Kodama Y, Tsutsumi K, Kuranari M, Kodama H, Fujii I, Takeyama M
Department of Clinical Pharmacy, Oita Medical University, Japan.
Eur J Clin Pharmacol. 1993;44(3):291-3. doi: 10.1007/BF00271375.
The in vivo serum protein binding characteristics of carbamazepine (CBZ) and carbamazepine-10,11-epoxide (CBZ-E) were assessed in sera from 23 paediatric patients on CBZ monotherapy. We assumed that CBZ and CBZ-E binding to serum proteins comprised specific binding sites on alpha 1-acid glycoprotein (AAG) and non-specific binding sites on serum albumin. Therefore, the binding characteristics of each compound were analysed according to specific and nonspecific binding equations. Association constants for drug-AAG binding were 0.096 l.mumol-1 for CBZ and 0.023 l.mumol-1 for CBZ-E. Within the concentration ranges investigated the specific binding of each compound contributes to the drug-serum protein interactions. Age did not show a significant correlation with the serum unbound fraction of each compound.
在23例接受卡马西平（CBZ）单药治疗的儿科患者的血清中评估了卡马西平（CBZ）和卡马西平-10,11-环氧化物（CBZ-E）的体内血清蛋白结合特性。我们假设CBZ和CBZ-E与血清蛋白的结合包括α1-酸性糖蛋白（AAG）上的特异性结合位点和血清白蛋白上的非特异性结合位点。因此，根据特异性和非特异性结合方程分析了每种化合物的结合特性。药物-AAG结合的缔合常数对于CBZ为0.096 l·μmol-1，对于CBZ-E为0.023 l·μmol-1。在所研究的浓度范围内，每种化合物的特异性结合都有助于药物-血清蛋白相互作用。年龄与每种化合物的血清未结合分数没有显著相关性。
