人血浆中依非韦伦的LC-MS/MS法测定及人体生物等效性

Determination of Efavirenz in Human Plasma by LC-MS/MS and Bioequivalence in Human Body

建立了液相色谱-串联质谱法测定人血浆中的依非韦伦。以多西他赛为内标,采用ESI源正离子模式、多反应监测（MRM）进行定量分析。依非韦伦在0.05~10μg/ml范围内线性关系良好,方法回收率为96.9%~100.1%,批内RSD≤4.6%,批间RSD≤6.1%。考察了22例男性健康志愿者单次空腹口服依非韦伦片（受试制剂和参比制剂）的生物等效性。两者的AUC和cmax无显著性差异,受试制剂的平均相对生物利用度F为（98.75±35.41）%,表明两制剂生物等效。

An LC-MS/MS method was established for the determination of efavirenz in human plasma. A tandem mass spectrometric detection was conducted using multiple reaction monitoring （MRM） under positive ionization mode with an electrospray ionization （ESI） interface. It was linear for efavirenz in the range of 0.05 - 10 μg/ml. The method recoveries were 96.9 % - 100.1%, with intra-assay RSDs ≤4.6 %, and inter-assay RSDs ≤ 6.1%, respectively. The bioequivalence of the efavirenz test and reference tablets were invesigated after single oral administration to 22 healthy male volunteers under fasting conditions. There was no significant differences of AUC and cmax between the test and reference tablets. The average relative bioavailability （F） of the test preparation was （98.75±35.41） %. The result showed that the test and reference preparations were bioequivalent.