Xu H Y, Zhong D F, Zhao L M, Zhang Y F, Zhang B J
Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University, Shenyang 110015, China.
Yao Xue Xue Bao. 2001 Jan;36(1):71-3.
To assess the pharmacokinetic profile of single doses of meloxicam in healthy Chinese volunteers.
The plasma concentrations of meloxicam after an oral dose of 15 mg to twenty healthy male volunteers were analyzed by means of a validated HPLC method. The pharmacokinetic parameters were subjected to Shapiro-Wilk test to determine whether these data were fitted to a normal distribution.
The twenty volunteers can be classified into extensive metabolizers and poor metabolizers according to pharmacokinetic parameters. The main parameters in the two groups obtained were as follows: T 1/2 were 21 +/- 4 and 38 +/- 9 h, AUC0-infinity were 49 +/- 10 and 110 +/- 8 micrograms.h.mL-1, respectively. Even the AUC data in extensive metabolizers were 1.7 times as that reported in White volunteers following the same doses of meloxicam.
There were significant individual differences in the pharmacokinetics of meloxicam in Chinese volunteers, which may be due to the genetic polymorphism of CYP2C9.
评估单剂量美洛昔康在健康中国志愿者体内的药代动力学特征。
采用经过验证的高效液相色谱法分析20名健康男性志愿者口服15毫克美洛昔康后的血浆浓度。药代动力学参数进行Shapiro-Wilk检验,以确定这些数据是否符合正态分布。
根据药代动力学参数,20名志愿者可分为快代谢型和慢代谢型。两组获得的主要参数如下:半衰期分别为21±4小时和38±9小时,药时曲线下面积(AUC0-∞)分别为49±10和110±8微克·小时·毫升-1。即使是快代谢型志愿者的AUC数据也是相同剂量美洛昔康后白种志愿者报道数据的1.7倍。
中国志愿者中美洛昔康的药代动力学存在显著个体差异,这可能归因于CYP2C9的基因多态性。