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Vol 23, No 6 (2020)

Articles

Excipients for use in medicated chewing gum technology

Alekseev K.V., Blynskaya E.V., Tishkov S.V., Bueva V.V., Ivanov A.A.

Abstract

Chewing gum medicines are a dosage form having unique characteristics such as elasticity, plastic deformation, chewing, optimal organoleptic properties and the release of pharmaceutical substance only during chewing. The shown properties of chewing gum medications are provided by a combination of various auxiliary substances, some of which are characteristic for obtaining these dosage forms. For example, the use of combinations of insoluble and soluble components: elastomers (Jelutong, Chicle, isobutylene and isoprene copolymers, etc.), polyvinyl acetate, texturants (magnesium and calcium carbonates, titanium oxide, etc.), plasticizers (terpene resins , lecithin, etc.), emulsifiers, sweeteners (sorbitol, xylitol, aspartame, potassium acesulfame, etc.), waxes, dyes, flavors, antioxidants, lubricants and glidants. The article presents a modern classification of excipients used for chewing gum medicinal products according to their functional purpose, discloses the features of the use of auxiliary substances in the technology for producing chewing gum medicinal products. In addition, various aspects of the use of the presented individual excipients, complex excipients and excipients that perform certain specific functions to modify release, etc. are described. The article presents a large number of examples of many classes of auxiliary substances used, includes basic ratios, mass fractions of components, primary and additional functional purpose, as well as technological aspects of their use. New directions of searching and improving the formulations of chewing gum medicines, for example, the development of biodegradable bases, the use of ion-exchange resins and cyclodextrins, have been reflected. Features of the use of some flavorings explains the aspects of taste masking depending on the pharmaceutical substance. A correlation was made between the ratio of components and the structural-mechanical, textural properties of the dosage form, such as chewing, hardness, stickiness, adhesion to the tooth surface, as well as the release of a pharmaceutical substance. The conclusion is drawn about the features of application, prospects and development trends of modern excipients for chewing gum medicinal.
Problems of Biological Medical and Pharmaceutical Chemistry. 2020;23(6):3-9
pages 3-9 views

Analysis of the range of drugs used for diabetes

Pavets N.R., Dzhavakhyan M.A.

Abstract

According to the State Register of Diabetes Patients, as of January 2015, in the Russian Federation, there are 4.04 million patients in terms of access to medical institutions: type 1 diabetes - 340 thousand and type 2 diabetes = 3.7 million (the most common type 2 diabetes) count. However, these figures are considered according to the results of the control and epidemiological studies conducted by the Endocrinological Research Center (ENC) of the Ministry of Health of the Russian Federation in the period from 2002 to 2010, do not reflect the true picture. The number of patients with diabetes in Russia is approximately 3-4 times more than officially registered and reaches 9-10 million people, which is about 7% of the population. Currently, diabetes mellitus (DM) is the most common among endocrinological diseases. The growth in the number of diabetes diseases over the past 10 years has doubled and amounted to 387 million people. According to the forecasts of the International Diabetes Federation, by 2035 592 million people will suffer from diabetes.
Problems of Biological Medical and Pharmaceutical Chemistry. 2020;23(6):10-15
pages 10-15 views

The study of the elemental composition of the herb Galega officinalis (Galega officinalis L.)

Bakun A.S., Gurina N.S., Tsarenkov V.M.

Abstract

Relevance. The medicinal value of plants is determined by the content of not only biologically active substances in them, but also macro-and microelements, the accumulation of which is due to environmental factors and the nature of plants. A promising object of study as a source of macro- and microelements is Galega officinalis (Galega officinalis L.). This plant is used in folk medicine as a hypoglycemic, hypolipidemic, lactogonous, antimicrobial agent, but it is not pharmacopoeial. The purpose of the work is to study the elemental composition, the content of heavy metals, arsenic, mercury, and the specific activity of cesium-137 in the samples of the herb Galega officinalis. Material and methods. The object of the study was the herb Galega officinalis, harvested in 2015-2017 in the Vitebsk region of the Republic of Belarus. Sample preparation for obtaining the mineral residue was carried out byashing samples of the herb Galega officinalis in a muffle furnace at a temperature of 600 °C for 1 hour. The structure and elemental composition of the mineral residue were studied by scanning electron microscopy with electron probe chemical analysis. The content of heavy metals, arsenic, and mercury was carried out by inductively coupled plasma atomic emission spectrometry. The specific activity of cesium-137 was determined by registering gamma radiation with a scintillation detection unit, followed by converting the obtained data using an information processing unit. Results. As a result of the study of the elemental composition of the herb Galega officinalis 9 elements were discovered and a series of accumulation of macro- and microelements was compiled: O > K > Ca > C > Mg > P > Cl > Si > S. Copper, zinc and chromium were found in samples of the herb Galega officinalis, which increases the pharmacological value of the herb Galega officinalis as a means for the prevention of diseases associated with the lack of these trace elements, in particular diabetes mellitus. No toxic heavy metals (lead, arsenic, mercury, cadmium)and radionuclides were detected in the herb of the Galega officinalis, which indicates the safety of this type of medicinal plant material and the possibility of its preparation in the natural and climatic conditions of the Republic of Belarus. Conclusion. The herb Galega officinalis can be used as a potential source of biotic elements for the treatment and prevention of diseases of various etiologies associated with disturbances in trace elements, as well as pathological conditions bordering on them.
Problems of Biological Medical and Pharmaceutical Chemistry. 2020;23(6):16-21
pages 16-21 views

Development of the methods of identification and quantitative determination of flavonoids in the herb of the groundnut peavine (Latyrus tuberosus L.)

Bubenchikov R.A., Kulik O.N., Bubenchikova K.R.

Abstract

Relevance. The article is devoted to the standardization of the raw material of the groundnut peavine to the legume family (Fabaceae). The groundnut peavine (Lathyrus tuberosus L.) is a perennial herbaceous plant that grows widely in the chernozem zone of Russia. Objective. The aim of the work was the development of methods of identification and quantitative determination of flavonoids in the herb of groundnut peavine. Material and methods. The object of study is the grass of the groundnut peavine, harvested during flowering in 2018-2019. The basis for qualitative definition of flavonoids is thin-layer chromatography, the basis of quantitative determination is spectrophotometric method. Results. When conducting quality identification installed the following conditions were established: Sorbfil plates on an aluminum substrate, the volume of application of the studied extraction - 10 ml, mobile phase: e butanol-acetic acid-water (4: 1: 2), the standard substance is rutin, cinaroside; detection treatment with 5% solution of aluminum chloride. Validation of the methodology. For the quantitative determination of flavonoids, a spectrophotometric determination method was developed in terms of rutin. The optimal extraction conditions were established. Conclusion. The procedure has been developed a technique for the qualitative identification and quantitative determination of flavonoids in the groundnut peavine herb. The content of flavonoids ranged from 1,88%±0,07% to 2,40±0,04%.
Problems of Biological Medical and Pharmaceutical Chemistry. 2020;23(6):22-27
pages 22-27 views

Mycelial fungi using for secondary processing of medicinal plant raw materials

Gordonova I.K., Nikitina Z.K.

Abstract

Currently, in the treatment of many chronic diseases, drugs based on medicinal plant raw materials are widely used. Modern herbal medicines, as a rule, combine high efficiency, relative safety and breadth of therapeutic action. In the production of many galenic and neogalenic preparations, in most cases, waste products of plant raw materials containing various biopolymers, including cellulose, the presence of which can, under certain conditions, induce the synthesis of the corresponding hydrolases - cellulases. The reviewed article is devoted to solving the actual problem of using mycelial fungi for secondary processing of medicinal plant raw materials. As an example of waste of plant raw materials, the authors used a schroth of roots and rhizomes of Rubia tinctorum, formed in the process of dry extract obtaining in the experimental production Department of All-Russian Scientific Institute of Medicinal and Aromatic Plants. A characteristic feature of various originschroth is a low fat content and a relatively high number of proteins and cellulose-containing substances. Previously, the authors showed that micromycetes from the VILAR collection have the ability to hydrolyze some insoluble proteins and various types of celluloses. In this regard, it is absolutely logical to try to use these biological objects for conversion of schroth. The article shows that all the studied mycelial fungi grew well on media with the replacement of easily metabolized carbohydrate with the schroth of the roots and rhizomes of Rubia tinctorum. Micromycetes formed lysis zones during surface cultivation, which indicates the synthesis and secretion of hydrolases into environment. In the result of a detailed study of 13 fungal strains, as well as regression and correlation analysis, were selected 5 micromycetes that are promising for secondary processing of medical plant raw materials.
Problems of Biological Medical and Pharmaceutical Chemistry. 2020;23(6):28-33
pages 28-33 views

Does threonine possess any ketogenic action?

Malinovsky A.V.

Abstract

With diabetes the glucogenic or ketogenic character of one or another amino acid reveals itself more distinctly. The introduction of the former into the organism decreases the ketosis indication, whereas that of the latter increases this meaning.Threonine is conventionally considered to be the glucogenic amino acid like phenylalanine, tyrosine and isoleucine. As it is stated in the present paper, in the process of evolution a man on the genetic level lost the ability to the synthesis of threoninedehydrogenase - a ferment which can be found with many animals and which could participate in transformation of threonine to acetyl - koa, and therefore to ketone bodies. Thus, conclusion about the full absence of ketogenic action with man can be made.
Problems of Biological Medical and Pharmaceutical Chemistry. 2020;23(6):34-38
pages 34-38 views

Patients laboratory testing optimization in infectious hospital under the pandemia of the new coronavirus infection COVID-19

Pushkin A.S., Akhmedov T.A., Rukavishnikova S.A., Yakovlev V.V., Saginbaev U.R.

Abstract

Relevance. In order to prevent the spread of infection caused by the SARS-CoV-2 virus, in the spring of 2020, a number of hospitals were re-profiled in St. Petersburg toreceive patients with pulmonological pathology, including infectious etiology. In the period from March 30 to April 30, 2194 patients were admitted to St. Petersburg City Hospital №2, including 1211 (57%) with pneumonia of various etiologies, 508 (24%) patients with COVID-19 and 475 (22%) patients with other acute upper respiratory tract infections. The aim of this study was to evaluate the structure of the results of prescribed studies to optimize the laboratory service and assess the laboratory and examined patients profiles. Results structure assessment of a general blood tests showed the predominance of relative lymphocytopenia- in 51.9%; hemodilution in 57.9%; the average platelet volume was below the reference limits of 59.6%. Leukocytosis was observed in 46.5% and neutrophilia in 53.7%. Absolute monocytosiswas found in 45%. Tests analysis of the biochemical analytes concentrations showed elevated levels of: C-reactive protein - in 74.8%; glucose - in 73.9%; troponin I - in 75.6%; lactate dehydrogenase - in 63.4%; procalcitonin -in 55%; gamma-glutamyltranspeptidases - in 52%. Conclusion. To optimize the laboratory service of the hospital, the quantity of goods was increased by no more than 10% in government contracts concluded with suppliers of laboratory reagents, which made it possible to purchase additional supplies to ensure uninterrupted laboratory examination of patients in the infectious hospital in the conditions of the new coronavirus infection COVID-19.
Problems of Biological Medical and Pharmaceutical Chemistry. 2020;23(6):39-44
pages 39-44 views

Study of liposome encapsulated monoacetate glycolysis inhibitor as an antitumor agent in a Lewis lung carcinoma model

Buyko E.E., Korshunov D.A., Kondakova I.V.

Abstract

Background. Advances in understanding the molecular mechanisms associated with the Warburg effect have become the basis for the creation of new specific anti-glycolytic agents. Despite their successful preclinical trials, many new anticancer agents based on glycolysis inhibitors have failed in clinical trials, demonstrating systemic toxicity. An effective approach to reducing systemic intoxication is targeted drug delivery using liposomes. However, there are technical difficulties in obtaining liposomes for low molecular weight compounds, which include glycolysis inhibitors, as well as the efficiency of delivery to the tumor due to the peculiarities of liposome biodistribution and pharmacokinetics. Aims. To evaluate the antitumor and antimetastatic effects of a monoiodoacetate glycolysis inhibitor immersed in liposomes. Material and methods. The therapeutic effect of antimetabolite was evaluated in C57BL/6j mice using a Lewis lung carcinoma model. Methotrexate was used as a reference preparation. Liposomes were obtained by extrusion. Ready liposomes were purified from the not included component by dialysis methods. Liposomes were injected through the tail vein. Results. The inhibition of the growth of the primary tumor in iodoacetate in an independent form was comparable with the effect of methotrexate, reaching an average of 15%. Treating with liposomal forms of iodoacetate increased the growth inhibition index to 25%. Inhibition of the growth of lung metastases in iodoacetate and methotrexate was stronger than the effect of drugs on the primary tumor. The averages in these treated groups were 65%. The liposomal form of iodoacetate, in contrast to the similar form of methotrexate, did not significantly inhibit the growth of metastases. Conclusions. Liposomal forms of iodoacetate inhibit the growth of the primary focus more strongly in comparison with their independent action, however, as a result of changes in biodistribution, the antimetastatic effect decreases.
Problems of Biological Medical and Pharmaceutical Chemistry. 2020;23(6):45-49
pages 45-49 views

INFLUENCE OF A CINNAMIC ACID DERIVATIVE ON CHANGES IN THE ACTIVITY OF MITOCHONDRIAL RESPIRATORY CHAIN COMPLEXES IN EXPERIMENTAL BRAIN ISCHEMIA

Pozdnyakov D.I., Zolotyh D.S., Larskij M.V.

Abstract

Relevance. It is known that mitochondrial dysfunction is a significant pathogenetic mechanism of ischemic brain damage and a promising pharmacotherapeutic target for cerebroprotective therapy. The aim of the study. To evaluate the effect of 4-hydroxy-3,5-di-tret-butyl cinnamic acid on the change of the mitochondrial respiratory chain complexes activity in rats brain supernatant in cerebral ischemia conditions. Material and methods. The study was performed on male Wistar rats that reproduced cerebral ischemia using the Tamura method. 4-hydroxy-3,5-di-tret-butyl cinnamic acid was administered at a dose of 100 mg / kg (per os) after 30 minutes when ischemia was reproduced and then once a day for 3 days. On day 4, a change in the activity of mitochondrial complexes I, II, IV, and V in the supernatant of the brain was assessed by the respirometric method. Results. Against the background of the administration of 4-hydroxy-3,5-di-tret-butyl cinnamic acid into animals, an increase in the activity of mitochondrial complexes was noted: NADH-dehydrogenase; succinate dehydrogenase; cytochrome c - oxidase; F1F0 ATP synthase in relation to animals that did not receive pharmacological support by 71% (p < 0.05); 86% (p < 0.05); 2.29 times (p < 0.05) and 1.9 times (p < 0.05) times, respectively. It should be noted that the 4-hydroxy-3,5-di-tret-butyl cinnamic acid test compound exceeded the reference drug succinic acid in an equivalent dose in terms of therapeutic efficacy. Conclusions. Based on the obtained results it can be assumed that 4-hydroxy-3,5-di-tret-butyl cinnamic acid has a cerebroprotective effect due to the restoration of mitochondrial function and the elimination of energy deficiency arising in the area of ischemic penumbra.
Problems of Biological Medical and Pharmaceutical Chemistry. 2020;23(6):50-54
pages 50-54 views

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