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目的建立测定2-甲氧基雌二醇大鼠血浆蛋白结合率的方法。方法采用平衡透析法对2-甲氧基雌二醇大鼠血浆蛋白结合率进行HPLC测定。结果高、中、低3个浓度(2、4、8 mg.L-1)的2-甲氧基雌二醇血浆蛋白结合率分别为(85.2±3.4)%、(82.1±5.3)%、(83.0±5.2)%。结论该方法灵敏度高,重现性好,操作简单,能满足生物样品分析要求。2-甲氧基雌二醇大鼠血浆蛋白结合率不具有浓度依赖性,使其临床用药具备较好的安全性。
Objective To establish a method for determination of plasma protein binding in 2-methoxyestradiol rats. Methods The dialysis method was used to determine the plasma protein binding rate of 2-methoxyestradiol in rats. Results The plasma protein binding rates of 2-methoxyestradiol were (85.2 ± 3.4)% and (82.1 ± 5.3)% in high, middle and low concentrations of 2,4,8 mg.L-1, (83.0 ± 5.2)%. Conclusion The method has high sensitivity, good reproducibility, simple operation and can meet the requirements of biological sample analysis. The plasma protein binding rate of 2-methoxyestradiol rat is not concentration-dependent, which makes its clinical medication have better safety.