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卷 72, 编号 8 (2023)
Pharmaceutical chemistry and pharmacognosy
Development and standardization of lozenges containing furosemide
摘要
Introduction. Increasing the bioavailability and speed of onset of the diuretic effect of furosemide are necessary for accelerated elimination of toxins in acute and chronic diseases associated with swelling, as well as in acute and chronic poisoning. In conditions where oral or parenteral administration of furosemide is difficult or impossible due to the presence of restrictions in a number of diseases, the use of dosage forms of furosemide with local resorptive action, in particular lozenges, is relevant.
Purpose of the study: Experimental substantiation of quality standards and methods of analysis of lozenges containing furosemide.
Material and methods. The objects of the study are furosemide and lozenges manufactured at the production site of a pharmaceutical company. Research methods: spectrophotometric, chromatographic (HPLC).
Results. The basic physicochemical and technological properties of furosemide have been studied. It has been established that furosemide, as a practically insoluble substance in water, is advisable to introduce into the composition of a drug with local resorptive action in the form of a water-soluble derivative. Methods have been developed for the determination of furosemide in lozenges using two methods, spectrophotometry and HPLC, which meet the main validation criteria, are characterized by accuracy, reproducibility, relative ease of execution, and allow for quality control of the drug at all stages of production.
Conclusion. The physicochemical properties of furosemide make it possible to obtain water-soluble derivatives that can be included in dosage forms with local resorptive action. We have obtained furosemide in the form of a potassium salt, which is the active ingredient of lozenges, the composition of the tablets has been selected and tested, and pilot series have been developed. Methods for the detection and quantitative determination of furosemide have been developed, tested and certified.
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Determination of vitamins in seeds and oil of amaranth tailed grown in Uzbekistan
摘要
Introduction. Today, a number of scientific studies are being carried out in Uzbekistan on the selection of medicinal plants and their reasonable use, in particular, medicinal species of amaranth cultivated in our country, having a sufficient raw material base, are in the center of attention of scientists.
Material and methods. This research work is devoted to the identification and determination of the amount of vitamins in the seeds and oil of amaranth tailed, grown in the Andijan region of the Republic of Uzbekistan.
Resuts. The research work was carried out using high-performance liquid chromatography-mass spectroscopy (LС-MS), which is considered one of the modern analytical methods, and 12 vitamins were tested, 8 of which were fixed in the contents of the seeds and 4 in the oil. content. High Performance Liquid Chromatography (HPLC) determined the amounts of vitamin E and vitamin D3, which were found to be the most retained among vitamins in oil, and obtained results of pharmaceutical significance.
Conclusion. According to the results of the study, it was concluded that amaranth seeds contain vitamins D3, E, B9, B1, B2, B5, B6, C, of which only D3, E, B9, B6 passed into its oil.
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Validation assessment of the method for the quantitative determination of phenolcarboxylic acids in the herb Phacelia tanacetifolia Benth
摘要
Introduction. Increasing the number of medicinal plant materials used is possible with the help of those plants that are widely used in folk medicine, and also, no less interesting for study are previously unexplored plants of foreign flora. Тansy-leaf phacelia is widely cultivated in our country as a honey plant. Phacelia honey has found its use in folk medicine. The chemical composition of the studied object is characterized by a predominant content of phenolic compounds: phenol carbonic acids, flavonoids, tannins, and anthocyanins. Among phenolic compounds, as the main group of the chemical composition of the herb Phacelia tansy, phenolcarboxylic acids dominate in content. For medicinal plants used in folk medicine, standardization of medicinal plant raw materials is carried out according to the main group of compounds. To assess the quality of the herb Phacelia tansy, a method has been developed for quantitative determination of the amount of phenolcarboxylic acids, at which the maximum yield of biologically active substances was observed.
Purpose of the study. Conducting a validation assessment of the developed method for standardizing the herb Phacelia tansy.
Material and methods. The object of the study is the herbs of Phacelia tanacetifolia Benth., grown and collected on the territory of the Republic of Dagestan in the vicinity of the city of Kaspiysk during the flowering period in April 2022. The grass was dried by air-shadow method.
Results. Validation of the developed method was carried out according to the following indicators: specificity, linearity, accuracy and precision (repeatability). Based on the results obtained, it is clear that the validated method meets the appropriate acceptance criteria, which means it can be used to control the quality of the studied medicinal plant raw materials.
Conclusion. Thus, the proposed method for quantitative determination of the amount of phenolcarboxylic acids in the herb Phacelia tansy is suitable for standardization for this indicator.
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The influence of metabolites isolated from Empetrum nigrum L. on the hemostasis system in vitro
摘要
Introduction. Empetrum nigrum L. produces a wide variety of secondary metabolites of polyphenolic nature. According to the literature, E. nigrum exhibits antitumor, antidiabetic, and hypolipidemic activity, due to which it can be used for the treatment and prevention of relevant diseases. The development of thrombosis is a significant complication that occurs in metabolic disorders and cancer, for the prevention and treatment of which it is necessary to search for new biologically active substances.
Purpose of the study. The purpose of this work is to screen individual components 1–19 isolated from E. nigrum shoots in relation to the hemostatic system.
Material and methods. In vitro experiments were performed on the blood of healthy male donors aged 18–24 years. The study of the effect on platelet aggregation was carried out using the Born method on an AT-02 aggregometer (NPF Medtech, Russia). Determination of anticoagulation activity was carried out by generally accepted clotting tests on a turbidimetric hemocoagulometer Solar CGL 2110 (ZAO SOLAR, Russia). As a marker of platelet activation, the expression of P-selectin on the surface of platelets was measured using a cytofluorometric method using a NovoCyte device (Agilent, USA).
Results. Compounds 1, 4, 5, 6, 11, 13, 15 and 18 showed antiaggregation activity at the level of acetylsalicylic acid in vitro, while compounds 3, 8 and 12 showed antiaggregation activity exceeding the values of acetylsalicylic acid. It was also found that compounds 9 and 14 did not affect the level of CD62 expression.
Conclusion. As a result of screening individual compounds 1-19 isolated from E. nigrum shoots, their antiaggregation and anticoagulation properties were established.
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Study of the component composition of peppermint leaves by HPLC method
摘要
Introduction. Peppermint (Mentha piperita L.) is a medicinal plant widely cultivated in the Russian Federation and CIS countries. Peppermint contains various groups of biologically active substances (essential oil, flavonoids, phenylpropanoids), which allow this plant to be used in the medicine, and also in pharmaceutical, food, agricultural industries.
The purpose of the study was to study the component composition of aqueous-alcoholic extracts from peppermint (Mentha piperita L.) leaves using HPLC.
Material and methods. The research material was samples of peppermint leaves (JSC Krasnogorskleksredstva, Reg. No. LP-003986, as well as cultivated in the Botanical Garden of Samara University, Samara).
Analysis of aqueous-alcoholic extracts from peppermint leaves by HPLC was carried out using working standard samples of rosmarinic acid, chlorogenic acid, caffeic acid, luteolin, cynaroside and 5,3'-dihydroxy-6,7,8,4'-tetramethoxyflavone, isolated by us preparatively.
HPLC analysis is carried out under reversed-phase chromatography conditions in a gradient mode on a high-performance liquid chromatograph microcolumn liquid chromatograph "Milichrome-6" (NPJSC "Nauchpribor") in a gradient mode, steel column "KAH-6-80-4" (No. 2; 2×80 mm; Separon-C18 7 µm), eluent system: acetonitrile – 1% acetic acid solution, elution rate – 100 µl/min. Detection of substances was carried out at wavelengths of 290, 330 and 350 nm. The volume of injected samples is 2 µl.
Results. It was determined that the dominant phenylpropanoid in the aqueous-alcoholic extract of peppermint leaves is rosmarinic acid, the retention time of which is 12,61 minutes. Chlorogenic acid, caffeic acid, cynaroside, luteolin, and 5,3'-dihydroxy-6,7,8,4'-tetramethoxyflavone were found and identified in the raw materials of this plant.
Conclusion. As a result of the study it was determined that the dominant component of aqueous-alcoholic extracts from peppermint leaves is rosmarinic acid.
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Technology of medicines
Biopharmaceutical substantiation of the composition and analysis of the soft dosage form with chloropyramine hydrochloride
摘要
Introduction. An urgent task of our time is the search for new dosage forms for already known and widely used active substances. An example is suprastin, which is used to treat allergic diseases that cause inflammatory processes: dermatoses, angioedema, urticaria, allergic rhinitis, initial manifestations of bronchial asthma and is usually prescribed orally in the form of tablets or solutions. However, these routes of administration have a number of disadvantages, which are easily mitigated in soft dosage forms. Ease of administration, good bioavailability, the possibility of systemic action of drugs and the speed of its development, active absorption of substances that undergo breakdown in the gastrointestinal tract. Considering the advantages of the ointment as a dosage form, and the data on the pharmacological effectiveness of suprastin, it seems appropriate to develop a soft dosage form with pronounced anti-inflammatory and antihistamine activity and methods for qualitative and quantitative determination of the active substance.
Purpose. Conduct biopharmaceutical research on the selection of a base for a soft dosage form with chloropyramine hydrochloride. To determine the optimal conditions for the spectrophotometric determination of chloropyramine hydrochloride, which is part of the dosage form.
Material and methods. The object of the study was ointment compositions, which included chloropyramine hydrochloride 0.1 g. When choosing the optimal conditions for confirming the authenticity of chloropyramine hydrochloride in the ointment, a model mixture was prepared with the exact content of all components. The CO spectra of chloropyramine hydrochloride and its extract from the ointment in water, solutions of sodium hydroxide and hydrochloric acid were recorded using an SF-56 spectrophotometer in the wavelength range from 220 to 350 nm.
Results. 5 ointment compositions with suprastin are proposed. Based on biopharmaceutical studies, the degree of release of the active substance was studied. To confirm the authenticity of the soft dosage form, the absorption spectra of chloropyramine hydrochloride in three solvents were used – purified water, 0.1 M sodium hydroxide solution and 0.1 M hydrochloric acid solution. The absorption spectrum in a 0.1 M solution of hydrochloric acid has more pronounced maxima and stable optical density.
Conclusion. The greatest release of the active complex occurs from the hydrophilic base, which can serve as a basis for its use in the production of soft dosage forms with suprastin.
Methods have been developed to confirm the authenticity of chloropyramine hydrochloride in soft dosage form. The possibility of using spectrophotometry to identify the studied medicinal substance in the ointment has been demonstrated.
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Development of a method for the quantitative determination of flavonoids in dill herb (Anethum graveolentis herba)
摘要
Introduction. The dill herb, collected before flowering, contains a complex of various biologically active compounds (BACs) and can act as an independent medicinal plant material. There is data confirming the activity of the aerial part of dill against Agrobacterium radiobacter pv. Tumefaciens, Erwinia carotovora, Pseudomonas fluorescens, Pseudomonas wisteria. The antimicrobial properties of the herb dill may be associated with the presence of phenolic compounds, including flavonoids, in the chemical composition, so the quantitative determination of the amount of these biologically active compounds is relevant.
Purpose of the work: to develop a method for quantitative determination of the amount of flavonoids in dill herb (Anethum graveolentis herba).
Material and methods. The object of study was air-dried dill herb (Anethum graveolens L.), harvested before flowering. Quantitative determination of the amount of flavonoids was carried out by spectrophotometric method after complexation reaction with aluminum chloride on a Lambda-950 spectrophotometer, Perkin Elmer, USA.
Results and discussion. As a result of the study, it was shown that to determine the amount of flavonoids in aromatic dill herb harvested before flowering, the following conditions are optimal: crushing of raw materials to a particle size of 1 mm, mass of raw materials about 2 g, extraction with 80% ethyl alcohol in a volume of 100 ml when heated for 50 min; the ratio of the volume of the extract and 2% aluminum chloride solution is 1:1, the complexation reaction time is 30 minutes.
Conclusion. A method has been developed for determining the amount of flavonoids in terms of rutin and absolutely dry raw materials in dill herb (Anethum graveolentis herba).
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Organization and economy
Quantitative characteristics of the labor potential of students enrolled in pharmaceutical education programs
摘要
Introduction. Studying the labor potential of the student population is the first step towards studying the reasons for the imbalance of supply and demand in the labor market in the pharmacy segment.
The purpose of the study is to study the quantitative characteristics of the labor potential of the contingent of students mastering secondary vocational education and higher education programs in the Russian Federation.
Material and methods. The object of the study is the student population. The source of quantitative data is federal statistical observation forms (SPO-1, VPO-1).
Results and discussion. The total number of VO students in the Russian Federation is 18,865 people, of which budget students are 52.7% (9,943 people), commercial students are 47.3% (8,922 people). Of the 85 constituent entities of the Russian Federation, training of specialists with higher education was carried out in 53 constituent entities. A retrospective analysis of VPO-1 showed a significant decrease in the supply of labor resources from the VO system.
The total number of SPO contingent in the Russian Federation is 44,143 people. The ratio of budget and commercial students is 14.1% (16,177 people) and 85.9% (37,909 people), respectively. 30% of students (1,867 people) studied at the expense of the federal budget. Training was carried out in 79 constituent entities of the Russian Federation. A retrospective analysis of SVE-1 shows a steady increase in the volume of labor supply generated by the SVE personnel training system.
Conclusion. There are 63,008 people in the pharmaceutical education system of the Russian Federation. The main share of supply is graduates of vocational training programs (70%), which corresponds to the structure of the personnel request of pharmacies. The main trend in changes in the quantitative characteristics of labor potential is a significant increase in the number of students in secondary vocational education and a reduction in the volume of training in the higher education system. The volume of training in the constituent entities of the Russian Federation is uneven.
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