The method of obtaining the extract from low-fat, milk thistle fruit

 

(57) Abstract:

The invention relates to pharmaceutical industry. As raw materials use of waste fatty milk Thistle oil is skimmed off. Their extracted with 70 to 85% ethanol by the method of repercolation first at room temperature, then at 60-85C. the Invention allows to increase the content of bioactive compounds in the product.

The invention relates to chemical-pharmaceutical industry, in particular to a method of obtaining the extract, milk Thistle [Silybum marianum (L.) Gaertn. (SEM. Asteraceae or Compositae)] of low-fat fruit of this plant (waste oil, milk Thistle).

Known methods of obtaining the amount flavolignans Thistle using different extractants - acetone, ethyl acetate, ethyl alcohol, aqueous alcohols[2, 3, 6, 8, 9]. These substances, the main biologically active substances which are silybin, silidianin, silikristin and other flavolignan, used for the production of such valuable hepatoprotective drugs as "Legalon", "Kars", "Zelibor", "Silimar and others [4].

However, the disadvantage is the later, the high prices obtained drugs. In addition, a disadvantage of known methods[2, 3, 6, 8, 9] is the fact that during the production of hepatoprotective drugs lose fat oil. Given the fact that the industrial production of milk Thistle oil, has marked regenerative properties, has become a reality [1, 4, 7], the objective necessity became the solution to the problem of waste production of this drug, in which the total content of flavolignans about 20% more than in the native fruits, milk Thistle (due to the removal of lipophilic complex).

This fact becomes especially important against the background of growing health needs in hepatoprotectors. One of the main factors of this trend is deteriorating environmental situation, leading to an increase in diseases with occupational diseases and ecopathology. The presence of a wide and affordable range of drugs based on fruits, milk Thistle could help to mitigate the harmful effects of environmental and other factors and, consequently, the recovery of the population of the Russian Federation. It is important to note that in Samersova, milk Thistle fruit, as at the farm "Sergius" and Middle-Volga zonal experimental station of the NGO "VILAR" (named Antonovka) created industrial plantations of this plant.

A prototype of the invention we have used the method of obtaining the extract, milk Thistle fruit, described in the literature [6].

This method involves the extraction of fruits, milk Thistle 80% ethyl alcohol by the method of repercolation combining the extraction of target compounds at room temperature with a subsequent exhaustive extraction flavolignans when heated in the temperature range of 60 - 85oC. thus obtain the target product, which represents an extract of milk Thistle liquid (1: 1), which has pronounced hepatoprotective properties [6].

The disadvantage of the prototype is that as raw material for the production of the target product (extract, milk Thistle) use fruits, milk Thistle, which leads to the loss of such a valuable substance, as a fatty oil which has marked regeneriruyuschim properties and used as a drug [1, 4, 7]. A rational approach to the use of, milk Thistle fruit, in our opinion, should zaklucatj the Thistle. This approach is still interesting that the content of biologically active compounds in low fat fruits higher in comparison with the native raw materials.

The purpose of the invention is the increase in the content of biologically active compounds in the target product and comprehensive utilization, milk Thistle fruit.

This goal is achieved by the fact that as raw material to extract, milk Thistle is waste product of fatty oil, milk Thistle [1], and the extraction of target compounds perform 70-85% ethanol. The extraction of low-fat, milk Thistle fruit (waste oil milk Thistle) is carried out, as in the case of the method of the prototype [6] , the method of repercolation combining the extraction of target compounds at room temperature, followed by exhaustive extraction flavolignans when heated in the temperature range of 60 - 85oC, but use 70-85% ethanol. This is due to the fact that the positive effect in the case of low-fat fruit deprived of lipophilic complex (fatty oil, fat-soluble vitamins, phytosterols), is achieved with the use of a wider range of concentrations of the extractant. Thus, the maximum in the increases and with the use of 70% and 85% ethanol: content amount flavolignans is in the target product, respectively, of 2.93% (example 2) and 3,01% (example 3). In addition, with regard to the removal of, milk Thistle fruit up to 20% of fatty oil in waste production is increasing fraction of the sum flavolignans - 2,73% to 3.25%, respectively. In the developed method for obtaining achieved a high yield of biologically active compounds from the raw materials used (93,0% of theoretical value), which allows to obtain the target product with a higher content of total flavolignans (totaling 3.04%) (example 1) compared to the prototype (of 2.51%) [6].

Conducted by the applicant search on scientific, technical and patent information sources and selected from the list of analogues prototype [6], we were able to identify the distinctive features of the claimed technical solution. Therefore, the inventive method of obtaining satisfies the criteria of the invention of "novelty."

Conducted by the applicant additional search of the known technical solutions [2, 3, 6-8] to detect in them the characteristics similar to the characteristics distinctive part of the formula of the proposed method of obtaining, showed that these signs are absent, therefore, the claimed technical solution meets the criterion of "inventive step".

The criteria of the invention "industrial applicability" podtverzhdaetsya.pochemu drug with a higher content of biologically active compounds, relatively simple to manufacture and relatively cheap due to the lack in technological scheme of production of expensive equipment. In addition, implementation of the developed method comprising obtaining an extract from the waste oil, milk Thistle, helps to solve the problem of complex use, milk Thistle fruit.

Use beyond the parameters of the concentration of the extractant does not achieve a positive effect, since there is a noticeable reduction in the yield of biologically active compounds from raw materials used: the total content of flavolignans in the extract of milk Thistle (target product) is in the case of 65% and 90% ethyl alcohol of 2.27% and 2.45%, respectively.

The inventive method is illustrated by the following examples.

Example 1. 400,0 g low-fat shredded, milk Thistle fruit (waste oil milk Thistle) is spread over 100.0 g 4 extractor, fill each extractor 300 ml of 80% ethanol and leave for 6 hours for soaking raw materials. Then in terms of repercolation perform one extraction at room temperature and successively two extraction at a temperature of 85

Example 2. 400,0 g low-fat shredded, milk Thistle fruit (waste oil milk Thistle) is spread over 100.0 g 4 extractor, fill each extractor 300 ml of 70% ethanol and leave for 6 hours for soaking raw materials. Then in terms of repercolation perform one extraction at room temperature and successively two extraction at a temperature of 85oC for 30 min in the calculation for each operation. The finished product (400 ml) collected from the 4th extractor and obtain a liquid extract, milk Thistle (1: 1). The total content of flavolignans (target substance), determined using the developed methodology [5], is the extract of 2.93%. The yield of the desired product in 90% of theoretical (the total content of flavolignans in production waste oil, milk Thistle is 3.25%).

Example 3. 400,0 g low-fat shredded fruits of milk Thistle Patni ml of 85% ethanol and leave for 6 hours for soaking raw materials. Then in terms of repercolation exercise Oder extraction at room temperature and successively two extraction at a temperature of 85oC for 30 min in the calculation for each operation. The finished product (400 ml) collected from the 4th extractor and obtain a liquid extract, milk Thistle (1: 1). The total content of flavolignans (target substance), determined using the developed methodology [5], is to extract 3,01%. The yield of the target product is 92% of theoretical (the total content of flavolignans in production waste oil, milk Thistle is 3.25%).

Using the proposed method allows the production in the pharmaceutical factories and other pharmaceutical companies, where there is no expensive equipment needed to obtain purified substances and tablets legform based on them. Using the proposed method extract from the waste oil milk Thistle allows to obtain the target product with a higher content of biologically active compounds and creates conditions for complex processing, milk Thistle fruit.

Implementation of the proposed method, basicity production effective hepatoprotective drugs which is in dire need of practical health care.

It should be noted that using the proposed method provides the following benefits:

1. The content of biologically active compounds (sum flavolignans) extract, milk Thistle (target product) increased to 3.04 from% compared to the prototype (of 2.51%), increased 1.2 times.

2. The inventive method allows to solve the problem of complex use, milk Thistle fruit, as the target product is produced from waste oil milk Thistle.

3. The cost of the target product, obtained by the claimed method, 20% less in comparison with the product obtained according to the method of the prototype that given the industrial production of milk Thistle oil will give benefits to 14 thousand rubles per ton of processed raw material, milk Thistle.

Sources of information:

1. Agamirov E. C., Pervushkin, S. C., Kurkin Century A. New approaches to technology of complex processing of medicinal plants // Ecology and health: proceedings of the IV all-Russian scientific-practical conference with international participation. - Samara, 1997, S. 192-193.

2. Zab the persons receiving the amount of polyoxyphenylene // Patent RF N 2038091, A 61 K 35/78, 27.06.95, Bull. N 18.

3. Dranik L. I., Dolgolenko L. G., Belikov centuries, armless P. I., Tkalich L. C., Nesian So Ya the Method of obtaining the amount of polyoxyphenylene // ABT.St. 603386 (USSR), A 61 K 35/78, 25.04.78, bull. N 15.

4. Kurkin Century A. Containing promising natural biologically active compounds. - Samara, 1996, 80 S.

5. Kurkin C. A., Sentsov M. F., E. Avdeeva Century, Pervushkin S. C. Method for quantitative determination silybin and amount flavolignans in fruits, milk Thistle // Samara medical archive. 1996, No. 1, S. 71-76.

6. Kurkin C. A., Lebedev, A. A., E. Avdeeva Century, Zapesochnaya gg, Pervushkin, S. C. , Simerini L. C., Bulatova M. C. a Method of obtaining the extract, milk Thistle // Patent RF N 2102999, A 61 K 35/78; A 61 K 9/08, 27.01.98, bull. N 3.

7. Lebedev, A. A., Simerini L. C., Lebedev, P. A. a Means with wound healing and hepatoprotective effects. - Pat. RF 2014840, A 61 K 35/78, publ. 30.06.94, bull. N 12.

8. Madaus R., Erler K., Malls Century, the Method of obtaining silimarina mixture // ABT.St. 1433391 (USSR), A 61 K 35/78, 23.10.88, bull. N 30.

9. Silagyi I., E. Terek, Stiber D. a Method of producing flavonoids // ABT. St. 598544 (USSR), A 61 K 35/78, 15.03.78, bull. N 10.

The method of obtaining the extract, milk Thistle fruit [Silybu first at room temperature, then when 60-85oC, characterized in that is used as raw material waste oil milk Thistle - low-fat fruits, milk Thistle and extraction of conduct 70-85% ethanol.

 

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SUBSTANCE: invention relates to the field in development of an agent of vegetable origin used for improvement of the functional state and prophylaxis of organic alterations in cardiovascular system, in particular, atherosclerosis. The biologically active supplement used for prophylaxis of cardiovascular diseases, in particular, atherosclerosis comprises clover dry extract, haw-thorn flowers powder, ascorbic and nicotinic acids, and accessory substances taken in the definite ratio. The biologically active supplement is made in the form of tablet or capsule. No adverse responses observed in intake of the supplement. The blood cholesterol level was reduced to the normal value in 68% of patients and reducing morbidity with acute respiratory-viral infections has been noticed. In patients with ischemic heart disease with cholesterolemia the improvement of the state is noted on the background of conventional therapy: the moderate reducing the arterial pressure value in its elevation, improved in the state of health, enhanced working capacity, reduced retrosternal pains, ear noise, vertigo, headache.

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