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目的:测定硫酸长春新碱靶向缓释制剂的血浆蛋白结合率,为该缓释制剂的药效学和临床研究提供相关参数。方法:采用平衡透析法测定硫酸长春新碱缓释制剂在Wistar大鼠血浆中的蛋白结合率,利用液-液萃取法提取药物,高效液相色谱法测定药物浓度。结果:硫酸长春新碱靶向缓释制剂在120h时达到最好平衡点,质量浓度为2.50,5.00,10.00,20.00,40.00和80.00mg.L-1的缓释制剂,血浆蛋白结合率分别为35.91%,40.01%,35.79%,32.55%,39.24%和41.34%。结论:硫酸长春新碱靶向缓释制剂中的高分子材料降解缓慢,故内部包裹药物可长期释放,同时,由于该制剂吸附和包裹药物的释放速率不同,导致血浆蛋白结合率在初期具有较大的波动性,但随着时间的延长,血浆蛋白结合率仍可达到稳定水平。
OBJECTIVE: To determine the plasma protein binding rate of vinblastine sulfate-targeted sustained-release preparations and provide relevant parameters for the pharmacodynamic and clinical studies of the sustained-release preparations. Methods: The protein binding rate of vinblastine sulfate sustained-release preparation in Wistar rats plasma was determined by equilibrium dialysis method. The drug was extracted by liquid-liquid extraction and the drug concentration was determined by HPLC. Results: The vincristine sulfate sustained-release preparations achieved the best balance point at 120h, the sustained-release preparations with mass concentrations of 2.50, 5.00, 10.00, 20.00, 40.00 and 80.00 mg.L-1, the plasma protein binding rates were 35.91%, 40.01%, 35.79%, 32.55%, 39.24% and 41.34%. CONCLUSIONS: The degradation of vinorelbine sulfate sustained-release preparations slowed the degradation of the polymeric materials. Therefore, the long-term release of the drug in the inner package and the different rate of release of the drug in the package resulted in a higher plasma protein binding rate Large volatility, but with the extension of time, the plasma protein binding rate can still reach a steady level.