JPS6133116A - External preparation for skin disease - Google Patents

Abstract

PURPOSE:The titled external preparation containing a compound such as cetraxate, etc. CONSTITUTION:An external preparation for skin diseases containing a compound shown by the formula (n is 0-6). The compound shown by the formula consists of cis and trans geometrical isomers. Especially a trans form (cetraxate) of the compound where n=2 is used as an improved remedy for gastritis and gastric ulcer by oral administration through pharmaceutical action such as improvement in very small blood circulation of gastric mucosa, suppression of pepsinogen in the mucosa, suppression of gastric juice secretion by antikallikrein action, etc. Zona, pemphigus vulgaris, pustular proriasis, cust, eczema nummulare, decubitus, burn, impetigo, skin moniliasis, athlete's foot, hydroa, atopic dermatitis, etc. may be cited as the skin diseases to which the external preparation is applied. An ointment, cream, lotion, etc. may be cited as the dosage form. Administration may be carried out by applying proper amounts two-three times a day.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Utilization Decomposition] The present invention is a compound of the formula (I) H2N cH2Q c oo% (ch ). 0OOH
The present invention relates to an external preparation for skin diseases containing a compound represented by (n means an integer of θ to 6) or a salt thereof.

The compound represented by formula (I) consists of cis and trans geometric isomers, and in particular, the trans isomer of the n-2 compound (common name: cetraxate) improves microblood circulation in the gastric mucosa when administered orally. .

Suppresses the activation of pepsinogen within the mucous membrane.

It is used as an excellent therapeutic agent for gastritis and gastric ulcers due to its pharmacological effects such as suppressing gastric juice secretion through its anti-kallikrein effect. [Effects of the Invention] The present inventors have been working diligently to find new uses for the compound of formula (I). As a result of investigation, it is effective against various skin diseases.

The present invention was completed by discovering that the compound of formula ff) exhibits excellent therapeutic effects when applied as an external preparation.

The skin diseases to which the external preparation of the present invention is applicable include herpes zoster, herpes vulgaris, psoriasis psoriasis, 2111 psoriasis, nummular eczema, decubitus sores, burns, and pyorrhea.

Examples include cutaneous candidiasis, albinism, aqueous dermatitis, and atopic dermatitis.

In the treatment of these diseases, the dosage form of the external preparation of the present invention may be an oil-based or water-soluble ointment, 9% type cream, or a siege preparation, but is not particularly limited. , ointments are preferably used. Conventional formulation techniques are used to produce these formulations. For example, when producing ointments, the bases are hydrocarbons such as vaseline, liquid halafine, squalane, microcrystalline, and wax, fatty acids such as stearic acid, myristic acid, and palmitic acid, lauryl alcohol, cetanol, stearyl alcohol, and lanolin. Higher alcohols such as alcohol, various oils and fats, glycols such as polyethylene glycol (macrogol) and propylene glycol are used, and the compound of formula (I) or its salt is added to this in an amount of about 0.5 to 15% of the total formulation amount. % amount, and if necessary, one or more of various surfactants, preservatives, fragrances, two pigments, etc. may be added to form an ointment. It is desirable to adjust the pH of the preparation to a range of S,O to 7.0 by adding a pH adjuster as necessary.To treat various skin diseases with the thus prepared external preparation, apply it to the affected area twice a day. You only need to apply the appropriate amount ~8 times.

9 The compound of the present invention represented by formula (I) is an extremely safe compound. 1 For example, the LD5o of cetraxate hydrochloride upon oral administration is 8000Tn9/mice.
lcg or more, rat 500 (9 or more in 1 m9/).

The present invention will be explained below with reference to Examples.

Example 1 Cetraxate 5% Macrogol 400 75% Stearyl alcohol 15% Stearin w1 5% A C ointment (pH -4,8) with the above formulation was prepared, and the obtained ointment was administered 1 to 4 times a day 2 to 8 times a day. Appropriate amount was applied to the affected areas of patients with skin diseases. The results are summarized in the table below, and a clear effect was observed on symptoms such as erythema, edema, and exudation by promoting drying of the lesion and fading of inflammation. Especially in the case of herpes zoster,
Ulcer.

The lesions became shallow and there was no secondary infection, and early healing was observed.

Example 2 Clinical trial effect of the topical preparation of the present invention on various skin diseases The ointment prescribed in Example 1 (however, cetraxate hydrochloride was used instead of cetraxate) was administered to a child with atopic dermatitis once or twice a day for 1 week. . As a result, improvements in symptoms such as erythema, papules, scales, and itching were observed in 8 out of 9 cases.

Its efficacy was approximately the same as that of the non-steroidal anti-inflammatory topical agent used as a control.

No side effects were observed.

Example 8 Cetraxate 10% White Vaseline 90% I made petrolatum ointment using the above recipe.

Example 4 Cetraxate 5% White Vaseline 25% Squalane 10% Cetyl alcohol 80% Span 60 2% Twin 60 8% Purified water 25% A % type cream was prepared using the above formulation.

Example 5 Heptraxate hydrochloride 2% Propylene glycol 5% 50% ethanol 98% A lotion was made using the above recipe.

Claims (1)

[Claims] External preparation for skin diseases containing a compound represented by the formula ▲ Numerical formula, chemical formula, table, etc. ▼ (n means an integer from 0 to 6) or a salt thereof