Pharmacokinetics and tissue distribution of coptisine in rats after oral administration by liquid chromatography–mass spectrometry. (1st February 2017)

• Record Type: Journal Article
• Authors: Yan, Yu; Zhang, Huifang; Zhang, Zhihui; Song, Junke; Chen, Yucai; Wang, Xiaobo; He, Yangyang; Qin, Hailin; Fang, Lianhua; Du, Guanhua
• Is Part Of: Biomedical chromatography. Volume 31:Number 7(2017:Jul.)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2017-02-01
• Subjects: bioavailability -- coptisine -- liquid chromatography–mass spectrometry -- pharmacokinetics -- tissue distribution; Chromatographic analysis -- Periodicals; Biology -- Periodicals; Medicine -- Periodicals; Biology -- Periodicals; Chromatography -- methods -- Periodicals; Medicine -- Periodicals; 543.089
• DOI: 10.1002/bmc.3918
• Languages: English
• ISSNs: 0269-3879

Abstract

Abstract: Coptisine, one of the main components isolated from Coptidis rhizoma, has been reported to have many beneficial pharmacological effects including anti‐inflammatory, anti‐hypercholesterolemia, neuroprotective and cardioprotective properties. However, to date the information related to the in vivo pharmacokinetics (PK) of coptisine is very limited. The purposes of our study are to establish a fast and sensitive quantification method of coptisine using liquid chromatography–mass spectrometry (LC–MS) and evaluate the PK profile of coptisine in rats. The calibration curve for coptisine was linear from 0.78 to 50 ng/mL. After single‐dose oral administration of coptisine, the mean peak plasma concentration values for groups treated with 30, 75 and 150 mg/kg doses ranged from 44.15 to 66.89 ng/mL, and the mean area under the concentration–time curve values ranged from 63.24 to 87.97 mg/L h. The absolute bioavailability was calculated to range from 1.87 to 0.52%. Coptisine remained in all analyzed samples at low concentrations after oral administration of 30 mg/kg.