Method for producing a pharmaceutical formulation of rocuronium bromide in the form of a stable lyophilisate and pharmaceutical composition obtained using said method

FIELD: pharmaceutics.

SUBSTANCE: present invention relates to pharmaceutical industry and to a method for producing a pharmaceutical formulation of rocuronium bromide in the form of a stable lyophilisate for injection or infusion. Method includes placing the solution rocuronium bromide in ampoules or bottles in a sublimation chamber, where the solution is frozen to (-41)-(-49)°C at the rate (-12)-(-13) deg/h during 7-9 hours, held for 6-9 hours, then the ampoules (bottles) are heated at a rate of 7-10 deg/h during 7-9 % to 20-25 °C and kept at this temperature for 5-9 hours. Pharmaceutical formulation includes rocuronium bromide as an active ingredient, sodium chloride or potassium chloride, acid to bring pH to 3.8-4.8 and water for injections.

EFFECT: pharmaceutical formulation storage life increases up to 5 years.

2 cl, 3 tbl, 1 ex

 



 

Same patents:

FIELD: medicine.

SUBSTANCE: anaesthetising patients with chronic pain syndrome undergoing a cyclophotocoagulation surgery involves the intravenous administration of the hormonal preparation dexamethasone in a dose of no more than 8 mg followed by the anxiolytic droperidol in a dose of no more than 2.5 mg 5 minutes prior to the operation before the peribulbar anaesthesia. A peripheral block in the form of the peribulbar anaesthesia involving administration of no more than 6 ml of a local anaesthetic follows. At the moment the surgical procedure starts, benzodiazepin, e.g. diazepam, is administered in a dose of no more than 5 mg.

EFFECT: achieving adequate anaesthesia in the given category of patients by blocking all the links of a pathological pain chain.

1 ex

FIELD: medicine.

SUBSTANCE: dexamethasone 8 mg and ketoprofen 100 mg is administered intravenously once prior to the operation. A lumbar plexus is blocked in a combination with a parasacral block and inserting perineural catheters to administer weak 0.2% Ropivacaine, local anaesthetic 20 ml. Paracetamol 1,000 mg is administered intravenously 30 minute before the operation is completed. After the operation is completed, the perineural catheter of the lumbar plexus is used to infuse 0.2% Ropivacaine 300 ml at 6-8 ml/hour for 4-5 days. Ketoprofen 100 mg is administered intramuscularly twice a day for 3 days. Through the perineural catheter of the parasacral plexus, 0.2% Ropivacaine 10 ml is administered twice every 12 hours.

EFFECT: method provides the adequate anaesthesia in the given category of patients by having an effect on primary pain components, as well as ensures the continuous and prolonged anaesthesia both intra-, and postoperatively, prevents the stable and chronic pain syndrome and the motor block of the extremities, reduces a rate of toxic complications.

1 ex

FIELD: medicine.

SUBSTANCE: preanaesthetic medication preceding gynaecological surgeries under general anaesthesia is ensured by prescribing diazepam 10mg, nefopam 10mg and ketoprofen 100mg intramuscularly 30-40 min before the surgery.

EFFECT: method enables reaching the sedative and analgesic effect of the preanaesthetic medication by the complementary action of preparations with no undesired side effects, requiring no time consumption and expensive equipment.

3 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: as active component pharmaceutical composition contains dihydrochloride of 9-(2-morpholine ethyl)-2-(4-fluorophenyl)imidazo[1,2-α]benzimidasol, and as additional substances - fillers, binding, sliding and film coatings, in quantities, given in the invention formula. Composition can be made in form of solid medication form, mainly in form of tablets and capsules.

EFFECT: obtained solid medication forms satisfy the requirements of the State Pharmacopoeia.

7 cl, 2 dwg, 3 tbl, 14 ex

FIELD: medicine.

SUBSTANCE: at the initial stage of the intraoperative period, immediately before the local anaesthesia and the femoral artery puncture, ketorolac tromethamine is administered intravenously as an analgesic, and propofol as a sedative agent. Ketorolac tromethamine is administered in a dose of 15-75 mg, while propofol is administered in a dose of 50-250 mg.

EFFECT: method prevents developing pain and psychoemotional responses caused by the given interventions, including postoperatively by the fast development of the adequate analgesic effect accompanied by the controlled sedation level.

1 tbl, 10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to benzimidazole derivatives of general formula (I) and to their pharmaceutically acceptable salts, mixed stereoisomers and enantiomers, wherein R1 is L1C(O)OL2C(O)OT; R2 is unsubstituted C1-C10alkyl; L1 is a bond; L2 is unsubstituted C2-C10alkylene; T is C1-C10alkyl. Also, the invention refers to a pharmaceutical composition of the compound of formula (I) and a method of anaesthetising on the basis of using the compound of formula (I).

EFFECT: there are prepared new imidazole derivatives effective as an anaesthetising agent.

15 cl, 9 dwg, 15 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a new compound, namely to (S)-enantiomer of 1'-{[5-(trifluoromethyl)furan-2-yl]methyl}spiro[furo[2,3-f][1,3]benzodioxol-7,3'-indole]-2'(1'H)-one of formula (I), and a method for preparing it which is effective for treating diseases and conditions, such as pain, an intensity of which can be reduced or relieved by modulating potential-dependent sodium channel gatings.

EFFECT: invention refers to the pharmaceutical composition of the above compound, methods of treating and a method of relieving an ion flux through the potassium channel gating in a cell.

10 cl, 5 tbl, 6 dwg, 11 ex

FIELD: biotechnology.

SUBSTANCE: aqueous composition for anaesthesia is proposed, which comprises propofol as an active agent, the PEG-660-12-hydroxystearate as a solubiliser, benzyl alcohol, or chloroethanol or parabens as preservative, the tocopherol and arginine or glycine at a specific content of components wt %. The GABA agonists can be additionally added to the composition, e.g. aminophenyl-butyric acid, local anesthetics such as lidocaine, alpha-2-adrenoceptor agonists such as xylazine. The method is proposed for implementing anaesthesia comprising administering to a patient of an effective amount of the claimed composition.

EFFECT: invention provides low toxicity of dosage form and high efficiency.

5 cl, 3 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: what is involved is infusion therapy with crystalloid solutions at 15 ml/kg of a patient's body weight. That is followed by puncturing and catheterising an epidural space at the level of ThVII-ThVIII according to the standard practice and introducing a test dose of 2% lidocaine 3 ml. If observing no signs of intrathecal introduction of local anaesthetics 10 minutes later, a basic dose containing 0.75-1% naropin 10 ml or 0.25-0.5% marcaine 10 ml and clofelin 3-5 mcg/kg is introduced. Total intravenous anaesthesia follows 20 minutes after pre-medication with atropine 0.01 mg/kg, 1% diphenylhydramine 1 ml and relanium 10 mg and urethral catheterisation. A narcosis is induced with propofol in a dose of 2 mg/kg. Anaesthesia is maintained with propofol 2-4 mg/kg·h. After that, within the first hour following the detoxification, naloxone 12 mg is introduced intravenously; a naloxone measurement rate is supposed to make 0.8 mg/h for 4-5 following hours of general anaesthesia. The repeated introduction of 0.75-1% naropin 6 ml or 0.25-0.5% marcaine 6 ml and clofelin 2-3 mcg/kg into the epidural space is performed 90 minutes later. After the procedure is terminated, and the patient recovers, prolonged epidural analgesia is conducted by introducing 0.2% naropin 10 ml and clofelin 1 mcg/kg into the epidural space every 4 hours for 24-48 hours.

EFFECT: method provides safety of ultrafast opioid detoxification and prolongs the remission in the given category of patients.

1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to anaesthesiology and resuscitation, and may be used in epidural anaesthesia. That is ensured by administering slowly intravenously a basic dose of the local anaesthetic: 0.2-1% naropin or 0.2-0.5% marcaine, or 1-2% lidocaine; 1% Sol. Nicotini acidi 1% - 0.5-1 ml into the epidural space 10-20 minutes later. After 5-10 minutes, nicotine test results are visually evaluated by determining a clear interface of skin colour - hyperemic and normal - along an axillary line from both sides. The normal skin interface corresponds to the sympathetic block.

EFFECT: method provides higher accuracy and simplification of measuring the sympathetic block.

1 ex

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

FIELD: medicine.

SUBSTANCE: pharmaceutical composition in form of lyophilisate for preparation of solution for parenteral application for tuberculosis treatment represents lyophilisate of prothionamide salt, which includes in composition additional substances, and in case of addition of pharmaceutically acceptable diluents is applicable for intravenous introduction. Pharmaceutical composition is obtained by dissolution of prothionamide substance in pharmaceutically acceptable acid, taken in equimolar ratio or with up to 20% excess, sterile filtering of solution, pouring in reservoirs and lyophilic drying. Finished medication is provided with pH corrector (sodium hydrocarbonate solution).

EFFECT: medication is stable in storage and is applied for preparation of solution for intravenous drip-feed.

9 cl, 2 ex

FIELD: medicine.

SUBSTANCE: pharmaceutical composition in form of lyophilisate with complexiant for preparation of solution for parenteral application to treat tuberculosis represents complex in form of prothionamide lyophilisate, which includes in composition water-soluble derivatives of β-cyclodextrine, and in case of addition of pharmaceutically acceptable diluent applicable for intravenous introduction. Pharmaceutical composition is obtained by dissolution of prothionamide substance in pharmaceutically acceptable acid (such as chloromethane, sulphuric, ascorbic, citric, etc.) in equimolar ratio or with up to 20% excess, obtaining complex with cyclodextrine derivative in equimolar ratio or with excess of cyclodextrine derivative up to 20%, sterile filtering of solution, pouring into reservoirs and lyophilic drying. As diluent applied is solution of sodium chloride, glucose and other pharmaceutically acceptable solutions. Finished medication is provided with pH corrector (sodium hydrocarbonate solution).

EFFECT: medication is stable in storage and is applied for preparation of solution for intravenous drip-feed.

11 cl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of lyophilisation of a composition, which contains purified antithrombin III (AT III) and a crystallised substance, selected from alanine, mannitol, glycine or NaCl. The claimed method includes freezing the composition at a temperature from -52°C to -60°C for 6-15 hours, annealing the composition at -30°C for 1 hour, re-freezing the composition at a temperature from -52°C to -60°C for 2-15 hours at keeping the product temperature between -48°C and -52.7°C for 4-10 before lyophilisation and drying the composition with obtaining a lyophilised cake. The invention also relates to a pharmaceutical set, which contains the said lyophilised cake and a liquid reagent.

EFFECT: invention provides obtaining the lyophilised composition, containing AT III, which preserves its activity and stability.

14 cl, 24 dwg, 5 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to pharmaceutics and medicine, and concerns protein and peptide stabilisation formulation which contains a hydrophilic polymer, a mixture of polyalcohol and sugar, wherein a weight ratio of polyalcohol to sugar makes from 2:1 to 5:1 (wt %), a detergent, and wherein the formulation is free from stabilising proteins. A composition and a kit for treating a disease or a composition caused by hyperactive cholinergic innervation of muscles or endocrine glands in a patient, and contain the above formulation and peptide, protein or a mixture thereof.

EFFECT: group of inventions provides the better protein stability in the absence of stabilising proteins.

13 cl, 4 ex

FIELD: chemistry.

SUBSTANCE: highly dispersive pharmaceutical composition contains from 5 to 100 mg of budesonide per 1 g of β-glycine. Composition is characterised by bulk density 0.008-0.035 g/cm3 and consists of porous spherical agglomerates with diameter to 50 mcm and separate fragments, formed in the process of destruction of agglomerates, which represent complex of joined into perforated layers separate particles. Composition is obtained by method, based on dispersing into tank with liquid nitrogen solutions of initial substances in mixed solvent tetrahydrofurane-water, in which concentration of tetrahydrofurane constitutes 20-25 wt %, solvents are removed from obtained by dispersion mixture of solid phases in dry nitrogen flow under pressure 100 Pa until pressure drop less than 2 Pa by step-by-step temperature increase in the interval from -196°C to -5°C to decompose clathrate hydrate formed in the system tetrahydrofurane-water and to remove components of used mixture of solvents by sublimation, then from -5°C to +30°C to remove residual moisture, with application of initial substances budesonide and α-glycine in mixed solvent tetrahydrofurane-water with ratio budesonide from 0.25 to 0.9 mg/g of solvent, α-glycine from 8 to 50 mg/g of solvent.

EFFECT: improved method of composition obtaining.

2 cl, 5 dwg, 2 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: as medications composition includes beclomethazone dipropionate and salbutamol, with beta-glycine serving as carrier. Composition is obtained by dispersing solutions of initial medications in mixed solvent into tank with liquid nitrogen with further removal of solvents from obtained by dispersion mixture solid phases in dry nitrogen flow under pressure 600±20 mtorr to pressure drop less than 8 mtorr with stopping nitrogen supply by step-by-step increase of temperature: in the interval from -196°C to -15°C, then from -15°C to +30°C. As initial substances used are: beclomethazone dipropionate 1.9-5.1 wt %, salbutamol 1.9-10.2 wt %, alpha-glycin to 100%. Composition of mixed solvent includes tetrahydrofurane 5-15 wt %, tert-butyl alcohol 15-5 wt %, water 77-80 wt %.

EFFECT: invention provides obtaining highly dispersed pharmaceutical composition of salbutamol and beclomethazone dipropionate.

2 cl, 10 dwg, 3 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of pharmaceutics and represents method of treating prostate cancer, which includes introduction to patient of composition, which contains degarelix lyophilisate or its pharmaceutically acceptable salt and excipient, dissolved in solvent, in initial dose 200-300 mg of degarelix in concentration 20-80 mg of degarelix per ml of solvent with the following after 14-56 days after initial dose supporting dose 320-55 mg of degarelix in concentration 50-80 mg of degarelix per ml of solvent, possibly with one or more than one following additional supporting dose 320-550 mg of degarelix in concentration 50-80 mg of degarelix per ml of solvent, introduced with interval from 56 days to 112 days between each supporting dose.

EFFECT: invention provides long release of degarelix from obtained depot of medication without increase of occurrence of side effects.

11 cl, 1 ex, 2 dwg, 4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to pharmaceutical compositions based on botulinum toxin and is intended for diagnostic or therapeutic introduction to a subject. A lyophilised or dried in vacuum composition contains botulinum toxin, stabilised with a non-protein excipient; a compound, selected from the group, consisting of the first monosaccharide, the first disaccharide, the first trisaccharide and the first alcohol, obtained by the reduction of the first monosaccharide; and a compound, selected from the group, consisting of the second monosaccharide, the second disaccharide, the second trisaccharide, the second alcohol and amino acid. In the other aspect the pharmaceutical composition contains botulinum toxin, stabilised with the non-protein excipient; polyethyleneglycol and a compound, selected from the group, consisting of monosaccharide, disaccharide, trisaccharide and amino acid. The pharmaceutical composition can contain botulinum toxin, stabilised with the non-protein excipient, polyvinylpyrrolidone; and disaccharide. The pharmaceutical composition of botulinum toxin, which does not contain an animal protein, includes botulinum toxin; a compound, selected from the group, consisting of the first monosaccharide, the first disaccharide, the first trisaccharide and amino acid.

EFFECT: application of the group of inventions provides the stable pharmaceutical composition for diagnostic or therapeutic introduction to a subject.

6 cl, 8 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: invention represents a medicinal preparation storage system comprising a chamber (3) accommodating at least two lyophilised active and/or additive substances (W1, W3, W5, W7) together in at least one chamber (3).

EFFECT: improving the system.

6 cl, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents a pharmaceutical composition for control of pain accompanying individual's joint diseases containing hyaluronic acid, which is cross-linked by cycling a double bond in a group of cinnamic acid in partially amidated hyaluronic acid presented by formula (1) to form a cyclobutane cycle, wherein in the above formula, Ar represents a phenyl group, n is equal to an integer 2 or 3; HA represents a carboxy residue of hyaluronic acid, and m represents a relation of amidation of hyaluronic acid to all the carboxyl groups and is equal to 3-50% in relation to all the carboxyl groups, and a pharmaceutically acceptable carrier, wherein the pharmaceutical composition represents a product for injection, wherein the pharmaceutical composition represents the product for injection, wherein the amount of the cross-linked hyaluronic acid makes 1 wt % at the total amount of the product for injection, wherein a single dose of the product for injection makes 2-3 ml, wherein the pharmaceutical composition represents a single-use preparation, which is administered every 13 weeks and more.

EFFECT: invention provides the extremely long analgesic action after the single administration, earlier onset of the analgesic action.

15 cl, 1 dwg, 5 tbl, 1 ex

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