JPH07242526A - Cosmetic - Google Patents

Abstract

PURPOSE:To obtain a cosmetic containing a specific lactone compound as an active component, having safe and excellent chapped skin prevention effect, cuticle improving effect, aging preventing effect and skin-beautifying effect, effective for promoting the proliferation of fibroblast cell and having high safety. CONSTITUTION:This cosmetic contains a lactone compound of formula I {(q) is group of formula II [R1, R2, R1' and R2' each is H, OR5 [R5 is H or OR6 (R6 is H, an alkyl or an acyl)], methyl or acetyl]; (n1) is l-4; (n3) is 0-4; R3 is H or group of formula III [A is H, CH2OR5, CHO or COOR7 (R7 is H or an alkyl); R4 is same as R5; (n2) is 0-5]} as an active component. The especially preferable lactone compounds are D-glucurono-6,3-lactone, alpha-D- glucoheptonic-gamma-lactone, delta-glucurolactone, alpha, beta-glucooctonic-gamma-lactone, L-gulonic-gamma- lactone, gamma-D-galactonolactone, D-saccharic-1,4-lactone, D-saccharic-3,6-lactone, etc.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a cosmetic which is safe and has an excellent effect of preventing rough skin, an effect of improving keratin, an effect of preventing aging and an effect of beautiful skin.
The present invention relates to an excellent cosmetic having a fibroblast proliferation promoting action and high safety.

[0002]

2. Description of the Related Art Wrinkles and tarmi are typical changes in skin aging, and become one of the most important cosmetic problems especially for women as the age increases. However, contrary to people's interest, at present, there is no definitive means to treat wrinkles and tarmi.

The development of wrinkles and tarmi occurs in connective tissue fibers of the dermis, and its main constituents are fibroblasts and extracellular matrix. The extracellular matrix consists of fibrous proteins such as collagen and elastin and amorphous components such as glucosaminoglycan and hyaluronic acid.
Since their formation is synthesized and decomposed by fibroblasts, they are greatly influenced by the proliferation and activity of the cells.

[0004] However, although the development of the cosmetics having a high activity of promoting the proliferation of fibroblasts and having a high safety has been delayed, a sufficiently excellent product has not been obtained yet.

[0005]

SUMMARY OF THE INVENTION In view of the current state of the art in the cosmetics industry, the present invention has been made for the purpose of newly developing the above-mentioned cosmetics, which are highly anticipated in the industry.

[0006]

The present invention has been made to achieve the above object.

[0007] In order to achieve the above-mentioned object, various investigations were conducted, focusing on the fact that lactone compounds have activity in cells, and as a result of searching various lactone compounds, it was found that the lactone compounds have a remarkable cell activating effect. I have found

The use of a lactone compound activates fibroblasts, promotes the production of extracellular matrix such as collagen, elastin, hyaluronic acid, etc., and promotes the firmness of the skin, and reduces wrinkles and tarmi. The present inventors have found that they can be prevented, and completed the present invention. Hereinafter, the present invention will be described in detail.

The active ingredient used in the present invention is a lactone compound having the general formula (I) shown below. In the present invention, one kind or two or more kinds of all compounds can be used as long as they are lactone compounds having the general formula (I). The representative compounds are exemplified below.

[0010]

[Chemical 2]

D-glucurono-6,3-lactone, α-
D-glucoheptonic-γ-lactone, δ-glucuronolactone, α, β-glucooctonic-γ-lactone, L-glonic-γ-lactone, γ-D-galactolactone, D-saccharic-1, 4-lactone, D
-Saccharic-3,6-lactone, D-(+)-ribonic-γ-lactone, α-butyrolactone, γ-butyrolactone, α-octanoic lactone, γ-octanoic lactone, nonanoic lactone, γ-valero Lactone, D-mannoic-δ-lactone, D-xyloic-δ-lactone, D-arabinoic-δ-lactone, stearoyl-δ-gluconolactone, D / L
-Pantolactone, palmitoyl-D / L-pantolactone.

To prepare the cosmetics according to the present invention, an ointment is prepared according to a conventional method for preparing cosmetics or external preparations, using a cosmetic or external preparation base which contains the compound of the present invention as an active ingredient.
It may be formulated into a cream, a liquid agent, an emulsion, and other dosage forms. Furthermore, the present invention broadly includes cosmetics containing the lactone compound having the general formula (I) as an active ingredient, and is not limited by the base or the like used.

The compound used in the present invention has extremely low toxicity, as will be apparent from the following description. Therefore, when preparing the cosmetic composition of the present invention, the amount of the active ingredient to be added is not particularly limited. Usually, it is preferable to add the lactone compound in an amount of 0.1 to 20%. Preferably, it is 3 to 10%. The usage is not different from the usual cosmetics, and in general, it may be applied to the intended place 1 to 3 times a day. With such usage, the effect is sufficiently exerted, and no side effect or toxicity is observed.

Next, the results of acute toxicity tests carried out on typical lactone compounds according to the present invention are shown in Tables 1, 2 and 3 below. The test was performed by oral administration using mice or rats (Compounds 1-5, 14-16).

[0015]

[Table 1]

[0016]

[Table 2]

[0017]

[Table 3]

As is clear from the above results, the compound used in the present invention was found to have extremely low toxicity and excellent safety.

Next, the action and effects of the typical active ingredient compounds according to the present invention will be described in detail with reference to test examples.

[0020]

[Test example]

 Fibroblast proliferation promoting action of lactone compounds

Human fibroblasts were added to Dulbecco's
8 × 10 ³ cells are seeded on a 3.83 cm ² plastic plate containing 1.0 ml of MEM medium (containing 10% FBS), and cultured at 37 ° C. under 5% carbon dioxide gas. After 5 days, the medium was exchanged and the final concentration of the lactone compound below was changed to
0.005%, 0.001%, 0.0001% respectively
0.1 ml of MEM medium adjusted to
Incubate at 37 ° C. under 5% carbon dioxide gas for 3 days.

The cell growth promoting effect was obtained by measuring the number of cells grown after culturing and using 3 wells for each concentration of one test substance. As a control, a medium supplemented with a medium instead of the test substance was cultured under the same conditions, and the results were expressed as a growth rate relative to the control. The growth rate (%) was expressed as the growth rate when the control was 100. The results are shown in Tables 4 and 5 below.

[0023]

[Table 4]

[0024]

[Table 5]

As described above, all the active ingredient compounds according to the present invention were found to have a strong fibroblast proliferation promoting effect. A prescription example is shown below.

[0026]

[Prescription example 1] Prescription compounding amount (wt%) 1 ethanol 5.0 2 vegetable oil 0.1 3 polyoxyethylene hydrogenated castor oil 0.5 4 D-glucuronic acid lactone 10.0 5 propylene glycol 5.0 6 pantetheine- S-calcium sulfonate 2.0 7 Preservative, fragrance Suitable amount 8 Purified water Total amount 100.0

1 to 4 are dissolved, and this is added to a solution of 5 to 8 and dissolved to obtain an aqueous solution type cosmetic.

[0028]

[Prescription example 2] Prescription compounded amount (% by weight) 1 Vaseline 2.5 2 Liquid paraffin 10.0 3 Cetostearyl alcohol 12.0 4 Polyoxyethylene sorbitan monostearate 7.0 5 Sorbitan monostearate 1.0 6 α, β-Gluococtonic-γ-lactone 2.07 Propylene glycol 5.08 Thiotaurine 1.09 Preservatives, flavors Suitable amount 10 Purified water Total amount 100.0

The oil layers 1 to 6 and the water layers 7 to 10 are respectively heated to 75 ° C. and mixed and emulsified. This is cooled to 30 ° C. to obtain a cream type cosmetic.

[0030]

[Prescription example 3: lotion] Prescription compounding amount (% by weight) 1 ethanol 5.0 2 methyl p-oxybenzoate 0.1 3 polyoxyethylene (40) hydrogenated castor oil 0.1 4 perfume 10.0 5 refining Water 5.0 6 γ-Galactonolactone 5.0 7 Palmitoyl Hypotaurine Sodium 2.0 8 1,3-Butylene Glycol 3.0 9 Glycerin 2.0 10 Xanthan Gum 0.02 11 Purified Water 77.7

Components 1 to 7 and components 8 to 11 are uniformly dissolved, mixed and filtered to obtain a product.

[0032]

[Formulation Example 4: Cream] Prescription Formulation amount (% by weight) 1 Stearic acid 2.0 2 Stearyl alcohol 2.0 3 Liquid paraffin 8.0 4 Glycerin monostearate 2.3 5 Sorbitan monooleate 2.5 6 Polyoxy Ethylene (10) sorbitan monooleate 0.8 7 Glycerin 6.0 8 D-Saccharic-3,6-lactone 2.0 9 D-Mannoic-γ-lactone 2.0 10 Methyl p-oxybenzoate 0.2 11 Purified water 72.2 12 Perfume Suitable amount

Oil phase components 1-7 and water phase components 8-11
Are each heated to 70 to 75 ° C. and dissolved, and then water phase components 8 to 11 are added to the oil phase components 1 to 7 to emulsify, and component 12 is added and mixed during cooling, and cooled to 30 ° C. Product.

[0034]

[Formulation Example 5: Cream] Formulation Compounding amount (% by weight) 1 γ-linolenic acid 2.0 2 Ethyl linoleate 4.0 3 Salami beeswax 4.0 4 Cetanol 2.0 5 Isopropyl myristate 5.0 6 Lanolin 2 0.07 Liquid paraffin 9.0 8 Self-emulsifying glyceryl monostearate 3.0 9 Polyoxyethylene sorbitan monostearate 1.5 (20, EO) 10 Propyl paraoxybenzoate 0.1 11 Palmitoyl ascorbate 2.0 12 Stearoyl-δ-gluconolactone 5.0 13 Kojic acid 1.0 14 Methyl paraoxybenzoate 0.2 15 Propylene glycol 5.0 16 Perfume 0.2 17 Purified water 54.0

The aqueous phase components 12 to 17 excluding the oil phase components 1 to 11 and component 16 were dissolved by heating at 70 to 75 ° C., respectively, and then the oil phase components 1 to 11 were added to the aqueous phase components 12 to 17 respectively.
Is added and emulsified, and component 16 is added and mixed during cooling, and 3
The product is cooled to 0 ° C.

[0036]

EFFECT OF THE INVENTION An excellent cosmetic having a fibroblast proliferation promoting action and high safety is provided. Therefore, by using the cosmetics according to the present invention, it is possible to maintain a young skin without wrinkles or tarmi.

Claims (4)

[Claims] 1. A cosmetic comprising a lactone compound having the general formula (I) represented by the following chemical formula 1 as an active ingredient. [Chemical 1] 2. The lactone compound is D-glucurono-
6,3-lactone, α-D-glucoheptonic-γ-
Lactone, δ-glucuronolactone, α, β-glucooctonic-γ-lactone, L-glonic-γ-lactone, γ-D-galactonolactone, D-saccharic-1,4-lactone, D-saccharic- 3,6-lactone, D-(+)-ribonic-γ-lactone, α-butyrolactone, γ-butyrolactone, α-octanoic lactone, γ-octanoic lactone, nonanoic lactone, γ-valerolactone, D -Mannoic-
δ-lactone, D-xyloic-δ-lactone, D-
One or more selected from the group consisting of arabinoic-δ-lactone, stearoyl-δ-gluconolactone, D / L-pantolactone and palmitoyl-D / L-pantolactone. The cosmetic material according to claim 1. 3. D-glucuronic acid lactone, α, β-glucooctonic-γ-lactone, γ-galactonolactone, D-saccharic-3,6-lactone, D-mannoic-γ-lactone, D / L. -Pantolactone and / or palmitoyl-D / L-pantolactone as an active ingredient, The liquid and / or cream type cosmetics according to claim 1 or 2. 4. The cosmetic according to claim 1, which has a fibroblast proliferation promoting action.
Cosmetics given in any 1 paragraph.