WO2024011868A1 - 香兰基丁醚在制备治疗头屑和体癣产品中的应用 - Google Patents
香兰基丁醚在制备治疗头屑和体癣产品中的应用 Download PDFInfo
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- WO2024011868A1 WO2024011868A1 PCT/CN2022/142574 CN2022142574W WO2024011868A1 WO 2024011868 A1 WO2024011868 A1 WO 2024011868A1 CN 2022142574 W CN2022142574 W CN 2022142574W WO 2024011868 A1 WO2024011868 A1 WO 2024011868A1
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- WIPO (PCT)
- Prior art keywords
- butyl ether
- vanillyl butyl
- products
- preparation
- application
- Prior art date
Links
- VLDFMKOUUQYFGF-UHFFFAOYSA-N 4-(butoxymethyl)-2-methoxyphenol Chemical compound CCCCOCC1=CC=C(O)C(OC)=C1 VLDFMKOUUQYFGF-UHFFFAOYSA-N 0.000 title claims abstract description 66
- 229940078465 vanillyl butyl ether Drugs 0.000 title claims abstract description 65
- 208000001840 Dandruff Diseases 0.000 title claims abstract description 32
- 238000002360 preparation method Methods 0.000 title claims abstract description 19
- 206010005913 Body tinea Diseases 0.000 title claims abstract description 18
- 208000002474 Tinea Diseases 0.000 title claims abstract description 18
- 201000003875 tinea corporis Diseases 0.000 title claims abstract description 18
- 239000006071 cream Substances 0.000 claims abstract description 21
- 239000003814 drug Substances 0.000 claims abstract description 10
- 229940079593 drug Drugs 0.000 claims abstract description 7
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 18
- 241000233866 Fungi Species 0.000 claims description 11
- 241000223229 Trichophyton rubrum Species 0.000 claims description 7
- 239000003995 emulsifying agent Substances 0.000 claims description 6
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 claims description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 6
- 206010017533 Fungal infection Diseases 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 239000000126 substance Substances 0.000 claims description 4
- 241000222122 Candida albicans Species 0.000 claims description 3
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 3
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 3
- 229940095731 candida albicans Drugs 0.000 claims description 3
- 229940081733 cetearyl alcohol Drugs 0.000 claims description 3
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 3
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 claims description 3
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 3
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims description 3
- 229940032094 squalane Drugs 0.000 claims description 3
- VBIIFPGSPJYLRR-UHFFFAOYSA-M Stearyltrimethylammonium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCCC[N+](C)(C)C VBIIFPGSPJYLRR-UHFFFAOYSA-M 0.000 claims description 2
- 239000007921 spray Substances 0.000 claims description 2
- 239000000341 volatile oil Substances 0.000 claims description 2
- 208000031888 Mycoses Diseases 0.000 claims 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 3
- XMSXQFUHVRWGNA-UHFFFAOYSA-N Decamethylcyclopentasiloxane Chemical compound C[Si]1(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O1 XMSXQFUHVRWGNA-UHFFFAOYSA-N 0.000 claims 1
- 241000894007 species Species 0.000 claims 1
- XMAYWYJOQHXEEK-OZXSUGGESA-N (2R,4S)-ketoconazole Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2C=NC=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 XMAYWYJOQHXEEK-OZXSUGGESA-N 0.000 abstract description 14
- 229960004125 ketoconazole Drugs 0.000 abstract description 14
- 230000000694 effects Effects 0.000 abstract description 8
- 201000004647 tinea pedis Diseases 0.000 abstract description 6
- BYBLEWFAAKGYCD-UHFFFAOYSA-N Miconazole Chemical compound ClC1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 BYBLEWFAAKGYCD-UHFFFAOYSA-N 0.000 abstract 1
- 206010067197 Tinea manuum Diseases 0.000 abstract 1
- 206010040882 skin lesion Diseases 0.000 description 14
- 231100000444 skin lesion Toxicity 0.000 description 14
- 208000003251 Pruritus Diseases 0.000 description 13
- 230000007803 itching Effects 0.000 description 13
- 239000000243 solution Substances 0.000 description 8
- 208000024891 symptom Diseases 0.000 description 7
- 238000002474 experimental method Methods 0.000 description 6
- 230000000844 anti-bacterial effect Effects 0.000 description 5
- 239000002674 ointment Substances 0.000 description 5
- 229920001817 Agar Polymers 0.000 description 4
- 239000008272 agar Substances 0.000 description 4
- 230000001580 bacterial effect Effects 0.000 description 4
- 230000000052 comparative effect Effects 0.000 description 4
- 210000002683 foot Anatomy 0.000 description 4
- MCCACAIVAXEFAL-UHFFFAOYSA-N 1-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]imidazole;nitric acid Chemical compound O[N+]([O-])=O.ClC1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 MCCACAIVAXEFAL-UHFFFAOYSA-N 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 239000001963 growth medium Substances 0.000 description 3
- 229960005040 miconazole nitrate Drugs 0.000 description 3
- 238000000386 microscopy Methods 0.000 description 3
- 206010015150 Erythema Diseases 0.000 description 2
- 208000010201 Exanthema Diseases 0.000 description 2
- 241000555676 Malassezia Species 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 230000002354 daily effect Effects 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 231100000321 erythema Toxicity 0.000 description 2
- 201000005884 exanthem Diseases 0.000 description 2
- 230000002538 fungal effect Effects 0.000 description 2
- 210000004247 hand Anatomy 0.000 description 2
- 210000003128 head Anatomy 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 239000002609 medium Substances 0.000 description 2
- 206010037844 rash Diseases 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 210000000689 upper leg Anatomy 0.000 description 2
- 238000005406 washing Methods 0.000 description 2
- 239000000263 2,3-dihydroxypropyl (Z)-octadec-9-enoate Substances 0.000 description 1
- RZRNAYUHWVFMIP-GDCKJWNLSA-N 3-oleoyl-sn-glycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@H](O)CO RZRNAYUHWVFMIP-GDCKJWNLSA-N 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 206010020649 Hyperkeratosis Diseases 0.000 description 1
- 208000001126 Keratosis Diseases 0.000 description 1
- 241001480037 Microsporum Species 0.000 description 1
- 241000893976 Nannizzia gypsea Species 0.000 description 1
- 206010033733 Papule Diseases 0.000 description 1
- 206010037888 Rash pustular Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 229940124350 antibacterial drug Drugs 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 239000003429 antifungal agent Substances 0.000 description 1
- FLNKWZNWHZDGRT-UHFFFAOYSA-N azane;dihydrochloride Chemical compound [NH4+].[NH4+].[Cl-].[Cl-] FLNKWZNWHZDGRT-UHFFFAOYSA-N 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- -1 cyclopentamethicone Substances 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 description 1
- 229960001259 diclofenac Drugs 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 210000001339 epidermal cell Anatomy 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 208000024386 fungal infectious disease Diseases 0.000 description 1
- 229910052602 gypsum Inorganic materials 0.000 description 1
- 239000010440 gypsum Substances 0.000 description 1
- 230000003780 keratinization Effects 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- RZRNAYUHWVFMIP-UHFFFAOYSA-N monoelaidin Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-UHFFFAOYSA-N 0.000 description 1
- 230000001314 paroxysmal effect Effects 0.000 description 1
- RGCLLPNLLBQHPF-HJWRWDBZSA-N phosphamidon Chemical compound CCN(CC)C(=O)C(\Cl)=C(/C)OP(=O)(OC)OC RGCLLPNLLBQHPF-HJWRWDBZSA-N 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 238000002203 pretreatment Methods 0.000 description 1
- 208000029561 pustule Diseases 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 210000004761 scalp Anatomy 0.000 description 1
- 238000013077 scoring method Methods 0.000 description 1
- 230000035807 sensation Effects 0.000 description 1
- 230000037380 skin damage Effects 0.000 description 1
- 210000000434 stratum corneum Anatomy 0.000 description 1
- BWMISRWJRUSYEX-SZKNIZGXSA-N terbinafine hydrochloride Chemical compound Cl.C1=CC=C2C(CN(C\C=C\C#CC(C)(C)C)C)=CC=CC2=C1 BWMISRWJRUSYEX-SZKNIZGXSA-N 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 210000003371 toe Anatomy 0.000 description 1
- 229940126680 traditional chinese medicines Drugs 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
- A61K31/075—Ethers or acetals
-
- 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
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
- A61Q5/006—Antidandruff preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
- A61Q5/12—Preparations containing hair conditioners
Definitions
- the present invention relates to the field of medical technology, specifically the application of vanillyl butyl ether in the preparation of products for treating dandruff and tinea corporis.
- Dandruff is a product of the metabolism of epidermal cells on the human head. It is metabolized from the basal layer cells into the non-nucleated and lifeless stratum corneum. The dry dead cells appear in the form of scales or flakes and fall off automatically. This is commonly known as dandruff.
- the root cause of dandruff is the destruction of scalp flora balance, in which too high levels of bran Sporospora is a major cause.
- Ketoconazole is currently the most widely used antifungal agent Spore fungus, dandruff treatment drug. However, treatment is ineffective and it is easy to relapse.
- Superficial tissue mycosis of the human body is a tinea corporis characterized by itching, skin damage, and plaque after the head, hands, feet, thighs and other parts are infected by superficial fungi such as Trichophyton rubrum.
- the most widely used drug at present is: miconazole nitrate cream (Dacin). Miconazole nitrate cream treatment has slow onset of action and is prone to recurring attacks. Therefore, it is necessary to find more efficient antibacterial drugs to reduce the recurrence rate.
- the object of the present invention is to provide an application of vanillyl butyl ether in the preparation of products for treating dandruff and tinea corporis, so as to solve the problems raised in the above background technology.
- vanillyl butyl ether in the preparation of products for treating dandruff and tinea corporis.
- the mass concentration of vanillyl butyl ether is 0.1 to 5%.
- the mass concentration of vanillyl butyl ether is 0.1 to 0.5%.
- the mass concentration of vanillyl butyl ether is 0.5%.
- the products include medicines and daily chemical products.
- the medicine is ointment or spray.
- the daily chemical products are conditioners, creams or essential oils.
- vanillyl butyl ether The molecular formula of vanillyl butyl ether is C 12 H 18 O 3 , and its aliases are: vanillyl butyl ether, vanillyl butyl ether, 2-methoxy-4-(butoxymethyl)phenol. CAS is 82654 ⁇ 98 ⁇ 6.
- Vanillyl butyl ether has an obvious effect in treating dandruff at a concentration of 0.1%. Through in vitro antibacterial experiments, it was found that at a concentration of 0.1% to 5%, it has an effective effect on dandruff. There is a significant inhibitory effect on spores, more than 5% ketoconazole.
- conditioners and creams made of vanillyl butyl ether can effectively reduce dandruff and tinea pedis, and are more effective than ketoconazole and daxonine.
- a conditioner containing vanillyl butyl ether adopts a conventional hair conditioner formula: water, cetearyl alcohol, cyclopentamethicone, propylene glycol, stearyltrimethyl chloride Ammonium chloride, amodimethicone, hydroxyethyl cellulose, stearyltrimethylammonium chloride; after the conditioner is emulsified to form an emulsion, and the temperature drops to 50°C, divide it into three groups and add them separately. 0.1%, 0.5% and 5% vanillyl butyl ether, homogenize and set aside.
- a cream containing vanillyl butyl ether uses a conventional cream formula: water, squalane, propylene glycol, A165 emulsifier, M68 emulsifier; after the cream emulsifies to form an emulsion and the temperature drops to 50°C, Divide into three groups, add 0.1%, 0.5% and 5% vanillyl butyl ether respectively, homogenize and set aside.
- Dixon medium is used for Malassezia, and Tween 80, glyceryl monooleate and fatty acids are added
- broth medium is used for Candida albicans
- Sandcastle weak agar is used for Trichophyton rubrum and Microsporum gypseum. culture medium.
- Bacterial culture Take a 9cm diameter petri dish and add 20mL of molten culture solution containing 5% agar. Pick bacterial colonies, dissolve in sterile physiological saline, mix thoroughly, and adjust the turbidity of the bacterial suspension to 0.5 to 1.0OD, which is equivalent to 5 ⁇ 10 6 to 10 ⁇ 10 6 CFU/mL. Take 0.1 ml of bacterial suspension and spread it evenly on the surface of the experimental culture medium plate.
- Punch holes and add medicine Use a 7mm diameter hole punch to punch holes in the culture medium after coating, carefully remove the agar in the holes, and add 5% ketoconazole cream and 0.1% vanillyl butyl ether cream respectively. , 0.5% vanillyl butyl ether cream, 5% vanillyl butyl ether cream, make the ointment level with the edge of the hole, and ensure that the ointment is not added to the agar plane outside the hole.
- Scoring of rash and itching symptoms refer to the scoring standards in the "Guiding Principles for Clinical Research of New Traditional Chinese Medicines (Trial)" and adopt a 4-level scoring method. Degree of itching: none (0 points), no itching sensation; mild (1 point), occasional itching, no medication, does not affect work, study, and life; moderate (2 points), paroxysmal itching, sometimes mild and sometimes severe, affecting Medication is required for sleep, work, study, and life; severe (3 points), severe itching, seriously affecting sleep, work, study, and life.
- Skin lesions erythema, blisters, keratosis, chapped, desquamated, etc., scored as 3 points for severe, 2 points for moderate, 1 point for mild, and 0 points for none.
- the skin lesion score reduction index is 100%, all skin lesions and itching disappear, and microscopic examination of dandruff fungi is negative;
- Pre-treatment symptom score average onset time cure rate Relapse rate after 30 days Darkening treatment group 6.52 ⁇ 1.54 2.58 ⁇ 1.51 ⁇ 2.5 60% 33% vanillyl butyl ether 6.76 ⁇ 1.36 0.70 ⁇ 0.26 ⁇ 1.5 ⁇ 90% ⁇ 13% ⁇
- Cure criteria skin lesions or dandruff completely subside, and itching disappears; markedly effective: skin lesions or dandruff are reduced by more than 50%, and itching is significantly reduced; effective: skin lesions or dandruff are reduced by 20%-50%, and itching is relieved; ineffective: condition No changes.
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Birds (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
本发明公开了一种香兰基丁醚在制备治疗头屑和体癣产品中的应用，属于医药技术领域。本发明提供了香兰基丁醚在制备治疗头屑和体癣产品中的应用，所述香兰基丁醚的质量浓度为0.1～5％；本发明的香兰基丁醚制成的护发素和乳霜可以有效减轻头皮屑和手脚癣，效果超过酮康唑和达克宁，有效添加浓度在0.1～5％。
Description
本申请要求于2022年07月13日提交中国专利局、申请号为CN202210820293.2、发明名称为“香兰基丁醚在制备治疗头屑和体癣产品中的应用”的中国专利申请的优先权，其全部内容通过引用结合在本申请中。
本发明涉及医药技术领域，具体是香兰基丁醚在制备治疗头屑和体癣产品中的应用。
头皮屑是人体头部表皮细胞新陈代谢的产物，从基底层细胞代谢形成为无核、无生命的角质层，干燥的死亡细胞呈鳞状或薄片状而自动脱落，这俗称为头皮屑。头屑产生的根源是头皮生菌态平衡遭到破坏，其中过高的糠
孢子菌是一个主要原因。酮康唑是目前使用最广泛的抗糠
孢子菌，治疗头屑药物。但治疗效果不佳，而且极易复发。
人体浅部组织真菌病，是头部、手、脚、股等部位被红色毛癣菌等浅部真菌感染后，出现的以痒、皮肤破损、菌斑等特征的体癣。目前使用最广泛的药物是：硝酸咪康唑霜(达克宁)。硝酸咪康唑霜治疗存在起效时间慢，易反复发作等。因而需要寻找更高效的抑菌药，减少复发率。
发明内容
本发明的目的在于提供一种香兰基丁醚在制备治疗头屑和体癣产品中的应用，以解决上述背景技术中提出的问题。
为实现上述目的，本发明提供如下技术方案：
香兰基丁醚在制备治疗头屑和体癣产品中的应用，所述香兰基丁醚的质量浓度为0.1～5％。
作为本发明进一步的方案：所述香兰基丁醚的质量浓度为0.1～0.5％。
作为本发明进一步的方案：所述香兰基丁醚的质量浓度为0.5％。
作为本发明进一步的方案：所述产品包括药品和日化用品。
作为本发明进一步的方案：所述药品为膏体或喷雾。
作为本发明进一步的方案：所述日化用品为护发素、乳霜或精油。
香兰基丁醚分子式C
12H
18O
3，别名：香草醇丁醚、香兰基丁基醚、2～甲氧 基～4～(丁氧甲基)苯酚。CAS为82654～98～6。
与现有技术相比，本发明的有益效果是：
1、香兰基丁醚在0.1％浓度时，即有明显治疗头屑效果，通过体外抑菌实验发现，在0.1％～5％浓度时，对糠
孢子菌有明显的抑制效果，超过5％酮康唑。
2、香兰基丁醚在0.1％浓度时，即有明显治疗手、脚、股等部位体癣，通过体外抑菌实验发现，在0.1～5％浓度时，对红色毛癣菌、有明显的抑制效果，超过硝酸咪康唑霜(达克宁)。
3、通过人体实验，发现香兰基丁醚制成的护发素和乳霜可以有效减轻头皮屑和手脚癣，效果超过酮康唑和达克宁。
下面结合具体实施方式对本专利的技术方案作进一步详细地说明。
实施例1
一种含香兰基丁醚的护发素，护发素采用常规护发素配方：水、鲸蜡硬脂醇、环五聚二甲基硅氧烷、丙二醇、硬脂基三甲基氯化铵、氨端聚二甲基硅氧烷、羟乙基纤维素、硬脂基三甲基氯化铵；在护发素乳化形成乳液，温度降至50℃后，分三组，分别加入0.1％、0.5％和5％的香兰基丁醚，均质均匀备用。
实施例2
一种含香兰基丁醚的乳霜，乳霜采用常规乳霜配方：水、角鲨烷、丙二醇、A165乳化剂、M68乳化剂；在乳霜乳化形成乳液，温度降至50℃后，分三组，分别加入0.1％、0.5％和5％的香兰基丁醚，均质均匀备用。
对比例1
以现有的达克宁为对比例1。
对比例2
以现有的5％酮康唑为对比例2。
实验例1
对头皮屑、体癣相关真菌进行抑菌实验：
菌株活化：马拉色菌用Dixon培养基，并加入吐温80，甘油单油酸酯和脂肪酸，白念珠菌用肉汤培养基，红色毛癣菌、石膏样小孢子菌用沙堡弱琼脂培养基。
菌培养：取直径9cm培养皿，加入含5％琼脂的熔化培养液20mL。挑取菌落，溶于灭菌生理盐水，充分混合均匀，调节菌悬液浊度0.5～1.0OD，相当于5×10
6～10×10
6CFU/mL。吸取0.1ml菌悬液，均匀涂布于实验用培养基平板表面。
打孔加药：以直径7mm的打孔器在涂菌后的培养基上打孔，小心挑去孔内的琼脂，分别加入5％酮康唑乳膏、0.1％香兰基丁醚乳膏、0.5％香兰基丁醚乳膏、5％香兰基丁醚乳膏，使药膏与孔边缘相平，确保药膏没有加至孔外琼脂平面。
(4)培养：马拉色菌置32℃，其余菌株置28℃，培养7天。
(5)结果观察：观察各药膏孔周围抑菌圈并记录直径，每株菌同时做3个平板。
达克宁与香兰基丁醚对3种浅部真菌的抑菌圈(mm)比较(n＝9)结果如下表1。
表1达克宁与香兰基丁醚对3种浅部真菌的抑菌效果
| 浅部真菌 | 达克宁 | 0.1％香兰基丁醚 | 0.5％香兰基丁醚 | 5％香兰基丁醚 |
| 红色毛癣菌 | 15.3±2.56 | 17.56±1.80 ■ | 19.56±2.21 ■■ | 23.25±3.20 ■■ |
| 石膏样小孢子菌 | 12.4±2.24 | 13.42±1.41 ■ | 17.28±2.31 ■■ | 19.26±2.15 ■■ |
| 白念珠菌 | 18.7±3.15 | 20.52±1.35 ■ | 22.27±2.53 ■■ | 25.57±3.54 ■■ |
备注：
■与达克宁组相比，p<0.05；
■■与达克宁组相比，p<0.01。
酮康唑与香兰基丁醚对头皮屑相关真菌的抑菌圈(mm)比较(n＝9)结果如下表2。
表2酮康唑与香兰基丁醚对头皮屑相关真菌的抑菌效果
备注：
■与酮康唑组相比，p<0.05；
■■与达克宁组相比，p<0.01。
实验例2
治疗手脚癣人体实验：30名脚气患者，根据病程和症状严重程度，平均分为达克宁治疗组和香兰基丁醚治疗组，使两组患者病情相近。诊断参照《中国临床皮肤病学》中手足癣的诊断标准：发于手掌或足底，病情进展逐渐蔓延，皮疹主要表现为角化、干燥及鳞屑；红斑、丘疹、水疱、脓疱；指/趾间浸渍发白。
皮疹及瘙痒症状评分：参照《中药新药临床研究指导原则(试行)》中计分标准，采用4级评分法。瘙痒程度：无(0分)，无瘙痒感觉；轻(1分)，偶尔瘙痒，不用药，不影响工作、学习、生活；中(2分)，阵发性瘙痒，时轻时重，影响睡眠、工作、学习、生活，需用药；重(3分)，剧烈瘙痒，严重影响睡眠、工作、学习、生活。皮损情况：红斑、水疱、角化、皲裂、脱屑等，严重计3分，中度计2分，轻度计1分，无计0分。
分别给予达克宁霜和香兰基丁醚霜，每天在洗脚后抹药膏，1天2次，连续7天，观察起效时间、症状改善度、治愈度等指标。一个月后复诊观察复发率。
疗效评定标准：
痊愈：皮损积分下降指数为100％，皮损、瘙痒全部消失，皮屑真菌镜检阴性；
显效：皮损、瘙痒大部分消失，70％≤皮损积分下降指数<100％，皮损真菌镜检阴性；
有效：皮损、瘙痒部分消失，30％≤皮损积分下降指数<70％，皮损真菌镜检结果为阴性或阳性；
无效：与治疗前相比，各方面均无进步或病情继续加重，皮损积分下降指数<30％，皮损真菌镜检结果阳性。
两组治疗前后及治疗效果对比(n＝15)结果如下表3。
表3达克宁和香兰基丁醚的治疗效果
| 治疗前症状评分 | 治疗后症状评分 | 平均起效时间 | 治愈率 | 30天后复发率 | |
| 达克宁治疗组 | 6.52±1.54 | 2.58±1.51 ▲ | 2.5 | 60％ | 33％ |
| 香兰基丁醚 | 6.76±1.36 | 0.70±0.26 ▲■ | 1.5 ■ | 90％ ■ | 13％ ■ |
备注：
▲与治疗前相比，p＜0.01；
■与达克宁组相比，p＜0.01。
实验例3
治疗头皮屑人体实验：30头中重度皮屑患者，根据病程和症状严重程度，平均分为酮康唑治疗组和香兰基丁醚治疗组(每组15例)，两组患者病情相近。分别给予混有2％酮康唑洗剂、0.5％香兰基丁醚的护发素，洗净头发后，取适量护发素，涂抹在头发上，按摩3～5分钟以促进充分吸收，保留30分钟后再冲洗干净即可。连续7天，观察起效时间、症状改善度、治愈度等指标。
治愈标准：皮损或头屑完全消退，瘙痒消失；显效：皮损或头屑减少50％以上，瘙痒明显减轻；有效：皮损或头屑减少20％—50％，瘙痒减轻；无效：病情无变化。
两组治疗前后及治疗效果对比(n＝15)结果如下表4。
表4酮康唑和香兰基丁醚治疗效果
| 治愈 | 显效 | 有效 | 无效 | 30天后复发 | |
| 酮康唑治疗组 | 2 | 5 | 6 | 2 | 2 |
| 香兰基丁醚 | 8 ■ | 5 | 2 | 0 | 2 |
备注：
■与酮康唑组相比，p＜0.01。
对于本领域技术人员而言，显然本发明不限于上述示范性实施例的细节，而且在不背离本发明的精神或基本特征的情况下，能够以其他的具体形式实现本发明。因此，无论从哪一点来看，均应将实施例看作是示范性的，而且是非限制性的，本发明的范围由所附权利要求而不是上述说明限定，因此旨在将落在权利要求的等同要件的含义和范围内的所有变化囊括在本发明内。
此外，应当理解，虽然本说明书按照实施方式加以描述，但并非每个实施方式仅包含一个独立的技术方案，说明书的这种叙述方式仅仅是为清楚起见，本领域技术人员应当将说明书作为一个整体，各实施例中的技术方案也可以经适当组合，形成本领域技术人员可以理解的其他实施方式。
Claims (14)
- 香兰基丁醚在制备治疗头屑和体癣产品中的应用，其特征在于，所述香兰基丁醚的质量浓度为0.1～5％。
- 根据权利要求1所述的香兰基丁醚在制备治疗头屑和体癣产品中的应用，其特征在于，所述香兰基丁醚的质量浓度为0.1～0.5％。
- 根据权利要求1所述的香兰基丁醚在制备治疗头屑和体癣产品中的应用，其特征在于，所述香兰基丁醚的质量浓度为0.5％。
- 根据如权利要求1～3任一所述的香兰基丁醚在制备治疗头屑和体癣产品中的应用，其特征在于，所述产品包括药品和日化用品。
- 根据权利要求4所述的香兰基丁醚在制备治疗头屑和体癣产品中的应用，其特征在于，所述药品为膏体或喷雾。
- 根据权利要求4所述的香兰基丁醚在制备治疗头屑和体癣产品中的应用，其特征在于，所述日化用品为护发素、乳霜或精油。
- 根据权利要求6所述的香兰基丁醚在制备治疗头屑和体癣产品中的应用，其特征在于，所述护发素的配方为香兰基丁醚、水、鲸蜡硬脂醇、环五聚二甲基硅氧烷、丙二醇、硬脂基三甲基氯化铵、氨端聚二甲基硅氧烷、羟乙基纤维素和硬脂基三甲基氯化铵。
- 根据权利要求6所述的香兰基丁醚在制备治疗头屑和体癣产品中的应用，其特征在于，所述乳霜的配方为香兰基丁醚、水、角鲨烷、丙二醇、A165乳化剂和M68乳化剂。
- 一种护发素，其特征在于，所述护发素的配方为香兰基丁醚、水、鲸蜡硬脂醇、环五聚二甲基硅氧烷、丙二醇、硬脂基三甲基氯化铵、氨端聚二甲基硅氧烷、羟乙基纤维素和硬脂基三甲基氯化铵；所述香兰基丁醚在所述护发素中的含量为0.1％、0.5％或5％。
- 一种乳霜，其特征在于，所述乳霜的配方为香兰基丁醚、水、角鲨烷、丙二醇、A165乳化剂和M68乳化剂；所述香兰基丁醚在所述乳霜中的含量为0.1％、0.5％或5％。
- 香兰基丁醚在制备抑制浅部真菌感染的产品中的应用，其特征在于，所述香兰基丁醚的质量浓度为0.1～5％。
- 根据权利要求11所述的香兰基丁醚在制备治疗浅部真菌感染的产品中 的应用，其特征在于，所述香兰基丁醚的质量浓度为0.1～0.5％。
- 根据权利要求11所述的香兰基丁醚在制备治疗浅部真菌感染的产品中的应用，其特征在于，所述香兰基丁醚的质量浓度为0.5％。
- 根据权利要求11～13任一项所述的香兰基丁醚在制备治疗浅部真菌感染的产品中的应用，其特征在于，所述浅部真菌包括红色毛癣菌、红色毛癣菌、白念珠菌和糠孢子菌中的一种或多种。
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