Abstract

Wutou decoction is widely used in China because of its therapeutic effect on rheumatoid arthritis. Benzoylmesaconine (BMA), the most abundant component of Wutou decoction, was used as the marker compound for the pharmacokinetic study of Wutou decoction. The aim of the present study was to compare the pharmacokinetics of BMA in rats after oral administration of pure BMA and Wutou decoction. Pure BMA (5 mg/kg) and Wutou decoction (0.54 g/kg, equivalent to 5 mg/kg BMA) were orally administered to rats with blood samples collected over 10 h. Quantification of BMA in rat plasma was achieved using sensitive and validated ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). Specifically, the half-life (T1/2) and mean residence time values of pure BMA were 228.3 ± 117.0 min and 155.0 ± 33.2 min, respectively, whereas those of BMA in Wutou decoction were decreased to 61.8 ± 35.1 min and 55.8 ± 16.4 min, respectively. The area under the curve (AUC) of BMA after administration of Wutou decoction was significantly decreased (five-fold) compared with that of pure BMA. The results indicate that the elimination of BMA in rats after the administration of Wutou decoction was significantly faster compared with that of pure BMA.

Highlights

  • Herbal medicine is mostly administered in combination based on the principle of traditional Chinese Medicine to achieve effect optimization or toxicity reduction

  • Pharmacokinetic study, a useful method to predict the in vivo process, has been used to elucidate the different processes between pure chemicals and multiple-ingredient prescriptions; it is important to conduct pharmacokinetic studies to evaluate the rationality of the traditional prescriptions

  • Since Wutou decoction has complex ingredients, herb-herb interactions may exert an influence on the efficacy of Chinese medicine; this study aims to compare the pharmacokinetics of BMA after oral administration of pure BMA and Wutou decoction to rats using a rapid, sensitive and reliable

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Summary

Introduction

Herbal medicine is mostly administered in combination based on the principle of traditional Chinese Medicine to achieve effect optimization or toxicity reduction. It is generally recognized that the combined use of prescriptions have a greater impact on the therapeutic effects. Pharmacokinetic study, a useful method to predict the in vivo process, has been used to elucidate the different processes between pure chemicals and multiple-ingredient prescriptions; it is important to conduct pharmacokinetic studies to evaluate the rationality of the traditional prescriptions. A well-known traditional prescription, comprises Radix Aconiti (derived from the dried root of Aconitum carmichaeli Debx.), Herba Ephedrae The decoction has been used for hundreds of years in China for rheumatoid arthritis (RA) treatment. Many studies have investigated the effects of Wutou decoction in patients with RA.

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