JP2005281279A - Lipase inhibitor and external preparation for improving pimple - Google Patents
Lipase inhibitor and external preparation for improving pimple Download PDFInfo
- Publication number
- JP2005281279A JP2005281279A JP2004102218A JP2004102218A JP2005281279A JP 2005281279 A JP2005281279 A JP 2005281279A JP 2004102218 A JP2004102218 A JP 2004102218A JP 2004102218 A JP2004102218 A JP 2004102218A JP 2005281279 A JP2005281279 A JP 2005281279A
- Authority
- JP
- Japan
- Prior art keywords
- lipase
- extract
- external preparation
- acne
- kiwata
- 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.)
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Landscapes
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Abstract
Description
本発明は新規なリパーゼ阻害剤及びニキビ改善用外用剤に関する。さらに詳しくは、リパーゼに起因する疾患を予防、防止することのできる安全性の高いリパーゼ阻害剤、及びニキビの予防、治療に有効なニキビ改善用外用剤に関するものである。 The present invention relates to a novel lipase inhibitor and an external preparation for improving acne. More specifically, the present invention relates to a highly safe lipase inhibitor that can prevent or prevent diseases caused by lipase, and an external preparation for improving acne that is effective in preventing and treating acne.
人体における細菌性リパーゼには、皮膚表層に常在する微生物（プロピオニバクテリウム アクネス：Propionibacterium acnes、ピティロスポラム オバール：Pityrosporum ovale、マイクロコッカス属：Micrococcus sp.など）が産生するリパーゼがあり、これらのリパーゼが皮脂中に含まれるトリグリセライドを分解し遊離脂肪酸を産生する。この遊離脂肪酸は、皮膚に対して刺激性の炎症反応を引き起こし、ニキビ、皮膚炎、フケなどの要因となると考えられている。特にニキビの原因とされるプロピオニバクテリウム アクネスの菌数と産生する遊離脂肪酸には相関関係があり、遊離脂肪酸が毛包壁に対して、刺激性の炎症反応とそれに伴う過角化、コメドの形成を引き起こすと考えられている（例えば非特許文献１）。
これに対し、細菌性のリパーゼを阻害して疾患を抑制または予防する薬剤の開発は未だあまり進められておらず、２−Ｐｙｒｉｄｙｌｍｅｔｈｙｌ−２−（ｐ−（２−ｍｅｔｈｙｌｐｒｏｐｙｌ）−ｐｈｅｎｙｌ）ｐｒｏｐｉｏｎａｔｅ（慣用名：イブプロフェンピコノール）（例えば非特許文献２）、テトラサイクリンおよび金属塩（例えば特許文献１）等が報告されているに過ぎない。しかしながら、これらの薬剤は他の配合成分との関係からリパーゼ阻害効果を発揮できなかったり、局所適用における安全性、有効性の点で必ずしも満足し得ないものであった。
Bacterial lipases in the human body include lipases produced by microorganisms that are resident on the skin surface (Propionibacterium acnes, Pityrosporum ovale, Micrococcus sp., Etc.). Breaks down triglycerides contained in sebum to produce free fatty acids. This free fatty acid is considered to cause an irritating inflammatory reaction to the skin and cause acne, dermatitis, dandruff and the like. In particular, there is a correlation between the number of Propionibacterium acnes, the cause of acne, and the free fatty acids produced, and the free fatty acids have a stimulating inflammatory reaction on the hair follicle wall and accompanying hyperkeratosis, comedo. It is thought that it causes formation of (for example, nonpatent literature 1).
On the other hand, development of a drug that inhibits bacterial lipase to suppress or prevent diseases has not been advanced so far, and 2-Pyrylmethyl-2- (p- (2-methylpropyl) -phenyl) propionate (conventional use) Name: ibuprofen piconol) (for example, Non-Patent Document 2), tetracycline, metal salt (for example, Patent Document 1), and the like have only been reported. However, these drugs cannot exhibit a lipase inhibitory effect due to the relationship with other compounding components, and are not always satisfactory in terms of safety and effectiveness in topical application.
一方、キワタ（木棉、学名：Ｂｏｍｂａｘ ｍａｌａｂａｒｉｃｕｍ）の抽出物に関しては、皮膚外用剤（例えば特許文献２）、テストステロン−５α−リダクターゼ阻害剤（例えば特許文献３）、マトリックスメタロプロテアーゼ活性阻害剤および皮膚外用剤（例えば特許文献４）、ならびに、抗酸化剤並びに皮膚化粧料及び美容用飲食品（例えば特許文献５）としての利用法がすでに報告されている。 On the other hand, regarding the extract of Kiwata (Kiso, scientific name: Bombax malabaricum), an external preparation for skin (for example, Patent Document 2), a testosterone-5α-reductase inhibitor (for example, Patent Document 3), an inhibitor for matrix metalloprotease activity, and an external application for skin The utilization method as an agent (for example, patent document 4), an antioxidant, skin cosmetics, and food and drink for cosmetics (for example, patent document 5) has already been reported.
本発明者らは上記事情に鑑み、安全性が高くさらにリパーゼ阻害効果に優れた薬剤を得るべく広く種々の物質についてリパーゼ阻害活性を調べた結果、キワタ（木棉、学名：Ｂｏｍｂａｘ ｍａｌａｂａｒｉｃｕｍ）の溶媒抽出物にリパーゼ阻害作用があるという事実を見い出し、この知見にもとづいて本発明を開発するに至った。 In view of the above circumstances, the present inventors have investigated the lipase inhibitory activity of a wide variety of substances in order to obtain a drug with high safety and excellent lipase inhibitory effect. As a result, solvent extraction of Kiwata (Kiso, scientific name: Bombax malabaricum) The present inventors have found the fact that a product has a lipase inhibitory action and have developed the present invention based on this finding.
すなわち本発明は、キワタ（木棉、学名：Ｂｏｍｂａｘ ｍａｌａｂａｒｉｃｕｍ）の抽出物よりなることを特徴とするリパーゼ阻害剤である。 That is, the present invention is a lipase inhibitor characterized by comprising an extract of Kiwata (Kiso, scientific name: Bombax malabaricum).
また、本発明によれば、キワタ（木棉、学名：Ｂｏｍｂａｘ ｍａｌａｂａｒｉｃｕｍ）の抽出物を有効成分として含有することを特徴とするニキビ改善用外用剤が提供される。 Moreover, according to this invention, the external preparation for acne improvement characterized by containing the extract of kiwata (Kiso, scientific name: Bombax malabaricum) as an active ingredient is provided.
本発明者らが知る限りにおいて、キワタの抽出物のリパーゼ阻害作用に関する報告はこれまでになく、またリパーゼ阻害剤及びニキビ改善用外用剤への応用も知られていない。 As far as the present inventors know, there has been no report on the lipase inhibitory action of the extract of Kiwata, and its application to lipase inhibitors and external preparations for improving acne is not known.
本発明のリパーゼ阻害剤はリパーゼを強力かつ有効に抑制する。また皮膚に対して刺激やホルモン様作用等の副作用を与えず、特にニキビの予防、治療、処置に有効に働き、頭皮に使用してフケを有効に予防することができる。さらに、本発明のニキビ改善用外用剤は、ニキビを有効に予防、治療することができる。 The lipase inhibitor of the present invention potently and effectively suppresses lipase. In addition, it does not give side effects such as irritation and hormone-like action to the skin, and particularly works effectively for prevention, treatment and treatment of acne, and can be used for scalp to effectively prevent dandruff. Furthermore, the external preparation for acne improvement of the present invention can effectively prevent and treat acne.
以下、本発明の構成について詳述する。
本発明に用いられるキワタ（木棉、学名：Ｂｏｍｂａｘ ｍａｌａｂａｒｉｃｕｍ）は、広東、海南、広西、福建、台湾、雲南等に分布するパンヤ科に属する落葉高木である。本発明に用いられる抽出物は上記キワタ（木棉、学名：Ｂｏｍｂａｘ ｍａｌａｂａｒｉｃｕｍ）の葉、枝、果実、樹皮等を抽出溶媒と共に浸漬または加熱還流した後、濾過し、濃縮して得られる。本発明に用いられる抽出物を調製するために使用する部位としては、葉、枝、花、根、果実、果皮、種子、樹皮など、各植物体の任意の部位を用いることができるが、特に樹皮が好ましく用いられる。
Hereinafter, the configuration of the present invention will be described in detail.
The cotton (Kiso, scientific name: Bombax malabaricum) used in the present invention is a deciduous tree belonging to the Panya family distributed in Guangdong, Hainan, Guangxi, Fujian, Taiwan, Yunnan and the like. The extract used in the present invention is obtained by immersing or heating, refluxing, and heating the leaves, branches, fruits, bark, and the like of the above cotton (Kiso, scientific name: Bombax malabaricum) together with an extraction solvent. As a site used for preparing the extract used in the present invention, any site of each plant body such as leaves, branches, flowers, roots, fruits, fruit skins, seeds, bark, etc. can be used. Bark is preferably used.
本発明に用いられる抽出溶媒は、通常抽出に用いられる溶媒であれば任意に用いることができ、特にメタノール、エタノール等のアルコール類、含水アルコール類、アセトン、酢酸エチルエステル等の有機溶媒を、それぞれ単独あるいは組み合わせて用いることができる。また、抽出物を上記の溶媒を用い、分配あるいは吸着クロマトグラフィー、もしくは、活性炭あるいは合成樹脂による吸着処理のごとき精製等の処理を加えて得られたものも用いることができる。 The extraction solvent used in the present invention can be arbitrarily used as long as it is a solvent that is usually used for extraction, and in particular, an alcohol such as methanol and ethanol, a hydrous alcohol, an organic solvent such as acetone and ethyl acetate, It can be used alone or in combination. In addition, the extract obtained by applying a treatment such as partitioning or adsorption chromatography or adsorption treatment with activated carbon or synthetic resin using the above-mentioned solvent can be used.
本発明のリパーゼ阻害剤をニキビ改善用外用剤として用いる場合、キワタ（木棉、学名：Ｂｏｍｂａｘ ｍａｌａｂａｒｉｃｕｍ）の溶媒抽出物の外用剤中への配合量は、乾燥重量として０．００１〜２０．０質量％、好ましくは０．０１〜１０．０質量％である。０．００１質量％未満であると十分なリパーゼ阻害効果が発揮されず、２０．０質量％を越えると匂いと着色の点で製剤上好ましくない。また、１０．０質量％以上配合してもさほど大きな効果の向上はみられない。 When the lipase inhibitor of the present invention is used as an external preparation for acne improvement, the compounding amount of the solvent extract of Kiwata (Kiso, scientific name: Bombax malabaricum) in the external preparation is 0.001 to 20.0 mass as dry weight. %, Preferably 0.01 to 10.0% by mass. If it is less than 0.001% by mass, a sufficient lipase inhibitory effect is not exhibited, and if it exceeds 20.0% by mass, it is not preferable in terms of odor and coloring. Moreover, the improvement of the big effect is not seen even if 10.0 mass% or more is mix | blended.
本発明のリパーゼ阻害剤をニキビ改善用外用剤として用いる場合には、上記必須成分以外に通常化粧品や医薬品等の皮膚外用剤に用いられる成分、例えば水性成分、油性成分、粉末成分、アルコール類、ヒアルロン酸等の保湿剤、増粘剤、紫外線吸収剤、美白剤、防腐剤、酸化防止剤、界面活性剤、香料、色剤、各種皮膚栄養剤等を必要に応じて適宜配合することができる。 When using the lipase inhibitor of the present invention as an external agent for improving acne, in addition to the above essential components, components that are usually used in external preparations for skin such as cosmetics and pharmaceuticals, such as aqueous components, oily components, powder components, alcohols, Moisturizers such as hyaluronic acid, thickeners, UV absorbers, whitening agents, preservatives, antioxidants, surfactants, fragrances, colorants, various skin nutrients, and the like can be appropriately blended as necessary. .
その他、エデト酸二ナトリウム、エデト酸三ナトリウム、クエン酸ナトリウム、ポリリン酸ナトリウム、メタリン酸ナトリウム、グルコン酸等の金属封鎖剤、カフェイン、タンニン、ベラパミル、甘草抽出物、グラブリジン、火棘の果実の熱水抽出物、各種生薬、酢酸トコフェロール、グリチルリチン酸、トラネキサム酸及びその誘導体またはその塩等の薬剤、ビタミンＣ、アスコルビン酸リン酸マグネシウム、アスコルビン酸グルコシド、アルブチン、コウジ酸、グルコース、フルクトース、トレハロース等の糖類なども適宜配合することができる。 Other metal sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid, caffeine, tannin, verapamil, licorice extract, grabrizine, fire thorn fruit Hot water extract, various herbal medicines, drugs such as tocopherol acetate, glycyrrhizic acid, tranexamic acid and derivatives or salts thereof, vitamin C, magnesium ascorbate phosphate, glucoside ascorbate, arbutin, kojic acid, glucose, fructose, trehalose, etc. These sugars can also be blended as appropriate.
本発明のニキビ改善用外用剤は、例えば軟膏、クリーム、ローション、パック等、外皮に適用できるものであればいずれでもよく、剤型は特に問わない。 The external preparation for improving acne according to the present invention may be any ointment, cream, lotion, pack, etc. as long as it can be applied to the outer skin, and the dosage form is not particularly limited.
次に実施例等をあげて本発明をさらに具体的に説明するが、本発明はこれにより限定されるものではない。配合量は質量％である。なお実施例に先立ち、本発明の植物抽出物のリパーゼ阻害作用及びニキビ改善効果に関する試験方法について説明する。 EXAMPLES Next, although an Example etc. are given and this invention is demonstrated more concretely, this invention is not limited by this. A compounding quantity is the mass%. Prior to the examples, a test method for the lipase inhibitory action and the acne improving effect of the plant extract of the present invention will be described.
１．リパーゼ阻害活性評価
（１）リパーゼの調製
Ｐａｂｌｏらの方法（Ｊ．Ｉｎｖｅｓｔ．Ｄｅｒｍａｔｏｌ．６３，２１３，１９７４）に準じてリパーゼを精製した 。すなわち、ブレイン・ハート・インフュージョンブイヨン培地中にヒト皮膚から分離したプロピオニバクテリウム アクネスの１白金耳を接種し、３７℃で７日間嫌気的に培養し、培養液を４℃、３０００ｒｐｍで１５分間遠心分離した。その上清１Ｌ中に−３０℃、９５％エタノールを１Ｌ添加し、−１０℃で３０分間スターラーで攪拌したのち、４℃、１０００ｒｐｍ、１５分間遠心分離を行い、沈渣を凍結乾燥して粗リパーゼとした。
この０．５ｇを０．１ＭＮａＣｌ−０．０２Ｍ酢酸緩衝液（ｐＨ５．２）３ｍＬに溶解し、セファデックスＧ−１００カラム（Φ２．６ｃｍ、長さ４５ｃｍ）を用いて、０．１ＭＮａＣｌ−０．０２Ｍ酢酸緩衝液でゲル濾過し、活性画分４０ｍＬを得て、これを酵素溶液とした。
1. Evaluation of Lipase Inhibitory Activity (1) Preparation of Lipase Lipase was purified according to the method of Pablo et al. (J. Invest. Dermatol. 63, 213, 1974). That is, 1 platinum ear of Propionibacterium acnes isolated from human skin was inoculated into a brain heart infusion broth medium, and anaerobically cultured at 37 ° C. for 7 days. Centrifuged for minutes. Add 1 L of -30 ° C. and 95% ethanol to 1 L of the supernatant, stir with a stirrer at −10 ° C. for 30 minutes, centrifuge at 4 ° C., 1000 rpm for 15 minutes, freeze-dry the sediment and crude lipase It was.
0.5 g of this was dissolved in 3 mL of 0.1 M NaCl-0.02 M acetate buffer (pH 5.2), and 0.1 M NaCl-0 .0 using a Sephadex G-100 column (Φ2.6 cm, length 45 cm). Gel filtration was performed with 02M acetate buffer to obtain 40 mL of an active fraction, which was used as an enzyme solution.
（２）試験試料の調製
キワタ（木棉、学名：Ｂｏｍｂａｘ ｍａｌａｂａｒｉｃｕｍ）の樹皮部分２００ｇを室温で１週間メタノール１Ｌに浸漬し、抽出液を濃縮してメタノール抽出物５．１９ｇを得た。この固形物をエタノールに溶解し、１％溶液を作成した。これを用いて以下の実験を行った。
(2) Preparation of test sample 200 g of bark portion of Kiwata (Kiso, scientific name: Bombax malabaricum) was immersed in 1 L of methanol for 1 week at room temperature, and the extract was concentrated to obtain 5.19 g of methanol extract. This solid was dissolved in ethanol to make a 1% solution. The following experiment was conducted using this.
（３）比較試料の調製
リパーゼ阻害効果のある薬剤として現在皮膚外用剤に使用されている、（Ａ）２−Ｐｙｒｉｄｙｌｍｅｔｈｙｌ−２−（ｐ−（２−ｍｅｔｈｙｌｐｒｏｐｙｌ）−ｐｈｅｎｙｌ）ｐｒｏｐｉｏｎａｔｅ（慣用名イブプロフェンピコノール）、（Ｂ）テトラサイクリン、（Ｃ），（Ｄ）阻害効果の報告されている金属塩を、以下の方法で調製したものを比較試料とした。
（Ａ）２−Ｐｙｒｉｄｙｌｍｅｔｈｙｌ−２−（ｐ−（２−ｍｅｔｈｙｌｐｒｏｐｙｌ）−ｐｈｅｎｙｌ）ｐｒｏｐｉｏｎａｔｅ
２−Ｐｙｒｉｄｙｌｍｅｔｈｙｌ−２−（ｐ−（２−ｍｅｔｈｙｌｐｒｏｐｙｌ）−ｐｈｅｎｙｌ）ｐｒｏｐｉｏｎａｔｅをジメチルスルフォキシドに、酵素溶液中で反応させるときの濃度が０．１質量％になるように溶解した。
（Ｂ）テトラサイクリン
テトラサイクリン塩酸塩（シグマ社製）をジメチルスルフォキシドに、酵素溶液中で反応させるときの濃度が０．１質量％になるように溶解した。
（Ｃ）金属塩
第１塩化鉄（和光純薬工業）を水に、酵素溶液中で反応させる時の濃度が０．１質量％になるように溶解した。
（Ｄ）金属塩
第２塩化鉄（和光純薬工業）を水に、酵素溶液中で反応させる時の濃度が０．１質量％になるように溶解した。
(3) Preparation of comparative sample (A) 2-Pyrylmethyl-2- (p- (2-methylpropyl) -phenyl) propionate (common name ibuprofen pico) currently used in a topical skin preparation as a lipase inhibitory drug Nord), (B) Tetracycline, (C), (D) A metal salt reported to have an inhibitory effect was prepared by the following method as a comparative sample.
(A) 2-Pyrylmethyl-2- (p- (2-methylpropyl) -phenyl) propionate
2-Pyrylmethyl-2- (p- (2-methylpropyl) -phenyl) propionate was dissolved in dimethyl sulfoxide so as to have a concentration of 0.1% by mass when reacted in an enzyme solution.
(B) Tetracycline Tetracycline hydrochloride (manufactured by Sigma) was dissolved in dimethyl sulfoxide so that the concentration when reacted in an enzyme solution was 0.1% by mass.
(C) Metal salt Ferrous chloride (Wako Pure Chemical Industries, Ltd.) was dissolved in water so that the concentration when reacted in an enzyme solution was 0.1% by mass.
(D) Metal salt Ferric chloride (Wako Pure Chemical Industries, Ltd.) was dissolved in water so that the concentration when reacted in an enzyme solution was 0.1% by mass.
（４）リパーゼ活性の測定法および阻害率の算出
上記（１）で得られた酵素溶液に、試験試料、比較試料（Ａ）〜（Ｄ）をそれぞれ加えて、３７℃で振盪した後、それぞれ正確に１ｍＬずつ取り分けた（酵素溶液ａ、酵素溶液ｂ〜ｅ）。他方、オリーブオイル乳液５ｍＬと０．１Ｍリン酸緩衝液（ｐＨ７．０）４ｍＬとを５０ｍＬ容共栓三角フラスコに正確に取り、よく混合し、３７℃の恒温水槽を用いて１０分間予熱した。次いで、ここに上記１ｍＬずつ取り分けた酵素溶液ａ、酵素溶液ｂ〜ｅを、それぞれ、一か所に集中しないように攪拌しながら加えてよく混合し、酵素反応を行わせた。正確に１０分間経過後、アセトン−エタノール混液２０ｍＬを注ぎ、フェノールフタレイン試薬５滴を加え、０．０５Ｎ水酸化ナトリウム溶液で滴定した。
(4) Lipase activity measurement method and inhibition rate calculation To each of the enzyme solutions obtained in (1) above, a test sample and comparative samples (A) to (D) were added and shaken at 37 ° C. Exactly 1 mL was dispensed (enzyme solution a, enzyme solutions be). On the other hand, 5 mL of olive oil emulsion and 4 mL of 0.1 M phosphate buffer (pH 7.0) were accurately taken into a 50 mL stoppered Erlenmeyer flask, mixed well, and preheated for 10 minutes using a 37 ° C. constant temperature water bath. Next, the enzyme solution a and the enzyme solutions b to e separated from each 1 mL were added with stirring so as not to concentrate in one place, and mixed well to cause an enzyme reaction. After exactly 10 minutes, 20 mL of an acetone-ethanol mixture was poured, 5 drops of phenolphthalein reagent were added, and titrated with 0.05N sodium hydroxide solution.
一方、これとは別に、オリーブ油乳液５ｍＬと０．１Ｍリン酸緩衝液（ｐＨ７．０）４ｍＬとを５０ｍＬ容共栓三角フラスコに正確に取り、３７℃で３０分間加温後、アセトン−エタノール混液２０ｍＬを注ぎ、次いで上記１ｍＬずつ取り分けた酵素溶液ａ、酵素溶液ｂ〜ｅをそれぞれ加えた後、フェノールフタレイン試薬５滴を加え、０．０５Ｎ水酸化ナトリウム溶液で滴定した。これを対照液として酵素反応を行わせた滴定量から差し引き、活性値を算出した。
これと同様に、試験試料、比較試料（Ａ）〜（Ｄ）を加えない酵素溶液の活性値を測定し、この値を酵素活性値１００（阻害率０％）とする阻害率で表した。その結果を表１に示した。
Separately, 5 mL of olive oil emulsion and 4 mL of 0.1 M phosphate buffer (pH 7.0) were accurately taken into a 50 mL stoppered Erlenmeyer flask, heated at 37 ° C. for 30 minutes, and then 20 mL of an acetone-ethanol mixture. Then, the enzyme solution a and the enzyme solutions be were separately added, and 5 drops of phenolphthalein reagent was added thereto, followed by titration with 0.05N sodium hydroxide solution. The activity value was calculated by subtracting this from the titration amount in which the enzyme reaction was performed using the control solution.
Similarly, the activity value of the enzyme solution to which the test sample and the comparative samples (A) to (D) were not added was measured, and this value was expressed as an inhibition rate with an enzyme activity value of 100 (inhibition rate 0%). The results are shown in Table 1.
上記表１から明らかなように、本発明に係るキワタ抽出物は、評価系中に０．１質量％存在する場合に７６％のリパーゼ阻害作用を示すことが分かった。その作用は、従来からリパーゼ阻害剤として知られているイブプロフェンピコノール、テトラサイクリン塩酸塩、及び金属塩よりも高いものであり、すなわち本発明品は、リパーゼ阻害効果の高い新規なリパーゼ阻害剤であるといえる。 As is clear from Table 1 above, it has been found that the Kitta extract according to the present invention exhibits a lipase inhibitory action of 76% when 0.1% by mass is present in the evaluation system. Its action is higher than that of ibuprofen piconol, tetracycline hydrochloride, and metal salt, which are conventionally known as lipase inhibitors, that is, the product of the present invention is a novel lipase inhibitor having a high lipase inhibitory effect. It can be said.
２．ニキビ改善効果評価
（１）試験試料
表２に示す実施例１及び比較例１の処方の皮膚外用剤を常法によって製造し、これを試験試料としてニキビ改善効果を評価した。なおキワタ抽出物は、前記のリパーゼ阻害活性評価と同様の方法によって調製した。
2. Acne Improvement Effect Evaluation (1) Test Sample The skin external preparations of the formulations of Example 1 and Comparative Example 1 shown in Table 2 were produced by a conventional method, and this was used as a test sample to evaluate the acne improvement effect. In addition, the kiwata extract was prepared by the method similar to the above-mentioned lipase inhibitory activity evaluation.
（２）対象
１７才から２５才までのニキビに悩む男女４０名。（１群２０名）
(2) Subjects 40 men and women who suffer from acne from 17 to 25 years old. (20 people per group)
（３）使用方法および観察日
化粧石鹸を用いて顔面をよく洗浄した後、皮疹上に各々の皮膚外用剤を１日に２〜３回塗布して、４週間後に患部の観察を行った。
(3) Method of use and observation date After thoroughly washing the face with a cosmetic soap, each external preparation for skin was applied 2-3 times a day on the rash, and the affected area was observed after 4 weeks.
（４）全般改善度
使用前に比較して使用薬剤により症状が改善された（ａ）、不変または悪化した（ｂ）の２段階に分けた。
(4) General improvement degree It was divided into two stages: (a) where symptoms were improved by the drug used compared to before use (a), unchanged or worsened (b).
（５）有効性評価基準
◎：全般改善度で２０名中、（ａ）が１５名以上。
○：全般改善度で２０名中、（ａ）が１０〜１４名。
△：全般改善度で２０名中、（ａ）が５〜９名。
×：全般改善度で２０名中、（ａ）が４名以下。
(5) Efficacy evaluation criteria A: Overall improvement is 20 out of 20, (a) is 15 or more.
○: Out of 20 people with general improvement, (a) is 10 to 14 people.
(Triangle | delta): (a) is 5-9 persons in 20 people by general improvement degree.
X: Out of 20 in general improvement, (a) is 4 or less.
上記の評価基準に従い実施例１及び比較例１の有効性を評価し、その結果を処方と合わせて下記表２に示した。数値は質量％を示す。 The effectiveness of Example 1 and Comparative Example 1 was evaluated according to the above evaluation criteria, and the results are shown in Table 2 below together with the formulation. A numerical value shows the mass%.
上記表２に示すように、キワタ抽出物を配合した本発明の外用剤は、優れたニキビ改善効果を有していた。 As shown in Table 2 above, the external preparation of the present invention blended with the kiwata extract had an excellent acne improving effect.
以下に種々の剤型の本発明によるニキビ改善用外用剤の処方例を示すが、各実施例の外用剤は、その剤型に応じて常法により製造した。また、各実施例のニキビ改善用外用剤に上記の試験・評価を施したところ、全て実施例１と同等の有効性が得られた。 The formulation examples of the external preparation for acne improvement according to the present invention of various dosage forms are shown below. The external preparations of each Example were produced by a conventional method according to the dosage form. Moreover, when said test and evaluation were given to the external preparation for acne improvement of each Example, all the same effectiveness as Example 1 was acquired.
実施例２ ローション
（１）リジンベタイン １．０質量％
（２）キワタエタノール抽出物 ０．２
（３）グリチルリチン酸ジカリウム ０．０５
（４）グリセリン ４．０
（５）１，３−ブチレングリコール ４．０
（６）エタノール ７．０
（７）ポリオキシエチレンオレイルアルコール ０．５
（８）メチルパラベン ０．０５
（９）クエン酸 ０．０１
（１０）クエン酸ソーダ ０．１
（１１）香料 ０．０５
（１２）精製水 残余
Example 2 Lotion (1) Lysine betaine 1.0 mass%
(2) Kiwata ethanol extract 0.2
(3) Dipotassium glycyrrhizinate 0.05
(4) Glycerin 4.0
(5) 1,3-butylene glycol 4.0
(6) Ethanol 7.0
(7) Polyoxyethylene oleyl alcohol 0.5
(8) Methylparaben 0.05
(9) Citric acid 0.01
(10) Sodium citrate 0.1
(11) Fragrance 0.05
(12) Purified water residue
実施例３ クリーム
（１）セトステアリルアルコール ３．５質量％
（２）スクワラン ４０．０
（３）ミツロウ ３．０
（４）還元ラノリン ５．０
（５）キワタブタノール抽出物 ０．７
（６）エチルパラベン ０．３
（７）ポリオキシエチレン（２０）ソルビタン
モノパルミチン酸エステル ２．０
（８）ステアリン酸モノグリセリド ２．０
（９）香料 ０．０３
（１０）トラネキサム酸ヘキシルアミド ３．０
（１１）リン酸ピリドキサール ０．１
（１２）オルニチンベタイン ０．０５
（１３）１，３−ブチレングリコール ５．０
（１４）グリセリン ５．０
（１５）精製水 残余
Example 3 Cream (1) cetostearyl alcohol 3.5% by mass
(2) Squalane 40.0
(3) Beeswax 3.0
(4) Reduced lanolin 5.0
(5) Kiwatabtanol extract 0.7
(6) Ethylparaben 0.3
(7) Polyoxyethylene (20) sorbitan
Monopalmitate 2.0
(8) Stearic acid monoglyceride 2.0
(9) Perfume 0.03
(10) Tranexamic acid hexylamide 3.0
(11) Pyridoxal phosphate 0.1
(12) Ornithine betaine 0.05
(13) 1,3-butylene glycol 5.0
(14) Glycerin 5.0
(15) Purified water residue
実施例４ 乳液
（１）トラネキサム酸塩酸塩 ２．０質量％
（２）キワタ１，３−ブチレングリコール抽出液（固形分濃度１．１％） １．０
（３）アラニンベタイン ０．１
（４）アラントイン ０．０５
（５）ステアリン酸 １．５
（６）セチルアルコール ０．５
（７）ミツロウ ２．０
（８）ポリオキシエチレン(10)モノオレイン酸エステル １．０
（９）グリセリンモノステアリン酸エステル １．０
（１０）プロピレングリコール ５．０
（１１）エタノール ３．０
（１２）エチルパラベン ０．３
（１３）香料 ０．０３
（１４）精製水 残余
Example 4 Latex (1) tranexamic hydrochloride 2.0% by mass
(2) Kiwata 1,3-butylene glycol extract (solid content concentration 1.1%) 1.0
(3) Alanine betaine 0.1
(4) Allantoin 0.05
(5) Stearic acid 1.5
(6) Cetyl alcohol 0.5
(7) Beeswax 2.0
(8) Polyoxyethylene (10) monooleate 1.0
(9) Glycerin monostearate 1.0
(10) Propylene glycol 5.0
(11) Ethanol 3.0
(12) Ethylparaben 0.3
(13) Perfume 0.03
(14) Purified water residue
実施例５ 軟膏
（１）トラネキサム酸ｎ−ヘキシルエステル塩酸塩 ３．０質量％
（２）グリチルリチン酸ピリドキシン １．０
（３）γ−ブチロベタイン ０．１
（４）キワタ熱水抽出物 １．５
（５）ステアリルアルコール １８．０
（６）モクロウ ２０．０
（７）ポリオキシエチレン(10)モノオレイン酸エステル ０．２５
（８）グリセリンモノステアリン酸エステル ０．２５
（９）ワセリン ４０．０
（１０）精製水 残余
Example 5 Ointment (1) tranexamic acid n-hexyl ester hydrochloride 3.0% by mass
(2) Pyridoxine glycyrrhizinate 1.0
(3) γ-butyrobetaine 0.1
(4) Kiwata hot water extract 1.5
(5) Stearyl alcohol 18.0
(6) Owl 20.0
(7) Polyoxyethylene (10) monooleate 0.25
(8) Glycerin monostearate 0.25
(9) Vaseline 40.0
(10) Purified water residue
実施例６ パック
（１）トラネキサム酸グアニジド ５．０質量％
（２）トリパルミチン酸ピリドキシン １．５
（３）フェニルアラニルベタイン ０．１
（４）ポリビニルアルコール １５．０
（５）キワタアセトン抽出物 ２．０
（６）ポリエチレングリコール ３．０
（７）プロピレングリコール ７．０
（８）エタノール １０．０
（９）メチルパラベン ０．０５
（１０）香料 ０．０５
（１１）精製水 残余
Example 6 Pack (1) tranexamic acid guanidide 5.0 mass%
(2) Pyridoxine tripalmitate 1.5
(3) Phenylalanyl betaine 0.1
(4) Polyvinyl alcohol 15.0
(5) Kiwata acetone extract 2.0
(6) Polyethylene glycol 3.0
(7) Propylene glycol 7.0
(8) Ethanol 10.0
(9) Methylparaben 0.05
(10) Fragrance 0.05
(11) Purified water residue
実施例７ 固形白粉
（１）タルク ８５．４質量％
（２）ステアリン酸 １．５
（３）ラノリン ５．０
（４）スクワラン ５．０
（５）キワタグリセリン抽出物 ０．３
（６）ソルビタンセスキオレイン酸エステル ２．０
（７）トリエタノールアミン １．０
（８）トラネキサム酸メチルアミド １．０
（９）ジカプリル酸ピリドキシン ０．１
（１０）グルタミン酸ベタイン ０．１
（１１）顔料 適量
（１２）香料 適量
Example 7 Solid white powder (1) Talc 85.4% by mass
(2) Stearic acid 1.5
(3) Lanolin 5.0
(4) Squalane 5.0
(5) Kiwatag lysine extract 0.3
(6) Sorbitan sesquioleate 2.0
(7) Triethanolamine 1.0
(8) Tranexamic acid methylamide 1.0
(9) Pyridoxine dicaprylate 0.1
(10) Betaine glutamate 0.1
(11) Appropriate amount of pigment (12) Appropriate amount of perfume
Claims (3)
The external preparation for acne improvement according to claim 2, wherein the amount of the extract of kiwata (Kiso, scientific name: Bombax malabaricum) is 0.001 to 20.0% by mass.
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011086891A1 (en) * | 2010-01-12 | 2011-07-21 | 株式会社ナノエッグ | Composition for non-invasively facilitating the removal of skin pigment |
| CN108795097A (en) * | 2018-05-21 | 2018-11-13 | 汕头大学 | A kind of isolation and purification method of kapok carthamin |
| CN109010211A (en) * | 2018-09-21 | 2018-12-18 | 张惠柳 | It is a kind of for preventing and treating the facial cleanser of subcutaneous fat tumor |
-
2004
- 2004-03-31 JP JP2004102218A patent/JP2005281279A/en not_active Withdrawn
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011086891A1 (en) * | 2010-01-12 | 2011-07-21 | 株式会社ナノエッグ | Composition for non-invasively facilitating the removal of skin pigment |
| CN108795097A (en) * | 2018-05-21 | 2018-11-13 | 汕头大学 | A kind of isolation and purification method of kapok carthamin |
| CN108795097B (en) * | 2018-05-21 | 2020-04-21 | 汕头大学 | A kind of separation and purification method of kapok red pigment |
| CN109010211A (en) * | 2018-09-21 | 2018-12-18 | 张惠柳 | It is a kind of for preventing and treating the facial cleanser of subcutaneous fat tumor |
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