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Vol 24, No 2 (2021)

Articles

MULTICOMPONENT MEDICINAL PREPARATIONS: ADVANTAGES OF THEIR USE IN CLINICAL PRACTICE

Nikolaev S.M., Shantanova L.N., Khobrakova V.B., Razuvaeva Y.G., Chukaev S.A., Khitrikheev V.E.

Abstract

The prospects of the use of multicomponent preparations in clinical practice are discussed on the base of the analysis of formularies. Today, many diseases are caused by stress, improper lifestyles associated with hypodynamie, impaired nutrition, and environmental distress. In this situation, it is necessary to regulate pharmacotherapy with complex drugs at the systemic level, which provides correction along the hierarchical ladder of life process management, mobilization of internal reserves for maintaining health, interfacing the action of the ingredients of the complex with the functional systems of the patient. In folk medicine of many countries, traditional eastern medicine, for thousands of years, multi-component (complex, combined, complex) drugs have been used, containing several ingredients, two or more active pharmacological substances. The inclusion of a number of medicinal components in one ready-made dosage form creates great amenities for the patient, eliminating the need to take many separate drugs, observing the order of their use, and experiencing inconvenience in the treatment and prevention of the disease. From the point of view of evidence-based medicine, they have withstood millennial trials, they have laid down centuries of experience in their successful use, and today, it is, multicomponent drugs of traditional medicine that are most interesting for research. The expressed effectiveness of the combined preparation is due to potentiation of the action of ingredients with unidirectional activity, but with different mechanisms. By reducing the proportion of components in the complex, the risk of undesirable effects when taken is reduced. Small doses of the components of the complex preparation allow modulating the natural processes of health restoration, accompanying the action of the main substances and creating conditions for the manifestation of the activity of the accompanying elements of the complex. The studies have shown that the complex drugs have a number of advantages: ease of use; drug potentiation; risk reduction of side effects; costs reduction; system effect of the complex as pharmacotherapeutic system. The emphasis is laid on the traditional combined remedies as their efficacy and safety have been proved for thousands of years and they are of great interest at present time.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(2):3-8
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INCLUSION OF RADACHLORIN PHOTOSENSITIZER INTO POLYMERIC MICROPARTICLES AS A PROMISING APPROACH TO IMPROVE ITS EFFICIENCY IN PHOTODYNAMIC THERAPY

Miroshkina A.M., Krechetov S.P., Solovyeva N.L., Krasnyuk I.I.

Abstract

The widespread use of photodynamic therapy as a method for treating oncological diseases is associated with its high efficiency and fewer side effects. The development of methods for the inclusion of photosensitizers into polymeric microparticles as delivery systems makes it possible to increase the accumulation of such particles by tumor cells and to reduce the manifestation of systemic undesirable effects. Based on a biocompatible copolymer poly(lactic-co-glycolic acid) microparticles with the inclusion of the photosensitizer radachlorin, perfluorodecalin, and magnetic nanoparticles were obtained by the double emulsion method. It is shown that exposure of the obtained microparticles to light radiation used in photodynamic therapy is accompanied by the formation of singlet oxygen, intensified by the presence of perfluorodecalin and magnetic nanoparticles in the polymer matrix. The research results make it possible to consider the obtained microparticles as a depot of radachlorin for local use in photodynamic therapy of tumors.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(2):9-14
pages 9-14 views

THE CONTENT OF PHENOLS (INCLUDING FLAVONOIDS) AND ANTIOXIDANTS IN THE LEAVES OF VISCUM ALBUM L. AND PYRUS COMMUNIS L

Adzhiahmetova S.L., Chervonnaja N.M., Pozdnjakov D.I., Oganesjan E.T.

Abstract

The results of a chemical study of polyphenols in Viscum album L. and Pyrus communis L. have been carried out in order to compare the composition of these compounds, which may be of great importance in the joint practical use of both plants as therapeutic and prophylactic agents. Aim of the study. Comparison of the polyphenol composition of Viscum album L. and Pyrus communis L. to determine the possible joint practical use of both plants as therapeutic and prophylactic agents. Material and methods. The test-objects were the leaves of Viscum album L. growing on a host-plant of Pyrus communis L. Raw material - the leaves of both plants, harvested in the fruiting phase. The guantitative determination of flavonoids was performed on a SF-102 spectrophotometer by the spectrophotometric method. The total content of phenolic compounds was determined spectrophotometrically from the products of their oxidation with the Folin-Chocalteu reagent. The total content of antioxidants was determined by the amperometric method using a calibration plot of the dependence of the output signal on the concentration of guercetin and gallic acid. Results. The maximum content of flavonoids in extracts from the leaves of the Viscum album L. and Pyrus communis L. is achieved when the raw material is extracted with 50% ethyl alcohol and is 0,552±0,004%; 2,63±0,010%, respectively. The highest content of the phenolic compounds was noted in 50% ethanolic extracts from leaves of Viscum album L. and Pyrus communis L., and is 2,679±0,009%; 13,14±0,16%, respectively. The total content of antioxidants in the analyzed extracts from the leaves of of Viscum album L. and Pyrus communis L. was determined by the amperometric method. The optimal extractant was ethyl alcohol 50%. Conclusions. Given the similarity of the chemical composition of the polyphenolic compounds of the leaves of Viscum album L. and Pyrus communis L., the leaves of both plants can be used for therapeutic and prophylactic purposes.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(2):15-22
pages 15-22 views

DEVELOPMENT OF THE QUANTITATIVE ANALYSIS METHOD OF THE FLAVONOIDS IN A SOFT DOSAGE FORM WITH PEONY EXTRACT OF GARDEN VARIETIES BASED ON TIZOL GEL

Nakaryakova N.I., Lyust E.N., Makhotina M.V., Peskova A.A., Soloveva V.V., Khoroshavina A.D.

Abstract

Varieties of garden peonies are of interest in the field of creating phytopreparations for the treatment of dermatological diseases due to its rich chemical composition. An important component in drug development is the assessment of product guality at all stages using methods that give reliable data. In this regard, the article is devoted to the development of a method for guantifying one of the main groups of biologically active substances, such as flavonoids, in a soft dosage form with peony extract of garden varieties dry in order to apply this method at various stages of guality control of this dosage form. For this purpose method of spectrophotometric determination of sum of flavonoids per rutin in extract of peony of garden varieties dry is modified. Integrated researches on the selection of the optimal solvent, the ratio of the recovery volumes and 2% aluminum chloride solution and the stability time of the flavonoid complex with the chromogenic reagent have been carried out since the analysis of the soft dosage form may be problematic due to the need to extract analysable substances from the ointment base. As a result of carried out studies extragent-alcohol ethyl 70%, ointment suspension 1.0 g, aliguot part of extraction of 2 ml, ratio of aliguot to chromogenic reagent 1:1 is chosen, with the time of sustainable complex of 30 minutes. In these conditions, the content of flavonoids in ointments with peony extract of garden varieties of dry 0,338 ± 0,015% is obtained, which is as close as possible to the content of this group of biologically active substances in the extract.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(2):23-28
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PHARMACOGNOSTIC STUDY OF THE POLLEN OF PINUS SYLVESTRIS L. AND PINUS PUMILA (PALL) REGEL

Erdyneeva S.A., Shiretorova V.G., Radnaeva L.D.

Abstract

Aim of the research. Characterization of the Pinus sylvestris (PS) and Pinus pumila (PP) pollen's external, anatomical and diagnostic features, phytochemical analysis and determination of raw material quality indicators, elemental composition. Materials and methods. The PS pollen was collected on the coast of the Lake Baikal, nearby village Manturiha, the PP pollen - at mountain range Ulan-Burgasyin 30 km from Ulan-Ude during May-June, 2020. Pollen quality indicators were determined according to RF State Pharmacopoeia. The total flavonoids and the total free amino acids were determined by spectrophotometric method, the content of tannins and ascorbic acid was determined according to pharmacopoeia methods. The quantitative content of elements in pollen was determined using atomic absorption spectrophotometer SolaarM6, after preliminary decomposition of pollen samples with concentrated nitric acid in the microwave system MARS 6. Results. The pollen of the studied pine species is a fine powder from light yellow to yellow (PS) and from yellow to dark yellow (PP) color. The smell is specific, weak. The taste is sweetish. The microscopy of pollen grains showed that they have a similar structure for both pine species, and consist of a body and two air sacs. The following indicators of raw material quality were determined: moisture content - 7.15-8.06%; total ash - 2.68-3.22%; ash insoluble in 10% HCI - 0.18-0.13%. The largest amount of extractive substances from pollen is extracted with 60% ethyl alcohol: from pollen PS - 35.51%, PP - 32.64%. The content of flavonoids (0.64-0.83%), free amino acids (2.45-3.65%), tannins (0.32-0.76%), ascorbic acid (33.84-34.21 mg%) was determined. The pine pollen elemental composition analysis results showed that the macroelements with highest content are potassium (11493-12942 mg/kg), and magnesium (925-1045 mg/kg), trace elements - manganese (65-155 mg/kg) and zinc (44-54 mg/kg). The content of heavy metals in pollen of both species is significantly lower than the limits established for medicinal plant products. Conclusion. For the first time the pharmacognostic study of the Pinus sylvestris and Pinus pumila pollen, growing in Buryatia, was carried out. The main external and anatomical-diagnostic features of pollen were determined, the similarity of features for PS and PP was established. The presence of flavonoids, tannins, amino acids, polysaccharides, ascorbic acid in the pollen of both pine species was established. The pollen's quality indicators satisfy the requirements for powdered medicinal plant raw materials and bee pollen. Analysis of the quantitative content of biologically active substances showed that PP pollen contains more free amino acids and tannins, and PS pollen contains slightly more flavonoids and ascorbic acid. The analysis of the elemental composition showed that the PS and PP pollen is rich in macroelements and trace elements, especially potassium, magnesium, manganese, iron and zinc. The content of heavy metals in pine pollen does not exceed the limits for medicinal plant raw materials. The results of this study could be useful in development of new therapeutic substances of plant origin from pine pollen, as well as to introduce it into official medicine as a medicinal plant material.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(2):29-34
pages 29-34 views

BINARY MEDICINAL SYSTEM: ANTIINFLAMMATORY ACTIVITY OF THE BINARY EUTECTIC SYSTEM

Tkachenko M.L., Loseva M.A., Zhnyakina L.E., Lyamin A.V.

Abstract

Eutectics are guite often considered pharmaceutical incompatibilities due to possible complications in the technology for the production of dosage forms; nevertheless, the eutectics themselves may be of interest as a promising form-forming basis for the development of new drugs with predictable biopharmaceutical characteristics. The aim of this work is to study phase eguilibria in the solid dispersed system «Diclofenac - Mexidol» and also to conduct preclinical tests of the anti-inflammatory activity of the eutectic composition of the system under consideration. The study of the binary system «Diclofenac - Mexidol» was carried out on a DSC-500 differential scanning calorimeter provided with a package of applied programs for automatic processing of the experimental results. In this work, under the name «Diclofenac», we used the corresponding acid, namely 2 - [(2,6-dichlorophenylamino) phenyl] acetic acid (CAS-15307-86-5), obtained by us by precipitation of diclofenac from a sodium solution (FS 42-0260-07) with mineral acid and then purified by repeated recrystallization from ethanol to obtain the same melting point (DSC) of the substance in the last two fractions (m.p. 158.3 ± 0.2 °С). Mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate), CAS code: 127464-43-1, manufacturer - Obninsk Chem.Pharm. company (JSC OHFK). It has antihypoxic, membrane protective, nootropic, anticonvulsant and anxiolytic effects, increases the body's resistance to stress, melting temperature 112 °С. Preclinical tests of the anti-inflammatory activity of the eutectic mixture of Diclofenac with Mexidol were carried out in comparison with pure Diclofenac on 30 intact laboratory outbred rats of both sexes with an average weight of 200-250 g. The experiments were carried out in accordance with the rules of good laboratory practice (GLP) during preclinical studies. in the Russian Federation, as well as the rules and International Recommendations of the European Convention for the Protection of Vertebrate Animals used in Experimental Research (1986). The data of phase eguilibria of the «diclofenac-mexidol» system are presented. It has been found that the eutectic is realized at a ratio of 30: 70 mol% (33.2: 66.8% by weight) with a melting point of 92 °С. The anti-inflammatory activity of the eutectic was more than 6 times higher than that of diclofenac.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(2):35-41
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STUDY OF THE ANTI-DIABETIC ACTIVITY OF HELICHRYSUM THIANSCHANICUM REGEL. IN ALLOXAN HYDRATE DIABETES MODEL

Sharofova M.U., Sagdieva S.S., Yusufi S.J., Numonov S.R., Rahmonov R.U., Ferubko E.V., Lupanova I.A.

Abstract

Relevance. The limited herbal medicines list is usedto prevent and treat the diabetes mellitus at present. The prospective raw material for such investigations is the Helichrysum thianschanicum Regel., the medicinal plant that widely grows in Tajikistan. The aim of the study was to investigate the antidiabetic properties of the Helichrysum thianschanicum Regel, flowers and leaves infusion in experimental diabetes model. Material and methods. We used 36 white nonlinear rats of both sexes weighing 180-220 grams. Flowers and leaves of the Helichrysum thianschanicum Regel, were collected in the Darvaz region (2400m above sea level) - the Republic of Tajikistan in July-August 2016-2017. The study of the antidiabetic activity was performed on the alloxan diabetes model in rats. Results. It was found that the Helichrysum thianschanicum Regel, flowers and leaves infusion has a significant antidiabetic and metabolism-corrective effect, improving the functional parameters of the kidneys and liver, has a antiatherogenic activity. Conclusion. The results show that the Helichrysum thianschanicum Regel, flowers and leaves infusion has potential for preclinical research and antidiabetic drug development.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(2):42-48
pages 42-48 views

INFLUENCE OF SUCCINATE ON SOME INDICATORS OF BIOENERGY METABOLISM IN SEMINAL VESICLES AND EPIDIDYMIS IN MALE RATS UNDER CONDITIONS OF CHRONIC HYPOXIA

Marsyanova Y.A., Zvyagina V.I.

Abstract

Relevance. Lactate in the cell performs a number of functions in the regulation of metabolism and is involved in energy metabolism. Under conditions of hypoxia, cells switch to succinate oxidation to maintain energy metabolism. The mechanism of action of succinate as an effective antihypoxic agent has been little studied, but its effectiveness is beyond doubt. Objective. Evaluation of changes in lactate level and LDH activity under conditions of chronic hypoxia and during the use of succinate. Material and methods. We used a model of chronic hypoxia in the modification: the animals were placed in a sealed chamber with a volume of 1.2 liters, connected to a gas analyzer, and were there until the oxygen content in the air reached 10%. The experiment was repeated daily for 14 days. The introduction of succinic acid was carried out in the form of a 4% solution in 0.9% NaCl intraperitoneally for 14 days at a dose of 100 mg / kg. Determined lactic acid and LDH activity in the cytoplasmic and mitochondrial fractions of seminal vesicles and epididymis. Results. Chronic normobaric hypoxia leads to a significant decrease in LDH activity in the epididymis head both in the cytoplasmic and mitochondrial fractions, and to a decrease in LDH activity in the epididymis tail only in the cytoplasm. In the seminal vesicles, no statistically significant changes in LDH activity were found under conditions of chronic hypoxia. The introduction of succinate against the background of hypoxia led to an increase in LDH activity relative to the group with hypoxia of the cytoplasmic fraction in the tail and the mitochondrial fraction of the epididymis head. The accumulation of lactate in the mitochondria of the epididymis head and in the cytoplasm of the seminal vesicles was also noted. Conclusions. Chronic normobaric hypoxia leads to inhibition of LDH activity. The accumulation of lactic acid occurs with an increase in the LDH activity of the mitochondrial fraction in comparison with the LDH activity of the cytoplasm. The receipt of succinate by animals during chronic hypoxia led to an increase in lactate in the mitochondrial fraction and facilitated adaptation of the mitochondrial function.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(2):49-54
pages 49-54 views

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