For the treatment and prevention of fungal diseases of the skin based on grizeofulvina


(57) Abstract:

The tool is intended for treatment and prophylaxis of fungal diseases of the skin. The tool contains, wt%: fungistatic antibiotic griseofulvin 1-4, salicylic acid 0.5 to 2.0, menthol 0,5-5,0, camphor 0.1 to 5.0, water-emulsion ointment base, including oil component 10-30, solvent, 10-25, combined-Trilon B 0.05 to 0.15, the emulsifier is a mixture of polyoxyethyleneglycol ethers of higher fatty alcohols, 1,5-5,0 with glycerin esters of fatty acids 2-6 and higher fatty alcohols fraction from C12to C243-8 and water - the rest. Ointment based grizeofulvina eliminates symptomatic manifestations of fungal skin - itching, irritation, and pain. 6 C.p. f-crystals, 1 table.

The invention relates to medicine, namely to the pharmaceutical industry and relates to means for the treatment and prevention of fungal diseases comprising as an antifungal agent griseofulvin, anti-inflammatory agents and antiseptics - salicylic acid.

Morbidity statistics shows a steady increase in the frequency of mycotic, in particular dermatological, lesions of the person. In most cases, is but the long and cured. The problem of prevention of ringworm and reduce side effects in the treatment remains one of the topical issues in dermatology.

Antibiotic griseofulvin produced by the domestic industry, is one of the main treatments for patients with dermatomycosis. Griseofulvin has a moderate fungistatic activity, lack of resistance to it pathogenic fungal flora. Most common in dermatological practice of oral grizeofulvina tablets and suspensions. However, the actual problem is the creation of local legform.

It is known for the treatment of ringworm [1], representing the ointment of the following composition, wt.%:

Griseofulvin - 9,0 - 10,0

Streptocide - 9,0 - 10,0

Boric acid - 2,0 - 3,0

Dimexide - 9,5 - 10,0

Remezov - Rest

Closest to the proposed invention is a liniment grizeofulvina of 2.5% [2]. The liniment is applied in dermatological practice, is an effective means share therapy trihofitii, microscopy and plicarum smooth skin of onychomycosis.

The drawbacks include the presence in the composition of the dosage form dioxin and high gigroskopichny, resulting irritating dehydrating action Essentials - itching, dry skin, dermatitis, redness, etc., in Addition, in some cases, the function of Dimexidum as conductor grizeofulvina is a negative factor, because there is the possibility of resorption grizeofulvina and its circulation in the blood. This limits the field of use of the drug and its dose in the local application, eliminates the possibility of treating large group of patients.

The objective of this invention is to provide an effective dosage forms grizeofulvina for topical application for the treatment and prevention of ringworm with no irritant effect, suitable for prolonged use, a positive effect on the skin, eliminating symptomatic symptoms - itching, irritation, and pain.

The task is implemented the proposed drug in the form of a cream containing fungistatic antibiotic griseofulvin, antiseptic - salicylic acid, painkillers and anti-aircraft components - menthol and camphor and auxiliary substances-water emulsion base.

Experimental designs offer certain studies have shown, the ratios of the main and auxiliary components of the proposed tools have a direct impact on therapeutic effect.

The obtained data allowed to determine the quantitative content and ratio of components, which is achieved ego highest bioavailability in the absence of resorption grizeofulvina in the blood; in addition, mild sedative effect on damaged skin, reducing pain and itching allow to speak about achieving optimal therapeutic effect when a certain ratio of the main and auxiliary components of the proposed tools.

The proposed remedy meets the requirements for soft dosage forms and cosmetic creams: high bioavailability, thermal and colloidal stability, good absorbency, ease of use.

The invention is illustrated in the examples (table).

Griseofulvin suspended in vaseline or vegetable oil; salicylic acid, menthol and camphor dissolved in propylene glycol or polyethylene glycol; prepare the alloy surface-active substances with butter, mix all the components and emuleret. Th the cream convenient and pleasant consistency, having high contact bioavailability.

The means obtained in example 6, is an unstable liquid emulsion.

The means obtained in example 7, is a heterogeneous bystrorasshiryayuscheysya emulsion, unfit for consumption.

The means obtained in example 8, is a heterogeneous unstable emulsion.

The means obtained in example 9, is a hard unstable emulsion.

Thus, the proposed tool is based on grizeofulvina in the form of a cream to treat ringworm has several advantages:

1. The scope of the proposed tools is expanding due to the absence in the composition of Dimexidum, providing local irritant action and is the conductor of griseofulvin in the blood.

2. Proposed product is suitable for long-term use, has a beneficial effect on the skin, has pretiosum and analgesic effect, can be used for preventive purposes.

The technology for the proposed tool is simple; all auxiliary substances and materials pharmacologically indifferent available, the resolution is myshlennostj


1. USSR author's certificate 1685447, class A 61 K 9/06, publ. 23.10.91. bull. N 39.

2. VFS 42-1404-84. Liniment grizeofulvina of 2.5%. the prototype.

1. For the treatment and prevention of ringworm, including fungistatic antibiotic griseofulvin, salicylic acid ointment base, characterized in that it additionally contains menthol and camphor, as well as ointment bases contains aqueous emulsion base comprising an oil component, a solvent, as complexone - Trilon B (salt is the disodium Ethylenediamine - N, N, N - tetraoxane acid) as an emulsifier is a mixture of surface-active substances polyoxyethyleneglycol ethers of higher fatty alcohols (product OS-20, grade a) with glycerin esters of fatty acids and higher fatty alcohols fractions from C12to C24and water in the following ratio, wt.%:

Griseofulvin - 1,0 - 4,0

Salicylic acid is 0.5 to 2.0

Menthol - 0,5 - 5,0

Camphor - 0,1 - 5,0

The oil component is 10 - 30

Solvent - 10 - 25

The combined-Trilon B (salt is the disodium Ethylenediamine - N, N, N - tetraoxane acid) 0.05 to 0.15

Polyoxyethyleneglycol esters of higher fatty alcohols (s from C12to C24- 3,0 - 8,0

Water - the Rest

2. Means under item 1, characterized in that the oil component contains liquid paraffin.

3. Means under item 1, characterized in that the oil component contains vegetable oil.

4. Means under item 1, characterized in that the solvent contains a polyethylene glycol-400.

5. Means under item 1, characterized in that the solvent contains 1,2-propylene glycol.

6. Means under item 1, characterized in that as glycerol esters of fatty acids contains distilled monoglycerides (MHD).

7. Means under item 1, characterized in that as glycerol esters of fatty acids contains emulsifier "Solid-2" (T-2).


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