JP3193441B2 - Whitening cosmetics - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a cosmetic which has a high whitening effect, inhibits the activity of hyaluronidase, and is effective for rough skin.

[0002]

2. Description of the Related Art Guava is called a bunjirou or a gemstone, and is a plant belonging to the genus Tsubami, genus Bunjiro, and its scientific name is Psidium Guajava L.
Generally, the berries are eaten raw, jam, juice, or the like. It is native to tropical America, but is widely cultivated in tropical and subtropical areas, cultivated in southern Kyushu in Japan, and wild in the Ryukyu Islands. It is also used as a drug for enteritis, dysentery, and dyspepsia.

On the other hand, various substances having a whitening effect that can be used as a raw material for cosmetics are known.
Synthetic products are not guaranteed for long-term application to human skin, and their use is being restricted. On the other hand, many natural products have a weak whitening effect. However, from the viewpoint of safety for human skin, it is a natural product that is eaten by humans for many years and is guaranteed in terms of safety, and has a strong whitening effect, and also has other effects on skin. Was desired.

[0004]

SUMMARY OF THE INVENTION An object of the present invention is to provide a whitening cosmetic which is safe when applied to the skin, has a large whitening effect, inhibits the activity of hyaluronidase, and further contains an effective ingredient for rough skin. It is to provide.

[0005]

Means for Solving the Problems In order to solve the above-mentioned problems, the present inventors have screened and examined plants which have been used for food for many years and whose safety to the human body has been confirmed, and used them as cosmetics. We considered something worthwhile. As a result, they have found that guava is very effective as a cosmetic ingredient or as a quasi-drug. As the confirmed effects, whitening action, inhibition of hyaluronidase activity, suppression of active oxygen, and antioxidant properties were confirmed.

That is, the present invention is a whitening cosmetic comprising, as an active ingredient, a solvent extract of guava leaves.

As a method of using guava leaves, extraction is performed with water or a hydrophilic organic solvent such as ethanol, methanol, acetone or the like. However, it is a matter of course that extraction with water, ethanol, or a mixed solvent thereof is preferable because it is the extraction of cosmetic raw materials. It is also effective to freeze-dry the extract and use it as a powder depending on the method of use.

This substance is used as a raw material for other cosmetics such as liquid oils such as squalane and jojoba oil, solid oils such as beeswax and cetyl alcohol, various activators, humectants such as glycerin and 1,3-butylene glycol and various chemicals. In addition, cosmetics of various dosage forms can be prepared. For example, a use form may be considered depending on the purpose, such as a lotion, a cream, an emulsion, a pack, and the like.

The effect of the extract of the present invention is, as described above, firstly a skin whitening effect. Second is the activity of suppressing the activity of hyaluronidase. Hyaluronidase is an enzyme that is widely distributed in living organisms and also present in the skin. As its name implies, it degrades hyaluronic acid. Hyaluronic acid is β-DN
-Acetylglucosamine and β-D-glucuronic acid are alternately linked linear high-molecular polysaccharides, and are a type of glycosaminoglycan widely present in connective tissues of mammals together with chondroitin sulfate. The function of hyaluronic acid in connective tissue is to hold water in the intercellular space, form a jelly-like matrix in the tissue to hold the cells, maintain the lubricity and flexibility of the skin, Injury)
And prevent bacterial infection. It is said that the hyaluronic acid in the skin decreases with age, resulting in aging such as fine wrinkles and dryness.
Therefore, suppressing the activity of hyaluronidase, which degrades this, can improve the stability of hyaluronic acid used in the preparation, the stability of hyaluronic acid in the preparation after application to the skin, and the hyaluronic acid existing in the skin. It is thought to contribute.

Third, there is an active oxygen suppressing action. There is oxygen in the air, without which organisms (except anaerobic ones) cannot exist. However, oxygen becomes active oxygen under the influence of ultraviolet rays and enzymes. Active oxygen oxidizes fatty acids and produces peroxide. Phospholipids in biological membranes of living organisms also oxidize and cause damage. In addition, it is said that the generated peroxide and active oxygen damage DNA and promote aging. This active oxygen affects the mechanism of producing melanin from tyrosine and is also involved in skin darkening. Suppressing this active oxygen is important for the skin, in other words, an important factor required for cosmetics. The guava of the present invention also has this active oxygen suppressing action and antioxidant property.

[0011]

EXAMPLES The following is an example of an actual method of use, but the present invention is not limited to this example. A production example of the guava extract used in this example is shown below.

(Production Example 1) 10 g of guava leaves (dried product)
To the mixture was added 300 ml of ethanol, and the mixture was left for 5 days with occasional stirring. This was lyophilized after filtration.

(Production Example 2) 10 g of guava leaves (dried product)
Was added to the mixture, and the mixture was left for 5 days with occasional stirring. This was lyophilized after filtration.

(Production Example 3) 10 g of guava leaves (dried product)
300 ml of purified water is added to the mixture and heated for 3 hours. After allowing this to cool, it was filtered and freeze-dried.

(Example 1) Lotion olive oil 0.5 Ethanol extract of guava of Production Example 0.5 Polyoxyethylene (20E.O.) Sorbitan monostearate 2.0 Polyoxyethylene (60E.O.) Hardened castor oil 2.0 Ethanol 10.0 1.0% aqueous sodium hyaluronate solution 5.0 Purified water 80.0

Example 2 Cream A Squalane 20.0 Olive oil 2.0 Mink oil 1.0 Jojoba oil 5.0 Beeswax 5.0 Cetostearyl alcohol 2.0 Glycerin monostearate 1.0 Sorbitan monostearate 2 0.0 50% ethanol extract of guava of Production Example 2 1.0 B Purified water 47.9 Polyoxyethylene (20E.O.) sorbitan monostearate 2.0 Polyoxyethylene (60E.O.) hydrogenated castor oil 1.0 Glycerin 5.0 1.0% aqueous solution of sodium hyaluronate 5.0 Methyl parahydroxybenzoate 0.1 A and B are each weighed, heated to 70 ° C., and A is gradually added to B with stirring. After that, 30 with slow stirring
Cooled to ° C.

(Example 3) Cream In Example-3, the extract of Production Example 2 of Example-2 was used.
What was created as an A component instead of an extract of

(Inhibition of Tyrosinase Activity) (Test Method) Mcllvaln buffer 0.9
1.0 ml of 1.66 mM tyrosine solution,
0.1 wt / v% aqueous solution of the above production example (freeze-dried product) (If it is difficult to dissolve, add ethanol to dissolve, then add purified water, evaporate, remove ethanol, then 0.1 wt / v% Was prepared in a screw vial and heated in a thermostat bath at 37 ° C. for 5 minutes or more. 0.1 ml of a tyrosinase solution (manufactured by Sigma, from mushrooms, 914 units / ml) was added,
The temperature was kept in a constant temperature water bath at 37 ° C., and the absorbance was measured at 475 nm after 10 minutes. As a control, pure water was added instead of the sample solution, and the measurement was performed in the same manner. In this test, the final concentration of the sample is 0.033%. (Calculation formula) Tyrosinase activity inhibition rate (%) = {B- (AP)} /
B × 100 where A: Absorbance of sample specimen B: Absorbance of control P: Absorbance due to coloring of sample specimen (3 times dilution)

[0019]

[Table 1]

(Test for Inhibition of Hyaluronidase Activity) (Test Method) 0.4% Sodium Hyaluronate 0.1 M
(PH 6.0) Weigh 6 g of phosphate buffer solution,
After standing in a constant temperature water bath at 5 ° C. for 5 minutes, a 0.1 wt / v% aqueous solution of the above production example (freeze-dried product) (if it is difficult to dissolve, add ethanol and dissolve, then add purified water, evaporate, and evaporate the ethanol. After removal, 1.0 ml of the mixture was prepared so as to have a concentration of 0.1 wt / v%, and the mixture was stirred. 0.01% hyaluronidase (manufactured by Sigma Corp., bovine testes, type IS)
1 ml of a 0.1 M (pH 6.0) phosphate buffer solution was added and stirred immediately, and 6 ml of the solution was placed in an Ostwald viscometer placed in a thermostat bath at 37 ° C. After 1 minute, 5 minutes, 10 minutes, 20 minutes, and 40 minutes, the viscosity was measured. As a control, pure water was added instead of the sample solution, and the measurement was performed in the same manner.
In this test, the final concentration of the sample is 0.0125%. 1
The results are shown in Table 2 as an index, with the viscosity after one minute being 100.

[0021]

[Table 2]

(Active Oxygen Suppression Test) There are various methods for measuring the effect of suppressing active oxygen. The following method was used in this study. pH 7.8 50 mM potassium phosphate buffer (containing 1.3 mM DETAPAC) 133 ml 40 unit / ml above potassium phosphate buffer of catalase 5 ml 2 mM nitro blue tetrazolium above potassium phosphate buffer 5 ml 1.8 mM xanthine above phosphorus Potassium acid buffer 17ml 160ml 2.4ml of the mixture of reagents and 0.3ml of the sample are added, and xanthine oxynase is added to the sample so that the absorbance increases by about 0.02 per minute. Adjust with the above potassium phosphate buffer) 0.3
Immediately after adding ml, the absorbance (560 nm) is measured. (Measurement is divided into two and the linearity is confirmed.) Calculation formula Inhibition rate = (AB) / A × 100 where A: change in absorbance per minute when the sample is water B: sample 1 Change in absorbance per minute The concentration step was performed several steps, and a 50% active oxygen production inhibition concentration was searched for. The method of preparing the sample is as follows. The above-mentioned production example (lyophilized product) is dissolved in an aqueous solution of an appropriate concentration (if it is difficult to dissolve, ethanol is added thereto, and then purified water is added thereto, followed by evaporation.
After removing the ethanol, it was adjusted to an appropriate concentration%). The results are shown in Table 3 at 50% active oxygen inhibition concentration.

[0023]

[Table 3]

(Antioxidant test) The following test solutions were prepared in 50 ml test tubes with screw caps. Specimen 5 mg 1% linoleic acid ethanol solution 10 ml 0.1 M, pH 7.0 phosphate buffer 10 ml purified water 5 ml This is left in a constant temperature bath at 40 ° C. while being shielded from light. The following measurements were made before, after 12, 16, 16, 20, and 24 days before placing the sample in a thermostat. 0.125 ml of test solution, 12.125 ml of 75% ethanol, and 0.125 ml of 30% ammonium thiocyanate were added, and the mixture was stirred and left for 3 minutes.
0.125 ml of 2N ferrous chloride 3.5% HCl aqueous solution was added, stirred, left for 3 minutes, and the absorbance was measured at a wavelength of 500 nm. The cell length was 10 mm, and the control cell was one in which the test solution was replaced with water. Table 4 shows the results (the same sample was measured three times and averaged).
Shown in

[0025]

[Table 4]

(Usage test) The face of each of seven women was divided into left and right, one of which was used as an example, and the other was used as a comparative example every day.
A questionnaire was given three months later after having used it at least once.
In the comparative example, various guava leaves of the production example were replaced with water from the examples. (Comparative Examples 1 and 2) In addition, 14 persons were divided into two groups, and experiments were performed using the following samples.

[0027]

[Table 5] The criteria are as follows, and the results of the questionnaire are summarized in Table 5 below. Example is very good 3 Example is considerably better 2 Example is slightly better 1 No difference 0 Comparative example is slightly better -1 Comparative example is much better -2 Comparative example Is much better -3

[0028]

[Table 6]

[0029]

Industrial Applicability The whitening cosmetic of the present invention has a large whitening effect and inhibits the activity of hyaluronidase. Therefore, hyaluronic acid is stabilized, active oxygen is suppressed, and an antioxidant effect is recognized. And suppress darkening of the skin. Therefore, a whitening cosmetic having excellent softening action while maintaining flexibility and skin luster and abrasion is provided.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification code FI A61P 43/00 111 A61P 43/00 111

Claims (1)

(57) [Claims] 1. A whitening cosmetic comprising a guava leaf solvent extract as an active ingredient.