and concomitant loss of elasticity and resilience of the bones, and enamel fluorosis, which is evident from the appearance of whitish enamel spots on the tooth surface. In addition, it is reported that the ingestion of high-dose dental care products, especially in children can trigger an acute fluoride intoxication, which can sometimes even be fatal. Furthermore, it is reported that WHO is unable to establish a value for a daily fluoride requirement since fluoride is not an essential trace element and thus there are no diagnostic parameters and no evidence of the existence of clinical symptoms of "fluoride deficiency".

Furthermore, the composition according to the invention comprises Ca ₅ (PO ₄ ) ₃ (OH), hydroxyapatite, preferably in a particulate form. That is, Ca ₅ (PO ₄ ) ₃ (OH) is preferably in a particle or particle form.

The X ₅₀ value of the volume-based particle size distribution Q ₃ (x) of the Ca ₅ (PO ₄ ) ₃ (OH) is preferably 1.0 to 15.0 μm, preferably 1.2 to 12.0 μm, more preferably 1.5 to 10.0 microns, most preferably 2.0 to 5.0 microns, wherein the X ₅₀ value of the volume-based particle size distribution is measured by laser diffraction.

For this purpose, a sample of the hydroxyapatite is first sonicated in an ultrasonic homogenizer with an energy output of 96 W for 9 minutes and then for 3 minutes in a device for sample preparation. The subsequent particle size distribution measurement (laser diffraction) is performed in a particle sizing instrument at a temperature of 25 ° C ± 0.3 ° C and the corresponding values are calculated according to the Mie theory. The measuring instruments used are exclusively commercially available devices.

In a preferred embodiment of the invention, the Ca ₅ (PO ₄ ) ₃ (OH) 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 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 evaluation of the corresponding X-ray powder diffractograms. The X-ray powder diffractograms themselves are obtained by measurement with a conventional powder diffractometer at the routine settings.

It is further preferred that the Ca ₅ (PO ₄ ) ₃ (OH) used according to the invention has a substantially spherical crystal morphology. In particular, it is preferred that the Ca ₅ (PO ₄ ) ₃ (OH) has no acicular crystal morphology. Such a needle-like crystal morphology could entail undesirable disadvantages similar to asbestos.

In a preferred embodiment, the Ca ₅ (PO ₄ ) ₃ (OH) is present in aggregated form. In this case, an aggregation is understood to mean an aggregation of molecules or particles into a larger dressing, the aggregate. This assembly or aggregate is caused and held together by various forces and / or modes of attachment such as ionic bonding, van der Waals forces, intermolecular forces or other chemical bonding modes. The degree of aggregation and also the size of the aggregate can be determined by scanning electron microscopy. It is preferred that with Ca ₅ (PO ₄ ) ₃ (OH) in aggregated form, no nanoparticles can be detected even after high energy input. Nanoparticles are particles with a size of less than 100 nm. With regard to nanoparticles, it is not yet known if they can have an adverse effect on humans, for example after a possible penetration of the intestinal wall.

A hydroxyapatite suitable according to the invention is described, for example, in the copending application DE 10 2016 114 189.5 described.

A suitable hydroxyapatite according to the invention is available, for example, under the name KALIDENT 100 Ist B (PF210715G1) or KALIDENT POWDER 100-B (PF210715G4) from Kalichem Italia s.r.l., Rezzato, Italy.

The oral composition according to the invention comprises citric extract as further constituent. A citrus extract is an extract that can be obtained using a citrus extraction process.

An extraction process is to be understood as meaning a separation process in which one or more components are extracted from the extraction material, a mixture of substances, with the aid of a solid, gaseous or liquid optionally heated extractant. The dissolved component (s), whether they are still dissolved in the extractant or not, are referred to as an extract, which can then be concentrated as needed by partially or completely removing the extractant. In a purely physical extraction, the extracted components are / are present in unchanged form. A chemical extraction is when the component / s undergo a chemical reaction, for example with the extractant.

As extracting agents, it is possible to use solvents which dissolve the component (s) to be extracted better than the mixture in the extraction material. Depending on the solubility of the component (s) to be extracted, water / steam, steam, acids, bases and liquefied carbon dioxide are used as organic solvents, for example alcohols, terpenes, diethyl ether, vegetable oils, chlorinated Hydrocarbons or n-hexane used as extractant. In order to increase the solubility of components to be extracted, the extraction can be carried out with warm / hot extractant and / or under pressure.

A citrus fruit is the special form of a berry of citrus plants, which belong to the family of the rhododendrons. The citrus fruits include, for example, bergamot, bitter orange, blood orange, clementine, grapefruit, Jaffa (orange), kumquat, lime, tangerine, Meyer lemon, minneola, orange, grapefruit, pomelo, Rangpur, Satsuma and lemon.

The citrus extract comprised by the oral composition according to the invention is preferably obtained by the extraction of citrus fruits with water / glycerol (solvent or extractant mixture). For this purpose, the citrus fruits are preferably freed from the shell and the remaining residue, the extraction material, obtained by macerating the extraction material with the above-mentioned mixed solution. In a preferred embodiment, a mixture of citrus fruits is used to obtain the citrus extract. Particularly preferred is a mixture of bitter orange, tangerine and orange. Furthermore, solid components are preferably separated from the citrus extract, for example by filtration, and the resulting citrus extract is then preferably further concentrated and centrifuged. The supernatant extract is then stored in isolated form until quality control. The citrus extract preferably comprises 40 to 80 percent by weight, more preferably 45 to 75 percent by weight, especially 50 to 70 percent by weight of glycerine.

In a preferred embodiment, the citrus extract comprised by the composition of the invention contains organic acids in an amount of from 1 to 10% by weight, preferably from 2 to 9.5% by weight, more preferably from 2.5 to 9.0% by weight, especially from 3.0 to 8.5 Weight percent based on the citrus extract.

In the context of the present application, organic acid is understood to mean an organic compound which undergoes an equilibrium reaction with water, an oxonium ion H ₃ O ^{+ being} formed by the release of a proton of the acid to water.

The organic acids include the group of carboxylic acids. Members of this group include one or more carboxy groups attached to an organic radical, - COOH.

Examples of organic carboxylic acids are acetic, propionic, adipic, lactic, tartaric, butyric, oxalic, citric, capric and malic acids.

In a preferred embodiment, the organic carboxylic acid comprises 2-10 carbon atoms, preferably 3 to 6 carbon atoms. Particularly preferred are citric and / or lactic acid.

Furthermore, the enols and phenols belong to the group of organic acids.

Enols are compounds in which a carbon-carbon double bond is substituted with a hydroxy group. The phenols are characterized by the fact that the carbon-carbon double bond belongs to an aromatic system.

In a preferred embodiment, the organic carboxylic acid comprises an enol of 4-12 carbon atoms, more preferably 5-10 carbon atoms. Particularly preferred is ascorbic acid.

In a preferred embodiment, the citrus extract comprised by the composition according to the invention contains polyphenols in an amount of 1 to 10% by weight, preferably 1.5 to 8.0% by weight, in particular 2.0 to 6.5% by weight, based on the citrus extract.

Polyphenols are aromatic compounds which carry two or more hydroxy groups as substituents. They belong to the phytochemicals and have an antioxidant effect and serve as a filter for high-energy UV-B radiation. Examples of polyphenols are flavonoids and anthocyanins, procyanidins and stilbene derivatives such as resveratrol.

• - 40 - 80 Gew.%, bevorzugt 45 - 75 Gew.%, mehr bevorzugt 50 - 70 Gew.% Glycerin,
• - 1 - 10 Gew.%, bevorzugt 2 - 9,5 Gew.%, mehr bevorzugt 2,5 - 9 Gew.%, insbesondere 3 - 8,5 organische Säuren
• - 1 - 10 Gew.%, bevorzugt 1,5 - 8 Gew.%, mehr bevorzugt 2 - 6,5 Gew.% Polyphenole

In a preferred embodiment of the invention, the citrus extract comprises

• - 40-80% by weight, preferably 45-75% by weight, more preferably 50-70% by weight glycerol,
• - 1 - 10 wt.%, Preferably 2 - 9.5 wt.%, More preferably 2.5 to 9 wt.%, In particular 3 - 8.5 organic acids
• From 1 to 10% by weight, preferably from 1.5 to 8% by weight, more preferably from 2 to 6.5% by weight, of polyphenols

Furthermore, the citrus extract comprised by the composition according to the invention may preferably contain water and further substances such as vitamins, minerals and / or trace elements.

An inventively suitable citrus extract is available, for example under the name Biosecur ^® C320C by the company Biosecur Lab.

In a preferred embodiment, the composition of the invention may contain a surfactant.

Surfactants are amphipathic molecules and consist of an oil and a water-soluble part. In other words, surfactants have a lipophilic and a hydrophilic part. Surfactants are classified based on the hydrophilic part and its charge. There is the class of nonionic, cationic, anionic and amphoteric surfactants.

The hydrophilic part of a nonionic surfactant is not charged. A nonionic surfactant does not comprise a dissociable group but has one or more polar groups such as ethers, ketones and alcohols. Frequently used nonionic surfactants are, for example, polyalkylene glycol ethers.

Cationic surfactants are positively charged in their hydrophilic part. Most cationic surfactants are quaternary ammonium compounds with halides as the counterion, such as distearyldimethylammonium chloride.

The hydrophilic part of an anionic surfactant is negatively charged. The anionic surfactants often carry as anionic part carboxy, alkoxy, sulfonate or sulfate groups with alkali or alkaline earth metal ions as counterion. An example of an anionic surfactant is sodium lauryl sulfate.

Depending on the pH, the hydrophilic portion of an amphoteric surfactant comprises at least one group that is or may be positively charged and at least one group that is or may be negatively charged. The group which is or can be positively charged is, for example, an amine or ammonium group. The group which is or may be negatively charged is, for example, a carboxy, alkoxy, sulfonate or sulfate group. Examples of amphoteric surfactants are amphoacetates, amphodiacetates, amphopropionates, amphodipropionates, sulfobetaines, and hydroxysultaines.

In a preferred embodiment, the surfactant comprised by the composition of the invention is an anionic or an amphoteric surfactant. Most preferably, the surfactant is selected from sodium lauryl sulfate, sodium cocoamphopropionate, cocoamidopropyl betaine, cocoamidopropyl hydroxy-sultaine, and sodium cocoamphoacetate, or mixtures thereof.

Preferably, the composition according to the invention contains surfactant in an amount of 0.05 to 5 wt.%, More preferably 0.07 to 4 wt.%, In particular 0.1 to 3 wt.%, Based on the total amount of the oral composition.

In a preferred embodiment, the oral composition according to the invention may contain one or more pharmaceutical or cosmetic auxiliaries. These pharmaceutical or cosmetic excipients are described, for example, in Toothpastes, Monographs in Oral Science, Vol. 23, 1 ^st edition, 2013 described.

Preferably, one or more pharmaceutical or cosmetic adjuvants comprises antimicrobials, pH regulators, xylitol, abrasives and flavorings.

Antimicrobial substances are substances that kill microorganisms, such as bacteria, or can greatly reduce their multiplication. In addition to antimicrobial substances with a non-specific defense against bacteria and fungi, there are also those that, for example, only act against specific bacteria. For example, the use of antimicrobial substances can also combat bad breath become. Preferably, antimicrobial substances may be contained in an amount of 0.01 to 1.0% by weight, preferably 0.05 to 0.5% by weight, in the oral composition of the present invention. Examples of the antimicrobial substances used in oral care are zinc compounds such as zinc chloride and zinc citrate, as well as chlorhexidine, triclosan, cetylpyridinium chloride and stannous chloride.

In a preferred embodiment, the composition according to the invention contains cetylpyridinium chloride. Furthermore, it is particularly preferred that the composition according to the invention does not contain chlorhexidine.

pH regulators are substances that can adjust a specific pH range, preferably a neutral range of pH 6.5 to 7.5. In the case of an acidic composition, there would be a risk of demineralization of the tooth hard substance (erosion). Examples of pH regulators are sodium hydroxide (NaOH) or phosphoric acid (H ₃ PO ₄ ), which can be used according to the desired pH. To raise too low a pH, sodium hydroxide may be added while at too high a pH, phosphoric acid may be added.

Furthermore, the oral composition according to the invention preferably contains xylitol. Xylitol can minimize the number of caries bacteria and inhibit their growth. Furthermore, xylitol can stimulate the salivation. The composition according to the invention may contain xylitol in an amount of 0.5 to 10% by weight, preferably 0.7 to 8% by weight, based on the total weight of the oral composition. In addition to xylitol, the composition of the invention may contain other sugar alcohols such as sorbitol.

Abrasives, also known as cleaning agents or abrasives, usually remove plaque and harmful bacteria from the tooth surface during tooth cleaning, along with the toothbrush, and may also lighten the skin. Abrasives may preferably be included in the oral composition of the invention in an amount of up to 10% by weight, based on the total weight of the oral composition. Examples of abrasives are whiting, marble powder and / or silicate compounds such as silica.

Flavorings can give the oral composition according to the invention the desired taste. In addition, flavorings can be saliva-stimulating, whereby the moisture of the saliva can have a positive influence on the remineralization of the tooth. An example of a saliva-stimulating flavorant is pellitorin, especially trans-pellitorin.

Furthermore, dentifrice compositions often contain fluoride compounds such as sodium fluoride, amine fluorides or zinc fluoride. In a particularly preferred embodiment, the oral composition according to the invention contains no fluoride compound and is thus fluoride-free.

As described above, the oral composition according to the invention may also comprise oral medical and / or cosmetic care products. These oral medical and / or cosmetic care products may be in any form known to those skilled in the art. The oral composition according to the invention is preferably in the form of a toothpaste, a mouth gel, a gum bag or a mouth rinse.

A toothpaste, also referred to as toothpaste, can be used for mechanical tooth cleaning and is a soft or semi-solid composition for oral use, especially on the teeth.

A mouth gel is a gel-like composition that can be used in the treatment of discomfort / pain, for example on the oral mucosa, gums and lips or to combat dry mouth. The oral gel is usually applied to the painful area such as in the case of aphthae on the oral mucosa.

For a gingival gum gel, essentially the same applies as for a mouth gel, with the gum pocket gum being applied essentially to the gum and the pockets it contains.

A mouthwash, also known as mouthwash, is a liquid that can be used, among other things, for the prophylaxis of tooth decay and other disorders in the mouth.

In a particularly preferred embodiment, the composition according to the invention is in the form of a toothpaste.

In an alternative particularly preferred embodiment, the composition according to the invention is in the form of a mouthwash.

The oral composition according to the invention preferably contains Ca ₅ (PO ₄ ) ₃ (OH) in an amount of 0.1 to 20% by weight, preferably 2.5 to 15% by weight, more preferably 3.5 to 13% by weight, in particular 4.5 to 11% by weight, based on the total weight of the oral composition. It is known that the amount of Ca ₅ (PO ₄ ) ₃ (OH) can also be dependent on the form in which the oral composition (toothpaste, oral gel, etc.) is present. For example, a toothpaste may contain a greater amount of Ca ₅ (PO ₄ ) ₃ (OH) than a mouthwash.

In a preferred embodiment, the oral composition according to the invention contains citrus extract in an amount of 0.01 to 1.5% by weight, preferably 0.05 to 1% by weight, more preferably 0.1 to 0.75% by weight, in particular 0, 15 to 0.5% by weight, based on the total weight of the oral care composition.

• - 5 bis 15 Gew.%, vorzugsweise 8 bis 12 Gew.% Ca₅(PO₄)₃(OH),
• - 0,05 bis 1 Gew.%, mehr bevorzugt 0,1 bis 0,75 Gew.%, insbesondere 0,15 bis 0,5 Gew.%, Zitrusextrakt
• - 0,07 bis 4 Gew.%, insbesondere 0,1 bis 3 Gew.%, Tensid
• - 0,05 bis 0,5 Gew.%, vorzugsweise 0,07 bis 0,35 Gew.%, Zinksalz, insbesondere Zinkchlorid,
• - 0,01 bis 0,6 Gew.%, vorzugsweise 0,015 bis 0,4 Gew.%, antimikrobielle Substanz, insbesondere Cetylpyridiniumchlorid,
• - 0,1 bis 3 Gew.%, vorzugsweise 0,3 bis 2,0 Gew.%, pH-Regulator, insbesondere Phosphorsäure,
• - 3 bis 10 Gew.%, vorzugsweise 4 bis 8 Gew.%, Xylit,
• - 1 bis 10 Gew.%, vorzugsweise 2 bis 8 Gew.%, Abrasivstoff, insbesondere Silica und
• - 0,25 bis 5 Gew.%, vorzugsweise 1,5 bis 4,5 Gew.%, Aromastoff, insbesondere Pellitorin,

wobei sich die Angaben in Gew.% auf das Gesamtgewicht der Oralzusammensetzung beziehen. Der pH-Wert liegt in einem neutralen Bereich von pH 6,5 bis 7,5.In a preferred embodiment, the oral composition according to the invention is a toothpaste and contains

• From 5 to 15% by weight, preferably from 8 to 12% by weight, of Ca ₅ (PO ₄ ) ₃ (OH),
• - 0.05 to 1 wt.%, More preferably 0.1 to 0.75 wt.%, In particular 0.15 to 0.5 wt.%, Citrus extract
• - 0.07 to 4 wt.%, In particular 0.1 to 3 wt.%, Surfactant
• From 0.05 to 0.5% by weight, preferably from 0.07 to 0.35% by weight, zinc salt, in particular zinc chloride,
• 0.01 to 0.6% by weight, preferably 0.015 to 0.4% by weight, antimicrobial substance, in particular cetylpyridinium chloride,
• From 0.1 to 3% by weight, preferably from 0.3 to 2.0% by weight, pH regulator, in particular phosphoric acid,
• From 3 to 10% by weight, preferably from 4 to 8% by weight, of xylitol,
• - 1 to 10 wt.%, Preferably 2 to 8 wt.%, Abrasivstoff, in particular silica and
• 0.25 to 5% by weight, preferably 1.5 to 4.5% by weight, flavoring agent, in particular pellitorin,

the data in% by weight refer to the total weight of the oral composition. The pH is in a neutral range of pH 6.5 to 7.5.

• - 2 bis 7 Gew.%, vorzugsweise 3 bis 6 Gew.% Ca₅(PO₄)₃(OH),
• - 0,05 bis 1 Gew.%, mehr bevorzugt 0,1 bis 0,75 Gew.%, insbesondere 0,15 bis 0,5 Gew.%, Zitrusextrakt
• - 0,07 bis 4 Gew.%, insbesondere 0,1 bis 3 Gew.% Tensid,
• - 0,2 bis 1,0 Gew.%, vorzugsweise 0,3 bis 0,7 Gew.%, Zinksalz, insbesondere Zink-PCA,
• - 0,01 bis 0,06 Gew.%, vorzugsweise 0,015 bis 0,04 Gew.%, antimikrobielle Substanz, insbesondere Cetylpyridiniumchlorid,
• - 0,1-3 Gew.% pH-Regulator,
• - 0,5 bis 2 Gew.%, vorzugsweise 0,75 bis 1,5 Gew.%, Xylit und
• - 0,25 bis 5 Gew.% Aromastoff, insbesondere Pellitorin,

wobei sich die Angaben in Gew.% auf das Gesamtgewicht der Oralzusammensetzung beziehen. Der pH-Wert liegt in einem neutralen Bereich von pH 6,5 bis 7,5.In an alternatively preferred embodiment, the oral composition according to the invention is a mouthwash and contains

• From 2 to 7% by weight, preferably from 3 to 6% by weight, of Ca ₅ (PO ₄ ) ₃ (OH),
• - 0.05 to 1 wt.%, More preferably 0.1 to 0.75 wt.%, In particular 0.15 to 0.5 wt.%, Citrus extract
• 0.07 to 4% by weight, in particular 0.1 to 3% by weight of surfactant,
• From 0.2 to 1.0% by weight, preferably from 0.3 to 0.7% by weight, zinc salt, in particular zinc PCA,
• 0.01 to 0.06% by weight, preferably 0.015 to 0.04% by weight, antimicrobial substance, in particular cetylpyridinium chloride,
• 0.1-3% by weight of pH regulator,
• - 0.5 to 2 wt.%, Preferably 0.75 to 1.5 wt.%, Xylitol and
• 0.25 to 5% by weight of flavoring agent, in particular pellitorin,

the data in% by weight refer to the total weight of the oral composition. The pH is in a neutral range of pH 6.5 to 7.5.

Furthermore, the present invention relates to the oral composition according to the invention for use in the reduction and / or avoidance of oral biofilms.

By using the oral composition of the invention, both the Neukolonisation of oral biofilms sustainably avoided as well as existing biofilms effectively reduced or completely removed. This does not only apply to biofilms on easily accessible places in the mouth. Rather, a successful biofilm management can be achieved even in hard to reach places such as the interdental spaces.

In a preferred embodiment, the oral composition according to the invention is used for the treatment and prophylaxis (prevention) of caries, periodontitis and halitosis. Thus, for example, the tooth hard substance, in particular the enamel, for a time protected against the increased settlement of harmful bacteria. In addition, the tooth enamel can be remineralized by the oral composition according to the invention, so that tooth decay, in particular in the early stages, can be treated, for example, by the repair of microcracks.

The invention will be explained below by way of examples.

Examples:

The citrus extract used in the following examples is the citrus extract Biosecur C320C ^® by the company Biosecur LAB.

Example 1:

A toothpaste was made containing the following ingredients: Demineralised water 117.24 g (39.08%) citrus extract 0.75 g (0.25%) xylitol 21.00 g (7.00%) zinc chloride 0.60 g (0.20%) glycerin 39.00 g (13.00%) sorbitol 45.00 g (15.00%) sodium carboxymethyl cellulose) 3.00 g (1.00%) Aroma 3.00 g (1.00%) N-cetylpyridinium chloride 0.060 g (0.020%) hydroxyapatite 30.00 g (10.00%) Aroma 1.05 g (0.35%) silica 15.00 g (5.00%) Silica, highly dispersed 7.50 g (2.50%) sodium lauryl sulfate 1.20 g (0.40%) Natriumcocoamphopropionat 1.20 g (0.40%) cocoamidopropyl 1.20 g (0.40%) Cocoamidopropylhydroxy-sultaine 1.20 g (0.40%) , sodium 1.20 g (0.40%) tetrapotassiumpyrophosphate 9.00 g (3.00%) Ortho-phosphoric acid 1.80 g (0.60%)

The toothpaste is a light beige, homogeneous, creamy paste with a taste of menthol and anise and has an averaged pH of 7.2.

Example 2:

A mouthwash was prepared containing the following ingredients: Purified water 6180.48 g (68.922%) citrus extract 22.5 g (0.25%) hydroxyethyl 36.00 g (0.40%) N-cetylpyridinium chloride 1.80 g (0.02%) Zinc PCA 45.00 g (0.50%) xylitol 90.00 g (1.00%) sweetener 0.72 g (0.008%) Aloe vera powder 4.50 g (0.05%) glycerin 1980.00 g (22.00%) Aroma 45.00 g (0.50%) Vegetol Matricaria 45.00 g (0.50%) , sodium 9.00 g (0.10%) tetrapotassiumpyrophosphate 45.00 g (0.50%) disodiumpyrophosphate 45.00 g (0.50%) hydroxyapatite 450.00 g (5.00%)

The mouthwash is a whitish suspension with a taste of menthol and anise and has an averaged pH of 6.6.

QUOTES INCLUDE IN THE DESCRIPTION

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

Cited patent literature

• DE 102016114189 [0038]

Cited non-patent literature

• Oral Science, Vol. 23, 1 ^st edition, 2013 [0066]

Claims (13)

Oral composition comprising - Ca ₅ (PO ₄ ) ₃ (OH) citrate extract. Oral composition after Claim 1 wherein the X ₅₀ value of the volume-based particle size distribution Q ₃ (x) of Ca ₅ (PO ₄ ) ₃ (OH) is 1.0 to 15.0 μm, the X ₅₀ value of the volume-based particle size distribution being determined by means of laser diffraction. Oral composition after Claim 1 or 2 , wherein the citrus extract is obtained by extraction of citrus fruits with water / glycerol. Oral composition according to one of Claims 1 to 3 wherein the citrus extract contains organic acids in an amount of 1 to 10% by weight. Oral composition according to one of Claims 1 to 4 wherein the citrus extract contains polyphenols in an amount of 1 to 10% by weight. Tooth care composition according to one of Claims 1 to 5 wherein the citrus extract comprises: - 40 to 80% by weight of glycerol - 1 to 10% by weight of organic acids - 1 to 10% by weight of polyphenols. Oral composition according to one of Claims 1 to 6 which further comprises a surfactant. Oral composition after Claim 7 wherein the surfactant is selected from sodium lauryl sulfate, sodium cocoamphopropionate, cocoamidopropyl betaine, cocoamidopropylhydroxy-sultaine and sodium cocoamphoacetate. Oral composition according to one of Claims 1 to 8th wherein the dentifrice composition further contains one or more pharmaceutical or cosmetic excipients. Oral composition after Claim 9 wherein the pharmaceutical excipient is cetylpyridinium chloride. Oral composition according to one of Claims 1 to 10 wherein the oral composition contains Ca ₅ (PO ₄ ) ₃ (OH) in an amount of 0.1 to 20% by weight, based on the total weight of the oral composition. Oral composition according to one of Claims 1 to 11 wherein the oral composition contains citruse extract in an amount of 0.01 to 1.5% by weight, based on the total weight of the oral composition. Use of the oral composition according to any one of Claims 1 to 12 for reducing and / or avoiding oral biofilms.