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LC-MS analysis of phase one biotransformation of K1277, a potential drug against Alzheimer's disease
Krchová, Lucie ; Štaud, František (advisor) ; Kučera, Radim (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Lucie Krchová Supervisor: Prof. PharmDr. František Štaud, Ph.D. Supervisor - Consultant: Mgr. et Mgr. Rafael Doležal, Ph.D. Title of diploma thesis: LC-MS analysis of phase one biotransformation of K1277, a potential drug against Alzheimer's disease. Alzheimer's disease belongs to the most common neurodegenerative diseases that several milions of people all around the world suffer from. There are few symptomatic drugs, which are able to reduce signs and symptoms of this type of dementia, however none of them is able to completely stop it. The diploma thesis is focused on a metabolomic study of compound K1277, synthesized as a combination of 6-chlortacrine and aminoacid tryptophan, which thanks to its properties belongs to promising potential drugs against Alzheimer's disease and which has not been published yet. The aim of this diploma thesis was to perform in vitro metabolomic screening of the compound K1277 using human liver microsomes focusing on qualitative and quantitative analysis. As intermediate aims of the thesis, necessary conditions for sufficient biotransformation of compound K1277 were investigated, quantity of metabolised compound K1277, identifications of particular metabolites...
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Stability Studies of Oral Liquid Preparations Using HPLC
Zahálka, Lukáš ; Solich, Petr (advisor) ; Kučera, Radim (referee) ; Muselík, Jan (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Analytical Chemistry Candidate Mgr. Lukáš Zahálka Supervisor Prof. RNDr. Petr Solich, CSc. Title of Doctoral Thesis Stability Studies of Oral Liquid Preparations Using HPLC According to the database of the Czech State Institute for Drug Control there are 59 thousand of registered drugs available in the Czech Republic, out of which 8 thousand drugs were marketed in July 2017; however, there are still some therapeutic needs that cannot be met by using of these commercially available drugs because of unsuitability of available dosage forms for being used, e.g., in pediatric patients. Thus, cooperation was established between the Faculty of Pharmacy in Hradec Králové (Department of Analytical Chemistry and Department of Pharmaceutical Technology) and the University Hospital in Motol (Prague) to address such therapeutic needs by developing of extemporaneous formulations of oral liquid preparations containing selected pharmaceutical active ingredients. Each project was composed of three major parts. First part was to develop several versions of drug formulations according to various requirements (e.g., sugar-free or preservative-free). This part was accomplished by the Department of Pharmaceutical Technology. The second (development...
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LC-MS analysis of phase one biotransformation of K1277, a potential drug against Alzheimer's disease
Krchová, Lucie ; Štaud, František (advisor) ; Kučera, Radim (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Lucie Krchová Supervisor: Prof. PharmDr. František Štaud, Ph.D. Supervisor - Consultant: Mgr. et Mgr. Rafael Doležal, Ph.D. Title of diploma thesis: LC-MS analysis of phase one biotransformation of K1277, a potential drug against Alzheimer's disease. Alzheimer's disease belongs to the most common neurodegenerative diseases that several milions of people all around the world suffer from. There are few symptomatic drugs, which are able to reduce signs and symptoms of this type of dementia, however none of them is able to completely stop it. The diploma thesis is focused on a metabolomic study of compound K1277, synthesized as a combination of 6-chlortacrine and aminoacid tryptophan, which thanks to its properties belongs to promising potential drugs against Alzheimer's disease and which has not been published yet. The aim of this diploma thesis was to perform in vitro metabolomic screening of the compound K1277 using human liver microsomes focusing on qualitative and quantitative analysis. As intermediate aims of the thesis, necessary conditions for sufficient biotransformation of compound K1277 were investigated, quantity of metabolised compound K1277, identifications of particular metabolites...
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Optimization of chromatographic parameters for chiral separation of biologically active compounds
Novák, Martin ; Kučera, Radim (advisor) ; Nobilis, Milan (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Chemistry and Pharmaceutical Analysis Student: Bc. Martin Novák Supervisor: doc. PharmDr. Radim Kučera, Ph.D. Consultant: Mgr. et Mgr. Rafael Doležal, Ph.D. Title of diploma thesis: Optimization of chromatographic parameters for chiral separation of biologically active compounds. The diploma thesis was focused on the development of a HPLC-UV method for the determination of K 1277 enantiomers of systematic name N-(2-((6-chloro-1,2,3,4-tetra- hydroacridin-9-yl)amino)hexyl-2-amino-3-(1H-indole-3-yl) propylamide dihydrochloride, which is one of the compounds from the tacrine-tryptophan hybrids group. These tacrine-tryptophan hybrids could be considered as promising candidates of potential drugs against Alzheimer's disease. The thesis brings an explanation of basic characteristic of chiral molecules, principles of chiral separation, pathophysiology, clinical manifestation and treatment of Alzheimer's disease and short characteristic of tacrine-tryptophan hybrids in the theoretical section. The aim of my diploma thesis was to find the optimal chromatographic conditions for separation of K 1277 enantiomers synthesized from tacrine and tryptophan fragments. The experimental part deals with the development of the chiral...
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Apartment building
Škrdlová, Aneta ; Kučera, Radim (referee) ; Sobotka, Jindřich (advisor)
The subject of the bachelor thesis is the design and development of project documentation for the construction of a residential building. It is an object with four above-ground floors, which at each level recede and create terraces. There are 7 apartments in the building, one of which is for people with limited mobility. Part of the ground floor is a shop. About 16 parking spaces. The roof is designed as a single-layer flat with a duo order of layers. The object is designed by POROTHERM
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Apartment building
Šedivý, Adam ; Kučera, Radim (referee) ; Sobotka, Jindřich (advisor)
The aim of the bachelor’s work is composition of project documentation for the constrution building of apartment building. Object is situated on the cadastral area of Město Náměšť nad Oslavou, number of builing plot is 780/189-190. Builing plot is located in new houses area. Terain is slightly sloping. In the apartment building there are 3 above-ground floor and 1 belowground floor. In the below-groun floor there are situated cellars, storage spaces and technical spaces. In the above-ground floor there are situated flats and two medical offices. Structural system of this builing is wall system. External wall is composed of vertically performe block Heluz. Floor structure is designed as a cast-in-place two way reinforced slab. Staircase is designet as cast-in-place reinforced contstruction too. Roofing of object is composed of flat roof. Floor construction are designed as floating floor.
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Detached house with a design office
Spáčilová, Kristýna ; Kučera, Radim (referee) ; Kolář, Radim (advisor)
This bachelor thesis deals with the design and processing of the design documentation for the construction of a new detached house with a design office, which is located in the cadastral unit of the village of Výkleky on plot no 79/1; 79/2. The house is divided into dwelling unit and establishment. The object is designed as a double floor and partly basement. The house is roofed with hipped roof. Construction systém wall, brick from brick´s blocks, basement is from permanent forwork. The bachelor thesis is elaborated in the form of project documentation for construction.
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Apartment building
Světlík, Adam ; Kučera, Radim (referee) ; Struhala, Karel (advisor)
The subject of bachelor thesis is the composition of project documentation of an apartment building at edge of city Bučovice. Apartment building is four-storey building without a basement and is detached building on almost flat terrain, consisting of several parcels, on the cadastral unit of Bučovice. The object is connected to the local road on the north side of the property. Between the object and the communication is parking for the user object, which has 17 parking spaces. The ground floor is divided into the dwelling unit and the technical facilities. Other storeys are divided into the two dwelling units and these units have balconies. The walls are composed of aerated concrete blocks YTONG, in combination with an acoustic internal sand-lime blocks and are based on concrete foundation strips. The celling is reinforced light-weight clay concrete LIASTROP. The floors are heavy floating. The roof is green warm flat roof. The whole object is insulated with contact thermal instulation from mineral isolation MULTIPOR and expanded polystyrene. The drawing part was drawn in AutoCAD.
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Home over water
Kosová, Karolína ; Kučera, Radim (referee) ; Struhala, Karel (advisor)
The subject of my bachelor thesis is a project of a new detached house with painting atelier in Martinice u Onšova. The designed house will be partly built partly on plot no. 140/2, the main part of the building is designed above the surface of the large pond (plot no. 145) Detached house for a four-member family has two overground floors. Parking is solved by a detached garage for two cars. Foundations are made up of reinforced concrete large diameter drilled pile and frame structure of strip foundation which supports loadbearing wall. Vertical loadbearing structures are designed of clay blocks. The vertical peripheral structures are provided with an insulation system with ventilated space. Floor-slab is designed of reinforced concrete. A two-layer barrel roof is a dominant of the building. A roof between detached house and atelier is designed as a walkable flat roof.
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Apartment house
Grolmus, Juraj ; Kučera, Radim (referee) ; Matějka, Libor (advisor)
The aim of the Bachelor thesis is project documentation for execution of an apartment house with four above-ground floors and one under-ground floor. There are 10 apartments in above-ground floors and in the under-ground floor there are common premises of the house equipment. Part of the under-ground floor are also garages, where a parking platforms are located, which provide a parking space for 18 cars. The top floor is designed as a recessing floor and to apartments located in this floor belongs spacious terrace. The roof above the top floor is designed as a one-layer flat roof with combined sequence of layers. The building is designed from a HELUZ system.
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