Differences between blacks and whites in plasma protein binding of drugs
Differences between blacks and whites in plasma protein binding of drugs
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DOI：
10.1007/s002280050235
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发表时间：
1997-02-01
影响因子：
2.9
通讯作者：
Livingston, TN
中科院分区：
文献类型：
--
作者：
Johnson, JA;Livingston, TN
目的：以异丙吡胺和水杨酸为模型化合物，研究α(1)-酸性糖蛋白(AGP)和白蛋白与药物结合的种族差异。健康志愿者29例(白人15例，黑人14例)。用C-14-二丙吡胺和C-14-水杨酸平衡透析法测定血浆中的二丙吡胺和水杨酸游离部分(Fu)。结果：黑人血浆中的二丙吡胺游离部分(0.131 vs0.113)和水杨酸游离部分(0.053 vs0.048)显著高于白人。经AGP和白蛋白浓度校正后，不再存在种族差异。结论：许多与AGP和/或白蛋白结合的药物在非结合部位可能存在种族差异。然而，这些差异可能是由蛋白质浓度的差异而不是蛋白质上结合位点数量的差异或蛋白质对药物亲和力的种族差异来解释的。
Objective: Disopyramide and salicylic acid were used as model compounds to characterize racial differences in binding of drugs by alpha(1)-acid glycoprotein (AGP) and albumin, respectively. Drug-free plasma was collected from 29 healthy volunteers (15 white, 14 black). Disopyramide and salicylic acid unbound fractions (fu) in plasma were determined by equilibrium dialysis using C-14-disopyramide and C-14-salicylic acid.Results: Disopyramide unbound fractions were significantly higher in blacks than whites (0.131 vs 0.113) as were salicylic acid unbound fractions (0.053 vs 0.048). When unbound fractions were corrected for AGP and albumin concentration, racial differences were no longer present.Conclusion: Many drugs which bind to AGP and/or albumin may exhibit racial differences in unbound fractions. However, these differences are likely explained by differences in protein concentrations rather than differences in the number of binding sites on the protein or racial differences in affinity of the protein for drugs.