Study of interspecies differences in plasma protein binding of 18F-labeled radiopharmaceuticals

Univerzita Karlova v Praze, Farmaceutická fakulta v Hradci Králové Katedra farmakologie a toxikologie Kandidát: Mgr. Dana Nováková Konzultant: Prof. PharmDr. Ing. Milan Lázníček, CSc. Název rigorózní práce: Studium plazmatické vazebnosti radiofarmak značených 18 F z hlediska mezidruhového srovnání Práce je zaměřena na plazmatickou vazebnost tří vybraných radiofarmak značených radionuklidem 18 F z pohledu mezidruhového srovnání. Experimenty byly prováděny s využitím bovinní, prasečí, lidské a potkaní plazmy. Vazebnost na plazmatické bílkoviny se stanovila u tří radiofarmak, konkrétně u 18 F-FDG, 18 F-fluorocholinu a 18 F-thymidinu. Byly použity dvě metody: rovnovážná dialýza a ultrafiltrace. Podstata těchto metod spočívá v oddělení volné a vázané složky. Pro separaci je využita semipermeabilní membrána pro rovnovážnou dialýzu a speciální filtry (AMICON a VIVASPIN) pro metodu ultrafiltrace. Volná frakce je významným parametrem dostupnosti léčiva pro distribuci do tkání a buněk, interakci s receptory, exkreci a metabolizmus. Všechny experimenty byly prováděny při fyziologické teplotě 37řC. Výsledky ukazují nízkou plazmatickou vazebnost těchto tří látek u všech zkoumaných druhů a nedochází tedy k významnému ovlivnění farmakokinetiky studovaného materiálu. Nejvyšší hodnota plazmatické vazebnosti byla...Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Mgr. Dana Nováková Consultant: Prof. PharmDr. Ing. Milan Lázníček, CSc. Title of Thesis: Study of interspecies differences in plasma protein binding of 18 F-labeled radiopharmaceuticals In this thesis, the binding ability of three radiopharmaceuticals containing radionuclide 18 F to the plasma proteins was examined in bovine, pig, human and rat plasma, and the interspecies comparison was performed. Examined radiopharmaceuticals included 18 F-FDG, 18 F-fluorocholine and 18 F-thymidine. The two main methods used are equilibrium dialysis and ultrafiltration. These methods are based on separation of free ligand from the linked component. During the separation, semi-permeable membrane and special filters (AMICON and VIVASPIN) were used for equilibrium dialysis and ultrafiltration, respectively. Free fraction of drugs is considered to be an important parameter for the availability of the drug distribution into the tissues and cells, interaction with receptors, excretion and metabolism. All experiments were carried out at the physiological temperature of 37řC. Obtained results indicate low plasma protein binding of the three radiopharmaceuticals in all studied species, which suggests...Katedra farmakologie a toxikologieDepartment of Pharmacology and ToxicologyFarmaceutická fakulta v Hradci KrálovéFaculty of Pharmacy in Hradec Králov

Hydrogeological evaluating of Ciężkow sandstone layer on the sheet 25-234 Horní Bečva

The occurrence of Ciężkow sandstone layer on map sheet 25-234 Horní Bečva is limited to narrow NW-SE zone between Vigantice and Horní Bečva. Among rocks of Flysch Belt of Western Carpathians Ciężkow sandstone has anomalous features – is very cleanly selected and silicious (80 % of quartz). Paleogene rocks and sediments (particularly their matrix) are usually calciferous. Lithological composition of Ciężkow sandstone makes specific conditions in groundwater circle and has an influent to ground water chemical composition: ground water has low mineralization and pH. Also the rock environment has similar conditions like crystalline rock environment. On surface has evolved peat bogs and specific vegetation – phytocenoses typical for acid soils without nutrients.The occurrence of Ciężkow sandstone layer on map sheet 25-234 Horní Bečva is limited to narrow NW-SE zone between Vigantice and Horní Bečva. Among rocks of Flysch Belt of Western Carpathians Ciężkow sandstone has anomalous features – is very cleanly selected and silicious (80 % of quartz). Paleogene rocks and sediments (particularly their matrix) are usually calciferous. Lithological composition of Ciężkow sandstone makes specific conditions in groundwater circle and has an influent to ground water chemical composition: ground water has low mineralization and pH. Also the rock environment has similar conditions like crystalline rock environment. On surface has evolved peat bogs and specific vegetation – phytocenoses typical for acid soils without nutrients

Minerální vody mikroregionu Bojkovsko

Mineral waters finding in Bojkovice region belong mostly to Luhačovice type of mineral waters, which are bounded to Nezdenice fault zone. Some of them present a rest of metamorphosed synsedimentary marine waters with typical mineralization, Na-Cl chemical type, contents of iodine, bromides and other substances. Thanks deep volcanic sources and tectonic faults are mineral waters saturated by carbon dioxide and hydrogen sulphide in concentrations higher than 1 g.l-1CO2 and 1 mg.l-1 of H2S. The contribution shows a situation of sources, current results of chemical analysis and field measuring during 2001–2005

Biodiversity of culturable procaryotes from the Hranice abyss and the role of microorganisms in carbonate speleothemes forming

Hranice Karst is situated in northeastern part of Moravia, Czech Republic, at the contact between two major geological units of the Bohemian Massif and Western Carpathians. This karst developed in combination of meteoric water and hydrothermal dissolution of deformed and tectonically stacked Devonian and Lower Carboniferous limestones. This karst, therefore, exceeds to considerable depths of several hundreds metres. In the 1977, unusually massive organic coatings high in microbial extracellular polymers, occurring together with biofilm structures, were discovered in the vertical caves of low hydrothermally active ‚Hranická propast (Hranice Abyss)‘, particularly on the cave walls in deep underwater environments. These mucilaginous formations may have been classified among ‚snottites‘, mucous-like coatings and stalactites. The present study provides the first insights into both the microbial diversity and morphological/structural variability of these extremophilic formations.Hranice Karst is situated in northeastern part of Moravia, Czech Republic, at the contact between two major geological units of the Bohemian Massif and Western Carpathians. This karst developed in combination of meteoric water and hydrothermal dissolution of deformed and tectonically stacked Devonian and Lower Carboniferous limestones. This karst, therefore, exceeds to considerable depths of several hundreds metres. In the 1977, unusually massive organic coatings high in microbial extracellular polymers, occurring together with biofilm structures, were discovered in the vertical caves of low hydrothermally active ‚Hranická propast (Hranice Abyss)‘, particularly on the cave walls in deep underwater environments. These mucilaginous formations may have been classified among ‚snottites‘, mucous-like coatings and stalactites. The present study provides the first insights into both the microbial diversity and morphological/structural variability of these extremophilic formations

Quantification of ascorbic acid and sodium ascorbate in powder blends for tableting and in vitamin C chewable tablets by NIR-chemometry

The paper proposes a near infrared methodable to directlyand simultaneously quantify ascorbic acid and sodium ascorbate in powder blends for tableting and in vitamin C chewable tablets without any sample preparation.In the first step, calibration models for the quantification of ascorbic acid and sodium ascorbate in powder blends for tabletingand subsequently in chewable vitamin C tablets (corresponding to 80–120 % active substance) were developed according to an experimental design with 2 variables and 5 levels. Then, using the best calibration models, the methods were fully validatedin terms of recovery, precision and accuracyfor both powder blends and vitamin Cchewable tablets.The validated concentration range was 15.14–18.51 % for ascorbic acid and 12.06–14.49 % for sodium ascorbate in powder blends and 91.85–111.03 mg per tablet for ascorbic acid and 71.01–84.50 mg per tablet for sodium ascorbate in tablets. Validation results showed good precision and accuracy

Návrh databázového zpracování subsystému základní prostředky ve Výzkumném ústavu Sigma Olomouc

Prezenční156 - Katedra národohospodářskáNeuveden

Biological aktivity of secondary plants metabolites I. Alkaloids of Narcissus jonquilla L.

Nováková D.: Biological activity of secondary plants metabolites I. Alkaloids of Narcissus jonquilla L. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2015, pp. 70. The aim of the diploma thesis was a preparation of alkaloid extracts to identification of alkaloid patterns and measure cholinesterase inhibitory activity. This activity is useful for treating Alzheimer's disease. Alkaloid extracts of seven Narcissus jonquilla L. (Amaryllidaceae) varieties (Sundial, Sundisc, Sweetness, Waterperry, Simplex, Twinkling Yellow, Yazz) were studied with respect to their acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE) inhibitory activity and alkaloid patterns. Twenty-three alkaloids were determined by GC/MS, and ten of them identified from their mass spectra and retention times. All samples exhibited content of galanthamine, most samples contained lycorine and tazettine. Promising HuAChE inhibition activity was demonstrated by Narcissus jonquilla L. cv. Waterperry with IC50 values of 6.53 ± 0.88 μg/mL. The strongest inhibitory activity against HuBuChE was detected in extract from Narcissus jonquilla L. cv. Sundisc with IC50 value of 5.09 ± 0.64 μg/mL. Keywords: Alzheimer's disease, Amaryllidaceae, Narcissus,..