RU2223108C1 - Agent eliciting sedative, spasmolytic, anti-inflammatory, cholagogic, general tonic and expectorative effect - Google Patents

Abstract

FIELD: medicine, phytotherapy, pharmacy. SUBSTANCE: invention relates to the development of pharmacological agents of vegetable origin eliciting sedative, spasmolytic, anti-inflammatory, cholagogic, general tonic and expectorative effect. Invention proposes an agent comprising pot-marigold flowers, nettle leaves, wild rose fruits, thyme herb, common balm herb, marjoram herb, ethyl alcohol, sugar, color and water taken in the definite ratio of components. Agent shows broad spectrum of pharmacological effect being without adverse symptoms. EFFECT: valuable medicinal properties of agent. 2 cl, 6 tbl

Description

 The invention relates to medicine, namely to the creation of pharmacological agents of plant origin with sedative, antispasmodic, anti-inflammatory, choleretic, restorative and expectorant effect, and can be used in the complex treatment of neurosis, acute respiratory viral infections, acute respiratory infections of the upper respiratory tract, chronic gastrointestinal diseases, to normalize metabolic processes in the body, restoration of mental and physical performance, to increase the overall resistance of the body.

 Currently, sedatives are widely used in medical practice for various neurotic conditions. Of the herbal products, valerian preparations are especially often used, including combined ones, such as valoserdine, valocormide, as well as motherwort and passiflora preparations. Of the modern plant-based sedatives, the drug Novo-Passit (Czech Republic), containing a complex extract of hawthorn, hop, St. John's wort, lemon balm, passionflower, elderberry, valerian and guaifenesin in the form of an alcoholic solution (Russian Radar, 5th ed. - M), should be called .: Remako, 1997/98, p. 638).

 Known use as a sedative tincture of grass roots of peony evasive, which is prescribed for neurasthenic conditions, insomnia, vegetovascular disorders of various etiologies (Sokolov S. Ya., Zamotaev I.P. Handbook of medicinal plants. - M .: Medicine, 1985, p. 52-53).

 Known fortifying agent containing microgranular rosehip extract, dolomite, stearic acid, starch, talc and ascorbic acid in a certain ratio of components (Patent RU 2121360, 1977).

 A known composition having a general strengthening effect, containing wheat germ and sugar and, in the embodiment, an additional licorice root extract dry and microcrystalline cellulose (CMC) (Patent RU 2176514, 2000) with a certain ratio of components.

 It is known that it has anti-inflammatory, restorative and antispasmodic action, used in the form of a 40% alcohol tincture and containing chamomile flowers, roots of meadowsweet, hemopiles, cinquefoil, elecampane and serpentine, eleutherococcus, hawthorn and rosehip leaves, plantain leaf and mother mother stepmothers, and dill seeds in a certain ratio of components (Patent RU 2177796, 2001).

 In the pathology of the gastrointestinal tract, one of the key places is occupied by diseases of the liver and gall bladder, and the most common recurrent inflammation of the gall bladder is chronic cholecystitis. Cholagogue preparations help to restore and maintain patency of the biliary tract due to both stimulation of bile formation and increased excretion of bile from the gallbladder into the intestine. Most choleretic drugs have such a combined effect, enhancing the secretion of bile and facilitating its entry into the intestine.

 Due to the combination of pathology and functional disorders in diseases of the digestive tract, the treatment of chronic cholecystitis and inflammation of the biliary tract with the help of herbal remedies gives a good effect. Tablets (allochol) containing extracts of garlic and nettles, condensed bile and activated charcoal are widely known from choleretic drugs (M.D. Mashkovsky. Medicines, 1997, v. 1, p. 508-509), sandwort flowers, choleretic collections 1 and 2, columns with stigmas of corn, tanatsehol, conflavin, flacumin, etc. (ibid., P. 510-511).

 Known choleretic collection containing immortelle flowers, mint leaf, coriander, birch leaf, tansy flowers, dandelion root, chamomile flowers, dill seed, shoots of marsh rosemary, corn stigmas and centaury grass taken in a certain ratio.

 This collection stimulates the formation of new liver cells, dilutes bile, dissolves the pigmented part of the stones, normalizes the function of the gallbladder (Patent RU 2157230, 1999).

 From herbal preparations with an expectorant effect, in medical practice are widely used products containing thermopsis herb, as well as an extract from this plant, which is part of the cough syrup for adults (list B) (MD Mashkovsky. Medicines, Vol. 13. - Kharkov: Torsing, 1997, v. 1, p. 344-345). For children, drugs based on the marshmallow root are used, including dry marshmallow root extract, marshmallow syrup, breast collections, cough syrup for children (ibid., P. 345). Mukaltin, preparations based on licorice root, roots of istoda and cyanosis, elecampane, plantain leaves, coltsfoot, thyme grass, violets, anise fruits, etc. (ibid., P. 345-349) should also be called.

 Many of these phytopreparations are highly effective in the treatment of certain diseases, however, they have an insufficiently wide pharmacological spectrum, or contain hardly accessible raw materials.

 In the available literature, we did not find a description of a drug that has a sedative, antispasmodic, anti-inflammatory, choleretic, restorative and expectorant effect.

 The objective of the present invention is the creation of a new domestic drug in the form of an elixir with both a sedative, antispasmodic, anti-inflammatory, choleretic, restorative and expectorant effect, without side effects so that it can be used for a long time in everyday, including home practice.

The problem is solved due to the fact that a remedy is proposed that has both a sedative, antispasmodic, anti-inflammatory, choleretic, general strengthening and expectorant effect, containing medicinal plants: calendula flowers, nettle leaves, rose hips, thyme grass, lemon grass, oregano grass, this alcohol , sugar, encoder in water at the following content of components, in g:
Calendula flowers - 1.0-3.0
Nettle leaves - 2.7-4.5
Rose hips - 8.0-14.0
Thyme herb - 2.7-4.5
Lemon balm herb - 2.7-4.5
Oregano grass - 3.0-50.0
Ethyl alcohol 96 ^o - 230.0-250.0
Sugar - 150.0-160.0
Kohler - 30.0-32.0
Purified water - Up to 1000 ml
The claimed tool is made in the dosage form of an aqueous-alcoholic extract and is an elixir of a reddish-brown color, sweet taste with a specific smell.

 The technical result obtained by using the invention is expressed in the expansion of the pharmacological spectrum, the reduction of side effects and the use of domestic raw materials.

The invention is illustrated by the following examples:
Example 1
The claimed tool includes these ingredients at their next content, in g:
Calendula flowers - 1.0
Nettle Leaves - 2.7
Rosehips - 8.0
Thyme herb - 2.7
Melissa herb - 2.7
Oregano Grass - 3.0
Ethyl alcohol 96 ^o - 230,0
Sugar - 150.0
Kohler - 30.0
Purified water - Up to 1000 ml
Example 2
The claimed tool includes these ingredients at their next content, in g:
Calendula flowers - 1.9
Nettle Leaves - 3.6
Rosehips - 11.0
Thyme herb - 3.6
Melissa herb - 3.6
Oregano grass - 32.5
Ethyl alcohol 96 ^o - 239.7
Sugar - 155.0
Kohler - 30.9
Purified water - Up to 1000 ml
Example 3
The claimed tool includes these ingredients at their next content, in g:
Calendula flowers - 3.0
Nettle Leaves - 4.5
Rosehips - 14.0
Thyme herb - 4.5
Melissa herb - 4.5
Oregano grass - 50.0
Ethyl alcohol 96 ^o - 250,0
Sugar - 160.0
Kohler - 32.0
Purified water - Up to 1000 ml
Any change in the qualitative or quantitative parameters of the proposed tool does not provide the claimed technical result.

 The claimed agent is obtained as follows: a raw material consisting of a mixture of crushed medicinal plants, taken in the declared amounts, is poured in a percolator “to the mirror” with 30% ethanol, insisted for 1 day, drained, then poured again “to the mirror” 30% ethanol, insist 1 day, drained, the same is repeated a third time; the alcoholic extracts are combined, mixed, filtered and sugar and color are added.

 All types of medicinal plant materials used in the claimed tool are approved for medical use in the Russian Federation and other countries of the world. The finished product contains terpenoids, flavonoids and free organic acids as the main active ingredients, and the sum of flavonoids in terms of luteolin is at least 0.18 mg / ml, and the amount of free organic acids in terms of malic acid is not less than 1.0 mg / ml.

 The specific activity of the claimed funds was evaluated experimentally on various models, as well as on volunteers.

 The sedative effect of the claimed drug was evaluated by the duration of non-butal sleep. Sleep was induced in white outbred rats after five times seeding with the claimed agent by intraperitoneal administration of sodium ethaminol at a dose of 30 mg / kg and the duration of sleep in animals was recorded.

 The data are presented in table 1. As follows from the experimental data of table 1, the claimed drug has a pronounced sedative effect, increasing the duration of non-butal sleep by 55%.

The antispasmodic activity of the claimed agent was determined by its effect on the tone of the isolated intestines of rats (Magnus method), spasmodic by introducing barium chloride into the nutrient solution. The experiments were carried out on outbred white rats of both sexes weighing 200-220 g. Sections of the duodenum were excised from experimental animals, one end of the segment was attached to a glass hook, and the other to the short shoulder of Engelmann’s lever, then the glass hook was placed in a glass with Tyrode’s solution which during the whole experiment was saturated with air using a glass tube and kept at a constant temperature of 37-38 ^o C. Intestinal cramps were caused by barium chloride at a concentration of 2 • 10 ^-4 g / ml, then recorded on a kimograph tape for 15 sec. After obtaining the initial background, the studied substances were added to the nutrient liquid. The contact time of substances with the intestines was 30-40 seconds. The results of the experiments are presented in table 2.

As follows from the data of table 2, the control at a concentration of 1 • 10 ^-4 g / ml has a weak antispasmodic effect, but does not have a noticeable effect but the tone of smooth muscles; the height of contraction of the isolated intestine of rats caused by barium chloride decreased in the control by 29.0 ± 3.2%. From the data presented in table 2 it is seen that the claimed agent possesses the most pronounced antispasmodic activity, which at a concentration of 1 • 10 ^-4 g / ml relieves spasm by 77.1 ± 8.4%. At the same time, the product as a whole, in contrast to the individual components, sharply reduces the smooth muscle tone of the isolated rat intestines.

 Thus, due to the pronounced sedative and antispasmodic effect, the claimed elixir can be used in the complex treatment of neurosis and neurocirculatory dystonia.

 An experimental study was conducted of the effect of the claimed agent on the rate of bile secretion and on the secretion of its individual components in animals.

 The experiments were carried out on white male Wistar rats weighing 180-240 g, after 12 hours of starvation, access to water is free. The secretion of rat bile components was studied in an acute experiment under nembutal anesthesia of 50 ml / kg by cannulation of the common bile duct after median laparotomy. Studied portions of bile obtained by 1 and 2 hours after drug administration. In each portion, the total bile acid content was determined, and the speed of the bile was calculated. The data are presented in table 3. In the control, a decrease in the concentration of bile acids occurs due to the experimental violation of the hepatic-intestinal circulation of the latter. The inventive tool helps to increase the concentration of bile acids in bile by 1 hour of the experiment by 20%, the speed of the bile increases significantly.

 The anti-inflammatory activity of the claimed drug was evaluated according to the method of Menkin. The studies were performed on 12 outbred white male rats weighing 180-200 g. The inflammatory reaction was reproduced by subcutaneous injection of animals with a 9% solution of acetic acid in a volume of 0.5 ml into the back at the same time as an intraperitoneal injection of a solution of dextral in a dose of 250 mg / kg. The inventive tool in the form of an elixir was administered intragastrically at a dose of 50 mg / kg. The first injection of the elixir was carried out 1 hour before the introduction of acetic acid, then daily 1 time per day for 22 days. Rats in the control group received distilled water in the same doses according to the same scheme. On the 2nd, 14th and 22nd days of the experiment, the area of necrotic tissue was determined. The data are presented in table 4.

 As follows from the data presented in table 4, course injections of the inventive elixir have an anti-inflammatory effect, reducing the degree of tissue alteration when exposed to a phlogogenic agent. Cholagogue and anti-inflammatory effect, combined with sedative antispasmodic and antihypoxic effects, allow the use of elixir in the treatment of chronic inflammatory diseases of the gastrointestinal tract: chronic gastritis with low acidity and chronic cholecystitis.

 Modern studies show that the proportion of fats in the diet of modern man is constantly increasing. However, increasing the fat content in the diet, especially saturated ones (margarines) in combination with a deficiency of vitamins and trace elements, contribute to the development of diseases such as atherosclerosis and coronary heart disease.

 10 volunteers aged 40 to 55 years took the claimed drug in a dose of 15 ml 3 times a day daily for 60 days against a normal diet. The content of total cholesterol, triglycerides, A-lipoproteins and B-lipoproteins was determined in blood serum at the beginning of the experiment, on the 30th day and at the end of the course of treatment. The data are presented in table 5.

 As follows from the data of table 5, by 30 days there was a tendency to normalize lipid metabolism in the body of volunteers who took the claimed drug. At the end of the administration of the claimed agent, the values of biochemical parameters approached the physiological norm, which may indicate the preventive role of the proposed agent in atherosclerosis and myocardial ischemic disease.

The effect of the claimed funds on physical performance in the experiment
The studies were carried out on outbred white rats weighing 170-190 g. Animals were divided into 3 groups of 12 rats in each group. The animals of the experimental and control groups were injected subcutaneously daily with a 50% oil solution of carbon tetrachloride at a rate of 0.3 ml per 100 g of body weight daily for 5 days. Starting from the 3rd day, the animals of the experimental group received the claimed drug at a dose of 2 ml per 100 g of body weight for 8 days. The animals were on a normal diet with free access to water.

 The physical performance of rats was assessed by the duration of the run on a treadmill to complete fatigue.

 The data are presented in table 6.

 As follows from the data of table 6, under the influence of carbon tetrachloride, the physical performance of rats is significantly reduced compared with the intact group / P <0.05 /. The proposed tool increases the duration of running on a treadmill by 60.6% (P <0.05) in relation to the control.

 The study of the claimed funds as a prevention of colds and as an expectorant.

 10 volunteer tourists from 20 to 45 years old took the claimed drug in the recommended dose daily in field conditions for a 15-day trip. The route passed in the mountains at an altitude of 2000-3000 m, during the entire route the weather was unfavorable: cold wind, fog, wet snow. At the same time, the second group of 10 tourists from 18 to 35 years old went the same route and served as control. Adverse meteorological conditions and increased physical activity caused colds in the control group: runny nose, acute respiratory viral infections, tonsillitis, while in the group taking the claimed drug, there were no colds.

 As a continuation of the experiment, 10 people were treated with a control group of tourists with various colds. They were divided into two subgroups of 5 people in each subgroup. The first subgroup took sulfonamide drugs according to the generally accepted scheme, cough syrup, mucaltin, multivitamins for 7 days, the second subgroup took the claimed drug 15 ml 3 times a day for 7 days. After 7 days, the health status in both subgroups was assessed as satisfactory, however, in the first subgroup, two people had an allergic reaction to sulfa drugs, and one person continued to cough; no adverse events were observed in the second subgroup; cough was not observed in all 5 members of the subgroup.

 The expectorant effect of the elixir in combination with antispasmodic, sedative and anti-inflammatory effects allows it to be recommended for use in acute and chronic inflammatory diseases of the upper respiratory tract.

Claims (2)

1. A remedy with a sedative, antispasmodic, anti-inflammatory, choleretic, restorative and expectorant effect, characterized in that it contains medicinal plants: calendula flowers, nettle leaves, rose hips, thyme grass, lemon balm grass, oregano grass, ethyl alcohol, sugar, Kohler and water at the following content of components, g: Calendula flowers 1.0 - 3.0 Nettle leaves 2.7 - 4.5 Rose hips 8,0 - 14,0 Thyme herb 2.7 - 4.5 Oregano grass 3.0 - 50.0 Lemon balm herb 2.7 - 4.5 Ethyl alcohol 96 ° 230.0 - 250.0 Sugar 150.0 - 160.0 Kohler 30.0 - 32.0 Water Up to 1000 ml 2. The tool according to claim 1, characterized in that it is an elixir and is made in the dosage form of an aqueous-alcoholic extract.

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