RU2688688C2 - Agent for treatment of inflammatory diseases of upper and lower airways - Google Patents

Abstract

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention refers to pharmaceutical industry, namely to an agent for treating inflammatory diseases of the upper and lower airways. An agent for treating inflammatory diseases of the upper and lower airways, which is a dry extract of nanopowder of aspen bark (Populus tremula L.), with dimensions of nanopowder of 50–150 nm, containing as biologically active substances: salicin 3.8–5.5 wt. %, arabinogalactanes 4.2–10.1 wt. %, polyphenols 3.9–7.2 wt. %.

EFFECT: agent described above has high efficacy in treating inflammatory diseases of the upper and lower airways.

1 cl, 2 ex

Description

The invention relates to medicine and herbal medicine, namely to herbal medicines, and can be used in complex pharmacotherapy for the treatment of respiratory organs.

Respiratory lesions occupy a leading place in the infectious pathology of various organs and systems, traditionally being the most widespread among the population, which affects both adults and children. Infection, as a rule, occurs through airborne droplets, as a result of which the infection settles in the respiratory organs.

Respiratory tract infections are acute diseases that occur as a result of ingress of infectious agents through the aerogenic mechanism of infection, that is, contagious, affecting the respiratory system, both primary and secondary, accompanied by inflammatory phenomena and characteristic clinical symptoms.

The main cause of respiratory diseases - microorganisms (bacteria, viruses, fungi, less parasites). The leading role is played by such bacterial pathogens as: pneumococci, hemophilus bacillus, mycoplasma, chlamydia, legionella (these pathogens cause mainly pneumonia), mycobacterium tuberculosis, influenza viruses type A and B. More often the disease is caused by one type of pathogen (monoinfection), but sometimes (old age, AIDS and other immunodeficiency diseases) there may be several (mixed infections).

Conventionally, all diseases of the respiratory tract can be divided into infections of the upper or lower parts. The most common of them are pharyngitis, laryngitis, and sinusitis, various pharyngeal inflammations. The most common diseases of the lower respiratory tract include inflammation of the lungs, bronchitis and tuberculosis. In addition, some of these diseases can affect both upper respiratory tract and lower respiratory tract.

A number of synthetic drugs have been developed for the treatment of any respiratory diseases. Their disadvantages are the rapid emergence of drug resistance to these drugs, the emergence of various toxic reactions from the liver, gastrointestinal tract and nervous system, weakening of the immune status.

The most severe diseases affecting the respiratory tract include bronchitis, pneumonia and tuberculosis. Modern pharmacotherapy of respiratory diseases is based on the integrated use of antibacterial drugs and immunostimulants, hormonal drugs and mucolytic agents. Their action is usually accompanied by side effects, the severity of which increases with their combined use. All this necessitates the search for new safe means.

To prevent or reduce the side effects arising from the pharmacotherapy of respiratory diseases, allow medicinal plants such as coltsfoot, oregano, licorice, wild rosemary and fees based on them (Pat. 0213 094). In the course of complex therapy of pulmonary tuberculosis, pneumonia, bronchitis, phytocompositions are additionally used, used against the background of antibacterial therapy or independently (US Pat. No. 2223107, 2362577, 2174402).

Closest to the proposed is a febrifuge, which is a powder from the bark of aspen, crushed to size 50-90 nm (RF patent №2431495) and the method of its production by drying and grinding vegetable raw materials, affecting the raw material by grinding bodies in planetary mills.

The effectiveness of this tool is insufficient, since the availability of biologically active substances is small, they are not fully recovered in the target product.

The objective of the invention is the creation of effective tools for the treatment of respiratory organs from plant materials that do not have toxic effects on the body, reducing and preventing side effects when used in complex treatment, improving the functional state of the respiratory system, increasing the effectiveness of its biological effect on the body (bioavailability).

The technical result is to increase the effectiveness of inflammatory diseases of the upper and lower respiratory tract, namely, bronchitis, pneumonia, as well as in complex therapy of tuberculosis, increasing the availability of complex biologically active substances.

The technical result is achieved by the use of an agent containing as the active principle a complex of biologically active substances: salicin 3.8-5.5% by weight, arabinogalactans 4-10% by weight, polyphenols 4-7% by weight, which is a dry extract, obtained from nanopowder (50-150 nm) of aspen bark (Populus tremula L.). The product is obtained from aspen bark collected during sap flow, which is crushed in a knife mill to a particle size of 1-2 mm, after it is dried to a moisture content of 8-10%, is dispersed in a roller type mill to a particle size of 50-150 nm, then subjected to water extraction by repercolation, the combined extract after settling concentrated in vacuo to 70% solids at 50 ° C, followed by drying to dry powder in vacuum.

Grinding and extraction of raw materials allows you to fully destroy the intermolecular and interaggregative bonds of the components and translate biologically active substances into a free state, which increases the yield of the target product with an increased content of active substances. The proposed tool is able to integrate into the cell wall and enter the cells of mycobacteria, disrupting their metabolism, which leads to the death of microorganisms. Phenol glycosides (salicin, salicortin, tremuloidin, tremulacin) inhibit the activity of the central transcription factor of inflammation and act as a hepatoprotector due to antioxidant properties. Arabinogalactans have an immunotropic effect, have an activating effect on macrophage cells, stimulating phagocytosis (Islamova Zh.I., Malikova M.Kh., Khushbaktova ZA, and others. Experimental evaluation of the immunotropic action of arabinogalactan and pectin polysaccharides from querist // // Experimental and Clinical Pharmacology. 2016. V. 79. No. 6. S. 12-14).

Polyphenols have an antimicrobial effect, antiviral activity and antioxidant properties of polyphenols have also been proven (Pisarev D.I., Novikov O.O., Selutin O.A., Pisareva N.A. Biological activity of plant polyphenols. Perspective of using anthocyanins in medical practice / Scientific statements of Belgorod State University, 2012. No. 10. 8 p .; Filipenko, T. A., Gribova, N. Yu., Antioxidant effect of extracts of medicinal plants and fractions of their phenolic compounds, Chemistry of Plant Raw Materials, 2012. No. 1. 5 s).

The yield of the target product is 21-26% wt. The content of salicin is 3.8–5.5% wt, arabinogalactans 4.2–10.1% wt, polyphenols 3.9–7.2 wt.%

The bioavailability of the drug, determined at the base department of pharmaceutical technology and biotechnology of the Siberian State Medical University, is 85%.

The study of the specific activity of the proposed agent was carried out in vivo in male inbred C57BL \ 6 mice from the vivarium of the Central Research Institute of Aviation Problems of the Russian Academy of Medical Sciences. Mice were infected by intravenous administration of M. tuberculosis strain Y37Rv. In the groups of animals receiving the complex therapy with isoniazid and the proposed remedy, a month after the infection, myobacteria were sown 100 times less than the group of animals receiving isoniazid monotherapy.

The following clinical observations.

Example 1

A group of patients (18 people) in the treatment of acute bronchitis. The diagnosis was made on the basis of a clinical auscultative pattern (malaise, cough, fever up to 38 ° C, hard breathing, dispersed dry rales in 7 people, in 1 patient dry and moist medium bubbling rales). In this case, radiodiagnosis was not shown and therefore was not performed. Patients were prescribed the proposed remedy for adults to 6 g, children 4-6 years old to 2 g, children 7-12 years old to 4 g per reception 3 times a day 30-40 minutes after meals with an interval of 6 hours. The course of treatment was 12 days. The age of patients ranged from 4 years to 70 years. After the course of treatment, the disappearance of subfebrile and symptoms of intoxication was noted. The phenomena of bronchitis disappeared by the end of the course of treatment with a dry extract of nanopowder aspen bark. In all patients, the temperature returned to normal, the general condition and state of health improved, the cough disappeared, and the auscultational pattern in the lungs returned to normal. No other therapy was performed in all clinical groups. Anti-inflammatory effect is also ascertained from other organs and systems.

Example 2

The study of the clinical efficacy of the proposed agent in the complex therapy of pulmonary tuberculosis was carried out at the Department of Phthisiology of the Kemerovo State Medical Academy. 102 patients with newly diagnosed tuberculosis or relapse from 18 to 70 years were studied. The main group - 62 people received anti-tuberculosis polychemotherapy + the proposed remedy (30 days). The control group - 40 people standard therapy (isoniazid + rifampicin + ethambutol + pyrazinamide or streptomycin). In the group of patients who received the proposed remedy, the best tolerability of anti-TB drugs was noted with a decrease in the incidence of toxic reactions. There was a cessation of m / b discharge with sputum in 63% of patients, resorption of infiltrate in the lungs in 49%, closure of cavities in 7%. The proposed tool prevents the development of severe adverse reactions, which often occur during anti-tuberculosis chemotherapy. The use of the drug together with traditional anti-TB drugs allows you to quickly achieve abacillation, removal of intoxication. Reducing the side effects of anti-TB drugs, preventing their occurrence allows for the treatment of tuberculosis in full, which in turn leads to a high level of clinical cure for tuberculosis.

The proposed tool has antibacterial, hepatoprotective, anti-inflammatory, action due to the complex effect of biologically active substances isolated from the bark of aspen (Populus tremula L), increased bioavailability. The proposed herbal remedy does not have a side effect on the body.

Claims (1)

Means for the treatment of inflammatory diseases of the upper and lower respiratory tract, which is a dry extract of aspen nanopowder (Populus tremula L.), with a nanopowder size of 50-150 nm, containing as biologically active substances: salicin 3.8-5.5% wt ., arabinogalactans 4.2-10.1% wt., polyphenols 3.9-7.2% wt.