Sodium chloride-containing moxifloxacin compositions

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.

6 cl.

 



 

Same patents:

FIELD: antibiotics, chemical technology.

SUBSTANCE: crystallization of azithromycin dihydrate is carried out by alkalization of an aqueous-organic azithromycin salt with the ratio water/solvent = from 1:1 to 3;1 and up to pH value 8-10. Methanol, ethanol, isopropanol, acetonitrile or dioxane can be used as a solvent. Method provides enhancing stability and homogeneity of the end crystalline product.

EFFECT: improved crystallizing method.

1 dwg, 3 ex

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

, 3)benzimidazole-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: organic chemistry, chemical technology.

SUBSTANCE: invention relates to new 5-aryl-1-phenyl-4-heteroyl-3-hydroxy-3-pyrroline-2-ones of the formula:

wherein (1) X means sulfur atom (S); R means (CH3)2CH; (2) X means sulfur atom (S); R means (CH3)3C; (3) X means oxygen atom (O); R means (CH3)3C. Compounds of the formula (I) are prepared by interaction of the corresponding heteroylpyruvic acid methyl ester with mixture of aniline and aromatic aldehyde in acetic acid medium at short-time heating. Compounds elicit an anti-bacterial activity with value MIC = 3.9-7.8 mcg/ml as compared with 62-1000 mcg/ml for analogue.

EFFECT: valuable properties of compounds.

1 tbl, 3 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention describes a method for preparing derivatives of benzoxazine and describes a method for preparing compound represented by the formula . Method involves of compound represented by the formula (I): with compound represented by the formula (II-1-a): in the presence of a base to form compound represented by the formula (III-1-a): followed by reduction of this compound to compound represented by the formula (IV-a): , interaction of this compound with compound represented by the following formula: to form compound represented by the formula (V-a): and the following treatment of this compound in the presence of a base to obtain compound represented by the formula (VI-a): , treatment of this compound with compound of boron trifluorine and its conversion by this manner to the boron chelate compound represented by the following formula: followed by reaction of this compound with 4-methylpiperazine to obtain compound represented by the following formula: followed by cleavage and elimination of boron chelate of this compound. In each of above given formulas X1, X2 and X3 represents independently halogen atom; R1 represents a leaving group; R3 represents hydrogen atom or carboxyl-protecting group; R4 represents hydroxyl-protecting group; each R5 and R6 represents independently alkyl group comprising 1-6 carbon atoms; R7 represents carboxyl-protecting group; Y represents alkoxy-group comprising 1-6 carbon atoms, halogen atom or dialkylamino-group (wherein alkyl groups can be similar or different and each represents alkyl group comprising 1-6 carbon atoms). Also, invention describes variants above described method, methods for preparing intermediate compounds and intermediate compound. Invention provides industrially favorable methods for preparing intermediate compounds that are useful for preparing compounds with antibacterial properties.

EFFECT: improved preparing methods, valuable properties of compounds.

96 cl, 102 ex

FIELD: applied immunology.

SUBSTANCE: composition contains, wt parts: borax decahydrate1-25, sodium thiosulfate pentahydrate 10-5-10-4, potassium carbonate 30-150, refined sugar 30-200, and water 100-200 per 100 wt parts of sodium metasilicate pentahydrate. In addition to its capability of improving resistance to diseases, body weight increase, productivity of agricultural plants, quality of crop, and ripening term (harvest time), composition according to invention possesses nonspecific immunostimulating activity, including production of antibodies and enhancement of immunity through activation of immunocytes thereby maximally strengthening vaccination effect regarding diseases caused by malignant neoplasm viruses.

EFFECT: increased assortment of immunostimulating agents.

10 cl, 11 dwg, 12 ex

FIELD: silicon-containing substances, medicine, pharmacy.

SUBSTANCE: invention describes silicon glycerates eliciting transcutaneous conductivity of medicinal agents with the composition of the formula: Si(C3H7O3)4 x xC3H8O3 wherein 3 ≤ x ≤ 10 with dynamic viscosity 4.6-28.5 Pa x s (20 ± 0.5°C). Compounds are prepared by interaction of tetraethoxysilane with glycerol in the mole ratio = 1:(7-14) in the presence of tetrabutoxy-titanium (0.06 mole/mole of tetraethoxysilane) and removal of formed ethyl alcohol in heating of reaction mass to 120-130°C and keeping at this temperature for 3 h, not less. Also, invention describes glycerohydrogels based on element-organic glycerates containing water and gel-forming additive that contain as element-organic glycerates silicon glycerates with the composition of the formula Si(C3H7O3)4 x xC3H8O3 wherein 3 ≤ x ≤ 10 as they contain electrolyte as a gel-forming additive in the following ratio of components, wt.-%: silicon glycerates, 8.2-65.1; electrolyte, 0.1-0.6, and water, the balance. Proposed compounds - silicon glycerates and glycerohydrogels based on thereof are physiologically active substances eliciting transcutaneous conductivity of medicinal agents with possible broad spectrum of their applying in medicine.

EFFECT: valuable medicinal properties of compounds.

2 cl, 2 tbl, 2 dwg, 7 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of aminomethylpyrrolidine of the formula (I) , their salts or hydrates wherein R1 represents aryl with from 6 to 10 carbon atoms or heteroaryl wherein heteroaryl is a five-membered ring or a six-membered ring and comprises from 1 to 2 heteroatoms taken among nitrogen, oxygen and sulfur atom; aryl and heteroaryl can comprise one or more substitutes taken among the group consisting of halogen atom or (C1-C6)-alkoxyl; each radical among R2, R3, R4, R5, R6, R7 and R8 represents hydrogen atom (H) independently; Q represents incomplete structure representing by the following formula: wherein R9 means (C3-C6)-cyclic alkyl that can be substituted with halogen atom; R10 means hydrogen atom (H); R11 means hydrogen atom (H), NH2; X1 means halogen atom; A1 represents incomplete structure representing by the formula (II): wherein X2 means hydrogen atom (H), halogen atom, halogenmethoxyl group, (C1-C6)-alkyl or (C1-C6)-alkoxyl group; X2 and above indicated R9 can be combined to form the ring structure and inclusion part of the main skeleton and such formed ring comprises oxygen, nitrogen or sulfur atom as a component atom of the ring and the ring can comprise (C1-C6)-alkyl as a substitute; Y means hydrogen atom (H). Compounds of the formula (I) elicit an antibacterial effect and can be used for preparing a therapeutic agent.

EFFECT: valuable medicinal properties of compounds.

2 tbl, 61 ex

FIELD: medicine, pharmaceutical industry.

SUBSTANCE: invention relates to an antibacterial, anti-inflammatory, antiviral, antiherpetic agent used for treatment of vulvovaginitis, palanitis, ballanopostitis induced by microorganisms, candidas, viruses, chlamydia, trichomones and infections of herpes simplex virus and for treatment of acne also. Invention relates to an antibacterial, anti-inflammatory, antiviral, antiherpetic medicinal agent used for treatment of diseases transferred by sexual way, in particular, to vulvovaginitis, palanitis, ballanopostitis induced by microorganisms, candidas, viruses, chlamydia, trichomones and infections of herpes simplex virus and for treatment of acne. The medicinal agent comprises a mixture of cream-like base (vehicle) and an alcoholic extract from leaves, fruits and stems of plant Tribulus terrestris (active component). This active component comprises active substance from Tribulus terrestris with the high content of steroid saponins. Also, invention relates to a method for preparing an antibacterial, anti-inflammatory, antiviral, antiherpetic medicinal agent that involves analysis of parts of plant Tribulus terrestris for gathering and further extraction, namely to a sample of leaves, fruits and stems of plant Tribulus terrestris gathered in the definite time period. Method involves addition of deionized water, stirring and evaluation of the level of water and foam in a mixer. After proving readiness of plant Tribulus terrestris for gathering samples of leaves, fruits and stems of plant Tribulus terrestris are taken. Samples are dried, milled and deionized water is added. The prepared aqueous mixture is treated in mixer, the level of water and foam is evaluated in an aqueous mixture. The prepared mixture is remained for precipitation, filtered, ethyl alcohol is distilled off and the concentrated aqueous extract is prepared. The prepared active component is added to the cream base (vehicle) or to a base (suppository). Agent promotes to effective treatment of vulvovaginitis, palanitis, ballanopostitis induced by microorganisms, candidas, viruses, chlamydia, trichomones and infections of herpes simplex virus and to treatment of acne also.

EFFECT: valuable medicinal properties of agent.

5 cl, 5 dwg

FIELD: biotechnology, medicine, in particular treatment, prevention and diagnosis of diseases, associated with Neisseria meningitides.

SUBSTANCE: Claimed protein includes one or more N. meningitides protein fragments with known amino acid sequences, wherein said fragment contains one or more antigen determinants and has not more than 1977 amino acid from SEQ ID NO:1 and/or not more than 1531 amino acid from SEQ ID NO:2 which are described in specification with the proviso, that general protein sequence is not characterized by amino acid sequences represented in NO:1 and NO:2. Each claimed protein is encoded by nuclear acid (NA) with nucleotide sequence that defines protein amino acid sequence according to gene code. Peptides and nuclear acid of present invention are useful in drug production for treatment and prophylaxis of infections induced neisseria, as well as in production of diagnostic reagent for detection of neisseria or specific antibodies. Aldo disclosed is peptide- or NA-based pharmaceutical composition in effective amount with acceptable carrier. Said composition is useful for treatment of N. meningitides mediated infection. For prophylaxis composition is applied in vaccine form. Invention makes it possible to overcome diversity of neisseria antigen properties.

EFFECT: improved method for neisseria infection prophylaxis and treatment.

24 cl, 2 tbl

FIELD: organic chemistry, pharmaceutical industry.

SUBSTANCE: invention relates to clathrate of azithromycin hydrate with 1,2-propyleneglycol of formula I , wherein m =1-2 and n = 0.20-0.40. Method for production of target compound includes azithromycin dissolution in acetone followed by addition of 1,2-propyleneglycol and water in solution, formed crystal filtering, washing with water and drying. Also disclosed is pharmaceutical composition for microbial infection treatment based on clathrate of formula I.

EFFECT: azithromycin with reduced hygroscopicity and increased storage stability.

7 cl, 7 dwg, 2 tbl, 4 ex

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: medicine, pharmacy.

SUBSTANCE: treatment involves using the injection solution based on water-soluble prednisolon formulation containing sodium salt and accessory additive. Prednisolon sodium phosphate is used as prednisolon water-soluble formulation, and anhydrous sodium hydrogen phosphate and sodium dihydrogen phosphate dihydrate taken in the ratio = (1.375-1.5):1, respectively, are used as sodium salt, and propylene glycol is used as an additional additive in the following ratio of components, wt.-%: prednisolon sodium phosphate (as measured for prednisolon), 2.5-3.5; anhydrous sodium hydrogen phosphate, 0.045-0.055; sodium dihydrogen phosphate dihydrate, 0.03-0.04; propylene glycol, 12-17, and injection water, the balance, up to 100%. Invention can be used in producing hormonal preparation prednisolon in injection formulation for treatment of rheumatism, infectious nonspecific polyarthritis, bronchial asthma, leukemia and other diseases. Invention provides enhancing stability of prednisolon-containing solution and prolonged storage time.

EFFECT: improved and valuable properties of solution.

3 tbl, 2 ex

FIELD: medicine, pharmacology, pharmacy.

SUBSTANCE: invention relates to the injection solution based on nalbuphine hydrochloride eliciting the expressed analgesic effect, and to a method for its preparing. The injection solution comprises the following components, wt.-%: nalbuphine hydrochloride, 0.8-2.2; buffer mixture, 0.5-3.5; stabilizing agent, 0.15-0.25; Trilon B (chelating component), 0.001-0.2, and water, the balance. Invention provides preparing the domestic preparation with analgesic effect and stability for above 2.5 years.

EFFECT: improved and valuable medicinal properties of solution.

11 cl, 1 tbl, 5 ex

FIELD: pharmaceutical industry.

SUBSTANCE: composition contains cellulose derivatives, glycosaminoglycanes, oligosaccharides, novocain or mercain (both as local anestetics), non-steroidal anti-inflammatory agent, adrenalin, glycerol, and purified water at specified proportions of components.

EFFECT: achieved protection of cornea against mechanical damage due to prevented access of air bubbles and blood under lens, best visualization of fundus of eye, and reduced operation time.

2 ex

FIELD: organic chemistry.

SUBSTANCE: invention relates to methods for stabilizing compounds based on benzimidazole or its physiologically acceptable salt. One variant of a method involves incorporation of crospovidone having small diameter of particles and at least one compound taken among sodium hydroxide and potassium hydroxide into benzimidazole-base compound represented by the formula (1):

wherein Het1 means:

Het2 means:

R1 and R2 are similar or different and taken among hydrogen atom, methoxy- and difluoromethoxy-group; R3 is taken among hydrogen and sodium atom; R4, R5 and R6 are similar or different and taken among group comprising hydrogen atom, methyl, methoxy-, methoxypropoxy- and trifluoroethoxy-group, or its physiologically acceptable salt. Other variants involve applying at least one compounds taken among sodium hydroxide and potassium hydroxide on core formed by incorporation of crospovidone into benzimidazole-base compound represented by the formula (1) or its physiologically acceptable salt, enteric soluble coating, or intermediate coating and the following applying additional enteric soluble coating on it. Also, invention relates to a method for prevention of the benzimidazole-base compound color change or its physiologically acceptable salts and this method involves incorporation of crospovidone and at least one compound taken among sodium hydroxide and potassium hydroxide into benzimidazole-base compound by cl. 1, or its physiologically acceptable salt.

EFFECT: improved stabilizing method.

7 cl, 2 tbl, 8 ex

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