JPH043363B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to an external skin preparation for treating acne containing chlormadinone acetate. Acne is a skin disease that primarily 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. ing. Therefore, creams and ointments containing sebum secretion inhibitors, keratolytic agents, and antibacterial substances are commonly used as external medicines for acne treatment. 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 have extremely high antibacterial activity in vitro against Propionibacterium acnes, an acne bacterium resident on the skin. However, when it is actually used in creams, ointments, etc. to treat acne, in most cases it does 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 acne treatment effect, and as a result, chlormadinone acetate achieved the above objectives. The present invention was completed based on this discovery. That is, the present invention provides an external skin preparation for treating acne, which contains chlormadinone acetate. The configuration of the present invention will be explained in detail below. Chlormadinone acetate used in the present invention has the following structural formula: It is a white to pale yellowish-white, odorless powder. The blending amount of chlormadinone acetate is approximately 0.001 to 2% by weight in the skin external preparation of the present invention. If the amount is less than 0.001% by weight, the effects 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 chlormadinone acetate, the skin external preparation of the present invention includes antibacterial agents such as hexachlorophene, phenol, benzalkonium chloride, cetylpyridinium chloride, undecylenic acid, trichlorocarbanilide, and bithionol, vitamin A acid, and photosensitive Although it varies depending on the substance, salicylic acid, zinc and its compounds, drugs such as lactic acid, keratolytic agents, and properties, the main ingredients include oil, surfactants, water, ethanol, humectants, thickeners, fragrances, and pigments. They can be blended as appropriate within a range that does not impair the effects of the invention. The skin external preparation 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 may be applied to the skin affected area in an amount of 0.1 mg to 0.5 g at a time, usually once to several times a day, depending on the symptoms. Next, the effects of the present invention will be explained in more detail by giving clinical examples. (Drug used) A lotion-type skin external preparation obtained by the following formulation and manufacturing method was used. Chlormadinone acetate 0.25g, polyoxyethylene (60mol) hydrogenated castor oil 2.0g, glycerin
10.0g, dipropylene glycol 10.0g, 1,3
- Dissolve 5.0 g of butylene glycol and 5.0 g of polyethylene glycol 1500 by heating at 60°C.
To this, 10.0 g of cetyl isooctanoate, 5.0 g of squalane and 1.3 g of methylparaben were added to the same 60 g.
The mixture is heated and dissolved at ℃, added and mixed, and treated with a homomixer to form a gel. Next, 0.3g of carboxyvinyl polymer and 0.03g of sodium hexametaphosphate dissolved in 11.0g of ion-exchanged water were gradually added to this gel, and after dispersing with a homomixer, 0.12g of potassium hydroxide was dissolved in 400g of ion-exchanged water. The mixture was added and mixed and emulsified using a homomixer to obtain a lotion type skin preparation for external use. (Targets used and observation period) A total of 20 men and women aged 15 to 32. (How to use) After thoroughly washing the face with cosmetic soap, the above-mentioned lotion type skin preparation was applied 1 to 3 times a day only on the skin eruption. (Observation items and observation date) Observe the three symptoms of comedones, papules, and pustules, and rate the severity of each finding as high (4) or moderate (3).
The evaluation was divided into five levels: mild (2), slight (1), 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 was performed before treatment, 1 week, 2 weeks, 3 weeks, and 4 weeks after treatment. (Overall improvement level) The degree of improvement in symptoms due to the drug used compared to before use was divided into 5 levels: markedly relieved (), considerably relieved (), somewhat relieved (+), unchanged (±), and worsened (-). . (Usefulness) Based on the overall degree of improvement, it was judged as extremely useful (), quite useful (), somewhat useful (+), and ineffective (±). (result)

[Table] The clinical test results for a total of 20 people, 3 males and 17 females, were positive.
4 (20%) said it was (somewhat useful), 7 (35%) said it was (very useful), and 8 (40%) said it was (very useful).
%), ± (ineffective) for 1 person (5%), proving the effectiveness of the skin external preparation of the present invention.

Claims (1)

[Claims] 1. A skin external preparation for treating acne characterized by containing chlormadinone acetate.