伏立康唑人体药代动力学的特征与差异研究

目的:研究健康受试者口服伏立康唑的药代动力学特征和差异.方法:70名健康志愿者单次口服伏立康唑200 mg后,用HPLC-MS/MS方法测定血中的伏立康唑浓度,分析不同个体伏立康唑的体内代谢过程与动力学差异.结果:伏立康唑药代动力学个体差异很大.其代谢特征可分为四种类型,A型占21%,达峰时间最短,而峰浓度最高,分布容积最小,属于快分布型;B型占53%,所有参数均为中间水平;C型占11%,为慢代谢型;D型占14%,峰浓度最低,达峰时间最晚,AUC最低,清除最快,为强代谢型.结论:伏立康唑个体代谢差异很大,需要进行血药浓度监测.

Pharmacokinetics and variance study of voriconazole in human

Objective: To investigate the pharmacokinetics and its variance of voriconazole in Chinese healthy volunteers.Methods: Serial blood samples were taken after single oral dose of 200 mg voriconazole in 70 healthy Chinese subjects.The whole blood concentrations of voriconazole were measured by HPLC-MS/MS.The metabolic process and pharmacokinetics variance of voriconazole in individuals were analyzed.Results: Significant variance was observed on the pharmacokinetics of voriconazole.The metabolic characteristics can be divided into 4 types based on the concentration-time curves of voriconazole.Mode A(21%) displayed the features of fast distribution which had the shortest peak time,highest peak concentration and the smallest Vd.Mode B(53%) showed the characteristics of intermediate metabolism with all parameters in intermediate levels.And mode C(11%) had a poor ability of metabolism.Mode D(14%) had the extensive metabolism ability with the lowest peak concentration,longest peak time and the smallest AUC.Conclusion: The individual differences of voriconazole in metabolism were significant.It is important to monitor the blood concentration of voriconazole in order to assure the clinical efficacy and rational medication.