A method of obtaining a total of substances with choleretic, hepatoprotective, hypocholesterolemic activity (options)

 

(57) Abstract:

The invention relates to the pharmaceutical industry. The herb Astragalus aspercentage extracted with 30%, or 50%, or 70% ethanol at 60 - 65C with a ratio of phases 1:10. Evaporated to 1/3 volume under vacuum. Removal of lipophilic substances are defending at a temperature of 2 - 4C for 48 hours Drying is carried out in a vacuum drying Cabinet at 40 - 45C and a pressure of 300 to 400 mm RT.article The invention allows to Podesite yield, increase activity, reduce costs. 3 C. p. F.-ly, 4 PL.

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

Known methods for producing from plants of the genus Astragalus polyphenols that have choleretic (the Method of obtaining the amount of polyphenols that have choleretic activity. A/C 1737796, 28.03.90) hepatoprotective, choleretic, anti-oxidant and analepticheskih activity (the Method of obtaining the amount of flavonoids with gipoazotemicescoe action. A/C 1768898/31-16, 25.01.75; the Method of obtaining the amount of polyphenols that possess hepatoprotective, choleretic, anti-oxidant and analepticheskih activity. Patent 2018315 from Hanoi activity. However, reports of choleretic, hypocholesterolemic, genatossio, antioxidant activity for total extracts from Astragalus is not detected, and A. Onobrychis L. has not been studied at all, although it is known about the use of it in folk medicine (farm Laborer, E. , E. N. Popov, I. N. Fursa New drugs of plant origin. Kiev, 1959; Stepashkin K. I. Astragalus and its application in medical practice. Kiev, 1960).

Describes how to get the total products with hepatoprotective, choleretic action of other plants. For example, zelibor used as a hepatoprotective agent (the Method of obtaining polyphenolic Romanov. And/603386), and the amount of polyphenolic compounds from herbs Wiki sowing has choleretic activity (the Method of obtaining the amount of polyphenolic compounds with choleretic activity. A/C 1018641, 16.12.81).

The method of producing celebra consists in extracting, milk Thistle 80% ethanol, followed by evaporation and dissolution of the residue in 50% ethanol. The solution process at the beginning of carbon tetrachloride, then a mixture of chloroform-ethanol 2:1. The organic phase is evaporated and dried, yielding the desired product with a yield 4,50 - 5,0% on raw, however, is new. AND/603386).

A method of obtaining the amount of polyphenolic compounds (flavonoids, oksikorichnye acids, oxycodeine), has choleretic activity by extraction with 30% hydrolysis alcohol grass common Vetch (Vicia Sativa L.) at 70oC. Water-alcohol extract evaporated and treated with 96% ethanol, the precipitate is filtered off, the filtrate is evaporated in vacuo and dried. The specific effect of the drug is one-way (the Way of getting the amount of polyphenolic compounds with choleretic activity. A/C 1018641, 16.12.81).

As a prototype the selected method of producing polyphenols from Astragalus burovskogo, which possess hepatoprotective, choleretic and antioxidantes activity. 1 kg of air-dried powdered raw materials are placed in a reactor and exhaustively (5 times) extracted with 80% ethanol in the ratio of raw material and extractant 1: 5 when heated to 70oC. United alcoholic extract (23,8 l) evaporated in vacuum at a temperature of 70 - 80oC to 300 ml and purify the residue is 10 times 100 ml of chloroform from chlorophyll, lipids and other dietary fibers. Then the purified fraction exhaustively extracted 10 times with 100 ml ethyl acetate. An ethyl acetate extract summarize, dried only 5-fold volume of dry chloroform. The precipitate was separated on a glass filter N 2 - 4, dried in a drying Cabinet at 60oC for 12 h Output amounted to 5.9% and 6.2% (the Method of obtaining the amount of polyphenols that possess hepatoprotective, choleretic, anti-oxidant and analepticheskih activity. Patent 2018315 from 22.01.92).

However, the known method does not provide a drug consisting of polysaccharides, flavonoids, oksikorichnye acids, saponins, oxycodeine speed-increasing bile secretion, and does not allow to obtain a sufficiently high yield of product.

The objective of the invention is to increase the yield of the target product, increase activity, reduce costs, obtaining substances containing different groups of biologically active substances.

The problem is solved by the fact that, according to the method of obtaining the amount of amino acids, polysaccharides, oxycodeine, polyphenols, saponins has choleretic, hepatoprotective, hypocholesterolemic activity by extraction of the herb Astragalus aspercentage 30%, 50% and 70% ethanol, evaporation to 1/3 volume under vacuum, purification from lipophilic substances by sedimentation at a temperature of 2 to 4oC within 48 hours, filtration, evaporation Phil the target product (100 kg) flavones, flavonols and their glycosides 15 - 17%, phenolic acids 5 to 6%, saponins 36 - 38%, coumarins 0,10 - 0,12%, polysaccharides 8 - 10%.

Example 1. 1 kg of air-dried powdered material was placed in the reactor and was exhaustively extracted with 30% ethanol in the ratio of raw materials-extractant 1:10 for 3 hours at ToC 60 - 65oC until complete depletion of raw materials. The amount of alcohol extract was 20 l, ethanol was evaporated at ToC 75 - 80o. The aqueous residue was evaporated in vacuum at a temperature of 40 - 50oC at 300 - 400 mm RT. tbsp. to 2 l and left in the refrigerator at a temperature of 2 to 4oC for 48 hours, filtered and dried in a vacuum drying Cabinet at a temperature of 40oC and a pressure of 300 to 400 mm RT.article.

Exit $ 28.6 - 29.6 per cent.

Example 2. 1 kg of air-dried powdered material was placed in a reactor heated and was extracted with 50% ethanol in the ratio of phases 1:10 when heated up to 60 - 65oC for 3 hours. The first contact phase - 2 hours, the second contact phase until full depletion of raw materials. The amount of alcohol extract was 20.2 liters of Ethanol was evaporated at To70 - 75oC, water balance, if To40 - 50oC at 300 - 400 mm RT.article up to 2 liters and left in the refrigerator at To2 to 4oC for 48 hours, then filter is composed of 30.0 - 32,5%.

Example 3. 1 kg of air-dried powdered material was placed in a reactor heated and was extracted with 70% ethanol in the ratio of phases 1:10 when heated to 70oC for 1 hour, the extraction was performed until complete depletion of raw materials. Volume was 19.6 kg Ethanol was evaporated at To70 - 72oC, water balance, if To40oC in vacuum at a pressure of 300 to 400 mm RT.article to 1.96 liters Left in the refrigerator at To2 to 4oC for 2 - 3 days. Lipophilic part was filtered, the residue was dried in a vacuum drying Cabinet at a temperature of 40oC at 300 - 400 mm RT.article The output was 29,0 - 30,0%. The data presented in table 1.

The study choleretic, hepatoprotective, hypocholesterolemic activity was carried out on white rats weighing 130 - 190 g Wistar rats. The study choleretic activity was performed according to the method of the Roller N. P. and Oleinik A. N. ("Pharmacology and toxicology". 1967, No. 3, S. 334 - 337).

This white rats under anesthesia (1% solution barbitala intraperitoneally calculation of 0.8 ml/100 g body weight) was administered cannula and collected bile within three hours.

Subject substance and the reference drug (flamin) was introduced in dwenadzatiperstnuu intestine.

The rate of secretion jelski processed (the State Pharmacopoeia of the USSR. 11th ed. M.: Medicine, 1987). The data presented in table 2.

Analyzing the data in the table we can conclude that choleretic activity total substance are at the level of cholelithiasis (30%-extractant) or exceeds the action to 1.27 - 1.28 times in comparison with the prototype above 2.06 to 2.7 times.

The study of hepatoprotective activity total substances was carried out on a model of acute fatty liver caused by tetrachlorethane (intragastric administration of a 50% oil solution of 0.75 ml/100 g body weight). The degree hepatoprotective action of the investigated substances were judged on their ability to reduce the activity of the indicator enzyme alanine aminotransferase (ALT) in the serum. The concentration of ALT in the serum was determined by the method Reitmanis S. and Frankels S. 1957 (Reitman S., Frankel S. Acolorimetric method for the olete rmination of serum glutamic oxalacetic and glutamic pyrivis transaminases Am. J Clin Path. - 1957. 28. P 56 - 59). The reference drug for this type of activity was selected zelibor. The data presented in table 3.

From table 3 it can be seen that the hepatoprotective effect of the total of the active substance, and the total substance obtained 50% and 70% ethanol exceeds the action celebra 1.24 - 1.47 times.

The study hypothesis is Triton WR-1339 (Lisiecka L. I. Influence of flavonoids on blood lipids in experimental hypocholesterolemia and atherosclerosis. //Abstract of Diss. Kida. Biol. Sciences - L.: - 1969. - 20 C.).

The analyte was injected I.P. in doses of 200 - 250 mg/kg of body weight of the animals twice:

- for the first time in 24 hour

- for the second time at the same time with Triton WR-1339 for 15 hours before decapitate.

For comparison hypocholesterolemic actions total substances from Astragalus aspercentage in the same conditions was introduced official preparations mickleton, polysporin and prototype. Control serve with experimental cholesterol-lowering pathology induced by intraperitoneal injection of Triton WR-1339, 15 hours before decapitate.

As indicators of lipid-lowering activity total input of substances from Astragalus aspercentage considered the reduction in total cholesterol (LDL) and triglycerides (TG) in the serum of experimental animals.

Introduction animals total substances from Astragalus aspercentage lead to a significant inhibition of the development of the hypocholesterolemic effect compared to administration of the drug of polysporin and Mickleson 1.12 - 1.5 times and is Bronislava according to the method of probit analysis Century. B. Prozorovsky to declare total substances is 5650 - 8840 mg/kg (Prozorovsky Century B., Prozorovsky M. P. //Pharmacology and toxicology. - 1980. - N-6. - S. 733 - 735).

1. The method of obtaining the total substances from herbs Astragalus aspercentage its choleretic, hepatoprotective, hypocholesterolemic activity, by extraction with ethanol with further evaporation under vacuum, removal of lipophilic substances, thickening under vacuum and dried in a vacuum drying Cabinet, characterized in that the extractant use 30% ethanol extraction was carried out at 60 - 65oC, when the ratio of phases 1 : 10, the cleaning is performed by settling at 2 to 4oC, drying at 40 - 45oC and a pressure of 300 to 400 mm RT.article.

2. The method of obtaining the total substances from herbs Astragalus aspercentage its choleretic, hepatoprotective, hypocholesterolemic activity, by extraction with ethanol with further evaporation under vacuum, removal of lipophilic substances, thickening under vacuum and dried in a vacuum drying Cabinet, characterized in that the extractant using 50% ethanol extraction was carried out at 60 - 65oC, when the ratio of phases 1 : 10, the cleaning is performed by settling when NCI of herbs Astragalus aspercentage, have choleretic, hepatoprotective, hypocholesterolemic activity, by extraction with ethanol with further evaporation under vacuum, removal of lipophilic substances, thickening under vacuum and dried in a vacuum drying Cabinet, characterized in that the extractant used 70% ethanol extraction was carried out at 60 - 65oC, when the ratio of phases 1 : 10, the cleaning is performed by settling at 2 to 4oC, drying at 40 - 45oC and a pressure of 300 to 400 mm RT.article

 

Same patents:

The invention relates to the field of medicine and is suitable for the treatment of cholecystitis, hepatitis, as well as urinary tract infections and gastroenteritis

The invention relates to the field of medicine and is suitable for the treatment of fungal diseases, and the prevention and treatment of fungal complications of antibiotic therapy

The invention relates to O6substituted derivatives of guanine, method of their production and to their use for the treatment of tumor cells
The invention relates to medicine, Oncology, can be used in the treatment of malignant tumors of the pancreas

The invention relates to medicine, in particular infectious diseases, and for the treatment of mumps orchitis in children

The invention relates to medicine, namely to therapy, and can be used in the treatment of malnutrition

The invention relates to the field of medicine and is suitable for the treatment of cholecystitis, hepatitis, as well as urinary tract infections and gastroenteritis

The invention relates to medicine, namely to infectious diseases, and can be used for the treatment of acute and chronic viral hepatitis In children

The invention relates to pharmaceutical compositions containing as active ingredient a derivative of triazine following General formula I or its MES, or its salt and a derivative of triazine

Cure for vitiligo // 2155055
The invention relates to the field of medicine
The invention relates to chemical-pharmaceutical industry and medicine and relates to the collection of medicinal plants that can be used to treat pyelonephritis

The invention relates to medicine, namely to clinical immunology, gynecology and for the treatment of yeast obesity resistant to standard therapy
The invention relates to the pharmaceutical industry, namely soluble effervescent dosage forms
The invention relates to the food and pharmaceutical industry and relates to biologically active additives
The invention relates to medicine, namely to the sexologist, and can be used for the treatment of sexual disorders diencephalic dysfunction in men

The invention relates to medicine, namely to the pharmacy, and can be used to obtain funds for the treatment of hypertension and methods for their preparation
Up!