Pharmaceutical composition possessing antithrombotic, thrombolytic, immunomodulatory, anti-inflammatory action, normalising lipid and carbohydrate metabolism

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, more specifically to a pharmaceutical composition possessing antithrombotic, thrombolytic, immunomodulatory, anti-inflammatory action, normalising lipid and carbohydrate metabolism, more specifically to the pharmaceutical composition of the substance Pijavitum (hereinafter referred to Pijavitum) made from lyophilised medicinal leech. The above pharmaceutical composition is presented in the form of an enteric coated tablet.

EFFECT: coating prevents the active ingredients of Pijavitum from destruction under action of the enzymes and acid medium of the stomach.

 

The invention relates to medicine, specifically to a pharmaceutical composition having antithrombotic, thrombolytic, immunomodulatory, anti-inflammatory action, normalizes lipid and carbohydrate metabolism, particularly to pharmaceutical compositions on the basis of the substance "pewit" (hereinafter pewit)made from dried leech and registered as such FC of the Russian Federation (number of state registration of normative document PEWIT SUBSTANCE P N00363/01 dated 07.08.2007. The never expires. The Fund 42-0543-06).

Active principle of the drug pewit is the salivary cells of the medicinal leech (SCQ), representing the vast "leech pharmacy", which is a balanced complex of more than hundreds of high molecular weight proteins and several hundred low-molecular compounds.

It is important to bear in mind that the FCS is able to retain its numerous functions only in a state of immobilization particles within the muscle tissue of the medicinal leech, which takes place in the composition of the dried and crushed the medicinal leech. In addition to the FCS important role in the composition of javita given to fragments of the intestinal canal leeches, which are the main source of inhibitors of proteolytic enzymes, trypsin and chymotrypsin, which protects the biologically active with the organisations FCS from destruction in the gastrointestinal tract.

When studying pevita were previously identified the main functions of javita: protective (plasma hemostasis, platelet-vascular hemostasis); thrombolytic; bacteriolytic and bactericidal action; hypoglycemic effect; protivopostavlenie; enhancing phagocytosis; immunomodulatory effects (activation of cellular immunity, suppression of humoral immunity; neuroregulation (neurotrophic effect, analgesia, memory trace conservation); antisclerotic (normalization of lipid metabolism) (Baskova I.P., isakhanyan G.S. "Hirudotherapy. Science and practice". 2004, M.: "Monolith").

Antithrombotic and anti-inflammatory effect is characterized antiproteolytic and anticoagulant activity, the latter aimed at the inhibition of platelet-vascular (Calin, saratin, apyrase and others) and plasma hemostasis (inhibitor of plasma kallikrein, inhibitor of factor XA, thrombin inhibitor is hirudin). Antiproteolytic activity (antichymotrypsin and antiaritmichesky) due to the presence in the complex of the salivary cells leeches substances such as belini (inhibitors of trypsin, plasmin and acrosin), agony (inhibitors of α-chymotrypsin, hematine, subtilisin, elastase and cathepsin G), Gerstein (inhibitor of tissue kallikrein, elastase and cathepsin G). Thrombolite the mini effect due to the presence of the enzyme destabilase - lysozyme, a bifunctional enzyme possessing isopeptidases (thrombolytic) and lysozyme (antibacterial) and non-enzymatic antimicrobial function. Additionally, this enzyme inhibits spontaneous and induced aggregation of human platelets. Lysis of the thrombus while slow, so you can connect reparative processes of healing of the wound surface of the vascular wall and thus prevents re-formation of a blood clot at the site of the vessel. Thrombolytic action of javita unlike known in medical practice drugs does not depend on the age of the thrombus.

Thus, the unique active complex of javita is that the drug has at the same time fibrinolytic and anticoagulant activities (dissolves existing blood clots and prevents the formation of new ones). This process is accompanied by the removal of the inflammatory phenomena caused by stagnation of blood in the vessels because of their thrombosis. Anti-inflammatory effect is also determined by the presence of an active complex of glinow and Giustina blocking anti-inflammatory enzymes elastase and cathepsin G neutrophils, analogue of prostacyclin, preventing the release of inflammatory mediators, as well as the presence of an inhibitor of kallikrein blood plasma, noise reduct the subsequent formation of inflammatory mediators - kinins.

Anti-edema effect contained in the active complex collagenase and hyaluronidase.

Anti-sclerotic and analgesic effect of the active complex due to antithrombotic and anti-inflammatory activity, the ability to normalize lipid metabolism, as well as a number of other factors studied in the present time.

Thus, pharmaceutical compositions on the basis of the substance of javita that contains a balanced package of highly effective substances produced medical leeches are effective preventive and therapeutic antithrombotic agent with thrombophlebitis of subcutaneous veins.

Among the first gained fame capsules pevita - drug oral drug Pewit-capsules" (number of state registration, regulatory document R N000363/02 dated 22.05.2008. The never expires. The Fund 42-0544-06. Solution N11-22486/09 from 02.11.2009. CAPSULES PEWIT, 150 mg). The drug is a gastric-soluble gelatin capsules containing 0.15 g or 0,30 g pewit-substance recommended for the prevention and treatment of thrombophlebitis of the superficial veins, as well as for the prevention and treatment of diabetic micro - and macroangiopathies. They are able to inhibit the activation of trombotsitarno-vascular and plasma hemostasis, anti-inflammatory, intiate accelerationtime and thrombolytic properties, normalize lipid and carbohydrate metabolism and have a number of other properties.

A known method of manufacturing pellets from lyophilised powder of medicinal leeches (published application CN 101897727 And abstract) has drawbacks consisting in the application of the granulation in the manufacture of tablets and the lack of effective preservative for enzymes leeches, which can lead to destruction of the components of javita.

There is a method of treatment of atopic dermatitis and heylity using ointment javita (RF Patent No. 2138276).

The proposed medicinal film containing pewit, for the treatment of inflammatory periodontal diseases (Patent RF №2201194).

Known therapeutic gel pewit with anticoagulant, anti-inflammatory and analgesic activities, and a method of producing gel (RF Patent No. 2268739).

The closest to the technical nature of the claimed object is proposed a method for the treatment of nonhealing wounds in patients with diabetes mellitus (RF Patent No. 2358757), which consists in applying to the surface of the wound ointment pewit 2-3 times a day surgery skin grafting and taking the capsules pivit in the amount of 300 mg 2 times a day during the entire course of treatment.

Lack of dosage forms in the form of capsules is the absorption of active substances of javita in the stomach, which leads to partial decomp is the supply of a number of biologically active components of javita under the action of gastric juice and reduce the effectiveness of the drug. In addition, the substance peewit has a characteristic (unpleasant) smell that permeates through a gelatin capsule.

The aim of the invention is a new pharmaceutical composition on the basis of the substance of javita in the form of tablets, enteric-coated shell. The coating protects the active components of javita from destruction under the action of enzymes and the acidic environment of the stomach, which is confirmed by experimental researches. Tablets, enteric-coated membrane was placed in an artificial gastric juice (pH 1-3), and the membrane pellets have been destroyed and there was no release of active enzymes pevita. It is shown that the film sheath on the basis of acrylite dissolves only in the intestines (rn,0-8,0) Released in the intestine, components pevita operate more efficiently, thereby reducing the dose of medications taken. It was established experimentally that the tablets are enteric-coated shell, more than doubled during the formation of a thrombus (table 3, examples 3 and 4). This pharmaceutical composition shall meet the requirements of the State Pharmacopoeia XI and XII, to have a shelf life of not less than 2 years.

This goal is achieved by creating a solid dosage pharmaceutical composition in tablet form containing AK the active substance pewit and targeted supplements.

The specified composition was prepared by pre-mixing the target additives and pevita with subsequent direct pressing of the mixture and coating the enteric coat.

The ratio of the active substance and the target additives is, wt.%:

active substance (powder pevita)5,0-40,0
additives target60,0-95,0

The choice of target components and their relations, helped to develop the technology of direct pressing of the mass with the substance of javita without granulation, which avoids degradation enzymes leeches.

As the target additives pharmaceutical composition contains optional simultaneously starch, sodium Crocker-mellow, polyvinylpyrrolidone, derivatives of cellulose, Aerosil, salts of stearic acid, correcting substances in the following ratio, wt.%:

0,0-5,0
starch1,0-15,0
sodium chloride5,0-60,0
crosscarmellose sodium2,0-5,0
polyvinylpyrrolidone
derivatives of cellulosea 2.0 to 50.0
colloidal silicon dioxide (Aerosil)0.5 to 10.0
salt of stearic acid0,5-1,0
acrylis5,0-10,0

Acrylis to Colorcon contains the ingredients: methacrylic acid copolymer, titanium dioxide, sodium bicarbonate, sodium lauryl sulfate, talc and colloidal silicon dioxide (Aerosil)

The presence of solid dosage forms of starch, Primerose, polyvinylpyrrolidones, cellulose derivatives increase the speed of release and the completeness of absorption of the active substance, increases raspadaemost and dissolution of the dosage form, and creates the conditions for the penetration of water and enzymes in pill.

Starch, preferably, use corn or potato.

The presence of salts of stearic acid provides the effect of slip required at the stage of pressing tablets. As the salts are useful stearate or calcium.

Sodium chloride acts as a preservative, as active components pevita contains organic compounds that are prone to oxidation and degradation. Adding the atrium chloride increases the shelf life of the dosage form.

Acrylis as an enteric film coating protects the tablet from decomposition by enzymes of the stomach and masks the odor of javita.

The claimed ratio of components and the technology of production by the method of direct compression was found experimentally to be optimal and can achieve a technical result that is appropriate to the task: the obtained pharmaceutical composition meets the requirements of the State Pharmacopoeia XI and XII publications, has a shelf life of not less than 2 years and provides a high pharmacological effect of the active substance.

The composition and methods of manufacture of the claimed pharmaceutical compositions described in the examples of the preparation of solid pharmaceutical composition in the form of tablets enteric-coated shell.

Example 1. In the apparatus with stirrer download the starch 2,14 kg (10,24%), colloidal silicon dioxide 2,04 kg (9,76%), sodium chloride (1.06 kg (5,07%), sodium croscarmelose 0.52kg (of 2.51%), microcrystalline cellulose 10,49 kg (50,23%); the mass is stirred for 10-15 minutes To the resulting homogeneous mass download of 2.27 kg (10,86%) substance of javita remaining starch 1.0 kg (4,78%), the mixture is stirred for 10 min, and then upload 0.21 kg (1,00%) of magnesium stearate. The mass is stirred until a homogenous mixture for 15-20 min. Get 19,45 kg datamateriale, containing 2,16 kg pevita that tabletirujut by direct pressing. Get 51184 pieces tablets-nuclei (mass nuclei - 380 mg), which cover the enteric coat. Consumption of acrylite is 1.02 kg (5,26%). Get 50360 pieces of tablets pewit weight of 400 mg enteric-coated shell containing 2,12 kg pevita. Output accounts for 93.4%, considering the original pewit.

The tablets comply with the requirements of Gasfurnace XI and XII publications (table 1).

Example 2. Analogously to example 1 from 0.4 kg (5,00%) pevita, 3.4 kg (42,50%) sodium chloride solution, 1,16 kg (14,50%) of corn starch, 2,08 kg (26,00%) cellulose microcrystalline, 0.16 kg (2,00%) sodium croscarmelose, 0.32 kg (4,00%) silicon dioxide colloidal, 0.08 kg (1,00%) of magnesium stearate and 0.4 kg (5,00%) of acrylite get 18000 pieces of tablets pewit weight of 400 mg enteric-coated shell containing 0.38 kg of javita. The output is 95,0%, considering the original pewit.

The tablets comply with the requirements of Gasfurnace XI and XII publications (table 1).

Example 3. Analogously to example 1 from 160 g (40,00%) pevita, 158 g (39,50%) of sodium chloride, 4 g (1,00%) of corn starch, 22 g (5,50%) of microcrystalline cellulose, 20 g (5,00%) sodium croscarmelose, 2 g (0,50%) silicon dioxide colloidal, 4.0 g (1,00%) of magnesium stearate and 30.0 g (7,50%) of acrylite get 948,0 pieces of tablets pewit weight of 400 mg coated symptoms such is rastvorimoi shell, containing 152 g pevita. The output is 95,0%, considering the original pewit.

The tablets comply with the requirements of Gasfurnace XI and XII publications (table 1).

Example 4. Analogously to example 1 from 2.00 kg (25,00%) pevita, 3,60 kg (45,00%) sodium chloride, 0.12 kg (1,50%) of corn starch, 0,44 kg (5,50%) cellulose microcrystalline, 0.28 kg (3,50%) sodium croscarmelose, 0.32 kg (4,00%) silicon dioxide colloidal, 0.04 kg (0,50%) of magnesium stearate, 0.4 kg (5,00%) polyvinylpyrrolidone and 0.8 kg (10,00%) of acrylite get 18000 pieces of tablets pewit weight of 400 mg enteric-coated shell containing 1.52 kg of javita. The output is 95,0%, considering the original pewit.

The tablets comply with the requirements of Gasfurnace XI and XII publications (Tables 1, 2).

Table 1
The compositions of the tablets javita
IngredientsExample 1Example 2Example 3Example 4
%mg%mg%mgmg
Pewit10,8643,445,02040,016025,0100
Starch15,026014,5581,0041,506
Colloidal silicon dioxide9,76394,0160,5024,0016
Sodium chloride5,0720,342,517039,515845,0180
Crosscarmellose sodiumof 2.5110,042,085,00 203,5014
Microcrystalline cellulose50,23200,926,01045,50225,5022
Magnesium stearate1,0041,0041,0040,502
Polyvinylpyrrolidone5,0020
Acrylis5,5522,25,0207,53010,040
Total100400,0100400 100400100400

Table 2
Indicators of quality solid pharmaceutical compositions are tablets pewit enteric-coated shell
The quality indicatorsStandards of quality requirementsThe actual indicators
Example 1Example 2Example 3Example 4
DescriptionWhite or white with white shadeWhiteWhiteWhiteWhite with white shade
Stability in gastric juiceMust not breakRelevant is the duty to regulate
The quantitative content of javitaNot less than 98,5%99,099,099,2the 98.9
ImpuritiesNot more than 1% (TLC)0.50.50.50.5
Stability2 years at 20°C2 years2 years2 years2 years

Table 3
Thrombolytic (anticoagulant) activity, AKE
Known capsules pevita, 150 mg, gastro-solubleTablets pewit enteric-coated shell
Example 1Example 2Example 3Example 4
43,44 mg20 mg160 mg100 mg
Not menee,0, AKEto 140.5, AKA63,2, AKA390,5, AKA308,0, AKA
Note: thrombolytic (anticoagulant) activity is expressed in arbitrary units (CRR) by lengthening the time of the formation of a clot (thrombus).

Table 4
Requirements for coating tablets
The conditions of the experimentRequirements for coating tabletsThe actual indicators
Example 1Example 2Example 3Example 4
pH 1-2 (conditions of the stomach)Should not break downMaintained the integrity of the coatingMaintained the integrity of the coatingSaved celest is here cover Maintained the integrity of the coating
rn-8 (conditions of the small intestine)Tablet disintegrates, releasing enzyme geroginaTablet disintegrates, releasing enzyme geroginaTablet disintegrates, releasing enzyme geroginaTablet disintegrates, releasing enzyme geroginaTablet disintegrates, releasing enzyme gerogina

Solid dosage pharmaceutical composition having antithrombotic, thrombolytic, immunomodulatory, anti-inflammatory action, normalizes lipid and carbohydrate metabolism, characterized by the fact that it is made in the form of tablets by direct pressing and contains as active substance a substance made from dried leech, and the target additives, sodium chloride, starch, sodium croscarmellose, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate, optional polyvinylpyrrolidone, in the following ratio, wt.%

Pewit5,0-40,0
Starch1,0-15,0
Sodium chloride5,0-60,0
Sodium croscamellose2,0-5,0
Polyvinylpyrrolidone0,0-5,0
Derivatives of cellulosea 2.0 to 50.0
Colloidal silicon dioxide (Aerosil)0.5 to 10.0
Salt of stearic acid0,5-1,0

This tablet enteric-coated membrane composition of Acrylis in the amount of 5-10%.



 

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21 cl, 7 dwg, 23 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine, namely to using at least one immunomodulatory compound of general formula (1) or a pharmaceutically acceptable, solvate or isomer thereof for preparing a pharmaceutical composition for treating a disease or disorder specified in asthma, atopic dermatitis, allergic rhinitis, inflammatory intestinal disease, diabetes or rheumatoid arthritis in homoiothermal animal, including a human. What is also presented is using (5S,11R)-1-amino-5-[(R)-3-dodecanoyloxytetradecanoylamino]-6-oxo-7-aza-11-[(R)-3-hydroxytetradecanoylamino]dodecan-12-ol-12-dihydrophosphate (OM-294-BA-MP (S,R)) or a pharmaceutically acceptable salt, solvate or isomer thereof for preparing the pharmaceutical composition.

EFFECT: group of inventions provides treating the above diseases by modulating the TH1/TH2 cytokine balance by reducing TH2-cytokine release and enhancing TH2-cytokine production.

11 cl, 16 dwg, 14 ex

FIELD: medicine.

SUBSTANCE: invention relates to a method of treating or reducing insulin resistance in susceptible warm-blooded animals, including people. Method includes introduction of a selective estrogen receptor modulator (SERM).

EFFECT: described is SERM combination with an amount of estrogen or a precursor of a sexual steroid hormone, selected from a group, consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-en-3b,17b-diol and compounds, converted in vivo into one of the said precursors or estrogen.

2 cl, 13 ex, 13 tbl, 8 dwg

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