JP2001322990A - Active oxygen scavenger and composition containing the same for erasing active oxygen - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an active oxygen scavenger excellent in active oxygen erasing capacity against active oxygen, especially, hydroxy radical, and a composition such as a cosmetic, a food or a medicine containing the active oxygen scavenger. SOLUTION: Ascorbic acid, an ascorbic acid derivative or its salt which is excellent in hydroxy radical erasing activity is added to a cosmetic, a food or a medicine.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an active oxygen scavenger and a composition containing the active oxygen scavenger for scavenging active oxygen.

[0002]

2. Description of the Related Art The generation of active oxygen in a living body has important physiological activities such as elimination of foreign substances and removal of pathogenic microorganisms, but also causes tissue damage, inflammation and aging. It has various adverse effects on living organisms, and its control is an important theme in maintaining normal life activity. In particular, there is no effective erasing means for the generated hydroxyl radical other than in vivo elimination by SOD (superoxide dismutase), and among active oxygen erasing abilities, it is desired to develop an active oxygen scavenger having excellent active oxygen erasing ability for hydroxy radicals. Was rare. Furthermore, it has been pointed out that such active oxygens are a cause of these diseases in inflammation such as atopic dermatitis and chemical hypersensitivity, for which the cause and treatment method have not been determined. Recognition is shared that controlling active oxygens so that they do not occur excessively in the living body is important for efficient elimination and control of the active oxygens in suppressing the onset of such diseases. Furthermore, wrinkles caused by excessive irradiation of the skin with light and the like are caused by direct effects of active oxygen, such as hydroxy radicals and hydrogen peroxide, caused by light irradiation on skin tissues and inflammation caused by light irradiation. It is thought to work synergistically and does not adversely affect inflammation,
It has been recognized that active oxygen scavengers having an effect of suppressing inflammation are extremely useful materials, but materials having such characteristics have not yet been found.

On the other hand, it has never been known that ascorbic acid, an ascorbic acid derivative, or an active oxygen scavenging agent such as a hydroxyl radical or hydrogen peroxide is eliminated.

[0004]

DISCLOSURE OF THE INVENTION The present invention has been made under such circumstances, and an active oxygen scavenger having excellent active oxygen scavenging ability, particularly an active oxygen scavenging ability for hydroxyl radicals, and a composition containing the same. An object of the present invention is to provide a composition such as a cosmetic, a food, or a pharmaceutical.

[0005]

In view of such circumstances, the present inventors have made intensive research efforts in search of an active oxygen scavenging agent having excellent active oxygen scavenging ability, particularly an active oxygen scavenging ability for hydroxy radicals. It has been found that ascorbic acid, ascorbic acid derivatives or salts thereof have an active oxygen scavenging action such as a hydroxyl radical. As a result of further studies, they have found an excellent active oxygen scavenging effect on compositions containing these ascorbic acids, such as cosmetics, foods and pharmaceuticals, and have completed the invention. That is, the present invention relates to the following technology. (1) An active oxygen scavenger comprising ascorbic acid, an ascorbic acid derivative or a salt thereof. (2) The active oxygen scavenger according to (1), wherein the ascorbic acid derivative is magnesium ascorbate phosphate. (3) The active oxygen scavenger according to (1), wherein the ascorbin derivative is ascorbic acid glucoside. (4) for erasing hydrogen peroxide,
(1) The active oxygen scavenger according to any one of (1) to (3). (5) A composition for scavenging active oxygen, comprising the active oxygen scavenger according to any one of (1) to (4). (6) The composition for eliminating active oxygen according to (5), which is a cosmetic. (7) being applied to an inflammatory site, (5)
Or the composition for eliminating active oxygen according to (6). Hereinafter, the present invention will be described in detail focusing on embodiments.

(8) The composition for erasing active oxygen according to any one of (5) to (7), which is for preventing wrinkle formation due to light.

DESCRIPTION OF THE PREFERRED EMBODIMENTS (1) Active oxygen scavenger of the present invention The active oxygen scavenger of the present invention comprises ascorbic acid, an ascorbic acid derivative or a salt thereof. Derivatives of ascorbic acid include glycosides such as glucoside, maltoside, riboside, deoxyriboside, and arabinoside, acetylated products of ascorbic acid or ascorbic acid glycosides, acylated products such as formylated products, lauroylated products, methylated products, and ethylated products. Preferred examples include alkylated compounds such as compounds. Of these derivatives, glycosides are particularly preferred, and glucosides are commercially available, and the use of these is particularly preferred in terms of availability and active oxygen scavenging effect. These ascorbic acid and ascorbic acid derivatives can be used as they are or as salts. Any salt can be used without particular limitation as long as it is physiologically acceptable. For example, alkali metal salts such as sodium and potassium, alkali metal salts such as calcium and magnesium, ammonium salts, and triethanolamine And organic amine salts such as triethylamine, and basic amino acid salts such as lysine and arginine. Among them, magnesium ascorbate is magnesium ascorbate in terms of availability or use. These ascorbic acids,
Both ascorbic acid derivatives and their salts have excellent active oxygen scavenging action, especially excellent hydroxy radical scavenging action. The active oxygen scavenger of the present invention may contain only one kind, or may contain two or more kinds in combination. When the active oxygen scavenger of the present invention is contained in a composition, the preferred content is 0.001 to 10
%, More preferably 0.01 to 5% by weight.

(2) The active oxygen scavenging composition of the present invention is characterized by containing the active oxygen scavenging agent of the present invention. Preferred examples of the composition for scavenging active oxygen of the present invention include skin external preparations such as foods, pharmaceuticals, and cosmetics. Among them, cosmetics can be exemplified as a suitable composition. This means that the dermal toxicity of the active oxygen scavenger of the present invention is extremely low,
This is because hydroxy radicals appear in the skin at sites such as inflammation and have an undesired effect on the skin, and the effect of eliminating them in the skin is extremely large. Particularly, in the case of cosmetics, administration of such an active oxygen scavenger to an inflamed site is particularly preferable since it exerts an action of suppressing inflammation. Examples of such inflammation include sun burns, atopic dermatitis, chemical sensitivity, and the like.

The composition of the present invention may contain, in addition to the active oxygen scavenger of the present invention, optional components usually used in foods, medicines or cosmetics. As such optional components, in the case of foods and orally administered drugs, excipients, coating agents, binders, disintegrants, lubricants, bulking agents, coloring agents, stabilizers, emulsifiers, dispersants, and the like can be preferably exemplified. And topical skin medicines, hydrocarbons such as squalane, petrolatum, microcrystalline wax, jojoba oil, carnauba wax, esters such as octyldodecyl oleate, triglycerides such as olive oil, tallow, coconut oil, stearin Acid, oleic acid, fatty acids such as ritinoleic acid, oleyl alcohol, stearyl alcohol,
Higher alcohols such as octyldodecanol; anionic surfactants such as sulfosuccinates and sodium polyoxyethylene alkyl sulfate; amphoteric surfactants such as alkyl betaine salts; cationic surfactants such as dialkylammonium salts; sorbitan fatty acids Nonionic surfactants such as esters, fatty acid monoglycerides, their polyoxyethylene adducts, polyoxyethylene alkyl ethers, polyoxyethylene fatty acid esters, and polyhydric alcohols such as polyethylene glycol, glycerin, and 1,3-butanediol , A thickening / gelling agent, an antioxidant, an ultraviolet absorber, a coloring material, a preservative, a powder, and the like. Among these, particularly preferred are polyhydric alcohols in skin external preparations such as cosmetics and skin external pharmaceutical compositions. This is because the properties of the skin, whose barrier function has been impaired by inflammation, can be preferably maintained. The preferred content of these polyhydric alcohols is 0.5 to 10% by weight, more preferably 1 to 5% by weight, based on the total amount of the cosmetic. It is also very advantageous to include a conventionally known anti-inflammatory component in order to effectively suppress the inflammation that has already occurred. As such anti-inflammatory component, anti-inflammatory agents such as indomethacin, suprofen, ketoprofen, ketotifen and the like can be suitably exemplified in the case of crude drug components such as birch extract and burdock extract, and external medicines for skin. The preferred content of the components is 0.001 to 1% by weight,
A more preferred content is 0.01 to 0.1% by weight.
The external preparation for skin such as the cosmetic and the external medicine for skin of the present invention can be produced by treating such essential components and optional components according to a conventional method. As the dosage form of the external preparation for skin of the present invention, any of emulsions, creams, lotions, and gels can be applied.
(000-20,000 centistokes) An emulsified type of essence is particularly preferred because it is easy to administer locally. The skin external preparation for use in the presence of inflammation of the present invention thus obtained has an action of relieving inflammation caused by active oxygen generated in the body such as atopic dermatitis and chemical hypersensitivity. It has the effect of preventing, suppressing and improving the care of the underlying skin and the sedation of such inflammation. Further, it is possible to prevent wrinkles and loss of elasticity caused by inflammation caused by such active oxygen.
In addition, active oxygen and inflammation have a particularly favorable preventive effect on wrinkles caused by irradiation with light in which synergism is involved in their formation. A preferred optional component of the composition for oral administration is an enteric coating agent capable of maintaining the action time of the active oxygen scavenger of the present invention, and such a coating agent is an extract of lac shell shellworm. Zein which is an insoluble protein contained in grains such as shellac, wheat and corn is preferably exemplified. The preferred content of these is 20 to 50% by weight based on the total amount of the composition. Such a composition for oral administration can also be produced by treating an arbitrary component and an essential component according to a conventional method.

[0009]

EXAMPLES Hereinafter, the present invention will be described in more detail with reference to Examples, but it goes without saying that the present invention is not limited to only these Examples.

<Example 1> (Erasing activity of hydroxy radicals of ascorbic acids)
Hydroxy radical scavenging activity was examined using ascorbic acids, which are active oxygen scavengers of the present invention. That is, iron sulfate (0.01 mM; 45 μl) -hydrogen peroxide (0.1
mM, 45 μl), ascorbic acids were added at different doses to the hydroxy radicals generated in the system, and the amount of hydroxy radicals eliminated by this was measured by the ESR spin trap method (trapping agent; DMPO).
An IC50 value was calculated from a plot of the erased value and the dose.
Table 1 shows the results. This indicates that ascorbic acids, which are the active oxygen scavengers of the present invention, are excellent in the action of scavenging hydroxy radicals among the excellent active oxygen.

[0011]

[Table 1]

Example 2 Five groups of hairless mice were used to examine the effect of ultraviolet rays on the formation of wrinkles in a wrinkle model. That is, a hairless mouse was prepared by adding 0.1 ml of a 50% aqueous ethanol solution containing 0.1% of the active oxygen scavenger of the present invention.
After coating and processing, the amount of ultraviolet light (B
(LB lamp; manufactured by Toshiba Corporation). This work
Performed 24 times at a rate of 5 times / week for 24 weeks, and the state of wrinkles on the skin was compared with the average level of the control group that was irradiated with ultraviolet rays and was not subjected to sample administration.
+: Clearly reduced wrinkles are recognized, ±: Somewhat less wrinkles are felt,-: Evaluated based on the same level of wrinkles. Table 2 shows the results. This indicates that the active oxygen scavenger of the present invention and the ultraviolet wrinkle model have an effect of preventing wrinkle formation.

[0013]

[Table 2]

Example 3 Effect on Inflammation Hartley white guinea pig (female, 300 to 350)
g) The back of 60 animals was shaved, and an irradiation site of 3 cm × 3 cm was provided. Was irradiated with ultraviolet light to cause inflammation. (M
24 hours after the irradiation) The skin reaction was evaluated 24 hours after irradiation by the criteria of Draize (++: reaction with edema, +: reaction with obvious erythema, ±: reaction with weak erythema,
−: No response), and 25 + animals having almost the same response level were selected. The selected animals were divided into 5 groups of 5 animals, one group containing 0.05 ml of a 50% ethanol solution containing 0.1% by weight of ascorbic acid, and the other group containing 0.1% by weight of magnesium phosphate ascorbate 50% by weight. 0.05 ml of an ethanol solution and 0.05 ml of a 50% ethanol solution containing 0.1% by weight of ascorbic acid glucoside for the third group,
Four groups received 0.05 ml of 50% ethanol at each irradiated site. Twenty-four hours after administration, the skin reaction was determined again based on the Draize standard. The results are shown in Table 3 as the number of appearance cases. This indicates that the active oxygen scavenger of the present invention tends to suppress inflammation. Therefore, it can be seen that administration of the active oxygen scavenger of the present invention to an inflamed site does not worsen inflammation, and that administration to such an inflamed site is possible.

[0015]

[Table 3]

Example 4 A lotion was prepared according to the following formulation. That is, the ingredients were stirred and solubilized at room temperature to obtain a lotion. Using this lotion, one panel of three panelists suffering from wrinkles for a year was used twice a day for one month in the morning and evening to evaluate the effect of preventing and improving the wrinkles.
The evaluation criteria are rating 2: marked improvement, rating 1: obvious improvement, rating 0.5: slight improvement, rating 0: no improvement. The average score was 0.91. It was recognized that the lotion containing the hydroxy radical scavenger of the present invention was effective in improving wrinkles. Ascorbic acid 0.1 parts by weight 1,3 butanediol 5 parts by weight Glycerin 3 parts by weight Sodium citrate 0.1 parts by weight Methylparaben 0.2 parts by weight Ethanol 8 parts by weight Water 83.7 parts by weight

Example 5 A lotion was prepared according to the following formulation. That is, the ingredients were stirred and solubilized at room temperature to obtain a lotion. Using this lotion, one panel of three panelists suffering from wrinkles for a year was used twice a day for one month in the morning and evening to evaluate the effect of preventing and improving the wrinkles.
The evaluation criteria are rating 2: marked improvement, rating 1: obvious improvement, rating 0.5: slight improvement, rating 0: no improvement. The average score was 0.71. It was recognized that the lotion containing the hydroxy radical scavenger of the present invention was effective in improving wrinkles. Ascorbic acid glucoside 0.1 parts by weight 1,3 butanediol 5 parts by weight Glycerin 3 parts by weight Sodium citrate 0.1 parts by weight Methylparaben 0.2 parts by weight Ethanol 8 parts by weight Water 83.7 parts by weight

Example 6 A pharmaceutical composition for external use on the skin was prepared according to the following formulation. That is, the prescription components were stirred and dispersed to obtain a skin external preparation. It showed a remarkable effect on atopic dermatitis. Magnesium phosphate ascorbate 0.1 part by weight Prednisolone 1 part by weight Vaseline 98.9 parts by weight

<Example 7> According to the following formula, a health food in the form of a sugar-coated tablet was prepared. That is, the part (a) was subjected to fluidized-bed granulation and then tableted to give an uncoated tablet. This was coated with enteric coating (b) and sugar-coated with the component (c) to prepare a food. A Hydroxypropyl cellulose 10 parts by weight Ascorbic acid 1 part by weight Chorei extract 1 part by weight Royal jelly 1 part by weight Lactose 37 parts by weight Shellac 20 parts by weight Ethanol 1980 parts by weight C Sucrose 25 parts by weight Gelatin 5 parts by weight

Example 8 According to the following formulation, a health food in the form of a sugar-coated tablet was prepared. That is, the part (a) was subjected to fluidized-bed granulation and then tableted to give an uncoated tablet. This was coated with enteric coating (b) and sugar-coated with the component (c) to prepare a food. I Hydroxypropylcellulose 10 parts by weight Ascorbic acid glucoside 1 part by weight Chorei extract 1 part by weight Royal jelly 1 part by weight Lactose 37 parts by weight Lo shellac 20 parts by weight Ethanol 1980 parts by weight C sucrose 25 parts by weight Gelatin 5 parts by weight

[0021]

According to the present invention, there is provided an active oxygen scavenger excellent in active oxygen scavenging ability, in particular, an active oxygen scavenging ability for hydroxyl radicals, and a composition such as cosmetics, food or medicine containing the same. can do.

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Claims (8)

[Claims] 1. An active oxygen scavenger comprising ascorbic acid, an ascorbic acid derivative or a salt thereof. 2. The method according to claim 1, wherein the ascorbic acid derivative is magnesium ascorbate.
The active oxygen scavenger according to the above. 3. The active oxygen scavenger according to claim 1, wherein the ascorbic acid derivative is ascorbic acid glucoside. 4. The active oxygen scavenger according to claim 1, which is used for scavenging hydroxyl radicals. 5. A composition for scavenging active oxygen, comprising the active oxygen scavenger according to any one of claims 1 to 4. 6. The active oxygen scavenging composition according to claim 5, which is a cosmetic. 7. The composition for scavenging active oxygen according to claim 5, wherein the composition is applied to an inflamed site. 8. The composition for erasing active oxygen according to claim 5, wherein the composition is for preventing wrinkle formation due to light.