Haughey D B, Lima J J
Biopharm Drug Dispos. 1983 Apr-Jun;4(2):103-12. doi: 10.1002/bdd.2510040202.
Concentrations of disopyramide (D) and mono-N-dealkyldisopyramide (MND) were measured in serum and urine following administration of 100, 150, 200, and 300 mg D to four volunteers. The free fraction of D in serum was drug concentration-dependent in all four subjects following the administration of the four doses. Areas under the free (unbound) D serum concentration-time curves (AUC free 0-9) were linearly related to dose following 100-200 mg D. AUC free 0-9 values were 30-60 per cent higher than expected in two subjects following 300 mg D due to an apparent dose-dependent decrease in D renal tubular secretion. Renal clearance of free D averaged 10.9 1 h-1. The renal clearance of MND averaged 10.3 1 h-1. The urinary excretion of MND was proportional to disopyramide dose.
给四名志愿者分别服用100、150、200和300毫克丙吡胺（D）后，测定其血清和尿液中丙吡胺（D）和单-N-去烷基丙吡胺（MND）的浓度。在给予四剂药物后，所有四名受试者血清中D的游离分数均呈药物浓度依赖性。在给予100-200毫克D后，游离（未结合）D血清浓度-时间曲线下面积（AUC游离0-9）与剂量呈线性相关。由于D肾小管分泌明显的剂量依赖性降低，在两名受试者给予300毫克D后，AUC游离0-9值比预期高30%-60%。游离D的肾清除率平均为10.9升/小时。MND的肾清除率平均为10.3升/小时。MND的尿排泄量与丙吡胺剂量成正比。
