Webb D, Buss D C, Fifield R, Bateman D N, Routledge P A
Br J Clin Pharmacol. 1986 Mar;21(3):334-6. doi: 10.1111/j.1365-2125.1986.tb05201.x.
The plasma protein binding of metoclopramide was measured after addition of the drug (60 ng ml-1) to plasma from 18 patients with renal disease and 18 age and sex matched healthy individuals. The mean free fraction in renal disease (0.59 range 0.41-0.71) was not significantly different from controls (mean 0.6 range 0.56-0.69). In both groups the binding ratio of metoclopramide was significantly related to plasma alpha 1-acid glycoprotein (AAG) concentration but not to albumin or plasma non-esterified fatty acids concentration. Metoclopramide bound to human serum albumin (HSA) to a limited extent and to human AAG to a greater extent indicating that AAG is the major binding protein for the drug in plasma.
在向18例肾病患者及18例年龄和性别相匹配的健康个体的血浆中加入药物(60 ng/ml)后,测定了胃复安的血浆蛋白结合率。肾病患者的平均游离分数为0.59(范围0.41 - 0.71),与对照组(平均0.6,范围0.56 - 0.69)无显著差异。在两组中,胃复安的结合率均与血浆α1-酸性糖蛋白(AAG)浓度显著相关,而与白蛋白或血浆非酯化脂肪酸浓度无关。胃复安与人类血清白蛋白(HSA)的结合程度有限,与人类AAG的结合程度更高,这表明AAG是该药物在血浆中的主要结合蛋白。