Dielectric study of the molecular mobility and the isothermal crystallization kinetics of an amorphous pharmaceutical drug substance

Alie, J; Ménégotto, J.; Cardon, P; Duplaa, Hélène; Caron, A.; Lacabanne, C.; Bauer, Michel

doi:10.1002/jps.10520

Cited by 136 publications

(146 citation statements)

References 47 publications

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“…In a study performed by Alie et al, dynamic dielectric spectroscopy (DDS) and thermo-stimulated current spectroscopy (TSC), collectively referred to as dielectric spectroscopy (DS), were used to study molecular mobility. [116] DDS detects the complex dielectric permittivity and the dielectric loss factor. TSC is performed by polarizing the sample in an electrostatic field at a temperature that allows orientation, followed by a cooling step that brings the sample to a temperature where polarization can be retained.…”

Section: Alpha and Beta Mobilitymentioning

confidence: 99%

Review: physical chemistry of solid dispersions

2009

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Objectives With poorly soluble drug candidates emerging in the drug discovery pipeline, the importance of the solid dispersion formulation approach is increasing. This strategy includes complete removal of drug crystallinity, and molecular dispersion of the poorly soluble compound in a hydrophilic polymeric carrier. The potential of this technique to increase oral absorption and hence bioavailability is enormous. Nevertheless, some issues have to be considered regarding thermodynamic instability, as well in supersaturated solutions that are formed upon dissolution as in the solid state. Key findings After a brief discussion on the historical background of solid dispersions and their current role in formulation, an overview will be given on the physical chemistry and stability of glass solutions as they form supersaturated solutions, and during their shelf life. Conclusions Thorough understanding of these aspects will elicit conscious evaluation of carrier properties and eventually facilitate rational excipient selection. Thus, full exploitation of the solid dispersion strategy may provide an appropriate answer to drug attrition due to low aqueous solubility in later stages of development.

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Section: Alpha and Beta Mobilitymentioning

confidence: 99%

Review: physical chemistry of solid dispersions

2009

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“…Aso et al 4,5 demonstrated a correlation between molecular mobility calculated (using Vogel-Tammann-Fulcher (VTF), Adam-Gibbs-Vogel equation) at and below T g and the crystallization rates of phenobarbital, nifedipine, and their dispersions with poly vinyl pyrollidone (PVP). Alie et al 6 correlated beta relaxation (relaxation secondary to alpha motion in the glassy state) with characteristic crystallization rates of the compound (SSR) the authors investigated. Such studies suggest that correlations may exist for the two properties of the amorphous solids, i.e.…”

Section: Introductionmentioning

confidence: 98%

Prediction of the Onset of Crystallization of Amorphous Sucrose Below the Calorimetric Glass Transition Temperature from Correlations with Mobility

Bhugra

Rambhatla

Bakri

et al. 2007

Journal of Pharmaceutical Sciences

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“…Refs. [8][9][10][11][12][13]. The sign of crystallization is a decrease in intensity of the signal, and the crystal fraction/concentration of the sample is often obtained by assuming that the relaxation strength is proportional to the volume fraction of liquid in the sample [14][15][16].…”

mentioning

confidence: 99%

A systematic study of the isothermal crystallization of the mono-alcohol n-butanol monitored by dielectric spectroscopy

Hansen

Alba‐Simionesco

Niss

et al. 2015

The Journal of Chemical Physics

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Isothermal crystallization of the mono-hydroxyl alcohol n-butanol was studied with dielectric spectroscopy in real time. The crystallization was carried out using two different sample cells at 15 temperatures between 120 K and 134 K. For all temperatures, a shift in relaxation times to shorter times was observed during the crystallization process, which is characterized by a drop in relaxation strength. The two different sample environments induced quite different crystallization behaviors, consistent and reproducible over all studied temperatures. An explanation for the difference was proposed on the background of an Avrami and a Maxwell-Wagner analysis. Both types analysis suggest that the morphology of the crystal growth changes at a point during the crystallization. The differences between the cells can be explained by this transition taking place at different times for the two cells.

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Dielectric study of the molecular mobility and the isothermal crystallization kinetics of an amorphous pharmaceutical drug substance

Cited by 136 publications

References 47 publications

Review: physical chemistry of solid dispersions

Review: physical chemistry of solid dispersions

Prediction of the Onset of Crystallization of Amorphous Sucrose Below the Calorimetric Glass Transition Temperature from Correlations with Mobility

A systematic study of the isothermal crystallization of the mono-alcohol n-butanol monitored by dielectric spectroscopy

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