JPH0522686B2 - - Google Patents

Description

[Detailed description of the invention]

[Industrial Application Field] The present invention is based on the formula () The present invention relates to an external preparation for skin diseases containing the compound represented by or a salt thereof. The compound represented by the formula () consists of cis and trans geometric isomers, and in particular, its trans form (generic name: cetraxate) improves microblood circulation in the gastric mucosa and increases pepsinogen in the mucosa when administered orally. It is used as an excellent therapeutic agent for gastritis and gastric ulcers due to its pharmacological effects such as suppressing activation and suppressing gastric juice secretion through anti-kallikrein effects. [Effects of the Invention] As a result of intensive study on new uses of the compound of formula (), the present inventors found that
The present invention was completed by discovering that the compound of formula () exhibits excellent therapeutic effects when applied as an external preparation. Skin diseases to which the topical preparation of the present invention is applicable include herpes zoster, pemphigus vulgaris, pustular psoriasis, palmoplantar pustulosis, nummular eczema, ulcers, burns, impetigo, cutaneous candidiasis, and sweat blisters. Examples include ringworm, bullosa, and atopic dermatitis. In the treatment of these diseases, the dosage form of the external preparation of the present invention is oil-based or water-soluble ointment, o/w type or w/w type.
O-type creams, lotions, etc. can be used, and ointments are preferably used, although they are not particularly limited. In producing these preparations, conventional formulation techniques are employed. For example, when producing ointments, the bases are hydrocarbons such as vaseline, liquid paraffin, 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,
Use various oils and fats, glycols such as polyethylene glycol (macrogol), propylene glycol, etc., and add the compound of formula (1) or its salt in an amount of about 0.5 to 15% of the total formulation amount, as necessary. One or more of various surfactants, preservatives, perfumes, pigments, etc. may be added to form an ointment. In addition, the formulation
It is desirable to adjust the pH to a range of 3.0 to 7.0 by adding a pH adjuster if necessary. To treat various skin diseases with the external preparations thus prepared, an appropriate amount may be applied to the affected area two to three times a day. The compound of the present invention represented by formula () is an extremely safe compound. For example, the LD ₅₀ of cetraxate hydrochloride when administered orally is
8000mg/Kg or more, rats 5000mg/Kg or more. The present invention will be explained below with reference to Examples. Example 1 Cetraxate 5% Macrogol 400 75% Stearyl alcohol 15% Stearic acid 5% An ointment (PH=4.8) was prepared using the above formulation, and the obtained ointment was applied to the skin 2 to 3 times a day for 1 to 4 weeks. An appropriate amount was applied to the affected area of the patient. 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. In particular, in the case of herpes zoster, the ulcers and lesions became shallow, and there was no secondary infection and early healing was observed.

[Table] Example 2 The ointment prescribed in Example 1 (however, cetraxate hydrochloride was used instead of cetraxate) was administered to children with atopic dermatitis once or twice a day for one week.
As a result, improvement in symptoms such as erythema, papules, scales, and itching was observed in 8 out of 9 cases. Its effectiveness was almost the same as that of the non-steroidal anti-inflammatory topical agent used as a control, and no side effects were observed. Example 3 Cetraxate 10% White petrolatum 90% A petrolatum ointment was prepared using the above formulation. Example 4 Cetraxate 5% White petrolatum 25% Squalane 10% Cetyl alcohol 30% Span 60 2% Twin 60 3% Purified water 25% An o/w cream was prepared using the above formulation. Example 5 Cetraxate hydrochloride 2% Propylene glycol 5% 50% Ethanol 93% A lotion was prepared using the above formulation.

Claims (1)

[Claims] 1 formula An external preparation for skin diseases containing the compound represented by or a salt thereof.