卷 3, 编号 1 (2021)

From the editor

From the editor

Narkevich I., Perelygin V.

摘要

Top universities, along with scientific organizations, have been taking a number of measures to modernize science and education and adapt them to the needs of the real sector of the economy in the implementation of the Strategy for Scientific and Technological Development of the Russian Federation until 2035. Most measures have been implemented.

Pharmacy Formulas. 2021;3(1):8-9
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Pharmaceutical Sciences

Docking of highly selective 5-HT2A/C receptor peptide ligands with antipsychotic activity

Orlova A., Sventitskaya A., Vengerovich N., Nikiforov A., Ivanov I., Proshina Y.

摘要

Search for new ligands selective to different subtypes of 5-HT2 receptors is an important scientific and practical problem for experimental psychopharmacology and clinical medicine. The majority of existing antagonists of the 5-HT2A and 5-HT2C subtypes possess all necessary anti-anxiety and antipsychotic properties, though they are partially selective to 5-HT2B receptors. Their activation leads to cardiotoxic side effects, so it significantly limits clinical application of these drugs.

For the search of new highly selective ligands of 5-HT2A/C receptors, an in silico screening algorithm was proposed using PScore.Max and Affinity.maxPScore parameters, which included the affinity of low molecular weight compounds for each 5-HT2 receptor subtype. Cyclic physiologically active substances of peptide nature have been proposed as new promising drugs with antipsychotic activity. Based on the CXXC library, a number of cyclopeptides with a high selectivity of structure to target binding sites were selected for further in vitro studies by extending of the peptide chain.

It was also found that a promising direction for increasing the selectivity of peptide ligands to 5-HT2A/C receptors is the introduction of non-proteinogenic amino acids during the formation of an initial docking library. The choice of these amino acids will be due to the nature of interactions between the reference ligands and amino acid residues of the binding site.

Pharmacy Formulas. 2021;3(1):10-17
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The development of an algorithm for introduction of a new drug on the existing pharmaceutical production. Stage 2. Transfer of technologies

Basevich A., Dzjuba A., Kaukhova I., Tretyakova A., Sakharov V.

摘要

The paper presents the results of the study based on the guidelines and scientific data on the technology transfer in the circulation of drugs. The initial data for calculations, assessment and analysis of the study results were taken from the current documentation at the operating production site of the pharmaceutical manufacturer with the participation of the company officials. The data was collected from the company work papers and job descriptions following interviews with a group of unit staff involved in the technology transfer.

The summary and the analysis of the data obtained during the research on the technology transfer for the preparation of new drugs were implemented. It was used to construct Gantt charts for some critical processes. Theassessment of the criticality of individual stages of technology transfer and a control chart of the project manager, indicating the control points of this process, was presented.

Hence, the original action plan for the new drug preparation by a pharmaceutical manufacturer has been developed: risk control and assessment system for the technology transfer project activities has been determined to assess the degree of criticality of deviations, both for the individual stages and the entire technology transfer project.

According to the objectives of the study, an original action plan for the new drug preparation by the pharmaceutical manufacturer based on the collection, processing and analysis of the data on the technology transfer at the manufacturing site has been developed.

If required, the original action plan may be tested by other drug manufacturers in the pharmaceutical industry.

Pharmacy Formulas. 2021;3(1):18-30
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The significance of the original characteristics of the active substance of injectable chondroitin sulfate preparations for intramuscular injections in the evidence-based medicine

Napalkova S., Okovityi S., Ivkin D., Pyatibrat A.

摘要

Given the data from normative control resources and the research and development information system of the Ministry of Science and Education of the Russian Federation, we were unable to review the results and the quality of publications comprising method development and analytical validation of quantitative and qualitative values of injectable chondroitin sulfate preparations for intramuscular injections.

Therefore, the results obtained in the research “The development of a method for determining the intrinsic viscosity of an injectable chondroitin sodium sulfate preparation for intramuscular injections of 100 mg/ml, 2 ml” remain valid, the method is considered reliable and practical.

The materials and methods used in the research “The development of a method for determining the intrinsic viscosity of an injectable chondroitin sulfate preparation” have provided the possibility to determine the intrinsic viscosity for injectable chondroitin sodium sulfate preparations for intramuscular injections and the use of 0.2 M sodium chloride solution as a solvent. Also, the viscosity of the tested solutions in the concentration range of chondroitin sulfate 4.5-20 mg/ml was accurately сalculated, the value of the intrinsic viscosity determined for each of the preparations under test was in the range of 0.03-0.042 m3/kg.

This study presents the results of a review of recent information, published in a number of academic journals, concerning modern approaches to the treatment and major clinical problems when applying chondroprotectors for arthrological diseases treatment.

Considering the continuing interest in chondroprotectors, stability problems with formulations and modern possibilities in the application of machine learning in drug discovery, additional pharmaceutical design research (Drug design) is expected - from the docking stage to the quantum calculations stage.

Pharmacy Formulas. 2021;3(1):32-45
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Biomedical Sciences

俄罗斯和俄罗斯联邦西北区肿瘤科活动客观评估系统的发展阶段 (恶性肿瘤患者发病率、死亡率、登记可靠性、年死亡率、中位存活期、观察存活率和相对存活率),第一部分。

Merabishvili V.M., Belyaev A.M.

摘要

俄罗斯和俄罗斯联邦西北区肿瘤科活动客观评估系统的发展阶段 (恶性肿瘤患者发病率、死亡率、登记可靠性、年死亡率、中位存活期、观察存活率和相对存活率),第一部分。

Pharmacy Formulas. 2021;3(1):46-55
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俄罗斯和俄罗斯联邦西北区肿瘤科客观评估系统的发展阶段 (恶性肿瘤患者发病率、死亡率、登记可靠性、年死亡率、中位生存期、观察存活率和相对存活率),第二部分。

Merabishvili V.M., Belyaev A.M.

摘要

基于抗癌措施计划与了解癌症服务状况应只使用其形成的可靠来源,为此,在俄罗斯成立了地区群体癌症登记系统.首个地区群体登记处,是1993年建立在圣彼得堡的地区群体癌症登记处。它成为创造俄罗斯各种行政区肿瘤服务活动的客观评估系统的方法论学派。俄罗斯卫生部于1996年4月19日发布的第420号命令使新的组织结构合法化,并委托P.A. 赫尔岑莫斯科肿瘤学研究所监督。遗憾的是,到现在国家状态报告形成时,不使用群体基于抗癌措施计划与了解癌症服务状况,及其形成的可靠来源。为此,俄罗斯成立了地区群体癌症登记系统登记处的数据库。但以群体癌症登记处数据库为基础的分析研究很少应用,只有圣彼得堡的群体癌症登记处应用了。现在,全俄罗斯联邦西北区和其他六个行政区也按我们的程序工作。以圣彼得堡群体癌症登记处数据库基础为基础,发表了20多篇关于圣彼得堡的、7个关于俄罗斯联邦西北区的表示肿瘤服务真实状态的专题文章。

在本论文中,我们表了以群体癌症登记处数据库为基础计算的分析指标的动态。这些指标跟7号年度报告的数据完全不一样。计算的指标接近欧洲的平均指标,并有积极的动态。

Pharmacy Formulas. 2021;3(1):56-65
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Comparison of the therapeutic effectiveness of the drug Mucosat based on glycosaminoglycans in oral and parenteral dosage forms in the treatment of osteoarthritis

Peshekhonova L., Peshekhonov D., Pyatibrat A., Vengerovich N.

摘要

The study aims to compare the methods of Mucosat drug use and administration for achieving the desired therapeutic effect in the treatment of osteoarthritis.

Despite extensive evidence base, improving complex therapy schemes for the use of successive and complementary dosage forms with the appropriate drug administration and use in order to achieve the desired therapeutic effect is still a valid aim.

In the course of the study, 50 knee osteoarthritis patients were examined and treated during the period from November, 2019 to April, 2020.

A clinical trial was carried out to assess Mucosat oral and parental administration effectiveness in the patients comparing their physical activity, functional ability and quality of life. The number of undesired side effects identified the degree of therapeutic tolerance against the comorbid diseases identified. A comparison of the therapeutic efficacy and tolerability of Musocat intramuscular and capsule administration, patient compliance, the need to take non-steroidal anti-inflammatory drugs (NSAIDs) was drawn.

Statistica 12 and Excel 2016 were used to carry out the statistical analysis of the data obtained. The study was generally marked by diagnostic accuracy with the use of modern methods, group homogeneity, prospective observational design.

By the time of pharmacotherapy completion, physical activity has become optimal in the study groups. However, parental therapy had significantly higher effectiveness than the oral one on all the subscales. As a result, articular syndrome severity has been reduced and the functional state of the joints expanded.

The study has shown that Mucosat demonstrates high efficacy both in injectable solution and capsule dosage forms as a basic chondroprotective drug. Mucosat pharmacotherapy course has contributed to permanent discontinuation of NSAIDs before completion of the therapy. The superiority of Mucosat parenteral administration over the oral one has been proven.

Pharmacy Formulas. 2021;3(1):66-75
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Dementia in elderly patients as a consequence of arterial hypertension: a literature review

Mikhailov S., Kozlov K., Shishkevich A., Bessonov E., Lukjanov N., Pukhalskaya A.

摘要

Alzheimer’s disease and vascular dementia are important causes of cognitive decline in the elderly and senile. This problem is becoming increasingly important in connection with the general aging of the world population and an increase in the number of patients with concomitant pathology, among which arterial hypertension plays an important role. There are a number of studies proving the link between arterial hypertension in middle age and dementia in the elderly. It is hoped that the normalization of blood pressure among middle-aged people will reduce the incidence of cognitive dysfunction. It is also known that maintaining blood pressure at acceptable levels in elderly and old people can improve brain function and reduce the prevalence of dementia, but it is not entirely clear which blood pressure numbers are optimal.

Pharmacy Formulas. 2021;3(1):76-83
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Biological sciences

Comparative bioelectronic diagnostics of the ecological state of contaminated water areas (on the example of some ducts of the Volga River Delta)

Kholodkevich S., Motruk M., Lyubimtsev V., Susloparova O.

摘要

Three Volga river delta ducts located in the city of Astrakhan and the Astrakhan region were chosen as objects for bioindication of the ecological status. The aim of the study was to carry out comparative bioelectronic diagnotics of the ecological status of the branches with different size and type of antropogenic load. The assessment was based on the physiological state (health) of the inhabitants – bivalve mollusc Anodonta anatine. The analysis of heart rate of the molluscs was implemented by the fiber-optic bioelectronic system. It has been found that Anodonta anatine collected demonstrate different heart rate recovery time after a 1-hour functional loading within 117–166 minutes. This is the case in mussels inhabiting significantly polluted water areas with the “Bad” ecological status. This characteristic of the water areas fully coincides with the ecological status of the Volga river delta ducts, according to the State report “On the state and protection of the environment in the Russian Federation in 2017”. In this report, the authors propose and substantiate the possibility of using the water area of the Gandurino River as a conditional reference duct for the Volga river delta region. In this case, by the value of the Ecological Quality Ratio (EQR),the status of the Gorodskoy and Maly ducts may be considered as “Good” regional ecological status.

Pharmacy Formulas. 2021;3(1):84-91
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Inonotus rickii (瑞克纤孔菌) 提取物对肌肉收缩强度影响的评估

Ranadive K.​., Jagtap N.V., Jagtap P.N., Zmitrovich I.V., Perelygin V.V.

摘要

本研究的目的是测试木腐真菌Inonotus Rickii子实体的水提取物、酯提取物和醇提取物对动物横切肌和平滑肌收缩引起的运动活性的影响。采用“剂量-反应” 曲线法(平滑肌)和口服提取物实验(CNS介导的对横断面肌的影响)in vitro 测定了I. rickii原料的药理活性。菌类材料水提取物与标准咖啡因相比,平滑肌运动活性呈现增加,这说明菌类提取物具有对突触的刺激作用。研究发现,I. rickii提取物具有类似神经递质乙酰胆碱的平滑肌收缩作用。同时,水提取物显示了最大的刺激活性,这可能与乙醚和乙醇对胆碱能受体的抑制作用有关。所描述的效应将活性提取物的分馏和所描述效应的治疗应用的进一步实验都提上了议事日程。该物质可能应用的领域包括心血管重塑,在一系列手术中维持平滑肌张力,以及对恶性肿瘤的姑息治疗。

Pharmacy Formulas. 2021;3(1):92-96
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Information and Prevention

Medical gas supply systems in the context of a pandemic

Kravchenko A.

摘要

Medical gases have long been used in healthcare. After pipelines began to be used everywhere in the 50s of the last century instead of heavy and clumsy gas supply systems from high-pressure cylinders, it became an almost universal requirement for hospitals to have systems for supplying medical oxygen, carbon dioxide, nitrous oxide, air and providing medical vacuum.

Pharmacy Formulas. 2021;3(1):102-103
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Heritage

Pyotr Ivanovich Astrakhantsev: the first post-war director of the Leningrad Institute of Pharmacy

Narkevich I., Stepanov S., Volgusheva A., Zvyagin Y., Vorobeva S., Perelygin V.

摘要

There were several periods in the history connected with the rebuilding of the Saint Petersburg State Chemical and Pharmaceutical University, which is over a century old, due to certain events related to the fate of Russia. One of these periods came after the Great Patriotic War. Some students and teachers were evacuated, some joined front line troops, others stayed in besieged Leningrad to live and work. Part of the facilities was evacuated. Another part was destroyed and lost. It was necessary to start all over again.

Based on unpublished documents from Saint Petersburg archives, this paper reconstructs the biography of P.I. Astrakhantsev (1905–1961), a university graduate, chemist, the first post-war director of the Leningrad Institute of Pharmacy. His life path was connected with Alma Mater, as well as with the work in the leading chemical institution of the USSR – the State Institute of Applied Chemistry (at present the Russian Scientific Center of Applied Chemistry) – he also taught chemistry in the 1st Leningrad Medical Institute, Molotov Pharmaceutical Institute, All-Union Correspondence Forest Engineering Institute.

Pharmacy Formulas. 2021;3(1):104-110
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The role of scientists in the Department of Psychiatry at the S.M. Kirov Military Medical Academy in the development of domestic narcology and pharmacological methods of treating this pathology

Tchudinovskih A., Zvyagin Y.

摘要

The study covers the history of the formation and development of narcology in the Russian Empire and the USSR. The role of the heads and psychiatrists in the Department of Psychiatry and the Clinic of Mental and Nervous Diseases at the S.M. Kirov Military Medical Academy in the fight against alcoholism in the country and the organization of drug treatment was identified. Particular emphasis was laid on the work of Vladimir M. Bekhterev, a prominent Russian and Soviet psychiatrist, neuropathologist, physiologist and psychologist, the founder of reflexology and pathopsychological direction in Russia. It was V.M. Bekhterev who did everything to reverse public views on alcoholism and transfer it from the category of moral turpitude to the status of the disease; he organized the research and treatment for alcoholic patients. This paper considers the aspects of scientific development of narcological issues by the staff and heads of the departments. The priority of domestic psychiatrists in the theoretical justification and practical application of conditioned reflex therapy for alcoholism has been shown.

Pharmacy Formulas. 2021;3(1):112-119
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