Method for preparing sown coriander herb dry extract possessing anti-stress, sedative, nootropic and hypotensive effect

FIELD: pharmaceutical industry and technology, pharmacy, medicine, phytotherapy.

SUBSTANCE: method involves three-times extraction of milled coriander herb with 40% ethyl alcohol taken in the ratio raw : extractant = 1:5 for 1 h in each extraction step. Extracts are combined, filtered, ethyl alcohol is removed and prepared aqueous residue is kept at temperature +10°C, not above, for 5 h, not less. Deposit is separated, aqueous extract is dried and the end product is prepared. Invention provides realizing the indicated designation.

EFFECT: improved preparing method.

5 tbl, 2 dwg, 1 ex

 

The invention relates to the pharmaceutical and medical industry and the receipt of a dry extract of the herb coriander seed, which has strong anti-stress, sedative, neuroprotective and anti-hypertensive effects.

It is known that a decoction of the herb coriander in folk medicine used in neurasthenia. Close the active extracts of Valerian, so they are used as sedatives in increased nervous excitability and cardiovascular neurosis. However, their anti-stress activity is expressed less than a sedative.

Known methods for producing extracts of Valerian. So, in the way described (A.S. No. 187234, CL AC 35/78), to obtain the tincture of Valerian roots, the last one before the extraction is treated with a solution of sodium bisulfite.

According to another method (Application Germany No. 2230626, CL AC 35/78) drug Valerian get extragere the roots of the lower lipophilic solvents, with the subsequent removal of solvent in vacuo and dissolve the residue in a polyhydric alcohol, fatty or essential oils or their mixtures in the ratio of raw materials and finished extract 1:1.

In the method of obtaining soluble extracts (Application Germany N 3715070, CL AC 35/78) 1 t Valerian root cleaned and chopped add 1800 l of water, extracted by heating, the precipitate of hoteltravel the t and get 1400 l of the extract product, which is dried in a known manner.

In the method of obtaining pharmacologically active funds (Japan's Bid No. 1-246211, CL AC 7/06) vegetable raw materials - mixture of 3 plants, including the roots of Valerian, treated with water-soluble organic solvent, for example methanol, ethanol, propanol, butanol, acetone and other or their aqueous solutions and get further therapeutic agent.

All these methods have the following major drawbacks:

none of these tools has not simultaneously and anti-stress, and nootropics, and antihypertensive effect.

- use as extractants lipophilic organic solvents;

- polyhydric alcohol glycerol;

- toxic organic solvents, methanol, butanol, and others;

- the need for regeneration of these solvents with regard to environmental requirements;

significant energy costs associated with grinding.

The closest analogue and a prototype for the proposed object is a method of obtaining a dry extract from Valerian, having a sedative effect (Patent RU N 2098115). This method consists in the extraction of raw materials 65-75%aqueous ethanol at a ratio of raw materials - extractant (1:4-6) filtration method, with subsequent evaporation, the Department of adca and drying of the target product.

The novelty of the invention lies in the fact that it is based on the technical problem of obtaining a dry extract of the herb coriander seed, characterized by a pronounced anti-stress, sedative, neuroprotective and anti-hypertensive activity. It is important to note that Valerian preparations nootropic effect is not characteristic. Another hallmark of the inventive object is the feature that used for extraction 40% aqueous ethanol, which makes it possible to extract the active ingredients, providing the above pharmacological properties. The criterion of novelty is the fact that to achieve the purpose above-ground part of the food plants of coriander seed. The apparent novelty of the proposed method demonstrates the creative nature of the decision, i.e. speaks about the relevance of the proposed solutions to the requirement of "singularity" and "primary".

The technical result is obtained in the course of solving the task, expressed through the use of new raw materials - grass coriander seed, related to the widely used food plants, as well as, in contrast to fruits, almost not used in scientific medicine.

Information confirming the possibility of implementation of the invention consist in the following:grass, collected during flowering in June - August, dried in shade, ground and passed through a sieve with the hole diameter 5 mm, the material is extracted with 40% aqueous ethanol in a flask at the temperature of boiling and stirring (multiplicity extraction - 3 time - 1 h from the beginning of the boil when the ratio of raw materials - extractant 1:5). The obtained extract was filtered while hot and accordingly unite. Spirit aqueous extract is evaporated in a vacuum to remove the alcohol. The resulting concentrate is maintained at a temperature not exceeding +10°With at least 5 hours. After settling separated resinous lipophilic substances with decanting and filtering. Purified water fraction is dried and obtain the target product.

Example. 20,0 kg of dried and crushed herbs coriander seed (particle size 5 mm) is loaded into the extractor macerating type dense layer. Raw material in the extractor at a temperature of 70°treated under stirring 40%aqueous ethanol within 2 hours. The extraction process is carried out at a ratio of raw materials - extractant 1:4, the ratio of extraction - 3. The selection of the extract is carried out by vacuum filtration with an average rate of about 15 l/h

The obtained extract was evaporated at a temperature of 70-80°and the residual pressure in the apparatus of 0.1-0.2 kgf/cm2to remove the C extract ethanol and getting about 25 l of concentrate.

The concentrate is transferred into the tank-the tank, which is covered with a lid and place in the refrigerating chamber, where it was incubated for 5 h at a temperature of +10°C.

Separated from the mother liquor resinous mass containing chlorophyll, carotenoids and other lipophilic substances, is localized at the surface of the solution or on the walls of the sump. It is separated by decantation and then the mother liquor is filtered on a suction filter through the layers of calico and paper.

The resulting aqueous filtrate is dried by spray drying type radar-10. The yield of the target product of 23.5%.

The obtained target product quality standartized method for quantitative spectrophotometry according to the content amount of flavonoids and coumarins, as well as other quality indicators.

As a result of implementing the proposed method uses a new type of vegetable raw grass coriander seed, which was not previously used. This contributes to the expansion of raw materials and integrated use of valuable plant materials coriander.

The study of the pharmacological activity of the obtained extract

The experiments were conducted on rats male Wistar weighing 200-220 g, bred in the vivarium of the Pyatigorsk state pharmaceutical Academy. The animals were kept in stationary conditions of the vivarium, received standard the Orme and water without restrictions. Participated in experiment experimental and control groups [guidelines for the quality assessment of laboratory animals for biomedical research (compilers Amespace, Rphmedia) - M., 1985. - 63 S.].

To create a stressful situation used a model of chronic adrenaline intoxication [Uwire, Avitamin. Energy metabolism in the arteries and veins in the conditions of the simulation adrenal lesions of the vascular wall. // Physiopathology. - 1989. No. 3, p.63-65]. The solution of epinephrine hydrochloride rats were injected intraperitoneally once daily at a dose of 100 mg/kg in two months.

After a 2-week injection of adrenaline experimental group were administered an aqueous solution of the dry extract of the herb coriander in a dose of 50 mg/kg orally once daily for 45 days. The control group in the equivalent volume was administered isotonic sodium chloride solution of 0.9%.

At 14, 30 and 60 day experiment recorded the neurological status of the animals: animal behavior in Open field (MRF) [Alarmel. Factor analysis of the behavior of rats in the open field test. // Ukr. the Supreme. a nerve. activity them. Pavlova. - 1988. - THHH. - Vol.5, s-863, K.V. Sudakov. Normal physiology. - M.: MIA, 1999, s-197, Saitou. Role orientirovannogo and defensive components in the behavior of white rats in the "open the field". // Ukr. the Supreme. a nerve. activity them. Pavlov, - 1980. - THHH. - 4 s-708] and evaluated the cognitive function test conditional reaction passive avoidance (passive avoidance reaction) [Abuses. Techniques and basic experiments for the study of brain and behavior. - M.: Higher school, 1999, 399 S.].

The conditioned reflex of passive avoidance was formed by the impact of the current 40 C. what animals were placed in the center of a square box. The box was put in charge of a small dark compartment, the floor of which was made of metal plates, connected to the current generator. After the subjects moved to a smaller room, they were shocked. In this way they developed a reflex to the entrance to the room, reminiscent of a hole, while (C) was recorded by stopwatch.

On the 60th day of the experiment recorded the change of time sleeping under the action of nematalosa anesthesia in a dose of 25 mg/kg [Manual on experimental (preclinical) study of new pharmacological substances. - M.: 2000. - 398 S., Sarnow L.N., Hazura CENTURIES, Elements of experimental pharmacology. - M.: 2000. - 352 S.].

Experiments to study the effect of the extract on the cardiovascular system were carried out on two other groups of animals, which the extract was administered orally for months at a dose of 20 g/kg and the control group was injected with saline in the equivalent volume. System artery is the emotional pressure (SBP) was measured in the carotid artery using a mercury manometer on anesthetized animals (urethane-chloralose 500 mg/kg and 50 mg/kg, respectively).

Study of acute toxicity, by definition LD50conducted according to the method of Cerberus in mice.

The obtained results of the experiments the data were processed statistically. The results in the tables are presented as mean values with confidence intervals (M±m) or standard deviation. The validity of the results was determined using t-student criterion [Polyakov, I.V., Sokolov NS Handbook on medical statistics. - L.: Medicine, 1975. - 152 C. Guidance on experimental (preclinical) study of new pharmacological substances. - M., 2000. - 398 S.].

The results and conclusions.

Studies of acute toxicity can take this extraction to the 4th class of danger according to GOST 12.1.007-76 or practically non-toxic substances according to the classification Sidorov, K.K. (1973) [Sidorov, K.K. ON the classification of the toxicity of poisons parenteral routes of administration // Toxicology of new industrial chemicals - M.: Medicine, 1973. - 475 C., Div. On the harmonization of domestic and international classifications of acute toxicity of chemical compounds / Toxicological Bulletin. No. 6 (November-December) 2004. - p.3.]. The calculated value LD50in our experiments was 5166,7±167,9 mg/kg [Makarova L., Nersessian SM TO the creation of medicines on the basis of Corian is RA seed. // Youth international medical Congress. St. Petersburg, 2005, s-155].

In the experimental group of animals without treatment, the disorder of cognitive functions was recorded in the fourth week of the experience, which survived until the end of the experiment. Therefore, the course introduction of epinephrine hydrochloride leads to disruption of cognitive functions (table 1).

The experimental animals developed a conditioned reflex firmly maintained throughout the experiment. As evidenced by the absence of the entry of animals into the dark compartment. The obtained data are presented in table 1.

Dynamics of indicators characterizing the behavior in the open field, shows that after a month of the experiment, the control group of animals decreased locomotor (average 66.2%) and research activity (53.3 percent). Violation of behavioral responses is maintained throughout the entire time of the experiment (table 2 and Fig. 1 and 2).

In the experimental group of animals to the end of the experiment, we also observed a decrease in locomotor activity, as evidenced by the decrease in the number of crossed squares (table 3 and figure 2). It should be noted that in the experimental group after two months of increases, the time spent by the animals in the center of the arena. This trend indicates a lower level of anxiety.

When is the analysis time of the sleep set, administration of the extract significantly inhibits the prolongation of sleep under the influence of anesthesia. The data obtained are presented in table No. 4.

The table shows that the experimental animals sleep a lot less than in the control group, and is approaching a time of sleep in the intact animal. Latent sleep time animals are equal.

Also found that the course introduction of the investigated extract leads to a decrease of the GARDEN. On average, 30 day experiment GARDEN is 98.3±5,7 mm Hg [Nersessian SM, Makarova L. Experimental study of the effect of exchange rate injection of extracts of the herb coriander seed on cerebral blood flow and systemic blood pressure // Youth science and modernity. Part II. The Kursk, 2005, pp.118-119].

Thus, pharmacological research suggests that the dry extract of the herb coriander has the above-mentioned pharmacological effects.

For a detailed study of the composition of the phenolic compounds obtained extraction we used the method of high performance liquid chromatography (HPLC). For analysis by HPLC - about 0.1 g (accurately weighed) of the extract was placed in a volumetric flask with a capacity of 25 ml, was added 20 ml of distilled water and placed in an ultrasonic bath and stirred while the temperature is round 50° C for 15 minutes. The solution volume was brought up to the mark with the same solvent (solution A), 1 ml solution was placed in a volumetric flask with a capacity of 25 ml and made up to the mark with mobile phase (test solution).

Chromatograph conditions were as follows

The analysis was performed on the high performance liquid chromatograph firm "GILSON" (France) (model 305) manual injector RHEODYNE-7125 (USA) with subsequent computer processing of the results of the study, using the program "Multichrome" for "Windows". As stationary phase was used metal column 4.6×250 mm PLATINUM EPS C18, 100, particle size 5 m.

As the mobile phase methanol-water-phosphoric acid is concentrated in the ratio of 400:600:5. The analysis was carried out at room temperature. The feed rate of eluent 0.5 ml/min analysis time 170 min Detection was carried out using a UV detector, GILSON UV/VIS model 151, at a wavelength of 254 nm.

In parallel was preparing a series of 0.05% solution comparison in 70% ethyl alcohol. 20 l sample solution and solutions comparison was injected into the chromatograph and chromatographically. Identification of the separated substances was performed by comparing retention times of the peaks obtained in the chromatogram of the sample, with retention times of standard solutions (RIS). Quantitative determination identified the substance in the sample was performed according to the peak areas, using the method of internal standardization.

As a result of the research we obtained 40% fraction of the herb coriander seed has been allocated 43 substances, of which identified 20 connection polyphenolic nature, which consists mainly of flavonoids, coumarins and derivatives of phenol carbonic and organic acids. It was found that substance coumarin nature in the greatest quantity are dikumarina, 4-oksikumarin, scopoletin, umbelliferone, esculin and esculetin; of flavonoid compounds - orientin, vitexin, diosmin, chrysoeriol, hesperidin; derived from phenol carbonic acids predominates ferulic and Gallic acid. The results presented in table No. 5.

It should be noted that the predominant component is Gallic acid. Such compounds as Gallic acid, arbutin, esculin, esculetin, diosmin, salicylic acid, orientin, dihydroquercetin, scopoletin, luteolin-7-glycoside, hyperoside, hesperidin, 4-oksikumarin, umbelliferon, vitamin, catechin, luteolin and apigenin were first identified in the grass coriander seed.

Thus, the study has found that the dry extract of the herb coriander seed contains a wide range of biologically active substances of polyphenolic nature. The floor of the obtained data testify to the significance of this object not only from a chemical point of view, but with the pharmacological serve as base material, proving the effectiveness of this extract as a preventive agent for various diseases.

Table No. 1
The latent time of the entry of animals into the dark compartment
Group/timeThe control group,Experienced group
The source data26,1±12,132,9±? 7.04 baby mortality
After 14 days--
After 4 weeks58,2±6,3*-
After 8 weeks45,0±1,3*-
Note: *significant differences (p>0,05) relative to the original data,

the "-" symbol to the lack of animals entering the dark compartment

Table No. 2
The performance behavior of the control group in the "open field"
Indicators/time issled.The source dataAfter 4 weeksAfter 8 weeks
Cal in cross channel. squares57,0±8,527,3±4,8* 6,2±1,6*
2. Upper rack11,2±2,3*6,1±1,30,5±0,1*
Hiring2,5±0,71,4±0,3*0,3±0,1*
4. Columns1,9±0,8*0,72±0,3*1,0±0,1
5. Peeking in the hole0,3±0,13--
Note: * significant differences (p>0,05) relative to the original data,

"-" denotes the absence of zaglyadyvanie

5. Ogladania in apertures
Table No. 3
The performance behavior of the experimental group in the "open field"
Indicators/timeThe source dataAfter 4 weeksAfter 8 weeks
Cal in cross channel. squares50,6±7,824,5±3,6315,0±4,6
2. Upper rack7,7±2,473,12±1,21,78±0,91*
3. Grooming3,0±1,04*1,8±0,5*0,89±0,13
4. Columns3,6±1,041,34±0,47*0,89±0,26*
0,3±0,13*0,2±0,110,3±0,12*
Note: * significant differences (p>0,05) relative to the original data

Table No. 4
Sleep under the influence of anesthesia
The group of animalslatent sleep time, minsleep time, min
The control group4,9±0,39112,3±9,4*
Experienced group4,7±0,52*60,3±5,9
The intact group4,5±0,5248,25±4,42*
Note: * significant differences (p>0,05) relative to the original data

Table No. 5
Polyphenolic compounds of the extract of the herb coriander
Identified connectionsRetention time, minProportion, %
Ferulic acidby 5.877,24
Gallic acid6,213,51
Chrysoeriol 17,055,55
Esculin7,32,7
Diosmin8,66,27
The dikumarina7,86,84
Esculetin9,91,94
Vitexin12,94,76
Orientin15,410,71
Scopoletin22,032,03
Hyperoside25,70,33
Rutin28,91,06
Hesperidin33,23of 5.29
4-oksikumarin34,892,11
Umbelliferon36,951,4
Vicenin40,360,83
Catechin72,00,13
Luteolin85,070,14
Apigenin99,550,22
Quercetin68,050,13

The method of obtaining anti-stress, sedative, hypotensive and nootropic agents from plant material, characterized in that the extraction spend 40%ethyl alcohol and as a source of raw materials is sportsouth grass plants coriander seed, raw materials are crushed and extracted three times with 40%ethyl alcohol at boiling temperature and constant stirring, the ratio of raw materials - extractant 1:5, for 1 h at each extraction, then extract combine, filtered while hot, the spirit of faction is removed under vacuum and the resulting aqueous residue is maintained at a temperature not exceeding +10°With at least 5 h, after settling separated resinous substances by decantation-filtration, purified water extract is dried and obtain the target product.



 

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12 cl, 1 tbl, 16 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention describes a pharmaceutical system for oral delivery of antioxidants, vitamin C and vitamin E. The delivery system comprises vitamin C in the amount providing delivery of the daily dose corresponding to 60 mg - 2 g of vitamin C, and comprises vitamin E in the amount providing delivery of the daily dose corresponding to 50 mg - 500 mg of α-tocopherol. Also, this delivery system provides the ratio of concentrations vitamin C and vitamin E in blood plasma in the range from 1:1 to 3:1, and wherein the solubility of vitamin E provides dissolving 90% of vitamin E for less in 30 min. The dissolving index is measured by heating at 37°C in 15 ml of water in the prescribed time intervals followed by decantation of the dissolving medium, washing out with 25 ml of 25% ethanol, combining the dissolving medium and decanted ethanol and measurement of the content of vitamin E in combined media for dissolving in ethanol, and wherein the solubility of vitamin C is so under conditions of the Test A that its dissolving after 1 h is less then 40% of vitamin C and wherein this test for solubility satisfies the order for the European Pharmacopoeia 711, and wherein administration of the indicated delivery system enhances the concentration of blood plasma vitamin E up to at least 20 mcmole/l, and the concentration of vitamin C to at least 40 mcmole/l. Also, invention represents methods for treatment including administration the claimed pharmaceutical system to a patient. The concentration and the ratio of these antioxidants corresponding to the stationary state of these antioxidants as was found are to be essential for prophylaxis and treatment of disorders associated with oxidative loading, such as arteriosclerosis, diabetes mellitus and damages of the nervous dystrophy type as Alzheimer disease.

EFFECT: improved and enhanced properties of pharmaceutical delivery system.

33 cl, 9 tbl, 3 dwg, 5 ex

FIELD: organic chemistry, pharmaceuticals.

SUBSTANCE: invention relates to new chemical compound of general formula I , or salts, or hydrates thereof. In formula I R1 represents group of formula -G1-R1a (wherein G1 represents single bond, oxygen, sulfur; R1a represents C1-C10-alkyl optionally substituted with halogen or C3-C8-cycloalkyl); R2, R3 and R4 are independently hydrogen or -G20-R20 (wherein G20 represents single bond, oxygen, sulfur, sulfinyl or sulfonyl; R20 represents C1-C6-alkyl optionally substituted with 1-3 halogen atoms or C3-C8-cycloalkyl); R5 and R6 are independently -X5-X6-X7 group (meanings of X5, X6 and X7 are as defined in specification) or R3 and R4 may together form pyrrol ring optionally substituted with C1-C6-alkyl; Ar represents phenyl, 1,3-benzodioxolyl, naphthyl, pyridyl, optionally substituted with 1-3 substituents (as defined in specification) Compounds of formula I has antagonistic activity in relates to receptors of corticotrophin releasing factor (CRF). Also disclosed are compounds, characterized by preferable structures, pharmaceutical compositions, using such compounds, intermediates for production thereof and method for treatment of various diseases mediated by CRF.

EFFECT: new compounds as antagonists of CRF receptors.

33 cl, 1 tbl, 316 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to using compounds of the general formula (I): and their pharmaceutically acceptable acid-additive salts. Compounds are used for preparing medicinal agents used in treatment diseases and state associated with system of adenosine receptors A2A, such as Alzheimer's disease, Parkinson's diseases, Huntington's syndrome, schizophrenia, anxiety state, pain, depression, narcomania to such substances as amphetamine, cocaine, opioides, ethyl alcohol, nicotine, cannabinoids, or in treatment of hypoxia, ischemia, epileptic attack. Also, proposed compounds exert neuroprotective effect and can be used as sedative, antipsychotic or anti-epileptic agents.

EFFECT: valuable medicinal properties of compounds.

18 cl, 1 tbl, 49 ex

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