RU2137496C1 - Preparation "kardiofit" for treatment of patients with cardiovascular diseases - Google Patents

Abstract

FIELD: medicine, cardiology, phytotherapy. SUBSTANCE: invention relates to the development of the preparation "Kardiofit" used for treatment of patients with cardiovascular diseases. Preparation provides cardiotonic, coronarolytic, hypotensive, antihypoxic, antithrombic and sedative effects and excludes the appearance of adverse effects. Preparation has a tincture consisting of 14 medicinal plants prepared on 40% ethyl alcohol. Preparation shows good therapeutic effect, promotes the retention of optimal working capability, decreases the development of diencephalic damages and improves the body state at physical loading. EFFECT: enhanced effectiveness of the preparation. 1 cl, 4 tbl

Description

 The invention relates to medicine, namely to the creation of a pharmaceutical product from plant materials for the treatment of cardiovascular diseases. The widespread spread of cardiovascular diseases throughout the world requires the constant creation of sufficiently effective and low-toxic drugs for their treatment and prevention. In a long series of various medicinal products, preparations made from medicinal plants occupy a significant place, their role has not lost significance to date.

 Known anti-ischemic agent (US Pat. RF N 2022561, A 61 K 35/78) containing an alcohol extract from the roots of Rhodiola rosea (50% alcoholic extract of industrial production).

 Known tonic "Eleutar" for the treatment of cardiovascular diseases and diseases of the central nervous system (US Pat. RF N 2005481, A 61 K 35/78), containing tincture of aralia and eleutherococcus extract with a ratio of components "tincture: extract" 1: 1, 5 - 1: 2.5.

 Known tools are easy to use, as they are ready for use and have a shelf life of 2 years.

 However, they have a narrowly targeted effect, can cause side effects with prolonged use and have a slight pharmacological effect.

Known drug from medicinal plants - tea collection "Kratevalin" (US Pat. RF N 2045276, A 61 K 35/78), containing infusion of rhizomes with valerian roots, hop inflorescences, dioecious nettle leaves and blood-red hawthorn inflorescences in the following ratio of components , wt.%:
Valerian root - 0.4 - 0.6
Stinging nettle leaf - 0.4-0.6
Inflorescences of hawthorn blood red - 0.4-0.6
Inflorescences of common hop - 0.06 - 0.08
Water - Else
A well-known drug provides the elimination of heartbeat, improves blood circulation to the heart muscle and brain. However, this drug does not provide cardiotonic, coronarolytic and hypertensive effects. And since this drug is a water tincture, the need for its preliminary preparation and shelf life not exceeding 7 days limits its use.

Known drug-collection for the treatment of cardiovascular diseases "<CORDIS>" (US Pat. RF N 2000807, A 61 K 35/78), including hawthorn fruit, a string of grass, marigold flowers, peppermint, motherwort, nettle and oregano, leaves bearberry and sage, valerian root, fennel and carrot seeds in the following ratio of components, wt.%:
Hawthorn fruits - 10
Grass string - 12
Calendula flowers - 4
Peppermint Herb - 24
Motherwort Grass - 16
Nettle grass - 12
Oregano Grass - 4
Bearberry leaves - 4
Sage Leaves - 4
Valerian Root - 6
Fennel Seeds - 2
Carrot Seeds - 2
or by weight, respectively 5; 6; 2; 12; eight; 6; 2; 2; 2; 3; l; l).

 This drug has mild cardiotonic, coronarolytic and sedative effects, to a greater extent it provides an enuretic effect. Like the above analogues, this drug is an aqueous solution.

Known drug tincture for the treatment and prevention of cardiac neurosis, stress, hypertension, radiophobia "LON-5" (US Pat. N 12375, A 61 K 35/78), containing water tincture of hawthorn flowers, hop cones, mint leaves pepper, yarrow and rhizomes with valerian roots in the following ratio of components, wt.%:
Hawthorn flowers - 40
Hop Cones - 10
Peppermint Leaves - 10
Yarrow Grass - 20
Rhizomes with valerian roots - 20
This drug does not have a cardiotonic and balanced hemodynamic effect and, as the above fees, is an aqueous solution. This drug is selected as a prototype.

 The basis of the present invention is the task of creating a drug for the treatment of cardiovascular diseases, which would have cardiotonic, coronarolytic, antihypertensive, antihypoxic, antithrombotic and sedative effects, would eliminate the occurrence of side effects, and would also expand the arsenal of medicinal plants for the treatment of these diseases.

The solution to this problem is provided by the fact that the preparation for the treatment of cardiovascular diseases "Cardiofit" containing hawthorn flowers, peppermint leaves and rhizomes with valerian roots, according to the invention additionally contains spring adolescent grass, clover, lily of the valley, motherwort and thyme, fruits of shrub amorphous , black elderberry flowers, nettle leaves and white mistletoe fresh, horse chestnut and rhizome seeds with licorice roots in 40% ethanol in the following ratio, wt.%:
Hawthorn flowers - 0.6 - 0.8
Elderberry flowers black - 0.6 - 0.8
Peppermint leaves - 0.6 - 0.8
Nettle leaves - 0.3 - 0.5
Fresh mistletoe white leaves - 0.5 - 0.6
Spring adonis grass - 0.6 - 0.8
Melilot grass - 0.6-0.8
Lily of the valley grass - 0.6 - 0.8
Motherwort grass - 0.6 - 0.8
Thyme herb - 0.6 - 0.8
Fruits of amorphous shrub - 0.6 - 0.8
Rhizomes with valerian roots - 0.9 - 1.1
Rhizomes with licorice roots - 0.6 - 0.8
Seeds of horse chestnut ordinary - 0.9 - 1.2
Ethyl Alcohol 40% - Else
The 14 medicinal plants that make up the Cardiofit preparation significantly complement each other, forming a single complex that provides the drug with a wide range of pharmacological activity in the pharmacotherapy of diseases of the cardiovascular system:
- coronary heart disease;
- cardiosclerosis;
- vegetative-vascular dystonia;
- heart neurosis;
- paroxysmal tachycardia;
- heart failure;
- hypertension;
as well as concomitant diseases of the thyroid gland and kidneys, psychoses and epilepsy.

 The ratio of the components in 40% ethanol of the proposed drug is adjusted with the total number of biologically active substances that make up the plants used, based on clinical trials conducted in the Clinical Pharmacology Department of the Ural Scientific Research Institute of Cardiology. Acad. ND Strazhesko, as well as on the basis of therapeutic and cardiology departments of the Department of Hospital Therapy N 2 of the National Medical University named after A.A. Bogomolets.

 Spring adonis herb has a cardiotonic, diuretic, and moderately sedative effect. The widespread use of adonis is due primarily to the content of cardiac glycosides in it. As the research results show, the glycosides contained in the adonis slow down the heart rate and lengthen the diastole. As a result of this, they increase the stroke volume.

 The second distinguishing feature in the pharmacological characteristics of the adonis is its diuretic effect. Two aspects are of primary importance for obtaining this effect - the improvement of blood circulation, which leads, respectively, to the improvement of blood irrigation of various organs, including the kidneys, and, as a result, to a positive effect on the functioning of the heart, and, secondly, the direct beneficial effect of active principles adonis on urine-forming kidney function.

 The sedative effects of adonis are the third practically used moment of the pharmacological characteristics of this plant.

 The fruits of shrubby amorphous have a cardiotonic and sedative effect. The amorphine glycoside contained in the fruits of the plant has a calming effect on the central nervous system in combination with a cardiotonic effect. It prevents convulsions, causes inhibition of conditioned reflex activity. Amorphine has a positive inotropic and tonotropic and negative chronotropic effect on the heart.

 Hawthorn flowers have a vasodilating, coronary dilating, cardiotonic and sedative effect. Under the action of hawthorn preparations, a significant increase in coronary production occurs, and along with this, myocardial oxygen utilization improves.

 Elderberry flowers have a diaphoretic and diuretic effect. Preparations from black elderberry have analgesic, sedative and weak hypotensive effects. Good therapeutic effects have also been found in sciatica, migraine, trigeminal neuralgia, herpes zoster. Clinical trials of an extract obtained from black elderberry in patients with edema of various origins (renal, heart disease) showed that it increases diuresis and reduces the specific gravity of urine.

 Rhizomes with valerian roots have a calming and antispasmodic effect. Rich clinical data have confirmed valerian and its preparations as well as an effective light sleeping pill. Due to its calming effect, valerian is especially widely used for cardiac neurosis and neurotic states of overstrain, anxiety, agitation, insurance experiences, menopausal disorders, hysteria.

 Melilotus grass has a soothing and calming effect. It has been established that clover coumarins improve conditioned reflex activity.

 Saponin, eocin, contained in the seeds of horse chestnut, reduces blood viscosity and is therefore recommended in the treatment of phlebitis, varicose veins, hemorrhoids, etc. Eocin acts on the sealing of capillaries, which is the basis for the therapeutic effect of this saponin, since the early phase of inflammation is characterized by a violation permeability of capillary walls. Horse chestnut preparations prevent the formation of blood clots in blood vessels and contribute to the spread of blood clots already formed. Along with this, saponins contained in horse chestnut preparations cause a decrease in blood pressure.

 Nettle leaves have a restorative, hemostatic and diuretic effect. This is a well-known and widely used since ancient times medicinal plant. In folk medicine, it is most often used as a hemostatic agent. Nettle is a good remedy against spring fatigue, anemia, increases resistance to various diseases, improves metabolism.

 Lily of the valley grass has a cardiotonic effect. The main lily of the valley glycoside - convallatoxin exerts a similar effect, like other cardiac glycosides - increases blood pressure, which is due to cardiotonic and constricting peripheral vessels. Strengthens heart contractions and minute volume, slows down sinus rhythm and atrioventricular conduction, lowers venous pressure. With perfusion of blood vessels of isolated organs, its direct vasoconstrictor effect is proved. It prolongs the latent period of conditioned reflexes and weakens the unconditioned, which is associated with its action on the subcortical structures. Enhances gastrointestinal motility and diuresis. Not cumulated, well absorbed in the intestines.

 Peppermint leaves have choleretic, antispasmodic, local anesthetic, antiseptic effect. The most significant effect of mint and the essential oil contained in it is their choleretic and choleretic effects. It was established experimentally that extract from mint leaves increases bile secretion by a factor of 9. Mint is excreted from the body with bile and due to this it has an antiseptic effect on bile and bile ducts.

 Peppermint oil, like chamomile essential oil, has a pronounced antispasmodic effect.

 Menthol has a local anesthetic, antispasmodic and carminative effect. When applied topically, it cools the tissues, makes the tactile endings of the nerve fibers numb, causing a vasoconstrictor effect on the peripheral vessels. Peppermint oil, like menthol itself, when taken orally, causes a vasodilatation in some areas, mainly coronary vessels, in a reflex way, which is why menthol is used alone or in combination for coronary spasm. In addition to the local anesthetic effect, menthol also has an antiemetic, choleretic, choleretic, antispasmodic and carminative effect.

 Leaves of mistletoe white have hypotensive and sedative effects. The substances contained in the white mistletoe have an inhibitory effect, prevent or relieve seizures, inhibit the cardiovascular center, and reduce central excitability. White mistletoe preparations mainly due to the overwhelming effect on the centers of the medulla oblongata lower blood pressure. The direct vasodilating effect in a number of areas — the lower extremities and the liver — definitely contributes to this effect. It was established that under experimental conditions the alcoholic extract of white mistletoe has a positive inotropic effect on the heart.

 Motherwort herb has a calming, anticonvulsant and antiarrhythmic effect. The main action of motherwort - anticonvulsant and sedative effect is associated mainly with the presence of a bitter substance in it - leonurin. Motherwort has a good calming effect, and it is used as an additional tool for anticonvulsant treatment, in particular epilepsy.

 Rhizomes with licorice roots have an expectorant, expectorant, diuretic and laxative effect. A good laxative effect is associated with the presence of liquoricin glycoside, which, upon hydrolysis, releases dioxiflavone of a lemon yellow color and is characterized by a softening and antispasmodic effect.

 Thyme herb has an expectorant, antibacterial and antispasmodic effect. Its pharmacological activity is due to the content of essential oil, which includes carvacrol and thymol. Thyme essential oil has a strong bactericidal effect and a weak fungicidal effect. It is highly active against pathogenic fungi, teni and trichocephalus. Thyme herb enhances the secretion of bronchial glands and has an expectorant and antispasmodic effect, due to which it has a good therapeutic effect in acute and chronic bronchitis, whooping cough.

 In the table. 1 shows the composition of the drug "Cardiofit" with different contents of the components. In the table. 2 provides an assessment of the overall clinical efficacy of the drug. In the table. 3 gives a subjective assessment of the effect of the drug. In the table. 4 shows an objective assessment of the effect of the drug.

 The technology of preparation of the drug "Cardiofit" is as follows. 10 kg of ground and carefully mixed medicinal herbs are loaded into the extractor (Table 1, columns 1, 2, 3). From the mixer, pour 100 l of a 40% alcohol solution. The extraction of plant materials is carried out with periodic stirring for 1 hour, followed by settling for 4-5 hours for 7 days. After insisting, the extract obtained is poured into a special collection, the remainder of the extractant in the amount of 20 l is also fed thereto to obtain 100 l of the alcohol-based preparation “Cardiofit”. Thus obtained preparation is additionally defended for 2-3 days, filtered in several stages through a special filter and transferred to packaging.

 As clinical trials have shown, going beyond the boundary values of at least one of the claimed components (Table 1, columns 4-6) leads either to hyper manifestations of sedative and hypotensive effects, which is dangerous for patients with diencephalic disorders, suffering from hypotension and heart failure (if exceeded the indicated magnitude of the components), either to the absence or low pharmacological effect in the treatment of patients with functional and organic diseases of the cardiovascular system (with a decrease in the indicated values components).

Clinical trials in the Department of Clinical Pharmacology of the Institute of Cardiology. Acad. ND Strazhesko conducted as follows. We examined 37 patients — 17 men and 22 women, the average age of 48.1 ⁺ 6.9 years. Patients with coronary heart disease (CHD) 1-P functional class (FC) - 12 people, with hypertension (GB) 1-P degree - 10 people, with neurocircular dystonia (NCD) - 15 people, 8 of them with paroxysmal supraventricular tachyarrhythmias and 12 with supraventricular and ventricular extrasystolic arrhythmias. Patients received routine therapy; sedation and other antidepressant drugs were excluded. As a result of a general clinical examination (including blood biochemistry, ECG and echocardiography), the patients were divided into two groups. The first included 15 people (patients with NDC), in whom complaints of a neurotic nature and some dysfunction of the cardiovascular system (cardialgia, transient arrhythmias, fluctuations in blood pressure (BP)) are associated with peculiarities of nervous regulation. In 22 patients of the second group (with coronary heart disease and hypertension) due to ischemic, persistent hypertensive and endocrine effects (menopause in 8 women), more persistent changes occurred in the myocardium, primarily detected on the ECG.

 The clinical picture of complaints of all patients consisted of cardiac and general neurotic manifestations. In 80% of patients, cardialgia was partially associated with irritation of sensitive nerve fibers in osteochondrosis. In addition, instability, lability of the heart rhythm with a tendency to tachycardia, manifesting themselves spontaneously or inadequately, was determined; blood pressure lability with a tendency to hypertension; respiratory disorders in the form of respiratory arrhythmias and feelings of lack of air ("dreary sighs"); signs of peripheral vascular disorders ("marbling" and cold extremities); signs of autonomic dysfunction (sweating, persistent dermographism); neurotic symptoms (irritability, headache, dizziness, anxiety, anxiety, sleep disturbance); lability of the final part of the ventricular ECG complex (T wave inversion, S-T segment change); positive ECG test with hyperventilation and orthostasis; positive ECG test with potassium chloride and beta-blockers; temporary reversal of a negative T wave during a physical exercise test. Each individual symptom was not very specific, but the plurality of complaints was very characteristic.

 All patients underwent a comprehensive examination according to the standard protocol according to the underlying disease, before and after 10 days of prescribing Cardiofit, 1 teaspoon three times a day.

 As a result of a continuous course of taking the drug “Cardiofit”, the majority of patients showed improvement in well-being, as well as an objectively more favorable course of the disease (Table 2-4).

 In patients of the first group, disorders of the neurohormonal-metabolic regulation of the cardiovascular system were realized in an inadequate response to ordinary stimuli and were expressed in tachycardia (with exertion, hyperventilation or in the orthostatic position), in the fluctuation of vascular tone (with an increase or decrease in blood pressure), inadequate growth cardiac output during exertion, fainting, vascular crises, various non-hazardous arrhythmias. In such patients, a significant decrease in clinical manifestations was observed, and hemodynamic parameters normalized.

 In patients of the second group, hemodynamic features were more specific. So, against the background of basic antihypertensive therapy, we noted an additional decrease in blood pressure by an average of 8.5%, which allowed us to reduce the dose of basic antihypertensive therapy in patients with mild hypertension. The daily fluctuations in blood pressure did not change, the presence of hypertensive conditions was not detected. Against the background of basic antianginal therapy, a weak sedative and antispasmodic effect was noted: the number and severity of anginal attacks decreased, including their daily variability and nitroglycerin intake. There is a problem of the relief of residual cardiac pain after the use of nitrates and analgesics for cardiac pain in patients with coronary artery disease in combination with vegetovascular dystonia (VVD). As you know, this combination of these two pathologies is observed in 78.9% of cases. The effect of "Cardiophyte" can be explained by its properties to normalize conditions with excessive sympathicotonia, as well as an increase in the reduced threshold of pain sensitivity in patients with VVD. The effect of the Cardiofit preparation on the bioelectrical activity of the heart was also revealed: a certain slowdown in the ectopic activity of the myocardium of the atria and ventricles, a decrease in the frequency of heart contractions by 6.7%. No changes in myocardial contractile function were noted.

 Significant psycho-sedative effect along with basic therapy and restorative factors was achieved in 86.8% of patients. High values of the neurotic factor indicate significant anxiety and excitability in combination with rapid exhaustion, asthenia and some weakening of the basic mental functions (sleep, memory, attention, thought process). The sedative effect was caused not only by the normalization of cortical-hypothalamic relationships, but also by the normalization of neurovisceral regulation, so many somatic disorders were reduced. This was most clearly manifested in relation to cardialgic syndrome, rhythm disturbances, peripheral angiospasm, respiratory disorders, etc. The effectiveness of the optimally selected new drug “Cardiofit” was manifested after a 10-day continuous intake. The dynamics of laboratory and other indicators in the treatment process was associated with the severity of vegetative-neurotic manifestations.

 In general, the claimed drug had a mild, balanced hemodynamic effect, smoothed out manifestations of diencephalic disorders, improved the quality of life of patients, tolerance of physical exertion, and contributed to maintaining optimal performance.

 Thus, the Cardiofit preparation has a pronounced sedative effect in all groups of patients with functional (NCD) and organic (IHD and GB) diseases of the cardiovascular system. In case of functional cardiovascular disorders, the Cardiofit preparation has an independent cardiotonic, antiarrhythmic and mild hypotensive effect. For organic diseases of the cardiovascular system, Cardiofit has an optimizing effect on the ongoing basic antianginal, antihypertensive, antiarrhythmic, antihypoxic and antithrombotic therapy due to the pronounced sympatholytic effect, without causing side effects.

Claims (1)

A preparation for the treatment of cardiovascular diseases containing hawthorn flowers, peppermint leaves and rhizomes with valerian roots, characterized in that it additionally contains spring adolescent grass, sweet clover, lily of the valley, motherwort and thyme, amorphous shrubs, black elderberry flowers, nettle leaves and fresh mistletoe, seeds of horse chestnut and rhizome with licorice roots in 40% ethanol in the following ratio, wt.%:
Hawthorn flowers - 0.6-0.8
Elderberry flowers black - 0.6-0.8
Peppermint leaves - 0.6-0.8
Nettle leaves - 0.3-0.5
Fresh mistletoe white leaves - 0.5-0.6
Spring adonis grass - 0.6-0.8
Melilot grass - 0.6-0.8
Lily of the valley grass - 0.6-0.8
Motherwort herb - 0.6-0.8
Thyme herb - 0.6-0.8
Fruits of amorphous shrub - 0.6-0.8
Rhizomes with valerian roots - 0.9-1.1
Rhizomes with licorice roots - 0.6-0.8
Seeds of horse chestnut ordinary - 0.9-1.2
Ethyl Alcohol 40% - Else

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