Dai Pei-Min, Wang Ying, Ye Ling, Zeng Shan, Zheng Zhi-Jie, Li Qiang, Lu Lin-Liu, Liu Zhong-Qiu
Department of Pharmaceutics, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, Guangdong, China.
Molecules. 2014 Oct 17;19(10):16757-69. doi: 10.3390/molecules191016757.
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.
乌头汤因其对类风湿性关节炎的治疗作用而在中国被广泛使用。苯甲酰新乌头碱（BMA）是乌头汤中含量最丰富的成分，被用作乌头汤药代动力学研究的标记化合物。本研究的目的是比较大鼠口服纯BMA和乌头汤后BMA的药代动力学。将纯BMA（5mg/kg）和乌头汤（0.54g/kg，相当于5mg/kg BMA）口服给予大鼠，并在10小时内采集血样。使用灵敏且经过验证的超高效液相色谱-串联质谱法（UPLC-MS/MS）对大鼠血浆中的BMA进行定量。具体而言，纯BMA的半衰期（T1/2）和平均驻留时间值分别为228.3±117.0分钟和155.0±33.2分钟，而乌头汤中BMA的半衰期和平均驻留时间值分别降至61.8±35.1分钟和55.8±16.4分钟。与纯BMA相比，口服乌头汤后BMA的曲线下面积（AUC）显著降低（五倍）。结果表明，与纯BMA相比，大鼠口服乌头汤后BMA的消除明显更快。
