JP4647733B2 - Transdermal absorption-enhancing topical agent - Google Patents
Transdermal absorption-enhancing topical agent Download PDFInfo
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- JP4647733B2 JP4647733B2 JP05241399A JP5241399A JP4647733B2 JP 4647733 B2 JP4647733 B2 JP 4647733B2 JP 05241399 A JP05241399 A JP 05241399A JP 5241399 A JP5241399 A JP 5241399A JP 4647733 B2 JP4647733 B2 JP 4647733B2
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- Prior art keywords
- fatty acid
- branched fatty
- acid
- transdermal absorption
- external preparation
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- Cosmetics (AREA)
Description
【０００１】
【発明の属する技術分野】
本発明は経皮吸収促進外用剤に関する。更に詳しくは、含有する低分子水溶性有効成分の経皮吸収性を高め、肌への有効性を向上させる経皮吸収促進外用剤に関する。
【０００２】
【従来の技術および発明が解決しようとする課題】
皮膚に対し有効性を示す組成物には、荒れ肌改善物質であるジイソプロピルアミンジクロロアセテートやコラーゲン産生促進物質であるアスコルビン酸誘導体など水溶性物質が多く含まれる。一方、一般に水溶性物質は油溶性物質に比較して経皮吸収性が低い。そこで、水溶性物質の経皮吸収性を高めるの検討が行われている。これまでにも経皮吸収促進剤としてＤＭＳＯのような物質非プロトン溶媒やＡＺＯＮＥ、テルペン類、メントール類などが報告されており、本出願人は、先に、セスキテルペン類を配合した経皮吸収促進効果を有する養毛料の毛成長効果を有することを見出し（特開平６−１３５８２１号公報）、提案した。ところが、これらを配合した製剤は表皮にダメージを与えたり、刺激を感じるなど皮膚外用剤として好ましくない場合がある。本発明は、このような実情に鑑みなされたものであって、皮膚への刺激が少なく有効性の高い皮膚外用剤を提供することを目的とするものである。
【０００３】
【課題を解決するための手段】
上記の目的を達成するための本発明の請求項１は、大豆由来の分岐脂肪酸を含有することを特徴とする経皮吸収促進外用剤である。また、本発明の請求項２は、１０℃において澄明な性状を呈する大豆由来の分岐脂肪酸を含有することを特徴とする経皮吸収促進外用剤である。
【０００４】
【発明の実施の形態】
以下、発明の実施の形態について詳述する。
【０００５】
本発明の大豆由来の分岐脂肪酸は、大豆油から加水分解を経て得られる分岐脂肪酸画分、及び大豆油を原料とするダイマー酸の製造における副産物として生成する分岐脂肪酸画分である。特に、１０℃において澄明な性状を呈する大豆由来の分岐脂肪酸が望ましい。
尚、１０℃において澄明な性状を呈する大豆由来の分岐脂肪酸は、大豆由来の分岐脂肪酸を１０℃において遠心分離によって沈殿物を単離して得られる。これらの大豆由来の分岐脂肪酸の本発明の経皮吸収促進外用剤中の配合量は、その総量を基準として０．０１〜３０重量％（下記の実施例等の数値は総量中のｗｔ％である）が好ましい。
【０００６】
経皮吸収が促進される事を目的として、本発明の経皮吸収促進外用剤に配合される低分子水溶性有効成分としては、皮膚に対して改善効果が見られるものであり、例えばジイソプロピルアミン塩、尿素、デカルボキシカルノシン等の有機アミン類、メバロン酸、グリチルリチン酸等の有機酸及びその塩、硫酸ナトリウム、メタ珪酸ナトリウム、塩化カルシウム等の無機塩類、セリン、スレオニン、γ−アミノ酪酸、β−ヒドロキシ−γ−アミノ酪酸等のアミノ酸、Ｎ−メチル−Ｌ−セリン、ザルコシン等のアミノ酸誘導体、Ｎ−アセチルグルコサミンおよびそのオリゴマー、アスコルビン酸、ナイアシン、ビオチン等の水溶性ビタミン類およびアスコルビン酸硫酸エステル塩、アスコルビン酸燐酸エステル塩等のビタミン誘導体類等を用いる事が出来る。
【０００７】
本発明の経皮吸収促進外用剤は医薬品、医薬部外品、化粧品等に適用でき、剤形としては例えば、化粧水、乳液類、クリーム類、パック類、化粧油、マッサージ類等に適用することができる。
【０００８】
尚、本発明の経皮吸収促進外用剤には上記の他にタール系色素、酸化鉄などの着色顔料、パラベン、フェノキシエタノールなどの防腐剤、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、環状シリコーン等のシリコーン油、パラフィン、ワセリン等の炭化水素類、オリーブスクワラン、米スクワラン、米胚芽油、ホホバ油、ヒマシ油、紅花油、オリーブ油、マカデミアナッツ油、ヒマワリ油などの植物油、ミツロウ、モクロウ、カルナバロウ等のロウ類、ミリスチン酸オクチルドデシル、パルミチン酸セチル、イソステアリン酸イソステアリル、ミリスチン酸イソプロピル等のエステル油、エタノール等の低級アルコール類、セタノール、ベヘニルアルコール、ステアリルアルコール、長鎖分岐脂肪族アルコール等の高級アルコール類、コレステロール、フィトステロール、分岐脂肪酸コレステロールエステル、マカデミアナッツ脂肪酸フィトステリルエステル等のステロール類及び誘導体、硬化油等の加工油類、ステアリン酸、ミリスチン酸、イソステアリン酸、オレイン酸、イソ型長鎖脂肪酸、アンテイソ型長鎖脂肪酸などの高級脂肪酸、リモネン、水素添加ビサボロール等のテルペン類、トリカプリル・カプリン酸グリセリル、２−エチルヘキサン酸グリセリル、トリイソ型長鎖脂肪酸グリセリル、トリパルミチン酸グリセリルなどのトリグリセリド、セチル硫酸ナトリウム、Ｎ−ステアロイル−Ｌ−グルタミン酸塩などの陰イオン界面活性剤、ポリオキシエチレンアルキルエーテル、ポリオキシエチレン脂肪酸エステル、ポリオキシエチレン多価アルコール脂肪酸エステル、ポリオキシエチレン硬化ヒマシ油、多価アルコール脂肪酸エステル、ポリグリセリン脂肪酸エステル、変性シリコン、蔗糖エステルなどの非イオン界面活性剤、テトラアルキルアンモニウム塩などの陽イオン界面活性剤、ベタイン型、スルホベタイン型、スルホアミノ酸型などの両性界面活性剤、レシチン、リゾフォスファチジルコリン、セラミド、セレブロシドなどの天然系界面活性剤、酸化チタン、酸化亜鉛などの顔料、ジブチルヒドロキシトルエンなどの抗酸化剤、ヒドロキシメトキシベンゾフェノンスルフォン酸塩等の紫外線吸収剤、ジプロピレングリコール、１，３ブチレングリコール、グリセリン、プロピレングリコール、ソルビトール、マルビトール、ジグリセリン、ラフィノースなどの多価アルコール等が挙げられるがこれに限定されるものではない。
【０００９】
【実施例】
以下、実施例及び比較例に基づいて本発明を詳細に説明する。尚、実施例に記載の経皮吸収量測定方法、荒れ肌改善試験は下記の通りである。
【００１０】
経皮吸収量測定方法
ヘアレスラットの腹部皮膚を装着したフランツ型垂直セルの角質層側に１４Ｃでラベルしたジイソプロピルアミン２０００００ｄｐｍを含有する試料を供し、８時間後の透過量を液体シンチレーションカウンターにて測定して累積透過率を計算した。
【００１１】
荒れ肌改善試験
試料を成人女性30名の顔面に塗布して（一日２回）３週間後の荒れ肌の改善の見られた人数にて示した。
【００１２】
【表１】
【表２】
実施例１〜３、比較例１〜４
表１に記載の分岐脂肪酸を用い、実施例及び比較例の組成物を表２の組成にもとづき組成物を調製し、それを試料として前記の諸実験を実施した。
【００１５】
各実施例及び比較例の組成物を試料とした試験の結果を表２に示す。このように、大豆由来の分岐脂肪酸を含有する実施例１、３の組成物は、由来の異なる分岐脂肪酸、直鎖脂肪酸をそれぞれ用いた比較例１〜３および脂肪酸を含まない比較例４の各組成物に比べて優れた経皮吸収促進性、荒れ肌改善効果を示す。
また、１０℃において澄明な性状を呈する大豆由来の分岐脂肪酸を含有する実施例２の組成物は、実施例１の組成物に比べてさらに優れた経皮吸収促進性、荒れ肌改善効果を示す。
【００１６】
【発明の効果】
以上記載のごとく、本発明が、低分子水溶性有効成分の経皮吸収性を高める経皮吸収促進外用剤を提供することは明らかである。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to an external preparation for promoting transdermal absorption. More specifically, the present invention relates to an external preparation for promoting percutaneous absorption that enhances the percutaneous absorbability of the contained low molecular weight water-soluble active ingredient and improves the effectiveness on the skin.
[0002]
[Background Art and Problems to be Solved by the Invention]
Compositions that are effective against the skin are rich in water-soluble substances such as diisopropylamine dichloroacetate, which is a rough skin improving substance, and ascorbic acid derivatives, which are collagen production promoting substances. On the other hand, water-soluble substances are generally less transdermally absorbable than oil-soluble substances. In view of this, studies have been made to increase the transdermal absorbability of water-soluble substances. There have been reported aprotic solvents such as DMSO, AZONE, terpenes, menthols and the like as transdermal absorption accelerators, and the present applicant has previously described transdermal absorption containing sesquiterpenes. It has been found and proposed that a hair nourishing agent having an accelerating effect has a hair growth effect (Japanese Patent Laid-Open No. 6-135821). However, preparations containing these may not be preferable as external preparations for skin, such as damaging the epidermis or feeling irritation. This invention is made | formed in view of such a situation, Comprising: It aims at providing the skin external preparation with little irritation | stimulation to skin and high effectiveness.
[0003]
[Means for Solving the Problems]
In order to achieve the above object, claim 1 of the present invention is an external preparation for promoting percutaneous absorption characterized by containing a branched fatty acid derived from soybean. Further, claim 2 of the present invention is an external preparation for promoting percutaneous absorption characterized by containing a branched fatty acid derived from soybean that exhibits a clear property at 10 ° C.
[0004]
DETAILED DESCRIPTION OF THE INVENTION
Hereinafter, embodiments of the present invention will be described in detail.
[0005]
The branched fatty acid derived from soybean of the present invention is a branched fatty acid fraction obtained by hydrolysis from soybean oil, and a branched fatty acid fraction produced as a by-product in the production of dimer acid using soybean oil as a raw material. In particular, a branched fatty acid derived from soybean that exhibits clear properties at 10 ° C. is desirable.
In addition, the branched fatty acid derived from soybean exhibiting clear properties at 10 ° C. is obtained by isolating a precipitate from the branched fatty acid derived from soybean at 10 ° C. The blended amount of these soy-derived branched fatty acids in the external preparation for promoting percutaneous absorption of the present invention is 0.01 to 30% by weight based on the total amount (the numerical values of the following examples and the like are wt% in the total amount). Is preferred).
[0006]
For the purpose of promoting percutaneous absorption, the low-molecular water-soluble active ingredient blended in the percutaneous absorption promoting external preparation of the present invention has an improvement effect on the skin, for example, diisopropylamine. Salts, organic amines such as urea and decarboxycarnosine, organic acids such as mevalonic acid and glycyrrhizic acid and salts thereof, inorganic salts such as sodium sulfate, sodium metasilicate, calcium chloride, serine, threonine, γ-aminobutyric acid, β Amino acids such as hydroxy-γ-aminobutyric acid, amino acid derivatives such as N-methyl-L-serine and sarcosine, N-acetylglucosamine and oligomers thereof, water-soluble vitamins such as ascorbic acid, niacin and biotin, and ascorbic acid sulfate Use vitamin derivatives such as salt and ascorbic acid phosphate Can.
[0007]
The percutaneous absorption promoting external preparation of the present invention can be applied to pharmaceuticals, quasi drugs, cosmetics, etc., and as dosage forms, for example, it is applied to lotions, emulsions, creams, packs, cosmetic oils, massages, etc. be able to.
[0008]
In addition to the above, the percutaneous absorption promoting external preparation of the present invention includes tar pigments, colored pigments such as iron oxide, preservatives such as paraben and phenoxyethanol, silicones such as dimethylpolysiloxane, methylphenylpolysiloxane, and cyclic silicone. Oils, hydrocarbons such as paraffin, petroleum jelly, olive squalane, rice squalane, rice germ oil, jojoba oil, sunflower oil, safflower oil, olive oil, macadamia nut oil, sunflower oil, and other vegetable oils, beeswax, molasses, carnauba wax, etc. , Octyldodecyl myristate, cetyl palmitate, isostearyl isostearate, isopropyl myristate, etc., lower alcohols such as ethanol, higher alcohols such as cetanol, behenyl alcohol, stearyl alcohol, long-chain branched aliphatic alcohols, etc. , Sterols and derivatives such as cholesterol, phytosterol, branched fatty acid cholesterol ester, macadamia nut fatty acid phytosteryl ester, processing oils such as hardened oil, stearic acid, myristic acid, isostearic acid, oleic acid, iso-type long chain fatty acid, anteiso Higher fatty acids such as type long chain fatty acids, terpenes such as limonene and hydrogenated bisabolol, triglycerides such as tricapryl / glyceryl caprate, glyceryl 2-ethylhexanoate, triiso type long chain fatty acid glyceryl, glyceryl tripalmitate, sodium cetyl sulfate Anionic surfactants such as N-stearoyl-L-glutamate, polyoxyethylene alkyl ether, polyoxyethylene fatty acid ester, polyoxyethylene polyhydric alcohol fat Nonionic surfactants such as esters, polyoxyethylene hydrogenated castor oil, polyhydric alcohol fatty acid esters, polyglycerin fatty acid esters, modified silicon and sucrose esters, cationic surfactants such as tetraalkylammonium salts, betaine type, sulfobetaine Type, amphoteric surfactants such as sulfoamino acid type, natural surfactants such as lecithin, lysophosphatidylcholine, ceramide, cerebroside, pigments such as titanium oxide and zinc oxide, antioxidants such as dibutylhydroxytoluene, hydroxy UV absorbers such as methoxybenzophenone sulfonate, polyhydric alcohols such as dipropylene glycol, 1,3 butylene glycol, glycerin, propylene glycol, sorbitol, malbitol, diglycerin, and raffinose However, the present invention is not limited to this.
[0009]
【Example】
Hereinafter, the present invention will be described in detail based on examples and comparative examples. In addition, the percutaneous absorption amount measuring method and the rough skin improvement test described in Examples are as follows.
[0010]
Percutaneous absorption measurement method A sample containing 200,000dpm of diisopropylamine labeled with 14C is provided on the stratum corneum side of a Franz vertical cell fitted with the abdominal skin of a hairless rat, and the amount of permeation after 8 hours is measured with a liquid scintillation counter. The cumulative transmittance was calculated.
[0011]
The rough skin improvement test sample was applied to the face of 30 adult women (twice a day) and indicated by the number of people who showed improvement of rough skin after 3 weeks.
[0012]
[Table 1]
[Table 2]
Examples 1-3, Comparative Examples 1-4
Using the branched fatty acids listed in Table 1, compositions of Examples and Comparative Examples were prepared based on the compositions of Table 2, and the above-described experiments were conducted using the compositions as samples.
[0015]
Table 2 shows the results of tests using the compositions of the examples and comparative examples as samples. Thus, the compositions of Examples 1 and 3 containing the branched fatty acid derived from soybean are the comparative examples 1 to 3 using different branched fatty acids and linear fatty acids, respectively, and comparative examples 4 not containing fatty acids. Excellent transdermal absorption promotion and rough skin improvement effect compared to the composition.
In addition, the composition of Example 2 containing a soybean-derived branched fatty acid that exhibits clear properties at 10 ° C. exhibits a further superior transdermal absorption promoting and rough skin improving effect compared to the composition of Example 1.
[0016]
【The invention's effect】
As described above, it is apparent that the present invention provides an external preparation for promoting percutaneous absorption that enhances the transdermal absorbability of a low-molecular water-soluble active ingredient.
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP05241399A JP4647733B2 (en) | 1999-03-01 | 1999-03-01 | Transdermal absorption-enhancing topical agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP05241399A JP4647733B2 (en) | 1999-03-01 | 1999-03-01 | Transdermal absorption-enhancing topical agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2000247827A JP2000247827A (en) | 2000-09-12 |
| JP4647733B2 true JP4647733B2 (en) | 2011-03-09 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP05241399A Expired - Fee Related JP4647733B2 (en) | 1999-03-01 | 1999-03-01 | Transdermal absorption-enhancing topical agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP4647733B2 (en) |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH02207018A (en) * | 1989-02-07 | 1990-08-16 | Kao Corp | Skin drug for external use |
| JPH045212A (en) * | 1990-04-20 | 1992-01-09 | Kao Corp | Cleansing composition |
| JP3303947B2 (en) * | 1994-05-18 | 2002-07-22 | 花王株式会社 | Method for producing branched fatty acid and branched fatty acid ester |
| JPH08104608A (en) * | 1994-10-06 | 1996-04-23 | Kao Corp | Topical skin |
| JP3625020B2 (en) * | 1998-03-02 | 2005-03-02 | 株式会社カネボウ化粧品 | Transdermal absorption enhancer and external preparation for skin |
-
1999
- 1999-03-01 JP JP05241399A patent/JP4647733B2/en not_active Expired - Fee Related
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| Publication number | Publication date |
|---|---|
| JP2000247827A (en) | 2000-09-12 |
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