RP-HPLC法测定大鼠血浆中蓝萼甲素含量与药代动力学及排泄研究

Research RP-HPLC determination of glaucocalyxin A in rat plasma and its pharmacokinetic and excretion

目的:研究蓝萼甲素在大鼠体内的药代动力学过程及排泄过程并建立大鼠生物样品测定的高效液相色谱方法。方法:采用液液萃取的方法从生物样品中提取出蓝萼甲素后用 Hypersil BDS C_(18)(250 mm×4.6 mm,5 μm)柱进行分离,流动相为甲醇-水(45:55)。结果:蓝萼甲素在大鼠体内静脉给药后药代动力学符合二房室模型。t_(1/2α)和 t_(1/2β)分别为4.32 min 和28.56min,12 h 蓝萼甲素在尿、粪便中的排泄量分别为12.8%和23.8%,在10 h 内胆汁中的排泄量为35.68%。结论:此方法快捷、灵敏、简便,适合于蓝萼甲素的药代动力学研究。

Objective： To study the phannacokinetic and excretion of glaucocalyxin A in rat and establish the HPLC method in rat plasma, bile, urine and feces. Method：A validated HPLC method was described for the determination of glaucocalyxin A in rat plasma ,bile, urine and feces using a liquid -liquid extraction and UV absorbance detection. Results：The extraction recovery of glaucocalyxin A ranged from 79. 11% to 82. 22%. The linear range was 0. 2 -10 μg · mL^-1 ,correlation coefficient r =0. 9996. Glaucocalyxin A pharmacokinetic application with iv in rats revealed that glaucocalyxin A followed two -compartment open model, t1/2α and t1/2αwere 4. 32 min and 28.56 min, respectively. The excretion of the parent drug amounted to 23.8% of the dosage within 12 h in feces and the excretion in urine to 12. 8% within 12 h. The bile excretion of glaucocalyxin A amounted to 35.68% of the dosage within 10 h. Conclusion： The method developed is successfully applied to a simple, rapid, specific and accurate HPLC method for investigation of the pharmacokinetics of glaucocalyxin A in rat.