JP5774004B2 - ヘキサミジン類とレチノイド類を含有するニキビ改善又は治療組成物 - Google Patents
ヘキサミジン類とレチノイド類を含有するニキビ改善又は治療組成物 Download PDFInfo
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- JP5774004B2 JP5774004B2 JP2012525495A JP2012525495A JP5774004B2 JP 5774004 B2 JP5774004 B2 JP 5774004B2 JP 2012525495 A JP2012525495 A JP 2012525495A JP 2012525495 A JP2012525495 A JP 2012525495A JP 5774004 B2 JP5774004 B2 JP 5774004B2
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- Prior art keywords
- skin
- hexamidine
- composition
- pharmaceutically acceptable
- ceramide
- Prior art date
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- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 description 1
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 229940114079 arachidonic acid Drugs 0.000 description 1
- 235000021342 arachidonic acid Nutrition 0.000 description 1
- 239000012298 atmosphere Substances 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 230000003796 beauty Effects 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000002981 blocking agent Substances 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 159000000007 calcium salts Chemical class 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 230000024245 cell differentiation Effects 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 229940048864 ceramide 1 Drugs 0.000 description 1
- 229940099417 ceramide 2 Drugs 0.000 description 1
- 229940044176 ceramide 3 Drugs 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 229920001436 collagen Polymers 0.000 description 1
- 230000001276 controlling effect Effects 0.000 description 1
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 239000000645 desinfectant Substances 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 210000001339 epidermal cell Anatomy 0.000 description 1
- 210000000981 epithelium Anatomy 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000001815 facial effect Effects 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 239000004088 foaming agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 229960005150 glycerol Drugs 0.000 description 1
- 210000003714 granulocyte Anatomy 0.000 description 1
- 239000007902 hard capsule Substances 0.000 description 1
- 229960000890 hydrocortisone Drugs 0.000 description 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 230000003780 keratinization Effects 0.000 description 1
- 230000002147 killing effect Effects 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000002502 liposome Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 230000036244 malformation Effects 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 239000002609 medium Substances 0.000 description 1
- 210000002752 melanocyte Anatomy 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- CBKLICUQYUTWQL-XWGBWKJCSA-N methyl (3s,4r)-3-methyl-1-(2-phenylethyl)-4-(n-propanoylanilino)piperidine-4-carboxylate;oxalic acid Chemical compound OC(=O)C(O)=O.CCC(=O)N([C@]1([C@H](CN(CCC=2C=CC=CC=2)CC1)C)C(=O)OC)C1=CC=CC=C1 CBKLICUQYUTWQL-XWGBWKJCSA-N 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 239000004530 micro-emulsion Substances 0.000 description 1
- 239000003094 microcapsule Substances 0.000 description 1
- 235000013336 milk Nutrition 0.000 description 1
- 239000008267 milk Substances 0.000 description 1
- 210000004080 milk Anatomy 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000003020 moisturizing effect Effects 0.000 description 1
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 1
- PDRAHDYJNDYBNK-UHFFFAOYSA-N n-[3-[hexadecanoyl(2-hydroxyethyl)amino]-2-hydroxypropyl]-n-(2-hydroxyethyl)hexadecanamide Chemical compound CCCCCCCCCCCCCCCC(=O)N(CCO)CC(O)CN(CCO)C(=O)CCCCCCCCCCCCCCC PDRAHDYJNDYBNK-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 238000007427 paired t-test Methods 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 230000035479 physiological effects, processes and functions Effects 0.000 description 1
- 230000019612 pigmentation Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 230000002633 protecting effect Effects 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 230000009993 protective function Effects 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000002207 retinal effect Effects 0.000 description 1
- NCYCYZXNIZJOKI-OVSJKPMPSA-N retinal group Chemical group C\C(=C/C=O)\C=C\C=C(\C=C\C1=C(CCCC1(C)C)C)/C NCYCYZXNIZJOKI-OVSJKPMPSA-N 0.000 description 1
- 229930002330 retinoic acid Natural products 0.000 description 1
- WWDMJSSVVPXVSV-YCNIQYBTSA-N retinyl ester Chemical compound CC1CCCC(C)(C)C1\C=C\C(\C)=C\C=C\C(\C)=C\C(O)=O WWDMJSSVVPXVSV-YCNIQYBTSA-N 0.000 description 1
- 208000008742 seborrheic dermatitis Diseases 0.000 description 1
- 239000003352 sequestering agent Substances 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 238000005549 size reduction Methods 0.000 description 1
- 230000037394 skin elasticity Effects 0.000 description 1
- 239000000344 soap Substances 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 229940083608 sodium hydroxide Drugs 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000013599 spices Nutrition 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 229940032094 squalane Drugs 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 210000004243 sweat Anatomy 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- 125000002640 tocopherol group Chemical group 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 229960001727 tretinoin Drugs 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- NCYCYZXNIZJOKI-UHFFFAOYSA-N vitamin A aldehyde Natural products O=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C NCYCYZXNIZJOKI-UHFFFAOYSA-N 0.000 description 1
- 239000000341 volatile oil Substances 0.000 description 1
- 235000019386 wax ester Nutrition 0.000 description 1
- 239000004563 wettable powder Substances 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- 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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/164—Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
-
- 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
- A61K31/07—Retinol compounds, e.g. vitamin A
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
- A61K31/203—Retinoic acids ; Salts thereof
-
- 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
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/41—Amines
-
- 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
- A61K8/67—Vitamins
- A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
-
- 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
- A61K8/68—Sphingolipids, e.g. ceramides, cerebrosides, gangliosides
-
- 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
- A61P17/08—Antiseborrheics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- A61Q19/06—Preparations for care of the skin for countering cellulitis
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Birds (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
Rは、C9−C21の飽和又は不飽和脂肪族鎖である)、
nは、1又は2であり;
R及びR’は、C9−C21の飽和又は不飽和脂肪族鎖である。)、
m及びnは、同一又は互いに異なって、1〜3の整数であり;
k及びlは、同一又は互いに異なって、1又は2であり;
jは、0又は1であり;
R及びR’は、同一又は互いに異なって、ヒドロキシ基を含有し又は含有しない、C1−C31の直鎖又は枝鎖の飽和又は不飽和アルキル基であり;
A1,A2及びA3は、同一又は互いに異なって、水素又は下記構造の置換基のいずれか一つであるが、A1,A2及びA3が同時に水素である場合は除く:
R及びR’は、同一又は互いに異なって、ヒドロキシ基を含有し又は含有しない、C10−C32の直鎖又は枝鎖の飽和又は不飽和アルキル基であり;
R3及びR4は、同一又は互いに異なって、水素又はC1−C4のアルキル基又はヒドロキシアルキル基であり;
R5は、−CH2CH2OA又は下記構造の置換基のいずれかである。
m及びnは、同一又は互いに異なって、1〜4の整数であり;
R及びR’は同一又は互いに異なって、ヒドロキシ基を含有し又は含有しない、C1−C31の直鎖又は枝鎖の飽和又は不飽和アルキル基であり;
A1及びA2は同一又は互いに異なって、水素又は下記構造の置換基のいずれかである。
m及びnは、同一又は互いに異なって、1〜3の整数であり;
k及びlは、同一又は互いに異なって、1又は2であり;
jは、0又は1であり;
A1,A2及びA3は、同一又は互いに異なって、水素又は下記構造の置換基のいずれかであり:
Rは、下記構造を有する置換基である:
前記のレチノイドを含有する組成物は、毛孔の過角質化を防ぎ、皮膚の皮脂をコントロールする効果があるが、毛孔でない部位においては、経皮伝達経路上、表皮層で刺激が生じ得るため、その濃度が多少高い場合、皮膚が赤くなったり、かゆみを伴うひりつきを感じたりする等の副作用が発生し得る。しかし、レチノイドを含有した組成物にセラミドをさらに含有させる場合、レチノイドによる皮膚刺激を緩和することができる。セラミドは、主に、毛孔ではなく、表皮の最外郭に存在する角質の細胞間脂質成分であるが、これは、皮膚角質層の障壁効果を増進させる機能を有する。したがって、セラミドをレチノイドとともに使用する場合、セラミドが形成される膜によりレチノイドが皮膚に直接接することが減少したり、レチノイドによる刺激があってもセラミドが皮膚障壁層を強化して皮膚の迅速な回復を図ったりするため、レチノイドによる皮膚刺激を緩和させるものと考えられる。また、セラミドの付加により、前記組成物は、皮膚水分を保持し、角質層を保護して、皮膚保湿及び皮膚改善効果が強化され得る。
また、前記の活性成分の投与量は、治療を受ける対象の年齢、性別、体重と、治療する特定の疾患又は病理状態、疾患又は病理状態の深刻度、投与経路、処方者の判断によって変わるであろう。こうした因子に基づく投与量の決定は、当業者の水準内にある。一般的な投与量は、0.001mg/kg/日〜2000mg/kg/日、より具体的には0.5mg/kg/日〜2.5mg/kg/日である。
下記の表1のような含量組成により実施例1,2及び実施例1を製造するが、まず、精製水に、グリセリン、水酸化ナトリウム及びヘキサミジン(及び/又はレチノール)を溶かし、別途アルコールにハイドロジェネイテッドキャスターオイルを溶かした後、2つのパートを高速で攪拌した。前記攪拌したものにカルボマーを添加し粘度を増加させて、可溶化ゲルを製造し、これを各々比較例1,2、実施例1とした。
健康な成人男女20人を対象に、前記比較例1,2、実施例1の可溶化ゲルを顔に塗布して、又は何も塗布せずに、塗布前、塗布2週後、及び塗布4週後の時点で、Facial Stage機器を使用して光学写真とUV写真を撮影した。このとき、被験者らは、洗顔をし、15分間、恒温恒湿条件で待機しながら皮膚状態を安定させた後、撮影した。
健康な成人男女20人を対象に、前記比較例1,2、実施例1の可溶化ゲルを顔に塗布して、又は何も塗布せずに、塗布前、塗布2週後、及び塗布4週後の時点で、スキンタッチ(Skin Touch)機器を使用して、UV写真を撮影した。このとき、被験者らは、洗顔をし、15分間、恒温恒湿状態で待機しながら皮膚状態を安定させた後、撮影した。
健康な成人男女20人を対象に、前記比較例1,2、実施例1の可溶化ゲルを顔に塗布して、又は何も塗布せずに、塗布前、塗布2週後、及び塗布4週後の時点で、スキンタッチ機器を使用して光学写真を撮影した。このとき、被験者は、洗顔をし、15分間、恒温恒湿状態で待機しながら皮膚状態を安定させた後撮影した。
48ウェルプレート(well plate)にメラン−a(melan−a)メラノサイト(Melanonocyte)(2.0×104)を入れ、温度37℃、10%CO2雰囲気で、一晩培養した。5日間、10%FBS含有RPMIに、刺激源としてアラキドン酸(Arachidonic acid)10μM、リノール酸(Linoleic acid)5μM、及びDHT10nMを処理した。その後5日間、10%FBSが含有されたRPMIに、陽性対照群としてヒドロキノン(hydroqunone)とアルブチン200ppmを、試験群として実施例1、比較例1及び2を処理すると同時に、刺激源のみを処理した陰性対照群と何も処理していない無処理群(control)もともに実験した。その後、1N NaOHでメラニンを溶かし、405nmでODを測定してローリー(lawry)法で定量した。下記式に従って陰性対照群のメラニン含有量と対比した各群のメラニン含有量を求め、図5に示した。
図5から見られるように、ヘキサミジン及びレチノールをともに含有する組成物の場合、ヘキサミジンやレチノールのみを含有する組成物に比べてメラニン含有量が低く示され、メラニン生成を抑制する効果が大きいことを確認することができた。また、これは、陽性対照群であるヒドロキノン1μM及びアルブチン200ppmよりも、その効果が優れていた。したがって、ヘキサミジン及びレチノールをともに含有する組成物は、メラニンが皮膚に沈着して生じる皮膚の色素沈着を予防、改善又は治療する効果に優れる。
以下の表2のような含有量組成により比較例3及び実施例2,3,4を製造するが、まず、精製水に、グリセリン、水酸化ナトリウム、ヘキサミジン及びレチノールを溶かし、別途アルコールにハイドロジェネイテッドキャスターオイル、セラミドを溶かし後、2つのパートを高速で攪拌した。前記攪拌したものにカルボマーを添加し粘度を増加させて、可溶化ゲルを製造し、それぞれ比較例3及び実施例2、3、4とした。
健康な成人男女20名(男10人、女10人)を対象に、ヘキサミジン及びレチノール10,000IUと類似セラミドの含量を異ならせた前記比較例3及び実施例2,3,4を、左腕の下側に、一週間、2μl/cm2ずつ塗布した後、日光に露出した状態に置いて、刺激程度を紅斑指数で測定した。次の一週間には塗布を中止して、紅斑指数を測定した。このとき、被験者は、腕の下側を石鹸で洗った後、15分間恒温恒湿状態で待機しながら皮膚状態を安定させた後、比較例3及び実施例2,3,4の刺激程度を紅斑指数により測定した。前記の結果は、図6にグラフで示した。
下記表3に記載の組成に従い、通常の方法で軟膏を製造した。
下記表4に記載の組成に従い、通常の方法で柔軟化粧水を製造した。
下記表5に記載の組成に従い、通常の方法で栄養クリームを製造した。
下記表6に記載の組成に従い、通常の方法でマッサージクリームを製造した。
下記表7に記載の組成に従い、通常の方法でパックを製造した。
Claims (5)
- ヘキサミジン、ヘキサミジンイセチオネート及びヘキサミジンジイセチオネートからなる群より選択された一つ以上;及び
レチノール、レチニルパルミテート及びレチニル酢酸からなる群より選択された1つ以上を含有するニキビ改善又は治療組成物。 - 前記ヘキサミジン、ヘキサミジンイセチオネート及びヘキサミジンジイセチオネートからなる群より選択された一つ以上を、組成物の総重量に基づき、0.0001重量%〜15重量%含む、請求項1に記載の組成物。
- 前記レチノール、レチニルパルミテート及びレチニル酢酸からなる群より選択された1つ以上を、組成物の総重量に基づき、0.0001重量%〜15重量%含む、請求項1または2に記載の組成物。
- 前記組成物は、セラミドを含む、請求項1〜3のいずれか一項に記載の組成物。
- 前記セラミドを、組成物の総重量に基づいて、0.001重量%〜10重量%含む、請求項4に記載の組成物。
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US9920357B2 (en) | 2012-06-06 | 2018-03-20 | The Procter & Gamble Company | Systems and methods for identifying cosmetic agents for hair/scalp care compositions |
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