JP2017007997A - Liquid composition for oral cavity - Google Patents
Liquid composition for oral cavity Download PDFInfo
- Publication number
- JP2017007997A JP2017007997A JP2015127630A JP2015127630A JP2017007997A JP 2017007997 A JP2017007997 A JP 2017007997A JP 2015127630 A JP2015127630 A JP 2015127630A JP 2015127630 A JP2015127630 A JP 2015127630A JP 2017007997 A JP2017007997 A JP 2017007997A
- Authority
- JP
- Japan
- Prior art keywords
- composition
- feeling
- liquid oral
- salt
- oral cavity
- 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.)
- Abandoned
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 69
- 239000007788 liquid Substances 0.000 title claims abstract description 44
- 210000000214 mouth Anatomy 0.000 title claims abstract description 25
- -1 ascorbic acid ester Chemical class 0.000 claims abstract description 54
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Natural products OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims abstract description 37
- 150000003839 salts Chemical class 0.000 claims abstract description 34
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims abstract description 26
- 235000010323 ascorbic acid Nutrition 0.000 claims abstract description 26
- 229960005070 ascorbic acid Drugs 0.000 claims abstract description 26
- 239000011668 ascorbic acid Substances 0.000 claims abstract description 26
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 claims abstract description 18
- 235000011007 phosphoric acid Nutrition 0.000 claims abstract description 15
- 150000005846 sugar alcohols Polymers 0.000 claims abstract description 14
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 claims description 31
- 229910019142 PO4 Inorganic materials 0.000 claims description 18
- 229910052731 fluorine Inorganic materials 0.000 claims description 17
- 239000011737 fluorine Substances 0.000 claims description 17
- 239000011775 sodium fluoride Substances 0.000 claims description 16
- 235000013024 sodium fluoride Nutrition 0.000 claims description 16
- 239000010452 phosphate Substances 0.000 claims description 13
- 150000001875 compounds Chemical class 0.000 claims description 12
- 239000002324 mouth wash Substances 0.000 claims description 12
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 claims description 11
- 229940051866 mouthwash Drugs 0.000 claims description 11
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 claims description 9
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 claims description 8
- 229960004711 sodium monofluorophosphate Drugs 0.000 claims description 8
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims description 7
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 7
- 239000001257 hydrogen Substances 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- ZPWVASYFFYYZEW-UHFFFAOYSA-L dipotassium hydrogen phosphate Chemical compound [K+].[K+].OP([O-])([O-])=O ZPWVASYFFYYZEW-UHFFFAOYSA-L 0.000 claims description 3
- GNSKLFRGEWLPPA-UHFFFAOYSA-M potassium dihydrogen phosphate Chemical compound [K+].OP(O)([O-])=O GNSKLFRGEWLPPA-UHFFFAOYSA-M 0.000 claims description 3
- YUOWTJMRMWQJDA-UHFFFAOYSA-J tin(iv) fluoride Chemical compound [F-].[F-].[F-].[F-].[Sn+4] YUOWTJMRMWQJDA-UHFFFAOYSA-J 0.000 claims description 3
- 230000000694 effects Effects 0.000 description 19
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 18
- 235000021317 phosphate Nutrition 0.000 description 17
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 14
- 235000019606 astringent taste Nutrition 0.000 description 13
- 235000019658 bitter taste Nutrition 0.000 description 13
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 12
- 238000002156 mixing Methods 0.000 description 10
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 9
- 239000000194 fatty acid Substances 0.000 description 9
- 239000003205 fragrance Substances 0.000 description 8
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 7
- 235000014113 dietary fatty acids Nutrition 0.000 description 7
- 229930195729 fatty acid Natural products 0.000 description 7
- 235000011187 glycerol Nutrition 0.000 description 7
- 239000008213 purified water Substances 0.000 description 7
- 239000000126 substance Substances 0.000 description 7
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- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 6
- 238000011156 evaluation Methods 0.000 description 6
- KWIUHFFTVRNATP-UHFFFAOYSA-N glycine betaine Chemical compound C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 6
- 238000000034 method Methods 0.000 description 6
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- 235000010994 magnesium phosphates Nutrition 0.000 description 5
- 239000002253 acid Substances 0.000 description 4
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- 238000013329 compounding Methods 0.000 description 4
- 230000002265 prevention Effects 0.000 description 4
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- 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 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
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- 239000004359 castor oil Substances 0.000 description 3
- 235000019438 castor oil Nutrition 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 3
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- 238000002360 preparation method Methods 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- 229910052708 sodium Inorganic materials 0.000 description 3
- 239000001509 sodium citrate Substances 0.000 description 3
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 3
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- 239000002562 thickening agent Substances 0.000 description 3
- XHXUANMFYXWVNG-ADEWGFFLSA-N (-)-Menthyl acetate Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1OC(C)=O XHXUANMFYXWVNG-ADEWGFFLSA-N 0.000 description 2
- ULDHMXUKGWMISQ-SECBINFHSA-N (-)-carvone Chemical compound CC(=C)[C@@H]1CC=C(C)C(=O)C1 ULDHMXUKGWMISQ-SECBINFHSA-N 0.000 description 2
- INAXVXBDKKUCGI-UHFFFAOYSA-N 4-hydroxy-2,5-dimethylfuran-3-one Chemical compound CC1OC(C)=C(O)C1=O INAXVXBDKKUCGI-UHFFFAOYSA-N 0.000 description 2
- GHBSPIPJMLAMEP-UHFFFAOYSA-N 6-pentyloxan-2-one Chemical compound CCCCCC1CCCC(=O)O1 GHBSPIPJMLAMEP-UHFFFAOYSA-N 0.000 description 2
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Abstract
Description
本発明は、優れた実効感(歯ぐきの引き締め感)を与えるアスコルビン酸エステル又はその塩含有の液体口腔用組成物に関する。 The present invention relates to a liquid oral composition containing an ascorbic acid ester or a salt thereof that gives an excellent feeling of effectiveness (a feeling of tightening gums).
アスコルビン酸は生体中で酵素活性発現に重要な役割を演じ、多様な生理活性を持つことが知られている。特にプロリル及びリジルヒドロキシラーゼの補酵素として作用し、コラーゲン合成に必須であるとされている。このため、コラーゲンの破壊に伴う歯肉炎、歯周炎の予防、治療に有用であり、従来から種々のアスコルビン酸誘導体が開発され、特にアスコルビン酸リン酸エステル等のアスコルビン酸エステル又はその塩が注目されている。アスコルビン酸エステル又はその塩を口腔用組成物に用いた技術は、数多く提案され、例えば特許文献1〜7に開示されている。 Ascorbic acid plays an important role in the expression of enzyme activity in the living body and is known to have various physiological activities. In particular, it acts as a coenzyme for prolyl and lysyl hydroxylase, and is essential for collagen synthesis. For this reason, it is useful for the prevention and treatment of gingivitis and periodontitis associated with collagen destruction, and various ascorbic acid derivatives have been developed in the past. In particular, ascorbic acid esters such as ascorbic acid phosphates or their salts have attracted attention. Has been. Many techniques using ascorbic acid esters or salts thereof in oral compositions have been proposed, and are disclosed in, for example, Patent Documents 1-7.
一方、口腔用組成物において、特に使用直後にその効果を使用者に実感させることは、継続的な使用やそれによる効果向上の点で有意義であり、アスコルビン酸エステル又はその塩含有の口腔用組成物においても同様である。 On the other hand, in the oral composition, it is significant in terms of continuous use and improvement in the effect that the user feels the effect immediately after use, and the oral composition containing ascorbic acid ester or a salt thereof is significant. The same applies to objects.
歯肉炎、歯周炎の予防や治療の実効感としては、使用後の適度な歯ぐきの引き締め感を付与することが好ましい。しかしながら、アスコルビン酸エステル又はその塩を配合した口腔用組成物では、その効果を実感させることが難しく、効果実感については今まで考慮されていないのが現状であった。 As an effective feeling of prevention and treatment of gingivitis and periodontitis, it is preferable to give an appropriate feeling of tightening gums after use. However, with oral compositions containing ascorbic acid esters or salts thereof, it is difficult to realize the effect, and the actual effect has not been considered so far.
本発明は、上記事情に鑑みなされたもので、優れた実効感(歯ぐきの引き締め感)を与えるアスコルビン酸エステル又はその塩含有の口腔用組成物を提供することを目的とする。 This invention is made | formed in view of the said situation, and it aims at providing the composition for oral cavity containing ascorbic acid ester or its salt which gives the outstanding effective feeling (feeling of tightening gums).
本発明者は、上記目的を達成するため鋭意検討を行った結果、アスコルビン酸エステル又はその塩として(A)アスコルビン酸リン酸エステル及び/又はその塩を特定量配合した液体口腔用組成物に、(B)フッ素イオン、特にその供給源としてフッ素含有化合物と、(C)オルトリン酸及び/又はその塩とを各々特定量で組み合わせて配合することによって、優れた実効感(歯ぐきの引き締め感)を与え、満足な効果実感を付与できることを知見し、本発明をなすに至った。 As a result of intensive studies to achieve the above object, the present inventor, as a liquid oral composition containing a specific amount of (A) ascorbic acid phosphate and / or a salt thereof as an ascorbic acid ester or a salt thereof, (B) Fluorine ions, particularly fluorine-containing compounds as their supply source, and (C) orthophosphoric acid and / or a salt thereof are combined in specific amounts to provide an excellent sense of effectiveness (feeling of tightening gums). The inventors have found that a satisfactory effect can be imparted, and have made the present invention.
即ち、アスコルビン酸リン酸エステル及び/又はその塩を配合した口腔用組成物における使用後の引き締め感の検討において、アスコルビン酸リン酸エステル及び/又はその塩には歯ぐきの引き締め感がなく、また、フッ素含有化合物、オルトリン酸及び/又はその塩にも歯ぐきの引き締め感がなく、即ち、これら3成分は各々単独では歯ぐきの引き締め感を与えることがないが、意外にも、本発明では、(A)、(B)、(C)成分を組み合わせると、各々の配合量が特定範囲内において、これら3成分が相互作用して歯ぐきの引き締め感が発現し、効果を実感させ難い洗口剤等の液体口腔用組成物であっても優れた歯ぐきの引き締め感を付与し、使用直後においてもその効果を十分に実感させることができる。
更に、(D)多価アルコール及び/又は糖アルコールを添加すると、(B)、(C)成分により生じる渋味・苦味・異味を改善し、使用感(渋味・苦味・異味のなさ)に優れた液体口腔用組成物とすることができる。
That is, in the examination of the tightening feeling after use in the oral composition containing ascorbic acid phosphate ester and / or salt thereof, ascorbic acid phosphate ester and / or salt thereof does not have a feeling of tightening gums, Fluorine-containing compounds, orthophosphoric acid and / or salts thereof do not have a feeling of tightening gums, that is, each of these three components alone does not give a feeling of tightening gums. ), (B), and (C), when combined, within a specific range, these three components interact to produce a feeling of tightening the gums, making it difficult to realize the effect of mouthwash, etc. Even if it is a composition for liquid oral cavity, the feeling of tightening excellent gums can be imparted and the effect can be fully realized even immediately after use.
Furthermore, when (D) polyhydric alcohol and / or sugar alcohol is added, the astringency, bitterness and off-taste caused by the components (B) and (C) are improved, and the feeling of use (no astringency, bitterness or off-taste) is achieved. An excellent liquid oral composition can be obtained.
なお、フッ化ナトリウム、モノフルオロリン酸ナトリウムといったフッ素含有化合物は、従来、歯面に作用することでう蝕予防効果を発揮する成分として知られているが、本発明では、このようなフッ素含有化合物から供給される(B)フッ素イオンが、(A)アスコルビン酸リン酸エステル及び/又はその塩、(C)オルトリン酸及び/又はその塩との共存により、予想外に歯ぐきに作用して歯ぐきの引き締め感を与え、液体口腔用組成物で格別顕著な作用効果を奏する。 Note that fluorine-containing compounds such as sodium fluoride and sodium monofluorophosphate are conventionally known as components that exert a caries prevention effect by acting on the tooth surface. In the present invention, such fluorine-containing compounds are known. (B) Fluorine ions supplied from the compound unexpectedly act on gums due to coexistence with (A) ascorbic acid phosphate and / or salt thereof, (C) orthophosphoric acid and / or salt thereof, and gum The liquid oral composition provides a particularly remarkable action and effect.
特許文献1、2には、アスコルビン酸リン酸エステル塩、フッ素含有化合物、リン酸水素二ナトリウムを含有する研磨剤配合の歯磨剤が記載され、また、特許文献3、4は、フッ素イオン、カルシウムイオンによるコロイド化促進に有効な物質としてアスコルビン酸誘導体、リン酸のアルカリ金属塩を使用し得ることを開示するが、これら特許文献1〜4では、アスコルビン酸エステル又はその塩含有の液体口腔用組成物の実効感(歯ぐきの引き締め感)について検討されておらず、言及もなく、特許文献5〜7にも言及されていない。特許文献1〜7から、本発明にかかわる(A)、(B)、(C)成分の組み合わせに特異な実効感(歯ぐきの引き締め感)の付与は予測できない。 Patent Documents 1 and 2 describe a dentifrice containing an ascorbic acid phosphate ester salt, a fluorine-containing compound and a disodium hydrogen phosphate, and Patent Documents 3 and 4 describe fluorine ions and calcium. It is disclosed that an ascorbic acid derivative or an alkali metal salt of phosphoric acid can be used as a substance effective for promoting colloidalization by ions. In these Patent Documents 1 to 4, a liquid oral composition containing an ascorbic acid ester or a salt thereof is disclosed. The effective feeling of the object (feeling of tightening the gums) has not been studied, nor is it mentioned, nor is it mentioned in Patent Documents 5-7. From Patent Documents 1 to 7, it is not possible to predict the provision of a specific effect (gum tightness) specific to the combination of the components (A), (B), and (C) according to the present invention.
従って、本発明は下記の液体口腔用組成物を提供する。
〔1〕
(A)アスコルビン酸リン酸エステル及び/又はその塩 0.1〜1質量%、
(B)フッ素イオン 5〜4,530ppm、
(C)オルトリン酸及び/又はその塩 0.01〜1質量%
を含有してなることを特徴とする液体口腔用組成物。
〔2〕
(B)フッ素イオン源が、フッ化ナトリウム、モノフルオロリン酸ナトリウム及びフッ化スズから選ばれる1種又は2種以上のフッ素含有化合物である〔1〕記載の液体口腔用組成物。
〔3〕
(C)成分が、リン酸二水素一ナトリウム、リン酸一水素二ナトリウム、リン酸二水素一カリウム及びリン酸一水素二カリウムから選ばれる1種又は2種以上のオルトリン酸の水素塩である〔1〕又は〔2〕記載の液体口腔用組成物。
〔4〕
(A)成分の含有量a、(B)成分の含有量bの合計と(C)成分の含有量cとの比率を示す(a+b)/c(但し、bは、(B)フッ素イオンの含有量から換算したフッ化ナトリウム相当量である。)が、質量比として0.35〜40である〔1〕、〔2〕又は〔3〕記載の液体口腔用組成物。
〔5〕
更に、(D)多価アルコール及び/又は糖アルコールを0.1〜20質量%含有してなる〔1〕〜〔4〕のいずれかに記載の液体口腔用組成物。
〔6〕
25℃におけるpHが6.5〜8である〔1〕〜〔5〕のいずれかに記載の液体口腔用組成物。
〔7〕
研磨剤を含まない〔1〕〜〔6〕のいずれかに記載の液体口腔用組成物。
〔8〕
洗口剤である〔1〕〜〔7〕のいずれかに記載の液体口腔用組成物。
Accordingly, the present invention provides the following liquid oral composition.
[1]
(A) 0.1-1% by mass of ascorbic acid phosphate and / or salt thereof,
(B) Fluorine ion 5-4,530 ppm,
(C) Orthophosphoric acid and / or salt thereof 0.01 to 1% by mass
A composition for liquid oral cavity, comprising
[2]
(B) The liquid oral composition according to [1], wherein the fluorine ion source is one or more fluorine-containing compounds selected from sodium fluoride, sodium monofluorophosphate and tin fluoride.
[3]
Component (C) is a hydrogen salt of one or more orthophosphoric acids selected from monosodium dihydrogen phosphate, disodium monohydrogen phosphate, monopotassium dihydrogen phosphate and dipotassium monohydrogen phosphate. [1] or [2] liquid oral composition.
[4]
(A) component content a, (B) component content b and (C) component content c (a + b) / c (where b is (B) fluorine ion The liquid oral composition according to [1], [2] or [3], wherein the mass ratio is 0.35 to 40 in terms of a sodium fluoride equivalent amount converted from the content.
[5]
Furthermore, (D) The composition for liquid oral cavity in any one of [1]-[4] formed by containing 0.1-20 mass% of polyhydric alcohol and / or sugar alcohol.
[6]
Liquid oral cavity composition in any one of [1]-[5] whose pH in 25 degreeC is 6.5-8.
[7]
The liquid oral composition according to any one of [1] to [6], which does not contain an abrasive.
[8]
The liquid oral cavity composition according to any one of [1] to [7], which is a mouthwash.
本発明によれば、優れた実効感(歯ぐきの引き締め感)を有するアスコルビン酸リン酸エステル及び/又はその塩含有の液体口腔用組成物を提供できる。更に、渋味・苦味・異味がなく使用感も良い前記液体口腔用組成物を提供できる。本発明の液体口腔用組成物によって、使用直後においても満足な効果実感があることから使用者の継続的な使用や、それによる歯周疾患の予防・治療効果向上が期待できる。 ADVANTAGE OF THE INVENTION According to this invention, the liquid oral cavity composition containing the ascorbic acid phosphate ester and / or its salt which has the outstanding effective feeling (feeling of tightening gums) can be provided. Furthermore, the liquid oral composition can be provided that has no astringency, bitterness, or off-flavor and is easy to use. Since the liquid oral composition of the present invention has a satisfactory effect immediately after use, it can be expected that the user will continue to use the product and thereby improve the prevention / treatment effect of periodontal diseases.
本発明の液体口腔用組成物は、(A)アスコルビン酸リン酸エステル及び/又はその塩、(B)フッ素イオン、(C)オルトリン酸及び/又はその塩を含有する。本発明では、これら(A)、(B)、(C)成分を組み合わせることによって実効感(歯ぐきの引き締め感)を与えるものであり、いずれかの成分を欠くと歯ぐきの引き締め感を付与することができない。 The composition for liquid oral cavity of the present invention contains (A) ascorbic acid phosphate and / or salt thereof, (B) fluorine ion, (C) orthophosphoric acid and / or salt thereof. In the present invention, these components (A), (B), and (C) are combined to give an effective feeling (a feeling of tightening the gums). I can't.
(A)成分のアスコルビン酸リン酸エステルとしては、アスコルビン酸の2位、3位、5位、6位の水酸基のいずれか1つ又は2つ以上がリン酸エステルになったもの、例えば、L−アスコルビン酸−2−リン酸エステル、L−アスコルビン酸−3−リン酸エステル、L−アスコルビン酸−6−リン酸エステル等が挙げられる。また、それらの塩類としては、ナトリウム塩、カリウム塩、カルシウム塩、マグネシウム塩等が挙げられる。これらアスコルビン酸リン酸エステル及びその塩は、1種を単独で又は2種以上を組み合わせて使用することができる。中でも、実効感付与、更には組成物の安定性の点から、アスコルビン酸の2位又は3位の水酸基がリン酸エステル化された誘導体が好ましく、より好ましくはアスコルビン酸−2−リン酸エステルのマグネシウム塩やナトリウム塩である。
具体的には、和光純薬工業(株)、DSMニュートリションジャパン(株)製のリン酸L−アスコルビルマグネシウム、リン酸L−アスコルビルナトリウム等の市販品を使用し得る。
As (A) component ascorbic acid phosphate, ascorbic acid, one, or two or more of hydroxyl groups at 2nd, 3rd, 5th and 6th positions are converted to phosphates, for example, L -Ascorbic acid-2-phosphate ester, L-ascorbic acid-3-phosphate ester, L-ascorbic acid-6-phosphate ester, etc. are mentioned. In addition, examples of the salts include sodium salts, potassium salts, calcium salts, and magnesium salts. These ascorbic acid phosphates and salts thereof can be used alone or in combination of two or more. Among them, from the viewpoint of imparting an effective feeling and further the stability of the composition, a derivative in which the hydroxyl group at the 2-position or 3-position of ascorbic acid is converted to a phosphate ester is preferable, and more preferable is an ascorbic acid-2-phosphate ester. Magnesium salt and sodium salt.
Specifically, commercially available products such as L-ascorbyl magnesium phosphate and L-ascorbyl sodium phosphate manufactured by Wako Pure Chemical Industries, Ltd. and DSM Nutrition Japan Co., Ltd. can be used.
(A)成分のアスコルビン酸リン酸エステル及び/又はその塩の配合量は、組成物全体の0.1〜1%(質量%、以下同様。)であり、好ましくは0.2〜0.8%である。配合量が0.1%に満たないと実効感(歯ぐきの引き締め感)を付与できない。1%を超えると実効感(歯ぐきの引き締め感)付与効果が低下し、満足な実効感を付与できない。 The blending amount of the component (A) ascorbic acid phosphate and / or salt thereof is 0.1 to 1% (mass%, the same applies hereinafter) of the whole composition, preferably 0.2 to 0.8. %. If the blending amount is less than 0.1%, an effective feeling (feeling of tightening gums) cannot be imparted. If it exceeds 1%, the effect of providing an effective feeling (a feeling of tightening the gums) decreases, and a satisfactory effective feeling cannot be provided.
(B)成分のフッ素イオンは、フッ素イオンを供給するフッ素含有化合物として配合することができる。前記フッ素含有化合物としては、フッ化ナトリウム、モノフルオロリン酸ナトリウム、フッ化スズ等が挙げられ、これらのうちの1種を単独で又は2種以上を混合して用いることができる。特に、実効感(歯ぐきの引き締め感)付与の点から、フッ化ナトリウム、モノフルオロリン酸ナトリウムが好ましく、より好ましくはフッ化ナトリウムである。 (B) The fluorine ion of a component can be mix | blended as a fluorine-containing compound which supplies a fluorine ion. Examples of the fluorine-containing compound include sodium fluoride, sodium monofluorophosphate, tin fluoride, and the like. One of these can be used alone or two or more of them can be used in combination. In particular, sodium fluoride and sodium monofluorophosphate are preferable, and sodium fluoride is more preferable from the viewpoint of imparting an effective feeling (a feeling of tightening gums).
(B)成分のフッ素イオンの組成物中の含有量は、5〜4,530ppm、好ましくは40〜2,300ppmである。含有量が前記範囲内であると、歯ぐきの引き締め感が優れる。
フッ素含有化合物は、前記フッ素イオン含有量の範囲内で配合され、その配合量は、フッ素イオン含有量から換算して求めることができる。例えば、フッ化ナトリウムの場合、その配合量は、換算して求めると組成物全体の0.001〜1%であり、好ましくは0.01〜0.5%である。モノフルオロリン酸ナトリウムの場合、その配合量は組成物全体の0.003〜3.4%、特に0.003〜1.7%が好ましい。
(B) Content in the composition of the fluorine ion of a component is 5-4,530 ppm, Preferably it is 40-2,300 ppm. When the content is within the above range, the feeling of tightening gums is excellent.
A fluorine-containing compound is mix | blended within the range of the said fluorine ion content, The compounding quantity can be calculated | required in conversion from fluorine ion content. For example, in the case of sodium fluoride, the blending amount is 0.001 to 1%, preferably 0.01 to 0.5% of the whole composition when calculated in terms of conversion. In the case of sodium monofluorophosphate, the blending amount is preferably 0.003 to 3.4%, particularly preferably 0.003 to 1.7% of the entire composition.
(C)オルトリン酸及び/又はその塩としては、正リン酸、そのアルカリ金属塩、アンモニウム塩、水素塩等を使用できる。
オルトリン酸塩としては、リン酸ナトリウム、リン酸カリウム、リン酸アンモニウム等の正塩、リン酸二水素一ナトリウム、リン酸一水素二ナトリウム、リン酸二水素一カリウム、リン酸一水素二カリウム等の水素塩が挙げられ、これらの1種を単独で又は2種以上を混合して用いることができる。中でも、実効感(歯ぐきの引き締め感)付与の点から、オルトリン酸の水素塩が好ましく、より好ましくはリン酸二水素一ナトリウム及び/又はリン酸一水素二ナトリウムである。
なお、オルトリン酸及び/又はその塩の代わりに、例えばピロリン酸塩、ポリリン酸塩等のリン酸基を有するキレート剤を用いても実効感(歯ぐきの引き締め感)は付与できず、本発明の目的は達成されない。
(C) As orthophosphoric acid and / or its salt, orthophosphoric acid, its alkali metal salt, ammonium salt, hydrogen salt, etc. can be used.
Orthophosphates include orthophosphates such as sodium phosphate, potassium phosphate, and ammonium phosphate, monosodium dihydrogen phosphate, disodium monohydrogen phosphate, monopotassium dihydrogen phosphate, dipotassium monohydrogen phosphate, etc. These can be used, and one of these can be used alone or two or more of them can be used in combination. Among these, from the viewpoint of imparting an effective feeling (a feeling of tightening of the gums), a hydrogen salt of orthophosphoric acid is preferable, and more preferably, it is monosodium dihydrogen phosphate and / or disodium monohydrogen phosphate.
In addition, even if a chelating agent having a phosphate group such as pyrophosphate or polyphosphate is used instead of orthophosphoric acid and / or a salt thereof, an effective feeling (a feeling of tightening gums) cannot be imparted. The goal is not achieved.
(C)成分のオルトリン酸及び/又はその塩の配合量は、組成物全体の0.01〜1%であり、好ましくは0.03〜0.5%である。配合量が0.01%に満たないと、実効感(歯ぐきの引き締め感)を付与できない。1%を超えると実効感(歯ぐきの引き締め感)付与効果が低下し、満足な実効感を付与できない。 The blending amount of orthophosphoric acid and / or a salt thereof as component (C) is 0.01 to 1%, preferably 0.03 to 0.5% of the entire composition. If the blending amount is less than 0.01%, it is impossible to give an effective feeling (feeling of tightening gums). If it exceeds 1%, the effect of providing an effective feeling (a feeling of tightening the gums) decreases, and a satisfactory effective feeling cannot be provided.
更に、本発明においては、(A)成分の含有量a、(B)成分の含有量bの合計と(C)成分の含有量cとの比率を示す(a+b)/cが、質量比として0.35〜40であることが好ましく、より好ましくは0.5〜40である。前記範囲内であると、実効感(歯ぐきの引き締め感)付与効果がより優れる。ここで、前記bは、(B)フッ素イオンの含有量から換算したフッ化ナトリウム相当量であり、(B)フッ素イオンの含有量(ppm)からフッ化ナトリウム化合物量(%)として換算して求めることができる(以下同様。)。 Furthermore, in the present invention, (a + b) / c indicating the ratio of the sum of the content (a) of the component (A) and the content (b) of the component (B) and the content c of the component (C) is a mass ratio. It is preferable that it is 0.35-40, More preferably, it is 0.5-40. Within the above range, the effect of giving an effective feeling (feeling of tightening gums) is more excellent. Here, the b is equivalent to sodium fluoride converted from the content of (B) fluorine ions, and converted from the content (ppm) of fluorine ions (ppm) as the amount of sodium fluoride compound (%). Can be obtained (the same applies hereinafter).
本発明組成物は、更に、(D)多価アルコール及び/又は糖アルコールを配合すると、使用感(渋味・苦味・異味のなさ)をより改善できる。
(D)多価アルコール、糖アルコールとしては、グリセリン、プロピレングリコール、ソルビトール、キシリトール、マルチトール、ラクチトール、エチレングリコール、ポリエチレングリコールなどが挙げられ、これらから選ばれる1種又は2種以上を使用し得るが、グリセリン、プロピレングリコール、ソルビトールが好ましく、特にグリセリンが、使用感(渋味・苦味・異味のなさ)の改善にはより好適である。
When the composition of the present invention further contains (D) a polyhydric alcohol and / or a sugar alcohol, the feeling of use (astringency, bitterness, tastelessness) can be further improved.
(D) Examples of the polyhydric alcohol and sugar alcohol include glycerin, propylene glycol, sorbitol, xylitol, maltitol, lactitol, ethylene glycol, polyethylene glycol and the like, and one or more selected from these may be used. However, glycerin, propylene glycol, and sorbitol are preferred, and glycerin is particularly suitable for improving the feeling of use (astringency, bitterness, and taste).
(D)成分の多価アルコール及び/又は糖アルコールを配合する場合、その配合量は組成物全体の0.1〜20%が好ましく、0.1〜10%がより好ましく、特に好ましくは0.2〜8%である。配合量が上記範囲内であると、使用感(渋味・苦味・異味のなさ)がより改善する。 (D) When mix | blending the polyhydric alcohol and / or sugar alcohol of a component, 0.1-20% of the whole composition is preferable, 0.1-10% is more preferable, Especially preferably, it is 0.1. 2-8%. When the blending amount is within the above range, the feeling of use (astringency, bitterness, tastelessness) is further improved.
本発明の液体口腔用組成物は、25℃におけるpHが6.5〜8であることが好ましく、より好ましくはpH7.0〜7.9である。本発明においては、pHが上記範囲内であると、使用感(渋味・苦味・異味のなさ)をより良好に保ちつつ実効感(歯ぐきの引き締め感)を付与できる。pHが高くなりすぎると刺激感が発現して使用感が低下したり、歯ぐきの引き締め感を十分かつ適度に付与できなくなる場合がある。
なお、前記pHに調整するため、必要に応じて、pH調整剤を、適宜添加して調整してもよい。pH調整剤としては、口腔用製剤に使用可能なpH調整剤であれば特に制限はなく、フタル酸、酢酸、フマル酸、クエン酸、酒石酸、リンゴ酸、炭酸、重炭酸やそれらのカリウム塩、ナトリウム塩、アンモニウム塩、リボ核酸及びその塩類、水酸化ナトリウム、塩酸等が挙げられる。
The liquid oral composition of the present invention preferably has a pH at 25 ° C. of 6.5 to 8, more preferably 7.0 to 7.9. In the present invention, when the pH is within the above range, it is possible to impart an effective feeling (feeling of tightening gums) while maintaining a better feeling of use (astringency, bitterness, tastelessness). If the pH is too high, a feeling of irritation may be manifested and the feeling of use may be reduced, or a feeling of tightening gums may not be imparted sufficiently and appropriately.
In addition, in order to adjust to the said pH, you may adjust by adding a pH adjuster suitably as needed. The pH adjuster is not particularly limited as long as it is a pH adjuster that can be used for oral preparations, such as phthalic acid, acetic acid, fumaric acid, citric acid, tartaric acid, malic acid, carbonic acid, bicarbonate, and potassium salts thereof, Examples include sodium salts, ammonium salts, ribonucleic acid and salts thereof, sodium hydroxide, hydrochloric acid and the like.
本発明の液体口腔用組成物は、洗口剤、口中清涼剤、濃縮タイプ洗口剤等の剤型、特に洗口剤として好適に調製、適用することができる。組成物を口中に含みそのまま漱ぐ洗口剤とすることが、効果発現の点でより好適である。この場合、上記成分に加えて、剤型に応じ、その他の公知成分を必要に応じて配合できる。例えば、液体媒体(溶剤)、増粘剤、界面活性剤、更に必要により、防腐剤、甘味剤、着色料、香料、有効成分等を、本発明の効果を妨げない範囲で配合できる。
なお、本発明の液体口腔用組成物は、配合成分が液体媒体に溶解、可溶化、もしくは乳化された製剤であり、研磨剤やパール化剤などの不溶性の固形成分の配合量は1%以下とすることが好ましく、配合されないことがより好ましい。
The liquid oral cavity composition of the present invention can be suitably prepared and applied as a dosage form such as a mouthwash, a mouth freshener, a concentrated mouthwash, and particularly as a mouthwash. A mouthwash containing the composition in the mouth and rinsing as it is is more preferable from the standpoint of effect. In this case, in addition to the above components, other known components can be blended as necessary according to the dosage form. For example, a liquid medium (solvent), a thickener, a surfactant, and, if necessary, preservatives, sweeteners, coloring agents, fragrances, active ingredients, and the like can be blended within a range that does not hinder the effects of the present invention.
The liquid oral composition of the present invention is a preparation in which the compounding components are dissolved, solubilized or emulsified in a liquid medium, and the compounding amount of insoluble solid components such as abrasives and pearlizing agents is 1% or less. It is preferable that it is not blended.
液体媒体には、通常、精製水が用いられる。精製水に加えてエタノール等の炭素数2〜4の低級一価アルコールを添加することもできるが、組成物全体に対して20%以下(0〜20%)とすることが好ましく、15%以下(0〜15%)とすることがより好ましく、5%以下(0〜5%)とすることが特に好ましい。前記低級アルコールを実質的に含有しない(含有量100ppm以下)アルコールフリーの製剤は、アルコールの刺激がないため極めて好ましい。 For the liquid medium, purified water is usually used. In addition to purified water, a lower monohydric alcohol having 2 to 4 carbon atoms such as ethanol can be added, but it is preferably 20% or less (0 to 20%), preferably 15% or less, based on the entire composition. (0 to 15%) is more preferable, and 5% or less (0 to 5%) is particularly preferable. Alcohol-free preparations that substantially do not contain the lower alcohol (content of 100 ppm or less) are extremely preferable because they do not stimulate alcohol.
増粘剤としては、キサンタンガム、カラギーナン、カルボキシメチルセルロースナトリウム、ヒドロキシエチルセルロース、アルギン酸ナトリウム、ポリビニルアルコール等が挙げられる。増粘剤の配合量は、通常、0〜1%、特に0.1〜1%である。 Examples of the thickener include xanthan gum, carrageenan, sodium carboxymethyl cellulose, hydroxyethyl cellulose, sodium alginate, polyvinyl alcohol and the like. The blending amount of the thickener is usually 0 to 1%, particularly 0.1 to 1%.
界面活性剤としては、公知のアニオン性界面活性剤、両性界面活性剤、非イオン性界面活性剤を使用し得る。具体的には、ラウリル硫酸ナトリウム等のアルキル硫酸エステル塩、ラウロイルサルコシンナトリウム、ラウロイルメチルタウリン等のアシルアミノ酸塩、ドデシルベンゼンスルホン酸ナトリウム、α−スルホ脂肪酸アルキルエステル・ナトリウム、アルキルリン酸エステル塩などのアニオン性界面活性剤;アルキルジメチルアミノ酢酸ベタイン、脂肪酸アミドプロピルジメチルアミノ酢酸ベタイン等の酢酸ベタイン型両性界面活性剤、N−脂肪酸アシル−N−カルボキシメチル−N−ヒドロキシエチルエチレンジアミン塩等のイミダゾリン型両性界面活性剤、N−脂肪酸アシル−L−アルギネート塩等のアミノ酸型両性界面活性剤;ポリグリセリン脂肪酸エステル、糖脂肪酸エステル、ソルビタン脂肪酸エステル、ポリオキシエチレンポリオキシプロピレンブロックコポリマー、ポリオキシエチレン脂肪酸エステル、脂肪酸モノグリセライド、ポリオキシエチレンアルキルエーテルなどの非イオン性界面活性剤が挙げられる。
界面活性剤の配合量は、通常、0〜10%、特に0.1〜5%である。
As the surfactant, a known anionic surfactant, amphoteric surfactant, or nonionic surfactant can be used. Specifically, alkyl sulfate salts such as sodium lauryl sulfate, acylamino acid salts such as sodium lauroyl sarcosine, lauroyl methyl taurine, sodium dodecylbenzenesulfonate, α-sulfo fatty acid alkyl ester / sodium, alkyl phosphate ester salts, etc. Anionic surfactants; betaine acetate type amphoteric surfactants such as alkyldimethylaminoacetic acid betaine and fatty acid amidopropyldimethylaminoacetic acid betaine; imidazoline type amphoteric such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salt Surfactant, amino acid type amphoteric surfactant such as N-fatty acid acyl-L-alginate salt; polyglycerin fatty acid ester, sugar fatty acid ester, sorbitan fatty acid ester, polyoxyethylene poly Carboxymethyl propylene block copolymer, polyoxyethylene fatty acid esters, fatty acid monoglyceride, non-ionic surfactants such as polyoxyethylene alkyl ether.
The compounding amount of the surfactant is usually 0 to 10%, particularly 0.1 to 5%.
防腐剤としては、メチルパラベン、エチルパラベン、プロピルパラベン、ブチルパラベン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、塩酸アルキルジアミノエチルグリシン、ソルビン酸カリウム等が挙げられる。
甘味剤としては、サッカリンナトリウム、ステビオサイト、スクラロース等が挙げられる。
着色料としては、青色1号、緑色3号、黄色4号、赤色105号など安全性の高い水溶性色素が挙げられる。
Examples of the preservative include paraoxybenzoic acid esters such as methylparaben, ethylparaben, propylparaben, and butylparaben, benzoic acid such as sodium benzoate or salts thereof, alkyldiaminoethylglycine hydrochloride, potassium sorbate, and the like.
Examples of the sweetening agent include saccharin sodium, steviosite, sucralose and the like.
Examples of the coloring agent include highly safe water-soluble pigments such as Blue No. 1, Green No. 3, Yellow No. 4, and Red No. 105.
香料としては、ペパーミント油、スペアミント油、ユーカリ油、ウィンターグリーン油、クローブ油、タイム油、セージ油、カルダモン油、ローズマリー油、マジョラム油、レモン油、ナツメグ油、ラベンダー油、パラクレス油等の天然精油、及び、l−カルボン、1,8−シネオール、メチルサリシレート、オイゲノール、チモール、リナロール、リモネン、メントン、メンチルアセテート、シトラール、カンファー、ボルネオール、ピネン、スピラントール等の上記天然精油中に含まれる香料成分、また、エチルアセテート、エチルブチレート、イソアミルアセテート、ヘキサナール、ヘキセナール、メチルアンスラニレート、エチルメチルフェニルグリシデート、ベンツアルデヒド、バニリン、エチルバニリン、フラネオール、マルトール、エチルマルトール、ガンマ/デルタデカラクトン、ガンマ/デルタウンデカラクトン、N−エチル−p−メンタン−3−カルボキサミド、メンチルラクテート、エチレングリコール−l−メンチルカーボネート等の香料成分、更には、いくつかの香料成分や天然精油を組み合わせてなるアップル、バナナ、ストロベリー、ブルーベリー、メロン、ピーチ、パイナップル、グレープ、マスカット、ワイン、チェリー、スカッシュ、コーヒー、ブランデー、ヨーグルト等の調合フレーバーが挙げられる。
配合量は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く、また、上記香料素材を使用した賦香用香料は、組成物中に0.1〜2%使用するのが好ましい。
Natural flavors such as peppermint oil, spearmint oil, eucalyptus oil, wintergreen oil, clove oil, thyme oil, sage oil, cardamom oil, rosemary oil, marjoram oil, lemon oil, nutmeg oil, lavender oil, paracres oil, etc. Essential oils and perfume ingredients contained in the above natural essential oils such as l-carvone, 1,8-cineol, methyl salicylate, eugenol, thymol, linalool, limonene, menthone, menthyl acetate, citral, camphor, borneol, pinene, spirantol Also, ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methyl phenyl glycidate, benzaldehyde, vanillin, ethyl vanillin, furaneol, malto , Perfume ingredients such as ethyl maltol, gamma / delta decalactone, gamma / deltown decalactone, N-ethyl-p-menthane-3-carboxamide, menthyl lactate, ethylene glycol-l-menthyl carbonate, Flavors such as apple, banana, strawberry, blueberry, melon, peach, pineapple, grape, muscat, wine, cherry, squash, coffee, brandy, yogurt and the like.
The blending amount is not particularly limited, but the above fragrance material is preferably used in the composition in an amount of 0.000001 to 1%, and the fragrance for fragrance using the above fragrance material is 0.00% in the composition. It is preferable to use 1 to 2%.
有効成分としては、本発明の効果を妨げない範囲で、公知の薬効成分を添加し得る。例えば、イソプロピルメチルフェノール、トリクロサン等の殺菌剤、トラネキサム酸、イプシロン−アミノカプロン酸等の抗炎症剤、デキストラナーゼ、アミラーゼ、プロテアーゼ、ムタナーゼ、リゾチーム、溶菌酵素、リテックエンザイム等の酵素、アルミニウムクロルヒドロキシアラントイン、アラントイン、アズレン、塩化リゾチーム、アスコルビン酸、ジヒドロコレステロール、グリチルレチン塩類、グリチルレチン酸類、ヒドロコレステロール、クロロフィル、銅クロロフィリンナトリウム、タイム、オウゴン、チョウジ、ハマメリス等の植物抽出物、グルコン酸銅、カロペプタイド、ポリリン酸ナトリウム、ポリビニルピロリドン、硝酸カリウム、乳酸アルミニウム等が挙げられる。 As an active ingredient, a well-known medicinal ingredient can be added in the range which does not prevent the effect of this invention. For example, bactericides such as isopropylmethylphenol and triclosan, anti-inflammatory agents such as tranexamic acid and epsilon-aminocaproic acid, enzymes such as dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme, lytechenzyme, aluminum chlorohydroxy allantoin , Plant extracts such as allantoin, azulene, lysozyme chloride, ascorbic acid, dihydrocholesterol, glycyrrhetin salts, glycyrrhetinic acid, hydrocholesterol, chlorophyll, copper chlorophyllin sodium, thyme, ogon, clove, hamamelis, copper gluconate, caropeptide, polyphosphoric acid Sodium, polyvinylpyrrolidone, potassium nitrate, aluminum lactate and the like can be mentioned.
本発明の液体口腔用組成物の粘度は、25℃における粘度(B型粘度計での測定値)が好ましくは1〜100mPa・sである。
また、液体口腔用組成物を充填する容器の材質には、PET(ポリエチレンテレフタレート)、ガラス、ポリプロピレン、ポリエチレン等が使用できる。
The viscosity of the composition for liquid oral cavity of the present invention is preferably 1 to 100 mPa · s at 25 ° C. (measured value with a B-type viscometer).
Moreover, PET (polyethylene terephthalate), glass, polypropylene, polyethylene, etc. can be used for the material of the container filled with the liquid oral 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。なお、pH、粘度は25℃における値であり、粘度は下記方法で測定した。 EXAMPLES Hereinafter, although an Example, a comparative example, a formulation example is shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example. In the following examples, “%” means “% by mass” unless otherwise specified. In addition, pH and a viscosity are the values in 25 degreeC, and the viscosity was measured with the following method.
[実施例、比較例]
(1)実験1
表1〜3に示す組成の液体口腔用組成物(洗口剤)を下記方法で調製し、下記方法に従って実効感(歯ぐきの引き締め感)を評価した。結果を表に併記した。
なお、(B)成分は、表に示すフッ素含有化合物として配合し、フッ素イオンの含有量はフッ素イオン濃度(ppm)として( )内に示した。また、(a+b)/cは、(A)成分の含有量a、(B)成分の含有量bの合計と(C)成分の含有量cとの質量比率(但し、bは、(B)フッ素イオンの含有量から換算したフッ化ナトリウム相当量である。)である(以下同様。)。
[Examples and Comparative Examples]
(1) Experiment 1
Liquid oral compositions (mouth washes) having the compositions shown in Tables 1 to 3 were prepared by the following method, and the effectiveness (gum tightness) was evaluated according to the following method. The results are shown in the table.
In addition, (B) component was mix | blended as a fluorine-containing compound shown in a table | surface, and content of a fluorine ion was shown in () as a fluorine ion concentration (ppm). In addition, (a + b) / c is the mass ratio of the content (a) of the component (A), the sum of the content (b) of the component (B) and the content c of the component (C) (where b is (B) It is equivalent to sodium fluoride converted from the content of fluorine ions.
液体口腔用組成物の調製方法;
精製水850gにアスコルビン酸リン酸エステル類及びそれ以外の成分を常温で混合し、アスコルビン酸リン酸エステル類が完全に溶解するまで1時間攪拌した。必要に応じて水酸化ナトリウム、塩酸等を添加してpHを調整した後、組成物の総量が1,000gとなるように精製水を添加して調製した。なお、水酸化ナトリウム及び塩酸は10%水溶液を調製したものを使用した。
A method for preparing a liquid oral composition;
Ascorbic acid phosphates and other components were mixed with 850 g of purified water at room temperature and stirred for 1 hour until the ascorbic acid phosphates were completely dissolved. After adjusting the pH by adding sodium hydroxide, hydrochloric acid or the like as necessary, purified water was added so that the total amount of the composition was 1,000 g. In addition, sodium hydroxide and hydrochloric acid used what prepared 10% aqueous solution.
実効感(歯ぐきの引き締め感)の評価方法;
サンプル(液体口腔用組成物)約10mlを口に含み、30秒間漱いだ後、洗口後の実効感(歯ぐきの引き締め感)について、下記の4段階の評点基準で官能評価した。10名の評価結果の平均値を求め、以下の判定基準で評価した。○以上を合格とした。
実効感(歯ぐきの引き締め感)の評点基準:
4点:歯ぐきの引き締め感があった。
3点:歯ぐきの引き締め感がわずかにあった。
2点:歯ぐきの引き締め感がほとんどなかった。
1点:歯ぐきの引き締め感がなかった。
実効感(歯ぐきの引き締め感)の判定基準:
◎:平均点3.5点以上4.0点以下
○:平均点3.0点以上3.5点未満
△:平均点2.0点以上3.0点未満
×:平均点2.0点未満
Evaluation method of effectiveness (feeling of tightening gums);
About 10 ml of a sample (composition for liquid oral cavity) was included in the mouth, and after squeezing for 30 seconds, the sensory evaluation of the effective feeling (feeling of tightening the gums) after mouthwashing was carried out based on the following four grades. An average value of the evaluation results of 10 people was obtained and evaluated according to the following criteria. ○ The above was accepted.
Evaluation criteria (feeling of tightening the gums):
4 points: There was a feeling of tightening the gums.
3 points: There was a slight feeling of tightening the gums.
2 points: There was almost no feeling of tightening the gums.
1 point: There was no feeling of tightening the gums.
Criteria for effectiveness (feeling of tightening gums):
◎: Average point 3.5 points or more and 4.0 points or less ○: Average point 3.0 points or more and less than 3.5 points △: Average point 2.0 points or more and less than 3.0 points ×: Average point 2.0 points Less than
粘度測定法;
B型粘度計(ローターNo.1、60rpm、25℃、1分後の測定値)で測定した。
Viscosity measurement method;
It was measured with a B-type viscometer (rotor No. 1, 60 rpm, 25 ° C., measured value after 1 minute).
(2)実験2
表4に示す組成の液体口腔用組成物(洗口剤)を上記と同様に調製し実効感(歯ぐきの引き締め感)を評価し、更に、下記方法に従って使用感を評価した。結果を表に併記した。
(2) Experiment 2
A liquid oral composition (mouthwash) having the composition shown in Table 4 was prepared in the same manner as described above, and the feeling of effectiveness (feeling of tightening gums) was evaluated. Further, the feeling of use was evaluated according to the following method. The results are shown in the table.
使用感(渋味・苦味・異味のなさ)の評価方法;
サンプル(液体口腔用組成物)約10mlを口に含み、30秒間漱いだ後、洗口後の使用感(渋味・苦味・異味のなさ)について、下記の4段階の評点基準で官能評価した。10名の評価結果の平均値を求め、以下の判定基準で評価した。○以上を合格とした。
使用感の評点基準
4点:渋味・苦味・異味がまったくない。
3点:渋味・苦味・異味がわずかにある。
2点:渋味・苦味・異味がややある。
1点:渋味・苦味・異味がかなりある。
使用感の判定基準
◎:平均点3.5点以上4.0点以下
○:平均点3.0点以上3.5点未満
△:平均点2.0点以上3.0点未満
×:平均点2.0点未満
Evaluation method of feeling of use (astringency, bitterness, tastelessness);
About 10 ml of sample (composition for liquid oral cavity) is put in the mouth, and after squeezing for 30 seconds, the feeling after use (astringency, bitterness, tastelessness) is organoleptically evaluated based on the following four grades. did. An average value of the evaluation results of 10 people was obtained and evaluated according to the following criteria. ○ The above was accepted.
Usability rating criteria 4 points: No astringency, bitterness, or off-flavor.
3 points: There are slight astringency, bitterness and off-flavor.
2 points: There is a bit of astringency, bitterness, and taste.
1 point: Astringency, bitterness, and off-taste are considerable.
Judgment criteria for feeling of use ◎: Average point 3.5 points or more and 4.0 points or less ○: Average point 3.0 points or more and less than 3.5 points △: Average point 2.0 points or more and less than 3.0 points ×: Average Less than 2.0 points
使用原料の詳細を下記に示す。
(A)リン酸L−アスコルビルマグネシウム:和光純薬工業(株)製、生化学用
(A)リン酸L−アスコルビルナトリウム:
DSMニュートリションジャパン(株)製、ステイC5
(B)フッ化ナトリウム:ステラケミファ(株)製、フッ化ナトリウム
(B)モノフルオロリン酸ナトリウム:ローディア日華(株)製
(C)リン酸二水素一ナトリウム:太平化学産業(株)製、リン酸二水素ナトリウム
(C)リン酸一水素二ナトリウム:太平化学産業(株)製、リン酸一水素ナトリウム
トリポリリン酸ナトリウム(比較品):太平化学産業(株)製、ポリリン酸ナトリウム
(D)グリセリン:阪本薬品工業(株)製
(D)ソルビトール:和光純薬工業(株)製
(D)プロピレングリコール:旭硝子(株)製
Details of the raw materials used are shown below.
(A) L-ascorbyl magnesium phosphate: manufactured by Wako Pure Chemical Industries, Ltd., for biochemistry (A) L-ascorbyl phosphate sodium:
DSM Nutrition Japan Co., Ltd., Stay C5
(B) Sodium fluoride: manufactured by Stella Chemifa Corporation, sodium fluoride (B) sodium monofluorophosphate: manufactured by Rhodia Nikka Co., Ltd. (C) monosodium dihydrogen phosphate: manufactured by Taihei Chemical Industrial Co., Ltd. Sodium dihydrogen phosphate (C) Disodium monohydrogen phosphate: manufactured by Taihei Chemical Industry Co., Ltd. Sodium monohydrogen phosphate, sodium tripolyphosphate (comparative product): manufactured by Taihei Chemical Industrial Co., Ltd., sodium polyphosphate (D ) Glycerin: Sakamoto Pharmaceutical Co., Ltd. (D) Sorbitol: Wako Pure Chemical Industries, Ltd. (D) Propylene glycol: Asahi Glass Co., Ltd.
以下に処方例を示す。 A prescription example is shown below.
[処方例1]洗口剤
(A)リン酸L−アスコルビルマグネシウム 0.3%
(B)フッ化ナトリウム 0.05
(フッ素イオン濃度 226ppm)
(C)リン酸二水素一ナトリウム 0.1
(D)グリセリン 4
ポリオキシエチレン硬化ヒマシ油(60) 0.5
クエン酸 0.07
クエン酸ナトリウム 0.25
水酸化ナトリウム 0.08
香料 0.2
精製水 バランス
合計 100.0%
(a+b)/c=3.5、pH(25℃);7.5
[Formulation Example 1] Mouthwash (A) L-ascorbyl magnesium phosphate 0.3%
(B) Sodium fluoride 0.05
(Fluorine ion concentration 226ppm)
(C) Monosodium dihydrogen phosphate 0.1
(D) Glycerin 4
Polyoxyethylene hydrogenated castor oil (60) 0.5
Citric acid 0.07
Sodium citrate 0.25
Sodium hydroxide 0.08
Fragrance 0.2
Purified water balance <br/> Total 100.0%
(A + b) /c=3.5, pH (25 ° C.); 7.5
[処方例2]洗口剤
(A)リン酸L−アスコルビルマグネシウム 0.3%
(B)フッ化ナトリウム 0.02
(フッ素イオン濃度 90ppm)
(C)リン酸二水素一ナトリウム 0.1
(D)グリセリン 4
ポリオキシエチレン硬化ヒマシ油(60) 0.5
クエン酸 0.07
クエン酸ナトリウム 0.25
水酸化ナトリウム 0.08
香料 0.2
精製水 バランス
合計 100.0%
(a+b)/c=3.2、pH(25℃);7.5
[Prescription Example 2] Mouthwash (A) L-ascorbyl magnesium phosphate 0.3%
(B) Sodium fluoride 0.02
(Fluorine ion concentration 90ppm)
(C) Monosodium dihydrogen phosphate 0.1
(D) Glycerin 4
Polyoxyethylene hydrogenated castor oil (60) 0.5
Citric acid 0.07
Sodium citrate 0.25
Sodium hydroxide 0.08
Fragrance 0.2
Purified water balance <br/> Total 100.0%
(A + b) /c=3.2, pH (25 ° C.); 7.5
[処方例3]洗口剤
(A)リン酸L−アスコルビルマグネシウム 0.3%
(B)モノフルオロリン酸ナトリウム 0.05
(フッ素イオン濃度 66ppm)
(C)リン酸二水素一ナトリウム 0.1
(D)グリセリン 4
ポリオキシエチレン硬化ヒマシ油(60) 0.5
クエン酸 0.07
クエン酸ナトリウム 0.25
水酸化ナトリウム 0.08
香料 0.2
精製水 バランス
合計 100.0%
b=0.015%、(a+b)/c=3.15、pH(25℃);7.5
[Formulation Example 3] Mouthwash (A) L-ascorbyl magnesium phosphate 0.3%
(B) Sodium monofluorophosphate 0.05
(Fluorine ion concentration 66ppm)
(C) Monosodium dihydrogen phosphate 0.1
(D) Glycerin 4
Polyoxyethylene hydrogenated castor oil (60) 0.5
Citric acid 0.07
Sodium citrate 0.25
Sodium hydroxide 0.08
Fragrance 0.2
Purified water balance <br/> Total 100.0%
b = 0.015%, (a + b) /c=3.15, pH (25 ° C.); 7.5
Claims (8)
(B)フッ素イオン 5〜4,530ppm、
(C)オルトリン酸及び/又はその塩 0.01〜1質量%
を含有してなることを特徴とする液体口腔用組成物。 (A) 0.1-1% by mass of ascorbic acid phosphate and / or salt thereof,
(B) Fluorine ion 5-4,530 ppm,
(C) Orthophosphoric acid and / or salt thereof 0.01 to 1% by mass
A composition for liquid oral cavity, comprising
Priority Applications (2)
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JP2015127630A JP2017007997A (en) | 2015-06-25 | 2015-06-25 | Liquid composition for oral cavity |
PCT/JP2016/068522 WO2016208624A1 (en) | 2015-06-25 | 2016-06-22 | Liquid composition for oral cavity |
Applications Claiming Priority (1)
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JP2015127630A JP2017007997A (en) | 2015-06-25 | 2015-06-25 | Liquid composition for oral cavity |
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JP (1) | JP2017007997A (en) |
WO (1) | WO2016208624A1 (en) |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2004026658A (en) * | 2002-06-21 | 2004-01-29 | Lion Corp | Composition for oral cavity |
JP4892957B2 (en) * | 2004-12-27 | 2012-03-07 | ライオン株式会社 | Liquid oral composition |
JP5644591B2 (en) * | 2011-03-03 | 2014-12-24 | ライオン株式会社 | Oral composition and inhibitor of active oxygen injury of gingival fibroblasts |
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2015
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