JPS6028918A - Dermatic drug for external application - Google Patents

Abstract

PURPOSE:To provide the titled drug containing 5,6-dimethyl-8-isopropenylbicyclo [4,4,0]decen-1-one-3, free from 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% 5,6-dimethyl-8- isopropenylbicyclo[4,4,0]decen-1-one 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. 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 of applying to the rash.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a government topical preparation for treating acne, which contains 5,6-dimethyl-8-impropenylbicyclo[number, number, 0] desenate-3.

Acne is a skin H9 disease that mainly occurs during adolescence.The name of the disease is ``Zabu vulgaris,'' and it is clinically defined as ``chronic inflammatory changes that occur in the upper foramen, mainly in the anterior sebaceous gland system.'' There is. 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, anterior keratosis, and anterior epidermis bacteria play important roles. It is considered. 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 hexachlorocarbane, trichlorocarbanilide, and penzalkonium chloride are effective against Propionibacterium acnes (P.
Even if it exhibits extremely high antibacterial activity in vitro (against acne), when it is actually mixed into creams, ointments, etc. and used to treat acne, most of the time it does not exhibit the expected therapeutic effect. .

In view of the above circumstances, the present inventors conducted repeated research into 5,6-dimethyl-8-in to obtain a drug that has hormone-like side effects, is gentle on the skin, and has an excellent effect on treating acne. propenylbicyclo(4,4,0)decene-
Found that 1-on-3 achieves the purpose stated in -,
The present invention has now been completed.

That is, the present invention provides an external film preparation for treating acne, which is prepared by combining 5,6-dimethyl-8-impropenylbicyclo(4,4,O]decen-1-one-3.

The configuration of the present invention will be described below.

5,6-dimethyl-8-impropenylbicyclo(4,4,0)decen-1-one-3 used in the present invention is
It is a compound having the following structural formula, and is a white to pale yellow-white, odorless powder.

5.6-dimethyl-8-impropenylbicyclo(4,
The blending amount of 4,0) decen-1-one-3 is approximately 0.001 to 2% by weight in the skin external preparation of the present invention. 0.00
The effect of the present invention will not be exhibited if the concentration is less than 1%. The larger the amount added, the greater the therapeutic effect on animals, but about 2% by weight is sufficient. The government external preparation of the present invention includes the above-mentioned 5, 6-
Dimethyl-8-impropenylbicyclo[4,4,0)
In addition to decen-1-one-3, antibacterial agents such as hexachloro7e7, phenol, be/sarkonium chloride, cedylpyrazinium chloride, undecylenic acid, trichloroI'l carbalide, and bidet A-nol , vitamin A acid, photosensitizer, zarydylic acid, zinc and its compounds, drugs such as lactic acid, keratolytic agents, and properties.
Oil, surfactant, water, ethanol, humectant, thickener,
Fragrances, pigments, etc. can be added to the barrel chamber as long as they do not impair the effects of the present invention.

The external film preparation of the present invention may be in any form such as cream, ointment, lotion, etc. as long as it can be used on the skin for a long time.

Depending on the disease, the film preparation for external use according to the present invention may be used for i'i
l~several times a day, 1111 ni, +[-0.5g
Just apply it to the affected area of f'Z skin eruption.

Next, clinical examples will be given to further demonstrate the effects of the present invention.
Explain to u.

(Drug used) A skin external preparation of Lawn 9 Fukuibu obtained by the following formulation and manufacturing method was used.

5.6-dimethyl-8-imp 11 penylbisic IJ (
0.25 gt poly of 4,4,0) decene-1-3]
Porin Edge ν7 (6 (H le) 8! Kahimashiura 2.Og,
Glycerin IO, Og, dipropylene glycol 10-
5.0 g of Ogx 1,3-butylene glycol and 5.0 g of polyethylene glycol 1500 are heated and dissolved at 60°C. In this, carboxyvinyl polymer 0,3
g dissolved in 43.0 g of ion-exchanged water was added and mixed, and emulsified with a homomixer to obtain a skin-like external preparation such as a lotion.

(Subject of use and observation period) A total of 20 men and women between the ages of 15 and 32.

(Method of Use) After thoroughly washing the face with a cosmetic soap, the above-mentioned Locilitative Dermatological Treatment 1 preparation was applied only on the eruption 1 to 3 times a day.

(Observation items and observation points) Observe the three symptoms of skin irritation, papules, and IC4 symptoms, and rate the severity of each finding as severe (4), moderate (3), mild (2), slight (1), or none. The evaluation was divided into five stages: 0). In addition, the severity of acne vulgaris was divided into three levels: severe, moderate, and sucrose syndrome based on the severity of these three symptoms. Follow-up observations were made before 'Rj treatment, and 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, divided into 5 levels: markedly relieved (111), considerably relieved (slightly relieved (+), unchanged (±), worsened (-)). Ta.

(Utility) Based on the overall degree of improvement, it was judged as extremely effective (+H), weakly useful (+), somewhat useful (slightly useful), and ineffective (±).

(Results) The clinical test results of 8,120 people, 4 men and 16 women, were 4 (20%) for + (for a little A1), 8 (40%) for 2 (for Kana Lij), + ( 6 people (30%) found it extremely useful
, ± (ineffective) was given by 2 people (10%), proving the effectiveness of the government topical preparation of the present invention.

Patent applicant: Shiseido Co., Ltd. Procedural amendment (spontaneous) September 1, 1983 1, Indication of the case, Patent Application No. 138339, 1982, 2, Name of the invention: External skin shavings 3, Person making the amendment: 4, Column 5 for detailed description of the invention of the subject of amendment. Contents of the amendment (1) On page 6, lines 2 and 3 of the specification, the phrase “carboxy” was replaced with “cetylisooctanony 1.I
O, Og, squalane 5.0g and methylparaben 1
．． 3g of the same solution was heated and dissolved at 60°C, added and mixed, and treated with a homomixer to form a gel. Next, add carboxy to this gel first.

(2) 0.3 g of r and 0.3 g of sodium hexametaphosphate in the third line of page 6 of the specification.
03g dissolved in 11.0g of exchanged water was added to the stem.
After dispersing with a homomixer, add 0.12 g of potassium hydroxide and correct it.

(3) Specification page 6, lines 3 to 4 [ion exchange water 43
, ``OgJ'' should be corrected as ``ion-exchanged water 40.OgJ.''

Claims (1)

[Claims] 5,6-dimethyl-8-impropenylbicyclo(4,4,0)deton-1-one- represented by the following structural formula
A skin external preparation characterized by containing 3.