JP2011241228A - Skin preparation for external use - Google Patents

Skin preparation for external use Download PDF

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JP2011241228A
JP2011241228A JP2011181088A JP2011181088A JP2011241228A JP 2011241228 A JP2011241228 A JP 2011241228A JP 2011181088 A JP2011181088 A JP 2011181088A JP 2011181088 A JP2011181088 A JP 2011181088A JP 2011241228 A JP2011241228 A JP 2011241228A
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skin
present
hinokitiol
external preparation
external use
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Yoko Tashiro
容子 田代
Kazuto Ishida
和人 石田
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Kishohin Kagaku Kaiho Kenkyusho KK
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Kishohin Kagaku Kaiho Kenkyusho KK
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Abstract

PROBLEM TO BE SOLVED: To provide a skin preparation for external use preventing development of or improving a wrinkle due to skin dryness, skin roughness, decline of skin firmness and elasticity.SOLUTION: There is provided the skin preparation for external use, that includes: (a) retinol palmitate; (b) hinokitiol and/or a derivative thereof; and (c) epidermal lipid and/or a similar ingredient thereof.

Description

本発明は皮膚外用剤に関し、詳しくは皮膚の乾燥、あれ肌、皮膚のハリや弾力の低下に伴う小じわ等の形成予防および改善に有効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 effective for preventing and improving the formation of dry skin, rough skin, fineness of skin, fine lines and the like due to a decrease in elasticity.

皮膚の乾燥、あれ肌、皮膚のハリや弾力の低下に伴う小じわ等は、加齢や日光曝露に加え、皮膚の血行不良による栄養不十分、不規則な生活、あやまったお手入れ、また、寒冷や乾燥等の環境要因などによって起こる。そこで、皮膚の乾燥、あれ肌、小じわ等の予防・改善を目的とし、種々の薬効成分の開発が求められてきた。   Skin dryness, rough skin, fineness caused by reduced skin elasticity and elasticity, etc. are caused by inadequate nutrition due to poor blood circulation of the skin, irregular life, ill-care, and coldness in addition to aging and sun exposure. It occurs due to environmental factors such as dryness. Therefore, development of various medicinal ingredients has been demanded for the purpose of preventing and improving dry skin, rough skin, fine wrinkles and the like.

近年、レチノール、ビタミンA酸やその誘導体等によるしわ改善技術が、このような皮膚の乾燥、あれ肌、小じわ等の予防・改善を目的とし使用されているが、その小じわ等の改善効果はいまだ十分とはいえない。よって、更なる、優れた効果のある皮膚外用剤の開発が待望されている。 In recent years, wrinkle improvement technology using retinol, vitamin A acid and its derivatives has been used for the purpose of preventing and improving such dry skin, rough skin, fine lines, etc. Not enough. Therefore, the development of a skin external preparation having further excellent effects is awaited.

こうした中、天然物から抽出した各種成分が配合された皮膚外用剤の開発や皮膜形成剤によって物理的にしかも一時的にしわを伸ばす方法などがその改善法として使われてきたが、いまだ不十分である。 Under these circumstances, the development of external preparations for skin containing various ingredients extracted from natural products and the method of physically and temporarily wrinkling with a film-forming agent have been used as improvement methods, but they are still insufficient. It is.

したがって、本発明の目的は皮膚の乾燥、あれ肌、皮膚のハリや弾力の低下に伴う小じわ等の発生を予防又は改善することのできる皮膚外用剤を提供することにある。   Accordingly, an object of the present invention is to provide an external preparation for skin which can prevent or improve the occurrence of dry skin, rough skin, skin firmness and fine lines associated with a decrease in elasticity.

前記目的を達成するために、本発明者らは安全性に優れた物質の中から、皮膚の乾燥、あれ肌、皮膚のハリや弾力の低下に伴う小じわ等の改善効果を発現させる物質を得るべく、鋭意研究を重ねた結果、ビタミンA、ヒノキチオール、並びに表皮脂質を含有する事によって、これらの問題点を解決し、本発明を完成するに至った。 In order to achieve the above-mentioned object, the present inventors obtain a substance that exhibits an improvement effect such as dry skin, rough skin, firmness of the skin, fine wrinkles associated with a decrease in elasticity, among substances having excellent safety. Therefore, as a result of intensive research, these problems were solved by containing vitamin A, hinokitiol, and epidermal lipid, and the present invention was completed.

すなわち本発明は(A)パルミチン酸レチノール、(B)ヒノキチオール、並びに(C)表皮脂質成分であるステロール、スフィンゴ脂質及びグリセリドから選ばれた少なくとも一種以上の物質を含有することを特徴とする皮膚外用剤を提供するものである。以下、本発明の構成について詳述する。   That is, the present invention contains at least one substance selected from (A) retinol palmitate, (B) hinokitiol, and (C) sterol, sphingolipid and glyceride, which are epidermal lipid components. An agent is provided. Hereinafter, the configuration of the present invention will be described in detail.

本発明に用いられるパルミチン酸レチノールとはビタミンA誘導体である。ビタミンAは、通常、皮膚角化症等の予防や治療、さらには皮膚老化、特にしわ等の防止や回復に有効な成分として利用されている化合物である。これらの中で、レチノール、レチナール、レチノイン酸等、その各種異性体もしくはその誘導体(パルミチン酸レチノール、酢酸レチノール等)がとりわけ好ましい。 The retinol palmitate used in the present invention is a vitamin A derivative. Vitamin A is a compound that is usually used as an effective component for the prevention and treatment of cutaneous keratosis and the like, as well as the prevention and recovery of skin aging, especially wrinkles. Among these, various isomers such as retinol, retinal, retinoic acid, and derivatives thereof (retinol palmitate, retinol acetate, etc.) are particularly preferable.

本発明の皮膚外用剤へのパルミチン酸レチノールの配合量については限定しないが、0.001重量%〜5.0重量%が好ましく、さらには0.01重量%〜1.0重量%がより好ましい。 The amount of retinol palmitate added to the external preparation for skin of the present invention is not limited, but is preferably 0.001% to 5.0% by weight, more preferably 0.01% to 1.0% by weight. .

本発明に用いられるヒノキチオールとはβ―ツヤプリシンとも呼ばれるトロポロン化合物で、天然には青森ヒバや台湾ヒノキの精油から抽出される成分である。ヒノキチオールは天然、合成に関わらず、通常、医薬品、化粧品等の分野で殺菌剤、細胞賦活剤等として幅広く利用されている化合物である。ヒノキチオールもしくはその誘導体がとりわけ好ましい。 The hinokitiol used in the present invention is a tropolone compound also called β-tsuyapricin, which is a component naturally extracted from essential oils of Aomori Hiba and Taiwan Hinoki. Hinokitiol is a compound that is widely used as a bactericidal agent, cell activator, etc., in the fields of pharmaceuticals, cosmetics, etc., regardless of whether it is natural or synthetic. Hinokitiol or its derivatives are particularly preferred.

本発明の皮膚外用剤へのヒノキチオールの配合量については限定しないが、0.0001重量%〜2.0重量%が好ましく、さらには0.0005重量%〜0.5重量%がより好ましい。 The amount of hinokitiol added to the external preparation for skin of the present invention is not limited, but is preferably 0.0001% by weight to 2.0% by weight, and more preferably 0.0005% by weight to 0.5% by weight.

本発明に用いられる表皮脂質とは、皮膚に存在する脂質の総称であり、通常、医薬品、化粧品等の分野で基剤、エモリエント剤として幅広く利用されている成分である。これらの中で、ステロール類及び/又はその誘導体、スフィンゴ脂質及び/又はその誘導体、リン脂質及び/又はその誘導体、グリセライド及び/又はその誘導体がとりわけ好ましい。 The epidermal lipid used in the present invention is a general term for lipids existing in the skin, and is a component that is generally widely used as a base or an emollient in fields such as pharmaceuticals and cosmetics. Among these, sterols and / or derivatives thereof, sphingolipids and / or derivatives thereof, phospholipids and / or derivatives thereof, glycerides and / or derivatives thereof are particularly preferable.

また、ステロール類としては、コレステロール、デヒドロコレステロール、エルゴステロール、シトステロール、カンペステロール、スチグマステロール、ブラシカステロール、フコステロール等、誘導体としてはそのエステル等が挙げられる。 In addition, examples of sterols include cholesterol, dehydrocholesterol, ergosterol, sitosterol, campesterol, stigmasterol, brassicasterol, and fucosterol, and derivatives include esters thereof.

また、スフィンゴ脂質としては、スフィンゴシン、スフィンゴミエリン、スフィンゴ糖脂質、セレブロシド、フィトスフィンゴシン、セラミド1、セラミド2、セラミド3、セラミド4、セラミド5、セラミド6等とその誘導体が挙げられる。 Examples of sphingolipids include sphingosine, sphingomyelin, glycosphingolipid, cerebroside, phytosphingosine, ceramide 1, ceramide 2, ceramide 3, ceramide 4, ceramide 5, ceramide 6 and their derivatives.

また、リン脂質としては、フォスファチジルコリン、リゾフォスファチジルコリン、フォスファチジルエタノールアミン、フォスファチジルイノシトール等とその誘導体が挙げられる。 Examples of phospholipids include phosphatidylcholine, lysophosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, and their derivatives.

また、グリセリドとしてはモノグリセリド、ジグリセリド、トリグリセリド等、動植物由来の油脂類とその誘導体が挙げられる。 Examples of glycerides include oils and fats derived from animals and plants such as monoglycerides, diglycerides and triglycerides, and derivatives thereof.

本発明の皮膚外用剤への表皮脂質及び/又はその類似成分の配合量については限定しないが、0.01重量%〜20.0重量%が好ましく、さらには0.1重量%〜10.0重量%がより好ましい。 The blending amount of the epidermal lipid and / or a similar component in the external preparation for skin of the present invention is not limited, but is preferably 0.01% to 20.0% by weight, more preferably 0.1% to 10.0%. Weight percent is more preferred.

本発明の皮膚外用剤は前記の必須成分に加えて、必要に応じ、本発明の効果を損なわない範囲内で、化粧料、医薬部外品、医薬品等に一般に用いられる各種成分、水性成分、保湿剤、増粘剤、紫外線吸収剤、紫外線散乱剤、防腐剤、酸化防止剤、香料、色剤、薬剤、生薬等が配合される。また、本発明の皮膚外用剤の剤型は任意であり、例えば化粧水等の可溶化系、乳液、クリーム等の乳化系、あるいは軟膏、粉末分散系、水―油二層系、水―油―粉三層系等のような剤系でもかまわない。 In addition to the essential components described above, the external preparation for skin of the present invention, if necessary, within the range not impairing the effects of the present invention, various components commonly used in cosmetics, quasi drugs, pharmaceuticals, etc., aqueous components, Moisturizers, thickeners, UV absorbers, UV scattering agents, preservatives, antioxidants, fragrances, colorants, drugs, herbal medicines, and the like are blended. The dosage form of the external preparation for skin of the present invention is arbitrary, for example, a solubilizing system such as lotion, an emulsifying system such as an emulsion or cream, or an ointment, a powder dispersion system, a water-oil two-layer system, a water-oil -An agent system such as a powder three-layer system may be used.

本発明の実施例を以下にあげて説明するが、これらは本発明を限定するものではない。なお、各製剤は80℃に加温した水相に同温度に加温した油相を加え、攪拌乳化し、室温まで冷却し調整した。 Examples of the present invention will be described below, but these examples do not limit the present invention. Each formulation was prepared by adding an oil phase heated to the same temperature to an aqueous phase heated to 80 ° C., stirring and emulsifying, and cooling to room temperature.

下記の組成物を製造し、あれ肌改善効果について検討した。あれ肌は、皮膚の乾燥が要因で生じ、放置すると小じわやしわへと進行することが知られている。 The following composition was manufactured and the skin improvement effect was examined. It is known that such skin is caused by dryness of the skin and progresses to fine lines and wrinkles when left untreated.

Figure 2011241228
<あれ肌改善試験方法> 人の前腕部(3cm×3cm)に10%ラウリル硫酸ナトリウム水溶液を、6時間閉鎖発布し、あれ肌モデルを作成する。実施例1、比較例1〜7をそれぞれ、0.05gずつ1日3回塗布し、4日後、8日後のあれ肌部を肉眼判定および角質水分量の測定により改善度の評価を行った。角質水分量の測定は、皮表角質水分量測定装置:SKICON−200(アイ・ビー・エス株式会社製)で行った。その結果を表2、表3に示す。
Figure 2011241228
<That Skin Improvement Test Method> A 10% sodium lauryl sulfate aqueous solution is closed and promulgated on a human forearm (3 cm × 3 cm) for 6 hours to create a skin model. Example 1 and Comparative Examples 1 to 7 were each applied 0.05 g three times a day, and the degree of improvement was evaluated by visual inspection and measurement of the amount of keratinous moisture after 4 and 8 days. The stratum corneum moisture content was measured with a skin surface stratum corneum moisture measuring device: SKICON-200 (manufactured by IBS Co., Ltd.). The results are shown in Tables 2 and 3.

Figure 2011241228
Figure 2011241228

Figure 2011241228
Figure 2011241228

表2、3の結果から明らかなように実施例1の本発明は比較例1〜7のものに比べて優れたあれ肌改善効果を有していることがわかった。 As is clear from the results of Tables 2 and 3, it was found that the present invention of Example 1 had an excellent skin improvement effect as compared with those of Comparative Examples 1-7.

Figure 2011241228
Figure 2011241228

次に、表4の組成物(実施例2、比較例8〜10)の処方を常法により調整し、2ヶ月間の実使用試験を行った。パネラーとしては皮膚の乾燥、小じわ等の症状を顕著に呈する30代後半〜50代の女性20名を用いた。これらの組成物は1日朝、晩2回、2ヶ月間使用してもらい、使用試験開始前および使用試験終了後に皮膚の状況について「改善した」、「やや改善」、「変化なし」の3段階にて評価した。試験の結果は各評価を得たパネラー数にて表5に示した。 Next, the formulation of the composition of Table 4 (Example 2, Comparative Examples 8 to 10) was adjusted by a conventional method, and an actual use test for 2 months was performed. As panelists, 20 women in their late 30's to 50's who had marked symptoms such as dry skin and fine lines were used. These compositions are used twice a day in the morning and evening for 2 months, and the skin condition is “improved”, “slightly improved”, and “no change” before the start of use test and after the end of use test. Evaluated. The results of the test are shown in Table 5 as the number of panelists that obtained each evaluation.

Figure 2011241228
表5に示されるように、皮膚の乾燥、ハリ・弾力性の低下、小じわ等の改善状況については、実施例2の本発明は比較例8〜10のものに比べて格段に優れた小じわ等の改善効果を有していることが認められた。また、実施例使用群において、皮膚刺激性反応や皮膚感作性反応を示したパネラーも存在しなかった。
Figure 2011241228
As shown in Table 5, with regard to the improvement status of skin dryness, reduction of elasticity / elasticity, fine wrinkles, etc., the present invention of Example 2 is significantly superior to those of Comparative Examples 8-10. It was confirmed to have an improvement effect. In addition, there was no panel exhibiting a skin irritation reaction or a skin sensitization reaction in the example use group.

次に、本発明のビタミンA、ヒノキチオール、並びに表皮脂質を配合した、皮膚外用剤の処方例を示す。 Next, the formulation example of the skin external preparation which mix | blended vitamin A of this invention, hinokitiol, and epidermal lipid is shown.

化粧水
パルミチン酸レチノール 0.01(重量%)
ヒノキチオール 0.001
水素添加大豆リン脂質 0.1
ヒドロキシエチルセルロール 0.1
1,3−ブチレングリコール 3.0
パラベン 0.2
ポリオキシエチレン硬化ヒマシ油 0.3
アルコール 10.0
植物エキス 0.5
香料 0.03
精製水 残 量
Lotion Toner Retinol Palmitate 0.01 (wt%)
Hinokitiol 0.001
Hydrogenated soybean phospholipid 0.1
Hydroxyethyl cellulose 0.1
1,3-butylene glycol 3.0
Paraben 0.2
Polyoxyethylene hydrogenated castor oil 0.3
Alcohol 10.0
Plant extract 0.5
Perfume 0.03
Purified water balance

乳液
酢酸レチノール 0.1(重量%)
ヒノキチオール 0.01
フォスファチジルエタノールアミン 0.5
セラミド3 0.01
カルボキシビニルポリマー 0.3
1,3−ブチレングリコール 5.0
パラベン 0.2
ポリオキシエチレン硬化ヒマシ油 0.1
ポリグリセリン脂肪酸エステル 1.0
ポリオキシエチレンソルビタン脂肪酸エステル 0.3
流動パラフィン 3.0
水酸化カリウム 0.07
植物エキス 0.5
香料 0.03
精製水 残 量
Latex Retinol acetate 0.1 (wt%)
Hinokitiol 0.01
Phosphatidylethanolamine 0.5
Ceramide 3 0.01
Carboxyvinyl polymer 0.3
1,3-butylene glycol 5.0
Paraben 0.2
Polyoxyethylene hydrogenated castor oil 0.1
Polyglycerin fatty acid ester 1.0
Polyoxyethylene sorbitan fatty acid ester 0.3
Liquid paraffin 3.0
Potassium hydroxide 0.07
Plant extract 0.5
Perfume 0.03
Purified water balance

クリーム
レチノール 0.1(重量%)
ヒノキチオール 0.1
コレステロール 1.0
リゾフォスファチジルコリン 0.1
オリーブ油 2.0
グリセリン 15.0
パラベン 0.2
カルボキシビニルポリマー 0.3
ポリオキシエチレン硬化ヒマシ油 0.1
モノグリセリン脂肪酸エステル 5.0
プロピレングリコール脂肪酸エステル 5.0
ポリエチレングリコール脂肪酸エステル 0.5
スクワラン 10.0
ベヘニルアルコール 3.0
ステアリン酸 1.0
植物エキス 0.5
香料 0.03
精製水 残 量
Cream Retinol 0.1 (wt%)
Hinokitiol 0.1
Cholesterol 1.0
Rhizophosphatidylcholine 0.1
Olive oil 2.0
Glycerin 15.0
Paraben 0.2
Carboxyvinyl polymer 0.3
Polyoxyethylene hydrogenated castor oil 0.1
Monoglycerin fatty acid ester 5.0
Propylene glycol fatty acid ester 5.0
Polyethylene glycol fatty acid ester 0.5
Squalane 10.0
Behenyl alcohol 3.0
Stearic acid 1.0
Plant extract 0.5
Perfume 0.03
Purified water balance

美容液
酢酸レチノール 0.1(重量%)
ヒノキチオール 0.001
サフラワー油 1.0
セラミド3 0.01
ヒドロキシエチルセルロース 0.6
ジプロピレングリコール 10.0
パラベン 0.2
ポリオキシエチレン硬化ヒマシ油 0.1
ポリグリセリン脂肪酸エステル 2.0
ポリオキシエチレンソルビタン脂肪酸エステル 0.5
スクワラン 5.0
ステアリン酸 1.0
植物エキス 0.5
香料 0.03
精製水 残 量
Cosmetic liquid Retinol acetate 0.1 (wt%)
Hinokitiol 0.001
Safflower oil 1.0
Ceramide 3 0.01
Hydroxyethyl cellulose 0.6
Dipropylene glycol 10.0
Paraben 0.2
Polyoxyethylene hydrogenated castor oil 0.1
Polyglycerin fatty acid ester 2.0
Polyoxyethylene sorbitan fatty acid ester 0.5
Squalane 5.0
Stearic acid 1.0
Plant extract 0.5
Perfume 0.03
Purified water balance

以上詳述したように、本発明の皮膚外用剤は、皮膚の乾燥、あれ肌、皮膚のハリや弾力の低下に伴う小じわ等の予防・改善において、他の組成と比較して格段に優れた効果を示すものである。   As described above in detail, the external preparation for skin of the present invention is remarkably superior to other compositions in preventing and improving dry skin, rough skin, skin firmness and fine lines caused by reduced elasticity. It shows the effect.

表3によって示されたあれ肌の角質水分量の経時的変化を示す。The change with time of the amount of keratin moisture of that skin shown by Table 3 is shown.

Claims (2)

(A)パルミチン酸レチノール、(B)ヒノキチオール、並びに(C)表皮脂質成分であるステロール、スフィンゴ脂質及びグリセリドから選ばれた少なくとも一種以上の物質を含有することを特徴とする皮膚外用剤。 A skin external preparation characterized by containing at least one or more substances selected from (A) retinol palmitate, (B) hinokitiol, and (C) sterol, sphingolipid and glyceride which are epidermal lipid components. 前記(C)成分としてフィトステロール、セラミド2及びメドフォーム油の三種を含有することを特徴とする皮膚外用剤。 A skin external preparation characterized by containing three types of phytosterol, ceramide 2 and medofoam oil as the component (C).
JP2011181088A 2011-08-23 2011-08-23 Skin preparation for external use Pending JP2011241228A (en)

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JP2019019101A (en) * 2017-07-20 2019-02-07 クラシエホームプロダクツ株式会社 Skin Cosmetic

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Publication number Priority date Publication date Assignee Title
JP2019019100A (en) * 2017-07-20 2019-02-07 クラシエホームプロダクツ株式会社 Skin Cosmetic
JP2019019101A (en) * 2017-07-20 2019-02-07 クラシエホームプロダクツ株式会社 Skin Cosmetic
JP7343885B2 (en) 2017-07-20 2023-09-13 クラシエホームプロダクツ株式会社 skin cosmetics

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