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| Content Provider | frontiers |
|---|---|
| Author | Li, Jie Li, Xin Ren, Yu-Shan Lv, Yuan-Yuan Zhang, Jun-Sheng Xu, Xiao-Li Wang, Xian-Zhen Yao, Jing-Chun Zhang, Gui-Min Liu, Zhong |
| Abstract | Although arctigenin (AG) has diverse bioactivities, such as anti-oxidant, anti-inflammatory, anti-cancer, immunoregulatory and neuroprotective activities, its pharmacokinetics have not been systematically evaluated. The purpose of this work was to identify the pharmacokinetic properties of AG via various experiments in vivo and in vitro. In this research, rats and beagle dogs were used to investigate the PK (pharmacokinetics, PK) profiles of AG with different drug-delivery manners, including intravenous (i.v), hypodermic injection (i.h), and sublingual (s.l) administration. The data shows that AG exhibited a strong absorption capacity in both rats and beagle dogs (absorption rate < 1 h), a high absorption degree (absolute bioavailability > 100%), and a strong elimination ability (t1/2 < 2 h). The tissue distributions of AG at different time points after i.h showed that the distribution of AG in rat tissues is rapid (2.5 h to reach the peak) and wide (detectable in almost all tissues and organs). The AG concentration in the intestine was the highest, followed by that in the heart, liver, pancreas, and kidney. In vitro, AG were incubated with human, monkey, beagle dog and rat liver microsomes. The concentrations of AG were detected by UPLC-MS/MS at different time points (from 0 min to 90 min). The percentages of AG remaining in four species’ liver microsomes were human (62 ± 6.36%) > beagle dog (25.9 ± 3.24%) > rat (15.7 ± 9%) > monkey (3.69 ± 0.12%). This systematic investi... |
| ISSN | 16639812 |
| DOI | 10.3389/fphar.2017.00376 |
| Volume Number | 8 |
| Journal | Frontiers in Pharmacology |
| Language | English |
| Publisher Date | 2017-06-14 |
| Access Restriction | Open |
| Subject Keyword | Arctigenin Bioavailability Pharmacokinetics UPLC/MS/MS Microsomes |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology Pharmacology (medical) |
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