WO2009084200A1 - ニキビ肌用皮膚外用剤 - Google Patents
ニキビ肌用皮膚外用剤 Download PDFInfo
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- WO2009084200A1 WO2009084200A1 PCT/JP2008/003956 JP2008003956W WO2009084200A1 WO 2009084200 A1 WO2009084200 A1 WO 2009084200A1 JP 2008003956 W JP2008003956 W JP 2008003956W WO 2009084200 A1 WO2009084200 A1 WO 2009084200A1
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- Prior art keywords
- skin
- rhododendrol
- acne
- derivatives
- extract
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- 0 CC(CCc(cc1)ccc1O*)O Chemical compound CC(CCc(cc1)ccc1O*)O 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
- A61K36/282—Artemisia, e.g. wormwood or sagebrush
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/35—Caprifoliaceae (Honeysuckle family)
- A61K36/355—Lonicera (honeysuckle)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/65—Paeoniaceae (Peony family), e.g. Chinese peony
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/72—Rhamnaceae (Buckthorn family), e.g. buckthorn, chewstick or umbrella-tree
- A61K36/725—Ziziphus, e.g. jujube
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/74—Rubiaceae (Madder family)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/75—Rutaceae (Rue family)
- A61K36/752—Citrus, e.g. lime, orange or lemon
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/75—Rutaceae (Rue family)
- A61K36/756—Phellodendron, e.g. corktree
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/347—Phenols
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/37—Esters of carboxylic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/008—Preparations for oily skin
Definitions
- the present invention is a highly safe skin external preparation for acne skin, which is excellent in preventing and improving acne scar pigmentation in addition to preventing and improving acne, and P.I. acnes compositions.
- the pathology of acne can be broadly divided into 1) comedones that are non-inflammatory skin rashes, 2) inflammatory papules such as red papules, 3) scars, and 4) post-inflammation pigmentation.
- the treatment is performed by one or a combination of the following three treatment methods: 1) topical external therapy, 2) systemic internal use therapy, and 3) physical therapy.
- topical external therapy is regarded as an effective treatment method for symptoms other than scarring, and external preparations containing various active ingredients have been developed so far (Non-patent Document 1).
- the mechanism of acne development is divided into two major stages.
- the first stage is comedone formation and the second stage is inflammation.
- the comedones are formed when the pores are blocked and sebum is stored in the hair follicles due to excessive sebum secretion and increased keratinization of the pores.
- comedones are a habitat suitable for the anaerobic bacterium Propionibacterium acnes (hereinafter abbreviated as P. acnes) which is a skin resident bacteria, the number of bacteria increases in comedones. Since an extracellular inflammation-inducing substance is produced, inflammatory papules such as red papules are induced (Non-patent Document 2).
- Measures to prevent and improve acne include cleansing to prevent sebum (triglyceride) and keratin thickening that cause pore closure, use of antiseborrheic agents such as vitamin B6, early exfoliation of unnecessary keratin due to resorcin, salicylic acid, etc.
- antiseborrheic agents such as vitamin B6, early exfoliation of unnecessary keratin due to resorcin, salicylic acid, etc.
- Prevention of deterioration by an antibacterial substance having a high bactericidal effect such as isopropylmethylphenol that inhibits the growth of acnes, and the use of anti-inflammatory agents are known (Non-patent Document 3).
- Non-patent Document 1 topical topical therapy with vitamin C (ascorbic acid) derivative has attracted attention (Non-patent Document 1), and further, a tyrosinase activity inhibitor and an antibacterial or anti-acne agent are combined.
- Patent Documents 1 and 2 methods for preventing or improving the darkening of acne scars have been reported.
- Acne prevention and improvement technologies using plant extracts include antibacterial / bactericidal activity, sebum suppression / absorption activity, lipase inhibitory activity, testosterone 5 ⁇ -reductase inhibitory activity, androgen receptor binding inhibitory activity of plant extract.
- the utilized technology has been reported (see Patent Documents 4 to 8).
- rhododendrol and its derivatives, meguslinoki extract containing rhododendrol are known as ingredients that prevent and improve skin pigmentation such as stains and freckles (see Patent Documents 9 to 11). It is not known about specific antibacterial effects such as rhododendrol.
- JP 2002-145802 A Japanese Patent No. 2883368 Japanese Patent No. 3524169 JP-A-3-39710 JP 2002-145793 A JP 2004-161623 A Japanese Patent Laying-Open No. 2005-8572 JP 2006-241059
- a Japanese Patent No. 3340928 Japanese Patent No. 3340935 Japanese Patent No. 3455406 FRAGRANCE JOURNAL, 2007, Vol. 35, No. 5, p. 12-17 COSMETIC STAGE, 2007, Vol. 1, No. 5, p. 23-27 FRAGRANCE JOURNAL, 2003, Vol. 31, No. 3, p. 23-28
- the present invention includes a skin external preparation for acne skin characterized by containing at least one selected from rhododendrol represented by the following general formula (1) and derivatives thereof, and anti-P.
- An acnes composition is provided.
- R is a hydrogen atom, an acyl group having 2 to 20 carbon atoms, or a sugar residue of a monosaccharide or disaccharide.
- the present invention provides at least one skin external preparation for acne skin and anti-P.
- the use for the production of acnes compositions is provided.
- the present invention relates to a method for treating acne, wherein at least one selected from the above-mentioned rhododendrol and derivatives thereof is applied to the skin.
- the present invention provides a method for treating acnes infection.
- the present invention provides an acne skin preparation for skin acne that is excellent in acne prevention and improvement effects and that can prevent and improve the pigmentation of acne scars.
- the present inventor has developed a skin external preparation for acne skin and anti-P.
- rhododendrol or its derivatives have low skin irritation and P. acne causing bacteria. It has an excellent growth inhibitory effect against acnes, and S. acnes is superior to conventional anti-acne components. It has been found that it has a weak action against resident bacteria that are inherently useful for the skin, such as epidermidis, and has a higher effect of preventing and improving acne scars than ascorbic acid and arbutin.
- the external preparation for skin of the present invention is excellent in preventing and improving acne, which is one of skin troubles, and preventing and improving acne scar pigmentation. Further, it does not unnecessarily inhibit the growth of resident skin bacterium useful for maintaining normal skin barrier function. Furthermore, the irritation to the skin is suppressed, and it has characteristics that are rich in safety as an external preparation for skin.
- the rhododendrol [4- (p-hydroxyphenyl) -2-butanol] in which R is a hydrogen atom in the above general formula (1), which is used in the present invention, is a known compound, and is also known as Acer nikenkoce maxim. .)) And the like.
- the rhododendrol may be synthesized by a conventionally known method or a commercially available product may be used. Moreover, you may use what was refine
- the rhododendrol and rhododendrol derivatives used in the present invention have optical isomers, but the (+) isomer, the ( ⁇ ) isomer alone, or a mixture thereof [denoted as ( ⁇ ), -251548] can also be used.
- acylated rhododendrol in which R is an acyl group having 2 to 20 carbon atoms is particularly limited as long as it is generally used. Is not to be done.
- the acylated rhododendrol can be easily obtained by acylating the rhododendrol by a conventionally known method.
- examples of the acyl group include an acetyl group, a propionyl group, a butyryl group, a pentanoyl group, a hexanoyl group, a decanoyl group, and a lauroyl group.
- acylated rhododendrol used in the present invention include (+) isomer, ( ⁇ ) isomer, and ( ⁇ ) such as hexanoyl rhododendrol and acetyl rhododendrol.
- the sugar residue in the rhododendrol glycoside where R is a sugar residue is a reducing monosaccharide or disaccharide.
- Specific examples include monosaccharides such as glucose, galactose, xylose, mannose and N-acetylglucosamine, and disaccharides such as maltose, cellobiose and gentibiose.
- the glycoside of the present invention has an isomer having an ⁇ bond or a ⁇ bond, but can be used alone or in a mixture thereof.
- the rhododendrol glycoside of the present invention can be obtained using a method already known as a method for synthesizing arbutin (USP No. 3121385).
- a method for synthesizing arbutin USP No. 3121385.
- Rhododendrol glycoside can be easily obtained as white powder crystals. It can also be obtained by reducing raspberry ketone glycosides. It is also possible to isolate from natural products.
- the glycosides of the present invention have optical isomers, but (+) isomer, ( ⁇ ) isomer alone or a mixture ( ⁇ ) thereof can also be used.
- glycosides used in the present invention include rhododendrol-D-glucoside ( ⁇ and / or ⁇ form), rhododendrol-D-galactoside ( ⁇ and / or ⁇ form), rhododendrol— (+) Isomer, (-) isomer, ( ⁇ ), such as D-xyloside ( ⁇ and / or ⁇ isomer), rhododendrol-D-maltoside ( ⁇ and / or ⁇ isomer) can be mentioned.
- anti-P Acnes action is strong and anti-P.
- Rhodendrol is particularly preferred because of the large difference between the acnes action and the antibacterial action against skin resident bacteria.
- rhododendrol As for the content of rhododendrol or a derivative thereof used in the present invention, in the case of rhododendrol in which R is a hydrogen atom in the general formula (1), 0.1 to about 0.1 to the total amount of the external preparation for skin or composition. 5% by mass, more preferably 0.3 to 5% by mass, and particularly preferably 0.4 to 3% by mass. Further, in the case of acylated rhododendrol in which R is an acyl group having 2 to 20 carbon atoms, 0.1 to 7% by mass, further 0.3 to 6% by mass, especially 0.3% based on the total amount of the external preparation for skin. 5 to 5% by mass is preferable.
- rhododendrol glycoside in which R is a sugar residue, 0.1 to 7% by mass, further 0.3 to 6% by mass, especially 0.5 to 5% by mass based on the total amount of the external preparation for skin. % Is preferred. If the content is within these ranges, P.I. In addition to being particularly excellent in antibacterial effects against acnes, the effects on other beneficial skin resident bacteria can be minimized. It is also possible to obtain a wider degree of freedom in the formulation design of the preparation.
- an epidermis cell ceramide synthesis promoting substance and / or a plant extract having an inflammation-inhibiting effect is added to the skin external preparation for acne skin, thereby further preventing and improving acne and preventing acne scars. It is possible to enhance the prevention / improvement effect.
- Examples of the epidermal cell ceramide synthesis promoting substance in the present invention include nicotinamide, carnitine, yeast extract or a bacterial culture containing the same. In this invention, it is possible to mix
- Nicotinamide used in the present invention is a known substance, and it can be extracted from a natural product (rice bran or the like) or synthesized by a known method.
- the content of nicotinamide in the present invention is preferably 0.1 to 10% by mass, particularly preferably 0.2 to 8% by mass, based on the total amount of the external preparation for skin or composition.
- Carnitine used in the present invention is 4-trimethylamino-3-hydroxybutyric acid and is a known substance.
- Carnitine in the present application refers to L-carnitine, DL-carnitine and their hydrochlorides and derivatives thereof.
- carnitine chloride which is a hydrochloride of carnitine, particularly levocarnitine chloride which is a hydrochloride of L-carnitine is preferably used.
- the formulation of carnitine and their hydrochlorides and their derivatives into skin cosmetics has already been disclosed (Japanese Patent Laid-Open No. 51-148042), and it is also known that carnitine chloride enhances the permeability barrier strength of the epidermis.
- the content of carnitine in the present invention is preferably 0.05 to 5% by mass, particularly preferably 0.1 to 4% by mass, based on the total amount of the external preparation for skin or composition.
- yeast extract or a bacterial culture containing the same used in the present invention include the yeast extract disclosed in JP-A-8-217658 and the bacterial culture containing the same.
- yeast extract include commercially available yeast extract and industrial yeast extract.
- yeast extract for reagent manufactured by Difco
- Cytodyne Brooks Industry
- yeast extract for industrial use Manufactured by Ssu
- chitocatalyzer manufactured by BIO-DELL
- PLANTOSOL manufactured by Arch Personal Care Products LP
- TONISKIN manufactured by Silab.
- Examples of the bacterial culture containing the yeast extract used in the present invention include a lactic acid bacterial culture cultured in a medium containing a yeast extract, a mushroom cell culture, and the like.
- Examples of the lactic acid bacteria include Streptococcus thermophilus, Lactobacillus bulgaricus, Streptococcus lactis, and the mushroom cells include, for example, Lentinus edodes, Shiretake, Pleurotus et al. magnatum (white truffle), Tuber melanosporum (black truffle) and the like.
- Specific examples of the bacterial culture containing a yeast extract include Whey CPA (registered trademark), Fermentation Pear B manufactured by Ichimaru Falcos, Achromatyl handled by Arista Life Sciences, and the like.
- the content of the yeast extract or the bacterial culture containing the same in the present invention is preferably 0.001 to 5% by mass (as a dry solid content) based on the total amount of the external preparation for skin or composition. 0.005 to 0.5% by mass is preferable.
- the amount is preferably 0.005 to 20% by mass, particularly preferably 0.01 to 10% by mass (as a dry solid) based on the total amount of the external preparation for skin or composition. If the content is within the above-mentioned preferable range, the prevention / improvement of acne and the enhancement of the effect of preventing / ameliorating acne scars are particularly excellent, and a preparation with good color and odor can be obtained.
- plant extracts having an anti-inflammatory effect in the present invention include sushi (Gardenia florida), peonies (Paeonia albiflora root), goldfish (Lonicera japonica flourt), zizyhus jujuu pits. Extracts from aurantium amara peel, from Phelliendron amurense bark, birch (Betula alba bark), Melissa (Melissa officinalis leaf), and gaiyou (Artemisia princeps).
- blend at least 1 sort (s) or more chosen from these groups from the standpoint of improving the prevention and improvement of acne and the prevention and improvement of acne scars.
- the blending amount of the plant extract having anti-inflammatory effect in the present invention is preferably 0.01 to 20% by mass, more preferably 0.05 to 10% by mass, based on the total amount of the external preparation for skin or composition, as a dry solid content. In particular, 0.1 to 5% by mass is preferable. If the content is within the above preferred range, acne prevention / improvement and enhancement of acne scar prevention / improvement effect are particularly excellent.
- a vitamin B6-related substance known as an anti-seborrheic agent may be formulated with a component selected from the group consisting of pyridoxine, pyridoxine hydrochloride, pyridoxine salts and derivatives thereof to enhance the acne treatment effect.
- a component selected from the group consisting of pyridoxine, pyridoxine hydrochloride, pyridoxine salts and derivatives thereof to enhance the acne treatment effect.
- Specific examples of vitamin B6-related substances include pyridoxine hydrochloride, pyridoxine dicaprylate, pyridoxine dipalmitate, pyridoxine glycyrrhizinate, pyridoxine dilaurate, pyridoxine tripalmitate, pyridoxal phosphate, pyridoxine trihexyldecanoate, and the like.
- Plant extracts include licorice, jujudama, honeysuckle, tonin, gardenia, saxifrage, tea seeds, camellia, orchid, ghetto leaves, apricot juice, wheat germ, rooibos, melia azakura leaf, acerola seeds, camcam fruit, Dutch pepper, Extracts obtained from Ages, Prunes, Black Tea, Oolong Tea, Seaweed, Bud Rye, Carrot, Arnica, Ginkgo, Chamomile, Clara, Sakuhakuhi, Maronie, Hibamata, Tachykosa, and Avocado Oil and Grape Seed Oil.
- fermented products include lotus seed fermentation and soymilk fermentation.
- Medicinal ingredients include ethyl glucoside, sodium hyaluronate, dipotassium glycyrrhizinate, dehydrocreosole, L-alanine, L-proline, L-serine, N-methyl-L-serine, mevalonolactone, flavin adenine dinucleotide 2Na, tocopherol acetate , Tocopherol nicotinate, ⁇ -carotene, ceramide 2, ceramide 3 and the like.
- the skin external preparation or composition of the present invention in addition to the above-mentioned components, other components that are usually blended in pharmaceuticals, quasi drugs, cosmetics, etc., such as oils, as long as the effects of the present invention are not impaired.
- Moisturizers, surfactants, thickeners, preservatives, sequestering agents, pH adjusters, water, alcohols, drugs, UV absorbers, UV scattering agents, dyes, fragrances, etc. are appropriately blended as necessary. be able to.
- Example 1 The antibacterial characteristics of the rhododendrol according to the present invention were evaluated according to the following antibacterial test.
- MIC minimum inhibitory concentration
- a culture medium prepared by adding an evaluation sample to [5000, 10,000, 15000 ⁇ g / mL] or [62.5, 125, 250, 500, 1000, 2000, 4000 ⁇ g / mL] was prepared and shown in Table 1.
- the growth of various microorganisms was evaluated using these media.
- the medium is P.P. acnes for brain heart infusion agar, C.I. For albicans, glucose peptone agar medium is used. For others, soybean, casein, digest agar medium is used. acnes is C.I. Albicans were cultured at 25 ° C. under aerobic conditions for 72 hours, and the others were cultured at 30 ° C. under aerobic conditions for 48 hours, and then their growth was confirmed. The results are shown in Table 2.
- the rhododendrol of the present invention is acnes, E.I. coli, S. et al.
- Antibacterial activity against highly pathogenic bacteria such as Aureus is as strong as resorcin, while S. It can be seen that the antibacterial activity against epidermidis is weak.
- Examples 6 to 11 (external preparation for acne skin) According to the formulation shown in Table 4 below, an external preparation for skin acne (skin lotion) was prepared, and its anti-acne effect and skin irritation were evaluated in the same manner as in the above test. As can be seen from the evaluation results shown in Table 4, each of the anti-acne skin external preparations of the present invention had an excellent effect.
- Examples 12 to 26, Comparative Examples 6 to 7 (Skin preparation for acne skin) According to the formulations shown in Table 5 and Table 6 below, a skin external preparation (emulsion composition) for acne skin was prepared as follows. That is, the components (A) and (B) were uniformly dissolved at 75 ° C., and then the component (B) was added to the agitated component (A), and emulsified and dispersed. (C) component was mix
- the skin external preparation for acne skin of the present invention is excellent in acne prevention / improvement effect, can prevent / improve pigmentation of acne scars, various cosmetics and quasi-drugs with low skin irritation and excellent safety It can be used as a medicine.
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Abstract
Description
また、植物抽出エキスを使用したニキビの予防・改善技術としては、植物抽出エキスの抗菌・殺菌活性、皮脂抑制・吸収活性、リパーゼ阻害活性、テストステロン5α-リダクターゼ阻害活性、アンドロゲン受容体結合阻害活性を利用した技術が報告されている(特許文献4~8参照)。
さらに、本発明は、上記ロドデンドロール及びその誘導体から選ばれる少なくとも1種以上を皮膚に適用することを特徴とするニキビ治療法及びP.acnes感染症治療法を提供するものである。
含有量がこれら範囲であれば、P.acnesに対する抗菌効果が特に優れるだけでなく、他の有益な皮膚常在菌に対する影響を最小限に抑えることができる。また、製剤の処方設計においてもより幅広い自由度を得ることも可能となる。
また、本発明の皮膚外用剤又は組成物には、前記成分の他、公知の植物エキス、発酵物、薬効成分を配合することができる。
植物エキスとしては、甘草、ジュズダマ、スイカズラ、トウニン、クチナシ、ユキノシタ、チャ実、ツバキ、オーキッド、ゲットウ葉、アンズ果汁、小麦胚芽、ルイボス、メリアアザジラクラ葉、アセロラ種子、カムカム果実、オランダガラシ、エイジツ、プルーン、紅茶、ウーロン茶、海藻、ブクリョウ、ニンジン、アルニカ、イチョウ、カミツレ、クララ、ソウハクヒ、マロニエ、ヒバマタ、タチジャコウウソウから得られる抽出エキス、アボカド油、ブドウ種子油が挙げられる。
発酵物としては、ハス種子発酵、豆乳発酵等が挙げられる。
薬効成分としては、エチルグルコシド、ヒアルロン酸ナトリウム、グリチルリチン酸ジカリウム、デヒドロクレオソール、L-アラニン、L-プロリン、L-セリン、N-メチル-L-セリン、メバロノラクトン、フラビンアデニンジヌクレオチド2Na、酢酸トコフェロール、ニコチン酸トコフェロール、β-カロチン、セラミド2、セラミド3等が挙げられる。
本発明に係るロドデンドロールの抗菌性の特徴を、以下の抗菌性試験に従って評価した。
日本化学療法学会標準法の寒天平板希釈法に準じて、最小発育阻止濃度(MIC、単位:μg/mL)を測定することにより抗菌性を評価した。即ち、評価試料を〔5000、10000、15000μg/mL〕、又は〔62.5、125、250、500、1000、2000、4000μg/mL〕となるように添加した培地を調製し、表1に示した各種微生物の増殖性をこれら培地を使用して評価した。培地は、P.acnesについてはブレイン・ハート・インフュージョン寒天培地、C.albicansについてはグルコース・ペプトン寒天培地、その他については・ソイビーン・カゼイン・ダイジェスト寒天培地を用い、P.acnesは37℃、嫌気条件下、C.albicansについては25℃、好気条件下で72時間、その他については30℃、好気条件下で48時間培養した後、それらの増殖性を確認した。結果を表2に示す。
下記表3に示す処方に従って、ニキビ肌用皮膚外用剤(化粧水)を調製し、その抗ニキビ効果と皮膚刺激性を、以下に示す評価法に従って評価した。
・ニキビ改善効果
顔面にニキビを有する18才から30才までの成人10名(男性5名、女性5名)を1群として各評価試料を評価した。朝晩1日2回、同じ洗顔石鹸にて洗顔後、各々の評価試料をブラインドにて使用させた。使用開始前と使用1週間後の顔面のニキビ状態を目視並びに写真撮影にて比較し、症状の変化について「改善」「やや改善」「変化なし」「やや悪化」「悪化」の5段階にて評価した。
前記の「ニキビ改善効果」の評価者にサンプルの継続連用をしてもらい、使用開始から4週間後の顔面のニキビ痕の状態について、目視並びに写真撮影にて、1週間後の状態と比較し、その変化について「改善」「やや改善」「変化なし」「やや悪化」「悪化」の5段階にて評価した。
それぞれ皮膚に対する刺激性を使用評価してもらい、使用中に刺激性を感じたと回答した人数を結果として記載した。
表3に示された評価結果から分かるように、実施例2~5の本発明の皮膚外用剤は、他のどの比較例の皮膚外用剤よりも、ニキビ改善効果、ニキビ痕改善効果において優れていた。また、皮膚刺激感においても、刺激を感じた被験者は比較例と比べて非常に少なかった。
下記表4に示す処方に従って、ニキビ肌用皮膚外用剤(化粧水)を調製し、その抗ニキビ効果と皮膚刺激性を、上記試験と同様に評価した。表4に示された評価結果から分かるように、本発明の抗ニキビ皮膚外用剤はいずれも優れた効果を有するものであった。
下記表5、表6に示す処方に従って、ニキビ肌用皮膚外用剤(乳化組成物)を以下に従って調製した。即ち、(A)成分、(B)成分をそれぞれ75℃にて均一に溶解、次いで(A)成分を攪拌した中へ(B)成分を加え、乳化分散した後、そのまま攪拌しながら温度50℃まで冷却して(C)成分を配合し、温度30℃まで冷却して調製した。
原料成分 配合量(%)
ジプロピレングリコール 12.0
濃グリセリン 5.0
ショ糖脂肪酸エステル(*1) 0.1
モノラウリン酸デカグリセリン 0.05
ロドデンドロール 1.0
エチルグルコシド 0.02
ヒアルロン酸ナトリウム(*2) 0.05
クエン酸 0.01
クエン酸ナトリウム 0.09
フェノキシエタノール 0.1
ニコチン酸アミド 0.5
甘草エキス(*3) 0.1
酵母エキス(注3) 0.1
ハス種子発酵エキス(*4) 0.05
チンピエキス(*5) 0.05
ジュズダマエキス(*6) 0.05
タイソウエキス(*7) 0.05
スイカズラエキス(*8) 0.05
トウニンエキス(*9) 0.05
クチナシエキス(*10) 0.05
ユキノシタエキス(*11) 0.05
チャ実エキス(*12) 0.01
ツバキエキス(*13) 0.01
オーキッドエキス(*14) 0.05
ゲットウ葉エキス(*15) 0.05
精製水 残 量
*1;サーフホープSE COSME C-1216(三菱化学フーズ社製)
*2;ヒアルロン酸FCH-SU(紀文フードケミカル社製)
*3;カンゾウ抽出液BG-J(丸善製薬社製)
*4;蓮醸果(テクノーブル社製)
*5;チンピ抽出液BG(丸善製薬社製)
*6;ヨクイニン抽出液BG-S(丸善製薬社製)
*7;タイソウ抽出液BG-J(丸善製薬社製)
*8;ファルコレックス スイカズラ SB(一丸ファルコス社製)
*9;ファルコレックス トウニン B(一丸ファルコス社製)
*10;ファルコレックス クチナシ B(一丸ファルコス社製)
*11;ユキノシタエキス(一丸ファルコス社製)
*12;茶の実抽出物(丸善製薬社製)
*13;ツバキ種子抽出物(丸善製薬社製)
*14;ファルコレックス ラン(一丸ファルコス社製)
*15;月桃葉抽出液BG(丸善製薬社製)
原料成分 配合量(%)
エタノール 5.0
1,3-ブチレングリコール 4.0
濃グリセリン 2.0
ジグリセリン 1.0
ポリオキシエチレン硬化ヒマシ油(60E.O.) 1.0
モノラウリン酸ポリオキシエチレン 0.3
ソルビタン(20E.O.)
ロドデンドロール-D-グルコシド 2.0
グリチルリチン酸ジカリウム 0.1
リン酸二水素カリウム 0.07
リン酸一水素ナトリウム 0.03
デヒドロジクレオソール 0.01
メチルパラベン 0.1
グリシン 0.01
L-アラニン 0.01
L-プロリン 0.01
L-セリン 0.01
N-メチル-L-セリン 0.1
L-塩化カルニチン 0.5
混合果実抽出液(*16) 0.05
アンズ果汁(*17) 0.05
小麦胚芽エキス(*18) 0.05
ルイボスエキス(*19) 0.05
メリアアザジラクタ葉エキス(*20) 0.05
シラカバエキス(*21) 0.1
シャクヤクエキス(*22) 0.1
トウヒエキス(*23) 0.1
精製水 残 量
*16;マルチフルーツBSC(Arch Personal Care Products社製)
*17;アプリコットエキスK(エスペリス社製)
*18;クラリスキン(Silab社製)
*19;ファルコレックス ルイボスB(N)(一丸ファルコス社製)
*20;ニームリーフリキッド B(一丸ファルコス社製)
*21;シラカバ抽出液BG(丸善製薬社製)
*22;シャクヤク抽出液BG-JC(丸善製薬社製)
*23;トウヒリキッドB(一丸ファルコス社製)
原料成分 配合量(%)
エタノール 10.0
ポリオキシエチレン硬化ヒマシ油(40E.O) 1.0
メチルフェニルポリシロキサン 1.0
ジプロピレングリコール 5.0
濃グリセリン 2.0
ヘキサノロドデンドロール 1.5
ヒアルロン酸ナトリウム(*2) 0.1
カルビキシビニルポリマー 0.3
水酸化カリウム 0.15
フェノキシエタノール 0.1
アセロラ種子抽出物(*24) 0.1
カムカム果実抽出物(*25) 0.1
メリッサエキス(*26) 0.1
ガイヨウエキス(*27) 0.1
メバロノラクトン 0.1
フラビンアデニンジヌクレオチド2Na(*28) 0.01
ニコチン酸アミド 1.0
塩酸ピリドキシン 0.1
トリ2-ヘキシルデカン酸ピリドキシン(*29) 0.1
アスコルビン酸硫酸二ナトリウム(*30) 0.1
酢酸トコフェロール(*31) 0.1
β-カロチン(*32) 0.001
精製水 残 量
*24;ニチレイ・アセロラ種子エキスB30(ニチレイ社製)
*25;ニチレシ・カムカムエキスB30(ニチレイ社製)
*26;ファルコレックス メリッサ B(一丸ファルコ社製)
*27;ガイヨウ抽出液BG(丸善製薬社製)
*28;FAD(協和発酵社製)
*29;NIKKOL VB6-IP(日光ケミカルズ社製)
*30;VC-SS(日本サーファクタント社製)
*31;酢酸dl-α―トコフェロール(エーザイ社製)
*32;βカロチン(ロッシュ社製)
原料成分 配合量(%)
水素添加大豆リン脂質 1.0
コレステロール 0.5
スクワラン 2.0
マカデミアナッツ油脂肪酸フィトステリル 0.5
セラミド2(*33) 0.5
1,3-ブチレングリコール 3.0
濃グリセリン 3.0
ポリグリセリン 1.0
スクワラン 1.0
ロドデンドロール 1.0
ニコチン酸アミド 1.0
ヒアルロン酸ナトリウム(*34) 0.1
アクリル酸メタクリル酸アルキル共重合体 0.05
キサンタンガム 0.05
水酸化ナトリウム 0.02
フェノキシエタノール 0.3
甘草エキス(*3) 0.1
酵母エキス(*4) 0.1
チンピエキス(*5) 0.05
ジュズダマエキス(*6) 0.05
タイソウエキス(*7) 0.05
スイカズラエキス(*8) 0.05
トウニンエキス(*9) 0.05
クチナシエキス(*10) 0.05
ユキノシタエキス(*11) 0.05
チャ実エキス(*12) 0.01
ツバキエキス(*13) 0.01
オーキッドエキス(*14) 0.05
ゲットウ葉エキス(*15) 0.05
精製水 残 量
*33;セラミドTIC-001(高砂香料社製)
*34;ヒアルロン酸FCH(FCH-120)(紀文フードケミカル社製)
原料成分 配合量(%)
セタノール 5.0
親油型モノステアリン酸グリセリン 1.0
ポリオキシエチレンセチルエーテル(2E.O.) 0.1
ショ糖脂肪酸エステル(*35) 0.5
植物性スクワラン 1.0
精製ホホバ油 1.0
精製マカデミア油 0.5
水添ポリイソブテン 0.5
セラミド3(*36) 0.1
ニコチン酸トコフェロール 0.1
トリ2-ヘキシルデカン酸ピリドキシン(*29) 0.1
オリブ油(*37) 0.1
アボガド油(*38) 0.1
ブドウ種子油(*39) 0.1
濃グリセリン 5.0
ロドデンドロール 2.5
塩化レボカルニチン 1.0
オウバクエキス(*40) 0.1
フェノキシエタノール 0.2
クロルフェネシン 0.1
水酸化カリウム 0.3
香料 0.02
精製水 残 量
*35;シュガーワックス A-10E(第一工業製薬社製)
*36;Ceramide IIIA(コスモファーム社製)
*37;クロピュアOL(クローダジャパン社製)
*38;クロピュアアボガド(クローダジャパン社製)
*39;グレープシード油(日光ケミカルズ社製)
*40;オウバク抽出液BG-J(丸善製薬社製)
原料成分 配合量(%)
エタノール 7.0
1,3-ブチレングリコール 5.0
濃グリセリン 5.0
ポリエチレングリコール1000 1.0
リゾレシチン 0.3
ポリオキシエチレン硬化ヒマシ油(40E.O.) 0.5
ジイソステアリン酸ポリグリセリン 0.5
ロドデンドロール-D-グルコシド 2.5
ヒアルロン酸ナトリウム(*2) 0.3
カラギーナン 0.2
フェノキシエタノール 0.2
ファーメンテージセイヨウナシB(注4) 0.1
塩酸ピリドキシン 0.05
チンピエキス(*5) 0.05
ジュズダマエキス(*6) 0.05
タイソウエキス(*7) 0.05
スイカズラエキス(*8) 0.05
トウニンエキス(*9) 0.05
クチナシエキス(*10) 0.05
シャクヤクエキス(*22) 0.05
トウヒエキス(*23) 0.05
豆乳発酵エキス(*41) 0.01
オランダガラシエキス(*42) 0.01
エイジツエキス(*43) 0.01
プルーンエキス(*44) 0.01
紅茶エキス(*45) 0.01
ウーロン茶エキス(*46) 0.01
海藻エキス(*47) 0.01
ブクリョウエキス(*48) 0.01
ニンジンエキス(*49) 0.01
カフェイン(*50) 0.01
アルニカエキス(*51) 0.01
イチョウエキス(*52) 0.01
カミツレエキス(*53) 0.01
クララエキス(*54) 0.01
ソウハクヒエキス(*55) 0.01
マロニエエキス(*56) 0.01
ヒバマタエキス(*57) 0.01
タチジャコウソウエキス(*58) 0.01
精製水 残 量
*41;豆乳発酵液(三省製薬社製)
*42;WATERCRESS KB(Silab社製)
*43;エイジツ抽出液BG-R(丸善製薬社製)
*44;プルーン抽出液WC(丸善製薬社製)
*45;紅茶リキッド(一丸ファルコス社製)
*46;ファルコレックス ウーロン E(一丸ファルコス社製)
*47;Phyco ARL EDTA(Codif社製)
*48;ファルコレックス ブクリョウ B(一丸ファルコス社製)
*49;ファルコレックス ニンジン B(一丸ファルコス社製)
*50;茶の素(白鳥製薬社製)
*51;アルニカ抽出液BG(丸善製薬社製)
*52;イチョウ葉抽出液BG(丸善製薬社製)
*53;カミツレ抽出液BG-J(丸善製薬社製)
*54;ファルコレックス クララB(一丸ファルコス社製)
*55;ファルコレックス ソウハクヒ BG(一丸ファルコス社製)
*56;マロニエ抽出液BG-J(丸善製薬社製)
*57;ファルコレックス ヒバマタ(一丸ファルコス社製)
*58;タチジャコウソウ抽出液BG(丸善製薬社製)
Claims (16)
- ロドデンドロール及びその誘導体から選ばれる1種以上の含有量が0.1~5質量%である請求項1記載のニキビ肌用皮膚外用剤。
- さらにセラミド合成促進物質を含有することを特徴とする、請求項1又は2記載のニキビ肌用皮膚外用剤。
- セラミド合成促進物質が、ニコチン酸アミド、カルニチン、イーストエキス及びそれを含む菌培養物からなる群より選ばれる少なくとも1種以上であることを特徴とする、請求項3記載のニキビ肌用皮膚外用剤。
- さらに炎症抑制効果を有する植物エキスを含有することを特徴とする、請求項1~4のいずれか1項記載のニキビ肌用皮膚外用剤。
- 炎症抑制効果を有する植物エキスが、サンシシ(Gardenia Florida)、シャクヤク(Paeonia Albiflora root)、キンギンカ(Lonicera japonica flower)、タイソウ(Zizyphus jujuba fruit)、チンピ(Citrus unshiu peel)、トウヒ(Citrus aurantium amara peel)、オウバク(Phellodendron amurense bark)、シラカバ(Betula alba bark)、メリッサ(Melissa officinalis leaf)、及びガイヨウ(Artemisia princeps leaf)からなる群から選ばれる少なくとも1種以上からの抽出物であることを特徴とする、請求項5記載のニキビ肌用皮膚外用剤。
- ロドデンドロール及びその誘導体から選ばれる1種以上の含有量が0.1~5質量%である請求項7記載の抗P.acnes組成物。
- ロドデンドロール及びその誘導体から選ばれる1種以上の含有量が0.1~5質量%である請求項9記載の使用。
- ロドデンドロール及びその誘導体から選ばれる1種以上の含有量が0.1~5質量%である請求項11記載の使用。
- ロドデンドロール及びその誘導体から選ばれる1種以上の含有量が0.1~5質量%である組成物を皮膚に適用する請求項13記載のニキビ治療法。
- ロドデンドロール及びその誘導体から選ばれる1種以上の含有量が0.1~5質量%である組成物を皮膚に適用する請求項15記載の治療法。
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Cited By (15)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2011000930A1 (fr) * | 2009-07-01 | 2011-01-06 | Pierre Fabre Dermo-Cosmetique | L-sérine pour son utilisation en tant que médicament pour prévenir et/ou traiter une réaction inflammatoire de la peau |
JP2012006838A (ja) * | 2010-06-22 | 2012-01-12 | Sansho Seiyaku Co Ltd | 皮膚外用剤 |
JP2012144462A (ja) * | 2011-01-11 | 2012-08-02 | Kao Corp | プロスタグランジン産生抑制剤 |
JP2012206973A (ja) * | 2011-03-29 | 2012-10-25 | Nippon Menaade Keshohin Kk | アクネ菌のバイオフィルム形成阻害剤 |
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Also Published As
Publication number | Publication date |
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CN101909586A (zh) | 2010-12-08 |
CN101909586B (zh) | 2013-01-02 |
JPWO2009084200A1 (ja) | 2011-05-12 |
TW200932205A (en) | 2009-08-01 |
KR20100095447A (ko) | 2010-08-30 |
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