Imperatorin sustained-release tablets: In Vitro and pharmacokinetic studies
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- 作者：Jingjing Pan (1)
Wen Lu (1)
Changhui Li (1)
Sicen Wang (1)
Langchong He (1) - 关键词：Imperatorin ; Hydroxypropyl methylcellulose ; Carbopol 934P ; Sustained release ; Pharmacokinetics
- 刊名：Archives of Pharmacal Research
- 出版年：2010
- 出版时间：August 2010
- 年：2010
- 卷：33
- 期：8
- 页码：1209-1216
- 全文大小：532KB
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Wen Lu (1)
Changhui Li (1)
Sicen Wang (1)
Langchong He (1)
1. School of Medicine, Xi鈥檃n Jiaotong University, Xi鈥檃n, 710061, China - ISSN：1976-3786
文摘
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.