JPS6028919A - Dermatic drug for external application - Google Patents

Abstract

PURPOSE:To provide the titled drug containing tocopherylquinone, free from the hormone-like side effects, and having mild effect to the skin and excellent remedying effect to pimple. CONSTITUTION:The titled dermatic drug for the remedy of pimple and having the above effects is prepared by compounding about 0.001-2wt% tocopherylquinone of formula in a drug for external application, e.g. cream, ointment, lotion, etc. The drug may contain, in addition to the above component, an antibacterial agent such as hexachlorophene, a drug such as vitamin A acid, a photosensitive compound, salicylic acid, zinc or its compound, lactic acid, etc., a kelatolytic agent, etc. and if necessary, an oil, a surface active agent, water, ethanol, a humectant, a thicknener, a perfumery, a pigment, etc. to an extent not to lower the above effect. The rate of application depends upon the symptom, however, usually about 0.1mg-0.5g per dose and one-several doses a day by applying to the rash.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an external skin preparation for treating acne containing tocopherylquinone.

Acne is a governmental disease that mainly occurs during adolescence, and is called acne vulgaris, and clinically it is defined as ``chronic inflammatory changes that occur in the name tag, mainly in the sebaceous gland system.'' Acne The etiology is currently not clear (a variety of factors are involved in 'IJ',
Although it is a film disease that is intertwined with H., it is generally believed that excessive sebum secretion, anterior epikeratosis, and anterior superior bacteria play important roles. Therefore, creams and ointments containing sebum secretion inhibitors, keratolytic agents, and antibacterial substances are commonly used as external medicines for the treatment of red kites.

However, existing anti-acne drugs containing various drugs have various drawbacks. For example, female hormones, which are sebum secretion inhibitors, suppress the growth of the epidermis and reduce the secretion of sebaceous glands, but the side effects caused by hormones are not desirable for adolescent men and women. In addition, sulfur and sulfur compounds such as selenium disulfide, which are typical examples of keratolytic agents, do not have hormone-like side effects, but when used repeatedly, there are many cases of complaints of irritation, dryness of the skin, etc. Furthermore, antibacterial agents such as hexachlorophene, trichlorocarbanilide, and benzalkonium chloride are effective against Propionibacterium acnes, which is a skin-resident acne bacterium.
), even if they exhibit extremely high antibacterial activity 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 circumstances of the article, the present inventors sought to obtain a drug that does not have hormone-like side effects, is gentle on the skin, and has excellent acne treatment effects. We have discovered that the above objective [1] can be achieved, and have completed the present invention.

That is, the present invention provides an external skin preparation for acne treatment J11 containing tocopheryl tonone.

The construction of the present invention will be described below.

The tocopherylquinone used in the present invention is a compound having the following structural formula, and is a light yellowish white and odorless powder.

The blending amount of tocopherylquinone is 0.001 to 2% by weight f5 degrees in the external preparation of the present invention. o, oo1 heavy view%
If it is less than that, the effect of the present invention will not be exhibited. The larger the amount, the greater the acne treatment effect, but about 2% by weight is sufficient.

In addition to the above-mentioned tocopherylquinone, the skin external preparation of the present invention includes anti-C2, such as hexachlorophene, phenol, penzalconium chloride, cedylpyridinium chloride, undecylenic acid, trichlorocarbanilide, and videonol. I agents, vitamin A acid, photosensors, salicylic acid, zinc and its compounds, lactic acid and other drugs and keratolytic agents,
Oil, surfactant, water, ethanol, humectant, thickener, fragrance, pigment, etc. may be appropriately incorporated within the range that does not impair the effects of the present invention, although these may vary depending on the properties.

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 a cream, ointment, or lotion.

The external preparation for skin according to the present invention can be applied to the affected area of skin eruption, depending on the symptoms, but it is usually applied to the affected area of skin eruption once to several times a day, at a time of about 0.5 mm.

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

(Medicine used) A lotion-type skin external preparation obtained by the following formulation and manufacturing method was used.

Tocopherylquinone 0.25g, Polio toshechile 7
(00t) hardened castor ura 2. Og1 Grease Serif
10.0c1 dipropylene glycol fO,og11
．． 3-butylene glycol 5.0g% right and 5. Og polyethylene glycol 1500 is heated and dissolved at 60°C. Add and mix 0.3 g of carboxyvinyl polymer dissolved in 43.0 g of ion-exchanged water 1,1.
It is emulsified with Fir Toza to create a lotion-type skin preparation for external use.

(Subject of use and observation period) 2,120 men and women between the ages of 15 and 30.

(How to use) After thoroughly washing the face using cosmetic stone M, the above-mentioned ``1-shicon type skin external preparation'' was applied 1 to 3 times a day only on the skin eruption.

(Observation items and observation points) Observations were made for the three symptoms of skin irritation, papules, and M-yaku, and the severity of each finding was classified as severe (4), moderate (3), and mild (
2)1. The evaluation was divided into five levels: slight (1), none (0). In addition, the severity of sitting vulgaris was divided into three levels: severe, moderate, and mild based on the severity of these three symptoms. Follow-up observation was performed before treatment, 1 week, 2 weeks, 3 weeks, and 4 weeks after treatment.

(General improvement lf) The degree of improvement in symptoms due to the drug used compared to before use was divided into 5 levels: markedly relieved (Kare), considerably relieved (#), somewhat relieved (+), unchanged (±), and worsened (-). Min IJ.

(Usefulness) From the overall level of improvement, it is extremely useful (ina) to quite useful (
Juice), somewhat useful (+), and ineffective (±).

(Results) The clinical test results for a total of 20 people, 3 men and 17 women, were 4 (20%) positive (somewhat useful) and 8 positive (20%).
40%), bone (very useful), 7 (35%), ±(
There was one patient (5%) who said "ineffective", demonstrating the effectiveness of the government's topical preparation of the present invention.

Patent Applicant: Shiseido Co., Ltd.: 〒1'子子-ito-ri1machi-j-[υt(r”1 其 訳）Showa 5) (September 14-Tl -11°:2.＼・ Japan Patent Office Director-General Kazuo Wakasugi (1) Indication of the case 1983 Application No. 1383439) (2) Name of the invention: Skin shavings for external use (3) Detailed explanation of the invention in the specification (5) , Contents of the amendment (1) Page 5 of the specification, lines 11 to 12, 1 - ``carboxy'' was replaced with ``1 to 1000 g of cetyl isooctanocony, 5.0 g of squalane, and 1.3 g of methylvarahene. The same mixture heated and dissolved at <60°C is added and mixed and treated with a homomixer to form a gel.Next, this gel is first corrected with carboxy.

(2) Specification page 5 line 12 r0.3g ion
As stated, rO, 3g and sodium hexametaphosphate 0
．． 03H'l・Ion was dissolved in 11.0 g of exchanged water and added.
After dispersing with a homomixer, 0.12 g of potassium hydroxide was corrected as ``ion''.

(3) Page 5 of the specification, lines 12 and 13, 1-・Ion exchange water 43, Ogj is replaced with [Ion exchange water 40. (f
With J? Ili if(L, Saizu.

Claims (1)

[Claims] External skin preparation characterized by containing tocopherylquinone