RU2368388C1 - Method of obtaining tinctura schizandrae - Google Patents

Abstract

FIELD: chemistry.

SUBSTANCE: invention relates to the chemical and pharmaceutical industry. Schizandra seeds are extracted using 70-90% ethyl alcohol first at room temperature and then while heating at temperature between 65-70°C.

EFFECT: invention increases output of active substances.

2 ex, 1 tbl, 1 dwg

Description

The invention relates to the chemical and pharmaceutical industry, in particular to a method for producing funds "Tincture of Schisandra chinensis" with neurotropic activity.

Currently, it is very urgent to expand the assortment of herbal medicines that increase the adaptive capabilities of the human body, especially against the background of an unfavorable environmental situation, a stressful rhythm of life, and psycho-emotional stress, caused or caused by asthenic conditions.

According to Russian scientists [1, 2], the leading group of biologically active compounds in the seeds of Schisandra chinensis is the group of phenylpropanoids - lignans, in particular schizandrin, γ-schisandrin, etc., which have a tonic effect. This circumstance was taken into account when developing a technological method for obtaining tincture of Schisandra chinensis.

As a result of previous studies, high purity gamma schizandrin (99.8%) was isolated, which is promising as a state standard sample (GSO) for the standardization of schisandra raw materials and preparations [3].

As a prototype of the invention, a method for producing tincture of Schisandra chinensis (Schizandra chinensis (Turcz.) Baill.)] Was taken by the method of maceration, using 95% ethanol as an extractant (“Tincture of Schisandra seeds”) [4, 5, 6]. The essence of this method is that the crushed seeds are poured with 95% ethanol, placed in a sealed vessel and insisted at a temperature of 15-20 ° C, shaking or stirring from time to time. After infusion (7 days), the extract is drained, the residue is squeezed several times and washed with extractant and the extracted extracts are brought to the required volume [4].

However, the disadvantages of this method are the complexity of the process, incomplete extraction of the target substances (lignans) and, as a result, the low yield of the target product.

The aim of the invention is to increase the yield of target substances from the seeds of Schisandra chinensis.

The inventive method of obtaining is implemented as follows: extraction of raw materials is carried out 70 ... 90% ethyl alcohol when heated in the temperature range 65-70 ° C.

This method allows, on the one hand, to obtain the most enriched extracts in a gentle mode, and on the other hand, to achieve greater extraction (the yield of lignans is 2.12% compared to 1.77% in the prototype).

As for the standardization of this drug, then on the chromatogram (TLC analysis) of the tincture obtained by the claimed method, a dominant spot of a substance belonging to γ-schizandrin is found. Spectrophotometric study of tincture of Schisandra chinensis showed that this preparation has an absorption curve characteristic of γ-schizandrin (absorption maxima at a wavelength of 220, 254 (pl.) And 280 nm). The content of the amount of lignans in the preparation in terms of γ-schizandrin is 2.12%.

The results of pharmacological studies indicate that the tincture obtained by the proposed method at a dose of 50 and 100 mg / kg reduces the duration of thiopental sleep by 75.4% and 40.7%, respectively, from 129.7 ± 26.6 to 31.9 ± 20.1 (p <0.05) min, and from 143.3 ± 11.0 to 85 ± 14.8 (p <0.05) min.

It is interesting that the test sample of tincture with 70% alcohol in its neurotropic activity exceeds the industrial sample by 90%.

A search by the applicant for scientific, technical and patent sources of information and a prototype selected from the list of analogues [4] made it possible to identify distinctive features in the claimed technical solution. Therefore, the claimed method of obtaining meets the criteria of the invention of "novelty" (table 1).

Table 1
Distinctive signs of receiving funds "tincture of lemongrass" No. p / p Method Parameters The inventive method Prototype The advantages of the proposed method one. Extractant Ethanol
(70% ... 90%) Ethyl alcohol 95% Lower cost 2. The content of lignans,% 2.12 1.77 Higher content (1.2 times) 3. The output of lignans,% 98.15 81.80 Higher yield (1.2 times) four. Process time 76 h 168 h 2.2 times shorter

The applicant conducted an additional search for known technical solutions [4] in order to detect in them features similar to those of the distinctive part of the formula of the claimed production method, showed that these signs are absent, therefore, the claimed technical solution meets the criterion of "inventive step".

The criterion of the invention "industrial applicability" is confirmed by the fact that the proposed method for producing tincture of Schisandra chinensis makes it possible to obtain a drug in industrial production that is quite simple to manufacture and relatively cheap due to the lack of expensive equipment in the production scheme, but with pronounced neurotropic activity.

The developed production method is illustrated by examples 1, 2.

Example 1. 300.0 g of crushed seeds of Schisandra chinensis to a particle size passing through a sieve with a hole diameter of 2 mm, is distributed 100.0 g into 3 extractors (see drawing). Three times the amount of 70% ethyl alcohol (300 ml) is poured into the 1st extractor to swell for 3 hours and then 5 volumes of extractant (500 ml) to extract the raw material for 24 hours at room temperature. In the 2nd extractor, 300 ml of 70% ethyl alcohol are placed for soaking and left for 3 hours.

After 24 hours (day 2), 500 ml of extract is transferred from the 1st extractor to the 2nd extractor and left at room temperature for 24 hours. In this maceration pause, 500 ml of fresh extractant is poured into the 1st extractor and left until the beginning of the 3rd day. In the 3rd extractor, 300 ml of 70% ethyl alcohol are placed for soaking and left for 3 hours.

After 24 hours (3rd day), 500 ml of extract is transferred from the 2nd extractor to the 3rd extractor and left for 24 hours for extraction at room temperature. From the 1st extractor, transfer 500 ml of the extract to the 2nd extractor and leave for 24 hours for extraction at room temperature. In this maceration pause, 500 ml of fresh extractant is poured into the 1st extractor and thermal extraction is carried out in the 1st extractor under reflux at a temperature of 65-70 ° C for 30 minutes. The obtained extract from the 1st extractor is poured into the receiver 1 and used in the subsequent stages for the thermal extraction of raw materials in the 2nd extractor.

After 24 hours (4th day), the extraction is drained from the 3rd extractor into a vessel with the finished product (1/3 part). 500 ml of extract is transferred from the 2nd extractor to the 3rd extractor and left for 24 hours for extraction at room temperature. Extract from the receiver 1 is poured into the 2nd extractor and carry out thermal extraction under reflux at a temperature of 65-70 ° C for 30 minutes 500 ml of the obtained extract is poured into the receiver 2 and used in the subsequent stages for the thermal extraction of raw materials in the 3rd extractor.

After 24 hours (5th day), the extraction is drained from the 3rd extractor into a vessel with the finished product (1/3 part). The extract from the receiver 2 is poured into the 3rd extractor and thermal extraction is carried out under reflux at a temperature of 65-70 ° C for 30 minutes and poured into a vessel with the finished product, and a total of 1500 ml of the finished product is obtained. The resulting finished product (1500 ml) is kept at a temperature of 8 ° C for 2-3 days and filtered.

The content of the sum of lignans (target substances) in the finished product is 2.12% in terms of γ-schizandrin. The yield of the target substances is 98.15% of theoretical (the content of the sum of lignans in the seeds of Schisandra chinensis is 10.80%).

Example 2. 300.0 g crushed to a particle size passing through a sieve with a hole diameter of 3 mm, is distributed 100.0 g into 3 extractors. Three times the amount of 90% ethyl alcohol (300 ml) is poured into the 1st extractor to swell for 3 hours and then 5 volumes of extractant (500 ml) are used to extract the raw material for 24 hours at room temperature. In the 2nd extractor, 300 ml of 90% ethyl alcohol are placed to soak the raw material and left for 3 hours.

Further, the technological process is carried out analogously to example 1, using 90% ethyl alcohol as an extractant at all stages. Receive 1500 ml of the finished product.

The content of the amount of lignans (target substances) in the finished product is in terms of γ-schizandrin - 1.93%. The yield of the target substances is 89.35% of theoretical (the content of the sum of lignans in the seeds of Schisandra chinensis is 10.80%).

Thus, the optimal conditions for obtaining the finished product - tincture of Schisandra chinensis (1: 5) are: extraction in three extractors with 70% ... 90% ethyl alcohol using the first two extracts of the raw material at room temperature and the third subsequent one when heated in the temperature range 65- 70 ° C.

Using the proposed method allows for production in a pharmaceutical factory and other pharmaceutical enterprises, where there is no expensive equipment necessary to obtain purified substances and tablet dosage forms based on them. The positive effect of the proposed method is that the yield of target substances from raw materials increases to 98.15% compared with 81.80% in the prototype, and the content of the target substances (the sum of lignans in terms of γ-schizandrin) in the finished product is 2, 12%, i.e. increases by 1.2 times compared with the same indicator in the target product (1.77%) obtained by the method described in the prototype [4] (table 1).

The expediency of this approach to obtaining the target substances and, therefore, a positive effect is also evidenced by the fact that the resulting tincture has pronounced tonic properties.

Based on this, we can conclude that the introduction of the proposed method will replenish the range of tonic agents with a competitive drug, easy to manufacture and relatively cheap and affordable for the general population.

It should be noted that the use of the proposed method provides the following advantages:

1. The content of the target substances in the finished product obtained by the claimed method is 2.12% compared with 1.77% in the prototype (an increase of 1.2 times).

2. The yield of the target substances in the target product obtained by the claimed method is 98.15% compared with the prototype - 81.80%.

3. The duration of the process is reduced by 2.2 times compared with the prototype (from 168 hours or 7 days to 76 hours).

4. A more pronounced tonic activity.

Information sources

1. Kurkin V.A. Pharmacognosy: Textbook for students of pharmaceutical universities / Ed. 2nd, rev. and additional - Samara: LLC “Etching”, GOU VPO “SamGMU”, 2007. - 1239 p.

2. Medicinal raw materials of plant and animal origin. Pharmacognosy: a training manual / ed. G.P. Yakovleva. - St. Petersburg: SpetsLit, 2006 .-- 845 p.

3. Satdarova F.Sh. Modern approaches to the standardization of raw materials and the development of new preparations of Schisandra chinensis with the study of the effect on bacteria virulent activity / F.Sh. Satdarova, P.N. Zolotarev, N.R.Shagalieva // Bulletin of the Samara Scientific Center of the Russian Academy of Sciences. Specialist. issue of the XII All-Russian Congress "Ecology and Human Health". - Samara, 2007 .-- T.2. - S.198-203.

4. Muravyov I.A. Technology of drugs. Ed. 3rd, rev. and add. - T.1. - M.: Medicine, 1980 .-- 704 p.

5. FS 42-1822-90. Tincture of lemongrass seeds / gos. inspection for quality control of medicines, products and products honey. technicians. Pharmacopoeia Committee. - Instead of FS 42-1822-82; Enter 09/28/90 to 06/30/95. - 5 sec.

6. The state register of medicines. - T.1 (official publication as of January 1, 2006 - M .: Ministry of Health of the Russian Federation, 2006. - 1300 p.

Claims (1)

A method of obtaining tincture of lemongrass using ethyl alcohol, characterized in that the seeds of Chinese magnolia vine are extracted with 70-90% ethyl alcohol, first at room temperature, and then when heated in the temperature range 65-70 ° C.

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