School of Pharmacy, Shenyang Pharmaceutical University, Benxi, China.
Jiangsu Kanion Pharmaceutical Co. Ltd., Lianyungang, China.
Biomed Chromatogr. 2020 Sep;34(9):e4866. doi: 10.1002/bmc.4866. Epub 2020 Jun 17.
A reliable and sensitive UPLC-MS/MS method was first established and validated for the simultaneous determination of seven active ingredients of Yaobitong capsule in rat plasma: ginsenoside Rg1, ginsenoside Rb1, osthole, tetrahydropalmatine, paeoniflorin, albiflorin, and ferulic acid. And this method was further applied for the integrated pharmacokinetic study of Yaobitong capsule in rats after oral administration. Plasma samples (100 μL) were precipitated with 300 μL of methanol using carbamazepine as internal standard. Chromatographic separation was achieved using an Aquity UPLC BEH C18 column (100 × 2.1 mm, 1.7 μm), with the mobile phase consisting of 0.1% formic acid and acetonitrile. The method was validated using a good linear relationship (r ≥ 0.991), and the lower limit of quantification of the analytes ranged from 0.5 to 40 ng/mL. In the integrated pharmacokinetic study, the weight coefficient was calculated by the ratio of AUC of each component to the total AUC of the seven active ingredients. The integrated pharmacokinetic parameters C , T , and t were 81.54 ± 9.62 ng/mL, 1.00 ± 0.21 h, and 3.26 ± 1.14 h, respectively. The integration of pharmacokinetic parameters showed a shorter t because of fully considering the contribution of the characteristics of each active ingredient to the overall pharmacokinetics.
首次建立并验证了一种可靠且灵敏的 UPLC-MS/MS 方法，用于同时测定大鼠血浆中要必通胶囊的 7 种活性成分：人参皂苷 Rg1、人参皂苷 Rb1、蛇床子素、延胡索乙素、白芍苷、阿魏酸和白花前胡甲素。该方法进一步应用于大鼠口服要必通胶囊后的综合药代动力学研究。用卡马西平作为内标，用 300μL 甲醇沉淀 100μL 血浆样品。采用 Aquity UPLC BEH C18 柱（100×2.1mm，1.7μm）进行色谱分离，流动相由 0.1%甲酸和乙腈组成。该方法具有良好的线性关系（r≥0.991），分析物的定量下限范围为 0.5-40ng/mL。在综合药代动力学研究中，通过各成分 AUC 与 7 种活性成分总 AUC 的比值计算权重系数。综合药代动力学参数 C、T 和 t 分别为 81.54±9.62ng/mL、1.00±0.21h 和 3.26±1.14h。整合药代动力学参数的 t 较短，因为充分考虑了每个活性成分对整体药代动力学的特征贡献。
