CS263178B1 - A method for preparing an inert carrier for dry tabletting - Google Patents

Abstract

The solution belongs to the field of chemistry, namely to the field of paper and cellulose processing. Its essence lies in the fact that beech sulphate viscose pulp is subjected to acidic heterogeneous hydrolysis with 0.55 to 0.69 molar hydrochloric acid, at a ratio of 1 part of solid phase to 7 to 10 parts by weight of liquid phase, at a temperature of 95 to 105 ° C and atmospheric pressure for a period of 70 to 100 minutes. The subject matter can be used in the pharmaceutical industry in the preparation of tablets by dry tableting.

Description

263178 2

The present invention relates to a process for the preparation of a carrier suitable for the manufacture of tablet dosage forms in the pharmaceutical industry by dry tabletting.

Known Process for Preparing Microcrystalline Cellulose / US Pat. No. 2,978,446 is based on an acidic heterogeneous hydrolysis of pulp with mineral acids having a concentration of from 1 to 2.5 M. The disadvantage of this process is that it makes it possible to produce a fine form of microcrystalline cellulose having a particle size of up to 50 microns, the shape of the particles being rod-shaped and bulk. about 180 g.dm 3. Another disadvantage is the high acid concentration, which leads to the formation of undesirable by-products and to the demands of the reactor material.

The method of AO 132 508, which is based on acidic heterogeneous hydrolysis with 1.0-2.5 M hydrochloric acid at 80-95 ° C for 45 minutes, as well as AO 213 442 based on acidic heterogeneous hydrolysis with 0.15% up to 0.30 M hydrochloric acid at 80 to 95 ° C for 120 minutes, have the disadvantage that the use of microcrystalline cellulose for its rod-shaped, low bulk density and powdered formulations is used for dry tabletting.

The method of SU 751 808 is based on the preparation of microcrystalline cellulose from hydrolyse lignin, at a nitric acid concentration of 1-2 M, at 90-100 ° C for 4-5 hours. The disadvantage of this method is the low stability of microcrystalline cellulose, making it suitable for the pharmaceutical industry.

The method of preparing microcrystalline cellulose by acid heterogeneous hydrolysis according to AO 214 499a is based on the treatment of microcrystalline cellulose prepared according to AO 213 442 by wet-damping in a water-fast mixer at a speed of 6 to 10,000 rpm. for 10-30 min. at a cellulose concentration in the range of 10 to 20% by weight; In a second step, the microcrystalline cellulose is filtered off, dried at 80-100 ° C, and in the third stage, the driedcrystalline cellulose defibrils on a dry defibrator and sorts the particle size in the range of 30-300.

A disadvantage of this method of microcrystalline cellulose treatment is the rod-shaped shape, powder form, particle size 30 to 300 and bulk density of 150 to 300 g.dm-3, which is unsuitable for application in the preparation of tablet drug forms by dry tabletting on high speed tableting machines.

The above-mentioned disadvantages are eliminated by the present invention, which is characterized in that the cellulose pulp is subjected to an acidic heterogeneous hydrolysis of 0.55 to 0.69 molar hydrochloric acid, with a hydromodule of 1 to 7 to 10, a temperature of 95 to 105 ° C, and a time of 70 to 100 minutes. After filtration with ethyl alcohol, the wet intermediate is passed through a wet worm granulator, providing an optimum post-drying in the chamber driers and milling on the nose nose mill. The granulated product is dried at 80-95 ° C after the dry defigration of the puncture nasal mill, the microcrystalline cellulose is phased into a fraction which provides optimum processing properties for dry tableting with a particle size of 60 to 500 microns and a bulk density of 450 to 450 g.dm

A major advantage of the present invention is that the microcrystalline cellulosic granular shape, 60 to 500 particle size, and bulk density of 350 to 450 g.dm 3, being a suitable carrier in the preparation of medicaments by dry tableting, is another advantage of this process. the proportion of the fraction with the indicated particle size is about.

The moisture of the prepared microcrystalline cellulose is 2 to 4%, the ash content is 0.12%, the pH is 5 to 6.5, the heavy metal content is 10 ppm, the water-soluble content is 0.12%, which corresponds to the world quality requirements for use as carrier for dry tabletting.

Claims (1)

The invention has a wide application in the pharmaceutical industry for the preparation of tablets by the dry route, further in the food industry and others. It is already implemented and used in Bukóza n.p. Vranov n / TopIou. Example 1 80 kg of beech sulphate viscose pulp are cut on a table cutter with a width of 150 mm. Before being fed to the reactor, the pulp strips are soaked in water and fed to the reactors for 15 minutes to 800 liters of 0.60 molar hydrochloric acid heated to 80 ° C. The pulp is subjected to acidic heterogeneous hydrolysis at 100 ° C and atmospheric pressure for 90 minutes . the intermediate obtained is washed with distilled water and ethyl alcohol. Drying of the filtrate with a wet intermediate is granulated on a wet screw granulator with a 10 mm diameter orifice and dried in a chamber stationary oven at 80 to 95 ° C. 0.060 and 0.500 mm. The fraction of the fraction with a range of 60 to 500 microns represents 70% of the total bulk density of 400 g. Example 2 80 kg of beech sulphate viscose pulp are cut on a 150 mm wide table cutter. Before being fed into the reactor, the pulp strips soaked in water and dosed into the reactor over a period of 15 minutes to 800 l of 0.55 molar hydrochloric acid are heated to 80 ° C. The pulp is subjected to acidic heterogeneous hydrolysis at 95 ° C and atmospheric pressure for 100 minutes. The intermediate obtained is washed with distilled water with ethyl alcohol. After aspiration, the wet intermediate is granulated on a wet screw granulator with 10 mm diameter nozzle orifices and dried in a continuous oven, leaving a dry defibrillation process and a sieving apparatus of 0.60 mm and 0.500 mm sieve fraction of 60 microcrystalline cellulose. up to 500 microns 87% and a bulk density of 370 g.drrT. β The invention is widely used in the pharmaceutical industry for the preparation of tablets by dry powder, further in the food industry, and the object of the present invention. to 0.69 M hydrochloric acid, at a ratio of 1 part of solid to 7 to 10 parts by weight of liquid phase, at 95 to 105 ° C and atmospheric pressure, for 70 to 100 minutes.