Department of Experimental and Clinical Pharmacology, University of Rzeszów, Kopisto 2a, 35-959 Rzeszow, Poland.
Laboratory for Innovative Research in Pharmacology, University of Rzeszów, Kopisto 2a, 35-959 Rzeszow, Poland.
Molecules. 2022 Mar 14;27(6):1883. doi: 10.3390/molecules27061883.
Vortioxetine (VOR) is a new antidepressant drug used to treat major depressive disorder. In this work, a novel, simple, rapid, accurate, precise, selective, stability-indicating, and fully validated high-performance liquid chromatography method with diode array detection (HPLC-DAD) was developed to determine VOR in bulk and pharmaceutical formulations. A Polar-RP column was used, with a mobile phase consisting of acetonitrile (ACN), methanol (MeOH), acetate buffer pH 3.5, and addition of diethylamine (DEA) in the isocratic elution mode. Assessing the stability of the VOR is fundamental to guarantee the efficacy, safety, and quality of drug products. In this study, the VOR active pharmaceutical ingredient (API) and tablets were subjected to a detailed study of forced degradation, using several degrading agents (acid, alkaline, water, heat, light, and oxidation agents). The developed HPLC-DAD method allows the collection of all the essential data to determine degradation kinetics. It was found that the decomposition of vortioxetine is fragile towards oxidative conditions and photolysis, yielding the first-order and second-order kinetic reaction in the above stress conditions, respectively. The degradation products (DPs) were identified by the high-resolution liquid chromatography coupled with electrospray ionization-quadrupole-time of flight-mass spectrometry (LC-ESI-QTOF-MS) method. The HPLC-DAD method was successfully applied for the quantification of VOR in tablets. Additionally, in silico toxicity prediction of the DPs was performed.
文拉法辛(VOR)是一种新型抗抑郁药,用于治疗重度抑郁症。在这项工作中,开发了一种新颖、简单、快速、准确、精密、选择性、稳定性指示且完全验证的高效液相色谱法-二极管阵列检测(HPLC-DAD),用于测定原料药和药物制剂中的文拉法辛。采用极性 RP 柱,以乙腈(ACN)、甲醇(MeOH)、醋酸缓冲液 pH3.5 和添加二乙胺(DEA)为流动相,采用等度洗脱模式。评估文拉法辛的稳定性对于保证药物产品的疗效、安全性和质量至关重要。在这项研究中,对文拉法辛原料药(API)和片剂进行了详细的强制降解研究,使用了几种降解剂(酸、碱、水、热、光和氧化剂)。开发的 HPLC-DAD 方法可以收集所有必要的数据来确定降解动力学。结果发现,文拉法辛在氧化条件和光解下容易分解,分别在上述应激条件下产生一级和二级动力学反应。通过高分辨液相色谱-电喷雾电离-四极杆飞行时间质谱联用(LC-ESI-QTOF-MS)方法鉴定了降解产物(DPs)。HPLC-DAD 方法成功应用于片剂中 VOR 的定量。此外,还对 DPs 进行了计算机毒性预测。