Method for preparing extract possessing anti-ulcerous activity

FIELD: medicine, gastroenterology, pharmaceutical industry.

SUBSTANCE: invention relates, in particular, to a method for preparing extract possessing the anti-ulcerous activity. Method for preparing extract eliciting an anti-ulcerous activity involves extraction of swampy sweet flag rhizomes with ethyl alcohol in diffusers battery under the definite conditions. Extract prepared by the claimed method possesses an anti-ulcerous activity and enhanced storage duration period.

EFFECT: improved preparing method, valuable medicinal properties of extract.

6 ex

 

The invention relates to the field pharmtechnology, particularly, to a method of producing a liquid extract having biological activity, from vegetable raw materials and pharmaceutical compositions based on it.

A method of obtaining liquid herbal extracts, consisting in the extraction of plant material in the battery percolation (diffusers) [1]. However, there are no specific criteria for carrying out the extraction for vegetable raw materials calamus swamp, the study of the properties of the extract which is of considerable interest.

Calamus rhizomes kind (finely ground powder) are part of the preparations Vikair and Usually used to treat gastritis and gastric ulcer. Also, calamus rhizomes are used in decoction, as a means of improving digestion [2]. However, to date there is no the best mode of the method of producing a liquid extract and the most efficient dosage form based on the total extraction of biologically active substances from the rhizomes of calamus swamp.

Liquid extract of the rhizomes of calamus swamp has a number of disadvantages,

1. The inconvenience of storing trasportinavigazione.it

2. Limited shelf-life (precipitate formation and reduction of potency during storage).

Neudobstvo use in the PE metricheskoi practice(contains ethyl alcohol).

The obtained experimental data characterizing 40% extract from the rhizomes of calamus swamp as a biologically active substance, for example, on the model of ulcerative pathology [3, 4].

An object of the invention is to expand the Arsenal of methods of obtaining extracts from plant material that has biological activity and the most rational dosage forms based on them.

The task to solve a new way to obtain an extract having biological activity, consisting in the extraction of plant raw material in the battery diffusers, using as extractant water-alcohol mixture, and as the plant materials used calamus rhizomes of marsh with a particle size of 1-5 mm, extraction was carried out with a ratio of raw materials extractant 1:4,35-1:6,0, when the concentration of ethanol up to 30-50% of the time insisting 7-35 hours, the battery from 2-8 diffusers.

Also proposed pharmaceutical composition based thick extract with a water content of 15-30%; may be made in the form of granules, which, in addition to the above extract, include excipients in the following ratio, wt.%:

Extract of calamus thick 10-30

Excipients (lactose, sucrose, pectin, MCC) 90-70

The method is as follows (example of the battery of diffusion):

Calamus rhizomes of marsh crushed to particle size of 1-5 mm, sifted through sieves d = 3 mm and 1 mm for the liberation of large particles and dust.

In the diffuser No. 1 load 10 g of raw material and fill of 43.5 ml of 40% ethanol (before the mirror) and left for 24 hours to draw.

After 24 hours, through drain valve, serves to extract from the diffuser # 1 cone # 2 to the education it mirrors. At the same time fill the cone No. 1 aliquot quantity of fresh extractant.

In the same way every 24 hours download third, fourth, fifth and sixth diffusers, to fill each cone is used to extract from the previous one, and the diffuser No. 1 serves a new portion of fresh extractant.

After a 24-hour infusion of all 6 diffusers diffuser No. 6 pour 20 ml of the finished product in the tank for settling. At the same time, giving him the extract from the diffuser No. 5, the diffuser No. 5 from No. 4 to No. 4 from No. 3 to No. 3 from No. 2, and No. 2 from No. 1. At this stage diffuser No. 1 does not fill with fresh extractant, and the spent raw material left in him, after recovery of residues of ethanol being unloaded.

Next, in the same way every 24 hours produces the shifting of extraction, consistently off from work diffusers№2, №3, №4, №5 and # 6. At each stage of the diffuser No. 6 issued on 20 ml of the finished product. All then the AI finished extract is poured into the tank for settling. The result is a 120 ml liquid extract (1:1), which advocated for three days at a temperature of 3-10°C, and then filtered.

The content of polysaccharides in the obtained extract was 8.3±0,18 %, and the dry residue 11,17±0,28%.

Justification mode

The extraction parameters were selected based on the following

1. The selected extraction method : - repercolation as the main active substances that lead to its biological activity, in particular in the mechanism of antiulcer effect are polysaccharides. The process of dissolution of polysaccharides characterized by the stage of swelling, which is time-consuming. Therefore, the method of dynamic extraction with a small contact time of the phases in this case did not justify itself and allow you to obtain an extract with a high content of dietary fibers and low content of polysaccharides.

2. The particle size of raw materials 1-5 mm At the smaller particle size of the packing materials in very dense diffuser that breaks the drainage of the solvent. If you increase the size of the particles decreases the yield of extractives and the depletion of raw materials.

3. The selection of the ratio of raw material and extractant 1:4,35-1:6,0 based on the fact that with fewer extractant it will not be enough to create a mirror in the diffuser as raw material has a low bulk weight, Bo is lsoi the ability to swell and high absorption of the extractant. When the number of the extractant decreases the quality of the finished product, because it dilutes (decreases the dry residue and the concentration of active substances).

4. The choice of the concentration of ethanol 30% to 50% based on the fact that at lower concentrations of ethanol in the final product decreases the amount of lipophilic substances, which are also involved in the mechanism of antiulcer action, thus decreasing the weight of the pharmacological effect. By increasing the concentration of ethanol decreases the yield of polysaccharides in the resulting extract.

5. The time of infusion is 7-35 hours. When shorter duration of infusion decreases the yield of extractives and the depletion of raw materials for the active substances. Longer infusion is impractical because to 24 hours extraction occurs the maximum depletion of raw materials and extractive active substances.

6. Using 2-8 diffusers due to the fact that the larger their number is impractical because the maximum depletion of raw materials is achieved by using a battery of 6 percolation and 24-hour infusion.

The content of polysaccharides in the obtained extract should be not less than 4.0%, and the dry residue is not less than 7.0%.

Examples of liquid extract, possessing the biological activity of the rhizomes of calamus b the pilot depending on the changing conditions of extraction.

Example No. 1. Obtaining a liquid extract of 40% ethanol from the rhizomes of calamus swamp with a particle size of 1-3 mm method of percolation. Insisting in one percolator within 36 hours. The ratio of raw material and extractant 1:4,35.

The dry residue in the resulting extract was 7,12±0,19%, and the content of polysaccharides 3,39±0,10 %.

Example No. 2. Obtaining a liquid extract of 40% ethanol from the rhizomes of calamus swamp with a particle size of 1-3 mm by dynamic maceration. The contact time of the phases 3 hours. The ratio of raw material and extractant 1:4,35.

The dry residue in the resulting extract was of 6.31±0,13%, and the content of polysaccharides 2,27±0,03 %.

Example No. 3. Obtaining a liquid extract of 40% ethanol from the rhizomes of calamus swamp with a particle size of 5-7 mm method repercolation, using a battery of 6 percolation and 24 hour infusion. The ratio of raw material and extractant 1:4,35.

The dry residue in the resulting extract was 6,94±0,17%, and the content of polysaccharides 3,86±0,13 %.

Example No. 4. Obtaining a liquid extract of 40% ethanol from the rhizomes of calamus swamp with a particle size of 1-3 mm method repercolation, using a battery of 6 percolation and 24-hour infusion. The ratio of raw material and extractant 1:6,1.

The dry residue in the resulting extract was 6,86 ± 0,17%, and the content of polysaccharides 4,88±0,14%.

Example No. 5. On the doctrine of liquid extract in 70% ethanol from the rhizomes of calamus swamp with a particle size of 1-3 mm method repercolation, using a battery of 6 percolation and 24-hour infusion. The ratio of raw material and extractant 1:4,35.

The dry residue in the resulting extract was there is a 10.03±0.25%, and the content of polysaccharides 2,67±0,05 %.

Example No. 6. Obtaining a liquid extract of 40% ethanol from the rhizomes of calamus swamp with a particle size of 1-3 mm method repercolation, using a battery of 6 percolation and 6-hour infusion. The ratio of raw material and extractant 1:4,35.

The dry residue in the resulting extract was becomes 9.97±0,22%, and the content of polysaccharides 3,76±0,11 %.

The liquid extract is concentrated to a moisture content of 15-30% (drying temperature not more than 70°). The content of polysaccharides in the thick extract should be at least 30%.

For convenience, use, and retention of the proposed pharmaceutical composition based thick extract of the rhizomes of calamus swamp, granules which contain, besides the above-mentioned extract excipients.

As auxiliary substances used lactose, sucrose, pectin, microcrystalline cellulose(MCC). Data accessories are widely used in pharmaceutical practice to obtain granules (5).

To obtain pellets take the following composition per dose:

Ingredient Qty, g
Extract of calamus thick0,3
Lactose0.5 to 1.5
Sucrose0.5 to 1.5
Pectin0,2-0,8
MCCof 0.1-0.3
Ethanol 70%q.s.

In the mixer load the calculated amount of sifted filler and while the mixer is injected heated extract of calamus dense. Then the resulting mass is added moisturizing liquid and mix to obtain a homogeneous mass. The wet mass is passed through a granulator - sieve No. 2 and dried at a temperature of 45°to the optimum residual moisture content of 4.5%. After drying, the granules are subjected to repeated extrusion through a drill with a smaller diameter holes. The drug is a cream-colored granules with specific pleasant smell and sweet taste, easily soluble in warm water.

The content of polysaccharides in the granules should not be less than 3.0 percent. The number of auxiliary substances were selected on the basis of experimental research, in all cases, the quantity of the extract was the same, varied only the number of auxiliary substances. It was shown that when the content of excipients less than 1.6 g weight bad was granulated and "sticks", and when the s content of more than 2.8 g mass was granulated satisfactorily, but the resulting pellets contained an insufficient number of active substances (polysaccharides) it was less necessary(less than 3%). In addition, the use of auxiliary substances in quantities of 90% for one dose dense extract economically irrational.

Thus the proposed method allows to obtain a liquid extract of the rhizomes of calamus swamp possessing biological activity, as well as based on it is more rational to use a pharmaceutical composition, which may be made of granulated.

Literature

1. Instructions for preparation of liquid extracts by the method of repercolation on variations N.A. Chulkov // Tr.-center. scientific studies. pharmacy laboratory. Scientific and practical information. M., 1943. No. 2.-P.9-12.

2. Mashkovsky PPM Medicines. Ed. 13-E. - Vol. 1. - Kharkov, 1997.-314 C.

3. Guriev A. M., Razin YEAR, Zueva, H.E., Kalinkina GI, Krylov YEAR, Amosov E.N., Usubov MS Experimental study calamus swamp (Acorns calamus L.) in the treatment of malignant neoplasms // pharmacy. 2003, No. 3.

4. Guriev A. M., Krylov YEAR, Razin YEAR, Zueva, H.E., Kalinkina GI, Amosov E.N., Usubov MS Experimental study of the antiulcer properties of calamus swamp (Acorus calamus L.) // Russian pharmacies. 2003, No. 10.

5. ANCOVA A.I., Technology of medicinal forms. M. Medicine, 1991, Vol.2, 53 S.

A method of obtaining an extract having anti-ulcer activity by extraction of plant raw materials ethyl alcohol in the battery diffusers, characterized in that the extraction of crushed up to 1-5 mm raw material rhizomes of calamus swamp carry out water-alcohol mixture with a ratio of raw material:extractant from 1:4,35 to 1:6.0 and concentration of ethanol 30-50% in the battery from 6-8 cones within 7-35 o'clock



 

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