Method for producing agent possessing anti-inflammatory, diuretic and antioxidant activity

FIELD: medicine.

SUBSTANCE: method for preparing an agent possessing anti-inflammatory, diuretic and antioxidant activity, involving milling Spiraea salicifolia shoots representing a mixture of leaves, blossom and shoots, extracting them three times by gradual maceration, mixing in infusing, filtering, condensing, separating, drying in the certain environment.

EFFECT: agent shoes the pronounced anti-inflammatory, diuretic and antioxidant activity.

2 dwg, 12 tbl

 

The invention relates to pharmaceutical industry and relates to a method of production of drugs from plant materials.

In recent years there has been a steady increase in inflammatory diseases of the genitourinary system, the gastrointestinal tract associated with adverse environmental conditions, improper and unhealthy diets. In Russia diseases of this group suffers every tenth citizen [Electronic resource. URL: http://www.pharmvestnik.ru/publs/staryi-arxiv-gazetv/12455.html#.UlIe21DIYlQ]. In the treatment of inflammatory diseases of the widely used synthetic drugs. However, when expressed therapeutic effect, they have side effects, contraindications and restrictions apply, does not always prevent the development of recurrent disease after their cancellation.

The advantage of medicinal plants and drugs from them is their low toxicity, long-term use without side effects, a wide range of pharmacological actions.

For the treatment of inflammatory diseases use the aqueous extract of the flowers of calendula officinal in the ratio (1:10) [the State register of medicines on 02.04.2012 [Electronic resource] URL: http://grls.rosminzdrav.ru]. Also used infusions of chamomile flowers [Sokolov, S. J. Phytotherapy and f is chopharmacology / S. J. Sokolov. - M.: MIA, 2000. - 970 S.].

The use of aqueous extracts in the form of infusions and decoctions have disadvantages, namely, that the shelf life after production is 2 days at a temperature of +4°C [Pharmaceutical technology. Technology of medicinal forms: textbook / I. I., Krasnik, Century, Mikhailova, I. C. Denisov, V. I. Woodrow Wilson; edited by I. I. of Krasnica, Century, Mikhailova. - M.: GOATER Media, 2011. - 657 C.]. Extraction of plant materials the purified water does not extract the full complex of biologically active substances [Minin, S. A. Chemistry and technology of herbal remedies: the textbook // S. A. Minin, I. E. Kauhava. - M.: GOATER Media, 2009. - 560 C.]. From 50 to 90% of active substances remains in raw materials.

At the present time proven herbs on the basis of dry extracts. In the process of obtaining extracts of dry ensures the maximum yield of biologically active substances (BAS), it is possible to develop dosage forms in the form of granules and tablets.

Closest to the claimed is the method of obtaining funds, possessing diuretic and anti-inflammatory activity [RF patent 2342945, M CL A61K 36/73, A61P 13/00, A61P 29/00, publ. 10.01.2009,]. This method consists in the fact that as a source of raw materials use leaves of strawberry - Fragaria ananassa L. the Air-dried leaves of elaut to particle size of 3 mm and extracted with 3 times 30 minutes of purified water in the ratio of raw materials-extractant 1:10 in the reactor of stainless steel with a false bottom with a capacity of 100 l, equipped with an anchor stirrer, a steam jacket and liner for a thermometer. Water extract combine. Cleaning combined aqueous extracts performed by filtering through Druk air filter and separation. Evaporation of the United water extraction is carried out in a circulating vacuum evaporation apparatus to 0.1 volume. Drying is conducted to the spray dryer. The yield is 20% by weight of vegetable raw materials.

The disadvantages of this method include the fact that it does not extract the entire complex of biologically active substances from plant materials, because in this way are extracted only water-soluble compounds.

The technical result of the proposed method is to increase the yield of the target product, expanding the resource base and the spectrum of pharmacological action.

The technical result is achieved by extraction of plant raw materials ethyl alcohol 40%, evaporation and drying.

New in the achievement of the technical result is that as the plant materials used shoots threshed Spiraea epolito (Spiraea salicifolia L), representing a mix of leaves, flowers and twigs no thicker than 3 mm

Spirea evalita is a shrub, up to 1.5 m, is widely spread on the territory of Russia. Aboveground organs contain the at coumarins, phenol carbonic acids (caffeic, ferulic), flavonoids (hyperoside, depantsed quercetin). Their maximum number is accumulated in the shoots of the current year in the flowering period. In folk medicine spirea evalita is used in diseases of the gastrointestinal tract and urogenital system [Plant resources of the USSR: flowering plants, their chemical composition and utilization. Family Hydrangeaceae-Haloragaceae. - SPb., 1991. - S. 101].

The aim of the present invention is to increase the yield of biologically active substances and expansion of a spectrum of pharmacological effects, which are provided by the extraction shoots Spiraea epolito - Spiraea salicifolia L. of ethyl 40% triple extraction, when the ratio of raw materials-extractant 1:14 in dynamic conditions, the mixing of raw materials, temperature of extraction 55°C, so that after combining the extracts spend assertion.

The optimal extraction parameters were set experimentally (table.1-5).

What's new is that as the extractant used ethyl alcohol 40%. To establish the optimal extractant were obtained extract using purified water and 10-90% ethyl alcohol. The content of extractives in the obtained extracts was determined by GF XI, flavonoids spectrophotometric method based on the reaction of complexo is obrazovaniya with aluminum chloride, the calculation of the percentage held in rutin. Output in the extraction of phenol carbonic acids was monitored by spectrophotometric method. The calculation of the percentage of the amount of phenol carbonic acids were converted into caffeic acid at the specific index of absorption of caffeic acid, equal 782 at a wavelength of 325 nm.

Purified water extracts less extractive substances, flavonoids and phenol carbonic acids. With increasing concentration of ethyl alcohol is an increase in the yield of biologically active substances. Their maximum number is obtained by using 40% ethyl alcohol (PL.1). Further increasing the concentration of ethyl alcohol in excelente leads to reduction of the yield of extractive substances and amounts of flavonoids.

What is new is that for extraction using raw materials with a particle size of 2 mm, it is Known that the particle size of the raw material determines the completeness and speed of transition in the solution of extracted substances. The optimal degree of grinding, which achieved the highest yield of extractive substances and flavonoids when the ratio of raw material and extractant 1:10 and room temperature is 2 mm (PL.2).

The extraction of raw materials by crushing, less than 1 mm, it is difficult to clean extraction from the smallest particles of the raw material, so d is nom case, the optimal particle size - 2 mm.

The output of extractive and, therefore, biologically active substances is influenced by the ratio of raw material to the extractant. The greatest number of extractive and biologically active substances - flavonoids and phenol carbonic acids extracted at a ratio of raw material and extractant 1:14 (PL.3), which is also new.

To increase the yield of extractive substances from medicinal plants is influenced by the temperature factor and the mixing process. The greatest number of extractive substances, flavonoids and phenol carbonic acids from shoots Spiraea evolites is extracted at a temperature of 55°C (table.4). The use of higher temperatures in this case is disadvantageous from an economic point of view and ensures the stability of the chemical composition of the target product.

What is new is the duration of stages of extraction: stage 1 - 120 min, 2nd level - 90 min, 3-stage - 60 min (table.5), which increases the yield of the target product.

What's new is that before filtering the combined extracts are defending at a temperature of +5°C for three days, which provides additional clearance from related and ballast substances that precipitate. This gives an increase in the content of the target product is the main biologically active substances the TV flavonoids, phenol carbonic acids, tannins.

To calculate the efficiency of the extraction was determined by the yield of extractives in each stage of extraction, summarized and expected output with respect to the mass of dry material (table.6).

Calculation of percentage yield of extractives to the mass of raw material (Y,%) was performed according to the formula:

where

X is the calculated mass of the dry residue in total in three levels, g, equal 3,3935;

m is the mass of absolutely dry raw material (9,279 g).

The efficiency of extraction of S (%), extractive substances was calculated by the formula:

where

Y - yield of extractives to absolutely dry raw material, %;

E - the content of extractives in the feedstock, %, equal 42,86%.

The efficiency of extraction of raw materials (extracts) is 85,33%.

The authors have conducted studies on the quantitative content of total flavonoids, phenol carbonic acids, tannins, target product, obtained according to the method and offer. Thus, the content according to the method of the amount of flavonoids is 5,12% offer - 6.83 per cent; the amount of phenol carbonic acid by a known method - 3,26% offer - rate of 7.54%; tanning substances by a known method - 11,28% declare - 14,31% (table.12).

The output of zelenog the product by a known method - 20% - 28%.

What's new is that the complex extracted biologically active substances by the proposed method not only has anti-inflammatory and diuretic and antioxidant activity (table.7-11).

Comparative analysis of the proposed solutions and prototype shows that the inventive method differs from the known fact that is used as raw material shoots threshed Spiraea evolites with a particle size of raw material is 2 mm, the Extraction was performed with ethyl alcohol 40% when the ratio of raw materials-extractant 1:14, when the temperature of the extraction 55°C with the following temporary contact phases: 1 contact 120 min, 2 contact 90 min, 3 contact 60 min; insisting on the extraction at a temperature of +5°C prior to filtration that meets the criterion of "novelty".

A new set of essential features provides increased target product by 40% and the expansion of raw materials due to the widespread Spiraea evolites that meets the criterion of "industrial applicability".

In the analysis of known methods revealed that they lack information about the impact of the distinctive features of the proposed method on the achievement of the technical result, therefore, the invention corresponds to the "inventive step".

In the experimentally selected parameter is in the extraction process circuit is composed of the technological process of production of dry extract of the shoots Spiraea epolito (Fig.1).

The optimum conditions for extraction were the basis of the technological process. A specific example of the method.

Description of the process

100 g of air-dry shoots Spiraea evolites with a particle size of raw material 2 mm is placed in the extractor and fill in 1400 ml of 40% ethyl alcohol. The extraction is performed on the magnetic stirrer at a temperature of 55°C. the First contact phase is 120 minutes. Removing merge in the amount of 860 ml (density 0.935 g/cm3). Then hold two more extraction, filling in the extractor 40% ethyl alcohol in an amount equal to the amount drained extraction, and extracted with the second contact of the phases of 90 minutes, when the third contact phase - 60 minutes Receive 500 ml of the second extraction (density - 0,933 g/cm) and 300 ml of the third extract (density 0,931 g/cm).

Extract unite and defend at a temperature of +5°C for 3 days, filtered through Druk-filter.

The filtrate is fed to oparka in a rotary evaporator. Oparka carried out at the temperature of the reaction mixture to 55°C and the pressure 9,81 hPa to 1 liter of the initial volume. The aqueous residue containing biologically active substances, is passed to the separation operation. Get the purified extract in the amount of 420 ml (density 1,039 g/cm3and sediment ballast substances - 6.8 g (humidity 62%), which is not used. Drying is carried out in the spray dryer.

Get the dry extract in the amount of 28 g, which is 28% by weight of air-dry raw material.

The dry extract is a powder from light brown to dark brown color with a faint odor and a bitter, slightly astringent taste.

The parameters of standardization of the final product is a dry extract.

Qualitative detection of biologically active substances:

0.1 g of the dry extract was dissolved in 20 ml of 40% ethyl alcohol by heating on a water bath for 10 min, filtered through a paper filter. To 2 ml of the filtrate add 0.1 g of magnesium powder and 1 ml of concentrated hydrochloric acid; the solution is stirred and heated on a water bath for 5 minutes; gradually appears red staining (flavonoids);

to 0.5 g of the dry extract was dissolved in 10 ml of water, stirred, is heated on a water bath for 10 minutes and filtered. To 2 ml of the filtrate add 2-3 drops of solution salesonlinevuh alum; appears black and green staining (tannins).

Quantitative determination of the amount of flavonoids

Differential UV spectrum of the alcohol solution of the extract in the presence of aluminum chloride has a maximum absorption in the long wavelength region at 412 nm and coincides with the maximum absorption of rutin in complex with aluminum chloride (Fig.2).

About 0.1 g (accurately weighed) of the extract su the CSOs are placed in a flask with a grinding capacity of 100 ml, add 30 ml of 40% ethyl alcohol, the flask is attached to the back of the fridge and heated in a boiling water bath for 15 minutes and Then the flask was cooled to room temperature. The contents of the flask was filtered through a paper filter into a volumetric flask with a capacity of 50 ml and the solution volume was adjusted to 40% ethyl alcohol to the mark, and mix (solution A).

In a volumetric flask with a capacity of 25 ml was placed 1 ml of solution A, add 1 ml of 1% alcohol solution of aluminum chloride and bring the solution up to the mark with 96% ethyl alcohol. After 40 minutes, measure the optical density of the solution in the spectrophotometer at a wavelength of 412 nm in a cell with a layer thickness of 10 mm

As the reference solution using solution consisting of 1 ml of solution A, 1 drop of 10% solution of acetic acid and brought 96% ethyl alcohol to the mark in a volumetric flask with a capacity of 25 ml

Simultaneously measure the optical density of the solution nor routine, prepared similarly to the subject an solution.

The content of total flavonoids rutin and absolutely dry extract in percent (X) is calculated by the formula:

,

where D is the optical density of the test solution; D0- the optical density of the solution nor routine; m is the mass of the extract, g; m0- mass RDF routine, t; W is the loss in weight on drying of the extract in percent.

Note. Preparation of the solution nor routine: about 0.05 g (accurately weighed) nor routine, pre-dried at a temperature of 130-135°C for 3 h, dissolved in 85 ml of 95% ethanol in a volumetric flask with a capacity of 100 ml by heating on a water bath, cooled, quantitatively transferred into a volumetric flask 100 ml capacity, bring the volume of solution in the same spirit to the mark and mix.

The content of total flavonoids in the extract dry 6.83 per cent.

Method for quantitative determination of the amount of phenol carbonic acids in the dry extract of Spiraea evolites.

For the quantitative determination of phenol carbonic acids used the method of direct spectrophotometrically using as a standard sample caffeic acid, since the maximum absorption of the alcohol solution of the extract dried meadowsweet evolites at 325 nm and coincides with caffeic acid.

1 ml of solution A (obtained for the quantitative measurement of the amount of flavonoids) are placed in a volumetric flask with a capacity of 50 ml and the volume was adjusted solution of 95% ethyl alcohol to the mark.

The optical density of the solution is determined on the spectrophotometer SF-46 at a wavelength of 325 nm in a cell with the length of the working layer 1 see as the reference solution using 95% ethyl alcohol.

The total content of phenol carbonic acids in terms of coffee KIS the GTC and air-dry the extract percentage (X) calculated by the formula:

,

where D is the optical density of the test solution; m is the mass of raw material, g; W is the loss in weight on drying of raw materials, %; 782 - specific absorption caffeic acid at 325 nm.

The total content of phenol carbonic acids in the extract dry rate of 7.54%.

The quantitative content of tannins and humidity in the dry extract was determined according to the methods GFH [State Pharmacopoeia of the USSR. - XI ed. - M.: Medicine. So 1, 2 (1987, 1990)].

The content of tannins was 14,31%, the humidity of the dry extract of 4.35%.

Anti-inflammatory activity

Research performed at 60 Wistar rats of both sexes weighing 180-200 g, contained on a standard diet with free access to water and food in vivarium conditions. Studies with animals were conducted in accordance with the "Rules of the European Convention for the protection of vertebrate animals used for experimental and other scientific purposes".

In the experiment used the methodology of the studies anti-inflammatory activity at different stages of inflammation: the accidentals - I. A. Euvino [oivin, I. A. the Methodology for the study of local violations of capillary permeability / I. A. oivin, SL. Setel // materials for the pathogenesis of inflammation and pathology of blood proteins. - Dushanbe, 1961. - T. 49, No. 5. - S. 167-173], exudate - Y. E. Strelnikov [who Strelnikov, Y. C. Comparative characteristics of anti-inflammatory action of some pyrimidine derivatives / Y. S. Strelnikov // Pharmacology and toxicology. - 1960. No. 6 - N-167-173], proliferation - F. N. Trinus [Trios, F. P. non-Steroidal anti-inflammatory drugs / F. P. Trines, N. A. Mokhort, B. M. Klebanov. - Kiev, 1975. - 240 S.]. Dry extract of Spiraea epolito was administered to rats enterline in aqueous solution at a dose of 100 mg/kg rats, rats in the control group received water purified in a volume of 1 ml.

On the impact of the dry extract of Spiraea epolito on the alteration of the tissue and the intensity of the processes of regeneration judged on the dynamics of healing of skin and muscle defect in rats caused by subcutaneous injection in the back area of 0.5 ml of 9% acetic acid with the simultaneous introduction of the dextran solution at a dose of 300 mg/kg weight of the animal. The first injection of the preparations was carried out for 1 hour before injection of acetic acid, then daily 1 time per day for 29 days. 9 and 29, the day of the experiment was estimated area of necrotic tissue by lineation necrosis on the transparent film.

Assessing the impact Spiraea evolites of dry extract on the exudative phase of inflammation was performed by a single injection in the hind limbs of the animals 0.1 ml of 3% formalin. The study drugs were injected 1 hour before the injection, and then through 5 and 18 hours is. Assessment antiexudative activity was calculated by calculating the percentage inhibition of edema compared to control.

When studying the formation of fibrous granulation tissue sterile cotton balls weighing 15 mg implanted rats under the skin in the back under aseptic conditions. Study drugs were administered 1 time per day for 7 days. Then the formed granulomas were weighed on an analytical balance immediately after extraction and after drying (at 70°C for 24 hours to constant weight).

The results of the experiment were statistically processed at a confidence level of 95%.

As can be seen from table 7, the dry extract of Spiraea evolites at a dose of 100 mg/kg anti-inflammatory effect, as evidenced by the decrease in the degree of alteration of the tissue and increase in the intensity of regeneration processes in inflammation. The area of tissue damage on 9 and 29 day decreased by 14.9 and 19.9%, respectively.

Tested dose of the extract dried meadowsweet evolites has antiexudative action, reducing swelling of the paws of animals by 36.5% compared with the control group (table.8).

The results of studying the effect of study drug on the stage of proliferation are presented in table 9.

The percentage stimulation of the formation of granulomas under the influence of dry extract of Spiraea evolites is 3.9%. Stimulation of the formation of granuloma dry extract increases compared with control 1.3 times.

Diuretic activity

Studies were performed on 20 white mice weighing 20 g according to the method of E. B. Burkina [1977]. For research diuretic actions used two groups of animals for 10 mice in each group: experimental, control. In the study of water diuresis in rats kept on a constant diet with free access to water. To water load of animals kept for two hours without food and water. Then the mice were injected into the stomach by means of the probe aqueous solution of the dry extract in the dose of 100 mg/kg the Amount of fluid extract was 2 ml simultaneously with the water load in the amount of 0.3 ml per 10 g of body weight of the animal. Urine was collected every hour for 4 hours. Control group mice received purified water.

Dry extract of Spiraea evolites caused increase of diuresis in animals by 87% in comparison with the control group (table.10), which points to its diuretic activity.

Antioxidant activity

Determination of antioxidant activity of extract dry conducted in vitro in serum donated human blood. To 2 ml of serum was added to 1 ml of the test extract, 0.1 ml of 0.5 M solution of copper sulfate (II), as the inductor FLOOR, and incubated at t=37°C for 16 hours In to what made the experience instead of the test drug was added 1 ml of 0.05 M solution of EDTA (EDTA) as an inhibitor of the FLOOR. [Shavard, A. L. Antioxidant activity of the flora of Altai / A. L. Shavard and [other] // Raises, resources. - 1998. - so 34. - vol.2. - S. 1-8].

Determined the content of the CD and MDA [Goncharenko, M. C. Method of assessing lipid peroxidation / M. S. Goncharenko, A. M. Latinova // Laboratory work. - 1985. No. 1. - S. 60-61].

Dry extract reduced the formation of DK in comparison with the control at 15%, MDA 58% (table.11), indicating that the antioxidant activity of the proposed tools.

Literature

1. Goncharenko, M. C. Method of assessing lipid peroxidation / M. S. Goncharenko, A. M. Latinova // Laboratory work. - 1985. No. 1. - S. 60-61.

2. The state register of medicines on 02.04.2012 [Electronic resource] URL: http://grls.rosminzdrav.ru

3. State Pharmacopoeia of the USSR. - XI ed. - M.: Medicine. So 1, 2 (1987, 1990).

4. Minina, S. A. Chemistry and technology of herbal remedies: the textbook // S. A. Minin, I. E. Kauhava. - M.: GOATER Media, 2009. - 560 C.

5. Oivin I. A. the Methodology for the study of local violations of capillary permeability / I. A. oivin, SL. Setel // materials for the pathogenesis of inflammation and pathology of blood proteins. - Dushanbe, 1961. - T. 49, No. 5. - S. 167-173. Plant resources of the USSR: flowering plants, their chemical composition and utilization. Family Hydrangeaceae-Haloragaceae. - SPb., 1991. - S. 101.

6. Sokolov, S. J. Phytotherapy and phytopharmacology / S. I. Sokolov. - M.: MIA, 2000. - 970 S.

7. With Melnikov, Y. C. Comparative characteristics of anti-inflammatory action of some pyrimidine derivatives / Y. S. Strelnikov // Pharmacology and toxicology. - 1960. No. 6 - N-167-173.

8. Trinus, F. P. non-Steroidal anti-inflammatory drugs / F. P. Trines, N. A. Mokhort, B. M. Klebanov. - Kiev, 1975. - 240 S.

9. Pharmaceutical technology. Technology of medicinal forms: textbook / I. I., Krasnik, Century, Mikhailova, I. C. Denisov, V. I. Woodrow Wilson; edited by I. I. of Krasnica, Century, Mikhailova. - M.: GOATER Media, 2011. - 657 S.

10. The shavard, A. L. Antioxidant activity of the flora of Altai / A. L. Shavard and [other] // Raises, resources. - 1998. - so 34. - vol.2. - S. 1-8.

Table 1
The output of the amount of extractives, flavonoids and phenol carbonic acids, depending on the type and concentration of the extractant
The extractantContent, %
ExtractivesThe amount of flavonoidsThe amount of phenol carbonic acids
Purified water31,490,551,30
Sleep is t ethyl
10%32,110,691,36
20%of 34.401,081,50
30%34,951,171,53
40%35,601,761,69
50%34,161,511,60
60%31,091,541,63
70%28,591,521,60
80%28,931,401,61
90%19,050,751,60

Table 2
OTL the ratio of raw material to the extractant on the yield of extractive substances, flavonoids and phenol carbonic acids
The particle size of raw material, mmContent, %
ExtractivesThe amount of flavonoidsThe amount of phenol carbonic acids
132,351,412,45
236,231,762,66
333,791,222,64
530,760,902,33

Table 3
The yield of extractive substances, flavonoids and phenol carbonic acids, depending on the ratio of raw material and extractant
The ratio of raw material and extractantContent, %
ExtractivesThe amount of flavonoids The amount of phenol carbonic acids
1:835,200,811,98
1:1039,071,20to 2.06
1:1239,321,302,64
1:1440,532,13to 2.67
1:1629,901,952,65

Table 4
Output and extractive substances, flavonoids, phenol carbonic acids, depending on the temperature of extraction
The temperature of extraction, °CContent, %
ExtractivesThe amount of flavonoidsThe amount of phenol carbonic acids
3040,512,14 2,68
4040,762,182,78
4540,822,202,81
5040,942,742,90
5541,162,313,39
6041,182,323,38
6541,172,303,37
7041,192,313,38

Table 5
The yield of extractive substances, depending on the number of stages and time of extraction
Step extractionTime minThe yield of extractives, %
I 6041,16
9043,82
12044,27
15044,26
II6015,77
7516,22
9017,88
12017,79
III3010,83
6010,81
9010,82

Table 6
The results of determining the efficiency of extraction of 10 g of raw material)
Content in raw materials, %Humidity of raw materials, %Step extractionContent in g per stage extractionThe efficiency of extraction, %
Extractives
42,867,2112,5739885,33%
20,64617
30,17332
just three steps3,39347

Table 7
The impact of the dry extract of Spiraea epolito on the alteration and regeneration in acute aseptic inflammation (M±M), n=6
The group of animals9 day29 day
The area of necrotic tissue, cm2The degree of reduction of skin damage, %The area of necrotic tissue, cm2The degree of reduction of skin damage, %
Control (H2O)5,50±0,20-3,26±0,10-
Spirea evalita and 4.68±0,12-14,92,71±0,11-16,9

Table 8
The impact of the dry extract of Spiraea epolito on exudative phase of inflammation (M±M), n=6
The group of animalsThe difference between the volume of inflamed and nevospalennyh feet, mlInhibition of edema, %
Control (H2O)2,44±0,0340
Spirea evalita1,55±0,10-36,5

Table 9
The impact of the dry extract of Spiraea epolito on the proliferative phase of inflammation (M±M), n=6
The group of animalsThe mass of newly formed granulation-fibrous tissue, mgStimulation of the formation of granulomas, %
Control (N2Oh)93,800
Spirea evalita122,78±of 2.51+30,9

Table 10
Diuretic activity of the extract dried meadowsweet epolito (M±M), n=6
ConditionControl (purified water)Extract of Spiraea evolites
The amount of urine, ml1,5±0,12,8±0,05
Increased output in comparison with the control+87%

Table 11
Antioxidant activity of the extract dried meadowsweet epolito (M±M), n=6
Conditions of experienceControlDry extract of Spiraea evolites
Diene conjugate (DC), the Optical unit3,98±0,13,39±0,1
The degree of reduction of the level of DC % -15%
Malonic dialdehyde (MDA), µm/mlmin2,15±0,11,71±0,05
The degree of reduction in MDA level, %-58%

Table 12
Comparative characteristics of the claimed method with the selected prototype
№ p/pOption compareThe known methodThe claimed method
1Vegetable raw materialsThe leaves of the wild strawberryShoots Spiraea evolites
2The extractantPurified waterEthyl alcohol 40%
3The ratio of raw material and extractant1:101:14
4The degree of grinding of raw material, mmfrom 1 to 32
5The temperature of extraction, °C7555
6The duration of the contact phase in minutes:
- first contact30120
the second contact3090
the third contact3060
7Defending at +5°C, 3 days-+
8The yield of the target product, %2028
9The content in the dry extract of total avonoids %5,126,83
10The content in the dry extract of the amount of phenol carbonic acids, %-7,54
11Soda is the content in the extract dry tannins, %-14,31
12Pharmacological action
- anti-inflammatory++
- diuretic++
- antioxidant+

The method of obtaining funds that have anti-inflammatory, diuretic and antioxidant activity, including grinding shoots Spiraea epolito, representing a mix of leaves, flowers and twigs no thicker than 3 mm, to a particle size of 2.0 mm, triple extraction method fractional maceration 40% ethyl alcohol in the ratio of raw materials - extractant 1:14, at a temperature of 55°C, stirring at the insistence, the first contact of the phases is 120 minutes, then removing the merge, spend two more extraction, filling of ethyl alcohol in the amount equal to the slit extraction, the second contact phase is 90 minutes, the third contact of the phases is 60 minutes; extract unite, defend during the day, filtered, concentrated, sephirot, dried.



 

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56 cl, 7 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, particularly to a method for recovering pinosylvin and methylpinosylvin from common pine (Pinus sylvestris) wood. The method for recovering pinosylvin and methylpinosylvin consists in extracting ground knots of common pine (Pinus sylvestris) wood, common pine (Pinus sylvestris) in isopropyl alcohol mixed with water, separating the extract and removing the solvent.

EFFECT: method enables a higher yield of pinosylvin and methylpinosylvin from common pine (Pinus sylvestris) wood.

3 cl, 5 ex, 2 dwg

FIELD: medicine.

SUBSTANCE: agent possessing the anti-inflammatory, antipyretic and antimicrobial action representing a dry extract of drug hedge hyssop leaves and blossom by grinding them, extracting in 96% alcohol on a water bath to a boil, and boiling, evaporating, diluting the evaporated residue by distilled water first, adding chloroform then, cooling to a room temperature and centrifuging, separating a water fraction and drying it in the certain environment.

EFFECT: agent possesses the pronounced anti-inflammatory, antipyretic and antimicrobial action.

5 dwg, 5 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry, in particular to a medication, possessing a nephroprotective action. The medication with the nephroprotective action, contains an extract of grass with roots and rhizomes of slender-leaf iris (Iris tenuifolia), stabilising agents and preservatives, taken in a certain ratio, where the extract is obtained by extraction of the grass with roots and rhizomes of slender-leaf iris (Iris tenuifolia) with a 30-70% water solution of polyol.

EFFECT: medication possesses an effective nephroprotective action.

3 cl, 3 dwg, 7 tbl, 14 ex.

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry, namely to a method of obtaining a preparation, possessing an antimicrobial activity. The method of obtaining the preparation, possessing he antimicrobial activity, where an aboveground part of freshly harvested bear leek (Allium ursinum L.) or victory onion (Allium victoriale L.) is crushed to a paste-like state, poured with ethyl alcohol, infused tree times, under certain conditions, after each extraction the extracts are poured off, the obtained extracts are combined.

EFFECT: medication, obtained by the claimed method, possesses an expressed antimicrobial activity.

2 cl, 1 tbl, 6 ex

FIELD: food industry.

SUBSTANCE: method involves raw material milling, extraction of useful substances, filtering and drying. The method characterisation is as follows: extraction is performed in an ultrasonic bath with a food acid with concentration not in excess of 5% in conversion to adipic acid at a temperature of 20-40°C during 15-30 min while drying is performed by high-temperature spraying method at a temperature of 70-100°C in a flow of extract ensuring production of a powered product. The food acid may be represented by adipic, orthophosphoric, malic, ascorbic, amber or acetic acid.

EFFECT: method enables production of powered preparations of non-fruit sea-buckthorn parts with high serotonin content.

2 cl, 1 tbl, 1 ex

FIELD: agriculture.

SUBSTANCE: method of complex processing of rice production wastes in the form of rice hulls and straw comprises preparing raw material by screening hulling bran or dust and washing with water, processing the prepared raw material to produce a solid phase and solution of organic compounds, at that in preparing the raw material the rice straw is crushed, the prepared raw material is treated with 0.5 N ammonium oxalate solution, the solid phase is separated from the solution by filtration and sent to the recovery of silicon-containing products, the filtrate is dialyzed against running water and then against distilled water, concentrated, treated with acetone or alcohol, the resulting precipitate is separated by centrifugation, dissolved in water and lyophilized to obtain the polysaccharides under certain conditions.

EFFECT: method enables to increase the number of target products extracted during processing of rice production wastes, to improve environmental security of production by minimizing the amount of wastes, while simultaneous expanding the resource base through the use of rice straw.

4 cl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and can be used as a hepatotrophic, lipotropic agent in gastroenterology, as well as for treating cardiac and cerebral atherosclerosis, in neurology in the lower extremity artery diseases (endarteritis). The agent contains tabletted powders of diisopropylammonium dichloroacetate, microcrystalline cellulose, lactose and excipients presented by Aerosil, Primogel and calcium stearyl fumarate.

EFFECT: agent possesses no toxicity, has the high adsorption properties, the apparent anti-inflammatory action, and provides metabolism and the liver regeneration.

3 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to heterocyclic compound - 6-methyl-5-morpholynomethyl-1-(thiethan-3-yl)pyrimidine-2,4(1H,3H)-dione of formula 6-methyl-5-morpholynomethyl-1-(thiethan-3-yl)pyrimidine-2,4(1H,3H)-dione of formula: .

EFFECT: novel compound, possessing antioxidant activity, is obtained.

2 cl, 6 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and concerns a pharmaceutical composition for treating gastroduodenal ulcer in the form of tablets, capsules or gel, containing therapeutic agents and a consistency base applicable for each dosage, wherein the therapeutic agents are as follows: recombinant interferon specified in a group: recombinant interferon alpha, recombinant interferon beta, recombinant interferon gamma; antiseptics; amino acids specified in a group: arginine, histidine, lysine, cysteine, methionine, glutamic acid; and antioxidants specified in a group: beta-carotene, vitamin C, vitamin E.

EFFECT: invention has the integrated body effect promoting faster healing of the mucosal defect accompanying the aggravated gastroduodenal ulcer and preventing recurrences, including by the eradication effect.

6 cl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and concerns a pharmaceutical composition in the form of tablets for oromucosal administration in treating infectious-inflammatory oropharyngeal diseases. The composition contains recombinant interferon specified in a group: recombinant interferon alpha, recombinant interferon beta, recombinant interferon gamma; amino acid specified in a group: arginine, histidine, glycine, glutathione, lysine, methionine, cysteine; an antiseptic, a preserving agent, flavours specified in a group: tea tree oil, eucalyptus leaf oil, mint leaf oil and a consistence base.

EFFECT: invention makes the composition applicable in fragile and frequently ill patients for reducing a disease recurrence.

7 cl, 1 ex

FIELD: food industry.

SUBSTANCE: biologically active food additive strengthening the organism adaptive power and body defences and having anti-inflammatory and antioxidant activity contains vegetal origin components represented by a complex extract of devil's-club root, Rhaponticum carthamoides root, Hedysarum neglectum Ledeb root, celery roots and leaves, rhodiola rosea root, Japanese angelica tree roots, boschniakia rossica roots, Hungarian sainfoin herb, magnolia-vine fruits; additionally the additive contains chitosan, trepang fermentative hydrolysate, ascorbic acid, taurine, glutathione, nicotinamide, vitamin B1, vitamin B2, vitamin B6, vitamin B12, folic acid, anhydrous calcium chloride, magnesium chloride, zinc chloride, bee honey at preset ingredients ratio.

EFFECT: biologically active food additive promotes effective strengthening of the organism adaptive power and body defences and human aging retardation.

4 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: invention relates to medical radiology and can be used for prevention of cerebral form of acute radiation sickness. Claimed is application of officinal drug pyrazinamide as medication for prevention of cerebral form of acute radiation sickness. Pyrazinamide has been used for treating tuberculosis.

EFFECT: preventing in 100% of cases development of early temporary incapacity in case of irradiation in dose 200 Gy, improvement of indices of behavioral and research activities in irradiated animals, in reduction of frequency of motor disorders, reduction of frequency and expression of convulsive-hyperkinetic syndrome and 9,5 fold increase of average life expectancy of irradiated animals Pyrazinamide is not inferior to drug - nicotinamide prototype in efficiency of radioprotective action.

4 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a composition possessing the antioxidant and antibacterial activity and containing lithium ascorbate, differing by the fact that it additionally contains lithium benzoate in the following proportions, wt %: lithium ascorbate - 50; lithium benzoate - 50.

EFFECT: invention provides extending the range of antioxidants with antibacterial activity possessing normothymic activity.

1 ex, 2 tbl

FIELD: medicine.

SUBSTANCE: method for increasing the antitoxic body function in healthy individuals occupied in the chemical load environment involving administering an antioxidant water containing carrot juice, cod liver oil, olive oil, honey; the water is taken daily before the working shift for 10 days.

EFFECT: using the invention enhances the antitoxic body function by administering the water having high antioxidant properties.

1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is described is using a pharmaceutical composition in the form of an orally disintegrated tablet containing 6-methyl-2-ethyl-3-hydroxypyridine succinate as an active substance and crospovidone as a disintegrating agent in ratio 2:1 respectively, as a motor stimulating and anorectic agent.

EFFECT: preparing motor stimulating and anorectic agent.

16 dwg, 34 tbl, 13 ex

FIELD: medicine.

SUBSTANCE: for the purpose of post-surgical treatment of cerebral tumours, memantine is prescribed in a dose of 10 mg daily for 5-7 days before radiation therapy, and in a dose of 20 mg during radiation therapy 4-6 hours before the radiation session. On completing the course of radiation therapy, memantine is prescribed in patients aged up to 60 years old in a dose of 10 mg for 2-3 months daily, in patients aged 60 and older in a dose of 20 mg for 5-6 months daily.

EFFECT: method enables providing the higher patients' quality of life with a view to cancellation of glucocorticoids, ensuring higher clinical effectiveness ensured by an increase of the medullary substance to radiation.

2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a controlled-release preparative form of diacerein administered once a day for treating or autoimmune diseases or their complications. The preparative form contains a core, an active layer, a sustained-release film layer and a delayed-release film layer, wherein the active layer is followed by the sustained-release film, and the delayed-release film layer thereafter. The sustained-release film layer contains ethyl cellulose polymer, povidone, triethylacetate and talc; the delayed-release film layer contains Eudragit polymer, triethylacetate and talc.

EFFECT: reducing the negative side action of diacerein.

18 cl, 23 ex, 33 tbl

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