RU2578980C2 - Costmary syrup - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention relates to tansy syrup possessing potassium-sparing effect. Syrup contains 10.0 wt% infusion of tansy flowers, 55.8 wt% sorbitol or fructose, and 34.2 wt% of purified water. Infusion of tansy flowers produced by modified maceration comprising triple extraction of plant material distributed on three percolators in equal amounts of 40% ethyl alcohol in a ratio of raw material - extractant is 1:5, where last stage of each percolator is conducted under heating in a water bath for 30 minutes.

EFFECT: invention is characterised by optimum composition and a higher content of active ingredients in comparison with analogues.

1 cl, 2 dwg, 2 ex

Description

The invention relates to the pharmaceutical industry, in particular to the production of a pharmaceutical preparation having potassium-sparing activity, common tansy syrup, obtained on the basis of tincture from common tansy flowers (Tanacetum vulgare L.).

In official medicine, tansy flowers are widely used as a source of choleretic drugs, due to the high content of flavonoids in them. In the Russian Federation, the following medications obtained from tansy flowers are registered: “Tanacehol tablets coated with a coating of 0.05 g”, “Sibektan tablets of 0.1 g”. Also, the flowers of tansy are included in the "Cholagogue collection No. 3" (1), collection "Polychitochol" and "Syrup with extract of tansy ordinary" (8). All these forms are used as choleretic and hepatoprotective agents.

There are also biological active additives, which include tansy - Antigelmos, Triplet Evalar, Trigelm, Tanaxol, Antizit, which have a predominantly antiparasitic effect. There are experimental data in the literature on the diuretic, anti-inflammatory and antioxidant activity of tansy preparations based on flowers and leaves (9.10).

As you know, many diuretic drugs increase the excretion of potassium and can lead to hypokalemia (Furosemide, Hypothiazide) (5). Therefore, the development of potassium-sparing agents is relevant.

“Syrup with tansy extract” was chosen by us for the prototype of the invention (8). However, the composition and method of obtaining this collection are not without drawbacks: the technology for producing a liquid extract is cumbersome (includes the stage of evaporation); low yield of target substances - flavonoids (63%); high content of toxic component - thujone; drug instability (turbid solution, which gives sediment during storage) and the presence of flavorings and preservatives that can cause allergies.

Thus, the aim of the invention is to develop a composition and a more rational technology for producing syrup with potassium-sparing effect.

The technical result of the proposed method is to obtain syrup of tansy with the use of more rational technology, which saves the consumption of raw materials and higher yield of active substances.

The goal is achieved by first obtaining a tincture from the flowers of common tansy, using 40% ethyl alcohol as an extractant, in a raw material-extractant ratio of 1: 5, by the method of modified maceration, including triple extraction of plant material distributed in equal amounts over three percolators, 40% ethanol in the ratio of raw materials-extractant 1: 5, where the last stage in each percolator is carried out by heating in a water bath for 30 minutes, as well as sorbitol or fructose as a base at eduyuschem component ratio, wt.%:

tinctures of tansy flowers at 40% alcohol 10.0 sorbitol or fructose 55.8 purified water 34.2

Use instead of sucrose, as a base, sorbitol or fructose, allows us to recommend the developed preparation “Syrup of tansy ordinary” in children's practice and for patients suffering from diabetes mellitus.

The developed method is implemented as follows. To obtain tinctures of tansy ordinary take the calculated amount of raw materials, i.e. five times less than the required volume of tincture. Extraction is carried out with 40% ethyl alcohol. Tansy flowers are distributed in 3 percolators, in equal quantities. The scheme of tincture of tansy ordinary developed by us includes 5 days. On the 1st day, the soaking and extraction of raw materials is carried out for 1 day. For these purposes, eight volumes of extractant are poured into the 1st percolator. Along with this, three volumes of extractant are poured into the second percolator to soak the feed. On the 2nd day from the 1st percolator to the 2nd percolator transfer the entire volume of extraction, which is not absorbed by raw materials. Then, in the 1st percolator, the next portion of the extractant is poured in an amount of five volumes. Three volumes of extractant are poured into the 3rd percolator to soak the feed. On day 3, five volumes of extraction are filtered from the 2nd percolator to the 3rd percolator. Then, five volumes of extraction are also transferred from the 1st percolator to the 2nd. Then five volumes of extractant are added to the 1st percolator. In parallel, percolator No. 2 and percolator No. 3 continue extraction during the day, and in percolator No. 1, the thermal stage of the technological process is carried out by heating in a water bath for 30 minutes. Then the resulting extract is transferred to the receiver No. 1. After this, the raw material of the 1st percolator is spent and is excluded from the technological scheme. On the 4th day, extracting five volumes from percolator No. 3 as the 1st portion of the finished product, in the amount of 1/3 of the total volume of the finished product, filter and transfer receiver No. 3. Then, extracting five volumes from percolator No. 2 is transferred to the 3rd percolator for further extraction for 1 day. Extract from receiver No. 1 is transferred to percolator No. 2 and heated for 30 minutes in a water bath. The raw material of the 2nd percolator is also spent and is excluded from the technological scheme after the thermal stage. The obtained extract from percolator No. 2 is filtered off in receiver No. 2. On day 5, a second portion of the finished product is filtered from percolator No. 3 to receiver No. 3. In total, receiver No. 3 contains 2/3 of the finished product. After that, the extract collected in the receiver No. 2, is transferred to the percolator No. 3. Then, in the percolator No. 3, the final stage of the technological process is carried out by heating in a water bath for 30 minutes. After the obtained extract, as a third portion of the finished product, it is filtered into a receiver No. 3. The raw material of the 3rd percolator is also spent and is excluded from the technological scheme.

The obtained tincture of tansy ordinary is defended for 2 days at a temperature not exceeding 8 ° C and subjected to filtration, after which the finished product is ready for further use. In parallel, syrup is prepared according to standard technology for sorbitol syrup - 60-64% by weight (6.7). The flavoring agent is moistened with a small amount of water, the remaining water is added and dissolved by heating. After preparing the taste syrup, it is cooled to room temperature and brought to its original mass, filtered if necessary, and the quality is evaluated according to the refractive index and density. In the prepared syrup with stirring, add by weight 10% tincture of tansy flowers. Control the quality of the syrup and transfer it to the packaging.

The technological scheme of the syrup is shown in Fig. one.

The inventive method is implemented by the following examples.

Example 1

To obtain 50 ml tincture of tansy ordinary, we took 10.0 g of raw material. The flowers of tansy were distributed among 3 percolators, 3.4 g each. On the 1st day, 27.2 ml of extractant - 40% ethyl alcohol was poured into the 1st percolator, 10.2 ml of extractant was poured into the 2nd percolator . On the 2nd day, 17.0 ml of extract was transferred from the 1st percolator to the 2nd percolator. Then, 17.0 ml of extractant was poured into the 1st percolator. 10.2 ml of extractant was poured into the 3rd percolator. On the 3rd day, 17.0 ml of extract was transferred from the 2nd percolator to the 3rd percolator. Then, 17.0 ml of extract was also transferred from the 1st percolator to the 2nd percolator. Then, 17.0 ml of extractant was added to the 1st percolator. Extract in percolator No. 1 was heated in a water bath for 30 minutes. After that, the obtained extract was transferred to the receiver No. 1. After this, the raw materials of the 1st percolator, as spent, were excluded from the technological scheme. On the 4th day, 17.0 ml of extraction from percolator No. 3, as the 1st portion of the finished product was filtered and transferred to receiver No. 3. Then, 17.0 ml of extract from percolator No. 2 was transferred to the 3rd percolator. Extract from receiver No. 1 was transferred to percolator No. 2 and heated for 30 minutes in a water bath. The raw materials of the 2nd percolator were excluded from the technological scheme as waste. The obtained extract from percolator No. 2 was filtered into receiver No. 2. On the 5th day, a second portion of the finished product in the volume of 17.0 ml was filtered from percolator No. 3 to receiver No. 3. After that, the extract collected in receiver No. 2 was transferred to percolator No. 3 and heated in a water bath for 30 minutes. After filtering the obtained extract into receiver No. 3, a third portion of the finished product was obtained in a volume of 17.0 ml The raw materials of the 3rd percolator were excluded from the technological scheme, as well as the spent ones. In total, 51 ml of the finished product was collected in receiver No. 3 - tansy tincture ordinary, obtained by the method of modified maceration, including triple extraction of plant material distributed in three percolators in equal amounts, 40% ethyl alcohol in the ratio of raw material-extractant 1: 5, where the last stage each percolator is carried out by heating in a water bath for 30 minutes. The resulting tincture was defended for 2 days at a temperature not exceeding 8 ° C and subjected to filtration.

In parallel, sorbitol-based syrup was prepared. 279 g of flavoring agent was wetted with 40 ml of water, 131 ml of water was added and dissolved by heating. After preparing the taste syrup, it was cooled to room temperature and brought to its original mass, filtered and quality was assessed by refractive index and density. 50.0 g of tansy flower tincture was dissolved in chilled syrup. The average amount of flavonoids in the finished product is 0.058%. As a result, from 10.0 g of raw materials we received 500.0 g of syrup.

The resulting syrup is a clear amber-colored liquid with pleasant organoleptic characteristics.

Example 2

Tincture, as a syrup intermediate, was prepared in accordance with Example 1. In parallel, fructose-based syrup was prepared in accordance with Example 1. 50.0 g of tansy flower tincture was dissolved in a cooled syrup in accordance with Example 1. The average amount of flavonoids in the finished product was is 0.057%. As a result, we obtained 500.0 g of syrup from 10.0 g of raw materials.

A quantitative determination of the amount of flavonoids in the developed tansy syrup ordinary and prototype. An analysis of the preparations using the modified method of determination (3) shows that the content of flavonoids in the inventive preparation “Common tansy syrup” is 0.057% -0.058%, which is slightly higher compared to the prototype 0.49% (Fig. 2).

Syrup of tansy, obtained by the claimed method, was studied on 140 white, outbred rats of both sexes weighing 200-220 g.

In the case of tansy tincture, the most effective dose was 200 mg / kg, which, when observed for 24 hours, caused a significant significant increase in diuresis of 178%, natriuresis of 189%, potassium uresis of 153%, and creatininuresis of 167%. In this case, a pronounced potassium-sparing effect of the drug is observed.

The introduction of the preparation “Syrup of tansy ordinary” of the claimed composition will expand the range of the drug with potassium-sparing effect, produce a competitive domestic drug, easy to manufacture and affordable for the general population.

Thus, the claimed composition of the drug have several advantages:

1. The optimality of the composition of tansy ordinary syrup, achieved by including tinctures of tansy flowers on 40% ethyl alcohol at a ratio of 1: 5.

2. The content of the amount of flavonoids in the developed product is higher compared to the prototype (approximately 18%).

3. The claimed method for producing syrup gives a five-fold economic effect, consisting in the fact that from 10.0 g of raw materials we obtain 500.0 g of syrup, compared with 100.0 g of the drug in the prototype.

4. In the developed preparation using TLC analysis, no toxic component, thujone, is detected.

5. The presence of potassium-sparing effect.

6. The optimal dosage in combination with the stability of the drug.

7. The developed syrup is characterized by potential hypoallergenicity and the absence of side effects due to the exclusion of preservatives and antioxidants, which is especially important for people with allergies.

INFORMATION SOURCES

1. The state register of medicines [Electronic resource]. - Electron, given. - 2011. - Access mode: http://grls.rosminzdrav.ru/grls.aspx - Zagl. from the screen.

2. Kurkin, V.A. Fundamentals of herbal medicine: a training manual / V.A. Kurkin. - Samara: Etching; Samara State Medical University, 2009 .-- 963 p.

3. Kurkina, A.V. Method for determining the amount of flavonoids in tansy flowers / A.V. Kurkina, A.I. Khusainova // Pharmacy. - 2010. - T. 58, No. 3. - S. 21-24.

4. Kurkina, A.V. Flavonoids of flowers Tanacetum vulgare / A.V. Kurkina, A.I. Khusainova, E.D. Daeva, V.I. Kadentsev // Chemistry of Natural Compounds. - 2011. - No. 2. - S. 256-257.

5. Mashkovsky, M.D. Medicines: in 2 tons / M.D. Mashkovsky. - M.: New Wave, 2008 .-- 1206 p.

6. Industrial technology of drugs: Textbook for universities: in 2 volumes, Volume 2 / B.I. Chueshov, M.Yu. Chernov, L.M. Khokhlova. - X .: MTK - Book; Publisher NFAAU, 2002. - 716 p.

7. Technology of dosage forms / Ed. L.A. Ivanova. - M .: Medicine, 1991. - T. 2. - 544 p.

8. Yakusevich, R.V. Development of the composition, technology and quality standards of the corrected dosage form - a syrup based on tansy (Tanacetum vulgare L.): author. dis ... cand. Pharmac Sciences: 14.04.01 / Yakusevich Roman Viktorovich. Pyatigorsk, - 2013 .-- 23 p.

9. Lahlou, S. Diuretic activity of the aqueous extracts of Carum carvi and Tanacetum vulgare in normal rats / S. Lahlou, A. Tahraoui, Z. Israili, B. Lyoussi // J. of Ethnopharmacology, 2007. - Vol. 110. - Iss. 3. - P. 458-463.

10. Mordujovich-Buschiazzo, P. Anti-inflammatory activity of Tanacetum vulgare I P. Mordujovich-Buschiazzo, E.M. Balsa, H.O. Buschiazzo, E. Mandrile, M. Rosella, G. Schinella, D. Fioravanti // J. Fitoterapia, 1996 .-- V 67. - Iss 4. - P. 319-322.

Claims (1)

Syrup of tansy ordinary, with a potassium-sparing effect, characterized in that it contains tincture of the flowers of tansy ordinary, obtained by the method of modified maceration, including triple extraction of plant material, distributed over three percolators in equal amounts, 40% ethyl alcohol in the ratio of raw material - extractant 1: 5, where the last stage in each percolator is carried out by heating in a water bath for 30 minutes, as well as sorbitol or fructose as a base in the following ratio of compo nents, wt.%:
tinctures of tansy flowers at 40% alcohol 10.0 sorbitol or fructose 55.8 purified water 34.2

Images