JPH0463850B2 - - Google Patents

Description

[Detailed description of the invention]

[B] Purpose of the Invention The present invention is a novel method using water-soluble extracts of safflower, sophia, yangmeipi, renyu, black tea, and green tea, which are selected from medicinal plants (herbal medicines) that have been used in traditional Chinese medicine since ancient times. Regarding whitening cosmetics. [Industrial Application Field] The whitening cosmetic according to the present invention has an effect of inhibiting (suppressing) tyrosinase activity. Therefore, it can be expected to prevent erythema and darkening caused by ultraviolet rays. Furthermore, the extracts obtained from safflower, sophora, yangmeipi, renyu, black tea, and green tea according to the present invention are water-soluble and do not cause precipitation even when used in creams, emulsions, and other transparent liquid cosmetics. It is easy to formulate. [Prior art] There are many examples of cosmetics using extracts from medicinal plants, but there are no known documents that search for tyrosinase activity inhibition and expect skin-whitening effects. For example, there is "Patent Publication No. 52-44375" by the present inventors. According to this, extracts of aloe, pollen, gardenia, mulberry bark, masu hemp, and others,
Extracted and isolated ingredients derived from plants are being applied. Furthermore, recently, “Public Patent Publication 1983-
23612". According to this, application to cosmetics using peonies, peony bark powder, water extraction, or hydroalcoholic extracts thereof is known. On the other hand, in Chinese herbal medicine prescriptions, among the herbal medicines known for their cosmetic effects, those that are said to be particularly effective against age spots include:
Rhizoma, peony, yellow lotus, mountain lily, safflower, licorice, rhubarb,
``Shimonoto with seasoned shoyo mixture: Dangki, Paeonia, Chaihu, Boului,
White 〓, rhizome, river〓, peony bark, mountain radish, licorice, ginger, light weight, ``Keizhi bukurei pill supplemented with yokusojin: yokusojin, keizhi, bouyin, peony bark, peach kernel, ginger'' ``Kojito: There are cinnamon bark, peony, peony bark, peach kernel, peonies, licorice, ginger, "shimotsuto: toki, peonies, river water, and rhizomes," all of which are decoctions or powders, or 30% in water or ethanol. The extract is taken (orally administered) at around 25°C in a solvent containing approximately [Problems to be solved by the invention] Searches have been made for plant extracts that are effective against age spots and freckles. It was not possible to achieve that effect. In view of these circumstances, the present inventors conducted a search for extracts from many medicinal plants that have an effective whitening effect.
For cosmetics, we have been conducting research on extracts with excellent stability over time. As a result, we picked up plants that had particularly prominent tyrosinase activity inhibitory effects, and finally we were able to select the medicinal plants shown in Table 1.

【table】

[Table] [Summary explanation of tyrosinase activity inhibition test method] L-tyrosine (1.0 mg/ml)...0.5 ml M/15 phosphate buffer (pH6.8)...2.0 ml Various crude drug extracts of the present invention...1.0 ml 1% copper sulfate solution 0.05ml Tyrodinase (potato) 5mg/ml ...2.0ml Measurement was performed by incubating in a constant temperature bath at 37.5℃ for 60 minutes, then measuring the absorbance at 640nm, and using a blank (water).
The tyrosinase activity inhibition rate of each extract was determined by comparing the absorbance with the absorbance. Comparison of activity inhibition was evaluated by 50% inhibition rate (ID ₅₀ ). Next, based on the results shown in “Table-1”,
When confirming the strength of the tyrosinase activity inhibition effect, it was confirmed that the strength of the effect was influenced by the difference in extraction solvent. Therefore, the present inventors further determined how to find extracts from plants selected according to "Table 1" that have a strong tyrosinase activity inhibitory effect and at the same time have good stability after being incorporated into cosmetics. I have focused my research on whether it is best to obtain the best possible results. The results showed that when the extract obtained by the extraction method shown in the following example is used in cosmetics, there is very little generation of scum and precipitate.
It was also found that it can be used in liquid water-based cosmetics. [B] Structure of the Invention The present invention further investigated the extraction solvent and concentration from the famous plants finally picked up in Table 1, and found that the immersion method is not suitable for extraction with water alone. be the best. On the other hand, when extracting with a lower alcohol solvent, the best method is the cold immersion method using ethanol, methanol, or n-pronol. When looking at these from the viewpoint of tyrosinase activity inhibition effect, when using a lower alcohol solvent, one or more of ethanol, methanol, and n-propanol are mixed to one part of water, It was found that the water-soluble extract extracted by the cold steeping method in a mixed solution with a lower alcohol mixing ratio of 1 was generally advantageous. [Means for Solving the Problems] Specific examples will be described below based on examples. Example 1 Based on safflower, sophora, yangmeipi, renyu, black tea, and green tea, one part of one of them, or one part of a mixture of one or more of them, Water is added in a proportion of 8 parts and digestion is carried out for a limited period of 8 hours at a temperature of 80-100°C. This digestion is repeated twice, and the resulting leachate is taken out and the water is distilled off using an evaporator, yielding 0.13 to 0.15 kg of water-soluble extract per 1 kg of raw material. Example 2 From the same plant group as used in Example 1, part 1
Take out the seeds or one or more kinds arbitrarily, and add 8 parts of ethanol, methanol, or n-propanol to 1 part of the seeds, or add 2 parts of ethanol, methanol, or n-propanol to 1 part of the seeds.
Add 8 parts of a solution containing any mixture of seeds or more, and heat at 5°C.
Cold soak twice for 4 days each at a low temperature of ~10°C. When the solvent is distilled off from the obtained leachate using an evaporator, 0.1 to 0.25 kg of water-soluble extract is obtained per 1 kg of the raw material plant. Example 3 From the plant groups used in Examples 1 and 2, one or more types were arbitrarily selected and made into one part of water and lower alcohols as shown in Table 2. 8 parts of the mixed solution of 1 to 7 were added, cold immersion was carried out twice in the same manner as in Example 2, and the resulting leachate was distilled off to remove the solvent using an evaporator. On the other hand, 0.19～
0.29Kg of water-soluble extract is obtained.

[Effect]

The water-soluble extracts obtained in Examples 1 to 3 above all have a tyrosinase activity inhibitory effect,
If we look at the effects of extracts from one type of these plants, they are almost the same as in Table 1. In addition, a mixed (composite) extract of one or more plants exhibits an inhibitory effect (ID ₅₀ ) value of about 0.2 to 400. However, even when these various plants were extracted in a mixed manner, the inhibitory effect did not show particularly strong numerical values. On the other hand, when using methanol, the yield tends to be higher than when using other extraction solvents. However, as the methanol content becomes higher in concentration, the extracted extract tends to eventually precipitate in an aqueous system. Note that this is ethanol, n-
This is a common point in the cold immersion extraction method using propanol alone. Furthermore, in aqueous systems, the solvents from which a large amount of insoluble extracts were extracted were methanol, n-propanol, and ethanol. However, it was found that the inhibitory effect on tyrosinase activity was also observed in extracts that showed precipitation over time after being dissolved in water. Therefore, all of the water-soluble extracts obtained by the methods shown in Examples 1 to 3 can be incorporated into cosmetics, but in the case of transparent water-based products, Example 1 or Example 3 It was found that the extract obtained in Example 2 is advantageous because it causes less sludge, and that the extract obtained in Example 2 is sufficient for creams and milky lotions that use emulsifiers (dispersants). In addition, with the product obtained in Example 2, the occurrence of sludge is naturally not observed in products that contain a high ethanol content, such as aerosol type products, lotions with a high ethanol concentration, or hair products. Easy to mix into products. The product obtained in Example 3 can be used in a wide range of products without any restrictions, including products that do not use dispersants, such as products with high alcohol content and transparent liquid products, as well as creams and milky lotions. Furthermore, the water-soluble extracts obtained in Examples 1 to 3 can also be used by being added to the formulation of pharmaceuticals, health foods, and the like. For example, it can be easily used in the formulation of beverage-type liquid products and external preparations, and can also be easily incorporated into powders, tablets, granules, and the like. It is unclear whether the water-soluble extracts obtained in Examples 1 to 3 can be administered orally (ingested) to produce whitening effects, or at least for external application, the hair on the backs of mice must be shaved. When the epidermis is irradiated with ultraviolet rays, the incidence of erythema is 0.3%.
Concentrations containing the above tend to be suppressed. In other words, the next step in suppressing erythema caused by sunlight is to progress to the darkening phenomenon, but rapid erythema causes erythema, etc., but it is fully expected that this can be prevented. It is something. Note that water-soluble extracts made from plant mixtures (compounds) exhibit stronger erythema suppressive effects. In addition, from the numerical values related to the tyrosinase activity inhibitory effect in the previous table "Table 1", and in terms of the relationship with the erythema suppressive effect, those with a remarkable erythema suppressive effect are:
There is a tendency for this to be observed more often in those with a low tyrosinase activity inhibitory effect (ID ₅₀ ) value. When applied to cosmetics, the effectiveness of suppressing erythema can vary depending on the selected plant, its extraction solvent, and whether it is soaked hot or cold. As a result, extracts extracted by cold soaking using a water-digested extract or a 1:1 mixture of lower alcohol and water have a low level of erythema suppressing effect as well as tyrosinase activity inhibiting effect. Compared to alcohol extracts,
It was found that overall good results were obtained. However, there were exceptions in which extracts from rhizoma were found to have an erythema-suppressing effect, even if they were extracted using lower alcohols. It is speculated that this is probably due to the transfer of other anti-inflammatory substances other than the tyrosinase activity inhibitor through lower alcohol extraction. Furthermore, from the perspective of the tyrosinase activity inhibiting effect, the temperature conditions in the digestion or cold soaking methods should be adjusted to 80 to 100°C as shown in Example 1 when extracting with water alone. The (ID ₅₀ ) value is low, and at temperatures below 30°C, an extract that shows almost no inhibitory effect on tyrosinase activity can be obtained. or,
In terms of yield, digestion at 80-100°C is particularly high compared to other temperature conditions. On the other hand, the relationship with temperature when extracting with lower alcohol is as shown in Examples 2 and 3.
Extracts obtained at ~10°C are preferable in terms of yield;
Extraction at a temperature higher than this increases the yield of crude extract, but increases the generation of scum and precipitates over time, making purification such as filtration difficult. Prescription example 1

[Lotion]

Ethanol…8.0% Lactic acid…0.2% Citric acid…0.8% Sorbitsu or UBC Liquid* …5.0% *Acidic mucopolysaccharide-containing extract Aqueous extract according to Examples 1 to 3...0.3 to 0.5% Flavoring agents and preservatives (appropriate amount) Make the total volume 100 with purified water. Prescription example 2

[Milky lotion]

Whale wax…3.0% Beeswax…14.0% Liquid paraffin…45.0% Aqueous extract according to Examples 1 to 3...3.0 to 5.0% Setanol…3.0% Borax…1.0% Fragrances and preservatives…0.5% Make the total volume 100 with purified water. Prescription example 3

[Vanishing cream]

Stearic acid…6.5% Sorbitan monostearate…14.0% Polyoxyethylene sorbitan monostearate
...2.0% Polpylene glycol ...2.0% Aqueous extracts according to Examples 1 to 3 ...0.3 to 5.0% Flavors and preservatives ... Bring the total amount to 100 with an appropriate amount of purified water. Prescription example 4

[Cold cream]

Beeswax…11.0% Ceresin…15.0% Vaseline…6.5% Liquid paraffin…19.0% Rice germ oil (Oryza oil S-1)…11.0%* Aqueous extract according to Examples 1 to 3...3.0% Fragrances and preservatives…appropriate amounts Make the total volume 100 with purified water. Prescription example 5

[Foundation cream]

Liquid paraffin…24.0% Lanolin…10.0% Solid paraffin…5.0% Sorbitan sesquioleate…4.0% Pigment…35.0% Silkgen G powder (silk protein)
...3.0% Aqueous extract according to Examples 1 to 3 ...5.0% Flavors and preservatives ... Make the total amount to 100 with an appropriate amount of purified water.

Claims (1)

[Claims] 1. 6 of safflower, sophora, yangmeipi, renyu, black tea, and green tea.
Based on starting materials limited to types, one of them
Using 8 parts of water for 1 part of the type alone or 1 part of a mixture of one or more types in any weight,
immersion under heating at 80 to 100°C, or
In advance, the mixing ratio of water and one or more lower alcohols among ethanol, methanol, and n-propanol is 1:1.
Using 8 parts of the mixed solution at a ratio of 1 part to 5 to
A whitening cosmetic characterized by containing a water-soluble extract obtained by soaking at a low temperature of 10°C.