利奈唑胺在中国健康人体内空腹和餐后的药代动力学研究

Pharmacokinetics of single administration of linezolid tablet in Chinese healthy volunteers under fasting and fed conditions

目的研究利奈唑胺片在中国健康受试者单次给药的空腹和餐后的药代动力学。方法 48名男性受试者分为空腹组和餐后组,均单次口服利奈唑胺片600 mg,采集不同时间的血样,用高效液相色谱-串联质谱法(LC-MS/MS)测定血浆中利奈唑胺的浓度,用DAS 3.2.7软件计算药代动力学参数。结果空腹单次口服利奈唑胺片的主要药代动力学参数:Cmax为(11.16±3.05)μg·m L-1,tmax为(2.00±1.17)h,t1/2为(5.90±2.01)h,AUC0-∞为(110.18±31.83)μg·h·m L-1;餐后单次口服利奈唑胺片的主要药代动力学参数:Cmax为(9.79±1.92)μg·m L-1,tmax为(2.66±1.27)h;t1/2为(5.57±2.67)h;AUC0-∞为(93.9±34.7)μg·h·m L-1。结论中国健康男性受试者单次口服利奈唑胺片600 mg,在24 h内餐后组的人体血药浓度比空腹组低;2组药代动力学参数与国外已报道基本一致。

Objective To investigate the pharmacokinetics of single administration of linezolid tablet in Chinese healthy volunteers. Methods Forty- eight male subjects were divided into two groups and respectively received single 600 mg dose of linezolid tablets under fasting and postprandial conditions. Plasma samples were collected at designed time and the concentrations of linezolid were determined by LC- MS / MS method.The pharmacokinetic parameters were calculated by DAS 3. 2. 7 software.Results The main pharmacokinetic parameters of single oral linezolid tablet of 600 mg under fasting condition were as follows： Cmax（ 11. 16 ±3. 05） μg · m L- 1,tmax（ 2. 00 ± 1. 17） h,t1 /2（ 5. 90 ± 2. 01） h,AUC0- ∞（ 110. 18 ± 31. 83） μg·h·m L- 1. The main pharmacokinetic parameters of single oral linezolid tablet of 600 mg under fed condition were as follows： Cmax（ 9. 79 ± 1. 92） μg·m L- 1,tmax（ 2. 66 ± 1. 27） h,t1 /2（ 5. 57 ± 2. 67） h,AUC0- ∞（ 93. 9 ± 34. 7） μg·h·m L- 1. Conclusion After receiving single dose of linezolid tablets 600 mg,human plasma concentrations of fed group were lower than those of fasting group within 24 h. The pharmacokinetic parameters of two groups are basically in consistent with the report abroad.