Li Qingqing, Chen Xiaohai, Zhang Siping, Li Wanshu, Lin Hangjuan
Department of Pharmacy, Ningbo Municipal Hospital of Traditional Chinese Medicine (TCM), Affiliated Hospital of Zhejiang Chinese Medical University, Ningbo, China.
The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, China.
Front Pharmacol. 2024 Sep 18;15:1470377. doi: 10.3389/fphar.2024.1470377. eCollection 2024.
Riociguat, an orally soluble guanylate cyclase (sGC)-promoting drug, is mainly used in the clinical treatment of pulmonary hypertension (PH). In this study, a novel ultra-performance liquid chromatography-tandem mass spectrometry method was developed to quantify the concentrations of riociguat and its metabolite (M1) in plasma. The precision, stability, accuracy, matrix effect, and recovery of the methodology were satisfactory. Quercetin, a well-recognized compound, functions as a novel anticancer agent with the potential to alleviate symptoms of PH. Therefore, the potential interaction between quercetin and riociguat was investigated in this study. The levels of riociguat and M1 in rat plasma were measured using the method developed in this study to evaluate the interactions between riociguat and quercetin in rats. The results revealed that quercetin significantly inhibited riociguat and M1 metabolism with increased systemic exposure.
利奥西呱是一种口服可溶的鸟苷酸环化酶（sGC）促进药物，主要用于肺动脉高压（PH）的临床治疗。在本研究中，开发了一种新型超高效液相色谱-串联质谱法来定量血浆中利奥西呱及其代谢物（M1）的浓度。该方法的精密度、稳定性、准确性、基质效应和回收率均令人满意。槲皮素是一种广为人知的化合物，作为一种新型抗癌药物，具有缓解PH症状的潜力。因此，本研究对槲皮素与利奥西呱之间的潜在相互作用进行了研究。采用本研究建立的方法测定大鼠血浆中利奥西呱和M1的水平，以评估利奥西呱与槲皮素在大鼠体内的相互作用。结果显示，槲皮素显著抑制利奥西呱和M1的代谢，全身暴露增加。
