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Study of radiolabelling of receptor-specific peptide from the group of gastrin derivatives I
Zeithamová, Jana ; Lázníčková, Alice (advisor) ; Kubíček, Vladimír (referee)
This work studies the radiolabeling of minigastrins using 111 In. For experimental purposes minigastrins 46, 47 and 48 were used with different amino acids sequences. It was made especially for radiochemical purity 111 InCl3 sign, since this parameter is very important for possible future use of these labeled peptides. Another parameter investigated was the monitoring of the stability of radioactively labeled minigastrins. Results were measured using high performance liquid chromatography, the clear evidence of pollution and possible degradation products. The second applied method was performed by instant thin-layer chromatography in several different environments. The objective was to determine the dependence on the purity of the product over time in both short and long time intervals.
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Determination of Lipophilicity of Potential Drugs
Coufalová, Iva ; Kubíček, Vladimír (advisor) ; Nováková, Veronika (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control Author: Mgr. Iva Coufalová Consultant: Ing. Vladimír Kubíček, CSc. Thesis Title: Determination of Lipophilicity of Potential Drugs This rigorous thesis deals with the determination of lipophilicity of new synthesized potential drugs based on pyrazine structure by reversed phase high performance liquid chromatography. The theoretical part contains a brief overview of the drugs development and clinical studies, there are also summarized historical and currently common used processes for lipophilicity estimating, including the basic principles of chromatography. Another part of thesis is engaged in to the measurement of specific samples of drugs on a Zorbax ECLIPSE XDB-C8 600 Bar, 50.0x3.0 mm, 1.8 µm column. This column was chosen in order to shorten the retention times of the measured samples compared with C18 column packing. For the lipophilicity values of the examined drugs are considered the logarithm of capacity factor values which were determined by extrapolation to zero concentration of methanol in the mobile phase. In conclusion there was made a comparison of the results with the values previously obtained on a Zorbax ECLIPSE XDB-C18 600Bar, 50.0x4.6 mm, 1.8 μm column and...
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Stability studies of monoclonal antibody nimotuzumab modified with chelator DOTA radiolabelled with lutetium-177 ([177Lu]Lu-hR3(p-SCN-Bn)DOTA)
Petřík, Michal ; Lázníčková, Alice (advisor) ; Kubíček, Vladimír (referee)
The higher expressivity of the gene for the receptor of epidermal growth factor (EGF) and consequently higher number of receptors (EGFR) on the surface of cells is closely linked with the tumour proliferation of these cells and with poor prognosis for patients. For such reason the EGFR became one of the main objectives in the therapy of tumours. Nimotuzumab (also known as h-R3) is humanized monoclonal antibody which blocks receptor for epidermal growth factor. The object of this thesis was to determinate radiochemical purity of this antibody conjugated with bifunctional chelator DOTA and marked by luthecium, possibly purification of this antibody and consequently determination of its stability in different environments. In acetate buffer pH = 7, in an environment of the surplus of competitive ligand EDTA and in plasma of rats. Adequate analytic methods were used for these tasks: high-efficiency liquid chromatography, gel permeation chromatography and chromatography on thin layer. The results of the thesis demonstrated that this way of modification for further radiolabelling is not appropriate for large protein structures such as Nimotuzumab
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Chromatographic Properties of Benzimidazoles
Tyrnová, Lucie ; Kubíček, Vladimír (advisor) ; Jezberová, Michaela (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biophysics and Physical Chemistry Candidate: Lucie Tyrnová Consultant: ing. Vladimír Kubíček, CSc. Title of Thesis: Chromatographic Properties of Benzimidazoles This thesis deals with research considering chromatographic properties of albendazole and its metabolites (albendazole sulfoxide and albendazole sulfone). Measurements were made by Reversed Phase High Performance Liquid Chromatography (RP HPLC). Two columns packed with stationary phases C18 (Zorbax SB and Atlantis T3) were tested during the research. According to a prior calculation there was a chance to expect the columns to show different selectivity during separation albendazole and its metabolites compared to column packed with stationary phase C18 LiChrosper 60 RP-Select B. For the determination of albendazole and its metabolites in biological material by RP HPLC, a part of this thesis was focused on finding a suitable internal standard. Results of the thesis show that the column Zorbax SB is suitable for separation of albendazole and its metabolites, while the column Atlantis T3 gave no satisfactory results. Oxibendazole was successfully tested as the internal standard. Unfortunately the column Zorbax C18 SB does not eliminate important difficulties...
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HPLC Analysis of Anthelmintics Using Core-shell Columns
Marková, Jitka ; Kubíček, Vladimír (advisor) ; Lázníčková, Alice (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biophysics and Physical Chemistry Candidate: Jitka Marková Consultant: Ing. Vladimír Kubíček, CSc. Title of Thesis: HPLC Analysis of Anthelmintics Using Core-shell Columns This diploma thesis deals with HPLC analysis of three anthelmintics included into AAD group (i. e. amino-acetonitrile derivatives). Suitable separation conditions were studied using three core-shell columns (i. e. Ascentis Express RP - Amide, Ascentis Express F5 and Kinetex PFP). Finally, an efficiency of two preextraction methods (SPE, LLE) was tested. The obtained results show the Ascentis Express RP-Amide column to be the suitable choice for the required purpose. The proposed mobile phases are MS compatible. SPE column STRATA X, exhibiting very high recoveries, is the best choice for SPE. The LLE recovery ratio can be taken as satisfactory.
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Alluminium complexes for biomedical applications
Beranová, Tereza ; Kubíček, Vojtěch (advisor) ; Havlíček, David (referee)
The aim of this work was to prepare ligands of macrocycle TACN with aminophosphinate pendant arms. Two ligands were prepared and fully characterized. A complex of aluminium ion was synthesized with one of the ligand. The complex was used for studying a fluoride coordination by a fluoride ion selective electrode. Key words: macrocyclic complex, positron emission tomography, phosphinic acid
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