WO2020047991A1 - 一种防螨添加剂在日化方面的应用 - Google Patents

一种防螨添加剂在日化方面的应用 Download PDF

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WO2020047991A1
WO2020047991A1 PCT/CN2018/114227 CN2018114227W WO2020047991A1 WO 2020047991 A1 WO2020047991 A1 WO 2020047991A1 CN 2018114227 W CN2018114227 W CN 2018114227W WO 2020047991 A1 WO2020047991 A1 WO 2020047991A1
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mite
diaryllactam
acarid
additive
chemical products
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PCT/CN2018/114227
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French (fr)
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范俊
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范俊
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Priority claimed from CN201811016701.9A external-priority patent/CN108675949A/zh
Priority claimed from CN201811016702.3A external-priority patent/CN108689902A/zh
Priority claimed from CN201811016666.0A external-priority patent/CN108685746A/zh
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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
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/14—Ectoparasiticides, e.g. scabicides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/02—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings containing insect repellants
    • 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
    • A61Q19/10—Washing or bathing preparations
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/10—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings

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  • the invention belongs to the field of daily chemistry, and relates to an application of an anti-mite additive in daily chemical.
  • Skin is one of the most important organs of the human body. It plays an important role in protecting various tissues and organs in the body and participating in various metabolic activities of the body. The health of the skin has a great impact on the health of the body. Since the skin is the outermost organ of the human body, the skin often bears the brunt when various external adverse factors come to the human body.
  • Human demodex mites are found all over the world and are widely parasitized in human hair follicles and sebaceous glands. They can flow in and out of pores unhindered, suck the cytoplasm of hair follicles and sebaceous glands as nutrients and survive, and they have a particularly strong ability to reproduce, and can reproduce in about 14 days.
  • the mite infection rate is as high as 68% to 97%, and the elderly can be infected from 48 days to 90 years of age, and the majority of infected people are asymptomatic carriers.
  • the harm it causes to the skin cannot be ignored, it not only damages the skin health, but also causes a series of facial skin diseases, which hinders beauty.
  • the purpose of the present invention is to provide an anti-mite additive for daily use.
  • R is:
  • diaryllactam compounds in the preparation of anti-mite daily chemicals.
  • R is:
  • diaryllactam compounds in the preparation of anti-mite daily chemicals.
  • R is:
  • diaryllactam compounds in the preparation of anti-mite daily chemicals.
  • the diaryllactam compound provided by the present invention has excellent anti-mite effect, and can be used as a shower gel or facial cleanser additive to make an anti-mite shower gel or anti-mite facial cleanser.
  • Fig. 1 shows the negative rate (%) of facial mites on days 6 and 11 of each group.
  • the structure of the diaryllactam compound to be tested is shown below. It is self-made and the purity is not less than 98%.
  • the matrix formula is as follows. After mixing the ingredients, it is stirred slowly at 55 ° C for 24 hours, and naturally cooled. The cooling process continues to stir.
  • diaryllactams 1 to 6 Adding 0.5% diaryllactams 1 to 6 to the above-mentioned bases, respectively, to obtain a facial cleanser containing diaryllactams 1 to 6.
  • the matrix formula is as follows. After mixing the ingredients, it is stirred slowly at 55 ° C for 24 hours, and then naturally cooled.
  • raw material name w /% raw material name w /% Lauryl ether ammonium sulfate (70%) 15 glycerin 2 Disodium lauryl sulfosuccinate 6 Carbomer 940 5 Cocoamide monoethanolamide 1.5 DP300 0.2 Coco fatty acid diethanolamide 2.5 EDTA disodium 0.1 Sodium lauroyl sarcosinate 5 Parabens 0.2 Pearl paste 3 essence 0.3 Propyl betaine 5 Deionized water Increase to 100
  • diaryllactams 1 to 6 Adding 0.5% diaryllactams 1 to 6 to the above-mentioned substrates, respectively, to obtain a shower gel containing diaryllactams 1-6.
  • Diaryllactam groups 1 to 6 Use the above-mentioned anti-mite cleansing milk containing diaryl lactams 1 to 6 to cleanse the face every morning and evening. Palm, drip a few drops of water on the palm until it foams, apply evenly on the face, and rub the face evenly for 5 minutes;
  • the control group cleansed the face with the matrix containing no diaryllactams 1 to 6 every morning and evening.
  • the method of cleansing was the same as above.
  • the inspection method is: use the squeeze method to test, first squeeze the fat on both sides of the nose, and then scrape the squeezed sebum with a knife Next, use a needle tip to remove a drop of sesame oil placed on a clean glass slide from the blade, stir it thoroughly until the sebum is completely diluted in the oil, and observe with a low-power microscope. If no mite is observed, it means that the mite is negative, as follows The formula calculates the negative rate (%) of each group.
  • Negative rate (%) number of negative people / total number of people ⁇ 100%
  • diaryllactams 1 to 5 have excellent anti-mite effects, and can be used as a shower gel or cleanser additive to make an anti-mite shower gel or anti-mite cleanser.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Dermatology (AREA)
  • Plant Pathology (AREA)
  • Pest Control & Pesticides (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Detergent Compositions (AREA)
  • Cosmetics (AREA)

Abstract

一种防螨添加剂在日化方面的应用。二芳基内酰胺类化合物具有优异的防螨效果，可以用作防螨沐浴露、防螨洗面奶和防螨日化方面的用途。

Description

一种防螨添加剂在日化方面的应用 技术领域
本发明属于日用化学领域，涉及一种防螨添加剂在日化方面的应用。
背景技术
皮肤是人体最重要的器官之一，它担负有保护全身各个组织器官及参与机体各种新陈代谢活动的重要功能，皮肤的健康状况对全身健康影响很大。由于皮肤是人体最外层的器官，在各种外界不利因素向人体袭来的时候，皮肤往往首当其冲。人体蠕形螨遍布于全世界，广泛寄生于人体的毛囊和皮脂腺内，分别称为毛囊蠕形螨和皮脂蠕形螨。它们能畅通无阻地进出毛孔，吸食毛囊和皮脂腺内的细胞质液作营养成分而生存，而且它们的繁殖能力特别强，14天左右就能繁殖一代。由于它体型细小，肉眼很难观察到。据国内外资料对90万人的调查报道，螨虫感染率高达68％～97％，从出生48天至90岁的老人都可感染，而且感染者绝大多数为无症状的带虫者。它对皮肤所造成的危害是不容忽视的，它不仅损害皮肤健康，而且还引发一系列的面部皮肤病，有碍美容。
因此，除螨日化产品具有广阔的市场。
发明内容
本发明的目的在于提供一种防螨添加剂在日化方面的应用。
本发明上述目的通过如下技术方案实现：
一种二芳基内酰胺类化合物，化学结构式如下：
Figure PCTCN2018114227-appb-000001
其中，R为：
Figure PCTCN2018114227-appb-000002
上述二芳基内酰胺类化合物在制备防螨沐浴露中的应用。
上述二芳基内酰胺类化合物在制备防螨洗面奶中的应用。
上述二芳基内酰胺类化合物在制备防螨日化方面中的应用。
一种二芳基内酰胺类化合物，化学结构式如下：
Figure PCTCN2018114227-appb-000003
其中，R为：
Figure PCTCN2018114227-appb-000004
上述二芳基内酰胺类化合物在制备防螨沐浴露中的应用。
上述二芳基内酰胺类化合物在制备防螨洗面奶中的应用。
上述二芳基内酰胺类化合物在制备防螨日化方面中的应用。
一种二芳基内酰胺类化合物，化学结构式如下：
Figure PCTCN2018114227-appb-000005
其中，R为：
Figure PCTCN2018114227-appb-000006
上述二芳基内酰胺类化合物在制备防螨沐浴露中的应用。
上述二芳基内酰胺类化合物在制备防螨洗面奶中的应用。
上述二芳基内酰胺类化合物在制备防螨日化方面中的应用。
有益效果：
本发明提供的二芳基内酰胺类化合物具有优异的防螨效果，可以用作沐浴露或洗面奶添加剂制成防螨沐浴露或防螨洗面奶。
附图说明
图1为各组第6、11天面部螨虫转阴率(％)。
具体实施方式
下面结合附图和实施例具体介绍本发明实质性内容，但并不以此限定本发明的保护范围。
一、实验材料
待测试的二芳基内酰胺类化合物的结构如下所示，自制，纯度不低于98％。
Figure PCTCN2018114227-appb-000007
二、实验方法
1、防螨洗面奶的配制
基质配方如下，将各成分混合后55℃缓慢搅拌24h，自然冷却，冷却过程继续搅拌。
原料名称 w/％ 原料名称 w/％
十六十八醇 3 丙二醇 6
硬脂酸单甘油酯 2 三乙醇胺 0.3
15#白矿油 8 月桂基醚硫酸钠(25％) 6
DC200二甲基硅油 3 对羟基苯甲酸酯 0.2
维生素E 0.5 香精 0.3
卡波姆940 0.3 去离子水 加至100
分别在上述基质中添加0.5％二芳基内酰胺1～6即得到含有二芳基内酰胺1～6的洗面奶。
2、防螨沐浴露的配制
基质配方如下，将各成分混合后55℃缓慢搅拌24h，自然冷却，冷却过程继续搅拌。
原料名称 w/％ 原料名称 w/％
月桂基醚硫酸铵(70％) 15 甘油 2
月桂醇磺基琥珀酸酯二钠 6 卡波姆940 5
椰油酰胺基单乙醇酰胺 1.5 DP300 0.2
椰油脂肪酸二乙醇酰胺 2.5 EDTA二钠 0.1
月桂酰肌氨酸钠 5 对羟基苯甲酸酯 0.2
珠光浆 3 香精 0.3
丙基甜菜碱 5 去离子水 加至100
分别在上述基质中添加0.5％二芳基内酰胺1～6即得到含有二芳基内酰胺1～6的沐浴露。
3、防螨洗面奶的防螨效果测试
为了验证防螨效果，选取70名证实面部有螨感染的受试者(螨虫阳性)，每组10人：
二芳基内酰胺1～6组：每天早晚分别使用上述含有二芳基内酰胺1～6的防螨洗面奶洁面一次，具体洁面方法为：每次挤压蚕豆粒大小的防螨洗面奶于掌心，滴几滴水于掌心揉至起泡沫，均匀涂抹于面部，并来回均匀揉搓面部5分钟；
对照组：每天早晚使用不含有二芳基内酰胺1～6的基质洁面一次，洁面方法同上。
分别于第6日、第11日清晨洁面前检查面部螨虫是否转阴性，检查方法为：用挤压法进行检验，先在鼻子两侧挤压取脂，再将挤压出的皮脂用刀刮下，用针尖从刀刃取下置于干净载物玻璃片上的一滴香油内，充分搅拌待皮脂完全稀释在油内，用低倍镜进行观察，未观察到螨虫则说明转为螨虫阴性，按如下公式计算各组转阴率(％)。
转阴率(％)＝转阴人数/总人数×100％
三、实验结果
实验结果如表1和图1所示，二芳基内酰胺1～5组第6天转阴率显著高于对照组，第11天已完全转阴；而二芳基内酰胺6组第6、11天转阴率与对照组无显著差异。
表1各组第6、11天面部螨虫转阴率(％)
组别 第6天转阴率(％) 第11天转阴率(％)
对照组 10 20
二芳基内酰胺1 70 100
二芳基内酰胺2 60 100
二芳基内酰胺3 70 100
二芳基内酰胺4 70 100
二芳基内酰胺5 60 100
二芳基内酰胺6 10 20
上述结果说明，二芳基内酰胺1～5具有优异的防螨效果，可以用作沐浴露或洗面奶添加剂制成防螨沐浴露或防螨洗面奶。
上述实施例的作用在于具体介绍本发明的实质性内容，但本领域技术人员应当知道，不应将本发明的保护范围局限于该具体实施例。

Claims (4)

  1. 一种二芳基内酰胺类化合物，其特征在于，化学结构式如下：
    Figure PCTCN2018114227-appb-100001
    其中，R为：
    Figure PCTCN2018114227-appb-100002
    或
    Figure PCTCN2018114227-appb-100003
    其中，R为：
    Figure PCTCN2018114227-appb-100004
    或
    Figure PCTCN2018114227-appb-100005
    其中，R为：
    Figure PCTCN2018114227-appb-100006
  2. 权利要求1所述的二芳基内酰胺类化合物在制备防螨沐浴露中的应用。
  3. 权利要求1所述的二芳基内酰胺类化合物在制备防螨洗面奶中的应用。
  4. 权利要求1所述的二芳基内酰胺类化合物在制备防螨日化方面中的应用。
PCT/CN2018/114227 2018-09-03 2018-11-06 一种防螨添加剂在日化方面的应用 WO2020047991A1 (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
CN201811016666.0 2018-09-03
CN201811016701.9 2018-09-03
CN201811016702.3 2018-09-03
CN201811016701.9A CN108675949A (zh) 2018-09-03 2018-09-03 一种防螨化合物及用作沐浴露或洗面奶添加剂的用途
CN201811016702.3A CN108689902A (zh) 2018-09-03 2018-09-03 一种添加剂及在沐浴露或洗面奶等日化产品中的应用
CN201811016666.0A CN108685746A (zh) 2018-09-03 2018-09-03 一种防螨沐浴露或洗面奶添加剂

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103006465A (zh) * 2012-12-04 2013-04-03 青岛美今生物科技有限公司 一种动物用除虱驱螨制剂
CN107235883A (zh) * 2016-03-29 2017-10-10 复旦大学 二芳基‑β‑内酰胺类化合物及其制备方法和在制药中的用途
CN108675949A (zh) * 2018-09-03 2018-10-19 范俊 一种防螨化合物及用作沐浴露或洗面奶添加剂的用途
CN108689902A (zh) * 2018-09-03 2018-10-23 范俊 一种添加剂及在沐浴露或洗面奶等日化产品中的应用
CN108685746A (zh) * 2018-09-03 2018-10-23 范俊 一种防螨沐浴露或洗面奶添加剂

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103006465A (zh) * 2012-12-04 2013-04-03 青岛美今生物科技有限公司 一种动物用除虱驱螨制剂
CN107235883A (zh) * 2016-03-29 2017-10-10 复旦大学 二芳基‑β‑内酰胺类化合物及其制备方法和在制药中的用途
CN108675949A (zh) * 2018-09-03 2018-10-19 范俊 一种防螨化合物及用作沐浴露或洗面奶添加剂的用途
CN108689902A (zh) * 2018-09-03 2018-10-23 范俊 一种添加剂及在沐浴露或洗面奶等日化产品中的应用
CN108685746A (zh) * 2018-09-03 2018-10-23 范俊 一种防螨沐浴露或洗面奶添加剂

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