Acta Pharm. 63 (2013) 305-334

 

full paper

Review

 

Methods of amorphization and investigation of the amorphous state

TOMAŽ EINFALT, ODON PLANINŠEK and KLEMEN HROVAT

tommy.einfalt@gmail.com

University of Ljubljana, Faculty of Pharmacy, 1000 Ljubljana, Slovenia

Accepted April 26, 2013

 

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 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.

 

Keywords: amorphous solid preparation, crystallinity, spectroscopy, calorimetry