CS250165B1 - Antimikotic agent - Google Patents

Abstract

6-Caprolactam-based antimycotic agent in which 1 part by weight of 6-caprolactam 10% of the substance limiting the water content of the skin, such as antihydrotic or keratoplaetic agents wherein the? -caprolactam content of the reagent is from 5 to 90% by weight.

Description

The invention relates to an antifungal agent based on 6-ceprolactam. 6-caprolectam at higher concentrations limits the growth of microorganisms, while at lower concentrations, the growth of microorganisms may be stimulated in the presence of other nutrients.

Since δ-caprolactam is applied to the skin rapidly decreasing concentration due to the ease of solubility of 6-caprolactam in water and thus loss of efficacy, 6-caprolactam is not yet of use in dermatology, although the use of 6-caprolactam as a solvent for antibiotics is known according to Belgian patent No. 866 419.

Significant progress in the application of 6-caprolactam in the field of dermatology has been achieved by the combination of? -Caprolactam and iodine according to U.S. Pat. The combination of the antimycotic effect of 6-caprolactam and the antiseptic effect of iodine achieves high efficacy in all types of superficial mycoses, candidiasis and various bacterial skin affections, but the violent effect of the iodo-lactam agent limits its use in some cases, results in the destruction of the superficial layers of the skin and brown discoloration of the skin.

The aforementioned disadvantages are overcome by the antimycotic agent based on 6-caprolactam according to the invention, which comprises 6-caprolactam in combination with skin-water-reducing agents in a ratio of 10 ^-2 to 10% by weight. parts per 1 wt. 6-caprolactam.

These may be anti-hydrotic agents, such as formaldehyde or tannin, or keratoplestic agents, such as resorcinol or salicylic acid. The content of 6-ceprolactam in the reagent ranges from 5 to 90% by weight.

For the dosage form of the agent, the excipient may be selected from a wide variety of solvents and lubricants. By preventing the agent from penetrating deeply into the agent and diluting the 6-caprolactam in the affected skin with tissue fluid, the choice of diluent is limited only by the mutual solubility of the components and the permissibility of its application to the skin.

Because of the solubility of 6-caprolactam in both polar and non-polar solvents, water, alcohols, hydrocarbons, ketones, ethers, esters or 1 of their halogenated derivatives can be used to prepare the agent of the present invention. further penetration into the subcutaneous tissue.

Since 6-caprolactam is a relatively stable substance and forms clear, colorless solutions, the proposed agent, due to its physical properties, approaches the diluent used over a wide range of 6-caprolactam concentrations.

The low reactivity of 6-caprolactam then guarantees the stability of the proposed agents in the form of solutions which appear to be the most effective dosage form. 6-Caprolactam itself is a non-toxic substance and is harmless and non-irritating when applied topically. Since it does not react with the components under normal conditions, it retains its biological properties in the form of a reagent.

The agent of the invention can be successfully used extensively in the field of dermatology for topical application. The advantage of the agent is that, while maintaining a higher concentration, the active ingredient stops the growth of most microorganisms, hence, in addition to the antifungal action, it is also an effective antiseptic.

A further advantage is that the combination of 6-caprolactam with anti-hydrotic or rubratoplastic agents reduces the activity to the superficial, mycosis-infected part of the skin, where the concentration of 6-dcaprolactam increases and thus the efficacy of the agent while not affecting healthy skin.

At the same time, the penetration of otherwise harmful solvents into the subcutaneous tissue is limited. Due to the presence of 6-caprolectam, the skin remains relatively supple during application. The efficacy of the agent is so perfect that it reliably removes even outdated fungal affections.

Example 1

An antifungal agent of 20 wt. % of 6-caprolactam, wt. % of formaldehyde, wt. parts of ethyl alcohol and wt. parts of water.

of

Can be applied to fungal affections with localization on smooth skin.

Example 2

An antifungal agent of 30 wt. % of 6-caprolactam, wt. parts by weight of salicylic acid, wt. parts of acetone and wt. parts of water.

Can be applied to tinea cruris or pityriasis versicolor.

Example 3

An antifungal agent of 20 wt. % of 6-caprolactam, wt. parts taninue parts of ethyl acetate.

Applicable to all tinea pedum species.

For example, an antifungal agent of 20 wt. parts of 6-caprolactam,

0.5 wt. part resorcin, wt. parts of trichlorethylene and '

1.5 wt. of water.

Applicable to fungal affections in localization intertriginous.

The practical use of the agent is determined by the fact that the antimycotic activity of 6-caprolactam has been demonstrated in 22 species of pathogenic fungi and yeasts. Especially valuable is the efficacy on the most prolific dermetophytes such as Triehophyton rubrum, Trichophyton interdigitale, Epidermophyton floccosum and on microsporia.

The almost universal efficacy of the agent to anthropophilic and zoophilic dermetophytes predisposes the agent to wide surface application in medical practice.

Claims (1)

An antimycotic agent based on 6-caprolectam, characterized in that it is per 1 part by weight 6-caprolactam contained therein cases even 10 ^-2 to ¹ parts by weight of the substance limiting the water content in the skin such as antihydrotické substances such as formaldehyde or tannin, or room keratoplastic agents, such as resorcinol or salicylic acid, wherein the content _{of T} six caprolactam agent it is dd 5 to 90% by weight.