刘同征, 钱之玉. 西红花酸在大鼠的药代动力学研究J. 药学学报, 2002, 37(5): 367-369.
引用本文: 刘同征, 钱之玉. 西红花酸在大鼠的药代动力学研究J. 药学学报, 2002, 37(5): 367-369.
LIU Tong-zheng, QIAN Zhi-yu. PHARMACOKINETICS OF CROCETIN IN RATSJ. Acta Pharmaceutica Sinica, 2002, 37(5): 367-369.
Citation: LIU Tong-zheng, QIAN Zhi-yu. PHARMACOKINETICS OF CROCETIN IN RATSJ. Acta Pharmaceutica Sinica, 2002, 37(5): 367-369.

西红花酸在大鼠的药代动力学研究

PHARMACOKINETICS OF CROCETIN IN RATS

  • 摘要: 目的建立高效液相色谱法测定大鼠血浆中西红花酸的浓度。方法用HPLC法,色谱柱为Hypersil C18柱(5 μm,4.6 mm×200 mm),流动相为甲醇-水-冰醋酸(75∶24.5∶0.5),流速1.0 mL·min-1,柱温30℃,检测波长423 nm。结果西红花酸浓度0.49~7.87 μg·mL-1与峰面积呈良好的线性关系(γ=0.9996),最低检测浓度为0.14 μg·mL-1(S/N=3)。样品的平均加样回收率为105.2%。日内、日间精密度的RSD均小于5%。不同时间、不同温度及冻融处理的稳定性考察,RSD分别为7.4%,4.9%和3.3%。结论本法稳定、简单、可靠,可用于西红花酸血药浓度分析及其药代动力学研究。

     

    Abstract: AIMTo develop an HPLC method for the determination of crocetin in rat plasma and study the pharmacokinetics in rats. METHODSHypersil C18 column (5 μm, 4.6 mm×200 mm) was used at column temperature 30℃. The mobile phase consisted of methanol-water-acetic acid (75∶24.5∶0.5) at the flow rate of 1.0 mL·min-1. The UV detection wave length was 423 nm. RESULTSThe calibration curve was linear (γ=0.9996) in the range from 0.49 μg·mL-1 to 7.87 μg·mL-1 for crocetin. The mean recovery was 105.2%. The lowest detectable concentration of crocetin was 0.14 μg·mL-1 (S/N=3). The RSDs of within-day and between-day were all less than 5%. The plasma crocetin was steady. The HPLC method of determination of crocetin in the plasma was established. After single dose of 50 mg·kg-1 ig in 10 rats, the main pharmacokinetic parameters were estimated as follows: T1/2α (30±6) min, Tmax (65±16) min, Cmax (5.0±1.0) μg·mL-1, AUC0-T (845±109) μg·min·mL-1, Vd (5.0±0.8) L·kg-1. Crocetin was shown to be absorbed into the blood through the gastrointestinal tract. CONCLUSIONThis method is quick, precise and reliable. Crocetin was shown to be quickly absorbed in rats.

     

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