Pharmaceutical composition in the form of a soluble effervescent tablets and how you can get

 

(57) Abstract:

The invention relates to chemical-pharmaceutical industry, namely soluble effervescent tablets for oral administration and to the way they are received. The invention lies in the fact that the pharmaceutical composition contains as a frame material dextrose anhydride, which leads to the fact that the pharmaceutical composition can be obtained in the form of tablets by direct pressing. The use of polyethylene glycol as a binder allows you to get face white pills with a good surface. The presence of various therapeutic agents, biologically active substances, vitamins, macro - and microelements extends the range of pharmacological activity, pharmaceutical compositions, resulting in expansion of the range. In a method of producing a pharmaceutical composition in the form of a soluble effervescent tablets all transactions are conducted at low absolute humidity in the range of 5-30%, and the tabletting operation carried out by the method of direct extrusion under pressure TC 3-10. The invention provides improved stability soluble effervescent tablets, extends spei 14 C.p. f-crystals.

The invention relates to chemical-pharmaceutical industry, namely soluble effervescent tablets for oral administration and to the way they are received.

It is known that at the present time one of the most popular pharmaceutical forms for introduction into the body of medicines, biologically active compounds, vitamins and minerals is the so-called soluble effervescent tablet.

From literature it is known that most effervescent tablets contains a therapeutic agent, a biologically active substance, the main component of sipacate, the acid component of sipacate, frame material, the binder components and the filler.

Moreover, the methods of obtaining effervescent tablets based on common techniques: granulation, drying, grinding, pelleting.

It is known complex of the invention in the Pharmaceutical composition in the form of effervescent tablets and method of reception" (see the patent of the Russian Federation 2043099, class a 61 K 9/20, And 61 To 31/60, And 61 To 47/12, the filing date 31.01.1994,, date of publication 10.09.1995 year).

Pharmaceutical composition in the form of effervescent tablets contains acetylsalicylic acid and gas-forming mixture consisting of saloon is, localseo sodium digitaltruth in the amount of 50-60% by weight of the tablet and nutrifaster in the amount of 15% by weight of the tablet, with the following ratio of components was:

Acetylsalicylic acid - 0,05-0,5

Sodium bicarbonate - 0,5-1,5

Sodium digitaltruth - 0,8-1,5

Sodium phosphate dihydrate - 0,01-0,1

The pharmaceutical composition have a number of significant drawbacks.

To the composition of the known pharmaceutical compositions entered nutrifaster, which are not essential for human and therefore not included in the list of substances allowed for use in pills as an auxiliary (State of Phamacopeia XI, vol. 2, T. 1, S. 155). In addition, nutrifaster, has a toxic effect, which in turn leads to the fact that renowned pharmaceutical composition can adversely affect the vital functions of the body.

Known soluble effervescent pharmaceutical composition, selected as a prototype (see the patent of the Russian Federation 2155033, class a 61 K 9/20, a 61 K 35/78, And 61 To 31/616, the filing date 18.11.1999,, date of publication, 27.08.2000) containing therapeutic agent in combination with a biologically active homestarrunner.

The main disadvantage of soluble effervescent pharmaceutical compositions is that the medicinal composition of the resulting "wet" method, i.e. the method of granulation.

Known effervescent tablet or pellet and method of their preparation, selected as a prototype (see the patent of the Russian Federation 2143891, class a 61 K 9/46, And 61 To 31/714 And 61 To 33/34, And 61 To 31/714 And 61 To 31/375, a 61 K 31/44, And 61 To 31/51, And 61 To 31/525, a 61 K 31/59, And 61 To 33/34, And 61 To 31/07 And 61 To 33/26, And 61 To 33/30, And 61 To 33/32, A 61 K 33/06 the filing date 10.03.1994,, date of publication 10.01.2000,), containing frame material, the main component of sipacate, the acid component of sipacate, connecting components, filler, vitamins, macro - and microelements.

The main disadvantage of this soluble effervescent pharmaceutical composition is that it received a "wet" method, i.e. the method of granulation.

The known method, selected as a prototype (see the patent of the Russian Federation 2043099, class a 61 K 9/20, And 61 To 31/60, And 61 To 47/12, the filing date 31.01.1994,, date of publication 10.09.1995 year).

A method of obtaining a pharmaceutical composition in the form of a soluble effervescent tablets includes grinding, granulation, sieving, mixing the Oia acid and alkaline components, moreover, the components are pre-ground to a particle size not exceeding 50 μm, the obtained granules are dried and sieved to particle size of 1200 μm, followed by mixing granulates, dusting sliding agent and pelletizing.

A method of obtaining a pharmaceutical composition in the form of a soluble effervescent tablets has some significant drawbacks. The presence of intermediate operations, such as separate granulation acid and alkaline components, drying, re-grinding, increase the duration and complexity of the technological cycle, which leads to high energy costs, increasing the cost of the composition.

From literature it is known that effervescent tablets currently produce "wet" method, though the method of direct compression is preferable.

The purpose of this complex of the invention is to remedy these disadvantages, that is,

- expanding the range of pharmacological activity;

- increase the yield of the finished product while reducing cost by simplifying the process and reducing energy consumption.

- improved stability effervescent the Oia in the form of a soluble effervescent tablets containing therapeutic agent in combination with a biologically active material, the main component of sipacate, the acid component of sipacate, frame material, the binder components and the filler according to the invention the pharmaceutical composition as a frame material contains dextrose anhydride in the following ratio, wt.%:

Therapeutic agent - 1-15

Biologically active substance - 5-13

The main component of sipacate - 10-40

The acid component of sipacate - 20-38

Dextrose ashith - 10-30

Connecting components - 1-2

The filler is 0.5 - 5

This pharmaceutical composition according to the invention contains as a therapeutic agent, a nonsteroidal antiinflammatory compound, mainly acetylsalicylic acid, and as a biologically active substance is ascorbic acid.

In addition, the pharmaceutical composition is in the form of a soluble effervescent tablets containing therapeutic agent, the main component of sipacate, the acid component of sipacate, frame material, the binder components and the filler according to the invention contains as a therapeutic agent, a mucolytic%:

Mucolytic drug - 1-10

The main component of sipacate - 10 - 30

The acid component of sipacate - 20-38

Dextrose anhydride - 10-30

Connecting components - 1-2

The filler is 0.5 - 5

This pharmaceutical composition according to the invention contains as a mucolytic drug Bromhexine, and as a sweetener, part of the filler - collamat sodium.

Pharmaceutical composition in the form of a soluble effervescent tablets containing frame material, the main component of sipacate, the acid component of sipacate, connecting components, filler, vitamins, macro - and micronutrients, according to the invention the pharmaceutical composition contains as a frame material dextrose anhydride in the following ratio, wt.%:

The main component of sipacate - 10-30

The acid component of sipacate - 20-38

Dextrose anhydride - 10-30

Connecting components - 1-2

The filler is 0.5 - 5

Vitamins, macro - and micronutrients in amounts necessary to bring the amount of components Up to 100%

The pharmaceutical composition according to the invention contains vitamins in the following amounts: vitamin C 0,5-1,5 g


Vitamin E - 5-15 mg

-carotene - 100-200 mcg

Vitamin a - 200-350 mg

Vitamin b11-3 mg

Vitamin b21-3 mg

Vitamin b6- 1 to 3 mg

Vitamin b12- 2-6 mcg

Nicotinamide - 15-20 mg

Calcium Pantothenate - 8-12 mg

Folic acid - 150-250 mg

Vitamin D is 10-30 mg

Vitamin K - 40-70 µg

Biotin - 40-70 µg

The pharmaceutical composition according to the invention contains macro - and micronutrients: iron, potassium, calcium, magnesium, manganese, copper, molybdenum, selenium, chromium, phosphorus, iodine, zinc.

Pharmaceutical composition in the form of a soluble effervescent tablets containing the main component of sipacate, the acid component of sipacate, frame material, the binder components, filler and vitamins, according to the invention the pharmaceutical composition further comprises one or more biologically active substances, at the same time as the frame material, the pharmaceutical composition contains dextrose anhydride in the following ratio, wt.%:

Biologically active substances of 0.1 - 4

The main component of sipacate - 10-40

The acid component of sipacate - 20-38

Dextrose anhydride - 10-30

Svetousileniya sum of components is Up to 100%

The pharmaceutical composition according to the invention contains as biologically active substances 2-4% of succinic acid relative to the weight of the composition, while it additionally contains as trace 0.05-0.1 mg selenium.

The pharmaceutical composition according to the invention contains vitamins in the following amounts, mg:

Vitamin C - 150-300

Vitamin E - 50-80

-carotene - 4-6

The pharmaceutical composition according to the invention contains as a biologically active substance 0,1-1% ginseng extract relative to the mass of the composition.

The pharmaceutical composition according to the invention contains as a biologically active substance 0,1-0,5% yohimbine hydrochloride in relation to the weight of the composition.

The pharmaceutical composition according to the invention contains as biologically active substances of 0.1 to 2.5% ginseng extract, 0.1 to 2.5% extract of lemongrass, 0.1 to 2.5% extract of Rhaponticum in relation to the weight of the composition.

The pharmaceutical composition according to the invention contains vitamins in the following amounts:

Vitamin C - 50-150 mg;

Vitamin E - 5-20 mg

-carotene - 100-500 mcg

Vitamin a - 200-500 mg

Vitamin BNicotinamide - 15-30 mg

Calcium Pantothenate - 8-20 mg

Folic acid - 150-400 mg

The pharmaceutical composition according to the invention contains carbonates and / or bicarbonates of alkali metals as a main component of sipacate, solid edible organic acid, preferably citric acid, as the acid component of sipacate, polyethylene glycol as a binder component, sweeteners and flavorings as filler.

The task is also solved by a method for obtaining a pharmaceutical composition in the form of a soluble effervescent tablets, including mixing, sieving, tableting, according to the invention, all operations are carried out at low absolute humidity in the range of 5-30%, and the tabletting operation carried out by the method of direct extrusion under pressure TC 3-10.

In addition, according to the invention, all components are sieved through a sieve with 1 mm

The decision of the specified problem are provided, as can be seen from the above, due to the fact that the pharmaceutical composition contains as a frame material dextrose anhydride, which leads to the fact that all the above CSF, the use of polyethylene glycol as a binder allows you to get face white pills with a good surface, which in turn leads to improved consumer properties.

The presence of various therapeutic agents, biologically active substances, vitamins, macro - and microelements extends the range of pharmacological activity, pharmaceutical compositions, resulting in expansion of the range.

In addition, to obtain good organoleptic characteristics in the pharmaceutical composition are introduced sweeteners and natural flavors.

The inventive method of obtaining the drug increases yield while reducing its cost by simplifying the process and reducing the time of the technological cycle.

To increase the stability of soluble effervescent tablets when storing all transactions are conducted at low absolute humidity of 5-20%.

The inventive pharmaceutical composition in the form of a soluble effervescent tablets and method of reception (see the patent of the Russian Federation 2043099, 2143891, 2155033) are different from the FR is, what about the have an inventive step.

Specified pharmaceutical composition in the form of a soluble effervescent tablets can be obtained and used in industry, therefore, meets the criterion of "industrial applicability".

An example of a specific implementation.

The inventive method is implemented as follows.

In mixer tank through a sieve with openings of not more than 1 mm is placed a therapeutic agent, biologically active substances, the main component of sipacate, the acid component of sipacate, frame material, the binder components, filler, vitamins, macro - and microelements. The mixing occurs within 10-15 minutes. The mixture for tabletting press with the help of tablet press machine-a method of direct pressing under pressure TC 3-10.

You get a white pill face shape with a good surface. The tablet diameter 25 mm, average weight of 3.5-5 g

All transactions are conducted at low absolute humidity of 5-20%.

The time of dissolution of the tablet in 100 ml of water at 60 C.

Shelf life 2 years.

The strength of the tablets on giving a new pharmaceutical composition in the form of effervescent soluble tablets

The inventive method of obtaining the drug provides

- increase the yield of the finished product while reducing cost by simplifying the process and reducing the time of the technological cycle.

1. Pharmaceutical composition in the form of a soluble effervescent tablets containing therapeutic agent in combination with a biologically active material, the main component of sipacate, the acid component of sipacate, frame material, the binder components and the filler, wherein the pharmaceutical composition as a frame material contains dextrose anhydride in the following ratio, wt. %:

Therapeutic agent - 1-15

Biologically active substance - 5-13

The main component of sipacate - 10-40

The acid component of sipacate - 20-38

Dextrose anhydride - 10-30

Connecting components - 1-2

The filler is 0.5 - 5

2. The pharmaceutical composition under item 1, characterized in that it contains as a therapeutic agent, a nonsteroidal antiinflammatory compound, mainly acetylsalicylic acid, and as a biologically active substance is ascorbic acid.

5. Pharmaceutical composition in the form of a soluble effervescent tablets containing frame material, the main component of sipacate, the acid component of sipacate, connecting components, filler, vitamins, macro - and micronutrients, wherein the pharmaceutical composition contains as a frame material dextrose anhydride in the following ratio, wt. %:

The main component of sipacate - 10-30

The acid component of sipacate - 20-38

Dextrose anhydride - 10-30

The binder is bringing the sum of the components 100

6. The pharmaceutical composition according to p. 5, characterized in that it contains vitamin C in the amount of 0.5-1.5 g

7. The pharmaceutical composition according to p. 5, characterized in that it contains vitamins in the following amounts:

Vitamin C is 50-100 mg

Vitamin E - 5-15 mg

-Carotene - 100-200 mcg

Vitamin a - 200-350 mg

Vitamin b11-3 mg

Vitamin b21-3 mg

Vitamin b61-3 mg

Vitamin b12- 2-6 mcg

Nicotinamide - 15-20 mg

Calcium Pantothenate - 8-12 mg

Folic acid - 150-250 mg

Vitamin D is 10-30 mg

Vitamin K - 40-70 µg

Biotin - 40-70 µg

8. The pharmaceutical composition according to p. 7, characterized in that it contains macro - and micronutrients: iron, potassium, calcium, magnesium, manganese, copper, molybdenum, selenium, chromium, phosphorus, iodine, zinc.

9. Pharmaceutical composition in the form of a soluble effervescent tablets containing the main component of sipacate, the acid component of sipacate, frame material, the binder components, filler and vitamins, wherein the pharmaceutical composition further comprises one or more biologically active substances, at the same time as frame material farmaceutiske active substances 0,1-4

The main component of sipacate - 10-40

The acid component of sipacate - 20-38

Dextrose anhydride - 10-30

Connecting components - 1-2

The filler is 0.5 - 5

Vitamins, macro - and micronutrients in amounts necessary to bring the amount of components Up to 100

10. The pharmaceutical composition according to p. 9, characterized in that it contains as biologically active substances 2-4% of succinic acid relative to the weight of the composition, while it additionally contains as trace 0.05-0.1 mg selenium.

11. The pharmaceutical composition according to paragraphs. 5 and 10, characterized in that it contains vitamins in the following amounts, mg:

Vitamin C - 150-300

Vitamin E - 50-80

-Carotene - 4-6

12. The pharmaceutical composition according to p. 9, characterized in that it contains as a biologically active substance 0,1-1% ginseng extract relative to the mass of the composition.

13. The pharmaceutical composition according to p. 9, characterized in that it contains as biologically active substances of 0.1-0.5% yohimbine hydrochloride in relation to the weight of the composition.

14. The pharmaceutical composition according to p. 9, characterized in that it contains as biologically asset the position.

15. The pharmaceutical composition according to paragraphs. 5, 12-14, characterized in that it contains vitamins in the following amounts:

Vitamin C - 50-150 mg

Vitamin E - 5-20 mg

-Carotene - 100-500 mcg

Vitamin a - 200-500 mg

Vitamin b1- 1-10 mg

Vitamin b2- 1-10 mg

Vitamin b6- 1-10 mg

Vitamin b12- 2-10 mg

Nicotinamide - 15-30 mg

Calcium Pantothenate - 8-20 mg

Folic acid - 150-400 mg

16. The pharmaceutical composition according to any one of paragraphs. 1, 3, 5, 9, characterized in that it contains carbonates and / or bicarbonates of alkali metals as a main component of sipacate, solid edible organic acid, preferably citric acid, as the acid component of sipacate, polyethylene glycol as a binder component, sweeteners and flavorings as filler.

17. The pharmaceutical composition according to p. 3, characterized in that it as a sweetener contains collamat sodium.

18. A method of obtaining a pharmaceutical composition in the form of a soluble effervescent tablets, including mixing, sieving, tableting, characterized in that all operations are carried out at low absolute humidity ASS="ptx2">

19. The method according to p. 2, characterized in that all components are sieved through a sieve with 1 mm

 

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