Methods of amorphization and investigation of the amorphous state

The amorphous form of pharmaceutical materials represents the most energetic solid state of a material. It provides advantages in terms of dissolution rate and bioavailability. This review presents the methods of solid- -state amorphization described in literature (supercooling of liquids, milling,...

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Bibliographic Details
Published in:Acta pharmaceutica (Zagreb, Croatia) Croatia), 2013-09, Vol.63 (3), p.305-334
Main Authors: Einfalt, Tomaž, Planinšek, Odon, Hrovat, Klemen
Format: Article
Language:English
Subjects:
amorphous solid preparation
Animals
Biological Availability
calorimetry
Chemistry, Pharmaceutical - methods
Chemistry, Pharmaceutical - trends
crystallinity
Crystallization
Desiccation - methods
Freeze Drying - methods
Freeze Drying - trends
Humans
Powders - chemistry
spectroscopy
X-Ray Diffraction - methods
X-Ray Diffraction - trends
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Summary:The amorphous form of pharmaceutical materials represents the most energetic solid state of a material. It provides advantages in terms of dissolution rate and bioavailability. This review presents the methods of solid- -state amorphization described in literature (supercooling of liquids, milling, lyophilization, spray drying, dehydration of crystalline hydrates), with the emphasis on milling. Furthermore, we describe how amorphous state of pharmaceuticals differ depending on the method of preparation and how these differences can be screened by a variety of spectroscopic (X-ray powder diffraction, solid state nuclear magnetic resonance, atomic pairwise distribution, infrared spectroscopy, terahertz spectroscopy) and calorimetry methods.
ISSN:1330-0075
1846-9558
DOI:10.2478/acph-2013-0026