筋骨草提取物有效成分在beagle犬体内药代动力学研究

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乙酰哈巴苷和哈巴苷是筋骨草提取物中含量最高的2种有效成分。该文建立了LC-MS/MS法,对beagle犬口服筋骨草提取物后乙酰哈巴苷和哈巴苷的药代动力学进行研究。健康雌性Beagle犬口服不同剂量的筋骨草提取物,对不同时间点的乙酰哈巴苷和哈巴苷血药浓度进行测定,采用winnonlin 6.3软件以非房室模型进行拟合。色谱条件:安捷伦ZORB-AX XDB-C18柱(2.1 mm×50 mm,3.5μm);柱温30℃;流动相(A为0.1%甲酸水溶液;B为乙腈)为0~2 min 5%B;2.1~5min 95%B;5.1~10 min 5%B。流速0.3 mL.min-1。质谱条件:电喷雾离子源;正离子模式;选择离子分别为乙酰哈巴苷(m/z 429.2→369.2)、哈巴苷(m/z 387.2→207.2)和肉桂酸(m/z 149.2→103.1)。干燥气流速10 L.min-1;干燥气温度300℃;毛细管电压4 000 V。结果表明Beagle犬口服筋骨草提取物后乙酰哈巴苷和哈巴苷存在剂量依赖性,乙酰哈巴苷和哈巴苷的达峰时间分别为1.7,1.57 h左右,远大于大鼠口服筋骨草提取物后的乙酰哈巴苷和哈巴苷的达峰时间,这可能是由于种属差异造成的。 Acetyl hexabarine and hababine are the two active ingredients in the extract of Fortunella. In this paper, a LC-MS / MS method was developed to study the pharmacokinetics of acetyl-habactidine and habazin in beagle dogs after oral administration of extract of Fortunella. Healthy female Beagle dogs were orally administered with different doses of Radix extract, and the concentrations of acetyl-habacin and hababin at different time points were determined. The non-compartmental model was used to fit the data with winnonlin 6.3 software. Chromatographic conditions: Agilent ZORB-AX XDB-C18 column (2.1 mm × 50 mm, 3.5 μm); column temperature 30 ° C .; mobile phase (A 0.1% formic acid in water; 2.1 ~ 5 min 95% B; 5.1 ~ 10 min 5% B. Flow rate 0.3 mL.min-1. Mass spectrometry conditions: electrospray ion source; positive ion mode; selected ions were acetyl-habacin (m / z 429.2 → 369.2), hababine (m / z 387.2 → 207.2) and cinnamic acid (m / z 149.2 → 103.1). Drying gas flow rate 10 L.min-1; drying temperature 300 ℃; capillary voltage 4000V. The results showed that the Beagle dog oral administration of Fortu extract after acetyl acetyl and hababin dose-dependent, acetyl-hababin and hababin peak time were 1.7,1.57 h or so, much larger than the rat oral Bumacao extract Acetyl hababine and hababin peak time, which may be due to species differences caused.
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