The application of pesticides and chemical fertilizers constitutes a potential risk to human and animals due to the presence of their residues in the food. Thiacloprid belongs to a group of neonicotinoid insecticides. It shows a cytotoxic/cytostatic effect in human peripheral blood lymphocytes probably due to DNA damage. The use of thiacloprid is increasingly widespread worldwide, therefore is very important the assessment of its possible genotoxic and cytotoxic effects on a living organism. That is the reason why we studied the thiacloprid influence on the structure and stability of DNA in presented work. We have been studied the thiacloprid interaction with calf thymus DNA. Association constant was determined by fluorescence spectroscopy using equilibrium receptor-ligand binding analysis. The thermal denaturation of DNA was used to identify the mode of interaction. Viscosity changes were recorded to confirm/disconfirm the intercalation mode of interaction. Given the results, we can conclude that neonicotinoid pesticide thiacloprid destabilizes DNA. It changes the structure and stability of DNA through binding into the minor groove by hydrophobic or hydrogen interactions.
The purpose of this work was to develop a new supergeneric product Meloxicam/Omeprazole. Such a combination brings a benefit in terms of decreasing side effects for the patients using meloxicam. The new combination is composed of a meloxicam powder blend (MPB) and omeprazole gastro-resistant pellets (OAP) in hard gelatin capsules. The main tasks were to select the excipients to keep the functional layer of OAP active and to prove the bioequivalence to the original products of meloxicam tablets together with omeprazole capsules. Although dissolution profiles similar to the original product were obtained, the unexpected results of omeprazole low bioavailability in the fed bioequivalence study (BES I) showed the necessity to investigate the formulation in greater depth. A modified more complex dissolution method was developed in order to understand the release of omeprazole under gastric conditions. This method revealed the degradation of omeprazole in the formulation when exposed to the fed conditions because of the increase in microenvironmental pH in the capsule caused by trisodium citrate, commonly used for improving solubility of meloxicam. This pH increase dissolved the gastro-resistant layer of OAP and caused the chemical degradation. To prevent this effect, a trisodium citrate-free formulation was developed. Reformulated capsules passed the repeated fed bioequivalence study (BES II).
- MeSH
- antiflogistika nesteroidní * aplikace a dávkování chemie farmakokinetika MeSH
- chemie farmaceutická MeSH
- citráty chemie MeSH
- fixní kombinace léků MeSH
- klinické křížové studie MeSH
- koncentrace vodíkových iontů MeSH
- lidé MeSH
- meloxikam MeSH
- omeprazol * aplikace a dávkování chemie farmakokinetika MeSH
- pomocné látky chemie MeSH
- prášky, zásypy, pudry MeSH
- protivředové látky * aplikace a dávkování chemie farmakokinetika MeSH
- terapeutická ekvivalence MeSH
- thiaziny * aplikace a dávkování chemie farmakokinetika MeSH
- thiazoly * aplikace a dávkování chemie farmakokinetika MeSH
- tobolky MeSH
- uvolňování léčiv MeSH
- želatina chemie MeSH
- Check Tag
- lidé MeSH
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- klinické zkoušky MeSH
Herein we report the polymer-supported synthesis of 3,4-dihydro-2H-1,4-oxazine-3-carboxylic acid derivatives using immobilized Fmoc-Ser(tBu)-OH and Fmoc-Thr(tBu)-OH as the starting materials. After the solid-phase-synthesis of N-alkyl-N-sulfonyl/acyl intermediates, the target dihydrooxazines were obtained using trifluoroacetic acid-mediated cleavage from the resin. This approach was also studied for the preparation of dihydrothiazines from immobilized Fmoc-Cys(Trt)-OH. Inclusion of triethylsilane in the cleavage cocktail resulted in the stereoselective formation of the corresponding morpholine/thiomorpholine-3-carboxylic acids. Stereochemical studies revealed the specific configuration of the newly formed stereocenter and also the formation of stable N-acylmorpholine rotamers.
- MeSH
- fluoreny chemie MeSH
- kyseliny karboxylové chemická syntéza chemie MeSH
- morfoliny chemická syntéza chemie MeSH
- oxaziny chemická syntéza chemie MeSH
- polymery chemie MeSH
- stereoizomerie MeSH
- techniky syntézy na pevné fázi metody MeSH
- thiaziny chemická syntéza chemie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
A brief survey of the artificial sweeteners and their properties and use aims to show the importance of this group of mainly renewable materials, to contribute to the knowledge of the practical chemistry that can be utilized, among others, in food and pharmaceutical industry. The article is also aimed as a teaching tool for teachers and students.
- MeSH
- aspartam chemie metabolismus škodlivé účinky MeSH
- bezpečnost potravin * MeSH
- chemické látky - účinky a užití MeSH
- cyklamáty chemie metabolismus škodlivé účinky MeSH
- dipeptidy chemie metabolismus terapeutické užití MeSH
- diterpeny kauranové chemie metabolismus škodlivé účinky MeSH
- konzumní sacharóza chemie metabolismus škodlivé účinky MeSH
- lidé MeSH
- nutriční hodnota MeSH
- potravní doplňky * MeSH
- sacharin analogy a deriváty chemie metabolismus škodlivé účinky MeSH
- sacharosa škodlivé účinky MeSH
- sladidla * aplikace a dávkování klasifikace metabolismus škodlivé účinky MeSH
- spotřebitelská bezpečnost produktů MeSH
- thiaziny chemie metabolismus škodlivé účinky MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- práce podpořená grantem MeSH
