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目的考察雷公藤内酯醇在不同种属的血浆蛋白结合率。方法超滤法分离结合型药物和游离型药物,LC-MS/MS法测定药物的浓度。结果雷公藤内酯醇在不同浓度下与大鼠血浆的蛋白结合率分别是(25.4±1.8)、(12.7±8.5)和(11.5.±3.2)ng/ml,与比格犬血浆的蛋白结合率分别是(16.1±2.2)、(28.6±0.3)和(25.0±1.2)ng/ml;与人血浆的蛋白结合率分别是(21.5±2.1)、(18.9±5.7)和(21.3±2.6)ng/ml。结论雷公藤内酯醇在实验浓度范围内与大鼠、比格犬和人血浆中蛋白结合率均较低,相同浓度雷公藤内酯醇与不同种属血浆蛋白结合率,以犬血浆最高[(28.6±0.3)ng/ml],与大鼠[(25.4±1.8)ng/ml]、人血浆[(18.9±5.7)ng/ml]相比均具有统计学差异(P<0.05),大鼠与人血浆之间无统计学差异。各种属血浆蛋白结合率与药物浓度无明显依赖关系。
Objective To investigate the plasma protein binding rate of triptolide in different species. Methods The combined drug and free drug were separated by ultrafiltration and the drug concentration was determined by LC-MS / MS. Results The binding rates of triptolide to rat plasma at different concentrations were (25.4 ± 1.8), (12.7 ± 8.5) and (11.5 ± 3.2) ng / ml, respectively. The protein binding rates (16.1 ± 2.2), (28.6 ± 0.3) and (25.0 ± 1.2) ng / ml, respectively. The protein binding rates to human plasma were (21.5 ± 2.1), (18.9 ± 5.7) and (21.3 ± 2.6) ng / ml. Conclusion Triptolide has a low binding rate to plasma in rat, beagle dog and human plasma in the range of experimental concentration. The plasma protein binding rate of triptolide to different species in the same concentration is the highest in canine plasma [(28.6 ± 0.3) ng / ml], compared with that in rats [(25.4 ± 1.8) ng / ml] and human plasma [(18.9 ± 5.7) ng / ml] There was no statistical difference between human plasma. All kinds of plasma protein binding rate and drug concentration no significant dependence.