Optimization of diclofenac sodium profile from halloysite nanotubules

Kateřina Krejčová, Patrick B. Deasy, Miloslava Rabišková

Čes. slov. farm. 2013, 62(2):71-77  

Halloysite, aluminosilicate clay with the particle shape of multilayered hollow nanotubes, used in various non-medical applications, e.g. in ceramic industry, was discovered for pharmaceutical purposes in recent years. Several drugs of hydrophilic and lipophilic nature have been successfully encapsulated into halloysite tubules in order to modify their dissolution profile. The main goal of this experiment was to optimize the dissolution profile of diclofenac sodium - a drug with problematic solubility - from halloysite tubules using various polymers. Loading of the drug together with povidone or Eudragit^® RS did not lead to drug burst...

Thiosemicarbazones and their antimycobacterial effects

Veronika Opletalová, Jan Doležel

Čes. slov. farm. 2013, 62(2):78-83  

Antimycobacterial effects of thiosemicarbazones were discovered in the late 1940s. The best known representative of these compounds is thioacetazone that has been used in the therapy of tuberculosis since the turn of the 1940s and 1950s. At present, it is used only rarely since it exhibits severe side effects. This paper deals with the antimycobacterial effects of thiosemicarbazones and N,N-dimethylthiosemicarbazones derived from 5-alkyl-2-acetylpyrazines. Some of these compounds displayed high inhibition of the growth of Mycobacterium tuberculosis H₃₇Rv, but were excluded from the in vivo studies due to their cytotoxic...

Aminopyrazinoic acid esters as potential antimycobacterial drugs

Martin Doležal, Jana Vobicková, Barbora Servusová, Pavla Paterová

Čes. slov. farm. 2013, 62(2):84-88  

A series of esters of the 3-aminopyrazine-2-carboxylic acid as potential antimycobacterial drugs was synthesized. A CEM Discover microwave reactor with an autosampler Explorer 24 which served to accelerate the reaction was used for synthesis. The prepared products were characterized by IR, ¹H NMR, ¹³C NMR spectra, elementary analysis and melting points. Log P and ClogP values were calculated. Final products were evaluated in vitro for their antimycobacterial activity. The most active compound was hexyl 3-aminopyrazine-2-carboxylate (7), whose antimycobacterial activity (MIC) against M. tuberculosis H37Rv was 6.25 μg/mL.

Influence of the degree of substitution on the absorptivity of acidic carboxymethyl cellulose in the form of nonwoven fabric

Ruta Masteiková, Lenka Vinklárková, Jan Muselík, David Vetchý, Jurga Bernatonienė, Tomáš Sopuch

Čes. slov. farm. 2013, 62(2):89-94  

Modern wound treatment is based on the creation of moist wound environment which accelerates healing. For these purposes some devices and materials may be used, including carboxymethyl cellulose (CMC). Wound dressings currently available on the market contain CMC in the form of sodium salt. CMC in the acidic form has not been used in wound healing therapy yet. Likewise, there are only a few papers describing the acidic CMC preparation and properties, which are inter alia dependent on the degree of substitution (DS). Therefore, the aim of the study was to evaluate the influence of DS on absorptivity, which is one of the main features of dressings...

Evaluation of the influence of sterilization method on the stability of carboxymethyl cellulose wound dressing

Jan Muselík, Lenka Wojnarová, Ruta Masteiková, Tomáš Sopuch

Čes. slov. farm. 2013, 62(2):95-98  

Carboxymethyl cellulose, especially its sodium salt, is a versatile pharmaceutical excipient. From a therapeutic point of view, sodium salt of carboxymethyl cellulose is used in the production of modern wound dressings to allow moist wound healing. Wound dressings must be sterile and stable throughout their shelf life and have to be able to withstand different temperature conditions. At the present time, a number of sterilization methods are available. In the case of polymeric materials, the selected sterilization process must not induce any changes in the polymer structure, such as polymer chains cleavage, changes in cross-linking, etc. This paper...

Physiological aspects of lipoxygenase in plant signaling systems. Part I. Octadecanoid pathway

Renáta Kollárová, Marek Obložinský, Veronika Kováčiková

Čes. slov. farm. 2013, 62(2):59-64  

Lipoxygenases (LOX, linoleate: oxygen oxidoreductases, EC 1.13.11.12) constitute a family of dioxygenases, which contain non-heme, non-sulfide iron. These enzymes occur not only in animals, but in plants as well. They have been detected in coral, moss, fungi and also in some bacteria. LOXs catalyse the regiospecific and stereospecific insertion of molecular oxygen into the molecule of polyunsaturated fatty acid with the cis,cis-1,4-pentadiene system to yield the corresponding hydroperoxides. This step of dioxygenation leads to a cascade of reactions called the lipoxygenase (octadecanoid) pathway. The products of this pathway (called oxylipins)...

Advances in the use of instrumental measurement of colour in the development, production and quality control of drugs, medicinal preparations and pharmaceutical auxiliary substances I

Jan Šubert, Jozef Čižmárik

Čes. slov. farm. 2013, 62(2):65-70  

Colour is one of the important indices of the quality of drugs, medicinal preparations and pharmaceutical auxiliary substances. The paper summarizes the development and use of instrumental measurement of colour in pharmacy in recent ten years focusing on the drugs of synthetic origin and pharmaceutical auxiliary substances including their control.

Prolegomenon of the Czech pharmacognosy: 21^st century

Lubomír Opletal

Čes. slov. farm. 2013, 62(2):99-102  

The paper analyzes the basic features of the development of pharmacognosy as the oldest profile subject of pharmacy primarily in Europe during the 20^th century. Historical consequences of its development are declared, which should create the basis for its embedment, new content and tasks in Czech pharmacy of the 21^st century, especially in education at Czech universities.

Fytoterapia v súčasnej medicíne

Jozef Čižmárik

Čes. slov. farm. 2013, 62(2):106  

Dr.h.c., prof. RNDr. Jozef Čižmárik, PhD. - sedemdesiatnik

J. Lehotay

Čes. slov. farm. 2013, 62(2):103-104  

RNDr. PhMr. Štefan Mareček *20. 7. 1920 †28. 1. 2013

Margita Ondraská

Čes. slov. farm. 2013, 62(2):104-105