JP7264049B2 - oral composition - Google Patents
oral composition Download PDFInfo
- Publication number
- JP7264049B2 JP7264049B2 JP2019521283A JP2019521283A JP7264049B2 JP 7264049 B2 JP7264049 B2 JP 7264049B2 JP 2019521283 A JP2019521283 A JP 2019521283A JP 2019521283 A JP2019521283 A JP 2019521283A JP 7264049 B2 JP7264049 B2 JP 7264049B2
- Authority
- JP
- Japan
- Prior art keywords
- extract
- oral composition
- mass
- oral cavity
- oral
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 235000001510 limonene Nutrition 0.000 description 1
- 229940087305 limonene Drugs 0.000 description 1
- 229930007744 linalool Natural products 0.000 description 1
- 235000010420 locust bean gum Nutrition 0.000 description 1
- 239000000711 locust bean gum Substances 0.000 description 1
- 239000004325 lysozyme Substances 0.000 description 1
- 235000010335 lysozyme Nutrition 0.000 description 1
- 229960000274 lysozyme Drugs 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical group [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Chemical group 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000001683 mentha spicata herb oil Substances 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 150000004702 methyl esters Chemical class 0.000 description 1
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
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- 229910052618 mica group Inorganic materials 0.000 description 1
- 239000004200 microcrystalline wax Substances 0.000 description 1
- 235000019808 microcrystalline wax Nutrition 0.000 description 1
- 229910000150 monocalcium phosphate Inorganic materials 0.000 description 1
- 235000019691 monocalcium phosphate Nutrition 0.000 description 1
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 1
- 235000019799 monosodium phosphate Nutrition 0.000 description 1
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 1
- 229920003052 natural elastomer Polymers 0.000 description 1
- 229920005615 natural polymer Polymers 0.000 description 1
- 229920001194 natural rubber Polymers 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- 229920001778 nylon Polymers 0.000 description 1
- JPMIIZHYYWMHDT-UHFFFAOYSA-N octhilinone Chemical compound CCCCCCCCN1SC=CC1=O JPMIIZHYYWMHDT-UHFFFAOYSA-N 0.000 description 1
- 229940114496 olive leaf extract Drugs 0.000 description 1
- 239000010502 orange oil Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 150000002936 p-menthane-3,8-diol derivatives Chemical class 0.000 description 1
- RUVINXPYWBROJD-UHFFFAOYSA-N para-methoxyphenyl Natural products COC1=CC=C(C=CC)C=C1 RUVINXPYWBROJD-UHFFFAOYSA-N 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 235000019809 paraffin wax Nutrition 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical group [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- 239000003208 petroleum Substances 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 description 1
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 1
- 229920002857 polybutadiene Polymers 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920002635 polyurethane Polymers 0.000 description 1
- 239000004814 polyurethane Substances 0.000 description 1
- 229920002689 polyvinyl acetate Polymers 0.000 description 1
- 239000011118 polyvinyl acetate Substances 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 229920000915 polyvinyl chloride Polymers 0.000 description 1
- 239000004800 polyvinyl chloride Substances 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 1
- 235000010409 propane-1,2-diol alginate Nutrition 0.000 description 1
- 239000000770 propane-1,2-diol alginate Substances 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 235000009566 rice Nutrition 0.000 description 1
- 239000010668 rosemary oil Substances 0.000 description 1
- 229940058206 rosemary oil Drugs 0.000 description 1
- 229940085605 saccharin sodium Drugs 0.000 description 1
- 229940112950 sage extract Drugs 0.000 description 1
- 235000020752 sage extract Nutrition 0.000 description 1
- 239000010670 sage oil Substances 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 150000004760 silicates Chemical class 0.000 description 1
- 229920002379 silicone rubber Polymers 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- 239000011775 sodium fluoride Substances 0.000 description 1
- 235000013024 sodium fluoride Nutrition 0.000 description 1
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 1
- RUTSRVMUIGMTHJ-UHFFFAOYSA-M sodium;tetradec-1-ene-1-sulfonate Chemical compound [Na+].CCCCCCCCCCCCC=CS([O-])(=O)=O RUTSRVMUIGMTHJ-UHFFFAOYSA-M 0.000 description 1
- CDGJVLFXHHVFFL-UHFFFAOYSA-M sodium;tetradecanoyl sulfate Chemical compound [Na+].CCCCCCCCCCCCCC(=O)OS([O-])(=O)=O CDGJVLFXHHVFFL-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000019721 spearmint oil Nutrition 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 229940013618 stevioside Drugs 0.000 description 1
- OHHNJQXIOPOJSC-UHFFFAOYSA-N stevioside Natural products CC1(CCCC2(C)C3(C)CCC4(CC3(CCC12C)CC4=C)OC5OC(CO)C(O)C(O)C5OC6OC(CO)C(O)C(O)C6O)C(=O)OC7OC(CO)C(O)C(O)C7O OHHNJQXIOPOJSC-UHFFFAOYSA-N 0.000 description 1
- 235000019202 steviosides Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000000542 sulfonic acid group Chemical group 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 239000000892 thaumatin Substances 0.000 description 1
- 235000010436 thaumatin Nutrition 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- 239000010936 titanium Substances 0.000 description 1
- 229910052719 titanium Inorganic materials 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 description 1
- 229960000401 tranexamic acid Drugs 0.000 description 1
- KHPCPRHQVVSZAH-UHFFFAOYSA-N trans-cinnamyl beta-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OCC=CC1=CC=CC=C1 KHPCPRHQVVSZAH-UHFFFAOYSA-N 0.000 description 1
- 229910000391 tricalcium phosphate Inorganic materials 0.000 description 1
- 229940078499 tricalcium phosphate Drugs 0.000 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
- MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 description 1
- 235000012141 vanillin Nutrition 0.000 description 1
- FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 239000009637 wintergreen oil Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
- 229930007845 β-thujaplicin Natural products 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/42—Amides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Cosmetics (AREA)
Description
本発明は、口臭の原因ともなる口腔内のねばつき感の改善効果が優れ、かつ優れたすっきり感付与効果を有し、口臭抑制用として好適な口腔用組成物に関する。 TECHNICAL FIELD The present invention relates to an oral cavity composition that is excellent in reducing the sticky feeling in the oral cavity, which is a cause of bad breath, and has an excellent effect of imparting a refreshing feeling, and is suitable for suppressing bad breath.
従来、口臭抑制には、殺菌剤による口臭原因菌の殺菌や、消臭剤、口臭原因物質の発生抑制剤等の有効成分の使用が有効であることが知られており、これらを配合した口腔用組成物が提案されている。例えば、シソ科やミカン科などの植物抽出エキスは、口臭抑制成分として知られており、これら以外にも植物のエキスを口臭防止のための有効成分として配合した口腔用組成物が提案されている(特許文献1~3:特開2005-289918号公報、特許第5776364号公報、特開2016-112634号公報)。これら植物抽出エキスを配合した口腔用組成物は、口臭の原因成分、例えば揮発性硫黄、メチルメルカプタン等の減少に有効であり、呼気(対人)としての口臭防止効果を有する。 Conventionally, it has been known that sterilization of halitosis-causing bacteria with bactericides, and use of active ingredients such as deodorants and inhibitors of halitosis-causing substances are effective in suppressing halitosis. have been proposed. For example, extracts from plants such as Labiatae and Rutaceae are known as bad breath suppressing ingredients, and other oral compositions containing plant extracts as active ingredients for preventing bad breath have been proposed. (Patent Documents 1 to 3: JP-A-2005-289918, JP-A-5776364, JP-A-2016-112634). Oral compositions containing these plant extracts are effective in reducing halitosis-causing components, such as volatile sulfur and methyl mercaptan, and have a halitosis-preventing effect on exhaled breath (for humans).
しかし、近年、実際には他人に検知されるような口臭(呼気口臭)がないにもかかわらず、口腔内に対する不快感によって口臭があるように感じて、対人への口臭を発症しているかもしれないという口臭不安を抱くケースが増加している。このため、このような口臭不安をも解消できれば、口臭が抑制されたという満足な効果感が得られると考えられる。 However, in recent years, even though there is no bad breath (exhalation halitosis) that can be detected by others, people may feel that they have bad breath due to discomfort in the oral cavity, and develop interpersonal halitosis. There are an increasing number of cases where people are worried about bad breath. For this reason, it is thought that if such anxiety about bad breath can be eliminated, a satisfactory effect of suppressing bad breath can be obtained.
しかしながら、従来の口臭抑制を目的とする口腔用組成物では、上述したような口臭不安をも解消し得るような十分な効果感を与えることができず、改善が望まれていた。 However, conventional compositions for the oral cavity intended to suppress halitosis cannot provide a sufficient feeling of effectiveness capable of relieving anxiety about halitosis as described above, and improvements have been desired.
本発明は、上記事情に鑑みなされたもので、口腔内のねばつき感の改善効果が優れ、かつ優れたすっきり感付与効果を有する口腔用組成物を提供することを目的とする。 The present invention has been made in view of the above circumstances, and an object of the present invention is to provide an oral cavity composition that has an excellent effect of improving stickiness in the oral cavity and imparting an excellent refreshing feeling.
本発明者らは、上記目的を達成するためには、特に口臭不安感の主な原因と考えられる口腔内のねばつき感や、すっきり感の少なさといった不快感を改善して口臭抑制の効果感を高めることが有効であると考え、これらの点に着目して更に検討を進めた。その結果、植物の抽出エキスと、冷感剤の中でも特定の成分を選択し、両成分をそれぞれ特定量かつ特定割合で併用すると、口腔内のねばつき感を改善し、かつ経時でも持続する高いすっきり感を与える優れた作用効果が得られることを見出した。そして、両成分の併用系を口腔用組成物に配合すると、口腔内のねばつき感の改善効果が優れる上に、上記のような持続的かつ優れたすっきり感付与効果を発揮し、また、口腔内刺激が抑えられ良好な使用感を与えることができ、これにより、口臭抑制の効果感も高まり、対人的な口臭の抑制のみならず口臭不安感をも解消可能であることを知見し、本発明をなすに至った。
即ち、本発明では、(A)植物エキスをエキス純分として0.00001~0.05質量%と、(B)N-(4-シアノメチルフェニル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-1)及びN-(2-(2-ピリジニル)エチル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-2)から選ばれる1種以上を0.00001~0.01質量%とを含有し、(A)/(B)が質量比として0.02~100であることによって、口腔内のねばつき感の改善効果が優れ、かつ優れたすっきり感付与効果を有し、使用感も良い口腔用組成物を提供できる。In order to achieve the above object, the present inventors have found an effect of suppressing bad breath by improving discomfort such as a sticky feeling in the oral cavity and a lack of refreshing feeling, which are considered to be the main causes of anxiety about bad breath. We considered that it would be effective to enhance the sense of urgency, and focused on these points and proceeded with further studies. As a result, by selecting specific components among plant extracts and cooling sensation agents, and using both components in specific amounts and ratios in combination, the feeling of stickiness in the oral cavity can be improved, and the feeling of stickiness in the oral cavity can be improved. It was found that an excellent action and effect of providing a refreshing feeling can be obtained. When a combination system of both components is blended into an oral composition, the effect of improving the sticky feeling in the oral cavity is excellent, and the effect of imparting a persistent and excellent refreshing feeling as described above is exhibited. It is possible to suppress internal irritation and provide a good feeling of use, thereby increasing the effect of suppressing bad breath, and finding that it is possible to eliminate not only interpersonal bad breath but also anxiety about bad breath. I came up with the invention.
That is, in the present invention, (A) 0.00001 to 0.05% by mass of a plant extract as a pure extract component, and (B) N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide ( B-1) and one or more selected from N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide (B-2) in an amount of 0.00001 to 0.01% by mass. By containing (A) / (B) in a mass ratio of 0.02 to 100, the effect of improving the sticky feeling in the oral cavity is excellent, and the effect of imparting an excellent refreshing feeling is obtained. A good oral composition can be provided.
更に詳述すると、後述の比較例にも示すように、(A)成分又は(B)成分の単独使用では、口腔内のねばつき感改善効果及びすっきり感付与効果がほとんどなかった(比較例1~15)。よって、この結果からは両者を併用することで両作用効果が向上するとは考えられなかったが、後述の実施例からも明らかなように、本発明では(A)成分と(B)成分とを組み合わせると、両者の配合量がそれぞれ特定範囲かつ(A)/(B)の質量比が特定範囲内において、両成分が相乗的に作用し、口腔内刺激を抑えてねばつき感の改善効果及びすっきり感付与効果が共に増強し、格別顕著な作用効果を奏した。このような本発明の作用効果は、(A)及び(B)成分の組み合わせに特異なものであり、(B)成分に代えて、同様に冷感又は清涼化作用を有するメントール、ペパーミント油又はモノメンチルサクシネートを(A)成分と併用したのでは劣り(比較例16~18)、また、(B)成分以外のN-置換-p-メンタン-カルボキサミドを(A)成分と併用した場合も劣った。
特許文献4~9(特開2014-125440号公報、特開2015-182983号公報、特開2016-102076号公報、特表2014-507440号公報、特表2012-508741号公報、特表2011-520925号公報)は、冷涼化又は清涼化剤のN-置換-p-メンタン-カルボキサミドによって清涼感やサッパリ感が改善した口腔用組成物、特許文献10(特開2013-112634号公報)は、p-メンタン-3,8-ジオール異性体混合物含有の口腔用組成物を開示する。これに対し、本発明は、(A)及び(B)成分の併用による、口腔内のねばつき感の改善及びすっきり感の付与であり、その技術的思想は特許文献4~10から予測できない。More specifically, as shown in Comparative Examples below, the single use of component (A) or component (B) had little effect of improving stickiness in the oral cavity and imparting refreshing feeling (Comparative Example 1). ~15). Therefore, from this result, it was not thought that the combined use of both would improve both functions and effects. When combined, both components act synergistically within a specific range of the blending amount of both and the specific range of the mass ratio of (A) / (B), suppressing irritation in the oral cavity and improving the sticky feeling. The effect of imparting a refreshing feeling was enhanced, and a particularly remarkable action and effect were exhibited. Such effects of the present invention are peculiar to the combination of components (A) and (B), and instead of component (B), menthol, peppermint oil, or When monomenthyl succinate is used in combination with component (A), the results are inferior (Comparative Examples 16 to 18), and when N-substituted-p-menthane-carboxamides other than component (B) are used in combination with component (A), inferior.
Patent Documents 4 to 9 (JP 2014-125440, JP 2015-182983, JP 2016-102076, JP 2014-507440, JP 2012-508741, JP 2011- 520925) is an oral composition in which coolness and freshness are improved by N-substituted-p-menthane-carboxamide as a cooling or refreshing agent; Disclosed are oral compositions containing p-menthane-3,8-diol isomer mixtures. On the other hand, the present invention aims to improve the sticky feeling in the oral cavity and impart a refreshing feeling by using the components (A) and (B) in combination, and the technical idea thereof cannot be predicted from Patent Documents 4 to 10.
従って、本発明は、下記の口腔用組成物を提供する。
〔1〕
(A)植物エキスをエキス純分として0.00001~0.05質量%と、
(B)N-(4-シアノメチルフェニル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-1)及びN-(2-(2-ピリジニル)エチル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-2)から選ばれる1種以上を0.00001~0.01質量%と
を含有し、(A)/(B)が質量比として0.02~100である口腔用組成物。
〔2〕
(A)植物エキスが、ローズマリー、オウゴン、ニンジン、セージ、カンゾウ、トウキ、柿、ナタマメ、オリーブ、チャ、キハダ、クロモジ、サンショウ、タイム、シラカバ、シャクヤク、ウラジロガシ、アセンヤク、ウコン、チョウジ、ステビア、ムクロジ、マジョラム、メリッサ、シソ、ローレル、ユーカリ、コーラ、羅漢果、ツバキ、クローブ、オールスパイス、スオウ、シコン、ダイオウ、レンギョウ、チンピ、ケイヒ、オレガノ、バジル、ナギナタコウジュ、ボタンピ及びセイタカミロバランから選ばれる1種以上の植物の抽出エキスである〔1〕に記載の口腔用組成物。
〔3〕
(A)植物エキスが、ローズマリー、オウゴン、ニンジン、セージ、カンゾウ、トウキ、柿、ナタマメ、オリーブ、チャ及びキハダから選ばれる1種以上の植物の抽出エキスである〔2〕に記載の口腔用組成物。
〔4〕
更に、(C)メンチルモノサクシネート、N-{(エトキシカルボニル)メチル}-p-メンタン-3-カルボキサミド及びメンチルラクテートから選ばれる1種以上を0.0001~0.01質量%含有する〔1〕~〔3〕のいずれかに記載の口腔用組成物。
〔5〕
歯磨剤又は洗口剤である〔1〕~〔4〕のいずれかに記載の口腔用組成物。
〔6〕
歯磨剤であり、更に、(D)研磨剤を8~70質量%含有する〔5〕に記載の口腔用組成物。Accordingly, the present invention provides the following oral compositions.
[1]
(A) a plant extract of 0.00001 to 0.05% by mass as a pure extract content;
(B) N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide (B-1) and N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide An oral composition containing 0.00001 to 0.01% by mass of one or more selected from (B-2), and having a mass ratio of (A)/(B) of 0.02 to 100.
[2]
(A) Plant extracts include rosemary, scutellaria root, carrot, sage, licorice, angelica root, persimmon, cattle bean, olive, tea, yellowfin tuna, kuromoji, Japanese pepper, thyme, white birch, peony, red beetle, asenyak, turmeric, clove, stevia , soapberry, marjoram, melissa, perilla, laurel, eucalyptus, cola, monk fruit, camellia, clove, allspice, suou, chikon, rhubarb, forsythia, chimp, cinnamon bark, oregano, basil, naginata koji, botanpi and seitakamyrobalan The oral composition according to [1], which is an extract of one or more plants.
[3]
(A) The oral cavity use according to [2], wherein the plant extract is one or more plant extracts selected from rosemary, scutellaria root, carrot, sage, licorice, angelica root, persimmon, jack bean, olive, tea and yellowfin tuna. Composition.
[4]
Furthermore, (C) one or more selected from menthyl monosuccinate, N-{(ethoxycarbonyl)methyl}-p-menthane-3-carboxamide and menthyl lactate is contained in an amount of 0.0001 to 0.01% by mass [1 ] to the oral cavity composition according to any one of [3].
[5]
The oral composition according to any one of [1] to [4], which is a dentifrice or mouthwash.
[6]
The oral cavity composition according to [5], which is a dentifrice and further contains (D) 8 to 70% by mass of an abrasive.
本発明によれば、口臭の原因ともなる口腔内のねばつき感の改善効果が優れ、かつ優れたすっきり感付与効果を有し、使用感も良い口腔用組成物を提供できる。本発明の口腔用組成物は、口臭抑制実感も高く、口臭抑制用として好適に使用できる。 ADVANTAGE OF THE INVENTION According to this invention, the oral-cavity composition which is excellent in the effect of improving the sticky feeling in the oral cavity which causes bad breath, has the effect of giving an excellent refreshing feeling, and has a good feeling in use can be provided. The composition for oral cavity of the present invention has a high feeling of suppressing bad breath, and can be suitably used for suppressing bad breath.
以下、本発明につき更に詳述する。本発明の口腔用組成物は、(A)植物エキスと、(B)N-(4-シアノメチルフェニル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-1)及びN-(2-(2-ピリジニル)エチル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-2)から選ばれる1種以上とを、それぞれ特定量かつ特定割合で含有する。 The present invention will be described in further detail below. The oral composition of the present invention comprises (A) a plant extract, and (B) N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide (B-1) and N-(2-( 2-Pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide (B-2) in specific amounts and in specific ratios.
(A)植物エキスは、植物の抽出エキスであり、(B)成分と併用することで、口腔内のねばつき感の低減作用を奏する。
ここで、エキスの原料となる植物としては、ローズマリー、オウゴン、ニンジン、セージ、カンゾウ、トウキ、柿(特に柿のタンニン)、ナタマメ、オリーブ(特にオリーブの葉)、チャ、キハダ(特に樹皮のオウバク)、クロモジ、サンショウ、タイム、シラカバ、シャクヤク、ウラジロガシ、アセンヤク、ウコン、チョウジ、ステビア、ムクロジ、マジョラム、メリッサ、シソ、ローレル、ユーカリ、コーラ、羅漢果、ツバキ、クローブ、オールスパイス、スオウ、シコン、ダイオウ、レンギョウ、チンピ、ケイヒ、オレガノ、バジル、ナギナタコウジュ、ボタンピ、セイタカミロバラン等が挙げられる。これらの中でも、ローズマリー、オウゴン、ニンジン、セージ、カンゾウ、トウキ、柿、ナタマメ、オリーブ、チャ、キハダ、クロモジ、サンショウが好ましく、より好ましくはローズマリー、オウゴン、ニンジン、セージ、カンゾウ、トウキ、柿、ナタマメ、オリーブ、チャ、キハダであり、更に好ましくはローズマリー、オウゴン、ニンジン、セージ、カンゾウである。(A) The plant extract is a plant extract, and when used in combination with the component (B), it has the effect of reducing stickiness in the oral cavity.
Plants used as raw materials for the extract include rosemary, Scutellaria root, carrot, sage, licorice, Angelica keiskei, persimmon (especially tannin of persimmon), jack bean, olive (especially olive leaf), tea, and yellowfin tuna (especially bark). Phellodendron bark), kuromoji, Japanese pepper, thyme, white birch, peony, red oak, ashen yak, turmeric, clove, stevia, soapberry, marjoram, melissa, perilla, laurel, eucalyptus, cola, monk fruit, camellia, clove, allspice, suou, chikon , rhubarb, forsythia, chimp, cinnamon bark, oregano, basil, naginatakoju, botanpi, seitakamyrobalan and the like. Among these, rosemary, scutellaria root, carrot, sage, licorice, angelica root, persimmon, natamame, olive, tea, yellowfin tuna, kuromoji, and Japanese pepper are preferable, and more preferably rosemary, scutellaria root, carrot, sage, licorice, angelica root, They are persimmon, jack bean, olive, tea and yellowfin tuna, more preferably rosemary, scutellaria root, carrot, sage and licorice.
植物エキスの抽出方法は、公知の方法を採用でき、通常の抽出条件で行うことができる。
具体的に、植物エキスは、原料植物、特に葉及び茎を粉砕して粉状にしたものを極性溶媒、非極性溶媒、又は極性溶媒と非極性溶媒との混合溶媒を用いて抽出することにより得ることができる。前記抽出溶媒としては、例えば、水、エチルエーテル、エチレンクロライド、ジオキサン、アセトン、エタノール、メタノール、酢酸エチル、プロピレングリコール、ブチレングリコール、グリセリン等の極性溶媒、もしくはn-ヘキサン、石油エーテル、リグロイン、シクロヘキサン、四塩化炭素、クロロホルム、ジクロルメタン、1,2-ジクロルエタン、トルエン、ベンゼン等の非極性溶媒、又はこれらの混合溶媒が挙げられる。
好ましい抽出溶媒としては、水、炭素数1~5の低級一価アルコール(特にメタノール、エタノール、プロパノール、イソプロパノール等)、グリコール(特にプロピレングリコール、ブチレングリコール等)、あるいはこれらの混合溶媒である。混合溶媒は、好ましくは水と低級一価アルコール又はグリコールとの混合比率が10:90~90:10(質量比)のものである。抽出溶媒は、水のみであってもよい。
また、抽出残渣を原料として、前記溶媒を用いて抽出処理された植物抽出物も、使用することができる。
このような(A)植物エキスは、市販品を使用することもできる。具体的には、丸善製薬(株)、(株)ヤマダ薬研等の市販品を用いることができる。A well-known method can be adopted as a method for extracting the plant extract, and the extraction can be performed under normal extraction conditions.
Specifically, a plant extract is obtained by extracting a raw material plant, especially a powder obtained by pulverizing leaves and stems, using a polar solvent, a nonpolar solvent, or a mixed solvent of a polar solvent and a nonpolar solvent. Obtainable. Examples of the extraction solvent include polar solvents such as water, ethyl ether, ethylene chloride, dioxane, acetone, ethanol, methanol, ethyl acetate, propylene glycol, butylene glycol, and glycerin, or n-hexane, petroleum ether, ligroin, and cyclohexane. , carbon tetrachloride, chloroform, dichloromethane, 1,2-dichloroethane, toluene, benzene, or a mixed solvent thereof.
Preferred extraction solvents are water, lower monohydric alcohols having 1 to 5 carbon atoms (especially methanol, ethanol, propanol, isopropanol, etc.), glycols (especially propylene glycol, butylene glycol, etc.), or mixed solvents thereof. The mixed solvent preferably contains water and a lower monohydric alcohol or glycol at a mixing ratio of 10:90 to 90:10 (mass ratio). The extraction solvent may be water only.
A plant extract obtained by extracting an extraction residue using the above-mentioned solvent can also be used.
A commercial item can also be used for such a (A) plant extract. Specifically, commercially available products such as Maruzen Pharmaceutical Co., Ltd. and Yamada Yaken Co., Ltd. can be used.
(A)植物エキスの配合量は、抽出溶媒を除いたエキス純分として組成物全体の0.00001~0.05%(質量%、以下同様)であり、好ましくは0.0001~0.005%であり、より好ましくは0.0002~0.005%である。配合量が0.00001%未満であると、ねばつき感の改善効果が劣る。0.05%を超えると、刺激が強すぎる。 (A) The blending amount of the plant extract is 0.00001 to 0.05 % (% by mass, the same shall apply hereinafter), preferably 0.0001 to 0.005, of the entire composition as a pure extract content excluding the extraction solvent. %, more preferably 0.0002 to 0.005%. If the blending amount is less than 0.00001%, the effect of improving stickiness is inferior. Exceeding 0.05% is too irritating.
(B)成分は、N-(4-シアノメチルフェニル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-1)及びN-(2-(2-ピリジニル)エチル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-2)から選ばれ、好ましくはN-(4-シアノメチルフェニル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-1)である。なお、(B)成分としては、(B-1)成分又は(B-2)成分を用いてもよく、また、効果発現の点で(B-1)及び(B-2)成分を用いてもよい。 Component (B) is N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide (B-1) and N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5- It is selected from methylcyclohexanecarboxamides (B-2), preferably N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide (B-1). In addition, as the component (B), the component (B-1) or the component (B-2) may be used. good too.
(B)成分の配合量は、組成物全体の0.00001~0.01%であり、好ましくは0.00003~0.005%である。0.00001%未満であると、ねばつき感の改善効果及びすっきり感の付与効果が劣る。0.01%を超えると、刺激が強すぎて後味が悪くなることがある。
なお、(B-1)成分、(B-2)成分のそれぞれの配合量は、上記(B)成分の配合量の範囲内で設定できる。The blending amount of component (B) is 0.00001 to 0.01%, preferably 0.00003 to 0.005%, of the total composition. If it is less than 0.00001%, the effect of improving the sticky feeling and the effect of imparting a refreshing feeling are inferior. If it exceeds 0.01%, the stimulation may be too strong and the aftertaste may be bad.
The blending amounts of the components (B-1) and (B-2) can be set within the range of the blending amount of the component (B).
本発明において、(A)成分と(B)成分との配合割合を示す(A)/(B)は、質量比として0.02~100であり、好ましくは0.05~20、より好ましくは0.2~5である。この範囲内であると、ねばつき感の改善効果及びすっきり感の付与効果が共に優れ、また、刺激が満足に抑制される。0.02未満であると、すっきり感の付与効果が十分に持続せず、刺激も強くなる。100を超えると、刺激が強くなる。 In the present invention, (A)/(B), which indicates the mixing ratio of component (A) and component (B), is 0.02 to 100, preferably 0.05 to 20, more preferably 0.05 to 20 as a mass ratio. 0.2 to 5. Within this range, both the effect of improving stickiness and the effect of imparting refreshing feeling are excellent, and stimulation is satisfactorily suppressed. If it is less than 0.02, the effect of imparting a refreshing feeling does not last sufficiently, and the stimulation becomes strong. If it exceeds 100, the stimulus becomes stronger.
本発明では、更に、(C)メンチルモノサクシネート、N-{(エトキシカルボニル)メチル}-p-メンタン-3-カルボキサミド及びメンチルラクテートから選ばれる1種又は2種以上を配合することが好ましい。(A)及び(B)成分に(C)成分を組み合わせて配合すると、ねばつき感の改善効果が更に高まる。
(C)成分は、好ましくはメンチルモノサクシネート、N-{(エトキシカルボニル)メチル}-p-メンタン-3-カルボキサミドであり、より好ましくはメンチルモノサクシネートである。In the present invention, it is preferable to blend one or more selected from (C) menthyl monosuccinate, N-{(ethoxycarbonyl)methyl}-p-menthane-3-carboxamide and menthyl lactate. When the (A) and (B) components are combined with the (C) component, the effect of improving stickiness is further enhanced.
Component (C) is preferably menthyl monosuccinate, N-{(ethoxycarbonyl)methyl}-p-menthane-3-carboxamide, and more preferably menthyl monosuccinate.
(C)成分の配合量は、組成物全体の0.0001~0.01%が好ましく、より好ましくは0.0003~0.005%である。この範囲内であると、ねばつき感の改善効果が更に向上する。0.01%を超えると、刺激が強くなって後味が悪くなる場合がある。 The blending amount of component (C) is preferably 0.0001 to 0.01%, more preferably 0.0003 to 0.005%, based on the total composition. Within this range, the effect of improving stickiness is further improved. If it exceeds 0.01%, the stimulation may become strong and the aftertaste may become bad.
本発明の口腔用組成物は、固体、液体、液状、ペースト状、ゲル状などの形態に調製し、練歯磨、液体歯磨、液状歯磨、潤製歯磨等の歯磨剤、洗口剤、口中清涼剤などの様々な剤型にすることが可能であるが、特に、歯磨剤又は洗口剤、とりわけ歯磨剤が好適であり、研磨剤を含む練歯磨がよい。その製造方法は剤型に応じた常法を採用できる。
更に、本発明では、組成物の目的、剤型等に応じて、上述した成分以外にも適宜な公知成分を、本発明の効果を損なわない範囲で必要に応じて配合できる。例えば、練歯磨剤の場合は、研磨剤、粘結剤、湿潤剤、界面活性剤、甘味剤、防腐剤、pH調整剤、香料、薬効成分等が挙げられる。洗口剤の場合は、湿潤剤、界面活性剤、甘味剤、防腐剤、pH調整剤、香料、薬効成分等が挙げられる。The oral composition of the present invention is prepared in the form of solid, liquid, liquid, paste, gel, etc., and can be used in dentifrices such as toothpaste, liquid dentifrice, liquid dentifrice, wet dentifrice, mouthwash, and mouth freshener. Although various formulations such as agents are possible, dentifrices or mouthwashes, particularly dentifrices, are particularly preferable, and toothpastes containing abrasives are preferable. As for the production method, a conventional method can be adopted depending on the dosage form.
Furthermore, in the present invention, in addition to the above-mentioned components, known ingredients can be blended as necessary depending on the purpose of the composition, the dosage form, etc., as long as the effects of the present invention are not impaired. For example, in the case of a toothpaste, abrasives, binders, wetting agents, surfactants, sweeteners, preservatives, pH adjusters, perfumes, medicinal ingredients and the like can be used. In the case of a mouthwash, humectants, surfactants, sweeteners, preservatives, pH adjusters, fragrances, medicinal ingredients and the like can be mentioned.
研磨剤としては、第2リン酸カルシウム・2水和塩又は無水和物、第1リン酸カルシウム、第3リン酸カルシウム、ピロリン酸カルシウム等のリン酸カルシウム系化合物;沈降性シリカ、アルミノシリケート、ジルコノシリケート、チタン結合性シリカ等のシリカ系研磨剤;炭酸カルシウム等の炭酸カルシウム系研磨剤;水酸化カルシウム、水酸化アルミニウム、第3リン酸マグネシウム、炭酸マグネシウム、硫酸カルシウム、ベントナイト、ハイドロキシアパタイトが挙げられ、これらの1種又は2種以上を配合できる。これらの中では、特に沈降性シリカ、アルミノシリケート、ジルコノシリケート、チタン結合性シリカ等のケイ酸塩を主成分とするシリカ系研磨剤や炭酸カルシウム系研磨剤、とりわけ沈降性シリカ等のシリカ系研磨剤が好ましい。 Abrasives include calcium phosphate-based compounds such as dicalcium phosphate dihydrate or anhydrate, monocalcium phosphate, tricalcium phosphate, and calcium pyrophosphate; precipitated silica, aluminosilicate, zirconosilicate, titanium-bonded silica, etc. calcium carbonate-based abrasives such as calcium carbonate; calcium hydroxide, aluminum hydroxide, magnesium tertiary phosphate, magnesium carbonate, calcium sulfate, bentonite, and hydroxyapatite; More than seeds can be blended. Among these, silica-based abrasives and calcium carbonate-based abrasives mainly composed of silicates such as precipitated silica, aluminosilicate, zirconosilicate, titanium-bonded silica, and especially silica-based abrasives such as precipitated silica, etc. Abrasives are preferred.
研磨剤、特に沈降性シリカは、粒径が1~40μmである研磨粒子が好ましく、また更に、BET比表面積は1gあたり80~250平方メートルであることが好ましい。前記粒径は、粒度分布測定装置(日機装(株)製、マイクロトラック粒度分布計、分散媒;水)による測定値である。
このようなシリカ系研磨剤としては、市販品を使用でき、例えば、HUBER社製のZeodent124、Zeodent113、Rhodia社製のTIXOSIL 73、TIXOSIL 63、Degussa社製のSident 3、Sident 20、多木化学(株)製のジルコノシリケート、アルミノシリケート等が挙げられる。
研磨剤の配合量は、組成物全体の8~70%、特に10~50%が好ましい。The abrasive, especially precipitated silica, is preferably abrasive particles having a particle size of 1-40 μm, and more preferably a BET specific surface area of 80-250 square meters per gram. The particle size is a value measured by a particle size distribution analyzer (Microtrac particle size distribution meter manufactured by Nikkiso Co., Ltd., dispersion medium: water).
As such silica-based abrasives, commercially available products can be used. Co., Ltd. zirconosilicate, aluminosilicate and the like.
The compounding amount of the abrasive is preferably 8 to 70%, particularly 10 to 50% of the total composition.
また、研磨剤は顆粒状であってもよく、研磨性を有する成分として、顆粒を配合できる。顆粒は、水不溶性粉体を顆粒状に形成させた粒子であり、シリカゲルを破砕した顆粒や粒状化に結合剤を用いた造粒物でもよい。
研磨剤は、上述の粒径1~40μmの研磨粒子と上述の顆粒を併用してもよい。Also, the abrasive may be in the form of granules, and granules can be blended as a component having abrasive properties. Granules are particles obtained by forming water-insoluble powder into granules, and may be granules obtained by crushing silica gel or granules using a binder for granulation.
As the abrasive, the abrasive particles having a particle size of 1 to 40 μm and the granules described above may be used in combination.
粘結剤としては、キサンタンガム、カルボキシメチルセルロースナトリウム、ポリアクリル酸ナトリウム、アルギン酸ナトリウム、ポリビニルピロリドン、カラギーナン、メチルセルロース、ヒドロキシエチルセルロースナトリウム、トラガントガム、カラヤガム、アラビヤガム、ローカストビーンガム、ポリビニルアルコール、カルボキシビニルポリマー、カーボポール、ビーガム、アルギン酸プロピレングリコール等の有機粘結剤、増粘性シリカ、ケイ酸アルミニウム等の無機粘結剤が配合できる。これらは1種又は2種以上で使用できる。粘結剤の配合量は、有機粘結剤の場合、組成物全体の0.8~5%、特に1~3%が好ましく、無機粘結剤の場合、組成物全体の0.5~10%、特に1~8%が好ましい。 Binders include xanthan gum, sodium carboxymethylcellulose, sodium polyacrylate, sodium alginate, polyvinylpyrrolidone, carrageenan, methylcellulose, sodium hydroxyethylcellulose, tragacanth gum, karaya gum, arabic gum, locust bean gum, polyvinyl alcohol, carboxyvinyl polymer, carbopol. , Veegum and propylene glycol alginate, and inorganic binders such as thickening silica and aluminum silicate. These can be used alone or in combination of two or more. The content of the binder is preferably 0.8 to 5%, particularly 1 to 3%, of the total composition in the case of an organic binder, and 0.5 to 10% of the total composition in the case of an inorganic binder. %, especially 1 to 8%.
湿潤剤としては、ソルビット、キシリット等の糖アルコール、プロピレングリコール、グリセリン等の多価アルコールが挙げられる。配合量は通常、組成物全体の5~50%、特に20~45%である。 Wetting agents include sugar alcohols such as sorbitol and xylite, and polyhydric alcohols such as propylene glycol and glycerin. The amount is usually 5-50%, especially 20-45% of the total composition.
界面活性剤としては、アニオン性界面活性剤、ノニオン性界面活性剤、両性界面活性剤が挙げられる。特に、アニオン性界面活性剤が好ましい。
アニオン性界面活性剤としては、アルキル硫酸塩、α-オレフィンスルホン酸塩、水素添加ココナッツ脂肪酸モノグリセリドモノ硫酸塩、ラウリルスルホ酢酸塩、N-メチル-N-アシルタウリン塩等のN-アシルタウリン塩、アシルサルコシン塩、N-アシル-L-グルタミン酸塩等のアシルアミノ酸塩が挙げられる。これらは1種又は2種以上で使用できる。中でも、泡立ち、泡質の良さの点で、スルホン酸基を含有するアニオン性界面活性剤が好ましく、より好ましくはアルキル硫酸塩、α-オレフィンスルホン酸塩である。前記塩としては、ナトリウム塩、カリウム塩、アンモニウム塩等が挙げられ、特にナトリウム塩が好ましい。
アルキル硫酸塩は、アルキル基の炭素数が好ましくは12~14であり、具体的には、アルキル硫酸塩としてラウリル硫酸ナトリウム、ミリストイル硫酸ナトリウムが挙げられる。Surfactants include anionic surfactants, nonionic surfactants, and amphoteric surfactants. Anionic surfactants are particularly preferred.
Examples of anionic surfactants include alkyl sulfates, α-olefin sulfonates, hydrogenated coconut fatty acid monoglyceride monosulfates, lauryl sulfoacetates, N-acyl taurates such as N-methyl-N-acyl taurates, Examples include acyl amino acid salts such as acyl sarcosine salts and N-acyl-L-glutamates. These can be used alone or in combination of two or more. Among them, anionic surfactants containing a sulfonic acid group are preferable, and alkyl sulfates and α-olefin sulfonates are more preferable in terms of foamability and foam quality. Examples of the salt include sodium salt, potassium salt, ammonium salt and the like, with sodium salt being particularly preferred.
The alkyl sulfate preferably has 12 to 14 carbon atoms in the alkyl group, and specific examples of the alkyl sulfate include sodium lauryl sulfate and sodium myristoyl sulfate.
α-オレフィンスルホン酸塩としては、炭素数が14~16のα-オレフィンスルホン酸のナトリウム、カリウム等のアルカリ金属塩を用いることができ、中でも炭素数14のα-オレフィンスルホン酸塩、特にナトリウム塩(一般名;テトラデセンスルホン酸ナトリウム)が好ましい。
界面活性剤、特にアニオン性界面活性剤の配合量は、例えば歯磨剤の場合は、組成物全体の0.6~2.5%が好ましく、より好ましくは1~2.5%である。洗口剤の場合は、組成物全体の0~1.0%、特に0~0.3%が好ましい。As the α-olefin sulfonate, an alkali metal salt such as sodium or potassium of an α-olefin sulfonate having 14 to 16 carbon atoms can be used. A salt (common name: sodium tetradecene sulfonate) is preferred.
The amount of surfactants, especially anionic surfactants, is preferably 0.6 to 2.5%, more preferably 1 to 2.5%, of the total composition, for example, in the case of dentifrices. For mouthwashes, it is preferably 0-1.0%, especially 0-0.3% of the total composition.
甘味剤としては、サッカリンナトリウム、ステビオサイド、ステビアエキス、パラメトキシシンナミックアルデヒド、ネオヘスペリジルジヒドロカルコン、ペリラルチン、グリチルリチン、ソーマチン、アスパラチルフェニルアラニンメチルエステル等が挙げられる。防腐剤としては、パラオキシ安息香酸エステル、安息香酸ナトリウム等が挙げられる。
pH調整剤としては、クエン酸、乳酸等の有機酸やその塩類;塩酸、水酸化ナトリウム、水酸化カリウム、リン酸水素二ナトリウム、リン酸二水素ナトリウム等の無機化合物が挙げられる。Sweeteners include sodium saccharin, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perillartine, glycyrrhizin, thaumatin, asparatylphenylalanine methyl ester and the like. Preservatives include paraoxybenzoic acid esters, sodium benzoate and the like.
Examples of pH adjusters include organic acids such as citric acid and lactic acid, salts thereof, and inorganic compounds such as hydrochloric acid, sodium hydroxide, potassium hydroxide, disodium hydrogen phosphate, and sodium dihydrogen phosphate.
香料としては、公知の口腔用香料、例えばメントール、アネトール、カルボン、オイゲノール、リモネン、n-デシルアルコール、シトロネロール、α-テルピネオール、シトロネリルアセテート、シネオール、リナロール、エチルリナロール、ワニリン、チモール、スペアミント油、ペパーミント油、レモン油、オレンジ油、セージ油、ローズマリー油、桂皮油、ピメント油、桂葉油、シソ油、冬緑油、丁字油、ユーカリ油等が挙げられる。 Flavoring agents include known oral fragrances such as menthol, anethole, carvone, eugenol, limonene, n-decyl alcohol, citronellol, α-terpineol, citronellyl acetate, cineole, linalool, ethyllinalool, vanillin, thymol, spearmint oil, Peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, pimento oil, cinnamon oil, perilla oil, wintergreen oil, clove oil, eucalyptus oil and the like.
薬効成分としては、デキストラナーゼ、アミラーゼ、プロテアーゼ、ムタナーゼ等の酵素;トラネキサム酸、イプシロンアミノカプロン酸、アズレン、グリチルリチン酸塩、グリチルレチン酸塩等の抗炎症剤;塩化ナトリウム、ビタミン類、アラントイン類等の細胞賦活剤;イソプロピルメチルフェノール、塩化セチルピリジニウム、塩化ベンザルコニウム、ヒノキチオール、塩化リゾチーム等の殺菌剤;銅クロロフィル、グルコン酸銅等の水溶性銅化合物;歯石予防剤;ビタミンE等の血行促進剤;アラニン、グリシン、プロリン等のアミノ酸類を配合できる。なお、薬効成分の配合量は、本発明の効果を妨げない範囲で有効量とすることができる。 Medicinal ingredients include enzymes such as dextranase, amylase, protease, and mutanase; anti-inflammatory agents such as tranexamic acid, epsilon aminocaproic acid, azulene, glycyrrhizinate, and glycyrrhizinate; Cell activators; Bactericides such as isopropylmethylphenol, cetylpyridinium chloride, benzalkonium chloride, hinokitiol, lysozyme chloride; Water-soluble copper compounds such as copper chlorophyll and copper gluconate; Anticalculus agents; Blood circulation promoters such as vitamin E ; Amino acids such as alanine, glycine, proline and the like can be added. In addition, the compounding amount of the medicinal component can be an effective amount within a range that does not impair the effects of the present invention.
更に、任意成分として、雲母チタン、酸化チタン、ベントナイト等の無機化合物;結晶性セルロース等のセルロース系の有機粉末;寒天、ゼラチン、デンプン、グルコマンナン等の天然高分子化合物;ポリ酢酸ビニル、アクリル樹脂、ポリウレタン、ポリエステル、ポリ塩化ビニル、ナイロン末、ポリエチレン末等の合成高分子化合物又はそれらの共重合体;カルナバワックス、ロジン、ライスワックス、マイクロクリスタリンワックス、ミツロウ、パラフィンワックス等のワックス類;セタノール、ステアリルアルコール等の高級アルコール;ポリイソブチレン、ポリブタジエン、シリコーン、天然ゴムを、本発明の効果を妨げない範囲で配合することができる。
なお、溶剤としては、精製水が一般的に用いられる。また、エタノール等の炭素数1~3の低級一価アルコールを配合してもよい。前記低級一価アルコールの配合量は組成物全体の0~10%がよい。Furthermore, as optional ingredients, inorganic compounds such as mica titanium, titanium oxide, and bentonite; cellulose-based organic powders such as crystalline cellulose; natural polymer compounds such as agar, gelatin, starch, and glucomannan; polyvinyl acetate, and acrylic resins. , synthetic polymer compounds such as polyurethane, polyester, polyvinyl chloride, nylon powder, polyethylene powder, or copolymers thereof; waxes such as carnauba wax, rosin, rice wax, microcrystalline wax, beeswax, paraffin wax; cetanol, Higher alcohols such as stearyl alcohol; polyisobutylene, polybutadiene, silicone, and natural rubber can be blended as long as the effects of the present invention are not impaired.
Purified water is generally used as the solvent. A lower monohydric alcohol having 1 to 3 carbon atoms such as ethanol may also be added. The blending amount of the lower monohydric alcohol is preferably 0 to 10% of the total composition.
以下、実施例及び比較例、処方例を示し、本発明を具体的に説明するが、本発明は下記の実施例に制限されるものではない。なお、下記の例において%は特に断らない限りいずれも質量%を示す。 EXAMPLES The present invention will be specifically described below by showing Examples, Comparative Examples, and Formulation Examples, but the present invention is not limited to the following Examples. In the following examples, % indicates % by mass unless otherwise specified.
[実施例、比較例]
表1~6に示す組成の歯磨剤組成物(練歯磨)又は洗口剤をそれぞれ常法によって調製し、通常の口腔用製剤容器(練歯磨:ラミネートチューブ、洗口剤:ボトル)に収容した。これらをサンプルとして用い、下記に示す方法で評価した。結果を表1~6に併記した。表中の(A)成分の配合量の数値は、抽出溶媒を除いたエキス純分量である。[Examples, Comparative Examples]
A dentifrice composition (toothpaste) or a mouthwash having the composition shown in Tables 1 to 6 was prepared by a conventional method and placed in a conventional oral formulation container (toothpaste: laminated tube, mouthwash: bottle). . These were used as samples and evaluated by the methods described below. The results are also shown in Tables 1-6. The numerical value of the blending amount of component (A) in the table is the pure amount of the extract excluding the extraction solvent.
<使用した原料>
(A)成分
《A1:ローズマリーエキス》
商品名:ローズマリー抽出物-J、抽出溶媒:50%エタノール、使用部位:葉
メーカー:丸善製薬(株)
《A2:オウゴンエキス》
商品名:オウゴン抽出物-J、抽出溶媒:50%エタノール、使用部位:根
メーカー:丸善製薬(株)
《A3:ニンジンエキス》
商品名:ニンジン抽出物、抽出溶媒:50%エタノール、使用部位:根
メーカー:丸善製薬(株)
《A4:セージエキス》
商品名:サルビア抽出物、抽出溶媒:50%エタノール、使用部位:葉
メーカー:丸善製薬(株)
《A5:カンゾウエキス》
商品名:カンゾウ抽出物、抽出溶媒:50%エタノール、使用部位:根
メーカー:丸善製薬(株)
《A6:ナタマメエキス》
商品名:AOF ナタマメエキス-HBG、抽出溶媒:50%1,3-ブチレングリコール、使用部位:種子
メーカー:(株)ヤマダ薬研
《A7:柿タンニンエキス》
商品名:パンシル BA-200E-1、抽出溶媒:水、使用部位:果実
メーカー:リリース科学工業
《A8:トウキエキス》
商品名:トウキ抽出物-JC、抽出溶媒:50%エタノール、使用部位:根
メーカー:丸善製薬(株)
《A9:オリーブ葉エキス》
商品名:オリーブ抽出物-BG、抽出溶媒:50%ブチレングリコール、使用部位:葉
メーカー:丸善製薬(株)<Raw materials used>
(A) Component <<A1: Rosemary Extract>>
Product name: Rosemary extract-J, Extraction solvent: 50% ethanol, Part used: Leaves Manufacturer: Maruzen Pharmaceutical Co., Ltd.
《A2: Scutellaria root extract》
Product name: Scutellaria root extract-J, Extraction solvent: 50% ethanol, Part used: Root manufacturer: Maruzen Pharmaceutical Co., Ltd.
<<A3: carrot extract>>
Product name: Carrot extract, Extraction solvent: 50% ethanol, Part used: Root Manufacturer: Maruzen Pharmaceutical Co., Ltd.
《A4: Sage Extract》
Product name: Salvia extract, Extraction solvent: 50% ethanol, Part used: Leaves Manufacturer: Maruzen Pharmaceutical Co., Ltd.
《A5: Glycyrrhiza Extract》
Product name: Glycyrrhiza extract, Extraction solvent: 50% ethanol, Part used: Root Manufacturer: Maruzen Pharmaceutical Co., Ltd.
《A6: Jack Bean Extract》
Product name: AOF Jack Bean Extract-HBG, Extraction solvent: 50% 1,3-butylene glycol, Part used: Seed manufacturer: Yamada Yakuen Co., Ltd. <<A7: Persimmon tannin extract>>
Product Name: Pancil BA-200E-1, Extraction Solvent: Water, Part Used: Fruit Maker: Release Science Industry <<A8: Touki Extract>>
Product name: Angelica keiskei extract-JC, Extraction solvent: 50% ethanol, Part used: Root Manufacturer: Maruzen Pharmaceutical Co., Ltd.
<<A9: Olive Leaf Extract>>
Product name: Olive extract-BG, Extraction solvent: 50% butylene glycol, Part used: Leaves Manufacturer: Maruzen Pharmaceutical Co., Ltd.
(B)成分
《B1:N-(4-シアノメチルフェニル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド》
商品名:エバクールG-180、メーカー:ジボダンジャパン社
《B2:N-(2-(2-ピリジニル)エチル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド》
商品名:エバクールG-190、メーカー:ジボダンジャパン社(B) Component <<B1: N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide>>
Product name: Evercool G-180, manufacturer: Givaudan Japan <<B2: N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide>>
Product name: Evercool G-190, Manufacturer: Givaudan Japan
(C)成分
《C1:メンチルモノサクシネート》
商品名:フィスクール、メーカー:ヴェマンフィス社
《C2:N-{(エトキシカルボニル)メチル}-p-メンタン-3-カルボキサミド》
商品名:WS-5、メーカー:シムライズ社
《C3:メンチルラクテート》
商品名:フレスコラットML、メーカー:シムライズ社
なお、香料は、後述の表7~15に示す香料組成物A~Pを各々使用した。(C) Component <<C1: menthyl monosuccinate>>
Product name: Fiscool, manufacturer: Vemanfis <<C2: N-{(ethoxycarbonyl)methyl}-p-menthane-3-carboxamide>>
Product name: WS-5, Manufacturer: Symrise <<C3: Menthyl lactate>>
Trade name: Frescolat ML, manufacturer: Symrise Inc. Fragrance compositions A to P shown in Tables 7 to 15 below were used as fragrances.
<評価方法>
被験者4名によって評価した。
歯ブラシ(クリニカアドバンテージ歯ブラシ、4列コンパクトふつう、ライオン(株)製)にサンプルの歯磨剤組成物1gを載せ、3分間歯みがきを行った後、10mLの水で1回、口腔内をすすいだ。サンプルが洗口剤の場合は10mLを口に含み、30秒間洗口したのちに吐出した。使用後の口腔内のねばつき感、使用して60分間経過後の口腔内のすっきり感、口腔内刺激(使用直後の口腔内での刺激感のなさ)を、それぞれ下記の評点基準によって判定し、4名の平均点を求め、下記の評価基準で評価した。<Evaluation method>
It was evaluated by 4 subjects.
1 g of the sample dentifrice composition was placed on a toothbrush (clinica advantage toothbrush, 4-row compact normal, manufactured by Lion Co., Ltd.), and after brushing the teeth for 3 minutes, the oral cavity was rinsed once with 10 mL of water. When the sample was a mouthwash, 10 mL was put in the mouth, washed for 30 seconds, and then discharged. Stickiness in the oral cavity after use, clean feeling in the oral cavity after 60 minutes of use, and oral irritation (absence of irritation in the oral cavity immediately after use) were evaluated according to the following rating criteria. , the average score of 4 people was obtained and evaluated according to the following evaluation criteria.
<口腔内のねばつき感>
評点基準
5:全く感じない
4:あまり感じない
3:どちらともいえない
2:やや感じる
1:非常に感じる
評価基準
◎:4点以上
○:3点以上4点未満
×:3点未満<Sticky feeling in the oral cavity>
Rating criteria 5: Not felt at all 4: Not felt much 3: Neither felt nor felt 2: Somewhat felt 1: Very felt Evaluation criteria ◎: 4 points or more ○: 3 points or more and less than 4 points ×: Less than 3 points
<口腔内のすっきり感>
評点基準
5:非常に感じる
4:感じる
3:どちらともいえない
2:あまり感じない
1:全く感じない
評価基準
◎:4点以上
○:3点以上4点未満
×:3点未満<Clean feeling in the oral cavity>
Rating criteria 5: Strongly felt 4: Fairly felt 3: Neither felt 2: Slightly felted 1: Not felt at all Evaluation criteria ◎: 4 points or more ○: 3 points or more and less than 4 points ×: Less than 3 points
<口腔内刺激>
評点基準
5:全く感じない
4:あまり感じない
3:どちらともいえない
2:やや感じる
1:非常に感じる
評価基準
◎:4点以上
○:3点以上4点未満
×:3点未満<Oral stimulation>
Rating criteria 5: Not felt at all 4: Not felt much 3: Neither felt nor felt 2: Somewhat felt 1: Very felt Evaluation criteria ◎: 4 points or more ○: 3 points or more and less than 4 points ×: Less than 3 points
以下に処方例を示す。使用原料は上記と同様である。 A formulation example is shown below. The raw materials used are the same as above.
[処方例1]歯磨剤
(A)A1:ローズマリーエキス エキス純分として0.0002%
(B)B1:N-(4-シアノメチルフェニル)-2-イソプロピル-5-
メチルシクロヘキサンカルボキサミド 0.001
(C)C1:メンチルモノサクシネート 0.0005
(C)C3:メンチルラクテート 0.0003
(D)研磨性シリカ 15
ソルビット液(70%) 30
プロピレングリコール 4
増粘性シリカ 4
キサンタンガム 1.5
ラウリル硫酸ナトリウム 1.5
フッ化ナトリウム 0.2
サッカリンナトリウム 0.2
香料 1
水 残部
計 100%
(A)/(B)=0.2[Prescription Example 1] Dentifrice (A) A1: Rosemary extract 0.0002% as pure extract content
(B) B1: N-(4-cyanomethylphenyl)-2-isopropyl-5-
Methylcyclohexanecarboxamide 0.001
(C) C1: menthyl monosuccinate 0.0005
(C) C3: menthyl lactate 0.0003
(D) abrasive silica 15
Sorbit solution (70%) 30
Propylene glycol 4
Thickening silica 4
Xanthan gum 1.5
Sodium lauryl sulfate 1.5
Sodium fluoride 0.2
Saccharin sodium 0.2
Perfume 1
water
Total 100%
(A)/(B) = 0.2
[処方例2]洗口剤
(A)A1:ローズマリーエキス エキス純分として0.0002%
(B)B2:N-(2-(2-ピリジニル)エチル)-2-イソプロピル-
5-メチルシクロヘキサンカルボキサミド 0.005
(C)C1:メンチルモノサクシネート 0.0005
(C)C3:メンチルラクテート 0.0003
エタノール 2.0
メントール 0.06
クエン酸 0.05
クエン酸ナトリウム 0.3
ポリオキシエチレン(60)硬化ヒマシ油 0.5
塩化セチルピリジニウム 0.05
パラオキシ安息香酸メチル 0.25
香料 1
水 残部
計 100%
(A)/(B)=0.04[Prescription Example 2] Mouthwash (A) A1: Rosemary extract 0.0002% as pure extract
(B) B2: N-(2-(2-pyridinyl)ethyl)-2-isopropyl-
5-methylcyclohexanecarboxamide 0.005
(C) C1: menthyl monosuccinate 0.0005
(C) C3: menthyl lactate 0.0003
Ethanol 2.0
Menthol 0.06
Citric acid 0.05
Sodium citrate 0.3
Polyoxyethylene (60) hydrogenated castor oil 0.5
Cetylpyridinium chloride 0.05
Methyl paraoxybenzoate 0.25
Perfume 1
water
Total 100%
(A)/(B) = 0.04
[処方例3]洗口剤
(A)A1:ローズマリーエキス エキス純分として0.0002%
(B)B2:N-(2-(2-ピリジニル)エチル)-2-イソプロピル-
5-メチルシクロヘキサンカルボキサミド 0.005
(C)C1:メンチルモノサクシネート 0.0005
(C)C3:メンチルラクテート 0.0003
プロピレングリコール 3.0
メントール 0.06
クエン酸 0.05
クエン酸ナトリウム 0.3
ポリオキシエチレン(60)硬化ヒマシ油 0.5
塩化セチルピリジニウム 0.05
パラオキシ安息香酸メチル 0.25
香料 1
水 残部
計 100%
(A)/(B)=0.04[Prescription Example 3] Mouthwash (A) A1: Rosemary extract 0.0002% as pure extract
(B) B2: N-(2-(2-pyridinyl)ethyl)-2-isopropyl-
5-methylcyclohexanecarboxamide 0.005
(C) C1: menthyl monosuccinate 0.0005
(C) C3: menthyl lactate 0.0003
Propylene glycol 3.0
Menthol 0.06
Citric acid 0.05
Sodium citrate 0.3
Polyoxyethylene (60) hydrogenated castor oil 0.5
Cetylpyridinium chloride 0.05
Methyl paraoxybenzoate 0.25
Perfume 1
water
Total 100%
(A)/(B) = 0.04
Claims (5)
(B)N-(4-シアノメチルフェニル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-1)及びN-(2-(2-ピリジニル)エチル)-2-イソプロピル-5-メチルシクロヘキサンカルボキサミド(B-2)から選ばれる1種以上を0.00001~0.01質量%と
を含有し、(A)/(B)が質量比として0.02~100である口腔用組成物。 (A) Water of one or more plants selected from rosemary, scutellaria root, carrot, sage, licorice, angelica root, persimmon, jack bean and olive, lower monohydric alcohol having 1 to 5 carbon atoms, glycol, or a mixed solvent extraction thereof 0.00001 to 0.05% by mass of the extract as a pure extract content,
(B) N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide (B-1) and N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide An oral composition containing 0.00001 to 0.01% by mass of one or more selected from (B-2), and having a mass ratio of (A)/(B) of 0.02 to 100.
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JP7611783B2 (en) * | 2021-04-21 | 2025-01-10 | 順也 藤森 | Method for producing phytochemical compositions |
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