Sign In  |  Register  

DOI: 10.1208/s12249-012-9801-8Pages: 772-784

Mechanically Induced Amorphization of Drugs: A Study of the Thermal Behavior of Cryomilled Compounds

1. Purdue University, Department of Industrial and Physical Pharmacy

Correspondence to:
Niraj S. Trasi
Tel: +1-765-4966404
Fax: +1-765-4946545
Email: ntrasi@gmail.com

Close

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 Tg 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.

To access the full text, please Sign in

If you have institutional access, please click here

400 Views

  • Accepted: May 2, 2012
  • Online: May 15, 2012

Article Tools