JP2019069927A - Oral composition - Google Patents
Oral composition Download PDFInfo
- Publication number
- JP2019069927A JP2019069927A JP2017198055A JP2017198055A JP2019069927A JP 2019069927 A JP2019069927 A JP 2019069927A JP 2017198055 A JP2017198055 A JP 2017198055A JP 2017198055 A JP2017198055 A JP 2017198055A JP 2019069927 A JP2019069927 A JP 2019069927A
- Authority
- JP
- Japan
- Prior art keywords
- composition
- hinokitiol
- component
- discoloration
- 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.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 90
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- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 claims abstract description 51
- 125000002525 phosphocholine group Chemical group OP(=O)(OCC[N+](C)(C)C)O* 0.000 claims abstract description 44
- TUFYVOCKVJOUIR-UHFFFAOYSA-N alpha-Thujaplicin Natural products CC(C)C=1C=CC=CC(=O)C=1O TUFYVOCKVJOUIR-UHFFFAOYSA-N 0.000 claims abstract description 39
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- 229950004354 phosphorylcholine Drugs 0.000 description 3
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Abstract
Description
本発明は、ヒノキチオールと、アラントイン及び/又はその誘導体(以下、「アラントイン類」と表記することもある)と、水とを含みながらも変色が抑制されている口腔用組成物に関する。 The present invention relates to an oral composition which is inhibited from discoloring while containing hinokitiol, allantoin and / or a derivative thereof (hereinafter sometimes referred to as "allantoins"), and water.
2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ブチル共重合体等のホスホコリン基含有重合体は、生体への親和性が高く、更に保湿性、口腔内への微生物の付着防止、歯肉炎の予防等の作用も報告されており、口腔用組成物において利用されている(例えば、特許文献1〜3参照)。 Phosphocholine group-containing polymers such as 2-methacryloyloxyethyl phosphorylcholine / butyl methacrylate copolymer have high affinity to living bodies, and further have effects such as moisture retention, prevention of adhesion of microorganisms to the oral cavity, prevention of gingivitis, etc. Have also been reported and used in oral compositions (see, for example, Patent Documents 1 to 3).
アラントイン類は、細胞の機能を活性化するとともに抗炎症作用、止血作用、殺菌作用、抗潰瘍作用等を有することが知られており、口腔用組成物に使用されている(例えば、特許文献4参照)。 Allantoins are known to activate cell functions and have anti-inflammatory, hemostatic, bactericidal, anti-ulcer effects and the like, and are used in oral compositions (for example, Patent Document 4) reference).
また、う蝕や歯周病の病原菌数を低下させるための殺菌剤が口腔用組成物に使用されている。口腔用組成物に使用される殺菌剤は種々知られているが、ヒノキチオールは、低毒性で幅広い抗菌スペクトルを示すため、口腔用組成物に広く使用されている。ヒノキチオールには、変色、含量減少といった不安定性の問題がある。ヒノキチオールの安定性を維持するために種々の提案がなされている。 In addition, a bactericidal agent for reducing the number of pathogens of caries and periodontal diseases is used in the composition for oral cavity. Although various bactericidal agents used in oral compositions are known, hinokitiol is widely used in oral compositions because it exhibits low toxicity and a broad antibacterial spectrum. Hinokitiol suffers from instability problems such as discoloration and content reduction. Various proposals have been made to maintain the stability of hinokitiol.
例えば、特許文献5では、ヒノキチオールを含有する口腔用組成物に対して、塩化ナトリウム等の水易溶性無機塩を配合することが記載されている。さらに良好な保存安定性を得る技術として、特許文献6では、ヒノキチオールを含有する口腔用組成物に対して、0.02〜1質量%のエデト酸塩と、0.2〜10重量%のエタノールと、エタノールに対し質量比で3〜200倍の水とを配合することが記載されている。しかしながら、特許文献6の製剤化技術では、処方に制約があるため、近年の多様化する液状口腔用組成物の処方に対応できないケースがある。そこで、口腔用組成物において、ヒノキチオールを安定化させる新たな製剤技術の開発が望まれている。 For example, Patent Document 5 describes that a water-soluble inorganic salt such as sodium chloride is blended with a composition for oral cavity containing hinokitiol. As a technique for obtaining even better storage stability, in Patent Document 6, 0.02 to 1% by mass of an edetate salt and 0.2 to 10% by weight of ethanol with respect to an oral composition containing hinokitiol And blending 3 to 200 times as much water as ethanol by mass ratio with ethanol is described. However, in the formulation technology of Patent Document 6, there are cases in which the formulation can not be adapted to the recent diversifying liquid oral composition formulations because the formulation is limited. Therefore, development of a new formulation technology for stabilizing hinokitiol in oral compositions is desired.
本発明者は、ヒノキチオールを含む口腔用組成物の製剤安定性について検討を行ったところ、ヒノキチオールをアラントイン類と共存させると、顕著な変色が生じるという新たな課題に直面した。つまり、ヒノキチオールとアラントインとを水中に含む口腔用組成物には、変色の問題という特有の課題が併存することが明らかとなった。 The present inventors examined formulation stability of an oral composition containing hinokitiol, and encountered a new problem that when hinokitiol coexists with allantoins, significant discoloration occurs. That is, it has become clear that the oral composition containing hinokitiol and allantoin in water has a unique problem of the problem of discoloration.
そこで本発明の目的は、ヒノキチオールとアラントイン類と水とを含みながらも、変色が抑制できる製剤化技術を提供することである。 Therefore, an object of the present invention is to provide a formulation technology that can suppress discoloration while containing hinokitiol, allantoins and water.
本発明者は、前記課題を解決すべく鋭意検討を行ったところ、口腔用組成物において、ヒノキチオール、アラントイン類、及び水と共に、ホスホコリン基含有重合体を含有する口腔用組成物は、変色が抑制できることを見出した。本発明は、かかる知見に基づいて更に検討を重ねることにより完成したものである。 The inventors of the present invention conducted intensive studies to solve the above-mentioned problems. As a result, in the composition for oral cavity, the composition for oral cavity containing phosphocholine group-containing polymer together with hinokitiol, allantoins and water suppresses discoloration. I found out what I could do. The present invention has been completed by further studies based on such findings.
即ち、本発明は、下記に掲げる態様の発明を提供する。
項1. (A)ヒノキチオールと、(B)アラントイン及びその誘導体よりなる群から選択される少なくとも1種と、(C)ホスホコリン基含有重合体と、(D)水と、を含有する口腔用組成物。
項2. 前記(C)成分が、2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ブチル共重合体である、項1又に記載の口腔用組成物。
項3. (A)ヒノキチオール、(B)アラントイン及びその誘導体よりなる群から選択される少なくとも1種及び(D)水を含有する口腔用組成物における変色を抑制するために使用される変色抑制剤であって、
(C)ホスホコリン基含有重合体を有効成分とする、変色抑制剤。
項4. (A)ヒノキチオール、(B)アラントイン及びその誘導体よりなる群から選択される少なくとも1種及び(D)水を含有する口腔用組成物における変色を抑制する方法であって、
口腔用組成物に、前記(A)成分と前記(B)成分と前記(D)成分と共に、(C)ホスホコリン基含有重合体を配合する、変色を抑制する方法。
That is, the present invention provides the invention of the aspects listed below.
Item 1. An oral composition comprising (A) hinokitiol, (B) at least one member selected from the group consisting of allantoin, and (C) a phosphocholine group-containing polymer, and (D) water.
Item 2. The composition for oral cavity as described in item 1 or 2 above, wherein the component (C) is a 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer.
Item 3. A discoloration inhibitor used to inhibit discoloration in an oral composition comprising (A) hinokitiol, (B) allantoin and at least one member selected from the group consisting of (D) water, ,
(C) A discoloration inhibitor comprising a phosphocholine group-containing polymer as an active ingredient.
Item 4. A method for suppressing discoloration in an oral composition comprising at least one member selected from the group consisting of (A) hinokitiol, (B) allantoin and derivatives thereof and (D) water,
A method for suppressing discoloration by incorporating a (C) phosphocholine group-containing polymer into the composition for oral cavity together with the (A) component, the (B) component and the (D) component.
本発明の口腔用組成物によれば、ヒノキチオールとアラントイン類と水とを含みながらも、変色が抑制でき、優れた製剤安定性を有しているので、保存中に良好な外観を維持でき、使用時にも良好な外観となることを可能とするとともに、ヒノキチオールによる効果の減弱を抑制することができる。 According to the composition for oral cavity of the present invention, while containing hinokitiol, allantoins and water, it is possible to suppress the color change and to have excellent formulation stability, so that a good appearance can be maintained during storage, While being able to become a favorable appearance also at the time of use, attenuation of the effect by hinokitiol can be suppressed.
1.口腔用組成物
本発明の口腔用組成物は、(A)ヒノキチオール(以下、(A)成分と表記することがある)と、(B)アラントイン及び/又はその誘導体(以下、(B)成分と表記することがある)と、(C)ホスホコリン基含有重合体(以下、(C)成分と表記することがある)と、(D)水(以下、(D)成分と表記することがある)とを含有することを特徴とする。以下、本発明の口腔用組成物について詳述する。
1. Oral Composition The oral composition of the present invention comprises (A) hinokitiol (hereinafter sometimes referred to as component (A)), (B) allantoin and / or a derivative thereof (hereinafter, component (B)) It may be described), (C) phosphocholine group-containing polymer (hereinafter, may be described as (C) component), (D) water (hereinafter, may be described as (D) component) And containing. Hereinafter, the composition for oral cavity of this invention is explained in full detail.
(A)ヒノキチオール
本発明の口腔用組成物は、(A)成分としてヒノキチオールを含有する。ヒノキチオールは、低毒性で幅広い抗菌スペクトルを示す殺菌作用を有することが知られている公知の薬剤である。
(A) Hinokitiol The composition for oral cavity of the present invention contains hinokitiol as the component (A). Hinokitiol is a known drug known to have low toxicity and bactericidal activity showing a broad antibacterial spectrum.
本発明において、ヒノキチオールは、天然物由来のものを使用してもよく、化学合成されたものを使用してもよい。また、本発明で使用されるヒノキチオールは、精製品又は粗精製品の別を問わず、例えば、樹木から得られたヒノキチオール含有精油を使用することもできる。 In the present invention, hinokitiol may be of natural origin or chemically synthesized. Moreover, the hinokitiol used by this invention can also use the hinokitiol containing essential oil obtained from the tree whether it is a purified product or a crudely purified product, for example.
本発明の口腔用組成物における(A)成分の含有量については、当該口腔用組成物の製剤形態や用途等に応じて適宜設定されるが、優れた殺菌作用を発揮させるという観点から、通常0.001〜0.5重量%、好ましくは0.005〜0.3重量%、より好ましくは0.01〜0.2重量%が挙げられる。 The content of the component (A) in the composition for oral cavity of the present invention is appropriately set according to the formulation form and application of the composition for oral cavity, but from the viewpoint of exhibiting excellent bactericidal action, 0.001 to 0.5% by weight, preferably 0.005 to 0.3% by weight, more preferably 0.01 to 0.2% by weight can be mentioned.
(B)アラントイン類
本発明の口腔用組成物は、(B)成分として、アラントイン及びその誘導体よりなる群から選択される少なくとも1種を含有する。
(B) Allantoin The composition for oral cavity of the present invention contains, as the component (B), at least one selected from the group consisting of allantoin and its derivative.
アラントインは、5−ウレイドヒダントインとも称される化合物であり、抗炎症作用、細胞賦活作用、止血作用、殺菌作用、抗潰瘍作用等を有することが知られている公知の薬剤である。 Allantoin is a compound also referred to as 5-ureidohydantoin, and is a known drug known to have anti-inflammatory action, cell activating action, hemostatic action, bactericidal action, anti-ulcer action and the like.
アラントインの誘導体としては、薬学的に許容できることを限度として特に制限されないが、具体的には、アラントインクロルヒドロキシアルミニウム、アラントインヒドロキシアルミニウム等が挙げられる。これらのアラントインの誘導体は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。 The derivative of allantoin is not particularly limited as long as it is pharmaceutically acceptable, and specific examples include allantoin chlorohydroxyaluminum, allantoin hydroxyaluminum and the like. These allantoin derivatives may be used alone or in combination of two or more.
本発明の口腔用組成物において、(B)成分として、アラントイン及びその誘導体の中から、1種を選択して使用してもよく、2種以上を組み合わせて使用してもよい。これらの(B)成分の中でも、優れた安定性を得る観点から、好ましくはアラントインが挙げられる。 In the composition for oral cavity of the present invention, as the component (B), one kind of allantoin and its derivative may be selected and used, or two or more kinds may be used in combination. Among these (B) components, allantoin is preferably mentioned from the viewpoint of obtaining excellent stability.
本発明の口腔用組成物において、(B)成分の含有量については、当該口腔用組成物に備えさせるべき薬効、当該口腔用組成物の製剤形態等に応じて適宜設定すればよいが、例えば、0.001〜2重量%、好ましくは0.005〜0.5重量%、更に好ましくは0.01〜0.3重量%が挙げられる。 In the composition for oral cavity of the present invention, the content of the component (B) may be appropriately set according to the medicinal effect to be prepared for the composition for oral cavity, the formulation form of the composition for oral cavity, etc. 0.001 to 2% by weight, preferably 0.005 to 0.5% by weight, and more preferably 0.01 to 0.3% by weight.
(C)ホスホコリン基含有重合体
本発明の口腔用組成物は、(C)成分として、ホスホコリン基含有重合体を含有する。ホスホコリン基含有重合体は、(A)成分及び(B)成分と共存させることで、変色を抑制することができる。
(C) Phosphocholine Group-Containing Polymer The composition for oral cavity of the present invention contains a phosphocholine group-containing polymer as the component (C). The phosphocholine group-containing polymer can suppress the color change by coexisting with the (A) component and the (B) component.
ホスホコリン基含有重合体とは、ホスホコリン基を含む単量体(以下、「ホスホコリン基含有単量体」と表記することがある)が重合したポリマーであり、保湿作用等を有する公知の成分である。 The phosphocholine group-containing polymer is a polymer obtained by polymerizing a monomer containing a phosphocholine group (hereinafter sometimes referred to as "phosphocholine group-containing monomer"), and is a known component having a moisturizing effect and the like. .
ホスホコリン基含有重合体において、ホスホコリン基含有単量体の種類については、特に制限されないが、例えば、ホスホコリン基とビニル基を有する単量体が挙げられる。ホスホコリン基含有単量体として、より具体的には、2−メタクリロイルオキシエチルホスホリルコリン、2−メタクリロイルオキシエチルホスホリルエタノールアミン等が挙げられる。ホスホコリン基含有重合体において、ホスホコリン基含有単量体は1種単独で含まれていてもよく、また2種以上組み合わされて含まれていてもよい。これらのホスホコリン基含有単量体の中でも、変色抑制効果をより一層向上させるという観点から、好ましくは2−メタクリロイルオキシエチルホスホリルコリンが挙げられる。 In the phosphocholine group-containing polymer, the type of the phosphocholine group-containing monomer is not particularly limited, and examples thereof include monomers having a phosphocholine group and a vinyl group. More specifically, examples of the phosphocholine group-containing monomer include 2-methacryloyloxyethyl phosphoryl choline and 2-methacryloyloxyethyl phosphoryl ethanolamine. In the phosphocholine group-containing polymer, the phosphocholine group-containing monomer may be contained singly or in combination of two or more. Among these phosphocholine group-containing monomers, 2-methacryloyloxyethyl phosphoryl choline is preferably mentioned from the viewpoint of further improving the color change suppressing effect.
本発明で使用されるホスホコリン基含有重合体は、1種のホスホコリン基含有単量体からなる単重合体であってもよく、また2種以上の単量体からなる共重合体であってもよい。 The phosphocholine group-containing polymer used in the present invention may be a homopolymer consisting of one kind of phosphocholine group-containing monomer, or a copolymer consisting of two or more kinds of monomers. Good.
ホスホコリン基含有重合体が共重合体である場合、2種以上のホスホコリン基含有単量体からなる共重合体であってもよく、また少なくとも1種のホスホコリン基含有単量体と少なくとも1種のホスホコリン基含有単量体以外の単量体からなる共重合体であってもよい。 When the phosphocholine group-containing polymer is a copolymer, it may be a copolymer composed of two or more types of phosphocholine group-containing monomers, and at least one type of a phosphocholine group-containing monomer and at least one type of monomer. The copolymer which consists of monomers other than a phosphocholine group containing monomer may be sufficient.
ホスホコリン基含有重合体に含まれるホスホコリン基含有単量体以外の単量体の種類については、薬学的に許容されるものであってホスホコリン基含有単量とラジカル重合可能であることを限度として特に制限されないが、例えば、ビニル基を有する単量体が挙げられる。ホスホコリン基含有単量体以外の単量体として、具体的には、メチル(メタ)アクリレート、エチル(メタ)アクリレート、ブチル(メタ)アクリレート、ラウリル(メタ)アクリレート、ステアリル(メタ)アクリレート、2−エチルヘキシル(メタ)アクリレート等のアルキル(メタ)アクリレート;ベンジル(メタ)アクリレート、フェノキシエチル(メタ)アクリレート、シクロヘキシル(メタ)アクリレート、ポリプロピレングリコールモノ(メタ)アクリレート、ポリテトラメチレングリコールモノ(メタ)アクリレート、ポリプロピレングリコールジ(メタ)アクリレート、ポリテトラメチレングリコールモノ(メタ)アクリレート、ポリプロピレングリコールポリエチレングリコールモノ(メタ)アクリレート、メタクリル酸ナトリウム、2−ヒドロキシ−3−メタクリロイルオキシプロピルトリメチルアンモニウム等が挙げられる。ホスホコリン基含有重合体において、ホスホコリン基含有単量体以外の単量体は1種単独で含まれていてもよく、また2種以上組み合わされて含まれていてもよい。これらのホスホコリン基含有単量体以外の単量体の中でも、保湿作用を有効に発揮させつつ変色抑制効果をより一層向上させるという観点から、好ましくはアルキル(メタ)アクリレート、2−ヒドロキシ−3−メタクリロイルオキシプロピルトリメチルアンモニウム、更に好ましくはアルキル基の炭素数が1〜18のアルキル(メタ)アクリレート、より好ましくはアルキル基の炭素数が3〜5のアルキル(メタ)アクリレート、特に好ましくはブチル(メタ)アクリレートが挙げられる。なお、本明細書において、「(メタ)アクリレート」とは、メタクリレート及び/又はアクリレートを示す。 The types of monomers other than the phosphocholine group-containing monomer contained in the phosphocholine group-containing polymer are pharmaceutically acceptable and particularly limited as far as they are radically polymerizable with a single amount of phosphocholine group-containing monomer. Although it does not restrict | limit, the monomer which has a vinyl group is mentioned, for example. As monomers other than the phosphocholine group-containing monomer, specifically, methyl (meth) acrylate, ethyl (meth) acrylate, butyl (meth) acrylate, lauryl (meth) acrylate, stearyl (meth) acrylate, 2- Alkyl (meth) acrylates such as ethyl hexyl (meth) acrylate; benzyl (meth) acrylate, phenoxyethyl (meth) acrylate, cyclohexyl (meth) acrylate, polypropylene glycol mono (meth) acrylate, polytetramethylene glycol mono (meth) acrylate, Polypropylene glycol di (meth) acrylate, polytetramethylene glycol mono (meth) acrylate, polypropylene glycol polyethylene glycol mono (meth) acrylate, methacryl Sodium 2-hydroxy-3-methacryloyloxy propyl trimethyl ammonium, and the like. In the phosphocholine group-containing polymer, monomers other than the phosphocholine group-containing monomer may be contained singly or in combination of two or more. Among monomers other than these phosphocholine group-containing monomers, alkyl (meth) acrylate, 2-hydroxy-3-, preferably from the viewpoint of further improving the color change suppressing effect while exhibiting the moisturizing action effectively. Methacryloyloxypropyltrimethylammonium, more preferably an alkyl (meth) acrylate having 1 to 18 carbon atoms, more preferably an alkyl (meth) acrylate having 3 to 5 carbon atoms of an alkyl group, particularly preferably butyl (meth) ) Acrylates. In the present specification, "(meth) acrylate" indicates methacrylate and / or acrylate.
本発明で使用されるホスホコリン基含有重合体として、具体的には、ポリメタクリロイルオキシエチルホスホリルコリン単重合体、2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ブチル共重合体(ポリクオタニウム−51)、2−メタクリロイルオキシエチレンホスホリルコリン・メタクリル酸ブチル・メタクリル酸ナトリウム共重合体(ポリクオタニウム−65)、2−メタクリロイルオキシエチルホスホリルコリン・2−ヒドロキシ−3−メタクリロイルオキシプロピルトリメチルアンモニウム共重合体(ポリクオタニウム−64)、2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ステアリル共重合体(ポリクオタニウム−61)等が挙げられる。なお、ホスホコリン基含有重合体に関する前記表記において、括弧内の名称は化粧品成分表示名称を示す。 Specific examples of the phosphocholine group-containing polymer used in the present invention include polymethacryloyloxyethyl phosphorylcholine homopolymer, 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer (polyquaternium-51), 2-methacryloyloxy Ethylene phosphorylcholine / butyl methacrylate / sodium methacrylate copolymer (polyquaternium-65), 2-methacryloyloxyethyl phosphorylcholine, 2-hydroxy-3-methacryloyloxypropyltrimethylammonium copolymer (polyquaternium-64), 2-methacryloyloxy Ethyl phosphoryl choline / stearyl methacrylate copolymer (polyquaternium-61) etc. are mentioned. In addition, in the said description regarding a phosphocholine group containing polymer, the name in parenthesis shows a cosmetic component display name.
本発明の口腔用組成物において、(C)成分として、1種のホスホコリン基含有重合体を使用してもよく、また2種以上のホスホコリン基含有重合体を組み合わせて使用してもよい。 In the composition for oral cavity of the present invention, as the component (C), one type of phosphocholine group-containing polymer may be used, or two or more types of phosphocholine group-containing polymers may be used in combination.
これらの(C)成分の中でも、保湿作用を有効に発揮させつつ変色抑制効果をより一層向上させるという観点から、好ましくは、2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ブチル共重合体、ポリメタクリロイルオキシエチルホスホリルコリン単重合体、2−メタクリロイルオキシエチルホスホリルコリン・2−ヒドロキシ−3−メタクリロイルオキシプロピルトリメチルアンモニウム共重合体;更に好ましくは、2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ブチル共重合体、2−メタクリロイルオキシエチルホスホリルコリン・2−ヒドロキシ−3−メタクリロイルオキシプロピルトリメチルアンモニウム共重合体;特に好ましくは、2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ブチル共重合体が挙げられる。 Among these (C) components, 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer and polymethacryloyloxyethyl are preferable, from the viewpoint of further improving the color change suppressing effect while exhibiting the moisturizing action effectively. Phosphoryl choline homopolymer, 2-methacryloyloxyethyl phosphorylcholine. 2-hydroxy-3-methacryloyloxypropyl trimethyl ammonium copolymer; more preferably 2-methacryloyloxyethyl phosphorylcholine butyl methacrylate copolymer, 2-methacryloyloxyethyl. Phosphorylcholine • 2-hydroxy-3-methacryloyloxypropyltrimethylammonium copolymer; particularly preferably 2-methacryloyloxyethyl phosphorylcholine • methacryl Butyl copolymer.
本発明の口腔用組成物において、(C)成分の含有量については、特に制限されないが、変色抑制効果をより一層向上させるという観点から、例えば、(C)成分の総量で0.05重量%以上、好ましくは0.05〜0.5重量%、更に好ましくは0.05〜0.3重量%、一層好ましくは0.05〜0.25重量%が挙げられる。 In the composition for the oral cavity of the present invention, the content of the component (C) is not particularly limited, but from the viewpoint of further improving the discoloration suppression effect, for example, 0.05% by weight in total of the component (C) Or more, preferably 0.05 to 0.5% by weight, more preferably 0.05 to 0.3% by weight, and still more preferably 0.05 to 0.25% by weight.
本発明の口腔用組成物において、(A)成分に対する(C)成分の比率については、(A)成分及び(B)成分の各含有量に応じて定まるが、変色抑制効果をより一層向上させるという観点から、例えば、(A)成分の1重量部当たり、(C)成分の総量が0.1重量部以上、好ましくは0.1〜500重量部、より好ましくは0.15〜60重量部、更に好ましくは0.25〜25重量部が挙げられる。 In the composition for the oral cavity of the present invention, the ratio of the component (C) to the component (A) is determined according to the content of each of the component (A) and the component (B), but the coloration suppressing effect is further improved. From the viewpoint of, for example, the total amount of the component (C) is 0.1 parts by weight or more, preferably 0.1 to 500 parts by weight, more preferably 0.15 to 60 parts by weight, per 1 part by weight of the component (A) More preferably, it is from 0.25 to 25 parts by weight.
(D)水
本発明の口腔用組成物は、基剤として水を含有する。前記の(A)成分及び(B)成分は、水との共存下で保存すると、変色を生じる傾向を示すが、本発明の口腔用組成物によれば、このような変色を効果的に抑制することができる。
(D) The oral composition of the water present invention contains water as a base. The components (A) and (B) tend to cause discoloration when stored in the presence of water, but according to the composition for oral cavity of the present invention, such discoloration is effectively suppressed. can do.
本発明の口腔用組成物において、(D)成分の含有量については、その製剤形態等に応じて適宜設定されるが、例えば、1〜95重量%、好ましくは3〜90重量%、更に好ましくは5〜85重量%が挙げられる。 In the composition for oral cavity of the present invention, the content of the component (D) is appropriately set according to the form of the formulation etc., but it is, for example, 1 to 95% by weight, preferably 3 to 90% by weight, more preferably Is 5 to 85% by weight.
その他の成分
本発明の口腔用組成物は、前述する成分以外に、本発明の効果を損なわない範囲で、口腔用組成物の製剤形態に応じて、当該技術分野で通常使用される成分を含有していてもよい。このような成分としては、例えば、防腐剤、殺菌剤、抗菌剤、消炎剤、研磨剤、グルコシルトランスフェラーゼ(GTase)阻害剤、プラーク抑制剤、知覚過敏抑制剤、歯石予防剤、歯質強化/再石灰化剤、抗ヒスタミン剤、局所麻酔剤、血行促進剤、増粘剤、湿潤剤、賦形剤、香料、甘味剤、清涼化剤、色素、消臭剤、界面活性剤、溶剤、pH調整剤等が挙げられる。
Other Components The composition for oral cavity of the present invention contains, in addition to the components described above, components generally used in the technical field according to the formulation form of the composition for oral cavity as long as the effects of the present invention are not impaired. It may be done. Such components include, for example, preservatives, bactericides, antibacterial agents, anti-inflammatory agents, abrasives, glucosyl transferase (GTase) inhibitors, plaque inhibitors, hypersensitivity inhibitors, anti-calculus agents, dentinaceous agent Mineralizer, antihistamine, local anesthetic, circulation enhancer, thickener, wetting agent, excipient, flavor, sweetener, refreshing agent, pigment, deodorant, surfactant, solvent, pH adjuster, etc. Can be mentioned.
防腐剤、殺菌剤、抗菌剤としては、上述の(A)成分を除く成分であればよく、例えば、安息香酸類、サリチル酸類、ソルビン酸類、パラベン類、塩化デカリニウム、塩化クロルヘキシジン、グルコン酸クロルヘキシジン、イソプロピルメチルフェノール、トリクロサン、塩化リゾチーム、塩酸クロルヘキシジン、ヨウ化カリウム等が挙げられる。 The preservative, bactericidal agent and antibacterial agent may be any component other than the above-mentioned component (A), for example, benzoic acids, salicylic acids, sorbic acids, parabens, decarinium chloride, chlorhexidine chloride, chlorhexidine gluconate, isopropyl Methylphenol, triclosan, lysozyme chloride, chlorhexidine hydrochloride, potassium iodide and the like can be mentioned.
消炎剤としては、上述の(B)成分を除く成分であればよく、例えば、グリチルリチン酸ジカリウム、グリチルレチン酸、グリチルリチン酸メチル、グリチルリチン酸ステアリル、グリチルレチン酸ピリドキシン、グリチルレチン酸ステアリル、グリチルレチン酸グリセリル、グリチルレチン酸モノグルクロニド、トラネキサム酸、イプシロンアミノカプロン酸、アズレン、塩化ナトリウム、ビタミン類等が挙げられる。 The anti-inflammatory agent may be any component other than the above-mentioned component (B), for example, dipotassium glycyrrhizinate, glycyrrhetinic acid, methyl glycyrrhizinate, stearyl glycyrrhizinate, pyridoxine glycyrrhetinate, stearyl glycyrrhetinate, glyceryl glycyrrhetinate, glycyrrhetinate Monoglucuronide, tranexamic acid, epsilon aminocaproic acid, azulene, sodium chloride, vitamins and the like can be mentioned.
研磨剤としては、例えば、無水ケイ酸、含水ケイ酸、酸化アルミニウム、水酸化アルミニウム、リン酸水素カルシウム、リン酸カルシウム、ピロリン酸カルシウム、炭酸カルシウム、結晶セルロース、ポリエチレン末、炭粒等が挙げられる。 Examples of the abrasive include anhydrous silicic acid, hydrous silicic acid, aluminum oxide, aluminum hydroxide, calcium hydrogen phosphate, calcium phosphate, calcium pyrophosphate, calcium carbonate, crystalline cellulose, polyethylene powder, carbon particles and the like.
GTase阻害剤としては、例えば、アカバナ科マツヨイグサ属植物の抽出物、ブドウ科ブドウ属植物の抽出物、デキストラナーゼ、ムタナーゼ、タステイン、タンニン類、エラグ酸、ポリフェノール、ウーロン茶抽出物、緑茶抽出物、センブリ、タイソウ、ウイキョウ、芍薬、ゲンチアナ、センソ、龍胆、黄連等が挙げられる。 As a GTase inhibitor, for example, an extract of a plant belonging to the genus Pinus vulgare L., an extract of Vitis vines, a dextranase, mutanase, tastein, tannins, ellagic acid, polyphenol, oolong tea extract, green tea extract, There are Semburi, Taisou, fennel, glaze, gentiana, senso, long-bowl, Huangren, etc.
プラーク抑制剤としては、例えばクエン酸亜鉛やグルコン酸等が挙げられる。 Examples of the plaque inhibitor include zinc citrate and gluconic acid.
知覚過敏抑制剤としては、例えば、硝酸カリウム、塩化ストロンチウム等が挙げられる。 Examples of the hypersensitivity suppressor include potassium nitrate, strontium chloride and the like.
歯石予防剤としては、例えば、ポリリン酸塩類、ゼオライト、エタンヒドロキシジホスフォネート等が挙げられる。 As an anti-calculus agent, for example, polyphosphates, zeolite, ethane hydroxy diphosphonate and the like can be mentioned.
歯質強化/再石灰化剤としては、例えば、フッ素、フッ化ナトリウム、フルオロリン酸ナトリウム、フッ化第一スズ等が挙げられる。 Examples of the tooth strengthening / remineralizing agent include fluorine, sodium fluoride, sodium fluorophosphate and stannous fluoride.
抗ヒスタミン剤としては、例えば、ジフェンヒドラミン、塩酸ジフェンヒドラミン等が挙げられる。 Examples of antihistamines include diphenhydramine, diphenhydramine hydrochloride and the like.
局所麻酔剤としては、例えば、プロカイン、テトラカイン、ブピパカイン、メピパカイン、クロロプロカイン、プロパラカイン、メプリルカイン又はこれらの塩、オルソカイン、オキセサゼイン、オキシポリエントキシデカン、ロートエキス、ペルカミンパーゼ、テシットデシチン等が挙げられる。 The local anesthetic includes, for example, procaine, tetracaine, bupipakine, mepipacain, chlorprocaine, proparacaine, meprilcain or salts thereof, orthokine, oxesazein, oxypolyentoxydecane, roto extract, percamine pase, tesitdectin and the like.
血行促進剤としては、例えば、ノニル酸ワニリルアミド、ニコチン酸ベンジルエステル、カプサイシン、トウガラシエキス等が挙げられる。 Examples of the blood circulation promoting agent include nonylic acid allirylamide, nicotinic acid benzyl ester, capsaicin, pepper extract and the like.
増粘剤としては、例えば、プルラン、プルラン誘導体、デンプン等の多糖類;ヒドロキシプロピルセルロース、ヒドロキシエチルセルロース、ヒドロキシプロピルメチルセルロース、ヒドロキシエチルメチルセルロース、カルボキシメチルセルロース、カルボキシメチルセルロース塩類(カルボキシメチルセルロースナトリウム、カルボキシメチルセルロースカリウム等)、メチルセルロース、エチルセルロース、ポリアクリル酸、ポリアクリル酸塩(ポリアクリル酸ナトリウム、アクリル酸・アクリル酸オクチルエステル共重合体等)、メタアクリル酸類の共重合体(メタアクリル酸とアクリル酸 n−ブチルの重合体、メタアクリル酸とメタアクリル酸メチルの重合体及びメタアクリル酸とアクリル酸エチルの重合体等)等のセルロース系高分子物質;カルボキシビニルポリマー、ポリエチレングリコール、ポリビニルアルコール、ポリビニルピロリドン等の合成高分子物質;レクチン、アルギン酸、アルギン酸塩(アルギン酸ナトリウム、アルギン酸カリウム、アルギン酸マグネシウム、アルギン酸プロピレングリコールエステル、アルギン酸トリエタノールアミン、アルギン酸トリイソプロパノールアミン、アルギン酸アンモニウム、アルギン酸ブチルアミン、アルギン酸ジアミルアミン等)、コンドロイチン硫酸ナトリウム、寒天、キトサン、カラギーナン等の天然系高分子物質;コラーゲン、ゼラチン等のアミノ酸系高分子物質;アラビアガム、カラヤガム、トラガカントガム、キサンタンガム、ローカストビーンガム、グアガム、タマリンドガム、ジェランガム等のゴム系高分子物質等が挙げられる。 As the thickener, for example, polysaccharides such as pullulan, pullulan derivatives, starch and the like; hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl methylcellulose, carboxymethyl cellulose, carboxymethyl cellulose salts (sodium carboxymethylcellulose, potassium carboxymethylcellulose etc.) , Methylcellulose, ethylcellulose, polyacrylic acid, polyacrylate (sodium polyacrylate, acrylic acid / acrylic acid octyl ester copolymer, etc.), methacrylic acid copolymers (methacrylic acid and n-butyl acrylate) Polymers, polymers of methacrylic acid and methyl methacrylate, polymers of methacrylic acid and ethyl acrylate, etc.) Polymeric substances; Synthetic polymeric substances such as carboxyvinyl polymer, polyethylene glycol, polyvinyl alcohol, polyvinyl pyrrolidone, etc .; Lectin, alginic acid, alginate (sodium alginate, potassium alginate, magnesium alginate, propylene glycol alginate, triethanolamine alginate, alginate Natural polymeric substances such as triisopropanolamine, ammonium alginate, butylamine alginic acid, diamylamine alginic acid sodium, chondroitin sulfate sodium, agar, chitosan, carrageenan, etc .; amino acid type polymeric substances such as collagen, gelatin; gum arabic, karaya gum, tragacanth gum, Xanthan gum, locust bean gum, guar gum, tamarind gum, gellan gum, etc. System polymer material, and the like.
湿潤剤としては、例えば、グリセリン、ソルビトール、エチレングリコール、プロピレングリコール、ポリエチレングリコール、ポリプロピレングリコール、キシリトール、マルチトール、ラクトール、エリスリトール等が挙げられる。 As the humectant, for example, glycerin, sorbitol, ethylene glycol, propylene glycol, polyethylene glycol, polypropylene glycol, xylitol, maltitol, lactol, erythritol and the like can be mentioned.
賦形剤としては、例えば、乳糖、白糖、マンニトール、デンプン、デキストリン、結晶セルロース、シリカ(軽質無水ケイ酸等)等が挙げられる。 Examples of the excipient include lactose, sucrose, mannitol, starch, dextrin, crystalline cellulose, silica (light anhydrous silicic acid etc.) and the like.
香料としては、例えば、天然香料(ウイキョウ油等)、合成香料、これらの調合香料等が挙げられる。 Examples of the fragrant include natural fragrant (such as fennel oil), synthetic fragrant, and blended fragrants thereof.
甘味剤としては、サッカリンナトリウム、ステビオサイド、ステビアエキス、アスパルテーム、キシリトール、水飴、蜂蜜、ソルビトール、マルチトール、マンニトール、エリスリトール、糖類(乳糖、白糖、果糖、ブドウ糖等)等が挙げられる。 As the sweetening agent, saccharin sodium, stevioside, stevia extract, aspartame, xylitol, starch syrup, honey, sorbitol, maltitol, mannitol, erythritol, saccharides (lactose, sucrose, fructose, glucose, etc.) and the like can be mentioned.
清涼化剤としては、例えば、メントール、エリスリトール、カンフル、ボルネオール、ゲラニオール、これらを含む精油等が挙げられる。 Examples of the refreshing agent include menthol, erythritol, camphor, borneol, geraniol, essential oils containing these, and the like.
色素としては、例えば、天然色素、合成色素、これらの混合物が挙げられる。 The dyes include, for example, natural dyes, synthetic dyes, and mixtures thereof.
消臭剤としては、例えば、塩化亜鉛、銅クロロフィリンナトリウム、コーヒー生豆抽出物、ゴボウパウダー、緑茶、焙煎米糠エキス等が挙げられる。 Examples of the deodorant include zinc chloride, sodium copper chlorophyllin, green coffee bean extract, burdock powder, green tea, roasted rice bran extract and the like.
界面活性剤としては、例えば、ポリオキシエチレンラウリルエーテル硫酸ナトリウム、ラウリル硫酸ナトリウム、ミリスチル硫酸ナトリウム、N−ラウロイルサルコシン酸ナトリウム、N−ミリストリルサルコシン酸ナトリウム、ドデシルベンゼンスルホン酸ナトリウム、水素添加ココナッツ脂肪酸モノグリセリドモノ硫酸ナトリウム、ラウリルスルホ酢酸ナトリウム、α−オレフィンスルホン酸ナトリウム、N−パルミトイルグルタルミン酸ナトリウム、N−メチル−N−アシルタウリンナトリウム等の陰イオン性界面活性剤;ポリオキシエチレン硬化ヒマシ油、ショ糖脂肪酸エステル、マルトース脂肪酸エステル、マルチトール脂肪酸エステル、ラクトール脂肪酸エステル、ソルビタン脂肪酸エステル、ポリオキシエチレンソルビタンモノステアレート、ポリオキシエチレン高級アルコールエーテル、ポリオキシエチレンポリオキシプロピレン共重合体、ポリオキシエチレンポリオキシプロピレン脂肪酸エステル、ポリグリセリン脂肪酸エステル等の非イオン性界面活性剤;ヤシ油脂肪酸アミドプロピルベタイン、ラウリルジメチルアミノ酢酸ベタイン、ラウリルジメチルアミンオキシド、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ウムベタイン、N−ラウリルジアミノエチルグリシン、N−ミリスチルジアミノエチルグリシン、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両性界面活性剤;塩化ラウリルトリメチルアンモニウム、塩化ステアリルトリメチルアンモニウム、塩化ベンゼトニウム、塩化ベンザルコニウム、塩化ステアリルジメチルベンジルアンモニウム等の陽イオン性界面活性剤が挙げられる。 As the surfactant, for example, sodium polyoxyethylene lauryl ether sulfate, sodium lauryl sulfate, sodium myristyl sulfate, sodium N-lauroyl sarcosinate, sodium N-myristryl sarcosinate, sodium dodecyl benzene sulfonate, hydrogenated coconut fatty acid monoglyceride Anionic surfactants such as sodium monosulfate, sodium lauryl sulfoacetate, sodium α-olefin sulfonate, sodium N-palmitoylglutarate, sodium N-methyl-N-acyl taurine, etc .; polyoxyethylene hydrogenated castor oil, Sugar fatty acid ester, maltose fatty acid ester, maltitol fatty acid ester, lactol fatty acid ester, sorbitan fatty acid ester, polyoxyethylene sorbitan mo Nonionic surfactants such as stearate, polyoxyethylene higher alcohol ether, polyoxyethylene polyoxypropylene copolymer, polyoxyethylene polyoxypropylene fatty acid ester, polyglycerin fatty acid ester; coconut oil fatty acid amidopropyl betaine, lauryl Dimethylaminoacetic acid betaine, lauryldimethylamine oxide, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolium betaine, N-lauryldiaminoethylglycine, N-myristyldiaminoethylglycine, N-alkyl-1-hydroxyethylimidazoline Amphoteric surfactants such as betaine sodium; lauryltrimethylammonium chloride, stearyltrimethylammonium chloride, benzethonium chloride, benzalkonium chloride , Cationic surfactants such as chloride stearyl dimethyl benzyl ammonium.
溶剤としては、例えば、エタノール、プロパノール、ブタノール、ペンタノール、ヘキサノール、イソプロパノール等の1価アルコール等が挙げられる。 Examples of the solvent include monohydric alcohols such as ethanol, propanol, butanol, pentanol, hexanol and isopropanol.
pH調整剤としては、例えば、酢酸、塩酸、硫酸、硝酸、クエン酸、リンゴ酸、乳酸、リン酸、安息香酸、水酸化ナトリウム、水酸化カリウム、酢酸ナトリウム、炭酸ナトリウム、クエン酸ナトリウム、クエン酸水素ナトリウム、乳酸ナトリウム、乳酸カルシウム、リン酸ナトリウム、リン酸水素ナトリウム、安息香酸ナトリウム等が挙げられる。 As a pH adjuster, for example, acetic acid, hydrochloric acid, sulfuric acid, nitric acid, citric acid, malic acid, lactic acid, phosphoric acid, benzoic acid, sodium hydroxide, potassium hydroxide, sodium acetate, sodium acetate, sodium carbonate, sodium citrate, citric acid Examples include sodium hydrogen, sodium lactate, calcium lactate, sodium phosphate, sodium hydrogen phosphate, sodium benzoate and the like.
本発明の口腔用組成物において、これらの成分を含有させる場合、その含有量については、当該技術分野で通常使用される範囲で適宜設定すればよい。 In the composition for oral cavity of the present invention, when these components are contained, the content thereof may be appropriately set in the range generally used in the relevant technical field.
pH
また、本発明の口腔用組成物のpHについては、口腔内への適用が許容される範囲で適宜設定すればよいが、例えば、4〜8、好ましくは5〜7.5、更に好ましくは6〜7が挙げられる。ここで、pHとは、25℃の温度条件下で測定される値である。
pH
In addition, the pH of the composition for oral cavity of the present invention may be appropriately set in the range in which application to the oral cavity is permitted, and for example, 4 to 8, preferably 5 to 7.5, and more preferably 6 -7 are mentioned. Here, pH is a value measured under a temperature condition of 25 ° C.
製剤形態
本発明の口腔用組成物の剤型については、口腔内への適用が可能であることを限度として特に制限されないが、例えば、液状又は半固形状(ゲル状、ペースト状)が挙げられる。
Dosage form The dosage form of the composition for oral cavity of the present invention is not particularly limited as far as it can be applied to the oral cavity, but includes, for example, liquid or semisolid (gel or paste). .
本発明の口腔用組成物の製剤形態については、口腔内に適用されて口腔内で一定時間滞留し得るものである限り特に制限されないが、例えば、液体歯磨剤、液状歯磨剤、練歯磨剤、洗口液(液体歯磨剤、洗口液は、一般にマウスリンス、マウスウォッシュ、デンタルリンス等と呼称されることがある)、口中清涼剤(マウススプレー等)、口腔用軟膏剤等の口腔衛生剤が挙げられる。これらの中でも、好ましくは液体歯磨剤、液状歯磨剤、練歯磨剤、洗口液、更に好ましくは液体歯磨剤、練歯磨剤、洗口液が挙げられる。 The preparation form of the oral composition of the present invention is not particularly limited as long as it can be applied in the oral cavity and can be retained in the oral cavity for a certain period of time, for example, liquid dentifrice, liquid dentifrice, toothpaste, Oral hygiene agents such as mouthwash (liquid dentifrice, mouthrinse may be generally referred to as mouthrinse, mouthwash, dental rinse etc.), mouth freshener (mouse spray etc), oral ointment etc Can be mentioned. Among these, preferred are liquid dentifrices, liquid dentifrices, toothpastes and mouthrinses, and more preferably liquid dentifrices, toothpastes and mouthrinses.
容器
本発明の口腔用組成物を充填する容器の材質としては特に限定されない。容器の材質の例としては、ガラス及び樹脂が挙げられる。樹脂の具体例としては、ポリプロピレンなどのポリオレフィン系樹脂、及びポリエチレンテレフタレート等のポリエステル系樹脂が挙げられる。変色抑制効果をより一層発揮させる観点からは、ポリオレフィン系樹脂が好ましく、ポリプロピレンがより好ましい。なお、容器が樹脂を含み、複層構造からなる積層体で構成される場合、上述の樹脂からなる樹脂層が容器の最内層となるように構成される。なお、上述の(C)成分を配合しない口腔用組成物は、ガラス容器の内壁に不溶性成分が吸着するが、本発明の口腔用組成物において(C)成分を配合することにより、ガラス製容器の内壁への不溶性成分の吸着も抑制することができる。
また、容器の形状としては特に限定されず、チューブ、ボトル等どのような形状であってもよい。
Container The material of the container filled with the composition for oral cavity of the present invention is not particularly limited. Examples of the material of the container include glass and resin. Specific examples of the resin include polyolefin resins such as polypropylene and polyester resins such as polyethylene terephthalate. From the viewpoint of further exhibiting the color change suppressing effect, polyolefin resins are preferable, and polypropylene is more preferable. In addition, when a container contains resin and it is comprised by the laminated body which consists of multilayer structures, it is comprised so that the resin layer which consists of the above-mentioned resin may become the innermost layer of a container. In addition, although the insoluble component adheres to the inner wall of a glass container, the composition for oral cavity which does not mix | blend the above-mentioned (C) component is a glass-made container by mix | blending (C) component in the composition for oral cavity of this invention It is also possible to suppress the adsorption of insoluble components on the inner wall of
Further, the shape of the container is not particularly limited, and any shape such as a tube or a bottle may be used.
2.変色抑制剤、及び変色を抑制する方法
前述するように、ホスホコリン基含有重合体は、ヒノキチオール、アラントイン類、及び水を含む口腔用組成物において、変色を抑制することができる。従って、本発明は、更に、ヒノキチオール、アラントイン類及び水を含む口腔用組成物における変色を抑制するために使用される変色抑制剤であって、ホスホコリン基含有重合体を有効成分とする変色抑制剤を提供する。また、本発明は、ヒノキチオール、アラントイン類、及び水を含む口腔用組成物において、変色を抑制する方法であって、口腔用組成物に、ヒノキチオール、アラントイン類、及び水と共に、ホスホコリン基含有重合体を配合する方法を提供する。
2. Discoloration inhibitors, and method for suppressing discoloration to above, phosphocholine group-containing polymer, hinokitiol, allantoin compounds, and in oral compositions comprising water, it is possible to suppress the discoloration. Therefore, the present invention is a discoloration inhibitor used to suppress discoloration in an oral composition containing hinokitiol, allantoins and water, which comprises a phosphocholine group-containing polymer as an active ingredient. I will provide a. Further, the present invention is a method for suppressing discoloration in an oral composition containing hinokitiol, allantoins, and water, wherein the oral composition includes a phosphocholine group-containing polymer together with hinokitiol, allantoins, and water. Provide a way to formulate
前記変色抑制剤はホスホコリン基含有重合体の添加剤としての用途であり、また、前記変色を抑制する方法は、ホスホコリン基含有重合体を利用して、ヒノキチオール、アラントイン類、及び水を含む口腔用組成物における変色を抑制する方法である。 The color change inhibitor is used as an additive for a phosphocholine group-containing polymer, and the method for suppressing the color change uses a phosphocholine group-containing polymer and is for oral cavity containing hinokitiol, allantoins, and water. It is a method of suppressing the discoloration in a composition.
前記変色抑制剤及び変色を抑制する方法において、使用する成分の種類や使用量、口腔用組成物の形態等については、前記「1.口腔用組成物」の欄に示す通りである。 In the color change inhibitor and the method for suppressing color change, the types and amounts of the components used, the form of the composition for oral cavity and the like are as described in the section of “1. Composition for oral cavity”.
以下に実施例を示して本発明をより具体的に説明するが、本発明はこれらに限定されるものではない。 EXAMPLES The present invention will be more specifically described below by way of Examples, but the present invention is not limited thereto.
試験例
表1に示す組成の液剤を調製した。具体的には、実施例においては、精製水にヒノキチオールを加えて撹拌し、溶解させた後、2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ブチル共重合体を添加して撹拌混合した。その後、アラントインを添加して撹拌し、溶解させた。すべての工程は80℃の加温条件にて行った。比較例及び参考例においては、2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ブチル共重合体、又はさらにアラントイン又はヒノキチオールを用いなかったことを除いて同様に液剤を得た。得られた液剤を、ガラス製のスクリュー管瓶(容量110mL)、ポリプロピレン(PP)製のボトル容器(容量100mL)、又はポリエチレンテレフタレート(PET)製のボトル容器(容量100mL)にそれぞれ50mL充填した。なお、全ての容器は透明タイプのものを使用した。各液剤について以下のとおり変色抑制性を評価した。
Test Example A solution of the composition shown in Table 1 was prepared. Specifically, in the examples, hinokitiol was added to purified water, stirred and dissolved, and then 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer was added and stirred and mixed. Then, allantoin was added and stirred to dissolve. All steps were performed at 80 ° C. heating conditions. In Comparative Examples and Reference Examples, solutions were similarly obtained except that 2-methacryloyloxyethyl phosphorylcholine / butyl methacrylate copolymer, or further allantoin or hinokitiol was not used. The resulting solution was filled 50 mL each in a glass screw tube bottle (volume 110 mL), a polypropylene (PP) bottle container (volume 100 mL), or a polyethylene terephthalate (PET) bottle container (volume 100 mL). In addition, all containers used the transparent type thing. The discoloration inhibition was evaluated for each solution as follows.
<変色抑制性>
充填した液剤を、遮光条件下、60℃で7日間保存した。その後、常温に戻し、以下に示す判定基準に従って変色抑制の程度を評価した。
××:製剤に極めて著しい変色が認められる。
×:製剤に著しい変色が認められる。
○:製剤に著しい変色が認められない。
◎:製剤にほとんど変色が認められない。
<Color change inhibition property>
The filled solution was stored at 60 ° C. for 7 days under light-shielded conditions. Thereafter, the temperature was returned to normal temperature, and the degree of discoloration inhibition was evaluated according to the judgment criteria shown below.
××: extremely remarkable discoloration is observed in the preparation.
×: Remarkable discoloration is observed in the preparation.
○: no significant discoloration was observed in the preparation.
◎: Almost no discoloration is observed in the preparation.
得られた結果を表1に示す。表1に示されるように、ヒノキチオール又はアラントインをそれぞれ単独で含む液剤(参考例1及び2)では変色は認められないが、ヒノキチオールとアラントインとの両方を含む液剤(比較例1及び2)では、著しい変色が認められた。特に、ポリプロピレン(PP)製の容器に充填させた液剤(比較例1及び2の「PP」)で、極めて著しい変色が認められた。これに対し、2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ブチル共重合体を配合した液剤(実施例1〜4)では、変色が飛躍的に抑制された。 The obtained results are shown in Table 1. As shown in Table 1, no discoloration was observed in the solutions containing hinokitiol or allantoin alone (Reference Examples 1 and 2), but in the solutions containing both Hinokitiol and Allantoin (Comparative Examples 1 and 2), Significant discoloration was observed. In particular, with the liquid agent ("PP" of Comparative Examples 1 and 2) filled in a container made of polypropylene (PP), extremely remarkable discoloration was observed. On the other hand, in the liquid preparation (Examples 1 to 4) in which 2-methacryloyloxyethyl phosphorylcholine / butyl methacrylate copolymer was blended, the color change was dramatically suppressed.
なお、表中には示していないが、変色抑制性の評価を行った液剤において、ヒノキチオールとアラントインとの両方を含み、ガラス製スクリュー管瓶に充填された液剤(比較例1及び2の「ガラス」)においては、液剤と接触するスクリュー管瓶の内壁に析出物が吸着することによる曇りが認められた。これに対し、2−メタクリロイルオキシエチルホスホリルコリン・メタクリル酸ブチル共重合体を配合した液剤(実施例1〜4の「ガラス」)では、析出物の吸着による曇りも認められなかった。 In addition, although not shown in the table, in the solution for which the discoloration inhibition evaluation was performed, the solution containing both hinokitiol and allantoin and filled in a glass screw tube (“glass in Comparative Example 1 and 2” In the case of ")", fogging due to the adsorption of the precipitate on the inner wall of the screw tube bottle in contact with the solution was observed. On the other hand, in the liquid agent ("glass" of Examples 1-4) which mix | blended 2-methacryloyl oxyethyl phosphoryl choline and the butyl methacrylate copolymer, the cloudiness by adsorption of a precipitate was not recognized, either.
製剤例1
表2及び表3に示す組成の口腔用組成物を調製した。なお、表中の各成分の含有量の単位は、重量%である。得られた表2の口腔用組成物を、ガラス製のスクリュー管瓶(容量110mL)、ポリプロピレン(PP)製のボトル容器(容量100mL)、又はポリエチレンテレフタレート(PET)製のボトル容器(容量100mL)にそれぞれ50mL充填し、得られた表3の口腔用組成物を、ガラス製のスクリュー管瓶(容量9mL)、ポリプロピレン(PP)製のラミネートチューブ、又はポリエチレンテレフタレート(PET)製のボトル容器(容量10mL)にそれぞれ5mL充填した。各製剤について、試験例1と同様に変色抑制性を評価した。得られた口腔用組成物はいずれも、変色が抑制されていた。
Formulation example 1
An oral composition having the composition shown in Table 2 and Table 3 was prepared. In addition, the unit of content of each component in a table | surface is weight%. The obtained composition for oral cavity of Table 2 was used as a glass screw tube bottle (volume 110 mL), a polypropylene (PP) bottle container (volume 100 mL), or a polyethylene terephthalate (PET) bottle container (volume 100 mL) The oral cavity composition of Table 3 obtained in each of the above was filled in 50 mL, the glass screw tube bottle (9 mL capacity), a laminated tube made of polypropylene (PP), or a bottle container made of polyethylene terephthalate (PET) (volume Each 10 mL) was filled with 5 mL. The color change inhibition was evaluated in the same manner as in Test Example 1 for each preparation. Discoloration was suppressed in any of the obtained oral compositions.
製剤例2
表4〜11に示す組成の口腔用組成物を製造した。なお、表中の各成分の含有量の単位は、重量%である。得られた口腔用組成物については、いずれも変色が抑制されていた。
Formulation example 2
The composition for oral cavity of the composition shown to Tables 4-11 was manufactured. In addition, the unit of content of each component in a table | surface is weight%. The color change was suppressed about the obtained composition for oral cavity.
Claims (4)
(C)ホスホコリン基含有重合体を有効成分とする、変色抑制剤。 A discoloration inhibitor used to inhibit discoloration in an oral composition comprising (A) hinokitiol, (B) allantoin and at least one member selected from the group consisting of (D) water, ,
(C) A discoloration inhibitor comprising a phosphocholine group-containing polymer as an active ingredient.
口腔用組成物に、前記(A)成分と前記(B)成分と前記(D)成分と共に、(C)ホスホコリン基含有重合体を配合する、変色を抑制する方法。 A method for suppressing discoloration in an oral composition comprising at least one member selected from the group consisting of (A) hinokitiol, (B) allantoin and derivatives thereof and (D) water,
A method for suppressing discoloration by incorporating a (C) phosphocholine group-containing polymer into the composition for oral cavity together with the (A) component, the (B) component and the (D) component.
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