目的:建立检测原芹菜素(protoapigenone)在人与鼠血浆药物浓度的高效液相色谱法(HPLC),测定原芹菜素在人与鼠血浆的蛋白结合率。方法:采用平衡透析法,结合HPLC测定原芹菜素在人与鼠血浆的蛋白结合率。结果:原芹菜素人血药透析袋内外平衡时间约为10h,在低、中、高(200,500,1000ug·L^-1)质量浓度下,其血浆蛋白结合率为(90.5±1.2)%,(89.6±1.7)%,(91.4±1.4)%;鼠血药透析袋内外平衡时间约为6h,在低、中、高(200,500,1000ug·L^-1)质量浓度下,鼠血浆蛋白结合率为(80.7±2.2)%,(81.1±1.8)%,(81.9±1.3)%。结论:原芹菜素在人、鼠血浆蛋白结合率之间差异有显著性(P〈0.01),但同一样品低、中、高浓度间,蛋白结合率差异无显著性(P〉0.05)。原芹菜素与人、鼠血浆蛋白具有较强的结合。
OBJECTIVE To develop a HPLC method for the determination of protoapigenone in human/rat plasma and study the plasma protein binding rate of protoapigenone. METHODS The equilibrium dialysis combined with HPLC was carried out for the determination of the plasma concentration and plasma protein binding rate of protoapigenone. RESULTS Human plasma protein binding rates of protoapigenone at low, middle and high concentrations (200,500,1 000ug·L^-1 ) were (90.5 ± 1.2)%, (89. 6 ± 1. 7) % and (91.4 ± 1.4) %, respectively. Accordingly, rat plasma protein binding rates of protoapigenone at low, middle and high concentrations were (80. 7 ± 2. 2) %, (81.1 ±1.8) % and (81.9 ± 1.3) %, respectively. CONCLUSION The high binding power of protoapigenone to human/rat plasma protein was confirmed by the proposed method of equilibrium dialysis combined with HPLC. Human or rat plasma protein binding rates of protoapigenone at low, medium and high concentrations showed no significant difference (P〈0.05). However, the plasma protein binding rates of protoapigenone towards the human plasma and rat plasma were significantly different (P〈0. 01 ).