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目的建立HPLC法测定中药复方天麻头风灵胶囊灌胃后大鼠血浆中天麻素(gastrodin,Gas)的浓度,并研究Gas在大鼠体内的药物动力学。方法Wistar雄性大鼠6只,灌胃给药后不同时间点眼眶采血,血浆样品用体积分数6%高氯酸溶液沉淀蛋白,取上清液进样分析,以间苯三酚为内标物,色谱柱为Diamonsil C18柱(200mm×4.6mm,5μm),流动相为乙腈-水(体积比28∶972),流速为1.0mL·min-1,柱温为35℃,检测波长为221nm。结果Gas质量浓度在25~10 000μg·L-1内与峰面积呈良好线性关系(r=0.998 1),日间和日内精密度RSD均小于6.5%,提取回收率大于69.4%。主要药物动力学参数为:ρmax=(1 100±283)μg·L-1,tmax=(0.5±0.2)h,t1/2=(0.39±0.07)h,AUC0→t=(1 365±341)μg·h·L-1,AUC0→∞=(1 377±346)μg·h·L-1。结论在考察浓度范围内,Gas在大鼠体内符合线性动力学过程。
OBJECTIVE To establish a HPLC method for the determination of gastrodin (Gas) in rat plasma and to study the pharmacokinetics of Gas in rats. Methods Six male Wistar rats were injected with orbital blood at different time points after intragastric administration. The plasma samples were precipitated with 6% perchloric acid solution in volume fraction, and the supernatant was injected for analysis. Phragnol was used as internal standard . The column was Diamonsil C18 (200mm × 4.6mm, 5μm). The mobile phase consisted of acetonitrile-water (volume ratio 28:972), the flow rate was 1.0mL · min-1, the column temperature was 35 ℃ and the detection wavelength was 221nm. Results Gas mass concentration showed a good linear relationship with the peak area (r = 0.998 1) in 25 ~ 10 000 μg · L-1. The RSDs were less than 6.5% and the extraction recovery was more than 69.4%. The main pharmacokinetic parameters were ρmax = (100 ± 283) μg · L-1, tmax = (0.5 ± 0.2) h, t1 / 2 = (0.39 ± 0.07) h, AUC0 → t = ) μg · h · L-1, AUC0 → ∞ = (1 377 ± 346) μg · h · L-1. Conclusions Gas meets the linear kinetic process in rats at the concentration range studied.