JPS6153209A - Skin cosmetic - Google Patents

Abstract

PURPOSE:A skin cosmetic that contains pivaloyl ascorbic acid, thus showing good ageing prevention and high skin-lightening effect without any undesirable side-effect on human bodies and skin irritation with high storage stability. CONSTITUTION:The objective skin cosmetic is obtained by adding at least one of dipivaloyl ascorbic acid such as 2,6-0,0'-dipivaloylascorbic acid, which are prepared by reaction between ascorbic acid and pivalic acid or pivaloyl chloride, in an amount of 0.05-20wt%. When the resultant cosmetic is applied to skin, the pivaloylascorbic acid rapidly dissolves and diffuses in skin to stimulate the activity and metabolism of skin tissues and develop action to prevent aging and lighten the skin.

Description

Detailed Description of the Invention [Field of Industrial Application] The present invention relates to a skin cosmetic containing a specific ascorbic acid derivative described below, and more specifically, it has no undesirable side effects or skin irritation on the human body, and has a long-term use. It is stable even when stored, and has excellent anti-aging and whitening effects at the same time.
The present invention relates to a skin cosmetic that can express and impart this effect.

[Prior Art] Conventionally, in order to restore sunburned skin to a healthy complexion, it has been believed that it is necessary to lighten the increasing amount of melanin pigment formed and to inhibit tyrosinase activity during the melanin production process.

As an active substance for whitening cosmetics applying the principle of ζn et al.
Several ascorbic acid derivatives have been studied, and 3-mono-linear fatty acid esters, 2,6-di-linear fatty acid esters, etc. of ascorbic acid have been proposed (Japanese Patent Publication No. 45-15
No. 391, Special Publication No. 45-28684). However, when applied to cosmetics, there are problems with stability over time and discoloration.

It has the disadvantage that it causes odor and does not provide excellent whitening effects.

As described above, excellent skin cosmetics that can express and provide skin anti-aging effects and whitening effects have not yet been found.

[Problem that the invention seeks to solve]

The purpose of the present invention is to be stable even after long-term storage, and to prevent discoloration and odor.
An excellent product that can beautify the body, increase attractiveness, keep the skin healthy, and simultaneously express and impart skin anti-aging effects and whitening effects while giving a good feel without causing skin irritation, without causing a decrease in activity, etc. Our goal is to provide skin care cosmetics.

[Means for solving problems]

The above object of the present invention is achieved by a skin cosmetic containing dipivaloyl ascorbic acid.

Di,pivaloyl ascorbic acid used in the present invention is a known compound, and can be obtained, for example, by reacting ascorbic acid and pivalic acid or ascorbic acid and piparoyl chloride.

A specific example of the dipivaloyl ascorbic acid used in the present invention is 2.6-0.0'-dipipparobic acid.

In the present invention, each dipivaloyl ascorbic acid is blended into the sebum cosmetic base either singly or as a mixture of two or more. Its blending amount is in the form of skin layer cosmetics (
Although it varies depending on the type (type), the overall blending amount is usually within the range of 0.05 to 20% by weight based on the total amount of prescription ingredients of the cosmetic (hereinafter the same).More specific blending amount range For creamy (emulsified) cosmetics, it is 0.05-10% (preferably 1-10%).
5% by weight), and 0.05-10% by weight for emulsion cosmetics (
preferably 1 to 5% by weight), and 0.05 to 2.0% by weight (preferably 0.01 to 1.0% by weight for aqueous transparent liquid cosmetics).
iζ%), 0.05 to 20% by weight for oily cosmetics (preferably 1 to 15% by weight), and 0.05 for cake-like cosmetics.
~17 heavy f19/2 (preferably 3-10 heavy f1%),
In powdered cosmetics, it is 5 to 20% by weight (preferably 7 to 15%).
% by weight), and 0.1 to 8 weight % (preferably 0.5 to 2 weight %) for pack agents.

The cream or emulsion cosmetic of the present invention is a base for known cream or emulsion skin cosmetics such as pine surge cream, cleansing cream, skin cream, foundation cream, and milky lotion. It is obtained by blending the above-mentioned dipivaloyl ascorbic acid in the above-mentioned required amount. A known method can be used for the blending method.

Base emulsifiers that can be used in the base of the cosmetic include:
For example, synthetic emulsifiers such as ordinary nonionic surfactants, anionic surfactants, amphoteric surfactants, lecithin,
Shi! ! Sugar fatty acid ester, higher acyl glutamate,
Natural surfactants such as pectin, karaya gum, locust bean gum, glycyrrhizin (18α monolithic or 18B monolithic) acid or its alkali metal salts, ammonium salts, water-soluble collagen (polypeptide), and sodium-type bentonite only. Known emulsifiers may be mentioned.

The amount of emulsifier added is usually 0.05 to 0.05 to the total amount of prescription ingredients.
It is within the range of 5% by weight.

First, the base oily substances include oily substances for cosmetics, such as vegetable oils, animal oils, higher fatty acids, higher alcohols, synthetic ester oils, waxes, silicone oils, and the like.

The blending amount of such an oily substance as a base material is usually 5 to 60% by weight based on the total amount of prescription ingredients.

Other ingredients that may be blended include fragrances, preservatives, pigments, etc., as well as skin nutrients, moisturizers, UV inhibitors,
A pHE reservoir may be applied.

The above-mentioned dipivaloyl ascorbic acid has good stability, compatibility with oily bases, emulsifying properties, etc., so it is suitable for formulation design of emulsified cosmetics, and has anti-aging and whitening effects. It is possible to easily obtain a product with good emulsion stability, storage stability, viscosity (hardness) stability, appearance (texture, gloss), spreadability and feel during use.

The aqueous transparent liquid cosmetic of the present invention can be obtained by blending the required amount of dipivaloyl ascorbic acid into a base such as a conventional low silane or film-type pack agent. In this case, the dipivaloyl ascorbic acid is easy to make into water or a water-alcohol system, and is highly stable, so it is easy to design a formulation, and it also has stable skin anti-aging and whitening effects. It is possible to easily obtain a transparent lotion or a transparent film-type skin whitening pack that retains the positive color.

In addition to vaginal bases such as ethanol and film agents, the aqueous transparent liquid whitening cosmetic base contains fragrances, colorants, preservatives, and if necessary, skin nutrients, moisturizers, PR adjusters, etc. can be blended.

The oily whitening cosmetic composition of the present invention can be obtained by adding an appropriate amount of the dipivaloyl ascorbic acid described above to a liquid oily base material as described below and uniformly dissolving it. Examples of the liquid oil base include almond oil, olive oil, sesame oil, safflower oil, mink oil, avocado oil, jojoba oil, isopropyl palmitate, isopropyl myristate, oleyl alcohol, isostearyl alcohol,
Octyldodecanol and the like can be mentioned. Among these, oily substances that are easily soluble in sebum are particularly preferred.

The sieve-like whitening cosmetic composition of the present invention is in the form of a substantially transparent oil with high fluidity, and is non-aqueous. As mentioned above, the dipivaloyl ascorbic acid is soluble,
Due to its high stability, it is completely dissolved in the liquid oil base, and exhibits good skin anti-aging and whitening effects without any loss of activity even after long-term storage. I can do it.

The cake-like cosmetic composition according to the present invention is produced by the known process G using a pigment and the monopivaloyl ascorbic acid or a conventional oily substance for cosmetics as main components.

The powdered whitening cosmetic of the present invention is produced by adding the dipivaloyl ascorbic acid of the present invention to a conventional powder base material such as starch, lactose, mannitol, precipitated calcium carbonate, etc., and uniformly kneading the mixture. Ru.

[For production]

The dipivaloyl ascorbic acid of the present invention has excellent stability in cosmetic systems, compatibility with oily base materials, emulsifying properties, and safety for the human body, so it is suitable for formulation design of skin cosmetics. It is possible to provide a cosmetic that is easy to use, has good stability over time, and provides a good feeling without irritating the skin.

When the skin cosmetic of the present invention is applied to the skin, the piparoyl ascorbic acid quickly dissolves and diffuses into the sebum and easily penetrates into the skin, promoting the activity and metabolism of the skin tissue, and as a result, the above-mentioned In addition to exhibiting an anti-aging effect on the skin, it also moderately inhibits the activity of tyrosinase in skin tissues, and can exhibit an excellent skin whitening effect.

〔Example〕

The present invention will be explained in more detail below with reference to Examples.

Incidentally, the parts shown in the examples are 1% by weight and 1% by weight.

In addition, it has the effect of improving rough skin, improving keratin, sensual effect, and beauty.
The test methods for whitening effect, storage stability, etc. are as follows.

(1) Test method for measuring effect on improving rough skin The effect of continuous application for 4 weeks was investigated on 20 middle-aged and elderly subjects who had rough skin on their lower legs. Approximately 12 skin cosmetics were applied to the test site of the left lower leg of the test subject twice a day, and the condition of the skin before and after the test was evaluated according to the criteria in Table 1. No sample was applied to the right lower leg, which served as a control.

Table 1 Judgment criteria for skin dryness m: Normal ±: Slight dryness, no flaking +: Dry smoke, mild flaking ++: Dryness, moderate flaking +++: Dryness, significant flaking Judgment results of the test site and control site before and after the test If the skin dryness has improved by two or more levels (e.g. +→-1)
++ → ±) is “valid”, and if it has been improved by one level, it is “ya?”
If there was no change, it was considered "invalid." There were no cases of skin dryness progressing during the test period.

(2) Test method for measuring the effect of improving keratin (increasing the anti-exfoliation properties of keratinocytes) Apply Scotch tape to the skin of the test area before and after the above rough skin improvement measurement test (using Scotch tape or Tiban mending tape)
When the tape was adhered and peeled off, the condition of the corneocytes attached to the tape was examined in detail using a scanning electron microscope, and the skin corneocyte anti-peeling properties were separated according to the criteria in Table 2, and the corneum improving effect was determined.

Table 2 Judgment criteria for keratin improvement effect (increased anti-desquamation property of keratinocytes) Evaluation points: 1 Not recognized on 2 scales 2: Small scales scattered 3: Small to medium scales noticeable 4: Large scales noticeable Table 2 shows 4 weeks When the difference between the evaluation score of the test site and that of the control site after continuous application was 2 points or more, it was considered "effective," when it was 1 point, "somewhat effective," and when it was 0 points, "ineffective."

There were no cases in which the evaluation score of the test site was higher than that of the control site.

The exfoliation properties of these corneocytes serve as an index for determining the structural properties of the stratum corneum, and in general, in dry skin and aging skin, the amount of intercellular connections is weak and the structure is dense. It has been confirmed that the index is high because the gender is also low.

(3) Sensory effect panel test The sample was applied to the faces of 50 middle-aged (30 to 50 years old) female panelists twice a day for two months, and each panelist tested the test before and after the test. The skin condition was evaluated for "wrinkle smoothing effect", "effect on firmness", and "effect on moist feeling".

(4) Panel test for skin whitening effect Samples were applied to a panel of 20 female subjects suffering from dark skin, age spots, and freckles every morning for two months. Panera himself judged which one.

(5) Storage stability test (stability of cosmetics after 16 months at 40°C) Appearance changes (presence or absence of separation, coloring, etc.) of cosmetics samples after storing them in a constant temperature room at 40°C for 6 months, Three specialized inspectors checked for the presence or absence of strange odors.

Example 1゜2, 6-0. Into a molten homogeneous mixture (80°C) consisting of 4 parts of O'-dipino shunyl ascorbic moromi, 5225 parts of stuff, 3 parts of cetyl alcohol, 5 parts of olive oil, 2 parts of glyceryl monostearate, and 8 parts of stearic acid, 05 xanthan gum was added. part, triethanolamine 0.8
An aqueous solution (80°C) consisting of 0.2 parts of methylparaben, 0.2 parts of methylparaben, and 56 parts of water was added under stirring to emulsify it, and then cooled to 40°C. When the temperature was lowered to 40°C, an appropriate amount of fragrance was added to make one bottle. A cream cosmetic of the % type emulsion of the invention was obtained.

The test results for this cosmetic are shown in Table 3 below.

Comparative Example 1 2.6-0.0-dipivaloyl ascorbic acid instead of 2.6-0.0-dipivaloyl ascorbic acid. A comparative cream cosmetic was obtained in the same manner as in Example 1, except that O'-dipalmitoyl ascorbic acid was used. The test results for this cosmetic are shown in Table 3 below.

Comparative Example 2 The same procedure as in Example 1 was carried out except that 2.6-0.0'-dipentanoyl ascorbic acid was used instead of 2.6-0.0'-dipivaloyl ascorbic acid. A comparative cream cosmetic was obtained.

The test results for this cosmetic are shown in Table 8 below and are shown in Table 3, Example 2゜8.6-0. 0.5 parts of xanthan gum, 18 parts of xanthan gum in a dissolved homogeneous mixture (80"C) consisting of 4 parts of O'-divinoylar ascorbic acid, 9212 parts of Stuff, 3 parts of olive oil, 3 parts of isocetyl myristate, and 1 part of Geiro
An aqueous solution consisting of 3 parts of monoammonium α-glycyrrhizinate, 0.2 parts of methylparaben, and 74.3 parts of water
0°C) was added under stirring to emulsify, and then cooled, and when the temperature dropped to 30°C, an appropriate amount of perfume was added to obtain a type 04 emulsion cosmetic of the present invention.

The test results for this cosmetic are shown in Table 4 below.Table 4 Example 3゜5.6-0. After dissolving 1 part of Q'-dipivaloyl ascorbic acid in 15 parts of ethanol, 5 parts of propylene glycol, 05 parts of polyoxyethylene hydrogenated castor oil (number of moles of ethylene oxide added is 60 moles), 78.5 parts of water, and Add appropriate volume while stirring, mix and dissolve uniformly,
A lotion of the present invention was obtained.

The stability of the obtained lotion after 16 months of 40'C is colored,
It was in good condition with no strange odor. In addition, the results of sensory tests such as wrinkle smoothing effect, firmness effect, moisturizing effect, and whitening effect were also good.

Example 4゜1 part of 2,6-0.0'-dipivaloyl ascorbic acid,
A mixed solution in which 13 parts of ethyl alcohol, 3 parts of glycerin, and 2 parts of polyoxyethylene hydrogenated castor oil are uniformly dissolved is gradually added to an aqueous solution of 7 parts of polyvinyl alcohol dissolved in 74 parts of water with stirring, and mixed. In this way, a pack agent of the present invention was obtained.

The stability of the obtained pack agent after 16 months at 40°C was good, with no coloration, odor, etc. In addition, the results of sensory tests such as elongation effect, firmness effect, moisturizing effect, and whitening effect were also good.

Example 5. 15 parts of 2.6-0.0'-dipivaloyl ascorbic acid, 30 parts of starch, 55 parts of lactose and an appropriate amount of fragrance were uniformly mixed to obtain a powdered cosmetic of the present invention.

This powdered cosmetic was uniformly kneaded in 10 times the amount of emulsion and applied to the face. When used twice a day for two months continuously, sensory tests such as wrinkle smoothing effect, firmness effect, moisturizing effect, and whitening effect were also good.

Claims (1)

[Claims] A skin cosmetic characterized by containing dipivaloyl ascorbic acid.