JPH10212225A - Wrinkle preventive - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a safe wrinkle preventive, capable of maintaining a fair complexion sustainably by compounding a highly useful, specific medicine(s) showing various excellent effects, e.g. making a complexion fair and antiinflammatroy effect, so as to prevent fine wrinkles caused by changed dryness of the horny cell layer. SOLUTION: This wrinkle preventive contains kojic acid and/or its derivative as the active ingredient(s). The kojic acid useful for the present invention is pure kojic acid (5-oxy-2-oxymethyl-γ-pyrone), a fermentation solution comprising kojic acid as the major ingredient, obtained by culturing known strains capable of producing kojic acid, the concentrate of the above fermentation solution, or the kojic acid extracted from the above fermentation solution and crystallized. Content of the active ingredient is 0.001 to 10wt.% based on the whole preventive.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an anti-wrinkle agent for external use on the skin, and more particularly, it comprises kojic acid and / or a derivative thereof as an active ingredient to prevent wrinkles resulting from a change in the drying property of the stratum corneum. The present invention relates to an anti-wrinkle agent for eliminating dullness.

[0002]

2. Description of the Related Art Kojic acid and its derivatives, which have been studied by the present applicant for many years, are known as highly useful drugs having various excellent characteristics such as a whitening effect and an anti-inflammatory effect. Is disclosed, for example, in Japanese Patent Application Laid-Open No. 55-157509.
JP, JP-B-57-46825, JP-B-58-
No. 34446, JP-A-60-137253,
JP-B-60-27648, JP-B-61-1044
7, JP-A-61-143314, JP-B-6-143
JP-A-3-27322, JP-A-1-132502, JP-A-1-275524, JP-A-1-275
515, JP-A-1-275517, JP-A-3-86821, JP-B-5-30422,
It is disclosed in Japanese Patent Publication No. 6-13448.

[0003] Wrinkles are physiological changes in the skin formed by the loss of elasticity and flexibility of the skin as a result of changes in the connective tissues constituting the dermis due to aging. It is said to be a contributing factor. Therefore, blocking sunlight is a necessary condition for preventing skin aging. As a measure to prevent such a symptom, the fact is that a cosmetic product containing an ultraviolet absorber is generally applied to the skin to prevent it symptomatically. On the other hand, wrinkles generated on the face such as the outer corner of the eyes and the mouth are mainly caused by changes in the epidermis where little change in connective tissue is observed, and are caused by drying of the stratum corneum. The occurrence of fine wrinkles adversely affects the clarity of the skin and creates a dull state of the skin, and has recently been widely treated as a cosmetic problem.Preventing the fine wrinkles of epidermis reduces dullness. The development of cosmetics to be eliminated was desired.

[0004]

SUMMARY OF THE INVENTION An object of the present invention is to provide a highly safe anti-wrinkle agent which prevents wrinkles caused by a change in the dryness of the stratum corneum and eliminates dullness.

[0005]

[Means to solve the problem] Although dullness has various causes and phenomena, it is difficult to clearly define it,
(1) atrophy and poor blood circulation of capillaries on the skin surface, (2) decrease in hemoglobin in capillaries, (3) stratification and thickening of the stratum corneum, (4) deterioration of the stratum corneum accompanied by reduced gloss, ( 5) Deterioration of morphological factors due to decrease in skin firmness is considered to be related to the occurrence of dullness. The present inventors have emphasized the viewpoints (3) to (5) among these factors. That is, when the skin surface is in a dry state due to the influence of the season, environment, physical condition, and the like, it is considered that the “glossiness” decreases and a dullness is felt. In addition, when the stratum corneum is disturbed, the tension decreases and slight wrinkles occur, various irregularities are formed on the skin surface,
It is considered that the skin becomes shaded and the brightness of the skin is reduced as a result.

Accordingly, the present inventors have developed a highly safe substance which has an effect of improving not only wrinkles derived from a decrease in elasticity of the dermis but epidermal changes caused by dry skin, so-called fine wrinkles, and eliminates dullness. As a result of intensive studies to search for, the present inventors have obtained new knowledge that kojic acid and / or a derivative thereof is a material that achieves the object, and completed the present invention. That is, according to the present invention, an anti-wrinkle agent comprising kojic acid and / or a derivative thereof as an active ingredient is provided.

The kojic acid used in the present invention (5-
Oxy-2-oxymethyl-γ-pyrone) includes 5
-Oxy-2-oxymethyl-γ-pyrone pure product, fermented solution containing kojic acid as a main component obtained by culturing a known strain having kojic acid-producing ability, concentrated solution of the fermented solution, and fermentation A product obtained by extracting kojic acid from a liquid and crystallizing the same is used.

Examples of the kojic acid derivative include, for example, Japanese Patent Publication Nos. 60-10005, 1-45472, 3-74229 and 58-221.
51 JP, by coupling a saccharide to 2-position of -CH ₂ OH group of the ester compound and kojic acid kojic acid disclosed in JP-B-58-22152, koji which to stabilize the kojic acid molecule Known compounds such as acid derivatives can be used alone or in combination of two or more.

The anti-wrinkle agent of the present invention is used, for example, by directly applying it to the affected part in the form of an external use such as a cosmetic or a quasi-drug acceptable cream or emulsion. The amount of the derivative is in the range of 0.001 to 10% by weight, preferably 0.1 to 5% by weight, based on the whole preparation.

The dosage form of the anti-wrinkle agent of the present invention is not particularly limited as long as it is suitable for external application. As described above, in addition to creams and emulsions, lotions, essences, gels, pastes, and ointments And widely used in known forms, such as coating preparations such as tinctures, sprays such as aerosols and sprays, patches such as cataplasms and plasters, and baths such as bath salts. It is.

Further, when preparing the anti-wrinkle agent of the present invention, various known active ingredients usually used, for example,
Peripheral vasodilators such as vitamin E, vitamin E nicotinate, nicotinic acid, nicotinamide, benzyl nicotinate, tincture tincture, and pepper tincture, anti-inflammatory agents such as corticosteroids, ε-aminocaproic acid, lysozyme chloride, glycyrrhizin, allantoin, etc. , Placenta extract,
Liquorice extract, purple root extract, various extracts derived from animals, plants, and microorganisms such as lactic acid bacteria culture extract can be used by appropriately adding them according to the purpose at the time as long as the purpose of the present invention is not impaired. it can. Further, in addition to these known active ingredients, the anti-wrinkle agent of the present invention may further contain base ingredients such as oils and fats, and if necessary, known humectants, preservatives, antioxidants, chelating agents, pH adjusters. Various additives such as a fragrance, a coloring agent and the like can be used in combination within a range not to impair the object of the present invention.

[0012]

Next, the present invention will be described with reference to experiments and prescription examples, but these disclosures show preferred embodiments of the present invention and do not limit the present invention in any way.

<Test Example 1> Observation and measurement of skin surface by replica method a) Test method Skin with a replica score of 1 due to irradiation with ultraviolet rays (skins and crevices disappeared, exfoliation of each layer over a wide range was observed. Fifty subjects having the above condition were randomly assigned to two groups, the first group containing the cream prepared in Formulation Example 1, and the second group containing the base (the active ingredient kojic acid from the cream in Formulation Example 1). 0.3 ± 0.1 g, 2 times a day
The skin was applied every 12 hours, and the surface state of the skin at the start of the application and one week after the application was taken as a replica, and the results were observed with a stereoscopic microscope (× 20). Replicas were prepared according to the method of Kumagai et al. [SCCJ. Vol 19, no. 1 (1985)
P. According to 9 to 19], a negative replica was obtained on the skin surface using a quick-drying silicone-based synthetic rubber, and this was filled with a polysulfide-based synthetic rubber to obtain a positive replica. In addition, the skin of the subject was visually inspected, and the degree of dullness of the skin was also evaluated.

B) Test Results In comparison with the determination of the replica of the skin surface before the use of the cream, the skin to which the cream of the present invention was applied showed a marked improvement in the surface condition of the skin. Table 1 shows the results.

[0015]

<Evaluation Classification of Skin Surface Condition> Evaluation 1: Disappearance of crevices / contuses and exfoliation of a wide range of stratum corneum are recognized. As a result of observation of the skin surface, dullness was severe. Evaluation 2: The skin sulcus / skin is unclear, and exfoliation of the stratum corneum is recognized. As a result of observation of the skin surface, it is quite dull. Evaluation 3: Although skin clefts and crusts are recognized, they are flat and flow in one direction. As a result of observation of the skin surface, it was slightly dull. Evaluation 4: The skin sulcus / skin is clear. As a result of observation of the skin surface, almost no dullness is felt. Evaluation 5: The skin sulcus and skin hills are clear and arranged in a mesh form. As a result of observing the skin surface, there is no dullness and a transparent feeling is felt. As is clear from the above results, it was proved that kojic acid has an excellent dulling prevention effect.

<Test Example 2> Improvement effect of wrinkles by the half-face method a) Test method The essence of the present invention (Prescription Example 9) was applied to 30 women (3
3 to 55 years old), apply it continuously to the face twice a day in the morning and evening.
A month later, the degree of improvement of fine wrinkles was examined. The application of the face
The evaluation was performed by applying the essence of the present invention to one side and the other side containing no kojic acid (control only) as a control.

B) Test Results As a result of judging the degree of improvement of fine wrinkles before use of the essence, a clear effect of improving fine wrinkles was recognized in the essence of the present invention. No skin abnormalities due to continuous use were observed. Table 2 shows the results. As is clear from the following results, it was proved that kojic acid had an excellent effect of improving fine wrinkles.

[0019]

[0020]

[Formulation Examples] Formulation examples of the anti-wrinkle agent of the present invention are shown below. In the formulation examples, “appropriate amount” means a ratio of 100% by weight in the entire formulation. <Formulation Example 1> Cream (1) (% by weight) 1. Kojic acid 1.00 2. Aqueous sodium hyaluronate solution 2.00 Polyethylene glycol 400 3.00 4. 4. Polyoxyethylene cetyl ether (25EO) 5.00 Stearic acid 5.00 6. Avocado oil 1.00 7. 7. Almond oil 10.00 8. dl-pyrrolidone carboxylate sodium solution 5.00 Paraoxybenzoic acid ester 0.20 10. 10. Disodium edetate 0.01 Purified water qs

<Formulation Example 2> Cream (2) (% by weight) Kojic acid 5.00 2.4-tert-butyl-4'-methoxy-dibenzoylmethane 1.50 3. Jojoba alcohol 1.00 4.1 1,3-butylene glycol 0.50 5. 5. Dimethylsiloxane / methyl 3.00 (polyoxyethylene / polyoxypropylene copolymer) Jojoba oil 7.00 7. 7. Decamethylcyclopentanesiloxane 3.00 Octamethylcyclotetrasiloxane 3.00 9. Dimethylpolysiloxane 5.00 10. 11. Sodium ascorbate 0.04 11.1% aqueous solution of sodium hyaluronate 2.00 Disodium edetate 0.01 13. Purified water qs

<Formulation Example 3> Emulsion (1) (% by weight) Kojic acid 4.00 2. 2. Octyldodecanol 3.00 Polyoxyethylene cetyl ether (25EO) 0.50 4. 4. Polyoxyethylene oleyl ether (20EO) 1.00 Stearic acid 0.50 6. Shea butter 0.50 7. 7. Avocado oil 4.00 8. paraoxybenzoate 0.20 Quinseed extract 5.00 10. Xanthan gum 0.14 11. 11. Disodium edetate 0.01 Purified water qs

<Formulation Example 4> Emulsion (2) (% by weight) Kojic acid 0.50 2. 2. ethylene glycol salicylate 0.10 3. Bacyl alcohol 3.50 4. Ascorbic acid 2.00 5. Coconut oil fatty acid monoethanolamine 2.00 Stearic acid 0.50 7. 7. myristic acid 0.50 Avocado oil 4.00 9. Fine particle titanium oxide 0.04 10. Paraoxybenzoate 0.20 11. Sodium hyaluronate 5.00 12. Ougon extract 0.14 13. 13. Disodium edetate 0.01 Purified water qs

<Formulation Example 5> Lotion (% by weight) Kojic acid glucoside 7.00 2. 2. 2-Ethylhexyl paramethoxycinnamate 2.00 3. ethylene glycol ethyl ether 3.00 4. Polyoxyethylene cetyl ether (60EO) 5.00 Cucumber extract 2.00 6. Time extract 0.50 7. 7. Paraoxybenzoic acid ester 0.10 8. Ascorbic acid 0.10 10. Sodium citrate 0.30 10.5% elastin hydrolyzate 4.00 11. Disodium edetate 0.01 Purified water qs

<Formulation Example 6> Cream pack (% by weight) 1. Ethyl kojate 2.00 2. Kojic acid 1.00 Polyethylene glycol 1500 5.00 4. 4. Stearic acid diethanolamide 5.00 Stearic acid 0.50 6. Myristic acid 15.00 7. Coconut oil 0.04 8. 8. Sunflower oil 0.20 Paraoxybenzoic acid ester 5.00 10. 10. Disodium edetate 0.01 Purified water qs

<Formulation Example 7> Ointment (% by weight) 1. Kojic acid 1.00 2. Phenyl salicylate 1.50 3. Sodium hydroxymethoxybenzophenone sulfonate 1.00 4. Isoamyl octyl gallate 2.00 5. Palm oil fatty acid monoethanolamide 5.00 Vaseline 10.00 7. 7. Stearic acid 5.00 Oleic acid 1.00 9. Olive oil 10.00 10. Paraoxybenzoate 0.20 11. Carrageenan 5.00 12. Disodium edetate 0.01 13. Purified water qs

<Formulation Example 8> Poultice (% by weight) 1. Kojic acid fructoside 0.50 Loquat leaf extract 2.00 3. 3. stearic acid diethanolamide 3.00 Polyacrylic acid 27.00 5. Liquiritin 0.10 6. Ougon extract 0.05 7. 7. Disodium edetate 0.05 7. Sodium polyacrylate 7.00 Aluminum chloride 0.30 10. Concentrated glycerin 20.00 11. Titanium oxide 4.00 12. Purified water qs

<Prescription Example 9> Essence (% by weight) 1. Kojic acid 1.00 2. Urocanic acid 0.50 Isopropanol 0.50 4. Benzyl alcohol 0.05 5. Kefiran aqueous solution 1.50 6. 6. Palm oil aliphatic monoethanolamide 2.00 Stearic acid 0.50 8. Linolenic acid 0.50 9. Avocado oil 2.00 10. Turtle oil 3.00 11. Liver extract 0.04 12. 13. Paraoxybenzoate 0.20 13.1% Carboxyvinyl polymer aqueous solution 5.00 Placenta extract 0.14 15. Disodium edetate 0.01 16. Appropriate amount of purified water It was confirmed that each of the above Formulation Examples 1 to 9 was a formulation having an effect satisfactory for the purpose of the present invention, as shown in the table.

[0029]

According to the present invention, there is provided an anti-wrinkle agent containing kojic acid and / or a derivative thereof. The anti-wrinkle agent prevents fine wrinkles resulting from a change in the drying property of the stratum corneum. It is a highly safe cosmetic that can continuously maintain skin clarity.

Claims (1)

[Claims] 1. An anti-wrinkle agent comprising kojic acid and / or a derivative thereof as an active ingredient.