Vol 5, No 3 (2017)



Nasukhova N.M., Logvinenko L.A., Kharchenko A.L., Konovalov D.A.


Laurus nobilis L. is an evergreen dioecious, rarely monecious plant up to 12-15 m high. The plant’s name is devoted to an Ancient Greek God of Sun Apollo and is a symbol of peace and victory. It was used in making up wreaths for emperors, generals, and poets. Its natural area includes Mediterranean countries with high level of annual precipitation. It is actively cultivated as a decorative plant in Europe, Russia, USA and other countries. It is cultivated in Turkey, Algeria, Morocco, Portugal, Spain, Italy, France, Russia, and Mexico. The aim of the study is the review of available literature about isolation, identification, quantitative determination of biologically active compounds of the Laurus nobilis leaves in the established species and their pharmacological activity. Materialsand methods. The study was carried out using searching (PubMed, CiteSeer, arXiv), library databases (eLibrary, Cyberleninka), and ResearchGate free social network. Results and discussion. We have established that Laurus nobilis leaves have components of essential oil, phenolic compounds, and sesquiterpenic lactones as the principal active substances. Qualitative composition and quantitative content of these compound groups in these raw materials varies depending on the ecological and geographical, edaphic, climatic factors, phase of the plant growth, cultivation technology, drying method etc. The results of the pharmacological studies of the extracts, summary fractions, and individual compounds of Laurus nobilis leaves characterize this type of raw materials as a perspective source for a more profound study. Conclusion. As the available open review data showed, the essential oil components, phenolic compounds (phenolic acids, flavonoids, etc), sesquiterpenic lactones of Laurus nobilis exhibit a diverse spectrum of pharmacological activity. Antimicrobial (widely), anti-virus, anti-inflammatory, anti-diabetic, and cytoxic (anticancer) activities, established in extracts, certain fractions, and individual compounds of Laurus leaves compounds are perspective from the point of further studies and development of new treatment and preventive medicinal drugs.
Pharmacy & Pharmacology. 2017;5(3):200-221
pages 200-221 views


Popova T.V., Karabinceva N.O., Rachkovskaya L.N., Tolstikova T.G., Kotlyarova A.A., Letyagin A.Y.


Modern technology and the level of fundamental studies allow us to create the medical sorbents with the predetermined structural, mechanical and adsorptional properties. Sorption materials are interesting not only as detoxicants that are used to remove toxic agents from the liquid media, but also as carriers for a delivery in zones a therapeutic effect of biologically active substances. The aim of this work is the substantiation of structure of the multifunctional drug with anti-bacterial and detoxifying effects due to the complex of silver and the sorption component – alumina-silica-containing sorbent. Materials and methods. We used physico-chemical (sorption activity of methylene blue dye, specific surface, pH in contact with water, atomic emission spectrometry with inductively coupled plasma) and pharmaceutical methods (bulk density, dissolution test for solid dosage forms). Results and discussion. The two-stage method of immobilization of a complex of silver and water repellent on the surface sorptionmatrix was justified. The sample of the optimum composition of silver-containing drugs was selected: aluminium oxide-hydroxide – 99.2%, clustered silver (Argovit – C – 2%) – 0.3 %, based on silver and subsidiary substance (repellents – brand PMS P – 841) – 0.5 %. The output of silver into the solution from the specified sample composition for 8 hours did not exceed 1,6 ± 0,3%, the value of specific surface area of 90 m2/ g, the value of pH to 8.1 ± 0.02, bulk density 1.12 ± 0.11 g/cm3. Conclusion. An experimentally substantiated composition of silver-containing drug AlSi/Ag was received, a comprehensive scientific data of its physico-chemical and technological properties were obtained.
Pharmacy & Pharmacology. 2017;5(3):242-253
pages 242-253 views


Marchenko M.A., Zilfikarov I.N., Ibragimov T.A., Maleev A.G.


The article presents new approaches to standardization of dry extract and medicinal preparations (MD) of ginkgo bilobate. Methods for the spectrophotometric determination of flavonoids, terpenolactones and ginkgoic acids in the active pharmaceutical substance “Ginkgo biloba dry extract “ (further in the text “ginkgo extract”), as well as methods for analysis of MD “GINKGO, tablets coated with 40 mg” (“GINKGO”, Tablets) and “GINKGO, solution for enteral use, 40 mg/ml “(“GINKGO, solution”). The aim – development and validation of methods for standardization of plant-derived APS – ginkgo extract, as well as MD based on it. Materials and methods. The samples of the APS “Ginkgo biloba dry extract “, MD “GINKGO, tablets” and “GINKGO, solution”, produced by CJSC “VIFITEH” (Russia) served as the objects of the study. Research methods: spectrophotometry (further in the text “SF-metry”) and high-performance liquid chromatography (HPLC). Used equipment: SF-56 spectrophotometer manufactured by LLC “LOMO-SPECTR” (Russia) and liquid chromatograph of the brand Shimadzu Prominence LC-20AD (Japan) with software control and computer processing of analysis results. Results and discussion. The use of the method of SF-metry optimizes the analysis process not only during the standardization of the finished product, but also at all stages of industrial production of MD within the framework of interoperational control. The content of the sum of flavonoids in the samples of two series of ginkgo extract in terms of rutine was determined by direct SF-metry – (29.64 ± 0.36)% and (28.88 ± 0.54)%; method of differential SF-metry – (21.78 ± 0.41) and (20.98 ± 0.24)%. The content of the amount of flavonoids in the preparations “GINKGO, tablets” and “GINKGO, solution” was: by direct SF-metry – (9.84 ± 0.15) mg/tab. and (10.07 ± 0.10) mg/ml; Method of differential SF-metry – (7.33 ± 1.13) mg/tab. and (8.30 ± 0.13) mg/ml, respectively. The analogues “MEMOPLANT” (“Dr. Willimar Schwabe GmbH & Co. KG”) and “TANAKAN®” (“Beaufour Ipsen Industrie”) were analyzed – the results obtained are comparable. Methods for quantitative determination of the amount of terpenolactones in the APS by the method of differential SF-metry and the residual content of the sum of ginkgoic acids by the direct SF-metry method are developed. During their approbation it was found that the amount of ginkgolactones in the samples studied is 7.87 ± 0.17% and 8.03 ± 0.22%, calculated as bilobalide, and the residual content of ginkgoic acid does not exceed 10 ppm. The expediency and effectiveness of using the HPLC method for simultaneous determination of the authenticity and evaluation of the benign nature of the substance and MD ginkgo was confirmed. Conclusion. The methods of the SF metric quantification of the amount of funds have been developed. The developed methods meet the validation tests, are characterized by accuracy and reproducibility in combination with simplicity of execution and are tested in the conditions of pharmaceutical production.
Pharmacy & Pharmacology. 2017;5(3):222-241
pages 222-241 views


Sabirzyanov D.R., Karpenko Y.N., Malkova T.L., Alekseeva I.V.


Anilocaine is a local anesthetic from the group of substituted amides, synthesized in the Perm State Pharmaceutical Academy. Anilocaine shows high surface anesthetic, infiltration and conduction anesthesia and shows the high efficiency in the various fields of medical practice. The quality of produced medicines depends on the quality of pharmaceutical substances. The purity is one of the most important parameters of the quality of pharmaceutical substances. The aim of this work was the development and validation of methods for identification of specific impurities in the substance of anilocaine by high-performance liquid chromatography (HPLC). Materials and methods. Studies were performed on liquid chromatography LC-20 Prominence (Shimadzu, Japan) equipped with a diode-array detector (SPD-M20A). Chromatographic column was Zorbax SB-C18 (4.6 mm × 250 mm, 5 μm). Validation assessment of the developed method conducted in accordance with the requirements of FP XIII and international requirementsICH (International Conference on Harmonization). Results and discussion. An experiment on the selection of the conditions of chromatographically showed that optimal separation of anilocaine and possible impurities (identified and unidentified) by the method of reversed-phase HPLC is observed in isocratic mode, using an eluent based on phosphate buffer pH 3 and acetonitrile. The flow rate of mobile phase is 1 ml/min; wavelength detection is 210 nm. Time check chromatogram is 20 minutes. Conclusion. The method for the quantitative determination of impurities in the substance of anilocaine by high-performance liquid chromatography was developed as the result of the research. The validation procedure of the analytical methods established its specificity, linearity, precision and accuracy. This method is included in the project monograph on substance of anilocaine.
Pharmacy & Pharmacology. 2017;5(3):254-266
pages 254-266 views


Chervonnaya N.M., Kharchenko I.I., Adzhiakhmetova S.L., Mykots L.P., Andreeva O.A., Oganesyan E.T.


Big molecular weight conditions are responsible for some properties, which are absent in low molecular compounds. Therefore, its determination allows revealing of some physical and technological properties of biopolymers and prediction of the possibility of their practical application. The aim of this work was to determine an average molarweight, to study the superficial properties at the border of “solution-air” phases, and to establish an isoelectric spot of water solutions of pectin substances (PS), isolated from a solvent cake of Tagetes patula inflorescences. Materials and methods. Polysaccharide complexes were isolated from the solvent cake of Tagetes patula inflorescences of Carmen species which was left after a raw material extraction with ethanol 40% with the method of Kochetkov and M. Sinnera. The time of water and PS solutions flow out was measured by the use of a capillary Ostwald viscosimeter; different types of viscosity were calculated. The density of solutions was determined by using a picnometric method, however due to the closeness of density of the analyzed solutions and water, they were not considered in the calculation of the relative viscosity. Series of solutions with 0.01 to 0.5% concentrations were prepared from 1% PS water solutions to determine a surface activity. Monometric liquid tension variations were set in Rehbinder’s apparatus in the moment of an air bubble appearance on the surface of PS solution. Isoelectric spot (IES) of PS was determined in acetate buffer solution with pH within 3.2 to 6.2 by using the viscometer method. Results and discussion. Fractioning of the obtained polysaccharide complexes showed that efficiency of the pectin substances amounted to 2.2%. Calculation shows that an average molar weight of PS amounted to 45272 g/mol. About the degree of interaction between macromolecules of polymer and solvent, structural properties of macromolecule, the degree of its branching can be judged by the value of Huggins test. The value was found to be 1.46, which proves the low solubility of PS in water. Apparently, a biopolymer chain has been branched which worsen the solubility of macromolecules and further may promote the formation of gelcondition. PS, isolated from the solvent cake of Tagetes patula, belong to the group of the surface active substances. Due to a big cross section of a molecule (S) and the high average molar weight, (45272 g/mol) molecules occupy a big volume at the surface of phase separation. We have established that macromolecule is in the isoelectric state at pH = 4.7. Conclusion. In the result of the studies using viscometer method, we have determined a molar weight of PS equal to 45272 g/mol. Huggins constant (1.46) which is connected to a low solubility of PS in water has been determined. We have established that PS, isolated from the solvent cake of Tagetes patula, are surface active. We have shown that PS macromolecule is in the state of polyamphion at pH = 4.7.
Pharmacy & Pharmacology. 2017;5(3):267-282
pages 267-282 views


Hladkykh F.V.


One of the main problems of the use of acetylsalicylic acid (ASA) is its withdrawal or initial “non-prescription” resulted from the prior developed or potential side effects in the gastrointestinal tract. In this case, the reasons for the abolition of ASA are not only serious complications in the form of gastrointestinal bleeding or perforations, butalso dyspeptic phenomena that are accompanied by the ongoing development of aspirin-induced gastroenteropathy. The aim of the study. To characterize the mechanisms of antiulcerogenic action of agonist TRPV1 (transient receptor potential vanilloid 1) vanillin (100 mg/kg) on the model of subchronic ASA-induced gastropathy in rats. Materials and methods. The study was performed on 35 mature male rats. Gastropathy induced by ASA was simulated by a fiveday intragastric (i.g.) introduction via the orogastric probe of an ASA suspension of 150 mg/kg/ day during 5 days. Omeprazole (50 mg/kg, i.g.) and vanillin (100 mg/kg, i.g.) were administered in the form of suspensions 60 minutes prior to the use of ASA. The concentration of malonic dialdehyde, and the activity of catalase were determined in the homogenates of gastric mucosa. The prooxidant/antioxidant ratio (ProAntidex) was calculated dased on the ratio of catalase activity (mcat/kg) and the concentration of malondialdehyde (MDA concentration (umol/kg). The content of NO metabolites in the stomach tissues was determined by the method of Miranda K.M. et al. Results and discussion. Preventive prophylactic use of vanillin (100 mg/kg) leads to the decrease in the intensity of processes of lipid peroxidation in the gastric mucosa caused by the action of ASA (150 mg/kg). This was indicated by a statistically significant (p≤0.05) decrease of 26.4% in MDA content and an increase in catalase activity by 29.0% relatively to those animalswith ASA-induced gastropathy without correction. Also, the use of vanillin resulted in a statistically significant (p≤0.05) increase in the content of NO metabolites by 68.0% (841.4 ± 35.95 umol / g) relatively to the animals of the control group. With the combined use of vanillin and omeprazole, a statistically significant (p≤0.05) absolute normalization of the NO metabolite level (927.4 ± 34.78 mmol/g) in the gastric mucosa was established, which corresponded to the indices of intact animals. Conclusion. The study showed that the activation of vanilloid (capsaicinoid) receptors due to the use of TRPV1 agonist, in particular vanillin, can reduce deistvie ulcerogenic NSAID, including ASA, that allows to consider the TRPV1 agonists as a new class gastroprotective drugs.
Pharmacy & Pharmacology. 2017;5(3):283-301
pages 283-301 views

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