目的 建立簡單、快速、靈敏的測定大鼠血漿中阿齊沙坦血藥濃度的HPLC-熒光分析方法。方法 色譜柱為Aglient Epilent plus C₁₈（250 mm×4.6 mm，5 μm），流動相為0.1%磷酸水溶液-甲醇（35∶65），激發(fā)波長為265 nm，吸收波長為378 nm。結(jié)果 血漿中內(nèi)源性物質(zhì)對待測物無干擾；線性范圍為0.1～100 μg/mL，R²=0.999；定量下限為0.1 μg/mL；高中低濃度樣品提取回收率在87.76%～95.65%，批內(nèi)批間精密度RSD在0.86 %～1.87%，相對誤差RE均小于5%，符合相關(guān)生物樣品檢測標(biāo)準(zhǔn)。SD大鼠ig給予2.0 g/kg的阿齊沙坦酯鉀后，阿齊沙坦在大鼠體內(nèi)AUC_0-t為（5451.94±297.96）μg/L·h，C_max為（258.01±49.75）μg/mL。結(jié)論 建立了專屬性強(qiáng)、靈敏度高、重復(fù)性好的HPLC-熒光分析方法，可用于阿齊沙坦在大鼠血漿中血藥濃度測定。

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.

中藥復(fù)方生殖發(fā)育毒性及毒代動力學(xué)關(guān)鍵技術(shù)研究（2015ZX09501004-002-001）