mp200546p_si_001.pdf (348.95 kB)
Modification of Crystallization Behavior in Drug/Polyethylene Glycol Solid Dispersions
journal contribution
posted on 2012-03-05, 00:00 authored by Qing Zhu, Michael T. Harris, Lynne S. TaylorThe crystallization kinetics of various active pharmaceutical
ingredient/polyethylene glycol (API/PEG) solid dispersions has been
investigated using wide-angle X-ray diffraction (XRD) and Raman spectroscopy.
APIs with different physicochemical properties and crystallization
tendency were employed to form solid dispersions with PEG. The crystallization
rate of benzocaine (BZC) in BZC/PEG (20/80 wt %) solid dispersions
was decreased substantially in comparison to that of the pure API,
while the PEG matrix did not affect the crystallization behavior of
haloperidol (HLP). The induction time for crystallization of ibuprofen
(IBP) and fenofibrate (FNB) in a PEG matrix was decreased relative
to the induction times for pure IBP and FNB. For the latter systems,
it appears that crystalline PEG acted as a favorable heterogeneous
nucleation site. The crystallization behavior of PEG in the API/PEG
systems was also affected to different extents, depending on the API
studied. These results suggest that PEG can delay, promote or have
no influence on the crystallization kinetics of different APIs, and
that any effects on crystallization behavior should be investigated
in order to be able to produce a solid dispersion with consistent
properties.