We developed and validated a liquid chromatography–electrospray ionization–time of flight/mass spectrometry method for the determination of abiraterone (Abi) and its metabolites (Δ⁴-Abi, 3-keto-5α-Abi, 3α-OH-5α-Abi and 3β-OH-5α-Abi) in human serum using Abi-d₄ as the internal standard. As a pretreatment procedure of serum samples, solid-phase extraction based on a silica-gel cartridge was used. The relative recovery of Abi and its metabolites was over the ranges of 84.5 – 109.2% at a concentration of 6.0 ng mL⁻¹ for Abi and 0.6 ng mL⁻¹ for its metabolites. The method was free from matrix effects. The calibration curve of Abi was linear over the range of 2.0 – 400 ng mL⁻¹ and those of its metabolites over the ranges 0.2 – 40 ng mL⁻¹. The results of the intra- and inter-day accuracy and precision data were within the FDA acceptance criteria. The optimized method was applied for the determination of Abi and its metabolites in human serum after oral administration of Abi acetate.

我们开发并验证了一种液相色谱-电喷雾电离-飞行时间/质谱法，用于测定阿比特龙 (Abi) 及其代谢物（Δ ⁴ -Abi、3-酮-5α-Abi、3α-OH-5α-Abi和 3β-OH-5α-Abi) 在人血清中使用 Abi- d ₄作为内标。作为血清样品的预处理程序，使用基于硅胶柱的固相萃取。在 Abi 浓度为 6.0 ng mL ^-1和代谢物浓度为0.6 ng mL ^{-1 时}，Abi 及其代谢物的相对回收率在 84.5 – 109.2% 的范围内。该方法没有基质效应。Abi 的校准曲线在 2.0 – 400 ng mL ^-1范围内呈线性及其代谢物的范围为 0.2 – 40 ng mL ^-1。日内和日间准确度和精密度数据的结果在 FDA 验收标准范围内。将优化后的方法用于测定口服醋酸阿比后人血清中阿比及其代谢物。