利奈唑胺片在中国健康受试者中的生物等效性研究  

Bioequivalence of linezolid tablets in Chinese healthy subjects

作　　者：赵彩芸[1] 吕媛[1] 魏敏吉[1] 崔洪[1] 张朴[1] 夏亚红[1] 田继红[1] 马雁[1] 刘燕[1] 王茜 吴景 王雅泰 潘梅 ZHAO Cai-yun;LüYuan;WEI Min-ji;CUI Hong;ZHANG Pu;XIA Ya-hong;TIAN Ji-hong;MA Yan;LIU Yan;WANG Xi;WU Jing;WANG Ya-tai;PAN Mei(Institute of Clinical Pharmacology,Peking University First Hospital,Beijing 100034,China;Guilin Pharmaceutical Co.Ltd.,Guilin 541004,Guangxi Zhuang Autonomous Region,China)

机构地区：[1]北京大学第一医院临床药理研究所,北京100034 [2]桂林南药股份有限公司,广西壮族自治区桂林541004

出　　处：《中国临床药理学杂志》2022年第11期1227-1231,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的评价2种利奈唑胺片在中国健康受试者的生物等效性。方法按单中心、随机、开放、单剂量、两制剂、两序列、双周期、交叉研究设计方法,随机交叉单次口服利奈唑胺片受试制剂与参比制剂600 mg,空腹状态下28例受试者完成试验,餐后状态下27例受试者完成试验,用LC-MS/MS法测定血浆中利奈唑胺的浓度,用WinNonlin 6.4软件按非房室模型计算药代动力学参数,并进行生物等效性评价。结果受试者口服利奈唑胺片受试制剂与参比制剂600 mg后,在空腹状态下给药的血浆主要药代动力学参数如下:C_(max)分别为(15.88±4.31)和(15.34±4.56)μg·mL^(-1),t_(max)分别为(1.08±0.98)和(1.22±0.92)h,AUC_(0-t)分别为(111.22±32.45)和(114.86±39.54)μg·mL^(-1)·h,AUC_(0-∞)分别为(117.72±35.09)和(120.38±42.47)μg·mL^(-1)·h;在餐后状态下给药的血浆主要药代动力学参数如下:C_(max)分别为(13.84±3.44)和(13.00±3.13)μg·mL^(-1),t_(max)分别为(2.06±1.02)和(1.88±1.13)h,AUC_(0-t)分别为(104.05±42.71)和(100.58±42.90)μg·mL^(-1)·h,AUC_(0-∞)分别为(110.29±44.61)和(107.56±45.46)μg·mL^(-1)·h。2种制剂的C_(max)、AUC_(0-t)和AUC_(0-∞)经对数转换后90%置信区间在空腹状态下分别为96.71%~112.66%,92.71%~103.20%和93.56%~104.71%;在餐后状态下分别为97.31%~117.12%,94.52%~114.07%和93.45%~113.55%。结论无论空腹还是餐后单次口服2种利奈唑胺片在中国健康受试者体内均具有生物等效性。Objective To evaluate the bioequivalence of the two linezolid tablets in Chinese healthy subjects.Methods This was a single-center,randomized,open label,single dose,two preparation,two period,crossover design.A total of 28 subjects in fasting state and 27 subjects in fed state were given single oral dose 600 mg of test and reference linezolid tablets.The concentrations of linezolid in plasma were determined by LC-MS/MS method.The pharmacokinetic parameters were calculated and the bioequivalence was compared by non-compartment model of WinNonlin 6.4 program.Results The main pharmacokinetics parameters of test and reference preparations of linezolid were as follows:in fasting state,C_(max) were(15.88±4.31)and(15.34±4.56)μg·mL^(-1),t_(max) were(1.08±0.98)and(1.22±0.92)h,AUC_(0-t) were(111.22±32.45)and(114.86±39.54)μg·mL^(-1)·h,AUC_(0-∞)were(117.72±35.09)and(120.38±42.47)μg·mL^(-1)·h;in fed state,C_(max) were(13.84±3.44)and(13.00±3.13)μg·mL^(-1),t_(max) were(2.06±1.02)and(1.88±1.13)h,AUC_(0-t) were(104.05±42.71)and(100.58±42.90)μg·mL^(-1)·h,AUC_(0-∞)were(110.29±44.61)and(107.56±45.46)mg·L^(-1)·h.The 90%CIs for C_(max),AUC_(0-t) and AUC_(0-∞)in fasting state were 96.71%-11266%,92.71%-103.20%and 93.56%-104.71%;in fed state were 97.31%-117.12%,94.52%-114.07%and 93.45%-113.55%,respectively.Conclusion The exposures were equivalent between two linezolid tablets administered in fasting or fed state in Chinese healthy subjects.

关 键 词：利奈唑胺片 中国健康受试者 生物等效性 

分 类 号：R978.1[医药卫生—药品]