Therapy of oral, esophageal and gastrointestinal candidiasis is still a common problem that can be solved by an administration of antimycotics. Major disadvantage of registered commercial antifungal medicinal products is their price, so the health care system and its payers may profit from extemporaneous compounding. An appropriate drug therapy for candidiasis (trush) is nystatin, which is a substance available in the Czech Republic for the magistral preparation relatively recently, since 2010. Making formulas for extemporaneous compounding is quite simple and preparations particularly useful for dentists, pediatricians, otolaryngologists, oncologists and gastroenterologists. The authors formulated composition of viscous oromucosal suspension, oral/oromucosal hydrogel and oromucosal gelatine globule which may be present as compounded products containing nystatin for oromucosal and/or oral administration. The preparation is practically verified and magistral products have been already used in clinical practice.
- MeSH
- antifungální látky aplikace a dávkování chemie MeSH
- aplikace bukální MeSH
- aplikace orální MeSH
- farmaceutická chemie MeSH
- farmaceutická technologie metody MeSH
- glycerol chemie MeSH
- hydrogely MeSH
- kandidóza farmakoterapie mikrobiologie MeSH
- lidé MeSH
- methylcelulosa analogy a deriváty chemie MeSH
- nystatin aplikace a dávkování chemie MeSH
- příprava léků MeSH
- viskozita MeSH
- xylitol chemie MeSH
- želatina chemie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
New antifungal agents are needed to treat life-threatening fungal infections, particularly with the development of resistance. Surface-active antifungals have the advantages of minimizing host toxicity and the emergence of drug resistance. We have developed a time-dependent drug exposure assay that allows us to rapidly investigate the mechanism of surface-active antifungal drug action. The assay uses a multidrug pump-deficient strain of Saccharomyces cerevisiae and the potentiometric dye 3,3'-dipropylthiacarbocyanine iodide [diS-C₃(3)] and can assess whether cells are depolarized, hyperpolarized, or permeabilized by drug exposure. In this work, we investigated the mechanisms of action of five surface-active compounds: SDS, nystatin, amphotericin B, octenidine dihydrochloride, and benzalkonium chloride. The diS-C₃(3) time-dependent drug exposure assay can be used to identify the mechanisms of action of a wide range of drugs. It is a fast and cost-effective method for screening drugs to determine their lowest effective concentrations.
- MeSH
- amfotericin B chemie farmakologie MeSH
- antifungální látky chemie farmakologie MeSH
- benzalkoniové sloučeniny chemie farmakologie MeSH
- dodecylsíran sodný chemie farmakologie MeSH
- fluorescenční spektrometrie MeSH
- kinetika MeSH
- mikrobiální testy citlivosti metody MeSH
- nystatin chemie farmakologie MeSH
- permeabilita buněčné membrány účinky léků MeSH
- povrchově aktivní látky chemie farmakologie MeSH
- pyridiny chemie farmakologie MeSH
- Saccharomyces cerevisiae cytologie účinky léků genetika MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
A new targeted intravenous conjugate of nystatin with pentaerythritol poly(ethylene glycol)ether has been prepared and characterised (NY(4)-sPEG, M=25 160). The conjugate contains a beta-d-glucopyranoside molecular switch sensitive to beta-glucosidases (E.C.3.2.1.21), which are specifically present in the enzyme outfit of fungal pathogens. The investigated conjugate is stable under in vitro conditions for 24h (solution of phosphate buffer pH=7.4). Spectrophotometrically controlled releasing of nystatin in model medium containing beta-glucosidase ((Aspergillus niger) 2mg/mL, 66.6 units/g; pH 7.4, 2 x 10(-2)M), reported decomposition half-life of conjugate tau(1/2)=(88+/-2)s. This implies that releasing of nystatin is controlled only enzymatically.
- MeSH
- antifungální látky aplikace a dávkování chemie metabolismus MeSH
- Aspergillus niger enzymologie MeSH
- celulasy izolace a purifikace metabolismus MeSH
- farmaceutická chemie MeSH
- farmaceutická technologie metody MeSH
- gelová chromatografie MeSH
- hydrolýza MeSH
- kinetika MeSH
- koncentrace vodíkových iontů MeSH
- léky s prodlouženým účinkem MeSH
- magnetická rezonanční spektroskopie MeSH
- nosiče léků MeSH
- nystatin aplikace a dávkování chemie metabolismus MeSH
- poločas MeSH
- polyethylenglykoly chemie MeSH
- příprava léků MeSH
- propylenglykoly chemie MeSH
- pufry MeSH
- rozpustnost MeSH
- spektrofotometrie ultrafialová MeSH
- stabilita léku MeSH
- vysokoúčinná kapalinová chromatografie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
