[Experimental study of the basic pharmacokinetic characteristics of dipeptide carnosine and its efficiency of penetration into brain tissues].

We have used an original chromatography/mass spectrometry technique to study the pharmacokinetics of dipeptide carnosine in C57 Black/6 mice after intra-peritoneal administration of the drug at a dose of 1 g/kg. The basic pharmacokinetic characteristics of carnosine were measured the in the blood and brain. The obtained concentration-time curve has a biexponential character. It is shown that the maximum concentration of carnosine in the blood plasma is Cmax = 1081.75 ± 124.24 µg/mL and it is achieved in a time interval of Tmax = 0.25 h. We showed that i.p. administration of exogenous carnosine could significantly increase the concentration of that substance in the brain. Tissue availability of dipeptide carnosine for brain tissue is relatively good and constitutes 59% from the total amount of blood carnosine. It was found that the maximum concentration of carnosine in the brain occurs at the sixth hour after i.p. administration when the concentration of drug in the blood is minimal.

Experimental investigation of pharmacodynamics and pharmacokinetics of carbamazepine nanoemulsion.

Anticonvulsant activity and pharmacokinetics of nanoemulsion and unmodified substance of carbamazepine were compared in experiments on mice. Carbamazepine nanoemulsion demonstrated significant anticonvulsant activity and was superior to unmodified substance of carbamazepine against seizures induced by maximum electric shock and picrotoxin. Relative bioavailability of carbamazepine after administration of nanoemulsion was 160% compared to unmodified substance. Carbamazepine nanoemulsion more effectively penetrated through BBB by 1.5 times in comparison with unmodified substance.

[Experimental study of pinostrobine oxime biotransformation].

We have experimentally studied pathways of elimination of an oximized derivative of phytoflavonoid pinostrobine by HPLC/mass spectrometry. Four potential metabolites of pinostrobine oxime have been found and there was an attempt to determine their molecular structures on the basis of their fragmentation under positive electrospray ionization conditions. It is established that pinostrobine oxime is removed from the organism mainly unchanged and also in the form of glucuronated derivative.

[Usage of flavonoids for effective correction of functional and structural breaches of erythrocytes membranes during an extraordinary physical strain in experiments].

The effect of treatment course of bioflavonoids quercetin and diquertin on phospholipids and fatty acid composition of erythrocytes membranes and amilorid-dependent activity Na+/H+ transmembrane exchanger of erythrocytes have been studied in condition of chronic physical tension in mice in consequence of extraordinary running strain. The studied drugs actively prevented from the changes of chemical composition and as a result structural and functional changes of erythrocytes membranes. It is established that the studied bioflavonoids prevented from the development of extraordinary physical strain syndrome.

[Effect of acetylsalicylic acid in complex with lipid nanostructures of various compositions on human platelet aggregation].

The effect of lipid nanocomplexes loaded with acetylsalicylic acid (aspirin) on platelet aggregation in vitro was investigated. The antithrombotic effect of aspirin in complex with liposomes prepared from pig brain glycosphingolipids is not only significantly higher compared to control, but also accompanied by leveling of the development of proaggregant effects. It was shown that ADP-induced platelet aggregation is reduced by the introduction of electrostatic charge in the structure of lipid bilayer of liposomes. The effect achieved for the liposomes possessing a negative charge was more pronounced in comparison to the effect of positively charged liposomes.

[Flavonoid correction of functional elasticity of erythrocyte membranes and hemorheological disorders during oxidative stress caused by chronic physical overstrain in mice].

Effect of a course of treatment by bioflavonoids quercetin and diquertin on the physical work capacity, oxidant and antioxidant status of organism, and hemorheological parameters and deformability of erythrocytes have been studied under conditions of chronic physical overstrain in mice caused by sequential extraordinary running load. The drugs effectively prevent the development of oxidative stress, loss of elasticity of erythrocyte membranes and growth in dynamic blood viscosity in microcirculatory link of hemodynamics. It is established that both bioflavonoids significantly increase the physical work capacity of animals and prevent from the development of physical overstrain syndrome.

[Drug bioavailability improvement by means of nanopharmacology: pharmacokinetics of liposomal drugs].

Modern approaches to increasing the efficiency of liposomal transport of substances are discussed. Examples of creating new nanopharmacological drugs that exceed the pharmacokinetic characteristic of their classical analogs are given.

The effects of Xanthigen in the weight management of obese premenopausal women with non-alcoholic fatty liver disease and normal liver fat.

AIM: To investigate the effects of Xanthigen (brown marine algae fucoxanthin + pomegranate seed oil (PSO)) on body weight, body fat, liver lipids, and blood biochemistry; and Xanthigen and its individual components on resting energy expenditure (REE) in obese, non-diabetic female volunteers with non-alcoholic fatty liver disease (NAFLD) and normal liver fat (NLF) content. METHODS: Sixteen-week, double-blind, randomized, placebo-controlled study. Food record data, body composition, REE (only 41 volunteers with NAFLD) and blood sample analysis were assessed weekly for 16 weeks in 151 non-diabetic, obese premenopausal women with liver fat content above 11% (NAFLD) n = 113, and below 6.5% (NLF) n = 38. RESULTS: Xanthigen-600/2.4 mg (300 mg PSO + 300 mg brown seaweed extract containing 2.4 mg fucoxanthin) resulted in statistically significant reduction of body weight (5.5 +/- 1.4 kg NAFLD group and 4.9 +/- 1.2 kg NLF group, p < 0.05), waist circumference (NAFLD group only), body (3.5 +/- 1.9 kg NAFLD group, p < 0.001; 3.6 +/- 0.7 kg NLF group, p < 0.05) and liver fat content, liver enzymes (NAFLD group only), serum triglycerides and C-reactive protein. Weight loss and reduction in body and liver fat content occurred earlier in patients with NLF than in patients with NAFLD. Fucoxanthin (> 2.4 mg) and Xanthigen-400/1.6 mg (200 mg PSO + 200 mg brown seaweed extract containing 1.6 mg fucoxanthin) significantly increased REE in NAFLD subjects compared to placebo. CONCLUSIONS: Xanthigen promoted weight loss, reduced body and liver fat content, and improved liver function tests in obese non-diabetic women. Xanthigen and Fucoxanthin also increased REE. This product may be considered a promising food supplement in the management of obesity.

[Nanotechnology applications in pharmacology].

The applications of nanotechnology to pharmacology are reviewed. The potential applications of biochips, nanosensors, bioreactors, neural stem cells, immune nanoparticles, biodegradable polymers, and convection-enhanced drug delivery in the diagnostics and treatment of diseases are discussed. Specific attention is given to developments in chemotherapeutic means, including advanced drug delivery systems and targeted nanotherapy, which will form the basis of the future nanomedicine. Numerous novel medicinal forms are discussed, including polymeric nanoparticles, nanotubes, micelles, liposomes, dendrimers, fullerenes, and hydrogels. In particular, highly stable glycosphyngolipid nanotubes and nanoliposomes are proposed as drug delivery systems. For this purpose, the model of stimulation of skin vasomotor reactions by nitroglycerin application is developed. The effect of nitroglycerin is shown to increase 1.5 times when used in the form of a dispersion with nanotubes as carriers and almost 2.5 times in the case of a dispersion with nanoliposomes as carriers. Nanotechnologically manufactured biologically active substances Apiton-25 (containing apis products) and Microhydrin (containing SiO 2 nanoparticles, silicon hydrogen bonds Si-H, and free negative charges for free radical neutralization) have been studied. The results indicate that both Apiton-25 and Microhydrin upon peroral administration enhance the cyclic trial performance during prolonged submaximal exercise in endurance-trained cyclists.

[Doping in sports].

Drugs used by athletes for the improvement of results are described and classified with respect to chemical structure and pharmacological action. The main groups of drugs treated as doping are considered and the WADA requirements to prohibited preparations are formulated. The main effects produced by drugs on the athletes and animals (race horses, fight dogs, etc ) are described and the measures of therapy against side effects are outlined.

Extract of Rhodiola rosea radix reduces the level of C-reactive protein and creatinine kinase in the blood.

The effects of extracts of Rhodiola rosea radix on blood levels of inflammatory C-reactive protein and creatinine kinase were studied in healthy untrained volunteers before and after exhausting exercise. Rhodiola rosea extract exhibited an antiinflammatory effect and protected muscle tissue during exercise.

[Comparative study of the effect of vitamax, synergin and alpha-tocopherol on physical endurance of highly trained athletes]. / Sravnitel'noe issledovanie vliianiia vitamaksa, sinergina i alpha-tokoferola na fizicheskuiu rabotosposobnost' sportsmenov vysokoi kvalifikatsii.

The influence of vitamax, synergin, and alpha-tocopherol on the exercise performance (ultimate run on a tretbahn with increasing load) of high-rank athletes has been studied. Peculiarities of the drug action upon lipid peroxidation (LPO) in unsaturated fatty acids were studied by a chemiluminescence technique and by monitoring the malonic dialdehyde in the course of a 21-day treatment-training session and within a 5-day period after termination of the drug administration. Vitamax and synergin increase the working capacity of high-rank athletes on the 10th and 11st day of administration, respectively, while alpha-tocopherol produces such effect only on the 21st day. All the drugs studied possess antioxidant properties, which are also more pronounced for vitamax and synergin.

Effect of extracts from Rhodiola rosea and Rhodiola crenulata (Crassulaceae) roots on ATP content in mitochondria of skeletal muscles.

We studied the effects of oral treatment with extracts from Rhodiola rosea (50 mg/kg) and Rhodiola crenulata (50 mg/kg) roots on the duration of exhaustive swimming and ATP content in mitochondria of skeletal muscles in rats. Treatment with R. rosea extract significantly (by 24.6%) prolonged the duration of exhaustive swimming in comparison with control rats and rats treated with R. crenullata. R. rosea extract activated the synthesis or resynthesis of ATP in mitochondria and stimulated reparative energy processes after intense exercise. Experiments proved different pharmacological characteristics of R. rosea and R. crenulata: R. rosea is most effective for improving physical working capacity.

[Effect of sulodexide on hemocoagulation and lipid peroxidation in athletes during physical load]. / Vliianie sulodeksida na gemokoaguliatsiiu i pereokislenie lipidov u sportsmenov pri fizicheskoi nagruzke.

High physical loads lead to an increase in the blood coagulation rate and inhibit fibrinolysis in athletes. At the same time, the fibrin-stabilizing factor activity and the fibrinogen concentration tend to increase. Sulodexide produces an anticoagulant effect, thus preventing from hypercoagulation. An increase in the working capacity of athletes caused by suloxide administration is accompanied by the antioxidant action.

[Comparative study of anabolizing activity of apilac and methandrostenolone on a model of isolated overload of the rat skeletal muscle]. / Sravnitel'noe izuchenie anaboliziruiushchei aktivnosti apilaka i metandrostenolona na modeli izolirovannoi peregruzki skeletnoi myshtsy goleni krys.

The anabolic activity of apilac was studied in rats in comparison to methanrdostenolone A 10-day administration of apilac (200 mg/kg) produced a pronounced anabolic effect manifested by a hypertrophy of m. soleus. Methanrdostenolone (10 mg/kg) also favored a gain in the muscle weight. The anabolic action of apilac was comparable to that of methanrdostenolone.

[The effect of elton, leveton, fitoton and adapton on the work capacity of experimental animals]. / Vliianie éltona, levetona, fitotona i adaptona na rabotosposobnost' éksperimental'nykh zhivotnykh.

The test with running on a treadbane showed a 56% increase of working capacity in the control group of male albino mice on the 20th day of training. Oral administration of elton, leveton, phytoton, and adapton, as well as Leuzea and Rhodiola extracts and Schisandra chinensis tincture caused a statistically significant increase in the time of running on the treadbane of animals by the 10th day of medication. The increase in the working capacity of the animals was more marked by the 20th day. In the test of swimming "to the limit" adapton, phytoton, leveton, and elton increased to a greater extent the working capacity of male albino rats in diminishing succession (from 213 to 168%). Schisandra tincture and Rhodiola and Leuzea extracts also increased the swimming time of the animals by 135-159%.