Vol 3, No 1 (2021)

From the editor

From the editor

Narkevich I.A., Perelygin V.V.

Abstract

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.B., Sventitskaya A.M., Vengerovich N.G., Nikiforov A.S., Ivanov I.M., Proshina Y.A.

Abstract

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.V., Dzjuba A.S., Kaukhova I.E., Tretyakova A.E., Sakharov V.A.

Abstract

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.M., Okovityi S.V., Ivkin D.Y., Pyatibrat A.O.

Abstract

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

Stages of the objective assessment system development for the activities of the oncological service in Russia and the Northwestern Federal District of the Russian Federation (morbidity, mortality, index accuracy, annual mortality, median survival, observed and relative survival of patients with malignant tumors). Part I

Merabishvili V.M., Belyaev A.M.

Abstract

The first part of the study includes a brief historical outline on the creation of an objective system for assessing the activities of the oncological service in Russia and the Northwestern Federal District of the Russian Federation.Dynamic series of all types of indicators of the population’s morbidity and mortality have been presented, an increasing process of reliability and improvement of the quality of registration of primary patients with malignant tumors has been shown.In Russia, aswell as in the Northwestern Federal District of the Russian Federation, standardized indicators of the malignant tumorsincidence remain at a relatively low level. In the world ranking of Cancer Registries, the Russian Federation is on 300th place among 450 others.The mortality rate of the population in most localizations isrecorded above the average European indicators.

Pharmacy Formulas. 2021;3(1):46-55
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Stages of the objective assessment system development for the activities of the oncological service in Russia and the Northwestern Federal District of the Russian Federation (morbidity, mortality, index accuracy, annual mortality, median survival, observed and relative survival of patients with malignant tumors). Part II

Merabishvili V.M., Belyaev A.M.

Abstract

To plan anti-cancer measures and to correctly manage its condition, it is necessary to use only reliable sources of its formation. For this purpose, a system of Population-based or territorial Cancer Registries (PCR) has been created in Russia.The first Registry was the St. Petersburg PCR, created by us in 1993, which became the school of methodological preparation of the system in the administrative territories of Russia.The corresponding Order No. 420 of April, 19, 1996 issued by the Ministry of Public Health of the Russian Federationhas legitimizeda new organizational structure and entrusted it with the supervision of the P. Hertsen Moscow Oncology Research Institute.

Unfortunately, to date, the PCR databases are not used, when creating state reports, analytical developments on the PCR database are either not conducted, or are used extremely rarely.The only exception was the St. Petersburg PCR, and now the entire Northwestern Federal District of the Russian Federation (NWFD RF) and 6 more administrative territories operating under our programs.The materials of the real state of the oncological service, prepared on the basis of the St. Petersburg PCR database, have been published by us in more than 20 monographs in St. Petersburg and the Northwestern Federal District of Russia.

In this paper, we present the dynamics of analytical indicators calculated according to the PCR database, which sharply differ from the data of the Form No. 7 Annual Reports. The calculated indicators are close to the European average and have a positive trend.

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.K., Peshekhonov D.V., Pyatibrat A.O., Vengerovich N.

Abstract

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.S., Kozlov K.L., Shishkevich A.N., Bessonov E.Y., Lukjanov N.G., Pukhalskaya A.E.

Abstract

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.V., Motruk M.K., Lyubimtsev V.A., Susloparova O.N.

Abstract

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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Investigating the effects of Inonotus rickii extracts on the muscle contraction intensity

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

Abstract

The aim of this study is to test the effect of aqueous, ethereal and alcoholic extracts of the fruit bodies of the wood-destroying fungus Inonotus rickii on locomotor activity resulting from contraction of both cross-striated and smooth muscles. The pharmacological activity of I. rickii raw materials was determined in vitro using the dose-response curve method (smooth muscles) and in experiments with oral intake of extracts (CNS-mediated effects on cross-lacing muscles). The aqueous extract of fungal material showed an increase in the motor activity of smooth muscles compared to standard caffeine, which indicates the ability of fungal extract to have a stimulating effect on the synapses. It was found that I. rickii extracts have an effect on smooth muscle contraction similar to the acetylcholine. It was shown that the greatest stimulating activity demonstrates an aqueous extract that may be a result of inhibitory effect of diethyl ether and ethanol on synapses. The described effects put on the agenda both the fractionation of active extracts and further experiments on the therapeutic applications of their described properties. As a field of possible application of this kind of substances can be considered the cardiovascular remodeling, the maintenance of smooth muscle tone during a number of surgical interventions, and the palliative cure of disseminated cancers.

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.G.

Abstract

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.A., Stepanov S.V., Volgusheva A.O., Zvyagin Y.Y., Vorobeva S.A., Perelygin V.V.

Abstract

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.G., Zvyagin Y.Y.

Abstract

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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