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Vol 24, No 5 (2021)

Articles

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TECHNOLOGICAL ASPECTS OF OBTAINING MICROCAPSULES OF PLANT ORIGIN SUBSTANCES

Semkina O.A., Dzhavakhyan M.A., Beloshapkina O.M., Gromakova A.N.

Abstract

The review presents data devoted to the specifics of microencapsulation of plant origin drugs, technological aspects of various microencapsulation methods and possibilities of microencapsulation application for solving problems related to the storage and stability of active substances. Domestic and foreign sources of open access literature were analyzed; the following electronic databases were used: PubMed, Elibrary, CyberLeninka and Google Scholar search system. The article presents features of microencapsulation methods and conditions of their application in practice. The limitations of the tech-nigues related to the physico-chemical properties of biologically active substances, namely the aggregate condition, solubility, low decomposition temperatures of active substances, changes in properties when interacting with other components, etc., have been identified. The conditions for efficient microencapsulation process, allowing to obtain particles with the given properties, have been investigated. The main encapsulation methods currently used for obtaining microcapsules are described. The conditions of application of methods for obtaining microcapsules of biologically active substances of plant origin are considered. The medicinal substances derived from plants, depending on the constituent components, reguire certain restrictions, namely the selection of temperature regime, excipients and eguipment, in the use of which the gualitative and guantitative composition of the substance remains unchanged.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(5):5-14
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REVIEW OF METHODS FOR PHARMACEUTICAL ANALYSIS OF SULFUR-CONTAINING ANTIOXIDANTS

Shinko T.G., Terentyeva S.V., Ivanovskaya E.A.

Abstract

Antioxidant protection is an effective and recognized way to control the free-radical oxidative mechanism in live organisms. Antioxidants are widely used in the treatment of hepatitis, atherosclerosis, and malignancies. One of the promising directions for the synthesis of new antioxidants is the inclusion of sulfur in its structures. Sulfur is an element that is easily oxidized and, in addition, is able to bind heavy metal cations. Methods for pharmaceutical analysis of such pharmaceuticals should estimate adeguate the condition of important functional groups and, if it is possible, correlate with antioxidant effect. In this research work methods for guality control of sulfur-containing antioxidant in pharmaceuticals and biosamples are reviewed. For this reason methods for analysis of thioctic acid, probucol, bucillamine and disulfiram, represented in European Pharmacopoeia 8th edition, USP 41, British Pharmacopoeia 2016, Japanese Pharmacopoeia 17th edition, were analysed. It was estimated, that along with reliable pharmacopoeial guantification methods, such as titrimetry, spectrophotometry, and high-performance liguid chromatography, electrochemical methods are being actively developed for the analysis of antioxidants. These methods can be used definitely or as detection for chromatography. Quantitative de- termination based on the redox potential of antioxidants can adequately reflect the functional state of such pharmaceuticals and thus guarantee its efficacy. Due to their high sensitivity and relative ease of sample preparation, electrochemical methods can also be used to determine the content of sulfur-containing antioxidants in biological samples. However, most of the considered methods of analyzing drugs in biosamples are chromatographic. This is because HPLC allow to determine at once pharmaceuticals and its metabolites, and HPLC-MS enable to identify the structure of metabolites.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(5):15-21
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IMPROVEMENT OF CERTAIN NUMERICAL INDICATORS QUALITY OF SOME SPECIES MEDICINAL PLANT RAW MATERIALS CONTAINING FLAVONOIDS

Zhdanov D.A., Kurkin V.A., Braslavsky V.B.

Abstract

Introduction. Currently the particular relevance research in the field standardization of medicinal plant raw materials and medicinal plant preparations. In this relation particular interest, the raw materials of such medicinal plants as Rosa (Rosehip), Tanacetum vul-gare L. (Tansy) and Hypericum (Saint John's Wort), in the case of which the methodological approaches implemented in the State pharmacopoeia of the Russian Federation of the XIV edition are contradictory. Aim. Scientific substantiation of new approaches to guality control and standardization of Rosae fructus, Tanaceti vulgaris flores and Hyperici herba, taking modern data on the chemical composition. Material and methods. Medicinal plant raw materials samples were cultivated in Samara, Orenburg and Voronezh regions, the Krasnodar Territory, the Chuvash Republic and the Republic of Mari El and prepared in the period from 2017 to 2020, as well as commercial samples. Thin-layer chromatography was used for determine the main groups of biologically active substances (BAS). The flavo-noids and anthracene derivatives were guantitative determination by direct and differential UV/VIS-spectroscopy on the Specord 40 (Analytik Jena AG, Germany). Results. The determination of flavonoids as one of the BAS groups in Rosae fructus along with ascorbic acid was justified. The expediency of using a reference solution of cynaroside in determining of the main group of BAS - flavonoids and their guantitative assessment (not less 1.7%) in Tanaceti vulgaris flores was demonstrated. For the Hyperici herba along with flavonoids numerical indicator the need to include a new numerical indicator in the State pharmacopoeia of the Russian Federation - the amount of anthracene derivatives expressed as hypericin (not less 0.1%). Conclusion. According to the results of a phytochemical study of pharmacopoeial species of medicinal plant raw materials containing flavonoids, the expediency of using modern approaches to guality control and standardization of Rosae fructus, Tanaceti vulgaris flores and Hyperici herba was justified.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(5):22-30
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STUDIES OF THE COMPOSITION OF SMOKING MIXTURES CONTAINING SYNTHETIC CANNABINOIDS

Oberenko A.V., Kachin S.V., Sagalakov S.A.

Abstract

Currently, in many countries, including Russia, there is an alarming increase in the consumption of potentially dangerous smoking mixtures containing synthetic cannabinoids (SM-SC). Against the background of a persistent trend of constant change («updates») it is very important to monitor their component composition in order to assess the potential risk of harm to the health of potential consumers and to take adeguate therapeutic measures in the event of drug cases, as well as to establish the source of production and the chain of their illegal distribution. The purpose of the work: a scientific review of publications with the results of component composition studies and the definition of the SM-SC analysis algorithm. An overview of the results of the SM-SC studies was presented. Information on the composition of SM-SC, procedures of sample preparation, methods of identification and determination of the main components and impurities, obtaining and processing chromatographic data were provided. The main components of the mixtures are the matrix, the physiologically active substance and various impurities. The modern classification of SC in accordance with their chemical structure was presented.Recommendations on the selection of profile impurities with identification significance were given. For the determination of volatile impurities, in some cases, it is effective to pre-vapor-phase separation from the matrix, capture from the gas phase with a solid sorbent and liguid microextraction of sorbates for further gas chromatographic (GC) studies. To establish a measure of similarity (difference) between SM-SC samples, numerical methods of processing GC data are used with calculations of Pearson correlation coefficients or Euclidean distances and the construction of corresponding dendrograms. An algorithm for SM-SC analysis was proposed, including visual examination of the sample, GC-MS identification of the physiologically active substance, impurity profiling, selection of target compounds, and mathematical processing of chromatograms. The implementation of the proposed algorithm for the analysis of SM-SC allows us to obtain the most complete information about the component composition of samples, which is very important for assessing their toxicity and taking adeguate therapeutic precautions. Impurity profiling and the selection of target compounds with identification significance, followed by mathematical processing of chromatographic data, are additional tools in determining the measure of similarity (difference) between samples taken from illegal circula-tion.The latter can be used to establish the source of production and the chain of their illegal distribution.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(5):31-37
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AEROGELS' BIOSAFETY ASSESSMENT IN LOCAL TREATMENT OF PURULENT WOUNDS

Legonkova O.A., Korotaeva A.I., Stafford V.V., Ogannisyan A.S., Terekhova R.P.

Abstract

The work is devoted to the study of cerium-based experimental antiseptic samples of draining sorbents in the form of aerogels obtained by lyophilic drying. Their antimicrobial and sorption properties in vitro conditions were studied, and biosafety in purulent wounds' local treatment in the inflammatory phase in vivo conditions were assessed. The studies were carried out in comparative aspect with the powdered sorbent "Klarisorb-A" used in clinical practice, intended for treatment of various etiologies exudating and bleeding wounds, in particular, infected wounds in the first phase of the wound process with microbial contamination level of 104 - 106 CFU/cm2. It was found that there were no fundamental differences in restoration of dermis layers and scar tissue'sformationwith the local application of various draining sorbents, and the use of cerium leads to increase of mast cells' number in dermis, which indicates a higher local immunity. The technique of purulent woundforming during in vivo experiment was developed for conducting research on elaboration of new types of powdered wound coatings. The use of fixing rings in purulent wound's formation in comparison with the experiment without their application, showed that dermis layers' cross-section for sewing rings complicatesplanimetry during the experiment, but also creates conditions for subcutaneous pocket'sformation. These experimental features do not stop the epithelialization process at the cellular level, but significantly slow down overall healing process and stimulate more massive scar tissue'sformation.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(5):38-45
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THE INFLUENCE OF COLD HELIUM PLASMA ON THE STATE OF FREE RADICAL PROCESSES UNDER EXPERIMENTAL THERMAL TRAUMA

Martusevich A.K., Galka A.G., Golygina E.S., Krasnova S.Y., Belyaeva K.L.

Abstract

The aim of the study was to estimate the effect of helium cold plasma (5 daily procedures of 1 min) on blood oxidative metabolism of rats with experimental thermal trauma. The experiment was performed on 30 male Wistar rats divided into 3 egual-sized groups. The first group of animals (n=10) was intact. The rats of the second and third groups (n=10 in each) were simulated contact thermal burn (area - 10% of the body surface) according to our own method, and local treatment of the wound with levomekol was performed. The animals of the third group were additionally treated with a course that included 5 daily procedures for treating a burn wound (1 min) localized on the skin of the back with a stream of cold helium plasma. The distance from the edge of the "plasma torch" to the treated surface was 1.0-1.2 cm. The cold plasma was produced using a special installation using the principle of microwave-induced ionization of the gas stream. Balloon helium of the A brand was used as the plasma carrier gas. The intensity of peroxidation in the plasma and membranes of red blood cells was studied by Fe-induced biochemiluminescence by the light sum of the latter. In addition, the analysis of the biochemiluminescence curve allowed us to calculate the total antioxidant activity of blood plasma. It was found that the course of treatment of an experimental burn wound with cold helium plasma has a positive effect on the blood metabolism of rats, allowing to neutralize the manifestations of oxidative stress and exerting an antioxidant effect. It was found that this effect is realized both in blood plasma and in red blood cell membranes.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(5):46-50
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EXPERIMENTAL STUDY OF THE IMMUNOTOXIC AND ALLERGENIC PROPERTIES OF THE HERB DRY EXTRACT LYCOPUS EUROPAEUS L

Bortnikova V.V., Krepkova L.V., Babenko A.N., Lemyaseva S.V., Borovkova M.V., Kuzina O.S.

Abstract

Relevance. In recent years, medicinal plants that serve as a source of antithyroid medicines have been of scientific interest for research. Such plants include Lycopuseuropaeus L., from the herb of which a dry extract with a pronounced thyrostatic effect was obtained in the Research Institute of Medicinal and Aromatic Plants. Because the violation of all types of metabolism in hyperthyroidism is one of the reasons for the development of secondary induced immunodeficiency, it was relevant to study the effect of the dry extract Lycopuseuropaeus L. on the functional state of the immune system of experimental animals. The aim is to study the immunotoxicity and allergenicity of a new antithyroidmedicine created on the basis ofthe herb dry extract Lycopuseuropaeus L. Material and methods. The choice of methods for studying the allergenicity and immunotoxicity of the herb dry extract Lycopuseuropaeus L. was determined by the reguirements set out in the"Guidelines for conducting preclinical studies of Medicines". Experiments were performed on albino guinea pigs (males, body weight 350-400 g), CBA/Lac and BALB/c mice (males, body weight 18-20 g). In this study, albino guinea pigs, CBA/Lac and BALB/c mice were administered the test extract at doses of 10 and 100 mg / kg in the form of 0,1 and 1,0% agueous solutions. Control animals received eguivalent volumes of isotonic NaCl solution. The potential allergenic properties of test extractwere evaluated using the following tests: general systemic reactions, active cutaneous anaphylaxis, and delayed-type hypersensitivity reactions. The effect of the herb dry extract Lycopuseuropaeus L. on humoral immunity was evaluated by the test of antibody-forming cell generation in the spleen and the titer of hemagglutinins in the blood serum of mice. The effect of test extract on the state of T-cell immunity was studied by the delayed-type hypersensitivity reaction induction test in CBA/Lac mice. Results. When studying the potential allergenic properties of the herb dry extract Lycopuseuropaeus L. in experiments on different types of laboratory animals, no statistically significant differences in the results between the control and experimental groups were revealed. It was shown that, under different schemes of introduction, the studied extract stimulated effectors of cellular immunity in CBA/Lacmice at a dose of 100 mg/kg. Conclusion. The herb dry extract Lycopuseuropaeus L. does not induce allergic reactions. The extract stimulates the cellular immune response and may reduce the risk of secondary immunodeficiency in patients with thyroid pathology.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(5):51-56
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ANALYSIS OF REFERENT AND GENERIC DRUGS OF AZELAIC ACID IN TERMS OF THE HYDRODYNAMIC RADIUS OF PARTICLES AND ZE7A-P0TENTIAL

Nesterov M.S., Khvostov D.V., Ageldinov R.A.

Abstract

Relevance. In recent years, medicinal plants that serve as a source of antithyroid medicines have been of scientific interest for research. Such plants include Lycopuseuropaeus L., from the herb of which a dry extract with a pronounced thyrostatic effect was obtained in the Research Institute of Medicinal and Aromatic Plants. Because the violation of all types of metabolism in hyperthyroidism is one of the reasons for the development of secondary induced immunodeficiency, it was relevant to study the effect of the dry extract Lycopuseuropaeus L. on the functional state of the immune system of experimental animals. The aim is to study the immunotoxicity and allergenicity of a new antithyroidmedicine created on the basis ofthe herb dry extract Lycopuseuropaeus L. Material and methods. The choice of methods for studying the allergenicity and immunotoxicity of the herb dry extract Lycopuseuropaeus L. was determined by the requirements set out in the"Guidelines for conducting preclinical studies of Medicines". Experiments were performed on albino guinea pigs (males, body weight 350-400 g), CBA/Lac and BALB/c mice (males, body weight 18-20 g). In this study, albino guinea pigs, CBA/Lac and BALB/c mice were administered the test extract at doses of 10 and 100 mg / kg in the form of 0,1 and 1,0% aqueous solutions. Control animals received equivalent volumes of isotonic NaCl solution. The potential allergenic properties of test extractwere evaluated using the following tests: general systemic reactions, active cutaneous anaphylaxis, and delayed-type hypersensitivity reactions. The effect of the herb dry extract Lycopuseuropaeus L. on humoral immunity was evaluated by the test of antibody-forming cell generation in the spleen and the titer of hemagglutinins in the blood serum of mice. The effect of test extract on the state of T-cell immunity was studied by the delayed-type hypersensitivity reaction induction test in CBA/Lac mice. Results. When studying the potential allergenic properties of the herb dry extract Lycopuseuropaeus L. in experiments on different types of laboratory animals, no statistically significant differences in the results between the control and experimental groups were revealed. It was shown that, under different schemes of introduction, the studied extract stimulated effectors of cellular immunity in CBA/Lacmice at a dose of 100 mg/kg. Conclusion. The herb dry extract Lycopuseuropaeus L. does not induce allergic reactions. The extract stimulates the cellular immune response and may reduce the risk of secondary immunodeficiency in patients with thyroid pathology.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(5):57-68
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