Pharmaceutical Analysis and Testing Department, Jiangsu Kanion Modern Chinese Medicine Institute, Nanjing, China.
State Key Laboratory of Pharmaceutical New-Tech for Chinese Medicine, Jiangsu Kanion Pharmaceutical Co., Ltd, Lianyungang, China.
Biomed Chromatogr. 2022 Jul;36(7):e5375. doi: 10.1002/bmc.5375. Epub 2022 Apr 13.
Qiwei Tongbi oral liquid (QWTB), a classical traditional Chinese medicine formula, is widely used to treat arthritis-related diseases in clinical practice. Currently, in vivo metabolic characteristics and pharmacokinetic studies are lacking. This study analyzed the prototype components of QWTB absorbed in the blood and their metabolic transformation process after intragastric administration and compared the differences in pharmacokinetic properties between healthy and rheumatoid arthritis model rats. In sum, 17 prototype components and 21 related metabolites were identified in the plasma and urine of the treated rats. Metabolites were derived from sinomenine and magnoflorine. Through systematic methodology verification, an accurate and stable detection method for sinomenine and magnoflorine in plasma samples was established and applied to pharmacokinetic research of QWTB. At the three dose levels, the AUC (area under the curve) of the two components showed a good positive correlation with the dose (R > 0.9). Compared with healthy rats, the T , t , and AUC of sinomenine were markedly increased, and C was decreased in rheumatoid arthritis model rats, indicating that the rate of absorption and elimination rate decreased, but the body exposure increased. However, there were no significant differences in the pharmacokinetic parameters of magnoflorine under healthy and pathological conditions. In summary, the main active ingredients of QWTB are sinomenine and magnoflorine, which exhibit linear kinetic characteristics within a set dose range, and the rheumatoid arthritis pathological state is more conducive to the absorption and efficacy of sinomenine. The results of this study demonstrate the rationality of the clinical application of the QWTB.
芪卫通痹口服液（QWTB）是一种经典的中药方剂，广泛用于临床治疗关节炎相关疾病。目前，体内代谢特征和药代动力学研究尚缺乏。本研究分析了灌胃给药后吸收到血液中的 QWTB 原型成分及其代谢转化过程，并比较了健康和类风湿关节炎模型大鼠之间药代动力学特性的差异。总之，在处理大鼠的血浆和尿液中鉴定出 17 种原型成分和 21 种相关代谢产物。代谢产物来源于青藤碱和粉防己碱。通过系统的方法学验证，建立并应用于 QWTB 药代动力学研究的血浆样品中青藤碱和粉防己碱的准确、稳定的检测方法。在三个剂量水平下，两个成分的 AUC（曲线下面积）与剂量呈良好的正相关（R > 0.9）。与健康大鼠相比，类风湿关节炎模型大鼠中青藤碱的 T 、 t 和 AUC 明显增加，C 降低，表明吸收速率和消除率降低，但机体暴露增加。然而，在健康和病理条件下，粉防己碱的药代动力学参数没有显著差异。总之，QWTB 的主要活性成分是青藤碱和粉防己碱，在设定剂量范围内表现出线性动力学特征，类风湿关节炎病理状态更有利于青藤碱的吸收和疗效。本研究结果证明了 QWTB 临床应用的合理性。
