Vol 10, No 1 (2022)

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.

Abbreviations: CNCD – chronic non-communicable diseases; RF – Russian Federation; WHO – World Health Organization; BMI – body mass index; WC – waist circumference; HC – hip circumference; CVD – cardiovascular diseases; NA – anorexia nervosa; BN – bulimia nervosa; PO – pathological overeating; GIT – gastrointestinal tract; AH – arterial hypertension; BP – blood pressure; DM2 – type 2 diabetes mellitus; CI – confidence interval.

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.

Abbreviations: AsA – ascorbic acid; SP – State Pharmacopoeia; OAs – organic acids; GPM – General Pharmacopoeia Monograph; PM – Pharmacopoeial Monograph; BASs – biologically active substances.

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.

Abbreviations: MP – medicinal product; DP – drug product; DF – dosage form; PS – pharmaceutical substance; API – active pharmaceutical ingredient; PVP – polyvinylpyrrolidone; MCC – microcrystalline cellulose; SCC – sodium croscarmellose; SSG – sodium starch glycolate; MS – magnesium stearate; SSF – sodium stearyl fumarate; GPM – General Pharmacopoeia Monograph.

The aim of the article is to evaluate the effectiveness of the thioctic acid preparation in the complex therapy of type 1 diabetes 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 effectiveness 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 carbohydrate 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 indications and monitoring the effectiveness of therapy makes it possible to implement a personalized approach to prescribing preventive treatment in T1DM children.

Abbreviations: GCP – good clinical practice; HbA1c – glicated hemoglobin; LADA – Latent Autoimmune Diabetes of Adults; MODY – maturity onset diabetes in youth; pNN50% – the mean number of times an hour in which the change in successive normal sinus (NN) intervals exceeds 50 ms; SDNN – standard deviation normal to normal; VLF – very low frequencies; АVА – arteriolo-venular anastomoses; ALA – Alphalipoic acid/α-lipoic acid; DCAN – diabetic cardiovascular autonomic neuropathy; VVR – vegetative-vascular regulation; ESPALIPON II – an octanoic acid bridged with two sulfurs; NATHAN I – Neurological Assessment of Thioctic Acid in Diabetic Neuropathy; LDF – Laser Doppler Flowmetry; HDLP- High-Density Lipoprotein; LDLP – Low-Density Lipoprotein; HR – heart rate; T1DM – type 1 diabetes mellitus; TG – triglycerids; ECG – electrocardiography; BMI – body mass index.

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.

Abbreviations: COVID-19 – novel coronavirus infection (Coronavirus disease 2019); AV – Artificial ventilation; GIT – gastrointestinal tract; ECMO – Extracorporeal membrane oxygenation; ITT – population of all included (Intent-to-treat) patients; PP – the population of patients who completed the study according to the protocol (Per protocol); NAATs – nucleic acid amplification techtiques; NYHA – New York Heart Association; e-IRK – electronic individual registration card; ARDS – Acute Respiratory Distress Syndrome; CRP – c-reactive protein; ESR – erythrocyte sedimentation rate; NAATs – Nucleic Acid Amplification Techniques; GIT – gastrointestinal tract; HR – heart rate; AspAT – aspartate transaminase; ALT – alanine aminotransferase; ULN – upper limit of normal; UDE – undesirable effects; IGs – Interim Guidelines; NSAIDs – non-steroidal anti-inflammatory drugs; GGT – gamma-glutamyl transpeptidase; CK – creatine kinase.