JP2002332237A - External preparation for skin - Google Patents

Abstract

(57) [Problem] To provide a remedy for acne having a more excellent therapeutic effect. SOLUTION: An external preparation for skin characterized by containing sulfur and a lipase activity inhibitor.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin,
More particularly, the present invention relates to an external preparation for skin which is excellent in treating acne.

[0002]

BACKGROUND OF THE INVENTION Acne (acne vulgaris) begins with the formation of comedones and progresses to inflammation. However, seborrhea in sebaceous follicles, abnormal keratinization of the follicular funnel, It is said that the indigenous bacteria are the factors. Sulfur having a keratin softening action and a bactericidal action is mainly used as a conventional remedy for general external preparations, and an ointment / cream containing a bactericide and an anti-inflammatory agent is often used.

[0003] However, the conventional treatment for acne containing sulfur is not sufficient in its therapeutic effect, and it has been desired to develop a therapeutic agent for acne which is more effective.

[0004]

SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide a therapeutic agent for acne having a better therapeutic effect.

[0005]

Means for Solving the Problems In order to solve the above-mentioned problems, the present inventors have studied in detail the progress of acne development. It was found that free fatty acids generated by decomposition and peroxide of squalene were involved.

[0006] Therefore, in addition to the conventional treatment methods, studies were conducted on the expectation that the therapeutic effect could be enhanced by suppressing the lipase activity that causes the progression of the symptoms. The present inventors have found that a synergistic therapeutic effect on acne can be obtained by using sulfur used in the treatment of acne in combination with a substance having a lipase activity inhibitory effect, and completed the present invention.

That is, the present invention provides a skin external preparation characterized by containing sulfur and a lipase activity inhibitor.

Further, the present invention provides the above-mentioned external preparation for skin, further comprising a medicinal ingredient selected from an antioxidant, an anti-inflammatory agent, a bactericide, a keratolytic agent, and an astringent.

[0009]

BEST MODE FOR CARRYING OUT THE INVENTION The external preparation for skin of the present invention is prepared by mixing sulfur and a lipase activity inhibitor into a usual base for external preparation for skin.

As the sulfur which is the active ingredient of the external preparation for skin of the present invention, sulfur generally used in the treatment of acne can be used, and it is particularly preferable to use precipitated sulfur having a small particle size of sulfur. .

As the lipase activity inhibitor used in the present invention, any substance can be used as long as it can inhibit lipase activity to some extent and has substantially no effect on the skin. Can be. Preferred examples of the lipase activity inhibitor include ibuprofen piconol.

The above-mentioned ibuprofen piconol has been approved in 1990 as a non-steroidal anti-inflammatory component, and comprises a hydrophilic polymer, a non-ionic surfactant, an oily substance, a pH regulator and water, and has a solid form. An external preparation formulated with a base containing no aliphatic higher alcohol is known, and among its indications, acne is also included (Japanese Patent Publication No. 7-35330). However, it has not even been suggested that it has a synergistic therapeutic effect when combined with sulfur.

In the present invention, the content of sulfur in the external preparation for skin is preferably 0.001 to 10% by mass (hereinafter referred to as "%"), particularly preferably 0.01 to 5%. The amount of the lipase activity inhibitor is 0.001 to 0.001 in the external preparation for skin.
10%, particularly preferably 0.01 to 5%.

In the external preparation for skin of the present invention, one or more active ingredients selected from antioxidants, anti-inflammatory agents, bactericides, keratolytic agents, and astringents, in addition to the above-mentioned components, may be used. It is preferable to mix them.

Among these active ingredients, antioxidants include vitamin E and its ester derivatives, vitamin C
Glycyrrhetinic acid and its derivatives, glycyrrhizic acid and its salts, allantoin, epsilon aminocaproic acid, lysotium chloride and the like as anti-inflammatory agents; Chlorhexidine acid, benzalkonium chloride, benzethonium chloride, phenol, hinokitiol and the like can be mentioned. Examples of the keratolytic agent include resorcinol, salicylic acid, and urea, and examples of the astringent agent include zinc oxide and tannic acid.

The skin external preparation of the present invention may further comprise, in addition to the above-mentioned components, components generally used in external preparations, for example, solid / semi-solid / liquid oils, surfactants, alcohols, humectants, preservatives Agents, fragrances, dyes, pH adjusters, stabilizers and the like can also be added.

The dosage form of the external preparation for skin of the present invention may be any form applicable to the outer skin such as cream, ointment, lotion, gel, liniment, patch and powder. . In addition, p of the external preparation for skin of the present invention
H is preferably 4 to 8, more preferably 5 to 7.

[0018]

EXAMPLES include the following Examples and Test Examples illustrate the present invention in more detail, but the present invention should not be construed as being in any way limited by these examples.

EXAMPLE 1 Cream: Sulfur 3 g 2. 2. ibuprofen piconol 3 g Vitamin E 2 g 4. 4. White petrolatum 2 g 5. Polysorbate 60 2 g 6. Sorbitan monostearate 0.6 g 7.cetanol 3 g 8. Medium chain fatty acid triglyceride 5 g Preservative 0.3 g 10. Propylene glycol 10 g 11. Sodium pyrosulfite 0.02 g 12. Carboxyvinyl polymer 0.6 g 13. Purified water qs. Triethanolamine qs 15 Perfume Fine amount Total amount 100 g Component 1 is dispersed in a liquid in which the above components 10 to 13 are dissolved, heated to about 80 ° C, and the above components 2 to 9 are heated and dissolved at about 80 ° C in the oil phase portion. With stirring. With stirring and cooling, components 14 to 15 were added to obtain 100 g of a cream.

[0020] The above components 2 to 6 were heated and dissolved at about 80 ° C. to disperse component 1. Add component 7 while stirring and cooling, and add 100 g.
Ointment was obtained.

Example 3 Lotion: 1. 1 g of sulfur 2. ibuprofen piconol 2 g 0.3 g of vitamin E4. 4. Isopropanol 50 g 5. Hydroxypropyl cellulose 0.6 g Citric acid qs. Sodium citrate qs 8. Purified water qs . Perfume Fine amount Total amount 100 g The above components 1 to 9 were stirred and mixed to obtain 100 g of a lotion.

[0022] The above components 1 to 12 were stirred and mixed to obtain 100 g of a gel.

Example 5 Liniment: 1. Diphenhydramine hydrochloride 1 g 2. Potassium glycyrrhizinate 1 g Sulfur 1 g 4. 4. Ibuprofen piconol 1 g Vitamin E 0.5 g 6. Lidocaine 0.5 g7. 7. Liquid phenol 2 g 8. zinc oxide 10 g 10. Polyoxyethylene hydrogenated castor oil 60 2.5 g10. Propylene glycol 8 g 11. Carmellose sodium 3 g 12. Fine amount of fragrance 13. Purified water qs 100 g The above components 1 to 13 were stirred and mixed to obtain 100 g of a liniment.

Test Example 1 Therapeutic effect on acne vulgaris: A clinical test was carried out using the acne therapeutic agent prepared in Example 1 by the following test method.
The results are shown in Tables 3 to 6.

(Test method) a) Target disease: acne vulgaris that occurred on the face (excluding the area around the eyes and lips) b) Number of cases: 49 cases (including 34 cases of efficacy analysis,
Number of safety analysis cases: 45) c) Administration method: twice a day (morning / evening) Apply appropriate amount to affected area after washing face with soap d) Administration period: 8 weeks (cancel when healing or worsening) e) Observation items … Rash on the face (comedone, papule, pustule)
F) Observation date: Study start date (day 0), 2 weeks (11 days to 17 days)
Days), 4 weeks (25 days to 31 days), 6 weeks (39 days to 45 days)
Sun), 8 weeks (53-59)

G) Evaluation Criteria • Overall Improvement Each day of observation, the residual ratio of the number of eruptions and the degree of remission of the eruptions were determined, and the results were applied to Table 1 below. ). Significant improvement (1) Improvement (2) Slight improvement (3) Unchanged (4) Deterioration (5)-Final overall improvement The same degree of overall improvement was evaluated at the end of the clinical trial (or at the end of the trial).・ Safety At the end of the study (or at the time of the discontinuation of the study), the following four grades (the evaluation points in parentheses) were evaluated. Safe (1) Almost safe (2) There is a problem with safety (3) Not safe (4) ・ Usability Apply the final overall improvement and safety evaluation results to Table 2 below to obtain the following. The evaluation was performed in five stages (the evaluation points in parentheses). Extremely useful (1) Very useful (2) Somewhat useful (3) Neither (4) Not desirable (5)

<Criteria for Evaluation of Overall Improvement>

[Table 1]

<Evaluation criteria for usefulness>

[Table 2]

(Results) <Changes in the number of rashes>

[Table 3]

<Effectiveness (n = 34)>

[Table 4]

<Usefulness (n = 34)>

[Table 5]

<Safety (n = 45)>

[Table 6]

As apparent from the results, the skin external preparation of the present invention had a useful rate of 73.5% for acne and a safety rate of 86.7% during use. In contrast, the useful rate of a preparation containing precipitated sulfur that is already commercially available is 5%.
It is reported to be about 3 to 57%, which indicates that the preparation of the present invention has an extremely excellent therapeutic effect on acne.

[0034]

The external preparation for skin of the present invention contains, in addition to sulfur effective for treating acne, a lipase activity inhibitor to suppress the formation of comedones, which can be said to be the first symptom of acne. Together, they provide excellent acne treatment effects.

Therefore, the external preparation for skin of the present invention can be advantageously used as cosmetics for preventing acne, quasi-drugs, and pharmaceuticals for treating acne. that's all

──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61P 43/00 111 A61P 43/00 111 // C07D 213/30 C07D 213/30 (72) Inventor Kazuki Matsumoto (72) Inventor, Shinichiro Katsuyama 7-204, Naka-ku, Yokohama-shi, Kanagawa Prefecture, Japan 71-204, 72-1-2 Inventor, Yoshikazu Suehiro 17-1-2605, Daikanyamacho, Shibuya-ku, Tokyo 72) Inventor Yoshiyuki Chiba 3-2-67-1 Benten, Urayasu-shi, Chiba (72) Inventor Yuki Sakai 1-20-6, Yotsukaido, Yotsukaido-shi, Chiba F-term (reference) MA02 MA63 NA05 ZA89 ZC20 ZC75 4C086 AA01 AA02 BC17 HA08 MA02 MA04 MA63 NA05 ZA89 ZC20 ZC75

Claims (4)

[Claims] An external preparation for skin, comprising sulfur and a lipase activity inhibitor. 2. The external preparation for skin according to claim 1, wherein the lipase activity inhibitor is ibuprofen piconol. 3. The external preparation for skin according to claim 1, further comprising a medicinal ingredient selected from an antioxidant, an anti-inflammatory agent, a bactericide, a keratolytic agent, and an astringent. 4. The method according to claim 1, which is an agent for preventing and treating acne.
Item 4. An external preparation for skin according to any one of Items 3 to 3.