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Vol 69, No 6 (2020)
- Year: 2020
- Articles: 9
- URL: https://journals.eco-vector.com/0367-3014/issue/view/5779
Articles
The uncertainty principle in biology and medicine
Abstract
Drugs based on biomacromolecules have emerged in recent decades. The macromolecules differ from small molecules in their effect on the body. Cytokines, including interferons and chemokines, as well as enzymes, glucans, and antibodies, have been established to have multiple binding sites on the same macromolecule with appropriate complementary structures in biological systems. The properties of cytokine pleiotropy and redundancy, which are determined by the nature of cytokine networks, determine different functional effects, i.e. cytokines can have more than one effect on the same cell. The same pattern has been found when studying the effects of interferons. There is ample evidence that the presence of several protein allosteric sites motivates the design of allosteric modulators of protein activity with their potentially higher specificity and lower toxicity than conventional orthosteric compounds. That is to say that any macromolecule has a potential probabilistic set of mechanisms of action. The use of macromolecules as drugs can trigger one or another specific mechanism of their action from the many potentially existing ones. Because of this, high-molecular-weight drugs, unlike low-molecular-weight pharmaceutical compounds, should have apparently their own characteristics when passing through regulatory organs.
Farmaciya (Pharmacy). 2020;69(6):5-7
5-7
Farnesol: properties, role, and prospects for use in the regulation of film formation in fungi of the genus Candida
Abstract
The paper describes the nature of farnesol, a secondary metabolite of isoprene substances, and its role as a QS-molecule in fungal intra- and interspecific chemocommunication. It discusses chemosignaling systems that regulate fundamental cellular processes, in which farnesol is involved. The authors analyze and systemize data on the use of farnesol in combination with antimycotic drugs against biofilms of yeast-like fungi of the genus Candida spp.
Farmaciya (Pharmacy). 2020;69(6):8-12
8-12
The chemical and toxicological properties of nonsteroidal anti-inflammatory drugs and methods for their determination
Abstract
Nonsteroidal anti-inflammatory drugs (NSAIDs) are a group of widely used analgesic, antipyretic, and anti-inflammatory agents in the world, with most of them sold over the counter. In this connection, there is a danger of poisoning from a drug overdose or systematic intake, which can proceed without obvious symptoms. Severe poisonings are characterized by metabolic acidosis, convulsions, coma, acute renal failure, etc. The facts of using the drugs in this group for non-medical purposes make up special cases. NSAIDs vary in chemical structure and therefore differ from each other in the strength and characteristics of action, the frequency and manifestations of side effects. The modification or introduction of new functional groups into medications leads to a decrease or increase in side effects: a positive relationship has been established between lipophilic, brominated compounds and cytotoxicity, while fluorination of the compounds in this group reduces the risk of undesirable effects. To minimize the systemic effect, various dosage forms (cream, gel, and foam for the skin) are brought to the pharmaceutical market. The paper describes modern techniques to identify and quantify the drugs of this group in various biological objects during chemical and toxicological analysis and discusses the possibility of using current methods to establish the fact of using NSAIDs, including those for non-medical purposes. Determination of biomarkers using proteomic technology for the early diagnosis of pathological changes in the systematic administration of NSAIDs is a promising diagnostic area. The structural foundations of the drugs and their classification are presented.
Farmaciya (Pharmacy). 2020;69(6):13-19
13-19
Elaboration of approaches to standardizing Emerson’s thorn (Crataegus submollis) fruits
Abstract
Introduction. The fruits of 12 hawthorn species are currently allowed for the production of drugs used to treat cardiovascular diseases, but not all of them grow widely in the Russian Federation. At the same time, the fruits of Emerson's thorn (Crataegus submollis Sarg.) that is a widely cultivated North American species are widely used in the food industry, but unused in medical practice. Flavonoids are the leading group of active ingredients in Emerson's thorn fruits. Objective: to develop a procedure for the quantitative determination of the total flavonoid content in Emerson's thorn fruits. Materials and methods. The object of the investigation was Emerson's thorn fruits plucked in the Samara Region in the fall of 2018. Aqueous alcoholic extracts from their raw materials were studied using UV spectrophotometry. Results. A procedure was developed for the quantitative determination of total flavonoid content in Emerson's thorn fruits by direct spectrophotometry using the state standard sample (SSS) of catechin at an analytical wavelength of 282 nm. The error of a single determination with a 95% confidence level was ±4.44%. Conclusion. The developed procedure was used to determine the total flavonoid content calculated with reference to catechin in Emerson's thorn fruits, which ranged from 4.17% to 5.35%.
Farmaciya (Pharmacy). 2020;69(6):20-24
20-24
Development of a procedure for standardization of the Rozmatin substance from Moldavian dragonhead (Dracocephalum moldavice) herb
Abstract
Moldavian dragonhead (Dracocephalum moldavica) is an annual herbaceous plant that is widely cultivated in Eastern and Central Europe as an essential oil-bearing, melliferous, and spicy-and-aromatic plant. The All-Russian Research Institute of Medicinal and Aromatic Plants has developed a technology for obtaining a dry purified Moldavian dragonhead herb extract arbitrarily called Rozmatin that contains flavonoids and phenylpropanoids. The substance has a tonic effect on the cardiovascular and nervous systems, as well as an anti-inflammatory effect. Objective: to develop a procedure for standardizing the Rozmatin substance and to make its validation assessment. Material and methods. The Rozmatin substance obtained from the aboveground part of the Moldavian dragonhead (the variety «Tenderness») growing in the All-Russian Research Institute of Medicinal and Aromatic Plants, which was harvested during the flowering phase. The investigators used the following techniques: thin layer chromatography (TLC), UV spectrophotometry, as well as the equipment: 10x15-cm Sorbfil ПТСХ-ПА plates (Russia) and UV-1800 (Shimadzu) and Cary 100 Scan (Varian) spectrophotometers. Results. The presence of flavonoids in the substance was confirmed by the cyanidin test (Shinoda's test) (a pink and red color). The UV spectrum of Rozmatin showed two absorption maxima at 327±2 and 288±2 nm in the wavelength range of 250 to 400 nm. The total phenolic compound content in the Rozmatin substance in terms of rosmarinic acid, which was determined using direct spectrophotometry, ranged from 60.67 to 88.02% in 5 series of balanced loads. Conclusion. Procedures have been developed for the qualitative and quantitative determination of phenolic compounds in the Rozmatin substance. The procedure for the quantitative determination of the total content phenolic compounds calculated with reference to rosmarinic acid meets all validation criteria.
Farmaciya (Pharmacy). 2020;69(6):25-30
25-30
The amino acid composition of knotweeds (Polygonum) of the series Amphibiae Kom
Abstract
Introduction. The genus Polygonum (Persicaria Mill.) that belongs to the buckwheat family (Polygonaceae Juss.) is represented by a wide variety of species and types - from xerophytes to hydrophytes. The plant is widespread throughout Russia. Polygonum amphibium is a perennial herbaceous plant of the genus Polygonum. There are two known types: aquatic (P. amphibia (L.) Gray) and terrestrial (P. amphibia var. terrestris Delarbre) plants. According to the scientific literature, the aqueous plant has an antimicrobial effect and contains large amounts of phenolic compounds. There is insufficient information on the chemical composition of the terrestrial plant and the characteristics of its use in medicine. The composition of plant amino acids has not been investigated. Objective: to comparatively investigate the amino acid composition of two types of Polygonum amphibium (aquatic and terrestrial plants) stored in the Voronezh Region. Material and methods. The investigation objects were the dried samples of two types of Polygonum amphibium, which were stored in the coastal zone of the Voronezh River in the Voronezh Region in 2017. Free amino acids (AAs) were qualitatively analyzed by thin-layer chromatography (TLC) in the butanol : acetic acid : water (4 : 1 : 2) system; the detection reagent was a 0.2% alcoholic ninhydrin solution. The amount of free AAs was quantified by spectrophotometry by the ninhydrin reaction at an analytical maximum of 568 nm. The overall composition of AAs was determined by capillary electrophoresis. Results. Individual components were identified in the investigated types of Polygonum amphibium and differences were revealed in the profile of free AAs. Capillary electrophoresis could show that all the objects contained 17 AAs, of them 7 AAs were essential. Each sample exhibited AAs that were dominant in the composition of biologically active substances in the raw materials. The amount of free AAs in the aquatic type of Polygonum amphibium was found to account for 0.66%, which was 12% less than that in its terrestrial type. Conclusion. The composition of AAs in the investigated types of Polygonum amphibium indicates that the knotweed can be an additional source of AAs. The results of the investigation may be used when assessing the identity and high-quality of the weed of Polygonum amphibium.
Farmaciya (Pharmacy). 2020;69(6):31-37
31-37
Regulatory aspects of preclinical and clinical trials of drugs
Abstract
Since 2014, the registration dossier in the Russian Federation has been submitted as a general technical document in accordance with the ICH requirements. The recognition of nonclinical and clinical trials conducted according to a single accepted standard in other countries leads to a considerable reduction in the time to market for a new drug. There have been comparative studies of the regulatory requirements for submitting the results of preclinical and clinical trials of drugs to the registration dossier in the United States (US), the European Union (EU), and the Russian Federation (RF). Main differences have been found in terms, requirements for the preparation and execution of documents of the results of nonclinical and clinical trials to the regulatory authorities in the USA, EU, and RF for marketing authorization or registration. A comparative analysis of the requirements for the registration and submission of documents as part of the registration dossier has shown that at the moment the main norms that govern non-clinical and clinical trials in Russia are harmonized with world practice. The main difficulty is the lack of worldwide recognition of the results of studies conducted in Russia. This is due to the fact that Russian laboratories are not accredited for compliance with international requirements. Harmonizing clinical research requirements is the most labor-intensive work. The international organizations WHO and ICH create a regulatory framework for the functioning of a single space for nonclinical and clinical trials.
Farmaciya (Pharmacy). 2020;69(6):38-45
38-45
Problems of the segment of medicines for children in pharmacy organizations
Abstract
In the daily clinical practice of a pediatrician, in order to increase the efficiency and safety of pharmacotherapy, the use of drugs should take into account and study the individual characteristics of the child's body and in accordance with the requirements of typical clinical and pharmacological characteristics. There is a problem with the production of drugs for low birth weight infants, as well as a problem of prescribing drugs, which have not been sufficiently investigated. There is very little data on the safety of medicine use in children and insufficient specific pediatric formulations. Objective: to study the problems of the segment of medicines for children in pharmacy organizations. Material and methods. The investigators used a set of methods: system analysis, marketing analysis of assortments, sociological survey. Results. At the moment, it is necessary to note a lack of knowledge regarding the characteristics of pediatric medicines, their relationship to the physiology of a child, and regarding adequate doses and formulations, etc. There are a number of restrictions on the manufacture of prescription drugs for children in pharmacies. The Russian industry practically does not produce children's dosage forms, whereas drugs made in foreign countries are not registered in the Russian Federation. Conclusion. The priority tasks in improving the manufacture of pediatric formulations are to conduct adequate clinical trials of drugs with the participation of children and to design special dosage forms for use in pediatrics, which will be able to register effective and safe drugs in the pediatric population in the future.
Farmaciya (Pharmacy). 2020;69(6):46-50
46-50
Features of the body distribution of ceftriaxone in warm-blooded animals
Abstract
Introduction. Ceftriaxone is a yellowish-white crystalline powder, is hygroscopic and readily soluble in water. It is a third-generation antibiotic with a broad spectrum of action. Objective: to study of the body distribution of ceftriaxone in warm-blooded animals when it is given at lethal doses. Material and methods. The distribution of the substance in free form or included in the erythrocyte carriers was studied in the groups of healthy mice and those with simulated toxic kidney damage caused by HgCl2. Isolation was carried out with an acetone-water mixture of 5:5 at a mass ratio of the insulating mixture and the biological object (2:1). The investigators used thin-layer chromatography, ultraviolet spectrophotometry, and high performance liquid chromatography for the identification of ceftriaxone and UV spectrophotometry for its quantitative determination. Results. Ceftriaxone was found in large quantities in the visceral organs and blood of poisonous organisms. Ceftriaxone intravenously injected in free form to healthy animals was present in the highest amounts in the bladder with urine (2718.93 mg/100 g), whereas it was also seen in the blood (523.02 mg/100 mg) and urinary bladder (571.10 mg/100 mg) of animals with simulated toxic kidney damage caused by HgCl2. When ceftriaxone included into the erythrocyte carriers was intravenously injected to the healthy mice, the maximum concentration of the drug was observed in the blood (937.57 mg/100 g) and urinary bladder (1184.59 mg/100 g). When erythrocyte carriers with ceftriaxone were administered to the group of mice with simulated renal toxicity induced by HgCl2, there were changes in the distribution of the test antibiotic. The peak concentration was observed in the kidneys (668.61 mg/100 g) and blood (663.41 mg/100 g). Conclusion. The results of the investigations make it possible to imagine differences in the nature of ceftriaxone distribution in the warm-blooded animals in health and in simulated renal disease when the antibiotic was intravenously injected as a substance or part of erythrocyte carriers.
Farmaciya (Pharmacy). 2020;69(6):51-56
51-56