JP2006045080A - Skin care preparation suitable as quasi-drug - Google Patents
Skin care preparation suitable as quasi-drug Download PDFInfo
- Publication number
- JP2006045080A JP2006045080A JP2004225501A JP2004225501A JP2006045080A JP 2006045080 A JP2006045080 A JP 2006045080A JP 2004225501 A JP2004225501 A JP 2004225501A JP 2004225501 A JP2004225501 A JP 2004225501A JP 2006045080 A JP2006045080 A JP 2006045080A
- Authority
- JP
- Japan
- Prior art keywords
- external preparation
- skin
- acid
- quaternium
- ascorbic acid
- 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
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 62
- 229940079593 drug Drugs 0.000 title claims description 9
- 239000003814 drug Substances 0.000 title claims description 9
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- 230000008099 melanin synthesis Effects 0.000 claims abstract description 34
- 235000010323 ascorbic acid Nutrition 0.000 claims abstract description 31
- 239000011668 ascorbic acid Substances 0.000 claims abstract description 31
- 229960005070 ascorbic acid Drugs 0.000 claims abstract description 31
- MRIXVKKOHPQOFK-UHFFFAOYSA-N 4-methoxysalicylic acid Chemical compound COC1=CC=C(C(O)=O)C(O)=C1 MRIXVKKOHPQOFK-UHFFFAOYSA-N 0.000 claims abstract description 26
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- 150000003839 salts Chemical class 0.000 claims abstract description 15
- IZZIWIAOVZOBLF-UHFFFAOYSA-N 5-methyloxysalicylic acid Natural products COC1=CC=C(O)C(C(O)=O)=C1 IZZIWIAOVZOBLF-UHFFFAOYSA-N 0.000 claims abstract description 13
- 229960000271 arbutin Drugs 0.000 claims abstract description 13
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- MLSJBGYKDYSOAE-DCWMUDTNSA-N L-Ascorbic acid-2-glucoside Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=C1O MLSJBGYKDYSOAE-DCWMUDTNSA-N 0.000 claims description 10
- 230000002401 inhibitory effect Effects 0.000 claims description 7
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- 238000012360 testing method Methods 0.000 description 11
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- WNWHHMBRJJOGFJ-UHFFFAOYSA-N 16-methylheptadecan-1-ol Chemical compound CC(C)CCCCCCCCCCCCCCCO WNWHHMBRJJOGFJ-UHFFFAOYSA-N 0.000 description 2
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- FVEWVVDBRQZLSJ-QTWKXRMISA-N 2-hydroxyethyl-dimethyl-[3-[[(2r,3s,4r,5r)-2,3,4,5,6-pentahydroxyhexanoyl]amino]propyl]azanium;chloride Chemical compound [Cl-].OCC[N+](C)(C)CCCNC(=O)[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FVEWVVDBRQZLSJ-QTWKXRMISA-N 0.000 description 2
- XPFCZYUVICHKDS-UHFFFAOYSA-N 3-methylbutane-1,3-diol Chemical compound CC(C)(O)CCO XPFCZYUVICHKDS-UHFFFAOYSA-N 0.000 description 2
- ALYNCZNDIQEVRV-UHFFFAOYSA-N 4-aminobenzoic acid Chemical compound NC1=CC=C(C(O)=O)C=C1 ALYNCZNDIQEVRV-UHFFFAOYSA-N 0.000 description 2
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
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- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 2
- 239000004386 Erythritol Substances 0.000 description 2
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 description 2
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Landscapes
- Cosmetics (AREA)
Abstract
Description
本発明は、皮膚外用剤に関し、更に詳細には、医薬部外品などの化粧料に好適な皮膚外用剤に関する。 The present invention relates to an external preparation for skin, and more particularly to an external preparation for skin suitable for cosmetics such as quasi drugs.
化粧料などの皮膚外用剤にとって、過剰にメラニン色素が産生されるのを防ぎ、肌を白く保つことは重要な要件の一つである。このため、種々のメラニン産生を抑制する物質(以下、「メラニン産生抑制物質」とも称する)が探索され、得られてきている。このような物質としては、例えば、1) グルタチオン誘導体、2) アスコルビン酸及びその誘導体(アスコルビン酸のリン酸エステル、及びアスコルビン酸グルコシドのようなアスコルビン酸の配糖体を含む)、3) 硫黄原子、4) ハイドロキノンやアルブチン、及びその配糖体、4) トラネキサム酸、5) 4−メトキシサリチル酸、6) コウジ酸などが好ましく例示できる。
これらのうち、メラニン産生抑制効果と安全性の面から、特に有望なものとして、アスコルビン酸及びその誘導体、アルブチン、トラネキサム酸、4−メトキシサリチル酸、ならびにこれらの塩などが挙げられる(例えば、非特許文献1を参照)。しかしながら、これらのメラニン産生抑制物質の多くは、還元性を有する物質であり、高温条件下における安定性に課題が存した。したがって、皮膚外用剤に含まれるメラニン産生抑制物質の高温条件下での安定性を向上させる手段の開発が望まれていた。
For skin preparations such as cosmetics, it is one of the important requirements to prevent excessive production of melanin pigment and keep the skin white. For this reason, various substances that suppress melanin production (hereinafter also referred to as “melanin production inhibitors”) have been searched and obtained. Examples of such substances include 1) glutathione derivatives, 2) ascorbic acid and its derivatives (including phosphate esters of ascorbic acid and glycosides of ascorbic acid such as ascorbic acid glucoside), 3) sulfur atoms 4) Hydroquinone and arbutin, and their glycosides, 4) tranexamic acid, 5) 4-methoxysalicylic acid, 6) kojic acid and the like can be preferably exemplified.
Among these, ascorbic acid and its derivatives, arbutin, tranexamic acid, 4-methoxysalicylic acid, and salts thereof are particularly promising from the viewpoint of melanin production inhibitory effect and safety (for example, non-patented) Reference 1). However, many of these melanin production inhibitors are substances having reducibility, and there has been a problem in stability under high temperature conditions. Therefore, it has been desired to develop a means for improving the stability of the melanin production inhibitor contained in the external preparation for skin under high temperature conditions.
なお、メラニン産生抑制物質などの還元性物質を安定化する手段はいくつか知られている。例えば、該物質の光に対する安定性を向上させる手段として、ベンゾフェノン類や桂皮酸エステル類等の紫外線吸収剤を組み合わせる方法が挙げられる(例えば、特許文献1を参照)。しかしながら、このような手段は、還元性物質の高温条件下における安定性を向上させる手段としては十分とはいえない。 Several means are known for stabilizing reducing substances such as melanin production inhibitors. For example, as a means for improving the light stability of the substance, a method of combining an ultraviolet absorber such as benzophenones and cinnamic acid esters can be mentioned (for example, see Patent Document 1). However, such means is not sufficient as means for improving the stability of the reducing substance under high temperature conditions.
一方、クオタニウムは、毛髪などの保水性を高める作用あるいは皮膚の立体形状の不均一を均一に見せる作用を有することが知られている(例えば、特許文献2〜3を参照)。 On the other hand, it is known that quaternium has an effect of enhancing water retention of hair or the like or an effect of uniformly showing unevenness of the three-dimensional shape of the skin (see, for example, Patent Documents 2 to 3).
しかしながら、前記メラニン産生抑制物質、およびクオタニウムを共に含有する皮膚外用剤は知られておらず、その皮膚外用剤が有する効果も知られていない。
本発明は、このような状況下においてなされたものであり、メラニン産生抑制物質(例えば、アスコルビン酸及びその誘導体(アスコルビン酸リン酸エステル、アスコルビン酸−2−グルコシド等を含む)、アルブチン、トラネキサム酸、4−メトキシサリチル酸、ならびにこれらの塩などを含む)の皮膚外用剤中での、高温条件下における安定性を向上せしめる手段を提供することを課題とする。
また、該手段を用いることで、高温条件下での保存安定性が高い、メラニン産生抑制作用を有する皮膚外用剤を提供することを課題とする。
The present invention has been made under such circumstances, and is a substance that suppresses melanin production (for example, ascorbic acid and its derivatives (including ascorbic acid phosphate ester, ascorbic acid-2-glucoside, etc.), arbutin, tranexamic acid. , 4-methoxysalicylic acid, and salts thereof, etc.) and a means for improving the stability under high temperature conditions.
Another object of the present invention is to provide an external preparation for skin having a storage stability under a high temperature condition and having a melanin production inhibitory effect by using the means.
この様な状況に鑑みて、本発明者らは、種々のメラニン産生抑制物質(アスコルビン酸及びその誘導体、アルブチン、トラネキサム酸、4−メトキシサリチル酸、ならびにこれらの塩などを含む)を含有する皮膚外用剤の、高温条件下における保存安定性をさらに向上させる手段を求めて、鋭意研究努力を重ねた。その結果、皮膚外用剤に含有されるメラニン産生抑制物質の保存安定性が、クオタニウムにより向上されることを見いだした。
この知見から、メラニン産生抑制物質を含有する皮膚外用剤に、さらにクオタニウムを含有させると、該皮膚外用剤が高温条件下においても安定に保存されうることを見出し、本発明を完成させるに至った。即ち、本発明は、以下に示す技術に関するものである。
In view of such a situation, the present inventors have used various skin melanin production inhibitors (including ascorbic acid and its derivatives, arbutin, tranexamic acid, 4-methoxysalicylic acid, and salts thereof). In search of means for further improving the storage stability of the agent under high temperature conditions, intensive research efforts were made. As a result, it was found that the storage stability of the melanin production inhibitor contained in the external preparation for skin was improved by quaternium.
From this finding, it was found that when the skin external preparation containing a melanin production-suppressing substance further contains quaternium, the skin external preparation can be stably stored even under high temperature conditions, and the present invention has been completed. . That is, this invention relates to the technique shown below.
(1) 1)アスコルビン酸及びその誘導体、アルブチン、トラネキサム酸、4−メトキシサリチル酸、並びにそれらの塩から選択される1種又は2種以上と、2)クオタニウムから選択される1種又は2種以上とを含有することを特徴とする皮膚外用剤。
(2) 前記アスコルビン酸の誘導体が、アスコルビン酸リン酸エステル又はアスコルビン酸−2−グルコシドであることを特徴とする、(1)に記載の皮膚外用剤。
(3) 前記アスコルビン酸及びその誘導体、アルブチン、トラネキサム酸、4−メトキシサリチル酸並びにそれらの塩から選択される1種又は2種以上の含有量が、皮膚外用剤全量に対して、0.1〜10質量%であることを特徴とする、(1)又は(2)に記載の皮膚外用剤。
(4) 前記クオタニウムから選択される1種又は2種以上の含有量が、皮膚外用剤全量に対して、0.01〜5質量%であることを特徴とする、(1)〜(3)のいずれかに記載の皮膚外用剤。
(5) 化粧料であることを特徴とする、(1)〜(4)のいずれかに記載の皮膚外用剤。
(6) メラニン産生を抑制するための医薬部外品であることを特徴とする、(1)〜(5)のいずれかに記載の皮膚外用剤。
(7) メラニン産生抑制作用を訴求したことを特徴とする、(1)〜(6)のいずれかに記載の皮膚外用剤。
(1) 1) One or more selected from ascorbic acid and derivatives thereof, arbutin, tranexamic acid, 4-methoxysalicylic acid, and salts thereof, and 2) one or more selected from quaternium A skin external preparation characterized by containing.
(2) The external preparation for skin according to (1), wherein the derivative of ascorbic acid is ascorbic acid phosphate ester or ascorbic acid-2-glucoside.
(3) The content of one or more selected from the ascorbic acid and its derivatives, arbutin, tranexamic acid, 4-methoxysalicylic acid and salts thereof is 0.1 to The external preparation for skin according to (1) or (2), wherein the external preparation is 10% by mass.
(4) Content of 1 type (s) or 2 or more types selected from said quaternium is 0.01-5 mass% with respect to the skin external preparation whole quantity, (1)-(3) characterized by the above-mentioned. The external preparation for skin according to any one of the above.
(5) The skin external preparation according to any one of (1) to (4), which is a cosmetic.
(6) The external preparation for skin according to any one of (1) to (5), which is a quasi-drug for suppressing melanin production.
(7) The skin external preparation according to any one of (1) to (6), characterized by appealing an inhibitory action on melanin production.
本発明によれば、高温条件下における保存安定性の高い皮膚外用剤を提供することができる。 ADVANTAGE OF THE INVENTION According to this invention, the skin external preparation with high storage stability in high temperature conditions can be provided.
(1) 本発明の皮膚外用剤の必須成分であるメラニン産生抑制物質
本発明の皮膚外用剤は、メラニン産生抑制物質を必須成分として含有することを特徴とする。メラニン産生抑制物質としては、アスコルビン酸及びその誘導体、アルブチン、トラネキサム酸、4−メトキシサリチル酸、並びにこれらの塩から選択される1種又は2種以上が挙げられる。これらの成分はいずれも、化粧料(とりわけ、医薬部外品の化粧料)に含有させることのできる成分として知られている。従って、これらの入手に関しては問題なく、市販されている原料を購入して用いることができる。
(1) Melanin production inhibitor which is an essential component of the external preparation for skin of the present invention The external preparation for skin of the present invention is characterized by containing a melanin production inhibitor as an essential ingredient. Examples of the melanin production inhibitor include one or more selected from ascorbic acid and derivatives thereof, arbutin, tranexamic acid, 4-methoxysalicylic acid, and salts thereof. All of these components are known as components that can be contained in cosmetics (particularly, quasi-drug cosmetics). Therefore, there is no problem regarding the acquisition of these, and commercially available raw materials can be purchased and used.
上記メラニン産生を抑制する物質のうち、アスコルビン酸は以下の式(I)で表される構造を有する化合物である。アスコルビン酸の誘導体としては、例えば、アスコルビン酸の脂肪酸エステル、アスコルビン酸のリン酸エステル、アスコルビン酸の配糖体等が好ましく例示できる。より好ましくはアスコルビン酸のリン酸エステル、アスコルビン酸の配糖体が例示される。 Among the substances that suppress melanin production, ascorbic acid is a compound having a structure represented by the following formula (I). Preferred examples of the derivatives of ascorbic acid include fatty acid esters of ascorbic acid, phosphate esters of ascorbic acid, glycosides of ascorbic acid, and the like. More preferable examples include phosphate esters of ascorbic acid and glycosides of ascorbic acid.
前記アスコルビン酸の脂肪酸エステルは、上記式(I)におけるA〜Dのいずれかのヒドロキシル基が脂肪酸エステル化されたものであるが、好ましくはA及び/又はDのヒドロキシル基が脂肪酸エステル化されたものである。脂肪酸エステルの脂肪酸としては、パルミチン酸などが挙げられるがこれらに限定されない。 The fatty acid ester of ascorbic acid is obtained by fatty acid esterification of any of hydroxyl groups A to D in the above formula (I), and preferably the hydroxyl group of A and / or D is fatty acid esterified. Is. Examples of the fatty acid of the fatty acid ester include, but are not limited to, palmitic acid.
アスコルビン酸のリン酸エステルとしては、上記式(I)におけるA〜Dのいずれかのヒドロキシル基がリン酸エステル化されたものであるが、好ましくはA又はBのヒドロキシル基がリン酸エステル化されたものであり、特に好ましくはAのヒドロキシル基がリン酸エステル化された、アスコルビン酸−2−リン酸エステルである。 As the phosphoric acid ester of ascorbic acid, the hydroxyl group of any one of A to D in the above formula (I) is phosphorylated, but preferably the hydroxyl group of A or B is phosphorylated. Particularly preferred is ascorbyl 2-phosphate ester in which the hydroxyl group of A is phosphorylated.
前記アスコルビン酸の配糖体は、アスコルビン酸と通常天然に存する糖との配糖体であり、特段の限定はされない。例えば、グルコシド、アラビノシド、リボシド、デオキシリボシド、ガラクトシド、ラムノシド、アラビノシルグルコシド、グルコシルガラクトシド、ラムノシルグルコシド等が好ましく例示できる。また、上記式(I)のAのヒドロキシル酸素原子と糖のC−1炭素原子とがエーテル結合した配糖体が好ましい。例えば、アスコルビン酸−2−グルコシドが特に好ましく例示される。 The glycoside of ascorbic acid is a glycoside of ascorbic acid and a normal naturally occurring sugar, and is not particularly limited. For example, glucoside, arabinoside, riboside, deoxyriboside, galactoside, rhamnoside, arabinosyl glucoside, glucosyl galactoside, rhamnosyl glucoside and the like can be preferably exemplified. Further, a glycoside in which the hydroxyl oxygen atom of A in the above formula (I) and the C-1 carbon atom of the sugar are ether-bonded is preferable. For example, ascorbic acid-2-glucoside is particularly preferably exemplified.
前記アスコルビン酸の配糖体は、常法に従って製造することもできるし、市販品を購入して使用することもできる。製造法としては、例えば、糖とそれを基質とする酵素とアスコルビン酸とを共存させ、30〜50℃でインキュベートすればよい。例えば、グルコシドであれば、アスコルビン酸、グルコース及びグルコシダーゼをインキュベートし、しかる後に、シリカゲルカラムクロマトグラフィー、「ダイアイオンHP−20」(三菱化成株式会社製)などのイオン交換樹脂を用いた分配クロマトグラフィー、ゲル濾過カラムクロマトグラフィー、ODSを充填剤としたカラムクロマトグラフィー等で順次精製することにより得ることができる。
一方、市販品としては、林原研究所株式会社より販売されているアスコルビン酸−2−グルコシドが好ましく例示できる。
The glycoside of ascorbic acid can be produced according to a conventional method, or a commercially available product can be purchased and used. As a production method, for example, a saccharide, an enzyme using it as a substrate, and ascorbic acid may be allowed to coexist and incubated at 30 to 50 ° C. For example, in the case of glucoside, ascorbic acid, glucose and glucosidase are incubated, and thereafter, silica gel column chromatography, partition chromatography using an ion exchange resin such as “Diaion HP-20” (manufactured by Mitsubishi Kasei Co., Ltd.). , Gel filtration column chromatography, column chromatography using ODS as a filler, and the like.
On the other hand, as a commercial item, ascorbic acid-2-glucoside currently sold from Hayashibara Laboratory Co., Ltd. can be illustrated preferably.
本発明の皮膚外用剤に含まれるメラニン産生抑制物質は、フリー体で含有されてもよいし、塩として含有されてもよい。当該塩としては、例えば、ナトリウム塩、カリウム塩等のアルカリ金属塩、カルシウム塩、マグネシウム塩等のアルカリ土類金属塩、アンモニウム塩、トリエチルアミン塩、トリエタノールアミン塩、モルホリン塩等の有機アミン塩、リジン塩、アルギニン塩等の塩基性アミノ酸塩等が好適に例示できる。これらの塩は、メラニン産生抑制物質と、それぞれ対応する塩基とを反応させることで得ることができる。 The melanin production inhibitor contained in the external preparation for skin of the present invention may be contained in a free form or as a salt. Examples of the salt include alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts such as calcium salt and magnesium salt, organic amine salts such as ammonium salt, triethylamine salt, triethanolamine salt and morpholine salt, Preferred examples include basic amino acid salts such as lysine salts and arginine salts. These salts can be obtained by reacting a melanin production inhibitor with a corresponding base.
メラニン産生抑制物質(アスコルビン酸及びその誘導体、アルブチン、トラネキサム酸
、4−メトキシサリチル酸、又はこれらの塩を含む)は、本発明の皮膚外用剤中に、一種単独で含有されることもできるし、二種以上を組み合わせて含有されることもできる。本発明の皮膚外用剤中のメラニン産生抑制物質の含有量は、皮膚外用剤全量に対して、総量で0.1〜10質量%であることが好ましく、0.5〜5質量%であることがより好ましい。前記含有量が、0.1質量%以上であるとメラニン産生抑制作用を十分に発揮するので好ましく、10質量%以下であるとコスト面などで好ましい。
Melanin production inhibitor (including ascorbic acid and its derivatives, arbutin, tranexamic acid, 4-methoxysalicylic acid, or salts thereof) can be contained alone in the skin external preparation of the present invention, Two or more kinds may be contained in combination. The content of the melanin production inhibitor in the external preparation for skin of the present invention is preferably 0.1 to 10% by mass, and preferably 0.5 to 5% by mass, based on the total amount of external preparation for skin. Is more preferable. When the content is 0.1% by mass or more, the melanin production inhibitory effect is sufficiently exhibited, and when the content is 10% by mass or less, it is preferable in terms of cost.
(2) 本発明の皮膚外用剤の必須成分であるクオタニウム
本発明の皮膚外用剤は、クオタニウムから選択される1種又は2種以上を必須成分として含有することを特徴とする。ここでクオタニウムとは、4級アミノ基を有する化合物であって、米国化粧品工業会(CTFA)で化粧料成分として認められ、クオタニウムに分類されてナンバーが付されているものを意味する。それらのうちから、特段の限定なく選択することができる。
(2) Quotanium as an essential component of the external preparation for skin of the present invention The external preparation for skin of the present invention is characterized by containing one or more kinds selected from quaternium as an essential component. Here, quaternium means a compound having a quaternary amino group, which is recognized as a cosmetic ingredient by the American Cosmetic Industry Association (CTFA), classified as quaternium, and numbered. Among these, it can select without special limitation.
クオタニウムとしては、例えば、クオタニウム14(塩化ラウリルジメチルエチルベンジルアンモニウム;マコートMQ2525M;マッソン社製)、クオタニウム15(N−(3−クロロアリル)ヘキサミニウムクロリド;ダウイシル200;ダウコーニング社製)、クオタニウム18(塩化ジメチルジ(水素化タロウ)アンモニウム;ヴァリソフト442 100P;デガッサ・スペシャリティ社製)、クオタニウム22(γ−グルコンアミドプロピル ジメチル2−ヒドロキシエチルアンモニウムクロリド;セラフィル60;インターナショナル・スペシャルティズ社製)、クオタニウム24(塩化デシルジメチルオクチルアンモニウム;マコート4050;マッソン社製)、クオタニウム26(ミンカミドプロピルジメチル2−ヒドロキシエチルアンモニウムクロリド;インクロコート26;クロダ社製)、クオタニウム27(4,5−ジヒドロー1−メチル−2−ノルタロウアルキル−1−(2−タロウアミドエチル)イミダゾリウムメチルサルフェート;AECクオタニウム27;A&Eコンノック社製)、クオタニウム33(N(N‘ラノリン脂肪酸アミドプロピル)N−エチル−N,N−ジメチルアンモニウムエチルサルフェート;ニッコールラノコートDES−50;日光ケミカルズ株式会社製)、クオタニウム43(コカミドプロピルジメチルアセタミドアンモニウムクロリド;シメキサンCK:シメックス社製)、クオタニウム45(ルミネックス;池田物産株式会社製)、クオタニウム52(POE(オクタデシルニトリリオ)トリ−2,1−エタンジイル)トリスヒドロキシホスフェート;デヒコートSP;コグニス社製)、クオタニウム53(インクロソフトT−90;クロダ社製)、クオタニウム60(ラノリン・イソステアラミドプロピルエチルジメチルアンモニウムエトサルフェート;ラノコート1751A;コグニス社製)、クオタニウム61(ダイマー酸・ビス(アミドプロピル−N,N−ジメチル−N−エチルアンモニウムエトスルフェート;シェルコートDAS;シェル社製)、クオタニウム70(ステアラミドプロピルジメチル(ミリスチルアセテート)アンモニウムクロリド;セラフィル70:インターナショナル・スペシャルティズ社製)、クオタニウム72(インクロソフトCFI75;クロダ社製)、クオタニウム73(感光素201;感光素株式会社製)、クオタニウム75(レーヴェノールコンディショナーC727;レーヴェンシュタイン社製)、クオタニウム76コラーゲン複合体(レクセインQX−3000;イノレックス社製)、クオタニウム77(フィンソフトHCM−100;フィネテックス社製)、クオタニウム79(マックプロNLP;マッキンタイル社製)、クオタニウム80(コヴァフィックス123;LCW社製)、クオタニウム82(ステパンコートDC1;ステパン社製)、クオタニウム84(マッカーニウムNLE;マッキンタイル社製)、クオタニウム85(2−ヒドロキシ−3−((2−ヒドロキシエチル)(2−((1−オキソテトラデシル(アミノ)エチル)アミノ)−N,N,N−トリメチル−1−プロパンアミニウムクロリド;アミノカチオンS−36;花王株式会社製)、クオタニウム86(ペコシルSWQ−40;フェニックス社製)、クオタニウム87(ヴァリソフトW575PG;デガッサ社製)、クオタニウム88(ネコートDAS−D;アルゾ社製)、クオタニウム89(フィン
コートCT−P;ファインテック社製)、クオタニウム91(クロダソフトDBQ;クロダ社製)等が好ましく例示できる。
これらのうち、より好ましいものとしては、クオタニウム33、クオタニウム45、クオタニウム73、クオタニウム80及びクオタニウム85が例示できる。
Examples of quaternium include quaternium 14 (lauryldimethylethylbenzylammonium chloride; McCourt MQ2525M; manufactured by Masson), quaternium 15 (N- (3-chloroallyl) hexanium chloride; Dauisil 200; manufactured by Dow Corning), and quaternium 18 ( Dimethyldi (hydrogenated tallow) ammonium chloride; Varisoft 442 100P; manufactured by Degassa Specialty), quaternium 22 (γ-gluconamidopropyl dimethyl 2-hydroxyethylammonium chloride; Cerafil 60; manufactured by International Specialties), quaternium 24 (Decyldimethyloctylammonium chloride; McCoat 4050; manufactured by Masson), quaternium 26 (mincamidepropyldimethyl 2-hydroxy) Cyethylammonium chloride; Incrocoat 26; manufactured by Kuroda), Quotanium 27 (4,5-dihydro-1-methyl-2-nortaroualkyl-1- (2-tallowamidoethyl) imidazolium methyl sulfate; AEC quaternium 27; A & E Connock), Quotanium 33 (N (N 'lanolin fatty acid amidopropyl) N-ethyl-N, N-dimethylammonium ethyl sulfate; Nikkor Lanocoat DES-50; manufactured by Nikko Chemicals Co., Ltd.), Quotanium 43 (Cocamid) Propyldimethylacetamide ammonium chloride; Simexan CK: manufactured by Simex Corporation), quaternium 45 (LUMEX; manufactured by Ikeda Bussan Co., Ltd.), quaternium 52 (POE (octadecylnitrilorio) tri-2,1-ethanediyl) Lithoxyphosphate; Dehicoat SP; manufactured by Cognis Co., Ltd.), Quotanium 53 (Incrosoft T-90; manufactured by Kuroda Co., Ltd.), Quaternium 60 (lanolin, isostearamidopropylethyldimethylammonium etosulphate; Lanocoat 1751A, manufactured by Cognis Co., Ltd.), quaternium 61 (dimer acid bis (amidopropyl-N, N-dimethyl-N-ethylammonium ethosulphate; shell coat DAS; manufactured by Shell), quaternium 70 (stearamidopropyldimethyl (myristyl acetate) ammonium chloride; cerafil 70: International Specialty Co., Ltd.), Quotanium 72 (Incrosoft CFI75; Kuroda Corp.), Quotanium 73 (Photosensitive Element 201; Photosensitive Element Co., Ltd.), Kuotaniu 75 (Levenol conditioner C727; made by Levenstein), quaternium 76 collagen complex (Lexaine QX-3000; made by Inorex), quaternium 77 (Finsoft HCM-100; made by Finetex), quaternium 79 (Mac Pro) NLP; manufactured by McKintile, Inc., quaternium 80 (Covafix 123; manufactured by LCW), quaternium 82 (stepan coat DC1; manufactured by Stepan), quaternium 84 (mackernium NLE; manufactured by McKintile), quaternium 85 (2- Hydroxy-3-((2-hydroxyethyl) (2-((1-oxotetradecyl (amino) ethyl) amino) -N, N, N-trimethyl-1-propaneaminium chloride; amino cation S-36; Kao stock Quotanium 86 (Pecosil SWQ-40; manufactured by Phoenix), Quaterium 87 (Varisoft W575PG; manufactured by Degassa), Quaterium 88 (Necoat DAS-D; manufactured by Arzo), Quotanium 89 (Fincoat CT-P) Preferably made by Finetech), and quaternium 91 (Kurodasoft DBQ; made by Kuroda).
Of these, more preferred are quaternium 33, quaternium 45, quaternium 73, quaternium 80 and quaternium 85.
クオタニウムは、既に化粧品原料として市販されているので、かかる市販品を購入して利用することができる。これらは何れも汎用されている成分であり、その入手は容易である。本発明の皮膚外用剤は、かかる成分の一種のみを含有することもできるし、二種以上を組み合わせて含有することもできる。本発明の皮膚外用剤中のかかる成分の含有量は、総量で、皮膚外用剤全量に対して0.01〜5質量%であることが好ましく、0.05〜3質量%であることがより好ましい。かかる成分の含有量が少なすぎると、前記のメラニン産生抑制物質(還元性の美白成分でありうる)の保存安定性を十分に向上させることが困難な場合があり、多すぎると、効果が頭打ちになり、使用感等を損なう場合があるからである。 Since quaternium is already marketed as a cosmetic raw material, such a commercial product can be purchased and used. These are all commonly used components and are readily available. The skin external preparation of this invention can also contain only 1 type of this component, and can also contain it in combination of 2 or more types. The content of such components in the external preparation for skin of the present invention is a total amount, preferably 0.01 to 5% by mass, more preferably 0.05 to 3% by mass with respect to the total amount of external preparation for skin. preferable. If the content of such a component is too small, it may be difficult to sufficiently improve the storage stability of the melanin production inhibitor (which may be a reducing whitening component). This is because the feeling of use may be impaired.
(3)本発明の皮膚外用剤
本発明の皮膚外用剤は、
1) アスコルビン酸及びその誘導体、アルブチン、トラネキサム酸、4−メトキシサリチル酸、並びにそれらの塩(メラニン産生抑制物質)から選択される1種又は2種以上と、2) クオタニウムから選択される1種又は2種以上とを含有することを特徴とするが、これらの必須成分に加えて、通常皮膚外用剤で使用される任意の成分を含有することができる。
(3) The external preparation for skin of the present invention The external preparation for skin of the present invention comprises:
1) Ascorbic acid and its derivatives, arbutin, tranexamic acid, 4-methoxysalicylic acid, and one or more thereof selected from salts thereof (melanin production inhibitor), and 2) one or more selected from quaternium Although it is characterized by containing 2 or more types, in addition to these essential components, it can contain the arbitrary components normally used with a skin external preparation.
このような成分としては、例えばオイル・ワックス類、炭化水素類、高級脂肪酸類、高級アルコール、合成エステル油類、油剤類、界面活性剤類、多価アルコール類、保湿成分類、増粘剤、粉体類、無機顔料類、パール剤類、有機色素類、有機粉体類、紫外線吸収剤類、低級アルコール類、ビタミン類、生体類似構造を有するポリマーなどが挙げられる。 Examples of such components include oils / waxes, hydrocarbons, higher fatty acids, higher alcohols, synthetic ester oils, oil agents, surfactants, polyhydric alcohols, moisturizing ingredients, thickeners, Examples thereof include powders, inorganic pigments, pearl agents, organic dyes, organic powders, ultraviolet absorbers, lower alcohols, vitamins, and polymers having a biologically similar structure.
オイル・ワックス類としては、例えばマカデミアナッツ油、アボガド油、トウモロコシ油、オリーブ油、ナタネ油、ゴマ油、ヒマシ油、サフラワー油、綿実油、ホホバ油、ヤシ油、パーム油、液状ラノリン、硬化ヤシ油、硬化油、モクロウ、硬化ヒマシ油、ミツロウ、キャンデリラロウ、カルナウバロウ、イボタロウ、ラノリン、還元ラノリン、硬質ラノリン、ホホバロウ等が、
炭化水素類としては、例えば流動パラフィン、スクワラン、プリスタン、オゾケライト、パラフィン、セレシン、ワセリン、マイクロクリスタリンワックス等が、
高級脂肪酸類としては、例えばオレイン酸、イソステアリン酸、ラウリン酸、ミリスチン酸、パルミチン酸、ステアリン酸、ベヘン酸、ウンデシレン酸等が、
高級アルコールとしては、例えばセチルアルコール、ステアリルアルコール、イソステアリルアルコール、ベヘニルアルコール、オクチルドデカノール、ミリスチルアルコール、セトステアリルアルコール等が、
合成エステル油類としては、例えばイソオクタン酸セチル、ミリスチン酸イソプロピル、イソステアリン酸ヘキシルデシル、アジピン酸ジイソプロピル、セバチン酸ジ−2−エチルヘキシル、乳酸セチル、リンゴ酸ジイソステアリル、ジ−2−エチルヘキサン酸エチレングリコール、ジカプリン酸ネオペンチルグリコール、ジ−2−ヘプチルウンデカン酸グリセリン、トリ−2−エチルヘキサン酸グリセリン、トリ−2−エチルヘキサン酸トリメチロールプロパン、トリイソステアリン酸トリメチロールプロパン、テトラ−2−エチルヘキサン酸ペンタンエリトリット等が、
油剤類としては、例えばジメチルポリシロキサン、メチルフェニルポリシロキサン、ジフェニルポリシロキサン等の鎖状ポリシロキサン、オクタメチルシクロテトラシロキサン、デカメチルシクロペンタシロキサン、ドデカメチルシクロヘキサンシロキサン等の環状
ポリシロキサン、アミノ変性ポリシロキサン、ポリエーテル変性ポリシロキサン、アルキル変性ポリシロキサン、フッ素変性ポリシロキサン等の変性ポリシロキサン等のシリコーン油等が好ましく例示できる。
Examples of oils and waxes include macadamia nut oil, avocado oil, corn oil, olive oil, rapeseed oil, sesame oil, castor oil, safflower oil, cottonseed oil, jojoba oil, coconut oil, palm oil, liquid lanolin, hardened coconut oil, hardened Oil, mole, hardened castor oil, beeswax, candelilla wax, carnauba wax, ibotarou, lanolin, reduced lanolin, hard lanolin, jojoba wax, etc.
Examples of hydrocarbons include liquid paraffin, squalane, pristane, ozokerite, paraffin, ceresin, petrolatum, and microcrystalline wax.
Examples of higher fatty acids include oleic acid, isostearic acid, lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, undecylenic acid,
Examples of higher alcohols include cetyl alcohol, stearyl alcohol, isostearyl alcohol, behenyl alcohol, octyldodecanol, myristyl alcohol, cetostearyl alcohol,
Synthetic ester oils include, for example, cetyl isooctanoate, isopropyl myristate, hexyl decyl isostearate, diisopropyl adipate, di-2-ethylhexyl sebacate, cetyl lactate, diisostearyl malate, ethylene di-2-ethylhexanoate Glycol, neopentyl glycol dicaprate, glycerin di-2-heptylundecanoate, glycerin tri-2-ethylhexanoate, trimethylolpropane tri-2-ethylhexanoate, trimethylolpropane triisostearate, tetra-2-ethylhexane Acid pentane erythritol, etc.
Examples of oils include chain polysiloxanes such as dimethylpolysiloxane, methylphenylpolysiloxane, and diphenylpolysiloxane, cyclic polysiloxanes such as octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, and dodecamethylcyclohexanesiloxane, and amino-modified polysiloxanes. Preferred examples include silicone oils such as modified polysiloxanes such as siloxane, polyether-modified polysiloxane, alkyl-modified polysiloxane, and fluorine-modified polysiloxane.
界面活性剤類としては、例えばアニオン界面活性剤類、カチオン界面活性剤類、両性界面活性剤類、非イオン界面活性剤類のいずれでもよい。
アニオン界面活性剤類としては、例えば脂肪酸セッケン(ラウリン酸ナトリウム、パルミチン酸ナトリウム等)、ラウリル硫酸カリウム、アルキル硫酸トリエタノールアミンエーテル等が、
カチオン界面活性剤類としては、例えば塩化ステアリルトリメチルアンモニウム、塩化ベンザルコニウム、ラウリルアミンオキサイド等が、
両性界面活性剤類としては、例えばイミダゾリン系両性界面活性剤(2−ココイル−2−イミダゾリニウムヒドロキサイド−1−カルボキシエチロキシ2ナトリウム塩等)、ベタイン系界面活性剤(アルキルベタイン、アミドベタイン、スルホベタイン等)、アシルメチルタウリン等が、
非イオン界面活性剤類としては、例えばソルビタン脂肪酸エステル類(ソルビタンモノステアレート、セスキオレイン酸ソルビタン等)、グリセリン脂肪酸類(モノステアリン酸グリセリン等)、プロピ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)、硬化ヒマシ油誘導体、グリセリンアルキルエーテル、POEソルビタン脂肪酸エステル類(POEソルビタンモノオレエート、モノステアリン酸ポリオキエチレンソルビタン等)、POEソルビット脂肪酸エステル類(POE−ソルビットモノラウレート等)、POEグリセリン脂肪酸エステル類(POE−グリセリンモノイソステアレート等)、POE脂肪酸エステル類(ポリエチレングリコールモノオレート、POEジステアレート等)、POEアルキルエーテル類(POE2−オクチルドデシルエーテル等)、POEアルキルフェニルエーテル類(POEノニルフェニルエーテル等)、プルロニック型類、POE・POPアルキルエーテル類(POE・POP2−デシルテトラデシルエーテル等)、テトロニック類、POEヒマシ油・硬化ヒマシ油誘導体(POEヒマシ油、POE硬化ヒマシ油等)、ショ糖脂肪酸エステル、アルキルグルコシド等が好ましく例示できる。
As the surfactants, for example, any of anionic surfactants, cationic surfactants, amphoteric surfactants, and nonionic surfactants may be used.
Examples of the anionic surfactants include fatty acid soap (sodium laurate, sodium palmitate, etc.), potassium lauryl sulfate, alkyl sulfate triethanolamine ether, etc.
Examples of cationic surfactants include stearyltrimethylammonium chloride, benzalkonium chloride, laurylamine oxide,
Examples of amphoteric surfactants include imidazoline-based amphoteric surfactants (2-cocoyl-2-imidazolinium hydroxide-1-carboxyethyloxy disodium salt, etc.), betaine surfactants (alkyl betaines, amide betaines). , Sulfobetaine, etc.), acylmethyl taurine, etc.
Nonionic surfactants include, for example, sorbitan fatty acid esters (such as sorbitan monostearate and sorbitan sesquioleate), glycerin fatty acids (such as glyceryl monostearate), and propylene glycol fatty acid esters (such as propylene glycol monostearate). ), Hardened castor oil derivative, glycerin alkyl ether, POE sorbitan fatty acid esters (POE sorbitan monooleate, polyoxyethylene sorbitan monostearate, etc.), POE sorbite fatty acid esters (POE-sorbite monolaurate, etc.), POE glycerin Fatty acid esters (POE-glycerol monoisostearate, etc.), POE fatty acid esters (polyethylene glycol monooleate, POE distearate, etc.), POE alkyl Ethers (POE2-octyldodecyl ether, etc.), POE alkylphenyl ethers (POE nonylphenyl ether, etc.), Pluronic types, POE / POP alkyl ethers (POE / POP2-decyltetradecyl ether, etc.), tetronics, POE castor oil / hardened castor oil derivatives (POE castor oil, POE hardened castor oil, etc.), sucrose fatty acid ester, alkyl glucoside and the like can be preferably exemplified.
多価アルコール類としては、例えばポリエチレングリコール、グリセリン、1,3−ブタンジオール、エリスリトール、ソルビトール、キシリトール、マルチトール、プロピレングリコール、ジプロピレングリコール、ジグリセリン、イソプレングリコール、1,2−ペンタンジオール、2,4−ヘキシレングリコール、1,2−ヘキサンジオール、1,2−オクタンジオール等が、
保湿成分類としては、例えばピロリドンカルボン酸ナトリウム、乳酸、乳酸ナトリウム等が、
増粘剤としては、例えばグアガム、クインスシード、カラギーナン、ガラクタン、アラビアガム、ペクチン、マンナン、デンプン、キサンタンガム、カードラン、メチルセルロース、ヒドロキシエチルセルロース、カルボキシメチルセルロース、メチルヒドロキシプロピルセルロース、コンドロイチン硫酸、デルマタン硫酸、グリコーゲン、ヘパラン硫酸、ヒアルロン酸、ヒアルロン酸ナトリウム、トラガントガム、ケラタン硫酸、コンドロイチン、ムコイチン硫酸、ヒドロキシエチルグアガム、カルボキシメチルグアガム、デキストラン、ケラト硫酸,ローカストビーンガム,サクシノグルカン,カロニン酸,キチン,キトサン、カルボキシメチルキチン、寒天、ポリビニルアルコール、ポリビニルピロリドン、カルボキシビニルポリマー、ポリアクリル酸ナトリウム、ポリエチレングリコール、ベントナイト等が好ましく例示できる。
Examples of polyhydric alcohols include polyethylene glycol, glycerin, 1,3-butanediol, erythritol, sorbitol, xylitol, maltitol, propylene glycol, dipropylene glycol, diglycerin, isoprene glycol, 1,2-pentanediol, 2 , 4-hexylene glycol, 1,2-hexanediol, 1,2-octanediol, etc.
Examples of moisturizing ingredients include sodium pyrrolidonecarboxylate, lactic acid, sodium lactate, etc.
Examples of thickeners include guar gum, quince seed, carrageenan, galactan, gum arabic, pectin, mannan, starch, xanthan gum, curdlan, methyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, methyl hydroxypropyl cellulose, chondroitin sulfate, dermatan sulfate, glycogen , Heparan sulfate, hyaluronic acid, sodium hyaluronate, tragacanth gum, keratan sulfate, chondroitin, mucoitin sulfate, hydroxyethyl guar gum, carboxymethyl guar gum, dextran, kerato sulfate, locust bean gum, succinoglucan, carolinic acid, chitin, chitosan, carboxy Methyl chitin, agar, polyvinyl alcohol, polyvinyl pyrrolidone, carboxy vinyl polymer Sodium polyacrylate, polyethylene glycol, bentonite and the like can be preferably exemplified.
粉体類としては、例えば、表面を処理されていても良い、マイカ、タルク、カオリン、合成雲母、炭酸カルシウム、炭酸マグネシウム、無水ケイ酸(シリカ)、酸化アルミニウ
ム、硫酸バリウム等が、
無機顔料類としては、例えば、表面を処理されていても良い、ベンガラ、黄酸化鉄、黒酸化鉄、酸化コバルト、群青、紺青、酸化チタン、酸化亜鉛が挙げられ、
パール剤類としては、例えば、表面を処理されていても良い、雲母チタン、魚燐箔、オキシ塩化ビスマス等が、
有機色素類としては、例えば、レーキ化されていても良い、赤色202号、赤色228号、赤色226号、黄色4号、青色404号、黄色5号、赤色505号、赤色230号、赤色223号、橙色201号、赤色213号、黄色204号、黄色203号、青色1号、緑色201号、紫色201号、赤色204号等が、
有機粉体類としては、例えば、ポリエチレン末、ポリメタクリル酸メチル、ナイロン粉末、オルガノポリシロキサンエラストマー等が好ましく例示できる。
As powders, for example, the surface may be treated, mica, talc, kaolin, synthetic mica, calcium carbonate, magnesium carbonate, anhydrous silicic acid (silica), aluminum oxide, barium sulfate, etc.
Examples of inorganic pigments include, for example, bengara, yellow iron oxide, black iron oxide, cobalt oxide, ultramarine, bitumen, titanium oxide, and zinc oxide, the surface of which may be treated.
Examples of pearl agents include, for example, mica titanium, fish phosphorus foil, bismuth oxychloride, etc. whose surface may be treated,
Examples of the organic dyes may be raked, red 202, red 228, red 226, yellow 4, blue 404, yellow 5, red 505, red 230, red 223. No., Orange No. 201, Red No. 213, Yellow No. 204, Yellow No. 203, Blue No. 1, Green No. 201, Purple No. 201, Red No. 204, etc.
Preferred examples of organic powders include polyethylene powder, polymethyl methacrylate, nylon powder, organopolysiloxane elastomer, and the like.
紫外線吸収剤類としては、例えばパラアミノ安息香酸系紫外線吸収剤、アントラニル酸系紫外線吸収剤、サリチル酸系紫外線吸収剤、桂皮酸系紫外線吸収剤、ベンゾフェノン系紫外線吸収剤、糖系紫外線吸収剤、2−(2’−ヒドロキシ−5’−t−オクチルフェニル)ベンゾトリアゾール、4−メトキシ−4’−t−ブチルジベンゾイルメタン等が、
低級アルコール類としては、例えばエタノール、イソプロパノール、フェノキシエタノール等が、
ビタミン類としては、例えばビタミンA又はその誘導体、ビタミンB6塩酸塩,ビタミンB6トリパルミテート,ビタミンB6ジオクタノエート,ビタミンB2又はその誘導体,ビタミンB12,ビタミンB15又はその誘導体等のビタミンB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,ビタミンEアセテート等のビタミンE類、ビタミンD類、ビタミンH、パントテン酸、パンテチン、ピロロキノリンキノン等が好ましく例示できる。
生体類似構造を有するポリマーとしては、例えばポリメタクリロイルリジン、ポリグリコシルエチルメタクリレート等が例示できる。
Examples of the UV absorbers include paraaminobenzoic acid UV absorbers, anthranilic acid UV absorbers, salicylic acid UV absorbers, cinnamic acid UV absorbers, benzophenone UV absorbers, sugar UV absorbers, 2- (2′-hydroxy-5′-t-octylphenyl) benzotriazole, 4-methoxy-4′-t-butyldibenzoylmethane, etc.
Examples of lower alcohols include ethanol, isopropanol, and phenoxyethanol.
Examples of vitamins include vitamin A or derivatives thereof, vitamin B6 hydrochloride, vitamin B6 tripalmitate, vitamin B6 dioctanoate, vitamin B2 or derivatives thereof, vitamin B such as vitamin B12, vitamin B15 or derivatives thereof, and α-tocopherol , Β-tocopherol, γ-tocopherol, vitamin E acetates such as vitamin E acetate, vitamin D, vitamin H, pantothenic acid, panthetin, pyrroloquinoline quinone and the like can be preferably exemplified.
Examples of the polymer having a bio-similar structure include polymethacryloyl lysine and polyglycosyl ethyl methacrylate.
これらの任意成分のうち、イソプレングリコール、1,2−ペンタンジオール、1,2−ヘキサンジオール、2,4−ヘキシレングリコール、1,2−オクタンジオール等の抗菌性多価アルコールを本発明の皮膚外用剤に含有させることが好ましい。
かかる抗菌性多価アルコールを含有させることにより、防腐目的で配合されるパラベンなどの一過性の刺激を誘発することのある物質の含有量を、低減または皆無にすることができるからである。このような効果を奏させるために、該抗菌性多価アルコールの好ましい含有量を、総量で、皮膚外用剤全量に対して1〜10質量%とするのが好ましく、2〜7質量%とするのがより好ましい。該抗菌性の多価アルコールは、唯一種を含有されることも出来るし、二種以上を組み合わせて含有されることもできる。
Among these optional components, antibacterial polyhydric alcohols such as isoprene glycol, 1,2-pentanediol, 1,2-hexanediol, 2,4-hexylene glycol and 1,2-octanediol are used in the skin of the present invention. It is preferable to make it contain in an external preparation.
This is because by containing such antibacterial polyhydric alcohol, it is possible to reduce or eliminate the content of a substance that may induce a transient stimulus such as paraben to be blended for antiseptic purposes. In order to exert such effects, the total content of the antibacterial polyhydric alcohol is preferably 1 to 10% by mass, and 2 to 7% by mass with respect to the total amount of the external preparation for skin. Is more preferable. The antibacterial polyhydric alcohol may contain only one species or may contain two or more species in combination.
本発明の皮膚外用剤は、保存安定性が高いという特徴を有するが、これは、第一の必須成分である、前記アスコルビン酸もしくはその誘導体、アルブチン、トラネキサム酸、4−メトキシサリチル酸、またはそれらの塩等のメラニン産生抑制物質(美白成分であり得る)が、第二の必須成分であるクオタニウムにより安定化されるためであると推察される。このことは、後述の実施例においても説明されている。 The skin external preparation of the present invention is characterized by high storage stability, which is the first essential component, ascorbic acid or a derivative thereof, arbutin, tranexamic acid, 4-methoxysalicylic acid, or their It is presumed that melanin production-suppressing substances such as salts (which may be whitening components) are stabilized by quaternium, which is the second essential component. This is also explained in the examples described later.
本発明の皮膚外用剤は、前記した必須成分、任意成分を常法に従って処理することにより製造することができる。
本発明の皮膚外用剤の剤形は、皮膚に塗布することができるものであれば特に限定されず、例えば、可溶化ローション剤形、増粘エッセンス剤形、乳化剤形等を挙げることができる。
The skin external preparation of this invention can be manufactured by processing the above-mentioned essential component and arbitrary component according to a conventional method.
The dosage form of the external preparation for skin of the present invention is not particularly limited as long as it can be applied to the skin, and examples thereof include a solubilized lotion dosage form, a thickening essence dosage form, and an emulsifier form.
本発明の皮膚外用剤はメラニン産生抑制作用を有し、それが皮膚に塗布されることによ
り、塗布部位のメラニン産生の亢進を抑制し、色素沈着の悪化を抑制し、かつ色素沈着を改善しうる。この作用により、美白効果が発現される。従って、本発明の皮膚外用剤はメラニン産生を抑制する作用を訴求したものであることが好ましい。例えば、メラニン産生を抑制する作用を有する旨の表示が該外用剤のパッケージ上に記載される、またはその旨の説明書が該外用剤に添付されていることが好ましい。あるいは宣伝または広告によって、本発明の皮膚外用剤がメラニン産生抑制作用を有することを伝えることもできる。
The external preparation for skin of the present invention has a melanin production inhibitory action, and when applied to the skin, it suppresses the increase in melanin production at the application site, suppresses deterioration of pigmentation, and improves pigmentation. sell. By this action, a whitening effect is exhibited. Therefore, it is preferable that the skin external preparation of this invention appeals the effect | action which suppresses melanin production. For example, it is preferable that an indication of having an action of suppressing melanin production is described on the package of the external preparation, or an instruction to that effect is attached to the external preparation. Or it can also tell that the external preparation for skin of this invention has a melanin production inhibitory effect by advertisement or advertisement.
本発明の皮膚外用剤の用途は、皮膚に外用塗布して使用されるためのものであれば特段の限定はされないが、例えば、化粧料、皮膚外用医薬、皮膚外用雑貨などの用途が好ましく例示でき、中でも化粧料がより好ましい。特に、本発明の皮膚外用剤は医薬部外品の化粧料であることが好ましい。ここで医薬部外品とは、薬事法で定義される医薬部外品をいう。 The use of the external preparation for skin of the present invention is not particularly limited as long as it is intended to be applied to the skin for external use, and examples thereof include, for example, cosmetics, external preparations for skin, sundries for skin use, and the like. Among them, cosmetics are more preferable. In particular, the external preparation for skin of the present invention is preferably a quasi-drug cosmetic. Here, a quasi-drug means a quasi-drug defined by the Pharmaceutical Affairs Law.
医薬部外品である本発明の皮膚外用剤には、薬事法に基づいた表示が付されていることが好ましい。例えば、紫外線などによって増加するメラニンの産生を抑制する作用を有する旨の表示、及びメラニン産生を抑制するための好適な使用法の表示が付されている。
好適な使用法の表示とは、例えば、メラニンの産生が亢進した部位に本発明の化粧料の適量を1日1回乃至は数回塗布すべき旨、及び前記塗布により、火照り、刺激感、ヒリヒリ感を感じた場合には直ちに塗布を中止し、皮膚科医に相談すべき旨の表示が好適に例示できる。この様な表示は、化粧料を充填した容器の裏面或いは包装の裏面に掲示すればよい。能書きに記して添付することも可能である。
The external preparation for skin of the present invention, which is a quasi-drug, preferably has a label based on the Pharmaceutical Affairs Law. For example, a display indicating that it has an action of suppressing the production of melanin that is increased by ultraviolet rays or the like, and a display of a suitable usage for suppressing the production of melanin are given.
The indication of suitable usage includes, for example, that an appropriate amount of the cosmetic of the present invention should be applied once or several times a day to a site where production of melanin is enhanced, and by the application, A display indicating that the application should be stopped immediately and a dermatologist should be consulted can be suitably exemplified when a tingling sensation is felt. Such a display may be posted on the back surface of the container filled with the cosmetic or the back surface of the package. It is also possible to write it down and attach it.
以下に、実施例を挙げて、本発明について更に詳細に説明を加えるが、本発明がかかる実施例にのみ限定されないことは言うまでもない。 Hereinafter, the present invention will be described in more detail with reference to examples, but it is needless to say that the present invention is not limited to such examples.
<実施例1>
以下の表1に示す処方に従って、化粧料(化粧水)を作製した。即ち、処方成分を80℃に加熱し、攪拌、可溶化し、攪拌冷却することにより化粧水を得た。この化粧水を化粧料1とする。
<Example 1>
A cosmetic (lotion) was prepared according to the formulation shown in Table 1 below. That is, the prescription ingredients were heated to 80 ° C., stirred, solubilized, and cooled by stirring to obtain a lotion. This skin lotion is designated as cosmetic 1.
<比較例1〜3>
化粧料1の処方成分であるクオタニウム33を水に置換した化粧水である比較化粧料1、化粧料1の処方成分であるクオタニウム33をポリアクリル酸ナトリウムに置換した化粧水である比較化粧料2、および化粧料1の処方成分であるアスコルビン酸−2−グルコシドを水に置換した化粧水である比較化粧料3を、実施例1と同様の方法で作製した。
<Comparative Examples 1-3>
Comparative cosmetic 1 which is a skin lotion in which quaternium 33 which is a prescription component of cosmetic 1 is replaced with water, and comparative cosmetic 2 which is a skin lotion in which quaternium 33 which is a prescription component of cosmetic 1 is replaced with sodium polyacrylate Comparative cosmetic 3 which is a skin lotion in which ascorbic acid-2-glucoside, which is a formulation component of cosmetic 1, is replaced with water was prepared in the same manner as in Example 1.
<試験例1>
化粧料1および比較化粧料1〜3の高温保存試験を実施した。高温保存試験では、50℃で3週間保存した。対照サンプルとして、化粧料1および比較化粧料1〜3とそれぞれ同じサンプルを5℃で保存した。保存終了後、それぞれのサンプルについて、5℃保存品との色差を、光計測器(「色彩色差計ミノルタCR−300」ミノルタ株式会社製)により測定した。これらの結果を表2に示す。
<Test Example 1>
The high temperature preservation test of cosmetic 1 and comparative cosmetics 1 to 3 was performed. In the high temperature storage test, it was stored at 50 ° C. for 3 weeks. As control samples, the same samples as cosmetic 1 and comparative cosmetics 1 to 3, respectively, were stored at 5 ° C. After completion of storage, the color difference between each sample and the product stored at 5 ° C. was measured with an optical measuring instrument (“Color Difference Meter Minolta CR-300” manufactured by Minolta Co., Ltd.). These results are shown in Table 2.
表2より、試験後の比較化粧料1および2(アスコルビン酸−2−グルコシドを含有)は、比較化粧料3(アスコルビン酸−2−グルコシドを非含有)と比較して、対照との色差が大きいことがわかる。
これに対し、試験後の化粧料1は、アスコルビン酸−2−グルコシドを含有するにもかかわらず、対照との色差が小さい。したがって、クオタニウム33は、アスコルビン酸−2−グルコシドの安定性を向上させており、それにより化粧料の保存安定性を高めていることがわかる。
From Table 2, the comparative cosmetics 1 and 2 (containing ascorbic acid-2-glucoside) after the test had a color difference from the control as compared with the comparative cosmetic 3 (containing no ascorbic acid-2-glucoside). You can see that it ’s big.
On the other hand, although the cosmetic 1 after the test contains ascorbic acid-2-glucoside, the color difference from the control is small. Therefore, it can be seen that the quaternium 33 improves the stability of ascorbic acid-2-glucoside, thereby enhancing the storage stability of the cosmetic.
<実施例2>
下記表3に示す処方に従って、実施例1と同様の方法で、化粧料2〜5(化粧水)を作製した。
<Example 2>
Cosmetics 2 to 5 (lotion) were prepared in the same manner as in Example 1 according to the formulation shown in Table 3 below.
<試験例2>
得られた化粧料2〜5について、試験例1と同様の保存試験を実施したところ、表4に示す結果が得られた。表4から、種々のクオタニウムが、化粧料の保存安定性を高める効果を有することが判る。
<Test Example 2>
About the obtained cosmetics 2-5, when the same storage test as Test Example 1 was implemented, the results shown in Table 4 were obtained. From Table 4, it can be seen that various quaterniums have the effect of enhancing the storage stability of cosmetics.
<実施例3>
下記表5に示す処方に従って、実施例1と同様の方法で、化粧料10〜13(化粧水)を作製した。
<Example 3>
Cosmetics 10 to 13 (lotion) were prepared in the same manner as in Example 1 according to the formulation shown in Table 5 below.
<試験例3>
得られた化粧料6〜9について、試験例1と同様の保存試験を実施した。これらの結果を表6に示す。表6より、種々のメラニン産生抑制物質を含む皮膚外用剤の保存安定性が、クオタニウムによって改善されていることがわかる。
<Test Example 3>
About the obtained cosmetics 6-9, the storage test similar to Test Example 1 was implemented. These results are shown in Table 6. From Table 6, it can be seen that the storage stability of the external preparation for skin containing various melanin production inhibitors is improved by quaternium.
本発明により、安定性に優れる美白化粧料に提供することができる。また、本発明により、美白化粧料の保存を容易にすることができる。 According to the present invention, it is possible to provide a whitening cosmetic composition having excellent stability. Further, according to the present invention, the whitening cosmetic can be easily stored.
Claims (7)
2) クオタニウムから選択される1種又は2種以上
とを含有することを特徴とする皮膚外用剤。 1) One or more selected from ascorbic acid and its derivatives, arbutin, tranexamic acid, 4-methoxysalicylic acid, and salts thereof;
2) A skin external preparation characterized by containing one or more selected from quaternium.
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| JP2004225501A JP2006045080A (en) | 2004-08-02 | 2004-08-02 | Skin care preparation suitable as quasi-drug |
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| JP2004225501A JP2006045080A (en) | 2004-08-02 | 2004-08-02 | Skin care preparation suitable as quasi-drug |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015151379A (en) * | 2014-02-18 | 2015-08-24 | 株式会社ノエビア | Aqueous cleansing fee |
| WO2023079779A1 (en) * | 2021-11-07 | 2023-05-11 | 株式会社ドクターズチョイス | Compound containing ascorbic acid derivative |
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| JP2002302419A (en) * | 2001-03-30 | 2002-10-18 | Aldeep Cosmetics Japan Inc | Cosmetic composition |
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| JPH06500079A (en) * | 1991-06-27 | 1994-01-06 | ジヨンソン・アンド・ジヨンソン・コンシユーマー・プロダクツ・インコーポレーテツド | skin care composition |
| JPH11181422A (en) * | 1997-12-18 | 1999-07-06 | Aquas Corp | Oxidizing substance remover in water |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JP2015151379A (en) * | 2014-02-18 | 2015-08-24 | 株式会社ノエビア | Aqueous cleansing fee |
| WO2023079779A1 (en) * | 2021-11-07 | 2023-05-11 | 株式会社ドクターズチョイス | Compound containing ascorbic acid derivative |
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