Preparation of regulatory documents for sodium heparin

Heparin is a direct-acting anticoagulant that regulates many biochemical and physiological processes. The quality of each drug or substance entering the market to the consumer, its packaging, storage conditions and shelf life, as well as quality control methods are established in accordance with the State Pharmacopoeia of the Russian Federation. However, despite the widespread use of heparin in medical practice, the State Pharmacopoeia of the Russian Federation XIV 2018 does not prescribe articles on the substance and drugs containing it as an active substance. Quality control of medicines is undoubtedly relevant. Thus, a negligent attitude in 2008 in China led to the fact that at the early stages of production, the drug was added to the sulfated chondroitin sulfate, which, like heparin, has anticoagulant properties, but is 100 times cheaper. As a result of the use of this drug, there have been more than 100 deaths in the United States and hundreds of serious adverse reactions in patients in Europe. In this regard, the purpose of this study is to determine the quality of heparin-containing injectable drugs

Electrochemical Determination of Some Triphenylmethane Dyes by Means of Voltammetry

AbstractThis paper provides the investigation of electrochemical properties of triphenylmethane dyes using a voltammetric method with constant-current potential sweep. Malachite green (MG) and basic fuchsin (BF) have been chosen as representatives of the triphenylmethane dyes. The electrochemical behavior of MG and BF on the surface of a mercury-film electrode depending on рН, the nature of background electrolyte and scan rate of potential sweep have been investigated. The conditions of registration have been determined for MG and BF detecting in the solution. It is demonstrated that the reduction peak currents of MG and BF increase linearly with their concentration in the range of 9.0·10-5- 7.0·10-3 mol/dm3 for MG, 6.0·10-5 – 8.0 10-3 mol/dm3 for BF with correlation coefficients of 0.9987 and 0.9961, respectively. The detection limit of MG is 5.0·10-5 mol/dm3 and for BF - 2.0·10-5 mol/dm3

Voltammetric Sensor for Total Cholesterol Determination

We report on a voltammetric sensor for the detection of total cholesterol. The sensor was fabricated by co-immobilization of two enzymes: cholesterol oxidase (ChOx) and horseradish peroxidase (HRP) on porous graphite. The electrochemical behavior of the sensor was studied with the use of linear sweep voltammetry. It has been shown that the sensor has high stability and high sensitivity (16 muA mM{-1} cm{-2}). The biosensor exhibited a wide linear range up to 300 mol/dm3 in a condition close to physiological (pH=6.86). Besides, the interferences of some key analytes containing in the blood were studied. As a matter of fact, making a fabricated sensor is rather promising for using in clinical practice

Investigation of Electrochemical Properties of Xanthine, Adenine and Thymine on a Glassy Carbon Electrode by Voltammetry

In this paper for investigation of electrochemical properties of nitrogenous bases by voltammetry xanthine (Xa), adenine (A) and thymine (T) with constant-current potential sweep with differentiation were used. The electrochemical behavior of Xa, A and T on the surface of a glassy carbon electrode were investigated. The conditions of registration of their joint detecting in the solution were defined. It is demonstrated that the oxidation peak currents of Xa, A and T increased linearly with their concentration in the range of 4.0 10{-8} - 1 10{-4} mol/dm{3} for Xa, 3.0 10{-7} – 1.0 10{-4} mol/dm{3} for A, and 1.0 10{-5}– 1.1 10{-3} mol/dm{3} for T with correlation coefficients of 0.996, 0.996 and 0.999, respectively

Synthesis, Biological Evaluation, and Molecular Modeling of Aza-Crown Ethers

Synthetic and natural ionophores have been developed to catalyze ion transport and have been shown to exhibit a variety of biological effects. We synthesized 24 aza- and diaza-crown ethers containing adamantyl, adamantylalkyl, aminomethylbenzoyl, and ε-aminocaproyl substituents and analyzed their biological effects in vitro. Ten of the compounds (8, 10–17, and 21) increased intracellular calcium ([Ca2+]i) in human neutrophils, with the most potent being compound 15 (N,N’-bis[2-(1-adamantyl)acetyl]-4,10-diaza-15-crown-5), suggesting that these compounds could alter normal neutrophil [Ca2+]i flux. Indeed, a number of these compounds (i.e., 8, 10–17, and 21) inhibited [Ca2+]i flux in human neutrophils activated by N-formyl peptide (fMLF). Some of these compounds also inhibited chemotactic peptide-induced [Ca2+]i flux in HL60 cells transfected with N-formyl peptide receptor 1 or 2 (FPR1 or FPR2). In addition, several of the active compounds inhibited neutrophil reactive oxygen species production induced by phorbol 12-myristate 13-acetate (PMA) and neutrophil chemotaxis toward fMLF, as both of these processes are highly dependent on regulated [Ca2+]i flux. Quantum chemical calculations were performed on five structure-related diaza-crown ethers and their complexes with Ca2+, Na+, and K+ to obtain a set of molecular electronic properties and to correlate these properties with biological activity. According to density-functional theory (DFT) modeling, Ca2+ ions were more effectively bound by these compounds versus Na+ and K+. The DFT-optimized structures of the ligand-Ca2+ complexes and quantitative structure-activity relationship (QSAR) analysis showed that the carbonyl oxygen atoms of the N,N’-diacylated diaza-crown ethers participated in cation binding and could play an important role in Ca2+ transfer. Thus, our modeling experiments provide a molecular basis to explain at least part of the ionophore mechanism of biological action of aza-crown ethers