目的 建立简单、快速、灵敏的测定大鼠血浆中阿齐沙坦血药浓度的HPLC-荧光分析方法。方法 色谱柱为Aglient Epilent plus C₁₈（250 mm×4.6 mm，5 μm），流动相为0.1%磷酸水溶液-甲醇（35∶65），激发波长为265 nm，吸收波长为378 nm。结果 血浆中内源性物质对待测物无干扰；线性范围为0.1～100 μg/mL，R²=0.999；定量下限为0.1 μg/mL；高中低浓度样品提取回收率在87.76%～95.65%，批内批间精密度RSD在0.86 %～1.87%，相对误差RE均小于5%，符合相关生物样品检测标准。SD大鼠ig给予2.0 g/kg的阿齐沙坦酯钾后，阿齐沙坦在大鼠体内AUC_0-t为（5451.94±297.96）μg/L·h，C_max为（258.01±49.75）μg/mL。结论 建立了专属性强、灵敏度高、重复性好的HPLC-荧光分析方法，可用于阿齐沙坦在大鼠血浆中血药浓度测定。

Objective To establish a HPLC-fluorescence method for determination of concentration of Azilsartan in rat plasma. Methods Chroma-tographic column: Aglient Epilent plμs C₁₈ (250 mm×4.6 mm, 5 μm); Mobile phase was 0.1% phosphoric acid solution and methanol (35:65); Excitation wavelength was 265 nm; Ereceiver wavelength was 378 nm. Results Endogenous substance in plasma samples had no effect on result. Calibration curves were linear over 0.1-100 μg/mL (R²=0.999) and the minimum detection concentration was 0.1 μg/mL. The recoveries of azilsartan from plasma were between 87.76% and 95.65%. The RSD values of intra and inter-day were between 0.86%-1.87%. The accuracy (RE%) was blow 5%. After i.g. of 2 000 mg/kg Azilsartan, the pharmacokinetics parameters were estimated as follows: AUC_0-t values were (5 451.94±297.96) μg/L·h and C_max were (258.01±49.75) μg/mL. Conclusion A sensitive and reliable HPLC-fluorescence method is developed, and it can be used for determination of concentration of Azilsartan in rat plasma.

中药复方生殖发育毒性及毒代动力学关键技术研究（2015ZX09501004-002-001）