Репозиторий Университета

Background High values of endogenous levels of magnesium (Mg) in the body and mechanisms of homeostasis regulation make it difficult to assess the bioavailability of these drugs. The aim of this study was to assess the Mg concentration in blood in volunteers and in erythrocytes in patients with hypomagnesemia. Methods The study included 20 healthy volunteers and 62 patients with chronic heart failure (CHF) I-III functional class (FC) NYHA classification. We studied the composition of Mgorotate and Mgorotate plus potassium (К)orotate. Blood sampling was carried out at 8 a.m. and within 10 h after administering the drugs. Measurement of Mg pharmacokinetic parameters: AUC (concentration of the active substance-time), and Cmax (maximum concentration) in volunteers and measurement of the concentration of Mg in erythrocytes of patients. Results The results indicated that both the AUC in volunteers and concentration of Mg in erythrocytes of patients are comparable, and the differences are not statistically significant. Conclusions The study showed that the standard method of calculating the AUC (total serum Mg) is insufficient for comparative evaluation of Mg absorption due to the high levels of its endogenous content and a small increase in concentration after taking the drugs. It is advisable to assess the concentration of Mg in the red blood cells of patients.

© 2018, Springer Science+Business Media, LLC, part of Springer Nature. Technology development for solid dosage forms with a solid dispersion of diclofenac is a crucial problem in pharmaceutical science and practice. The goal of the work was science-based and experimental technology development for tablets containing a solid dispersion of diclofenac with improved biopharmaceutical indicators as an equivalent to the substance. The obtained granulates and tablets had indicators that met the corresponding standards of the Russian SP XIIIth Ed. Almost 100% of the diclofenac was released from the developed tablets. This was 1.3 times greater than from commercial tablets. The recommended shelf life under these conditions is two years. The proposed technology could not only increase the bioavailability of the slightly soluble non-salt form of diclofenac but also facilitate further development of new medicinal preparations with improved bioavailability.

© 2018 Izdatel'stvo Meditsina. All rights reserved. Results of studying the comparative bioavailability of pharmaceutical preparations - alternative analogs of endogenous compounds containing calcium and colecalciferol are presented. The drug concentrations were recalculated with allowance for the endogenous calcium level, in accordance with the relevant normative guidelines. The standard methodology of bioequivalence studies can be used to evaluate the quality of reproduced calcium preparations, taking into account low values of intra-individual variability of pharmacokinetic parameters.

© 2018 Izdatel'stvo Meditsina. All rights reserved. Indomethacin, a non-steroid anti-inflammatory drug (NSAID), has been used in different spheres of medicine since the 1960s. It is successfully administered as an anti-inflammatory and pain-relieving medication in rheumatoid and other diseases. According to recent research, indomethacin may become a promising drug enhancing endogenous remyelination in patients with multiple sclerosis. Also, indomethacin affects cell proliferation and invasion, thus it is used to manage pancreatic cancer in patients with hyperglycemia. In addition, indomethacin can inhibit protein synthesis in colorectal carcinoma and other types of cancer cells. The article reviews modern indomethacin medications and the different dosage forms on the Russian pharmaceutical market. Indomethacin poor water solubility is one of the reasons for decreasing its biopharmaceutical characteristics. According to the conducted research, a prospective way to improve indomethacin solubility and bioavailability is the Solid Dispersion (SD) method. SDs are bi- or multicomponent systems consisting of the drug and the carrier. They are a highly dispersed solid phase of the drug or molecular-dispersed solid solutions with a partial formation of a variable composition complex and a carrier. The article provides a brief overview on different aspects of obtaining, investigating, and applying indomethacin SDs with various polymers.

© The Author(s) 2018. Published by Oxford University Press on behalf of the International Life Sciences Institute. All rights reserved. Vitamin B12 (B-12) deficiency is still relatively common in low-, medium-, and high-income countries, mainly because of dietary inadequacy and, to a lesser extent, malabsorption. This narrative review is based on a systematic search of evidence on methods to assess B-12 bioavailability and technologies to enhance its absorption. A total of 2523 scientific articles identified in PubMed and 1572 patents identified in Orbit Intelligence were prescreened. Among the reviewed methods, Schilling's test and/or its food-based version (using cobalamin-labeled egg yolk) were used for decades but have been discontinued, largely because they required radioactive cobalt. The qualitative CobaSorb test, based on changes in circulating holo-transcobalamin before and after B-12 administration, and the14C-labeled B-12 test for quantitative measurement of absorption of a low-dose radioactive tracer are currently the best available methods. Various forms of B-12 co-formulated with chemical enhancers (ie, salcaprozate sodium, 8-amino caprylate) or supplied via biotechnological methods (ie, microbiological techniques, plant cells expressing cobalamin binding proteins), encapsulation techniques (ie, emulsions, use of chitosan particles), and alternative routes of administration (ie, intranasal, transdermal administration) were identified as potential technologies to enhance B-12 absorption in humans. However, in most cases the evidence of absorption enhancement is limited.

© Copyright 2018 Inderscience Enterprises Ltd. Sanguinarine is a plant alkaloid with relatively low toxicity and high antiangiogenic, antitumour and antiviral potential. In order to increase its bioavailability and effectiveness, sanguinarine liposomes were prepared by a reverse phase evaporation method and characterised. Dynamic light scattering showed mean liposome size of 65 ± 11 nm, zeta-potential equal to -54 ± 1.2 mV, and polydispersity index equal to 0.26. The encapsulation efficiency was 78.6 ± 5.1%. The study on experimental models showed a prolonged sanguinarine release from liposome preparations. Liposomal sanguinarine showed dose-dependent cytotoxic activity in vitro on B16 (murine melanoma) and HeLa (human cervical carcinoma) cell lines. The highest cytotoxicity was observed on B16 cell line (IC50 6.5 μM). HeLa cell line cytotoxicity was relatively lower, equal to 8.03 μM. Compared with free sanguinarine, liposomal sanguinarine may have advantages for in vivo anticancer therapy, due to its lower toxicity and 'passive targeting' as a result of enhanced permeability of tumour vessels.