高效液相色谱法评价氟康唑片的人体生物等效性  

Bioequivalence Assessment of Fluconazole Tablets in Human Plasma by HPLC

作　　者：陈碧[1] 李莲新[1] 王志华[1] 

机构地区：[1]湖南省郴州市第一人民医院,湖南郴州423000

出　　处：《药物生物技术》2010年第5期438-441,共4页Pharmaceutical Biotechnology

摘　　要：为研究氟康唑片在健康人体内的相对生物利用度,评价不同厂家生产的氟康唑片的生物等效性。采用随机双周期自身交叉对照试验设计,给18名健康男性受试者分别口服受试和参比氟康唑片50mg,采用高效液相色谱法测定给药后不同时间氟康唑的血药浓度,计算主要药物动力学参数,并评价其生物等效性。结果显示受试和参比氟康唑片的Cmax分别为(2.69±0.45)μg/mL和(2.81±0.55)μg/mL;tmax分别为(1.5±0.9)h和(1.6±0.9)h;t1/2分别为(43.3±11.3)h和(41.9±10.0)h;AUC0～t分别为(111.3±18.1)μg/(h.mL)和(109.7±21.4)μg/(h.mL);AUC0～∞分别为(126.4±28.8)μg/(h.mL)和(122.8±28.1)μg/(h.mL)。受试氟康唑片的相对生物利用度为(102.7±10.7)%。结果显示根据双单侧检验表明两种氟康唑片具有生物等效性。To study the bioequivalence of fluconazol tablets supplied by different companies in healthy voluteers,a single oral dose of 50mg test and reference fluconazol（in tablets）was given to 18 healthy male volunteers in a randomized two-period cross-over trial.The plasma drug concentrations at different time were determined by HPLC method using bambuterol as internal standard with a mobile phase of 0.02mol/L phosphate buffer（pH 6.0）and acetonitrile（30∶70 V/V）.The relative bioavailability and main pharmacokinetic parameters of test and reference fluconazol in tablets were calculated and their bioavailability was evaluated.The pharmacokinetic parameters of test and reference fluconazol（in tablets）were as follows：Cmax was（2.69±0.45）μg/mL and（2.81±0.55）μg/mL;tmax was（1.5±0.9）h and（1.6±0.9）h;t1/2 was（43.3±11.3）h and（41.9±10.0）h;AUC0～t was（111.3±18.1）μg/（h·mL）and（109.7±21.4）μg/（h·mL）.AUC0-∞ was（111.3±18.1）μg/（h·mL）and（109.7±21.4）μg/（h·mL）.The average relative bioavailability of test fluconazol in tablets was（102.7±10.7）%.The test and reference formulation are bioequivalent according to two one-side tests.

关 键 词：氟康唑 药动学 生物等效性 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学] R927.2[医药卫生—药学]