BG65352B1 - Means for psoriasis treatment - Google Patents

Abstract

The means shows antiphlogistic, antiseptic, antimycotic, antiputrifactive, antiparasitic, keratolytic and adstringent effect, has expressed anaesthetic and anti-itching effect. It results in correct growing of the epithelial cells, increases the stability of the epithelial tissue and accelerates the epithelization. It possesses all properties of the tar, regulates the cellular proliferation, improves the blood circulation and the resolution of the infiltrate. The means has coal; and wood tar, preferably pine-tree tar, salicylic acid, as well as castor oil, Pomorie lye, optionally also benzocain, together with subsidiary substances, in the following quantitative ratios. in %: benzocain 1.00-3.00, tar from 0.5 to 30.0, salicylic acid from 0.5 to 5.00. urea from 2.00 to 17.00, castor oil from 10.00 to 30.00, Pomorie lye from 10.0 to 30 and subsidiary substances up to 100.

Description

Technical field

The invention relates to a topical agent for the treatment of psoriasis.

BACKGROUND OF THE INVENTION

Psoriasis is a common disease characterized by the presence of red scaly plaques that are found on the arms, legs and body. Very rarely, the face is affected, and sometimes the scalp may be affected. Mild forms are quite common.

The etiology of psoriasis is unclear. The treatment is combined, includes diet, UV irradiation, baths, air conditioning, application of topical preparations - creams, ointments, lotions.

Among the classic anti-psoriasis agents is coal tar and preparations based on it [British Pharmacopeia 98, p. 1258] Coal tar Solution, Coal tar and Salicylic Acid Ointment, Strong Coal tar Solution, Zink and Coal Tar Paste.

For example, WO 2001/083031 discloses a composition of a softening cream for topical treatment of psoriasis containing glucosamine, and optionally a keratilitic agent such as tar extract, salicylic acid. It may also contain an antioxidant anti-inflammatory plant extract.

GB 1 020 613 discloses a pharmaceutical composition for treating psoriasis and similar skin flaking conditions comprising lecithin and tar or a synthetic mixture of phenols, aromatic bases and aromatic hydrocarbons characteristic of tar dispersed in a suitable vehicle for use on the skin, for example in the form of cream.

WO 1997/048403 is known for the topical treatment of skin diseases, including psoriasis, containing 0.1 to 90 wt. % tar solution, 0.1 to 40 wt. % at least one component selected from the group: talc, bismuth gallate and finely dispersed sulfur, and liquid or solid vehicle or diluent up to 100%.

US 4 178 373 is known locally for the treatment of skin diseases, in particular psoriasis and eczema containing tar, as active ingredient in the gel base, from 0.5 to 20 wt. %, 2 to 10% of the fatty acid derivative of sarcosine, the fatty acid radical having 6 to 16 carbon atoms, and 25 to 75% by weight. fatty acid glyceryl ester of 6 to 22 carbon atoms.

From GB 2 290 470, a topical agent containing isoquinoline from 1 to 15% and a vasidilator from 0.25 to 5% is known to relieve skin conditions such as dermatitis, psoriasis and eczema. The preferred source of isoquinoline is tar and the preferred vasodilator is menthol. The agent is in the form of an ointment and may additionally contain a softener such as glycerol.

Hydrophilic ointment for treating psoriasis containing urea, zinc oxide, castor oil and starch is known from US 4 512 978 and may also contain crude tar, hydrocortisone, petrolatum and water.

Dithranol, a synthetic hydrocarbon, analogous to the action of wood and coal tar, is known. When applied, it is absorbent and slightly keratolytic.

The Bulgarian drug psanol is known [Uzunov P. Medicinal Products Handbook, 1994]. 100 ml of liquid preparation contains 95 ml of isopropyl coal tar extract at a ratio of 4: 1.3 g salicylic acid and 2 g urea. The preparation is intended for local treatment of psoriasis, with especially good effect in case of changes localized to the hairy parts, some forms of chronic eczema, neurodermatitis. It has a resorptive effect by inhibiting cell proliferation and improving skin circulation. It has an anti-inflammatory, keratolytic effect (due to the content of salicylic acid). The individual ingredients penetrate deep due to the presence of urea. Side effects: Rarely irritating dermatitis and folliculitis, photosensitizing effect when exposed to exposed parts and therefore not suitable for use in combination therapy with UV or sun exposure.

One of the problems with psoriasis is the different response of individual patients to the disease

65352 Bl personal coal based tar preparations, hence the need to create new drugs to increase efficiency and expand the patient contingent. Another problem arises from the fact that topical administration of drugs is aimed at influencing the numerous external manifestations of the disease, i. it is necessary to achieve itching, softening and hydrating the new skin, after peeling 10 plaques, preventing or suppressing inflammatory processes, nourishing the epidermis with the missing acids, vitamins and trace elements. Known formulations also contain, in addition to coal tar, 15 to three other active ingredients, i. E. cover only part of the required impacts, which is why they have a partial effect or are only effective in a limited number of cases. Therefore, the technical problem is to create 20 drugs that have an effective effect on the maximum number of manifestations of the disease and can be used in severe cases and phases and in a large number of patients.

SUMMARY OF THE INVENTION

This problem is solved with a local psoriasis treatment containing in% tar - coal or woody, preferably boron tar - from 0.5 to 30.00, salicylic acid - from 0.5 to 5.00, urea - from 2.00 to 17.00, castor oil - from 10.00 to 30.00, Pomorie - from 10.00 to 30.00, optionally benzocaine - from 1 to 3.00, excipients - 35 ca - up to 100 wt.

The composition of the agent according to the invention has all the properties of tar, regulates cell proliferation, improves blood circulation and spreads infiltrate. It has 40 anti-inflammatory, antiseptic, antifungal, antiparasitic, antiparasitic, keratolytic and astringent effects. It has a pronounced anesthetic and itchy effect. Castor oil in the composition contributes to the proper development of epithelial cells, enhances the resistance of epithelial tissue and accelerates epithelialization. Provides penetration into the skin of the missing vitamins A and D and omega-3- and omega-6-fatty acids. Moreover, thanks to the castor oil content, the agent according to the invention has a calming and softening effect on the skin, faster healing of wounds is achieved. Due to the content of the Pomorie lye, the trace elements zinc and selenium are provided.

During the treatment, the active substances are absorbed by the pathologically altered skin areas and act keratolytic, anti-inflammatory and keratoplastic until the disappearance of parakeratosis and clinical healing of the skin.

Benzocaine is the international, non-patent name, N-p-Aminobenzoate (4-aminoethyl benzoic acid ester), Coal tar (Coal tar, Pix Lithantracis, Pix Carbonis) is a product derived from bituminous coal by destructive distillation and is approximately 1000 degrees distillation. a complex mixture of cyclic hydrocarbons and heterocyclic compounds and their derivatives.

Pomorie Lye is a medical lye, a natural biologically active product of the salt lakes near the Black Sea, Pomorie. It is a standardized colloidal and saline solution. It is a concentrate of mineral salts of magnesium, calcium, sodium, chlorine, fluorine, bromine, iron, contains micro- and macronutrients magnesium, potassium, calcium, sodium, chlorine, bromine, iron, manganese, copper, cobalt, iodine, molybdenum, zinc , bimuth, fluorine, selenium, etc., as well as colloids, acids and bases and other substances of organic origin. Total mineralization: 350 g / l.

Embodiments of the invention

Example 1.

Composition of 100 g of finished liniment formulation:

Active substances: Benzocaine 2.00 Coal tar 20,00 Salicylic acid 1.50 Urea 10,00 Castor oil 21,50 Pomorie meadow 15,00 Excipients: Polyethylene glycol 400 25,00 Polysorbate80 5,00

65352 Bl

Example 2. Composition in grams per 100 g of ointment Active substances: Boron tar 1.50 Salicylic acid 1.50 Urea 10,00 Castor oil 20,50 Pomorie meadow 12,00 Excipients: Carboxymethylcellulose 23,370 th most common Propyl p-hydroxybenzoate 0.030 Methyl-p-hydroxybenzoate 0.100 Polysorbate 80 5,00 Lanolin 8,00 Cetyl alcohol 8,00 Yellow wax 6,00 The agent according to the invention tion used to treat psoriasis vulgaris, hy- perkeratosis and parakeratosis of the epidermis,

skin drop, acute inflammatory-exudative conditions, neurodermatitis and eczema with different etiology.

At the start of treatment, psoriatic changes should be in a calm state. Do not apply any treatment in the aftermath. The changes are smeared moderately and lightly twice daily - morning and evening. The bathing should be done in 3 days.

The treatment is carried out until the disappearance of 5 infiltrates and psoriatic flakes, ie. to clinical healing - normal relief and skin color. Psoriasis has 24 to 48 hours of occlusive dressings.

Do not use for more than 2-3 weeks. 10

Claims (1)

Claims 1. A psoriasis treatment comprising tar, salicylic acid and urea, 15 comprising charcoal or wood, preferably boron tar, salicylic acid, urea, as well as castor oil, Pomorskie alkali, and benzocaine, together with excipients, 20 at the following quantitative ratios in%: benzocaine - from 1,00 to 3,00, tar - from 0,5 to 30,00, salicylic acid - from 0,5 to 5,00, urea 2.00 to 17.00, castor oil - 10.00 to 30.00, Pomorie - 10.00 to 30.00 and excipients to 100. Expert: R. Jovovich Publication of the Patent Office of the Republic of Bulgaria 1797 Sofia, 52-B Dr. GM Dimitrov Blvd. Editor: R. Georgieva Cf. № 63999 Circulation: 40 VC