Liu Yi-ming, Lin Ai-hua, Chen Hui, Zeng Fan-dian
Institute of Clinical Pharmacology, Tongji Medical College, China.
Yao Xue Xue Bao. 2003 Oct;38(10):775-8.
To establish a solid phase extraction-high performance liquid chromatographic (SPE-HPLC) method for determining plasma scutellarin concentration, and study its pharmacokinetics after i.v. breviscapine in rabbits.
Methanol-water-phosphoric acid (50:50:0.5) mixture was used as mobile phase, Nucleosil C18 column (250 mm x 4.6 mm ID) was selected. The wavelength of UV detection was 335 nm. Fifteen rabbits, randomized into 3 groups, were given breviscapine i.v. at the dose of 10, 20 and 40 mg.kg-1. Scutellarin in plasma was determined by SPE-HPLC method.
Linearity was obtained over the range of 0.02-10.0 mg.L-1 of scutellarin. The method recovery was 96.15%-99.31%; the within-day and between-day RSDs were all below 10%. After i.v. 10, 20 and 40 mg.kg-1 of breviscapine to rabbits, the concentration-time curve of scutellarin fitted to a three compartment model. The main pharmacokinetic parameters showed no significant difference between low and medium doses, but the difference was significant between high dose and other doses.
This assay method was accurate, sensitive, simple and suitable for the measurement of plasma scutellarin concentration. The pharmacokinetic characteristics were found to fit a three-compartment model following i.v. injection of breviscapine to rabbits. The changes of drug concentration in vivo exhibited linear kinetics ove the dosage range of 10-20 mg.kg-1, but when the dosage was 40 mg.kg-1, the linear kinetic properties disappeared.
建立一种用于测定血浆中灯盏花素浓度的固相萃取-高效液相色谱（SPE-HPLC）法，并研究灯盏花素静脉注射后在兔体内的药代动力学。
以甲醇-水-磷酸（50:50:0.5）混合液为流动相，选用Nucleosil C18柱（250 mm×4.6 mm内径）。紫外检测波长为335 nm。将15只兔随机分为3组，分别静脉注射灯盏花素，剂量为10、20和40 mg·kg-1。采用SPE-HPLC法测定血浆中的灯盏花素。
灯盏花素在0.02 - 10.0 mg·L-1范围内呈线性关系。方法回收率为96.15% - 99.31%；日内和日间相对标准偏差均低于10%。给兔静脉注射10、20和40 mg·kg-1灯盏花素后，灯盏花素的浓度-时间曲线符合三室模型。主要药代动力学参数在低剂量和中剂量之间无显著差异，但高剂量与其他剂量之间差异显著。
该测定方法准确、灵敏、简便，适用于血浆中灯盏花素浓度的测定。静脉注射灯盏花素后，兔体内药代动力学特征符合三室模型。在10 - 20 mg·kg-1剂量范围内，体内药物浓度变化呈现线性动力学，但当剂量为40 mg·kg-1时，线性动力学特性消失。
