JPH10236955A - Therapeutic agent for common acne containing adrenocortical steroid as active ingredient - Google Patents

Abstract

PROBLEM TO BE SOLVED: To prepare a therapeutic agent capable of rapidly exterminating common acne by including an adrenocortical steroid therein. SOLUTION: This therapeutic agent for common acne comprises an adrenocortical steroid as an active ingredient. An antimicrobial substance as an auxiliary agent and further a lactic acid fermentation product as an auxiliary ingredient can be contained therein. Cortisone, prednisone, etc., are cited as the adrenocortical steroid and the adrecortical steroid agent is preferably contained in an amount of 0.04-0.07 mg based on 1g base. Although the adrenocortical steroid has hitherto never been used for treating the common acne at all, bacteria on the skin surface and Propionibacterium acnes living in depth can be sterilized to prevent the formation of free fatty acids with the lipase thereof. Thereby, the generation of the common acne can be suppressed. Since the amount of the adrenocortical steroid used is extremely small, there is no fear of inducing infectious diseases or causing other side effect.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a remedy for acne comprising a corticosteroid as an active ingredient, a remedy for acne comprising a corticosteroid as an active ingredient and an antibacterial substance as an adjuvant,
Acne treatments with corticosteroids as active ingredients and lactic acid fermentation products as auxiliary ingredients, and corticosteroids as active ingredients, antibacterial substances as adjuvants and lactic acid fermentation products as auxiliary ingredients. The invention relates to a remedy for acne.

[0002]

2. Description of the Related Art Hitherto, as an acne countermeasure or treatment, an acne remedy for killing bacteria on the surface of skin containing sulfur, resorcin, and phenol as active ingredients has been used.

[0003]

One of the measures against acne is to apply mainly sulfur, resorcinol, phenol, antibiotics and other antibacterial substances to acne to kill bacteria that inhabit the acne epithelium. It has been done by removing. However, their effects were only temporary until the bacteria re-established due to the loss of antibacterial activity, and acne eradication treatment was not possible. As a cause of acne, it is said that lipase produced by bacteria breaks down lipids produced by the grease and the free fatty acids produced cause irritation to human skin. Yes. The present inventor has been working on the development of a method for treating acne whose main function is to suppress the synthesis of a substance that causes acne in ecological tissues and to suppress their secretion, and to treat eczema quickly. Focused on drug development.

[0004]

Means for Solving the Problems A first structure of the present invention is as follows.
It is a remedy for acne, comprising a corticosteroid as an active ingredient. A second aspect of the present invention is a remedy for acne, which is characterized by containing a corticosteroid as an active ingredient and an antibacterial substance as an auxiliary.
A third configuration of the present invention is a remedy for acne characterized by using a corticosteroid as an active ingredient and a lactic acid fermentation product as an auxiliary component, and a fourth configuration of the present invention is effective for using a corticosteroid. An acne remedy characterized by comprising, as an ingredient, an antibacterial substance as an adjuvant and a lactic acid fermentation product as an adjunct ingredient. The corticosteroid used as an active ingredient in the present invention includes, for example, cortisone, cortisol, hydrocortisone, cortisone acetate, cortisone preparations such as hydrocortisone acetate, prednisolone, methylprednisolone, prednisolone sodium succinate, prednisolone acetate, prednisolone butyl acetate and the like , Prednisone, prednisone, methylprednisone, triamcinolone, texamethasone, paramethasone, betamethasone and the like. When applying corticosteroids to acne for acne disease, do one or two or more bactericides or antibacterial substances be used as adjuvants to kill bacteria that inhabit the acne epithelium? Or it is desirable to suppress those activities. The above-mentioned adjuvant also has the function of a bactericide in the conventional acne treatment agent, the antibacterial agent itself, but the combined use of the adjuvant suppresses the acne-suppressing effect of the corticosteroid, which is an active ingredient, with a smaller dose of a corticosteroid. Can be achieved effectively. The bactericide or antibacterial agent can be selected from antibiotics or chemical bactericides that exhibit bactericidal or antibacterial action against bacteria that metabolize secretions including the epithelial steroids. The effect of corticosteroids on the treatment of acne is extremely remarkable and rapid. One of the therapeutic agents of the present invention containing about 2 mg or less of corticosteroids per gram of the base is applied to the epithelium of acne one to two times. Multiple applications often lead to complete healing.
Since Propionibacterium acnes lives as a resident bacterium in the hair funnel, it is considered to be involved in acne development. The lower limit effective dose of the therapeutic agent for acne of the present invention was subjected to a susceptibility test for Propionibacterium acnes, which is considered to be the cause of acne, and as a result, significant results were already obtained in a small amount. Based on this result, the actual therapeutically effective amount of acne patients was traced by a clinical test. As a result, a corticosteroid was used in an amount of 0.02 mg or more, preferably about 0.04 mg / g of the base.
Desirably, it contains 〜0.07 mg.

[0005]

[Action] Conventionally, corticosteroids have never been used in the treatment of acne, and the pharmacological action on acne is not always clear. However, corticosteroids inhabit not only bacteria on the skin surface but also deeply. Propionium acnes (P. acnes) is also sterilized, and the production of free fatty acids by its lipase is prevented, so that it is presumed that acne generation is suppressed.

[0006]

EXAMPLE 1 The present invention will be explained by the results of clinical tests on acne patients. For about 170 test patients, presonisolone 2m was used as a corticosteroid in 1g of the base.
g. A treatment drug in the form of an ointment containing 3 mg of fradiomycin sulfate as an antibiotic was applied to acne once a day. 17
Most of the 0 patients showed a remarkable effect with one application, and the other patients showed a complete therapeutic effect with up to two applications. Almost the same therapeutic effects were observed in clinical trials for acne patients using methylprednisolone and cortisone as corticosteroids. The remedy for acne of the present invention uses a very small amount of corticosteroids, is unlikely to cause infections or cause other side effects, and does not require long-term continuous use. Not at all.

[0007]

[Test example]

Test for susceptibility of Propionibacterium acnes to corticosteroids Subcultured test strains were inoculated into enrichment medium,
After cultivation under anaerobic conditions for 8 hours, the culture solution was adjusted to about 10 ⁶ /
The mixture was diluted with a culture medium for enrichment, and one loopful of cells was transplanted into GAM broth "Nissui Pharmaceutical Co., Ltd." and cultured at 35 ° C. for 24 hours under anaerobic conditions to obtain a bacterial solution for inoculation. The above bacterial solution was dispensed in 15 ml portions to each petri dish containing GAM agar medium “Nissui Pharmaceutical Co., Ltd.” so that the number of bacteria was about 10 ⁶ / ml, and fixed. Then, a test piece containing 5 mg of prednisolone as a corticosteroid per 1 g of the base cream was further added to the same base cream for 1, 7, 28,
A diluted ointment that is serially diluted 280, 2800, 28000 times (active ingredient concentration: 28,000, 4000, 1
000, 100, 10 and 1 ppm).
5 mg of the sample dilution ointment was applied to a dry and heat-sterilized paper disc having a diameter of 10 mm to prepare a test piece. The test piece was placed on the center of the test plate medium so that the coated surface of the test piece was in contact with the surface of the medium, and cultured at 35 ° C. for 48 hours under anaerobic conditions. Table 1 shows the test bacteria p of the test piece.
3 shows the results of an antibacterial activity test on the presence of a halo (growth inhibition zone) against R. ropionobacterium acnes. From the test results, the effective dose of corticosteroids for patients with squirrels was determined. Predinisolone was added to 1 g of an ointment cream as a base at 0.02 m corresponding to the minimum growth inhibitory concentration (dilution factor 280: 5 mg / 280) at which the formation of a halo circle was observed in the sensitivity test.
The acne treatment containing g / g was applied once to the acne. Improvement was observed in 170 patients, but the symptoms were reduced once, but recurred in one week. This application concentration was effective to some extent, but was not always sufficient for some symptoms. . When the same application treatment was performed by further increasing the application concentration of prednidron to 0.04 to 0.07 mg / g, 0.04 mg /
In most cases, a therapeutic effect is obtained by administration of g,
In addition, the above 0.04 mg / g
The same effect as in the case of administration of g was obtained. That is, about one application of 0.04 mg / g gives about 2 mg / g.
As in the following one or two administrations of the active ingredient, a therapeutic effect for acne was observed.

[0008]

[Table 1]

[0009]

According to the first aspect of the present invention, a remarkable therapeutic effect can be obtained by treating a small amount of a corticosteroid with respect to acne which has been difficult to cure. Furthermore, according to the second aspect of the present invention, when an antibacterial agent is used in combination for acne disease, which has been conventionally difficult to cure, a remarkable therapeutic effect can be obtained by a small amount of administration of a corticosteroid and the drug effect period is further extended. be able to. According to the third aspect of the present invention, the combined use of a lactic acid fermentation product for acne can be used for a long time without causing the side effects of corticosteroids. According to the fourth invention, bacteria on the surface of the acne affected area are sterilized, and bacteria inside the skin such as Propionibacterium acnes are also sterilized,
Repairs scars caused by acne, reduces the dose of corticosteroids, produces a remarkable therapeutic effect, prolongs the duration of the drug, and can be used for a long time without causing side effects of corticosteroids .

Claims (4)

[Claims] 1. A remedy for acne comprising a corticosteroid as an active ingredient. 2. A remedy for acne, comprising a corticosteroid as an active ingredient and an antibacterial substance as an adjuvant. 3. A remedy for acne, comprising a corticosteroid as an active ingredient and a lactic acid fermentation product as an auxiliary ingredient. 4. A remedy for acne, comprising a corticosteroid as an active ingredient, an antibacterial substance as an adjuvant, and a lactic acid fermentation product as an auxiliary ingredient.