In the group of fat-soluble vitamins, vitamin D is one of the most relevant objects, that is why the problem of its technology optimization is under consideration. In general, there is a number of ways to obtain this substance, although it is not produced in Russia yet.The aim of the study was to select optimal process conditions to increase the efficiency of protein transformation with the isolation of a fat fraction containing fat-soluble vitamin D.Materials and methods. Various types of fish and the vitamins contained in them are described as the main research models. Variants of technological solutions have been considered: the possibility of using extraction to obtain the vitamin D substance has been tested. Classical maceration and intensifying maceration have been used; the circulating extraction method and the alkaline hydrolysis method have been applied. The yield of the target product has been determined by HPLC.Results. Methods for obtaining the substance of fat-soluble vitamin D from fish raw materials have been considered in detail. The optimal technological characteristics of the vitamin release by alkaline hydrolysis with a 12.5% decrease in the concentration of the hydrolyzing alkaline component – potassium hydroxide – has been established; that concentration ensured the maximum yield of the fat fraction containing vitamin D.Conclusion. The use of the resulting substance makes it possible to develop domestic standard samples applicable both in the pharmaceutical field and in the field of technical regulation.
The genus Persicaria Mill. species belonging to the buckwheat family (Polygonaceae Juss.) and widespread in Russia, are weeds. The chemical composition’s main components of the genus Persicaria Mill. species, are flavonoid glycosides (rutin, avicularin, hyperoside, etc.). The data concerning a comparative study of the organic acids in the herb representatives of genus Persicaria Mill., have not been detected in the available literature.The aim of the research is a comparative study of the organic acids qualitative and quantitative composition in the genus Persicaria Mill. species growing in the Voronezh region.Materials and methods. The objects of the study were dried herb samples of the genus Persicaria Mill. species. All the species were harvested in the Voronezh region during the blooming period. The quantitative content of ascorbic acid and the amount of organic acids in terms of malic (hydroxy-succinic) acid was carried out according to the titrimetric methods of the Russian Federation State Pharmacopeia, the XIVth ed. The study of the qualitative composition of the organic acids profile and their quantitative content assessment in the studied objects, the herbs, was carried out by the method of capillary electrophoresis (“Kapel”, St. Petersburg, Russia).Results. With the help of pharmacopoeial titrimetric methods, it was established that the highest content of the organic acids total amount is characteristic of the Persicaria maculosa Mill. herb (5,60%), the lowest one – of the Persicaria tomentósa (Schrank) E. P. Bicknell herb (4.03%). Persicaria maculosa S. F. Gray and Persicaria hydropiper (L.) Delarbre are the richest in ascorbic acid (0.17% and 0.15%, respectively). Using the method of capillary electrophoresis, the composition of the total amount of the studied organic acids has been established. It is represented by oxalic, formic, citric, malic, wine, propionic, lactic, benzoic and other acids.Conclusion. The study of the organic acids of the genus Persicaria Mill. species has been carried out. It has been established that in the studied species, the organic acids total amount in terms of malic acid and the amount of ascorbic acid are similar. By the method of capillary electrophoresis, a complete composition of organic acids has been studied, and the quantitative content of each component has been established. In all the studied Persicaria Mill. species, the predominance of oxalic, formic and malic acids has been revealed.
Obesity is a vivid example of a multifactorial disease. In its development, not only the discrepancy between the energy intake and its expenditure but also various neurohumoral mechanisms, as well as external socio-economic and psychosocial factors, play important roles. One of the frequent options for combining psychoemotional disorders with obesity is the development of certain types of eating disorders in a patient. In this regard, the actual problem is to find the optimal therapeutic and prophylactic strategy in the management of such patients.The aim of the work is to analyze the literature data on the features of the pathogenetic mechanisms of the obesity development against the background of psychoemotional disorders that are realized through eating disorders, and to identify the possibilities of using sibutramine to carry out a pharmacological correction of these pathological conditions.Materials and methods. In the process of selecting materials for writing a review article, the following databases were uses: PubMed, Scopus, Web of Science, Google Scholar, ScienceDirect, etc. The search carried out, was based on the publications for the period from 2009 to 2020. The following words and phrases were chosen as parameters for the literature selection: obesity, psycho-emotional disorders, eating disorders, sibutramine.Results. This review summarizes the main pathogenetic aspects that unite both the development of psychoemotional and metabolic disorders. A modern classification of obesity, taking into account the latest domestic and international recommendations of professional communities, is given. Eating disorders are considered in detail, their socio-psychological and psychiatric classifications are given. The prospect of choosing a therapeutic and prophylactic strategy for managing such patients is assessed, depending on the presence of psycho-emotional and eating disorders.Conclusion. Thus, the combined drug containing sibutramine and metformin registered in the Russian Federation is effective, safe and can be used in patients with alimentary obesity and eating disorders, taking into account contraindications.
The aim of the research is the development of quantification procedures of flavonoids in Juglans nigra L. barks preparations using modern instrumental analytical techniques (spectrophotometry, high performance liquid chromatography).Materials and methods. The subjects of research were tincture and dry extract of Juglans nigra L. bark, the samples of which were prepared in March and April 2020 in the Botanical Garden of Samara State Medical University (Samara); the standard samples (SS) of myricitrin, myricetin. The registration of the electronic spectra was carried out with a spectrophotometer «Specord 40» (Analytik Jena, Germany). The chromatographic analysis was carried out by the method of reversed-phase HPLC on a microcolumn liquid chromatograph “Milichrom-6” (NPAO “Nauchpribor”, Russia).Results. Using differential spectrophotometry, methods for the quantitative determination of the total amount of flavonoids in terms of myricitrin in the tincture and dry extract of Juglans nigra L. bark, has been developed. It has been determined that the content of the total amount of flavonoids in terms of myricitrin in the tincture and dry extract of Juglans nigra L., is 0.84±0.07% and 12.38±0.24%, respectively. The error of a single determination of the total amount of flavonoids in terms of myricitrin in the tincture and dry extract of Juglans nigra L. bark with a confidence probability of 95%, is ± 8.91% and ± 2.10%, respectively. Methods for the quantitative determination of myricitrin in the tincture and dry extract of Juglans nigra L. bark by HPLC has been developed. The content of the dominant flavonoid – myricitrin (myricetin-3-O-α-L-rhamnopyranoside) – in the tincture and dry extract of Juglans nigra L., was 0.42±0.06% and 8.45±0.24%, respectively. The error of the single determination of myricitrin in the tincture and dry extract of Juglans nigra L. with a confidence probability of 95% is ± 15.04% and ±2.96%, respectively.Conclusion. The developed methods for the quantitative determination of flavonoids in the preparations of Juglans nigra L. barks L. can be used in solving the problems of standardization of Juglans nigra L. preparations.
Taking into account the current Product specification file, the aim of the work was to develop the composition and technology for obtaining effervescent tablets based on solid dispersions of furazolidone in the form of an aqueous solution for external use.Materials and methods. The used substances were: furazolidone, anhydrous sodium carbonate (chemically pure), polyvinylpyrrolidone-24000±2000 (chemically pure), malic acid (analytically pure), tartaric acid (chemically pure), citric acid (chemically pure), sodium benzoate (chemically pure), ethyl alcohol 96% (chemically pure), purified water. Preparation of granulates is separate wet granulation in a fluidized bed (Mycrolab, BOSCH, Germany). Obtaining tablets is the process of pressing on a manual hydraulic test press (“PRG”, VNIR, Russia). The dependence of disintegration, abrasion capacity and crushing resistance on compacting pressure was investigated. Technological parameters of granulates, еру obtained effervescent tablets, shelf life and storage conditions were investigated according to the State Pharmacopoeia of the Russian Federation XIVth ed.Results. Two compositions of effervescent tablets containing solid dispersions of furazolidone as an active substance were obtained, which, when dissolved in 100 ml of water at room temperature (20°C), form a solution of furazolidone with a concentration of 0.004% in less than 5 minutes. The method of quantitative determination of the furazolidone content in the effervescent tablets was validated. A complex of physicochemical methods for the analysis of tablets was carried out. Quality standards have been developed. The developed compositions stability of instant tablets during storage during accelerated and long-term tests has been experimentally confirmed. The preliminary shelf life and storage conditions have been determined.Conclusion. The result of technological and chemical-pharmaceutical research is the creation and evaluation of the quality of a new instant furazolidone dosage form as effervescent tablet formulations.
The aim of the article is to evaluate the effectiveness of the thioctic acid preparation in the complex therapy of type 1 diabe-tes mellitus (T1DM) in children with cardiovascular autonomic neuropathy at the preclinical stage.Materials and methods. A design is a prospective randomized study. A clinical and instrumental examination of 64 children with preclinical stage signs of diabetic cardiovascular autonomic neuropathy (DCAN) was carried out. The cohort was divided into 2 groups: in the main and control groups, glycemic control was normalized by adjusting a dose of insulin therapy; in the main group, the children additionally received thioctic acid at the dose of 600 mg/day for 3 months. To control the effective-ness of the therapy, the technique of laser Doppler flowmetry was used.Results. After the pharmacological intervention, there was an improvement in the disease course, normalization of carbohy-drate and lipid metabolism, increased vasomotor mechanisms of the regulation of the tissue blood flow due to an increase in endothelial and neurogenic kinds of activity in combination with a decrease in the intravascular tone and an increase in the effective perfusion in tissues. An increase in the heart rate variability was detected, positive dynamics of cardiovascular tests indicators according to D. Ewing, temporal (pNN50%, SDNN) and spectral indicators (VLF) were diagnosed. Achievement and maintenance of the target values of glycemic control indicators, as well as the absence of glycemic variability, turned out to be clinically significant for reducing the manifestations of neuropathy. The non-invasive technique of laser Doppler flowmetry is informative for the early diagnosis of DCAN in T1DM children.Conclusion. The carried out studies have demonstrated the effectiveness of the lipoic acid use at the dose of 600 mg/day for 3 months in the children with DCAN signs at the preclinical stage. The method of laser Doppler flowmetry for determining in-dications and monitoring the effectiveness of therapy makes it possible to implement a personalized approach to prescribing preventive treatment in T1DM children.
The aim of the study is the identification and evaluation of a new antioxidant activity in a potentially new medicinal raw material of Actinidia arguta folia . Materials and methods. The total content of antioxidants was measured on a Tsvet Yauza-01-AA liquid chromatograph using the amperometric method. In parallel, the antioxidant activity of Actinidia arguta extracts was studied in vitro in the following dilution range: 62.5 µg/ml, 125 µg/ml, 250 µg/ml, 500 µg/ml and 1000 µg/ml. Herewith, DPPH, superoxide, and hydroxyl radical inhibitory properties of the analyzed samples were evaluated. The studies of the antioxidant activity with the determination of the activity of superoxide dismutase, glutathione peroxidase, catalase, the concentration of malondialdehyde and diene conjugates, have been conducted in vivo . Results. When studying the antiradical activity ( in vitro tests), it was found out that the highest radical-inhibiting activity comparable to the individual compound - quercetin, has the extraction from Actinidia arguta folia , obtained by the extraction with 40% ethyl alcohol. The IC 50 value for the given extract in relation to DPPH; superoxide and hydroxyl radical, amounted to 537.6±23.924 µg/ml; 26.6±2.627 µg/ml and 72.6±3.264 µg/ml, respectively, which may indicate that this extract has reducing and radical scavenging properties. In parallel, the study of the total content of antioxidants in terms of quercetin and gallic acid has been carried out. It has also been found out that in the Actinidia arguta folia extract, obtained by the extraction with 40% ethyl alcohol, the content of the antioxidants is maximum. Conclusion. The data obtained using the in vitro test were confirmed in the in vivo study, in which the course application of the Actinidia arguta folia extract, obtained by the extraction with 40% ethyl alcohol to the degree comparable to quercetin, contributed to an increase in the superoxide dismutase activity, a decrease in the lipid peroxidation products. The maximum content of antioxidants for Actinidia arguta folia was 0.73±0.007 and 0.47±0.005 mg/g in terms of quercetin and gallic acid, respectively. The extractant was 40% ethyl alcohol.
The aim of the article is the evaluation of the economic damage (ED) because of the absence of pneumococcal vaccination as a leading risk factor for the development of community-acquired pneumonia (CAP) and acute exacerbations of а chronic obstructive pulmonary disease (COPD).Materials and methods. The method of attributive statistics was used for the first time to assess the ED of the vaccination absence as an independent risk factor contributing to the development of CAP and COPD exacerbations in the Astrakhan region for the period of 2015–2019. To do this, at the beginning of the study based on the literature data, a relative risk of COPD complications associated with the absence of pneumococcal vaccination was determined. Using it as a risk factor, prevalence rates (a proportion of non-vaccinated patients with COPD), the population attributable risk (PAR) was calculated. Further, the annual economic damage (ED) from the development of CAP and COPD exacerbations was determined. To assess the cost-effectiveness of the COPD complications prevention, vaccination costs of newly registered patients were calculated and the ratio of these costs to the average annual ED was determined.Results. A decrease in the non-vaccinated patients’ proportion corresponds to the decrease in the total ED from COPD complications: from 13.16 million rubles to 6.06 million rubles during the observation period. The calculations showed that due to the increase in the vaccinated patients’ proportion over a five-year observation period, the ED from the CAP development decreased by 2.1 times, from exacerbations of COPD – by 2.3 times. The vaccination costs of newly diagnosed COPD cases amounted to 0.63 million rubles. Thus, to prevent the annual ED of 3.24 million rubles, the sum for the state to spend, should be 5.2 times as small.Conclusion. A study on the evaluation of the ED due to the risk factor (RF), the pneumococcal vaccination absence, showed that its elimination reduces the risk of acute COPD exacerbations and the development of CAP, as well the ED, as associated with them. Reducing the economic costs of the health care system with significantly lower vaccination costs, makes this preventive measure economically viable.
Nitric oxide as a therapeutic approach to the treatment of cardiovascular diseases attracted the attention of researchers at the end of the 19th century. As a vasodilator, nitric oxide may be a unique therapeutic agent for the treatment of hypertension and, as a result, renal failure and left ventricular hypertrophy.The aim of the article is to analyze the literature data on possible ways of modulating the activity of various nitric oxide synthases as an approach to the treatment of endothelial dysfunction.Materials and methods. When searching for materials for writing a review article, such abstract databases as PubMed, Google Scholar, e-Library, etc., were used. The search was carried out on the publications for the period from 1990 to 2021. The following words and phrases were chosen as parameters for the literature selection: nitric oxide; NO synthase; endothelial dysfunction; NO synthase activator; NO synthase inhibitor.The following words and phrases were chosen as parameters for the literature selection:Results. The article presents the history of the nitric oxide discovery and its biological role, the process of its biosynthesis, as well as the isoforms of its synthesizing enzymes (NOS): neuronal – nNOS, endothelial – eNOS and inducible iNOS, and their role in normal and pathological physiology. The process of NOS uncoupling (its molecular mechanisms) has been considered as the basis of endothelial dysfunction.The examples of the pharmacological correction (BH4, arginase inhibitors, statins, resveratrol) are presented. In addition, NO synthase activators (calcium dobesilate, cavNOxin, and some NOS transcription activators), as well as non-selective (L-NMMA, 1-NNA, L-NAME, ADMA, 546C88, VAS203) and selective (L-NIO, 7-nitroindazole, aminoguanidine, L-NIL, GW273629, GW274150, cavtratin) inhibitors of nitric oxide synthasehave been described.Conclusion. Nitric oxide synthases continue to be promising targets for the development of agents that modulate their activity to correct various pathologies. As a therapeutic approach, modulation of the nitric oxide synthase activity can be implemented to treat endothelial dysfunction, which is the cause for complications of many diseases.
The aim of this study is to conduct a comprehensive pharmacoeconomic evaluation of the use of long-acting subcutaneous lanreotide gel compared to alternative drugs, for the treatment of acromegaly.Materials and methods. Based on the literature data, a treatment model with a 1-year outlook was developed, a cost-effectiveness analysis (CEA) in pharmacoeconomics and a sensitivity analysis of changes in the model parameters were carried out. Direct medical costs for the annual therapy course were calculated. The data on the medicines costs were taken from the register of marginal prices of the State Register of Medicines.Results. According to the unified Russian registry of the pituitary-hypothalamic tumors area, the achievement of remission in the acromegaly patients using lanreotide, a long-acting gel for a subcutaneous administration, compared to the long-acting octreotide, is 51% vs 24%. During the first year of treatment with octreotide, the total pharmacotherapy costs were lower than with lanreotide (RUB 225,496.07 vs RUB 574,451.84). According to the results of the cost-effectiveness analysis for one achieved case of remission, the advantage of using lanreotide over long-acting octreotide was revealed (RUB 1,251,870.56 versus RUB 1,431,005.31). The sensitivity analysis demonstrated the model’s stability to increases in the lanreotide price (up to +18%), decreases in the octreotide prices (up to –22%), increases in the transsphenoidal adenomectomy prices (up to +59%), and decreased lanreotide remission rates (up to –12%).Conclusion. Although the treatment costs analysis showed lower total per year costs of the treatment with long-acting octreotide compared to lanreotide, the calculation of the cost-effectiveness ratio per remission showed that lanreotide had been superior to long-acting octreotide.
The article presents modern scientific data on long-term clinical and pathogenetic effects of the antiviral drug Areplivir (Favipiravir) in patients with metabolic syndrome in the post-COVID period.The aim of the article is to study long-term cytokine-mediated (IL-6/sIL6r and LIF/sLIFr) pathogenetic effects of the favipiravir (Areplivir®) based drug on the incidence of complications in patients with metabolic syndrome in the post-COVID period.Material and methods. With the approval of the local ethics committee at the N.P. Ogarevs Mordovia State University (Protocol No. 5 dated May 17, 2020) “An open prospective comparative study of the Areplivir® (Favipiravir) drug effectiveness in reducing the risk of complications in the post-COVID period in patients with metabolic syndrome” in the Republic of Mordovia was carried out.The study included 190 metabolic syndrome patients who received the outpatient treatment for COVID-19 at Saransk polyclinics from February 2021 to March 2021. The case of COVID-19 was diagnosed in accordance with the current Temporary Guidelines for the prevention, diagnosis and treatment of the new coronavirus infection.Results. The analysis of the metabolic syndrome patients’ follow-up within 1 year after undergoing COVID-19, revealed significant differences in the incidence of complications depending on the intake of the favipiravir based drug. The patients who were administrated with favipiravir at the early stage of infection, were characterized by lower serum levels of four members of the interleukin 6 family – IL-6 (IL-6, sIL6r and LIF, sLIFr) 10, 30 and 180 days after a clinical and laboratory recovery (p<0.001). The average statistical changes in the IL-6 /sIL6r system of the group administrated with favipiravir, were 90%, and they were higher than in the group not administrated with antiviral drugs. In the group of the patients administrated with favipiravir, there was a significant (p<0.001) positive dynamic of the sLIFr indicator, while in the comparison group, there was an increase in this indicator.A protective effect of the early favipiravir use was characterized by a decrease in the frequency of cardiovascular complications, a 2.66-fold decrease in the risk of a stroke and the ACS in the post-COVID period.Conclusion. The areplivir therapy in the acute period of coronavirus infection made it possible to timely reduce the viral load. It helps to correct the pro-inflammatory vector of the immune response at the post-COVID stage and, accordingly, reduces the risk of progression of atherosclerosis, transient cerebrovascular accidents with a cognitive decline, an endothelial dysfunction, and can be considered a secondary prevention of life-threatening cardiovascular complications.
Nigella sativa L. is a promising plant object, herbal medicinal raw materials of which can be comprehensively used for the development of drugs with an antimicrobial activity.The aim of the study was to screen and compare the antimicrobial activity of water-ethanolic extractions from the Nigella sativa L. herbs with a eucalyptus tincture of as a reference preparation.Materials and methods. Chromatograms of the extracts were obtained by thin layer chromatography in the system of chloroform – ethanol – water (26:16:3). The detection of adsorption zones was carried out in daylight, in the UV light at λ=254 nm and λ=365 nm, as well as by treatment with reagents – a 3% alcohol solution of aluminum chloride and a solution of diazobenzosulfonic acid in a 20% sodium carbonate solution. The next step was to determine the minimum inhibitory concentration by the method of double serial dilutions in Mueller-Hinton nutrient broth (Bio-Rad, USA). As test cultures, the strains of the American Type Culture Collection (ATCC) microorganisms were used: Staphylococcus aureus (ATCC 29213), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), as well as Candida albicans (a clinical strain). Simultaneously, an experiment to establish a “negative” control was carried out. For the comparative evaluation of the studied samples activity, its activity was compared with the reference preparation with a proven antimicrobial activity – a eucalyptus tincture.Results. For all water-ethanolic extractions and the Nigella sativa L. herb tincture, the adsorption zones characteristic of flavonoids with Rf1 = 0.28, Rf2 = 0.15, Rf3 = 0.11 were revealed, and under the action of an alcoholic solution of aluminum chloride, the fluorescence of the adsorption zones was also enhanced, which indicates the phenolic nature of these compounds.In the course of the study, it was found out that all water-ethanolic extractions from the Nigella sativa L. herbs have the greatest antimicrobial effect against the Pseudomonas aeruginosa strain. When compared with the reference preparation – a eucalyptus tincture, it was notified that the specified tincture of the Nigella sativa L. herbs has an advantage in the antimicrobial activity over the strain of Pseudomonas aeruginosa – the action at the 16-fold dilution vs the 4-fold dilution. The action on the Escherichia coli and Candida albicans strains is comparable for the both tinctures.Conclusion. The obtained results of phytochemical and microbiological analyses will be used as a rationale for the introduction of antimicrobial preparations based on the Nigella sativa herbs in medical and pharmaceutical practice.
The article presents clinical study results of the efficacy and safety of combination therapy with sibutramine and metformin (fixed combination) in comparison with sibutramine therapy with microcrystalline cellulose in patients with alimentary obesity.The aim is to evaluate the efficacy and safety of using the sibutramine+metformin fixed dose combination (Reduxin® Forte) and compare it with the sibutramine + microcrystalline cellulose combination (Reduxin®) in patients with alimentary obesity in the course of the obesity therapy.Materials and methods. Male and female patients (240 people) aged 18 to 65 years inclusive with alimentary obesity, meeting the inclusion criteria and not meeting the non-inclusion criteria, were randomized into 2 groups in a 1:1 ratio. One group (n=120) received sibutramine+ metformin p. o., 1 tablet (850 mg + 10 mg) once per day, the second group (n=120) received sibutramine+ microcrystalline cellulose (MCC) p. o., 1 capsule (10 mg + 158.5 mg) once per day in the morning. On day 30 ± 1, in the absence of a 2 kg weight loss compared to the first visit, the dose was increased in accordance with the medical instruction. The therapy period was 180 days. The randomization list was generated by the factory method of random numbers. The efficacy and safety were assessed by anthropometric, clinical and laboratory parameters and the SF-36 questionnaire. The proportion of patients who achieved a decrease in body weight by more than 5% in 6 months, the magnitude and dynamics of changes in body weight and body mass index, waist and hip measurements, their ratios, changes in lipid profile, blood pressure, as well as the total number of adverse events, their frequency and nature of occurrence were analyzed.Results. The both drugs have demonstrated efficacy in all parameters of the obesity therapy. At the same time, in a comparative analysis, a statistically significant advantage of therapy with sibutramine + metformin was demonstrated in relation to the proportion of patients who had achieved more than 5% weight loss (body weight dynamics). Significant benefits were shown in terms of the magnitude of the change in body mass index (BMI); there was a statistically significant increase in the proportion of the patients who had switched from one category of BMI to another. By the end of the study, the vast majority of patients had no longer met the criteria for the diagnosis of “Obesity”. There was also a statistically significant benefit of sibutramine + metformin in terms of lowering triglycerides and low-density lipoprotein levels. The analysis of the safety parameters of sibutramine + metformin confirms a high safety profile of the drug, a comparative statistical analysis of adverse events in terms of their presence, severity, causal relationship with therapy and outcome have not revealed intergroup differences. Adverse events were transient and did not require discontinuation of therapy.Conclusion. The results of the study showed that therapy with Reduxin® and Reduxin® Forte provides a pronounced decrease in body weight. However, the use of a fixed combination has a more effective positive effect on the lipid profile and patients’ quality of life, which, combined with a high safety profile, proves the possibility and expediency of using Reduxin® Forte for the treatment of obesity and restoring metabolic health, even in patients without additional carbohydrate metabolism disorders.
The aim of the study is to determine antioxidant, anti-inflammatory and hypolipidemic activities of the extracts from Cosmos bipinnatus Cav. three varieties, obtained by the extraction with 70% ethyl alcohol.Materials and methods. The antioxidant effect was studied in vitro using a model of iron-induced lipid peroxidation in the lecithin liposome system. The study of the anti-inflammatory activity was carried out on 30 male rats of the “Wistar” line. Diclofenac was used as a reference drug (p. o., the dose of 13 mg/kg in terms of the weight of an adult). The substances were administered to animals in the form of an aqueous suspension stabilized with Tween-80. To simulate the inflammatory process, a model of “cotton granuloma” was created. A hypolipidemic activity of the extracts was studied on 36 white male rats of the “Wistar” line. To study the hypolipidemic activity of the studied extracts, a tween model was used to create a hyperlipidemic state in rats, the concentrations of total cholesterol and triglycerides was determined in the serum of the experimental animals.Results. The conducted model experiments made it possible to conclude that the alcohol extracts obtained from the dried inflorescences of the “Dazzler”, “Rosea” and “Purity” varieties of Cosmos bipinnatus Cav. have antioxidant, anti-inflammatory and hypolipidemic kinds of activities. It has been established that the extracts from the “Dazzler” and “Rosea” varieties (Cosmos bipinnatus Cav.) contribute to a better reduction in the accumulation of peroxide compounds, compared to the extract obtained from the “Purity” variety. The data analysis on the anti-inflammatory activity shows that all the studied objects significantly (p = 0.05) reduce the stage of exudation compared with the control group animals by 50% (the «Purity» variety), by 52% (the «Rosea» variety) and by 40% (the “Dazzler” variety).An experiment on the study of a hypolipidemic activity in the control group of the animals revealed a significant, in relation to the values of the intact group, increase in the cholesterol level of the blood serum by 78%, and in the level of triglycerides (TGCs) – by 64%.The administration of the extracts obtained from Cosmos bipinnatus Cav. “Purity”, “Rosea”, “Dazzler” varieties to the animals, led to a decrease in cholesterol in blood serum by 44%, 47%, 50%, and triglycerides by 52%, 52% and 57%, respectively. Both indicators reached the normal level and did not differ significantly from the values in healthy (intact) animals.Conclusion. According to the conducted studies, it can be concluded that alcohol extracts obtained from Cоsmos bipinnatus Cav., have pronounced antioxidant, anti-inflammatory and hypolipidemic kinds of effect.
Research in the development of new therapeutic agents with a wide spectrum of the antiviral activity and a low ability to develop resistance remains the main dimension in combating the global threat to public health. The need for a parenteral form of favipiravir was dictated by the necessity to increase the efficacy of therapy in COVID-19 inpatients. This dosage form has expanded the possibilities of drug therapy in the inpatients, for whom a therapeutic effect acceleration and a high safety profile of the drugs used are especially important. The aim of the article is the evaluation of the efficacy and safety of a medicinal product containing favipiravir for the parenteral administration against the background of pathogenetic and symptomatic therapy, in comparison with standard therapy in hospitalized COVID-19 patients. Materials and methods. An open, randomized, multicenter comparative study was conducted in 6 research centers in the Russian Federation to evaluate the efficacy and safety of favipiravir, a lyophilisate for the preparation of a concentrate for the infusion solution administrated to the patients hospitalized with COVID-19. Screening procedures and randomization were completed in 217 patients, 209 of which had completed the study in accordance with the protocol. Results. Between the study groups, statistically significant differences have been found out, making it possible to consider the hypothesis of the drug Areplivir (favipiravir) superiority for the parenteral administration over the standard therapy, which included favipiravir (p. o.) and remdesivir. A comparative analysis has shown that a course of therapy with the parenteral favipiravir drug leads to a significant improvement in the condition of patients with COVID-19, significant benefits in terms of the speed and frequency of improvement in the clinical status of patients, as well as a reduction in the hospital stay length. It has been proven that therapy with a drug containing favipiravir for the parenteral administration does not adversely affect the parameters of clinical and biochemical blood tests, urinalysis, coagulograms, vital signs and ECG, which indicates the therapy safety. The study drug is characterized by a high safety profile and tolerability. Conclusion. The versatility and resistance to mutations of RNA-dependent RNA polymerase make it possible to consider it as the main target for combating the most common RNA viruses that cause ARVI, that determines the need further studies of favipiravir to expand the range of its indications.
The aim of the article is the structure and content specification of the subject area professional term “drug supply” in order to deepen and concretize the conceptual apparatus in the field of the pharmaceutical activity.Materials and methods. The review presents the analysis of 389 titles of scientific pharmaceutical publications for the periods of 1995–1998 and 2010–2019. The selection of publications was carried out by the random sampling based on the phrases: «drug provision», «medical care», «provision of medicines», «pharmaceutical care», «medicinal services», «drug supply» and their English-language counterparts in Russian and foreign electronic information sources. A methodological base of the study was a cluster analysis of the subject area concept of “drug supply” according to the methodology proposed by E.A. Korzhavykh and I.V. Voronovich. In this study, a cluster was interpreted as a set of publications in which a certain pair of terms was simultaneously cited with a preset frequency of co-citation.Results. When analyzing the publications, two clusters of the “drug supply” concept were formed for the time periods indicated above. The comparison of the clusters showed an increase in the activity of the scientific research to expand the structure and content of the subject area of the “drug supply” concept. For the modern cluster, 124 co – cited pairs of lexical units were selected. They were grouped into 9 hierarchy levels according to the strength of relationship between an interval of 10 units and mentioning frequencies of the “drug supply” term. At the final stage, a graphical model of the “drug supply” concept cluster was formed. It was established that the lexical units included from the first to the fifth level, are the cluster nucleus of the “drug supply” concept as the most stable part of the lexical array, which it is advisable to rely on when developing a definition for the concept under study.Conclusion. Thus, the subject field of the “drug supply” concept is characterized by the scientific research, reflecting the socio-economic significance of the objects under study in the field of pharmaceutical activities, and its content is characterized by a high level of pharmaceutical knowledge which describes the most stable elements that make it possible to formulate an adequate definition of the “drug supply” definition.
Zea maydis styli cum stigmatis (Engl. corn silk) are well known in medical practice. In the scientific literature, a lot of informa-tion has been accumulated about the chemical composition and pharmacotherapeutic actions of this medicinal plant mate-rial. A chronological analysis of this information shows that earlier, the scope of scientific publications was mainly devoted to the study of the choleretic, diuretic, hemostatic kinds of Zea maydis styli cum stigmatis activity, and the identification of the active substances responsible for these types of action. Currently, there is a growing scientific interest not only in the individual natural compounds of the Zea maydis styli cum stigmatis composition, but also in the search for new aspects of their medical application. The aim of the article is a review and systematization of modern scientific data in the field of the Zea maydis styli cum stig-matis chemical composition and their pharmacological action. Materials and methods. For the information and analytical search, the scientific data posted on the following electronic re-sources were used: PubMed, Web of Science, ScienceDirect, Scopus, Google Scholar, eLibrary. The search was carried out in the period from 2005 to 2021 using the following keywords: Zea mays L.; Zea maydis styli cum stigmatis; corn silk; chemical composition; pharmacological action. Results. The review is devoted to the generalization and analysis of modern scientific data on the Zea maydis styli cum stig-matis chemical composition and their pharmacological action. It has been shown that, as before, the greatest attention of scientists is attracted by flavonoids in the Zea maydis styli cum stigmatis chemical composition. Alongside with them, phe-nolcarboxylic acids, vitamin K, phytosterols, volatile compounds and polysaccharides are of no small importance for the Zea maydis styli cum stigmatis pharmacological activity. Modern ideas about the Zea maydis styli cum stigmatis pharmacological activity have been expanded by summarizing the study results of their antioxidant, anti-inflammatory, antidiabetic, hypoten-sive, neuro-and photoprotective activities. The data on the effectiveness of their use as parts of the complex tumor diseases therapy have been published. Conclusion. As a result of the data analysis of modern scientific literature, it has been found out that Zea maydis styli cum stigmatis are still in the sphere of scientists' interest. Alongside with the flavonoids of this raw material, other groups of phar-macologically active substances are also being actively studied. It has been revealed that the information about potentially significant and confirmed types of the Zea maydis styli cum stigmatis therapeutic action is significantly updated. The results of this review may be useful for identifying promising directions for the development of the drugs based on Zea maydis styli cum stigmatis.
The creation of drugs with an anxiolytic activity, which do not have the main side effects characteristic of drugs of this group, is an important and socially significant task. For its implementation, within the framework of the development of an original drug with an anxiolytic activity, the composition and manufacturing of GML-1 tablets (N-benzyl-N-methyl-1-phenylpyrrolo [1,2-a] pyrazine-3-carboxamide) are being developed.The aim of this article is to study, using a four-factor analysis of variance, the influence of composition factors on the manufacturing properties of GML-1 tablets and the selection of the type, the amount, stage of the disintegrant addition and the type of lubricating excipients used in the technology of wet granulation of GML-1 tablets.Materials and methods. The materials used are: the substance – GML-1 (N-benzyl-N-methyl-1-phenylpyrrolo [1,2-a] pyrazine-3-carboxamide). Excipients: microcrystalline cellulose 101 (MCC 101); polyvinylpyrrolidone (PVP); crospovidone, croscarmellose sodium (CCS), sodium starch glycolate (SSG); magnesium stearate (MS), sodium stearyl fumarate (SSF). To obtain tablet mixtures, wet granulation and tableting with the study of their main pharmaceutical and technological properties was used.Results. Model compositions were developed and their pharmaceutical and technological properties were studied. These results have been analyzed, the degree of these factors’ influence and their interactions have been determined. In most of the cases considered, the interactions of the factors did not cause a significant change in the optimization criteria. With an increase in the amount of a disintegrant, the disintegration time decreased unevenly, so an increase in the amount of these excipients from 4 to 6 mg had a stronger effect than from 2 to 4 mg. Factor B affected the release degree non-linearly. Factor A influenced all the optimization criteria considered, especially a PS release. The best release and disintegration were observed with crospovidone, which was of a particular importance when processing the test results using a generalized desirability method.Conclusion. In view of the conflicting variance analysis results, for particular factors, the resulting values were additionally analyzed using the generalized desirability function. The use of this method made it possible to reduce the conflicting variance analysis results to the most optimal composition.
The aim. To identify polypharmacy cases and develop the ways to optimize pharmacotherapy of patients with COVID-19 hospitalized in infectious disease facilities.Materials and methods. ATC/DDD analysis with calculation of DDDs/100 bed days and a sample analysis of 500 patients’ prescriptions were performed for presenting drug utilization statistics in the infectious disease facilities of Volgograd region, which had been reassigned to treat patients with COVID-19 in 2020 and 2021.Results. Five or more drugs were administered simultaneously in 96.8% of patients. Antibacterial drugs were in 74.3% of the analyzed prescriptions in 2020 and in 73.5% in 2021. The total consumption of antibiotics was 102.9 DDDs/100 bed-days in 2020 and 95.7 DDDs/100 bed-days in 2021. The cases of multiple administrations of biological disease modifying antirheumatic drugs and the use of cyclophosphamide have been identified. In 73.6% of prescriptions in 2020 and 85.4% of 2021, omeprazole at the dose of 40 mg per day was used (77.3 and 84.6 DDDs/100 bed-days, respectively). In 2021, there were cases of concomitant intravenous prescribing of acetylcysteine under the trade name of Fluimucil® with tableted forms of ambroxol and acetylcysteine under the name of ACC®. The cumulative consumption of hepatotoxic drugs was 269.2 DDDs/100 bed-days in 2020 and 401.5 DDDs/100 bed-days in 2021.Conclusion. Lack of drugs with proven effectiveness for treatment of COVID-19, worked-out treatment algorithms, a high mortality of patients in the hospitals led to polypragmasy, excessive prescribing of drugs in the hospitals. The prescription of antibacterial drugs, omeprazole, mucolytics, hepatotoxic drugs, immunosuppressors in infectious hospitals should be monitored by clinical pharmacologist.
The aim of the study is the elaboration of Rules for Harvesting/Collecting of Pollen to minimize the risks associated with the use of pollen-based medicinal products. Materials and methods. The following electronic resources were used in the study: PubMed, Medline, ScienceDirect, Web of Science, Scopus, Google Scholar, eLibrary, World Allergy Organization, Cochrane Database, Stallergenesgreer, Allergenscienceandconsulting, Pharmacopoeia, Fda.gov, fs.usda.gov, Ema.europa.eu. The analysis covered the period from January 1, 2010 until December 31, 2021. Results. Currently, there are some general requirements for the quality of pollen in Russia, but there are no controls or standardised procedures for harvesting, drying, and purification of pollen. The USA and EU also lack established qualification programmes for pollen-collecting companies and/or individual pollen collectors. Regulatory authorities establish requirements only for visual control of raw materials or delegate responsibility to the manufacturer. The analysis of the existing regulatory documentation revealed lack of requirements for collection, storage, and processing of pollen used as the raw material for the production of allergen products. This calls for the elaboration of appropriate regulatory documents. The authors have compiled the Rules for Harvesting/Collection of Pollen, which include 6 parts. The Rules are intended for individuals directly involved in harvesting/collection of pollen, and contain requirements for pollen collectors, the process of pollen collection, documentation, storage, and transportation. Conclusion. The authors have prepared the Rules for Harvesting/Collecting of Pollen, which include 6 parts. The Rules cover the whole process of pollen collection and all related processes. The implementation of this document will improve the process of pollen collection, thus reducing the risks associated with the use of pollen-based medicines. Further studies will assess the impact of the pollen quality on the safety of medicinal products.
