JPS6056921A - Dermatic drug for external application - Google Patents

Abstract

PURPOSE:To provide a dermatic drug for external application, free from hormone-like action, giving mild action to the skin, and having excellent remedying effect to pimples, by using oxendolone known as a remedy for prostatomegamy as an active component. CONSTITUTION:The objective agent for the remedy of pimples is obtained by using oxendolone (16beta-ethyl-17beta-hydroxy-4-estern-3-one) as an active component. The amount of oxendolone is about 0.001-2wt%. It is administered in the form suitable for the application to the skin, e.g. cream, ointment, lotion, etc. The agent may be compounded with an antibacterial agent such as hexachlorophene, vitamin A acid, zinc, keratolytic agent, etc. within a range to keep the effect of the present invention.

Description

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

Acne is a skin disease that mainly occurs during adolescence and is called acne vulgaris, and is clinically defined as ``chronic inflammatory changes that occur in the pores, mainly in the pilosebaceous system.'' The etiology of acne is currently not clear, and although it is a skin disease in which various factors are intricately intertwined, it is generally believed that excessive sebum secretion, hair follicle keratinization, and bacteria within the hair follicle play important roles. Therefore, creams and ointments containing sebum secretion inhibitors, keratolytic agents, and antibacterial substances are commonly used as external medicines for treating acne.

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 adolescents. 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. Furthermore, antibacterial agents such as hexachlorophene, trichlorocarbanilide, and benzalkonium chloride are effective against Propionibacterium acnes (l.
'rop + onibacterium acnas), even though it exhibits extremely high antibacterial activity in vitro.
When actually used in creams, ointments, etc. to treat acne, in most cases they do not exhibit the expected therapeutic effect.

In view of the above circumstances, the present inventors sought to obtain a drug that does not cause hormone-like side effects, is gentle on the skin, and has an excellent acne treatment effect. The inventors have discovered that a known oxendron achieves the above object, and have completed the present invention.

That is, the present invention provides an external skin preparation for treating acne, which contains oxendrone.

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

Oxentro/ used in the present invention has a chemical name of 10β
-Ethyl-17β-Hydroxy Ichiban-estrene-3-
It is a white to pale yellowish-white, odorless powder.

The compounding amount of Oxentro/ is 0 in 1 external preparation for the skin of the present invention.
．． The amount of 001 weight 2iln is about %. 0.001in
The effect of the present invention is not exhibited when Jil% is not grooved. Formulation 1
Although the acne treatment effect is greater as the number of particles increases, about 2 lit% is sufficient.

Next, the results of an acute toxicity test for Oxendo 0/ used in the present invention will be shown.

Unit: s+g/kg In addition to the above-mentioned oxendrone, the skin external preparation of the present invention also contains antibacterial agents such as hexachlorophene, phenol, benzalkonium chloride, cetylpyridinium chloride, undecylenic acid, trichlorocarbanilide, and bithionol. , vitamin A acid, photosensitizer, zarydylic acid, zinc and its compounds, lactic acid and other drugs and keratolytic agents, as well as oils, surfactants, water, ethanol, humectants, thickeners, fragrances, etc. Appropriate amounts of pigments and the like can be added within a range that does not impair the effects of the present invention.

The external skin preparation of the present invention may be in any form that can be applied to the skin, such as cream, ointment, and lawn 2).

The skin external preparation according to the present invention usually has a
It is sufficient to apply about 0.1 to 0.5 g at a time to the eruption-affected area several times a day.

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.

Oxendron 0.25g 1 polyoxyethylene (60
L) Hydrogenated castor oil 2.0 g 1 Glycerin IO, Og.

5.0 g of dipropylene glycol 1o, og, 1,3-zoylene glycol, and 5.0 g of polyethylene glycol 1500 are heated and dissolved at 60°C. To this, 10.0 g of cetyl isooctanoate, 5.0 g of squalane
g and 1.3 g of methylparaben heated and dissolved at <60'C are added and mixed, and treated with a homomixer to form a gel. Next, 0.3 g of carboxyvinyl polymer and 0.03 g of sodium hexametaphosphate were added to this gel.
After gradually adding the solution dissolved in 11.0 g of ion-exchanged water and dispersing with a homomixer, 0.12 g of potassium hydroxide was added.
was dissolved in 40.0 g of ion-exchanged water and mixed, and emulsified with a homomixer to obtain a lotion-type skin preparation for external use.

(Subject of use and observation period) 3,120 men and women between the ages of 15 and 32.

(How to use) After thoroughly washing your face with soap, apply the above lotion-type skin preparation once a day only on the skin eruption.
It was applied ~3 times.

(Observation items and observation ports) Observations were made for the following three symptoms: facets, papules, and Il[, and the severity of each individual finding was graded as high II)' (4) and moderate (4).
3) Evaluation was divided into five stages: slight (slight), slight (I), and none (0). In addition, the severity of acne vulgaris was divided into three levels: severe, moderate, and mild by combining the severity of these three symptoms. Follow-up observation is before treatment, 1 week after treatment, 2 weeks after treatment, and 3 weeks after treatment.
The test was carried out once a week later and once again after 4 weeks.

(Overall improvement level) The degree of improvement in symptoms due to the drug used compared to before use, in 5 levels: markedly relieved (*), considerably relieved (++), somewhat relieved (+), unchanged (±), and worsened (-). divided.

(Effectiveness) Extremely useful (*) in terms of overall improvement level, Kanarii J
It was judged as useful (f), slightly useful (+), and invalid (±).

(Results) The clinical test results of a total of 20 people (3 men and 17 women) were 2 (10%) who said + (slightly effective) and 8 (4) who said 廿 (quite useful).
0%), 8 people (45%) said it was extremely useful, and 1 person (5%) said it was ± (ineffective), proving the effectiveness of the topical preparation of the present invention.

Patent applicant Shiseido Co., Ltd. Takeda Pharmaceutical Forest Company 19 wa

Claims (1)

[Claims] External skin preparation characterized by containing Oxenthro/