Lin T S, Lai M L, Huang J D
Department of Neurology, National Cheng-Kung University Medical Center, Taiwan, R.O.C.
Zhonghua Yi Xue Za Zhi (Taipei). 1991 May;47(5):336-41.
To investigate the autoinduction of carbamazepine (CBZ) metabolism in Chinese, eleven healthy male volunteers joined in this study. There were two phases of drug administration with a wash-out interval of one month, 400 mg CBZ was taken orally in single-dose phase, and 200 mg three times per day were given for seven days in multiple-dose phase. Plasma samples were obtained in series of time after the last dose of drug in each phase. CBZ concentrations were determined by a high pressure liquid chromatography method. A non-linear regression program was applied in a personal computer to estimate the pharmacokinetic parameters. The average CBZ half-lives in single- and multiple-dose phases were 50.1 +/- 12.1 (mean +/- SD) hours and 26.1 +/- 4.2 hours and the clearances were 16.4 +/- 3.3 ml/kg/h and 45.3 +/- 23.4 ml/kg/h respectively, both with significant differences (p less than 0.005). There is evidence to support the presumption of autoinduction in Chinese.
为研究在中国人群中卡马西平(CBZ)代谢的自身诱导作用,11名健康男性志愿者参与了本研究。药物给药分为两个阶段,洗脱期为1个月,单剂量阶段口服400mg CBZ,多剂量阶段每日3次,每次200mg,共服用7天。在每个阶段最后一剂药物后的一系列时间点采集血浆样本。采用高压液相色谱法测定CBZ浓度。在个人计算机上应用非线性回归程序估算药代动力学参数。单剂量和多剂量阶段CBZ的平均半衰期分别为50.1±12.1(均值±标准差)小时和26.1±4.2小时,清除率分别为16.4±3.3ml/kg/h和45.3±23.4ml/kg/h,两者均有显著差异(p<0.005)。有证据支持在中国人群中存在自身诱导的推测。