JPS6160802B2 - - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a skin-whitening cosmetic containing a 2-alkyl-5-oxy-γ-pyrone compound, which has great whitening and sun protection effects.

It is common for women to want to have fair and beautiful skin, and traditionally, treatments such as hydrogen peroxide, zinc peroxide, magnesium peroxide, sodium peroxide, zinc perborate, magnesium perborate, or sodium perborate have been used. Cosmetics containing peroxide were used. However, since the above-mentioned peroxides are extremely unstable substances, there are problems in terms of storage stability and incorporation into cosmetics, and their whitening effect is not sufficient. In recent years,
Cosmetics containing vitamin C, cysteine, colloidal sulfur, etc. have been developed and are now in use, but they are still far from being fully satisfactory.

However, the inventors of the present invention have conducted extensive research over many years in order to find a compound that does not have any undesirable side effects on the human body and has an excellent whitening effect, and has found the general formula: The 2-alkyl-5-oxy-γ-pyrone compound represented by the formula (wherein R is a lower alkyl group) has a particularly excellent melanin production inhibiting effect, and has an outstanding whitening effect and sun protection effect. Having discovered this new fact, we have now completed the present invention.

That is, the present invention is a fair-skinned cosmetic comprising a 2-alkyl-5-oxy-γ-pyrone compound contained in a suitable cosmetic base, and wherein a 2-alkyl-5-oxy-γ-pyrone compound is contained in a suitable cosmetic base. Various basic cosmetic base materials, such as various alcohols, animal and vegetable fats, surfactants, pectin, carboxymethyl cellulose, alginates, as well as stabilizers, pigments, fragrances and other ingredients, are blended as appropriate, and if necessary. Anything that has been heated and melted or melted and stirred can be used as is.

The 2-alkyl-5-oxy-γ-pyrone compound used as a skin whitening agent in the present invention is a substance whose action and effect are almost unknown. The fact that it inhibits the action of tyrosinase in the skin and inhibits melanin production, resulting in a remarkable whitening effect, was something that no one could have predicted before, and was revealed for the first time by the present inventor. .

2-alkyl-5-oxy- preferably employed
A representative example of the γ-pyrone compound is allomaltol. These γ
- The melanin production inhibiting effect of pyrone compounds will be explained below with reference to experimental examples.

Experimental Example A 0.01% (wt%) malomaltol aqueous solution was prepared.

Next, add L-tyrosine solution (0.3 mg/
ml) and 1 ml of Matsukulbane's buffer solution (PH
6.8) and 0.9 mL of the above aromatol aqueous solution.
After incubating for 10 minutes in a thermostatic water bath at 37°C, add tyrosinase solution (1 mg/ml) to this.
ml), stir well, and immediately set it in a spectrophotometer to measure the absorbance at 475 mμ over time (in minutes) to determine the formation of red dopachrome (precursor of melanin pigment). We sought the relationship between quantity and time.

The attached drawing is a graph showing the above experimental results, and this graph shows that allomaltol has the effect of strongly suppressing the production of dopachrome, which is a precursor of melanin pigment, and is therefore an excellent whitening agent. It can be seen that it has a sunburn prevention effect.

As can be seen from the above experimental results, such 3 (or 5)-oxy-γ-pyrone compounds usually have a concentration of 0.01
% aqueous solution exhibits an excellent effect of inhibiting dopachrome formation, and when the fairing cosmetic of the present invention is prepared by incorporating a 2-alkyl-5-oxy-γ-pyrone compound into a cosmetic base material, A content of 5% or less, especially about 0.01 to 2.0%, is sufficient, and even with such a small amount, the purpose of the present invention can be completely achieved.

In addition, such 2-alkyl-5-γ-pyrone compounds generally have good blendability in cosmetic base materials, and have good stability with little change over time against pH, heat, decolorization, etc., so they may be included. The fair skin cosmetic of the present invention is an excellent product that does not deteriorate in efficacy or change in quality during storage.

Next, formulation examples of the fair skin cosmetic of the present invention will be listed, but the present invention is not limited to these formulation examples.

Prescription example 1 [Lotion] (Ingredients) (Parts by weight) Allomaltol 0.5 Aminoacetic acid 0.20 Pyridoxine hydrochloride 0.05 Zinc phenolsulfonate 0.30 Propylene glycol 8.00 Ethanol 5.00 Refined water 86.35 Fragrances and preservatives Small amount prescription example 2 [Pack] (Ingredients) (Parts by weight) Pyromeconic acid 0.25 Aminoacetic acid 0.20 Zinc phenolsulfonate 0.30 Propylene glycol 13.00 Carboxyvinyl polymer 1.20 Sodium hydroxide 0.14 Ethanol 2.50 Titanium oxide 0.02 Purified water 82.54 Flavoring and preservative Small amount formulation example 3 [Package] ] (Ingredients) (Parts by weight) Polyvinyl alcohol 15.00 Polyvinylpyrrolidone 4.00 Propylene glycol 6.00 Ethanol 10.00 Aromaltol 0.5 Purified water 69.70 Fragrances and preservatives Small amount formulation example 4 [Milk lotion] (Ingredients) (Parts by weight) Stearic acid 2.00 Setanol 0.50 Lanolin 2.00 Oleyl oleate 2.00 Squalane 3.00 Liquid paraffin 8.00 Emulsifier 2.60 Pyromeconic acid 0.2 Triethanolamine 1.00 Propylene glycol 4.00 Purified water 74.90 Fragrances, antioxidants and preservatives Small quantity formulation example 5 [Vanishing Cream ] (Ingredients) (Parts by weight) MC stearic acid 8.00 Beeswax 5.00 Setanol 3.00 Lanolin 2.00 Isopropyl myristate 6.00 Liquid paraffin 7.00 Olive oil 2.00 Emulsifier 5.50 Pyromeconic acid 0.4 Triethanolamine 0.60 Propylene glycol 3.00 Purified water 57 .70 Fragrances, Antioxidants Semed and preservatives small quantity prescription Example 6 [cold cream] (component) (weight part) white vassin 7.00 white vassin 3.00 ranoline 3.00 msopropyl 3.00 squaralan 4.00 paling paraphroses polyoxyethylene ether 2.370 Emps 2.3. 0 Aroma Lutol 0.3 Propylene glycol 2.00 Purified water 23.00 Fragrances, antioxidants and preservatives Small amounts (Melanin production inhibition test) Women aged 20-50 using the cream of Formulation Example 5 65
It was applied once a day to the affected areas of human patients with hyperpigmentation for three months.

As a result, among the patients tested, the symptoms were completely cured.
21 patients showed improvement in symptoms, 32 patients showed improvement in symptoms, and 12 patients showed no change.

The results of this test showed that as many as 81% of patients saw some improvement in symptoms, indicating that the drug had a significant melanin production suppressing effect.

Further, when a similar test was conducted on the cold cream of Formulation Example 6, similar results were obtained.

[Brief explanation of the drawing]

The figure is a graph showing the relationship between the amount of dopachrome produced and time to show the melanin production inhibiting effect of allomaltol.

Claims (1)

[Claims] 1. General formula: A fair-skinned cosmetic containing a 2-alkyl-5-oxy-γ-pyrone compound represented by the formula (wherein R is a lower alkyl group). 2. The fair-skinned cosmetic according to claim 1, wherein the content of the 2-alkyl-5-oxy-γ-pyrone compound is 5% by weight or less. 3. A fair-skinned cosmetic according to claim 1 or 2, wherein the 2-alkyl-5-oxy-γ-pyrone compound is aromaltol.