RU2800375C1 - Angent with creatininuretic action - Google Patents

Abstract

FIELD: chemical and pharmaceutical industry.

SUBSTANCE: invention relates to a medicinal product with creatinine activity. A medicinal product with a creatininuretic effect, characterized by the following: it is a thick extract of blood-red hawthorn shoots with a total content of flavonoids in terms of hyperoside 3.44±0.17%, to obtain which 100 g of crushed hawthorn shoots are dried, 150 ml of 70% ethyl alcohol is added, left to soak for a day, on the second day 30 ml of 70% ethyl alcohol is placed in the same flask and infused for two days, on the fourth day, the obtained extract is drained from the flask in the amount of 30 ml, obtaining the first portion of the extract, a fresh portion of the extractant is again poured in the amount of 30 ml, on the sixth day another 30 ml of the extract is poured from the flask, obtaining the second portion of the extract, combining it with the first portion of the extract, then 40 ml of a fresh portion of 70% ethanol is poured into the flask and left for a day, on the seventh day the contents of the flask are heated in a water bath to boil and after cooling, 40 ml of the extract is poured, combining it with the first two portions of the extract, the resulting liquid extract is settled in a cold dark place for 3 days at a temperature not higher than 8°C, filtered and the extractant is removed until a moisture content is not more than 25%.

EFFECT: above agent has a pronounced creatininuretic effect, and is characterized by a high content of flavonoids.

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Description

The invention relates to the chemical and pharmaceutical industry and can be used in enterprises for the processing of medicinal plant raw materials in order to obtain medicinal herbal preparations.

Fruits and flowers of hawthorn are used as medicinal plant materials for the preparation of cardiotonic drugs [1]. Blood red hawthorn ( Crataegus sanguinea Pall.) is the most widely distributed in the territory of the Russian Federation [1, 3]. Both types of hawthorn raw materials contain many different biologically active compounds, of which flavonoids are the main ones [3]. From hawthorn fruits on the basis of 70% alcohol, the drug "Hawthorn fruit tincture" is obtained [1]. This drug was chosen by us as a prototype. The disadvantages of this drug are: the high content of ethyl alcohol in the drug (65%) and the low content of flavonoids (not less than 0.003% in terms of hyperoside). Ethyl alcohol is contraindicated in some categories of patients, and the low content of active ingredients in the preparation does not allow achieving high efficiency in the treatment of cardiovascular diseases. In addition, the drug "Hawthorn fruit tincture" does not have a significant effect on the excretory function of the kidneys.

One of the possible types of blood-red hawthorn raw materials for obtaining medicinal preparations is the shoots of the first year, collected at the flowering stage of the plant [4]. This raw material, shoots, consists of leaves, flowers, and non-lignified stems [2, 5]. Harvesting hawthorn shoots is much easier than harvesting flowers and causes less damage to the plant's thickets.

Thus, the aim of the invention is the development of a medicinal product based on a new type of raw material - shoots of blood-red hawthorn, characterized by a high level of flavonoids, the absence of ethyl alcohol in its composition and having a creatininuretic effect.

The technical result is the creation of a thick extract of shoots of blood-red hawthorn, which has a creatininuretic effect.

To do this, 100 g of dried and crushed hawthorn shoots are placed in a 500 ml flask, 150 ml of ethyl alcohol 70% is added and left to soak for a day. On the second day, 30 ml of ethyl alcohol 70% is placed in the same flask and infused for two days. On the fourth day, the resulting extract is drained from the flask in an amount of 30 ml (finished product) and a fresh portion of the extractant is poured again in an amount of 30 ml. On the sixth day, another 30 ml of extract (finished product) is drained from the flask, combining it with the first portion of the extract. After that, 40 ml of a fresh portion of 70% ethyl alcohol is again poured into the flask and left for a day. On the seventh day, the contents of the flask are heated in a water bath to a boil and after cooling, 40 ml of the extract (finished product) is poured off, combining it with the first two portions. The resulting liquid extract stand in a cold dark place for 3 days at a temperature not exceeding 8°C. After settling, the liquid extract is filtered and the extractant is removed by heating and drying under vacuum. The resulting thick extract should contain no more than 25% moisture and meet all the requirements for thick extracts. The content of flavonoids in the obtained thick extract of blood-red hawthorn shoots in terms of hyperoside was 3.44±0.17%. This figure exceeds the prototype (Hawthorn fruit tincture) by more than 1000 times.

The resulting thick extract of blood red hawthorn shoots was used to study the excretory function of the kidneys in preclinical studies on outbred laboratory rats. The study of diuretic activity was carried out in a chronic experiment on outbred rats of both sexes weighing from 200 to 250 grams. The animals were kept in a vivarium on a standard diet. All animals were divided into groups. There were 10 animals in each group. On the day of the experiment, the experimental group of animals was administered once intragastrically with a probe a water load in the amount of 3% of body weight and the test drug at a dose of 10 mg/kg of the live weight of the animal. The control group received a water load in the amount of 3% of body weight. After all manipulations, the animals were placed in exchange cages for a day. 4-hour and 24-hour urine samples were collected. Furosemide at a threshold dose of 1 mg/kg was chosen as the reference drug in a 4-hour experiment, and hypothiazide at an effective average therapeutic dose of 20 mg/kg in a 24-hour experiment. The renal excretion of water was determined, and the concentration of creatinine in portions of the urine was also recorded. The data obtained as a result of the experiment were processed statistically using the Mann-Whitney test.

As a result of the experiments, it was found that a thick extract of blood-red hawthorn shoots significantly increases creatinine excretion, both in 4 hours of the experiment (by 67%) and in 24 hours of the study (by 35%) compared with the indicators of animals in the control group. The obtained results testify to a pronounced creatininuretic effect (the ability to remove the product of protein metabolism creatinine from the body) of a thick extract of blood-red hawthorn shoots. This action does not have the drug "Hawthorn fruit tincture".

Thus, the proposed method for obtaining an agent, which is a thick extract of blood-red hawthorn shoots, has the following advantages:

1. Dense extract of blood-red hawthorn shoots has a pronounced creatinine-uretic effect.

2. A thick extract of blood-red hawthorn shoots exceeds the drug "Hawthorn fruit tincture" in terms of the content of the amount of flavonoids, more than 1000 times.

3. A thick extract of blood-red hawthorn shoots does not contain ethyl alcohol in its composition.

INFORMATION SOURCES:

1. State Pharmacopoeia of the Russian Federation. - Fourteenth edition. - M.: Ministry of Health of the Russian Federation, 2018. / URL: http://femb.ru/femb/pharmacopea.php.

2. State Pharmacopoeia of the Republic of Belarus. 1st editions. Volume 2. Ministry of Health of the Republic of Belarus: Minsk. - 2007.

3. Kurkin V.A. Pharmacognosy. Textbook for students of pharmaceutical universities (faculties). - 3rd ed., revised. and additional - Samara: LLC "Etching"; FGBOU VO SamGMU of the Ministry of Health of Russia, 2016. - 1279 p.

4. Kurkin V.A., Pravdivtseva O.E., Shaikhutdinov I.Kh., Kurkina A.V., Zaitseva E.N., Volkova N.A. Species of the genus hawthorn ( Crataegus L.): standardization and development of drugs: Monograph. - Samara: OOO "Ofort", 2020. - 118 p.

5. European Pharmacopoeia. - 8 ed. Strasbourg: Directorate for the Quality of Medicines & HealthCare of the Council of Europe. - 2013.

Claims (1)

A drug with a creatininuretic effect, characterized in that it is a thick extract of blood-red hawthorn shoots with a total flavonoid content in terms of hyperoside of 3.44 ± 0.17%, to obtain which 100 g of crushed hawthorn shoots are dried, 150 ml of 70% ethyl alcohol is added, left for soaking for a day, for the second day, 30 ml of 70% ethyl alcohol is placed in the same flask and infused for two days, on the fourth day, the resulting extract is drained from the flask in the amount of 30 ml, obtaining the first portion of the extract, a fresh portion of the extractant is again poured in the amount of 30 ml, on the sixth day another 30 ml of the extract is poured from the flask, obtaining the second portion of the extract, combining it with the first portion of the extract, then pour 40 ml of fresh portion into the flask 70% ethyl alcohol and left for a day, on the seventh day the contents of the flask are heated in a water bath to a boil and after cooling, 40 ml of the extract is poured, combining it with the first two portions of the extract, the resulting liquid extract is settled in a cold dark place for 3 days at a temperature not exceeding 8 ° C, filtered and the extractant is removed to a moisture content of not more than 25%.