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建立测定人血浆中阿那曲唑浓度的方法。方法:用气相色谱-电子捕获法分离分析阿那曲唑和内标物(地西泮),采用50％苯基甲基础酮毛细管柱(30m×0.53mm,0.5μm),以高纯氮(99.999％)为载气,压力为170kPa,尾吹为60mL·min~(-1)。进样口温度为260℃,炉温为220℃。~(63)Ni电子捕获测器,检测器温度为260℃。血样在碱性条件下,用甲基叔丁醚1次提取。结果:血药浓度测定的线性范围为1.325～106μ·L~(-1)。低、中、高血药浓度(5.3,21.2,53.0μg·L~(-1))提取回收率分别为76.8％,87.0％,78.7％。日内和日间精密度均小于9％。20名中国健康男性志愿者单剂量口服阿那曲唑2mg后,0.55～132h内血药浓度在2.8～53.2μg·L~(-1)的范围内。结论:该法简便、准确、灵敏,可用于阿那曲唑生物利用度和药代动力学研究。
A method for the determination of anastrozole concentration in human plasma was established. Methods: Anastrozole and internal standard substance (diazepam) were separated and analyzed by gas chromatography - electron capture method. The column was eluted with 50% phenylmethyl ketal capillary column (30m × 0.53mm, 0.5μm) %) As the carrier gas, pressure of 170kPa, tail blowing 60mL · min ~ (-1). Inlet temperature is 260 ° C and furnace temperature is 220 ° C. ~ (63) Ni electron capture detector, the detector temperature is 260 ℃. Blood samples were extracted once with methyl tert-butyl ether under alkaline conditions. Results: The linear range of plasma concentration was 1.325 ~ 106μ · L -1. The recoveries of low, middle and high plasma concentrations (5.3, 21.2 and 53.0 μg · L -1) were 76.8%, 87.0% and 78.7%, respectively. Intra- and inter-day precision are less than 9%. Twenty healthy Chinese male volunteers received a single oral dose of anastrozole 2 mg and the plasma concentration ranged from 2.8 to 53.2 μg · L -1 within 0.55 to 132 hours. Conclusion: The method is simple, accurate and sensitive and can be used for the bioavailability and pharmacokinetics of anastrozole.