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KMID : 0043320100330081209
Archives of Pharmacal Research
2010 Volume.33 No. 8 p.1209 ~ p.1216
Imperatorin sustained-release tablets: In Vitro and pharmacokinetic studies
Pan Jingjing

Lu Wen
Li Changhui
Wang Sicen
He Langchong
Abstract
We prepared and evaluated imperatorin (IMP) sustained-release tablets. IMP is an active compound in Angelica dahuricae, a Chinese herbal medicine. We used different polymers, such as hydroxypropyl methylcellulose (HPMC K4M, K15M, and K100M), carbopol 934P, sodium carboxymethyl cellulose (CMC-Na), and their combinations to prepare the matrix tablets and achieve the desired sustained release profile. The in vitro release profiles of these formulations were examined and fit to various kinetic release models. We also tested the effects of polymer combination ratios on the in vitro release rate. In vivo studies were performed for the optimized formulation in six beagle dogs, and pharmacokinetic parameters were compared with plain IMP tablets. IMP sustained-release tablets exhibited a more sustained plasma concentration than the plain tablets, with a relative bioavailability of 127.25%. The in vitro releases rates and in vivo absorption correlated for the initial 8 hours. These results demonstrate that the sustained-release tablet system can effectively control the release of IMP.
KEYWORD
Imperatorin, Hydroxypropyl methylcellulose, Carbopol 934P, Sustained release, Pharmacokinetics
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