CAJ | 학술논문

目的：建立人血清帕拉德福韦浓度检测方法并运用于人体药代动力学研究。方法：血清样品乙腈沉淀蛋白处理后，采用液相色谱串联质谱（LC-MS/MS）法测定。以0.2 mmol·L-1乙酸铵水溶液（A）-乙腈（B）为流动相，Thermo BDS HYPERSIL C18 column（150 mm×2.1 mm，5μm）分离，梯度洗脱。帕拉德福韦及内标（恩替卡韦）监测离子对为m/z 424.1→151.0；m/z 278.3→152.1。运用建立的方法测定健康受试者血清中药物浓度。结果：帕拉德福韦血清药物浓度在0.5~500 ng·mL-1的范围内线性关系良好，方法回收率、日内及日间精密度均符合方法学要求。结论：该方法专属性强、灵敏度高，可用于帕拉德福韦人体药动学研究。
목적：건립인혈청파랍덕복위농도검측방법병운용우인체약대동역학연구。방법：혈청양품을정침정단백처리후，채용액상색보천련질보（LC-MS/MS）법측정。이0.2 mmol·L-1을산안수용액（A）-을정（B）위류동상，Thermo BDS HYPERSIL C18 column（150 mm×2.1 mm，5μm）분리，제도세탈。파랍덕복위급내표（은체잡위）감측리자대위m/z 424.1→151.0；m/z 278.3→152.1。운용건립적방법측정건강수시자혈청중약물농도。결과：파랍덕복위혈청약물농도재0.5~500 ng·mL-1적범위내선성관계량호，방법회수솔、일내급일간정밀도균부합방법학요구。결론：해방법전속성강、령민도고，가용우파랍덕복위인체약동학연구。
Objective: To set up a liquid chromatographic-tandem mass spectrometric (LC/MS/MS) method for the determination of pradefovir in human serum and to apply it to the clinical pharmacokinet-ics. Methods: The serum sample was precipitated by acetonitrile, and the supernatant was analyzed by LC-MS/MS. Chromatographic separation was performed on a Thermo BDS HYPERSIL C18 column (150 mm× 2.1 mm, 5μm) with a gradient elution system of 0.2 mmol·L-1 ammonium acetate buffer - acetonitrile at a flow-rate of 0.3 mL·min-1. The ion transitions recorded in multiple reaction monitoring mode were m/z 424.1([M+H]+) →151.0 for pradefovir and m/z 278.3([M+H]+) →152.1 for the internal standard. The estab-lished method was used to determine the serum concentration of pradefovir in healthy subjects. Results:The linear range of calibration curves for pradefovir was 0.5-500 ng·mL-1. The recovery and the intra-and inter-assay precisions met the requirements of bioanalytical methods. Conclusions: The method is proven to be rapid, specific and sensitive. It can be used for the clinical pharmacokinetic study.