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Validation of an HPLC method for the determination of scutellarin in rat plasma and its pharmacokinetics.

机译:HPLC方法在大鼠血浆中黄cut素含量测定及其药代动力学方面的验证。

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摘要

A validated HPLC method was developed for the quantification of scutellarin in rat plasma using a liquid-liquid extraction and an ultraviolet detection. Chromatographic separation of scutellarin in plasma was performed on a C(18) column, with a mobile phase of acetonitrile-water (23:77, v/v), adjusted to pH 2.5 with 1M phosphoric acid, and rutin was used as an internal standard. The calibration curve was linear over the range 0.1-100mug/ml in rat plasma. The average extraction recoveries were 85.9+/-8.9, 71.0+/-4.6, 72.7+/-1.2% (n=3) at concentrations of 0.1, 2, 100mug/ml, respectively, and the within-day and between-day precisions were less than 15%. After intravenous administration to rats over the doses range of 10-40mg/kg, the plasma concentration-time curve of scutellarin was best conformed to three-compartment open model. The AUC of scutellarin was proportional to dose, and the systemic clearance (Cl), elimination half-life (t(1/2)beta) and apparent volume of distribution (V(c)) were not significantly different among the three doses, suggestive of the linear pharmacokinetics characteristic of scutellarin after intravenous administration.
机译:开发了一种经过验证的HPLC方法,使用液-液萃取和紫外检测技术对大鼠血浆中的黄cut苷进行定量。在C(18)色谱柱上进行血浆中黄cut素的色谱分离,流动相为乙腈-水(23:77,v / v),用1M磷酸调节至pH 2.5,并将芦丁用作内部溶剂标准。在大鼠血浆中,校准曲线在0.1-100ug / ml范围内呈线性。在浓度为0.1、2、100 ug / ml的情况下以及当日和当日之间,平均提取回收率分别为85.9 +/- 8.9、71.0 +/- 4.6、72.7 +/- 1.2%(n = 3)。精度低于15%。给大鼠静脉内给药10-40mg / kg剂量后,黄cut素的血药浓度-时间曲线最符合三室开放模型。黄cut苷的AUC与剂量成正比,三种剂量之间的全身清除率(Cl),消除半衰期(t(1/2)beta)和表观分布体积(V(c))并无显着差异,提示黄intravenous素静脉内给药后的线性药代动力学特征。

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