JP7455317B2 - 口腔用組成物 - Google Patents
口腔用組成物 Download PDFInfo
- Publication number
- JP7455317B2 JP7455317B2 JP2017129902A JP2017129902A JP7455317B2 JP 7455317 B2 JP7455317 B2 JP 7455317B2 JP 2017129902 A JP2017129902 A JP 2017129902A JP 2017129902 A JP2017129902 A JP 2017129902A JP 7455317 B2 JP7455317 B2 JP 7455317B2
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- JP
- Japan
- Prior art keywords
- sodium
- acid
- browning
- salt
- extract
- 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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- 239000000203 mixture Substances 0.000 title claims description 74
- 150000003839 salts Chemical class 0.000 claims description 52
- RHFUXPCCELGMFC-UHFFFAOYSA-N n-(6-cyano-3-hydroxy-2,2-dimethyl-3,4-dihydrochromen-4-yl)-n-phenylmethoxyacetamide Chemical compound OC1C(C)(C)OC2=CC=C(C#N)C=C2C1N(C(=O)C)OCC1=CC=CC=C1 RHFUXPCCELGMFC-UHFFFAOYSA-N 0.000 claims description 37
- 235000019410 glycyrrhizin Nutrition 0.000 claims description 35
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims description 27
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- -1 polyoxyethylene Polymers 0.000 claims description 27
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 24
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 claims description 24
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- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 20
- 229960004949 glycyrrhizic acid Drugs 0.000 claims description 20
- 229910001515 alkali metal fluoride Inorganic materials 0.000 claims description 19
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- LPLVUJXQOOQHMX-UHFFFAOYSA-N glycyrrhetinic acid glycoside Natural products C1CC(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2=O)C(O)=O)C)(C)CC2)(C)C2C(C)(C)C1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O LPLVUJXQOOQHMX-UHFFFAOYSA-N 0.000 claims description 18
- 239000001685 glycyrrhizic acid Substances 0.000 claims description 18
- UYRUBYNTXSDKQT-UHFFFAOYSA-N glycyrrhizic acid Natural products CC1(C)C(CCC2(C)C1CCC3(C)C2C(=O)C=C4C5CC(C)(CCC5(C)CCC34C)C(=O)O)OC6OC(C(O)C(O)C6OC7OC(O)C(O)C(O)C7C(=O)O)C(=O)O UYRUBYNTXSDKQT-UHFFFAOYSA-N 0.000 claims description 18
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 10
- 235000011187 glycerol Nutrition 0.000 claims description 10
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- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 10
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- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 6
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 6
- 239000000843 powder Substances 0.000 claims description 5
- WNIFXKPDILJURQ-UHFFFAOYSA-N stearyl glycyrrhizinate Natural products C1CC(O)C(C)(C)C2CCC3(C)C4(C)CCC5(C)CCC(C(=O)OCCCCCCCCCCCCCCCCCC)(C)CC5C4=CC(=O)C3C21C WNIFXKPDILJURQ-UHFFFAOYSA-N 0.000 claims description 5
- CAKDFKUXFMLCAR-UIOGXPPZSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4S,5S,6S)-2-[[(3S,4aR,6aR,6bS,8aS,11S,12aR,14aR,14bS)-11-methoxycarbonyl-4,4,6a,6b,8a,11,14b-heptamethyl-14-oxo-2,3,4a,5,6,7,8,9,10,12,12a,14a-dodecahydro-1H-picen-3-yl]oxy]-6-carboxy-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@]([C@@]3(CC[C@H]2C1(C)C)C)(C)CC[C@@]1(C)CC[C@](C[C@H]14)(C)C(=O)OC)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O CAKDFKUXFMLCAR-UIOGXPPZSA-N 0.000 claims description 4
- IJALWSVNUBBQRA-UHFFFAOYSA-N 4-Isopropyl-3-methylphenol Chemical compound CC(C)C1=CC=C(O)C=C1C IJALWSVNUBBQRA-UHFFFAOYSA-N 0.000 claims description 4
- 102000008186 Collagen Human genes 0.000 claims description 4
- 108010035532 Collagen Proteins 0.000 claims description 4
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 4
- 229920001436 collagen Polymers 0.000 claims description 4
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- 239000001509 sodium citrate Substances 0.000 claims description 4
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- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 3
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- 229960001927 cetylpyridinium chloride Drugs 0.000 claims 6
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 claims 6
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- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims 4
- MIDXCONKKJTLDX-UHFFFAOYSA-N 3,5-dimethylcyclopentane-1,2-dione Chemical compound CC1CC(C)C(=O)C1=O MIDXCONKKJTLDX-UHFFFAOYSA-N 0.000 claims 3
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- WINXNKPZLFISPD-UHFFFAOYSA-M Saccharin sodium Chemical compound [Na+].C1=CC=C2C(=O)[N-]S(=O)(=O)C2=C1 WINXNKPZLFISPD-UHFFFAOYSA-M 0.000 claims 3
- OEWBEINAQKIQLZ-CMRBMDBWSA-N [(2s)-2-[(2r)-3,4-bis(2-hexyldecanoyloxy)-5-oxo-2h-furan-2-yl]-2-(2-hexyldecanoyloxy)ethyl] 2-hexyldecanoate Chemical compound CCCCCCCCC(CCCCCC)C(=O)OC[C@H](OC(=O)C(CCCCCC)CCCCCCCC)[C@H]1OC(=O)C(OC(=O)C(CCCCCC)CCCCCCCC)=C1OC(=O)C(CCCCCC)CCCCCCCC OEWBEINAQKIQLZ-CMRBMDBWSA-N 0.000 claims 3
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- HELXLJCILKEWJH-NCGAPWICSA-N rebaudioside A Chemical compound O([C@H]1[C@H](O)[C@@H](CO)O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O HELXLJCILKEWJH-NCGAPWICSA-N 0.000 description 1
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- SFVFIFLLYFPGHH-UHFFFAOYSA-M stearalkonium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 SFVFIFLLYFPGHH-UHFFFAOYSA-M 0.000 description 1
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- 229910001631 strontium chloride Inorganic materials 0.000 description 1
- AHBGXTDRMVNFER-UHFFFAOYSA-L strontium dichloride Chemical compound [Cl-].[Cl-].[Sr+2] AHBGXTDRMVNFER-UHFFFAOYSA-L 0.000 description 1
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Landscapes
- Medicinal Preparation (AREA)
- Cosmetics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
項1. (A)グリチルリチン酸、その誘導体、及び/又はそれらの塩と、(B)ヒアルロン酸及び/又はその塩と、(C)アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩と、(D)水とを含有する、口腔用組成物。
項2. 前記(B)成分の含有量(重量%)に対する前記(C)成分のフッ素原子の含有量(重量%)の比率が0.002~200である、項1に記載の口腔組成物。
項3. 前記(B)成分の含有量(重量%)に対する前記(C)成分のフッ素原子含有量(重量%)の比率が0.18~14.5である、項1又は2に記載の口腔組成物。
項4. (A)グリチルリチン酸、その誘導体、及び/又はそれらの塩と、(B)ヒアルロン酸及び/又はその塩と、(D)水とを含有する口腔用組成物における褐変を抑制するために使用される褐変抑制剤であって、
(C)アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩を有効成分とする、褐変抑制剤。
項5. (A)グリチルリチン酸、その誘導体、及び/又はそれらの塩と、(B)ヒアルロン酸及び/又はその塩と、(D)水とを含有する口腔用組成物において褐変を抑制する褐変抑制方法であって、
口腔用組成物に、前記(A)成分と前記(B)成分と前記(D)成分と共に、(C)アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩を配合する、褐変抑制方法。
本発明の口腔用組成物は、グリチルリチン酸、その誘導体、及び/又はそれらの塩(以下、 (A)成分と表記することがある)と、ヒアルロン酸及び/又はその塩(以下、(B)成分と表記することがある)と、アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩(以下、(C)成分と記載することがある)と、水(以下、(D)成分と表記することがある)とを含有する。以下、本発明の口腔用組成物について詳述する。
本発明の口腔用組成物は、(A)成分として、グリチルリチン酸、その誘導体、及び/又はそれらの塩を含有する。
本発明の口腔用組成物は、(B)成分として、ヒアルロン酸及び/又はその塩を含有する。ヒアルロン酸及び/又はその塩は、保湿作用または湿潤作用を有する公知の成分である。
(式) 極限粘度(dL/g)=3.6×10-4M0.78
本発明の口腔用組成物は、(C)成分として、アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩を含有する。これらのフッ素化合物は、殺菌作用を有することが知られている公知の薬剤である。本発明においては、フッ素化合物は、(A)成分、(B)成分及び(D)成分と共存させることによって、高温で保存した際に生じる褐変を、沈殿物を生じさせることなく抑制することができる。
本発明の口腔用組成物は、基剤として水を含有する。(A)成分と(B)成分とを含む水性組成物を高温条件下で保存すると、褐変を生じる傾向を示すが、本発明の口腔用組成物によれば、このような褐変を、沈殿物を生じさせることなく効果的に抑制することができる。
本発明の口腔用組成物は、前述する成分以外に、本発明の効果を損なわない範囲で、口腔用組成物の製剤形態に応じて、当該技術分野で通常使用される成分を含有していてもよい。このような成分としては、例えば、防腐剤、殺菌剤、抗菌剤、消炎剤、研磨剤、グルコシルトランスフェラーゼ(GTase)阻害剤、プラーク抑制剤、知覚過敏抑制剤、歯石予防剤、増粘剤、湿潤剤、賦形剤、香料、甘味剤、清涼化剤、色素、消臭剤、界面活性剤、溶剤、pH調整剤等が挙げられる。
また、本発明の口腔用組成物のpHについては、口腔内への適用が許容される範囲で適宜設定すればよいが、例えば、4~9、好ましくは6~8.5が挙げられる。ここで、pHとは、25℃の温度条件下で測定される値である。
本発明の口腔用組成物の剤型については、口腔内に適用可能であることを限度として特に制限されないが、例えば、液状又は半固形状(ゲル状、ペースト状)が挙げられる。
前述するように、アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩は、グリチルリチン酸類、ヒアルロン酸及び/又はその塩、及び水を含む口腔用組成物において、高温で保存した際に生じる褐変を、沈殿物を生じさせることなく抑制することができる。従って、本発明は、更に、グリチルリチン酸類、ヒアルロン酸及び/又はその塩、及び水を含む口腔用組成物における高温保存により生じる褐変を沈殿を生じることなく抑制するために使用される褐変抑制剤であって、アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩を有効成分とする褐変抑制剤を提供する。また、本発明は、グリチルリチン酸類、ヒアルロン酸及び/又はその塩、及び水を含む口腔用組成物、高温で保存した際に生じる褐変を、沈殿物を生じさせることなく抑制する褐変析出抑制方法であって、口腔用組成物に、グリチルリチン酸類、ヒアルロン酸及び/又はその塩、及び水と共に、アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩を配合する、褐変抑制方法を提供する。
表1及び表2に示す組成の液剤を調製した。表1及び表2に示す組成において、それぞれの配合量の単位は重量%である。また、ヒアルロン酸ナトリウムは、平均分子量(Mw)が1,890のもの(ヒアロナノ、キユーピー株式会社製)、2,480又は5,000のもの(ヒアロオリゴ、キユーピー株式会社製)、14,030のもの(ヒアルロンサンHA-LF5-A、キユーピー株式会社製)、878,000のもの(ヒアベスト(J) 、キユーピー株式会社製)、1,827,000(ヒアルロンサンHA-LQH、キユーピー株式会社製)を用いた。
◎:褐変は全く認められない。
○:僅かな褐変しか認められず、液剤全体的に澄明な状態が維持できている。
×:褐変が認められ、澄明な状態が失われている。
◎:沈殿物は全く認められない。
×:容器の底に沈殿物が少し生成している。
××:容器の底に沈殿物が多量に生成している。
表3~11に示す組成の練歯磨剤、表12に示す組成の洗口液、表13に示す組成のマウススプレー剤を製造した。なお、表3~13において、各成分の含有量の単位は、重量%である。得られた各口腔用組成物については、いずれも保存後に褐変及び沈殿物の生成を抑制できていた。
Claims (3)
- (A)グリチルリチン酸、グリチルリチン酸メチル、グリチルリチン酸ステアリル、及び/又はそれらの塩と、(B)ヒアルロン酸及び/又はその塩と、(C)アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩と、(D)水とを含有し、
前記(B)成分の含有量(重量%)に対する前記(C)成分のフッ素原子含有量(重量%)の比率が0.18~14.5である、口腔用組成物(但し、ピグメントホワイト18、ソルビトール、グリセリン、キシリトール、茶抽出物、テアニン、シリカ、キサンタンガム、エトキシル化水添ヒマシ油(加水分解)、レモン果実エキス、メントール、サッカリンナトリウム、ラウリル硫酸ナトリウム、及びカラメルを含む練歯磨と;グリセリン、プロピレングリコール、ポリオキシエチレン硬化ヒマシ油、キシリトール、ラウリル硫酸ナトリウム、香料、クエン酸、水酸化ナトリウム、塩化セチルピリジニウム、イソプロピルメチルフェノール、ポリビニルピロリドン、アロエエキス及びポリリン酸ナトリウムを含む歯みがきと;ソルビット、グリセリン、無水ケイ酸、ポリオキシエチレン硬化ヒマシ油、エタノール、マクロゴール 400、塩化セチルピリジニウム、キシリトール、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、香料、ラウリル硫酸ナトリウム、クエン酸ナトリウム、クエン酸、l -メントール、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、チャ乾溜液、テトラ2-ヘキシルデカン酸アスコルビル、アロエエキス、加水分解コラーゲン液、プラセンタエキス、パール末、及び着色剤を含む歯磨き剤と、を除く)。 - (A)グリチルリチン酸、グリチルリチン酸メチル、グリチルリチン酸ステアリル、及び/又はそれらの塩と、(B)ヒアルロン酸及び/又はその塩と、(D)水とを含有する口腔用組成物(但し、ピグメントホワイト18、ソルビトール、グリセリン、キシリトール、茶抽出物、テアニン、シリカ、キサンタンガム、エトキシル化水添ヒマシ油(加水分解)、レモン果実エキス、メントール、サッカリンナトリウム、ラウリル硫酸ナトリウム、及びカラメルを含む練歯磨と;グリセリン、プロピレングリコール、ポリオキシエチレン硬化ヒマシ油、キシリトール、ラウリル硫酸ナトリウム、香料、クエン酸、水酸化ナトリウム、塩化セチルピリジニウム、イソプロピルメチルフェノール、ポリビニルピロリドン、アロエエキス及びポリリン酸ナトリウムを含む歯みがきと;ソルビット、グリセリン、無水ケイ酸、ポリオキシエチレン硬化ヒマシ油、エタノール、マクロゴール 400、塩化セチルピリジニウム、キシリトール、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、香料、ラウリル硫酸ナトリウム、クエン酸ナトリウム、クエン酸、l -メントール、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、チャ乾溜液、テトラ2-ヘキシルデカン酸アスコルビル、アロエエキス、加水分解コラーゲン液、プラセンタエキス、パール末、及び着色剤を含む歯磨き剤と、を除く)における褐変を抑制するために使用される褐変抑制剤であって、
(C)アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩を有効成分とする、褐変抑制剤。 - (A)グリチルリチン酸、グリチルリチン酸メチル、グリチルリチン酸ステアリル、及び/又はそれらの塩と、(B)ヒアルロン酸及び/又はその塩と、(D)水とを含有する口腔用組成物(但し、ピグメントホワイト18、ソルビトール、グリセリン、キシリトール、茶抽出物、テアニン、シリカ、キサンタンガム、エトキシル化水添ヒマシ油(加水分解)、レモン果実エキス、メントール、サッカリンナトリウム、ラウリル硫酸ナトリウム、及びカラメルを含む練歯磨と;グリセリン、プロピレングリコール、ポリオキシエチレン硬化ヒマシ油、キシリトール、ラウリル硫酸ナトリウム、香料、クエン酸、水酸化ナトリウム、塩化セチルピリジニウム、イソプロピルメチルフェノール、ポリビニルピロリドン、アロエエキス及びポリリン酸ナトリウムを含む歯みがきと;ソルビット、グリセリン、無水ケイ酸、ポリオキシエチレン硬化ヒマシ油、エタノール、マクロゴール 400、塩化セチルピリジニウム、キシリトール、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、香料、ラウリル硫酸ナトリウム、クエン酸ナトリウム、クエン酸、l -メントール、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、チャ乾溜液、テトラ2-ヘキシルデカン酸アスコルビル、アロエエキス、加水分解コラーゲン液、プラセンタエキス、パール末、及び着色剤を含む歯磨き剤と、を除く)において褐変を抑制する褐変抑制方法であって、
口腔用組成物に、前記(A)成分と前記(B)成分と前記(D)成分と共に、(C)アルカリ金属のフッ化物、フルオロリン酸、及び/又はフルオロリン酸の塩を配合する、褐変抑制方法。
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