Method of obtaining tinctura schizandrae

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

 

The invention relates to chemical-pharmaceutical industry, in particular to a method for the Infusion of Chinese Magnolia"with neurotropic activity.

At the present time is a very urgent problem of expanding the range of herbal medicines that increase the adaptive capacity of the human body, especially on the unfavorable ecological situation, busy rhythm of life, psycho-emotional stress, the cause or the consequence of which are asthenic conditions.

According to Russian scientists [1, 2] in the seeds of schisandra chinensis leading group of biologically active compounds is a group containing - lignans, in particular schizandrin, γ-schisandrin, etc. that have a tonic effect. This circumstance was taken into account when developing technological way of getting infusions of schisandra chinensis.

In the previous studies highlighted gamma-schizandrin high purity (99.8 per cent), which is promising as the state standard (GSO) for the standardization of raw materials and preparations schisandra [3].

A prototype of the invention taken by way of receiving infusions of schisandra chinensis [Schizandra chinensis (Turcz.) Baill.)] method of maceration, is used as the extractant 95% ethyl alcohol (Tincture of lemongrass seeds") [4, 5, 6]. The essence of this method lies in the fact that the crushed seeds fill in 95% ethanol, placed in a sealable vessel and insist at a temperature of 15-20°C, occasionally shaking or stirring. After infusion (7 days) removing the merge, the residue is repeatedly squeezed and washed with extractant and pulled the hood is brought up to the required volume [4].

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

The aim of the invention is to increase the yield of the target substance from the seeds of schisandra chinensis.

The inventive method get is as follows: the extraction of raw materials spend 70...90% ethyl alcohol by heating at the temperature of 65-70°C.

This method allows, on the one hand, in a sparing mode to get the most enriched extracts, and on the other to achieve greater extraction (output Lignano is 2.12% compared to 1.77% in the prototype).

With regard to the standardization of the drug on the chromatogram (TLC analysis) tincture obtained by the claimed method, it is found dominant spot substances belonging to γ-schisandrin. Spectrophotometric study of tincture of schisandra chinensis showed that this PR is parathas has a curve of absorption, characteristic γ-schizandrin (absorption maxima at a wavelength of 220, 254 (square) and 280 nm). The total content of Lignano in the product in terms of γ-schisandrin is 2.12%.

The results of pharmacological studies suggest that the tincture obtained by the proposed method, the dose of 50 and 100 mg/kg reduces the duration thiopental sleep 75.4% and 40.7%, respectively, with 129,7±26.6 to 31,9±20,1 (p<0,05) min, and br143.3±11.0 to 85±14,8 (p<0,05) minutes

Interestingly, the study sample tinctures 70% alcohol by its neurotropic activity exceeds industrial design at 90%.

Conducted by the applicant search on scientific, technical and patent information sources and selected from the list of analogues prototype [4] allowed us to identify the distinctive features of the claimed technical solution. Therefore, the inventive method of obtaining satisfies the criteria of the invention of "novelty" (table 1).

Table 1
The hallmarks obtain the "Tincture of lemon"
№ p/pThe parameters of the methodThe inventive methodThe placeholderThe advantages of the proposed method
1. The extractantEthyl alcohol
(70%...90%)
Ethyl alcohol 95%Lower cost of
2.Content Lignano, %2,121,77A higher content of (1.2 times)
3.Output Lignano, %98,1581,80Higher output (1.2 times)
4.The duration of the technological process76 h168 h2.2 times shorter

Conducted by the applicant additional search of the known technical solutions [4] for the purpose of detecting their symptoms, similar to the signs of the 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" is confirmed by the fact that the proposed method for the infusion of Chinese Magnolia vine allows you to get industrial is m the manufacture of the medicinal product relatively simple to manufacture and relatively cheap due to the lack in technological scheme of production of expensive equipment, but with pronounced neurotropic activity.

Developed a method of obtaining is illustrated by examples 1, 2.

Example 1. of 300.0 g of crushed seeds of schisandra chinensis to the size of particles passing through a sieve with the hole diameter of 2 mm, spread over 100.0 g 3 extractor (see drawing). In the 1st extractor is poured three times the amount of 70% ethanol (300 ml) to swell for 3 hours and then 5 volumes of extractant (500 ml) for extraction of raw materials within 24 hours at room temperature. In the 2nd extractor is placed 300 ml of 70% ethyl alcohol for soaking and leave at 3 o'clock

After 24 h (day 2) from the 1st extractor pour 500 ml of the extract in the 2nd extractor and left for 24 h at room temperature. In this maturational a pause in the 1st extractor pour 500 ml of fresh extractant and leave before the start of the 3rd day. In the 3rd extractor is placed 300 ml of 70% ethyl alcohol for soaking and leave at 3 o'clock

After 24 h (day 3) from the 2nd extractor pour 500 ml of the extract in the 3rd extractor and left for 24 h for extraction at room temperature. From the 1st extractor pour 500 ml of the extract in the 2nd extractor and left for 24 h for extraction when the room is Noah temperature. In this maturational a pause in the 1st extractor pour 500 ml of fresh extractant and carry out thermal extraction of the 1-m extractor under reflux at a temperature of 65-70°C for 30 minutes the resulting extract from the 1st of the extractor is placed in the receiver 1 and use it on subsequent stages for thermal extraction of raw materials in the 2nd extractor.

After 24 h (day 4) perform plum extract from the 3rd extractor in a container of finished products (1/3 part). From the 2nd extractor pour 500 ml of the extract in the 3rd extractor and left for 24 h for extraction at room temperature. Extract from the receiver 1 receives the 2nd extractor and carry out thermal extraction under reflux at a temperature of 65-70°C for 30 minutes with 500 ml of extract obtained was poured in the receiver 2 and use it on subsequent stages for thermal extraction of raw materials in the 3rd extractor.

After 24 h (day 5) perform plum extract from the 3rd extractor in a container of finished products (1/3 part). Extract from the receiver 2 is placed in the 3rd extractor and carry out thermal extraction under reflux at a temperature of 65-70°C for 30 min and poured into a vessel with the finished product and thus receive a total of 1500 ml of the finished product. The finished product (1500 ml) maintained at temperature the round of 8°C for 2-3 days and filter.

The total content of Lignano (target substance) in the finished product is in terms of γ-schisandrin - 2,12%. The yield of the target substances is 98,15% of theoretical (the total content of Lignano in the seeds of schisandra chinensis is 10,80%).

Example 2. 300,0 g chopped to the size of particles passing through a sieve with the hole diameter of 3 mm, spread over 100.0 g 3 extractor. In the 1st extractor is poured three times the amount of 90% ethyl alcohol (300 ml) to swell for 3 hours and then 5 volumes of extractant (500 ml) for extraction of raw materials within 24 hours at room temperature. In the 2nd extractor is placed 300 ml of 90% ethyl alcohol for soaking raw materials and leave at 3 o'clock

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

The total content of Lignano (target substance) in the finished product is in terms of γ-schisandrin - 1,93%. The yield of the target substances is 89,35% of theoretical (the total content of Lignano 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 of three extractors 70%...90% ethanol using the first two extraction the materials is at room temperature, and the third follow - when heated in the temperature range of 65-70°C.

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 tablet dosage forms based on them. The positive effect of the proposed method is that the yield of the target substances from raw materials increased to 98,15% compared with 81,80% in the prototype, and the content of the target substances (amount Lignano in terms of γ-schizandrin) in the finished product is 2.12%, i.e. increased 1.2 times compared with the same period in the target product (1,77%)obtained by the method described in the prototype [4] (table 1).

About the feasibility of this approach to obtain the target substance 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 implementation of the proposed method will allow you to replenish stock tonics competitive product, easy to manufacture and relatively cheap and affordable for the General population.

It should be noted that using the proposed method provides the following advantages to the company:

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

2. The yield of the target substance in the target product, obtained by the claimed method is 98,15% compared with the prototype - 81,80%.

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

4. More pronounced toning activity.

Sources of information

1. Kurkin V.A. Pharmacognosy: a Textbook for students of pharmaceutical universities / Ed. 2nd, revised and enlarged extra - Samara LLC "Etching", SEI HPE "Samara state medical University", 2007. - 1239 S.

2. Medicinal raw materials of vegetable and animal origin. Pharmacognosy: the textbook / under the editorship Gpicview. - SPb.: Spec lit, 2006. - 845 S.

3. Sattarova VS Modern approaches to standardization of raw materials and the development of new drugs schisandra chinensis to explore the effect on the virulence activity of bacteria / Piscatawa, Pentalateral, Nurgalieva // proceedings of Samara scientific center of Russian Academy of Sciences. Spec. issue XII all-Russian Congress "Ecology and human health. - Samara, 2007. - Vol.2. - S-203.

4. Ants I.A. Technology of drugs. Ed. 3rd, revised and enlarged extra - V.1. - M.: Medicine, 1980. - 704 S.

5. FS 42-1822-90. Infusion of lemongrass seeds / State. inspection control is and the quality of medicines, products and honey. equipment. Pharmacopoeial Committee. - Instead of FS 42-1822-82; with an Introd. 28.09.90 to 30.06.95. - 5 S.

6. The state register of medicines. - Vol. 1 (the official newspaper of January 1, 2006): Ministry of health, 2006. - 1300 C.

The method of obtaining schisandra tincture using alcohol, characterized in that the seeds of schisandra chinensis extracted 70-90% ethyl alcohol at room temperature, and then heated at the temperature of 65-70°C.



 

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