Bachmann K, Sarver J G
Center for Applied Pharmacology, University of Toledo, OH 43606, USA.
Pharmacology. 1996 Mar;52(3):169-77. doi: 10.1159/000139381.
The objective of this investigation was to determine whether the oral clearance (CL) of chlorzoxazone could be estimated accurately from a single plasma chlorzoxazone measurement. In 6 healthy male subjects the mean clearance estimate (CLest) from a single 6-hour postdose measurement of plasma chlorzoxazone was within 6% of the actual mean CL calculated conventionally from the area under the plasma concentration versus time curve (AUC). After a second dose of chlorzoxazone administered 1 week later, the 6-hour mean CLest was within approximately 10% of the value from the previous week and within 15% of the value of CL from the previous week. No significant differences occurred between these three clearances, suggesting that for purposes of phenotyping CYP2E1 activity in humans with chlorzoxazone, a single-dose, single-sample procedure may suffice.
本研究的目的是确定是否可以通过单次血浆氯唑沙宗测量准确估计氯唑沙宗的口服清除率（CL）。在6名健康男性受试者中，单次给药后6小时血浆氯唑沙宗测量的平均清除率估计值（CLest）在根据血浆浓度-时间曲线下面积（AUC）常规计算的实际平均CL的6%以内。1周后给予第二剂氯唑沙宗，6小时平均CLest在前一周数值的约10%以内，且在前一周CL数值的15%以内。这三个清除率之间无显著差异，表明对于用氯唑沙宗对人类CYP2E1活性进行表型分析而言，单剂量、单样本程序可能就足够了。
