Rheological studies of tautomerization kinetics in supercooled glibenclamide drug

Wojnarowska, Ż.; Wang, Yangyang; Sokolov, Alexei P.; Paluch, Marian

doi:10.1103/physreve.86.067104

Cited by 3 publications

(1 citation statement)

References 15 publications

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“…there are bands corresponding to νCN and βC–OH vibrations, while the NH band associated with the amide moiety of indapamide molecule is almost absent, one can conclude that the tautomeric equilibrium achieved at the melting temperature is conveyed into the amorphous material. In recent years, there has been a growing interest in experimental as well as theoretical studies of the tautomerization reaction. − This is due to likely serious consequences of the proton transfer. Especially, isomerization of pharmaceuticals becomes an important problem as various tautomers of one drug may reveal different pharmacological activity.…”

Section: Resultsmentioning

confidence: 99%

Molecular Dynamics, Physical Stability and Solubility Advantage from Amorphous Indapamide Drug

et al. 2013

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This study for the first time investigates physicochemical properties of amorphous indapamide drug (IND), which is a known diuretic agent commonly used in the treatment of hypertension. The solid-state properties of the vitrified, cryomilled and ball-milled IND samples were analyzed using X-ray powder diffraction (XRD), mass spectrometry, nuclear magnetic resonance (NMR), infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and broadband dielectric spectroscopy (BDS). These analytical techniques enabled us (i) to confirm the purity of obtained amorphous samples, (ii) to describe the molecular mobility of IND in the liquid and glassy state, (iii) to determine the parameters describing the liquid-glass transition i.e. Tg and dynamic fragility, (iv) to test the chemical stability of amorphous IND in various temperature conditions and finally (v) to confirm the long-term physical stability of the amorphous samples. These studies were supplemented by density functional theory (DFT) calculations and apparent solubility studies of the amorphous IND in 0.1 M HCl, phosphate buffer (pH=6.8), and water (25 and 37 °C).

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