Investigation of the impact of annealing on global molecular mobility in glasses: optimization for stabilization of amorphous pharmaceuticals

Journal of Pharmaceutical Sciences
Suman A LuthraMichael J Pikal

Abstract

The purpose of this research was to investigate the effect of annealing on the molecular mobility in lyophilized glasses using differential scanning calorimetry (DSC) and isothermal microcalorimetry (IMC) techniques. A second objective that emerged was a systematic study of the unusual pre-T(g) thermal events that were observed during DSC warming scans after annealing. Aspartame lyophilized with three different excipients; sucrose, trehalose and poly vinyl pyrrolidone (PVP) was studied. The aim of this work was to quantify the decrease in mobility in amorphous lyophilized aspartame formulations upon systematic postlyophilization annealing. DSC scans of aspartame:sucrose formulation (T(g) = 73 degrees C) showed the presence of a pre-T(g) endotherm which disappeared upon annealing. Aspartame:trehalose (T(g) = 112 degrees C) and aspartame:PVP (T(g) = 100 degrees C) showed a broad exotherm before T(g) and annealing caused appearance of endothermic peaks before T(g). This work also employed IMC to measure the global molecular mobility represented by structural relaxation time (tau(beta)) in both un-annealed and annealed formulations. The effect of annealing on the enthalpy relaxation of lyophilized glasses, as measured by DSC and IM...Continue Reading

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Citations

Feb 10, 2010·Pharmaceutical Research·Mark Cornell ManningDerrick S Katayama
Apr 24, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Norman ChiengMichael Pikal
May 15, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Masayasu Mizuno, Michael J Pikal
May 16, 2014·Journal of Pharmaceutical Sciences·Paul E Luner, Jeffery J Seyer
May 16, 2008·Journal of Pharmaceutical Sciences·Suman A LuthraMichael J Pikal
Sep 22, 2011·Journal of Pharmaceutical Sciences·Suman A LuthraJoseph W Lubach
Feb 22, 2011·Journal of Pharmaceutical Sciences·Satoshi Ohtake, Y John Wang
Nov 26, 2015·Molecular Pharmaceutics·Marcin SkotnickiPaul Hodgkinson
Apr 11, 2012·International Journal of Pharmaceutics·Sarah P HudsonPeter McLoughlin
Aug 17, 2011·Advanced Drug Delivery Reviews·Jared A Baird, Lynne S Taylor
Feb 15, 2011·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·N Perez-MoralR Parker
Apr 23, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Laurent HansenThomas De Beer
May 31, 2016·International Journal of Pharmaceutics·Yannick GuinetAlain Hédoux
Dec 17, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Luz María MartínezSamuel Castro
Oct 29, 2008·Molecular Pharmaceutics·J F Willart, M Descamps

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