Abstract: this paper presents the results of therapeutic drug monitoring of lamotrigine, an anticonvulsant epilepsy medication, in patients with cryptogenic focal epilepsy using plasma and saliva as a biological material for drug testing. Comparative analysis of the steady-state plasma and saliva lamotrigine concentrations (СssMIN and СssMAX) allows the conclusion that saliva can be used as a suitable biological substrate for therapeutic drug monitoring.
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.
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.
We have developed a new method for the quantitative determination of valproic acids based on gas chromatography with mass spectrometric detection of three ion fragments of a parent molecule with m / z = 73, 102, and 115. The proposed technique has been used to solve the tasks of anticonvulsant therapeutic drug monitoring and applied to determining individual pharmacokinetic characteristics of patients at the Research Center of Neurology of the Russian Academy of Medical Science with respect to valproic acid.
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.
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.
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.