Pharmaceutical composition for treating locomotor disorders

FIELD: medicine.

SUBSTANCE: group of inventions refers to a pharmaceutical composition in the form of a soft dosage form for treating locomotor disorders, possessing anti-inflammatory, anaesthetic and anti-oedematous action, containing a combination of heparin sodium salt, dexpanthenol, diethylene glycol monoethyl ether and/or dimethylsulphoxide and target additives. The latter are presented by a gelation agent, a solvent/a solubiliser, a neutraliser, a flavouring agent/a moistening agent and water. The invention also discloses a method for producing the pharmaceutical composition.

EFFECT: reducing side actions, particularly allergic responses; it is characterised by high pharmacological activity, and simplified method for producing.

15 cl, 5 ex, 3 tbl

 

The invention relates to the field of pharmaceutical industry and relates to pharmaceutical compositions in the form of soft medicinal forms, including a combination of heparin sodium salt, dexpantenol, the monoethyl ether of diethylene glycol and/or dimethylsulfoxide and the target additives, which can be used for treatment of edema, hematoma and soft tissue inflammation, swelling and pain and microcirculatory-trophic disorders on the background of chronic venous insufficiency.

The prior art discloses the preparation of the gel of Hepatrombin for the treatment and prevention of pathological lesions of blood vessels and tissues (firm Godecke/Parke-Devis, Germany). The drug in 100 g contains 30000 IU of heparin, 0.25 g of dexpantenol, in addition, it includes a 0.25 g of allantoin and 0.80 mg of oil of turpentine two species of pine. Allantoin partially provides treatment of edema and inflammation. Dexpanthenol is involved in reparative processes of healing of surface vessels and skin. It is known that dexpanthenol goes in the body to Pantothenic acid, which is a constituent of coenzyme A and is involved in more than 70 important enzymatic reactions of metabolism in the body. The disadvantage is the use as a fragrance oil of turpentine two species of pine, as the essential oils of conifers can cause allergies.

Investingactivities of the drug (German patent No. 19536244, IPC AC 9/12, Regenold Juergen, etc.) containing at least one active component on the basis of heparin, its salts and/or its derivative in a concentration of 20000 ME per 100 g of ointment. The drug is intended for topical use, sports injuries, hemorrhages, varicose syndrome, thrombophlebitis, etc. the Disadvantage is the use as the active component only of heparin, whereas the combined drugs have a broader spectrum of action.

We have patent WO 2005063224, priority of 22.12.2004, the patentee Merkle GmbH (Germany), which describes the preparations for external use containing dimethyl sulfoxide and dexpanthenol. Nevertheless, the presence in the aforementioned drug dexpantenol and dimethylsulfoxide does not solve a number of issues related to the treatment of diseases of specified origin: chronic venous insufficiency, thrombophlebitis.

It is also known anticoagulant direct action - drug "Dolobene gel" manufactured by Merkle GmbH, used in the treatment of closed injuries, bruises, acute neuralgia, varicose veins.

"Dolobene" contains heparin sodium - 50000 ME and dexpanthenol - 2.5 g /100 g of gel, and as an amplifier of activity of dimethyl sulfoxide (REFERENCE VIDAL, drugs in Russia: a Handbook. M:Astroparticules, 2004, p. B-411). The preparation also contains various essential oils such as oil of rosemary, oil of mountain pine, citronella oil.

Essential oil of pine is produced from the various parts of an evergreen tree in the family Pinaceae. Note that turpentine pine can cause an allergic reaction, they are poorly tolerated by patients with cardiovascular disorders, Turpin is contraindicated in nephritis. The same actions may have and the medicines containing essential oil of pine.

Rosemary oil is one of the most popular essential oils. Rosemary, also known as Rosmarinus Officinalis, belongs to the family Lamiaceae. Sometimes rosemary oil causes allergic reactions and can lead to vomiting and cramps. Pregnant and breastfeeding women should not use rosemary oil. Elderly people and persons suffering from hypertension, to use rosemary with caution because of possible rise in blood pressure. Be used with caution for sensitive type of skin. Possible photosensitivity, does not apply to the skin in less than 60 minutes before sunbathing, as this may lead to a more intensely colored areas of the skin. These side effects may occur when using products containing essential oil rosm�Rina.

Clear photo toxicity of the essential oils of citrus fruit, obtained by pressing (orange, lemon, citronella). These oils are responsible for the reddening of the skin after application of some colognes (containing the appropriate oil) and further exposure to the sun, which causes fotoohi. These deficiencies can manifest itself in preparations containing essential oil of citronella.

The above-mentioned oils in the composition of the drug significantly increases the cost and complicates the process.

Thus, given the need for effective and safe combination drugs for the treatment of diseases of the musculoskeletal system for local use, still urgent task is the development of the domestic pharmaceutical composition in the form of soft medicinal forms that possess anti-inflammatory, analgesic and anti-edematous effect.

The objective of the proposed complex of the invention is to provide an accessible domestic product for the treatment of diseases of the musculoskeletal system, in the form of a pharmaceutical composition of soft dosage forms containing a combination of heparin sodium salt, dexpantenol, the monoethyl ether of diethylene glycol and/or dimethylsulfoxide, region�gives high therapeutic effect, due to better percutaneous penetration, the absence of allergic reactions, storage stability due to optimum ratio of the components and improving the manufacturing technology.

The technical result is achieved by the fact that experimentally the optimal ratio and possible variations in the composition of the pharmaceutical composition in the form of soft medicinal forms, possessing anti-inflammatory, analgesic and anti-edematous action that contains a good combination of heparin in the form of sodium salt, dexpantenol, the monoethyl ether of diethylene glycol and/or dimethylsulfoxide, and special additives. The pharmaceutical composition preferably performed in the form of gel, as this dosage form is more useful for external application in the treatment of edema, hematoma, soft tissue inflammation, swelling and pain and microcirculatory-trophic disorders on the background of chronic venous insufficiency (varicose veins, acute and chronic thrombophlebitis).

The technical result is also achieved by a method of producing a pharmaceutical composition.

The technical result is also achieved by replacing essential oils of rosemary, mountain pine, citronella lavender oil, this prevents allergic Rea�tion, to reduce the cost of the drug and to simplify the process.

To achieve the technical result of there are several options of pharmaceutical compositions.

Option 1:

Pharmaceutical composition in the form of soft medicinal forms contains a combination of heparin in the form of sodium salt, dexpantenol, the monoethyl ether of diethylene glycol and target additives in the following ratio of ingredients, g/100 g total weight of the composition:

Heparin sodium salt50000-100000 ED
DexpanthenolOf 1.0-10.0
The monoethyl ether of diethylene glycol5,0-30,0
Additives targetTo 100 g

Heparin has anti-inflammatory action, promotes regeneration of connective tissue, exerts antithrombotic effect.

Dexpanthenol, replenishing the reserve endogenous Pantothenic acid, activates metabolic processes, stimulates tissue regeneration and wound healing.

The monoethyl ether of diethylene glycol - modern transcutaneous (percutaneous) conductor, having high conductive properties, provides moserova�ing the delivery of all active substances gel through the skin deep into the tissue, due to its high solubility plays the role of an effective framework for other components of the drug. Also has the property metered release introduced into the tissues of the active substance and their complexes without changing the activity of other components of the drug. His transcutaneous properties above 2.5 times than that of the well-known dimethylsulfoxide and it does not cause allergic reactions.

The use of the monoethyl ether of diethylene glycol in the preparation of the gel system of the present invention provides obvious advantages both from the point of view of physico-chemical characteristics, and from the point of view of the characteristics of the release and absorption of the drug. In particular, the monoethyl ether of diethylene glycol is particularly effectively increases the absorption of active ingredient due to its ability to dissolve the dermal lipid barrier, has film-forming properties and good feeling on the skin gel. Has no peculiar smell.

Option 2:

Pharmaceutical composition in the form of soft medicinal forms contains a combination of heparin in the form of sodium salt, dexpantenol, the monoethyl ether of diethylene glycol, dimethyl sulfoxide and target additives in the following ratio of ingredients, g/100 g total weight of the composition:

Heparin sodium salt50000-100000 ED
Dexpanthenol1,0-10,0
The monoethyl ether of diethylene glycol5,0-30,0
Dimethyl sulfoxide1,0-20,0
Additives targetTo 100 g

Dimethyl sulfoxide, as well as the monoethyl ether of diethylene glycol, has a high conductive properties and promotes better penetration of active substances into the affected tissue. In addition to the above properties of the dimethylsulfoxide has anti-inflammatory, decongestant and local anesthetic action that improves the efficiency of the pharmaceutical composition.

Option 3:

Pharmaceutical composition in the form of soft medicinal forms contains a combination of heparin in the form of sodium salt, dexpantenol, dimethylsulfoxide and target additives in the following ratio of ingredients, g/100 g total weight of the composition:

Heparin sodium salt50000-100000 ED
Dexpanthenol1,0-10,0
Dimethyl sulfoxide1,0-30,0
Additives targetTo 100 g

Replacement of the monoethyl ether of diethylene glycol to dimethyl sulfoxide promotes the expansion of the resource base, in the absence of the monoethyl ether of diethylene glycol can be replaced by dimethylsulfoxide. Also dimethyl sulfoxide improves the quality and efficiency of the composition due to the anti-inflammatory, decongestant and local anesthetic.

The claimed ratio of the components sufficient to provide a therapeutic effect of the drug without side effects such as allergic reactions on the skin, allow to obtain a soft dosage form with good absorbability and spotting ability that increases the effectiveness of the inventive pharmaceutical compositions that remain active for 3 years.

On the basis of normal skin reaction the preferred pH range of pharmaceutical drug is 5.0 to 7.5, more preferably - 5,0-7,0.

As the target additives, the composition preferably includes a gelling agent, solvent/solubilizer, Converter, aromatizer/humidifier and water in the following ratio, g/100 g total weight of the composition:

the gelling agent0,5-3,0
the solvent/solubilizer10,0-45,0
Converter0,1-1,5
aromatizer/humidifier0,1-1,5
waterto 100 g

A method of producing a pharmaceutical composition comprises preparing aqueous-alcoholic gel bases by mixing the gelling agent with water and solvent/solubilizer; an introduction to gel obtained the basis of the monoethyl ether of diethylene glycol and/or dimethylsulfoxide; preparation of the solution dexpantenol and heparin sodium in water and introduction to gel the composition; preparation of the solution of flavoring/humidifier in solvent/solubilizer and an introduction to gel the composition; preparation of the solution of catalyst in the mixture solvent/solubilizer and water and introducing the resulting solution into a gel composition.

As the gelling agent of the inventive pharmaceutical composition contains carbomer, which is marketed under the trade name "CARBOPOL", in particular "CARBOPOL" 934P, 940, 971P and 980, but is not limited to this. Preferably the gelling agent prima�'yat of carbomer brand 940 or 980, who together with the neutralizer provides optimal viscosity and pH of the proposed pharmaceutical composition.

Examples of solvents/solubilization are propylene glycol, ethylene glycol, dimethylacetamide, 1-methyl-2-pyrrolidone, isopropyl alcohol, ethyl alcohol, dimethyl sulfoxide, macrogolglycerol hydroxystearate, diethylene glycol monoethyl ether, and water, preferably a combination of non-aqueous solvent, particularly alcohol and water, but is not limited to this. In the most preferred embodiment, the composition as the non-aqueous solvent/solubilizer used is isopropanol, which is administered in combination with water, as well as macrogolglycerol hydroxystearate. The use of nonaqueous solvents in the preparation of the gel systems of the present invention provides obvious advantages both from the point of view of physico-chemical characteristics, and from the point of view of the characteristics of the release and absorption of active ingredients.

As a neutralizer, you can use sodium bicarbonate, sodium hydroxide, potassium hydroxide, triethanolamine or trometamol, but is not limited to this. Preferably as a neutralizer application of trometamol, as this ensures the storage stability during the shelf life (3 years).

As aroma�of'izator/humidifier use lavender oil. Lavender essential oil is one of the most common, since lavender is grown almost everywhere. The advantage of lavender essential oil in that it has a wide range of useful actions, and can be used to care for almost any skin type. For example, it copes well with a variety of irritable and inflammatory processes on the skin, eliminates redness, peeling and itching that can successfully be used in the care of hypersensitive skin prone to allergies, and reacts negatively to many cosmetic products and procedures. The use of lavender oil in teenagers and even the use of lavender essential oil for children does not lead to serious consequences or side effects, as lavender oil is non-toxic. In addition to the above properties, lavender oil moisturizes and nourishes the skin, improving its circulation and relieves various irritation and inflammation.

In the most preferred embodiment of the invention the pharmaceutical composition contains carbomer as a gelling agent, a solution of isopropyl alcohol and water, and macrogolglycerol hydroxystearate as a solvent/solubilizer, trometamol as a neutralizer, oil of lavender as a flavoring/moisturizer. There are several options.�s (the ratio of ingredients, g/100 g total weight of the composition).

Option 1:

Heparin sodium salt50000-100000 ED
Dexpanthenol1,0-10,0
The monoethyl ether of diethylene glycol5,0-30,0
Carbomer0,5-3,0
Isopropyl alcohol9,5-43,0
Macrogolglycerol hydroxystearate0,5-2,0
Trometamol0,1-1,5
Lavender0,1-1,5
WaterTo 100 g

Option 2:

Heparin sodium salt50000-100000 ED
Dexpanthenol1,0-10,0
The monoethyl ether of diethylene glycol5,0-30,0
Dimethyl sulfoxide1,0-20,0
Carbomer 0,5-3,0
Isopropyl alcohol9,5-43,0
Macrogolglycerol hydroxystearate0,5-2,0
Trometamol0,1-1,5
Lavender0,1-1,5
WaterTo 100 g

Option 3:

Heparin sodium salt50000-100000 ED
Dexpanthenol1,0-10,0
Dimethyl sulfoxide1,0-30,0
Carbomer0,5-3,0
Isopropyl alcohol9,5-43,0
Macrogolglycerol hydroxystearate0,5-2,0
Trometamol0,1-1,5
Lavender0,1-1,5
WaterTo 100 g

A method of obtaining a pharmaceutical composition in the reactor homogenizer No. 1 load water and and�profilemy alcohol, with the help of a vacuum pre-load suspended carbomer, stirred to obtain a homogeneous gel bases at a speed of homogenization 1500 Rev/min, gradually increasing to 6000 Rev/min; then to the reactor homogenizer No. 1 administered pre-weighed amount of monoethyl ether of diethylene glycol and/or dimethyl sulfoxide, mix thoroughly; with reactor No. 2 is charged with dexpanthenol, add an equal amount of water, stirred to obtain a homogeneous solution, then added heparin sodium salt; in reactor No. 3 load a pre-weighed amount of macrogolglycerol of hydroxystearate and pre-weighed amount of lavender oil, mix until dissolved; separately, a solution of trometamol in the remaining amount of water and isopropyl alcohol; then to the reactor homogenizer №1 with stirring, the contents of reactor No. 2; then under stirring was added in portions a solution of reactor No. 3, and a separately prepared solution of trometamol; mixing is performed under vacuum until a homogeneous mixture and the resulting gel is Packed in tubes.

The following examples illustrate the invention and are merely illustrative but not restrictive.

Example 1.

Composition / 100 g

Heparin sodium 50000 IU
Dexpanthenol2.5 g
The monoethyl ether of diethylene glycol25,0 g
Carbomer1.0 g
Isopropyl alcohol30,0 g
Macrogolglycerol hydroxystearate1.5 g
Trometamol0.5 g
Lavender oil1.0 g
Purified waterTo 100 g

Example 2.

Composition / 100 g

Heparin sodium75000 IU
Dexpanthenol3.0 g
The monoethyl ether of diethylene glycol5.0 g
Dimethyl sulfoxide10.0 g
Carbomer2.0 g
Isopropyl alcohol43,0 g
Macrogolglycerol GI�oxystearate 0.5 g
Trometamol1.0 g
Lavender oil0.3 g
Purified waterTo 100 g

Example 3.

Amounting to 100 g.

Heparin sodium100,000 IU
Dexpanthenol5.0 g
The monoethyl ether of diethylene glycol30,0 g
Carbomer1.5 g
Ethanol30,0 g
Macrogolglycerol hydroxystearate2.0 g
Trometamol1.3 g
Lavender oil1.5 g
Purified waterTo 100 g

Example 4.

Composition / 100 g

Heparin sodium50000 IU
Dexpanthenol2,5 �
Dimethyl sulfoxide15.0 g
Carbomer1.3 g
Isopropyl alcohol35.0 g
Macrogolglycerol hydroxystearate1.0 g
Trometamol0.3 g
Lavender oil0.5 g
Purified waterTo 100 g

Example 5.

Composition / 100 g

Heparin sodium50000 IU
Dexpanthenol1.5 g
Dimethyl sulfoxide15.0 g
Carbomer2.5 g
Ethanol34,0 g
Macrogolglycerol hydroxystearate1.0 g
Trometamol1.5 g
Lavender oil0.5 g
Propylene glycol10.0 g
Purified waterTo 100 g

The results of the combined gel for external use of examples 1, 2, 3 are presented in table 1, 2, 3, respectively.

-”-
Table 1
The results of the pharmaceutical compositions according to example 1
The date of production and numberDescriptionAuthenticitypH of 5.0 to 7.0The homogeneity. Should be homogeneousMicrobiological purity. Category 2Quantification in 1 gShelf lifeConclusions storage
Clear, colorless gel with the scent of lavender.Heparin sodium. After 30 min plasma should not coagulateDexpanthenol. The retention time of the main peak at chromatopelma the test solutions should suitable�VAT retention time of the main peak of dexpantenol on chromatopelma solution WITH Heparin sodium from 450 UNITS to 550 UNITSDexpanthenol from 0,0225 g to 0,0275 g
1234567891011
S. 10610Transparent bezumnyy gel with the smell of lavenderPositivePositive5,49The party.The party.503,50,0258-Fit
The sameThe sameThe same5,44The sameThe sameTo 502.10,02531 yearFit
-”--”--”-5,39-”-499,50,02502 yearsFit
-”--”--”-Of 5.32-”--”-489,90,02493 yearsFit
S. 20610Clear, colorless gel with the smell of lavenderPositivePositive5,61The party.The party.538,00,0237-Fit
The sameThe sameThe sameTo 5.62TooToo536,40,02341 yearFit
-”--”- 5,57-”--”-532,80,02322 yearsFit
-”--”--”-5,51-”--”-527,90,02303 yearsFit
S. 30610Transparent bezumnyy gel with the smell of lavenderPositivePositive5,34The party.The party.469,50,0251-Fit
The sameThe sameThe sameOf 5.32The sameThe same465,30,02471 yearFit
-”--”-5,30-”--”-462,40,02492 yearsFit
-”--”--”-5,28-”--”-458,90,02453 yearsFit

The same
Table 3
The results of the pharmaceutical composition of example 3
Series numberDescriptionAuthenticitypH of 5.0 to 7.0The homogeneity. Should be homogeneousMicrobiological purity. Category 2Quantification in 1 gShelf lifeIn�water storage
Clear, colorless gel with the smell of lavenderHeparin sodium. After 30 min plasma should not coagulateDexpanthenol. The retention time of the principal peak in the chromatogram of the test solution should correspond to the retention time of the main peak of dexpantenol on the chromatogram of the solution WITHHeparin sodium from AD to 850 IUDexpanthenol from or 0.045 to 0.055 g g
1234567891011
C. 10810Transparent bezumnyy gel with the smell of lavenderPositivePositiveThe 5.25The party.The party.990,50,0541-Fit
The sameThe same5,21The sameThe same989,20,05361 yearFit
-”--”--”-5,19-”--”-985,40,05392 yearsFit
-”--”--”-5,20-”--”-972,50,05303 yearsFit
p 20810Transparent bezumnyy gel with the smell of lavenderPositivePositive5,43The party.The party.1008,40,0526-Fit
We �e The sameThe same5,42The sameThe same1003,50,05191 yearFit
-”--”--”-Levels lower than the 5.37-”--”-997,60,05202 yearsFit
-”--”--”-5,35-”--”-994,00,05133 yearsFit
S. 30810Clear, colorless gel with the smell of lavenderPositivePositive5,10Sothwest.The party.1044,80,0478- Fit
The sameThe sameThe same5,07The sameThe same1039,40,04801 yearFit
-”--”--”-5,04-”--”-1032,50,04672 yearsFit
-”--”--”-Of 5.02-”--”-1030,10,04653 yearsFit

Sources of information

1. Mashkovsky M. D. Medicines. - 15th ed., Rev., Rev. and extra - M.: OOO "Publishing house New wave", 2005. - 1200 p.: ill.

2. Guide The Pharmaceutical Industry. - 2-e Izd., EXT., - P. S.: CJSC "Pharmaceutical publishing house "Faros Plus", 1997. - 752 p.

3. Drugs of foreign firms in Russia. Guide. - M.: "Astrafarm�Ellis", 1993. - 717 p.

4. On The Main Page. Drugs in Russia: a Handbook. - M.: Astroparticules, 2004

5. The state register of medicines http://grls.rosminzdrav.ru/

6. RLS. Encyclopedia of drugs, 12th ed., M.: OOO "radar-2005", 2004.

7. Heparin: physiology, biochemistry, pharmacology and clinical application. Markosyan, A. A., Academy of Sciences of the USSR, etc. - Nauka, Leningrad. DEP.-tion, 1969 - 214.

8. The German patent No. 19536244, IPC AC 9/12, Regenold Juergen and others.

9. Patent WO 2005063224, the patentee Merkle GmbH (Germany).

1. Pharmaceutical composition in the form of soft medicinal forms, possessing anti-inflammatory, analgesic and anti-edematous action, containing a combination of heparin sodium salt and dexpantenol, characterized in that it further comprises the monoethyl ether of diethylene glycol and the target additive in the following ratio of ingredients, g/100 g total weight of the composition:

Heparin sodium salt50000-100000 ED
Dexpanthenol1,0-10,0
The monoethyl ether of diethylene glycol5,0-30,0
Additives targetTo 100 g

2. Pharmaceutical�I composition in the form of soft medicinal forms, possessing anti-inflammatory, analgesic and anti-edematous action, containing a combination of heparin sodium salt and dexpantenol, characterized in that it further comprises the monoethyl ether of diethylene glycol, dimethyl sulfoxide and the target additive in the following ratio of ingredients, g/100 g total weight of the composition:

Heparin sodium salt50000-100000 ED
Dexpanthenol1,0-10,0
The monoethyl ether of diethylene glycol5,0-30,0
Dimethyl sulfoxide1,0-20,0
Additives targetTo 100 g

3. Pharmaceutical composition according to claim 1 or 2, which is made in the form of a gel.

4. Pharmaceutical composition according to claim 3, which contains as special additives gelling agent, solvent/solubilizer, Converter, aromatizer/humidifier and water in the following ratio of ingredients, g/100 g total weight of the composition:

The gelling agent0,5-3,0
Dissolve�ü/solubilizer 10,0-45,0
Converter0,1-1,5
Aromatizer/humidifier0,1-1,5
WaterTo 100 g

5. Pharmaceutical composition according to claim 4, which contains as a gelling agent of carbomer.

6. Pharmaceutical composition according to claim 4, which contains as solvent/solubilizer solution of alcohol and water, and macrogolglycerol hydroxystearate.

7. Pharmaceutical composition according to claim 4, which contains as a neutralizer trometamol.

8. Pharmaceutical composition according to claim 4, which contains as an aromatizer/humidifier lavender oil.

9. Pharmaceutical composition according to claim 1 or 4, which contains carbomer as a gelling agent, isopropyl alcohol and macrogolglycerol hydroxystearate as a solvent/solubilizer, trometamol as a neutralizer, oil of lavender as a flavoring/humidifier and water in the following ratio of ingredients, g/100 g total weight of the composition:

The monoethyl ether of diethylene glycol
Heparin sodium salt50000-100000 ED
Dexpanthenol1,0-10,0
5,0-30,0
Carbomer0,5-3,0
Isopropyl alcohol9,5-43,0
Macrogolglycerol hydroxystearate0,5-2,0
Trometamol0,1-1,5
Lavender0,1-1,5
WaterTo 100 g

10. Pharmaceutical composition according to claim 2 or 4, which contains carbomer as a gelling agent, isopropyl alcohol and macrogolglycerol hydroxystearate as a solvent/solubilizer, trometamol as a neutralizer, oil of lavender as a flavoring/humidifier and water in the following ratio of ingredients, g/100 g total weight of the composition:

Heparin sodium salt50000-100000 ED
Dexpanthenol1,0-10,0
The monoethyl ether of diethylene glycol5,0-30,0
Dimethyl sulfoxide1,0-20,0
Carbomer0,5-3,0
Isopropyl alcohol9,5-43,0
Macrogolglycerol hydroxystearate0,5-2,0
Trometamol0,1-1,5
Lavender0,1-1,5
WaterTo 100 g

11. Pharmaceutical composition in the form of soft medicinal forms, possessing anti-inflammatory, analgesic and anti-edematous action, containing a combination of heparin sodium salt and dexpantenol, characterized in that it additionally contains dimethyl sulfoxide and target additives: carbomer as a gelling agent, isopropyl alcohol and macrogolglycerol hydroxystearate as a solvent/solubilizer, trometamol as a neutralizer, oil of lavender as a flavoring/humidifier and water in the following ratio of ingredients, g/100 g total weight of the composition:

Heparin sodium salt50000-100000 ED
Dexpanthenol1,0-10,0
Dimethyl sulfoxide 1,0-30,0
Gelling agent - carbomer0,5-3,0
The solvent/solubilizer - isopropyl alcohol9,5-43,0
and macrogolglycerol hydroxystearate0,5-2,0
Neutralizer - trometamol0,1-1,5
Aromatizer/humidifier - lavender0,1-1,5
WaterTo 100 g

12. Pharmaceutical composition according to claim 11, with the following ratio of ingredients, g/100 g total weight of the composition:

Heparin sodium salt50000 IU
Dexpanthenol2.5 g
Dimethyl sulfoxide15.0 g
Carbomer1.3 g
Isopropyl alcohol35.0 g
Macrogolglycerol hydroxystearate1.0 g
Trometamol0.3 g
Lavender oil0.5 g
Purified waterTo 100 g

13. Pharmaceutical composition according to claims. 1, 2 or 11, which has a pH of 5.0 to 7.5.

14. A method of obtaining a pharmaceutical composition according to claims. 1, or 2, or 11, picture comprising preparing a hydroalcoholic gel bases by mixing the gelling agent with water and solvent/solubilizer; an introduction to gel obtained the basis of the monoethyl ether of diethylene glycol and/or dimethylsulfoxide; preparation of the solution dexpantenol and heparin sodium in water and introduction to gel the composition; preparation of the solution of flavoring/humidifier in solvent/solubilizer and an introduction to gel the composition; preparation of the solution of catalyst in the mixture solvent/solubilizer and water and introducing the resulting solution into a gel composition.

15. A method of obtaining a pharmaceutical composition according to claims. 1, 2 or 11, characterized in that in the reactor homogenizer No. 1 load water and isopropyl alcohol, using a vacuum pre-load suspended carbomer, stirred to obtain a homogeneous gel bases at a speed of homogenization 1500 Rev/min, gradually increasing to 6000 Rev/min; then to the reactor homogenizer No. 1 administered before�till then weighed the amount of monoethyl ether of diethylene glycol and/or dimethylsulfoxide, mix thoroughly; in reactor No. 2 is charged with dexpanthenol, add an equal amount of water, stirred to obtain a homogeneous solution, then added heparin sodium salt; in reactor No. 3 load a pre-weighed amount of macrogolglycerol of hydroxystearate and pre-weighed amount of lavender oil, mix until dissolved; separately, a solution of trometamol in water and isopropyl alcohol; then to the reactor homogenizer №1 with stirring, the contents of reactor # 2: then under stirring was added in portions a solution of reactor No. 3, and a separately prepared solution of trometamol; mixing is performed under vacuum until a homogeneous mixture and the resulting gel is Packed in tubes.



 

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FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine, namely to orthopaedics, and can be used for producing a transplant for long bone tissue repair. That is ensured by collecting bone marrow aspirate into lithium heparin test tubes, diluting with phosphate salt buffer, filtered through a filter with pore size 70 mcm and centrifuging for 10 min at 400 g. That is followed by inoculating flasks 150 cm2 with the produced mesenchymal stem cells (MSCs) at 1×106 cells/cm2, culturing at temperature 37°C and 5% CO2 in air, in the Dulbecco's Modified Eagle's medium containing glucose 1 g/l and less, with 10% embryo calve serum. The medium is changed every 3 days. Before preparing the transplant, the cells are removed from the substrate with 0.05% trypsin EDTA, washed and re-suspended. The cell suspension is applied on the matrix, incubated for 3 hours at temperature 37°C with rocking in a rotation shaker at 25 rpm. The matrix is filled with the DMEM medium with 10% bovine foetal serum, dexamethasone 10-7 M, β-glycerophosphate 10 mM, ascorbate-2-phosphate 0.05 mM, 1% streptomycin 100 mcg/ml or penicillin 100 units/ml. The MSCs are cultured for 28 days. What is also presented is a method for long bone tissue repair.

EFFECT: group of inventions provides the uniform bone tissue repair in replacing the bone tissue defect of critical size with the transplant.

3 cl, 2 tbl, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a controlled-release preparative form of diacerein administered once a day for treating or autoimmune diseases or their complications. The preparative form contains a core, an active layer, a sustained-release film layer and a delayed-release film layer, wherein the active layer is followed by the sustained-release film, and the delayed-release film layer thereafter. The sustained-release film layer contains ethyl cellulose polymer, povidone, triethylacetate and talc; the delayed-release film layer contains Eudragit polymer, triethylacetate and talc.

EFFECT: reducing the negative side action of diacerein.

18 cl, 23 ex, 33 tbl

FIELD: medicine.

SUBSTANCE: non-invasive treatment of Dupuytren's contracture of degree III-IV is ensured by injecting Collalysin dissolved in 2% Novocaine into a subcutaneous fold or nodes in a projection of fetlock, proximal digital joints and/or into a fold base; 24 hours later, the fold is separated from the skin subcutaneously; the skin is mobilised, and the involved finger (fingers) are redressed.

EFFECT: invention enables the non-invasion recovery of the complete motion function of the fingers.

4 dwg, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of biochemistry, in particular to single variable domain, aimed against IL-6R, to polypeptide and construction, directed against IL-6R, containing said single variable domain, as well as to methods of obtaining them. Disclosed are nucleic acids, coding said single variable domain, polypeptide and construction, as well as genetic constructions, containing said nucleic acids. Described are host cells and host organisms, containing said nucleic acids. Invention also deals with composition for blocking interaction of IL-6/IL-6R, containing effective quantity of described single variable domain, polypeptide, construction, nucleic acid or genetic construction. Also disclosed is method of prevention and/or treatment of at least one of diseases or disorders, associated with IL-6, IL-6R, complex IL-6/IL-6R and/or signal pathways, in which IL-6, IL-6R or complex IL-6/IL-6R is involved and/or biological functions and reactions, win which IL-6, IL-6R or complex IL-6/IL-6R takes part with application of described single variable domain, polypeptide, construction or composition.

EFFECT: invention makes it possible to block interaction of IL-6/IL-6R effectively with increased affinity and biological activity.

25 cl, 70 dwg, 56 tbl, 61 ex

FIELD: medicine.

SUBSTANCE: method for integrated treatment of hip diseases accompanying a total replacement involves a postoperative background therapy with using an infusion therapy, an antibiotic therapy, an anticoagulant therapy, therapeutic exercises and a physical therapy; aqueous herbal tea containing willow bark, common St.-John's wort herb, balm lemon herb, liquorice root, meadowsweet herb, mountain ash fruit, raspberry leaves taken in certain proportions 14 days before the operation and for three postoperative months in a dose of 0.5 glass 4 times a day half an hour before a meal.

EFFECT: method enables providing the higher effectiveness of the surgical management of hip diseases by improving patient's rehabilitation, promotes reducing trait and state anxieties, a rate of administration of analgesic preparations, improving the motor function of limbs and preventing postoperative complications.

1 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, particularly to a composition possessing anti-inflammatory properties. The composition with the anti-inflammatory properties comprising a herbal extract prepared by extracting rose hip shells or rose hip shells and kernels in water or a mixture of water and ethanol followed by purifying and drying together with collagen hydrolysate. A method for preparing the composition. The composition with the anti-inflammatory properties. Using the composition for preparing a therapeutic agent or a biologically active food supplement or a balanced diet for preventing or for relieving symptoms accompanying joint complaints. The therapeutic agent with the anti-inflammatory properties containing the composition. The biologically active food supplement with the anti-inflammatory properties containing the composition. The balanced dietary product with the anti-inflammatory properties containing the composition.

EFFECT: agents possess the evident anti-inflammatory properties.

10 cl, 13 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to traumatology and orthopaedics, and aims at conservative treatment of plantar fasciitis. That is ensured by administering platelet rich autoplasma in an amount of 2.0 ml for each injection into an attachment point of the plantar aponeurosis to the calcaneum (the heel sac), inner and outer side surfaces of a midfoot, as well as to a plantar surface of the midfoot. The autoplasma is prepared 1-2 hours before the procedure, and it contains from 1243 thousand/mcl to 3029 thousand/mcl platelets. The normal autoplasma contains from 162 thousand/mcl to 358 thousand/mcl platelets. The autoplasma is activated with 0.25% CaCl2 in a ratio of 2:1 with added 5% sodium hydrocarbonate in a ratio of 1:20 to the prepared platelet rich plasma.

EFFECT: above method enables providing pain management, recovering the extremity function, ensuring the stable clinical effect, and preventing complications.

2 ex

FIELD: medicine.

SUBSTANCE: group of inventions deals with medical prostheses for implantation into a human organism and methods of their manufacturing, in particular prosthesis of the jaw bone, which can be used in cosmetic surgery of the jaw bone or in the jaw bone reconstruction. Claimed is an implant of the jaw bone, manufactured in accordance with the method, including the following stages: selection of material of animal origin from an organism of cattle or pigs, with the material of animal origin being the jaw bone; shaping the material of animal origin to obtain a desirable shape of the jaw bone implant; removal of cells from the material of animal origin, crosslinking of the material of animal origin; removal of antigens from the material of animal origin; subjection of the material of animal origin to alkaline processing; introduction of active substances, improving adhesion on the implant of the growth factor and stem cells, produced by the human organism into the material of animal origin; packing the material of animal origin into a container with a sterilising solution. The jaw bone implant, manufactured by the said method, possesses high tissue compatibility.

EFFECT: group of inventions provides elimination of development or, at last, minimisation of phenomena of various types of discomfort under an impact of moving muscles in the period of the implant growing into tissues of the host organism, resorption and replacement with the new bone tissue with simultaneous provision of high tissue compatibility with elimination, or, at least, minimisation of phenomena of immunological rejection of a biological prosthesis of the jaw bone.

14 cl, 1 ex, 4 dwg

FIELD: medicine.

SUBSTANCE: pharmaceutical composition possessing a therapeutic action on various skin pathologies contains triptantrin, chitosan and distilled water, a lanoline and Vaseline mixture and protein-nucleic hydrolyzate of the salmonid fishes milt in a certain mixture ratio.

EFFECT: composition enables increasing the clinical effectiveness in the skin pathologies of various origins and extending the range of pharmaceutical compositions having the therapeutic effect on the various skin pathologies.

3 tbl, 4 dwg, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry, namely to production of medications for treating dermatosis. Medication according to invention, made in form of cream, contains mometasone furoate, preservative, hydrophilic no-aqueous solvent, emulsifying agent of 1st kind, emulsifying agent of 2nd kind, emollient, disodium edetate (trilon B), pH-regulating agent, and purified water in quantities, given in invention formula.

EFFECT: invention can be applied for treating inflammatory diseases and itching in case of dermatosis, yielding to glycocorticosteroid therapy.

9 cl, 3 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: pharmaceutical composition contains drug substances and a consistency-forming base. According to the invention, it contains anaesthetics as drug substances specified in a group: anaesthesine, lidocaine, promedol and antiseptic specified in a group of: ethacridine lactate, Furacilin, dioxidine, chlorhexidine, boric acid, 0.5% silver solution in the following ratio, g in 1 ml of the mixture: anaesthetics 0.00001-0.5; antiseptics 0.00001-0.5; consistency-forming base - the rest. Besides, it contains lysozyme in an amount of 0.1-0.3 g per 1 ml of the mixture, alpha-lipoic acid as an antioxidant in an amount of 0.00001-0.5 g per 1 ml of the mixture, regenerants specified in a group of: pantothenic acid, calcium pantotenate, beta-carotene, coenzyme Q, sodium deoxyribonucleate, inosine, vitamins A, D, E, K in an amount of 0.00001-0.5 g per 1 ml of the mixture, anabolics specified in a group of: methyluracil, riboxinum, potassium orotate, orotic acid, L-carnitine in an amount of 0.00001-0.5 g per 1 ml of the mixture, glycyrrhizic acid and/or its salts in an amount of 0.00001-0.5 g per 1 ml of the mixture, recombinant interferon specified in a group of: recombinant interferon-alpha, recombinant interferon-beta, recombinant interferon-gamma in an amount of 100-1,000,000 International units, glucocorticoids specified in a group of: hydrocortisone, prenisolone, polcortolone in an amount of 0.00001-0.5 g per 1 ml of the mixture. The consistency-forming base contains the components specified in a group: hypromellose, sodium alginate, acetyl phthalyl cellulose, macrogol, polyvinylpyrrolidone.

EFFECT: improving the properties of the composition.

9 cl, 11 ex

FIELD: medicine.

SUBSTANCE: what is described is a bioactive wound coating of a hydrogel nanocomposite, which contains antimicrobial and antioxidant ingredients: silver-modified montmorillonite and fullerenol used to optimise the clinical course of the wound process, to prevent and suppress a wound infection. The wound coating can be used to treat gun-shot injuries, severe mechanical injuries, infected and uninfected wounds, including septic and persistent, granulating wounds following deep thermal, chemical and radioactive burns, in the combined therapy of trophic ulcers and bed sores at hospital, in the outpatient setting and in the field. The wound coating is elastic, not fragmented in dressing that facilitates wound care. A high sorption ability of the wound coating matrix, including of coarse-molecular ingredients of the wound effluent, provides the fast elimination of the wound bed. Using the hydrogel, i.e. possessing high degree of hydration, the wound coating meets the modern wound management in the humid medium.

EFFECT: optimum conditions for the early activation of the repair processes.

5 dwg, 2 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compositions for local application for the prevention and treatment of local eye pathologies, in particular inflammatory keratites and conjunctivitis and the dry eye syndrome, which contain as active ingredients polyunsaturated fatty acids of the omega-3 and omega-6 type, namely, EPA (eicosapentaenoic acid), DHA (docosahexaenoic acid) and GLA (γ-linolenic acid), mixed with vitamin E acetate and combined into a stable composition in a hydrogel, that is in the disperse form in a water solution, containing one or more gel-forming polymers. The claimed compositions are especially recommended for application as artificial tears.

EFFECT: invention provides an increased efficiency of the prevention and treatment of eye pathologies.

15 cl, 15 tbl, 3 dwg, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, more specifically to a composition for treating dermatologic diseases, preferentially skin itching. The composition causes antiallergic action and is used in treating allergic reactions (rash, urticaria), insect bites, ultraviolet erythema and skin burns. The pharmaceutical composition contains azelastine hydrochloride and benzocaine as active substances, and a hydrophobic ingredient, a hydrophilic ingredient, an emulsifying agent and a pH corrective agent as additive agents. As the pH corrective agent, the composition contains preferentially succinic acid. The pharmaceutical composition is presented as a soft dosage form, preferentially in the form of a cream.

EFFECT: composition according to the invention is characterised by high pharmacologic activity, good package extrusion, and storage-stability.

9 cl, 1 tbl, 14 ex

FIELD: medicine.

SUBSTANCE: therapeutic agent contains carboxymethyl cellulose sodium salt as a base and a combination of antiseptic, 0.01% Myramistinum and metronidazole as therapeutic ingredients. The invention provides preparing the therapeutic agent possessing the antiseptic, wound-healing and sorption action on local pyoinflammatory processes in soft tissues and mucous membranes, used in surgery, dermatology, obstetrics and gynaecology, otorhinolaryngology.

EFFECT: agent possesses the higher efficacy.

2 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: therapeutic agent contains an alloy of polyethylene oxide of molecular weight 400 and 1500 as a base and comprises a combination of antiseptic, benzalkonium chloride and metronidazole as therapeutic ingredients. The invention provides preparing the therapeutic agent possessing the antimicrobial, sorption and wound-healing action on local pyoinflammatory processes in soft tissues and mucous membranes, used in surgery, dermatology, obstetrics and gynaecology, otorhinolaryngology.

EFFECT: agent possesses the higher efficacy.

2 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: first, the method involves teeth cleaning, surgical site isolation with cotton swabs, drug-induced treatment of 2% chlorhexidine and drying. Then, an erosion surface and adjoining solid dental tissues are coated with a phytoapipreparation for 15-20 minutes. The preparation is presented in the form of an ointment and has the following composition, weight fractions: 40% alcoholate (1:10) of tartarian catchfly or rhizomes and roots of maral root 10 ml, 40% alcoholate (1:10) of spirea herb 5 ml, apilac 0.5 g, clove ester 0.5 ml, lanolin 25.2 g, Vaselin 58.8 g. The ointment is used once a day for 10 days with the patients advised to avoid eating for one hour.

EFFECT: method is easy-to-use and physiological, and ensures an absolute recovery.

2 ex

FIELD: medicine.

SUBSTANCE: pharmacological composition contains a therapeutic agent and a pharmaceutically acceptable base. As a therapeutic agent, it contains recombinant interferon specified in a group: recombinant interferon alpha, recombinant interferon beta, recombinant interferon gamma, as well as hypromellose, boric acid as an antiseptic, anesthesin or lidocaine as local anaesthetics in the following proportions, g per 1 ml of the mixture: recombinant interferon, IU 100-10,000,000, hypromellose 0.00001-0.5, boric acid 0.00001-0.5, anesthesin or lidocaine 0.00001-0.5, a pharmaceutically acceptable base - the rest. Besides, the pharmaceutical composition contains heparin in an amount of 0.00001-0.5 g; antibiotics specified in a group of: baneocin, levomycin, tetracycline, amoxicilline in an amount of 0.00001-0.5 g. And as a pharmaceutically acceptable base, the pharmaceutical composition contains macrogol 400, or macrogol 1500, or macrogol 4000.

EFFECT: more effective treatment.

4 cl, 9 ex

FIELD: chemistry.

SUBSTANCE: invention relates to chemistry and presents a conjugation product, comprising polysaccharides T1 and T2, where the monosaccharides which form the polysaccharides T1 and T2 are bonded to each other by alpha-1,4-glycosidic links. At least one of the polysaccharides T1 and/or T2 comprises at least one amino group. T1 and T2 are bonded to each other covalently by a linker. T1 and/or T2 carry m groups -(L-A), wherein A is glucosaminoglycan or a derivative of glucosaminoglycan, glucosaminoglycan or a derivative of glucosaminoglycan with fluorescence labels, L is a second linker, by which T1 and/or T2 are covalently bonded to A, and m is at least 1.

EFFECT: invention also relates to a pharmaceutical composition, comprising a bonded product; use of the product in medicine and cosmetology and to the method of preparation of the bonded product.

22 cl, 5 ex

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