CN105358128A - Oral biofilm remover and composition for oral cavity - Google Patents
Oral biofilm remover and composition for oral cavity Download PDFInfo
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- CN105358128A CN105358128A CN201480038713.5A CN201480038713A CN105358128A CN 105358128 A CN105358128 A CN 105358128A CN 201480038713 A CN201480038713 A CN 201480038713A CN 105358128 A CN105358128 A CN 105358128A
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Abstract
Description
技术领域technical field
本发明涉及以化学方法高效地除去作为龋齿的原因的生物膜的口腔生物膜除去剂以及口腔用组合物。The present invention relates to an oral biofilm removing agent and a composition for oral cavity that chemically and efficiently remove biofilm that is the cause of dental caries.
背景技术Background technique
以往,作为洁齿剂中的牙菌斑(牙垢)除去技术,具有研磨剂等的清洁剂引起的物理性除去,酶等引起的生物化学性除去等。Conventionally, techniques for removing plaque (tartar) in dentifrices include physical removal by cleaning agents such as abrasives, biochemical removal by enzymes, and the like.
使用清洁剂进行除去时,为了发挥其效果需要增加研磨剂的量,提高硬度,但伴随着研磨力上升,有易于产生牙齿和牙龈损伤等的危害性、刺激性的可能。另一方面,为了稳定混合酶,需要并用各种稳定剂,有影响起泡和味道等使用感的情况。When removing with a cleaning agent, it is necessary to increase the amount of the abrasive and increase the hardness in order to exert its effect, but as the abrasive force increases, there is a possibility that harmfulness and irritation such as damage to teeth and gums may easily occur. On the other hand, in order to stabilize the mixed enzyme, it is necessary to use various stabilizers in combination, which may affect the usability such as foaming and taste.
此外,近年,若能将牙垢作为生物膜捕获,除去生物膜,则能更有效地除去牙垢。对于除去口腔内的生物膜,不仅使用牙刷刷牙的物理方法有用,而且能将牙刷无法接触到的生物膜除去的化学方法也有用。生物膜是由各种口腔内细菌的共聚集体和胞外多糖类构成。因此,作为化学除去方法,已知有使用具有抑制共聚集作用的赤藓糖醇和,使用分解胞外多糖的酶的蛋白酶或葡聚糖酶、变聚糖酶等的方法,但其效果还有改善的空间。In addition, in recent years, if the plaque can be captured as a biofilm and the biofilm can be removed, the plaque can be removed more effectively. For the removal of biofilm in the oral cavity, not only the physical method of brushing teeth with a toothbrush is useful, but also the chemical method of removing the biofilm that cannot be touched by the toothbrush. Biofilms are composed of co-aggregates of various oral bacteria and exopolysaccharides. Therefore, as a chemical removal method, there are known methods using erythritol, which has a co-aggregation-inhibiting effect, and protease, dextranase, mutanase, etc., which decompose exopolysaccharide enzymes, but the effect is still room for improvement.
此外,已知表面活性剂具有洗涤作用,可以作为洗涤剂用于口腔用组合物。这种情况下,已知月桂基磺基乙酸钠是不具有阴离子性表面活性剂特有的刺激的活性剂(专利文献1:日本专利特开平6-72836号公报)。In addition, surfactants are known to have a cleansing effect and can be used in oral compositions as cleansers. In this case, sodium lauryl sulfoacetate is known to be an active agent that does not have the irritation peculiar to anionic surfactants (Patent Document 1: Japanese Patent Laid-Open No. 6-72836).
但是,一直以来的现状是表面活性剂,从其渗透作用,表面洁净化作用的观点考虑,虽然只具有轻微的效果但还是认为其具有牙垢除去效果,可是并不认为单独使用表面活性剂时具有充分的牙垢乃至生物膜除去效果。However, the status quo has always been that surfactants, from the viewpoint of their penetrating action and surface cleaning action, are considered to have a tartar removal effect although they have only a slight effect, but they are not considered to be effective when they are used alone. Sufficient plaque and biofilm removal effect.
另外,专利文献2(日本专利特表2008-519043号公报)中公开了并用磺基乙酸烷基的碱金属盐或铵盐与水溶性锌盐的方法,但是磺基乙酸烷基盐是用于降低锌盐的收敛性的化合物,并没有显示生物膜的除去效果。进一步地,专利文献3(日本专利特开平9-508120号公报)公开了含有月桂基磺基乙酸钠的牙膏作为减轻对口腔黏膜的刺激的口腔用组合物,但并没有涉及提高生物膜除去效果。In addition, Patent Document 2 (Japanese Patent Publication No. 2008-519043) discloses a method of using an alkali metal salt or an ammonium salt of an alkyl sulfoacetate and a water-soluble zinc salt in combination, but the alkyl sulfoacetate is used for Compounds that reduce the astringency of zinc salts did not show a biofilm removal effect. Furthermore, Patent Document 3 (Japanese Patent Laid-Open No. 9-508120) discloses a toothpaste containing sodium lauryl sulfoacetate as an oral composition for reducing irritation to the oral mucosa, but does not refer to improving the biofilm removal effect .
另一方面,已知缩聚磷酸盐具有化学性的除去牙齿污渍的效果(专利文献4:日本专利特开平9-175966号公报),但并不认为单独使用缩聚磷酸盐时具有充分的牙垢以及生物膜除去效果。On the other hand, it is known that condensed phosphates have the effect of chemically removing tooth stains (Patent Document 4: Japanese Patent Laid-Open No. 9-175966), but it is not considered that condensed phosphates alone have sufficient tartar and biological stain removal effects. Membrane removal effect.
现有技术文献prior art literature
专利文献patent documents
专利文献1:日本专利特开平6-72836号公报Patent Document 1: Japanese Patent Laid-Open No. 6-72836
专利文献2:日本专利特表2008-519043号公报Patent Document 2: Japanese Patent Application Publication No. 2008-519043
专利文献3:日本专利特开平9-508120号公报Patent Document 3: Japanese Patent Laid-Open No. 9-508120
专利文献4:日本专利特开平9-175966号公报Patent Document 4: Japanese Patent Laid-Open No. 9-175966
发明内容Contents of the invention
发明要解决的课题The problem to be solved by the invention
本发明的课题是鉴于上述情况提供一种以化学方法高效地除去作为龋齿的原因的生物膜的口腔生物膜除去剂以及口腔用组合物。An object of the present invention is to provide an oral biofilm removing agent and a composition for oral cavity that chemically and efficiently remove biofilm that is a cause of dental caries in view of the above circumstances.
解决课题的手段means of solving problems
本发明为了达到上述本发明的课题经过深入研究,结果发现通过并用(A)α-烯烃磺酸盐以及(B)缩聚磷酸盐(B-1)和/或两性表面活性剂(B-2)能够解决上述课题。As a result of intensive studies in order to achieve the above-mentioned subject of the present invention, the present invention found that by using (A) α-olefin sulfonate and (B) condensed phosphate (B-1) and/or amphoteric surfactant (B-2) in combination The above-mentioned problems can be solved.
具体而言,本发明人们发现,通过组合(A)α-烯烃磺酸盐与(B)缩聚磷酸盐(B-1),能够显著提高口腔生物膜的除去效果,而且能够抑制(A)成分特有的苦味,此外能够赋予适当的起泡(第I发明)。Specifically, the present inventors have found that by combining (A) α-olefin sulfonate and (B) condensed phosphate (B-1), the effect of removing oral biofilm can be significantly improved, and the effect of (A) component can be suppressed. Unique bitterness, in addition, can impart appropriate foaming (1st invention).
第I发明中,(A)成分与(B-1)成分,特别是(A)/(B-1)的质量比在0.1~10的范围内时,特异且协同地起作用,增强分散除去口腔生物膜的作用。此外,能够抑制源自(A)成分的苦味,赋予由(A)成分引起的适当的起泡。In the first invention, when the mass ratio of (A) component to (B-1) component, especially (A)/(B-1) is in the range of 0.1 to 10, they act specifically and synergistically to enhance dispersion removal The role of oral biofilms. Moreover, the bitterness originating in (A) component can be suppressed, and the appropriate foaming by (A) component can be provided.
即,如后述实施例以及比较例所示,单独使用(A)成分的α-烯烃磺酸盐时,制作的生物膜的除去率停滞在不足70%。此外,发现即使缩聚磷酸盐(B-1)中的生物膜除去率不足50%,也不具有充分的生物膜除去效果,但并用(A)成分与(B-1)成分时,意外地两种成分协同起作用,能够得到充分的生物膜除去效果。此外,发现这种情况下,即使将(A)成分以外的阴离子性表面活性剂,例如月桂基硫酸钠,与缩聚磷酸盐并用,也无法得到充分的生物膜除去效果,上述生物膜除去效果是(A)成分与(B-1)成分并用的情况下的特异的作用效果。进一步地,α-烯烃磺酸盐具有苦味,以往,虽然在文献中公开了它的使用,但实际在口腔制剂中是属于回避的材料,而本发明人们发现将(A)成分与(B-1)成分并用时,能够抑制源自(A)成分的苦味,赋予良好的使用感,维持(A)成分引起的适当的起泡,制成适合实际使用的制剂,从而完成本发明。That is, as shown in Examples and Comparative Examples described later, when the α-olefin sulfonate of the component (A) was used alone, the removal rate of the produced biofilm stagnated at less than 70%. In addition, it was found that even if the biofilm removal rate in the condensed phosphate (B-1) was less than 50%, it did not have a sufficient biofilm removal effect, but when the (A) component and (B-1) component were used together, unexpectedly, both These ingredients work synergistically to obtain a sufficient biofilm removal effect. In addition, in this case, it was found that even if an anionic surfactant other than component (A), such as sodium lauryl sulfate, was used in combination with condensed phosphate, a sufficient biofilm removal effect could not be obtained. The above biofilm removal effect was Specific effect when (A) component and (B-1) component are used together. Furthermore, α-olefin sulfonate has a bitter taste. Although its use has been disclosed in the literature, it is actually a material to be avoided in oral preparations. 1) When the components are used together, the bitterness derived from the (A) component can be suppressed, a good feeling can be provided, and the appropriate foaming caused by the (A) component can be maintained, and a formulation suitable for practical use can be prepared, thereby completing the present invention.
此外,本发明人们为了达到上述本发明的课题经过深入研究,结果发现通过组合(A)α-烯烃磺酸盐与(B)两性表面活性剂(B-2),能够显著提高口腔生物膜的除去效果,并且能够抑制(A)成分特有的苦味,此外能够赋予适当的起泡(第II发明)。Furthermore, as a result of intensive research by the present inventors in order to achieve the above-mentioned subject of the present invention, it was found that the combination of (A) α-olefin sulfonate and (B) amphoteric surfactant (B-2) can significantly improve the oral cavity biofilm The bitterness peculiar to (A) component can be suppressed while removing an effect, and can provide appropriate foaming (II invention).
第(II)发明中,(A)成分与(B-2)成分,特别是(A)/(B-2)的质量比在0.2~8的范围内时,特异且协同地起作用,增强分散除去口腔生物膜的作用。此外,能够抑制源自(A)成分的苦味,赋予由(A)成分引起的适当的起泡。In the (II) invention, when the mass ratio of (A) component and (B-2) component, especially (A)/(B-2) is in the range of 0.2 to 8, they act specifically and synergistically to enhance Disperses the action of removing oral biofilm. Moreover, the bitterness originating in (A) component can be suppressed, and the appropriate foaming by (A) component can be provided.
即,如后述实施例以及比较例所示,单独使用(A)成分的α-烯烃磺酸盐时,制作的生物膜的除去率停滞在不足70%。此外,发现虽然两性表面活性剂(B-2)中的生物膜除去率不足50%,不具有充分的生物膜除去效果,即使与将其与其他表面活性剂并用,也不认为能使生物膜除去效果提高,但将(A)成分与(B-2)成分并用时,意外地两种成分协同地起作用,通过表面活性剂体系能够得到充分的生物膜除去效果。此外,发现这种情况下,即使将(A)成分以外的阴离子性表面活性剂,例如月桂基硫酸钠,与两性表面活性剂并用,也无法得到充分的生物膜除去效果,上述生物膜除去效果是并用(A)成分与(B-2)成分时的特异的作用效果。进一步地发现,α-烯烃磺酸盐具有苦味,虽然以往在文献中公开了它的使用,但实际上它的使用是被回避的,但是当并用(A)成分与(B-2)成分时,能够抑制源自(A)成分的苦味,赋予良好的使用感,此外能够维持(A)成分引起的适当的起泡,制成适合实际使用的制剂,完成了本发明。That is, as shown in Examples and Comparative Examples described later, when the α-olefin sulfonate of the component (A) was used alone, the removal rate of the produced biofilm stagnated at less than 70%. In addition, it was found that although the biofilm removal rate in the amphoteric surfactant (B-2) is less than 50%, it does not have a sufficient biofilm removal effect, and even if it is used in combination with other surfactants, it is not considered that the biofilm The removal effect was improved, but when the (A) component and the (B-2) component were used together, both components unexpectedly acted synergistically, and a sufficient biofilm removal effect was obtained by the surfactant system. In addition, it was found that in this case, even if an anionic surfactant other than component (A), such as sodium lauryl sulfate, is used in combination with an amphoteric surfactant, a sufficient biofilm removal effect cannot be obtained. It is the specific action effect when the component (A) and the component (B-2) are used together. Furthermore, it was found that α-olefin sulfonate has a bitter taste, and although its use has been disclosed in the literature, its use has actually been avoided. However, when components (A) and (B-2) are used together , can suppress the bitterness originating from (A) component, can impart favorable use feeling, can maintain the appropriate foaming caused by (A) component in addition, can make the formulation suitable for actual use, and completed the present invention.
第II发明中,进一步地混合(C)季铵盐、(D)木糖醇和/或赤藓糖醇时,能够特异地赋予更优异的口腔生物膜除去效果。In the second invention, when the (C) quaternary ammonium salt, (D) xylitol, and/or erythritol are further mixed, a more excellent oral biofilm removal effect can be specifically imparted.
这种情况下,更优选含有(A)成分、(B-2)成分,进一步优选含有(C)成分的洁齿剂组合物,或者更优选含有(A)成分、(B-2)成分,进一步优选含有(D)成分的漱口水组合物。In this case, it is more preferable to contain (A) component, (B-2) component, the dentifrice composition containing (C) component is more preferable, or it is more preferable to contain (A) component, (B-2) component, More preferably, the mouthwash composition containing (D)component.
因此,本发明(第I发明)提供下述口腔生物膜除去剂以及口腔用组合物。Therefore, the present invention (first invention) provides the following oral biofilm removing agent and oral composition.
〔I-1〕一种口腔生物膜除去剂,含有(A)α-烯烃磺酸盐与(B-1)缩聚磷酸盐。[I-1] An oral biofilm removing agent comprising (A) α-olefin sulfonate and (B-1) condensed phosphate.
〔I-2〕如〔I-1〕记载的口腔生物膜除去剂,其中,(A)/(B-1)的质量比为0.1~10。[I-2] The oral biofilm removing agent according to [I-1], wherein the mass ratio of (A)/(B-1) is 0.1-10.
〔I-3〕如〔I-1〕或〔I-2〕记载的口腔生物膜除去剂,其中,(A)成分的α-烯烃磺酸盐是碳原子数为14~16的α-烯烃磺酸盐。[I-3] The oral biofilm removing agent according to [I-1] or [I-2], wherein the α-olefin sulfonate of the component (A) is an α-olefin having 14 to 16 carbon atoms Sulfonate.
〔I-4〕一种口腔用组合物,其特征在于,含有(A)α-烯烃磺酸盐与(B-1)缩聚磷酸盐。[I-4] An oral composition comprising (A) α-olefin sulfonate and (B-1) condensed phosphate.
〔I-5〕如〔I-4〕记载的口腔用组合物,其中,(A)/(B-1)的质量比为0.1~10。[I-5] The composition for oral cavity according to [I-4], wherein the mass ratio of (A)/(B-1) is 0.1-10.
〔I-6〕如〔I-4〕或〔I-5〕记载的口腔用组合物,其中,含有(A)成分α-烯烃磺酸盐0.3~5质量%。[I-6] The composition for oral cavity according to [I-4] or [I-5], which contains (A) component α-olefin sulfonate in an amount of 0.3 to 5% by mass.
〔I-7〕如〔1-4〕、〔I-5〕或〔I-6〕记载的口腔用组合物,其中,含有(B-1)成分缩聚磷酸盐0.1~5质量%。[I-7] The composition for oral cavity according to [1-4], [I-5] or [I-6], which contains 0.1 to 5% by mass of the polycondensed phosphate as the component (B-1).
〔I-8〕如〔I-4〕~〔I-7〕的任一项记载的口腔用组合物,是洁齿剂组合物或漱口水组合物。[I-8] The composition for oral cavity according to any one of [I-4] to [I-7], which is a dentifrice composition or a mouthwash composition.
〔I-9〕如〔I-4〕~〔I-8〕的任一项记载的口腔用组合物,是口腔生物膜除去用口腔用组合物。[I-9] The oral composition according to any one of [I-4] to [I-8], which is an oral composition for removing oral biofilm.
因此,本发明(第II发明)提供下述的口腔生物膜除去剂以及口腔用组合物。Therefore, this invention (II invention) provides the following oral cavity biofilm removal agent and oral cavity composition.
〔II-1〕一种口腔生物膜除去剂,含有(A)α-烯烃磺酸盐与(B-2)两性表面活性剂。[II-1] An oral biofilm removing agent comprising (A) an α-olefin sulfonate and (B-2) an amphoteric surfactant.
〔II-2〕如〔II-1〕记载的口腔生物膜除去剂,其中,(A)/(B-2)的质量比为0.2~8。[II-2] The oral biofilm removing agent according to [II-1], wherein the mass ratio of (A)/(B-2) is 0.2-8.
〔II-3〕如〔II-1〕或〔II-2〕记载的口腔生物膜除去剂,其中,(B-2)成分的两性表面活性剂是从脂肪酸酰胺烷基甜菜碱、咪唑啉鎓甜菜碱以及氨基乙酸甜菜碱中选出的1种以上的甜菜碱系两性表面活性剂。[II-3] The oral biofilm removing agent described in [II-1] or [II-2], wherein the amphoteric surfactant of the component (B-2) is selected from fatty acid amide alkyl betaine, imidazolinium One or more betaine-based amphoteric surfactants selected from betaine and glycine betaine.
〔II-4〕如〔II-1〕、〔II-2〕或〔II-3〕记载的口腔生物膜除去剂,其中,(A)成分的α-烯烃磺酸盐是碳原子数为14~16的α-烯烃磺酸盐。[II-4] The oral biofilm removing agent according to [II-1], [II-2] or [II-3], wherein the α-olefin sulfonate of the component (A) has 14 carbon atoms ~16 α-olefin sulfonates.
〔II-5〕如〔II-1〕~〔II-4〕中任一项记载的口腔生物膜除去剂,其中,进一步含有(C)季铵盐。[II-5] The oral biofilm removing agent according to any one of [II-1] to [II-4], further comprising (C) a quaternary ammonium salt.
〔II-6〕如〔II-5〕记载的口腔生物膜除去剂,其中,(C)成分的季铵盐是选自西吡氯铵、苯扎氯铵以及苄索氯铵的1种以上。[II-6] The oral biofilm removing agent according to [II-5], wherein the quaternary ammonium salt of the component (C) is at least one selected from cetylpyridinium chloride, benzalkonium chloride, and benzethonium chloride .
〔II-7〕如〔II-1〕~〔II-6〕中任一项记载的口腔生物膜除去剂,其中,进一步含有(D)木糖醇和/或赤藓糖醇。[II-7] The oral biofilm removing agent according to any one of [II-1] to [II-6], further comprising (D) xylitol and/or erythritol.
〔II-8〕一种口腔用组合物,其特征在于,含有(A)α-烯烃磺酸盐和(B-2)两性表面活性剂。[II-8] An oral composition comprising (A) α-olefin sulfonate and (B-2) an amphoteric surfactant.
〔II-9〕如〔II-8〕记载的口腔用组合物,其中,(A)/(B-2)的质量比为0.2~8。[II-9] The composition for oral cavity according to [II-8], wherein the mass ratio of (A)/(B-2) is 0.2-8.
〔II-10〕如〔II-8〕或〔II-9〕记载的口腔用组合物,其中,含有(A)成分α-烯烃磺酸盐0.1~3质量%、(B-2)成分两性表面活性剂0.05~5质量%。[II-10] The composition for oral cavity according to [II-8] or [II-9], which contains (A) component α-olefin sulfonate in an amount of 0.1 to 3% by mass, (B-2) component amphoteric Surfactant 0.05-5% by mass.
〔II-11〕如〔II-8〕、〔II-9〕或〔II-10〕记载的口腔用组合物,其中,进一步含有(C)季铵盐0.003~0.05质量%。[II-11] The composition for oral cavity according to [II-8], [II-9] or [II-10], further comprising 0.003 to 0.05% by mass of (C) a quaternary ammonium salt.
〔II-12〕如〔II-8〕~〔II-11〕中任一项记载的口腔用组合物,其中,进一步含有(D)木糖醇和/或赤藓糖醇0.1~2质量%。[II-12] The oral composition according to any one of [II-8] to [II-11], further comprising (D) xylitol and/or erythritol in an amount of 0.1 to 2% by mass.
〔II-13〕如〔II-8〕~〔II-12〕中任一项记载的口腔用组合物,其是洁齿剂组合物或漱口水组合物。[II-13] The composition for oral cavity according to any one of [II-8] to [II-12], which is a dentifrice composition or a mouthwash composition.
〔II-14〕如〔II-8〕~〔II-13〕中任一项记载的口腔用组合物,其是口腔生物膜除去用口腔用组合物。[II-14] The oral composition according to any one of [II-8] to [II-13], which is an oral composition for removing oral biofilm.
发明的效果The effect of the invention
本发明的口腔生物膜除去剂以及口腔用组合物,在以化学方法除去作为龋齿的原因的口腔生物膜方面效果优异。此外,能够抑制苦味赋予良好的使用感,赋予适当的起泡。The oral biofilm removing agent and composition for oral cavity of the present invention are excellent in chemically removing oral biofilm which is the cause of dental caries. In addition, it is possible to suppress bitterness, provide a good feeling in use, and provide appropriate foaming.
具体实施方式detailed description
以下,对本发明进行进一步详细说明。Hereinafter, the present invention will be described in further detail.
本发明是含有(A)α-烯烃磺酸盐以及(B)缩聚磷酸盐(B-1)和/或两性表面活性剂(B-2)的口腔生物膜除去剂。此外,本发明是含有上述(A)以及(B)成分的口腔用组合物。The present invention is an oral biofilm removing agent comprising (A) α-olefin sulfonate, (B) condensed phosphate (B-1) and/or amphoteric surfactant (B-2). Moreover, this invention is a composition for oral cavity containing said (A) and (B) component.
本发明中,第I发明的特征在于,并用(A)α-烯烃磺酸盐与作为(B)成分的缩聚磷酸盐(B-1)。In the present invention, the first invention is characterized in that (A) α-olefin sulfonate and polycondensed phosphate (B-1) as the component (B) are used in combination.
通过并用(A)α-烯烃磺酸盐以及(B-1)成分,能够显著提高生物膜的分散除去效果,此外,能够抑制(A)成分的苦味,能够适当地赋予起泡性。By using (A) α-olefin sulfonate and (B-1) component in combination, the dispersion removal effect of biofilm can be significantly improved, and the bitterness of (A) component can be suppressed, and foaming property can be imparted suitably.
作为(A)α-烯烃磺酸盐,可以使用碳原子数为14~16的α-烯烃磺酸的钠、钾等碱金属盐,优选碳原子数14的α-烯烃磺酸盐。这些可以是能够获取的能用于口腔用制剂的市售品。As (A) α-olefin sulfonate, alkali metal salts such as sodium and potassium of α-olefin sulfonic acid having 14 to 16 carbon atoms can be used, preferably α-olefin sulfonate having 14 carbon atoms. These may be available commercial products that can be used for oral preparations.
第I发明中使用的(B)成分的缩聚磷酸盐(B-1)与(A)成分并用时,生物膜除去效果提高,此外,抑制苦味,赋予适当的起泡性。When the condensed phosphate (B-1) of the (B) component used in the first invention is used in combination with the (A) component, the biofilm removal effect is improved, and bitterness is suppressed, and appropriate foaming properties are imparted.
作为(B)成分的缩聚磷酸盐,可以使用下述通式(1)所示的直链状的水溶性聚磷酸盐。例如,可列举聚合度n=2的焦磷酸钠或焦磷酸钾、n=3的三聚磷酸钠或三聚磷酸钾、n=4的四聚磷酸钠或四聚磷酸钾、n=5的五聚磷酸钠、进一步地高聚合度的偏磷酸钠或偏磷酸钾等。这些可以单独使用1种或组合2种以上使用,其中,从效果体现的方面考虑,适宜为焦磷酸钠、焦磷酸钾、三聚磷酸钠,特别优选三聚磷酸钠。As the polycondensed phosphate of the component (B), linear water-soluble polyphosphate represented by the following general formula (1) can be used. For example, sodium pyrophosphate or potassium pyrophosphate with a degree of polymerization of n=2, sodium or potassium tripolyphosphate with n=3, sodium or potassium tetrapolyphosphate with n=4, Sodium pentapolyphosphate, sodium metaphosphate or potassium metaphosphate with a further high degree of polymerization, etc. These can be used individually by 1 type or in combination of 2 or more types, Among them, sodium pyrophosphate, potassium pyrophosphate, and sodium tripolyphosphate are suitable from the viewpoint of effect expression, and sodium tripolyphosphate is especially preferable.
Mn+2PnO3n+1(1)M n+2 P n O3 n+1 (1)
(式中,M表示Na或K,n≧2。)(In the formula, M represents Na or K, n≧2.)
具体地可以使用焦磷酸钠(太平化学产业株式会社制、东北化学株式会社制)、焦磷酸钾(太平化学产业株式会社制、东亚合成化学株式会社制)、三聚磷酸钠(太平化学产业株式会社制、Central硝子株式会社(セントラル硝子(株))制、日本builder株式会社(日本ビルダー(株))制)、三聚磷酸钾(太平化学产业株式会社制)、四聚磷酸钠(太平化学产业株式会社制)、五聚磷酸钠(太平化学产业株式会社制)等。Specifically, sodium pyrophosphate (manufactured by Taihei Chemical Industry Co., Ltd., Tohoku Chemical Co., Ltd.), potassium pyrophosphate (manufactured by Taihei Chemical Industry Co., Ltd., Toa Gosei Chemical Co., Ltd.), sodium tripolyphosphate (manufactured by Taihei Chemical Industry Co., Ltd. Co., Ltd., Central Glass Co., Ltd. (Central Glass Co., Ltd.), Nippon Builder Co., Ltd. (Nippon Builder Co., Ltd.), potassium tripolyphosphate (Taihei Chemical Industry Co., Ltd.), sodium tetrapolyphosphate (Taihei Chemical Co., Ltd. Sangyo Co., Ltd.), sodium pentapolyphosphate (made by Taihei Chemical Industry Co., Ltd.), etc.
第I发明中,(A)成分与(B-1)成分的混合比例在特定范围时,口腔生物膜除去效果更优异。(A)/(B-1)的比率没有特别限定,但作为质量比优选0.1~10,更优选为0.2~5,进一步地优选为0.6~3,特别优选为1.2~3。In the first invention, when the mixing ratio of (A) component and (B-1) component is in a specific range, the effect of removing oral biofilm is more excellent. The ratio of (A)/(B-1) is not particularly limited, but is preferably 0.1-10 as a mass ratio, more preferably 0.2-5, still more preferably 0.6-3, particularly preferably 1.2-3.
在上述比例范围内时,生物膜除去效果更优异。此外,从抑制苦味,赋予良好的起泡方面考虑,优选比例值为10以下。Within the range of the above ratio, the biofilm removal effect is more excellent. In addition, the ratio is preferably 10 or less from the viewpoint of suppressing bitterness and imparting favorable foam.
此外,本发明中,第II发明的特征在于,并用(A)α-烯烃磺酸盐与作为(B)成分的两性表面活性剂(B-2)。Moreover, in this invention, II invention is characterized by using together (A) α-olefin sulfonate, and the amphoteric surfactant (B-2) which is (B) component.
通过并用(A)α-烯烃磺酸盐以及(B-2)成分,能够显著提高生物膜的分散除去效果,此外,能够抑制(A)成分的苦味,能够适当地赋予起泡性。By using (A) α-olefin sulfonate and (B-2) component together, the dispersion removal effect of biofilm can be significantly improved, and the bitterness of (A) component can be suppressed, and foaming property can be imparted suitably.
这种情况下,(A)成分与上述第I发明相同。In this case, (A) component is the same as the said 1st invention.
第II发明中使用的(B)成分两性表面活性剂(B-2),通过与(A)成分并用,口腔生物膜的分散除去效果显著提高,此外,抑制苦味,赋予适当的起泡性。The (B) component amphoteric surfactant (B-2) used in the second invention is used in combination with (A) component to remarkably improve the dispersion and removal effect of oral biofilm, and to suppress bitterness and impart appropriate foaming properties.
作为两性表面活性剂,可以使用甜菜碱系,例如脂肪酸酰胺烷基甜菜碱、咪唑啉鎓甜菜碱、氨基乙酸甜菜碱。其中,脂肪酸的碳原子数为8~18,优选烷基的碳原子数为1~5的脂肪酸酰胺烷基甜菜碱,更优选脂肪酸酰胺丙基甜菜碱。作为这样的脂肪酸酰胺丙基甜菜碱,可以使用外原规(医药部外品原料标准)记载的椰油脂肪酸酰胺丙基甜菜碱。As the amphoteric surfactant, betaines such as fatty acid amidoalkyl betaines, imidazolinium betaines, and glycine betaines can be used. Among them, the fatty acid has 8 to 18 carbon atoms, preferably a fatty acid amidoalkyl betaine having an alkyl group of 1 to 5 carbon atoms, and more preferably a fatty acid amidopropyl betaine. As such a fatty acid amidopropyl betaine, coco fatty acid amidopropyl betaine described in the foreign standard (Standards for Quasi-Drug Raw Materials) can be used.
两性表面活性剂可以是能够获取的能用于口腔用制剂的市售品。具体地,作为椰油脂肪酸酰胺丙基甜菜碱,可列举市售的商品名称TEGOBetainCKOK(EVONIK公司制)。As the amphoteric surfactant, commercially available ones that can be used in oral preparations may be used. Specifically, as coco fatty acid amidopropyl betaine, commercially available brand name TEGO Betain CKOK (made by EVONIK company) is mentioned.
第II发明中,(A)成分与(B-2)成分的混合比例在特定范围时,口腔生物膜除去效果更优异。这种情况下,优选(A)/(B-2)比以质量比计为0.2~8,更优选为0.4~5,进一步优选为0.4~4,特别优选为0.5~3.1。在上述比例范围内时,生物膜除去效果更优异。此外,从赋予更加良好的起泡,进一步抑制苦味的方面考虑,优选8以下。In the second invention, when the mixing ratio of (A) component and (B-2) component is in a specific range, the effect of removing oral biofilm is more excellent. In this case, the (A)/(B-2) ratio is preferably 0.2 to 8 by mass ratio, more preferably 0.4 to 5, still more preferably 0.4 to 4, particularly preferably 0.5 to 3.1. Within the range of the above ratio, the biofilm removal effect is more excellent. Moreover, it is preferably 8 or less from the viewpoint of imparting better foaming and further suppressing bitterness.
本发明,特别是第II发明,优选进一步混合(C)季铵盐,混合(C)季铵盐时,口腔生物膜的分散除去效果进一步提高。此外,起泡进一步提高。In the present invention, especially in the second invention, it is preferable to further mix the (C) quaternary ammonium salt. When the (C) quaternary ammonium salt is mixed, the effect of dispersing and removing oral biofilm is further improved. In addition, foaming is further improved.
作为(C)成分的季铵盐,可列举西吡氯铵、苯扎氯铵、苄索氯铵等,这些可以使用1种或使用2种以上,特别是从生物膜除去效果的方面考虑,更优选西吡氯铵。As the quaternary ammonium salt of the (C) component, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, etc. can be mentioned, and these can be used alone or in two or more kinds, especially from the aspect of biofilm removal effect, More preferred is cetylpyridinium chloride.
混合(C)成分时,从提高生物膜除去效果的观点考虑,优选(A)/(C)以质量比计在10~500的范围内进行混合。When mixing (C)component, it is preferable to mix (A)/(C) within the range of 10-500 by mass ratio from a viewpoint of improving biofilm removal effect.
本发明,特别是第II发明,优选进一步混合(D)木糖醇和/或赤藓糖醇,混合(D)木糖醇和/或赤藓糖醇时,口腔生物膜的分散除去效果进一步提高。另外,作为(D)成分,可以单独混合木糖醇或赤藓糖醇,也可以混合木糖醇以及赤藓糖醇。In the present invention, especially in the second invention, it is preferable to further mix (D) xylitol and/or erythritol. When (D) xylitol and/or erythritol are mixed, the effect of dispersing and removing oral biofilm is further improved. Moreover, as (D)component, xylitol or erythritol may be mixed independently, and xylitol and erythritol may be mixed.
混合(D)成分时,从提高生物膜除去效果的观点考虑,优选(A)/(D)以质量比计在0.01~5的范围内进行混合。When mixing (D) component, it is preferable to mix (A)/(D) in the range of 0.01-5 in mass ratio from a viewpoint of improving biofilm removal effect.
第I发明的口腔生物膜除去剂可以适当地混合到口腔用组合物中。这种情况下,第I发明的口腔用组合物中,(A)成分的混合量优选为组合物整体的0.3~5%(质量%,下同。),更优选0.5~5.0%。混合量越多,生物膜除去效果越高,在0.3%以上时,能赋予充分的生物膜除去效果。此外,能够赋予良好的起泡性。在5%以下时,苦味不会变强,在使用上优选。The oral biofilm removing agent of the first invention can be appropriately mixed with the oral composition. In this case, in the oral composition of the first invention, the compounding amount of the component (A) is preferably 0.3 to 5% (mass%, the same below) of the entire composition, more preferably 0.5 to 5.0%. The larger the blending amount, the higher the biofilm removal effect, and at 0.3% or more, a sufficient biofilm removal effect can be imparted. In addition, good foamability can be imparted. When it is 5% or less, the bitterness does not become strong, which is preferable in use.
此外,第I发明的口腔用组合物中,(B-1)成分的混合量优选为组合物整体的0.1~5%,更优选0.2~5%,进一步优选0.3~5%。(B-1)成分的混合量越多,生物膜除去效果越高,但从得到抑制苦味,赋予良好的起泡,得到使用上优选的材料方面考虑,优选5%以下。In addition, in the oral composition of the first invention, the compounding amount of the component (B-1) is preferably 0.1 to 5%, more preferably 0.2 to 5%, and even more preferably 0.3 to 5% of the entire composition. (B-1) The larger the compounding amount of the component, the higher the biofilm removal effect, but it is preferably 5% or less from the viewpoint of suppressing bitterness, imparting good foaming, and obtaining a material suitable for use.
第II发明的口腔生物膜除去剂适宜混合于口腔用组合物中,其含有(A)α-烯烃磺酸盐和作为(B)成分的两性表面活性剂(B-2),进一步优选含有(C)季铵盐,此外进一步优选含有(D)木糖醇和/或赤藓糖醇。特别地若为含有(A)成分、(B-2)成分,进一步优选含有(C)成分的洁齿剂组合物,或者含有(A)成分、(B-2)成分,进一步优选含有(D)成分的漱口水组合物时,口腔生物膜除去效果进一步提高。The oral biofilm removing agent of the second invention is preferably mixed in a composition for oral cavity, which contains (A) α-olefin sulfonate and amphoteric surfactant (B-2) as (B) component, and more preferably contains ( C) The quaternary ammonium salt further preferably contains (D) xylitol and/or erythritol. Particularly if it is a dentifrice composition containing (A) component, (B-2) component, more preferably containing (C) component, or containing (A) component, (B-2) component, more preferably containing (D ) components, the oral biofilm removal effect is further improved.
第II发明的口腔用组合物中,(A)成分的混合量优选为组合物整体的0.1~3%。这种情况下,特别是洁齿剂组合物中,优选混合(A)成分0.3~3%,特别优选混合0.5~2.5%。此外,漱口水组合物中,优选混合(A)成分0.1~3%,特别优选混合0.1~2.5%,尤其优选混合0.1~1%。混合量越多,生物膜除去效果越高,在0.1%以上时,能赋予充分的生物膜除去效果。此外,能够赋予良好的起泡性。在3%以下时,苦味不会变强,在使用上优选。In the composition for oral cavity of 2nd invention, it is preferable that the compounding quantity of (A) component is 0.1-3% of the whole composition. In this case, especially in the dentifrice composition, it is preferable to mix (A) component 0.3-3%, and it is especially preferable to mix 0.5-2.5%. Moreover, in a mouthwash composition, it is preferable to mix (A) component 0.1-3%, especially preferably 0.1-2.5%, and especially preferably mix 0.1-1%. The larger the blending amount, the higher the biofilm removal effect, and at 0.1% or more, a sufficient biofilm removal effect can be imparted. In addition, good foamability can be imparted. When it is 3% or less, the bitterness does not become strong, which is preferable in use.
此外,第II发明的口腔用组合物中,(B-2)成分的混合量优选为组合物整体的0.05~5%,特别优选为0.1~5%,更优选为0.3~5%,进一步优选0.5~3%。(B-2)成分的混合量越多,生物膜除去效果越高,此外赋予良好的起泡,但为了不产生苦味,优选在5%以下。In addition, in the oral composition of the second invention, the compounding amount of the component (B-2) is preferably 0.05 to 5% of the entire composition, particularly preferably 0.1 to 5%, more preferably 0.3 to 5%, and even more preferably 0.5-3%. (B-2) The larger the compounding amount of the component, the higher the biofilm removal effect and impart good foaming, but it is preferably 5% or less in order not to generate bitterness.
混合(C)季铵盐时,特别是在第II发明中涉及的洁齿剂组合物中,其混合量优选组合物整体的0.003~0.05%,更优选0.005~0.01%。混合量越多,生物膜除去效果越高。为了不产生季铵盐的粘膜刺激,优选0.05%以下。When mixing (C) quaternary ammonium salt, especially in the dentifrice composition which concerns on II invention, the compounding quantity becomes like this. Preferably it is 0.003-0.05% of the whole composition, More preferably, it is 0.005-0.01%. The more the mixing amount, the higher the biofilm removal effect. In order not to cause mucosal irritation of the quaternary ammonium salt, it is preferably 0.05% or less.
混合(D)木糖醇和/或赤藓糖醇时,特别是在第II发明涉及的漱口水组合物中,优选其混合量为组合物整体的0.1~2%,更优选为0.3~1%。混合量越多生物膜除去效果越高。为了不产生苦味,优选在2%以下。When mixing (D) xylitol and/or erythritol, especially in the mouthwash composition according to the second invention, the mixing amount is preferably 0.1 to 2%, more preferably 0.3 to 1% of the entire composition . The larger the mixing amount, the higher the biofilm removal effect. In order not to produce a bitter taste, it is preferably 2% or less.
本发明的口腔用组合物可以制备成液体、液状、膏状等的形态,可以通过通常的方法制备成牙膏、液体洁齿剂、液状洁齿剂、润制牙粉(潤製歯磨)等洁齿剂,漱口水等。The oral composition of the present invention can be prepared in the form of liquid, liquid, paste, etc., and can be prepared into toothpaste, liquid dentifrice, liquid dentifrice, moisturizing tooth powder (moisturizing dentifrice), etc. medicine, mouthwash, etc.
这种情况下,除上述成分以外,还可以根据需要在不损害本发明的效果的范围内按照剂型混合其它任意成分。具体地,洁齿剂的情况下可以混合研磨剂、粘合剂、增稠剂、表面活性剂、甜味剂、防腐剂、香料、色素、各种有效成分、水等的溶剂、pH调节剂等。此外,漱口水的情况下可以混合润湿剂、表面活性剂、溶剂、pH调节剂、防腐剂、杀菌剂、香料、甜味剂、色素、各种有效成分等。In this case, in addition to the above-mentioned components, other arbitrary components may be mixed according to the dosage form as needed within the range not impairing the effect of the present invention. Specifically, in the case of dentifrices, abrasives, binders, thickeners, surfactants, sweeteners, preservatives, fragrances, coloring agents, various active ingredients, solvents such as water, and pH adjusters can be mixed. Wait. In addition, in the case of mouthwash, wetting agents, surfactants, solvents, pH adjusters, preservatives, bactericides, fragrances, sweeteners, coloring agents, and various active ingredients can be mixed.
以下显示任意成分的具体例子,但本发明的组合物中能混合的成分并不局限于这些成分。Specific examples of optional components are shown below, but the components that can be mixed in the composition of the present invention are not limited to these components.
作为研磨剂,可列举晶态二氧化硅、非晶态二氧化硅、硅胶、硅酸铝等二氧化硅系研磨剂,沸石、无水磷酸氢钙、二水合磷酸氢钙、焦磷酸钙、碳酸钙、氢氧化铝、氧化铝、碳酸镁、磷酸三镁、硅酸锆、磷酸三钙、羟基磷灰石、磷酸四钙、合成树脂系研磨剂等。洁齿剂的情况下,这些研磨剂通常可以混合组合物整体的5~70%,特别是可以混合组合物整体的10~50%。As the abrasive, silica-based abrasives such as crystalline silica, amorphous silica, silica gel, and aluminum silicate, zeolite, anhydrous calcium hydrogen phosphate, dihydrate calcium hydrogen phosphate, calcium pyrophosphate, Calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, trimagnesium phosphate, zirconium silicate, tricalcium phosphate, hydroxyapatite, tetracalcium phosphate, synthetic resin abrasives, etc. In the case of a dentifrice, these abrasives may be mixed generally at 5 to 70% of the entire composition, particularly at 10 to 50% of the entire composition.
作为粘合剂,可列举普鲁兰多糖、明胶、甲基纤维素、羟乙基纤维素、羟丙基纤维素、羧甲基纤维素钠、卡拉胶、海藻酸钠、黄原胶、聚丙烯酸钠、阿拉伯胶、瓜尔胶、刺槐豆胶、聚乙烯醇、聚乙烯吡咯烷酮等,可以单独使用1种或组合2种以上使用。这些粘合剂通常可以混合组合物整体的0~10%,特别是0.1~5%。Examples of binders include pullulan, gelatin, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, carrageenan, sodium alginate, xanthan gum, poly Sodium acrylate, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, polyvinylpyrrolidone, etc. may be used alone or in combination of two or more. These binders can usually be mixed in an amount of 0 to 10%, especially 0.1 to 5%, of the whole composition.
作为增稠剂(湿润剂),可列举山梨糖醇或、丙二醇、丁二醇、甘油、聚乙二醇等多元醇。这些增稠剂的混合量通常为组合物整体的0~70%,特别是3~50%。Examples of the thickener (humectant) include polyhydric alcohols such as sorbitol, propylene glycol, butylene glycol, glycerin, and polyethylene glycol. The compounding quantity of these thickeners is 0-70% of the whole composition normally, especially 3-50%.
作为表面活性剂,可以混合(A)成分以外的阴离子性表面活性剂、非离子性表面活性剂,例如,可以使用烷基硫酸盐、甘油脂肪酸酯的硫酸盐等阴离子性表面活性剂,聚氧乙烯烷基醚、聚氧乙烯-聚氧丙烯嵌段共聚物、聚氧乙烯氢化蓖麻油、聚氧乙烯甘油脂肪酸酯、蔗糖脂肪酸酯、脂肪酸烷基醇酰胺等非离子性表面活性剂。这些表面活性剂可以使用1种或2种以上,通常可以混合组合物整体的0~10%,特别是0.1~5%。此外,(A)成分以外的阴离子性表面活性剂的混合量可以是0%,混合的情况下,优选0.1~1.5%,特别优选0.1~1.0%。As the surfactant, anionic surfactants and nonionic surfactants other than the (A) component can be mixed, for example, anionic surfactants such as alkyl sulfates and glycerin fatty acid ester sulfates can be used, poly Oxyethylene alkyl ether, polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene hydrogenated castor oil, polyoxyethylene glycerin fatty acid ester, sucrose fatty acid ester, fatty acid alkylolamide and other nonionic surfactants . One or more of these surfactants can be used, and usually 0 to 10% of the entire composition, particularly 0.1 to 5%, can be mixed. Moreover, although the compounding quantity of the anionic surfactant other than (A) component may be 0%, when compounding, 0.1-1.5% is preferable, and 0.1-1.0% is especially preferable.
作为甜味剂,可列举糖精钠、甜菊糖、新橙皮苷二氢查耳酮等。作为防腐剂,可以混合苯甲酸钠、对羟基苯甲酸甲酯、对羟基苯甲酸乙酯等对羟基苯甲酸酯等。Examples of sweeteners include sodium saccharin, stevioside, neohesperidin dihydrochalcone, and the like. As a preservative, parabens such as sodium benzoate, methyl paraben, and ethyl paraben can be mixed.
作为香料,可以组合使用椒样薄荷油(ペパーミント油)、绿薄荷油、茴香油、桉叶油、冬青油、肉桂油、丁香油、百里香油、鼠尾草油、柠檬油、橙油、薄荷油(ハッカ油)、小豆蔻油、芫荽油、橘皮油、酸橙油、熏衣草油、迷迭香油、月桂油、洋甘菊油、藏茴香油、马郁兰油、月桂油、柠檬草油、牛至油、松针油、橙花油、玫瑰油、茉莉油、葡萄柚油、白金柚油(スウィーティー油)、柚油、鸢尾浸膏、椒样薄荷精油、玫瑰精油、橙花等天然香料,以及对这些天然香料进行加工处理(除前馏分、除后馏分、分馏、液液提取、精炼、香料粉末处理)得到的香料,以及l-薄荷醇、香芹酮、茴香脑、桉叶油素、水杨酸甲酯、肉桂醛、丁子香酚、3-l-薄荷氧基丙烷-1,2-二醇、百里酚、芳樟醇、乙酸芳樟酯、柠檬烯、薄荷酮、乙酸薄荷酯、N-取代-对薄荷烷-3-甲酰胺、蒎烯、辛醛、柠檬醛、胡薄荷酮、乙酸香芹酯、茴香醛、乙酸乙酯、丁酸乙酯、环己基丙酸烯丙酯、邻氨基苯甲酸甲酯、甲基苯基环氧丙酸乙酯、香草醛、十一烷酸内酯、己醛、丁醇、异戊醇、己烯醇、二甲基硫醚、甲基环戊烯醇酮、糠醛、三甲基吡嗪、乳酸乙酯、硫代乙酸乙酯等单种香料,还有,草莓味、苹果味、香蕉味、菠萝味、葡萄味、芒果味、黄油味、奶味、水果混合味、热带水果味等调配香料等能用于口腔用组合物的公知的香料材料。As spices, peppermint oil (peppermint oil), spearmint oil, fennel oil, eucalyptus oil, wintergreen oil, cinnamon oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, peppermint can be used in combination Oil (Hacka Oil), Cardamom Oil, Coriander Oil, Orange Peel Oil, Lime Oil, Lavender Oil, Rosemary Oil, Bay Oil, Chamomile Oil, Fennel Oil, Marjoram Oil, Laurel Oil, Lemongrass Oil, Oregano oil, pine needle oil, neroli oil, rose oil, jasmine oil, grapefruit oil, platinum pomelo oil (スウィーティー oil), pomelo oil, iris extract, peppermint essential oil, rose essential oil, orange blossom and other natural fragrances, And the spices obtained by processing these natural flavors (removing the front fraction, removing the rear fraction, fractionation, liquid-liquid extraction, refining, spice powder treatment), and l-menthol, carvone, anethole, eucalyptol , methyl salicylate, cinnamaldehyde, eugenol, 3-l-menthoxypropane-1,2-diol, thymol, linalool, linalyl acetate, limonene, menthone, menthyl acetate Esters, N-substituted-p-menthane-3-carboxamides, pinene, octanal, citral, pulegone, carvyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, cyclohexylpropionate Propyl ester, Methyl anthranilate, Ethyl methyl phenylglycidate, Vanillin, Undecanolide, Hexanal, Butanol, Isoamyl alcohol, Hexenol, Dimethyl sulfide , methylcyclopentenolone, furfural, trimethylpyrazine, ethyl lactate, ethyl thioacetate and other single flavors, as well as strawberry, apple, banana, pineapple, grape, mango Known flavoring materials that can be used in oral compositions such as flavoring, buttery flavoring, milky flavoring, fruit blend flavoring, tropical fruity flavoring and the like.
作为色素,可以根据目标色调使用能使用于口腔用组合物的色素。作为食用色素,例如可列举艳蓝、酒石黄等,作为颜料可列举氧化钛等。As a coloring matter, what can be used for an oral composition can be used according to the target color tone. Examples of food colorings include brilliant blue, tartrazine, and the like, and examples of pigments include titanium oxide and the like.
作为有效成分(药用成分),可以在药剂学容许的范围内有效量使用例如氯己定、三氯生、异丙基甲基苯酚、葡萄糖酸锌,柠檬酸锌等杀菌或抑菌剂,乙烷羟基二磷酸酯等牙结石预防剂,氨甲环酸、甘草酸及其盐、尿囊素碱式氯化铝等抗炎剂,氟化钠、单氟磷酸钠等氟化物,羟乙基纤维素二甲基二烯丙基氯化铵等涂覆剂,葡聚糖酶、变位酶、氯化溶菌酶等酶剂,抗坏血酸、醋酸生育酚等维生素类,氯化钠等收敛剂,乳酸铝、氯化锶、硝酸钾等感觉过敏抑制剂,氟化钠、单氟磷酸钠、氟化亚锡等氟化物等。As active ingredients (medicinal ingredients), bactericidal or bacteriostatic agents such as chlorhexidine, triclosan, isopropylmethylphenol, zinc gluconate, and zinc citrate can be used in an effective amount within the scope of pharmacy, Dental calculus preventive agents such as ethanehydroxy diphosphate, anti-inflammatory agents such as tranexamic acid, glycyrrhizic acid and its salts, allantoin basic aluminum chloride, fluorides such as sodium fluoride and sodium monofluorophosphate, hydroxyethyl Coating agents such as cellulose dimethyl diallyl ammonium chloride, enzyme agents such as dextranase, mutase, and lysozyme chloride, vitamins such as ascorbic acid and tocopheryl acetate, and astringent agents such as sodium chloride , Aluminum lactate, strontium chloride, potassium nitrate and other hypersensitivity inhibitors, sodium fluoride, sodium monofluorophosphate, stannous fluoride and other fluorides, etc.
此外,作为溶剂可以混合乙醇、水等。Moreover, ethanol, water, etc. can be mixed as a solvent.
口腔用组合物为洁齿剂组合物时,优选溶剂为水,优选水的含量为组合物整体的60%以下。此外,口腔用组合物为漱口水组合物的情况,优选溶剂为水,或水和乙醇的混合溶剂,优选乙醇为组合物整体的10%以下。When the oral composition is a dentifrice composition, the solvent is preferably water, and the water content is preferably 60% or less of the entire composition. Furthermore, when the oral composition is a mouthwash composition, the solvent is preferably water or a mixed solvent of water and ethanol, and ethanol is preferably 10% or less of the entire composition.
组合物的pH可以为通常的口腔用组合物的范围,但优选25℃时的pH为5.5~8.5,更优选6~8。另外,可以根据需要使用pH调节剂调节pH,作为pH调节剂可列举氢氧化钠、盐酸、碳酸钠、碳酸氢钠、硼酸或其盐等,其中,适宜为氢氧化钠、氢氧化钾、盐酸。这些pH调节剂的混合量只要能将pH值调节至上述范围内即可。The pH of the composition may be within the range of common oral compositions, but the pH at 25°C is preferably 5.5-8.5, more preferably 6-8. In addition, the pH can be adjusted using a pH adjuster as needed, and examples of the pH adjuster include sodium hydroxide, hydrochloric acid, sodium carbonate, sodium bicarbonate, boric acid, or salts thereof, among which sodium hydroxide, potassium hydroxide, hydrochloric acid, and the like are suitable. . The compounding quantity of these pH adjusters should just be able to adjust pH to the said range.
[实施例][Example]
以下,显示实施例以及比较例、处方例,具体地说明本发明,但本发明并不局限于下述实施例。另外,在下述例子中%在没有特别限定时都表示质量%。Hereinafter, although an Example, a comparative example, and a formulation example are shown, and this invention is concretely demonstrated, this invention is not limited to a following example. In addition, in the following examples, % represents mass % unless there is a particular limitation.
[实施例I、比较例I][Example 1, Comparative Example 1]
按照下述所示的方法制备表1、2所示组分的洁齿剂组合物,用下述方法评价。结果一并记载于表1、2中。Dentifrice compositions with the components shown in Tables 1 and 2 were prepared according to the methods shown below, and evaluated by the following methods. The results are recorded in Tables 1 and 2 together.
洁齿剂组合物的制备方法:The preparation method of dentifrice composition:
首先,在常温下将(B-1)成分缩聚磷酸盐、所用的水溶性成分混合于含有山梨糖醇液等增稠剂的纯化水中后,进一步混合粘合剂、稳定剂,用分散机进行分散。在捏合机中加入分散液、研磨剂混合后,加入香料、(A)成分α-烯烃磺酸盐。将捏合机内减压至大约5kPa而进行脱泡,进一步继续混合得到洁齿剂组合物。另外,比较例的组合物按照上述方法进行制备。First, mix the polycondensed phosphate of the component (B-1) and the water-soluble components used in purified water containing a thickener such as sorbitol liquid at room temperature, and then further mix a binder and a stabilizer, and carry out the process with a disperser. dispersion. Add the dispersion liquid and the grinding agent to the kneader and mix, then add the fragrance and (A) component α-olefin sulfonate. The inside of the kneader was depressurized to about 5 kPa to defoam, and further mixing was continued to obtain a dentifrice composition. In addition, the composition of the comparative example was prepared according to the above-mentioned method.
<口腔生物膜除去效果的评价方法><Evaluation method of oral biofilm removal effect>
(1)模型生物膜的制作方法(1) Preparation method of model biofilm
将直径7mm×厚3.5mm的羟基磷灰石(HA)板(旭光学株式会社制),用经0.45μm过滤器过滤的人无刺激唾液处理4小时,用作模型生物膜制作的载体,培养液使用最小缓冲甲醇(ベイサルメディウムムチン)培养液(BMM)*1。用于制作模型生物膜的菌株使用从美国典型培养物保藏中心(AmericanTypeCultureCollection)购入的粘性放线菌(Actinomycesviscosus)ATCC43146、小韦荣氏球菌(Veillonellaparvula)ATCC17745、核梭杆菌(Fusobacteriumnucleatum)ATCC10953、口腔链球菌(Streptococcusoralis)ATCC10557、变形链球菌(Streptococcusmutans)ATCC25175。将这5种菌株分别以1×107cfu/mL(cfu:菌落形成单位)的方式接种到预先加入有BMM3000mL的旋转圆盘反应器(培养槽)中,与经唾液处理过的HA载体一起在37℃、厌氧条件下(5vol%二氧化碳,95vol%氮)培养24小时。然后,在相同的条件下以置换率5vol%/小时的比例连续供给BMM培养基培养10天,在HA表面形成5种菌种混合的模型生物膜。A hydroxyapatite (HA) plate (manufactured by Asahi Optical Co., Ltd.) with a diameter of 7 mm x a thickness of 3.5 mm was treated with human non-irritating saliva filtered through a 0.45 μm filter for 4 hours, used as a carrier for the production of a model biofilm, and cultured As the medium, minimally buffered methanol (Beisal Medium) culture medium (BMM) *1 was used. The strains used to make the model biofilm were Actinomyces viscosus ATCC43146, Veillonella parvula ATCC17745, Fusobacterium nucleatum ATCC10953 purchased from the American Type Culture Collection. Streptococcus (Streptococcus oralis) ATCC10557, Streptococcus mutans (Streptococcusmutans) ATCC25175. These five strains were inoculated at 1×10 7 cfu/mL (cfu: colony forming unit) into a rotating disk reactor (culture tank) pre-filled with 3000 mL of BMM, together with the HA carrier treated with saliva Cultivate at 37° C. under anaerobic conditions (5 vol% carbon dioxide, 95 vol% nitrogen) for 24 hours. Then, under the same conditions, the BMM medium was continuously supplied with a replacement rate of 5 vol%/hour for 10 days, and a model biofilm in which 5 strains were mixed was formed on the surface of HA.
(2)模型生物膜的除去效果(2) Removal effect of model biofilm
将形成的模型生物膜转移到24孔多孔板(住友电木公司(住友ベークライト社)制),加入2mL制备的洁齿剂组合物(利用采集自健康人的唾液稀释3倍的离心上清液(10000rpm,10分钟)),浸渍3分钟(将未加入洁齿剂组合物的组作为对照样品)。然后用PBS(和光纯药工业公司制)1mL洗涤6次,在添加有相同的PBS2mL的试管(直径13mm×10mm)内通过超声波处理(200μA,10秒)进行分散。测定该分散液在波长550nm的浑浊度(OD),从而测定生物膜残存量。The formed model biofilm was transferred to a 24-well multiwell plate (manufactured by Sumitomo Bakelite Co., Ltd.), and 2 mL of the prepared dentifrice composition (centrifuged supernatant diluted 3-fold with saliva collected from a healthy person) was added. (10000rpm, 10 minutes)), dipped for 3 minutes (the group without adding the dentifrice composition was used as a control sample). Then, it was washed 6 times with 1 mL of PBS (manufactured by Wako Pure Chemical Industries, Ltd.), and dispersed by ultrasonic treatment (200 μA, 10 seconds) in a test tube (diameter 13 mm×10 mm) to which 2 mL of the same PBS was added. The turbidity (OD) of the dispersion liquid at a wavelength of 550 nm was measured to measure the remaining amount of biofilm.
试验组合物的生物膜除去效果,通过下式求出相对于对照组的除去率,按照下述基准从该除去率判定口腔生物膜除去效果。For the biofilm removal effect of the test composition, the removal rate relative to the control group was obtained from the following formula, and the oral biofilm removal effect was judged from the removal rate according to the following criteria.
生物膜除去率(%)=(对照组的浑浊度-试验组合物的浑浊度)/对照组的浑浊度×100Biofilm removal rate (%)=(turbidity of control group-turbidity of test composition)/turbidity of control group×100
口腔生物膜除去效果的判定基准Criteria for judging the effect of oral biofilm removal
◎◎:生物膜除去率在95%以上◎◎: Biofilm removal rate is above 95%
◎:生物膜除去率在90%以上小于95%◎: Biofilm removal rate is above 90% and less than 95%
○:生物膜除去率在80%以上小于90%○: Biofilm removal rate is above 80% and less than 90%
△:生物膜除去率在70%以上小于80%△: Biofilm removal rate is above 70% and less than 80%
×:生物膜除去率在50%以上小于70%×: Biofilm removal rate is above 50% and less than 70%
××:生物膜除去率小于50%××: Biofilm removal rate is less than 50%
*1BMM的组分:用1升中的质量表示。 *1 Composition of BMM: Expressed by mass in 1 liter.
蛋白胨(BectonandDickinson公司制):4g/LPeptone (manufactured by Becton and Dickinson): 4g/L
胰蛋白胨(BectonandDickinson公司制):2g/LTryptone (manufactured by Becton and Dickinson): 2g/L
酵母抽提物(BectonandDickinson公司制):2g/LYeast extract (manufactured by Becton and Dickinson): 2g/L
粘蛋白(Sigma公司制):5g/LMucin (manufactured by Sigma): 5g/L
氯化血红素(Sigma公司制):2.5mg/LHemin (manufactured by Sigma): 2.5 mg/L
维生素K(和光纯药工业公司制):0.5mg/LVitamin K (manufactured by Wako Pure Chemical Industry Co., Ltd.): 0.5 mg/L
KCl(和光纯药工业公司制):1g/LKCl (manufactured by Wako Pure Chemical Industry Co., Ltd.): 1g/L
半胱氨酸(和光纯药工业公司制):0.2g/LCysteine (manufactured by Wako Pure Chemical Industries Ltd.): 0.2g/L
蒸馏水:余量(以总量达到1L的方式进行定容,在121℃下高压灭菌器处理20分钟。)Distilled water: remaining amount (constant volume so that the total amount reaches 1L, and autoclave at 121°C for 20 minutes.)
<苦昧的有无以及起泡的优劣的评价方法><How to evaluate the presence or absence of bitterness and the quality of foaming>
表中所示的洁齿剂组合物的苦味的有无以及起泡的优劣通过下述方法进行感官评价。The presence or absence of bitterness and the quality of foaming of the dentifrice compositions shown in the table were sensory evaluated by the following methods.
取洁齿剂组合物1g至牙刷上,刷牙3分钟根据下述评分基准进行评价。由6名评价者基于下述评价基准评价苦味的有无以及起泡的优劣。Take 1 g of the dentifrice composition on the toothbrush, brush your teeth for 3 minutes, and evaluate according to the following scoring criteria. The presence or absence of bitterness and the quality of foaming were evaluated by 6 evaluators based on the following evaluation criteria.
苦味的有无presence or absence of bitterness
评价基准Evaluation benchmark
5:未感觉到苦味5: Bitterness is not sensed
4:几乎感觉不到苦味4: Almost no bitterness is felt
3:稍微感觉到苦昧3: feel a little bitter
2:感觉到苦昧2: feel bitter
1:感觉到强劲的苦昧1: Feel strong bitterness
评价基准Evaluation benchmark
◎:平均值在4分以上5分以下◎: The average value is between 4 and 5
○:平均值在3分以上小于4分○: The average value is more than 3 points and less than 4 points
△:平均值在2分以上小于3分△: The average value is more than 2 points and less than 3 points
×:平均值在1分以上小于2分×: The average value is more than 1 point and less than 2 points
起泡的优劣Advantages and disadvantages of foaming
评价基准Evaluation benchmark
5:起泡非常良好5: Very good foaming
4:起泡略好4: slightly better foaming
3:起泡一般3: Moderate foaming
2:起泡稍差2: slightly poor foaming
1:起泡很差1: Poor foaming
评价基准Evaluation Benchmark
◎:平均值在4分以上5分以下◎: The average value is between 4 and 5
○:平均值在3分以上小于4分○: The average value is more than 3 points and less than 4 points
△:平均值在2分以上小于3分△: The average value is more than 2 points and less than 3 points
×:平均值在1分以上小于2分×: The average value is more than 1 point and less than 2 points
使用原料的详细说明如下所示。Detailed instructions for using raw materials are given below.
(A)成分(A) Ingredients
十四烯磺酸钠(α-烯烃(C14)磺酸钠):狮王株式会社制Sodium tetradecene sulfonate (sodium α-olefin (C14) sulfonate): manufactured by Lion Corporation
(B)成分(B) Ingredients
(B-1)三聚磷酸钠:太平化学产业株式会社制(B-1) Sodium tripolyphosphate: Taihei Chemical Industry Co., Ltd. make
(B-1)焦磷酸钠:太平化学产业株式会社制(B-1) Sodium pyrophosphate: Taihei Chemical Industry Co., Ltd. make
(B-1)焦磷酸钾:太平化学产业株式会社制(B-1) Potassium pyrophosphate: manufactured by Taihei Chemical Industry Co., Ltd.
【表1】【Table 1】
【表2】【Table 2】
[实施例II、比较例II][Example II, Comparative Example II]
按照下述所示的方法制备表3~6所示组分的口腔用组合物(表3、4为洁齿剂组合物,表5、6为漱口水组合物),用与上述相同的方法进行评价。结果一并记载于表3~6中。Prepare the oral composition of the components shown in Tables 3 to 6 according to the method shown below (Tables 3 and 4 are dentifrice compositions, and Tables 5 and 6 are mouthwash compositions), using the same method as above Make an evaluation. The results are also described in Tables 3-6.
另外,用下述方法对漱口水组合物的苦味的有无以及起泡的优劣进行感官评价。In addition, sensory evaluation was performed for the presence or absence of bitterness and the quality of foaming of the mouthwash composition by the following methods.
将漱口水10mL含入口中洗漱20秒,基于上述评分基准判定漱口时的苦味的有无。基于上述评价基准根据6名评价者的平均进行评价。10 mL of mouthwash was contained in the mouth and swished for 20 seconds, and the presence or absence of bitterness at the time of gargling was judged based on the above scoring criteria. Evaluation was performed based on the average of 6 evaluators based on the above evaluation criteria.
洁齿剂组合物的制备方法:The preparation method of dentifrice composition:
首先,在常温下将氟化钠等所用的水溶性成分混合于含有山梨糖醇液等的增稠剂的纯化水中,然后进一步地同时混合粘合剂与(B-2)成分,进一步混合(C)成分,用分散机进行分散。在捏合机中加入上述分散液、研磨剂等的粉体混合后,加入香料、(A)成分。将捏合机内减压至大约5kPa而进行脱泡,进一步继续混合得到洁齿剂组合物。First, water-soluble components such as sodium fluoride are mixed with purified water containing thickeners such as sorbitol liquid at room temperature, and then the binder and (B-2) components are further mixed at the same time, and further mixed ( C) Components are dispersed with a disperser. Add the above-mentioned dispersion liquid, abrasive powder, etc. powder to the kneader and mix, then add fragrance and (A) component. The inside of the kneader was depressurized to about 5 kPa to defoam, and further mixing was continued to obtain a dentifrice composition.
漱口剂组合物的制备方法:The preparation method of mouthwash composition:
漱口水组合物的制备,依次将(A)成分、(B-2)成分、(D)成分以及其他原料加入到纯化水中搅拌使其均一溶解。另外,制造中使用三合一电机(スリーワンモーター)(BL1200,HEIDON公司制)。In preparation of the mouthwash composition, (A) component, (B-2) component, (D) component and other raw materials are sequentially added to purified water and stirred to dissolve uniformly. In addition, a three-in-one motor (BL1200, manufactured by HEIDON Corporation) was used in the production.
比较例的洁齿剂组合物、漱口水组合物按照上述方法进行制备。The dentifrice composition and the mouthwash composition of the comparative example were prepared according to the above-mentioned method.
使用原料的详细说明如下所示。Detailed instructions for using raw materials are given below.
(A)成分(A) Ingredients
十四烯磺酸钠(α-烯烃(C14)磺酸钠):狮王株式会社制Sodium tetradecene sulfonate (sodium α-olefin (C14) sulfonate): manufactured by Lion Corporation
(B)成分(B) Ingredients
(B-2)椰油脂肪酸酰胺丙基甜菜碱:30%品(各例中的混合量为纯含量),TEGOBetainCKOK,EVONIK株式会社制(B-2) Coco fatty acid amidopropyl betaine: 30% product (the mixing amount in each example is the pure content), TEGO Betain CKOK, manufactured by EVONIK Co., Ltd.
(B-2)咪唑啉鎓甜菜碱:日光化学株式会社(日光ケミカルズ(株))制(B-2) imidazolinium betaine: manufactured by Nikko Chemicals Co., Ltd.
(B-2)氨基乙酸甜菜碱:日光化学株式会社制(B-2) Glycine betaine: manufactured by Nikko Chemical Co., Ltd.
(C)西吡氯铵:和光纯药工业株式会社制(C) Cetylpyridinium chloride: manufactured by Wako Pure Chemical Industries, Ltd.
(C)苯扎氯铵:和光纯药工业株式会社制(C) Benzalkonium chloride: manufactured by Wako Pure Chemical Industries, Ltd.
(C)苄索氯铵:日油株式会社制(C) Benzethonium chloride: manufactured by NOF Corporation
(D)木糖醇:ROCKET日本株式会社(ロケットジャパン(株))制(D) Xylitol: manufactured by ROCKET JAPAN CO., LTD.
(D)赤藓糖醇:和光纯药工业株式会社制(D) Erythritol: manufactured by Wako Pure Chemical Industries, Ltd.
【表3】【table 3】
洁齿剂组合物Dentifrice Composition
【表4】【Table 4】
洁齿剂组合物Dentifrice Composition
【表5】【table 5】
漱口水组合物mouthwash composition
【表6】【Table 6】
漱口水组合物mouthwash composition
由表中的结果可知,并用(A)成分和(B)成分时,口腔生物膜除去效果显著提高。此外,苦味得到抑制。进一步地,口腔用组合物,特别是洁齿剂组合物具有适当的起泡。From the results in the table, it was found that the oral cavity biofilm removal effect was significantly improved when the (A) component and the (B) component were used in combination. In addition, bitterness is suppressed. Further, oral compositions, especially dentifrice compositions, have suitable foaming.
以下显示处方例。另外,使用原料与上述相同。Prescription examples are shown below. In addition, the raw materials used are the same as above.
[处方例I-1]漱口水[Prescription Example I-1] Mouthwash
(A)/(B-1)比:1.6(A)/(B-1) ratio: 1.6
该漱口水的口腔生物膜除去效果优异,此外苦味得到抑制,起泡良好。This mouthwash was excellent in the effect of removing oral biofilm, and in addition, bitterness was suppressed, and foaming was favorable.
[处方例II-1]漱口水[Prescription Example II-1] Mouthwash
(A)/(B-2)比:3.0(A)/(B-2) ratio: 3.0
该漱口水的生物膜除去效果优异,此外苦味得到抑制。This mouthwash was excellent in biofilm removal effect, and also suppressed bitterness.
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| CN111050747A (en) * | 2017-11-29 | 2020-04-21 | 狮王株式会社 | Dentifrice composition |
| CN111417381A (en) * | 2017-11-30 | 2020-07-14 | 狮王株式会社 | Oral soil remover, oral soil formation inhibitor, and oral composition |
| CN113507966A (en) * | 2019-02-28 | 2021-10-15 | 花王株式会社 | Oral composition |
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| JP2016138047A (en) * | 2015-01-26 | 2016-08-04 | ライオン株式会社 | Dentifrice composition |
| CN108366950B (en) | 2015-11-30 | 2022-02-18 | 狮王株式会社 | Oral composition |
| KR102637277B1 (en) * | 2015-11-30 | 2024-02-16 | 라이온 가부시키가이샤 | Oral composition |
| JP6874688B2 (en) * | 2015-11-30 | 2021-05-19 | ライオン株式会社 | Toothpaste composition and oral biofilm remover |
| JP6834978B2 (en) * | 2015-11-30 | 2021-02-24 | ライオン株式会社 | Toothpaste composition and oral biofilm remover |
| JP6617535B2 (en) * | 2015-11-30 | 2019-12-11 | ライオン株式会社 | Dentifrice composition |
| JP7264619B2 (en) * | 2017-12-27 | 2023-04-25 | 花王株式会社 | oral composition |
| JP7411788B2 (en) * | 2019-09-30 | 2024-01-11 | ザ プロクター アンド ギャンブル カンパニー | Oral care composition comprising a source of stannous ions, a neutral amino acid, and a polyphosphate |
| JP7670063B2 (en) * | 2020-09-24 | 2025-04-30 | ライオン株式会社 | Polyhydric alcohol-based dentifrice composition |
| KR102633791B1 (en) * | 2020-12-22 | 2024-02-02 | 주식회사 엘지생활건강 | Composition comprising phosphate for removal biofilm |
| KR20220107992A (en) | 2021-01-26 | 2022-08-02 | 주식회사 마루치 | Oral composition for preventing and improving sensitive teeth |
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| JPWO2015008824A1 (en) | 2017-03-02 |
| MY177921A (en) | 2020-09-26 |
| JPWO2015008823A1 (en) | 2017-03-02 |
| CN107875031B (en) | 2021-08-20 |
| JP6299761B2 (en) | 2018-03-28 |
| KR102146681B1 (en) | 2020-08-21 |
| CN105358128B (en) | 2019-03-01 |
| JP6269672B2 (en) | 2018-01-31 |
| WO2015008823A1 (en) | 2015-01-22 |
| KR20160031997A (en) | 2016-03-23 |
| CN107875031A (en) | 2018-04-06 |
| WO2015008824A1 (en) | 2015-01-22 |
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