Pharmaceutical composition possessing hepatoprotecting, hypolipidemic, immunostimulating and normalising kidney function action, and method of its obtaining

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of medicine, namely to pharmaceutical industry and deals with solid pharmaceutical composition, possessing high physical strength. Claimed invention also presents method of manufacturing solid pharmaceutical composition. Claimed pharmaceutical composition contains 7 varicoloured types of granules in form of capsule. Granules contain, wt %: nikotinamide 1-35; pyridoxine 0.1-8; calcium pantitenate 0.1-15, thiamin 0.1-30; tryptophan 1-30; tocoferol 0.5-5; ascorbic acid 0.1-50; 5-hydroxyanthranyl acid 0.01-10; Riboflavin 0.1-10; folic acid 0.1-6; cyanocobalomin 0.001-6; isoleucin 0.5-10; leucin 0.5-15; lysine 0.5-20; phenylalanine 0.1-5; threonine 0.1-5.0; valin 0.1-8.0; methionine 0.1-15; lactose 1-4.0; ergocalcioferol 1-95.0 and auxiliary substances for obtaining granules.

EFFECT: claimed composition possesses excellent properties of medication release and digectionin application composition possesses hepatoprotective hypolipidemic immunostimulating and normalising kidney activity action.

2 cl. 2 ex. 5 tbl

 

The present invention relates to solid pharmaceutical compositions having high physical strength, which has excellent release property of the medicinal product and digestibility in the application and has hepatoprotective, hypolipidemic, immune stimulating and normalizing the function of the kidneys action. The present invention also provides a method of manufacturing the solid pharmaceutical composition.

The urgency of the problem is associated with an increase in the frequency and severity of diseases of the liver is the primary organ of detoxification of exogenous poisons (the reasons for the increasing incidence of liver are the environmental problem in most parts of the world), and also with concomitant diseases of the whole body and the need to create drugs with an extended spectrum of action.

Additional and directly associated with environmental factors is the reduction of immunity in the population, leading to significant growth of infectious lesions of the liver, primarily viral hepatitis.

Regardless of the input gate of the virus eventually reaches the liver, where it has a direct toxic effect on liver cells, which is combined with immune-mediated damage to their membranes.

Renowned pharmaceutical composition, the soda is containing-amino-methylthiophenol acid (methionine) or-amino-hydroxybutyric acid (threonine) (Patent RU №2283114).

Closest to the claimed composition to the technical essence and the achieved result is a drug Moriamin Forte (http://www.moriamin-forte.ru/instruction.php).

The scope of the product is restricted for use as a medicine.

The aim of the invention is to provide a composition, the design of which takes into account all the shortcomings of the previously described products and which possesses hepatoprotective, hypolipidemic, immune stimulating and normalizing activity of kidney effects in children and adults.

The composition can be used (by regulation of the course of treatment and dosage) as a drug or biologically active food supplements.

The technical object of the present invention is to provide a combined composition with maximum retention, extended range of pharmacological actions, with improved bioavailability and therapeutic activity that can reduce the treatment time.

The technical problem is solved due to the fact that the pharmaceutical composition in the form of capsules contains 7 colorful types of granules:

1. White granule contains nicotinamide, pyridoxine, calcium Pantothenate, starch, lactose, cellulose, calcium carboxymethyl cellulose, titanium oxide in the following ratio ingredien is s, in wt.%:

Nicotinamide1-35
Pyridoxine0,1-8
Calcium Pantothenate0.1 to 15
Lactose1-20
The titanium oxide0,1-20
Carboxymethylcellulose calcium1-11
Cellulose crystalline100

2. White granule contains thiamine Mononitrate, starch, lactose, cellulose, karboksimetilcelljulozy calcium, methylcellulose, titanium oxide at the following ratio, wt.%:

Thiamine0,1-30
Starch1-10
Cellulose10-12
Carboxymethylcellulose calcium1-15
The methylcellulose0,1-5
The titanium oxide0,1-5
Lactose100

3. Red pellet contains L-tryptophan, tocopherol acetate, starch, lactose, crystalline cellulose, karboksimetilcelljulozy calcium, hydroxypropylcellulose, macrogol 6000, synthetic aluminum silicate in the following ratio of ingredients, wt.%:

Tryptophan1-30
Tocopherol0,5-5
Starch1-25
Crystalline cellulose0,5-6
Carboxymethylcellulose calcium0,5-6
Hydroxypropylcellulose0,1-6
Macrogol 60000.1 to 2
Aluminum silicate0.1 to 15
Dye0,001-1
Lactose100

4. Chocolate pellet contains ascorbic acid, starch, lactose, crystalline cellulose, karboksimetilcelljulozy calcium, methylcellulose, macrogol 600 in the following ratio of ingredients, in wt.%:

Ascorbic acidof 0.1-50
Starch0,5-10
Cellulose crystalline5-7
Carboxymethylcellulose calcium1-10
The methylcellulose0,1-6
Macrogol 60000,1-10
Dye0,001-1
Lactose100

5. Orange granule contains 5-hydroxyanthranilic acid, Riboflavin, folic acid, cyanocobalamin, starch, lactose, crystalline cellulose, karboksimetilcelljulozy calcium, hydroxypropylcellulose, macrogol 6000 in the following ratio, wt.%:

5-hydroxyanthranilic acid0,01-10
Riboflavin0,1-10
Folic acid0,1-6
Cyanocobalamin 0,001-6
Starch0,5-30
Cellulose crystalline1-10
Carboxymethylcellulose calcium0,1-6
Hydroxypropylcellulose0,1-7
Macrogol 60000,1-5
Dye0,001-1
Lactose100

6. Yellow granule contains isoleucine, leucine, lysine, phenylalanine, threonine, valine, methionine, starch, lactose, cellulose, methylcellulose calcium, hydroxypropylcellulose, the dye in the following ratio, wt.%:

Isoleucine0,5-10
Leucine0.5 to 15
Lysine0,5-20
Phenylalanine0,1-5
Threonine0,1-5,0
Valineof 0.1 to 8.0
Methionine 0.1 to 15
Lactose1-4,0
Cellulose1-11
The methylcellulose calcium1-3,0
Hydroxypropylcellulose0,1-1,0
Dyeof 0.001 to 1.0
Starch100

7. Light yellow granule contains ergocalciferol in the following ratio, wt.%:

Ergocalciferol1-95,0
Starch100

Moreover, the essential characteristic of which is the ratio of the granules in the capsule 1 white 17%, 2 white 7%, yellow 36%, orange 12%red 8%, chocolate 13%, light yellow 7%.

All types of granules can contain additionally one or more vitamins, one or more amino acids, one or more macro - or micronutrients or other pharmaceutical drug from the group of flavonoids, immunomodulators, hepatoprotectors, plant extracts. Pets using the optional preservative (e.g., potassium sorbate).

Protein is the main substance of manifestation of life, making the cells, tissues, organs, and control body functions.

Allocate eight amino acids which are not synthesized in the body, and they are called essential.

Amino acids are required for the connection of proteins in the blood and tissues, to move existing amino acids, the reconstruction of damaged tissues and the formation of new proteins.

Ascorbic acid. Vitamin C is required for normal development of the placenta and increase the body's resistance to infections. Vitamin C provides the synthesis of collagen, helps to maintain healthy skin. Affects the formation of hemoglobin and erythrocyte maturation.

Ergocalciferol regulates the exchange of CA2+and phosphorus, the process of building the structure of the bones; it increases the absorption of CA2+in the intestine, protein synthesis in the small intestine, liver and bones; the excretion of phosphate by the kidneys. Vitamin D3 is essential for the formation of bone tissue of the fetus.

Nicotinamide stabilizes the processes of tissue respiration, lipid and carbohydrate metabolism, metabolism Xen is biotikos. Nicotinamide normalizes microcirculation. Involved in the processes of tissue respiration, lipid and carbohydrate metabolism.

Pyridoxine hydrochloride as a coenzyme involved in the metabolism of amino acids and proteins in the synthesis of neurotransmitters.

Retinol palmitate. Retinol is essential for normal function of the retina: it binds with openam (red pigment of the retina), forming the optic purple rhodopsin required for visual adaptation to the dark. Vitamin a is necessary for bone growth, normal reproductive function, embryonic development, regulation of division and differentiation of the epithelium (enhances the reproduction of epithelial skin cells, rejuvenates cell population, hinders the process of keratinization). Vitamin a participates as a cofactor in various biochemical processes.

Riboflavin catalyst processes of cellular respiration and lipid peroxidation of endogenous substances and xenobiotics, glukuronirovania.

Thiamine Mononitrate plays an important role in the metabolism of carbohydrates and fats. Substance is necessary for the normal processes of growth and development and helps to maintain proper functioning of the heart, nervous and digestive systems. Thiamine, being water-soluble compounds, not stores the I in the body and has no toxic properties.

Vitamin E has antioxidant properties, protects unsaturated fatty acids in membranes from lipoperoxidation; participates in the formation of intercellular substance, collagen and elastic fibers of connective tissue, smooth muscles of blood vessels, the digestive tract. A positive effect on peripheral circulation.

Calcium Pantothenate, a component of coenzyme a, is involved in the acetylation and oxidation of carbohydrates and fats, synthesis of fatty acids and steroids from carbohydrates, in the implementation of links glycolysis, Krebs cycle and fat oxidation. Calcium Pantothenate is involved in the regeneration of the epithelium and endothelium, promotes healing, reduces adverse and toxic effects of antibiotics and antibacterial drugs.

Cyanocobalamin together with folic acid is involved in the synthesis of nucleotides, in the formation of red blood cells and nerve cells membranes, necessary for growth of the organism.

Folic acid is a vital vitamin that is essential for growth and development of the blood and immune system. The biological effect of folic acid: Antianemic, preventing intrauterine fetal anomalies, increase mental and physical performance, neuroprotective, antidepressant, restores the structure of the nervous tissue; antiatherosclerotic the definition, stimulating the production of hydrochloric acid, firming intestinal wall, antidiarrheal agents, protecting against intestinal parasites and pathogenic flora, estrogen, lactogenic; dermatropnye, onkoprotektornye and other Folic acid is necessary for normal blood formation, plays an important role in cell division, participates in the formation of the placenta, provides growth and development of the fetus.

A method of producing granules is in the weighing of ingredients, mixing, granulating, drying the pellets, weighing and blending of the granules together in a specific proportion with the subsequent kapsulirovaniem.

The invention is illustrated below by examples of industrial application in the production environment.

Example 1

1. White granules. Give nicotinamide in the amount of 1%, is mixed with pyridoxine 0.1% and the calcium Pantothenate is 0.1%, then add lactose and 1.0%, carboxymethylcellulose calcium 1%, the titanium oxide is 0.1%, then the parts added under stirring lactose to 100%, the mixture is uniformly moistened with 1% water. Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

2. White granules. Mix the thiamine of 0.10%starch 1%, cellulose 1%, carboxymethylcellulose calcium 1%, titanium oxide 0.1% methylcellulose of 0.1%, then the parts we use the t with stirring lactose to 100%, uniformly moisten 1% water. The mixture granularit through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

3. Red granules. Mix tryptophan 1% tocopherol of 0.5%starch 1%, hydroxypropylcellulose of 0.1%, crystalline cellulose of 0.5%carboxymethylcellulose calcium 0,5%, macrogol 6000 0.1%aluminium silicate 0.1%dye 0,001%, add parts in several stages with constant stirring lactose to 100%, moisture 1% water. Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

4. Chocolate granules. Mix ascorbic acid in an amount of 0.1% starch, 0.5%, and crystalline cellulose 1%carboxymethylcellulose calcium 1%methylcellulose 0.1%macrogol 6000 0.1% of the dye of 0.001%. Add parts in several stages with constant stirring lactose to 100%, moisture 1% water. Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

5. Orange granules. Mix 5-hydroxyanthranilic acid of 0.01% with Riboflavin 0.1 percent, folic acid 0.1%cyanocobalamine of 0.001%, the starch of 0.5%, crystalline cellulose 1%carboxymethylcellulose calcium 0,1%, GI is oksipropiltselljuloza of 0.1%, the macrogol 6000 0.1% of the dye of 0.001%. Add parts in several stages with constant stirring lactose to 100%, moisture 1% water. Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

6. Yellow granules. Mix isoleucine in the amount of 0.5% by leucine of 0.5%, lysine 0,5%, phenylalanine 0.1%threonine 0.1%valine 0.1%methionine 0.1%lactose 1%cellulose 1%methylcellulose calcium 1%, hydroxypropylcellulose 0.1%dye 0,001%add parts in several stages with constant stirring starch to 100%, hydrate a mixture of 1% water. Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

7. Light yellow granules. Ergocalciferol 1% mixed with starch in the amount of 99%. If necessary, moisten the mixture with water in a small amount. Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

The granules are mixed with each other in the number 1 white 17%, 2 white 7%, yellow 36%, orange 12%red 8%, chocolate 13%, light yellow 7% and fill the capsules.

As the capsules are hard gelatin capsules consisting of the cap and body.

Example 2

1. White granules. Give nicotinamide in the amount of 35%, is mixed with pyridoxine 8% and Pantothenate calcium 15%, then add lactose 20%, carboxymethylcellulose calcium 11%, titanium oxide 2%, then lactose and 100%, the mixture is uniformly moistened with 1% water. Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

2. White granules. Mix thiamin 30%starch 10%, cellulose 15%, carboxymethylcellulose calcium 15%, titanium oxide 5% methylcellulose 5%, then add with stirring lactose to 100%, the mixture is uniformly moistened with 1% water. The mixture granularit through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

3. Red granules. Mix tryptophan 30% tocopherol 5%, starch 25%, hydroxypropylcellulose 6%, crystalline cellulose, 6%, carboxymethylcellulose calcium 6%, macrogol 6000 2%, silicate of aluminium, 15%, dye and 1.0%, add lactose to 100%, moisture 1% water. Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

4. Chocolate granules. Mix the ascorbic acid in the amount of 50% starch 10%, crystalline cellulose 9%, carboxymethyl cellulose to LCIA 10%, methylcellulose 6%, macrogol 6000 10% and the dye of 1.0%. Add lactose to 100%, moisture 1% water. Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

5. Orange granules. Mix 5-hydroxyanthranilic acid 10% Riboflavin 10%, folic acid 6%, cyanocobalamine 6%starch 30%, crystalline cellulose 10%, carboxymethylcellulose calcium 6%, hydroxypropylcellulose 7%, macrogol 6000 5% dye 1%. Add lactose to 100%, moisture 1% water.

Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

6. Yellow granules. Mix isoleucine in an amount of 10% leucine 15%, lysine 20%, phenylalanine 5%, threonine 5%, valine 8%, methionine 15%, lactose 4%, cellulose 11%, methylcellulose calcium 3%, hydroxypropylcellulose 1%dye 1%, added with constant stirring starch to 100%, hydrate a mixture of 1% water. Then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

7. Light yellow granules. Ergocalciferol 5% mixed with starch in the amount of 95%. If necessary, moisten the mixture with water in a small amount. Then gra is aliroot the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%. The finished granules are poured into the container.

The granules are mixed with each other in the number 1 white 17%, 2 white 7%, yellow 36%, orange 12%red 8%, chocolate 13%, light yellow 7% and fill the capsules.

As the capsules are hard gelatin capsules consisting of the cap and body.

In practice, you can make changes and modify described the preferred embodiments of the present invention, without departing from the scope and aims of the present invention, within the stated claims.

Clinical study for the composition prepared according to Example 2 confirms that the proposed treatment composition can significantly improve the relative symptoms and laboratory parameters.

In the treatment of liver diseases appointment improves liver function, increases the formation of serum reduces the number of dead cells and, therefore, obviously eliminates symptoms such as fatigue, apathy, pain in the liver, Gilchrest, swelling of the liver, as well as parameters such as ALT, AST, etc.

With regard to kidney disease, especially in patients who need to restrict the input protein, constantly making small quantities of essential amino acids and vitamins, leading to the improvement of the neg is negative nitrogen balance to increase the bioavailability of non-essential amino acids, reduce the production of nitrogen and performing the main functions of the kidney. The proposed treatment composition can be reduced to the usual symptoms of kidney disease, such as fatigue, abdominal pain, edema, etc., the increase in the concentration of plasma albumin and basic amino acids and reducing the concentration of non-essential amino acids.

Treatment of cirrhosis

Objects and method:

1. Selection of patients

Patients diagnosed with cirrhosis of the liver by albumin in the range of 28-35 g/L. Patients conditionally divided into two groups.

2. Method of treatment

Group treatment (n=10): 2 capsules per time, three times a day for 6 weeks. Control group (n=7): a tool prototype

3. Research options

Was recorded before and after treatment the following parameters.

Symptoms: fatigue, apathy, nausea, vomiting, pain, liver, small temperature etc.

In all patients before treatment was observed: ascites, small pulmonary edema, etc.

Studied laboratory parameters: albumin, globin, prothrombin time, bilirubin, titration in the gas phase, proper blood flow, platelet etc.

4. Statistical data

Tests X2N used to compare treatment and control groups, respectively.

Result

The results of clinical studies of patients with CIRR the zoom liver after treatment proposed composition shown in tables 1, 2 and 3, which represent:

1. The proposed composition showed significant efficacy in elimination of symptoms of cirrhosis of the liver, such as fatigue and apathy;

2. The composition showed significant efficacy in ascites and removing the bottom of pulmonary edema in patients with cirrhosis of the liver.

3. The composition is able to increase protein and reduce prothrombin time, significantly reduce the level of globin, a large number of red cells and platelets, but does not improve laboratory parameters such as titration in gas form, bilirubin, etc.

4. The composition has no adverse reactions during treatment.

5. The positive effect of the treatment proposed composition was achieved in a shorter time than from the treatment composition of the prototype.

The compositions can provide nutrition to the cells of the tissue, accelerate protein synthesis in tissue and improve tissue metabolism. These results show that treatment of patients with cirrhosis of the proposed composition can significantly improve cellular function of the liver, as well as to provide nourishment to the cells of the liver, especially in the treatment of hypoalbuminemia, the proposed composition is a drug with high efficiency, safety and ease of use

Treatment of chronic renal fake is technote

1. Patients: 22 cases with chronic liver diseases, among which 12 men and 10 women aged 9-56 years (average 2.6±8.2). Common diseases include 7 cases of chronic nephritis, 3 cases of pyelitis, 2 cases of diabetic nephritis, 2 cases of gout liver. In addition we have recruited a control group consisting of 10 people.

Drugs and dosage: suggested composition 2 capsules three times a day for 31-54 day.

All patients with chronic liver disease, followed by infection, was treated after infection, and patients with hypertension were treated to restore the pressure.

In each group were recorded basic laboratory parameters before treatment and after treatment, were tested: blood and urine, the content of substances: urea nitrogen (BUN), Kretinin (Scr), the rate of purification of the internal creatinine (Ccr), the total number of proteins in the plasma (TP), plasma albumin (Alb), calcium, phosphorus, glycerides (TG), cholesterol (Ch) and glucose (Glu).

Amino acids were determined exact build chromatogram and were analyzed using fluorometry, the apparatus Millipore-Wates Cop. Sigma Cop., which fixes the standard samples of 16 amino acids.

1. Liver function and biochemical test results are presented in table 1. Shows the reduction of nitrogen and phosphorus in the blood, the increase of calcium in to the Ovi (P< 0.005). Other parameters do not differ from the above.

2. The blood of SIL-2R, urine SIL-2R in the experimental group were higher than those of the control group (P<0.01).

3. Differences in performance in the two groups are presented in table 2.

4. Determined the number of amino acids in plasma. Before treatment were found 4 amino acids, at lower concentrations than after treatment (Cm. table 3).

This study shows that application of the proposed composition, combined with a low-protein diet reduces the amount of nitrogen in the urea chronic liver disease and improves symptoms of high phosphorus concentrations and low concentrations of calcium in the blood, as well as the impact on the amount of sugar in the blood and creatine in the blood. In addition to the above change does not increase at the end of the treatment period, which must match each patient with liver disease, and only diet cannot change the dialysis of blood. In the above group received treatment - dialysis blood.

After applying the proposed composition of the patients in this group have a significant increase in the number of amino acids in plasma and reducing non-essential amino acids. Thus, it is obvious that the composition modulates the levels of various amino acids in their General is Alceste, meanwhile, the concentration of phosphorus in the blood obviously decreases. When the continuation time of treatment, there is a need for further research to determine the effectiveness of treatment to improve the condition of the liver.

Immunostimulatory effects of the proposed tool was determined by the following indicators IgA (g/l)IgM (g/l)IgG (g/l), C3 (g/l), the test transmission cells lymph (LTT, %), 2 groups, control and treatment. The treatment group received the proposed composition 2 capsules 2 times a day for 10 days.

The data obtained indicate that the inventive tool increases the body's defenses to the effects of carcinogens and other environmental factors (table 4).

The study of the hypolipidemic actions proposed composition on lipid levels and PL in animals with experimental DLP atherogenic nature conducted in rats and rabbits, using the models of pathological conditions.

To determine the lipid used standardized biochemical methods in accordance with the recommendations of the all-Russian scientific society of cardiology (GFCF, 2004). The level of cholesterol in blood serum of rats and rabbits was determined by colorimetric enzymatic method (CHOD-PAP) with the use of a set of reagents company "Vital Diagnostics". Determination of HDL cholesterol in the serum of rats and rabbits were conducted decree of the mentioned above method using reagents from the same company after the pre-deposition of atherogenic LP. For the determination of triglycerides in serum of rats and rabbits used a set of reagents company "Vital Diagnostics" [Wahlfeld A.W. In: Methods of enzymatic analysis. Acad. Press, NY; 1974: 1831]. The content of cholesterol in the liver was determined using the conventional color reaction Lieberman-Burchard, after extraction of the sample of the liver with a mixture of chloroform with carbinol [Bragdon GH In: Lipids and steroid hormons in clinical medicine. Ph. 1960: 6-10]. The content of triglycerides in the liver was determined by the method of Neri and Frings of Cologne (1973), modified by the authors, consisting of the replacement of the sorbent is a zeolite mixture of alumina [Okuniewicz IV, Sapronov NS, Indenbom M. Chem.-Pharm. W. 1999; 11: 14-16]. The content of total cholesterol in the aorta of rabbits was carried out colorimetrically, using the reaction of the Lieberman-Burchard, after extraction of a sample. To prepare a chloroform extract of the aorta was ground with quartz sand [Ryzhenkov, V.E., Khromov-Borisov N.V., Mosin IV, Indenbom M. Pharmacol. toxicol. 1979; 6: 632-635]. The content of cholesterol in the adrenal glands was determined by the extraction method, as described above, after homogenization of the tissue sample, its extraction with chloroform, and applying the subsequent reaction of the Lieberman-Burchard [Okuniewicz IV, Ryzhenkov VE Pat. Fiziol. the experts. Ter. 2002; 2: 14-18].

Results studies

Hypolipidemic activity in models of DLP.

Experience 1. Model tritanomaly of dyslipoproteinemia (DLP) in rats.

Hypolipidemic activity of study and 60 rats male on screening model DLP, caused by the detergent Triton WR-1339 (225 mg/kg once, intraperitoneally). This model is characterized by the development of persistent hyperlipidemia - a significant increase in the level of cholesterol and triglycerides in the blood of rats (weighing 250-300 g) compared with the contents of these indicators in intact animals [Shurr P.E., Shultz Y.R. Lipids 1972; 7(1): 68-74].

Claimed the drug was administered to rats at a dose of 100 mg/kg orally twice (before the introduction of and simultaneously with the injection of Triton WR-1339). After 10 hours the degree of development of hyperlipidemia was defined by the level of cholesterol and triglycerides in the blood serum that when therapy claimed the drug showed significant reduction of elevated under conditions tritanomaly AGP levels of cholesterol and triglycerides: 25% and 50%, respectively.

Thus, the model tritanomaly of dyslipoproteinemia was found pronounced hypolipidemic action.

Experience 2. Hypolipidemic action proposed composition on the model of chronic nutritional DLP in rats.

The experiments were carried out on 72 rats male (weighing 230-250 g) in terms of nutritional DLP, characterized by a high level of lipids and PL in the serum and liver, and at the same time a reduced content of cholesterol atherogenic HDL in the blood. These violations were caused by a diet containing 7.5% of cholesterol, 30% of a mixture of animal fats and heated sunflower oil (2:1) and 500,000 MI vitamin D2. The duration of the existence of the deposits of experience accounted for 21 days.

The proposed composition at a dose of 100 mg/kg orally was administered to rats for 21 days on the background of the special hypercholesterinemia diet (GHS diet). In the serum was determined the levels of total cholesterol, triglycerides and HDL cholesterol. On the basis of these indicators according to the standard formula of Friedwald hoped cholesterol atherogenic LDL. According to the formula Klimov (LDL - HDL cholesterol)/HDL cholesterol was determined by the amount of cholesterol atherogenic index (IA). In the liver was determined by the content of cholesterol and triglycerides, feeding rats GHS diet leads to the development of DSP: increase the level of cholesterol in 2.6 times, TG - 2.9 times, reducing the concentration of LDL atherogenic HDL 2.3 times. In addition, significantly increase the calculated value of the content of cholesterol atherogenic LDL and cholesterol IA, reflecting the development of the ATA. Under these conditions, the use of the proposed drug is a significant hypolipidemic effect: reduced levels of cholesterol and TT serum and 31.7%, respectively. These facts point to a positive Outlook in preventing the development of Antibodies in experimental animals in therapy.

Hypolipidemia

The drug tested in 25 patients with hypolipidemia (aged 56-70 years) in stationary conditions).

The results of the study show that the drug has a pronounced hypolipidemic effect, manifested already on the 10th day of treatment with progressive is a growing effect in subsequent periods. So, total cholesterol decreased by 15.6% (day 10), 21.0 per cent (25 day) and 24.4% (3 months), triglycerides, respectively, 32.9, 40,6, to 44.7%, LDL - 15.0, 26,7, 24.3 per cent. The content of cholesterol in low density lipoprotein (LDL-C - vysokopatogennyj lipoproteins) was decreased more significantly - 25.6, 36,9, 41,4% (respectively 10, 25 and 90 days of treatment), and the concentration of cholesterol in high density lipoprotein ("HDL cholesterol is atherogenic lipoproteins) increased, respectively, by treatment time by 20.6, to 32.7, 32.7 per cent.

The stability of the proposed composition was determined using the developed analytical methods of analysis for each active substance included in the composition.

Riboflavin, ascorbic acid, pyridoxine hydrochloride, nicotinamide, thiamine Mononitrate, folic acid, retinol palmitate, ergocalciferol, alpha-tocopherol acetate, leucine, isoleucine, lysine hydrochloride, phenylalanine, threonine, valine, tryptophan, methionine. The determination carried out by HPLC method.

According to the data obtained (table 5 - results of a study of the stability of the composition), the shelf life is 3 years.

The results of pharmacological tests showed that the compositions of granules, pellets ensures the effectiveness of the drug: hepatoprotective, hypolipidemic, immune is stimulating and normalizing the function of the kidneys effects.

Based on the above we can conclude that the proposed arrangement has a number of advantages in comparison with the prototype.

Application examples of the present invention allows to expand the range of effective drugs.

Table 1
The results of biochemical analysis before and after treatment
Before treatmentAfter the treatment
BUN (mmol/l)44.76±12.7829.64±9.60*
Scr (imol/l)1034.28±495.041105.32±459.31
Ccr (ml/min)5.94±3.325.93±1.79
Alb (g/l)39.21±6.7239.21±5.62
TP (g/l)69.42±7.8272.82±5.62
Hb (g/l)81.72±21.3280.71±31.42
Calcium (mmol/l)1.78±0.622.29±0.86*
Phosphorus (mol/l)2.20±0.861.62±0.92
TG (mmol/l)1.32±0.421.42±0.32
Gh (mmol/l)7.75±3.326.98±2.12
Glucose (mmol/l)5.06±0.415.12±0.82

Table 2
Change of SIL-2R in the blood and urine (u/ml)
BloodUrine
The control group110.05±38.8982.01±13.84
Before treatment244.68±19.36*162.82±78.32
After the treatment117.04±35.0194.32 P<0.0519.30
- Comparison of control and treatment groups, P<0.01

Table 3
Concentration is Oia plasma amino acids before and after treatment
Before treatmentAfter the treatment
Threonine141.62±31.16195.14±47.62
Valine232.42±41.92*329.40±53.08
Methionine32.61±at 13.9236.79±25.31
Isoleucine60.80±10.32*100.86±25.04
Leucine106.43±55.16156.26±42.79
Phenylalanine84.15±35.94**220.81±62.73
Tryptophan29.74±10.02*57.94±15.49
Lysine177.61±44.63189.87±30.75
All essential amino acids1008.28±81.72*1145.22±60.41
AsparagineAt 54.08±12.73**18.32±5.86
Serine93.66±27.21*147.32±39.06
Glutamic acid155.03±51.92**62.81±22.80
Glycine442.47±82.95**223.35±41.12
Alanine562.73±131.11**343.18±71.01
Tyrosine80.57±40.4783.28±34.47
Histidine182.01±29.86*151.86±at 26.81
Arginine159.51±26.20*132.21±40.31
Only non-essential amino acids1730.52±123.53**1162.41±80.52
The ratio of total essential amino acids to the total number of non-essential amino acids0.582±0.094**0.985±0.117
* P<0.05; ** P<0.01

Table 4
The result of the analysis of immunity in two groups
PointsMedical group is and The control grouptP
IgA1.53±0.051.09±0.103.96<0.001
IgM1.36±0.401.39±0.470.04>0.05
IgG10.10±1.578.09±1.309.52<0.001
C31.42±0.140.80±0.261.35>0.05
LTT57.03±10.7141.82±11.795.16<0.001

1. The composition having hepatoprotective, hypolipidemic, immune stimulating and normalizing the function of the kidneys effect, containing vitamins and excipients, characterized in that it consists of seven types of granules, and white granule contains nicotinamide, pyridoxine, calcium Pantothenate, starch, lactose, cellulose, ka is ice carboxymethyl cellulose, the titanium oxide in the following ratio of ingredients, wt.%:

Nicotinamide1-35
Pyridoxine0,1-8
Calcium Pantothenate0.1 to 15
Lactose1-20
The titanium oxide0,1-20
Carboxymethylcellulose calcium1-11
Cellulose crystallineto 100

white granule contains thiamine Mononitrate, starch, lactose, cellulose, karboksimetilcelljulozy calcium, methylcellulose, titanium oxide at the following ratio, wt.%:
Thiamine0,1-30
Starch1-10
Cellulose10-12
Carboxymethylcellulose calcium1-15
The methylcellulose0,1-5
The titanium oxide 0,1-5
Lactoseto 100

red pellet contains L-tryptophan, tocopherol acetate, starch, lactose, crystalline cellulose, carboxymethylcellulose calcium, hydroxypropylcellulose, macrogol 6000, synthetic aluminum silicate in the following ratio of ingredients, wt.%:
Tryptophan1-30
Tocopherol0,5-5
Starch1-25
Crystalline cellulose0,5-6
Carboxymethylcellulose calcium0,5-6
Hydroxypropylcellulose0,1-6
Macrogol 60000.1 to 2
Aluminum silicate0.1 to 15
Dye0,001-1
Lactoseto 100

chocolate pellet contains ascorbic acid, starch, lactose, crystalline cellulose, carboxymethylcellulose calcium, matila is lulose, marcopol 6000 in the following ratio of ingredients, wt.%:
Ascorbic acidof 0.1-50
Starch0,5-10
Cellulose crystalline5-7
Carboxymethylcellulose calcium1-10
The methylcellulose0,1-6
Marcopol 60000,1-10
Dye0,001-1
Lactoseto 100

orange granule contains 5-hydroxyanthranilic acid, Riboflavin, folic acid, cyanocobalamin, starch, lactose, crystalline cellulose, carboxymethylcellulose calcium, hydroxypropylcellulose, macrogol 6000 in the following ratio, wt.%:
5-hydroxyanthranilic acid0,01-10
Riboflavin0,1-10
Folic acid0,1-6
Cyanocobalamin0,001-6
Starch0,5-30
Cellulose crystalline1-10
Carboxymethylcellulose calcium0,1-6
Hydroxypropylcellulose0,1-7
Macrogol 60000,1-5
Dye0,001-1
Lactoseto 100

yellow granule contains isoleucine, leucine, lysine, phenylalanine, threonine, valine, methionine, starch, lactose, cellulose, methylcellulose calcium, hydroxypropylcellulose, the dye in the following ratio, wt.%:
Isoleucine0,5-10
Leucine0.5 to 15
Lysine0,5-20
Phenylalanine0,1-5
Threonine0,1-5,0
Valineof 0.1 to 8.0
Methionine0.1 to 15
Lactose1-4,0
Cellulose1-11
The methylcellulose calcium1-3,0
Hydroxypropylcellulose0,1-1,0
Dyeof 0.001 to 1.0
Starchto 100

light yellow granule contains ergocalciferol in the following ratio, wt.%:
Ergocalciferol1-95,0
Starch100

2. A method of obtaining a composition according to claim 1, having hepatoprotective, hypolipidemic, immune stimulating and normalizing the function of the kidneys action in seven pellets, and white granules contain nicotinamide, which is mixed with pyridoxine, calcium Pantothenate, then, lactose, carboxymethylcellulose calcium, titanium oxide, then the parts added under stirring lactose, the mixture is uniformly moistened with water, then granularit the mixture through a sieve granulator, dried granules to a residual is humidity not more than 0.5%, the finished granules are poured into the container, prepare white granules, mixed thiamine, starch, cellulose, carboxymethylcellulose calcium, titanium oxide and methylcellulose, and parts added under stirring lactose, evenly moistened with water, the mixture granularit through a sieve granulator, dried granules to a residual moisture content not more than 0.5%, and the finished pellets are poured into the container, then prepare red granules, for this mix tryptophan with tocopherol, starch, hydroxypropylcellulose, crystalline cellulose, carboxymethylcellulose calcium, macrogol 6000, aluminium silicate, dye, add parts in several stages, with constant stirring lactose, moisturize with water; then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%, the finished pellets are poured container, then prepare chocolate granules, for this mix ascorbic acid with starch, crystalline cellulose, carboxymethylcellulose calcium, methyl cellulose, macrogol 6000 and dye, add parts in several stages with constant stirring, lactose hydrate with water, then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%, and the finished pellets are poured into the container, then prepare orange granules, with eshivot 5-hydroxyanthranilate acid Riboflavin, folic acid, cyanocobalamine, starch, crystalline cellulose, carboxymethylcellulose calcium, hydroxypropylcellulose, macrogol 6000 and dye, add parts in several stages with constant stirring lactose hydrate with water, then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%, the finished pellets are poured into the container, then prepare yellow granules, mixed isoleucine with leucine, lysine, phenylalanine, threonine, valine, methionine, lactose, cellulose, methylcellulose calcium, hydroxypropylcellulose, dye, add parts in several stages with constant stirring starch, moisten the mixture with water then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%, the finished pellets are poured into a container and prepare a light yellow granules, ergocalciferol mixed with starch, if necessary, moisten the mixture with water in a small amount, then granularit the mixture through a sieve granulator, dried granules to a residual moisture content not more than 0.5%, the finished pellets are poured into the container and mix the granules with each other in the amount of: white 17%, white 7%, yellow 36%, orange 12%red 8%, chocolate 13%, light yellow 7%, and fill the capsules.



 

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22 cl, 7 ex, 6 tbl

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12 cl, 1 ex

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5 cl, 6 ex, 12 tbl

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14 cl, 39 ex

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15 cl, 39 ex

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3 cl, 14 tbl, 7 ex

FIELD: medicine.

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17 cl, 15 ex

FIELD: medicine.

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6 cl, 4 ex

FIELD: medicine, pharmaceutics.

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19 cl, 8 ex

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13 cl, 48 dwg, 2 tbl, 24 ex

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