Preview

Pharmacokinetics and Pharmacodynamics

Advanced search
No 4 (2016)
View or download the full issue PDF (31,3 МБ) (Russian)

PHARMACOKINETICS STUDIES

3-8 1684
Abstract
In a single-dose, two-treatment, two-period, two-sequence crossover study with a 14-days washout period was carried out the bioequivalence study of two tablet coated formulation of mycophenolic acid that given to 48 volunteers in equal doses (dosage 360 mg). There were calculated the followed parameters: AUC0-t, Cmax, Tmax, Cmax/AUC. 90% confidence interval for ratio of geometric mean AUC0-t values was 98,97% - 111,49% and one for ratio of geometric mean Cmax was 121,27% - 153,94%. The upper limit of the confidence interval of Cmax valuesa goes beyond the permissible range according to the protocol study (75-133%). It is not possible to state bioequivalence of drugs. Possible causes of discrepancies of pharmacokinetic parameters were analyzed.

STUDIES OF PHARMACOLOGICAL ACTIVITY OF METABOLITES

9-18 2005
Abstract
Most studies on the relationship between vitamin D and various pathologies use only one of the metabolites of vitamin D-25-hydroxyvitamin D3 (25(OH)D3). Hence, the potential effects associated with changes in the levels of other vitamin D metabolites remain outside of the focus of most researchers. In this paper we analyze the known biotransformations of cholecalciferol, possible errors in the assessment of D deficiency related to the properties of various metabolites of vitamin D3, a fundamental biologicaL roLe of the different metabolites of vitamin D3, and prospects for the use of the determination of vitamin D3 metabolite levels for clinical diagnostics.

PRECLINICAL STUDIES

19-30 1047
Abstract
The paper presents the results of chemorectome modeling of the pharmacological effects of ethylmethylhydroxypyridine succinate (mexidol) as compared to control molecules (choline alfoscerate, piracetam, glycine, semax). Chemoreactome analysis showed that mexidol may be (1) an agonist of acetylcholine and GABA-A receptors; (2) an anti-inflammatory agent, the effects of which are carried out by inhibiting the synthesis of pro-inflammatory prostaglandins; (3) a neurotrophic agent with neuroprotective properties; (4) a coagulation inhibitor; (5) a diabetes medication and (6) a hypolipidemic agent. From the “control” molecules mexidol is distinguished by a more pronounced safety profile (a lower impact on serotonin, dopamine and adrenergic receptors, a lesser degree of interaction with the potassium channels of the heart, with the MAO enzyme and with the P450 cytochromes). The results of the chemoreactome modeling allowed us to formulate the mechanisms of action of mexidol at the molecular level.

PROTEOMIC ANALYSIS

31-42 890
Abstract
Laennec preparation is based on standardized human placenta hydrolyzate and is highly effective in the regeneration of tissues. This study presents the results of analysis of the light peptide fraction of Laennec (<3 000 Da) by using three methods: (1) mass spectrometry using Q-Exactive (ThermoScientific, Germany), (2) enzyme immunoassay for the discovery of epitopes of proteins by enzyme-linked immunosorbent assay (ELISA) with monoclonal antibodies to IGF-1, TGF-1, HGF, VEGF, PDGF, EGF and chemokines (IL-8, IL-1a, IL-1b, TNFa, IL-12) and (3) peptide sequencing. The results indicated high degree of standardization of Laennec concerning the peptide composition. Amino acid sequences of 47 peptides were established using standard software. The composition of Laennec includes the peptide fragments of albumin, collagens Ia2, Va2, XIXa1, «zinc fingers», regenerative growth factors IGF-1, TGF-1, HGF, VEGF, PDGF, EGF. The presence of these peptides in Laennec allowed us to formulate a number of previously unknown molecular mechanisms of the Laennec action

SECURITY RESEARCH

43-54 1783
Abstract
Toxicity study in male Wistar albino rats showed that the LD50 of Lithium ascorbate is 6,334 g/kg which refers the substance to grade 5 toxicity (practically non toxic). Accumulation ratio of Lithium ascorbate was found to be 14,8 thus indicating a Low cumulative effect and confirming Low toxicity. HistoLogicaL findings in animaLs treated with Lithium ascorbate daiLy for 30 days in doses cLose to LD50 indicate that an excess strain is exerted upon the neuroendocrine system (heterogeneity of ceLL eLements, signs of dystrophic changes) and, to a Lesser extent, upon the internaL organs. At the same time, after the subtoxic doses were ceased a partiaL restoration of functionaL activity of the organs invoLved was observed.

CLINICAL STUDIES

55-62 462
Abstract
TSupport with micronutrients functions of vision in students with myopia underutilized reserve of health-saving technologies. Students myopia is one of the major problems that at the school is only growing. This paper presents the results two centers randomized trial of the effectiveness of the usage of vitamin-mineraL complex "Focus Forte" in the group of 120 young patients at the age of (1619 years, students of fuLL-time education in Ivanovo and Krasnodar) in the context of integrated therapy for 2 months. Patients were randomized to receive drug (n = 60) or controL group (standard therapy, n = 60). On day "0" day and "60" were measured more than 80 parameters of a spatiaL-contrast sensitivity with the use of speciaL computer software package. The comparison of the investigated indicators of view on the day "60" showed a number of statisticaLLy significant differences in eLectroacousticaLLy (O.S. 4,6, 95% DI 1,4-16, p = 0,03), spatiaL contrast sensitivity (O.S. 9,0, 95% DI 1,5-17, p < 0,006) and brightness sensitivity (O.S. 5,6, 95% DI 1,7-19,0; p = 0,003). The drug contributed to a statisticaLLy significant reduction of cLinicaL symptoms of hypovitaminosis, and zinc deficiency (р < 0,001). Correction of micronutrients designed to support your eyesight, promotes normaphisioLogicaL processes of vision, improve visuaL function and compensation phenomena of asthenopia among students.


Creative Commons License
This work is licensed under a Creative Commons Attribution 4.0 License.


ISSN 2587-7836 (Print)
ISSN 2686-8830 (Online)