CN115006374A - Application of vanillyl butyl ether in preparation of product for treating dandruff and tinea corporis - Google Patents

Application of vanillyl butyl ether in preparation of product for treating dandruff and tinea corporis Download PDF

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Publication number
CN115006374A
CN115006374A CN202210820293.2A CN202210820293A CN115006374A CN 115006374 A CN115006374 A CN 115006374A CN 202210820293 A CN202210820293 A CN 202210820293A CN 115006374 A CN115006374 A CN 115006374A
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China
Prior art keywords
butyl ether
vanillyl butyl
product
dandruff
tinea corporis
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CN202210820293.2A
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Chinese (zh)
Inventor
王剑
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Guangzhou Wenhan Biotechnology Co ltd
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Guangzhou Wenhan Biotechnology Co ltd
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Priority to CN202210820293.2A priority Critical patent/CN115006374A/en
Publication of CN115006374A publication Critical patent/CN115006374A/en
Priority to PCT/CN2022/142574 priority patent/WO2024011868A1/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/075Ethers or acetals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/347Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • A61Q5/006Antidandruff preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • A61Q5/12Preparations containing hair conditioners

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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

The invention discloses an application of vanillyl butyl ether in preparing a product for treating dandruff and tinea corporis, belonging to the technical field of medicines; the application of vanillyl butyl ether in preparing a product for treating dandruff and tinea corporis, wherein the mass concentration of the vanillyl butyl ether is 0.1-5%; the hair conditioner and cream prepared from vanillyl butyl ether can effectively relieve dandruff and tinea manus and pedis, the effect is better than that of ketoconazole and dacron, and the effective addition concentration is 0.1-5%.

Description

Application of vanillyl butyl ether in preparation of product for treating dandruff and tinea corporis
Technical Field
The invention relates to the technical field of medicines, in particular to application of vanillyl butyl ether in preparation of a product for treating dandruff and tinea corporis.
Background
Dandruff is a product of metabolism of epidermal cells of the human head, is metabolized from basal layer cells to form an anucleated and inanimate horny layer, and dry dead cells are automatically shed in a scaly or flaky shape, which is commonly called dandruff. The root of dandruff production is the disruption of scalp ecological balance, with the excess bran sporozoite being a major cause. Ketoconazole is currently the most widely used anti-bran sporozoite drug for dandruff treatment. But the treatment effect is not good and the disease is easy to recur.
The superficial mycosis of human body is tinea corporis characterized by itching, skin damage, bacterial plaque and the like after the head, hands, feet, thighs and other parts are infected by superficial fungi such as trichophyton rubrum and the like. The most widely used drugs at present are: miconazole nitrate cream (dacron). The miconazole nitrate cream has the characteristics of slow response time, easy relapse and the like in treatment. Therefore, more effective bacteriostat is needed to be found, and the recurrence rate is reduced.
Disclosure of Invention
The invention aims to provide application of vanillyl butyl ether in preparing a product for treating dandruff and tinea corporis, so as to solve the problems in the background technology.
In order to achieve the purpose, the invention provides the following technical scheme:
the application of the vanillyl butyl ether in preparing products for treating dandruff and tinea corporis is that the mass concentration of the vanillyl butyl ether is 0.1-5%.
As a further scheme of the invention: the mass concentration of the vanillyl butyl ether is 0.1-0.5%.
As a further scheme of the invention: the mass concentration of the vanillyl butyl ether is 0.5%.
As a further scheme of the invention: the products include pharmaceuticals and daily chemicals.
As a further scheme of the invention: the medicine is ointment or spray.
As a further scheme of the invention: the daily chemical product is hair conditioner, cream or essential oil.
Vanillyl butyl ether molecular formula C 12 H 18 O 3 And alias: vanillyl butyl ether, 2-methoxy-4- (butoxymethyl) phenol. CAS is 82654-98-6.
Compared with the prior art, the invention has the beneficial effects that:
1. the vanillyl butyl ether has obvious effect of treating dandruff when the concentration is 0.1 percent, and the in vitro bacteriostasis experiment shows that the vanillyl butyl ether has obvious effect of inhibiting bran spore bacteria when the concentration is 0.1 to 5 percent, and the content is more than 5 percent of ketoconazole.
2. The vanillyl butyl ether has obvious effect of treating tinea corporis of hands, feet, thighs and other parts at the concentration of 0.1 percent, and has obvious inhibition effect on trichophyton rubrum at the concentration of 0.1 to 5 percent through in-vitro bacteriostasis experiments, which is more than miconazole nitrate cream (dacron).
3. Human body experiments show that the hair conditioner and the cream prepared from vanillyl butyl ether can effectively relieve dandruff and tinea manus and pedis, and the effect is better than that of ketoconazole and dacron.
Detailed Description
The technical solution of the present patent will be described in further detail with reference to the following embodiments.
Example 1
A hair conditioner containing vanillyl butyl ether adopts a conventional hair conditioner formula: water, cetostearyl alcohol, cyclopentadimethyl siloxane, propylene glycol, stearyl trimethyl ammonium chloride, amodimethicone, hydroxyethyl cellulose, stearyl trimethyl ammonium chloride; emulsifying in hair conditioner to form emulsion, cooling to 50 deg.C, dividing into three groups, adding 0.1%, 0.5% and 5% vanillyl butyl ether, homogenizing, and keeping.
Example 2
A cream containing vanillyl butyl ether adopts a conventional cream formula: water, squalane, propylene glycol, an A165 emulsifier, and an M68 emulsifier; emulsifying in cream to form emulsion, cooling to 50 deg.C, dividing into three groups, respectively adding vanillyl butyl ether 0.1%, 0.5% and 5%, and homogenizing.
Comparative example 1
The existing dacron is used as comparative example 1.
Comparative example 2
The existing 5% ketoconazole was used as comparative example 2.
Experimental example 1
Antibacterial experiments are carried out on dandruff and tinea corporis related fungi:
strain activation: the Malassezia furfur is cultured in Dixon medium, and added with Tween 80, glycerol monooleate and fatty acid, culture broth for Candida albicans, and culture broth for Trichophyton rubrum and Microsporum gypseum in Sabourne agar.
And (3) culturing bacteria: a9 cm-diameter petri dish was charged with 20mL of a molten culture solution containing 5% agar. Selecting colony, dissolving in sterilized normal saline, mixing well, adjusting turbidity of bacterial suspension to 0.5-1.0OD (equivalent to 5 × 10) 6 -10×10 6 CFU/mL. 0.1ml of the bacterial suspension is sucked up and evenly spread on the surface of a culture medium plate for experiments.
Punching with a puncher with diameter of 7mm, carefully removing agar in the hole, and respectively adding 5% ketoconazole cream, 0.1% vanillyl butyl ether cream, 0.5% vanillyl butyl ether cream and 5% vanillyl butyl ether cream to 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.
(4) Culturing: culturing Malassezia at 32 deg.C and the rest strains at 28 deg.C for 7 days.
(5) And (4) observing results: observing the inhibition zone around each ointment hole and recording the diameter, and simultaneously making 3 flat plates for each strain.
The results of the inhibition zones (mm) of dacron and vanillyl butyl ether against 3 superficial fungi (n = 9) are as follows:
superficial fungi Daktarin 0.1% vanillyl butyl ether 0.5% vanillyl butyl ether 5% vanillyl butyl ether
Trichophyton rubrum 15.3±2.56 17.56±1.80 19.56±2.21 ■■ 23.25±3.20 ■■
Microsporidian gypseum 12.4±2.24 13.42±1.41 17.28±2.31 ■■ 19.26±2.15 ■■
Candida albicans 18.7±3.15 20.52±1.35 22.27±2.53 ■■ 25.57±3.54 ■■
Remarking: in comparison with the Daktarin group, p<0.05; ■■ In comparison with the Daktarin group, p<0.01。
The results of ketoconazole versus zone of inhibition (mm) of the dandruff-associated fungus with vanillyl butyl ether (n = 9) are as follows:
5% Ketoconazole 0.1% vanillyl butyl ether 0.5% vanillyl butyl ether 5% vanillyl butyl ether
Bran spore bacteria 15.36±3.20 17.28±2.50 20.17±2.58 ■■ 25.35±3.16 ■■
Remarking: in comparison with the ketoconazole group, p<0.05; ■■ In comparison with the Daktarin group, p<0.01。
Experimental example 2
Human body experiment for treating tinea manuum and tinea pedis: 30 patients with beriberi are averagely divided into a Daktarin treatment group and a vanillylbutyl ether treatment group according to the disease course and the severity of symptoms, so that the disease conditions of the two groups of patients are similar. The diagnosis refers to the diagnosis standard of tinea manuum and tinea pedis in Chinese clinical dermatology: the disease condition is gradually spread when it is applied to the palms or soles, and the rash is mainly manifested as keratosis, dryness and scales; erythema, papules, blisters, pustules; the finger/toe is soaked and whitened.
Rash and itching symptom score: referring to scoring standard in the guidelines (trial) of clinical research on new Chinese medicines, a 4-grade scoring method is adopted. Degree of itching: no (0 point), no itching feeling; light (1 point), occasional pruritus and no medication, and does not influence work, study and life; in the middle (2 minutes), paroxysmal pruritus, mild and severe, affects sleep, work, study and life and needs to be taken; severe (3 points), severe itching, which seriously affects sleep, work, study, and life. Skin damage condition: erythema, blisters, keratosis, chapping, desquamation, etc., with a severity of 3 points, a medium of 2 points, a mild of 1 point, and no 0 point.
Applying Dakening cream and vanillyl butyl ether cream respectively, applying the ointment after washing feet every day for 1 day and 2 times, continuously for 7 days, and observing the indexes of onset time, symptom improvement degree, cure degree and the like. The recurrence rate is observed after one month of double diagnosis.
The treatment effect evaluation standard is as follows:
and (3) healing: the integral reduction index of the skin damage is 100 percent, the skin damage and the pruritus are completely disappeared, and the microscopic examination of the dandruff fungus is negative;
the effect is shown: most of the skin damage and pruritus disappear, the integral reduction index of the skin damage is more than or equal to 70 percent and less than 100 percent, and the microscopic examination of the fungus on the skin damage is negative;
the method has the following advantages: the skin damage and the pruritus are eliminated, the integral reduction index of the skin damage is more than or equal to 30 percent and less than 70 percent, and the microscopic examination result of the skin damage fungus is negative or positive;
and (4) invalidation: compared with the prior treatment, the method has no progress in all aspects or the disease condition is continuously aggravated, the skin damage integral reduction index is less than 30 percent, and the microscopic examination result of the skin damage fungi is positive.
Results of both groups before and after treatment and comparison of treatment effect (n = 15) were as follows:
symptom scoring before treatment Symptom scoring after treatment Mean onset of action The cure rate Recurrence rate after 30 days
Daktarin 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%
Remarking: p is less than 0.01 compared to before treatment; compared with the Daktarin group, p is less than 0.01.
Experimental example 3
Human experiments for treatment of dandruff: 30 patients with moderate or severe dandruff are averagely divided into a ketoconazole treatment group and a vanillylbutyl ether treatment group (15 cases in each group) according to the disease course and the symptom severity, and the disease conditions of the two groups of patients are similar. Respectively adding hair conditioner mixed with 2% ketoconazole lotion and 0.5% vanillyl butyl ether, cleaning hair, taking a proper amount of hair conditioner, smearing the hair conditioner on the hair, massaging for 3-5 minutes to promote full absorption, keeping for 30 minutes, and then washing to be clean. Continuously observing the indexes such as onset time, symptom improvement degree, cure degree and the like for 7 days.
The standard of cure is as follows: the skin lesions or dandruff are completely removed, and the pruritus disappears; the effect is shown: the skin damage or the scurf is reduced by more than 50 percent, and the pruritus is obviously relieved; the method has the following advantages: the skin damage or the dandruff is reduced by 20 to 50 percent, and the pruritus is relieved; and (4) invalidation: the disease condition was unchanged.
Results of both groups before and after treatment and comparison of treatment effect (n = 15) were as follows:
cure of disease Show effect Is effective Invalidation Relapse after 30 days
Ketoconazole treatment groups 2 5 6 2 2
Vanillyl butyl ether 8 5 2 0 2
Remarking: compared with the ketoconazole group, p is less than 0.01.
It will be evident to those skilled in the art that the invention is not limited to the details of the foregoing illustrative embodiments, and that the present invention may be embodied in other specific forms without departing from the spirit or essential attributes thereof. The present embodiments are therefore to be considered in all respects as illustrative and not restrictive, the scope of the invention being indicated by the appended claims rather than by the foregoing description, and all changes which come within the meaning and range of equivalency of the claims are therefore intended to be embraced therein.
Furthermore, it should be understood that although the present description refers to embodiments, not every embodiment may contain only a single embodiment, and such description is for clarity only, and those skilled in the art should integrate the description, and the embodiments may be combined as appropriate to form other embodiments understood by those skilled in the art.

Claims (6)

1. The application of the vanillyl butyl ether in preparing products for treating dandruff and tinea corporis is characterized in that the mass concentration of the vanillyl butyl ether is 0.1-5%.
2. Use of vanillyl butyl ether in the manufacture of a product for the treatment of dandruff and tinea corporis according to claim 1, wherein the mass concentration of vanillyl butyl ether is 0.1 to 0.5%.
3. Use of vanillyl butyl ether in the manufacture of a product for the treatment of dandruff and tinea corporis according to claim 1, wherein the mass concentration of vanillyl butyl ether is 0.5%.
4. Use of vanillyl butyl ether according to any one of claims 1 to 3 in the manufacture of a product for the treatment of dandruff and tinea corporis, wherein said product comprises pharmaceutical products and daily use chemicals.
5. Use of vanillyl butyl ether in the manufacture of a product for the treatment of dandruff and tinea corporis according to claim 4, wherein the product is a paste or a spray.
6. Use of vanillyl butyl ether according to claim 4 in the manufacture of a product for the treatment of dandruff and tinea corporis, wherein the daily chemical product is a hair conditioner, cream or essential oil.
CN202210820293.2A 2022-07-13 2022-07-13 Application of vanillyl butyl ether in preparation of product for treating dandruff and tinea corporis Pending CN115006374A (en)

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CN202210820293.2A CN115006374A (en) 2022-07-13 2022-07-13 Application of vanillyl butyl ether in preparation of product for treating dandruff and tinea corporis
PCT/CN2022/142574 WO2024011868A1 (en) 2022-07-13 2022-12-28 Use of vanillyl butyl ether in preparation of products for treating dandruff and tinea corporis

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Cited By (1)

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WO2024011868A1 (en) * 2022-07-13 2024-01-18 广州文翰生物科技有限公司 Use of vanillyl butyl ether in preparation of products for treating dandruff and tinea corporis

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Application publication date: 20220906