大鼠血浆中藏红花素的HPLC法测定及其药代动力学研究(英文)

DETERMINATION OF CROCIN IN RAT PLASMA AND PHARMACOKINETICS STUDY BY HPLC

目的 建立大鼠血浆中藏红花素的RP-HPLC测定法,研究藏红花素的药代动力学特征. 方法 血样经乙腈预处理后,进行HPLC分析,色谱柱为Lichrospher C18 （5 m,250 mm×4.6 mm）,流动相为乙腈-甲醇-0.5%乙酸溶液 （15：20：50, v/v）.10只健康大鼠肌肉注射藏红花素水溶液,计算主要药动学参数. 结果 在1.08～ 10.80 μg/ml范围内藏红花素浓度与峰面积线性关系良好（r = 0.9996）, 定量限为1.08 μg/ml,日内精密度为1.86%～12.98%、日间精密度均小于为2.08%～9.75%,回收率为85.4%～91.7%.龙胆苦苷在家兔的主要药代动力学参数tmax 、Cmax 、t1/2 和AUC分别为87.0 min、3.74 μg/ml、140.4 min和768 μg·min/ml. 结论 所建分析方法灵敏、准确、简便,适合于藏红花素的药代动力学研究.

Objective A highly sensitive method for quantitation of crocin in rat plasma was established by using high performance liquid chromatography.Methods After taken from 10 rats, plasma were treated by aceonitrile and separated by HPLC on a C18 reversed-phase column using mobile phase of acetonitrile-methanol-0.5% aqueous acetic acid （15：20：50, v/v）. Results Calibration curves, which were linear over the range 1.08 to 10.80 μg/ml, were analyzed contemporaneously with each batch of samples, along with low （1.08 μg/ml）, medium （4.32 μg/ml） and high （10.08 μg/ml） quality control samples. The intra and inter-assay variability ranged from 1.86% to 12.96% for the low, medium and high quality control samples. The absolute recovery of crocin from plasma was in the range of 85.4%-91.7%. Pharmacokinetics parameters of crocin were as follow： tmax and Cmax were 87.0 min and 3.74 μg/ml respectively, t1/2 was 140.4 min, and AUC was 768 μg·min/ml. Conclusion The method was sensitive,accurate and simple for the determination of crocin in rat plasma,it has been used successfully to study crocin pharmacokinetics in adult rats.