JP6138538B2 - 口腔用透明液状組成物 - Google Patents
口腔用透明液状組成物 Download PDFInfo
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- JP6138538B2 JP6138538B2 JP2013062843A JP2013062843A JP6138538B2 JP 6138538 B2 JP6138538 B2 JP 6138538B2 JP 2013062843 A JP2013062843 A JP 2013062843A JP 2013062843 A JP2013062843 A JP 2013062843A JP 6138538 B2 JP6138538 B2 JP 6138538B2
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- 239000000216 gellan gum Substances 0.000 description 1
- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- 229930182478 glucoside Natural products 0.000 description 1
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- 239000004220 glutamic acid Substances 0.000 description 1
- 235000013922 glutamic acid Nutrition 0.000 description 1
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- 239000010651 grapefruit oil Substances 0.000 description 1
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- 238000001906 matrix-assisted laser desorption--ionisation mass spectrometry Methods 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
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- 239000012046 mixed solvent Substances 0.000 description 1
- 125000001421 myristyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- RHFUFDFUKULQPY-UHFFFAOYSA-N n'-ethylethane-1,2-diamine;sodium Chemical compound [Na].CCNCCN RHFUFDFUKULQPY-UHFFFAOYSA-N 0.000 description 1
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- 229920003052 natural elastomer Polymers 0.000 description 1
- 229920005615 natural polymer Polymers 0.000 description 1
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- 239000001702 nutmeg Substances 0.000 description 1
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- 239000010452 phosphate Substances 0.000 description 1
- 235000011007 phosphoric acid Nutrition 0.000 description 1
- FIADGNVRKBPQEU-UHFFFAOYSA-N pizotifen Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2CCC2=C1C=CS2 FIADGNVRKBPQEU-UHFFFAOYSA-N 0.000 description 1
- 239000000419 plant extract Substances 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000004323 potassium nitrate Substances 0.000 description 1
- 235000010333 potassium nitrate Nutrition 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- JUJWROOIHBZHMG-UHFFFAOYSA-O pyridinium Chemical compound C1=CC=[NH+]C=C1 JUJWROOIHBZHMG-UHFFFAOYSA-O 0.000 description 1
- 150000003856 quaternary ammonium compounds Chemical class 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 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
- 230000009467 reduction Effects 0.000 description 1
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- 239000010668 rosemary oil Substances 0.000 description 1
- 229940058206 rosemary oil Drugs 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 239000010670 sage oil Substances 0.000 description 1
- 239000012488 sample solution Substances 0.000 description 1
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 description 1
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- 238000000926 separation method Methods 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
- 239000004299 sodium benzoate Substances 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- NTHWMYGWWRZVTN-UHFFFAOYSA-N sodium silicate Chemical compound [Na+].[Na+].[O-][Si]([O-])=O NTHWMYGWWRZVTN-UHFFFAOYSA-N 0.000 description 1
- 229910052911 sodium silicate Inorganic materials 0.000 description 1
- SLBXZQMMERXQAL-UHFFFAOYSA-M sodium;1-dodecoxy-4-hydroxy-1,4-dioxobutane-2-sulfonate Chemical compound [Na+].CCCCCCCCCCCCOC(=O)C(S(O)(=O)=O)CC([O-])=O SLBXZQMMERXQAL-UHFFFAOYSA-M 0.000 description 1
- 239000010676 star anise oil Substances 0.000 description 1
- 125000003696 stearoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 150000003432 sterols Chemical class 0.000 description 1
- 235000003702 sterols Nutrition 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
- 239000005720 sucrose Substances 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 239000008399 tap water Substances 0.000 description 1
- 235000020679 tap water Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 235000019640 taste Nutrition 0.000 description 1
- 239000010677 tea tree oil Substances 0.000 description 1
- 229940111630 tea tree oil Drugs 0.000 description 1
- 239000000892 thaumatin Substances 0.000 description 1
- 235000010436 thaumatin Nutrition 0.000 description 1
- 150000003573 thiols Chemical class 0.000 description 1
- 239000001585 thymus vulgaris Substances 0.000 description 1
- 230000017423 tissue regeneration Effects 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- 239000000606 toothpaste Substances 0.000 description 1
- 229940034610 toothpaste Drugs 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
- XJPBRODHZKDRCB-UHFFFAOYSA-N trans-alpha-ocimene Natural products CC(=C)CCC=C(C)C=C XJPBRODHZKDRCB-UHFFFAOYSA-N 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- 229910021642 ultra pure water Inorganic materials 0.000 description 1
- 239000012498 ultrapure water Substances 0.000 description 1
- 150000004670 unsaturated fatty acids Chemical group 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 239000003021 water soluble solvent Substances 0.000 description 1
- 239000009637 wintergreen oil Substances 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000000811 xylitol 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
- 229960002675 xylitol Drugs 0.000 description 1
- 239000011592 zinc chloride Substances 0.000 description 1
- 235000005074 zinc chloride Nutrition 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
Landscapes
- Cosmetics (AREA)
Description
成分(a): 0.01質量%以上、0.3質量%以下の塩化セチルピリジニウム
成分(b): 0.01質量%以上、0.4質量%以下の、エチレンオキシドの平均付加モル数が10以上、30以下のポリオキシエチレン硬化ヒマシ油
成分(c): 0.01質量%以上、1.0質量%以下のメントール
成分(d): 60質量%以上、99.8質量%以下の水系溶媒
成分(e): 0.01質量%以上、0.3質量%以下で且つ成分(b)の配合量以下の、エチレンオキシドの平均付加モル数が40以上、100以下のポリオキシエチレン硬化ヒマシ油
上記成分(e)は、油溶性成分を組成物中で安定的に分散して透明性を維持するのに有効な成分である。
成分(f): 油溶性薬効成分、メントール以外の油溶性香料、油溶性アルコール、油溶性防腐剤から選択される1種または2種以上の油溶性成分
本発明に用いられる塩化セチルピリジニウムは、第四級アンモニウム化合物に分類されるカチオン性殺菌剤であり、特にう蝕や歯肉炎の原因となる口腔内細菌に対して高い殺菌効果を示すことから、口腔用組成物の薬効成分として広く使用されているものである。
当該成分(b)は、本発明組成物の必須成分であるメントールを可溶化すると共に、薬効成分である塩化セチルピリジニウムをミセル中で過剰に安定化することなく、歯牙や口腔粘膜に対する吸着性を高める重要な成分である。
本発明組成物において、メントールは、組成物の使用時に爽やかな使用感を付与し、嗜好性を顕著に向上させることのできるものであり、口腔用組成物に多用されている香料成分である。また、その作用機序は必ずしも明らかではないが、エチレンオキシドの平均付加モル数が10以上、30以下のポリオキシエチレン硬化ヒマシ油を界面活性剤として使用した場合には、薬効成分である塩化セチルピリジニウムの歯牙や口腔粘膜に対する吸着性を高める効果を示す可能性もある。
本発明に係る組成物は、口腔に用いられる透明な液状のものである。よって、本発明組成物に用いられる溶媒は、生体に害が無い或いは害の少ない水系溶媒とする。
当該成分(e)は、油溶性成分を比較的多く配合する場合に、それらを液状組成物中に安定的に分散して透明性を維持するための成分である。
本発明組成物には、メントールに加え、口腔用組成物へ一般的に配合される油溶性成分を添加してもよい。かかる油溶性成分とは、20℃における水への溶解度が1[g/g−H2O]以下の化合物をいい、具体的には、メントール以外の油溶性香料、油溶性アルコール、油溶性防腐剤をいう。これら油溶性成分は、1種のみを選択して使用してもよいし、2種以上を選択して組合わせて使用してもよい。
本発明の口腔用組成物は、上記成分(a)〜(f)以外に、剤形などに応じて、口腔用組成物に通常用いられる添加剤を、本発明の作用効果を損なわない範囲で適宜添加してもよい。
表1に示す組成の口腔用組成物を調製した。具体的には、適量の精製水にグリセリンとプロピレングリコールを混合し、各成分を添加してよく混合した後、さらに精製水を添加混合した。次いで、pH調整剤としてクエン酸またはクエン酸ナトリウムを適量添加し、組成物のpHを5.8〜6.2の範囲に調整した。なお、表1において、括弧書きの数値は、エチレンオキシド(E.O.)の平均付加モル数を意味する。
調製直後の組成物の外観を目視で観察し、下記判断基準に従い、液体製剤としての透明性を評価した。
○:無色透明
×:白濁または相分離
歯牙エナメル質のモデルとして、ヒドロキシアパタイト粉末(米国BIO−RAD Lab.社製のHydroxyapatite Bio−Gel(登録商標)HTP Gel)(以下、「HA」と略する。)50mgを、紫外線で滅菌したヒト唾液2mL中に37℃で15時間浸漬したものを用意し、ペリクル(唾液タンパク質)の層を上記HA表面に形成させた。その後、3000rpmで10分間遠心処理し、上清を除去した。
◎:外観性状が○で、且つ、CPCの吸着量が840μg以上
○:外観性状が○で、且つ、CPCの吸着量が820μg以上、840μg未満
×:外観性状が×、または外観性状が○で且つCPCの吸着量が820μg未満
成分 配合量
塩化セチルピリジニウム 0.1
ポリオキシエチレン(30)硬化ヒマシ油 0.25
ポリオキシエチレン(60)硬化ヒマシ油 0.05
β−グリチルレチン酸(油溶性薬効成分) 0.01
l−メントール 0.1
パラオキシ安息香酸メチル 0.1
グリセリン 10
プロピレングリコール 3
サッカリンナトリウム 0.01
pH調整剤(クエン酸、クエン酸ナトリウム) 適量
精製水 残部
合計 100
成分 配合量
塩化セチルピリジニウム 0.2
ポリオキシエチレン(20)硬化ヒマシ油 0.2
ポリオキシエチレン(80)硬化ヒマシ油 0.1
イソプルピルメチルフェノール(油溶性薬効成分) 0.05
l−メントール 0.2
グリセリン 9
エタノール 7
サッカリンナトリウム 0.01
pH調整剤(クエン酸、クエン酸ナトリウム) 適量
精製水 残部
合計 100
成分 配合量
塩化セチルピリジニウム 0.3
ポリオキシエチレン(20)硬化ヒマシ油 0.13
ポリオキシエチレン(60)硬化ヒマシ油 0.05
ペパーミント系香料(l−メントール10%含有) 0.1
ソルビトール 10
1,3−ブチレングリコール 5
サッカリンナトリウム 0.01
pH調整剤(リン酸ニ水素ナトリウム、
リン酸一水素ナトリウム) 適量
精製水 残部
合計 100
成分 配合量
塩化セチルピリジニウム 0.3
ポリオキシエチレン(20)硬化ヒマシ油 0.4
ポリオキシエチレン(40)硬化ヒマシ油 0.3
ヒノキチオール(油溶性薬効成分) 0.01
l−メントール 0.3
グリセリン 10
エタノール 3
サッカリンナトリウム 0.01
pH調整剤(クエン酸、クエン酸ナトリウム) 適量
精製水 残部
合計 100
成分 配合量
塩化セチルピリジニウム 0.03
ポリオキシエチレン(10)硬化ヒマシ油 0.01
ポリオキシエチレン(60)硬化ヒマシ油 0.01
l−メントール 0.01
ヒドロキシエチルセルロース 1
グリセリン 30
プロピレングリコール 5.0
サッカリンナトリウム 0.02
pH調整剤(クエン酸、クエン酸ナトリウム) 適量
精製水 残部
合計 100
成分 配合量
塩化セチルピリジニウム 0.3
ポリオキシエチレン(10)硬化ヒマシ油 0.3
ポリオキシエチレン(60)硬化ヒマシ油 0.2
ニコチン酸トコフェロール(油溶性薬効成分) 0.2
l−メントール 0.2
ヒドロキシエチルセルロース 3
グリセリン 30
プロピレングリコール 5
サッカリンナトリウム 0.02
pH調整剤(クエン酸、クエン酸ナトリウム) 適量
精製水 残部
合計 100
成分 配合量
塩化セチルピリジニウム 0.04
ポリオキシエチレン(20)硬化ヒマシ油 0.4
塩酸クロルヘキシジン(油溶性薬効成分) 0.05
ペパーミント油(l−メントール20%含有) 1
硝酸カリウム 5
フッ化ナトリウム 0.2
グリセリン 25
プロピレングリコール 3
ヒドロキシプロピルメチルセルロース 3
pH調整剤(クエン酸、クエン酸ナトリウム) 適量
精製水 残部
合計 100
成分 配合量
塩化セチルピリジニウム 0.01
ポリオキシエチレン(20)硬化ヒマシ油 0.05
オレンジ油(油溶性香料) 0.2
l−メントール 0.05
エタノール 35
グリセリン 10
サッカリンナトリウム 0.1
pH調整剤(クエン酸、クエン酸ナトリウム) 適量
精製水 残部
合計 100
成分 配合量
塩化セチルピリジニウム 0.3
ポリオキシエチレン(20)硬化ヒマシ油 0.2
レモン油(油溶性香料) 0.05
l−メントール 0.15
エタノール 30
グリセリン 5
サッカリンナトリウム 0.1
pH調整剤(クエン酸、クエン酸ナトリウム) 適量
精製水 残部
合計 100
成分 配合量
塩化セチルピリジニウム 0.02
ポリオキシエチレン(20)硬化ヒマシ油 0.04
ポリオキシエチレン(60)硬化ヒマシ油 0.01
l−メントール 0.02
パラオキシ安息香酸メチル 0.005
ソルビトール 30
グリセリン 30
ヒアルロン酸 0.1
ヒドロキシエチルセルロース 1
pH調整剤(リン酸ニ水素ナトリウム、
リン酸一水素ナトリウム) 適量
精製水 残部
合計 100
成分 配合量
塩化セチルピリジニウム 0.1
ポリオキシエチレン(20)硬化ヒマシ油 0.34
ポリオキシエチレン(60)硬化ヒマシ油 0.1
ニコチン酸トコフェロール(油溶性薬効成分) 0.05
スペアミント油 0.3
l−メントール 0.01
トリメチルグリシン 0.5
ソルビトール 20
グリセリン 10
サッカリンナトリウム 0.2
精製水 残部
合計 100
Claims (4)
- 下記の成分(a)、成分(b)、成分(c)および成分(d)を含有することを特徴とする口腔用透明液状組成物。
成分(a): 0.01質量%以上、0.3質量%以下の塩化セチルピリジニウム
成分(b): 0.01質量%以上、0.4質量%以下の、エチレンオキシドの平均付加モル数が10以上、30以下のポリオキシエチレン硬化ヒマシ油
成分(c): 0.01質量%以上、1.0質量%以下のメントール
成分(d): 60質量%以上、99.8質量%以下の水系溶媒 - さらに、下記の成分(e)を含有する請求項1に記載の口腔用透明液状組成物。
成分(e): 0.01質量%以上、0.3質量%以下で且つ成分(b)の配合量以下の、エチレンオキシドの平均付加モル数が40以上、100以下のポリオキシエチレン硬化ヒマシ油 - 成分(a)に対する成分(b)と成分(e)との合計の割合が0.6以上、4.4以下である請求項1または2に記載の口腔用透明液状組成物。
- さらに、下記の成分(f)を含有する請求項1〜3のいずれかに記載の口腔用透明液状組成物。
成分(f): 油溶性薬効成分、メントール以外の油溶性香料、油溶性アルコール、油溶性防腐剤から選択される1種または2種以上の油溶性成分
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