Analgesic antipyretic drug and method thereof

 

(57) Abstract:

The invention relates to the pharmaceutical industry, in particular the production of medicines used for colds, relieving headaches and neuralgia. Analgesic antipyretic medication contains acetylsalicylic acid, paracetamol, caffeine, cocoa, starch, citric acid, sugar, talc, calcium stearate, and can additionally include polyvinylpyrrolidone (mol. mass 9900-35500, at a certain ratio of components. The method of obtaining new funds includes the preparation of raw materials, obtaining mass for tableting by mixing paracetamol, starch, caffeine, cocoa, moistening the mixture 45-50% solution of citric acid, 4,5-7,5% starch paste and 10-80% sugar syrup or 45-50% solution of citric acid and 10-80% sugar syrup, wet granulation, drying, dusting acetylsalicylic acid, starch, talc and calcium stearate, dry granulation. This is followed by tableting the resulting mass. The invention provides increased strength tablets. 4 C.p. f-crystals, 1 table.

The invention relates to pharmaceuticas is s, for relieving headaches and neuralgia.

Known analgiziruyuschee antipyretic drug (patent RF №2034533, class a 61 K 9/16, 9/20, 31/60, 31/62, 31/135, 31/615), containing acetylsalicylic acid, paracetamol, caffeine, cocoa, starch, citric acid, talc, calcium stearate.

It is also known drug (patent RF №2105547, class a 61 K 9/16) similar actions are taken for the prototype and containing wt.%: acid acetylsalicylic 41,4-45,8; paracetamol 31,3 or 33.3; caffeine is 4.9 to 6.0; cocoa 1,4-4,1; starch 10,0-15,0; citric acid 0,4-1,8; talc from 0.5 to 0.95; calcium stearate 0.5 to 1.0.

A method of obtaining analgesic drugs (patent RF №2034533, class a 61 K 9/16, 9/20, 31/60, 31/62, 31/135, 31/615), including the preparation of raw materials, obtaining mass for tabletting, by mixing paracetamol, starch, caffeine, cocoa, moistening the mixture of 55.5% citric acid solution and 7-10% solution of starch paste, wet granulation, drying, dusting tablet mass acetylsalicylic acid, starch, and calcium stearate, dry granulation, tableting.

A disadvantage of the known medicines is that tablets of this tool are relatively Nevis and packaging.

The aim of the invention is to obtain medicines, tablets which have a higher mechanical strength.

This goal is achieved by the introduction of the new medicines ingredient refined sugar (for example, according to GOST 22-94) and changes in the ratio of ingredients. Refined sugar used in the preparation of the humidifier has better binding properties than starch, and is introduced into the composition instead of this ingredient.

Moreover, the analgesic drug contains components in the following ratio, wt.%: acid acetylsalicylic 41,4-45,8; paracetamol 31,3-34,5; caffeine is 4.9 to 6.0; cocoa 1,4-4,1; starch 5,0-15,0; refined sugar of 0.05 to 10.0; citric acid 0,4-1,8; talc 0,5-3,0; calcium stearate 0.5 to 1.0.

To improve raspadaemosti tablets offered by the drug may further comprise polyvinylpyrrolidon mol. mass 9900-35500 in an amount of 0.1-1.5 wt.%.

New in the proposed composition of the medicinal product is new, in comparison with the prototype, ingredient refined sugar.

The proposed ratio and limits changes in the content of the ingredients is drugs. When the ratio is changed and the limits of existing drugs (acetylsalicylic acid, paracetamol and caffeine) worsens therapeutic effect of the medicinal product. Reduced cocoa content (less than 1.4 wt.%) leads to deterioration of the appearance and taste of the tablets, and the increase (more than 4.1 wt.%) increases time raspadaemosti tablets. The decrease in starch content (less than 5.0 wt.%) increases raspadaemosti tablets, and the increase (more than 15.0 wt.%) to decrease the strength of the tablets. The reduction in the content of refined sugar (less than 0.05 wt.%) leads to insufficient strength of the tablets, and the increase (more than 10.0 wt.%) increase the time raspadaemosti tablets (more than 15 min). The reduction in the content of talc (less than 0.5 wt.%) leads to ethnological tabletting process, and the increase (more than 3.0 wt.%) invalid due to the toxicity of the ingredient. The reduction in the content of citric acid (less than 0.4 wt.%) leads to deterioration of the quality of the tablets because of low strength, and the increase (more than 1.8 wt.%) increase the time raspadaemosti tablets (more than 15 min). The reduction of calcium stearate (less than 0.5 wt.%) affects the sliding properties of the granulate in Ableton medicines (GF XI, C. 2).

A method of obtaining analgesic antipyretic drugs (patent RF №2034533, class a 61 K 9/16, 9/20, 31/60, 31/62, 31/135, 31/615 the prototype does not allow to obtain high strength tablets, guaranteeing the security requirements of normative documentation in appearance.

We propose a method of manufacture of a medicinal product, in order to increase the strength of the tablets, in contrast to the known method, the moisture mass after mixing the ingredients undergo additional sugar syrup concentration of 10-80% with partial or complete replacement of starch paste. For humidification of the applied solution of citric acid concentration of 45-50%, and starch paste, if using, applied concentration 4,5-7,5%.

The proposed method, therefore, involves the preparation of raw materials, obtaining mass for tableting by mixing paracetamol, starch, caffeine, cocoa, moistening the mixture 45-50% solution of citric acid, 4,5-7,5% solution of starch paste and/or 10-80% sugar, wet granulation, drying, dusting tablet mass acetylsalicylic acid, starch, talc and calcium stearate, dry the humidifier sugar syrup concentration of 10-80%.

Preferably, in order to improve raspadaemosti when moistened mixture was also used 1-10% solution of polyvinylpyrrolidone with a molecular mass of 9900-35500.

To improve color and odor tablets drug, preferably a part of the cocoa in the amount of 0.2 to 1.5 wt.% to enter transactions dusting tablet mass.

The table below shows the composition and characteristics of samples of the tablets offered drugs compared to the prototype. The sample preparation was carried out using standard equipment: blade mixer, dryer fluidized bed SP-60, granulator, rotary tablet machine RTM-41. Strength tablets crush strength was determined on the tester tensile strength of tablets ERWEKA TVN 20. From the above results it follows that the proposed technical solutions allow you to increase the strength of the pill crushing on 12-51%, the abrasion resistance 0.2-0.8%, while ensuring their good raspadaemosti.

1. Analgesic antipyretic medication containing acetylsalicylic acid, paracetamol, caffeine, cocoa, starch, citric acid, talc and calcium stearate, characterized in,">Acetylsalicylic acid 41,4-45,8

Paracetamol 31,1-34,5

Caffeine Is 4.9 To 6.0

Cocoa 1,4-4,1

Starch 5,0-15,0

Refined sugar is 0.05 to 10.0

Citric acid 0,4-1,8

Talc 0,5-3,0

Calcium stearate 0.5 to 1.0

2. Drug under item 1, characterized in that it further contains 0.1 to 1.5 wt.% polyvinylpyrrolidone (mol. mass 9900-35500.

3. The method of obtaining analgesic antipyretic drugs under item 1, including the preparation of raw materials, obtaining mass for tableting by mixing paracetamol, starch, caffeine, cocoa, moistening the mixture, wet granulation, drying, dusting acetylsalicylic acid, starch, talc and calcium stearate, dry granulation, tableting, characterized in that the hydration of the mixture after mixing ingredients spend 45-50% solution of citric acid, 4,5-7,5% starch paste and 10-80% sugar syrup or 45-50% solution of citric acid and 10-80%th sugar syrup.

4. The method according to p. 3, characterized in that the hydration of the mixture of ingredients is conducted additionally 1-10% solution of polyvinylpyrrolidone (mol. mass 9900-35500.

5. JV the mass.



 

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