Oral Care Composition
Patent Information
- Application Number
- JP2023579288
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2021-08-04
- Filing Date
- 2022-06-21
- Publication Date
- 2025-06-25
AI Technical Summary
There is a need for additional oral care compositions that can effectively reduce bacterial adhesion, biofilm formation, and disrupt biofilms to improve oral hygiene and prevent conditions such as demineralization, gingivitis, plaque, periodontitis, bad breath, and dental caries.
The development of oral care compositions containing specific compounds like myristic acid, cis-3-hexenylhexanoate, citronellol, nootkatone, and others, which are formulated to reduce bacterial adhesion, inhibit biofilm formation, and disrupt existing biofilms, with preferred concentrations ranging from 0.001% to 5% of each compound in the composition.
These compositions demonstrate statistically significant reductions in bacterial adhesion and biofilm formation, effectively preventing or treating oral pathologies by disrupting biofilms, thereby improving oral health.
Abstract
Description
[Technical field]
[0001] Introduction Oral diseases such as dental caries are highly prevalent in society. They can cause chronic and acute pain to patients and can even lead to death. Oral hygiene plays a vital role in reducing the impact of such diseases. Examples of oral hygiene include regular brushing, flossing, tongue cleaning, and of course regular visits to the dentist.
[0002] Oral care preparations, such as mouthwashes and mouth rinses, have been known for a long time and have been developed to clean and freshen the oral cavity or oral surfaces by inhibiting or killing microorganisms that cause malodour, caries, periodontal disease, gingivitis and periodontal disease.
[0003] While oral care compositions having antibacterial activity are known, there is a need in society for additional compositions to improve oral hygiene and reduce the incidence of oral disease.
[0004] Summary of the Invention The present invention relates to an extract of any of the following compounds: myristic acid, cis-3-hexenyl hexanoate, citronellol, nootkatone, ambrette seed absolute, spinach absolute, Helichrysum italicum absolute, butanol, geraniol, β-ionone, isoamyl alcohol, methyl (2-pentyl-3-oxocyclopentyl) acetate, anethole, decanoic acid, undecanoic acid, nutmeg oil, clary sage oil, lemongrass oil, lime oil, peppermint oil (e.g., mint piperita reco nat, mint piperita boulder sx, or mint piperita yakima single cut). The present invention solves the above-mentioned problems by providing an oral care composition comprising one or more of the following compounds or compositions: glyceryl stearate, glyceryl stearate, glyceryl stearate, stearate-containing sorbitol ...
[0005] One embodiment of the present invention provides an oral care composition, wherein the compound or composition is selected from myristic acid, cis-3-hexenyl hexanoate, citronellol, nootkatone, ambrette seed absolute, spinach absolute, Helichrysum italicum absolute, butanol, geraniol, β-ionone, isoamyl alcohol, methyl (2-pentyl-3-oxocyclopentyl) acetate, nutmeg oil, clary sage oil, lemongrass oil, peppermint oil, and γ-octalactone.
[0006] One embodiment of the present invention provides an oral care composition, wherein the compound or composition is selected from myristic acid, citronellol, nootkatone, nutmeg oil, clary sage oil, lemongrass oil, peppermint oil, and gamma-octalactone.
[0007] One embodiment of the present invention provides an oral care composition, wherein the compound or composition is present in a concentration of 0.001% to 5%, particularly preferably 0.005% to 3%, preferably 0.05% to 2.5%, preferably 0.1% to 2.5%, preferably 0.5% to 2%, based on the total weight of the oral care composition.
[0008] One embodiment of the present invention provides an oral care composition further comprising one or more of the following ingredients: a flavor system, a cooling agent, a surfactant, a humectant, a pigment, an antimicrobial agent, a thickener, a fluoride source, a tartar control agent, and / or a preservative.
[0009] One embodiment of the present invention provides an oral care composition that is coated or encapsulated.
[0010] A further aspect of the present invention provides an oral care product, or a nutritional or cooling product, comprising the oral care composition of the present invention.
[0011] In one embodiment of the invention, the oral care product is selected from the group consisting of toothpaste, tooth powder, tooth gel, liquid toothpaste, foam toothpaste, toothpaste tablets, mouthwash, mouth rinse, mouth spray, dental floss, chewing gum, dental aligners, lozenges, denture effervescent tablets; denture effervescent tablets and dental aligners.
[0012] A further aspect of the present invention provides a method for treating or preventing demineralization due to erosion, gingivitis, plaque, periodontitis, halitosis and / or dental caries comprising applying a composition according to any one of the preceding claims to the oral cavity of a person in need thereof.
[0013] A further aspect of the present invention provides the use of an oral care composition of the present invention for treating or preventing demineralization due to tooth erosion, gingivitis, plaque, periodontitis, halitosis, and / or dental caries.
[0014] A further aspect of the invention is a method for identifying a test composition having use in oral health care comprising the steps of: (a) assessing whether a test composition reduces bacterial adhesion; and / or (b) assessing whether the test composition reduces biofilm formation; and / or (c) assessing whether the test composition disrupts the biofilm; Including, Compositions that score positive in one or more of the evaluations are useful as oral health care compositions. A method is provided.
[0015] In one embodiment of the method of identifying a test composition, evaluating step (a) comprises exposing the substrate to saliva and / or bacteria, with or without the addition of the test composition, to determine whether the test composition reduces adhesion of bacteria to the substrate.
[0016] In one embodiment of the method of identifying a test composition, the evaluating in step (b) comprises exposing the substrate to saliva and / or bacteria under culture conditions for at least 24 hours and then exposing the cultured mixture to the test composition to determine whether the test composition reduces biofilm formation on the substrate.
[0017] In one embodiment of the method of identifying a test composition, evaluating in step (c) comprises exposing the substrate to saliva and / or bacteria under culture conditions for at least 72 hours to form a biofilm on the substrate, and then exposing the cultured mixture to the test composition to determine whether the test composition disrupts the biofilm.
[0018] In one embodiment of the method for identifying a test composition, the effect of the test composition on a biofilm is determined by harvesting the biofilm and identifying the amount and type of bacteria present in the biofilm.
[0019] One embodiment of the method for identifying a test composition further comprises preparing an oral care composition using the test composition that is positive in one or more of the evaluations. [Brief description of the drawings]
[0020] [Figure 1] FIG. 1 shows the change in plaque index between sampling time points and the bacterial load of used mouthrinse on day 7.
[0021] Detailed Description of the Invention Oral biofilm is a well-known term in the art. Oral biofilm is a community of microorganisms and their products embedded in a matrix that adheres to soft tissues in the mouth, such as tooth enamel and tongue. The cooperative nature of the microbial community in the biofilm provides advantages to the bacteria present therein, promoting growth in a wider range of habitats, and providing higher resistance to host defenses and antimicrobial agents, which in turn increases the pathogenicity of the microbial community.
[0022] Oral biofilms are commonly found in the clean mouth, however, biofilms can cause oral pathologies such as erosive demineralization, gingivitis, plaque, periodontitis, halitosis and / or dental caries.
[0023] Mechanically disrupting biofilms with brushing or dental flossing can remove some of the pathogenic microorganisms and aid in oral hygiene, but biofilms can rapidly regenerate. Thus, there is a need to identify compounds and compositions that can be used alone or in combination with mechanical disruption to retard the formation of oral biofilms.
[0024] The present inventors have sought to identify compounds or compositions that can be used in oral care compositions to improve oral hygiene.
[0025] The inventors have devised a method for identifying whether a test compound or composition can be utilized in an oral care composition, comprising: (a) assessing whether the test composition reduces bacterial adhesion; and / or (b) assessing whether the test composition reduces biofilm formation; and / or (c) assessing whether the test composition disrupts biofilms, wherein a composition testing positive in one or more of the assessments is useful as an oral health care composition.
[0026] Further information regarding the performance of the evaluation is provided by the accompanying examples and is further explained below.
[0027] From this study, the inventors have found that myristic acid, cis-3-hexenyl hexanoate, citronellol, nootkatone, ambrette seed absolute, spinach absolute, Helichrysum italicum absolute, butanol, geraniol, β-ionone, isoamyl alcohol, methyl (2-pentyl-3-oxocyclopentyl) acetate, anethole, decanoic acid, undecanoic acid, nutmeg oil, clary sage oil, lemongrass oil, lime oil, peppermint oil, and oleaginous acid are all effective in treating chronic conditions. A number of compounds or compositions have been identified that modulate bacterial adhesion, and / or biofilm formation, and / or biofilm disruption, including mint oil (e.g., mint piperita reconat, mint piperita boulder sx, or mint piperita yakimasu single cut), γ-octalactone, 3-hexenyl acetate, lavender oil, cinnamaldehyde, clove oil, arvensis mint oil (e.g., arvensis mint tpc), linseed oil, and thymol.
[0028] Thus, the present invention provides oral care compositions comprising one or more of the compounds or compositions referred to herein that have an anti-oral biofilm effect, i.e., reduce bacterial adhesion and / or reduce biofilm formation and / or disrupt biofilm, and are therefore useful for the prevention or treatment of oral pathologies such as erosive demineralization, gingivitis, plaque, periodontitis, halitosis, and / or dental caries.
[0029] "Reduce" includes cases where the compound or composition exhibits a positive result in one or more of the assays used in the embodiments of the invention described herein. By "positive result," we mean that the composition confers a statistically significant effect, i.e., a reduction effect, compared to a control reaction using the same sample mixture, but without the test compound or composition.
[0030] As used herein, "statistically significant effect" refers to a compound or composition having a p-value (i.e., 95% confidence interval) of less than 0.05 as measured by Student's T-test.Of course, such a reduction is considered beneficial for reducing the possibility that a subject will develop such oral lesions.
[0031] In one embodiment of the invention, the oral care product is selected from the group consisting of toothpaste, tooth powder, tooth gel, liquid toothpaste, foam toothpaste, toothpaste tablets, mouthwash, mouth rinse, mouth spray, dental floss, chewing gum, dental aligners, lozenges, denture effervescent tablets; denture effervescent tablets and dental aligners.
[0032] The term "oral health care composition" as used herein refers to a product that, in the normal course of use, is not intentionally swallowed for the purpose of systemic administration of a particular therapeutic agent, but rather is retained in the oral cavity for a time sufficient to contact substantially all of the dental surfaces and / or oral tissues for the purpose of acting within the oral cavity. Oral health care compositions may be in a variety of forms, such as toothpaste, tooth powder, tooth gel, liquid toothpaste, foam toothpaste, tablet toothpaste, mouthwash, mouth rinse, mouth spray, dental floss, chewing gum, dental aligners, lozenges, effervescent tablets for dentures; effervescent tablets for dentures and dental aligners.
[0033] The oral health care compositions may be incorporated onto floss, strips, or films, or incorporated into devices or applicators, such as toothbrushes, dental aligners, or roll-ons, for direct application or attachment to oral surfaces. Such applicators may be for single or multiple use.
[0034] The term "dentifrice" as used herein, unless otherwise specified, may be a paste, gel, or liquid formulation. The dentifrice composition may be a single phase composition or a combination of two or more separate dentifrice compositions. The dentifrice composition may be in any desired form, such as deep striped, surface striped, multi-layered, a paste surrounded by a gel, or any combination thereof. Each of the dentifrice compositions of a dentifrice comprising two or more separate dentifrice compositions may be contained in physically separate compartments of a dispenser and dispensed side-by-side.
[0035] As used herein, the term "dispenser" refers to any pump, tube, or container suitable for dispensing a composition such as a dentifrice.
[0036] As noted above, the inventors have identified a number of compounds or compositions that can be used in oral health care compositions.
[0037] One embodiment of the present invention is a combination of myristic acid, cis-3-hexenyl hexanoate, citronellol, nootkatone, ambrette seed absolute, spinach absolute, Helichrysum italicum absolute, butanol, geraniol, β-ionone, isoamyl alcohol, methyl (2-pentyl-3-oxocyclopentyl) acetate, anethole, decanoic acid, undecanoic acid, nutmeg oil, clary sage oil, lemon Provided is an oral care composition comprising one or more of the following compounds or compositions: grass oil, lime oil, peppermint oil (e.g., mint piperita reconat, mint piperita boulder sx, or mint piperita yakimasu single cut), gamma-octalactone, 3-hexenyl acetate, lavender oil, cinnamaldehyde, clove oil, arvensis mint oil (e.g., arvensis mint tpc), linseed oil, and thymol.
[0038] The compounds or compositions used in the oral care compositions of the present invention are discussed below.
[0039] "Myristic acid" is a material well known in the art. It is found in nutmeg butter. "Myristic acid" includes materials registered under CAS 544-63-8 and is commercially available from a number of sources.
[0040] "Cis-3-hexenyl hexanoate" is a material well known in the art, has a fruity green pear scent, and is used in fragrances. "Cis-3-hexenyl hexanoate" includes materials registered under CAS 31501-11-8, and is commercially available from a number of sources.
[0041] "Citronellol" is a material well known in the art. It has a fresh floral rose note and is used in perfumery. "Citronellol" includes materials registered under CAS000106-22-9 and is commercially available from a number of sources.
[0042] "Nootkatone" is a material well known in the art. It is a flavoring agent best known for being present in grapefruit. "Nootkatone" includes materials registered under CAS004674-50-4 and is commercially available from a number of sources.
[0043] "Ambrette seed absolute" is a material well known in the art, used in perfumery, and has a dry, musky odor. "Ambrette seed absolute" includes materials registered under CAS 8015-62-1, and is commercially available from a number of sources.
[0044] "Spinach absolute" is a material well known in the art that is used in perfumery and has a spinach-like aroma profile. "Spinach absolute" includes materials registered under CAS 68917-48-6 and is commercially available from a number of sources.
[0045] "Helichrysum italicum absolute" is a material well known in the art, used in perfumery, and has a floral amber note. "Helichrysum italicum absolute" includes materials registered under CAS0008023-95-8, and is commercially available from a number of sources.
[0046] "Butanol" is a material well known in the art that can be used as a perfume base and also has an alcohol-like odor. "Butanol" includes materials registered under CAS 71-36-3 and is commercially available from a number of sources.
[0047] "Geraniol" is a material well known in the art. It has a rose-like scent, a common characteristic of many essential oils, and is used in perfumes and flavors. "Geraniol" includes materials registered under CAS 106-24-1 and is commercially available from a number of sources.
[0048] "β-ionone" (having the chemical formula: (3E)-4-(2,6,6-trimethylcyclohex-1-en-1-yl)but-3-en-2-one) is a material well known in the art. It has a rose-like odor, a common characteristic of many essential oils, and is used in perfumes and flavors. "β-ionone" includes materials registered under CAS 79-77-6 and is commercially available from a number of sources.
[0049] "Isoamyl alcohol" is a material well known in the art. It has a fruity, banana-like odor and is used in perfumes and flavors. "Isoamyl alcohol" includes materials registered under CAS 123-51-3 and is commercially available from a number of sources.
[0050] "Methyl (2-pentyl-3-oxocyclopentyl) acetate" is a compound used in fragrances. It has a floral jasmine note with citrus freshness. "Methyl (2-pentyl-3-oxocyclopentyl) acetate" includes materials registered under CAS0024851-98-7, available from Firmenich SA (www.firmenich.com).
[0051] "Anethole" is a material well known in the art. It is used in perfumery and has a sweet licorice-like odor. "Anethole" includes materials registered under CAS004180-23-8 and is commercially available from a number of sources.
[0052] "Decanoic acid" is a material well known in the art. It is used in perfumery and has a sweet licorice-like odor. "Decanoic acid" includes materials registered under CAS 334-48-5 and is commercially available from a number of sources.
[0053] "Undecanoic acid" is a material well known in the art. It is used in flavorings and has a waxy, creamy cheese-like odor. "Undecanoic acid" includes materials registered under CAS 112-37-8 and is commercially available from a number of sources.
[0054] "Nutmeg oil" is a material well known in the art. It is used in perfumery and has a spicy, woody odor. "Nutmeg oil" includes materials registered under CAS 8008-45-5 and is commercially available from a number of sources.
[0055] "Clary sage oil" is a material well known in the art. It is used in perfumery and has a fresh herbal tea-like odor. Examples of "clary sage oil" include materials registered under CAS8016-63-5.
[0056] "Lemongrass oil" is a material well known in the art. It is a complex oil containing several compounds such as citral, myrcene, and limonene, and is prepared from the leaves and stems of the lemongrass (Cymbopogon citratus plant). The oil is commonly used for cooking and health purposes. "Lemongrass oil" includes materials registered under CAS8007-02-1 and is commercially available from a number of sources.
[0057] "Lime oil" is a material well known in the art. It is a complex oil containing several compounds, such as limonene, gamma-terpinene, and beta-pinene, and is prepared from the Mexican lime (Citrus aurantifolia plant). "Lime oil" includes materials registered under CAS 8008-26-2 and is commercially available from a number of sources.
[0058] "Peppermint oil" is a material well known in the art. It is a complex oil containing several compounds such as menthol, menthone, and cineole, and is prepared from the leaves and stems of the peppermint (Mentha x piperita plant). This oil is commonly used for cooking and health purposes. "Peppermint oil" includes oils obtained from a number of different varieties of plants. For example, peppermint oils known as Mint Piperita Reconat (material registered under CAS0068917-18-0), Mint Piperita Boulder sx (material registered under CAS0008006-90-4), or Mint Piperita Yakima Single Cut (material registered under CAS8006-90-4) are included within the scope of "peppermint oil" for the purposes of this application. The above "peppermint oil" is commercially available from many sources, such as Essex Laboratories (http: / / www.essexlabs.com / ).
[0059] "γ-Octalactone" is a material well known in the art. It has a sweet coconut odor and is used in the preparation of perfumes and other fragrance materials. "γ-Octalactone" includes materials registered under CAS 104-50-7 and is commercially available from a number of sources.
[0060] "3-Hexenyl acetate" is a material well known in the art. It has a green, fruity odor and is used in the preparation of perfumes and other fragrance materials. "3-Hexenyl acetate" includes materials registered under CAS 1708-82-3 and is commercially available from a number of sources.
[0061] "Lavender oil" is a material well known in the art. It is a complex oil containing several compounds such as linalool and linalyl acetate, and is prepared from lavender species, most commonly true lavender (Lavandula angustifolia) and spike lavender (Lavandula latifolia). Lavender oil has been used for fragrance purposes since ancient times. "Lavender oil" includes materials registered under CAS8008-28-0 and is commercially available from many sources.
[0062] "Cinnamaldehyde" is a material well known in the art. It has a cinnamon-like odor and is used in perfumes and flavors. "Cinnamaldehyde" includes materials registered under CAS 14371-10-9 and is commercially available from a number of sources.
[0063] "Clove oil" is a material well known in the art. It is a complex oil containing several compounds such as eugenol, eugenyl acetate, and caryophyllene, and is prepared from the Syzygium aromaticum plant. Clove oil has been used for flavoring and medicinal purposes since ancient times. "Clove oil" includes materials registered under CAS8008-34-8 and is commercially available from a number of sources.
[0064] "Arvensis mint oil" is a material well known in the art. It is a menthol mint oil, like peppermint, containing several compounds such as menthol and menthone, and is prepared from Menthe arvensis. Arvensis mint oil has been used for fragrance and flavor purposes since ancient times. "Arvensis mint oil" includes materials registered under CAS 68917-18-0 and is commercially available from many sources, such as Sharp Mint Ltd (http: / / www.sharpmint.com / ) and Swati Menthol Allied (http: / / swatimenthol.com / ).
[0065] "Linseed oil" is a material well known in the art. It is a complex oil containing several compounds such as linolenic acid, palmitic acid, and stearic acid, and is prepared from flax (Linum usitatissimum). Linseed oil has been used for industrial purposes since ancient times. "Linseed oil" includes materials registered under CAS 60-33-3 and is commercially available from many sources. In a preferred embodiment, the linseed oil comprises a mixture of the linoleic acid isomers (Z,Z)-9,12-octadecadienoic acid and (Z,Z,Z)-9,12,15-octadecatrienoic acid.
[0066] "Thymol" is a material well known in the art. It is used for flavoring and medicinal purposes. "Thymol" includes materials registered under CAS 89-83-8 and is commercially available from a number of sources.
[0067] The oral care composition of the present invention preferably comprises one or more compounds or compositions that show positive results in two or more of the evaluations used in the aspects of the present invention described herein.Accordingly, in a further embodiment of the present invention, the oral care composition comprises myristic acid, cis-3-hexenylhexanoate, citronellol, nootkatone, ambrette seed absolute, spinach absolute, Helichrysum italicum absolute, butanol, geraniol, β-ionone, isoamyl alcohol, methyl (2-pentyl-3-oxocyclopentyl) acetate, anethole, decanoic acid, undecanoic acid, The compounds or compositions include one or more of the following: nutmeg oil, clary sage oil, lemongrass oil, lime oil, peppermint oil (e.g., mint piperita reconatto, mint piperita boulder sx, or mint piperita yakima single cut), gamma-octalactone, 3-hexenyl acetate, lavender oil, cinnamaldehyde, clove oil, arvensis mint oil (e.g., arvensis mint tpc), linseed oil, and thymol.
[0068] More preferably, the oral care composition of the present invention comprises one or more compounds or compositions that show positive results in all three evaluations used in the aspects of the present invention described herein.Thus, in a further embodiment of the present invention, the oral care composition comprises one or more of the compounds or compositions that are myristic acid, citronellol, nootkatone, nutmeg oil, clary sage oil, lemongrass oil, peppermint oil and gamma-octalactone.
[0069] As mentioned above, the oral care composition of the present invention comprises one or more of the compounds or compositions described herein. In one embodiment of the present invention, the oral care composition of the present invention comprises myristic acid, cis-3-hexenyl hexanoate, citronellol, nootkatone, ambrette seed absolute, spinach absolute, Helichrysum italicum absolute, butanol, geraniol, β-ionone, isoamyl alcohol, methyl (2-pentyl-3-oxocyclopentyl) acetate, anethole, decanoic acid, undecanoic acid, nutmeg oil, clary sage oil, lemongrass oil, lime juice, citronellol, nootkatone, ambrette seed absolute, spinach absolute, helichrysum italicum absolute, butanol, geraniol, β-ionone, isoamyl alcohol, methyl (2-pentyl-3-oxocyclopentyl) acetate, anethole, decanoic acid, undecanoic acid, nutmeg oil, clary sage oil, lemongrass oil, lime juice, citronellol, nootkatone ... oil, peppermint oil (e.g., mint piperita reconat, mint piperita boulder sx, or mint piperita yakimasu single cut), gamma octalactone, 3-hexenyl acetate, lavender oil, cinnamaldehyde, clove oil, arvensis mint oil (e.g., arvensis mint tpc), linseed oil, and thymol.
[0070] As shown in the accompanying examples, the present inventors have prepared a series of oral care compositions comprising combinations of compounds or compositions described herein, which are referred to as "Flavor Compositions A-D." The series of oral care compositions have shown good anti-biofilm activity in vitro and in vivo.
[0071] Thus, in a preferred embodiment, the oral care composition of the present invention comprises isoamyl alcohol, linseed oil, and methyl(2-pentyl-3-oxocyclopentyl).Preferably, the oral care composition of the present invention comprises 10% isoamyl alcohol, 10% linseed oil, and 2.5% methyl(2-pentyl-3-oxocyclopentyl).
[0072] In a further preferred embodiment, the oral care composition of the present invention comprises mint arvensis tpc and mint piperita yakima single cut.Preferably, the oral care composition of the present invention comprises 16.67% mint arvensis tpc and 16.67% mint piperita yakima single cut.
[0073] In a further preferred embodiment, the oral care composition of the present invention comprises cinnamaldehyde and clove oil.Preferably, the oral care composition of the present invention comprises 15% cinnamaldehyde and 15% clove oil.
[0074] Of course, the amount of the compound or composition can vary depending on the particular compound or composition and the formulation and intended use.
[0075] However, an embodiment of the present invention provides an oral care composition of the present invention, wherein the compound or composition is present at a concentration of from 0.001% to 5%, particularly preferably from 0.005% to 3%, and preferably from 0.5% to 2%, respectively, based on the total weight of the oral care composition.
[0076] One embodiment of the present invention provides an oral care composition of the present invention further comprising one or more of the following ingredients: a flavor system, a cooling agent, a surfactant, a humectant, a pigment, an antimicrobial agent, a thickener, a fluoride source, a tartar control agent, and / or a preservative.
[0077] In some embodiments, the composition further comprises a flavor system. The flavor system can mask any unpleasant taste and sensation caused by a given ingredient contained in the composition, such as antibacterial actives or peroxides. Without intending to be limited to a particular theory, a pleasant-tasting composition improves user compliance with the prescribed or recommended use of oral care products. The flavor system may comprise conventional flavor ingredients, particularly flavor ingredients that are relatively stable in the presence of carrier materials or excipients of conventional oral care products. The combination of the selected flavor system with the composition presented herein can provide a high-impact refreshing sensation with a balanced flavor profile.
[0078] In some embodiments, the flavor system comprises oil of wintergreen, cassia, sage, parsley oil, marjoram, orange, cis-jasmone, 2,5-dimethyl-4-hydroxy-3(2H)-furanone, 5-ethyl-3-hydroxy-4-methyl-2(5H)-furanone, vanillin, ethyl vanillin, anisaldehyde, 3,4-methylenedioxybenzaldehyde, 3,4-dimethoxybenzaldehyde, 4-hydroxybenzaldehyde, 2-methoxybenzaldehyde, benzaldehyde, propenylguaethol, heliotropin, 4-cis-heptenal, diacetyl, methyl-p-tert-butyl In some embodiments, the flavor components may contain additional flavor ingredients such as, but not limited to, phenyl acetate, methyl salicylate, ethyl salicylate, L-menthyl acetate, oxanone, α-irisone, ethyl butyrate, ethyl acetate, methyl anthranilate, isoamyl acetate, isoamyl butyrate, allyl caproate, eugenol, eucalyptol, octanol, octanal, decanol, decanal, phenylethyl alcohol, benzyl alcohol, α-terpineol, maltol, ethyl maltol, anethole, dihydroanethole, carvone, menthone, b-damascenone, and mixtures thereof.
[0079] Generally, suitable flavoring ingredients include structural features and functional groups that are not prone to redox reactions. These include derivatives of flavor chemicals that contain saturated or stable aromatic rings or ester groups. Also suitable are flavor chemicals that undergo some degree of oxidation or decomposition without significant changes in flavor characteristics or profile. The flavoring ingredients are provided in the composition as single or purified chemicals, or by adding natural oils or extracts. The natural oils or extracts are preferably refined to remove components that are relatively unstable and that may degrade or alter the desired flavor profile, resulting in a product that is unacceptable from an organoleptic perspective. Flavoring agents can generally be used in the composition at levels of about 0.001% to about 5% by weight of the composition.
[0080] In some embodiments, the flavor system may further comprise a sweetener.Suitable sweeteners include those well known in the art, including both natural and artificial sweeteners.Suitable water-soluble sweeteners include monosaccharides, disaccharides, and polysaccharides, such as xylose, xylitol, ribose, glucose (dextrose), mannose, galactose, fructose (levulose), sucrose (sugar), maltose, invert sugar (a mixture of fructose and glucose derived from sucrose), partially hydrolyzed starch, corn syrup solids, dihydrochalcones, monellin, stevioside, and glycyrrhizin.Monk fruit-derived sweeteners include mogrosides.Stevia rebaudiana-derived sweeteners also include stevioside and rebaudioside (especially rebaudioside A). Suitable water-soluble artificial sweeteners include soluble saccharin salts, i.e., sodium or calcium saccharin salts, cyclamate salts, the sodium, ammonium or calcium salt of 3,4-dihydro-6-methyl-1,2,3-oxathiazin-4-one-2,2-dioxide, the potassium salt of 3,4-dihydro-6-methyl-1,2,3-oxathiazin-4-one-2,2-dioxide (acesulfame-K), the free acid form of saccharin, and the like. Other suitable sweeteners include dipeptide-based sweeteners, such as those derived from L-aspartic acid, e.g., L-aspartyl-L-phenylalanine methyl ester (aspartame), and the materials described in U.S. Pat. No. 3,492,131, L-α-aspartyl-N-(2,2,4,4-tetramethyl-3-thietanyl)-D-alaninamide hydrate, the methyl ester of L-aspartyl-L-phenylglycerin and L-aspartyl-L-2,5,dihydrophenyl-glycine, L-aspartyl-2,5-dihydro-L-phenylalanine, L-aspartyl-L-(1-cyclohexylene)-alanine, and the like.Water-soluble sweeteners derived from naturally occurring water-soluble sweeteners can be used, such as chlorinated derivatives of normal sugars (sucrose), known, for example, under the trade name sucralose, as well as sweeteners derived from proteins such as Thaumatoccous daniellii (thaumatins I and II).
[0081] In some embodiments, the composition may comprise from about 0.1% to about 10%, alternatively from about 0.1% to about 1%, of a sweetener, by weight of the composition.
[0082] In some embodiments, the flavor system may further include salivating agents, warming agents, and numbing agents, which may be present in the composition at levels of from about 0.001% to about 10%, or alternatively from about 0.1% to about 1%, by weight of the composition.
[0083] Suitable salivating agents include Jambu® manufactured by Takasago Co., Ltd. Suitable numbing agents include benzocaine, lidocaine, clove bud oil, and ethanol. Examples of warming agents include ethanol, capsicum, and nicotinic acid esters such as benzyl nicotinate.
[0084] In some embodiments, the oral care compositions of the present invention may further comprise a cooling agent, such as those described in U.S. Patents 9,394,287 and 9,732,071. Additional examples of cooling agents include 5-methyl-2-(propan-2-yl)cyclohexyl-N-ethyloxamate, N-ethyl-p-menthanecarboxamide (WS-3, also known as menthane-3-carboxylic acid-N-ethylamide), N-2,3-trimethyl-2-isopropylbutanamide (WS-23), menthyl lactate (Frescolat®-ML), menthone glycerin acetal (Frescolat®), and the like. MGA), monomenthyl succinate (Physcool®), monomenthyl glutarate, O-menthyl-glycerin, menthyl-N,N-dimethylsuccinamate, N-(4-cyanomethylphenyl)-p-menthanecarboxamide, N-(2-(pyridin-2-yl)ethyl)-3-p-menthanecarboxamide, menthol and menthol derivatives (e.g., L-menthol, D-menthol, racemic menthol, isomenthol, neoisomenthol, neomenthol), menthyl ethers (e.g., (L-menthoxy)-1,2-propanediol, (L-menthoxy)-2-methyl-1,2-propanediol, 1-menthyl-methyl ether), menthyl esters (e.g., menthyl formate, menthyl acetate, menthyl isobutyrate, menthyl lactate, L-menthyl-L-lactic acid, L-menthyl-D-lactic acid, menthyl-(2-methoxy)acetate, menthyl (2-methoxyethoxy)acetate, menthyl pyroglutamate), N-(4-cyanomenthylphenyl)-p-menthanecarboxamide, N-(2-(pyridin-2-yl)ethyl)-3-p-menthanecarboxamide, menthyl carbonate (e.g., menthyl propylene glycol carbonate, menthyl ethylene glycol carbonate, menthyl glycerin carbonate, or mixtures thereof), menthane carboxylic acid amides (e.g., menthane carboxylic acid-N-ethylamide [WS3], N-α-(menthane-carbonyl)glycine ethyl ester [WS5], menthane carboxylic acid-N-(4-cyanophenyl)amide, menthane carboxylic acid-N-(alkoxyalkyl)amides), menthone and menthone derivatives (e.g., L-menthone glycerin ketal), 2,3-dimethyl- 2-(2-propyl)-butyric acid derivatives (e.g., 2,3-dimethyl-2-(2-propyl)-butyric acid-N-methylamide [WS23]), isopulegol or its esters (1-(-)-isopulegol, 1-(-)-isopulegol acetate), menthane derivatives (e.g., p-menthane-3,8-diol), N-(4-cyanomethylphenyl)-p-menthanecarboxamide, N-(2-(pyridin-2-yl)ethyl)-3-p-menthanecarboxamide, cubebol or synthetic or natural mixtures containing cubebol, cyclohexane, Pyrrolidone derivatives of alkyldione derivatives (e.g. 3-methyl-2(1-pyrrolidinyl)-2-cyclopenten-1-one) or tetrahydropyrimidin-2-ones (e.g. icilin or related compounds described in WO 2004 / 026840), N-(4-cyanomethylphenyl)-p-menthanecarboxamide, N-(2-(pyridin-2-yl)ethyl)-3-p-menthanecarboxamide, menthyl ethers (e.g. (L-menthoxy)-1,2-propanediol, (L-menthoxy)-2-methyl-1,2-propanediol), more polar menthyl esters (e.g., menthyl lactate, L-menthyl-L-lactic acid, L-menthyl-D-lactic acid, menthyl (2-methoxy)acetate, menthyl (2-methoxyethoxy)acetate, menthyl pyroglutamate), menthyl carbonates (e.g., menthyl propylene glycol carbonate, menthyl ethylene glycol carbonate, menthyl glycerin carbonate), semiesters of menthol with dicarboxylic acids or their derivatives (e.g., monomenthyl succinate, monomenthyl glutarate, monomenthyl malonate, O-menthyl succinate-N,N-(di)- methyl)amide, O-menthyl succinic acid ester amide), 3,4-methylenedioxycinnamic acid-N-cyclohexyl-N-2-pyridylamide, isopropyl-(5-methoxy-2-pyridin-2-yl-pyrimidin-4-yl)-amine, 3,4,6,7,11b,12-hexahydro-3,3-dimethyl-spiro[13H-dibenzo[a,f]quinolizine-1--3,2'-[1,3]dithiolane]-1(2H)-one, 5,6,10b,11-tetrahydro-3-methyl-spiro[12H-benzo[a]furo[3,4-f]quinolizine-1--2,2'-[1,3]dithiolane]-1(3H)-one. Most preferred cooling compounds are 5-methyl-2-(propan-2-yl)cyclohexyl-N-ethyloxamate, N-ethyl-p-menthanecarboxamide (WS-3, also called menthane-3-carboxylic acid-N-ethylamide), menthyl lactate (Frescolat® ML), menthone glycerin acetal (Frescolat® MGA), N-(4-cyanomethylphenyl)-p-menthanecarboxamide, and (L-menthoxy)-1,The compound is selected from the group consisting of 2-propanediol, 2-(4-methylphenoxy)-N-(1H-pyrazol-5-yl)-N-(2-thienylmethyl)acetamide, 2-(4-methylphenoxy)-N-(1H-pyrazol-3-yl)-N-(2-thienylmethyl)acetamide, and a mixture of 2-(4-methylphenoxy)-N-(1H-pyrazol-5-yl)-N-(2-thienylmethyl)acetamide and 2-(4-methylphenoxy)-N-(1H-pyrazol-3-yl)-N-(2-thienylmethyl)acetamide.
[0085] In addition to the above components, the compositions of the present invention may contain further optional ingredients and / or orally ingestible carrier materials.
[0086] In some embodiments, the oral care composition comprises a surfactant component.
[0087] Any orally ingestible surfactant (most of which are anionic, nonionic or amphoteric) can be used. Suitable anionic surfactants include, but are not limited to, sodium lauryl sulfate, sodium coconut monoglyceride sulfonate, sodium lauryl sarcosinate, sodium lauryl isethionate, sodium laureth carboxylate, and sodium dodecylbenzenesulfonate. Suitable nonionic surfactants include poloxamers, polyoxyethylene sorbitan esters, fatty alcohol ethoxylates, alkylphenol ethoxylates, tertiary amine oxides, tertiary phosphine oxides, dialkyl sulfoxides, etc. Suitable amphoteric surfactants include derivatives of Cs2O aliphatic secondary and tertiary amines with anionic groups such as carboxylates, sulfates, sulfonates, phosphates or phosphonates.
[0088] In some embodiments, the surfactant component comprises (i) a surfactant selected from the group consisting of poly(oxyethylene)-poly(oxypropylene)-poly(oxyethylene) block copolymers, poly(oxyethylene) modified hydrogenated castor oil, and poly(oxyethylene) modified fatty acid monoesters of sorbitan, and (ii) a surfactant selected from the group consisting of polyol esters and sugar esters.
[0089] In some embodiments, the oral care composition includes a pigment. Suitable orally ingestible pigments can include talc, mica, magnesium carbonate, calcium carbonate, magnesium silicate, magnesium aluminum silicate, silica, titanium dioxide, zinc oxide, red, yellow, brown and black iron oxide, ferric iron oxide, manganese violet, ultramarine, titanated mica, bismuth oxide chloride, and the like.
[0090] In some embodiments, the oral care composition comprises a fluoride ion source. Suitable fluoride ion sources include stannous fluoride, sodium fluoride, potassium fluoride, potassium monofluorophosphate, sodium monofluorophosphate, ammonium monofluorophosphate, sodium fluorosilicate, ammonium fluorosilicate, amine fluorides, ammonium fluoride, and combinations thereof.
[0091] In some embodiments, the oral care composition comprises an antibacterial agent. Suitable antibacterial agents include ethanol, triclosan, cetylpyridinium chloride (CPC), chlorhexidine (CHX), isopropyl methylphenol (IPMP), zinc sulfate (ZnSO4), zinc citrate, zinc chloride (ZnCl2).
[0092] An embodiment of the present invention provides oral care compositions of the present invention that are coated or encapsulated.
[0093] Various methods are known in the art for producing oral care compositions in which one or more ingredients are coated or encapsulated with powder-coated dissolvable film fragments, for example, a film matrix containing a water-insoluble active agent.
[0094] A further aspect of the present invention provides an oral care product, or a nutritional or cooling product, comprising the oral care composition of the present invention.
[0095] In some embodiments, the oral care composition comprises a moisturizer component.Examples of moisturizers include propylene glycol, hexylene glycol, butylene glycol, aloe vera gel, alpha hydroxy acids such as lactic acid, egg yolk and egg white, glyceryl triacetate, honey, lithium chloride, molasses, polymeric polyols such as polydextrose, quillaja, sodium hexametaphosphate E452i, sugar alcohols (sugar polyols) such as glycerol, sorbitol, xylitol, maltitol, urea, and castor.
[0096] A further aspect of the invention provides one or more of the following compounds or compositions: lemongrass oil, lime oil, peppermint oil (e.g., mint piperita reconat, mint piperita boulder sx, or mint piperita yakimasu single cut), γ-octalactone, 3-hexenyl acetate, butanol, geraniol, lavender oil, β-ionone, isoamyl alcohol, cinnamaldehyde, clove oil, arvensis mint oil (e.g., arvensis mint tpc), linseed oil, methyl (2-pentyl-3-oxocyclopentyl) acetate, and thymol, or an oral care composition according to any of the previous aspects of the invention for use as an anti-oral biofilm agent.
[0097] A further aspect of the present invention provides a consumer food or beverage product comprising an oral care composition of the present invention.
[0098] In a preferred embodiment of a consumer food or beverage product, the oral care composition of the present invention comprises isoamyl alcohol, linseed oil, and methyl(2-pentyl-3-oxocyclopentyl).Preferably, the oral care composition of the present invention comprises 10% isoamyl alcohol, 10% linseed oil, and 2.5% methyl(2-pentyl-3-oxocyclopentyl).
[0099] In a preferred embodiment of a consumer food or beverage product, the oral care composition of the present invention comprises arvensis mint tpc and mint piperita yakima single cut.Preferably, the oral care composition of the present invention comprises 16.67% arvensis mint tpc and 16.67% mint piperita yakima single cut.
[0100] In a preferred embodiment of a consumer food or beverage product, the oral care composition of the present invention comprises cinnamaldehyde and clove oil. Preferably, the oral care composition of the present invention comprises 15% cinnamaldehyde and 15% clove oil.
[0101] "Consumer food or beverage products" includes, for example, confectioneries such as chewing gum, lozenges, hard candies, beverages such as soft drinks and flavored waters, dairy beverages and dairy products such as yogurt drinks, lactose-free yogurt, sour milk, coffee cream or whipped cream, cheese, quark, ice cream, and other frozen desserts. Also included are alcoholic and non-alcoholic beverages. Other suitable food and beverage products will be known to those skilled in the art.
[0102] A further aspect of the present invention provides a method for treating or preventing demineralization due to acid erosion, gingivitis, plaque, periodontitis, halitosis and / or dental caries comprising applying a composition according to any of the previous aspects of the present invention to the oral cavity of a person in need thereof.
[0103] A further aspect of the invention provides the use of an oral care composition according to any of the previous aspects of the invention for treating or preventing demineralisation due to tooth erosion, gingivitis, plaque, periodontitis, halitosis and / or dental caries.
[0104] "Anti-oral biofilm agent" refers to a compound or composition that prevents or treats oral lesions associated with oral biofilms. Thus, the present invention includes cases where the compounds and compositions described herein are used to prevent or treat demineralization due to erosion, gingivitis, plaque, periodontitis, halitosis, and / or dental caries.
[0105] A further aspect of the invention is a method for identifying a test composition having use in oral health care comprising the steps of: (a) assessing whether a test composition reduces bacterial adhesion; and / or (b) assessing whether the test composition reduces biofilm formation; and / or (c) assessing whether the test composition disrupts the biofilm; Including, Compositions that score positive in one or more of the evaluations are useful as oral health care compositions. A method is provided.
[0106] The methods of the present invention determine whether a test composition has oral health care utility according to one or more positive results obtained in the assays used in the embodiments of the present invention. By "positive result" we mean that the composition confers a statistically significant effect compared to a control reaction using the same sample mixture but without the test compound or composition.
[0107] The accompanying examples provide detailed descriptions of each of the evaluation methods in this method of the invention, and further information is provided below.
[0108] One evaluation is used to determine whether the test composition reduces bacterial adhesion. In carrying out this evaluation, dental enamel replacement material is used as a substrate suitable for the adhesion of oral biofilm-producing bacteria. The dental enamel replacement material is exposed to oral biofilm-producing bacteria in the presence and absence of the test composition, and after a suitable incubation time, the effect of the test composition on bacterial adhesion is determined. Thus, the reduction of oral biofilm-producing bacteria adhesion to dental enamel replacement material is beneficial in terms of reducing the formation of biofilm on teeth, and thus reducing the lesions associated with oral biofilm (as described above).
[0109] The evaluation is therefore designed to mimic the adhesion of early colonizing species of bacteria onto sterile surfaces, specifically onto dental enamel replacement materials. The evaluation is carried out with and without treatment with the test composition. This is the evaluation step (a) listed in the method of the present invention.
[0110] Thus, in one embodiment of the method for identifying a test composition, evaluating step (a) involves exposing the substrate to saliva and / or bacteria with or without the addition of the test composition and determining whether the test composition reduces adhesion of bacteria to the substrate.
[0111] Suitable dental enamel replacement materials include hydroxyapatite (HA) disks or bovine dentin and enamel. The dental enamel replacement materials are exposed to oral biofilm-generating microorganisms in the presence or absence of test compositions for a period of time, for example, 30 minutes to 24 hours, preferably 24 hours. The biofilms are then harvested and analyzed by recording the number and condition of the microorganisms.
[0112] Further evaluations are used to determine whether the test compositions reduce biofilm formation, which mimics the development of dental biofilms at an early stage, by exposing the evaluation plates with saliva-applied wells to the test compositions at various times during an incubation period, after which the number and condition of the microorganisms are recorded, thereby analyzing the effect of the test compositions on biofilm formation.
[0113] The assay plates are exposed to the test composition multiple times, preferably two exposures over a 24 hour period.
[0114] The evaluation is therefore designed to mimic the early stages of biofilm formation. Evaluation is performed with and without treatment with the test composition, and the treatment is applied as described above when the biofilm develops on the dental enamel replacement material. This is step (b) of the evaluation set forth in the method of the present invention.
[0115] Thus, in an embodiment of the method of the invention, the evaluating in step (b) comprises exposing the substrate to saliva and / or bacteria under culture conditions for at least 24 hours, then exposing the cultured mixture to a test composition, and determining whether the test composition reduces biofilm formation on the substrate.
[0116] Further evaluation is used to determine whether the test composition disrupts biofilms. This evaluation is designed to evaluate the ability of the test composition to disrupt mature biofilms. Biofilms are formed according to the formation evaluation described above. Then, once the biofilms have matured (approximately 3-7 days after the start of the culture), they are exposed to the test composition several times during the test period, after which the number and condition of the microorganisms are recorded to analyze the effect of the test composition on biofilm formation.
[0117] Therefore, this evaluation is designed to mimic mature biofilm.The evaluation is carried out with and without treatment with the test composition, and the treatment is applied after biofilm develops on dental enamel replacement material, as described above, for example at least 3 days, preferably about 7 days.This is the evaluation step (c) listed in the method of the present invention.
[0118] In one embodiment of the method of identifying a test composition, evaluating in step (c) comprises exposing the substrate to saliva and / or bacteria under culture conditions for at least 72 hours to form a biofilm on the substrate, and then exposing the cultured mixture to the test composition to determine whether the test composition disrupts the biofilm.
[0119] In a further embodiment of the method of identifying a test composition, the effect of the test composition on a biofilm is determined by harvesting the biofilm and identifying the amount and type of bacteria present in the biofilm.
[0120] A further embodiment of the method of identifying a test composition includes preparing an oral care composition using a test composition that is positive in one or more of the evaluations.
[0121] The present invention will now be described in more detail with reference to the following examples which illustrate the advantages of the present invention. EXAMPLES
[0122] Example 1: In vitro screening of flavor ingredients for anti-biofilm activity Inoculum preparation A total of 12 strains were selected based on scientific literature. Strains were grown in media recommended by the strain supplier. Cultures were adjusted to log7 CFU / mL with growth medium containing 20% glycerol. For C. matruchotii, colony culture plates were washed using growth medium containing glycerol, and the cell suspension was then vortexed and homogenized with glass beads. Aerobic and anaerobic strains were mixed and aliquoted separately. Inocula were stored at -80°C until use.
[0123] [Table 1-1] [Table 1-2]
[0124] Preparation of saliva and oral inoculum: Saliva and oral microbiota samples were collected from healthy volunteers by the saliva suction technique using methods previously described [1].
[0125] (a) Bacterial adhesion evaluation: Pegs of 96-well MBEC plates (Innovotech, Canada) were submerged in saliva to form a pellicle. Overnight cultures of A. oris, A. naeslundii, S. mitis, and S. oralis were normalized to OD = 0.1 using 0.85% NaCl and mixed in equal proportions. The plates were treated with samples for 2 min and incubated with the incubation mixture for 30 min at 37 °C and 5% CO2. The pegs of the 96-well plates were then washed three times before harvesting.
[0126] (b) Biofilm formation assessment: Saliva-coated 96-well MBEC plates were incubated with inoculum overnight anaerobically. The next day, the inoculum was replaced with modified BHI medium (BHI supplemented with 1 g / L mucin, 0.5 mg / L vitamin K, and 10 mg / L hemin). The devices were treated twice for 2 min to mimic the application of dental care products, after which the treatment solution was replaced with fresh modified BHI medium and incubation continued. Biofilms were harvested after 2 days.
[0127] (c) Biofilm destruction evaluation: Inoculation and cultivation were performed in the same manner as described in the formation evaluation, except that the cultivation time was extended to 7 days. Then, the mature biofilms were treated twice a day for 3 days as described in the formation evaluation, and then harvested.
[0128] Biofilm harvesting: To harvest attached cells, the pegs of the MBEC device were immersed in 200 μL of saline solution per well. The plates were sonicated in an ultrasonic bath to obtain cell suspensions. For attachment assessment, the suspensions were serially diluted and cultured on tryptic soy agar using Microlab STAR (Hamilton). For formation and disruption assessment, the suspensions were subjected to SYTO 9 staining using LIVE / DEAD® BacLight Bacterial Viability Kits L7012 (Thermo Fisher Scientific) according to the manufacturer's instructions.
[0129] result Table 2 lists all compounds and compositions that significantly reduced biofilm in any of the three assessments.
[0130] Table 2: Compounds and compositions that showed positive results in anti-biofilm evaluations with a defined inoculum. p-value is the statistical significance of the t-test between control and treatment bases; Δ is the difference in relative biofilm abundance between control and treatment bases. For attachment evaluation, biofilms were quantified as relative CFU relative to 100. For formation and destruction evaluation, biofilms were quantified as relative fluorescence intensity relative to 100.
[0131] [Table 2]
[0132] Example 2: In vitro studies of the anti-biofilm activity of compounds and compositions using oral inocula Flavor compositions containing the compounds and compositions listed in Table 2 were evaluated for their anti-biofilm activity using biofilms derived from oral samples taken from volunteers. Table 3 shows the flavor compositions that produced a significant reduction in biofilms in any of the three evaluations.
[0133] The flavour compositions used were as follows (all amounts expressed as percentages of the total composition): Flavor A - 10% Isoamyl alcohol, 10% Linseed oil, and 2.5% Methyl (2-pentyl-3-oxocyclopentyl) Flavor B - 16.67% Arvensis Mint tpc and 16.67% Mint Piperita Yakima Single Cut Flavor C - 25% Mint Piperita Yakima Single Cut Flavor D – 15% cinnamaldehyde, and 15% clove oil. Table 3: Flavor compositions that showed positive results in anti-biofilm evaluation using oral inoculum. p-value is the statistical significance of the t-test between control and treatment bases; Δ is the difference in relative biofilm abundance between control and treatment bases. For adhesion evaluation, biofilm was quantified as relative CFU relative to 100. For formation and destruction evaluation, biofilm was quantified as relative fluorescence intensity relative to 100.
[0134] [Table 3]
[0135] Example 3: Composition and preparation of the final product Table 4: Mouthwash composition Mouthwash samples were prepared for each of the compounds and compositions shown in Table 2, as well as for flavor mixtures AD described in Example 2.
[0136] [Table 4]
[0137] The compounds and compositions shown in Table 2 or the flavor mixtures described in Example 2 were mixed with RH40 (Component A). The remaining ingredients were mixed to prepare a master mix (Component B) and then aliquoted. Component A was slowly added to Component B with constant mixing until completely dissolved.
[0138] Example 4: Effect of mouthwash on in vivo plaque regrowth The mouthwash solution prepared in Example 3 was then used in the following experiments. Volunteers without major oral diseases were recruited. The simplified plaque index, soft debris index, and calculus index were evaluated by two dentists four times throughout the study as a measure of oral hygiene. On day 0 of the study, the subjects underwent professional dental cleaning to remove all tartar and plaque. The subjects were then asked to use 20 mL of mouthwash after cleaning and to refrain from using other dental cleaning products until their next dental examination on day 1. The subjects were then instructed to brush their teeth twice a day using a standard toothpaste (brand name: Lion Floral Mint) and to use mouthwash three times a day. On days 7 and 14, the mouthwash used at noon was collected and cultured on tryptic soy agar and Mitis salivarius agar to determine the bacterial load.
[0139] result Between day 7 and day 1, the increase in the mean plaque index in the group treated with flavor D was significantly lower compared to the control, while the bacterial load in the used mouthwash was also lower, indicating that the mouthwash improved the oral hygiene of the subjects (Figure 1).
[0140] Example 5: Further in vitro screening of anti-biofilm activity of flavour ingredients We used the above assay to screen for additional ingredients with activity in model mouthwashes (Table 5).
[0141] The compounds and compositions for activity testing shown in Table 6 were dissolved in DMSO. The remaining components of the mouthwash shown in Table 5 were mixed to make a master mix in water and then aliquoted. The DMSO solution was then added to the master mix and homogenized.
[0142] [Table 5]
[0143] Table 6: Compounds and compositions that showed positive results in anti-biofilm evaluations with a defined inoculum. p-values are the statistical significance of t-tests between control and treatment bases; Δ is the difference in relative biofilm abundance between control and treatment bases. For attachment evaluations, biofilms were quantified as relative CFU relative to 100. For formation and destruction evaluations, biofilms were quantified as relative fluorescence intensity relative to 100.
[0144] [Table 6]
Claims
1. An oral care composition comprising one or more of a compound or composition of myristic acid, cis-3-hexenyl hexanoate, citronellol, nootkatone, ambroxan absolute, spinach absolute, helichrysum italicum absolute, butanol, geraniol, β-ionone, isoamyl alcohol, methyl (2-pentyl-3-oxocyclopentyl) acetate, anethole, decanoic acid, undecanoic acid, nutmeg oil, clarissa oil, lemongrass oil, lime oil, peppermint oil (e.g., mint piperita reconaught, mint piperita boulder sx, or mint piperita yaki machine single cut), γ-octalactone, 3-hexenyl acetate, lavender oil, cinnamaldehyde, clove oil, albensis mint oil (e.g., albensis mint tpc), linseed oil, and thymol.
2. The oral care composition according to claim 1, wherein the compound or composition is selected from myristic acid, citronellol, nootkatone, nutmeg oil, clarissa oil, lemongrass oil, peppermint oil, and γ-octalactone.
3. The oral care composition according to claim 1 or 2, wherein the compound or composition is at a concentration of 0.001% to 5%, particularly preferably 0.005% to 3%, preferably 0.05% to 2.5%, preferably 0.1% to 2.5%, preferably 0.5% to 2% based on the total weight.
4. The oral care composition according to claim 1 or 2, further comprising one or more of a flavor system, a cooling agent, a surfactant, a humectant, a pigment, an antibacterial agent, a thickening agent, a fluoride source, a tartar control agent, and / or a preservative.
5. The oral care composition according to claim 1 or 2, which is coated or encapsulated.
6. An oral care product comprising the oral care composition according to claim 1 or 2, or a product for obtaining a nutritional or refreshing sensation.
7. The oral care product according to claim 6, selected from the group consisting of toothpaste, tooth powder, tooth gel, liquid toothpaste, foam toothpaste, tablet toothpaste, mouthwash, mouth spray, dental floss, chewing gum, dental aligner, lozenge, effervescent tablet for dentures; effervescent tablet for dentures and dental aligner.
8. A method for treating or preventing demineralization due to dental erosion, gingivitis, plaque, periodontitis, bad breath, and / or dental caries, comprising applying the composition according to claim 1 or 2 to the oral cavity of a person in need thereof.
9. A method for identifying a test composition having an oral health care use, comprising (a) evaluating whether the test composition reduces bacterial adhesion, and / or (b) evaluating whether the test composition reduces biofilm formation, and / or (c) evaluating whether the test composition destroys the biofilm comprising A composition that is positive in one or more of the evaluations is useful as an oral health care composition. method.
10. The method according to claim 9, wherein the evaluation in step (a) comprises exposing a substrate to saliva and / or bacteria in the presence or absence of the test composition to determine whether the test composition reduces bacterial adhesion to the substrate.
11. The method according to claim 9, wherein the evaluation in step (b) comprises exposing a substrate to saliva and / or bacteria for at least 24 hours under culture conditions, then exposing the cultured mixture to the test composition to determine whether the test composition reduces biofilm formation on the substrate.
12. The method according to claim 9, wherein the evaluation in step (c) comprises exposing a substrate to saliva and / or bacteria for at least 72 hours under culture conditions to form a biofilm on the substrate, then exposing the cultured mixture to the test composition to determine whether the test composition destroys the biofilm.
13. The method according to any one of claims 9 to 12, wherein the effect of the test composition on the biofilm is determined by collecting the biofilm and identifying the amount and type of bacteria present in the biofilm.
14. The method according to any one of claims 9 to 12, comprising preparing an oral care composition using a test composition that is positive in one or more of the evaluations.