![开放存取](https://journals.eco-vector.com/lib/pkp/templates/images/icons/text_open.png)
![受限制的访问](https://journals.eco-vector.com/lib/pkp/templates/images/icons/text_unlock.png)
![受限制的访问](https://journals.eco-vector.com/lib/pkp/templates/images/icons/text_lock.png)
卷 26, 编号 12 (2023)
- 年: 2023
- 文章: 9
- URL: https://journals.eco-vector.com/1560-9596/issue/view/8372
- DOI: https://doi.org/10.29296/25877313-2023-12
Pharmaceutical chemistry
Carotenoids and chlorophylls when present together: analytical and technological features
摘要
Relevance.An analytical approach to choosing the direction of technological research has always been relevant, and taking into account the production of drugs using “green” extractants, the justification of technological parameters of extraction and its analytical support on models of already known, widely studied and used plant objects, for example, stinging nettle (Urtica dioica L.), can be considered as rational.
The purpose of the study is an analytical study of carotenoids and chlorophylls in the co-presence of stinging nettle leaves and the rationale for the temperature regime for obtaining an oil extract from this plant, taking into account the co-presence of pigments in the extracts.
Material and methods. The content of carotenoids and chlorophylls in raw materials and oil extracts was determined by spectrophotometry. Oil extracts were obtained by fractional maceration at two temperature conditions: 25 °C and 50 °C.
Results. The content of carotenoids and chlorophylls when jointly present in stinging nettle leaves was determined by spectrophotometry. When obtaining six model oil extracts of stinging nettle leaves, the temperature regime was experimentally optimized at 50 °C; the optimization parameter was the quantitative content of carotenoids and chlorophylls.
Conclusion. A detailed determination of the content of chlorophyll a, chlorophyll b, their sum and carotenoids in the presence of chlorophylls gives a detailed idea of the quantitative ratio of these types of pigments in the raw material and makes it possible to eliminate the overlap of absorption bands of carotenoids and chlorophylls. This approach made it possible to optimize the temperature conditions for obtaining the oil extract of nettle leaves. The applied analytical approach can be used to control the content of carotenoids and chlorophylls when present together to optimize the technological parameters of oil extracts obtained from other types of medicinal plant raw materials.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Methodology of specific enzyme biotest-systems in vitro application in herbal medicines complex laboratory quality control system
摘要
Relevance. Improving methods for quality control of medicines, including those of plant origin, is one of the urgent tasks of modern pharmaceutical science and practice. The growing interest in herbal medicine stimulates not only the expansion of the diversity of raw materials and the development of new drugs, but also the constant improvement of approaches and methods for controlling their quality.
The purpose of the study is to develop a methodology for the use of specific in vitro enzyme biotest systems (IBTS) in complex laboratory quality control of herbal medicines for additional assessment of their biological activity, which determines therapeutic effectiveness, in addition to physical, physicochemical, and chemical indicators.
Material and methods. We used in silico (PASS), in vitro (specific enzyme biotest systems) and in vivo (experimental models) methods.
Results. A method has been developed for the use of specific in vitro enzyme biotest systems (IBTS) in complex laboratory quality control of medicines, as well as methods of physical, physico-chemical, and chemical analysis to assess their biological properties, which determine the therapeutic effectiveness of medicines.
Conclusions. Specific enzyme biotest systems make it possible to identify the specific biological activity of research objects and confirm the feasibility of their use in an in vitro quality control system for herbal medicines at different stages of their life cycle, as demonstrated by the example of extracts from native and biotechnological raw materials, as well as experimental dosage forms, developed at FGBNU VILAR, and comparison drugs.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Proposal of the method for quantitative determination of proteolytic activity of a pancreatin reference standard
摘要
Relevance. Pancreatin is a polyenzyme drug with lipolytic, amylolytic and proteolytic activity, and is prescribed as a replacement therapy for exocrine pancreatic insufficiency. Modern requirements for quality control of drugs involve the use of highly specific and highly sensitive methods of analysis using reference standards (RS).For RS certification it is necessary to establish the values of the certifiable characteristic. For enzyme preparations the certifiable characteristic is catalytic activity. In this connection for certification of pancreatin RS it is necessary to establish the value of its catalytic activity.The analysis of the proteolytic activity of pancreatin consists in performing a proteolysis reaction and quantifying the reaction products. The most common methods used for this purpose are those in which the quantitative content of proteolysis products is determined by measuring the optical density of the solution using tyrosine as a standard. It should be noted that the value of proteolytic activity established in this way is relative, since the measured optical density actually corresponds to a mixture of tyrosine and tryptophan. The absolute method for determining proteolytic activity is the Kjeldahl method for analyzing fragmented peptide nitrogen.
Aim. Propose the method for quantitative determination of the proteolytic activity of a pancreatin RS.
Material and methods. The object of the study was a pharmaceutical substance pancreatin. Quantitative determination of proteolytic activity in pancreatin substance samples was performed according to the proposed method by determining protein nitrogen by the Kjeldahl method after the enzymatic reaction.
Results. As a result of testing the samples of pancreatin substance using the proposed method of quantitative analysis of proteolytic activity, we obtained reliable results, indicating the high sensitivity, accuracy and reliability of this method.
Conclusions. The present study proposed the method for quantitative determination of the proteolytic activity of pancreatin substance and evaluated the acceptability of its use in the quality control of a pancreatin RS.
Conflict of interest. The authors declare that they have no obvious and potential conflicts of interest related to the publication of this article.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Development of approaches to the analysis of elemental impurities in titanium dioxide (antimony definition)
摘要
Reltvance. Due to its properties, substance of titanium dioxide is still widely used in the pharmaceutical industry as a drug excipient. However, from the point of view of the safe use of any component of drugs, one of the most important factors is the determination of its content of elemental impurities (PE). The pharmacopoeic requirements for titanium dioxide to contain elemental impurities are not harmonized today. It was therefore advisable to develop approaches to defining them under the strictest of standards.
Research objective. This work is devoted to the development of approaches to the analysis and further validation of the method of determination of antimony in the substance titanium dioxide at the level of 2 ppm.
Material and Methods. The method used in this paper is based on the extraction into the organic phase of ionic associates, in which the halogen complex SbCl6-antimony acts as an anion and interacts with the triphenylmethane dye - diamond green. All the reagents and materials used were pharmacopoeic. A sample of titanium dioxide, produced by Venator Germany GmbH, Germany, was used as the research object. The validation of the methodology was carried out in accordance with the requirements of the SP RF on the following characteristics: specificity, linearity, LOQ, correctness, repeatability, intralaboratory precision and range of methods.
Results. The article shows applicability of the method of determination of antimony in the substance titanium dioxide, at the level of 2 ppm, using as a reagent diamond green. At the same time, the validation evaluation of the methodology showed that the obtained results met the criteria of acceptability for all the studied characteristics.
Conclusions. Control of PE is an important aspect of the safe use of any component of the drug.
Due to the wide variety of pharmacopeic requirements for PE content in the substance TiO2, this study shows the possibility of using the extraction and photometric method with the use of a triphenylmethane dye (diamond green) to determine Sb at the most stringent standards (2 ppm).
At the same time, the validation of the methodology on such characteristics as specificity, linearity, LOQ, correctness, repeatability, intralaboratory precision and range confirmed the possibility of quantitative estimation of Sb content in the substance TiO2 in the range of 50% (LOQ) up to 150% of the specification level.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Development of quality indicators of trichoderma atrobrunneum culture fluid extract vkpm f-1434
摘要
Relevance. It is relevant to solve the problems of quality control of medicinal substances, drugs, preparations by conducting pharmaceutical analysis.
The purpose of the study – determination of physico-chemical and biological properties of Trichoderma atrobrunneum VKPM F-1434 culture fluid extract. Development of a method for determining the mass concentration of culture fluid extract T. atrobrunneum VKPM F-1434 in bioproducts.
Material and methods. The strain Trichoderma atrobrunneum VKPM F-1434 synthesizing low molecular weight biologically active compounds with bacteriostatic effect was used in the work. The extract was obtained by single-stage mixing and settling extraction with ethyl acetate from the culture liquid of T. atrobrunneum VKPM F-1434 after 5 days of deep cultivation at a temperature of 28 ° C, the seed material was the vegetative mycelium of the producer in the late exponential growth phase. The mass concentration of
T. atrobrunneum VKPM F-1434 culture fluid extract was determined in a healing liniment for wound healing.
Results. Based on the study of physico-chemical and biological properties of culture fluid extract T. atrobrunneum VKPM F-1434, its individual characteristics have been established. The method "Determination of the mass concentration of culture fluid extract T. atrobrunneum VKPM F-1434 in the finished bioproduct" has been developed. Scope of the method: determination of the extract’s mass concentration at the stages of the technological process of preparation, as well as in ready-made dosage forms, therapeutic and preventive orientation of zootechnical and veterinary purposes. Characteristic of the method: the range of determined values – mass concentrtion (ω): 1 – 10%; repeatability: CV = 1.69%; reproducibility CV1 = 1.68%; CV2 = 1.78%; Fr = 1.09; Ft = 3.44; correctness:
R = 100.1%.
Conclusions. Physico-chemical and biological properties of culture fluid extract T. atrobrunneum VKPM F-1434 can be used to establish its authenticity and quality assessment. The method of determining the mass concentration of culture fluid extract T. atrobrunneum VKPM F-1434 can be considered suitable for a reliable assessment of the composition of the finished bioproduct.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Development of compositions and technology of gels containing phytoextracts
摘要
Relevance. Today, interest in the use of natural medicinal substances, medicinal products created on their basis and corresponding dosage forms continues to develop. This interest is associated with the unique properties of various phytocompositions, as well as with the intensive development of such classical sciences as biology, chemistry, and pharmacology. An urgent task is the development and introduction into production of original domestic dosage forms for external use, created on the basis of medicinal plant raw materials, which will solve the issues of successful pharmacotherapy for a number of diseases.
The purpose of our research is to develop optimal compositions of gels based on Ginkgo biloba leaves and Rhodiola rosea rhizomes with roots of thick extracts, their biopharmaceutical studies in vitro for subsequent more in-depth pharmacotechnological studies. Material and methods. The object of our research is soft dosage forms developed on the basis of thick extracts of Ginkgo biloba leaves and Rhodiola rosea rhizomes with roots. Thick extracts were obtained by condensation in a rotary vacuum evaporator), into which the extracts and an alcohol-water-glycerin mixture 1:6:3 were placed. The ratio of thick extract and solvent mixture was 1:1. Mixing was carried out with a stirrer rotating no more than 30 rpm at room temperature until the mass was completely homogenized. The release of biologically active substances was studied by direct diffusion into agar and gelatin gels and by equilibrium dialysis through a semipermeable membrane.
Results. Studies have shown that the most complete and rapid release of the active complex of the thick extract of Rhodiola rosea occurs from the Na-CMC base (TU 9199-001-07508109-2004). The highest degree of release of the active complex of the thick extract of Ginkgo biloba is observed from the chitosan base (TU 9289-067-00472124-03 Bioprogress LLC).
Conclusions. In vitro biopharmaceutical studies were carried out to determine the level of release of the studied active substances of thick extracts of Rhodiola rosea rhizomes with roots and Ginkgo biloba leaves from various gel compositions, allowing to select the optimal composition of the dosage form.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Medical chemistry
Prospects for innovative drugs for the treatment of rheumatoid arthritis
摘要
Rheumatoid arthritis is an immune-inflammatory disease with multifactorial etiology, affecting directly or indirectly all organs and systems of the body. Generally accepted standards of drug therapy of rheumatoid arthritis, represented by baseline anti-inflammatory drugs, glucocorticoids and non-steroidal anti-inflammatory drugs, have remained unchanged for a long time, but often they only alleviate or slow down the course of the disease, without curing the patient completely. Therefore, new pharmacologic targets for therapy are being actively investigated. A review of the literature concerning the development of innovative drugs for the treatment of rheumatoid arthritis is presented. The prospects for the development of new drugs based on inhibitors of Janus kinases, transcription factor NF-kB, mitogen-activated kinase p38, histone diethylase, phosphoinositide-3-kinase, low-molecular-weight antagonists of proteinase-activated PAR2 receptors, and anti-PAR-2-specific monoclonal antibodies are outlined.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Bioelementology
The levels of essential trace elements in blood serum and urine of women with osteoporosis
摘要
The objective of the study was to assess serum and urinary concentrations of essential trace elements in women with osteoporosis.
Material and methods. A total of 100 women aged 30-70 years old including 50 patients with osteoporosis (ICD-10: M81) and 50 healthy controls were examined. Assessment of serum and urinary trace element levels was performed using inductively-coupled plasma mass-spectrometry.
Results. The obtained data demonstrate that urinary cobalt and zinc levels in women with osteoporosis were 42% and 44% lower than those in the control women. Analysis of covariance demonstrated a significant impact of osteoporosis and body mass index (BMI) values on urinary Zn concentration. The influence of the presence of osteoporosis on urinary Co concentration was nearly significant. At the same time, serum Co concentration in osteoporotic women was 21% lower than in healthy controls, while no significant difference in serum Zn levels was observed. The presence of osteoporosis in the examined women was also considered a key factor affecting serum Co levels independently of age and BMI values.
Conclusion. Therefore, the results of the present study demonstrated the association between Zn and Co deficiency and the presence of osteoporosis in women. It is suggested that personalized correction of body burden of these trace elements may reduce the risk of osteoporosis due to osteogenic effect of zinc and cobalt. At the same time, intimate mechanisms of this association, as well as efficiency of supplementation strategies in management of osteoporosis requires further investigation.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Problems of experimental biology and medicine
Study of the psychotropic effect of glycyrrhiza glabra root extract under conditions of dapsone-induced exposure
摘要
Relevance. Dapsone (4,4'-diaminodiphenylsulfone) is used as a powerful antibacterial agent in the treatment of infectious diseases. Despite the complex pharmacological effect and high efficacy, dapsone has a number of negative properties, one of which is the occurrence of severe neuropsychiatric pathology with long-term use in the presence of predisposing factors. In this connection, correction of dapsone-induced changes on the part of various systems, including the nervous system, is an urgent task. As a means of correcting dapsone-induced neuropsychiatric changes, an extract of licorice naked horses can act.
The aim of the study was to evaluate the effect of licorice root extract on dapsone–induced changes in behavioral reactions and the severity of the psychomodulatory effect of licorice extract.
Material and methods. All experiments were carried out on white mongrel rats (6-8 months), which were divided into groups (n= 10): group 1 consisted of control rats receiving an equiobject of water for injection; group 2 - individuals receiving intragastric dapsone (Novartis; Switzerland) at a dose of 25 mg/kg for 28 days; group 3 – animals receiving intragastric dapsone at a dose of 25 mg / kg and licorice extract naked through a probe at a dose of 50 mg / kg for 28 days. The effect of licorice root extract on the behavioral reactions of rats under the conditions of course use of dapsone was evaluated using the "Porsolt" and "Open Field" tests.
Results. Against the background of intragastric administration of licorice root extract, there was a restoration of the ratio of immobilization time, active and passive swimming in the Porsolt test, an increase in horizontal and specific mink activity of animals, a decrease in the number of boluses, grooming and freezing in the "Open Field" test compared with the group of animals receiving intragastric dapsone.
Conclusions. Evaluation of the effect of licorice root extract on dapsone-induced changes in behavioral reactions showed the presence of an antidepressant and psychomodulatory effect in the extract, which can be used in the development of a psychocorrective agent based on this medicinal plant.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)