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Vol 22, No 12 (2019)

Articles

Igor' Vasil'evich Matveychuk (k 70-letiyu so dnya rozhdeniya)

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Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):3-4
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Direction of development of medical treatment of infectious conjunctivities (literature review)

Kovalenko A.V., Shatalov D.O., Kedik S.A., Gromakova A.I., Kaplun A.P., Ivanov I.S., Sterin I.V.

Abstract

Eye pathologies are serious diseases of modern man. Conjunctivitis make up about 35% of all eye diseases, they are the main clinical forms of eye infection - 66.7% of the total number of patients with inflammatory eye diseases. Conjunctivitis is an inflammatory disease of the conjunctiva, a thin transparent tissue that lines the inner surface of the eyelid and the visible part of the sclera, which has an infectious or other etiology. Infectious conjunctivitis is classified according to the course of the disease (acute or chronic) and etiological factor. By etiology are divided into the following types - bacterial, viral, chlamydial and fungal. The typical symptoms for bacterial conjunctivitis are copious discharge from the eyes; when dried, it gives a crust on the eyelashes and eyes. One of the problems arising from the use of various antimicrobial agents (biocides, antibiotics) is the ability of microorganisms consisting of representatives of one species or the association of microorganisms to form biofilms. Drugs that can prevent the development of biofilms or disrupt the structure are now of great interest all over the world. Recently, a number of guanidine-based polymeric preparations have become widely spread, the merits of which include a wide range of antimicrobial activity, both with respect to bacteria, yeast, viruses, and with respect to vegetative cells and fungal spores. One of the promising oligomeric guanidine derivatives is a branched oligohexamethylene guanidine hydrosuccinate. In conclusion, we can say that cationic polymers have a number of advantages compared with the traditionally used antimicrobial substances. Proven high efficacy against a number of pathogenic microorganisms, especially against yeast fungi of the genus Candida and Pseudomonas aeruginosa, and low toxicity makes it possible to use oligohexamethienguanidine hydrosuccinate as substances of pharmaceutical use, including for creating effective drugs for the treatment and prevention of infectious conjunctivitis.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):5-11
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A new method for selective extraction of euglobals with monoterpenoid structure from Eucalyptus viminalis leaves

Boyko N.N., Zhilyakova E.T., Pisarev D.I., Novikov O.O., Mizina P.G., Saybel O.L., Sidelnikova M.K.

Abstract

The purpose of this work is to test experimentally a working hypothesis about the possibility of euglobals' extraction from Eucalyptus viminalis leaves with two different perfluoro organic solvents, Novec 1230 and Novec 7100. Materials and methods. For extraction of euglobals from Eucalyptus viminalis leaves, we used a circulation method for extraction in Soxhlet extractor at plant raw material / solvent ratio 1:5 w/v. For analysis of euglobals, we used a method of reverse phase high performance liquid chromatography. As standard euglobal-containing substances, we used Spissum extract of Chlorophyllipt standard sample of the State Pharmacopoeia of Ukraine and eucalimin standard sample. Results. It is determined that perfluoro organic solvent Novec 1230 does not extract euglobals, while solvent Novec 7100 exhibits selective but incomplete extraction level of euglobals with monoterpenoid structure. A circulation method of solvent Novec 7100 in Soxhlet extractor demonstrates that in two hours of extraction from Eucalyptus viminalis leaves, the yield of dominant euglobal with monoterpenoid structure was equal to 49.3±2.5 %, and the yield of dry residue relatively to plant raw material initial weight was equal to 0.63±0.03 %. In the extract obtained, no chlorophylls or macrocarpales were detected. Conclusions. Our working hypothesis about the possibility of euglobals' extraction from Eucalyptus viminalis leaves with perfluoro organic solvent has been verified experimentally. The yield of euglobals significantly depend not only on the fluorination degree of the solvent molecule, but also on the value of topological polar surface area of euglobal molecule. A new method for selective extraction of euglobals with monoterpenoid structure from Eucalyptus viminalis leaves by perfluoro organic solvent Novec 7100 has been suggested.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):12-22
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The phase diagram of the binary medicinal condensed system «Ketoprofen - Phenylbutazone»; anti-inflammatory activity of the binary eutectic system

Seryakova A.N., Tkachenko M.L., Moschenskyi Y.V.

Abstract

The data of phase equilibria of the condensed system «Ketoprofen - Phenylbutazone » are represented according to the results of measurements by the method of the differential scanning calorimetry (DSC) in the heating mode. It is established that the eutectic system reters to the eutectic systems with restricted (partial) mutual solubility in the solid state. Congruent equilibrium for this system is implemented at a ratio of 60:40% mol. (55,3:44,7% of mass.) of Ketoprofen and Phenylbutazone respectively. Melting point of the eutectic structure is 68 °C. Data shows the phase diagram of a system melting state. Preclinical tests of antiinflammatory activity were carried out on model of acute exudative inflammation (carrageenan edema of rats paw) on white outbred rats in comparative option with the use of: substances of Phenylbutazone, substance of Ketoprofen, mix of Phenylbutazone and Ketoprofen in the ratio 1:1 mol. and the eutectic system «Ketoprofen - Phenylbutazone». The results of experiments showed that the anti-exudative and antiinflammatory activity of the eutectic structure is twice higher than activities of individual components and their mix 1:1 mol. in comparable doses.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):23-28
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Development and validation of the method of quantitative determination of fluorine-containing drugs by the method of highly effective liquid chromatography

Tyutrina V.A., Chmelevskaya N.V., Illarionova E.A.

Abstract

Objective. To develop and validate methods for the quantitative determination of fluorine-containing drugs in tablets by high performance liquid chromatography. Material and methods. In the work we used: pharmaceutical substance and tablets of linezolid, efavirenza and ofloxacin, which meet the requirements of regulatory documents. To develop methods for detecting and quantifying linezolid, efavirenz, and ofloxacin in tablets, a reverse-phase version of high-performance liquid chromatography in gradient elution was used, the conditions of which were selected experimentally. Optimal chromatographic conditions: column size - 75 x 2 mm, polymer sorbent - ProntoSil 120-5C AQ, mobile phase - Eluent A: 0.2 M LiClO4 - 0.005 M HClO4 (pH 2,8), Eluent B: Acetonitrile, gradient: 3700 pl from 5% to 70% eluent B, flow rate 100 pl / min, column temperature 40 ° C, sample volume 2 pl, wavelength 210 nm. Results. The conditions found were used to develop methods for the quantitative content of these substances in tablets. The retention times of ofloxacin were 15.39 minutes, linezolid 16.16 minutes and efavirenza 34.49 minutes. The relative error of the quantitative determination by the developed methods does not exceed 1.22% for ofloxacin, 1.08% for linezolid and 1.39% for efavirenz. Findings. During the study, unified methods were developed for the quantitative determination of fluorine-containing heterocyclic drugs - linezolid, efavirenz, and ofloxacin in tablets by high-performance liquid chromatography. A validation assessment of the developed methods was carried out. Thus, the developed methods make it possible to obtain sufficiently reliable and reproducible results for the intended field of application and can be recommended for pharmaceutical, chemical-toxicological, and forensic chemical analysis.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):29-33
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Development of betaine hydrochloride as a pharmaceutical substance for the production of a drug analog acidin

Kajsheva N.S., Kajshev A.S., Mikelov V.A., Mnatsakanyan A.V., Maslovskaya E.A.

Abstract

The aim of the study was to prove experimentally the possibility of separating betaine hydrochloride (acidin) from post-alcohol corn bard and to study its analytical parameters. The object of the bard corn grain distillery alcohol production enterprise «Suvorov». The technology of betaine hydrochloride separation consists in: separation of bard into liquid and solid phases, removal of carbohydrates from the liquid phase (in the form of calcium saccharate), its neutralization with ammonium oxalate, concentration, treatment with concentrated hydrochloric acid, activated carbon, crystallization of betaine hydrochloride. The target product is purified with 96% alcohol, concentrated hydrochloric acid, recrystallization. To solve analytical problems, a substance used as a standard sample of acidin was isolated from the tablets «Acidin-pepsin» (Republic of Belarus). The test and standard samples of betaine hydrochloride were compared according to analytical parameters: physical and chemical (description, solubility in water and alcohol, pH of 1% aqueous solutions), authenticity (reaction of thermal decomposition of N-methylated α-aminoacids, complexation with copper (II) ions, deposition with silver ions), quantitative content (alkalimetric titration in the presence of phenolphthalein). As a result of the study, betaine hydrochloride (acidin) was isolated from the liquid phase of post - alcohol corn bard with a technological yield to the liquid phase - 0.8% (crude) and 0.4% (purified), which is 2-4 times more than molasses bard (traditional raw material). In addition to the target product (betaine hydrochloride), purified glutamic acid (0.1% to the liquid phase), calcium saccharate (3.0% to the liquid phase), a mixture of humins and potassium chlorides, sodium (0.4% to the liquid phase) are additionally isolated from the liquid phase of bards. According to physical and chemical parameters, the test and standard samples of betaine hydrochloride are identical: white crystalline powders, easily soluble in water and alcohol, pH, respectively, 1.05 and 0.93. Both samples gave positive results for the reaction of authenticity: the characteristic smell of trimethylamine in the thermolysis reaction, blue crystalline precipitates in the com-plexation reaction, white curd precipitates in the deposition reaction. The quantitative content of betaine hydrochloride in terms of dry matter in the test sample was 99.2%, in the standard sample - 99.9%. The possibility of obtaining betaine hydrochloride from domestic secondary raw materials with a large technological output, its identity with the standard sample create the prospect of import substitution of drugs based on betaine.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):34-37
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Comparative study of the composition of essential oil Phlojodicarpus sibiricus (Steph. Ex Spreng.) Koso-pol. from the eastern Baikal region and its anti-radical activity

Taraskin V.V., Potonova A.V., Gulyaev S.M., Dylenova E.P., Nikolaev Y.N., Tykheev Z.A., Urbagarova B.M.

Abstract

Aim of the research: a comparative study of the composition of essential oil obtained from the herb, rhizomes and roots of Phlojodicarpus sibiricus (Steph. ex Spreng.) Koso-Pol. from the population of Pribaikalsky region and determination of its antiradical activity. Material and methods. The objects of studying were herb, rhizomes and roots of Phlojodicarpus sibiricus (Steph. ex Spreng.) Koso-Pol. growing within the Pribaikalsky region of the Republic of Buryatia (Lake Baikal's coast), collected during bearing stage of growth (July, 2017). Essential oils from the herb, rhizomes and roots were obtained using commonly used method - steam distillation. The content of essential oil was determined using volumetric method. The qualitative composition and relative quantitative content of the components of essential oils was identified by gas-chromato-mass spectrometric method. The analysis of antiradical activity of obtained essential oils was conducted using DPPH-test. Results. For the first time the chemical composition of essential oils obtained from herb, rhizomes and roots of Phlojodicarpus sibiricus from the population of Pribaikalsky region was studied. According to the results the stability of the composition of essential oils depending on the place of growth was shown. Y-Terpinene (14.8%), cis-Nerolidol (9.84%), Germacrene D (9.70%) and p-Cymol (7.04%) were the main components of essential oil from the herb. In the essential oils from rhizomes and roots the main constituents were Y-Terpinene (29.60%), Terpinolene (22.85%), p-Cymol (15.95%) and Limonene (7.64%). High antiradical activity of the investigated essential oils was established. IC50 for essential oils from the aerial part of Phlojodicarpus sibiricus was 13.44 |jg/ml, and from rhizomes and roots - 16.07 |jg/ml. In addition, high antiradical activity of essential oils contained in pharmacologically active water-alcohol extracts may partly explain their neuroprotective activity. Conclusion. The chemical composition of the essential oils obtained from herb, rhizomes and roots of Phlojodicarpus sibiricus from the Pribaikalsky population was studied. High antiradical activity of analyzed essential oils was estimated. As a result, we found it rationally to obtain essential oils from the raw material during the development of coumarin-containing remedies.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):38-43
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Daghestan natural samples of the seeds of Carum carvi L. as sources of terpenoids

Vagabova F.A., Musaev A.M., Aliev A.M., Radjabov G.K.

Abstract

The component composition of the essential oil of the fruits of Carum carvi L., collected from the natural populations of Dagestan in 2015 during their full maturation, was studied for the first time. The investigated essential oil obtained from the fruit by the method of hydrodistillation on the device clevenger within 3 hours. The resulting oil had a light yellow color, the output was from 1.35 to 4.88%, depending on the place of growth of raw materials. Chromato-mass spectral analysis of the component composition of volatile substances of essential oils revealed 12 characteristic compounds for this type. Each of the chromatographic peaks is identified by a retention index and MS data. The main components of the essential oil of seeds of all the population are carvon (47.55-52.59%) and limonene (43.67-48.02%), making up about 90% of the sum of all components. These compounds have a wide pharmaceutical effect. It should be noted that some valuable components, such as carvacrol, were not found in the essential oils of the fruits of the Daghe-stani samples of C. carvi, but compounds were found that are not characterized by the samples of essential oils given in the literature. Cluster analysis by the component attribute of C. carvi fruit essential oils showed a strong scatter of cumin seed populations between samples according to geography.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):44-50
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The K, Na, Ca, Mg, P content in the hair of foreign male students of the first year of education

Skalny A.A., Kirichuk A.A., Lobanova Y.N., Barinov A.V., Titov N.V., Chernyavka A.I., Tkachenko B.D., Chizhov A.Y.

Abstract

It is known that external and internal factors influence the formation of human mineral metabolism depending on its habitat, climate, nutrition, nature and type of activity, features and national traditions. Aim. Assessment of the content of potassium, sodium, calcium, magnesium, phosphorus in the hair of students to identify the features of mineral exchange of foreign students depending on the region of permanent residence; according to the results of the survey to recommend a set of measures aimed at reducing the incidence, increasing adaptive capacity, improving the quality of life and education in the first year of study at the University. Material and Methods. Male (177 people) students of the first year of study (average age from 18 to 38 years), who came to study from different countries of the world, were selected hair samples for analysis of the content of macroelements (K, Na, Ca, Mg, P) by inductively coupled plasma mass spectrometry (ISP-MS) on the Nexion 300D device ("Perkin-Elmer", USA) after microvawe decomposition. Results. The content of these macroelements in hair was compared between groups of foreign male students from different countries, as well as foreign students with Russian students. The elemental composition of hair in different countries is different, especially the difference in the content of calcium in the hair of students of the 5th and 6th groups compared to the 4th. In terms of potassium content, a significant difference was found in the 3rd group compared to the 1st and 2nd. According to the concentration of magnesium in the hair, significant differences were observed between groups 1 and 3, 1 and 4, 2 and 5, 3 and 4, 5 and 4, 6 and 4. In terms of sodium content, significant differences were found between the 1st and 3rd groups. The phosphorus concentration was significantly different in groups of 5 and 3. Conclusions. Determination of the content of potassium, sodium, calcium, magnesium and phosphorus in the hair of foreign students of the first year of study with subsequent corrective measures can be recommended in order to improve adaptation, increase the effectiveness of training and reduce morbidity.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):51-57
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80 let Nauchno-issledovatel'skomu i uchebno-metodicheskomu tsentru biomeditsinskikh tekhnologiy FGBNU VILAR

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Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):58-61
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Nauchnoe nasledie akademika S.S. Debova (k 100-letiyu so dnya rozhdeniya)

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Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):62-63
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ISSLEDOVANIE BIOFORTIFIKATsII RASTENIY ASTRAGALA ShERSTISTOTsVETKOVOGO (ASTRAGALUS DASYANTHUS PALL.) AMINOKISLOTOY L-SELENOTsISTINOM

Poluboyarinov P.A., Elistratov D.G.
Problems of Biological Medical and Pharmaceutical Chemistry. 2019;22(12):64-64
pages 64-64 views

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