JPS62413A - Cosmetic - Google Patents

Abstract

PURPOSE:To obtain a cosmetic having excellent effect to retain moisture on the skin surface and constantly keep fair and moistened skin, by using 2-(p- isobutylphenyl)propionic acid 2-pyridinemethyl ester as an active component. CONSTITUTION:The compound of formula is used as an active component of the objective cosmetic in an amount of 0.01-3wt%, preferably 0.5-2wt% based on the cosmetic base. The compound of formula is an ester of 2-pyridine-ethanol and ibuprofen known as an antiinflammatory agent for oral administration and can be produced by acid anhydride process, acid halide process, etc. It can be compounded easily to various cosmetic bases and formed in the form of various cosmetic preparations without causing discoloration, odorization, decomposition or deactivation with time. It can be applied safely to the human body absolutely without causing problems such as toxicity, skin damage, etc.

Description

[Detailed description of the invention] <Industrial application field> This E! Item A relates to a cosmetic that retains moisture on the skin surface and has excellent skin beautifying effects that constantly moisturizes the skin.

More specifically, the present invention provides 2-(p-inbutylphenyl)flopion relative-2-pyridine methyl ester (
The present invention provides a cosmetic composition containing F1 ibuprofen piconol as an active ingredient. The cosmetics of the present invention have a useful effect on improving skin conditions caused by skin dryness such as cracks, chapped skin, and rough skin. It is important to add smoothness to makeup,
A cosmetic effect that can improve gloss and prevent deterioration of fine wrinkles can be obtained.

<Problems to be solved by the invention> In general, cracks, chapped skin, and rough skin are caused by dryness in the winter when the air is dry, due to a decrease in the amount of secretion of the skin, especially lipids. function decreases, transepidermal water loss (
This is a phenomenon that is caused by an increase in the amount of water (hereinafter abbreviated as T, W, L) or by a physical cause (for example, water in the epidermis is drawn out by washing).

On the other hand, a condition in which the moisture content of the stratum corneum decreases to around 10% even under normal conditions depending on age and constitution is called dry skin, and when this skin condition occurs, the skin's luster decreases and fine wrinkles become noticeable. The appearance of makeup such as makeup becomes worse. These phenomena are as follows: Water in the stratum corneum of the epidermis normally combines with constituent components of the stratum corneum to maintain normal skin function, but environmental changes (low temperature, low humidity), aging, changes in constitution, etc. This occurs as a result of a decrease in the water content M of the stratum corneum. In order to improve these skin conditions, K prevents a decrease in the moisture content of the stratum corneum and restores normal skin a.
(It is necessary to maintain the performance of each building), and methods for each building have been studied so far.

Conventional technology> The conventional method is to use an occluding agent [T
, W, and L, and a method of increasing the skin hydration effect using a humectant.

The former method uses Vaseline ointment or water-in-oil emulsion as a hydrophobic material that has good contact with the skin.
It has the disadvantage of giving an unpleasant feeling such as being oily and sticky.

The latter method uses polyhydric alcohols such as sorbitol, marbitol, ethylene glycol, phlopylene gelicol, 1.3-7' ethylene glycol, and glycerin, which have excellent moisture absorption and moisturizing power, as well as POA soda, lactate sodium, etc. This method uses an emulsified composition containing humectants such as salts, but in order to increase the effect, large amounts of these substances must be blended, resulting in unpleasant sensations such as stickiness and sliminess. It has the disadvantage that it gives a tactile feel.

The Ministry of Invention and others conducted extensive research in order to solve the above-mentioned drawbacks of conventional products and to find a substance that has a high ability to enhance moisture retention without relying on conventional closing agents or humectants. However, it has been found that ibuprofen piconol is effective in improving dry and polished skin conditions such as rough skin, shine, and fine wrinkles. Main issue:! J1 is based on this knowledge.

The present invention will be explained below with #f=iK.

Ibuprofen piconol, which is an active ingredient of the cosmetic according to the present invention, is a compound represented by the formula r, and is an ester compound of ibuprofen and 2-pyridine methanol, which is known as a light anti-inflammatory drug.

As a method for obtaining this property, various methods are known, such as the acid anhydride method and the acid halide method.
(Refer to each publication No. 0).

Ibuprofen piconol is a pale yellow, clear, slightly viscous substance with no odor.It can be used in organic solvents such as ethanol and acetone, vegetable oils such as olive oil, jojoba oil, soybean oil, and other esters. Mix well with. Therefore, this product has the property of being easily blended into various volatile cosmetic materials. moreover,
This substance also causes discoloration, odor, and
It does not undergo changes over time such as decomposition and inactivation, and there is no concern about toxicity or skin irritation, so it can be used safely.

As the cosmetic base used in the cosmetic of the present invention, any base commonly used in cosmetics can be used. Although not particularly specified, specific examples include cream, milky lotion, Examples include oils, lotions, packs, and ointments, among which creams, milky lotions, oils, and the like are preferred from the viewpoint of transdermal absorption. Common raw materials used include, for example, beeswax, cetanol, olive oil, stearic acid, lanolin, petrolatum, squalane, parapetrum, glycerin, propylene glycol monostearate, and POE cetyl ether in cream, emulsion, oil, and ointment bases. Lotion bases include oleyl alcohol, ethanol, glycerin, 1.3-' ethylene glycol, POE lauryl ether, sorbitan monolaurate, and pack bases include polyvinyl acetate emulsion, Examples include polyvinyl alcohol and ethanol. From these raw materials, appropriate fx raw materials are selected according to the intended dosage form, and cosmetics such as sifreeme, milky lotion, oil, lotion, pack, and soft floss are prepared by a conventional method.

The amount of ibuprofen piconol used in the cosmetics of the present invention is usually 0.01 to 3%, preferably 0.01 to 3%.
5-2 weight is easy. If the amount is less than 0.01% by weight, the above-mentioned effect cannot be sufficiently obtained, and even if the amount exceeds 3% by weight, no enhancement of the effect is observed, so it is ignored.

The method of blending ibuprofen piconol into the cosmetic base 41K is, for example, when blending it into creams, emulsions, oils, ointments, etc. For water or packs, after dissolving in alcohol or polyhydric alcohol,
A method of blending is adopted.

<Effects of the Invention> When applied directly to the skin, the cosmetic containing ibuprofen piconol according to the present invention has an effect on improving rough skin on hands, fingers, etc., and on facial gloss and fine wrinkles. can be achieved. It is thought that ibuprofen piconol administered to the skin is absorbed into the sebaceous glands and remains in the sebaceous glands, improving lipid metabolism and thereby increasing the skin's water retention function. Ibuprofen piconol has been used as a pharmaceutical preparation for its anti-inflammatory and analgesic effects, but when applied in such a small amount, it has the effect of restoring the skin's moisture retention function. This was discovered for the first time by the present inventors, and was completely unexpected from the prior art.

Here, in order to evaluate the cosmetics of the present invention, Example 2 (described below)
As shown in Example 3, milky lotions and creams were prepared as examples of cosmetics according to the present invention, and practical tests were conducted to confirm their efficacy. In addition, as comparison products, the milky lotions of Example 2 and Example 6 described later and 71
An emulsion and hand cream prepared by adding f% of the ibuprofen piconol in the hand cream to 2-ethylhexane and cetyl? Using. The test method used was the method shown in Section F. The results are shown in Cloth 1 and Table 2.

Test method: 150 Japanese adult women with dry skin were randomly assigned to group A (35 people), group SS (65 people), and group C# (
40 people) and Group B (40 people), the emulsion according to the example of the present invention was applied to the face of An, and the emulsion of the comparative product was applied to the face of Group B. In addition, a hand cream according to an example of the present invention was applied to the fingers of group 0, and a comparative hand cream was applied to the fingers VC of group B for 6 weeks. After 6 weeks, the improvement status and spontaneous worsening of the swelling and related evaluation factors were compared between the groups.

Table 2: Improvement of dry skin on hands and natural exacerbation (evaluation)
Kan: Clearly removed: Kanashi Kaigo +: Slightly improved M: No change As shown in the results in Tables 1 and 2, the emulsion according to the present invention has lower evaluation factors than the comparative emulsion. It showed good effects on the skin in general, and in particular had significant effects (improvement or inhibition of natural aggravation) on dryness, fine wrinkles, and less makeup, proving that the skin was immersed in beautifying effects. Similarly, it has been revealed that the hand cream according to the present invention has a remarkable effect of improving dryness of hands and fingers, skin irritation, etc., or has an effect of suppressing natural aggravation.

<Example> Hereinafter, as an example of the present invention, a formulation example and a method for preparing a vegetable composition will be shown. In addition, the blending ratio is shown in % of the base weight.

Example 1 Soft lotion (A) #I Seisui 7a4 Glycerin 5.0 Propylene glycol 4.0 (B) P
OEC20) Rubitan monolaurate 1
．． 5POE! (20) Lauryl ether 0
．． 5 ethanol 10.0 fragrance
Fee 0.1
Ibuprofen Piconol 0.5 Combine the ingredients of Preparation Method (4) and boil at room temperature. Ten thousand,(
The components of B) are combined and dissolved in a bath at room temperature, and this is added to the outside of the formulation of (A) to solubilize.

Example 2 Emulsion (A) PI (50) hydrogenated castor oil 1.5
Coconut Oil Fatty Acid Monoglyceride 1.0 Oleic Acid Triglyceride 7.5 Ej-10 Fenpiconeau #1.0) Glycerin
2.5 Purified water 86.3 (C) Fragrance
0.2 Combine the ingredients of Preparation Method (4), heat mix, and bring to 70C.

Combine the components of (B), heat and mix at 70°C, add (4) to this and emulsify, and add (0) while cooling.

Example 3 Hand cream (4) Vaseline 1aO Setanol aO Ifuflofuenbiconol 2.0FOI (20)
Oleyl ether 1.4 Sorbitan monostearate 0.8 (B) Preservative 0.3 nI Ice 69.
3(C) Flavoring
a2 Consistent manufacturing method The same method as in Example 2 was used.

Example 4 Water injection ointment (A) poz (3o) *Tyl ether 2.0 glyceryl monostearate IQ, 0 liquid paraffin
10.0 Vaseline 4
．． 0 Setanol 5.0 Ibupro 7
Empiconol 5゜Preservative α2 CB) Propylene glycol 1 (LOJr
f! Water production 55.8 Combine each component of preparation method (4) and heat to 80°C. (to))
Combine each component and heat to 82°C or higher. While stirring (A), add CB) to it.
, Stir and emulsify, then dissolve.

Example 5 Gel cosmetic oil pile) 1.3-butylene glycol 1αQ glycerin 26.5n Ice making 5.0 Preservative 0
．． 6(0) Liquid paraffin 20.
0 Olive oil 30.0 2-Ethylhexane-related triglysenides 5.0 Ibupro7
Empiconol 1.0 (To) Fragrance
Combine the components of α2 preparation method (B), heat to 70 to 80°C, and dissolve K (Al). Add the ingredients of (C) to this,
Once cooled to 40C, add (l) and then cool.

Example 6 Non-alcoholic lotion Buddha) Propylene glycol ZO polyoxyethylene (50) Hydrogenated castor oil 1.0 Ibuprofen Piconol 1.0 Fragrance
0.1(B) Quen 1[0,1
5 Sodium citrate a1 Methylparaben 0.05nIM water 90.
6. Dissolve each component of Preparation Method (4) in a mixed bath at room temperature or under heating, and add this to the recipe in [Medium] while stirring at high speed to solubilize.

Claims (1)

[Claims] 1) The cosmetic base is 2-pyridinemethyl 2-(p-isobutylphenyl)propionate represented by the formula (I) ▲There are mathematical formulas, chemical formulas, tables, etc.▼(I) A cosmetic product characterized by containing an ester as an active ingredient. 2) The proportion of the above-mentioned 2-(p-isobutylphenyl)propionic acid-2-pyridine methyl ester is 0.
．． The cosmetic composition according to claim 1, wherein the content is 01 to 3% by weight.