JP4344844B2 - 口腔用組成物 - Google Patents
口腔用組成物 Download PDFInfo
- Publication number
- JP4344844B2 JP4344844B2 JP2004053204A JP2004053204A JP4344844B2 JP 4344844 B2 JP4344844 B2 JP 4344844B2 JP 2004053204 A JP2004053204 A JP 2004053204A JP 2004053204 A JP2004053204 A JP 2004053204A JP 4344844 B2 JP4344844 B2 JP 4344844B2
- Authority
- JP
- Japan
- Prior art keywords
- arbutin
- sodium
- mass
- gums
- conventional method
- 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.)
- Expired - Lifetime
Links
- 239000000203 mixture Substances 0.000 title claims description 31
- BJRNKVDFDLYUGJ-ZIQFBCGOSA-N alpha-Arbutin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-ZIQFBCGOSA-N 0.000 claims description 30
- 229940033280 alpha-arbutin Drugs 0.000 claims description 30
- 239000000551 dentifrice Substances 0.000 claims description 16
- 239000000606 toothpaste Substances 0.000 claims description 15
- 239000007788 liquid Substances 0.000 claims description 6
- 230000003020 moisturizing effect Effects 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 18
- XUMBMVFBXHLACL-UHFFFAOYSA-N Melanin Chemical compound O=C1C(=O)C(C2=CNC3=C(C(C(=O)C4=C32)=O)C)=C2C4=CNC2=C1C XUMBMVFBXHLACL-UHFFFAOYSA-N 0.000 description 16
- 238000007796 conventional method Methods 0.000 description 14
- 238000002360 preparation method Methods 0.000 description 14
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 13
- -1 gums Substances 0.000 description 13
- 238000009472 formulation Methods 0.000 description 12
- 229940034610 toothpaste Drugs 0.000 description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 12
- 239000008213 purified water Substances 0.000 description 11
- 239000003205 fragrance Substances 0.000 description 10
- 239000002674 ointment Substances 0.000 description 10
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 9
- 235000011187 glycerol Nutrition 0.000 description 9
- 239000002202 Polyethylene glycol Substances 0.000 description 8
- 230000002401 inhibitory effect Effects 0.000 description 8
- 230000008099 melanin synthesis Effects 0.000 description 8
- 229920001223 polyethylene glycol Polymers 0.000 description 8
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 description 7
- 239000011627 DL-alpha-tocopherol Substances 0.000 description 7
- 235000001815 DL-alpha-tocopherol Nutrition 0.000 description 7
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 7
- 229940085605 saccharin sodium Drugs 0.000 description 7
- 229960000984 tocofersolan Drugs 0.000 description 7
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 7
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 239000001768 carboxy methyl cellulose Chemical class 0.000 description 6
- 210000000214 mouth Anatomy 0.000 description 6
- 239000002324 mouth wash Substances 0.000 description 6
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical class C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 description 5
- 208000012641 Pigmentation disease Diseases 0.000 description 5
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical class [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 5
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- 102000004190 Enzymes Human genes 0.000 description 4
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- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 4
- 235000014113 dietary fatty acids Nutrition 0.000 description 4
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- 239000011734 sodium Substances 0.000 description 4
- 229910052708 sodium Inorganic materials 0.000 description 4
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 4
- 230000002087 whitening effect Effects 0.000 description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 3
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- 229910000019 calcium carbonate Inorganic materials 0.000 description 3
- XAAHAAMILDNBPS-UHFFFAOYSA-L calcium hydrogenphosphate dihydrate Chemical compound O.O.[Ca+2].OP([O-])([O-])=O XAAHAAMILDNBPS-UHFFFAOYSA-L 0.000 description 3
- 239000004359 castor oil Substances 0.000 description 3
- 229960001927 cetylpyridinium chloride Drugs 0.000 description 3
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 229940112822 chewing gum Drugs 0.000 description 3
- 235000015218 chewing gum Nutrition 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 235000019700 dicalcium phosphate Nutrition 0.000 description 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 3
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 3
- 229940051866 mouthwash Drugs 0.000 description 3
- 239000000049 pigment Substances 0.000 description 3
- 230000019612 pigmentation Effects 0.000 description 3
- 235000012239 silicon dioxide Nutrition 0.000 description 3
- 230000000391 smoking effect Effects 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 description 2
- 239000004382 Amylase Substances 0.000 description 2
- 108010065511 Amylases Proteins 0.000 description 2
- 102000013142 Amylases Human genes 0.000 description 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 2
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 description 2
- MPDGHEJMBKOTSU-UHFFFAOYSA-N Glycyrrhetinsaeure Natural products C12C(=O)C=C3C4CC(C)(C(O)=O)CCC4(C)CCC3(C)C1(C)CCC1C2(C)CCC(O)C1(C)C MPDGHEJMBKOTSU-UHFFFAOYSA-N 0.000 description 2
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- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 description 2
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- 229930006000 Sucrose Natural products 0.000 description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 2
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Landscapes
- Cosmetics (AREA)
- Confectionery (AREA)
Description
口腔粘膜の中でも歯ぐきは色素沈着する頻度が高く、かつ見えやすい部位である。近年のデンタルエステティックに関する意識の高まりから、歯においては美しく白い歯が求められ、ホワイトニングが一般化している。それに併せて、歯ぐきに関しても自然で健康的なピンク色の色調が求められている。
一方、口腔粘膜の変色防止剤としてヒドロキシ-2-ピロリドン誘導体を含有した口腔用組成物が提案されている(例えば、特許文献1参照。)。
しかしながら、従来から用いられる物質の多くは安定性、安全性において問題があり、また色素の沈着を防ぐ効果は未だ十分に満足し得るものでなく、より優れた薬剤の開発が期待されている。
従って本発明は、α−アルブチンを含有することを特徴とする口腔用組成物である。本発明の実施態様では、口腔用組成物中、α−アルブチンを0.001〜10質量%含有させることが適当である。
本明細書中でα−アルブチンとは、ハイドロキノン−α−D−グルコピラノシドを意図し、その構造は以下のとおりである。
本発明の口腔用組成物におけるα−アルブチンの含有量は、本発明が目的とする効果を発揮し且つコストの観点から、口腔組成物の全質量に基づいて0.001〜10質量%が適当であり、好ましくは0.01〜5質量%であり、より好ましくは0.1〜5質量%である。
例えば練歯磨剤といった歯磨剤には、例示すると次のような基剤や添加剤を配合することができる。
研磨剤:結晶質シリカ、非晶質シリカ、その他の無水ケイ酸、含水ケイ酸といったシリカ系研磨剤、アルミノシリケート、酸化アルミニウム、水酸化アルミニウム、不溶性メタリン酸ナトリウム、不溶性メタリン酸カリウム、酸化チタン、第2リン酸カルシウム・2水和物、第2リン酸カルシウム・無水和物、重質炭酸カルシウム、軽質炭酸カルシウム、ピロリン酸カルシウム等(通常配合量3〜99質量%)。
湿潤剤:ソルビット、グリセリン、エチレングリコール、プロピレングリコール、1,3−ブチレングリコール、ポリエチレングリコール、ポリプロピレングリコール、キシリット、マルチット、ラクチットなど(通常配合量1〜50質量%)。
なお、これらの任意成分の添加量は、本発明の効果を防げない範囲で通常量とすることができる。
[メラニン生成抑制作用の試験]
α−アルブチンについて、メラニン生成抑制作用について試験した。
[試験方法および評価方法]
25cm2培養フラスコにマウス由来B16メラノーマ細胞を播種し、10%FBSを含むイーグルMEM培地を用い、二酸化炭素濃度5%、37℃の条件下で培養した。培養24時間後に10%FBSおよびテオフィリン(0.08mg/ml)含有イーグルMEM培地に交換し、α−アルブチンを最終濃度が10、100μg/mlとなるように添加し、混和した。さらに二日間培養後、培地を除去し、リン酸緩衝液で洗浄後、トリプシンおよびEDTA含有培地を使用して細胞をフラスコから剥離させ、細胞懸濁液から遠心分離により細胞を回収した。得られた細胞は10%DMSO含有1N NaOHを加え、80℃で60分間加熱、溶解させ405nmの吸光度を測定し、下記式によりメラニン生成抑制率を求めた。
なお、メラニン量は細胞あたりの量として求めた。また、比較としてβ−アルブチンについても同様に試験を行った。
メラニン生成抑制率(%)={(コントロールメラニン量−試料メラニン量)/コントロールメラニン量}×100
結果を表1に示す。
試験方法は、被検歯磨剤1品につき男性10名とし、毎日、朝と夜の2回、歯ブラシにつけて歯ぐきをマッサージするように使用した。試験は40日行った。より本来の歯ぐきの色にもどることを美白効果として、以下の基準によって評価し、10名のスコアを合計した。その結果を表2に示す。
スコア3 著効
スコア2 有効
スコア1 やや有効
スコア0 無効
以下の処方(単位:質量%)にて、練歯磨剤を常法に従って調製した。
リン酸水素カルシウム無水和物 20.0
リン酸水素カルシウム2水和物 20.0
無水ケイ酸 5.0
カラーギナン 0.7
カルボキシメチルセルロースナトリウム 0.3
グリセリン 20.0
70%ソルビット液 10.0
パラオキシ安息香酸メチル 0.1
トリクロサン 0.1
サッカリンナトリウム 0.1
ラウリル硫酸ナトリウム 1.5
DL−α−トコフェロール 0.1
ポリエチレングリコール 1.0
α−アルブチン 0.1
香料 1.0
精製水 残
100.0%
以下の処方(単位:質量%)にて、練歯磨剤を常法に従って調製した。
無水ケイ酸 20.0
二酸化チタン 0.5
カラーギナン 1.0
プロピレングリコール 3.0
70%ソルビット液 20.0
グリセリン 20.0
パラオキシ安息香酸メチル 0.1
モノフルオロリン酸ナトリウム 0.05
塩化セチルピリジニウム 0.1
ラウリル硫酸ナトリウム 1.7
ラウロイルサルコシンナトリウム 0.3
銅クロロフィリンナトリウム 0.05
DL−α−トコフェロール 0.1
ポリエチレングリコール 1.0
α−アルブチン 0.1
香料 1.0
精製水 残
100.0%
以下の処方(単位:質量%)にて、練歯磨剤を常法に従って調製した。
水酸化アルミニウム 30.0
無水ケイ酸 5.0
塩化ナトリウム 10.0
カルボキシメチルセルロースナトリウム 1.0
グリセリン 20.0
ラウリル硫酸ナトリウム 1.8
イソプロピルメチルフェノール 0.02
酢酸トコフェロール 0.1
ポリオキシエチレン硬化ヒマシ油 3.0
パラオキシ安息香酸エチル 0.1
DL−α−トコフェロール 0.1
ポリエチレングリコール 1.0
α−アルブチン 0.1
香料 1.0
精製水 残
100.0%
以下の処方(単位:質量%)にて、練歯磨剤を常法に従って調製した。
ピロリン酸カルシウム 32.0
無水ケイ酸 6.0
カルボキシメチルセルロースナトリウム 1.0
グリセリン 25.0
グリチルレチン酸 0.2
塩化セチルピリジニウム 0.05
イプシロンアミノカプロン酸 0.1
DL−α−トコフェロール 0.1
ポリエチレングリコール 1.0
α−アルブチン 0.1
香料 0.1
精製水 残
100.0%
以下の処方(単位:質量%)にて、液状歯磨剤を常法に従って調製した。
無水ケイ酸 10.0
キサンタンガム 1.0
グリセリン 10.0
70%ソルビット液 30.0
キシリトール 1.0
パラオキシ安息香酸エチル 0.1
パラオキシ安息香酸ブチル 0.05
リン酸二水素ナトリウム2水和物 0.3
水酸化ナトリウム 0.05
DL−α−トコフェロール 0.1
ポリエチレングリコール 1.0
α−アルブチン 0.1
香料 0.5
精製水 残
100.0%
以下の処方(単位:質量%)にて、洗口液を常法に従って調製した。
エタノール 5.0
ポリオキシエチレン硬化ヒマシ油 0.5
グリセリン 5.0
キシリトール 25.0
塩化セチルピリジニウム 0.05
グリチルリチン酸ジカリウム 0.05
パラオキシ安息香酸エチル 0.05
パラオキシ安息香酸プロピル 0.05
クエン酸 0.03
クエン酸ナトリウム 0.12
黄色4号 0.0002
緑色3号 0.0002
DL−α−トコフェロール 0.1
ポリエチレングリコール 1.0
α−アルブチン 0.1
精製水 残
100.0%
以下の処方(単位:質量%)にて、チューインガムを常法に従って調製した。
ガムベース 40.0
炭酸カルシウム 2.0
水アメ 15.0
砂糖 30.0
クエン酸マグネシウム 2.55
ソルビン酸 0.2
DL−α−トコフェロール 0.1
ポリエチレングリコール 1.0
α−アルブチン 0.1
精製水 残
100.0%
以下の処方(単位:質量%)にて、軟膏を常法に従って調製した。
セタノール 20.0
スクワラン 5.0
ソルビタンモノオレイン酸エステル 1.0
サッカリンナトリウム 0.1
香料 0.3
α−アルブチン 0.1
精製水 残
100.0%
以下の処方(単位:重量%)にて,軟膏を常法に従って調製した
白色ワセリン 10.0
プロピレングリコール 5.0
ステアリルアルコール 10.0
ヒドロキシプロピルセルロース 2.0
ポリエチレングリコール400 60.0
サッカリンナトリウム 0.1
香料 0.3
α−アルブチン 0.1
精製水 残
100.0%
以下の処方(単位:質量%)にて、軟膏を常法に従って調製した。
濃グリセリン 30.0
カルボキシメチルセルロースナトリウム 2.0
サッカリンナトリウム 0.1
香料 0.3
α−アルブチン 0.1
精製水 残
100.0%
以下の処方(単位:質量%)にて、軟膏を常法に従って調製した。
濃グリセリン 30.0
寒天 2.0
サッカリンナトリウム 0.1
香料 0.3
α−アルブチン 0.1
精製水 残
100.0%
以下の処方(単位:重量%)にて、軟膏を常法に従って調製した。
エタノール 1.0
サッカリンナトリウム 0.1
香料 0.3
α−アルブチン 0.1
ゲル化炭化水素 残
100.0%
Claims (4)
- α−アルブチンを含有することを特徴とする歯磨剤組成物。
- 粉歯磨剤、練歯磨剤、液状歯磨剤、潤製歯磨剤及び液体歯磨剤から選ばれる請求項1記載の歯磨剤組成物。
- α−アルブチンを0.001〜10質量%含有する請求項1又は2記載の歯磨剤組成物。
- α−アルブチンを0.1〜1.0質量%含有する請求項3の歯磨剤組成物。
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