KR20040043703A - Retinoid containing chemical peeling agent - Google Patents

Abstract

PURPOSE: Provided is a retinoid-containing chemical peeling agent which improves and treats acne scars, pore expansion, skin wrinkles, skin pigmentation and the like. CONSTITUTION: A retinoid-containing chemical peeling agent is characterized by containing 1000-200000 IU, preferably 5000-150000 IU of retinoid as a peeling active material, and 0.001-10 wt.%, preferably 0.01-5 wt.% of phytic acid to alleviate stimulation and increase peeling effect.

Description

Retinoid containing chemical peeling agent

The present invention improves acne scars, enlarged pores, fine lines skin. The present invention relates to a chemical peel agent that heals and improves skin pigmentation abnormalities such as blemishes and pigmentation. Skin pigmentation disorders such as blemishes, freckles, and senile plaques are caused by abnormally activated melanin production in melanocytes, resulting in excessive production and deposition of melanin. This hyperpigmentation can be a serious mental burden from a skin cosmetic point of view and interfere with normal social activities. In ancient times, Asian women have preferred white and fair skin, which has been the standard of beauty. On the other hand, acne, acne scars, and enlarged pores of the skin are excessive sebum secretion in the sebaceous gland and mold penetrates into the pores, causing inflammation. Inflammation occurs when hyperkeratosis occurs, resulting in purulent acne, acne scars, and pores. Exaggerated skin has a hard, dull skin color that looks cosmetically bad.

Trichloroacid solution, alpha hydroxy acid (hereinafter referred to as 'AHA'), beta hydroxy acid (hereinafter referred to as 'BHA'), and zener's solution as a method for removing such pigmentation or acne scars Chemical peeler such as Jessner's solution has been used as a method of treating pigmentation and acne scars by applying it to the skin with various concentrations of aqueous solutions for a suitable time to exfoliate the stratum corneum or dissolve and remove the stratum corneum. However, these agents are dependent on pH, concentration and application time, and even at low concentrations, side effects such as erythema, burning, blisters and burns are required and require a skilled professional when used.

The present inventors stabilize the retinoid with ceramide, lecithin, resorcitin without using drugs such as AHA or BHA, and apply the drug mixed with phytic acid to the area where peeling is required to exfoliate keratin strongly and regenerate the skin. It was found to be excellent. In addition, there is no side effect such as erythema, pigmentation, tingling, etc. during the procedure or after the procedure, fine wrinkles are eliminated and spots are removed, and the invention has been invented a chemical dermabrasion composition that treats acne, pores, acne scars.

The present inventors have long been found that 1,000 to 200,000 IU, preferably retinol 5,000 to 150,000 IU and phytic acid 0.001 to 10%, preferably 0.01 to 5% of retinoids stabilized with ceramide, lecithin, resorcithin and the like When used in combination or alone, it has been invented a composition that has an excellent peeling effect and the effect of exfoliating the skin clear and transparent. The specific objects and functions of the present invention are clearly presented to those skilled in the art from the following detailed description of the invention.

Chemical peeling composition of the present invention for achieving the above object is 1,000 to 200,000 IU, preferably 5,000 to 150,000 IU retinoid, 0.001 to 10% by weight of phytic acid, preferably 0.01 to 5% by weight It is characterized by containing 1 to 100% by weight of one peel agent composition based on the total weight of the composition.

More detailed description is as follows.

The retinoid of the component used in the present invention is the main component, retinol (3,7-dimethyl-9- (2,6,6-trimethyl-1-cyclohexen-1-yl) -2,4,6 , 8-nonatetraen-1-ol), retinyl acetate, retinyl palmitate, retiic acid, retinyl oleate and the like. Among them, the most suitable component for the present invention is preferably retinol. These compounds can be used individually or in mixture of 2 or more types. The retinoid component promotes the proliferation and differentiation of the cells constituting the epidermis of the skin, thereby quickly exfoliating the skin. However, retinoids are unstable and need a way to stabilize. When the retinoid is decomposed or oxidized, the retinoid loses its original function and the function of exfoliating the skin is also lost. Therefore, retinoids have long-lasting stability of retinol when the water content is low, but the lower the water content, the lower the permeability or peeling effect of the skin, so stabilizing the retinoid in oil-in-water (O / W) type. desirable. In addition, when water is present when stabilizing the retinoid, an antioxidant should be used because the retinoid is easily oxidized.

The antioxidant used for the purpose of preventing oxidation of the retinoid in the composition is tocopherol and the amount used depends on the amount of added retinoid.

In addition, retinoids are easily decomposed by metal ions in the presence of metal ions. It is preferable to add a metal ion sequestrant as a stabilizer to prevent decomposition by such metal ions, and the metal ion sequestrant which may be used in the composition may be phytic acid, BHT, EDTA, phosphate, or the like. .

In particular, the component used in the present invention is preferably phytic acid. Phytic acid is an ingredient extracted from the eye of rice and forms the structure of inositol hexaphosphate. Phytic acid has excellent chelating ability, moisturizes skin, improves skin elasticity, eliminates irritation indicated by retinoids and increases skin peeling effect when used with retinoids.

The chemical dermabrasion composition of the present invention is used for the purpose of improving or treating skin with abnormal skin pigmentation such as acne scars, pore enlargement, fine wrinkles, blemishes, and pigmentation with clear and bright skin, and is particularly limited in its formulation. No fragrance, odor control agents, surfactants, preservative humectants, and the like may be added within a range not inhibited by dermabrasion.

When using the chemical dermabrasive of the present invention, unlike the usual method (a method of applying dermabrasion to the skin and wiping the dermabrasion after a certain period of time), the skin is washed with 3-4 days After passing, the stratum corneum of the skin is peeled off and after 7-10 days, the skin is naturally peeled off. Retinoids and phytic acid affect the dermal and basal cells of the skin epidermis, promoting the proliferation and differentiation of cells and exfoliating aged cells. As a result, acne is treated without side effects on the skin, wrinkles are improved, and skin pigmentation is treated or improved.

Hereinafter, examples and comparative examples of the present invention will be described with reference to various examples.

Prescription Examples 1-4 and Comparative Example 1

The raw materials of phases A and B in the table below are mixed uniformly and heated to 60-70 ° C., and then the two phases are emulsified. After cooling to 40 ° C., retinoid and phytic acid, flavor, preservative, and odor control agent were added and mixed in order to obtain a final product.

Unit: weight% ingredient Prescription Example 1 Prescription Example 2 Prescription Example 3 Prescription Example 4 Comparative Example 1 Retinoid - 10000IU 100000IU 200000IU - Phytic acid - - - - - A Cetostearyl alcohol 2.0 2.0 2.0 2.0 2.0 Squalene 5.0 5.0 5.0 5.0 5.0 Liquid paraffin 3.0 3.0 3.0 3.0 3.0 Polysorbate 60 2.0 2.0 2.0 2.0 2.0 Cyclomethicone 4.0 4.0 4.0 4.0 4.0 Tocopherol or tocopherol derivatives 1.0 1.0 1.0 1.0 1.0 B Purified water to 100 to 100 to 100 to 100 to 100 Collagen 0.1 0.1 0.1 0.1 0.1 Concentrated glycerin 15.0 15.0 15.0 15.0 15.0 1,3 butylene glycol 15.0 15.0 15.0 15.0 15.0 Glycolic acid - - - - 12.0 Lactic acid - - - - 12.0 Salicylic acid - - - - 12.0 Fragrance, preservative, odor control Quantity Quantity Quantity Quantity Quantity

Prescription 5-Prescription 8

It manufactured by the same method as Formulation Examples 1-4.

Unit: weight% ingredient Prescription Example 5 Prescription Example 6 Prescription Example 7 Prescription Example 8 Retinoid - 10000IU 100000IU 200000IU Phytic acid 0.1 One 3 5 A Cetostearyl alcohol 2.0 2.0 2.0 2.0 Squalene 5.0 5.0 5.0 5.0 Liquid paraffin 3.0 3.0 3.0 3.0 Polysorbate 60 2.0 2.0 2.0 2.0 Cyclomethicone 4.0 4.0 4.0 4.0 Tocopherol or tocopherol derivatives 1.0 1.0 1.0 1.0 B Purified water to 100 to 100 to 100 to 100 Collagen 0.1 0.1 0.1 0.1 Concentrated glycerin 15.0 15.0 15.0 15.0 1,3 butylene glycol 15.0 15.0 15.0 15.0 Glycolic acid - - - - Lactic acid - - - - Salicylic acid - - - - Fragrance, preservative, odor control Quantity Quantity Quantity Quantity

Experimental Example 1 Peeling Effect Experiment

① Experimental Method: The chemical peeling agent prepared by mixing Comparative Example 1 and Prescription Example 1-Prescription 8 was divided into nine groups of 90 women in their 20s and 60s, and each composition was coated with one composition. Comparative Example 1 was applied to the face of group 1 women and wiped off after 3 minutes. Prescription Example 1-Prescription Example 8 was applied to the face of each group of women, and left as it was for one day. This was done for 1 month at intervals of once / 10 days. In Comparative Example 1, severe burns or blisters may be generated if not wiped, and thus the same procedure as in actual use was made. Prescription Example 1-Preparation Example 8 was left unwashed because there is no risk of side effects. In addition, the same sunscreen of SPF30 was used to prevent skin damage and melanogenesis by UV rays during the day. The degree of peeling and the affinity of the skin for 7 days were compared.

②Comparison Method: After applying the peeling agent to the face, the area of the peeled part was compared with the total applied area in terms of percentage and the evaluation target was evaluated as an average. .

③ Peeling effect

Item Prescription Example 1 Prescription Example 2 Prescription Example 3 Prescription Example 4 Prescription Example 5 Prescription Example 6 Prescription Example 7 Prescription Example 8 Comparative Example 1 Peeling result 0% 43% 64% 78% 22% 52% 79% 81% 73%

In the above experiments, when using retinol, a peeling effect of more than 60% was obtained, and a similar effect to the existing fruit acid was obtained. Also, when the phytic acid was used in combination with the retinol, the peeling effect was slightly increased.

Experimental Example 2 Safety Confirmation Experiment on Composition of Human Skin

In order to verify the irritation of the skin that may occur in the exfoliation effect of the composition of Comparative Example 1 and Formulation Example 1-8 to the human skin, the human skin cumulative stimulation test was performed.

A total of nine 24-hour cumulative intelligence will be performed every 20 days on the upper forearm. The sphincter method was using a Finn Chamber (Finn Chamber), dropping 15μl of composition per chamber and then applying a patch, each time to calculate the degree of reaction appeared in the skin according to the following formula 3 and the results are shown in Table 2 below Averaged. At this time, if the reaction is mild, 1 point, slightly reddening only 2 points, itching, erythema is 3 points, if inflammation appears 4 points, when the average reactivity is less than 3 is determined as a safe composition.

Average Responsiveness = ((Responders * Response) / (Total Number of Subjects * Highest Score) * 100) / Total Number of Tests

Test substance Number of subjects with response Average reactivity 1 week 2 weeks 3 weeks Prescription Example 1 One - - --- --- --- --- --- --- --- --- 0.14 Prescription Example 2 3-- --- --- --- --- --- --- --- --- 0.42 Prescription Example 3 3 1- 2 1- --- --- --- --- --- --- --- 0.63 Prescription Example 4 3 2- 3 1- 2 1- 1 1- --- --- --- --- --- 1.53 Prescription Example 5 One - - --- --- --- --- --- --- --- --- 0.14 Prescription Example 6 2 - - --- --- --- --- --- --- --- --- 0.38 Prescription Example 7 2 1- --- --- --- --- --- --- --- --- 0.42 Prescription Example 8 3 1- 3-- 2 - - One - - --- --- --- --- --- 1.50 Comparative Example 1 6 2- 6 3- 5 3- 4 1- 2 - - 2 - - One - - --- --- 5.40 Inspector 20 20 20 20 20 20 20 20 20

From the results of Table 2, Comparative Example 1 containing fruit acid as a conventional peeling agent showed severe skin irritation, but the remaining compositions did not show a distinct cumulative stimulation pattern. In addition, phytic acid containing only showed a slight tendency to alleviate the stimulus.

Experimental Example 3 Measurement test of the degree of transdermal moisture loss (TEWL)

Experimental Example 1 Apply the composition of Formulation Examples 1 to 8 and Comparative Example 1 to the skin areas such as blemishes and freckles of the subjects who participated in the test, and before applying, after 5 days, 10 days, and 20 days, Tewameter TM210 (Courage + Khazaka, Germany) to improve the elasticity and wrinkles of the skin. The measurement results are shown in Table 2 below (values are average numbers of four people).

Changes in Transdermal Moisture Loss with Treatment (Unit: g / m ² h) Prescription Example 1 Prescription Example 2 Prescription Example 3 Prescription Example 4 Prescription Example 5 Prescription Example 6 Prescription Example 7 Prescription Example 8 Comparative Example 1 5 days later 28.8 27.8 24.4 23.8 25.0 22.7 22.5 20.2 32.3 10 days later 24.6 23.9 22.5 20.7 23.1 20.7 20.1 18.3 30.7 After 20 days 23.8 21.4 19.6 18.2 20.9 19.4 17.3 15.8 31.5

As a result of the above experiments, it was confirmed from the experimental results that the retinol and the phytic acid-containing composition were remarkably dropped in the loss of each layer water content.

As described above, the skin peeling agent composition comprising the retinol and the phytic acid provided by the present invention has no side effects such as erythema, pigmentation, and scars after the procedure, and the amount of moisture loss in each layer is increased to increase the elasticity of the skin, It can be seen that there is an effect of peeling the pigmented skin, such as freckles, clean and transparent.

Claims (3)

A skin dermabrasion composition containing 1,000 to 200,000 IU, preferably 5,000 to 150,000 IU, and 0.001 to 10% by weight of phytic acid, preferably 0.01 to 5% by weight, is 1 to 100 based on the total weight of the composition. A skin dermabrasion composition, characterized in that it contains by weight percent. The skin dermabrasion composition of claim 1, wherein the retinoid is retinol, retinol palmitate, retinic acid, retinyl acetate, retinyl oleate or a mixture thereof. 2. The skin dermabrasion composition of claim 1, wherein the skin dermabrasion composition is a transdermal formulation such as a pack, ointment, gel, lotion or patch.