【摘要】：目的:建立快速靈敏高效液相色譜-串聯(lián)質(zhì)譜(HPLC-MS/MS)法測定健康女性使用塞克硝唑栓后體內(nèi)塞克硝唑栓的濃度,并研究其在體內(nèi)的藥代動力學(xué)特征。方法:色譜柱Welch Ultimate C_(18)(2.1 mm×50 mm,5μm);流動相:乙腈-0.1%乙酸+5 mmol·L~(-1)乙酸銨水溶液(12∶88,V/V);流速:0.5 mL·min~(-1),進樣量5μL。采用ESI+源,多重反應(yīng)監(jiān)測(MRM)模式,對離子反應(yīng)m/z186.3→128.3(塞克硝唑)和m/z192.4→128.3(Secnidazole-d6)進行監(jiān)測。20名健康女性受試者,單次與多次給藥試驗各10名,分別給予塞克硝唑栓。根據(jù)檢測的血漿中塞克硝唑濃度,用DAS 3.2.7進行數(shù)據(jù)處理以及SPSS 19.0對結(jié)果進行統(tǒng)計分析。結(jié)果:塞克硝唑在0.05~8.0mg·L~(-1)范圍內(nèi)線性良好(r0.99),定量下限0.05 mg·L~(-1),批間、批內(nèi)RSD皆小于15%。健康女性血漿中塞克硝唑栓單劑量C_(max)(3.00±0.96)mg·L~(-1),t_(max)(8.90±2.68)h,t_(1/2)(18.07±2.96)h,AUC_(0-96)(97.78±35.81)mg·L~(-1)·h~(-1),AUC_(0-∞)(101.11±36.96)mg·L~(-1)·h~(-1);多劑量C_(max,ss)(6.01±2.01)mg·L~(-1),t_(max)(7.20±2.86)h,t_(1/2)(21.87±7.60)h,AUC_(ss)(107.15±33.62)mg·L~(-1)·h~(-1),AUC_(0-96)(202.11±82.07)mg·L~(-1)·h~(-1),AUC_(0-∞)(217.47±103.50)mg·L~(-1)·h~(-1)。結(jié)論:該方法靈敏、準(zhǔn)確、可靠,專屬性強,適用于塞克硝唑栓在人體內(nèi)的藥代動力學(xué)研究。
[Abstract]:Objective: to establish a rapid and sensitive high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method for the determination of Sai Ke nitrazole suppository in healthy women after treatment with Sai Ke niazole suppository and to study its pharmacokinetic characteristics. Methods: Welch Ultimate C18 (2.1 mm 脳 50 mm,5 渭 m);) mobile phase: acetonitrile-0.1% acetic acid 5 mmol L ~ (-1) ammonium acetate aqueous solution (12: 8 V / V), flow rate: 0.5 mL min~ (-1), sample volume 5 渭 L. By using ESI source and multiple reaction monitoring (MRM) model, 20 healthy female subjects were monitored for ion-reactive m/z186.3 128.3 (Sai Ke nitrazole) and m/z192.4 128.3 (Secnidazole-d6). 10 healthy women were treated with Sai Ke niazol suppository respectively. According to the concentration of Sai Ke in plasma, the data were processed with DAS 3.2.7 and the results were statistically analyzed by SPSS 19.0. Results: Sai Ke nidazole had a good linearity in the range of 0.05~8.0mg L ~ (-1) (r ~ (0.99), the lower limit of quantification was 0.05 mg L ~ (-1), and the RSD of interassay and intra-assay was less than 15 ~ (-1). 鍋ュ悍濂蟲，

本文編號：2230691