Plaque formation inhibitory composition
Quaternary ammonium salts with C10-C14 alkyl groups, especially when combined with cetylpyridinium chloride, efficiently target Fusobacterium, addressing the ineffectiveness of existing oral care products in inhibiting plaque formation and reducing periodontal disease risk.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2021-09-30
- Publication Date
- 2026-03-16
AI Technical Summary
Existing oral care compositions are ineffective in efficiently killing Fusobacterium, a vector bacterium that mediates plaque formation, leading to the attachment and aggregation of late-stage bacteria and subsequent plaque maturation, which contributes to periodontal disease.
Incorporation of quaternary ammonium salts with C10-C14 alkyl groups, particularly with cetylpyridinium chloride, to enhance bactericidal effects against Fusobacterium, thereby inhibiting plaque formation.
The compositions effectively kill Fusobacterium, suppressing plaque formation and its maturation, thus preventing periodontal disease.
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Abstract
Description
[Technical Field]
[0001] This disclosure relates to compositions for inhibiting plaque formation, etc. All references cited herein are incorporated herein by reference. [Background technology]
[0002] Plaque is a biofilm formed by the aggregation of oral microorganisms and is thought to be a cause of dental caries and periodontal disease. Therefore, plaque control, especially the suppression of plaque formation, is important.
[0003] Broadly speaking, plaque is formed as follows: First, a thin film of protein called a "pellicle," derived from saliva and physiological gingival crevicular fluid, forms on the tooth surface. Facultative anaerobic bacteria (initial attachment bacteria), such as streptococci, attach to the tooth surface via this pellicle. Vector bacteria, such as Fusobacterium, which co-aggregate with various oral bacteria, attach to these initial attachment bacteria. Furthermore, late attachment bacteria, such as anaerobic bacteria like Porphyromonas gingivalis and Treponema denticola, attach and aggregate via these vector bacteria, and the plaque matures. In particular, late attachment bacteria are known to cause periodontal disease and are directly or indirectly involved in the destruction of periodontal tissue. [Prior art documents] [Non-patent literature]
[0004] [Non-Patent Document 1] J Dent Res 90(11):1271-1278, 2011 [Overview of the project] [Problems that the invention aims to solve]
[0005] Based on the above, suppressing plaque formation on the tooth surface, and especially inhibiting the attachment and aggregation of late-stage attaching bacteria and the maturation of plaque, is important for preventing periodontal disease. [Means for solving the problem]
[0006] The inventors focused on Fusobacterium, a vector bacterium, and conducted their research. This is because they believe that if the activity of Fusobacterium, a vector bacterium capable of co-aggregating with various bacteria, can be suppressed, it will be possible to suppress the attachment and aggregation of late-adhering bacteria to the tooth surface, and consequently, to suppress the maturation of plaque formation.
[0007] Therefore, we investigated methods for killing Fusobacterium. However, even after examining various disinfectants commonly used in oral care compositions, we were unable to find a disinfectant that could efficiently kill Fusobacterium.
[0008] Cetylpyridinium chloride, an example of a bactericide commonly used in oral compositions, was no exception; no efficient bactericidal effect against Fusobacterium was observed. However, the inventors further investigated and discovered that cetylpyridinium chloride is a C16 alkylpyridinium chloride, and that the length of this alkyl group may be influencing its bactericidal effect against Fusobacterium. Based on this, they made further improvements.
[0009] This disclosure includes, for example, the following subjects: Section 1. A plaque formation inhibitory composition containing a quaternary ammonium salt having a C10-C14 alkyl group. Section 2. A plaque formation inhibitory composition containing a quaternary ammonium salt having a C10-C14 alkyl group and cetylpyridinium chloride. Section 3. Quaternary ammonium salts having C10-C14 alkyl groups, Formula (1):
[0010] [ka] Compounds represented by the formula (wherein R represents a C10-C14 linear alkyl group and X represents Cl or Br), and Formula (2):
[0011]
Chem.
[0012] ,
[0014] , , , , , ,
[0013] , represents a C10 - C14 linear alkyl group, R 2 and R 3 each independently represent a C1 - C4 alkyl group, and X represents Cl or Br) a compound represented by selected from the group consisting of at least one of the composition according to item 1 or 2. Item 4. A quaternary ammonium salt having a C10 - C14 alkyl group, Formula (1a):
[0012]
Chem.
[0013]
Chem.
[0015] [ka] (In the formula, R 1 R represents a C10-C14 linear alkyl group, 2 and R 3 Compounds represented by (where C1-C4 alkyl groups are the same or different, and X represents Cl or Br) It is at least one selected from the group consisting of, A plaque formation inhibitory effect enhancer as described in item 5. Section 7. Quaternary ammonium salts having C10-C14 alkyl groups, Formula (1a):
[0016] [ka] Compounds represented by the formula (wherein R is the same as above), and Formula (2a):
[0017] [ka] (In the formula, R 1 Compounds represented as above It is at least one selected from the group consisting of, A plaque formation inhibitory effect enhancer as described in item 6. Section 8. A quaternary ammonium salt containing a C10-C14 alkyl group, comprising cetylpyridinium chloride, that enhances the bactericidal effect of Fusobacterium. Section 9. Quaternary ammonium salts having C10-C14 alkyl groups, Formula (1):
[0018] [ka] Compounds represented by the formula (wherein R represents a C10-C14 linear alkyl group and X represents Cl or Br), and Formula (2):
[0019] [Chemical formula] (wherein, R 1 represents a C10-C14 linear alkyl group, R 2 and R 3 each independently represents a C1-C4 alkyl group, and X represents Cl or Br) a compound selected from the group consisting of at least one selected from the group consisting of the fusobacterium bactericidal effect enhancer according to item 8. Item 10. The quaternary ammonium salt having a C10-C14 alkyl group, Formula (1a):
[0020] [Chemical formula] (wherein, R is the same as defined above) a compound represented by, and Formula (2a):
[0021] [Chemical formula] (wherein, R 1 is the same as defined above) a compound represented by at least one selected from the group consisting of the fusobacterium bactericidal effect enhancer according to item 9. [Advantages of the Invention]
[0022] There is provided a method for efficiently killing fusobacterium, which is a mediating bacterium in plaque formation. As a result, it is also possible to efficiently suppress plaque formation. [Brief Description of the Drawings]
[0023] [Figure 1] The results of examining the bactericidal effect of fusobacterium of the quaternary ammonium salt (CPC and / or DPC) having a C10-C14 alkyl group are shown. [Figure 2] The results of the study on the bactericidal effect of quaternary ammonium salts (CPC and / or OPC) having C10-C14 alkyl groups on Fusobacterium are shown. [Figure 3] The results of the study on the bactericidal effect of quaternary ammonium salts (CPC and / or BKC12, BKC14, or BKC16) having C10-C14 alkyl groups on Fusobacterium are shown. [Figure 4a] The results of the study on the bactericidal effect of alkylpyridinium chloride (CPC and DPC) on Fusobacterium are shown. [Figure 4b] The results of the study on the bactericidal effect of alkylpyridinium chloride (CPC and OPC) on Fusobacterium are shown. [Figure 5] The results of studies on the bactericidal effect of compositions containing CPC and / or DPC on Fusobacterium are shown. [Figure 6] The results of studies on the bactericidal effect of compositions containing CPC and / or DPC on Fusobacterium are shown. [Figure 7a] The results of the study on the bactericidal effect of alkylpyridinium chloride (CPC and DPC) on Fusobacterium are shown. [Figure 7b] The results of the study on the bactericidal effect of alkylpyridinium chloride (CPC and DPC) on Fusobacterium are shown. [Modes for carrying out the invention]
[0024] The embodiments included in this disclosure will be described in more detail below. This disclosure preferably includes, but is not limited to, compositions for inhibiting plaque formation and agents for enhancing plaque formation inhibition effects, and so on. This disclosure includes everything disclosed herein and that can be recognized by those skilled in the art.
[0025] The compositions included in this disclosure contain a quaternary ammonium salt having a C10-C14 (C10, C11, C12, C13, or C14) alkyl group, and preferably further contain cetylpyridinium chloride. Such compositions may be referred to as "the compositions of this disclosure." The compositions of this disclosure are suitable for inhibiting plaque formation, and when used for this purpose, they may be specifically referred to as "the plaque formation inhibiting compositions of this disclosure."
[0026] As quaternary ammonium salts having a C10-C14 alkyl group, chloride salts or brominated salts are preferred. The alkyl group may be linear or branched, and is preferably linear.
[0027] More specifically, a quaternary ammonium salt having a C10-C14 alkyl group is, for example, formula (1):
[0028] [ka] Compounds represented by formula (2): (wherein R represents a C10-C14 linear alkyl group and X represents Cl or Br), and formula (2):
[0029] [ka] (In the formula, R 1 R represents a C10-C14 linear alkyl group, 2 and R 3 Compounds represented by (where are the same or different C1-C4 alkyl groups, and X represents Cl or Br) are preferred. The C1-C4 alkyl groups here may be linear or branched, and are preferably linear. There are no particular limitations, but methyl or ethyl groups are preferred, and R 2 and R 3 It is particularly preferable that both are methyl groups. Also, "C number" represents the number of carbon atoms. Furthermore, the compound represented by formula (1) is sometimes called "compound (1)", and the compound represented by formula (2) is sometimes called "compound (2)".
[0030] Among compound (1), formula (1a):
[0031] [ka] A compound represented by the formula (wherein R is the same as above) is more preferred.
[0032] Also, among compounds (2), formula (2a):
[0033] [ka] (In the formula, R 1 Compounds represented by (the same as above) are more preferred.
[0034] Quaternary ammonium salts having C10-C14 alkyl groups can be used individually or in combination of two or more.
[0035] The compositions disclosed herein can exhibit excellent fusobacterium bactericidal effects by containing a quaternary ammonium salt having a C10-C14 (C10, C11, C12, C13, or C14) alkyl group, and preferably further containing cetylpyridinium chloride. This allows for excellent plaque formation inhibition.
[0036] Therefore, the compositions of this disclosure can also be preferably used as compositions for killing Fusobacterium.
[0037] In this context, Fusobacterium is not particularly limited to any bacterium of the genus Fusobacterium that acts as a vector between early-adhering and late-adhering bacteria in plaque formation, but Fusobacterium nucleatum is a preferred example.
[0038] When the composition of this disclosure contains cetylpyridinium chloride, the preferred content ratio of cetylpyridinium chloride to a quaternary ammonium salt having a C10-C14 alkyl group is, for example, about 1 to 100 parts by mass of cetylpyridinium chloride per 10 parts by mass of the quaternary ammonium salt. The upper or lower limit of this range (1 to 100 parts by mass) is, for example, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, The amounts may be 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, or 99 parts by mass. For example, the range may be approximately 2 to 90 parts by mass or approximately 5 to 50 parts by mass.
[0039] The content of the quaternary ammonium salt having a C10-C14 alkyl group in the composition of this disclosure is not particularly limited as long as the effect is achieved, but for example, it is about 0.005 to 0.5% by mass. The upper or lower limits of this range are, for example, 0.01, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14, 0.15, 0.16, 0.17, 0.18, 0.19, 0.20, 0.21, 0.22, 0.23, 0. The mass percentages may be 0.24, 0.25, 0.26, 0.27, 0.28, 0.29, 0.3, 0.31, 32, 0.33, 0.34, 0.35, 0.36, 0.37, 0.38, 0.39, 0.4, 0.41, 0.42, 0.43, 0.44, 0.45, 0.46, 0.47, 0.48, and 0.49. For example, the range may be approximately 0.01 to 0.3 mass percent.
[0040] Furthermore, when the composition of this disclosure contains cetylpyridinium chloride, the cetylpyridinium chloride content is not particularly limited as long as the effect is achieved, but for example, it is about 0.01 to 0.5% by mass. The upper or lower limits of this range are, for example, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14, 0.15, 0.16, 0.17, 0.18, 0.19, 0.20, 0.21, 0.22, 0.23, and 0.24. The values may also be 0.25, 0.26, 0.27, 0.28, 0.29, 0.3, 0.31, 32, 0.33, 0.34, 0.35, 0.36, 0.37, 0.38, 0.39, 0.4, 0.41, 0.42, 0.43, 0.44, 0.45, 0.46, 0.47, 0.48, and 0.49 mass%. For example, the range may be approximately 0.02 to 0.3 mass% or approximately 0.03 to 0.1 mass%.
[0041] As described above, the inventors found that cetylpyridinium chloride alone does not exhibit an efficient bactericidal effect against Fusobacterium. However, further investigation revealed that cetylpyridinium chloride enhances the bactericidal effect of quaternary ammonium salts having C10-C14 alkyl groups against Fusobacterium. For this reason, the compositions of this disclosure exhibit particularly excellent bactericidal effects against Fusobacterium when they contain cetylpyridinium chloride, and consequently, can also exert a plaque formation inhibitory effect.
[0042] Therefore, this disclosure also includes fusobacterium bactericides comprising cetylpyridinium chloride and quaternary ammonium salts having a C10-C14 alkyl group, and plaque formation inhibitory effect enhancers comprising cetylpyridinium chloride and quaternary ammonium salts having a C10-C14 alkyl group. The above-described explanation of cetylpyridinium chloride and quaternary ammonium salts having a C10-C14 alkyl group for the compositions of this disclosure also preferably applies to the enhancers.
[0043] The compositions of this disclosure are particularly suitable for use as oral compositions. Furthermore, since these oral compositions are useful for killing Fusobacterium, they can also be preferably used for killing Fusobacterium. In other words, the compositions of this disclosure can be preferably used as oral compositions for inhibiting plaque formation or for killing Fusobacterium. When using the compositions of this disclosure as oral compositions, the compositions may be referred to as "the oral compositions of this disclosure."
[0044] The oral compositions of this disclosure may be solid compositions or liquid compositions. These oral compositions can be used, for example, as pharmaceuticals or quasi-drugs. The forms of the oral compositions of this disclosure are not particularly limited, but can be made into forms (dosage forms) such as ointments, pastes, pastes, gels, liquids, sprays, mouthwashes, liquid toothpastes, toothpastes, and gums according to conventional methods. Among these, mouthwashes, liquid toothpastes, toothpastes, ointments, pastes, liquids, and gels are preferred.
[0045] The oral compositions of this disclosure may contain, alone or in addition to two or more optional components that can be incorporated into oral compositions, as long as they do not impair the effects.
[0046] For example, nonionic surfactants, anionic surfactants, or amphoteric surfactants can be incorporated as surfactants. Specifically, examples of nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters, maltose fatty acid esters, and lactose fatty acid esters; fatty acid alkanolamides; sorbitan fatty acid esters; fatty acid monoglycerides; polyoxyethylene alkyl ethers with a polyoxyethylene addition coefficient of 8 to 10 and 13 to 15 carbon atoms in the alkyl group; polyoxyethylene alkylphenyl ethers with a polyoxyethylene addition coefficient of 10 to 18 and 9 carbon atoms in the alkyl group; diethyl sebacate; polyoxyethylene hydrogenated castor oil; and fatty acid polyoxyethylene sorbitan. Examples of anionic surfactants include sulfate ester salts such as sodium lauryl sulfate and sodium polyoxyethylene lauryl ether sulfate; sulfosuccinates such as sodium lauryl sulfosuccinate and sodium polyoxyethylene lauryl ether sulfosuccinate; acyl amino acid salts such as sodium cocoyl sarcosinate and sodium lauroyl methylalanine; and sodium cocoyl methyl taurate. Examples of amphoteric surfactants include betaine-type surfactants such as lauryldimethylaminoacetic acid betaine and coconut oil fatty acid amidopropyldimethylaminoacetic acid betaine; imidazoline-type surfactants such as N-cocoyl-N-carboxymethyl-N-hydroxyethylethylenediamine sodium; and amino acid-type surfactants such as N-lauryldiaminoethylglycine. These surfactants can be used individually or in combination of two or more. The amount used is usually 0.1 to 5% by mass of the total composition.
[0047] Furthermore, as flavoring agents, for example, menthol, carboxylic acid, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronenyl acetate, methyl eugenol, cineole, linalool, ethyl linalool, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil, wintergreen oil, clove oil, eucalyptus oil, pimento oil, d-camphor, d-borneol, fennel oil, cinnamon oil, cinnamaldehyde, peppermint oil, vanillin, and other fragrances can be used. These can be added individually or in combination of two or more in amounts of, for example, 0.001 to 1.5% by mass of the total composition.
[0048] Furthermore, sweeteners such as sodium saccharin, potassium acesulfamethamate, stevioside, neohesperidyl dihydrochalcone, perillartin, thaumatin, aspartylphenylalanyl methyl ester, and p-methoxycinnamic aldehyde can be used. These can be added in amounts of, for example, 0.01 to 1% by mass relative to the total amount of the composition.
[0049] Furthermore, sorbitol, ethylene glycol, propylene glycol, glycerin, 1,3-butylene glycol, polypropylene glycol, xylitol, maltitol, lactitol, polyoxyethylene glycol, etc., can be used as humectants, either individually or in combination of two or more.
[0050] As preservatives, parabens such as methylparaben, ethylparaben, propylparaben, and butylparaben, sodium benzoate, phenoxyethanol, and alkyldiaminoethylglycine hydrochloride may be included.
[0051] As coloring agents, legally approved pigments such as Blue No. 1, Yellow No. 4, Red No. 202, and Green No. 3, mineral pigments such as ultramarine, enhanced ultramarine, and navy blue, and titanium dioxide may be added.
[0052] As pH adjusters, citric acid, phosphoric acid, malic acid, pyrophosphate, lactic acid, tartaric acid, glycerophosphate, acetic acid, nitric acid, or chemically possible salts thereof, or sodium hydroxide may be included. These can be included individually or in combination of two or more so that the pH of the composition is in the range of 4 to 8, preferably 5 to 7. The amount of pH adjuster may be, for example, 0.01 to 2% by weight.
[0053] The oral compositions disclosed herein include not only quaternary ammonium salts having C10-C14 alkyl groups and cetylpyridinium chloride, but also, as active ingredients, vitamin E derivatives such as dl-α-tocopherol acetate, tocopherol succinate, or tocopherol nicotinate; amphoteric bactericides such as dodecyldiaminoethylglycine; nonionic bactericides such as triclosan, isopropylmethylphenol, and hinokitiol; anionic bactericides such as sodium lauroyl sarcosinate; cationic bactericides such as chlorhexidine hydrochloride and benzethonium chloride; dextranase, amylase, protease, mutanase, lysozyme, and lysozyme. Enzymes such as Ritec Enzyme, alkali metal monofluorophosphates such as sodium monofluorophosphate and potassium monofluorophosphate, fluorides such as sodium fluoride and stannous fluoride, tranexamic acid, epsilon-aminocaproic acid, aluminum chlorohydroxyl allantoin, dihydrocholesterol, glycyrrhetinic acid, glycyrrhizic acid, copper chlorophyllin sodium, glycerophosphate, chlorophyll, sodium chloride, caropeptide, allantoin, carbazochrome, hinokitiol, potassium nitrate, and palatinite can be formulated individually or in combination of two or more.
[0054] Furthermore, it is possible to add alcohols, silicones, apatite, white petrolatum, paraffin, liquid paraffin, microcrystalline wax, squalane, Plastibase, etc., as base materials.
[0055] Furthermore, the oral compositions of this disclosure can be prepared by known methods or by methods readily conceivable from known methods. For example, they can be prepared by appropriately mixing a quaternary ammonium salt having a C10-C14 alkyl group, preferably further containing cetylpyridinium chloride, and other components as needed.
[0056] The subjects to whom the oral compositions of this disclosure can be applied are not particularly limited, but humans and non-human mammals are preferred. Preferred non-human mammals include livestock and pets, more specifically dogs, cats, mice, rats, horses, cattle, sheep, monkeys, etc. Furthermore, as described above, the oral compositions of this disclosure contain a quaternary ammonium salt having a C10-C14 alkyl group, preferably further containing cetylpyridinium chloride, and can efficiently kill Fusobacterium, a vector bacterium. Therefore, they are particularly suitable for application to the oral cavity of subjects where plaque has not formed or is in the process of forming (where late-stage attached bacteria have not yet attached).
[0057] Furthermore, the above-mentioned descriptions of oral compositions in this disclosure may also apply to compositions of this disclosure that are not used as oral compositions (for example, when used for denture cleaning).
[0058] In this specification, the term "comprising" includes "consisting essentially of" and "consisting of." Furthermore, this disclosure encompasses all any combination of the constituent elements described herein.
[0059] Furthermore, the various characteristics (properties, structure, function, etc.) described in each embodiment of this disclosure above may be combined in any way to identify the subject matter covered by this disclosure. In other words, this disclosure covers all subject matter consisting of any combination of the combinable characteristics described herein. [Examples]
[0060] The embodiments of this disclosure will be described in more detail below with examples, but the embodiments of this disclosure are not limited to the examples below.
[0061] Investigation of the bactericidal effect of quaternary ammonium salts against Fusobacterium The following alkylpyridinium chloride and benzylalkyldimethylammonium chloride were dissolved in water at concentrations of 0.01%, 0.02%, 0.03%, 0.04%, 0.05%, 0.07%, or 0.10% and used as a disinfectant solution. In this disinfectant solution, each component was used individually or in combination. Although the alkylpyridinium chloride concentration (%) in this disinfectant solution is expressed as w / v%, due to the solvent being water and the relatively low concentration, it is almost the same as mass% (w / w%) and can be approximated accordingly.
[0062] Octylpyridinium chloride (OPC): R = (CH2)7CH3 Dodecylpyridinium chloride (DPC): R = (CH2) 11 CH3 Cetylpyridinium chloride (CPC): R = (CH2) 15 CH3
[0063] [ka]
[0064] Benzylldodecyldimethylammonium chloride (BKC12): R 1 =C 12 H 25 Benzyltetradecyldimethylammonium chloride (BKC14): R 1 =C 14 H 29 Benzylhexadecyldimethylammonium chloride (BKC16): R 1 =C16 H 33
[0065] [ka]
[0066] In addition, the following two subspecies of Fusobacterium were used as test bacteria. Bacteria 1: Fusobacterium nucleatum subsp. nucleatum ATCC23726 Bacteria 2: Fusobacterium nucleatum subsp. nucleatum ATCC25586
[0067] Each test bacterium was inoculated into 10 ml of GAM broth medium (Nissui Pharmaceutical Co., Ltd.) and incubated anaerobically at 37°C for 2 days. This culture solution was used as the test bacterial solution.
[0068] 200 μl of the test bacterial suspension was mixed with 200 μl of disinfectant solutions of different concentrations. 30 seconds after mixing, 100 μl of the mixture was taken, and 900 μl of drug-inactivated PBS (phosphate-buffered saline) was added, which had been prepared by adding soy lecithin and Tween 80 to phosphate-buffered saline (PBS) to final concentrations of 0.07% and 0.5%, respectively (diluting the mixture 10-fold) to inactivate the bactericidal action of the disinfectant. The mixture was then serially diluted with drug-inactivated PBS, and the mixture was 10-fold. 1 ~10 7 Diluted up to twice the original volume (serialized mixed solution).
[0069] 100 μl each of the prepared serially diluted mixtures was spread onto CDC anaerobic sheep blood agar plates (Becton Dickinson Japan Co., Ltd.), incubated anaerobically at 37°C for 3 days, and the number of viable bacteria was counted.
[0070] The results are shown in Figures 1, 2, and 3. These figures are graphs with Log(viable cell count) CFU / ml on the vertical axis, where a value of 2 is the detection limit. (A value of less than 2 indicates that the bacteria were sterilized to less than 100 CFU.) The concentrations of CPC, DPC, OPC, BKC12, BKC14, and BKC16 in these figures and the following figures represent the concentrations of the respective components prepared as disinfectant solutions.
[0071] It was found that CPC and OPC do not show bactericidal effects against Fusobacterium, while DPC shows bactericidal effects against Fusobacterium even at relatively low concentrations. Furthermore, although CPC alone does not show bactericidal effects against Fusobacterium, it was found that when combined with DPC, it enhances the bactericidal effect of DPC against Fusobacterium. Here, the results when OPC, DPC, or CPC are used individually are selected from Figures 1 and 2 and shown in Figures 4a and 4b.
[0072] Similarly, it was found that BKC16 does not show a bactericidal effect against Fusobacterium, while BKC14 or BKC12 do show a bactericidal effect against Fusobacterium even at relatively low concentrations. Furthermore, although CPC alone does not show a bactericidal effect against Fusobacterium, it was found that when combined with BKC14 or BKC12, it enhances the bactericidal effect of BKC14 or BKC12 against Fusobacterium.
[0073] Investigation of the bactericidal effect of compositions containing quaternary ammonium salts and CPC against Fusobacterium. Liquid compositions containing quaternary ammonium salts and CPC at various concentrations were prepared by adding these components to water, a solvent (glycerin), fragrance, preservative, and solubilizer (polyoxyethylene hydrogenated castor oil), etc.
[0074] The bactericidal effect was investigated using the liquid composition in the same manner as described above. The results are shown in Figure 5.
[0075] Furthermore, the bactericidal effect of the liquid composition against a wider range of Fusobacterium subspecies was investigated in the same manner as described above. Specifically, instead of bacteria 1 and 2, bacteria 3, 4, 5, 6, and 7 were used to examine the bactericidal effect. The results are shown in Figure 6. Bacteria 3:Fusobacterium necrophorum subsp. necrophorum ATCC25286 Bacteria 4:Fusobacterium nucleatum subsp. polymorphum ATCC10953 Bacteria 5: Fusobacterium nucleatum subsp. fusiforme ATCC51190 Bacteria 6:Fusobacterium nucleatum subsp. vincentii ATCC49256 Bacteria 7:Fusobacterium nucleatum subsp. animalis ATCC51191
[0076] It was confirmed that the DPC and CPC-containing compositions examined sterilized Fusobacterium to below the detection limit. Furthermore, the bactericidal effect against Fusobacterium of compositions containing alkylpyridinium chloride at various concentrations, either alone or in combination, was re-examined in the same manner as described above. The results are shown in Figures 7a and 7b.
[0077] The following are examples of prescriptions. Note that the values for each component in the following examples are shown as mass percent.
[0078] Prescription examples [Liquid Gel] [Table 1]
[0079] [Toothpaste] [Table 2]
Claims
1. A composition for inhibiting plaque formation, comprising dodecylpyridinium chloride and cetylpyridinium chloride.
2. A composition for killing Fusobacterium containing dodecylpyridinium chloride and cetylpyridinium chloride.
3. A plaque formation inhibitory agent comprising cetylpyridinium chloride, which enhances the plaque formation inhibitory effect of dodecylpyridinium chloride.
4. A fusobacterium bactericidal agent consisting of cetylpyridinium chloride, specifically dodecylpyridinium chloride.
Citation Information
Patent Citations
JPP6968964B
Oral compositions
US4472373A