Glass-Transition Temperature of the β-Relaxation as the Major Predictive Parameter for Recrystallization of Neat Amorphous Drugs

The Journal of Physical Chemistry. B
Eric Ofosu KissiThomas Rades

Abstract

Recrystallization of amorphous drugs is currently limiting the simple approach to improve solubility and bioavailability of poorly water-soluble drugs by amorphization of a crystalline form of the drug. In view of this, molecular mobility, α-relaxation and β-relaxation processes with the associated transition temperatures Tgα and Tgβ, was investigated using dynamic mechanical analysis (DMA). The correlation between the transition temperatures and the onset of recrystallization for nine amorphous drugs, stored under dry conditions at a temperature of 296 K, was determined. From the results obtained, Tgα does not correlate with the onset of recrystallization under the experimental storage conditions. However, a clear correlation between Tgβ and the onset of recrystallization was observed. It is shown that at storage temperature below Tgβ, amorphous nifedipine retains its amorphous form. On the basis of the correlation, an empirical correlation is proposed for predicting the onset of recrystallization for drugs stored at 0% RH and 296 K.

References

Jan 1, 1997·Journal of Pharmaceutical Sciences·B C Hancock, G Zografi
Feb 1, 1989·Physical Review. B, Condensed Matter·J Y CavailleG P Johari
Feb 4, 1985·Physical Review Letters·J M Carpenter, D L Price
Jul 23, 2004·The Journal of Chemical Physics·K L Ngai, M Paluch
Aug 5, 2004·Pharmaceutical Research·Rahul SuranaRaj Suryanarayanan
Jul 20, 2005·International Journal of Pharmaceutics·Paul G RoyallMarc B Brown
Jan 3, 2006·Pharmaceutical Research·Sergey Vyazovkin, Ion Dranca
May 29, 2007·The Journal of Physical Chemistry. B·Sergey Vyazovkin, Ion Dranca
Aug 28, 2007·Journal of Pharmaceutical Sciences·Chandan Bhugra, Michael J Pikal
Jul 29, 2008·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Pekka HoppuAnne Mari Juppo
Jan 27, 2009·International Journal of Pharmaceutics·Denny MahlinPaul G Royall
Apr 28, 2009·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Kirsten A GraeserThomas Rades
May 13, 2009·Molecular Pharmaceutics·Deliang ZhouEric A Schmitt
Jun 6, 2009·Journal of Pharmaceutical Sciences·Sisir Bhattacharya, Raj Suryanarayanan
Dec 24, 2011·Advanced Drug Delivery Reviews·David S JonesGavin P Andrews
Jun 20, 2015·Molecular Pharmaceutics·Juraj SibikJ Axel Zeitler
Jun 20, 2015·The Journal of Physical Chemistry. B·S CapaccioliD Prevosto
Jul 25, 2015·Nature Communications·Q WangJ Lu
Aug 4, 2015·Molecular Pharmaceutics·Katarzyna NurzyńskaPeter M Fischer
Sep 1, 2015·The Journal of Physical Chemistry. B·K L NgaiLi-Min Wang
Sep 5, 2015·The Journal of Physical Chemistry. B·K L NgaiLi-Min Wang
Sep 6, 2015·International Journal of Pharmaceutics·Amjad AlhalawehChristel A S Bergström
Feb 20, 2016·Molecular Pharmaceutics·Mehak MehtaRaj Suryanarayanan
Feb 10, 2017·The Journal of Chemical Physics·Marcus T Cicerone, Madhusudan Tyagi
Nov 3, 2017·Physical Chemistry Chemical Physics : PCCP·Michael T RuggieroJ Axel Zeitler

❮ Previous
Next ❯

Citations

Aug 31, 2019·Physical Chemistry Chemical Physics : PCCP·Eric Ofosu KissiKorbinian Löbmann
Apr 18, 2020·Physical Chemistry Chemical Physics : PCCP·Thomas KörberErnst A Rössler
Mar 8, 2020·Nature Communications·Peter Ouma OkeyoAnja Boisen
Nov 8, 2020·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Luke I ChambersJonathan W Steed
Aug 21, 2020·Journal of Pharmaceutical Sciences·Andrew Toye Ojo, Ping I Lee
Mar 23, 2021·Therapeutic Delivery·Ridhima SinghAbhay T Sangamwar
Apr 23, 2021·Journal of Materials Chemistry. B, Materials for Biology and Medicine·A P P FugolinC S Pfeifer
Apr 23, 2021·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Tobias Palle HolmRagna Berthelsen
Aug 8, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Eric Ofosu KissiIngunn Tho
Nov 8, 2019·The Journal of Physical Chemistry. B·Felix KrohnHans-Werner Schmidt
Nov 24, 2018·Journal of the American Chemical Society·Maximilian KarlThomas Rades
Oct 24, 2018·Molecular Pharmaceutics·Sofia ValentiRoberto Macovez
Jul 19, 2018·Molecular Pharmaceutics·Eric Ofosu KissiHolger Grohganz
Sep 22, 2018·The Journal of Physical Chemistry Letters·Hai-Bin YuKonrad Samwer
Jun 13, 2019·ACS Applied Materials & Interfaces·Liyang YuChristian Müller
Aug 31, 2021·Advanced Drug Delivery Reviews·Benedict BrownKofi Asare-Addo
Oct 14, 2021·Scientific Reports·Michela RomaniniJosep Lluís Tamarit

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.