Anti-infectious combinations of active substances and their applying for topical treatment of fungal disease of finger nail, foot and wrist

FIELD: medicine, dermatology.

SUBSTANCE: invention proposes an anti-infectious preparation comprising the combination of active substances with topical and systemic antifungal agents and a water-insoluble film-forming agent. The systemic antifungal agent is taken among the group including intraconazole, terbinafine and fluconazole or their salts. The topical antifungal agent is taken among the group including ciclopirox, 6-(2,4,4-trimethylpentyl)-1-hydroxy-4-methyl-2(1H)-pyridone, amorolfine and butenafine or their salts. The preparation is used as lacquer for nails in therapy of onychomycosis. The lacquer preparation provides high concentration of systemic antifungal agents in nails after its topical applying. The significant advantage of the preparation involves short time in treatment of anychomycosis.

EFFECT: enhanced effectiveness and valuable medicinal properties of preparation.

6 cl, 6 ex

 

Fungal infections of the nails toes and hands (onychomycosis) are widely distributed in the world. It is among the highly industrialized countries such chronic not prone to samothracian diseases are becoming more significant. Onychomycosis a proportion of up to 40% of today's diseases of the nails. Disease onychomycosis at the present level is from 2.8 to 8.4%. Mycosis of the nails now account for about 30% of all ringworm. Epidemiological studies show that 20 to 30% of patients with fungal lesions of the feet also have onychomycosis.

Many patients feel limited social contacts, particularly if onychomycosis clearly marked on the nails of fingers. Moreover, due to the manifestations of the disease occur may have difficulty sense of touch, mobility and manual abilities. The need for treatment arises also for the reason that onychomycosis as a source of infection contribute to the spread of the disease from nails on the loose skin. Additionally they pose a risk of infection for an ever-increasing population.

Since the early nineties has been proposed many methods for the treatment of onychomycosis. On the one hand, these were new system active antifungal agents; for example, Itraconazole, see patent US 4267179 (E)-N-(6,6-dimethyl-2-hepten-4-INF-yl)-N-methyl-1-naphthalenemethanamine, which is also known as terbinafine, and α-(2,4-differenl)-α-(1H-1,2,4-triazole-1-ylmethyl)-1H-1,1,4-triazole-1-ethanol, also known as fluconazole, as well as applied topically lacquer drugs, which make the treatment of onychomycosis promising.

Systemic therapy experience can sometimes lead to burdensome, unwanted, life-threatening side effects of the medicinal product, as the active substance must reach the infectious focus through the circulatory system.

Side effects and interactions with other drugs already programmed for many elderly suffering from many diseases patients. Systemic antifungal drugs in addition responsible for other spam related effects, such as gaps in the spectrum capable of therapeutic agents or unstable partial resorption.

Recently conducted various studies with lacquer preparations containing antifungal agents, in combination with systemic therapy with Itraconazole or terbinafine in patients with severe onychomycosis. The results show that in the treatment of severe onychomycosis combination of local lacquer drug with the system taking Itraconazole or terbinafine is significantly higher than the effect of monotherapy it is econazole and terbinafine. So far the available data indicate that the percentage of failure in systemic treatment of onychomycosis can be significantly reduced by combination therapy local lacquer preparation containing the active antifungal agents, and system active antifungal agent.

The disadvantage of the combined treatment of local and systemic antifungal agent in the treatment of onychomycosis is system load with all its associated negative consequences that arise from the patient when the specified treatment strategies. An important disadvantage is the small number of systemic antifungal agent that reaches the nail toes or hands. In addition, still managed to enter the systemic antifungal agents such as Itraconazole, therapeutically active concentrations outer effective methods topically to the nails toes and hands (see patent WO 96/19186).

The task of the invention is the provision of the drug, which has no known drawbacks described local/systemic combination therapy of onychomycosis.

In spite of the technical prejudice that systemic antifungal agents such as Itraconazole, the local application penetrate in sufficient concentration only p is after the dissolution of sulfur bridges of the keratin of the nails and using supplements of urea (patent WO 96/19186), it has been unexpectedly discovered that a combination of local and systemic antifungal agents on lacquer base after local application is able to penetrate into therapeutically active concentrations through nails without the above activities and the named additives. Additionally, patients who were treated with systemic antifungal agent, had only relatively low concentrations of antifungal agents in the finger nails of the feet or hands.

Thus, the invention relates to a pharmaceutical preparation containing the active combination of local and systemic antifungal agents on physiologically acceptable lacquer base.

In particular, the invention relates to a pharmaceutical preparation containing a water-insoluble film former, at least one systemic antifungal drug from the group of Itraconazole, terbinafine and fluconazole and/or physiologically acceptable salts of Itraconazole, terbinafine and fluconazole and at least one local antifungal drug from the group of ciclopirox, 6-(2,4,4-trimethylpentyl)-1-hydroxy-4-methyl-2(1H)-pyridone, amorolfine and butenafine and/or physiologically acceptable salts ciclopirox, 6-(2,4,4-trimethylpentyl)-1-hydroxy-4-methyl-2(1H)-pyridone, amorolfine and butenafine or a mixture of several of the above against the fungal funds or their salts.

Preferred are pharmaceutical preparations which as antifungal agents contain ciclopirox (which is denoted as 6-cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone) and Itraconazole, or hydrochloride butenafine and fluconazole, or ciclopirox and fluconazole, or hydrochloride amorolfine and terbinafine hydrochloride.

The above local and systemic antifungal agents administered in free form and in the form of physiologically acceptable salts. If the salts to apply an organic base, use is preferably volatile ingredients of the base, for example, low-molecular alkanolamine, such as ethanolamine, diethanolamine, N-acylethanolamine, N-methyldiethanolamine, triethanolamine, Diethylaminoethanol, 2-amino-2-methyl-n-propanol, dimethylaminopropanol, 2-amino-2-methylpropanol, three-isopropanolamine. As other volatile ingredients grounds should be mentioned, for example, Ethylenediamine, hexamethylenediamine were, morpholine, piperidine, piperazine, cyclohexylamine, tributylamine, dodecylamine, N,N-dimethyldodecylamine, stearylamine, oleylamine, benzylamine, dibenzylamine, N-ethylbenzylamine, dimethylstyrene, N-methylmorpholine, N-methylpiperazine, 4-methylcyclohexylamine, N-hydroxyethylation. Can also be used salts of Quaternary ammonium hydroxide, such as Hydra is xed of trimethylantimony, the hydroxide of Tetramethylammonium or hydroxide of tetraethylammonium additionally guanidine and its derivatives, in particular, the products of alkylation. However, you can also use as soleobrazutaya, for example, low-molecular bonds alkylamines, such as methylamine, ethylamine or triethylamine. In the proposed input connections are also salts with inorganic cations, for example alkali metal salts, in particular salts of sodium, potassium or ammonium, in particular, hydrochloride, salts of alkaline earth metals, such as, in particular, salts of magnesium or calcium, and salt with from two to polyvalent cations, for example, salts of zinc, aluminum or zirconium.

Additionally, the invention relates to the use of combinations of active ingredients from local and systemic antifungal agents on physiologically acceptable lacquer base for local pharmaceutical preparation for the prophylactic and therapeutic treatment of fungal infections of nails, toes and wrists.

The invention relates also to the use of water-insoluble film-forming agents, at least one systemic antifungal agents from the group of Itraconazole, terbinafine and fluconazole and/or physiologically acceptable salts of Itraconazole, terbinafine and fluconazole and at least odnovalentnogo antifungal agents from the group of ciclopirox, 6-(2,4,4-trimethylpentyl)-1-hydroxy-4-methyl-2(1H)-pyridone, amorolfine and butenafine and/or physiologically acceptable salts ciclopirox, 6-(2,4,4-trimethylpentyl)-1-hydroxy-4-methyl-2(1H)-pyridone, amorolfine and butenafine or a mixture of several of the aforementioned antifungal agents or their salts to obtain local pharmaceutical preparation for the prevention and treatment of fungal infections of nails, toes and wrists.

The content of local and systemic active substances in the proposed patent drugs depends on the structure of each of the active substance and, thus, on his release from varnish film, its ability of penetration into the nail and its antifungal properties.

In the proposed pharmaceutical preparations for the treatment of onychomycosis, which is used in the form of nail Polish, that is in the form of solvent applications, local active substance is usually contained in an amount of from 0.25 to 20 weight percent, preferably from 2 to 15 weight percent. Content system-active compounds is usually from 0.05 to 10 weight percent, preferably from 0.1 to 5 weight percent.

Proposed lipsticks in addition to the active substance dissolved in the solvent or solvent mixture, as a necessary component contains one or more planroom is atobatele, after drying of the drug form on the nails water-insoluble film.

As the foaming agent is applicable, for example, substances based on cellulose nitrate or a physiologically acceptable polymer, for example, commonly used in cosmetics, preferably in a mixture with cellulose nitrate. It should be called, for example, polyvinyl acetate and partially saponified polyvinyl acetate, copolymer of vinyl acetate and acrylic acid or crotonic acid, or monoalkyl ether maleic acid ternary copolymer of vinyl acetate and crotonic acid and ventilationthe or crotonic acid and finalproject copolymer simple metilfenidato ether and complex monoalkyl ester of maleic acid, in particular in the form of a complex monobutyl ester of maleic acid, a copolymer of vinyl ester of fatty acid and of acrylic acid or methacrylic acid, a copolymer of N-vinylpyrrolidone, methacrylic acid and complex Olkiluoto of methacrylic acid, copolymer of acrylic acid and methacrylic acid or complex Olkiluoto ether acrylic acid or complex Olkiluoto of methacrylic acid, polyvinyl acetate and polyvinyl butyral, alkyl substituted poly-N-vinyl pyrrolidone, complex alkilany soporific olefins and maleic anhydride and the product came the action of rosin with acrylic acid, where in the complex sobolifera alkyl residues are usually short-chain and contain not more than four carbon atoms.

Preferably use preparations containing water-insoluble film former from the group of a copolymer of acrylate-methyl methacrylate-trimethylammoniumchloride, copolymer of esters of acrylic and methacrylic acids with a share of trimethylammoniumchloride, copolymer simple metilfenidato ether and monobutyl ether maleic acid copolymer, polyvinyl butyral and cellulose nitrate or copolymer of methacrylic acid and ethyl acrylate.

As physiologically acceptable solvent applicable customary in cosmetics hydrocarbons, halogenated hydrocarbons, alcohols, ethers, ketones and esters, in particular esters of acetic acid with a monohydroxy alcohols, such as ethyl and butyl acetate, if necessary, in a mixture with aromatic hydrocarbons, such as toluene, and/or alcohols, such as ethanol or isopropanol.

It is known that the combination of solvent is crucial for the drying time, the ability to smearing and other important properties of the varnish or lacquer films. The solvent system preferably consists of an optimal mixture of low-boiling (= solvent with a boiling point d is 100° C) and sredneskifskogo (= solvent with a boiling point up to 150° (C), if necessary with a small portion of high-boiling (= solvent with a boiling point up to 200°).

The proposed nail Polish may further contain commonly used in cosmetics additives, such as softeners based on phthalate or camphor, dyes or pigments, forming a pearly luster substance inhibitor deposition sulfonamidnuyu resins, silicates, fragrances, binders, such as dioctylsulfosuccinate sodium, derivatives of lanolin, light shielding means, such as 2-hydroxy-4-methoxybenzophenone, antibacterial substances and substances with keratolytic and/or keratoplastic action, such as urea, allantoin, enzymes and salicylic acid.

Dyed or pigmented lipsticks have, for example, the advantage that the proposed remedy can be adapted to the aesthetic sense of the patient and existing nail changes are not immediately apparent to others.

A method of obtaining a water-insoluble lacquers involves mixing a physiologically acceptable lacquer bases in dissolved form with antifungals and further necessary processing of the finished product.

Every once in relation to the number of non-volatile components, i.e. umanee quantity of foaming agent, added, if necessary, pigment, softener and other non-volatile additives, and entered active antifungal agents, in the proposed drug antifungal agents are typically present in the amount of 2 to 80 weight percent, preferably from 10 to 60 percent by weight and in particular from 20 to 40 weight percent.

With the proposed lacquer drug for the treatment of onychomycosis could achieve a complete cure without the occurrence of systemic side effects and interactions with other medicinal substances. In comparison with the hitherto existing experience therapy this result is important. An additional advantage is the much shorter time of treatment offered a pharmaceutical drug. This is manifested, in particular, significantly higher concentrations of systemic antifungal agents in the nails after local application.

The proposed pharmaceuticals applicable also for prophylactic use against onychomycosis, and reach a high enough depo active substances in the nails, so that in case of infection by the fungus does not occur outbreaks caused by fungus infections of the nails. Used for the prevention of pharmaceutical preparations contain smaller amounts of antifungal substances by cf is the ranking used therapeutically. Preferably in pharmaceutical preparations for the prevention of onychomycosis, which is used in the form of nail Polish, as well as in the applications of solvent containing the active substance is usually administered in amounts of from 0.25 to 4 weight percent, preferably from 1 to 4 weight percent. Content system-active compounds is usually from 0.05 to 3 weight percent, preferably from 0.1 to 1 weight percent. In comparison with systemic monotherapy for creating the appropriate depot active substances requires significantly less substances.

The invention additionally relates to the use of the proposed products in the cosmetics.

The invention is illustrated by the following examples, which, however, do not limit its scope. Unless otherwise noted, the quantitative data given in the calculation of the weight.

Example 1

Hydrochloride amorolfine5,0%
Hydrochloride terbinafine2,5%
A copolymer of acrylic ester
and methacrylic acids with a share
trimethylammoniumchloride20,0%
(for example, EUDRAGIT RL 100)
Isopropy monistat 2,5%
Isopropyl alcohol70,0%

Example 2

Hydrochloride butenafine5,0%
Fluconazole5,0%
The copolymer simple
metilfenidato ether and monobutyl
ether maleic acid25,0%
Ethanol 96%65,0%

Example 3

Ciclopirox8,0%
Itraconazole0,5%
Isopropylmyristate5,0%
1,2-Propylene glycol4,0%
The copolymer simple
metilfenidato ether and monobutyl
ether maleic acid7,5%
The ethyl acetate25,0%
Isopropyl alcohol50,0%

Example 4

Ciclopirox7,5%
Fluconazole5,0%
The copolymer simple
metilfenidato ether and monobutyl the
ether maleic acid15,0%
The ethyl acetate30,0%
Ethanol 96%42,5%

Example 5

After applying the proposed drug on the nail after cutting the nails of the test in the distal nail material after extraction by HPLC was determined by a combination of active substances.

6 weeks after 2-week treatment with the compound according to example 3 had the following values:

Itraconazole800 mcg/g nail
Ciclopirox140 g/g nail

After oral daily dose of 100 mg of Itraconazole for 3 months at the current level of technology concentration in the distal nail plates was 100 g/g of nails.

Thus, through the proposed pharmaceutical product can achieve in a short time about eight concentrations of Itraconazole in the nail compared with systemic treatment.

Example 6

2 weeks 2-week treatment with the preparation according to example 4 obtained the following values:

Fluconazole17 g/g nail
Ciclopirox the 92 mcg/g nail

1. The product containing water-insoluble film former and a combination of active substances from the at least one antifungal agent from a group of Itraconazole, terbinafine and fluconazole and/or physiologically acceptable salts of Itraconazole, terbinafine and fluconazole and at least one antifungal agent from a group of ciclopirox, 6-(2,4,4-trimethylpentyl)-1-hydroxy-4-methyl-2(1H)-pyridone, amorolfine and butenafine and/or physiologically acceptable salts ciclopirox, 6-(2,4,4-trimethylpentyl)-1-hydroxy-4-methyl-2(1H)-pyridone, amorolfine and butenafine.

2. The preparation according to claim 1, containing as antifungal agents ciclopirox and Itraconazole, or hydrochloride butenafine and fluconazole, or ciclopirox and fluconazole, or hydrochloride amorolfine and terbinafine hydrochloride.

3. The preparation according to claim 1 or 2, containing as the physiologically acceptable lacquer basics foaming agent based on cellulose nitrate, polyvinyl acetate and partially saponified polyvinyl acetate, copolymer of vinyl acetate and of acrylic acid or crotonic acid or monoalkyl ether maleic acid ternary copolymer of vinyl acetate and crotonic acid and ventilationthe, or crotonic acid and finalproject, copolymer simple metilfenidato ether and the false monoalkyl ester of maleic acid, in particular, in the form of complex monobutyl ester of maleic acid, a copolymer of vinyl ester of fatty acid and of acrylic acid or methacrylic acid, copolymer of N-vinylpyrrolidone, methacrylic acid and complex Olkiluoto of methacrylic acid, copolymer of acrylic acid and methacrylic acid or complex Olkiluoto ester of acrylic acid or complex Olkiluoto of methacrylic acid, polyvinyl acetate and polyvinyl butyral, alkyl substituted poly-N-vinylpyrrolidone, complex Olkiluoto of sobolifera olefins and maleic anhydride and the product of the interaction of the resin with acrylic acid, where in the complex sobolifera alkyl residues are usually short-chain and contain not more than four carbon atoms.

4. The preparation according to claim 3, containing a water-insoluble film-forming copolymer of ethyl acrylate-methyl methacrylate-trimethylammoniumchloride, a copolymer of esters of acrylic and methacrylic acids with a share of trimethylammoniumchloride copolymer simple metilfenidato ether and monobutyl ether maleic acid copolymer, polyvinyl butyral and cellulose nitrate or copolymer of methacrylic acid and ethyl acrylate.

5. The drug is one or more of claims 1, 2 or 4, containing antifungal substances the STW group ciclopirox, 6-(2,4,4-trimethylpentyl)-1-hydroxy-4-methyl-2(1H)-pyridone, amorolfine and butenafine in the amount of from 0.25 to 20 wt.%, preferably from 2 to 15 wt.%, and antifungal drug from the group of Itraconazole, terbinafine and fluconazole in the amount of from 0.05 to 10 wt.%, preferably from 0.1 to 5 wt.%.

6. The way to obtain a pharmaceutical preparation according to one or more of claims 1 to 5, characterized in that the physiologically acceptable lacquer based in dissolved form is mixed with antifungal agents.



 

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