JP2020094029A - Oral composition - Google Patents
Oral composition Download PDFInfo
- Publication number
- JP2020094029A JP2020094029A JP2019117446A JP2019117446A JP2020094029A JP 2020094029 A JP2020094029 A JP 2020094029A JP 2019117446 A JP2019117446 A JP 2019117446A JP 2019117446 A JP2019117446 A JP 2019117446A JP 2020094029 A JP2020094029 A JP 2020094029A
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- JP
- Japan
- Prior art keywords
- mass
- composition
- oral
- acid
- oral composition
- 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.)
- Pending
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- 239000000203 mixture Substances 0.000 title claims abstract description 109
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 39
- 239000000194 fatty acid Substances 0.000 claims abstract description 39
- 229930195729 fatty acid Natural products 0.000 claims abstract description 39
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- 229920001353 Dextrin Polymers 0.000 claims abstract description 34
- 235000019425 dextrin Nutrition 0.000 claims abstract description 34
- 150000001875 compounds Chemical class 0.000 claims abstract description 33
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- 150000004665 fatty acids Chemical class 0.000 claims abstract description 24
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 19
- 238000000034 method Methods 0.000 claims abstract description 18
- 230000002708 enhancing effect Effects 0.000 claims abstract description 11
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- 229930195733 hydrocarbon Natural products 0.000 claims description 10
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- AFCARXCZXQIEQB-UHFFFAOYSA-N N-[3-oxo-3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)propyl]-2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidine-5-carboxamide Chemical compound O=C(CCNC(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F)N1CC2=C(CC1)NN=N2 AFCARXCZXQIEQB-UHFFFAOYSA-N 0.000 description 5
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- 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 5
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound 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 4
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- FUWUEFKEXZQKKA-UHFFFAOYSA-N beta-thujaplicin Chemical compound CC(C)C=1C=CC=C(O)C(=O)C=1 FUWUEFKEXZQKKA-UHFFFAOYSA-N 0.000 description 4
- 229910000389 calcium phosphate Inorganic materials 0.000 description 4
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- BIVBRWYINDPWKA-VLQRKCJKSA-L Glycyrrhizinate dipotassium Chemical compound [K+].[K+].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@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C([O-])=O)[C@@H]1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O BIVBRWYINDPWKA-VLQRKCJKSA-L 0.000 description 3
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- 239000001570 sorbitan monopalmitate Substances 0.000 description 1
- 229940031953 sorbitan monopalmitate Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
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- 230000007480 spreading Effects 0.000 description 1
- 238000003892 spreading Methods 0.000 description 1
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- 239000008117 stearic acid Substances 0.000 description 1
- 229940012831 stearyl alcohol Drugs 0.000 description 1
- 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 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 229940013618 stevioside Drugs 0.000 description 1
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- 235000019202 steviosides Nutrition 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 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
- 235000019408 sucralose Nutrition 0.000 description 1
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 229920003002 synthetic resin Polymers 0.000 description 1
- 239000000057 synthetic resin Substances 0.000 description 1
- 229940104261 taurate Drugs 0.000 description 1
- 229960003080 taurine Drugs 0.000 description 1
- TUNFSRHWOTWDNC-HKGQFRNVSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCC[14C](O)=O TUNFSRHWOTWDNC-HKGQFRNVSA-N 0.000 description 1
- 235000019818 tetrasodium diphosphate Nutrition 0.000 description 1
- 239000001577 tetrasodium phosphonato phosphate Substances 0.000 description 1
- 239000000892 thaumatin Substances 0.000 description 1
- 235000010436 thaumatin Nutrition 0.000 description 1
- 230000008719 thickening Effects 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- YUOWTJMRMWQJDA-UHFFFAOYSA-J tin(iv) fluoride Chemical compound [F-].[F-].[F-].[F-].[Sn+4] YUOWTJMRMWQJDA-UHFFFAOYSA-J 0.000 description 1
- 229960000984 tocofersolan Drugs 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 239000000606 toothpaste Substances 0.000 description 1
- 229940034610 toothpaste Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 229940074410 trehalose Drugs 0.000 description 1
- 125000005270 trialkylamine group Chemical group 0.000 description 1
- 229940078499 tricalcium phosphate Drugs 0.000 description 1
- 229910000391 tricalcium phosphate Inorganic materials 0.000 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- VXYADVIJALMOEQ-UHFFFAOYSA-K tris(lactato)aluminium Chemical compound CC(O)C(=O)O[Al](OC(=O)C(C)O)OC(=O)C(C)O VXYADVIJALMOEQ-UHFFFAOYSA-K 0.000 description 1
- UKFUWZNDLZTKGK-UHFFFAOYSA-L trisodium carboxylato carbonate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)OC([O-])=O UKFUWZNDLZTKGK-UHFFFAOYSA-L 0.000 description 1
- WCTAGTRAWPDFQO-UHFFFAOYSA-K trisodium;hydrogen carbonate;carbonate Chemical compound [Na+].[Na+].[Na+].OC([O-])=O.[O-]C([O-])=O WCTAGTRAWPDFQO-UHFFFAOYSA-K 0.000 description 1
- WGIWBXUNRXCYRA-UHFFFAOYSA-H trizinc;2-hydroxypropane-1,2,3-tricarboxylate Chemical compound [Zn+2].[Zn+2].[Zn+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O WGIWBXUNRXCYRA-UHFFFAOYSA-H 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000010457 zeolite Substances 0.000 description 1
- 239000011592 zinc chloride Substances 0.000 description 1
- 235000005074 zinc chloride Nutrition 0.000 description 1
- 239000011746 zinc citrate Substances 0.000 description 1
- 235000006076 zinc citrate Nutrition 0.000 description 1
- 229940068475 zinc citrate Drugs 0.000 description 1
- 239000011787 zinc oxide Substances 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
- 239000004711 α-olefin Substances 0.000 description 1
- 239000002076 α-tocopherol Substances 0.000 description 1
- 235000004835 α-tocopherol Nutrition 0.000 description 1
- FYGDTMLNYKFZSV-BYLHFPJWSA-N β-1,4-galactotrioside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@H](CO)O[C@@H](O[C@@H]2[C@@H](O[C@@H](O)[C@H](O)[C@H]2O)CO)[C@H](O)[C@H]1O FYGDTMLNYKFZSV-BYLHFPJWSA-N 0.000 description 1
- 239000011590 β-tocopherol Substances 0.000 description 1
- 235000007680 β-tocopherol Nutrition 0.000 description 1
- 239000002478 γ-tocopherol Substances 0.000 description 1
- QUEDXNHFTDJVIY-DQCZWYHMSA-N γ-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1 QUEDXNHFTDJVIY-DQCZWYHMSA-N 0.000 description 1
- 239000002446 δ-tocopherol Substances 0.000 description 1
Abstract
Description
本発明は、口腔用組成物に関する。 The present invention relates to an oral composition.
歯周炎(歯槽膿漏)や歯茎炎等、歯周病の予防や治療に用いるための、抗炎症剤や殺菌剤などの有効成分を配合した歯磨剤やゲル剤等の口腔用組成物が知られている。特許文献1には、水溶性のピリジニウム化合物、第四級アンモニウム化合物又はビグアニド系殺菌剤、特定の分子量とカチオン化度を有するカチオン化ヒドロキシエチルセルロース、特定の界面活性剤及び、特定量の非シリカ系研磨剤を含有する練歯磨組成物が開示されている。 Oral compositions such as dentifrices and gels containing active ingredients such as anti-inflammatory agents and bactericides for use in the prevention and treatment of periodontal diseases such as periodontitis (alveolar pyorrhea) and gum inflammation Are known. Patent Document 1 discloses a water-soluble pyridinium compound, a quaternary ammonium compound or a biguanide fungicide, a cationized hydroxyethyl cellulose having a specific molecular weight and a cationization degree, a specific surfactant, and a specific amount of a non-silica type. A toothpaste composition containing an abrasive is disclosed.
本発明は、上述のような状況の中、歯茎又は口腔粘膜に対する密着性に優れる口腔用組成物を提供することを目的とする。 An object of the present invention is to provide an oral composition having excellent adhesion to gums or oral mucosa in the above-mentioned situation.
本発明者らは、鋭意検討した結果、(A)脂肪酸デキストリン、(B)高分子化合物及び/又は研磨剤、並びに、(C)水を含有することによって、歯茎表面への高い密着性を有する口腔用組成物を調製できることを見出し、本発明に至った。 As a result of intensive studies, the present inventors have high adhesion to the gum surface by containing (A) fatty acid dextrin, (B) polymer compound and/or abrasive, and (C) water. The inventors have found that a composition for oral cavity can be prepared, and have completed the present invention.
すなわち、本発明は、以下の口腔用組成物を提供する。
項1.
(A)脂肪酸デキストリン、(B)高分子化合物及び/又は研磨剤、並びに、(C)水、を含有する、口腔用組成物。
項2.
(B)高分子化合物及び/又は研磨剤が、直鎖状高分子化合物である、項1に記載の口腔用組成物。
項3.
(B)高分子化合物及び/又は研磨剤が、カルボキシビニルポリマー、アルギン酸又はその塩、プルラン、及びセルロース系高分子からなる群より選択される少なくとも1種以上である、項1又は2に記載の口腔用組成物。
項4.
(A)成分の総含有量1質量部に対する(B)成分の総含有量が、0.01〜500質量部である、項1〜3のいずれか一項に記載の口腔用組成物。
項5.
(C)水を、30質量%以上含有する、項1〜4のいずれか一項に記載の口腔用組成物。
項6.
(A)脂肪酸デキストリンが、パルミチン酸デキストリンである、項1〜5のいずれか一項に記載の口腔用組成物。
項7.
さらに、殺菌剤、組織修復剤、抗炎症剤、及び血行促進剤からなる群より選択される少なくとも一種を含有する、項1〜6のいずれか一項に記載の口腔用組成物。
項8.
さらに、高級アルコールを含有する、項1〜7のいずれか一項に記載の口腔用組成物。
項9.
さらに、界面活性剤を含有する、項1〜8のいずれか一項に記載の口腔用組成物。
項10.
さらに、炭化水素を含有する、項1〜9のいずれか一項に記載の口腔用組成物。
項11.
歯磨剤、塗布剤、又は含嗽剤である、項1〜10のいずれか一項に記載の口腔用組成物。
That is, the present invention provides the following oral compositions.
Item 1.
An oral composition containing (A) a fatty acid dextrin, (B) a polymer compound and/or an abrasive, and (C) water.
Item 2.
Item 2. The oral composition according to Item 1, wherein the polymer compound and/or the polishing agent (B) is a linear polymer compound.
Item 3.
Item (1) or (2), in which the polymer compound (B) and/or the abrasive is at least one selected from the group consisting of carboxyvinyl polymer, alginic acid or a salt thereof, pullulan, and a cellulosic polymer. Oral composition.
Item 4.
Item 4. The oral composition according to any one of Items 1 to 3, wherein the total content of the component (B) is 0.01 to 500 parts by mass relative to the total content of the component (A) of 1 part by mass.
Item 5.
(C) The oral cavity composition according to any one of Items 1 to 4, which contains 30% by mass or more of water.
Item 6.
(A) The composition for oral cavity according to any one of Items 1 to 5, wherein the fatty acid dextrin is dextrin palmitate.
Item 7.
Item 7. The oral composition according to any one of Items 1 to 6, further containing at least one selected from the group consisting of a bactericide, a tissue repair agent, an anti-inflammatory agent, and a blood circulation promoter.
Item 8.
Further, the oral composition according to any one of Items 1 to 7, which contains a higher alcohol.
Item 9.
Furthermore, the composition for oral cavity of any one of claim|item 1-8 containing a surfactant.
Item 10.
Further, the oral composition according to any one of Items 1 to 9, which contains a hydrocarbon.
Item 11.
Item 11. The oral composition according to any one of Items 1 to 10, which is a dentifrice, a coating agent, or a mouthwash.
さらに、本発明は、以下の方法を提供する。
項12.
(A)脂肪酸デキストリン、(B)高分子化合物及び/又は研磨剤、並びに、(C)水、を含有させる工程を含む、口腔用組成物の歯茎への密着性を増強する方法。
Furthermore, the present invention provides the following methods.
Item 12.
A method for enhancing the adhesion of an oral composition to the gums, which comprises the step of containing (A) a fatty acid dextrin, (B) a polymer compound and/or an abrasive, and (C) water.
本発明の口腔用組成物は、歯茎、口腔粘膜などの口腔組織に対する密着性が増強される。その結果、水溶性及び油溶性の薬効成分などを基剤ごと口腔組織に密着させることができ、口腔内における剤の薬効作用などを高めることができる。 The oral composition of the present invention has enhanced adhesion to oral tissues such as gums and oral mucosa. As a result, the water-soluble and oil-soluble medicinal components and the like can be brought into close contact with the oral tissue together with the base, and the medicinal action of the drug in the oral cavity can be enhanced.
[口腔用組成物]
本発明の口腔用組成物は、(A)脂肪酸デキストリン、(B)高分子化合物及び/又は研磨剤、並びに、(C)水、を含有する、口腔用組成物である。
[Composition for oral cavity]
The oral composition of the present invention is an oral composition containing (A) a fatty acid dextrin, (B) a polymer compound and/or an abrasive, and (C) water.
[(A)脂肪酸デキストリン]
脂肪酸デキストリンとは、デキストリンと脂肪酸とのエステル化合物をいう。
[(A) Fatty acid dextrin]
The fatty acid dextrin refers to an ester compound of dextrin and fatty acid.
脂肪酸デキストリンを構成する脂肪酸は、炭素数6〜24のものが好ましく、例えば、パルミチン酸、ステアリン酸、アラキン酸、オクタン酸、カプリン酸、ラウリン酸、ミリスチン酸、ベヘン酸等が挙げられる。中でも、本発明の効果をより顕著に奏する観点から、脂肪酸デキストリンを構成する脂肪酸としては、パルミチン酸が好ましい。 The fatty acid constituting the fatty acid dextrin preferably has 6 to 24 carbon atoms, and examples thereof include palmitic acid, stearic acid, arachidic acid, octanoic acid, capric acid, lauric acid, myristic acid, and behenic acid. Among them, palmitic acid is preferable as the fatty acid that constitutes the fatty acid dextrin, from the viewpoint that the effect of the present invention is more remarkably exhibited.
本発明の口腔用組成物に含まれる脂肪酸デキストリンは、1種以上の脂肪酸により構成され得る。 The fatty acid dextrin contained in the oral composition of the present invention may be composed of one or more fatty acids.
脂肪酸デキストリンは、医薬品、医薬部外品又は化粧品分野において一般的に用いられるものであれば特に限定されず、例えば、市販のものを利用でき、商品名「レオパールKL(表示名称:パルミチン酸デキストリン)」(千葉製粉株式会社製)、「レオパールKL2(表示名称:パルミチン酸デキストリン)」(千葉製粉株式会社製)、商品名「レオパールTL(表示名称:パルミチン酸デキストリン)」(千葉製粉株式会社製)、商品名「レオパールTL2(表示名称:パルミチン酸デキストリン)」(千葉製粉株式会社製)、商品名「レオパールTT(表示名称:(パルミチン酸/オクタン酸)デキストリン)」(千葉製粉株式会社製)、商品名「レオパールTT2(表示名称:(パルミチン酸/オクタン酸)デキストリン)」(千葉製粉株式会社製)等が挙げられる。 The fatty acid dextrin is not particularly limited as long as it is generally used in the fields of pharmaceuticals, quasi drugs or cosmetics, and, for example, commercially available products can be used, and the trade name is “Leopearl KL (display name: dextrin palmitate). "(Chiba Flour Milling Co., Ltd.), "Leopearl KL2 (Display name: dextrin palmitate)" (Chiba Flour Milling Co., Ltd.), product name "Leopearl TL (display name: Dextrin palmitate dextrin)" (Chiba Flourishing Co., Ltd.) , Product name "Leopearl TL2 (display name: dextrin palmitate)" (manufactured by Chiba Flour Milling Co., Ltd.), product name "Leopearl TT (display name: (palmitic acid/octanoic acid) dextrin)" (manufactured by Chiba Milling Co., Ltd.), The trade name is "Leopard TT2 (display name: (palmitic acid/octanoic acid) dextrin)" (manufactured by Chiba Flour Milling Co., Ltd.) and the like.
(A)成分の含有量は、特に限定されないが、口腔組織に対する密着性を高める観点から、口腔用組成物の全量に対して、好ましくは、0.01質量%以上、より好ましくは0.05質量%以上、更に好ましくは0.1質量%以上、特に好ましくは0.25質量%以上である。 The content of the component (A) is not particularly limited, but from the viewpoint of enhancing the adhesion to oral tissues, it is preferably 0.01% by mass or more, and more preferably 0.05% by mass with respect to the total amount of the oral composition. It is at least mass%, more preferably at least 0.1 mass%, particularly preferably at least 0.25 mass%.
(A)成分の含有量は、使用感を良好とする観点から、口腔用組成物の全量に対して、好ましくは2質量%以下、より好ましくは1質量%以下、特に好ましくは0.75質量%以下である。 The content of the component (A) is preferably 2% by mass or less, more preferably 1% by mass or less, and particularly preferably 0.75% by mass, based on the total amount of the oral composition, from the viewpoint of improving the feeling of use. % Or less.
(A)成分の含有量は、口腔用組成物の全量に対して、好ましくは0.05〜2質量%、より好ましくは0.1〜1質量%、更に好ましくは0.25〜0.75質量%である。 The content of the component (A) is preferably 0.05 to 2% by mass, more preferably 0.1 to 1% by mass, and still more preferably 0.25 to 0.75, based on the total amount of the oral composition. It is% by mass.
[(B)高分子化合物又は研磨剤]
本発明の口腔用組成物に含まれる高分子化合物は、天然由来の物質であっても、化学合成によって得られる物質であってもよい。
[(B) Polymer Compound or Abrasive]
The polymer compound contained in the oral composition of the present invention may be a naturally derived substance or a substance obtained by chemical synthesis.
高分子化合物としては、例えば、カルボキシビニルポリマー、ポリアクリル酸ナトリウム、ポリビニルアルコール、ポリビニルピロリドン、アクリル酸メタクリル酸アルキル共重合体、ポリエチレングリコール、マクロゴール、(アクリル酸ヒドロキシエチル/アクリロイルジメチルタウリンNa)コポリマー、(アクリロイルジメチルタウリンアンモニウム/ビニルピロリドン)コポリマー、ポリペプチド(ゼラチン等)、直鎖状多糖類(アルギン酸又はその塩、プルラン、セルロース系高分子、ペクチン、カラギーナン、ジェランガム、寒天、アルギン酸プロピレングリコール、コンドロイチン硫酸ナトリウム、ヒアルロン酸、ヒアルロン酸ナトリウム等)などの直鎖状高分子化合物;グアーガム、ローカストビーンガム、キサンタンガム、アラビアガム、カラヤガム、増粘性無水ケイ酸、ベントナイトなどの分岐鎖状高分子化合物が挙げられる。 Examples of the polymer compound include carboxyvinyl polymer, sodium polyacrylate, polyvinyl alcohol, polyvinylpyrrolidone, alkyl methacrylate methacrylate copolymer, polyethylene glycol, macrogol, (hydroxyethyl acrylate/acryloyldimethyltaurine Na) copolymer. , (Acryloyldimethyltaurine ammonium/vinylpyrrolidone) copolymer, polypeptide (gelatin etc.), linear polysaccharide (alginic acid or its salt, pullulan, cellulosic polymer, pectin, carrageenan, gellan gum, agar, propylene glycol alginate, chondroitin Linear polymer compounds such as sodium sulfate, hyaluronic acid, sodium hyaluronate); branched polymer compounds such as guar gum, locust bean gum, xanthan gum, gum arabic, karaya gum, thickening anhydrous silicic acid and bentonite. Be done.
本発明の口腔用組成物に含まれる研磨剤としては、限定はされないが、例えばリン酸水素カルシウム(第二リン酸カルシウム)・2水和物又は無水和物、ピロリン酸カルシウム、第三リン酸カルシウム、ハイドロキシアパタイト、第四リン酸カルシウム等のリン酸カルシウム系研磨剤;無水ケイ酸、結晶性シリカ、非晶性シリカ、シリカゲル、沈降性シリカ、アルミノシリケート、ジルコノシリケート等のシリカ系研磨剤;ゼオライト;炭酸カルシウム系研磨剤;不溶性メタリン酸カリウム;酸化アルミニウム;水酸化アルミニウム;アルミナ;炭酸マグネシウム;第三リン酸マグネシウム;酸化亜鉛;合成樹脂系研磨剤などを用いることができる。中でも、リン酸カルシウム系研磨剤又はシリカ系研磨剤がより好ましく、リン酸カルシウム系研磨剤が更に好ましく、リン酸水素カルシウム・2水和物又は無水和物が特に好ましい。 The abrasive contained in the composition for oral cavity of the present invention is not limited, for example, calcium hydrogen phosphate (dicalcium phosphate) dihydrate or anhydrate, calcium pyrophosphate, tricalcium phosphate, hydroxyapatite, Calcium phosphate-based abrasives such as quaternary calcium phosphate; silica-based abrasives such as silicic acid anhydride, crystalline silica, amorphous silica, silica gel, precipitated silica, aluminosilicate, and zirconosilicate; zeolite; calcium carbonate-based abrasive; Insoluble potassium metaphosphate; aluminum oxide; aluminum hydroxide; alumina; magnesium carbonate; magnesium triphosphate; zinc oxide; synthetic resin abrasives and the like can be used. Among them, calcium phosphate-based abrasives or silica-based abrasives are more preferred, calcium phosphate-based abrasives are still more preferred, and calcium hydrogen phosphate dihydrate or anhydrate is particularly preferred.
これらの(B)成分は、医薬品、医薬部外品又は化粧品分野において一般的に用いられるものであれば特に限定されず、例えば、市販のものも使用することができる。 The component (B) is not particularly limited as long as it is generally used in the fields of medicines, quasi drugs or cosmetics, and for example, commercially available products can be used.
これらの(B)成分は、すべて、1種単独で用いてもよく、2種以上を任意に組み合わせて用いてもよい。限定はされないが、本発明の効果を顕著に奏する観点及び口腔組織との間の摩擦を低減する観点から、(B)成分は、高分子化合物が好ましく、直鎖状高分子がより好ましく、カルボキシビニルポリマー、アルギン酸又はその塩、プルラン及びセルロース系高分子からなる群から選ばれる成分がさらに好ましい。また、(B)成分は、2種以上組み合わせることができる。(B)成分を2種以上組み合わせる場合、限定はされず、他の配合成分の種類及び含有量、製剤形態、使用方法等に応じて適宜設定されるが、カルボキシビニルポリマー、アルギン酸又はその塩、プルラン及びセルロース系高分子からなる群から選ばれる2種以上を組み合わせることが好ましい。 These (B) components may be used alone or in any combination of two or more. Although not limited, the component (B) is preferably a polymer compound, more preferably a linear polymer, from the viewpoint of significantly exhibiting the effect of the present invention and the viewpoint of reducing friction with the oral tissue, and carboxy. A component selected from the group consisting of vinyl polymer, alginic acid or a salt thereof, pullulan and a cellulosic polymer is more preferable. Further, the component (B) can be a combination of two or more kinds. When two or more kinds of the component (B) are combined, there is no limitation, and it is appropriately set according to the type and content of other compounding ingredients, the form of the formulation, the method of use, etc., but a carboxyvinyl polymer, alginic acid or a salt thereof, It is preferable to combine two or more selected from the group consisting of pullulan and a cellulosic polymer.
カルボキシビニルポリマーは、カルボキシル基を有するアクリル酸、メタアクリル酸等を主体とするビニルポリマーであり、そのモノマー構成や分子量等に特に制約はなく、市販されている種々のカルボキシビニルポリマーを特に制限無く使用することができる。これら市販品としては、例えば、ルーブリゾール(Lubrizol Advanced Materials)社から販売されているカーボポール940(Carbopol 940)、カーボポール941(Carbopol 941)、カーボポール980(Carbopol 980)、カーボポール981(Carbopol 981)、カーボポールUltrez10(Carbopol Ultrez10)、カーボポールETD2050(Carbopol ETD2050)や、和光純薬社から販売されているハイビスワコー103、ハイビスワコー104、ハイビスワコー105、3Vシグマ社から販売されているシンタレンK、シンタレンLや、住友精化社から販売されているアクペックHV-501(AQUPEC HV-501)、アクペックHV-504(AQUPEC HV-504)、アクペックHV-505(AQUPEC HV-505)、アクペックHV-501E(AQUPEC HV-501E)、アクペックHV-504E(AQUPEC HV-504E)、アクペックHV-505E(AQUPEC HV-505E)、アクペックHV-501ER(AQUPEC HV-501ER)、アクペックHV-505ED(AQUPEC HV-505ED)等が挙げられる。 Carboxyvinyl polymer is a vinyl polymer mainly composed of acrylic acid having a carboxyl group, methacrylic acid, etc., there is no particular restriction on the monomer composition or molecular weight, and various commercially available carboxyvinyl polymers are not particularly limited. Can be used. Examples of these commercially available products include Carbopol 940, Carbopol 941, Carbopol 980, and Carbopol 981 sold by Lubrizol Advanced Materials. 981), Carbopol Ultrez10 (Carbopol Ultrez10), Carbopol ETD2050 (Carbopol ETD2050) and Hibiswako 103, Hibiswako 104, Hibiswako 105, Hibiswako 105 sold by Wako Pure Chemicals Co., and Shintalen sold by 3V Sigma. K, Synthalene L, and Apec HV-501 (AQUPEC HV-501), Apepek HV-504 (AQUPEC HV-504), Apepek HV-505 (AQUPEC HV-505), Apepek HV sold by Sumitomo Seika. -501E (AQUPEC HV-501E), Akpek HV-504E (AQUPEC HV-504E), Akpek HV-505E (AQUPEC HV-505E), Akpek HV-501ER (AQUPEC HV-501ER), Akpek HV-505ED (AQUPEC HV-) 505ED) and the like.
アルギン酸は、2種類のウロン酸、即ち、D−マンヌロン酸(M)とL−グルロン酸(G)から構成される直鎖状多糖類である。アルギン酸は市販品を使用することもできる。本発明におけるアルギン酸の塩としては、例えば、ナトリウム塩、カリウム塩などが挙げられるがこれらに限定されない。好ましくは、アルギン酸ナトリウムである。アルギン酸又はその塩は、1種又は2種以上を組み合わせて使用してもよい。アルギン酸又はその塩は、本発明の口腔内組成物の物性を好適に調整する観点から、カルシウム塩と組み合わせて用いることがより好ましい。 Alginic acid is a linear polysaccharide composed of two types of uronic acids, namely D-mannuronic acid (M) and L-guluronic acid (G). A commercial item can also be used for alginic acid. Examples of the salt of alginic acid in the present invention include, but are not limited to, sodium salt, potassium salt and the like. Preferred is sodium alginate. You may use alginic acid or its salt 1 type or in combination of 2 or more types. From the viewpoint of suitably adjusting the physical properties of the oral composition of the present invention, alginic acid or a salt thereof is more preferably used in combination with a calcium salt.
プルランは、グルコース3分子がそれぞれα−1,4結合したマルトトリオースが、規則正しくα−1,6−結合でつながれた構造を持つ水溶性多糖である。市販品として、例えば(株)林原から食品添加物として販売されているものなどを使用することができる。 Pullulan is a water-soluble polysaccharide having a structure in which maltotriose in which three glucose molecules are each linked by α-1,4 are regularly linked by α-1,6-bonds. As a commercially available product, for example, one sold as a food additive by Hayashibara Co., Ltd. can be used.
セルロース系高分子化合物は、セルロースのヒドロキシル基を他の官能基で置き換えることで得られるセルロース系高分子化合物である。セルロースのヒドロキシル基を置換する官能基としてはメトキシ基、エトキシ基、ヒドロキシメトキシ基、ヒドロキシエトキシ基、ヒドロキシプロポキシ基、カルボキシメトキシ基、カルボキシエトキシ基等がある。セルロース系高分子化合物は、例えば、具体的には、メチルセルロース、エチルセルロース、ヒドロキシエチルメチルセルロース、ヒドロキシエチルセルロース(HEC)、ヒドロキシプロピルセルロース(HPC)、ヒドロキシプロピルメチルセルロース(HPMC)、カルボキシメチルセルロース(CMC)及びその塩類(例えば、カルメロースナトリウム、カルメロースカルシウム、カルメロースアンモニウム)、ステアロキシヒドロキシプロピルメチルセルロース、結晶セルロース、塩化O−[2−ヒドロキシ−3−(トリメチルアンモニオ)プロピル]ヒドロキシエチルセルロース等が挙げられる。これらのセルロース系高分子は、1種又は2種類以上を組み合わせて使用することもできる。また、これらのセルロース系高分子化合物は、市販のものを用いることができ、これらの化合物の1種又は2種以上を組み合わせて使用してもよい。 The cellulose-based polymer compound is a cellulose-based polymer compound obtained by replacing the hydroxyl group of cellulose with another functional group. Examples of the functional group that replaces the hydroxyl group of cellulose include a methoxy group, an ethoxy group, a hydroxymethoxy group, a hydroxyethoxy group, a hydroxypropoxy group, a carboxymethoxy group, and a carboxyethoxy group. Specific examples of the cellulose-based polymer compound include methyl cellulose, ethyl cellulose, hydroxyethyl methyl cellulose, hydroxyethyl cellulose (HEC), hydroxypropyl cellulose (HPC), hydroxypropyl methyl cellulose (HPMC), carboxymethyl cellulose (CMC) and salts thereof. (For example, carmellose sodium, carmellose calcium, carmellose ammonium), stearoxyhydroxypropyl methylcellulose, crystalline cellulose, O-[2-hydroxy-3-(trimethylammonio)propyl]hydroxyethyl cellulose chloride and the like. These cellulose-based polymers may be used alone or in combination of two or more. Moreover, as these cellulose-based polymer compounds, commercially available products may be used, and one kind or two or more kinds of these compounds may be used in combination.
(B)成分の総含有量は、特に限定されず、他の配合成分の種類及び含有量、製剤形態、使用方法等に応じて適宜設定されるが、本発明の効果を顕著に奏する観点から、口腔用組成物の全量に対して、好ましくは0.01質量%以上、より好ましくは0.05質量%以上、更に好ましくは0.1質量%以上、さらにより好ましくは0.25重量%以上、特に好ましくは0.5質量%以上である。 The total content of the component (B) is not particularly limited and may be appropriately set depending on the types and contents of other compounding ingredients, the form of the formulation, the method of use, etc., but from the viewpoint of remarkably exerting the effect of the present invention. , Preferably 0.01% by mass or more, more preferably 0.05% by mass or more, further preferably 0.1% by mass or more, even more preferably 0.25% by weight or more, based on the total amount of the composition for oral cavity. , Particularly preferably 0.5% by mass or more.
(B)成分の総含有量は、本発明の効果を顕著に奏する観点から、口腔用組成物の全量に対して、好ましくは50質量%以下、より好ましくは30質量%以下、更に好ましくは20質量%以下、特に好ましくは15質量%以下である。 The total content of the component (B) is preferably 50% by mass or less, more preferably 30% by mass or less, and further preferably 20% with respect to the total amount of the oral composition, from the viewpoint of remarkably exerting the effect of the present invention. It is not more than 15% by mass, particularly preferably not more than 15% by mass.
(B)成分の総含有量は、口腔用組成物の全量に対して、好ましくは0.01〜50質量%、より好ましくは0.05〜30質量%、更に好ましくは0.1〜20質量%、さらにより好ましくは0.25〜20重量%、特に好ましくは0.5〜15質量%である。 The total content of the component (B) is preferably 0.01 to 50% by mass, more preferably 0.05 to 30% by mass, and still more preferably 0.1 to 20% by mass based on the total amount of the oral composition. %, even more preferably 0.25 to 20% by weight, and particularly preferably 0.5 to 15% by weight.
(B)成分が高分子化合物である場合、高分子化合物の総含有量は、特に限定されず、他の配合成分の種類及び含有量、製剤形態、使用方法等に応じて適宜設定されるが、本発明の効果を顕著に奏する観点から、口腔用組成物の全量に対して、好ましくは0.05質量%以上、より好ましくは0.1質量%以上、更に好ましくは0.5質量%以上、特に好ましくは1質量%以上である。 When the component (B) is a polymer compound, the total content of the polymer compound is not particularly limited and may be appropriately set depending on the types and contents of other compounding ingredients, the form of the formulation, the method of use, etc. From the viewpoint of remarkably exerting the effect of the present invention, preferably 0.05 mass% or more, more preferably 0.1 mass% or more, still more preferably 0.5 mass% or more with respect to the total amount of the oral composition. , Particularly preferably 1% by mass or more.
(B)成分が高分子化合物である場合、高分子化合物の総含有量は、本発明の効果を顕著に奏する観点から、口腔用組成物の全量に対して、好ましくは7.5質量%以下、より好ましくは5質量%以下、更に好ましくは3質量%以下、特に好ましくは2質量%以下、最も好ましくは1.5重量%以下である。 When the component (B) is a polymer compound, the total content of the polymer compounds is preferably 7.5% by mass or less with respect to the total amount of the composition for oral cavity, from the viewpoint of remarkably exerting the effect of the present invention. , More preferably 5% by mass or less, further preferably 3% by mass or less, particularly preferably 2% by mass or less, and most preferably 1.5% by mass or less.
(B)成分が高分子化合物である場合、高分子化合物の総含有量は、口腔用組成物の全量に対して、好ましくは0.05〜7.5質量%、より好ましくは0.1〜5質量%、更に好ましくは0.5〜3質量%、特に好ましくは1〜2質量%である。 When the component (B) is a polymer compound, the total content of the polymer compounds is preferably 0.05 to 7.5% by mass, more preferably 0.1 to 7.5% by mass relative to the total amount of the oral composition. It is 5% by mass, more preferably 0.5 to 3% by mass, and particularly preferably 1 to 2% by mass.
限定はされないが、好ましい態様では、例えば、カルボキシビニルポリマーを(B)成分として含有する場合に、カルボキシビニルポリマーの単独の含有量は、口腔用組成物の全量に対して、好ましくは0.05〜7.5質量%、より好ましく0.1〜5質量%、更に好ましくは0.5〜2質量%、特に好ましくは1〜1.5質量%である。 Although not limited, in a preferred embodiment, for example, when a carboxyvinyl polymer is contained as the component (B), the content of the carboxyvinyl polymer alone is preferably 0.05 with respect to the total amount of the oral composition. ˜7.5% by mass, more preferably 0.1 to 5% by mass, even more preferably 0.5 to 2% by mass, particularly preferably 1 to 1.5% by mass.
限定はされないが、好ましい態様では、例えば、アルギン酸又はその塩を(B)成分として含有する場合に、アルギン酸又はその塩の単独の含有量は、口腔用組成物の全量に対して、好ましくは0.01〜10質量%、より好ましくは0.05〜5質量%、更に好ましくは0.1〜2質量%、特に好ましくは0.3〜1質量%である。 Although not limited, in a preferred embodiment, for example, when alginic acid or a salt thereof is contained as the component (B), the content of alginic acid or a salt alone is preferably 0 relative to the total amount of the oral composition. 0.01 to 10% by mass, more preferably 0.05 to 5% by mass, still more preferably 0.1 to 2% by mass, and particularly preferably 0.3 to 1% by mass.
(B)成分が研磨剤である場合、(B)成分の総含有量は、特に限定されず、他の配合成分の種類及び含有量、製剤形態、使用方法等に応じて適宜設定されるが、本発明の効果をより顕著に奏する観点から、口腔用組成物の全量に対して、好ましくは0.5質量%以上、より好ましくは1質量%以上、更に好ましくは5質量%以上である。 When the component (B) is an abrasive, the total content of the component (B) is not particularly limited, and is appropriately set according to the types and contents of other compounding components, the formulation form, the method of use, and the like. From the viewpoint of more remarkably exerting the effect of the present invention, it is preferably 0.5% by mass or more, more preferably 1% by mass or more, and further preferably 5% by mass or more based on the total amount of the oral composition.
(B)成分が研磨剤である場合、(B)成分の総含有量は、本発明の効果をより顕著に奏する観点から、口腔用組成物の全量に対して、好ましくは50質量%以下、より好ましくは20質量%以下、更に好ましくは15質量%以下である。 When the component (B) is an abrasive, the total content of the component (B) is preferably 50% by mass or less based on the total amount of the composition for oral cavity, from the viewpoint of more conspicuously exhibiting the effect of the present invention. It is more preferably 20% by mass or less, still more preferably 15% by mass or less.
(B)成分が研磨剤である場合、研磨剤の総含有量は、口腔用組成物の全量に対して、好ましくは0.5〜50質量%、より好ましくは1〜20質量%、更に好ましくは5〜15質量%である。 When the component (B) is an abrasive, the total content of the abrasive is preferably 0.5 to 50% by mass, more preferably 1 to 20% by mass, and still more preferably the total amount of the oral composition. Is 5 to 15% by mass.
[各成分の比]
本発明の口腔用組成物における(A)成分の総含有量1質量部に対する(B)成分の総含有量((B)/(A))は、特に限定されないが、本発明の効果を顕著に奏する観点から、好ましくは0.01〜500質量部、より好ましくは0.05〜200質量部、更に好ましくは0.1〜100質量部、特に好ましくは0.5〜50質量部である。
[Ratio of each component]
The total content ((B)/(A)) of the component (B) per 1 part by mass of the total content of the component (A) in the oral composition of the present invention is not particularly limited, but the effect of the present invention is remarkable. From the viewpoint of achieving the above, the amount is preferably 0.01 to 500 parts by mass, more preferably 0.05 to 200 parts by mass, further preferably 0.1 to 100 parts by mass, and particularly preferably 0.5 to 50 parts by mass.
本発明の(B)成分が高分子化合物である場合、本発明の口腔用組成物における(A)成分の総含有量1質量部に対する(B)成分の総含有量((B)/(A))は、特に限定されないが、本発明の効果を顕著に奏する観点から、好ましくは0.1〜50質量部、より好ましくは0.5〜20質量部、更に好ましくは1〜10質量部、特に好ましくは1.3〜6質量部である。 When the component (B) of the present invention is a polymer compound, the total content of the component (B) per part by mass of the component (A) in the oral composition of the present invention ((B)/(A )) is not particularly limited, but is preferably 0.1 to 50 parts by mass, more preferably 0.5 to 20 parts by mass, still more preferably 1 to 10 parts by mass, from the viewpoint of significantly exhibiting the effect of the present invention. It is particularly preferably 1.3 to 6 parts by mass.
本発明の(B)成分が研磨剤である場合、本発明の口腔用組成物における(A)成分の総含有量1質量部に対する(B)成分の総含有量((B)/(A))は、特に限定されないが、本発明の効果を顕著に奏する観点から、好ましくは、0.1〜500質量部、より好ましくは0.5〜200質量部、更に好ましくは1〜100質量部、特に好ましくは5〜50質量部である。 When the component (B) of the present invention is an abrasive, the total content of the component (B) with respect to 1 part by mass of the total content of the component (A) in the oral composition of the present invention ((B)/(A)) ) Is not particularly limited, but from the viewpoint of significantly exhibiting the effect of the present invention, preferably 0.1 to 500 parts by mass, more preferably 0.5 to 200 parts by mass, further preferably 1 to 100 parts by mass, It is particularly preferably 5 to 50 parts by mass.
[(C)水]
本発明の口腔用組成物は、水を含む。水の含有量は、使用感を向上させる観点から、口腔用組成物の全量に対して、好ましくは30質量%以上、より好ましくは40質量%以上、更に好ましくは50質量%以上であり、好ましくは80重量%以下、より好ましくは75重量%以下、更に好ましくは70重量%以下である。
[(C) Water]
The oral composition of the present invention contains water. From the viewpoint of improving the feeling of use, the content of water is preferably 30% by mass or more, more preferably 40% by mass or more, and further preferably 50% by mass or more, based on the total amount of the oral composition. Is 80% by weight or less, more preferably 75% by weight or less, still more preferably 70% by weight or less.
[薬効成分]
本発明の口腔用組成物には、本発明の効果を損なわない範囲で、薬効成分として、例えば、殺菌剤(カチオン性殺菌剤(塩化セチルピリジニウム、塩化ベンゼトニウム、グルコン酸クロルヘキシジン、塩酸クロルヘキシジンなど)、両性殺菌剤(ドデシルアミノエチルグリシンなど)、非イオン性殺菌剤(イソプロピルメチルフェノール、ヒノキチオール、トリクロサン、チモール、1,8−シネオールなど)、アニオン性殺菌剤(ラウロイルサルコシンナトリウム(LSS)など))、組織修復剤(アラントイン;アラントインβ−グリチルレチン酸、アラントインジヒドロキシアルミニウム(アルジオキサ)、アラントインクロルヒドロキシアルミニウム(アルクロキサ)、アラントインポリガラクツロン酸、アラントインアスコルビン酸、アラントインアセチル−DL−メチオニン、アラントインDL−パントテニルアルコール、DL−ピロリドンカルボン酸ナトリウム・アラントイン等のアラントインの塩;パンテノールなど)、抗炎症剤(アラントイン又はその塩、トラネキサム酸、グリチルリチン酸又はその塩(グリチルリチン酸二カリウム、グリチルリチン酸モノアンモニウム等)、β−グリチルレチン酸又はその誘導体(グリチルレチン酸ステアリル等)、サリチル酸メチル、l−メントール、トラネキサム酸、ε−アミノカプロン酸、オウバクエキスなど)、出血抑制剤(カルバゾクロム、トラネキサム酸、ε−アミノカプロン酸など)、知覚過敏抑制剤(硝酸カリウム、塩化ストロンチウム、乳酸アルミニウムなど)、血行促進剤(ビタミンE類(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;酢酸dl−α−トコフェロール等の酢酸トコフェロール、ニコチン酸トコフェロール、コハク酸トコフェロール等)など)、収斂剤(塩化ナトリウムなど)、再石灰化剤(フッ化ナトリウム、モノフルオロリン酸ナトリウム(MFP)、フッ化スズなど)、酵素(ラクトフェリン、ラクトパーオキシダーゼ、デキストラナーゼ、リゾチーム、プロテアーゼ、アミラーゼ、ムタナーゼなど)、銅クロロフィリンナトリウム、リン酸L−アスコルビルマグネシウム、塩化亜鉛、ポリリン酸ナトリウム、ピロリン酸ナトリウムなどを組み合わせて用いることができる。これらの薬効成分は、1種単独で用いてもよいし、2種以上の組み合わせで用いてもよい。
[Medicinal properties]
The oral composition of the present invention, as long as the effect of the present invention is not impaired, as a medicinal component, for example, a bactericide (cationic bactericide (cetylpyridinium chloride, benzethonium chloride, chlorhexidine gluconate, chlorhexidine hydrochloride, etc.), Amphoteric fungicides (dodecylaminoethylglycine, etc.), nonionic fungicides (isopropylmethylphenol, hinokitiol, triclosan, thymol, 1,8-cineole, etc.), anionic fungicides (lauroylsarcosine sodium (LSS), etc.), Tissue repair agent (allantoin; allantoin β-glycyrrhetinic acid, allantoin dihydroxyaluminum (aldioxa), allantoin chlorhydroxyaluminum (alcloxa), allantoin polygalacturonic acid, allantoin ascorbic acid, allantoin acetyl-DL-methionine, allantoin DL-pantothenyl alcohol, Allantoin salts such as DL-pyrrolidone carboxylic acid sodium allantoin; panthenol etc.), anti-inflammatory agents (allantoin or its salts, tranexamic acid, glycyrrhizinic acid or its salts (dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, etc.), β -Glycyrrhetinic acid or a derivative thereof (stearyl glycyrrhetinate, etc.), methyl salicylate, 1-menthol, tranexamic acid, ε-aminocaproic acid, oat extract, etc., bleeding inhibitor (carbazochrome, tranexamic acid, ε-aminocaproic acid, etc.), perception Hypersensitivity inhibitors (potassium nitrate, strontium chloride, aluminum lactate, etc.), blood circulation promoters (vitamin Es (α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol; tocopherol acetate such as dl-α-tocopherol acetate, nicotine) Acid tocopherol, tocopherol succinate, etc.), astringent (sodium chloride, etc.), remineralizing agent (sodium fluoride, sodium monofluorophosphate (MFP), tin fluoride, etc.), enzyme (lactoferrin, lactoperoxidase) , Dextranase, lysozyme, protease, amylase, mutanase, etc.), sodium copper chlorophyllin, magnesium L-ascorbyl phosphate, zinc chloride, sodium polyphosphate, sodium pyrophosphate and the like can be used in combination. These medicinal components may be used alone or in combination of two or more.
本発明の口腔用組成物には、本発明の効果を損なわない範囲で、アスナロエキス、オウバクエキス、トウキエキス、オウゴンエキス、カミツレエキス、ラタニアエキス、ミルラエキス、マヌカハニー抽出物、ポリフェノール類、カテキン類、フラボン類、プロアントシアニン類などの植物由来の薬効成分を単独で、又は2種以上を組み合わせて用いることができる。 In the oral composition of the present invention, as long as the effect of the present invention is not impaired, asunaro extract, psyllium extract, Japanese laurel extract, sardine extract, chamomile extract, latania extract, myrrh extract, manuka honey extract, polyphenols, catechins , Medicinal ingredients derived from plants such as flavones and proanthocyanins can be used alone or in combination of two or more kinds.
本発明の口腔用組成物には、本発明の効果を損なわない範囲で、その他の薬効成分として、クエン酸亜鉛、サンギナリン、デルモピノール、ナイシン、キトサン、クロロフィルなどを、単独で、又は2種以上を組み合わせて用いることができる。 The oral composition of the present invention, as long as the effects of the present invention are not impaired, as other medicinal components, zinc citrate, sanguinarine, delmopinol, nisin, chitosan, chlorophyll, etc., alone or in combination of two or more. It can be used in combination.
本発明の口腔用組成物は、本願発明の効果をより顕著に奏する観点から、薬効成分としては、殺菌剤、組織修復剤、抗炎症剤、及び血行促進剤からなる群より選択される少なくとも一種を含有することが好ましく、カチオン性殺菌剤、アラントイン、グリチルリチン酸又はその塩、β−グリチルレチン酸又はその誘導体、及びビタミンE類からなる群より選択される少なくとも一種を含有することが好ましく、塩化セチルピリジニウム、アラントイン、グリチルリチン酸二カリウム、β―グリチルレチン酸、及び酢酸トコフェロールからなる群より選択される少なくとも一種を含有することが更に好ましい。 The oral composition of the present invention has at least one selected from the group consisting of a bactericidal agent, a tissue repairing agent, an anti-inflammatory agent, and a blood circulation promoting agent, as the medicinal component, from the viewpoint of more remarkably exhibiting the effect of the present invention. It is preferable to contain a cationic bactericide, allantoin, glycyrrhizinic acid or a salt thereof, β-glycyrrhetinic acid or a derivative thereof, and at least one selected from the group consisting of vitamin Es, and cetyl chloride. It is more preferable to contain at least one selected from the group consisting of pyridinium, allantoin, dipotassium glycyrrhizinate, β-glycyrrhetinic acid, and tocopherol acetate.
本発明の口腔用組成物に用いられる薬効成分は、水溶性であっても非水溶性であっても本発明の効果を抑制せず、また本発明の効果により歯茎への密着性増強作用が期待できる。中でも、水溶性の薬効成分がより好ましい。 The medicinal component used in the composition for oral cavity of the present invention does not suppress the effect of the present invention whether it is water-soluble or water-insoluble, and the effect of the present invention has an action of enhancing adhesion to gums. Can be expected. Of these, water-soluble medicinal components are more preferable.
[界面活性剤]
本発明の口腔用組成物は、界面活性剤を更に含有してもよい。界面活性剤を含有することで、本発明による効果がより顕著に奏される。
[Surfactant]
The oral composition of the present invention may further contain a surfactant. By containing the surfactant, the effect of the present invention is more remarkably exhibited.
界面活性剤としては、非イオン性界面活性剤、両性界面活性剤、陰イオン性界面活性剤、陽イオン性界面活性剤などを用いることができる。中でも、本発明の効果を顕著に奏する観点から、非イオン性界面活性剤及び両性界面活性剤からなる群より選択される少なくとも1種以上を含むことが好ましい。 As the surfactant, a nonionic surfactant, an amphoteric surfactant, an anionic surfactant, a cationic surfactant and the like can be used. Among them, it is preferable that at least one selected from the group consisting of nonionic surfactants and amphoteric surfactants is contained from the viewpoint of remarkably exerting the effect of the present invention.
非イオン性界面活性剤としては、例えば、ソルビタンモノイソステアレート、ソルビタンモノラウレート、ソルビタンモノパルミテート、ソルビタンモノステアレート、ペンタ−2−エチルヘキシル酸ジグリセロールソルビタン、テトラ−2−エチルヘキシル酸ジグリセロールソルビタン等のソルビタン脂肪酸エステル類;モノラウリル酸ポリオキシエチレン(20)ソルビタン(ポリソルベート20)、モノステアリン酸ポリオキシエチレン(20)ソルビタン(ポリソルベート60)、モノオレイン酸ポリオキシエチレン(20)ソルビタン(ポリソルベート80)、イソステアリン酸ポリオキシエチレン(20)ソルビタン等のポリオキシエチレンソルビタン脂肪酸エステル類;モノオレイン酸ポリエチレングリコール、モノラウリン酸ポリエチレングリコール等のポリエチレングリコール脂肪酸エステル類;モノステアリン酸プロピレングリコール等のプロピレングリコール脂肪酸エステル類;ポリオキシエチレン硬化ヒマシ油40(HCO−40)、ポリオキシエチレン硬化ヒマシ油50(HCO−50)、ポリオキシエチレン硬化ヒマシ油60(HCO−60)、ポリオキシエチレン硬化ヒマシ油80等の硬化ヒマシ油誘導体;ラウリン酸ジエタノールアミド等の脂肪酸アルカノールアミド;グリセリンアルキルエーテル;ラウリルグルコシド、デシルグルコシド等のアルキルグルコシド;ポリオキシエチレン(20)オレイルエーテル、ポリオキシエチレンセチルエーテル等のポリオキシアルキレンアルキルエーテル;ポリグリセリン脂肪酸エステル、ポリオキシエチレングリセリン脂肪酸エステル、ポリオキシアルキレン脂肪酸エステル、モノステアリン酸グリセリル等のグリセリン脂肪酸エステル、ショ糖脂肪酸エステル、マルトース脂肪酸エステル等の糖脂肪酸エステル;マルチトール脂肪酸エステル等の糖アルコール脂肪酸エステル;ポリオキシエチレンラウリルアルコールエーテルなどが挙げられる。 Examples of nonionic surfactants include sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, penta-2-ethylhexyl diglycerol sorbitan, tetra-2-ethylhexyl diglycerol. Sorbitan fatty acid esters such as sorbitan; polyoxyethylene (20) sorbitan monolaurate (polysorbate 20), polyoxyethylene (20) sorbitan monostearate (polysorbate 60), polyoxyethylene (20) sorbitan monooleate (polysorbate) 80), polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene (20) sorbitan isostearate; polyethylene glycol fatty acid esters such as polyethylene glycol monooleate and polyethylene glycol monolaurate; propylene glycol fatty acid such as propylene glycol monostearate Esters; polyoxyethylene hydrogenated castor oil 40 (HCO-40), polyoxyethylene hydrogenated castor oil 50 (HCO-50), polyoxyethylene hydrogenated castor oil 60 (HCO-60), polyoxyethylene hydrogenated castor oil 80, etc. Hydrogenated castor oil derivative; fatty acid alkanolamide such as lauric acid diethanolamide; glycerin alkyl ether; alkyl glucoside such as lauryl glucoside and decyl glucoside; polyoxyalkylene alkyl such as polyoxyethylene (20) oleyl ether and polyoxyethylene cetyl ether Ether; polyglycerin fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyoxyalkylene fatty acid ester, glycerin fatty acid ester such as glyceryl monostearate, sucrose fatty acid ester, sugar fatty acid ester such as maltose fatty acid ester; maltitol fatty acid ester, etc. Sugar alcohol fatty acid ester; polyoxyethylene lauryl alcohol ether and the like.
両性界面活性剤としては、例えば、2−アルキル−N−カルボキシメチル−N−ヒドロキシエチル−N−イミダゾリニウムベタイン等のイミダゾリニウムベタイン;ラウリルスルホベタイン、ラウリルヒドロキシスルホベタイン等のアルキルスルホベタイン;ラウリルジメチルアミノ酢酸ベタイン等の酢酸ベタイン;ヤシ油脂肪酸アミドプロピルベタイン等のヤシ油脂肪酸アミドアルキルベタイン;N−アルキル−1−ヒドロキシエチルイミダゾリンベタインナトリウム等の長鎖アルキルイミダゾリンベタイン塩などが挙げられる。 Examples of the amphoteric surfactant include imidazolinium betaines such as 2-alkyl-N-carboxymethyl-N-hydroxyethyl-N-imidazolinium betaine; alkylsulfobetaines such as laurylsulfobetaine and laurylhydroxysulfobetaine; Examples thereof include betaine acetate such as lauryl dimethylamino acetic acid betaine; palm oil fatty acid amide alkyl betaine such as coconut oil fatty acid amide propyl betaine; and long chain alkyl imidazoline betaine salt such as N-alkyl-1-hydroxyethyl imidazoline betaine sodium.
陰イオン性界面活性剤としては、例えば、アルキル硫酸塩(ラウリル硫酸ナトリウム等)、脂肪酸モノカルボン酸塩(ラウリン酸塩、パルミチン酸塩等)、ポリオキシエチレンアルキルエーテルカルボン酸塩、N−アシルサルコシン塩、N−アシルアミノ酸塩(N−アシルグルタミン酸塩等)、ジアルキルスルホコハク酸塩、アルカンスルホン酸塩(アルキルスルホン酸塩)、α−オレフィンスルホン酸塩、直鎖アルキルベンゼンスルホン酸塩、アルキル(分岐鎖)ベンゼンスルホン酸塩、N−メチル−N−アシルタウリン酸、ポリオキシエチレンアルキルエーテル硫酸塩、アルキルリン酸塩、ポリオキシエチレンアルキルエーテルリン酸塩、ポリオキシエチレンアルキルフェニルエーテルリン酸塩などが挙げられる。 Examples of the anionic surfactant include alkyl sulfates (sodium lauryl sulfate, etc.), fatty acid monocarboxylates (laurate, palmitate, etc.), polyoxyethylene alkyl ether carboxylates, N-acyl sarcosine. Salt, N-acyl amino acid salt (N-acyl glutamate, etc.), dialkyl sulfosuccinate, alkane sulfonate (alkyl sulfonate), α-olefin sulfonate, linear alkylbenzene sulfonate, alkyl (branched chain) ) Benzene sulfonate, N-methyl-N-acyl taurate, polyoxyethylene alkyl ether sulfate, alkyl phosphate, polyoxyethylene alkyl ether phosphate, polyoxyethylene alkyl phenyl ether phosphate and the like. Be done.
陽イオン性界面活性剤としては、例えば、モノアルキルアミン塩、ジアルキルアミン塩、トリアルキルアミン塩、アルキルトリメチルアンモニウム、ジアルキルジメチルアンモニウム塩、塩化アルキルベンザルコニウムなどが挙げられる。 Examples of the cationic surfactant include monoalkylamine salts, dialkylamine salts, trialkylamine salts, alkyltrimethylammonium salts, dialkyldimethylammonium salts, alkylbenzalkonium chlorides and the like.
その他の界面活性剤として、例えば、ポリオキシエチレン・メチルポリシロキサン共重合体、ラウリルPEG−9ポリジメチルシロキシエチルジメチコン、PEG−9ポリジメチルシロキシエチルジメチコン等のシリコーン系界面活性剤などが挙げられる。 Other surfactants include, for example, silicone surfactants such as polyoxyethylene/methylpolysiloxane copolymer, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, and PEG-9 polydimethylsiloxyethyl dimethicone.
界面活性剤としては、本発明の効果をより顕著に奏する観点から、非イオン性界面活性剤、陰イオン性界面活性剤が好ましく、非イオン性界面活性剤がより好ましく、ソルビタン脂肪酸エステル類、ポリオキシエチレンソルビタン脂肪酸エステル類が更に好ましい。
界面活性剤の総含有量は、特に限定されず、界面活性剤の種類、他の配合成分の種類及び含有量、製剤形態、使用方法等に応じて適宜設定されるが、本発明の効果をより顕著に奏し、かつ、洗浄力を十分に奏する観点から、口腔用組成物の全量に対して、好ましくは0.1〜20質量%、より好ましくは0.5〜10質量%、更に好ましくは1〜7.5質量%、特に好ましくは2〜5質量%である。
界面活性剤が非イオン界面活性剤である場合、非イオン界面活性剤の総含有量は、口腔用組成物の全量に対して、好ましくは0.1〜20質量%、より好ましくは0.5〜10質量%、更に好ましくは1〜7.5質量%、特に好ましくは2〜5質量%である。
The surfactant is preferably a nonionic surfactant or an anionic surfactant, more preferably a nonionic surfactant, or a sorbitan fatty acid ester, or a polysiloxane, from the viewpoint of more significantly exhibiting the effect of the present invention. Oxyethylene sorbitan fatty acid esters are more preferred.
The total content of the surfactant is not particularly limited, and is appropriately set depending on the type of surfactant, the type and content of other compounding ingredients, the formulation form, the method of use, etc. From the viewpoint of more remarkably and sufficiently exerting the detergency, it is preferably 0.1 to 20% by mass, more preferably 0.5 to 10% by mass, and still more preferably the total amount of the oral composition. It is 1 to 7.5 mass %, particularly preferably 2 to 5 mass %.
When the surfactant is a nonionic surfactant, the total content of the nonionic surfactant is preferably 0.1 to 20% by mass, more preferably 0.5, with respect to the total amount of the oral composition. -10 mass%, more preferably 1-7.5 mass%, particularly preferably 2-5 mass%.
[炭化水素]
本発明の口腔用組成物は、炭化水素を更に含有してもよい。炭化水素を含有することで、本発明による効果がより顕著に奏される。
[hydrocarbon]
The oral composition of the present invention may further contain a hydrocarbon. By containing a hydrocarbon, the effect of the present invention is more remarkably exhibited.
炭化水素としては、パラフィン系炭化水素やオレフィン系炭化水素が用いられ、例えば、流動パラフィン、ワセリン、スクワラン、スクワレン、セレシン、軽質流動パラフィン、パラフィンワックス、蜜蝋、カルナバワックス、プリスタン、マイクロクリスタリンワックスなどが挙げられる。本発明の効果をさらに高める観点から、流動パラフィン又はワセリンがより好ましく、流動パラフィンが更に好ましい。 As the hydrocarbon, a paraffinic hydrocarbon or an olefinic hydrocarbon is used, and examples thereof include liquid paraffin, petrolatum, squalane, squalene, ceresin, light liquid paraffin, paraffin wax, beeswax, carnauba wax, pristane, and microcrystalline wax. Can be mentioned. From the viewpoint of further enhancing the effect of the present invention, liquid paraffin or petrolatum is more preferable, and liquid paraffin is further preferable.
炭化水素の総含有量は、特に限定されず、炭化水素の種類、他の配合成分の種類及び含有量、製剤形態、使用方法等に応じて適宜設定されるが、本発明の効果を顕著に奏する観点、及び使用感をさらに高める観点から、口腔用組成物の全量に対して、好ましくは0.5〜30質量%、より好ましく1〜25質量%、更に好ましくは3〜20質量%、特に好ましくは5.1〜15質量%である。 The total content of hydrocarbons is not particularly limited, and is appropriately set depending on the type of hydrocarbon, the type and content of other compounding components, the form of the formulation, the method of use, etc. From the viewpoint of playing, and from the viewpoint of further enhancing the feeling of use, it is preferably 0.5 to 30% by mass, more preferably 1 to 25% by mass, still more preferably 3 to 20% by mass, particularly preferably 3 to 20% by mass, relative to the total amount of the oral composition. Preferably it is 5.1 to 15 mass %.
[その他添加剤]
本発明の口腔用組成物は、本発明の効果を損なわない範囲で、医薬品、医薬部外品、化粧品、食品等として用いられ得る、公知の高級アルコール、溶解補助剤、湿潤剤、保存剤、キレート剤、pH調整剤、甘味料、香料、着色剤などの添加剤を配合することができる。これらの添加剤は、いずれも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。
[Other additives]
The oral composition of the present invention is a range that does not impair the effects of the present invention, and can be used as a drug, a quasi drug, a cosmetic, a food, a known higher alcohol, a solubilizer, a wetting agent, a preservative, Additives such as chelating agents, pH adjusters, sweeteners, flavors, and colorants can be added. These additives may be used alone or in combination of two or more.
本発明の口腔用組成物は、高級アルコールを用いることができる。高級アルコールは、炭素数6以上のアルコールを指し、直鎖状又は分枝状の構造のいずれでも良い。高級アルコールとしては、限定はされないが、C8〜C24脂肪族アルコールが好ましい。このようなアルコールには、セタノール(セチルアルコール)、ステアリルアルコール、セトステアリルアルコール、ラウリルアルコール、ミリスチルアルコール、オレイルアルコール、カプリルアルコール、リノリルアルコール、又はベヘニルアルコールが含まれる。本発明の口腔用組成物の効果をさらに高める観点から、好ましくはセタノール、ステアリルアルコール、及びセトステアリルアルコールから選ばれる1種以上、より好ましくはセタノール又はステアリルアルコールから選ばれる1種以上、更に好ましくはセタノールが用いられる。 Higher alcohols can be used in the oral composition of the present invention. The higher alcohol refers to an alcohol having 6 or more carbon atoms, and may have either a linear or branched structure. As the higher alcohol, but are not limited to, C 8 -C 24 fatty alcohols are preferred. Such alcohols include cetanol (cetyl alcohol), stearyl alcohol, cetostearyl alcohol, lauryl alcohol, myristyl alcohol, oleyl alcohol, capryl alcohol, linoleyl alcohol, or behenyl alcohol. From the viewpoint of further enhancing the effect of the oral composition of the present invention, preferably one or more selected from cetanol, stearyl alcohol, and cetostearyl alcohol, more preferably one or more selected from cetanol or stearyl alcohol, and further preferably Cetanol is used.
湿潤剤としては、例えば、キシリトール、エリスリトール、マルチトール、ソルビトール、ラクチトール、トレハロース、マンニトール等の糖アルコール;エチレングリコール、プロピレングリコール、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、グリセリンなどの多価アルコールが挙げられる。 Examples of the wetting agent include sugar alcohols such as xylitol, erythritol, maltitol, sorbitol, lactitol, trehalose, and mannitol; polyhydric alcohols such as ethylene glycol, propylene glycol, butylene glycol, polyethylene glycol, polypropylene glycol, and glycerin. ..
溶解補助剤の好適な例としては、例えば、エタノール、プロパノールなどの低級アルコールなどが挙げられる。 Preferable examples of the solubilizing agent include lower alcohols such as ethanol and propanol.
保存剤としては、例えば、パラベン類(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)、安息香酸、安息香酸ナトリウム、デヒドロ酢酸、デヒドロ酢酸ナトリウム、パラオキシ安息香酸イソブチル、パラオキシ安息香酸イソプロピル、パラオキシ安息香酸ブチル、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、パラオキシ安息香酸ベンジル、パラオキシ安息香酸メチル、フェノキシエタノール、塩酸アルキルジアミノエチルグリシン、塩化ベンザルコニウム、塩化ベンゼトニウムなどが挙げられる。 Examples of the preservative include parabens (methylparaben, ethylparaben, propylparaben, butylparaben, etc.), benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, and paraoxybenzoic acid. Examples thereof include butyl, ethyl paraoxybenzoate, propyl paraoxybenzoate, benzyl paraoxybenzoate, methyl paraoxybenzoate, phenoxyethanol, alkyldiaminoethylglycine hydrochloride, benzalkonium chloride, and benzethonium chloride.
キレート剤としては、例えば、EDTA・2ナトリウム塩、EDTA・カルシウム・2ナトリウム塩などが挙げられる。 Examples of the chelating agent include EDTA.disodium salt and EDTA.calcium.disodium salt.
pH調整剤としては、例えば、無機酸(塩酸、硫酸、硝酸、リン酸など)、有機酸(乳酸、クエン酸、コハク酸、グルコン酸、マレイン酸、アジピン酸、コハク酸など)、無機塩基(水酸化カリウム、水酸化ナトリウムなど)、有機塩基(トリエタノールアミン、ジイソプロパノールアミン、トリイソプロパノールアミンなど)、塩(乳酸ナトリウム、コハク酸ナトリウム、クエン酸ナトリウム、クエン酸水素ナトリウム、酢酸ナトリウム、リン酸ナトリウム、リン酸二水素ナトリウム、炭酸ナトリウム、セスキ炭酸ナトリウム(二炭酸一水素三ナトリウム)など)、塩基性アミノ酸(リジン、アルギニンなど)などが挙げられる。 Examples of the pH adjuster include inorganic acids (hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, etc.), organic acids (lactic acid, citric acid, succinic acid, gluconic acid, maleic acid, adipic acid, succinic acid, etc.), inorganic bases ( Potassium hydroxide, sodium hydroxide, etc., organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, etc.), salts (sodium lactate, sodium succinate, sodium citrate, sodium hydrogen citrate, sodium acetate, phosphoric acid) Examples thereof include sodium, sodium dihydrogen phosphate, sodium carbonate, sodium sesquicarbonate (trisodium monohydrogen dicarbonate), and basic amino acids (lysine, arginine, etc.).
甘味料としては、例えば、糖類又は糖アルコール(キシリトール、パラチノース、エリスリトール、マルチトール、アラビトール)、ステビオサイド、ステビアエキス、ソーマチン、グリチルリチン、スクラロース、アセスルファムカリウム、サッカリンナトリウム、アスパルテーム、ネオヘスペリジルジヒドロカルコン、ペリラルチンなどが挙げられる。 Examples of the sweetener include sugars or sugar alcohols (xylitol, palatinose, erythritol, maltitol, arabitol), stevioside, stevia extract, thaumatin, glycyrrhizin, sucralose, acesulfame potassium, saccharin sodium, aspartame, neohesperidyl dihydrochalcone, perillartin and the like. Is mentioned.
[pH]
本発明の口腔用組成物のpHは、(A)及び(B)成分の種類、他の配合成分の種類及び含有量、製材形態、使用方法等に応じて適宜設定され、生理学的又は薬学的に許容できる範囲であれば制限されないが、使用感を良好にする観点から、好ましくはpH3.5〜9、より好ましくは4〜8、更に好ましくは4.5〜7である。
[PH]
The pH of the oral composition of the present invention is appropriately set depending on the types of the components (A) and (B), the types and contents of other compounding components, the lumber form, the method of use, etc. It is not limited as long as it is within the allowable range, but it is preferably pH 3.5 to 9, more preferably 4 to 8, and still more preferably 4.5 to 7 from the viewpoint of improving the feeling of use.
[用途]
本発明の口腔用組成物は、歯周組織などの口腔内の組織と接触して密着し、残存することで、口腔内の組織に薬理成分などを持続的に作用させることができる。そのため、歯肉炎や歯槽膿漏などの歯周病の改善又は予防、むし歯や知覚過敏などの歯の疾患の改善又は予防、口腔内の組織の状態の改善などに用いることができるが、歯周病の改善又は予防に用いられることが好ましい。
[Use]
The oral composition of the present invention can be brought into contact with and closely adhere to the tissues in the oral cavity such as periodontal tissue and remain, so that the pharmacological component and the like can be continuously acted on the tissues in the oral cavity. Therefore, it can be used to improve or prevent periodontal diseases such as gingivitis and alveolar pyorrhea, to improve or prevent tooth diseases such as caries and hyperesthesia, and to improve the condition of tissues in the oral cavity. It is preferably used for amelioration or prevention of diseases.
本発明の口腔用組成物は、研磨剤を含まない態様とすることもできる。その場合は、口腔組織との間に発生する摩擦を低減させる作用が期待できる。より具体的には、歯ブラシ等に本実施形態にかかる組成物を塗布して、歯茎をブラッシングした際に歯茎と歯ブラシの間等で発生する摩擦を低減させることができ、そのため、歯茎等の口腔組織を傷つけずにブラッシングすることが可能となるため、上記の用途にとって好ましい。 The composition for oral cavity of the present invention may be in a mode not containing an abrasive. In that case, an effect of reducing friction generated between the oral tissues can be expected. More specifically, by applying the composition according to the present embodiment to a toothbrush or the like, it is possible to reduce the friction generated between the gum and the toothbrush when brushing the gum, and therefore, the oral cavity such as gums. It is preferable for the above-mentioned applications because it allows brushing without damaging the tissue.
歯周病は、その病状の進行によって、大きく歯茎炎(歯肉炎)と歯槽膿漏(歯周炎)の2つに分けられる。本発明の口腔用組成物は、これらいずれの改善又は予防にも用いることができる。 Periodontal disease is broadly divided into two types depending on the progress of the condition: gum inflammation (gingivitis) and alveolar pyorrhea (periodontitis). The oral composition of the present invention can be used for improving or preventing any of these.
本明細書において、口腔内の組織と密着する、とは、口腔内の組織に付着してとどまることを指す。そのため、「密着」若しくは「密着性」は、「滞留」若しくは「滞留性」、又は「付着」若しくは「付着性」と置き換えて解釈することができる。 In the present specification, “adhering to the tissue in the oral cavity” means that the tissue adheres to the tissue in the oral cavity and stays there. Therefore, “adhesion” or “adhesion” can be interpreted by replacing “adhesion” or “adhesion” or “adhesion” or “adhesion”.
本明細書において「予防」とは、疾病若しくは症状の発症の防止若しくは遅延、又は疾病若しくは症状の発症の危険性を低下させることをいう。 As used herein, the term "prevention" refers to preventing or delaying the onset of a disease or symptom, or reducing the risk of developing a disease or symptom.
また、本明細書において「改善」とは、疾病、症状若しくは健康状態の好転若しくは緩和、疾患、症状若しくは健康状態の悪化の防止若しくは遅延、又は疾患若しくは症状の進行の逆転、防止若しくは遅延をいう。 Further, in the present specification, “improvement” means improvement or alleviation of a disease, symptom or health condition, prevention or delay of deterioration of disease, symptom or health condition, or reversal, prevention or delay of progression of disease or symptom. ..
[剤形]
本発明の口腔用組成物の性状は、医薬品、医薬部外品、化粧品として公知の形態であれば、特に限定されず、液体状、流動状、又は半固形状とすることができる。また製剤形態としては、例えば、ペースト剤、クリーム剤、液剤、乳剤、軟膏剤、ゲル剤、懸濁剤、乳液、ローション剤等の製剤とすることができる。中でも、ペースト剤、クリーム剤、液剤、乳剤、又は軟膏剤がより好適であり、ペースト剤又はクリーム剤がさらにより好適であり、クリーム剤が特に好適である。なお、ペースト剤、クリーム剤、液剤、乳剤、軟膏剤等が、油性基剤と水性基剤とを含む場合は、O/W型でもW/O型でもよい。但し、本発明の効果をより顕著に奏する観点から、好ましくはO/W型エマルジョンである。
[Dosage form]
The property of the composition for oral cavity of the present invention is not particularly limited as long as it is a form known as a drug, a quasi drug, or a cosmetic, and may be liquid, fluid, or semisolid. In addition, the formulation form may be, for example, a paste, cream, liquid, emulsion, ointment, gel, suspension, emulsion, lotion or the like. Among them, pastes, creams, solutions, emulsions or ointments are more preferable, pastes or creams are even more preferable, and creams are particularly preferable. When the paste, cream, liquid, emulsion, ointment, etc. contain an oily base and an aqueous base, they may be of O/W type or W/O type. However, an O/W type emulsion is preferable from the viewpoint of more remarkably exerting the effect of the present invention.
本発明の口腔用組成物の形態は医薬品、医薬部外品、化粧品、又は食品として公知の形態であれば、特に限定されないが、例えば、歯磨剤、塗布剤、含嗽剤、歯茎に適用する美容液、洗口剤などに用いることができる。中でも、口腔内の組織にまんべんなく行きわたらせ、薬効成分や栄養成分を組織に持続的に接触・浸透させる観点から、歯磨剤、塗布剤、又は含嗽剤が好ましく、歯磨剤であることがさらに好ましい。 The form of the composition for oral cavity of the present invention is not particularly limited as long as it is a form known as a drug, quasi drug, cosmetic, or food, for example, a dentifrice, a coating agent, a mouthwash, and a beauty applied to gums. It can be used as a liquid, a mouthwash, etc. Among them, dentifrices, coating agents, and gargles are preferable, and dentifrices are more preferable, from the viewpoint of evenly spreading to tissues in the oral cavity and continuously contacting and penetrating medicinal components and nutritional components into tissues.
[製造方法]
本発明の口腔用組成物は、公知の方法により製造することができる。必要に応じて、滅菌工程を含めることができる。
[Production method]
The composition for oral cavity of the present invention can be produced by a known method. A sterilization step can be included if desired.
[歯茎への密着性を増強する方法]
本発明の歯茎への密着性を増強する方法とは、以下の方法である。
(A)脂肪酸デキストリン、(B)高分子化合物及び/又は研磨剤、並びに、(C)水、を含有させる工程を含む、口腔用組成物の歯茎への密着性を増強する方法。
[Method of enhancing adhesion to gums]
The method of enhancing the adhesion to the gums of the present invention is the following method.
A method for enhancing the adhesion of an oral composition to the gums, which comprises the step of containing (A) a fatty acid dextrin, (B) a polymer compound and/or an abrasive, and (C) water.
当該方法における、(A)成分、(B)成分及び(C)成分の種類及び含有量等、その他の成分の種類及び含有量等、口腔用組成物の製剤形態及び用途等については、[口腔用組成物]で説明したとおりである。 Regarding the formulation form and use of the oral composition, such as the types and contents of the components (A), (B) and (C), the types and contents of other components in the method, refer to [oral cavity Composition for use].
次に、実施例や試験例により本発明を具体的に説明するが、本発明は以下の実施例や試験例に限定されるものではない。 Next, the present invention will be specifically described with reference to Examples and Test Examples, but the present invention is not limited to the following Examples and Test Examples.
[試験例1.密着力試験]
下記表1に示す組成の歯磨剤を、常法により調製し、これらを用いて、密着力を評価した。
表1に示される歯磨剤(比較例1−1、1−2、実施例1−1、1−2)を調製した。
次いで、200mLビーカーに精製水200mL、直径3cmの十字型撹拌子を入れ、スライドガラス(長辺7.6cm、幅2.6cm)の中央に0.2gの製剤を、厚さ約1.4mmで塗布し、このビーカーに、製剤塗布面が下向きになるように立て掛けて浸した。このとき、塗布部は、撹拌子の約1.5cm上部に設置される。
スターラー(KPI、MIGHTY STIRRER、HE・16GX6)のツマミを5に合わせ、塗布した製剤が、全てスライドガラスから浮上するまでの時間(付着時間)(秒)を測定した。なお、電源は100V交流、周波数60Hzを使用した。
次に、下記式にて、対応する比較例に対する各実施例の付着力向上率(%)を算出した。なお、実施例1−1に対応する比較例は比較例1−1、実施例1−2に対応する比較例は比較例1−2である。
<付着率向上率(%)>
付着力向上率(%)
=(実施例の付着時間−対応する比較例の付着時間)/対応する比較例の付着時間×100
算出された付着力向上率(%)の値を基に、下記の基準で評価した。
0%未満 :×
1%以上10%未満 :△
10%以上〜20%未満 :〇
20%以上 :◎
[Test Example 1. Adhesion test]
Dentifrice having the composition shown in Table 1 below was prepared by a conventional method, and the adhesive strength was evaluated using these.
The dentifrices shown in Table 1 (Comparative Examples 1-1 and 1-2, Examples 1-1 and 1-2) were prepared.
Next, put 200 mL of purified water and a cross-shaped stirrer with a diameter of 3 cm into a 200 mL beaker, and place 0.2 g of the preparation in the center of a slide glass (long side 7.6 cm, width 2.6 cm) with a thickness of about 1.4 mm. The solution was applied, and the beaker was dipped in such a manner that the preparation application surface was faced downward. At this time, the coating unit is installed about 1.5 cm above the stirring bar.
The knob of a stirrer (KPI, MIGHTY STIRRR, HE16GX6) was adjusted to 5, and the time (adhesion time) (second) until all the applied preparations floated up from the slide glass was measured. The power source used was 100 V AC and a frequency of 60 Hz.
Next, the adhesion improvement rate (%) of each example with respect to the corresponding comparative example was calculated by the following formula. The comparative example corresponding to Example 1-1 is Comparative Example 1-1, and the comparative example corresponding to Example 1-2 is Comparative Example 1-2.
<Adhesion rate improvement rate (%)>
Adhesion improvement rate (%)
=(Adhesion time of Example-Adhesion time of corresponding Comparative Example)/Adhesion time of corresponding Comparative Example x 100
Based on the calculated value of the adhesive force improvement rate (%), the evaluation was made according to the following criteria.
Less than 0%: ×
1% or more and less than 10%: △
10% or more and less than 20%: 〇 20% or more: ◎
表1のように、カルボキシビニルポリマー及び精製水を含有する比較例1−1、アルギン酸ナトリウム及び精製水を含有する比較例1−2に対して、更にパルミチン酸デキストリンを含有する実施例1−1、実施例1−2では、顕著に付着率が向上していることが確認された。 As shown in Table 1, as compared with Comparative Example 1-1 containing a carboxyvinyl polymer and purified water and Comparative Example 1-2 containing sodium alginate and purified water, Example 1-1 further containing dextrin palmitate. In Example 1-2, it was confirmed that the adhesion rate was remarkably improved.
また、スターラーのツマミを10に合わせる以外は上記と同じ方法を用いて比較例1−1、2に対する実施例1−1、2の付着力向上率をそれぞれ求めた。その結果、実施例1−1及び実施例1−2の付着力向上率はともに10%以上であった。 Further, the adhesive force improvement rates of Examples 1-1 and 2 with respect to Comparative Examples 1-1 and 2 were obtained using the same method as described above except that the stirrer knob was set to 10. As a result, the adhesive force improvement rates of Example 1-1 and Example 1-2 were both 10% or more.
パルミチン酸デキストリンは、脂溶性成分のゲル化剤であるため、W/O系組成物に用いられるが、O/W系組成物には通常用いられない。しかし、実施例1−1及び1−2の組成物は、付着率の向上と合わせて、チューブからの押し出し、使用時の製剤の切れ、及び歯磨き時の使用感等においても優れた性質を有していた。 Since dextrin palmitate is a gelling agent for fat-soluble components, it is used in W/O-based compositions, but it is not usually used in O/W-based compositions. However, the compositions of Examples 1-1 and 1-2 have excellent properties in terms of extruding from a tube, breakage of the preparation at the time of use, feeling of use at the time of brushing teeth, etc., together with the improvement of the adhesion rate. Was.
[試験例2.使用感試験(1)]
上記試験例1の表1に示す組成の歯磨剤を、常法により調製し、これらを用いて、使用感を評価した。
表1に示される歯磨剤(比較例1−1、実施例1−1)を調製した。
歯磨剤開発者を含む3名のパネラーに、各歯磨剤を0.5gずつ歯ブラシに乗せ、歯を磨いてもらい、磨き始めから1分経過後に感じる、歯茎への密着感、及び不快な酸味の程度について、下記の基準に基づいて評価させた。
結果を表2に示す。
<歯茎への密着感 評価基準>
強い密着感を感じる :5
密着感を感じる :4
やや密着感を感じる :3
殆ど密着感を感じない :2
全く密着感を感じない :1
<不快な酸味 評価基準>
耐え難いほど不快な酸味を感じる :5
強く不快な酸味を感じる :4
はっきりと認識できる程度に不快な酸味を感じる :3
わずかに不快な酸味を感じる :2
殆ど不快な酸味を感じない :1
[Test Example 2. Usability test (1)]
A dentifrice having the composition shown in Table 1 of Test Example 1 was prepared by a conventional method, and the feeling of use was evaluated using these.
The dentifrices shown in Table 1 (Comparative Example 1-1, Example 1-1) were prepared.
To the three panelists including the dentifrice developer, put 0.5g of each dentifrice on the toothbrush and have them brush their teeth. Feel the adhesiveness on the gums and the unpleasant acidity after 1 minute from the start of brushing. The degree was evaluated based on the following criteria.
The results are shown in Table 2.
<Evaluation criteria for adhesion to gums>
Feel a strong feeling of contact: 5
Feeling close contact: 4
Feel a little close to each other: 3
Almost no feeling of contact :2
I don't feel any contact :1
<Unpleasant sourness evaluation criteria>
Feeling unbearably sour: 5
Feel a strong and unpleasant acidity: 4
Feels unpleasantly sour to the extent that it can be clearly recognized: 3
Slightly unpleasant sourness: 2
Almost no unpleasant sourness: 1
実施例1−1では、比較例1−1に比べて明らかに、歯茎への密着力の向上を実感することができた。また、比較例1−1では、不快な酸味が感じられたが、(B)成分に加えて(A)成分としてパルミチン酸デキストリンを含有する実施例2では、不快な酸味が感じられず、快適に使用することができた。 In Example 1-1, it was possible to clearly feel an improvement in the adhesive force to the gums as compared with Comparative Example 1-1. Further, in Comparative Example 1-1, an unpleasant sourness was felt, but in Example 2 containing the dextrin palmitate as the (A) component in addition to the (B) component, the unpleasant sourness was not felt, and it was comfortable. Could be used for.
[試験例3.使用感試験(2)]
下記表3に示す組成の歯磨剤を、常法により調製し、これらを用いて、使用感を評価した。
表3に示される歯磨剤(比較例2、実施例2)を調製した。
歯磨剤開発者を含む3名のパネラーに、各歯磨剤を0.5gずつ歯ブラシに乗せ、歯を磨いてもらい、磨き始めから1分経過後に感じる、歯茎への密着感、及び不快な酸味の程度について、いずれの歯磨剤を使用したときに、より感じたかを評価させた。
結果を表4に示す。
[Test Example 3. Usability test (2)]
Dentifrice having the composition shown in Table 3 below was prepared by a conventional method, and the feeling of use was evaluated using these.
The dentifrices shown in Table 3 (Comparative Example 2, Example 2) were prepared.
To the three panelists including the dentifrice developer, put 0.5g of each dentifrice on the toothbrush and have them brush their teeth. Feel the adhesiveness on the gums and the unpleasant acidity after 1 minute from the start of brushing. Regarding the degree, it was evaluated which dentifrice was more felt when used.
The results are shown in Table 4.
実施例2のように、表1の処方例に替えて、カルボキシビニルポリマー等、各成分の濃度を変更した場合にも、パルミチン酸デキストリンを含有しない場合と比較して、歯茎への密着感向上効果、不快な酸味の抑制効果が得られることが確認された。また、比較例2に比ベ、実施例2の方が、使用時に感じる刺激が低減している傾向が得られた。 As in Example 2, even when the concentration of each component such as carboxyvinyl polymer was changed in place of the formulation example of Table 1, the feeling of adhesion to the gums was improved as compared with the case where dextrin palmitate was not contained. It was confirmed that the effect and the effect of suppressing unpleasant sourness were obtained. Further, in comparison with Comparative Example 2, in Example 2, there was a tendency that the irritation felt during use was reduced.
従って、試験例2及び3から、(B)成分として高分子化合物を含む場合には、(A)成分であるパルミチン酸デキストリンを組み合わせることによって、歯茎への密着感を向上させるとともに、不快な酸味を抑制する効果が奏されることが明らかとなった。 Therefore, from Test Examples 2 and 3, when the high molecular compound was contained as the component (B), by combining the dextrin palmitate as the component (A), the feeling of adhesion to the gums was improved and unpleasant sourness It was revealed that the effect of suppressing
[製剤例]
以下、本発明に係る口腔組成物を用いたいくつかの製剤例について説明する。以下の製剤例は、次に記載する処方において常法により調製することができる。各成分の含有量の単位は全てw/w%である。
[Example of formulation]
Hereinafter, some formulation examples using the oral composition according to the present invention will be described. The following formulation examples can be prepared by a conventional method in the formulation described below. The unit of the content of each component is all w/w%.
(製剤例1)歯磨剤
アラントイン 0.1
トコフェロール酢酸エステル 0.04
セチルピリジニウム塩化物水和物 0.02
グリチルリチン酸二カリウム 0.2
ハッカ油 0.3
ユリエキス 0.1
加水分解コンキオリン液 0.1
流動パラフィン 10
白色ワセリン 1
パルミチン酸デキストリン 0.5
モノステアリン酸ソルビタン 1.5
カルボキシビニルポリマー 1.1
プルラン 0.1
ポリソルベート60 1.5
ラウリル硫酸Na 1
濃グリセリン 5
パラベン 0.1
香料 0.2
L−アルギニン 適量
精製水 残量
全量 100
(Formulation Example 1) Dentifrice Allantoin 0.1
Tocopherol acetate 0.04
Cetylpyridinium chloride hydrate 0.02
Dipotassium glycyrrhizinate 0.2
Mint oil 0.3
Lily extract 0.1
Hydrolyzed conchiolin solution 0.1
Liquid paraffin 10
White vaseline 1
Dextrin palmitate 0.5
Sorbitan monostearate 1.5
Carboxyvinyl polymer 1.1
Pullulan 0.1
Polysorbate 60 1.5
Lauryl sulfate Na 1
Concentrated glycerin 5
Paraben 0.1
Fragrance 0.2
L-Arginine Suitable amount
Purified water Total remaining amount 100
(製剤例2)歯磨剤
トコフェロール酢酸エステル 0.04
イソプロピルメチルフェノール 0.05
ヒノキチオール 0.1
硝酸カリウム 5
塩化ナトリウム 5
ハッカ油 1
ユリエキス 0.05
流動パラフィン 6
パルミチン酸デキストリン 0.5
モノステアリン酸グリセリン 1.5
カルボキシビニルポリマー 0.5
アルギン酸ナトリウム 0.5
ポリオキシエチレンセチルエーテル 1.5
ラウロイルメチルタウリンNa 1
プロピレングリコール 5
フェノキシエタノール 0.3
香料 0.1
L−アルギニン 適量
精製水 残量
全量 100
(Formulation Example 2) Dentifrice Tocopherol Acetate 0.04
Isopropyl methylphenol 0.05
Hinokitiol 0.1
Potassium nitrate 5
Sodium chloride 5
Peppermint oil 1
Lily extract 0.05
Liquid paraffin 6
Dextrin palmitate 0.5
Glycerin monostearate 1.5
Carboxy vinyl polymer 0.5
Sodium alginate 0.5
Polyoxyethylene cetyl ether 1.5
Lauroyl methyl taurine Na 1
Propylene glycol 5
Phenoxyethanol 0.3
Perfume 0.1
L-Arginine Suitable amount
Purified water Total remaining amount 100
(製剤例3)歯磨剤
塩化ベンザルコニウム 0.01
モノフルオロリン酸ナトリウム 0.07
ラウロイルサルコシンNa 0.2
ポリエチレングリコールa 5
メントール 0.3
加水分解コンキオリン液 1
流動パラフィン 5
白色ワセリン 0.1
パルミチン酸デキストリン 0.5
モノステアリン酸ソルビタン 1.5
リン酸水素カルシウム 10
ポリオキシエチレン硬化ヒマシ油 1.5
2−アルキル−N−カルボキシメチル−
N−ヒドロキシエチルイミダゾリニウムベタイン 1
1,3−ブチレングリコール 5
フェノキシエタノール 0.5
香料 0.05
L−アルギニン 適量
精製水 残量
全量 100
(Formulation Example 3) Dentifrice benzalkonium chloride 0.01
Sodium monofluorophosphate 0.07
Lauroyl sarcosine Na 0.2
Polyethylene glycol a 5
Menthol 0.3
Hydrolyzed conchiolin liquid 1
Liquid paraffin 5
White petrolatum 0.1
Dextrin palmitate 0.5
Sorbitan monostearate 1.5
Calcium hydrogen phosphate 10
Polyoxyethylene hydrogenated castor oil 1.5
2-alkyl-N-carboxymethyl-
N-hydroxyethyl imidazolinium betaine 1
1,3-butylene glycol 5
Phenoxyethanol 0.5
Fragrance 0.05
L-Arginine Suitable amount
Purified water Total remaining amount 100
Claims (12)
A method for enhancing the adhesion of an oral composition to the gums, which comprises the step of containing (A) a fatty acid dextrin, (B) a polymer compound and/or an abrasive, and (C) water.
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