JP2009269842A - External preparation for skin - Google Patents
External preparation for skin Download PDFInfo
- Publication number
- JP2009269842A JP2009269842A JP2008120225A JP2008120225A JP2009269842A JP 2009269842 A JP2009269842 A JP 2009269842A JP 2008120225 A JP2008120225 A JP 2008120225A JP 2008120225 A JP2008120225 A JP 2008120225A JP 2009269842 A JP2009269842 A JP 2009269842A
- Authority
- JP
- Japan
- Prior art keywords
- atemoya
- extract
- skin
- external preparation
- added
- 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.)
- Granted
Links
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- ZWLUXSQADUDCSB-UHFFFAOYSA-N phthalaldehyde Chemical compound O=CC1=CC=CC=C1C=O ZWLUXSQADUDCSB-UHFFFAOYSA-N 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 239000002798 polar solvent Substances 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 229930002330 retinoic acid Natural products 0.000 description 1
- 229960003471 retinol Drugs 0.000 description 1
- 235000020944 retinol Nutrition 0.000 description 1
- 239000011607 retinol Substances 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 210000001626 skin fibroblast Anatomy 0.000 description 1
- 239000000344 soap Substances 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 238000002415 sodium dodecyl sulfate polyacrylamide gel electrophoresis Methods 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- LHWPSDLHLAAELL-UHFFFAOYSA-N sodium;2-sulfanylidene-1,3-diazinane-4,6-dione Chemical compound [Na].O=C1CC(=O)NC(=S)N1 LHWPSDLHLAAELL-UHFFFAOYSA-N 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229960001727 tretinoin Drugs 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Landscapes
- Medicines Containing Plant Substances (AREA)
- Cosmetics (AREA)
Abstract
Description
本発明は、アテモヤの抽出物を含有することを特徴とする、シワの予防や改善、抗炎症作用等に優れた皮膚外用剤に関する。 The present invention relates to a skin external preparation excellent in prevention and improvement of wrinkles, anti-inflammatory action and the like, characterized by containing an extract of Atemoya.
近年、生体成分を酸化させる要因として、フリーラジカルや活性酸素がとりあげられ、その悪影響が問題となっている。フリーラジカルや活性酸素は体内で生じ、コラーゲンなどの生体組織を分解あるいは架橋し、また、油脂類を酸化して、細胞に障害を与える過酸化脂質をつくると言われている。このような障害は、肌のシワや張りの低下等の原因になると考えられており、これらを防ぐ方法の一つに過酸化脂質の生成を抑制する方法が知られている。従来、抗酸化剤にはアスコルビン酸、トコフェロール、BHT(3,5−tert−ブチル−4−ヒドロキシトルエン)やスーパーオキシドジスムターゼ(SOD)等が用いられてきた。 In recent years, free radicals and active oxygen have been taken up as factors that oxidize biological components, and their adverse effects have become a problem. It is said that free radicals and active oxygen are generated in the body and decompose or crosslink biological tissues such as collagen, and oxidize fats and oils to form lipid peroxides that damage cells. Such a disorder is considered to cause skin wrinkles, a decrease in tension, and the like, and a method for suppressing the formation of lipid peroxide is known as one of the methods for preventing these problems. Conventionally, ascorbic acid, tocopherol, BHT (3,5-tert-butyl-4-hydroxytoluene), superoxide dismutase (SOD), and the like have been used as antioxidants.
また、シワの原因としては、コラーゲン、エラスチン等の真皮マトリックスの線維減少、変性が起こることが知られている。近年研究が進み、この変化を誘導する因子として、特にMMPの関与が指摘されている。また、MMPの中でも、コラゲナーゼとゼラチナーゼは皮膚の真皮マトリックスの主な構成成分であるコラーゲンを分解する酵素として知られ、その発現は紫外線の照射により大きく増加し、紫外線によるコラーゲンの減少変性の原因の一つとなり、シワの形成等の大きな要因の一つであると考えられている。よって、これらの酵素を阻害することは、コラーゲンを保護し、線維を形成するマトリックスを保護することとなり、シワを防ぐうえで重要である。このようなシワを防ぐ方法の一つにMMP活性阻害剤が知られている。従来、シワを予防する成分としてレチノイン酸、α−ヒドロキシ酸、レチノール等が用いられてきた。 Further, it is known that wrinkles are caused by fiber reduction and degeneration of the dermal matrix such as collagen and elastin. In recent years, research has progressed and it has been pointed out that MMP is particularly involved as a factor inducing this change. Among the MMPs, collagenase and gelatinase are known as enzymes that degrade collagen, which is the main component of the dermal matrix of the skin, and its expression is greatly increased by irradiation with ultraviolet rays, which causes the decrease and degeneration of collagen by ultraviolet rays. It is considered to be one of the major factors such as the formation of wrinkles. Therefore, inhibiting these enzymes protects the collagen and protects the matrix that forms the fibers, and is important in preventing wrinkles. MMP activity inhibitors are known as one method for preventing such wrinkles. Conventionally, retinoic acid, α-hydroxy acid, retinol, and the like have been used as components for preventing wrinkles.
肌荒れの一因として紫外線等による皮膚炎症があり、その炎症を沈め、肌荒れを改善する皮膚外用剤が望まれている。その治療法の一つとして、炎症時に生じる起炎物質であるヒスタミンの遊離を抑制する方法がある。従来、肌荒れの治療には、ステロイド剤やインドメタシン等を外用する処置が行われてきた。しかし、以上に述べたシワの予防や改善及び抗炎症作用の指標である、過酸化脂質生成抑制作用、MMP活性阻害作用及びヒスタミン遊離抑制作用について、植物原料のアテモヤは検討されていなかった。 There is skin inflammation caused by ultraviolet rays or the like as a cause of rough skin, and an external preparation for skin that subsides the inflammation and improves rough skin is desired. As one of the treatment methods, there is a method for suppressing the release of histamine, which is a inflammatory substance that occurs during inflammation. Conventionally, treatments for rough skin have been performed using steroids, indomethacin or the like. However, the plant material Atemoya has not been studied for the lipid peroxidation inhibitory action, the MMP activity inhibitory action, and the histamine release inhibitory action, which are the indicators of wrinkle prevention and improvement and anti-inflammatory action described above.
皮膚のシワの予防や改善又は抗酸化を目的として用いられるSODは不安定であり、製剤化が難しく、トコフェロールも効果が充分であるとは言えない。また、合成化合物であるBHT等は安全性に問題があり、配合量に制限があることから、化学合成品ではなく、安定でかつ副作用の少ない天然原料が望まれている。同様に、安全で安定なMMP活性阻害作用を有することがシワの予防や改善に好ましい。また、従来のヒスタミンの遊離を抑制する作用を持つ皮膚外用材は、ステロイド剤等の化学合成で得られた物質を含有するものがほとんどであり、副作用の危険性もあるため、同様に安定性が高く、効果の優れた天然物由来の皮膚外用剤が望まれている。 SOD used for the purpose of preventing or improving skin wrinkles or for antioxidant purposes is unstable, difficult to formulate, and tocopherol cannot be said to be sufficiently effective. Moreover, since BHT etc. which are synthetic compounds have a problem in safety | security and there exists a restriction | limiting in compounding quantity, it is not a chemical synthetic product but the natural raw material which is stable and has few side effects is desired. Similarly, it is preferable for prevention and improvement of wrinkles to have a safe and stable MMP activity inhibitory action. In addition, most of the conventional skin external materials that have the action of suppressing the release of histamine contain substances obtained by chemical synthesis such as steroids, and there is a risk of side effects. Therefore, a skin external preparation derived from a natural product having a high effect and an excellent effect is desired.
以上のことから、安全で安定性に優れ、シワの予防や改善及び抗炎症作用に優れた皮膚外用剤が望まれている。 From the above, a skin external preparation that is safe and excellent in stability, is excellent in prevention and improvement of wrinkles, and an anti-inflammatory action is desired.
このような事情により、本発明者らは鋭意検討した結果、アテモヤの抽出物が優れた過酸化脂質生成抑制作用、MMP活性阻害作用及びヒスタミン遊離抑制作用をもち、安定性においても優れていることを見出した。さらに、その抽出物を含有する皮膚外用剤が、安全で安定であり、シワの予防や改善及び抗炎症作用に優れていることを見出し、本発明を完成するに至った。 Under such circumstances, as a result of intensive studies, the present inventors have found that the extract of Atemoya has excellent lipid peroxide production inhibitory action, MMP activity inhibitory action and histamine release inhibitory action, and is also excellent in stability. I found. Furthermore, the skin external preparation containing the extract was found to be safe and stable, and excellent in prevention and improvement of wrinkles and an anti-inflammatory action, and the present invention was completed.
本発明に用いるアテモヤ(学名:Annona atemoya)は、バンレイシ科バンレイシ属に属する植物であり、バンレイシ(バンレイシ科、学名:Annona squamosa)とチェリモヤ(バンレイシ科:Annona cherimola)を人工的に掛け合わせ品種改良した果樹である。その実は食用として広く流通しているが、化粧料としての利用は報告されていない。 Atemoya (scientific name: Annona atemoya) used in the present invention is a plant belonging to the genus Vanleci, and is an artificially improved variety of bream (Banleciaceae, scientific name: Annona squamosa) and cherimoya (Annona cherimola). It is a fruit tree. In fact, it is widely distributed for food use, but its use as a cosmetic has not been reported.
本発明に用いるアテモヤの抽出物とは、アテモヤの葉、茎、樹皮、花、果実、根等の植物体の一部又は全草から抽出したものである。好ましくは、果実、果肉、果皮、種子等から抽出したものが良い。その抽出方法は特に限定されず、例えば、加熱抽出したものであっても良いし、常温抽出したものであっても良い。また、生のアテモヤを用いても良いし、乾燥したものを用いても良い。 The extract of Atemoya used in the present invention is extracted from a part of the plant body such as Atemoya leaves, stems, bark, flowers, fruits, roots or whole plants. Preferably, those extracted from fruits, pulp, pericarp, seeds and the like are good. The extraction method is not particularly limited, and for example, it may be a heat extraction or a room temperature extraction. Further, raw atemoya may be used, or a dried one may be used.
抽出する溶媒としては、例えば、水、低級アルコール類(メタノール、エタノール、1−プロパノール、2−プロパノール、1−ブタノール、2−ブタノール等)、液状多価アルコール(1,3−ブチレングリコール、プロピレングリコール、グリセリン等)、ケトン類(アセトン、メチルエチルケトン等)、アセトニトリル、エステル類(酢酸エチル、酢酸ブチル等)、炭化水素類(ヘキサン、ヘプタン、流動パラフィン等)、エーテル類(エチルエーテル、テトラヒドロフラン、プロピルエーテル等)が挙げられる。好ましくは、水、低級アルコール及び液状多価アルコール等の極性溶媒が良く、特に好ましくは、水、エタノール、1,3−ブチレングリコール及びプロピレングリコールが良い。これらの溶媒は一種でも二種以上を混合して用いても良い。 Examples of the solvent to be extracted include water, lower alcohols (methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, etc.), liquid polyhydric alcohols (1,3-butylene glycol, propylene glycol). , Glycerin, etc.), ketones (acetone, methyl ethyl ketone, etc.), acetonitrile, esters (ethyl acetate, butyl acetate, etc.), hydrocarbons (hexane, heptane, liquid paraffin, etc.), ethers (ethyl ether, tetrahydrofuran, propyl ether) Etc.). Preferred are polar solvents such as water, lower alcohols and liquid polyhydric alcohols, and particularly preferred are water, ethanol, 1,3-butylene glycol and propylene glycol. These solvents may be used alone or in combination of two or more.
上記抽出物は、抽出した溶液のまま用いても良く、必要に応じて、濃縮、希釈及び濾過処理、活性炭等による脱色、脱臭処理等をして用いても良い。更には、抽出した溶液を濃縮乾固、噴霧乾燥、凍結乾燥等の処理を行い、乾燥物として用いても良い。 The extract may be used as it is, or may be used after concentration, dilution and filtration treatment, decolorization with activated carbon, deodorization treatment, or the like, if necessary. Further, the extracted solution may be subjected to a treatment such as concentration to dryness, spray drying, freeze drying, etc., and used as a dried product.
本発明の皮膚外用剤には、上記抽出物をそのまま使用しても良く、抽出物の効果を損なわない範囲内で、外用剤に用いられる成分である油脂類、ロウ類、炭化水素類、脂肪酸類、アルコール類、エステル類、界面活性剤、金属石鹸、pH調整剤、防腐剤、香料、保湿剤、粉体、紫外線吸収剤、増粘剤、色素、酸化防止剤、美白剤、キレート剤等の成分を配合することができる。 In the external preparation for skin of the present invention, the above extract may be used as it is, and within the range not impairing the effect of the extract, oils and fats, waxes, hydrocarbons, fatty acids which are components used in the external preparation , Alcohols, esters, surfactants, metal soaps, pH adjusters, preservatives, fragrances, moisturizers, powders, UV absorbers, thickeners, pigments, antioxidants, whitening agents, chelating agents, etc. These components can be blended.
本発明の皮膚外用剤は、化粧品、医薬部外品、医薬品のいずれにも用いることができ、その剤形としては、例えば、化粧水、クリ−ム、乳液、ゲル剤、エアゾール剤、エッセンス、パック、洗浄剤、浴用剤、ファンデ−ション、打粉、口紅、軟膏、パップ剤等の皮膚に適用されるものが挙げられる。 The external preparation for skin of the present invention can be used for any of cosmetics, quasi drugs, and pharmaceuticals. Examples of the dosage form include skin lotions, creams, emulsions, gels, aerosols, essences, Examples include packs, cleaning agents, bath preparations, foundations, dusting powders, lipsticks, ointments, and poultices applied to the skin.
本発明に用いる上記抽出物の配合量は、本発明の皮膚外用剤全量に対し、固形物に換算して0.0001重量%以上、好ましくは0.001〜10重量%の配合が良い。0.0001重量%未満では十分な効果は望みにくい。10重量%を越えて配合した場合、効果の増強は認められにくく不経済である。また、添加の方法については、予め加えておいても、製造途中で添加しても良く、作業性を考えて適宜選択すれば良い。 The amount of the extract used in the present invention is 0.0001% by weight or more, preferably 0.001 to 10% by weight in terms of solid matter, based on the total amount of the external preparation for skin of the present invention. If it is less than 0.0001% by weight, a sufficient effect is hardly expected. When the blending amount exceeds 10% by weight, the enhancement of the effect is hardly recognized and it is uneconomical. In addition, the addition method may be added in advance or during the production, and may be appropriately selected in consideration of workability.
本発明のアテモヤの抽出物は、優れた過酸化脂質生成抑制作用、MMP活性阻害作用及びヒスタミン遊離抑制作用を有し、安定性にも優れていた。さらに、これらの抽出物を含有する皮膚外用剤は、安全で優れたシワの予防や改善及び抗炎症作用を示した。 The extract of Atemoya of the present invention had an excellent lipid peroxide production inhibitory action, MMP activity inhibitory action and histamine release inhibitory action, and was also excellent in stability. Furthermore, the external preparation for skin containing these extracts showed safe and excellent wrinkle prevention and improvement and anti-inflammatory action.
次に本発明を詳細に説明するため、実施例として本発明に用いる抽出物の製造例、本発明の処方例及び実験例を挙げるが、本発明はこれに限定されるものではない。処方例に示す配合量の部とは重量部を、%とは重量%を示す。 Next, in order to describe the present invention in detail, examples of producing the extract used in the present invention, formulation examples and experimental examples of the present invention will be given as examples, but the present invention is not limited thereto. The part of the compounding amount shown in the prescription example means part by weight, and% means weight%.
製造例1 アテモヤ果皮の熱水抽出物
アテモヤ果皮の乾燥物20gに精製水400gを加え、95〜100℃で2時間抽出した後、濾過し、その濾液を濃縮し、凍結乾燥してアテモヤ果皮の熱水抽出物を6.1g得た。
Production Example 1 Hot water extract of Atemoya pericarp 400 g of purified water was added to 20 g of dried Atemoya pericarp, extracted at 95-100 ° C. for 2 hours, filtered, and the filtrate was concentrated, freeze-dried and dried with Atemoya pericarp. 6.1 g of hot water extract was obtained.
製造例2 アテモヤ果実の熱水抽出物
アテモヤ果実の乾燥物20gに精製水400gを加え、95〜100℃で2時間抽出した後、濾過し、その濾液を濃縮し、凍結乾燥してアテモヤ果実の熱水抽出物を10.4g得た。
Production Example 2 Hot Water Extract of Atemoya Fruit Add 400 g of purified water to 20 g of dried Atemoya fruit, extract at 95-100 ° C. for 2 hours, filter, concentrate the filtrate, freeze-dry, 10.4 g of hot water extract was obtained.
製造例3 アテモヤ種子の熱水抽出物
アテモヤ種子の乾燥物20gに精製水400gを加え、95〜100℃で2時間抽出した後、濾過し、その濾液を濃縮し、凍結乾燥してアテモヤ種子の熱水抽出物を1.7g得た。
Production Example 3 Hot Water Extract of Atemoya Seeds 400 g of purified water was added to 20 g of dried products of Atemoya seeds, extracted at 95-100 ° C. for 2 hours, filtered, and the filtrate was concentrated and freeze-dried. 1.7 g of hot water extract was obtained.
製造例4 アテモヤ果皮の50%エタノール抽出物
アテモヤ果皮の乾燥物20gに50(v/v)%エタノール水溶液400gを加え、常温で5日間抽出した後、濾過し、その濾液を濃縮し、凍結乾燥してアテモヤ未熟果皮の50%エタノール抽出物を7.1g得た。
Production Example 4 50% ethanol extract of Atemoya pericarp 400 g of 50 (v / v)% ethanol aqueous solution was added to 20 g of dried Atemoya pericarp, extracted at room temperature for 5 days, filtered, and the filtrate was concentrated and freeze-dried As a result, 7.1 g of 50% ethanol extract of Atemoya immature pericarp was obtained.
製造例5 アテモヤ果皮のエタノール抽出物
アテモヤ果皮の乾燥物20gにエタノール400gを加え、常温で5日間抽出した後、濾過し、その濾液を濃縮し、凍結乾燥してアテモヤ果皮のエタノール抽出物を0.2g得た。
Production Example 5 Ethamo extract of Atemoya pericarp 400 g of ethanol was added to 20 g of dried Atemoya pericarp and extracted at room temperature for 5 days, followed by filtration. The filtrate was concentrated and freeze-dried to obtain an ethanol extract of Atemoya pericarp. 0.2 g was obtained.
処方例1 化粧水
処方 配合量
1.アテモヤ果皮の熱水抽出物(製造例1) 0.1部
2.1,3−ブチレングリコール 8.0
3.グリセリン 2.0
4.キサンタンガム 0.02
5.クエン酸 0.01
6.クエン酸ナトリウム 0.1
7.エタノール 5.0
8.パラオキシ安息香酸メチル 0.1
9.ポリオキシエチレン硬化ヒマシ油(40E.O.) 0.1
10.香料 適量
11.精製水にて全量を100とする
[製造方法]成分1〜6及び11と、成分7〜10をそれぞれ均一に溶解し、両者を混合し濾過して製品とする。
Formulation Example 1 Lotion Formulation Amount Hot water extract of Atemoya peel (Production Example 1) 0.1 part 2.1,3-butylene glycol 8.0
3. Glycerin 2.0
4). Xanthan gum 0.02
5. Citric acid 0.01
6). Sodium citrate 0.1
7). Ethanol 5.0
8). Methyl paraoxybenzoate 0.1
9. Polyoxyethylene hydrogenated castor oil (40E.O.) 0.1
10. Perfume
11. [Manufacturing method] Components 1 to 6 and 11 and components 7 to 10 are uniformly dissolved in purified water, and both are mixed and filtered to obtain a product.
比較例1 従来の化粧水
処方例1において、アテモヤ果皮の熱水抽出物(製造例1)を精製水に置き換えたものを従来の化粧水とした。
Comparative Example 1 Conventional lotion In Formulation Example 1, the hot water extract of Atemoya peel (Production Example 1) was replaced with purified water to obtain a conventional lotion.
処方例2 クリーム
処方 配合量
1.アテモヤ果皮の50%エタノール抽出物(製造例4) 0.05部
2.スクワラン 5.5
3.オリーブ油 3.0
4.ステアリン酸 2.0
5.ミツロウ 2.0
6.ミリスチン酸オクチルドデシル 3.5
7.ポリオキシエチレンセチルエーテル(20E.O.) 3.0
8.ベヘニルアルコール 1.5
9.モノステアリン酸グリセリン 2.5
10.香料 0.1
11.パラオキシ安息香酸メチル 0.2
12.パラオキシ安息香酸エチル 0.05
13.1,3−ブチレングリコール 8.5
14.精製水にて全量を100とする
[製造方法]成分2〜9を加熱溶解して混合し、70℃に保ち油相とする。成分1及び11〜14を加熱溶解して混合し、75℃に保ち水相とする。油相に水相を加えて乳化して、かき混ぜながら冷却し、45℃で成分10を加え、更に30℃まで冷却して製品とする。
Formulation Example 2 Cream Formulation Amount 50 parts ethanol extract of Atemoya peel (Production Example 4) 0.05 part Squalane 5.5
3. Olive oil 3.0
4). Stearic acid 2.0
5. Beeswax 2.0
6). Octyldodecyl myristate 3.5
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Behenyl alcohol 1.5
9. Glycerol monostearate2.5
10. Fragrance 0.1
11. Methyl paraoxybenzoate 0.2
12 Ethyl paraoxybenzoate 0.05
13.1,3-Butylene glycol 8.5
14 [Manufacturing method] Components 2 to 9 are heated and dissolved and mixed with purified water to a total amount of 100, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 11 to 14 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring. The component 10 is added at 45 ° C., and further cooled to 30 ° C. to obtain a product.
比較例2 従来のクリーム
処方例2において、アテモヤ果皮の50%エタノール抽出物(製造例4)を精製水に置き換えたものを従来のクリームとした。
Comparative Example 2 Conventional Cream In Formulation Example 2, a 50% ethanol extract of Atemoya peel (Production Example 4) was replaced with purified water to obtain a conventional cream.
処方例3 乳液
処方 配合量
1.アテモヤ果実の熱水抽出物(製造例2) 0.001部
2.スクワラン 5.0
3.オリーブ油 5.0
4.ホホバ油 5.0
5.セタノール 1.5
6.モノステアリン酸グリセリン 2.0
7.ポリオキシエチレンセチルエーテル(20E.O.) 3.0
8.ポリオキシエチレンソルビタンモノオレエート
(20E.O.) 2.0
9.香料 0.1
10.プロピレングリコール 1.0
11.グリセリン 2.0
12.パラオキシ安息香酸メチル 0.2
13.精製水にて全量を100とする
[製造方法]成分2〜8を加熱溶解して混合し、70℃に保ち油相とする。成分1及び10〜13を加熱溶解して混合し、75℃に保ち水相とする。油相に水相を加えて乳化して、かき混ぜながら冷却し、45℃で成分9を加え、更に30℃まで冷却して製品とする。
Formulation Example 3 Emulsion Formulation Formulation 1. 1. Hot water extract of Atemoya fruit (Production Example 2) 0.001 part Squalane 5.0
3. Olive oil 5.0
4). Jojoba oil 5.0
5. Cetanol 1.5
6). Glycerol monostearate 2.0
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Polyoxyethylene sorbitan monooleate (20E.O.) 2.0
9. Fragrance 0.1
10. Propylene glycol 1.0
11. Glycerin 2.0
12 Methyl paraoxybenzoate 0.2
13. Make the total volume 100 with purified water
[Manufacturing method] Components 2 to 8 are dissolved by heating and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 10-13 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring. The component 9 is added at 45 ° C., and further cooled to 30 ° C. to obtain a product.
処方例4 ゲル剤
処方 配合量
1.アテモヤ果皮の50%エタノール抽出物(製造例4) 1.0部
2.エタノール 5.0
3.パラオキシ安息香酸メチル 0.1
4.ポリオキシエチレン硬化ヒマシ油(60E.O.) 0.1
5.香料 適量
6.1,3−ブチレングリコール 5.0
7.グリセリン 5.0
8.キサンタンガム 0.1
9.カルボキシビニルポリマー 0.2
10.水酸化カリウム 0.2
11.精製水にて全量を100とする
[製造方法]成分2〜5と、成分1及び6〜11をそれぞれ均一に溶解し、両者を混合して製品とする。
Formulation Example 4 Gel formulation Formulation amount 1. 1. 50 parts ethanol extract of Atemoya peel (Production Example 4) 1.0 part Ethanol 5.0
3. Methyl paraoxybenzoate 0.1
4). Polyoxyethylene hydrogenated castor oil (60 EO) 0.1
5. Perfume
6.1,3-Butylene glycol 5.0
7). Glycerin 5.0
8). Xanthan gum 0.1
9. Carboxyvinyl polymer 0.2
10. Potassium hydroxide 0.2
11. [Production method] Ingredients 2 to 5 and ingredients 1 and 6 to 11 are uniformly dissolved in purified water, and the two are mixed to obtain a product.
処方例5 パック
処方 配合量
1.アテモヤ果皮の熱水抽出物(製造例1) 0.1部
2.アテモヤ果皮の50%エタノール抽出物(製造例4) 0.1
3.ポリビニルアルコール 12.0
4.エタノール 5.0
5.1,3−ブチレングリコール 8.0
6.パラオキシ安息香酸メチル 0.2
7.ポリオキシエチレン硬化ヒマシ油(20E.O.) 0.5
8.クエン酸 0.1
9.クエン酸ナトリウム 0.3
10.香料 適量
11.精製水にて全量を100とする
[製造方法]成分1〜11を均一に溶解し製品とする。
Formulation Example 5 Pack Formulation Formulation 1. 1. Hot water extract of Atemoya peel (Production Example 1) 0.1 part 50% ethanol extract of Atemoya peel (Production Example 4) 0.1
3. Polyvinyl alcohol 12.0
4). Ethanol 5.0
5.1,3-Butylene glycol 8.0
6). Methyl paraoxybenzoate 0.2
7). Polyoxyethylene hydrogenated castor oil (20 EO) 0.5
8). Citric acid 0.1
9. Sodium citrate 0.3
10. Perfume proper amount11. [Production Method] Components 1 to 11 are uniformly dissolved in purified water to make a total amount of 100 to obtain a product.
処方例6 ファンデーション
処方 配合量
1.アテモヤ果皮のエタノール抽出物(製造例5) 1.0部
2.ステアリン酸 2.4
3.ポリオキシエチレンソルビタンモノステアレート
(20E.O.) 1.0
4.ポリオキシエチレンセチルエーテル(20E.O.) 2.0
5.セタノール 1.0
6.液状ラノリン 2.0
7.流動パラフィン 3.0
8.ミリスチン酸イソプロピル 6.5
9.カルボキシメチルセルロースナトリウム 0.1
10.ベントナイト 0.5
11.プロピレングリコール 4.0
12.トリエタノールアミン 1.1
13.パラオキシ安息香酸メチル 0.2
14.二酸化チタン 8.0
15.タルク 4.0
16.ベンガラ 1.0
17.黄酸化鉄 2.0
18.香料 適量
19.精製水にて全量を100とする
[製造方法]成分2〜8を加熱溶解し、80℃に保ち油相とする。成分19に成分9をよく膨潤させ、続いて、成分1及び10〜13を加えて均一に混合する。これに粉砕機で粉砕混合した成分14〜17を加え、ホモミキサーで撹拌し75℃に保ち水相とする。この水相に油相をかき混ぜながら加え、冷却し、45℃で成分18を加え、かき混ぜながら30℃まで冷却して製品とする。
Formulation Example 6 Foundation Formulation Amount Ethanol extract of Atemoya peel (Production Example 5) 1.0 part Stearic acid 2.4
3. Polyoxyethylene sorbitan monostearate (20EO) 1.0
4). Polyoxyethylene cetyl ether (20E.O.) 2.0
5. Cetanol 1.0
6). Liquid lanolin 2.0
7). Liquid paraffin 3.0
8). Isopropyl myristate 6.5
9. Sodium carboxymethylcellulose 0.1
10. Bentonite 0.5
11. Propylene glycol 4.0
12 Triethanolamine 1.1
13. Methyl paraoxybenzoate 0.2
14 Titanium dioxide 8.0
15. Talc 4.0
16. Bengala 1.0
17. Yellow iron oxide 2.0
18. Perfume proper amount19. [Manufacturing method] Components 2 to 8 are heated and dissolved in purified water to a total amount of 100, and kept at 80 ° C to obtain an oil phase. Swell component 9 well in component 19, then add components 1 and 10-13 and mix uniformly. To this, components 14 to 17 pulverized and mixed with a pulverizer are added, and the mixture is stirred with a homomixer and kept at 75 ° C. to obtain an aqueous phase. The oil phase is added to this aqueous phase with stirring, cooled, component 18 is added at 45 ° C., and cooled to 30 ° C. with stirring to give a product.
処方例7 浴用剤
処方 配合量
1.アテモヤ種子の熱水抽出物(製造例3) 5.0部
2.炭酸水素ナトリウム 50.0
3.黄色202号(1) 適量
4.香料 適量
5.硫酸ナトリウムにて全量を100とする
[製造方法]成分1〜5を均一に混合し製品とする。
Formulation Example 7 Bath preparation formulation 1. Atomoya seed hot water extract (Production Example 3) 5.0 parts Sodium bicarbonate 50.0
3. Yellow No. 202 (1) Appropriate amount 4. Perfume appropriate amount 5. [Manufacturing method] Ingredients 1 to 5 are mixed uniformly with sodium sulfate to make a product.
処方例8 軟膏
処方 配合量
1.アテモヤ果皮の熱水抽出物(製造例1) 0.01部
2.アテモヤ果皮の50%エタノール抽出物(製造例4) 0.5
3.ポリオキシエチレンセチルエーテル(30E.O.) 2.0
4.モノステアリン酸グリセリン 10.0
5.流動パラフィン 5.0
6.セタノール 6.0
7.パラオキシ安息香酸メチル 0.1
8.プロピレングリコール 10.0
9.精製水にて全量を100とする
[製造方法]成分3〜6を加熱溶解して混合し、70℃に保ち油相とする。成分1、2及び7〜9を加熱溶解して混合し、75℃に保ち水相とする。油相に水相を加えて乳化して、かき混ぜながら30℃まで冷却して製品とする。
次に、本発明の効果を詳細に説明するため、実験例を挙げる。
Formulation Example 8 Ointment Formulation Formulation 1. 1. Hot water extract of Atemoya peel (Production Example 1) 0.01 part 50% ethanol extract of Atemoya peel (Production Example 4) 0.5
3. Polyoxyethylene cetyl ether (30E.O.) 2.0
4). Glycerol monostearate 10.0
5. Liquid paraffin 5.0
6). Cetanol 6.0
7). Methyl paraoxybenzoate 0.1
8). Propylene glycol 10.0
9. [Production Method] Components 3 to 6 are heated and dissolved and mixed with purified water to a total amount of 100, and kept at 70 ° C. to obtain an oil phase. Ingredients 1, 2, and 7-9 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled to 30 ° C. with stirring to obtain a product.
Next, experimental examples will be given to explain the effects of the present invention in detail.
実験例1 ヒト皮膚繊維芽細胞NB1RGBを用いた過酸化脂質生成抑制作用
紫外線による繊維芽細胞の過酸化脂質生成抑制効果をTBA法にて測定した。
Experimental Example 1 Lipid peroxide production inhibitory action using human skin fibroblasts NB1RGB The lipid peroxide production inhibitory effect of fibroblasts by ultraviolet rays was measured by the TBA method.
試料は製造例1、4及び5を用いた。 Samples 1, 4, and 5 were used as samples.
対数増殖期にある繊維芽細胞をφ60mmdishに3×104細胞播種し、Eagles’MEM(10%FBSを含む)を加え、37℃、5%CO2条件下にて培養した。培養6日後に最終濃度1.0mg/mLになるように試料を加えたPBSを添加し、37℃、5%CO2条件下にて30分培養後、UVA(6.5J/cm2)を照射した。照射後、細胞をdishから剥離し、細胞を超音波破砕した後、細胞破砕液0.2mLに、8.1%SDS0.2mL、20%酢酸(pH3.5)1.5mL、0.8%チオバルビツール酸ナトリウム1.5mL、蒸留水0.6mLを加え、よく攪拌した。さらに400mM BHT0.01mLを加え、100℃で1時間反応させた。冷却後、反応液2mLに6.25%ピリジン含有n−ブチルアルコール溶液2mLを加え、よく攪拌した後、遠心分離し、n−ブチルアルコール層の蛍光強度(励起波長515nm、蛍光波長553nm)を測定し、過酸化脂質量とした。さらに、紫外線を照射しないものを作成し、紫外線照射したものとの差を過酸化脂質生成量とした。過酸化脂質生成抑制率は、試料の代わりに溶媒のみを添加した場合の過酸化脂質生成量を100とし、試料添加時の過酸化脂質生成量との割合から算出した。 Fibroblasts in the logarithmic growth phase were seeded at 3 × 10 4 cells in a φ60 mm dish, Eagles'MEM (containing 10% FBS) was added, and the cells were cultured at 37 ° C. under 5% CO 2 conditions. PBS added with a sample to a final concentration of 1.0 mg / mL after 6 days of culture was added, cultured at 37 ° C. under 5% CO 2 for 30 minutes, and then irradiated with UVA (6.5 J / cm 2). . After irradiation, the cells were detached from the dish, and the cells were ultrasonically disrupted. Then, 0.2 mL of the cell disruption solution, 0.2 mL of 8.1% SDS, 1.5 mL of 20% acetic acid (pH 3.5), 0.8% Sodium thiobarbiturate 1.5mL and distilled water 0.6mL were added and stirred well. Further, 0.01 mL of 400 mM BHT was added and reacted at 100 ° C. for 1 hour. After cooling, add 2 mL of 6.25% pyridine-containing n-butyl alcohol solution to 2 mL of the reaction solution, stir well, and centrifuge to measure the fluorescence intensity (excitation wavelength 515 nm, fluorescence wavelength 553 nm) of the n-butyl alcohol layer. And the amount of lipid peroxide. Furthermore, the thing which did not irradiate with an ultraviolet-ray was created, and the difference from what was irradiated with an ultraviolet-ray was made into the amount of lipid peroxide production. The lipid peroxide production inhibition rate was calculated from the ratio of the amount of lipid peroxide produced when the sample was added, with the amount of lipid peroxide produced when only the solvent was added instead of the sample being 100.
これらの結果を表1に示した。アテモヤ果皮の抽出物は極めて高い過酸化脂質生成抑制作用を有していることが認められた。 These results are shown in Table 1. It was found that the extract of Atemoya peel has an extremely high lipid peroxide production inhibitory action.
実験例2 MMP活性阻害試験 Experimental Example 2 MMP activity inhibition test
試料は製造例1、3、4及び5を用いた。 Production examples 1, 3, 4 and 5 were used as samples.
0.6mg/mLのゼラチンを含む10%SDS−PAGEゲル(1mm厚)を作製し、線維芽細胞の培養上清0.015mLを非還元条件下で電気泳動した。その後、ゲルを2.5%TritonX−100(SIGMA社製)の溶液にて室温で30分間2回洗浄してSDSを除去し、200mM塩化ナトリウム、5mM塩化カルシウム、0.01%brij−35(SIGMA社製)を含む30mMトリス塩酸緩衝液(pH7.6)中にて37℃で24時間インキュベートした。この際、ゲルを浸した緩衝液中に試料を添加した。反応終了後ゲルを0.2%クマシーブリリアントブルーR(SIGMA社製)の溶液にて染色し、5%メタノール−7.5%酢酸溶液にて脱色した。青色のゲル上で染色されないバンドとして検出される72kDa付近のバンドにおけるコラゲナーゼ活性をデンシトメーター(アトー社製、アトーデンシトグラフ、AE−6905)にて定量化し、活性阻害率を算出した。阻害率の計算は、試料を添加していない場合のデンシトメーターの数値を100とし、試料添加時の数値との割合から算出した。 A 10% SDS-PAGE gel (1 mm thickness) containing 0.6 mg / mL gelatin was prepared, and 0.015 mL of the culture supernatant of fibroblasts was electrophoresed under non-reducing conditions. Thereafter, the gel was washed twice with a solution of 2.5% Triton X-100 (manufactured by SIGMA) at room temperature for 30 minutes to remove SDS, and 200 mM sodium chloride, 5 mM calcium chloride, 0.01% brij-35 ( Incubation was carried out at 37 ° C. for 24 hours in 30 mM Tris-HCl buffer (pH 7.6) containing SIGMA. At this time, the sample was added to a buffer solution in which the gel was immersed. After completion of the reaction, the gel was stained with a solution of 0.2% Coomassie Brilliant Blue R (manufactured by SIGMA) and decolorized with a 5% methanol-7.5% acetic acid solution. Collagenase activity in a band near 72 kDa detected as a non-stained band on a blue gel was quantified with a densitometer (Atoden, Atodensitograph, AE-6905), and the activity inhibition rate was calculated. The inhibition rate was calculated from the ratio of the densitometer value when the sample was not added to 100 and the value when the sample was added.
これらの結果を表2に示した。アテモヤの抽出物は極めて高いMMP活性阻害作用を有していることが認められた。 These results are shown in Table 2. It was confirmed that the extract of Atemoya has an extremely high inhibitory action on MMP activity.
実験例3 ヒスタミン遊離抑制試験 Experimental Example 3 Histamine release inhibition test
試料は製造例1、4及び5を用いた。 Samples 1, 4, and 5 were used as samples.
Wister系雄性ラット(8週齢)腹腔から採取した肥満細胞浮遊液を2×105個/mLとなるように調整し、その650μLにIgE抗体を含むラット血清の8倍希釈液320μLを加え、37℃で30分インキュベートした。次に、試料を1.0あるいは0.3mg/mLとなるように加え、37℃で10分間インキュベートした。さらに、卵白アルブミン20μg及びフォスファチジルセリン30μgを加え、37℃で20分間インキュベートして抗原刺激を行った後、肥満細胞浮遊液を4℃に冷却し、反応を停止させた。十分に冷却した後、3,000回転で5分間遠心分離し、遊離したヒスタミンを含む上清を回収した。上清のヒスタミンは、n−ヘプタン中で塩酸を加えてヒスタミン塩酸塩とした後、o−フタルアルデヒド法により、蛍光強度を測定することにより定量した。 A mast cell suspension collected from the abdominal cavity of Wister male rats (8 weeks old) was adjusted to 2 × 10 5 cells / mL, and 320 μL of an 8-fold dilution of rat serum containing IgE antibody was added to 650 μL of the suspension. Incubated for 30 minutes at ° C. Next, the sample was added to 1.0 or 0.3 mg / mL and incubated at 37 ° C. for 10 minutes. Furthermore, after adding 20 μg of ovalbumin and 30 μg of phosphatidylserine and incubating at 37 ° C. for 20 minutes for antigen stimulation, the mast cell suspension was cooled to 4 ° C. to stop the reaction. After cooling sufficiently, the mixture was centrifuged at 3,000 rpm for 5 minutes, and the supernatant containing the released histamine was collected. The supernatant histamine was quantified by adding hydrochloric acid in n-heptane to form histamine hydrochloride, and then measuring the fluorescence intensity by the o-phthalaldehyde method.
これらの結果を表3に示した。アテモヤ果皮の抽出物は極めて高いヒスタミン遊離抑制作用を有していることが認められた。 These results are shown in Table 3. It was confirmed that the extract of Atemoya pericarp has a very high inhibitory action on histamine release.
実験例4 使用試験1
処方例1の化粧水、処方例2のクリーム、比較例1の従来の化粧水及び比較例2の従来のクリームを用いて、女性20人(21〜46才)を対象に1ヶ月間の使用試験を行った。使用後、肌のシワの改善効果をアンケートにより判定した。
Experimental example 4 Use test 1
One month use for 20 women (21 to 46 years old) using the lotion of Formulation Example 1, the cream of Formulation Example 2, the conventional lotion of Comparative Example 1 and the conventional cream of Comparative Example 2. A test was conducted. After use, the effect of improving skin wrinkles was determined by a questionnaire.
これらの試験結果を表4に示した。アテモヤの抽出物を含有する皮膚外用剤は優れたシワの改善作用を示した。なお、試験期間中、皮膚トラブルは一人もなく、安全性においても問題なかった。また、処方成分の劣化についても問題なかった。 The test results are shown in Table 4. The topical skin preparation containing the extract of Atemoya showed an excellent wrinkle-improving action. During the test period, there was no skin problem and there was no problem with safety. There was also no problem with the deterioration of the prescription ingredients.
実験例5 使用試験2
処方例1の化粧水、処方例2のクリーム、比較例1の従来の化粧水及び比較例2の従来のクリームを用いて、肌荒れに悩む女性20人(21〜46才)を対象に1ヶ月間の使用試験を行った。使用後、肌荒れの改善効果をアンケートにより判定した。
Experiment 5 Use test 2
One month for 20 women (21 to 46 years old) who suffer from rough skin using the lotion of Formulation Example 1, the cream of Formulation Example 2, the conventional lotion of Comparative Example 1 and the conventional cream of Comparative Example 2 A usage test was conducted. After use, the improvement effect of rough skin was judged by a questionnaire.
これらの試験結果を表5に示した。アテモヤの抽出物を含有する皮膚外用剤は、優れた肌荒れの改善作用を示した。なお、試験期間中、皮膚トラブルは一人もなく、安全性においても問題なかった。また、処方成分の劣化についても問題なかった。 The test results are shown in Table 5. The external preparation for skin containing the extract of Atemoya showed an excellent effect of improving rough skin. During the test period, there was no skin problem and there was no problem with safety. There was also no problem with the deterioration of the prescription ingredients.
実施例3〜8についても同様に使用試験を行ったところ、優れたシワ、肌荒れ等の改善作用を示した。 Examples 3 to 8 were also tested in the same manner, and showed excellent improving effects such as wrinkles and rough skin.
以上のことから、本発明のアテモヤの抽出物は、優れた過酸化脂質生成抑制作用、MMP活性阻害及びヒスタミン遊離抑制作用を有し、安全性が高く、化粧品、食品、医薬品などに利用可能である。
From the above, the extract of Atemoya of the present invention has an excellent lipid peroxide production inhibitory action, MMP activity inhibitory action and histamine release inhibitory action, is highly safe, and can be used for cosmetics, foods, pharmaceuticals and the like. is there.
Claims (3)
An anti-inflammatory agent comprising an extract of Atemoya.
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JP2017210417A (en) * | 2016-05-24 | 2017-11-30 | 日本メナード化粧品株式会社 | Absorption enhancer |
US10603270B2 (en) | 2013-10-30 | 2020-03-31 | Unigen, Inc. | Skin care compositions and methods of use thereof |
CN113116770A (en) * | 2019-12-26 | 2021-07-16 | 大江生医股份有限公司 | Use of pineapple custard juice in composition for improving skin condition |
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JP2001172157A (en) * | 1999-12-17 | 2001-06-26 | Shiseido Co Ltd | Gelatinase activity inhibitor and anti-aging skin preparation for external use |
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JP2001220312A (en) * | 2000-02-09 | 2001-08-14 | Ichimaru Pharcos Co Ltd | Cosmetic composition containing steam distillate of plant |
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JP2005521649A (en) * | 2002-01-15 | 2005-07-21 | コグニス・フランス・ソシエテ・アノニム | Active substances for use in cosmetic and / or pharmaceutical products obtained by fermentation of plant components and / or plant extracts |
JP2006249051A (en) * | 2005-03-14 | 2006-09-21 | Kyoei Kagaku Kogyo Kk | Fibroblast-activator and skin lotion containing the same |
FR2895906A1 (en) * | 2006-01-06 | 2007-07-13 | Limousine D Applic Biolog Dite | Use of an active ingredient obtained from Annona squamosa for a cosmetic composition e.g. to fight against cutaneous aging, appearance of wrinkles and to improve the biomechanical properties of the skin |
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JP2001172157A (en) * | 1999-12-17 | 2001-06-26 | Shiseido Co Ltd | Gelatinase activity inhibitor and anti-aging skin preparation for external use |
JP2001181129A (en) * | 1999-12-28 | 2001-07-03 | Shiseido Co Ltd | Collagenase activity inhibitor |
JP2001220312A (en) * | 2000-02-09 | 2001-08-14 | Ichimaru Pharcos Co Ltd | Cosmetic composition containing steam distillate of plant |
JP2001335494A (en) * | 2000-05-29 | 2001-12-04 | Okinawa Shokuryo Kk | Angiotensin-converting enzyme inhibitor |
JP2005521649A (en) * | 2002-01-15 | 2005-07-21 | コグニス・フランス・ソシエテ・アノニム | Active substances for use in cosmetic and / or pharmaceutical products obtained by fermentation of plant components and / or plant extracts |
JP2004059525A (en) * | 2002-07-30 | 2004-02-26 | Ogawa & Co Ltd | Antibacterial composition |
JP2006249051A (en) * | 2005-03-14 | 2006-09-21 | Kyoei Kagaku Kogyo Kk | Fibroblast-activator and skin lotion containing the same |
FR2895906A1 (en) * | 2006-01-06 | 2007-07-13 | Limousine D Applic Biolog Dite | Use of an active ingredient obtained from Annona squamosa for a cosmetic composition e.g. to fight against cutaneous aging, appearance of wrinkles and to improve the biomechanical properties of the skin |
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Cited By (4)
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US10603270B2 (en) | 2013-10-30 | 2020-03-31 | Unigen, Inc. | Skin care compositions and methods of use thereof |
JP2017210417A (en) * | 2016-05-24 | 2017-11-30 | 日本メナード化粧品株式会社 | Absorption enhancer |
CN113116770A (en) * | 2019-12-26 | 2021-07-16 | 大江生医股份有限公司 | Use of pineapple custard juice in composition for improving skin condition |
CN113116770B (en) * | 2019-12-26 | 2023-08-29 | 大江生医股份有限公司 | Use of pineapple Sakya juice in cosmetic composition for improving skin condition |
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