Composite regulating metabolic processes and method for its preparing
FIELD: medicine, medicinal biochemistry, pharmaceutical technology.
SUBSTANCE: invention proposes the composite that comprises complex of vitamins D3, B6, C, K and calcium salts, citric acid, lactose and sorbitol as the special supplement, and lubricating agent and correcting agent for taste and/or odor. The method for preparing the composite involves mixing the above said components and if necessary the following tableting process of the prepared mixture. The new composite shows stability of quality indices in the store process being among them index "the content of vitamin D3" that provides the fitness time above 2 years and absence of by-side adverse toxic effect that is typical for destruction products of active components.
EFFECT: improved preparing method, improved and valuable properties of composite.
7 cl, 1 tbl, 4 ex
The invention relates to the field of medicine and is suitable for the treatment and prevention of conditions involving vitamin D deficiency and calcium in the body, including the prevention and treatment of osteoporosis and its complications (fractures).
Osteoporosis is a systemic skeletal disease characterized by reduced bone mass per unit volume and a violation of microarchitecture of bone tissue leading to enhanced bone fragility and a high risk of fracture. The main focus in the treatment of osteoporosis is a pathogenetic principle, which is to normalize the components of bone remodeling - the suppression of increased bone resorption and/or stimulation of bone formation. The main mineral component of bone is calcium, however, the application of a source of calcium by itself was ineffective for inhibiting the loss of bone density and almost not effective to prevent violations of the bone structure.
A tool that provides a multi-faceted effect on the bone tissue and on both the process of bone remodeling, is vitamin D. Vitamin D regulates metabolic processes in the body, primarily supports calcium and phosphate homeostasis, and its deficiency in the body can be accompanied by the development of different forms of the OST is the porous and some other pathological conditions. This led to the use of vitamin D in clinical practice as a means of regulating metabolic processes, including for the treatment and prevention of osteoporosis [Mashkovsky PPM Medicines, Vol.2, ed. 14-e, M.: Publishing house New Wave, 2001, p.93].
The drug of vitamin D can be used in combination with a calcium source. Calcium, in the form of pharmacologically acceptable salts, and vitamin D, as a rule, are assigned to the patient at the same time. However, each drug has its own specific dosage forms such as tablets calcium salt and drops of vitamin D. Therefore, it is difficult compliance with the relative doses of calcium and vitamin D, which is very important for the effectiveness of therapy, especially if it is held for a long period. In addition, this calls for a separate packaging for these products.
In this regard, attempts have been made to combine calcium and vitamin D in a single dosage form. So, in the international application WO 94/06435 described pharmaceutical composition, which contains a combination of a source of calcium and vitamin D. the Drug can be made in the form of tablets, however, used excipients are not disclosed. In U.S. patent No. 6080431, 2000, proposed a combined composition for the treatment of osteoporosis, comprising a salt of calcium and vitamin D. Site is titanium option perform the composition is in liquid form, therefore, the source of calcium imposed significant limitations of the calcium salt is selected from the group comprising soluble salts: citrate/malate calcium or a mixture.
In order to enhance therapeutic effect of the combination of a source of calcium and vitamin D can be supplemented with other biologically active compounds. In the patent of Russian Federation № 2152216, 2000, describes a composition for protecting bones from vacuum containing a source of calcium, vitamin D and trace elements boron, copper, magnesium, manganese and zinc (in the form of corresponding salts). Present trace elements perform mainly restorative function, so well-known structure is proposed as a dietary food Supplement. However, in order for the product could be widely applied, it should have less contraindications, can be both safe and effective. Hence, the introduction of a very large number of different minerals is not always justified, and in some cases is contraindicated.
The closest technical solution to the claimed invention is a combination composition of the source of calcium and vitamin D (RF patent No. 2154466, 2000). As the target additive composition includes universal binder for granulation of dry product or in a humid environment), preferably polyvinylpyrrolidone or mi is recrystallizes cellulose, a lubricating substance, such as magnesium stearate, a diluent or a binder, with at least one of the last of these compounds is a sweetener, preferably a polyol.
The composition may also optionally contain flavouring (flavouring agent) and/or an acidulant and/or additional sweetener selected from the group comprising sodium saccharinate, sodium cyclamate and aspartame.
A method of obtaining a known composition comprises wet granulation source of calcium with universal binder, drying and mixing of dry granules with a separate mixture of vitamin D and sweetening binder - sorbitol and a mixture of other ingredients.
The preferred composition contains calcium in the form of carbonate, vitamin D3, polyvinylpyrrolidone, xylitol, sorbitol, magnesium stearate, flavor, and the ratio of vitamin D3in international units (ME) and elemental calcium in mg is 1:1,25. The disadvantages of known composition is very great weight of the tablets (in example 2.5 g) and the volatility of the current component - vitamin D3in medicinal form, which significantly reduces the shelf life. In the decomposition of the concentration of the active ingredient is significantly reduced, and, accordingly, falls sharply those who piticescu activity of the medicinal product, in addition, the decay products can cause allergic side effects.
The objective of this invention is to provide a combined structure that regulates metabolic processes, in the form of a solid dosage form which is stable for a sufficiently long period (at least 2 years) and that has no side effects caused by degradation products of vitamin D.
To accomplish the tasks proposed structure for regulation of metabolic processes, which includes the active principle and the target additives, characterized in that the active principle is a combination of vitamin D3In6, C, K and calcium salt, and the composition further comprises citric acid and lactose in the following ratio of ingredients, μg per 1 IU of vitamin D3:
Vitamin b6- 6-18,
Vitamin C - inlet 150 up to 450,
Vitamin K is 0.5 to 1.5,
Salt of calcium (in terms of
elemental calcium) - 500-1500,
Citric acid - 20-400,
Milk sugar - 40-1000,
Targeted supplements - the rest.
As active principle according to the invention is used in combination with vitamin D3In6, C, K and calcium salts.
Salt calcium performs a function of a source of calcium, which is the main mineral component of bone tissue. As the calcium salt can p imeetsya various pharmacologically acceptable calcium salts, for example calcium carbonate, calcium lactate, calcium gluconate, glycerol calcium, calcium citrate and other salts, or their mixture, preferably calcium carbonate, containing a high percentage of elemental calcium (40.0 wt.%).
Included in the drug vitamins exclusively necessary for the regulation and normalization of bone tissue metabolism. Vitamin D (cholecalciferol) has a positive influence on calcium metabolism, reflected in a slowing of the rate of bone loss, and, therefore, is an important factor in maintaining the integrity of the skeleton and bone mass. Vitamin C (ascorbic acid) helps to improve the biochemical and mechanical properties of the bone tissue condition and leads to a reduction of its anomalies. Vitamin b6(pyridoxine hydrochloride) supports bone matrix in an appropriate state. Because as the basis for the deposition of mineral crystals in bone can only be properly organized matrix, introduction to the composition of this vitamin prevents and/or eliminates the pathological and morphological changes in the structure of collagen and bone structures. Vitamin K (fitomenadion) normalizes again resurfacing activity of bone tissue, with bone mineralization increases, and the risk of fractures caused by osteoporosis, decreases.
Introduction to the left for regulation of metabolic processes, includes the specified combination of active ingredients, citric acid and lactose at stated intervals allows to obtain a technical result that corresponds to the task at hand, namely the claimed composition is characterized by stable quality parameters during storage, including indicator "vitamin D3"what causes the shelf life of over 2 years, and the absence of adverse toxic effects, inherent degradation products of active ingredients. The preferred content of citric acid in the inventive composition is 50-200 mcg/1 IU of vitamin D3more preferably 80-120 ug/1 IU of vitamin D3.
The preferred content of the milk sugar in the inventive composition is 80-400 mg/1 IU of vitamin D3more preferably 180 to 300 mcg/1 IU of vitamin D3.
Used in the composition of the target additives include sorbitol, grease and corrigent taste and/or smell. As the lubricant, the new composition may contain stearic acid, salt of stearic acid, hydrogenated vegetable oil, castor, cottonseed oil, or other substances commonly used in the pharmaceutical industry as a lubricant, preferably a salt of stearic acid, in particular magnesium stearate.
With the goals of the firm improve the organoleptic properties of the composition may include corrigent taste and/or smell, for example, the sweetener and/or flavoring with the corresponding aroma is fruits, lemon, orange or similar. As a sweetener, you can use aspartame, sodium saccharinate, sodium cyclamate, preferably aspartame.
The preferred content of the target additives is, μg per 1 IU of vitamin D3:
Sorbitol - 1000-3300,
Grease - 15-150,
Corrigent taste and/or odor - 5-200.
The use of special additives in the above ratio gives you more than 2 times to reduce the weight of the unit dosage forms and to achieve a high strength of a tablet form that is required for subsequent packaging and transportation without the use of binder such as polyvinylpyrrolidone or microcrystalline cellulose, which promotirovat the processes of destruction.
The proposed ratio of ingredients is best found experimentally.
As the target additives can also be applied to other substance commonly used in the pharmaceutical industry, such as maltodextrin and nutriceuticals.
A study was conducted Toxicological actions of the proposed structure. The experiment was carried out on the nonlinear rats-males by drug intragastrically at doses of 10.0 (therapeutic) and 100.0 mg/kg once a day during the s 2 weeks. According to the results of the experiment in laboratory animals revealed no irritating effect on the mucous membrane of the gastro-intestinal tract, and significant effects on integral performance (weight gain, feed consumption, water and the General behavior of animals). Experimental data show no significant difference from peripheral blood, lipid and carbohydrate in the liver, as well as the functions of the urinary, cardiovascular and nervous systems during a two-week drug effects in the studied doses compared with the control group. In the studied doses of the new composition did not cause structural abnormalities in organs and tissues. Thus, it was experimentally confirmed no side effects from the new drug.
The proposed pharmaceutical composition is in the form of solid dosage forms, preferably in tablet form that provides maximum adaptability subsequent packaging and precision dosing of the active substance.
The way to get a new composition involves mixing active and auxiliary ingredients and then tableting the mixture. To improve the homogeneity of the dosing possible prior receipt of a mixture of ingredients present in very small amounts, such as vitamins to anti scar the us, with the entire amount or part of milk sugar. The use of the claimed quantitative and qualitative composition of ingredients allows to exclude from the process flowsheet stage wet granulation and drying, which significantly simplifies the manufacture of the dosage form, reduces losses. Mix ingredients in specified proportions also provides satisfactory strength tablets (more than 10 kgf).
The invention is illustrated by the following examples (see Table).
Example 1. Pre-prepare a mixture of 6 mg (or 240 000 ME) vitamin D3, 0.24 g of vitamin K (1.0 to hereinafter relative quantity in µg per 1 IU of vitamin D3), 2,88 g vitamin Be (12 μg) and 72 g of vitamin C (300 mg) with 120 g of milk sugar (500 g) and add to it 631,6 g of calcium carbonate brand DESTAB (1000 μg in terms of elemental calcium), 480 g of sorbitol, 24 g of citric acid (100 g), 10 g of aspartame, 14 g of orange flavor sweet and 12 g of magnesium stearate is added and stirred in a homogenizer-mixer to obtain a homogeneous mass. The mixture tabletirujut on a tablet press and get a tablet with an average weight of 1.15 g, which satisfy the requirements of the pharmaceutical agent. Strength tablets - 19,8 kg. The shelf life of the composition over 30 months.
Examples 2-4 perform similarly, with the difference that in example 2 as the e lubricants used stearic acid, in example 3, as corrigenda taste and/or odor - flavor apricot mixture and sodium saccharinate and to obtain a pre-mixture with vitamins load only half of the total number of milk sugar, and the rest is injected together with citric acid and targeted supplements, and in example 4 Corrigendum taste and/or smell is only aspartame, and as a salt of calcium using calcium lactate. The obtained tablets meet the requirements of the pharmaceutical agent and have a shelf life of more than 24 months.
|Ingredients||Content, μg per 1 IU of vitamin D3|
|Vitamin D3in ME||1||1||1||1|
|Salt of calcium, in terms of elemental calcium||1000||500||1500||500|
|Corrigent taste and/or odor||100||5||200||100|
1. Composition for regulation of metabolic processes, which includes the active principle and the target additives, characterized in that the composition further comprises citric acid and lactose, the active principle is a combination of vitamin D3B6, C, K and calcium salts, and the target additive composition contains sorbitol, grease and corrigent taste and/or smell, in the following ratio of ingredients, μg per 1 IU of vitamin D3:
|Vitamin C||Inlet 150 up to 450|
|Vitamin K||0.5 to 1.5|
|Salt calcium (Perez is n|
|Corrigent taste and/or odor||5-200|
2. The composition according to claim 1, characterized in that it contains as the lubricant magnesium stearate.
3. The composition according to claim 1, characterized in that it contains as corrigenda taste and/or smell of sweetener and/or flavoring.
4. The composition according to claim 3, characterized in that it contains as a sweetener aspartame.
5. The composition according to any one of claims 1 to 4, characterized in that it is made in tablet form.
6. A method of obtaining a composition for regulation of metabolic processes, described in claims 1 to 5, which comprises mixing vitamin D3In6, C, K, calcium salts, citric acid, lactose and specific additives and, if necessary, subsequent tableting the mixture.
7. The method of receiving according to claim 6, wherein the pre-receive a mixture of vitamins D3In6, And with the entire amount or part of milk sugar.
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention proposes phenylpyridazine compounds represented by the following formula (I): wherein R1 represents unsubstituted or substituted phenyl wherein substitutes are taken among the group comprising halogen atom, lower alkyl, lower alkoxy-group and phenylthio-group, or pyridyl; R2 represents lower alkoxy-group, lower alkylthio-group, lower alkylsulfinyl or lower alkylsolfonyl; R3 represents hydrogen atom or lower alkoxy-group; or R2 and R3 can be condensed in common forming lower alkylenedioxy-group; R4 represents cyano-group, carboxyl, unsubstituted or substituted lower alkyl wherein substitutes are taken among the group comprising hydroxyl, carboxyl and N-hydroxy-N-lower alkylaminocarbonyl; lower alkenyl; lower alkylthio-group; lower alkylsulfinyl; lower alkylsulfonyl; lower alkylsulfonyloxy; unsubstituted or substituted phenoxy-group wherein substitutes are taken among the group comprising halogen atom, lower alkoxy-, nitro-, cyano-group; unsubstituted phenylthio-group or phenylthio-group substituted with halogen atom; pyridyloxy-; morpholino-group; morpholinylcarbonyl; 1-piperazinylcarbonyl substituted with lower alkyl; unsubstituted or substituted amino-group wherein substitutes are taken among the group comprising lower alkyl, benzyl, phenyl that can be substituted with halogen atoms or lower alkoxy-groups, and n = 0, or their salts. Proposed compounds possess the excellent inhibitory activity against biosynthesis of interleukin-1β and can be used in preparing a medicinal agent inhibiting biosynthesis of interleukin-1β, in particular, in treatment and prophylaxis of such diseases as diseases of immune system, inflammatory diseases and ischemic diseases. Also, invention proposes intermediate compounds for preparing compounds of the formula (I). Except for, invention proposes a medicinal agent and pharmaceutical composition that inhibit biosynthesis of interleukin-1β and inhibitor of biosynthesis of interleukin-1β.
EFFECT: valuable medicinal properties of compounds and composition.
7 cl, 1 tbl, 66 ex
FIELD: medicine, orthopedics.
SUBSTANCE: the present innovation deals with treating osseous diseases caused by calcium exchange disorders. For this purpose certain calcium preparations should be reduced up to amorphous state to be perorally applied per 0.5-1.0 g, 2-4 times daily, at courses of not less than 10 d. The innovation provides efficient treatment due to high biodigestibility of amorphous calcium and its active accumulation in bony tissue.
EFFECT: higher efficiency of therapy.
1 cl, 2 ex
FIELD: medicine; medical engineering.
SUBSTANCE: biotransplant has genetically unmodified mesenchyma stem cell culture as active component obtained from fetal donor autologous material. The tissue is subjected to disaggregation and the produced cell suspension is resuspended and cultivated on growth medium containing transferrin, insulin, fibroblast growth factor and heparin to accumulate mature stroma in cell culture. Method involves intravenously dropping mesenchyma stem cell culture in the amount of 50 to 500 mln in 50-100 ml of physiologic saline.
EFFECT: accelerated recovery of bone tissue; positive biochemical factors dynamics; improved patient locomotor activity.
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel substituted 2-aryl-3-(heteroaryl)imidazo[1,2-a]-pyrimidines of the formula (I):
or to their pharmaceutically acceptable salts wherein: (a) R1 is taken among the group consisting of -NH2, C1-5-alkylamino-, di-C1-5-alkylamino-, phenylmethylamino-group; (b) Y is taken among the group consisting of hydrogen atom (H), halogen atom, piperidine, OR4, SR4, -SO2CH3, NHR4 and NR4R5 wherein R4 and R5 are taken independently among hydrogen atom (H), α-alkylphenyl-C1-5-alkyl, linear or branched alkyl substituted optionally with C3-5-carbocycle, phenyl or substituted phenyl wherein indicated phenyl can be substituted with one or some substituted taken among C1-5-alkoxy-group; (c) R2 represents from one to five members taken independently among the group including hydrogen atom (H), halogen atom, trifluoromethyl; (d) R3 represents hydrogen atom (H), or radicals R3 taken in common form aromatic ring; (e) X represents nitrogen atom (N) or -CH. Also, invention relates to methods for preparing indicated compounds and to a method for treatment based on these compounds. Invention provides preparing novel compounds that can be used in relief states by reducing the level of inflammatory cytokines, for example, the indicated state represents proliferative (rheumatic) arthritis.
EFFECT: valuable medicinal properties of compounds and compositions.
40 cl, 1 tbl, 4 ex
FIELD: medicine, phytotherapy, pharmaceutical industry, pharmacy.
SUBSTANCE: invention relates to using Belamcanda chinensis extract for preparing organ-selective medicinal preparation without uterotropic effect or with minimal such effect that is used as estrogen-like preparation. This preparation is used in selective treatment and/or prophylaxis of cardiovascular diseases, in particular, atherosclerosis and osteoporosis, climacteric disturbances, especially for prophylaxis or softening congestions of blood. Extract is used in manufacturing a medicinal preparation in ready formulation for selective treatment and/or prophylaxis of cardiovascular diseases, in particular atherosclerosis, and for selective treatment and/or prophylaxis of osteoporosis, climacteric disturbances, especially for prophylaxis and softening congestions of blood. Extract promotes to effective prophylaxis and/or treatment of cardiovascular diseases, in particular, atherosclerosis, climacteric disturbances, especially for prophylaxis and softening congestions of blood.
EFFECT: valuable medicinal properties of extract.
4 cl, 4 ex
FIELD: organic chemistry, vitamins, medicine, pharmacy.
SUBSTANCE: invention relates to a new compound of the formula (I): wherein X means hydrogen atom or hydroxy group; R1 and R2 that can be similar or different mean hydrogen atom, (C1-C4)-alkyl; R3 means hydrogen atom, methyl group, fluorine or chlorine atom. Also, invention relates to its esters able to hydrolysis in vivo in combination with pharmaceutically acceptable acids. Also, invention relates to a pharmaceutical composition eliciting the inhibitory activity with respect to proliferation and promoting differentiation of cells and comprising the effective dose of compound of the formula (I) in common with pharmaceutically acceptable carriers and/or excipients. Also, invention relates to applying compound of the formula (I) for preparing a medicine used in treatment and prophylaxis of disease characterizing by abnormal differentiation of cells and/or proliferation of cells.
EFFECT: valuable medicinal properties of compounds.
13 cl, 3 sch, 3 tbl, 6 ex
FIELD: medicine, chemical-pharmaceutical industry.
SUBSTANCE: invention relates to new applying EP4 receptors agonist for treatment and/or prophylaxis of diseases associated with loss of osseous mass. Agonists of EP4 receptors show high effectiveness in treatment of diseases associated with loss of osseous mass, among the, as osteoporosis of different genesis. Agonists of EP4 receptors involve prostaglandin skeleton base.
EFFECT: valuable medicinal properties of pharmaceutical composition.
16 cl, 3 tbl, 5 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to new derivatives of indol-3-yl of the formula (I):
wherein each A and B represents independently of one another oxygen atom (O), NH, CONH, NHCO or a direct bond; X means (C1-C2)-alkylene or a direct bond; R1 means hydrogen atom (H); R2 means hydrogen atom (H); R3 means NHR6, -NR6-C(=NR6)-NHR6, -C(=NR6)-NHR6, -NR6-C(=NR9)-NHR6, -C(=NR9)-NHR6 or Het1; each R4 and R5 represents independently of one another hydrogen atom (H); R7 means -(CH2)o-Ar, Het, OR6; R6 means hydrogen atom (H); R7 means (C1-C10)-alkyl, (C3-C10)-cycloalkyl; R8 means Hal, NO2 (nitro-group), CN (cyano-group), Z, -(CH2)o-Ar, COOR1, OR1, CF3, OCF3, NHR1; R9 means CN or NO2; Z means (C1-C6)-alkyl; Ar means aryl that can represent unsubstituted, monosubstituted, or polysubstituted R8; Hal means F, Cl, Br, J; Het means saturated, partially or completely saturated monocyclic or bicyclic heterocyclic radical comprising from 5 to 10 ring members wherein 1 or 2 nitrogen atom (N) and/or 1 or two sulfur atom (S) present, and heterocyclic radical can be monosubstituted with phenyl; Het1 means saturated, partially or completely unsaturated monocyclic or bicyclic heterocyclic radical comprising from 5 to 10 ring members and from 1 to 4 nitrogen atoms (N) that can be unsubstituted or monosubstituted NHX, or oxo-group; n = 0, 1 or 2; m = 0, 1, 2, 3, 4, 5 or 6; o means 0, 1 or 2; and their physiologically acceptable salts and solvates. Compounds of the formula (I) elicit intergin-inhibitory effect that allows their using as components of pharmaceutical composition. Also, invention describes intermediate compounds.
EFFECT: valuable medicinal properties of compounds.
11 cl, 4 sch, 1 tbl, 34 ex
SUBSTANCE: on should apply the suggested compound of formula 1 for treating and/or preventing osteoporosis and related osseous diseases.
EFFECT: higher efficiency of therapy and prophylaxis.
7 cl, 2 dwg, 21 ex, 6 tbl
FIELD: organic synthesis.
SUBSTANCE: invention provides compounds of general formula I:
in which R1 represents H, halogen, OCH3, or OH; R2 represents (a) -X-(CH2)n-CH2-N(R4)R5, where (i) X represents NH or S; n is integer from 1 to 4; R4 and R5, the same or different, represent C1-C4-alkyl, H, -CH2C≡CH, or -CH2CH2OH; or R4 and R5, together, form nitrogen-containing five- or six-membered cycle or heteroaromatic cycle; or where (ii) X represents O; n is integer from 1 to 4; one of R4 and R5 is CH2C≡CH, or -CH2CH2OH and the other H or C1-C4-alkyl; or R4 and R5, together, form imidazole cycle or nitrogen-containing six-membered cycle or heteroaromatic cycle; or R2 represents (b) -Y-(CH2)nCH2-O-R5, where (i) Y represents O; n is integer from 1 to 4; and R6 represents -CH2CH2OH or -CH2CH2Cl; or where (ii) Y represents NH or S; n is integer from 1 to 4; and R6 represents H, -CH2CH2OH, or -CH2CH2Cl; or R2 represents (c) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, or 2,2-diethyl-2-hydroxy-ethoxy; R3 represents H. halogen, OH, or -OCH3. Claimed compounds are novel selective estrogen receptor modulators. Invention also discloses pharmaceutical composition and a method for production of tissue-specific estrogenic and/or antiestrogenic effect in patient, for whom indicated effect is required.
EFFECT: increased choice of estrogen receptor modulators.
19 cl, 7 tbl, 11 ex
FIELD: sterilization agents and facilities in medicine.
SUBSTANCE: sterilization method comprises first-step treatment of an object with 0.05-0.3% (based on active component) solution of biocide agents based on clatrate of quaternary ammonium compound with urea and second-step treatment with solution containing 2.5-3.5% hydrogen peroxide. Kit contains (i) concentrate of biocide agent based on clatrate of quaternary ammonium compound with urea and (ii) peroxide compound.
EFFECT: allowed quick achievement of sterility of objects and suppressed final stage of washing objects in sterile water or other liquid to remove the rest of biocides.
13 cl, 1 tbl
SUBSTANCE: pills comprise natural interferon or recombinant -α, -β or -γ manifesting activity in low or high doses. Pills comprising interferon inductor in the amount of 100 mcg to 25 mg or interferon inductor in the amount of l/5-1/20 of therapeutical unit dose with one of recombinant human gene engineering interferons in the amount of 500-1000 IU taken in 2:1 - 3:1 proportion.
EFFECT: enhanced effectiveness in stimulating local oromucosal and systemic immune response; increased antiviral organism resistance.
6 cl, 3 tbl
FIELD: medicine, in particular dry azithromicine mixtures to produce azithromicine pellets by direct pressing.
SUBSTANCE: claimed formulation contains non-dehydrated azithromicine selected from group containing B, D, E, F, G, H, J, M, N, O, P, Q, R forms or mixtures thereof, and at least one pharmaceutically acceptable carrier. Pellet containing non-dehydrated azithromicine mixture and at least one pharmaceutically acceptable carrier, as well as azithromicine pellet obtained by providing of dry mixture containing non-granulated azithromicine A and at least one pharmaceutically acceptable carrier, followed by direct pressing said mixture also are disclosed.
EFFECT: direct pressable azithromicine-containing formulations; azithromicine pellets having acceptable hardness and frangibility.
14 cl, 6 ex, 1 dwg, 6 tbl
SUBSTANCE: invention provides (i) compacted vaccine composition containing lyophilized antigenic component and an auxiliary component enhancing dissolution and (ii) stable compacted vaccine composition containing a second lyophilized component including neutralizing antibodies against above lyophilized antigenic component. Invention further provides syringe containing vaccine composition, kit, and method of immunizing veterinary animal.
EFFECT: increased stability of composition.
50 cl, 11 ex
SUBSTANCE: the suggested solid dosed form of disinfectant contains a quaternary ammonium compound as an active substance and/or its compounds as clathrates, preferably, clathrate carbamide didecyldimethylammonium bromide and/or chloride, and additional substance - an acid component chosen out of boric acid, water-soluble acidic salts of phosphoric acids, acidic salts of sulfuric acid. The innovation provides wide range of antimicrobial activity being of high stability, solubility, low toxicity, comfort in usage and transportation.
EFFECT: higher efficiency.
17 cl, 8 ex, 2 tbl
FIELD: medicine, pharmacy, pharmaceutical industry.
SUBSTANCE: invention proposes a pharmaceutical composition used as a nootropic agent. The nootropic agent represents the condensed extract from the plant Atragene sibirica (family Ranunculaceae) prepared by condensing the liquid alcoholic extract from plant the Atragene sibirica under vacuum at temperature 50°C up to the moisture content 25%, and filling agents comprising lactose, microcrystalline cellulose, polyplazdon XL-10, potato starch, aerosil, magnesium stearate chosen in the definite ratio of components. Agent possesses the effective nootropic effect.
EFFECT: valuable medicinal property of pharmaceutical composition.
2 cl, 7 tbl, 4 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to a soluble, carbonated, anti-inflammatory, analgesic and antipyretic agent as a tablet. Agent comprises acetylsalicylic acid, caffeine, ascorbic acid, paracetamol, basic component, acidic component and accessory substances. Invention provides the possibility of rapid release of the preparation in blood, decreasing time for undesirable contact of the preparation with stomach mucosa and its high activity.
EFFECT: valuable medicinal and pharmaceutical properties of agent.
6 cl, 6 tbl, 11 ex
FIELD: medicine, pharmacology, pharmacy.
SUBSTANCE: invention relates to the development of a new medicinal agent representing the complex enzyme preparation with the digestive effect. Agent comprises enzyme pectate lyase providing effective cleavage of vegetable food intercellular substances, in particular, pectin and protopectin that results to formation of the homogenous and easily digestible mass, and promotes to assimilation vegetable food that is not assimilated by human organism that results to the more complete digestion of food, its cleavage and assimilation of nutrient substances. The optimal content of enzyme pectate lyase and pancreatin in a tablet covered by the enterosoluble envelope promotes to the more rapid and complete digestion of food in intestine and shows significant advantages as compared with the known digestive preparations.
EFFECT: improved and valuable properties of agent.
5 cl, 11 tbl
FIELD: medicine, endocrinology.
SUBSTANCE: invention elates to a method for treatment of diabetes mellitus type 2, method for declining the glucose content in patient blood and method for reducing resistance to insulin, diminishing the hemoglobin A1c content, enhancing the insulin level after eating, and reducing the amplitude change content ("mobility") of glucose in diabetic patients. Method involves administration of metformin to patient in the low dose (160-750 mg) in combination with the second anti-diabetic agent chosen from the group including glucose oxidase inhibitor, glucagons-like peptide-1 (GLP-1), insulin, α/β-double agonist of PRAP other than thiazolidinedione, meglitimide and inhibitor aP2 wherein the second anti-diabetic agent is administrated as a daily dose in interval between the initial daily dose comprising 20-60% of the initial daily dose of this anti-diabetic agent used in usual medicinal practice in therapy of the first order in treatment of diabetes mellitus up to the daily supporting dose comprising 40-60% of the daily supporting dose of this anti-diabetic agent used in usual medicinal practice as therapy of the first order in treatment of diabetes mellitus. Invention provides the effectiveness in treatment of diabetes mellitus that is equivalent practically to effectiveness of treatment by using combination of metformin and other indicated anti-diabetic agent used in doses prescribing in usual medicinal practice but with significantly less adverse effects.
EFFECT: improved method for treatment of diabetes mellitus.
7 cl, 10 dwg, 4 tbl, 3 ex
SUBSTANCE: claimed method includes blending of active base and auxiliary ingredients to form tablet corn, representing composition of sugar powder, monocrystalline cellulose, vinylpyrrolidone and calcium stearate; humidifying of obtained mixture; drying of obtained granules; dry granulation through granulator with standardized holes; pelletization of standardized granules to produce tablet corn; and coating. Mixture is humidified with 5-7 % starch mucilage in starch mucilage/humidifying mixture mass ratio of 1:25-30, wherein mixture is blending with starch mucilage for homogeneous distribution wet in whole mass.
EFFECT: tablets with increased hardness and enhanced pharmacological activity.
2 cl, 2 ex
FIELD: veterinary science.
SUBSTANCE: the present innovation deals with preventing and treating puerperal endometritis in cows. One should introduce the foam into uterine cavity that appears after interacting with warm water containing 10 U oxytocin and a suppository that includes medicinal substances reduced up to amorphous state. Moreover, components in a suppository are in the following ratio, g (weight%): potassium iodide 1.5 (5.4), ephedrine hydrochloride 0.5 (1.8), furacillin 0.5 (1.8), metronidazole (trichopol) 1.5 (5.4), proserine (prostigmin) 0.06 (0.2), analgin 0.5 (1.8), sodium bicarbonate 9.0 (32.7), potato starch 4.0 (14.6), common salt 1.5 (5.4), citric acid 6.9 (25), calcium stearate 0.3 (1.1), 20%-alcoholic solution of MGD-2 emulsifier or MGD-2-similar one 1.3 (4.8). The innovation provides higher efficiency of local impact of medicinal substances upon pathogenic uterine microflora.
EFFECT: higher efficiency.
1 cl, 1 tbl