JP2001206813A - Skin preparation for external use for physical therapy - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a means for preventing and improving pigmentation in cicatrice caused by physical therapy such as surgical therapy and radiotherapy. SOLUTION: This skin preparation for external use such as a cosmetic contains an alkylresorcinol and/or a salt thereof.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to an external preparation for skin, such as cosmetics, for physical treatment such as surgical operation or radiation treatment.

[0002]

2. Description of the Related Art In the field of medical treatment, the problem of maintaining "quality of life" has recently been highlighted, and thus, in the past, surgical resection of breast cancer has been performed. However, in recent years, breast conservative treatment using radiation therapy or chemotherapy has been taken. Under such an ideological background, there is an increasing tendency to make an effort to minimize the influence on the body and the like even in physical treatment such as surgical treatment. Under these circumstances, the most problematic in physical treatment is the formation of scars such as keloid formation and pigmentation. Among such scar formations, in the formation of keloids, substances acting on growth factors and the like have become known,
A clue has been found, but for pigmentation,
There was no clue to the solution. This is because components such as ascorbic acids and glutathiones, which have a melanin production inhibitory effect and are effective for skin pigmentation such as spots, were almost ineffective for pigmentation in scars. That is, although scars generated in physical treatments such as surgical treatments and radiation treatments, means for preventing or improving pigmentation have been demanded, but at present, they have not been obtained.

On the other hand, regarding alkylresorcinols, these substances have a melanin production inhibitory property, are useful for improvement of spots and the like, and have an antibacterial action against microorganisms. Although it was already known to contain it, it was not known at all to be excellent in preventing and improving pigmentation in scars.

[0004]

SUMMARY OF THE INVENTION The present invention has been made under such circumstances, and means for preventing or improving pigmentation in scars caused by physical treatment such as surgical treatment or radiation treatment. The task is to provide

[0005]

In view of such circumstances, the present inventors have eagerly sought a means for preventing or improving pigmentation in scars caused by physical treatment such as surgical treatment or radiation treatment. As a result of research efforts, they have found such effects on alkyl resorcinol and / or its salt, especially 4-n-butyl resorcinol and / or its salt,
The inventor has found that such prevention and improvement can be achieved by including this in an external preparation for skin such as cosmetics and transdermally administering it during physical treatment, thereby completing the invention. That is, the present invention relates to the following technology. (1) A skin external preparation for physical treatment, comprising an alkylresorcinol and / or a salt thereof. (2) alkyl resorcinol and / or a salt thereof is 4-
The skin external preparation for physical treatment according to (1), which is n-butyl resorcinol and / or a salt thereof. (3) The external preparation for skin according to (1) or (2), wherein the physical treatment is one or more selected from surgical incision, surgical resection, radiation therapy, and particle beam therapy. (4) The external preparation for skin according to any one of (1) to (3), which is for preventing or improving scarring caused by physical treatment. (5) The scar is pigmentation, (4)
2. The external preparation for skin according to item 1. (6) (1) to (5) characterized in that it is a cosmetic.
The external preparation for skin according to any one of the above. (7) An agent for preventing scar formation comprising an alkylresorcinol and / or a salt thereof. (8) The scar is pigmentation, (7)
The agent for preventing scar formation according to item 1. (9) When the alkylresorcinol and / or a salt thereof is 4-
The agent for preventing scar formation according to (7) or (8), which is n-butyl resorcinol and / or a salt thereof.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION (1) Alkyl resorcinol and / or a salt thereof, which is an essential component of the skin external preparation for physical treatment of the present invention, is an essential component of the skin external preparation for physical treatment of the present invention. It is characterized by containing an alkylresorcinol and / or a salt thereof. The position of the alkyl group of the alkylresorcinol may be any position as long as there is hydrogen on the aromatic ring in resorcinol, and any of the 2-, 4- and 5-positions is possible, but the 4-position It is particularly preferred to introduce The alkyl group has a carbon chain of 1-2.
0 is preferable, and 1 to 4 are particularly preferable. As the alkyl group, any of a linear group, a group having a branched structure and a group having a cyclic structure are possible, but a linear group is particularly preferable. Such alkyl resorcinols include, for example, 4-methyl resorcinol,
Ethyl resorcinol, 4-propyl resorcinol,
4-n-butyl resorcinol, 4-sec-butyl resorcinol, 4-tert-butyl resorcinol,
4-amyl resorcinol, 4-isoamyl resorcinol, 4-octyl resorcinol, 4-dodecanyl resorcinol, 2-n-butyl resorcinol, 5-n
-Butyl resorcinol and the like. Of this,
Particularly preferred is 4-n-butyl resorcinol and / or a salt thereof. This is because the effect of preventing and improving scarring is particularly excellent. These alkyl resorcinols can be produced according to a conventional method, for example, according to the method described in JP-A-2-49715. That is, a resorcinol and a fatty acid of a carbon chain corresponding to an alkyl group are condensed in the presence of zinc chloride, and zinc amalgam /
Examples thereof include a method of catalytic reduction with hydrochloric acid and a method of condensing resorcinol with a corresponding alcohol having a carbon chain at a high temperature of 200 to 400 ° C. The alkylresorcinol thus obtained can be converted into a salt by reacting it with various alkalis. The salt that can be used as an essential component of the present invention is not particularly limited as long as it is physiologically acceptable. For example, alkali metal salts such as sodium and potassium, and alkaline earth salts such as calcium and magnesium Preferred examples include metal salts, ammonium salts, organic amine salts such as triethanolamine salts and triethylamine salts, and basic amino acid salts such as lysine salts and arginine salts. Among these salts, particularly preferred are alkali metal salts, and among them, sodium salt is particularly preferred. The preferred content of the alkyl resorcinol and / or a salt thereof in the physical external preparation for physical treatment of the present invention is 0.000 relative to the total amount of the external preparation for skin.
The content is 1 to 10% by weight, and more preferably 0.01 to 5% by weight. This is because if the amount is too small, the effect may not be exhibited, and if the amount is too large, the effect may reach a plateau.

(2) External preparation for skin of the present invention The external preparation for skin of the present invention is characterized by containing the above-mentioned alkylresorcinol and / or a salt thereof. here,
The external preparation for skin referred to in the present invention means a general term for those applied externally to the skin, and examples thereof include cosmetics and external medicines for skin, among which cosmetics are particularly preferred. This is because the action of alkylresorcinol and / or a salt thereof, which is an essential component of the external preparation for skin of the present invention, is eased and excellent in safety. The skin external preparation for physical treatment of the present invention comprises the above-mentioned alkylresorcinol and / or
Or, besides its salt, it can contain optional components usually used in external preparations for skin, and such optional components include:
For example, hydrocarbons such as squalane, petrolatum, microcrystalline wax, etc., esters such as jojoba oil, carnauba wax, octyldodecyl oleate, triglycerides such as olive oil, tallow, coconut oil, stearic acid, oleic acid, ritinoleic acid Fatty acids such as oleyl alcohol, stearyl alcohol, higher alcohols such as octyl dodecanol, anionic surfactants such as sulfosuccinates and sodium polyoxyethylene alkyl sulfate, amphoteric surfactants such as alkyl betaine salts, and dialkylammonium salts Such as cationic surfactants, sorbitan fatty acid esters, fatty acid monoglycerides, polyoxyethylene adducts thereof, polyoxyethylene alkyl ethers, polyoxyethylene fatty acid esters, etc. Contains surfactants, polyhydric alcohols such as polyethylene glycol, glycerin and 1,3-butanediol, thickening / gelling agents, antioxidants, ultraviolet absorbers, coloring materials, preservatives, powders, etc. can do. Of these, particularly preferred are polyhydric alcohols. This is because the properties of the skin 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 external preparation for skin. The external preparation 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 emulsion, cream, lotion and gel can be applied, and among these, the form of an emulsion type essence having a high viscosity (viscosity of 1000 to 20,000 centistokes) is used. It is particularly preferred because it is easy to administer locally. The external preparation for skin of the present invention thus obtained has an action of preventing, suppressing, and improving the formation of scars such as pigmentation that occur during surgery or radiation treatment.

[0008]

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 An emulsified high-viscosity essence (cosmetic) as an external preparation for skin of the present invention was prepared according to the following formulation. That is, prescription components a), b) and c) are each heated to 70 ° C, b is added to b and neutralized,
This was gradually added to emulsify, emulsified particles were prepared with a homogenizer, and the mixture was stirred and cooled to obtain an essence. A) Sodium polyacrylate 1 part by weight Acrylic acid / methacrylic acid (C10-30) copolymer (Pemrene TR-2) 0.2 part by weight 1,3-butanediol 7 parts by weight Xanthan gum 0.1 part by weight Ethanol 3 Parts by weight Water 40 parts by weight 4-n-butylresorcinol 0.3 parts by weight b) 10% aqueous solution of potassium hydroxide 0.6 parts by weight Water 31.1 parts by weight C) Squalane 6 parts by weight Jojoba oil 6 parts by weight Vaseline 1. 5 parts by weight Cetanol 1.5 parts by weight Serakyl alcohol 1.5 parts by weight Sucrose fatty acid ester 0.1 parts by weight Monoglyceride stearate 0.1 parts by weight

<Example 2> With respect to the cosmetics of Example 1 described above, the preventive effect of scarring due to surgery was examined using a group of 20 guinea pigs, 5 in total. After shaving the abdomen of the colored guinea pig, the sample was applied 0.1 g each day for 5 days, and a laparotomy / suture operation was performed with a laser knife 72 hours after the final administration. Four weeks later, the lightness difference between the operative site and the non-operative site was measured as a ΔL value using a color difference meter, and the average was determined for each group. The first group was the cosmetic of Example 1, the second group was the cosmetic of Comparative Example 1 in which 4-n-butyl resorcinol of Example 1 was replaced with ascorbic acid, and the third group was the cosmetic of Example 1. n-
Comparative Example 2 in which butyl resorcinol was replaced with glutathione
And the fourth group was the cosmetic of Comparative Example 1 in which 4-n-butylresorcinol of Example 1 was replaced with water. Table 1 shows the results. From this, the cosmetic of the present invention is excellent in the action of preventing scars (pigmentation) caused by surgery and such an action is not recognized in the conventional melanin production inhibitor, so that the cosmetic of the present invention It can also be seen that this is the characteristic of an external preparation.

[0011]

[Table 1]

<Example 3> Using the same protocol as in Example 2, the effect of suppressing scar formation was examined with the administration of the sample being performed 5 days after the operation. Table 2 shows the results. Accordingly, the cosmetic of the present invention is excellent in the action of inhibiting scar formation (pigmentation), and such an action is not recognized in the conventional melanin production inhibitor, and is characteristic of the cosmetic of the present invention. I understand.

[0013]

[Table 2]

<Example 4> Using the cosmetic of Example 1,
The effect of improving scarring was examined in three subjects with marked postoperative scarring (pigmentation). That is, the cosmetics of the present invention were applied to the surgical site of these persons once a day for 30 consecutive days,
The lightness difference (ΔL value) between the operative site and the non-operative site before and after the treatment was measured. Table 3 shows the results. From this, it can be seen that the effect of the cosmetic of the present invention is recognized in all three subjects as in the animal experiment.

[0015]

[Table 3]

Example 5 According to the following formulation, an emulsified high-viscosity essence (cosmetic) as a skin external preparation of the present invention was prepared. That is, prescription components a), b) and c) are each heated to 70 ° C, b is added to b and neutralized,
This was gradually added to emulsify, emulsified particles were prepared with a homogenizer, and the mixture was stirred and cooled to obtain an essence. According to the screening in Example 3, the lightness difference was -0.38.
Admitted. A) Sodium polyacrylate 1 part by weight Acrylic acid / methacrylic acid (C10-30) copolymer (Pemrene TR-2) 0.2 part by weight 1,3-butanediol 7 parts by weight Xanthan gum 0.1 part by weight Ethanol 3 Parts by weight Water 40 parts by weight 4-Isoamyl resorcinol 0.3 parts by weight b) 10% aqueous solution of potassium hydroxide 0.6 parts by weight Water 31.1 parts by weight C) Squalane 6 parts by weight Jojoba oil 6 parts by weight Vaseline 1.5 parts by weight Parts Cetanol 1.5 parts by weight Seraquil alcohol 1.5 parts by weight Sucrose fatty acid ester 0.1 parts by weight Monoglyceride stearate 0.1 parts by weight

Example 6 An emulsified high-viscosity essence as an external preparation for skin of the present invention was prepared according to the following formulation. That is, the prescription components a), b) and c) are each heated to 70 ° C, b is added to b to neutralize, b is gradually added thereto to emulsify, and emulsified particles are prepared with a homogenizer,
After stirring and cooling, an essence was obtained. In this case, a brightness difference of -0.44 was recognized in the screening of Example 3. A) Sodium polyacrylate 1 part by weight Acrylic acid / methacrylic acid (C10-30) copolymer (Pemrene TR-2) 0.2 part by weight 1,3-butanediol 7 parts by weight Xanthan gum 0.1 part by weight Ethanol 3 Parts by weight Water 40 parts by weight 4-Lauryl resorcinol 0.3 parts by weight b) 10% aqueous solution of potassium hydroxide 0.6 parts by weight Water 31.1 parts by weight C) Squalane 6 parts by weight Jojoba oil 6 parts by weight Vaseline 1.5 parts by weight Parts Cetanol 1.5 parts by weight Seraquil alcohol 1.5 parts by weight Sucrose fatty acid ester 0.1 parts by weight Monoglyceride stearate 0.1 parts by weight

<Example 7> Using the cosmetic of Example 6,
Treatment of a person with scars (pigmentation) by radiation therapy (once a day for 30 consecutive days) showed a difference in lightness of-
It improved from -1.1 to -0.76. This shows that the same effect can be obtained even if the length of the alkyl group is changed.

Example 8 An emulsified high-viscosity essence (cosmetic) as a skin external preparation of the present invention was prepared according to the following formulation. That is, prescription components a), b) and c) are each heated to 70 ° C, b is added to b and neutralized,
This was gradually added to emulsify, emulsified particles were prepared with a homogenizer, and the mixture was stirred and cooled to obtain an essence. A) Sodium polyacrylate 1 part by weight Acrylic acid / methacrylic acid (C10-30) copolymer (Pemrene TR-2) 0.2 part by weight 1,3-butanediol 7 parts by weight Xanthan gum 0.1 part by weight Ethanol 3 Parts by weight Water 40 parts by weight 4-tert-butyl resorcinol 0.3 part by weight b) 10% aqueous solution of potassium hydroxide 0.6 part by weight Water 31.1 parts by weight c) Squalane 6 parts by weight Jojoba oil 6 parts by weight Vaseline 1. 5 parts by weight Cetanol 1.5 parts by weight Serakyl alcohol 1.5 parts by weight Sucrose fatty acid ester 0.1 parts by weight Monoglyceride stearate 0.1 parts by weight

[0020]

According to the present invention, it is possible to provide a means for preventing or improving pigmentation in scars which occur during physical treatment such as surgical treatment or radiation treatment.

 ──────────────────────────────────────────────────続 き Continuing from the front page (72) Inventor Yasuhiro Fukuda 27-1, Takashimadai, Kanagawa-ku, Yokohama-shi, Kanagawa Prefecture Inside the Paula Yokohama Research Center (72) Inventor Fukuyoshi Mori 27-1, Takashimadai, Kanagawa-ku, Yokohama-shi, Kanagawa Pref. In-house F term (reference) 4C083 AA122 AB032 AC022 AC072 AC102 AC122 AC422 AC442 AC471 AC472 AD092 AD352 CC02 EE16 EE50 4C206 AA01 AA02 CA19 MA01 NA14 ZA89 ZC80

Claims (9)

[Claims] 1. An external preparation for skin for physical treatment, characterized by containing an alkylresorcinol and / or a salt thereof. 2. The external preparation for physical treatment according to claim 1, wherein the alkyl resorcinol and / or a salt thereof is 4-n-butyl resorcinol and / or a salt thereof. 3. The external preparation for skin according to claim 1, wherein the physical treatment is at least one selected from surgical incision, surgical excision, radiation therapy, and particle beam therapy. 4. The external preparation for skin according to any one of claims 1 to 3, wherein the external preparation is for preventing or improving scars caused by physical treatment. 5. The external preparation for skin according to claim 4, wherein the scar is pigmentation. 6. The external preparation for skin according to any one of claims 1 to 5, which is a cosmetic. 7. An agent for preventing scar formation comprising an alkylresorcinol and / or a salt thereof. 8. The preventive agent for scar formation according to claim 7, wherein the scar is pigmentation. 9. The agent according to claim 7, wherein the alkyl resorcinol and / or a salt thereof is 4-n-butyl resorcinol and / or a salt thereof.