卡马西平健康人体药物动力学特性

Pharmacokinetics Profile of Carbamazepine Tablets in Healthy Volunteers

目的:建立测定卡马西平(CBZ)的高效液相色谱法。分析CBZ在健康受试者体内药动学特性,探讨临床应用个体差异的原因。方法:12名健康受试者单剂量(200 mg)口服CBZ片,HPLC法测定血浆样品药物浓度。结果:CBZ的线性范围为(0.05～10)μg·ml^(-1),最低检测浓度为0.05μg·ml^(-1),方法平均回收率为94.4%。单剂量口服CBZ后血浆浓度符合一级吸收一房室模型,其主要药动学参数为:C_(max)为(4.71±0.99)μg·ml^(-1),t_(max)为(16±12)h,AUC为(361.62±49.43)μg·h·ml^(-1),t_(1/2)= (38.39±6.37)h。结论:该法测定血浆中CBZ浓度高效、灵敏、准确,CBZ体内药动学特性存在明显个体差异。

Objective： To establish an HPLC method for the determination of carbamazepine concentration in human plasma and explore the reason of individual variation of this drug through analyzing its pharmacokinetics profile in Chinese healthy volunteers. Method： A single 200 mg dose of carbamazepine was performed in healthy male volunteers. Plasma drug concentration was determined by HPLC. Result： The linear range of CBZ was 0.05 - 10 μg·ml^-1, the quantitative limit was 0.05 μg·ml^-1 which was enough to detect the concentration of CBZ in plasma, the average recovery was 94.4%, the main pharmacokinetics parameters were （4.71 ± 0.99） μg·ml^-1 for C max, （ 16 ± 12） h for tmax, （361.62 ± 49.43） μg·h·ml^-1 for AUC, （38.39 ± 6.37 ） h for t1/2, respectively. Plasma-drug concentration curve of CBZ in single oral administration was conformed to be one compartment model of the first order absorption. Conclusion： The method was high sensitivity and selectivity for determination the plasma - drug concentration of CBZ in human. The pharmacokinetics profile proved to be significant individual difference of this drug.