Chondroitin sulfate solid medicinal formulation

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to the solid medicinal formulation comprising chondroitin sulfate. The proposed medicinal formulation comprises 250 mg of chondroitin sulfate as an active component, filling agent, binding agent, antifriction substances and can comprise a solubilizing agent additionally. Pharmaceutical composition is made as a tablet. Invention provides development of the preparation for oral administration with the less amount of active substance and with indices satisfying requirements of the State Pharmacopoeia.

EFFECT: improved and valuable properties of formulation.

8 cl, 16 tbl, 39 ex

 

The invention relates to the field of medicine and for the creation of a medicinal product in the form of tablets based on chondroitin sulfate used for treatment of degenerative diseases of joints and spine.

According to the world health organization more than 50% of the population over the age of 50 years suffer from disorders of the joints and spine.

The main changes of metabolic processes in degenerative joint disease associated with impaired metabolism of cartilage and its depletion the main polysaccharide of animal tissue chondroitin sulfate. As a result, the cartilage loses its mechanical properties: elasticity, strength, resistance, reduced in volume and degrades. In this regard, the important is the problem of finding new reliable and also secure funds chondroprotective action.

Known ointment for the treatment of joints “handaxe” [1]. The tool is “external”. It should be noted that, given the commitment to the treatment preferred drugs are taken enterline.

Known dosage form in the form of tablets, coated [2] “Cartilag Vitrum”, containing chondroitin sulfate in the amount of 750 mg, excipients in this source is not disclosed. This dosage form is selected by the authors as a prototype. And what's information about the tablets on the basis of chondroitin sulfate in the available sources are not detected.

Known dosage form is a tablet of large volume, as it contains a large number of active substances, as a result makes it difficult to swallow.

Object of the present invention is to provide a preparation for oral administration in the form of tablets with a smaller amount of active ingredient chondroitin sulfate, a smaller amount comfortable for ingestion, with characteristics that satisfy the requirements of the State Pharmacopoeia, which is needed to replenish the register of medicines.

The technical result achieved during the implementation of the present invention is the preparation of solid dosage forms, i.e. tablets based on chondroitin sulfate, convenient for oral administration, in which the content of active substance is reduced to 250 mg mainly, and providing androstenolone, regenerating, anti-inflammatory effect. This composition complies with the requirements of the State Pharmacopoeia XI edition and expands the Arsenal of drugs suitable for use in medical practice.

This technical result is achieved by creating a solid dosage form containing chondroitin sulfate as the active substance, according to the invention it is more the tion contains anti-friction substance, binder and filler in the following ingredients, wt.%:

Chondroitin sulfate 49,58-55,83

Binder 1,0-3,5

Anti-friction substance 0,5-1,0

Filler To 100

Preferably the binder form contains the low-molecular polyvinylpyrrolidone, or kollidon, or plasmon, or paseli.

Preferably as anti-friction substances form contains Aerosil, or talc, or calcium stearate, or magnesium stearate, or a mixture of magnesium/calcium stearate and Aerosil, or a mixture of magnesium/calcium stearate and talc, or a mixture of magnesium/calcium stearate, talc and Aerosil.

Preferably the filler form contains magnesium carbonate basic, or microcrystalline cellulose, or a mixture of magnesium carbonate and microcrystalline cellulose, or primogen.

It is preferable that the solid dosage form may further comprise a solubilizer in an amount of not more than 6.0 wt.%.

Preferably as a solubilizer it contains polyplasdone, or crosspovidone, or primogel, or Primerose.

It is preferable that the solid dosage form is made in tablet form.

It is preferable that the solid dosage form can be coated.

The proposed ratio of ingredients found experimentally and is optimal.

Binder - this is an auxiliary substances which promote the formation of granules from components tabletas mass, thereby compressibility mass and strength tablets [3, str]. In the proposed composition is used, the low molecular weight polyvinylpyrrolidone, such as FS 42-1194-98, or Kollidon (ND 42-8482-98), or plasdone K-25 (ND 42-10112-99), or plasmon To 29/32 (ND 42-10109-99), or pateli (USP).

Anti-friction substance, in turn, are divided into moving and lubricating, gaining traction on the surface of the granules (particles), eliminate their roughness and thereby increase the fluidity of the tablet mass, which ensures uniform filling of the matrix tablet press and leads to a homogeneous mass of tablets. In addition, reduce the friction on the contact (mass press) areas, greatly facilitates the deformation of the particles due to the adsorption of lowering their strength [3, str].

In the proposed structure of this component may be represented by the following options:

- Aerosil (GOST 14922-77);

- talc (FS 42-006601);

- calcium stearate (TU 6-09-4233-76);

- magnesium stearate (TU 6-09-129-75);

a mixture of magnesium/calcium stearate and Aerosil (GOST 14922-77);

a mixture of magnesium/calcium stearate and talc;

a mixture of magnesium/calcium stearate, talc and Aerosil.

Soljubilizatory - substances that contribute to the dissolution of the acting is th component [3, str], the proposed structure can be represented by the following options:

- polyplasdone XL-10 (ND 42-10113-99);

- crosspovidone (ND 42-8871-98);

- primogel (EP, USP);

- Primerose (EP, USP).

The filler gives the mass of the required quality, allows you to have constant weight pills [4], the proposed farbkomposition can be represented by the following options:

- magnesium carbonate basic (GOST 6419-78);

- microcrystalline cellulose (FS 42-3728-99);

a mixture of magnesium carbonate and microcrystalline cellulose;

- promogran (USP, EP)

When coatings are used ready mix “Opadry” company “use” (USA), or the film Collicut BASF (Germany), or Eudragit company “REM-Pharma (Germany), as well as coatings based on cellulose derivatives, providing for the dissolution of the active substance in the stomach.

The inventive composition provides a specified pharmacological action meets the requirements of the State Pharmacopoeia XI ed., stable during storage and has a shelf life of not less than two years.

The proposed structure can be illustrated by the following examples.

Example 1.

wt.%

Chondroitin sulfate 49,58

The low-molecular polyvinylpyrrolidone 1,0

Polyplasdone 6,0

Calcium stearate 1,0

Magnesium carbonate basic 100

Example 2. The composition p is similar to example 2 the composition of example 1, only as a binder is used collide.

Example 3. The composition according to example 3 is similar to the composition of example 1, except that the binder used Plascon.

Example 4. The composition according to example 4 is similar to the composition of example 1, except that the binder used paseli.

Example 5. The composition according to example 5 is similar to the composition of example 1, except that as an antifriction material used are presented.

Example 6. The composition according to example 6 is similar to the composition of example 1, except that as an antifriction material used talc.

Example 7. The composition according to example 7 is similar to the composition of example 1, except that as an antifriction material used magnesium stearate.

Example 8. The composition according to example 8 is similar to the composition of example 1, except that as the lubricating substance is used a mixture of magnesium stearate and Aerosil.

Example 9. The composition according to example 9 is similar to the composition of example 1, except that as the lubricating substance is used a mixture of calcium stearate and Aerosil.

Example 10. The composition according to example 10 is similar to the composition of example 1, except that as the lubricating substance is used a mixture of calcium stearate and talc.

Example 11. The composition according to example 11 is similar to the composition of example 1, except that as the lubricating substance is used a mixture of magnesium stearate and tal is CA.

Example 12. The composition according to example 12 is similar to the composition of example 1, except that as the lubricating substance is used a mixture of calcium stearate, talc and Aerosil.

Example 13. The composition according to example 13 is similar to the composition of example 1, except that as the lubricating substance is used a mixture of magnesium stearate, talc and Aerosil.

Example 14. The composition according to example 14 is similar to the composition of example 1, except that as a solubilizer is used crosspovidone.

Example 15. The composition according to example 15 is similar to the composition of example 1, except that as a solubilizer is used primogel.

Example 16. The composition according to example 16 is similar to the composition of example 1, except that as a solubilizer is used Primerose.

Example 17.

wt.%

Chondroitin sulfate 49,58

The low-molecular polyvinylpyrrolidone 1,0

Magnesium stearate 1,0

Microcrystalline cellulose To 100

Example 18. The composition according to example 18 is similar to the composition of example 17, only as a binder is used collide.

Example 19. The composition according to example 19 is similar to the composition of example 17, only as a binder is used, platton.

Example 20. The composition according to example 20 is similar to the composition of example 17, only as a binder is used paseli.

Example 21. The composition according to example 21 is similar to the composition of example 17, just as the anti-Christ. reaktsionnogo substances used are presented.

Example 22. The composition of example 22 is similar to the composition of example 17 as an antifriction material used talc.

Example 23. The composition according to example 23 is similar to the composition of example 17 as an antifriction material used calcium stearate.

Example 24. The composition of example 24 is similar to the composition of example 17 as an anti-friction substance is used a mixture of magnesium stearate and Aerosil.

Example 25. The composition of example 25 is similar to the composition of example 17 as an anti-friction substance is used a mixture of calcium stearate and Aerosil.

Example 26. The composition according to example 26 is similar to the composition of example 17 as an anti-friction substance is used a mixture of calcium stearate and talc.

Example 27. The composition according to example 27 is similar to the composition of example 17 as an anti-friction substance is used a mixture of magnesium stearate and talc.

Example 28. The composition according to example 28 is similar to the composition of example 17 as an anti-friction substance is used a mixture of calcium stearate, talc and Aerosil.

Example 29. The composition according to example 29 is similar to the composition of example 17 as an anti-friction substance is used a mixture of magnesium stearate, talc and Aerosil.

Example 30.

wt.%

Chondroitin sulfate 55,83

Polyvinyle the Lydon low molecular weight 3,5

Magnesium stearate 0.5 to

A mixture of magnesium carbonate basic

and microcrystalline cellulose

the ratio of 1:1 To 100

Example 31. The composition of example 31 is similar to the composition of example 30 as an anti-friction substance use are presented.

Example 32. The composition according to example 32 is similar to the composition of example 30 as an antifriction material used talc.

Example 33. The composition according to example 33 is similar to the composition of example 30 as an antifriction material used calcium stearate.

Example 34. The composition according to example 34 is similar to the composition of example 30 as an anti-friction substance is used a mixture of magnesium stearate and Aerosil.

Example 35. The composition according to example 35 is similar to the composition of example 30 as an anti-friction substance is used a mixture of calcium stearate and Aerosil.

Example 36. The composition of example 36 is similar to the composition of example 30 as an anti-friction substance is used a mixture of calcium stearate and talc.

Example 37. The composition of example 37 is similar to the composition of example 30 as an anti-friction substance is used a mixture of magnesium stearate and talc.

Example 38. The composition according to example 38 is similar to the composition of example 30 as an anti-friction substance is used a mixture of calcium, stear is the talc and Aerosil.

Example 39. The composition according to example 39 is similar to the composition of example 30 as an anti-friction substance is used a mixture of magnesium stearate, talc and Aerosil.

The above compositions according to the qualities meet the requirements of the global Fund XI, issue 2, str.

A method of manufacturing the proposed composition is as follows. Filler, possibly part of a solubilizer, hydrate binder, dried and granularit, then optivault active ingredient, anti-friction and possibly part of a solubilizer. The resulting mass tabletirujut and possibly covered with a shell in the amount not exceeding 0,024 g per tablet.

The content of chondroitin sulphate in one tablet is determined by therapeutic dose. When the amount of binder is less than 1% is not achieved the necessary strength pills, and when the amount of more than 3.5% is deteriorating dissolving tablets. The increase in the number of anti-friction substances more than 1% technologically feasible, and less than 0.5% does not ensure the flowability of the granules. The increase in the number of solubilizer more than 6% technologically impractical.

To determine the General toxic action and evidence of the effectiveness of the proposed tools, namely tablets based on chondroitin sulfate, convenient for oral administration, in which the content of active substance reduced to 250 mg mainly and providing androstenolone, regenerating, anti-inflammatory, were conducted its pre-clinical trials. Preclinical trials were conducted at the Central research laboratory of the Nizhny Novgorod state medical Academy in 2004.

To test the proposed tool was presented in the form of tablets of the following composition (table 17).

To establish toxic doses proposed funds were spent acute experiments intragastric the way of its introduction experimental animals of different species. In experiments were used 60 white mice of both sexes and 18 rats males. The number of animals in each group was 6.

Changes in behavior, appearance, and body weight of mice immediately after injection and during the 14 days was not detected (table 1, 2).

Sredneseriynoe dose after intragastric administration offer a means of nonlinear white mice was not achieved. The results of acute tests with intragastric introduction of the proposed tools mice were allowed to take him to the 4th class of low-hazard compounds (GOST 12.1.007-76). The sexual sensitivity of animals to the proposed tool is not installed.

Intragastric administration of the proposed means to rats at a dose of 20 g/kg also not the call is about the death of animals (table 3).

Thus, the proposed tool is not dangerous in terms of acute poisoning with specific pharmacological route of entry into the body.

After a single intragastric administration of the proposed tools in the experimental animals at necropsy and macroscopic description of the vital organs (size, shape, color, texture) within 14 days of the change relative to the control series is not revealed.

To study the General toxic effect of the proposed devices with regard to the intake path, recommended for clinical use, studied its effect when repeated intragastric application of rats in equicharacteristic doses (83 mg/kg) and doses exceeding equitisations 20 times (1660 mg/kg). The duration of injection was 30 days.

After intragastric application of the proposed tool in equicharacteristic and high doses did not reveal differences in the dynamics of body mass (table 4), the indicators of higher nervous activity (table 5), the state of the cardiovascular system (table 6).

The study of the basic biochemical parameters of blood serum revealed a high content of urea groups of experimental animals compared to control groups (table 7). On the 15th day of the recovery period statistically significant different is the extent to which the urea level in the studied groups of animals were not identified (table 8), the concentration of urea was within the physiological norm.

The results of hematologic studies showed that repeated intragastric application of the proposed tool does not cause significant differences in the indicators during the first days after the injection, and during the whole follow-up period compared with the control series (table, 10). The ratio of the individual forms of leukocytes in the leukocyte formula remains unchanged.

When evaluating membranotropic effect of the proposed means of intragastric application there were no significant differences with control (table).

The data obtained in the measurement of osmotic resistance of erythrocytes indicate no negative impact of the proposed remedies on erythrocyte membranes after intragastric application of the dose 83 mg/kg and 1660 mg/kg within 30 days.

At autopsy, the animals and the macroscopic description of the vital organs (size, shape, texture, color) changes it is not revealed.

Pathomorphological study of the structure of the heart, lungs, liver, kidneys, spleen, stomach and small intestine did not reveal any pathological changes in these organs in experimental animals after intragastric application of the proposed tool in equitisations dose (83 mg/kg).

After 15 suto is after the cancellation of the proposed tools in equitisations dose (83 mg/kg) pathomorphological study in the control and experimental groups of animals did not reveal violations in the microscopic structure of all studied bodies.

In the study of the microstructure of the heart, lungs, liver, kidneys, spleen, gastrointestinal tract, there were no differences in the structure of these organs in experimental and control rats after intragastric application of the proposed tools in a dose considerably higher than therapeutic (1660 mg/kg).

Within 15 days after the cancellation of the proposed tools in a dose exceeding equitisations (1660 mg/kg), pathological changes in the microscopic structure of all studied organs were not found.

Daily intragastric administration of the proposed means to rats at doses of 83 mg/kg and 1660 mg/kg for 30 days does not lead to a significant difference in the changes of weights of organs of rats compared to control after completion of the course the introduction of the proposed means, and after the recovery period (table).

Comparative pathological study of the vital organs of rats in experiments for the study of chronic 30-day toxicity proposed funds dose 83 mg/kg and 1660 mg/kg did not reveal any structural damage in heart tissue, lung, liver, kidney, spleen, stomach and small intestine.

The local effect of the proposed remedies were studied in applications at a dose of 20 mg/cm2the liberation is Noah from the hairline to the skin of rabbits. After 4 hours of exposure on the skin of rabbits there was no increase in skin folds. The color of the skin after 4 h were slightly altered, was observed weak redness. The state experienced skin after 1, 24, 48 hours after a single application of the proposed remedy did not differ from control (table 13).

Assessment of the sensitizing properties of the proposed tools were conducted in rabbits by repeated applications in a dilution of 1:10 for 20 days. Allow dose was applied in a dilution of 1:50 and 1:100. Sensitizing properties for cutaneous application is not installed. Local skin reaction was absent. The thickness of the skin fold was not changed. The number of eosinophils in the blood of experimental animals did not differ significantly from the initial state (table 14).

The regenerative action of the drugs studied in the simulation of osteoarthritis in rats.

The proposed remedy for the correction caused by the violations have introduced experimental animals intraperitoneally daily for 14 days., starting from the 8th day after injection of corticosteroids in equitisations dose 83 mg/kg

After completing the experiment was conducted in the determination of sialic acid in serum (table) and pathological examination of tissue of the knee joint of the hind paws of the rats in the control group (without treatment the Oia) and after treatment proposed remedy within 14 days.

Throughout the experiment evaluated the appearance of animals, the overall functional status, weight gain (table 16).

Determination of sialic acids, which are markers of inflammation or acute phase proteins, showed that the application of the proposed tool reduces their content, indicating a decrease in activity of the inflammatory process.

In preclinical studies assessed General toxic and specific pharmacological effects of the proposed tools.

Thus, our studies show that the proposed tool has a strong specific pharmacological effect, showing chondroprotective and regenerative effects in experimental arthritis and arthrosis, and has expressed no General toxic effect at different doses and routes of exposure of experimental animals.

Experimental studies were conducted in accordance with the requirements of the normative document “Guidance on experimental (preclinical) study of new pharmacological substances. - 2000”.

Literature

1. The radar. Encyclopedia of drugs. 2004, str.

2. The prototype. The radar. Encyclopedia of drugs, 2003, str.

3. Yourable. Technology of drugs, vol. 1. M.: Medicine, 1980.

4. State farm is copeia XI, 2), str.

1. Solid dosage form containing chondroitin sulfate as the active substance, characterized in that it further comprises anti-friction substance, a binder and filler in the following ingredients, wt.%

Chondroitin sulfate 49,58-55,83

Binder 1,0-3,5

Anti-friction substance 0,5-1,0

Filler To 100

2. Solid dosage form according to claim 1, characterized in that the binder form contains the low-molecular polyvinylpyrrolidone, or kollidon, or plasmon, or paseli.

3. Solid dosage form according to claim 1, characterized in that the antifriction substances it contains Aerosil, or talc, or calcium stearate, or magnesium is earth, or a mixture of magnesium/calcium stearate and Aerosil, or a mixture of magnesium/calcium stearate and talc, or a mixture of magnesium/calcium stearate, talc and Aerosil.

4. Solid dosage form according to claim 1, characterized in that the filler form contains magnesium carbonate basic, or microcrystalline cellulose, or a mixture of magnesium carbonate and microcrystalline cellulose, or primogen.

5. Solid dosage form according to claim 1, characterized in that it optionally contains a solubilizer in an amount of not more than 6.0 wt.%.

6. Solid dosage form according to claim 5, characterized in that as a solubilizer it contains polyplasdone, or crosspovidone, or primogel, or Primerose.

7. Solid dosage form according to claim 1, characterized in that it is made in the form of tablets.

8. Solid dosage form according to claim 7, characterized in that it can be coated.



 

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SUBSTANCE: invention relates to medicinal formulations. Tablet consists of a mixture of medicinal agents and accessory substances and made with internal cavity filled with air. Cavity can involve isolated cells and the reduced specific weight of tablet is less 1 g/cm3. Invention provides enhanced effectiveness and safety of orally ingested tableted medicinal agents and safety of dissolving process and absorption of medicinal agent in stomach.

EFFECT: improved and valuable properties of tablet.

2 cl

FIELD: pharmaceutical industry.

SUBSTANCE: pharmaceutical composition exhibiting neotropical, antiepileptic, sedative, and antistress activities, normalizing metabolic processes in body, contains aminoacetic acid and pharmaceutically acceptable carrier constituted by mixture of sorbitol and crosslinked carboxymethylcellulose sodium salt at weight ratio between 1:1 and 1:3 with additive selected from vinylpyrrolidone/vinyl acetate, stearic acid, stearic acid sodium salt, and mixtures thereof.

EFFECT: increased bioavailability and active component release velocity.

2 cl, 1 tbl

FIELD: pharmaceutics, medicine.

SUBSTANCE: the present innovation deals with cardiotherapy for treating and preventing coronary deficiency. The preparation is designed as a plate (film) consisted of three layers, each of them is manufactured out of co-polymer of vinyl pyrrolidone, acrylamide and nitroglycerin-containing ethylacrylate; moreover, internal layer additionally contains solid fat - cacao oil, and weight ratio for the sum of external layers to internal corresponds to 1 : 1. The suggested preparation could additionally contain brilliant green dyestuff. The preparation should be manufactured out of pre-obtained mixture of nitroglycerin and copolymer in solution of alcohol and water followed by layer-by-layer forming three-layer film due to spreading the mixture onto solid bottom plate and drying at 30-50 C. The innovation provides higher adhesion to gingival mucosal surface, decreased side action, improved bioavailability and stability of therapeutic effect.

EFFECT: higher efficiency of therapy.

3 cl, 3 ex

FIELD: pharmaceutical industry, medicine.

SUBSTANCE: invention relates to peroral immediate-released drug in solid form, containing low molecular thrombin inhibitor based on peptide with pH-depending solubility. Claimed drug has size particle less than 300 mum and contains combination of microcrystal cellulose and sodium glycolate starch in amount of more than 35 mass % (calculates as preparation mass).

EFFECT: drug with reduced dependence of thrombin inhibitor dissolution from pH and increased releasing rate from tablet.

17 cl, 3 ex, 3 dwg

FIELD: medicinal industry.

SUBSTANCE: the present innovation deals with manufacturing medicinal preparation containing drotaverin hydrochloride to be applied for interrupting spasms of smooth musculature. Mass for tableting should be prepared due to mixing the powder of drotaverin hydrochloride with that of dyed granulate at the ratio of 1:3 to 2:1. One should obtain the dyed granulate by moisturizing inert pharmaceutical filler with binder's solution dyed with quinoline yellow dyestuff. Then comes drying up to 0.1-2.5% followed by granulation and tableting. The innovation enables to obtain tablets of drotaverin hydrochloride upon industrial equipment at its degradability being below 15 min, being stable during manufacturing and at storage. Quality of tablets meets all the requirements of pharmacopoeic article.

EFFECT: higher efficiency of manufacturing.

2 cl, 4 ex, 3 tbl

FIELD: medicine, hygiene.

SUBSTANCE: the present tablets are designed in solid form and contain the substance of purifying action in the form of finely dispersed insoluble abrasive components, SAS, aromatizing agents, dyestuffs, thickening agents, moreover, the content of water in components should be decreased by 35-37%. The suggested tablets should be prepared due to mixing the components with water to form solid forms out of obtained homogeneous plastic material at the room temperature to be then dried up and packed. Tablets for disposable intake provide great consumer's latitude being very convenient at usage.

EFFECT: higher efficiency of application.

16 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: the suggested composition includes therapeutically efficient quantity of para-aminosalicylic acid (PASA) as an active substance and target additives as sorbitol, polyvinyl pyrrolidone, salt of stearic acid, talc and citric acid. Pharmaceutical composition is designed as tablets covered with a membrane. The latter contains either "Acryl-iz" of Calarcon firm or composition consisting of copolymer of methacrylic acid with ethylacrylate, titanium dioxide, talc, propylene glycol and iron oxide. The suggested PASA-based antitubercular preparation meets all normative requirements of the State Pharmacopoeia, XI publication and has expiry terms of 2 yr.

EFFECT: higher efficiency of application.

6 cl, 3 ex, 1 tbl

The invention relates to the field of pharmaceutical industry and relates to means for treating diseases of the joints
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