RU2260440C1 - Method for preparing preparation "alloocholum" - Google Patents

Abstract

FIELD: medicine, gastroenterology, pharmacy.

SUBSTANCE: invention relates to a method for preparing the cholagogic agent "Allocholum" used in chronic hepatitis, cholangitis, cholecystitis and habitual constipation associated with intestine atonia. Method for preparing "Allochole" tablets involves mixing such components as bile, vegetable products, nettle extract, garlic, potato starch, activated carbon, taste supplements and molding the medicinal formulation by granulation, drying and powdering. Method involves mixing dried garlic, nettle leaves, average-molecular polyvinylpyrrolidone and separating preparing a mixture of dried bile of particles size 0.6-1.0 mm with aerosil, talc and average-molecular polyvinylpyrrolidone. To the prepared mixture dried granulate is added, the mixture is tableted, moistened with 70% sugar syrup containing 0.35-0.40% of average-molecular polyvinylpyrrolidone and by forming envelope and powdering with magnesium basic carbonate powder. Invention provides enhancing strength of tablet in simultaneous rapid its degradation, enhancing stability in storage.

EFFECT: improved preparing method.

2 tbl

Description

The invention relates to medicine and the medical industry, in particular to a method for producing a choleretic agent allochol, used for chronic hepatitis, cholangitis, cholecystitis and the usual constipation associated with intestinal atony.

In recent years, diseases of the gastrointestinal tract have become widespread, the share of which is about 40%. The relevance of the problem is confirmed by a large number of studies conducted in this area.

As a rule, the solution to this problem comes down either to the creation of whole compositions, including extracts of plant origin (US Pat. RF No. 2034849, 2045956), or to the search for technologies for their purification and production (ed. St. USSR No. 1343497, 1343592), or to the allocation of biologically active agents from animal raw materials (US Pat. RF №№2019172, 2054947).

Currently, a number of drugs with choleretic, cholekinetic effect are known. These are drugs such as olimetin (OAO \ Nizhpharm \), pumpkin (ZAO \ Evropat Biofarm \) - preparations from plant materials, urosal (Czech Republic), oddestol (Poland) - preparations obtained from chemical raw materials. The existing need of domestic health care for affordable gastroenterological agents stimulated work on obtaining domestic preparations from raw materials of animal origin, including through the development of new technologies for producing dosage forms.

As pharmaceuticals for digestive disorders, the domestic pharmaceutical industry produces lyobil (FS 42-2523-88), tablets with lyophilized bovine bile, pancreatin (FS 42-1397-83), multi-enzyme tablets containing trypsin and amylase (Drug Register 2000 )

Known choleretic agent allochol in the form of coated tablets containing animal bile, dry garlic extract, nettle extract, activated charcoal and excipients / Mashkovsky M.D. Medicines, t. 1, M. 2000 /.

Closest to the claimed method for producing allohol is a method for producing allahol in the form of tablets, which consists in mixing components, such as bile, plant products of nettle extract, garlic, potato starch, activated carbon, flavoring agents, forming a dosage form by granulation, drying, dusting (Application RU No. 94013129, 05.20.1996.)

The disadvantages of the known methods is the low strength of the obtained tablets, low technological method of obtaining the drug. In addition, the tablet has an unpleasant taste.

The purpose of this invention is the creation of technology that allows you to get a simple and affordable form of the drug in the form of a coated tablet, increasing the strength of the tablet while its rapid disintegration in water, increasing storage stability.

The goal is achieved by using the method of producing allahol in the form of tablets, which consists in mixing components, such as bile, plant products of nettle extract, garlic, potato starch, activated carbon, flavoring agents, the formation of the dosage form by granulation, drying, dusting. At the same time, dried garlic, nettle leaves, medium-molecular PVP are mixed, while a mixture of dry bile with a particle size of 0.6-1.0 mm with aerosil, talc and medium-PVP is separately prepared, dry granulate is added to the resulting mixture, the mixture is tabletted, moistened 70 % sugar syrup containing 0.35-0.40% PVP of medium molecular weight, forming a shell, dusted with magnesium powder of basic carbonate.

The authors found that bile causes a partial hydrolysis of starch and sugar to form glucose and other substances. The resulting glucose under these conditions is oxidized, forming colored products. Therefore, when stained, brown spots appear on the surface of the tablet, and then the entire mass of the tablet becomes brown.

The invention is illustrated by the following example of the preparation of a coated tablet preparation.

Pre-grind the nettle leaves. Then the nettle leaf powder is heated to 70-80 ° C and dried for 2.5-3.0 hours to a residual moisture content of 6%. The dried leaves are sieved through a sieve with a hole diameter of 0.35 mm.

Activated carbon is heated separately in the apparatus to 130-140 ° C and dried for 2.5-3.0 hours to a residual moisture content of 6%. Coal is sieved through a No. 25 sieve.

Starch with a moisture content of 18% at a temperature of 40-50 ° C for 1.5-2.0 hours is dried to a moisture content of not more than 3%. Cool and sift. A 9% starch paste is prepared by adding to the water heated to 95 ° C. a suspension consisting of starch and water at a ratio of 1: 1.7. The mixture is stirred for 10-15 minutes and cooled to 20-30 ° C. Dry bile is passed through a granulator with a mesh of 0.6-1.0 mm. Talc is calcined by aging with stirring for 2 hours at a temperature of 100-120 ° C, sieved through a sieve. All remaining raw materials are sieved: dried garlic through a 0.25 mm sieve, magnesium oxide through a 0.2 mm sieve, talc, aerosil, calcium stearate, medium molecular weight PVP, potato starch through a sieve 0.38, magnesium carbonate through a sieve 0, 23 mm. Then, 70% sugar syrup with medium molecular weight PVP is prepared, for which medium-molecular weight PVP is added to water heated to 50-60 ° C and mixed until completely dissolved, then sugar is added and the temperature of the syrup is brought to 100-120 ° C with stirring, the syrup is evaporated to dry content of 70%. The finished syrup is cooled and filtered.

To obtain wet granules, dried garlic, chopped nettles, activated carbon, medium-molecular-weight PVP, magnesium oxide, dry starch are mixed, after which they are moistened with a 9% starch paste in 3-4 doses. Stir until smooth. The moisture content of the mixture should be in the range of 35-38%. Wet granulation is carried out on a granulator with a diameter of the holes of the cleaning mesh 5 mm Wet granulate is dried at a temperature of 40-50 ° C for 30-40 minutes to a residual moisture content of 5.5-7%. The dried mass is sent to dry granulation.

To dry bile with a particle size of 0.6-1.0 mm, aerosil is added in 3 doses for dusting, the mixture is stirred, then talc, calcium stearate and medium molecular weight PVP are added, mixed. Dry granulate is added, mixed. The resulting mixture is tabletted, moistened with 70% sugar syrup containing 0.35-0.40% PVP of medium molecular weight, after uniform distribution of the syrup on the surface of the tablets, they are sprinkled with basic magnesium carbonate powder. After the tablets have dried, they are again watered with 70% syrup with PVP and sprinkled with basic magnesium carbonate. The operation is repeated several times. The tablets are dried. The surface of the obtained tablets is glossed with beeswax.

The experimental results are summarized in tables 1 and 2.

Strict adherence to the parameters of the proposed method allowed to achieve the goal.

Table 1 Technological parameters 1 2 3 Wet granulation: dried garlic 34 35.5 36 nettle leaves 4 4.46 5 activated carbon twenty 22.2 23 magnesium oxide 23.5 24.1 24.5 potato starch 7.5 7.94 8.5 PVP is a medium molecule. 5.5 5.8 6.0 Dry mix: bile particle size 0.6-1.0 mm 89 89.4 90 aerosil 0.4 0.43 0.5 talc 5.5 5.69 6.0 PVP is a medium molecule. 2 2.24 3.0 calcium stearate 2 2.24 3.0

table 2 Example No. The value of quality indicators during storage for 1 month Compressive strength, kg / s Abrasion,% Disintegration, s 1 3.6 0.06 435 2 4.1 0.9 379 3 3.8 1,1 421 The method according to the prototype 3 No. 94013129 (tablet without shell) 2,8 3.2 732

Claims (1)

A method of producing allohol in the form of tablets, which consists in mixing components, such as bile, plant products: nettle extract, garlic, potato starch, activated carbon, flavoring agents, forming a dosage form by granulation, drying, dusting, characterized in that the dried garlic, nettle leaves, medium-molecular weight PVP, while separately preparing a mixture of dry bile with a particle size of 0.6-1.0 mm with aerosil, talc and medium-molecular weight PVP, add su oh granulation mixture is tableted, moistened with 70% sugar syrup containing 0.35-0.40% PVP middle molecular form a shell with powder dusted basic magnesium carbonate.