WO2021013283A1 - Oral hygiene agents containing caffeine and l-lysin as bitter blocking agents - Google Patents

Abstract

The present invention relates to compositions for oral hygiene agents, in particular toothpastes, which contain caffeine and lysin-containing bitter blocking agents.

Description

Oral hygiene products containing caffeine and L-lysine as bitter blockers

description

Background of the invention

Caffeine has a positive impact on the cardiovascular system. In the study Spyridopoulos et al. (2008), Arterioscler Thromb Vase Biol, 28, 1967-1974, it was shown that in humans, after consuming four cups of coffee, a caffeine concentration of 20-50 micromoles / liter is achieved in the blood serum, for a total of 15-35 milligrams corresponds.

Caffeine in these physiological concentrations led to functional improvements in the cells of the innermost layer of the blood vessel wall, the endothelial cells, and their precursors. Interestingly, these phenomena were dependent on intact mitochondria, which assigns these cell organelles a central role in improving the function of endothelial cells through caffeine.

Mitochondria provide the energy the body needs in the form of the adenosine triphosphate (ATP) molecule. The substrates required for this, so-called reduction equivalents (NADH ⁺ H ⁺ and FADH2) originate from the citrate cycle and fatty acid oxidation, processes that also take place in the mitochondria.

The reduction equivalents are introduced into the respiratory chain, where they are used to reduce oxygen to water. As a by-product of the respiratory chain, oxygen radicals are constantly being created, which damage macromolecules such as proteins, lipids and the DNA present in the mitochondria and can ultimately damage the functioning of the mitochondria.

The production of oxygen radicals increases with advancing age and is also increased in cardiovascular diseases and type 2 diabetes mellitus, which explains the loss of function of the mitochondria both in old age and in the diseases mentioned.

Recent studies provide evidence of the molecular mechanism of caffeine on mitochondria. According to recent studies, caffeine has an intensifying effect on the import of p27 (CDKN1B, "Cyclin Dependent Kinase Inhibitor 1B") into mitochondria. This was accompanied by an improvement in the function of various cell types in the heart.

CONFIRMATION COPY Heart muscle cells were thus protected from cell death, such as that which occurs during a heart attack. Furthermore, connective tissue cells of the heart, cardiac fibroblasts, were able to differentiate better into myofibroblasts. Myofibroblasts compensate for dead heart muscle cells by forming scar tissue. Furthermore, endothelial cells showed an increased ability to migrate, this is essential for the healing of vascular damage.

In mice, the functionality of the mitochondria from old animals could be brought back to the level of younger animals by administration of caffeine depending on p27. Ultimately, the administration of caffeine in the drinking water of mice reduced the damage after an experimental heart attack, which had previously been brought to the physiological level of a type 2 diabetic using special diets.

These studies support the findings from epidemiological studies, according to which moderate caffeine consumption has a positive effect on the cardiovascular system.

In addition, it has long been known that caffeine increases the analgesic potency of acetylsalicylic acid or paracetamol.

Further applications are, in addition to increasing alertness or the elimination of signs of fatigue, circulatory and respiratory stimulation, prevention of bronchopulmonary dysplasia, and other effects on skin and hair.

Details of the invention

Moderate consumption of caffeine in safe and effective amounts is therefore considered to be medically beneficial. However, the intake of caffeine, e.g. through the consumption of coffee and tea, is not always achievable or is not a preferred means. Tea and coffee consumption, for example, can have negative effects on gastrointestinal diseases, in particular the acid contained in coffee can trigger heartburn or other complaints in people. Negative cosmetic effects, such as the discoloration of the teeth from frequent tea or coffee consumption, are also a reason for some to refrain from consuming them completely. Some diets or medication also prohibit the morning consumption of coffee or tea. Of course, taste preferences also play a role. There are therefore a number of groups of people who do not have easy access to caffeine in safe and effective amounts.

It is therefore part of the present invention to make caffeine available in oral hygiene products, particularly toothpaste, mouthwash and the like. The oral-topical Dosage form avoids a number of the aforementioned side effects, as the caffeine is absorbed directly through the oral mucosa and does not have to be absorbed through the gastrointestinal tract. In this form, the administered caffeine does not lead to the usual discoloration of the teeth, as is the case with coffee and tea, for example. The administration can also be easily integrated into the daily morning routine, even if lack of time, diets or medication prohibit the morning consumption of coffee or tea.

However, this approach also poses problems which the present invention has been able to overcome.

Oral hygiene products are usually not swallowed, but rather spat out. Therefore, for the amount of caffeine to be effective, it must be in a sufficiently large concentration. However, caffeine is relatively bitter and therefore has a very unpleasant taste from a certain concentration.

It is therefore important to mask the bitterness of the caffeine with a suitable bitter blocker.

In the context of the present invention, a bitter blocker was therefore developed which, in taste tests, allows a pleasant taste experience even with high caffeine concentrations.

The present invention relates to compositions for oral hygiene products comprising: caffeine and at least one bitter blocker.

The caffeine contained in the composition according to the invention, in a safe and effective amount, can be produced synthetically (e.g. anhydrous caffeine (Ph. Eur.)) Or an extract from one of the plants or plant families produced using conventional methods: coffee (Cojfea), guarana ( Paullinia cupana), mate (Ilex paraguariensis), tea (Camellia sinensis), kola nut (Cola) and / or cocoa (Theobroma cacao). Combinations of various of the aforementioned caffeine sources are also conceivable.

The aim of this invention is to give the end user a dose of caffeine per application of the oral hygiene agent which corresponds to one cup of coffee or 100 mg of caffeine. Accordingly, a “portion” of the oral hygiene agent, as it is usually used, should contain between 50 and 200 mg, in one embodiment 75 to 150 mg, in other embodiments 80, 85, 90, 95, 100, 105, 110, 115, 120 mg of caffeine .

A "portion" is to be understood here as the amount of oral hygiene product that is recommended for consumption per application.

A usual “portion” for toothpaste is in the range of approx. 1 to 1.5 g, but in some embodiments it can also be between 0.5 and 3 g. A usual "portion" for mouthwashes is around 15 ml, in some embodiments between 5 and 30 ml. For dental care chewing gums, for example, one or two chewing gums.

The person skilled in the art can determine the corresponding percentage of the total weight composition on the basis of the target amount of approx. 100 mg caffeine, the average density of caffeine and the usual portion size of the respective oral hygiene agent.

The proportion of caffeine in the total composition by weight of toothpastes is usually between 1% and 20%; between 10% and 15%; in one embodiment more than 5%, 10%, 15%; in a further embodiment up to 13%, 15%, 18%, 19%, 20%; in one embodiment exactly 13%.

The proportion of caffeine in the total composition by weight in mouthwashes is usually between 0.5% and 10%; in another embodiment between 1% and 5%; in one embodiment at more than 1%, 2% and up to 3%, 4%, 5%; in one embodiment at about 2%, in another embodiment at 2.3%.

The bitter blocker according to the invention consists between 0.5 to 15%, in one embodiment between 2 and 12%, in a further embodiment between 3 to 10%, in a further embodiment 1, 2, 3, 4, 5, 6, 7, 8 or 9% from L-lysine, in a further embodiment as L-lysine hydrochloride and a bitter blocker carrier. Here, enough bitter blocker carrier is added that a total percentage of 100% is achieved for the bitter substance itself. For example, 85% bitter blocker carrier with 15% L-lysine, 95% bitter blocker with 5% L-lysine; and up to 99.5% bitter blocker carrier with 0.5% L-lysine. In one embodiment, the bitter blocker consists of 8% L-lysine and 92% bitter blocker carrier, in another embodiment 7% L-lysine and 93% bitter blocker carrier, in another embodiment 9% L-lysine and 91% bitter blocker carrier. The amino acid lysine, especially the L-enantiomer, is one of the most important ingredients in nutrient solutions for artificial nutrition. It is needed in the body for building muscle and building other amino acids. It is also involved in bone growth, cell division and wound healing. As a so-called “essential” amino acid, the substance must be taken in through food because the body cannot produce it itself. L-lysine plays an important role in the repair, maintenance and regeneration of tissue, bones, hormones, enzymes and cells. The body also uses lysine to synthesize its own camitine and collagen. As a collagen component, L-lysine can influence the elasticity of the skin. Lysine also keeps the nitrogen balance in the body and plays an important role in the immune system.

It is a surprising finding of the present invention, however, that L-lysine is also suitable as a bitter blocker. Based on the prior art, this was not to be expected, since the taste of pure L-lysine is described as slightly bitter.

Without being tied to a specific molecular mechanism, the surprising finding of this invention is that L-Lysine is able to suppress the bitterness of caffeine without triggering other negative taste impressions in the required concentrations, such as "powderiness", " Furry ”“ saltiness ”,“ excessive sweetness ”or“ sour taste ”.

In this regard, L-lysine is also advantageous over other bitter blockers known in the art, such as adenosine monophosphate (AMP). Free AMP has a regulatory effect as an allosteric effector molecule, inter alia, in the phosphofructokinase reaction positively regulated by AMP or in the fructose diphosphatase reaction negatively regulated by AMP. As a cyclic AMP (cAMP) it plays a role as a second messenger in cellular signal transduction (transmission of nerve impulses) and in particular leads to the activation of many peptide hormones (protein kinases). Therefore, undesirable side effects of AMP or cAMP cannot be ruled out and have not yet been conclusively investigated.

In addition, the taste impression of products with AMP is described as that of “meat broth”, so there is the assumption that the taste impression “umami” is triggered by AMP. In addition, as a bitter blocker, AMP influences the taste perception on a very broad level, so that certain taste suggestions are then described by test persons as "bland" or "uninteresting". It was therefore a further object of the present invention to provide a bitter blocker which does not have the described side effects of AMP and is nevertheless suitable for blocking or reducing the bitter taste of caffeine. L-lysine in the composition described here solves this problem.

“Bitterness” is a subjective taste impression that cannot be assessed by test procedures without the involvement of test persons.

The reduction in bitterness is determined by interviewing a sufficiently large number of test persons who receive the composition to be tested with different bitter blocker concentrations and who rate the subjective bitterness from 1 to 10 (1 = no bitterness, 10 = maximum bitterness) in a questionnaire.

During the survey, an average value is then formed that is below 5 in one embodiment, below 4 in another embodiment, below 3, below 2 and up to a value between 1 and 0 in another embodiment.

At the same time, the test persons are asked to describe other unusual taste sensations, such as "numbness", "furiness", "meat broth taste", etc. during the survey.

Ideally, the selected bitter blocker concentration has a good value of less than 5, 4 or 3 in the evaluation of the bitterness, without causing unusual or undesirable other taste sensations.

The bitter blocker carrier, which supplements the bitter blocker L-lysine, is in one embodiment maltodextrin, ie a water-soluble carbohydrate mixture that is produced by hydrolysis of starch (poly-a-glucose) using the methods of the prior art. It is hydrolyzed partly by acid and partly by enzymatic means.

Maltodextrin is a mixture of monomers, dimers, oligomers and polymers of glucose. The percentage composition differs depending on the degree of hydrolysis. This is described by the dextrose equivalent. According to the invention, maltodextrins with a dextrose equivalent between 3 and 20. But maltodextrins with a dextrose equivalent of more than 20 (dry glucose) can also be used, in particular, for example, in solid products such as chewing toothpaste, dental care chewing gum or the like.

The ideal concentration of the bitter blocker can be determined by the previously described interviews with test persons. However, the weight percentage of caffeine can also be added per 100g oral hygiene product is considered a good indicator to determine the weight percentage of the biterblocker. In some embodiments, a ratio of 3: 1 to 1: 3, in some embodiments from 2: 1 to 1: 2, in some embodiments from 2.2: 1 to 2.9: 1; aimed in one embodiment of 2.6: 1 of caffeine and biterblockers.

In toothpastes, the proportion by weight of the bit blocker according to the invention is below 10%, below 8%, below 6%; less than 5%; in one embodiment between 0.01%, 0.1%, 0.5%, 1% and up to 6%, 8% or 10%, in some embodiments between 3% and 5%, or in one embodiment exactly at 5 %.

In the case of mouthwashes, the weight percentage is between 0.1% and 5%; between 0.1% and 1%, between 0.2% and 0.6%, in another embodiment at 0.4%; in another embodiment at 1%.

Too high concentrations of more than 6%, more than 10%, more than 15% of the bit blocker can affect the taste in some compositions and make the taste impression "furry". In some cases, concentrations of the bit blocker that are too low of less than 0.4%, less than 0.3% and less than 0.2% do not adequately block bitterness and can lead to a rejection of the product, especially in the case of sensitive people.

In addition to L-lysine, the composition can also contain other substances that have a positive effect on the bitterness of the composition, such as sodium gluconate (complexing agent), sodium saccharin (sweetener) and flavorings. One embodiment contains, for example, coconut oil (Cocos Nucifera Oil), which has a masking effect and also reduces or inhibits the basic smell or taste of the product.

In addition to caffeine and the bit blocker (L-lysine with bit carrier maltodextrin) and other substances that have a positive effect on bitterness, the composition according to the invention for oral hygiene can contain the following additional ingredients, depending on the intended use:

For toothpaste compositions, a toothpaste carrier comprising a dental abrasive, a surfactant, a thickener, a humectant, a flavoring and / or sweetening agent, a fluorine source, colorants and / or water.

For mouthwash compositions, a mouthwash carrier comprising an alcohol (e.g., ethanol or propanediol), a humectant, a surface-active agent, a flavor and / or sweeteners, a source of fluorine, antibacterial agents, coloring agents and / or water.

For dental solution composition, a dental solution carrier comprising a preservative, preferably paraben preservative and / or water.

For chewing toothpaste (toothpaste tablets) e.g. microcrystalline cellulose, sodium bicarbonate, silica gel, sodium lauroyl, glutamate, magnesium stearate, aroma, menthol, xanthan gum, stevioside, citric acid, sodium fluoride, eugenol.

For dental care chewing gum e.g. gum, sweetener (e.g. xylitol, aspartame), sorbitol, thickener (e.g. gum arabic), humectant (e.g. glycerine), flavors, filler (s) (e.g. calcium phosphate), emulsifier (e.g. soy lecithin), acesulfame K, dyes) (e.g. E171), coating agents (e.g. camauba wax), antioxidants (e.g. Bha), dyes) (e.g. E133).

The pH value of the compositions of the present invention, for which compositions the pH value can be measured, is in one embodiment 2 to 9, in another embodiment 4 to 8, in another embodiment 6.0 to 7.0.

The% numbers used here always relate to percent by weight (abbreviation% by weight), i.e. the proportion of a substance in a mixture or a solution, which is measured in grams per 100 g mixture. For example, 15% or 15 percent by weight in this application correspond to the statement: “The mass fraction of the mixture component i is 15%” (or in the form of an equation: wi = 15%).

A "safe and effective amount" as used herein means an amount of a substance high enough to produce a marked positive change in the condition being treated, but low enough to avoid severe side effects (with a reasonable benefit / Risk ratio), as part of the sound medical assessment.

"Topical oral carrier" or "Carrier ⁴ , as used herein, refers to a carrier for the composition which is administered topically to the oral cavity, held therein for a period of time and then largely spat out rather than swallowed. Such compositions include toothpastes, tooth gels, Tooth powders, mouthwashes, mouth sprays, prophylactic pastes, dental treatment solutions, biogels or other sustained release products and the like. The components of the topical oral carrier are suitable for administration into the oral cavity of a human or lower animal (dogs, cats, pets and farm animals) and are compatible with each other and with the other components used in an oral composition of the present invention.

The term "compatible" as used herein means that the components of the compositions are capable of being mixed with one another in such a way that no interaction occurs which, under normal conditions of use, would considerably reduce the effectiveness of the oral composition.

Topical oral carriers according to this invention accordingly provide the desired properties for toothpastes, tooth gels, tooth powders, mouthwashes, mouth sprays, prophylactic pastes, dental treatment solutions and the like. The topical oral carriers include components that are typically used in such compositions known to those skilled in the art.

Such components include, but are not limited to, anti-caries agents, anti-plaque agents, anti-tartar agents, dental abrasives, surfactants, flavorings, sweeteners, binders, humectants, thickeners, buffers, preservatives, dyes and pigments, ethanol, and water.

Water is an optional component of the topical oral carrier of the compositions of the present invention. Water used to make the commercially useful compositions should preferably be of low ionic content and free of organic contaminants. Preferably water makes up from 2% to 99%, in one embodiment from 20% to 95% of the compositions of the present invention. When the compositions are in the form of toothpastes, they preferably contain 2% to 45%, in another embodiment 30% to 40% water, while mouthwashes in another embodiment 45% to 95%, in another embodiment 75% to 90% Contain water.

Dental abrasives suitable for the topical oral carriers of the compositions of the present invention include a wide variety of materials. The material selected must be one which is compatible within the composition of interest and which does not unduly abrade the enamel. Suitable abrasives include, for example, silicas including gels and fillings, insoluble sodium polymetaphosphate, hydrated alumina and resinous abrasives.

9 In one embodiment, the composition contains propylene glycol as a carrier (substance).

One group of abrasives of the invention for use in the present compositions are particulate thermosetting polymerized resins. Suitable resins include, for example, melamines, phenolic resins, urea resins, melamine-urea resins, melamine-formaldehyde resins, urea-formaldehyde resins, melamine-urea-formaldehyde resins, crosslinked epoxides and crosslinked polyesters.

Silica dental abrasives are also used in the compositions of the present invention. The abrasive, polishing silica material usually has an average particle size between 0.1 and 30 μm, preferably between 5 and 15 μm. The abrasive can be precipitated silica or a silica gel. Mixtures of abrasives can also be used.

The total amount of abrasives in the dentifrice compositions of the present invention preferably ranges from 10 to 30%; Toothpastes preferably contain 15 to 20% abrasive. Solutions, mouth sprays and mouthwash compositions of the present invention can contain amounts of abrasive as low as 0%.

Flavoring agents may be used in the topical oral carriers of the compositions of the present invention to make them more palatable. Typical flavoring agents include methanol, wintergreen oil, peppermint oil, spearmint oil, sassaffa oil, and clove oil. When flavoring agents are included, they are usually present in the present compositions in an amount of from 0.04 to 2%. In some compositions of this invention the aroma “Optamint ^® (257459)” has been used, a fresh type of peppermint with a very complex bouquet-note combination of anise, clove, cardamom, coriander, nutmeg and juniper.

Sweeteners are also used in the topical oral carriers of the compositions of the present invention in some instances to make them more palatable. Typical sweeteners include saccharin salts, dextrose, levulose, thaumatin, aspartame, D-tryptophan, dihydrochalcones, acesulfame and cyclamate salts, especially sodium cyclamate and sodium saccharin. When present, sweeteners are usually present in the instant compositions in amounts from 0.01 to 5%.

Another optional component of the topical oral carriers of the compositions of the present invention is a humectant. The humectant is used to prepare toothpaste compositions while they are exposed to air to keep it from hardening, and to impart a moisturizing sensation to mouthwashes and toothpaste compositions. Certain humectants can also impart a desired sweetness of taste to mouthwash and toothpaste compositions.

The humectant, on a pure humectant basis, usually constitutes 0 to 70%, preferably 2 to 55% of the present compositions. Suitable humectants for use in the compositions of the present invention include edible polyhydric alcohols such as glycerin, sorbitol, xylitol, polyethylene glycol and propylene glycol, especially sorbitol and glycerin. Further humectants are e.g. hydrogenated starch hydrolysates.

Buffer materials are another optional component of the topical oral carriers of the compositions of the present invention. The buffering agents serve to keep the pH of the compositions within the preferred range. The buffering agents usually make up 0-10%, preferably 0.2-5%, of the present

Compositions from. Suitable buffering agents for use in the

Compositions of the present invention comprise soluble phosphate salts.

Other optional components of the topical oral carriers of the compositions of the present invention are preservatives. The preservatives prevent microbial growth in the compositions. Suitable preservatives include methyl paraben, propyl paraben, benzoates and ethanol. When the preservative is ethanol it usually makes up 0 to 35%, preferably 5 to 15% of that of the invention. Compositions from. Other preservatives usually make up 0 to 5%, preferably 0.1 to 2% of the compositions according to the invention.

Binders and thickeners can be used in the topical oral vehicles of the compositions of the present invention, particularly in toothpaste compositions. Binders and thickeners according to the invention include, for example, carrageenan (e.g. Irish moss, Viscarin TP-5, which is an iota-carrageenan), cellulose derivatives (e.g. hydroxyethyl cellulose, sodium carboxymethyl cellulose, sodium carboxymethyl hydroxypropyl cellulose), carboxyvinyl polymers (carbomers, natural gums), natural gums (e.g. karay gums) arabicum, tragacanth gum), polysaccharide gums (e.g. xanthan gum), fumed silica, and colloidal magnesium aluminum silicate. In one embodiment, cellulose gum (cellulose gum). In another embodiment, hydrated silica and / or silica as an abrasive and thickening agent.

When present, these binders and thickeners are included in amounts from 0.1% to 5% of the compositions of the present invention.

The compositions of the present invention can also contain a surfactant. Suitable surfactants are those which are reasonably stable and preferably foam over the pH range of the compositions. Surfactants which are useful as foaming agents can be soaps and anionic, nonionic, cationic, zwitterionic and amphoteric organic synthetic detergents and compatible mixtures thereof. The terms “surface-active agent” and “surface-active agent” are used synonymously in this application.

Such surfactants are usually present in the compositions of the present invention at a level of from 0% to 10%, preferably from 0.2% to 5%. Surfactants can also be used as solubilizers to help keep poorly soluble components, such as some flavoring agents, in solution. Suitable surfactants for this purpose include polysorbates and poloxamers.

The compositions of the present invention can also contain surfactants such as sodium C14-C16 olefin sulfonate (Sodium C14-C16 olefin sulfonate).

The compositions of the present invention can also contain one or more solubilizers. Solubilizers according to the invention are sodium lauriminodipropionate and / or cocamidopropyl betaine in concentrations of 0.1% -3%; in one embodiment at 0.5%, 1% or 1.5%.

Tripotassium citrate can also be present in the composition in one embodiment; it increases the solubility of zinc citrate and reduces the astringent effect. The sensitivity of the teeth to pain can be reduced. Sensible concentrations are between 0.5% and 5%, in one embodiment 1%, 1.5% or 2%.

The compositions of the present invention can therefore also contain zinc citrate. Zinc citrate has an antimicrobial effect and thus against plaque and bad breath, has an anti-inflammatory effect and a tartrate-inhibiting effect and thus leads to whiter teeth. Concentrations of 0.1% - 3% can be provided; in one embodiment at 0.5%, 1% or 1.5%.

The compositions of the present invention can also contain zinc chloride. Zinc chloride has an antimicrobial effect and prevents plaque, and

Bad breath before.

The compositions of the present invention can also contain sodium pyrophosphate (Sodium Pyrophosphate). It acts as a complexing agent, supports the preservation and prevents discoloration.

The compositions of the present invention can also contain one or more anti-caries agents. Anti-caries agents according to the invention are water-soluble fluoride ion sources. Usually, fluoride ions also help stabilize pyrophosphate (usually an anti-tartar agent) in the oral cavity, thereby enhancing the benefits provided by any soluble pyrophosphate included in the compositions. Fluoride ion source materials of the present invention include: sodium fluoride, potassium fluoride, and sodium monofluorophosphate, and mixtures thereof. Sodium fluoride is the preferred source of fluoride in one embodiment. The amount of the fluoride ion sources in the oral compositions of the present invention, if present, is preferably sufficient to provide 0.005% to 0.35%, in a further embodiment 0.05% to 0.3% fluoride ions in the compositions. A fluoride source according to the invention is pure sodium fluoride. (Ph.Eur.) 450 ppm fluoride glycerine in a concentration of 0.01%; 0.05%, 0.1%, 0.2%, 0.3% and up to 0.5%, 0.6%; 0.7% 0.8%; 0.9%, or up to 1%.

Antimicrobial anti plaque agents can also be optionally present in the oral compositions of the present invention. Such active ingredients can be triclosan or 5-chloro-2- (2,4-dichlorophenoxy) phenol. When antimicrobial anti-tartar agents are present, they typically constitute 0.1 to 5% of the compositions of the present invention.

The compositions of the present invention can also contain one or more anti-tartar agents. Anti-tartar agents that can be useful in the compositions of the present invention include pyrophosphates or polyphosphates, polyacrylates, polycarboxylates, polyepoxysuccinates, ethylenediaminetetraacetic acid, nitrilotriacetic acid and related compounds, and polyphosphonates. When a When anti-tartar agents are present, it usually constitutes 0.2% to 13%, preferably 0.4% to 6% of the compositions of the present invention.

The compositions of the present invention may contain dyes such as Chlorophyllin Sodium Dye (C.I.75810), Vegebrite Lime Green Blend LWS, Vegebrite Blue Spirulina PWS, Dye (C.I.74160), and / or Dye (C.I.44090). When making the selection, it is of course important to have approval as a food coloring.

Another composition contains an “optical effect substance” such as Timiron ^® Snowflake MP-99 as “mica / pearlescent luster”.

Compositions of the present invention according to the invention are in the form of toothpastes. The components of such toothpastes usually include a dental abrasive (from 10% to 50%), a surfactant (from 0.5% to 10%), a thickener (from 0.1% to 5%), a moisturizer (from 10%) to 55%), a flavor title (from 0.04% to 2%), a sweetener (from 0.1% to 3%), a coloring title (from 0.01% to 0.5%) and water (from 2 % to 45%). Such toothpastes can also contain one or more anti-caries agents from 0.05% to 0.3%, such as fluoride ion), an anti-tartar agent (from 0.1% to 13%) and an anti-plaque agent (from 0.1% to 5%) exhibit. In one embodiment, the composition contains Aroma Optamint ^® (257459).

Other compositions of the present invention according to the invention are mouthwashes and mouth sprays. The components of such mouthwashes and mouth sprays include water (from 45% to 95%), ethanol (from 0% to 25%), a moisturizer (from 0% to 50%), a surfactant (from 0.01% to 7% ), a flavor title (from 0.04% to 2%), a sweetener (from 0.1% to 3%) and a coloring title (from 0.001% to 5%). Such mouthwashes and mouth sprays can also contain one or more anti-caries agents (from 0.05% to 3%, such as fluoride ion), an anti-tartar agent (from 0.1% to 3%), and an anti-plaque agent (from 0.1% to 5%) include.

Other compositions of the present invention according to the invention are dental solutions. The components of such dental solutions usually include water (from 90% to 99%), preservatives (from 0.01% to 0.5%), thickeners (from 0% to about 5%), flavoring agents (from 0.04% to 2 %), Sweetener (from 0.1% to 3%) and surfactant (from 0% to 5%). The compositions of the invention can also be used to treat periodontal diseases by topical application to the gingiva affected by the disease.

When used, the compositions of the present invention are brought into contact with the oral cavity tissue affected by periodental diseases for at least 15 seconds, preferably from about 20 seconds to about 10 minutes, in an embodiment from about 30 seconds to about 60 seconds .

The following examples serve to illustrate the compositions of the present invention.

Experiments

example 1

Example of a typical composition as a toothpaste according to the invention would be:

Example 2

Examples of typical compositions as a mouthwash according to the invention would be:

Example 3 - Subject Evaluation of Bitterness

15 test persons were given the toothpaste with different proportions of the bitter blocker, with otherwise the same composition. The test persons were asked after the usual use of the toothpaste to rate the bitterness of the toothpaste on a scale between 1 (= lowest possible bitterness) and 10 (= highest possible bitterness) and the mean value was determined from this.

It can be clearly seen that even with 0.4% by weight of the bitter blocker, a significant improvement in bitterness is brought about and the best results are achieved with 5%. With proportions of the bitter blocker of more than 8%, more than 9% or more than 10%, a "furry" taste appeared, which should be avoided.

The present invention relates to a composition for an oral hygiene agent, comprising: caffeine and at least one bitter blocker which contains L-lysine.

The composition of claim 1 wherein the bitter blocker is between 1% L-lysine hydrochloride and 99% maltodextrin; and contains 15% L-lysine hydrochloride and 85% maltodextrin. In one embodiment, the bitter blocker contained in the aforementioned composition consists of 8% L-lysine hydrochloride and 92% maltodextrin.

In one embodiment, the concentration of caffeine per serving is

Oral hygiene agent of the aforementioned composition between 50 and 200mg.

In one embodiment, the concentration of caffeine per serving is

Oral hygiene agent of the aforementioned composition at about 100mg.

In one embodiment, the proportion by weight of the caffeine is

Total composition by weight 13% and the proportion by weight of the bitter blocker 5%.

In one embodiment, the caffeine comes from one or more caffeine sources selected from the group comprising coffee (Coffea), guarana (Paullinia cupana), mate (Ilex paraguariensis), tea (Camellia sinensis), kola nut (Cola) and / or cocoa (Theobroma cacao).

In one embodiment, the bitter blocker carrier is maltodextrin.

In one embodiment, the composition contains one or more ingredients selected from the group comprising dental abrasives, alcohol, surface-active agents, thickeners, humectants, colorants, flavorings, sweeteners and / or water.

In one embodiment, the composition also contains water, sodium fluoride, zinc chloride, sodium saccharin, at least one dye, sodium gluconate, sorbitol solution, sodium carboxymethyl cellulose, at least one silica-based abrasive, at least one oil, at least one flavoring, sodium C14-C16 olefin Sulfonate, and optionally at least one optical effect substance.

In a further embodiment, the composition also contains water, zinc citrate, tripotassium citrate, glycerin, sodium fluoride, sodium gluconate, sodium saccharin, at least one dye, sodium polyphosphate, propylene glycol, at least one surface-active agent, at least one flavoring substance.

In one embodiment, the composition has a pH of 6.0 to 7.0.

The present invention also extends to the use of the aforesaid oral hygiene product.

In one embodiment, the composition of a topical, oral medicament is used for the treatment and / or prevention of periodontal diseases. In one embodiment, the use of an oral hygiene agent is selected from the group comprising toothpaste, chewing toothpaste, chewing gum, tooth gel, oral spray, mouthwash and / or dental solution composition.

In one embodiment, the use of the aforementioned composition comprises that it is held in the oral cavity for a period of time and then largely spat out instead of swallowed.

Claims

Claims 1. A composition for an oral hygiene product comprising: Caffeine and at least one bitter blocker that contains L-lysine. 2. The composition of claim 1 wherein the bitter blocker is between 1% L-lysine hydrochloride and 99% maltodextrin; and contains 15% L-lysine hydrochloride and 85% maltodextrin. 3. The composition according to claim 1 or 2 wherein the bitter blocker consists of 8% L-lysine hydrochloride and 92% maltodextrin. 4. The composition according to any one of claims 1 to 3, wherein the concentration of caffeine per serving of the oral hygiene agent is between 50 and 200 mg. 5. The composition according to any one of claims 1 to 4, wherein the concentration of caffeine per serving of the oral hygiene agent is about 100 mg. 6. The composition according to any one of claims 1 to 5, wherein the The proportion by weight of the caffeine in the total composition by weight is 13% and the proportion by weight of the bitter blocker is 5%. 7. The composition according to any one of claims 1 to 6, wherein the caffeine comes from one or more caffeine sources selected from the group comprising coffee {Coffea), guarana (Paullinia cupana), mate (. Ilex paraguariensis), tea (Camellia sinensis) , Kola nut (cola) and / or cocoa (theobroma cacao). 8. The composition according to any one of claims 1 to 7, wherein the The bitter blocker carrier is maltodextrin. 9. The composition according to any one of claims 1 to 8, furthermore one or more ingredients selected from the group comprising dental abrasives, alcohol, surface-active agents, thickeners, humectants, coloring agents, flavoring agents, sweeteners and / or water. 10. A composition with the ingredients as mentioned in claims 1 to 9, as well as water, sodium fluoride, zinc chloride, sodium saccharin, at least one dye, sodium gluconate, sorbitol solution, sodium carboxymethyl cellulose, at least one silica-based abrasive, at least one oil, at least one flavoring substance, sodium C14-C16 olefin sulfonate, and optionally at least one optical effect substance. 11. A composition with the ingredients as mentioned in claims 1 to 9, as well as water, zinc citrate, tripotassium citrate, glycerol, sodium fluoride, sodium Gluconate, sodium saccharin, at least one color, sodium polyphosphate, propylene glycol, at least one surface-active agent, at least one flavoring agent. 12. The composition of any one of claims 1 to 11, wherein the composition has a pH of 6.0 to 7.0. 13. Use of the composition of a topical, oral medicament according to claims 1 to 12 for the treatment and / or prevention of periodontal diseases. 14. The use of an oral hygiene agent according to claim 13 selected from the group comprising toothpaste, chewing toothpaste, chewing gum, tooth gel, oral spray, mouthwash and / or dental solution composition. 15. The use of claim 13 or 14, wherein the composition is held in the oral cavity for a period of time and then largely spat out rather than swallowed.