Molecularly imprinted polymers

Natalia Denderz, Jozef Lehotay, Jozef Čižmárik

Čes. slov. farm. 2012, 61(3):79-86  

Nowadays about 28 million different simple or complex chemical entities are known. Today we cannot imagine the life without different kinds of drugs, cosmetics, pesticides, food additives or stimulants. In the recent period in the field of analytical chemistry or pharmacy more modern techniques or methodologies are required which will allow selective determination of different kinds of analytes, especially in complex biological matrices. The imprinted polymers are very often used for the preparation of samples before analysis and this procedure can reduce the possibilities of interferences. This paper deals with the characterization, preparation, properties...

Hot-melt extrusion

Jana Šalandová, Miloslava Rabišková

Čes. slov. farm. 2012, 61(3):87-92  

Hot-melt extrusion (HME), originally coming from plastic industry, becomes at present an interesting technology also in the pharmaceutical field. The number of drugs with poor solubility and also bioavailability is increasing. In addition, most of the organic drugs are exhibiting polymorphism. Together with the utilization of appropriate carriers and other excipients, HME introduces an interesting possibility how to increase the solubility of poorly soluble drugs or protect unwanted polymorphic changes and how to improve bioavailability of problematic drugs. HME can also be used in the formation of dosage forms with controlled drug release, e.g. pellets...

Gamma-secretase inhibitors in Alzheimer's disease therapy

Katarína Špilovská, Jan Korábečný, Kamil Kuča, Kamil Musílek

Čes. slov. farm. 2012, 61(3):93-100  

Neuritic plaques, which are situated in the brain of Alzheimer's disease (AD) patients, are composed mainly of peptides containing 40 or 42 amino acid residues known as ß-amyloid plaques (Aß). The Aß peptide is the result of the enzymatic cleavage of the amyloid precursor protein (APP). In the so-called amyloidogenic pathway, the ß-secretase enzyme releases a protein fragment (C99), which is subsequently metabolized by the enzyme γ-secretase. Monomer forms of Aß are turned into oligomer forms, which are the main cause of cellular neuronal death in AD patients. The following study is focused on γ-secretase inhibitors that can slow down the...

Modulation of leukotriene pathway - potential targets

Peter Hoffman, Lýdia Bezáková

Čes. slov. farm. 2012, 61(3):101-106  

Leukotrienes (LT), namely cysteinyl LT and LTB₄, are potent lipid mediators taking part in the signal pathways of many inflammatory processes. The arachidonic acid transformation into leukotrienes can be signed as the leukotriene pathway. The key enzyme is 5-lipoxygenase, a dioxygenase containing a nonheme-bound ferric central ion, which in the catalytic complex with 5-lipoxygenase activating protein forms 5-hydroperoxyeicosatetraenoic acid. In the next steps this process involves leukotriene A₄-hydrolase or leukotriene C₄-synthase. According to the progress in recent years in the area of X-ray structural analysis and...

Microbial secondary metabolites as inhibitors of pharmaceutically important transferases and oxidoreductases

Eva Buchtová, Mária Šturdíková

Čes. slov. farm. 2012, 61(3):107-114  

Microorganisms are known for their production of an enormous variety of biologically active secondary metabolites including antibiotics, immunosuppressants and anticancer agents. These compounds have many important biological activities used in the clinical practice in drug treatment of cancer, inflammatory, autoimmune diseases and metabolic disorders. The science and medicine research have been yielded hundreds items of useful knowledge in the therapy of many serious human diseases caused by pathophysiological mechanisms of enzymes. Many substances were discovered already in the last century, but the research of their potential and various modifications...

Phenotyping of enzymes participating in drug metabolism

Svatopluk Světlík, Karolína Hronová, Ondřej Slanař

Čes. slov. farm. 2012, 61(3):115-126  

Pharmacogenetics is a rapidly developing field of science promising individualization of treatment through determination of genetic polymorphism in pharmacodynamics (receptors and other drug targets) and pharmacokinetics (carriers, metabolic enzymes). Enzyme activity may be predicted using genotyping or directly phenotyped - after administration of a probe substrate. This review article deals with some important metabolic enzyme polymorphisms and their phenotyping methods. Special consideration is given to the analytical methods described in the literature, which can be used to determine the metabolic rate.

SOLUTIO 2011

J. Solich

Čes. slov. farm. 2012, 61(3):126  

Prof. RNDr. J. Čižmárik, PhD. - doctor honoris causa

Eva Sedlárová

Čes. slov. farm. 2012, 61(3):133  

Doc. RNDr. Ingrid Tumová, CSc., jubiluje

Jozef Čižmárik

Čes. slov. farm. 2012, 61(3):133-134  

Životné jubileum docenta RNDr. Jozefa Sokolíka, CSc.

F. Devínsky, R. Horáková

Čes. slov. farm. 2012, 61(3):134-135  

Pod ochranou sv. Dymphny - LIV. sympozium z historie farmacie a veterinární medicíny

Jan Babica

Čes. slov. farm. 2012, 61(3):100  

High active potential antimycobacterial agents against Mycobacterium avium

Karel Waisser, Jiří Kuneš, Jiřina Stolaříková

Čes. slov. farm. 2012, 61(3):127-129  

Derivatives of 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-dione are active against Mycobacterium avium when substituted in position 7 with a methyl. One or two carbonyl groups have to be replaced with a thioxo group. High active derivatives are the compounds without substitution on the phenyl, or those substituted on the phenyl in position 3 or 4 with chlorine, bromine or a methyl. The substitution in position 3 and 4 with two atoms of chlorine lowers the activity. The compounds are active against INH resistant strains. We synthesized other 44 derivatives with a similar structure of the compounds as in the paper but substituted in position...

Studies of local anaesthetics - Part 197. Effect of xylitol on pharmaceutical availability of lidocaine and flow properties of hydrogels

Zuzana Vitková, Petra Herdová, Jozef Čižmárik, Daniel Grančai, Lukáš Benč

Čes. slov. farm. 2012, 61(3):130-132  

The paper examines the formulation of hydrogel on the base of a synthetic polymer containing a local anaesthetic and a mass-produced drug in the form of a solution with an antiphlogistic effect. It aimed to prepare a hydrogel of a suitable composition with suitable flow properties and drug release, the active ingredient being lidocaine hydrochloride. Besides the role of a synthetic polymer which ensures that the active ingredient remains at the affected site, an important role in the formulation is played by the presence of an artificial sweetener, which to a great extent as a taste correcting agent of the unpleasant taste of the active ingredient...