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Vol 25, No 9 (2022)

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Articles

Identification of tinctures by the polarimetric method

Syroeshkin A.V., Ogotoeva D.D., Galkina D.A., Dzhavakhyan M.A., Elizarova T.E., Uspenskaya E.V., Pleteneva T.V.

Abstract

Relevance. The ambiguity of the observed therapeutic effects of tinctures and the absence of pharmacopoeial articles require the development of new approaches to their quality control. In this work, for the first time, the polarimetry method and the dynamic light scattering method were used to identify tinctures with sedative and cardiotonic effects. The purpose. To develop the methods of polarimetry and dynamic light scattering for quality control of valerian, motherwort and hawthorn tinctures Material and methods. Objects of research: tinctures of rare series from different manufacturers. Methods: polarimetry (POL-1/2, Atago, Japan); dynamic light scattering method - DLS (Zetasizer Nano ZS, Malvern, UK). Results. Polarimetric method established that tinctures are optically active environment. This made it possible to develop a method for identifying tinctures with sedative and cardiotonic effects, which is based on measuring the optical rotation angle of 95% ethanol dilutions of different multiplicities. When diluting valerian tincture in a ratio of 1:40, the angle of optical rotation is in the range of -0.10° 2.5° were excluded from consideration as unstable dispersed systems. Conclusions. A polarimetric method for identifying tinctures based on measuring the optical activity of dilutions with 95% ethanol has been developed. The angle of optical rotation of valerian tinctures is in the range -0.10°2.5° as unstable disperse systems.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(9):3-9
pages 3-9 views

Modeling of the structure of mineral carriers of medicinal substances

Bondarev A.V., Zhilyakova E.T., Avtina N.V., Novikov O.O.

Abstract

Relevance. The study of the structure and properties of medical clays obtained from medicinal mineral raw materials is an important scientific task. An indisputable assistant in solving this problem is computer 3D modeling of an elementary cell. The purpose of the work is to model the structure of mineral carriers of medicinal substances. Material and methods. Kaolin from the Eleninsky deposit, montmorillonite clay from the Belgorod deposit, and zeolites from the Kholinsky deposit were used as research objects. The construction of virtual three-dimensional molecular models of mineral substances was carried out using the Java Applet Jmol program. Results. Virtual three-dimensional models of Kaolinite, Montmorillonite and Clinoptilolite were obtained. Their analysis was carried out. It has been established that a system of intracrystalline pores and cavities is formed in Montmorillonite and Clinoptilolite, in which occlusion and adsorption of drug molecules of the appropriate size can occur. Conclusion. Medical clays can be used to create mineral carriers of medicinal substances in which the immobilization, delivery and isolation of the drug molecule occurs through sorption processes in the pores. Based on the results of the study, the use of Montmorillonite and Clinoptilolite medical clays for obtaining mineral carriers is justified. Conflict of interest: There is no conflict of interest.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(9):10-15
pages 10-15 views

Physical, chemical and technological aspects of a gel for oral administration Lycopus europaeus L. herb dry extract

Semkina O.A., Zvereva V.I., Dzhavakhyan M.A., Pavets N.P.

Abstract

Relevance. Modern trends in the development of medicines in the form of soft dosage forms are gels for oral administration. Their undoubted advantages: convenience and ease of reception, high bioavailability of active substances, the possibility of use in pediatric and geriatric practice, as well as in patients suffering from dysphagia. Aim. Experimental substantiation of the choice of structure-forming substances of the gel for oral administration of the Lycopus europaeus L. herb dry extract. Material and methods: Lycopus europaeus L. herb dry extract standardized (the content of the sum of phenolic compounds in terms of rosemary acid is not less than 15%). Lycopus europaeus L. herb dry extract has an effect on the functional condition of the thyroid gland and can be used to obtain thyroid-stimulating drugs. The measurement of the viscosity of the gel samples was carried out in accordance with the method of General Pharmacopoeia XIV, Monograph 1.2.1.0015.15 "Viscosity". The determination of the pH value was carried out according to General Pharmacopoeia XIV, Monograph 1.2.1.0004.15 "Ionometry". Instruments and apparatus: Rotary viscometer "Reotest-2" type RV (Germany), mixing device PE-8100 (Ekros, Russia) at a speed of 100 rpm, pH-meter 121, analytical scales VLA-200-M. Results. The article presents the results of the development of a dosage form (DF) of Lycopus europaeus L. herb dry extract - a gel for oral administration. Lycopus europaeus L. herb dry extract have an effect on the functional state of the thyroid gland and can be used to obtain thyroid-stimulating drugs. The choice of excipients was carried out taking into account the nosology, the method of administration of the drug, the physicochemical and technological properties of the substance, its compatibility with excipients. Conclusion. The structure of gel samples was studied by microscopy, the features of the technology of obtaining a gel for ingestion of Lycopus europaeus L. herb dry extract were substantiated. Conflict of interest: no conflict of interest.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(9):16-25
pages 16-25 views

Prospects for the use of spectrophotometry and chemical methods in the analysis and study of the properties of new soft dosage forms made on glycerohydrogel Tizol

Zamaraeva A.I.

Abstract

In the last few decades, research has been actively conducted in the field of new ointment bases that affect the resorption and therapeutic efficacy of the dosage form. A promising solution is the choice of "Tizol" gel as the carrier of the active substance. The titanium glycerosolvate aquacomplex is an activator of the absorption of biologically active substances, enhances their own pharmacological effect, and exhibits concomitant therapeutic effects. Currently, the development of new dosage forms on a tizol basis is becoming relevant. The study of the literature data made it possible to determine the demand, make a choice and offer new ointment compositions based on glycerohydrogel "Tizol" for use in medical practice. The creation of new soft dosage forms involves the development of methods for their pharmaceutical analysis. Some identification methods, methods of quantitative analysis and biopharmaceutical properties of the studied medicinal compositions are considered.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(9):26-33
pages 26-33 views

Pharmacognostic study of Pinus sylvestris L. microstrobils

Erdyneeva S.A., Shiretorova V.G., Radnaeva L.D.

Abstract

Aim of the research. Pharmacognostic study of the pine microstrobils (Pinussylvestris, L), growing in Buryatia. Material and methods. The object of the study was microstrobils Pinus sylvestris, L, growing in the Republic of Buryatia, formed as waste during pollen harvesting. Standardization of plant raw materials was carried out according to the methods specified in State Pharmacopoeia XIV. Determination of essential oil content was carried out by hydrodistillation using a modified Clevenger attachment. The amount of hydroxycinnamic acids was determined by the spectrophotometric method in terms of chlorogenic acid. Results. The diagnostic external and microscopic signs of raw material P. sylvestri microstrobili were determined. Whole or partially crumbled microstrobili are generative buds collected in spike-shaped dense inflorescences located at the base of young shoots, ovate-conical or elongated-ovoid in shape, which consist of an axis with microsporophylls located on it. Microscopic analysis of microsporo-phylls showed that the inner layers of the epidermis consist of wide polygonal cells penetrated by pore tubules, the surface layers - of rectangular low cells with a thickened cell wall, on which fibrous thickenings (exotecia) are observed. On the transverse section, vertically elongated cells of the epidermis are visible, with abundant slit-like pores, yellowish in color. To establish the authenticity of raw materials, it is proposed to use qualitative reactions for the detection of essential oils, tannins and the determination of chlorogenic acid by TLC. To quantify the content of active substances, methods for determining the content of essential oil (the degree of grinding of raw materials is 7 mm, the duration of hydrodistillation is 2 hours) and the amount of hydroxycinnamic acids in terms of chlorogenic acid (the extractant is ethyl alcohol 60% in a ratio of 1:100, the degree of grinding of raw materials 1 mm, extraction duration - 60 min twice) were developed. The indicators of good quality were determined: extractive substances extracted by purified water - at least 20%; extractives extracted with ethyl alcohol 60% - not less than 20%; the content of essential oil on dry matter - not less than 0.3%; the sum of hydroxycinnamic acids in terms of chlorogenic acid - not less than 1.0%; humidity - no more than 10%; total ash - no more than 10%; ash insoluble in 10% hydrochloric acid - no more than 3%; parts that have changed color (darkened and blackened) - no more than 1%; needles - no more than 1%; organic impurities - no more than 2%; mineral impurity - no more than 1%; particles passing through a 3 mm sieve (for whole raw materials) - no more than 5%; particles that do not pass through a 7 mm sieve (for crushed raw materials) - no more than 5%; particles passing through a 0.5 mm sieve (for crushed raw materials) - no more than 5%. Conclusion. For the first time a pharmacognostic study of P. sylvestris microstrobiles, which are formed as waste products during pollen harvesting, was carried out. The results of the study can be used to create new herbal remedies from pine microstrobils, as well as for introduction into official medicine as a medicinal plant material, and will also solve the problem of complex processing of raw materials and reduce the amount of waste.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(9):34-39
pages 34-39 views

Evaluation of the efficiency of use of a biologically active supplement based on the extract of galega officinalis in the complex therapy of type 2 diabetes mellitus

Burkova V.N., Sergun V.P., Ivanov A.A., Samoylova Y.G., Oleinik O.A.

Abstract

Relevance. Diabetes mellitus is one of the most common chronic diseases in the world. The vast majority of patients suffering from this pathology have type 2 diabetes mellitus, for the treatment of which drugs with various effects on metabolic processes are used. In recent years, the interest in a study of medicinal plants with antidiabetic activity has grown in the scientific and medical community. The purpose of this work was to study the efficiency and safety of the complex application of a biologically active supplement (dietary supplement) to food based on the extract of the herb Galega officinalis L. in disorders of carbohydrate metabolism in patients with type 2 diabetes mellitus. Results. When using dietary supplements in combination with basic therapy in patients with type 2 diabetes mellitus, there was a significant improvement in glycemic variability indices by the end of the study. Intraday fluctuations in glucose levels significantly decreased, the frequency of hyperglycemic phenomena decreased, glycemic indices were within the target range. The main indicator of diabetes mellitus compensation is the determination of the level of glycated hemoglobin HbA1c. In the group of patients with dietary supplements compared with basic therapy, there was a significant decrease in the level of glycated hemoglobin: HbA1c in the group of patients with dietary supplements decreased by 0.8%, and in the group of standard therapy increased by 0.05%. This indicates a positive dynamics of the glycemic profile and a decrease in the rate of development of late complications of diabetes mellitus. Conclusion. Thus, the continuous monitoring of glycemia testified to the efficiency and safety of the use of dietary supplements based on the extract of the herb Galega officinalis in the complex therapy of type 2 diabetes mellitus.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(9):40-46
pages 40-46 views

The effects of liposomes containing astaxanthin ethers on cytokine secretion by human peripheral blood mononuclear cells

Malashenkova I.K., Krynskiy S.A., Ogurtsov D.P., Ratushnyy A.Y., Lotosh N.Y., Kulikov E.A., Akulova A.R., Moskvina S.N., Selishcheva A.A., Didkovsky N.A.

Abstract

Relevance. According to the literature, astaxanthin (AST) esters have a pronounced neuroprotective and anti-inflammatory effect in experimental animals with neurodegeneration. Due to the low water solubility, the use of AST esters in the form of phospholipid nanoemulsions is promising. The principal mechanisms of the neuroprotective effect of AST esters include anti-inflammatory action, so it is relevant to study the anti-inflammatory and immunomodulatory effect of nanoemulsions containing AST esters. The aim of this work was to study the effect of phospholipid-based nanoemulsions of AST esters on the secretion of major cytokines and inflammatory mediators (GM-CSF (granulocyte-macrophage colony-stimulating factor), IL-ip, IL-6, IFNy) by human peripheral blood mononuclear cells (PBMC). Material and Methods. Lipid nanoemulsions were prepared from Lipoid S75 by hot emulsification method. AST esters from Haematococcus pluvalis were used for incorporation into nanoemulsions. PBMCs from 6 healthy volunteers (men, age 21-31 years) were isolated from blood in a one-step ficoll urographin density gradient. Cultivation was performed under the following conditions: 1) without addition of nanoemulsions and phytohemagglutinin A (PGA); 2) with PGA, without nanoemulsions; 3) with PGA and nanoemulsions of AST esters; 4) with PGA and nanoemulsions containing no AST esters; 5) with nanoemulsions of AST esters; 6) with nanoemulsions containing no AST esters. Multiplex analysis was used to determine cytokines in the cell supernatants. Results. Nanoemulsions with AST esters suppressed the FGA-stimulated secretion of innate and adaptive immunity cytokines (GM-CSF, IL-1P, IL-6, IFNy) by PBMCs. Addition of nanoemulsions without AST to the PBMCs partially suppressed cell activation by inhibiting the secretion of adaptive immunity cytokine IFNy, but did not affect the levels of proinflammatory cytokines. Conclusion. The results indicate an anti-inflammatory and immunomodulatory effect of AST esters in the form of nanoemulsions, which shows the prospects for further studies of their effects mediating neuroprotection in models of neurodegenerative diseases.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(9):47-52
pages 47-52 views

Proteolytic and collagenolytic activity of mycelial fungi in the process of deep cultivation study

Nikitina Z.K., Gordonova I.K., Nasibov E.M.

Abstract

Relevance. Enzymes with proteolytic and collagenolytic activity have been considered in recent years as therapeutic agents that can be used in medicine for the treatment of various pathologies. The use of microorganisms as producers of these biologically active substances has a number of advantages. Despite the existence of numerous studies devoted to the study of the hydrolytic activity of various microorganisms, the search for new producers of proteinases and collagenases remains an urgent biotechnological task. Objective. To study the proteolytic and collagenolytic activity of previously selected mycelial fungi during deep cultivation using a modified Chapek medium. Material and methods. The objects of the study were 5 strains of 4 species of micromycetes from the VILAR microorganisms collection: Aspergillus fumigatus F 22, A. sydowii F 25, Botrytis terrestris F 38, Cladosporium herbarum F 33, 57. Deep cultivation was carried out using a liquid modified medium Chapek with partial replacement of sucrose for collagen (0.5% sucrose and 1.5% collagen). The concentration of protein, sucrose, total proteolytic and collagenolytic activity were determined in the filtrates of the culture fluid. Results. The conducted studies have shown that in the process of deep cultivation, the studied micromycetes grew on modified media with partial replacement of sucrose with collagen. It was noted that on 3-4 days there was complete utilization of sucrose from the nutrient fluid and the beginning of active accumulation of extracellular proteins. It was found that the micromycete A. fumigatus F 22 had the highest proteolytic, specific proteolytic activity during cultivation, as well as the maximum collagenolytic activity of secreted enzymes. Conclusions. Based on the results obtained, the culture of A. fumigatus F 22 was selected for further research as a potential colla-genase producer.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(9):53-59
pages 53-59 views

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