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.
|A copolymer of acrylic ester|
|and methacrylic acids with a share|
|(for example, EUDRAGIT RL 100)|
|The copolymer simple|
|metilfenidato ether and monobutyl|
|ether maleic acid||25,0%|
|The copolymer simple|
|metilfenidato ether and monobutyl|
|ether maleic acid||7,5%|
|The ethyl acetate||25,0%|
|The copolymer simple|
|metilfenidato ether and monobutyl the|
|ether maleic acid||15,0%|
|The ethyl acetate||30,0%|
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:
|Itraconazole||800 mcg/g nail|
|Ciclopirox||140 µg/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 µg/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.
2 weeks 2-week treatment with the preparation according to example 4 obtained the following values:
|Fluconazole||17 µg/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.
FIELD: medicine, veterinary science.
SUBSTANCE: a new group of compounds, such as: 1) 1.3-benzodixole-5-β-nitroethylene
, 2) 1.3-benzodioxole-5-β-nitropropylene
, 4) 2-methylbenzimidazole-5-β-nitroethylene
, 5) benzoxazole-5-β-nitroethylene
, 6) 2-methylbenzoxazole-5-β-nitropropylene
has been suggested to protect against the agents of bacterial, protozoan and fungoid nature. Compounds are being the derivatives of heteronitroalkenes (dioxoles, oxazoles, imidazoles) with below-mentioned structural formulas being efficient to gram-positive bacteria and gram-negative aerobes, fungi of Candida, Trichophyton and other types, trichomonads. They could be applied at treating wound infections, fungoid lesions, septic states, pneumonia, trachoma, ornithosis, salmonellosis.
EFFECT: higher efficiency of protection.
5 cl, 5 tbl
FIELD: medicine, dermatology, chemical-pharmaceutical industry, pharmacy.
SUBSTANCE: invention relates to an antifungal gel pharmaceutical composition based on ketoconazole and clotrimazole that are derivatives of imidazole. The composition comprises ketoconazole or clotrimazole as an active component, polyethylene glycol-400 (PEG-400) as a solvent, carboxyvinyl polymer as a gel-forming agent, polyethylene glycol as a gel stabilizing agent, organic amine or inorganic bas as a regulator of pH and water taken in the definite ratio of components. The composition is prepared by dissolving active component in PEG-400, dispersing carboxyvinyl polymer in water, successive addition to dispersion propylene glycol as a stabilizing agent and regulator of pH and combination of prepared solution and gel followed by stirring the mixture up to preparing the gel composition with pH 5-7. Invention provides preparing antifungal composition with reduced adverse effect.
EFFECT: improved preparing method, valuable medicinal properties of composition.
2 cl, 1 tbl, 11 ex
FIELD: medicine, veterinary science, mycology.
SUBSTANCE: the suggested preparation for external application includes the mixture of Microsporum canis, Microsporum gypseum and Trichophyton mentagrophytes homogenates at the ratio of 1:1:2 in solvent, for example, in physiological solution, and formalin. Concentration of mycotic elements corresponds to 50.0-500.0 mln./ml ready-to-use product. This preparation should be applied in the method to treat dermatomycosis due to rubbing it into affected skin sites till hyperemia at 0.2-2.0 ml preparation/1-4 sq.cm skin surface once daily for 4-6 d. Both the preparation and the method suggested provide healing during the terms mentioned being convenient, reliable and efficient.
EFFECT: higher efficiency of therapy.
4 cl, 5 ex
FIELD: chemico-pharmaceutical industry.
SUBSTANCE: the present innovation deals with new stabilized pharmaceutical composition in its lyophilized form including the compound of formula I
as an active ingredient and lactose disaccharide as a stabilizing agent. The present pharmaceutical compositions are of high stability at storage. As for active ingredient it is not destroyed in the course of time.
EFFECT: higher efficiency.
10 cl, 15 ex, 6 tbl
SUBSTANCE: preparation comprises echinocandine substance of formula I or its pharmaceutically permissible salt, pharmaceutically permissible micelle-forming surface-active agent and non-toxic aqueous solvent and stabilizing agent.
EFFECT: improved stability and bioaccessibility properties.
48 cl, 4 tbl
FIELD: medicine, dermatology, pharmacy.
SUBSTANCE: invention relates to an antifungal preparation for external applying. The preparation comprises 2-chloro-4-nitrophenol, polyethylene glycol (PEG-400) and 50% ethyl alcohol. The preparation is used for treatment of epidermophytosis, trichophytosis, fungal eczema, cutaneous candidiasis and other diseases. Invention provides preparing the more effective antifungal preparation based on the domestic raw.
EFFECT: enhanced effectiveness of preparation, valuable medicinal properties.
FIELD: medicine, cosmetics.
SUBSTANCE: the present innovation deals with, a) at least, one fungicide substance and b) at least, one water-soluble film-forming substance, where b)-component is chitosan derivative chosen out of hydroxyalkyl chitosans and carboxyalkyl chitosans; nail vanish that includes the above-mentioned composition, and nail vanish that includes, at least, one water-soluble film-forming substance chosen out of hydroxyalkyl chitosans and carboxyalkyl chitosans. The suggested nail vanish is of high fungicide action and is free of multiple dermatological and esthetic disadvantages.
EFFECT: higher efficiency of application.
23 cl, 10 ex, 1 tbl
FIELD: medicine; medical engineering.
SUBSTANCE: method involves locally administering 30-50% hypertonic solution of xymedon hydrochloride, combined smoothly corrugated draining device, introducing gauze drain into upper part of wound cavity and intra-drain ultrasonic cavitation.
EFFECT: enhanced effectiveness of treatment; reduced risk of complications.
5 cl, 4 dwg
FIELD: medicine, pharmaceutical industry, pharmacy.
SUBSTANCE: invention relates to a pharmaceutical composition used in stomatology in the topical anesthesia. The pharmaceutical composition comprising articaine hydrochloride and epinephrine hydrochloride and accessory substances, such as sodium metabisulfite, sodium chloride and water for injection involves additionally glycine and pH-regulating substance taken in the definite ratio of components. Invention provides preparing the preparation that is stable, non-toxic and doesn't cause allergic response reactions and elicits highly expressed infiltration and conducting anesthetic activity, good tissue tolerance and activity promoting to accelerated wound-healing in the post-operative period.
EFFECT: improved and valuable medicinal properties of composition.
3 cl, 3 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to an aqueous composition consisting of moxifloxacin hydrochloride and sodium chloride and comprising from 0.04% to 0.4% (mas/vol) (as measured for the amount of moxifloxacin) of moxifloxacin hydrochloride and from 0.4% to 0.9% (mas/vol) of sodium chloride. Also, invention relates to applying this composition with the aim for preparing a medicinal agent used for prophylaxis or treatment of bacterial infections in humans or animals. Invention provides stability of the prepared moxifloxacin solution as moxifloxacin hydrochloride in the presence of iron ions.
EFFECT: improved properties of compositions.
FIELD: chemical-pharmaceutical industry, pharmacy.
SUBSTANCE: invention relates to a new pharmaceutical composition comprising benzamide derivative and one or some additives taken among the following substances: 1) mixture of polyethylene glycol and surface-active substance; 2) amino acid or inorganic acid salt, and 3) propylene carbonate. The composition comprises benzamide derivative taken in the amount from 0.001 to 1000 mg per a single dosing formulation. The composition shows the enhanced solubility and absorption capacity in oral route of administration.
EFFECT: improved medicinal and pharmaceutical properties of composition.
9 cl, 4 tbl, 1 dwg, 5 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to manufacturing medicinal preparations with wound-healing effect, in particular, to preparation with wound-healing effect comprising an agent stimulating epithelization. The wound-healing agent comprises vitamin E in concentrations 0.01-5.0 wt.-% in chitosan gel. Preferable variant represents applying chitosan gel formed by fractionated low-molecular chitosan of molecular mass from 10 to 20 kDa, or from 20 to 50 kDa, or from 50 to 300 kDa taken in the concentration from 1.0 to 10.0 wt.-%. Except for, it is possible additional applying antibacterial agent in wound-healing agent taken among the following order: chloramfenicol, lyncomycin, metronidazol, ciprofloxacin, benzalkonium chloride, additional using an antibacterial agent and lidocaine in agent, additional using an antibacterial agent and adrenaline in agent, and additional using hydrocortisone in the concentration 0.5 wt.-% in agent. Invention provides preparing wound-healing effect that occurs early essentially in epithelization and without formation of colloidal scars and reduces time for appearance of tissue regeneration markers.
EFFECT: valuable properties of agent.
8 cl, 2 tbl, 3 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to the propofol anesthetic composition suitable for parenteral administration. The composition comprises propofol in the concentration from 1 mg/ml to 20 mg/ml, d-alpha-tocopheryl polyethylene glycol-1000 succinate (TPGS) in the concentration from 10 mg/ml to 200 mg/ml, and water. The mass ratio of propofol to TPGS is at least 1:10. The composition is sterilized by final sterilization in autoclave. The present composition overcomes shortcomings of the ready preparative formulation in the emulsion form, namely, it provides the stable clear product in storage under regulated temperature conditions, i. e . in cooling.
EFFECT: improved and valuable pharmaceutical properties of composition.
11 cl, 7 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to pharmaceutical composition for intranasal administration contains zolmitriptan that is agonist of 5-HT1-receptor and pharmaceutically acceptable carrier. The composition has pH value less 6.0. The composition can be used for treatment of migraine and related disorders. The composition shows the improved stability in storage and provides effective relief for patients suffering with migraine.
EFFECT: improved and valuable medicinal properties of composition.
11 cl, 1 tbl, 9 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to an antiviral medicinal preparation. The preparation comprises ribavirin, phosphatidylcholine, cholesterol, α-tocopherol, sucrose, sodium chloride and represents lyophylizate in isotonic solution. Invention provides preparing the liposomal ribavirin eliciting high biological and therapeutic effectiveness with low toxicity.
EFFECT: improved, enhanced and valuable medicinal properties of preparation.
3 cl, 2 tbl
FIELD: pharmaceutical chemistry.
SUBSTANCE: invention relates to drugs for prevention and treatment of a variety of viral proliferative diseases and immunity disorders. Proposed solution contains: high-purity alpha-interferon; inert polymeric filler (in particular dextran or rheopolyglucin with molecular mass of dextran 30-50 kD); nonionic surfactant: tween 80, ethylenediaminetetraacetic acid or sodium salt thereof; buffer system including sodium acetate to provide solution pH 4.5-5.5; sodium chloride as osmotic pressure regulator; and injection water, all in specified proportions.
EFFECT: prolonged high activity and stability of preparation (up to 30 months) and improved quality characteristics thereof.
2 cl, 5 tbl, 2 ex
FIELD: pharmaceutical chemistry.
SUBSTANCE: invention, in particular, relates to prolonged therapeutical form of domestic slow calcium channel blocker, namely ankardin-retard-AZIn (active principle 7,7-ethylenedioxybenzopyran-2,2-dione) in the form of 0.1% solution administered in dose 1 ml in the form of complex with poly(ethylene oxide) 400. Pre-clinical investigations indicated that Ankardin-retard-AZIn was a sufficiently active calcium ion antagonist and, after clinical investigations, it could be applied in medical practice for prevention and treatment of cardiovascular diseases.
EFFECT: extended choice of drugs.
6 tbl, 4 ex
FIELD: organic chemistry, heterocyclic compounds, medicine.
SUBSTANCE: invention relates to derivatives of piperazine and piperidine of the formula (I): wherein ---Z represents =C or -N; Q means benzyl or 2-, 3- or 4-pyridylmethyl that can be substituted with one or more substitutes taken among group comprising halogen atom, cyano-group, (C1-C3)-alkoxy-group, CF3, OCF3, SCF3, (C1-C4)-alkyl, (C1-C3)-alkylsulfonyl and their salts, and to a method for their preparing also. It has been found that these compounds elicit valuable pharmacological properties owing to combination of (partial) agonism with respect to members of dopamine receptors subtype and affinity with respect to corresponding serotonin and/or noradrenergic receptors and can be useful in preparing compositions used in treatment of fear and/or depression or Parkinson's disease.
EFFECT: valuable medicinal properties of compounds.
7 cl, 1 tbl, 3 ex