Vol 6, No 5 (2018)



Konovalov D.A., Khamilonov A.A., Shevchuk O.M., Logvinenko L.A.


Artemisinin is a sesquiterpene lactone isolated from the aerial part of sweet wormwood (Artemisia annua L.) in the 1970s. Based on its derivatives, the most effective medicines for the treatment of malaria have been created and are widely used. Over the past two decades, numerous in vitro and in vivo studies have been performed. They have shown the anticancer activity of these drugs in relation to certain cancer cell lines. The aim of the study is the review the scientific information on the clinical cases and the results of clinical trials carried out using drugs based on artemisinin derivatives. Material and methods. The study was conducted with the use of information search (PubMed, ScholarGoogle,) and library databases (Cochrane, eLibrary, Cyberleninca), as well as ResearchGate application for semantic search. Results and discussion. It has been established that the largest number of known clinical cases and completed clinical studies is associated with the study of the anticancer activity of one of the artemisinin derivatives - artesunate. The data obtained by various research groups do not yet allow us to speak of a pronounced activity of the latter. However, the facts of prolonging the life of patients, improving its quality, increasing control over the disease have been established. Conclusion. The published data of clinical cases and clinical studies performed for the period from 2001 to 2016, instill restrained optimism about the prospect of using drugs based on some artemisinin derivatives in oncology.
Pharmacy & Pharmacology. 2018;6(5):402-418
pages 402-418 views


Mardanly S.G., Pomazanov V.V., Kiseleva V.A., Neskorodov Y.B.


Both bee products themselves and their combinations are widely represented in the domestic pharmaceutical market, however, modern experimental studies of the biological activity of these compounds are few, and in many of the existing publications the authors describe an extremely wide and controversial range of therapeutic effects. The aim of the study is to analyze the experimental works on the study of biological activity of bee products. Materials and methods. The study was conducted using search and information (eLibrary, PubMed, CyberLeninka, ResearchGate) and library databases (Russian State Library, Central Scientific Agricultural Library). In the designated databases, publications were searched by such terms as “biological activity”, “royal jelly”, etc. The depth of the search was not limited. Results and discussion. The analysis of the published works shows that such substances as bee venom and royal jelly have experimentally confirmed their biological activity. In both cases, the active substances have been described and a review of their detected biological activity has been carried out. Conclusion. The authors suggest that when developing the method of laboratory synthesis of decene acids, it can be possible to carry out their large-scale preclinical research, which may become the basis for the creation of a drug with a selective effect.
Pharmacy & Pharmacology. 2018;6(5):419-439
pages 419-439 views


Orlova O.L., Nikolaeva L.L., Korol L.A., Dmitrieva M.V., Polozkova A.P., Lantsova A.V., Gulyakin I.D., Oborotova N.A.


Despite the development of biotherapy, chemotherapy remains one of the main methods of treatment of cancer patients. Currently, there are more than 100 anticancer drug substances, however, every year new drugs enter clinical practice and various therapeutic regimens are tested, expanding the possibilities of therapy and improving the results of treatment. Therefore, the adequate use of modern chemotherapy requires constant updating of information about anticancer drugs and methods of their use. Oral administration of drugs is the most natural and convenient way to introduce drugs into the human body. There are about 75% of orally administered drugs that have the ability to be absorbed in the gastrointestinal tract within 1−3 hours after administration. Oral dosage forms (DF) are most common due to the relative simplicity of their production, convenience of use, accuracy of dosing and high stability. Therefore, pharmaceutical companies often reproduce generics in the form of tablets and capsules for oral administration. However, most active pharmaceutical ingredient (API) are destroyed by the action of the gastrointestinal tract environment, which makes it impossible to use the oral administration. This review of the literature describes the main groups of anticancer drugs that are effective when taken orally. The aim of the study is to compile the information on the main groups of anticancer drugs used internally. Materials and methods. The object of the study was well-known anticancer drugs approved for oral administration. The study was conducted using search information and library databases (eLibrary, PubMed, CyberLeninka, ResearchGate), as well as State Register of Medicinal Remedies. Results and discussion. Analyzing the arsenal of cytotoxic drugs, it should be noted that antitumor substances are characterized by high chemical lability they are photosensitive, heat-labile, hygroscopic and hydrolytically unstable. These properties complicate both obtaining reproducible therapeutic effect when taken orally and technological inprocesses. In addition, anticancer drugs have mutagenic, teratogenic, sensitizing and allergenic effects. Conclusion. Lack of sufficient selectivity of the antitumor effect of cytotoxic drugs and a small breadth of pharmacological action require the use of DF, ensuring control of drug delivery to the body, including dosage accuracy and standard bioavailability. DF plays a very important role in the delivery of drugs to the lesion site. Capsules and coated tablets are necessarily created to avoid high toxicity of anticancer drugs and local tissue reactions when taken orally.
Pharmacy & Pharmacology. 2018;6(5):440-461
pages 440-461 views


Serebryanaya F.K., Zayer G.


The micromorphological investigations of Marrubium alysson L. growing on the territory of the Tunisian Republic have been conducted. The aim of the study was to conduct comparative ecological and morphological researches of Marrubium alysson aerian parts, to study an anatomical structure of caulifoliary system elements including stems, petioles, leaf margins a structure of the epidermis. Materials and methods. As an object of the research, dried-up herb and herbarium specimens of Marrubium alysson L., growing on the territory of the Tunisian Republic, were used. The micromorphological investigations were conducted by morphological and histochemical methods. Results and discussion. Comparative ecological and morphological researches have been conducted. The anatomic structure of the elements of the caulifoliary system including stems, petioles, leaf margins has been studied. The anatomic structure of the epidermis has been studied, too. The diacytic type of the stomatal apparatus, numerous branched trichomes with multicellular basis, located both on top and lower leaf parts have been found out. The conducted researches are a fragment of complex researches of perspective raw plants of Tunisian flora. Conclusion. Comparative eсological and micromorphological researches have been conducted, the anatomic structure of the stems, petioles, leaf margins, and also the epidermis structure of top and lower leaf parts has been also carried out. The diacytic type of the stomatal apparatus, trichomes with multicellular basis located both on top and lower leaf parts have been found out. The collenchyme is located in the subepidermal zone of a stem, petioles and in the zone of the central vein of a limb. The revealed signs can be included into product specification files on herbal raw materials
Pharmacy & Pharmacology. 2018;6(5):462-474
pages 462-474 views


Zhilyakova E.T., Tsvetkova Z.E., Pisarev D.I., Boyko N.N., Tymoshenko E.Y.


The aim. This article is devoted to the intensification of the production process of a thick extract of milk thistle fruits using ultrasonic processing of raw materials. Materials and methods. As an object of the study, the crushed milk thistle fruitss from Penza “Biokor” company were used. As the extractant, an aqueous solution of ethanol 70% vol. was used. For ultrasonic processing of plant materials and extractant, the installation “Bandelin SONOPULS HD 3200” was used, the ultrasound frequency was 20 kHz, the radiator power was 280 W, and the temperature was 25°С. The concentration of the extract was performed using a rotary evaporator RV-10 at the temperature of 60°C and a vacuum of 600–650 Mmhg to a residual moisture content of 25%. Qualitative and quantitative analysis of the thick extract was carried out using spectrophotometry and chromatography. Quantitative analysis of the amount of flavolignans was performed on an SF-56 spectrophotometer. The separation of the flavolignan complex and the quantification of silibinin was performed on a liquid chromatograph “Agilent Technologies 1200 Infinity”. Results and discussion. During the study it was found out, that processing of the crushed milk thistle fruits by ultrasound at the soaking stage almost doubles the output of the flavoligan complex from medicinal plant materials. The maximum amount of flavolignans is extracted when the fruits of milk thistle and extractant are processed with ultrasound at the frequency of 20 kHz for 5 minutes. Thus the obtained thick extract of milk thistle fruits in the component composition contains both the target flavolignan complex (87.39%, silibinin – 24.36%), providing the hepatoprotective effect, and flavonoids – chlorogenic acid (1.69%) and dihydroquercetin (10.92%) exhibiting antioxidant activity. It was established that, according to the qualitative composition of flavolignans, the obtained thick extract corresponds to preparations based on milk thistle. Thus, for the first time, the method was proposed for obtaining a thick extract of milk thistle fruits using ultrasonic processing of raw materials and extractant at the soaking stage. The obtained thick extract is proposed to be used as an active pharmaceutical substance for the production of granules based on methionine and milk thistle flavolignans. Conclusion. The results of the experiments allow us to recommend obtaining a thick extract of the milk thistle fruits, using the stage of ultrasonic processing of raw materials and extractant for 5 minutes at the ultrasound frequency of 20 kHz.
Pharmacy & Pharmacology. 2018;6(5):475-487
pages 475-487 views


Voronkov A.V., Lysenko A.S.


The main objective of the phenomenon of cerebral autoregulation is to maintain a constant cerebral blood flow rate with changes in systemic arterial pressure in the range of 50 mmH up to 150 Mmhg. To study this phenomenon, there are two approaches: dynamic and static. The dynamic approach is known to the study autoregulation, can indirectly characterize this phenomenon with the help of calculated indicators, and the described static methods can characterize only the lower limit of autoregulation of cerebral blood flow. The aim of the study was to develop a method for determining the value of pressure at the “breakdown” point of the upper limit of cerebral hemodynamics autoregulation. Materials and methods. The experiment was carried out on male rats of the Wistar line weighing 200–250 g, kept in standard vivarium conditions. The essence of the method of establishing the upper “breakdown” point of the autoregulatory mechanisms of cerebral circulation is pumping blood from the femoral artery to both carotid arteries by means of a peristaltic pump, while controlling the pressure and cerebral blood flow velocity. In order to avoid blood loss as a result of blood flow redistribution, external carotid arteries were ligated. The pressure was measured by the direct method. Since the pressure is created by the resistance of the cerebral vessels, it can be measured at the entrance by specially modeled carotid catheters. Cerebral blood flow velocity was measured by an ultrasound doppler scanner using MDK-Minimax Doppler v .2.1 program. To establish the possibility of using this method in the study of the influence of substances on the autoregulation of cerebral circulation, the effect of nicergoline on this phenomenon was studied. The drug was administered as a suspension intragastrally to rats 1 hour before metering. The results and discussion of the experiment showed that in intact rats the “breakdown” point of the upper limit of autoregulation was recorded at 165.0 ± 3.4 Mmhg (M ± m). Statistical processing of the obtained data indicates the normal distribution of the sample and the validity of the developed method. The introduction of nicergoline led to the increase in pressure at which there was a “breakdown” of the autoregulation mechanisms to 181.7 ± 4.7 Mmhg, which was significantly higher than the values of the intact group. Conclusion. As a result of the experiment on male rats, a valid method was developed for determining the blood pressure value at the highest point of “breakdown” of cerebral hemodynamics autoregulation and it was established that nicergoline shifts the functioning limit of the autoregulation phenomenon to higher values.
Pharmacy & Pharmacology. 2018;6(5):488-498
pages 488-498 views

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