Method of producing water-soluble lyophilisate of 4-(3-oxo-3-ethoxypropanoyl)amino)benzoic acid possessing anti-ischemic and antioxidant activity

FIELD: pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and represents a method of producing a water-soluble lyophilisate, involving producing a combined solution of an active substance and a compound containing hydroxyl and amino groups (amino alcohol), characterized by that the active substance is 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid (EPABA) possessing anti-ischemic and antioxidant activity. Amino alcohol is selected from a group of N-methylglucamine or tris(hydroxymethyl)aminomethane; herewith the said substance and amino alcohol taken in the molar ratio from 1:1 to 1:10 are dissolved in water, the solution is added with an acid agent up to pH 6.8-7.5, neutral solution is filtered, frozen and dried by sublimation.

EFFECT: invention enables to obtain water-soluble stable neutral lyophilisates of EPABA corresponding to process requirements of preparations for parenteral administration.

3 cl, 4 dwg, 4 tbl, 2 ex

 



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to cardiovascular surgery and cardiology, and deals with complex correction of immunoinflammatory responses of cardiovascular bed. For this purpose, in case of presence of high level of circulating immune complexes and/or complement in patient, three sessions of plasmapheresis in accordance with conventional methods, and in case of low level of IgG and reduced phagocytic activity of neutrophils and monocytes, as well as in case of confirmed autoimmune process, a course of intravenous infusions of human polyvalent immunoglobulin is carried out in accordance with conventional schemes.

EFFECT: method provides reduction of both hypo- and hyperactive disorders in immune system of patients and resulting increase of efficiency of treatment of cardiovascular system diseases.

3 ex

FIELD: medicine.

SUBSTANCE: limb ischemia is simulated in a male Wistar rat anaesthetised with chloral hydrate in a dose of 250-300 mg/kg by the surgical removal of femoral, popliteal arteries and the front shin artery. That is followed by introducing a prepared mononuclear fraction of the autologous bone marrow in a dose of 4×106 cells in an amount of 200 mcl. The above is introduced into the ischemic limb from two points in an amount of 100 mcl each. One point is found directly under the femoral arch paravasally within the anatomical position of collaterals of the inner iliac artery and its branches. The other point is located in the calf muscle on an anteriolateral surface of the midleg.

EFFECT: more effective experimental treatment ensured by stimulating the collateral blood flow in the ischemic limb and improving the arterial blood flow from the proximal to distal parts of the limb.

1 ex, 1 tbl

FIELD: medicine.

SUBSTANCE: early postoperative period involves administering low-molecular heparins and anti-inflammatory agents. Anti-inflammatory therapy requires administering cycloferon according to the schedule: 2 tablets of cycloferon 0.15 mg on the first preoperative day, 2 tablets on the first postoperative day, 2 tablets in the morning on the 2nd, 4th, 6th postoperative day, and further, every third day throughout 1 postoperative month (on the 9th, 12th, 15th, 18th, 21st, 24th, 27th, 30th day).

EFFECT: method provides the effective prevention of postpericardiotomy syndrome with a lower risk of side effects by administering cycloferon according to the developed schedule requiring non-steroidal anti-inflammatory agents and glucocorticosteroids.

2 ex, 3 tbl

Treatment // 2554801

FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine, and concerns using a human Annexin-1 antibody (Anx-A1), which has the sequence SEQ ID NO: 23 for treating a disease caused by abnormal T-cell activation. The group of inventions also concerns a method of treating a disease caused by abnormal T-cell activation, involving administering a therapeutic amount of the above antibody into an individual in need thereof; using the above antibody for producing a therapeutic agent for treating a disease caused by abnormal T-cell activation.

EFFECT: group of inventions provides treating the disease caused by abnormal T-cell activation.

9 cl, 11 ex, 22 dwg

FIELD: medicine.

SUBSTANCE: invention concerns rehabilitation of elderly patients with ischemic heart disease (IHD) accompanied by chronic heart insufficiency (CHI) following myocardial in myocardial infarction (MI). That is ensured by administering Omacor, a preparation of omega-3-polyunsaturated fatty acids in the remote period, 6 or more months after the suffered MI with underlying a standard drug therapy 60 minutes before the graduated walking.

EFFECT: this complex of the drug preparations combined with the graduated physical exercises provides higher tolerance to physical exercises, improving the cardiovascular function and normalising the lipid exchange that in turn leads to reducing a number of unfavourable cardiovascular episodes and delaying CHI.

2 ex, 5 tbl

FIELD: medicine.

SUBSTANCE: claimed is the application of N-(2-adamantyl)-hexamethylenimine hydrochloride (himantane) as a medication for treating cerebral circulation disorders and brain traumas. An ability of himantane to reduce animal morbidity and increase cognitive and motor indices in case of its introduction after 3.5 hours after modelling a hematoma in rats and further introduction for 4 days was determined, which testifies to its possessing the neuroprotective potential on the model of the intracerebral post-traumatic hematoma. The technical result consists in the realisation of the claimed purpose: it has been shown that himantane in a dose of 5 mg/kg in case of intravenous introduction causes the increase of cerebral circulation in the rats' brain after ischemic brain affection without changing the level of arterial pressure.

EFFECT: medication did not produce a significant impact on the blood supply of the brain of the intact animals and did not cause a change in the heart rate and respiratory rate.

1 dwg, 6 tbl

FIELD: medicine.

SUBSTANCE: group of inventions relates to medicine, namely to neurology, and deals with the treatment of ischemic stroke. For this purpose the introduction of ubidecarenone by injection, mainly intravenous, is carried out.

EFFECT: introduction of the medication provides the reduction of the zone of brain tissue injury and reduction of neurologic deficiency expression due to the accumulation of ubidecarenone, possessing an expressed neuroprotective action, in brain tissues.

7 cl, 4 dwg, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula , which is a methylhydrofumarate (MHF) prodrug. In formula (I), radicals and symbols have the values specified in the patent claim. The invention also refers to a pharmaceutical composition containing the declared methylhydrofumarate drugs, to using the declared methylhydrofumarate drugs and the pharmaceutical composition containing them, for treating diseases, such as psoriasis, asthma, multiple sclerosis, inflammatory intestinal disease and arthritis, and to a method of treating the above diseases.

EFFECT: higher oral bioavailability and plasma MHF, dimethylfumarate and/or other metabolites.

47 cl, 1 tbl, 54 ex

FIELD: medicine.

SUBSTANCE: antianginal therapy is accompanied by a primary discrete plasmapheresis in a refrigerate centrifuge PC-6 having a rotating speed of 2,000 rpm for 15 minutes at a temperature of 22°C in number of 5 sessions every second day. One session involves removing the whole blood in an amount of: 2 flexible PVC packages x 450 ml if the patient's body weight index is from 18 to 29.9 kg/m2, 3 flexible PVC packages x 450 ml if the patient's body weight index is over 30 kg/m2. The total volume of the removed plasma makes 600-900 ml. The circulating blood volume is replaced with 0.9% NaCl in an amount of half as much as the removed plasma volume. Once the plasmapheresis course is completed, the blood is exposed to ultraviolet light generated by OVK-3 apparatus for at wave length more than 400 nm in number of 5 procedures every second day.

EFFECT: effective treatment of the given category of the patients by improving the haemorheology, normalising the lipid spectrum without increasing liver enzymes with preserving the hepatic function, decreasing the dyslipidemia level and functional class of angina in the patients with limited use of statins with underlying cholestasis.

2 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: urgent surgery on vessels of a lower extremity involves placing an electrode for transoesophageal atrial temporal pacing (TOTP). That is followed by administering a beta adrenergic blocking agent intravenously in a load dose to achieve a decreased heart rate of ≤ 60 beats per minute. The dose of the beta adrenergic blocking agent is reduced to a maintaining one with preserving a sinus decreased heart rate from 72 to 74 beats per minute for the whole surgery and for 2-3 days thereafter as it may be necessary. The surgical repair of coronary arteries is performed at least 3-4 weeks after the surgery on the vessels of the lower extremities.

EFFECT: therapeutic approach provides preventing minor cardiac output syndrome and other cardiovascular adverse effects accompanying the repair surgeries on the arteries of the lower extremities that enables a coronary artery bypass surgery 3-4 weeks later.

2 cl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely to selenium nanocomposites of natural hepatotrophic galactose-containing polysaccharide matrixes, representing water-soluble orange-red powders containing zerovalent selenium (Se0) nanoparticles sized 1-100 nm in the quantitative content of 0.5 - 60 wt %, possessing antioxidant activity for treating and preventing redox-related pathologies, particularly for treating toxic liver damage, to a method for producing and to an antioxidant agent containing the above nanocomposites.

EFFECT: invention provides the targeted agent delivery to liver cells, as well as higher agent accessibility and lower toxic action of selenium.

7 cl, 11 ex, 4 tbl

FIELD: medicine.

SUBSTANCE: method involves chelation of ferric (III) ions both in vivo, and in vitro with using 2-ethyl-6-methyl-3-hydroxypyridine succinate (Mexidol) to produce a stable stained complex having a high molecular weight and a complex (organic-inorganic) composition not identified among the known compounds.

EFFECT: high effectiveness of the chelation process and low toxicity of Mexidol that makes it promising for biomedical application.

4 dwg, 3 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to novel compound - 5(6)-nitro-1-(thietanyl-3)-2-ethoxybenzimidazole, inhibiting peroxidation of lipids.

EFFECT: novel compound, possessing useful biological properties, has been obtained.

2 cl, 1 dwg, 2 ex

FIELD: medicine.

SUBSTANCE: invention represents a mixture of two structural isomers: 2,6-di(1,7,7-trimethylbicyclo[2.2.1]hept-2-yl)-4-methylphenol and its diastereomers, and 2-(1,7,7-trimethylbicyclo[2.2.1]hept-2-yl)-6-(2,2,1-trimethylbicyclo[2.2.1]hept-5-yl)-4-methylphenol, and their diastereomers with the ratio of the first and second structural isomer isomers from 60:40 wt % to 95:5 wt %.

EFFECT: extension of the arsenal of means, possessing simultaneously haemorheological, anti-aggregate, anti-thrombogenic, retinoprotecting, endothelium-protecting, neuroprotecting, anti-arrhythmia and anti-ischemic activity, enhancing the cerebral blood flow.

4 dwg, 20 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: what is presented is using Histochrom (same as echinochrome A or pentahydroxyethyl naphthoquinone) as an agent able to prevent pulmonary fibrosis developed under cytostatic agents. The invention can be used for the pharmacological prevention and correction of the pulmonary tissue disorders caused by administering the cytostatic agents.

EFFECT: preventing hypertrophy of interalveolar connective tissue in the lungs associated with administering bleomycin.

4 dwg, 1 tbl

FIELD: medicine.

SUBSTANCE: drops possessing antiviral and immunomodulatory effects characterised by the fact that they represent a 95% ethanol infusion of wild strawberry leaves and fruit specified in: red raspberry fruit, mountain ash fruit, bilberry fruit, blood-red hawthorn fruit, cinnamon rose fruit; 15-25 mg of the substance in 1 ml of the infusion.

EFFECT: drops possess pronounced antiviral and immunomodulatory effects.

15 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: melanin having water-solubility of at least 80% and an paramagnetic centre concentration of at least 8·1017 spin/g is administered orally into the animals having been exposed to the radiation in a dose high enough to cause a spinal radiation injury; melanin is administered after dissolved in distilled water in the effective concentration. Melanin water is used as drinking water for the mice having been exposed to single and fractionated acute radiation, which is able to cause acute radiation disease. Melanin water is taken from the 1st to 30th day following the single radiation, or from the 1st day of the fractionated radiation to the 30th day on completion of the radiation.

EFFECT: higher survival rate, faster recovered haemopoiesis, body weight and orientation and motion activity.

7 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention provides a composition having antioxidant properties in the form of a tablet, comprising an active agent based on nicotinamide adenine dinucleotide in reduced form (NADH) and inert filling agents, characterised by that the active ingredient is a complex which is a mixture of 10 wt % NADH with 63 wt % vegetable fats, 17 wt % beeswax and 10 wt % chlorophyll, and the inert filling agents are in the form of microcrystalline cellulose, Macrogol 6000, intense sweetener and a food flavourant.

EFFECT: invention provides a new tablet form of NADH.

1 ex

FIELD: medicine.

SUBSTANCE: invention refers to a pharmaceutical composition with anti-ischemic and antioxidant activity in the form of tablets or capsules, and a method for preparing it. The composition contains 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid in an amount of 40 to 80 wt %, an amino-containing compound and pharmaceutically acceptable excipients. The amino-containing compound is specified in a group of trometamol, methyl glucamine and L-lysine; 1 mole of 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid is accounted for 0.05 to 0.25 mole of the above amino-containing compound. The composition also contains lactose, microcrystalline cellulose, calcium stearate and other pharmaceutically acceptable excipients. According to the method for preparing the composition, taking 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid and amino-containing compound in molar ratio 1:0.05 to 1:0.25, pre-mixing, moisturising with a aqueous or alcohol solution of a binding agent, adding pharmaceutically acceptable excipients in such an amount to provide the content of 4-((3-oxo-3-ethoxypropanoyl)amino)benzoic acid from 40 to 80 wt %, granulating the mixture, drying and producing tablets or capsules according to the known technique.

EFFECT: implementing the above application.

6 cl, 7 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: claimed is the application of 5(6)-nitro-1-(1,1-dioxothietanyl-3)-2-chlorobenzimidazole of formula (I) , earlier known as the means with broncholytic and spasmolytic activity, as the means, inhibiting peroxide oxidation of lipids.

EFFECT: realisation of the claimed purpose.

1 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine and deals with histidine-trehalose composition, stable after storage, containing antibody T1h, histidine buffer, trehalose and non-ionic surface-active substance.

EFFECT: invention provides reduction of quantity of highly molecular weight proteins (HMWP) by approximately 20% by weight with respect to initial quantity of HMWP in histidine-trehalose composition within five weeks.

4 cl, 5 ex, 27 dwg

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