CN113476336B - Acne-removing composition and preparation method and application thereof - Google Patents

Acne-removing composition and preparation method and application thereof Download PDF

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CN113476336B
CN113476336B CN202110759861.8A CN202110759861A CN113476336B CN 113476336 B CN113476336 B CN 113476336B CN 202110759861 A CN202110759861 A CN 202110759861A CN 113476336 B CN113476336 B CN 113476336B
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acne
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removing composition
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CN113476336A (en
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成秋桂
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Guangzhou Meier Biotechnology Co ltd
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    • 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
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • A61K8/738Cyclodextrins
    • 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
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/27Zinc; Compounds thereof
    • 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
    • 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
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362Polycarboxylic acids
    • 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
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/368Carboxylic acids; Salts or anhydrides thereof with carboxyl groups directly bound to carbon atoms of aromatic rings
    • 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
    • A61K8/46Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
    • A61K8/466Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur containing sulfonic acid derivatives; Salts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier 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
    • A61Q17/005Antimicrobial preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/008Preparations for oily skin
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)

Abstract

The invention discloses an acne-removing composition and a preparation method and application thereof, and relates to the technical field of cosmetics. The invention provides an acne-removing composition, which comprises an aqueous phase; the water phase comprises the following components in parts by weight: 4-10 parts of cyclodextrin, 0.1-8 parts of salicylic acid, 0.1-10 parts of azelaic acid, 0.01-0.5 part of bactericide, 50-70 parts of solubilizer and 1-5 parts of pH regulator. The acne removing composition provided by the invention is completely free of grease, so that the problem of acne caused by grease is avoided; the acne-removing composition provided by the invention has good bactericidal power, and the high-efficiency bactericide is added to effectively kill propionibacterium acnes.

Description

Acne-removing composition and preparation method and application thereof
Technical Field
The invention relates to the technical field of cosmetics, in particular to an acne-removing composition and a preparation method and application thereof.
Background
The pathogenesis of acne is mainly related to the following four factors: hyperseborrhoea, hyperkeratosis at the opening of the pilosebaceous canal, proliferation of propionibacterium acnes, and inflammatory reactions. In the common acne-removing formulations on the market, only cream has good effect, and various active ingredients can be introduced. But the raw materials used in the essence and the gel are limited, and the effect is not ideal. At the same time, however, acne cream is introduced with grease, so that the final efficacy is weakened (acne is usually caused by vigorous sebum secretion).
Disclosure of Invention
Based on the above, the invention aims to overcome the defects of the prior art and provide the acne-removing composition and the preparation method and application thereof.
In order to achieve the purpose, the technical scheme adopted by the invention is as follows: an acne-removing composition comprising an aqueous phase; the water phase comprises the following components in parts by weight: 4-10 parts of cyclodextrin, 0.1-8 parts of salicylic acid, 0.1-10 parts of azelaic acid, 0.01-0.5 part of bactericide, 50-70 parts of solubilizer and 1-5 parts of pH regulator.
The invention provides an acne-removing composition, which is prepared by clathrating salicylic acid with cyclodextrin due to poor water solubility of salicylic acid, so that the problem of poor water solubility of salicylic acid is solved, the high addition amount of salicylic acid in an aqueous agent is realized, and cutin exfoliation is facilitated. The acne-removing composition provided by the invention is mild in effect, is acidic and relatively irritant after salicylic acid is generally added, and has a pH close to neutral after inclusion, so that irritation to skin is reduced. Azelaic acid strongly controls oil, and pigmentation is obviously reduced, azelaic acid is difficult to be added into cream, and demulsification is easy to happen when the content of azelaic acid is too high.
Preferably, the aqueous phase comprises the following components in parts by weight: 5 parts of cyclodextrin, 5 parts of salicylic acid, 8 parts of azelaic acid, 0.2 part of bactericide, 69 parts of solubilizer and 3 parts of pH regulator. The inventor of the application discovers through a great amount of experiments that the acne removing composition prepared by selecting the components and the parts by weight in the water phase has a better effect.
Preferably, the bactericide is hexamidine bis (isethionate); the solubilizer is at least one of ethanol, propylene glycol, ethoxy diethylene glycol and hydrogenated castor oil; the pH regulator is sodium hydroxide.
Preferably, the acne removing composition further comprises a powder phase and water, wherein the powder phase comprises the following components in parts by weight: 40-60 parts of zinc azelaic acid and 40-60 parts of zinc salicylate. The inventor of the application discovers through a large number of experiments that the acne removing composition prepared by the zinc azelate and the zinc salicylate in the weight parts has a better effect.
Preferably, the powder phase comprises the following components in parts by weight: 50 parts of zinc azelaic acid and 50 parts of zinc salicylate. Through a large number of experiments, the inventor of the application discovers that the effect of the acne-removing composition prepared from the zinc azelate and the zinc salicylate in the specific weight part is optimal.
Preferably, the water phase, the powder phase and the water are as follows by mass percent: water phase: powder phase: water = 20-50. The inventor of the application discovers through a great amount of experiments that when the acne removing composition adopts a brand-new formulation, the water phase, the powder phase and the water are selected according to the mass percentage, the obtained acne removing composition has a better effect.
Preferably, the water phase, the powder phase and the water are as follows by mass percent: water phase: powder phase: water = 25-45. Preferably, the mass percentages of the water phase, the powder phase and the water are as follows: water phase: powder phase: water =42: 25:33. the inventor of the application discovers through a great amount of experiments that when the acne-removing composition adopts a brand-new formulation, the water phase, the powder phase and the water are selected according to the mass percentage, the obtained acne-removing composition has the best effect.
In addition, the application provides a preparation method of the aqueous phase and powder combined acne removing composition, which comprises the following steps:
(1) Mixing salicylic acid, cyclodextrin and water, and heating to dissolve to obtain a mixture A; mixing and dissolving azelaic acid, solubilizer and bactericide to obtain a mixture B;
(2) Mixing the mixture A, the mixture B and water obtained in the step (1), adjusting the pH value to 5-7, and cooling to obtain a water phase;
(3) And (3) mixing and uniformly dispersing zinc salicylate, zinc azelate and water, and mixing with the water obtained in the step (2) to obtain the acne-removing composition.
Further, the application provides application of the acne-removing composition in cosmetics.
Compared with the prior art, the invention has the beneficial effects that: acne is related to hypersecretion of sebum, the final efficacy of cream is weakened due to the addition of grease, the preparation is completely free of grease, and the problem of acne caused by grease is avoided; the acne-removing composition provided by the invention has good bactericidal power, and the high-efficiency bactericide is added to effectively kill propionibacterium acnes; the addition of powdered zinc salicylate and zinc azelate helps to reduce inflammation and sebum secretion, thereby alleviating the problem of acne.
Detailed Description
To better illustrate the objects, aspects and advantages of the present invention, the present invention will be further described with reference to specific examples.
In the examples, the experimental methods used were all conventional methods unless otherwise specified, and the materials, reagents and the like used were commercially available without otherwise specified.
The invention is provided with the following examples and comparative examples, the specific components and parts by weight are selected as shown in table 1, in the examples of the invention, the total parts by weight of the water phase is 100 parts, and the total parts by weight of the powder phase is 100 parts:
TABLE 1 selection of Components and parts by weight of examples 1-5
Figure SMS_1
TABLE 2 selection of Components and parts by weight for examples 6-7 and comparative examples 1-2
Figure SMS_2
TABLE 3 selection of Components and parts by weight for examples 8-10 and comparative example 3
Figure SMS_3
The preparation method of the acne-removing composition disclosed by the embodiment 1-2 of the invention comprises the following steps:
(1) Mixing salicylic acid, cyclodextrin and water, and heating to dissolve to obtain a mixture A; mixing azelaic acid, ethanol and hexamidine di (isethionic acid) salt for dissolution to obtain a mixture B;
(2) Mixing the mixture A, the mixture B and water obtained in the step (1), adjusting the pH value to 6, and cooling to obtain the aqueous acne-removing composition.
The preparation method of the acne-removing composition disclosed by the embodiments 3-10 and the comparative examples 1-3 comprises the following steps:
(1) Mixing salicylic acid, cyclodextrin and water, and heating to dissolve to obtain a mixture A; mixing and dissolving azelaic acid, ethanol and hexamidine di (isethionic acid) salt to obtain a mixture B;
(2) Mixing the mixture A, the mixture B and water obtained in the step (1), adjusting the pH value to 6, and cooling to obtain a water phase;
(3) And (3) mixing and uniformly dispersing zinc salicylate, zinc azelate and water, and mixing with the water obtained in the step (2) to obtain the acne-removing composition.
Test example 1 acne removal and oil control effect test
The test process comprises the following steps: subject: selecting 130 volunteers with the age of 15 to 30 years who suffer from acne of II degree or more as subjects; the face was cleaned with warm water every morning and evening, and then the sample was spread on the skin and gently rubbed until it was absorbed by the skin for 2 weeks.
Grading standard of acne: degree I: skin lesions are comedones, sporadic or multiple inflammatory rashes; II degree: the degree I plus superficial abscess has a large number of inflammations, but is limited to the face; and (3) III degree: II, the degree II deepens the inflammatory skin rash with cyst, and the cyst occurs on the face, the neck, the chest and the back; and IV degree: if cyst is added at the third degree, scar is easily formed and occurs in the upper half body;
and (3) test results: as shown in table 4 below:
table 4 acne-removing and oil-controlling effect test results
Figure SMS_4
As can be seen from table 4, in the acne-removing compositions of examples 1 to 2 of the present invention, which contain the aqueous phase alone, the acne-removing effect can reach more than 60%, and in the acne-removing compositions of examples 3 to 10, which are provided by the present invention, the aqueous phase and the powder are combined, and the acne-removing effect can reach 100%. Comparative examples 1 and 2 are such that the choice of the parts by weight of zinc azelate and zinc salicylate in the powder phase is outside the scope of the protection of the invention, and comparative example 3 is such that the ratio of the aqueous phase and powder phase is outside the scope of the protection of the invention, the end result showing that the effect is markedly worse.
Test example 2 test of rate of change of fat
The test process comprises the following steps: sebumeter SM815 (German CK), which adopts a world recognized Sebumeter method, works based on the principle of an oil spot photometer, a special extinction adhesive tape of 0.1 mm is pasted on skin, after the oil spot photometer absorbs the oil on the skin of a human body, the adhesive tape can become a semitransparent adhesive tape, and the light transmittance changes correspondingly, so that the transparency is proportional to the amount of the oil spot photometer, the more oil is absorbed, the larger the light transmittance is, and the skin oil content is measured by measuring the light transmittance.
The invention selects volunteers 18-40 years old, half of men and half of women, and requires that the skin of a subject is healthy, has no dermatosis and allergic history, and mainly has oily skin; test area: in the experiment, the right half part of the forehead of the tested person is selected as an experiment area, and the left forehead is used as a comparison area.
Carrying out experiments after the volunteers are in a certain temperature and humidity condition for 30 minutes; before smearing the sample, measuring the sebum value of the part to be measured, and recording a numerical value T0; volunteers sampled at 1.25. Mu.l/cm 2 Coating density is uniform; measuring sebum values of the cosmetic after 0h, 0.5h, 1h and 2h respectively to obtain T1, T2, T3 and T4;
a rate of change in oil content = ((oil content after use of sample-oil content before use of sample)/oil content before use of sample) × 100%;
and (3) test results: as shown in table 5 below;
TABLE 5 test results for rate of change of grease
T1(au) 0.5h oil content change rate (%) 1h oil content Change Rate (%) 2h oil content Change Rate (%)
Example 1 114.55 -8.78 -8.24 -7.56
Example 2 115.45 -8.24 -7.89 -7.31
Example 3 114.43 -10.74 -10.21 -9.08
Example 4 117.48 -10.81 -10.35 -9.21
Example 5 110.59 -12.36 -12.05 -11.58
Example 6 111.45 -11.78 -11.05 -10.00
Example 7 110.58 -11.69 -11.47 -10.24
Example 8 114.58 -10.68 -9.21 -9.07
Example 9 113.60 -10.88 -9.61 -9.35
Example 10 115.55 -10.85 -9.41 -9.19
Comparative example 1 114.55 -10.35 -9.01 -8.15
Comparative example 2 113.51 -10.65 -9.52 -8.54
Comparative example 3 112.52 -10.49 -9.57 -8.98
Blank (not painting) 130.5 5.2 6.5 7.8
As can be seen from table 5, examples 1-2 of the present invention are acne-removing compositions containing aqueous phase alone, and have excellent oil control effect. Examples 3-10 are the acne removing compositions provided by the invention, which combine water phase and powder, and have better oil control effect. Comparative examples 1 and 2 are powder phase, the weight parts of zinc azelate and zinc salicylate are not selected within the scope of the present invention, and comparative example 3 is the ratio of water phase and powder phase is not within the scope of the present invention, and the final results show that the effect is remarkably deteriorated.
Finally, it should be noted that the above embodiments are only used for illustrating the technical solutions of the present invention and not for limiting the protection scope of the present invention, and although the present invention is described in detail with reference to the preferred embodiments, it should be understood by those skilled in the art that modifications or equivalent substitutions can be made to the technical solutions of the present invention without departing from the spirit and scope of the technical solutions of the present invention.

Claims (7)

1. An acne-removing composition is characterized by consisting of a water phase, a powder phase and water; the water phase comprises the following components in parts by weight based on 100 parts by weight: 4-10 parts of cyclodextrin, 0.1-8 parts of salicylic acid, 0.1-10 parts of azelaic acid, 0.01-0.2 part of bactericide, 50-70 parts of solubilizer, 1-5 parts of pH regulator and the balance of water; the powder phase comprises the following components in parts by weight: 40-60 parts of zinc azelate and 40-60 parts of zinc salicylate; the water phase, the powder phase and the water are as follows by mass percent: water phase: powder phase: water = 20-50;
wherein the bactericide is hexamidine di (isethionic acid) salt.
2. The acne removal composition of claim 1, wherein the aqueous phase comprises, based on 100 parts by weight, the following components in parts by weight: 5 parts of cyclodextrin, 5 parts of salicylic acid, 8 parts of azelaic acid, 0.2 part of bactericide, 69 parts of solubilizer, 3 parts of pH regulator and the balance of water.
3. The acne-removing composition according to claim 1 or 2, wherein the solubilizer is at least one of ethanol, propylene glycol, ethoxydiglycol, hydrogenated castor oil; the pH regulator is sodium hydroxide.
4. The acne removal composition according to claim 1, wherein the powder phase comprises the following components in parts by weight: 50 parts of zinc azelaic acid and 50 parts of zinc salicylate.
5. The acne-removing composition according to claim 1, wherein the water phase, the powder phase and the water are as follows by mass percent: water phase: powder phase: water =42: 25:33.
6. a method for preparing the acne-removing composition according to any one of claims 1-5, which comprises the following steps:
(1) Mixing salicylic acid, cyclodextrin and water, and heating to dissolve to obtain a mixture A; mixing and dissolving azelaic acid, solubilizer and bactericide to obtain a mixture B;
(2) Mixing the mixture A, the mixture B and water obtained in the step (1), adjusting the pH value, and cooling to obtain a water phase;
(3) And (3) mixing and dispersing zinc salicylate, zinc azelate and water uniformly, and mixing with the water obtained in the step (2) to obtain the acne-removing composition.
7. Use of an anti-acne composition according to any of claims 1 to 5 in the preparation of a cosmetic product.
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GB9712272D0 (en) * 1997-06-12 1997-08-13 Procter & Gamble Cosmetic composition
CN105796424B (en) * 2016-03-31 2018-10-09 广东食品药品职业学院 A kind of acne-removing composition and its application in cosmetics
CN108143639B (en) * 2018-02-08 2021-05-07 广州美尔生物科技有限公司 Acne removing cream and preparation method thereof
CN108553411B (en) * 2018-07-25 2020-05-12 成都卓阳生物科技有限公司 Azelaic acid gel and preparation method and application thereof
US11872297B2 (en) * 2018-10-30 2024-01-16 Advance ZincTek Limited Anti-acne composition

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