JPS6028924A - External preparation for skin - Google Patents

Abstract

PURPOSE:An external preparation for the skin having no side effect like hormone, mildness to the skin, useful for remedying pimples, containing 4-androsten- 3-one-17beta-carboxylic acid ester. CONSTITUTION:An external preparation for the skin having 0.001-2wt% 4-androsten-3-one-17beta-carboxylic acid ester shown by the formula which is white or light yellowish white, and odorless powder. It is further properly blended with an antibacterial agent such as hexachlorophene, phenol, etc., vitamin A acid, photosensitizer element, salicylic acid, oily component, perfume, etc., and made into cream, ointment, lotion, etc. It is applied usually 1-several times daily, in an amount about 0.1mg-0.5g each time.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an external skin preparation for treating acne, which contains nisder 4-androsten-3-one-17β-carboxylate.

Acne occurs mainly during adolescence and is called acne vulgaris by the government, and is clinically defined as ``chronic inflammatory changes that occur in the name tag, mainly in the anterior sebaceous gland system.'' The etiology of acne is still unclear, and although it is a disease caused by a complex interplay of various factors, it is generally believed that excessive sebum secretion, hyperkeratosis, and epidermal bacteria play important roles. There is. Therefore, creams and ointments containing sebum shunt inhibitors, keratolytic agents, and antibacterial substances are commonly used as external medicines for treating acne, depending on various factors.

However, existing anti-acne drugs containing various drugs have various drawbacks. For example, for women who are using a 1t/J drug to increase sebum production; 1; Lumon suppresses the growth of the epidermis and reduces the secretion of sebaceous glands, but the side effects caused by hormonal drugs are favorable for adolescent men and women. isn't it. Further, sulfur and sulfur compounds such as selenium disulfide, which are typical examples of keratolytic agents, do not have hormone-like side effects, but there are many cases where people complain of skin irritation, dry skin, etc. when used repeatedly. In addition, antibacterial agents such as hexachlorophenylene, trichlorocarbanilide, and penzalkonium chloride are effective against the acne-prone skin disease Propionibacterium acnes (Propionibacterium acnes).
Even if they exhibit extremely high antibacterial activity against cncs) in vitro, when they are actually incorporated into creams, ointments, etc. and used to treat acne, most of them do not exhibit the expected therapeutic effect.

In view of the above circumstances, the present inventors conducted intensive research to obtain a drug that does not have hormone-like side effects, is gentle on the skin, and has an excellent therapeutic effect on 4-androstene. 3-one-17β-carboxylic acid ester is
! i! [We have found that one objective can be achieved and have completed the present invention.

That is, the present invention provides an external skin preparation for treating acne, which contains Nisder 4-androstene-3-olylphenol-β-carboxylate.

The configuration of the present invention will be explained in detail below.

4-androsten-3-one-1 used in the present invention
7β-carboxylic acid ester is a compound having the following drawing 2 〇-OR, and is a white, completely pale yellowish white, odorless powder.

The blending amount of 4-androsten-3-one-17β-carboxylic acid ester is 0.001 to 0.001 in the government external preparation of the present invention.
It is about 2% by weight. If the amount is less than 0.001% by weight, the effects of the present invention will not be exhibited. The larger the amount added, the greater the acne treatment effect, but approximately 2N1'r amount % is sufficient. The skin external preparation of the present invention includes -1-4-androstene-3
In addition to -one-17β-carboxylic acid esters, antibacterial agents such as hex-su-chlorophene, )tinol, penzalkonium chloride, cetylpyridinium chloride, undecyle/acid, trichlorocarbanilide, and bithionol, and vitamin A acid , photosensitizers, salicylic acid, zinc and its compounds, drugs such as lactic acid, keratolytic agents, and although they vary depending on the properties, flexibilities, surfactants, water, ethanol, humectants, thickeners, fragrances, pigments, etc. They can be blended as appropriate within a range that does not impair the effects of the present invention.

The external preparation for skin of the present invention may be in any form as long as it can be applied to the skin, such as cream, ointment, and lotion.

The topical preparation for skin according to the present invention depends on the symptoms, but usually 1.
Approximately 0.1 to 0.5 g may be applied to the affected area of the skin once to several times a day.

Next, the effects of the present invention will be explained in more detail by giving clinical examples.

(Drug used) An external skin preparation of rJ-Shikunquip obtained by the following formulation and manufacturing method was used.

0.25 g of 4-androsten-3-one-17β-nonorboxylic acid ester 1 polyoxyethylene (60 L) hydrogenated castor oil 2.0 gs glycerin + 0.0 gs dipropylene glycol 10.0 g, 1.3-butylene glycol + 7 coles 5, 0 g s and 5.0 g of Polynib-Astragalus IJ Cole 1500 are heated and dissolved at 60°C.

Add and mix 0.3 g of 1τ xyvinyl polymer dissolved in 43.0 g of ion-exchanged water, emulsify with Homo Miki No. 1, and make V-John type skin disease Jr.
l six lI i5.

(Subject of use and observation period) A total of 20 men and women between the ages of 16 and 30.

(How to use) After thoroughly washing your face with a cosmetic stone boat, apply the above-mentioned one-skin type external skin preparation once a day only to the soil of JK eruption.
~Apply 3 times.

(Observation items and observation ports) Observations were made for the three symptoms of skin irritation, papules, and impetigo, and the severity of each finding was evaluated as severe (4), rliv (3), mild (2), and minor (1). ), 0), 5 steps ζ: minute ()
It was evaluated. In addition, the severity of these three symptoms is combined to indicate the severity of S-sexual sedentary symptoms: severe, moderate j+'+i, and drop Y.
The disease was divided into three stages. Follow-up was before treatment, lr; treatment 1
Weeks later, 2 weeks later, 3 weeks later, 4i! ! I went to each session after the interval.

(Overall improvement level) The degree of improvement in barking due to the drug used compared to before use, 5 levels: markedly improved (World), considerably improved (H), somewhat improved (+), unchanged (±), and worsened (-). Divided into.

(Utility) Based on the overall degree of improvement, it was judged as extremely useful (H4), quite useful (+1), somewhat useful (+), and ineffective (±).

(Results) The clinical test results for 20 people, 2 males and 18 females, were +(
5 people (25%) said it was somewhat useful, and 7 people said it was useful.
Name (35%), # (for very good 1゛) is 7 active club X)
, ± (ineffective) was given by 1 person (5%), proving the effectiveness of the external film preparation of the present invention.

Patent Applicant: Shiseido Co., Ltd. Procedural Amendment (Voluntary) September 1988 Case 1 1. Indication of the case: 1981 Provisional Application No. 138342 2. Name of the invention: Skin external preparation 3. Person making the amendment: 4. Detailed description of the invention in the specification to be amended 5. Contents of the amendment (1) On page 6, lines 4 to 5 of the specification, the phrase “carboxy” was replaced with “cetyl inoctanony” 110
, Og, squalane 5.0g and methylparaben 1.
3g of the same was heated and melted at 60°C, added and mixed, and subjected to homomixir treatment to form a gel. Next, this gel is first corrected with carboxy.

(2) Specification page 6 line 5 r 0.3g ion
Toai) Potassium hydroxide O,1 after dispersing with a fir tree
First, I corrected the 2g by saying, ``Imen''.

(3) Specification, page 6, line 5 [ion exchange water 43. hJ
It says, ``-Ion-exchanged water 40.OT!J'' is corrected first.

Claims (1)

[Claims] A film external preparation characterized by containing androstene-3-one-17β-carboxylic acid ester according to the following Mizozo formula: