RU2578453C1 - Collection of medicinal plants of nootropic action - Google Patents

Abstract

FIELD: pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely to collection of medicinal plants with nootropic activity. Herbal tea possessing nootropic activity, including meadowsweet herb, common alchemillae herba, sprouts of whortleberry, leather bergenia green leaves taken in certain proportions.

EFFECT: above herbal tea has nootropic activity with high therapeutic efficacy.

1 cl, 2 tbl, 5 ex

Description

The invention relates to medicine, specifically to clinical pharmacology, and can be used for pharmacological correction of disorders of higher nervous activity in diseases of the central nervous system and relates to fees with nootropic effects obtained from plant materials.

The synthetic drugs used to treat these diseases do not always satisfy the requirements of clinical pharmacology in their therapeutic effectiveness, primarily due to the presence of a number of side effects: increased irritability, anxiety, sleep disturbance, tremor, increased tendon reflexes, dizziness, and also dyspeptic disorders, increased coronary insufficiency, increased blood pressure, subfebrile condition, allergic reactions, changes in blood picture and condition internal organs, which limits their use, particularly in terms of work [1, 2]. The collection of medicinal plants can play a significant role in solving this problem.

An adequate prototype was not found in the literature.

It is known to use a condensed extract of Prince of Siberia (RF patent No. 2276992, IPC A61K 36/71, 9/20, publ. 2006), dry birch bark extract (RF patent No. 2300389, IPC A61K 36 / 18B, 25/00, publ. 2007), aqueous or aqueous-ethanol or carbon dioxide extracts of plants of the forget-me-not genus (Myosotis) (RF patent No. 2335293, IPC A61K 36/30, 25/08, 25/28, publ. 2008), 40% alcohol extract plant materials (grass of dried mashmallow, roots of Scutellaria baicalensis, shoots of shrubs, shamrocks, rhizome of a bloodthirsty pharmacy, roots of peony evading, rose hips and grass of the mountaineer pt. whose) (RF patent No. 2331432, IPC A61K 36/739, 36/53, 36/65, 36/704, 36/28, 25/28, publ. 2008), 70% alcohol extract of hairy root culture of the roots of Scutellaria Baikal Scutellaria baicalensis Georgi (RF patent No. 2438691, IPC A61K 36/539, 25/00, 25/28, 35/00, 11/02, publ. 2012) as a nootropic agent. However, these agents are not effective enough due to their low bioavailability due to the weak or lack of such a pronounced effect on vascular microcirculation, hepatoprotective effects, as well as adaptogenic and immunotropic effects. In addition, these tools require the use of ethyl alcohol or other solvents, which complicates and increases the cost of the process of obtaining and subsequent use by patients. The use of fees is characterized by a complex effect of exposure, preservation of the nativeness of biologically active substances and, as a consequence, a pronounced pharmacological effect, as well as ease of use. In the literature there are no data on the use of collections of medicinal plants of nootropic action.

The objective of the invention is to expand the arsenal of herbal remedies for the protection of the central nervous system with nootropic effects.

The problem is solved by using, as a collection of medicinal plants, having a nootropic effect, the composition in the following ratio of components,%: grass of meadowsweet (20-30), grass of the common cuff (10-20), shoots of common blueberry (10-20) and green leaves of frankincense (40-50).

It is new that for the first time as a collection of medicinal plants with a nootropic effect, they use a composition containing grass of the meadowsweet, cuff grass, common blueberry shoots and green leaves of the frangipani.

The collection is obtained by mechanical mixing of pre-dried and crushed grass of meadowsweet herb, grass cuff ordinary, shoots of common blueberry and green leaves of frankincense. Herbs, shoots and leaves were crushed to particles no larger than 5 mm in size. In all cases, the crushed dust was sieved through a sieve with a hole diameter of 0.18-0.2 mm.

The components added to the collection have the following characteristics:

1. The grass of the creeping foliage (Filipendula ulmaria (L.) Maxim.) Contains simple phenols (spirein, monotropitin, rhododendrol, saligenin, salicin, isosalicin), flavonoids (quercetin, campferol, apigenin, luteolin, taxifolin, isoquercin, isovert spireoside, 4'-O-β-D-galactopyranoside quercetin, rutin), organic acids (benzoic, salicylic, m-hydroxybenzoic, anisic, vanillic, gentisic, gallic, p-coumaric, coffee, chlorogenic, ferulic, quinic) substances (hydrolyzable, including ellagic acid), triterpene compounds (ursolic, oleanolic acid), amines, amino acids (valine, glutamic acid, histidine) and inorganic components, thus improving integrative indicators of brain activity in normal and pathological conditions (for example, against the background of caffeine intoxication), has antistress, adaptogenic, nootropic, anxiolytic, hepatoprotective and immunotropic effects. Using this component allows you to avoid some side effects of nootropics (increased irritability, anxiety, sleep disturbance, dizziness, dyspeptic disorders, changes in blood picture and condition of internal organs).

2. The grass of the common cuff (Alchemilla vulgaris L.) contains simple phenols (arbutin), flavonoids (luteolin, apigenin, campferol, quercetin, hyperoside, luteolin-7-glucoside, apigenin-7-glucoside, rutin), phenol carboxylic acids (gallic, coffee, chlorogenic, ellagic, luteonic), tannins (ellagotanins: agrimonin, laevigatin, pedunculagin), polysaccharides, vitamins (ascorbic acid, riboflavin), nitrous bases of nucleic acids, amino acids (valine, leucine, isoleucine, threonine, lysonine, methylene chloride phenylalanine, proline, oxylysine, asp araginic and glutamic acids, glycine), macro- and microelements, which provides hemorheological, hypolipidemic, nootropic, as well as hypoglycemic, lymphotropic and immunocorrective effects, which improves the bioavailability of biologically active substances.

3. The shoots of common blueberries (Vaccinium myrtillus L.) contain simple phenols (hydroquinone, rhododendrol, rhododendrin, arbutin), flavonoids (including anthocyanins), phenol carboxylic acids (gallic, vanillic, gentisic, coffee, ferulic, chlorogenic) umbelliferone, esculletin, scopoletin, fraksetin), hydrolyzable tannins, triterpene compounds (α-amyrin, oleanolic, ursolic acids), amino acids (valine, threonine), contribute to the manifestation of nootropic, antioxidant, as well as antidiabetic effects, attached with Boron expressed properties to improve vascular microcirculation of the brain, which additionally provides greater bioavailability, contributing to the effects of biologically active substances at the cellular level.

4. The green leaves of the frangipani (Bergenia crassifolia (L.) Fritsch.) Contain simple phenols (hydroquinone, arbutin), flavonoids (quercetin, kempferol, apigenin, luteolin, taxifolin, isocvercitrin, rutin), phenolcarboxylic gentinic acid (gallic acid) , ferulic, chlorogenic), coumarins (bergenin, esculletin), hydrolyzable and condensed tannins, polysaccharides, carotenoids, amino acids, which contributes to the effective improvement of the learning process and memory in the norm, as well as in various pathological conditions, is caused t pronounced antihypoxic, adaptogenic and antioxidant activity.

Therefore, the claimed collection improves indicators of integrative brain activity: memory, stimulates learning processes (especially if they are disturbed), increases the level of brain wakefulness and the body's resistance to harmful factors (hypoxia, intoxication, trauma, stress, etc.), as well as vascular microcirculation , increases the body's adaptation along with hepatoprotective and immunotropic effects.

There is no data in the literature on the use, as a collection of medicinal plants, which has a nootropic effect, of a composition containing grass of meadowsweet, cuff grass, common blueberry shoots and green leaves of frangipani.

Components and their contents are selected experimentally. The use of herb meadowsweet, cuff grass, common blueberry shoots and green leaves of frankincense in the collection for the proposed purpose was made possible by identifying experimentally its new properties, namely the ability to normalize the central nervous system due to the nootropic effect.

The new collection, which contains grass of the meadowsweet (20-30%), grass of the common cuff (10-20%), shoots of common bilberry (10-20%) and green leaves of frangipani (40-50%), showed as a result of the experimental studying the nootropic effect.

New properties and the composition of the collection, do not explicitly follow from the prior art in this field and are not obvious to a specialist. It was established for the first time that, as a collection of medicinal plants with a nootropic effect, one can use a composition containing grass of the meadowsweet herb, grass of the common cuff, shoots of common bilberry and green leaves of the frangipani.

An identical set of medicinal plants was not found in the patent and medical literature.

The proposed collection of medicinal plants can be successfully used in practical health care for the correction of central nervous system diseases.

Based on the foregoing, the present invention should be considered relevant to the conditions of patentability "Novelty", "Inventive step", "Industrial applicability".

The invention will be clear from the following description.

Example 1. Grass of meadowsweet grass (Filipendula ulmaria (L.) Maxim.), Grass of common cuff (Alchemilla vulgaris L.), shoots of common blueberry (Vaccinium myrtillus L.), green leaves of frangipani (Bergenia crassifolia (L.) Fritsch. ) dried by air, crushed to a fine powder (humidity 6.5%) (PS).

Example 2. The preparation of the broth is carried out as follows: 10.0 g of the collection is filled with 120 ml of water (1:10, taking into account the coefficient of water absorption), heated in a boiling water bath for 30 minutes, filtered hot, squeezed out the raw materials, after cooling, the volume of the resulting broth is adjusted with water up to 100 ml (OS).

Example 3. The preparation of the infusion is carried out as follows: 10.0 g of collection is poured into 120 ml of water (1:10, taking into account the coefficient of water absorption), heated in a boiling water bath for 15 minutes, filtered hot, squeezed out raw materials, after cooling, the volume of the resulting broth is adjusted with water up to 100 ml (HC).

Pharmacological studies were performed on 72 CD-I male outbred mice (category I, according to the certificate) weighing 20-22 g. Animals were obtained from the Department of Experimental Biological Models of the Federal State Budget Scientific Institution Scientific Research Institute of Pharmacology and Regenerative Medicine named after E. D. . Goldberg "(Tomsk). The experiments were carried out in the winter. Work in the framework of experimental methods was carried out from 9 to 15 hours. The animals were kept in standard vivarium conditions on a normal feeding diet (except in cases where other conditions are specifically agreed) in accordance with the rules adopted by the European Convention for the Protection of Vertebrate Animals Used for Experimental and scientific goals (Strasbourg, 1986).

The pharmacological effects of the new collection, which contains grass of meadowsweet, cuff grass, common blueberry shoots and green leaves of coniferous leaves, were evaluated by the effect on cognitive-mnemonic functions after hypoxic exposure, modeled under the conditions of hermetic hypoxia [3].

Dried crushed collection, broth and infusion of plant collection were administered daily in an animal course for 5 days through a tube into the stomach in the form of a solution or suspension in water 1 hour before the start of experimental manipulations. Dried, crushed to a fine powder collection was introduced at a dose of 500 mg / kg. The dose of decoction and infusion was 5 ml / kg. This dose corresponds to the amount of collection (powder) by the content of extractives. The indicated doses were determined as the most active in preliminary experiments. As a comparison drug (prototype), a dry extract of the root of Scutellaria baicalensis (Scutellaria baicalensis Georgi) was used at a dose of 50 mg / kg. Animals of the control groups received an equivalent amount of water.

The obtained experimental data were processed statistically. The significance of the differences was judged by testing the probability of the null hypothesis using the Student t test and the Fisher angular method for comparing fractions. Differences were considered significant at p≤0.05.

Example 4: Orientation-research behavior was studied in the context of the “open field” model, which is one of the most commonly used methodological methods used to judge the functional state of the central nervous system [4]. The “open field” experimental setup is a 40 × 40 × 20 cm camera with a square floor and white walls. Its floor, divided into 16 squares, has in each of them a circular hole with a diameter of 3 cm. From above, the camera is illuminated by an electric incandescent lamp with a power of 100 W, located at a height of 1 m from the floor. The mouse is placed in one of the corners of the chamber and within 2 minutes the number of movements from square to square (horizontal activity), the number of stands on the hind legs (vertical activity), the number of hole examinations (mink reflex), the number of washings (grooming) and the number of acts are recorded defecation by the number of fecal balls (boluses).

The transferred hypoxic injury causes violations of the exploitative behavior of animals. In the group of hypoxic control, a decrease in orientational research activity (horizontal movements and vertical struts, mink reflex) is observed by a factor of 4.6 relative to intact animals (Table 1).

The course introduction of the proposed collection in the form of a powder, decoction, infusion containing grass of meadowsweet herb, grass of the common cuff, shoots of common blueberry and green leaves of coniferous leaves exerts a protective effect on the functional state of the central nervous system of animals (Table 1) that underwent hypoxic injury. The use of the collection increases the tentative research activity in the test "open field" when registering 15 minutes after exposure to 2.1-3.1 times compared with animals of the hypoxic control group. The use of a collection in the form of a powder, decoction or infusion helps to restore indicators of exploratory behavior mainly by increasing horizontal and vertical activities, and a mink reflex. With the introduction of broth and infusion, a more pronounced increase in motor activity is noted in comparison with the group of hypoxic control, especially horizontal movements and vertical racks. However, in comparison with them, the comparison drug has a less restorative effect on the orientational research behavior of animals that suffered a hypoxic injury.

Example 5: The effect on learning and memory was studied in the development and reproduction of the conditioned reflex of passive avoidance (passive avoidance avoidance). The passive avoidance reaction [5] is based on the suppression of the innate reflex of preference for dark space in rodents. The experimental setup is a camera consisting of two compartments - large (light) and small (dark). The animal is placed in the light compartment and after a while it goes into the dark one, after which the hole connecting the two compartments is closed with a door and the electric compartment is supplied with pulses of 50 ms duration, frequency 5 Hz and amplitude, onto the floor of the dark compartment, which is a grid of parallel alternating electrodes 50 mA After 10 seconds, the door is opened and the animal can jump out into the bright compartment with the usual floor. As a result of the described procedure, a conditioned reflex of avoiding dark space is developed in animals. When checking the reflex, the animal is placed in the corner of the chamber of the bright compartment, opposite from the entrance, and observed for 3 minutes The time of the first entry into the dark compartment (latent time of entry), the total time spent in the dark compartment, the number of animals with a developed reflex are recorded. The criterion for the presence of a reflex is the absence of an animal entering the dark compartment for 3 minutes from the moment the mouse was placed in a bright chamber. Checking the safety of the reflex is carried out on 14 and 21 days after the development of the reflex.

The transferred hypoxic effect contributes to the deterioration of the passive avoidance reaction during its testing in the group of hypoxic control, which indicates a violation of conditioned-reflex behavior in animals (Table 2).

The course introduction of the proposed collection in the form of a powder, decoction, infusion containing grass of meadowsweet herb, grass of the common cuff, shoots of common blueberry and green leaves of coniferous leaves, increases the preservation of passive avoidance reaction and promotes reproducibility of the reflex from 70 to 90% when tested on 14 and 21 days after production in animals after hypoxic injury (table. 2). In this case, the comparison drug is significantly inferior to all objects of research (powder, broth, infusion of the collection) in reproducibility of the conditioned reflex in the early stages (14 days) during the test.

Thus, when studying the influence of the collection containing the grass of the meadowsweet, the cuff grass, the bilberry shoots and the green leaves of the frangipani, on some indicators of the state of the central nervous system of experimental animals (increased passive avoidance reaction and motor activity after hypoxic exposure), its pronounced nootropic effect was established, superior extract of Scutellaria baicalensis (reference drug) in terms of recovery of indicative research behavior and reproducibility of the conditioned reflex in the early stages after a hypoxic injury.

Based on the conducted experimental studies, it can be concluded that the use of a collection containing grass of meadowsweet herb, grass of the common cuff, shoots of common bilberry and green leaves of frangipani is promising for a higher therapeutic effect.

The technical result is achieved through the use of a collection containing grass of meadowsweet, cuff grass, common blueberry shoots and green leaves of frankincense, as nootropic, which allowed to expand the arsenal of herbal remedies with nootropic effect, with increased therapeutic efficacy. Literature

1. Mashkovsky M.D. Medicines - M: New Wave, 2002. - T. 1. - S. 31-142.

2. Malin D.I. Side effect of psychotropic drugs. - M.: University Book, 2000 .-- S. 184-189.

3. Guidelines for preclinical studies of drugs / ed. A.N. Mironova. - M.: Grif and K, 2012 .-- S. 276-296.

4. Walsh R.N., Cummins R.A. The open - field test: a critical review // Psychol. Bull. - 1976. - V. 83. - P. 482-504.

5. Buresh Ya., Bureshova O., Houston J.P. Techniques and basic experiments on the study of the brain and behavior. - M .: Higher school, 1991 .-- 175-177.

Claims (1)

The collection of medicinal plants of nootropic action, including the grass of the meadowsweet, the grass of the cuff ordinary, shoots of common blueberry and the green leaves of the frangipani in the following ratio,%:
herb meadowsweet 20-30,
grass cuff ordinary 10-20,
shoots of common blueberries 10-20,
green leaves of 40–50 bladia.