A5074390871- Analytical Chemistry and Chromatography
- Drug Solubulity and Delivery Systems
- Drug Transport and Resistance Mechanisms
- Protein purification and stability
- Electrochemical Analysis and Applications
- Analytical Methods in Pharmaceuticals
- Trace Elements in Health
- Free Radicals and Antioxidants
- Mass Spectrometry Techniques and Applications
- Cancer therapeutics and mechanisms
- Metal complexes synthesis and properties
- Chemical and Physical Properties in Aqueous Solutions
- Sirtuins and Resveratrol in Medicine
- Organic Chemistry Cycloaddition Reactions
- Pharmaceutical studies and practices
- Tea Polyphenols and Effects
- Adsorption and biosorption for pollutant removal
- Antibiotics Pharmacokinetics and Efficacy
- Microfluidic and Capillary Electrophoresis Applications
- Surfactants and Colloidal Systems
- Inorganic and Organometallic Chemistry
- Advanced Drug Delivery Systems
- Analytical Chemistry and Sensors
- Computational Drug Discovery Methods
- Bioactive Compounds and Antitumor Agents
Semmelweis University
2001-2019
Hungarian Academy of Sciences
2001-2019
Lapatinib (LAP), the tyrosine kinase inhibitor drug with moderate bioavailability, was characterized in terms of physicochemical properties: acid-base characteristics, lipophilicity, and solubility. The highly lipophilic nature its extremely low water solubility (<mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML" id="M1"><mml:msub><mml:mrow><mml:mi>S</mml:mi></mml:mrow><mml:mrow><mml:mn fontstyle="italic">0</mml:mn></mml:mrow></mml:msub><mml:mo>=</mml:mo><mml:mn...
Erlotinib (ERL), the anticancer drug of poor bioavailability, was quantified in terms bio-relevant physicochemical parameters, such as acid–base properties, lipophilicity and solubility, a comprehensive study on its inclusion complexation carried out. The protonation constant ERL (log K = 5.32) indicates that it exists mainly deprotonated form at pH blood plasma. high p 2.75) explains good permeability, while very low solubility (S0 12.46 μM) causes bioavailability renders injection...
The aim of this study is to confirm the formation inclusion complexes between bifonazole (BFZ) and different cyclodextrin (CD) derivatives. Bifonazole, an imidazole antifungal derivative,is a very hydrophobic compound, which major drawback in obtaining topical pharmaceutical formulations with optimal bioavailability. Cyclodextrins may increase local drug delivery by enhancing release and/or permeation. binary systems cyclodextrins were prepared two molar ratios physical-mixture methods.The...
A novel method was elaborated, and a set of 1H NMR-pH indicator molecules selected to develop an NMR-based pH determination method, which does not need any glass or other electrodes separate reference compound, being thus devoid the usual acid base errors combined electrodes. The utilizes organic compounds accurately known basicity two more carbon-bound protons, whose chemical shifts respond differently changes. Accurate protonation constants in extrema achieved by relative basicities using...
Spectinomycin, a tricyclic aminoglycoside antibiotic with peculiar chemical structure and pharmacological profile was characterized in terms of microscopic protonation constants. 1H-15N HMBC–pH titrations were carried out to allocate the order basicities two similar methylamino functions spectinomycin, 1H NMR–pH performed on spectinomycin actinamine, its symmetrical model compound determine basicity amino sites. It found that moiety position 3 is some 60% higher than counterpart 1, at one...
Clotrimazole, a widely used imidazole-type antifungal agent and its cyclodextrin complexes were studied. Stoichiometries, structures stability constants of the inclusion with fourteen different derivatives characterized using NMR spectroscopy as primary technique. The found to be high (logK ] 2). 2D ROESY spectra revealed formation isomeric every highest constant was observed sulfobutylated β-CD, interestingly enough heptakis(2,3,6-tri-O-methyl)-β-cyclodextrin showed lowest stability.
Ezetimibe, the antihyperlipidemic drug of poor bioavailability was complexed with native and derivatized cyclodextrins.The complexes were characterized in terms stability, stoichiometry structure using various 1D 2D solution NMR spectroscopic techniques. The found to be moderate stability (logK[3). least stable inclusion complex is formed b-cyclodextrin, while ezetimibe-methylated-b--cyclodextrin has a 7-fold higher stability. results can useful improve water-solubility concomitant ezetimibe.