The review presents the results of the blood substitute development based on perfluororganic compounds (PFC). The limitations of PFC due to which their further development was suspended are described. The presented data allows us to imagine a possible way to create optimal drugs based on PFC. Chemically inactive perfluorocomponents should be used — perfluorinated hydrocarbons and tertiary perfluorinated amines. However, in order to emulsify and stabilize the emulsion, other types of effective and chemically indifferent surfactants that do not interact with oxygen and other components of the drug are needed.
Background: Pathology of the hepatobiliary system includes a heterogeneous group of diseases of the liver and biliary system caused by viral, bacterial and parasitic infections, neoplasms, toxic chemicals, including alcohol, nutritional errors, metabolic disorders and heart failure. One of the basic groups for pharmacological correction of this group of diseases is the use of hepatoprotectors, drugs that have a predominantly selective effect on the liver. The active ingredient of most plant hepatoprotectors are flavonoids and hydroxycinnamic acids. The most popular plants – hepatoprotectors containing these active substances include – artichoke prickly (Cynara scolymus (L.)) and sandy everlasting (Helichrysum arenarium (L.) Moench), a plant with choleretic action, also capable of hepatoprotective activity. The aim of the study: Development and comparative characterisation of methods for the analysis of polyphenolic composition of sandy everlasting flowers and artichoke leaves in complex pharmacological studies using HPLC and capillary electrophoresis methods. Materials and methods: The sum of polyphenolic compounds was subjected to chromatographic separation in gradient elution mode. Capillary electrophoresis was carried out in a variant of micellar electrokinetic chromatography (MEKC). The buffer solution used was a mixture of: borate buffer 20 mM (pH - 9.3) – beta-cyclodextrin 20 mM – ethyl alcohol (10:10:5). Results: The electrophoregrams of the separation of artichoke leaf extract by the MECC method showed the presence of 7 components belonging to oxycinnamic acids and flavonoids. The dominant ones are chlorogenic acid and luteolin7-glucoside. Similar results were obtained by the HPLC method. The electrophoregram of immortelle flower extract shows 9 components, of which the dominant one belongs to isosalipurposide. Chromatographic analysis of sandy everlasting flower extract showed the presence of the same components. Conclusion: The results of the analysis of the polyphenolic complex of artichoke leaves and sandy everlasting flowers by capillary electrophoresis agree with the data obtained by HPLC chromatography. This allows us to conclude that the MECC method allows the identification and quantification of each component in artichoke leaves and HPLC chromatography flowers along with HPLC. Moreover, the performance of the analysis by CE is more economically feasible than HPLC, since it does not require the use of solvents for the mobile phase and the availability of a set of columns.
Cytostatic activity of baicalin, baicalein, and neogalenical drug Chlorophyllipt was studied in vitro on HeLa-v cells. Standard samples of Eucalimin, baicalin, and baicalein, as well as Chlorophyllipt and paclitaxel (reference drug Taxacad) were used. The cell deaths were determined by MTT assay in a Multiskan FC microplate reader with incubator. The effective inhibition concentration (IC50) of the tested substances were: paclitaxel (4.0±0.4 μM)—baicalein (10.5±1.1 μM)—baicalin (16.5±1.7 μM)—sum of euglobals in Chlorophyllipt (24.1±2.5 μM). Chlorophyllipt was found to exhibit cytostatic activity. Cytostatic activity of baicalein, baicalin, and Chlorophyllipt was lower than cytostatic activity of the reference drug by 2.6, 4.1, and 6 times, respectively. The prospects of further evaluation of the synergetic effect of baicalin, baicalein, and chlorophyllipt used in combinations with different cytostatic agents for finding the most effective combination have been shown.
РезюмеАктуальность: Ар-турмерон один из основных компонентов эфирного масла корневищ Curcuma longa L. Он обусловливает специфичность состава эфирного масла корневищ C
Aim to develop and test an analytical method for the quantitative determination of carbon tetrachloride in freons used in the composition of medicines in the form of an aerosol. Material and methods. Carbon tetrachloride (tetrachloromethane, Freon-10) - CCl4, M.m. = 153.81, heavy, colorless, volatile liquid with a sweet smell reminiscent of chloroform. Melting point - 22.96 С, boiling point - 76.75 C, relative density at 20 - [d]420 1.595. Poorly soluble in water (0.5 g/l), unrestrictedly miscible with alcohol, ether, acetone, benzene (chemically pure grade). To determine the tests for the presence and quantitative determination of carbon tetrachloride in propellant gases used in medicinal preparations, we chose the drug "Salbutamol-Pharmstandard". To identify and quantify carbon tetrachloride in propellants used in medicinal products, the gas-liquid chromatography method with electron capture detection with a capillary column was applied. Results. The developed method was used to determine carbon tetrachloride in the test preparation "Salbutamol". The results were statistically processed and showed that the content of carbon tetrachloride in the test preparation was 0.01580.0007 mg/l. The error of a single experiment with a confidence probability P = 95% was 4.42% Conclusion. We proposed a method for estimating the content of carbon tetrachloride impurities in aerosol dosage forms by gas-liquid chromatography with an electron capture detector. The technique involved the gas chromatographic separation of a sample, taken from an aerosol can, on a capillary chromatographic column. The most appropriate detector in this case turned out to be an electron capture detector.
Introduction. Lactoferrin is a biologically active substance, a natural glycoprotein from the group of iron-containing proteins, transferrin. This article is devoted to a review of the literature data on the properties and prospects for the use of lactoferrin in medicine and veterinary medicine.Text. The problem of widespread use of lactoferrin is the need to use a large volume of raw materials, the difficulty of extracting it from agricultural raw materials and subsequent purification. In this view, at present, it is very promising to use transgenic animals to obtain such a valuable compound in the required volume. Discovered in 1939 in cow's milk, lactoferrin exhibits a wide spectrum of biological activity, new properties of this protein are constantly being established. The most studied are the immunomodulatory effects, anti-inflammatory, antimicrobial, antiviral, antifungal activities of lactoferrin, and the search for the possibility of using this compound for the treatment and prevention of the new coronavirus infection SARS-CoV-2, as well as for the prevention of postCOVID complications, has begun. In recent years, the antitumor activity of lactoferrin has been actively studied, as well as the prospects for its use as a biomarker for early diagnosis of neurodegenerative diseases. Lactoferrin can play a special role in the delivery of drugs to target organs, as well as in the manufacture of functional food products and various drugs for both humans and animals.Conclusion. Thus, the performed theoretical study and the data obtained on a wide spectrum of biological activity of lactoferrin confirm the prospects and expediency of the development of formulations and technology of drugs, functional food products, veterinary drugs and animal products based on lactoferrin.
Introduction. Curcuminoids are natural polyphenolic colorants with a wide spectrum of pharmacological activity. Modern hybrid and classical methods are used for the determination of curcuminoids. However, the problem of the analysis of curcuminoids in the composition of plant and medicinal objects remains relevant. In this work, capillary electrophoresis (HPCE) in the variant of micellar electrokinetic chromatography with diode array detection (MEKC/DAD) was used as such a method. Aim. The purpose of this analysis is the choice of optimal conditions for the separation of curcuminoids using capillary electrophoresis in the form of micellar electrokinetic chromatography. Materials and methods. Separation of curcuminoids was carried out on an Agilent 7100 CE capillary electrophoresis instrument with a diode array detector and an Agilent Chem Station monitoring and data acquisition system. Borate buffer (20 mM, pH 9.3) with the addition of sodium dodecyl sulfate – SDS (30 mM) in ratios of 1 : 1 was used like the electrolyte. The sample was injected hydrodynamically – 50 mbar/3 sec, electrode voltage is +25 kV, quartz capillary – total capillary length/effective capillary length = 30/40 cm, ID = 50 µm, capillary temperature +20 ° С. The output of curcuminoids was monitored at the wavelength of the diode-matrix detector – λ max = 425 nm/4 nm, the refereed wavelength is 360 nm/100 nm. Results and discussion. Curcuminoids in a borate buffer solution with the addition of SDS are practically not separated, which is associated with a high activity of the electroosmotic flow, to suppress which 95 % ethyl alcohol was added. In the course of research, it was found that the addition of ethyl alcohol in an amount of 20 % relative to the buffer solution makes it possible to separate the mixture of curcuminoids. Conclusion. Thus, the conditions for the separation of the total curcuminoids by the HPCE method in the variant of micellar electrokinetic chromatography (MEKC) were selected. It has been established that for the separation of curcuminoids by this method, it is necessary to use an electrolyte consisting of a mixture of equal volumes of borate buffer (20 mM) and sodium dodecisulfate (30 mM) and ethyl alcohol in an amount of 20 % of the electrolyte volume. A further increase in the concentration of ethyl alcohol in the electrolyte is unreasonable, since it can adversely affect the stability of micelles.
A great variety of components in multivitamin preparations containing folic acid, and a variety of test methods and conditions of folic acid determination proposed by manufacturers, require alignment of test procedures for products with similar composition.The aim of the study was to compare the results of experimental verification of folic acid determination procedures which use reversed phase high-performance liquid chromatography (RP HPLC) with isocratic elution mode. Materials and methods: The Agilent 1260 Infinity II LC system with a diode array detector (280 nm), isocratic elution mode, C8- and C18-bonded silica gel chromatographic columns, model mixtures containing folic acid, cyanocobalamin, ferrous sulfate, and potassium iodide, were used in the study.Results: The lowest relative standard deviation of the folic acid peak area (RSD=0.09%), and the lowest asymmetry factor (As=1.04) for folic acid were observed for the model mixture “ferrous sulfate+folic acid+cyanocobalamin” and the following test conditions. Column: 250×4.0 mm, silica gel for chromatography, octylsilyl (C8), endcapped; mobile phase: methanol‒phosphate buffer (12:88), pH 6.6; column temperature: 25ºС. The study demonstrated the feasibility of using these conditions for determination of pteroic acid impurity with simultaneous precipitation of interfering ferrous ions, using ethylenediaminetetraacetic acid solution, pH 9.5, as a solvent.Conclusions: RP HPLC can be recommended as an optimal aligned test procedure for determination of folic acid in combination products. It is recommended to use a solution containing folic and pteroic acids for system suitability testing.
We developed a method for quantitatively analyzing some components of the unsaponifiable fraction of edible oils and validated its characteristics. The component composition of the unsaponifiable fraction of 26 edible oil species was studied by gas chromatography/mass spectrometry. Squalene, sterols, and triterpene alcohols were quantified in oils using cholestenol as an internal standard. Some correlations were found between the structure of sterols and triterpene alcohols and their retention indices and electron impact fragmentation. More than 150 chemical compounds—unsaponifiable components—were identified. The method can be used to estimate the concentration of sterols, triterpene alcohols, and squalene in edible oils and determine the authenticity of oils by the characteristic profiles of the unsaponifiable fraction.
Electrothermal atomic absorption spectrometry (ETAAS) is one of the most well-known methods for determining trace amounts of elements in natural objects, since it is simple in instrumentation and rather cheap. It is especially promising for the pharmaceutical analysis of medicinal plant raw materials for quality control purposes. A new unified ETAAS technique for the determination of cadmium, lead and arsenic in solutions obtained after acid decomposition (with HNO3) of plant raw material under microwave heating conditions has been developed. It was shown that cadmium can be determined without a modifier, while for lead and arsenic the presence of a modifier is necessary. Inexpensive and widely available substances were proposed as modifiers: 1% solution of ascorbic acid (for lead), 1% solution of Ni(NO3)(2) (for arsenic), which were previously used in the Russian Federation exclusively in geochemical studies. The conditions for the preparation of the analysed samples are proposed. The using prospects of the developed technique for the natural substances quality control, as well as its universality for the analysis of plant raw material of various morphological groups have been demonstrated. The technique was validated in terms of specificity, accuracy, precision, repeatability, linearity, range, robustness. The technique can be recommended for determination of these ecotoxicants accumulation in wild-growing and cultivated medicinal plants.
Laurel noble – Laurus nobilis L., a plant whose leaves are widely used in cooking and are used in folk medicine. L. nobilis L. leaves contain more than 80 volatile components, represented mainly by monocyclic monoterpenes. The identification of more and more new therapeutic properties of the plant testifies to its incompletely undisclosed therapeutic potential. However, despite the impressive therapeutic potential of the plant, it is not used in domestic scientific medicine. The aim of the study: To describe the spectrum of types of pharmacological activity of L. nobilis L. and selection of the optimal extractant for the extraction of essential oil from the leaves of the object under study. Materials and methods: Laurel leaves were used as the test material. The essential oil from the leaves was obtained by extraction with freons, which are methoxynonafluorobutane and fluoroketone. The extractant for comparison was n-hexane. The method of studying essential oils was chromatography- mass spectrometry. Chromatography was performed on a gas chromatograph – mass spectrometer – GCMS-QP2010 Ultra, Shimadzu, Japan. Ionization is carried out in the electronic shock mode, detection by the total ionic current (SCAN) in the programmed temperature mode. Results: According to the literature, the essential oil of L. nobilis L. leaves have a pronounced antibacterial, antioxidant and antiinflammatory effect. Polyphenolic compounds of L. nobilis L. leaves are represented by flavonoids, derivatives of kaempferol and quercetin. It is believed that flavonoids are responsible for hypoglycemic, insular protective, antioxidant effects. The results of chromatography showed that the essential oil is represented mainly by 12 compounds, the dominant of which were 1.8-cineole (eucalyptol), alpha-terpenyl acetate and methyleugenol. During chromatography, it was also found that the optimal extractant is methoxynonafluorobutane, which extracts terpenoids with the highest yield. The prospects of using freons as agents for obtaining essential oil from laurel leaves have been shown. The composition of the essential oil isolated by freons from the leaves of laurel was determined by the method of gas chromatography-mass spectrometry. The results of chromatography showed that in the obtained freon extracts, 1.8-cineole (eucalyptol), alpha-terpenyl acetate and methyleugenol were dominant, which is close in composition to the native essential oil, according to literature data. Conclusion: The prospects of using freons as agents for extracting essential oil from L. nobilis L. leaves were shown. During chromatography, it was found that the optimal extractant is methoxynonafluorobutane, which extracts volatile components with the highest yield compared to fluoroketone and n-hexane; in addition, methoxyfluorobutane is non-toxic compared to n-hexane.
Авторы были добавлены в раздел «Вклад авторов». Вместо: Г. Бакореза, Р. А. Абрамович, Н. Н. Бойко, С. Лазар разработали схему выделения липофильных и гидрофильных компонентов семян N. sativa L. Д. И. Писарев, О. О. Новиков, А. В. Хромов и О. Г. Потанина провели аналитическое исследование выделенных фракций семян N. sativa L., обработку данных и интерпретацию результатов. Все авторы принимали участие в обсуждении результатов и написании текста статьи. Исправлено на: Г. Бакореза, Р. А. Абрамович, Н. Н. Бойко, С. Лазар разработали схему выделения липофильных и гидрофильных компонентов семян N. sativa L. С. В. Горяинов, В. А. Ивлев, С. Эспарса, Д. И. Писарев, О. О. Новиков, А. В. Хромов и О. Г. Потанина провели аналитическое исследование выделенных фракций семян N. sativa L., обработку данных и интерпретацию результатов. Все авторы принимали участие в обсуждении результатов и написании текста статьи.
The development of an ophthalmic therapeutic system includes research on the spatial structure of soft contact lens polymers and the study of the processes of saturation and release of medicinal substances from them. This allows you to determine the methods of saturation of contact lenses with medicinal agents and will open up new opportunities in the treatment of ophthalmological diseases. The purpose of this preliminary fragment of large-scale research was to study the surface structure of soft contact lenses made of various polymers. The following polymers were used in the work: Nelfilcon A, Hilafilcon B, Nezofilcon A, Etafilcon A, Lotrafilcon B. The following pharmaceutical substances were used: Brimonidine Tartrate, Betaxolol Hydrochloride, Pyridoxine Hydrochloride. The surface structure of soft contact lenses was studied using atomic force microscopy. Each material under study has a different surface character, which together with the differences in pore properties determines its individuality. Based on this, it should be assumed that the surface of soft contact lenses affects the possibility of their potential use as a means of delivering drug agent molecules to the eye tissues. In all cases of soft contact saturation, the highest absorption capacity was demonstrated by Hilafilcon B and Etafilcon A with a similar surface.
Introduction. Seeds of Nigella sativa L. are widely known as a source of fatty oil with a very rare component-thymoquinone. The therapeutic potential of biologically active compounds of plant seeds covers a positive effect on the gastrointestinal tract, cardiovascular and immune systems. In addition, hypoglycemic, antioxidant, antitumor, oncoprotective, immunomodulating effects were found in thymoquinone. In addition to fatty oil and thymoquinone, a number of other significant compounds are present in the seeds, which also make up their own pharmacological asset. Aim. Study was to develop a processing flow chart and analyze the lipophilic and hydrophilic components of the seeds of N. sativa L.Materials and methods. The following methods were used as analytical methods: gas-liquid chromatography with a flame ionization detector - for the analysis of sterols and triterpenes; chromatography-mass spectrometry (gas-liquid chromatography with mass spectrometric detection) - for the study of essential oil; chromatography-mass spectrometry (high performance liquid chromatography with mass spectrometric detection) - to study flavonoids. To obtain individual fractions of biologically active compounds of seeds of N. sativa L., fractional extraction was used.Results and discussion. The principle of this approach in this case is to extract the entire lipid complex of seeds with n-hexane, followed by removal of the extractant. The thickened hexane extract is treated with ethyl alcohol, which extracts unsaponifiable compounds - terpenes, quinones, sterols and does not dissolve triacylglycerides. The seed meal remaining after hexane extraction is treated with ethyl alcohol 70 %, into which hydrophilic molecules, in particular flavonoids, pass.Conclusion. After transesterification, 5 compounds were identified in the lipophilic fraction of saponifiable lipids, the linoleic and oleic acids being dominant. A characteristic feature of this fraction is the presence of cis-11,14-eicosadiene acid, which can act as a marker element of the fatty oil of the seeds of N. sativa L. Sterols and triterpenes were found in the unsaponifiable fraction. The major component of this fraction is β-sitosterol. In addition to the indicated sterol, campesterol and stigmasteri are present. Triterpenes are represented by cycloartenol and its derivatives. Simple phenols, quinones and monoterpenes were found in the essential oil complex, p-cymol, thymoquinone and α-thuyen predominate. The hydrophilic fraction of the seeds of N. sativa L. includes flavonoids of the methoxylated series of flavones and kempferol glycosides.
The theses contain a criminological analysis of indicators for measuring intellectual property crimes for 2019-2020 on the basis of official data from criminal statistics and generalized convictions.
Introduction. This article provides a tentative justification of use of soft contact lenses as a carrier of ophthalmological solutions to eye tissues.Aim. The aim of the research is to develop the composition of the ophthalmic transport system for the treatment of glaucoma. Also, the proposed manufacturing algorithms were proposed for drug loading ophthalmological solutions.Materials and methods. Preparation of sodium hyaluronate solution was carried out based on the methodology described in EP 7.0 [01/2011:1472] (Sodium hyaluronate).Results and discussion. The conducted investigation with the purpose to justify a concentration of sodium hyaluronate helped to determine its concentration that gives the viscosity level as close to the upper limit stated in Russian Pharmacopoeia as possible. Buffer solution was chosen with criteria to use as less components in ophthalmological solution as possible. Also, it was found out that the more components are added to the viscous solution, the more viscosity level is decreased. Thus, initial viscosity of solution containing sodium hyaluronate was 149.59 mm2/s, and after addition of active pharmaceutical substance it dropped down to 88.49 mm2/s and 81.36 mm2/s for model solution number 1 and 2, respectively. After addition of citric acid and disodium hydrophosphate, the viscosity of model solution was found to be 78.11 mm2/s and 75.28 mm2/s for model solution number 1 and 2, respectively.Conclusion. As a result of the studies, two alternative model compositions of an ophthalmic solution for the saturation of soft contact lenses for the treatment of glaucoma were proposed. The choice of active pharmaceutical substances, and excipients has been justified. Technological procedure of preparation of model solution was described and explained, where the most attention was paid on dissolving of sodium hyaluronate in purified water.
The purpose of this work was the studying and modeling of the extraction properties of the sorbitol-based natural deep eutectic solvent (NADES) and sorbitol-based solvents in regard to biologically-active substances (BASs) from Glycyrrhizae roots using theoretical fundamentals based on the laws of statistical physics, thermodynamics, and physical chemistry previously developed by us. In our studies, we used Glycyrrhizae roots, simple maceration, plant raw material:solvent ratio 1:10 w/v, temperature 25 °C, extraction time 24 h; standards of licuroside and glycyram; RP HPLC, differential scanning calorimetry, integral dielectric, impedance and conductivity spectroscopy method of analysis; the following solvents: sorbitol-based NADES sorbitol:malic acid:water (1:1:3 in molar ratio), a modified solvent based on NADES sorbitol:malic acid:water:glycerin (1:1:1:1 in molar ratio) and sorbitol-based solvents sorbitol:ethanol:water at different ratios. It has been found that regression equations for sorbitol-based solvents in coordinates predicted by the theory have a high value of determination coefficient that equals to R2e = 0.993 for glycyram and R2e = 0.976 for licuroside. It has been found that the extraction properties of sorbitol-based NADES with a dielectric constant (ε) equal to 33 ± 2 units are equivalent to those of the sorbitol:ethanol:water solvent with ε = 34 units, and the extraction properties of modified solvent based on NADES with ε = 41 ± 2 units are inferior to those of the sorbitol-ethanol-water solvents with maximum value of BASs yield with the dielectric constant range 40 ÷ 50 units. The theoretical fundamentals suggested provide a possibility for an explanation of the mechanism, quantitative description of the extraction properties of the solvent, and target search of the optimal solvent by its dielectric constant.