Department of Pharmacy, The First Affiliated Hospital of Xi'an Jiaotong University, Xi'an, China.
Health Science Center, Xi'an Jiaotong University, Xi'an, China.
Eur J Mass Spectrom (Chichester). 2022 Jun;28(3-4):81-88. doi: 10.1177/14690667221128934. Epub 2022 Sep 22.
Zanubrutinib (BGB-3111) belongs to the class of irreversible inhibitors of Bruton's tyrosine kinase (BTK) for treating B-cell malignancies. A validated assay with excellent sensitivity, selectivity, and simplicity is required to measure plasma concentration and investigate its pharmacokinetics. The plasma of mice containing zanubrutinib and roxithromycin (internal standard) was processed with acetonitrile for protein precipitation. Then the supernatant was analyzed by high-performance liquid chromatography coupled with a triple quadrupole mass spectrometer using electrospray ionization in the positive mode. Zanubrutinib was given to mice intragastrically at 30 mg/kg to determine its pharmacokinetic parameters. The method was verified and showed good linearity in the range of 0.1-100 ng/mL. The method's sensitivity, accuracy, and precision were all within acceptable bounds. By this method, the pharmacokinetic profile of zanubrutinib in mouse plasma was measured.
赞布替尼（BGB-3111）属于布鲁顿酪氨酸激酶（BTK）不可逆抑制剂，用于治疗 B 细胞恶性肿瘤。需要建立一种灵敏、专属性强、操作简便的方法来测定血浆浓度并研究其药代动力学。含赞布替尼和罗红霉素（内标）的小鼠血浆经乙腈沉淀蛋白后，采用电喷雾离子源正离子模式，在高效液相色谱-串联质谱系统中进行分析。以 30mg/kg 剂量灌胃给予小鼠赞布替尼，测定其药代动力学参数。该方法经过验证，在 0.1-100ng/mL 范围内线性关系良好。方法的灵敏度、准确度和精密度均符合要求。采用该方法测定了小鼠血浆中赞布替尼的药代动力学特征。
