目的 建立UPLC-MS/MS法測定人血漿中艾司奧美拉唑濃度，并應(yīng)用于人體生物等效性研究。方法 采用UPLCMS/MS法，以艾司奧美拉唑-d3為內(nèi)標(biāo)，ACE 3 C₁₈-AR （50 mm×2.1 mm，3 μm）為分析柱，流動相A為5 mmol·L^-1乙酸銨水溶液，流動相B為乙腈，體積流量為0.6 mL·min-1進行梯度洗脫；采用電噴霧離子源，以多反應(yīng)監(jiān)測（MRM）正離子模式進行檢測，用于定量分析的離子對為m/z 346.1→198.1（艾司奧美拉唑）、m/z 349.1→198.1（艾司奧美拉唑-d3）。應(yīng)用建立的方法測定人血漿中艾司奧美拉唑濃度，并計算生物等效性。結(jié)果 艾司奧美拉唑在3~3 000 ng·mL^-1范圍線性關(guān)系良好（r ≥ 0.999 4），批內(nèi)、批間精密度和準(zhǔn)確度、回收率、基質(zhì)效應(yīng)及穩(wěn)定性均符合生物樣品測定要求。應(yīng)用該方法進行人體生物等效性樣品測定，證明受試制劑和參比制劑生物等效。結(jié)論 建立的人血漿中艾司奧美拉唑濃度測定方法準(zhǔn)確、靈敏、選擇性好、重現(xiàn)性高，可用于受試者單次口服40 mg艾司奧美拉唑鎂腸溶干混懸劑的生物等效性研究，受試制劑和參比制劑生物等效。

Objective To established and validated a UPLC-MS/MS method for the determination of esomeprazole in human plasma, which was applied to bioequivalence study. Methods UPLC-MS/MS method using esomeprazole-d3 as the internal standard(IS) was used to determine esomeprazole in human plasma. The determination was performed on ACE 3 C₁₈-AR (50 mm×2.1 mm, 3 μm) with a linear gradient, the flow rate was 0.6 mL·min-1. The mobile phase A consisted of water containing 5 mmol·L^-1 ammonium acetate, the mobile phase B consisted of acetonitrile. The ion transitions under multiple reaction monitoring (MRM) mode by ESI⁺ ionization were performed at m/z 346.1→198.1 and m/z 349.1→198.1 for carbamazepin and esomeprazole-d3. The established method was used to determine the concentration of esomeprazole in human plasma in the bioequivalence study. Results The liner range of esomeprazole were 3-3 000 ng·mL^-1(r ≥ 0.999 4). The intra-day and inter-day accuracies and precisions, the recoveries and matrix effects, and the sample stability were all suitable to the biological samples determination. The method was applied to determine human plasma samples of bioequivalence study, and it was proved that the test preparation and the reference preparation were bioequivalent. Conclusion The method was proved to be highly accurate, sensitive, selective, and suitable for the bioequivalence study of esomeprazole in healthy Chinese volunteers after a single oral dose of 40 mg esomeprazole suspension. The test preparation and the reference preparation were bioequivalent.

R969.1