Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Students' University Hospital, Mansoura University, Mansoura 35516, Egypt.
Molecules. 2022 Dec 18;27(24):9038. doi: 10.3390/molecules27249038.
Vandetanib (Caprelsa; VNB) is a prescription medicine that is used for the treatment of medullary thyroid cancer that has disrupted other body parts or that cannot be removed by surgery. It is considered a tyrosine kinase inhibitor (TKI). Fast, sensitive and validated HPLC-UV was established for VNB quantification in pure human biological fluids (urine and plasma) and human liver microsomes (HLMs). This analytical methodology was applied also to the metabolic stability assessment of VNB. This method was performed using a phenyl column (250 mm × 4.6 mm id, 5 µm particle size). A sodium dodecyl sulphate solution (0.05 M, pH 3.0 using 0.02 M orthophosphoric acid) containing 0.3% triethylamine and 10% n-butanol was used as a mobile phase and was pumped isocratically at a flow rate of 0.7 mL/min and at a 260 nm detection wavelength. The total elution time was 6 min with an injection volume of 20 μL. The linearity of the established methodology ranged from 30 to 500 ng/mL in pure form and 50 to 500 ng/mL (r ≥ 0.9994) in human biological fluids and HLMs. No significant interference from the matrix components was observed. The proposed methodology revealed the benefits of being green, reliable and economic.
凡德他尼（Caprelsa；VNB）是一种处方药物，用于治疗已经扩散到身体其他部位或无法通过手术切除的甲状腺髓样癌。它被认为是一种酪氨酸激酶抑制剂（TKI）。建立了快速、灵敏和经过验证的 HPLC-UV 法，用于纯人体生物流体（尿液和血浆）和人肝微粒体（HLMs）中 VNB 的定量。该分析方法也应用于 VNB 的代谢稳定性评估。该方法使用苯基柱（250mm×4.6mm id，5µm 粒径）进行。含有 0.3%三乙胺和 10%正丁醇的十二烷基硫酸钠溶液（0.05M，使用 0.02M 正磷酸调至 pH3.0）用作流动相，并以 0.7mL/min 的流速等度泵出，检测波长为 260nm。总洗脱时间为 6 分钟，进样量为 20μL。建立的方法在纯品中的线性范围为 30-500ng/mL，在人体生物流体和 HLMs 中的线性范围为 50-500ng/mL（r≥0.9994）。未观察到基质成分的显著干扰。所提出的方法具有绿色、可靠和经济的优点。
