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目的建立测定人血浆中赖诺普利浓度的液相色谱一串联质谱(LC—MS—MS)法,评价赖诺普利试验片与参比片的生物等效性。方法 20名志愿者随机单剂量双交叉口服赖诺普利试验片和参比片10mg,采用沉淀蛋白法预处理血浆样品后,进行 LC-MS-MS 法测定。结果试验片和参比片中药物主要药动学参数如下:c_(max)分别为(54±21)和(53±23)μg·L~(-1),t_(max)分别为(6.4±1.4)和(6.7±1.1)h,AUC(0～36)。分别为(569±244)和(566±269)μg·h·L~(-1),AUC_(0-∞)分别为(589±250)和(587±268)μg·h·L~(-1);按 AUC_(0～36)计算,赖诺普利试验片的相对生物利用度为(102±8)%。结论本方法操作简单,灵敏度,准确度、精密度和定量分析线性关系均良好,符合生物样品测定要求;经统计学检验,试验片与参比片生物等效。
Objective To establish a liquid chromatography-tandem mass spectrometry (LC-MS-MS) method for the determination of lisinopril in human plasma to evaluate the bioequivalence of lisinopril and reference tablets. Methods Twenty volunteers were randomized to receive lisinopril test and reference tablets 10mg twice daily randomly. The plasma samples were pretreated with precipitated protein and analyzed by LC-MS-MS. Results The main pharmacokinetic parameters of the drugs in the test tablets and the reference tablets were as follows: c max were 54 ± 21 and 53 ± 23 μg · L -1, and t max were 6.4 ± 1.4) and (6.7 ± 1.1) h, AUC (0-36). (569 ± 244) and (566 ± 269) μg · h · L -1, respectively. The AUC_ (0-∞) were 589 ± 250 and 587 ± 268 μg · h · L ~ -1). The relative bioavailability of lisinopril was (102 ± 8)% based on AUC_ (0 ~ 36). Conclusion The method has simple operation, good linearity of sensitivity, accuracy, precision and quantitative analysis, which meets the requirements of biological samples. The results of statistical tests show that the test samples and reference tablets are bioequivalent.