JPH072640A - External preparation for protecting ultraviolet disorder - Google Patents

Abstract

PURPOSE:To obtain the subject external preparation containing p- hydroxybenzaldehyde as an active ingredient, capable of preventing skin disorder caused by ultraviolet exposure, useful for beauty culture and prevention of sunburn by mixing with a cosmetic base, an ointment, etc. CONSTITUTION:p-Hydroxybenzaldehyde of the formula is used as an active ingredient, mixed with a polyoxyethylene hardened castor oil, ethanol, citric acid, sodium citrate, 1,3-butylene glycol, an antiseptic, a perfume, purified water, etc., uniformly stirred, blended, dissolved and pharmaceutically manufactured into a lotion, etc., to give the objective external preparation capable of protecting various organism disorders caused by ultraviolet exposure, useful for beauty culture, prevention of sunburn, chapped skin, etc.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an external preparation for protecting various biological disorders caused by exposure to ultraviolet rays, which is compounded in a cosmetic base or an ointment and is useful for whitening, sunburning, preventing rough skin, etc. Is.

[0002]

2. Description of the Related Art In recent years, various obstacles to human skin due to exposure to ultraviolet rays have become a problem. Usually, most of the ultraviolet rays that humans receive are sun rays. And the ultraviolet rays contained in this sunlight and reaching the ground are 290 to 32
320nm with 0nm medium wavelength ultraviolet ray (hereinafter referred to as UVB)
It can be roughly classified into 400 nm long-wavelength ultraviolet light (hereinafter referred to as UVA). UVB causes acute inflammation (erythema) and sun-burn on human skin,
It is also considered to be a major factor responsible for the generation or exacerbation of spots and freckles, as well as the cause of skin cancer, and its protective measures have been investigated from an early stage. Regarding UVA, the effect on human skin was thought to be about primary blackening (Suntaning), but the UVA irradiation dose on the ground surface was UV.
As a result of the recent confirmation that it reaches about 15 times that of B and reaches the inside of the dermis, UVA causes microchronic changes in elastic fibers in the blood vessel wall and connective tissue, leading to aging of the skin. With the introduction, it has been expected that it will cause an increase in the UVB irradiation effect, and there has been great interest in UVA protection measures.

As the conventional means for protecting ultraviolet rays, the use of ultraviolet absorbers (sunscreen agents) is the most common.
However, although these UV absorbers are used for the purpose of preventing UV rays from reaching the skin, it is actually difficult to completely block UV rays. For this reason, methods for preventing the UV damage of the skin itself are being sought.

From the recent research results, it has come to be considered that the above-mentioned skin damage due to ultraviolet rays is largely caused by the oxidation of skin lipids due to ultraviolet rays. Therefore, the idea of using an antioxidant to alleviate skin damage caused by ultraviolet rays was proposed. Of course, various antioxidants have been conventionally blended in cosmetics and the like, but these are usually for the purpose of preventing the oxidation of oil and fat components contained in the cosmetic itself. Moreover, butylhydroxyanisole (B
Although synthetic antioxidants such as HA) and butylhydroxytoluene (BHT) have excellent general antioxidant ability, their purpose and amount are strictly limited from the viewpoint of safety.
On the other hand, natural antioxidants such as α-tocopherol, which is less problematic in terms of safety, can be expected to have antioxidant ability against oils and fats such as foods, but are said to have extremely low UV damage-protecting ability. Therefore, it is desired to develop a UV-protective agent derived from a natural product, which is less problematic in terms of safety.

[0005]

SUMMARY OF THE INVENTION The present invention has been made in view of the above circumstances, and its object is excellent stability and safety, can be used as an external preparation, and is excellent in UV damage. It is to provide a drug having a protective effect.

[0006]

The external agent for protecting against UV damage of the present invention, which has been able to solve the above problems, is characterized in that it contains p-hydroxybenzaldehyde as an active ingredient.

[0007]

The present inventors have conducted various studies on external preparations for protection against UV damage and found that p-hydroxybenzaldehyde suppresses peroxidation of skin lipids, which is said to be the primary cause of various skin damage caused by UV irradiation. It was Further, they have found that this compound has an excellent effect of protecting against ultraviolet rays and is excellent in stability and the like when compounded as an external preparation in a cosmetic base, an ointment base or the like, and thus completed the present invention.

[0008] p-Hydroxybenzaldehyde is a compound which is present in small amounts in various plants, and has an anti-cancer effect (Japanese Patent Laid-Open No. 5-58200).
5-51018) and the like are known. Its acute toxicity LD ₅₀ is 4000 mg / kg body weight (rat, oral). The method for producing p-hydroxybenzaldehyde is not particularly limited. For example, as a chemical synthesis method, Reim
er Tiemano method, electrolytic reduction method and the like can be adopted.

The external preparation of the present invention is used for the purpose of preventing UV damage, in addition to cosmetics such as creams, lotions, packs, powders and foundations, pharmaceuticals such as emulsions, lotions and ointments. It can be formulated into various external forms such as quasi-drugs, and the bases, excipients, stabilizers, pigments, fragrances, preservatives, sequestering agents, organic acids, etc., which are commonly used in each formulation, can be added appropriately. Good. In addition, in order to further enhance the effect of protecting against UV damage, it is of course effective to add a UV blocker or UV absorber.

The content of p-hydroxybenzaldehyde varies depending on the form of use, purpose of use, method of use, dosage form and the like. For example, 0.001 to 3% (by weight, the same applies hereinafter) for cosmetics and 0. It is from 01 to 10%.

[0011]

The present invention will be described in more detail with reference to the following examples, but the following examples are not intended to limit the present invention, and all modifications can be made without departing from the spirit of the preceding and the following. It is included in the technical scope of the present invention. Example 1 Representative formulation examples using the external preparation for ultraviolet ray protection of the present invention are listed, but of course the present invention is not limited thereto.

<Lotion> Part by weight • Polyoxyethylene hydrogenated castor oil 1.0 • Ethanol 15.0 • Citric acid 0.1 • Sodium citrate 0.3 • 1,3-Butylene glycol 4.0 • p- Hydroxybenzaldehyde 0.05 ・ Preservative proper amount ・ Perfume trace amount ・ Purified water Residual components were uniformly stirred, mixed and dissolved to obtain a lotion.

<Ointment> Parts by weight (A) • Polyoxyethylene sorbitan monostearate 1.0 • Polyoxyethylene sorbit tetraoleate 1.5 • Self-emulsifying glyceryl monostearate 1.5 • Salix beeswax 2. 0-paraffin 2.0-stearic acid 3.0-hevenyl alcohol 3.0-shea butter 12.0-liquid paraffin 5.0-methyl polysiloxane 0.01-p-hydroxybenzaldehyde 0.5-preservative proper amount・ Small amount of fragrance (B) ・ 1,3-butylene glycol 5.0 ・ Citric acid 0.3 ・ dl-lauroyl-L-sodium glutamate 0.5 ・ Purified water The components belonging to the residual (A) are dissolved by heating, Separately, the components belonging to (B) were dissolved by heating (oil phase) (aqueous phase). The aqueous phase was added to the oil phase, and the mixture was stirred and emulsified and then cooled to obtain an ointment.

<Test Example 1> Method for evaluating mid-wavelength ultraviolet (UVB) damage protection activity Method by Namiki et al. (Journal of Agricultural Food Chemistry (J. Agric. F)
good Chem. ), 35, 808, 1987
500 μl of rabbit red blood cell membrane solution (2 mg / ml as the protein concentration) prepared according to the above (1 year), and an appropriate amount of the test substance is added thereto. And 2 medium wavelength ultraviolet (UVB)
After irradiation with 0 J / cm ² (2.5 mW / cm ² , 133 minutes), 2M trichloroacetic acid / 1.7M hydrochloric acid solution and 0.67% thiobarbituric acid / 4 mM sodium hydroxide solution were added, and 100 ° C. Incubate for 15 minutes. Then, the reaction solution is cooled to room temperature and then centrifuged at 3000 rpm for 15 minutes, and the absorbance of the supernatant at 535 nm is measured. The lipid peroxidation inhibition rate (%) is calculated by the following formula from the difference between this absorbance and the control which is not irradiated with medium wavelength ultraviolet (UVB). In addition, FL for Toshiba is used for UVB irradiation.
A 20S-E ultraviolet lamp (maximum emission wavelength 313 nm) was used. Peroxide inhibition rate (%) = [1-{(A _{535 of} test substance)-
C2} / {C1-C2}] × 100, where C1: medium wavelength ultraviolet (UVB) irradiation control A ₅₃₅ C2: medium wavelength ultraviolet (UVB) non-irradiation control A
_{Represents 535} .

The inhibition rate (%) of lipid peroxidation was plotted against the concentration of the test substance, and the concentration giving a lipid peroxidation inhibition degree of 50% was determined by IC ₅₀ (Inhibited conceal).
(Translation of 50%, μg / ml), and the strength of the activity was compared at this value.

Using p-hydroxybenzaldehyde as the test agent and BHA and α-tocopherol as the comparative agents, the protective activity against mid-wavelength ultraviolet rays was evaluated according to the above evaluation method. The test was carried out by adding p-hydroxybenzaldehyde at a final concentration of 25, 12.5, 6.
As a result of measuring the mid-wavelength ultraviolet ray protective activity by changing it in 6 steps of 3, 3.1, 1.6 and 0.8 μg / ml, IC
₅₀ was 8.6 μg / ml. The results are shown in Figure 1 and Table 1.

[0017]

[Table 1]

As is apparent from Table 1, the protective activity against p-hydroxybenzaldehyde in the medium wavelength ultraviolet ray is BHA.
Although it is lower than (IC ₅₀ : 2.0 μg / ml), it has about 7 times the activity as compared with α-tocopherol (IC ₅₀ : 60 μg / ml).

[0019]

The present invention is configured as described above,
From a new viewpoint completely different from the conventional ultraviolet absorber (sunscreen agent), it has become possible to provide an ultraviolet damage protector capable of alleviating and suppressing the skin damage itself caused by UV exposure.

[Brief description of drawings]

FIG. 1 is a graph showing the relationship between the concentration of a test substance and the protective activity against medium wavelength ultraviolet rays.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁶ Identification number Internal reference number FI Technical indication location A61K 31/11 ADA 9454-4C (72) Inventor Yoshimasa Takahara 1-25 Kannondai, Tsukuba-shi, Ibaraki No. 14 Stock Company Kobe Steel Works Tsukuba Research Area

Claims (1)

[Claims] 1. An external preparation for protecting against UV damage, which comprises p-hydroxybenzaldehyde represented by the following formula as an active ingredient. [Chemical 1]