A simple, rapid, and sensitive method of liquid chromatography-tandem mass spectrometry (LC/MS/MS) method was developed and validated for the determination of vardenafil in rabbit plasma. A simple protein precipitation method with ice-cold acetonitrile was used for plasma extraction. The mass transitions m/z 489⟶151 and m/z 390⟶169 were used to measure vardenafil and tadalafil (internal standard), respectively, with a total assay run time of 6 min. The limit of detection was 0.2 ng/mL. The assay was reproducible with intra-assay and interassay precision ranging 1.17%–9.17% and 1.31%–5.86%, respectively. There was also good intra-assay and interassay accuracy between 89.3%–105.3% and 94%–102% of the expected value, respectively. The linearity range was 0.5–60 ng/mL in rabbit plasma ( ≥ 0.99). The measured AUC from 0 to 24 h for the test and reference formulations were 174.38 ± 95.91 and 176.45 ± 76.88, respectively. For the test, and were 75.36 ± 59.53 ng/mL and 1.42 ± 0.19 h, whereas, for the reference, these were 58.22 ± 36.11 ng/mL and 2.04 ± 0.33 h, respectively. The test formulation achieved a slightly lower value ( > 0.05), higher values ( > 0.05), faster ( < 0.05), and almost equal bioavailability compared with the reference formulation.

中文翻译：

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液相色谱-串联质谱法测定伐地那非及其生物等效性应用


开发并验证了一种简单、快速、灵敏的液相色谱-串联质谱 (LC/MS/MS) 方法，用于测定兔血浆中的伐地那非。使用冰冷乙腈的简单蛋白质沉淀方法用于血浆提取。质量转变 m/z 489⟶151 和 m/z 390⟶169 分别用于测量伐地那非和他达拉非（内标），总检测运行时间为 6 分钟。检测限为0.2 ng/mL。该测定具有重复性，测定内和测定间精度分别为 1.17%–9.17% 和 1.31%–5.86%。测定内和测定间准确度也良好，分别为预期值的 89.3%–105.3% 和 94%–102%。兔血浆中的线性范围为 0.5–60 ng/mL (≥ 0.99)。测试制剂和参比制剂在 0 至 24 小时内测得的 AUC 分别为 174.38 ± 95.91 和 176.45 ± 76.88。对于测试， 和 分别为 75.36 ± 59.53 ng/mL 和 1.42 ± 0.19 h，而对于参考，这些分别为 58.22 ± 36.11 ng/mL 和 2.04 ± 0.33 h。与参考制剂相比，测试制剂实现了略低的值（> 0.05）、更高的值（> 0.05）、更快（< 0.05）和几乎相同的生物利用度。