The Role of Glass Transition Temperatures in Coamorphous Drug-Amino Acid Formulations

Molecular Pharmaceutics
Eric Ofosu KissiHolger Grohganz

Abstract

The improved physical stability associated with coamorphous drug-amino acid (AA) formulations may indicate a decrease in mobility of the amorphous drug molecules, compared to the neat amorphous form of the drug. Since the characteristic glass transition temperatures ( Tgα and Tgβ) represent molecular mobility in amorphous systems, we aimed to characterize Tgα and Tgβ and to determine their role in physical stability as well as their potential usefulness to determine the presence of an excess component (either drug or AA) in coamorphous systems. Indomethacin (IND)-tryptophan (TRP) and carvedilol (CAR)-TRP were used as model coamorphous systems. The analytical techniques used were X-ray powder diffractometry (XRPD) to determine the solid-state form, dynamic mechanical analysis (DMA) to probe Tgα and Tgβ, and differential scanning calorimetry (DSC) to probe thermal behavior of the coamorphous systems. Tgα analysis showed a gradual monotonous increase in Tgα values with increasing AA concentration, and this increase in the Tgα value is not the cause of the improved physical stability. The Tgβ analysis for the IND-TRP sample with 10% drug had a Tgβ of 226.8 K, and samples with 20-90% drug had similar Tgβ values around 212.5 K. For C...Continue Reading

References

Sep 1, 1971·Journal of Pharmaceutical Sciences·W L Chiou, S Riegelman
Jun 1, 1968·The Journal of Physical Chemistry·E Berlin, M J Pallansch
Jul 23, 2004·The Journal of Chemical Physics·K L Ngai, M Paluch
Jan 3, 2006·Pharmaceutical Research·Sergey Vyazovkin, Ion Dranca
Jul 23, 2008·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Norman ChiengThomas Rades
Apr 1, 2009·Journal of Controlled Release : Official Journal of the Controlled Release Society·Morten AllesøJaakko Aaltonen
Jun 6, 2009·Journal of Pharmaceutical Sciences·Sisir Bhattacharya, Raj Suryanarayanan
May 10, 2012·International Journal of Pharmaceutics·Riikka LaitinenThomas Rades
May 23, 2012·International Journal of Pharmaceutics·Korbinian LöbmannKeith C Gordon
Dec 4, 2012·Molecular Pharmaceutics·Sunny P BhardwajRaj Suryanarayanan
Mar 30, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Korbinian LöbmannThomas Rades
Apr 10, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Korbinian LöbmannHolger Grohganz
May 15, 2013·Profiles of Drug Substances, Excipients, and Related Methodology·Kevin BeattieJasmina Novakovic
Jun 1, 2014·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Swapnil J DengaleKrishnamurthy Bhat
Jun 10, 2015·Molecular Pharmaceutics·Katrine Tarp JensenThomas Rades
Jun 20, 2015·Molecular Pharmaceutics·Juraj SibikJ Axel Zeitler
Jan 26, 2016·Advanced Drug Delivery Reviews·Swapnil Jayant DengaleKorbinian Löbmann
Apr 7, 2016·Pharmaceutical Development and Technology·Ying HuangXuefeng Mei
Jul 3, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Katrine Tarp JensenHolger Grohganz
Oct 18, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Andreas BeyerClaudia S Leopold
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
Jul 21, 2020·Expert Opinion on Drug Delivery·Jiawei HanShuai Qian
Aug 6, 2020·Pharmaceutics·Bishal Raj AdhikariShyamal C Das
Feb 10, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Rong DiThomas Rades
Mar 23, 2021·Therapeutic Delivery·Ridhima SinghAbhay T Sangamwar
Apr 30, 2021·International Journal of Pharmaceutics·Dani Lakshman YarlagaddaKrishnamurthy Bhat
Jun 19, 2021·International Journal of Pharmaceutics·Jingwen LiuHolger Grohganz
Aug 29, 2021·Pharmaceutics·Do-Hyun KimJaeh-Wi Lee

❮ 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.

Related Papers

International Journal of Pharmaceutics
Georgia KastenThomas Rades
European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Katrine Tarp JensenHolger Grohganz
The Journal of Pharmacy and Pharmacology
Katrine Tarp JensenKorbinian Löbmann
© 2022 Meta ULC. All rights reserved