KR101654225B1 - Composition for prevention and treatment of pimples comprising complex salt of baicalin and zinc - Google Patents

Abstract

The present invention relates to a composition for external application for skin having excellent sebum secretion inhibitory effect, improvement of shine on the skin and prevention of acne, comprising baicalin-zinc complex as an active ingredient. The baicalin- It is possible to develop a more effective external preparation for skin because of its excellent effect of inhibiting, improving the shine of skin, preventing and treating acne.

Description

Technical Field [0001] The present invention relates to a composition for improving acne skin, comprising baicalin-zinc complex,

The present invention relates to a composition for improving skin comprising baicalin-zinc complex. More specifically, the present invention relates to a composition for inhibiting sebum secretion including baicalin-zinc complex, an improvement effect on shine of skin, The present invention relates to a composition for improving skin.

Generally, sebaceous glands in the skin, including the scalp and face, play a role in preventing moisturization and invasion of microorganisms. However, excessive secretion of sebum is caused by shine of skin, lifting of makeup, enlargement of pores, And promotes the production of acne. Several causes are involved in the excessive secretion of sebum, among which the cause of activation of sebaceous cells by the action of hormones is known to be the most important factor. Traditionally, female hormones such as estrogen have been used to treat sebaceous hypertension and acne caused by male hormones. However, they are currently being discontinued due to skin inflammation and hormone administration, or they are used in extremely low doses. Also, in the field of cosmetics, the excessive secretion of sebum is a matter of great interest as a cause of expulsion of make-up and enlargement of pores, but the research is insufficient. Currently, the method of inhibiting sebum secretion in cosmetics utilizes a porous powder that temporarily adsorbs sebum or an extract known to inhibit sebum, but its effect is insignificant because its active ingredient content is very small .

On the other hand, the peroxisome proliferator activated receptor (PPAR) is a known class of nuclear hormone receptors with three subtypes of alpha, beta / delta, gamma of various histological distributions. The peroxisome proliferator activated receptor subtype (hereinafter referred to as 'PPAR-alpha') is initially identified by the action of a peroxisome proliferator, such as a derivative of the fibrinic acid, (Issemann and Green, Nature, 1990, 347: 645-650). Also, an important role of fatty acids in tissues performed by PPAR-a has been demonstrated in the literature (Leone et al., Proc. Natl. Acad. Sci., USA, 1999, 96: 7473-7478). Lipid activators of PPAR-a, such as linoleic acid, are known in the art. They have been shown to promote the formation of in vitro skin epithelial barrier (Hanley et al., J. Clin. Inv., 1977, 100: 705-712). In addition, activators of PPAR-gamma have recently been shown to reduce the amount of glucose and insulin as well as to increase insulin sensitivity in animal experiments, suggesting potential as a therapeutic agent for diabetes and some complications thereof (Ricote M. et < RTI ID = 0.0 > , Nature, 1998,391: 79-82). In addition, PPAR-γ has been reported to affect the maturation of sebocytes in the sebaceous glands (Kuenzli et al., British J. Derm., 2003, 149: 229-236) , And there are few examples using this in the art. WO2003 / 068205 mentions a food which can prevent metabolic diseases such as hypertension and cholesterol by PPAR-alpha and PPAR-y agonist, but the mention of PPAR-gamma inactivation agent And the use of the composition is limited to metabolic diseases.

In order to solve such skin problems, many cosmetic products using natural products have been developed to reduce skin irritation caused by various chemical substances and the like. In addition to low adverse effects on skin, natural materials have recently become increasingly appreciated as a cosmetic raw material as consumers' response to cosmetics using natural materials has increased. Accordingly, Korean Patent Registration No. 10-1211754 discloses a cosmetic composition which is effective for prevention or treatment of acne due to stress by containing, as an active ingredient, a complex extract or a compacted extract comprising gold, licorice, persimmon, horse rid, Lt; / RTI >

Since the gold used in Korean Patent Registration No. 10-1211754 shows a low level of the effect on the prevention or treatment of direct acne due to the nature of the natural product, the use of the effective ingredient of Baikalin in the prevention and treatment of acne Studies have been actively carried out to develop a pharmaceutical preparation, but the above-mentioned baicalin is also somewhat deficient in the prevention or treatment of acne, and thus it is desired to develop a derivative which is effective for the prevention or treatment of acne, Research is underway, but no results have yet been reported.

Under these circumstances, the inventors of the present invention have made extensive efforts to develop a bicalin derivative which is more effective in the prevention or treatment of acne. As a result, it has been found that bicalin- The present invention has been accomplished on the basis of these findings.

Accordingly, it is an object of the present invention to provide a composition for improving skin, which has an effect of inhibiting sebum secretion including baicalin-zinc complex, an improvement effect on skin shine, and an effect of preventing and treating acne.

According to an aspect of the present invention,

The present invention provides a composition for cosmetics which is excellent in sebum secretion inhibiting effect, which contains baicalin-zinc complex as an active ingredient, an improvement effect on skin shine, and an acne prevention effect.

In the cosmetic composition according to the present invention, 0.05 to 5.0% by weight of the above-mentioned active ingredient baicalin-zinc complex salt may be contained.

According to another aspect of the present invention,

The present invention provides a pharmaceutical composition for topical application to skin, which has an effect of inhibiting sebum secretion containing BaCalumin-zinc complex as an active ingredient, an improvement effect on skin shine, and an effect of preventing and treating acne.

In the pharmaceutical composition for external application for skin according to the present invention, the active ingredient, bicalin-zinc complex, may be contained in an amount of 0.05 to 5.0% by weight.

The baicalin-zinc complex salt of the present invention is effective in inhibiting sebum secretion, improving the shine of skin, preventing and treating acne, and developing a more effective external skin preparation.

Fig. 1 is a view showing the result of evaluation analysis by inflammatory acne counting. Fig.
2 is a view showing the results of skin erythema analysis using the principle of absorption.
FIG. 3 is a diagram showing the results of the questionnaire evaluation analysis on efficacy.

Hereinafter, the present invention will be described in detail.

The present invention relates to a composition for improving skin comprising baicalin-zinc complex. More specifically, the present invention relates to a composition for inhibiting sebum secretion including baicalin-zinc complex, an improvement effect on shine of skin, The composition of the present invention preferably contains, as an active ingredient, a bocalin-zinc complex in an amount of 0.05 to 5.0% by weight based on the entire composition for external application for skin, When the content is less than 0.05% by weight, the effect of improving the skin hardly occurs. When the content is more than 5.0% by weight, the effect of increasing the content is insignificant, which is not economical.

The composition for external application for skin of the present invention may be selected from cosmetics, gels, water-soluble liquids, creams, essences, liquid preparations, ointments, patches, oil-in-water (O / W) And the composition for external application for skin of the present invention may be a cosmetic composition or a composition for external application to skin.

The composition according to the present invention may further contain additives such as a stabilizer, a dissolution aid, an auxiliary agent such as a transdermal absorption promoter, a fragrance, and an antiseptic to prepare a composition for external application for skin.

Hereinafter, the present invention will be described in detail with reference to examples. It is apparent that the scope of protection of the present invention is not limited to the following examples.

≪ Example: Preparation of Baikalin-zinc complex >

100 g of zinc acetate was added to 3 kg of purified water and stirred to completely dissolve. Then, 100 g of bicalin of the following formula 1 was slowly added thereto, and the reaction solution was washed five times with 3 kg of purified water and dried overnight at 45 ° C, 2 < / RTI >

≪ Formula 1 >

(2)

≪ Example: Test for improving acne in baicalin-zinc complex salt >

1. Test products

1-1. Product features : Serum

1-2. Active ingredient : 0.5% by weight of baicalin-zinc complex

1-3 How to use the product : Twice a day (morning / evening), after cleansing, it is pumped 2 ~ 3 times on the face and applied as a whole.

2. Test method

This test was conducted by examining history and skin condition, and using more than 20 female subjects suitable for the test purpose according to the method of use. Subjects were asked to take the test after taking 20 minutes of stabilization under the condition of constant temperature and humidity (22 ㅁ 2 ℃, 50 ㅁ 5%) after washing with the designated cleanser.

2-1. Subject selection

Subjects in this study selected 20 or more subjects aged 18 or older who had inflammatory acne on their face.

2-1-1. Subject selection criteria

Applicants who meet the conditions described below were selected as test subjects.

① An adult female aged 18 to 55 years or older who has at least one inflammatory acne on the face as judged by the state investigator

② Applicants who voluntarily signed a written agreement before he / she has fully explained the purpose and contents of the examination prior to the examination

③ Those who can follow up during the test period

2-1-2. Subject exclusion criteria

Applicants who fall under the following categories are excluded from the test subjects.

① If you plan to become pregnant during pregnancy, lactation or within 3 months

② When skin mold containing steroid is used for more than 1 month for treatment of skin disease

③ If one month has not elapsed after participating in the same test

④ If you have sensitive or irritable skin

⑤ If there is skin abnormalities such as erythema and capillary dilatation on the test site

⑥ If the same or similar cosmetics or medicines are used in the test site within 3 months of the start of the test

⑦ In the case of chronic wasting disease (asthma, diabetes, hypertension, etc.)

⑧ If the follow-up is difficult during the test period

⑨ If it is determined that the test is difficult due to the judgment of the other state tester

2-1-3. Limitations

The subjects were prohibited from mixing with functional cosmetics or drugs other than the test product.

2-1-4. Number of Subjects and Basis

The number of subjects was 20 or more according to the Guideline for Evaluation of Functional Cosmetics (2003, 2005), Cosmetics Labeling and Test Method Guideline for Advertising Demonstration (2013).

2-2. Evaluation by Inflammatory Acne Coefficient

Before and after 2 weeks and 4 weeks of use, facial papules and pustules were counted independently by two testers at a constant illumination and angle, and the counting criteria of the lesions were shown in Table 1 below (Table 1, Criteria of lesion counting ).

Lesion Criteria description Papules A lesion with a size of 0.1-0.5 cm is accompanied by redness or swelling Pastules 0.1 to 0.5 cm in size with peaks at the apex of the papule

2-3. Measurement of skin erythema using absorption principle

Skin erythema is Mexameter  MX 18 (C + K, Germany). This is a device for measuring the amount of melanin and hemoglobin, which are the main factors for determining skin color, by using the principle of absorption. In the probe, there are an emitter emitting three wavelengths of light and a receptor receiving light reflected by the object. Emit a certain amount of light from the emitter, and detect the amount of light reflected from the skin in the receiver to calculate the amount of light absorbed by the skin. The skin erythema digitizes and displays the absorption rate of hemoglobin in the wavelength range excluding the absorption peak and the interference of other pigments such as bilirubin.

In this study, one papule accompanied by redness on the face was selected and measured three times in total, and the mean value was analyzed.

2-4. Questionnaire evaluation by subjects

The efficacy questionnaire was used to ask the subjects directly to the questionnaire on the 5-point scale (1, not at all; ~ 5, very similar) at 2 weeks and 4 weeks after the use and analyzed the positive answers (choices 4 and 5) .

2-5. Skin safety evaluation

Subjective skin irritation and objective skin irritation were assessed at 2 weeks and 4 weeks after the use of the product by observing and interviewing the tester.

2-6. Statistical analysis

Statistical significance of all data was analyzed using SPSS  Package Program (IBM, USA). The normality test was verified by Shapiro-Wilks test or kurtosis and skewness, and RM ANOVA was used for the parameters and Wilcoxon signed-ranks test was used for the non-parametric tests. When the intraclass correlation coefficient (ICC) value was 0.8 or more, the reliability of the test was evaluated and the mean value was applied. Statistical significance was set to p value less than 0.05 increase and decrease rate was calculated according to the following equation.

<Calculation formula of increase / decrease rate>

(%) = (Measured value before using the product - Measured value after using the product) / Measured value before using the product x 100

3. Test result

3-1. Subject skin characteristics

Twenty-six female subjects aged 20 to 51 years (mean age: 28.6 ㅁ 9.09 years) who participated in the exclusion and selection criteria participated in the study, but one person disappeared (# 06, protocol failure) Respectively. The skin characteristics of the subjects participating in the test were analyzed and classified into the following Tables 2, 3 and 4.

Item Classification Frequency (n) Percentage (%) Skin type
(Skin type) Dry 7 28.00 Normal 6 24.00 Oily One  4.00 Dry and oily 9 36.00 Problematic skin (Problematic) 2  8.00 moisture
(Hydration) Sufficient 0  0.00 Normal 16 64.00 Deficient 9 36.00 Oil
(Sebum) Glossy 6 24.00 Normal 17 68.00 Deficient 2  8.00 Surface condition
(Surface) Smooth 4 16.00 Normal 17 68.00 Rough 4 16.00 Skin thickness
(Thickness) Thin 5 20.00 Normal 11 44.00 Thick 9 36.00 UV exposure time
(Duration of UV-exposure) Within 1 hour (Less than 1hr) 4 16.00 1-3 hours (1-3 hrs) 16 64.00 More than 3hrs 5 20.00 Sleep time
(Sleeping hours) Within 5 hours (Less than 5hrs) One  4.00 5 to 8 hours (5 to 8 hrs) 23 92.00 More than 8hrs One 4.00 Stimulation sensitivity
(Irritability) Yes (Yes) 7 28.00 No 18 72.00 Stimulation sensitivity
Reason of
Irritability) Cosmetics, food, medicine
(Cosmetics, food, medicine) 5 20.00 Climate One 4.00 Sunlight 0 0.00 Other (Etc) One 4.00 Sting sensitivity
(Stinging) Yes (Yes) 0 0.00 No 25 100.00 Adverse experience
(Adverse reactions) Yes (Yes) 0 0.00 No 25 100.00

Item Classification Frequency
(N) Percentage (%) When acne occurs
(Onset age) Elementary School
(At elementary school) 7 28.00 middle School
(At middle school) 9 36.00 high school
(At high school) 5 20.00 After graduating high school
(After graduation high school) 4 16.00 Family history of acne
(Family history) None 3 12.00 Parents 3 12.00 Brother 17 68.00 Parents and siblings (All including parents and brother) 2 8.00 Severe acne
(Severe site) Foreheads 2 8.00 Cheeks 15 60.00 Nose 2 8 Jaw 6 24.00 Neck 0 0.00 Body 0 0.00 Acne related
Interest
(Interest with acne) Acne 2 8.00 Skin surface roughness
(Roughness of skin surface) 7 28.00 Skin color (signs of acne, pigmentation) (Skin color such as PIH ¹ ) 9 36.00 Enlarged pore 7 28.00 Oiliness 0 0.00 Skin scale 0 0.00 Acne and
Relationship of Stress
(Influence of stress on acne skin) Yes (worse) (Yes) 12 91.30 No (Not relevant) (No) 13 48.00 Acne and
Physiological relationship
(Relation between acne and menstruation cycle) None 8 32.00 Deterioration just before menstruation
(Before menstruation) 14 56.00 Worse during menstruation
(During menstruation) One 4.00 Deterioration immediately after menstruation
(After menstruation) 2 8.00 During the day
Number of cleansing
(Washing time
a day) Hardly ever wash 0 0.00 1-2 times (1-2 times) 21 84.00 3-4 times (3-4 times) 4 16.00 More than 5 times (Above 5 times) 0 0.00 ¹ Post-inflammatory hyperpigmentation

Item Classification Frequency
(N) Percentage (%) Basic cosmetics in use
(Skin-care cosmetics) Almost never
(Hardly ever use) One 4.00 General Basics Products
(Products for normal skin) 23 92.00 Acne Products
(Product for acne skin) One 4.00 Cleaner in use
(Cleanser) Cleanse with water only
(With water, no cleanser) One 4.00 General Soap (Soup) 2 8.00 General cleanser
(Cleanser for normal skin) 20 80.00 Acne cleanser
(Cleanser for acne skin) 2 8.00 Stress about acne Yes (Yes) 12 48.00 No 13 52.00 Stress due to acne No (No) 12 48.00

3-2. Assessment analysis by inflammatory acne factor

The results are shown in Table 5 and FIG. 1, and the results showed that papules and pustules were significantly decreased ( p <0.05), and the improvement rate of papules Were 24.15%, 30.81%, and pustule was 71.13% and 60.82%, respectively.

Parameter Week N Mean ¹ SD SEM p-value Decrement (%) Papules Before 25 13.50 9.48 1.90 - - 2W 25 10.24 7.34 1.47 0.010 * 24.15 ▼ 4W 25 9.34 7.30 1.46 0.000 * 30.81 ▼ Pustules

Before 25 1.94 2.94 0.59 - - 2W 25 0.56 1.19 0.24 0.013 * 71.13 ▼ 4W 25 0.76 1.74 0.35 0.030 * 60.82 ▼ ¹ Decrease of the mean value represents reduction of papule and pustule number (▼).
* Significantly different at p <0.05 compared with before treatment.

3-3. Analysis of skin erythema using absorption principle

The results are shown in Table 6 and FIG. 2, and the results showed that the erythema decreased significantly ( p <0.05), and the improvement rate 12.20% and 16.19%, respectively.

Week N Mean ¹ SD SEM p-value Decrement (%) Before 25 389.39 83.85 16.77 - - 2W 25 341.87 78.22 15.64 0.000 * 12.20 ▼ 4W 25 326.33 97.88 19.58 0.001 * 16.19 ▼ ¹ Decrease of the mean value represents reduction of papule and pustule number (▼).
* Significantly different at p <0.05 compared with before treatment.

3-4. Analysis of questionnaire evaluation by subjects

3-4-1. Assessment of efficacy questionnaire

The results of the efficacy questionnaire were analyzed and the results are shown in Table 7 and FIG. 3. The results are as follows. At the 2nd week after use, 'sebum reduction', 'reduction of shine', 'reduction of inflammatory acne' 44% ~ 48% of the subjects in the overall improvement section showed a decrease in sebum reduction, reduction of shine, reduction of inflammatory acne, reduction of new acne production, improvement of existing acne, Approximately 52% ~ 68% of the respondents answered positively in the overall improvement.

Item 2W 4W N ¹ % ² N ¹ % ² Decrease of sebum 11 44.00 15 60.00 Reduce shine
(Decrease of grease) 11 44.00 14 56.00 Inflammatory acne reduction
(Decrease of inflammatory lesions) 12 48.00 17 68.00 Reduces the generation of new acne
(Decrease of novel acne production) 9 36.00 13 52.00 Improve existing acne
(Improvement of existing acne) 11 44.00 17 68.00 Overall improvement
(Improvement of overall acne) 11 44.00 15 60.00 ¹ Frequency (N): The number of positive answers (4, Agree ~ 5, Strongly agree)
² Percentage (%) = Number of positive answers / Total number of subjects (25) x 100

3-5. Skin safety evaluation analysis

The results of the skin stability evaluation analysis are shown in Table 8, and no abnormal reaction was observed in all subjects in Table 8.

Symptom 2W 4W Subjective stimulation
(Subjective irritation) Itching 0 0 Stinging like a needle piercing 0 0 Burning 0 0 Prickling 0 0 Stiffness 0 0 Tightness 0 0 Burning of eyes 0 0 Weeping 0 0 Other (etc.) 0 0 Objective stimulus
(Objective irritation) Redness 0 0 Edema 0 0 Desquamation 0 0 Other (etc.) 0 0 Number of total abnormal responders 0 0

4. Summary of results

1) Assessment analysis by inflammatory acne counting

The rates of papules and pustules were significantly decreased ( p <0.05) at 2 weeks and 4 weeks after the use of the product compared with before use. The rates of improvement of papules were 24.15%, 30.81%, pustules 71.13% and 60.82%, respectively.

2) Analysis of skin erythema using absorption principle

At 2 weeks and 4 weeks after use, the erythema was significantly decreased ( p <0.05) and the improvement rates were 12.20% and 16.19%, respectively.

3) Questionnaire evaluation analysis by subject

The results of the efficacy questionnaire evaluation showed that 44% ~ 48% of the subjects in the item 'Reduce sebum reduction', 'Reduce shine', 'Reduce inflammatory acne', 'Improve existing acne' Approximately 52% ~ 68% of the subjects were positive in terms of "Reduce sebum," "Reduce inflammation," "Reduce inflammation acne," "Reduce new acne formation," "Improve existing acne, Respectively.

4) Skin safety evaluation analysis

No adverse events were observed in all subjects during the study period.

Claims (4)

A composition for cosmetics which is excellent in suppressing the secretion of sebum, containing the baicalin-zinc complex as an active ingredient, improving the skin against shine, and preventing acne. The cosmetic composition according to any one of claims 1 to 3, which comprises 0.05 to 5.0% by weight of the active ingredient baicalin-zinc complex salt. A pharmaceutical composition for external application for skin, which has an effect of suppressing the secretion of sebum comprising the baicalin-zinc complex as an active ingredient, an improvement effect on skin shine, and an effect of preventing and treating acne. 4. The composition for external application for skin according to claim 3, wherein the active ingredient is comprised of 0.05 to 5.0% by weight of bicalyin-zinc complex salt.

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