KR101151008B1 - Cosmetic composition containing phytantriol and hexamidine diisethionate for improving acnes - Google Patents

Abstract

The present invention relates to a cosmetic composition for improving acne, and more specifically, phytantriol (Phytantriol) by disturbing the cell membrane of Propionibacterium acnes (causal agent of acne) hexamidine di-ethionate (Hexamidine It relates to an anti acne cosmetic composition effective in improving acne by increasing the antibacterial activity of diisethionate).

Description

Cosmetic composition for improving acne containing phytantriol and hexamidine diethionate {Cosmetic composition containing Phytantriol and Hexamidine diisethionate for improving acnes}

The present invention relates to a cosmetic composition for improving acne, and more specifically, phytantriol (Phytantriol) by disturbing the cell membrane of Propionibacterium acnes (causal agent of acne) hexamidine di-ethionate (Hexamidine It relates to an anti acne cosmetic composition effective in improving acne by increasing the antibacterial activity of diisethionate).

In general, acne is an inflammatory response caused by stimulation of free fatty acids produced by lipase of propionibacterium acnes, which is an excess of sebum secretion, excessive keratinization and anaerobic dermatitis, and various small molecule substances. This is known as the cause. Drugs in the form of oral or external preparations have been used to treat acne, for example, anti-androgens that inhibit sebum production, nonsteroidal anti-inflammatory agents that act as anti-inflammatory agents, and lesocinols, sulfur, salicylic acid, and benzoyl peroxide. And antimicrobial agents such as isotretinoin and keratin release agents, tetracycline, erythromycin, and methods for inhibiting the activity of propionibacterium acne bacteria by antibiotics such as methacycline. On the other hand, recently, a treatment method using a vitamin A derivative such as retinoic acid and a skin method using azelaic acid are also widely used. In addition, a technology related to cosmetics effective for acne using myrrh, which has been used as a medicinal herb for a long time, was also introduced in Korea Patent Publication No. 95-8762 (Lee Jae-jae, etc.).

However, the methods described above have some results in acne treatment, but have some problems in terms of effectiveness, side effects, and usability. In other words, the use of hormonal agents has been reported to inhibit epidermal growth and other hormonal abuse side effects, and keratin exfoliants such as retinoic acid and benzoyl peroxide may cause skin irritation and contact dermatitis due to exfoliation. The antibiotics mentioned above are known for the emergence of resistant bacteria and for the possibility of photosensitivity. In particular, isotretinoin is known to have a teratogenic effect on the fetus. In addition, cosmetic compositions effective for acne using conventional oriental herbal plant extracts, such as myrrh, may be effective in acknowledgment, but may have an allergic hypersensitivity reaction to acne-sensitive skin in some cases. I have a problem.

Therefore, the necessity of developing a safe and effective product for the human body in acne skin is steadily emerging.

The present inventors have found that phytantriol alone has no effect on acne improvement, but surprisingly, phytantriol disrupts the cell membranes of propionibacterium acnes to increase the antimicrobial activity of hexamidine diethionate, thus completing the present invention. It was.

Therefore, the present invention contains a phytantriol (Phytantriol) and hexamidine diisethionate (Hexamidine diisethionate) containing a cosmetic composition for improving acne having an effective effect on acne skin by inhibiting acne-inducing bacteria propionibacterium acnes to provide.

The present invention may include the following means to solve the above problems.

The cosmetic composition for improving acne according to the present invention contains phytantriol and hexamidine diethionate as active ingredients.

     The phytantriol is characterized in that it contains 0.01 to 10.0% by weight based on the total weight of the composition.

The hexamidine diisethionate is characterized in that it contains 0.0001 to 5.0% by weight relative to the total weight of the composition.

The cosmetic composition is selected from the group consisting of supple cosmetics, astringent cosmetics, nourishing cosmetics, eye cream, nourishing cream, massage cream, cleansing cream, cleansing foam, cleansing water, solid soap, liquid soap, powder, essence, pack It is characterized by having a formulation.

The present invention relates to a cosmetic composition for improving acne, which is effective for improving acne by increasing the antimicrobial activity of hexamidine diethionate by disturbing the cell membrane of propionibacterium acnes, which is a cause of acne, phytantriol acne. Cosmetic compositions can be provided.

The inventors have found that phytantriol and hexamidine diethionate exhibit excellent antimicrobial activity against propionibacterium acnes, the causative agent of acne, and found that the effect is also excellent.

The phytantriol of the present invention is a conventional name of a compound known as 3,7,11,15-tetramethylhexadecane-1,2,3-triol, as represented by the following formula (1), BASF (1609 Biddle Avenue, Whyandotte, MI).

Petantriol, an aliphatic alcohol, has the formula C ₂₀ H ₄₂ O ₃ and a molecular weight of 330.55. A yellow viscous liquid that is easy to dissolve in oils and alcohols. Phytantriol, when added to hair products, is known to improve the hair's moisturizing ability, improve the hair's adsorption capacity of amino acids, improve the hair's strength, and protect the hair from the hot air of the hair dry, and is also reported as a penetration enhancer (Kozment (Spec. Issue. ), 19-25 (1994)).

The hexamidine diethionate of the present invention is represented by the following general formula (2), and is a conventional name of a compound known as 4,4'diamidino-α-ω-diphenoxyhexane, bis (b-hydroxyethane sulfonate), Cognis Co., Ltd. It is commercially available from (France). The cationic substance, hexamidinediisethionate, has the formula C ₂₄ H ₃₈ N ₄ O ₁₀ S ₂ and a molecular weight of 606.72.

In the present invention, it is characterized by containing 0.01% to 10.0% of the total weight of the composition of phytantriol having an effective effect on acne skin by inhibiting acne bacteria. If the amount is less than 0.01% by weight, the effect is insignificant. If it is added in excess of 10.0% by weight, problems of precipitation due to solubility may occur.

The content of hexamidine diisethionate is characterized by containing 0.0001% to 5.0% by weight of the total weight of the composition. If the amount is less than 0.0001% by weight, the effect is insignificant. If the amount is more than 5.0% by weight, the synergistic effect due to the excess amount is not economical.

The cosmetic composition containing the phytantriol and hexamidine diethionate may be prepared in any formulation commonly prepared in the art, for example, softening water, astringent makeup, nourishing cosmetic, eye cream, nutrition Creams, massage creams, cleansing creams, cleansing foam, cleansing water, powder, essences, packs and the like is not particularly limited, and may be prepared according to the formulation or purpose of use of the cosmetics.

Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are only for illustrating the present invention in more detail, it is to those skilled in the art that the scope of the present invention is not limited by these examples in accordance with the gist of the present invention. Will be self-evident.

Experimental Example 1 Antibacterial Effect of Pitanium Triol and Hexamidine Diethionate

In order to measure the antimicrobial effect of the phytantriol and hexamidine diethionate of the present invention against acne bacteria, inoculated with propionibacterium acnes ATCC 6919 in brain heart infusion culture medium and incubated for 24 hours in a 37 ℃ shaking incubator After measuring the concentration to the OD 600nm value was inoculated in a medium containing 10 ~ 10000ppm of the sample shown in Table 1 at a final concentration of 10 ⁷ CFU / ml. Then, after incubating at 37 ° C. and 200 rpm for 48 hours, the antimicrobial activity was measured by using a minimum inhibitory concentration (MIC) as a concentration that significantly reduced the number of bacteria inoculated.

Minimum Growth Inhibition Concentration (MIC) Sample Name MIC (ppm) Phytantriol > 10000 Hexamidine diethionate 20 Pitatantriol + hexamidine diethionate (2: 8) 10 Tea tree oil 10000 Erythromycin 200 Benzoyl peroxide 1000

As can be seen from Table 1, hexamidine dietisionate showed a very good antibacterial activity compared to tea tree oil, erythromycin, benzoyl peroxide, which has been used as an active ingredient in conventional acne treatment. Although phytantriol itself has no antimicrobial activity against acne bacteria, the mixture of phytantriol and hexamidine diethionate in a 2: 8 ratio showed better antimicrobial activity than those used alone. Therefore, excellent acne healing effect of the cosmetic composition using the same is expected.

In order to measure the acne improvement effect and skin irritation of the acne improvement cosmetic composition containing phytantriol and hexamidine diethionate, the acne cosmetic composition was prepared according to Examples and Comparative Examples 1 to 3, respectively, according to a conventional method. The composition is shown in Table 2 below.

Examples and Comparative Examples 1-3 Compounding ingredient Example Comparative Example 1 Comparative Example 2 Comparative Example 3 Hexamidine diethionate 0.16 0.2 - - Phytantriol 0.04 - 0.2 - Propylene glycol 6.0 6.0 6.0 6.0 glycerin 4.0 4.0 4.0 4.0 Triethanolamine 1.2 1.2 1.2 1.2 Tocophenyl Acetate 3.0 3.0 3.0 3.0 Liquid paraffin 5.0 5.0 5.0 5.0 Squalane 3.0 3.0 3.0 3.0 Macadamia Nut Oil 2.0 2.0 2.0 2.0 Polysorbate 60 1.5 1.5 1.5 1.5 Sorbitan sesquioleate 1.0 1.0 1.0 1.0 Xanthan Gum 0.3 0.3 0.3 0.3 Incense, preservative a very small amount a very small amount a very small amount a very small amount Purified water To 100 To 100 To 100 To 100

Experimental Example 2 Measurement of Improvement of Acne

 In order to confirm the effect of acne treatment of the present invention, blind test was conducted on 80 healthy men and women aged 20 to 30 years with acne. The experimental method was randomly divided into four groups of 20 people, and Examples and Comparative Examples 1 to 3 were applied twice a day for 2 months. The evaluation was carried out by classifying acne status according to the criteria in Table 3 and combining survey and visual survey. The skin condition of acne in clinical trial subjects was judged to be excellent if it showed more than 3 grade reduction compared to the start of the experiment, good if it showed 1 ~ 2 grade reduction, no effect if there was no grade difference, and worsened if the grade was increased. . The results are shown in Table 4 below.

Rating Skin condition 0 normal One Small number of cotton veins 2 Medium cotton patch without inflammation 3 Scalp of inflammatory papules 4 Small nodules and inflammatory scalp 5 Papular nodules 6 Moderate inflammatory nodules 7 Large number of inflammatory nodules 8 Severe nodular scalp 9 Severe cystic and inflammatory nodules

term Great Good no effect worse Example 13/20 (65%) 5/20 (25%) 2/20 (10%) -/ 20 Comparative Example 1 7/20 (35%) 7/20 (35%) 6/20 (30%) -/ 20 Comparative Example 2 - - 18/20 (90%) 2/20 (10%) Comparative Example 3 - - 16/20 (80%) 4/20 (20%)

As can be seen in Table 4, the cosmetic composition (Example) containing phytantriol and hexamidine diethionate at the same time is used in a cosmetic composition (Comparative Example 1) using hexamidine diethionate alone. Compared to the improvement of acne can be seen that excellent.

Experimental Example 3 Skin Patch Test (Patch Test)

20 subjects (mean age 29 years, age distribution 23-39 years) to measure the skin safety of the cosmetic composition containing the phytantriol and hexamidine diethionate of the present invention (Example) and Comparative Examples 1 to 3 ) And the skin patch experiment on the upper arm using Examples and Comparative Examples 1-3. However, psoriasis, eczema, and other skin lesion holders, pregnant women, lactating or contraceptives, antihistamines, etc. were excluded from the experiment.

First, the test area was wiped with 70% ethanol, dried, and the prepared test material was added dropwise into the pin chamber (Finn chamber, 100x10, EPITEST, Finland) by 15 µg, and then airtightly wrapped on the inner part of the subject's forearm. The patch was marked for 24 hours, the patch was removed, and the test site was marked with a pen. After 1 hour and 24 hours after the marking, the magnification (8MC-150, DAZOR, United States of America) was used to observe the test site, and erythema and edema were observed.

The skin response was determined according to the regulations of the International Contact Dermatitis Research Group (ICDRG), and the mean skin response rate was calculated according to Equation 1. The results are shown in Table 5.

* Evaluation criteria and score of skin reaction

sign score Evaluation standard - 0 No response ± 0.5 Faint or light erythema + One Boundary but weak erythema, edema and papules ++ 2 Pronounced erythema, papules and vesicles +++ 3 Severe erythema and alveolar, scleroderma

Mean skin responsiveness (mean score) = (score × number of responses × 100 × 1/2) / [3 (maximum score) × total number of subjects (n)]

Test substance After 1 hour After 24 hours Reactivity (%)
(n = 20) ± + ++ ± + ++ Example One - - - - - 0.42 Comparative Example 1 One - - - - - 0.42 Comparative Example 2 One - - - - - 0.42 Comparative Example 3 One - - - - - 0.42

As can be seen in Table 5, the cosmetic composition containing the phytantriol and hexamidine diethionate of the present invention (Example) is similar to Comparative Example 3 and the degree of irritation to the skin is found to be almost no skin irritation Can be.

Hereinafter, various formulation examples for the cosmetic composition containing the phytantriol and hexamidine dietisionate of the present invention are prepared according to a manufacturing method in the conventional cosmetic field. However, the composition of the present invention is not limited to the following formulation examples.

Formulation Example 1 Preparation of Soft Cosmetics (Skin)

To prepare a flexible lotion containing phytantriol of the present invention and hexamidinediisethionate, it is blended as described in Table 6 below and prepared according to a manufacturing method in a conventional cosmetic field.

Compounding ingredient Content (% by weight) Hexamidine diethionate 0.02 Phytantriol 0.1 1,3-butylene glycol 6.0 glycerin 4.0 Oleyl alcohol 0.1 Polysorbate 20 0.5 ethanol 15.0 Benzophenone-9 0.05 Incense, preservative a very small amount Purified water To 100

Formulation Example 2-nourishing lotion (milk lotion)

To prepare a nourishing lotion containing phytantriol and hexamidine diethionate of the present invention, it is blended as described in Table 7 and prepared according to a manufacturing method in a conventional cosmetic field.

Compounding ingredient Content (% by weight) Hexamidine diethionate 0.05 Phytantriol 0.1 Propylene glycol 6.0 glycerin 4.0 Triethanolamine 1.2 Tocophenyl Acetate 3.0 Liquid paraffin 5.0 Squalane 3.0 Macadamia Nut Oil 2.0 Polysorbate 60 1.5 Sorbitan sesquioleate 1.0 Xanthan Gum 0.3 Incense, preservative a very small amount Purified water To 100

Formulation Example 3 Preparation of Nutritional Cream

To prepare a nourishing cream containing phytantriol and hexamidine diethionate of the present invention, it is combined as described in Table 8 and prepared according to a manufacturing method in a conventional cosmetic field.

Compounding ingredient Content (% by weight) Hexamidine diethionate 0.05 Phytantriol 0.1 vaseline 7.0 Liquid paraffin 10.0 Beeswax 2.0 Polysorbate 60 2.5 Sorbitan sesquioleate 1.5 Squalane 3.0 Propylene glycol 6.0 glycerin 4.0 Triethanolamine 0.5 Xanthan Gum 0.5 Tocophenyl Acetate 0.1 Incense, preservative a very small amount Purified water To 100

Formulation Example 4 Preparation of Massage Cream

To prepare a massage cream containing phytantriol of the present invention and hexamidinediisethionate, it is combined as described in Table 9 and prepared according to a manufacturing method in a conventional cosmetic field.

Compounding ingredient Parts by weight (%) Hexamidine diethionate 0.02 Phytantriol 0.1 Propylene glycol 6.0 glycerin 4.0 Triethanolamine 0.5 Beeswax 2.0 Tocophenyl Acetate 0.1 Polysorbate 60 3.0 Sorbitan sesquioleate 2.5 Cetearyl Alcohol 2.0 Liquid paraffin 30.0 Xanthan Gum 0.5 Incense, preservative a very small amount Purified water To 100

Formulation Example 5 Pack Preparation

To prepare a pack containing the phytantriol of the present invention and hexamidine diethionate, it is combined as described in Table 10 below and prepared according to the manufacturing method in the conventional cosmetic field.

Compounding ingredient Content (% by weight) Hexamidine diethionate 0.05 Phytantriol 0.1 Propylene glycol 2.0 glycerin 4.0 Polyvinyl alcohol 10.0 ethanol 7.0 Fiji-40 Hydrogenated Castor Oil 0.8 Triethanolamine 0.3 Incense, preservative a very small amount Purified water To 100

Claims (5)

A cosmetic composition for improving acne, comprising 0.01 to 10.0% by weight of phytantriol and 0.0001 to 5.0% by weight of hexamidine diethionate, based on the total weight of the composition. delete delete The cosmetic composition for improving acne according to claim 1, wherein the phytantriol and hexamidine diethionate are contained in a weight ratio of 2: 8. According to claim 1 or 4, wherein the cosmetic composition, softening longevity, astringent longevity, nourishing longevity, eye cream, nutrition cream, massage cream, cleansing cream, cleansing foam, cleansing water, solid soap, liquid soap, powder, Essence, a cosmetic composition for improving acne, characterized in that it has a formulation selected from the group consisting of packs.