Milan Lázníček

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The transfer kinetics of cyclosporine across the dually perfused rat placenta in the maternal to fetal direction and a possible involvement of P-glycoprotein were investigated. The transplacental clearance of cyclosporine in the materno-fetal direction was found to be dependent on the maternal inflow concentration of cyclosporine. Coadministration of(More)
Three different procedures for the labeling of hyaluronan (HA) with (111)In, (125)I and (14)C radionuclides were compared, and the kinetic stability of radiolabeled HA under different conditions (saline, artificial gastric juice and plasma) was established. Modification of HA structure with bifunctional chelating agents (DTPA) or with the prosthetic group(More)
Plasma protein binding and pharmacokinetic parameters of CHIP (cis-dichloro-trans-dihydroxy-bisisopropylamine platinum IV) and CBDCA (cis-diammine-1,1-cyclobutane dicarboxylate platinum II) were investigated in male Wistar rats. The plasma clearance of total and non-protein-bound platinum was determined and compared with that of 99mTc-DTPA. for binding(More)
The pharmacokinetics of two isomers, o- and m-iodohippurate, were determined in rabbits and rats and the effect of protein binding on their elimination is demonstrated. Both isomers are rapidly eliminated by transport systems in the kidney and their clearance by the kidney approaches the renal plasma flow regardless of protein binding, m-Iodohippurate is(More)
BACKGROUND Hyaluronan (HYA) is a high molecular weight glucosaminoglycan with a great perspective for medical applications. Because HYA is widespread in the body, it is difficult to determine the fate of exogenously administered HYA. METHODS In this study, HYAof different molecular weights (0.1-1 MDa) was labelled with (99m)Tc, and the distribution(More)
The protein binding of tolfenamic acid in plasma from patients with renal and hepatic disorders was studied by equilibrium dialysis. Drug binding to the cellular components of whole blood and blood cell suspensions was also measured. Salicylic acid was used as the reference drug in all experiments. Renal and hepatic diseases increased the unbound fraction(More)
UNLABELLED 99mTc-labeled peptides, particularly those of a lipophilic nature, are often excreted through the hepatobiliary system, and the subsequent accumulation in the intestine may obscure receptor-mediated uptake in tumor sites in the pelvis. We have therefore explored the route and rate of excretion of a small series of Tc-labeled peptides to shed some(More)
RATIONALE AND OBJECTIVES Newer radiologic techniques require fast bolus injections and thus low-viscosity, high-concentration, well-tolerated contrast media (CM), especially in vulnerable patients. To this end, we designed and developed iosimenol, a novel isotonic nonionic dimer, and have conducted tests to enable its clinical evaluation. METHODS Standard(More)
Renal elimination pathways of three positional isomers of iodobenzoic acid (2-iodobenzoate, 3-iodobenzoate and 4-iodobenzoate radiolabelled with 125I) were compared using the perfused rat kidney in-situ. All agents were eliminated both in a parent form (involving all renal elimination mechanisms i.e. glomerular filtration, tubular secretion, and tubular(More)
The present study compares distribution and elimination characteristics of111In-DTPA-D-Phe1-octreotide and111In-DTPA-L-Phe1 octreotide in rats and evaluated the effect of the replacement of the terminal L-phenylalanine by D-phenylalanine on pharmacokinetic profiles of the radiolabelled peptides. Both agents exhibited rapid radioactivity clearance from the(More)