85. Jin, H., Hemingway, M.,
Gupta, R.B.; Xia, F., Zhao, Y., Preparation of thalidomide nano-flakes
by supercritical antisolvent with enhanced mass
transfer, Particuology 2012 10 (1), 17-23.
Abstract
Thalidomide
treats multiple myeloma and protracts
life-span of patient, but its bioavailability is limited as it is poorly water soluble. Thalidomide nano-flakes are produced to improve the drug dissolution rate. Two
nanoflake production methods are utilized for a comparative study: a
supercritical antisolvent (SAS) method and a supercritical antisolvent with enhanced mass transfer (SAS-EM). SAS-EM utilizes ultrasonication to improve dispersion upon injection within the
supercritical carbon dioxide.
Comparative study of SAS and SAS-EM thalidomide confirmed that the application of ultrasonication improved the micro/nano particles produced by SAS. The effects of
ultrasound power on the formation of thalidomide
particles are examined. The particle size and morphology
were characterized by SEM. The thalidomide nano-flakes produced
by SAS-EM were smaller
than the particles
produced by SAS. Dissolution rates of
the produced particles, evaluated by HPLC, demonstrated an increase in
the
thalidomide dissolution rate for
the
SAS-EM produced particles. The polymorphs and crystallinity of thalidomide particles
(flakes) were observed by
FTIR and XRD. In this research, the supercritical processing significantly modified the crystal formation of thalidomide from an original
state of a-polymorph to the amorphous state
b-polymorph after supercritical processing.
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