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Determination and Pharmacokinetic Study of Gentiopicroside, Geniposide, Baicalin, and Swertiamarin in Chinese Herbal Formulae after Oral Administration in Rats by LC-MS/MS

by Chia-Ming Lu 1, Lie-Chwen Lin 1,2 and Tung-Hu Tsai 1,3,4,5,*
1
Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, No. 155, Sec. 2, Li-Nong St, Beitou District, Taipei 11221, Taiwan
2
National Research Institute of Chinese Medicine, No. 155-1, Sec. 2, Li-Nong St., Beitou District, Taipei 11221, Taiwan
3
Graduate Institute of Acupuncture Science, China Medical University, No. 91, Hsueh-Shih Road, Taichung 404, Taiwan
4
School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, No. 100, Shih-Chuan 1st Road, Kaohsiung 80708, Taiwan
5
Department of Education and Research, Taipei City Hospital, No.145, Zhengzhou Rd., Datong Dist., Taipei 103, Taiwan
*
Author to whom correspondence should be addressed.
Molecules 2014, 19(12), 21560-21578; https://doi.org/10.3390/molecules191221560
Received: 2 November 2014 / Revised: 1 December 2014 / Accepted: 17 December 2014 / Published: 22 December 2014
(This article belongs to the Section Natural Products Chemistry)
A sensitive and efficient liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for the simultaneous determination of gentiopicroside, geniposide, baicalin, and swertiamarin in rat plasma. To avoid the stress caused by restraint or anesthesia, a freely moving rat model was used to investigate the pharmacokinetics of herbal medicine after the administration of a traditional Chinese herbal prescription of Long-Dan-Xie-Gan-Tang (10 g/kg, p.o.). Analytes were separated by a C18 column with a gradient system of methanol–water containing 1 mM ammonium acetate with 0.1% formic acid. The linear ranges were 10–500 ng/mL for gentiopicroside, geniposide, and baicalin, and 5–250 ng/mL for swertiamarin in biological samples. The intra- and inter-day precision (relative standard deviation) ranged from 0.9% to 11.4% and 0.3% to 14.4%, respectively. The accuracy (relative error) was from −6.3% to 10.1% at all quality control levels. The analytical system provided adequate matrix effect and recovery with good precision and accuracy. The pharmacokinetic data demonstrated that the area under concentration-time curve (AUC) values of gentiopicroside, geniposide, baicalin, and swertiamarin were 1417 ± 83.8, 302 ± 25.8, 753 ± 86.2, and 2.5 ± 0.1 min µg/mL. The pharmacokinetic profiles provide constructive information for the dosage regimen of herbal medicine and also contribute to elucidate the absorption mechanism in herbal applications and pharmacological experiments. View Full-Text
Keywords: phytochemical analysis; LC-MS/MS; herbal medicine; pharmacokinetics; traditional Chinese medicine phytochemical analysis; LC-MS/MS; herbal medicine; pharmacokinetics; traditional Chinese medicine
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Lu, C.-M.; Lin, L.-C.; Tsai, T.-H. Determination and Pharmacokinetic Study of Gentiopicroside, Geniposide, Baicalin, and Swertiamarin in Chinese Herbal Formulae after Oral Administration in Rats by LC-MS/MS. Molecules 2014, 19, 21560-21578.

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