Vardenafil, a remedy for erectile dysfunction, is easily modified, facilitating the creation of analogues that have been illegally added to functional foods and counterfeit medications. However, the medical profile of these analogues, including their safety, efficacy, safe drug combinations, metabolism and excretion, has not been completely evaluated, which could cause serious health problems. In this study, two representative vardenafil analogues, pseudovardenafil and hydroxyvardenafil, were metabolized with in-vitro model (human liver microsome) and in-vivo model (rats). The metabolized samples were extracted and characterized, using liquid chromatography quadrupole-time of flight mass spectrometry (LC-Q-TOF-MS). Some imprecise interpretations were evaluated with tandem mass spectrometry (LC-Q-TOF-MS/MS) for mass fragmentation analysis. A total of 11 metabolites of pseudovardenafil and 13 metabolites of hydroxyvardenafil that were identified have never been reported. These new metabolites could be usefully applied to forensic science and other metabolic fields. Furthermore, they could serve as principal references for the toxicity, danger, and side effects of unlawful vardenafil counterfeits.

中文翻译：

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伐地那非类似物的代谢研究：Pseudovardenafil和hydroxyvardenafil。

伐地那非是一种勃起功能障碍的药物，可以轻松地进行修饰，从而有助于创建已被非法添加到功能性食品和假药中的类似物。但是，这些类似物的医学特性，包括其安全性，功效，安全的药物组合，代谢和排泄，尚未得到完整评估，这可能会导致严重的健康问题。在这项研究中，两种代表性的伐地那非类似物，伪vardenafil和hydroxyvardenafil被体外模型（人肝微粒体）和体内模型（大鼠）代谢。使用液相色谱四极杆飞行时间质谱（LC-Q-TOF-MS）提取并表征代谢的样品。串联质谱分析（LC-Q-TOF-MS / MS）对一些不精确的解释进行了质量碎片分析。从未报告过总共鉴定出11种假vardenafil代谢物和13种羟基vardenafil代谢物。这些新的代谢产物可有效地应用于法医学和其他代谢领域。此外，它们可以作为非法伐地那非假冒产品的毒性，危险和副作用的主要参考。