CN113413331B

CN113413331B - Acne-removing composition and preparation and application thereof

Info

Publication number: CN113413331B
Application number: CN202011612163.7A
Authority: CN
Inventors: 吴慎剑; 林秋秋; 苏金净; 张晶; 林君玉; 高剑滨
Original assignee: Xiamen Zhong Ling Yi Yong Technology Co ltd
Current assignee: Xiamen Zhong Ling Yi Yong Technology Co ltd
Priority date: 2020-12-30
Filing date: 2020-12-30
Publication date: 2022-09-13
Anticipated expiration: 2040-12-30
Also published as: CN113413331A

Abstract

The invention discloses an acne-removing composition, and a preparation and application thereof. The raw materials of the acne-removing composition comprise allantoin, safflower oil, evening primrose oil, hexamidine di (isethionic acid) salt, phloretin and the like. The acne-removing composition disclosed by the invention can quickly and effectively kill propionibacterium acnes, inhibit inflammation, simultaneously relax and condition skin, keep clean and achieve the effect of quickly removing acne, overcomes the incompatibility of hexamidine di (isethionic acid) salt, enables the system of the composition to be stable and effective, and has a wide application prospect.

Description

Acne-removing composition and preparation and application thereof

Technical Field

The invention belongs to the technical field of cosmetics, and particularly relates to an acne-removing cosmetic.

Background

The long whelk is a trouble experienced by most people, and particularly for teenagers, because the metabolism is vigorous in the adolescence stage, the grease on the surface of the skin is increased, and a small amount or even a large amount of pimples appear on the face, which eliminates the problem. In daily study and life, the influence of the acne is huge, which not only causes skin itch continuously and pain is difficult to endure physiologically, but also influences social contact, and serious people can generate inferior psychology and erode physical and mental health of teenagers.

The occurrence of whelk is closely related to factors such as excessive sebum secretion, blockage of pilosebaceous ducts, bacterial infection and inflammatory reaction. After adolescence, the level of androgen, particularly testosterone, in a human body is rapidly increased, the development of sebaceous glands is promoted, and a large amount of sebum is produced. Meanwhile, abnormal keratinization of the pilosebaceous canal causes the canal to be blocked, sebum is discharged to be obstructed, and a cutin plug, namely a micro acne is formed. A number of microorganisms in the hair follicle, particularly propionibacterium acnes, multiply in number, and lipases produced by propionibacterium acnes break down sebum to produce free fatty acids, while chemotactic inflammatory cells and mediators, ultimately inducing and exacerbating the inflammatory response.

Currently, most commonly used acne-removing cosmetics are salicylic acids, oligopeptides, and aloe vera gels. Salicylic acid can soften skin stratum corneum, promote drug penetration, but easily cause skin allergy; oligopeptides and aloe vera gel are focused on late pit repair and have little inhibitory effect on the early growth of whelk. The broad spectrum antibacterial agents used at present are salicylic acid, quaternary ammonium salt-73, and caprylhydroxamic acid, etc. For example, in the acne removing essence disclosed in CN111803433A and the preparation method thereof, caprylyl hydroximic acid and quaternary ammonium salt-73 are used as antibacterial agents, but the rest components in the acne removing essence have no acne removing function, and are only used as general system components, and do not contain synergistic components, so that the acne removing effects of the two antibacterial agents cannot be fully exerted, and the effect is not good.

The hexamidine di (isethionic acid) salt belongs to hexamidine and salts thereof, and the substances are broad-spectrum water-soluble bactericides, have broad-spectrum antibacterial and bactericidal properties, and have strong resisting and killing functions on gram-negative bacteria, gram-positive bacteria, mold, yeast, dermatophyte and the like. Reports show that the bactericide hexamidine di (isethionic acid) salt has lower minimum bactericidal concentration than the bactericide, has more specific killing effect on propionibacterium acnes, and is a potential acne-removing substance. But hexamidine di (isethionate) salt is a cationic species which, when added to the system, causes the two to react to form a precipitate or floc, resulting in system collapse. Hexamidine di (isethionate) salt, on the other hand, only exerts its bactericidal activity in the free state, and if it forms a precipitate or floc, it loses its activity. For example, in the acne-removing traditional Chinese medicine composition disclosed in CN111588815A and the application thereof and the acne-removing balance essence containing the composition, although hexamidine di (isethionic acid) salt is used, xanthan gum and acrylic acid (ester) which are thickening stabilizers belong to anionic substances, and are liable to react with hexamidine di (isethionic acid) salt to form precipitates or flocs, which causes system instability. In addition, the Chinese herbal medicine composition has limited effect, really plays a role of acne-removing synergistic components, and the components have the condition of overlapping effect and single function, do not have the synergistic effect of other functional substances, and have poor actual use effect.

Therefore, although many researches on the acne removing aspect of the hexamidine di (isethionic acid) salt are reported, in the actual product development process, due to the particularity of difficult compatibility and the large irritation and toxic and side effects of the hexamidine di (isethionic acid) salt on the skin, the acne removing product adopting the hexamidine di (isethionic acid) salt as the main material still has little success in the market.

Disclosure of Invention

The invention aims to overcome the defects of the prior art and provides an acne-removing composition, a preparation and application thereof.

One of the technical schemes adopted by the invention for solving the technical problems is as follows:

the acne-removing composition comprises the following raw materials in parts by weight: 20-150 parts of PEG-40 hydrogenated castor oil or PEG-50 hydrogenated castor oil, 10-200 parts of hydroxyethyl cellulose or hydroxypropyl methyl cellulose, 10-50 parts of allantoin, 10-50 parts of safflower oil, 5-50 parts of evening primrose oil, 5-150 parts of hexamidine di (hydroxyethyl sulfonate) salt and 1-5 parts of phloretin.

Further, the raw materials of the acne-removing composition also comprise: 9350-9940 parts of water.

Preferably, the acne-removing composition comprises the following raw materials in parts by weight: 95-105 parts of PEG-40 hydrogenated castor oil or PEG-50 hydrogenated castor oil, 95-105 parts of hydroxyethyl cellulose or hydroxypropyl methyl cellulose, 18-22 parts of allantoin, 38-42 parts of safflower oil, 38-42 parts of evening primrose oil, 8-12 parts of hexamidine di (hydroxyethyl sulfonate) salt and 1-2 parts of phloretin.

Still more preferably, the acne-removing composition comprises the following raw materials in parts by weight: 9688 to 9690 parts of water, 99 to 101 parts of PEG-50 hydrogenated castor oil, 99 to 101 parts of hydroxyethyl cellulose, 19 to 21 parts of allantoin, 39 to 41 parts of safflower oil, 39 to 41 parts of evening primrose oil, 9 to 11 parts of hexamidine di (isethionic acid) salt, and 1 to 1.2 parts of phloretin.

In the acne-removing composition, the raw material components have the following functions:

water: a solvent;

PEG-40 hydrogenated Castor oil or PEG-50 hydrogenated Castor oil: has the functions of moisture retention and solubilization, and can uniformly disperse oily substances into water after being added, so that a solution system is more stable;

hydroxyethyl cellulose or hydroxypropyl methylcellulose: thickening agent and humectant to prevent too rapid volatilization of water and protect skin;

allantoin: soothing the skin;

safflower oil: diminishing inflammation, relieving pain and promoting the absorption of the medicine;

evening primrose oil: anti-inflammatory, improving skin environment;

hexamidine di (isethionic acid) salt: bactericides and preservatives;

phloretin: an antioxidant.

In the acne-removing composition, the hexamidine di (hydroxyethyl sulfonate) salt is a broad-spectrum bacteriostatic agent and can inhibit and kill propionibacterium acnes and malassezia inside whelk; evening primrose oil and safflower oil can enhance the acne-removing effect; when the hexamidine di (isethionate) salt is used alone, the acne removing effect is poor; after the evening primrose oil and the safflower oil are added, the absorption of the skin can be promoted, the sterilization effect can be enhanced, the skin state can be improved, and the effect of curing the acne can be achieved. The acne-removing composition further reduces the skin irritation through the matching of the components, has the effects of relieving, diminishing inflammation, relieving itching and easing pain, and overcomes the defects of large skin irritation and large toxic and side effects caused by the practical application of hexamidine di (isethionate).

The invention further researches and discovers that the growth of the whelk is mainly divided into four stages, namely a latent stage, a growing stage, a vigorous stage and a repairing stage. Wherein the incubation period and the growth period are initial stages of the propionibacterium acnes beginning to proliferate, the vigorous stage is a stable stage of bacteria mass propagation and inflammation initiation, and the repair period is a wound surface left by the natural death of the bacteria after inflammatory reaction. Most acne removing formulas on the market are usually only concentrated in the repair period after acne growth, and have no actual or weak intervention capacity for the first three stages. The acne removing composition provided by the invention depends on the stronger bactericidal ability of hexamidine di (isethionic acid) salt and the synergistic promotion effect of safflower oil and evening primrose oil, and can kill bacteria in advance in the incubation period and the growth period or quickly kill bacteria in the vigorous period so as to reduce the time and degree of inflammation, thereby reducing the wound surface.

On the other hand, long-term stability of cosmetics is critical to chemical stability (e.g., whether or not a precipitate or floc is produced), microbial contamination, and oxidation problems. In the aspect of chemical stability, as mentioned above, hexamidine di (isethionic acid) salt is a cationic bacteriostatic agent, and has incompatibility with part of common auxiliary materials, for example, it can be crosslinked with anionic surfactant, so that precipitate is separated out, and the bacteriostatic performance is ineffective. The acne-removing composition disclosed by the invention does not generate precipitates or floccules through proper component compatibility; the physicochemical properties of the acne-removing composition, such as color, transparency, pH value, viscosity and the like, are reduced or added within the range of the mixture ratio of the acne-removing composition, and the physicochemical properties, the stability and the like are not obviously changed. In the aspect of microbial pollution, hexamidine di (isethionic acid) salt is used as a bactericidal preservative, and most of microorganisms cannot grow in a system; in terms of oxidation problems, phloretin is an antioxidant that effectively protects the system from oxidation. Therefore, the acne-removing composition overcomes the incompatibility through the matching of the components, and has a stable system.

The second technical scheme adopted by the invention for solving the technical problems is as follows:

the acne removing composition is used for preparing cosmetics.

The third technical scheme adopted by the invention for solving the technical problems is as follows:

a preparation comprising the acne-removing composition comprises a water agent or an ointment.

The water aqua provided by the invention is a liquid preparation prepared by dissolving the acne-removing composition and other optional components in water. Application may be by painting, rolling, etc.

The paste of the invention is a semisolid or thick liquid external preparation prepared by mixing the acne-removing composition and other optional components with a proper substrate, and can be in a cream shape, a gel shape or a thick liquid shape.

Preferably, the formulation is aqueous. For example, the acne removing essence can be prepared for use.

The preparation may further comprise other adjuvants, as required.

According to the needs, the preparation can further comprise other components with the functions of removing acnes, sterilizing and inhibiting bacteria. For example, when a material having a peeling and penetrating function such as salicylic acid is added, the effect on closed acne is more excellent.

The equipment, reagents, processes, parameters and the like related to the invention are conventional equipment, reagents, processes, parameters and the like except for special description, and no embodiment is needed.

All ranges recited herein include all point values within the range.

Compared with the background technology, the technical scheme has the following advantages:

1. when the acne-removing composition is compatible, incompatibility of hexamidine di (isethionic acid) salt and each component is avoided, and selected components do not react with the hexamidine di (isethionic acid) salt to form precipitates or floccules, so that the system of the composition can be kept stable and effective.

2. The acne-removing composition disclosed by the invention inhibits and kills propionibacterium acnes in the acne through the hexamidine di (hydroxyethyl sulfonate) salt, so that the occurrence of inflammation is reduced, the acne to be grown can be eliminated as soon as possible, and the effect of quickly removing the acne is achieved; the safflower oil and the evening primrose oil are added to have the functions of relieving, diminishing inflammation and promoting absorption, and have synergistic effect with hexamidine di (isethionate), so that absorption can be promoted, the acne is sterilized and removed, and itching and pain can be quickly relieved in use experience.

3. The acne-removing composition disclosed by the invention can quickly and effectively kill propionibacterium acnes and inhibit inflammation in the latent period, the growth period and the vigorous period of acnes, and meanwhile, the acne-removing composition is capable of relaxing and conditioning the skin, keeping the skin clean and achieving the effect of quickly removing acnes.

4. The acne-removing composition disclosed by the invention is harmless to a human body, has no toxic or side effect, is remarkable in acne-removing effect, is simple in preparation method and use method, and has a wide application prospect.

Detailed Description

The present invention is specifically illustrated by the following examples:

example 1: compatibility stability study of acne-removing composition

Formulation 1-1; the components in parts by weight are as follows: 9990 parts of water and 10 parts of hexamidine di (hydroxyethyl sulfonate) salt.

1-2 of a formula; the components in parts by weight are as follows: 9980 parts of water, 10 parts of hexamidine di (hydroxyethyl sulfonate) salt and 10 parts of hydroxyethyl cellulose.

1-3 of a formula; the components in parts by weight are as follows: 9980 parts of water, 10 parts of hexamidine di (hydroxyethyl sulfonate) salt and 10 parts of hydroxypropyl methyl cellulose.

1-4 of a formula; the components in parts by weight are as follows: 9980 parts of water, 10 parts of hexamidine di (isethionic acid) salt and 10 parts of carbomer.

1-5 of a formula; the components in parts by weight are as follows: 9980 parts of water, 10 parts of hexamidine di (hydroxyethyl sulfonate) salt and 10 parts of xanthan gum.

1-6 of a formula; the components in parts by weight are as follows: 9980 parts of water, 10 parts of hexamidine di (hydroxyethyl sulfonate) salt and 10 parts of bisabolol.

1-7 of a formula; the components in parts by weight are as follows: 9980 parts of water, 10 parts of hexamidine di (isethionic acid) salt and 10 parts of sodium hyaluronate.

1-8 of a formula; the components in parts by weight are as follows: 9980 parts of water, 10 parts of hexamidine di (isethionic acid) salt and 10 parts of dipotassium glycyrrhizinate.

TABLE 1 results for stability of formulation

As can be seen from table 1, the commonly used auxiliary components in the acne-removing cosmetics, such as dipotassium glycyrrhizinate, bisabolol, sodium hyaluronate and the like, belong to cationic substances, and cannot be used together with hexamidine di (isethionic acid) salt; adjuvant ingredients such as carbomer and xanthan gum are also cationic materials and may not be used.

According to the invention, through research, allantoin, nicotinamide and beta-glucan can be compatible with hexamidine di (isethionic acid) salt, hydroxyethyl cellulose and hydroxypropyl methyl cellulose can be used as thickening agents, no precipitate or floccule is formed, and the system is stable.

Example 2: efficacy study of acne-removing composition

Formulation 2-1: the raw materials are as follows according to the weight portion: 9869 parts of water, 100 parts of PEG-50 hydrogenated castor oil, 10 parts of hydroxyethyl cellulose, 20 parts of allantoin and 1 part of phloretin;

and (2) formula 2-2: the raw materials comprise the following components in parts by weight: 9699 parts of water, 100 parts of PEG-50 hydrogenated castor oil, 100 parts of hydroxyethyl cellulose, 20 parts of allantoin, 40 parts of safflower oil, 40 parts of evening primrose oil and 1 part of phloretin;

and (2) formula 2-3: the raw materials are as follows according to the weight portion: water 9729 parts, PEG-50 hydrogenated castor oil 100 parts, hydroxyethyl cellulose 100 parts, allantoin 20 parts, evening primrose oil 40 parts, hexamidine di (isethionic acid) salt 10 parts, and phloretin 1 part.

And (2) formula 2-4: the raw materials are as follows according to the weight portion: water 9729 parts, PEG-50 hydrogenated castor oil 100 parts, hydroxyethyl cellulose 100 parts, allantoin 20 parts, safflower oil 40 parts, hexamidine bis (isethionic acid) salt 10 parts, and phloretin 1 part.

And (2) formula 2-5: the raw materials are as follows according to the weight portion: 9689 parts of water, 100 parts of PEG-50 hydrogenated castor oil, 100 parts of hydroxyethyl cellulose, 20 parts of allantoin, 40 parts of safflower oil, 40 parts of evening primrose oil, 10 parts of hexamidine di (isethionic acid) salt and 1 part of phloretin.

TABLE 2 raw material composition of formulas 2-1 to 2-5

The formula 2-1 to 2-5 is directly prepared into a water aqua as an essence which is directly smeared on an affected part when being used. Can also be used for whole face.

According to the ' clinical evaluation standard for acne-removing skin care products ' in the ' national institute of non-public medical institutions ' association standards (T/CNMIA0012-2020 '), 100 volunteers are selected, and 20 testers are selected from each test group. The acne removing essence prepared according to the formula 2-1-2-5 is used by participants every day for 7 days.

Firstly, symptom improvement evaluation:

other skin care products of the same type must not be used during the experiment, and the subjects have completed the verification process, and the experimental results are shown in table 3, wherein:

and (3) healing: the skin damage regression rate is more than or equal to 90 percent;

the effect is shown: the skin damage fading rate is 60-89%;

improvement: the skin damage fading rate is 20-59%;

and (4) invalidation: the skin damage fading rate is less than or equal to 20 percent.

TABLE 3 acne removing Effect

	Recovery method	Show effect	Improvement of life	Invalidation
					Formulation 2-1	0	2	1	17
Formulation 2 to 2	2	3	6	9
					Formulations 2 to 3	10	6	4	2
Formulations 2 to 4	9	5	6	0
					Formulations 2 to 5	18	1	1	0

As can be seen from the clinical improvement evaluation results in Table 3, the acne-removing composition provided by the formulas 2 to 5 has a good acne-removing effect on the skin of most of the testers, and the aim of quickly removing acnes is fulfilled.

Secondly, safety evaluation:

adverse reactions included the appearance of erythema, papules, dryness, desquamation, itching, burning, stinging, and other symptoms, assessed as in table 4, where:

mild adverse reactions: adverse reactions were easily tolerated and were occasionally felt by the subjects;

moderate adverse reactions: adverse reactions hinder daily activities, and subjects have obvious subjective symptoms but can tolerate the symptoms without stopping taking the test products;

severe adverse reactions: adverse reactions hampered daily activities, with subjective symptoms noted by subjects who were intolerable and required discontinuation.

TABLE 4 adverse reaction assessment

	No adverse reaction	Mild degree of	Of moderate degree	Severe degree of gravity
					Formulation 2-1	16	4	0	0
Formulation 2-2	19	1	0	0
					Formulations 2 to 3	18	2	0	0
Formulations 2 to 4	19	1	0	0
					Formulations 2 to 5	20	0	0	0

As can be seen from the safety evaluation results in table 4, the acne-removing compositions provided by the formulas 2 to 5 of the present invention have no adverse reaction or few mild adverse reactions, which indicates that the components in the formula range of the acne-removing compositions of the present invention have no adverse reaction basically.

Example 3: evaluation of skin irritation of acne-removing composition:

the evaluation method comprises the following steps: human body patch test

60 volunteers applied the spot tester with acne-removing product on the back or forearm of the subject with a low-sensitivity adhesive tape according to the skin spot test of human body described in technical Specification for cosmetic safety (2015 edition), and applied the patch tester on the skin uniformly by pressing with palm for 24 h. The anti-acne essence prepared according to formulas 2-1 to 2-5 is tested for irritation to human skin, and the results are shown in table 5, wherein:

stage 0: no reaction

Level 1: pale erythema

And 2, stage: erythema, infiltrations, papules

And 3, level: erythema, edema, papules, blisters

4, level: erythema, edema, bulla

TABLE 5 evaluation of skin irritation

	Grade of rating	Skin reactions
			Formulation 2-1	1	Slight reaction
Formulation 2 to 2	0	Negative reaction
			Formulations 2 to 3	1	Slight erythema
Formulations 2 to 4	1	Slight erythema
			Formulations 2 to 5	0	Negative reaction

As can be seen from the results of the skin irritation evaluation in table 5, the acne removal products prepared according to formulas 2 to 5 have not only good acne removal effects but also low skin irritation, and it is presumed that the safflower oil and the evening primrose oil have good effects of soothing the skin and reducing irritation, and the safflower oil and the evening primrose oil synergistically eliminate the skin irritation caused by hexamidine bis (isethionic acid) salt.

The above description is only a preferred embodiment of the present invention, and therefore should not be taken as limiting the scope of the invention, which is defined by the appended claims and their equivalents.

Claims

1. An acne-removing composition is characterized in that: the raw materials comprise the following components in parts by weight: 20-150 parts of PEG-40 hydrogenated castor oil or PEG-50 hydrogenated castor oil, 10-200 parts of hydroxyethyl cellulose or hydroxypropyl methyl cellulose, 10-50 parts of allantoin, 10-50 parts of safflower oil, 5-50 parts of evening primrose oil, 5-150 parts of hexamidine di (hydroxyethyl sulfonate) salt and 1-5 parts of phloretin; the preparation of the acne-removing composition is water aqua.

2. The acne-removing composition according to claim 1, wherein: the acne-removing composition also comprises the following raw materials: 9350-9940 parts of water.

3. The acne-removing composition according to claim 1, wherein: the acne-removing composition comprises the following raw materials in parts by weight: 95-105 parts of PEG-40 hydrogenated castor oil or PEG-50 hydrogenated castor oil, 95-105 parts of hydroxyethyl cellulose or hydroxypropyl methyl cellulose, 18-22 parts of allantoin, 38-42 parts of safflower oil, 38-42 parts of evening primrose oil, 8-12 parts of hexamidine di (hydroxyethyl sulfonate) salt and 1-2 parts of phloretin.

4. The acne-removing composition according to claim 1, characterized in that: the acne-removing composition comprises the following raw materials in parts by weight: 9688 to 9690 parts of water, 99 to 101 parts of PEG-50 hydrogenated castor oil, 99 to 101 parts of hydroxyethyl cellulose, 19 to 21 parts of allantoin, 39 to 41 parts of safflower oil, 39 to 41 parts of evening primrose oil, 9 to 11 parts of hexamidine di (isethionic acid) salt, and 1 to 1.2 parts of phloretin.

5. Use of the acne-removing composition according to any one of claims 1 to 4 in the preparation of cosmetics.