Mechanically induced amorphization of drugs: a study of the thermal behavior of cryomilled compounds.

AAPS PharmSciTech
Niraj S Trasi, Stephen Byrn

Abstract

The purpose of this work was to determine what aspect of the milled compound influences its thermal profile. For this, six different compounds with different properties were chosen and cryomilled for different times to get an amorphous solid. Differential scanning calorimetry (DSC) and X-ray powder diffraction were used to characterize the material and look at the thermal behavior. Melt-quenched samples were also prepared, and the thermal profile upon milling was determined and correlated with the thermal behavior of the cryomilled samples. Growth rates were determined by hot-stage microscopy. Ketoconazole, when cryomilled, showed only one crystallization exotherm in the DSC profile. Ursodiol, and to some extent indomethacin, initially showed a double exotherm which eventually become a single exotherm on further milling. Griseofulvin, carbamazepine, and piroxicam exhibited a double exotherm in the DSC profile upon cryomilling to the amorphous state. Surface crystal growth rates around T (g) were found to be highest for compounds showing the double exotherm in the DSC. Thus, it was seen that compounds which have high surface crystallization tendency will exhibit the double exotherm during heating.

References

Aug 1, 1969·Journal of Pharmaceutical Sciences·J Haleblian, W McCrone
Jul 1, 1984·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·T UmedaY Matsuda
Feb 1, 1984·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·N KaneniwaM Otsuka
Oct 1, 1996·Journal of Pharmaceutical Sciences·L E McMahonP York
Jun 1, 1997·Pharmaceutical Research·E YonemochiK Yamamoto
Apr 16, 2003·International Journal of Pharmaceutics·F VrecerA Meden
Apr 9, 2005·International Journal of Pharmaceutics·Zohra ZiliHatem Fessi
Aug 11, 2006·The Journal of Physical Chemistry. B·Tian Wu, Lian Yu
Aug 24, 2006·Pharmaceutical Research·Meena RaniRaj Suryanarayanan
Aug 24, 2006·Pharmaceutical Research·Tian Wu, Lian Yu
Oct 6, 2006·Pharmaceutical Research·Simon BatesAnn Newman
Apr 25, 2007·Journal of Pharmaceutical Sciences·Hajime IshidaLian Yu
Oct 29, 2008·Molecular Pharmaceutics·J F Willart, M Descamps
Nov 18, 2008·International Journal of Pharmaceutics·Tao FengM Teresa Carvajal
May 13, 2009·Molecular Pharmaceutics·Deliang ZhouEric A Schmitt
May 13, 2009·Molecular Pharmaceutics·Lei ZhuLian Yu
Apr 24, 2010·Pharmaceutical Research·Lei ZhuTian Wu
May 22, 2010·Pharmaceutical Research·Niraj S TrasiStephen Robert Byrn
Jun 22, 2010·International Journal of Pharmaceutics·Shan-Yang LinWen-Ting Ke
Jul 14, 2010·Journal of Pharmaceutical Sciences·Jared A BairdLynne S Taylor
Jul 21, 2011·Physical Review Letters·L ZhuL Yu
Dec 17, 2011·Pharmaceutical Research·Sayantan ChattorajChangquan Calvin Sun
Jan 19, 2012·Journal of Pharmaceutical Sciences·Jean-François WillartMarc Descamps

❮ Previous
Next ❯

Citations

Oct 10, 2013·Journal of Pharmaceutical Sciences·Christian MuehlenfeldMarkus Thommes
May 21, 2013·Journal of Pharmaceutical Sciences·Jean-Francois WillartMarc Descamps
Jan 31, 2016·Advanced Drug Delivery Reviews·M Descamps, J F Willart
Jan 6, 2016·AAPS PharmSciTech·Justin S LaFountaineRobert O Williams
Oct 1, 2014·Faraday Discussions·William Jones, Mark D Eddleston
May 31, 2016·International Journal of Pharmaceutics·Yannick GuinetAlain Hédoux
Aug 24, 2018·Pharmaceutics·Maria Rosa GigliobiancoPiera Di Martino
Jan 5, 2020·AAPS PharmSciTech·Antoine TouzetYann Pellequer
Apr 23, 2020·Assay and Drug Development Technologies·Rajvi J WaniHarsh Chauhan
Dec 1, 2020·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Philip da IgrejaMarkus Thommes
Mar 23, 2021·Therapeutic Delivery·Ridhima SinghAbhay T Sangamwar
Mar 25, 2019·Journal of Pharmaceutical Sciences·Mansour LatrecheFlorence Danède
May 24, 2019·Molecular Pharmaceutics·Navpreet KaurRaj Suryanarayanan
Sep 28, 2020·International Journal of Pharmaceutics·Anthony DupontJean-François Willart

❮ 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.