氯化两面针碱人血浆蛋白结合率的测定

目的建立测定人血浆中氯化两面针碱的高效液相色谱法,并研究氯化两面针碱与人血浆蛋白的结合情况。方法离子对试剂萃取技术对样品进行预处理,乙腈-0.15%磷酸(36:64,V:V,用三乙胺调pH值至3.5)为流动相,C_(18)柱(250mm×4.6mm,5μm)为固定相,紫外检测波长271nm,以氯霉素为内标,采用平衡透析法对氯化两面针碱的人血浆蛋白结合率进行测定。结果氯化两面针碱与内标完全分离,样品中其他成份无干扰,在0.03188～2.040mg·L~(-1)范围内线性关系良好,低、中、高3种不同质量浓度的方法回收率>95%,日内、日间精密度均符合方法学要求。低、中、高3种药物浓度的血浆蛋白结合率分别为68.9%、67.4%、67.9%。结论方法简便、快速,结果准确、可靠,能满足生物样品分析要求。氯化两面针碱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。

Determination of human plasma protein binding rate of nitidine chloride

AIM To develope HPLC for determining the concentration of nitidine chloride in human plasma and to study the plasma protein binding rate of nitidine chloride.METHODS Nitidine chloride was extracted from plasma with ion pair reagent.A mixture of acetonitrile-phosphoric acid(36:64,V:V,pH was adjusted to 3.5 by triethylamine)was used as mobile phase,C_(18) column(250mm×4.6mm,5μm)was selected as the fixed phase.The wavelength of UV detection was 271 nm.Chloramphenicol was taken as an internal standard.Human plasma protein binding rate of nitidine chloride was carried out by equilibrium dialysis. RESULTS Nitidine chloride and the internal standard were separated completely with no interference to other ingredients.The calibration curves of nitidine chloride was in good linear correlation the range of 0.03188- 2.040mg·L~(-1).The low,middle and high three different substantial concentrations with recollection rate>95% was demonstrated,and within intra-day and inter-day precisions of low-,mid-,high-concentrations of nitidine chloride in plasma met the requirements of methodology.The plasma protein binding rates of nitidine chloride in low,middle and high concentrations were 68.9%,67.4%,67.9% respectively in human plasma. CONCLUSION The method is simple,fast with sensitive,accurate and reproducible outcomes;satisfing the need for bio-sampling analysis.Nitidine chloride possesses medium capacities of protein binding rate in human plasma,with no significant relation to drug concentrations in dialysis liquid of among low,middle and high concentrations.