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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 29, Number 4
BKCSDE 29(4)
April 20, 2008 

Biopharmaceutical Evaluation of a Solid Dispersion System Containing Sibutramine Freebase
Minsuk Lee, Heechul Chang, Taewan Kim, Junghwa Park, Bongsang Lee, Sung Hee Kim, Do-Hwan Kim, Bo Gyun Kim, Seong Tae Oh, Myung Joo Kang, Jong Hyeok Park, Jaehwi Lee*, Young Wook Choi*
Solid dispersion, Sibutramine freebase, Solubility, Pharmacokinetic behavior
To increase the solubility of sibutramine freebase, the solid dispersion was prepared using a fluid-bed granulator. The solid dispersion containing sibutramine freebase was characterized by differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). After filling the sibutramine solid dispersion in the gelatin hard capsule, we performed in vitro dissolution test, the stability test under accelerated conditions and pharmacokinetic study in beagle dogs. The DSC and XRD data showed that sibutramine solid dispersion would be amorphous state. The dissolution rate of sibutramine solid dispersion was significantly increased about 70% than sibutramine freebase. The stability of sibutramine solid dispersion capsules was equivalent or above to commercial product of sibutramine. In beagle dogs, the sibutramine solid dispersion showed equivalent pharmacokinetic behavior with commercial product of sibutramine hydrochloride. In conclusion, the solid dispersion system provided a possible way to overcome the low solubility of sibutramine freebase, and the sibutramine solid dispersion can be a bioequivalent with the commercial product in humans.
749 - 754
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