Obtaining a dry extract of fenugreek seeds and the creation of a biologically active food supplement based on it

The article discusses the possibility of obtaining a biologically active food supplement based on dry extract of fenugreek seeds obtained by microwave drying. As a result of the study, optimal filler and granulating liquid for this object were selected.В статье рассмотрена возможность получения биологически активной добавке к пище на основе сухого экстракта семян пажитника сенного полученного методом СВЧ сушки. В результате исследования были подобраны оптимальные наполнитель и гранулирующая жидкость для данного объекта

DISSOLUTION PROFILE STUDIES FOR RAMIPRIL AND LERCANIDIPINE FIXED-DOSE COMBINATION

This article describes the results of the development of composition and technology of a combined drug, containing lercanidipine and ramipril, affording equivalent dissolution kinetics with original drugs. The comparative release profiles of the active pharmaceutical ingredients are shown. The choice of a solid dosage form in the form of bi-layer tablets was substantiated

Tablet Development for a Hydroscopic Drug Using Solid Dispersion

Introduction. Traumatic brain injury is a damage to the brain from an external mechanical force, possibly leading to permanent or temporary impairment of cognitive, physical, and psychosocial functions. It is a leading cause of death and disability among children and young adults. In connection with the above, the objective of developing new, more effective nootropic and antiasthenic drugs in the framework of restorative neurology is considered as one of the priority tasks of medical science in Russia.Aim. Development the composition and technology of tablets containing a hygroscopic substance using solid dispersions.Materials and methods. The pharmaceutical substance of a diethylaminoethanol derivative having antihypoxic, neuroprotective, adaptogenic and antioxidant effects is a hygroscopic powder. PEG 6000 was chosen as a matrix for solid dispersion production. Solid dispersions were obtained by high shear mixing and hot-melt extrusion. The technological properties of granulate and the quality indicators of the tablets were determined according to the methods described in the State Pharmacopoeia of the Russian Federation (14th edition).Results and discussion. The lactose mixed with the DEAE-PEG composition alloy improve the technological properties of granulate.Conclusion. A decrease water-absorbing ability of DEAE was achieved using PEG 6000 as a matrix carrier. The increase PEG content did not lead to a significant change in the kinetics of the release of DEAE from tablets

Kinetics of Extraction of Dioscine from Vegetable Raw Materials in Vibrocavitation Homogenizer

Introduction. In recent years, substances extracted from plant materials have been widely used in the pharmaceutical, cosmetic and food industries. Such substances are used as solutions, dry extracts for the manufacture of medicines, dietary supplements, cosmetic creams, food additives in various forms – tablets, capsules, solutions, granular powders. The extraction of valuable substances from plant materials is carried out using the extraction process, which is carried out by various methods and in apparatuses of various designs. Earlier, a comparative study of the extraction of dioscin from fenugreek by various methods was carried out: in devices with a stirrer, in an ultrasonic field, supercritical, fluid СО2 extraction, and in a vibro-cavitation homogenizer. It is shown that the most effective method is the extraction carried out in a vibrocavitation homogenizer.Aim.To analyze the kinetics of the extraction of dioscin from fenugreek seeds, to determine the optimal values of the required degree of grinding of the raw materials, working temperature, the concentration of ethyl alcohol in the solution and the rotational speed of the rotor of the vibrocavitation homogenizer. Determine the effective mass transfer coefficient responsible for the intensity of mass transfer inside the particles.Materials and methods. An experimental study of the extraction of valuable components from plant materials was carried out in a laboratory unit with a vibrocavitation homogenizer of periodic action. As raw materials were used seeds of hay fenugreek, ecotype of Morocco, acquired in the company Fitokasa, Casablanca (Morocco), which we used for research. Commodity analysis showed that raw materials comply with the requirements of the State Pharmacopoeia XIVth edition. As extractants, aqueous solutions of ethanol with an alcohol concentration of 40, 50, 60, 70, 80, and 90 %. The analysis of the kinetics of the process was based on the following ideas. Extraction begins with the surface of the particles of plant material. As the extracted component moves into the volume of the solution, the extractant penetrates into the internal pores of the particles, and the surface on which the extractant and the extracted component interact is gradually shifted into the individual particles. In this case, the resistance to mass transfer in the region between the specified surface and the outer surface of the particle increases over time.Results and discussion. An analysis of the results shows that the rotor speed significantly intensifies the process. In addition, the influence of the rotor speed is most pronounced at the initial stage of the process, when the surface layers of particles of plant material are extracted. It was also found that the resistance to mass transfer inside particles increases significantly as it approaches the final stage of the process, and with an increase in the rotor speed, it increases, especially at the initial stage of the process, which is associated with the intensity of cavitation and the weakening of its effect as the process deepens inward particles.Conclusions. The obtained dependences are necessary to determine the duration of the extraction process in a batch mode, or the average residence time of seeds in the working volume when organizing the process in a continuous mode

The Analysis of Process of Crushing in the Vibrocavitational Homogenizer

Introduction. Vibration cavitation homogenizers are increasingly used in various industries, including the pharmaceutical industry – for the preparation of creams, gels to give them a homogeneous composition, and more recently for the extraction of valuable substances from plant materials. As we have shown earlier, a comparison of the extraction of dioscin from fenugreek seeds, carried out in devices of various designs, under the same conditions for organizing the process showed that the most effective method was the extraction method in a vibro-cavitation field. Obviously, this is due to the fact that cavitation reduces the diffusion resistance of the process and, thus, increases the intensity of the process of transferring the mass of a substance from the solid phase to the solution. However, the extraction process in apparatus of this type is complex and is accompanied by crushing of seeds, which leads to a change in the dispersed composition of the solid phase.Aim. Conduct a theoretical and experimental analysis of the process of grinding hay fenugreek seeds particles in a vibrocavitation homogenizer, accompanied by the extraction of biologically active substances, as well as obtaining dependences that allow evaluating the contribution of grinding to the formation of the dispersed composition of the meal in this apparatus and determining the average particle size as a result of crushing. In earlier works, using the example of the extraction of dioscin from fenugreek seeds, it was shown that an increase in the rotor speed increases the yield of biologically active substances. However, fine grinding of raw materials often leads to the formation of a sediment layer that pollutes the solution with ballast substances and complicates its purification, and also reduces the yield of biologically active substances, therefore, the study of this process is necessary to control the dispersed composition in order to ensure the highest extraction efficiency in devices of this type.Materials and methods. The first stage of the study was the theoretical analysis of the grinding process, since it is a special case of a large class of processes in which the dispersed composition of the solid phase is not constant. Therefore, in this work, for the mathematical description of particle grinding, a model is used that takes into account the kinetic features of the process under consideration. An experimental study of the extraction of valuable components from plant raw materials was carried out in a laboratory setup with a vibro-cavitation homogenizer of periodic action. As a raw material, we used fenugreek seeds purchased from LLC «Stoing», Moscow (Russia), which we used for research. Commodity analysis showed the compliance of raw materials with the requirements of the GF XIV edition. The initial, aqueous solution of ethanol (volume concentration 60 %) with fenugreek seeds was loaded into glass 6, in a volume of 0.2 liters, then the rotor of the apparatus was brought into rotation and brought to a given rotation frequency. The experiments were carried out at a rotation frequency of 1000, 3000 and 5000 rpm (16.7; 50 and 83.3) 1/s. At each value of the rotor speed, the process time varied in the range from 0 to 50 minutes, and the process was carried out for 60, 120, 180, 240 and 300 seconds. Studies carried out for 5 minutes or more showed that the dispersed composition of the meal practically does not change over time, but significantly depends on the rotor speed. Thus, after 5 minutes, a certain stabilization of the dispersed composition occurs and further residence of the material in the apparatus does not lead to a noticeable change in the dispersed composition. After each experiment, the meal was taken, dried, and sieve analysis of the dispersed composition was carried out.Results and discussion. Based on the results obtained by processing the experimental data according to the equation, the values of the average probability of particle crushing were calculated and, as it turned out, it practically does not depend on time, but depends only on the rotor speed. The dependence of the change in the average probability of particle grinding at different rotor speed was obtained. The analysis of these results showed that the value of the average probability of particle grinding in the cavitation homogenizer increases with an increase in the rotor speed, which is quite expected, since the frequency of contacts of particles with the working organs of the apparatus increases. In addition, the obtained dependence for the average probability of particle crushing is linear. This Expression quite accurately describes the values of the change in time of the relative mass of particles in the working range n = 16.7 – 83.3 1/s. Taking these values into account, the experimental and calculated results are in good agreement.Conclusions. The proposed approach and the results obtained can be used to assess the dispersed composition of particles obtained in other designs of devices of similar action

MODERN COATING TECHNOLOGIES FOR DRUG ELUTING CORONARY STENTS (REVIEW)

The review is devoted to modern polymer coating technologies for drug-eluting coronary stents. The most promising technologies and also the methods which are the subject of experimental investigation have been described. Key advantages and disadvantages of the dip, spray, layer-by-layer, ink-jet, and plasma coating, electrostatic coating and electrochemical deposition methods have been shown. The examples of clinically proven coronary stents have been given. The review illustrates the current level of polymer coating technologies for stents, and also their further development trends

Development of the Composition and Technology of New Neuroprotective Drug Tablets Using Fractional Factorial Design

Introduction. The creating an effective and safe domestic neuroprotective medicines with a complex of pleiotropic effects realized through specific orphan receptors (SUCNR1, HCA2) of glial cells, is a pressing problem of modern pharmacology and a promising possibility of pharmacotherapy of brain injury and cerebrovascular diseases. Ideally, the medicine should helps restore lost cognitive functions and physical performance after damage to the central nervous system, and its use should improve the quality of life of patients and reduce the risk of complications.Aim. To develop composition and technology of a new medicine tablets with neuroprotective effect, using fractional factorial design of experiment and the Harrington desirability function.Materials and methods. The shape and size of particles, physicochemical (solubility, melting point) and technological properties (bulk density, compressibility factor, fractional composition, hygroscopicity) of the pharmaceutical substance of DEAE derivative were studied according to the methods described in the State Pharmacopoeia of the Russian Federation (14th edition). A three-factor fractional plan based on the 4 × 4 Latin square design for selection a scientifically based composition of solid dosage form was chosen. 16 experiments to test the significance of the factors were carried out. The tablets obtained according to the planning matrix were investigated for disintegration; tablet crush resistance, friability, and hygroscopicity. To optimize the quality of the tablets, the generalized Harrington desirability function was used.Results and discussion. The study of the physicochemical and technological properties of the DEAE derivative substance showed that it is a highly hygroscopic, amorphous, white or pale yellow, odourless powder, prone to the formation of agglomerates. The powder is very easily soluble in water. Taking into account the values of the general desirability function, the best result was shown by sample № 4 consisting of mannitol, calcium stearate, and partially pregelatinized maize starch.Conclusion. The physicochemical and technological properties of the DEAE derivative were studied. The DEAE derivative is a highly hygroscopic substance. Via the method of mathematical planning of the experiment the composition of DEAE derivative tablets was selected and scientifically grounded: DEAE derivative 60 mg, mannitol, partially pregelatinized maize starch, calcium stearate. The average tablet weight is 300 mg. The parameters of pressing tablets were selected

Comparative Analysis of Perspective Extragation Methods for Receiving Extractions from Fenugreek Seeds

Introduction. Today, innovative technologies are widely used in pharmacology (in particular, in the production of herbal preparations), in cosmetology (obtaining various extracts and oils, complex preparations), as well as in the food industry (as natural dyes, etc.). Plant extracts with a high level of risk do not have a harmful effect on the human body, except that they provide environmental safety, which creates a special interest for the pharmaceutical industry . vibrocavitation and supercritical fluid СО2 extraction.Aim. The choice of the optimal level of extraction to obtain a high level of fenugreek seeds.Materials and methods. Obtaining a vibrocavitation extract with an experimental vibration-explosive installation made at the Department of Processes and Apparatus of the St. Petersburg State Technology Institute. Extracts at a temperature of 60±2 ºС. The frequency of revolutions of the homogenizer ranged from 1000 to 5000 rpm. Ultrasonic impact using ultrasound unit I100-6/4 Ultrasonic effect on solid plant material with an intensity of 22 kHz for 60 minutes. The time of extraction in a vibro-cavitation extractor-homogenizer was studied for optimal values.Supercritical fluid СО2-extraction is obtained in two versions with the use of extragent (96% ethanol in the presence of carbon dioxide: ethanol 9:1) and without it. Extraction of the sound of a supercritical fluid extraction system with a 1-liter vessel. SFE1000-2-BASE with a kit for upgrading the SFE1000-2-BASE system to an SFE1000M1-2-FMC50 system (Waters, USA). The flow rate of the extractant was 60 g/min. Emergency listening for one hour and pressure 200, 300 and 400 bar. Extraction is observed three times. The obtained extracts indicate the amount of extractive substances according to article of Russian state pharmacopoeia 1.5.3.0006.15 «Determination of the content of extractive substances in plant raw materials and medicinal plant preparations». Quantitative determination of the saponin complex of parasitic seed seeds on an Agilent QTOF-6530 chromatograph with two ESI and APCI ionization sources according to Gravel et al.Results and discussion. Studies have allowed to determine the amount of extractives in the seeds and choose the most promising method. Conclusion. As a result of our research, it was found that the most promising extraction method for extracting seeds is a parasitic with vibration extraction at frequent revolutions of the homogenizer of 5000 rpm and an extraction time of 60 minutes

Study of Lercanidipine Drug Release from Medicine in Combination with Ramipril <i>in vitro</i> and <i>in vivo

Introduction. Hypertension is the most common non-infectious disease in the world. New clinical recommendations for the diagnosis and management of patients with arterial hypertension are considering the issue of prescribing combination therapy and prefer fixed combinations of drugs in a single pill. The study of the pharmacokinetics of medicinal substances and the consideration of their pharmacokinetic parameters today is a necessary step in the complex of work, both in the creation of new original medicines and in the application of known generic drugs, and this is primarily due to obtaining objective characteristics of all processes occur in the body of the animal (human) with the drug. Pharmacokinetics is assessed in individual studies or as part of efficacy, safety, and tolerability studies.Aim. The study of the release of lercanidipine from bilayer tablets containing two API (ramipril and lercanidipine) in the dissolution medium used for quality control in vitro and release in vivo, after oral administration of the drug to rabbits.Materials and methods. Studies have been conducted on the release of lercanidipine from the combined drug in vitro and in vivo. As a test system were used laboratory rabbits Soviet chinchilla breed. Pharmacokinetic parameters were determined.Results and discussion. A graph of the release of lercanidipine from the combined drug was constructed and the dependence of the concentration of this substance in the blood plasma of rabbits on time was revealed. Calculated pharmacokinetic parameters. An in vivo release study shows that the pharmacokinetics of lercanidipine are consistent with literature data.Conclusion. The test drug has all the advantages of a rational fixed combination of antihypertensive drugs and simplifies therapy, meets the requirements of the latest clinical guidelines

Arctic Edible Brown Alga <i>Fucus distichus</i> L.: Biochemical Composition, Antiradical Potential and Human Health Risk

Fucus distichus L. is the dominant canopy-forming macroalga in the rocky intertidal areas of the Arctic and Subarctic. In the present study, the impact of the geographic location of F. distichus collected in the Baffin Sea (BfS), Norwegian Sea (NS), White Sea (WS), and Barents Sea (BS) on the variations in biochemical composition, antiradical properties, and health risk was evaluated. The accumulation of main carbohydrates (fucoidan, mannitol, and alginic acid) varied from 335 mg/g dry weight (DW) in NS to 445 mg/g DW in BS. The highest level of the sum of polyphenols and flavonoids was found in samples of F. distichus from WS and was located in the following ranking order: BS F. distichus samples, Cd, Cr, Pb, and Ni were not detected or their concentrations were below the limit of quantification. According to calculated targeted hazard quotient and hazard index values, all studied samples of Arctic F. distichus are safe for daily consumption as they do not pose a carcinogenic risk to the health of adults or children. The results of this study support the rationale for using Arctic F. distichus as a rich source of polysaccharides, polyphenols, and flavonoids with important antiradical activity. We believe that our data will help to effectively use the potential of F. distichus and expand the use of this algae as a promising and safe raw material for the food and pharmaceutical industries