JP6628839B2 - Astringent composition - Google Patents
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- JP6628839B2 JP6628839B2 JP2018123518A JP2018123518A JP6628839B2 JP 6628839 B2 JP6628839 B2 JP 6628839B2 JP 2018123518 A JP2018123518 A JP 2018123518A JP 2018123518 A JP2018123518 A JP 2018123518A JP 6628839 B2 JP6628839 B2 JP 6628839B2
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- 239000000203 mixture Substances 0.000 title claims description 85
- 239000000284 extract Substances 0.000 claims description 49
- 235000018553 tannin Nutrition 0.000 claims description 21
- 229920001864 tannin Polymers 0.000 claims description 21
- 239000001648 tannin Substances 0.000 claims description 21
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- 239000003814 drug Substances 0.000 description 9
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- DIZPMCHEQGEION-UHFFFAOYSA-H aluminium sulfate (anhydrous) Chemical compound [Al+3].[Al+3].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O DIZPMCHEQGEION-UHFFFAOYSA-H 0.000 description 1
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- Cosmetics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
本発明は、収斂用組成物に関する。より詳細には、本発明は、収斂剤の収斂作用を増強して発揮できる収斂用組成物に関する。 The present invention relates to astringent compositions. More specifically, the present invention relates to an astringent composition that can enhance and exert the astringent action of an astringent.
収斂剤には、皮膚や粘膜のタンパク質を一時的に変性、凝集させたり、浸透圧による脱水作用を発揮させたりすることにより、組織を引き締めて外界からの物理的又は化学的刺激に対する保護機能を高める作用があり、抗炎症、止血、制汗等の目的で口腔用組成物や皮膚外用組成物に配合されている。従来、収斂作用を有する成分について精力的に検討されており、収斂剤として利用可能な成分が種々報告されている（例えば、特許文献１及び２参照）。 Astringents have a protective function against physical or chemical stimuli from the outside by tightening tissues by temporarily denaturing and agglutinating proteins in the skin and mucous membranes and by exerting dehydration by osmotic pressure. It has an enhancing effect and is incorporated into oral compositions and skin external compositions for the purpose of anti-inflammatory, hemostatic, antiperspirant and the like. Conventionally, components having an astringent action have been energetically studied, and various components usable as astringents have been reported (for example, see Patent Documents 1 and 2).
一方、近年、消費者が訴求する薬理効果が多様化しており、より強い収斂作用を好む人がいる反面、緩やかな収斂作用を好む人もおり、収斂剤によって発揮される収斂作用に対する要望も多様化している。このような多様化する要望に追従するためにも、収斂剤の収斂作用を増強させる製剤技術の開発が求められている。 On the other hand, in recent years, the pharmacological effects appealed by consumers have diversified, and some people prefer stronger astringent effects, while others prefer moderate astringent effects, and the demand for astringent effects exerted by astringents is also diverse. Is becoming In order to follow such diversifying demands, there is a demand for the development of a formulation technique for enhancing the astringent action of an astringent.
通常、収斂剤によって発揮される収斂作用を増強させるには、収斂剤の配合量を増加させることによって実現し得るが、収斂剤の配合量の増加は、白濁や沈殿等を生じさせ製剤性状を不安定化させたり、また収斂剤自体が有する苦み、渋み、塩味等によって使用感が損なわれたりすることがある。特に、口腔用組成物の場合には、収斂剤の配合量の増加によってもたらされる呈味の低下は、使用感の著しい悪化を伴ってしまう。そのため、収斂剤の配合量を増加せずとも、収斂作用を増強して発揮可能な製剤技術の開発が望まれている。 Normally, the astringent effect exerted by the astringent can be enhanced by increasing the amount of the astringent. However, the increase in the amount of the astringent causes cloudiness or precipitation, etc. It may destabilize, or the feeling of use may be impaired by the bitterness, astringency, saltiness, etc. of the astringent itself. In particular, in the case of an oral composition, a decrease in taste brought about by an increase in the amount of the astringent is accompanied by a marked deterioration in feeling in use. Therefore, it is desired to develop a formulation technique capable of exhibiting enhanced astringent action without increasing the amount of the astringent.
しかしながら、従来、収斂剤の収斂作用の増強という観点からは、十分な検討がなされていないのが現状である。 However, at present, sufficient studies have not been made from the viewpoint of enhancing the astringent action of astringents.
本発明は、収斂剤を含有する収斂用組成物において、収斂剤の収斂作用を増強させる製剤技術を提供することを目的とする。 An object of the present invention is to provide a formulation technique for enhancing the astringent action of an astringent in an astringent composition containing the astringent.
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、(A)収斂剤と共に、(B)アセンヤクエキス及び／又はカキタンニンを併用した収斂用組成物は、収斂剤の収斂作用が相乗的に増強して発揮されることを見出した。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。 Means for Solving the Problems The present inventor has conducted intensive studies in order to solve the above-mentioned problems. As a result, the astringent composition comprising (A) an astringent extract and / or (A) acacia extract and / or oyster tannin together with the astringent has an astringent effect of the astringent. Was found to be synergistically enhanced. The present invention has been completed by further study based on such knowledge.
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)収斂剤、並びに(B)アセンヤクエキス及びカキタンニンよりなる群から選択される少なくとも１種を含有することを特徴とする、収斂用組成物。
項２． 前記(A)成分が、アラントイン誘導体、ウラジロガシエキス、シラカバエキス、
及び乳酸アルミニウムよりなる群から選択される少なくとも１種である、項１に記載の収斂用組成物。
項３． 前記(A)成分の総量１重量部当たり、前記(B)成分が総量で０．０００１〜１７０重量部含まれる、項１又は２に記載の収斂用組成物。
項４． 口腔用組成物である、項１〜３のいずれかに記載の収斂用組成物。
項５． アセンヤクエキス及びカキタンニンよりなる群から選択される少なくとも１種を有効成分とする、収斂作用増強剤。
項６． 収斂剤を含有する収斂用組成物に、アセンヤクエキス及びカキタンニンよりなる群から選択される少なくとも１種を配合する工程を含む、収斂作用の増強方法。
That is, the present invention provides the following aspects of the invention.
Item 1. An astringent composition comprising (A) an astringent, and (B) at least one selected from the group consisting of acacia extract and oyster tannin.
Item 2. The component (A) is an allantoin derivative, a vulgaris extract, a birch extract,
Item 2. The astringent composition according to Item 1, which is at least one selected from the group consisting of aluminum lactate.
Item 3. Item 3. The astringent composition according to Item 1 or 2, wherein the component (B) is contained in a total amount of 0.0001 to 170 parts by weight per 1 part by weight of the total amount of the component (A).
Item 4. Item 4. The astringent composition according to any one of Items 1 to 3, which is an oral composition.
Item 5. An astringent-enhancing agent comprising, as an active ingredient, at least one selected from the group consisting of Acacia catechu extract and persimmon tannin.
Item 6. A method for enhancing astringent action, comprising a step of blending at least one selected from the group consisting of acacia extract and oyster tannin with a composition for astringent containing an astringent.
本発明の収斂用組成物によれば、収斂剤によって発揮させる収斂作用を相乗的に増強できるので、口腔内や皮膚等の組織に対して優れた収斂効果を付与し、これらの組織の保護機能を格段に向上させることができる。また、本発明の収斂用組成物によれば、収斂剤の配合量を増大させずに収斂作用を増強できるので、収斂剤の配合量の増大によってもたらされる呈味低下を回避でき、口腔用組成物として使用しても、良好な使用感を得ることができる。 According to the composition for astringent of the present invention, since the astringent effect exerted by the astringent can be synergistically enhanced, an excellent astringent effect is imparted to tissues such as the oral cavity and skin, and the protective function of these tissues is provided. Can be significantly improved. Further, according to the astringent composition of the present invention, since the astringent action can be enhanced without increasing the amount of the astringent, the taste reduction caused by the increase in the amount of the astringent can be avoided, and the oral composition Even when used as a product, a good feeling of use can be obtained.
１．収斂用組成物
本発明の収斂用組成物は、収斂剤（以下、単に(A)成分と表記することもある）、並びに、アセンヤクエキス及びカキタンニンよりなる群から選択される少なくとも１種（以下、単に(B)成分と表記することもある）を含有することを特徴とする。以下、本発明の収斂用組成物について詳述する。
(A)成分
本発明の収斂用組成物は、収斂作用を発揮する成分として収斂剤を含有する。
1. Astringent composition The astringent composition of the present invention comprises an astringent (hereinafter sometimes simply referred to as the component (A)), and at least one selected from the group consisting of acacia extract and persimmon tannin ( Hereinafter, it may be simply referred to as the component (B)). Hereinafter, the astringent composition of the present invention will be described in detail.
(A) Component The astringent composition of the present invention contains an astringent as a component exhibiting an astringent action.
本発明で使用される収斂剤については、収斂作用を発揮でき、薬学的に許容されることを限度として特に制限されないが、後述する(B)成分による収斂作用の増強をより効果的に実現するという観点から、皮膚や粘膜のタンパク質を一時的に変性、凝集させる作用を発揮する収斂剤が好適に使用される。 The astringent used in the present invention can exert an astringent action, and is not particularly limited as long as it is pharmaceutically acceptable, but more effectively realizes the enhancement of the astringent action by the component (B) described below. From the viewpoint, an astringent which exerts an action of temporarily denaturing and coagulating proteins on the skin and mucous membranes is preferably used.
このような収斂剤としては、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、アラントインジヒドロキシアルミニウム等のアラントイン誘導体；シラカバエキス、ウラジロガシエキス等の植物エキス；乳酸アルミニウム、ミョウバン、塩化アルミニウム等のアルミニウム塩；塩化亜鉛、酸化亜鉛、パラフェノールスルホン酸亜鉛、硫酸亜鉛等の亜鉛塩；塩化ナトリウム等のナトリウム塩等が挙げられる。これらの収斂剤は、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。 Specific examples of such astringents include allantoin derivatives such as allantoinchlorohydroxyaluminum and allantoindihydroxyaluminum; plant extracts such as birch extract and vulgaris extract; aluminum salts such as aluminum lactate, alum and aluminum chloride; zinc chloride , Zinc oxide, zinc salts of paraphenolsulfonate, zinc sulfate and the like; sodium salts such as sodium chloride and the like. One of these astringents may be used alone, or two or more thereof may be used in combination.
収斂剤として使用される植物エキスについては、その抽出方法等については、日本薬局方外医薬品規格、医薬部外品原料規格等に示されており公知である。 About the plant extract used as an astringent, the extraction method etc. are shown in the Japanese Pharmacopoeia non-pharmaceutical standard, the quasi-drug raw material standard, etc., and are known.
例えば、シラカバエキスは、医薬部外品原料規格に記載されており、公知である。具体的には、シラカバエキスは、ヨーロッパシラカバ（Betula alba linne（Betulaceae))の
葉及び／又は樹液に対して抽出溶媒を用いて抽出処理することにより得ることができる。シラカバエキスの抽出処理に使用される抽出溶媒としては、例えば、水；エタノール、プロパノール等の低級アルコール；１，３−ブチレングリコール等の多価アルコール；これらの混合液等の極性溶媒が挙げられる。これらの抽出溶媒の中でも、好ましくはエタノール、又は水と１，３−ブチレングリコールの混合溶媒である。
For example, birch extract is described in quasi-drug raw material standards and is known. Specifically, the birch extract can be obtained by extracting leaves and / or sap of European birch (Betula alba linne (Betulaceae)) using an extraction solvent. Examples of the extraction solvent used for the extraction treatment of birch extract include water; lower alcohols such as ethanol and propanol; polyhydric alcohols such as 1,3-butylene glycol; and polar solvents such as a mixture thereof. Among these extraction solvents, ethanol or a mixed solvent of water and 1,3-butylene glycol is preferable.
また、例えば、ウラジロガシエキスは、日本薬局方外医薬品規格に記載されており、公知である。具体的には、ウラジロガシエキスは、ウラジロガシ（Quercus salicina Blume(Fagaceae))の乾燥した小枝付葉を粗切し、水を加えて浸出することにより得ることができる。 In addition, for example, Virginia vulgaris extract is described in Pharmaceutical Standards outside the Japanese Pharmacopoeia and is known. Specifically, the Vulgaris extract can be obtained by roughly cutting the dried twigs of Quercus salicina Blume (Fagaceae), adding water, and leaching.
これらの収斂剤は、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。 One of these astringents may be used alone, or two or more thereof may be used in combination.
これらの収斂剤の中でも、収斂作用をより効果的に増強させるという観点から、好ましくはアラントイン誘導体、シラカバエキス、ウラジロカシエキス、乳酸アルミニウム、更に好ましくはアラントインクロルヒドロキシアルミニウム、アラントインジヒドロキシアルミニウム、シラカバエキス、ウラジロガシエキス、乳酸アルミニウムが挙げられる。 Among these astringents, from the viewpoint of enhancing the astringent action more effectively, preferably an allantoin derivative, birch extract, urajiloca extract, aluminum lactate, more preferably allantoin hydroxyaluminum, allantoin dihydroxyaluminum, birch extract, Virgin oak extract and aluminum lactate.
本発明の収斂用組成物における(A)成分の含有量については、特に制限されないが、例
えば０．０１〜５重量％、好ましくは０．０１〜３重量％、より好ましくは０．０１〜２重量％が挙げられる。良好な呈味を付与しつつ、収斂作用をより効果的に増強させるという観点から、(A)成分の種類毎の含有量としては、以下の範囲が挙げられる。
(A)成分がアラントイン誘導体の場合：好ましくは０．０１〜１重量％、より好ましくは０．０１〜０．５重量％、更に好ましくは０．０１〜０．３重量％。
(A)成分がシラカバエキスの場合：好ましくは０．０１〜２重量％、より好ましくは０．２〜２重量％、更に好ましくは１〜２重量％。
(A)成分がウラジロガシエキスの場合：好ましくは０．０１〜１重量％、より好ましくは０．０１〜０．３重量％。
(A)成分が乳酸アルミニウムの場合：好ましくは０．０１〜２重量％、より好ましくは０．２〜２重量％。
The content of the component (A) in the astringent composition of the present invention is not particularly limited, but is, for example, 0.01 to 5% by weight, preferably 0.01 to 3% by weight, and more preferably 0.01 to 2% by weight. % By weight. From the viewpoint of more effectively enhancing the astringent action while imparting a good taste, the content of each type of the component (A) includes the following ranges.
When the component (A) is an allantoin derivative: preferably 0.01 to 1% by weight, more preferably 0.01 to 0.5% by weight, and still more preferably 0.01 to 0.3% by weight.
When the component (A) is a birch extract: preferably 0.01 to 2% by weight, more preferably 0.2 to 2% by weight, and still more preferably 1 to 2% by weight.
When the component (A) is Vulgaris extract: preferably 0.01 to 1% by weight, more preferably 0.01 to 0.3% by weight.
When the component (A) is aluminum lactate: preferably 0.01 to 2% by weight, more preferably 0.2 to 2% by weight.
なお、本明細書において、シラカバエキスの含有量については、試料１０ｍｌを蒸発皿に精密に量り、水浴上で蒸発乾固し、さらに残留物を１０５℃で３時間乾燥し、デシケーター中等で放冷した際にその質量が０．０８ｇ（蒸発残留物）になる液状物の場合を基準とした値である。本発明の収斂用組成物を製造するに当たり、使用するシラカバエキスの濃縮の程度等を踏まえた上で、実質的に含有されるシラカバエキスの成分量が前記基準の場合と同様になるように適宜設定すればよい。 In this specification, for the content of birch extract, 10 ml of a sample is precisely weighed in an evaporating dish, evaporated to dryness on a water bath, and the residue is dried at 105 ° C. for 3 hours and cooled in a desiccator or the like. It is a value based on the case of a liquid material whose mass becomes 0.08 g (evaporation residue) when performing the above. In producing the composition for astringent of the present invention, based on the degree of concentration of the birch extract to be used and the like, the amount of components of the birch extract substantially contained is appropriately adjusted so as to be the same as in the case of the above standard. Just set it.
また、本明細書において、ウラジロガシエキスの含有量については、試料約１．０ｇを精密に量り１０５℃で３時間乾燥した際に、その減量が３重量％（乾燥減量）である固形物の場合を基準とした値であり、本発明の収斂用組成物を製造するに当たり、使用するウラジロガシエキスの濃縮の程度等を踏まえた上で、実質的に含有されるウラジロガシエキスの成分量が前記基準の場合と同様になるように適宜設定すればよい。
(B)成分
本発明の収斂用組成物は、収斂剤の収斂作用を増強させる成分として、アセンヤクエキス及びカキタンニンよりなる群から選択される少なくとも１種を含有する。このような特定の(B)成分を収斂剤と併用することによって、収斂剤の収斂作用を相乗的に増強して発
揮させることが可能になる。
Further, in the present specification, the content of the vulgaris extract is a solid substance whose weight loss is 3% by weight (drying loss) when about 1.0 g of a sample is precisely measured and dried at 105 ° C. for 3 hours. In the production of the composition for astringent of the present invention, based on the degree of concentration of the extract of Virginia vulgaris used, etc., the amount of the component of Virginia vulgaris extract substantially contained is based on the above-mentioned standard. What is necessary is just to set suitably so that it may become the same as a case.
(B) Component The astringent composition of the present invention contains, as a component that enhances the astringent action of the astringent, at least one selected from the group consisting of acacia extract and persimmon tannin. By using such a specific component (B) in combination with an astringent, the astringent action of the astringent can be synergistically enhanced and exerted.
本発明において(B)成分として使用されるアセンヤクエキスは、医薬部外品原料規格等に示されており公知である。具体的には、アセンヤクエキスは、ガンビノールノキ（Uncaria gambur Roxburg(Rubbiaceae))の葉及び／又は若枝に対して抽出溶媒を用いて抽出処理することにより得ることができる。シャクヤクエキスの抽出処理に使用される抽出溶媒としては、例えば、水；エタノール、プロパノール等の低級アルコール；１，３−ブチレングリコール等の多価アルコール；これらの混合液等の極性溶媒が挙げられる。より具体的には、アセンヤクエキスは、ガンビノールノキの葉及び若枝に対して水を用いて抽出処理を行った後に乾燥させ、更に低級アルコール、多価アルコール、又はこれらの混合溶媒（好ましくはエタノール、１，３−ブチレングリコール、又はこれらの混合溶媒）を用いて抽出処理することによって得ることができる。 The Acacia catechu extract used as the component (B) in the present invention is publicly known, as indicated in the standard for quasi-drug raw materials and the like. Specifically, the senile extract can be obtained by subjecting leaves and / or shoots of Gambinoki tree (Uncaria gambur Roxburg (Rubbiaceae)) to an extraction treatment using an extraction solvent. Examples of the extraction solvent used for the extraction of the peony extract include water; lower alcohols such as ethanol and propanol; polyhydric alcohols such as 1,3-butylene glycol; and polar solvents such as a mixture thereof. More specifically, Acacia catechu extract is subjected to extraction treatment with water on leaves and shoots of Gambinol tree and then dried, and further dried with lower alcohol, polyhydric alcohol, or a mixed solvent thereof (preferably ethanol, (1,3-butylene glycol, or a mixed solvent thereof).
カキタンニンとは、渋柿（ディオスピロス カキ スンベルグ（エベナシア）（Diospyros kaki Thunberg(Ebenaceae)）の果実の搾汁より得られるタンニンである。カキタンニンの製造方法についても公知である。具体的には、カキタンニンは、渋柿の果実を圧搾機にかけて搾汁液を得て減圧乾燥する方法、渋柿の搾汁液に酵素を用いて密閉保存した後に糖分を除去し、減圧下にて脱水する方法等によって得ることができる。 The persimmon tannin is tannin obtained from squeezed fruit of Diospyros kaki Thunberg (Ebenaceae), which is also known as a method for producing persimmon tannin. The persimmon tannin is obtained by, for example, a method in which a juice of astringent persimmon is squeezed into a squeezer to obtain a squeezed liquid and dried under reduced pressure, a method in which the squeezed liquid of the astringent persimmon is sealed and stored using an enzyme to remove sugar, and dehydrated under reduced pressure. Can be.
本発明の収斂用組成物において、(B)成分として、アセンヤクエキス及びカキタンニンの中から１種を単独で使用してもよく、またこれらを組み合わせて使用してもよい。 In the composition for astringent of the present invention, as the component (B), one from among the Acacia catechu extract and the persimmon tannin may be used alone or in combination.
本発明の収斂用組成物における(B)成分の含有量については、使用する(A)成分の種類や含有量、使用する(B)成分の種類、増強させる収斂作用の程度等に応じて適宜設定されるが、例えば０．０００１〜３重量％、好ましくは０．０００５〜２．５重量％が挙げられる。良好な呈味を付与しつつ、収斂剤の収斂作用をより効果的に増強させるという観点から、(B)成分の種類毎の含有量としては、以下の範囲が挙げられる。
(B)成分がアセンヤクエキスの場合：好ましくは０．００５〜２重量％、より好ましくは０．０１〜２重量％、更に好ましくは０．０１〜１重量％。
(B)成分がカキタンニンの場合：好ましくは０．０００５〜０．５重量％、より好ましくは０．０００５〜０．０１重量％。
The content of the component (B) in the astringent composition of the present invention is appropriately determined according to the type and content of the component (A) used, the type of the component (B) used, the degree of astringent action to be enhanced, and the like. Although it is set, for example, 0.0001 to 3% by weight, preferably 0.0005 to 2.5% by weight. From the viewpoint of more effectively enhancing the astringent action of the astringent while imparting a good taste, the content of each type of the component (B) includes the following ranges.
When the component (B) is an senile extract: preferably 0.005 to 2% by weight, more preferably 0.01 to 2% by weight, and still more preferably 0.01 to 1% by weight.
When the component (B) is oyster tannin: preferably 0.0005 to 0.5% by weight, more preferably 0.0005 to 0.01% by weight.
なお、本明細書において、アセンヤクエキスの含有量については、試料１０ｍｌを蒸発皿に精密に量り、水浴上で蒸発乾固し、さらに残留物を１０５℃で６時間乾燥し、デシケータ中等で放冷した際にその質量が０．３５ｇ（蒸発残留物）になる液状物の場合を基準とした値である。本発明の収斂用組成物を製造するに当たり、使用するアセンヤクエキスの濃縮の程度等を踏まえた上で、実質的に含有されるアセンヤクエキスの成分量が前記基準の場合と同様になるように適宜設定すればよい。 In the present specification, for the content of Acacia catechu extract, a sample (10 ml) was precisely weighed in an evaporating dish, evaporated to dryness on a water bath, and the residue was dried at 105 ° C. for 6 hours and released in a desiccator or the like. The value is based on the case of a liquid material whose mass becomes 0.35 g (evaporation residue) when cooled. In producing the composition for astringent of the present invention, based on the degree of concentration of the sensilla extract used, etc., the component amount of the sensilla extract substantially contained is the same as in the case of the above standard. May be set appropriately.
また、本発明の収斂用組成物において、(A)成分に対する(B)成分の比率としては、使用する(A)成分と(B)成分の種類等に応じて適宜設定すればよいが、収斂剤の収斂作用を効果的に増強させるという観点から、(A)成分１重量部に対して、(B)成分が０．０００１〜１７０重量部、好ましくは０．００１〜１７０重量部が挙げられる。特に、良好な呈味を付与しつつ、前記(A)成分の収斂作用をより効果的に増強させるという観点から、(A)成分の種類に応じた(A)成分と(B)成分の比率については以下の範囲が好適である。
(A)成分がアラントイン誘導体の場合：(A)成分の総量１重量部に対して、(B)成分が好ま
しくは０．０２〜１７０重量部、より好ましくは０．０６〜７０重量部、更に好ましくは０．０６〜２０重量部、特に好ましくは０．０６〜７重量部。
In the astringent composition of the present invention, the ratio of the component (B) to the component (A) may be appropriately set according to the types of the components (A) and (B) to be used. From the viewpoint of effectively enhancing the astringent action of the agent, the component (B) is 0.0001 to 170 parts by weight, preferably 0.001 to 170 parts by weight, based on 1 part by weight of the component (A). . In particular, while imparting a good taste, from the viewpoint of more effectively enhancing the astringent action of the component (A), the ratio of the component (A) and the component (B) according to the type of the component (A) The following ranges are suitable for
When component (A) is an allantoin derivative: component (B) is preferably 0.02 to 170 parts by weight, more preferably 0.06 to 70 parts by weight, and more preferably 1 to 6 parts by weight, based on 1 part by weight of the total amount of component (A). Preferably 0.06 to 20 parts by weight, particularly preferably 0.06 to 7 parts by weight.
(A)成分がシラカバエキスの場合：(A)成分の総量１重重量部に対して、(B)成分が好ましくは０．００１〜１重量部、より好ましくは０．００１〜０．１重量部。
(A)成分がウラジロガシエキスの場合：(A)成分の総量１重量部に対して、(B)成分が好ましくは０．０２〜１７０重量部、より好ましくは０．０２〜７０重量部、更に好ましくは０．１〜１０重量部、特に好ましくは１〜１０重量部。
When the component (A) is a birch extract: The component (B) is preferably 0.001 to 1 part by weight, more preferably 0.001 to 0.1 part by weight, based on 1 part by weight of the total amount of the component (A). Department.
When the component (A) is a vulgaris extract: the component (B) is preferably 0.02 to 170 parts by weight, more preferably 0.02 to 70 parts by weight, and more preferably 1 to 2 parts by weight based on the total amount of the component (A). Preferably it is 0.1 to 10 parts by weight, particularly preferably 1 to 10 parts by weight.
(A)成分が乳酸アルミニウムの場合：(A)成分の総量１重重量部に対して、(B)成分が好ましくは０．００５〜１．５重量部、より好ましくは０．００８〜１重量部、更に好ましくは０．００８〜０．５重量部、特に好ましくは０．００８〜０．１重量部。
製剤形態
本発明の収斂用組成物の形状については特に制限されず、液状、固形状、半固形状（ゲル状、軟膏状、ペースト状）等のいずれであってもよい。
When the component (A) is aluminum lactate: The component (B) is preferably 0.005 to 1.5 parts by weight, more preferably 0.008 to 1 part by weight, based on 1 part by weight of the total amount of the component (A). Parts, more preferably 0.008 to 0.5 parts by weight, particularly preferably 0.008 to 0.1 parts by weight.
Formulation The shape of the astringent composition of the present invention is not particularly limited, and may be any of liquid, solid, semi-solid (gel, ointment, paste) and the like.
本発明の収斂用組成物は、口腔用組成物、皮膚外用組成物等として使用され、口腔粘膜や皮膚等の組織に適用して当該組織を収斂させる目的で使用される。特に、本発明の収斂用組成物は、収斂剤の配合量を増大させずに収斂作用を増強でき、収斂剤の配合量の増大によってもたらされる呈味低下を回避できている。このような本発明の効果に鑑みれば、本発明の収斂用組成物は、呈味が重視される製剤形態である口腔用組成物として好適に使用することができる。 The astringent composition of the present invention is used as a composition for the oral cavity, a composition for the external use of the skin, and the like, and is used for the purpose of applying to a tissue such as the oral mucosa and the skin to converge the tissue. In particular, the astringent composition of the present invention can enhance the astringent action without increasing the amount of the astringent, and can avoid the taste reduction caused by the increase in the amount of the astringent. In view of such effects of the present invention, the astringent composition of the present invention can be suitably used as an oral composition in a formulation form in which taste is emphasized.
本発明の収斂用組成物を口腔用組成物として使用する場合、本発明の収斂用組成物には、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添加成分を含有していてもよい。このような添加成分としては、例えば、研磨剤、防腐剤、殺菌剤、抗菌剤、消炎剤、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、粘着剤、粘稠剤、賦形剤、滑沢剤、香料、甘味剤、清涼化剤、色素、消臭剤、界面活性剤、ｐＨ調整剤、基剤、溶剤、安定化剤等が挙げられる。 When the astringent composition of the present invention is used as an oral composition, the astringent composition of the present invention may be used according to the formulation of the oral composition within the range not impairing the effects of the present invention. It may contain additional components commonly used in the field. Examples of such additional components include abrasives, preservatives, bactericides, antibacterial agents, anti-inflammatory agents, glucosyltransferase (GTase) inhibitors, plaque inhibitors, hypersensitivity inhibitors, tartar preventives, adhesives, adhesives, Thickeners, excipients, lubricants, flavors, sweeteners, cooling agents, pigments, deodorants, surfactants, pH adjusters, bases, solvents, stabilizers and the like can be mentioned.
本発明の収斂用組成物を口腔用組成物として使用する場合、当該口腔用組成物は、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、可食性、非可食性の別を問わない。当該口腔用組成物は、例えば、口腔衛生剤、食品（機能性食品、健康保健用食品、病者用食品等を含む）、医薬品（医薬部外品を含む）、化粧品等のいずれの形態であってもよい。口腔用組成物の製剤形態として、具体的には、液体歯磨剤、練歯磨剤、潤製歯磨剤、粉歯磨剤、洗口剤（マウスウォッシュ）、マウスリンス、含嗽剤、口中清涼剤（マウススプレー等）、口腔用パスタ剤、歯肉マッサージクリーム、口腔咽候薬（トローチ剤等）等の口腔衛生剤；可食性フィルム、チューインガム、キャンディ、グミキャンディ、タブレット、顆粒、細粒、粉末、カプセル等の可食性口腔用剤等が挙げられる。これらの中でも、口腔衛生剤は、口腔粘膜に対して収斂作用を付与し易く、好適な製剤形態である。 When the astringent composition of the present invention is used as an oral composition, the oral composition is edible, non-edible, as long as it is applied to the oral cavity and can stay in the oral cavity for a certain period of time. Regardless. The composition for oral cavity may be, for example, in any form such as an oral hygiene agent, food (including functional foods, health and health foods, foods for the sick, etc.), pharmaceuticals (including quasi-drugs), and cosmetics. There may be. Specific examples of the formulation of the oral composition include a liquid dentifrice, a toothpaste, a lubricating dentifrice, a dentifrice, a mouthwash (mouthwash), a mouth rinse, a gargle, a mouthwash (mouse) Oral hygiene agents such as sprays), oral pasta, gum massage cream, oropharyngeal medicine (troches); edible films, chewing gum, candy, gummy candy, tablets, granules, fine granules, powder, capsules, etc. Edible oral preparations and the like. Among them, the oral hygiene agent easily gives an astringent effect to the oral mucosa, and is a suitable formulation.
また、本発明の収斂用組成物を皮膚外用組成物として使用する場合、本発明の収斂用組成物には、本発明の効果を損なわない範囲で、皮膚外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添加成分を含有していてもよい。このような添加成分としては、例えば、無機顔料、紫外線吸収剤、美白剤、界面活性剤、細胞賦活剤、消炎剤、抗菌剤、保湿剤、清涼化剤、香料、着色剤、消臭剤、界面活性剤、粘着剤、粘稠剤、ｐＨ調整剤、基剤、溶剤、安定化剤等が挙げられる。 Further, when the astringent composition of the present invention is used as a skin external composition, the astringent composition of the present invention may be used in a range that does not impair the effects of the present invention. It may contain additional components commonly used in the art. Examples of such additional components include inorganic pigments, ultraviolet absorbers, whitening agents, surfactants, cell activators, anti-inflammatory agents, antibacterial agents, humectants, fresheners, fragrances, coloring agents, deodorants, Examples include a surfactant, a pressure-sensitive adhesive, a thickener, a pH adjuster, a base, a solvent, and a stabilizer.
本発明の収斂用組成物を皮膚外用組成物として使用する場合、当該皮膚外用組成物は、皮膚に適用されるものである限り、化粧料、医薬品、皮膚洗浄料等のいずれの形態であってもよい。当該皮膚外用組成物の製剤形態として、具体的には、軟膏、クリーム、乳液、化粧水、ローション、パック、ゲル等の化粧料；液剤、貼付剤、エアゾール剤、軟膏、クリーム剤、ゲル剤等の皮膚外用医薬品；ボディーシャンプー、ヘアシャンプー、リンス等の皮膚洗浄料等が挙げられる。
製造方法
本発明の収斂用組成物は、前述する(A)成分、(B)成分、及び必要に応じて配合される添加成分を配合して、その製剤形態に応じた所定の形状に調製することによって製造される。本発明の収斂用組成物には、その製剤形態に応じて、可食性の担体又は薬学的に許容される担体等を含むことができる。
２．収斂作用増強剤
前述するように、アセンヤクエキス及びカキタンニンよりなる群から選択される少なくとも１種には、収斂剤の収斂作用を増強させる作用がある。従って、本発明は、更に、アセンヤクエキス及びカキタンニンよりなる群から選択される少なくとも１種を有効成分とする収斂作用増強剤を提供する。
When the astringent composition of the present invention is used as a skin external composition, the skin external composition may be in any form of cosmetics, pharmaceuticals, skin cleansers, etc. as long as it is applied to the skin. Is also good. Specific examples of the formulation of the composition for external use on the skin include ointments, creams, emulsions, lotions, lotions, packs, gels, and other cosmetics; liquids, patches, aerosols, ointments, creams, gels, and the like. Skin external preparations such as body shampoos, hair shampoos, and rinses.
Production Method The astringent composition of the present invention is prepared by blending the above-mentioned component (A), component (B), and optional components to be added as necessary, to prepare a predetermined shape according to the formulation form. Manufactured by The astringent composition of the present invention may contain an edible carrier or a pharmaceutically acceptable carrier depending on the form of the preparation.
2. Astringent enhancer As described above, at least one selected from the group consisting of Acacia catechu extract and persimmon tannin has an effect of enhancing the astringent effect of the astringent. Therefore, the present invention further provides an astringent-enhancing agent comprising as an active ingredient at least one selected from the group consisting of Acacia catechu extract and persimmon tannin.
本発明の収斂作用増強剤は、収斂剤を含む口腔内組成物や皮膚外用組成物等に添加して、当該収斂剤の収斂作用を増強させる目的で使用される。本発明の収斂作用増強剤において、有効成分として使用されるアセンヤクエキス及びカキタンニンの種類や使用量、収斂作用の増強対象となる収斂剤の種類や使用量、適用可能な口腔内組成物や皮膚外用組成物等については、前記「１．収斂用組成物」の欄に記載の通りである。 The astringent-enhancing agent of the present invention is used for the purpose of enhancing the astringent action of the astringent by adding it to an intraoral composition or an external skin composition containing the astringent. In the astringent action enhancer of the present invention, the type and amount of acacia extract and persimmon tannin used as active ingredients, the type and amount of astringent to be augmented for astringent action, applicable oral compositions and The composition for external use on the skin and the like are as described in the above-mentioned section “1.
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。なお、以下の実施例において、シラカバエキスは、製品名「シラカバ抽出液」（丸善製薬株式会社製）（試料１０ｍｌを蒸発皿に精密に量り、水浴上で蒸発乾固し、さらに残留物を１０５℃で３時間乾燥し、デシケーター中等で放冷した際にその質量が０．０８ｇ（蒸発残留物）になる液状物）、ウラジロガシエキスは、（日本新薬株式会社製）（試料約１．０ｇを精密に量り１０５℃で３時間乾燥した際に、その減量が３重量％（乾燥減量）である固形物）、アセンヤクエキスは、製品名「アセンヤク抽出液ＢＧ」（丸善製薬株式会社製）（試料１０ｍｌを蒸発皿に精密に量り、水浴上で蒸発乾固し、さらに残留物を１０５℃で６時間乾燥し、デシケータ中等で放冷した際にその質量が０．３５ｇ（蒸発残留物）になる液状物）を使用した。
試験例１
表１〜５に示す組成の試験液を調製し、その収斂作用を評価するために、以下に示すアルブミン凝集性試験を行った。
＜アルブミン凝集性試験＞
先ず、アルブミン含有水溶液（アルブミン含有量０．３重量％、クエン酸含有量１．５重量％、ｐＨ４．０）を準備した。各試験液とアルブミン含有水溶液を１：２の容量比で混合し、３７℃で３０分間インキュベートした。次いで、インキュベート後の混合液について、６５０ｎｍにおける濁度を測定した。なお、本試験において、濁度の値が高い程、タンパク質変性効果が強く、収斂作用が大きいと判定される。前記で測定された濁度を用いて、下記式に従って収斂作用の増強率（％）を算出した。
収斂作用の増強率（％）＝[｛（各試験液を使用した場合の濁度）−（対応するコントロールの試験液を使用した場合の濁度）｝／（対応するコントロールの試験液を使用した場合の濁度）]×１００ 得られた結果を表１〜５に示す。参考例１〜３から明らかなように、アセンヤクエキス及びカキタンニンは、単独では、収斂作用が見られなかった。一方、収斂剤（アラントインクロルヒドロキシアルミニウム、シラカバエキス、ウラジロガシエキス、又は乳酸アルミニウム）と、アセンヤクエキス又はカキタンニンを組み合わせると、収斂作用の増強効果が認められた。一方、グリチルレチン酸、メントール、ケイヒアルデヒド、チョウジ油では、収斂剤の収斂作用の増強は認められず、寧ろ収斂作用を減弱させていた。以上の結果から、収斂剤の収斂作用の増強効果は、特定の成分（アセンヤクエキス及び／又はカキタンニン）を選択して収斂剤と共存させることによって認められる特有の効果であることが明らかとなった。特に、実施例１−１及び１−３と、実施例１−５との比較から分かるように、アセンヤクとカキタンニンの両方を含む場合、収斂作用の増強効果に特に優れることが明らかとなった。
Hereinafter, the present invention will be described more specifically with reference to Examples, but the present invention is not limited thereto. In the following examples, birch extract was used as the product name “birch extract” (manufactured by Maruzen Pharmaceutical Co., Ltd.) (a 10 ml sample was precisely weighed in an evaporating dish, evaporated to dryness on a water bath, and the residue was dried to 105%). C. and dried for 3 hours in a desiccator or the like, and when left to cool in a desiccator or the like, the mass of which becomes 0.08 g (evaporation residue). When weighed precisely and dried at 105 ° C. for 3 hours, the weight loss is 3% by weight (dry weight loss) (solid matter). Asenyaku extract is a product name “Asenyaku extract BG” (manufactured by Maruzen Pharmaceutical Co., Ltd.) ( A sample (10 ml) is precisely weighed in an evaporating dish, evaporated to dryness on a water bath, and the residue is dried at 105 ° C. for 6 hours. When the residue is cooled in a desiccator or the like, its mass becomes 0.35 g (evaporation residue). Liquid material)
Test example 1
Test liquids having the compositions shown in Tables 1 to 5 were prepared, and an albumin cohesion test shown below was performed to evaluate the astringent action.
<Albumin aggregation test>
First, an aqueous solution containing albumin (albumin content 0.3% by weight, citric acid content 1.5% by weight, pH 4.0) was prepared. Each test solution and the aqueous solution containing albumin were mixed at a volume ratio of 1: 2, and incubated at 37 ° C. for 30 minutes. Next, the turbidity at 650 nm of the mixed solution after the incubation was measured. In this test, it is determined that the higher the turbidity value, the stronger the protein denaturing effect and the greater the astringent effect. Using the turbidity measured as described above, the astringent enhancement rate (%) was calculated according to the following equation.
Enhancement rate of astringent action (%) = [{(turbidity when using each test solution)-(turbidity when using corresponding control test solution)] / (using corresponding control test solution) Turbidity in case of performing)] × 100 The obtained results are shown in Tables 1 to 5. As is evident from Reference Examples 1 to 3, the acacia extract and the persimmon tannin alone did not show an astringent action. On the other hand, when an astringent (allantoinchlorohydroxyaluminum, birch extract, urajirogashi extract, or aluminum lactate) was combined with an asenyaku extract or oyster tannin, an effect of enhancing astringent action was observed. On the other hand, in the case of glycyrrhetinic acid, menthol, cinnamaldehyde, and clove oil, no enhancement of the astringent effect of the astringent was observed, but rather the astringent effect was attenuated. From the above results, it is clear that the astringent enhancing effect of the astringent is a unique effect recognized by selecting a specific component (acenilla extract and / or oyster tannin) and coexisting with the astringent. became. In particular, as can be seen from the comparison between Examples 1-1 and 1-3 and Example 1-5, it was revealed that when both Asenyaku and oyster tannin were included, the astringent action was particularly excellent in enhancing effect. .
試験例２
表６〜９に示す組成の試験液を調製し、口腔内に適用した場合の使用感について評価した。具体的には、３名のパネラーによって、各試験液１０ｍｌを口に含ませて下記判定基準に従って呈味を評点化した。
（呈味の判定基準）
評点
５：口腔内組成物として相応しい呈味であり、使用感が良好である。
４：口腔内組成物としてやや相応しい呈味であり、使用感がやや良好である。
３：口腔内組成物として普通の呈味であり、使用感も普通である。
２：口腔内組成物としてあまり相応しくない呈味であり、使用感がやや悪い。
１：口腔内組成物として相応しくない呈味であり、使用感が悪い。
Test example 2
Test liquids having the compositions shown in Tables 6 to 9 were prepared and evaluated for the feeling of use when applied in the oral cavity. Specifically, the taste was scored by three panelists by putting 10 ml of each test solution in their mouth according to the following criteria.
(Taste criteria)
Rating 5: Taste suitable as an intraoral composition and good feeling in use.
4: The taste is somewhat suitable as an intraoral composition, and the feeling in use is somewhat good.
3: It has a normal taste as an intraoral composition, and the feeling of use is also normal.
2: The taste is not very suitable as an intraoral composition, and the feeling of use is somewhat poor.
1: The taste is unsuitable as an intraoral composition, and the feeling of use is poor.
次いで、各パネラーが判定した評点を合計し、下記の分類基準に従って、使用感を評価した。
（使用感の分類基準）
＋＋＋＋：評点の合計が１２点以上
＋＋＋ ：評点の合計が９点以上１１点以下
＋＋ ：評点の合計が６点以上８点以下
＋ ：評点の合計が５点以下
得られた結果を表６〜９に示す。この結果から、収斂剤と共に、アセンヤクエキス、又はカキタンニンを併用すると、口腔内に適用された際の呈味が良好になることが確認された。また、表６〜９に示すいずれの試験液においても、（A）成分又は（B）成分をそれぞれ単独で含有する場合に比べて、（A）成分及び（B）成分の両方を含有する場合の方が、収斂効果は高まっていた。即ち、本試験結果から、収斂剤と、シャクヤクエキス、トウキエキス、又はムクロジエキスとを併用した収斂用組成物は、口腔用組成物として使用しても、収斂効果が高まり、且つ呈味の点でも良好であり、優れた使用感が得られることが明らかとなった。
Next, the scores determined by each panel were totaled, and the usability was evaluated according to the following classification criteria.
(Criteria for classification of usability)
+++++: Total score is 12 points or more +++: Total score is 9 points or more and 11 points or less ++: Total score is 6 points or more and 8 points or less +: Total score is 5 points or less Table 6- It is shown in FIG. From these results, it was confirmed that the taste when applied in the oral cavity was improved when the senile extract or the persimmon tannin was used in combination with the astringent. In addition, in any of the test liquids shown in Tables 6 to 9, when both the component (A) and the component (B) are contained as compared with the case where the component (A) or the component (B) is contained alone. Had a higher convergence effect. That is, from the present test results, the astringent composition using an astringent, a peony extract, a squid extract, or a mulberry extract, even when used as an oral composition, has an increased astringent effect, and has a point of taste. However, it was clear that an excellent feeling in use was obtained.
製造例１
表１０〜１３に示す組成の練歯磨剤を製造した。いずれの練歯磨剤においても、（B）
成分を含有しない場合に比べて、収斂剤の収斂作用の相乗的な増強効果が認められ、味も良好であった。
Production Example 1
Toothpastes having the compositions shown in Tables 10 to 13 were produced. In any toothpaste, (B)
Compared to the case where no component was contained, a synergistic enhancement effect of the astringent action of the astringent was recognized, and the taste was also good.
製造例２
表１４に示す組成の液体歯磨剤を製造した。当該液体歯磨剤においても、（B）成分を
含有しない場合に比べて、収斂剤の収斂作用の相乗的な増強効果が認められ、味も良好であった。
Production Example 2
A liquid dentifrice having the composition shown in Table 14 was produced. Also in the liquid dentifrice, a synergistic enhancing effect of the astringent of the astringent was recognized and the taste was good as compared with the case where the component (B) was not contained.
製造例３
表１５に示す組成の口腔咽喉薬（トローチ剤：ドロップ）を製造した。当該口腔咽喉薬においても、（B）成分を含有しない場合に比べて、収斂剤の収斂作用の相乗的な増強効果が認められ、味も良好であった。
Production Example 3
Oral and throat drugs (troches: drops) having the composition shown in Table 15 were produced. Also in the oropharyngeal drug, a synergistic enhancing effect of the astringent action of the astringent was recognized and the taste was good as compared with the case where the component (B) was not contained.
Claims (2)
前記(A)成分の含有量が０．０１〜０．１重量％であり、且つ口腔用組成物であることを特徴とする、収斂用組成物。 (A) an allantoin derivative , and (B) containing at least one selected from the group consisting of acacia extract and oyster tannin ,
Wherein (A) is from 0.01 to 0.1% by weight content of the component, and is characterized in der Rukoto oral composition, astringent composition.
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| JP2887636B2 (en) * | 1993-06-11 | 1999-04-26 | 株式会社粘土科学研究所 | Oral preparation |
| JP2002003353A (en) * | 2000-06-19 | 2002-01-09 | Kansai Koso Kk | Methionase and/or protease inhibitor and composition for oral cavity |
| JP2002322075A (en) * | 2001-04-23 | 2002-11-08 | Yoshiki Okano | Composition |
| JP5710241B2 (en) * | 2010-12-28 | 2015-04-30 | 花王株式会社 | Liquid oral composition |
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2018
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