No 1 (2017)
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PHARMACEUTICAL TECHNOLOGY AND NANOTECHNOLOGY
52-57 541
Abstract
Microcapsules consisted of biocompatible components- bovine serum albumin and tannic acid were made using Layer-by-Layer encapsulation method. Process of microcapsule formation was studied. Poly(allyl)amine hydrochloride (PAH) was included into the microcapsules and process of its release into medium with neutral and alkaline pH and trypsin was studied. The ability to control release of model substance PAH from these capsules with the help of trypsin was shown.
58-64 782
Abstract
Release profiles were investigated from tablets of ibuprofen in media simulating the conditions of the gastrointestinal tract. Carbopol Ultrez 21 was used as prolongator polymer. The formulations with three different neutralizing agents [L-lysine, N-methylglucosamine (MGA), sodium hydrocarbonate] in several carbopol : neutralizer ratios were tabletted with using the wet granulation method. Faster release of ibuprofen has been observed in formulations with sodium hydrocarbonate, than in formulations with amine containing L-lysine and MGA. Both the amount and neutralization rate of carbopol influence significantly on rate and extent of ibuprofen release from tablets. Carbopol swelling rate grows up with increasing of neutralizer content in tablet.
66-69 578
Abstract
This article presents the results of modeling and optimization of the process of producing carotenoids by the example of β-carotene. The complex quantitative estimation of five technological parameters influence on the exit of individual carotenoid is conducted by the method of the mathematical planning of experiment. The complex quantitative estimation of influence of five technological parameters is conducted on the exit of individual carotenoids the method of the mathematical planning of experiment. The goal is achieved by constructing a mathematical model based on regression equations of the first order. We prove the adequacy of the work produced mathematical models and optimization carried out the process of obtaining β-carotene by a steep ascent.
70-77 779
Abstract
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.
MODIFICATION AND METHOD OF DETERMINING OF ACTIVE GROUPS OF HEPARIN ON THE SURFACE OF SUTURE MATERIAL
78-81 628
Abstract
The coating with the application of biopolymers of polyhydroxyalkanoate class and unfractionated heparin is perspective for giving thromboresistant properties to a surgical suture. We used a chemical reaction which was performed in several stages to give strength and uniformity to the antithrombotic coating. The first stage was the initiation of the centers of graft copolymerization on the surface of the material by ozonation. At the second stage we created an additional underlayer of polymethacryloylchloride having active acid chloride groups in its content, which can form strong covalent links with heparin. The third stage was a chemical grafting of heparin on the formed underlayer from its solution in bicarbonate buffer at a reduced temperature. Quality assessment of heparin addition to the suture material was evaluated by Raman scattering spectroscopy. The obtained results showed that the modification of the suture material with the help chemical initiation method allows to firmly secure the heparin on the surface of the suture.
A. V. Belyatskaya,
I. I. Krasnyuk,
I. I. (jr.) Krasnyuk,
O. I. Stepanova,
L. A. Korol,
O. V. Rastopchina
82-85 2103
Abstract
The article highlights the importance of the pharmaceutical drugs manufacturing. There are analysis of prescriptions coming from pharmacies in Moscow. There are investigated the structure of extemporaneous drugs in accordance with the classification of the state of aggregation. The article revealed the use of ready-made drugs in extemporaneous technology of powder for children manufacturing. This circumstance is due to the lack of modern pharmaceutical substances in pharmacies. The article deals with the legal aspect of the problem.
88-92 2925
Abstract
One of the major nuclear medicine agent is radiopharmaceutical (RPh) which is a composition comprising a radioactive isotope in certain chemical form. Quality control, namely the determination of radiochemical purity of radiopharmaceuticals produced in a medical institution, prior to administration to the patient is mandatory in all developed countries of the world since the mid-1980s. In our country, virtually the same procedure has been mandatory since the beginning of 2016, along with other measures, the implementation of which should guarantee the high quality and safety of nuclear medicine procedures according to the Order of the Ministry of Health of the Russian Federation from 27.04.2015 N 211n «On approval of the radiopharmaceutical preparation directly in medical institutions», which came into force from January 01, 2016. This article presents the main approaches to the implementation of quality control (determination of radiochemical purity) of radiopharmaceuticals manufactured directly in the medical institutions.
ANALYTICAL AND QUALITY CONTROL METHODS
A. M. Frolova,
D. A. Grafov,
V. S. Tukova,
E. V. Vorfolomeeva,
N. A. Keryanov,
E. V. Feelonenko,
A. V. Panov,
M. A. Green,
S. A. Kedeek
94-102 937
Abstract
In this paper key indicators due to Pharmacopoeia XIII [1] that can be used to standardize the cationic derivative of bakteriopurpurinimid as pharmaceutical substance (PS) are presented. The prime application of this compound to be a photosensitiser for antimicrobial photodynamic therapy (PDT).
104-107 900
Abstract
There are results of the possibility of applying a chromatographic column Zorbax NH2 150х4,6 mm (5 µm) to separate the esters of 4-hydroxybenzoic acid (parabens). Separation of test compounds on the column with aminosorbents in hydrophilic interaction chromatography is possible at a content of more than 95% of acetonitrile in the mobile phase. The resolution between peaks of parabens in a hydrophilic interaction liquid chromatography is substantially less than in a reverse-phase chromatography. In contrast to the amino nitrile groups Zorbax XDB CN columns practically haven’t affinity for the phenolic hydroxyl groups of parabens in a hydrophilic interaction liquid chromatography. Chromatography column Zorbax NH2 can be used to detect a normalized impurity in paraben - 4-hydroxybenzoic acid [mobile phase: acetonitrile - 1% acetic acid in water (80:20)].
108-110 665
Abstract
The aim of the research was investigation of the antimicrobial and antifungal activity of the reaction products of 2,5-substituted 4-hydroxy-6H-1,3-oxazin-6-ones with N-nucleophiles. The activity of the obtained substances was tested on the test-cultures Staphylococcus aureus, Escherichia coli и Candida albicans, respectively. The significant antifungal effect of the studied compounds was revealed.
112-114 1137
Abstract
The reaction of formylation by Vilsmeier - Haack was held. The effect of excess phosphorus oxychloride in the direction of the reaction. Optimal conditions were conducting formylation reaction to obtain a single compound with a high yield. The result of the reaction product mixture was conducted chromatographic separation on a column packed with silica gel 60 Silica.
116-118 516
Abstract
New amino derivatives of 5,7-dichloro-4,6-dinitrobenzofuroxan where synthesized. IR and elemental analysis proved their structure. Their acaricidal and bacteriostatic activity against Staphylococcus and Escherichia coli was studied. As a resulti compounds showed a high pharmacological activity, surpassing the reference drug. Relevant search of new compounds among the amino derivatives of 5,7-dichloro-4,6-dinitrobenzofuroxan was showed.
120-124 1019
Abstract
Investigation of the phenolic compounds of catnip herbs (Nepeta cataria L.) the flora of the North-West region of Russia by thin-layer and paper chromatography was carried out. Have been identified 11 compounds of the phenolic nature from which 6 substances of flavonoid nature (rutin, luteolin, cynaroside, hyperoside, quercetin and apigenin), 3 hydroxycinnamic acids (caffeic, chlorogenic and rosmarinic) and 2 phenolcarbolic acids (gallic and vanillic). The results of the study create the preconditions for further study of quantitative content of phenolic substances, establishing markers and subsequent standardization of medicinal plant raw materials.
126-129 1126
Abstract
The article presents the results of experiments in selection of juglona pericarp Juglans nigra L. and the study of its antibiotic activity against strains of Staphulococcus aureus and Escherichia coli as the most characteristic typical) representatives of gram-positive and gram-negative bacteria.
130-132 525
Abstract
A comparative study of the biologically active compounds (BAC) composition of alcoholic extracts of leaves and fruits was carried out by GLC-MS. It is shown that the BAC composition of leaves of Hedera caucasica is more extensive: the structure of 22 following compounds was determined: pinene, catechol, germacrene, sinapic alcohol, phytol, falkarinol, palmitic acid, oleic acid, linolenic acid and their esters; stigmasterol, lupeol, sitosterol, panaxadiol and panaxinon. The last three compounds - panaxidol, panaxinon and sitosterol - were not found in fruit extract.
134-137 739
Abstract
The study was carried out on the effect of the duration of ultrasonic influence on the total output of biologically active substances from the extraction of birch buds extractants of different polarity. The water, 70% aqueous solution of ethanol and mixture of isopropanol-water 60:40 were used as extractants. Extraction was conducted by maceration. Analysis of the obtained extracts was performed by the degree of extraction of extractive substances from raw materials, the content of ascorbic acid and carbohydrates.The intensification of the process of extracting the ultrasound is not depending on the extractant. There is an increase in overall yield of extractives, including carbohydrates, while the content of ascorbic acid in the extracts is reduced or completely absent.
138-143 695
Abstract
Developed and validated method of determining the amount of free and bound sugars picric method in the fruit of sea buckthorn. Validation assessment methodology characteristics: specificity, linearity, limit of detection, intra- and inter-laboratory reproducibility and repeatability demonstrated its compliance with the basic eligibility criteria. A determination of the amount of simple sugars and polysaccharides in the fruit of sea buckthorn of pharmacopoeial methods (ortsine and anthrone methods). It established the content of free and bound sugars in the fruit. The stability of the complex polysaccharide in the fruit of sea buckthorn on drying.
144-148 729
Abstract
The diagnostic features of the combination plant medicinal product powder «Lorpoliphyt», consisting of the flowers of calendula, horsetail, plantain leaves, grass St. John's wort, chamomile flowers, yarrow herb, rhizomes and roots of elecampane were determined by microscopic analysis. The description and photomicrographs of the morphological and anatomic diagnostic features were given. The obtained information will be used for the preparation of the normative documentation to combination plant medicinal product powder.
DRUG PRODUCTS EFFICACY AND SAFETY
150-155 935
Abstract
The kinetic evaluation of solubility of drug substances of different chemical and pharmacological groups (bendazol hydrochloride, lactose monohydrate and taurine) was conducted in aqueous solutions with different isotopic composition of hydrogen. The choice of solvent was made due to the fact that the replacement of purified water, containing 141,0 ± 0,9 ррm 21H(D) heavy isotope of hydrogen, to water with low content of 21H(D) can accelerate the solubility of the active process pharmaceutical ingredients (APIs), approximately in 1,5 times. The study was carried out by the laser light diffraction method, which is the basis of the Monograph.1.2.1.0008.15 SF RF XIII «Particle size distribution». In contrast to the existing methods of the pharmacopoeial analysis governing the visual assessment of the completeness of the solubility of the API, the laser diffraction method allows to get an objective assessment of the solubility of the API based on the change of the integral characteristics of dispersion over time.
156-162 835
Abstract
Dissolution test plays an important role at different levels of the development and manufacturing drugs as one of the major quality control tools and an integral part of In vitro tests in the study of drug release from the developed dosage forms. Article describes the basic parameters that should be considered in predictive dissolution tests, such as the selection criteria and the composition of biorelevant dissolution media, fluid dynamics, volume and transfer of the dissolution media.
164-166 696
Abstract
The results of Indomethacin release from the oral drug delivery systems based on interpolymer complexes with Eudragit® copolymers are presented. The release assessment was performed by two methods - flow-through cell (USP IV Apparatus) and the reciprocating cylinder (USP III Apparatus) in standard buffer solutions and biorelevant media. The release of indomethacin can be described as "intestinal" type. According to the results Indomethacin was released faster using USP III Apparatus due to stress-effect on the erosion type matrices.
168-176 907
Abstract
Active use of medical devices in contact with the blood stream has created the need to articulate the testing requirements of such products [1], various methods of modelling and assessment of potential complications. One of the most important aspects of testing such products is to evaluate their direct impact on blood. To obtain objective results of the study any modeling should be as close as possible to the situation of clinical use and reproduce the characteristics of blood flow. And also take into account the possibility of the use of anticoagulants and introducing in the model additional pharmacological preparations if they can influence the biochemical and physical characteristics of blood and their use is inextricably linked to the use of the product. The present article contains the results of the conducted scientific-research and experimental-design works on creation of the device to simulate the conditions of the blood flow to the preclinical testing of experimental samples of materials and devices intended for implantation in the human body for permanent or prolonged contact with blood
178-180 662
Abstract
Antihelminthic potency 10-getiryamides 1,4-decarboxylic acids was analyzed. 5 mL of 0.5% aqueous solution of investigated substances was placed in the Petrie dish and earthworms were immersed in a solution. Time of death of each species was determined according to the cessation of motion activity in response to mechanical irritation. Antihelminthic products Pirantel and Levomizol were used as references. Three substances have an antihelminthic effect exceeding the activity of Pirantel, one of them is twice as active as Levomizol.
182-186 963
Abstract
The issues (aspects) of bronchodilator and tocolytic actions of β₂-adrenoceptor agonists are reviewed. The data on short-acting and new long-acting β₂-agonists are presented. It is marked that it is necessary to use long-acting β₂-agonists and glucocorticosteroids concomitantly. Examples of clinical efficacy of locally produced β₂-adrenoceptor agonist salbutamol hemisuccinate in various dosage forms used as a bronchodilator for treatment of bronchopulmonary diseases, and also as a tocolytic for habitual noncarrying of pregnancy are given.
188-192 2600
Abstract
The review is dedicated to the description of interferon inducers - new generation drugs created by Russian scientists as a result of the screening of thousands of high- and low-molecular synthetic and natural compounds. The drugs selected for clinical applications have a common ability to induce synthesis of endogenous interferons (IFN) after introduction into the organism. The main advantage of interferon inducers is a wide spectrum of antiviral activity, which is based on etiotropic and immunomodulatory effects of this group of drugs. Special attention is paid to the results of clinical application of interferon inducers.
194-200 1318
Abstract
Interferons were one of the first groups of cytokines to be cloned and produced in bacteria. Interferon-based drugs are widely used for treatment of various infections, inflammatory and autoimmune diseases and malignant tumors. Clinical use of interferons can result in wide range of side effects, including unwanted influence on immune system of patients. Therefore it is important to study immunogenicity of interferones. The method of indirect ELISA was adopted and validated for analysis of antibodies to human recombinant interferon in mice blood plasma. The specificity was confirmed for mice antibodies. The linearity was 3.75-60.00 ng/ml, the detection limit was 2.19 ng/ml. Accuracy, interday and intraday precision did not exceed 15% at all concentration levels, that satisfies all validation requirements.
REGULATORY ISSUES
202-205 541
Abstract
Manufacturer of domestic medical immunobiological preparations audited three transport companies on their degree of compliance with the rules of the GDP. Required measures were offered to eliminate detected violations.
206-211 593
Abstract
The features of new products market launch by small innovative enterprises are the theme for careful study. The reason is the problems that Russia has nowadays - the need for reindustrialization, the economic diversification and the import substitution for improving the competitiveness of domestic producers, the necessity for increase of real employment, the reduction of qualified personnel’s leak. It acquires special relevance in the pharmaceutical industry as it is one of the most high-technology industries. The innovative small and medium-sized enterprises (SME) could play a big role in solving these problems, as they could initiate innovations, lead (alone or in a partnership with larger companies) high-technology research and development, promote the commercialization of innovations.
212-215 869
Abstract
This article provides an overview of the changes in requirements, processes, organization, planning, conducting and quality control of preclinical studies medicines, as well as making their results and archiving, approved by order of Ministry of Health of the Russian Federation from 01 April 2016 N 199n.
216-221 773
Abstract
In connection with the latest achievements of the theoretical crystallography the question of a potential patentability of new co-crystals of the known substances, as well as the estimation of their novelty and inventive step, becomes more and more relevant. In this article the author, basing on existing legal precedents, tries to analyze the question of patentability of co-crystals and to elaborate criteria, which help to increase chances for the patent granting. In addition, the author gives some recommendations with regard to the search directions for the new co-crystals.
HISTORY OF PHARMACY
222-228 855
Abstract
The paper presents the literature data on the occurrence of the term "Galenic medicines" and the contribution of K. Galen in the formation and development of pharmacy. The source of information were the materials published in domestic and foreign literature. We describe some of the recipes for medicines used by Galen in his practice. Discussed technological techniques and the most frequently used drugs. Specific examples are shown the knowledge and experience of Galen in the field of pharmacy.
ISSN 2305-2066 (Print)
ISSN 2658-5049 (Online)
ISSN 2658-5049 (Online)