Pharmaceutical composition containing lysine, proline and triterpenic acid derivatives for treating and preventing viral infections caused by rna- and dna-containing viruses, such as: influenza, herpes, herpes zoster, human papilloma, adenoviruses, as well as bacterial infections caused by gram-positive and gram-negative microorganisms

FIELD: medicine.

SUBSTANCE: pharmaceutical composition possessing antiviral and antibacterial activity and containing L-N-2,6-diamino-hexanoyl-D-glucosamine, L-y-glutamyl-cysteinyl-glycyl-proline, lysine glycyrisinate, desoxyribonuclease, palmitoyl hydroxypropyl trimmonium amylopectin/glycerin cross polymer, hydroxypropyl-beta-cyclodextrin, D,L-pyrrolidone carboxylate N-cocoyl ethylarginate, escin, an emulsifying agent, a preserving agent, a pH control agent, demineralised water in certain amounts. The pharmaceutical composition possessing antiviral and antibacterial activity and containing L-N-2,6-diamino-hexanoyl-ascorbyl phosphate, N-pyrrolidine-carbamoyl-D-glucosamine, lysine ursolate, ribonuclease, a modified acrylic thickening agent, hydroxypropyl-beta-cyclodextrin, D,L-pyrrolidone carboxylate N-cocoyl ethylarginate, glycyrrhizic acid, an emulsifying agent, a preserving agent, a pH control agent, demineralised water in certain amounts. The pharmaceutical composition possessing antiviral and antibacterial activity and containing L-N-2,6-diamino-hexanoyl-hinokitiol, N-pyrrolidine-carbamoyl-D-glucosamine, lysine betulinate, collagenase, palmitoyl hydroxypropyl trimmonium amylopectin/glycerin cross polymer, hydroxypropyl-beta-cyclodextrin, chlorhexidine bigluconate, D-panthenol, an emulsifying agent, a preserving agent, a pH control agent, demineralised water in certain amounts. The pharmaceutical composition possessing antiviral and antibacterial activity and containing fusidoyl lysine, lysyl-valyl-proline pomolate, proline escinate, lysozyme, hydroxypropyl trimmunium maltodextrin, cross polymer, hydroxypropyl-beta-cyclodextrin, D,L-pyrrolidone carboxylate N-cocoyl ethylarginate, cedar extract, an emulsifying agent, a preserving agent, a pH control agent, demineralised water in certain amounts.

EFFECT: compositions possess expressed antiviral and antibacterial activity and are stable.

4 cl, 2 tbl, 11 ex

 

The present invention relates to medicine, namely to pharmaceutical compositions containing the derivatives of lysine, Proline and triterpene acids, which can be used in medicine for the treatment and prophylaxis of viral infections caused by RNA-and DNA-containing viruses, such as influenza, herpes, herpes zoster, papilloma of the person, adenovirus, as well as bacterial infections caused by gram-positive and gram-negative microorganisms.

Known medicines for local use, used for the treatment and prophylaxis of herpes infections, containing antiviral components that are not enzymes, such as cream Zovirax™ (acyclovir); spray Epigenome sex™ (glycyrrhizin acid); ointment: alpizarin, Halpin, flakozid containing plant extracts.

Known Proline (pyrrolidin-α-carboxylic acid) - heterocyclic amino acid (or ipinakikita). Exists in two optically isomeric forms L and D, as well as in the form of a racemate. L-Proline is one of the twenty proteinogenic amino acids. It is believed that the Proline is included in all proteins of all organisms. Especially rich in Proline main protein of connective tissue - collagen. Proline contains a nitrogen atom directly connected to the preceding amino acid residue, amino acid radical and the GRU who sing CH. He is very sharp bends of the peptide chain. In the structure of collagen Proline with the participation of ascorbic acid is oxidized in hydroxyproline. Alternating residues of Proline and hydroxyproline contribute to the creation of a stable trehspalnaya structure of collagen, giving the molecule strength (http://ru.wikipedia.org/wiki/%CF%F0%EE%EB%E8%ED).

From RU 2010151556 known composition having antiviral and antibacterial effect, containing lysozyme, escin, liposomes. The difference between the claimed invention from EN 2010151556 is that the composition also contains derivatives of lysine, Proline, triterpene acids.

From RU 2379312 renowned pharmaceutical composition comprising a compound based lysine, are used in the treatment and prevention of HIV infection.

Known food additive "Lisit" on the basis of lysine, providing immunostimulating effect and used in prevention and complex treatment of chronic viral infections, especially when urogenital viral infections and cold sores (Herpes simplex and Herpes zoster) (http://www.apollux.com/product-01.htm).

Known lysine (2,6-diaminohexanoic acid) - aliphatic amino acid with strong Foundation properties. Lysine is an essential amino acid, which is part of almost all proteins necessary for growth, tissue repair, production of antibodies, hormones, enzymes, albumins This amino acid has antiviral action, especially against the viruses that cause herpes and acute respiratory infections (retrieved from the Internet: http://ru.wikipedia.org/wiki/%CB%E8%E7%E8%ED).

Known L-lysine ascent, decreasing the activity of lysosomal hydrolases, which prevents the degradation of mucopolysaccharides in the walls of capillaries and connective tissue that surrounds them and thus normalizes increased vascular tissue permeability and has antiexudative (anti-edema and analgesic action (http://www.vidal.ru/poisk_preparatov/l-lysine-aescinat.htm).

Known drug Intesol 40 in the form of solution for infusion, containing lysine and used for stimulation of anabolic processes parenteral nutrition (http://www.vidal.ru/poisk_preparatov/infesol-40.htm).

From RU 2464033 known usnic acid and its oxidized derivative, which can be used as inhibitors of reproduction of influenza virus.

Known betulin acid (3β-hydroxy-20(29)-lupen-28-OIC acid) is a natural pentacyclic triterpenoids. Contained in the bark of some species of plants, mainly birch (Betula pubescens), which got its name. Betulin acid and its derivatives have anti-inflammatory, antitumor and anti-HIV activity (E. Pisha Method for selectivity values inhibiting melanoma, using betulinic acid. Nat. Med. 1995. Vol. 1. P. 1046-1051 T. Fujioka Compounds and methods of use to treat HIV infections. J. Nat. Prod. 1994. Vo. 57. P. 243-247.).

Known ursolic acid - Pyh triterpene compound emitted from plant material, exhibits physiological activity as for exterior and interior use. Its anti-inflammatory, anticancer and antimicrobial properties allow its use in cosmetics. Ursolic acid and its isomer, associated in most plants, oleanolic acid, have been recommended for the treatment and prevention of skin cancer in several countries. Both triterpene compounds promote hair growth by stimulating the peripheral blood flow in the scalp and activation of the maternal hair cells. Skin treatment preparations comprising these compounds, prevents hair loss and dandruff. For the ursolic acid and its derivatives identified a wide range of biological activities: anti-inflammatory, hypocholesterolemic, protivoateroskleroticheskim, antimicrobial, hypolipidemic, cardiotonic. In addition, ursolic acid may be used as a modifier of protein synthesis, as a cosmetic, as a means against linfocitos leukemia and anticancer drug (http://www.nioch.nsc.ru/russ/research/res_6.htm).

What is known about the antiviral activity of poolboy acid. (http://www.ijpbs.net/vol-2_issue-3/harma_science/44.pdf).

From WO 2012106188, US 2011313191, US 2012101098 known derivatives of Betulinol acid used for the treatment of viral infections, in particular HIV infection.

From KR 20110018671 known pharmaceutical compositions containing triterpene acids for the prevention and treatment of cardiovascular disorders caused by hypercholesterolemia.

FROM KR 2010040107 known compositions containing triterpene acid to eliminate wrinkles.

From JP 2011020989 known method of stabilizing triterpene acid N-medierranean.

From RU 2445317 known derivatives of Betulinol acid, used as an antineoplastic.

From WO 2011051520 known compositions containing triterpene acid as an auxiliary component in the composition of protein vaccines.

From RU 2098135 known ointment containing corticosteroid and beta-cyclodextrin, which has anti-inflammatory and antiallergic effect, in which the use of beta-cyclodextrin provides increased bioavailability of the drug, prolonged action, reducing the number of the active substance two times and reduce side effects, and the cheapening of the product.

From RU 2188004 C2 (WELFIDE CORPORATION), 27.08.2002 known use in pharmaceutical compositions for the treatment of hydrogenated lecithin, an example of which is selective is p lecithin and egg protein and soy lecithin (C. 4, last paragraph).

From RU 2302857 C2 (TROMMSDORFF GMBH & CO. KG ARZNEIMITTEL) (description of C. 8 and 9) is known as a solvent for adhesives purified water, and a suitable adhesive patches are monomers or mixtures thereof, such as methyl methacrylate and butylmethacrylate.

Known medical wipes containing desoksiribonukleaza and liposomes from moisture-resistant paper and nonwoven material "Spunbond", for the prevention of herpes (EN 2008140954).

From RU 2006114277 known cosmetic composition containing the desoksiribonukleaza and/or ribonuclease for the prevention of herpes infection.

Known medicinal and cosmetic products for local use, used for the treatment and prevention of scars, ulcers and wounds containing enzymes, such as ointment Iruksol™ containing enzyme: clostridiales and antibiotics: chloramphenicol (http://www.rlsnet.ru/tn_index_id_1605.htm); powder caritatem™ containing enzymes: papain and lysozyme, to prevent scarring (http://www.caripazymum.ru/instruction.html); gel Terminal containing complex collagenolytic proteases (http://fermencol.ru/); balsam Morical containing enzyme: morikazu (http://ekogoods.ru/catalog/11-balzam_%ABmorikrol%BB) Sodermix cream containing enzyme: superoxiddismutase (http://sodermix.ru/).

There are some preparations that do not contain enzymes, but used for the treatment and prevention of ulcers and R is h, for example, the gel Contractubex, including heparin, the extract of onion and allantoin (http://contractubex.ru/about/active_ingredients/), cream Clofibrate containing a combination of heparin, camphor and urea (http://apteka-evrofarm.com/kelofibraze_kelofibrase_krem_50_g_review_6/), silicone coating Zeraderm consisting of silicones, zinc oxide, vitamins E and K, coenzyme Q (http://zeraderm.su/), silicone gels Scan-fade, Kelo-Cote, Dermatix (http://www.dermatix-gel.ru/pages/informaciya_dlya_specialistov.html; http://www.kelo-cote.ru/kelo/harakteristiki_kelo-cote.php; http://www.scarfade.com/), oil Camelots with vitamin E, wheat germ oil and essential oil of rosemary (http://vertex.spb.ru/catalog/37/19/kameloks_maslo_s_witaminom_e_i_rozmarinom.html).

Known combined drug Exalis containing as an antimicrobial components - bilateral and lysozyme, enoxolone, isolated from glycyrrhizic acid as an anti-inflammatory component (http://www.vidal.ru/poisk_preparatov/hexalyse~22640.htm).

Known drug "Sangviritrin" issued in the form of tablets, solutions and liniment used in purulent-inflammatory diseases (http://medi.ru/doc/g3418.htm).

Known drugs Collagenase QC" and "Collalysin for enzyme purification wounds of different etiology, venous ulcers, accelerated rejection of necrotic tissue and Slough after burns and frostbite, when scarring of the eyelids and conjunctiva, symblepharon (http://www.rlsnet.ru/tn_index_id_5958.htm; www.rlsnet.ru/tn_index_id_5958htm).

Known cosmetic products for local use, used for the prevention of herpes containing antiviral components that are not enzymes, such as extracts of medicinal plants and germaniyorganicescoe connection (Lipstick preventive anti-herpes "Antiherpes" (P16 9158 915854 71.100.70) 292472. THE 9124-001-00358210-96), glycyrrhizin acid ointment "Germinal" ointment; ban. 20 ml; No. 77.01.12.915.P. 02970.02.00 from the Institute for atherosclerosis research the Academy of natural Sciences (Russia), INAT-PHARMA (Russia) (http://www.biomedservice.ru/publish/pub16.htm).

Well-known cosmetic sidezym enzymatic composition, where the enzyme is selected from the group of proteases, including trypsin, chymotrypsin, bromelain, papain and fitsin, and lysozyme, elastase, α-lipase and α-amylase, which is used for the treatment of acne, skin care and cleansing of the skin (DE 4305460). Described composition does not contain enzymes, nucleases, with direct antiviral activity, and, therefore, cannot be used to prevent viral infections.

Known toothpaste with sidezym enzymatic composition, where the enzyme is selected from the group of proteases, including papain (Whitening toothpaste "Rembrandt" (USA), as well as pasta, containing lysozyme, glucose oxidase, lactoperoxidase and lactoferrin (toothpaste Biotene (Finland), which is used for the treatment of xerostomia.

zwesten drug "Lysozyme", produced in the form of a hermetically sealed vials of 0.05, 0.1 and 0.15 g of providing bacteriolytic action and has the ability to stimulate nonspecific reactivity of the organism.

Well-known pharmaceutical drug "Desoksiribonukleaza", produced in the form of lyophilized powder in a hermetically sealed vials and ampoules 0,005; 0,01; 0.025 and 0.05, This drug is prescribed for herpetic keratitis, adenoviral conjunctivitis, to reduce viscosity and improve evacuation of sputum and pus when multiple bronchiectasis and is used topically in the form of a 0.2% solution of isotonic sodium chloride solution.

Well-known pharmaceutical drug "Ribonuclease", produced in the form of lyophilized powder in a hermetically sealed vials of 0.01, This drug is prescribed for respiratory diseases with difficult to spit sputum, periodontitis, gingivitis, festering wounds, trophic ulcers, tick-borne encephalitis, thrombophlebitis, the local application sprinkled the wound surface in the amount of 0.025 to 0.05,

Pharmaceutical compositions containing the derivatives of lysine, Proline and triterpene acids which can be used in medicine for the treatment and prophylaxis of viral infections caused by RNA-and DNA-containing viruses, such as influenza, herpes, herpes whether the AI, papilloma of the person, adenovirus, as well as bacterial infections caused by gram-positive and gram-negative microorganisms, are not described.

Thus, the present invention is to provide a pharmaceutical composition comprising a derivative of lysine, Proline and triterpene acids, which can be used in medicine for the treatment and prophylaxis of viral infections caused by RNA-and DNA-containing viruses, such as influenza, herpes, herpes zoster, papilloma of the person, adenovirus, as well as bacterial infections caused by gram-positive and gram-negative microorganisms.

According to the present invention proposed a pharmaceutical composition comprising as an active ingredient about 0.001-5.00 wt.% derivatives of lysine, 0.001 to 5.00 wt.% Proline 0.001 to 5.00 wt.% triterpene acids, as the carrier is 0.01 to 20.0 wt.% liposomes or β-cyclodextrins, including hydroxypropyl-β-cyclodextrins, or silicone quaternium-16, or qualitatsprodudukten chloride, or polyquaternium, or palmitoylethanolamide the amylopectin/glycerin of crosspolymer, or xanthan gum, or carragenin, or modified acrylic thickener, or hydroxypropyltrimonium maltodextrin of crosspolymer, or adhesives based on silicone (DC 7-700; 7-9800; 7-9850; 7-9900), or silicone fluid DC Q7-9120 (Q-9180), or DC Silagan media or DC ST-Elastomer 10, or other silicones PDMS patterns or fullerenes and pharmaceutically acceptable polymeric carriers or excipients.

As a preferred embodiment of the claimed invention proposed pharmaceutical composition specified above, optionally containing one or more than one anti-inflammatory ingredient.

Most preferred is a pharmaceutical composition for the treatment and prevention of viral and bacterial infections comprising as an active ingredient about 0.001-5.00 wt.% derivatives of lysine: ascorbyl phosphate lysine, L-N-2,6-diamino-hexanoyl-ascorbyl phosphate, L-N-2,6-diamino-hexanoyl-D-panthenol, L-N-2,6-diamino-hexanoyl-spagnol, L-N-2,6-diamino-hexanoyl-isothemal, fusicology, L-N-2,6-diamino-hexanoyl-hinokitiol, pninat lysine, L-N-2,6-diamino-hexanoyl-usnic acid, L-N-2,6-diamino-hexanoyl-D-glucosamine, ursolic lysine, glycyl-lysyl-Proline the glycyrrhizinate, lysyl-glycyl-Proline Pamyat, uncolorized, oleanolic, Betulinol, parillin, L-y-glutamyl-cysteinyl-glycyl-lysine, 0.001 to 5.00 wt.% Proline: ascorbyl phosphate Proline, N-pyrrolidin-carbamoyl-D-glucosamine, oleanolic Proline, pninat Proline, glycyl-methionyl-Proline the glycyrrhizinate, lysyl-poured-Proline Pamyat, URS is Lorrain, cleanarray, betweenopposing, parisberlin, L-y-glutamyl-cysteinyl-glycyl-Proline 0.001 to 5.00 wt.% triterpene acids: Proline ascent, lysine glycyrrhizinate, lysine Pamyat, the lysine betulina, lysine ursolic, lysine oleanolic, as the carrier is 0.01 to 20.0 wt.% liposomes or β-cyclodextrins, including hydroxypropyl-β-cyclodextrin, or silicone quaternium-16, or qualitatsprodudukten chloride, or polyquaternium, or palmitoylethanolamide the amylopectin/glycerin of crosspolymer, or xanthan gum, or carragenin, or modified acrylic thickener, or hydroxypropyltrimonium maltodextrin of crosspolymer, or adhesives based on silicone (DC 7-9700; 7-9800; 7-9850; 7-9900), or silicone fluid DC Q7-9120 (Q-9180), or DC Silagan media or DC ST-Elastomer 10, or other silicones PDMS patterns, or fullerenes and pharmaceutically acceptable polymeric carriers or excipients, in the following ratio, wt.%:

L-N-2,6-diamino-hexanoyl-D-glucosamine0,001-5,00
L-y-glutamyl-cysteinyl-glycyl-Proline0,001-5,00
Lysine glycyrrhizinate0,001-5,00
Desoksiribonukleaza0,001-5,00
Silicone quaternium-16 or
qualitatsprodudukten chloride or
polyquaternium or
palmitoylethanolamide
the amylopectin/glycerin of crosspolymer
or xanthan gum
or carragenin
or modified acrylic thickener
or hydroxypropyltrimonium maltodextrin
crosspolymer or adhesives based on silicone
(DC 7-9700; 7-9800; 7-9850; 7-9900)
or DC silicone liquids is ü Q7-9120 (Q-9180)
or DC Silagan media
or DC ST-Elastomer 10
or other silicones PDMS patterns0,05-5,00
Hydroxypropyl-beta-cyclodextrin0,10-5,00
D,L-pyrrolidonecarboxylic N-Cocoyl of tilargininefrom 0.01 to 5.00
Escinfrom 0.01 to 5.00
Emulsifierfrom 0.01 to 5.00
Preservative0,01-1,00
The pH regulator0,01-1,00
Water demineralizedRest

As another preferred embodiment of the claimed invention proposed pharmaceutical composition in the following ratio, wt.%:

L-N-2,6-diamino-hexanoyl-ascorbyl phosphate0,001-5,00
N-pyrrolidin-carbamoyl-D-glucosamine0,001-5,00
Lysine ursolic0,001-5,00
Ribonuclease0,001-5,00
Silicone quaternium-16 or
qualitatsprodudukten chloride or
polyquaternium or
palmitoylethanolamide
the amylopectin/glycerin of crosspolymer
or xanthan gum
or carragenin
or modified acrylic thickener
or hydroxypropyltrimonium maltodextrin
crosspolymer or adhesives based on silicone
(DC 7-9700; 7-9800; 7-9850; 7-9900)
or DC silicone fluid Q7-9120 (Q-9180)
or DC Silagan media or DC ST-Elastomer 10
or other silicones PDMS patterns0,05-5,00

Hydroxypropyl-beta-cyclodextrin0,10-5,00
D,L-pyrrolidonecarboxylic N-Cocoyl of tilargininefrom 0.01 to 5.00
Glycyrrhizin acidfrom 0.01 to 5.00
Emulsifierfrom 0.01 to 5.00
Preservative0,01-1,00
The pH regulator0,01-1,00
Water demineralizedRest

As another preferred embodiment of the claimed invention proposed pharmaceutical composition in the following ratio, wt.%:

L-N-2,6-diamino-hexanoyl-hinokitiol0,001-5,00
N-pyrrolidin-carbamoyl-D-glucosamine0,001-5,00
Lysine betulinic0,001-5,00
Collagenase0,001-5,00
Silicone quaternium-16 or
qualitatsprodudukten chloride or
polyquaternium or
palmitoylethanolamide
the amylopectin/glycerin of crosspolymer
or xanthan gum
or carragenin
or modified acrylic thickener
or hydroxypropyltrimonium maltodextrin
crosspolymer or adhesives based on silicone (DC 7-9700; 7-9800; 7-9850; 7-9900) or DC silicone fluid Q7-9120 (Q-9180) or DC Silagan media or DC ST-Elastomer 10 or other silicones PDMS patterns0,05-5,00
Hydroxypropyl-beta-cyclodextrin0,10-5,00
Chlorhexidine digluconatefrom 0.01 to 5.00
D-panthenolfrom 0.01 to 5.00
Emulsifierfrom 0.01 to 5.00
Preservative0,01-1,00
The pH regulator0,01-1,00

Water demineralizedRest

As another preferred embodiment of the claimed invention proposed pharmaceutical composition in the following ratio, wt.%:

Guidolin0,001-5,00
N-pyrrolidin-carbamoyl-D-glucosamine0,001-5,00
Proline ascent0,001-5,00
Lysozyme0,001-5,00
Silicone quaternium-16 or
qualitatsprodudukten chloride or
polyquaternium or
palmitoylethanolamide
the amylopectin/glycerin of crosspolymer
or xanthan gum
or carragenin
or modified acrylic thickener
or hydroxypropyltrimonium maltodextrin
crosspolymer0,05-5,00
Hydroxypropyl-beta-cyclodextrin0,10-5,00
D,L-pyrrolidonecarboxylic N-Cocoyl of tilargininefrom 0.01 to 5.00
Extract of thujafrom 0.01 to 5.00
Emulsifierfrom 0.01 to 5.00
Preservative0,01-1,00
The pH regulator0,01-1,00
Water demineralizedRest

Active ingredients claimed in pharmaceutical preparations is practical compositions are: derivatives of lysine: ascorbyl phosphate lysine, L-N-2,6-diamino-hexanoyl-ascorbyl phosphate, L-N-2,6-diamino-hexanoyl-D-panthenol, L-N-2,6-diamino-hexanoyl-spagnol, L-N-2,6-diamino-hexanoyl-isothemal, fusicology, L-N-2,6-diamino-hexanoyl-hinokitiol, pninat lysine, L-N-2,6-diamino-hexanoyl-usnic acid, L-N-2,6-diamino-hexanoyl-D-glucosamine, ursolic lysine, glycyl-lysyl-Proline the glycyrrhizinate, lysyl-glycyl-Proline Pamyat, uncolorized, oleanolic, Betulinol, parillin, L-y-glutamyl-cysteinyl-glycyl-lysine, a derivative of Proline: ascorbyl phosphate Proline, N-pyrrolidin-carbamoyl-D-glucosamine, oleanolic Proline, pninat Proline, glycyl-methionyl-Proline the glycyrrhizinate, lysyl-poured-Proline Pamyat, arcelorbremen, cleanarray, betweenopposing, parisberlin, L-y-glutamyl-cysteinyl-glycyl-Proline derived triterpene acids: Proline ascent, lysine glycyrrhizinate, lysine Pamyat, the lysine betulina, lysine ursolic, lysine oleanolic, enzymes: desoksiribonukleaza, ribonuclease, lysozyme, collagenase, an extract of thuja, D-panthenol, glycyrrhizin acid, chlorhexidine, D,L-pyrrolidonecarboxylic N-Cocoyl of tilarginine and escin. L-N-2,6-diamino-hexanoyl-spagnol, L-N-2,6-diamino-hexanoyl-isothemal, fusicology, L-N-2,6-diamino-hexanoyl-hinokitiol, pninat lysine, L-N-2,6-diamino-hexanoyl-usnic acid, ursolic lysine, glycyl-lysyl-Proline the glycyrrhizinate, whether the Il-glycyl-Proline Pamyat, uncolorized, oleanolic, Betulinol, parillin, oleanolic Proline, pninat Proline, glycyl-methionyl-Proline the glycyrrhizinate, lysyl-poured-Proline Pamyat, arcelorbremen, cleanarray, betweenopposing, parisberlin, lysine glycyrrhizinate, lysine Pamyat, the lysine betulina, lysine ursolic, lysine oleanolic, which have a pronounced antiviral effect in viral infections caused by RNA-and DNA-containing viruses, such as influenza, herpes, herpes zoster, papilloma of the person, adenovirus and other antimicrobial effect against bacterial infections caused by gram-positive and gram-negative microorganisms. The ascorbyl phosphate lysine and L-N-2,6-diamino-hexanoyl-ascorbyl phosphate promote the synthesis of collagen due to the integrated effect of increasing the concentration of the source of substrate for the synthesis of collagen (lysine) and stimulation of formation of hydroxy-lysine. L-N-2,6-diamino-hexanoyl-D-panthenol, L-y-glutamyl-cysteinyl-glycyl-lysine accelerate regeneratio tissues. L-N-2,6-diamino-hexanoyl-D-glucosamine and N-pyrrolidin-carbamoyl-D-glucosamine has a positive effect on the synthesis of connective tissue. Lysozyme catalyzes the hydrolysis of 1,4 - bond between N-acetylmuramic acid and 2-acetamido-2-deoxy-D-glucose (N-acetylglucosamine) contained in mucopolysaccharide is, mucopeptide and chitin in the cell walls of bacteria, fungi and protozoa, has a pronounced antimicrobial: destroys the cell wall of most gram-positive and some gram-negative bacteria, mycocide: delays the development of microscopic fungi, and wound-healing effect. Lysine, as antagonista arginine, inhibits the synthesis of viral proteins. Glycyrrhizin acid and its salts are used as antiviral agent for external and local application. Glycyrrhizin acid active against DNA - and RNA-containing viruses, including different strains of the Herpes simplex virus, Varicella zoster, human papilloma virus, cytomegaloviruses. The antiviral effect is connected, apparently, with the induction of the formation of interferon. Interrupts the replication of the virus in the early stages, causes the output of virion capsid, thereby preventing its penetration into cells. This is due to the selective dose-dependent inhibition fosforiliruyusciye kinase R. Interacts with the structures of the virus, changing the different phases of the viral cycle that is accompanied by irreversible inactivation of viral particles (located in the free state outside the cells), blocking the introduction of active viral particles through the cell membrane into the cell, as well as the impaired ability of viruses to SinTe the new structural components. Inhibits viruses at concentrations non-toxic for normal functioning of cells. Viral strains resistant to acyclovir and iodouridine, high sensitivity to glycyrrhizin acid. Also has anti-inflammatory, analgesic and improves tissue regeneration action as early manifestations of viral infection and ulcerative forms (http://www.vidal.ru/poisk_preparatov/act_1347.htm).

D-glucosamine is a tool to influence metabolism in cartilage tissue. Replenishes the natural deficiency of glucosamine stimulates the synthesis of proteoglycans and hyaluronic acid synovial fluid, increases the permeability of articular capsules, restores the enzymatic processes in the cells of the synovial membrane and articular cartilage. Promotes fixation of sulfur in the synthesis process chondroitinase acid facilitates the normal deposition of calcium in bone tissue, inhibits the development of degenerative processes in the joints, restore function and reduce pain (http://www.vidal.ru/poisk_preparatov/act_473.htm).

Fozilova acid is an antibiotic that is bacteriostatic or bactericidal effect. The mechanism of action is associated with inhibition of protein synthesis by inhibiting factor required for translocation of the protein subunits and the elongation of the peptide chain, which results in further destruction of the pathogen. High activity is against Staphylococcus spp., especially Staphylococcus aureus and Staphylococcus epidermidis (including methicillin-resistant strains), Nocardia asteroides, Clostridium spp. Less active against Streptococcus spp., Enterococcus spp., Neisseria spp., Bacteroides spp., Mycobacterium tuberculosis, Mycobacterium leprae. Fozilova acid is active against some protozoa, including Giardia lamblia, Plasmodium falciparum (http://www.vidal.ru/poisk_preparatov/act_1197.htm).

The ascorbyl phosphate is a stable form of vitamin C that stimulates collagen formation in the skin, ensuring at the same time, antioxidant protection.

Chlorhexidine antiseptic and disinfectant. Depending on the concentration manifests as a bacteriostatic and bactericidal effect. Bacteriological action as water and alcohol working solutions is evident in the concentration of 0.01% or less; bactericidal in a concentration of more than 0.01% at a temperature of 22°C and exposed for 1 min Fungicidal activity - at a concentration of 0.05% at a temperature of 22°C and exposed to 10 minutes Virucidal effect is manifested at a concentration of 0.01-1%. Effective against pathogens of sexually transmitted infections - Gardnerella, genital herpes; gram-positive and gram-negative bacteria Treponema spp., Neisseria gonorrhoeae, Trichomonas spp., Chlamydia spp., Ureaplasma spp. He acts on the acid-resistant forms of bacteria, microbial spores, fungi. Stable, after treatment of the skin (hands, personnage fields) is stored on it in a number of sufficient for antimicrobial effect. Remains active (although somewhat reduced in the presence of blood, pus, various secrets and organic substances.

Dexpanthenol or its derivatives belong to the b vitamins, are derivatives of Pantothenic acid. Plays an important role in the acetylation and oxidation, is involved in carbohydrate and fat metabolism, the synthesis of acetylcholine, corticosteroids, porphyrins. Has a marked influence on the formation and function of epithelial tissue, has some anti-inflammatory activity (http://www.vidal.ru/poisk_preparatov/act_303.htm).

Escin - triterpene glycosides (saponins) from the fruits (seeds), horse chestnut (as sodium salt). Has expressed capillarisation activity has antiexudative action (http://www.vidal.ru/poisk_preparatov/act_23.htm).

D,L-pyrrolidonecarboxylic N-Cocoyl of tilarginine a cationic surfactant that is used as an antimicrobial and conditioning treatment (http://ajinomoto.ru/ru-ru/%d0%bf%d1%80%d0%be%d0%b4%d1%83%d0%ba%d1%82%d1%8b/%d1%81%d1%8b%d1%80%d1%8c%d1%91%d0%b4%d0%bb%d1%8f%d0%ba%d0%be%d1%81%d0%bc%d0%b5%d1%82%d0%b8%d1%87%d0%b5%d1%81%d0%ba%d0%b8%d1%85%d1%81%d1%80%d0%b5%d0%b4%d1%81%d1%82%d0%b2/cae.aspx).

Desoksiribonukleaza (DNA-Aza) has the ability to hydrolyze the DNA of the herpes viruses, adenovirus and other DNA-containing viruses without damaging the DNA of cells of the microorganism. Ribonuclease(RNA-Aza) has the ability to hydrolyze RNA of influenza viruses, parainfluenza, tick-borne encephalitis and other RNA-containing viruses without damaging the RNA of the cells of the microorganism. Extract of thuja has a pronounced anti-inflammatory and antimicrobial action.

For the preparation of compositions use: substance content of the basic substance is not less than 97%, extracts content of extractives not less than 40% and the enzyme substance: "Desoksiribonukleaza", "Ribonuclease, Lysozyme, Collagenase".

The desoksiribonukleaza, ribonuclease, lysozyme, collagenase in the form of these drugs is not used for the treatment and prevention of viral and bacterial infections due to their difficulty suction and low level of consumer properties, as well as lack of stability at a moisture content of over 10% and in solution, with the loss of enzyme activity during the day.

Unexpectedly found that lysozyme, desoksiribonukleaza, ribonuclease, collagenase can be included in a stable pharmaceutical composition with preservation of the activity of these enzymes in a long time, despite the fact that this composition contains a significant amount of water (up to 90%).

The pharmaceutical composition of the present invention are usually produced in a common manner using acceptable solid or liquid carriers Il the excipients, selected from emulsifiers, dispersing agents, preservatives, flavoring agents, pH regulators, polymeric carriers and other excipients, which are suitable for preparing compositions. The pharmaceutical composition of the present invention can be prepared in the form of a gel, cream, patch, cream, gel, pastes, drops, suppositories, ointments and the like.

Additional advantages of the specified compositions are high stability, strong antibacterial and antiviral action, the ability to penetrate biological barriers and, consequently, rapid absorption, ease of use, and ease of dispensing.

The rapid penetration due to the binding of enzymes and other functional ingredients with media that are used in medicine in pharmaceuticals, for example IFN-EU-lient.

In addition, the active ingredients can be used in combination with one or more than one anti-inflammatory ingredient, such as D-panthenol, chlorhexidine, D,L-pyrrolidonecarboxylic N-Cocoyl of tilarginine extract of thuja, escin and glycyrrhizin acid, providing an additional advantage of the claimed composition.

The claimed pharmaceutical composition is stable in relation to the activity of enzymes is walking in its composition, for prolonged storage, which is achieved by immobilization of the enzymes on the media contained in the specified composition. As these media can be used any compounds which are capable of contacting the enzyme with the formation of complexes of the enzyme-carrier. Examples of such carriers are liposomes, β-cyclodextrins, including hydroxypropyl-β-cyclodextrin, silicone quaternium-16, qualitatsprodudukten chloride, polyquaternium, palmitoylethanolamide the amylopectin/glycerin of crosspolymer, xanthan gum, carrageenin, modified acrylic thickener, hydroxypropyltrimonium maltodextrin of crosspolymer, adhesives based on silicone (DC 7-9700; 7-9800; 7-9850; 7-9900), DC silicone fluid Q7-9120 (Q-9180), DC Silagan media, DC ST-Elastomer 10 and other silicones PDMS structures, fullerenes and other Advantages of liposomes, xanthan gum and carrageenate, adhesives based on silicone (DC 7-9700; 7-9800; 7-9850; 7-9900), DC silicone fluid Q7-9120 (Q-9180), DC Silagan media, DC ST-Elastomer 10 and other silicones PDMS patterns is high biocompatibility. The benefits of quaternium-16, qualitatsprodudukten chloride, polyquaternium, palmitoylethanolamide the amylopectin/glycerin of crosspolymer modified acrylic thickener, hydroxypropyltrimonium the maltodextrin of crosspolymer is the presence of strong positive charge of the modified ammonium ion. This causes the antimicrobial properties of these polymers, defines a high affinity to enzymes, amino acids and anions triterpene acids, the ability to increase the stability of the complex with enzymes. Additional media is hydroxypropyl-beta-cyclodextrin, which promotes the solubility of the derivatives of lysine, Proline, triterpene acids and the creation of a stable conformation of the active center of enzymes, which determines their high activity.

Thus the complex antiviral, antimicrobial and anti-inflammatory effect of the claimed composition.

The present invention is illustrated by the following examples.

EXAMPLE 1

Pharmaceutical composition in the form of ointment for nose has the following composition, in wt.%:

L-y-glutamyl-cysteinyl-glycyl-Proline5,00
Lysine glycyrrhizinate5,00
Desoksiribonukleaza5,00
Silicone quaternium-165,00
Hydroxypropyl-beta-cyclodextrin5,00
D,L-pyrroline the carboxylate N-Cocoyl of tilarginine 5,00
Escin5,00
Emulsifier5,00
Preservative1,00
The pH regulator1,00
Water demineralizedRest

The above composition is prepared by the following method. In demineralized water dissolve all of the components, the resulting ointment mix, vacuum and homogenized.

EXAMPLE 2

Pharmaceutical composition in the form of eye ointment has the following composition, in wt.%:

L-N-2,6-diamino-hexanoyl-D-glucosamine0,001
L-y-glutamyl-cysteinyl-glycyl-Proline0,001
Lysine glycyrrhizinate0,001
Desoksiribonukleaza0,001
Palmitoylethanolamide
the amylopectin/glycerin of crosspolymer5,00
Hydroxypropyl-beta-cyclodextrin0,10
D,L-pyrrolidonecarboxylic N-Cocoyl of tilarginine0,01
Escin0,01
Emulsifier0,01
Preservative0,01
The pH regulator0,01
Water demineralizedRest

The above composition is prepared as in EXAMPLE 1.

EXAMPLE 3

Pharmaceutical composition in the form of antiviral ointment has the following composition, in wt.%:

L-N-2,6-diamino-hexanoyl-ascorbyl phosphate0,001
N-pyrrolidin-carbamoyl-D-glucosamine0,001
Lysine ursolic0,001
Ribonuclease0,001
Modified acrylic thickener1,0
Hydroxypropyl-beta-cyclodextrin0,1
D,L-pyrrolidonecarboxylic N-Cocoyl of tilarginine0,01
Glycyrrhizin acid0,01
Emulsifier0,01
Preservative0,01
The pH regulator0,01
Water demineralizedRest

The above composition is prepared as in EXAMPLE 1.

EXAMPLE 4

Pharmaceutical composition in the form of ointment from the scar has the following composition, in wt.%:

L-N-2,6-diamino-hexanoyl-hinokitiol0,1
N-pyrrolidin-carbamoyl-D-glucosamine5,00
Lysine betulinic5,00
Collagenase0,1
Palmitoylethanolamide
the amylopectin/glycerin of crosspolymer5,00
Hydroxypropyl-beta-cyclodextrin the 5,00
Chlorhexidine digluconate0,1
D-panthenol5,00
Emulsifier5,00
Preservative1,00
The pH regulator1,00
Water demineralizedRest

The above composition is prepared as in EXAMPLE 1.

EXAMPLE 5

Pharmaceutical composition in the form of ointments for burns has the following composition, in wt.%:

Guidolin0,001
Lysyl-poured-Proline Pamyat2,00
Proline ascent0,001
Lysozyme0,001
Hydroxypropyltrimonium maltodextrin
crosspolymer0,5
Hydroxypropyl-beta-cyclodextrin0,10
D,L-pyrrolidonecarboxylic N-Cocoyl of tilarginine0,01
Extract of thuja0,01
Emulsifier0,01
Preservative0,01
The pH regulator0,01
Water demineralizedRest

The above composition is prepared as in EXAMPLE 1.

EXAMPLE 6

Pharmaceutical composition in the form of strips from the scar has the following composition, in wt.%:

L-N-2,6-diamino-hexanoyl-usnic acid0,1
N-pyrrolidin-carbamoyl-D-glucosamine5,00
Lysine ursolic5,00
Collagenase0,1
DC Silagan media2,00
Hydroxypropyl-beta-cyclodextrin2,00
Chlorhexidine digluconate0,5
D-panthenol5,00
Emulsifier5,00
Preservative1,00
The pH regulator1,00
Water demineralizedRest

An adhesive mass is the number

Nonwoven Spunbond

The above composition is prepared as in EXAMPLE 1. The mixture is treated nonwoven Spunbond and then put a layer of an adhesive mass.

EXAMPLE 7

Pharmaceutical composition in the form of strips from the scar has the following composition, in wt.%:

Betulinol0,5
N-pyrrolidin-carbamoyl-D-glucosamine5,00
Lysine oleanolic5,00
Collagenase0,1
DC 7-97005,00
Hydroxypropyl-beta-cyclodextrin5,00
Chlorhexidine digluconate
D-panthenol5,00
Emulsifier5,00
Preservative1,00
The pH regulator1,00
Water demineralizedRest

An adhesive mass is the number

Nonwoven Spunbond

The above composition is prepared as in EXAMPLE 1. The mixture is treated nonwoven Spunbond and then put a layer of an adhesive mass.

EXAMPLE 8

Pharmaceutical composition in the form of strips from the scar has the following composition, in wt.%:

L-N-2,6-diamino-hexanoyl-Spagna0,5
Glycyl-methionyl-Proline the glycyrrhizinate5,00
Lysine oleanolic5,00
Collagenase0,1
Liposomes containing hydrogenated
lecithins in combination with cholesterol20,0
The methyl methacrylate1,0
Butylmethacrylate1,0
Hydroxypropyl-beta-cyclodextrin3,00
Chlorhexidine digluconate0,1
D-panthenol5,00
Emulsifier5,00
Preservative1,00
The pH regulator1,00
Water demineralizedRest

An adhesive mass is the number

Nonwoven Spunbond

The above composition is prepared as in EXAMPLE 1. The mixture is treated nonwoven Spunbond and then put a layer of an adhesive mass.

EXAMPLE 9

Pharmaceutical composition in suppository from adhesions and bacterial infections, for proctitis has the following composition, in wt.%:

L-N-2,6-diamino-hexanoyl-Spagna0,5
Lysyl-poured-Proline Pamyat 5,00
Lysine glycyrrhizinate5,00
Collagenase0,1
DC silicone fluid Q7-91802,00
Hydroxypropyl-beta-cyclodextrin3,00
Chlorhexidine digluconate0,1
D-panthenol5,00
Hydrophilic base70,00
Preservative1,00
The pH regulator1,00
Water demineralizedRest

The above composition is prepared by the following method. Melt at 40°C hydrophilic base, dispersed in all components. The resulting mixture is then poured into the form.

EXAMPLE 10

Pharmaceutical composition in suppository from adhesions and bacterial infections, for proctitis has the following composition, in wt.%:

L-N-2,6-diamino-hexanoyl-Spagna0,5
Glycyl-methionyl-Proline the glycyrrhizinate5,00
Lysine Pamyat5,00
Collagenase0,1
DC ST Elastomer2,00
Hydroxypropyl-beta-cyclodextrin3,00
Chlorhexidine digluconate0,1
D-panthenol5,00
Emulsifier5,00
Preservative1,00
The pH regulator1,00
Water demineralizedRest

An adhesive mass is the number

Nonwoven Spunbond

The above composition is prepared by the following method. Melt at 40°C hydrophobic base, dispersed in all components. The resulting mixture is then poured into the form.

EXAMPLE 11

Pharmaceutical composition in the form of eye drops for bacterial and viral infections of the eye, in wt.%:

L-N-2,6-diamino-hexanoyl-isothemal0,5
Glycyl-methionyl-Proline the glycyrrhizinate0,01
Lysine oleanolic0,01
Desoksiribonukleaza0,05
Carragenin0,05
Hydroxypropyl-beta-cyclodextrin0,1
Chlorhexidine digluconate0,01
D-panthenol1,00
Emulsifier1,00
Preservative0,05
The pH regulator0,05
Water demineralizedRest

The above composition is prepared as in EXAMPLE 1.

Evaluation of the stability of enzymes in the compositions

Since the main drawback of enzymes is their instability during long-term storage of finished dosage forms based on them within the expiration date was the comparative assessment of the preservation of the enzyme activity is ri stored in the form of a solution in the form of a composition (for example, gel).

Activity of deoxyribonuclease, ribonuclease, lysozyme, collagenase was determined by the following methods.

1) determining the activity of lysozyme was carried out according to the method of O. Bukharin Century, based on the measurement values of optical density by adding enzyme to the bacterial suspension. In a test tube filled with 0.4 ml of phosphate buffer (pH 6.2) and 0.1 ml of the investigated solution and 2 ml of a standardized suspension of micrococci. The mixture is incubated for 30 minutes at 37°C, then measure its optical density on FEC-M at λ=540 nm.

Per unit activity of lysozyme take the least amount of enzyme which under the influence of it on the substrate in terms of experience analyzes this amount of culture suspension Mycrococcus lysodeikticus, which leads to an increase in optical density at a wavelength of 540 nm by one unit.

2) Determination of the activity of dnaase and RNA-ASE was carried out according to the method of Konitsa. Per unit activity of dnaase (RNA-ASE) take the least amount of enzyme which under the influence of it on the substrate in terms of experience frees this number colorstorm products, which leads to an increase in optical density at a wavelength of 260 nm by one unit. In the control and two experimental tubes contribute 0.5 ml of substrate (DNA or RNA) and 0.3 ml of 0.2 M Tris-buffer (pH=7). In the experimental, pre-prog is all tubes contribute 0.2 ml of an enzyme solution. Sample thermostatic for 30 minutes at a temperature of 37.5°C. Then the samples are added 1 ml) cooled in an ice bath, 1N. solution of perchloric acid (HClO4), in the control and 0.2 ml of an enzyme solution. The tubes are shaken and incubated in an ice bath 16-25 minutes. The formed precipitation was separated by centrifugation at 4000 rpm for 10 minutes. From the supernatant layer selected 0.5 ml of solution, add 2.5 ml of water and measure the optical density at λ=260 nm.

3) To determine the proteolytic activity of papain used the modified method of Konitsa. One proteolytic unit take that amount of enzyme, which when exposed to the substrate casein for 10 minutes under standard conditions is released such quantity of the products of hydrolysis, which leads to an increase in optical density at a wavelength of 280 nm per unit.

The results are shown in the following table.

As can be seen from the table, the introduction of the enzymes in the composition allows to obtain a stable pharmaceutical composition for the treatment and prevention of viral and bacterial infections. Despite the fact that the introduction of the enzymes in the composition of these songs is a minor loss of enzyme activity, with further storage for 1 year, the enzymes do not change their activity due to the fixation of unstable structures of the enzyme carrier.

Evaluation of antiviral and antibacterial activity of the composition

To evaluate antiviral and antibacterial activity, a study was conducted of the effectiveness of the composition of EXAMPLE 3 in comparison with the antiviral drug Acyclovir cream. The study involved 39 patients aged 18 to 45 years, with clinical manifestations of herpes infection. On the floor, the group was divided as follows: male - 11 female - 28. Disease duration ranged from 2 years to 12 years. While the vast majority of patients reported mild and moderate for herpes infection - 2-3 times a year 14, 4-6 times per year - at 22 and 6-8 times a year in 3 patients. Among women in the observed group of Orofacial manifestations were observed in 18, genital localization in 10 man. In the group of men in 7 patients registered with genital herpes, and 4 observed was noted defeat in the face zone. With 7 men and 2 women - 5) was observed joining manifestations of herpes conditionally pathogenic bacterial flora with the development of complications such as strepto-stphiladelphia.

Most patients were registered small area of damage, ranging from 0.5 to 1.0 cm in 29 cases, the centers of area of 1.5 cm in 9 observed.

In the comparison group were 11 patsie the tov manifestations of herpetic infection receiving outdoor therapy cream Acyclovir". On the floor of the comparison group were divided as follows - men - 7 women, 4 men. Manifestations of herpes all men were in the genital location, 1 women herpes also had genital localization, and 3 women were observed Orofacial herpes. By severity 8 patients in the control group had a mild case, 3 - moderate severity.

Before treatment and 4 weeks after end of treatment all patients performed the following studies:

Survey and inspection

- Study of the material from the lesion using the polymerase chain reaction for detection of herpes simplex virus human

- Examination of scrapings from the urogenital tract to detect chlamydia, Miko and ureaplasmas (with lesions of the urogenital tract)

Testing serum for syphilis; research on HIV after conducting a pre-test interview

- The clinical analysis of blood.

All patients after obtaining informed consent for external treatment was assigned the composition of EXAMPLE 3, 4-6 applications per day, three patients with severe were simultaneously conducted systemic therapy drugs acyclic nucleosides within 5 days. In the comparison group patients received the outer is therapy cream Acyclovir" 6 applications per day.

The treatment ended 31 patients. 8 patients after remission did not report for follow-up. Most of the patients (28 people) reported good tolerability of the drug. 3 people in the process of the drug was noted quite pronounced burning sensation after applying the cream on the lesions. In the process of observation none of the patients was not observed allergic reactions to the composition of EXAMPLE 3.

The positive effect from the use of the composition of EXAMPLE 3 was observed in all patients and was expressed in the acceleration of epithelialization of the foci and the impact on opportunistic bacterial flora with a resolution of infectious complications.

While examining patients of the main group on the background of treatment positive clinical effect was observed for most of the observed in the form of cessation of new lesions on average 3±1,2 day, the beginning of epithelization 6±2,1 day, complete epithelialization was observed to 11±2,3 day. The epithelization time depended on the size of the initial lesion and the degree of severity of herpes infection. Positive therapeutic effect was observed in patients with bacterial complications of herpes infection, probably due to part of the existing components. Noteworthy is the fact that quite good results is s obtained in patients with severe herpes infections, where combination therapy was carried out. At the same time epithelialization of the lesions in these patients were compared with a group of patients with a mild case of herpes.

In the group of patients that used the cream Acyclovir obtained similar results in terms of the cessation of new lesions (3±1.4 days), by the time the epithelization (6±2.3 days), then as full epithelialization of the foci of lesions occurred more slowly and was 14±2.1 days. Physical examination conducted before treatment, abnormalities not identified as persons of the core group and the comparison group.

Thus, a study on a small group of patients, allows to draw the following conclusions:

1. Found that using the compositions of EXAMPLE 3 is possible in the treatment of lesions caused by herpes virus 1, 2 type.

2. The drug is well tolerated by patients.

3. Side effects registered in 3 patients who participated in this study and resulted in burning sensation in the area of the coating compositions of EXAMPLE 3, an allergic reaction to the drug in the study were not met.

4. Perhaps the use of the composition of EXAMPLE 3 in bacterial complications of herpes infection that is caused by the presence in its composition of ingredients with proteomika the m action.

5. The use of a composition of EXAMPLE 3 promotes more rapid epithelialization of the lesions compared with the use of cream Acyclovir".

6. The composition of EXAMPLE 3 can also be used in combined therapy of patients with severe recurrent herpes infection, contributing to more rapid epithelialization.

Evaluation of antimicrobial activity of the composition

Antimicrobial activity of the composition of EXAMPLE 1 was determined by serial dilution method. As the test microorganism culture: Staphylococcus spp., Streptococcus spp., Enterococcus spp., Shigella spp., Escherichia spp., Salmonella spp., Proteus spp., Acinetobacter spp., Citrobacter spp., Pseudomonas spp., Serratia spp., Klebsiella spp., Antracoides spp., Cryptococcus spp., mushrooms of the genus Microsporum, Trichophyton, Nocardia, Aspergillus, Candida, Actinomycetes, protozoa: Entamoeba histolytica, Trichomonas vaginalis. In each tube was made a one-day culture in quantities of 1000 cells/ml. All cultures of microorganisms, except Microsporum, Trichophyton, Nocardia, Aspergillus, Candida, Actinomycetes, were grown in test tubes on the environment mesopartner broth at 37°C during the day, and the culture of Microsporum, Trichophyton, Nocardia, Aspergillus, Candida, Actinomycetes on Anisimovna environment Saburo at 24°C for two days. The titration was started with a concentration of 10 mg/ml (dilution 1/10). As control was used a test tube, which was made only nutrient medium and the microorganism. The concentration in the last tube with no growth when is Kali for minimum inhibitory concentration. For the evaluation of bactericidal activity (minimum inhibitory concentration) of the test tubes with no growth did take the red Cup with mesopartner broth. Cup thermostatically at 37°C during the day. A bactericidal effect was observed in the absence of growth on solid nutrient medium.

As can be seen from table 2, the minimum inhibitory concentration is: for Staphylococcus spp., Streptococcus spp., Enterococcus spp., Shigella spp., Escherichia spp., Salmonella spp., Proteus spp., Acinetobacter spp., Citrobacter spp., Pseudomonas spp., Serratia spp., Klebsiella spp., Antracoides spp., Cryptococcus spp. - 12.5 mg/ml; for Microsporum, Trichophyton, Nocardia, Aspergillus, Candida, Actinomycetes, Entamoeba histolytica, Trichomonas vaginalis - 25 mg/ml; the minimum inhibitory concentration is: for Staphylococcus spp., Streptococcus spp., Enterococcus spp., Shigella spp., Escherichia spp., Salmonella spp., Proteus spp., Acinetobacter spp., Citrobacter spp., Pseudomonas spp., Serratia spp., Klebsiella spp., Antracoides spp., Cryptococcus spp. 25 mg/ml; for Microsporum, Trichophyton, Nocardia, Aspergillus, Candida, Actinomycetes, Entamoeba histolytica, Trichomonas vaginalis, 50 mg/ml Similar results were obtained when determining the antimicrobial activity of the compositions of EXAMPLES 2-11.

Assessment of the efficiency of the composition against influenza virus

To assess the effectiveness of the composition was the study of the composition of EXAMPLE 3. The study involved 50 patients aged 18 to 50 years old, with clinical manifestations Gris the PA. 25 patients was administered intranasally three times per day the composition of EXAMPLE 3, 25 patients were assigned to symptomatic treatment. In this study identified the following clinical effects of the composition of EXAMPLE 3: the observed acceleration edema fever and the prevalence in all age groups critical of the type of temperature reduction (on average 53% of patients). This effect is explained by the antiviral effect of the composition and is evidenced in the reduction in the duration of detection of viral antigen in smears from the mucous membranes of the nose. Significantly reduced the duration of cold and cough. Marked clinical efficacy of the composition of EXAMPLE 3 was accompanied by a protective effect against subsequent disease within 6 months. The number of episodes of flu per patient was 3 times lower in patients received therapy compositions of EXAMPLE 3. An important advantage of the treatment composition of EXAMPLE 3 was preventive effect in relation to the layers of secondary bacterial flora: receiving the composition from EXAMPLE 3 complications were recorded significantly less (23.7 per cent) in contrast to the comparison group (45%) (p<0,05). Evaluation of the transformation of forms in purulent rhinitis reliably confirmed this effect was 7.9% during therapy composition of EXAMPLE 3 and 20% of the comparison group.

Ozokeritovogo effect of the composition of EXAMPLE 3 was carried out on the basis of PCR diagnostics, implemented in 1-2-th and the 5-6th day of the disease. Half of the patients treated with the composition of EXAMPLE 3, the etiological agent on the 5-6th day of the disease were found, whereas in the placebo group - one-third of patients (p<0,05).

Similar data were obtained in the study of the compositions of EXAMPLES 1-2, 4-11.

Thus, on the basis of obtained data we can conclude that the antiviral effect of the compositions of EXAMPLES 1-2, 4-11 against the flu virus.

1. Pharmaceutical composition having antiviral and antibacterial activity, comprising, in wt.%:

L-N-2,6-diamino-hexanoyl-D-glucosamine0,001
L-y-glutamyl-cysteinyl-glycyl-Proline0,001
Lysine glycyrrhizinate0,001
Desoksiribonukleaza0,001
, Which hydroxypropyltrimonium
the amylopectin/glycerin of crosspolymer5,00
Hydroxypropyl-beta-cyclodextrin0,10
D,L-pyrrolidonecarboxylic N is coil of tilarginine 0,01
Escin0,01
Emulsifier0,01
Preservative0,01
The pH regulator0,01
Water demineralizedRest

2. Pharmaceutical composition having antiviral and antibacterial activity, comprising, in wt.%:

L-N-2,6-diamino-hexanoyl-ascorbyl phosphate0,001
N-pyrrolidin-carbamoyl-D-glucosamine0,001
Lysine ursolic0,001
Ribonuclease0,001
Modified acrylic thickener1,00
Hydroxypropyl-beta-cyclodextrin0,10
D,L-pyrrolidonecarboxylic N-Cocoyl of tilarginine0,01
Glycyrrhizin acid 0,01
Emulsifier0,01
Preservative0,01
The pH regulator0,01
Water demineralizedRest

3. Pharmaceutical composition having antiviral and antibacterial activity, comprising, in wt.%:

L-N-2,6-diamino-hexanoyl-hinokitiol0,001

N-pyrrolidin-carbamoyl-D-glucosamine0,001
Lysine betulinic0,001
Collagenase0,1
, Which hydroxypropyltrimonium
the amylopectin/glycerin of crosspolymer5,00
Hydroxypropyl-beta-cyclodextrin5,00
Chlorhexidine digluconate0,1
D-panthenol 5,00
Emulsifier5,00
Preservative1,00
The pH regulator1,00
Water demineralizedRest

4. Pharmaceutical composition having antiviral and antibacterial activity, comprising, in wt.%:

Guidolin0,001
Lysyl-poured-Proline Pamyat2,00
Proline ascent0,001
Lysozyme0,001
Hydroxypropyltrimonium maltodextrin
Crosspolymer0,50
Hydroxypropyl-beta-cyclodextrin0,10
D,L-pyrrolidonecarboxylic N-Cocoyl of tilarginine0,01
Extract of thuja0,01
Emulsifier 0,01
Preservative0,01
The pH regulator0,01
Water demineralizedRest



 

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2 cl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to using a polycarboxylic fullerene C60 derivative as a microbiocidal antiviral agent for the herpes simplex virus (HSV) and cytomegalovirus (CMV) inhibition. The polycarboxylic fullerene C60 derivative has the structural formula .

EFFECT: invention provides the agent for the emergency prevention of HSV and CMV sexual transmission.

7 dwg, 2 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: invention refers to veterinary immunology. A method for the vaccinal prevention of respiratory diseases in calves involves immunising 20-30-day-old clinically healthy calves three times every 10-12 days by subcutaneous injections of animal donor's hyperimmune serum containing anti-parainfluenza virus type 3 hemagglutinin antibodies in titre min. 1:1280, anti-rednose virus hemagglutinin antibodies in titre min. 1:256, anti-viral diarrhoea virus hemagglutinin antibodies in titre min. 1:1024, anti-respiratory syncytial virus hemagglutinin antibodies in titre min. 1:128, anti-rotavirus and anti-coronavirus hemagglutinin antibodies in titre min. 1:128, in a dose of 1 ml/kg of body weight; 15 days after the last injection, the animals are vaccinated by double administration of the inactivated combined vaccine Combovac for rednose, parainfluenza type 3, viral diarrhoea, respiratory syncytial, rota- and coronavirus diseases according to the instructions.

EFFECT: method provides higher postvaccinal immunity and the stimulated antibody production as a result of activating cell and humoral immunity and optimising the natural body resistance.

3 tbl, 2 ex

FIELD: medication.

SUBSTANCE: invention relates to medication against HIV/AIDS transmission through sexual contact and to method of HIV-infection prevention by introduction of said medication. Medication is made in form of suppository, which includes active substance and pharmacologically acceptable base. As active substance used is fraction of humic acids, extracted from oxidised brown coal, which possesses anti-HIV activity. As base used is cocoa butter or hard confectionery fat and emulsifier. Medication is introduced intravaginally 30 minutes before sexual intercourse.

EFFECT: invention is aimed at creation of safe microbicide with anti-HIV activity based on substances, extracted from natural sources.

2 cl, 6 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine, namely to biopharmaceutics, and can be applied for the preservation of an immunogenic composition in the suitable condition for introduction to an animal. For this purpose the claimed composition contains an antigen of foot-and-mouth disease (FMD) and an emulsion, which is a single emulsion at the first temperature lower than the temperature of the animal body, and the said emulsion is used at the second temperature between the first temperature and the body temperature. The method includes: provision of the composition, freezing the composition and storing the frozen composition until it is required for introduction to the animal. A group of inventions also relates to a method of testing the immunogenic composition.

EFFECT: group of inventions makes it possible to reach an increase of the storage term of a vaccine against FMD, based on the emulsion as an adjuvant, and it is possible to apply the process of slow freezing, without rendering an impact on adjuvant properties of the emulsion.

13 cl, 6 dwg, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to preparing alkylbenzyldimethylammoniumfluorides possessing antiviral and antibacterial action. The declared method consists in a reaction of a mixture of 1.5 M alkyl iodide of formula RJ, wherein R represents alkyl C8H17-C18H37, in absolute alcohol with dimethylbenzylamine at boiling; that is followed by a sequential ethanol stripping in vacuum, resolution of a residue in ethyl acetate, drying in diethyl ester, separation of an oil-precipitated intermediate product and residual ester stripping. The intermediate product is resolved in mixed ethanol and water in volume ratio 1:1 and titred in 10% aqueous AgF until iodide ions disappear from the solution; the solution is filtered, and the filter is boiled down, and crystallised from mixed methanol and hexane.

EFFECT: method provides preparing effective low-toxic therapeutic agent.

2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a novel 5-methyl-6-nitro-7-oxo-4,7-dihydro-1,2,4-triazolo[1,5-α]pyrimidinide l-argininium monohydrate of formula (1) The compound has antiviral activity with respect to group A and B strain viruses in in vitro and in vivo systems.

EFFECT: compound has low toxicity.

4 dwg, 3 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I), wherein A means morpholinyl, 1,4-oxazepamyl, piperidinyl, pyrrolidinyl or azetidinyl which is bound to N; R1 means C1-C6-alkyl group; R2 means bicyclic aryl group specified in 1H-indolyl, 1H-pyrrolo[3,2-b]pyridyl, quinolyl, naphthyl, 1H-pyrrolo[2,3-b]pyridyl, 5H-pyrrolo[3,2-d]pyrimidinyl, 7H-pyrrolo[2,3-d]pyrimidinyl, benzo[b]thiophenyl, imidazo[1,2-a]pyridyl, benzo[b]thiazolyl, 5H-pyrrolol[2,3-b]pyrazinyl and quinoxalinyl which can be substituted by R4; R3 means hydrogen or halogen atom; R4 means C1-C6-alkyl group, C1-C6-halogenalkyl group, OR1A, halogen, -(CH2)aOH, CN, NHCOR1A, SO2R1A or NHSO2R1A; R5 means C1-C6-alkyl group, -(CH2)aOH, -(CH2)aOR1B, halogen or CONH2; provided p is a plural number, R5 can be identical or different, or R5 can be combined with another R5; each of R1A and R1B independently means C1-C6-alkyl group; a is equal to 0, 1 or 2; n is equal to 1 or 2; p is equal to 0, 1, 2, 3, 4 or 5. Besides, the invention refers to intermediate compounds of formulas (IA) and (IB) for preparing the compounds of formula (I), to a preventive or therapeutic agent containing the compounds of formula (I), pharmaceutical compositions, using the compounds of formula (I) and to a method for preventing or treating diseases.

EFFECT: compounds of formula (I) as selective 5-HT2B receptor antagonists.

11 cl, 1 dwg, 18 tbl, 88 ex

Antimicrobial gels // 2535013

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine, particularly to aspects covering antimicrobial compositions, and described antimicrobial compositions, antimicrobial silicone gel based on the above antimicrobial composition, a wound dressing and methods for preparing them. Among other things, the antimicrobial compositions contain at least one alkenyl- and/or alkynyl-substituted polysiloxane, at least one polysiloxane containing silicone-linked hydrogen atoms, and at least one hydroxylation catalyst, at least one hydrophilic ingredient, at least one silver salt.

EFFECT: invention can be used for preparing a drug preparation to be used in treating burns, scars, bacterial infections, viral infections and/or mycotic infections.

19 cl, 5 dwg, 8 ex, 6 tbl

FIELD: veterinary science.

SUBSTANCE: method involves intramuscular injections of a drug preparation. The drug preparation is presented by a mixture of a medical solution of formaldehyde and normal saline at the weight portion ratio (2-6):(994-998). First, the preparation is injected into ill, latently ill and healthy animals starting from 3-month-old calves in two doses of 5-6 ml every 7-8 days during the period from September to November. Thereafter, the injections are continued for the ill animals only, but for no more than 5 weeks, and 5-7 days after the last injection the remaining ill animals are detected and isolated.

EFFECT: method enables recovering the farm effectively from necrobacteriosis.

1 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to veterinary science and aims at treating subclinical mastitis in cows. A preparation and a method for using it are declared. The preparation contains silver nanoparticles stabilised by submicrone titanium dioxide particles, poly-N-vinylpyrrolidone-2, and water in the following proportions, wt %: silver nanoparticles having a size of 200-300 nm 2.0×10-3, titanium dioxide particles having a size of 2-4 mcm 60.0×10-3, poly-N-vinylpyrrolidone-2 10.0, water - the rest up to 100.0. The method involves intracisternal introduction of the declared drug preparation in a dose of 10.0 ml twice a day for 2-4 days.

EFFECT: using the method enables providing the higher clinical effectiveness and reduces the length of recovery.

2 cl, 4 dwg, 7 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: declared group of inventions refers to veterinary science and is applicable for treating the animals suffering from bacteriosis and yeast mycosis. A declared preparation contains oxytetracycline hydrochloride, sulphadimine, ampicillin sodium, nistatine, a solvent and the active substance conduit dimethyl sulphoxide, the quick-relief anaesthetic lidocaine in the following proportions, wt %: ampicillin sodium 4.0-8.0, oxytetracycline hydrochloride 2.0-4.0, nistatine 1.0-2.0, sulphadimine 2.0-4.0, novocaine 0.25-0.5, lidocaine 0.25-0.5, dimethyl sulphoxide 10.0-20.0, 1,2-propylene glycol - the rest. A method of treating the animals consists in administering the declared preparation in a dose of 0.1-0.2 cm3 per 1 kg of body weight.

EFFECT: using the declared group of inventions is high-efficiency for treating the animals suffering from bacteriosis and yeast mycosis and enables improving livestock farms with an unfavourable incidence of bacteriosis and yeast mycosis.

5 cl, 9 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining a polymer conjugate of an indolocarbazole compound of formula (I), where R1, R2, R3, W1 and W2 represent hydrogen, X represents methoxy-polyethyleneglycol. The method includes the interaction of a polymer compound of formula (II) with an indolocarbazole compound of formula (III), where Y stands for a methoxygroup. The nvention also relates to a polymer conjugate of formula (I), a pharmaceutical composition, containing the conjugate of formula (I) as an active ingredient, and to the application of the polymer conjugate of formula (I).

EFFECT: obtaining the polymer conjugate of the formula with a high output, the polymer conjugate of the formula for treatment of skin pathologies and HMGB1-associated pathologies.

48 cl, 7 dwg, 7 tbl, 15 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to broad-spectrum antibacterial preparations. What is presented is an agent representing sodium dihydroxocystine diaminodiargenate possessing the antibacterial activity. The agent represents a complex C6H12Ag2N2Na2O6S2 of two silver ions with a disodium salt of natural amino acid L-cystine being coordinately linked. The method for preparing the agent involves adding an estimated amount of argentous oxide to a solution of cysteine disodium salt, mixing a reaction mixture at room temperature until argentous oxide dissolves completely, and precipitating a target product in alcohol.

EFFECT: new agent, sodium dihydroxocystine diaminodiargenate possesses the evident antibacterial action on the pathogenic strains of Staphylococcus, Proteus, Salmonella typhimurium, Pseudomonas aeruginosa, and also inhibits the yeast growth, has low toxicity and storage-stability.

1 tbl, 4 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to dentistry, and can be used for the preventing and treating infectious processes accompanying dental surgeries. That is ensured by intraoperative administration of a therapeutic antibacterial preparation of penicillin and an antibacterial preparation of the third-generation cephalosporin. The above preparation is administered daily for 3-5 postoperative days. The above preparation is administered intra- and post-operatively once a day intravenously drop by drop for 15-35 minutes in a dose of 30-55% of the recommended daily dose.

EFFECT: invention enables reducing a possibility of antibiotic dosage with complete withdrawal of repeated intra- and post-operative one-day administration of the antibiotics, with avoiding the developing early and late postoperative infectious-inflammatory complications.

3 cl, 5 ex

FIELD: pharmacology.

SUBSTANCE: as an antibacterial quinolone compound, a composition contains one of the quinolone compounds, namely lomefloxacin, or norfloxacin, or pefloxacin, or levofloxacin, or sparfloxacine, or moxifloxacin, or gatifloxacin, or gemifloxacin, or their acceptable salts; a preserving agent is paraben esters, or a mixture thereof, or benzalkonium chloride, or cetrimide, or chlorobutanol, or chlorhexidine, and an ointment base in the following proportions, wt %: quinolone compound - 0.05-0.9, preserving agents - 0.0,2, ointment base up to 100. Methods for preparing the composition provide the ointment homogeneity and stability.

EFFECT: group of inventions provides prolonging the period of therapeutic action of the ointment, reducing the dosage frequency.

6 cl, 6 tbl, 32 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a cefdinir acid salt, represented by formula I, where M represents Na+, K+, NH4+, or Cs+; Y represents SO42- or PO43-, and 1) if Y represents SO42-: if m=1, then n=1; if m=0.5, then n=1.5; and 2) if Y represents PO43-: if m=1, then n=2. Also claimed is a method of obtaining the cefdinir acid salt of formula (I), including preparation of a homogeneous mixture of cefdinir with a solvent, drop introduction into the homogenous mixture of cefdinir of a solution with an equimolar quantity of acid from the group: sulphuric acid, phosphoric acid, with further addition to the obtained transparent solution of an ammonium compound from the group: ammonium acetate, ammonium propionate, gaseous ammonia, aqueous ammonia solution, or with further addition to the obtained transparent solution of a compound of alkali metal from the group: sodium, potassium, cesium; or into the homogenous cefdinir mixture introduced by drop introduction is an equimolar amount of ammonium hydrosulphate or hydrosulphate of alkali metal from the group: sodium, potassium, or ammonium dihydrophosphate or alkali dihydrophosphate of alkali metal from the group: sodium, potassium, after which the obtained product of reaction, taking place for 15 minutes, is concentrated, crystallised, filtered and dried. In case, if acid or the compound contains a sulphate group, the obtained product is cefdinir acid salt, and if acid or the compound contains a phosphate group, the obtained product is cefdinir phosphate salt.

EFFECT: cefdinir acid salt, possessing high solubility.

8 cl, 2 tbl, 48 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a compound of formula (I)CE, wherein "-----" means a bond, V represents CH, and U represents CH or N, or "-----" means a bond, V represents CR6 and U represents CH, or also "-----" means a bond, V represents N and U represents CH, or "-----" is absent, V represents CH, and U represents CH2, NH or NR9; R0 represents H, or provided "-----" means a bond, can also represent C1-3alkoxygroup; R1 represents H, halogen, cyanogroup, C1-3alkyl or ethinyl; R2 represents H, acetyl or a group of formula -CH2-R3; R3 represents H, C1-3alkyl or C1-3hydroxyalkyl; R4 represents H, or provided n is other than 0, and R5 means H, can also represent OH; R5 represents H, C1-3alkyl, C1-3hydroxyalkyl, C1-3aminoalkyl, C1-3alkoxyC1-3alkyl, carboxyl group or C1-3alkoxycarbonyl; R6 represents C1-3hydroxyalkyl, carboxyl group, C1-3alkoxycarbonyl or a group -(CH2)q-NR7R8, wherein q is 1, 2 or 3 and each of R7 and R8 independently represents H or C1-3alkyl, or R7 and R8 together with a nitrogen atom to which they are attached, form a pyrrolodinyl or piperidinyl ring; R9 represents C1-3alkyl, 2-hydroxyethyl, 2-hydroxypropyl or 3-hydroxypropyl; A represents -(CH2)p-, -CH2CH2CH(OH)- or -COCH2CH(OH)-; G represents a phenyl group which is mono- or disubstituted in m- and/or n-position(s)by substitutes independently specified C1-4alkyl, C1-3alkoxygroup and halogen, or G means a group of one of formulas below G1 and G2, wherein Q means O or S, and X means CH or N; and each Y1, Y2 and Y3 represents CH, or one of Y1 and Y3 represents N, and the other one represents CH; and n is equal to 0, provided A represents -CH2CH2CH(OH)- or -COCH2CH(OH)-, and n is equal to 0, 1 or 2, provided A represents (CH2)p, wherein p is equal to 1, 2, 3 or 4, provided a sum of n and p is then equal to 2, 3 or 4; or a pharmaceutically acceptable salt of this compound.

EFFECT: compound of formula (I)CE or its pharmaceutically acceptable salt are applicable as a therapeutic agent for preventing or treating a bacterial infection.

29 cl, 2 tbl, 202 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to use of enalaprilat, a water-soluble substance based on [L-alanyl]-[L-proline] dipeptide, in medicine. Disclosed is use of enalaprilat as an agent for inhibiting formation of zinc-dependent beta-amyloid dimers.

EFFECT: inhibiting formation of zinc-dependent beta-amyloid dimers.

3 dwg, 1 tbl

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