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口服给药后白芍及其经硫磺熏蒸白芍中典型成分的药代动力学比较。

Pharmacokinetic comparisons of typical constituents in white peony root and sulfur fumigated white peony root after oral administration to mice.

机构信息

Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, China.

出版信息

J Ethnopharmacol. 2010 May 27;129(2):167-73. doi: 10.1016/j.jep.2009.12.040. Epub 2010 Jan 4.

Abstract

AIM

White peony root and sulfur fumigated white peony root are produced by different processing methods from the root of Paeonia lactiflora Pall, but the two traditional Chinese medicines are used under the same common name white peony root. In order to clarify the influence of sulfur fumigation on pharmacokinetics of the main monoterpene glucoside components in white peony root, an investigation was carried out to compare the pharmacokinetics of sodium paeoniflorin sulfonate (1) and paeoniflorin (2), benzoylpaeoniflorin sulfonate (3) and benzoylpaeoniflorin (4), as well as 1 in sulfur fumigated white peony root extract (SWPE) and 2 in white peony root extract (WPE).

MATERIALS AND METHODS

A high-performance liquid chromatographic (HPLC) assay was developed to determine the plasma concentrations of the four analytes. Kunming species of mice were orally administered the four compounds and the two extracts with approximately the same dose.

RESULTS

It was found that C(max) and AUC of 1 and 3 were increased (P<0.05), and the T(max) and t(1/2) were prolonged (P<0.05) by comparison with that of 2. Similar results were also observed for the pharmacokinetics parameters of 1 in SWPE and 2 in WPE. However, benzoylpaeoniflorin (4) was not detected in plasma collected at certain intervals after administered orally to mice.

CONCLUSIONS

These results indicate that sulfonation of the monoterpene components could improve the bioavailability and delay the absorption of them in mice.

摘要

目的

白芍和醋白芍是由芍药的根经不同的炮制方法制成的,但这两种中药都以白芍的通用名使用。为了阐明硫磺熏制对白芍中主要单萜苷类成分药代动力学的影响,本研究比较了磺酸钠芍药苷(1)和芍药苷(2)、苯甲酰芍药苷磺酸钠(3)和苯甲酰芍药苷(4),以及硫磺熏制白芍提取物(SWPE)中 1 和白芍提取物(WPE)中 2 的药代动力学。

材料与方法

建立了一种高效液相色谱(HPLC)测定法,用于测定四种分析物的血浆浓度。昆明种小鼠分别给予四种化合物和两种提取物,剂量大致相同。

结果

与 2 相比,1 和 3 的 C(max)和 AUC 增加(P<0.05),T(max)和 t(1/2)延长(P<0.05)。SWPE 中 1 和 WPE 中 2 的药代动力学参数也观察到类似的结果。然而,苯甲酰芍药苷(4)在给小鼠口服后某些时间点采集的血浆中未检测到。

结论

这些结果表明,单萜类成分的磺化可以提高其生物利用度,并延缓其在小鼠体内的吸收。

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