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Molecular Docking: Methodological Approaches of Risk Assessment 分子对接:风险评估的方法论方法
Drug Development and Registration Pub Date : 2023-05-29 DOI: 10.33380/2305-2066-2023-12-2-206-210
A. Kh. Taldaev, I. D. Nikitin, R. P. Terekhov, I. A. Selivanova
{"title":"Molecular Docking: Methodological Approaches of Risk Assessment","authors":"A. Kh. Taldaev, I. D. Nikitin, R. P. Terekhov, I. A. Selivanova","doi":"10.33380/2305-2066-2023-12-2-206-210","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-2-206-210","url":null,"abstract":"Introduction. Computational chemistry methods and, particularly, the noncovalent molecular docking are increasingly implemented into the practice of drug development. Previously, a risk management of potential biases did not applied for this relatively young research instrument. Aim. The study objective was to design the risk assessment system for noncovalent molecular docking. Materials and methods. The development of bias risk assessment system was based on the world's leading practices in noncovalent molecular docking. Results and discussions. As a result of the deductive analysis of the molecular docking process, bias domains were identified and a risk-based algorithm was proposed, which was tested on a sample of articles obtained during a systematic review. A tendency to frequent limited provision of information on the methodology of the computational experiment, as well as on the application of practices proven to lead to irrelevant results of molecular docking, has been revealed. Conclusion. The data obtained cannot be extrapolated to all studies that refer to the results of molecular modeling. However, through the proposed risk-based algorithm, the attention of researchers is focused on assessing the quality of such publications. We hope that the developed tool for bias risk assessment in noncovalent molecular docking will be finalized and eventually put into practice. It will possibly reduce the share of low-quality work in the field of drug development at the earliest stages.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"5 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135792816","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Study of the Radiosensitizing Action of Lithium Ascorbate Under Neutron and Photon Irradiation of Tumor Cells 抗坏血酸锂在肿瘤细胞中子和光子照射下的放射增敏作用研究
Drug Development and Registration Pub Date : 2023-05-29 DOI: 10.33380/2305-2066-2023-12-2-185-189
M. S. Tretyakova, A. G. Drozd, M. V. Belousov, K. S. Brazovskiy, M. S. Larkina, S. V. Krivoshchekov, A. A. Artamonov, I. A. Miloichikova, A. V. Bezmaga, A. M. Bolshakov, E. S. Sukhikh, E. V. Plotnikov
{"title":"Study of the Radiosensitizing Action of Lithium Ascorbate Under Neutron and Photon Irradiation of Tumor Cells","authors":"M. S. Tretyakova, A. G. Drozd, M. V. Belousov, K. S. Brazovskiy, M. S. Larkina, S. V. Krivoshchekov, A. A. Artamonov, I. A. Miloichikova, A. V. Bezmaga, A. M. Bolshakov, E. S. Sukhikh, E. V. Plotnikov","doi":"10.33380/2305-2066-2023-12-2-185-189","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-2-185-189","url":null,"abstract":"Introduction. Radioresistance of cancer cells is a serious problem in radiation therapy of tumor diseases. Radiosensitizers make malignant cells more sensitive to radiation and increase the effectiveness of radiation therapy; however, their widespread clinical use is limited by significant side effects. The development and study of new radiosensitizers seems to be an urgent task of modern pharmacology. Aim. The purpose of this work was to study the effectiveness of lithium ascorbate as a radiosensitizer under the influence of photon and neutron radiation in wide dose range. Materials and methods. Evaluation of the biological effect was carried out using the tumor line of prostate cancer PC-3. We used a cyclotron to produce neutron radiation and a Cobalt-60 source to produce gamma radiation. Results and discussion. We have proved an increase in the cytotoxic effect with the combined use of different types of ionizing radiation and lithium ascorbate. The resistance of the prostate cancer line to gamma radiation at an absorbed dose of 0.5–3.0 Gy was revealed. It was shown that tumor cells of prostate cancer are more sensitive to the effects of the study drug in minimal concentrations in combination with neutron irradiation compared to gamma radiation in the same absorbed dose. The main mechanism of the radiosensitizing action of lithium ascorbate is the local induction of oxidative stress, which synergistically enhances the action of ionizing radiation. Conclusion. The combination of lithium ascorbate with neutron radiation leads to a more pronounced resulting cytotoxic effect. An increase in the concentration of lithium ascorbate led to the pro-oxidative action with an increase in the damaging effect on cells.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"27 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135741617","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Effect of a Farnesoid X-receptor Agonist on Postprandial Lipemia in Rats Fed a Supraphysiological Fat Dozes Farnesoid x受体激动剂对喂食超生理脂肪睡眠大鼠餐后脂血症的影响
Drug Development and Registration Pub Date : 2023-05-29 DOI: 10.33380/2305-2066-2023-12-2-174-184
Yu. N. Alekhin, O. S. Popova, V. S. Ponamarev, P. A. Parshin
{"title":"Effect of a Farnesoid X-receptor Agonist on Postprandial Lipemia in Rats Fed a Supraphysiological Fat Dozes","authors":"Yu. N. Alekhin, O. S. Popova, V. S. Ponamarev, P. A. Parshin","doi":"10.33380/2305-2066-2023-12-2-174-184","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-2-174-184","url":null,"abstract":"Introduction. One of the most progressive directions of the modern stage of development of biology is the deepening of knowledge about the mechanisms of regulation of metabolic processes, in particular about signal molecules that transmit information to the cell through ion channels and nuclear receptors associated with G-protein or with enzymatic activity. The nuclear Farnesoid X receptor (FXR) is mainly expressed in the liver and intestines, it regulates key genes that provide the processes of synthesis, transport and reabsorption of bile acids, and is also involved in the metabolism of lipids and carbohydrates. Aim. To evaluate the effect of a farnesoid X receptor agonist on postprandial lipemia in rats fed a supraphysiological fat diet. Materials and methods. An experimental, prospective, controlled, unblinded, randomized study was conducted to study the effect of a farnesoid X receptor agonist (obeticholic acid) on postprandial lipemia in rats receiving a diet containing a supraphysiological dose of fats. Results and discussion. It has been shown that when assessing postprandial lipemia, an oral test for tolerance to supraphysiological doses of fat with the determination of the initial lipid profile parameters and 4 hours after exercise has a sufficiently high information content. It was found that in animals that received a diet containing an increased amount of fat for 28 days, there was an imbalance in lipid metabolism with activation of their absorption in the intestine, but a \"slow\" reaction of the mechanisms of intermediate lipid metabolism, which was accompanied by the accumulation of triglycerides and cholesterol in the blood of hungry rats, chylomicrons and LDL. At 4 hours post-feeding, these animals showed abnormal increases in triglycerides and cholesterol. Conclusion. The use of obeticholic acid harmonizes lipid metabolism against the background of alimentary fat load, due to the activation of farnesoid X-receptors of the intestine and liver, which is manifested by a simultaneous increase in the intensity of lipid absorption processes and their intermediate metabolism. As a result, the risk of hyperchylomicronemia, hypercholesterolemia and hypertriglyceridemia is eliminated, the likelihood of developing secondary hyperlipedemia, insulin tolerance and functional overload (or pathology) of the liver is reduced.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"20 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135793014","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Hypertonic Activity of Injection Solutions Can Cause Post-injection Complications (Review) 注射液的高渗活性可引起注射后并发症(综述)
Drug Development and Registration Pub Date : 2023-05-29 DOI: 10.33380/2305-2066-2023-12-2-164-173
A. L. Urakov, N. A. Urakova, Z. V. Shubina, L. V. Lovtsova, A. V. Samorodov, K. G. Gurevich, A. P. Stolyarenko, V. I. Korunas, D. O. Lipatov, D. D. Muminov
{"title":"Hypertonic Activity of Injection Solutions Can Cause Post-injection Complications (Review)","authors":"A. L. Urakov, N. A. Urakova, Z. V. Shubina, L. V. Lovtsova, A. V. Samorodov, K. G. Gurevich, A. P. Stolyarenko, V. I. Korunas, D. O. Lipatov, D. D. Muminov","doi":"10.33380/2305-2066-2023-12-2-164-173","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-2-164-173","url":null,"abstract":"Introduction. A review of the scientific literature showed that the current standards for assessing the quality of drugs does not include an assessment of the osmotic activity of drug solutions and their local irritant effect on tissues at the sites of subcutaneous, intramuscular and intravenous injections. Therefore, currently injectable solutions considered to be of high quality may not have isotonic activity and high postinjection safety. Text. A study of the concentration range of quality drug solutions ready for injection showed that the acceptable concentration value of the main ingredients is in the range of 0.01 to 76 %. Direct measurement with an osmometer of the osmotic activity of injection solutions, considered qualitative today, has shown that injection solutions can have hypotonic, isotonic and hypertonic activity and their osmotic activity can be in the range of 0 – 3900 mosmol/l water. Study of acidic activity of drug solutions showed that in accordance with pharmacopoeial requirements of drug quality modern quality drug solutions ready for injection can have acidic, neutral or alkaline activity. Solutions with hypertonic activity have been found to have a local irritant effect. Moreover, an increase in hypertonic activity of drug solutions increases their local irritant effect. It has been found that excessively high hypertonic activity of drug solutions may be the cause of the development of a local postinjection complication known as \"Nicolaou syndrome\", the cause of which has remained unknown for a long time. Nicolaou syndrome includes local pain syndrome, aseptic inflammation, necrosis, and abscess. Conclusion. The authors conducted a literature review, the results of which led to conclusions and assumptions. Solutions containing drugs in concentrations greater than 10 % may have the highest hypertonic activity, which can cause excessive dehydrating, local irritating and cauterizing effects. Therefore, injections of such drugs are most dangerous with the development of post-injection necroses and abscesses. That is why timely dilution of concentrated drug solutions with water by 2–10 times increases injection safety. It is proposed to include the assessment of osmotic activity and local irritant effect of drug solutions in the standard of drug quality control.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"26 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135693391","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Regulation of the Launch of Orphan Drugs on the Market of the Eurasian Economic Union as a Mechanism to Increase the Availability of Treatment for Rare Diseases (Review) 作为增加罕见病治疗可得性机制的欧亚经济联盟孤儿药上市监管(审查)
Drug Development and Registration Pub Date : 2023-05-29 DOI: 10.33380/2305-2066-2023-12-2-198-205
A. V. Foteeva, N. A. Koneva, O. S. Beloglazova, N. B. Rostova
{"title":"Regulation of the Launch of Orphan Drugs on the Market of the Eurasian Economic Union as a Mechanism to Increase the Availability of Treatment for Rare Diseases (Review)","authors":"A. V. Foteeva, N. A. Koneva, O. S. Beloglazova, N. B. Rostova","doi":"10.33380/2305-2066-2023-12-2-198-205","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-2-198-205","url":null,"abstract":"Introduction. Providing high-quality, effective and safe drugs intended for the treatment of rare (orphan) diseases among the population of the Member States of the Union is one of the most significant and promising development vectors for manufacturers-developers. Ensuring the availability of medicines (MP) for patients suffering from rare diseases should be regulated by state incentives for the development and launch of orphan drugs on the market by domestic manufacturers through updating and timely updating of regulatory legal acts in the field of drug registration, as well as providing benefits when initiating the registration process. Text. The article assessed the possibilities and prospects for the introduction of orphan drugs into circulation within the framework of the Eurasian Economic Union for domestic manufacturers. Conclusion. A review of the possibilities and prospects for launching orphan drugs for domestic manufacturers indicates the need to develop regulatory and legal regulation of aspects of pharmaceutical development in order to increase the availability of treatment for patients with rare diseases, both at the level of the Russian Federation and within the legal framework of the Eurasian Economic Space.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"24 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135792996","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The Content of Minor Elements in the Breast Collection No. 4 《乳房文集》第4号中微量元素的内容
Drug Development and Registration Pub Date : 2023-05-28 DOI: 10.33380/2305-2066-2023-12-2-113-123
I. V. Gravel, D. V. Levushkin
{"title":"The Content of Minor Elements in the Breast Collection No. 4","authors":"I. V. Gravel, D. V. Levushkin","doi":"10.33380/2305-2066-2023-12-2-113-123","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-2-113-123","url":null,"abstract":"Introduction. Trace elements are an essential part of the human body, but about 80 % of the human population notes an imbalance in their content. Medicinal plants contain minerals in an accessible and digestible form together with biologically active substances. Medicinal herbal preparations are very popular for the prevention and as part of the complex therapy of various diseases. However, information about the content of trace elements in multicomponent medicinal herbal preparations is very limited. Therefore, it is necessary to study the mineral composition, which will allow us to consider plant collections as an additional source of trace elements. Aim. The purpose of our study was to study the content of trace elements (B, Si, Al, Ba, Sr, Ti) in breast collection No. 4, its components and aqueous extracts from them. Materials and methods. The objects of the study were breast collection No. 4, its individual components and aqueous extracts from them. Infusions from the samples were obtained according to the instructions for use on the packaging of a medicinal herbal preparation. The samples were prepared for analysis with a mixture of concentrated nitric acid and water deionized in the Milestone Ethos Up microwave system (Milestone, Italy). The analysis was carried out by atomic emission spectrometry with inductively coupled plasma on the ISP-NPP 720-ES device (Agilent Technologies, USA). Results and discussion. It was found that the concentrations of Si, Al, B, Sr, Ba, Ti in individual components of the collection varied in the range of 2.9–1240 mg/kg, the transition of trace elements to aqueous extracts was 0.4–34.2 %. The content of these elements in breast collection No. 4 was found to be 13.3–920.7 mg/kg, and the degree of extraction the infusion was 3–40 %. Comparative analysis showed that the extraction of B, Al, Ba from the collection into the infusion is 14–58 % higher than from the individual components included in its composition. It has been established that 50 % of boron and 264 % of silicon from the recommended adequate level of consumption in the Russian Federation enters the human body with an infusion from the breast collection No. 4. Conclusion. The study showed that breast collection No. 4 can be considered as an additional source of B and Si in the human body. The concentrations of Al, Sr, Ba, Ti were within the average values of the range of the content of these elements in plants.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"42 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135895421","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development and Validation of a Method for the Quantitative Determination of Etoricoxib in Liquid Dosage Form 依托昔布液体剂型定量测定方法的建立与验证
Drug Development and Registration Pub Date : 2023-05-28 DOI: 10.33380/2305-2066-2023-12-2-95-102
A. Kh. Amandusova, A. E. Kovalenko, A. V. Morozov, K. R. Savelyeva, T. L. Batalova, O. A. Ostapyuk, L. V. Persanova, T. Yu. Andreevicheva, A. G. Beniashvili, V. N. Shestakov, S. V. Polyakov
{"title":"Development and Validation of a Method for the Quantitative Determination of Etoricoxib in Liquid Dosage Form","authors":"A. Kh. Amandusova, A. E. Kovalenko, A. V. Morozov, K. R. Savelyeva, T. L. Batalova, O. A. Ostapyuk, L. V. Persanova, T. Yu. Andreevicheva, A. G. Beniashvili, V. N. Shestakov, S. V. Polyakov","doi":"10.33380/2305-2066-2023-12-2-95-102","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-2-95-102","url":null,"abstract":"Introduction. Etoricoxib is a selective cyclooxygenase (COX-2) inhibitor used for the treatment of acute pain and has anti-inflammatory and analgesic efficacy. Etoricoxib causes fewer complications compared to other non-steroidal anti-inflammatory drugs (NSAIDs). FSI \"SID and GP\" has developed an ophthalmic liquid dosage form based on etoricoxib. This article proposes a method for determining the content of etoricoxib in a liquid dosage form by high performance liquid chromatography with UV detection. Aim. Development and validation of a method for the quantitative determination of etoricoxib in liquid dosage form. Materials and methods. Eye drops with a concentration of the active substance etoricoxib of 0.05 % were used for the analysis, a standard sample of etoricoxib (Kekule Pharma Limited, India, series ACE-3 WS001/15). Chromatographic separation performed on an Agilent 1220 Infinity II LC high performance liquid chromatograph (Agilent Technologies, USA) equipped with a gradient pump, a column thermostat, and a diode array detector. The analysis carried out on a Kromasil C8 column 250 × 4.6 mm, using acetonitrile and 0.05 M buffer solution of potassium dihydrogen phosphate pH = 4.2 as a mobile phase in a ratio of 46 : 54. The analysis time was 15 minutes at a detection wavelength of 235 nm. Results and discussion. A method for the quantitative determination of etoricoxib in a liquid dosage form developed and validated according to the following indicators: specificity, linearity, accuracy, range, intermediate precision, repeatability. Conclusion. According to the results of validation tests, all of the listed parameters meet the acceptance criteria. The proposed method characterize by high efficiency and specificity.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"222 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135895419","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Physicochemical and Functional Characterization of Medicinal Product Rinsulin® R 药物胰岛素®R的理化及功能表征
Drug Development and Registration Pub Date : 2023-05-28 DOI: 10.33380/2305-2066-2023-12-2-124-134
A. V. Babina, R. V. Drai, V. B. Saparova, A. N. Afanasyeva, P. G. Zaikin, V. I. Shmurak, T. E. Eltysheva, I. E. Makarenko
{"title":"Physicochemical and Functional Characterization of Medicinal Product Rinsulin® R","authors":"A. V. Babina, R. V. Drai, V. B. Saparova, A. N. Afanasyeva, P. G. Zaikin, V. I. Shmurak, T. E. Eltysheva, I. E. Makarenko","doi":"10.33380/2305-2066-2023-12-2-124-134","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-2-124-134","url":null,"abstract":"Introduction. Currently, biosimilars have found quite widespread use in the treatment of a number of chronic and life-threatening diseases. Thanks to them, there is a significant decrease of the economic pressure of biological drugs on the health care system and wide access of patients to effective and safe medicines is ensured. One of the most important stages of proving biosimilarity is the physicochemical and functional characterization of proteins. This set of studies is generally accepted, as sensitive as possible and allows us to give a conclusion about the compliance of the biosimilar with the original drug. Aim. Conducting physicochemical and functional characterization of medicinal product Rinsulin® R (GP40051) in comparison with the original drug Humulin® Regular. Materials and methods. Primary structure was analyzed by high-performance liquid chromatography with mass spectrometry detection and matrix assisted laser desorption/ionization. The identity of the higher protein structures was proved by the methods of circular dichroism, capillary isoelectric focusing, spectrometry and dynamic light scattering. The comparability of the impurity profiles of the preparations was evaluated using the methods of exclusive chromatography and reverse-phase high-performance liquid chromatography. Functional characterization included a metabolic cell test \"glucose uptake\" and insulin receptor–binding assay (kinetics of binding to type A and B receptors, phosphorylation of insulin receptor). Results and discussion. In the course of this research, the identity of the physicochemical and functional characteristics of GP40051 was shown. A complete overlap of primary sequence, high-order structures and impurity profiles was demonstrated between the comparison drug GP40051 and the reference drug Humulin® Regular. Functional studies have shown that GP40051 and Humulin® Regulars have the same activity. Conclusion. The results of the quality comparability study demonstrated similarity of Rinsulin® R to the reference medicinal product Humulin® Regular, providing the scientific basis for conducting a specifically designed clinical programme, and supported registration in Russian Federation.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"7 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135895422","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Phytochemical Analysis of the Aerial Part of Golden Dock (<i>Rumex Maritimus</i> L.) 金码头(&lt;i&gt;Rumex Maritimus&lt;/i&gt;)地上部分植物化学分析l .)
Drug Development and Registration Pub Date : 2023-05-28 DOI: 10.33380/2305-2066-2023-12-2-73-78
V. V. Podgurskaya, E. A. Luksha, I. A. Savchenko, I. N. Korneeva, E. V. Ivanova
{"title":"Phytochemical Analysis of the Aerial Part of Golden Dock (&lt;i&gt;Rumex Maritimus&lt;/i&gt; L.)","authors":"V. V. Podgurskaya, E. A. Luksha, I. A. Savchenko, I. N. Korneeva, E. V. Ivanova","doi":"10.33380/2305-2066-2023-12-2-73-78","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-2-73-78","url":null,"abstract":"Introduction. Golden dock ( Rumex maritimus L., Polygonaceae ) is used as a medicinal and food plant in Asian countries. The plant contains phytochemicals of various classes: flavonoids, tannins, anthraquinones etc. Plant extracts exhibit antibacterial, antioxidant, anti-inflammatory, astringent activity, and have antidiabetic potential. The plant is annual, and most of the biologically active substances accumulate in its aboveground organs. An important problem is the standardization of Rumex maritimus and the development of regulatory documentation for its the introduction to medical practice. Aim. To conduct phytochemical analysis of the aerial part of golden dock. Materials and methods. Air-dried aerial part of Rumex maritimus collected at flowering and beginning of fruiting stage, as well as individual above-ground organs (leaves, flowers, fruits, stems), were used for obtaining the extracts. Qualitative analysis of the extracts was carried out using reverse phase HPLC. The relative content of the components in the mixture was calculated by the method of simple normalization. Total content of free anthraquinones and anthraglycosides in terms of chrysophanic acid was determined using spectrophotometric method after acid hydrolysis. Total tannin content was calculated by titrimetric method. Results and discussion. Flavonoids isoquercetin and avicularin were first discovered in the aerial part of Rumex maritimus . The dominant component of the plant is rutin. Chrysophanol predominates among anthraquinones. The highest concentration of anthraquinones (2.80 ± 0.04 %) was found in flowers. Tannins accumulate mainly in leaves (9.97 ± 0.02 %). A significant amount of tannins (6.60 ± 0.03 %) and anthracene derivatives (1.96 ± 0.03 %) is contained in the whole aerial part. Conclusion. Phytochemical analysis of the aerial part of Rumex maritimus showed the presence of a significant amount of anthraquinones. As a plant raw material it is proposed to use the herb of Rumex maritimus . Standardization is recommended for anthraquinones in terms of chrysophanic acid (at least 1.5 %).","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"100 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135895423","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Phase I Pharmacokinetics Study of Drug for Infusion «Areplivir» (INN: Favipiravir) (LLC "PROMOMED RUS", Russia) 输注用药物“Areplivir”(INN: Favipiravir) (LLC " promed RUS",俄罗斯)的I期药代动力学研究
Drug Development and Registration Pub Date : 2023-05-28 DOI: 10.33380/2305-2066-2023-12-2-146-153
T. N. Komarov, N. S. Bagaeva, K. K. Karnakova, I. E. Shohin, K. Ya. Zaslavskaya, P. A. Bely
{"title":"Phase I Pharmacokinetics Study of Drug for Infusion «Areplivir» (INN: Favipiravir) (LLC \"PROMOMED RUS\", Russia)","authors":"T. N. Komarov, N. S. Bagaeva, K. K. Karnakova, I. E. Shohin, K. Ya. Zaslavskaya, P. A. Bely","doi":"10.33380/2305-2066-2023-12-2-146-153","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-2-146-153","url":null,"abstract":"Introduction. The novel coronavirus infection COVID-19 (Coronavirus Disease 2019) is caused by an enveloped, positive-sense, single-stranded ribonucleic acid (RNA) virus SARS-CoV-2 (severe acute respiratory syndrome-related coronavirus 2). Favipiravir is the antiviral drug recommended for etiotropic treatment of COVID-19. Parenteral therapy has advantages over the other routes of the drug administration: there are no interaction with food and digestive enzymes, may be used for patients with diseases of the digestive system and unconscious patients. For parenteral drug administration of favipiravir the drug \"Areplivir\" has been registered in Russia. Aim. The aim is pharmacokinetics study of drug \"Areplivir\", a lyophilisate for the preparation of a concentrate for the infusion solution (the manufacturer is JSC \"Biokhimic\", LLC \"Promomed RUS\" as registration certificate holder) by intravenous infusion in healthy volunteers in a phase I pharmacokinetics study. Materials and methods. The clinical and analytical phases of the pharmacokinetic study as well as pharmacokinetic analyses have been performed as part of a clinical trial of the drug \"Areplivir\" in different doses, a lyophilisate for the preparation of a concentrate for the infusion solution (LLC \"Promomed RUS\", Russia). Chromatographic separation and detection were carried out on a LC-2040C high-performance liquid chromatograph (Shimadzu Corporation, Japan) with a built-in UV detector, a low-pressure four-component gradient pump, a degasser, an autosampler, a column thermostat and a controller. The pharmacokinetic parameters were calculated with the Boomer pharmacokinetic analysis add-in for Microsoft Excel (Department of Pharmacokinetics and Drug Metabolism, Allergan, Irvine, CA 92606, USA). Descriptive pharmacokinetic statistics were calculated with Microsoft Excel (Microsoft Corporation, USA). Correlation and Regression Analysis were conducted with IBM SPSS Statistics (version 23.0), IBM, USA. Results and discussion. For single dose administration of 400, 800, 1600 and 1800 mg in 4 cohorts of 5 volunteers pharmacokinetic parameters were calculated. For C max and an administered dose the strong correlation coefficient on the Chaddock scale ( r = 0,98; p = 0,02; r – Pearson correlation coefficient; p – the reached significance value) and the determination coefficient ( R 2 = 0,96; F = 45,97; p = 0,02; R 2 – determination coefficient; F – the actual value of the Fisher's criterion) were statistically significant. For AUC 0- t and an administered dose the strong correlation coefficient on the Chaddock scale ( r = 0,97; p = 0,03) and the determination coefficient ( R 2 = 0,94; F = 33,54; p = 0,03) were statistically significant. The obtained results show the linearity of C max and an administered dose and the linearity of AUC 0- t and an administered dose (400–1800 mg). Conclusion. According to the concentrations of favipiravir from the analytical phase of the pharmacokinetic study the pharmacok","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135895417","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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