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Vol 70, No 4 (2021)

Articles

Analysis of the need for narcotic drugs as a factor of their availability for medical use

Krasnopeeva I.V., Barankina T.A., Yakimenko O.N., Nozdrachev K.G., Barankina N.B.

Abstract

To improve the mechanisms of state drug trafficking regulation, certain changes in Russian legislation are required not only to simplify the process of drug trafficking and to decriminalize the actions of medical and pharmaceutical workers, but also to introduce current approaches to treating pain syndrome into medical practice, to expand the range of narcotic drugs and to optimize their need calculation. The stated need for narcotic drugs placed under international control in several countries was studied; priorities were identified in the range of legal narcotic analgesics, and their availability was explored in different regions of the world, including in Russia.
Farmaciya (Pharmacy). 2021;70(4):5-10
pages 5-10 views

Treatment for multiple myeloma: pharmacoeconomic aspects

Zabolotneva Y.A., Gurevich K.G., Zaborovsky A.V., Tararina L.A.

Abstract

To date, the choice of treatment policy for patients with multiple myeloma (MM) is based primarily on factors, such as age and concomitant diseases. The widespread use and clinical application of cytogenetic techniques (karyotyping and fluorescence in situ hybridization (FISH)) has made it possible to identify and use cytogenetic abnormalities as prognostic biomarkers to assess key parameters, such as progression-free survival (PFS) and overall survival (OS), in patients with MM. Chromosomal abnormalities enable the identification of patients with a poor prognosis (high-risk myeloma) who have the lowest prognostic survival. Despite the clarification of the main mutations that cause a poor prognosis for survival in patients with myeloma, the question of choosing the most optimal therapy regimen to increase survival is still relevant. However, the optimal treatment has not been developed for patients with MM with high-risk cytogenetics at the time of diagnosis. With allowance made for the steadily increasing costs of managing MM patients, there is a need for their optimization just at the stage of choosing first-line therapy. The FISH assay may serve as the most rational approach to identifyng high-risk chromosomal abnormalities and to prescribing triplet therapy with new agents for these patients. The review provides brief information about the main chromosomal rearrangements occurring in MM ad their prognostic value and considers the pharmacoeconomic aspects of the treatment of patients with myeloma.
Farmaciya (Pharmacy). 2021;70(4):11-19
pages 11-19 views

The amino acid composition of the herb of some Astragalus L. species

Matvienko U.A., Durnova N.A., Karavaeva L.V., Romanteeva Y.V.

Abstract

Introduction. The genus Astragalus L. belonging to the legume (Fabaceae) family is represented by a wide variety of life forms and has about 3000 species. Saponins, flavonoids, and polysaccharides are the main biologically active substances (BASs) of plants of the genus Astragalus. Among the related compounds, amino acids (AAs) that are widely distributed in nature and participate in the regulation of different life processes in plants and animals are of interest. The search for new promising sources of AAs generates scientific interest and has practical significance in expanding the range of officinal medicinal plant raw materials. From this point of view, it is relevant to investigate the amino acid composition of Astragalus herb and to quantify this group of BASs in the examined samples. Objective: to comparatively study the amino acid composition of five Astragalus species growing in the Saratov Region Material and methods. The investigation objects were the herb samples of Astragalus henningii (Stev.) Klok., Astragalus varius S.G. Gmel., Astragalus testiculatus Pall., Astragalus dasyanthus Pall., and Astragalus zingeri Korsh., which had been collected in the Saratov Region in 2020-2021. Qualitative analysis was carried out using thin-layer chemical chromatography (TLC) in the n-butanol - glacial acetic acid - water (35:35:10:20) system. The reagent for detection was a 2% ninhydrin ethanol solution. The amount of free AAs was measured by a spectrophotometric method on a SHIMADZU UV-1800 spectrophotometer (Japan) at an analytical wavelength of 568 nm. Results. TLC was used to determine the amino acid composition of the aqueous extracts of the herb of the examined Astragalus species. Asparagine and proline were detected in all the samples analyzed. Nine amino acids, eight of which were significantly identified as arginine, asparagine, proline, glutamic acid, threonine, valine, methionine, and phenylalanine, were first found in the extracts from the herb of Astragalus henningii (Stev.) Klok., Astragalus varius S.G. Gmel., and Astragalus testiculatus Pall. The highest content of AAs was established to be in the aqueous extract from the herb of Astragalus henningii (Stev.) Klok. (5.50%) and Astragalus testiculatus Pall. (5.23%) and the lowest one was in Astragalus zingeri Korsh. (1.67%). Conclusion. The composition and quantification of the content of AAs in the examined samples show that the herb of these plants along with other BASs may be a promising source of AAs. The findings of this investigation can be used when assessing the identity and high quality of the herb of the Astragalus species analyzed.
Farmaciya (Pharmacy). 2021;70(4):20-25
pages 20-25 views

Chemical composition and anatomical study of Spanish cockle (Vaccaria hispanica)

Darmogray S.V., Erofeeva N.S., Darmogray V.N., Ostrikova T.O., Morozova V.A., Darmogray N.F., Lizunova A.S.

Abstract

Introduction. Spanish cockle (Vaccaria hispanica (Miller.) Rauschert.) is a widespread, annual, monotypic species. It is found in all regions of Central Russia as a weed, in crops, and is also often grown as an ornamental plant. It is used in folk medicine in Central Asia and China. The plant contains triterpene saponins, flavonoids, and phenol carboxylic acids in its different parts. Presumably, the plant may contain ecdysons. Objective: to investigate the anatomical structure of Spanish cockle leaves and flower and to analyze the biologically active compounds of the plant, by using the current techniques (HPLC). Material and methods. The Spanish cockle herb collected near the settlement of Golenchino, Ryazan Region, served as an investigation object. The test compounds were analyzed by HPLC on a Gilson 305 chromatograph with a UV detector (France). Results. HPLC proved that ecdysteroids (ecdysterone, polypodin B) and polyphenolic compounds (vicenin, caffeic, gallic, chicory, ferulic acids, epicatechin, epigallacatechingallate) were present in the aboveground part of the plant. Conclusion. Spanish cockle herb contains biologically active and highly effective chemical compounds that are of great importance for chemotaxonomy. The object deserves more research for the possible production of drugs; therefore it is necessary to develop methods for cultivating the species in order to obtain medicinal raw materials of the examined plant.
Farmaciya (Pharmacy). 2021;70(4):26-31
pages 26-31 views

Features and analysis of the current problems with the use of NSAIDs in the Arab countries

Alhodri A., Ibragimova A.N., Suslina S.N.

Abstract

Musculoskeletal system diseases affect not only the elderly, but also the young who belong to the economically active population. These diseases are almost always accompanied by pain and limited mobility, which negatively affects quality of life and its expectancy, including those in Arab countries. Among the musculoskeletal system diseases, rheumatoid arthritis is widespread among low- and middle-income groups, especially among those with lower socioeconomic status. Nonsteroidal anti-inflammatory drugs (NSAIDs) are the mainstay of treatment for musculoskeletal diseases in the Arab countries. Elderly people (over 65 years old) take NSAIDs almost daily. At the same time, many patients do not have complete information about the drugs, their adverse reactions, interaction with other groups of drugs, and they do not know or cannot calculate the correct dosage of drugs and the frequency of their administration. Today, the main problems with the use of NSAIDs are associated with lack of patients' awareness of their adverse reactions, drug interactions, and the possibility of further pharmacocorrection. The identified problems with the use of NSAIDs in the Arab countries suggest that selective anti-inflammatory drugs should be designed for systemic administration. They are characterized as drugs with the lowest spectrum of adverse reactions, the low frequency of administration and, as a result, can be recommended for patients with certain concomitant diseases, for example, those in the gastrointestinal tract, cardiovascular system, etc.
Farmaciya (Pharmacy). 2021;70(4):32-36
pages 32-36 views

Financial results of Saint Petersburg pharmaceutical cluster companies’ activities

Trofimova E.O., Yasinskaya L.E.

Abstract

Introduction. In recent years, Saint Petersburg pharmaceutical companies have surpassed the overall production dynamics of manufacturing and all industries in Saint Petersburg in terms of production growth rates. They have been also included in the group of leading industries by investment and innovation activities and the level of labor remuneration. The Saint Petersburg pharmaceutical companies are beneficiaries of state programs for the development of pharmaceutical and all industries and are residents of the special economic zone and use preferences provided to investors at the regional level. Objective: to provide a marketing and financial assessment of the results of activities of the Saint Petersburg pharmaceutical cluster companies in the period 2015-2019. Material and methods. The marketing analysis was based on the IQVIA research company data on sales in the Russian pharmaceutical market. The financial analysis was based on the SPARK-Interfax database. The sample included 14 drug manufacturers with a total revenue of more than 500 million rubles in 2019. Results. In 2015 to 2019, the Saint Petersburg pharmaceutical companies dynamically improved their positions in the domestic market and amounted to as much as 25% of the total sales volume of Russian companies in the public procurement segment and 12% in the pharmacy segment. In the total sales structure in the companies, the deliveries for state needs and commercial sales accounted for 60% and 40%, respectively. In 2015 to 2019, the operating profit of the Saint Petersburg companies showed the high growth rates that exceeded the trends in the overall indicators of the Saint Petersburg industry. Despite a substantial increase in the currency component of costs and a regulatory pressure on prices, the average operating income margin of the companies remained at a high level (38%). In response to a high investment activity, there was a dynamic original capital growth. Despite the attraction of considerable amounts of debt funding for investment purposes, the share of equity capital consistently accounts for more than 50% of the total capital structure of the companies. Conclusion. The representatives of the Saint Petersburg pharmaceutical cluster are characterized by strong positions in the domestic market, high business performance indicators, an optimal asset structure, and significant amounts of equity capital. The companies have substantial resources to continue investments in the development of production and product portfolios.
Farmaciya (Pharmacy). 2021;70(4):37-43
pages 37-43 views

Evaluation of the anti-inflammatory activity of a new 1,6-dihydropyrimidine derivative

Kuvaeva E.V., Kolesnik D.A., Levshukova P.O., Kirillova E.N., Ivkin D.Y.

Abstract

Introduction. Compounds based on the 1,3-diazine cycle have different types of biological activity. Many of them have shown themselves to good advantage in the pharmaceutical market as effective and safe medicines. The production of new compounds based on the pyrimidine core and the study of their biological activity are an urgent area. Objective: to evaluate the in silico and in vivo acute toxicity and anti-inflammatory activity of 5-butyl-1,2-diphenyl-6-oxo-1,6-dihydropyrimidine-4-sodium olate. Material and methods. The acute toxicity of the test compound was predicted using the local version of the GUSAR software. In vivo acute toxicity was determined in outbred male albino mice. Computer-aided screening of biological activity was performed using the PASS program located on a web service that was freely available via the Internet. Two models (a murine formalin-induced paw edema model and a rat cotton pellet-induced granuloma model) were included in the study to experimentally evaluate anti-inflammatory activity. Results. Predicted and experimental data on acute toxicity correlate with each other. The test compound belongs to the class of practically non-toxic ones. Biological activity screening with the PASS program yielded data on putative anti-inflammatory activity. Studies of in vivo anti-inflammatory activity showed that 5-butyl-1,2-diphenyl-6-oxo-1,6-dihydropyrimidine-4-sodium olate had a pronounced anti-inflammatory activity. Conclusion. The results of computer simulation could determine the acute toxicity of the new 5-butyl-1,2-diphenyl-6-oxo-1,6-dihydropyrimidine-4-sodium olate and identify its potential biological activity. It has been experimentally proven that the test compound has low toxicity and exhibits a pronounced anti-inflammatory activity.
Farmaciya (Pharmacy). 2021;70(4):44-47
pages 44-47 views

Investigation of the pharmacokinetics of an original drug for the treatment of HIV-1 infection

Kosman V.M., Demchenko D.V., Jain E.A., Makarov V.G., Balabaniyan V.Y.

Abstract

Introduction. HIV-1 infections have been proposed to be treated with the original drug 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil as tablets. The necessary stage of preclinical trials of the original drug is to investigate its pharmacokinetics. Objective: to evaluate the pharmacokinetics of the drug based on the benzophenone derivative of pyrimidine for the treatment of HIV-1 infection in two animal species. Material and methods. The investigation was conducted with sexually mature male rats and rabbits after single intragastric administration (in rats), oral administration as three doses (in rabbits), and multiple administration as two doses to the rats. The concentrations of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil in plasma, tissues, organs, and feces were determined by high-performance liquid chromatography (HPLC) coupled with ultraviolet (UV) detection. The pharmacokinetic parameters were calculated by the extramodel method of statistical moments. Results. The authors’ previously developed procedure for the quantitative determination of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil in rabbit plasma is adapted for the analysis of rat plasma, tissues and organs (for example, the liver). It was found that the pharmacokinetics of the test drug was nonlinear in the dose range of 20-100 mg/kg for rats and 10-50 mg/kg for rabbits. The time to maximum concentration (Tmax) was about 5-6 h; the mean retention time (MRT) was about 30-50 h for rats and about 16-17 h for rabbits; the half-life (T1/2) was about 31-36 h for rats and about 11-13 h for rabbits. Comparison of the data obtained for two biological species (rats and rabbits) revealed the higher values of a number of pharmacokinetic parameters (Cmax and AUC0-48, MRT and T1/2 ) for rats, which could indicate the species-specific pharmacokinetics of the test drug. Repeated administration of the drug at the doses of 60 and 100 mg/kg to the rats for 3 days did not result in the accumulation of an active ingredient. The active ingredient was distributed to the highly vascularized organs responsible for excretion, such as the liver and kidneys. The supply of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil to the heart and spleen, as well as the ability of the analyzed compound to penetrate the blood-brain barrier and to enter the brain have not been established. About 9% of the active ingredient was excreted unchanged in the feces; no analyte was detected in the urine. Conclusion. Pharmacokinetic parameters of original drug were evaluated. The procedures are validated in accordance with the present-day requirements.
Farmaciya (Pharmacy). 2021;70(4):48-56
pages 48-56 views

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