Department of Medicinal Chemistry, Medical University of Lublin, 20-090 Lublin, Poland.
Department of Cancer Genetics with Cytogenetics Laboratory, Medical University of Lublin, 20-080 Lublin, Poland.
Molecules. 2021 May 13;26(10):2903. doi: 10.3390/molecules26102903.
High performance liquid chromatography with ultra-violet detection (HPLC-UV) and gas chromatography-mass spectrometry (GC-MS) methods were developed and validated for the determination of chlorambucil (CLB) and valproic acid (VPA) in plasma, as a part of experiments on their anticancer activity in chronic lymphocytic leukemia (CLL). CLB was extracted from 250 µL of plasma with methanol, using simple protein precipitation and filtration. Chromatography was carried out on a LiChrospher 100 RP-18 end-capped column using a mobile phase consisting of acetonitrile, water and formic acid, and detection at 258 nm. The lowest limit of detection LLOQ was found to be 0.075 μg/mL, showing sufficient sensitivity in relation to therapeutic concentrations of CLB in plasma. The accuracy was from 94.13% to 101.12%, while the intra- and inter-batch precision was ≤9.46%. For quantitation of VPA, a sensitive GC-MS method was developed involving simple pre-column esterification with methanol and extraction with hexane. Chromatography was achieved on an HP-5MSUI column and monitored by MS with an electron impact ionization and selective ion monitoring mode. Using 250 µL of plasma, the LLOQ was found to be 0.075 μg/mL. The accuracy was from 94.96% to 109.12%, while the intra- and inter-batch precision was ≤6.69%. Thus, both methods fulfilled the requirements of FDA guidelines for the determination of drugs in biological materials.
建立并验证了高效液相色谱-紫外检测(HPLC-UV)和气相色谱-质谱联用法(GC-MS),用于测定血浆中的苯丁酸氮芥(CLB)和丙戊酸(VPA),这是它们在慢性淋巴细胞白血病(CLL)中的抗癌活性实验的一部分。CLB 用甲醇从 250 µL 的血浆中提取,采用简单的蛋白沉淀和过滤。在 LiChrospher 100 RP-18 端封柱上,使用乙腈、水和甲酸的流动相进行色谱分离,检测波长为 258nm。发现最低检测限 LLOQ 为 0.075 μg/mL,与 CLB 在血浆中的治疗浓度相比具有足够的灵敏度。准确度在 94.13%至 101.12%之间,而批内和批间精密度均≤9.46%。对于 VPA 的定量,建立了一种灵敏的 GC-MS 方法,涉及用甲醇进行简单的柱前酯化和用己烷提取。在 HP-5MSUI 柱上进行色谱分离,采用电子轰击电离和选择离子监测模式进行 MS 监测。使用 250 µL 的血浆,LLOQ 为 0.075 μg/mL。准确度在 94.96%至 109.12%之间,而批内和批间精密度均≤6.69%。因此,这两种方法均符合 FDA 指南中关于生物材料中药物测定的要求。