JP6911845B2 - 口腔用組成物 - Google Patents
口腔用組成物 Download PDFInfo
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- JP6911845B2 JP6911845B2 JP2018520905A JP2018520905A JP6911845B2 JP 6911845 B2 JP6911845 B2 JP 6911845B2 JP 2018520905 A JP2018520905 A JP 2018520905A JP 2018520905 A JP2018520905 A JP 2018520905A JP 6911845 B2 JP6911845 B2 JP 6911845B2
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- -1 acyl taurine Chemical compound 0.000 claims description 46
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- 239000000230 xanthan gum Substances 0.000 claims description 28
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- 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 claims description 22
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- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 3
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- 238000003860 storage Methods 0.000 description 3
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- IJALWSVNUBBQRA-UHFFFAOYSA-N 4-Isopropyl-3-methylphenol Chemical compound CC(C)C1=CC=C(O)C=C1C IJALWSVNUBBQRA-UHFFFAOYSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- 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 2
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- 229910019142 PO4 Inorganic materials 0.000 description 2
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- MSCCTZZBYHQMQJ-AZAGJHQNSA-N Tocopheryl nicotinate Chemical compound C([C@@](OC1=C(C)C=2C)(C)CCC[C@H](C)CCC[C@H](C)CCCC(C)C)CC1=C(C)C=2OC(=O)C1=CC=CN=C1 MSCCTZZBYHQMQJ-AZAGJHQNSA-N 0.000 description 2
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- A61K8/67—Vitamins
- A61K8/678—Tocopherol, i.e. vitamin E
-
- 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
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- A61K8/25—Silicon; Compounds thereof
-
- 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
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
-
- 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
- A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
-
- 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
- A61K8/67—Vitamins
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- 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
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
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Description
また、口腔用組成物におけるトコフェロール又はその誘導体の安定性改善に関して、特許文献2(特公平7−88292号公報)には、アルキル硫酸エステル塩存在下でトコフェロール又はその誘導体の保存安定性が特定のアミノ酸によって改善すること、特許文献3(特許第4496429号公報)には、ビタミンE又はその誘導体とアニオン性界面活性剤が配合された歯磨剤組成物で、容器内でのビタミンE又はその誘導体の安定性が特定のノニオン性界面活性剤混合物によって維持されること、更に、特許文献4(特開2015−110664号公報)には、アスコルビン酸リン酸エステル又はその塩と共にビタミンE又はその誘導体の保存安定性が、特定のノニオン界面活性剤によって改善することが開示されているが、トコフェロール又はその誘導体の口腔内滞留性については検討されておらず言及もない。
(A)トコフェロール又はその誘導体、
(B)キサンタンガム及びカラギーナン、
(C)アシルアミノ酸、アシルタウリン及びこれらの塩から選ばれる1種又は2種以上のアニオン性界面活性剤
を含有し、(B)成分の含有量が1.2〜3質量%、(C)成分の含有量が0.1〜3質量%であることを特徴とする口腔用組成物
を提供する。
トコフェロール又はその誘導体としては、例えばd−α−トコフェロール、dl−α−トコフェロール、β−トコフェロール、γ−トコフェロール、δ−トコフェロールや、これらの酢酸、ニコチン酸、コハク酸、リノレン酸等の有機酸とのエステル、これらの塩等が挙げられる。このようなトコフェロール誘導体として具体的には、酢酸d−α−トコフェロール、酢酸dl−α−トコフェロール、ニコチン酸d−α−トコフェロール、ニコチン酸dl−α−トコフェロール、コハク酸d−α−トコフェロール、コハク酸dl−α−トコフェロール、リノレン酸d−α−トコフェロール、リノレン酸dl−α−トコフェロール、コハク酸トコフェロールカルシウム等が挙げられる。これらは、1種又は2種以上使用し得るが、中でもdl−α−トコフェロール、酢酸dl−α−トコフェロール、ニコチン酸dl−α−トコフェロール、特に酢酸dl−α−トコフェロールが、製剤外観(色調)が良好である点で好ましい。
なお、上記粘度は、ブルックフィールド型回転粘度計、ローターNo.3、60rpm、25℃、測定時間30秒による値である。
このようなキサンタンガムとしては、市販品、例えばADMファーイースト(株)製のノヴァザン、CPケルコ社製のモナートガムDA、ケルザンT、ケルデント、大日本製薬(株)製のエコーガム等を使用できる。
更に、上記合計配合量の範囲内で、キサンタンガムの配合量は組成物全体の0.6〜2.8%が好ましく、より好ましくは0.9〜2.1%であり、カラギーナンの配合量は組成物全体の0.2〜2.4%が好ましく、より好ましくは0.4〜1.6%である。
アシルアミノ酸及びその塩としては、アシル基が上記炭素数のアシルグルタミン酸塩、アシルアスパラギン酸塩、アシルグリシン塩、特にアシルグルタミン酸塩、とりわけラウロイルグルタミン酸ナトリウムが、他のアミノ酸残基を有するものよりも異味(苦味)が弱く、好適である。
アシルアミノ酸塩としては、例えばN−ラウロイル−L−グルタミン酸ナトリウム、N−ミリストイル−L−グルタミン酸ナトリウム、N−ヤシ油脂肪酸アシル−L−グルタミン酸カリウム等のアシルグルタミン酸塩、N−ラウロイル−L−アスパラギン酸ナトリウム等のアシルアスパラギン酸塩、N−ヤシ油脂肪酸アシルグリシンカリウム等のアシルグリシン塩等が挙げられる。
アシルタウリン塩として具体的には、ココイルメチルタウリンナトリウム、ココイルメチルタウリンカリウム、ラウロイルメチルタウリンナトリウム、ステアロイルメチルタウリンナトリウム、ミリストイルメチルタウリンナトリウム、オレオイルメチルタウリンナトリウム、パルミトイルメチルタウリンナトリウム、ココイルタウリンナトリウムが挙げられる。
これらの中で、アシルメチルタウリン塩、特にラウロイルメチルタウリンナトリウムが好適である。
なお、口腔用組成物では、口腔内に薬用成分を滞留させるには使用後の水すすぎ回数を減らすほうが好ましく、本発明においても、すすぎ易さの観点から、水不溶性粉体、特にシリカ系研磨剤等の研磨剤量は少ないほうが好ましい。本発明組成物は、研磨剤を含まない(研磨剤量0%)、ゲル組成、特に水性ゲル組成の歯磨剤であることが更に好ましい。
これら粘結剤の配合量は、0.5〜10%、特に1〜8%が好ましい。
なお、(B)成分以外の有機粘結剤は、(A)成分の口腔内滞留性や製剤の押し出し性の点で、配合量が0.2%以下、特に0.1%以下であることが好ましく、無配合(0%)とすることも好ましい。
また、塩化ジステアリルメチルアンモニウム等のアルキルアンモニウム型等のカチオン性界面活性剤、ベタイン型、酢酸ベタイン型、イミダゾリン型等の両性界面活性剤を配合することもできる。
これら界面活性剤の配合量は、通常、0.01〜10%、特に0.1〜5%である。
防腐剤としては、パラオキシ安息香酸メチル等のパラオキシ安息香酸エステル、安息香酸ナトリウム等の安息香酸又はその塩等が挙げられる。
また、pH調整剤を添加してもよく、例えば水酸化ナトリウム等のアルカリ金属の水酸化物、炭酸水素塩、炭酸塩、硫酸塩等が挙げられる。
また、配合量も特に限定されないが、上記の香料素材は、組成物中に0.000001〜1%使用するのが好ましい。また、上記香料素材を使用した賦香用香料としては、組成物中に0.1〜2%使用するのが好ましい。
表1〜3に示す組成の歯磨剤組成物を下記方法によって調製し、下記方法で評価した。結果を表に併記した。
製造方法:精製水に水溶性成分を配合後、プロピレングリコールに分散させた(B)成分を投入し混合、次いで香料、(A)成分、(C)成分を順次投入し、脱泡混合して作製した。
なお、使用したキサンタンガムは、塩化カリウムを1%含むキサンタンガム1%水溶液の粘度(ブルックフィールド型回転粘度計、ローターNo.3、60rpm、25℃、測定時間30秒)が約1,500mPa・sであり、カラギーナンはι−カラギーナンである。
歯磨剤組成物を水で3倍希釈した歯磨希釈液40μLを直径10mmにパンチアウトしたハムスターチークポーチ(日本SLC(株)製、3週齢♂Syrian)に載せた。3分間静置後、水で7回洗浄し、エタノール1mLで抽出し、液体クロマトグラフィーにより下記方法で油溶性成分のトコフェロール又はその誘導体を定量した。
測定条件は、内径4.6mm、長さ15cmのステンレス管に5μmの液体クロマトグラフ用オクタデシルシリル化シリカゲルを充填したカラムを用い、メタノールを移動相に用い、カラム温度25℃、1.0mL/分の流量で、紫外吸光光度(測定波長284nm)での絶対検量線法により測定した。
トコフェロール又はその誘導体の口腔内滞留量について、繰り返し3回の平均値を求め、初期値量(最初に処置した3倍希釈液40μL中に含まれるトコフェロール又はその誘導体の量)に対する残存量の割合を算出し、下記基準に従って評価した。
評価基準
◎:滞留量が30%以上
○:滞留量が20%以上30%未満
△:滞留量が10%以上20%未満
×:滞留量が10%未満
歯磨剤組成物を口径8mmのラミネートチューブ容器に50g充填し、各組成3本を−5℃で1ヶ月間保存した後、歯磨剤組成物を押し出し、下記の4段階で押し出し固さの度合いを評価した。
評価基準
◎:スムーズに歯磨剤組成物が押し出せる
○:やや固いが問題なく歯磨剤組成物が押し出せる
△:固くて歯磨剤組成物がやや押し出しにくい
×:固くて歯磨剤組成物が押し出しにくい
口径8mmのラミネートチューブ容器に歯磨剤組成物を充填し、チューブより歯ブラシ上に約1g載せた後、上方向にチューブと歯ブラシを引き離した際の練り切れ(曳糸性)を試験した。曳糸性とは、チューブから取り出した時、歯磨剤組成物が糸を引くように伸びる性状をいい、その長さを測定した。下記基準で評価した。
評価基準
◎:曳糸性が0.5cm未満であり、練り切れが良い
○:0.5cm以上、1cm未満の曳糸性が認められるが使用上問題ない
△:1cm以上、1.5cm未満の曳糸性が認められ、使用上やや問題がある
×:1.5cm以上の曳糸性が認められ、使用上問題がある
(A)トコフェロール酢酸エステル 1.0%
(B)キサンタンガム 1.5
(B)カラギーナン 0.5
(C)ラウロイルメチルタウリンナトリウム 1.0
研磨性シリカ 10
増粘性シリカ 5
70%ソルビット液 40
サッカリンナトリウム 0.2
イソプロピルメチルフェノール 0.1
フッ化ナトリウム 0.21
ポリオキシエチレン(20)硬化ヒマシ油 1.2
ポリオキシエチレン(5)ステアリルエーテル 1.2
プロピレングリコール 3
水酸化ナトリウム 0.1
リン酸二水素ナトリウム 0.1
香料 0.8
精製水 バランス
合計 100.0%
キサンタンガム/カラギーナン比;3 (B)/(C);2
Claims (11)
- (A)トコフェロール又はその誘導体、
(B)キサンタンガム及びカラギーナン、及び
(C)アシルアミノ酸、アシルタウリン及びこれらの塩から選ばれる1種又は2種以上のアニオン性界面活性剤
を含有し、(B)成分の含有量が1.2〜3質量%、(C)成分の含有量が0.1〜3質量%である口腔用組成物。 - キサンタンガム/カラギーナンで表されるキサンタンガムとカラギーナンとの含有質量比が、0.5〜5である請求項1記載の口腔用組成物。
- キサンタンガムの含有量が0.6〜2.8質量%、カラギーナンの含有量が0.2〜2.4質量%である請求項1又は2記載の口腔用組成物。
- (C)成分が、アシル基の炭素数が8〜20であるアシルグルタミン酸塩、アシルアスパラギン酸塩及びアシルグリシン塩、並びにアシル基の炭素数が8〜20であるアシルタウリン塩及びアシルメチルタウリン塩から選ばれる1種又は2種以上のアニオン性界面活性剤である請求項1〜3のいずれか1項記載の口腔用組成物。
- (C)成分以外のアニオン界面活性剤の量が、アニオン界面活性剤総量の50質量%以下である、請求項1〜4のいずれか1項記載の口腔用組成物。
- (B)/(C)で表される(B)成分と(C)成分との含有質量比が、0.5〜10である請求項1〜5のいずれか1項記載の口腔用組成物。
- (A)成分の含有量が0.1〜2質量%である請求項1〜6のいずれか1項記載の口腔用組成物。
- 更に、研磨剤を10質量%含有する請求項1〜7のいずれか1項記載の口腔用組成物。
- 研磨剤を含有しない請求項1〜8のいずれか1項記載の口腔用組成物。
- 更に、無機粘結剤を0.5〜10質量%含有する請求項1〜9のいずれか1項記載の口腔用組成物。
- 歯磨剤である請求項1〜10のいずれか1項記載の口腔用組成物。
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