The method of producing paracetamol tablets

 

(57) Abstract:

The invention relates to chemical-pharmaceutical industry, in particular, to methods for drugs, namely paracetamol, intended for the treatment of gout, migraines, and also used as analgesic and antipyretic. The invention is as follows: first, mixing paracetamol with starch 2 - 3% moisture content in the ratio of 1: (of 0.066 - 0,068), then moisten the mixture of starch paste in a ratio of 1: (0,27 - 0,29) accordingly, drying of the granules is carried out at a temperature of 40 - 50oC, dusting spend a mixture of starch 2 - 3% moisture content with stearic acid at a ratio of 1: (0,97 - 0,99) and when the ratio of the mass of the granulate mass apadravya a mixture of 1: (0,015 - 0,017). table 1.

The invention relates to the medical industry, in particular, to methods for producing pharmaceuticals for the treatment of gout, migraines, and also used as analgesics and antipyretics.

Such tools include paracetamol, representing parazitologiia. The most frequently used synonym of paracetamol, approved by the world organization strstr X ed. page 505.

Known methods for producing paracetamol (U.S. Pat. USA 4757090; U.S. Pat. GDR 270465). A method of obtaining tablets of paracetamol (Industrial regulations on the production of tablets of paracetamol 0.2 g, PR 64-1409-82-89), including mixing and hydration of the components of the tablet mass, wet granulation, drying of the granulate, dry granulation and dusting granulate.

Known technology is not allowed to increase the mass of the tablet. When the radiation-generating opportunities by known techniques tablets with weight, for example 0.5 g, was detected incompliance with the requirements of the State Pharmacopoeia of the strength and raspadaemosti tablets.

The feasibility of increasing the dose of paracetamol from 0.2 to 0.5 g shown in the study of pharmacokinetics of various tablets. Dose was increased, almost no impact on the full elimination of the drug from the body, provides rapid achievement of the maximum concentration of paracetamol in the blood necessary for providing therapeutic effects.

The tablet obtained by known techniques with a dose of 0.2 g contain:

Paracetamol 90,91%

Starch with moisture content of 10% 5,12%

Stearic acid 0,79%

Syrup of krahmer of tablets compared with foreign products "Panadol" (UK) and "Paracetamol" 0,5 (India). In addition, when the drying of the granulate was required elevated temperature 60 70oC, which led to partial decomposition of starch.

In the proposed method of obtaining tablets of paracetamol, including mixing and hydration of the components of the tablet mass, wet granulation, drying of the granulate, dry granulation and dusting granulate, mixing and hydration of the components of the tablet mass is conducted sequentially: first, mixing paracetamol with starch 2 3% moisture in the ratio 1: (of 0.066 - 0,068), then moistening the mixture of starch paste in a ratio of 1: (0,27 0,29), drying of the granules is carried out at a temperature of 40 50oC, dusting spend a mixture of starch 2 3% humidity with stearic acid at a ratio of 1: (0,97 0,99) and when the ratio of the mass of the granulate mass apadravya a mixture of 1: (0,015 0,017).

The composition of the tablets with a dose of paracetamol 0.5 for the proposed method comprises the following components: paracetamol, starch with moisture content of 2 to 3% and stearic acid.

The percentage of the components of the tablet as claimed method, and known the same as the total starch content and starch syrup (starch) in the tablet, Pius proposed method from the known (prototype).

Mixing and hydration of the components of the tablet mass is carried out in two stages

a) mixing paracetamol with starch in a ratio of 1: (of 0.066 0,068),

b) wetting the mixture of starch paste in a ratio of 1: (0,27 0,29).

This difference allowed us to improve the quality of the tablet, its pharmacokinetics, absorption performance.

Drying of the granules is carried out at a temperature of 40 50oC instead of 60 - 70oC by a known method, thus avoiding partial degradation of starch.

The dusting granulate is carried out with a mixture of starch 2 3% humidity with stearic acid 1: (0,97 0,99) when the ratio of the mass of the granulate mass apadravya a mixture of 1: (0,015 0,017) that allows you to get a tablet with a dose of 0.5 g of paracetamol corresponding to the strength requirements of the State Pharmacopoeia X ed.

Justification of the choice of the optimal proportions and technology parameters are given in table 1.

Regulatory indicators solubility and strength of the tablets, which are determined in accordance with the State Pharmacopoeia XI ed. vol. 2, pp. 156, 157.

For the implementation of the proposed method paracetamol mixed with potato starch vladismaksi mixture of paracetamol by weight of starch paste 1: (0,27 0,29). The wet mass is passed through a granulator with a hole diameter of 2.0 mm

The moist granulate is dried at a temperature of 40 50oC to a residual moisture content of 2 to 3% of the Dry granulate is passed through a granulator hole diameter 1.5 to 2.0 mm and optivault mixture of potato starch 2 3% moisture and stearic acid in a ratio of mass of starch by weight stearic acid 1: (0,97 0,99). The ratio of the mass of the granulate mass apadravya mixture (starch with stearic acid) is 1: (0,015 - 0,017).

The resulting mass tabletirujut on a tablet press tool with a diameter of 12 mm punches

The proposed method allowed us to obtain tablets of paracetamol with a dose of 0.5 g with the strength of 97 to 98.5% solubility 75 80% in 45 minutes and to avoid degradation of starch during drying.

Tablets of the proposed method on the pharmacokinetics are at the level of the best foreign samples "Panadol" (UK) and Paracetamol 0.5" (India).

The method of producing tablets of paracetamol by mixing and wetting of the components of the tablet mass, wet granulation, drying of the granulate, dry granulation and dusting granulate, wherein the mixing and moistening companies resulting mixture of starch paste in a ratio of 1:(0,27 0,29), respectively, drying of the granules is carried out at a temperature of 40 to 50C to a residual moisture content of 2 to 3% of the dusting granulate is carried out with a mixture of starch 2 3% humidity and stearic acid in a ratio of 1:(0,97 0,99), respectively, and the ratio of the mass of granular and apadravya a mixture of 1:(0,015 - 0,017).

 

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