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Pharmacokinetic Comparisons of Benzoylmesaconine in Rats Using Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry after Administration of Pure Benzoylmesaconine and Wutou Decoction

机译:苯甲酰美沙酮碱和五头汤给药后超高效液相色谱-串联质谱法测定苯甲酰美沙酮在大鼠体内的药代动力学比较

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摘要

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 (T-1/2) 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.
机译:雾头汤因对类风湿关节炎具有治疗作用,因此在中国得到广泛应用。乌头汤中含量最丰富的成分苯甲酰美沙酮(BMA)被用作五头汤药代动力学研究的标志物。本研究的目的是比较口服纯BMA和五头汤对大鼠BMA的药代动力学。向大鼠口服纯BMA(5 mg / kg)和五头汤(0.54 g / kg,相当于5 mg / kg BMA),并在10小时内收集血样。使用灵敏且经过验证的超高效液相色谱-串联质谱(UPLC-MS / MS)对大鼠血浆中的BMA进行定量。具体来说,纯BMA的半衰期(T-1 / 2)和平均停留时间分别为228.3 +/- 117.0分钟和155.0 +/- 33.2分钟,而雾头汤中的BMA则降至61.8 + /-35.1分钟和55.8 +/- 16.4分钟。与纯BMA相比,五头汤给药后BMA的曲线下面积(AUC)明显减小(五倍)。结果表明,与纯BMA相比,乌头汤给药后大鼠对BMA的清除速度明显加快。

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