"noopept"-base pharmaceutical composition

FIELD: medicine, pharmacology, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical composition comprising the medicinal preparation "Noopept" as an active component. Pharmaceutical composition for preparing solid medicinal formulations of the preparation comprises "Noopept", microcrystalline cellulose, polyvinylpyrrolidone, stearic acid or stearate as tablets. The medicinal preparation "Noopept" representing N-phenylacetyl-L-prolylglycine ethyl ester elicits the nootropic and neuroprotective activity in broad ranges of doses. The composition comprises small amounts of special additives, tablet release active component easily and invention provides its high bioavailability. Tablets satisfy all requirements of the State Pharmacopoeia of XI edition.

EFFECT: improved and valuable pharmaceutical and medicinal properties of pharmaceutical composition.

7 cl, 1 tbl, 3 ex

 

The invention relates to medicine, in particular, pharmacology, and relates to pharmaceutical compositions containing as active ingredient the drug noopept, and also to the said pharmaceutical composition in tablet form.

Drug noopept (ethyl ester of N-phenylacetyl-L-polyglycine) belongs to a new group of compounds that have different types of psychotropic activity, in particular antiamnesic, antihypoxic and anorectic action. The need for non-toxic and highly active nootropic drugs that can be used to treat deterioration of mental abilities caused by various destructive factors, there is still. The use of noopept in effective doses indicated for the treatment of patients suffering from mental drop caused by a brain injury, aging, senile dementia, and mentally retarded children; obesity; disorders of the Central nervous system as a result of chemical toxicity, mainly caused by saturnism; sickle cell anemia; withdrawal benzodiazepine, which manifests itself as aggression, anxiety, and seizures; and alcohol dependence. The active dose noopept obtained in the experiment on the different models is x pathological conditions, approximately 0.1-0.5 mg/kg For comparison, the level of active dose piracetam similar models is approximately 200-800 mg/kg (Patent RF №2119496, published in Bulletin of inventions No. 27, 1998). Noopept can be administered in dosage forms containing a small amount of the active ingredient (for example, 1-20 mg). But some physical properties of this medication cause impossibility of making compositions, suitable for tablets.

For example, noopept is a friable material with relatively low bulk density and bulk weight. This complicates the introduction of drugs in small tablet, uniform in density, hardness and other desirable for tablet properties. In addition, noopept has some undesirable flow characteristics, for example, electrified and can stick to the surface, for example on the surface forms for tabletting and the surface of the dies, causing problems in forming tablets, especially on high-speed press.

The essence of the invention is to provide pharmaceutical compositions on the basis of noopept that meets all the requirements of the State Pharmacopoeia XI edition.

This is achieved by the development of the pharmaceutical composition on the basis of noopept containing a therapeutically effective the top the number of noopept and targeted supplements, which use lactose, microcrystalline cellulose (MCC), polyvinylpyrrolidone, stearic acid or its salts in the following ratio of components per tablet, g:

Noopept0,001-0,020
MCC0,02-0,04
Lactose0,079 to 0.13
Polyvinylpyrrolidone0,04-0,008
Stearic acid or its salt0,001-0,002

As filler in the compositions of this invention can be used one or more compounds capable of receiving the tablets of the desired mass. It is desirable to apply the filler in a quantity close to the lower limit of interval weight filler. The preferred fillers are inorganic phosphate such as dibasic calcium phosphate, sugars such as lactose aqueous or anhydrous lactose, cellulose or derivatives of cellulose, such as microcrystalline cellulose.

As binders in the compositions of this invention can be applied one or more connections that can facilitate the granulation of noopept in more dense and larger and/or more free flowing particles. Preferred binders are cellulo is a or derivatives of cellulose, such as sodium carboxymethylcellulose (most preferably used in the amount of 2-6%), ethylcellulose (most preferably applied in amounts of 2-3%) hydroxyethylcellulose (most preferably applied in amounts of 2-5%), hydroxypropylcellulose (most preferably used in the amount of 2-6%), hypromellose (most preferably applied in amounts of 2-5%), or methylcellulose (most preferably used in the amount of 2-6%); gelatine (most preferably applied in amounts of 2-10%); polyvinylpyrrolidone (most preferably applied in amounts of 2-20%); or starch (most preferably applied in amounts of 5-20%).

As dezintegriruetsja substances in the composition of this invention can be applied one or more connections that can facilitate the dispersion of the tablets obtained from the composition, upon contact of the tablet with water. Preferred dezinfeciruyuhimi substances are cellulose or derivatives of cellulose such as sodium carboxymethyl cellulose (most preferably used in the amount of 2-6%), microcrystalline cellulose (most preferably applied in amounts of 5-15%), powdered cellulose (most preferably applied in kolichestvo-15%) or nutritionnelles (most preferably applied in amounts of 2-5%), crosspovidone (most preferably applied in amounts of 2-5%), pre-gelatinising starch (most preferably applied in amounts of 5-10%), sodium starch glycolate (most preferably applied in an amount of 2-8%) or starch (most preferably applied in an amount of 3-15%).

As a moving substance in the composition of this invention can be used one or more compounds able to resolve the problems associated with the formation of tablets, such as the release of the molding machine manufactured from the composition of the tablets, eliminating buildup on the surface of the upper or lower press to form tablets. Preferred slip agents are fatty acids or derivatives of fatty acids such as calcium stearate (most preferably used in quantities of 0.5-2%), glycerylmonostearate (most preferably used in quantities of 0.5-2%), glycerylmonostearate (most preferably applied in an amount of 0.2-2%), magnesium stearate (most preferably used in the amount of 1-2%).

As filler in the composition is anhydrous lactose. Microcrystalline cellulose is used as a disintegrator. For binding particles for granulation is used mainly 10% of the races is the thief of polyvinylpyrrolidone and 5% starch paste. As the moving substances are salts of stearic acid is predominantly magnesium stearate.

The pharmaceutical composition is made in a solid form, mostly in the form of tablets containing about 0.001-0,020 g noopept.

Methods of manufacturing:

Tablets can be obtained from the compositions of this invention any suitable method to obtain tablets. Preferably the tablets obtained from the compositions of this invention using wet granulation. One such method includes the following stages:

I obtain granules containing the active drug:

I.1 mixing noopept, part of the filler (preferably from approximately 5 to approximately 80% of the total amount of filler), part dezintegriruetsja substance (preferably from approximately 50 to approximately 80% of the total number dezintegriruetsja material), a binder, and to obtain a powder mixture, and optionally sieving the mixture (for example, grinding for grinding coarse particles);

I.2 re-mixing;

I.3 granulating the blend with a granulating liquid to obtain granules (for example, using a high-speed mixer/granulator);

I.4 drying of granules (for example, in a furnace or preferably in a fluidized bed dryer);

I.5 sieving the dried granules (EmOC is emer, grinding or sieving through a sieve);

II the mixture of granules of a certain size, obtained in stage (I.5), "winegrowing" song (composition, which contribute granules obtained in stage (I.5):

II.1 mix the rest of the filler, the rest of dezintegriruetsja substances (one or more of these components can be pre-mixed and the size of the particles is brought to a desired value (for example, by grinding for grinding coarse particles), and re-mixed with granules of a certain size, obtained in stage (I.5) with a granular mixture;

II.2 mixing lubricant with granular mixture;

III compressing the mixture obtained in stage (II.2), to obtain tablets (for example, with the use of a press for forming tablets). Solid source materials of these compositions preferably before applying sift through a sieve. The weight ratio of water (preferably purified water or water for injection) to the solid materials used in stage (I.3), is preferably in the range from approximately 25% to approximately 60%.

Possible ways to obtain tablets noopept wet granulation.

1. Granulation of medicinal substance with filler using a solution of a binding.

2. Granulating a mixture of drug is substances, filler and binder using pure solvent.

3. Granulating a mixture of medicinal substance with filler and part of the binder using the solution of the remaining portion of the binder.

4. Granulating a mixture of medicinal substance with filler using parts of the binder solution followed by the addition of dry binder in the finished granular material.

The tablets obtained from the compositions of this invention preferably contain (on a tablet) from about 1 to about 20 mg noopept. The mass of the obtained tablet is preferably from about 100 to about 200 mg. of the Composition of this invention can also be used for producing granulated products, granules for dispersion or capsules, the latter, for example, is filled with powder or above a granular drug or granules. The methods used to obtain such compositions are well known qualified specialists and can be used for the preparation of these dosage forms.

The TECHNOLOGICAL characteristics of the SUBSTANCE NOOPEPT
IndexThe value of the index
With pochesti, g/s0
Bulk density, g/cm30,255±0,023
The compressibility, N.94,73±15,319
Density, g/cm31,09±0,05
The TECHNOLOGICAL characteristics of the GRANULAR PHARMACEUTICAL COMPOSITION BASED ON NOOPEPT
IndexThe value of the index
Flowability, g/s10±0,3
Bulk density, g/cm30,45±0,03
The compressibility, N.87,5±11,54
Characteristics of the FINISHED TABLETS NOOPEPT
IndexThe value of the index
Raspadaemost, minNot more than 15
Compressive strength, N47,81
Abrasion, %99,7
The dissolution of the active substance for 45 min, %86,56

Example 1. A method of obtaining a pharmaceutical composition based on Noopept

In a clean, dry mixer sequentially load the pre is varicella sifted dry powders of Noopept (0.01 g), lactose (0.08 g) and microcrystalline cellulose (0.02 g), stirred for 10-15 minutes, the mixture is moistened with stirring 10%solution of polyvinylpyrrolidone (0.004 g) until a homogeneous hydrated mass. The wetted mass is passed through a granulator drum diameters of 1.2 mm, after which the mixture is spread out on trays with a layer of 1.5-2 cm and dried in a dryer at a temperature of 60±5°C for 10-12 hours, stirring occasionally, until a residual moisture content of 3.0±0,5%. To the resulting dry granulate add sifted dry stearate (0.001 g) and stirred for 10-15 minutes

Example 2. The method of producing tablets Noopept

In a clean, dry mixer pre-load dry sifted powders based on 1 tablet Noopept (0.01 g), lactose (0,065 g), microcrystalline cellulose (0.02 g), stirred for 10-15 min, the mixture is moistened with stirring 10%solution of polyvinylpyrrolidone (0.004 g) until a homogeneous hydrated mass. The wetted mass is passed through a granulator drum diameters of 1.2 mm, after which the mixture is spread out on trays with a layer of 1.5-2 cm and dried in a dryer at a temperature of 60±5°C for 10-12 hours, stirring occasionally, until a residual moisture content of 3.0±0,5%. To the resulting dry granulate add sifted dry stearate (0.001 g) and stirred for 10-15 minutes Received Mac is the tabletirujut on a rotary press on the punches with a diameter of 6 mm The tablet must have a face shape, smooth edges, a smooth, uniform surface. Raspadaemost 4-5 min, dissolution - 90% for 45 minutes in the water, uniformity of dosage meets the requirements of the global Fund XI, impurities - less than 0.5%, microbiological purity meets the requirements of the global Fund XI and amendment No. 3 (category 3A).

Example 3. The method of producing capsules Noopept

Getting granulate is carried out similarly to the method described in example 1. The obtained granulate capsulebuy in hard gelatin capsules. Capsules meet the requirements of pharmaceutical tool set GF XI. Raspadaemost 5-7 min, dissolution - 90% for 45 minutes in the water, uniformity of dosage meets the requirements of the global Fund XI, impurities - less than 0.5%, microbiological purity meets the requirements of the global Fund XI and amendment No. 3 (category 3A).

1. Pharmaceutical composition for production of solid dosage forms of the drug noopept, comprising as active ingredient a therapeutically effective amount of noopept, and as excipients lactose, microcrystalline cellulose, polyvinylpyrrolidone, stearic acid or its salt in the following ratio of components, g:

tr>
Noopept0,001-0,020
Lactose0,079 to 0.13
Microcrystalline cellulose0,02-0,04
Polyvinylpyrrolidone0,004-0,008
Stearic acid or its salt0,001-0,002

2. The pharmaceutical composition according to claim 1, characterized in that it is made mainly in the form of tablets.

3. The pharmaceutical composition according to claim 1, characterized in that it contains in each tablet 0,001-0,02 g noopept.

4. The pharmaceutical composition according to claim 1, characterized in that as lactose it contains mainly lactose anhydrous and/or lactose monohydrate.

5. The pharmaceutical composition according to claim 1, characterized in that as the salt of stearic acid is used primarily magnesium salt.

6. The pharmaceutical composition according to claim 1, characterized in that it is made mostly in the form of solid dosage forms.

7. Tablets drug noopept containing 0.01 g of noopept, 0,065 g of lactose, 0.02 g of microcrystalline cellulose, 0.004 g of polyvinylpyrrolidone, 0.001 g of magnesium stearate in one pill.



 

Same patents:

FIELD: medicine, pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to a method for preparing rosavine possessing the nootropic activity. Method for preparing rosavine involves three-fold extraction of rosewort (Rhodiola rosea L.) milled rhizomes with 70-90% ethyl alcohol in the definite ratio raw : extractant, evaporation of combined extracts under vacuum to obtain dense residue, chromatography separation on silica gel, evaporation of eluates and crystallization wherein the first extraction is carried out at definite temperature and two other extractions are carried out at definite temperature with reflux condenser. Proposed method provides increasing the yield of the end product from rosewort rhizomes and reducing duration of the technological process.

EFFECT: improved preparing method.

3 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: method involves introducing tacrolimus derivative of known formula (1) for stimulating nerve cell growth or regeneration. Another method is suggested for repairing transected peripheral nerve or spinal cord by making contact of the transected peripheral nerve ends or spinal cord with the compound (1) or by introduced the compound (1) to the patient and transplanting a transplant into peripheral nerve or spinal cord.

EFFECT: sharp growth of regenerated myelinated axons; improved motor function of feet; high neurotropic and low immunosuppressive activity level.

17 cl, 8 tbl

FIELD: internal diseases.

SUBSTANCE: patient is administered diet including 0.3-0.5 g/kg/day animal for 10 days followed by increase to dose 0.8-1 g/kg/day during 1 month, after which 5% glucose solution is administered intravenously in dose 400-500 ml for 1 weak, lactulose in dose 60-90 ml divided into 2-3 intakes for 4 weeks, and probiotics over a 2-weak period 30 min before meal time. Simultaneously, L-ornithine-L-aspartate is given during 10 days in dose 30-40 g a day divided into 2-3 intakes followed by dose 5-7 g thrice a day during 10 days.

EFFECT: achieved involution of neurological and psychical manifestations of encephalopathy, reduced hepatic coma development incidence, and increased protein tolerance in patients.

4 cl, 3 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of pyrimidine of the general formula (I) that possess properties of antagonists to adenosine A2-receptors and can be effective in relieve, for example, of defecation. In compound of the general formula (I) each R1 and R2 represents hydrogen atom; R3 represents hydrogen atom, halogen atom, amino-group, cyano-group, alkyl group comprising 1-6 carbon atoms, alkoxy-group comprising 1-6 carbon atoms, alkenyloxy-group comprising 2-6 carbon atoms, phenyl group that can be substituted with halogen atom, pyridyl group, furyl group or thienyl group; R4 represents pyridyl that can be substituted with a substitute chosen from the group comprising: hydrogen atom, halogen atom, amino-group, mono- or dialkylamino-group, aminoalkylamino-group wherein each has in alkyl residue from 1 to 6 carbon atoms, alkyl group comprising from 1 to 6 carbon atoms that can be substituted with halogen atom, hydroxy-group, amino-group, mono- or dialkylamino-group, alkoxycarbonyl wherein each has in alkyl residue from 1 to 6 carbon atoms, alkoxy-group comprising in alkyl group from 1 to 6 carbon atoms substituted with phenyl or pyridyl, hydroxyalkoxy-group comprising in alkyl residue from 1 to 6 carbon atoms, hydroxycarbonyl, alkoxycarbonyl comprising from 1 to 6 carbon atoms in alkyl residue, alkenyl group comprising from 2 to 6 carbon atoms, alkynyl group comprising from 2 to 6 carbon atoms, piperidinyl group that can be substituted with hydroxyl group, or represents group of the formula (IV): R5 represents phenyl that can be substituted with halogen atom, pyridyl group, thienyl or furyl group.

EFFECT: valuable biological properties of derivatives.

16 cl, 2 tbl, 185 ex

FIELD: organic chemistry of heterocyclic compounds, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of pyrimidine of the general formula (I) and their pharmaceutically acceptable acid-additive salts possessing properties of neurokinin-1 (NK) receptors antagonists. In the general formula (I): R1 means lower alkyl, lower alkoxyl, pyridinyl, pyrimidinyl, phenyl, -S-lower alkyl, -S(O2)-lower alkyl, -N(R)-(CH2)n-N(R)2, -O-(CH)n-N(R)2, -N(R)2 or cyclic tertiary amine as a group of the formula: R1 means lower alkyl, lower alkoxyl, pyridinyl, pyrimidinyl, phenyl, -S-lower alkyl, -S(O2)-lower alkyl, -N(R)-(CH2)n-N(R)2, -O-(CH)-N(R)2, -N(R)2 or cyclic tertiary amine of the formula: that can comprise additional heteroatom chosen from atoms N, O or S, and wherein this group can be bound with pyrimidine ring by bridge -O-(CH2)n-; R2 means hydrogen atom, lower alkyl, lower alkoxyl, halogen atom or trifluoromethyl group; R3/R3' mean independently of one another hydrogen atom or lower alkyl; R4 means independently of one another halogen atom, trifluoromethyl group or lower alkoxyl; R means hydrogen atom or lower alkyl; R means independently of one another hydrogen atom or lower alkyl; X means -C(OH)N(R)- or -N(R)C(O)-; Y means -O-; n = 1, 2, 3 or 4; m means 0, 1 or 2. Also, invention relates to a pharmaceutical composition comprising one or some compounds by any claim among claims 1-19 and pharmaceutically acceptable excipients. Proposed compounds can be used in treatment, for example, inflammatory diseases, rheumatic arthritis, asthma, benign prostate hyperplasia, Alzheimer's diseases and others.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

21 cl, 1 tbl, 76 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to using phenylethenyl- or phenylethynyl-derivatives as antagonists of glutamates receptors. Invention describes using compound of the general formula (I):

wherein each among R1, R2, R3, R4 and R5 means independently of one another hydrogen atom, (C1-C6)-alkyl, -(CH2)n-halogen, (C1-C6)-alkoxy-group, -(CH2)n-NRR', -(CH2)n-N(R)-C(O)-C1-C6)-alkyl, phenyl or pyrrolyl that can be unsubstituted or substituted with one or more (C1-C6)-alkyl; each among R, R' and R'' means independently of one another hydrogen atom or (C1-C6)-alkyl; A means -CH=CH- or C≡C; B means ,, , , or wherein R6 means hydrogen atom, (C1-C)-alkyl, -(CH2)n-C(O)OR, or halogen atom; R7 means hydrogen atom, (C1-C6)-alkyl, -(CH2)n-C(O)OR', halogen atom, nitro-group or oxodiazolyl group that can be unsubstituted or substituted with (C1-C6)-alkyl or cycloalkyl; R8 means hydrogen atom, (C1-C6)-alkyl, -(CH2)n-OH, -(CH2)n-C(O)OR'' or phenyl; R9 means (C1-C6)-alkyl; R10 and R11 mean hydrogen atom; R12 means -(CH2)n-N(R)-C(O)-(C1-C6)-alkyl; R13 means hydrogen atom; each R14, R15, R16 and R17 independently of one another means hydrogen atom or (C1-C6)-alkoxy-group; each R18, R19 and R20 independently of one another means hydrogen atom; R21 means hydrogen atom or (C1-C6)-alkyl; R22 means hydrogen atom, (C1-C6)-alkyl or (C1-C6)-alkyl comprising one or more substitutes chosen from groups hydroxy- or halogen atom; R23 means hydrogen atom, (C1-C6)-alkanoyl or nitro-group; each among R24, R25 and R26 independently of one another means hydrogen atom or (C1-C6)-alkyl; n = 0, 1, 2, 3, 4, 5 or 6; X means -O- or -S-; Y means -CH= or -N=, and its pharmaceutically acceptable salts used in preparing medicinal agents designates for treatment or prophylaxis of disorders mediated by mGluR5-receptors. Also, invention describes compounds of the formula (I-A), compound of the formula (I-B-1) given in the invention description, and a medicinal agent used in treatment or prophylaxis of disorders mediated by mGluR5-receptors.

EFFECT: valuable medicinal properties of compounds.

44 cl, 1 tbl, 44 ex

FIELD: medicine.

SUBSTANCE: method involves introducing recombinant human granulocytic colony-stimulating factor.

EFFECT: enhanced effectiveness of treatment; increased number of stem cells and their improved homing in lesion foci without polypragmasia effects.

5 tbl

FIELD: medicine.

SUBSTANCE: method involves introducing Hypoxen at a peroral dose of 0.5 g 40 min before premedication with Benzodiazepine series tranquilizer.

EFFECT: enhanced effectiveness in retaining psychic and motor functions after surgical intervention.

FIELD: medicine, veterinary science.

SUBSTANCE: invention relates to a method for improving the cognitive function in mammals and humans. Method involves administration in mammal needing in such treatment bis-[(2-hydroxyethyl)-N,N,N-trimethylaminium] succinate. This provides improving different cognitive functions in mammals being without the development of by-side effects and results to the improvement of the life quality and social adaptation in persons suffering with these disorders.

EFFECT: improved method for enhancing cognitive function.

2 tbl, 3 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical composition possessing capacity to release the therapeutically effective dose of active substance rivastigmin and showing the time-controlled pattern. The pharmaceutical composition is designated for treatment of patients suffering with Alzheimer's diseases dementia from small to middle severity degree. Compositions show safety and time-controlled release pattern of active substance rivastigmin.

EFFECT: valuable medicinal and pharmaceutical properties of composition.

5 cl, 2 tbl, 7 ex

FIELD: pharmaceutical industry, in particular production of stable ginger extract-based preparation.

SUBSTANCE: claimed preparation contains dry ginger extract and polyvinyl pyrrolidone as stabilizing ancillary agent in specific ratio. Method for production of said preparation includes extraction of ground ginger roots to produce liquid extract solution, solution concentration to produce viscous extract, dilution of viscous extract, addition of polyvinyl pyrrolidone solution as stabilizing ancillary agent to natural extract, stripping and drying. Also disclosed is galenia preparation, containing abovementioned stabilized ginger extract-based preparation and additional ancillary agents such as silicium dioxide, maltodextrin, magnesium stearate, cellulose or carboxymethylstarch. Such preparation is useful in treatment of dyspeptic disorders, naupthia sypptoms, as antiemetic agent, antidiabetic agent, etc. Stable ginger extract-based preparation obtained by abovementioned method and galena preparation based on the same are characterized by constant ratio of [6]-gingerol to [6]-shogaol.

EFFECT: stable therapeutic agent based on ginger extract.

13 cl, 2 dwg, 7 tbl, 4 ex

FIELD: medicine, pharmacy, pharmacology.

SUBSTANCE: invention relates to a pharmaceutical composition comprising the medicinal preparation afobasol as an active component. Indicated pharmaceutical composition is prepared as a tablet formulation and comprises medicinal preparation afobasol, i. e. 5-ethoxy-2-[2-(morpholino)ethylthio]benzimidazole hydrochloride, eliciting the expressed anxiolytic activity in the broad range of doses. The composition comprises small amounts of special additives, such as lactose, starch, polyvinylpyrrolidone, stearic acid or stearate. Invention provides easy release of active component that provides its high bioavailability. Tablets satisfy all requirements of the State Pharmacopoeia of XI edition.

EFFECT: improved and valuable pharmaceutical and medicinal properties of pharmaceutical composition.

8 cl, 1 tbl, 3 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a solid medicinal formulation as a chewing tablet possessing the antacid effect. Proposed pharmaceutical composition comprises magnesium carbonate and calcium carbonate as active components, methylcellulose, talc, stearate, aromatic principles and sorbitol as accessory substances wherein state is represented by magnesium state or calcium state. Invention provides preparing a chewing tablet possessing rapidly active effective antacid effect and can be used for oral intake in case of unexpressed organic pathology of digestive tract including patients with diabetes mellitus. The final technical effect exceeds effect caused by the known properties of components only.

EFFECT: improved and valuable pharmaceutical properties of formulation.

2 cl, 1 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates, in particular, to a solid pharmaceutical composition used in treatment and prophylaxis of osteoporosis. The composition comprises derivative of bis-phosphonic acid that involves carbohydrate alcohol-base nuclei, preferably, mannitol and uniformly distributed in a homogenous mixture of active component and filling agents. Also, invention discloses a process for preparing the composition described above. Invention eliminates the chemical instability problem of derivatives of bis-phosphonic acid that are ready for using in solid medicinal formulations and during the process for their preparing, good physical properties (strength) of the solid medicinal formulation.

EFFECT: improved and valuable medicinal and pharmaceutical properties of composition.

12 cl, 2 tbl, 1 ex

FIELD: pharmaceutics.

SUBSTANCE: a solid pharmaceutical composition contains therapeutically efficient quantity of peptide as a pharmacological active substance, crospovidone or povidone, and an agent that favors peptide's introduction. A peptide is being calcitonin, salmon's calcitonin preferably. The above-mentioned agent is being 5-CNAC (N-(5-chlorsalicyloyl)-8-aminocaprylic acid), preferably, disodium salt 5-CNAC. The composition suggested provides high biological availability of peptides, such, for example, as calcitonin.

EFFECT: higher efficiency of application.

9 cl, 5 ex, 4 tbl

FIELD: pharmaceutics.

SUBSTANCE: the present innovation deals with mixing dry St. John's wort extract with additional substances followed by compressing, sieving, treating compact extract with additional substances including titanium dioxide and talc with subsequent tableting, moreover, compressing should be carried out with highly dispersed silicon dioxide only, at a certain portion of silicon dioxide supplemented before compression, one should apply the particles of compact extract at certain distribution according to the size of particles to achieve certain bulk density of particles of compact extract and density after compression; the particles of compact extract should be additionally covered with combination of aerators chosen out of sodium-crosscarmelose, sodium-carboxymethyl starch. The above-mentioned method enables to obtain tablets at high portion of extract, high characteristics of decomposition and releasing of biologically active substances.

EFFECT: higher efficiency.

5 cl

FIELD: medicine.

SUBSTANCE: the present innovation deals with a solid antibacterial preparation that contains efficient quantity of sitafloxacin or its salt, or its hydrates, and tartaric acid at the quantity ranged 0.1-1 M/0.5-1 M sitafloxacin. Tartaric acid provides steady sitafloxacin absorption at high dosage out of digestive tract.

EFFECT: higher efficiency.

2 cl, 4 ex, 4 tbl

FIELD: chemico-pharmaceutics.

SUBSTANCE: the present innovation deals with decreasing blood level of homocysteine and normalizing myocardial state in case of ischemic cardiac disease. The suggested preparation contains pyridoxine hydrochloride (vitamin B6), cyanocobalamin (vitamin B12), folic acid (vitamin Bc) being designed as a tablet at the following ratio of components in g per 1 tablet of 0.31-0.37 g: pyridoxine hydrochloride 0.003-0.005; cyanocobalamine 0.000005-0,000007; folic acid 0.004-0.006; additional substances - the rest. The composition suggested is of high synergistic effect.

EFFECT: higher efficiency of therapy and prophylaxis.

1 ex, 1 tbl

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to tablet containing cetirizine and pseudoephedrine used in treatment of allergic disorders. Invention relates to a tablet comprising two separate layers. Invention relates to combinations of two pharmaceutical substances representing cetirizine and pseudoephedrine prepared in the weight ratio pseudoephedrine to cetirizine = 12-30. Pseudoephedrine-containing segment comprises inert pharmaceutical excipients and an alkalinizing agent. Pharmacokinetics patterns of cetirizine and pseudoephedrine are similar practically with pharmacokinetic pattern of medicinal preparations containing each of these components taken separately in the same doses. Invention provides the development of combination of pharmaceutical substances useful in treatment being without adverse effects.

EFFECT: improved and valuable medicinal properties of tablet.

44 cl, 5 tbl, 3 ex

FIELD: medicine, pharmaceuticals.

SUBSTANCE: invention relates to new method for production of granules containing 5-aminosalicylic acid, as well as to new method for production of peroral pharmaceutical composition for treatment of non-specific ulcerative colitis and Cron's disease. Said composition includes 5-aminosalicylic acid as active ingredient, and granulation is carried out by using water as solvent.

EFFECT: granules containing 5-aminosalicylic acid with increased strength, glib surface and narrow granule size distribution.

24 cl, 3 ex, 12 tbl, 9 dwg

FIELD: bioorganic chemistry, biochemistry, pharmacy.

SUBSTANCE: invention relates to novel aspartyl derivatives of histamine of the general formula (I): , wherein R means hydrogen atom (H), or , or that are able to modulate activity of enzymes of antioxidant protection - superoxide dismutase (SOD) and catalase. Also, invention relates to using the known compounds of the general formula (I) for the same designation wherein at the same values of X the value R represents acetyl group, and to their pharmaceutically acceptable salts. Also, invention relates to a pharmaceutical composition possessing capacity to modulate activity of SOD and catalase and comprising the effective amount of compound of the general formula (I), and to a method for synthesis of compounds of the general formula (I). Method involves interaction of pentafluorophenyl ester Nα-Z-, β- or α-benzyl ester of aspartic acid with histamine followed by hydrogenolysis without isolation of intermediated protected derivatives of aspartyl histamine.

EFFECT: improved method of synthesis, valuable biochemical properties of derivatives.

12 cl, 3 tbl, 2 sch, 2 dwg, 8 ex

Up!