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目的:研究荆芥内酯与大鼠血浆蛋白的结合情况。方法:采用平衡透析法测定体外荆芥内酯对大鼠血浆蛋白的结合率,以HPLC法测定透析袋两侧溶液中荆芥内酯的质量浓度,计算其血浆蛋白结合率。结果:荆芥内酯与内标完全分离,血浆中其他成分无干扰,在0.05～50.3μg.mL-1浓度范围内线性关系良好。日内、日间精密度及提取回收率均符合方法学要求。低、中、高(0.08,0.63,6.30μg.mL-1)质量浓度下,荆芥内酯在大鼠血浆中的蛋白结合率分别为(62.23±1.25)%,(62.71±0.04)%和(63.99±0.79)%。结论:该方法操作简便、快速、准确,灵敏度高,能满足生物样品的分析要求。荆芥内酯具有中等强度的蛋白结合率,蛋白结合率与透析液的药物浓度无关。
Objective: To study the combination of nepetalactone and rat plasma protein. Methods: The binding rate of nepetalactone to plasma protein in rats was determined by equilibrium dialysis. The concentration of nepetalactone in solution on both sides of the dialysis bag was determined by HPLC, and the plasma protein binding rate was calculated. Results: Nepetalactone was completely separated from the internal standard, and no interference was observed in other components of plasma. The linear relationship was found between 0.05 and 50.3μg.mL-1. The intra-day and inter-day precision and extraction recovery rate all met the methodological requirements. The protein binding rates of nepetalactone in rat plasma were (62.23 ± 1.25)%, (62.71 ± 0.04)% and (63.99 ± 0.79)%. Conclusion: The method is simple, rapid, accurate and sensitive. It can meet the analytical requirements of biological samples. Nepetalactone has a moderate protein binding rate, the protein binding rate has nothing to do with the dialysate drug concentration.