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Molecules 2015, 20(1), 1560-1570; doi:10.3390/molecules20011560

Comparative Pharmacokinetics of Hypaconitine after Oral Administration of Pure Hypaconitine, Aconitum carmichaelii Extract and Sini Decoction to Rats

Department of Pharmacy, Eastern Hepatobiliary Surgery Hospital, Second Military Medical University, Shanghai 200438, China
These authors contributed equally to this work.
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Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 22 October 2014 / Accepted: 7 January 2015 / Published: 16 January 2015
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Hypaconitine (HC) is one of the main aconitum alkaloids in Aconitum carmichaelii (AC), which is considered to be effective on cardiovascular disease, although it also has high toxicity. Sini Decoction (SND), composed of Aconitum carmichaelii, Glycyrrhiza uralensis and Zingiber officinale, is a traditional Chinese multi-herbal formula for recuperating the depleted yang. The aim of this study was to compare the pharmacokinetics of HC in rat plasma after oral administration of HC, AC extract and SND, and investigate the effect of other two herbal ingredients on absorption, metabolism and elimination of HC. A sensitive and specific LC-MS/MS method was developed to determine HC in rat plasma. Eighteen male Sprague-Dawley rats were randomly assigned to three groups: HC, AC and SND group. Plasma concentrations of HC were determined at designated points after oral administration, and main pharmacokinetic parameters were estimated. It was found that there was obvious difference (p < 0.05) on the pharmacokinetic parameters among three groups. Compared with AC group, Tmax, Cmax, k, AUC(0-24) and AUC(0-∞) decreased in SND group, while t1/2 and MRT had been lengthened, which indicated that the ingredients in other two herbs could influence the pharmacokinetic behavior of HC. View Full-Text
Keywords: hypaconitine; Aconitum carmichaelii; Sini decoction; pharmacokinetics; LC-MS/MS hypaconitine; Aconitum carmichaelii; Sini decoction; pharmacokinetics; LC-MS/MS
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Zhang, W.; Zhang, H.; Sun, S.; Sun, F.-F.; Chen, J.; Zhao, L.; Zhang, G.-Q. Comparative Pharmacokinetics of Hypaconitine after Oral Administration of Pure Hypaconitine, Aconitum carmichaelii Extract and Sini Decoction to Rats. Molecules 2015, 20, 1560-1570.

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