Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, China.
Bostal Drug Delivery Co., Ltd., Guangzhou, China.
Pak J Pharm Sci. 2023 Jul;36(4):1113-1119.
Fosaprepitant dimeglumine, an injectable phosphorylated prodrug of aprepitant, has been approved for preventing chemotherapy-induced nausea and vomiting. A novel stability-indicating HPLC method was designed and validated to determine process- and degradation-related impurities of fosaprepitant dimeglumine in an injection formulation. Chromatographic separation was done on a NanoChrom C18 (250 mm×4.6 mm, 5µm) column at a column oven temperature of 35C. Mobile phase A had 0.5 M ammonium dihydrogen phosphate solution (pH fixed to 2.2 with orthophosphoric acid) and acetonitrile at 80:20 ratio and mobile phase B had methanol and acetonitrile at 70:30 ratio. The formulations underwent forced degradation conditions, like acidic, basic, thermal oxidation and photolytic conditions. The designed HPLC approach was validated per International Conference of Harmonization (ICH) guidelines, including limit of detection (LOD), specificity, limit of quantitation (LOQ), accuracy, linearity, precision and robustness. The results showed that this method is specific, sensitive, precise, accurate and robust.
福沙匹坦双葡甲胺是一种前体药物，可注射用，为阿瑞匹坦的磷酰化产物，已被批准用于预防化疗引起的恶心和呕吐。设计并验证了一种新的专属性高效液相色谱（HPLC）方法，用于检测注射用福沙匹坦双葡甲胺制剂中的工艺相关及降解相关杂质。色谱分离在 NanoChrom C18（250mm×4.6mm，5μm）柱上进行，柱温为 35℃。流动相 A 为 0.5 M 磷酸二氢铵溶液（用磷酸调 pH 值至 2.2）与乙腈的 80:20 比例，流动相 B 为甲醇与乙腈的 70:30 比例。制剂经历了强制降解条件，如酸性、碱性、热氧化和光解条件。所设计的 HPLC 方法按照国际人用药品注册技术协调会（ICH）指南进行了验证，包括检测限（LOD）、专属性、定量限（LOQ）、准确度、线性、精密度和稳健性。结果表明，该方法专属性强、灵敏度高、精确、准确且稳健。
